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    .DELTA..sup.9(11) -5.alpha.-20-KETO STEROIDS AND PROCESS FOR THEIR PRODUCTION
    22.
    发明授权
    .DELTA..sup.9(11) -5.alpha.-20-KETO STEROIDS AND PROCESS FOR THEIR PRODUCTION 失效
    {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。

    D-homo-20-ketopregnanes and method for inducing anesthesia or narcosis
    23.
    发明授权
    D-homo-20-ketopregnanes and method for inducing anesthesia or narcosis 失效
    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。

    Novel D-homo steroids
    24.
    发明授权
    Novel D-homo steroids 失效
    新型D-homo类固醇

    公开(公告)号：US4025563A

    公开(公告)日：1977-05-24

    申请号：US609706

    申请日：1975-09-02

    申请人： Robert C. Nickolson ,  Ulrich Kerb ,  Rudolf Wiechert

    发明人： Robert C. Nickolson ,  Ulrich Kerb ,  Rudolf Wiechert

    IPC分类号： A61K31/11 ,  C07J63/00 ,  C07C49/48

    CPC分类号： C07J63/008

    摘要： D-homo steroids of the formula ##STR1## wherein X is H, F or CH.sub.3 ; Y is H, F or Cl; Z is CH.sub.2, CO, .beta.-HOCH.sub.2, .beta.-AcOCH.sub.2 or, when Y is Cl, also .beta.-FCH.sub.2 or .beta.-ClCH.sub.2 ; R.sub.1 is H or CH.sub.3, R.sub.2 is H, OH or AcO; and one of R.sub.3 and R.sub.4 is H and the other is OH or alkoxy or both are O, possess anti-inflammatory activity.

    摘要翻译： 其中X是H，F或CH 3的式“IMAGE”的D-同型类固醇; Y为H，F或Cl; Z是CH 2，CO，β-HOCH 2，β-AcOCH 2，或者当Y是Cl时，也是β-FCH2或β-ClCH2; R1是H或CH3，R2是H，OH或AcO; R3和R4之一为H，另一个为OH或烷氧基或二者为O，具有抗炎活性。

    Process for the preparation of 17.alpha.-(3-iodobenzoyloxy)-9.alpha.-chloro-4-pregnene-3,20-diones and their D-homo homologs
    26.
    发明授权
    Process for the preparation of 17.alpha.-(3-iodobenzoyloxy)-9.alpha.-chloro-4-pregnene-3,20-diones and their D-homo homologs 失效
    17α-（3-碘苯甲酰氧基）-9α-氯-4-孕烯-3,20-二酮及其D-同系物的制备方法

    公开(公告)号：US4260464A

    公开(公告)日：1981-04-07

    申请号：US953323

    申请日：1978-10-20

    申请人： Ulrich Kerb ,  Manfred Stahnke ,  Rudolf Wiechert

    发明人： Ulrich Kerb ,  Manfred Stahnke ,  Rudolf Wiechert

    IPC分类号： C07J5/00 ,  C07J7/00 ,  C07J63/00 ,  B01J19/08

    CPC分类号： C07J5/0076 ,  C07J5/0053 ,  C07J63/00 ,  C07J7/0045 ,  Y10S204/90 ,  Y10S204/914

    摘要： Novel 17.alpha.-(3-iodobenzoyloxy)-9.alpha.-chloro-4-pregnene-3,20-diones and the D-homo homologs thereof, of the formula ##STR1## wherein n is 1 or 2;C.sub.1 -----C.sub.2 represents a C--C single or C.dbd.C double bond;R.sub.1 is hydrogen, hydroxy, or lower acyloxy;R.sub.2 is hydrogen or methyl;R.sub.3 is hydrogen, methyl or fluorine; andwhen n is 1, C.sub.15 -----C.sub.16 represents a C--C single or C.dbd.C double bond; and when n is 2, C.sub.16 -----C.sub.17 represents a C--C single or C.dbd.C double bond;which have valuable pharmacological properties and also serve as intermediates in the preparation of known pharmacologically active compounds, can be prepared by irradiating a 17.alpha.-(3-iodobenzoyloxy)-4-pregnene-3,20-dione or a D-homo homolog thereof of the formula ##STR2## with long wavelength ultraviolet radiation in the presence of phenyliodine dichloride.

    摘要翻译： 新型17α-（3-碘苯甲酰氧基）-9α-氯-4-孕烯-3,20-二酮及其同型同系物，其中n为1或2; C1 ----- C2表示C-C单或C = C双键; R1是氢，羟基或低级酰氧基; R2是氢或甲基; R3是氢，甲基或氟; 当n为1时，C15 ----- C16表示C-C单或C = C双键; 当n为2时，C16 ---- -C17表示C-C单或C = C双键; 其具有有价值的药理学性质并且还可用作制备已知的药理学活性化合物的中间体，可以通过照射17α-（3-碘苯甲酰氧基）-4-孕烯-3,20-二酮或其D-同源同系物 在具有二碘化苯二碘的存在下，具有长波长紫外线辐射的式“IMAGE”。

    .DELTA..sup.9 (11) -5.alpha.-D-homo-20-keto steroids
    27.
    发明授权
    .DELTA..sup.9 (11) -5.alpha.-D-homo-20-keto steroids 失效
    {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。

    D-homo steroids
    28.
    发明授权
    D-homo steroids 失效
    D-类固醇

    公开(公告)号：US4033995A

    公开(公告)日：1977-07-05

    申请号：US609707

    申请日：1975-09-02

    申请人： Robert C. Nickolson ,  Ulrich Kerb ,  Rudolf Wiechert

    发明人： Robert C. Nickolson ,  Ulrich Kerb ,  Rudolf Wiechert

    IPC分类号： A61K31/185 ,  A61K31/21 ,  C07J63/00

    CPC分类号： C07J63/008 ,  Y10S435/832 ,  Y10S435/911 ,  Y10S514/861 ,  Y10S514/863

    摘要： D-Homo-21-carboxylic acids of the formula ##STR1## the represents a single bond or a double bond; X is a hydrogen atom, a fluorine atom, or methylene;Y is a hydrogen atom, a fluorine atom, or a chlorine atom;Z is methylene, carbonyl, .beta.-hydroxymethylene, a .beta.-alkanoyloxymethylene or when Y is a chlorine atom, also .beta.-fluoromethylene or .beta.-chloromethylene;R.sub.1 is a hydrogen atom or methyl; andR.sub.2 is a hydrogen atom, hydroxy or alkanoyloxy; and their physiologically acceptable salts with bases and the 21-esters thereof, possess topical anti-inflammatory activity.

    摘要翻译： 式“IMAGE”的D-homo-21-羧酸代表单键或双键; X是氢原子，氟原子或亚甲基; Y是氢原子，氟原子或氯原子; Z是亚甲基，羰基，β-羟基亚甲基，β-烷酰氧基亚甲基或当Y是氯原子时，也是β-氟亚甲基或β-氯亚甲基; R1是氢原子或甲基; R2为氢原子，羟基或烷酰氧基; 并且其与碱及其21-酯的生理上可接受的盐具有局部抗炎活性。