KR102421235B1 - Lsd1 저해제로서 사이클로프로필아민 - Google Patents

Lsd1 저해제로서 사이클로프로필아민 Download PDF

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KR102421235B1
KR102421235B1 KR1020167025508A KR20167025508A KR102421235B1 KR 102421235 B1 KR102421235 B1 KR 102421235B1 KR 1020167025508 A KR1020167025508 A KR 1020167025508A KR 20167025508 A KR20167025508 A KR 20167025508A KR 102421235 B1 KR102421235 B1 KR 102421235B1
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alkyl
delete delete
cancer
aryl
cycloalkyl
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KR20160132409A (ko
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량싱 우
춘훙 헤
딩-취안 쳰
보 선
샤오자오 왕
원칭 야오
펑레이 장
조엘 알. 코터
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인사이트 코포레이션
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • C07D211/32—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020167025508A 2014-02-13 2015-02-12 Lsd1 저해제로서 사이클로프로필아민 Active KR102421235B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201461939488P 2014-02-13 2014-02-13
US61/939,488 2014-02-13
US201462061283P 2014-10-08 2014-10-08
US62/061,283 2014-10-08
PCT/US2015/015706 WO2015123465A1 (en) 2014-02-13 2015-02-12 Cyclopropylamines as lsd1 inhibitors

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KR20160132409A KR20160132409A (ko) 2016-11-18
KR102421235B1 true KR102421235B1 (ko) 2022-07-15

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SM (1) SMT201900680T1 (OSRAM)
TW (2) TWI741478B (OSRAM)
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WO (1) WO2015123465A1 (OSRAM)
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Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2014306149B2 (en) 2013-08-06 2019-09-19 Imago Biosciences Inc. KDM1A inhibitors for the treatment of disease
US9346776B2 (en) 2014-02-13 2016-05-24 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
PT3105218T (pt) 2014-02-13 2019-12-05 Incyte Corp Ciclopropilaminas como inibidores de lsd1
DK3105226T3 (da) 2014-02-13 2019-10-14 Incyte Corp Cyclopropylaminer som lsd1-inhibitorer
US9428470B2 (en) 2014-02-13 2016-08-30 Takeda Pharmaceutical Company Limited Heterocyclic compound
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
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
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
MX387224B (es) 2015-02-12 2025-03-18 Imago Biosciences Inc Inhibidores de kdm1a para el tratamiento de enfermedades.
EP3626720A1 (en) 2015-04-03 2020-03-25 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
EP3307909A1 (en) 2015-06-12 2018-04-18 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
WO2017013061A1 (en) 2015-07-17 2017-01-26 Oryzon Genomics, S.A. Biomarkers associated with lsd1 inhibitors and uses thereof
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
US10059668B2 (en) 2015-11-05 2018-08-28 Mirati Therapeutics, Inc. LSD1 inhibitors
MX384792B (es) 2015-12-29 2025-03-14 Mirati Therapeutics Inc Inhibidores de desmetilasa especifica de lisina 1 (lsd1).
JP2019500394A (ja) 2015-12-30 2019-01-10 ノバルティス アーゲー 有効性が増強された免疫エフェクター細胞治療
SG11201807965YA (en) 2016-03-15 2018-10-30 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
ES3042059T3 (en) 2016-03-16 2025-11-18 Oryzon Genomics Sa Methods to determine kdm1a target engagement and chemoprobes useful therefor
CN107200706A (zh) * 2016-03-16 2017-09-26 中国科学院上海药物研究所 一类氟取代的环丙胺类化合物及其制备方法、药物组合物和用途
PE20190377A1 (es) * 2016-04-22 2019-03-08 Incyte Corp Formulaciones de un inhibidor de lsd 1
KR102479789B1 (ko) * 2016-05-09 2022-12-22 주빌런트 에피코어 엘엘씨 이중 lsd1/hdac 억제제로서 사이클로프로필-아마이드 화합물
CN107459476B (zh) * 2016-06-03 2022-06-24 中国科学院上海药物研究所 反吲哚啉环丙胺类化合物及其制备方法、药物组合物和用途
WO2018035259A1 (en) * 2016-08-16 2018-02-22 Imago Biosciences, Inc. Methods and processes for the preparation of kdm1a inhibitors
EP3535420A1 (en) 2016-11-03 2019-09-11 Oryzon Genomics, S.A. Biomarkers for determining responsiveness to lsd1 inhibitors
WO2018083138A1 (en) 2016-11-03 2018-05-11 Oryzon Genomics, S.A. Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents
RU2763898C9 (ru) 2017-01-24 2022-03-18 Цспц Чжунци Фармасьютикал Текнолоджи (Шицзячжуан) Ко., Лтд. Ингибитор lsd1, а также способ его получения и его применение
CN106860453A (zh) * 2017-02-17 2017-06-20 杨燕 一种治疗溃疡性结肠炎的药物组合物
EP3628044B1 (en) 2017-05-15 2023-11-22 The Regents of The University of Michigan Pyrrolo[2,3-c]pyridines and related analogs as lsd-1 inhibitors
DK3661510T3 (da) 2017-08-03 2025-01-02 Oryzon Genomics Sa Fremgangsmåder til behandling af adfærdsændringer
WO2019083971A1 (en) 2017-10-23 2019-05-02 Children's Medical Center Corporation METHODS OF TREATING CANCER USING LSD1 INHIBITORS IN COMBINATION WITH IMMUNOTHERAPY
IL279260B2 (en) 2018-05-11 2024-10-01 Imago Biosciences Inc Kdm1a inhibitors for the treatment of disease
EP3794003A1 (en) 2018-05-15 2021-03-24 The Regents Of The University Of Michigan Imidazo[4,5-c]pyridine compounds as lsd-1 inhibitors
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
SG11202109159VA (en) 2019-03-20 2021-10-28 Oryzon Genomics Sa Methods of treating borderline personality disorder
JP7535797B2 (ja) 2019-03-20 2024-08-19 オリソン ヘノミクス，ソシエダ アノニマ 化合物バフィデムスタット（ｖａｆｉｄｅｍｓｔａｔ）などｋｄｍ１ａ阻害剤を使用した注意欠陥多動性障害の処置方法
JP2022546908A (ja) 2019-07-05 2022-11-10 オリゾン・ゲノミクス・ソシエダッド・アノニマ Ｋｄｍ１ａ阻害剤を使用した小細胞肺がんの個別化された処置のためのバイオマーカーおよび方法
CN114502561B (zh) * 2019-09-29 2023-12-26 南昌弘益药业有限公司 Lsd1抑制剂
WO2021214502A1 (en) * 2020-04-21 2021-10-28 Idience Co., Ltd. Process for preparing a phthalazinone derivative and intermediates thereof
US12059419B2 (en) 2020-10-16 2024-08-13 Idience Co., Ltd. Pharmaceutical composition comprising phthalazinone derivatives
CA3231846A1 (en) 2021-04-08 2022-10-13 Tamara Maes Combinations of lsd1 inhibitors for treating myeloid cancers
MX2024002173A (es) 2021-08-18 2024-03-26 Chemocentryx Inc Compuestos de arilsulfonilo como inhibidores de ccr6.
KR20240049280A (ko) 2021-08-18 2024-04-16 케모센트릭스, 인크. Ccr6 억제제로서의 아릴 설포닐(하이드록시) 피페리딘
WO2023067058A1 (en) 2021-10-20 2023-04-27 Queen Mary University Of London Sequential treatments and biomarkers to reverse resistance to kinase inhibitors
GB202115017D0 (en) 2021-10-20 2021-12-01 Univ London Queen Mary Sequential treatments and biomarkers to reverse resistance to kinase inhibitors
JP2025516647A (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阻害薬を用いる悪性末梢神経鞘腫（ｍｐｎｓｔ）の治療法
CN119497613A (zh) 2022-05-09 2025-02-21 奥莱松基因组股份有限公司 使用lsd1抑制剂治疗nf1-突变肿瘤的方法
WO2024110649A1 (en) 2022-11-24 2024-05-30 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors and menin inhibitors for treating cancer
CN118787751A (zh) * 2023-04-12 2024-10-18 中国科学院上海药物研究所 Lsd1抑制剂与药物联用治疗癌症的用途
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012135113A2 (en) * 2011-03-25 2012-10-04 Glaxosmithkline Llc Cyclopropylamines as lsd1 inhibitors

Family Cites Families (320)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL7013068A (OSRAM) 1969-09-17 1971-03-19
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
JPH032778Y2 (OSRAM) 1986-12-15 1991-01-24
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
JP2844351B2 (ja) 1989-07-13 1999-01-06 株式会社科薬 安定なポリミキシン系抗生物質水性溶液
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.
EP0649425B1 (en) 1992-06-17 1999-03-10 PHARMACIA & UPJOHN COMPANY Pyridino-, pyrrolidino- and azepino-substituted oximes useful as anti-atherosclerosis and anti-hypercholesterolemic agents
JP2923139B2 (ja) 1992-10-05 1999-07-26 三井化学株式会社 製 剤
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.
US5932223A (en) 1996-09-26 1999-08-03 Merck & Co., Inc. Rotavirus vaccine formulations
TR200001728T2 (tr) 1997-11-11 2000-09-21 Ono Pharmaceutical Co., Ltd. Birleşik pirazin türevleri
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
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
JP4032566B2 (ja) 1999-06-21 2008-01-16 東レ株式会社 発光素子
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
UA80667C2 (en) 1999-09-28 2007-10-25 Panacea Biotec Ltd Controlled release composition comprising nimesulide and process for the preparation thereof
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
ES2244613T3 (es) 2000-04-27 2005-12-16 Astellas Pharma Inc. Derivados de imidazopiridina.
US6403588B1 (en) 2000-04-27 2002-06-11 Yamanouchi Pharmaceutical Co., Ltd. Imidazopyridine derivatives
EP1294358B1 (en) 2000-06-28 2004-08-18 Smithkline Beecham Plc Wet milling process
AR029538A1 (es) 2000-07-06 2003-07-02 Wyeth Corp Composiciones farmaceuticas de agentes estrogenicos
HUP0301801A2 (hu) 2000-07-14 2003-09-29 Bristol-Myers Squibb Pharma Company Imidazo[1,2-a]pirazin-származékok és az ezeket tartalmazó gyógyszerkészítmények
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
AU2001295992A1 (en) 2000-10-24 2002-05-06 Sankyo Company Limited Imidazopyridine derivatives
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
ES2251518T3 (es) 2000-11-10 2006-05-01 MERCK SHARP & DOHME LTD. Derivados de imidazo-triazina como ligandos para receptores gaba.
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
EP1513522A2 (en) 2002-01-18 2005-03-16 Sri International Methods of treating conditions associated with an edg receptor
US20050113283A1 (en) 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 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
US20060276339A1 (en) 2002-10-16 2006-12-07 Windsor J B Methods and compositions for increasing the efficacy of biologically-active ingredients
AU2003301226A1 (en) 2002-12-20 2004-07-22 Pharmacia Corp Acyclic pyrazole compounds for the inhibition of mitogen activated protein kinase-activated protein kinase-2
US7160885B2 (en) 2003-02-10 2007-01-09 Cgi Pharmaceuticals, Inc. Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex activity
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
EP2385040A1 (en) 2003-03-14 2011-11-09 ONO Pharmaceutical Co., Ltd. Nitrogen-containing heterocyclic derivatives and drugs containing the same as the active ingredient
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
ES2338656T3 (es) 2003-04-11 2010-05-11 High Point Pharmaceuticals, Llc Uso farmaceutico de 1,2,4-triazoles fusionados.
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
US7132426B2 (en) 2003-07-14 2006-11-07 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
US7538120B2 (en) 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
EP1663193B1 (en) 2003-09-12 2012-04-04 Merck Serono SA Sulfonamide derivatives for the treatment of 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
WO2005044793A2 (en) 2003-10-31 2005-05-19 Takeda Pharmaceutical Company Limited Nitrogen-containing fused heterocyclic compounds
EP1698335A4 (en) 2003-12-26 2007-08-01 Ono Pharmaceutical Co AGENT FOR PREVENTING AND / OR TREATING DISEASES INVOLVING A MITOCHONDRIAL BENZODIAZEPINE RECEPTOR
EP1717238A4 (en) 2004-02-16 2008-03-05 Daiichi Seiyaku Co FUNGICIDES HETEROCYCLIC COMPOUNDS
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
CA2564356A1 (en) * 2004-04-26 2005-11-03 Pfizer Inc. Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors
JP5154924B2 (ja) 2004-05-11 2013-02-27 エガレット エイ／エス ジェランガムを含む膨張可能な投与形態
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
WO2006026703A2 (en) 2004-09-02 2006-03-09 Smithkline Beecham Corporation Chemical compounds
US7524860B2 (en) 2004-10-07 2009-04-28 Pfizer Inc. Antibacterial agents
AU2005309761A1 (en) 2004-11-22 2006-06-01 Threshold Pharmaceuticals, Inc. Tubulin binding anti cancer agents and prodrugs thereof
ATE443063T1 (de) 2004-12-01 2009-10-15 Merck Serono Sa Ä1,2,4ütriazoloä4,3-aüpyridin-derivative zur behandlung hyperproliferativer erkrankungen
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
AP2007004067A0 (en) 2005-02-22 2007-08-31 Pfizer Oxyindole derivatives as 5HT4 receptor agonists
ITBO20050123A1 (it) 2005-03-07 2005-06-06 Alfa Wassermann Spa Formulazioni farmaceutiche gastroresistenti contenenti rifaximina
JP2008536950A (ja) 2005-04-18 2008-09-11 ニューロジェン・コーポレーション 置換ヘテロアリールのｃｂ１拮抗薬
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
EP1901748B1 (en) 2005-06-09 2010-09-08 Oncalis AG Angiogenesis inhibitors
US7632837B2 (en) 2005-06-17 2009-12-15 Bristol-Myers Squibb Company Bicyclic heterocycles as cannabinoid-1 receptor modulators
US7572808B2 (en) 2005-06-17 2009-08-11 Bristol-Myers Squibb Company Triazolopyridine cannabinoid receptor 1 antagonists
US7452892B2 (en) 2005-06-17 2008-11-18 Bristol-Myers Squibb Company Triazolopyrimidine cannabinoid receptor 1 antagonists
TWI255587B (en) 2005-07-04 2006-05-21 Quanta Comp Inc Multi-frequency planar antenna
JP2009507032A (ja) 2005-09-02 2009-02-19 アボット・ラボラトリーズ 新規なイミダゾ系複素環
US7700773B2 (en) 2005-09-09 2010-04-20 Schering Corporation 4-cyano, 4-amino, and 4-aminomethyl derivatives of pyrazolo[1,5-a]pyridines, pyrazolo[1,5-c]pyrimidines and 2H-indazole compounds and 5-cyano, 5-amino, and 5-aminomethyl derivatives of imidazo[1,2-a]pyridines, and imidazo[1,5-a]pyrazines as cyclin dependent kinase inhibitors
AR056785A1 (es) 2005-11-10 2007-10-24 Schering Corp COMPUESTOS DE IMIDAZO[1,2-A]PIRAZINAS, uTILES COMO INHIBIDORES, REGULADORES O MODULADORES DE PROTEINQUINASAS
EP1959966B1 (en) 2005-11-28 2020-06-03 Marinus Pharmaceuticals, Inc. Ganaxolone formulations and methods for the making and use thereof
CA2633536A1 (en) 2005-12-27 2007-07-05 F. Hoffmann-La Roche Ag 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
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
AR061229A1 (es) 2006-06-06 2008-08-13 Schering Corp Imidazopirazinas como inhibidores de la proteina quinasa
DK2029554T3 (da) 2006-06-22 2014-06-10 Medibeacon Llc Pyrazinderivater og anvendelser heraf til nyreovervågning
CA2655857C (en) 2006-06-22 2014-12-02 Mallinckrodt Inc. Pyrazine derivatives with extended conjugation and uses thereof
EP2032560B1 (en) 2006-06-29 2013-05-01 Merck Sharp & Dohme Corp. Substituted bicyclic and tricyclic thrombin receptor antagonists
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
US8217177B2 (en) 2006-07-14 2012-07-10 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
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
CA2658764A1 (en) 2006-07-20 2008-01-24 Mehmet Kahraman Benzothiophene inhibitors of rho kinase
US7563797B2 (en) 2006-08-28 2009-07-21 Forest Laboratories Holding Limited Substituted imidazo(1,2-A)pyrimidines and imidazo(1,2-A) pyridines as cannabinoid receptor ligands
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
AU2007307031B2 (en) 2006-10-11 2011-11-24 Amgen Inc. Imidazo- and triazolo-pyridine compounds and methods of use therof
AU2007317242B2 (en) 2006-11-08 2013-08-01 Neurocrine Biosciences, Inc. Substituted 3-isobutyl-9, 10-dimethoxy-1,3,4,6,7,11B-hexahydro-2H-pyrido[2,1-a] isoquinolin-2-ol compounds and methods relating thereto
CN101646419A (zh) 2006-11-08 2010-02-10 诺瓦瓦克斯股份有限公司 制备多相药物组合物的固体剂型的方法
WO2008056176A1 (en) 2006-11-10 2008-05-15 Scottish Biomedical Limited Pyrazolopyrimidines as phosphodiesterase inhibitors
GEP20125658B (en) 2006-11-22 2012-10-10 Incyte Corp Imidazotriazines and imidazo pyrimidines as kinase inhibitors
DE602007012133D1 (de) 2006-12-01 2011-03-03 Andrew Burritt Triazolopyridinverbindungen zur behandlung von degenerations- und entzündungskrankheiten
AU2007338631A1 (en) 2006-12-22 2008-07-03 Combinatorx, Incorporated Pharmaceutical compositions for treatment of parkinson's disease and related disorders
US7803810B2 (en) 2007-03-09 2010-09-28 Probiodrug Ag Inhibitors
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
ES2380395T3 (es) 2007-04-16 2012-05-11 Leo Pharma A/S Triazolopiridinas como inhibidores de fosfodiesterasa para el tratamiento de enfermedades dérmicas
US8546394B2 (en) 2007-04-17 2013-10-01 Bristol-Myers Squibb Company Substituted [1,2,4]triazolo[4,3-A]pyrazine 11-beta-hydroxysteroid dehydrogenase inhibitors
EP2155747B1 (en) 2007-05-10 2012-10-24 GE Healthcare Limited Imidazol (1,2-a)pyridines and related compounds with activity at cannabinoid cb2 receptors
JP5343845B2 (ja) 2007-05-21 2013-11-13 東レ株式会社 特定の有機酸を含有する経口製剤並びに経口製剤の溶出性及び化学的安定性の改善方法
WO2008154241A1 (en) 2007-06-08 2008-12-18 Abbott Laboratories 5-heteroaryl substituted indazoles as kinase inhibitors
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
PE20090365A1 (es) 2007-06-14 2009-04-04 Schering Corp Imidazopirazinas como inhibidores de proteina quinasa
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.
US20090004281A1 (en) 2007-06-26 2009-01-01 Biovail Laboratories International S.R.L. Multiparticulate osmotic delivery system
AR067562A1 (es) 2007-07-18 2009-10-14 Novartis Ag Compuestos heterociclicos inhibidores de kinasa
KR20100042287A (ko) 2007-07-31 2010-04-23 쉐링 코포레이션 항암요법으로서의 항-유사분열제 및 아우로라 키나제 억제제 조합물
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
EA201000201A1 (ru) 2007-08-10 2010-12-30 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Азотсодержащие бициклические химические вещества для лечения вирусных инфекций
US20090047336A1 (en) 2007-08-17 2009-02-19 Hong Kong Baptist University novel formulation of dehydrated lipid vesicles for controlled release of active pharmaceutical ingredient via inhalation
FR2920091A1 (fr) 2007-08-24 2009-02-27 Oreal Composition tinctoriale comprenant une base d'oxydation aminopyrazolopyridine, un coupleur et un polyol particulier.
FR2920090A1 (fr) 2007-08-24 2009-02-27 Oreal Composition tinctoriale comprenant une base d'oxydation aminopyrazolopyridine particuliere, un coupleur et un tensioactif particulier.
KR20090022616A (ko) 2007-08-31 2009-03-04 한올제약주식회사 베실산클로피도그렐 함유 경구투여용 약제
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
JP4705695B2 (ja) 2007-10-11 2011-06-22 アストラゼネカ アクチボラグ プロテインキナーゼｂ阻害剤としてのピロロ［２，３−ｄ］ピリミジン誘導体
EP3733161A1 (en) 2007-10-12 2020-11-04 Novartis AG Compositions comprising sphingosine 1 phosphate (s1p) receptor modulators
CA2710194C (en) 2007-12-19 2014-04-22 Amgen Inc. Inhibitors of p13 kinase
CA2704125A1 (en) 2007-12-19 2009-07-09 Genentech, Inc. 8-anilinoimidazopyridines and their use as anti-cancer and/or anti-inflammatory agents
KR100988233B1 (ko) 2007-12-26 2010-10-18 한미홀딩스 주식회사 클로피도그렐 1,5-나프탈렌 다이술폰산 염 또는 이의수화물의 약학 조성물 및 제제
MX2010010012A (es) 2008-03-11 2010-10-20 Incyte Corp Derivados de azetidina y ciclobutano como inhibidores de jak.
PL2262505T3 (pl) 2008-03-12 2015-04-30 Intra Cellular Therapies Inc Podstawione heterocykliczne skondensowane gamma-karboliny w postaci stałej
EP2265603B1 (en) 2008-03-13 2014-05-07 The General Hospital Corporation Inhibitors of the bmp signaling pathway
JP5547099B2 (ja) 2008-03-14 2014-07-09 インテリカイン， エルエルシー キナーゼ阻害剤および使用方法
JPWO2009128520A1 (ja) 2008-04-18 2011-08-04 塩野義製薬株式会社 Ｐｉ３ｋ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
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
WO2010010187A1 (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
UY32049A (es) 2008-08-14 2010-03-26 Takeda Pharmaceutical Inhibidores de cmet
TR200806298A2 (tr) 2008-08-22 2010-03-22 Bi̇lgi̇ç Mahmut Farmasötik formülasyon
US20120021519A1 (en) 2008-09-19 2012-01-26 Presidents 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
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
EP2361242B1 (en) 2008-10-17 2018-08-01 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
ES2403633T3 (es) 2008-12-04 2013-05-20 Proximagen Limited Compuestos de imidazopiridina
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
WO2010090991A1 (en) 2009-02-04 2010-08-12 Supernus Pharmaceuticals, Inc. Formulations of desvenlafaxine
TR200900878A2 (tr) 2009-02-05 2010-08-23 Bi̇lgi̇ç Mahmut Tek bir dozaj formunda kombine edilen farmasötik formülasyonlar
TR200900879A2 (tr) 2009-02-05 2010-08-23 Bi̇lgi̇ç Mahmut Aktif maddelerin tek bir dozaj formunda kombine edildiği farmasötik bileşimler
ES2435804T3 (es) 2009-02-13 2013-12-23 Bayer Intellectual Property Gmbh Pirimidinas condensadas como inhibidores de Akt
WO2010104307A2 (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
WO2010107404A1 (en) 2009-03-16 2010-09-23 Mahmut Bilgic Stable pharmaceutical combinations
TW201035078A (en) 2009-03-20 2010-10-01 Incyte Corp Substituted heterocyclic compounds
KR101772963B1 (ko) 2009-03-31 2017-08-31 깃세이 야쿠힌 고교 가부시키가이샤 인돌리진 유도체 및 그 의약용도
CN102428087B (zh) 2009-04-16 2015-06-17 卡洛斯三世国家癌症研究中心基金会 用作激酶抑制剂的咪唑并吡嗪类化合物
TWI461426B (zh) 2009-05-27 2014-11-21 Merck Sharp & Dohme （二氫）咪唑並異〔５，１－ａ〕喹啉類
RU2011153723A (ru) 2009-06-10 2013-07-20 Суновион Фармасьютикалз Инк. Обратные агонисты и антагонисты н3 рецепторов гистамина и способы их применения
AU2010266040B2 (en) 2009-06-25 2015-01-15 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds
HRP20190016T1 (hr) 2009-08-17 2019-03-08 Intellikine, Llc Heterociklički spojevi i njihova upotreba
US9708255B2 (en) 2009-08-18 2017-07-18 Robert A. Casero (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
KR101736218B1 (ko) 2009-09-25 2017-05-16 오리존 지노믹스 에스.에이. 라이신 특이적 디메틸라아제-1 억제제 및 이의 용도
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
US8614315B2 (en) 2009-12-25 2013-12-24 Mahmut Bilgic Cefdinir and cefixime formulations and uses thereof
EP2526102B1 (en) 2010-01-22 2017-03-08 Fundación Centro Nacional de Investigaciones Oncológicas Carlos III Inhibitors of PI3 kinase
WO2011097607A1 (en) 2010-02-08 2011-08-11 Southern Research Institute Anti-viral treatment and assay to screen for anti-viral agent
WO2011106574A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
WO2011106573A2 (en) 2010-02-24 2011-09-01 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
AU2011229423B2 (en) 2010-03-18 2015-12-10 Institut National De La Sante Et De La Recherche Medicale (Inserm) Anti-infective compounds
CA2793279A1 (en) 2010-03-18 2011-09-22 Ulrich Klar Imidazopyrazines
MX342161B (es) 2010-04-02 2016-09-19 Euroscreen Sa Compuestos antagonistas selectivos de receptor nk-3 novedosos, composicion farmaceutica y metodos para utilizarse en trastornos transmitidos por receptores nk-3.
BR122019020471B1 (pt) 2010-04-19 2021-06-22 Oryzon Genomics S.A. Inibidores da desmetilase específica para lisina 1, seus usos e método para sua identificação, e composições farmacêuticas
PL2560949T3 (pl) 2010-04-20 2017-01-31 Università Degli Studi Di Roma "La Sapienza" Pochodne tranylocyprominy jako inhibitory demetylazy histonowej LSD1 i/lub LSD2
MX2012012145A (es) 2010-04-28 2012-11-21 Daiichi Sankyo Co Ltd Compuestos [5, 6] heterociclico.
US20130131057A1 (en) 2010-05-13 2013-05-23 Centro Nacional De Investigaciones Oncologicas (Cnio New bicyclic compounds as pi3-k and mtor inhibitors
SG185515A1 (en) 2010-05-13 2012-12-28 Amgen Inc Nitrogen heterocyclic compounds useful as pde10 inhibitors
CN102247321A (zh) 2010-05-20 2011-11-23 上海亚盛医药科技有限公司 一种阿朴棉子酚酮自乳化药物传递系统及其制备方法
WO2011149438A1 (en) 2010-05-28 2011-12-01 Mahmut Bilgic Combination of antihypertensive agents
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
CN101987082B (zh) 2010-07-16 2013-04-03 钟术光 固体制剂及其制备方法
CN101987081B (zh) 2010-07-16 2012-08-08 钟术光 一种控释制剂
WO2012013728A1 (en) * 2010-07-29 2012-02-02 Oryzon Genomics S.A. Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use
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
WO2012034116A2 (en) 2010-09-10 2012-03-15 The Johns Hopkins University Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders
CN102397552B (zh) 2010-09-10 2016-06-08 广州自远生物科技有限公司 一种含喹诺酮类的药物复合制剂及其制备方法和应用
CN103221412B (zh) 2010-09-29 2015-08-19 橘生药品工业株式会社 (氮杂)中氮茚衍生物及其药物用途
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
ES2525441T3 (es) 2010-10-18 2014-12-23 E.I. Du Pont De Nemours And Company Sulfonamidas nematocidas
ES2816600T3 (es) 2010-10-21 2021-04-05 Medivation Tech Llc Sal tosilato de (8S,9R)-5-fluoro-8-(4-fluorofenil)-9-(1-metil-1H-1,2,4-triazol-5-il)-8,9-dihidro-2H-pirido[4,3,2-de]ftalazin-3(7H)-ona cristalina
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
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
WO2012080729A2 (en) 2010-12-14 2012-06-21 Electrophoretics Limited CASEIN KINASE 1δ (CK1δ) INHIBITORS
WO2012080230A1 (en) 2010-12-17 2012-06-21 Bayer Pharma Aktiengesellschaft 6 substituted imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
WO2012080236A1 (en) 2010-12-17 2012-06-21 Bayer Pharma Aktiengesellschaft 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?.
JP5822944B2 (ja) 2010-12-17 2015-11-25 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 過剰増殖性障害の治療におけるｍｐｓ−１およびｔｋｋ阻害剤として使用するための２置換イミダゾピラジン
WO2012080234A1 (en) 2010-12-17 2012-06-21 Bayer Pharma Aktiengesellschaft Substituted 6-imidazopyrazines for use as mps-1 and tkk inhibitors in the treatment of hyperproliferative disorders
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
EP2655334B1 (en) 2010-12-22 2018-10-03 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
WO2012100229A2 (en) 2011-01-21 2012-07-26 The General Hospital Corporation Compositions and methods for cardiovascular disease
BRPI1100101B1 (pt) 2011-01-28 2020-10-20 Universidade De São Paulo Usp anel oito articulado
EP2712316A1 (en) 2011-02-08 2014-04-02 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders
EP3981395A1 (en) 2011-02-08 2022-04-13 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
JP5808826B2 (ja) 2011-02-23 2015-11-10 インテリカイン， エルエルシー 複素環化合物およびその使用
US9464065B2 (en) 2011-03-24 2016-10-11 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
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
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
WO2012156537A2 (en) 2011-05-19 2012-11-22 Oryzon Genomics, S.A. Lysine demethylase inhibitors for thrombosis and cardiovascular diseases
WO2012156531A2 (en) 2011-05-19 2012-11-22 Oryzon Genomics, S.A. Lysine demethylase inhibitors for inflammatory diseases or conditions
AU2012265842A1 (en) 2011-06-07 2014-01-23 SPAI Group Ltd. Compositions and methods for improving stability and extending shelf life of sensitive food additives and food products thereof
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
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
BR112014003382B1 (pt) 2011-08-15 2022-03-15 University Of Utah Research Foundation Análogos de (e)-n-(1-feniletilideno) benzo-hidrazida substituída como inibidores de histona desmetilase e composições farmacêuticas compreendendo-os
WO2013033688A1 (en) 2011-09-01 2013-03-07 The Brigham And Women's Hospital, Inc. Treatment of cancer
WO2013033515A1 (en) 2011-09-02 2013-03-07 Promega Corporation Compounds and methods for assaying redox state of metabolically active cells and methods for measuring nad(p)/nad(p)h
CN104703987B (zh) 2011-10-10 2017-05-03 H.隆德贝克有限公司 具有咪唑并吡嗪酮骨架的pde9抑制剂
CN104203914B (zh) 2011-10-20 2017-07-11 奥瑞泽恩基因组学股份有限公司 作为lsd1抑制剂的(杂)芳基环丙胺化合物
CL2014000988A1 (es) 2011-10-20 2014-11-03 Oryzon Genomics Sa Compuestos derivados de (aril o heteroaril) ciclopropilamida, inhibidores de lsd1; procedimiento para prepararlos; composicion farmaceutica que los comprende; y metodo para tratar o prevenir cancer, una enfermedad neurologica, una infeccion viral y la reactivacion viral despues de la latencia.
UA116765C2 (uk) 2011-10-20 2018-05-10 Орізон Джіномікс, С.А. (гетеро)арилциклопропіламіни як інгібітори lsd1
ITMI20111971A1 (it) 2011-10-28 2013-04-29 Mesogenics Srl Inibitori dell'enzima lsd-1 per l'induzione del differenziamento osteogenico
US9266881B2 (en) 2011-11-14 2016-02-23 Merck Sharp & Dohme Corp. Triazolopyridinone PDE10 inhibitors
CA2857964A1 (en) 2011-12-05 2013-06-13 Brandeis University Treatment of amyloidosis by compounds that regulate 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
CN102579381B (zh) 2012-03-30 2013-07-10 河南中帅医药科技发展有限公司 盐酸胍法辛缓释制剂及其制备方法
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
PE20190736A1 (es) * 2012-06-13 2019-05-23 Incyte Holdings Corp Compuestos triciclicos sustituidos como inhibidores del receptor del factor de crecimiento de fibroblastos (fgfr)
JP6273274B2 (ja) 2012-06-28 2018-01-31 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
CN102772444A (zh) 2012-07-06 2012-11-14 周明千 中药超微破壁口服片剂饮片的加工方法
GB201212513D0 (en) 2012-07-13 2012-08-29 Ucb Pharma Sa Therapeutic agents
CA2886187C (en) 2012-09-28 2020-04-14 Vanderbilt University Fused heterocyclic compounds as selective bmp inhibitors
MX2015004151A (es) 2012-10-05 2015-07-06 Rigel Pharmaceuticals Inc Inhibidores del factor de diferenciacion de crecimiento-8 (gdf-8).
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
WO2014078479A2 (en) 2012-11-14 2014-05-22 The Board Of Regents Of The University Of Texas System INHIBITION OF HIF-2α HETERODIMERIZATION WITH HIF1β (ARNT)
WO2014084298A1 (ja) 2012-11-28 2014-06-05 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
WO2014085613A1 (en) 2012-11-30 2014-06-05 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
RU2015129087A (ru) 2012-12-19 2017-02-02 Вокхардт Лимитед Стабильная водная композиция, содержащая инсулин человека или его аналог или производное
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
EP2956441A4 (en) 2013-02-18 2016-11-02 Scripps Research Inst MODULATORS OF VASOPRESSIN RECEPTORS WITH THERAPEUTIC POTENTIAL
US8558008B2 (en) 2013-02-28 2013-10-15 Dermira, Inc. Crystalline glycopyrrolate tosylate
WO2014164867A1 (en) 2013-03-11 2014-10-09 Imago Biosciences Kdm1a inhibitors for the treatment of disease
JP2016516399A (ja) 2013-03-13 2016-06-09 オーストラリアン ニュークリア サイエンス アンド テクノロジー オーガニゼーション 非機能性ｔｓｐｏ遺伝子を有するトランスジェニック非ヒト生物
US20140343118A1 (en) 2013-03-14 2014-11-20 Duke University Methods of treatment using arylcyclopropylamine compounds
EP2968343A4 (en) 2013-03-14 2016-11-02 Epizyme Inc COMBINATION THERAPY FOR THE TREATMENT OF CANCER
EP3003301B1 (en) 2013-05-30 2021-02-24 Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas Novel suicidal lsd1 inhibitors targeting sox2-expressing cancer cells
AU2014281398B2 (en) 2013-06-19 2018-10-04 University Of Utah Research Foundation Substituted (E)-N'-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors
SMT202000071T1 (it) 2013-06-21 2020-03-13 Myokardia Inc Composti di pirimidinadione contro le condizioni cardiache
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
US9770514B2 (en) 2013-09-03 2017-09-26 ExxPharma Therapeutics LLC Tamper-resistant pharmaceutical dosage forms
DK3043778T3 (da) 2013-09-13 2017-11-27 Bayer Pharma AG Farmaceutiske sammensætninger, der indeholder refametinib
KR101568724B1 (ko) 2013-11-13 2015-11-12 서울대학교산학협력단 신규한 화합물, 이의 생산 방법, 및 히스톤 디메틸라제 저해제로서 이의 용도
LT3080100T (lt) 2013-12-11 2023-02-27 Celgene Quanticel Research, Inc. Lizinui specifinės demetilazės-1 inhibitoriai
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
US9428470B2 (en) 2014-02-13 2016-08-30 Takeda Pharmaceutical Company Limited Heterocyclic compound
US9346776B2 (en) 2014-02-13 2016-05-24 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
DK3105226T3 (da) 2014-02-13 2019-10-14 Incyte Corp Cyclopropylaminer som lsd1-inhibitorer
PT3105218T (pt) 2014-02-13 2019-12-05 Incyte Corp Ciclopropilaminas como inibidores de lsd1
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015145145A1 (en) 2014-03-24 2015-10-01 Cipla Limited Pharmaceutical composition comprising lapatinib
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
KR102379518B1 (ko) 2014-04-02 2022-03-25 브리스톨-마이어스 스큅 컴퍼니 비아릴 키나제 억제제
WO2015155281A1 (en) 2014-04-11 2015-10-15 Sanovel Ilac Sanayi Ve Ticaret A.S. Pharmaceutical combinations of dabigatran and proton pump inhibitors
EP2929884A1 (en) 2014-04-11 2015-10-14 Sanovel Ilac Sanayi ve Ticaret A.S. Pharmaceutical combinations of dabigatran and h2-receptor antagonists
TN2016000418A1 (en) 2014-04-11 2018-04-04 Takeda Pharmaceuticals Co 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
DK3148974T3 (en) 2014-05-30 2018-10-29 St Europeo Di Oncologia S R L CYCLOPROPYLAMINE COMPOUNDS AS HYDONDEMETHYLASE INHIBITORS
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
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
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
GB201417828D0 (en) 2014-10-08 2014-11-19 Cereno Scient Ab New methods and compositions
CN104173313B (zh) 2014-08-25 2017-05-17 杭州朱养心药业有限公司 利伐沙班片剂药物组合物
JP6653116B2 (ja) 2014-08-27 2020-02-26 日本ケミファ株式会社 オルメサルタンのプロドラッグ製剤
KR102550852B1 (ko) 2014-10-08 2023-07-05 에프. 호프만-라 로슈 아게 알도스테론 신타아제 억제제로서의 스피로다이아민 유도체
WO2016161279A1 (en) 2015-04-03 2016-10-06 Bristol-Myers Squibb Company Inhibitors of indoleamine 2,3-dioxygenase for the treatment of cancer
BR112017020935A2 (pt) 2015-04-03 2018-07-10 Mutabilis ?compostos, composição farmacêutica e conjunto?
EP3626720A1 (en) 2015-04-03 2020-03-25 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
CN112656772B (zh) 2015-10-15 2022-05-20 浙江东日药业有限公司 利伐沙班药物组合物
MX384792B (es) 2015-12-29 2025-03-14 Mirati Therapeutics Inc Inhibidores de desmetilasa especifica de lisina 1 (lsd1).
JPWO2017130933A1 (ja) 2016-01-25 2018-11-29 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
EP3570843A1 (en) 2017-01-18 2019-11-27 Vanderbilt University Fused heterocyclic compounds as selective bmp inhibitors
CN109963854B (zh) 2017-03-16 2022-04-12 江苏恒瑞医药股份有限公司 杂芳基并[4,3-c]嘧啶-5-胺类衍生物、其制备方法及其在医药上的应用
MA53097A (fr) 2018-07-05 2021-05-12 Incyte Corp Dérivés de pyrazine fusionnés en tant qu'inhibiteurs d'a2a/a2b
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012135113A2 (en) * 2011-03-25 2012-10-04 Glaxosmithkline Llc Cyclopropylamines as lsd1 inhibitors

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