公开(公告)号：US10662180B2

公开(公告)日：2020-05-26

申请号：US15882094

申请日：2018-01-29

申请人： H. Lee Moffitt Cancer Center and Research Institute, Inc.

发明人： Harshani R. Lawrence ,  Said M. Sebti ,  Sevil Ozcan

IPC分类号： C07D271/06 ,  C07D417/00 ,  C07D413/00 ,  C07D401/04 ,  A61K31/41 ,  C07D413/04 ,  C07D271/04

摘要： Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e. substitution of one of the hydrogens by methyl) demonstrated chiral discrimination in proteasome CT-L activity inhibition (the S-enantiomer was 35-40 fold more potent than the R-enantiomer).

公开(公告)号：US10111873B1

公开(公告)日：2018-10-30

申请号：US15873450

申请日：2018-01-17

申请人： KING SAUD UNIVERSITY

发明人： Mashooq Ahmad Bhat

IPC分类号： C07D413/00 ,  A61K31/513 ,  A61K31/5375 ,  A61K31/12 ,  A61K31/04 ,  A61K31/497

摘要： A dihydropyrimidinone derivative having a chemical structure according to Formula 1: wherein Z is selected from N and O; X is selected from O and S; and R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl, wherein the substituted aryl or substituted heteroaryl have one or more substituents selected from halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, hydroxyl, alkylthio, alkylamino, heteroaryl, aryloxy, haloaryloxy, arylthio, arylamino, and pharmaceutically acceptable salts thereof.

公开(公告)号：US09991454B2

公开(公告)日：2018-06-05

申请号：US14967202

申请日：2015-12-11

申请人： SAMSUNG DISPLAY CO., LTD. ,  INDUSTRY-ACADEMIC COOPERATION FOUNDATION GYEONGSANG NATIONAL UNIVERSITY

发明人： Heeyeon Kim ,  Soonki Kwon ,  Mikyung Kim ,  Yunhi Kim ,  Jihyun Seo ,  Hyein Jeong

IPC分类号： C09K11/00 ,  H01L51/00 ,  C07F15/00 ,  C09K11/06 ,  C09K11/02 ,  C07D413/14 ,  C07D413/00 ,  H01L51/50

CPC分类号： H01L51/0085 ,  C07D413/00 ,  C07D413/14 ,  C07F15/0033 ,  C09K11/025 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/1029 ,  C09K2211/185 ,  H01L51/5016

摘要： An organic light-emitting device includes a first electrode; a second electrode facing the first electrode; and an organic layer between the first electrode and the second electrode, wherein the organic layer includes an emission layer and at least one organometallic compound of Formula 1. An organic light-emitting device including an organometallic compound of Formula 1 may have low driving voltage, high efficiency, and excellent color purity.

公开(公告)号：US09924721B2

公开(公告)日：2018-03-27

申请号：US14914230

申请日：2014-08-26

申请人： BAYER CROPSCIENCE AKTIENGESELLSCHAFT

发明人： Stefan Hillebrand ,  Matthias Riedrich ,  Sebastian Hoffmann ,  Mark James Ford ,  Joachim Telser ,  Mazen Es-Sayed ,  Guenter Hoemberger ,  Pierre Wasnaire ,  Ulrike Wachendorff-Neumann ,  Tomoki Tsuchiya ,  Valerie Toquin

IPC分类号： C07D401/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D421/00 ,  A01N43/80 ,  A01N43/82 ,  A01N43/78 ,  C07D417/14

CPC分类号： A01N43/80 ,  A01N43/78 ,  A01N43/82 ,  C07D417/14

摘要： Malonic ester derivatives of the formula (I) in which the symbols A1, A2, Y, R10, p, X, R2, G, Q, L2 and R1 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

公开(公告)号：US09790210B2

公开(公告)日：2017-10-17

申请号：US14442604

申请日：2013-11-12

申请人： Array BioPharma Inc.

发明人： Steven Wade Andrews ,  James F. Blake ,  Barbara J. Brandhuber ,  Timothy Kercher ,  Shannon L. Winski

IPC分类号： C07D231/00 ,  C07D403/00 ,  C07D401/00 ,  C07D211/72 ,  C07D413/00 ,  C07D405/12 ,  C07D403/12 ,  C07D401/14 ,  C07D231/40 ,  C07D231/44 ,  C07D401/04 ,  C07D413/12 ,  C07D231/52 ,  C07D401/12 ,  C07D405/04 ,  A61K31/4155

CPC分类号： C07D405/12 ,  A61K31/4155 ,  C07D231/40 ,  C07D231/44 ,  C07D231/52 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/04 ,  C07D413/12

摘要： Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome.

公开(公告)号：US09730936B2

公开(公告)日：2017-08-15

申请号：US14998042

申请日：2015-12-23

申请人： Gilead Sciences, Inc. ,  Institute of Organic Chemistry and Biochemistry of the AS CR, v.v.i.

发明人： Ond{hacek over (r)}ej Baszczy{hacek over (n)}ski ,  Milan Dejmek ,  Yunfeng Eric Hu ,  Petr Jansa ,  Eric Lansdon ,  Richard L. Mackman ,  Petr {hacek over (S)}imon

IPC分类号： A01N43/54 ,  A61K31/517 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D401/12 ,  C07D239/94 ,  A61K45/06 ,  C07D239/84 ,  C07D239/95 ,  C07D403/12

CPC分类号： A61K31/517 ,  A61K45/06 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D401/12 ,  C07D403/12

摘要： Described herein are compounds of Formula (I) and tautomers and pharmaceutical salts thereof, compositions and formulations containing such compounds, and methods of using and making such compounds.

公开(公告)号：US09708309B2

公开(公告)日：2017-07-18

申请号：US14848649

申请日：2015-09-09

申请人： Oryzon Genomics S.A.

发明人： Alberto Ortega Muñoz ,  Matthew Colin Thor Fyfe ,  Marc Martinell Pedemonte ,  Iñigo Tirapu Fernandez De La Cuesta ,  Maria de los Ángeles Estiarte-Martinez

IPC分类号： C07D239/02 ,  C07D413/00 ,  C07D417/00 ,  A61K31/505 ,  A61K31/44 ,  C07D417/12 ,  A61K31/433 ,  A61K31/4245 ,  A61K31/422 ,  C07D213/73 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D253/07 ,  C07D261/14 ,  C07D263/48 ,  C07D271/07 ,  C07D271/113 ,  C07D277/40 ,  C07D285/12 ,  C07D401/12 ,  C07D413/12 ,  C07D285/135 ,  C07D285/08

CPC分类号： C07D417/12 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/433 ,  C07D213/73 ,  C07D237/20 ,  C07D239/42 ,  C07D241/20 ,  C07D253/07 ,  C07D261/14 ,  C07D263/48 ,  C07D271/07 ,  C07D271/113 ,  C07D277/40 ,  C07D285/08 ,  C07D285/12 ,  C07D285/135 ,  C07D401/12 ,  C07D413/12

摘要： The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).

公开(公告)号：US09630947B2

公开(公告)日：2017-04-25

申请号：US14692434

申请日：2015-04-21

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： Masaki Suzuki ,  Kazumi Kondo ,  Muneaki Kurimura ,  Krishna Reddy Valluru ,  Akira Takahashi ,  Takeshi Kuroda ,  Haruka Takahashi ,  Tae Fukushima ,  Shin Miyamura ,  Indranath Ghosh ,  Abhishek Dogra ,  Geraldine Harriman ,  Amy Elder ,  Satoshi Shimizu ,  Kevin J. Hodgetts ,  Jason S. Newcom

IPC分类号： A01N43/54 ,  A61K31/517 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  A61K45/06

CPC分类号： C07D401/04 ,  A61K31/517 ,  A61K45/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04

摘要： Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP), such as those of formula (III), and composition thereof are described herein. Exemplary disorders include schizophrenia and cognitive deficit.

公开(公告)号：US09624174B2

公开(公告)日：2017-04-18

申请号：US14943091

申请日：2015-11-17

申请人： GlaxoSmithKline LLC

发明人： Mui Cheung ,  Raghuram S. Tangirala

IPC分类号： A61K31/50 ,  A61K31/501 ,  A61K31/4965 ,  A01N43/40 ,  A61K31/44 ,  A01N43/78 ,  A61K31/425 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D213/04 ,  C07D277/00 ,  C07D213/72 ,  A61K31/122 ,  C07D237/20 ,  C07D213/74 ,  C07D277/42 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

CPC分类号： C07D213/72 ,  A61K31/122 ,  A61K31/50 ,  C07D213/74 ,  C07D237/20 ,  C07D277/42 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

摘要： Compounds of Formula (I) are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), useful in the treatment of obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as mycocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.

公开(公告)号：US09434693B2

公开(公告)日：2016-09-06

申请号：US13968465

申请日：2013-08-16

申请人： Janssen Pharmaceutica NV

发明人： Mark Wall ,  Nalin Subasinghe ,  Zhihua Sui ,  Christopher Flores

IPC分类号： A61K31/00 ,  A61K31/415 ,  A61K31/445 ,  A61K31/42 ,  C07D401/00 ,  C07D231/00 ,  C07D403/00 ,  C07D403/02 ,  C07D261/00 ,  C07D413/00 ,  C07D231/22 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14

CPC分类号： C07D231/22 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14

摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, ring A, and G are defined herein.