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1.发明授权Process for preparing 2-substituted benzo �B! Thiophene compounds and intermediates thereof 失效制备2-取代苯并[B]噻吩化合物及其中间体的方法
公开(公告)号：US5712390A
公开(公告)日：1998-01-27
申请号：US549596
申请日：1995-10-27
IPC分类号： C07D333/52 , C07D333/54 , C07D333/56 , C07D333/62 , C07D401/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07F5/02 , C07D409/12 , C07D413/12
CPC分类号： C07D333/54 , C07D333/56 , C07D333/62 , C07F5/025 , Y02P20/55
摘要： The present invention provides processes for preparing compounds of formula I ##STR1## and for preparing compounds of formula VII ##STR2## Also provided are processes for preparing compounds of formula VII in addition to intermediates of formula IX ##STR3## wherein R.sup.1' is --OH, or --OR.sup.3, in which R.sup.3 is a hydroxy protecting group; and Z is bromo, iodo, triflate, or --B(OH).sub.2.
摘要翻译： 本发明提供制备式I化合物的方法和用于制备式VII化合物的方法VII还提供除了式IX的中间体以外制备式VII化合物的方法，其中R1' 是-OH或-OR 3，其中R 3是羟基保护基; 和Z是溴，碘，三氟甲磺酸酯或-B（OH）2。
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2.发明授权Process for preparing 2-substituted benzo�B!thiophene compounds and intermediates thereof 失效制备2-取代的苯并[B]噻吩化合物及其中间体的方法
公开(公告)号：US5710285A
公开(公告)日：1998-01-20
申请号：US549595
申请日：1995-10-27
IPC分类号： C07D333/52 , C07D333/54 , C07D333/56 , C07D333/62 , C07D401/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07F5/02 , C07D333/06 , C07D333/16
CPC分类号： C07D333/54 , C07D333/56 , C07D333/62 , C07F5/025 , Y02P20/55
摘要： The present invention provides useful intermediates for preparing 2-(substituted phenyl)benzothiophenes compounds said intermediates having the structure ##STR1## wherein R.sup.1 ' is --OH, or --OR.sup.3, in which R.sup.3 is a hydroxy protecting group; and Z is bromo, iodo, triflate, or --B(OH).sub.2 with the proviso that when Z is bromo or iodo, R1' is not alkoxy.
摘要翻译： 本发明提供用于制备2-（取代苯基）苯并噻吩化合物的有用中间体，所述中间体具有结构单元IX，其中R 1'是-OH或-OR 3，其中R 3是羟基保护基; 并且Z是溴，碘，三氟甲磺酸酯或-B（OH）2，条件是当Z是溴或碘时，R 1'不是烷氧基。
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3.发明授权Process for preparing 2-substituted benzo[b]thiophene compounds and intermediates thereof 失效制备2-取代的苯并[b]噻吩化合物的方法及其中间体
公开(公告)号：US5614639A
公开(公告)日：1997-03-25
申请号：US415014
申请日：1995-03-31
IPC分类号： C07D333/52 , C07D333/54 , C07D333/56 , C07D333/62 , C07D401/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07F5/02 , C07D333/72 , C07D405/00
CPC分类号： C07D333/54 , C07D333/56 , C07D333/62 , C07F5/025 , Y02P20/55
摘要： The present invention provides processes for preparing 2-substituted benzo[b]thiophene compounds, some of which are useful as intermediates for preparing pharmaceutically-active compounds and others which are useful, inter alia, for the treatment of osteoporosis in postmenopausal women.
摘要翻译： 本发明提供了制备2-取代的苯并[b]噻吩化合物的方法，其中一些可用作制备药物活性化合物的中间体和其它用于治疗绝经后妇女骨质疏松症的其它化合物。
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公开(公告)号：US6020362A
公开(公告)日：2000-02-01
申请号：US47285
申请日：1998-03-24
申请人： Matthew J. Fisher , Anne Marie Happ , Joseph A. Jakubowski , Michael Dean Kinnick , Allen D. Kline , Michael John Martinelli , John Michael Morin, Jr. , Michael Paal , Gerd Ruhter , Kenneth James Ruterbories , Daniel J. Sall , Theo Schotten , Marshall A. Skelton , Wolfgang Stenzel , Robert Theodore Vasileff
发明人： Matthew J. Fisher , Anne Marie Happ , Joseph A. Jakubowski , Michael Dean Kinnick , Allen D. Kline , Michael John Martinelli , John Michael Morin, Jr. , Michael Paal , Gerd Ruhter , Kenneth James Ruterbories , Daniel J. Sall , Theo Schotten , Marshall A. Skelton , Wolfgang Stenzel , Robert Theodore Vasileff
IPC分类号： C07D487/04 , A61K31/195 , A61K31/215 , A61K31/335 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/47 , A61K31/472 , A61K31/495 , A61P7/02 , A61P9/10 , C07C257/18 , C07C257/20 , C07C271/64 , C07D211/22 , C07D211/32 , C07D211/34 , C07D213/82 , C07D217/04 , C07D217/06 , C07D217/24 , C07D221/00 , C07D311/22 , C07D311/58 , C07D311/66 , C07D311/70 , C07D319/16 , C07D333/38 , C07D401/12 , C07D405/06 , C07D405/12 , C07D491/052 , C07D497/04 , G03F7/20 , C07D311/04
CPC分类号： C07D211/34 , C07C257/18 , C07C271/64 , C07D211/22 , C07D213/82 , C07D217/04 , C07D217/06 , C07D217/24 , C07D311/22 , C07D311/58 , C07D333/38 , C07D401/12 , C07D405/06 , C07D405/12 , C07C2102/10
摘要： This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
摘要翻译： 本发明涉及具有由两个稠合的六元环形成的核的某些二环化合物，例如苯并吡喃，异喹啉，异喹诺酮，四氢萘，二氢萘或四氢萘酮，其被碱性和酸性官能团所取代，其可用于抑制血小板聚集 。
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公开(公告)号：US5618843A
公开(公告)日：1997-04-08
申请号：US255821
申请日：1994-07-08
申请人： Matthew J. Fisher , Anne M. Happ , Joseph A. Jakubowski , Michael D. Kinnick , Allen D. Kline , John M. Morin, Jr. , Daniel J. Sall , Marshall A. Skelton , Robert T. Vasileff
发明人： Matthew J. Fisher , Anne M. Happ , Joseph A. Jakubowski , Michael D. Kinnick , Allen D. Kline , John M. Morin, Jr. , Daniel J. Sall , Marshall A. Skelton , Robert T. Vasileff
IPC分类号： C07D487/04 , A61K31/015 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/335 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/44 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61P7/02 , A61P9/10 , C07C257/18 , C07C271/64 , C07D211/22 , C07D211/34 , C07D213/82 , C07D217/04 , C07D217/06 , C07D217/24 , C07D221/00 , C07D311/22 , C07D311/58 , C07D333/38 , C07D401/12 , C07D405/06 , C07D405/12 , C07D491/052 , C07D497/04 , G03F7/20 , C07C251/02
CPC分类号： C07C271/64 , C07C257/18 , C07D211/22 , C07D211/34 , C07D213/82 , C07D217/04 , C07D217/06 , C07D217/24 , C07D311/22 , C07D311/58 , C07D333/38 , C07D401/12 , C07D405/06 , C07D405/12 , C07C2102/10
摘要： This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
摘要翻译： 本发明涉及具有由两个稠合的六元环形成的核的某些双环化合物，例如异喹啉，异喹啉酮，四氢萘，二氢萘或四氢萘酮，其被碱性和酸性官能团所取代，其可用于抑制血小板聚集。
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公开(公告)号：US5488037A
公开(公告)日：1996-01-30
申请号：US206499
申请日：1994-03-04
申请人： Daniel J. Sall , Robert T. Shuman
发明人： Daniel J. Sall , Robert T. Shuman
IPC分类号： A61K38/55 , A61P7/02 , C07D207/16 , C07D401/06 , C07D403/06 , C07K5/023 , A61K38/00 , C07D279/10 , C07D279/12 , C07D417/00
CPC分类号： C07D401/06 , C07D207/16 , C07D403/06
摘要： This invention relates to L-Arginine aldehyde derivatives, pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.
摘要翻译： 本发明涉及L-精氨酸醛衍生物，含有这些化合物的药物制剂及其用作凝血酶抑制剂，凝血抑制剂和血栓栓塞障碍剂的方法。
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公开(公告)号：US06448269B1
公开(公告)日：2002-09-10
申请号：US09883639
申请日：2001-06-18
申请人： Matthew J. Fisher , Anne Marie Happ , Joseph A. Jakubowski , Michael Dean Kinnick , Allen D. Kline , Michael John Martinelli , John Michael Morin, Jr. , Michael Paal , Gerd Rühter , Kenneth James Ruterbories , Daniel J. Sall , Theo Schotten , Marshall A. Skelton , Wolfgang Stenzel , Robert Theodore Vasileff
发明人： Matthew J. Fisher , Anne Marie Happ , Joseph A. Jakubowski , Michael Dean Kinnick , Allen D. Kline , Michael John Martinelli , John Michael Morin, Jr. , Michael Paal , Gerd Rühter , Kenneth James Ruterbories , Daniel J. Sall , Theo Schotten , Marshall A. Skelton , Wolfgang Stenzel , Robert Theodore Vasileff
IPC分类号： C07D40112
CPC分类号： C07D311/22 , C07C257/18 , C07C271/64 , C07C2602/10 , C07D211/22 , C07D211/34 , C07D213/82 , C07D217/04 , C07D217/06 , C07D217/24 , C07D311/58 , C07D333/38 , C07D401/12 , C07D405/06 , C07D405/12
摘要： This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
摘要翻译： 本发明涉及具有由两个稠合的六元环形成的核的某些二环化合物，例如苯并吡喃，异喹啉，异喹诺酮，四氢萘，二氢萘或四氢萘酮，其被碱性和酸性官能团所取代，其可用于抑制血小板聚集 。
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公开(公告)号：US5508292A
公开(公告)日：1996-04-16
申请号：US422288
申请日：1995-04-14
申请人： Daniel J. Sall , Gerald F. Smith
发明人： Daniel J. Sall , Gerald F. Smith
IPC分类号： C12N9/99 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/445 , A61K31/4535 , A61K31/55 , A61P7/02 , A61P43/00 , C07D333/56
CPC分类号： A61K31/4535 , A61K31/40 , A61K31/4025 , A61K31/445 , A61K31/55
摘要： A method of inhibiting thrombin and its attending diseases and conditions comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidino, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
摘要翻译： 一种抑制凝血酶及其主要疾病和病症的方法，包括向需要治疗的人施用有效量的具有式（I）的化合物，其中R 1和R 3独立地是氢，-CH 3，其中 Ar是任选取代的苯基; R2选自吡咯烷子基，六亚甲基氨基和哌啶子基; 或其药学上可接受的盐的溶剂合物。
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公开(公告)号：US6137002A
公开(公告)日：2000-10-24
申请号：US710823
申请日：1996-09-23
申请人： Matthew J. Fisher , Anne Marie Happ , Joseph A. Jakubowski , Michael Dean Kinnick , Allen D. Kline , John Michael Morin, Jr. , Daniel J. Sall , Marshall A. Skelton , Robert Theodore Vasileff
发明人： Matthew J. Fisher , Anne Marie Happ , Joseph A. Jakubowski , Michael Dean Kinnick , Allen D. Kline , John Michael Morin, Jr. , Daniel J. Sall , Marshall A. Skelton , Robert Theodore Vasileff
IPC分类号： C07D487/04 , A61K31/195 , A61K31/215 , A61K31/335 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/44 , A61K31/47 , A61K31/472 , A61K31/495 , A61P7/02 , A61P9/10 , C07C257/18 , C07C271/64 , C07D211/22 , C07D211/34 , C07D213/82 , C07D217/04 , C07D217/06 , C07D217/24 , C07D221/00 , C07D311/22 , C07D311/58 , C07D333/38 , C07D401/12 , C07D405/06 , C07D405/12 , C07D491/052 , C07D497/04 , G03F7/20 , C07C251/02
CPC分类号： C07C257/18 , C07C271/64 , C07D211/22 , C07D211/34 , C07D213/82 , C07D217/04 , C07D217/06 , C07D217/24 , C07D311/22 , C07D311/58 , C07D333/38 , C07D401/12 , C07D405/06 , C07D405/12 , C07C2102/10
摘要： This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
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公开(公告)号：US5731324A
公开(公告)日：1998-03-24
申请号：US376191
申请日：1995-01-19
申请人： Matthew J. Fisher , Anne Marie Happ , Joseph A. Jakubowski , Michael Dean Kinnick , Allen D. Kline , Michael John Martinelli , John Michael Morin, Jr. , Michael Paal , Gerd Ruhter , Kenneth James Ruterbories , Daniel J. Sall , Theo Schotten , Marshall A. Skelton , Wolfgang Stenzel , Robert Theodore Vasileff
发明人： Matthew J. Fisher , Anne Marie Happ , Joseph A. Jakubowski , Michael Dean Kinnick , Allen D. Kline , Michael John Martinelli , John Michael Morin, Jr. , Michael Paal , Gerd Ruhter , Kenneth James Ruterbories , Daniel J. Sall , Theo Schotten , Marshall A. Skelton , Wolfgang Stenzel , Robert Theodore Vasileff
IPC分类号： C07D487/04 , A61K31/195 , A61K31/215 , A61K31/335 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/47 , A61K31/472 , A61K31/495 , A61P7/02 , A61P9/10 , C07C257/18 , C07C257/20 , C07C271/64 , C07D211/22 , C07D211/32 , C07D211/34 , C07D213/82 , C07D217/04 , C07D217/06 , C07D217/24 , C07D221/00 , C07D311/22 , C07D311/58 , C07D311/66 , C07D311/70 , C07D319/16 , C07D333/38 , C07D401/12 , C07D405/06 , C07D405/12 , C07D491/052 , C07D497/04 , G03F7/20 , C07D311/02
CPC分类号： C07D211/34 , C07C257/18 , C07C271/64 , C07D211/22 , C07D213/82 , C07D217/04 , C07D217/06 , C07D217/24 , C07D311/22 , C07D311/58 , C07D333/38 , C07D401/12 , C07D405/06 , C07D405/12 , C07C2102/10
摘要： This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
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