EA201591532A1 - Ингибиторы carm1 и их применение - Google Patents

Ингибиторы carm1 и их применение

Info

Publication number
EA201591532A1
EA201591532A1 EA201591532A EA201591532A EA201591532A1 EA 201591532 A1 EA201591532 A1 EA 201591532A1 EA 201591532 A EA201591532 A EA 201591532A EA 201591532 A EA201591532 A EA 201591532A EA 201591532 A1 EA201591532 A1 EA 201591532A1
Authority
EA
Eurasian Patent Office
Prior art keywords
carm1
compounds
application
formula
inhibitors
Prior art date
Application number
EA201591532A
Other languages
English (en)
Inventor
Ричард Чесуорт
Оскар Мигель Морадей
Гидеон Шапиро
Лей Дзин
Роберт И. Бабин
Original Assignee
Эпизим, Инк.
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 Эпизим, Инк. filed Critical Эпизим, Инк.
Publication of EA201591532A1 publication Critical patent/EA201591532A1/ru

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
    • C07D487/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/10Spiro-condensed systems
    • 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
    • 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Epidemiology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

В настоящем документе представлены соединения формулы (I)и их фармацевтически приемлемые соли, и фармацевтические композиции с ними; где X, R, R, R, R, R, Rопределены в настоящем документе, и кольцо НЕТ является 6-членной моноциклической гетероарильной кольцевой системой с формулойгде L, R, G, G, Gи Gопределены в настоящем документе. Соединения в соответствии с настоящим изобретением применимы для ингибирования активности CARM1. Также описываются способы применения соединений для лечения опосредованных CARM1 нарушений.
EA201591532A 2013-03-15 2014-03-14 Ингибиторы carm1 и их применение EA201591532A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361794442P 2013-03-15 2013-03-15
US201461937333P 2014-02-07 2014-02-07
PCT/US2014/028463 WO2014144169A1 (en) 2013-03-15 2014-03-14 Carm1 inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
EA201591532A1 true EA201591532A1 (ru) 2016-03-31

Family

ID=50687649

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201591532A EA201591532A1 (ru) 2013-03-15 2014-03-14 Ингибиторы carm1 и их применение

Country Status (14)

Country Link
US (6) US9738651B2 (ru)
EP (1) EP2970219B1 (ru)
JP (2) JP2016519078A (ru)
KR (1) KR20160003647A (ru)
CN (1) CN105228997B (ru)
AU (2) AU2014227775B2 (ru)
BR (1) BR112015022787A2 (ru)
CA (1) CA2903813C (ru)
EA (1) EA201591532A1 (ru)
HK (1) HK1219947A1 (ru)
IL (1) IL241370A0 (ru)
MX (1) MX2015012803A (ru)
SG (1) SG11201507070XA (ru)
WO (1) WO2014144169A1 (ru)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE034925T2 (en) * 2011-09-02 2018-03-28 Purdue Pharma Lp Pyrimidines as sodium channel blockers
CA2894157A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP2935240A1 (en) 2012-12-21 2015-10-28 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP2935241A1 (en) 2012-12-21 2015-10-28 Epizyme, Inc. Prmt5 inhibitors and uses thereof
PT2935222T (pt) 2012-12-21 2018-12-10 Epizyme Inc Inibidores de prmt5 e seus usos
US8940726B2 (en) 2012-12-21 2015-01-27 Epizyme, Inc. PRMT5 inhibitors and uses thereof
EP2970135B1 (en) 2013-03-14 2018-07-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9598374B2 (en) 2013-03-14 2017-03-21 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9765035B2 (en) 2013-03-14 2017-09-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
AU2014260433A1 (en) 2013-03-14 2015-09-10 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
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9045455B2 (en) 2013-03-14 2015-06-02 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
BR112015022787A2 (pt) * 2013-03-15 2017-11-07 Epizyme Inc compostos, composições farmacêuticas, kit ou artigo farmacêutico embalado, e método de tratamento de um distúrbio mediado por carm1
EP2970266B1 (en) 2013-03-15 2018-01-31 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
CA2953572A1 (en) 2014-08-04 2016-02-11 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP3194398A4 (en) * 2014-09-17 2018-02-21 Epizyme, Inc. Salts, co-crystals, amorphous forms, and crystalline forms of a co-activator-associated arginine methyltransferase 1 (carm1) inhibitor
JP2017530959A (ja) * 2014-09-17 2017-10-19 エピザイム,インコーポレイティド Carm1阻害剤およびその使用
WO2017007755A1 (en) 2015-07-06 2017-01-12 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
PL3319959T3 (pl) 2015-07-06 2022-02-14 Alkermes, Inc. Hetero-haloinhibitory deacetylazy histonowej
AU2017324942B2 (en) * 2016-09-07 2022-01-27 The Regents Of The University Of California Allosteric corticotropin-releasing factor receptor 1 (CRFR1) antagonists that decrease p-Tau and improve cognition
US11160823B2 (en) 2016-11-07 2021-11-02 University Of Massachusetts Therapeutic targets for facioscapulohumeral muscular dystrophy
EP3568135B1 (en) 2017-01-11 2021-04-07 Alkermes, Inc. Bicyclic inhibitors of histone deacetylase
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
CN110382482A (zh) 2017-01-26 2019-10-25 亚瑞克西斯制药公司 稠合的杂-杂二环化合物及其使用方法
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
US10745385B2 (en) 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
JP7152471B2 (ja) 2017-08-07 2022-10-12 ロダン・セラピューティクス,インコーポレーテッド ヒストン脱アセチル化酵素の二環阻害剤
CN112584833A (zh) * 2018-08-01 2021-03-30 亚瑞克西斯制药公司 杂环螺化合物及其用于治疗癌症的使用方法
CN112007032B (zh) * 2020-09-16 2021-10-22 厦门大学 化合物在制备小分子抑制剂或治疗癌症的药物中的应用及小分子抑制剂和治疗癌症的药物

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB148830A (en) 1918-12-04 1921-11-10 Aegir Electrische Bordapp Und Device for signalling liquid levels at a distance
US4011321A (en) 1973-12-19 1977-03-08 Smith Kline & French Laboratories Limited Pharmaceutical compositions and methods of inhibiting β-adrenergic receptors
GB1488330A (en) 1973-12-19 1977-10-12 Smith Kline French Lab Dihydropyridazinones
GB1464242A (en) 1974-04-18 1977-02-09 Smithkline Corp Benzoyl benzofurans and compositions comprising them
US4001426A (en) 1974-10-17 1977-01-04 Smithkline Corporation Substituted benzofurans and benzothiophenes
GB1548601A (en) 1976-03-29 1979-07-18 Smith Kline French Lab Pyridazines
US4728651A (en) 1985-10-24 1988-03-01 Hoechst-Roussel Pharmaceuticals Inc. Antihypertensive thieno-isoxazoles and -pyrazoles
US5221675A (en) 1989-12-15 1993-06-22 Abbott Laboratories Aza-spirocyclic compounds that enhance cholinergic neurotransmission
GB9325217D0 (en) * 1993-12-09 1994-02-09 Zeneca Ltd Pyrimidine derivatives
SK286123B6 (sk) * 1998-05-15 2008-04-07 Astrazeneca Ab Benzamidové deriváty, spôsob ich prípravy, farmaceutická kompozícia a ich použitie na prípravu liečiva na liečenie chorôb sprostredkovaných cytokínmi
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
WO2001030780A2 (en) 1999-10-27 2001-05-03 Cor Therapeutics, Inc. Pyridyl-containing spirocyclic compounds as inhibitors of fibrinogen-dependent platelet aggregation
GB0004886D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
DE10010067A1 (de) 2000-03-02 2001-09-06 Bayer Ag Neue Imidazotriazinone und ihre Verwendung
CN1441800A (zh) 2000-07-13 2003-09-10 伊莱利利公司 β3肾上腺素能激动剂
US6864267B2 (en) 2001-07-16 2005-03-08 Smithkline Beecham Corporation Calcilytic compounds
AU2003297431A1 (en) * 2002-12-20 2004-07-22 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
AU2004218456A1 (en) 2003-02-28 2004-09-16 Encysive Pharmaceuticals Inc. Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists.
US7408008B2 (en) 2003-12-09 2008-08-05 Janssen Pharmaceutica, N.V. Method of producing highly functionalized 1,3-diamino-propan-2-ols from solid support
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
AR057579A1 (es) 2005-11-23 2007-12-05 Merck & Co Inc Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac)
FR2904827B1 (fr) * 2006-08-11 2008-09-19 Sanofi Aventis Sa Derives de 5,6-bisaryl-2-pyridine-carboxamide, leur preparation et leur application en therapeutique comme antiganistes des recepteurs a l'urotensine ii
WO2008032191A2 (en) 2006-09-13 2008-03-20 Astrazeneca Ab Spiro-oxazolidinone compounds and their use as metabotropic glutamate receptor potentiators
EP2137158A4 (en) 2007-02-28 2012-04-18 Methylgene Inc LOW-MOLECULAR INHIBITORS OF PROTEINARGININE METHYLTRANSFERASES (PRMTS)
MX2010009561A (es) 2008-02-29 2010-09-24 Renovis Inc Compuestos amida, composiciones y usos de los mismos.
US20100144722A1 (en) 2008-09-03 2010-06-10 Dr. Reddy's Laboratories Ltd. Novel heterocyclic compounds as gata modulators
WO2010120994A2 (en) * 2009-04-17 2010-10-21 Wyeth Llc Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis
JP2013107824A (ja) 2010-03-17 2013-06-06 Dainippon Sumitomo Pharma Co Ltd 新規単環ピリミジン誘導体
JP5970003B2 (ja) 2011-03-04 2016-08-17 ローカス ファーマシューティカルズ インコーポレイテッド アミノピラジン化合物
CA2833169A1 (en) 2011-04-15 2012-12-20 Rib-X Pharmaceuticals, Inc. Antimicrobial compounds and methods of making and using the same
CN103841657B (zh) 2012-11-21 2018-08-14 中兴通讯股份有限公司 一种本地ip访问连接的释放方法和mrn
EP2935241A1 (en) 2012-12-21 2015-10-28 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2894157A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2014100764A2 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Methods of inhibiting prmt5
US8940726B2 (en) 2012-12-21 2015-01-27 Epizyme, Inc. PRMT5 inhibitors and uses thereof
PT2935222T (pt) 2012-12-21 2018-12-10 Epizyme Inc Inibidores de prmt5 e seus usos
EP2935240A1 (en) 2012-12-21 2015-10-28 Epizyme, Inc. Prmt5 inhibitors and uses thereof
TWI644899B (zh) 2013-02-04 2018-12-21 健生藥品公司 Flap調節劑
US9365527B2 (en) 2013-03-14 2016-06-14 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9447079B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. PRMT1 inhibitors and uses thereof
US9045455B2 (en) 2013-03-14 2015-06-02 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9765035B2 (en) 2013-03-14 2017-09-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
AU2014260433A1 (en) 2013-03-14 2015-09-10 Epizyme, Inc. Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof
US9598374B2 (en) 2013-03-14 2017-03-21 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153090A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives asprmt1 inhibitors and uses thereof
EP2970135B1 (en) 2013-03-14 2018-07-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
BR112015022787A2 (pt) 2013-03-15 2017-11-07 Epizyme Inc compostos, composições farmacêuticas, kit ou artigo farmacêutico embalado, e método de tratamento de um distúrbio mediado por carm1
US9346802B2 (en) 2013-03-15 2016-05-24 Epizyme, Inc. CARM1 inhibitors and uses thereof
EP2970266B1 (en) 2013-03-15 2018-01-31 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof
EP3160466A4 (en) 2014-06-25 2017-12-27 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US20170198006A1 (en) 2014-06-25 2017-07-13 Epizyme, Inc. Prmt5 inhibitors and uses thereof
CA2953572A1 (en) 2014-08-04 2016-02-11 Epizyme, Inc. Prmt5 inhibitors and uses thereof
JP2017530959A (ja) * 2014-09-17 2017-10-19 エピザイム,インコーポレイティド Carm1阻害剤およびその使用
WO2016044641A2 (en) 2014-09-17 2016-03-24 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
BR112017005393A2 (pt) 2014-09-17 2017-12-05 Genentech Inc composto de fórmula i, método de preparação de um conjugado de fórmula a, conjugado de fórmula a1, composição compreendendo uma mistura dos compostos de conjugado de anticorpo-fármaco, composição farmacêutica, e uso de um conjugado ou de uma composição
US20170291905A1 (en) 2014-09-17 2017-10-12 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US20170280720A1 (en) 2014-09-17 2017-10-05 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP3200588A4 (en) 2014-09-17 2018-04-25 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2016044650A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
EP3194398A4 (en) 2014-09-17 2018-02-21 Epizyme, Inc. Salts, co-crystals, amorphous forms, and crystalline forms of a co-activator-associated arginine methyltransferase 1 (carm1) inhibitor
WO2017136699A1 (en) 2016-02-05 2017-08-10 Epizyme, Inc Arginine methyltransferase inhibitors and uses thereof
KR20190040971A (ko) 2016-07-25 2019-04-19 에피자임, 인코포레이티드 Crebbp 관련 암 치료법
US20190083482A1 (en) 2017-09-18 2019-03-21 Epizyme, Inc. Prmt5 inhibitors and uses thereof

Also Published As

Publication number Publication date
AU2014227775B2 (en) 2018-05-31
AU2018211214A1 (en) 2018-08-23
US20190135819A1 (en) 2019-05-09
US20160039834A1 (en) 2016-02-11
US20230279020A9 (en) 2023-09-07
JP2018118994A (ja) 2018-08-02
CA2903813A1 (en) 2014-09-18
US20210155631A1 (en) 2021-05-27
US10633389B2 (en) 2020-04-28
MX2015012803A (es) 2016-08-19
US10118931B2 (en) 2018-11-06
BR112015022787A2 (pt) 2017-11-07
KR20160003647A (ko) 2016-01-11
EP2970219A1 (en) 2016-01-20
EP2970219B1 (en) 2019-02-27
US20230416263A1 (en) 2023-12-28
US20170320883A1 (en) 2017-11-09
US9856267B2 (en) 2018-01-02
SG11201507070XA (en) 2015-10-29
AU2014227775A1 (en) 2015-09-10
WO2014144169A1 (en) 2014-09-18
HK1219947A1 (zh) 2017-04-21
US9738651B2 (en) 2017-08-22
IL241370A0 (en) 2015-11-30
US20180282343A1 (en) 2018-10-04
JP2016519078A (ja) 2016-06-30
CA2903813C (en) 2023-08-29
CN105228997B (zh) 2018-03-27
US11834455B2 (en) 2023-12-05
CN105228997A (zh) 2016-01-06

Similar Documents

Publication Publication Date Title
EA201591532A1 (ru) Ингибиторы carm1 и их применение
EA201591531A1 (ru) Ингибиторы аргининметилтрансферазы и их применения
PH12020550552A1 (en) Inhibitors of hepatitis c virus
GEP201706671B (en) Heterocyclyl compounds as mek inhibitors
EA201891191A1 (ru) 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
EA201590975A1 (ru) Ингибиторы prmt5 и их применение
EA201791955A1 (ru) ИНГИБИТОРЫ TGF-β
CL2015003200A1 (es) Potenciador de inhibidores del homólogo de zeste
EA201691803A1 (ru) Ингибиторы калликреина плазмы человека
EA201690669A1 (ru) Замещенные производные хинолизина, которые можно использовать как ингибиторы интегразы вич
WO2016044641A3 (en) Carm1 inhibitors and uses thereof
EA201690223A1 (ru) Ингибиторы фактора в комплемента на основе производных пиперидинилиндола и их применение
EA201690752A1 (ru) Ингибиторы g12c kras
EA201491824A1 (ru) Производные бензамида для ингибирования активности abl1, abl2 и bcr-abl1
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
EA201592182A1 (ru) Ингибиторы фосфатидилинозитол-3-киназы
WO2014153100A3 (en) Arginine methyltransferase inhibitors and uses thereof
WO2014153235A3 (en) Arginine methyltransferase inhibitors and uses thereof
EA201690094A1 (ru) Ингибиторы syk
EA201891553A1 (ru) Ингибиторы syk
EA201891063A1 (ru) Производные дигидроимидазопиразинона, применимые в лечении рака
EA201690687A1 (ru) Ингибиторы репликации вируса иммунодефицита
EA201591301A1 (ru) Новые пиримидиновые и пиридиновые соединения и их применение
EA201591360A1 (ru) Азабензимидазолы в качестве ингибиторов изозимов фдэ4 для лечения цнс и других расстройств
EA201692003A1 (ru) Макроциклические производные пиримидина