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1. 发明申请

WO1994015932A1 NOVEL 3,4-DIARYL THIOPHENES AND ANALOGS THEREOF HAVING USE AS ANTIINFLAMMATORY AGENTS 审中-公开
标题翻译：新型3,4-DIARYL THIOPHENES及其作为抗炎剂的模拟物
公开(公告)号：WO1994015932A1
公开(公告)日：1994-07-21
申请号：PCT/US1994000466
申请日：1994-01-14
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , BERTENSHAW, Stephen, R. , COLLINS, Paul, W. , PENNING, Thomas, D. , REITZ, David, B. , ROGERS, Roland, S.
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07D333/18
CPC分类号： C07D409/04 , A61K31/341 , A61K31/365 , C07D307/38 , C07D307/58 , C07D333/16 , C07D333/18 , C07D333/28 , C07D333/38
摘要： A class of 3,4-diaryl substitued thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (I), wherein Y is selected from O, S and NR ; wherein R is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R and R are independently aryl or heteroaryl; and wherein R and R are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：一类3,4-二芳基取代的噻吩，呋喃和吡咯衍生物及其类似物，含有它们的药物组合物和使用它们治疗炎症和炎症相关疾病的方法。特别感兴趣的化合物由式（I）定义，其中Y选自O，S和NR 1; 其中R 1选自氢和低级烷基; 其中X是一个或两个选自氢，卤素，低级烷氧基羰基和羧基的取代基; 其中R 2和R 3独立地为芳基或杂芳基; 并且其中R 2和R 3在可取代的位置任选被一个或多个选自磺酰胺基，烷基磺酰基，卤素，低级烷氧基和低级烷基的基团取代; 或其药学上可接受的盐。

2. 发明申请

WO1994021602A1 UREA DERIVATIVES USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：尿素衍生物作为抗肿瘤抑制剂有用
公开(公告)号：WO1994021602A1
公开(公告)日：1994-09-29
申请号：PCT/US1994002157
申请日：1994-03-09
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , TJOENG, Foe, S. , ADAMS, Steven, P. , ZUPEC, Mark, E.
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07C279/12
CPC分类号： C07K5/06113 , A61K38/00 , C07C279/12 , C07D213/55
摘要： Novel urea derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.
摘要翻译：提供抑制血小板聚集的新型尿素衍生物。本发明还涉及使用这些衍生物的药物组合物和方法。

3. 发明申请

WO1992001477A1 POLYMERIC DRUG DELIVERY SYSTEM 审中-公开
标题翻译：聚合物药物递送系统
公开(公告)号：WO1992001477A1
公开(公告)日：1992-02-06
申请号：PCT/US1991005029
申请日：1991-07-22
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , TREMONT, Samuel, J. , COLLINS, Paul, Waddell , PERKINS, Williams, Eldredge , JONES, Peter, Hadley
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： A61K47/48
CPC分类号： C08G73/0226 , A61K31/557 , A61K47/58 , A61K47/59 , A61K47/61 , C08G73/02 , Y10S514/925 , Y10S525/923
摘要： A drug delivery system adapted to release an effective amount of a drug at pH values of about 1 to 7 without releasing a significant amount of the drug at pH values of about 7 and above, the system comprising a polymeric material and a drug covalently bonded to the polymeric material through a pH sensitive covalent bond capable of being cleaved in the pH range of 1 to about 7.
摘要翻译：一种药物递送系统，适于以约1至7的pH值释放有效量的药物，而不在大约7及更高的pH值下释放大量的药物，所述系统包含聚合物材料和共价键合到聚合物材料通过能够在1至约7的pH范围内被切割的pH敏感的共价键。

4. 发明申请

WO1995006030A1 HYDROXYETHYLAMINO SULPHONAMIDES USEFUL AS RETROVIRAL PROTEASE INHIBITORS 审中-公开
标题翻译：羟丙基氨基磺酸盐作为替代蛋白酶抑制剂有用
公开(公告)号：WO1995006030A1
公开(公告)日：1995-03-02
申请号：PCT/US1994009139
申请日：1994-08-23
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , VAZQUEZ, Michael, L. , MUELLER, Richard, A. , TALLEY, John, J. , GETMAN, Daniel, P. , DECRESCENZO, Gary, A. , FRESKOS, John, N. , BERTENSHAW, Deborah, E. , HEINTZ, Robert, M.
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07C311/29
CPC分类号： C07D213/30 , A61K38/00 , C07C311/05 , C07C311/18 , C07C311/29 , C07C311/41 , C07C317/10 , C07C317/14 , C07C323/67 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/10 , C07D213/64 , C07D213/73 , C07D213/81 , C07D213/89 , C07D215/48 , C07D233/64 , C07D239/26 , C07D277/24 , C07D277/82 , C07D307/20 , C07D307/42 , C07D307/79 , C07D317/62 , C07D333/34 , C07D405/12 , C07D417/12 , C07K5/06026 , C07K5/06139
摘要： Hydroxyethylamino sulphonamide compounds of formulae (1) and (2), wherein A, R , R , R , R , x, P and P are as defined in claims 1 and 8 are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译：式（1）和（2）的羟乙基氨基磺酰胺化合物，其中A，R 2，R 3，R 4，R 6，x，P 1和P 2定义如上在权利要求1和8中作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。

5. 发明申请

WO1994017041A1 AMIDINOPHENYL SUBSTITUTED UREA, THIOUREA OR GUANIDINO DERIVATIVES USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：氨基苯甲酸取代的尿素，硫脲或胍基衍生物作为片剂聚集抑制剂有用
公开(公告)号：WO1994017041A1
公开(公告)日：1994-08-04
申请号：PCT/US1994000511
申请日：1994-01-24
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , TSOENG, Foe, S. , TOTH, Mihaly, V. , MCMACKINS, Dudley, E. , ADAMS, Steven, P.
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07D213/55
CPC分类号： C07C279/18 , C07C275/42 , C07D213/55 , C07D317/60
摘要： The present invention relates to a class of compounds represented by formula (I) which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives. In said formula, R is preferably selected from the group consisting of hydrogen, lower alkyl, lower alkenyl radicals, lower alkynyl radicals, pyridyl and 1,3-benzodioxole; more preferably pyridyl and 1,3-benzodioxole and hydrogen; even more preferably hydrogen. W is preferably selected from the group consisting of hydrogen, lower alkyl, lower alkenyl radicals, lower alkynyl radicals; more preferably hydrogen. Z, Z' are preferably selected from the group consisting of hydrogen and lower alkyl; more preferably hydrogen. X is preferably selected from the group consisting of oxygen, sulfur or nitrogen radicals, wherein nitrogen radicals may be substituted with hydrogen or lower alkyl radicals. R', R'' are preferably selected from the group consisting of hydrogen, lower alkyl radicals, lower alkenyl radicals, monocyclic or bicyclic aromatic hydrocarbon radicals, and pyridyl; more preferably hydrogen, monocyclic aromatic hydrocarbon radicals and pyridyl.
摘要翻译：本发明涉及抑制血小板聚集的一类由式（I）表示的化合物。本发明还涉及使用这些衍生物的药物组合物和方法。在所述式中，R优选选自氢，低级烷基，低级烯基，低级炔基，吡啶基和1,3-苯并间二氧杂环戊烯; 更优选吡啶基和1,3-苯并间二氧杂环戊烯和氢; 更优选氢。 W优选选自氢，低级烷基，低级烯基，低级炔基; 更优选氢。 Z，Z'优选选自氢和低级烷基; 更优选氢。 X优选选自氧，硫或氮原子，其中氮基可以被氢或低级烷基取代。 R'，R“优选选自氢，低级烷基，低级烯基，单环或双环芳族烃基，和吡啶基; 更优选氢，单环芳族烃基和吡啶基。

6. 发明申请

WO1992020705A1 PEPTIDE MIMETIC COMPOUNDS USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：肽类化合物可用作片剂聚集抑制剂
公开(公告)号：WO1992020705A1
公开(公告)日：1992-11-26
申请号：PCT/US1992003573
申请日：1992-05-06
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , GARLAND, Robert, Bruce , MIYANO, Masateru , ZABLOCKI, Jeffery, Alan , BOVY, Philippe, Roger , MCMACKINS, Dudley, Elgin , RICO, Joseph, Gerace , TJOENG, Foe, Siong , TOTH, Mihaly, Vadkerti
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07K05/02
CPC分类号： C07D333/60 , C07C257/18 , C07D213/55 , C07D317/60
摘要： This invention relates to a compound having formula (I) or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidines derivatives.

7. 发明申请

WO1994004493A1 SULFONYLALKANOYLAMINO HYDROXYETHYLAMINO SULFONAMIDES USEFUL AS RETROVIRAL PROTEASE INHIBITORS 审中-公开
标题翻译：磺酰氨基亚氨基羟基乙氨基磺酰胺有助于抗病毒蛋白酶抑制剂
公开(公告)号：WO1994004493A1
公开(公告)日：1994-03-03
申请号：PCT/US1993007816
申请日：1993-08-24
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , VAZQUEZ, Michael, L. , MUELLER, Richard, A. , TALLEY, John, J. , GETMAN, Daniel , DECRESCENZO, Gary, A. , FRESKOS, John, N.
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07C317/44
CPC分类号： A61K31/63 , A61K31/18 , C07C317/44
摘要： Sulphonamide-containing hydroxyethylamine compounds represented by formula (I) where R, R , R , R , R , R , R , R , Y, t and x are as defined in claim 1, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译：由式（I）表示的含磺酰胺的羟乙胺化合物，其中R 1，R 2，R 2，R 3，R 4，R 6，R 20，R 21，Y t和x如权利要求1中所定义，作为逆转录病毒蛋白酶抑制剂，特别是作为HIV蛋白酶抑制剂是有效的。

8. 发明申请

WO1994004491A1 N-(ALKANOYLAMINO-2-HYDROXYPROPYL)-SULFONAMIDES USEFUL AS RETROVIRAL PROTEASE INHIBITORS 审中-公开
标题翻译：用作退行蛋白酶抑制剂的N-（亚烷基亚氨基-2-羟基丙基） - 磺酰胺
公开(公告)号：WO1994004491A1
公开(公告)日：1994-03-03
申请号：PCT/US1993007815
申请日：1993-08-25
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , VAZQUEZ, Michael, L. , MUELLER, Richard, A. , TALLEY, John, J. , GETMAN, Daniel , DECRESCENZO, Gary, A. , FRESKOS, John, N.
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07C311/18
CPC分类号： A61K31/5375 , A61K31/18 , A61K31/195 , A61K31/197 , A61K31/381 , A61K31/4406 , A61K31/4409 , C07C311/05 , C07C311/18 , C07C311/29
摘要： Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要翻译：琥珀酰氨基羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。

9. 发明申请

WO1993018058A1 PEPTIDES MIMICS USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译： PEPTIDES MIMICS有用作为平板聚集抑制剂
公开(公告)号：WO1993018058A1
公开(公告)日：1993-09-16
申请号：PCT/US1993001710
申请日：1993-03-02
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , BOVY, Philippe, Roger , GARLAND, Robert, Bruce , MIYANO, Masateru , RICO, Joseph, Gerace , ROGERS, Thomas, Edward , ZABLOCKI, Jeffery, Alan
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07K05/02
CPC分类号： C07K5/06113 , A61K38/00 , C07C257/18 , C07D209/16
摘要： This invention relates to compounds having formula (I) or 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.
摘要翻译：本发明涉及具有式（I）化合物或其药学上可接受的盐，其可用于抑制血小板聚集，这种苯基脒衍生物的药物组合物，以及通过施用这些化合物和组合物来抑制哺乳动物血小板聚集的方法。

10. 发明申请

WO1994001396A1 PHENYL AMIDINE UREA DERIVATIVES AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：苯胺类尿素衍生物作为平板聚集抑制剂
公开(公告)号：WO1994001396A1
公开(公告)日：1994-01-20
申请号：PCT/US1993005602
申请日：1993-06-16
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , TJOENG, Foe, Siong , ZABLOCKI, Jeffery, Alan
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07C275/24
CPC分类号： C07C275/24 , C07D213/55
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 including the compounds, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
摘要翻译：本发明涉及可用于抑制血小板聚集的式（I）化合物或其药学上可接受的盐，包括该化合物的药物组合物，以及通过施用这些化合物和组合物来抑制哺乳动物血小板聚集的方法。

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