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1. 发明授权

US06403578B1 Bicyclic fibrinogen antagonists 失效
标题翻译：双相纤维蛋白原拮抗剂
公开(公告)号：US06403578B1
公开(公告)日：2002-06-11
申请号：US08464779
申请日：1995-08-04
申请人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Thomas Wen-Fu Ku , Kenneth Allen Newlander , James Martin Samanen , Irene Nijole Uzinskas
发明人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Thomas Wen-Fu Ku , Kenneth Allen Newlander , James Martin Samanen , Irene Nijole Uzinskas
IPC分类号： A61K3155
CPC分类号： C07D223/16 , A61K31/55 , A61K31/551 , A61K31/5513 , C07D243/14 , C07D401/12
摘要： This invention relates to compounds of the formulae: wherein A1 is O, S, N—R1 or CHR1; A4 is N—R4 or CHR4; R2 is a sidechain containing an acid or ester group; R1, R4 and R5 are substituents such as H, alkyl and aryl alkyl, and R6 is a sidechain containing a nitrogen group; and pharmaceutically acceptable salts thereof, which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
摘要翻译：本发明涉及下式的化合物：其中A 1是O，S，N-R 1或CHR 1; A 4是N-R 4或CHR 4; R 2是含有酸或酯基的侧链; R 1，R 4和R 5是取代基，例如H ，烷基和芳基烷基，R 6是含有氮基的侧链; 其抑制血小板聚集有效的药学上可接受的盐，以及用于抑制血小板聚集的方法。

2. 发明授权

US6117866A Bicyclic fibrinogen antagonists 失效
标题翻译：双相纤维蛋白原拮抗剂
公开(公告)号：US6117866A
公开(公告)日：2000-09-12
申请号：US875359
申请日：1996-07-03
申请人： William Edward Bondinell , James Martin Samanen
发明人： William Edward Bondinell , James Martin Samanen
IPC分类号： C07D243/24 , A61K31/55 , A61K31/551 , A61P7/02 , A61P9/08 , A61P9/10 , A61P43/00 , C07D223/16 , C07D243/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/06 , A61K31/5513
CPC分类号： C07D223/16 , C07D243/14 , C07D401/12 , C07D401/14 , C07D409/06 , Y02P20/55
摘要： Certain compounds within formula (I) are inhibitors of platelet aggregation: ##STR1## wherein A.sup.1 is NH or CH.sub.2 ;R is H, C.sub.1-6 alkyl, benzyl or a carboxy protecting group;R.sup.3 is C.sub.1-6 alkyl, Ar-C.sub.0-6 alkyl, C.sub.3-7 cycloalkylC.sub.0-6 alkyl, or Het-C.sub.0-6 alkyl;R.sup.6 is 4-amidino-Ar-N(CH.sub.3)CO, [[2-(4-piperidinyl)ethyl](N-methyl)amino]carbonyl, (4,4'-bipiperidin-1-yl)carbonyl, [4-(2-aminoethyl)piperidin-1-yl]carbonyl, [[[3-(4-piperidinyl]propyl]methylamino]carbonyl, 1-[4-(4-pyridyl)piperazinyl]carbonyl, [[2-[(2-amino)pyrid-4-yl]ethyl]methylamino]carbonyl, [[2-(4-piperidinyl)ethyl]carbonyl]amino, [[2-(4-piperidinyl)ethyl]carbonyl]amino, [[2-(1-piperazinyl)ethyl]methylamino]-carbonyl, or [[(1,2,3,4-tetrahydro-7-isoquinolinyl]amino]carbonyl; andX is H, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkthio, trifluoroalkyl, N(R').sub.2, CO.sub.2 R', CON(R').sub.2, OH, F, Cl, Br or I.
摘要翻译： PCT No.PCT / US95 / 00248 Sec。 371日期：1996年7月3日 102（e）日期1996年7月3日PCT 1995年1月9日PCT PCT。出版物WO96 / 日期：1995年7月13日化学式（I）中的化合物是血小板聚集抑制剂：其中A1是NH或CH2; R为H，C 1-6烷基，苄基或羧基保护基; R3是C1-6烷基，Ar-C0-6烷基，C3-7环烷基C0-6烷基或Het-C0-6烷基; R6是4-脒基-Ar-N（CH3）CO，[[2-（4-哌啶基）乙基]（N-甲基）氨基]羰基，（4,4'-联哌啶-1-基）羰基，[4 - （2-氨基乙基）哌啶-1-基]羰基，[[[（3-哌啶基）丙基]甲基氨基]羰基，1- [4-（4-吡啶基）哌嗪基]羰基，[[2 - [ 2-氨基）吡啶-4-基]乙基]甲基氨基]羰基，[[2-（4-哌啶基）乙基]羰基]氨基，[[2-（4-哌啶基）乙基]羰基]氨基，[[2- （1-哌嗪基）乙基]甲基氨基]羰基或[[（1,2,3,4-四氢-7-异喹啉基）氨基]羰基; X是H，C 1-4烷基，C 1-4烷氧基，C 1-4烷硫基，三氟烷基，N（R'）2，CO 2 R'，CON（R'）2，OH，F，Cl，Br或I.

3. 发明授权

US5643872A Cyclic anti-aggregatory peptides 失效
公开(公告)号：US5643872A
公开(公告)日：1997-07-01
申请号：US296621
申请日：1994-08-26
申请人： Fadia El-Fehail Ali , James Martin Samanen
发明人： Fadia El-Fehail Ali , James Martin Samanen
IPC分类号： A61K38/00 , C07K5/09 , C07K5/10 , C07K5/103 , C07K5/11 , C07K5/12 , C07K7/06 , C07K7/64 , C07K14/75
CPC分类号： C07K7/06 , C07K14/75 , C07K5/0817 , C07K5/1008 , C07K5/1013 , C07K5/1019 , C07K5/123 , C07K7/64 , A61K38/00
摘要： This invention relates to compounds of the formula: ##STR1## wherein: A' is absent, Asn, Gln, Ala or Abu;A is absent or a D- or L-amino acid chosen from Arg, HArg, (Me.sub.2)Arg, (Et.sub.2)Arg, Abu, Ala, Gly, His, Lys, or an .alpha.-R' substituted derivative thereof, Dtc, Tpr and Pro;B is a D- or L-amino acid chosen from Arg, HArg, NArg, (Me.sub.2)Arg, (Et.sub.2)Arg and Lys or an .alpha.-R' substituted derivative thereof;Q is absent or a D or L amino acid chosen from Tyr, (Alk)Tyr, Phe, (4'W)Phe, HPhe, Phg, Pro, Trp, His, Ser, (Alk)Ser, Thr, (Alk)Thr, (Alk)Cys, (Alk)Pen, Ala, Val, Nva, Met, Leu, Ile, Nle and Nal, or an .alpha.-R' substituted derivative thereof;M is absent or Gly or a D- or L-amino acid chosen from Glu, Phe, Pro, Lys and Ser or, provided n is 1, B-Gly-Glu-Q;W is halogen or Alk;R' is Alk or PhCH.sub.2 ; ##STR2## wherein Z.sub.1 and Z.sub.2 are linked via a covalent bond between L.sup.1 and L.sup.2 ; or Z.sub.1 and Z.sub.2 are, taken together, a covalent bond between the amino terminal residue and the carboxy terminal residue;L.sup.1 and L.sup.2 are --S-- or --(CH.sub.2).sub.p --;X is R.sub.4 R.sub.5 N or H;Y is H, CONR.sub.1 R.sub.2 or CO.sub.2 R.sub.2 ;R.sub.1 and R.sub.2 are H, Alk or (CH.sub.2).sub.p Ar;R.sub.3 and R.sub.3' are H, Alk, (CH.sub.2).sub.p Ar or taken together are --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --;R.sub.4 is H or Alk;R.sub.5 is R.sub.11, R.sub.11 CO, R.sub.11 OCO, R.sub.11 OCH(R.sub.11')CO, R.sub.11 NHCH(R.sub.11')CO, R.sub.11 SCH(R.sub.11')CO, R.sub.11 SO.sub.2 or R.sub.11 SO;R.sub.6 is Alk, OAlk, halogen or X;R.sub.7 is H, Alk, OAlk, halogen or Y;R.sub.8 and R.sub.8' are H, Alk, (CH.sub.2).sub.p Ph, (CH.sub.2).sub.p Nph or taken together are --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --;R.sub.9 is H, Alk or Y;R.sub.10 is H or Alk;R.sub.11 and R.sub.11' are H, C.sub.1-5 alkyl, C.sub.3-7 cycloalkyl, Ar, Ar--C.sub.1-5 alkyl, Ar--C.sub.3-7 cycloalkyl;Ar is phenyl or phenyl substituted by one or two C.sub.1-5 alkyl, trifluoromethyl, hydroxy, C.sub.1-5 alkoxy or halogen groups;n is 1 or 2;q is 0 or 1; andp is 0, 1, 2 or 3;or a pharmaceutically acceptable salt thereof;which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, a method for inhibiting platelet aggregation and clot formation in a mammal, and a method for inhibiting reocclusion of a blood vessel following fibrinolytic therapy.

4. 发明授权

US6117910A Bicyclic fibrinogen antagonists 失效
标题翻译：双相纤维蛋白原拮抗剂
公开(公告)号：US6117910A
公开(公告)日：2000-09-12
申请号：US875361
申请日：1997-06-13
申请人： James Francis Callahan , Richard McCulloch Keenan , Chet Kwon , James Martin Samanen
发明人： James Francis Callahan , Richard McCulloch Keenan , Chet Kwon , James Martin Samanen
IPC分类号： A61K31/47 , A61K31/472 , A61P7/02 , A61P9/00 , A61P9/10 , C07C233/32 , C07C233/43 , C07C251/02 , C07C257/18 , C07D217/06 , A61K31/16 , C07D217/00
CPC分类号： C07D217/06 , C07C233/32 , C07C257/18 , C07C2102/10
摘要： This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
摘要翻译： PCT No.PCT / US95 / 15937 Sec。 371日期：1997年6月13日 102（e）日期1997年6月13日PCT提交1995年12月7日PCT公布。 WO96 / 18602 PCT出版物日期1996年6月20日本发明涉及下列化合物：其有效抑制血小板聚集，用于实现该活性的药物组合物和抑制血小板聚集的方法。

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