[go: up one dir, main page]

TW201613925A - Imidazopyrazines as LSD1 inhibitors - Google Patents

Imidazopyrazines as LSD1 inhibitors

Info

Publication number
TW201613925A
TW201613925A TW104122392A TW104122392A TW201613925A TW 201613925 A TW201613925 A TW 201613925A TW 104122392 A TW104122392 A TW 104122392A TW 104122392 A TW104122392 A TW 104122392A TW 201613925 A TW201613925 A TW 201613925A
Authority
TW
Taiwan
Prior art keywords
imidazopyrazines
lsd1 inhibitors
lsd1
inhibitors
imidazo
Prior art date
Application number
TW104122392A
Other languages
English (en)
Inventor
Liang-Xing Wu
Chun-Hong He
Liang Lu
xiao-zhao Wang
Wenqing Yao
Colin Feng-Lei Zhang
Jincong Zhuo
Joel R Courter
jing-wei Li
Ya-Ping Sun
Original Assignee
Incyte Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of TW201613925A publication Critical patent/TW201613925A/zh

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
TW104122392A 2014-07-10 2015-07-09 Imidazopyrazines as LSD1 inhibitors TW201613925A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462022913P 2014-07-10 2014-07-10

Publications (1)

Publication Number Publication Date
TW201613925A true TW201613925A (en) 2016-04-16

Family

ID=53682879

Family Applications (1)

Application Number Title Priority Date Filing Date
TW104122392A TW201613925A (en) 2014-07-10 2015-07-09 Imidazopyrazines as LSD1 inhibitors

Country Status (4)

Country Link
US (3) US9695180B2 (zh)
AR (1) AR101174A1 (zh)
TW (1) TW201613925A (zh)
WO (1) WO2016007736A1 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116836167A (zh) * 2022-03-25 2023-10-03 腾讯科技(深圳)有限公司 咪唑并[1,2-a]吡嗪或吡唑并[1,5-a]嘧啶衍生物及其用途

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
RS59559B1 (sr) 2014-02-13 2019-12-31 Incyte Corp Ciklopropilamini kao lsd1 inhibitori
PE20161384A1 (es) 2014-02-13 2016-12-28 Incyte Corp Ciclopropilaminas como inhibidores de lsd 1
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
KR102662215B1 (ko) 2014-11-06 2024-05-02 비알 - 알&디 인베스트먼츠, 에스.에이. 치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도
AU2015342883B2 (en) 2014-11-06 2020-07-02 Bial - R&D Investments, S.A. Substituted pyrrolo(1,2-a)pyrimidines and their use in the treatment of medical disorders
EP3215510B1 (en) 2014-11-06 2023-06-07 Bial-R&D Investments, S.A. Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders
TWI714567B (zh) 2015-04-03 2021-01-01 美商英塞特公司 作為lsd1抑制劑之雜環化合物
CN107849611A (zh) 2015-06-12 2018-03-27 奥瑞泽恩基因组学股份有限公司 与lsd1抑制剂相关的生物标志物及其用途
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
HUE070538T2 (hu) 2015-08-12 2025-06-28 Incyte Holdings Corp Egy LSD1 inhibitor sói
CN107174584B (zh) * 2016-03-12 2020-09-01 福建金乐医药科技有限公司 含哌嗪结构化合物在制备lsd1抑制剂中的应用
CN109195593A (zh) 2016-03-15 2019-01-11 奥莱松基因组股份有限公司 用于治疗实体瘤的lsd1抑制剂的组合
US11034991B2 (en) 2016-03-16 2021-06-15 Oryzon Genomics S.A. Methods to determine KDM1A target engagement and chemoprobes useful therefor
CA3020305A1 (en) 2016-04-06 2017-10-12 Lysosomal Therapeutics Inc. Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
CN109311887B (zh) 2016-04-06 2022-09-13 Bial研发投资股份有限公司 吡唑并[1,5-a]嘧啶基甲酰胺化合物以及它们在治疗医学病症中的用途
EP3440081A4 (en) 2016-04-06 2019-09-18 Lysosomal Therapeutics Inc. PYRROLO [1,2-A] PYRIMIDINYL-CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDER
PE20190377A1 (es) 2016-04-22 2019-03-08 Incyte Corp Formulaciones de un inhibidor de lsd 1
WO2017192931A1 (en) * 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
CA3022670A1 (en) 2016-05-05 2017-11-09 Lysosomal Therapeutics Inc. Substituted imidazo[1,2-b]pyridazines, substituted imidazo[1,5-b]pyridazines, related compounds, and their use in the treatment of medical disorders
EP3535420A1 (en) 2016-11-03 2019-09-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
US20200069677A1 (en) 2016-12-09 2020-03-05 Constellation Pharmaceuticals, Inc. Markers for personalized cancer treatment with lsd1 inhibitors
AU2018269947B2 (en) * 2017-05-15 2021-10-14 The Regents Of The University Of Michigan Pyrrolo(2,3-c)pyridines and related analogs as LSD-1 inhibitors
WO2019002606A1 (en) * 2017-06-30 2019-01-03 Selvita S.A. ADENOSINE A2A RECEPTOR 5,6-BICYCLO-IMIDAZO [1,2-A] PYRAZINE MODULATORS
BR112020000827A2 (pt) 2017-08-03 2020-07-21 Oryzon Genomics, S.A. métodos de tratamento de alterações de comportamento
TWI794294B (zh) * 2017-09-13 2023-03-01 南韓商韓美藥品股份有限公司 吡唑衍生化合物及其用途
WO2019068326A1 (en) 2017-10-05 2019-04-11 Université D'aix-Marseille INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES
US11685782B2 (en) 2017-10-23 2023-06-27 Children's Medical Center Corporation Methods of treating cancer using LSD1 inhibitors in combination with immunotherapy
CN108220422B (zh) * 2018-01-05 2020-10-16 武汉惠康达科技有限公司 组蛋白去甲基化酶在筛选治疗脂肪肝及其相关疾病药物中的应用
WO2019222069A1 (en) 2018-05-15 2019-11-21 The Regents Of The University Of Michigan Imidazo[4,5-c]pyridine compounds as lsd-1 inhibitors
WO2020047198A1 (en) 2018-08-31 2020-03-05 Incyte Corporation Salts of an lsd1 inhibitor and processes for preparing the same
US12479845B2 (en) * 2019-02-01 2025-11-25 Hanmi Pharm. Co., Ltd. Imidazopyridine derivative compounds and use of same
SG11202109159VA (en) 2019-03-20 2021-10-28 Oryzon Genomics Sa Methods of treating borderline personality disorder
ES3053813T3 (en) 2019-03-20 2026-01-26 Oryzon Genomics Sa Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat
EP3994280A1 (en) 2019-07-05 2022-05-11 Oryzon Genomics, S.A. Biomarkers and methods for personalized treatment of small cell lung cancer using kdm1a inhibitors
WO2021094208A1 (en) 2019-11-12 2021-05-20 Bayer Aktiengesellschaft Substituted imidazo pyrimidine ep3 antagonists
EP3964204A1 (en) 2020-09-08 2022-03-09 Université d'Aix-Marseille Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues
EP4319732A1 (en) 2021-04-08 2024-02-14 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors for treating myeloid cancers
GB202115017D0 (en) 2021-10-20 2021-12-01 Univ London Queen Mary Sequential treatments and biomarkers to reverse resistance to kinase inhibitors
WO2023067058A1 (en) 2021-10-20 2023-04-27 Queen Mary University Of London Sequential treatments and biomarkers to reverse resistance to kinase inhibitors
CN119546292A (zh) 2022-05-09 2025-02-28 奥莱松基因组股份有限公司 使用lsd1抑制剂治疗恶性周围神经鞘瘤(mpnst)的方法
JP2025516648A (ja) 2022-05-09 2025-05-30 オリゾン・ゲノミクス・ソシエダッド・アノニマ Lsd1阻害薬を用いるnf1変異腫瘍の治療法
EP4622635A1 (en) 2022-11-24 2025-10-01 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer

Family Cites Families (265)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4537889A (en) 1982-12-27 1985-08-27 Eli Lilly And Company Inotropic agents
US4614810A (en) 1984-09-24 1986-09-30 Pennwalt Corporation 4,5-dihydro-4-oxo-2-[(2-trans-phenylcyclopropyl)amino]-3-furancarboxylic acids and derivatives thereof
US4625040A (en) 1984-09-24 1986-11-25 Pennwalt Corporation N-(phenyl) or N-(phenylcyclopropyl)-2,5-dihydro-2-oxo-4[(substituted phenyl)amino]-3-furancarboxamide derivatives
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
AU622330B2 (en) 1989-06-23 1992-04-02 Takeda Chemical Industries Ltd. Condensed heterocyclic compounds having a nitrogen atom in the bridgehead for use as fungicides
IL96432A0 (en) 1989-11-30 1991-08-16 Schering Ag Pesticidal compositions containing pyridine derivatives and novel pyridine derivatives
FR2662163A1 (fr) 1990-05-16 1991-11-22 Lipha Nouvelles 8-amino-1,2,4-triazolo(4,3-a) pyrazines, procedes de preparation et medicaments les contenant.
DE69323883T2 (de) 1992-06-17 1999-07-22 Pharmacia & Upjohn Co., Kalamazoo, Mich. Pyrridino-, pyrrolidino- und azepino-substituierte oxime als antiatherosklerosemittel und antihypercholesterolemiemittel
DE4327027A1 (de) 1993-02-15 1994-08-18 Bayer Ag Imidazoazine
FR2711993B1 (fr) * 1993-11-05 1995-12-01 Rhone Poulenc Rorer Sa Médicaments contenant des dérivés de 7H-imidazol[1,2-a]pyrazine-8-one, les nouveaux composés et leur préparation.
US6451796B1 (en) 1997-11-11 2002-09-17 Ono Pharmaceutical Co., Ltd. Fused pyrazine compounds
JP2000319278A (ja) 1999-05-11 2000-11-21 Ono Pharmaceut Co Ltd 縮合ピラジン化合物およびその化合物を有効成分とする薬剤
JP2000319277A (ja) 1999-05-11 2000-11-21 Ono Pharmaceut Co Ltd 縮合ピラジン化合物およびその化合物を有効成分とする薬剤
JP4032566B2 (ja) 1999-06-21 2008-01-16 東レ株式会社 発光素子
JP2001000687A (ja) 1999-06-23 2001-01-09 Ace Denken:Kk 遊技機
JP4041624B2 (ja) 1999-07-21 2008-01-30 三井化学株式会社 有機電界発光素子
JP2001057292A (ja) 1999-08-20 2001-02-27 Toray Ind Inc 発光素子
SE9903611D0 (sv) 1999-10-06 1999-10-06 Astra Ab Novel compounds III
DE19948434A1 (de) 1999-10-08 2001-06-07 Gruenenthal Gmbh Substanzbibliothek enthaltend bicyclische Imidazo-5-amine und/oder bicyclische Imidazo-3-amine
JP4409680B2 (ja) 1999-10-18 2010-02-03 株式会社ヤクルト本社 三環性縮合イミダゾール誘導体
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
DE60112272T2 (de) 2000-04-27 2006-05-24 Astellas Pharma Inc. Imidazopyridin-derivate
AU2002215608B2 (en) 2000-06-28 2004-12-09 Smithkline Beecham P.L.C. Wet milling process
US6589952B2 (en) 2000-07-14 2003-07-08 Bristol-Myers Squibb Pharma Company Imidazo[1,2-a]pyrazines for the treatment of neurological disorders
DE10050663A1 (de) 2000-10-13 2002-04-18 Gruenenthal Gmbh Verwendung von substituierten Imidazo[1,2-a]pyridin-, -pyrimidin- und pyrazin-3-yl-amin-Derivaten zur Herstellung von Medikamenten zur NOS-Inhibierung
WO2002034748A1 (fr) 2000-10-24 2002-05-02 Sankyo Company, Limited Derives d'imidazopyridine
JP2002205992A (ja) 2000-11-08 2002-07-23 Takeda Chem Ind Ltd 二環式トリアゾロン誘導体およびそれを含有する除草剤
ATE310740T1 (de) 2000-11-10 2005-12-15 Merck Sharp & Dohme Imidazotriazin-derivate als liganden für gaba- rezeptoren
EP1343785A2 (de) 2000-12-13 2003-09-17 Basf Aktiengesellschaft Verwendung von substituierten imidazoazinen, neue imidazoazine, verfahren zu deren herstellung, sowie sie enthaltende mittel
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
EP1377549A1 (en) 2001-03-12 2004-01-07 Millennium Pharmaceuticals, Inc. Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
AR035543A1 (es) 2001-06-26 2004-06-16 Japan Tobacco Inc Agente terapeutico para la hepatitis c que comprende un compuesto de anillo condensado, compuesto de anillo condensado, composicion farmaceutica que lo comprende, compuestos de benzimidazol, tiazol y bifenilo utiles como intermediarios para producir dichos compuestos, uso del compuesto de anillo con
IL159811A0 (en) 2001-07-13 2004-06-20 Neurogen Corp Heteroaryl substituted fused bicyclic heteroaryl compounds as gabaa receptor ligands
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
US20050113283A1 (en) 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 receptor
EP1513522A2 (en) 2002-01-18 2005-03-16 Sri International Methods of treating conditions associated with an edg receptor
WO2004017950A2 (en) 2002-08-22 2004-03-04 Piramed Limited Phosphadidylinositol 3,5-biphosphate inhibitors as anti-viral agents
UA80296C2 (en) 2002-09-06 2007-09-10 Biogen Inc Imidazolopyridines and methods of making and using the same
AU2003297431A1 (en) 2002-12-20 2004-07-22 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
WO2004072080A1 (en) 2003-02-10 2004-08-26 Cellular Genomics, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of hsp90 complex activity
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
KR101078505B1 (ko) 2003-03-14 2011-10-31 오노 야꾸힝 고교 가부시키가이샤 질소 함유 복소환 유도체 및 이들을 유효 성분으로 하는약제
JP2006522750A (ja) 2003-04-11 2006-10-05 ノボ ノルディスク アクティーゼルスカブ 代謝性症候群ならびに関連の疾患および障害を治療するために、11β−ヒドロキシステロイドデヒドロゲナーゼ1型阻害剤および抗高血圧剤を使用する併用療法
EP1615647B1 (en) 2003-04-11 2010-01-20 High Point Pharmaceuticals, LLC Pharmaceutical use of fused 1,2,4-triazoles
AU2004233828B2 (en) 2003-04-24 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
SE0301653D0 (sv) 2003-06-05 2003-06-05 Astrazeneca Ab Novel compounds
BRPI0412689A (pt) 2003-07-14 2006-10-03 Arena Pharm Inc derivados de heteroarila e arila fundida como moduladores de metabolismo e a profilaxia e tratamento de distúrbios relacionados a ele
US7538120B2 (en) 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
ES2385219T3 (es) 2003-09-12 2012-07-19 Merck Serono Sa Derivados de sulfonamida para el tratamiento de diabetes
JP2005089352A (ja) 2003-09-16 2005-04-07 Kissei Pharmaceut Co Ltd 新規なイミダゾ[1,5−a]ピラジン誘導体、それを含有する医薬組成物およびそれらの用途
ATE369370T1 (de) 2003-10-10 2007-08-15 Pfizer Prod Inc Substituierte 2h-(1,2,4)triazolo(4,3-a)pyrazine als gsk-3-inhibitoren
US7419978B2 (en) 2003-10-22 2008-09-02 Bristol-Myers Squibb Company Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors
US7714009B2 (en) 2003-10-31 2010-05-11 Takeda Pharmaceutical Company Limited Nitrogen-containing fused heterocyclic compounds
US20080249154A1 (en) 2003-12-26 2008-10-09 Ono Pharmaceutical Co., Ltd. Preventive and/or Therapeutic Agent For Disease In Which Mitochondrial Benzodiazephine Receptor Participates
JPWO2005077948A1 (ja) 2004-02-16 2008-01-10 第一製薬株式会社 抗真菌作用複素環化合物
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
WO2006015263A2 (en) 2004-07-29 2006-02-09 Threshold Pharmaceuticals, Inc. Lonidamine analogs
WO2006018727A2 (en) 2004-08-18 2006-02-23 Pharmacia & Upjohn Company Llc Triazolopyridine compounds useful for the treatment of inflammation
EP1799680A2 (en) 2004-10-07 2007-06-27 Warner-Lambert Company LLC Triazolopyridine derivatives as antibacterial agents
WO2006057946A2 (en) 2004-11-22 2006-06-01 Threshold Pharmaceuticals, Inc. Tubulin binding anti cancer agents and prodrugs thereof
AU2005311451A1 (en) 2004-12-01 2006-06-08 Merck Serono Sa [1,2,4]triazolo[4,3-a]pyridine derivatives for the treatment of hyperproliferative diseases
WO2006073938A2 (en) 2004-12-30 2006-07-13 East Carolina University Method for the synthesis of 3-substituted indolizine and benzoindolizine compounds
US7456289B2 (en) 2004-12-31 2008-11-25 National Health Research Institutes Anti-tumor compounds
MX2007010139A (es) 2005-02-22 2007-09-27 Pfizer Derivados de oxiindol como agonista del receptor 5ht4.
AU2006236387A1 (en) 2005-04-18 2006-10-26 Neurogen Corporation Subtituted heteroaryl CB1 antagonists
US7572807B2 (en) 2005-06-09 2009-08-11 Bristol-Myers Squibb Company Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
US7579360B2 (en) 2005-06-09 2009-08-25 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
CA2611391A1 (en) 2005-06-09 2006-12-14 Oncalis Ag Angiogenesis inhibitors
TW200726765A (en) 2005-06-17 2007-07-16 Bristol Myers Squibb Co Triazolopyridine cannabinoid receptor 1 antagonists
US7452892B2 (en) 2005-06-17 2008-11-18 Bristol-Myers Squibb Company Triazolopyrimidine cannabinoid receptor 1 antagonists
US7632837B2 (en) 2005-06-17 2009-12-15 Bristol-Myers Squibb Company Bicyclic heterocycles as cannabinoid-1 receptor modulators
TW200800213A (en) 2005-09-02 2008-01-01 Abbott Lab Novel imidazo based heterocycles
KR20080074963A (ko) 2005-11-10 2008-08-13 쉐링 코포레이션 단백질 키나제 억제제로서의 이미다조피라진
US7399769B2 (en) 2005-12-27 2008-07-15 Hoffmann-La Roche Inc. Aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives
WO2007074491A1 (en) 2005-12-28 2007-07-05 Universita Degli Studi Di Siena HETEROTRICYCLIC AMIDE DERIVATIVES AS NEUROKININ-l (NKl) RECEPTOR LIGANDS
PE20070978A1 (es) 2006-02-14 2007-11-15 Novartis Ag COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks)
WO2007113226A1 (en) 2006-03-31 2007-10-11 Novartis Ag Organic compounds
MX2008015747A (es) 2006-06-06 2008-12-19 Schering Corp Imidazopirazinas como inhibidores de la proteina quinasa.
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
JP2009541323A (ja) 2006-06-22 2009-11-26 マリンクロット インコーポレイテッド 拡張された共役を有するピラジン誘導体およびその使用
ES2456042T3 (es) 2006-06-22 2014-04-21 Medibeacon, LLC Derivados de pirazina y usos de los mismos en la monitorización renal
AR061664A1 (es) 2006-06-29 2008-09-10 Schering Corp Derivados de himbacina como antagonistas del receptor de trombina biciclicos y triciclicos sustituidos. composiciones farmaceuticas.
WO2008005423A1 (en) 2006-07-03 2008-01-10 Cambrex Charles City, Inc. Improved method of making sufentanil
US7501438B2 (en) 2006-07-07 2009-03-10 Forest Laboratories Holdings Limited Pyridoimidazole derivatives
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
WO2008011560A2 (en) 2006-07-20 2008-01-24 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
WO2008027812A2 (en) 2006-08-28 2008-03-06 Forest Laboratories Holdings Limited Imidazopyridine and imidazopyrimidine derivatives
DE102006041292A1 (de) 2006-09-01 2008-03-06 Henkel Kgaa Wasserstoffperoxid-Aktivierung mit N-Heterocyclen
WO2008037607A1 (de) 2006-09-25 2008-04-03 Basf Se Carbonylgruppen-enthaltende heterocyclische verbindungen und deren verwendung zur bekämpfung von phytopathogenen pilzen
EP2086973B1 (en) 2006-10-11 2012-01-25 Amgen Inc., Imidazo- and triazolo-pyridine compounds and methods of use therof
WO2008056176A1 (en) 2006-11-10 2008-05-15 Scottish Biomedical Limited Pyrazolopyrimidines as phosphodiesterase inhibitors
SI3034075T1 (sl) 2006-11-22 2018-12-31 Incyte Holdings Corporation Imidazotriazini in imidazopirimidini kot inhibitorji kinaze
EP2086540B8 (en) 2006-12-01 2011-03-02 Galapagos N.V. Triazolopyridine compounds useful for the treatment of degenerative & inflammatory diseases
EP2118101B1 (en) 2007-03-09 2012-09-26 Probiodrug AG Imidazo [1,5-a] pyridine derivatives as inhibitors of glutaminyl cyclase
DE102007012645A1 (de) 2007-03-16 2008-09-18 Bayer Healthcare Ag Substituierte Imidazo- und Triazolopyrimidine
EP1972628A1 (en) 2007-03-21 2008-09-24 Schwarz Pharma Ag Indolizines and aza-analog derivatives thereof as CNS active compounds
ATE540037T1 (de) 2007-04-16 2012-01-15 Leo Pharma As Triazolopyridine als phosphodiesterasehemmer zur behandlung von hautkrankheiten
CN101687873A (zh) 2007-04-17 2010-03-31 百时美施贵宝公司 具有稠合杂环的11β-羟基类固醇Ⅰ型脱氢酶抑制剂
US20110206607A1 (en) 2007-05-10 2011-08-25 Roger Olsson Imidazol (1,2-a)pyridines and related compounds with activity at cannabinoid cb2 receptors
EP2168579B1 (en) 2007-05-21 2017-10-11 Toray Industries, Inc. Oral preparation comprising specific organic acid, and method for improvement in dissolution property and chemical stability of oral preparation
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
MX2009013213A (es) 2007-06-08 2010-03-30 Abbott Lab Indazoles 5-sustituidos 5-heteroarilo como inhibidores de cinasa.
WO2008156614A2 (en) 2007-06-14 2008-12-24 Schering Corporation Imidazopyrazines as protein kinase inhibitors
CL2008001839A1 (es) 2007-06-21 2009-01-16 Incyte Holdings Corp Compuestos derivados de 2,7-diazaespirociclos, inhibidores de 11-beta hidroxil esteroide deshidrogenasa tipo 1; composicion farmaceutica que comprende a dichos compuestos; utiles para tratar la obesidad, diabetes, intolerancia a la glucosa, diabetes tipo ii, entre otras enfermedades.
US8053574B2 (en) 2007-07-18 2011-11-08 Novartis Ag Organic compounds
CN101808666A (zh) 2007-07-31 2010-08-18 先灵公司 作为抗癌治疗的抗有丝分裂剂和激光激酶抑制剂组合
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
BRPI0814939A2 (pt) 2007-08-10 2015-01-27 Glaxosmithkline Llc Entidade química, composição farmacêutica, e, método para tratar uma infecção viral em um mamífero.
FR2920090A1 (fr) 2007-08-24 2009-02-27 Oreal Composition tinctoriale comprenant une base d'oxydation aminopyrazolopyridine particuliere, un coupleur et un tensioactif particulier.
FR2920091A1 (fr) 2007-08-24 2009-02-27 Oreal Composition tinctoriale comprenant une base d'oxydation aminopyrazolopyridine, un coupleur et un polyol particulier.
US8119658B2 (en) 2007-10-01 2012-02-21 Bristol-Myers Squibb Company Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
GB0719803D0 (en) 2007-10-10 2007-11-21 Cancer Rec Tech Ltd Therapeutic compounds and their use
TWI453021B (zh) 2007-10-11 2014-09-21 Astrazeneca Ab 新穎蛋白質激酶b抑制劑
NZ600355A (en) 2007-10-12 2013-02-22 Novartis Ag Compositions comprising sphingosine 1 phosphate (S1P) receptor modulators
DK2231662T3 (da) 2007-12-19 2011-08-29 Genentech Inc 8-Anilinoimidazopyridiner og deres anvendelse som anticancer- og/eller antiinflammatoriske midler
CL2008003798A1 (es) 2007-12-19 2009-10-09 Amgen Inc Compuestos derivados de heterobiciclos aromaticos sustituidos, inhibidores de pi3 quinasa; composicion farmaceutica; utiles en el tratamiento de cancer, melanomas, glioblastomas, entre otras enfermedades.
HUE029767T2 (en) 2008-03-11 2017-04-28 Incyte Holdings Corp JAK inhibitor azetidine and cyclobutane derivatives
US8507501B2 (en) 2008-03-13 2013-08-13 The Brigham And Women's Hospital, Inc. Inhibitors of the BMP signaling pathway
WO2009128520A1 (ja) 2008-04-18 2009-10-22 塩野義製薬株式会社 P13k阻害活性を有する複素環化合物
DE102008023801A1 (de) 2008-05-15 2009-11-19 Bayer Schering Pharma Aktiengesellschaft Substituierte Imidazo- und Triazolopyrimidine, Imidazo- und Pyrazolopyrazine und Imidazotriazine
US8349210B2 (en) 2008-06-27 2013-01-08 Transitions Optical, Inc. Mesogenic stabilizers
WO2010010189A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
WO2010010184A1 (en) 2008-07-25 2010-01-28 Galapagos Nv [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors
WO2010010187A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
UY32049A (es) 2008-08-14 2010-03-26 Takeda Pharmaceutical Inhibidores de cmet
WO2010033906A2 (en) 2008-09-19 2010-03-25 President And Fellows Of Harvard College Efficient induction of pluripotent stem cells using small molecule compounds
JP2010070503A (ja) 2008-09-19 2010-04-02 Daiichi Sankyo Co Ltd 抗真菌作用2−アミノトリアゾロピリジン誘導体
JP5731978B2 (ja) 2008-09-26 2015-06-10 インテリカイン, エルエルシー 複素環キナーゼ阻害剤
WO2010043721A1 (en) 2008-10-17 2010-04-22 Oryzon Genomics, S.A. Oxidase inhibitors and their use
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
WO2010064020A1 (en) 2008-12-04 2010-06-10 Proximagen Ltd. Imidazopyridine compounds
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
EP2389362B1 (en) 2009-01-21 2019-12-11 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
CA2750517A1 (en) 2009-02-04 2010-08-12 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5667085B2 (ja) 2009-02-13 2015-02-12 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH Aktインヒビターとしての融合されたピリミジン
KR20100101054A (ko) 2009-03-07 2010-09-16 주식회사 메디젠텍 세포핵에서 세포질로의 gsk3의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물
TW201035078A (en) 2009-03-20 2010-10-01 Incyte Corp Substituted heterocyclic compounds
HRP20130846T1 (hr) 2009-03-31 2013-11-22 Kissei Pharmaceutical Co., Ltd. Derivati indolizina i njihova uporaba u medicinske svrhe
CA2756759C (en) 2009-04-16 2017-11-07 Joaquin Pastor Fernandez Imidazopyrazines for use as kinase inhibitors
TWI461426B (zh) 2009-05-27 2014-11-21 Merck Sharp & Dohme (二氫)咪唑並異〔5,1-a〕喹啉類
KR20120035183A (ko) 2009-06-10 2012-04-13 선오비온 파마슈티컬스 인코포레이티드 히스타민 h3 역 작용제 및 길항제, 및 이의 사용 방법
JP5732453B2 (ja) 2009-06-25 2015-06-10 アルカーメス ファーマ アイルランド リミテッド Nh酸性化合物のプロドラッグ
IN2012DN01961A (zh) 2009-08-17 2015-08-21 Intellikine Llc
AU2010284221B2 (en) 2009-08-18 2016-09-22 Casero, Robert A (bis) urea and (bis) thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders
EP2473495A1 (en) 2009-09-18 2012-07-11 Almac Discovery Limited Pharmaceutical compounds
CN102639496B (zh) 2009-09-25 2014-10-29 奥瑞泽恩基因组学股份有限公司 赖氨酸特异性脱甲基酶-1抑制剂及其应用
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
US8541404B2 (en) 2009-11-09 2013-09-24 Elexopharm Gmbh Inhibitors of the human aldosterone synthase CYP11B2
CA2787714C (en) 2010-01-22 2019-04-09 Joaquin Pastor Fernandez Inhibitors of pi3 kinase
US20130085133A1 (en) 2010-02-08 2013-04-04 Sourthern Research Institute Office of Commercialization and Intellectual Prop. Anti-viral treatment and assay to screenfor anti-viral agent
WO2011106105A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
US9186337B2 (en) 2010-02-24 2015-11-17 Oryzon Genomics S.A. Lysine demethylase inhibitors for diseases and disorders associated with Hepadnaviridae
TW201200518A (en) 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
WO2011113862A1 (en) 2010-03-18 2011-09-22 Bayer Pharma Aktiengesellschaft Imidazopyrazines
EP2547678B1 (en) 2010-03-18 2016-03-16 Institut Pasteur Korea Anti-infective compounds
SMT201700282T1 (it) 2010-04-02 2017-07-18 Ogeda Sa Nuovi composti antagonisti selettivi del recetiore nk-3, composizione farmaceutica e metodi per l'uso in disturbi mediati dai recettori nk-3
CN102947265B (zh) 2010-04-19 2015-07-29 奥瑞泽恩基因组学股份有限公司 赖氨酸特异性脱甲基酶-1抑制剂及其应用
ES2564352T3 (es) 2010-04-20 2016-03-22 Università Degli Studi Di Roma "La Sapienza" Derivados de tranilcipromina como inhibidores de la histona-desmetilasa LSD1 y/o LSD2
WO2011143365A1 (en) 2010-05-13 2011-11-17 Amgen Inc. Nitrogen heterocyclic compounds useful as pde10 inhibitors
US20130131057A1 (en) 2010-05-13 2013-05-23 Centro Nacional De Investigaciones Oncologicas (Cnio New bicyclic compounds as pi3-k and mtor inhibitors
CN102295642B (zh) 2010-06-25 2016-04-06 中国人民解放军军事医学科学院毒物药物研究所 2-芳基咪唑并[1,2-a]吡啶-3-乙酰胺衍生物、其制备方法及用途
NZ604478A (en) 2010-07-02 2014-12-24 Gilead Sciences Inc Fused heterocyclic compounds as ion channel modulators
EP2593451B1 (en) 2010-07-12 2015-08-19 Bayer Intellectual Property GmbH Substituted imidazo[1,2-a]pyrimidines and -pyridines
WO2012009475A1 (en) 2010-07-14 2012-01-19 Oregon Health & Science University Methods of treating cancer with inhibition of lysine-specific demethylase 1
WO2012016133A2 (en) 2010-07-29 2012-02-02 President And Fellows Of Harvard College Ros1 kinase inhibitors for the treatment of glioblastoma and other p53-deficient cancers
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
EP2598482B1 (en) 2010-07-29 2018-04-04 Oryzon Genomics, S.A. Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use
US9527805B2 (en) 2010-09-10 2016-12-27 Robert A. Casero Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders
WO2012043638A1 (ja) 2010-09-29 2012-04-05 キッセイ薬品工業株式会社 (アザ)インドリジン誘導体及びその医薬用途
US20130303545A1 (en) 2010-09-30 2013-11-14 Tamara Maes Cyclopropylamine derivatives useful as lsd1 inhibitors
US20120108500A1 (en) 2010-10-07 2012-05-03 Naoki Sakane Compositions and Methods for Modulating Immunodeficiency Virus Transcription
MX343596B (es) 2010-10-18 2016-11-11 E I Du Pont De Nemours And Company * Sulfonamidas nematocidas.
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
WO2012071469A2 (en) 2010-11-23 2012-05-31 Nevada Cancer Institute Histone demethylase inhibitors and uses thereof for treatment o f cancer
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
JP5937102B2 (ja) 2010-12-14 2016-06-22 エレクトロフォレティクス リミテッド カゼインキナーゼ1デルタ(ck1デルタ)阻害剤
CA2821834A1 (en) 2010-12-17 2012-06-21 Bayer Intellectual Property Gmbh 6 substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
CA2821819A1 (en) 2010-12-17 2012-06-21 Marcus Koppitz 6-substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
UY33805A (es) 2010-12-17 2012-07-31 Boehringer Ingelheim Int ?Derivados de dihidrobenzofuranil-piperidinilo, aza-dihidrobenzofuranilpiperidinilo y diaza-dihidrobenzofuranil-piperidinilo, composiciones farmacéuticas que los contienen y usos de los mismos?.
EP2651944B1 (en) 2010-12-17 2015-09-23 Bayer Intellectual Property GmbH Substituted 6-imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
ES2544609T3 (es) 2010-12-17 2015-09-02 Bayer Intellectual Property Gmbh Imidazopirazinas 2-sustituidas para uso como inhibidores de Mps-1 y TTK en el tratamiento de trastornos hiper-proliferativos
US8987271B2 (en) 2010-12-22 2015-03-24 Eutropics Pharmaceuticals, Inc. 2,2′-biphenazine compounds and methods useful for treating disease
TWI617559B (zh) 2010-12-22 2018-03-11 江蘇恆瑞醫藥股份有限公司 2-芳基咪唑并[1,2-b]嗒.2-苯基咪唑并[1,2-a]吡啶,和2-苯基咪唑并[1,2-a]吡衍生物
US20140038953A1 (en) 2011-01-21 2014-02-06 The General Hospital Corporation Compositions and methods for cardiovascular disease
WO2012107498A1 (en) 2011-02-08 2012-08-16 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative disorders
US20140163041A1 (en) 2011-02-08 2014-06-12 Oryzon Genomics S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
WO2012129562A2 (en) 2011-03-24 2012-09-27 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
CA2831143C (en) 2011-03-25 2019-05-21 Glaxosmithkline Intellectual Property Development Limited Cyclopropylamines as lsd1 inhibitors
WO2012147890A1 (ja) 2011-04-27 2012-11-01 持田製薬株式会社 新規アゾール誘導体
EP2741741A2 (en) 2011-05-19 2014-06-18 Oryzon Genomics, S.A. Lysine demethylase inhibitors for inflammatory diseases or conditions
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
US20140296255A1 (en) 2011-05-19 2014-10-02 Oryzong Genomics, S.A. Lysine demethylase inhibitors for thrombosis and cardiovascular diseases
ES2560611T3 (es) 2011-06-20 2016-02-22 Incyte Holdings Corporation Derivados de fenil de azetidinilo, carboxamida de piridilo o pirazinilo como inhibidores de JAK
TW201311149A (zh) 2011-06-24 2013-03-16 Ishihara Sangyo Kaisha 有害生物防治劑
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
AU2012293223B2 (en) 2011-08-09 2017-03-02 Takeda Pharmaceutical Company Limited Cyclopropaneamine compound
PL2744330T3 (pl) 2011-08-15 2020-12-14 University Of Utah Research Foundation Podstawione analogi (e)-n'-(1-fenyloetylideno)benzohydrazydu jako inhibitory demetylazy histonowej
WO2013033688A1 (en) 2011-09-01 2013-03-07 The Brigham And Women's Hospital, Inc. Treatment of cancer
US9273343B2 (en) 2011-09-02 2016-03-01 Promega Corporation Compounds and methods for assaying redox state of metabolically active cells and methods for measuring NAD(P)/NAD(P)H
HK1211023A1 (zh) 2011-10-10 2016-05-13 H. Lundbeck A/S 具有咪唑并吡嗪骨架pde9i
BR112014009306B1 (pt) 2011-10-20 2021-07-20 Oryzon Genomics S.A. Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1
US9469597B2 (en) 2011-10-20 2016-10-18 Oryzon Genomics S.A. (Hetero)aryl cyclopropylamine compounds as LSD1 inhibitors
ITMI20111971A1 (it) 2011-10-28 2013-04-29 Mesogenics Srl Inibitori dell'enzima lsd-1 per l'induzione del differenziamento osteogenico
EP2785183B1 (en) 2011-11-14 2018-12-19 Merck Sharp & Dohme Corp. Triazolopyridinone pde10 inhibitors
EP2787990A4 (en) 2011-12-05 2015-09-02 Univ Brandeis TREATMENT OF AMYLOIDOSE BY COMPOUNDS FOR REGULATING RETROMER STABILIZATION
WO2013131609A1 (en) 2012-03-07 2013-09-12 Merck Patent Gmbh Triazolopyrazine derivatives
GB201205669D0 (en) 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
CN103373996A (zh) 2012-04-20 2013-10-30 山东亨利医药科技有限责任公司 作为crth2受体拮抗剂的二并环衍生物
ES2710491T3 (es) 2012-06-28 2019-04-25 Novartis Ag Moduladores de la vía del complemento y sus usos
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
EP2900238B1 (en) 2012-09-28 2017-12-06 Vanderbilt University Fused heterocyclic compounds as selective bmp inhibitors
AU2013326867B2 (en) 2012-10-05 2018-03-08 Rigel Pharmaceuticals, Inc. GDF-8 inhibitors
JP6325449B2 (ja) 2012-10-12 2018-05-16 武田薬品工業株式会社 シクロプロパンアミン化合物およびその用途
CA2890897A1 (en) 2012-11-14 2014-05-22 The Board Of Regents Of The University Of Texas System Inhibition of hif-2.alpha. heterodimerization with hif 1.beta. (arnt)
JP6238908B2 (ja) 2012-11-28 2017-11-29 京都府公立大学法人 リシン構造を有するlsd1選択的阻害薬
EP2925307B1 (en) 2012-11-30 2020-10-28 McCord, Darlene E. Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition
EP2740474A1 (en) 2012-12-05 2014-06-11 Instituto Europeo di Oncologia S.r.l. Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
CN103054869A (zh) 2013-01-18 2013-04-24 郑州大学 含三唑基的氨基二硫代甲酸酯化合物在制备以lsd1为靶标药物中的应用
CN103933036B (zh) 2013-01-23 2017-10-13 中国人民解放军军事医学科学院毒物药物研究所 2‑芳基咪唑并[1,2‑α]吡啶‑3‑乙酰胺衍生物在制备防治PTSD的药物中的用途
WO2014127350A1 (en) 2013-02-18 2014-08-21 The Scripps Research Institute Modulators of vasopressin receptors with therapeutic potential
WO2014164867A1 (en) 2013-03-11 2014-10-09 Imago Biosciences Kdm1a inhibitors for the treatment of disease
US20160050895A1 (en) 2013-03-13 2016-02-25 Australian Nuclear Science And Technology Organization Transgenic non-human organisms with non-functional tspo genes
AU2014236348B2 (en) 2013-03-14 2018-05-10 Epizyme, Inc. Combination therapy for treating cancer
US20140343118A1 (en) 2013-03-14 2014-11-20 Duke University Methods of treatment using arylcyclopropylamine compounds
WO2014194280A2 (en) 2013-05-30 2014-12-04 The Board of Regents of the Nevada System of Higher Education on behalf of the University of Novel suicidal lsd1 inhibitors targeting sox2-expressing cancer cells
WO2014205213A1 (en) 2013-06-19 2014-12-24 University Of Utah Research Foundation Substituted (e)-n'-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors
US9186391B2 (en) 2013-08-29 2015-11-17 Musc Foundation For Research Development Cyclic peptide inhibitors of lysine-specific demethylase 1
US9556170B2 (en) 2013-08-30 2017-01-31 University Of Utah Research Foundation Substituted-1H-benzo[d]imidazole series compounds as lysine-specific demethylase 1 (LSD1) inhibitors
KR101568724B1 (ko) 2013-11-13 2015-11-12 서울대학교산학협력단 신규한 화합물, 이의 생산 방법, 및 히스톤 디메틸라제 저해제로서 이의 용도
SI3080100T1 (sl) 2013-12-11 2023-04-28 Celgene Quanticel Research, Inc. Inhibitorji lizin specifične demetilaze-1
PE20161384A1 (es) 2014-02-13 2016-12-28 Incyte Corp Ciclopropilaminas como inhibidores de lsd 1
RS59559B1 (sr) 2014-02-13 2019-12-31 Incyte Corp Ciklopropilamini kao lsd1 inhibitori
WO2015123408A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9346776B2 (en) 2014-02-13 2016-05-24 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
US9428470B2 (en) 2014-02-13 2016-08-30 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
CN103893163B (zh) 2014-03-28 2016-02-03 中国药科大学 2-([1,1′-联苯]-4-基)2-氧代乙基4-((3-氯-4-甲基苯基)氨基)-4-氧代丁酸酯在制备lsd1抑制剂药物中的应用
RS58062B1 (sr) 2014-04-02 2019-02-28 Bristol Myers Squibb Co Biaril inhibitori kinaze
EP3129369A1 (en) 2014-04-11 2017-02-15 Takeda Pharmaceutical Company Limited Cyclopropanamine compound and use thereof
CN103961340B (zh) 2014-04-30 2019-06-25 南通中国科学院海洋研究所海洋科学与技术研究发展中心 一类lsd1抑制剂及其应用
JP6320570B2 (ja) 2014-05-30 2018-05-09 イエオ−イスティトゥート・エウロペオ・ディ・オンコロジア・エッセ・エッレ・エッレ ヒストンデメチラーゼ阻害剤としてのシクロプロピルアミン化合物
CN104119280B (zh) 2014-06-27 2016-03-16 郑州大学 含氨基类脲与端炔结构单元的嘧啶衍生物、制备方法及应用
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
GB201417828D0 (en) 2014-10-08 2014-11-19 Cereno Scient Ab New methods and compositions
AU2015330141B2 (en) 2014-10-08 2019-12-05 F. Hoffmann-La Roche Ag Spirodiamine derivatives as aldosterone synthase inhibitors
EA201792186A1 (ru) 2015-04-03 2018-03-30 Бристол-Майерс Сквибб Компани Ингибиторы индоламин-2,3-диоксигеназы и способы их применения
TWI714567B (zh) 2015-04-03 2021-01-01 美商英塞特公司 作為lsd1抑制劑之雜環化合物
KR20170132316A (ko) 2015-04-03 2017-12-01 무타빌리스 헤테로고리 화합물 및 박테리아 감염의 예방 또는 치료에서 그들의 용도
HUE070538T2 (hu) 2015-08-12 2025-06-28 Incyte Holdings Corp Egy LSD1 inhibitor sói
WO2017130933A1 (ja) 2016-01-25 2017-08-03 国立大学法人熊本大学 神経変性疾患治療剤
PE20190377A1 (es) 2016-04-22 2019-03-08 Incyte Corp Formulaciones de un inhibidor de lsd 1
US20200054643A1 (en) 2017-01-18 2020-02-20 Vanderbilt University Fused heterocyclic compounds as selective bmp inhibitors
UA125592C2 (uk) 2017-03-16 2022-04-27 Джянгсу Хенгруй Медісін Ко., Лтд. ПОХІДНА ГЕТЕРОАРИЛ[4,3-c]ПІРИМІДИН-5-АМІНУ, СПОСІБ ЇЇ ОТРИМАННЯ ТА ЇЇ МЕДИЧНІ ЗАСТОСУВАННЯ

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116836167A (zh) * 2022-03-25 2023-10-03 腾讯科技(深圳)有限公司 咪唑并[1,2-a]吡嗪或吡唑并[1,5-a]嘧啶衍生物及其用途

Also Published As

Publication number Publication date
US20160009720A1 (en) 2016-01-14
AR101174A1 (es) 2016-11-30
US10112950B2 (en) 2018-10-30
WO2016007736A1 (en) 2016-01-14
US20170369497A1 (en) 2017-12-28
US20190106426A1 (en) 2019-04-11
US9695180B2 (en) 2017-07-04
US10556908B2 (en) 2020-02-11

Similar Documents

Publication Publication Date Title
TW201613925A (en) Imidazopyrazines as LSD1 inhibitors
ZA201605715B (en) Cyclopropylamines as lsd1 inhibitors
SG10201908028SA (en) Cyclopropylamines as lsd1 inhibitors
EP3107914B8 (en) Pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds as cdk inhibitors and their therapeutic use
TW201613860A (en) Cyclopropylamines as LSD1 inhibitors
MY191796A (en) Heterocyclic compounds as lsd1 inhibitors
NZ758528A (en) Bicyclic heterocycle compounds and their uses in therapy
PH12016501898B1 (en) Quinoxaline derivatives useful as fgfr kinase modulators
PH12016501232A1 (en) Pyrazolo[1,5-a]pyridine derivatives and methods of their use
HK1245247A1 (zh) 溴结构域的抑制剂
JO3618B1 (ar) صيغة قرص2-فلورو-nميثيل -4 -[7-(كوينولين-6-يل ميثيل)اميدازو[2,1-b] [4,2,1] تريازين-2-يل] بنزاميد
MX2015014234A (es) Derivados 2-aminopirido-[4,3-d]pirimidin-5-ona y su uso como inhibidores de wee-1.
MX2017003466A (es) Inhibidores de histona desmetilasa.
IL290419B (en) Imidazo[a-1,5]pyrazine derivatives as inhibitors of pi3k delta
MY180844A (en) Solid pharmaceutical compositions comprising biopterin derivatives and uses of such compositions
AU2018253600A1 (en) Dosage forms and therapeutic uses of l-4-chlorokynurenine
AU2015373422A8 (en) New imidazo[1,2-a]quinoxalines and derivates thereof for the treatment of cancer