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1. 发明授权

US5132299A 11.beta.-phenyl-4,9,15-estratrienes, their manufacture and pharmaceutical preparations containing same 失效
标题翻译： 11（BETA）-PHENYL-4,9,15-ESTRATRIENES，其制造和含有其的药物制剂
公开(公告)号：US5132299A
公开(公告)日：1992-07-21
申请号：US458668
申请日：1990-01-16
申请人： Eckhard Ottow , Helmut Hofmeister , Stefan Scholz , Guenter Neef , Walter Elger , Sybille Beier , Krzysztof Chwalisz
发明人： Eckhard Ottow , Helmut Hofmeister , Stefan Scholz , Guenter Neef , Walter Elger , Sybille Beier , Krzysztof Chwalisz
IPC分类号： C07J1/00 , C07J3/00 , C07J21/00 , C07J41/00 , C07J51/00
CPC分类号： C07J51/00 , C07J1/0096 , C07J21/006 , C07J41/0083
摘要： New 11.beta. phenyl-4,9,15-estratrienes of formula I ##STR1## are described, where X implies an oxygen atom or a hydroxyimino grouping N.about.OH,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 implies a hydrogen atom, an alkyl radical or an acyl radical with in each case 1 to 10 carbon atoms,R.sup.3 stands for a hydrogen atom, a cyanomethyl group, --(CH.sub.2).sub.n CH.sub.2 Z where n implies the numbers 0, 1, 2, 3, 4 or 5, Z=--H or --OR.sup.5 with R.sup.5 having the significance of a hydrogen atom or an alkyl or acyl group with in each case 1 to 10 carbon atoms, or for --(CH.sub.2).sub.m --C.tbd.C--Y where m=0-2 and Y implies a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group with in each case 1 to 10 carbon atoms,R.sup.4 represents a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 8 carbon atoms which contains the grouping ##STR2## with X having the above significance. The compounds have antigestagenic and antiglucocorticoid activity.
摘要翻译： PCT No.PCT / DE88 / 00447 Sec。 371日期1990年1月16日 102（e）日期1990年1月16日PCT提交1988年7月15日PCT公布。出版物WO89 / 00578 日本1月26日，1989年。新的11β型苯基-4,9,15-雌三醇，其中X表示氧原子或羟基亚氨基，N代表OH，R1代表氢原子或甲基，R2表示氢原子，烷基或酰基，在每种情况下为1-10个碳原子，R3表示氢原子，氰基甲基， - （CH2）nCH2Z其中n表示数字 0,1,2,3,4或5，Z = -H或-OR 5，其中R 5具有氢原子或烷基或酰基的含义，在每种情况下为1-10个碳原子，或 - （CH 2） mC 3BOND CY，其中m = 0-2，Y表示氢，氯，氟，碘或溴原子，烷基，羟基烷基，烷氧基烷基或酰氧基烷基，在每种情况下为1-10个碳原子，R4表示直链或含有至多8个碳原子的支链，饱和或不饱和烃基，其含有具有上述意义的X的分组。这些化合物具有抗前列腺素和抗糖皮质激素活性。

2. 发明授权

US5273971A 13-alkyl-11.beta.-phenylgonanes 失效
标题翻译： 13-烷基-11β-苯并二氢呋喃
公开(公告)号：US5273971A
公开(公告)日：1993-12-28
申请号：US374809
申请日：1989-07-03
申请人： Stefan Scholz , Eckhard Ottow , Guenter Neef , Walter Elger , Sybille Beier , Krzysztof Chwalisz
发明人： Stefan Scholz , Eckhard Ottow , Guenter Neef , Walter Elger , Sybille Beier , Krzysztof Chwalisz
IPC分类号： A61K31/58 , A61K31/00 , A61K31/585 , A61P5/00 , A61P5/36 , A61P35/00 , C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J15/00 , C07J17/00 , C07J21/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J71/00
CPC分类号： C07J71/001 , C07J1/0088 , C07J15/00 , C07J17/00 , C07J33/002 , C07J41/0094 , C07J43/003 , C07J51/00
摘要： There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.
摘要翻译：提供式I的13-烷基-11β-苯基 - 正膦（I）其中Z是氧原子或N-OH; R2是α-或β-位甲基或乙基; R 1选自杂芳基，环烷基，环烯基，芳基，烯基和其中R2为α-位的烷基和R2为β-位的乙基; 并且R3和R4选自两个不同取代基组之一，进行选择的基团由R2的位置确定。

3. 发明授权

US5446036A 13-alkyl-11beta-phenylgonanes 失效
标题翻译： 13-烷基-11β-苯基庚烷
公开(公告)号：US5446036A
公开(公告)日：1995-08-29
申请号：US144474
申请日：1993-11-02
申请人： Stefan Scholz , Eckhard Ottow , Guenter Neef , Walter Elger , Sybille Beier , Krzysztof Chwalisz
发明人： Stefan Scholz , Eckhard Ottow , Guenter Neef , Walter Elger , Sybille Beier , Krzysztof Chwalisz
IPC分类号： A61K31/58 , A61K31/00 , A61K31/585 , A61P5/00 , A61P5/36 , A61P35/00 , C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J15/00 , C07J17/00 , C07J21/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J71/00 , C07J19/00
CPC分类号： C07J71/001 , C07J1/0088 , C07J15/00 , C07J17/00 , C07J33/002 , C07J41/0094 , C07J43/003 , C07J51/00
摘要： There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.
摘要翻译：提供式I的13-烷基-11β-苯基 - 正膦（I）其中Z是氧原子或N-OH; R2是α-或β-位甲基或乙基; R 1选自杂芳基，环烷基，环烯基，芳基，烯基和其中R2为α-位的烷基和R2为β-位的乙基; 并且R3和R4选自两个不同取代基组之一，进行选择的基团由R2的位置确定。

4. 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。

5. 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。

6. 发明授权

US4536401A 11.beta.-aryl estradienes, processes for their production and pharmaceutical preparations containing them 失效
标题翻译： 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。

7. 发明授权

US4870067A Oxytocins and antigestagens in combination for induction of birth 失效
标题翻译：催产素和抗生素联合用于诱导出生
公开(公告)号：US4870067A
公开(公告)日：1989-09-26
申请号：US904133
申请日：1986-09-05
申请人： Krzsysztof Chwalisz , Sybille Beier , Walter Elger , Guenter Neef
发明人： Krzsysztof Chwalisz , Sybille Beier , Walter Elger , Guenter Neef
IPC分类号： A61K31/56 , A61K31/565 , A61K38/11 , A61K45/06 , A61P13/02 , A61P15/00
CPC分类号： A61K38/11 , Y10S514/935
摘要： A combination product contains oxytocin and/or an oxytocin analog and an antigestagen for induction of birth.
摘要翻译：组合产品含有催产素和/或催产素类似物和用于诱导出生的抗丝氨酸。

8. 发明授权

US06596713B1 Steroid esters and amides, process for their production and their pharmaceutical use 失效
标题翻译：类固醇酯和酰胺，其生产过程及其药物用途
公开(公告)号：US06596713B1
公开(公告)日：2003-07-22
申请号：US08914176
申请日：1997-08-19
申请人： Ulrich Klar , Arwed Cleve , Guenter Neef , Eckhard Ottow , Klaus Stoekemann , Karl-Heinrich Fritzemeier
发明人： Ulrich Klar , Arwed Cleve , Guenter Neef , Eckhard Ottow , Klaus Stoekemann , Karl-Heinrich Fritzemeier
IPC分类号： A61K3156
CPC分类号： C07J53/00 , C07J41/0083 , C07J41/0094 , C07J53/002
摘要： New steroids and amides of formula I are described, in which the variables are defined by the description. Relative to the basic hydroxy compounds (“initial compounds”), the new compounds are distinguished by a considerably improved solubility and partially also by increased biological action and selectivity. The new compounds are suitable for the production of pharmaceutical agents.
摘要翻译：描述了新的类固醇和酰胺，其中变量由描述定义。相对于碱性羟基化合物（“初始化合物”），新化合物通过显着改善的溶解度和部分地通过增加的生物作用和选择性来区分。新化合物适用于制药。

9. 发明授权

US4596808A Pharmacologically active 3-substituted beta-carbolines useful as tranquilizers 失效
标题翻译：药理活性的3-取代的β-咔啉可用作镇定剂
公开(公告)号：US4596808A
公开(公告)日：1986-06-24
申请号：US556869
申请日：1983-12-01
申请人： Claus T. Braestrup , Jogen A. Christensen , Mogens Engelstoft , Guenter Neef , Ulrich Eder , Ralph Schmiechen , Andreas Huth , Dieter Rahtz , Dieter Seidelmann , Wolfgang Kehr , Dieter Palenschat
发明人： Claus T. Braestrup , Jogen A. Christensen , Mogens Engelstoft , Guenter Neef , Ulrich Eder , Ralph Schmiechen , Andreas Huth , Dieter Rahtz , Dieter Seidelmann , Wolfgang Kehr , Dieter Palenschat
IPC分类号： A61K31/435 , A61K31/44 , A61K31/445 , A61K31/675 , A61P25/00 , A61P25/20 , C07D209/08 , C07D209/20 , C07D471/04 , C07F9/6561 , C07D487/14
CPC分类号： C07D471/04 , C07D209/08 , C07D209/20 , C07F9/6561
摘要： 3-Substituted beta-carbolines of the formula ##STR1## wherein R.sup.A is H, F, Cl, Br, I, NO.sub.2, CN, CH.sub.3, CF.sub.3, SCH.sub.3, NR.sup.16 R.sup.17 or NHCOR.sup.16,wherein R.sup.16 and R.sup.17 are the same or different and each is hydrogen or alkyl, alkenyl or alkynyl each of up to 6 C-atoms, aralkyl or cycloalkyl each of up to 10 C-atoms,or wherein R.sup.16 and R.sup.17 together form a saturated or unsaturated 3-7 membered heterocyclic ring;said compounds possess valuable psychotropic properties which make them useful for example as tranquilizers.

10. 发明授权

US07211680B2 Vitamin D derivatives with carbo-or heterocyclic substituents at C-25, a process for their production, intermediate products and their use for producing medicaments 失效
标题翻译： C-25具有碳或杂环取代基的维生素D衍生物，其生产方法，中间产物及其用于生产药物的用途
公开(公告)号：US07211680B2
公开(公告)日：2007-05-01
申请号：US10658326
申请日：2003-09-10
申请人： Andreas Steinmeyer , Gerald Kirsch , Guenter Neef , Katiea Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey , Marianne Fahnrich
发明人： Andreas Steinmeyer , Gerald Kirsch , Guenter Neef , Katiea Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey , Marianne Fahnrich
IPC分类号： C07C401/00 , A61K31/593
CPC分类号： C07D207/333 , C07C35/32 , C07C401/00 , C07D233/64 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/24 , C07D307/42 , C07D333/16
摘要： Compounds of Formula I, wherein Y1, Y2, R1–R6, Q and Z are as defined herein, are vitamin D derivatives. These compounds are useful for, e.g., the treatment hyperprolifierative diseases of the skin, tumor diseases and precancerous stages, auto-immune diseases, rejection reactions in the case of autologous, allogenic or xenogenic transplants, AIDS, atopic skin conditions, secondary hyperparathyroidism, renal osteodystrophia, senile and postmenopausal osteoporosis, diabetes mellitus type II, degenerative diseases of the peripheral and central nervous system, hypercalcemias, granulomatous diseases, paraneoplastic hypercalcemias, hypercalcemias in hyperparathyroidism, hirsutism, ateriosclerosis, and/or inflammatory diseases.
摘要翻译：其中Y 1，Y 2，R 1〜R 6，Q和Z的式I化合物是如本文所定义的是维生素D衍生物。这些化合物可用于例如治疗皮肤过度增压疾病，肿瘤疾病和癌前期，自身免疫疾病，自体，同种异体移植或异种移植中的排斥反应，艾滋病，特应性皮肤病，继发性甲状旁腺功能亢进，肾脏骨质疏松症，老年人和绝经后骨质疏松症，II型糖尿病，外周和中枢神经系统的退行性疾病，高钙血症，肉芽肿性疾病，副肿瘤性高钙血症，甲状旁腺功能亢进的高钙血症，多毛症，动脉硬化和/或炎症性疾病。

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