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1. 发明专利

JP2002121194A PYRAZOLOPYRIMIDINE 审中-公开
公开(公告)号：JP2002121194A
公开(公告)日：2002-04-23
申请号：JP2001265611
申请日：2001-09-03
申请人： JANSSEN PHARMACEUTICA NV , NEUROCRINE BIOSCIENCES INC
发明人： CHEN CHEN , WEBB THOMAS R , MCCARTHY JAMES R , MORAN TERENCE J , WILCOXEN KEITH M , CHARLES FANG
IPC分类号： A61K31/00 , A61K31/435 , A61K31/439 , A61K31/485 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/519 , A61K31/529 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61P1/00 , A61P1/04 , A61P1/12 , A61P1/14 , A61P3/00 , A61P3/04 , A61P9/00 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/14 , A61P13/12 , A61P19/02 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/30 , A61P25/32 , A61P29/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D471/08 , C07D471/10 , C07D487/04 , C07D489/09 , C07D491/18 , C07D491/20 , C07D495/22
摘要： PROBLEM TO BE SOLVED: To provide pyrazolopyrimidine that is antagonistic to CRF receptor and a pharmaceutical composition that contain the same as active ingredients. SOLUTION: The objective compound is a pyrazolopyrimidine is represented by general formula (II') [R2 is an alkyl, an alkyloxy or an alkylthio; R3 is H, an alkyl, an alkyl-sulfonyl, an alkylsulfonyloxy or an alkylthio; Ar is phenyl, a substituted phenyl, pyridinyl, substituted pyridinyl; W' is hydroxy, a halogen, mesityloxy or tosyloxy], typically 3-(2,4-dichlorophenyl)-5-methyl-7-(N-propyl-N- cyclopropane-methylamino)-pyrazolo[2,3-a]pyrimidine. The pharmaceutical composition is effective for treating the endocrinological, psychiatric and neurological conditions or diseases including the disorders relating to general stress, for example, depression.

2. 发明申请

WO0240480A3 CRF RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 审中-公开
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：WO0240480A3
公开(公告)日：2003-05-15
申请号：PCT/US0147919
申请日：2001-11-02
申请人： NEUROCRINE BIOSCIENCES INC , HADDACH MUSTAPHA , LANIER MARION C , HUANG CHARLES Q , MCCARTHY JAMES R
发明人： HADDACH MUSTAPHA , LANIER MARION C , HUANG CHARLES Q , MCCARTHY JAMES R
IPC分类号： A61K31/519 , A61K31/551 , A61P1/00 , A61P5/04 , A61P25/00 , A61P25/22 , A61P25/24 , A61P43/00 , C07D471/06 , C07D471/16
CPC分类号： C07D471/06
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.
摘要翻译：公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。

3. 发明申请

WO0027846A3 CRF RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 审中-公开
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：WO0027846A3
公开(公告)日：2000-11-16
申请号：PCT/US9927054
申请日：1999-11-12
申请人： NEUROCRINE BIOSCIENCES INC , HADDACH MUSTAPHA , NELSON JODIE , DYCK BRIAN P , GUO ZHIQIANG , HUANG CHARLES Q , MCCARTHY JAMES R
发明人： HADDACH MUSTAPHA , NELSON JODIE , DYCK BRIAN P , GUO ZHIQIANG , HUANG CHARLES Q , MCCARTHY JAMES R
IPC分类号： A61K31/4985 , A61K31/551 , A61P5/02 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/24 , C07D471/16 , C07D487/16
CPC分类号： C07D471/16 , C07D487/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have structure (I) including stereoisomers and pharmaceutically acceptable salts thereof, wherein n , m , A, B, C, R, R1, R2 and Ar are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
摘要翻译：公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。本发明的CRF受体拮抗剂具有包括立体异构体及其药学上可接受的盐的结构（I），其中n，m，A，B，C，R，R 1，R 2 和Ar如本文所定义。还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

4. 发明申请

WO0027850A2 CRF RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 审中-公开
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：WO0027850A2
公开(公告)日：2000-05-18
申请号：PCT/US9926984
申请日：1999-11-12
申请人： NEUROCRINE BIOSCIENCES INC , HADDACH MUSTAPHA , GUO ZHIQIANG , MCCARTHY JAMES R
发明人： HADDACH MUSTAPHA , GUO ZHIQIANG , MCCARTHY JAMES R
IPC分类号： A61K31/4985 , A61P1/00 , A61P1/14 , A61P3/04 , A61P9/10 , A61P9/12 , A61P25/00 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/30 , A61P29/00 , A61P37/02 , A61P43/00 , C07D471/16 , C07D487/16 , A61K31/551
CPC分类号： C07D471/16 , C07D487/16
摘要： Compounds are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in warmblooded animals, including stroke. The compounds of this invention have structures (I): (a) wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.
摘要翻译：公开了可用于治疗各种疾病的化合物，包括治疗在温血动物（包括中风）中表现出CRF过度分泌的病症。本发明的化合物具有结构（I）：（a）其中n，m，R，R 1，R 2，X和Ar如本文所定义，包括立体异构体及其药学上可接受的盐。

5. 发明申请

WO9835967A3 CRF RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO 审中-公开
标题翻译： CRF受体拮抗剂及其相关方法
公开(公告)号：WO9835967A3
公开(公告)日：1998-12-10
申请号：PCT/US9802932
申请日：1998-02-17
申请人： NEUROCRINE BIOSCIENCES INC , MCCARTHY JAMES R
发明人： MCCARTHY JAMES R
IPC分类号： A61K31/4184 , A61K31/437 , A61K31/4375 , A61K31/5025 , A61K31/519 , A61K31/53 , A61P1/04 , A61P1/14 , A61P3/04 , A61P9/08 , A61P9/12 , A61P25/22 , A61P25/24 , A61P27/02 , A61P29/00 , C07D235/08 , C07D471/04 , C07D473/00 , C07D487/04 , C07D487/00
CPC分类号： C07D471/04 , C07D235/08 , C07D473/00 , C07D487/04
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animal, such as stroke. In formulae (I), (II), (III), (IV), (V) and (VI), A, B, C are all C or N. Ar, R1 and R2 are as defined in the application.

6. 发明专利

DE69818248D1 未知
公开(公告)号：DE69818248D1
公开(公告)日：2003-10-23
申请号：DE69818248
申请日：1998-04-15
申请人： JANSSEN PHARMACEUTICA NV , NEUROCRINE BIOSCIENCES INC
发明人： HUANG CHARLES , WILCOXEN KEITH M , CHEN CHEN , HADDACH MUSTAPHA , MCCARTHY JAMES R
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/517 , A61P1/00 , A61P25/00 , A61P25/08 , A61P25/22 , A61P25/24 , A61P43/00 , C07D215/12 , C07D215/22 , C07D215/233 , C07D215/36 , C07D215/42 , C07D239/94 , C07D401/04 , A61K31/495
摘要： This invention concerns compounds of formulaincluding the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono- or di(C3-6cyclo-alkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C1-6alkyl or C1-6alkyloxyC1-6alkyl; and Ar1 and Ar2 are each optionally substituted phenyl; and Het1 is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective

7. 发明专利

NO20031997D0 未知
公开(公告)号：NO20031997D0
公开(公告)日：2003-05-02
申请号：NO20031997
申请日：2003-05-02
申请人： NEUROCRINE BIOSCIENCES INC
发明人： HADDACH MUSTAPHA , LANIER MARION C , HUANG CHARLES Q , MCCARTHY JAMES R
IPC分类号： A61K31/519 , A61K31/551 , A61P1/00 , A61P5/04 , A61P25/00 , A61P25/22 , A61P25/24 , A61P43/00 , C07D471/06 , C07D471/16 , C07D
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.

8. 发明专利

PT1129091E 未知
公开(公告)号：PT1129091E
公开(公告)日：2003-02-28
申请号：PT99960363
申请日：1999-11-12
申请人： NEUROCRINE BIOSCIENCES INC
发明人： MCCARTHY JAMES R , HADDACH MUSTAPHA , NELSON JODIE , DYCK BRIAN P , GUO ZHIQIANG , HUANG CHARLES Q
IPC分类号： A61K31/4985 , A61K31/551 , A61P5/02 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/24 , C07D471/16 , C07D487/16
摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure:including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2 and Ar are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same

9. 发明专利

PT863882E 未知
公开(公告)号：PT863882E
公开(公告)日：2002-07-31
申请号：PT96934690
申请日：1996-10-15
申请人： JANSSEN PHARMACEUTICA NV , NEUROCRINE BIOSCIENCES INC
发明人： MCCARTHY JAMES R , WEBB THOMAS R , MORAN TERENCE J
IPC分类号： C07D251/18 , A61K31/00 , A61K31/505 , A61P25/22 , A61P25/24 , A61P43/00 , C07D239/42 , C07D239/48 , C07D251/14
摘要： Pyrimidines and triazines of formula (I)wherein R is C1-6alkyl, amino, mono- or diC1-6alkylamino; R1 is hydrogen, C1-6alkyl, C3-6alkenyl, hydroxyC1-6alkyl or C1-6alkyloxy-C1-6alkyl; R2 is C1-6alkyl, mono- or diC3-6cycloalkylmethyl, phenylmethyl, substituted phenylmethyl, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, C3-6alkenyl; or R1 and R2 taken together with the nitrogen to which they are attached may form a pyrrolidinyl, morpholinyl or piperidinyl group; X is N or CR3; R3 is hydrogen or C1-6alkyl; R4 is phenyl or substituted phenyl; A is or -CR7R8- wherein R5 and R6 each independently are hydrogen or C1-4alkyl; R7 is hydrogen or OH, R8 is hydrogen or C1-6alkyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing these compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

10. 发明专利

DE69708059T2 未知
公开(公告)号：DE69708059T2
公开(公告)日：2002-07-18
申请号：DE69708059
申请日：1997-01-30
申请人： JANSSEN PHARMACEUTICA NV , NEUROCRINE BIOSCIENCES INC
发明人： CHEN CHEN , WEBB THOMAS R , MCCARTHY JAMES R , MORAN TERENCE J
IPC分类号： A61P5/04 , A61P25/18 , C07D495/04 , A61K31/505
摘要： This invention concerns compounds of formulaincluding the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO2; R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula -Alk-O-CO-Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).

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