公开(公告)号：EP2675786B1

公开(公告)日：2018-12-26

申请号：EP12705582.0

申请日：2012-02-13

申请人： ALLERGAN, INC.

发明人： WOODWARD, David, F. ,  WANG, Jenny, W. ,  GARST, Michael, E. ,  BURK, Robert, M. ,  GAC, Todd, S. ,  POLOSO, Neil, J.

IPC分类号： C07C405/00 ,  A61K8/42 ,  A61Q7/00

CPC分类号： C07C235/34 ,  A61K8/42 ,  A61Q7/00 ,  C07C405/00 ,  C07C405/0041 ,  C07C2601/08

摘要： Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same.

公开(公告)号：EP2872493B1

公开(公告)日：2018-11-14

申请号：EP13817021.2

申请日：2013-07-12

申请人： Indiana University Research and Technology Corporation ,  The Brigham and Women's Hospital, Inc. ,  The University of Massachusetts

发明人： ANDROPHY, Elliot J. ,  CHERRY, Jonathon J. ,  CUNY, Gregory D. ,  GLICKSMAN, Marcie A.

IPC分类号： C07D261/06 ,  C07D413/12 ,  A61K31/42 ,  A61P21/00

CPC分类号： C07D493/04 ,  C07C311/37 ,  C07C2601/08 ,  C07C2603/20 ,  C07D213/75 ,  C07D215/227 ,  C07D215/44 ,  C07D221/10 ,  C07D231/14 ,  C07D233/88 ,  C07D239/47 ,  C07D239/82 ,  C07D261/06 ,  C07D261/14 ,  C07D261/18 ,  C07D263/48 ,  C07D267/14 ,  C07D277/46 ,  C07D285/135 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07K14/47

摘要： Disclosed herein are compositions and methods for treatment of spinal muscular atrophy (SMA). In certain embodiments, compounds are provided that increase full-length survival of motor neuron (SMN) protein production by an SMN2 gene.

公开(公告)号：EP3389379A1

公开(公告)日：2018-10-24

申请号：EP16809068.6

申请日：2016-12-12

申请人： Syngenta Participations AG

发明人： WEISS, Matthias ,  GAGNEPAIN, Julien, Daniel, Henri ,  HOFFMAN, Thomas, James ,  SULZER-MOSSE, Sarah ,  LAMBERTH, Clemens

IPC分类号： A01N37/52 ,  C07C257/12 ,  A01P3/00

CPC分类号： C07C257/12 ,  A01N37/52 ,  A01N43/10 ,  A01N43/36 ,  A01N43/38 ,  A01N43/40 ,  A01N43/54 ,  A01N43/56 ,  A01N43/653 ,  C07C317/32 ,  C07C321/28 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07D213/61 ,  C07D231/12 ,  C07D231/56 ,  C07D235/08 ,  C07D239/34 ,  C07D249/08 ,  C07D295/125 ,  C07D333/20 ,  C07D333/58

摘要： Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.

公开(公告)号：EP3383845A1

公开(公告)日：2018-10-10

申请号：EP16822513.4

申请日：2016-11-11

申请人： Chinoin Gyógyszer és Vegyészeti Termékek Gyára Zrt.

发明人： TAKÁCS, László ,  FEKETE, Ibolya ,  BUZDER-LANTOS, Péter ,  LÁSZLÓFI, István ,  HORTOBÁGYI, Irén ,  HAVASI, Gábor ,  KARDOS, Zsuzsanna

IPC分类号： C07C405/00

CPC分类号： C07C405/00 ,  C07C2601/08

摘要： The subject of the invention is a process for the preparation of Latanoprostene bunod of formula (I) with a purity higher than 95% where chromatography is used applying normal phase gravity silicagel column chromatography where the used silicagel is irregular silicagel or spherical silicagel an as eluent and eluent mixture consisting of an apolar and a polar solvent is used and if desired, contamination of the purified compound of formula I arising from the solvents are removed by silicagel filtration chromatography.

公开(公告)号：EP2655334B1

公开(公告)日：2018-10-03

申请号：EP11851853.9

申请日：2011-12-22

申请人： Eutropics Pharmaceuticals, Inc.

发明人： CARDONE, Michael H. ,  YU, Xiang Y. ,  KOLODZIEJ, Andrew F.

IPC分类号： C07D233/56 ,  C07D233/58

CPC分类号： A61K31/498 ,  A61K31/454 ,  A61K31/573 ,  A61K31/69 ,  A61K45/06 ,  C07C217/92 ,  C07C229/18 ,  C07C229/34 ,  C07C229/36 ,  C07C229/48 ,  C07C229/58 ,  C07C229/60 ,  C07C229/64 ,  C07C311/21 ,  C07C317/36 ,  C07C317/44 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/08 ,  C07D209/34 ,  C07D211/46 ,  C07D211/60 ,  C07D213/79 ,  C07D215/48 ,  C07D231/14 ,  C07D231/38 ,  C07D235/26 ,  C07D239/28 ,  C07D239/42 ,  C07D241/46 ,  C07D261/18 ,  C07D263/34 ,  C07D263/48 ,  C07D309/14

摘要： The invention relates to a chemotherapeutic cancer treatment in which compounds (BH3Is) are administered to a mammal to treat B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. The invention also provides a method for treating types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more disclosed compounds in combination with other therapies, for example, 26S proteosome inhibitors, such as, for example, Bortezomib. The invention also relates to autoimmune treatment with pharmaceutical compositions comprising one or more disclosed compounds. The invention also relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease. Illustrative compounds are those of Formula II:

公开(公告)号：EP2318355B1

公开(公告)日：2018-09-12

申请号：EP09781046.9

申请日：2009-07-24

申请人： Boehringer Ingelheim International GmbH

发明人： ECKHARDT, Matthias ,  HAMILTON, Bradford, S. ,  HIMMELSBACH, Frank

IPC分类号： C07C255/45 ,  C07C69/00 ,  C07D263/56 ,  C07C271/24 ,  C07D217/04 ,  C07C69/753 ,  C07D223/16 ,  C07D235/16 ,  C07C211/35 ,  C07D239/74 ,  C07D241/04 ,  C07C233/32 ,  C07D257/04 ,  C07D205/04 ,  C07D207/08 ,  C07D271/06 ,  C07D209/08 ,  C07D211/56 ,  C07D295/185 ,  C07D213/64 ,  C07C62/06

CPC分类号： C07D295/185 ,  C07C62/06 ,  C07C62/38 ,  C07C69/00 ,  C07C69/753 ,  C07C211/35 ,  C07C233/32 ,  C07C233/57 ,  C07C233/58 ,  C07C233/60 ,  C07C255/45 ,  C07C271/24 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/74 ,  C07D205/04 ,  C07D207/08 ,  C07D209/08 ,  C07D209/44 ,  C07D211/56 ,  C07D213/64 ,  C07D217/04 ,  C07D223/16 ,  C07D235/16 ,  C07D239/74 ,  C07D241/04 ,  C07D257/04 ,  C07D263/56 ,  C07D271/06

摘要： The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11&bgr;-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases.

公开(公告)号：EP2980056B1

公开(公告)日：2018-08-29

申请号：EP14775478.2

申请日：2014-03-26

申请人： Zeon Corporation

发明人： NAKANO, Yasushi ,  SASANUMA, Takashi

IPC分类号： C07C41/06 ,  C07C43/184 ,  C07B61/00

CPC分类号： C07C41/06 ,  C07C2601/08 ,  C07C43/184

摘要： The present invention is a method for producing a cycloalkyl alkyl ether compound comprising reacting substituted or unsubstituted cyclopentene or substituted or unsubstituted cyclohexene with an alcohol compound represented by a formula (2): R 1 OH (wherein R 1 is a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, or a substituted or unsubstituted cycloalkyl group having 3 to 8 carbon atoms) in a gaseous state in presence of an acidic ion-exchange resin to produce a cycloalkyl alkyl ether compound represented by a formula (1): R 1 -O-R 2 (wherein R 1 is the same as defined above, and R 2 is a substituted or unsubstituted cyclopentyl group or a substituted or unsubstituted cyclohexyl group), the acidic ion-exchange resin having a specific surface area of 20 to 50 m 2 /g, an average pore size of 20 to 70 nm, and a total exchange capacity of 4.8 to 6.0 eq/L-R wet resin.

公开(公告)号：EP2502907B1

公开(公告)日：2018-08-29

申请号：EP12003856.7

申请日：2009-03-25

申请人： Grünenthal GmbH

发明人： Nolte, Bernd ,  Schröder, Wolfgang ,  Linz, Klaus ,  Englberger, Werner ,  Schick, Hans ,  Graubaum, Habil Heinz ,  Braun, Birgit ,  Ozegowski, Sigrid ,  Bálint, József ,  Sonnenschein, Helmut

IPC分类号： C07D209/12 ,  C07D209/14 ,  C07C211/40 ,  C07C215/42 ,  C07C233/36 ,  C07C311/18 ,  A61K31/404 ,  A61K31/137 ,  A61P25/00 ,  C07C215/14 ,  C07C217/74 ,  C07C223/04 ,  C07C229/16 ,  C07C233/40 ,  C07C233/41 ,  C07C233/62 ,  C07C233/79 ,  C07C235/54 ,  C07C237/06 ,  C07C275/24 ,  C07C311/07

CPC分类号： C07D209/20 ,  A61K31/135 ,  A61K31/136 ,  A61K31/165 ,  A61K31/18 ,  A61K31/404 ,  A61K31/53 ,  A61K31/5377 ,  A61K45/06 ,  C07C211/40 ,  C07C211/54 ,  C07C215/14 ,  C07C215/42 ,  C07C217/74 ,  C07C223/04 ,  C07C229/16 ,  C07C233/36 ,  C07C233/40 ,  C07C233/41 ,  C07C233/62 ,  C07C233/79 ,  C07C235/54 ,  C07C237/06 ,  C07C237/24 ,  C07C275/24 ,  C07C311/07 ,  C07C311/18 ,  C07C311/37 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07D209/12 ,  C07D209/14 ,  C07D211/62 ,  C07D213/12 ,  C07D213/82 ,  C07D231/14 ,  C07D251/48 ,  C07D251/54 ,  C07D295/135 ,  C07D309/08 ,  C07D333/20 ,  C07D403/08 ,  C07D409/08

公开(公告)号：EP3357916A1

公开(公告)日：2018-08-08

申请号：EP16850389.4

申请日：2016-09-30

申请人： CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd.

发明人： SHI, Ying ,  MI, Yi ,  YANG, Hanyu ,  WANG, Xuliang ,  GONG, Denghuang ,  BAI, Min ,  CHEN, Xiaozhuo ,  CHEN, Yujie ,  ZHANG, Xuejiao ,  MA, Yuxiu ,  GAO, Qingzhi

IPC分类号： C07D237/24 ,  C07D403/12 ,  A61K31/50 ,  A61K31/44 ,  A61P29/00 ,  A61P19/00 ,  A61P9/00 ,  A61P11/00

CPC分类号： C07C235/84 ,  A61K31/44 ,  A61K31/50 ,  C07C231/12 ,  C07C237/38 ,  C07C237/42 ,  C07C273/1854 ,  C07C275/38 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/16 ,  C07D211/46 ,  C07D213/81 ,  C07D213/82 ,  C07D237/24 ,  C07D277/82 ,  C07D295/192 ,  C07D333/38 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D409/06

摘要： The present invention relates to a benzamide derivative of general formula I, a drug composition containing same and a use thereof as a drug, wherein the definitions of R 1 , Z and Q are as described in the description.

公开(公告)号：EP3350158A1

公开(公告)日：2018-07-25

申请号：EP16847451.8

申请日：2016-09-16

申请人： Metacrine, Inc.

发明人： SMITH, Nicholas D. ,  GOVEK, Steven P. ,  NAGASAWA, Johnny Y.

IPC分类号： C07C233/55 ,  C07C255/60 ,  C07C233/63 ,  C07D309/06 ,  C07D305/06 ,  A61K31/16

CPC分类号： C07C233/54 ,  A61K31/16 ,  A61K31/216 ,  A61K31/27 ,  A61K31/277 ,  A61K31/337 ,  A61K31/351 ,  A61K31/36 ,  A61K31/382 ,  A61K31/397 ,  A61K31/402 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/426 ,  A61K31/4406 ,  A61K31/4453 ,  A61K31/45 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5375 ,  A61K45/06 ,  A61P1/16 ,  C07C233/63 ,  C07C233/65 ,  C07C233/81 ,  C07C233/87 ,  C07C235/04 ,  C07C235/16 ,  C07C235/40 ,  C07C235/56 ,  C07C235/64 ,  C07C235/82 ,  C07C237/24 ,  C07C255/57 ,  C07C255/60 ,  C07C271/24 ,  C07C271/28 ,  C07C311/07 ,  C07C311/08 ,  C07C317/32 ,  C07C317/44 ,  C07C323/50 ,  C07C323/61 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/16 ,  C07C2602/42 ,  C07C2603/74 ,  C07D205/04 ,  C07D209/04 ,  C07D211/06 ,  C07D211/62 ,  C07D211/76 ,  C07D211/94 ,  C07D211/96 ,  C07D213/40 ,  C07D231/12 ,  C07D231/56 ,  C07D235/04 ,  C07D235/08 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D249/18 ,  C07D261/08 ,  C07D265/30 ,  C07D277/28 ,  C07D295/088 ,  C07D295/135 ,  C07D295/195 ,  C07D295/26 ,  C07D305/08 ,  C07D309/08 ,  C07D317/58 ,  C07D319/12 ,  C07D335/02 ,  A61K2300/00

摘要： Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.