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1. 发明授权

US4045574A D-Homo-20-ketopregnanes 失效
标题翻译： D-HOMO-20-KETOPREGNANES
公开(公告)号：US4045574A
公开(公告)日：1977-08-30
申请号：US528328
申请日：1974-11-29
申请人： Ulrich Kerb , Rudolf Wiechert , Klaus Kieslich , Karl Petzoldt , Helmut Wachtel , Dieter Palenschat , Reinhard Horowski , Gert Paschelke , Wolfgang Kehr
发明人： Ulrich Kerb , Rudolf Wiechert , Klaus Kieslich , Karl Petzoldt , Helmut Wachtel , Dieter Palenschat , Reinhard Horowski , Gert Paschelke , Wolfgang Kehr
IPC分类号： C07J63/00 , C12P33/00 , A01N9/14 , A61K31/255 , C07C49/26
CPC分类号： C07J63/008 , C12P33/00 , Y10S514/816
摘要： D-homo-20-ketopregnanes of the formula ##STR1## wherein R.sub.1 is oxygen, ##STR2## in which R.sub.5 is hydrogen or lower acyl; R.sub.2 is hydrogen or methyl; R.sub.3 is oxygen, ##STR3## or two hydrogen atoms; R.sub.4 is hydrogen, hydroxy or acyloxy; R.sub.6 is hydrogen or methyl; and R.sub.7 is hydrogen, acetyl, hydroxy or lower acyloxy in the .alpha.- or .beta.-position possess CNS-depressant activity, including anesthesia upon parenteral administration, and are produced by hydrogenating the corresponding steroids having double bonded C.sub.5 and/or C.sub.16 carbon atoms.

2. 发明授权

US4894336A Racemic dissociation of 3-acyloxy bicyclo(3.3.0)octan-7-one-2-carboxylic acid esters by stereospecific enzymatic or microbiological acylate hydrolysis 失效
标题翻译： 3-立体特异性酶或微生物酰化物水解3-酰氧基双环（3.3.0）辛-7-酮-2-羧酸酯的外消旋解离
公开(公告)号：US4894336A
公开(公告)日：1990-01-16
申请号：US237109
申请日：1988-07-13
申请人： Karl Petzoldt , Helmut Dahl , Werner Skuballa
发明人： Karl Petzoldt , Helmut Dahl , Werner Skuballa
IPC分类号： C07C405/00 , C07D317/72 , C07D319/08 , C12P7/12 , C12P7/26 , C12P7/42 , C12P7/62 , C12P17/02 , C12P41/00 , C12R1/01 , C12R1/05 , C12R1/15 , C12R1/20 , C12R1/785 , C12R1/80 , C12R1/84 , C12R1/85 , C12R1/865 , C12R1/885
CPC分类号： C07D317/72 , C07C405/0083 , C07D319/08 , C12P17/02 , C12P41/004 , C12P7/26 , C12P7/42 , C12P7/62
摘要： Process for the production of optically active (+)-bicyclo[3.3.0]octanol derivatives of formula (+)-I, in which R.sub.1 and R.sub.2 represent jointly an oxygen atom or the double-bond residue --O--X--O-- with X as a straight or branched-chain alkylene with 1-7 C-atoms, or R.sub.1 and R.sub.2 represent separately the residue OR.sub.5 with R.sub.5 as a straight or branched-chain alkyl with 1-7 C-atoms, and R.sub.3 the residue COOZ with Z as a hydrogen atom, straight or branched chain alkyl with 1-7 C atoms, cycloalkyl with 3-6 C atoms, phenyl or aralkyl with 7-10 atoms or R.sub.3 is the residue --(CH.sub.2).sub.n --O--COR.sub.4 with n having the meaning 1-4 and R.sub.4 as a straight or branched-chain alkyl with 1-7 C atoms, cycloalkyl with 3-6 C atoms, phenyl or aralkyl with 7-10 C atoms. The process is characterized in that racemic 3.alpha.-cyloxy-cis-bicyclo[3.3.0]-octane derivatives of formula (+)-II, wherein R.sub.1, R.sub.2 R.sub.3 and R.sub.4 have the above meanings, are subjected enzymatically or microbiologically to a stereospecific acylate hydrolsis and the (+)-bicyclo[3.3.0]-octanol derivative produced is separated from the unsaponified bicyclo[3.3.0]-octanol acylate of formula (-)-II or the unsaponified enantiomers (+)-II are separated from the saponified bicyclo[3.3.0]octanol derivative (-)-I and then subjected to chemical acylate hydrolysis.
摘要翻译： PCT No.PCT / DE87 / 00513 Sec。 371日期：1988年7月13日 102（e）日期1988年7月13日PCT提交1987年11月12日PCT公布。出版物WO88 / 03567 日期：1988年5月19日。制备式（+） - I的光学活性（+） - 双环[3.3.0]辛醇衍生物的方法，其中R 1和R 2共同表示氧原子或双键残基-OXO - X为具有1-7个C原子的直链或支链亚烷基，或者R1和R2分别表示残基OR5与R5作为具有1-7个C原子的直链或支链烷基，R3表示残基具有Z作为氢原子的COOZ，具有1-7个C原子的直链或支链烷基，具有3-6个C原子的环烷基，具有7-10个原子的苯基或芳烷基或R3是残基 - （CH2）nO-COR4，其中n 具有1-4和R4为具有1-7个C原子的直链或支链烷基，具有3-6个C原子的环烷基，具有7-10个C原子的苯基或芳烷基。该方法的特征在于其中R1，R2R3和R4具有上述含义的式（+） - II的外消旋3α-甲氧基 - 顺式 - 双 - 二环[3.3.0] - 辛烷衍生物经酶促或微生物方式进行立体特异性将酰化物水解和（+） - 双环[3.3.0] - 辛醇衍生物与式（ - ） - II的未皂化的双环[3.3.0] - 辛醇酰化物分离，或未分离的对映异构体（+） - 从皂化的双环[3.3.0]辛醇衍生物（ - ） - I中，然后进行化学酰化物水解。

3. 发明授权

US4435327A 3.beta.,7.beta.,15.alpha.-Trihydroxy-5-androsten-17-one, its 3,15-dipivalate, and their preparation 失效
标题翻译： 3β，7β，15α-三羟基-5-雄酮-17-酮，其3,15-二氰酸酯及其制备
公开(公告)号：US4435327A
公开(公告)日：1984-03-06
申请号：US420674
申请日：1982-09-21
申请人： Karl Petzoldt , Henry Laurent , Rudolf Wiechert
发明人： Karl Petzoldt , Henry Laurent , Rudolf Wiechert
IPC分类号： A61K31/565 , A61P5/38 , C07J1/00 , C07J53/00 , C07J71/00 , C12P33/06 , C12P33/12
CPC分类号： C12P33/12 , C07J1/0011 , C07J53/008 , C07J71/001 , C12P33/06
摘要： A process for the preparation of 3.beta.,7.beta.,15.alpha.-trihydroxy-5-androsten-17-one and the 3,15-dipivalate thereof comprises epimerizing 3.beta.,7.alpha.,15.alpha.-trihydroxy-5-androsten-17-one in the presence of a ketone with or without a solvent, with dilute mineral acid and subsequent treatment with an organic base, and optionally subsequently esterifying the 3.beta.- and 15.alpha.-positions of the resultant 3.beta.,7.beta.,15.alpha.-triol with a reactive derivative of pivalic acid.
摘要翻译：制备3β，7β，15α-三羟基-5-雄酮-17-和其3,5-二异戊酸的方法包括差向异构化3β，7α，15α-三羟基-5-雄酮-17 在有或没有溶剂的酮的存在下，用稀的无机酸进行处理，随后用有机碱处理，随后任意地将所得的3β，7β，15α的3β-和15α-位酯酯化三醇与新戊酸的活性衍生物。

4. 发明授权

US4307088A 1-Hydroxy steroids, a process for the production thereof, and pharmaceutical preparations containing them 失效
标题翻译： 1-羟基类固醇，其制备方法和含有它们的药物制剂
公开(公告)号：US4307088A
公开(公告)日：1981-12-22
申请号：US227304
申请日：1981-01-22
申请人： Karl Petzoldt , Rudolf Wiechert , Hermann Steinbeck , Walter Elger
发明人： Karl Petzoldt , Rudolf Wiechert , Hermann Steinbeck , Walter Elger
IPC分类号： A61K31/57 , C07J1/00 , C12P33/06 , C12R1/66 , A61K31/56 , C07J7/00
CPC分类号： C07J1/0096 , C12P33/06 , Y10S514/843
摘要： 1-Hydroxy steroids of formula I ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen or alkanoyl of 1-8 carbon atoms are distinguished by strong progestational activity and only very minor androgenic side effects.
摘要翻译：式I的1-羟基类固醇（I）其中R1和R2独立地是氢或1-8个碳原子的烷酰基，其特征在于强烈的促孕活性，只有非常小的雄激素副作用。

5. 发明授权

US4011314A 7-Hydroxyestradiols 失效
标题翻译： 7-羟基吗啉
公开(公告)号：US4011314A
公开(公告)日：1977-03-08
申请号：US621136
申请日：1975-10-09
申请人： Karl Petzoldt , Hans-Jorg Vidic , Klaus Prezewowsky , Yukishige Nishino , Rudolf Wiechert , Henry Laurent
发明人： Karl Petzoldt , Hans-Jorg Vidic , Klaus Prezewowsky , Yukishige Nishino , Rudolf Wiechert , Henry Laurent
IPC分类号： C07J11/00 , A61K31/565 , C07J1/00 , C07J17/00 , C07J31/00 , A61K31/58
CPC分类号： C07J31/006 , C07J1/0059 , C07J1/0081 , C07J1/0096 , C07J17/00 , Y10S435/911 , Y10S435/912 , Y10S435/913 , Y10S435/939
摘要： 7-Hydroxyestradiols of the formula ##STR1## wherein R.sub.1 is hydrogen, acyl, alkyl, cycloalkyl, an oxygenated saturated heterocyclic group or hydrocarbylsulfonyl; R.sub.2 and R.sub.3 each are hydrogen, acyl, oxygenated saturated heterocyclic group or R.sub.2 is hydrocarbylsulfonyl and R.sub.4 is alkyl, alkenyl, chlorinated alkenyl, alkynyl or chlorinated alkynyl, are useful for treating estrogen deficiency symptoms.

6. 发明授权

US5403724A Microbiological reduction of prostacyclin intermediate products with a 15-keto group 失效
标题翻译：前列环素中间产物与15-酮基的微生物降低
公开(公告)号：US5403724A
公开(公告)日：1995-04-04
申请号：US176927
申请日：1994-01-03
申请人： Karl Petzoldt , Helmut Dahl , Werner Skuballa
发明人： Karl Petzoldt , Helmut Dahl , Werner Skuballa
IPC分类号： C12P7/26 , C07C49/743 , C07C69/78 , C07D317/72 , C07D319/08 , C07F7/18 , C12P7/62 , C12P17/04 , C12P17/06 , C12P17/18 , C12P31/00 , C12R1/72 , C12R1/84 , C12N1/14
CPC分类号： C07D317/72 , C12P17/04 , C12P31/00 , C12R1/72 , C12R1/84 , Y10S435/911 , Y10S435/921
摘要： A process for production of 15-alpha-hydroxyprostaglandin intermediates of formula I ##STR1## wherein X is CH.sub.2,A is trans --CH.dbd.CH--B is ethylenedioxy or 2,2-dimethylpropylenedioxy,R.sub.1 is benzoyl, andR.sub.2 is ##STR2## by treating a ketone of formula II ##STR3## wherein A, B, X, R.sub.1 and R.sub.2 have the meanings indicated above, with a culture of Candida solani (NCYC 41) and isolating the resulting 15-alpha-hydroxyprostaglandin intermediate.
摘要翻译：制备式I的15-α-羟基前列腺素中间体的方法，其中X为CH 2，A为反式-CH = CH-B为亚乙二氧基或2,2-二甲基亚丙基二氧基，R 1为苯甲酰基，R 2为通过用茄酸假丝酵母（NCYC 41）的培养物处理其中A，B，X，R 1和R 2具有上述含义的式II的酮（II）的酮，并分离所得的15-α- 羟脯氨酸中间体。

7. 发明授权

US4603013A Estrane derivatives 失效
标题翻译： Estrane衍生物
公开(公告)号：US4603013A
公开(公告)日：1986-07-29
申请号：US644465
申请日：1984-08-27
申请人： Gunter Neef , Karl Petzoldt , Gerhard Sauer , Helmut Hofmeister
发明人： Gunter Neef , Karl Petzoldt , Gerhard Sauer , Helmut Hofmeister
IPC分类号： C07J1/00 , C12P33/12 , C12R1/645 , C12R1/65 , C12R1/77
CPC分类号： C12P33/12 , C07J1/0059
摘要： Estrane derivatives of the general formula I ##STR1## wherein one of the substituents X or Z signifies a hydrogen atom and the other together with Y represents a carbon-carbon bond, or wherein the substituents X and Z represent hydrogen atoms and Y represents an .alpha.-position hydroxy group or a .beta.-position alkyl group with up to 6 carbon atoms, are valuable intermediates for preparation of pharmacologically effective substances.
摘要翻译：其中一个取代基X或Z表示氢原子，另一个与Y一起代表碳 - 碳，或其中取代基X和Z表示氢原子，Y 表示具有至多6个碳原子的α-位羟基或β-位烷基，是用于制备药理学有效物质的有价值的中间体。

8. 发明授权

US4416985A Process for preparing 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroids 失效
标题翻译：制备3β，7β-二羟基-DTATA 5-类固醇的方法
公开(公告)号：US4416985A
公开(公告)日：1983-11-22
申请号：US317822
申请日：1981-11-03
申请人： Karl Petzoldt , Rudolf Wiechert , Henry Laurent , Klaus Nickisch , Dieter Bittler
发明人： Karl Petzoldt , Rudolf Wiechert , Henry Laurent , Klaus Nickisch , Dieter Bittler
IPC分类号： C07J21/00 , C07J53/00 , C07J71/00 , C12P33/06 , C12P33/20 , C12R1/645 , C07J7/00
CPC分类号： C12P33/06 , C07J53/008 , C07J71/001
摘要： A process for preparing a 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 steroid of the formula ##STR1## wherein Q is ##STR2## and R.sub.1 is hydrogen, trimethylacetyl, tert-butyldimethylsilyl, dimethyl-2-(3-methylbutyl)silyl or tribenzylsilyl,comprises fermenting a 3.beta.-hydroxy-.DELTA..sup.5 -steroid of the formula ##STR3## wherein Q is as defined above, andR.sub.2 is hydrogen or alkanoyl of 2-6 carbon atoms,with a culture of Botryodiplodia malorum to obtain the corresponding 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid; and, optionally, reacting the resultant product with trimethylacetic anhydride, tert-butyldimethylsilyl chloride, dimethyl-2-(3-methylbutyl)silyl chloride, or tribenzylsilyl chloride.
摘要翻译：制备式“IMAGE”的3β，7β-二羟基-TATA 5类的方法，其中Q是R 1，R 1是氢，三甲基乙酰基，叔丁基二甲基甲硅烷基，二甲基-2-（3-甲基丁基）甲硅烷基或三苄基甲硅烷基包括发酵式为“IMAGE”的3β-羟基-TATA5-类固醇，其中Q如上所定义，R 2为2-6个碳原子的氢或链烷酰基，并具有葡萄孢属（Botryodiplodia malorum）的培养物，以获得相应的3 β，β-二羟基-DTATA5-类固醇; 和任选地使所得产物与三甲基乙酸酐，叔丁基二甲基甲硅烷基氯，二甲基-2-（3-甲基丁基）甲硅烷基氯或三苄基甲硅烷基氯反应。

9. 发明授权

US4353985A Process for the preparation of 11 .beta.-hydroxy steroids 失效
标题翻译：制备11种β-羟基类固醇的方法
公开(公告)号：US4353985A
公开(公告)日：1982-10-12
申请号：US167888
申请日：1980-07-14
申请人： Karl Petzoldt , Klaus Annen , Henry Laurent , Rudolf Wiechert
发明人： Karl Petzoldt , Klaus Annen , Henry Laurent , Rudolf Wiechert
IPC分类号： C12P33/08
CPC分类号： C12P33/08 , Y10S435/911
摘要： A process for preparing an 11.beta.-hydroxy steroid of the formula ##STR1## wherein represents a single bond or a double bond;X is hydrogen, fluorine, chlorine or methyl; andV is methylene, ethylene, ethylidene or vinylidene;comprises fermenting an 11-deoxy steroid of the formula ##STR2## wherein , X and V are as defined above,R.sub.1 is hydrogen or C.sub.1-6 -alkyl; andR.sub.2 is C.sub.1-6 -alkyl;with a fungal culture of a genus Curvularia.
摘要翻译：制备式“IMAGE”的11β-羟基类固醇的方法，其中代表单键或双键; X是氢，氟，氯或甲基; 和V是亚甲基，亚乙基，亚乙基或亚乙烯基; 包括发酵式为“IMAGE”的11-脱氧类固醇，其中X和V如上定义，R 1是氢或C 1-6 - 烷基; 并且R 2是C 1-6 - 烷基; 具有曲霉属属的真菌培养物。

10. 发明授权

US4144334A Novel .alpha.-hydroxy steroids 失效
标题翻译：新型{60-羟基类固醇
公开(公告)号：US4144334A
公开(公告)日：1979-03-13
申请号：US767420
申请日：1977-02-10
申请人： Karl Petzoldt , Walter Elger
发明人： Karl Petzoldt , Walter Elger
IPC分类号： C07J1/00 , C12P33/00 , A61K31/56 , C07J7/00
CPC分类号： C07J1/0096 , C12P33/00 , Y10S435/911
摘要： 1.alpha.-Oxysteroid of the formula ##STR1## wherein R.sub.1 is methyl or ethyl,R.sub.2 and R.sub.3 each are hydrogen or alkanoyl of 1-8 carbon atoms, andR.sub.4 is hydrogen or hydrocarbon of 1-4 carbon atoms,Are progestestionally active and useful in oral contraceptive and menopausal compositions.
摘要翻译： 1α-类型的化学式其中R 1是甲基或乙基，R 2和R 3各自是氢或碳原子的烷酰基，且R 4是氢或1-4个碳原子的烃，ARE PROGESTESTIONALLY ACTIVE AND USEFUL 口服合同和男性组成。

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