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1. 发明申请

WO0240484A2 NOVEL IMIDAZOLE DERIVATIVES, PRODUCTION METHOD THEREOF AND USE THEREOF 审中-公开
标题翻译：新型咪唑衍生物，其制备方法及其用途
公开(公告)号：WO0240484A2
公开(公告)日：2002-05-23
申请号：PCT/JP0110002
申请日：2001-11-16
申请人： TAKEDA CHEMICAL INDUSTRIES LTD , TASAKA AKIHIRO , HITAKA TAKENORI , MATSUNAGA NOBUYUKI , KUSAKA MASAMI , ADACHI MARI , AOKI ISAO , OJIDA AKIO
发明人： TASAKA AKIHIRO , HITAKA TAKENORI , MATSUNAGA NOBUYUKI , KUSAKA MASAMI , ADACHI MARI , AOKI ISAO , OJIDA AKIO
IPC分类号： C07D233/62 , A61K31/165 , A61K31/4174 , A61K31/4188 , A61K31/437 , A61K45/00 , A61P5/28 , A61P35/00 , A61P43/00 , C07D233/54 , C07D471/04 , C07D487/04
CPC分类号： C07D233/64 , C07D471/04 , C07D487/04
摘要： The present invention provides a compound having a steroid C17,20-lyase-inhibitory activity and useful for the therapy and prophylaxis of tumor such as prostatism, breast cancer and the like, and a method for efficiently separating an optically active compound of this compound from a mixture of optical isomers thereof, a compound of the formula:wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof, and a method for obtaining an optically active compound by optically resolving a mixture of optical isomers by the use of a resolving agent such as tartranilic acid and the like.
摘要翻译：本发明提供具有类固醇C17,20-裂解酶抑制活性并可用于治疗和预防诸如前列腺症，乳腺癌等肿瘤的化合物，以及将该化合物的光学活性化合物从其光学异构体的混合物，下式的化合物：其中每个符号如说明书中所定义，其盐或其前药，以及通过光学拆分光学异构体的混合物获得光学活性化合物的方法，使用分解剂如tart铵酸等。

2. 发明申请

WO2006064944A1 SUBSTITUTED PYRROLE DERIVATIVE 审中-公开
标题翻译：取代吡啶衍生物
公开(公告)号：WO2006064944A1
公开(公告)日：2006-06-22
申请号：PCT/JP2005/023215
申请日：2005-12-13
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , MATSUNAGA, Nobuyuki , ITO, Mitsuhiro , HITAKA, Takenori
发明人： MATSUNAGA, Nobuyuki , ITO, Mitsuhiro , HITAKA, Takenori
IPC分类号： C07D401/06 , C07D207/32 , A61K31/40 , A61P35/00
CPC分类号： C07D207/327 , C07D207/34 , C07D401/06 , C07D413/14
摘要： The present invention provides a novel pyrrole derivative having excellent androgen receptor antagonism, which is represented by the formula (I): wherein R 1 represents a hydrogen atom, a cyano group or a group represented by the formula COOR A (wherein R A represents an optional substituted C 1-6 alkyl group), R 2 and R 4 are the same or different, and each represents a hydrogen atom, a C 1-6 alkyl group, a C 3-6 cycloalkyl group, a trifluoromethyl group, an amino-C 1-6 alkyl group, a mono-or di-substituted amino-C 1-6 alkyl group, an optionally halogenated C 1-6 alkyl group substituted with an optionally substituted hydroxyl group, a C 2-6 alkenyl group substituted with an optionally substituted hydroxyl group, a C 1-6 alkyl group substituted with an optionally substituted and optionally oxidized thiol group, an optionally substituted with and optionally oxidized thiol group, a cyano group, an acyl group, an optionally substituted oxazolyl group or a 1,3-dioxolan-2-yl group, R 3 represents a group represented by the formula (a): (wherein X represents a halogen atom, Y represents a carbon atom or a nitrogen atom, Alk represents an optionally substituted C 1-4 alkylene group, and R B represents a hydrogen atom or an acyl group), and R 5 represents a phenyl group which has a cyano group at a 4-position or a 3-position thereof, and may be further substituted, or a salt thereof. The present invention also provides an androgen receptor antagonist containing the pyrrole derivative, or a salt thereof.
摘要翻译：本发明提供具有优异的雄激素受体拮抗作用的新颖的吡咯衍生物，其由式（I）表示：其中R 1表示氢原子，氰基或由式COOR表示的基团（其中R A表示任选的取代的C 1-6烷基），R 2和R 2， SUP> 4 <！ - SIPO - >相同或不同，并且各自表示氢原子，C 1-6烷基，C 3-6环烷基，三氟甲基，氨基-C 1-6烷基，单取代或二取代的氨基-C 1-6烷基，任选卤代的C

3. 发明申请

WO2002040484A3 NOVEL IMIDAZOLE DERIVATIVES, PRODUCTION METHOD THEREOF AND USE THEREOF 审中-公开
公开(公告)号：WO2002040484A3
公开(公告)日：2002-05-23
申请号：PCT/JP2001/010002
申请日：2001-11-16
申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. , TASAKA, Akihiro , HITAKA, Takenori , MATSUNAGA, Nobuyuki , KUSAKA, Masami , ADACHI, Mari , AOKI, Isao , OJIDA, Akio
发明人： TASAKA, Akihiro , HITAKA, Takenori , MATSUNAGA, Nobuyuki , KUSAKA, Masami , ADACHI, Mari , AOKI, Isao , OJIDA, Akio
IPC分类号： C07D487/04
摘要： The present invention provides a compound having a steroid C17,20-lyase-inhibitory activity and useful for the therapy and prophylaxis of tumor such as prostatism, breast cancer and the like, and a method for efficiently separating an optically active compound of this compound from a mixture of optical isomers thereof, a compound of the formula:wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof, and a method for obtaining an optically active compound by optically resolving a mixture of optical isomers by the use of a resolving agent such as tartranilic acid and the like.

4. 发明申请

WO2007145349A3 SUBSTITUTED PYRROLE DERIVATIVES 审中-公开
标题翻译：取代的吡咯衍生物
公开(公告)号：WO2007145349A3
公开(公告)日：2008-04-03
申请号：PCT/JP2007062194
申请日：2007-06-12
申请人： TAKEDA PHARMACEUTICAL , ITO MITSUHIRO , MATSUNAGA NOBUYUKI , YAMADA MASAMI , HITAKA TAKENORI , YAMAMOTO SATOSHI
发明人： ITO MITSUHIRO , MATSUNAGA NOBUYUKI , YAMADA MASAMI , HITAKA TAKENORI , YAMAMOTO SATOSHI
IPC分类号： C07D403/06 , C07D413/06 , C07D417/06 , C07D471/04
CPC分类号： C07D417/06 , C07D403/06 , C07D413/06 , C07D471/04
摘要： The present invention provides novel pyrrole derivatives represented by formula (I): wherein R 1 represents a hydrogen atom, cyano, optionally halogenated C 1-6 alkyl or an optionally substituted C 1-6 alkoxy-carbonyl; R 2 and R 4 may be the same or different and represent a hydrogen atom, C 1-6 alkyl, C 2-6 alkenyl substituted with an optionally substituted hydroxy, an optionally substituted or oxidized thiol, etc.; R 3 represents an optionally substituted thiazolyl, an optionally substituted pyrazolyl, an optionally substituted oxazolyl, etc.; and R 5 represents an optionally substituted phenyl having a cyano at the 4- or 3-position, and androgen receptor antagonists containing the same.
摘要翻译：本发明提供由式（I）表示的新颖的吡咯衍生物：其中R 1表示氢原子，氰基，任选卤代的C 1-6烷基或任选取代的C 1-6烷氧羰基; R 2和R 4可以相同或不同，表示氢原子，C 1-6烷基，C 2〜被任选取代的羟基取代的6个链烯基，任选取代的或氧化的硫醇等; R 3表示任选取代的噻唑基，任选取代的吡唑基，任选取代的恶唑基等; R 5表示任选取代的在4-或3-位有氰基的苯基，和含有它们的雄激素受体拮抗剂。

5. 发明申请

WO0177107B1 OXAZOLE DERIVATIVES AND THEIR USES AS TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：氧唑衍生物及其作为酪氨酸激酶抑制剂的用途
公开(公告)号：WO0177107B1
公开(公告)日：2001-12-20
申请号：PCT/JP0102937
申请日：2001-04-05
申请人： TAKEDA CHEMICAL INDUSTRIES LTD , TASAKA AKIHIRO , HITAKA TAKENORI , MATSUTANI ETSUYA
发明人： TASAKA AKIHIRO , HITAKA TAKENORI , MATSUTANI ETSUYA
IPC分类号： A61P35/00 , C07D263/32 , C07D413/12 , A61K31/422
CPC分类号： C07D413/12 , C07D263/32
摘要： A compound represented by formula (1) wherein m is 1 or 2, R is a halogen or an optionally halogenated C1-2 alkyl; one of R and R is a hydrogen atom and the other is a group represented by formula (2) or (3) wherein n is 3 or 4; R is a C1-4 alkyl group substituted by 1 or 2 hydroxy groups, or a salt thereof shows tyrosine kinase-inhibiting activity.
摘要翻译：由式（1）表示的化合物，其中m为1或2，R 1为卤素或任选卤代的C 1-2烷基; R 2和R 3中的一个是氢原子，另一个是由式（2）或（3）表示的基团，其中n是3或4; R 4是被1或2个羟基取代的C 1-4烷基，或其盐表示酪氨酸激酶抑制活性。

6. 发明申请

WO2007145349A2 SUBSTITUTED PYRROLE DERIVATIVES 审中-公开
标题翻译：取代的吡咯衍生物
公开(公告)号：WO2007145349A2
公开(公告)日：2007-12-21
申请号：PCT/JP2007/062194
申请日：2007-06-12
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , ITO, Mitsuhiro , MATSUNAGA, Nobuyuki , YAMADA, Masami , HITAKA, Takenori , YAMAMOTO, Satoshi
发明人： ITO, Mitsuhiro , MATSUNAGA, Nobuyuki , YAMADA, Masami , HITAKA, Takenori , YAMAMOTO, Satoshi
CPC分类号： C07D417/06 , C07D403/06 , C07D413/06 , C07D471/04
摘要： The present invention provides novel pyrrole derivatives represented by formula (I): wherein R 1 represents a hydrogen atom, cyano, optionally halogenated C?1-6#191 alkyl or an optionally substituted C?1-6#191 alkoxy-carbonyl; R 2 and R 4 may be the same or different and represent a hydrogen atom, C?1-6#191 alkyl, C?2-6#191 alkenyl substituted with an optionally substituted hydroxy, an optionally substituted or oxidized thiol, etc.; R 3 represents an optionally substituted thiazolyl, an optionally substituted pyrazolyl, an optionally substituted oxazolyl, etc.; and R 5 represents an optionally substituted phenyl having a cyano at the 4- or 3-position, and androgen receptor antagonists containing the same.
摘要翻译：本发明提供由式（I）表示的新颖的吡咯衍生物：其中R 1表示氢原子，氰基，任意卤代的C 1-6〜18-18个烷基或任意取代的C 1-6〜＃191烷氧基 - 羰基; R 2和R 4可以相同或不同，表示氢原子，C 1-6 1-6烷基，C 2-6 - 任选取代的羟基，任选取代的或氧化的硫醇等; R 3表示任选取代的噻唑基，任选取代的吡唑基，任选取代的恶唑基等; R 5表示任选取代的在4-或3-位有氰基的苯基，和含有它们的雄激素受体拮抗剂。

7. 发明申请

WO0177107A8 OXAZOLE DERIVATIVES AND THEIR USES AS TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：氧唑衍生物及其作为酪氨酸激酶抑制剂的用途
公开(公告)号：WO0177107A8
公开(公告)日：2003-02-13
申请号：PCT/JP0102937
申请日：2001-04-05
申请人： TAKEDA CHEMICAL INDUSTRIES LTD , TASAKA AKIHIRO , HITAKA TAKENORI , MATSUTANI ETSUYA
发明人： TASAKA AKIHIRO , HITAKA TAKENORI , MATSUTANI ETSUYA
IPC分类号： A61P35/00 , C07D263/32 , C07D413/12 , A61K31/422
CPC分类号： C07D413/12 , C07D263/32
摘要： A compound represented by formula (1) wherein m is 1 or 2, R is a halogen or an optionally halogenated C1-2 alkyl; one of R and R is a hydrogen atom and the other is a group represented by formula (2) or (3) wherein n is 3 or 4; R is a C1-4 alkyl group substituted by 1 or 2 hydroxy groups, or a salt thereof shows tyrosine kinase-inhibiting activity.
摘要翻译：由式（1）表示的化合物，其中m为1或2，R 1为卤素或任选卤代的C 1-2烷基; R 2和R 3中的一个是氢原子，另一个是由式（2）或（3）表示的基团，其中n是3或4; R 4是被1或2个羟基取代的C 1-4烷基，或其盐表示酪氨酸激酶抑制活性。

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