公开(公告)号：EP4327879A3

公开(公告)日：2024-05-22

申请号：EP23205273.8

申请日：2017-05-31

Applicant: The Trustees of the University of Pennsylvania

Inventor： RIDKY, Todd ,  NATALE, Christopher ,  WINKLER, Jeffrey

IPC: A61K31/473 ,  A61K39/395 ,  A61P35/00

CPC classification number: A61K45/06 ,  C07D221/16 ,  C07D491/08 ,  C07D221/22 ,  C07D405/04 ,  C07D409/04 ,  C07D491/056 ,  A61K39/3955 ,  C07K16/2818 ,  A61K2039/50520130101 ,  C07K2317/7620130101 ,  A61P35/00 ,  A61P35/02 ,  A61K38/15 ,  A61K31/473 ,  A61K2300/0020130101

Abstract: The present invention includes compounds, compositions and methods that are useful for preventing or treating melanoma or any other Myc-expressing cancer in a subject. In certain embodiments, the compounds comprise estrogen (including estrogen derivatives or analogues), a selective GPER agonist and/or another small molecule G-protein coupled receptor (GPCR) agonist that increases cancer cell differentiation.

公开(公告)号：EP3180086A4

公开(公告)日：2017-12-27

申请号：EP15824601

申请日：2015-07-23

Applicant: UNIV NORTHEASTERN ,  UNIV OF FLORIDA RESEARCH FOUNDATION INC

Inventor： THAKUR GANESHSINGH A ,  KULKARNI ABHIJIT R ,  PAPKE ROGER LEE

IPC: C07D221/16 ,  A61K31/473 ,  A61P25/00 ,  A61P25/16 ,  A61P27/02 ,  A61P29/00 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D417/04 ,  C07D491/048 ,  C07D495/04

CPC classification number: C07D495/04 ,  C07D221/16 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D417/04 ,  C07D491/048

Abstract: Compounds are provided which bind to an allosteric site on the mammalian alpha-7 nicotinic acetylcholine receptor (alpha-7 nAChR) and act as positive allosteric modulators with or without allosteric agonist activity. The compounds are useful in diagnosing, preventing, or treating a variety of disorders involving cognition, learning, memory, neurodegeneration, drug addiction, inflammation, chronic pain, and neuropathic pain. The compounds also can be used to enhance memory and learning in normal individuals.

公开(公告)号：EP2838883B1

公开(公告)日：2017-11-08

申请号：EP13716291.3

申请日：2013-04-15

Applicant: F. Hoffmann-La Roche AG

Inventor： AEBI, Johannes ,  AMREIN, Kurt ,  HORNSPERGER, Benoît ,  KUHN, Bernd ,  LIU, Yonfu ,  MAERKI, Hans P. ,  MARTIN, Rainer E. ,  MAYWEG, Alexander V. ,  MOHR, Peter ,  TAN, Xuefei

IPC: C07D217/22 ,  C07D217/24 ,  C07D221/16 ,  A61K31/472 ,  A61K31/435 ,  A61P9/12

CPC classification number: C07D217/14 ,  C07D217/22 ,  C07D217/24 ,  C07D221/04 ,  C07D221/16 ,  C07D405/12

公开(公告)号：EP3044285A1

公开(公告)日：2016-07-20

申请号：EP14752276.7

申请日：2014-08-13

Applicant: Merck Patent GmbH

Inventor： STOESSEL, Philipp ,  KOENEN, Nils

IPC: C09K11/06 ,  H05B33/10

CPC classification number: H01L51/0072 ,  C07D221/16 ,  C07D221/18 ,  C07D221/20 ,  C07D221/22 ,  C07D237/26 ,  C07D471/04 ,  C07D471/14 ,  C07D471/18 ,  C07D471/22 ,  C07D491/048 ,  C07D491/08 ,  C07D491/147 ,  C09B3/14 ,  C09B5/00 ,  C09B5/008 ,  C09B5/028 ,  C09B57/00 ,  C09B57/001 ,  C09K11/02 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/1011 ,  C09K2211/1029 ,  C09K2211/1044 ,  C09K2211/1059 ,  C09K2211/1088 ,  H01L51/0067 ,  H01L51/0071 ,  H01L51/0085 ,  H01L51/0087 ,  H01L51/5012 ,  H01L51/5016 ,  H01L51/5072 ,  H05B33/10 ,  Y02E10/549

Abstract: The invention concerns heterocyclic compounds and electronic devices, in particular organic electroluminescent devices, containing these compounds.

公开(公告)号：EP3043646A1

公开(公告)日：2016-07-20

申请号：EP14839840.7

申请日：2014-08-29

Applicant: Mcquade, D., Tyler ,  Gupton, B., Frank ,  Longstreet, Ashley, R. ,  Opalka, Suzanne, M.

Inventor： Mcquade, D., Tyler ,  Gupton, B., Frank ,  Longstreet, Ashley, R. ,  Opalka, Suzanne, M.

IPC: A01N43/40

CPC classification number: C07D213/85 ,  C07D217/26 ,  C07D221/10 ,  C07D221/16 ,  C07D409/04

Abstract: A method of making a 2-halonicotinonitrile comprises reacting an alkylidene nitrile with a C1-compound in an organic solvent and a dehydrating agent. The dehydrating agent substantially retards dimerization of the alkylidene nitrile during the reaction. The enamine intermediate that forms from the reaction is cyclized using a halide donor to make the 2-halonicotinonitrile.

Abstract translation: 制备2-卤代烟腈的方法包括使亚烷基腈与C1-化合物在有机溶剂和脱水剂中反应。 脱水剂在反应过程中基本上延迟亚烷基腈的二聚。 由反应形成的烯胺中间体使用卤化物供体环化以制备2-卤代烟腈。

公开(公告)号：EP2599774B1

公开(公告)日：2016-07-06

申请号：EP11812552.5

申请日：2011-07-28

Applicant: Astellas Pharma Inc.

Inventor： MATSUSHIMA, Yuji ,  KAMEDA, Minoru ,  HONDA, Shugo ,  SUGANO, Yukihito ,  USUDA, Hiroyuki ,  TERASAKA, Tadashi ,  TERASAWA, Takeshi ,  NISHIGAKI, Fusako

IPC: C07D217/26 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/553 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D237/34 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D495/04

CPC classification number: C07D217/26 ,  C07D217/22 ,  C07D217/24 ,  C07D221/04 ,  C07D221/06 ,  C07D221/16 ,  C07D237/26 ,  C07D237/34 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D495/04

公开(公告)号：EP2757096A9

公开(公告)日：2014-11-26

申请号：EP13197322.4

申请日：2008-09-11

Applicant: GILEAD SCIENCES, INC.

Inventor： Tsantrizos, Youla, S. ,  Bailey, Murray, D. ,  Bilodeau, François ,  Carson, Rebekah, J. ,  Coulombe, René ,  Fader, Lee ,  Halmos, Teddy ,  Kawai, Stephen ,  Landry, Serge ,  Laplante, Steven ,  Morin, Sébastien ,  Parisien, Mathieu ,  Poupart, Marc-André ,  Simoneau, Bruno

IPC: C07D215/14 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/538 ,  A61P31/18 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D491/06

CPC classification number: C07D215/14 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/538 ,  A61K31/5383 ,  C07D215/18 ,  C07D221/16 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D491/06 ,  C07D498/06

Abstract: Compounds of formula I:

wherein R 4 , R 6 and R 7 are defined herein, are useful as inhibitors of HIV replication.

公开(公告)号：EP2801569A1

公开(公告)日：2014-11-12

申请号：EP13382170.2

申请日：2013-05-09

Applicant: Ikerchem, S.L. ,  Universidad del Pais Vasco

Inventor： Cossio Mora, Fernando Pedro ,  Vara Salazar, Yosu Ion ,  Masdeu Margalef, María del Carmen ,  Alcalà Caffarena, María Remedios ,  Villafruela Cáneva, Sergio ,  Otaegui Ansa, Dorleta ,  Aldaba Arévalo, Eneko ,  Zubia Olascoaga, Aizpea ,  San Sebastián Larzabal, Eider

IPC: C07D219/10 ,  A61K31/435 ,  C07D221/06 ,  C07D471/04 ,  A61P19/00

CPC classification number: C07D471/04 ,  C07D219/04 ,  C07D219/10 ,  C07D221/06 ,  C07D221/16 ,  C07D401/12

Abstract: The present invention refers to compounds of formula (I):

as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or chemoprevention of cancer hematological malignancy, proliferative diseases, neurological disorders and immunological disorders.

Abstract translation: 本发明涉及化学式（I）的化合物：以及一种用于其制备方法，药物组合物包含相同的，及其用于癌症恶性血液疾病，增殖性疾病，神经系统疾病及免疫学的治疗和/或化学预防 障碍。

公开(公告)号：EP2702042A1

公开(公告)日：2014-03-05

申请号：EP12723982.0

申请日：2012-04-27

Applicant: Bristol-Myers Squibb Company

Inventor： ROBL, Jeffrey A. ,  LI, Jun ,  KENNEDY, Lawrence J. ,  WALKER, Steven J. ,  WANG, Haixia ,  WASHBURN, William N. ,  AHMAD, Saleem ,  NGU, Khehyong

IPC: C07D215/08 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  A61K31/4709 ,  A61K31/553 ,  A61K31/554 ,  A61P3/00 ,  A61P9/00 ,  C07D401/14 ,  C07D413/14

CPC classification number: C07D401/04 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/473 ,  A61K31/4747 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61K31/675 ,  A61K45/06 ,  C07D215/08 ,  C07D221/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07F9/60

Abstract: Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R
3 , R
4 , R
4a , R
5a , R
5b , R
5c , R
5d , R
5e , R
6a , R
6b , and R
6c are defined herein, are provided which are TGR5 G protein-coupled receptor modulators. TGR5 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring TGR5 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the TGR5 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.

公开(公告)号：EP2496559A1

公开(公告)日：2012-09-12

申请号：EP10782081.3

申请日：2010-11-05

Applicant: Vitae Pharmaceuticals, Inc. ,  Boehringer Ingelheim International GmbH

Inventor： ECKHARDT, Matthias ,  PETERS, Stefan ,  NAR, Herbert ,  HIMMELSBACH, Frank ,  ZHUANG, Linghang

IPC: C07D221/10 ,  C07D401/06 ,  C07D401/12 ,  C07D417/06 ,  C07D471/04 ,  A61K31/473 ,  A61K31/497 ,  A61K31/498 ,  A61K31/5377 ,  A61P3/00 ,  C07D401/14 ,  C07D405/14 ,  C07D498/04

CPC classification number: C07D221/10 ,  C07D221/06 ,  C07D221/16 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D417/06 ,  C07D471/04 ,  C07D498/04

Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11beta-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, in particular diabetes type 2, obesity, and dyslipidemia.

Abstract translation: 本发明涉及由式I定义的化合物，其中变量R1，R2，R3，R4和m如权利要求1中所定义，具有有价值的药理学活性。 特别地，这些化合物是11β-羟基类固醇脱氢酶（HSD）1的抑制剂，因此适用于治疗和预防可受该酶抑制影响的疾病，例如代谢疾病，特别是2型糖尿病，肥胖症和血脂异常 。