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101. 发明授权

US5093507A 10.beta.,11.beta.-bridged steroids 失效
标题翻译： 10（BETA），11（BETA）-BRIDGED STEROIDS
公开(公告)号：US5093507A
公开(公告)日：1992-03-03
申请号：US367165
申请日：1989-06-16
申请人： Cornelius Scheidges , Eckhard Ottow , Gunter Neef , Sybille Beier , Walter Elger
发明人： Cornelius Scheidges , Eckhard Ottow , Gunter Neef , Sybille Beier , Walter Elger
IPC分类号： A61K31/58 , A61P3/06 , A61P3/08 , A61P5/38 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P17/00 , A61P27/02 , A61P35/00 , A61P43/00 , C07B61/00 , C07J31/00 , C07J41/00 , C07J63/00 , C07J71/00
CPC分类号： C07J31/003 , C07J41/0044 , C07J71/0078
摘要： 10.beta.,11.beta.-bridged steroids of Formula I ##STR1## wherein R.sup.1 is H or methyl;R.sup.2 is H, a cyanide residue, a heteroaryl residue, a straight-chain or branched aliphatic, e.g., alkyl group of up to 20 carbon atoms, optionally exhibiting double or triple bonds and, if desired, being substituted by one or several oxo groups, a C.sub.4-7 cycloalkyl or C.sub.4-7 cycloalkenyl group, an OR.sup.3 --, SR.sup.3 --, --OSO.sub.2 --R.sup.11 -- group wherein R.sup.11 means a perfluroinated C.sub.1 -C.sub.4 -alkyl group or an NR.sup.3 R.sup.4 -group wherein R.sup.3 means an H atom or C.sub.1 -C.sub.8 -alkyl residue, R.sup.4 means R.sup.3, a cyanide or a C.sub.1 -C.sub.10 -acyl residue, or R.sup.3 and R.sup.4 jointly with the inclusion of N means of 5- or 6-membered heterocyclic ring wherein the ring can additionally contain a further hetero atom N, O, or S, or a 4-cyano-, 4-methoxy- or 4-dimethylamino-substituted phenyl group,A and B either mean jointly a further bond between C4 and C5, or A is an .alpha.-hydroxy group and B is H,X is a keto or oxime group, andZ is a pentagonal or hexagonal ring residue which is optionally substituted and optionally unsaturated,or pharmaceutically compatible acid additional salts thereof which possess antigestagen and antiglucocorticoid properties.
摘要翻译： 10β，11β-桥连类固醇，其中R1是H或甲基; R2是H，氰化物残基，杂芳基残基，直链或支链脂族，例如至多20个碳原子的烷基，任选地表现出双键或三键，并且如果需要，被一个或几个氧代基团，C4-7环烷基或C4-7环烯基，OR3-，SR3-，-OSO2-R11-基，其中R11表示全氟化C1-C4-烷基或NR3R4-基团，其中R3表示H原子或C1 -C 8 - 烷基残基，R4表示R3，氰化物或C1-C10酰基残基，或R3和R4与N或5元或6元杂环的N基相结合，其中环可以另外含有另外的杂原子原子N，O或S或4-氰基 - ，4-甲氧基 - 或4-二甲基氨基取代的苯基，A和B可以共同意指C4和C5之间的另一个键，或A是α-羟基并且B是H，X是酮基或肟基，Z是任选被取代且任选不饱和的五
角或六方晶的残基，或药学上相容性其酸性附加盐，其具有抗老化和抗糖皮质激素特性。

102. 发明授权

US4891368A Use of antigestagens for softening the nonpregnant cervix 失效
标题翻译：使用抗前列腺素软化非妊娠宫颈
公开(公告)号：US4891368A
公开(公告)日：1990-01-02
申请号：US287258
申请日：1988-12-21
申请人： Krzysztof Chwalisz , Sybille Beier , Angelika Esch , Walter Elger
发明人： Krzysztof Chwalisz , Sybille Beier , Angelika Esch , Walter Elger
IPC分类号： A61K31/565 , A61K31/575 , A61P3/04 , A61P13/02 , A61P15/00 , C07J1/00 , C07J41/00 , C07J63/00
CPC分类号： A61K31/575 , A61K31/565 , Y10S514/01
摘要： Antigestagens are useful for softening the nonpregnant cervix.
摘要翻译：抗消化药用于软化非妊娠宫颈。

103. 发明授权

US4870069A 11.beta.-alkynyl-estrenes and -estradienes, their production and pharmaceutical preparations containing them 失效
标题翻译： 11β-炔基 - 雌酮和雌二醇，其生产和含有它们的药物制剂
公开(公告)号：US4870069A
公开(公告)日：1989-09-26
申请号：US147475
申请日：1988-01-25
申请人： Eckhard Ottow , Rudolf Wiechert , Guenter Neef , Juergen Bardenhagen , Sybille Beier , Walter Elger , David Henderson
发明人： Eckhard Ottow , Rudolf Wiechert , Guenter Neef , Juergen Bardenhagen , Sybille Beier , Walter Elger , David Henderson
IPC分类号： A61K31/565 , A61K31/57 , A61K31/58 , A61P5/38 , C07J1/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J17/00 , C07J21/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J63/00 , C07J71/00
CPC分类号： C07J1/0059 , C07J1/0081 , C07J1/0096 , C07J17/00 , C07J21/00 , C07J21/003 , C07J31/006 , C07J33/002 , C07J41/0077 , C07J43/003 , C07J71/001
摘要： 11.beta.-substituted steroids of the formula ##STR1## wherein A and B together represent a second bond between the 6-position and 7-position carbon atoms, or, respectively, are each H;X is O, two H atoms or hydroximino;Z is the residue of a pentagonal or hexagonal ring which is optionally substituted and optionally saturated;R.sup.1 is vinyl, C.sub.3-7 -cyclo-1-alkenyl, phenyl, naphthyl or 5- or 6-membered heterocyclic aromatic having at least one N, O or S atom, each being unsubstituted or substituted by 1-3 halogen atoms, 1-3 C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -acyl, C.sub.2-10 -alkenyl, C.sub.1-4 -acyloxy, phenyl, nitro, hydroxy, carboxy, cyanide, COOR.sup.4 or amino optionally substituted by 1-2 C.sub.1-4 -alkyl;R.sup.2 is methyl or ethyl,R.sup.3 is H, Cl or methyl; andR.sup.4 is C.sub.1-4 -alkyl optionally substituted by phenyl which itself is optionally substituted by C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, halogen or phenylhave valuable pharmacological properties.
摘要翻译：其中A和B一起表示6位和7-位碳原子之间的第二键，或分别为H; X是O，两个H原子或肟基; Z是任选被取代且任选饱和的五边形或六方晶环的残基; R1是具有至少一个N，O或S原子的乙烯基，C 3-7 - 环-1-链烯基，苯基，萘基或5-或6-元杂环芳族，各自未被取代或被1-3个卤素原子取代，1 -3 C 1-4 - 烷基，C 1-4 - 烷氧基，C 1-4 - 酰基，C 2-10 - 烯基，C 1-4 - 酰氧基，苯基，硝基，羟基，羧基，氰基，COOR 4或任选被1- 2 C 1-4 - 烷基; R2是甲基或乙基，R3是H，C1或甲基; R4是任选被苯基取代的C 1-4 - 烷基，其本身任选被C 1-4 - 烷基，C 1-4 - 烷氧基，卤素或苯基取代，具有有价值的药理学性质。

104. 发明授权

US4829060A 11 Beta-N,N-dimethylaminophenyl-estradienes, their manufacture and pharmaceutical preparations containing them 失效
标题翻译： 11β-N，N-二甲基氨基苯基 - 雌二醇，其制备和含有它们的药物制剂
公开(公告)号：US4829060A
公开(公告)日：1989-05-09
申请号：US832604
申请日：1986-02-24
申请人： Eckhard Ottow , Guenter Neef , Ralph Rohde , Rudolf Wiechert , Sybille Beier , Walter Elger , David Henderson
发明人： Eckhard Ottow , Guenter Neef , Ralph Rohde , Rudolf Wiechert , Sybille Beier , Walter Elger , David Henderson
IPC分类号： A61K31/565 , A61P5/38 , C07J41/00
CPC分类号： C07J41/0083
摘要： Descriptions are given of 11.beta.-aryl-estradienes of general formula I ##STR1## where X means an oxygen atom or a hydroxyimino group N.about.OH, where the hydroxy group may be in the syn or anti position,R.sup.1 means a methyl or ethyl groupR.sup.2 means a --C.tbd.C--CH.dbd.CH.sub.2, a --CH.sub.2 --(CH.sub.2).sub.n --Y--R.sup.3 or a --CH.dbd.CH--(CH.sub.2).sub.m --Y--R.sup.3 group,Y standing for an oxygen or sulfur atom, n for numbers 0 or 1, m for numbers 1, 2 or 3 and R.sup.3 for a hydrogen atom, for an alkyl or acyl radical with 1 to 4 carbon atoms respectively,with the proviso that when m stands for 1 and Y for an oxygen atom, R.sup.3 means an alkyl radical with 1 to 4 carbon atoms.The new 11.beta.-aryl-estradienes possess antigestagenic and antiglucocorticoid effects.
摘要翻译：给出了通式I（I）的11个β-芳基 - 雌二醇的描述，其中X表示氧原子或羟基亚氨基N差异OH，其中羟基可以在顺式或反位，R1表示甲基或乙基R2表示-C3OND C-CH = CH2，-CH2-（CH2）nY-R3或-CH = CH-（CH2）mY-R3基团，Y表示氧或硫原子， n为0或1，m为1,2或3，R3为氢原子，分别为具有1至4个碳原子的烷基或酰基，条件是当m表示1时，Y表示氧原子，R3表示具有1至4个碳原子的烷基。新的11β-芳基 - 雌二醇具有抗前列腺素和抗糖皮质激素作用。

105. 发明授权

US4738957A Estriol esters 失效
标题翻译：雌三醇酯
公开(公告)号：US4738957A
公开(公告)日：1988-04-19
申请号：US842691
申请日：1986-03-21
申请人： Henry Laurent , Dieter Bittler , Sybille Beier , Walter Elger
发明人： Henry Laurent , Dieter Bittler , Sybille Beier , Walter Elger
IPC分类号： A61K31/565 , C07J1/00 , A61K31/56
CPC分类号： C07J1/0059 , C07J1/007
摘要： Estriol esters of Formula I ##STR1## wherein R is, in each case, the residue of an aliphatic monocarboxylic acid of 3-10 carbon atoms,surpass estriol in strength and duration of estrogen activity.
摘要翻译：式I的雌三醇酯（I）其中R是每种情况下的3-10个碳原子的脂肪族单羧酸的残基，超过雌三醇的强度和雌激素活性持续时间。

106. 发明授权

US4489092A Prostanoic acid derivatives and their preparation 失效
标题翻译：前列腺酸衍生物及其制备
公开(公告)号：US4489092A
公开(公告)日：1984-12-18
申请号：US413940
申请日：1982-09-01
申请人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
发明人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
IPC分类号： A61K31/27 , A61K31/19 , A61K31/215 , A61K31/255 , A61K31/275 , A61P43/00 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/535 , C07C177/00 , A61K31/557
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0041 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07F9/5352
摘要： Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is an acid, ester, amide or hydroxyalkylene group; R.sub.2 and R.sub.3 are H or alkyl; R.sub.4 and R.sub.5 are both CH.sub.3 or one is Cl and the other is CH.sub.3 ; A is CH.sub.2 CH.sub.2 or --CH.dbd.CH; B is CH.sub.2 CH.sub.2, trans-CH.dbd.CH, --C.tbd.C-- or ##STR2## W is free or functionally modified hydroxyalkylene or carbonyl; Z is free or functionally modified hydroxymethylene or carbonyl; X Y is either ##STR3## or, when Z is free or functionally modified hydroxymethylene, ##STR4## or, when Z is free or functionally modified carbonyl, --CH.dbd.CH--, R.sub.12 being H, CH.sub.3, CH or free or functionally modified hydroxy; and physiologically acceptable salts thereof when R.sub.1 is an acid group, possess pharmacological activity, including abortion triggering activity.
摘要翻译：其中R1是酸，酯，酰胺或羟基亚烷基的式IMA曲前酯衍生物; R2和R3是H或烷基; R4和R5都是CH3，一个是Cl，另一个是CH3; A是CH 2 CH 2或-CH = CH; B是CH 2 CH 2，反式-CH = CH，-C 3 D或W是游离或官能改性的羟基亚烷基或羰基; Z是游离的或官能改性的羟基亚甲基或羰基; 或者当Z是游离的或官能改性的羟基亚甲基时，或者当Z是游离的或官能改性的羰基时，-CH = CH-，R 12是H，CH 3，CH或游离或官能改性的羟基 ; 当R1为酸基时，其生理上可接受的盐具有药理活性，包括流产触发活性。

107. 发明授权

US4468395A Prostaglandins and prostacyclins, processer for their preparation and their use as medicaments 失效
标题翻译：前列腺素和前列腺素，其制备过程及其用作药物
公开(公告)号：US4468395A
公开(公告)日：1984-08-28
申请号：US380326
申请日：1982-05-20
申请人： VorbruHelmut , Walter Elger , Michael-Harold Town , Ekkehard Schillinger
发明人： VorbruHelmut , Walter Elger , Michael-Harold Town , Ekkehard Schillinger
IPC分类号： C07C405/00 , C07D263/14 , C07D277/10 , C07D417/12 , C07F7/18 , C07D233/14 , A61K31/42
CPC分类号： C07D417/12 , C07C405/0041 , C07D263/14 , C07D277/10 , C07F7/1856
摘要： Compounds of Formula I ##STR1## wherein R.sub.1 is a prostaglandin or prostacyclin residue;Y is oxygen, sulfur, imino, or N-(C.sub.1 -C.sub.4 -alkyl) imino;Q is (CR.sub.6 R.sub.7).sub.p wherein p is an integer of 0 to 3;R.sub.2 is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; C.sub.1 -C.sub.4 -alkoxycarbonyl; benzyloxycarbonyl; cyano; or di-C.sub.1 -C.sub.4 -alkylaminocarbonyl;R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each independently is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; or aryl; andR.sub.3 and R.sub.4 together form a trimethylene, tetramethylene, or 1,3-butadienylene group when R.sub.2 and R.sub.5 together represent a direct bond;have valuable pharmacological properties, e.g., as blood-pressure-lowering or abortive agents.
摘要翻译：式I的化合物其中R 1是前列腺素或前列环素残基; Y是氧，硫，亚氨基或N-（C 1 -C 4 - 烷基）亚氨基; Q是（CR 6 R 7）p，其中p是0至3的整数; R2是氢; 任选被羟基或氨基取代的1-6个碳原子的烷基; C 1 -C 4烷氧基羰基; 苄氧羰基氰基; 或二-C 1 -C 4烷基氨基羰基; R3，R4，R5，R6和R7各自独立地为氢; 任选被羟基或氨基取代的1-6个碳原子的烷基; 或芳基; 当R 2和R 5一起代表直接键时，R 3和R 4一起形成三亚甲基，四亚甲基或1,3-丁二烯基; 具有有价值的药理学性质，例如作为降血压药或降血糖药。

108. 发明授权

US4359467A Prostanoic acid derivatives and their preparation 失效
标题翻译：前列腺酸衍生物及其制备
公开(公告)号：US4359467A
公开(公告)日：1982-11-16
申请号：US256369
申请日：1981-04-22
申请人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
发明人： Helmut Vorbruggen , Norbert Schwarz , Olaf Loge , Walter Elger
IPC分类号： A61K31/27 , A61K31/19 , A61K31/215 , A61K31/255 , A61K31/275 , A61P43/00 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07F9/535 , C07C177/00 , A61K31/557
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0016 , C07C405/0025 , C07C405/0041 , C07C51/38 , C07C57/03 , C07C57/13 , C07C57/52 , C07F9/5352
摘要： Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is an acid, ester, amide or hydroxyalkylene group; R.sub.2 and R.sub.3 are H or alkyl; R.sub.4 and R.sub.5 are both CH.sub.3 or one is Cl and the other is CH.sub.3 ; A is CH.sub.2 CH.sub.2 or --CH.dbd.CH; B is CH.sub.2 CH.sub.2, trans- ##STR2## W is free or functionally modified hydroxyalkylene or carbonyl; Z is free or functionally modified hydroxymethylene or carbonyl; X Y is either ##STR3## or, when Z is free or functionally modified hydroxymethylene, ##STR4## or, when Z is free or functionally modified carbonyl, --CH.dbd.CH--, R.sub.12 being H, CH.sub.3, CN or free or functionally modified hydroxy; and physiologically acceptable salts thereof when R.sub.1 is an acid group, possess pharmacological activity, including abortion triggering activity.
摘要翻译：其中R1是酸，酯，酰胺或羟基亚烷基的式IMA曲前酯衍生物; R2和R3是H或烷基; R4和R5都是CH3，一个是Cl，另一个是CH3; A是CH 2 CH 2或-CH = CH; B是CH 2 CH 2，反式 - W是游离的或官能改性的羟基亚烷基或羰基; Z是游离的或官能改性的羟基亚甲基或羰基; 或者当Z是游离或官能改性的羟基亚甲基时，或者当Z是游离或官能改性羰基时，-CH = CH-，R 12是H，CH 3，CN或游离或官能改性的羟基 ; 当R1为酸基时，其生理上可接受的盐具有药理活性，包括流产触发活性。

109. 发明授权

US4337311A 15 Hydroxylation of 1.alpha.,2.alpha.-methylene steroids 失效
标题翻译： 15个α，2个α-亚甲基类固醇的羟基化
公开(公告)号：US4337311A
公开(公告)日：1982-06-29
申请号：US96349
申请日：1979-11-21
申请人： Karl Petzoldt , Hermann Steinbeck , Walter Elger
发明人： Karl Petzoldt , Hermann Steinbeck , Walter Elger
IPC分类号： C12P33/12 , A61K31/57 , A61P17/00 , C07J7/00 , C07J53/00
CPC分类号： C07J53/005
摘要： Steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 are identical or different and each is hydrogen or the residue of an organic or inorganic acid,and for the esters (R.sub.1 or R.sub.2 is not H) capable of salt formation, the salts thereof, possess valuable pharmacoligical properties, e.g., good antiandrogenic activity with low progestational activity.
摘要翻译：其中R1和R2相同或不同，并且各自为氢或有机酸或无机酸的残基，并且对于能够形成盐的酯（R 1或R 2不是H），其盐，具有宝贵的药理学性质，例如良好的抗雄激素活性，具有较低的孕激素活性。

110. 发明授权

US4196204A Hydroxylated 1 alpha, 2 alpha-methylene steroids 失效
标题翻译：羟化1α，2α-亚甲基类固醇
公开(公告)号：US4196204A
公开(公告)日：1980-04-01
申请号：US886014
申请日：1978-03-13
申请人： Karl Petzoldt , Hermann Steinbeck , Walter Elger
发明人： Karl Petzoldt , Hermann Steinbeck , Walter Elger
IPC分类号： C12P33/12 , A61K31/57 , A61P17/00 , C07J7/00 , C07J53/00 , A61K31/58 , C07J3/00
CPC分类号： C07J53/005
摘要： Steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 are identical or different and each is hydrogen or the residue of an organic or inorganic acid,and for the esters (R.sub.1 or R.sub.2 is not H) capable of salt formation, the salts thereof, possess valuable pharmacological properties, e.g., good antiandrogenic activity with low progestational activity.
摘要翻译：其中R1和R2相同或不同，并且各自为氢或有机酸或无机酸的残基，并且对于能够形成盐的酯（R 1或R 2不是H），其盐，具有宝贵的药理性质，例如具有低促孕活性的良好的抗雄激素活性。

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