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1. 发明申请

WO2014115167A3 NOVEL COMPOUNDS OF 11BETA-HYDROXY-STEROIDS FOR USE IN MITOCHONDRIA BIOGENESIS AND DISEASES ASSOCIATED WITH MITOCHONDRIAL DYSFUNCTION OR DEPLETION 审中-公开
标题翻译：用于麻醉生物制剂和与麻醉药物功能丧失相关的疾病的11BETA-羟基甾体化合物的新化合物
公开(公告)号：WO2014115167A3
公开(公告)日：2014-12-04
申请号：PCT/IN2014000048
申请日：2014-01-23
申请人： SPHAERA PHARMA PVT LTD
发明人： DUGAR SUNDEEP , SCHREINER FREDERIC GEORGE , MAHAJAN DINESH , SHARMA AMIT , PATIL ISHWAR RAKESH , KUILA BILASH
IPC分类号： A61K31/56 , C07J5/00 , C07J71/00
CPC分类号： C07J17/00 , C07J1/0011 , C07J1/0022 , C07J3/005 , C07J5/0015 , C07J5/0053 , C07J7/0005 , C07J7/002 , C07J7/007 , C07J9/00 , C07J11/00 , C07J21/00 , C07J21/006 , C07J31/006 , C07J41/0011 , C07J41/0016 , C07J41/0038 , C07J41/005 , C07J43/003
摘要： The present invention provides novel compounds of 11&bgr;-hydroxy steroids and compositions and their application as pharmaceuticals for preventing or reversing injury to mitochondria, for treating or preventing diseases relating to mitochondrial dysfunction or depletion, and for inducing regeneration or restructuring of mitochondria as a means of treating diseases relating to abnormalities in mitochondrial structure and function in a human or animal subject. Also disclosed herein are methods for diagnosing injury to mitochondria and for diagnosing the success or failure of therapeutics designed to treat, prevent, or reverse injury to or depletion of mitochondria.
摘要翻译：本发明提供11β-羟基类固醇及其组合物的新化合物及其作为用于预防或逆转线粒体损伤的药物的用途，用于治疗或预防与线粒体功能障碍或消耗相关的疾病，以及诱导线粒体再生或重组作为手段治疗与人或动物受试者的线粒体结构和功能异常有关的疾病。本文还公开了用于诊断线粒体损伤和诊断设计用于治疗，预防或逆转线粒体损伤或消耗的治疗剂的成功或失败的方法。

2. 发明申请

WO2013135744A1 COMBINED SYNTHESIS ROUTE FOR ETONOGESTREL AND DESOGESTREL 审中-公开
标题翻译：组合合成路线和灭菌系统
公开(公告)号：WO2013135744A1
公开(公告)日：2013-09-19
申请号：PCT/EP2013/055084
申请日：2013-03-13
申请人： MSD OSS B.V. , OSTENDORF, Martin
发明人： OSTENDORF, Martin
IPC分类号： C07J5/00 , C07J33/00
CPC分类号： C07J33/007 , C07J1/0059 , C07J1/0096 , C07J11/00 , C07J21/008
摘要： The present invention relates to a synthesis route and to steroid derivatives of general formula VI and VII useful in the synthesis of desogestrel and etonogestrel.
摘要翻译：本发明涉及用于合成去氧孕烯和依托孕烯的通式VI和VII的类固醇衍生物的合成途径。

3. 发明申请

WO2012083090A3 METHODS AND COMPOUNDS FOR PREPARING 3ALPHA-OXYGEN SUBSTITUTED STEROIDS 审中-公开
标题翻译：制备3α-氧取代的甾体类化合物的方法和化合物
公开(公告)号：WO2012083090A3
公开(公告)日：2012-12-06
申请号：PCT/US2011065298
申请日：2011-12-15
申请人： HARBOR BIOSCIENCES INC , GE YU , WHITE STEVEN K , HUANG YUJIN
发明人： GE YU , WHITE STEVEN K , HUANG YUJIN
IPC分类号： A61K31/56
CPC分类号： C07J11/00 , C07J1/0011 , C07J1/0022 , C07J1/0025 , C07J1/0048 , C07J21/003 , C07J41/0038 , C07J51/00 , C07J71/001
摘要： The invention relates to processes for preparing 3a-O-linked steroids including 3a-O-linked-androst-5-ene steroids and 3a-O-linked-5a-androstane steroids. In one process a 3a,4a-epoxy androst-5-en-17-one is predominately reduced at the epoxy moiety wherein reduction of the 3a,4a epoxy functional group occurs preferentially at position C4 with retention of configuration at position C3 to provide a 3a-O-linked-androst-5-ene steroid. In another process, conditions are provided for inversion of configuration of a 3ß-hydroxy-androst-5-ene steroid by the Mitsunobu reaction to provide a 3a-O-linked-androst-5-ene steroid with reduced amounts of 3a,5a-cycloandrostane side-product impurities.
摘要翻译：本发明涉及制备3α-O-连接类固醇的方法，所述类固醇包括3α-O-连接的雄甾-5-烯类固醇和3α-O-连接的5α-雄甾烷类固醇。在一个方法中，3a，4a-环氧雄甾-5-烯-17-酮在环氧部分处主要被还原，其中3a，4a环氧官能团的还原优先在位置C4处发生，在位置C3处保留构型以提供 3α-O-连 - 雄甾-5-烯甾族化合物。在另一种方法中，通过Mitsunobu反应提供了用于3β-羟基 - 雄甾-5-烯类固醇构型转化的条件，以提供3a-O-连接的雄甾-5-烯类固醇，其中3a，5a- 环雄甾烷副产物杂质。

4. 发明申请

WO0226759A3 17 alpha FLUOROALKYL STEROIDS, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS 审中-公开
标题翻译： 17α-氟烷基stareroids，它们的制备方法和含有这些化合物的药物组合物
公开(公告)号：WO0226759A3
公开(公告)日：2002-06-20
申请号：PCT/DE0103732
申请日：2001-09-28
申请人： JENAPHARM GMBH , RING SVEN , KAUFMANN GUENTER , WYRWA RALF , ELGER WALTER
发明人： RING SVEN , KAUFMANN GUENTER , WYRWA RALF , ELGER WALTER
IPC分类号： A61K31/569 , A61K31/58 , A61P5/26 , A61P15/00 , A61P15/10 , A61P15/16 , A61P35/00 , C07J1/00 , C07J11/00 , C07J43/00 , C07J71/00 , A61K31/565
CPC分类号： C07J71/0047 , C07J1/0037 , C07J1/0085 , C07J11/00 , C07J71/0063 , C07J71/0084
摘要： The invention relates to 17 alpha fluoroalkyl steroids of the general formula (I), STEROID (I), wherein R3 represents a group of the formula CnFmHo, wherein n = 1, 2, 3, 4, 5 or 6, m > 1 and m+o = 2n+1. The invention further relates to methods for producing the same and to compositions that contain said compounds. The inventive composition of the general formula (I) possess androgenic activity.
摘要翻译：本发明涉及17阿尔法-Fluoraklylsteroide通式（I）其中R 3是下式基团的CnFmHo，其中n = 1，2，3，4，5或6，M> 1，且m + O = 2N + 1 其制备方法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。

5. 发明申请

WO1993025569A1 OESTRADIOL PRODRUGS 审中-公开
标题翻译：雌二醇前体药物
公开(公告)号：WO1993025569A1
公开(公告)日：1993-12-23
申请号：PCT/EP1993001543
申请日：1993-06-15
申请人： SCHERING AKTIENGESELLSCHAFT , MUHN-SEIPOLDY, Hans-Peter , CLEVE, Arwed , PETZOLDT, Karl , NEEF, Günter , KRATTENMACHER, Rolf , STÖCKEMANN, Klaus , GOTTWALD, Matthias
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J41/00
CPC分类号： C07J41/0016 , C07J1/007 , C07J1/0074 , C07J11/00 , C07J21/006
摘要： The invention concerns compounds of general formula (I), in which either X is a hydroxyimino group (= N SIMILAR OH), a hydroxy group and a hydrogen atom, a C1-C20 alkanoyloxy group and a hydrogen atom or two hydrogens atoms and A----B is a C-C double bond and B----C is a C-C single bond or X is a keto group protected in the form of a cyclic ketal and A----B is a C-C single bond and B----C is a C-C double bond and in both cases Z is an oxygen atom or an OR group and a hydrogen atom, and R and R , independently of each other, are each a hydrogen atom or a C1-C20 alkanoyl group. The compounds of formula (I) have oestrogenic properties.

6. 发明申请

WO1990011290A1 METHOD FOR THE PREPARATION OF 3-DESOXY-4-ENE STEROIDS 审中-公开
标题翻译：制备3-脱氧-4-烯酮甾体的方法
公开(公告)号：WO1990011290A1
公开(公告)日：1990-10-04
申请号：PCT/DE1990000183
申请日：1990-03-08
申请人： SCHERING AKTIENGESELLSCHAFT , WINTERFELDT, Ekkehard , TILSTAMM, Ulf , HOFMEISTER, Helmut , LAURENT, Henry
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J11/00
CPC分类号： C07J11/00
摘要： The invention concerns a method for the preparation of 3-desoxy-4-ene steroids of the general formula I in which R1, R2 and R3 are a hydrogen atom or a methyl group, R4 is a lower alkyl group, a phenyl group or a free, esterified or etherified hydroxyl group, R5 is a hydrogen atom, a vinyl group or the -C=CR6 grouping, R6 being a hydrogen atom, an alkyl group with at the most 4 carbon atoms or a halogen atom, X is a methylene group, a fluoromethylene group, an ethylidene group or a vinylidene group, Y and U are a methylene group or an ethylidene group, and Z is a methylene group, an ethylidene group, a vinylidene group, a chloromethylene group or a hydroxymethylene group, and in which the bonds are three single bonds, or a double bond and two single bonds, or a conjugated double bond. The 3-oxo-4-ene steroid is reduced using a reaction mixture comprising trifluoroacetic or trichloroacetic acid, optionally additional carboxylic acid, and sodium borohydride.
摘要翻译：本发明涉及制备通式Ⅰ的3-脱氧-4-烯类固醇的方法，其中R1，R2和R3为氢原子或甲基，R4为低级烷基，苯基或游离的，酯化的或醚化的羟基，R5是氢原子，乙烯基或-C = CR6基，R6是氢原子，具有最多4个碳原子的烷基或卤素原子，X是亚甲基亚乙基，亚乙烯基，Y和U是亚甲基或亚乙基，Z是亚甲基，亚乙基，亚乙烯基，氯亚甲基或羟基亚甲基，和其中键是三个单键，或双键和两个单键，或共轭双键。使用包含三氟乙酸或三氯乙酸，任选的另外的羧酸和硼氢化钠的反应混合物还原3-氧代-4-烯类固醇。

7. 发明申请

WO2019035061A1 NOVEL STEROIDS AND METHODS OF MANUFACTURE 审中-公开
公开(公告)号：WO2019035061A1
公开(公告)日：2019-02-21
申请号：PCT/IB2018/056205
申请日：2018-08-16
申请人： TRUSTEES OF DARTMOUTH COLLEGE
发明人： MICALIZIO, Glenn C. , EASTMAN, Alan
IPC分类号： C07C13/66 , A61K9/00 , A61K31/01 , A61K31/015 , C07C13/38 , C07C13/62
CPC分类号： A61P25/00 , C07C41/30 , C07J11/00 , C07J15/00 , C07J75/005 , C07C43/23
摘要： The present disclosure relates to methods of producing enantiodefined polycyclic ring compounds. More particularly, the present disclosure provides synthetic methods of producing biologically active enantiodefined steroidal compositions of both natural and unnatural ("ent-") absolute stereochemistry. The present disclosure also relates to methods of using said steroidal compositions prepared from this method as biologically active (e.g., therapeutic) components in compositions and/or directly as human and/or animal therapeutics and medicines. The present disclosure further relates to methods of producing and using said steroidal compositions of matter in chemical, pharmacological, and biological studies and research.

8. 发明申请

WO2015181275A1 CHOLANE DERIVATIVES FOR USE IN THE TREATMENT AND/OR PREVENTION OF FXR AND TGR5/GPBAR1 MEDIATED DISEASES 审中-公开
标题翻译：用于治疗和/或预防FXR和TGR5 / GPBAR1介导性疾病的CHOLANE衍生物
公开(公告)号：WO2015181275A1
公开(公告)日：2015-12-03
申请号：PCT/EP2015/061802
申请日：2015-05-28
申请人： BAR PHARMACEUTICALS S.R.L.
发明人： ZAMPELLA, Angela
IPC分类号： C07J9/00 , C07J31/00 , C07J41/00 , A61K31/575 , A61P1/16 , A61P9/00 , A61P9/10 , A61K35/00
CPC分类号： C07J31/006 , C07J9/00 , C07J9/005 , C07J11/00 , C07J41/0094
摘要： 13073PTWO 56 ABSTRACT The present invention relates to compounds having cholane scaffolds of formula (I), said compounds for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases. 5
摘要翻译：摘要本发明涉及具有式（I）的胆固醇支架的化合物，所述化合物用于治疗和/或预防FXR和TGR5 / GPBAR1介导的疾病。五

9. 发明申请

WO2009108388A2 ENZYMATIC PRODUCTION OR CHEMICAL SYNTHESIS AND USES FOR 5,7-DIENES AND UVB CONVERSION PRODUCTS THEREOF 审中-公开
标题翻译：酶促生产或化学合成及其用于5,7-二烯及其UVB转化产物的用途
公开(公告)号：WO2009108388A2
公开(公告)日：2009-09-03
申请号：PCT/US2009/001324
申请日：2009-03-02
申请人： UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
发明人： ZJAWIONY, Jordan, K. , LI, Wei , ZBYTEK, Blazej , TUCKEY, Robert, C. , ZJAWIONY Jordan, K. , NGUYEN, Minh Ngoc , ZMIJEWSKl Michal, A. , JANJETOVIC, Zorica , SWEATMAN Trevor, W. , MILLER, Duane, D. , CHEN, Jianjun
IPC分类号： A61K8/63 , C07J11/00 , C07J3/00 , A61P35/00
CPC分类号： C07C401/00 , A61K8/63 , A61K2800/81 , A61K2800/94 , A61Q19/00 , C07J3/00 , C07J11/00 , C12P7/02
摘要： Provided herein are steroidal compounds that are androsta-5,7-dienes or a pregna-5,7-dienes and ultraviolet B (UVB) conversion products thereof which includes pharmaceutical compositions of the steroidal compounds. Also provided is a method for producing hydroxylated metabolites of cholecalciferol via the P450scc (CYPl IA 1) or CYP27B 1 enzyme systems and the hydroxylated metabolites so produced. In addition, a method for inhibiting proliferation of either a normally or abnormally proliferating cell by contacting the cell with any of the compounds described herein. A related method is provided of treating a condition associated with the proliferating cell such as a cancer, a skin disorder, a defect in cell differentiation, cosmetic, prophylaxsis, or healthy cell maintenance.
摘要翻译：本文提供的是甾族化合物，其为雄甾-5,7-二烯或孕甾-5,7-二烯及其紫外B（UVB）转化产物，其包括甾体化合物的药物组合物。还提供了通过P450scc（CYP11A1）或CYP27B1酶系统产生胆钙化醇的羟基化代谢物和如此产生的羟基化代谢物的方法。此外，通过使细胞与本文所述的任何化合物接触来抑制正常或异常增殖细胞的增殖的方法。提供了治疗与增殖细胞相关的病症例如癌症，皮肤病症，细胞分化缺陷，美容，预防或健康细胞维持的相关方法。

10. 发明申请

WO2004014934A2 PROCESS AND NEW INTERMEDIATES FOR THE PREPARATION OF STEROIDS WITH A PROGESTOGEN ACTIVITY 审中-公开
标题翻译：用生物活性制备甾体的方法和新的中间体
公开(公告)号：WO2004014934A2
公开(公告)日：2004-02-19
申请号：PCT/EP0308505
申请日：2003-07-31
申请人： POLI IND CHIMICA SPA , GRISENTI PARIDE , PECORA FABIO , VERZA ELISA , LEONI MASSIMO , BOSSI LAURA
发明人： GRISENTI PARIDE , PECORA FABIO , VERZA ELISA , LEONI MASSIMO , BOSSI LAURA
IPC分类号： C07J1/00 , C07J11/00 , C07J21/00 , C07J
CPC分类号： C07J1/0059 , C07J11/00 , C07J21/008
摘要： The present invention relates to a new process of synthesis and to some new intermediates for the preparation of steroids with progestogen activity, more particularly, for the preparation of Desogestrel of formula (I). Said process is characterized by the regioselective reduction of the compound of formula (II) to give the intermediate of formula (III).
摘要翻译：本发明涉及一种新的合成方法和用于制备具有孕激素活性的类固醇的一些新的中间体，更具体地涉及式（I）的去氧孕烯的制备。所述方法的特征在于式（II）化合物的区域选择性还原以得到式（III）的中间体。

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