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36 条记录 (耗时 0.031 秒)

    D-homopregnanes
    14.
    发明授权
    D-homopregnanes 失效
    D-己内酯

    公开(公告)号：US4131655A

    公开(公告)日：1978-12-26

    申请号：US898070

    申请日：1978-04-20

    申请人： Leo Alig ,  Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Rudolf Wiechert

    发明人： Leo Alig ,  Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Rudolf Wiechert

    IPC分类号： A61K31/12 ,  A61K31/215 ,  A61K31/22 ,  A61K31/57 ,  A61P29/00 ,  C07J63/00 ,  C07F9/09 ,  C07C49/44

    CPC分类号： C07J63/008

    摘要： D-homopregnanes of the formula ##STR1## wherein R.sup.6 is hydrogen, chloro, fluoro or methyl; X is .beta.-hydroxymethylene or carbonyl; R.sup.17a is hydroxy, lower alkanoyloxy or aroyloxy; R.sup.21 is hydrogen, chloro, fluoro, hydroxy, lower alkanoyloxy, aroyloxy, sulfate or phosphate; and the dotted line in the 1,2-position of the A-ring denotes an additional carbon-carbon bondAnd pharmaceutically acceptable salts thereof, processes for the preparation thereof and pharmaceutical compositions containing them as the active ingredient are disclosed. The D-homopregnanes of the present invention exhibit hormonal activity and are useful for the treatment of inflammation.

    摘要翻译： 其中R6是氢，氯，氟或甲基的式XI的D-己内酯; X是β-羟基亚甲基或羰基; R17a是羟基，低级烷酰氧基或芳酰氧基; R21是氢，氯，氟，羟基，低级烷酰氧基，芳氧基，硫酸根或磷酸根; A环的1,2位的虚线表示另外的碳 - 碳键，并且其药学上可接受的盐，其制备方法和作为活性成分的药物组合物被公开。 本发明的D-己内酯具有激素活性，可用于治疗炎症。

    .DELTA..sup.9(11) -5.alpha.-20-KETO STEROIDS AND PROCESS FOR THEIR PRODUCTION
    17.
    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。

    Novel D-homo steroids
    18.
    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。

    D-homo-19-norsteroids
    19.
    发明授权
    D-homo-19-norsteroids 失效
    D-homo-19-降胆固醇

    公开(公告)号：US3984476A

    公开(公告)日：1976-10-05

    申请号：US621850

    申请日：1975-10-14

    申请人： Andor Furst ,  Marcel Muller ,  Jurg Albert Walter Gutzwiller ,  Ulrich Kerb ,  Rudolf Wiechert

    发明人： Andor Furst ,  Marcel Muller ,  Jurg Albert Walter Gutzwiller ,  Ulrich Kerb ,  Rudolf Wiechert

    IPC分类号： C07J63/00 ,  C07C49/45

    CPC分类号： C07J63/008 ,  Y10S514/843

    摘要： D-Homosteroids of the formula ##SPC1##Wherein R.sup.3 .alpha. is hydrogen, R.sup.3 .beta. is hydrogen, lower alkanoyloxy or aroyloxy and R.sup.3 .alpha. and R.sup.3 .beta. taken together are oxo; R.sup.13 is lower alkyl; R.sup.17a .beta. is hydrogen, lower alkanoyl, aroyl or lower alkyl; R.sup.17a .alpha. is hydrogen, lower alkyl, ethynyl, 1-propynyl, vinyl, chloroethynyl, butadiynyl or propadienyl and the dotted line in the A-ring denotes an additional carbon bond in either the 4,5- or 5(10)-position and processes for the preparation thereof are disclosed.The D-homosteroids of the present invention are useful as contraceptives and regulators of the female menstrual cycle.

    摘要翻译： 式中的D-类固醇，其中R3为氢，R3为氢，低级烷酰氧基或芳酰基，R3和R3为一起为氧代; R 13是低级烷基; R17aβ是氢，低级烷酰基，芳酰基或低级烷基; R17aa是氢，低级烷基，乙炔基，1-丙炔基，乙烯基，氯乙炔基，丁二炔基或丙二烯基，A环中的虚线表示在4,5-或5（10） - 位中的另外的碳键， 公开了其制备方法。

    Novel D-homosteroids
    20.
    发明授权
    Novel D-homosteroids 失效
    新型D-类固醇激素

    公开(公告)号：US4578475A

    公开(公告)日：1986-03-25

    申请号：US573983

    申请日：1984-01-26

    申请人： Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Rudolf Wiechert

    发明人： Andor Furst ,  Marcel Muller ,  Ulrich Kerb ,  Rudolf Wiechert

    IPC分类号： A61K31/15 ,  A61K31/275 ,  C07J63/00 ,  C07J71/00 ,  C07D211/70 ,  C07D307/94

    CPC分类号： C07J71/001 ,  C07J63/008 ,  C07J71/0047 ,  C07J71/0063

    摘要： The novel D-homosteroids of the formula ##STR1## wherein R.sup.1 represents a --CN, .dbd.NOH or .dbd.CH--NHOH group; R.sup.2 represents oxo or, where R.sup.1 represents a --CN group, R.sup.2 represents oxo or a --OAc group; or R.sup.1 and R.sup.2 together with carbon atoms 2 and 3 of the steroid skeleton represents a [2,3-d]-fused isoxazole ring, a [3,2-c]-fused pyrazole ring, a [3,2-c]-fused N-acylated pyrazole ring or a [2,3-c]-fused furazan ring; Ac represents an acyl group; R.sup.3 and R.sup.4 represent methyl and R.sup.5 and R.sup.6 together represent an additional bond between carbon atoms 5 and 6 of the steroid skeleton; or R.sup.4 and R.sup.5 together represent --O--, R.sup.3 represents hydrogen or methyl, and R.sup.6 represents hydrogen; R.sup.7 represents hydrogen, lower-alkyl or ethynyl; R.sup.8 represents hydroxy or acyloxy; or R.sup.7 and R.sup.8 together represent a spiroether group of the formula ##STR2## or a spirolactone group of the formula ##STR3## the dotted 16,17-bond is an optional additional carbon-carbon bond; and the dotted 2,3-bond is an additional carbon-carbon bond when R.sup.1 and R.sup.2 together with carbon atoms 2 and 3 form the isoxazole or pyrazole ring or when R.sup.2 represents a --OAc group,inhibit the synthesis of progesterone in organisms and can be used for fertility control. The novel D-homosteroids can be manufactured by molecular modifications of other D-homosteroids.

    摘要翻译： 式中，R1表示-CN，= NOH或= CH-NHOH基团的新型D-类固醇类化合物。 R 2表示氧代，或其中R 1表示-CN基，R 2表示氧代或-OCc基; 或R 1和R 2与类固醇骨架的碳原子2和3一起代表[2,3-d] - 稠合的异恶唑环，[3,2-c] - 引入的吡唑环，[3,2-c] - 引入的N-酰化吡唑环或[2,3-c] - 呋喃环; Ac表示酰基; R3和R4表示甲基，R5和R6一起代表类固醇骨架的碳原子5和6之间的附加键; 或R 4和R 5一起表示-O-，R 3表示氢或甲基，R 6表示氢; R7表示氢，低级烷基或乙炔基; R8表示羟基或酰氧基; 或者R 7和R 8一起表示式Ia的螺醚基或式Ia的螺内酯基团，点缀的16,17-键是任选的另外的碳 - 碳键; 当R 1和R 2与碳原子2和3一起形成异恶唑或吡唑环时，或当R 2表示-OAc基团时，虚线的2,3-键是另外的碳 - 碳键，抑制生物体中孕酮的合成， 用于生育控制。 新型D-类固醇可以通过其他D-类固醇激素的分子修饰来制造。