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1. 发明授权

US4178381A C-homoestratrienes 失效
公开(公告)号：US4178381A
公开(公告)日：1979-12-11
申请号：US966162
申请日：1978-12-04
申请人： Gregor Haffer , Ulrich Eder , Gerhard Sauer , Rudolf Wiechert , Yukishige Nishino , Gunter Neef
发明人： Gregor Haffer , Ulrich Eder , Gerhard Sauer , Rudolf Wiechert , Yukishige Nishino , Gunter Neef
IPC分类号： C07J63/00 , C07J71/00 , A61K31/05 , A61K31/085 , A61K31/12
CPC分类号： C07J71/001 , C07J63/006 , C07J71/0005
摘要： C-homoestratrienes of the formula ##STR1## wherein ##STR2## R.sub.1 and R.sub.2 are the same or different, and each is hydrogen, acyl, alkyl, cycloalkyl or tetrahydropyranyl; andR.sub.3 is hydrogen, ethynyl or chloroethynyl; possess very good estrogenic properties.
摘要翻译：其中，R 1和R 2相同或不同，并且各自为氢，酰基，烷基，环烷基或四氢吡喃基; 并且R 3是氢，乙炔基或氯乙炔基; 具有非常好的雌激素特性。

2. 发明授权

US4155923A Process for the preparation of 17.beta.-hydroxy-20-alkoxypregnane-21-oic acid derivatives 失效
标题翻译：制备17 {62-羟基-20-烷氧基孕烷-21-酸酸衍生物的方法
公开(公告)号：US4155923A
公开(公告)日：1979-05-22
申请号：US873444
申请日：1978-01-30
申请人： Gunter Neef , Gregor Haffer , Ulrich Eder , Gerhard Sauer , Rudolf Wiechert
发明人： Gunter Neef , Gregor Haffer , Ulrich Eder , Gerhard Sauer , Rudolf Wiechert
IPC分类号： C07J1/00 , C07J13/00 , C07J7/00
CPC分类号： C07J13/005 , C07J1/0033 , C07J13/007
摘要： A process for the preparation of 17.beta.-hydroxy-20-alkoxypregnane-21-oic acid derivatives of the formula ##STR1## WHEREIN R.sub.1 is methyl or ethyl;R.sub.2 is hydrogen or methyl, either being in the .alpha.-or .beta.-position;R.sub.3 is lower alkyl of 1-4 carbon atoms;R.sub.4 is alkyl of 1-8 carbon atoms or benzyl; andSt is the residue of a steroid ABC ring system;Comprises reacting (a) a 17-oxo compound of the formula ##STR2## WHEREIN R.sub.1 and R.sub.2 are as defined above andSt* is said steroid ABC ring system residue, St, in a form which is chemically compatible with said reaction;With (b) an enolate ion of an alkoxyacetic acid alkyl ester of the formula ##STR3## wherein R.sub.3 and R.sub.4 are as defined above.
摘要翻译：制备式Ia的17β-羟基-20-烷氧基孕烷-21-酸酸衍生物的方法，其中R1是甲基或乙基; R2是氢或甲基，或者是α位或β-位; R3是1-4个碳原子的低级烷基; R4是1-8个碳原子的烷基或苄基; St是类固醇ABC环系统的残基; 包含反应（A）制剂的17-OXO化合物，其中R1和R2如上所定义，St *是所述类固醇ABC环系统残基St，以与所述反应化学相容的形式; 具有（B）式（A）的化合物，其中R 3和R 4如上所定义的烷氧基酸酯。

3. 发明授权

US4077996A Process for the preparation of trans-deca hydronaphthalene derivatives 失效
标题翻译：反十氢化萘衍生物的制备方法
公开(公告)号：US4077996A
公开(公告)日：1978-03-07
申请号：US676805
申请日：1976-04-14
申请人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
发明人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
IPC分类号： C07C69/013 , C07C45/00 , C07C49/385 , C07C49/517 , C07C49/753 , C07C67/00 , C07C69/66 , C07C253/00 , C07C255/31 , C07D317/50 , C07D317/72 , C07D321/00 , C07F7/18 , C07C120/00 , C07C121/46 , C07D319/02 , C07D319/04
CPC分类号： C07F7/1856 , C07D317/50
摘要： A process for the preparation of trans-decahydronaphthalene compounds of Formula I ##STR1## wherein X is lower alkyl, --(CH.sub.2).sub.3 --Z--R.sub.2, ##STR2## --(CH.sub.2).sub.3 COOR.sub.4, or --(CH.sub.2).sub.3 CN; Y and Z are ketalized carbonyl or free, esterified, or etherified hydroxymethylene;U is halogen;R.sub.1, r.sub.2, and R.sub.3 are lower alkyl; andR.sub.4 is alkyl;Wherein an octahydronaphthalene compound of Formula II ##STR3## is converted, in the presence of bases, by reaction of a trialkyl chlorosilane of the formula(R.sub.5).sub.3 Si--Clwherein the R.sub.5 each are lower alkyl group, to a hexahydronaphthalene compound of the formula ##STR4## The hexahydronaphthalene compound is hydrogenated, in an inert solvent with hydrogen in the presence of a platinum-, palladium-, or rhodium-containing hydrogenation catalyst, to an octahydronaphthalene compound of the formula ##STR5## and a vinyl ketone of the formulaXCOCH.dbd.CH.sub.2is added to the thus-obtained octahydronaphthalene compound in an inert solvent in the presence of a Lewis acid.
摘要翻译：制备式I的反十氢萘化合物的方法，其中X是低级烷基， - （CH 2）3 -Z-R 2， - （CH 2）3 COOR 4或 - （CH 2）3 C 3; Y和Z是缩酮化羰基或游离的，酯化的或醚化的羟基亚甲基; U是卤素; R1，R2和R3是低级烷基; 和R4是烷基; 在碱的存在下，通过式（R5）3Si-Cl的三烷基氯硅烷与各自为低级烷基的R 5反应得到式II的六氢萘化合物，其中式II的甲氧基二苯甲酮化合物转化为式VI化合物在惰性溶剂中，在含有铂，钯或铑的氢化催化剂的存在下，用氢气将其氢化成式为“八氢”的八氢化合物和式在路易斯酸存在下，在惰性溶剂中将式XCOCH = CH 2加入到如此获得的八氢萘化合物中。

4. 发明授权

US4024166A Process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones 失效
标题翻译：制备13 {62-烷基-4-锑烯-3,17-二酮的方法
公开(公告)号：US4024166A
公开(公告)日：1977-05-17
申请号：US621384
申请日：1975-10-10
申请人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
发明人： Gerhard Sauer , Ulrich Eder , Gregor Haffer , Gunter Neef , Rudolf Wiechert
IPC分类号： B01J23/00 , C07B61/00 , C07C317/14 , C07D317/26 , C07D317/72 , C07J1/00
CPC分类号： C07C317/00 , C07D317/26 , C07D317/72 , C07J1/0059
摘要： Novel process for the preparation of 13.beta.-alkyl-4-gonene-3,17-diones of the formula ##STR1## wherein R.sub.1 is methyl or ethyl, consists of REACTING A 7A.beta.-ALKYL,5,6,7,7A-TETRAHYDROINDANE-1,5-DIONE WITH FORMALDEHYDE AND AN ARYLSULFINIC ACID OR AN ADDUCT OF FORMALDEHYDE AND ARYLSULFINIC ACID TO PRODUCE A TETRAHYDROINDANE DERIVATIVE;Hydrogenating the tetrahydroindane derivative with hydrogen in the presence of a palladium-, platinum-, or rhodium-containing hydrogenation catalyst to produce a perhydroindane derivative;Condensing the perhydroindane derivative in the presence of a proton-accepting agent with a 7,7-alkylenedioxy-3-oxooctanoic acid ester;Treating the product obtained with a strong aqueous base and then heating the product in an inert solvent to produce a 4,5-secosteroid;Hydrogenating the 4,5-secosteroid in the presence of a palladium-, platinum-, rhodium-, or nickel-containing hydrogenation catalyst; andHydrolyzing and cyclizing the hydrogenated 4,5-secosteroid by treatment with a strong acid.
摘要翻译：用于制备式“IMAGE”的13β-烷基-4-单宁-3,17-二酮的新方法，其中R 1是甲基或乙基，由反应A7Aβ-烷基，5,6,7,7a- 四氢呋喃-1,5-二酮与甲醛和氨基磺酸或甲醛和芳香酸的添加以生产四氢衍生物衍生物; 在含有氢氧化钯，或含氢氧化铑的氢化催化剂存在下氢化四氢呋喃衍生物生成四氢呋喃衍生物; 在具有7,7-亚甲基氧化亚硝酸酯酸酯的接受原料的情况下，冷凝该衍生物衍生物; 处理用强碱性基质获得的产品，然后加入产品中的产品用于生产4,5代谢物; 在含有钯，铑，铑，或含镍的氢化催化剂存在下氢化4,5-二氧化硫; 并通过用强酸处理氢化和循环氢化的4,5代谢物。

5. 发明授权

US4333928A 16 .alpha.-Alkyl steroids, their preparation, and pharmaceutical preparations thereof 失效
标题翻译： 16α-烷基甾类，它们的制备及其药物制剂
公开(公告)号：US4333928A
公开(公告)日：1982-06-08
申请号：US150518
申请日：1980-05-16
申请人： Gunter Neef , Ulrich Eder , Gregor Haffer , Gerhard Sauer , Rudolf Wiechert , Hermann Steinbeck
发明人： Gunter Neef , Ulrich Eder , Gregor Haffer , Gerhard Sauer , Rudolf Wiechert , Hermann Steinbeck
IPC分类号： A61K31/565 , A61K31/58 , C07J1/00 , C07J17/00 , C07J41/00 , A61K31/56
CPC分类号： C07J1/0096 , C07J1/0059 , C07J1/007 , C07J17/00 , C07J41/0005 , C07J41/0088
摘要： 16 .alpha.-Alkyl steroids of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen, alkyl, acyl, or glycosylR.sub.3 is hydrogen or a substituted or unsubstituted, saturated or unsaturated lower hydrocarbon residue, andR.sub.4 is methyl, ethyl or propyl, exhibit strong progestational activity and a very low androgenic activity.
摘要翻译： 16α-烷基甾族化合物，其中R1是氢或甲基，R2是氢，烷基，酰基或糖基R3是氢或取代或未取代的饱和或不饱和低级烃基，R4是甲基，乙基或丙基，表现出强烈的促孕活性和非常低的雄激素活性。

6. 发明授权

US4170518A Microbiological conversion of sterol derivatives to 5-androsten-17-one derivatives and their use 失效
标题翻译：固醇衍生物微生物转化为5-雄酮-17-一种衍生物及其用途
公开(公告)号：US4170518A
公开(公告)日：1979-10-09
申请号：US710559
申请日：1976-07-30
申请人： Alfred Weber , Mario Kennecke , Alfred Popper , Rudolf Muller , Ulrich Eder , Gregor Haffer , Gerhard Sauer , Gunter Neef , Rudolf Wiechert
发明人： Alfred Weber , Mario Kennecke , Alfred Popper , Rudolf Muller , Ulrich Eder , Gregor Haffer , Gerhard Sauer , Gunter Neef , Rudolf Wiechert
IPC分类号： C12P33/16 , A61K31/5685 , C07J1/00 , C07J7/00 , C07J9/00 , C07J13/00 , C07J21/00 , C12P33/00 , C12R1/01 , C12R1/06 , C12R1/07 , C12R1/32 , C07B29/02
CPC分类号： C07J13/005 , C07J1/0011 , C07J1/0022 , C07J1/0037 , C07J1/0048 , C07J21/006 , C07J7/002 , C07J7/003 , C07J9/00 , C12P33/005
摘要： Sterol derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom and R.sub.2 is lower alkoxy, or R.sub.1 and R.sub.2 collectively are lower alkylenedioxy and R.sub.3 is a sterol hydrocarbon side chain are converted to the corresponding androsten-17-ones by the oxidative degradation activity of a species of microorganism which degrades sterol side chains, preferably of the genus Mycobacterium. The ether group of those compounds wherein R.sub.1 is a hydrogen atom and R.sub.2 is lower alkoxy, and the corresponding 17.beta.-hydroxy and 17.alpha.-hydrocarbon-17.beta.-hydroxy compounds is cleaved by reaction with an alkanoic acid chloride or anhydride in the presence of a Lewis acid.
摘要翻译：其中R 1是氢原子，R 2是低级烷氧基，或者R 1和R 2一起是低亚烷基二氧基并且R 3是一个固醇烃侧链的甾醇衍生物通过氧化降解被转化成相应的sten -17- 降解甾醇侧链，优选分枝杆菌属的微生物物种的活性。其中R 1为氢原子且R 2为低级烷氧基的那些化合物的醚基，并且相应的17β-羟基和17α-烃-17β-羟基化合物在存在下与链烷酰氯或酸酐反应而被裂解的路易斯酸。

7. 发明授权

US4298538A 16-Dimethylaminomethylene-3-methoxy-1,3,5-(10)-estratrien-17-one, a process for the preparation thereof and its use as a preparative intermediate 失效
标题翻译： 16-二甲基氨基亚甲基-3-甲氧基-1,3,5-（10） - 雌三醇17-酮，其制备方法及其作为制备中间体
公开(公告)号：US4298538A
公开(公告)日：1981-11-03
申请号：US104949
申请日：1979-12-18
申请人： Gunter Neef , Ulrich Eder , Gregor Haffer , Gerhard Sauer
发明人： Gunter Neef , Ulrich Eder , Gregor Haffer , Gerhard Sauer
IPC分类号： C07J1/00 , C07J41/00
CPC分类号： C07J1/0059 , C07J1/007 , C07J41/0088
摘要： 16-dimethylaminomethylene-3-methoxy-1,3,5(10)-estratrien-17-one is a valuable new preparative intermediate which may be used, e.g., to prepare 17.beta.-hydroxy-16.beta.-ethyl-4-estren-3-one or 16.beta.-ethylestradiol.
摘要翻译： 16-二甲基氨基亚甲基-3-甲氧基-1,3,5（10） - 雌三醇17-酮是一种有价值的新制备中间体，可用于制备17β-羟基-16β-乙基-4-雌酮 -3-one或16β-乙基雌二醇。

8. 发明授权

US4057561A D-Homo-19-norsteroids 失效
标题翻译： D-Homo-19-诺贝星
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。

9. 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。

10. 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。

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