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1. 发明授权

US5521212A Cyclopropyl N-hydroxyurea and N-hydroxyacetamides which inhibit lipoxygenase 失效
标题翻译：抑制脂氧合酶的环丙基N-羟基脲和N-羟基乙酰胺
公开(公告)号：US5521212A
公开(公告)日：1996-05-28
申请号：US244739
申请日：1994-08-26
申请人： Takafumi Ikeda , Akiyoshi Kawai , Takashi Mano , Yoshiyuki Okumura , Rodney W. Stevens
发明人： Takafumi Ikeda , Akiyoshi Kawai , Takashi Mano , Yoshiyuki Okumura , Rodney W. Stevens
IPC分类号： C07C259/06 , C07C275/64 , C07C323/44 , C07D295/15 , A61K31/40 , A61K31/33 , A61K31/445 , C07D295/195
CPC分类号： C07D295/15 , C07C259/06 , C07C275/64 , C07C323/44 , C07C2101/02
摘要： Compounds of the formula ##STR1## wherein A is C1 to C3 alkylene, Ar is phenyl or styryl, R is halosubstituted C1 to C3 alkyl, NHR' or ##STR2## R' is hydrogen or C2 to C8 alkytthioalkyl, n is an integer of from 1 to 4 and p is an integer of from 2 to 5, with the proviso that when R' is hydrogen then Ar is styryl, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.
摘要翻译： PCT No.PCT / US92 / 08979 Sec。 371日期1991年8月26日 102（e）1991年8月26日PCT PCT 1991年10月27日PCT。其中A为C1至C3亚烷基，Ar为苯基或苯乙烯基的式为“IMAGE”的化合物，R为卤素取代的C1至C3烷基，NHR'或 R 1为氢或C 2至C 8烷硫基烷基，n为1至4的整数，p为2至5的整数，条件是当R'为氢时Ar为苯乙烯基，其可接受的盐抑制酶脂氧合酶，并且可用于治疗已经涉及脂加氧酶的作用的过敏和炎性和心血管疾病。这些化合物在用于治疗这些病症的药物组合物中形成活性成分。

2. 发明授权

US06291520B1 Hydroxamic acid and N-hydroxyurea derivatives and their use 失效
标题翻译：羟肟酸和N-羟基脲衍生物及其用途
公开(公告)号：US06291520B1
公开(公告)日：2001-09-18
申请号：US08070327
申请日：1993-06-28
申请人： Takafumi Ikeda , Akiyoshi Kawai , Takashi Mano , Yoshiyuki Okumura , Rodney William Stevens
发明人： Takafumi Ikeda , Akiyoshi Kawai , Takashi Mano , Yoshiyuki Okumura , Rodney William Stevens
IPC分类号： A61K3127
CPC分类号： C07D271/07 , C07C275/64 , C07C311/59 , C07C323/47 , C07C335/40 , C07C2601/04 , C07C2601/08 , C07D307/52
摘要： Certain novel hydroxamic acid derivatives having the structure inhibit the enzyme lipoxygenase. These compounds, and the pharmaceutically acceptable salts thereof, are useful in the treatment or alleviation of inflammatory diseases, allergic conditions and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
摘要翻译：某些具有抑制酶脂氧合酶结构的新型异羟肟酸衍生物。这些化合物及其药学上可接受的盐可用于治疗或缓解哺乳动物中的炎性疾病，过敏性疾病和心血管疾病，并且可用作用于治疗这些病症的药物组合物中的活性成分。

3. 发明授权

US5792882A Phenoxyphenyl cyclopentenyl hydroxyureas 失效
标题翻译：苯氧基苯基环戊烯基羟基脲
公开(公告)号：US5792882A
公开(公告)日：1998-08-11
申请号：US591634
申请日：1996-05-24
申请人： Akiyoshi Kawai , Rodney W. Stevens
发明人： Akiyoshi Kawai , Rodney W. Stevens
IPC分类号： A61K31/17 , A61P9/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07C275/26 , C07C275/64 , C07C53/02
CPC分类号： C07C275/64 , A61K31/17 , C07C2101/10
摘要： The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein R.sup.1 is hydrogen, fluoro, or chloro, and R.sup.2 is hydrogen or methyl. The above compounds are lipoxygenase inhibitors. The invention also relates to pharmaceutical compositions containing the above compounds, and to methods of treating inflammatory and allergic conditions by administering the above compounds.
摘要翻译： PCT No.PCT / JP94 / 01349 Sec。 371日期：1996年5月24日 102（e）日期1996年5月24日PCT提交1994年8月15日PCT公布。公开号WO95 / 05360 日期1995年2月23日本发明涉及式IMA的化合物及其药学上可接受的盐，其中R 1是氢，氟或氯，R 2是氢或甲基。上述化合物是脂氧合酶抑制剂。本发明还涉及含有上述化合物的药物组合物，以及通过施用上述化合物治疗炎性和过敏症状的方法。

4. 发明授权

US5798383A Aryloxycycloalkenyl and aryloxyiminocycloalkenylhydroxyureas 失效
公开(公告)号：US5798383A
公开(公告)日：1998-08-25
申请号：US836452
申请日：1997-05-08
申请人： Akiyoshi Kawai , Makoto Kawai , Rodney W. Stevens
发明人： Akiyoshi Kawai , Makoto Kawai , Rodney W. Stevens
IPC分类号： C07C275/26 , A01N47/28 , A61K20060101 , A61K31/17 , A61K31/275 , A61K31/34 , A61K31/38 , A61K31/435 , A61K31/44 , A61K31/47 , A61K31/557 , A61P29/00 , C07C20060101 , C07C67/02 , C07C69/66 , C07C69/76 , C07C273/18 , C07C275/64 , C07C309/23 , C07C309/27 , C07C313/02 , C07C317/22 , C07C317/42 , C07C323/18 , C07C323/43 , C07C323/47 , C07C323/65 , C07D213/24 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/60 , C07D213/63 , C07D215/12 , C07D215/14 , C07D215/16 , C07D215/20 , C07D307/38 , C07D307/52 , C07D307/56 , C07D307/58 , C07D307/78 , C07D307/79 , C07D307/81 , C07D307/82 , C07D307/83 , C07D333/06 , C07D333/26 , C07D333/32 , C07D333/54 , C07D333/62 , C07D333/64 , C12N20060101
CPC分类号： C07C275/64
摘要： The prevent invention provides a compound of formula (I): ##STR1## wherein Ar is (a) phenyl, naphthyl and biphenyl, each optionally substituted with C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 hydroxyalkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkoxy, C.sub.2-4 alkoxyalkoxy, C.sub.1-4 alkylthio, hydroxy, halo, cyano, amino, C.sub.1-4 alkylamino, di (C.sub.2-8) alkylamino, C.sub.2-6 alkanoylamino, carboxy, C.sub.2-6 alkoxycarbonyl, or optionally substituted phenyl, phenoxy, phenylthio or phenylsulfinyl or (b) furyl, benzo�b!furyl, thienyl, benzo�b!thienyl, pyridyl or quinolyl, each optionally substituted with C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halo, C.sub.1-4 alkoxy, optionally-substituted phneyl, phenoxy or phenylthio, X is C.sub.1 -C.sub.4 alkylene, C.sub.2 -C.sub.4 alkenylene, --(CHR.sup.1).sub.m --Q.sup.1 --(CHR.sup.2).sub.n --, --O--(CHR.sup.1).sub.j --Q.sup.2 -- and --(CHR.sup.1)--O--N.dbd. in which the N.dbd. moiety is attached to the cycloalkene ring; and in which Q.sup.1 is O, S, SO, SO.sub.2, NR.sup.3, CH.dbd.N--O or CO, Q.sup.2 is O, S, SO, SO.sub.2 or NR.sup.3, and R.sup.1, R.sup.2 and R.sup.3 are each hydrogen or C.sub.1 -C.sub.4 alkyl, m and n are each an integer from 0 to 4 and j is an integer from 1 to 4; p is an integer of 1 or 2; Y is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, C.sub.1-4 alkoxy, C.sub.2-4 alkoxyalkyl, C.sub.1-4 alkylthio, hydroxy, halo, cyano or amino; Z is hydrogen or C.sub.1-4 alkyl; and M is hydrogen, a pharmaceutically acceptable cation or a pharmaceutically acceptable metabolically cleavable group. Further the invention provides a pharmaceutical composition for treating a medical condition for which a 5-lipoxygenase inhibitor is needed in a mammalian subject which comprises a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. Preferably the medical condition is an inflammatory disease, allergy or cardiovascular diseases.

5. 发明授权

US5665768A Heteroaryl cycloalkenyl hydroxyureas 失效
标题翻译：杂芳基环烯基羟基脲
公开(公告)号：US5665768A
公开(公告)日：1997-09-09
申请号：US586833
申请日：1996-01-18
申请人： Akiyoshi Kawai , Rodney W. Stevens
发明人： Akiyoshi Kawai , Rodney W. Stevens
IPC分类号： C07D307/52 , A61K31/17 , A61K31/34 , A61K31/341 , A61P9/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D307/58
CPC分类号： C07D307/58
摘要： Certain novel heteroaryl cycloalkenyl hydroxyurea compounds having the ability to inhibit the 5-lipoxygenase enzyme and having formula (I) and the pharmaceutically acceptable salts thereof, wherein each R.sup.1, independently, is hydrogen, hydroxy, chloro, fluoro, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl or C.sub.1 -C.sub.4 haloalkoxy; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.3 is hydrogen, chloro, fluoro or C.sub.1 -C.sub.4 alkyl; X is O, S, SO or SO.sub.2 ; Z is methylene or ethylene; A is divalent radical derived from furan, thiophene, pyridine, benzofuran, benzothiophene or quinoline, or one of these groups having one substituent selected from chloro, fluoro, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl and C.sub.1 -C.sub.4 haloalkoxy; n is 1, 2 or 3; and M is hydrogen or a pharmaceutically acceptable cation. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.
摘要翻译： PCT No.PCT / JP94 / 01093 Sec。 371日期：1996年1月18日 102（e）1996年1月18日PCT PCT 1994年7月5日PCT公布。公开号WO95 / 03292 日期1995年2月2日具有抑制5-脂氧合酶并具有式（I）的能力的新型杂芳基环烯基羟基脲化合物及其药学上可接受的盐，其中每个R 1独立地是氢，羟基，氯，氟，C 1 C 1-4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基或C 1 -C 4卤代烷氧基; R2是氢或C1-C4烷基; R3是氢，氯，氟或C1-C4烷基; X是O，S，SO或SO 2; Z是亚甲基或亚乙基; A是衍生自呋喃，噻吩，吡啶，苯并呋喃，苯并噻吩或喹啉的二价基团，或这些具有一个选自氯，氟，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基和C 1 -C 4 卤代烷氧基 n为1,2或3; 和M是氢或药学上可接受的阳离子。这些化合物可用于治疗或缓解哺乳动物的炎性疾病，变态反应和心血管疾病，并用作治疗这些病症的药物组合物中的活性成分。

6. 发明授权

US07141580B2 Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents 有权
标题翻译：芳基或杂芳基稠合咪唑化合物作为抗炎和止痛剂
公开(公告)号：US07141580B2
公开(公告)日：2006-11-28
申请号：US10771696
申请日：2004-02-04
申请人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
发明人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
IPC分类号： A61K31/437
CPC分类号： C07D213/75 , A61K31/00 , A61K31/4178 , A61K31/437 , A61K31/64 , C07D231/12 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18 , C07D235/30 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , Y02P20/55
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is 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 C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, 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, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl, etc.; Q2 is 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 prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中Y 1，Y 2，Y 3和 Y 4独立地选自N，CH等; R 1是H，C 1-8烷基等; Q 1是5-12元单环或双环芳族环，任选地含有至多4个选自O，N和S的杂原子等; A是任选含有至多3个选自O，N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH，O等; R 2是H，C 1-4烷基等; Z是任选地含有至多3个选自O，N和S的杂原子的5-12元单环或双环芳环等; L为卤素，C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R 5是H，C 1-4烷基等; Q 2是5-12元单环或双环芳族环或三环，任选地含有至多3个选自O，N和S的杂原子等。这些化合物可用于治疗介导的医学病症通过前列腺素如疼痛，发烧或炎症等。本发明还提供了包含上述化合物的药物组合物。

7. 发明授权

US06710054B2 Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents 有权
标题翻译：芳基或杂芳基稠合咪唑化合物作为抗炎和止痛剂
公开(公告)号：US06710054B2
公开(公告)日：2004-03-23
申请号：US09977621
申请日：2001-10-15
申请人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
发明人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
IPC分类号： A61K31437
CPC分类号： C07D213/75 , A61K31/00 , A61K31/4178 , A61K31/437 , A61K31/64 , C07D231/12 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18 , C07D235/30 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , Y02P20/55
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N, and S, etc.; A is 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; B is C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected form O, N and S, etc.; L is halo, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl; R5 is H, C1-4 alkyl; etc.; Q2 is 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 prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中Y 1，Y 2，Y 3和Y 4独立地选自N，CH等; R 1是H，C 1-8烷基等; Q 1是任选地含有至多4个选自O，N和S的杂原子的5-12元单环或双环芳环等; A是任选含有至多3个选自O，N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH，O等; R 2是H，C 1-4烷基等; Z是任选地含有至多3个选自O，N和S等的杂原子的5-12元单环或双环芳环; L是卤素，C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R 5是H，C 1-4烷基; 等等。; Q 2是任选地含有至多3个选自O，N和S的杂原子的5-12元单环或双环芳族环或三环，这些化合物可用于治疗由前列腺素介导的医学病症如疼痛，发热或炎症等。本发明还提供包含上述化合物的药物组合物。

8. 发明申请

US20070155732A1 Aryl or Heteroaryl Fused Imidazole Compounds as Anti-Inflammatory and Analgesic Agents 有权
标题翻译：芳基或杂芳基稠合咪唑化合物作为抗炎和镇痛药
公开(公告)号：US20070155732A1
公开(公告)日：2007-07-05
申请号：US11556523
申请日：2006-11-03
申请人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
发明人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4745 , C07D471/02
CPC分类号： C07D213/75 , A61K31/00 , A61K31/4178 , A61K31/437 , A61K31/64 , C07D231/12 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18 , C07D235/30 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , Y02P20/55
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is 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 C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, 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, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl ; R5 is H, C1-4 alkyl, etc.; Q2 is 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.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中Y 1，Y 2，Y 3和 Y 4独立地选自N，CH等; R 1是H，C 1-8烷基等; Q 1是5-12元单环或双环芳族环，任选地含有至多4个选自O，N和S的杂原子等; A是任选含有至多3个选自O，N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH，O等; R 2是H，C 1-4烷基等; Z是任选地含有至多3个选自O，N和S的杂原子的5-12元单环或双环芳环等; L为卤素，C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R 5是H，C 1-4烷基等; Q 2是5-12元单环或双环芳族环或三环，任选地含有至多3个选自O，N和S的杂原子等。这些化合物可用于治疗介导的医学病症通过前列腺炎如疼痛，发热或炎症等。本发明还提供包含上述化合物的药物组合物。

9. 发明授权

US07479564B2 Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents 有权
标题翻译：芳基或杂芳基稠合咪唑化合物作为抗炎和止痛剂
公开(公告)号：US07479564B2
公开(公告)日：2009-01-20
申请号：US11556523
申请日：2006-11-03
申请人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
发明人： Kazunari Nakao , Yoshiyuki Okumura , Miyako Matsumizu , Naomi Ueno , Yoshinobu Hashizume , Tomoki Kato , Akiyoshi Kawai , Yoriko Miyake , Seiji Nukui , Katsuhiro Shinjyo , Kana Taniguchi
IPC分类号： A61K31/4184 , C07D235/06
CPC分类号： C07D213/75 , A61K31/00 , A61K31/4178 , A61K31/437 , A61K31/64 , C07D231/12 , C07D233/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18 , C07D235/30 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , Y02P20/55
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y1, Y2, Y3 and Y4 are independently selected from N, CH, etc.; R1 is H, C1-8 alkyl, etc.; Q1 is 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 C1-6 alkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; R2 is H, C1-4 alkyl, 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, C1-4 alkyl, etc.; m is 0, 1 or 2; R3 and R4 are independently selected from H and C1-4 alkyl ; R5 is H, C1-4 alkyl, etc.; Q2 is 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.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中Y 1，Y 2，Y 3和Y 4独立地选自N，CH等; R1是H，C1-8烷基等; Q1是任选地含有至多4个选自O，N和S的杂原子的5-12元单环或双环芳环; A是任选含有至多3个选自O，N和S的杂原子的5-6元单环芳环等; B是任选被氧代基取代的C 1-6亚烷基等; W是NH，O等; R2是H，C1-4烷基等; Z是任选地含有至多3个选自O，N和S的杂原子的5-12元单环或双环芳环等; L是卤素，C 1-4烷基等; m为0,1或2; R 3和R 4独立地选自H和C 1-4烷基; R5是H，C1-4烷基等; Q2是任选地含有至多3个选自O，N和S等杂原子的5-12元单环或双环芳族环或三环，这些化合物可用于治疗前列腺素介导的医学病症，例如疼痛，发热或炎症等。本发明还提供包含上述化合物的药物组合物。

10. 发明授权

US06417202B1 Pyridylpyrrole compounds useful as interleukin-and TNF antagonists 失效
标题翻译：可用作白细胞介素和TNF拮抗剂的吡啶基吡咯化合物
公开(公告)号：US06417202B1
公开(公告)日：2002-07-09
申请号：US09214573
申请日：1999-12-10
申请人： Akiyoshi Kawai , Makoto Kawai , Yoshinori Murata , Junji Takada , Minoru Sakakibara
发明人： Akiyoshi Kawai , Makoto Kawai , Yoshinori Murata , Junji Takada , Minoru Sakakibara
IPC分类号： A61K314427
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14 , C07D491/04 , C07D491/10
摘要： The present invention provides a compound of the formula: and its pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5 and m are as defined in claim 1. The present invention also provides processes for the preparation thereof, the use thereof in treating cytokines mediated diseases and/or cell adhesion molecules (CAMs) mediated diseases and pharmaceutical compositions for use in such therapy.
摘要翻译：本发明提供下式的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5和m如权利要求1中所定义。本发明还提供其制备方法，治疗细胞因子介导的疾病和/或细胞粘附分子（CAM）介导的疾病和用于这种治疗的药物组合物。

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