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公开(公告)号：US4708823A
公开(公告)日：1987-11-24
申请号：US776923
申请日：1985-09-17
申请人： Helmut Hofmeister , Klaus Annen , Henry Laurent , Rudolf Wiechert
发明人： Helmut Hofmeister , Klaus Annen , Henry Laurent , Rudolf Wiechert
IPC分类号： B01J23/50 , C07B61/00 , C07J1/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J41/00 , C07J63/00 , C07J75/00
CPC分类号： C07J5/0053 , C07J1/0011 , C07J1/0033 , C07J41/0038 , C07J63/008 , C07J7/0085
摘要： Known pregnane derivatives are prepared by esterificiation of known androstane derivatives to give new ester of Formula III ##STR1## wherein in each case symbolizes a single bond or a double bond,n is 1 or 2,R.sub.1 is hydrogen or methyl,R.sub.2 is hydrogen or formyl, andR.sub.3 is chlorine, hydroxy or an alkanoyloxy group of up to 6 carbon atoms,and reaction of the latter with Ag(I) and formic acid.
摘要翻译： 已知的孕烷衍生物通过已知的雄甾烷衍生物的酯化制备得到式III的新的酯（III），其中在每种情况下符号是单键或双键，n为1或2，R 1为氢或甲基，R 2为 是氢或甲酰基，R3是氯，羟基或至多6个碳原子的烷酰氧基，后者与Ag（I）和甲酸的反应。
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2.发明授权11.beta.-aryl estradienes, processes for their production and pharmaceutical preparations containing them 失效11β-芳基雌二醇，其制备方法和含有它们的药物制剂
公开(公告)号：US4536401A
公开(公告)日：1985-08-20
申请号：US581853
申请日：1984-02-21
申请人： Guenter Neef , Gerhard Sauer , Rudolf Wiechert , Helmut Hofmeister , Ralph Rohde , Klaus Annen , Henry Laurent , Sybille Beier , Wolfgang Losert , Walter Elger , David Henderson
发明人： Guenter Neef , Gerhard Sauer , Rudolf Wiechert , Helmut Hofmeister , Ralph Rohde , Klaus Annen , Henry Laurent , Sybille Beier , Wolfgang Losert , Walter Elger , David Henderson
IPC分类号： C07J1/00 , C07J21/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J63/00 , C07J71/00 , A61K31/58
CPC分类号： C07J41/0083 , C07J1/0081 , C07J21/003 , C07J21/006 , C07J31/006 , C07J33/005 , C07J41/0088 , C07J43/003 , C07J43/006 , C07J63/008 , C07J71/001
摘要： Compounds of the formula I ##STR1## wherein R.sub.1 is ##STR2## wherein R.sup.I and R.sup.II each independently is alkyl of 1-4 carbon atoms, or R.sup.I and R.sup.II together with the connecting N-atom form a 5- or 6-membered heterocyclic ring whose remaining atoms are all C-atoms, or which also includes and additional N-atom, an additional O or S atom or a combination thereof; ##STR3## wherein R.sup.I and R.sup.II are as defined above; --SR.sup.III, wherein R.sup.III is methyl, ethyl or phenyl; or--OR.sup.IV, wherein R.sup.IV is methyl, ethyl, propyl, methoxymethyl, allyl, or .beta.-dimethylaminoethyl;R.sub.2 is hydrogen, methyl, or ethyl; ##STR4## wherein the wavy lines mean that the substituent is in the .alpha.- or .beta.-position, and ##STR5## M is Na, K or Li; and R.sup.V, R.sup.VI, R.sup.VII and R.sup.VIII each independently is alkyl of 1-4 carbon atoms, have valuable pharmacological properties, e.g., a combination of antiprogestational and antimineralocorticordal effects.
摘要翻译： 式Ⅰ的化合物其中R 1是R 1，其中R 1和R 2各自独立地是1-4个碳原子的烷基，或者R 1和R II与连接的N-原子一起形成5-或6-元环， 其余的原子都是C原子，或者还包括和另外的N原子，另外的O或S原子或它们的组合; 其中RI和RII如上所定义; -SRIII，其中RIII是甲基，乙基或苯基; 或-ORIV，其中RIV是甲基，乙基，丙基，甲氧基甲基，烯丙基或β-二甲基氨基乙基; R2是氢，甲基或乙基; 其中波浪线意味着取代基位于α位或β位，而图像中的取代基为< + RE M是Na，K或Li; RV，RVI，RVII和RVIII各自独立地为1-4个碳原子的烷基，具有有价值的药理学性质，例如抗孕素和抗肌钙蛋白作用的组合。
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3.发明授权11-Methylene steroids, their preparation and pharmaceutical preparations containing them 失效11-亚甲基类固醇，其制剂和含有它们的药物制剂
公开(公告)号：US4277468A
公开(公告)日：1981-07-07
申请号：US135066
申请日：1980-03-28
CPC分类号： C07J21/006 , C07J1/0081 , Y10S514/843
摘要： 11-Methylene steroids of Formula I ##STR1## wherein R is hydrogen or acyl, andX is oxygen or two hydrogen atomshave valuable pharmacological properties.
摘要翻译： 其中R是氢或酰基，X是氧或两个氢原子具有有价值的药理学性质的式Ⅰ的11-亚甲基类固醇。
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公开(公告)号：US4176126A
公开(公告)日：1979-11-27
申请号：US839486
申请日：1977-10-04
申请人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Rudolf Wiechert , Hans Wendt , Joachim-Friedrich Kapp
发明人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Rudolf Wiechert , Hans Wendt , Joachim-Friedrich Kapp
CPC分类号： C07J21/00 , C07J31/006 , C07J5/0053 , C07J7/0085
摘要： Novel corticoids of formula I ##STR1## wherein X is .beta.-hydroxymethylene, .beta.-fluoromethylene or carbonyl; Y is fluorine, chlorine, hydroxy, or acyloxy of 1-10 carbon atoms; and R.sub.1 is acyloxy of 1-10 carbon atoms, possess strong anti-inflammatory activity when administered topically and display only minor systemic side effects.
摘要翻译： 式I的新型皮质激素（I），其中X是β-羟基亚甲基，β-氟亚甲基或羰基; Y是1-10个碳原子的氟，氯，羟基或酰氧基; R1为1-10个碳原子的酰氧基，当局部给药时具有强的抗炎活性，仅显示轻微的全身副作用。
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公开(公告)号：US4049804A
公开(公告)日：1977-09-20
申请号：US668394
申请日：1976-03-19
申请人： Henry Laurent , Klaus Annen , Rudolf Wiechert , Helmut Hofmeister
发明人： Henry Laurent , Klaus Annen , Rudolf Wiechert , Helmut Hofmeister
CPC分类号： C07J7/0095 , C07J7/009 , C07J71/0031
摘要： Pregnanoic acid derivatives of general formula ##STR1## wherein is a single bond or a double bond; X is hydrogen, fluorine or methyl; Y is hydrogen, fluorine or chlorine; Z is .beta.-hydroxymethylene, .beta.-acyloxymethylene, .beta.-fluoromethylene, .beta.-chloromethylene, carbonyl or methylene; R.sub.1 is hydrogen, methyl in the .alpha.- or .beta.-position or methylene and R.sub.2 is hydrogen, hydroxy or acyloxy, or R.sub.1 and R.sub.2 collectively are alkylidendioxy and U.sub.1 is halogen, halogenated alkyl of 1-5 carbon atoms or halogenated phenyl, are topically effective anti-inflammatory agents.
摘要翻译： 通式
的孕酸衍生物，其中是单键或双键; X是氢，氟或甲基; Y是氢，氟或氯; Z是β-羟基亚甲基，β-酰氧基亚甲基，β-氟亚甲基，β-氯亚甲基，羰基或亚甲基; R1是氢，α或β-位中的甲基或亚甲基，R2是氢，羟基或酰氧基，或R1和R2共同是亚烷基二氧基，U1是卤素，1-5个碳原子的卤代烷基或卤代苯基是局部的 有效的抗炎剂。 -
6.发明授权1.alpha.,2.alpha.-methylene-6-methylene- and 6.alpha.-methylpregnenes, their preparation and pharmaceutical use 失效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
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。
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7.发明授权Process for the preparation of 17.alpha.-bromoethynyl- and 17.alpha.-iodoethynyl-17.beta.-hydroxy steroids and novel products thereof 失效制备17α-溴乙炔基 - 和17α-碘代乙炔基-ββ-羟基类固醇的方法及其新产物
公开(公告)号：US4550100A
公开(公告)日：1985-10-29
申请号：US552537
申请日：1983-11-16
CPC分类号： A61K51/0493 , C07J1/0033 , C07J1/0081 , C07J63/008 , A61K2123/00
摘要： A process for preparing bromine- or iodine-unlabeled or radioactively labeled 17.alpha.-bromoethynyl- and 17.alpha.-iodoethynyl-17.beta.-hydroxy steroids of the androstane and estrane series of the partial formula ##STR1## wherein is a single bond or a double bond,V is a carbon-carbon bond or a methylene group,R is hydrogen or methyl, andX is bromine or iodine,from corresponding 17.alpha.-ethynyl-17.beta.-hydroxy steroids, comprises treating the starting steroid in an inert solvent with a brominating agent or an iodinating agent in the presence of a silver salt.The process enables production of old and new compounds having value as pharmacologically active compounds and also as diagnostic agents when the iodine or bromine is radioactive.
摘要翻译： 制备溴或碘未标记或放射性标记的17α-溴乙炔基 - 和17α-碘代乙炔基-17β-羟基类固醇的方法，所述甾族化合物和部分分子式“IMAGE”的雌激素系列是单键或双重 键，V是碳 - 碳键或亚甲基，R是氢或甲基，X是溴或碘，来自相应的17α-乙炔基-17β-羟基类固醇，包括在惰性溶剂中处理起始类固醇， 溴化剂或碘化剂在银盐存在下进行。 该方法能够生产具有价值作为药理活性化合物的老化合物和新化合物，并且当碘或溴是放射性时也可以作为诊断剂。
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公开(公告)号：US4435390A
公开(公告)日：1984-03-06
申请号：US409263
申请日：1982-08-18
申请人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Rudolf Wiechert
发明人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Rudolf Wiechert
CPC分类号： C07J5/0053 , Y10S514/826 , Y10S514/849 , Y10S514/861 , Y10S514/862 , Y10S514/863 , Y10S514/887 , Y10S514/926
摘要： Hydrocortisone derivatives of Formula I ##STR1## wherein is a single bond or a double bond,n is 1 or 2,R.sub.1 is hydrogen or methyl,R.sub.2 is alkyl of 1-6 carbon atoms, andR.sub.3 is hydrogen or 1-oxoalkyl (alkanoyl) of 2-6 carbon atoms,are pharmacologically active compounds, e.g., as antiinflammatories.
摘要翻译： 式I的氢化可的松衍生物其中是单键或双键，n是1或2，R1是氢或甲基，R2是1-6个碳原子的烷基，R3是氢或1- 2-6个碳原子的氧代烷基（烷酰基）是药理活性化合物，例如作为抗炎剂。
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9.发明授权Cyclocarbonate esters of 16.alpha.,17.alpha., dihydroxy anti-inflammatory steroids 失效16α，17α，二羟基抗炎类固醇的环碳酸酯
公开(公告)号：US4432976A
公开(公告)日：1984-02-21
申请号：US410756
申请日：1982-08-23
申请人： Klaus Annen , Henry Laurent , Helmut Hofmeister
发明人： Klaus Annen , Henry Laurent , Helmut Hofmeister
CPC分类号： C07J71/0031 , Y10S514/826 , Y10S514/849 , Y10S514/861 , Y10S514/862 , Y10S514/863 , Y10S514/887
摘要： Corticoids of Formula I ##STR1## wherein is a single bond or a double bond,X is hydrogen, fluorine, or chlorine,Y represents two hydrogen atoms or an oxygen atom, andZ is hydrogen or acyloxy of 2-6 carbon atoms, are pharmacologically active compounds, e.g., as anti-inflammatories.
摘要翻译： 式I的皮质激素（I）其中是单键或双键，X是氢，氟或氯，Y代表两个氢原子或氧原子，Z是氢或2-6碳的酰氧基 原子是药理活性化合物，例如作为抗炎剂。
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10.发明授权.DELTA..sup.9(11) - And .DELTA..sup.16 -21-chloro-20-keto steroids of the pregnane and D-homopregnane series, their preparation and use as intermediates for the synthesis of highly effective corticoids 失效DELTA 9（11） - 和DELTA 16-21-氯-20-酮类固醇的孕烷和D-均孕烷系列，它们的制备和用作合成高效皮质激素的中间体
公开(公告)号：US4404141A
公开(公告)日：1983-09-13
申请号：US356615
申请日：1982-03-09
申请人： Klaus Annen , Henry Laurent , Helmut Hofmeister
发明人： Klaus Annen , Henry Laurent , Helmut Hofmeister
CPC分类号： C07J63/008 , C07J13/005 , C07J31/006 , C07J41/005 , C07J7/0085 , C07J71/0031
摘要： .DELTA..sup.16 - and .DELTA..sup.17 -21-chloro-20-keto steroids of the formula ##STR1## wherein n is 1 or 2,C.sub.1 C.sub.2 and C.sub.9 C.sub.11 represent a CC-single or CC-double bond,R.sub.1 is H or OH,R.sub.2 is H or CH.sub.3,R.sub.3 is H or F wherein, when R.sub.3 =F, C.sub.9 C.sub.11 is a CC-single bond, andR.sub.4 is H, CH.sub.3, or F,are valuable intermediates for preparation of highly effective, known steroids.A process for preparing these compounds involves heating the corresponding 11.beta.- and/or 17.alpha.- or 17a.alpha.-nitrooxy-21-mesyloxy-20-keto steroids with lithium chloride in a dipolar aprotic solvent at temperatures above room temperature.
摘要翻译： DELTA 16-和DELTA 17-21-氯代-20-酮类固醇，其中n为1或2，C1 C2和C9 C11为CC-单或CC-双键，R1为H或OH， R2是H或CH3，R3是H或F，其中当R3 = F时，C9C11是CC-单键，R4是H，CH3或F，是制备高效，已知类固醇的有价值的中间体。 制备这些化合物的方法包括在高于室温的温度下，在偶极非质子传递溶剂中用氯化锂加热相应的11β-和/或17α-或17aα-硝基氧基-21-甲氧基-20-酮类固醇。
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