Quinazoline Salt Compounds

Salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity.

NILOTINIB HCL CRYSTALLINE FORMS

Crystalline forms of Nilotinib HCl are described.

Nilotinib HCl crystalline forms

Crystalline forms of Nilotinib HCl are described.

Crystalline complexes of fluticasone-2-furoate

There is provided a crystalline complex comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in that the crystalline complex is of space group P2 1 2 1 2 1 having unit cell dimensions of about 12.5±1.0 §, 15±1.0 §, and 16.2±1.0 § when determined at either 120K or 150K.

Polymorphs of N-[(6-cyano-2-fluoro)-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide as kallikrein inhibitors

The invention provides new polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, pharmaceutical compositions containing them and their use in therapy.

Acid addition salts of piperazine derivatives

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glycosidase inhibitors.

Polymorphs of n-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[2-oxopyridin-1-yl)methyl]phenyl} methyl)pyrazole-4-carboxamide as iallikrein inhibitors

The invention provides new polymorphs of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide and salts thereof, pharmaceutical compositions containing them and their use as kallikrein inhibitors in therapy.

Nilotinib HCl crystalline forms

Crystalline forms of Nilotinib HCl are described.

Solid Forms of an eIF4E Inhibitor

The present invention relates to solid forms of 7-(5-chloro-2-(3-(5-cyano-6-(1-(3,3-difluorocyclobutyl)piperidin-4-yl)(methyl)amino)-2-methyl-4-oxopyrido[3,4-d]pyrimidin-3(4H)-yl)prop-1-yn-1-yl)phenyl)-N-(methylsulfonyl)thieno[3,2-b]pyridine-3-carboxamide, to pharmaceutical compositions comprising such solid forms, and to methods of using such solid forms and pharmaceutical compositions for the treatment of cancer.

POLYMORPHS OF N-[(3-FLUORO-4-METHOXYPYRIDIN-2-YL)METHYL]-3-(METHOXYMETHYL)-1-({4-[(2-OXOPYRIDIN-1-YL)METHYL]PHENYL}METHYL)PYRAZOLE-4-CARBOXAMIDE AND SALTS THEREOF

The invention provides new polymorphs of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide and salts thereof, pharmaceutical compositions containing them and their use in therapy. 1. A method of treating a disease or condition mediated by plasma kallikrein in a mammal in need of such treatment , said method comprising administering to the mammal a therapeutically effective amount of a crystalline form of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide , wherein the N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide is crystalline form 1 of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide , which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation , expressed in degrees 2θ) at 11.2±0.3 , 12.5±0.3 , 13.2±0.3 , 14.5±0.3 , and 16.3±0.3.2. The method of claim 1 , wherein the disease or condition mediated by plasma kallikrein is impaired visual acuity claim 1 , diabetic retinopathy claim 1 , retinal vascular permeability associated with diabetic retinopathy claim 1 , diabetic macular edema claim 1 , hereditary angioedema claim 1 , diabetes claim 1 , pancreatitis claim 1 , cerebral haemorrhage claim 1 , nephropathy claim 1 , cardiomyopathy claim 1 , neuropathy claim 1 , inflammatory bowel disease claim 1 , arthritis claim 1 , inflammation claim 1 , septic shock claim 1 , hypotension claim 1 , cancer claim 1 , adult respiratory distress syndrome claim 1 , disseminated intravascular coagulation claim 1 , blood coagulation during cardiopulmonary bypass surgery claim 1 , or bleeding from post-operative surgery.3. The method of claim 1 , wherein the disease or condition mediated by plasma kallikrein is retinal vascular permeability associated ...

ACID ADDITION SALTS OF PIPERAZINE DERIVATIVES

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glycosidase inhibitors. 114.-. (canceled)19. The acid addition salt according to any one of - in a molar ratio of the compound of formula I to acid of 1 to 1.20. The acid addition salt according to claim 19 , selected from:N-(5-{4-[(1S)-1-(2,3-dihydro-1-benzofuran-6-yl)ethyl]piperazin-1-yl}-1,3,4-thiadiazol-2-yl)acetamide, mono-hydrochloride;N-(5-{4-[(1S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-1,3,4-thiadiazol-2-yl)acetamide, mono-hydrochloride;2-{4-[(1S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-N-methyl-1,3-thiazole-5-carboxamide, mono-hydrochloride;2-{4-[(1S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-N-methylpyrimidine-5-carboxamide, mono-hydrochloride;N-(2-{4-[(1S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}pyrimidin-5-yl)acetamide, mono-hydrochloride; and2-{4-[(1 S)-1-(2,3-dihydro-1-benzofuran-6-yl)ethyl]piperazin-1-yl}-4H,5H,6H,7H-[1,3]thiazolo[5,4-c]pyridin-4-one, mono-hydrochloride.21. N-(5-{4-[(1S)-1-(2H-1 claim 19 ,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-1 claim 19 ,3 claim 19 ,4-thiadiazol-2-yl)acetamide claim 19 , mono-hydrochloride in a solid form having the characteristic X-ray powder diffraction pattern as shown on .22. A method for the preparation of an acid addition salt of hydrochloric acid claim 15 , maleic acid claim 15 , tartaric acid sulfuric acid or p-toluolsulfonic acid with a compound of formula I according to claim 15 , comprising the following steps:a) suspending or dissolving the selected compound of formula I and the selected acid in a suitable solvent or solvent mixture;b) heating the mixture obtained in step a) to a temperature of between 30° C. to the boiling point of the selected solvent or solvent mixture, and allowing the mixture to cool to room temperature;c) optionally repeating step b) several times; ...

SOLID FORMS OF A PLASMA KALLIKREIN INHIBITOR AND SALTS THEREOF

New solid forms of the plasma kallikrein inhibitor, 1-({4-[(5-fluoro-2-oxopyridin-1-yl)methyl]phenyl}methyl)-N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)pyrazole-4-carboxamide and its salts, are described. 2. The solid form according to that is the a solid form of the compound of Formula A (i) and having an X-ray powder diffraction pattern substantially the same as that shown in claim 1 , and/or exhibiting an endothermic peak in its STA thermograph at 148±3° C. claim 1 , and/or having an STA thermograph substantially the same as that shown in .3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. The solid form according to that is the solid form of the compound of Formula A (ii) and having an X-ray powder diffraction pattern substantially the same as that shown in .9. (canceled)10. The solid form according to that is the solid form of the compound of Formula A (iii) and having an X-ray powder diffraction pattern substantially the same as that shown in .11. (canceled)12. The solid form according to that is the solid form of the compound of Formula A (iv) and having an X-ray powder diffraction pattern substantially the same as that shown in .13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. (canceled)22. (canceled)23. The solid form according to claim 1 , that is the solid form of the compound of Formula A (xii) and having an X-ray powder diffraction pattern substantially the same as that shown in and/or which exhibits an endothermic peak in its DSC thermograph at 158±3° C. claim 1 , and/or has an DSC thermograph substantially the same as that shown in .24. (canceled)25. (canceled)26. (canceled)27. The solid form according to that is the solid form of the compound of Formula A (xiii) and having an X-ray powder diffraction pattern substantially the same as that shown in claim 1 , and/or exhibits an endothermic peak in its DSC thermograph at 166±3° C. claim 1 , and/or has a ...

SUCCINATE AND FUMARATE ACID ADDITION SALTS OF PIPERAZINE DERIVATIVES

The invention relates to succinic acid addition salts or fumaric acid addition salts of piperazine derivatives of formula (I), as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glucosidase inhibitors. 6. The succinic acid or fumaric acid addition salt according to any one of to in a molar ratio of a compound of formula I , Ia , Ib , Ic , Id , Ie , If , Ig , Ih , Ii , Ij , Ik , IL , I1a , I1b , I2a , I2b , I3a , I3b , I1 , I2 or I3 to acid of 1 to 1.7. The mono-succinic acid salt of one of the compounds Ia claim 5 , Ib claim 5 , Ic claim 5 , Id according to in a solid form having the characteristic X-ray powder diffraction pattern as shown on .8. The mono-fumaric acid salt of one of the compounds Ia claim 5 , Ib claim 5 , Ic claim 5 , Id according to in a solid form having the characteristic X-ray powder diffraction pattern as shown on .9. A method for the preparation of an acid addition salt of succinic acid or fumaric acid with compounds of formula I and their stereoisomers comprising the following steps:a) suspending or dissolving the selected compound of formula I and the respective acid in a suitable solvent or solvent mixture;b) heating the mixture obtained in step a) to a temperature of between about 30° C. to about the boiling point of the selected solvent or solvent mixture, and allowing the mixture to cool to room temperature;c) optionally repeating step b) several times;d) separating and drying the solid thus obtained.10. A solid oral dosage form comprising a succinic acid addition salt or fumaric acid addition salt according to any one of to .11. A succinic acid addition salt or fumaric acid addition salt according to any one of to for use as a medicament.12. A succinic acid addition salt or fumaric acid addition salt according to any one of to for use in a method of treating a condition selected from the group consisting of neurodegenerative diseases claim 5 , diabetes claim ...

POLYMORPHS OF N-[(6-CYANO-2-FLUORO)-3-METHOXYPHENYL)METHYL]-3-(METHOXYMETHYL)-1-({4-[(2-OXOPYRIDIN-1-YL)METHYL]PHENYL}METHYL)PYRAZOLE-4-CARBOXAMIDE AS KALLIKREIN INHIBITORS

The invention provides new polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, pharmaceutical compositions containing them and their use in therapy. 1. A crystalline form of N-[(6-cyano-2-fluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide , that is:(a) crystalline Form 1, which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 9.0±0.3, 14.3±0.3, 18.1±0.3, 19.6±0.3 and 24.0±0.3; or(b) crystalline Form 2, which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 8.3±0.3, 10.5±0.3, 16.6±0.3, 19.6±0.3, and 23.8±0.3, or(c) crystalline Form 3, which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 7.3±0.3, 10.2±0.3, 12.4±0.3, 12.9±0.3 and 18.1±0.3; or(d) crystalline Form 4, which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 9.0±0.3, 14.3±0.3, 15.0±0.3, 18.1±0.3, and 19.5±0.3.2. The crystalline form 1 of having an X-ray powder diffraction pattern substantially the same as that shown in .3. The crystalline form 1 of claim 1 , which exhibits an endothermic peak in its DSC thermograph at 149±3° C.4. The crystalline form 1 according to any one of having a DSC thermograph substantially the same as that shown in .5. A crystalline form 1 of N-[(6-cyano-2-fluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide claim 1 , which exhibits an endothermic peak in its DSC thermograph at 149±3° C.6. The crystalline form 1 of having a DSC thermograph substantially the same as that shown in .7. The crystalline form 2 of claim 1 , which exhibits at least X ray powder diffraction peaks (Cu Kα radiation claim 1 , expressed in degrees 2θ) at 8.3±0.3 claim 1 , 10.5±0.3 claim 1 , 16.6±0.3 ...

POLYMORPHS OF N-[(3-FLUORO-4-METHOXYPYRIDIN-2-YL)METHYL]-3-(METHOXYMETHYL)-1 -({4-[2-OXOPYRIDIN-1-YL)METHYL]PHENYL} METHYL)PYRAZOLE-4-CARBOXAMIDE AS IALLIKREIN INHIBITORS

The invention provides new polymorphs of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide and salts thereof, pharmaceutical compositions containing them and their use as kallikrein inhibitors in therapy 1. A crystalline form of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide , that is:(a) crystalline form 1, which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 11.2±0.3, 12.5±0.3, 13.2±0.3, 14.5±0.3, and 16.3±0.3; or(b) crystalline form 8, which exhibits at least the following characteristic X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at approximately 5.1±0.3, 7.5±0.3, 12.0±0.3, 15.2±0.3, and 17.9±0.3.2a.. The crystalline form 1 of having an X-ray powder diffraction pattern that is substantially the same as that shown in3. The crystalline form 1 of claim 1 , which exhibits an endothermic peak in its DSC thermograph at 151±3° C.4. The crystalline form 1 of having a DSC thermograph substantially the same as that shown in .5. A crystalline form 1 of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide claim 1 , which exhibits an endothermic peak in its DSC thermograph at 151±3° C.6. The crystalline form of having a DSC thermograph substantially the same as that shown in .7. The crystalline form 8 of claim 1 , which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation claim 1 , expressed in degrees 2θ) at 5.1±0.3 claim 1 , 7.5±0.3 claim 1 , 12.0±0.3 claim 1 , 15.2±0.3 claim 1 , and 17.9±0.3.8. The crystalline form 8 of having an X-ray power diffraction pattern substantially the same as shown in .9. The crystalline form 8 of claim 7 , which exhibits an endothermic peak in its DSC thermograph at 110±3° C.10. The crystalline form of having a DSC ...

POLYMORPHS OF N-[(2,6-DIFLUORO-3-METHOXYPHENYL)METHYL]-3-(METHOXYMETHYL)-1-({4-[(2-OXOPYRIDIN-1YL)METHYL]PHENYL}METHYL)PYRAZOLE-4-CARBOXAMIDE

The invention provides new polymorphs of N-[(2,6-difluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, pharmaceutical compositions containing them and their use in therapy. 1. A crystalline form of N-[(2 ,6-difluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide , that is:(a) crystalline Form 1, which exhibits at least the characteristic X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 5.5±0.3, 9.5±0.3, 12.7±0.3, 14.7±0.3, and 16.7±0.3; or(b) crystalline Form 2 which exhibits at least the characteristic X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 9.5±0.3, 10.3±0.3, 13.2±0.3, 15.6±0.3, and 16.9±0.3; or(c) crystalline Form 3, which exhibits at least the characteristic X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 12.3±0.3, 13.7±0.3, 20.7±0.3, 26.2±0.3, and 27.8±0.3.2. The crystalline Form 1 of having an X-ray powder diffraction pattern substantially the same as that shown in .3. The crystalline Form 1 of claim 1 , which exhibits an endothermic peak in its DSC thermograph at 157±3° C.4. The crystalline Form 1 of having a DSC thermograph substantially the same as that shown in .5. A crystalline Form 1 of N-[(2 claim 1 ,6-difluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide claim 1 , which exhibits an endothermic peak in its DSC thermograph at 157±3° C.6. The crystalline Form 1 of having a DSC thermograph substantially the same as that shown in .7. The crystalline Form 2 of claim 1 , which exhibits at least the characteristic X-ray powder diffraction peaks (Cu Kα radiation claim 1 , expressed in degrees 2θ) at 9.5±0.3 claim 1 , 10.3±0.3 claim 1 , 13.2±0.3 claim 1 , 15.6±0.3 claim 1 , and 16.9±0.3.8. The crystalline Form 2 of having an X-ray powder diffraction pattern substantially ...

Solid forms of a plasma kallikrein inhibitor and salts thereof

The present invention relates to new solid forms of a plasma kallikrein inhibitor, a pharmaceutical composition containing them and their use in therapy. Also provided are processes for preparing the solid forms of the present invention.

ACID ADDITION SALTS OF PIPERAZINE DERIVATIVES

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glycosidase inhibitors. 114.-. (canceled)19. The acid addition salt according to in a molar ratio of the compound of formula I to acid of 1 to 1.20. The acid addition salt according to in a molar ratio of the compound of formula I to acid of 1 to 1.21. The acid addition salt according to in a molar ratio of the compound of formula I to acid of 1 to 1.22. The acid addition salt according to in a molar ratio of the compound of formula I to acid of 1 to 1.24. The acid addition salt according to claim 23 , selected from the group consisting of:N-(5-{4-[(1 S)-1-(2,3-dihydro-1-benzofuran-6-yl)ethyl]piperazin-1-yl}-1,3,4-thiadiazol-2-yl)acetamide, mono-hydrochloride;N-(5-{4-[(1 S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-1,3,4-thiadiazol-2-yl)acetamide, mono-hydrochloride;2-{4-[(1 S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-N-methyl-1,3-thiazole-5-carboxamide, mono-hydrochloride;2-{4-[(1 S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}-N-methylpyrimidine-5-carboxamide, mono-hydrochloride;N-(2-{4-[(1 S)-1-(2H-1,3-benzodioxol-5-yl)ethyl]piperazin-1-yl}pyrimidin-5-yl)acetamide, mono-hydrochloride; and2-(4-[(1 S)-1-(2,3-dihydro-1-benzofuran-6-yl)ethyl]piperazin-1-yl)-4H, 5H,6H,7H-[1,3]thiazolo[5,4-c]pyridin-4-one, mono-hydrochloride.25. A solid oral dosage form comprising an acid addition salt according to .26. A method for the preparation of an acid addition salt of hydrochloric acid claim 15 , maleic acid claim 15 , tartaric acid sulfuric acid or p-toluolsulfonic acid with a compound of formula I according to claim 15 , comprising the following steps:a) suspending or dissolving the selected compound of formula I and the selected acid in a suitable solvent or solvent mixture;b) heating the mixture obtained in step a) to a temperature of between 30° C. to the ...

Nilotinib hci crystalline forms

Crystalline forms of Nilotinib HCl are described. (I)

Solid forms of a plasma kallikrein inhibitor and salts thereof

New solid forms of the plasma kallikrein inhibitor, 1-({4-[(5-fluoro-2-oxopyridin-1-yl)methyl]phenyl}methyl)-N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)pyrazole-4-carboxamide and its salts, are described.

Polymorphs of n-((3-fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-((4-(2-oxopyridin-1-yl)methyl)phenyl)methyl)pyrazole-4-carboxamide as kallikrein inhibitors

Polymorphs of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1 -({4-[2-oxopyridin-1 -yl)methyl]phenyl} methyl) pyrazole -4-carboxamide as kallikrein inhibitorss

The invention provides new polymorphs of N-[(3-fluoro-4- methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-l-({4-[(2- oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide and salts thereof, pharmaceutical compositions containing them and their use as kallikrein inhibitors in therapy

POLYMORPHS OF N-[(3-FLUOR-4-METHOXYPYRIDIN-2-YL)METHYL]-3-(METHOXYMETHYL)-1-({4-[2-OXOPYRIDIN-1-YL)METHYL]PHENYL}METHYL)PYRAZOLE- 4-CARBOXAMIDE AS KALLIKREIN INHIBITORS

Crystalline complexes of fluticasone 2-furoate

There is provided a crystalline complex comprising a compound of formula (I) in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in that the crystalline complex is of space group P212121 having unit cell dimensions of about 12.5 ± 1.0 Å, 15 ± 1.0 Å, and 16.2 ± 1.0 Å when determined at either 120K or 150K.

Nilotinib hci crystalline forms

Crystalline forms of Nilotinib HC1 are described.

Polymorphs of n-[(2,6-difluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide

The invention provides new polymorphs of N-[(2,6-difluoro-3-methoxyphenyl)methyl]-3- (methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, pharmaceutical compositions containing them and their use in therapy.

Polymorphs of n-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide as kallikrein inhibitors

Polymorphs of n-[(2,6-difluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide

The invention provides new polymorphs of N-[(2,6-difluoro-3-methoxyphenyl)methyl]-3- (methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, pharmaceutical compositions containing them and their use in therapy.

Acid addition salts of piperazine derivatives

Solid forms of a plasma kallikrein inhibitor and salts thereof.

La presente invención se refiere a nuevas formas sólidas de un inhibidor de calicreína en plasma, una composición farmacéutica que lo contiene y su uso en terapia. También se proporcionan procesos para preparar las formas sólidas de la presente invención.

Acid addition salts of piperazine derivatives

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glycosidase inhibitors.

Acid addition salts of piperazine derivatives

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.

Nilotinib hci crystalline forms

Crystalline forms of Nilotinib HCl are described. (I)

Solid forms of a plasma kallikrein inhibitor and salts thereof

The present invention relates to new solid forms of a plasma kallikrein inhibitor, a pharmaceutical composition containing them and their use in therapy. Also provided are processes for preparing the solid forms of the present invention.

Acid addition salts of piperazine derivatives

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glycosidase inhibitors.

Kristalline komplexe von fluticasone 2-furoat

Forma sólida de polimorfos den-[(3-flúor-4-metoxipiridin-2-il)metil]-3- (metoximetil)-1-({4-[(2-oxopiridin-1-il) metil]fenil}metil)pirazol-4-carboxamida, processo de preparação, composição farmacêutica e seus usos como inibidores de calicreína

a presente invenção refere-se aos novos polimorfos de n-[(3-flúor-4-metoxipiridin-2-il)metil]-3-(metoximetil)-1-({4-[(2-oxopiridin-1-il)metil]fenil]fenil}metil)pirazol-4-carboxamida e os sais dos mesmos, as composições farmacêuticas contendo-os e ao seu uso como inibidores de calicreína em terapia.

Sole addycyjne kwasu bursztynowego lub kwasu fumarowego z pochodnymi piperazyny użyteczne jako inhibitory glikozydazy

Solid forms of an eif4e inhibitor

The present invention relates to solid forms of 7-(5-chloro-2-(3-(5-cyano-6-((1-(3,3-difluorocyclobutyl)piperidin-4-yl)(methyl)amino)-2-methyl-4-oxopyrido[3,4-d]pyrimidin-3(4H)-yl)prop-1-yn-1-yl)phenyl)-N-(methylsulfonyl)thieno[3,2-b]pyridine-3-carboxamide, to pharmaceutical compositions comprising such solid forms, and to methods of using such solid forms and pharmaceutical compositions for the treatment of cancer.

Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors

Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors

The invention relates to succinic acid addition salts or fumaric acid addition salts of piperazine derivatives of formula (I), as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.

Sales de adición de ácido de succinato y fumarato de derivados de piperazina útiles como inhibidores de glucosidasa

La invención se refiere a sales de adición de ácido succínico o sales de adición de ácido fumárico de derivados de piperazina de fórmula (I), así como a formas sólidas, tales como formas polimórficas, de los mismos, que son útiles como ingredientes farmacéuticos y en particular como inhibidores de glicosidasas. (Traducción automática con Google Translate, sin valor legal)

Succinate and fumarate acid addition salts of piperazine derivatives useful as glycosidase inhibitors

The invention relates to succinic acid addition salts or fumaric acid addition salts of piperazine derivatives of formula (I), as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.

Inclusion complexes of rosiglitazone

Inclusion complexes of rosiglitazone

Inclusion complexes of rosiglitazone

A host-guest complex, wherein the host is a cyclodextrin or a mixture of cyclodextrins (the Cyclodextrin) and the guest is 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, (Compound (I)) or a pharmaceutically acceptable derivative thereof or a mixture thereof; a process for the preparation of said complex, a pharmaceutical composition comprising such complex and the use of such complex in medicine.

Polymorphs of n-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide and salts thereof

The invention provides new polymorphs of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide and salts thereof, pharmaceutical compositions containing them and their use in therapy.

Solid forms of an eif4e inhibitor

The present invention relates to solid forms of 7-(5-chloro-2-(3-(5-cyano-6-((1-(3,3-difluorocyclobutyl)piperidin-4-yl)(methyl)amino)-2-methyl-4-oxopyrido[3,4-d]pyrimidin-3(4H)-yl)prop-1-yn-1-yl)phenyl)-N-(methylsulfonyl)thieno[3,2-b]pyridine-3-carboxamide, to pharmaceutical compositions comprising such solid forms, and to methods of using such solid forms and pharmaceutical compositions for the treatment of cancer.

Formas solidas de un inhibidor de eif4e

La presente invención se refiere a formas sólidas de 7-(5-cloro-2-(3-(5-ciano-6-(1-(3,3-difluorociclobutil) piperidin-4-il) (metil) amino)-2-metil-4-oxopirido [3,4-d] pirimidin -3 (4H)-il) prop-1-in-1-il) fenil)-N-(metilsulfonil) tieno [3 2-b] piridin-3-carboxamida, a composiciones farmacéuticas que comprenden tales formas sólidas, y a métodos para usar tales formas sólidas y composiciones farmacéuticas para el tratamiento de cáncer.

Acid addition salts of piperazine derivatives

The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.

Succinate and fumarate acid addition salts of piperazine derivatives

The invention relates to succinic acid addition salts or fumaric acid addition salts of piperazine derivatives of formula (I), as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.

Sales de adición de ácido de succinato y fumarato de derivados de piperazina útiles como inhibidores de glucosidasa.

La invención se refiere a sales de adición de ácido succínico o sales de adición de ácido fumárico de derivados de piperazina de fórmula (I), así como formas sólidas, tales como formas polimórficas, de las mismas, que son útiles como ingredientes farmacéuticos y en particular como inhibidores de glucosidasa.