Pfizer Corporation

Raqualia Pharma Inc.

Pfizer Pharmaceuticals, Inc.

Akiyoshi Kawai

Tomoki Kato

Rodney W Stevens

Yoshiyuki Okumura

Kazuo Ando

Makoto Kawai

Tomomi Nonomura

Seiji Nukui

Kazunari Nakao

Yoshinobu Hashizume

Kana Taniguchi

Miyako Matsumizu

Katsuhiro Shinjyo

Yoriko Miyake

Naomi Ueno

Takashi Mano

Takafumi Ikeda

Hengmiao Cheng

Yoshinori Murata

Junji Takada

Minoru Sakakibara

Naomi Uneo

This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y, Y, Yand Yare independently selected from N, CH, etc.; Ris H, Calkyl, etc.; Qis a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is Calkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; Ris H, Calkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, Calkyl, etc.; m is 0, 1 or 2; Rand Rare independently selected from H and Calkyl ; Ris H, Calkyl, etc.; Qis a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamadin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents

This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y, Y, Yand Yare independently selected from N, CH, etc.; Ris H, Calkyl, etc.; Qis a 5&#x2013;12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5&#x2013;6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is Calkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; Ris H, Calkyl, etc.; Z is a 5&#x2013;12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, Calkyl, etc.; m is 0, 1 or 2; Rand Rare independently selected from H and Calkyl; Ris H, Calkyl, etc.; Qis a 5&#x2013;12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.

This invention provides a compound of the formula:or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; Ris optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, Ris heteroaryl; Ris Calkyl; halo-substituted Calkyl, Calkylamino, Cdialkylamino or amino; R, Rand Rare independently hydrogen, halo, Calkyl, halo-substituted Calkyl or the like; or two of R, Rand Rare taken together with atoms to which they are attached and form a 4-7 membered ring. Rand Rare independently hydrogen, halo, Calkyl, halo-substituted Calkyl, Calkoxy, Calkylthio, Calkylamino or N,N-di Calkylamino; and m and n are independently 1, 2, 3 or 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

Sulfonylbenzene compounds as anti-inflammatory/analgesic agents

Pyridylthiophene compounds

Acetylene derivatives as anti-inflammatory/analgesic agents

Pyridylpyrrole compounds useful as interleukin-and TNF antagonists

This invention provides a compound of the formula:

Certain novel hydroxamic acid derivatives having the structure

Hydroxamic acid and N-hydroxyurea derivatives and their use

A compound of the formula: ##STR1## and its pharmaceutically effective salts, wherein R.sup.1 and R.sup.2 are independently selected from the following: (a) hydrogen, halo, R.sup.5 --, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, hydroxy-R.sup.5 --, R.sup.5 --O--R.sup.5 --, or the like; (b) Ar--, Ar--R.sup.5 --, Ar--C.sub.2-6 alkenyl, Ar--C.sub.2-6 alkynyl, Ar--O--, Ar--O--R.sup.5 -- or the like; (c) R.sup.5 --C(O)--, --NO.sub.2, cyano, NH.sub.2 --C(O)--, R.sup.5 --NH--C(O)--, (R.sup.5).sub.2 --N--C(O)--, Ar--C(O)-- or the like; and (d) R.sup.5 --C(O)--NH--, Ar--C(O)--NH-- or the like; wherein Ar is optionally substituted aryl or heteroaryl such as phenyl and pyridyl; and wherein R.sup.5 is optionally halo-substituted C.sub.1-6 alkyl; R.sup.3 is selected from the following: (e) cyano, formyl, tetrazolyl, triazolyl, imidazolyl, oxazolyl, thiazolyl, R.sup.5 --C(O)--, C.sub.2-6 alkenyl-C(O)--, C.sub.2-6 alkynyl-C(O)--, R.sup.5 --C(O)--R.sup.5 --, or the like; (f) R.sup.5 --C(O)--NH--, Ar--C(O)--NH--, or the like; (g) R.sup.5 --S--, R.sup.5 --S(O)--, R.sup.5 --NH--S(O).sub.2 --, or the like; and (h) Ar--C(O)--, Ar--R.sup.5 --C(O)--, Ar--C.sub.2-6 alkenylene-C(O)-- or the like; or two of R.sup.1, R.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --B.sup.1 --A.sup.2 -- or --A.sup.1 --B.sup.1 --A.sup.3 --B.sup.2 --A.sup.2 -- such as cyclic alkyl optionally substituted with oxo; R.sup.4 is hydrogen, halo, R.sup.5 --C(O)-- and the like; X is O, S, S(O) or S(O).sub.2 ; m is 0, 1, 2, 3 or 4. The present invention also provides processes for the preparation thereof, the use thereof in treating cytokine mediated diseases and/or cell adhesion molecule (CAM) mediated diseases and pharmaceutical compositions for use in such therapy.

Pyridylfuran and pyridylthiophene compounds

Aryloxycycloalkenyl and aryloxyiminocycloalkenylhydroxyureas

Phenoxyphenyl cyclopentenyl hydroxyureas

Heteroaryl cycloalkenyl hydroxyureas

Growing community of inventors

Chita-gun, Japan

Akiyoshi Kawai