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1. 发明公开

EP3206494A4 COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS 审中-公开
公开(公告)号：EP3206494A4
公开(公告)日：2018-07-04
申请号：EP15851530
申请日：2015-10-16
申请人： SAGE THERAPEUTICS INC
发明人： MARTINEZ BOTELLA GABRIEL , SALITURO FRANCESCO G , ROBICHAUD ALBERT JEAN , HARRISON BOYD L
IPC分类号： C07J43/00 , A01N51/00 , A61K31/575 , A61K31/58 , A61P23/00 , A61P25/08 , A61P25/20 , C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J11/00 , C07J13/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , C07J71/00
CPC分类号： C07J43/003 , A61K31/575 , A61K31/58 , A61K45/06 , C07J1/0011 , C07J1/0022 , C07J3/005 , C07J5/0053 , C07J7/002 , C07J7/007 , C07J7/008 , C07J9/00 , C07J11/00 , C07J13/007 , C07J21/00 , C07J31/006 , C07J41/0066 , C07J51/00 , C07J71/001
摘要： Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein (II), A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

2. 发明公开

EP2968576A4 SYNTHESIS OF ENT-PROGESTERONE AND INTERMEDIATES THEREOF 失效转让
标题翻译： ENT孕酮和中间体的合成方法
公开(公告)号：EP2968576A4
公开(公告)日：2017-01-25
申请号：EP14764927
申请日：2014-03-15
申请人： THE FLORIDA STATE UNIV RES FOUND INCORPORATED , PREVACUS INC
发明人： CRAN JOHN W , HAN YINGLIN , ZHANG FALIANG
IPC分类号： A61K47/24 , A61K9/127 , A61K9/51 , A61K39/00 , A61K47/08
CPC分类号： C07J1/00 , C07C17/16 , C07C17/361 , C07C21/14 , C07C21/22 , C07C45/41 , C07C45/59 , C07C2601/10 , C07D317/72 , C07F7/0801 , C07F7/0809 , C07F7/0812 , C07F7/1852 , C07F7/1868 , C07F9/5022 , C07F9/5059 , C07F9/5442 , C07F9/5456 , C07F9/65517 , C07J5/0053 , C07J15/005 , C07J61/00 , C07C47/20 , C07C49/647
摘要： The present invention relates to the synthesis of ent-progesterone and intermediates thereof.
摘要翻译：本发明涉及对映 - 孕酮及其中间体的合成。

3. 发明公开

EP3107925A1 PROCESS FOR THE PRODUCTION OF 21 -METHOXY-11 -BETA-PHENYL-19-NOR-PREGNA-4,9-DIENE-3,20-DIONE DERIVATIVES 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON 21-甲氧基-11-苯乙烯-19-壬 - 孕-4,9-二烯-3,20-二氢衍生物
公开(公告)号：EP3107925A1
公开(公告)日：2016-12-28
申请号：EP15708050.8
申请日：2015-02-16
申请人： Richter Gedeon Nyrt.
发明人： MAHÓ, Sándor , SÁNTA, Csaba , CSÖRGEI, János , SZABÓ, Gábor , SCHÄFER, Tamás , BÉNI, Zoltán
IPC分类号： C07J5/00 , C07J41/00 , C07J51/00
CPC分类号： C07J41/0083 , C07J5/0053 , C07J51/00
摘要： The present invention relates to a process for the synthesis of compounds of formula (I), (I) wherein the meaning of R is dimethylamino or acetyl group, using the compound of formula (III) or (IV), wherein the meaning of R' is dimethylamino or 2-methyl-l,3-dioxan-2-yl group, as starting material and methoxymethy] lithium as reagent. (III) (IV)
摘要翻译：本发明涉及使用式（III）或（IV）的化合物合成式（I），（I）的化合物的方法，其中R的含义是二甲基氨基或乙酰基，其中R 二甲基氨基或2-甲基-1,3-二恶烷-2-基作为起始原料，甲氧基甲基]锂作为试剂。（三）（四）

4. 发明公开

EP3080140A2 POLYMORPHIC FORMS OF A STEROID-LIKE COMPOUND AND METHODS FOR THE PREPARATION AND USE THEREOF 审中-公开
标题翻译：多晶型生产和使用它们的类固醇式连接和方法
公开(公告)号：EP3080140A2
公开(公告)日：2016-10-19
申请号：EP14824667.1
申请日：2014-12-12
申请人： ALLERGAN, INC.
发明人： FENG, Shaoxin , SMITH, Scott W. , LAMBERT, Olivier M.G. , BUTTAR, Suzanne
IPC分类号： C07J5/00 , A61K31/573 , A61P27/06
CPC分类号： C07J7/008 , C07B2200/13 , C07J5/0053
摘要： Provided herein are multiple solid forms of a defined steroid-like compound, and methods for the preparation and use thereof. In one aspect, there is provided a crystalline form of said steroid-like compound, and methods for the preparation and use thereof. In another aspect, there is provided a substantially amorphous form of said steroid-like compound, and methods for the preparation and use thereof. In yet another aspect, there are provided compositions containing compounds according to the present invention. In certain aspects, such compositions are suitable for delivery of active agents according to the present invention to a subject in need thereof. In another aspect of the invention, there are provided methods for the treatment of a variety of indications, including glaucoma, ocular hypertension, and the like. In still another aspect of the present invention, there are provided kits containing compounds according to the present invention and/or compositions containing same.

5. 发明公开

EP2986623A4 19-NOR C3,3-DISUBSTITUTED C21-N-PYRAZOLYL STEROIDS AND METHODS OF USE THEREOF 有权
标题翻译： 19-NOR-C3,3二取代C21-N-PYRAZOLYLSTEROIDE及其方法使用
公开(公告)号：EP2986623A4
公开(公告)日：2016-09-28
申请号：EP14785712
申请日：2014-04-17
申请人： SAGE THERAPEUTICS INC
发明人： BOTELLA GABRIEL MARTINEZ , HARRISON BOYD L , ROBICHAUD ALBERT JEAN , SALITURO FRANCESCO G , BERESIS RICHARD THOMAS
IPC分类号： C07J3/00 , A61K31/57 , A61K31/573 , A61K31/58 , A61P25/00 , C07J7/00 , C07J15/00
CPC分类号： A61K31/58 , A61K9/0019 , A61K31/573 , C07J1/0059 , C07J1/007 , C07J1/0074 , C07J3/00 , C07J5/0015 , C07J5/0053 , C07J7/00 , C07J7/002 , C07J7/007 , C07J7/0085 , C07J13/007 , C07J15/00 , C07J21/00 , C07J31/006 , C07J43/003
摘要： and pharmaceutically acceptable salts thereof; wherein , R1, R2, R3a, R3b, R4a, R4b, R5, R6, and R7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

6. 发明公开

EP3040342A1 PURIFIED DEOXYCHOLIC ACID AND ITS COSMETIC USE IN THE NON-SURGICAL REMOVAL OF UNDESIRABLE FAT DEPOSITS 无效
标题翻译： CLEAN脱氧胆酸和多余脂肪堆积的非手术切除的美容用途
公开(公告)号：EP3040342A1
公开(公告)日：2016-07-06
申请号：EP15202046.7
申请日：2010-12-17
申请人： Kythera Biopharmaceuticals, Inc.
发明人： MORIARTY, Robert M. , REID, John Gregory , SWARINGEN Jr, Roy A.
IPC分类号： C07J9/00 , A61K31/575 , C07J5/00 , C07J13/00 , C07J41/00 , C07J1/00
CPC分类号： C07J9/005 , A61K31/575 , C07J1/0011 , C07J5/0053 , C07J9/00 , C07J13/007 , C07J41/0061 , Y02P20/55
摘要： Compositions of deoxycholic acid (DCA) containing a steroidal DCA precursor or by-product containing a 12.beta.-hydroxy group (in particular 12.beta.-DCA) and their use in a cosmetic method of non-surgical removal of undesirable fat deposits.
摘要翻译：的脱氧胆酸（DCA）含类固醇前体DCA或副产品含一个12.beta.羟基基团的组合物（特别是12.beta.-DCA）及其在非手术去除的不希望的脂肪的美容方法使用存款。

7. 发明公开

EP2968576A2 SYNTHESIS OF ENT-PROGESTERONE AND INTERMEDIATES THEREOF 失效转让
标题翻译：耳 - 孕酮的合成及其中间体
公开(公告)号：EP2968576A2
公开(公告)日：2016-01-20
申请号：EP14764927.1
申请日：2014-03-15
申请人： The Florida State University Research Foundation Inc. , Prevacus Inc.
发明人： CRAN, John, W. , HAN, Yinglin , ZHANG, Faliang
IPC分类号： A61K47/24 , A61K47/08 , A61K39/00 , A61K9/127 , A61K9/51
CPC分类号： C07J1/00 , C07C17/16 , C07C17/361 , C07C21/14 , C07C21/22 , C07C45/41 , C07C45/59 , C07C2601/10 , C07D317/72 , C07F7/0801 , C07F7/0809 , C07F7/0812 , C07F7/1852 , C07F7/1868 , C07F9/5022 , C07F9/5059 , C07F9/5442 , C07F9/5456 , C07F9/65517 , C07J5/0053 , C07J15/005 , C07J61/00 , C07C47/20 , C07C49/647
摘要： The present invention relates to the synthesis of ent-progesterone and intermediates thereof.
摘要翻译：本发明涉及对黄体酮及其中间体的合成。

8. 发明公开

EP2805720A1 Non-hormonal steroid modulators of NF-KB for treatment of disease 无效转让
标题翻译： Nichthormonale steroide Modulatoren von NF-KB zur Behandlung von Erkrankungen
公开(公告)号：EP2805720A1
公开(公告)日：2014-11-26
申请号：EP14173342.8
申请日：2009-05-28
申请人： Validus Biopharma, Inc.
发明人： Mccall, John, M. , Hoffman, Eric , Kanneboyina, Nagaraju
IPC分类号： A61K31/575 , A61P21/00 , A61P19/02 , A61P11/06
CPC分类号： A61K31/573 , A61K31/57 , A61K31/575 , C07J5/0038 , C07J5/0053 , C07J5/0076 , Y02A50/479 , Y10S514/824 , Y10S514/825 , Y10S514/826 , Y10S514/903
摘要： The present invention is directed to a compound for use in reducing the symptoms of muscular dystrophy, wherein said compound has structural Formula I:

wherein:
said dashed line indicates an optional double bond;
each R 1 is hydrogen;
R 2 is selected from the group consisting of hydrogen and methyl;
R 3 is selected from the group consisting of hydrogen, hydroxyl, and methyl;
or R 2 and R 3 may be taken together to form a double bond;
R 4 is -(CO) n (C(R 5 )(R 6 )) m (R 7 );
R 5 and R 6 are independently selected from the groups consisting of hydrogen and C 1-3 alkyl;
R 7 is selected from the group consisting of -N(R 8 )(R 9 ) and -OR 10 ;
R 8 , and R 9 are each independently selected from the group consisting of hydrogen, lower alkyl, and -(C(R 5 ) 2 ) p R 11 ; or R 8 and R 9 may be taken together to form a heterocycloalkyl;
R 10 is selected from the group consisting of hydrogen, acyl, lower alkyl, and-(C(R 5 ) 2 ) p R 11 ;
R 11 is selected from the group consisting of hydroxyl and amino;
n is 0 or 1;
m is an integer between 1 and 3;
p is an integer between 1 and 3; and
q is an integer between 1 and 4.
摘要翻译：本发明涉及用于减轻肌营养不良症状的化合物，其中所述化合物具有结构式I：其中：所述虚线表示任选的双键; 每个R 1是氢; R 2选自氢和甲基; R 3选自氢，羟基和甲基; 或者R 2和R 3可以一起形成双键; R 4为 - （CO）n（C（R 5）（R 6））m（R 7）; R 5和R 6独立地选自氢和C 1-3烷基; R 7选自-N（R 8）（R 9）和-OR 10; R 8和R 9各自独立地选自氢，低级烷基和 - （C（R 5）2）p R 11; 或R 8和R 9可以一起形成杂环烷基; R 10选自氢，酰基，低级烷基和 - （C（R 5）2）p R 11; R 11选自羟基和氨基; n为0或1; m是1和3之间的整数; p是1和3之间的整数; q为1〜4之间的整数。

9. 发明公开

EP2776041A1 PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF 4-PREGENEN-11ß-17-21-TRIOL-3,20-DIONE DERIVATIVES 审中-公开
标题翻译：药物组合物和使用4 PREGENEN-11β-17-21三醇-3,20-二酮衍生物的方法
公开(公告)号：EP2776041A1
公开(公告)日：2014-09-17
申请号：EP12787337.0
申请日：2012-11-09
申请人： ALLERGAN, INC.
发明人： EDELMAN, Jeffrey L. , NEHME, Alissar
IPC分类号： A61K31/575 , A61P27/02
CPC分类号： A61K31/58 , A61K9/0048 , A61K31/56 , A61K31/573 , A61K31/575 , A61K2121/00 , C07J5/0053 , C07J7/008 , C07J17/00 , C07J31/006
摘要： The present invention relates to pharmaceutical compositions comprising 4-pregenen-11&bgr;-17-21-triol-3,20-dione derivatives, and their use as pharmaceuticals as modulators of the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR). The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat ocular conditions associated with the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR).

10. 发明公开

EP2755939A2 HALOGENATED PHENOLS FOR DIAGNOSTICS, ANTIOXIDANT PROTECTION AND DRUG DELIVERY 审中-公开
标题翻译：卤代酚诊断，抗氧化剂保护及药物CHARGE
公开(公告)号：EP2755939A2
公开(公告)日：2014-07-23
申请号：EP12811241.4
申请日：2012-07-13
申请人： Latham, Keith, R.
发明人： Latham, Keith, R.
IPC分类号： C07C39/24 , C07C39/34 , C07C205/00
CPC分类号： A61K47/48023 , A61K49/006 , A61K49/0438 , A61K51/0446 , C07C43/295 , C07C217/60 , C07C229/36 , C07C233/25 , C07C323/52 , C07D209/36 , C07D475/08 , C07D489/02 , C07D499/897 , C07J1/0022 , C07J5/0053 , G01N33/52 , Y10T436/145555
摘要： The present invention provides compositions and methods for the administration and targeted delivery, release and/or formation of a drug compound from a halogenated phenol starting compound of the present invention at site(s) within the body of an individual having high FROS, such as within a diseased and/or inflamed tissue. The present invention further provides compositions and methods for the administration of FROS scavenging compounds to an individual to protect cells and tissues from damage that might be caused by FROS. The present invention further provides compositions and methods for the detection of a detectable product, such as an indigo-like compound or other product of a dehalogenation reaction, formed from a compound of the present invention as a measurement or indication of the amount and/or localization of high FROS levels in the body of an individual.

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