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1. 发明授权

US08530504B2 Pyrazolothiazole compound 失效
标题翻译：吡唑并噻唑化合物
公开(公告)号：US08530504B2
公开(公告)日：2013-09-10
申请号：US12900026
申请日：2010-10-07
申请人： Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda , Kodo Shikata , Akira Inomata
发明人： Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda , Kodo Shikata , Akira Inomata
IPC分类号： A61K31/429 , A61P25/24
CPC分类号： C07D513/04
摘要： A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkylthio group.
摘要翻译：由式（I）表示的化合物或其药理学上可接受的盐表现出优异的CRF受体拮抗作用，其中X为氮原子或CH; R1为-A11-A12; A11是单键或C1-6亚烷基; A12是氢原子，C1-6烷基或C3-6环烷基等; R2为-A21-A22; A21是单键或C1-6亚烷基; A22为氢原子，C1-6烷基，C3-6环烷基，非芳族杂环基或杂芳基等; R3是C1-6烷基，C3-6环烷基，C1-6烷氧基，C3-6环烷氧基C1-6烷基，二C1-6烷基氨基，卤素原子，氰基，甲酰基或羧基等; R4是氢原子或C1-6烷氧基; R5是卤素原子，C1-6烷基或C1-6烷氧基; R6是氢原子，C1-6烷基，C1-6烷氧基，C1-6烷硫基或C1-6烷基亚磺酰基等; 且R 7为C 1-6烷基，C 1-6烷氧基或C 1-6烷硫基。

2. 发明申请

US20110086898A1 PYRAZOLOOXAZOLE COMPOUND 审中-公开
标题翻译：吡唑并噻唑化合物
公开(公告)号：US20110086898A1
公开(公告)日：2011-04-14
申请号：US12900046
申请日：2010-10-07
申请人： Kogyoku SHIN , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda , Kodo Shikata , Akira Inomata
发明人： Kogyoku SHIN , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda , Kodo Shikata , Akira Inomata
IPC分类号： A61K31/4162 , C07D487/04 , A61P25/00 , A61P1/00
CPC分类号： C07D498/04
摘要： A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism. wherein R1 and R2 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, a C1-6 alkyl group substituted with a cyclic group selected from a C3-6 cycloalkyl group, a tetrahydropyranyl group, a dihydropyranyl group, a tetrahydrofuryl group, a dioxanyl group, a tetrahydrothienyl group, a dithianyl group and a hexahydrothiepinyl group, etc; R3, R4 and R5 are the same or different and are a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C1-6 alkoxy-C1-6 alkyl group, a C3-6 cycloalkoxy-C1-6 alkyl group or a halogen atom; R6 is a hydrogen atom or a C1-6 alkyl group; and R7 is a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkylthio group.
摘要翻译：由式（I）表示的化合物或其药理学上可接受的盐表现出优异的CRF受体拮抗作用。其中R1和R2相同或不同，为氢原子，C1-6烷基，选自C 3-6环烷基，四氢吡喃基，二氢吡喃基，四氢呋喃基，二氧杂环己烷基，四噻吩基，二噻烷基和六氢硫杂基，被选自C 3-6环烷基，四氢吡喃基，二氢吡喃基，四氢呋喃基，二烷基，四氢噻吩基中的环状基取代的C 1-6烷基二硫代基，六氢噻吩基等; R 3，R 4和R 5相同或不同，为氢原子，C 1-6烷基，C 3-6环烷基，C 1-6烷氧基，C 1-6烷氧基-C 1-6烷基， C 3-6环烷氧基-C 1-6烷基或卤素原子; R6是氢原子或C1-6烷基; 并且R 7是C 1-6烷基，C 1-6烷氧基或C 1-6烷硫基。

3. 发明申请

US20090259049A1 3-PHENYLPYRAZOLO[5,1-b]THIAZOLE COMPOUNDS 有权
标题翻译： 3-苯基吡唑并[5,1-b]噻唑化合物
公开(公告)号：US20090259049A1
公开(公告)日：2009-10-15
申请号：US12421182
申请日：2009-04-09
申请人： Hisashi Shibata , Kodo Shikata , Akira Inomata , Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda
发明人： Hisashi Shibata , Kodo Shikata , Akira Inomata , Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda
IPC分类号： C07D513/02
CPC分类号： C07D513/04
摘要： A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.
摘要翻译：由下式（I）表示的化合物或其盐表现出优异的CRF受体拮抗作用，作为药物具有充分的药理活性，安全性和药代动力学性质。其中R1表示式-A11-A12; R2表示四氢呋喃基甲基，四氢吡喃基甲基或四氢吡喃基; A11表示单键，亚甲基或1,2-亚乙基; A12表示C1-6烷基，C3-6环烷基或具有甲基的C3-6环烷基; R3表示甲氧基，氰基，环丁氧基甲基，甲氧基甲基或乙氧基甲基; R4表示甲氧基或氯。

4. 发明授权

US08431603B2 3-phenylpyrazolo[5,1-b]thiazole compounds 有权
标题翻译： 3-苯基吡唑并[5,1-b]噻唑化合物
公开(公告)号：US08431603B2
公开(公告)日：2013-04-30
申请号：US12421182
申请日：2009-04-09
申请人： Hisashi Shibata , Kodo Shikata , Akira Inomata , Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda
发明人： Hisashi Shibata , Kodo Shikata , Akira Inomata , Kogyoku Shin , Taro Terauchi , Yoshinori Takahashi , Minako Hashizume , Kunitoshi Takeda
IPC分类号： A61K31/4439 , C07D513/02
CPC分类号： C07D513/04
摘要： A compound represented by the following formula (I), or salt thereof exhibits excellent CRF receptor antagonism, and sufficient pharmacological activity, safety and pharmacokinetic properties as a drug. wherein R1 represents the formula -A11-A12; R2 represents tetrahydrofurylmethyl, tetrahydropyranylmethyl or tetrahydropyranyl; A11 represents a single bond, methylene or 1,2-ethylene; A12 represents C1-6 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl having methyl; R3 represents methoxy, cyano, cyclobutyloxymethyl, methoxymethyl or ethoxymethyl; and R4 represents methoxy or chlorine.
摘要翻译：由下式（I）表示的化合物或其盐表现出优异的CRF受体拮抗作用，作为药物具有充分的药理活性，安全性和药代动力学性质。其中R1表示式-A11-A12; R2表示四氢呋喃基甲基，四氢吡喃基甲基或四氢吡喃基; A11表示单键，亚甲基或1,2-亚乙基; A12表示C1-6烷基，C3-6环烷基或具有甲基的C3-6环烷基; R3表示甲氧基，氰基，环丁氧基甲基，甲氧基甲基或乙氧基甲基; R4表示甲氧基或氯。

5. 发明申请

US20070249663A1 PYRAZOLO[1,5-a]PYRIDINES AND MEDICINES CONTAINING THE SAME 失效
标题翻译：吡咯并[1,5-a]吡啶类和含有它的药物
公开(公告)号：US20070249663A1
公开(公告)日：2007-10-25
申请号：US11757595
申请日：2007-06-04
申请人： Shigeki Hibi , Koichi Kikuchi , Yorihisa Hoshino , Motohiro Soejima , Tatsuya Yoshiuchi , Kogyoku Shin , Mutsuko Ono , Yoshinori Takahashi , Hisashi Shibata , Mitsuhiro Ino , Tetsuya Hirakawa
发明人： Shigeki Hibi , Koichi Kikuchi , Yorihisa Hoshino , Motohiro Soejima , Tatsuya Yoshiuchi , Kogyoku Shin , Mutsuko Ono , Yoshinori Takahashi , Hisashi Shibata , Mitsuhiro Ino , Tetsuya Hirakawa
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04 , A61K31/437 , C07F5/025 , C07F7/2208
摘要： Compounds represented by the general formula: [wherein R1 represents methoxy, ethyl, methylthio, etc., R2, R3 and R4 each represent hydrogen, a halogen, etc., R5 and R6 each represent —X5—X6—X7 (wherein X5 represents a single bond or —CO—, X6 represents a single bond, —NR3a, etc. and X7 and R3a each represent hydrogen, C1-10 alkyl, etc.), and Ar represents phenyl, pyridyl, etc.], salts thereof and hydrates of the foregoing.
摘要翻译：由以下通式表示的化合物：其中R 1表示甲氧基，乙基，甲硫基等，R 2，R 3和R 3， SUP> 4 各自表示氢，卤素等，R 5和R 6各自表示-X 5〜其中X 5表示单键或-CO-，X 6表示单键键，-NR 3a等，且X 7和R 3a各自表示氢，C 1-10烷基，烷基等），Ar表示苯基，吡啶基等]，其盐和上述的水合物。

6. 发明授权

US06927221B2 Tricyclic fused heterocyclic compound, process for preparing it and medicament comprising it 失效
标题翻译：三环稠合杂环化合物，其制备方法和包含它的药物
公开(公告)号：US06927221B2
公开(公告)日：2005-08-09
申请号：US10903387
申请日：2004-08-02
申请人： Shigeki Hibi , Yorihisa Hoshino , Tatsuya Yoshiuchi , Kogyoku Shin , Kouichi Kikuchi , Motohiro Soejima , Mutsuko Tabata , Yoshinori Takahashi , Hisashi Shibata , Tetsuya Hirakawa
发明人： Shigeki Hibi , Yorihisa Hoshino , Tatsuya Yoshiuchi , Kogyoku Shin , Kouichi Kikuchi , Motohiro Soejima , Mutsuko Tabata , Yoshinori Takahashi , Hisashi Shibata , Tetsuya Hirakawa
IPC分类号： A61P1/04 , A61P1/08 , A61P1/10 , A61P1/12 , A61P1/14 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , C07D471/14 , C07D487/14 , C07D491/14 , C07D471/04 , A61K31/437 , A61P25/24
CPC分类号： C07D471/14 , C07D487/14 , C07D491/14
摘要： The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula, a pharmacologically acceptable salt thereof or hydrates thereof, wherein R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; the partial structure - - - represents a single or double bond; M′ represents a hydrogen atom, a halogen atom or a C1-6 alkyl group; R7′ represents a hydrogen atom or a C1-6 alkyl group; and W′ represents a phenyl group, pyridyl group, thienyl group, or furyl group, each being optionally substituted; and a pharmacologically acceptable salt thereof or hydrates thereof.
摘要翻译：本发明提供具有优异的促肾上腺皮质激素释放因子受体拮抗活性的新型化合物。也就是说，它提供由下式表示的化合物，其药理学上可接受的盐或其水合物，其中R 2是氢原子等; R 3是氢原子等; 部分结构 - - - 表示单键或双键; M'表示氢原子，卤素原子或C 1-6烷基; R 7表示氢原子或C 1-6烷基; W'表示苯基，吡啶基，噻吩基或呋喃基，各自任选被取代; 及其药理学上可接受的盐或其水合物。

7. 发明申请

US20050004147A1 Tricyclic fused heterocyclic compound, process for preparing it and medicament comprising it 失效
标题翻译：三环稠合杂环化合物，其制备方法和包含它的药物
公开(公告)号：US20050004147A1
公开(公告)日：2005-01-06
申请号：US10903059
申请日：2004-08-02
申请人： Shigeki Hibi , Yorihisa Hoshino , Tatsuya Yoshiuchi , Kogyoku Shin , Kouichi Kikuchi , Motohiro Soejima , Mutsuko Tabata , Yoshinori Takahashi , Hisashi Shibata , Takayuki Hida , Tetsuya Hirakawa , Mitsuhiro Ino
发明人： Shigeki Hibi , Yorihisa Hoshino , Tatsuya Yoshiuchi , Kogyoku Shin , Kouichi Kikuchi , Motohiro Soejima , Mutsuko Tabata , Yoshinori Takahashi , Hisashi Shibata , Takayuki Hida , Tetsuya Hirakawa , Mitsuhiro Ino
IPC分类号： A61P1/04 , A61P1/08 , A61P1/10 , A61P1/12 , A61P1/14 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , C07D471/14 , C07D487/14 , C07D491/14 , A61K31/519
CPC分类号： C07D471/14 , C07D487/14 , C07D491/14
摘要： The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula, a pharmacologically acceptable salt thereof or hydrates thereof. Wherein A, B and D are the same as or different from each other and each represents a group represented by the formula —(CR1R2)m— (wherein R1 and R2 are the same as or different from each other and each represents a C1-6 alkyl group etc.), —NR3— (wherein R3 represetns hydrogen etc.) etc.; E and G are the same as or different from each other and each represents a group represented by the formula —(CR6R7)p— (wherein R6 and R7 are the same as or different from each other and each represents hydrogen etc.; and p represents an integer of 0, 1 or 2); J represents a carbon atom or nitrogen atom, each substituted with C1-6 alkyl group optionally substituted with a halogen atom, etc.; K and L are the same as or different from each other and each represents carbon atom or nitrogen atom; M means hydrogen, a halogen atom, an optionally substituted C1-6 alkyl group etc.; and the partial structure means a single or double bond.
摘要翻译：本发明提供具有优异的促肾上腺皮质激素释放因子受体拮抗活性的新型化合物。也就是说，它提供由下式表示的化合物，其药理学上可接受的盐或其水合物。其中A，B和D彼此相同或不同，并且各自表示由式 - （CR 1 R 2）m - 表示的基团（其中R 1和R 2为相同或不同，各自表示C1-6烷基等），-NR 3 - （其中R 3表示氢等）等; E和G彼此相同或不同，并且各自表示由下式表示的基团 - （CR 6 R 7）p - （其中R 6和R 7与彼此不同，各自表示氢等; p表示0,1或2的整数）; J表示碳原子或氮原子，各自被任选被卤素原子取代的C 1-6烷基取代; K和L彼此相同或不同，各自表示碳原子或氮原子; M表示氢，卤原子，任意取代的C 1-6烷基等; 并且部分结构是指单键或双键。

8. 发明授权

US07772249B2 Imidazo[1,2-b]pyridazine compound 失效
标题翻译：咪唑并[1,2-b]哒嗪化合物
公开(公告)号：US07772249B2
公开(公告)日：2010-08-10
申请号：US12397132
申请日：2009-03-03
申请人： Shigeki Hibi , Yoshinori Takahashi , Yorihisa Hoshino , Koichi Kikuchi , Motohiro Soejima , Tatsuya Yoshiuchi , Kogyoku Shin , Mutsuko Ono , Hisashi Shibata , Mitsuhiro Ino , Tetsuya Hirakawa
发明人： Shigeki Hibi , Yoshinori Takahashi , Yorihisa Hoshino , Koichi Kikuchi , Motohiro Soejima , Tatsuya Yoshiuchi , Kogyoku Shin , Mutsuko Ono , Hisashi Shibata , Mitsuhiro Ino , Tetsuya Hirakawa
IPC分类号： A61K31/44
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula or a salt thereof. Wherein R1 denotes a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group and the like; R2 denotes a halogen atom, a cyano group, a nitro group, a C1-10 alkyl group, a C2-10 alkenyl group, C2-10 alkynyl group and the like; R3 denotes a C6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may have a substituent; and X, Y and X are independent of each other and each denotes N or CR4 (wherein R4 denotes a hydrogen atom, a halogen atom, a cyano group, a nitro group, an optionally halogenated C1-6 alkyl group and the like) and, in this case, at least two of X, Y and Z denote CR4.
摘要翻译：本发明提供具有优异的促肾上腺皮质激素释放因子受体拮抗活性的新型化合物。也就是说，它提供由下式表示的化合物或其盐。其中R1表示氢原子，C1-6烷基，C1-6烷氧基等; R2表示卤素原子，氰基，硝基，C1-10烷基，C2-10烯基，C2-10炔基等; R3表示可以具有取代基的C 6-14芳族烃环状基团或5〜14元芳香族杂环基团。 X，Y和X彼此独立地表示N或CR4（其中R4表示氢原子，卤素原子，氰基，硝基，任意卤代的C 1-6烷基等）和在这种情况下，X，Y和Z中的至少两个表示CR 4。

9. 发明授权

US07625925B2 Pyrazolo[1,5-a]pyridines and medicines containing the same 失效
标题翻译：吡唑并[1,5-a]吡啶和含有它们的药物
公开(公告)号：US07625925B2
公开(公告)日：2009-12-01
申请号：US11757595
申请日：2007-06-04
申请人： Shigeki Hibi , Koichi Kikuchi , Yorihisa Hoshino , Motohiro Soejima , Tatsuya Yoshiuchi , Kogyoku Shin , Mutsuko Ono , Yoshinori Takahashi , Hisashi Shibata , Mitsuhiro Ino , Tetsuya Hirakawa
发明人： Shigeki Hibi , Koichi Kikuchi , Yorihisa Hoshino , Motohiro Soejima , Tatsuya Yoshiuchi , Kogyoku Shin , Mutsuko Ono , Yoshinori Takahashi , Hisashi Shibata , Mitsuhiro Ino , Tetsuya Hirakawa
IPC分类号： A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , C07F5/025 , C07F7/2208
摘要： Compounds represented by the general formula: [wherein R1 represents methoxy, ethyl, methylthio, etc., R2, R3 and R4 each represent hydrogen, a halogen, etc., R5 and R6 each represent —X5—X6—X7 (wherein X5 represents a single bond or —CO—, X6 represents a single bond, —NR3a, etc. and X7 and R3a each represent hydrogen, C1-10 alkyl, etc.), and Ar represents phenyl, pyridyl, etc.], salts thereof and hydrates of the foregoing.
摘要翻译：由以下通式表示的化合物：[其中R1表示甲氧基，乙基，甲硫基等，R2，R3和R4各自表示氢，卤素等，R5和R6各自表示-X5-X6-X7（其中X5表示单键或-CO-，X6表示单键，-NR3a等，X7和R3a各自表示氢，C1-10烷基等），Ar表示苯基，吡啶基等]，其盐和上述的水合物。

10. 发明申请

US20060217348A1 Pyrazolo[1,5-a] pyridines and medicines containing the same 失效
标题翻译：吡唑并[1,5-a]吡啶和含有它们的药物
公开(公告)号：US20060217348A1
公开(公告)日：2006-09-28
申请号：US11446416
申请日：2006-06-05
申请人： Shigeki Hibi , Koichi Kikuchi , Yorihisa Hoshino , Motohiro Soejima , Tatsuya Yoshiuchi , Kogyoku Shin , Mutsuko Ono , Yoshinori Takahashi , Hisashi Shibata , Mitsuhiro Ino , Tetsuya Hirakawa
发明人： Shigeki Hibi , Koichi Kikuchi , Yorihisa Hoshino , Motohiro Soejima , Tatsuya Yoshiuchi , Kogyoku Shin , Mutsuko Ono , Yoshinori Takahashi , Hisashi Shibata , Mitsuhiro Ino , Tetsuya Hirakawa
IPC分类号： A61K31/69 , A61K31/555 , A61K31/4745 , C07F5/02 , C07F7/22 , C07D471/02
CPC分类号： C07D471/04 , A61K31/437 , C07F5/025 , C07F7/2208
摘要： Compounds represented by the general formula: [wherein R1 represents methoxy, ethyl, methylthio, etc., R2, R3 and R4 each represent hydrogen, a halogen, etc., R5 and R6 each represent —X5—X6—X7 (wherein X5 represents a single bond or —CO—, X6 represents a single bond, —NR3a, etc. and X7 and R3a each represent hydrogen, C1-10 alkyl, etc.), and Ar represents phenyl, pyridyl, etc.], salts thereof and hydrates of the foregoing.
摘要翻译：由以下通式表示的化合物：其中R 1表示甲氧基，乙基，甲硫基等，R 2，R 3和R 3， SUP> 4 各自表示氢，卤素等，R 5和R 6各自表示-X 5〜其中X 5表示单键或-CO-，X 6表示单键键，-NR 3a等，X 7和R 9各自表示氢，C 1-10烷基，烷基等），Ar表示苯基，吡啶基等]，其盐和上述的水合物。

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