公开(公告)号：US06444677B2

公开(公告)日：2002-09-03

申请号：US09731995

申请日：2000-12-07

申请人： Takafumi Ikeda ,  Mitsuhiro Kawamura ,  Noriaki Murase ,  Seiji Nukui ,  Yuji Shishido ,  Makato Kawai ,  Yoshiyuki Okumura

发明人： Takafumi Ikeda ,  Mitsuhiro Kawamura ,  Noriaki Murase ,  Seiji Nukui ,  Yuji Shishido ,  Makato Kawai ,  Yoshiyuki Okumura

IPC分类号： C07D40100

CPC分类号： C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein A is independently halo; Y1 is —(CH2)m—, C(O) or S(O); Y2 is N or CH; R1 and R2 are independently C1-4 alkyl; R3 is selected from the following: (a) optionally substituted —(CH2)p—C3-7 cycloalkyl; (b) optionally substituted —C5-7 alkyl; and (c) substituted —C1-4 alkyl; and (d) optionally substituted C7-9 bicycloalkyl; R4 is optionally substituted thiazolyl, imidazolyl or oxazolyl; X is S, —NH, —N—C1-4 alkyl or O; R5 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl or halo; m is 0, 1 or 2; n is 0, 1, 2, 3, 4 or S; and p is 0, 1, 2, 3, 4, 5 or 6. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound.

摘要翻译： 本发明提供式（I）的化合物或其药学上可接受的盐，其中A独立地为卤素; Y1是 - （CH2）m-，C（O）或S（O）; Y2是N或CH; R1和R2独立地是C1-4烷基; R3选自如下：（a）任选取代的 - （CH 2）p -C 3-7环烷基;（b）任选取代的-C 5-7烷基; 和（c）取代的C 1-4烷基; 和（d）任选取代的C 7-9双环烷基; R 4是任选取代的噻唑基，咪唑基或恶唑基; X是S，-NH，-N-C 1-4烷基或O; R 5是氢或C 1-4烷基; R6是C1-4烷基或卤素; m是0,1或2; n为0，1，2，3，4或S; 并且p为0,1,2,3,4,5或6.这些化合物可用于治疗由缓激肽引起的疾病如炎症，心血管疾病，疼痛等。本发明还提供一种药物组合物，其包含 以上化合物。

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。

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。

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。

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。

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。

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。

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。

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。

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。