CCR2 receptor antagonists and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

New ccr2 receptor antagonists and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of Formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

New ccr2 receptor antagonists and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single bond, ═CH—, —CH—, —O—, —S—, and —NH—; wherein n is 1, 2 or 3; wherein Z is C or N, the other variables are as defined in the claims, as well as in form of their acid addition salts with pharmacologically acceptable acids. 4. The compound of claim 1 , wherein Ris selected from among —H claim 1 , -methyl claim 1 , -ethyl claim 1 , -propyl claim 1 , -1-propyl claim 1 , -cyclopropyl claim 1 , -butyl claim 1 , -i-butyl claim 1 , -t-butyl claim 1 , —F claim 1 , —Cl claim 1 , —Br claim 1 , —I claim 1 , —CN claim 1 , —CH═CH claim 1 , —C≡CH claim 1 , and —OCH.5. The compound of claim 1 , wherein Ris selected from among —H claim 1 , -Methyl claim 1 , -Ethyl claim 1 , —Br claim 1 , and —OCH.6. The compound of claim 1 , wherein Ris selected from among —H claim 1 , and -methyl.9. The compound of claim 1 , wherein Ris selected from among an electron pair claim 1 , —H claim 1 , and —C(O)—NH.10. The compound of claim 1 , wherein Ris selected from among —H claim 1 , —CH claim 1 , —CH claim 1 , —O—CH claim 1 , —O—CH claim 1 , —F claim 1 , —CF claim 1 , and —OCF.11. The compound of claim 1 , wherein Ris H or —O—CH.12. The compound of claim 1 , wherein A is selected from a single bond claim 1 , ═CH— claim 1 , —CH claim 1 , —O— or —NH—.13. The compound of claim 1 , wherein A is selected from among —O— and —NH—.14. The compound of claim 1 , wherein A is —NH—.15. The compound of claim 1 , wherein Z is C or N.16. (canceled)17. A method for the treatment of inflammatory diseases comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to or a pharmacologically acceptable salt thereof.18. The method according to claim 17 , wherein the inflammatory diseases are selected ...

NEW CCR2 RECEPTOR ANTAGONISTS, METHOD FOR PRODUCING THE SAME, AND USE THEREOF AS MEDICAMENTS

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases. 2. The compound of formula (I) according to claim 1 ,{'sub': 1', '1', '4', '3', '3', '6, 'wherein Ris a group selected from among —H, -halogen, —C-C-alkyl, —CF, —OCF, and —C-heteroaryl comprising a N atom;'}{'sub': 7', '1', '4', '3', '3', '6, 'wherein Ris a group selected from among —H, -halogen, —C-C-alkyl, —CF, —OCF, and —C-heteroaryl comprising a N atom; and'}{'sub': '4', 'wherein Rdenotes -hydrogen.'}3. The compound of formula (I) according to claim 1 ,{'sub': 7', '1', '4, 'wherein Rand Ron two neighbouring ring atoms together form a —C-alkenylene group, such that an annellated aromatic ring is formed, in which one or two carbon centers may optionally be replaced by 1 or 2 hetero atoms selected from N;'}{'sub': 4', '1', '3, 'wherein Ris a group selected from among -hydrogen, and —C-C-alkyl.'}4. The compound of formula (I) according to claim 1 , wherein A denotes N.5. The compound of formula (I) according to claim 1 , wherein A denotes C.6. The compound of formula (I) according to claim 1 , wherein Ris selected from among —H claim 1 , —C-C-alkyl claim 1 , and —O—C-C-alkyl.7. The compound of formula (I) according to claim 1 , wherein Ris selected from among -methyl claim 1 , and —OCH.8. The compound of formula (I) according to claim 1 , wherein Rdenotes -hydrogen.9. The compound of formula (I) according to claim 1 , wherein n is 2.10. The compound of formula (I) according to claim 1 , wherein G and E are N.11. The compound of formula (I) according to claim 1 ,{'sub': 5', '10', '10′, 'wherein Ris a group of the structure —N(R,R),'}{'sub': 10', '10′', '4, 'wherein Rand R, together form a —C-alkylene group such that a ring is formed,'}{'sub': 0', '3', '2', '1', '3, 'wherein such ring is optionally substituted with one or more groups ...

NOVEL CCR2 RECEPTOR ANTAGONISTS, METHOD FOR PRODUCING THE SAME, AND USE THEREOF AS MEDICAMENTS

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases. 2. The compound of formula (I) according to claim 1 ,wherein HET is a group according to formula (IIa),{'sub': 1', '7', '6, 'wherein Ris —H, and wherein Ris —C-aryl,'}{'sub': 7', '3', '1', '6', '1', '6, 'and wherein the ring Ris optionally substituted with one or more groups selected from among —CF, —C-C-alkyl, —O—C-C-alkyl, and -halogen'}{'sub': '16', 'and wherein Ris -hydrogen;'}{'sub': 7', '1', '4, 'or wherein Rand Ron two neighbouring ring atoms together form a —C-alkenylene group, such that an annellated aromatic ring is formed, in which one carbon center may optionally be replaced by 1 nitrogen atom,'}{'sub': 1', '3', '3', '3, 'wherein the resulting annelated ring being optionally substituted by one or more groups selected from among —C-C-alkyl, —CN, —CF, —OCF, and -halogen,'}{'sub': '16', 'and wherein Ris a group selected from -hydrogen, and ═O;'}{'sub': 7', '1', '1, 'or wherein Rand Ron two neighbouring ring atoms together form a —C-alkylene group such that an annellated ring is formed,'}{'sub': 5', '10, 'wherein the resulting annelated ring being optionally substituted by a group of the structure —C-C-aryl,'}{'sub': '16', 'and wherein Ris -hydrogen;'}{'sub': 7', '5', '5', '4', '2', '1', '3', '1', '6', '3', '3', '5', '10, 'or wherein Ris a group selected from among spiro —C-cycloalkenyl, and spiro —C-heterocyclyl, wherein said spirocyclic ring being optionally substituted on two neighbouring ring atoms by a —C-alkenylene group, such that an annellated aromatic ring is formed, wherein the aromatic ring being optionally substituted by one or more groups selected from among —OH, —NH, —C-C-alkyl, —O—C-C-alkyl, —CN, —CF, —OCF, halogen, —C-C- ...

Novel antagonists for ccr2 and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

NEW SELECTIVE CCR2 ANTAGONISTS

The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain. 2. The compound of claim 1 ,{'sub': 4', '5', '4', '5', '4', '5, 'wherein Z denotes a five-, or six-membered ring formed by a —C-C-alkylene, wherein the —C-C-alkylene is bi-valently linked to the N atom, and in which one carbon center of the —C-C-alkylene may optionally be replaced by 1 hetero atom selected from N, and O,'}{'sub': 3', '4', '1', '3', '2', '1', '3', '2', '1', '3', '2', '1', '3, 'and wherein the ring Z is further bi-valently substituted on two neighbouring ring atoms, such that an annellated ring is formed by a group selected from among —C-C-alkylene, in which one carbon center may optionally be replaced by 1 hetero atom selected from O, and N, and wherein the bivalent group is optionally substituted by one or more groups selected from —N(C-C-alkyl)-SO—C-C-alkyl, —NH—SO—C-C-alkyl, and —SO—C-C-alkyl.'}7. The compound of claim 1 , wherein Ris a group selected from among —CH claim 1 , —OCH claim 1 , and -cyclopropyl.8. The compound of claim 1 , wherein Ris selected from among —H claim 1 , —CH claim 1 , —OCH claim 1 , —CF claim 1 , and -cyclopropyl.9. The compound of claim 1 , wherein Ris selected from among —H claim 1 , —CH claim 1 , —CH claim 1 , —O—CH claim 1 , —O—CH claim 1 , —F claim 1 , —CF claim 1 , and —OCF.10. The compound of claim 1 , wherein A denotes —NH-L-Rand Lis a bond.11. The compound of claim 1 , wherein G and E are N.12. The compound of claim 1 , wherein n is 2.13. A method for the treatment of an inflammatory disease of the respiratory tract selected from chronic obstructive pulmonary disease claim 1 , asthma claim 1 , and cystic fibrosis claim 1 , comprising administering to a patient in need thereof a therapeutic amount of a compound according to or a pharmacologically acceptable salt thereof.14 ...

NOVEL AND SELECTIVE CCR2 ANTAGONISTS

The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain. 3. The compound of claim 1 ,{'sub': 3', '2', '2', '3, 'wherein Ris a group selected from among —CHF, —CHF, and —CF.'}7. The compound of claim 1 , wherein Ris a group selected from among —H claim 1 , —CH claim 1 , —OCH claim 1 , and -cyclopropyl.8. The compound of claim 1 , wherein Ris selected from among —H claim 1 , —CH claim 1 , —OCH claim 1 , —CF claim 1 , and —OH.9. The compound of claim 1 , wherein Ris selected from among —H claim 1 , —CH claim 1 , —CH claim 1 , —O—CH claim 1 , —O—CH claim 1 , —F claim 1 , —CF claim 1 , and —OCF.10. The compound of claim 1 , wherein Ris a group of the structure -L-R claim 1 ,{'sub': 1', '3, 'wherein Lis selected from among —NH—, and —N(CH)—,'}{'sub': 13', '6, 'wherein Ris —C-heterocyclyl comprising an O atom, and'}{'sub': 13', '1', '4, 'wherein Ris optionally substituted by a group selected from among —O—C-C-alkyl, and -halogen.'}11. The compound of claim 1 , wherein Ris a group of the structure —N(R claim 1 ,R) claim 1 ,{'sub': 1', '1′', '5', '3', '3', '3', '1', '4', '0', '1', '2', '1', '3, 'wherein Rand R, together form a —C-alkylene group such that a ring is formed, wherein one carbon atom may be replaced by a group selected from among O, and wherein such ring is optionally substituted with one or more groups selected from among —OH, —OCH, —CF, —OCF, —CN, -halogen, —C-C-alkyl, ═O, and —N(C-C-alkyl)-SO—C-C-alkyl.'}12. The compound of claim 1 , wherein G and E are N.13. The compound of claim 1 , wherein n is 2.14. A method for the treatment of inflammatory diseases of the respiratory tract selected from chronic obstructive pulmonary disease claim 1 , asthma claim 1 , and cystic fibrosis claim 1 , comprising administering an effective amount of a compound of to a patient in need thereof ...

CCR2 ANTAGONISTS AND USES THEREOF

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. 2. The compound of formula (I) according to claim 1 ,{'sub': 1', '1', '6, 'wherein Ris -L-R,'}{'sub': 1', '1, 'and wherein Lis a bond or wherein Ldenotes methylene,'}{'sub': '6', 'and wherein Ris a ring selected from among -cyclopropyl, -cyclobutyl, -cyclopentyl, -cyclohexyl, -cycloheptyl, -pyrrolidinyl, -piperidinyl, -azepanyl, -tetrahydrofuranyl, -tetrahydropyranyl, -oxepanyl, -phenyl, -pyridyl, and -furanyl,'}{'sub': 6', '3', '3', '1', '3', '3', '3', '3, 'wherein the ring Ris optionally substituted with one or more groups selected from among —F, —Cl, -methyl, -ethyl, -propyl, -i-propyl, -cyclopropyl, -t-butyl, —CF, —O—CF, —CN, —O-methyl, -furanyl and -phenyl, wherein said -phenyl is optionally independently substituted by one or more groups selected from among —C-C-alkyl, halogen, —OCH, —CF, and —OCF.'}3. The compound of formula (I) according to claim 1 ,{'sub': 1', '1', '6, 'wherein Ris -L-R,'}{'sub': 1', '1, 'and wherein Lis a bond or wherein Ldenotes methylene,'}{'sub': 6', '3', '8', '5', '10, 'and wherein Ris a ring selected from among —C-C-heterocyclyl, and —C-C-aryl,'}{'sub': 6', '3', '3', '1', '6, 'wherein the ring Ris optionally substituted with one or more groups selected from among —CF, —O—CF, —CN, —C-C-alkyl, and -halogen,'}{'sub': 6', '1', '6', '5', '10', '5', '10', '3', '3, 'or wherein the ring Ris optionally substituted with one or more groups selected from among —C-C-alkyl, —C-C-aryl, —C-C-heteroaryl optionally being substituted by one or more groups selected from —CF, and —OCF.'}6. The compound of formula (I) according to claim 1 , wherein Rdenotes —CH.7. The compound of formula (I) according to claim 1 , wherein Ris selected from among —H claim 1 , and methyl.8. The compound of formula (I) according to claim 1 , wherein Rdenotes —H.9. ...

NEW CCR2 ANTAGONISTS

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (Ia) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. 2. The compound of formula (I) according to claim 1 ,{'sub': 1', '1', '2', '1', '2, 'wherein A is selected from among —O—, and —NH, and wherein Lis a linker selected from a bond or a group selected from among —C-C-alkylene, and —C-C-alkenylene,'}{'sub': 7', '3', '8', '3', '8', '5', '10', '5', '10, 'and wherein Ris a ring selected from among —C-C-cycloalkyl, —C-C-heterocyclyl, —C-C-aryl, and —C-C-heteroaryl,'}{'sub': 7', '3', '1', '6', '3', '1', '6', '1', '6', '1', '6, 'wherein the ring Ris optionally substituted with one or more groups selected from among —CF, —C-C-alkyl, —O—CF, —CN, —O—C-C-alkyl, —C-C-alkenyl, and —C-C-alkynyl, and -halogen,'}{'sub': 7', '5', '10', '5', '10', '3', '8', '3', '8', '2', '1', '4', '1', '6', '3', '3, 'or wherein the ring Ris optionally substituted with one or more groups selected from among —C-C-aryl, —C-C-heteroaryl, —C-C-cycloalkyl, —C-C-heterocyclyl, optionally being substituted by one or more groups selected from among —OH, —NH, —C-C-alkyl, —O—C-C-alkyl, —CN, —CF, —OCF, halogen, and ═O,'}{'sub': 7', '1', '6', '2', '6', '4', '6', '2', '1', '4', '1', '6', '3', '3, 'or wherein the ring Ris optionally further bi-valently substituted on two neighbouring ring atoms, such that an annellated ring is formed by one or more groups selected from among —C-C-alkylene, —C-C-alkenylene and —C-C-alkynylene, in which one or two carbon centers may optionally be replaced by 1 or 2 hetero atoms selected from N, O and S, the bivalent group being optionally substituted by one or more groups selected from —OH, —NH, —C-C-alkyl, —O—C-C-alkyl, —CN, —CF, —OCF, halogen, and ═O.'}3. The compound of formula (I) according to claim 1 , wherein Lis a linker selected from a bond or —C-C-alkylene.4. The compound of formula (I) according to ...

NOVEL PYRAZOLOPYRIMIDINES

This invention relates to novel pyrazolopyrimidines and their use as metabotropic glutamate 5 receptor antagonists (mGlu5 receptor antagonists), pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of mGlu5 receptor mediated disorders. 2. A method of treating a disease comprising administering an effective amount of a compound according to claim 1 , to a patient in need thereof.3. A pharmaceutical composition comprising at least one compound according to or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable adjuvant claim 1 , diluent and/or carrier.4. A method of treating a disease selected from psychiatric diseases claim 1 , disorders or conditions; neurological diseases claim 1 , disorders or conditions; and pain diseases claim 1 , disorders or conditions claim 1 , comprising administering an effective amount of a compound according to or a pharmaceutically acceptable salt thereof claim 1 , to a patient in need.5. The method of wherein the psychiatric diseases claim 4 , disorders or conditions to be treated are selected from a group consisting of psychotic disorders claim 4 , schizophrenia claim 4 , depression and bipolar mood disorders claim 4 , anxiety disorders claim 4 , general anxiety disorder claim 4 , panic claim 4 , posttraumatic stress claim 4 , phobia claim 4 , acute stress claim 4 , paranoia claim 4 , obsessive or compulsive disorders claim 4 , anorexia claim 4 , bulimia claim 4 , personality disorders claim 4 , failure to thrive claim 4 , sexual dysfunction claim 4 , substance related disorders and disorders of impulse control.6. The method of wherein the neurological diseases claim 4 , disorders or conditions to be treated are selected from a group consisting of epilepsy claim 4 , Alzheimer's disease claim 4 , cognitive disorders claim 4 , memory deficits claim 4 , Parkinson's disease claim 4 , Aids related dementia claim 4 , anoxic and ischemic ...

CYCLIC PYRIMIDIN-4-CARBOXAMIDES AS CCR2 RECEPTOR ANTAGONISTS FOR TREATMENT OF INFLAMMATION, ASTHMA AND COPD

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. 4. The compound of claim 1 , wherein Ris selected from among —H claim 1 , -methyl claim 1 , -ethyl claim 1 , -propyl claim 1 , -i-propyl claim 1 , -cyclopropyl claim 1 , -butyl claim 1 , -i-butyl claim 1 , -t-butyl claim 1 , —F claim 1 , —Cl claim 1 , —Br claim 1 , —I claim 1 , —CN claim 1 , —CH═CH claim 1 , —C≡CH claim 1 , and —OCH.5. The compound of claim 1 , wherein Ris selected from among —H claim 1 , -methyl claim 1 , -ethyl claim 1 , —Br claim 1 , and —OCH.6. The compound of claim 1 , wherein Ris selected from among —H claim 1 , and -methyl.9. The compound of claim 1 , wherein Ris selected from among an electron pair claim 1 , —H claim 1 , and —C(O)—NH.10. The compound of claim 1 , wherein Ris selected from among —H claim 1 , —CH claim 1 , —CH claim 1 , —O—CH claim 1 , —O—CH claim 1 , —F claim 1 , —CF claim 1 , and —OCF.11. The compound of claim 1 , wherein Ris H or —O—CH.1214-. (canceled)15. The compound of claim 1 , wherein Z is C.16. (canceled)17. A method for the treatment of inflammatory diseases comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to or a pharmacologically acceptable salt thereof.18. (canceled)19. The method according to claim 17 , wherein the diseases is chronic obstructive pulmonary disease.20. A method for the treatment of neurologic diseases comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to or a pharmacologically acceptable salt thereof.2124-. (canceled)25. A method for the treatment of osteoarthritis claim 1 , diabetic nephropathy claim 1 , low back pain claim 1 , neuropathic pain or a pain disease comprising administering to a patient in need thereof a therapeutically effective amount of a ...

CCR2 RECEPTOR ANTAGONISTS AND USES THEREOF

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. 2. The method of claim 1 , wherein Li is —NH—.3. The method of claim 2 , wherein Ris —C-C-heterocyclyl substituted by one or more groups selected from among halogen claim 2 , —CF claim 2 , —OCF claim 2 , —CN claim 2 , —OH claim 2 , —O—C-C-alkyl claim 2 , and —C-C-alkyl.4. The method of claim 3 , wherein Ris phenyl optionally substituted with one or more groups selected from among —CF claim 3 , —O—CF claim 3 , —CN claim 3 , —C-C-alkyl claim 3 ,—C(CH)—CN claim 3 , and halogen.5. The method of claim 4 , wherein Ris —H claim 4 , and Ris —C-C-alkyl.6. The method of claim 5 , wherein Ris —H.8. The method of claim 1 , wherein the neurologic disease is inflammatory pain.9. The method of claim 4 , wherein the neurologic disease is inflammatory pain.10. The method of claim 7 , wherein the neurologic disease is inflammatory pain.11. The method of claim 1 , wherein the neurologic disease is neuropathic pain.12. The method of claim 4 , wherein the neurologic disease is neuropathic pain.13. The method of claim 7 , wherein the neurologic disease is neuropathic pain.14. The method of claim 11 , wherein the neuropathic pain is low back pain claim 11 , hip pain claim 11 , leg pain claim 11 , non-herpetic neuralgia claim 11 , post herpetic neuralgia claim 11 , diabetic neuropathy claim 11 , nerve injury-induced pain claim 11 , phantom limb pain claim 11 , post-surgical pain claim 11 , stump pain claim 11 , or trigeminal neuralgia.15. The method of claim 1 , wherein the neurologic disease is neuropathic pain due to chemotherapy caused nerve injury.16. The method of claim 13 , wherein the neuropathic pain is leg pain.17. The method of claim 13 , wherein the neuropathic pain is nerve injury-induced pain.18. The method of claim 13 , wherein the neuropathic pain is hip pain ...

NEW CCR2 RECEPTOR ANTAGONISTS AND USES THEREOF

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. 124-. (canceled)26. The method according to claim 25 , wherein the disease is selected from diabetic nephropathy claim 25 , osteoarthritis claim 25 , neuropathic pain claim 25 , low back pain or a pain disease. The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases where activation of CCR2 plays a causative role, especially pulmonary diseases like asthma and COPD, neurologic disease, especially of pain diseases, immune related diseases, especially diabetes mellitus including diabetes nephropathy, and cardiovascular diseases, especially atherosclerotic disease.The chemokines are a family of small, proinflammatory cytokines, with potent chemotatctic activities. Chemokines are chemotactic cytokines that are released by a wide variety of cells to attract various cells, such as monocytes, macrophages, T cells, eosinophils, basophils and neutrophils to sites of inflammation.Chemokine receptors, such as CCR2 or CCR5 have been implicated as being important mediators of inflammatory and immunoregulatory disorders and diseases as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. Accordingly, agents which modulate chemokine receptors such as the CCR2 and CCR5 receptor would be useful in such disorders and diseases.In particular it is widely accepted that numerous conditions and diseases involve inflammatory processes. Such inflammations are critically triggered and/or promoted by the activity of macrophages, which are formed by differentiation out of monocytes. It has further been found that monocytes are characterized by, e.g., a high expression of membrane-resident CCR2, whereas the CCR2 expression in macrophages is lower. ...

CCR2 RECEPTOR ANTAGONISTS

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. 3. The compound of formula (I) according to claim 1 ,{'sub': 1', '7, 'wherein A is —NH-L-R,'}{'sub': 1', '1, 'and wherein Lis a bond or wherein Ldenotes methylene,'}{'sub': '7', 'and wherein Ris a ring selected from among -cyclopropyl, -cyclobutyl, -cyclopentyl, -cyclohexyl, -cycloheptyl, -pyrrolidinyl, -piperidinyl, -azepanyl, -tetrahydrofuranyl, -tetrahydropyranyl, -oxepanyl, -phenyl, -pyridyl, and -furanyl,'}{'sub': 7', '3', '3', '1', '4', '3', '3', '3, 'wherein the ring Ris optionally substituted with one or more groups selected from among —F, —Cl, -methyl, -ethyl, -propyl, -i-propyl, -cyclopropyl, -t-butyl, —CF, —O—CF, —CN, —O-methyl, -furanyl and -phenyl, wherein said -phenyl is optionally independently substituted by one or more groups selected from among —C-C-alkyl, halogen, —OCH, —CF, and —OCF.'}4. The compound of formula (I) according to claim 1 ,{'sub': 1', '7, 'wherein A is —NH-L-R'}{'sub': 1', '1, 'and wherein Lis a bond or wherein Ldenotes methylene,'}{'sub': 7', '3', '8', '5', '10, 'and wherein Ris a ring selected from among —C-C-heterocyclyl, and —C-C-aryl,'}{'sub': 7', '3', '1', '6, 'wherein the ring Ris optionally substituted with one or more groups selected from among —O—CF— and —C-C-alkyl,'}{'sub': 7', '1', '4', '3, 'or wherein the ring Ris optionally substituted with one or more groups selected from -phenyl, optionally being substituted by one or more groups selected from —C-C-alkyl, and —OCF.'}7. The compound of formula (I) according to claim 1 , wherein Ris selected from among —H claim 1 , —CF claim 1 , and —CH.8. The compound of formula (I) according to claim 1 , wherein Ris selected from among —H claim 1 , —OCH claim 1 , and -methyl.9. The compound of formula (I) according to claim 1 , wherein Ris selected from among-H claim 1 , ...

PROCESS AND INTERMEDIATES FOR THE PRODUCTION OF CCR2 ANTAGONISTS

The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof. The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases where activation of CCR2 plays a causative role, especially pulmonary diseases like asthma and COPD, neurologic disease, especially of pain diseases, immune related diseases, especially diabetes mellitus including diabetes nephropathy, and cardiovascular diseases, especially atherosclerotic disease.The chemokines are a family of small, proinflammatory cytokines, with potent chemotactic activities. Chemokines are chemotactic cytokines that are released by a wide variety of cells to attract various cells, such as monocytes, macrophages, T cells, eosinophils, basophils and neutrophils to sites of inflammation.Chemokine receptors, such as CCR2 or CCR5 have been implicated as being important mediators of inflammatory and immunoregulatory disorders and diseases as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. Accordingly, agents which modulate chemokine receptors such as the CCR2 and CCR5 receptor would be useful in such disorders and diseases.In particular it is widely accepted that numerous conditions and diseases involve inflammatory processes. Such inflammations are critically triggered and/or promoted by the activity of macrophages, which are formed by differentiation out of monocytes. It has further been found that monocytes are characterized by, e.g., a high expression of membrane-resident CCR2, whereas the CCR2 expression in macrophages is lower. CCR2 is a critical regulator of monocytes trafficking, which can be described as the movement of the monocytes towards an inflammation along a gradient of monocyte chemoattractant proteins (MCP-1, MCP-2, MCP-3, MCP-4).Therefore, in order to reduce macrophage-induced inflammation, it ...

Ccr2 receptor antagonists and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

NEW CCR2 RECEPTOR ANTAGONISTS AND USES THEREOF

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. 124-. (canceled)26. The method of claim 25 , wherein Lis —NH—.27. The method of claim 25 , wherein Ris —C-C-heterocyclyl substituted by one or more groups selected from among halogen claim 25 , —CF claim 25 , —OCF claim 25 , —CN claim 25 , —OH claim 25 , —O—C-C-alkyl claim 25 , and —C-C-alkyl.28. The method of claim 26 , wherein Ris —C-C-heterocyclyl substituted by one or more groups selected from among halogen claim 26 , —CF claim 26 , —OCF claim 26 , —CN claim 26 , —OH claim 26 , —O—C-C-alkyl claim 26 , and —C-C-alkyl.29. The method of claim 25 , wherein Ris phenyl optionally substituted with one or more groups selected from among —CF claim 25 , —O—CF claim 25 , —CN claim 25 , —C-C-alkyl claim 25 , —C(CH)—CN claim 25 , and halogen.30. The method of claim 28 , wherein Ris phenyl optionally substituted with one or more groups selected from among —CF claim 28 , —O—CF claim 28 , —CN claim 28 , —C-C-alkyl claim 28 , —C(CH)—CN claim 28 , and halogen.31. The method of claim 25 , wherein Ris a group selected from among —H claim 25 , and Ris —C-C-alkyl.32. The method of claim 30 , wherein Ris —H claim 30 , and Ris —C-C-alkyl.33. The method of claim 32 , wherein Ris —H.34. The method of claim 26 , wherein the neurologic disease is inflammatory pain.35. The method of claim 28 , wherein the neurologic disease is inflammatory pain.36. The method of claim 33 , wherein the neurologic disease is inflammatory pain.37. The method of claim 26 , wherein the neurologic disease is neuropathic pain.38. The method of claim 28 , wherein the neurologic disease is neuropathic pain.39. The method of claim 33 , wherein the neurologic disease is neuropathic pain.40. The method of claim 39 , wherein the neuropathic pain is selected from the group consisting of low back pain claim 39 ...

New ccr2 receptor antagonists and uses thereof

Jedinjenje formule (I),u kojoj R1 je grupa odabrana između -H, -halogena, -CN, -O-C1-C4-alkila, -C1-C4-alkila, -CH=CH2, -CECH, -CF3, -OCF3, -OCF2H, i -OCFH2;u kojoj R7 je prsten odabran između -C3-C8-cikloalkila, -C3-C8-heterociklila, -C5-C10-arila, i -C5-C10-heteroarila,pri čemu je prsten R7 opciono supstituisan sa jednom ili više grupa odabranih između -CF3, -O-CF3, -S-CF3, -CN, -C1-C6-alkila, -C(CH3)2-CN, i -halogena, ili pri čemu je prsten R7 opciono supstituisan sa jednom ili više grupa odabranih između -C1-C6-alkila, -O-C1-C6-alkila, -C5-C10-arila, -C5-C10-heteroarila, -C3-C8-cikloalkila, -C3-C8-heterociklila, -C2-C6-alkenila, i -C2-C6-alkinila, koji je opciono supstituisan sa jednom ili više grupa odabranih između -OH, -NH2, -C1-C3-alkila, -O-C1-C6-alkila, -CN, -CF3, -OCF3, halogena, -metila, i =O, ili pri čemu je prsten R7 opciono dalje bivalentno supstituisan na dva susedna atoma prstena, tako da je obrazovan anelacijski prsten sa jednom ili više grupa odabranih između -C1-C6-alkilena, -C2-C6-alkenilena i -C4-C6-alkinilena, gde jedan ili dva ili tri ugljenikova centra mogu opciono biti zamenjeni sa 1 ili 2 ili 3 hetero atoma odabranih između N, O i S, bivalentna grupa koja je opciono supstituisana sa jednom ili više grupa odabranih između -OH, -NH2, -C1-C3-alkila, -O-C1-C6-alkila, -CN, -CF3, -OCF3, halogena, i =O;u kojoj R2 je odabran između -H, -halogena, -CN, -O-C2-C4-alkila, -C1-C4-alkila, -CH=CH2, -C=CH, -CF3, -OCF3, -OCF2H, i -OCFH2;u kojoj R3 je odabran između -H, -metila, -etila, -propila, -i-propila, -ciklopropila, -OCH3, -CF3, iu kojoj n je 1, 2 ili 3;u kojoj G i E su nezavisno odabrani između C-H ili N;u kojoj Z je C,a R4 i R5 su nezavisno odabrani između -H, - C1-C6-alkila, -NH2, -C3-C8- cikloalkila, -C3-C8-heterociklila, -C5-C10-arila, -C5-C10-heteroarila, i -C(O)-N(R8,R8'), sa R8 i R8' koji su nezavisno odabrani između -H, i -C1-C6-alkila,ili u kojoj Z je N,a R4 označava elektronski par, a R5 je odabran između -H, - C1-C6-alkila, -NH2, ...

New ccr2 antagonists

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (Ia) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

Ccr2 receptor antagonists and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonarydiseases like asthma and COPD.

(4 - ((3r, 4r) -3-methoxytetrahydro-pyrano-4-ylamino) piperidin-1-yl) (5-methyl-6 - (((2r, 6s) -6- (p-tolyl) citrate tetrahydro-2hpyrano-2-yl) methylamino) pyrimidin-4-yl) methanone

Sal de citrato del compuesto I: **(Ver fórmula)** que tiene la formula **(Ver fórmula)** Citrate salt of compound I: ** (See formula) ** that has the formula ** (See formula) **

Pyridazine carboxamides as CCR2 receptor antagonists

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

(4-((3R,4R)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4yl)methanone citrate

The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as the citrate salt of (4-((3

Ccr2 receptor antagonists

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

Novel ccr2 receptor antagonists and usage thereof

There is represented compound of formula (I), (I) and usage therefor the remedies preparation.

A process for the production of new CCR2 receptor antagonists and intermediates thereof

The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof.

Novel antagonists for ccr2 and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

Cyclic pyrimidin-4-carboxamides as ccr2 receptor antagonists for treatment of inflammation, asthma and copd

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single bond, =CH-, -CH2-, -O-, -S-, and -NH-; wherein n is 1, 2 or 3; wherein Z is C or N, the other variables are as defined in the claims, as well as in form of their acid addition salts with pharmacologically acceptable acids.

Analgetic phenylsulphonamides

Pyridine-piperazine-phenyl derivatives (I) or their enantiomers, diastereomers or salts, preferably salts with organic or inorganic acid or base, are new. Pyridin-piperazin-phenyl derivative (I) of formula (R 5>-A-R 4>-B 1>-R 3>-A-D-Y 1>-N(R 2>)-SO 2-R 1>) or their enantiomers, diastereomers or salts, preferably salts with organic or inorganic acid or base, are new. A : a bond or 1-4C alkylene; B 1> : a bond, 1-3C alkylene, -O- or -C(O)-; D : amine group of formula (-N(R 2>)-C(O)-) or (-C(O)-N(R 2>)-); Y 1> : 1-4C-alkylene optionally substituted by R 2>, where a methylene group can be replaced in addition by Y 2>; Y 2> : -O-, -S-, -S(O)-, -N(R 2>)-, -N(R 2>)-C(O)-, -C(O)-N(R 2>)-, -C(O)-, -CH(aryl)- or -S(O) 2-; R 1> : 3-7C-cycloalkyl- or aryl-, heteroaryl- or aryl-1-3C-alkyl- (all substituted with 1-4 R1a); R 2> : H or 1-3C-alkyl, where each methylene group is substituted with up to two F and each methyl group is replaced with up to 3 F; R 3> : arylene, heteroarylene, saturated 4-7-membered heterocyclic ring, unsaturated 5-7 membered heterocyclic ring (all substituted with 1 or 2 R3a) or 1-6C-alkylene; R 4> : arylene, heteroarylene, saturated 4-7-membered heterocyclic ring, unsaturated 5-7 membered heterocyclic ring (all substituted with 1 or 2 R4a), -O-, -C(O)O-, -C(O)NR 2>-, -NR 2>-, -NR 2>-NR 2>-, -3-7C-cycloalkylene- or -1-6C-alkylene-; R 5> : heteroaryl, 4-7 membered saturated heterocyclic ring (both substituted with 1 or 2 R5a), H, 1-8C alkyl, 3-7C-cycloalkyl (optionally substituted with 1-3C alkyl), H 2N-, 1-4C-alkyl-NH-, (1-4C-alkyl) 2N- or H 2N-C(O)-; and R1a, R3a, R4a, R5a : H, F, Cl, Br, I, 1-3C-alkyl-, HO-, 1-3C-alkyl-O- or 1-3C-alkyl-O-2-4C-alkylene-O-. An independent claim is included for pyridin-piperazin-phenyl salts with inorganic or organic acids or bases. ACTIVITY : Analgesic; Antimigraine; Neuroprotective; Dermatological; Cerebroprotective; Vasotropic; Antiallergic; ...

(4-((3r,4r)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2r,6s)-6-(p-tolyl)tetrahydro-2h-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone citrate

The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as die citrate salt of Compound I: (4-((3R,4R)-3-methoxytetrahydropyran-4-ylamino)piperidin-l-yl)(5-methyl-6-(((2R,6S)-6-(ptolyl)tetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone, and pharmaceutical compositions containing the same, processes for preparing the same, and medical uses thereof.

New ccr2 receptor antagonists and uses thereof

Ccr2 receptor antagonists and uses thereof

CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.

PYRIMIDINE DERIVATIVES AS ANTAGONISTS OF THE CCR2 RECEPTOR

REFERIDA A UN COMPUESTO DERIVADO DE PIRIMIDINA DE FORMULA (I), DONDE R1 ES -L1-R7; L1 ES UN ENLACE, ALQUILENO C1-C2, ALQUENILENO C1-C2, ENTRE OTROS; R7 ES CICLOALQUILO C3-C8, HETEROARILO C5-C10, ARILO C5-C10, ENTRE OTROS; R2 ES H, HALOGENO, CN, O-ALQUILO C1-C4, ENTRE OTROS; R3 ES H, METILO, ETILO, PROPILO, ENTRE OTROS; R4 Y R5 SON UN PAR DE ELECTRONES, H, ALQUILO C1-C6, NH2, ENTRE OTROS; R6 ES H, ALQUILO C1-C4, OH, HALOGENO, ENTRE OTROS; A ES UN ENLACE SENCILLO, =CH, CH2, O, NH; Z ES C O N; n ES 1, 2 O 3. SON COMPUESTOS PREFERIDOS: (a), (b), ENTRE OTROS. DICHOS COMPUESTOS SON ANTAGONISTAS DE CCR2 (RECEPTOR 2 DE QUIMIOQUINA CC) Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES PULMONARES, NEUROLOGICAS, RELACIONADAS CON EL SISTEMA INMUNE, ENTRE OTRAS REFERRING TO A COMPOUND DERIVED FROM PYRIMIDINE OF FORMULA (I), WHERE R1 IS -L1-R7; L1 IS A LINK, C1-C2 ALKYLENE, C1-C2 ALKYLENE, AMONG OTHERS; R7 IS C3-C8 CYCLOALKYL, C5-C10 HETEROARYL, C5-C10 ARYL, AMONG OTHERS; R2 IS H, HALOGEN, CN, O-C1-C4 ALKYL, AMONG OTHERS; R3 IS H, METHYL, ETHYL, PROPYL, AMONG OTHERS; R4 AND R5 ARE A PAIR OF ELECTRONS, H, C1-C6 ALKYL, NH2, AMONG OTHERS; R6 IS H, C1-C4 ALKYL, OH, HALOGEN, AMONG OTHERS; A IS A SINGLE LINK, = CH, CH2, O, NH; Z IS C O N; n IS 1, 2 OR 3. THE PREFERRED COMPOUNDS ARE: (a), (b), AMONG OTHERS. SUCH COMPOUNDS ARE ANTAGONISTS OF CCR2 (CC CHEMOKINE RECEPTOR 2) AND ARE USEFUL IN THE TREATMENT OF PULMONARY DISEASES, NEUROLOGICAL, RELATED TO THE IMMUNE SYSTEM, AMONG OTHERS

New ccr2 receptor antagonists and uses thereof

THE PRESENT INVENTION RELATES TO NOVEL ANTAGONISTS FOR CCR2 (CC CHEMOKINE RECEPTOR 2) OF FORMULA (I) AND THEIR USE FOR PROVIDING MEDICAMENTS FOR TREATING CONDITIONS AND DISEASES, ESPECIALLY PULMONARY DISEASES LIKE ASTHMA AND COPD. (NO SUITABLE

Cyclic pyrimidin-4-carboxamides as CCR2 receptor antagonists for treatment of inflammation, asthma and COPD

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single bond, =CH-, -CH

Premedine-4 annular carboxamide as antagonists of the receptor ccr2 for the treatment of infections, asthma and COPD

CETTE INVENTION CONCERNE DE NOUVEAUX ANTAGONISTES DE CCR2 (RÉCEPTEUR 2 DE CHIMIOKINE CC) ET LEUR UTILISATION DANS DES MÉDICAMENTS DESTINÉS AU TRAITEMENT D'ÉTATS PATHOLOGIQUES ET DE MALADIES, EN PARTICULIER DE L'ASTHME ET LES BRONCHO-PNEUMOPATHIES CHRONIQUES OBSTRUCTIVES, COMME REPRÉSENTÉ DANS LA FORMULE (I), OÙ A EST PRIS DANS UNE LIAISON UNIQUE, =CH-, -CH2-, -O-, -S-, AND -NH-; N VAUT 1, 2 OU 3; Z EST C OU N, LES AUTRES VARIABLES ÉTANT COMME DÉFINIES DANS LES REVENDICATIONS, AINSI QUE LEURS FORMES DE SELS D'ADJONCTION ACIDES AVEC DES ACIDES DE QUALITÉ PHARMACOLOGIQUE. THIS INVENTION INVOLVES NOVEL CCR2 ANTAGONISTS (CHEMOKINE CC RECEPTOR 2) AND THEIR USE IN MEDICAMENTS FOR THE TREATMENT OF DISEASE CONDITIONS AND DISEASES, IN PARTICULAR ASTHMA AND OBSTRUCTIVE CHRONIC BRONCHO-PNEUMOPATHIES, AS REPRESENTED IN THE FORMULA (I), WHERE HAS BEEN TAKEN IN A SINGLE BINDING, = CH-, -CH2-, -O-, -S-, AND -NH-; N VAUT 1, 2 OR 3; Z IS C OR N, THE OTHER VARIABLES BEING AS DEFINED IN THE CLAIMS, AND THEIR SHAPES OF ACID ADDITION SALTS WITH ACIDS OF PHARMACOLOGICAL QUALITY.

Ccr2 receptor antagonists and uses thereof

New compounds

The invention relates to compounds of the general formula (I) in which A, B, D, Y, R1, R2, R3, R4 and R5 are defined as per claim 1, to their enantiomers, their diastereomers, their mixtures and their salts, especially their physiologically compatible salts with organic or inorganic acids or bases, which have valuable properties, to their preparation, to medicaments comprising the pharmacologically effective compounds, their preparation and their use.

Novel ccr2 receptor antagonists, method for producing the same, and use thereof as medicaments

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.

ccr2 receptor antagonists and uses thereof

Cyclic pyrimidin-4-carboxamides as ccr2 receptor antagonists for treatment of inflammation, asthma and copd

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single bond, =CH-, -CH2-, -O-, -S-, and -NH-; wherein n is 1, 2 or 3; wherein Z is C or N, the other variables are as defined in the claims, as well as in form of their acid addition salts with pharmacologically acceptable acids.

CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.

Arylsulfonamides with analgesic action

(I) Oppfinnelsen angår forbindelser med den generelle formel (I) hvor A, B, D, Y, R1, R2, R3, R4 og R5 er som definert i krav 1, deres enantiomerer, deres diastereomerer, blandinger derav og salter derav, spesielt deres fysiologisk kompatible salter med organiske eller uorganiske syrer eller baser, som har verdifulle egenskaper, deres fremstilling, medikamenter omfattende de farmakologisk effektive forbindelser, fremstilling derav og anvendelse derav.

CCR2 Receptor Antagonists and Uses Thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

New ccr2 receptor antagonists and uses thereof

New ccr2 receptor antagonists and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of Formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

(4-((3r,4r)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2r,6s)-6-(p-tolyl)tetrahydro-2h-pyran-2-yl)methylamino)pyrimidin-4yl)methanone citrate

New selective ccr2 antagonists

The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain.

New ccr2 receptor antagonists and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of Formula (I) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

Ccr2 receptor antagonists and uses thereof

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

Citrato de (4-((3r,4r)-3-metoxitetra-hidro-piran-4- ilamino)piperidin-1-il) (5- metil-6-(((2r, 6s)-6-(p-tolil) tetra-hidro-2h-piran-2-il)metilamino)pirimidin-4-il) metanona, seu uso e seu método de preparação, e composição farmacêutica

citrato de (4-((3r, 4r)-3-metoxitetrahidro-piran-4-ilamino)piperidin-1-il)(5-metil-6-(((2r, 6s)-6-(p-tolil)tetra-hidro-2h-piran-2-il)metilamino)pirimidin4-il)metanona. a presente invenção refere-se a um sal de uma tetra-hidro-piranilmetilaminopirimidina amina, tal como o sal de citrato de (4-((3r, 4r)-3-metoxitetra-hidropirano-4-ilamino)piperidin-1-il)(5-metil-6-((2r, 6s) -6-(p-tolil)tetra-hidro-2h-piran-2-il)metilamino)pirimidin-4-il)metanona, composições farmacêuticas contendo o mesmo, processos para a preparação do mesmo e métodos de tratamento com medicação usando o mesmo.

(4-((3r,4r)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2r,6s)-6-(p-tolyl)tetrahydro-2h-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone citrate

The invention provides a salt of a tetrahydropyranylmethylaminopyrimidine amide, such as the citrate salt of Compound I: (see Compound I) (4-((3R,4R)-3-methoxytetrahydropyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2R,6S)-6-(p-tolyptetrahydro-2H-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone, and pharmaceutical compositions containing the same, processes for preparing the same, and medical uses thereof.

Antagonists receptor ccr2 and their use

Nuevos compuestos en base a amidas sustituidas de acidos carboxilicos, sus enantiomeros, diasteromeros y sales farmacéuticamente compatibles y aplicaciones

Objeto de la presente invencion son compuestos de la formula general I en la que A,B,D,Y, R1,R2,R3,R4 y R5 están definidos como en la reivindicacion 1, sus enantiomeros, sus diastereoisomeros, sus mezclas y sus sales, en especial sus sales fisiologicamente compatibles con ácidos o bases orgánicos o inorgánicos los cuales presentan valiosas propiedades, su preparacion, los medicamentos que contienen los compuestos farmacologicamente activos, su preparacion y su uso.