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101. 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。

102. 发明授权

US4159343A Prostane derivatives 失效
标题翻译：前列腺衍生物
公开(公告)号：US4159343A
公开(公告)日：1979-06-26
申请号：US883428
申请日：1978-03-03
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Eckehard Schillinger
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Olaf Loge , Eckehard Schillinger
IPC分类号： C07C405/00 , C07D309/12 , C07C69/34 , A61K31/225
CPC分类号： C07C405/0025 , C07C405/0016 , C07D309/12
摘要： Prostan-1-ol esters and intermediates for their preparation are described; the former compounds exhibit improved organ specificity and a longer duration of activity at lower dosages than the corresponding non-esterified prostaglandins and are useful, inter alia, in triggering abortion, inducing labor and regulating the menstrual cycle.
摘要翻译：描述了用于其制备的丙烷-1-醇酯和中间体; 前者的化合物表现出改善的器官特异性和较低的剂量比相应的未酯化的前列腺素更长的活性持续时间，并且尤其用于触发流产，诱导劳动和调节月经周期。

103. 发明授权

US4088775A 15-Ethylenedioxy-prostanoic acid derivatives and esters thereof and intermediates thereof 失效
标题翻译： 15-亚乙二氧基 - 前列腺酸衍生物及其酯及其中间体
公开(公告)号：US4088775A
公开(公告)日：1978-05-09
申请号：US595015
申请日：1975-07-11
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Walter Elger , Wolfgang Losert , Olaf Loge
IPC分类号： C07D407/04 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D317/00 , C07D317/30 , C07D317/46 , C07F9/535 , C07F9/655 , A61K31/335 , A61K31/36
CPC分类号： C07C405/00 , C07D317/30
摘要： Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl of 1-10 carbon atoms, aryl or --CH.sub.2 --U--V wherein U is a direct bond, carbonyl, or carbonyloxy and V is phenyl or substituted phenyl, e.g. substituted by at least one of phenyl, alkoxy of 1-2 carbon atoms or a halogen atom; one of R.sub.2 and R.sub.3 is hydroxy and the other is a hydrogen atom or R.sub.2 and R.sub.3 collectively are an oxygen atom; A is --CH.sub.2 --CH.sub.2 -- or trans--CH.dbd.CH; B is --CH.sub.2 --CH.sub.2 -- or cis--CH.dbd.CH; D and E collectively are a direct bond, or D is alkylene or 1-5 carbon atoms and E is an oxygen or sulfur atom; R.sub.4 is alkyl of 1-10 carbon atoms, alkyl of 1-5 carbon atoms substituted by unsubstituted or substituted aryl, unsubstituted or substituted aryl, or benzodioxol-2-yl-; X--Y is ##STR2## when one of R.sub.2 and R.sub.3 is a hydroxy group and the other is a hydrogen atom or X--Y is ##STR3## or --CH.dbd.CH-- when R.sub.2 and R.sub.3 collectively are an oxygen atom; and when R.sub.1 is a hydrogen atom, the physiologically acceptable salts thereof with bases, have an activity spectrum similar to but stronger and longer lasting activity than the corresponding natural prostaglandins.
摘要翻译：其中R1是氢原子，1-10个碳原子的烷基，芳基或-CH2-U-V，其中U是直接键，羰基或羰氧基，V是苯基或取代的苯基，例如，被苯基，1-2个碳原子的烷氧基或卤素原子中的至少一个取代; R2和R3之一是羟基，另一个是氢原子，R2和R3共同是氧原子; A是-CH 2 -CH 2 - 或反-CH = CH; B是-CH 2 -CH 2 - 或顺式-CH = CH; D和E共同是直接键合，或D是亚烷基或1-5个碳原子，E是氧或硫原子; R4是1-10个碳原子的烷基，1-5个碳原子的烷基被未取代或取代的芳基，未取代或取代的芳基或苯并间二氧杂环戊烯-2-基取代; 当R2和R3中的一个是氧原子时，当R 2和R 3中的一个是羟基，另一个是氢原子或X-Y是<或>时，X-Y是当R1是氢原子时，其与碱的生理上可接受的盐具有与相应的天然前列腺素相似但更强和更持久的活性的活性谱。

104. 发明授权

US08193252B1 Mesoprogestins (progesterone receptor modulators) for the treatment and prevention of benign hormone dependent gynecological disorders 有权
标题翻译：美孕激素（孕激素受体调节剂）用于治疗和预防良性激素依赖性妇科疾病
公开(公告)号：US08193252B1
公开(公告)日：2012-06-05
申请号：US10450029
申请日：2000-08-31
申请人： Kristof Chwalisz , Walter Elger , Gerd Shubert
发明人： Kristof Chwalisz , Walter Elger , Gerd Shubert
IPC分类号： A61K31/56
CPC分类号： A61K31/56 , Y10S514/843 , Y10S514/899
摘要： This present invention disclosed the use of mesoprogestins, a new class of progesterone receptor modulators (PRMs), for the treatment and prevention of benign hormone dependent gynecological disorders: a) for the treatment of gynecological disorder such as endometriosis, uterine fibroids, postoperative peritoneal adhesions, dysfunctional bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; b) for the prevention of gynecological disorders such as postoperative, peritoneal adhesions, dysfunctional uterine bleeding (metrorrhagia, menorrhagia) and dysmenorrhea; and c) a method of treatment and prevention of the above mentioned disorders in a female, preferably in a human female, in need of treatment or prevention of one or more of these disorders, with an effective amount of a mesoprogestin. Mesoprogestins are defined as compounds possessing both agonistic and antagonistic activities at the progesterone receptor (PR) in vivo. They stabilize the function of PR at an intermediate level of agonistic and antagonistic. Corresponding functional states cannot be achieved with progestins or antiprogestins. The daily dose of mesoprogestin is 0.5 to 100 mg, preferably 5.0 to 50 mg and most preferably 10 to 25 mg. J867, J912, J956 and J1042 are the mesoprogestins preferred according to the invention.
摘要翻译：本发明公开了用于治疗和预防良性激素依赖性妇科疾病的新型孕激素受体调节剂（PRM）的使用：a）用于治疗妇科疾病如子宫内膜异位症，子宫肌瘤，术后腹膜粘连功能障碍性出血（metrorrhagia，月经过多）和痛经; b）用于预防妇科疾病如术后，腹膜粘连，功能障碍性子宫出血（metrorrhagia，月经过多）和痛经; 和c）有效量的中孕酮治疗和预防女性，优选在人类女性中需要治疗或预防这些疾病中的一种或多种的上述病症的方法。中孕烯孕素被定义为在体内孕酮受体（PR）具有激动作用和拮抗活性的化合物。他们将PR的功能稳定在激进和对抗的中间水平。孕激素或抗孕激素不能达到相应的功能状态。中孕酮的日剂量为0.5〜100mg，优选为5.0〜50mg，最优选为10〜25mg。 J867，J912，J956和J1042是根据本发明优选的中孕妇。

105. 发明授权

US07550451B2 Progesterone receptor modulators with increased antigonadotropic activity for female birth control and hormone replacement therapy 有权
标题翻译：孕激素受体调节剂具有增加的女性避孕和激素替代疗法的抗增生性活性
公开(公告)号：US07550451B2
公开(公告)日：2009-06-23
申请号：US10631967
申请日：2003-08-01
申请人： Alexander Hillisch , Walter Elger , Gerd Schubert , Birgitt Schneider , Gudrun Reddersen
发明人： Alexander Hillisch , Walter Elger , Gerd Schubert , Birgitt Schneider , Gudrun Reddersen
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J41/0083 , A61K31/565 , A61K31/566 , A61K45/06 , C07J1/00 , Y10S514/814 , A61K2300/00
摘要： The invention relates to new compounds of general formula I, their production and pharmaceutical preparations that contain these compounds. The compounds according to the invention are preferably used for female birth control and for HRT.
摘要翻译：本发明涉及通式Ⅰ的新化合物，它们的生产和含有这些化合物的药物制剂。根据本发明的化合物优选用于女性避孕和HRT。

106. 发明授权

US07507725B2 Compounds with sulphonamide group and pharmaceutical compositions containing these compounds 失效
标题翻译：具有磺酰胺基团的化合物和含有这些化合物的药物组合物
公开(公告)号：US07507725B2
公开(公告)日：2009-03-24
申请号：US10296973
申请日：2001-05-08
申请人： Walter Elger , Alexander Hillisch , Annemarie Hedden , Sigfrid Schwarz , Klaus Schollkopf
发明人： Walter Elger , Alexander Hillisch , Annemarie Hedden , Sigfrid Schwarz , Klaus Schollkopf
IPC分类号： A61K31/56
CPC分类号： C07J41/0044 , C07J41/0038 , C07J41/005
摘要： The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The uptake of these compounds by and/or the binding thereof to the erythrocytes is made possible by a group of formula —SO2NR1R2, wherein R1 and R2, independently of each other, mean a hydrogen atom, an acyl group, an alkyl group, a cycloalkyl group, an aryl group, a cyano group or a hydroxy group. The inventive prodrugs enable active agents such as endogenic substances, natural substances and synthetic substances with therapeutically useful properties which have a high “first path” effect, to be administered orally effectively or significantly improve the oral activity thereof.
摘要翻译：本发明涉及作为前药和/或支持物的化合物，使活性剂能够被红细胞和/或活性剂吸收以结合红细胞。这些化合物通过和/或其与红细胞的结合的吸收通过式-SO 2 NR 1 R 2的基团可以实现，其中R 1和R 2彼此独立地表示氢原子，酰基，烷基，环烷基，芳基，氰基或羟基。本发明的前药使得具有高“第一途径”效果的具有治疗有用性质的内源性物质，天然物质和合成物质等活性剂能够有效口服或显着改善其口服活性。

107. 发明申请

US20080306164A1 NEW 2-SUBSTITUTED D-HOMO-ESTRA-1,3,5(10)-TRIENES AS INHIBITORS OF 17BETA-HYDROXY STEROID DEHYDROGENASE TYPE 1 失效
标题翻译：新的2-取代的D-HOMO-ESTRA-1,3,5（10） - 作为17BA-羟基甾体脱氢酶1型的抑制剂
公开(公告)号：US20080306164A1
公开(公告)日：2008-12-11
申请号：US12192446
申请日：2008-08-15
申请人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
发明人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
IPC分类号： C07J63/00 , A61K31/122
CPC分类号： C07J63/00
摘要： The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17β-hydroxy steroid dehydro-genase type 1.
摘要翻译：本发明涉及通式I的新的2-取代的D-异 - 雌-1,3,5（10） - 三烯，其中R 2表示C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基或卤素原子，R 13表示氢原子或甲基，R 17表示氢原子或氟原子，以及它们的药学上可接受的盐，它们的制备和用途，作为预防和治疗雌激素依赖性疾病的药物，其可受抑制17β-羟基类固醇脱氢基因型1型。

108. 发明授权

US07435757B2 2-substituted D-homo-estra-1,3,5(10)-trienes as inhibitors of 17β-hydroxy steroid dehydrogenase type 1 失效
标题翻译： 2-取代的D-均一雌-1,3,5（10）三烯作为17β-羟基类固醇脱氢酶1型的抑制剂
公开(公告)号：US07435757B2
公开(公告)日：2008-10-14
申请号：US11171476
申请日：2005-07-01
申请人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
发明人： Alexander Hillisch , Olaf Peters , Christian Gege , Wilko Regenhardt , Gabriele Moeller , Dominga Deluca , Jerzy Adamski , Walter Elger , Birgitt Schneider
IPC分类号： A61K31/12 , A61K31/56 , C07J1/00 , C07C49/00
CPC分类号： C07J63/00
摘要： The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I in which R2 means a C1-C8-alkyl group, a C1-C8-alkyloxy group or a halogen atom, R13 means a hydrogen atom or a methyl group, R17 means a hydrogen atom or a fluorine atom, as well as their pharmaceutically acceptable salts, their manufacture and use as medicaments for prophylaxis and therapy of estrogen-dependent diseases that can be influenced by inhibition of 17β-hydroxy steroid dehydro-genase type 1.
摘要翻译：本发明涉及通式I的新的2-取代的D-异 - 雌-1,3,5（10） - 三烯，其中R 2是指C 1〜 -C 8 - 烷基，C 1 -C 8 - 烷氧基或卤素原子，R 13 >表示氢原子或甲基，R 17表示氢原子或氟原子，以及它们的药学上可接受的盐，它们作为用于预防和治疗雌激素依赖性药物的制备和用途可能受到抑制17β-羟基类固醇脱氢基因型1的影响的疾病。

109. 发明授权

US07388003B2 Δ15-D-Homosteroids with androgenic action 失效
标题翻译：具有雄激素作用的Delta15-D-类固醇激素
公开(公告)号：US07388003B2
公开(公告)日：2008-06-17
申请号：US10923080
申请日：2004-08-23
申请人： Ralf Wyrwa , Sven Ring , Guenter Kaufmann , Walter Elger , Birgitt Schneider
发明人： Ralf Wyrwa , Sven Ring , Guenter Kaufmann , Walter Elger , Birgitt Schneider
IPC分类号： A61K31/56 , C07J1/00
CPC分类号： C07J63/00 , Y10S514/841
摘要： The invention relates to Δ15-D-homosteroids of general formula (I) process for their production and pharmaceutical compositions that contain these compounds. The compounds of general formula I according to the invention have androgenic activity.
摘要翻译：本发明涉及其制备的通式（I）的三羟甲基-D-类固醇激素和含有这些化合物的药物组合物。根据本发明的通式I的化合物具有雄激素活性。

110. 发明授权

US07335650B2 Composition 失效
标题翻译：组成
公开(公告)号：US07335650B2
公开(公告)日：2008-02-26
申请号：US10120275
申请日：2002-04-10
申请人： Barry Victor Lloyd Potter , Michael John Reed , Walter Elger , Gudrun Roddersen , Heinrich-Thomas Proske
发明人： Barry Victor Lloyd Potter , Michael John Reed , Walter Elger , Gudrun Roddersen , Heinrich-Thomas Proske
IPC分类号： A61K31/56
CPC分类号： A61K31/566 , A61K31/565 , A61K31/567
摘要： There is provided a pharmaceutical composition comprising (i) a compound of the formula wherein: X is a hydrocarbyl ring having at least 4 atoms in the ring; K is a hydrocarbyl group; Rs is a sulphamate group; (ii) optionally admixed with a pharmaceutically acceptable carrier, diluent, excipient or adjuvant, wherein the compound is present in an amount to provide a dosage of no greater than 200 μg/day.
摘要翻译：提供了一种药物组合物，其包含（i）下式的化合物其中：X是在环中具有至少4个原子的烃基环; K是烃基; Rs是氨基磺酸盐基团; （ii）任选地与药学上可接受的载体，稀释剂，赋形剂或佐剂混合，其中所述化合物以提供不大于200杯/天的剂量的量存在。

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