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1. 发明申请

WO9747329A2 RADIOPHARMACEUTICAL COMPOSITIONS CAPABLE OF LOCALIZING AT SITES OF THROMBUS 审中-公开
标题翻译：放射性物质组合物可以在THROMBUS的位点定位
公开(公告)号：WO9747329A2
公开(公告)日：1997-12-18
申请号：PCT/US9709292
申请日：1997-06-05
申请人： SEARLE & CO , MALLINCKRODT MEDICAL INC , FEIGEN LARRY P , FLYNN DANIEL LEE , NEEDLEMAN PHILIP , SRINIVASAN ANANTHACHARI , ZABLOCKI JEFFERY ALAN
发明人： FEIGEN LARRY P , FLYNN DANIEL LEE , NEEDLEMAN PHILIP , SRINIVASAN ANANTHACHARI , ZABLOCKI JEFFERY ALAN
IPC分类号： A61K38/00 , A61K51/00 , A61K51/08 , C07K5/072 , A61K51/58
CPC分类号： C07K5/06113 , A61K51/088 , A61K2121/00 , A61K2123/00
摘要： A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively. Methods of imaging a site of thrombus in a mammalian body by administering a diagnostically effective amount of the radiopharmaceutical composition of this invention complexed with a selected diagnostic metal radionuclide and methods of providing therapy to a site of thrombus in a mammalian body by administering a therapeutically effective amount of the radiopharmaceutical composition of this invention complexed with a selected therapeutic metal radionuclide are also provided as well as kits for preparing such radiopharmaceutical compositions.
摘要翻译：提供能够定位在哺乳动物体内含有活化血小板的血栓部位的放射性药物，其中放射性药物包含能够特异性结合血栓中血小板的GPIIb / IIIa整联蛋白受体的线性拟肽含量配体和共价结合的放射性核素含拟肽的配体。提供本发明的配体组合物与所选择的金属放射性核素复合以形成诊断或治疗性放射性药物以分别对血栓位点成像或向血栓部位提供放射治疗。通过施用诊断上有效量的本发明的放射性药物组合物与选定的诊断性金属放射性核素复合而在哺乳动物体内成像血栓位点的方法和通过施用治疗有效的方法向哺乳动物体内的血栓位点提供治疗还提供了与选定的治疗性金属放射性核素复合的本发明的放射性药物组合物的量以及用于制备这种放射性药物组合物的试剂盒。

2. 发明专利

AU3474997A Radiopharmaceutical compositions capable of localizing at sites of thrombus 未知
公开(公告)号：AU3474997A
公开(公告)日：1998-01-07
申请号：AU3474997
申请日：1997-06-05
申请人： SEARLE & CO , MALLINCKRODT MEDICAL INC
发明人： FEIGEN LARRY P , FLYNN DANIEL LEE , NEEDLEMAN PHILIP , SRINIVASAN ANANTHACHARI , ZABLOCKI JEFFERY ALAN
IPC分类号： A61K38/00 , A61K51/00 , A61K51/08 , C07K5/072
摘要： A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively. Methods of imaging a site of thrombus in a mammalian body by administering a diagnostically effective amount of the radiopharmaceutical composition of this invention complexed with a selected diagnostic metal radionuclide and methods of providing therapy to a site of thrombus in a mammalian body by administering a therapeutically effective amount of the radiopharmaceutical composition of this invention complexed with a selected therapeutic metal radionuclide are also provided as well as kits for preparing such radiopharmaceutical compositions.

3. 发明申请

WO9215607A3 PHENYL AMIDINES DERIVATIVES USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：苯甲酰胺衍生物有用的片剂聚集抑制剂
公开(公告)号：WO9215607A3
公开(公告)日：1992-10-29
申请号：PCT/US9201531
申请日：1992-03-05
申请人： SEARLE & CO
发明人： GARLAND ROBERT BRUCE , MIYANO MASATERU , ZABLOCKI JEFFERY ALAN , SCHRETZMAN LORI ANN
IPC分类号： A61K31/195 , A61K31/197 , A61K31/198 , A61K31/22 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61P7/02 , C07C257/18 , C07D209/16 , C07D209/20 , C07K5/06 , C07K5/072 , C07K14/75 , A61K37/02
CPC分类号： C07K5/06113 , A61K38/00 , C07C257/18 , C07D209/16 , C07K5/06 , C07K14/75
摘要： This invention relates to phenyl amidines derivatives having formula (I) or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidines derivatives.

4. 发明专利

ES2191659T3 未知
公开(公告)号：ES2191659T3
公开(公告)日：2003-09-16
申请号：ES92922021
申请日：1992-10-06
申请人： SEARLE & CO
发明人： BOVY PHILIPPE ROGER , RICO JOSEPH GERACE , ROGERS THOMAS EDWARD , TJOENG FOE SIONG , ZABLOCKI JEFFERY ALAN
IPC分类号： C07D239/42 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/505 , A61P7/02 , C07D213/55 , C07D213/58 , C07D239/26 , C07D307/54 , C07D317/60 , C07D317/62 , C07D317/66 , C07D333/24 , C07D333/38 , A61K31/335

5. 发明专利

DK0630366T3 未知
公开(公告)号：DK0630366T3
公开(公告)日：2003-04-22
申请号：DK92922021
申请日：1992-10-06
申请人： SEARLE & CO
发明人： ZABLOCKI JEFFERY ALAN , BOVY PHILIPPE ROGER , RICO JOSEPH GERACE , ROGERS THOMAS EDWARD , TJOENG FOE SIONG
IPC分类号： C07D239/42 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/505 , A61P7/02 , C07D213/55 , C07D213/58 , C07D239/26 , C07D307/54 , C07D317/60 , C07D317/62 , C07D317/66 , C07D333/24 , C07D333/38 , A61K31/335

6. 发明专利

CA2159450A1 1-AMIDINOPHENYL-PYRROLIDONES PIPERIDINONES AZETINONES AS PLATELET AGGREGATION INHIBITORS 未知
公开(公告)号：CA2159450A1
公开(公告)日：1994-10-13
申请号：CA2159450
申请日：1994-03-30
申请人： SEARLE & CO
发明人： ABOOD NORMAN ANTHONY , FLYNN DANIEL LEE , GARLAND ROBERT BRUCE , SCHRETZMAN LORI ANN , WILLIAMS KENNETH , ZABLOCKI JEFFERY ALAN , HOCKERMAN SUSAN LANDIS
IPC分类号： C07D227/12 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P7/02 , C07C255/60 , C07C271/22 , C07D205/08 , C07D205/085 , C07D207/26 , C07D207/27 , C07D207/273 , C07D211/40 , C07D211/58 , C07D211/76 , C07D405/12 , C07D409/12 , C07F7/08 , C07F7/10 , A61K31/695
摘要： This invention relates to compounds having formula (I) or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidin es derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

7. 发明专利

IE921574A1 PEPTIDE MIMETIC COMPOUNDS USEFUL AS PLATELET AGGREGATION¹INHIBITORS 未知
公开(公告)号：IE921574A1
公开(公告)日：1992-11-18
申请号：IE921574
申请日：1992-07-01
申请人： SEARLE & CO , MONSANTO CO
发明人： GARLAND ROBERT BRUCE , MIYANO MASATERU , ZABLOCKI JEFFERY ALAN , BOVY PHILIPPE ROGER , MCMACKINS DUDLEY ELGIN , RICO JOSEPH GERACE , TJOENG FOE SIONG , TOTH MIHALY VADKERTI
IPC分类号： C07C257/18 , C07D213/55 , C07D317/60 , C07D333/60 , C07C257/10 , C07D213/04 , C07D317/46 , C07D333/58 , C07K5/06
摘要： The present invention relates to a class of compounds represented by the formula: or a pharmaceutically acceptable salt thereof, wherein W is the radical OR1 wherein R1 is hydrido, alkyl, phenyl, phenylalkyl which may be further substituted; or W is the amino radical of the formula NHOH; R2 is hydrido, alkyl, alkenyl, cycloalkyl, cycloalkenyl which may be further substituted; or R2 is phenyl, phenylalkyl, naphthyl, naphthylalkyl which may be further substituted; or R2 is a heteromonocyclic ring structure having 5 or 6 ring carbon atoms wherein 1 or 2 of the ring carbon atoms are replaced by nitrogen, oxygen or sulfur and wherein the ring is selected from saturated, partially unsaturated, and fully unsaturated rings or a fused bicyclic ring structure having 10 to 12 ring carbon atoms wherein 1 to 3 of the ring carbon atoms may be replaced by nitrogen, oxygen or sulfur and each ring may independently be saturated, partially unsaturated or fully unsaturated which may be further stituted; R3 and R4 are each independently selected from hydrido, alkyl having 1 to 6 carbon atoms, hydroxy and halo; R5 and R6 are each independently selected from hydrido, alkyl having 1 to 6 carbon atoms, hydroxy, halo and alkoxy having 1 to 6 carbon atoms; and Y is alkyl having 1 to 6 carbon atoms, alkenyl having 2 to 6 carbon atoms, alkynyl having 2 to 6 carbon atoms or carbonylalkyl which may be further substituted. Such compounds and compositions thereof have usefulness as inhibitors of platelet aggregation.

8. 发明专利

IE920710A1 PHENYL AMIDINES DERIVATIVES USEFUL AS PLATELET AGGREGATION¹INHIBITORS 未知
公开(公告)号：IE920710A1
公开(公告)日：1992-09-09
申请号：IE920710
申请日：1992-03-05
申请人： SEARLE & CO
发明人： GARLAND ROBERT BRUCE , MIYANO MASATERU , ZABLOCKI JEFFERY ALAN
IPC分类号： A61K31/195 , A61K31/197 , A61K31/198 , A61K31/22 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61P7/02 , C07C257/18 , C07D209/16 , C07D209/20 , C07K5/06 , C07K5/072 , C07K14/75 , A61K37/02
摘要： This invention relates to phenyl amidines derivatives having the following formula or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidines derivatives.

9. 发明专利

AT195117T 未知
公开(公告)号：AT195117T
公开(公告)日：2000-08-15
申请号：AT94913308
申请日：1994-03-30
申请人： SEARLE & CO
发明人： ABOOD NORMAN ANTHONY , FLYNN DANIEL LEE , GARLAND ROBERT BRUCE , SCHRETZMAN LORI ANN , WILLIAMS KENNETH , ZABLOCKI JEFFERY ALAN , HOCKERMAN SUSAN LANDIS
IPC分类号： C07D227/12 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P7/02 , C07C255/60 , C07C271/22 , C07D205/08 , C07D205/085 , C07D207/26 , C07D207/27 , C07D207/273 , C07D211/40 , C07D211/58 , C07D211/76 , C07D405/12 , C07D409/12 , C07F7/08 , C07F7/10
摘要： PCT No. PCT/US94/03259 Sec. 371 Date May 23, 1995 Sec. 102(e) Date May 23, 1995 PCT Filed Mar. 30, 1994 PCT Pub. No. WO94/22820 PCT Pub. Date Oct. 13, 1994This invention relates to compounds having the following formula or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

10. 发明专利

NO305950B1 未知
公开(公告)号：NO305950B1
公开(公告)日：1999-08-23
申请号：NO953844
申请日：1995-09-28
申请人： SEARLE & CO
发明人： ABOOD NORMAN ANTHONY , FLYNN DANIEL LEE , GARLAND ROBERT BRUCE , SCHRETZMAN LORI ANN , WILLIAMS KENNETH , ZABLOCKI JEFFERY ALAN , HOCKERMAN SUSAN LANDIS
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/443 , C07D227/12 , A61K31/4433 , A61K31/445 , A61P7/02 , C07C255/60 , C07C271/22 , C07D205/08 , C07D205/085 , C07D207/26 , C07D207/27 , C07D207/273 , C07D211/40 , C07D211/58 , C07D211/76 , C07D405/12 , C07D409/12 , C07F7/08 , C07F7/10
摘要： PCT No. PCT/US94/03259 Sec. 371 Date May 23, 1995 Sec. 102(e) Date May 23, 1995 PCT Filed Mar. 30, 1994 PCT Pub. No. WO94/22820 PCT Pub. Date Oct. 13, 1994This invention relates to compounds having the following formula or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.

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