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公开(公告)号:US20090281133A1
公开(公告)日:2009-11-12
申请号:US12387921
申请日:2009-05-08
申请人: David Mark Rotstein , Hanbiao Yang
发明人: David Mark Rotstein , Hanbiao Yang
IPC分类号: A61K31/438 , C07D215/02 , A61P31/18
CPC分类号: C07D471/10
摘要: This invention relates to piperidine derivatives of formula I wherein R1, R2 and R3 are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPR.
摘要翻译: 本发明涉及式I的哌啶衍生物,其中R 1,R 2和R 3如本文所定义,可用于治疗多种疾病,包括涉及CCR5受体调节的疾病。 可以由本发明衍生物治疗或预防的疾病包括HIV和遗传相关的逆转录病毒感染(和所得的获得性免疫缺陷综合征,AIDS),类风湿性关节炎,实体器官移植排斥(移植物抗宿主病),哮喘和COPR。
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公开(公告)号:US20090093501A1
公开(公告)日:2009-04-09
申请号:US12284039
申请日:2008-09-18
IPC分类号: A61K31/438 , C07D471/10 , A61P31/12 , A61P11/00 , A61P37/00 , A61K31/506 , A61K31/4545
CPC分类号: C07D471/10
摘要: This invention relates to piperidine derivatives of formula I wherein R1, R2, R3, R4 and Y are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPR.
摘要翻译: 本发明涉及式I的哌啶衍生物,其中R 1,R 2,R 3,R 4和Y如本文所定义,可用于治疗多种疾病,包括涉及CCR5受体调节的疾病。 可以由本发明衍生物治疗或预防的疾病包括HIV和遗传相关的逆转录病毒感染(和所得的获得性免疫缺陷综合征,AIDS),类风湿性关节炎,实体器官移植排斥(移植物抗宿主病),哮喘和COPR。
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公开(公告)号:US07164019B2
公开(公告)日:2007-01-16
申请号:US11147851
申请日:2005-06-08
IPC分类号: C07D239/24
CPC分类号: C07D487/04
摘要: Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are allieviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.
摘要翻译: 趋化因子受体拮抗剂,特别是根据式(I)的3,7-二氮杂双环[3.3.0]辛烷化合物是可用于治疗或预防人类免疫缺陷病毒(HIV)感染或治疗AIDS的趋化因子CCR5受体的拮抗剂 或ARC。 本发明还提供了治疗与CCR5拮抗剂相关的疾病的方法。 本发明包括药物组合物和使用该化合物治疗这些疾病的方法。 本发明还包括制备式I化合物的方法。
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公开(公告)号:US6150397A
公开(公告)日:2000-11-21
申请号:US337695
申请日:1999-06-21
IPC分类号: C07D295/12 , A61K31/10 , A61K31/12 , A61K31/18 , A61K31/195 , A61K31/27 , A61K31/275 , A61K31/341 , A61K31/40 , A61K31/4015 , A61K31/4402 , A61K31/4409 , A61K31/445 , A61K31/453 , A61K31/5375 , A61P29/00 , A61P37/06 , A61P43/00 , C07C311/15 , C07C311/16 , C07C311/29 , C07C311/37 , C07C311/51 , C07C317/22 , C07C317/24 , C07C317/44 , C07C323/22 , C07C323/67 , C07D207/26 , C07D207/27 , C07D207/48 , C07D211/54 , C07D211/58 , C07D213/42 , C07D295/13 , C07D295/26 , C07D307/38 , C07D307/46 , C07D307/52 , C07D307/56 , C07D333/06 , C07D333/22 , C07D405/06 , A61K31/381
CPC分类号: C07D207/26 , C07C311/16 , C07C311/29 , C07C311/51 , C07C317/22 , C07C317/24 , C07C317/44 , C07C323/22 , C07C323/67 , C07D211/58 , C07D213/42 , C07D295/13 , C07D295/26 , C07D307/46 , C07D307/52 , C07D333/22 , C07D405/06 , C07C2101/04 , C07C2101/14
摘要: The present invention relates to certain 5-aroylnaphthalene derivatives of formula (I): ##STR1## that are inhibitors of prostaglandin G/H synthase, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
摘要翻译: 本发明涉及某些式(I)的5-芳酰基萘衍生物:其为前列腺素G / H合成酶的抑制剂,含有它们的药物组合物,其用途及其制备方法。
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公开(公告)号:US07625905B2
公开(公告)日:2009-12-01
申请号:US11901498
申请日:2007-09-18
IPC分类号: A61K31/4545
CPC分类号: C07D487/04
摘要: Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) wherein R1-R3 and Ar are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.
摘要翻译: 趋化因子受体拮抗剂,特别是根据式(I)的3,7-二氮杂双环[3.3.0]辛烷化合物,其中R 1 -R 3和Ar如本文所定义,是趋化因子CCR5受体的拮抗剂,其可用于治疗或预防人 免疫缺陷病毒(HIV)感染或治疗AIDS或ARC。 本发明还提供了用于治疗被CCR5拮抗剂缓解的疾病的方法。 本发明包括药物组合物和使用该化合物治疗这些疾病的方法。 本发明还包括制备式I化合物的方法。
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公开(公告)号:US20080139544A1
公开(公告)日:2008-06-12
申请号:US12008452
申请日:2008-01-11
IPC分类号: A61K31/537 , C07D401/04 , C07D265/04 , A61K31/4747
CPC分类号: C07D498/10 , A61K31/435 , A61K31/4747 , A61K31/537 , A61K31/538 , A61K45/06 , A61K2300/00
摘要: This invention relates to piperidine derivatives of formulae Ia and Ib with substituents as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. More particularly, the present invention relates to 1-oxa-3,8-diaza-spiro[4.5]decan-2-one and 1-oxa-3,9-diaza-spiro[5.5]undecan-2-one compounds and related derivatives, to compositions containing and to uses of such derivatives. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), diseases of the immune system and inflammatory diseases.
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公开(公告)号:US06979693B2
公开(公告)日:2005-12-27
申请号:US10066040
申请日:2002-02-01
申请人: David Michael Goldstein , Sharada Shenvi Labadie , David Mark Rotstein , Eric Brian Sjogren , Francisco Xavier Talamas
发明人: David Michael Goldstein , Sharada Shenvi Labadie , David Mark Rotstein , Eric Brian Sjogren , Francisco Xavier Talamas
IPC分类号: B01L3/00 , C07D231/38 , C07D401/10 , C07D401/12 , C07D403/12 , G01N21/01 , G01N21/27 , G01N33/49 , G01N33/543 , G01N33/558 , A61K31/415 , A61K31/4155 , C07D401/06
CPC分类号: C07D231/38 , C07D401/10 , C07D401/12 , C07D403/12 , G01N21/01 , G01N21/27 , G01N33/4905 , G01N33/54366 , G01N33/558
摘要: The present invention relates to certain pyrazole derivatives of Formula (I): that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
摘要翻译: 本发明涉及某些式(I)的吡唑衍生物:其为p-38MAP激酶抑制剂,含有它们的药物组合物,其使用方法和制备这些化合物的方法。
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公开(公告)号:US07714018B2
公开(公告)日:2010-05-11
申请号:US11637423
申请日:2006-12-11
IPC分类号: A61K31/40 , C07D487/02 , C07D491/02 , C07D495/02 , C07D497/02 , C07D209/44 , C07D209/52
CPC分类号: C07D487/04
摘要: Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.
摘要翻译: 趋化因子受体拮抗剂,特别是根据式(I)的3,7-二氮杂双环[3.3.0]辛烷化合物是可用于治疗或预防人类免疫缺陷病毒(HIV)感染或治疗AIDS的趋化因子CCR5受体的拮抗剂 或ARC。 本发明还提供了用于治疗被CCR5拮抗剂缓解的疾病的方法。 本发明包括药物组合物和使用该化合物治疗这些疾病的方法。 本发明还包括制备式I化合物的方法。
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公开(公告)号:US20090028818A1
公开(公告)日:2009-01-29
申请号:US12220485
申请日:2008-07-24
IPC分类号: A61K38/20 , C07D401/14 , A61K39/395 , A61P31/18 , A61P11/06 , A61P19/02 , A61P37/02 , A61K31/445
CPC分类号: C07D401/14 , C07D407/14 , C07D413/14
摘要: This invention relates to piperidine derivatives of formula I wherein R1, R2, R3 and R4 are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 receptors is implicated. Disorders that may be treated or prevented by the present derivatives include HIV and genetically related retroviral infections (and the resulting acquired immune deficiency syndrome, AIDS), rheumatoid arthritis, solid organ transplant reject (graft vs. host disease), asthma and COPR.
摘要翻译: 本发明涉及式I的哌啶衍生物,其中R 1,R 2,R 3和R 4如本文所定义,可用于治疗各种疾病,包括涉及CCR5受体调节的疾病。 可以由本发明衍生物治疗或预防的疾病包括HIV和遗传相关的逆转录病毒感染(和所得的获得性免疫缺陷综合征,AIDS),类风湿性关节炎,实体器官移植排斥(移植物抗宿主病),哮喘和COPR。
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公开(公告)号:US06444696B1
公开(公告)日:2002-09-03
申请号:US09909966
申请日:2001-07-19
申请人: David Michael Goldstein , Sharada Shenvi Labadie , David Mark Rotstein , Eric Brian Sjogren , Francisco Xavier Talamas
发明人: David Michael Goldstein , Sharada Shenvi Labadie , David Mark Rotstein , Eric Brian Sjogren , Francisco Xavier Talamas
IPC分类号: A61K314155
CPC分类号: C07D231/38 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/06
摘要: The present invention relates to certain pyrazole derivatives of Formula (I): that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
摘要翻译: 本发明涉及某些式(I)的吡唑衍生物:其为p-38MAP激酶抑制剂,含有它们的药物组合物,其使用方法和制备这些化合物的方法。
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