公开(公告)号：US10532051B2

公开(公告)日：2020-01-14

申请号：US14875506

申请日：2015-10-05

Applicant: ChemoCentryx, Inc.

Inventor： Karen Ebsworth ,  Yu Wang ,  Yibin Zeng ,  Penglie Zhang ,  Joanne Tan

IPC: A61K31/502 ,  A61K31/4412 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/415 ,  A61K31/5377 ,  A61K39/395 ,  C07K16/28 ,  A61P1/00

Abstract: Provided herein are compositions, methods and kits for treating inflammatory bowel disease (IBD) such as Crohn's disease and ulcerative colitis in a mammal in need thereof. The method include administering to a subject with IBD a combination therapy containing a therapeutically effective amount of a chemokine receptor 9 (CCR9) inhibitor compound and a therapeutically effective amount of an anti-α4β7 integrin antibody such as vedolizumab. Also provided herein is a kit containing the CCR9 inhibitor compound and anti-α4β7 integrin antibody.

公开(公告)号：US10364240B2

公开(公告)日：2019-07-30

申请号：US15697414

申请日：2017-09-06

Applicant: ChemoCentryx, Inc.

Inventor： Solomon Ungashe ,  John J. Wright ,  Andrew Pennell ,  Zheng Wei ,  Anita Melikian

IPC: C07D417/12 ,  C07D213/26 ,  C07D213/50 ,  C07D213/52 ,  C07D213/70 ,  C07D213/74 ,  C07D213/84 ,  C07D213/89 ,  C07D241/12 ,  C07D405/12 ,  C07D413/12 ,  A61K31/4409 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D239/26 ,  C07D401/12 ,  C07D409/12

Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

公开(公告)号：US10342781B2

公开(公告)日：2019-07-09

申请号：US15659488

申请日：2017-07-25

Applicant: CHEMOCENTRYX, INC.

Inventor： Xi Chen ,  Dean R. Dragoli ,  Pingchen Fan ,  Juan C. Jaen ,  Yandong Li ,  Jay P. Powers ,  Viengkham Malathong ,  Sreenivas Punna ,  Hiroko Tanaka ,  Penglie Zhang

IPC: A61K45/06 ,  A61K31/437 ,  C07D231/40 ,  C07D233/88 ,  C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196

Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam 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：US10266492B2

公开(公告)日：2019-04-23

申请号：US15659468

申请日：2017-07-25

Applicant: CHEMOCENTRYX, INC.

Inventor： Pingchen Fan ,  Jaroslaw Kalisiak ,  Antoni Krasinski ,  Rebecca M. Lui ,  Jay Powers ,  Sreenivas Punna ,  Hiroko Tanaka ,  Penglie Zhang

IPC: C07D211/60

Abstract: Intermediates and methods are provided for the preparation of selected C5aR antagonist compounds.

公开(公告)号：US09493417B2

公开(公告)日：2016-11-15

申请号：US14832755

申请日：2015-08-21

Applicant: ChemoCentryx, Inc.

Inventor： Joanna Bis ,  David H. Igo

IPC: C07D211/70 ,  C07D213/89 ,  A61K31/4425 ,  A61K45/06

CPC classification number: C07D213/89 ,  A61K31/44 ,  A61K31/4425 ,  A61K45/06 ,  C07B2200/13

Abstract: Disclosed are novel novel polymorphic solvated and desolvated forms of the sodium salt of 4-tert-butyl-N-[chloro-2-(1-oxy-pyridine-4-carbonyl)phenyl]-benzenesulfonamide. One embodiment of the present invention is directed to a crystalline sodium salt of 4-tert-butyl-N-[4-chloro-2-(1-oxy-pyridine-4-carbonyl)-phenyl]benzenesulfonamide (hereinafter “Compound A-1,4-dioxane/water solvate”), wherein the crystalline form is characterized by an X-ray powder diffraction pattern comprising diffraction angles (° 28), when measured using Cu Ku radiation, at about 4.0, 8.1, 10.1, 14.2, 16.2, 18.6, 20.3, 24.7, 25.0, and 26.5.

Abstract translation: 公开了4-叔丁基-N- [氯-2-（1-氧 - 吡啶-4-羰基）苯基] - 苯磺酰胺的钠盐的新型多晶型溶剂化和脱溶剂形式。 本发明的一个实施方案涉及4-叔丁基-N- [4-氯-2-（1-氧 - 吡啶-4-羰基） - 苯基]苯磺酰胺（以下称为“化合物A- 1,4-二恶烷/水溶剂合物“），其中结晶形式的特征在于包括衍射角（°28）的X射线粉末衍射图，当使用Cu Ku辐射测量时，其衍射角约为4.0,8.1,10.1,14.2， 16.2,18.6,20.3,24.7,25.0和26.5。

公开(公告)号：US09394307B2

公开(公告)日：2016-07-19

申请号：US14043602

申请日：2013-10-01

Applicant: ChemoCentryx, Inc.

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

IPC: A01N43/90 ,  A61K31/519 ,  A61K31/52 ,  C07D473/00 ,  C07D471/04 ,  C07D471/12

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。

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：US08835468B2

公开(公告)日：2014-09-16

申请号：US13462393

申请日：2012-05-02

Applicant: Trevor T. Charvat ,  Cheng Hu ,  Anita Melikian ,  Aaron Novack ,  Andrew M. K. Pennell ,  Edward J. Sullivan ,  William D. Thomas ,  Solomon Ungashe ,  Penglie Zhang ,  Jay Powers ,  Sreenivas Punna

Inventor： Trevor T. Charvat ,  Cheng Hu ,  Anita Melikian ,  Aaron Novack ,  Andrew M. K. Pennell ,  Edward J. Sullivan ,  William D. Thomas ,  Solomon Ungashe ,  Penglie Zhang ,  Jay Powers ,  Sreenivas Punna

IPC: A01N43/64 ,  A61K31/41 ,  A61K31/415 ,  A01N43/56

CPC classification number: C07D473/00 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/496 ,  A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/08 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/56 ,  C07D233/61 ,  C07D235/06 ,  C07D235/08 ,  C07D249/06 ,  C07D249/18 ,  C07D401/04 ,  C07D401/14 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C12N2501/999

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

Abstract translation: 提供了作为CCR9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，CCR9的特征性疾病。 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CCR9介导的疾病的方法，以及用于鉴定CCR9拮抗剂的测定中的对照。

公开(公告)号：US20140154179A1

公开(公告)日：2014-06-05

申请号：US14091641

申请日：2013-11-27

Applicant: ChemoCentryx, Inc.

Inventor： Junfa Fan ,  Antoni Krasinski ,  Christopher W. Lange ,  Rebecca M. Lui ,  Jeffrey P. McMahon ,  Jay P. Powers ,  Yibin Zeng ,  Penglie Zhang

IPC: C07D487/04 ,  A61K49/10 ,  A61K51/04

CPC classification number: C07D487/04 ,  A61K51/0459 ,  G01N33/57492 ,  G01N2333/7158

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：US20130237514A1

公开(公告)日：2013-09-12

申请号：US13645921

申请日：2012-10-05

Applicant: CHEMOCENTRYX, INC

Inventor： Trevor T. Charvat ,  Hiufung Chu ,  Antoni Krasinski ,  Christopher W. Lange ,  Manmohan Reddy Leleti ,  Jay P. Powers ,  Sreenivas Punna ,  Timothy J. Sullivan ,  Solomon Ungashe

IPC: C07D207/277 ,  C07D405/04 ,  C07D491/052 ,  C07D413/06 ,  C07D209/52 ,  C07D209/46 ,  C07D401/04 ,  C07D491/048 ,  C07D403/06

CPC classification number: C07D207/277 ,  C07D207/416 ,  C07D209/46 ,  C07D209/52 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D413/06 ,  C07D491/048 ,  C07D491/052 ,  C07D493/04

Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.

Abstract translation: 提供吡咯烷酮甲酰胺化合物，其可用于抑制配体与ChemR23受体的结合。