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公开(公告)号:US5670512A
公开(公告)日:1997-09-23
申请号:US633990
申请日:1996-04-17
申请人: James E. Audia , Kenneth S. Hirsch , Charles D. Jones , David E. Lawhorn , Loretta A. McQuaid , Leland O. Weigel
发明人: James E. Audia , Kenneth S. Hirsch , Charles D. Jones , David E. Lawhorn , Loretta A. McQuaid , Leland O. Weigel
IPC分类号: A61K31/47 , A61K31/435 , A61K31/473 , A61P13/08 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , C07C45/00 , C07C45/51 , C07C45/56 , C07C49/697 , C07C49/737 , C07C49/747 , C07C49/755 , C07C205/45 , C07C229/46 , C07D211/00 , C07D221/06 , C07D221/10 , C12N9/99 , A61K31/345
CPC分类号: C07D221/10 , C07C227/16 , C07C229/46 , C07C41/16 , C07C45/00 , C07C45/513 , C07C45/562 , C07C49/697 , C07C49/747 , C07C49/755 , C07C59/255 , C07C2102/10 , C07C2103/70
摘要: This invention relates to hexa- and octaahydrobenzo�f!quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
摘要翻译: 本发明涉及六氢和八氢苯并[f]喹啉-3-酮,含有这些化合物的药物制剂及其用作类固醇5α-还原酶抑制剂的方法。
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公开(公告)号:US5334767A
公开(公告)日:1994-08-02
申请号:US52960
申请日:1993-04-23
申请人: James E. Audia , Kenneth S. Hirsch , Charles D. Jones , David E. Lawhorn , Loretta A. McQuaid , Leland O. Weigel
发明人: James E. Audia , Kenneth S. Hirsch , Charles D. Jones , David E. Lawhorn , Loretta A. McQuaid , Leland O. Weigel
IPC分类号: A61K31/47 , A61K31/435 , A61K31/473 , A61P13/08 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , C07C45/00 , C07C45/51 , C07C45/56 , C07C49/697 , C07C49/737 , C07C49/747 , C07C49/755 , C07C205/45 , C07C229/46 , C07D211/00 , C07D221/06 , C07D221/10 , C12N9/99 , C07C49/792 , C07C49/796 , C07C49/807
CPC分类号: C07D221/10 , C07C227/16 , C07C229/46 , C07C41/16 , C07C45/00 , C07C45/513 , C07C45/562 , C07C49/697 , C07C49/747 , C07C49/755 , C07C59/255 , C07C2102/10 , C07C2103/70
摘要: This invention relates to hexa- and octahydrobenzo [f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
摘要翻译: 本发明涉及六氢和八氢苯并[f]喹啉-3-酮,含有这些化合物的药物制剂及其用作类固醇5α-还原酶抑制剂的方法。
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公开(公告)号:US5495021A
公开(公告)日:1996-02-27
申请号:US223884
申请日:1994-04-06
IPC分类号: A61K31/47 , A61K31/435 , A61K31/473 , A61P13/08 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , C07C45/00 , C07C45/51 , C07C45/56 , C07C49/697 , C07C49/737 , C07C49/747 , C07C49/755 , C07C205/45 , C07C229/46 , C07D211/00 , C07D221/06 , C07D221/10 , C12N9/99 , C07D215/227 , C07D215/38
CPC分类号: C07D221/10 , C07C227/16 , C07C229/46 , C07C41/16 , C07C45/00 , C07C45/513 , C07C45/562 , C07C49/697 , C07C49/747 , C07C49/755 , C07C59/255 , C07C2102/10 , C07C2103/70
摘要: This invention relates to hexa- and octahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
摘要翻译: 本发明涉及六氢和八氢苯并[f]喹啉-3-酮,含有这些化合物的药物制剂及其用作类固醇5α-还原酶抑制剂的方法。
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公开(公告)号:US5541190A
公开(公告)日:1996-07-30
申请号:US445806
申请日:1995-05-22
申请人: James E. Audia , Kenneth S. Hirsch , Charles D. Jones , David E. Lawhorn , Loretta A. McQuaid , Leland O. Weigel
发明人: James E. Audia , Kenneth S. Hirsch , Charles D. Jones , David E. Lawhorn , Loretta A. McQuaid , Leland O. Weigel
IPC分类号: A61K31/47 , A61K31/435 , A61K31/473 , A61P13/08 , A61P17/00 , A61P17/08 , A61P17/10 , A61P17/14 , A61P35/00 , A61P43/00 , C07C45/00 , C07C45/51 , C07C45/56 , C07C49/697 , C07C49/737 , C07C49/747 , C07C49/755 , C07C205/45 , C07C229/46 , C07D211/00 , C07D221/06 , C07D221/10 , C12N9/99 , C07D215/227 , C07D215/12
CPC分类号: C07D221/10 , C07C227/16 , C07C229/46 , C07C41/16 , C07C45/00 , C07C45/513 , C07C45/562 , C07C49/697 , C07C49/747 , C07C49/755 , C07C59/255 , C07C2102/10 , C07C2103/70
摘要: This invention relates to hexa- and octahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
摘要翻译: 本发明涉及六氢和八氢苯并[f]喹啉-3-酮,含有这些化合物的药物制剂及其用作类固醇5α-还原酶抑制剂的方法。
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公开(公告)号:US5574160A
公开(公告)日:1996-11-12
申请号:US443994
申请日:1995-05-18
IPC分类号: C07C211/42 , C07C319/20 , C07C323/38 , C07D221/10 , C07D215/227
CPC分类号: C07C211/42 , C07C319/20 , C07D221/10 , C07C2102/10
摘要: A 1-pot process for preparing 10b-methyl-3-oxo-benzo[f] quinolines.
摘要翻译: 制备10b-甲基-3-氧代 - 苯并[f]喹啉的1釜法。
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公开(公告)号:US5239069A
公开(公告)日:1993-08-24
申请号:US918196
申请日:1992-07-22
申请人: Leland O. Weigel
发明人: Leland O. Weigel
IPC分类号: C07C231/10 , C07D205/085 , C07D403/04 , C07D403/12 , C07D405/14 , C07D463/00 , C07D501/04
CPC分类号: C07D403/04 , C07C231/10 , C07D205/085 , C07D403/12 , C07D405/14 , Y02P20/55
摘要: The invention provides compounds of the formula ##STR1## wherein R* is a group of the formula ##STR2## wherein R and R.sup.0 are individually C.sub.1 -C.sub.6 alkyl groups or together form a ring consisting of the nitrogen atom to which they are attached and two to seven carbon atoms, said ring optionally substituted by one or more C.sub.1 -C.sub.6 alkyl and/or C.sub.1 -C.sub.6 substituted alkyl groups;Q and Q' are individually hydrogen, C.sub.1 -C.sub.6 alkyl, or when taken together form a divalent radical of the formula --CH.dbd.CH--CH.dbd.CH--;A is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 substituted alkyl, --S--(C.sub.1 -C.sub.6 alkyl)CO.sub.2 R", or --CH.sub.2 (C.sub.1 -C.sub.6 alkyl) CO.sub.2 R" wherein R"is hydrogen or a carboxy-protecting group;A' is hydrogen, an amide-protecting group, or a group of the formula --CH.sub.2 CO.sub.2 R".
摘要翻译: 本发明提供式IMA的化合物,其中R *是下式的基团:其中R和R0分别是C1-C6烷基或一起形成由它们连接的氮原子组成的环,两个 所述环任选地被一个或多个C 1 -C 6烷基和/或C 1 -C 6取代的烷基取代; Q和Q'分别为氢,C 1 -C 6烷基,或者一起形成式-CH = CH-CH = CH-的二价基团; A是C 1 -C 6烷基,C 1 -C 6取代的烷基,-S-(C 1 -C 6烷基)CO 2 R“或-CH 2(C 1 -C 6烷基)CO 2 R”,其中R“是氢或羧基保护基 ; A'是氢,酰胺保护基或式-CH 2 CO 2 R“的基团。
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公开(公告)号:US4831145A
公开(公告)日:1989-05-16
申请号:US197712
申请日:1988-05-23
IPC分类号: C07D215/20 , C07D471/04
CPC分类号: C07D471/04 , C07D215/20
摘要: This invention provides a process for preparing trans 2-aminopyrimido[4,5-g]quinolines employing novel intermediates.
摘要翻译: 本发明提供了使用新型中间体制备反式-2-氨基嘧啶并[4,5-g]喹啉的方法。
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公开(公告)号:US4764609A
公开(公告)日:1988-08-16
申请号:US845916
申请日:1986-03-31
IPC分类号: A61K31/505 , A61P25/00 , A61P43/00 , C07D215/12 , C07D215/20 , C07D239/74 , C07D471/04
CPC分类号: C07D471/04 , C07D215/20
摘要: This invention provides a process for preparing trans 2-aminopyrimido[4,5-g]quinolines employing novel intermediates.
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公开(公告)号:US5296615A
公开(公告)日:1994-03-22
申请号:US12109
申请日:1993-02-01
申请人: Leland O. Weigel
发明人: Leland O. Weigel
IPC分类号: C07B55/00 , C07C303/30 , C07C309/65 , C07C309/67 , C07C309/73 , C07D301/02 , C07D303/48 , C07D307/33 , C07D307/32
CPC分类号: C07D307/33 , C07C303/30 , C07D303/48
摘要: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.
摘要翻译: 通过基于催化的醇解由新的二氢-3R-取代的磺酰氧基-4R-羟基-2-(3H)呋喃酮制备手性环氧丁酸酯。 产品手性环氧丁酸酯是合成1-咔唑-1-脱氢头孢烯抗生素的有用中间体。
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公开(公告)号:US5183910A
公开(公告)日:1993-02-02
申请号:US770676
申请日:1991-10-03
申请人: Leland O. Weigel
发明人: Leland O. Weigel
IPC分类号: C07C303/30 , C07C309/65 , C07C309/73 , C07D303/48 , C07D307/33
CPC分类号: C07D307/33 , C07C303/30 , C07D303/48
摘要: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.
摘要翻译: 通过基于催化的醇解由新的二氢-3R-取代的磺酰氧基-4R-羟基-2-(3H)呋喃酮制备手性环氧丁酸酯。 产品手性环氧丁酸酯是合成1-咔唑-1-脱氢头孢烯抗生素的有用中间体。
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