公开(公告)号：EP3126336A1

公开(公告)日：2017-02-08

申请号：EP15713528.6

申请日：2015-04-02

Applicant: Sanofi

Inventor： SCHWINK, Lothar ,  BUNING, Christian ,  GLOMBIK, Heiner ,  GOSSEL, Matthias ,  KADEREIT, Dieter ,  HALLAND, Nis ,  LOHMANN, Matthias ,  PÖVERLEIN, Christoph ,  RITTER, Kurt

IPC: C07D231/56 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/4745 ,  C07D249/18 ,  C07D471/04 ,  A61P3/00

CPC classification number: C07D471/04 ,  A61K31/155 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/702 ,  A61K45/06 ,  C07D231/56 ,  C07D249/18 ,  C07D401/14 ,  A61K2300/00

Abstract: The substituted fused heterocyclic compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of substituted fused heterocyclic compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract translation: 所述substituiertem稠合杂环化合物是GPR119调节剂和用于治疗糖尿病，肥胖，血脂异常和相关疾病的预防和/或治疗是有用的。 本发明进一步更涉及使用的substituiertem稠合杂环化合物作为医药品的活性成分，以及包含它们的药物组合物。

公开(公告)号：EP3122743A1

公开(公告)日：2017-02-01

申请号：EP15769990.1

申请日：2015-03-27

Applicant: Azevan Pharmaceuticals, Inc.

Inventor： BROWNSTEIN, Michael J.

IPC: C07D409/14 ,  C07D413/04

CPC classification number: C07D413/04 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/4453 ,  A61K31/496 ,  A61K45/00 ,  C07D413/14

Abstract: Compounds, and compositions, methods, and uses thereof, are described herein for treating neurodegenerative diseases and disorders. In particular, vasopressin receptor modulators, and compositions, methods and uses thereof, are described herein for treating neuropsychiatric aspects of neurodegenerative diseases such as Huntington's Disease, Parkinson's Disease, and Alzheimer's Disease.

Abstract translation: 本文描述了用于治疗神经变性疾病和病症的化合物及其组合物，方法和用途。 特别地，本文描述了加压素受体调节剂及其组合物，方法和用途，用于治疗神经变性疾病如亨廷顿病，帕金森病和阿尔茨海默病的神经精神方面。

公开(公告)号：EP3116497A2

公开(公告)日：2017-01-18

申请号：EP15711448.9

申请日：2015-03-12

Applicant: F. Hoffmann-La Roche AG ,  Genentech, Inc.

Inventor： HAGER, Jeffrey H. ,  CHOW MANEVAL, Edna ,  SMITH, Nicholas D. ,  FRIEDMAN, Lori ,  SAMPATH, Deepak

IPC: A61K31/397 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/428 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06 ,  A61P35/00

CPC classification number: A61K31/4439 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/416 ,  A61K31/4188 ,  A61K31/424 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/437 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/553 ,  A61K45/06 ,  A61K2300/00

Abstract: Described herein are therapeutic combinations with estrogen receptor modulators for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract translation: 本文描述的是用于治疗介导或依赖于雌激素受体的疾病或病症的雌激素受体调节剂的治疗组合。

公开(公告)号：EP3112343A1

公开(公告)日：2017-01-04

申请号：EP15755910.5

申请日：2015-02-27

Applicant: Tohoku University ,  National University Corporation Gunma University ,  Fuso Pharmaceutical Industries, Ltd.

Inventor： KIKUCHI, Haruhisa ,  OSHIMA, Yoshiteru ,  HATTORI, Toshio ,  KUBOHARA, Yuzuru ,  YAMADA, Osamu ,  ZHANG, Jing ,  MATSUSHITA, Yoshihisa ,  KIDA, Shinya

IPC: C07C235/50 ,  A61K31/165 ,  A61K31/166 ,  A61K31/351 ,  A61K31/4045 ,  A61K31/437 ,  A61P1/16 ,  A61P9/10 ,  A61P11/00 ,  A61P13/04 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C233/36 ,  C07C233/62 ,  C07C233/78 ,  C07C235/48

CPC classification number: C07C235/50 ,  A61K31/165 ,  A61K31/166 ,  A61K31/167 ,  A61K31/351 ,  A61K31/381 ,  A61K31/397 ,  A61K31/40 ,  A61K31/4045 ,  A61K31/437 ,  A61K31/4409 ,  A61K31/445 ,  C07C233/36 ,  C07C233/62 ,  C07C233/78 ,  C07C235/48 ,  C07C235/60 ,  C07C237/22 ,  C07C237/34 ,  C07C237/42 ,  C07C2101/14 ,  C07C2601/14 ,  C07D205/04 ,  C07D207/16 ,  C07D209/14 ,  C07D211/60 ,  C07D213/81 ,  C07D309/08 ,  C07D333/38 ,  C07D471/04

Abstract: The present invention provides a useful medicament for the treatment and/or prophylaxis of a disease associated with the enhancement of OPN production including cancer, which comprises a compound of formula:

wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , m, n, p, X, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明提供了一种治疗和/或预防与包括癌症在内的OPN产生增强有关的疾病的有用药物，其包含下式的化合物：其中R 1，R 2，R 3，R 4，R 5， R 6，R 7，m，n，p，X和Y如说明书中所定义，或其药学上可接受的盐。

公开(公告)号：EP3010502A4

公开(公告)日：2017-01-04

申请号：EP14813526

申请日：2014-06-18

Applicant: SERAGON PHARMACEUTICALS INC

Inventor： GOVEK STEVEN P ,  KAHRAMAN MEHMET ,  SMITH NICHOLAS D ,  HAGER JEFFREY H ,  CHOW MANEVAL EDNA

IPC: A61K31/397 ,  A61K9/06 ,  A61K9/08 ,  A61P35/00 ,  C07D405/12

CPC classification number: A61K31/397 ,  A61K9/0014 ,  A61K9/0053 ,  A61K9/06 ,  A61K9/08 ,  A61K9/20 ,  A61K9/48 ,  A61K45/06 ,  C07D405/12

Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

Abstract translation: 本文描述的是雌激素受体调节剂的化合物。 还描述了包括本文所述化合物的药物组合物和药物，以及使用这样的雌激素受体调节剂单独和与其它化合物组合用于治疗介导或依赖于雌激素受体的疾病或病症的方法。

公开(公告)号：EP3094318A4

公开(公告)日：2016-11-23

申请号：EP15734870

申请日：2015-01-09

Applicant: KANNALIFE INC

Inventor： BRENNEMAN DOUGLAS E ,  KINNEY WILLIAM ALVIN ,  MCDONNELL MARK ,  PETKANAS DEAN

IPC: A61K31/05 ,  C07D205/04 ,  C07D205/06 ,  C07D249/04

CPC classification number: A61K31/4192 ,  A61K31/397 ,  C07B59/002 ,  C07B2200/05 ,  C07D205/04 ,  C07D205/06 ,  C07D249/04

Abstract: Pharmaceutical compositions of the invention include novel functionalized 1,3-benzenediols having a disease-modifying action in the treatment of hepatic encephalopathy and related conditions. Pharmaceutical compositions of the invention further include novel neuroprotective agents.

公开(公告)号：EP3089739A1

公开(公告)日：2016-11-09

申请号：EP14876988.8

申请日：2014-12-30

Applicant: Hanmi Pharm. Co., Ltd.

Inventor： CHO, Jung Hyun ,  KIM, Jin Cheul ,  KIM, Yong Il ,  LEE, Seung Jun ,  PARK, Jae Hyun ,  WOO, Jong Soo

IPC: A61K9/16 ,  A61K9/48 ,  A61K9/20 ,  A61K47/38 ,  A61K31/505

CPC classification number: A61K9/2009 ,  A61K9/0053 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/209 ,  A61K9/2095 ,  A61K9/4833 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/397 ,  A61K31/505 ,  A61K2300/00

Abstract: Provided are a solid composite formulation for oral administration, the solid composite formulation including: an ezetimibe granules-part including ezetimibe, said ezetimibe having a particle size distribution wherein the average particle size d
(0.9) for the bottom 90% is about 10 ㎛ or less; and a rosuvastatin mixture-part including rosuvastatin or a pharmaceutically acceptable salt thereof, and a method of preparing the composite formulation.

Abstract translation: 提供一种用于口服给药的固体复合制剂，所述固体复合制剂包括：包含依泽替米贝的依泽替米贝颗粒 - 所述依泽替米贝具有粒度分布，其中底部90％的平均粒径d（0.9）为约10μm，或 减; 和包含瑞舒伐他汀或其药学上可接受的盐的罗苏伐他汀混合物组分，以及制备复合制剂的方法。

公开(公告)号：EP2970119A4

公开(公告)日：2016-10-26

申请号：EP14763846

申请日：2014-03-10

Applicant: MERCK SHARP & DOHME

Inventor： ACTON JOHN J III ,  ANAND RAJAN ,  ARASAPPAN ASHOK ,  DANG QUN ,  SEBHAT IYASSU ,  PU ZHIFA ,  SUZUKI TAKAO

IPC: C07D209/12 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4353 ,  A61K31/495 ,  A61K31/5365 ,  A61P3/10 ,  C07D209/30 ,  C07D403/10 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D471/04 ,  A61K31/366 ,  A61K31/397 ,  A61K31/404 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  C07D209/08 ,  C07D209/12 ,  C07D209/18 ,  C07D209/30 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/10 ,  C07D413/04 ,  C07D413/10 ,  C07D493/04 ,  C07D519/00 ,  A61K2300/00

Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

公开(公告)号：EP3057960A1

公开(公告)日：2016-08-24

申请号：EP14790543.4

申请日：2014-10-16

Applicant: AbbVie Deutschland GmbH & Co. KG ,  AbbVie Inc.

Inventor： AMBERG, Wilhelm ,  POHLKI, Frauke ,  LANGE, Udo ,  WANG, Ying ,  ZHAO, Hongyu ,  LI, Huan-Qiu ,  BREWER, Jason ,  VASUDEVAN, Anil ,  LAO, Yanbin ,  HUTCHINS, Charles W.

IPC: C07D405/14 ,  C07D311/58 ,  C07D405/04 ,  A61K31/352 ,  A61P25/02

CPC classification number: A61K31/501 ,  A61K31/397 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4433 ,  C07D311/58 ,  C07D405/04 ,  C07D405/14

Abstract: The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.

Abstract translation: 本发明涉及药物组合物，其包括寻求氨基苯并二氢吡喃噻喃及氨基-1,2,3,4-四氢喹啉衍生物，以及使用搜索的氨基苯并二氢吡喃噻喃及氨基-1,2,3,4-四氢喹啉衍生物用于治疗目的。 的氨基苯并二氢吡喃噻喃及氨基-1,2,3,4-四氢喹啉衍生物是GlyT1抑制剂。

公开(公告)号：EP3052088A2

公开(公告)日：2016-08-10

申请号：EP14800125.8

申请日：2014-09-30

Applicant: Egis Gyógyszergyár Zrt.

Inventor： FEHÉR, András ,  ZSIGMOUND, Zsolt ,  UJFALUSSY, György ,  TONKA-NAGY, Péter ,  ORBÁN, Ádám ,  AGYAGOS, Mónika

IPC: A61K9/20 ,  A61K9/48 ,  A61K31/397 ,  A61K31/505

CPC classification number: A61K9/4808 ,  A61K9/2013 ,  A61K31/397 ,  A61K31/505 ,  A61K2300/00

Abstract: The present invention is related to a pharmaceutical composition containing rosuvastatin and ezetimibe, wherein the interaction of the active ingredient and excipient is minimized, the active ingredients are present in spatially separated or contacting physical phases and wherein the active ingredient release from the two phases takes place in temporarily separated manner rather than occuring at the same time or begins delayed from one phase compared to the other, other. A further aspect of the present invention is method for decreasing an active ingredient- excipient interaction or interaction between active ingredients in combined pharmaceutical composition containing several solid phases produced by compression, which comprises adjusting the disintegration time of the compressed solid phases different from each other.