公开(公告)号：US07727981B2

公开(公告)日：2010-06-01

申请号：US11924480

申请日：2007-10-25

Applicant: Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

Inventor： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

IPC: C07D413/14 ,  A61K31/4439

CPC classification number: A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract translation: 描述了具有抗哺乳动物因子Xa活性的新型苯甲酰胺化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内可用于预防或治疗凝血障碍。

公开(公告)号：US06835739B2

公开(公告)日：2004-12-28

申请号：US10687334

申请日：2003-10-15

Applicant: Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

Inventor： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

IPC: C07D40102

CPC classification number: A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

公开(公告)号：US20040097561A1

公开(公告)日：2004-05-20

申请号：US10687334

申请日：2003-10-15

Applicant: Millennium Pharmaceuticals, Inc.

Inventor： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

IPC: C07D213/72 ,  A61K031/44

CPC classification number: A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract translation: 描述了具有抗哺乳动物因子Xa活性的新型苯甲酰胺化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内可用于预防或治疗凝血障碍。

公开(公告)号：US06376515B2

公开(公告)日：2002-04-23

申请号：US09794225

申请日：2001-02-28

Applicant: Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

Inventor： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

IPC: A61K3144

CPC classification number: A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract translation: 描述了具有抗哺乳动物因子Xa活性的新型苯甲酰胺化合物，包括其药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物在体外或体内可用于预防或治疗凝血障碍。

公开(公告)号：US20180036296A1

公开(公告)日：2018-02-08

申请号：US15466530

申请日：2017-03-22

Applicant: Millennium Pharmaceuticals, Inc.

Inventor： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

IPC: A61K31/44 ,  A61K9/20 ,  A61K9/48 ,  A61K31/616 ,  A61K45/06 ,  C07C237/42 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D249/08 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07D233/56 ,  C07D233/64 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

CPC classification number: A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

公开(公告)号：US20170239257A1

公开(公告)日：2017-08-24

申请号：US15277550

申请日：2016-09-27

Applicant: Los Angeles Biomedical Research Institute at Harbor- UCLA Medical Center

Inventor： Nestor F. Gonzalez-Cadavid ,  Jacob Rajfer

IPC: A61K31/53 ,  A61K31/519 ,  A61K9/00 ,  A61K31/4985

CPC classification number: A61K31/53 ,  A61K9/0053 ,  A61K31/00 ,  A61K31/4985 ,  A61K31/519 ,  A61K48/00 ,  A61K48/005 ,  A61K2201/094 ,  C12N15/86 ,  C12N2710/10343 ,  C12N2830/008 ,  C12N2830/85

Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart. In certain embodiments, the compositions may comprise a PDE-4 inhibitor, a PDE-5 inhibitor, a compound that elevates cGMP and/or PKG, a stimulator of guanylyl cyclase and/or PKG, a combination of a compound that elevates cGMP, PKG or NO with an antioxidant that decreases ROS, or a compound that increases MMP activity.

公开(公告)号：US20160317511A1

公开(公告)日：2016-11-03

申请号：US14742465

申请日：2015-06-17

Applicant: Millennium Pharmaceuticals, Inc.

Inventor： Bing-Yan Zhu ,  Penglie Zhang ,  Lingyan Wang ,  Wenrong Huang ,  Erick A. Goldman ,  Wenhao Li ,  Jingmei Zuckett ,  Yonghong Song ,  Robert M. Scarborough

IPC: A61K31/44 ,  A61K9/48 ,  A61K9/20

CPC classification number: A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

公开(公告)号：US09108922B2

公开(公告)日：2015-08-18

申请号：US14175087

申请日：2014-02-07

Applicant: Millennium Pharmaceuticals, Inc.

Inventor： Bing-Yan Zhu ,  Wenrong Huang

IPC: C07D213/75 ,  A61K31/44 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14 ,  A61K31/616 ,  A61K45/06

CPC classification number: A61K31/44 ,  A61K9/20 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/48 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/616 ,  A61K45/06 ,  A61K2201/094 ,  C07C237/42 ,  C07C255/60 ,  C07C257/18 ,  C07C259/18 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/125 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14

Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.

公开(公告)号：US20140364453A1

公开(公告)日：2014-12-11

申请号：US14296888

申请日：2014-06-05

Applicant: Indiana University Research and Technology Corporation

Inventor： Hiroki Yokota ,  Kazunori Hamamura

IPC: A61K31/4706 ,  A61K31/155

CPC classification number: A61K31/4706 ,  A61K31/155 ,  A61K2201/094 ,  A61K2300/00

Abstract: A method is disclosed for the in vivo treatment of a breast cancer tumor utilizing a therapeutically effective amount of an agent that inactivates the Rac1 GTPase and results in a reduction in cancer cell invasion, reduced cancer cell motility, and reduced volume and weight of the tumor. Agents that can be used in this treatment include salubrinal, guanabenz, and combinations thereof. The agents additionally have proven useful in reducing the development of osteoclastogenesis and reducing bone metastasis.

Abstract translation: 公开了一种用于体内治疗乳腺癌肿瘤的方法，其利用治疗有效量的灭活Rac1GTP酶的试剂，并导致癌细胞侵袭减少，癌细胞运动减少，肿瘤体积和重量减少 。 可用于该治疗的药剂包括salubrinal，guanabenz及其组合。 该试剂另外被证明可用于减少破骨细胞发生和减少骨转移的发展。

公开(公告)号：US20140364396A1

公开(公告)日：2014-12-11

申请号：US14366949

申请日：2012-12-21

Applicant: Ares Trading S.A.

Inventor： Dominique Swinnen ,  Stefano Crosignani ,  Jeyaprakashnarayanan Seenisamy ,  Federica Morandi

IPC: C07F5/02 ,  A61K31/69

CPC classification number: C07F5/025 ,  A61K31/69 ,  A61K45/06 ,  A61K2201/094 ,  C07F5/02

Abstract: The present invention provides compounds of Formula (I) as inhibitors of LMP7 for the treatment of autoimmune and inflammatory diseases.

Abstract translation: 本发明提供作为LMP7抑制剂的式（I）化合物用于治疗自身免疫性和炎性疾病。