Pfizer Corporation

Raqualia Pharma Inc.

Hiroaki Wakabayashi

Kunio Satake

Masami Nakane

Fumitaka Ito

Yuji Shishido

Toshihide Kokura

Takafumi Ikeda

Masaya Ikunaka

Rodney W Stevens

Kazuo Ando

Kaoru Shimada

Toyoharu Numata

Masaki Sudo

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.

Polymorph forms

Substituted benzylaminopiperidine compounds

The invention provides a substituted benzylaminopiperidine compounds that are useful in the treatment of gastrointestinal disorders; central nervous system (CNS) disorders; inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by,or angiogenesis, especially CNS disorders in a mammalian subject, especially in humans.

Substituted benzolactam compounds as substance P antagonists

Benzyloxyquinuclidines as substance P antagonists

##STR1## Compounds of formula (1), wherein W, Ar.sup.1, Ar.sup.2 and Ar.sup.3 are defined as below; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

Substituted 3-aminoquinuclidines

Substituted quinuclidines as substance P antagonists

This invention provides a compound of the formula: ##STR1## and its pharmaceutically acceptable salts, wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, halo C.sub.1 -C.sub.6 alkyl or terahydropyranyl, having one or more substituents selected from cyano, 1,3-thiazolanyl, COOR.sup.2, COR.sup.2, OCOR.sup.2, CONR.sup.3 R.sup.4, NR.sup.3 R.sup.4, NR.sup.5 COR.sup.3 and C.ident.CR.sup.6, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sup.3 and R.sup.4 are independently hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl, R.sup.5 is C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl and R.sup.6 is hydrogen, halo, cyano, C.sub.1 -C.sub.6 alkyl, COOH, COO(C.sub.1 -C.sub.4 alkyl) or phenyl; X is C.sub.1 -C.sub.6 alkoxy or halo C.sub.1 -C.sub.6 alkoxy; and Ar is phenyl optionally substituted with halo. These compounds are useful in the treatment of allergic disorders, angiogenesis, gastrointestinal disorders, central nervous system disorders, inflammatory diseases, emesis, urinary incontinence, pain, migraine, sunburn, and diseases, disorders and adverse conditions caused by Helicobacter pylori, in a mammalian subject.

3-�5-substituted benzyl)amino!-2-phenylpiperidines as substance P

Quinuclidine derivatives as substance P antagonists

Aminobenzosultam derivatives, which are inhibitors of lipoxygenase, having the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Ar is cycloalkyl having five to seven carbon atoms, tetrahydropyranyl, pyridyl, oxazolyl, phenyl or substituted phenyl wherein said substituent is methyl, methoxy, fluoro, chloro or trifluoromethyl; n is an integer of 1 to 3; X is hydrogen, methyl, methoxy, fluoro, chloro or trifluoromethyl; Z is --NH--, --O--, or --CH.sub.2 --; and R.sup.1 is hydrogen or alkyl having one to three carbon atoms.

Aminobenzosultam derivatives as lipoxygenase inhibitors

Compounds having the structure ##STR1## wherein X is nitrogen, oxygen, sulfur or a bond and Z is oxygen or sulfur have been synthesized. These compounds are lipoxygenase inhibitors and are useful as the active agent in pharmaceutical compositions for treating inflammatory conditions in humans and other mammals for which lipoxygenase activity has been implicated.

Antiinflammatory hydroxamic acids and N-hydroxyureas

A series of 2-amino-5,6-dimethyl-1,4-benzoquinone derivatives, inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergic and antiinflammatory agents.

Growing community of inventors

Kariya, Japan

Hiroaki Wakabayashi