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1. 发明申请

WO1995018619A1 BICYCLIC FIBRINOGEN ANTAGONISTS 审中-公开
标题翻译：双相纤维蛋白拮抗剂
公开(公告)号：WO1995018619A1
公开(公告)日：1995-07-13
申请号：PCT/US1995/000248
申请日：1995-01-09
申请人： SMITHKLINE BEECHAM CORPORATION , BONDINELL, William, Edward , CALLAHAN, James, Francis , HUFFMAN, William, Francis , KEENAN, Richard, McCulloch , KU, Thomas, Wen-Fu , NEWLANDER, Kenneth, Allen , SAMANEN, James, Martin , UZINSKAS, Irene, Nijole
发明人： BONDINELL, William, Edward , CALLAHAN, James, Francis , HUFFMAN, William, Francis , KEENAN, Richard, McCulloch , KU, Thomas, Wen-Fu , NEWLANDER, Kenneth, Allen , SAMANEN, James, Martin , UZINSKAS, Irene, Nijole
IPC分类号： A61K31/55
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 wherein A 1 is NH or CH 2 ; R is H, C 1-6 alkyl, benzyl or a carboxy protecting group; R 3 is C 1-6 alkyl, Ar- C 0-6 alkyl, C 1-6 cycloalkyl C 0-6 alkyl, or Het C 0-6 alkyl; R 6 is 4-amidino-Ar-N(CH 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; and X is H, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkthio, trifluoroalkyl, N(R') 2 , CO 2 R', CON(R') 2 , OH, F, Cl, Br or I.
摘要翻译：式（I）中的某些化合物是血小板聚集抑制剂，其中A 1是NH或CH 2; R为H，C 1-6烷基，苄基或羧基保护基; R 3是C 1-6烷基，Ar-C 1-6烷基，C 3-7环烷基C 1-6烷基或Het-C 1-6烷基; R 6是4-脒基-Ar-N（CH 3）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-（4-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- [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.

2. 发明申请

WO1996000574A1 VITRONECTIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：维生素受体拮抗剂
公开(公告)号：WO1996000574A1
公开(公告)日：1996-01-11
申请号：PCT/US1995008146
申请日：1995-06-29
申请人： SMITHKLINE BEECHAM CORPORATION , COUSINS, Russell, Donovan , KEENAN, Richard, McCulloch , KWON, Chet , MILLER, William, Henry , UZINSKAS, Irene, Nijole
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： A61K31/55
CPC分类号： C07D223/16 , C07D235/14 , C07D243/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/04
摘要： Compounds of formula (I) are disclosed which are inhibitors of the vitronectin receptor, wherein X-X' is NR -CH, NC(O)R -CH, N=C, CR =C, CHR -CH, O-CH or S-CH; R is H, C1-6alkyl or benzyl; R is (CH2)nCO2H; R is H, C1-6alkyl, Ar-C0-6alkyl, Het-C0-6 alkyl, or C3-6cycloalkyl-C0-6alkyl; R is W-U, Y-(CHR )m-U or Z-C(O); R and R are independently chosen from H, C1-6alkyl, Ar-C0-6alkyl;, Het-C0-6alkyl and C3-6cycloalkyl-C0-6alkyl; m is 1 or 2; n is 1 or 2; U is NR C(O), C(O)NR , CH=CH, CC, CH2-CH2, O-CH2, CH2-O or CH2OCONR ; W is (a), (b) or (c); R is H, OH, NO2, N(R )2, CON(R )2, CH2N(R )2, or R HN-C(=NH); Y is NH2, NHR , N(R )2, C(O)N(R )2, OH, =N-OR , (d), (e) or (f); Z is (g) or (h); R is H, N(R )2, C1-4alkyl, CON(R )2, OH, OR , or Ar-C0-4alkyl; R is H, C1-4alkyl, 2- or 3-pyridinyl, 1-, 2- or 3-piperidinyl, or 2- or 4-pyrimidinyl; and pharmaceutically acceptable salts thereof.
摘要翻译：公开了式（I）化合物，其为玻连蛋白受体的抑制剂，其中XX'为NR 1 -CH，NC（O）R 3 -CH，N = C，CR 1 = C，CHR -CH，O-CH或S-CH; R 1是H，C 1-6烷基或苄基; R 2是（CH 2）n CO 2 H; R 3是H，C 1-6烷基，Ar-C 0-6烷基，Het-C 0-6烷基或C 3-6环烷基-C 0-6烷基; R 4是W-U，Y-（CHR 5）m-U或Z-C（O）; R 5和R 6独立地选自H，C 1-6烷基，Ar-C 0-6烷基，Het-C 0-6烷基和C 3-6环烷基-C 0-6烷基; m为1或2; n为1或2; U是NR 1 C（O），C（O）NR 1，CH = CH，CC，CH 2 -CH 2，O-CH 2，CH 2 -O或CH 2 OCONR 1; W是（a），（b）或（c）; R a是H，OH，NO 2，N（R 6）2，CON（R 6）2，CH 2 N（R 6）2或R 6 HN-C（= NH） ; Y是NH 2，NHR 6，N（R 6）2，C（O）N（R 6）2，OH，= N-OR 6，（d），（e） F）; Z是（g）或（h）; R d是H，N（R 1）2，C 1-4烷基，CON（R 1）2，OH，OR 1或Ar-C 0-4烷基; R e是H，C 1-4烷基，2-或3-吡啶基，1-，2-或3-哌啶基，或2-或4-嘧啶基; 及其药学上可接受的盐。

3. 发明申请

WO1994014776A2 BICYCLIC FIBRINOGEN ANTAGONISTS 审中-公开
标题翻译：双相纤维蛋白拮抗剂
公开(公告)号：WO1994014776A2
公开(公告)日：1994-07-07
申请号：PCT/US1993012436
申请日：1993-12-21
申请人： SMITHKLINE BEECHAM CORPORATION , BONDINELL, William, Edward , CALLAHAN, James, Francis , HUFFMAN, William, Francis , KEENAN, Richard, McCulloch , KU, Thomas, Wen-Fu , NEWLANDER, Kenneth, Allen , SAMANEN, James, Martin , UZINSKAS, Irene, Nijole
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , C07D211/18 , C07D211/70 , C07D213/24 , C07D243/04 , C07D243/14 , C07D243/24 , C07D267/14 , C07D401/12 , C07D403/12 , C07D453/02
摘要： This invention relates to compounds of formulae (I), (II), (II), wherein A is O, S, N-R or CHR ; A is N-R or CHR ; R is a sidechain containing an acid or ester group; R , R and R are substituents such as H, alkyl and aryl alkyl, and R 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：本发明涉及式（I），（II），（II）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H，烷基和芳基烷基的取代基，R 6是含有氮基的侧链; 和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。

4. 发明申请

WO9414776A3 BICYCLIC FIBRINOGEN ANTAGONISTS 审中-公开
标题翻译：双相纤维蛋白拮抗剂
公开(公告)号：WO9414776A3
公开(公告)日：1994-09-01
申请号：PCT/US9312436
申请日：1993-12-21
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM EDWARD , CALLAHAN JAMES FRANCIS , HUFFMAN WILLIAM FRANCIS , KEENAN RICHARD MCCULLOCH , KU THOMAS WEN FU , NEWLANDER KENNETH ALLEN , SAMANEN JAMES MARTIN , UZINSKAS IRENE NIJOLE
发明人： BONDINELL WILLIAM EDWARD , CALLAHAN JAMES FRANCIS , HUFFMAN WILLIAM FRANCIS , KEENAN RICHARD MCCULLOCH , KU THOMAS WEN-FU , NEWLANDER KENNETH ALLEN , SAMANEN JAMES MARTIN , UZINSKAS IRENE NIJOLE
IPC分类号： A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/451 , A61K31/55 , A61K31/551 , A61P7/02 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/70 , C07D213/24 , C07D213/74 , C07D223/16 , C07D243/04 , C07D243/14 , C07D243/24 , C07D267/14 , C07D295/04 , C07D295/08 , C07D295/10 , C07D295/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D453/02
CPC分类号： C07D223/16 , C07D211/18 , C07D211/70 , C07D213/24 , C07D243/04 , C07D243/14 , C07D243/24 , C07D267/14 , C07D401/12 , C07D403/12 , C07D453/02
摘要： This invention relates to compounds of formulae (I), (II), (II), wherein A1 is O, S, N-R?1 or CHR1; A4 is N-R4 or CHR4; R2¿ is a sidechain containing an acid or ester group; R?1, 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.

5. 发明申请

WO1992005156A1 PYRIDYLTHIO OR PYRIDYLOXY ALKANOIC ACIDS 审中-公开
标题翻译：吡咯烷基或吡咯烷基亚烷基酸
公开(公告)号：WO1992005156A1
公开(公告)日：1992-04-02
申请号：PCT/US1991006494
申请日：1991-09-10
申请人： SMITHKLINE BEECHAM CORPORATION , FRAZEE, James, Simpson , GLEASON, John, Gerald , HALL, Ralph, Floyd , KINZIG, Charles, Michael , UZINSKAS, Irene, Nijole
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： C07D213/70
CPC分类号： C07D213/70 , C07D213/55
摘要： This invention relates to alkanoic acid compounds having pyridyl and arylthio or alkylthio substituents, or their oxygen analogs, which are useful as leukotriene antagonists.
摘要翻译：本发明涉及具有吡啶基和芳硫基或烷硫基取代基或其氧类似物的链烷酸化合物，其可用作白三烯拮抗剂。

6. 发明申请

WO9518619A9 BICYCLIC FIBRINOGEN ANTAGONISTS 审中-公开
标题翻译：双相纤维蛋白拮抗剂
公开(公告)号：WO9518619A9
公开(公告)日：2004-10-21
申请号：PCT/US9500248
申请日：1995-01-09
申请人： SMITHKLINE BEECHAM CORP , BONDINELL WILLIAM EDWARD , CALLAHAN JAMES FRANCIS , HUFFMAN WILLIAM FRANCIS , KEENAN RICHARD MCCULLOCH , KU THOMAS WEN-FU , NEWLANDER KENNETH ALLEN , SAMANEN JAMES MARTIN , UZINSKAS IRENE NIJOLE
发明人： BONDINELL WILLIAM EDWARD , CALLAHAN JAMES FRANCIS , HUFFMAN WILLIAM FRANCIS , KEENAN RICHARD MCCULLOCH , KU THOMAS WEN-FU , NEWLANDER KENNETH ALLEN , SAMANEN JAMES MARTIN , UZINSKAS IRENE NIJOLE
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 , C07D223/00
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 wherein A is NH or CH ; R is H, C1-6alkyl, benzyl or a carboxy protecting group; R is C1-6alkyl, Ar- C0-6alkyl, C1-6cycloalkyl C0-6alkyl, or Het C0-6alkyl; R is 4-amidino-Ar-N(CH3)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; and X is H, C1-4alkyl, C1-4 alkoxy, C1-4 alkthio, trifluoroalkyl, N(R')2, CO2R', CON(R')2, OH, F, Cl, Br or I.
摘要翻译：式（I）中的某些化合物是血小板聚集抑制剂，其中A 1是NH或CH 2; R为H，C 1-6烷基，苄基或羧基保护基; R 3是C 1-6烷基，Ar-C 1-6烷基，C 1-6环烷基C 1-6烷基或Het C 1-6烷基; R 6是4-脒基-Ar-N（CH 3）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] [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. 发明申请

WO1991017149A1 3-NAPHTHYL-3-CARBOXYALKYLTHIO OR OXY SUBSTITUTED ALKANOIC ACID LEUKOTRIENE ANTAGONISTS 审中-公开
标题翻译： 3-萘基-3-羧基乙基或氧代替的碱性酸性白蛋白拮抗剂
公开(公告)号：WO1991017149A1
公开(公告)日：1991-11-14
申请号：PCT/US1991002889
申请日：1991-04-26
申请人： SMITHKLINE BEECHAM CORPORATION , FRAZEE, James, Simpson , GLEASON, John, Gerald , HALL, Ralph, Floyd , UZINSKAS, Irene, Nijole
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： C07D257/04
CPC分类号： C07D257/04 , C07C45/46 , C07C45/56 , C07C45/565 , C07C45/68 , C07C45/71 , C07C59/66 , C07C59/68 , C07C69/76 , C07C69/94 , C07C323/56 , C07C49/697 , C07C47/546 , C07C47/55 , C07C47/548 , C07C47/575
摘要： This invention relates to alkanoic acid compounds having a naphthyl ring and thio substituents which are useful as leukotriene antagonists.
摘要翻译：本发明涉及具有萘环的链烷酸化合物和可用作白三烯拮抗剂的硫取代基。

8. 发明申请

WO1991016889A1 FIVE-MEMBERED RING ALKANOIC ACID LEUKOTRIENE ANTAGONISTS 审中-公开
标题翻译：五种环状酸性白蛋白拮抗剂
公开(公告)号：WO1991016889A1
公开(公告)日：1991-11-14
申请号：PCT/US1991002884
申请日：1991-04-26
申请人： SMITHKLINE BEECHAM CORPORATION , FRAZEE, James, Simpson , GLEASON, John, Gerald , HALL, Ralph, Floyd , UZINSKAS, Irene, Nijole
发明人： SMITHKLINE BEECHAM CORPORATION
IPC分类号： A61K31/34
CPC分类号： C07D233/64 , A61K31/38 , A61K31/415 , C07D307/54 , C07D333/24 , C07D403/06 , C07D409/06
摘要： This invention relates to alkanoic acid compounds having a 5-membered heterocyclic ring and a thio substituent which are useful as leukotriene antagonists.
摘要翻译：本发明涉及可用作白三烯拮抗剂的具有5元杂环和硫代取代基的链烷酸化合物。

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