ACOUSTIC MIXING FOR AUTO GRANULATION

A process for acoustically mixing a bulk drug substance involves the application of acoustic energy to drive an accelerative force in a mixing vessel containing the drug substance. The drug substance may be, for example, Elagolix.

Carbidopa And L-Dopa Prodrugs And Methods Of Use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease. 130-. (canceled)31. A crystalline polymorph of L-dopa 4′-monophosphate identified by powder X-ray diffraction wherein the crystalline polymorph is:crystalline L-dopa 4′-monophosphate anhydrate (i) demonstrating at least one characteristic peak in the powder X-ray diffraction pattern at values of two theta of 10.261±0.20, 12.053±0.20, 13.759±0.20, 14.932±0.20, 16.147±0.20, 16.718±0.20, 17.34±0.20, 19.254±0.20, 20.654±0.20, 22.078±0.20, 23.599±0.20, 24.198±0.20, 25.898±0.20, 26.338±0.20, and 27.117±0.20; orcrystalline L-dopa 4′-monophosphate anhydrate (ii) demonstrating at least one characteristic peak in the powder X-ray diffraction pattern at values of two theta of 8.468±0.20, 10.234±0.20, 11.821±0.20, 13.084±0.20, 13.503±0.20, 15.48±0.20, 15.848±0.20, 16.513±0.20, 18.447±0.20, 19.346±0.20, 20.239±0.20, 21.139±0.20, 24.221±0.20, 24.865±0.20, 25.647±0.20.32. A crystalline L-dopa 3′-monophosphate demonstrating at least one characteristic peak in the powder X-ray diffraction pattern at values of two theta of 8.662±0.20 , 11.286±0.20 , 15.079±0.20 , 15.678±0.20 , 16.786±0.20 , 17.288±0.20 , 18.438±0.20 , 19.682±0.20 , 20.946±0.20 , 22.188±0.20 , 22.671±0.20 , 23.088±0.20 , 24.144±0.20 , 24.744±0.20 , and 25.383±0.20.33. A crystalline L-dopa 3′4-diphosphate trihydrate demonstrating at least one characteristic peak in the powder X-ray diffraction pattern at values of two theta of 7.118±0.20 , 10.342±0.20 , 11.355±0.20 , 12.161±0.20 , 14.201±0.20 , 17.36±0.20 , 17.632±0.20 , 19.196±0.20 , 19.444±0.20 , 20.83±0.20 , 21.504±0.20 , 22.491±0.20 , 23.085±0.20 , 24.487±0.20 , and 25.11±0.20.34. A crystalline polymorph of carbidopa 4′- ...

Elagolix Sodium Compositions and Processes

The present invention relates to compositions of elagolix sodium, and process and intermediates for the preparation thereof.

Carbidopa and L-Dopa Prodrugs and Methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease. 130-. (canceled)32. A method of treating Parkinson's disease comprising administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition according to .33. The method of claim 32 , further comprising administering another anti-Parkinson's agent to the subject.34. A kit comprising the pharmaceutical composition of . The present disclosure relates to (a) carbidopa prodrugs, (b) L-dopa prodrugs, (c) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (d) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.Parkinson's disease is a chronic and progressive neurodegenerative condition characterized by reduced levels in the brain of the neurotransmitter dopamine (i.e., 3,4-dihydroxyphenethylamine). Administration of L-dopa (i.e., L-3,4-dihydroxyphenylalanine) currently is the most effective therapy for treating a patient with Parkinson's disease. L-dopa, which unlike dopamine can cross the blood-brain barrier, is enzymatically converted in the brain to dopamine resulting in an increase in dopamine levels:The conversion of L-dopa to dopamine is catalyzed by aromatic L-amino acid decarboxylase, a ubiquitous enzyme that promotes central as well as peripheral metabolism of L-dopa to dopamine. Due to the peripheral metabolism of L-dopa, a relatively large dose of L-dopa is required to achieve therapeutically effective dopamine levels in the brain. Administration of such large L-dopa doses results in elevated peripheral ...

Carbidopa and L-Dopa Prodrugs and Methods of Use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease. 2. The pharmaceutical combination of claim 1 , wherein the first compound or pharmaceutically acceptable salt thereof claim 1 , and the second compound or pharmaceutically acceptable salt thereof are present in separate pharmaceutical compositions.3. The pharmaceutical combination of claim 1 , wherein the first compound or pharmaceutically acceptable salt thereof claim 1 , and the second compound or pharmaceutically acceptable salt thereof are present in a same pharmaceutical composition.9. The pharmaceutical combination of claim 1 , wherein a weight ratio of the first compound or pharmaceutically acceptable salt thereof to the second compound or pharmaceutically acceptable salt thereof is from about 1:4 to about 1:10.10. The pharmaceutical combination of claim 1 , wherein the combination is an aqueous combination suitable for intragastric claim 1 , subcutaneous claim 1 , intramuscular claim 1 , intrajejunum claim 1 , oral claim 1 , intranasal or intravenous administration.11. The pharmaceutical combination of claim 1 , wherein the combination is an aqueous combination suitable for subcutaneous administration.12. The pharmaceutical combination of claim 1 , wherein the first compound or pharmaceutically acceptable salt thereof has a solubility of at least about 200 mg/ml in aqueous solution at about neutral pH claim 1 , and the second compound or pharmaceutically acceptable salt thereof has a solubility of at least about 400 mg/ml in aqueous solution at about neutral pH.14. The compound or pharmaceutically acceptable salt of claim 13 , wherein Rand Rare each independently selected from the group consisting of hydrogen claim 13 , ...

Acoustic mixing for auto granulation

A process for acoustically mixing a bulk drug substance involves the application of acoustic energy to drive an accelerative force in a mixing vessel containing the drug substance. The drug substance may be, for example, Elagolix.

Carbidopa prodrugs

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Carbidopa Prodrug

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease. 130-. (canceled) The present disclosure relates to (a) carbidopa prodrugs, (b) L-dopa prodrugs, (c) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (d) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.Parkinson's disease is a chronic and progressive neurodegenerative condition characterized by reduced levels in the brain of the neurotransmitter dopamine (i.e., 3,4-dihydroxyphenethylamine). Administration of L-dopa (i.e., L-3,4-dihydroxyphenylalanine) currently is the most effective therapy for treating a patient with Parkinson's disease. L-dopa, which unlike dopamine can cross the blood-brain barrier, is enzymatically converted in the brain to dopamine resulting in an increase in dopamine levels:The conversion of L-dopa to dopamine is catalyzed by aromatic L-amino acid decarboxylase, a ubiquitous enzyme that promotes central as well as peripheral metabolism of L-dopa to dopamine. Due to the peripheral metabolism of L-dopa, a relatively large dose of L-dopa is required to achieve therapeutically effective dopamine levels in the brain. Administration of such large L-dopa doses results in elevated peripheral dopamine levels that can cause nausea in some patients. To overcome these problems, L-dopa generally is co-administered with a peripheral aromatic L-amino acid decarboxylase inhibitor such as carbidopa (i.e., (2S)-3-(3,4-dihydroxyphenyl)-2-hydrazino-2-methylpropanoic acid):Co-administration of carbidopa with L-dopa inhibits the peripheral metabolism ...

Carbidopa and l-dopa prodrugs and method of use thereof

【課題】パーキンソン病および関連状態の治療するための組成物の提供。【解決手段】式（I-a)等のカルビドパプロドラッグと式（II-a)等のＬ−ドーパプロドラッグを含む医薬組み合わせ及び組成物。【選択図】なし

Carbidopa and l-dopa prodrugs and methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Carbidopa and l-dopa prodrugs and methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Carbidopa and L-dopa prodrugs and their use to treat Parkinson's disease

Composición farmacéutica que comprende un primer compuesto que corresponde en estructura a la Fórmula (I):**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que R1 y R2 se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, -P(O)(OH)2 y -R5-O-P(O)(OH)2; R5 es un alquilo C1-C4; R6 es hidrógeno o un alquilo C1-C4; y siempre que al menos uno de R1 y R2 sea -P(O)(OH)2 o -R5-O-P(O)(OH)2; y el segundo compuesto que corresponde en estructura a la Fórmula (II):**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que R3 y R4 se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, -P(O)(OH)2 y -R5-O-P(O)(OH)2; R5 es un alquilo C1-C4; R6 es hidrógeno o un alquilo C1-C4; y siempre que al menos uno de R3 y R4 sea -P(O)(OH)2 o -R5-O-P(O)(OH)2.

Προφαρμακα καρβιντοπας και l-ντοπας και η χρηση τους στην αγωγη της νοσου parkinson

Η παρούσα αποκάλυψη αναφέρεται σε (a) προφάρμακα καρβιντόπας, (b) φαρμακευτικούς συνδυασμούς και συνθέσεις που περιλαμβάνουν ένα προφάρμακο καρβιντόπας και/ή ένα προφάρμακο L-ντόπας και (c) μεθόδους αγωγής της νόσου Parkinson και σχετικών παθήσεων που περιλαμβάνουν τη χορήγηση ενός προφαρμάκου καρβιντόπας και ενός προφαρμάκου L-ντόπας σε ένα άτομο με νόσο Parkinson.

Carbidopa and l-dopa prodrugs and methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

カルビドパおよびｌ－ドーパプロドラッグならびにそれらの使用方法

【課題】パーキンソン病および関連状態の治療するための組成物の提供。【解決手段】式（I-a)等のカルビドパプロドラッグと式（II-a)等のＬ－ドーパプロドラッグを含む医薬組み合わせ及び組成物。TIFF2023174770000165.tif75164【選択図】なし

Elagolix sodium compositions and processes

Elagolix sodium compositions and processes

Elagolix sodium compositions and processes

Acoustic mixing for auto granulation

A process for acoustically mixing a bulk drug substance involves the application of acoustic energy to drive an accelerative force in a mixing vessel containing the drug substance. The drug substance may be, for example, Elagolix.

Carbidopa and L-dopa prodrugs and methods of use

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.