公开(公告)号：US08093247B2

公开(公告)日：2012-01-10

申请号：US12582001

申请日：2009-10-20

Applicant: Solomon Ungashe ,  Zheng Wei ,  Arindrajit Basak ,  Trevor T. Charvat ,  Wei Chen ,  Jeff Jin ,  Jimmie Moore ,  Yibin Zeng ,  Sreenivas Punna ,  Daniel Dairaghi ,  Derek Hansen ,  Andrew M. K. Pennell ,  John J. Wright

Inventor： Solomon Ungashe ,  Zheng Wei ,  Arindrajit Basak ,  Trevor T. Charvat ,  Wei Chen ,  Jeff Jin ,  Jimmie Moore ,  Yibin Zeng ,  Sreenivas Punna ,  Daniel Dairaghi ,  Derek Hansen ,  Andrew M. K. Pennell ,  John J. Wright

IPC: A61K31/50 ,  A61K31/44

CPC classification number: A61K31/444 ,  A61K31/437 ,  A61K31/4439 ,  A61K45/06 ,  C07C311/21 ,  C07D213/75 ,  C07D241/22 ,  C07D401/06 ,  C07D401/10 ,  C07D407/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12 ,  C07D471/04 ,  C07D498/04

Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Abstract translation: 提供了作为CCR2受体的有效拮抗剂的化合物。 动物实验表明，这些化合物可用于治疗炎症，CCR2的标志性疾病。 化合物通常为芳基磺酰胺衍生物，并且可用于药物组合物，用于治疗CCR2介导的疾病的方法，以及用于鉴定CCR2拮抗剂的测定中的对照。

公开(公告)号：US20100311753A1

公开(公告)日：2010-12-09

申请号：US12823039

申请日：2010-06-24

Applicant: Pingchen Fan ,  Kevin Lloyd Greenman ,  Manmohan Reddy Leleti ,  Yandong Li ,  Jay P. Powers ,  Hiroko Tanaka ,  Ju Yang ,  Yibin Zeng

Inventor： Pingchen Fan ,  Kevin Lloyd Greenman ,  Manmohan Reddy Leleti ,  Yandong Li ,  Jay P. Powers ,  Hiroko Tanaka ,  Ju Yang ,  Yibin Zeng

IPC: A61K31/5377 ,  C07D211/32 ,  C07D401/06 ,  C07D401/12 ,  C07D413/14 ,  A61K31/451 ,  A61K31/4545 ,  A61K31/454 ,  A61P9/00 ,  A61P9/10 ,  A61P7/02 ,  A61P25/00 ,  A61P37/00 ,  A61P29/00 ,  A61P3/10 ,  A61P25/28

CPC classification number: A61K31/5377 ,  A61K31/445 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  C07D211/60 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/10 ,  C07D413/12 ,  C07D413/14

Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

公开(公告)号：US20100152186A1

公开(公告)日：2010-06-17

申请号：US12708900

申请日：2010-02-19

Applicant: Trevor T. Charvat ,  Cheng Hu ,  Jeff Jin ,  Yandong Li ,  Anita Melikian ,  Andrew M.K. Pennell ,  Sreenivas Punna ,  Solomon Ungashe ,  Yibin Zeng

Inventor： Trevor T. Charvat ,  Cheng Hu ,  Jeff Jin ,  Yandong Li ,  Anita Melikian ,  Andrew M.K. Pennell ,  Sreenivas Punna ,  Solomon Ungashe ,  Yibin Zeng

IPC: C07D401/04 ,  A61K31/4439 ,  C07D401/14 ,  A61K31/454 ,  A61K31/444 ,  C07D413/14 ,  A61K31/5377 ,  A61P9/10 ,  A61P21/00 ,  A61P1/00 ,  A61P13/12 ,  A61P19/02 ,  A61P3/04 ,  A61P11/00 ,  A61P35/00 ,  A61K31/437 ,  C07D487/04

CPC classification number: C07D401/14

Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.

Abstract translation: 提供了作为CCR2或CCR9受体的有效拮抗剂的化合物。 动物试验表明，这些化合物可用于治疗炎症，CCR2和CCR9的标志性疾病。 化合物通常为芳基磺酰胺衍生物，并且可用于药物组合物，用于治疗CCR2介导的疾病，CCR9介导的疾病的方法，作为用于鉴定CCR2拮抗剂的测定中的对照和用于鉴定CCR9拮抗剂的测定中的对照 。

公开(公告)号：US20100056509A1

公开(公告)日：2010-03-04

申请号：US12582001

申请日：2009-10-20

Applicant: Solomon Ungashe ,  Zheng Wei ,  Arindrajit Basak ,  Trevor T. Charvat ,  Wei Chen ,  Jeff Jin ,  Jimmie Moore ,  Yibin Zeng ,  Sreenivas Punna ,  Daniel Dairaghi ,  Derek Hansen ,  Andrew M.K. Pennell ,  John J. Wright

Inventor： Solomon Ungashe ,  Zheng Wei ,  Arindrajit Basak ,  Trevor T. Charvat ,  Wei Chen ,  Jeff Jin ,  Jimmie Moore ,  Yibin Zeng ,  Sreenivas Punna ,  Daniel Dairaghi ,  Derek Hansen ,  Andrew M.K. Pennell ,  John J. Wright

IPC: A61K31/5377 ,  C07D471/02 ,  C07D401/06 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506 ,  C07D413/06 ,  C07D498/02

CPC classification number: A61K31/444 ,  A61K31/437 ,  A61K31/4439 ,  A61K45/06 ,  C07C311/21 ,  C07D213/75 ,  C07D241/22 ,  C07D401/06 ,  C07D401/10 ,  C07D407/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12 ,  C07D471/04 ,  C07D498/04

Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.

Abstract translation: 提供了作为CCR2受体的有效拮抗剂的化合物。 动物实验表明，这些化合物可用于治疗炎症，CCR2的标志性疾病。 化合物通常为芳基磺酰胺衍生物，并且可用于药物组合物，用于治疗CCR2介导的疾病的方法，以及用于鉴定CCR2拮抗剂的测定中的对照。

公开(公告)号：US08445518B2

公开(公告)日：2013-05-21

申请号：US12708900

申请日：2010-02-19

Applicant: Trevor T. Charvat ,  Cheng Hu ,  Jeff Jin ,  Yandong Li ,  Anita Melikian ,  Andrew M. K. Pennell ,  Sreenivas Punna ,  Solomon Ungashe ,  Yibin Zeng

Inventor： Trevor T. Charvat ,  Cheng Hu ,  Jeff Jin ,  Yandong Li ,  Anita Melikian ,  Andrew M. K. Pennell ,  Sreenivas Punna ,  Solomon Ungashe ,  Yibin Zeng

IPC: A61K31/4439 ,  C07D401/00

CPC classification number: C07D401/14

Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.

Abstract translation: 提供了作为CCR2或CCR9受体的有效拮抗剂的化合物。 动物试验表明，这些化合物可用于治疗炎症，CCR2和CCR9的标志性疾病。 化合物通常为芳基磺酰胺衍生物，并且可用于药物组合物，用于治疗CCR2介导的疾病，CCR9介导的疾病的方法，作为用于鉴定CCR2拮抗剂的测定中的对照和用于鉴定CCR9拮抗剂的测定中的对照 。

公开(公告)号：US09126939B2

公开(公告)日：2015-09-08

申请号：US13806339

申请日：2011-06-24

Applicant: Pingchen Fan ,  Kevin Lloyd Greenman ,  Manmohan Reddy Leleti ,  Yandong Li ,  Jay Powers ,  Hiroko Tanaka ,  Ju Yang ,  Yibin Zeng

Inventor： Pingchen Fan ,  Kevin Lloyd Greenman ,  Manmohan Reddy Leleti ,  Yandong Li ,  Jay Powers ,  Hiroko Tanaka ,  Ju Yang ,  Yibin Zeng

IPC: A61K31/445 ,  C07D211/60 ,  C07D401/14 ,  C07D413/14 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5377 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D405/10 ,  C07D413/12 ,  C07D405/12

CPC classification number: C07D211/60 ,  A61K31/445 ,  A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5377 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/10 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14

Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

Abstract translation: 提供了作为C5a受体调节剂的化合物。 化合物是取代的哌啶并且可用于药物组合物，用于治疗涉及C5a受体的病理活化的疾病和病症的方法。

公开(公告)号：US08853202B2

公开(公告)日：2014-10-07

申请号：US12778913

申请日：2010-05-12

Applicant: Xi Chen ,  Dean R. Dragoli ,  Pingchen Fan ,  Mark M. Gleason ,  Juan C. Jaen ,  Lianfa Li ,  Jeffrey P. McMahon ,  Jay Powers ,  Yibin Zeng ,  Penglie Zhang ,  Junfa Fan

Inventor： Xi Chen ,  Dean R. Dragoli ,  Pingchen Fan ,  Mark M. Gleason ,  Juan C. Jaen ,  Lianfa Li ,  Jeffrey P. McMahon ,  Jay Powers ,  Yibin Zeng ,  Penglie Zhang ,  Junfa Fan

IPC: A61K31/497 ,  A61P35/00 ,  A61P9/10 ,  C07D401/14 ,  C07D417/14 ,  C07D403/14

CPC classification number: C07D401/14 ,  C07D403/14 ,  C07D417/14

Abstract: Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.

Abstract translation: 提供具有式I化合物或其药学上可接受的盐，水合物或N-氧化物，并且可用于结合CXCR7，并且治疗至少部分依赖于CXCR7活性的疾病。 因此，本发明还提供含有一种或多种上述化合物与药学上可接受的赋形剂混合的组合物。

公开(公告)号：US08343975B2

公开(公告)日：2013-01-01

申请号：US12557428

申请日：2009-09-10

Applicant: Penglie Zhang ,  Yibin Zeng

Inventor： Penglie Zhang ,  Yibin Zeng

IPC: A61K31/497 ,  C07D487/00

CPC classification number: C07D487/04

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 4-amino-3-imidazoyl-pyrazolo[3,4-d]pyrimidine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.

公开(公告)号：US20120165303A1

公开(公告)日：2012-06-28

申请号：US13411171

申请日：2012-03-02

Applicant: Trevor T. Charvat ,  Cheng Hu ,  Anita Melikian ,  Aaron Novack ,  Andrew M.K. Pennell ,  Sreenivas Punna ,  Edward J. Sullivan ,  Xuefei Tan ,  William D. Thomas ,  Solomon Ungashe ,  Yibin Zeng

Inventor： Trevor T. Charvat ,  Cheng Hu ,  Anita Melikian ,  Aaron Novack ,  Andrew M.K. Pennell ,  Sreenivas Punna ,  Edward J. Sullivan ,  Xuefei Tan ,  William D. Thomas ,  Solomon Ungashe ,  Yibin Zeng

IPC: A61K31/4196 ,  C07D405/04 ,  C07D403/04 ,  C07D401/04 ,  A61K31/454 ,  C07D413/04 ,  C07D413/06 ,  A61K31/5377 ,  A61K31/497 ,  A61P9/10 ,  A61P9/00 ,  A61P25/00 ,  A61P1/00 ,  A61P13/12 ,  A61P29/00 ,  A61P3/04 ,  A61P3/10 ,  A61P11/00 ,  A61P37/06 ,  A61P35/00 ,  A61K31/4439 ,  C07D403/06 ,  C07D487/04 ,  A61K31/519 ,  C07D249/08

CPC classification number: C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D413/04

Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.

Abstract translation: 提供了作为CCR2或CCR9受体的有效拮抗剂的化合物。 动物试验表明，这些化合物可用于治疗炎症，CCR2和CCR9的标志性疾病。 化合物通常为芳基磺酰胺衍生物，并且可用于药物组合物，用于治疗CCR2介导的疾病，CCR9介导的疾病的方法，作为用于鉴定CCR2拮抗剂的测定中的对照和用于鉴定CCR9拮抗剂的测定中的对照 。

公开(公告)号：US07884110B2

公开(公告)日：2011-02-08

申请号：US12171782

申请日：2008-07-11

Applicant: Antoni Krasinski ,  Sreenivas Punna ,  Solomon Ungashe ,  Qiang Wang ,  Yibin Zeng

Inventor： Antoni Krasinski ,  Sreenivas Punna ,  Solomon Ungashe ,  Qiang Wang ,  Yibin Zeng

IPC: A01N43/90 ,  A61K31/52 ,  A61K31/519 ,  C07D473/00 ,  C07D487/00

CPC classification number: C07D487/04 ,  C07D213/79 ,  C07D213/81 ,  C07D213/84 ,  C07D471/04 ,  C07D471/12 ,  C07D473/00

Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.

Abstract translation: 提供了作为CCR2受体的有效拮抗剂的化合物。 化合物通常为芳基磺酰胺衍生物，并且可用于药物组合物，用于治疗CCR2介导的疾病的方法和用于鉴定CCR2拮抗剂的测定中的对照。