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公开(公告)号:US4057561A
公开(公告)日:1977-11-08
申请号:US770433
申请日:1977-02-22
申请人: Andor Furst , Jurg Gutzwiller , Marcel Muller , Rudolf Wiechert , Ulrich Eder , Gunter Neef
发明人: Andor Furst , Jurg Gutzwiller , Marcel Muller , Rudolf Wiechert , Ulrich Eder , Gunter Neef
IPC分类号: C07J63/00 , C07C49/48 , C07C69/02 , C07D309/22
CPC分类号: C07J63/008
摘要: D-homosteroids of the formula ##STR1## WHEREIN R.sup.3.alpha. is hydrogen, R.sup.3.beta. is hydroxy, lower alkanoyloxy or aroyloxy and R.sup.3.alpha. and R.sup.3.beta. taken together are oxo; R.sup.17a.alpha. is hydrogen, lower alkyl, ethynyl, vinyl, allyl, methallyl, propadienyl, 1-propynyl, butadiynyl or chloroethynyl; R.sup.17a.beta. is hydrogen, alkanoyl, aroyl, lower alkyl, cycloalkyl-lower-alkyl, benzyl, furfuryl or tetrahydropyranyl; R.sup.18 is hydrogen or methyl and the dotted line in the C-ring denotes an additional carbon to carbon bond in the 11,12-position andProcesses for the preparation thereof are disclosed.The D-homosteroids of the present invention are useful as ovulation inhibitors and androgenic/anabolic agents.
摘要翻译: 式中的β-均质甾族化合物,其中R3a是氢,R3β是羟基,低级烷酰氧基或芳酰氧基,R3a和R3β一起是氧代; R17a是氢,低级烷基,乙炔基,乙烯基,烯丙基,甲代烯丙基,丙炔基,1-丙炔基,丁二炔基或氯乙炔基; R17aβ是氢,烷酰基,芳酰基,低级烷基,环烷基 - 低级 - 烷基,苄基,糠基或四氢吡喃基; R18是氢或甲基,C环中的虚线表示11,12位中的另外的碳 - 碳键,并且其制备方法被公开。
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公开(公告)号:US4361578A
公开(公告)日:1982-11-30
申请号:US321954
申请日:1981-11-16
申请人: Leo Alig , Andor Furst , Peter Keller , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
发明人: Leo Alig , Andor Furst , Peter Keller , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
CPC分类号: C07J63/008
摘要: The invention is directed to 3-oxo-D-homosteroids and derivatives thereof which are useful as antiantigens.
摘要翻译: 本发明涉及可用作抗原的3-氧代-D-类固醇类及其衍生物。
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公开(公告)号:US4252729A
公开(公告)日:1981-02-24
申请号:US36477
申请日:1979-05-07
申请人: Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
发明人: Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
CPC分类号: C07J3/005
摘要: The present disclosure is concerned with 9.alpha.-chloro-17-(m-iodobenzyloxy) steroids and a process for their manufacture. The subject compounds are useful as intermediates in the synthesis of pharmacologically-active substances and have themselves been found to exhibit pharmacological activity.
摘要翻译: 本公开涉及9α-氯代-17-(间碘苄氧基)类固醇及其制造方法。 本发明化合物可用作合成药理活性物质的中间体,并且已被发现具有药理活性。
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公开(公告)号:US4139716A
公开(公告)日:1979-02-13
申请号:US670211
申请日:1976-03-25
CPC分类号: C07J63/008 , C07J71/001
摘要: The present disclosure relates to D-homosteroids. More particularly, the disclosure is concerned with 19-nor-D-homopregnanes, a process for the manufacture thereof and pharmaceutical preparations containing same.
摘要翻译: 本公开内容涉及D-类固醇。 更具体地说,本公开内容涉及19-去甲-D-己内酯,其制备方法和含有它们的药物制剂。
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公开(公告)号:US4272630A
公开(公告)日:1981-06-09
申请号:US111424
申请日:1980-01-11
申请人: Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Klaus Kieslich , Rudolf Wiechert
发明人: Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Klaus Kieslich , Rudolf Wiechert
CPC分类号: C07J63/008 , C12P33/02 , C12P33/08
摘要: The present invention is directed to 3-oxo, 6,9-hydro or halo, 11-oxo or (.alpha.--H,.beta.--OH), 17a-alkanoyloxy, 17a.beta.-carboxylate D-homosteroids which are useful as antiinflammatory agents.
摘要翻译: 本发明涉及可用作抗炎剂的3-氧代,6,9-氢或卤素,11-氧代或(α-H,β-OH),17a-烷酰氧基,17β-羧酸酯D-类固醇激素。
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公开(公告)号:US4155918A
公开(公告)日:1979-05-22
申请号:US887161
申请日:1978-03-16
申请人: Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
发明人: Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
IPC分类号: C07J21/00 , C07J41/00 , C07J63/00 , C07D309/22 , C07C49/48
CPC分类号: C07J21/006 , C07J21/00 , C07J41/0038 , C07J63/008
摘要: The present disclosure relates to novel D-homosteroids. More particularly, the invention is concerned with hormonally active novel D-homosteroids, a process for the manufacture thereof and pharmaceutical preparations containing same.
摘要翻译: 本公开涉及新型D-类固醇。 更具体地,本发明涉及激素活性的新型D-类固醇激素,其制备方法和含有它们的药物制剂。
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公开(公告)号:US4131655A
公开(公告)日:1978-12-26
申请号:US898070
申请日:1978-04-20
申请人: Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
发明人: Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Rudolf Wiechert
IPC分类号: A61K31/12 , A61K31/215 , A61K31/22 , A61K31/57 , A61P29/00 , C07J63/00 , C07F9/09 , C07C49/44
CPC分类号: C07J63/008
摘要: D-homopregnanes of the formula ##STR1## wherein R.sup.6 is hydrogen, chloro, fluoro or methyl; X is .beta.-hydroxymethylene or carbonyl; R.sup.17a is hydroxy, lower alkanoyloxy or aroyloxy; R.sup.21 is hydrogen, chloro, fluoro, hydroxy, lower alkanoyloxy, aroyloxy, sulfate or phosphate; and the dotted line in the 1,2-position of the A-ring denotes an additional carbon-carbon bondAnd pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them as the active ingredient are disclosed. The D-homopregnanes of the present invention exhibit hormonal activity and are useful for the treatment of inflammation.
摘要翻译: 其中R6是氢,氯,氟或甲基的式XI的D-己内酯; X是β-羟基亚甲基或羰基; R17a是羟基,低级烷酰氧基或芳酰氧基; R21是氢,氯,氟,羟基,低级烷酰氧基,芳氧基,硫酸根或磷酸根; A环的1,2位的虚线表示另外的碳 - 碳键,并且其药学上可接受的盐,其制备方法和作为活性成分的药物组合物被公开。 本发明的D-己内酯具有激素活性,可用于治疗炎症。
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公开(公告)号:US4029692A
公开(公告)日:1977-06-14
申请号:US671381
申请日:1976-03-29
申请人: Leo Alig , Robert Nickolson , Rudolf Wiechert , Andor Furst , Klaus Kieslich , Marcel Muller , Ulrich Kerb
发明人: Leo Alig , Robert Nickolson , Rudolf Wiechert , Andor Furst , Klaus Kieslich , Marcel Muller , Ulrich Kerb
IPC分类号: A61K31/185 , A61K31/19 , A61K31/21 , A61K31/215 , A61K31/22 , A61K31/56 , A61P5/38 , A61P29/00 , C07J63/00 , C12P33/02 , C07C69/74 , C07C61/36 , C07C69/16 , C07C69/28
CPC分类号: C07J63/008 , C07J63/00 , Y10S514/87 , Y10S514/93
摘要: The present disclosure relates to steroid carboxylic acids and derivatives thereof. More particularly, the disclosure is concerned with D-homosteroid carboxylic acids and their derivatives, a process for the preparation thereof and pharmaceutical compositions containing same. The instant compounds are active endocrinal agents, especially as antiinflammatory agents.
摘要翻译: 本公开涉及类固醇羧酸及其衍生物。 更具体地,本公开涉及D-类固醇类羧酸及其衍生物,其制备方法和含有它们的药物组合物。 本发明化合物是活性内分泌剂,特别是作为抗炎剂。
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公开(公告)号:US4202841A
公开(公告)日:1980-05-13
申请号:US973336
申请日:1978-12-26
申请人: Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Klaus Kieslich , Rudolf Wiechert
发明人: Leo Alig , Andor Furst , Marcel Muller , Ulrich Kerb , Klaus Kieslich , Rudolf Wiechert
CPC分类号: C07J63/008 , C12P33/02 , C12P33/08
摘要: D-Homopregnanes of the formula ##STR1## wherein the dotted line in the 1,2-position together with the corresponding solid line denotes a single or double carbon-carbon bond; R.sup.6 is hydrogen, fluoro, chloro or methyl; R.sup.9 is hydrogen, fluoro, chloro or bromo; R.sup.11 is hydroxyl, acyloxy, fluoro or chloro; and R.sup.17a is hydroxyl or acyloxy with the proviso that when R.sup.9 is fluoro, chloro or bromo and R.sup.11 is fluoro or chloro, the atomic number of R.sup.11 is less than or equal to that of R.sup.9 ; and with the further proviso that when R.sup.6 is hydrogen, and R.sup.11 and R.sup.17a are hydroxy or when R.sup.6 is fluoro, R.sup.11 and R.sup.17a are hydroxyl and the dotted line in the 1,2-position together with the corresponding solid line denotes a single carbon-carbon bond, R.sup.9 is fluoro, chloro or bromo and processes for the preparation thereof are disclosed.
摘要翻译: 式Ⅰ的D-homopregnanes其中1,2位虚线连同相应实线表示单碳双键; R6是氢,氟,氯或甲基; R9是氢,氟,氯或溴; R11是羟基,酰氧基,氟或氯; 并且R 17a是羟基或酰氧基,条件是当R 9是氟时,氯或溴,R 11是氟或氯,R 11的原子数小于或等于R 9的原子数; 并且进一步的条件是当R6为氢时,R11和R17a为羟基或当R6为氟时,R11和R17a为羟基,1,2-位与虚线相应的实线表示单个碳 - 碳键,R9是氟,氯或溴,并且其制备方法被公开。
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公开(公告)号:US3984476A
公开(公告)日:1976-10-05
申请号:US621850
申请日:1975-10-14
CPC分类号: C07J63/008 , Y10S514/843
摘要: D-Homosteroids of the formula ##SPC1##Wherein R.sup.3 .alpha. is hydrogen, R.sup.3 .beta. is hydrogen, lower alkanoyloxy or aroyloxy and R.sup.3 .alpha. and R.sup.3 .beta. taken together are oxo; R.sup.13 is lower alkyl; R.sup.17a .beta. is hydrogen, lower alkanoyl, aroyl or lower alkyl; R.sup.17a .alpha. is hydrogen, lower alkyl, ethynyl, 1-propynyl, vinyl, chloroethynyl, butadiynyl or propadienyl and the dotted line in the A-ring denotes an additional carbon bond in either the 4,5- or 5(10)-position and processes for the preparation thereof are disclosed.The D-homosteroids of the present invention are useful as contraceptives and regulators of the female menstrual cycle.
摘要翻译: 式中的D-类固醇,其中R3为氢,R3为氢,低级烷酰氧基或芳酰基,R3和R3为一起为氧代; R 13是低级烷基; R17aβ是氢,低级烷酰基,芳酰基或低级烷基; R17aa是氢,低级烷基,乙炔基,1-丙炔基,乙烯基,氯乙炔基,丁二炔基或丙二烯基,A环中的虚线表示在4,5-或5(10) - 位中的另外的碳键, 公开了其制备方法。
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