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。

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：US20070265446A1

公开(公告)日：2007-11-15

申请号：US11821493

申请日：2007-06-22

申请人： Terrence Connolly ,  Paul Keitz ,  Eun Lee ,  Jim Li ,  Francisco Lopez-Tapia ,  Patrick McGarry ,  Chris Melville ,  Dov Nitzan ,  Counde O'Yang ,  Fernando Padilla ,  Klaus Weinhardt

发明人： Terrence Connolly ,  Paul Keitz ,  Eun Lee ,  Jim Li ,  Francisco Lopez-Tapia ,  Patrick McGarry ,  Chris Melville ,  Dov Nitzan ,  Counde O'Yang ,  Fernando Padilla ,  Klaus Weinhardt

IPC分类号： C07D239/88 ,  C07D401/02

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.

公开(公告)号：US20050124607A1

公开(公告)日：2005-06-09

申请号：US10884595

申请日：2004-07-02

申请人： Elbert Chin ,  Richard Cournoyer ,  Paul Keitz ,  Eun Lee ,  Francisco Lopez-Tapia ,  Chris Melville ,  Fernando Padilla ,  Klaus Weinhardt

发明人： Elbert Chin ,  Richard Cournoyer ,  Paul Keitz ,  Eun Lee ,  Francisco Lopez-Tapia ,  Chris Melville ,  Fernando Padilla ,  Klaus Weinhardt

IPC分类号： A61K31/517 ,  A61K31/549 ,  A61P13/00 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/02 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10 ,  C07D498/10 ,  C07D43/02

CPC分类号： C07D401/04 ,  C07D239/95 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/10

摘要： Compounds which are alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Q is a monocyclic or bicyclic optionally-substituted heterocyclic ring as defined herein; Z is —C(═O)— or —S(═O)2—; R and R′ are lower alkyl; R5 is halogen, cyano, hydroxy, —R6, or —OR6; and R6 is alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclo, or substituted heterocyclo; and pharmaceutically-acceptable salts, hydrates, prodrugs, and isomers thereof.

摘要翻译： 作为α-1A / B肾上腺素受体拮抗剂并由式I表示的化合物：其中Q是如本文所定义的单环或双环任选取代的杂环; Z是-C（-O） - 或-S（-O）2 - 。 R和R'是低级烷基; R 5是卤素，氰基，羟基，-R 6或-OR 6; R 6是烷基，取代的烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，环烷基，取代的环烷基，杂环或取代的杂环; 及其药学上可接受的盐，水合物，前体药物和异构体。

公开(公告)号：US20050107365A1

公开(公告)日：2005-05-19

申请号：US10971522

申请日：2004-10-22

申请人： Cyrus Becker ,  Joan Caroon ,  Chris Melville ,  Fernando Padilla ,  Jurg Pfister ,  Xiaoming Zhang

发明人： Cyrus Becker ,  Joan Caroon ,  Chris Melville ,  Fernando Padilla ,  Jurg 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

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.

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：US20050038016A1

公开(公告)日：2005-02-17

申请号：US10884768

申请日：2004-07-02

申请人： Terrence Connolly ,  Paul Keitz ,  Eun Lee ,  Jim Li ,  Francisco Lopez-Tapia ,  Patrick McGarry ,  Chris Melville ,  Dov Nitzan ,  Counde O'Yang ,  Frenando Padilla ,  Klaus Weinhardt

发明人： Terrence Connolly ,  Paul Keitz ,  Eun Lee ,  Jim Li ,  Francisco Lopez-Tapia ,  Patrick McGarry ,  Chris Melville ,  Dov Nitzan ,  Counde O'Yang ,  Frenando Padilla ,  Klaus Weinhardt

IPC分类号： A61K31/517 ,  A61K31/549 ,  C07D239/90 ,  C07D239/95 ,  C07D285/24 ,  C07D285/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/02 ,  C07D417/12

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。

公开(公告)号：US06576619B2

公开(公告)日：2003-06-10

申请号：US09317523

申请日：1999-05-24

申请人： Brent K. Blackburn ,  Chris Melville ,  Jeff A. Zablocki ,  Venkata P. Palle ,  Elfaith O. Elzein ,  Lisa Wang

发明人： Brent K. Blackburn ,  Chris Melville ,  Jeff A. Zablocki ,  Venkata P. Palle ,  Elfaith O. Elzein ,  Lisa Wang

IPC分类号： A61K3170

CPC分类号： C07H19/16

摘要： Esters of N6-oxa, thia, thioxa and azacycloalkyl substituted adenosine derivatives having the following formula; wherein the compounds are selective adenosine type 1 receptor agonists that are useful for the treatment cardiovascular diseases and central nervous system disorders.

摘要翻译： 具有下式的N6-氧杂，硫杂，噻吩和氮杂环烷基取代的腺苷衍生物的酯;其中所述化合物是可用于治疗心血管疾病和中枢神经系统疾病的选择性腺苷1型受体激动剂。