公开(公告)号：JP2003159088A

公开(公告)日：2003-06-03

申请号：JP2002259364

申请日：2002-09-04

Applicant: UNIV CALIFORNIA ,  COR THERAPEUTICS INC

Inventor： COUGHLIN SHAUN R ,  SCARBOROUGH ROBERT M

IPC: A61K38/00 ,  A61K39/00 ,  A61K39/395 ,  A61K49/00 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07K7/02 ,  C07K7/06 ,  C07K14/705 ,  C07K16/00 ,  C07K16/28 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N9/74 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12P21/08 ,  C12R1/19 ,  G01N33/53

Abstract: PROBLEM TO BE SOLVED: To provide materials involved in the control of the circulatory system, more specifically, to provide a recombinant material useful for the production of a thrombin receptor, to provide use of the receptor as a diagnostic tool, and to provide a therapeutic agent which either stimulates or blocks thrombin receptor activation and diagnostic compositions relevant to the receptor. SOLUTION: The materials include a mutant thrombin, a DNA molecule, and a recombinant host cell; wherein the mutant thrombin, producible in a recombinant way, is such that the 57- and/or 99- and/or 205-position(s) is (are) different from that(those) in a wild-type thrombin b-chain, the DNA molecule has an expression system capable of producing the thrombin in a host when transformed to the recombinant host and includes a DNA sequence encoding the thrombin linked agonistically to an abnormal regulatory sequence so that the expression system is operable in the host, and the recombinant host cell is subject to transformation by the expression system. COPYRIGHT: (C)2003,JPO

公开(公告)号：JP2002234899A

公开(公告)日：2002-08-23

申请号：JP2001395485

申请日：2001-12-26

Applicant: COR THERAPEUTICS INC

Inventor： DAVID WOLF

IPC: C12N15/09 ,  A61K38/43 ,  A61P7/00 ,  A61P9/08 ,  A61P9/10 ,  C07K14/745

Abstract: PROBLEM TO BE SOLVED: To provide another method that increases the specificity of blocking the formation of active prothrombinase complex and can prolong the duration time of this action. SOLUTION: The objective medicine is the factor Xa of the blood factor that is modified so that the half-life may be transitorily prolonged in the serum and the modified blood factor gives the activated form of the blood factor in the presence of serum. The factor Xa that is the blood factor modified so that the half-life thereof may be prolonged in the serum is mixed with a pharmaceutically acceptable excipient and is used for treating hemophilia wherein the activated form of the blood factor is produced in the presence of serum.

公开(公告)号：JP2002136296A

公开(公告)日：2002-05-14

申请号：JP2001269587

申请日：2001-09-05

Applicant: COR THERAPEUTICS INC

Inventor： SCARBOROUGH ROBERT M

IPC: A61K38/00 ,  A61K35/58 ,  A61P7/02 ,  C07K1/00 ,  C07K14/435 ,  C07K14/46 ,  C07K14/75 ,  C07K16/00 ,  C07K16/18 ,  C12N1/15 ,  C12N1/19 ,  C12N1/21 ,  C12N5/10 ,  C12N15/09 ,  C12P21/02 ,  C12R1/91

Abstract: PROBLEM TO BE SOLVED: To provide another method of antithrombosis treatment by specifically inhibiting the bonding of vWF to a GPIb-IX complex containing platelets. SOLUTION: A DNA molecule composition comprising DNA molecules each containing a sequence encoding a platelet anti-adhesive peptide obtained from snake venoms selected from the following group; Agkistrodon, Bitis, Bothrops, Cerastes, Crotalus, C, Echis carinatus sochurecki, Eristicophis macmahoni, Pseudocerastes persicus, Sistrurus, Trimeresurus, and Vipera.

公开(公告)号：JP2000355600A

公开(公告)日：2000-12-26

申请号：JP2000126152

申请日：2000-04-26

Applicant: COR THERAPEUTICS INC

Inventor： RAMAKRISHNAN VANITHA ,  ESCOBEDO MARIA A ,  FRETTO LARRY J

IPC: A61K39/395 ,  A61K9/20 ,  A61K38/00 ,  A61K48/00 ,  A61P9/00 ,  A61P9/08 ,  A61P35/00 ,  A61P43/00 ,  C07K7/08 ,  C07K14/705 ,  C07K14/71 ,  C07K16/00 ,  C07K16/28 ,  C12N5/18 ,  C12N15/09 ,  C12N15/13 ,  C12P21/02 ,  C12P21/08 ,  G01N33/53 ,  G01N33/531 ,  G01N33/566 ,  G01N33/577

Abstract: PROBLEM TO BE SOLVED: To obtain an antibody capable of inhibiting the PDGF(platelet derived growth factor) BB lag phase of cells expressing human β-PDGF in a defined concentration to a higher extent than a specific value and useful e.g. for the therapy and diagnosis of adult dyspnea syndrome-related pulmonary fibrosis or the like. SOLUTION: This antibody can specifically bind to a β-PDGF receptor not existing in the fifth extracellular Ig-like domain and inhibits the PDGF BB lag phase of cells expressing β-PDGF in an antibody concentration of 10 μg/mL to an extent of >80%. The antibody preferably inhibits the binding of the PDGF BB to cells expressing a β-PDGF receptor or binds to the extracellular Ig-like domain of a β-PDGF receptor. A composition comprising the antibody and a medicinally permissible excipient preferably is prepared. The daily dosage level of the antibody preferably is from 0.1 mg/kg to 10.0 mg/kg.

公开(公告)号：JP2000355548A

公开(公告)日：2000-12-26

申请号：JP2000126131

申请日：2000-04-26

Applicant: COR THERAPEUTICS INC

Inventor： RAMAKRISHNAN VANITHA ,  ESCOBEDO MARIA A ,  FRETTO LARRY J

IPC: A61K39/395 ,  A61K9/20 ,  A61K38/00 ,  A61K48/00 ,  A61P9/00 ,  A61P9/08 ,  A61P35/00 ,  A61P43/00 ,  C07K7/08 ,  C07K14/705 ,  C07K14/71 ,  C07K16/00 ,  C07K16/28 ,  C12N5/18 ,  C12N15/09 ,  C12N15/13 ,  C12P21/02 ,  C12P21/08 ,  G01N33/53 ,  G01N33/531 ,  G01N33/566 ,  G01N33/577

Abstract: PROBLEM TO BE SOLVED: To obtain the subject composition useful for the treatments of restenosis, adult respiratory distress syndrome-related fibroid lung and the like by including an antibody specifically bindable to a specific growth factor receptor so as to be capable of specifically inhibiting the receptor's activation. SOLUTION: This composition is obtained by including an anti-platelet-derived growth factor(PDGF) receptor antibody at effective levels. This antibody is preferably a monoclonal antibody, preferably anti-PDGF-β-receptor antibody. The above composition is preferably a medicinal composition to inhibit the proliferation of smooth muscle cells at the lesion sites of blood vessel and- preferably comprises enough quantity of the anti-growth factor receptor antibody to inhibit mitosis induction and/or transfer of smooth muscle cells of blood vessel at the lesion sites, and also preferably the above antibody is selected from anti-PDGF-βreceptor antibodies. In the above composition, an aqueous carrier, conventional nontoxic solid carrier or the like can be used.

公开(公告)号：WO02070707A2

公开(公告)日：2002-09-12

申请号：PCT/US0149168

申请日：2001-12-18

Applicant: CURAGEN CORP ,  COR THERAPEUTICS INC ,  PADIGARU MURALIDHARA ,  GERLACH VALERIE L ,  SMITHSON GLENNDA ,  STONE DAVID ,  BIN-YANG RUEY ,  CONLEY PAMELA ,  HART MATTHEW ,  TOMLINSON JAMES E ,  TOPPER JAMES N ,  KEKUDA RAMESH ,  CASMAN STACIE J ,  EDINGER SCHLOMIT ,  MACDOUGALL JOHN R

Inventor： PADIGARU MURALIDHARA ,  GERLACH VALERIE L ,  SMITHSON GLENNDA ,  STONE DAVID ,  BIN-YANG RUEY ,  CONLEY PAMELA ,  HART MATTHEW ,  TOMLINSON JAMES E ,  TOPPER JAMES N ,  KEKUDA RAMESH ,  CASMAN STACIE J ,  EDINGER SCHLOMIT ,  MACDOUGALL JOHN R

IPC: A61K38/00 ,  C07K14/705 ,  C12N15/12 ,  A61K31/7088 ,  A61K38/17 ,  A61K39/395 ,  C07K16/28 ,  C12N15/63 ,  C12Q1/68 ,  G01N33/50 ,  G01N33/53

CPC classification number: C07K14/705 ,  A61K38/00 ,  A61K2039/505

Abstract: Disclosed herein are nucleic acid sequences that encode G-coupled protein-receptor related polypeptides. Also disclosed are polypeptides encoded by these nucleic acid sequences, and antibodies, which immunospecifically-bind to the polypeptide, as well as derivatives, variants, mutants, or fragments of the aforementioned polypeptide, polynucleotide, or antibody. The invention further discloses therapeutic, diagnostic and research methods for diagnosis, treatment, and prevention of disorders involving any one of these novel human nucleic acids and proteins.

Abstract translation: 本文公开了编码G偶联蛋白 - 受体相关多肽的核酸序列。 还公开了由这些核酸序列编码的多肽，以及免疫特异性结合多肽的抗体以及上述多肽，多核苷酸或抗体的衍生物，变体，突变体或片段。 本发明还公开了用于诊断，治疗和预防与这些新型人核酸和蛋白质中的任一种相关的病症的治疗，诊断和研究方法。

公开(公告)号：WO0236587A3

公开(公告)日：2002-08-22

申请号：PCT/US0145400

申请日：2001-11-01

Applicant: COR THERAPEUTICS INC ,  KANTER JAMES ,  PANDEY ANJALI ,  ROBINSON JAMES ,  SCARBOROUGH ROBERT M

Inventor： KANTER JAMES ,  PANDEY ANJALI ,  ROBINSON JAMES ,  SCARBOROUGH ROBERT M

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

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 slats 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，以及由该方法生产的最终产物及其板条或前药。 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：WO0164642A3

公开(公告)日：2002-05-02

申请号：PCT/US0106247

申请日：2001-02-28

Applicant: COR THERAPEUTICS INC ,  ZHU BING YAN ,  ZHANG PENGLIE ,  WANG LINGYAN ,  HUANG WENRONG ,  GOLDMAN ERICK ,  LI WENHAO ,  ZUCKETT JINGMEI ,  SONG YONGHONG ,  SCARBOROUGH ROBERT

Inventor： ZHU BING-YAN ,  ZHANG PENGLIE ,  WANG LINGYAN ,  HUANG WENRONG ,  GOLDMAN ERICK ,  LI WENHAO ,  ZUCKETT JINGMEI ,  SONG YONGHONG ,  SCARBOROUGH ROBERT

IPC: A61K31/443 ,  A61K31/444 ,  A61P7/02 ,  C07C311/16 ,  C07C311/46 ,  C07C317/40 ,  C07C317/44 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D217/22 ,  C07D333/38 ,  C07D401/12 ,  C07D409/12 ,  C07D409/14 ,  C07D521/00 ,  A61K31/18 ,  A61K31/44 ,  C07C257/18 ,  C07D203/18 ,  C07D205/04 ,  C07D213/79 ,  C07D213/80 ,  C07D231/40 ,  C07D233/26 ,  C07D295/18 ,  C07D317/44 ,  C07D401/14 ,  C07D403/12

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: Benzamide compounds of formula A-Q-D-E-G-J-X, where the variables are as defined in the claims, 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: 描述式A-Q-D-E-G-J-X的苯甲酰胺化合物，其中变量如权利要求中所定义，包括其对哺乳动物因子Xa具有活性的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：WO0192250A3

公开(公告)日：2002-04-25

申请号：PCT/US0117667

申请日：2001-06-01

Applicant: KANTER JAMES ,  MULLINS JOHN J G ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT ,  COR THERAPEUTICS INC

Inventor： KANTER JAMES ,  MULLINS JOHN J G ,  PANDEY ANJALI ,  SCARBOROUGH ROBERT

IPC: C07D311/22 ,  C07D311/58

CPC classification number: C07D311/58 ,  C07D311/22

Abstract: Novel processes for producing enantiomerically enriched and enantiomerically pure compositions of 2-acyl substituted chromane compounds, and 2-acylchromane compounds that are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors are disclosed. Further disclosed are processes for producing salts such as acid addition salts for such enantiomerically enriched compositions.

公开(公告)号：WO0217711A2

公开(公告)日：2002-03-07

申请号：PCT/US0126936

申请日：2001-08-31

Applicant: COR THERAPEUTICS INC ,  RAMAKRISHNAN VANITHA ,  PHILLIPS DAVID

Inventor： RAMAKRISHNAN VANITHA ,  PHILLIPS DAVID

IPC: A61P7/00 ,  C07K14/705 ,  C12N15/85 ,  G01N33/569 ,  G01N33/86 ,  A01K67/027

CPC classification number: C12N15/8509 ,  A01K67/0276 ,  A01K2217/075 ,  A01K2227/105 ,  A01K2267/03 ,  A01K2267/0375 ,  C07K14/705 ,  G01N33/56966 ,  G01N33/86 ,  G01N2333/435 ,  G01N2333/70546 ,  G01N2333/974 ,  G01N2500/10

Abstract: The present invention relates to therapeutics and diagnostics that take advantage of a novel signal transduction pathway in platelets. In addition, the present invention provides methods for identifying agents that modulate activities mediated by the novel transduction pathway including platelet activation and thrombosis.

Abstract translation: 本发明涉及利用血小板中的新型信号转导途径的治疗和诊断。 此外，本发明提供了鉴定调节由新型转导途径介导的活性（包括血小板活化和血栓形成）的药剂的方法。