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1. 发明授权

US4061661A .DELTA..sup.9(11) -5.alpha.-20-KETO STEROIDS AND PROCESS FOR THEIR PRODUCTION 失效
标题翻译： {66 {HU 9（11）{B -5 {60 -20-KETO STEROIDS AND PROCESS FOR PRODUCRECTION
公开(公告)号：US4061661A
公开(公告)日：1977-12-06
申请号：US693848
申请日：1976-06-08
申请人： Rudolf Wiechert , Ulrich Kerb , Otto Engelfried
发明人： Rudolf Wiechert , Ulrich Kerb , Otto Engelfried
IPC分类号： C07J7/00 , C07J1/00
CPC分类号： C07J7/002
摘要： 3.alpha.-Hydroxy and 3.alpha.-acyloxy- .DELTA..sup.9(11) -5.alpha.-20-ketopregnenes of the formula ##STR1## wherein R is hydrogen or acyl, R.sub.1 is hydrogen or methyl and R.sub.2 is methyl or ethyl, are produced by esterifying a corresponding 3.beta.-hydroxy-5.alpha.-20-keto pregnane of the formula ##STR2## wherein R.sub.1 and R.sub.2 have the values given above, with m-iodobenzoic acid with inversion of the 3.beta.-oxy group to a 3.alpha.-oxy group; chlorinating the thus-produced 3.alpha.-m-iodobenzoyl ester with dichloroiodobenzene under irradiation; and treating the reaction product with a dehydrohalogenating silver salt. Optionally thereafter, the 3.alpha.-iodobenzoyl group is split off in a conventional manner to produce the corresponding 3.alpha.-hydroxy steroid and optionally the thus-produced 3.alpha.-hydroxy steroid is esterified to produce a desired 3-ester thereof.
摘要翻译： 3α-羟基和3α-酰氧基-TATA 9（11）-5α-α-酮戊二酸，其中R是氢或酰基，R 1是氢或甲基，R 2是甲基或乙基，由酯化相应的具有式（IMAGE）的3β-羟基-5α-20-酮孕烷，其中R1和R2具有上述给出的值，将间苯二甲酸与3β-氧基转化为3α- 氧基; 在照射下用二碘碘苯氯化如此制备的3α-碘代苯甲酰基酯; 并用脱卤化氢的银盐处理反应产物。此后任选地，以常规方式将3α-碘代苯甲酰基分离出来以产生相应的3α-羟基类固醇，任选地，由此产生的3α-羟基类固醇被酯化以产生所需的3-酯。

2. 发明授权

US4056633A D-homo-20-ketopregnanes and method for inducing anesthesia or narcosis 失效
标题翻译： D-均聚-20-酮戊二酸和诱导麻醉或麻醉的方法
公开(公告)号：US4056633A
公开(公告)日：1977-11-01
申请号：US641602
申请日：1975-12-17
申请人： Ulrich Kerb , Rudolf Wiechert , Helmut Wachtel , Otto Engelfried , Klaus Kieslich
发明人： Ulrich Kerb , Rudolf Wiechert , Helmut Wachtel , Otto Engelfried , Klaus Kieslich
IPC分类号： A61K31/12 , A61K31/56 , C07J63/00 , C07J71/00 , C01B33/24
CPC分类号： C07J71/001 , C07J63/008
摘要： D-homo-20-ketopregnanes of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, alkyl, alkoxy, or azido;R.sub.2 is oxygen, ##STR2## and R.sub.7 is hydrogen, lower alkyl, or acyl of up to 5 carbon atoms; R.sub.3 is hydrogen or methylR.sub.4 is oxygen, two hydrogens, ##STR3## R.sub.5 is hydrogen, hydroxy, alkoxy, azido, mercapto, thiocyano, cyano, dialkylamino, morpholino, thiomorpholino, or piperazino;R.sub.6 is methyl or ethyl;The hydrogen atom in the 5-position is of the .alpha.- or .beta.-configuration;And acid addition salts thereof, possess narcotic-anesthetic activity.
摘要翻译：其中R 1是氢，氟，氯，溴，烷基，烷氧基或叠氮基的D-均聚-20-酮戊酸; R2是氧，R7是氢，低级烷基或至多5个碳原子的酰基; R3是氢或甲基R4是氧，两个氢，R5是氢，羟基，烷氧基，叠氮基，巯基，硫氰基，氰基，二烷基氨基，吗啉代，硫代吗啉代或哌嗪基; R6是甲基或乙基; 5位氢原子是α - 或β - 配位体; 和酸添加剂，它的最佳的NARCOTIC-ANESTHETIC活动。

3. 发明授权

US4097678A .DELTA..sup.9 (11) -5.alpha.-D-homo-20-keto steroids 失效
标题翻译： {66 {HU 9（11）{B -5 {60-D-homo-20-keto类固醇
公开(公告)号：US4097678A
公开(公告)日：1978-06-27
申请号：US693847
申请日：1976-06-08
申请人： Ulrich Kerb , Rudolf Wiechert , Otto Engelfried
发明人： Ulrich Kerb , Rudolf Wiechert , Otto Engelfried
IPC分类号： C07J63/00
CPC分类号： C07J63/008
摘要： 3.alpha.-Hydroxy and 3.alpha.-acyloxy- .DELTA..sup.9(11) -5.alpha.-D-homo-20-ketopregnenes of the formula ##STR1## wherein R is hydrogen or acyl, R.sub.1 is hydrogen or methyl and R.sub.2 is methyl or ethyl, are produced by esterifying a corresponding 3.beta.-hydroxy-5.alpha.-20-keto pregnane of the formula ##STR2## wherein R.sub.1 and R.sub.2 have the values given above, with m-iodo-benzoic acid with inversion of the 3.beta.-oxy group to a 3.alpha.-oxy group; chlorinating the thus-produced 3.alpha.-m-iodobenzoyl ester with dichloroiodobenzene under irradiation; and treating the reaction product with a dehydrohalogenating silver salt. Optionally thereafter, the 3.alpha.-iodobenzoyl group is split off in a conventional manner to produce the corresponding 3.alpha.-hydroxy steroid and optionally the thus-produced 3.alpha.-hydroxy steroid is esterified to produce a desired 3-ester thereof.
摘要翻译： 3α-羟基和3α-酰氧基-TATA 9（11）-5α-D-高-20-酮戊二酸，其中R是氢或酰基，R 1是氢或甲基，R 2是甲基或乙基通过酯化相应的具有上述给出的值的式“IMAGE”的相应的3β-羟基-5α-20-酮孕烷与通过3β-氧代反相的间 - 碘 - 苯甲酸组成3个α氧基; 在照射下用二碘碘苯氯化如此制备的3α-碘代苯甲酰基酯; 并用脱卤化氢的银盐处理反应产物。此后任选地，以常规方式将3α-碘代苯甲酰基分离出来以产生相应的3α-羟基类固醇，任选地，由此产生的3α-羟基类固醇被酯化以产生所需的3-酯。

4. 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。

5. 发明授权

US3935245A Radioactively labeled steroid derivatives 失效
标题翻译：放射性标记的类固醇衍生物
公开(公告)号：US3935245A
公开(公告)日：1976-01-27
申请号：US476279
申请日：1974-06-04
申请人： Otto Engelfried , Bob Nieuweboer , Karl Petzoldt , Ulrich Kerb , Klaus Lubke
发明人： Otto Engelfried , Bob Nieuweboer , Karl Petzoldt , Ulrich Kerb , Klaus Lubke
IPC分类号： G01N33/53 , A61K51/04 , C07J1/00 , C07J7/00 , C07J13/00 , C07J41/00 , C07J43/00 , C07J53/00 , C07J71/00 , C12P33/00 , G01N33/74 , C07J9/00
CPC分类号： A61K51/0493 , C07J1/0011 , C07J1/0025 , C07J1/0059 , C07J1/007 , C07J1/0096 , C07J13/005 , C07J41/0005 , C07J43/003 , C07J53/005 , C07J7/002 , C07J7/003 , C07J71/001 , G01N33/743 , A61K2121/00
摘要： Steroids bearing the substituent --X-NR.sub.1 R.sub.2 wherein --NR.sub.1 R.sub.2 is a tritium of carbon-14 labeled amino or amino-acid group and --X-- is --R.sub.3 --, --OCOR.sub.3 --, =N--O--R.sub.3 -- or --NHCOR.sub.3 -- wherein R.sub.3 is --(CH.sub.2).sub.n CO-- in which n is 0-4, are useful as diagnostic agents.
摘要翻译：带有取代基-X-NR1R2的类固醇，其中-NR1R2是碳-14标记的氨基或氨基酸基团的氚，-X-是-R3-，-OCOR3-，= NO-R3-或-NHCOR3-，其中R3是 - （CH2）nCO-，其中n为0-4，可用作诊断剂。

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