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1. 发明授权

US08084476B2 Substituted methyl aryl or heteroaryl amide compounds 有权
标题翻译：取代的甲基芳基或杂芳基酰胺化合物
公开(公告)号：US08084476B2
公开(公告)日：2011-12-27
申请号：US12368778
申请日：2009-02-10
申请人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： A61K31/44 , C07D211/72
CPC分类号： C07D213/74 , C07C235/42 , C07C235/46 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D213/82 , C07D213/89
摘要： This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物：其中X表示碳原子等：Y表示亚氨基等：R 1表示具有1至6个碳原子的烷基等：R 2和R 3独立地表示氢原子等。这些化合物可用于治疗由前列腺素介导的疾病状况，例如哺乳动物中的疼痛等。本发明还提供了包含上述化合物的药物组合物。

2. 发明申请

US20090163558A1 Substituted Methyl Aryl or Heteroaryl Amide Compounds 有权
标题翻译：取代的甲基芳基或杂芳基酰胺化合物
公开(公告)号：US20090163558A1
公开(公告)日：2009-06-25
申请号：US12368778
申请日：2009-02-10
申请人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： A61K31/44 , C07D213/56
CPC分类号： C07D213/74 , C07C235/42 , C07C235/46 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D213/82 , C07D213/89
摘要： This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物：其中X表示碳原子等：Y表示亚氨基等：R 1表示具有1至6个碳原子的烷基等：R 2和R 3独立地表示氢原子等。这些化合物可用于治疗由前列腺素介导的疾病状况，例如哺乳动物中的疼痛等。本发明还提供了包含上述化合物的药物组合物。

3. 发明授权

US07534914B2 Substituted methyl aryl or heteroaryl amide compounds 失效
标题翻译：取代的甲基芳基或杂芳基酰胺化合物
公开(公告)号：US07534914B2
公开(公告)日：2009-05-19
申请号：US11118497
申请日：2005-04-29
申请人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： C07C229/00
CPC分类号： C07D213/74 , C07C235/42 , C07C235/46 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D213/82 , C07D213/89
摘要： This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物：其中X表示碳原子等：Y表示亚氨基等：R 1表示具有1至6个碳原子的烷基等：R 2和R 3独立地表示氢原子等。这些化合物可用于治疗由前列腺素介导的疾病状况，例如哺乳动物中的疼痛等。本发明还提供了包含上述化合物的药物组合物。

4. 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。

5. 发明授权

US5681858A Cycloalkyl hydroxyureas 失效
标题翻译：环烷基羟基脲
公开(公告)号：US5681858A
公开(公告)日：1997-10-28
申请号：US525748
申请日：1995-10-03
申请人： Rodney William Stevens , Takashi Mano , Yoshiyuki Okumura , Masami Nakane
发明人： Rodney William Stevens , Takashi Mano , Yoshiyuki Okumura , Masami Nakane
IPC分类号： A61K31/17 , A61P29/00 , A61P37/08 , A61P43/00 , C07C273/08 , C07C273/18 , C07C275/64 , C07C323/47 , C07C273/02 , C07C275/24
CPC分类号： C07C275/64 , C07C323/47 , C07C2101/04 , C07C2101/08
摘要： The present invention provides a novel N-hydroxyurea compound of chemical formula (I) wherein R.sup.1 and R.sup.2 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl; Ar is phenyl or mono-, di- or trisubstituted phenyl; A is a valence bond or a C.sub.1 -C.sub.6 alkylene chain, optionally having one double bond or one triple bond in the chain, and optionally having one or more C.sub.1 -C.sub.4 alkyl groups attached to the chain: X is oxygen or sulfur, n is an integer of 3 to 6; M is hydrogen, pharmaceutically acceptable cation or a metabolically cleavable group: and X and A may be attached at any available position on the ring. These compounds are useful for 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 / 00567 Sec。 371 1995年10月3日第 102（e）日期1995年10月3日PCT 1994年4月5日PCT PCT。第WO94 / 22814号公报（I）本发明提供一种化学式（I）的新型N-羟基脲化合物，其中R 1和R 2各自独立地为氢或C 1 -C 4烷基; Ar是苯基或单，二或三取代的苯基; A是价键或C 1 -C 6亚烷基链，任选在链中具有一个双键或一个三键，并且任选地具有连接到链上的一个或多个C 1 -C 4烷基：X是氧或硫，n是 3〜6的整数; M是氢，药学上可接受的阳离子或代谢可切割基团：X和A可以连接在环上的任何可用位置。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，并用作用于治疗这些病症的药物组合物中的活性成分。

6. 发明授权

US07238714B2 Aryl or heteroaryl amide compounds 有权
标题翻译：芳基或杂芳基酰胺化合物
公开(公告)号：US07238714B2
公开(公告)日：2007-07-03
申请号：US10932463
申请日：2004-09-02
申请人： Kazunari Nakao , Seiji Nukui , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Kazunari Nakao , Seiji Nukui , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： C07D401/02 , A61K31/44
CPC分类号： C07C233/87 , C04B35/632 , C07C235/60 , C07C255/57 , C07D213/643 , C07D213/65 , C07D213/82 , C07D257/04 , C07D401/12 , C07D417/12
摘要： This invention provides a compound of the formula (I): wherein A represents a phenyl group or the like: B represents an aryl or the like: E represents a 1,4-phenylene group; R1 and R2 independently represent a hydrogen atom or the like: R3 and R4 independently represent a hydrogen atom or the like: R5 represents —CO2H or the like: R6 represents an alkyl group having from 1 to 6 carbon atoms or the like: X represents a methylene group or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物：其中A表示苯基等：B表示芳基等：E表示1,4-亚苯基; R 1和R 2独立地表示氢原子等：R 3和R 4独立地表示氢原子，氢原子等：R 5表示-CO 2 H等：R 6表示具有1至6个碳原子的烷基原子等：X表示亚甲基等。这些化合物可用于治疗由前列腺素介导的疾病状况，例如哺乳动物中的疼痛等。本发明还提供了包含上述化合物的药物组合物。

7. 发明申请

US20050267170A1 Substituted methyl aryl or heteroaryl amide compounds 失效
标题翻译：取代的甲基芳基或杂芳基酰胺化合物
公开(公告)号：US20050267170A1
公开(公告)日：2005-12-01
申请号：US11118497
申请日：2005-04-29
申请人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： A61K31/195 , A61K31/455 , C07C235/42 , C07C235/46 , C07C235/70 , C07D213/56 , C07D213/65 , C07D213/74 , C07D213/82 , C07D213/89
CPC分类号： C07D213/74 , C07C235/42 , C07C235/46 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D213/82 , C07D213/89
摘要： This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物：其中X表示碳原子等：Y表示亚氨基等：R 1表示具有1至6个碳原子的烷基 R 2，R 3和R 3独立地表示氢原子等。这些化合物可用于治疗由前列腺素介导的疾病状况，例如哺乳动物中的疼痛等。本发明还提供了包含上述化合物的药物组合物。

8. 发明申请

US20050065188A1 Aryl or heteroaryl amide compounds 有权
标题翻译：芳基或杂芳基酰胺化合物
公开(公告)号：US20050065188A1
公开(公告)日：2005-03-24
申请号：US10932463
申请日：2004-09-02
申请人： Kazunari Nakao , Seiji Nukui , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Kazunari Nakao , Seiji Nukui , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： A61P29/00 , C07C233/87 , C07C235/60 , C07C255/57 , C07D213/64 , C07D213/643 , C07D213/65 , C07D213/82 , C07D257/04 , C07D401/12 , C07D417/12 , A61K31/4439 , A61K31/18 , A61K31/195 , A61K31/198 , A61K31/355
CPC分类号： C07C233/87 , C04B35/632 , C07C235/60 , C07C255/57 , C07D213/643 , C07D213/65 , C07D213/82 , C07D257/04 , C07D401/12 , C07D417/12
摘要： This invention provides a compound of the formula (I): wherein A represents a phenyl group or the like: B represents an aryl or the like: E represents a 1,4-phenylene group; R1 and R2 independently represent a hydrogen atom or the like: R3 and R4 independently represent a hydrogen atom or the like: R5 represents —CO2H or the like: R6 represents an alkyl group having from 1 to 6 carbon atoms or the like: X represents a methylene group or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物：其中A表示苯基等：B表示芳基等：E表示1,4-亚苯基; R 1和R 2独立地表示氢原子等：R 3和R 4独立地表示氢原子等：R 5表示-CO 2 H等：R 6 >表示具有1〜6个碳原子的烷基等：X表示亚甲基等。这些化合物可用于治疗由前列腺素介导的疾病状况，例如哺乳动物中的疼痛等。本发明还提供了包含上述化合物的药物组合物。

9. 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。

10. 发明授权

US6063928A 5-lipoxygenase inhibitors 失效
标题翻译： 5-脂氧合酶抑制剂
公开(公告)号：US6063928A
公开(公告)日：2000-05-16
申请号：US207342
申请日：1998-12-08
申请人： Rodney W. Stevens , Takashi Mano , Kazunari Nakao , Yoshiyuki Okumura
发明人： Rodney W. Stevens , Takashi Mano , Kazunari Nakao , Yoshiyuki Okumura
IPC分类号： C07D233/60 , C07D233/61 , C07D309/08 , C07D521/00 , C07D207/323 , C07D207/36 , C07D235/10 , C07D235/14 , C07D401/10 , C07D403/10 , C07D405/10
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D309/08
摘要： Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, amino and the like; X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, C.sub.1-4 alkyl and the like; R.sup.1 and R.sup.2 are each C.sub.1-4 alkyl, or together they form a group of formula --D.sup.1 --Z--D.sup.2 -- which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D.sup.1 and D.sup.2 are C.sub.1-4 alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D.sup.1 and D.sup.2 may be substituted by C.sub.1-3 alkyl; and Y is CONR.sup.3 R.sup.4, CN, C(R.sup.3).dbd.N--OR.sup.4, COOR.sup.3, COR.sup.3 or CSNR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are each H or C.sub.1-4 alkyl. 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：具有抑制5-脂肪氧合酶并具有下式I的能力的新型化合物及其药学上可接受的盐，其中Ar1是选自咪唑基，吡咯基，吡唑基，1,2,3-三唑基，，2,4-三唑基，吲哚基，吲唑基和苯并咪唑基，其通过环氮原子与X1连接，并且其可任选被一个或两个选自卤素，羟基，氰基，氨基，C 1-4烷基的取代基取代，类似; X1是直接键或C1-4亚烷基; Ar 2是任选被卤素，羟基，氰基，氨基等取代的亚苯基; X2是-A-X或-X-A-，其中A是直接键或C 1-4亚烷基，X是氧基，硫代，亚磺酰基或磺酰基; Ar 3是任选被一个或两个选自卤素，羟基，氰基，氨基，C 1-4烷基等的取代基取代的亚苯基，亚吡啶基，亚噻吩基，呋喃基，恶唑基或噻唑基; R1和R2各自为C1-4烷基，或者它们一起形成式-D1-Z-D2-的基团，与其所连接的碳原子一起形成具有3至8个原子的环，其中D1和D2是 C 1-4亚烷基，Z是直接键或氧基，硫基，亚磺酰基，磺酰基或亚乙烯基，D1和D2可以被C 1-3烷基取代; 并且Y是CONR 3 R 4，CN，C（R 3）= N-OR 4，COOR 3，COR 3或CSNR 3 R 4，其中R 3和R 4各自为H或C 1-4烷基。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。

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