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31. 发明授权

US4118488A 4-Androsten-3-ones and process for the preparation thereof 失效
标题翻译： 4-雄甾-3-酮及其制备方法
公开(公告)号：US4118488A
公开(公告)日：1978-10-03
申请号：US773982
申请日：1977-03-03
申请人： Rainer Philippson , Bernhard Krieger , Jorge Casals-Stenzel , Ulrich Kerb , Wolfgang Losert , Klaus Prezewowsky , Rudolf Wiechert , Dieter Bittler
发明人： Rainer Philippson , Bernhard Krieger , Jorge Casals-Stenzel , Ulrich Kerb , Wolfgang Losert , Klaus Prezewowsky , Rudolf Wiechert , Dieter Bittler
IPC分类号： A61K31/565 , A61P7/10 , C07J1/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J53/00 , C07J9/00 , A61K31/56
CPC分类号： C07J1/0081 , C07J1/0033 , C07J31/003 , C07J41/0038 , C07J43/003 , C07J51/00 , C07J53/00 , C07J53/007
摘要： 4-Androsten-3-ones of the formula ##STR1## wherein R.sub.1 is hydrogen or the acyl radical of an organic or inorganic acid, R.sub.2 is hydrogen, alkyl, or the acyl radical of an organic or inorganic acid, R.sub.3 is methyl or ethyl, R.sub.4 is hydrogen or methyl, ##STR2## and R.sub.5 is lower alkyl, have diuretic activity.
摘要翻译：其中R 1是氢或有机或无机酸的酰基，R 2是有机或无机酸的氢，烷基或酰基，R 3是甲基或乙基 R4是氢或甲基，R5是低级烷基，具有利尿活性。

32. 发明授权

US4029777A 18-Methyl-19-nor-20-ketopregnanes and process for the preparation thereof 失效
标题翻译： 18-甲基-19-去甲-20-酮戊二酸及其制备方法
公开(公告)号：US4029777A
公开(公告)日：1977-06-14
申请号：US602098
申请日：1975-08-05
申请人： Otto Engelfried , Ulrich Kerb , Rudolf Wiechert , Helmut Wachtel , Dieter Palenschat , Reinhard Horowski , Gert Paschelke , Wolfgang Kehr
发明人： Otto Engelfried , Ulrich Kerb , Rudolf Wiechert , Helmut Wachtel , Dieter Palenschat , Reinhard Horowski , Gert Paschelke , Wolfgang Kehr
IPC分类号： C07J7/00 , C07J5/00 , A61K31/56
CPC分类号： C07J7/002
摘要： 18-Methyl-19-nor-20-keto steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 collectively are an oxygen atom, or each is hydrogen, or one of R.sub.1 and R.sub.2 is hydrogen and the other is hydroxy, and R.sub.3 is a ketonic oxygen atom or two hydrogen atoms, possess CNS-depressant activity, especially anesthetic-narcotic activity.
摘要翻译：其中R 1和R 2共同为氧原子，或各自为氢，或者R 1和R 2中的一个为氢，另一个为羟基，R 3为酮氧原子或两个氢原子，具有CNS抑制活性，特别是麻醉药物的麻醉活性。

33. 发明授权

US5529993A 14.alpha., 17.alpha.-ethano-16.alpha.-hydroxy-estratrienes 失效
标题翻译： 14α，17α-乙酰基-16α-羟基 - 雌三烯
公开(公告)号：US5529993A
公开(公告)日：1996-06-25
申请号：US619947
申请日：1990-11-29
申请人： Gerald Kirsch , Gunter Neef , Henry Laurent , Rudolf Wiechert , James Bull , Peter Esperling , Walter Elger , Sybille Beier
发明人： Gerald Kirsch , Gunter Neef , Henry Laurent , Rudolf Wiechert , James Bull , Peter Esperling , Walter Elger , Sybille Beier
IPC分类号： A61K31/565 , A61P5/00 , C07J1/00 , C07J53/00
CPC分类号： C07J53/002 , Y10S514/843 , Y10S514/935
摘要： A 14.alpha.,17.alpha.-bridged estratriene of formula I ##STR1## wherein (a) OR.sup.3 is in .alpha.-positionR.sup.1, R.sup.2 and R.sup.3, each independently are (i) hydrogen, (ii) ##STR2## in which R.sup.4 is an organic radical with up to 11 carbon atoms or (iii) --(CH.sub.2).sub.n COOH wherein n=1-4, or (iv) R.sup.1 is a benzyl, C.sub.1 -C.sub.8 alkyl or C.sub.3 -C.sub.5 cycloalkyl, or(b) OR.sup.3 is in .beta.-positionR.sup.1, R.sup.2 and R.sup.3, each independently are (i) hydrogen, (ii) an acyl group with 1 to 12 carbon atoms or (iii) R.sup.1 is C.sub.1 -C.sub.8 alkyl, and in both (a) and (b) A--B is an etheno or ethano bridge.
摘要翻译：式（I）的14α，17α-桥羟基雌三烯，其中（a）OR 3在α位R1，R2和R3各自独立地为（i）氢，（ii）其中或（iv）R 1是苄基，C 1 -C 8烷基或C 3 -C 5环烷基，或者（b）R 4是具有至多11个碳原子的有机基团或（iii） - （CH 2）n COOH，其中n = OR 3为β位R1，R2和R3各自独立地为（i）氢，（ii）具有1至12个碳原子的酰基或（iii）R 1为C 1 -C 8烷基，并且（a）和（b）AB是乙烯或乙醇桥。

34. 发明授权

US5095129A 19,11 .beta.-bridged steroids, their manufacture and pharmaceutical preparations containing them 失效
标题翻译： 19,11（BETA） - 混合型STEROIDS，其制造和含有它们的药物制剂
公开(公告)号：US5095129A
公开(公告)日：1992-03-10
申请号：US283632
申请日：1988-12-09
申请人： Eckhard Ottow , Rudolf Wiechert , Gunter Neef , Sybille Beier , Walter Elger , David A. Henderson
发明人： Eckhard Ottow , Rudolf Wiechert , Gunter Neef , Sybille Beier , Walter Elger , David A. Henderson
IPC分类号： A61K31/565 , A61K31/58 , A61P5/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J53/00 , C07J63/00 , C07J71/00
CPC分类号： C07J71/0063 , C07J21/006 , C07J31/006 , C07J41/0038 , C07J53/002 , C07J71/0005 , C07J71/0047
摘要： New 19,11.beta.-bridged steroids of the general formula I ##STR1## where R.sup.1 stands for a methyl or ethyl radical,R.sup.2 for a hydrogen or chlorine atom or a C.sub.1 -C.sub.4 -alkyl radical,B and G, which are the same or different, respectively for a hydrogen atom, a C.sub.1 -C.sub.4 -alkyl radical or, together, for a second bond between the carbon atoms 6 and 7,B and R.sup.2 together for a methylene or an ethylene group,Z for the radical of a pentagonal or hexagonal ring, which is possibly substituted and possibly unsaturated,V stands for a possibly substituted carbocyclic or heterocyclic aryl radical,the ring A for ##STR2## M and N together meaning a second bond or M a hydrogen atom and N a hydroxy group,X means an oxygen atom, two hydrogen atoms or a hydroxyimino grouping N.about.OH,R.sup.3 and D, which are the same or different, respectively a hydrogen atom, a nitrile radical or a C.sub.1 -C.sub.4 -alkyl radical or, together, a methylene or ethylene group,E a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl radical,D and E together meaning a second bond between carbon atoms 1 and 2 or together a methylene group ##STR3## with R.sup.11 in the meaning of a hydrogen atom or a C.sub.1 -C.sub.8 -alkyl radical,are described as well as their pharmaceutically tolerated addition salts with acids. The new compounds possess valuable pharmacological properties.
摘要翻译：新的19,11个β-桥连类固醇，其通式为Ⅰ（Ⅰ），其中R1代表甲基或乙基，R2代表氢或氯原子或C1-C4烷基，B和G，其中分别对于氢原子，C 1 -C 4 - 烷基或碳原子6和7之间的第二个键，B和R 2一起为亚甲基或亚乙基，Z为相同或不同的可能被取代且可能不饱和的五角或六方环的基团V代表可能被取代的碳环或杂环芳基，A，A，M和N一起表示第二个键或M是氢原子和N是羟基，X表示氧原子，两个氢原子或羟基亚氨基基团N分别OH，R3和D分别相同或不同，分别为氢原子，腈基或C1-C4烷基或者一起是亚甲基或亚乙基，E是氢原子或C 1 -C 4烷基，D和E togeth 呃意指碳原子1和2之间的第二个键或一起与氢原子或C 1 -C 8 - 烷基的含义中的R 11一起形成的亚甲基基团b）或者c），以及它们与酸的药学上耐受的加成盐。新化合物具有宝贵的药理性质。

35. 发明授权

US4977147A 17-methylene- and 17-ethylidene-estratrienes 失效
标题翻译： 17-亚甲基和17-亚乙基 - 雌三烯
公开(公告)号：US4977147A
公开(公告)日：1990-12-11
申请号：US280803
申请日：1988-12-07
申请人： Peter Jungblut , Rudolf Wiechert , Dieter Bittler
发明人： Peter Jungblut , Rudolf Wiechert , Dieter Bittler
IPC分类号： A61K31/56 , A61K31/57 , A61K31/58 , A61P5/00 , A61P35/00 , C07J13/00 , C07J17/00
CPC分类号： A61K31/56 , A61K31/58
摘要： A pharmaceutical preparation for treating menopausal symptoms, estrogen deficiency and hormone-dependent tumors, and for use as a contraceptive, comprises a compound of formula I ##STR1## wherein R.sub.1 is hydrogen, methyl, a tetrahydropyranyl group or an acyl group andR.sub.2 is hydrogen or methyl.
摘要翻译：用于治疗绝经期症状，雌激素缺乏和激素依赖性肿瘤以及用作避孕药物的药物制剂包含其中R 1是氢，甲基，四氢吡喃基或酰基的式I化合物， R2是氢或甲基。

36. 发明授权

US4885117A Process for the preparation of (Z)-17.alpha.-halovinyl steroids 失效
标题翻译：制备（Z）-17α-乙酰基乙酰基类固醇的方法
公开(公告)号：US4885117A
公开(公告)日：1989-12-05
申请号：US84042
申请日：1987-08-11
申请人： Helmut Hofmeister , Henry Laurent , Rudolf Wiechert
发明人： Helmut Hofmeister , Henry Laurent , Rudolf Wiechert
IPC分类号： C07J1/00 , C07J21/00
CPC分类号： C07J1/0033 , C07J1/0081 , C07J21/006
摘要： (Z)-17.alpha.-halovinyl steroids of general Formula I ##STR1## wherein . . . . is a single bond or a double bond,V is a carbon-to-carbon bond or a methylene group,R.sub.1 is a hydrogen atom or a methyl group,X is a chlorine atom, a bromine atom or an iodine atom, andA symbolizes the remainder of the steroid molecule,are prepared by hydrogenating a 17.alpha.-haloethynyl steroid of formula II with diimide. ##STR2## wherein . . . , V, R.sub.1, X and A have the meanings given above. The compounds of Formula I include both known and novel compounds, all of which are pharmacologically active.
摘要翻译：（Z）-17α-乙酰基类固醇通式Ⅰ（I）其中。。。。是单键或双键，V是碳 - 碳键或亚甲基，R1是氢原子或甲基，X是氯原子，溴原子或碘原子，A表示类固醇分子的其余部分通过用二酰亚胺将17α-卤代乙炔基类固醇与二酰亚胺氢化来制备。（II）其中。。。，V，R1，X和A具有上述含义。式I的化合物包括已知的和新的化合物，它们都是药理活性的。

37. 发明授权

US4814327A 11 .beta.-(4-isopropenylphenyl)estra-4,9-dienes, their production, and pharmaceutical preparations containing same 失效
标题翻译： 11β-（4-异丙烯基苯基）雌-4,9-二烯，它们的生产和含有它们的药物制剂
公开(公告)号：US4814327A
公开(公告)日：1989-03-21
申请号：US077359
申请日：1987-07-24
申请人： Eckhard Ottow , Rudolf Wiechert , Gunter Neef , Sybille Beier , Walter Elger , David Henderson
发明人： Eckhard Ottow , Rudolf Wiechert , Gunter Neef , Sybille Beier , Walter Elger , David Henderson
IPC分类号： A61K31/565 , A61P5/00 , A61P13/02 , A61P15/00 , C07J20060101 , C07J1/00 , C07J17/00 , C07J21/00 , C07J41/00 , A61K31/56
CPC分类号： C07J1/0081 , C07J17/00 , C07J21/006 , C07J41/0094
摘要： 11 .beta.-(4-isopropenylphenyl)-estra-4,9-dienes of general Formula I ##STR1## wherein X is an oxygen atom or a hydroxyimino grouping N OH,R.sup.1 is a hydrogen atom or a methyl group,R.sup.2 is a hydrogen atom or an acyl residue of 1-10 carbon atoms,R.sup.3 is a hydrogen atom, the cyanomethyl group, --(CH.sub.2).sub.n --, CH.sub.2 Z, --CH.dbd.CH--(CH.sub.2).sub.m Z or --C.tbd.C--Y wherein n=0 to 5 and m=1 to 4, Z meaning a hydrogen atom or the OR.sup.4 group with R.sup.4 meaning a hydrogen atom, an alkyl or alkanoyl group each of 1-4 carbon atoms, and Y meaning a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group each of 1-4 carbon atoms in the alkyl or acyl residue, possess antiprogestational activity.
摘要翻译： 11β-（4-异丙烯基苯基） - 雌-4,9-二烯通式Ⅰ其中X是氧原子或羟基亚氨基，N OH，R 1是氢原子或甲基，R 2 是氢原子或1-10个碳原子的酰基，R3是氢原子，氰基甲基， - （CH2）n-，CH2Z，-CH = CH-（CH2）mZ或-C3OND CY其中n = 0〜5，m = 1〜4，Z表示氢原子或具有R4的OR4基团，表示氢原子，1-4个碳原子的烷基或烷酰基，Y表示氢，氯，氟，碘或溴原子，烷基或酰基残基中1-4个碳原子的烷基，羟基烷基，烷氧基烷基或酰氧基烷基具有抗供体活性。

38. 发明授权

US4719210A 3-vinyl and 3-thyinyl-beta-carbolines, and their use as benzodiazepine receptor antagonists or agonists 失效
标题翻译： 3-乙烯基和3-甲酰基-β-咔啉，以及它们作为苯并二氮杂受体拮抗剂或激动剂的用途
公开(公告)号：US4719210A
公开(公告)日：1988-01-12
申请号：US915360
申请日：1986-10-06
申请人： Dieter Seidelmann , Andreas Huth , Ralph Schmiechen , Rudolf Wiechert , Herbert Schneider , David N. Stephens
发明人： Dieter Seidelmann , Andreas Huth , Ralph Schmiechen , Rudolf Wiechert , Herbert Schneider , David N. Stephens
IPC分类号： A61K31/435 , A61P25/00 , A61P25/08 , A61P25/20 , C07D471/04 , A61K31/38 , A61K31/495
CPC分类号： C07D471/04 , Y02P20/55
摘要： Compounds of formula I ##STR1## wherein R.sup.1 is hydrogen or a protecting group,R.sup.2 is --CH.dbd.CR.sub.2.sup.4 or --C.tbd.CR.sup.4,R.sup.4 is hydrogen or halogen,R.sup.3 is hydrogen, lower alkyl or lower alkoxyalkyl,R.sup.A is, inter alia, hydrogen, OR.sup.7, lower alkyl, which optionally is substituted with aryl, lower alkoxy or NR5R6,R.sup.5 and R.sup.6 can be the same or different and in each case is hydrogen, lower alkyl or together with the nitrogen atom a 5-6 member ring, which can contain another heteroatom,R.sup.7 is lower alkyl, optionally substituted aryl or aralkyl, andeach compound can contain one or more R.sup.A radicals which are not hydrogen, have valuable pharmacological properties.
摘要翻译：式I化合物其中R 1是氢或保护基，R 2是-CH = CR 24或-C 3 CON CR 4，R 4是氢或卤素，R 3是氢，低级烷基或低级烷氧基烷基，特别地，氢，OR 7，任选被芳基，低级烷氧基或NR 5 R 6，R 5和R 6取代的低级烷基可以相同或不同，并且在每种情况下均为氢，低级烷基或与氮原子一起5-6 成员环，其可以含有另一个杂原子，R7是低级烷基，任选取代的芳基或芳烷基，并且每种化合物可以含有一个或多个不是氢的RA基团，具有有价值的药理学性质。

39. 发明授权

US4670427A 1.alpha.,2.alpha.-methylene-6-methylene- and 6.alpha.-methylpregnenes, their preparation and pharmaceutical use 失效
标题翻译： 1α，2α-亚甲基-6-亚甲基和6α-甲基孕烯，其制备和药物用途
公开(公告)号：US4670427A
公开(公告)日：1987-06-02
申请号：US692488
申请日：1985-01-18
申请人： Klaus Annen , Henry Laurent , Walter Elger , Rudolf Wiechert , Helmut Hofmeister , Michael Topert
发明人： Klaus Annen , Henry Laurent , Walter Elger , Rudolf Wiechert , Helmut Hofmeister , Michael Topert
IPC分类号： A61K31/57 , C07J7/00 , C07J51/00 , C07J53/00 , C07J1/00 , A61K31/56
CPC分类号： C07J53/005 , C07J7/0045
摘要： 1.alpha.,2.alpha.-methylene-6-methylene- and 6.alpha.-methylpregnenes of Formula I ##STR1## wherein A is ##STR2## and R is a hydrogen atom, an acyl group, or an alkoxymethyl groupare strong antiandrogens, and suitable for the topical treatment of seborrhea, acne, alopecia, and hirsutism.
摘要翻译：式Ⅰ的α，α，α，亚甲基-6-亚甲基和6α-甲基孕烯，其中A是A，而R是氢原子，酰基或烷氧基甲基是强抗雄激素，适用于皮脂溢，痤疮，脱发和多毛症的局部治疗。

40. 发明授权

US4609651A 11.beta.-arylestradienes, their production, and pharmaceutical preparations containing same 失效
标题翻译： 11β-芳基染料，它们的生产和含有它们的药物制剂
公开(公告)号：US4609651A
公开(公告)日：1986-09-02
申请号：US685088
申请日：1984-12-21
申请人： Ralph Rohde , Klaus Annen , Gunter Neef , Rudolf Wiechert , Sybille Beier , Walter Elger , David Henderson
发明人： Ralph Rohde , Klaus Annen , Gunter Neef , Rudolf Wiechert , Sybille Beier , Walter Elger , David Henderson
IPC分类号： A61K31/565 , A61P5/38 , C07F7/08 , C07F7/10 , C07J1/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J53/00 , C07J63/00 , C07J71/00 , A61K31/56
CPC分类号： C07J31/006 , C07F7/0818 , C07F7/0827 , C07F7/10 , C07J1/0081 , C07J21/006 , C07J41/0083 , C07J43/006 , C07J51/00 , C07J63/008 , C07J71/001
摘要： 11.beta.-Arylestradienes of general Formula I are disclosed ##STR1## wherein R.sup.2 is a hydrogen atom, a methyl group, or an ethyl group,R.sup.3 is a hydrogen atom or an acyl group,R.sup.1 and A-B have various meanings,which possess antigestagen and antimineralocorticoid activity.
摘要翻译： 11β-一般式I的丙烯雌二醇公开了其中R 2是氢原子，甲基或乙基，R 3是氢原子或酰基，R 1和AB具有各种含义，具有抗老化和抗皮质激素活性。

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