公开(公告)号：US20080103125A1

公开(公告)日：2008-05-01

申请号：US11901498

申请日：2007-09-18

申请人： Remy Lemoine ,  Chris Melville ,  David Rotstein ,  Jutta Wanner

发明人： Remy Lemoine ,  Chris Melville ,  David Rotstein ,  Jutta Wanner

IPC分类号： A61K31/4545 ,  A61K31/4155 ,  A61K31/4439 ,  A61K31/501 ,  A61P31/18 ,  C07D487/04 ,  A61K31/506 ,  A61K31/497 ,  A61K31/454

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定义如上 本文是可用于治疗或预防人类免疫缺陷病毒（HIV）感染或治疗AIDS或ARC的趋化因子CCR5受体的拮抗剂。 本发明还提供了治疗由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。

公开(公告)号：US20070117859A1

公开(公告)日：2007-05-24

申请号：US11637423

申请日：2006-12-11

申请人： Eun Lee ,  Chris Melville ,  David Rotstein

发明人： Eun Lee ,  Chris Melville ,  David Rotstein

IPC分类号： A61K31/407 ,  C07D487/02

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.

公开(公告)号：US20060014767A1

公开(公告)日：2006-01-19

申请号：US11147851

申请日：2005-06-08

申请人： Eun Lee ,  Chris Melville ,  David Rotstein

发明人： Eun Lee ,  Chris Melville ,  David Rotstein

IPC分类号： A61K31/513 ,  C07D487/02

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。

公开(公告)号：US20050176703A1

公开(公告)日：2005-08-11

申请号：US11055642

申请日：2005-02-10

申请人： Stephen Gabriel ,  David Rotstein

发明人： Stephen Gabriel ,  David Rotstein

IPC分类号： A61K31/435 ,  A61K31/4747 ,  A61K31/537 ,  A61K31/538 ,  A61K45/06 ,  C07D498/10 ,  C07D491/10

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.

摘要翻译： 本发明涉及式Ia和Ib的哌啶衍生物，其具有如本文定义的取代基，其可用于治疗各种疾病，包括涉及CCR5受体调节的各种疾病。 更具体地说，本发明涉及1-氧杂-3,8-二氮杂 - 螺[4.5]癸-2-酮和1-氧杂-3,9-二氮杂螺[5.5]十一烷-2-酮化合物及其相关 衍生物，含有和用于此类衍生物的组合物。 本衍生物可能治疗或预防的疾病包括艾滋病毒和基因相关的逆转录病毒感染（以及由此产生的获得性免疫缺陷综合征，艾滋病），免疫系统疾病和炎性疾病。

公开(公告)号：US20070191406A1

公开(公告)日：2007-08-16

申请号：US11706728

申请日：2007-02-15

申请人： Rcmy Lemoine ,  Chris Melville ,  Fernando Padilla ,  David Rotstein ,  Jutta Wanner

发明人： Rcmy Lemoine ,  Chris Melville ,  Fernando Padilla ,  David Rotstein ,  Jutta Wanner

IPC分类号： A61K31/506 ,  A61K31/4439 ,  C07D487/02

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 R6c and X1 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，R 3， 本文所定义的是可用于治疗或预防人类免疫缺陷病毒（HIV）感染或治疗AIDS或ARC的趋化因子CCR5受体的拮抗剂。 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。

公开(公告)号：US20070191335A1

公开(公告)日：2007-08-16

申请号：US11706807

申请日：2007-02-15

申请人： Remy Lemoine ,  Chris Melville ,  David Rotstein ,  Jutta Wanner

发明人： Remy Lemoine ,  Chris Melville ,  David Rotstein ,  Jutta Wanner

IPC分类号： A61K31/506 ,  A61K31/497 ,  A61K31/501 ,  A61K31/454 ,  A61K31/4439 ,  C07D487/02

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 R6c and X1 are as defined herein are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV-1) 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 treating diseases mediated by the CCR5 receptor.

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，R 3， X和X 1如本文所定义的可用于治疗或预防人类免疫缺陷病毒（HIV-1）感染或治疗AIDS或ARC的趋化因子CCR5受体的拮抗剂。 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由CCR5受体介导的疾病的方法。