公开(公告)号：EP3848382B1

公开(公告)日：2023-11-29

申请号：EP21160246.1

申请日：2017-05-18

发明人： WEYMOUTH-WILSON, Alexander, Charles ,  KOMSTA, Zofia ,  WALLIS, Laura ,  DAVIES, Ieuan ,  BATCHELOR, Rhys ,  EVANS, Timothy ,  OTTER, Carl

IPC分类号： C07J71/00 ,  C07J9/00 ,  C07J17/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00 ,  C07J13/00 ,  C07J21/00 ,  C07J31/00

公开(公告)号：EP3719029A1

公开(公告)日：2020-10-07

申请号：EP20159317.5

申请日：2015-11-27

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 ,  C07J17/00 ,  C07J43/00 ,  A61K31/56 ,  A61P25/08 ,  A61P25/00 ,  A61K45/06 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J9/00

摘要： Described herein are neuroactive steroids of the Formula ( II ):

or a pharmaceutically acceptable salt thereof; wherein A, R 1 , R 2a , R 2b , R 3a , R 3b , R 4a , R 4b , R 5 , R 6 and ------ 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.

公开(公告)号：EP3224269B1

公开(公告)日：2020-02-26

申请号：EP15862506.1

申请日：2015-11-27

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 ,  C07J17/00 ,  C07J43/00 ,  A61K31/56 ,  A61P25/08 ,  A61P25/00 ,  A61K45/06 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  C07J9/00

公开(公告)号：EP2039701A3

公开(公告)日：2013-02-27

申请号：EP08101671.9

申请日：1999-03-05

申请人： RESEARCH TRIANGLE INSTITUTE

发明人： Cook, Edgar, C. ,  Kepler, John, A. ,  Zhang, Ping-sheng ,  Lee, Yue-wei ,  Tallent, Ray, C.

IPC分类号： C07J33/00 ,  C07J43/00 ,  A61K31/58 ,  A61P5/36 ,  C07J41/00

CPC分类号： C07J41/0083 ,  A61K31/58 ,  C07J43/006 ,  Y10S514/841 ,  Y10S514/843

摘要： The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.

公开(公告)号：EP2067784A3

公开(公告)日：2012-08-22

申请号：EP08020059.5

申请日：2001-08-03

申请人： Glaxo Group Limited

发明人： Payne, Jeremy John ,  Jones, Paul ,  Biggadike, Keith

IPC分类号： C07J31/00 ,  A61K31/58 ,  C07J33/00 ,  C07J71/00 ,  C07J3/00 ,  A61P5/44

CPC分类号： C07J31/006

摘要： There are provided according to the invention compounds of formula (I)

wherein
R 1 represents C 1-6 alkyl or C 1-6 haloalkyl;
R 2 represents -C(=O)-aryl or -C(=O)-heteroaryl;
R 3 represents hydrogen, methyl (which may be in either the α or β configuration) or methylene;
R 4 and R 5 are the same or different and each represents hydrogen or halogen; and
----- represents a single or a double bond;
and salts and solvates thereof.
There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.

公开(公告)号：EP1305330B1

公开(公告)日：2008-12-03

申请号：EP01954149.9

申请日：2001-08-03

申请人： GLAXO GROUP LIMITED

发明人： BIGGADIKE, Keith, c/o GlaxoSmithKline ,  JONES, Paul, c/o GlaxoSmithKline ,  PAYNE, Jeremy, John, c/o GlaxoSmithKline

IPC分类号： C07J31/00 ,  A61K31/58 ,  C07J33/00 ,  C07J71/00 ,  C07J3/00 ,  A61P5/44

CPC分类号： C07J31/006

摘要： There are provided according to the invention compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents -C(=O)-aryl or -C(=O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the α or β configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and ---- represents a single or a double bond; and salts and solvates thereof. There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.

公开(公告)号：EP1395604B1

公开(公告)日：2008-06-25

申请号：EP02730498.9

申请日：2002-06-11

申请人： GLAXO GROUP LIMITED

发明人： BIGGADIKE, Keith GlaxoSmithKline ,  JONES, Paul GlaxoSmithKline

IPC分类号： C07J31/00 ,  C07J17/00 ,  C07J33/00 ,  C07J43/00 ,  A61K31/58 ,  A61P5/44

CPC分类号： C07J33/002 ,  C07J17/00 ,  C07J43/003

摘要： There are provided compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents a 4-7 membered non-aromatic ring containing 1-3 heteroatoms selected from O, N and S optionally substituted with one or more methyl, ethyl or halogen groups; R3 represents hydrogen, methyl (which may be in either the alpha or beta configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and (a) represents a single or a double bond; and salts and solvates thereof; processes for preparing them and their use in therapy.

公开(公告)号：EP1554303B1

公开(公告)日：2006-12-27

申请号：EP03766325.9

申请日：2003-07-28

申请人： Novartis AG ,  Novartis Pharma GmbH

发明人： JORDINE, Guido ,  MUTZ, Michael

IPC分类号： C07J33/00 ,  A61K31/58 ,  A61P11/00

CPC分类号： C07J33/00 ,  C07J33/002

摘要： Polymorphic crystal forms of 3-methylthiophene-2-carboxylic acid (6S,9R,10S,11S,13S,16R,17R)-9-chloro-6-fluoro-11-hydroxy-l7-methoxycarbonyl-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-l7-yl ester. The crystal forms possess anti-inflammatory activity and have very good stability. Methods for preparing the crystal forms are also described.

摘要翻译： 3-甲基噻吩-2-羧酸（6S，9R，10S，11S，13S，16R，17R）-9-氯-6-氟-11-羟基-17-甲氧基羰基-10,13,16-三氟甲基苯并呋喃的多晶形晶体形式 3-三甲基-3-氧代-6,7,8,9,10,11,12,13,14,15,16,17-十二氢-3H-环戊二烯并[a]菲-17-基酯。 晶体形式具有抗炎活性并具有非常好的稳定性。 还描述了制备晶型的方法。

公开(公告)号：EP1144431B1

公开(公告)日：2005-12-21

申请号：EP00907539.1

申请日：2000-02-09

申请人： Schering Aktiengesellschaft

发明人： KÜNZER, Hermann ,  KNAUTHE, Rudolf ,  LESSL, Monika ,  FRITZEMEIER, Karl-Heinrich ,  HEGELE-HARTUNG, Christa ,  BÖMER, Ulf ,  MÜLLER, Gerd ,  KOSEMUND, Dirk

IPC分类号： C07J53/00 ,  C07J1/00 ,  A61K31/565 ,  C07J31/00 ,  C07J41/00 ,  C07J33/00 ,  C07J15/00

CPC分类号： C07J41/0094 ,  C07J1/0055 ,  C07J1/0066 ,  C07J15/00 ,  C07J31/006 ,  C07J33/002 ,  C07J53/004

摘要： The invention relates to novel compounds as pharmaceutical agents which have in vitro a higher affinity to estrogen receptor preparations of the rat prostate than to estrogen receptor preparations of the rat uterus and which preferably have in vivo a preferential effect on bones as compared to the uterus and/or a marked effect with regard to the stimulation of the expression of the 5HT2a receptor and transporter. The invention also relates to the production and to the use in therapy of these compounds and to pharmaceutical administration forms containing said novel compounds. The novel compounds are 16 alpha and 16 beta hydroxy-estra,1,3,5(10)-estratriene which carry additional substituents at the steroid backbone and one or more additional double bonds on the B, C and/or D rings.

公开(公告)号：EP1060186A1

公开(公告)日：2000-12-20

申请号：EP99909531.8

申请日：1999-03-05

申请人： RESEARCH TRIANGLE INSTITUTE

发明人： COOK, C., Edgar ,  KEPLER, John, A. ,  ZHANG, Ping-sheng ,  LEE, Yue-wei ,  TALLENT, C., Ray

IPC分类号： C07J33/00 ,  C07J43/00 ,  A61K31/58

CPC分类号： C07J41/0083 ,  A61K31/58 ,  C07J43/006 ,  Y10S514/841 ,  Y10S514/843

摘要： The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.