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公开(公告)号:US5559127A
公开(公告)日:1996-09-24
申请号:US416770
申请日:1995-05-31
申请人: George D. Hartman , John D. Prugh , Melissa S. Egbertson , Mark E. Duggan , William Hoffman , Wasyl Halezenko , Ben Askew
发明人: George D. Hartman , John D. Prugh , Melissa S. Egbertson , Mark E. Duggan , William Hoffman , Wasyl Halezenko , Ben Askew
IPC分类号: C07D333/54 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61P7/02 , C07D209/10 , C07D209/14 , C07D235/28 , C07D263/58 , C07D277/68 , C07D307/79 , C07D307/80 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , A61K31/445
CPC分类号: C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06
摘要: Fibrinogen receptor antagonists of the formula: ##STR1## wherein A,B,D,E,Y are as defined in the specification, are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.
摘要翻译: PCT No.PCT / US93 / 09730 Sec。 371日期:1995年5月31日 102(e)日期1995年5月31日PCT提交1993年10月12日PCT公布。 第WO94 / 08962号公报 日期1994年4月28日公开了以下结构式的纤维蛋白原受体拮抗剂:其中A,B,D,E,Y如说明书中所定义,用于抑制纤维蛋白原与血小板的结合和抑制聚集 的血小板。
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公开(公告)号:US5786373A
公开(公告)日:1998-07-28
申请号:US416772
申请日:1995-05-31
IPC分类号: A61K31/38 , A61K31/381 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/454 , A61P7/02 , C07C311/06 , C07C311/19 , C07D233/64 , C07D333/38 , C07D401/12 , C07D409/06 , C07D409/12 , C07D413/12 , A61K31/415 , A61K31/44 , C07D333/22
CPC分类号: C07D401/12 , C07C311/06 , C07C311/19 , C07D333/38 , C07D409/06 , C07D409/12 , C07D413/12
摘要: Novel fibrinogen receptor antagonists of the formula: X--Y--Z-Aryl-A--B and the pharmaceutically acceptable salts thereof, wherein Aryl is a 5-membered aromatic ring system containing 1 or 2 heteroatoms chosen from N, O or S wherein ring atoms may be unsubstituted or substituted with R.sup.5 and wherein S may be substituted with 0, 1 or 2 oxygen atoms; and X comprises various Nitrogen substituents including aromatic or nonaromatic systems; Y comprises, for example, alkyl or alkylaminocarbonylalkyl groups and Z and A are substituents which when present are independently chosen from alkyl or alkyloxyalkyl or other groups as defined herein; B is (a) or (b). The claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating or preventing thrombus formation.
摘要翻译: PCT No.PCT / US93 / 09750 Sec。 371日期:1995年5月31日 102(e)日期1995年5月31日PCT提交1993年10月12日PCT公布。 第WO94 / 08577号公报 日期1994年04月28日图像(a)<图像>(b)新型的具有下式的纤维蛋白原受体拮抗剂:XYZ-Aryl-AB及其药学上可接受的盐,其中芳基是含有1个 或选自N,O或S的2个杂原子,其中环原子可以是未取代的或被R 5取代,并且其中S可以被0,1或2个氧原子取代; X包括各种氮取代基,包括芳族或非芳族体系; Y包括例如烷基或烷基氨基羰基烷基,Z和A是当存在时独立地选自烷基或烷氧基烷基或本文定义的其它基团的取代基; B是(a)或(b)。 所要求保护的化合物显示纤维蛋白原受体拮抗剂活性,抑制血小板聚集,因此可用于调节或预防血栓形成。
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公开(公告)号:US5648368A
公开(公告)日:1997-07-15
申请号:US448347
申请日:1995-06-01
申请人: Melissa S. Egbertson , Laura M. Vassallo , George D. Hartman , Wasyl Halczenko , David B. Whitman , James J. Perkins , Amy E. Krause , Nathan Ihle , David Alan Claremon , William Hoffman , Mark E. Duggan
发明人: Melissa S. Egbertson , Laura M. Vassallo , George D. Hartman , Wasyl Halczenko , David B. Whitman , James J. Perkins , Amy E. Krause , Nathan Ihle , David Alan Claremon , William Hoffman , Mark E. Duggan
IPC分类号: C07D295/08 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/495 , A61P7/02 , A61P43/00 , C07C255/57 , C07C271/22 , C07C309/66 , C07C311/19 , C07D205/04 , C07D207/08 , C07D211/22 , C07D211/26 , C07D211/32 , C07D211/34 , C07D211/46 , C07D211/70 , C07D213/30 , C07D213/71 , C07D233/54 , C07D233/60 , C07D233/64 , C07D295/084 , C07D295/092 , C07D295/096 , C07D295/155 , C07D401/12 , C07D409/12 , C07D521/00 , C07D211/20 , C07D211/98
CPC分类号: C07D213/30 , C07C311/19 , C07D205/04 , C07D211/22 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/70 , C07D213/71 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D295/084 , C07D295/088 , C07D295/096 , C07D295/155 , C07D401/12 , C07D409/12
摘要: Novel fibrinogen receptor antagonists of the formula:X--Y--Z--Aryl--A--Bare provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.
摘要翻译: PCT No.PCT / US93 / 11623 Sec。 371日期:1995年6月1日 102(e)1995年6月1日PCT 1993年11月29日PCT PCT。 公开号WO94 / 12181 日期1994年6月9日提供了以下结构式的新型纤维蛋白原受体拮抗剂:X-Y-Z-芳基-A-Bare,其中要求保护的化合物表现出纤维蛋白原受体拮抗剂活性,抑制血小板聚集,因此可用于调节血栓形成。
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公开(公告)号:US5880136A
公开(公告)日:1999-03-09
申请号:US130334
申请日:1998-08-06
申请人: Mark E. Duggan , Melissa S. Egbertson , Wasyl Halczenko , George D. Hartman , William L. Laswell
发明人: Mark E. Duggan , Melissa S. Egbertson , Wasyl Halczenko , George D. Hartman , William L. Laswell
IPC分类号: C07D211/30 , A61K31/185 , A61K31/195 , A61K31/215 , A61K31/255 , A61K31/265 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/435 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/452 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/55 , A61K31/66 , A61P7/02 , A61P43/00 , C07C311/02 , C07C311/06 , C07C311/13 , C07C311/19 , C07C313/06 , C07C313/20 , C07C323/59 , C07C327/12 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/273 , C07D209/12 , C07D209/30 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/46 , C07D213/75 , C07D223/08 , C07D233/02 , C07D233/64 , C07D237/08 , C07D239/04 , C07D239/26 , C07D241/04 , C07D241/12 , C07D249/04 , C07D249/08 , C07D263/46 , C07D267/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08 , C07F9/38 , C07F9/40
CPC分类号: C07C311/06 , C07C311/13 , C07D211/22 , C07D409/12
摘要: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
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公开(公告)号:US5292756A
公开(公告)日:1994-03-08
申请号:US860747
申请日:1992-03-25
IPC分类号: C07D211/30 , A61K31/185 , A61K31/195 , A61K31/215 , A61K31/255 , A61K31/265 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/435 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/452 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/55 , A61K31/66 , A61P7/02 , A61P43/00 , C07C311/02 , C07C311/06 , C07C311/13 , C07C311/19 , C07C313/06 , C07C313/20 , C07C323/59 , C07C327/12 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/273 , C07D209/12 , C07D209/30 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/46 , C07D213/75 , C07D223/08 , C07D233/02 , C07D233/64 , C07D237/08 , C07D239/04 , C07D239/26 , C07D241/04 , C07D241/12 , C07D249/04 , C07D249/08 , C07D263/46 , C07D267/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08 , C07F9/38 , C07F9/40 , C07D267/22
CPC分类号: C07C311/06 , C07C311/13 , C07D211/22 , C07D409/12
摘要: A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
摘要翻译: 一系列式(IMAGE)的非肽衍生物
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公开(公告)号:US5852045A
公开(公告)日:1998-12-22
申请号:US729968
申请日:1996-10-15
申请人: Ben C. Askew , George D. Hartman , Mark E. Duggan , Steven D. Young , John H. Hutchinson , John S. Wai , Melissa S. Egbertson , Laura M. Vassallo , Laura A. Libby , Amy E. Krause , Wasyl Halczenko , Nathan C. Ihle
发明人: Ben C. Askew , George D. Hartman , Mark E. Duggan , Steven D. Young , John H. Hutchinson , John S. Wai , Melissa S. Egbertson , Laura M. Vassallo , Laura A. Libby , Amy E. Krause , Wasyl Halczenko , Nathan C. Ihle
IPC分类号: C07D401/06 , C07D401/14 , C07D405/14 , C07D453/04 , C07D521/00 , C07K5/06 , A61K31/445 , A61K31/495
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D405/14 , C07D453/04 , C07K5/06026
摘要: Fibrinogen receptor antagonists having the structure, for example, of ##STR1## for example ##STR2##
摘要翻译: 具有例如
结构的纤维蛋白原受体拮抗剂,例如 -
公开(公告)号:US5814643A
公开(公告)日:1998-09-29
申请号:US861545
申请日:1997-05-22
申请人: Mark E. Duggan , Melissa S. Egbertson , Wasyl Halczenko , George D. Hartman , William L. Laswell
发明人: Mark E. Duggan , Melissa S. Egbertson , Wasyl Halczenko , George D. Hartman , William L. Laswell
IPC分类号: C07D211/30 , A61K31/185 , A61K31/195 , A61K31/215 , A61K31/255 , A61K31/265 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/435 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/452 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/55 , A61K31/66 , A61P7/02 , A61P43/00 , C07C311/02 , C07C311/06 , C07C311/13 , C07C311/19 , C07C313/06 , C07C313/20 , C07C323/59 , C07C327/12 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/273 , C07D209/12 , C07D209/30 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/46 , C07D213/75 , C07D223/08 , C07D233/02 , C07D233/64 , C07D237/08 , C07D239/04 , C07D239/26 , C07D241/04 , C07D241/12 , C07D249/04 , C07D249/08 , C07D263/46 , C07D267/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08 , C07F9/38 , C07F9/40
CPC分类号: C07C311/06 , C07C311/13 , C07D211/22 , C07D409/12
摘要: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
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公开(公告)号:US5658929A
公开(公告)日:1997-08-19
申请号:US505417
申请日:1995-07-21
申请人: Mark E. Duggan , Melissa S. Egbertson , Wasyl Halczenko , George D. Hartman , William L. Laswell
发明人: Mark E. Duggan , Melissa S. Egbertson , Wasyl Halczenko , George D. Hartman , William L. Laswell
IPC分类号: C07D211/30 , A61K31/185 , A61K31/195 , A61K31/215 , A61K31/255 , A61K31/265 , A61K31/40 , A61K31/4015 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/435 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/452 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/55 , A61K31/66 , A61P7/02 , A61P43/00 , C07C311/02 , C07C311/06 , C07C311/13 , C07C311/19 , C07C313/06 , C07C313/20 , C07C323/59 , C07C327/12 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/273 , C07D209/12 , C07D209/30 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/46 , C07D213/75 , C07D223/08 , C07D233/02 , C07D233/64 , C07D237/08 , C07D239/04 , C07D239/26 , C07D241/04 , C07D241/12 , C07D249/04 , C07D249/08 , C07D263/46 , C07D267/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D403/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/08 , C07F9/38 , C07F9/40
CPC分类号: C07C311/06 , C07C311/13 , C07D211/22 , C07D409/12
摘要: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
摘要翻译: 作为纤维蛋白原IIb / IIIa受体的拮抗剂的一系列非肽衍生物,因此是可用于预防和治疗由血栓形成引起的疾病的血小板抗聚集化合物。
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公开(公告)号:US5264420A
公开(公告)日:1993-11-23
申请号:US860748
申请日:1992-03-25
申请人: Mark E. Duggan , Melissa S. Egbertson , Nathan Ihle , George D. Hartman , Laura M. Turchi , David Whitman
发明人: Mark E. Duggan , Melissa S. Egbertson , Nathan Ihle , George D. Hartman , Laura M. Turchi , David Whitman
IPC分类号: C07D211/34 , C07D401/12 , A61K37/02 , C07K5/02 , C07K5/06 , C07K5/08
CPC分类号: C07D401/12 , C07D211/34
摘要: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.
摘要翻译: 公开了用于抑制纤维蛋白原与血小板结合和抑制血小板聚集的式I的纤维蛋白原受体拮抗剂。
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公开(公告)号:US5854245A
公开(公告)日:1998-12-29
申请号:US883108
申请日:1997-06-26
IPC分类号: C07D471/04 , C07D493/04 , A61K31/495 , A61K31/435 , C07D241/04 , C07D241/38
CPC分类号: C07D471/04 , C07D493/04
摘要: Fibrinogen receptor antagonists having the structure X--Y--Z--A--B and pharmaceutically acceptable salts, wherein X is a 5, 6 or 7 membered aromatic or nonaromatic ring, and Y is a 5 or 6 membered aromatic ring, e.g., ##STR1##
摘要翻译: 具有结构X-Y-Z-A-Band药学上可接受的盐的纤维蛋白原受体拮抗剂,其中X是5,6或7元芳族或非芳族环,Y是5或6元芳族环,例如,
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