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1. 发明申请

WO2015057894A1 METHODS FOR TREATING POLYCYSTIC KIDNEY DISEASE AND POLYCYSTIC LIVER DISEASE 审中-公开
标题翻译：治疗多囊性疾病和多发性肝病的方法
公开(公告)号：WO2015057894A1
公开(公告)日：2015-04-23
申请号：PCT/US2014/060774
申请日：2014-10-15
申请人： MASSACHUSETTS INSTITUTE OF TECHNOLOGY , YALE UNIVERSITY
发明人： FEDELES, Bogdan, I. , FEDELES, Sorin, V. , CROY, Robert, G. , SOMLO, Stefan , ESSIGMANN, John, M.
IPC分类号： A61K31/122 , A61K31/567 , A61P1/16 , A61P13/12
CPC分类号： C07J41/0077 , A61K31/122 , A61K31/567
摘要： The present invention provides compounds of Formula (I) or (II), which are thought to be able to inhibit mTOR (mammalian target of rapamycin) signaling pathway, induce UPR (unfolded protein response), and/or perturb mitochondrial function of a cyst cell (e.g., a cyst cell causing polycystic kidney disease (PKD, e.g., autosomal dominant PKD (ADPKD) or autosomal recessive PKD (ARPKD)) or polycystic liver disease (PLD, e.g., autosomal dominant PLD (ADPLD) or autosomal recessive PLD (ARPLD)). The invention also provides pharmaceutical compositions, kits, and methods involving the compounds described herein for use in treating PKD or PLD, inhibiting the growth of a cyst cell, and/or killing a cyst cell.
摘要翻译：本发明提供式（I）或（II）的化合物，其被认为能够抑制mTOR（雷帕霉素的哺乳动物靶标）信号通路，诱导UPR（展开的蛋白质应答）和/或扰乱囊肿的线粒体功能细胞（例如，引起多囊肾病（PKD，例如常染色体显性PKD（ADPKD）或常染色体隐性PKD（ARPKD））或多囊肝病（PLD，例如常染色体显性PLD（ADPLD）或常染色体隐性遗传性PLD 本发明还提供涉及本文所述化合物用于治疗PKD或PLD，抑制囊肿细胞生长和/或杀死囊肿细胞的药物组合物，试剂盒和方法。

2. 发明申请

WO9933859A2 NOVEL ANTI-ESTROGENIC STEROIDS, AND ASSOCIATED PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：新颖的抗雌激素类固醇，以及相关的药物组合物和使用方法
公开(公告)号：WO9933859A2
公开(公告)日：1999-07-08
申请号：PCT/US9827406
申请日：1998-12-23
申请人： STANFORD RES INST INT
发明人： TANABE MASATO , PETERS RICHARD H , CHAO WAN-RU , JONG LING
IPC分类号： A61K31/57 , A61K9/02 , A61K31/56 , A61K31/575 , A61K31/58 , A61P3/06 , A61P5/32 , A61P11/00 , A61P19/10 , A61P35/00 , A61P43/00 , C07J13/00 , C07J41/00 , C07J43/00
CPC分类号： C07J41/00 , A61K9/02 , C07J41/0072 , C07J41/0077 , C07J43/003
摘要： Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependant disorders. Preferred compounds have 1,3,5-estratiene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratienes. Therapeutic methods and pharmaceutical compositions are provided as well.
摘要翻译：提供了新的抗雌激素化合物，其可用于治疗多种疾病，特别是雌激素依赖性疾病。优选的化合物具有1,3,5-雌二醇核，并且在C-17或C-11位置被分子部分取代，这使得化合物有效竞争性地阻断雌激素与其受体的结合。特别优选的化合物是17-脱氧-1,3,5-雌甾烯。还提供了治疗方法和药物组合物。

3. 发明申请

WO99033859A3 NOVEL ANTI-ESTROGENIC STEROIDS, AND ASSOCIATED PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：新型抗雌激素类固醇和相关药物组合物及其使用方法
公开(公告)号：WO99033859A3
公开(公告)日：1999-12-23
申请号：PCT/US1998/027406
申请日：1998-12-23
IPC分类号： A61K31/57 , A61K9/02 , A61K31/56 , A61K31/575 , A61K31/58 , A61P3/06 , A61P5/32 , A61P11/00 , A61P19/10 , A61P35/00 , A61P43/00 , C07J13/00 , C07J41/00 , C07J43/00
CPC分类号： C07J41/00 , A61K9/02 , C07J41/0072 , C07J41/0077 , C07J43/003
摘要： Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependant disorders. Preferred compounds have 1,3,5-estratiene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratienes. Therapeutic methods and pharmaceutical compositions are provided as well.
摘要翻译：提供了新的抗雌激素化合物，其可用于治疗多种疾病，特别是雌激素依赖性疾病。优选的化合物具有1,3,5-雌酮核，并且在C-17或C-11位置被分子部分取代，这使得化合物有效地竞争性阻断雌激素与其受体的结合。特别优选的化合物是17-脱氧-1,3,5-雌酮。也提供治疗方法和药物组合物。

4. 发明申请

WO9933859A9 NOVEL ANTI-ESTROGENIC STEROIDS, AND ASSOCIATED PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE 审中-公开
公开(公告)号：WO9933859A9
公开(公告)日：1999-09-23
申请号：PCT/US9827406
申请日：1998-12-23
申请人： STANFORD RES INST INT
发明人： TANABE MASATO , PETERS RICHARD H , CHAO WAN-RU , JONG LING
IPC分类号： A61K31/57 , A61K9/02 , A61K31/56 , A61K31/575 , A61K31/58 , A61P3/06 , A61P5/32 , A61P11/00 , A61P19/10 , A61P35/00 , A61P43/00 , C07J13/00 , C07J41/00 , C07J43/00
CPC分类号： C07J41/00 , A61K9/02 , C07J41/0072 , C07J41/0077 , C07J43/003
摘要： Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependant disorders. Preferred compounds have 1,3,5-estratiene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratienes. Therapeutic methods and pharmaceutical compositions are provided as well.

5. 发明申请

WO1988001868A1 17'alpha'-(SUBSTITUTED-METHYL)-17'beta'-HYDROXY/ESTERIFIED HYDROXY STEROIDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： 17α-（取代甲基）-17β-羟基/纯化的羟基甾族化合物和含有它们的药物组合物
公开(公告)号：WO1988001868A1
公开(公告)日：1988-03-24
申请号：PCT/US1987002303
申请日：1987-09-15
申请人： RESEARCH TRIANGLE INSTITUTE
发明人： RESEARCH TRIANGLE INSTITUTE , COOK, C., Edgar , TALLENT, C., Ray , REEL, Jerry, R. , WANI, Mansukh, C.
IPC分类号： A61K31/58
CPC分类号： C07J41/0016 , C07J41/0077 , C07J41/0083 , C07J51/00
摘要： Steroids of formula (I) which are characterized by a 17alpha-cyanomethyl, azidomethyl, methoxymethyl, phenylmethyl, or ethynylmethyl substituent and a 17beta-hydroxy/esterified hydroxy substituent. The steroids of this invention have glucocorticoid, anti-glucocorticoid, progestational, or anti-progestational activity, depending on the particular structure.

6. 发明申请

WO1987005908A1 STEROIDS COMPRISING A SPIRANIC CYCLE IN POSITION 17, PREPARATION PROCESS AND UTILIZATION THEREOF 审中-公开
标题翻译：包含位置17中的SPIRANIC循环的STEROIDS，其制备过程及其利用
公开(公告)号：WO1987005908A1
公开(公告)日：1987-10-08
申请号：PCT/FR1987000096
申请日：1987-03-26
申请人： ROUSSEL-UCLAF , NIQUE, François , NEDELEC, Lucien , PHILIBERT, Daniel , MOGUILEWSKY, Martine
发明人： ROUSSEL-UCLAF
IPC分类号： C07J21/00
CPC分类号： C07J43/003 , C07J31/006 , C07J33/002 , C07J41/0077 , C07J41/0083 , Y10S514/843
摘要： Products having the formula (I) wherein R1 is an aryl or aralkyl, R2 is a hydrocarbonated radical (1-18 carbon atoms), the dotted lines indicate an optional bond, the cycles A, B and C represent (II), (III), (IV), (V), (VI); R' and R'' are H, alkyl (1-4 carbon atoms), Re is H, alkyl (1-6 carbon atoms), acyl, and their salts, their preparation, their application as medicaments, the pharmaceutical compositions containing them and intermediaries.
摘要翻译：具有式（I）的产物，其中R 1是芳基或芳烷基，R 2是烃基（1-18个碳原子），虚线表示任选的键，循环A，B和C表示（II），（III ），（IV），（V），（VI） R'和R“是H，烷基（1-4个碳原子），Re是H，烷基（1-6个碳原子），酰基及其盐，它们的制备，它们作为药物的应用，含有它们的药物组合物和中介。

7. 发明申请

WO2010003391A2 ANIONIC PREGNANE COMPOUNDS, METHOD FOR THEIR PRODUCING AND USE OF THEM 审中-公开
标题翻译： ANIONIC PREGNANE化合物，其生产和使用方法
公开(公告)号：WO2010003391A2
公开(公告)日：2010-01-14
申请号：PCT/CZ2009000091
申请日：2009-07-09
申请人： USTAV ORSANICKE CHEMIE A BIOCH , FYZIOLQGICKY USTAV , STASTNA EVA , CHODOUNSKA HANA , POUZAR VLADIMIR , KAPRAS VOJTECH , CAIS ONDREJ , VYKLICKY LADISLAV , KOHOUT LADISLAV
发明人： STASTNA EVA , CHODOUNSKA HANA , POUZAR VLADIMIR , KAPRAS VOJTECH , CAIS ONDREJ , VYKLICKY LADISLAV , KOHOUT LADISLAV
CPC分类号： C07J41/0077 , C07J7/002 , C07J31/006
摘要： This invention relates to pregnane anionic compounds of general formula I in which R1 is ester group, which is able to form ion such as sulfate, pyridinium sulfate, hemisuccinate etc., R2 is hydrogen atom in alpha or beta configuration, and R3 is ester group, as is acetoxy group, nicotinoyloxy group etc., and their pharmaceutically acceptable salts. Compounds of general formula I are preferably produced from the diol of formula II or diol of formula VIII, which are converted according to described sequence of reactions, to compounds of general formula I, in which R1 is ester group, which is able to form ion such as sulfate, pyridinium sulfate, hemisuccinate etc., R2 is hydrogen atom in alpha or beta configuration, and R3 is ester group. The compounds of general formula I are useful as active ingredients for production of pharmaceuticals for the treatment of neurological and psychiatric diseases and conditions associated with excessive activation of NMDA receptors such as neuroprotective agents against excitotoxic damage of the central nervous system (CNS), conditions associated with excessive activation of NMDA-subtype glutamate receptors or, where this type of receptor is involved in the creation or during the certain mental and neurological diseases, in particular concerning the traumatic and hypoxic damage Io nervous tissue in the central nervous system diseases, such as Alzheimer's, Huntington's and Parkinson's disease, also in cognitive disorders in aging; the other indications could be tardive dyskinesia, amyotrophic lateral sclerosis, olivopontocerebellar degeneration, neurological problems1 associated with AIDS infection, allergic encephalomyelitis, and for medication of epilepsy, anxiety, depression, schizophrenia, chronic pain and drug addiction.
摘要翻译：本发明涉及通式Ⅰ的孕烷阴离子化合物，其中R1为酯基，能够形成硫酸根离子，硫酸吡啶硫酸盐，半琥珀酸盐等，R2为α或β构型的氢原子，R3为酯基，如乙酰氧基，烟酰氧基等，及其药学上可接受的盐。通式I的化合物优选由式II的二醇或根据所述反应顺序转化的式VIII的二醇制备成通式I的化合物，其中R1是酯基，其能够形成离子如硫酸盐，硫酸吡啶鎓，半琥珀酸盐等，R2是α或β构型的氢原子，R3是酯基。通式I的化合物可用作生产用于治疗神经和精神疾病的药物的活性成分，以及与NMDA受体过度激活相关的病症，例如针对中枢神经系统（CNS）的兴奋性毒性损伤的神经保护剂，与之相关的病症 NMDA亚型谷氨酸受体过度激活，或者这种类型的受体涉及创造或某些精神和神经疾病时，特别是关于中枢神经系统疾病中的神经组织的创伤性和缺氧性损伤，例如老年痴呆症，亨廷顿病和帕金森病，也在老龄化认知障碍中; 其他适应症可能是迟发性运动障碍，肌萎缩性侧索硬化，橄榄体小脑变性，与艾滋病感染相关的神经问题1，过敏性脑脊髓炎，以及用于癫痫，焦虑，抑郁，精神分裂症，慢性疼痛和药物成瘾的药物。

8. 发明申请

WO2003080642A1 11BETA-SUBSTITUIERTE 19-NOR-17ALPHA-PREGNA-1,3,5(10)-TRIEN-17BETA-OLE MIT EINEM 21,16ALPHA-LAKTONRING 审中-公开
标题翻译： 11β-取代19-NOR-17α-乙烯 - 孕-1,3,5（10）WITH A 21,16ALPHA内酯 - 三烯17β-OLE
公开(公告)号：WO2003080642A1
公开(公告)日：2003-10-02
申请号：PCT/EP2003/003221
申请日：2003-03-27
申请人： SCHERING AG
发明人： HILLISCH, Alexander , MÜLLER, Gerd , BOHLMANN, Rolf , HOFFMANN, Jens , FRITZEMEIER, Karl-Heinrich
IPC分类号： C07J41/00
CPC分类号： C07J41/0077 , C07J1/0003
摘要： Die vorliegende Erfindung betrifft neue 19-Nor-17a-pregna-1,3,5(10)-trien-17b-ole mit einem 21,16a-Laktonring mit einem langkettigen Substituenten in 11b-Stellung der allgemeinen Formel (II) worin R11 ein langkettiger, ein Stickstoffatom aufweisender Alkylrest ist, der endständig mit einer Perfluoralkylgruppe substituiert sein kann. Die Verbindungen wirken gewebeselektiv als reine Antiestrogene und sind aufgrund dieser Eigenschaften zur Herstellung von Arzneimitteln geeignet.
摘要翻译：本发明涉及新颖的19-去 - 17A - 孕-1,3,5（10） - 三烯17B醇类与21,16a内酯环与通式（II），其中R 11的11B-位置的长链取代基是长链烷基具有氮原子，其可以与全氟烷基末端取代。的化合物作为组织选择性抗雌激素纯和适合于生产，因为这些性质的药物。

9. 发明申请

WO1994024146A1 NOVEL ANDROGENS AND ANABOLIC AGENTS 审中-公开
标题翻译：新型蛋白同化雄性激素
公开(公告)号：WO1994024146A1
公开(公告)日：1994-10-27
申请号：PCT/DE1994000316
申请日：1994-03-18
申请人： HESCH, Rolf-Dieter
IPC分类号： C07J31/00
CPC分类号： C07J41/0077 , C07J1/0025 , C07J31/006 , C07J41/0038 , C07J41/0088 , C07J43/003
摘要： Androgens and their derivates and analogs, such as anabolic agents, are characterized by at least one substituent or substituent grouping with radical trapping properties. These compounds are used as androgen or anabolic agent substitutes or therapeutical agents for treating androgen defficiency; for treating benign prostate hypertrophy and prostate carcinome, in particular with a testosterone-based compound; for treating osteoporosis, in particular post-menopausal osteoporosis in women, preferably associated with estrogen and/or gestagens; for treating brain oedema induced by vasculary or ischemic troubles, subarachnoidal bleeding, ischemic shock and cerebral insult; for treating asthma in its various forms, for treating Alzheimer's disease, Parkinson's disease; for organ transplants; and for treating androgen-dependent and non androgen-dependent malign neoplasia.

10. 发明申请

WO1983003099A1 3-KETO-DELTA 4,9-19-NORSTEROIDS 审中-公开
公开(公告)号：WO1983003099A1
公开(公告)日：1983-09-15
申请号：PCT/FR1983000034
申请日：1983-02-25
申请人： ROUSSEL-UCLAF
发明人： ROUSSEL-UCLAF , PHILIBERT, Daniel , TEUTSCH, Jean, Georges , COSTEROUSSE, Germain , DERAEDT, Roger
IPC分类号： C07J01/00
CPC分类号： C07J1/0096 , C07J7/003 , C07J7/0045 , C07J7/0075 , C07J17/00 , C07J21/006 , C07J31/006 , C07J33/002 , C07J41/0016 , C07J41/0077 , C07J41/0083 , C07J41/0094 , C07J51/00 , C07J71/001
摘要： The invention relates to products having the general formula I, wherein R1 is thienyl or phenyl optionally substituted, furyl, cycloalkyl, naphtyl, phenyl-phenyl, alkyl or alkenyl; R2 is methyl or ethyl; R3 is H, OH, alkyl, alkenyl, optionally substituted alkynyl, acetyl, hydroxy acetyl, optionally esterified or salified carboxy alkoxy, optionally esterified hydroxy alkyl; R4 is H, OH, alkyl, alkenyl, alkynyl optionally substituted by amino, alkyl or dialkyl amino, halogen, thioalkyl, alkoxy, trialkylsylyl or cyano; R5 is H or methyl; X is O, hydroxyimino or alkoxyimino; A and B are alpha -epoxy or a second bond; preparation method thereof, application thereof as drugs, compositions containing them and new intermediaries obtained.
摘要翻译：本发明涉及具有通式I的产物，其中R 1是噻吩基或任选取代的苯基，呋喃基，环烷基，萘基，苯基 - 苯基，烷基或链烯基; R2是甲基或乙基; R 3是H，OH，烷基，烯基，任选取代的炔基，乙酰基，羟基乙酰基，任选酯化或盐化的羧基烷氧基，任选酯化的羟基烷基; R4是H，OH，烷基，烯基，任选被氨基，烷基或二烷基氨基，卤素，硫代烷基，烷氧基，三烷基亚基或氰基取代的炔基; R5是H或甲基; X是O，羟基亚氨基或烷氧基亚氨基; A和B是α-环氧基或第二键; 其制备方法，作为药物的应用，含有它们的组合物和获得的新中间体。

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