公开(公告)号：US20110207935A1

公开(公告)日：2011-08-25

申请号：US13124345

申请日：2009-10-14

申请人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

发明人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

IPC分类号： C07D215/52 ,  C07D277/56 ,  C07D263/34 ,  C07D275/03 ,  C07D285/08 ,  C07D271/06 ,  C07C255/57 ,  C07D231/14 ,  C07D213/79

CPC分类号： C07C255/57 ,  A61K31/192 ,  A61K31/415 ,  A61K31/426 ,  A61K31/44 ,  A61K31/47 ,  C07C255/54 ,  C07D213/79 ,  C07D215/50 ,  C07D231/14 ,  C07D277/20 ,  C07D277/56

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), X1 and X2 represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.

摘要翻译： 本发明提供了可用作预防或治疗与异常血浆尿酸水平等相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的稠环衍生物，可用作预防或治疗与血浆尿酸水平异常有关的疾病，其前药，其盐或类似物 。 在式（I）中，X 1和X 2表示CH或N; 环U表示芳基或杂芳基; m表示0〜2的整数; n表示0〜3的整数; R1表示羟基，氨基或C1-6烷基; R 2表示C 1-6烷基，C 1-6烷氧基C 1-6烷基等。

公开(公告)号：US08263622B2

公开(公告)日：2012-09-11

申请号：US13124345

申请日：2009-10-14

申请人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

发明人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

IPC分类号： A61K31/426 ,  A61K31/433 ,  A61K31/4709 ,  A61K31/4725 ,  C07D215/16 ,  C07D239/72 ,  C07D277/24

CPC分类号： C07C255/57 ,  A61K31/192 ,  A61K31/415 ,  A61K31/426 ,  A61K31/44 ,  A61K31/47 ,  C07C255/54 ,  C07D213/79 ,  C07D215/50 ,  C07D231/14 ,  C07D277/20 ,  C07D277/56

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), X1 and X2 represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.

摘要翻译： 本发明提供了可用作预防或治疗与异常血浆尿酸水平等相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的稠环衍生物，可用作预防或治疗与血浆尿酸水平异常有关的疾病，其前药，其盐或类似物 。 在式（I）中，X 1和X 2表示CH或N; 环U表示芳基或杂芳基; m表示0〜2的整数; n表示0〜3的整数; R1表示羟基，氨基或C1-6烷基; R 2表示C 1-6烷基，C 1-6烷氧基C 1-6烷基等。

公开(公告)号：US08748452B2

公开(公告)日：2014-06-10

申请号：US13259621

申请日：2010-03-30

申请人： Kazuo Shimizu ,  Masato Iizuka ,  Yasushi Takigawa

发明人： Kazuo Shimizu ,  Masato Iizuka ,  Yasushi Takigawa

IPC分类号： A61K31/437 ,  A61P13/12 ,  A61P19/02 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R1 represents halogen, a hydroxy group or the like; R2 represents halogen, a hydroxy group, alkyl, alkoxy, alkyl substituted by fluorine, alkoxy substituted by fluorine or the like; m represents a number from 0 to 2; n represents a number from 0 to 3; and R3 represents hydrogen, fluorine or the like.

摘要翻译： 本发明提供可用作预防或治疗与血清尿酸水平异常等有关的疾病的药剂的化合物。 也就是说，本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的中氮茚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药，其盐或 类似。 在该式中，环U表示芳基或杂芳基; R1表示卤素，羟基等; R 2表示卤素，羟基，烷基，烷氧基，被氟取代的烷基，被氟取代的烷氧基等; m表示0〜2的数; n表示0〜3的数; R 3表示氢，氟等。

公开(公告)号：US08466152B2

公开(公告)日：2013-06-18

申请号：US13116389

申请日：2011-05-26

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/404 ,  A61K31/437 ,  A61K31/5025 ,  A61K31/519 ,  C07D209/10 ,  C07D209/30 ,  C07D209/42 ,  C07D471/04 ,  C07D487/14

CPC分类号： C07D209/30 ,  A61K31/165 ,  A61K31/404 ,  A61K31/407 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/42 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/056 ,  A61K2300/00

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, nitro, alkyl, alkoxy and the like; X1, X2 and X3 independently represent CR2 or N; R1 and R2 independently represent halogen, cyano, haloalkyl, A-D-E-G, —N(-D-E-G)2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO2 and the like.

摘要翻译： 本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药或盐 其中。 在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X1，X2和X3独立地表示CR2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G，-N（-D-E-G）2等，式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

公开(公告)号：US08003647B2

公开(公告)日：2011-08-23

申请号：US12595476

申请日：2008-04-10

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/404 ,  A61K31/437 ,  A61K31/5025 ,  A61K31/519 ,  C07D209/10 ,  C07D209/30 ,  C07D209/42 ,  C07D471/04 ,  C07D487/14

CPC分类号： C07D209/30 ,  A61K31/165 ,  A61K31/404 ,  A61K31/407 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/42 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/056 ,  A61K2300/00

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetrazolyl and the like; Y represents H, OH, NH2, halogen, nitro, alkyl, alkoxy and the like; X1, X2 and X3 independently represent CR2 or N; R1 and R2 independently represent halogen, cyano, haloalkyl, A-D-E-G, —N(-D-E-G)2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO2 and the like.

摘要翻译： 本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药或盐 其中。 在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X1，X2和X3独立地表示CR2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G，-N（-D-E-G）2等，式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

公开(公告)号：US09023882B2

公开(公告)日：2015-05-05

申请号：US13494380

申请日：2012-06-12

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/4025 ,  C07D231/10 ,  C07D207/30 ,  A61K31/4155 ,  C07D403/04 ,  A61K31/402 ,  A61K31/165 ,  A61K31/404 ,  A61K31/415 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D231/14 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/40 ,  C07D401/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04

CPC分类号： A61K31/402 ,  A61K31/165 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D231/14 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/40 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  A61K2300/00

摘要： 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.

摘要翻译： 具有黄嘌呤氧化酶抑制活性的通式（I）表示的5元杂环衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病或其前药或其盐的药剂。 在式（I）中，T表示硝基，氰基等; 环J表示芳基或杂芳基; Q表示羧基，5-四唑基等; Y表示H，OH，NH 2，卤素，卤代烷基等; X1和X2独立地表示CR2或N; R2代表H，烷基等; R 1表示卤素，氰基，卤代烷基，A-D-E-G-L-M，-N（-D-L-M）2等，A表示单键O，S等; D，G和M独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E和L独立地表示单键O，S，COO，SO 2等。

公开(公告)号：US20110201815A1

公开(公告)日：2011-08-18

申请号：US13124336

申请日：2009-10-14

申请人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

发明人： Kazuo Shimizu ,  Masato Iizuka ,  Hideki Fujikura ,  Yasushi Takigawa ,  Masahiro Hiratochi

IPC分类号： C07D401/10 ,  C07D417/10

CPC分类号： C07D401/04 ,  A61K31/427 ,  A61K31/443 ,  A61K31/4439 ,  C07D405/04 ,  C07D417/04

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), T represents trifluoromethyl, nitro or cyano; ring Q represents heteroaryl; X1 and X2 independently represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.

摘要翻译： 本发明提供了可用作预防或治疗与异常血浆尿酸水平等相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由下式（I）表示的稠合杂环衍生物，可用作预防或治疗与血浆尿酸水平异常有关的疾病，其前体药物，其盐或类似物 。 在式（I）中，T代表三氟甲基，硝基或氰基; 环Q表示杂芳基; X1和X2独立地表示CH或N; 环U表示芳基或杂芳基; m表示0〜2的整数; n表示0〜3的整数; R1表示羟基，氨基或C1-6烷基; R 2表示C 1-6烷基，C 1-6烷氧基C 1-6烷基等。

公开(公告)号：US20100056521A1

公开(公告)日：2010-03-04

申请号：US12595476

申请日：2008-04-10

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/404 ,  C07D209/18 ,  C07D409/12 ,  C07D413/10 ,  C07D401/04 ,  C07D471/04 ,  A61K31/4439 ,  A61K31/5377 ,  A61P43/00

CPC分类号： C07D209/30 ,  A61K31/165 ,  A61K31/404 ,  A61K31/407 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/42 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/056 ,  A61K2300/00

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, nitro, alkyl, alkoxy and the like; X1, X2 and X3 independently represent CR2 or N; R1 and R2 independently represent halogen, cyano, haloalkyl, A-D-E-G, —N(-D-E-G)2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO2 and the like.

摘要翻译： 本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病，其前药或盐 其中。 在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X1，X2和X3独立地表示CR2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G，-N（-D-E-G）2等，式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

公开(公告)号：US20120289506A1

公开(公告)日：2012-11-15

申请号：US13494380

申请日：2012-06-12

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/40 ,  C07D231/14 ,  A61K31/415 ,  C07D405/10 ,  C07D231/22 ,  A61P13/12 ,  A61K31/4439 ,  A61K31/454 ,  C07D413/06 ,  A61K31/5377 ,  A61P19/06 ,  C07D207/34 ,  C07D401/04

CPC分类号： A61K31/402 ,  A61K31/165 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D231/14 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/40 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  A61K2300/00

摘要： 5-membered heterocyclic derivatives represented by general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, —N(-D-L-M)2 and the like, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.

摘要翻译： 具有黄嘌呤氧化酶抑制活性的通式（I）表示的5元杂环衍生物，可用作预防或治疗与血清尿酸水平异常有关的疾病或其前药或其盐的药剂。 在式（I）中，T表示硝基，氰基等; 环J表示芳基或杂芳基; Q表示羧基，5-四唑基等; Y表示H，OH，NH 2，卤素，卤代烷基等; X1和X2独立地表示CR2或N; R2代表H，烷基等; R 1表示卤素，氰基，卤代烷基，A-D-E-G-L-M，-N（-D-L-M）2等，A表示单键O，S等; D，G和M独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E和L独立地表示单键O，S，COO，SO 2等。

公开(公告)号：US08227500B2

公开(公告)日：2012-07-24

申请号：US12595437

申请日：2008-04-10

申请人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

发明人： Kazuo Shimizu ,  Yasushi Takigawa ,  Hideki Fujikura ,  Masato Iizuka ,  Masahiro Hiratochi ,  Norihiko Kikuchi

IPC分类号： A61K31/405 ,  C07D207/00

CPC分类号： A61K31/402 ,  A61K31/165 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D231/14 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/40 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  A61K2300/00

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to 5-membered heterocyclic derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro, cyano and the like; ring J represents aryl or heteroaryl; Q represents carboxy, 5-tetazolyl and the like; Y represents H, OH, NH2, halogen, haloalkyl and the like; X1 and X2 independently represent CR2 or N; R2 represents H, alkyl and the like; R1 represents halogen, cyano, haloalkyl, A-D-E-G-L-M, -N(-D-L-M)2 and the like, in the formula, A represents a single bond, O, S and the like; D, G and M independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E and L independently represent a single bond, O, S, COO, SO2 and the like.

摘要翻译： 本发明提供可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的5元杂环衍生物，可用作预防或治疗与血清尿酸水平异常相关疾病，其前药或盐类的药物 其中。 在式（I）中，T表示硝基，氰基等; 环J表示芳基或杂芳基; Q表示羧基，5-四唑基等; Y表示H，OH，NH 2，卤素，卤代烷基等; X1和X2独立地表示CR2或N; R2代表H，烷基等; R 1表示卤素，氰基，卤代烷基，A-D-E-G-L-M，-N（-D-L-M）2等，式中，A表示单键O，S等; D，G和M独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E和L独立地表示单键O，S，COO，SO 2等。