Crystalline forms of (r)-8-chloro-1-methyl- 2,3,4,5-tetrahydro-1h-3-benzazepine hydrochloride

Patent metadata

Field	Value
Publication number	US-2016009654-A1
Application number	US-201514635146-A
Country	US
Kind code	A1
Filing date	Mar 2, 2015
Priority date	Dec 21, 2004
Publication date	Jan 14, 2016
Grant date	—

Abstract

The present invention is directed to crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, compositions containing the same and uses thereof.

First claim

1 .- 40 . (canceled)

41 . A crystal form of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (Form I).

42 . A composition comprising the crystal form of claim 41 .

43 . A composition comprising the crystal form of claim 41 and a pharmaceutically acceptable carrier.

44 . A method of treatment of obesity comprising administering to an individual in need of such treatment a therapeutically effective amount of the crystal form of claim 41 .

45 . A method of decreasing food intake comprising administering to an individual in need of such administration a therapeutically effective amount of the crystal form of claim 41 .

46 . A method of inducing satiety comprising administering to an individual in need of such administration a therapeutically effective amount of the crystal form of claim 41 .

47 . A method of controlling weight gain comprising administering to an individual in need of such administration a therapeutically effective amount of the crystal form of claim 41 .

48 . A process for preparing a crystal form of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (Form I) comprising the step of:
heating crystalline (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride, where the crystalline (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride contains one or more crystalline forms other than Form I.

49 . The process of claim 48 , wherein the crystalline (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride comprises (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (Form II).

50 . The process of claim 48 , wherein the crystalline (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride comprises (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride hemihydrate (Form III).

51 . The process of claim 48 , wherein the crystalline (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride comprises a mixture of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (Form II) and (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride hemihydrate (Form III).

52 . The process of claim 48 , wherein the crystalline (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride is heated at a temperature of at least about 60° C.

53 . A crystal form of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (Form I) prepared by the process of claim 48 .

54 . A method of preparing a pharmaceutical composition comprising mixing (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (Form I) with a pharmaceutically acceptable carrier.

55 . The method of claim 14 , wherein the (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (Form I) is prepared by a method of claim 48 .

56 . A method according to claim 54 , further comprising forming the pharmaceutical composition into a tablet, a pill, a powder, a soft or hard gelatin capsule, or a sterile packaged powder.

57 . A solid pharmaceutical composition prepared by the method of claim 54 .

58 . A solid pharmaceutical composition prepared by the method of claim 56 , wherein the pharmaceutical composition is in a form chosen from a tablet, a pill, a powder, a soft or hard gelatin capsule, or a sterile packaged powder.

Assignees

• Arena Pharm Inc

Inventors

• Agarwal Rajesh Kumar
• Betts Iii William L
• Henshilwood James A
• Kiang Yuan-Hon
• Post Noah

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P7/12

  Antidiuretics, e.g. drugs for diabetes insipidus (ADH A61P5/10) · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P25/30

  for treating abuse or dependence · CPC title