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公开(公告)号:US06514982B1
公开(公告)日:2003-02-04
申请号:US09439840
申请日:1999-11-12
申请人: Mustapha Haddach , Brian P. Dyck , Charles Q. Huang , Jodie Nelson , Zhiqiang Guo , James R. McCarthy
发明人: Mustapha Haddach , Brian P. Dyck , Charles Q. Huang , Jodie Nelson , Zhiqiang Guo , James R. McCarthy
IPC分类号: C07D48704
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 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
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公开(公告)号:US06531475B1
公开(公告)日:2003-03-11
申请号:US09574751
申请日:2000-05-18
申请人: Mustapha Haddach , Brian P. Dyck , Charles Q. Huang , Jodie Nelson , Zhiqiang Guo , James R. McCarthy
发明人: Mustapha Haddach , Brian P. Dyck , Charles Q. Huang , Jodie Nelson , Zhiqiang Guo , James R. McCarthy
IPC分类号: C07D47114
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 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
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受体拮抗剂具有以下结构:包括立体异构体及其药学上可接受的盐,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
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公开(公告)号:US06723721B2
公开(公告)日:2004-04-20
申请号:US10027789
申请日:2001-12-20
IPC分类号: A61K31495
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 a warm-blooded animals, including stroke. The compounds of this invention have the following structures: wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.
摘要翻译: 公开了可用于治疗多种疾病的化合物,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以下结构: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。
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公开(公告)号:US06348466B1
公开(公告)日:2002-02-19
申请号:US09439841
申请日:1999-11-12
IPC分类号: A61K31495
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 a warm-blooded animals, including stroke. The compounds of this invention have the following structures: wherein n, m, R, R1, R2, X and Ar are as defined herein, including stereoisomes and pharmaceutically acceptable salts thereof.
摘要翻译: 公开了可用于治疗多种疾病的化合物,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以下结构: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。
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公开(公告)号:US06747034B2
公开(公告)日:2004-06-08
申请号:US10016694
申请日:2001-11-02
IPC分类号: A61K31505
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。
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公开(公告)号:US06610678B2
公开(公告)日:2003-08-26
申请号:US10266662
申请日:2002-10-08
IPC分类号: A61K3133
CPC分类号: C07D215/233 , C07D215/12 , C07D215/36 , C07D215/42 , C07D239/94 , C07D401/04
摘要: This invention concerns compounds of formula including 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 amount of a compound of formula (I).
摘要翻译: 本发明涉及包括其立体异构体及其药学上可接受的酸加成盐形式的化合物,其中R 1是C 1-6烷基,NR 6 R 7,OR 6或SR 7; R2是氢,C1-6烷基,C1-6烷氧基或C1-6烷硫基; R3是Ar1或Het1; R 4和R 5各自独立地选自氢,卤素,C 1-6烷基,C 1-6烷氧基,三氟甲基,氰基,硝基,氨基和单或二(C 1-6烷基)氨基; R6是氢,C1-6烷基,C1-6烷基磺酰基,C1-6烷基亚磺酰基或C1-6烷硫基; R 7是氢,C 1-8烷基,一或二(C 3-6环烷基)甲基,C 3-6环烷基,C 3-6烯基,羟基C 1-6烷基,C 1-6烷基羰氧基-C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 6是C 1-8烷基,单或二(C 3-6环烷基) - 甲基,Ar 2 CH 2,C 1-6烷氧基C 1-6烷基,羟基C 1-6烷基,C 3-6烯基,噻吩基甲基,呋喃基甲基,C 1-6烷硫基C 1-6烷基,单或二 1-6烷基)氨基C 1-6烷基,二(C 1-6烷基)氨基,C 1-6烷基羰基C 1-6烷基; 或R6和R7与它们所连接的氮原子一起可以形成任选被C 1-6烷基或C 1-6烷氧基C 1-6烷基取代的吡咯烷基,哌啶基,高哌啶基或吗啉基; Ar 1和Ar 2各自为任意取代的苯基; Het1是任选取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效的方法治疗与CRF分泌过高有关的疾病,如抑郁症,焦虑症,药物滥用
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公开(公告)号:US06482836B1
公开(公告)日:2002-11-19
申请号:US09403393
申请日:1999-10-19
IPC分类号: A61K314706
CPC分类号: C07D215/233 , C07D215/12 , C07D215/36 , C07D215/42 , C07D239/94 , C07D401/04
摘要: This invention concerns compounds of formula including 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(C3-6cycloalkyl)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 amount of a compound of formula (I).
摘要翻译: 本发明涉及包括立体异构体及其药学上可接受的酸加成盐形式的化合物,其中R 1是C 1-6烷基,NR 6 R 7,OR 6或SR 7; R2是氢,C1-6烷基,C1-6烷氧基或C1-6烷硫基; R3是Ar1或Het1; R 4和R 5各自独立地选自氢,卤素,C 1-6烷基,C 1-6烷氧基,三氟甲基,氰基,硝基,氨基和单或二(C 1-6烷基)氨基; R6是氢,C1-6烷基,C1-6烷基磺酰基,C1-6烷基亚磺酰基或C1-6烷硫基; R 7是氢,C 1-8烷基,一或二(C 3-6环烷基)甲基,C 3-6环烷基,C 3-6烯基,羟基C 1-6烷基,C 1-6烷基羰氧基-C 1-6烷基或C 1-6烷氧基C 1-6烷基; R 6是C 1-8烷基,单或二(C 3-6环烷基) - 甲基,Ar 2 CH 2,C 1-6烷氧基C 1-6烷基,羟基C 1-6烷基,C 3-6烯基,噻吩基甲基,呋喃基甲基,C 1-6烷硫基C 1-6烷基,单或二 1-6烷基)氨基C 1-6烷基,二(C 1-6烷基)氨基,C 1-6烷基羰基C 1-6烷基; 或R6和R7与它们所连接的氮原子一起可以形成任选被C 1-6烷基或C 1-6烷氧基C 1-6烷基取代的吡咯烷基,哌啶基,高哌啶基或吗啉基; Ar 1和Ar 2各自为任意取代的苯基; Het1是任选取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效的治疗来治疗与CRF过度分泌有关的疾病的方法,例如抑郁,焦虑,药物滥用
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公开(公告)号:US20120208792A1
公开(公告)日:2012-08-16
申请号:US13315103
申请日:2011-12-08
IPC分类号: A61K31/4745 , A61K31/5377 , A61K31/497 , C12N5/09 , A61P35/00 , A61P35/02 , A61P29/00 , A61K31/496 , A61K31/551
CPC分类号: C07D471/04 , C07D471/14 , C07D495/04 , C07D513/04
摘要: The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate Pim kinase activity and/or FMS-like tyrosine kinase (Flt) activity. The invention also relates in part to methods for using such molecules.
摘要翻译: 本发明部分地涉及具有某些生物活性的分子,包括但不限于抑制细胞增殖,调节蛋白激酶活性和调节聚合酶活性。 本发明的分子可以调节Pim激酶活性和/或FMS样酪氨酸激酶(Flt)活性。 本发明还部分涉及使用这种分子的方法。
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公开(公告)号:US20120190669A1
公开(公告)日:2012-07-26
申请号:US13354563
申请日:2012-01-20
IPC分类号: A61K31/404 , C07D405/14 , A61K31/551 , A61P29/00 , A61K31/496 , A61P35/00 , A61P35/02 , C07D405/06 , A61K31/4439
CPC分类号: C07D405/06 , C07D405/14 , C07D417/14
摘要: The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.
摘要翻译: 本发明提供抑制PIM激酶和Flt3激酶的化合物,以及含有这些化合物的组合物。 这些化合物和组合物可用于治疗增殖性疾病如癌症,以及其它激酶相关病症,包括炎症。
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公开(公告)号:US20100298302A1
公开(公告)日:2010-11-25
申请号:US12784055
申请日:2010-05-20
申请人: Fabrice PIERRE , Mustapha Haddach , Peter C. Chua
发明人: Fabrice PIERRE , Mustapha Haddach , Peter C. Chua
IPC分类号: A61K31/551 , C07D487/04 , A61K31/4985 , C07D243/08 , C07D413/14 , A61K31/5377 , A61P9/00 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/00
CPC分类号: C07D487/04 , C07D413/14
摘要: The invention provides compounds that inhibit selected kinases (Pim, Flt and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders.
摘要翻译: 本发明提供抑制所选择的激酶(Pim,Flt和/或CK2激酶)的化合物和含有这些化合物的组合物。 这些化合物和组合物可用于治疗增殖性疾病如癌症,以及其它激酶相关病症,包括炎症,疼痛以及某些感染和免疫学疾病。
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