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1. 发明专利

DE60018462T2 未知
公开(公告)号：DE60018462T2
公开(公告)日：2006-02-16
申请号：DE60018462
申请日：2000-12-13
申请人： EISAI CO LTD
发明人： HIBI SHIGEKI , HOSHINO YORIHISA , YOSHIUCHI TATSUYA , SHIN KOGYOKU , KIKUCHI KOUICHI , SOEJIMA MOTOHIRO , TABATA MUTSUKO , TAKAHASHI YOSHINORI , SHIBATA HISASHI , HIDA TAKAYUKI , HIRAKAWA TETSUYA , INO MITSUHIRO
IPC分类号： A61K31/437 , A61K31/519 , A61P1/04 , A61P1/08 , A61P1/10 , A61P1/12 , A61P1/14 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , C07D471/14 , C07D473/02 , C07D487/14 , C07D491/14 , C07D495/14
摘要： Fused heterocyclic compounds (I) are new. Fused heterocyclic compounds of formula (I) and their salts and hydrates are new. [Image] A, B, D, E, G : N, O, S, (CR 1R 2) m, CO, CS, NR 3, SO or SO 2; R 1, R 2H, Alk, 2-6C alkenyl, 2-6C alkynyl, CycOAlk, AlkOAlk, AlkCyc or 1-6C alkyl-aryl, or CR 1R 23-8 membered ring or is replaced by CR 2=CR 2 or N=CR 2; m : 0-4; Alk : 1-6C alkyl; Cyc : 3-8C cycloalkyl; R 3H, COR 4, S(O) nR 5, Alk 2, optionally substituted aryl or optionally benzene fused Cyc (optionally substituted by 1-4C alkyl); Alk 21-10C alkyl, 2-10C alkenyl or 2-10C alkynyl (all optionally substituted by Q); R 4, R 5Alk or Ar; n : 0-2; J : N, CJ 1, NJ 1 or CJ 1J 1; J 1H, amino, CN, Alk, 1-6C haloalkyl, SO 2NHAlk, aryl or optionally substituted, optionally unsaturated heterocyclyl; K, L : C or N; M : H, halo, CN, Alk 3, NR 11R 12, OR 13, S(O) qR 14, or optionally substituted 2-10C alkenyl, 2-10C alkynyl, aryl or heteroaryl; Alk 3Alk, OAlk or SAlk (all optionally substituted by 1 or more Q); Q : halo, OH, NO 2, CN, COOH, COOAlk, S(O) rR 15, NR 18R 19, Alk, OAlk, Cyc (optionally substituted by 1-4C alkyl), 1-4C alkoxy-1-6C alkyl, 3-8 membered saturated heterocyclyl (optionally substituted by 1-4C alkyl), or optionally substituted aryl or heteroaryl; R 11, R 12H, Alk (optionally substituted by Q), 1-4C alkylacyl or Ar; Ar : optionally substituted aryl-1-4C alkyl, heteroaryl-1-4C alkyl, aryl or heteroaryl; R 13H, Q, 1-4C alkylacyl or Ar; R 14Alk or Ar; q : 0-2; R 15, R 16H Alk (optionally substituted by optionally substituted aryl), 1-4C alkylacyl or Ar; R 18, R 19H, Alk or 1-4C alkylacyl; provided that: (i) KEGJL form a 5 or 6 membered optionally unsaturated ring; and (ii) when K and L = N or K = N, L = C, A, B = CH2 then J is not amino, CN, optionally substituted aminosulfonyl or C(1H-tetrazol-5-yl). ACTIVITY : Antidepressant; tranquilizer; antiinflammatory; hypotensive; gastrointestinal; antiulcer; antiemetic; nootropic; neuroprotective; anabolic; anorectic; antidiabetic; CNS; anticonvulsant; antialcoholic; analgesic; cerebroprotective; auditory; endocrine; vasotropic; cytostatic; anti-HIV; hemostatic; osteopathic; antithyroid; antiasthmatic. MECHANISM OF ACTION : Corticoliberin antagonist. In assays using AtT-20 cells, 8-(1-ethylpropyl)-3-mesityl-2,5-dimethyl-7,8-dihydro-6H-pyrazolo(1,5-a)pyrrolo(3,2-e)pyrimidine (Ia) HCl exhibited an IC 50 value for CRF 1 receptor binding of 100 nM.

2. 发明专利

AT300546T 未知
公开(公告)号：AT300546T
公开(公告)日：2005-08-15
申请号：AT03029058
申请日：2000-12-13
申请人： EISAI CO LTD
发明人： HIBI SHIGEKI , HOSHINO YORIHISA , YOSHIUCHI TATSUYA , SHIN KOBYOKU , KIKUCHI KOICHI , SOEJIMA MOTOHIRO , ONO MUTSUKO , TAKAHASHI YOSHINORI , SHIBATA HISASHI , HIDA TAKAYUKI , HIRAKAWA TETSUYA , INO MITSUHIRO
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 , C07D473/02 , C07D495/14 , A61K31/437 , A61K31/519
摘要： Fused heterocyclic compounds (I) are new. Fused heterocyclic compounds of formula (I) and their salts and hydrates are new. [Image] A, B, D, E, G : N, O, S, (CR 1R 2) m, CO, CS, NR 3, SO or SO 2; R 1, R 2H, Alk, 2-6C alkenyl, 2-6C alkynyl, CycOAlk, AlkOAlk, AlkCyc or 1-6C alkyl-aryl, or CR 1R 23-8 membered ring or is replaced by CR 2=CR 2 or N=CR 2; m : 0-4; Alk : 1-6C alkyl; Cyc : 3-8C cycloalkyl; R 3H, COR 4, S(O) nR 5, Alk 2, optionally substituted aryl or optionally benzene fused Cyc (optionally substituted by 1-4C alkyl); Alk 21-10C alkyl, 2-10C alkenyl or 2-10C alkynyl (all optionally substituted by Q); R 4, R 5Alk or Ar; n : 0-2; J : N, CJ 1, NJ 1 or CJ 1J 1; J 1H, amino, CN, Alk, 1-6C haloalkyl, SO 2NHAlk, aryl or optionally substituted, optionally unsaturated heterocyclyl; K, L : C or N; M : H, halo, CN, Alk 3, NR 11R 12, OR 13, S(O) qR 14, or optionally substituted 2-10C alkenyl, 2-10C alkynyl, aryl or heteroaryl; Alk 3Alk, OAlk or SAlk (all optionally substituted by 1 or more Q); Q : halo, OH, NO 2, CN, COOH, COOAlk, S(O) rR 15, NR 18R 19, Alk, OAlk, Cyc (optionally substituted by 1-4C alkyl), 1-4C alkoxy-1-6C alkyl, 3-8 membered saturated heterocyclyl (optionally substituted by 1-4C alkyl), or optionally substituted aryl or heteroaryl; R 11, R 12H, Alk (optionally substituted by Q), 1-4C alkylacyl or Ar; Ar : optionally substituted aryl-1-4C alkyl, heteroaryl-1-4C alkyl, aryl or heteroaryl; R 13H, Q, 1-4C alkylacyl or Ar; R 14Alk or Ar; q : 0-2; R 15, R 16H Alk (optionally substituted by optionally substituted aryl), 1-4C alkylacyl or Ar; R 18, R 19H, Alk or 1-4C alkylacyl; provided that: (i) KEGJL form a 5 or 6 membered optionally unsaturated ring; and (ii) when K and L = N or K = N, L = C, A, B = CH2 then J is not amino, CN, optionally substituted aminosulfonyl or C(1H-tetrazol-5-yl). ACTIVITY : Antidepressant; tranquilizer; antiinflammatory; hypotensive; gastrointestinal; antiulcer; antiemetic; nootropic; neuroprotective; anabolic; anorectic; antidiabetic; CNS; anticonvulsant; antialcoholic; analgesic; cerebroprotective; auditory; endocrine; vasotropic; cytostatic; anti-HIV; hemostatic; osteopathic; antithyroid; antiasthmatic. MECHANISM OF ACTION : Corticoliberin antagonist. In assays using AtT-20 cells, 8-(1-ethylpropyl)-3-mesityl-2,5-dimethyl-7,8-dihydro-6H-pyrazolo(1,5-a)pyrrolo(3,2-e)pyrimidine (Ia) HCl exhibited an IC 50 value for CRF 1 receptor binding of 100 nM.

3. 发明公开

EP1364952A4 BICYCLIC NITROGENOUS FUSED-RING COMPOUND 审中-公开
标题翻译：双环含氮化合物稠合环
公开(公告)号：EP1364952A4
公开(公告)日：2005-03-30
申请号：EP02711424
申请日：2002-02-08
申请人： EISAI CO LTD
发明人： HIBI SHIGEKI , TAKAHASHI YOSHINORI , HOSHINO YORIHISA , KIKUCHI KOICHI , SOEJIMA MOTOHIRO , YOSHIUCHI TATSUYA , SHIN KOGYOKU , ONO MUTSUKO , SHIBATA HISASHI , INO MITSUHIRO , HIRAKAWA TETSUYA
IPC分类号： A61P1/14 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/02 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/00 , A61P15/08 , A61P15/10 , A61P15/12 , A61P17/14 , A61P19/10 , A61P21/00 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/20 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/00 , A61P27/06 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/04 , A61P37/08 , A61P43/00 , C07D471/04 , C07D487/04 , A61K31/437 , A61K31/4985 , A61K31/5025 , A61K31/519 , A61K31/5377
CPC分类号： C07D471/04 , C07D487/04
摘要： A novel compound having an excellent antagonistic effect on a corticotropin-releasing-factor receptor. It is a compound represented by the following formula or a salt thereof. (I) In the formula, R1 represents hydrogen, C¿1-6? alkyl, C1-6 alkoxy, etc.; R?2¿ represents halogeno, cyano, nitro, C¿1-10? alkyl, C2-10 alkenyl, C2-10 alkynyl, etc.; R?3¿ represents an optionally substituted C¿6-14? aromatic hydrocarbon group or an optionally substituted, 5- to 14-membered aromatic heterocyclic group; and X, Y, and Z each independently represents nitrogen or CR?4¿ (wherein R4 represents hydrogen, halogeno, cyano, nitro, optionally halogenated C¿1-6? alkyl, etc.), provided that at least two of X, Y, and Z represent CR?4¿.

4. 发明公开

EP1389618A4 PYRAZOLO 1,5-A PYRIDINES AND MEDICINES CONTAINING THE SAME 有权
标题翻译：吡唑并1,5-吡啶和含有药物
公开(公告)号：EP1389618A4
公开(公告)日：2005-07-20
申请号：EP02720608
申请日：2002-04-25
申请人： EISAI CO LTD
发明人： HIBI SHIGEKI , KIKUCHI KOICHI , HOSHINO YORIHISA , SOEJIMA MOTOHIRO , YOSHIUCHI TATSUYA , SHIN KOGYOKU , ONO MUTSUKO , TAKAHASHI YOSHINORI , SHIBATA HISASHI , INO MITSUHIRO , HIRAKAWA TETSUYA
IPC分类号： A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/00 , A61P19/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P37/08 , A61P43/00 , C07D471/04 , C07F5/02 , C07F7/22 , A61K31/437 , A61K31/444
CPC分类号： C07D471/04 , A61K31/437 , C07F5/025 , C07F7/2212
摘要： Compounds represented by the general formula (I), salts thereof, and hydrates of both: (I) wherein R1 is methoxy, ethyl, methylthio, or the like; R?2, R3 and R4¿ are each hydrogen, halogeno, or the like; R?5 and R6¿ are each a group represented by the general formula: -X5-X6-X7 (wherein X5 is a single bond or CO-; X6 is a single bond, -NR3a-, or the like; X?7 and R3a¿ are each hydrogen, C¿1-10? alkyl, or the like); and Ar is phenyl, pyridyl, or the like.

5. 发明公开

EP1238979A4 FUSED HETEROTRICYCLIC COMPOUNDS, PROCESS FOR PREPARING THE COMPOUNDS AND DRUGS CONTAINING THE SAME 有权
标题翻译： ANNE内衬杂环，制法连接和含药
公开(公告)号：EP1238979A4
公开(公告)日：2003-01-15
申请号：EP00983479
申请日：2000-12-13
申请人： EISAI CO LTD
发明人： HIBI SHIGEKI , HOSHINO YORIHISA , YOSHIUCHI TATSUYA , SHIN KOGYOKU , KIKUCHI KOUICHI , SOEJIMA MOTOHIRO , TABATA MUTSUKO , TAKAHASHI YOSHINORI , SHIBATA HISASHI , HIDA TAKAYUKI , HIRAKAWA TETSUYA , INO MITSUHIRO
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 , A61K31/437 , A61K31/519 , C07D473/02 , C07D495/14
CPC分类号： C07D471/14 , C07D487/14 , C07D491/14
摘要： Compounds represented by general formula (I) are provided, which exhibit antagonism against corticotropin-releasing factor receptor, wherein A, B and C are each independently -(CR1R2)m- (wherein R?1 and R2¿ are each C¿1-6? alkyl or the like, and m is an integer of 1 to 4), -NR?3¿- (wherein R3 is hydrogen or the like), or the like; E and G are each independently a heteroatom such as nitrogen, -(CR6R7)p- (wherein R?6 and R7¿ are each hydrogen or the like, and p is an integer of 0 to 2), or the like; J is a carbon atom substituted with aryl or the like, or a nitrogen atom; K and L are each independently carbon or nitrogen; M is hydrogen, optionally substituted alkyl, or the like; and the partial structures ----- are each a single or double bond.

6. 发明专利

DK1238979T3 未知
公开(公告)号：DK1238979T3
公开(公告)日：2005-06-20
申请号：DK00983479
申请日：2000-12-13
申请人： EISAI CO LTD
发明人： HIDA TAKAYUKI , HIBI SHIGEKI , HOSHINO YORIHISA , YOSHIUCHI TATSUYA , SHIN KOGYOKU , KIKUCHI KOUICHI , SOEJIMA MOTOHIRO , TABATA MUTSUKO , TAKAHASHI YOSHINORI , SHIBATA HISASHI , HIRAKAWA TETSUYA , INO MITSUHIRO
IPC分类号： A61P1/04 , A61P1/08 , A61P1/10 , A61P1/12 , C07D471/14 , C07D487/14 , C07D491/14 , A61K31/437 , A61K31/519 , A61P1/14 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , C07D473/02 , C07D495/14

7. 发明专利

PL367067A1 PYRAZOLO[1,5-A]PYRIDINES AND MEDICINES CONTAINING THE SAME 未知
公开(公告)号：PL367067A1
公开(公告)日：2005-02-21
申请号：PL36706702
申请日：2002-04-25
申请人： EISAI CO LTD
发明人： HIBI SHIGEKI , KIKUCHI KOICHI , HOSHINO YORIHISA , SOEJIMA MOTOHIRO , YOSHIUCHI TATSUYA , SHIN KOGYOKU , ONO MUTSUKO , TAKAHASHI YOSHINORI , SHIBATA HISASHI , INO MITSUHIRO , HIRAKAWA TETSUYA
IPC分类号： A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/00 , A61P19/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P37/08 , A61P43/00 , C07D471/04 , C07F5/02 , C07F7/22 , A61K31/437
摘要： Compounds represented by the general formula: Äwherein R represents methoxy, ethyl, methylthio, etc., R , R and R each represent hydrogen, a halogen, etc., R and R each represent -X -X -X (wherein X represents a single bond or -CO-, X represents a single bond, -NR , etc. and X and R each represent hydrogen, C1-10 alkyl, etc.), and Ar represents phenyl, pyridyl, etc.Ü, salts thereof and hydrates of the foregoing.

8. 发明专利

HU0401292A2 PYRAZOLO[1,5-A]PYRIDINES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AND PROCESS FOR PREPARATION THEREOF 未知
公开(公告)号：HU0401292A2
公开(公告)日：2004-12-28
申请号：HU0401292
申请日：2002-04-25
申请人： EISAI CO LTD
发明人： HIBI SHIGEKI , KIKUCHI KOICHI , HOSHINO YORIHISA , SOEJIMA MOTOHIRO , YOSHIUCHI TATSUYA , SHIN KOGYOKU , ONO MUTSUKO , TAKAHASHI YOSHINORI , SHIBATA HISASHI , INO MITSUHIRO , HIRAKAWA TETSUYA
IPC分类号： A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/00 , A61P19/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P37/08 , A61P43/00 , C07D471/04 , C07F5/02 , C07F7/22
摘要： Compounds represented by the general formula: Äwherein R represents methoxy, ethyl, methylthio, etc., R , R and R each represent hydrogen, a halogen, etc., R and R each represent -X -X -X (wherein X represents a single bond or -CO-, X represents a single bond, -NR , etc. and X and R each represent hydrogen, C1-10 alkyl, etc.), and Ar represents phenyl, pyridyl, etc.Ü, salts thereof and hydrates of the foregoing.

9. 发明专利

CZ20032937A3 Pyrazolo[1,5-a]pyridines and medicaments containing thereof 未知
公开(公告)号：CZ20032937A3
公开(公告)日：2004-03-17
申请号：CZ20032937
申请日：2002-04-25
申请人： EISAI CO LTD
发明人： HIBI SHIGEKI , KIKUCHI KOICHI , HOSHINO YORIHISA , SOEJIMA MOTOHIRO , YOSHIUCHI TATSUYA , SHIN KOGYOKU , ONO MUTSUKO , TAKAHASHI YOSHINORI , SHIBATA HISASHI , INO MITSUHIRO , HIRAKAWA TETSUYA
IPC分类号： A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/00 , A61P19/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P37/08 , A61P43/00 , C07D471/04 , C07F5/02 , C07F7/22 , A61K31/437
摘要： Compounds represented by the general formula: Äwherein R represents methoxy, ethyl, methylthio, etc., R , R and R each represent hydrogen, a halogen, etc., R and R each represent -X -X -X (wherein X represents a single bond or -CO-, X represents a single bond, -NR , etc. and X and R each represent hydrogen, C1-10 alkyl, etc.), and Ar represents phenyl, pyridyl, etc.Ü, salts thereof and hydrates of the foregoing.

10. 发明专利

JP2001233876A TRICYCLIC CONDENSED HETEROCYCLIC COMPOUND, METHOD FOR PRODUCING THE SAME AND MEDICAMENT USING THE SAME 失效
公开(公告)号：JP2001233876A
公开(公告)日：2001-08-28
申请号：JP2000375811
申请日：2000-12-11
申请人： EISAI CO LTD
发明人： HIBI SHIGEKI , HOSHINO TAKEHISA , YOSHIUCHI TATSUYA , SHIN MITSUTAMA , KIKUCHI KOICHI , SOEJIMA HIROYOSHI , TABATA MUTSUKO , TAKAHASHI YOSHINORI , SHIBATA HISASHI , HIDA TAKAYUKI , HIRAKAWA TETSUYA , INO MITSUHIRO
IPC分类号： C07D487/14 , A61K31/4375 , A61K31/4745 , A61K31/519 , A61K31/52 , A61K31/55 , A61P1/00 , A61P1/08 , A61P1/14 , A61P3/04 , A61P3/10 , A61P5/14 , A61P11/06 , A61P13/08 , A61P15/08 , A61P15/10 , A61P15/12 , A61P17/14 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/06 , A61P31/18 , A61P37/00 , A61P37/08 , A61P43/00 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/147 , C07D495/14
摘要： PROBLEM TO BE SOLVED: To provide a new compound having excellent antagonism against corticotropin-releasing factor receptors. SOLUTION: This new compound is shown by the formula [wherein, A and B are each a group of the formula (CR1R2)m (wherein, R1 and R2 are each a 1-6C alkyl or the like) or the formula NR3 (wherein, R3 is H or the like) or the like; E and G are each a group of the formula(CR6R7)p (wherein, R6 and R7 are each H or the like; and p is an integer of 0, 1 or 2) or the like; J is a carbon or nitrogen atom substituted with (halogen-substituted) 1-6C alkyl or the like, or the like; K and L are each a carbon or nitrogen atom; M is H, a halogen atom, (substituted) 1-6C alkyl or the like; and partial structure denotes a single or double bond]. The other objective pharmacologically acceptable salt thereof and hydrates thereof are also provided, respectively.

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