公开(公告)号：US07834143B2

公开(公告)日：2010-11-16

申请号：US11827396

申请日：2007-07-11

Applicant: Johan Sundelin ,  Robert M. Scarborough

Inventor： Johan Sundelin ,  Robert M. Scarborough

IPC: C07K7/00 ,  C07K7/06 ,  C07K7/08 ,  C07K14/705 ,  C07K14/47

CPC classification number: C07K7/06 ,  A61K38/00 ,  A61K48/00 ,  C07K7/08 ,  C07K14/705 ,  C07K14/723 ,  G01N2333/726 ,  G01N2500/00

Abstract: Nucleic acid molecules encoding the C140 cell surface receptor have been cloned and sequenced. The availability of C140 receptor DNA permits the recombinant production of the C140 receptor which can be produced on the surface of a cell, including an oocyte. The nucleic acid molecules are useful in an assay for detecting a substance which affects C140 receptor activity, either receptor agonists or antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in such assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with one or more antigenic epitopes of the C140 receptor.

Abstract translation: 编码C140细胞表面受体的核酸分子已被克隆并测序。 C140受体DNA的可用性允许重组产生可在细胞表面（包括卵母细胞）上产生的C140受体。 核酸分子可用于检测影响C140受体活性的物质，即受体激动剂或拮抗剂。 此外，阐明C140受体的结构允许设计可用于此类测定中的激动剂和拮抗剂化合物。 C140受体的可用性还允许产生与C140受体的一个或多个抗原表位特异性免疫反应的抗体。

公开(公告)号：US20100249117A1

公开(公告)日：2010-09-30

申请号：US12777956

申请日：2010-05-11

Applicant: Yonghong SONG ,  Zhaozhong J. JIA ,  Anjali PANDEY ,  Robert M. SCARBOROUGH ,  Carroll SCARBOROUGH

Inventor： Yonghong SONG ,  Zhaozhong J. JIA ,  Anjali PANDEY ,  Robert M. SCARBOROUGH ,  Carroll SCARBOROUGH

IPC: A61K31/541 ,  C07D401/14 ,  A61K31/4439 ,  C07D413/14 ,  A61K31/5377 ,  C07D241/18 ,  A61K31/497 ,  C07D403/14 ,  A61K31/501 ,  C07D279/12 ,  C07D239/10 ,  A61K31/513 ,  C07D233/64 ,  A61K31/4178 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/444 ,  A61P9/00 ,  A01N1/02

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

Abstract: The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.

Abstract translation: 本发明涉及作为因子Xa抑制剂的式（I）化合物及其药学上可接受的盐，酯和前药。 本发明还涉及用于制备这种化合物的中间体，含有这种化合物的药物组合物，预防或治疗许多不希望的血栓形成特征的病症的方法和抑制血液样品凝固的方法。

公开(公告)号：US20100248380A1

公开(公告)日：2010-09-30

申请号：US12723250

申请日：2010-03-12

Applicant: Richard D. Gless, JR. ,  Rebecca Cosford ,  Tad Dean ,  Michael Horton ,  Dean Marbury ,  Malcolm Montgomery ,  Robert M. Scarborough

Inventor： Richard D. Gless, JR. ,  Rebecca Cosford ,  Tad Dean ,  Michael Horton ,  Dean Marbury ,  Malcolm Montgomery ,  Robert M. Scarborough

IPC: G01N30/72

CPC classification number: G01N30/88 ,  G01N2030/884 ,  Y10T436/17

Abstract: Disclosed herein are the methods and assays for quantitative determination of acetamide in a composition of a sample.

Abstract translation: 本文公开了在样品组合物中定量测定乙酰胺的方法和测定法。

公开(公告)号：US07709640B2

公开(公告)日：2010-05-04

申请号：US11313289

申请日：2005-12-19

Applicant: James Kanter ,  Anjali Pandey ,  James Robinson ,  Robert M. Scarborough

Inventor： James Kanter ,  Anjali Pandey ,  James Robinson ,  Robert M. Scarborough

IPC: C07D295/182

CPC classification number: C07D239/94

Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

Abstract translation: 本发明提供含氮杂环化合物及其药学上可接受的盐及其制备方法。 这些化合物对抑制这种激酶活性的激酶的磷酸化具有抑制活性。 本发明还提供了可用于该方法的中间体化合物，以及通过该方法生产的最终产物及其盐或前药。 本发明进一步提供了通过抑制激酶的磷酸化来抑制哺乳动物激酶和治疗疾病状态的方法，包括向有需要的患者施用有效量的本发明化合物。

公开(公告)号：US20090176780A1

公开(公告)日：2009-07-09

申请号：US11959341

申请日：2007-12-18

Applicant: Anjali Pandey ,  Robert M. Scarborough ,  Kenji Matsuno ,  Michio Ichimura ,  Yuji Nomoto ,  Shinichi Ide ,  Eiji Tsukuda ,  Nee Junko Irie Junko Sasaki ,  Shoji Oda

Inventor： Anjali Pandey ,  Robert M. Scarborough ,  Kenji Matsuno ,  Michio Ichimura ,  Yuji Nomoto ,  Shinichi Ide ,  Eiji Tsukuda ,  Nee Junko Irie Junko Sasaki ,  Shoji Oda

IPC: A61K31/5377 ,  A61K31/517

CPC classification number: C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

Abstract translation: 本发明涉及对抑制这种激酶活性的激酶磷酸化具有抑制活性的含氮杂环化合物及其药学上可接受的盐。 本发明还涉及通过抑制激酶的磷酸化来抑制哺乳动物的激酶和治疗疾病状态的方法。 在一个特定方面，本发明提供了抑制PDGF受体的磷酸化以阻止异常细胞生长和细胞游动的含氮杂环化合物及其药学上可接受的盐，以及预防或治疗细胞增殖性疾病如动脉硬化，血管 重建，癌症和肾小球硬化症。

公开(公告)号：US20090131411A1

公开(公告)日：2009-05-21

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: A61K31/4439 ,  A61P7/00 ,  C07D409/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/506 ,  A61K31/4545

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：US07351792B2

公开(公告)日：2008-04-01

申请号：US10643627

申请日：2003-08-19

Applicant: Johan Sundelin ,  Robert M. Scarborough

Inventor： Johan Sundelin ,  Robert M. Scarborough

IPC: C07K7/08 ,  C07K7/00 ,  C07K7/06 ,  C07K14/705 ,  C07K14/435 ,  A61K38/00

CPC classification number: C07K7/06 ,  A61K38/00 ,  A61K48/00 ,  C07K7/08 ,  C07K14/705 ,  C07K14/723 ,  G01N2333/726 ,  G01N2500/00

Abstract: Nucleic acid molecules encoding the C140 cell surface receptor have been cloned and sequenced. The availability of C140 receptor DNA permits the recombinant production of the C140 receptor which can be produced on the surface of a cell, including an oocyte. The nucleic acid molecules are useful in an assay for detecting a substance which affects C140 receptor activity, either receptor agonists or antagonists. Further, the elucidation of the structure of the C140 receptor permits the design of agonist and antagonist compounds which are useful in such assays. The availability of the C140 receptor also permits production of antibodies specifically immunoreactive with one or more antigenic epitopes of the C140 receptor.

Abstract translation: 编码C140细胞表面受体的核酸分子已被克隆并测序。 C140受体DNA的可用性允许重组产生可在细胞表面（包括卵母细胞）上产生的C140受体。 核酸分子可用于检测影响C140受体活性的物质，即受体激动剂或拮抗剂。 此外，阐明C140受体的结构允许设计可用于此类测定中的激动剂和拮抗剂化合物。 C140受体的可用性还允许产生与C140受体的一个或多个抗原表位特异性免疫反应的抗体。

公开(公告)号：US07205296B2

公开(公告)日：2007-04-17

申请号：US11236051

申请日：2005-09-26

Applicant: Robert M. Scarborough ,  Meenakshi S. Venkatraman ,  Xiaoming Zhang ,  Anjali Pandey

Inventor： Robert M. Scarborough ,  Meenakshi S. Venkatraman ,  Xiaoming Zhang ,  Anjali Pandey

IPC: C07D409/12 ,  C07D409/14 ,  A61K31/538

CPC classification number: C07D413/12 ,  C07D413/14

Abstract: Substituted benzoxazin-4(3H)-ones are provided which are useful for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.

Abstract translation: 提供了取代的苯并恶嗪-4（3H） - 酮，其可用于治疗患者的血栓形成和降低患者二次缺血事件的可能性和/或严重程度。

公开(公告)号：US07115741B2

公开(公告)日：2006-10-03

申请号：US10237153

申请日：2002-09-06

Applicant: Daniel E. Levy ,  Mark S. Smyth ,  Robert M. Scarborough

Inventor： Daniel E. Levy ,  Mark S. Smyth ,  Robert M. Scarborough

IPC: C07D495/04 ,  A61K31/519 ,  A61P7/02

CPC classification number: C07D495/04 ,  C07D473/34

Abstract: Compounds of formula II are provided: wherein A, J and L are independently a direct link or a divalent linking group. The compounds are useful in the treatment of thrombosis.

Abstract translation: 提供式II化合物：其中A，J和L独立地是直链或二价连接基团。 该化合物可用于治疗血栓形成。

公开(公告)号：US06951937B2

公开(公告)日：2005-10-04

申请号：US10041160

申请日：2002-01-08

Applicant: James Kanter ,  Anjali Pandey ,  James Robinson ,  Robert M. Scarborough

Inventor： James Kanter ,  Anjali Pandey ,  James Robinson ,  Robert M. Scarborough

IPC: C07D239/86 ,  A61K31/517 ,  A61K31/5377 ,  A61P9/10 ,  A61P13/12 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07B61/00 ,  C07D239/94 ,  A61K31/495 ,  C07D487/00 ,  C07D487/04

CPC classification number: C07D239/94

Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

Abstract translation: 本发明提供了含氮杂环化合物及其药学上可接受的盐及其制备方法。 这些化合物对抑制这种激酶活性的激酶的磷酸化具有抑制活性。 本发明还提供了可用于该方法的中间体化合物，以及通过该方法生产的最终产物及其盐或前药。 本发明进一步提供了通过抑制激酶的磷酸化来抑制哺乳动物激酶和治疗疾病状态的方法，包括向有需要的患者施用有效量的本发明化合物。