公开(公告)号：WO2012129084A3

公开(公告)日：2012-09-27

申请号：PCT/US2012/029417

申请日：2012-03-16

Applicant: GENZYME CORPORATION ,  BOURQUE, Elyse ,  CELATKA, Cassandra ,  HIRTH, Bradford ,  METZ, Markus ,  ZHAO, Zhong ,  SKERLJ, Renato ,  XIANG, Yibin ,  JANCISICS, Katherine ,  MARSHALL, John ,  CHENG, Seng ,  SCHEULE, Ronald ,  CABRERA-SALAZAR, Mario ,  GOOD, Andrew

Inventor： BOURQUE, Elyse ,  CELATKA, Cassandra ,  HIRTH, Bradford ,  METZ, Markus ,  ZHAO, Zhong ,  SKERLJ, Renato ,  XIANG, Yibin ,  JANCISICS, Katherine ,  MARSHALL, John ,  CHENG, Seng ,  SCHEULE, Ronald ,  CABRERA-SALAZAR, Mario ,  GOOD, Andrew

IPC: A01N43/00

Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.

公开(公告)号：WO2008070758A1

公开(公告)日：2008-06-12

申请号：PCT/US2007/086588

申请日：2007-12-06

Applicant: GENZYME CORPORATION ,  BOURQUE, Elyse ,  METZ, Markus ,  BAIRD, Ian, R. ,  YANG, Wen ,  BRIDGER, Gary ,  SKERLJ, Renato, T.

Inventor： BOURQUE, Elyse ,  METZ, Markus ,  BAIRD, Ian, R. ,  YANG, Wen ,  BRIDGER, Gary ,  SKERLJ, Renato, T.

IPC: A01N43/40 ,  A61K31/445

CPC classification number: C07D417/14 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14

Abstract: Compounds that modulate the activity of chemokine receptors, in particular CCR5, are disclosed.

Abstract translation: 公开了调节趋化因子受体，特别是CCR5的活性的化合物。

公开(公告)号：WO2006138350A2

公开(公告)日：2006-12-28

申请号：PCT/US2006/023125

申请日：2006-06-14

Applicant: ANORMED INC. ,  ZHOU, Yuanxi ,  BOURQUE, Elyse ,  ZHU, Yongbao ,  LANGILLE, Jonathan ,  METZ, Markus ,  YANG, Wen ,  MCEACHERN, Ernest, J. ,  HARWIG, Curtis ,  BAIRD, Ian, R. ,  LI, Tong-shuang ,  SKERLJ, Renato, T.

Inventor： ZHOU, Yuanxi ,  BOURQUE, Elyse ,  ZHU, Yongbao ,  LANGILLE, Jonathan ,  METZ, Markus ,  YANG, Wen ,  MCEACHERN, Ernest, J. ,  HARWIG, Curtis ,  BAIRD, Ian, R. ,  LI, Tong-shuang ,  SKERLJ, Renato, T.

IPC: A61K31/4545

CPC classification number: C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

Abstract: The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR5. Thesd compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).

Abstract translation: 本发明涉及趋化因子受体结合化合物，药物组合物及其用途。 更具体地，本发明涉及趋化因子受体活性的调节剂，优选CCR5的调节剂。 该化合物显示针对人类免疫缺陷病毒（HIV）感染靶细胞的保护作用。

公开(公告)号：WO2004091518A3

公开(公告)日：2004-12-23

申请号：PCT/US2004011328

申请日：2004-04-12

Applicant: ANORMED INC ,  BRIDGER GARY J ,  MCEACHERN ERNEST J ,  SKERLJ RENATO ,  SCHOLS DOMINIQUE ,  BAIRD IAN ,  KALLER AL ,  HARWIG CURTIS ,  ZHU YONGBAO ,  CHEN GANG ,  SKUPINSKA KRYSTYNA

Inventor： BRIDGER GARY J ,  MCEACHERN ERNEST J ,  SKERLJ RENATO ,  SCHOLS DOMINIQUE ,  BAIRD IAN ,  KALLER AL ,  HARWIG CURTIS ,  ZHU YONGBAO ,  CHEN GANG ,  SKUPINSKA KRYSTYNA

IPC: C07D213/38 ,  C07D213/61 ,  C07D213/65 ,  C07D213/69 ,  C07D213/70 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D213/80 ,  C07D213/82 ,  C07D213/89 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D451/04 ,  C07D471/06 ,  C07D401/02 ,  A61K31/44 ,  A61K31/47

CPC classification number: C07D413/14 ,  C07D213/38 ,  C07D213/61 ,  C07D213/65 ,  C07D213/69 ,  C07D213/70 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D213/80 ,  C07D213/82 ,  C07D213/89 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D451/04 ,  C07D471/06

Abstract: The present invention relates to compounds that bind to chemokine receptors, and having the formula (I) wherein each A, X, Y, R , R and R are substituents. The present invention also relates to methods of using such compounds, such as in treating HIV infection and inflammatory conditions such as rheumatoid arthritis. Furthermore, the present invention relates to methods to elevate progenitor and stem cell counts, as well as methods to elevate white blood cell counts, using such compounds.

Abstract translation: 本发明涉及结合趋化因子受体并具有式（I）的化合物，其中每个A，X，Y，R 1，R 2和R 3是取代基。 本发明还涉及使用这些化合物的方法，例如用于治疗HIV感染和炎性病症如类风湿性关节炎。 此外，本发明涉及提高祖细胞和干细胞计数的方法，以及使用这些化合物提高白细胞计数的方法。

公开(公告)号：WO2009137081A3

公开(公告)日：2009-11-12

申请号：PCT/US2009/002845

申请日：2009-05-07

Applicant: MASSACHUSETTS INSTITUTE OF TECHNOLOGY ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  GENZYME CORPORATION ,  BASTOS, Cecilia ,  BOOKER, Michael, L. ,  CELATKA, Cassandra, A. ,  CLARDY, Jon, C. ,  CORTESE, Joseph ,  PATEL, Vishal, P. ,  SKERLJ, Renato ,  WIEGAND, Roger, C. ,  WIRTH, Dyann, F.

Inventor： BASTOS, Cecilia ,  BOOKER, Michael, L. ,  CELATKA, Cassandra, A. ,  CLARDY, Jon, C. ,  CORTESE, Joseph ,  PATEL, Vishal, P. ,  SKERLJ, Renato ,  WIEGAND, Roger, C. ,  WIRTH, Dyann, F.

IPC: C07D333/38 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  A61K31/4184 ,  A61P33/06

Abstract: Inhibitors of dihydroorotate dehydrogenase (DHODH) for the Plasmodium enzyme have been identified and characterized. The inhibitors have high specificity, submicromolar efficacy against cultured parasite strains, exhibit drug-like properties, and are not overtly cytotoxic.

公开(公告)号：WO2006039250A3

公开(公告)日：2006-10-19

申请号：PCT/US2005034491

申请日：2005-09-26

Applicant: ANORMED INC ,  CRAWFORD JASON B ,  ZHU YONGBAO ,  CHEN GANG ,  BAIRD IAN R ,  SKERLJ RENATO

Inventor： CRAWFORD JASON B ,  ZHU YONGBAO ,  CHEN GANG ,  BAIRD IAN R ,  SKERLJ RENATO

IPC: A61K31/47 ,  C07D215/12

CPC classification number: C07D401/12

Abstract: The present invention relates to chemokine-binding heterocyclic compound salts, methods of use thereof, and methods for preparing the same.

Abstract translation: 本发明涉及趋化因子结合杂环化合物盐，其使用方法及其制备方法。

公开(公告)号：WO2004106493A3

公开(公告)日：2005-08-25

申请号：PCT/US2004015977

申请日：2004-05-21

Applicant: ANORMED INC ,  BRIDGER GARY J ,  KALLER AL ,  HARWIG CURTIS ,  SKERLJ RENATO ,  BOGUCKI DAVID ,  WILSON TREVOR R ,  CRAWFORD JASON ,  MCEACHERN ERNEST J ,  ATSMA BEM ,  NAN SIQIAO ,  ZHOU YUANXI ,  SCHOLS DOMINIQUE ,  SMITH CHRISTOPHER DENNIS ,  DI FLURI MARIA ROSARIA

Inventor： BRIDGER GARY J ,  KALLER AL ,  HARWIG CURTIS ,  SKERLJ RENATO ,  BOGUCKI DAVID ,  WILSON TREVOR R ,  CRAWFORD JASON ,  MCEACHERN ERNEST J ,  ATSMA BEM ,  NAN SIQIAO ,  ZHOU YUANXI ,  SCHOLS DOMINIQUE ,  SMITH CHRISTOPHER DENNIS ,  DI FLURI MARIA ROSARIA

IPC: A01N43/42 ,  A01N43/50 ,  A01N43/52 ,  A01N43/58 ,  A01N43/60 ,  A61K31/415 ,  A61K31/47 ,  A61K31/495 ,  A61K31/50 ,  C07D235/10 ,  C07D235/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D471/06 ,  C07D491/04 ,  C12N20060101

CPC classification number: A61K31/4184 ,  A61K31/415 ,  A61K31/436 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/50 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  C07D235/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D471/06 ,  C07D491/04 ,  C07D491/052

Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infections of target cells by a human immunodeficiency virus (HIV).

Abstract translation: 本发明涉及由三个侧基包围的核心氮原子组成的杂环化合物，其中三个侧基中的两个优选为苯并咪唑基甲基和四氢喹啉基，第三侧基含有N并且任选地含有另外的环。 这些化合物结合趋化因子受体，包括CXCR4和CCR5，并表现出针对人类免疫缺陷病毒（HIV）对靶细胞感染的保护作用。

公开(公告)号：WO2004093817A2

公开(公告)日：2004-11-04

申请号：PCT/US2004/012627

申请日：2004-04-22

Applicant: ANORMED INC. ,  BRIDGER, Gary, J. ,  MCEACHERN, Ernest, J. ,  SKERLJ, Renato ,  SCHOLS, Dominique

Inventor： BRIDGER, Gary, J. ,  MCEACHERN, Ernest, J. ,  SKERLJ, Renato ,  SCHOLS, Dominique

IPC: A61K

CPC classification number: C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: Compounds that interact with the CXCR4 receptor are described. The compounds are useful in treating for Example, HIV infection and inflammatory conditions such as rheumatoid arthritis, as well as asthma or cancer, and are useful in methods to elevate progenitor and stem cell counts as well as methods to elevate white blood cell counts.

Abstract translation: 描述了与CXCR4受体相互作用的化合物。 该化合物可用于治疗实例，HIV感染和炎性病症如类风湿性关节炎，以及哮喘或癌症，并且可用于提高祖细胞和干细胞计数的方法以及升高白细胞计数的方法。

公开(公告)号：WO2003022785A2

公开(公告)日：2003-03-20

申请号：PCT/US2002/029372

申请日：2002-09-12

Applicant: ANORMED INC. ,  MCEACHERN, Ernest, J. ,  BRIDGER, Gary, J. ,  SKUPINSKA, Krystyna, A. ,  SKERLJ, Renato, T.

Inventor： MCEACHERN, Ernest, J. ,  BRIDGER, Gary, J. ,  SKUPINSKA, Krystyna, A. ,  SKERLJ, Renato, T.

IPC: C07C

CPC classification number: C07D217/22 ,  C07D215/06 ,  C07D215/20 ,  C07D215/38 ,  C07D215/40 ,  C07D215/42 ,  C07D215/48 ,  C07D221/04 ,  C07D241/42 ,  C07D307/79 ,  C07D491/04

Abstract: This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)- forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)- enantioner of primary amino-substituted fused bicyclic ring systems.

Abstract translation: 本发明描述了合成和拆分外消旋氨基取代的稠合双环体系的各种方法。 一个方法利用氨基取代的稠合双环芳族环系统的选择性氢化。 另一种方法是通过亚硝化制备外消旋氨基取代的稠合双环体系。 此外，本发明描述了外消旋混合物的酶拆分以产生（R） - 和（S） - 形式的氨基取代的稠合双环，以及外消旋化方法以回收未预期的对映异构体。 本发明进一步提供的是主要氨基取代的稠合双环体系的（R） - 或（S） - 对映体的不对称合成。

公开(公告)号：WO2002034745A1

公开(公告)日：2002-05-02

申请号：PCT/US2001/029590

申请日：2001-09-17

Applicant: ANORMED INC. ,  BRIDGER, Gary ,  SKERLJ, Renato ,  KALLER, Al ,  HARWIG, Curtis ,  BOGUCKI, David ,  WILSON, Trevor, R. ,  CRAWFORD, Jason ,  MCEACHERN, Ernest, J. ,  ATSMA , Bem ,  NAN, Siqiao ,  ZHOU, Yuanxi ,  SCHOLS, Dominique ,  SMITH, Christopher, Dennis ,  DI FLURI, Rosaria, Maria

Inventor： BRIDGER, Gary ,  SKERLJ, Renato ,  KALLER, Al ,  HARWIG, Curtis ,  BOGUCKI, David ,  WILSON, Trevor, R. ,  CRAWFORD, Jason ,  MCEACHERN, Ernest, J. ,  ATSMA , Bem ,  NAN, Siqiao ,  ZHOU, Yuanxi ,  SCHOLS, Dominique ,  SMITH, Christopher, Dennis ,  DI FLURI, Rosaria, Maria

IPC: C07D403/12

CPC classification number: C07D213/81 ,  A61K31/4709 ,  C07D213/38 ,  C07D213/65 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D493/04 ,  Y02A50/411

Abstract: Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.

Abstract translation: 公开了调节趋化因子受体活性的化合物。 这些化合物优选为包含四氢喹啉和苯并咪唑的叔胺。