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1. 发明授权

US6127359A Bicyclic fibrinogen antagonists 失效
标题翻译：双相纤维蛋白原拮抗剂
公开(公告)号：US6127359A
公开(公告)日：2000-10-03
申请号：US312006
申请日：1999-05-14
申请人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Thomas Wen-Fu Ku , Kenneth Allen Newlander
发明人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Thomas Wen-Fu Ku , Kenneth Allen Newlander
IPC分类号： C07D223/16 , C07D243/14 , C07D267/14 , C07D281/10 , A61K31/55 , C07D227/08 , A61K37/48
CPC分类号： C07D223/16 , C07D243/14 , C07D267/14 , C07D281/10
摘要： Compounds of the formula: ##STR1## wherein A.sup.1 to A.sup.5 form a seven-membered ring containing one optionally substituted nitrogen atom and one heteroatom selected from oxygen and nitrogen;D.sup.1 to D.sup.4 form a substituted six membered ring, optionally containing up to two nitrogen atoms;R is preferably at least one acid containing substituent;R* is is one or more groups chosen from H, Q-C.sub.1-6 alkyl, Q-C.sub.1-6 oxoalkyl, Q-C.sub.2-6 alkenyl, Q-C.sub.3-4 oxoalkenyl, Q-C.sub.3-4 oxoalkynyl, Q-C.sub.2-4 alkynyl, C.sub.3-6 cycloalkyl, Ar or Het;Q is H, C.sub.3-6 cycloalkyl, Het or Ar;R.sup.6 is preferably a basic nitrogen containing substituent;are inhibitors of platelet aggregation.
摘要翻译：下式的化合物：其中A1至A5形成含有一个任选取代的氮原子和一个选自氧和氮的杂原子的七元环; D1至D4形成任选含有至多两个氮原子的取代六元环; R优选为至少一种含酸取代基; R *是一个或多个选自H，Q-C 1-6烷基，Q-C 1-6氧基烷基，Q-C 2-6烯基，Q-C 3-4烯基，Q-C 3-4氧代炔基，Q-C 2-4亚炔基， 6环烷基，Ar或Het; Q是H，C 3-6环烷基，Het或Ar; R6优选为碱性含氮取代基; 是血小板聚集的抑制剂。

2. 发明授权

US5726192A Platelet aggregation inhibiting compounds 失效
标题翻译：血小板聚集抑制化合物
公开(公告)号：US5726192A
公开(公告)日：1998-03-10
申请号：US464728
申请日：1995-08-08
申请人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Brian Walter Metcalf , James Samanen , Tobias Oregon Yellin
发明人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Brian Walter Metcalf , James Samanen , Tobias Oregon Yellin
IPC分类号： A61K31/195 , A61K31/415 , A61K31/4184 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K38/00 , A61P7/02 , A61P9/00 , C07D213/56 , C07D213/73 , C07D213/75 , C07D235/30 , C07D277/64 , C07D417/12 , C07K5/02 , C07K5/087 , C07K5/09 , C07K5/11 , C07D213/02
CPC分类号： C07D213/73 , C07D213/56 , C07D235/30 , C07D277/64 , C07D417/12 , C07K5/0202 , C07K5/0205 , C07K5/0812 , C07K5/0815 , C07K5/0817 , A61K38/00
摘要： This invention relates to compounds of the formula: W--Z--(CR'R.sup.10).sub.r --U--(CR'.sub.2).sub.s --V--A wherein: ##STR1## A is W is R'R"N--; Z is Het; U and V independently are absent or present as CO, CR'.sub.2, C(.dbd.CR'.sub.2), S(O).sub.r, O, NR', CR'OR', CR'(OR")CR'.sub.2, CR'.sub.2 CR'(OR"), C(O)CR'.sub.2, CR'.sub.2 C(O), CONR', NR'CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR', NR'C(S), S(O).sub.r NR', NR'S(O).sub.r, N.dbd.N, NR'NR', NR'CR'.sub.2, NR'CR'.sub.2, CR'.sub.2 O, OCR'.sub.2, .sup.c.tbd.c, CR'.dbd.CR', or CR'(NR'R")C(O); each r independently is 0 to 3; s is 0 to 2; each R' independently is H, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, or Ar--C.sub.0-4 alkyl; each R" independently is R', --C(O)R', or --C(O)OR.sup.15 ; R.sup.10 is as H, C.sub.1-4 alkyl, or --NR'R'; each R.sup.15 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, or AR--C.sub.0-4 alkyl; R.sup.2 is present once or twice as C.sub.1-4 alkyl, J--CO.sub.2 R', CONR', SR', NR'R", C.sub.1-4 alkoxy, hydroxy, CN, CF.sub.3, halo, or ##STR2## with the proviso that at least one R.sup.2 is J--CO.sub.2 R; J is a single bond, --OCR'.sub.2 --, --NR'CR'.sub.2 --, CR'.sub.2 --CR'.sub.2 --, --CR'.sub.2 --, --CR'.dbd.CR', or --C(O)NR'CR'.sub.2 --; and each R.sup.14 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, Ar--C.sub.0-4 alkyl, C(O)R', CN, NO.sub.2, SO.sub.2 R', or C(O)OR.sup.15 ; or a pharmaceutically acceptable salt thereof.
摘要翻译： PCT No.PCT / US93 / 12530 Sec。 371日期：1995年8月8日 102（e）日期1995年8月8日PCT提交1993年12月22日PCT公布。第WO94 / 14775号公报日期：1994年7月7日本发明涉及下式的化合物：WZ-（CR'R10）rU-（CR'2）sV-A其中：不存在或作为CO，CR'2，C（= CR'2），S（O）r，O，NR'，CR'OR'，CR'（OR“）CR'2，CR'2CR'（OR”），C（O）CR'2， CR（O），CONR'，NR'CO，OC（O），C（O）O，C（S）O，OC（S），C（S）NR'，NR'C（S） S（O）rNR'，NR'（O）r，N = N，NR'NR'，NR'CR'2，NR'CR'2，CR'2O，OCR'2，c 3BOND c，CR'= CR '或CR'（NR'R“）C（O）; 每个r独立为0至3; s为0〜2; 每个R'独立地为H，C 1-4烷基，C 3-7环烷基-C 0-4烷基或Ar-C 0-4烷基; 每个R“独立地是R'，-C（O）R'或-C（O）OR 15; R 10为H，C 1-4烷基或-NR'R'; 每个R 15独立地为C 1-4烷基，C 3-7环烷基-C 0-4烷基或AR-C 0-4烷基; R2存在一次或两次作为C 1-4烷基，J-CO 2 R'，CONR'，SR'，NR'R“，C 1-4烷氧基，羟基，CN，CF 3，卤素或”IMAGE“，条件是至少一个R2是J-CO2R; J是单键，-OCR'2-，-NR'CR'2-，CR'2-CR'2-，-CR'2-，-CR'= CR'或-C（O）NR' CR'2-; 并且每个R 14独立地为C 1-4烷基，C 3-7环烷基-C 0-4烷基，Ar-C 0-4烷基，C（O）R'，CN，NO 2，SO 2 R'或C（O）OR 15; 或其药学上可接受的盐。

3. 发明授权

US06518267B1 Protease inhibitors 失效
标题翻译：蛋白酶抑制剂
公开(公告)号：US06518267B1
公开(公告)日：2003-02-11
申请号：US09700828
申请日：2000-11-21
申请人： William Edward Bondinell , Renee Louise DesJarlais , Daniel Frank Veber , Dennis Shinji Yamashita
发明人： William Edward Bondinell , Renee Louise DesJarlais , Daniel Frank Veber , Dennis Shinji Yamashita
IPC分类号： A61K31535
CPC分类号： C07D213/89 , A61K38/00 , C07C271/22 , C07C311/16 , C07D213/56 , C07D215/48 , C07D215/54 , C07D295/155 , C07D307/85 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D495/04 , C07K5/06026 , C07K5/06139
摘要： The present invention provides bis-aminomethyl carbonyl protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
摘要翻译：本发明提供了二氨基甲基羰基蛋白酶抑制剂及其药学上可接受的盐，水合物和溶剂合物，其抑制蛋白酶，包括组织蛋白酶K，这些化合物的药物组合物，以及用于治疗过度骨丢失或软骨或基质降解的疾病的方法，包括骨质疏松症 ; 牙龈疾病包括牙龈炎和牙周炎; 关节炎，更具体地，骨关节炎和类风湿性关节炎; 佩吉特病恶性高钙血症; 和代谢性骨病，其包括通过向有需要的患者施用本发明的化合物来抑制所述骨丢失或过度软骨或基质降解。

4. 发明授权

US6069143A Fibrinogen receptor antagonists 失效
标题翻译：纤维蛋白原受体拮抗剂
公开(公告)号：US6069143A
公开(公告)日：2000-05-30
申请号：US584030
申请日：1996-01-11
申请人： Fadia El-Fehail Ali , William Edward Bondinell , Raul Rolando Calvo , Thomas Wen-Fu Ku , William Henry Miller , James Samanen , Joseph Walter Venslavsky , Tobias Oregon Yellin
发明人： Fadia El-Fehail Ali , William Edward Bondinell , Raul Rolando Calvo , Thomas Wen-Fu Ku , William Henry Miller , James Samanen , Joseph Walter Venslavsky , Tobias Oregon Yellin
IPC分类号： C07D295/12 , A61K31/454 , A61K31/495 , A61P7/02 , A61P9/00 , A61P43/00 , C07D211/58 , C07D211/62 , C07D295/135 , C07D295/20 , C07D295/215 , C07D401/12 , A61K31/445 , C07D401/14
CPC分类号： C07D295/215 , C07D211/58 , C07D211/62 , C07D295/135
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：本发明涉及下列化合物：其有效抑制血小板聚集，用于实现这种活性的药物组合物和抑制血小板聚集的方法。

5. 发明授权

US5693636A Bicyclic fibrinogen antagonists 失效
标题翻译：双相纤维蛋白原拮抗剂
公开(公告)号：US5693636A
公开(公告)日：1997-12-02
申请号：US923794
申请日：1992-06-26
申请人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Thomas Wen-Fu Ku , Kenneth Allen Newlander
发明人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Thomas Wen-Fu Ku , Kenneth Allen Newlander
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/675 , A61K31/69 , A61P7/02 , A61P9/08 , A61P9/10 , C07D223/16 , C07D243/12 , C07D243/14 , C07D267/14 , C07D281/10 , C07D471/04 , C07D491/048 , C07F9/40 , C07D403/00
CPC分类号： C07D223/16 , C07D243/14 , C07D267/14 , C07D281/10
摘要： This invention relates to compounds of the formula: ##STR1## wherein A.sup.1 to A.sup.5 form an accessible substituted seven-membered ring, which may be saturated or unsaturated, optionally containing up to two heteroatoms chosen from the group of O, S and N wherein S and N may be optionally oxidized; D.sup.1 to D.sup.4 form an accessible substituted six membered ring, optionally containing up to two nitrogen atoms; R is at least one substituent chosen from the group of R.sup.7, or Q--C.sub.1-4 alkyl, Q--C.sub.2-4 alkenyl, Q--C.sub.2-4 alkynyl, preferably substituted by an acidic function; R* is H, Q--C.sub.1-6 alkyl, Q--C.sub.1-6 oxoalkyl, Q--C.sub.2-6 alkenyl or Q--C.sub.2-4 alkynyl, C.sub.3-6 cycloalkyl, Ar or Het, optionally substituted by one or more substitutents; and R.sup.6 is preferably a substituent containing a basic nitrogen moiety; or a pharmaceutically acceptable salt 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： PCT No.PCT / US92 / 05463 Sec。 371日期：1992年6月26日 102（e）日期1992年6月26日PCT提交1992年6月26日PCT公布。第WO93 / 00095号公报日本1993年1月7日本发明涉及下式的化合物：其中A1至A5形成可取代的七元环，其可以是饱和或不饱和的，任选地含有至多两个选自O， S和N，其中S和N可以任选被氧化; D1至D4形成可取代的六元环，任选地含有至多两个氮原子; R是选自R7或Q-C1-4烷基，Q-C2-4链烯基，Q-C2-4炔基，优选被酸性官能团取代的至少一个取代基; R *是任选被一个或多个取代基取代的H，Q-C 1-6烷基，Q-C 1-6氧代烷基，Q-C 2-6烯基或Q-C 2-4亚炔基，C 3-6环烷基，Ar或Het。并且R 6优选为含有碱性氮部分的取代基; 或其药学上可接受的盐，其有效抑制血小板聚集，用于实现这种活性的药物组合物和抑制血小板聚集的方法。

6. 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.

7. 发明授权

US6028087A Platelet aggregation inhibiting compounds 失效
标题翻译：血小板聚集抑制化合物
公开(公告)号：US6028087A
公开(公告)日：2000-02-22
申请号：US10238
申请日：1998-01-21
申请人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Brian Walter Metcalf , James Samanen , Tobias Oregon Yellin
发明人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Brian Walter Metcalf , James Samanen , Tobias Oregon Yellin
IPC分类号： A61K38/00 , C07D213/56 , C07D213/73 , C07D417/12 , C07K5/083 , C07K5/09 , A61K31/44
CPC分类号： C07D213/73 , C07D213/56 , C07D417/12 , C07K5/0806 , C07K5/0815 , C07K5/0817 , A61K38/00
摘要： Compounds of the formula (I):W--Z--(CR'R.sup.10).sub.r --U--(CR'.sub.2).sub.s --V--A (I)wherein:A is ##STR1## W is .sup.N ; Z is (CH.sub.2).sub.1-2 ;U and V independently are present as CO, CR'.sub.2, C(.dbd.CR'.sub.2), S(O).sub.r, O, NR', CR'OR', CR'(OR")CR'.sub.2, CR'.sub.2 CR'(OR"), C(O)CR'.sub.2, CR'.sub.2 C(O), CONR', NR'CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR', NR'C(S), S(O).sub.r NR', NR'S(O).sub.r, N.dbd.N, NR'NR', NR'CR'.sub.2, NR'CR'.sub.2, CR'.sub.2 O, OCR'.sub.2, C.tbd.C, CR'.dbd.CR', or CR'(NR'R")C(O);each r independently is 0 to 3;s is 0 to 2;each R' independently is H, C.sub.1-4 alkyl, C.sub.3-7 cycloalky-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;each R" independently is R', --C(O)R', or --C(O)OR.sup.15 ;R.sup.10 is H, C.sub.1-4 alkyl, or --NR'R';each R.sup.15 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;R.sup.2 is present once or twice as C.sub.1-4 alkyl, J--CO.sub.2 R', CONR', SR', NR'R", C .sub.1-4 alkoxy, hydroxy, CN, CF.sub.3, halo, or ##STR2## with the proviso that at least one R.sup.2 is J--CO.sub.2 R; and J is a single bond, --OCR'.sub.2 --, --NR'CR'.sub.2 --, CR'.sub.2 --CR'.sub.2 --, --CR'.sub.2 --, --CR'.dbd.CR', or --C(O)NR'CR'.sub.2 --;each R.sup.14 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, Ar-C.sub.0-4 alkyl, C(O)R', CN, NO.sub.2, SO.sub.2 R', or C(O)OR.sup.15 ;or a pharmaceutically acceptable salt thereof, are effective for inhibiting platelet aggregation.
摘要翻译：式（I）的化合物：W-Z-（CR'R10）r-U-（CR'2）s-V-A（I）其中：A是W是+ E，crc N + EE; Z是（CH 2）1-2; U和V独立地作为CO，CR'2，C（= CR'2），S（O）r，O，NR'，CR'OR'，CR'（OR“）CR'2，CR' （OR），C（O）CR'2，CR'2C（O），CONR'，NR'CO，OC（O），C（O）O，C（O）），C（S）NR'，NR'C（S），S（O）rNR'，NR'S（O）r，N = N，NR'NR'，NR'CR'2，NR'CR'2， CR'2O，OCR'2，C 3BOND C，CR'= CR'或CR'（NR'R“）C（O）; 每个r独立为0至3; s为0〜2; 每个R'独立地为H，C 1-4烷基，C 3-7环烷基-C 0-4烷基或Ar-C 0-4烷基; 每个R“独立地是R'，-C（O）R'或-C（O）OR 15; R 10是H，C 1-4烷基或-NR'R'; 每个R 15独立地为C 1-4烷基，C 3-7环烷基-C 0-4烷基或Ar-C 0-4烷基; R 2存在一次或两次作为C 1-4烷基，J-CO 2 R'，CONR'，SR'，NR'R“，C 1-4烷氧基，羟基，CN，CF 3，卤素，或条件是至少一个R 2 是J-CO2R; 并且J是单键，-OCR'2 - ，-NR'CR'2 - ，CR'2-CR'2，-CR'2-，-CR'= CR'或-C（O）NR 'CR'2-; 每个R 14独立地是C 1-4烷基，C 3-7环烷基-C 0-4烷基，Ar-C 0-4烷基，C（O）R'，CN，NO 2，SO 2 R'或C（O）OR 15; 或其药学上可接受的盐对抑制血小板聚集是有效的。

8. 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。

9. 发明授权

US5939412A Bicyclic fibrinogen antagonists 失效
标题翻译：双相纤维蛋白原拮抗剂
公开(公告)号：US5939412A
公开(公告)日：1999-08-17
申请号：US953039
申请日：1997-10-17
申请人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Thomas Wen-Fu Ku , Kenneth Allen Newlander
发明人： William Edward Bondinell , James Francis Callahan , William Francis Huffman , Richard McCulloch Keenan , Thomas Wen-Fu Ku , Kenneth Allen Newlander
IPC分类号： C07D223/16 , C07D243/14 , C07D267/14 , C07D281/10 , A61K31/55
CPC分类号： C07D223/16 , C07D243/14 , C07D267/14 , C07D281/10
摘要： Compounds of the formula: ##STR1## wherein A.sup.1 to A.sup.5 form a seven-membered ring containing one optionally substituted nitrogen atom;D.sup.1 to D.sup.4 form a substituted six membered ring, optionally containing up to two nitrogen atoms;R is preferably at least one acid containing substituent;R* is is one or more groups chosen from H, Q-C.sub.1-6 alkyl, Q-C.sub.1-6 oxoalkyl, Q-C.sub.2-6 alkenyl, Q-C.sub.3-4 oxoalkenyl, Q-C.sub.3-4 oxoalkynyl, Q-C.sub.2-4 alkynyl, C.sub.3-6 cycloalkyl, Ar or Het;Q is H, C.sub.3-6 cycloalkyl, Het or Ar;R.sup.6 is preferably a basic nitrogen containing substituent; are inhibitors of platelet aggregation.
摘要翻译：下式的化合物：其中A1至A5形成含有一个任选取代的氮原子的七元环; D1至D4形成任选含有至多两个氮原子的取代六元环; R优选为至少一种含酸取代基; R *是一个或多个选自H，Q-C 1-6烷基，Q-C 1-6氧基烷基，Q-C 2-6烯基，Q-C 3-4烯基，Q-C 3-4氧代炔基，Q-C 2-4亚炔基， 6环烷基，Ar或Het; Q是H，C 3-6环烷基，Het或Ar; R6优选为碱性含氮取代基; 是血小板聚集的抑制剂。

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