BR112015022785A2 - composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt - Google Patents

composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt

Info

Publication number
BR112015022785A2
BR112015022785A2 BR112015022785A BR112015022785A BR112015022785A2 BR 112015022785 A2 BR112015022785 A2 BR 112015022785A2 BR 112015022785 A BR112015022785 A BR 112015022785A BR 112015022785 A BR112015022785 A BR 112015022785A BR 112015022785 A2 BR112015022785 A2 BR 112015022785A2
Authority
BR
Brazil
Prior art keywords
rmt
inhibiting
article
treating
gene expression
Prior art date
Application number
BR112015022785A
Other languages
English (en)
Inventor
Shapiro Gideon
Kalai Swinger Kerren
Helen Mitchell Lorna
Chesworth Richard
Original Assignee
Epizyme Inc
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 Epizyme Inc filed Critical Epizyme Inc
Publication of BR112015022785A2 publication Critical patent/BR112015022785A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/08—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems

Abstract

resumo composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt são descritos aqui compostos da fórmula (i), seus sais farmaceuticamente aceitáveis, e suas composições farmacêuticas. os compostos descritos aqui são úteis para inibir a atividade de arginina metiltransferase. também são descritos métodos de uso dos compostos para o tratamento de distúrbios mediados por arginina metiltransferase. 1/1
BR112015022785A 2013-03-14 2014-03-14 composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt BR112015022785A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361781051P 2013-03-14 2013-03-14
US201361876034P 2013-09-10 2013-09-10
PCT/US2014/029710 WO2014153226A1 (en) 2013-03-14 2014-03-14 Arginine methyltransferase inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
BR112015022785A2 true BR112015022785A2 (pt) 2017-07-18

Family

ID=50483598

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015022785A BR112015022785A2 (pt) 2013-03-14 2014-03-14 composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt

Country Status (25)

Country Link
US (4) US9598374B2 (pt)
EP (1) EP2970132B1 (pt)
JP (1) JP6581076B2 (pt)
KR (2) KR102028793B1 (pt)
CN (2) CN105339351B (pt)
AU (2) AU2014236146B2 (pt)
BR (1) BR112015022785A2 (pt)
CA (1) CA2903394C (pt)
CY (1) CY1123637T1 (pt)
DK (1) DK2970132T3 (pt)
EA (1) EA030481B1 (pt)
ES (1) ES2837034T3 (pt)
HK (1) HK1219736A1 (pt)
HR (1) HRP20202008T1 (pt)
HU (1) HUE052926T2 (pt)
IL (2) IL241368B (pt)
LT (1) LT2970132T (pt)
MX (1) MX2015012850A (pt)
PL (1) PL2970132T3 (pt)
PT (1) PT2970132T (pt)
RS (1) RS61231B1 (pt)
SG (1) SG11201506972PA (pt)
SI (1) SI2970132T1 (pt)
WO (1) WO2014153226A1 (pt)
ZA (1) ZA201507441B (pt)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9604930B2 (en) 2012-12-21 2017-03-28 Epizyme, Inc. Tetrahydro- and dihydro-isoquinoline PRMT5 inhibitors and uses thereof
WO2014100716A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP2935247B1 (en) 2012-12-21 2019-08-28 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US8940726B2 (en) 2012-12-21 2015-01-27 Epizyme, Inc. PRMT5 inhibitors and uses thereof
CA2894126A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US20160031839A1 (en) 2013-03-14 2016-02-04 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970133B1 (en) 2013-03-14 2018-10-24 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014153214A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
WO2014153235A2 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
JP2016518336A (ja) 2013-03-14 2016-06-23 エピザイム，インコーポレイティド Ｐｒｍｔ１阻害剤としてのピラゾール誘導体およびその使用
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970135B1 (en) 2013-03-14 2018-07-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
SG11201506972PA (en) 2013-03-14 2015-10-29 Epizyme Inc Arginine methyltransferase inhibitors and uses thereof
US9776972B2 (en) 2013-03-14 2017-10-03 Epizyme Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9346802B2 (en) 2013-03-15 2016-05-24 Epizyme, Inc. CARM1 inhibitors and uses thereof
US9718816B2 (en) 2013-03-15 2017-08-01 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as CARM1 inhibitors and uses thereof
CA2903813C (en) 2013-03-15 2023-08-29 Epizyme, Inc. Carm1 inhibitors and uses thereof
US10653693B2 (en) 2014-08-04 2020-05-19 Epizyme, Inc. PRMT5 inhibitors and uses thereof
WO2016044576A1 (en) * 2014-09-17 2016-03-24 Epizyme, Inc. Salts, co-crystals, amorphous forms, and crystalline forms of an arginine methyltransferase inhibitor
KR20190090822A (ko) * 2016-12-01 2019-08-02 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 조합 요법
BR112019011388A2 (pt) * 2016-12-01 2019-10-15 Glaxosmithkline Ip Dev Ltd terapia de combinação
CN110225983A (zh) * 2016-12-01 2019-09-10 葛兰素史密斯克莱知识产权发展有限公司 治疗癌症的方法
CN111867584A (zh) * 2018-03-01 2020-10-30 德州大学系统董事会 作为蛋白质精氨酸甲基转移酶的抑制剂的乙二胺-杂环衍生物
CN112469441A (zh) * 2018-05-31 2021-03-09 葛兰素史克知识产权开发有限公司 用icos结合蛋白和精氨酸甲基转移酶抑制剂的组合疗法
WO2020182018A1 (zh) * 2019-03-12 2020-09-17 四川科伦博泰生物医药股份有限公司 氮杂环化合物、其制备方法及用途
EP3947387A4 (en) * 2019-03-25 2022-11-30 California Institute Of Technology PRMT5 INHIBITORS AND USES THEREOF
WO2021023609A1 (en) * 2019-08-02 2021-02-11 Glaxosmithkline Intellectual Property Development Limited Combination of a type i protein arginine methyltransferase (type i prmt) inhibitor and a methionine adenosyltransferase ii alpha (mat2a) inhibitor
CN110950841A (zh) * 2019-11-22 2020-04-03 济南大学 一类新型三唑类化合物的合成及应用
KR102219251B1 (ko) 2020-03-03 2021-02-22 김명수 전문가 추천 플랫폼을 제공하는 서버 및 그 운용방법
CN111481532B (zh) * 2020-06-28 2020-09-22 南京中澳转化医学研究院有限公司 化合物28d在制备提高γ-珠蛋白表达量的药物中的应用

Family Cites Families (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH085859B2 (ja) 1986-07-01 1996-01-24 日本バイエルアグロケム株式会社 新規アルキレンジアミン類
EP0352581A3 (de) 1988-07-28 1990-07-04 F. Hoffmann-La Roche Ag Aethylendiaminmonoamid-Derivate
US5204482A (en) 1988-07-28 1993-04-20 Hoffman-Laroche Inc. Compounds for treating and preventing cognitive diseases and depression and methods of making same
EP0796270A2 (en) 1994-12-02 1997-09-24 Fujisawa Pharmaceutical Co., Ltd. Peptide compounds for prevention and/or treatment of no-mediated diseases
SE9902765D0 (sv) 1999-07-21 1999-07-21 Astra Pharma Prod Novel compounds
CN1331326A (zh) * 2000-06-30 2002-01-16 上海博德基因开发有限公司 一种新的多肽——人精氨酸甲基转移酶(hrmt)32.12和编码这种多肽的多核苷酸
US20020090627A1 (en) 2000-10-05 2002-07-11 Rachel Meyers 27419, a novel human arginine-N-methyl transferase and uses thereof
DE10149370A1 (de) 2001-10-06 2003-04-10 Merck Patent Gmbh Pyrazolderivate
NZ534830A (en) 2002-03-13 2005-08-26 Janssen Pharmaceutica Nv Compounds with histone deacetylase HDAC inhibiting activity and oral bioavailability useful for treating proliferative diseases
GB0219961D0 (en) 2002-08-28 2002-10-02 Pfizer Ltd Oxytocin inhibitors
AU2003288994A1 (en) 2002-12-10 2004-06-30 Ono Pharmaceutical Co., Ltd. Nitrogen-containing heterocyclic compounds and medicinal use thereof
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
DE10315572A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
GB0309637D0 (en) 2003-04-28 2003-06-04 Cancer Rec Tech Ltd Pyrazole compounds
WO2004098634A2 (en) 2003-04-30 2004-11-18 Government Of The United States Of America As Represented By The Sercretary Of The Department Of Health And Human Services National Institutes Of Health Protein arginine n-methyltransferase 2 (prmt-2)
US20050032794A1 (en) 2003-08-05 2005-02-10 Padia Janak K. Diamine derivatives of quinone and uses thereof
DE102004008807A1 (de) 2004-02-20 2005-09-08 Bayer Cropscience Ag Pyrazolopyrimidine
SI1725537T1 (sl) 2004-03-15 2011-11-30 Janssen Pharmaceutica Nv Nove spojine kot modulatorji opioidnih receptorjev
ME01309B (me) 2004-08-26 2013-12-20 Pfizer Pirazolom supstituirani heteroarilni spojevi kao inhibitori proteinskih kinaza
WO2006025832A1 (en) 2004-08-31 2006-03-09 University Of North Carolina At Chapel Hill Dot1 histone methyltransferases as a target for identifying therapeutic agents for leukemia
WO2006033995A2 (en) 2004-09-16 2006-03-30 Valeant Research And Development Thiazolidin-4-ones having anti-hepatitis b activity
JP2008515950A (ja) 2004-10-13 2008-05-15 バイエル・ヘルスケア・アクチェンゲゼルシャフト 泌尿器系障害の処置用の冷メントール受容体−１（ｃｍｒ−１）アンタゴニストとしての４−置換ベンジルオキシ−フェニルメチルアミド誘導体
WO2006063356A1 (en) 2004-12-10 2006-06-15 Isis Phamaceuticals, Inc. Regulation of epigenetic control of gene expression
US20070060589A1 (en) 2004-12-21 2007-03-15 Purandare Ashok V Inhibitors of protein arginine methyl transferases
BRPI0606455A (pt) 2005-01-21 2008-03-11 Astex Therapeutics Ltd compostos farmacêuticos
WO2006113458A1 (en) 2005-04-15 2006-10-26 Bristol-Myers Squibb Company Heterocyclic inhibitors of protein arginine methyl transferases
US8063071B2 (en) 2007-10-31 2011-11-22 GlaxoSmithKline, LLC Chemical compounds
SG140147A1 (en) 2005-08-19 2008-03-28 Aventis Pharma Inc Combination of a hypnotic agent and substituted bis aryl and heteroaryl compound and therapeutic application thereof
EP1985620A4 (en) 2006-02-07 2012-08-15 Taisho Pharmaceutical Co Ltd COMPOUND 10a-AZALIDE
WO2007149782A2 (en) 2006-06-23 2007-12-27 University Of Medicine And Dentistry Of New Jersey Selective inhibitors for transferases
EP2035436B1 (en) 2006-06-26 2011-05-25 UCB Pharma S.A. Fused thiazole derivatives as kinase inhibitors
AU2007273057A1 (en) * 2006-07-12 2008-01-17 Merck Sharp & Dohme Corp. Substituted pyrazoles as ghrelin receptor antagonists
CN101511802A (zh) 2006-09-13 2009-08-19 阿斯利康(瑞典)有限公司 螺唑烷酮化合物及其作为代谢型谷氨酸受体增效剂的用途
NZ575689A (en) 2006-09-15 2011-12-22 Celgene Corp N-methylaminomethyl isoindole compounds and compositions comprising and methods of using the same
US8338437B2 (en) 2007-02-28 2012-12-25 Methylgene Inc. Amines as small molecule inhibitors
US20080312298A1 (en) 2007-04-11 2008-12-18 Kenneth William Foreman Methods for Identification of Modulators of Carm1 Methyl Transferase Activity
US20090062286A1 (en) 2007-05-04 2009-03-05 Kenneth William Foreman Crystal Structure of SMYD3 Protein
US20090012031A1 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan EZH2 Cancer Markers
US8133904B2 (en) 2007-09-07 2012-03-13 Jenrin Discovery, Inc. Cannabinoid receptor antagonists/inverse agonists useful for treating obesity
EP2226315A4 (en) 2007-12-28 2012-01-25 Carna Biosciences Inc 2-AMINOQUINAZOLINE DERIVATIVE
JP2009179616A (ja) 2008-01-31 2009-08-13 Kowa Co ３−ナフチルピラゾール化合物
ES2557281T3 (es) 2008-02-29 2016-01-25 Evotec Ag Compuestos amida, composiciones y usos de los mismos
WO2009126537A1 (en) 2008-04-07 2009-10-15 Syndax Pharmaceuticals, Inc. Administration of an inhibitor of hdac and an hmt inhibitor
US8512944B2 (en) 2008-08-27 2013-08-20 Oncotherapy Science, Inc. PRMT1 for target genes of cancer therapy and diagnosis
WO2010034737A1 (en) 2008-09-24 2010-04-01 Basf Se Pyrazole compounds for controlling invertebrate pests
US8323918B2 (en) 2008-12-12 2012-12-04 University Of South Carolina Chloroacetamidine based inhibitors and activity based probes for the protein arginine methytransferases
WO2010094009A2 (en) 2009-02-13 2010-08-19 Children's Hospital Medical Center Methods and compositions for the treatment of ras associated disorders
US20130345268A1 (en) 2009-02-13 2013-12-26 The Trustees Of Dartmouth College Methods and Compositions for the Treatment of RAS Associated Disorders
EP2221053A1 (de) 2009-02-20 2010-08-25 Albert-Ludwigs-Universität Freiburg Pharmazeutische Zusammensetzung enthaltend Hemmstoffe der Proteinmethyltransferase I und deren Verwendung zur Behandlung von Tumorerkrankungen
RU2011141121A (ru) * 2009-03-11 2013-04-20 Окленд Юнисервисиз Лимитед Пролекарственные формы ингибиторов киназ и их применение в терапии
IN2012DN00352A (pt) 2009-06-16 2015-08-21 Bikam Pharmaceuticals Inc
US20110021362A1 (en) 2009-07-20 2011-01-27 Constellation Pharmaceuticals Agents for stimulating activity of methyl modifying enzymes and methods of use thereof
US9044432B2 (en) 2009-12-22 2015-06-02 Ohio State Innovation Foundation Compositions and methods for cancer detection and treatment
WO2011082098A1 (en) 2009-12-30 2011-07-07 The Rockefeller University Lysine and arginine methyltransferase inhibitors for treating cancer
WO2011096210A1 (en) 2010-02-03 2011-08-11 Oncotherapy Science, Inc. Prmt1 and prmt6 for target genes of cancer therapy and diagnosis
EP2531598A4 (en) 2010-02-03 2013-05-22 Oncotherapy Science Inc WHSC1 AND WHSC1L1 FOR TARGET GENES TO CANCER THERAPY AND DIAGNOSIS
US20110251216A1 (en) 2010-02-19 2011-10-13 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
JP5864545B2 (ja) 2010-05-07 2016-02-17 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ インドール
US8637509B2 (en) 2010-05-07 2014-01-28 Glaxosmithkline Llc Azaindazoles
KR102061353B1 (ko) 2010-09-10 2020-01-02 에피자임, 인코포레이티드 인간 ｅｚｈ2의 억제제 및 이의 사용 방법
WO2012060760A1 (en) 2010-11-05 2012-05-10 Fujirebio Diagnostics Ab Molecular marker for cancer
WO2012068589A2 (en) 2010-11-19 2012-05-24 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
ES2607064T3 (es) 2010-12-01 2017-03-29 Glaxosmithkline Llc Indoles
WO2012082436A2 (en) 2010-12-03 2012-06-21 Epizyme, Inc. Modulators of histone methyltransferase, and methods of use thereof
BR112013013659B8 (pt) 2010-12-03 2024-02-27 Epizyme Inc Compostos moduladores de enzimas epigenéticas, composição farmacêutica compreendendo ditos compostos e usos da dita composição farmacêutica para tratar câncer, câncer hematológico ou leucemia
EP2646441B1 (en) 2010-12-03 2015-12-02 Epizyme, Inc. Carbocycle-substituted purine and 7-deazapurine compounds
KR20130124959A (ko) 2010-12-03 2013-11-15 에피자임, 인코포레이티드 히스톤 메틸전달효소의 7-데아자퓨린 조절제 및 그의 사용방법
AU2012223448B2 (en) 2011-02-28 2017-03-16 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
TW201733984A (zh) 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
US9458174B2 (en) 2012-05-23 2016-10-04 Stemergie Biotechnology Sa Inhibitors of the activity of complex (III) of the mitochondrial electron transport chain and use thereof
WO2014034750A1 (ja) 2012-08-30 2014-03-06 国立大学法人 東京大学 内部寄生虫防除剤
EP3143994A1 (en) 2012-08-30 2017-03-22 The University of Tokyo Endoparasite control agent and use thereof
WO2014100716A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US8940726B2 (en) 2012-12-21 2015-01-27 Epizyme, Inc. PRMT5 inhibitors and uses thereof
EP2935247B1 (en) 2012-12-21 2019-08-28 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2894126A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US9604930B2 (en) 2012-12-21 2017-03-28 Epizyme, Inc. Tetrahydro- and dihydro-isoquinoline PRMT5 inhibitors and uses thereof
WO2014100764A2 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Methods of inhibiting prmt5
EP2970135B1 (en) 2013-03-14 2018-07-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9776972B2 (en) 2013-03-14 2017-10-03 Epizyme Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US20160031839A1 (en) 2013-03-14 2016-02-04 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
SG11201506972PA (en) 2013-03-14 2015-10-29 Epizyme Inc Arginine methyltransferase inhibitors and uses thereof
JP2016518336A (ja) 2013-03-14 2016-06-23 エピザイム，インコーポレイティド Ｐｒｍｔ１阻害剤としてのピラゾール誘導体およびその使用
EP2970133B1 (en) 2013-03-14 2018-10-24 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153214A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyl transferase inhibtors and uses thereof
WO2014153235A2 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9346802B2 (en) 2013-03-15 2016-05-24 Epizyme, Inc. CARM1 inhibitors and uses thereof
CA2903813C (en) 2013-03-15 2023-08-29 Epizyme, Inc. Carm1 inhibitors and uses thereof
US9718816B2 (en) 2013-03-15 2017-08-01 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as CARM1 inhibitors and uses thereof
US20170210751A1 (en) 2014-06-25 2017-07-27 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP3160477A4 (en) 2014-06-25 2018-07-04 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US10653693B2 (en) 2014-08-04 2020-05-19 Epizyme, Inc. PRMT5 inhibitors and uses thereof
WO2016044641A2 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
US20170291905A1 (en) 2014-09-17 2017-10-12 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US20170305922A1 (en) 2014-09-17 2017-10-26 Epizyme, Inc. Carm1 inhibitors and uses thereof
WO2016044585A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP3200588A4 (en) 2014-09-17 2018-04-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US20170283440A1 (en) 2014-09-17 2017-10-05 Epizyme, Inc. Carm1 inhibitors and uses thereof
WO2016044576A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Salts, co-crystals, amorphous forms, and crystalline forms of an arginine methyltransferase inhibitor
JP2017527594A (ja) 2014-09-17 2017-09-21 エピザイム，インコーポレイティド コアクチベーター関連アルギニンメチルトランスフェラーゼ１（ｃａｒｍ１）阻害剤の塩、共結晶、非晶質形態、および結晶形態
WO2017136699A1 (en) 2016-02-05 2017-08-10 Epizyme, Inc Arginine methyltransferase inhibitors and uses thereof
US20190083482A1 (en) 2017-09-18 2019-03-21 Epizyme, Inc. Prmt5 inhibitors and uses thereof

Also Published As

Publication number Publication date
KR102158756B1 (ko) 2020-09-23
JP2016516067A (ja) 2016-06-02
SG11201506972PA (en) 2015-10-29
PL2970132T3 (pl) 2021-04-06
CN105339351A (zh) 2016-02-17
IL268189A (en) 2019-09-26
US20170267642A1 (en) 2017-09-21
CN109265400B (zh) 2022-10-04
IL241368B (en) 2019-07-31
DK2970132T3 (da) 2020-12-21
MX2015012850A (es) 2016-06-24
CN109265400A (zh) 2019-01-25
KR20160003648A (ko) 2016-01-11
US20190100496A1 (en) 2019-04-04
HUE052926T2 (hu) 2021-05-28
EA201591531A1 (ru) 2016-02-29
SI2970132T1 (sl) 2021-02-26
JP6581076B2 (ja) 2019-09-25
AU2018203056A1 (en) 2018-07-19
CN105339351B (zh) 2018-11-06
IL241368A0 (en) 2015-11-30
HK1219736A1 (zh) 2017-04-13
PT2970132T (pt) 2020-12-30
KR20190112334A (ko) 2019-10-04
CA2903394C (en) 2021-08-31
EA030481B1 (ru) 2018-08-31
CY1123637T1 (el) 2022-03-24
US11512053B2 (en) 2022-11-29
US10081603B2 (en) 2018-09-25
WO2014153226A1 (en) 2014-09-25
US10800743B2 (en) 2020-10-13
AU2018203056B2 (en) 2020-05-21
US20210078951A1 (en) 2021-03-18
LT2970132T (lt) 2021-01-11
CA2903394A1 (en) 2014-09-25
KR102028793B1 (ko) 2019-10-07
ES2837034T3 (es) 2021-06-29
HRP20202008T1 (hr) 2021-02-19
EP2970132A1 (en) 2016-01-20
EP2970132B1 (en) 2020-09-23
RS61231B1 (sr) 2021-01-29
AU2014236146B2 (en) 2018-05-17
AU2014236146A1 (en) 2015-09-10
ZA201507441B (en) 2021-01-27
US20160024016A1 (en) 2016-01-28
IL268189B (en) 2022-02-01
US9598374B2 (en) 2017-03-21
WO2014153226A9 (en) 2015-01-08

Similar Documents

Publication Publication Date Title
BR112015022785A2 (pt) composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
BR112022004248A2 (pt) Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, método para inibir a atividade de prmt5 em uma célula, e, método para o tratamento de câncer
BR112019003504A2 (pt) compostos de amino-pirrolopirimidinona e métodos de uso dos mesmos
BR112015014590A2 (pt) composto; composição farmacêutica; estojo ou farmacêutico empacotado; método de inibição de prmt5; método de alteração da expressão de genes; método de alteração da transcrição; e método de tratamento ou prevenção de um distúrbio mediado por prmt5
BR112018070123A2 (pt) oxiesterós e métodos de uso dos mesmos
BR112015022787A2 (pt) compostos, composições farmacêuticas, kit ou artigo farmacêutico embalado, e método de tratamento de um distúrbio mediado por carm1
EA201891191A1 (ru) 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
WO2014153235A3 (en) Arginine methyltransferase inhibitors and uses thereof
WO2014153100A3 (en) Arginine methyltransferase inhibitors and uses thereof
BR112015022462A8 (pt) inibidores de ido, composição farmacêutica, método de inibição de atividade de indolamina 2,3-dioxigenase e uso dos referidos inibidores
WO2016044556A3 (en) Arginine methyltransferase inhibitors and uses thereof
BR112015021999A8 (pt) inibidores de indoleamina 2,3-dioxigenase (ido), seus usos, composição farmacêutica, e método para inibir a atiavidade de indoleamina 2,3-dioxigenase
CO7160104A2 (es) Inhibidores de virus de hepatitis c
BR112016028818A2 (pt) composição farmacêutica, métodos de tratamento de uma doença ou condição, de inibição da atividade de um polipeptídeo de fosfatidilinositol 3-quinase e de inibição de reações imunes excessivas ou destrutivas ou crescimento ou proliferação de células cancerosas, kit, composto, sal, isômero, ou uma mistura farmaceuticamente aceitável do mesmo, e, uso de um composto, um sal, isômero, ou uma mistura farmaceuticamente aceitável do mesmo.
BR112016028642A2 (pt) composto, composição farmacêutica, método de tratamento de uma doença ou condição, método de inibição da atividade de um polipeptídeo de fosfatidilinositol 3-quinase, método de inibição de reações imunes ou crescimento excessivo ou destrutivo ou de proliferação de células cancerosas, kit, e, uso de um composto, de um sal, de um isômero ou de uma mistura farmaceuticamente aceitável do mesmo.
BR112014026493A2 (pt) derivados de imidazotiadiazol como inibidores do receptor ativado por protease 4 (par4) para tratar a agregação de plaqueta
BR112016029846A2 (pt) ?composto, composição farmacêutica, métodos para o método para tratamento de um humano, para inibição da atividade de um polipeptídio de fosfatidilinositol 3-quinase e inibição excessiva ou reações imunes destrutivas ou crescimento ou uma proliferação de células de câncer, kit, e, uso de um composto, um sal farmaceuticamente aceitável, isômero, ou uma mistura do mesmo?
BR112015032595A2 (pt) inibidores de ido
EA201890086A1 (ru) 1,4-замещенные производные пиперидина
BR112013001632A2 (pt) composto, composição farmacêutica, método de inibir uma atividade uma jak quinase in vitro, uso de um composto, ou da composição farmacêutica, e, método de fabricar um composto
BR112016000489A8 (pt) composto, composição farmacêutica que o compreende, uso da composição e métodos para fabricar compostos
BR112016028876A2 (pt) composto, composição farmacêutica, método para tratar uma doença ou condição em um ser humano, kit, e, uso de um composto, um sal, isômero ou uma mistura farmaceuticamente aceitável dos mesmos.
BR112014026643A8 (pt) derivados de imidazotiadiazol e imidazopirazina como inibidores de receptor 4 ativado por protease (par4) para o tratamento de agregação de plaqueta, seus usos e composição farmacêutica
BR112014010420A2 (pt) inibidores de pak para o tratamento de distúrbios proliferativos celulares
BR112015020139A2 (pt) compostos terapêuticos e usos dos mesmos

Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]
B12B Appeal against refusal [chapter 12.2 patent gazette]