公开(公告)号：EP3150600A4

公开(公告)日：2017-04-05

申请号：EP15799888

申请日：2015-05-27

Applicant: MEDSHINE DISCOVERY INC

Inventor： HE HAIYING ,  ZHOU KAI ,  QIN HUA ,  LI XIAOLIN ,  ZHOU YUEDONG ,  WANG XIAOFEI ,  CHI XUEMEI ,  LI JIAN ,  CHEN SHUHUI

IPC: C07D471/04 ,  A61K31/519 ,  A61K31/527 ,  A61K31/5377 ,  A61P1/16 ,  A61P31/20 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

CPC classification number: C07D513/04 ,  A61K31/519 ,  A61K31/527 ,  A61K31/5377 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D498/04

Abstract: Disclosed is a dihydropyrimido loop derivative as a HBV inhibitor, and in particular relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof.

Abstract translation: 公开了作为HBV抑制剂的二氢嘧啶环衍生物，特别涉及式（I）所示的化合物或其药学上可接受的盐。

公开(公告)号：EP3122730A1

公开(公告)日：2017-02-01

申请号：EP15769715.2

申请日：2015-03-27

Applicant: Calitor Sciences, LLC ,  Sunshine Lake Pharma Co., Ltd.

Inventor： XI, Ning ,  LI, Minxiong ,  LI, Xiaobo ,  DAI, Weilong ,  WANG, Tingjin

IPC: C07D239/24 ,  C07D239/28 ,  C07D239/48 ,  C07D239/49

CPC classification number: C07D403/14 ,  A61K31/506 ,  A61K31/527 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D493/04

Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.

Abstract translation: 本发明提供了用于预防，治疗或减轻蛋白激酶介导的疾病的严重性的新型杂芳基化合物，其药学上可接受的盐和制剂。 本发明还提供包含这些化合物的药学上可接受的组合物和使用该组合物治疗蛋白激酶介导的疾病的方法。

公开(公告)号：EP2989106A4

公开(公告)日：2016-03-02

申请号：EP14787642

申请日：2014-04-22

Applicant: BEIGENE LTD

Inventor： GUO YUNHANG ,  WANG ZHIWEI

IPC: C07D487/04 ,  A61K31/5517 ,  A61P35/00 ,  A61P37/00 ,  C07D487/12

CPC classification number: C07D487/20 ,  A61K31/4188 ,  A61K31/435 ,  A61K31/437 ,  A61K31/438 ,  A61K31/519 ,  A61K31/527 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5517 ,  A61K45/06 ,  C07D471/14 ,  C07D471/20 ,  C07D487/04 ,  C07D487/14 ,  C07D519/00

Abstract: The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.

公开(公告)号：EP2968338A2

公开(公告)日：2016-01-20

申请号：EP14763482.8

申请日：2014-03-17

Applicant: Intra-Cellular Therapies, Inc.

Inventor： WENNOGLE, Lawrence

IPC: A61K31/519

CPC classification number: A61K31/519 ,  A61K31/517 ,  A61K31/527 ,  A61K31/53 ,  G01N33/84 ,  G01N2333/4727 ,  G01N2800/28

Abstract: The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.

Abstract translation: 主题一般涉及治疗和/或预防CNS疾病，病症和/或损伤的方法。 一方面，本主题涉及磷酸二酯酶1（PDE1）的抑制剂作为神经保护剂和/或神经再生剂。 另一方面，本主题涉及处于CNS疾病或病症发展风险中的个体。

公开(公告)号：EP2897961A1

公开(公告)日：2015-07-29

申请号：EP13771007.5

申请日：2013-09-17

Applicant: Novartis AG

Inventor： DILLON, Michael, Patrick ,  LINDVALL, Mika ,  POON, Daniel ,  RAMURTHY, Savithri ,  RAUNIYAR, Vivek ,  SHAFER, Cynthia ,  SUBRAMANIAN, Sharadha ,  TANNER, Huw

IPC: C07D487/04 ,  C07D207/36 ,  A61K31/519 ,  A61P35/00

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  C07D207/36 ,  C07D487/10

Abstract: The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof; as further described herein. The present invention further provides pharmaceutical compositions comprising these compounds, and combinations comprising these compounds combined with or used with a therapeutic co-agent, as well as therapeutic uses of these compounds and compositions. These are useful in the treatment of diseases such as cancer that are associated with activation of ERKl and/or ERK2, and especially for MAPK pathway dependent cancers showing resistance to Raf and/or MEK inhibitory cancer therapeutics

公开(公告)号：EP2516434B1

公开(公告)日：2015-05-27

申请号：EP10800835.0

申请日：2010-12-17

Applicant: Takeda Pharmaceutical Company Limited

Inventor： ARIKAWA, Yasuyoshi ,  JONES, Benjamin ,  LAM, Betty ,  NIE, Zhe ,  SMITH, Christopher ,  TAKAHASHI, Masashi ,  DONG, Qing ,  FEHER, Victoria

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61P7/00 ,  A61P11/00 ,  A61P17/00 ,  A61P19/00 ,  A61P35/00 ,  A61P37/00 ,  A61P29/00

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  C07D471/04 ,  C07D487/10 ,  C07D519/00

公开(公告)号：EP2139475A4

公开(公告)日：2012-03-07

申请号：EP08744515

申请日：2008-03-27

Applicant: OMEROS CORP

Inventor： BERGMANN JOHN E ,  CUTSHALL NEIL S ,  DEMOPULOS GREGORY A ,  FLORIO VINCENT A ,  GAITANARIS GEORGE ,  GRAY PATRICK ,  HOHMANN JOHN ,  ONRUST RENE ,  ZENG HONGKUI

IPC: A61K31/435 ,  A61K31/195 ,  A61K31/433 ,  A61K31/519 ,  A61K31/527

CPC classification number: A61K31/195 ,  A61K31/433 ,  A61K31/519 ,  A61K31/527

公开(公告)号：EP1491212A4

公开(公告)日：2009-10-28

申请号：EP03715566

申请日：2003-03-28

Applicant: MITSUBISHI TANABE PHARMA CORP

Inventor： TESHIMA KOJI ,  MINOGUCHI MASANORI

IPC: A61K31/00 ,  A61K31/454 ,  A61K31/527 ,  A61P25/20 ,  C07D401/04 ,  A61K45/00 ,  C07D235/26 ,  C07D235/28

CPC classification number: C07D401/04 ,  A61K31/00 ,  A61K31/454 ,  A61K31/527

公开(公告)号：EP1699795B1

公开(公告)日：2007-04-25

申请号：EP04804431.7

申请日：2004-12-17

Applicant: Sanofi-Aventis ,  Mitsubishi Pharma Corporation

Inventor： CHEREZE, Nathalie ,  LOCHEAD, Alistair ,  SAADY, Mourad ,  SLOWINSKI, Franck ,  YAICHE, Philippe

IPC: C07D487/04 ,  A61K31/505 ,  A61P25/28

CPC classification number: A61K31/527 ,  A61K31/397 ,  C07D487/04 ,  Y02P20/142

Abstract: The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: (I) wherein: X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom, a C1-4 alkoxy carbonyl group, a C3-6 cycloalkyl carbonyl group, a benzoyl group, a C1-6 alkyl group, the groups being optionally substituted; o and m represent 1 to 2; n represents 0 to 3; p represents 0 to 2; and q represents 0 to 2. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.

Abstract translation: 本发明涉及由式（I）表示的二氢螺环Ä环烷基胺嘧啶酮衍生物或其盐：其中：X表示两个氢原子，硫原子，氧原子或C 1-2烷基和氢 原子; Y表示键，羰基，任选取代的亚甲基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环，该环任选被取代; R2代表苯环或萘环; 所述环任选被取代; R3表示氢原子，C1-6烷基或卤素原子; R4表示氢原子，C1-4烷氧基羰基，任选取代的C 1-6烷基; o和m表示1〜2; n表示0〜3; p表示0〜2; 并且q表示0至2.本发明还涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3的异常活性引起的神经变性疾病 beta，如阿尔茨海默病。

公开(公告)号：EP2902392B1

公开(公告)日：2018-10-17

申请号：EP14199188.5

申请日：2010-12-17

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Arikawa, Yasuyoshi ,  Jones, Benjamin ,  Lam Betty ,  Nie, Zhe ,  Smith, Christopher ,  Takahashi, Masashi ,  Dong, Qing ,  Feher, Victoria

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61P7/00 ,  A61P11/00 ,  A61P17/00 ,  A61P19/00 ,  A61P35/00 ,  A61P37/00 ,  A61P29/00

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  C07D471/04 ,  C07D487/10 ,  C07D519/00

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L 1 , L 2 , R 1 , R 2 , R 3 , and R 4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula I, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.