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公开(公告)号：US20080249087A1
公开(公告)日：2008-10-09
申请号：US12079746
申请日：2008-03-28
IPC分类号： A61K31/537 , C07D265/14 , A61P31/18 , A61P11/06 , A61P9/00 , A61P29/00 , A61P19/02
CPC分类号： C07D498/10
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 COPD.
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是 如本文所定义的，可用于治疗多种疾病，包括涉及CCR5受体调节的疾病。 本衍生物可能治疗或预防的疾病包括艾滋病病毒和遗传相关的逆转录病毒感染（以及由此获得的获得性免疫缺陷综合征，AIDS），类风湿关节炎，实体器官移植排斥（移植物抗宿主病），哮喘和COPD。
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公开(公告)号：US07625891B2
公开(公告)日：2009-12-01
申请号：US12079746
申请日：2008-03-28
IPC分类号： C07D413/14 , A61K31/537
CPC分类号： C07D498/10
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 COPD.
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。 本衍生物可能治疗或预防的疾病包括艾滋病病毒和遗传相关的逆转录病毒感染（以及由此获得的获得性免疫缺陷综合征，AIDS），类风湿关节炎，实体器官移植排斥（移植物抗宿主病），哮喘和COPD。
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3.发明授权公开(公告)号：US07091200B2
公开(公告)日：2006-08-15
申请号：US10971522
申请日：2004-10-22
申请人： Cyrus Kephra Becker , Joan Marie Caroon , Chris Richard Melville , Fernando Padilla , Jürg Roland Pfister , Xiaoming Zhang
发明人： Cyrus Kephra Becker , Joan Marie Caroon , Chris Richard Melville , Fernando Padilla , Jürg Roland Pfister , Xiaoming Zhang
IPC分类号： A61K31/54 , A61P13/08 , C07D285/22 , A61K31/549 , A61K31/517 , A61K31/519 , C07D487/04 , C07D241/36 , C07D471/02
CPC分类号： C07D417/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/04
摘要： This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is carbon or nitrogen, Y is carbon, and X-Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要翻译： 本发明涉及通常为α-1A / B肾上腺素受体拮抗剂并由式I表示的化合物：其中Z为-C（O） - 或-S（O）2 - ，X为 碳或氮，Y是碳，并且XY一起考虑为环A的两个邻接的原子，所述环是每个环5至6个原子的稠合芳环，每个环任选地并入一个至两个杂原子，选自N，O， 或S; 而其它取代基如说明书中所定义; 或各异构体，异构体的外消旋或非外消旋混合物，或其药学上可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。
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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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5.发明授权公开(公告)号：US06900220B2
公开(公告)日：2005-05-31
申请号：US10040319
申请日：2002-01-02
申请人： Cyrus Kephra Becker , Joan Marie Caroon , Chris Richard Melville , Fernando Padilla , Jürg Roland Pfister , Xiaoming Zhang
发明人： Cyrus Kephra Becker , Joan Marie Caroon , Chris Richard Melville , Fernando Padilla , Jürg Roland Pfister , Xiaoming Zhang
IPC分类号： A61K31/517 , A61K31/519 , A61K31/549 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/04 , A61K31/535 , C07D417/00 , C07D471/00 , C07D487/00
CPC分类号： C07D417/04 , C07D401/04 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/14 , C07D487/04 , C07D491/04
摘要： This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is carbon or nitrogen, Y is carbon, and X—Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要翻译： 本发明涉及通常为α-1A / B肾上腺素受体拮抗剂并由式I表示的化合物：其中Z为-C（O） - 或-S（O）2 - ，X为 碳或氮，Y是碳，并且XY一起考虑为环A的两个邻接的原子，所述环是每个环5至6个原子的稠合芳环，每个环任选地并入一个至两个杂原子，选自N，O， 或S; 而其它取代基如说明书中所定义; 或各异构体，异构体的外消旋或非外消旋混合物，或其药学上可接受的盐或溶剂合物。 本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。
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![Octahydro-pyrrolo[3,4-c]pyrrole CCR5 receptor antagonists](/abs-image/US/2009/12/01/US07625905B2/abs.jpg.150x150.jpg)
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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7.发明授权Arylamine-substituted quinazolinone compounds useful as alpha 1A/B adrenergic receptor antagonists 失效可用作α1A / B肾上腺素能受体拮抗剂的芳胺取代的喹唑啉酮化合物公开(公告)号：US07244738B2
公开(公告)日：2007-07-17
申请号：US10884768
申请日：2004-07-02
申请人： Terrence Joseph Connolly , Paul Francis Keitz , Eun Kyung Lee , Jim Li , Francisco Javier Lopez-Tapia , Patrick Finbar McGarry , Chris Richard Melville , Dov Nitzan , Counde O'Yang , Fernando Padilla , Klaus Kurt Weinhardt
发明人： Terrence Joseph Connolly , Paul Francis Keitz , Eun Kyung Lee , Jim Li , Francisco Javier Lopez-Tapia , Patrick Finbar McGarry , Chris Richard Melville , Dov Nitzan , Counde O'Yang , Fernando Padilla , Klaus Kurt Weinhardt
IPC分类号： A61K31/517 , A01N43/54 , C07D239/72 , A61K31/549 , C07D417/02 , C07D285/26
CPC分类号： C07D401/12 , C07D239/90 , C07D239/95 , C07D285/24 , C07D401/14 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds represented by Formula I: which are useful as are alpha-1A/B adrenoceptor antagonists, to methods of treating conditions associated with the activity of alpha-1A/B adrenoceptors, and to methods of making said compounds, wherein Ar, Z, R, R′, R5 and R10 are as defined herein.
摘要翻译： 由式I表示的化合物：其可用作α-1A / B肾上腺素受体拮抗剂，用于治疗与α-1A / B肾上腺素受体的活性相关的病症的方法，以及制备所述化合物的方法，其中Ar，Z，R R'，R 5和R 10如本文所定义。
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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：US06559153B2
公开(公告)日：2003-05-06
申请号：US09942385
申请日：2001-08-29
IPC分类号： C07D40112
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： This invention relates to compounds which are generally alpha-1B adrenergic receptor antagonists and which are represented by Formula (I): wherein R′, R″, R1, R2, m, n, and A are as defined in the specification, or acceptable prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要翻译： 本发明涉及通常为α-1B肾上腺素能受体拮抗剂并由式（I）表示的化合物：其中R'，R“，R 1，R 2，m，n和A如说明书中所定义，或 可接受的前药，盐或溶剂化物。 本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。
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