Raqualia Pharma Inc.

Pfizer Corporation

Askat Inc.

Requalia Pharma Inc.

Toyoharu Numata

Chikara Uchida

Koji Ando

Masaki Sudo

Yoshinori Murata

Noriaki Murase

Hiroki Sone

Tatsuo Ueki

Satoru Iguchi

Takashi Kojima

Tomoki Kato

Yoshiyuki Okumura

Hirohide Noguchi

Hiroaki Wakabayashi

Takako Okumura

Yasuhiro Iwata

Kaoru Shimada

Hideyuki Aoyama

Nobuaki Waizumi

Xufeng Sun

Zheng Jane Li

Kaori Muraji

Andrew Vincent Trask

Saturu Iguchi

Naoaki Haruta

The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms of Polymorph Form I, Polymorph Form II, Polymorph Form III, Polymorph Form IV, Polymorph Form V, and Polymorph Form VI, and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.

Polymorph forms

Salts of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid are disclosed. More particularly, salt forms (HCl-salt, HBr-salt, p-toluenesulfonate salt and ethanedisulfonate salt) are disclosed. Furthermore, processes for the preparation of such salt forms, compositions containing such salt forms, and uses of such salt forms are disclosed. A method of treating disease conditions mediated by 5-HT4 receptor activity includes administering an effective amount of such salt forms to an animal, including a human, in need of such treatment.

Benzisoxazole derivative salt

The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.

This invention relates to salts and crystal forms of (S)-6-chloro-7-(1,1-dimethylethyl)-2-trifluoromethyl-2H-1-benzopyran-3-carboxylic acid, Compound A, which is cyclooxygenase-2 inhibitor. The present invention provides a salt of compound A, a crystal form thereof, a process for preparing the said salt and a pharmaceutical composition thereof and its use. The salts and/or co-crystals of Compound A of the present invention show good formulation properties such as high aqueous solubility, good intrinsic dissolution, good crystallinity, good thermal stability or low hygroscopicity.

Salts and crystal forms

The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.

Polymorph form of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid

The invention relates to the essentially pure &#x39b;/-[({2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl}amino)carbonyl]-4-methylbenzenesulfonamide Polymorph Forms A and B and to processes for the preparation of, compositions containing and to the uses of, such crystal forms.

Crystal forms of an imidazole derivative

This invention relates to compounds of the formula (I): wherein R, R, R, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HTreceptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.

Benzimidazolone carboxylic acid derivatives

Growing community of inventors

Aichi, Japan

Toyoharu Numata