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)
Russian (ru)
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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/10—Spiro-condensed systems
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D405/12—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
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged systems
    • 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
    • C07D493/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (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)
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 (13)

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

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9163008B2 (en) * 2011-09-02 2015-10-20 Purdue Pharma, L.P. Pyrimidines as sodium channel blockers
US9365555B2 (en) 2012-12-21 2016-06-14 Epizyme, Inc. PRMT5 inhibitors and uses thereof
JP2016505002A (ja) 2012-12-21 2016-02-18 エピザイム，インコーポレイティド ジヒドロイソキノリンまたはテトラヒドロイソキノリンを含有するｐｒｍｔ５阻害剤およびその使用
US10118918B2 (en) 2012-12-21 2018-11-06 Epizyme, Inc. PRMT5 inhibitors and uses thereof
US9908887B2 (en) 2012-12-21 2018-03-06 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
CA2903394C (en) 2013-03-14 2021-08-31 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9394258B2 (en) 2013-03-14 2016-07-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
JP2016514164A (ja) 2013-03-14 2016-05-19 エピザイム，インコーポレイティド アルギニンメチルトランスフェラーゼ阻害剤としてのピラゾール誘導体およびその使用
EP2970135B1 (en) 2013-03-14 2018-07-18 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2014153172A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
WO2014144169A1 (en) * 2013-03-15 2014-09-18 Epizyme, Inc. Carm1 inhibitors and uses thereof
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
EP2970266B1 (en) 2013-03-15 2018-01-31 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
AU2015301196A1 (en) 2014-08-04 2017-01-12 Epizyme, Inc. PRMT5 inhibitors and uses thereof
US20170298073A1 (en) * 2014-09-17 2017-10-19 Epizyme, Inc Salts, co-crystals, amorphous forms, and crystalline forms of a co-activator-associated arginine methyltransferase 1 (carm1) inhibitor
WO2016044604A1 (en) * 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
HUE057041T2 (hu) 2015-07-06 2022-04-28 Alkermes Inc Hiszton deacetiláz hetero-halogén gátlói
WO2017007755A1 (en) 2015-07-06 2017-01-12 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
EP3510029B1 (en) * 2016-09-07 2025-11-05 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
HRP20220223T1 (hr) 2017-01-11 2022-04-29 Alkermes, Inc. Biciklički inhibitori histon deacetilaze
EP3573971A1 (en) 2017-01-26 2019-12-04 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
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
CN110869358A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 Kras的共价抑制剂
US11225475B2 (en) 2017-08-07 2022-01-18 Alkermes, Inc. Substituted pyridines as inhibitors of histone deacetylase
BR112021001709A2 (pt) * 2018-08-01 2021-05-04 Araxes Pharma Llc compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer
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
GB1488330A (en) 1973-12-19 1977-10-12 Smith Kline French Lab Dihydropyridazinones
US4011321A (en) 1973-12-19 1977-03-08 Smith Kline & French Laboratories Limited Pharmaceutical compositions and methods of inhibiting β-adrenergic receptors
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
US6579872B1 (en) * 1998-05-15 2003-06-17 Astrazeneca Ab Bezamide derivatives for the treatment of diseases mediated by cytokines
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
HUP0301329A2 (hu) 2000-07-13 2003-08-28 Eli Lilly And Co. Béta3 Adrenergiás agonisták, valamint ezen vegyületeket tartalmazó gyógyászati készítmények és eljárás e vegyületek előállítására
US6864267B2 (en) 2001-07-16 2005-03-08 Smithkline Beecham Corporation Calcilytic compounds
BR0317430A (pt) * 2002-12-20 2005-10-25 Pharmacia Corp Compostos inibidores de quinase-2 de proteìna ativada por quinase de proteìna ativada por mitógeno
JP2006519258A (ja) 2003-02-28 2006-08-24 エンサイシブ・ファーマシューティカルズ・インコーポレイテッド ピリジン、ピリミジン、キノリン、キナゾリンおよびナフタレン系のウロテンシン−ｉｉ受容体拮抗薬
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
US20060235037A1 (en) 2005-04-15 2006-10-19 Purandare Ashok V 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
JP2010503656A (ja) 2006-09-13 2010-02-04 アストラゼネカ アクチボラグ スピロ−オキサゾリジノン化合物と代謝共役型グルタミン酸受容体ポテンシエーターとしてのその使用
US8338437B2 (en) 2007-02-28 2012-12-25 Methylgene Inc. Amines as small molecule inhibitors
WO2009110985A2 (en) 2008-02-29 2009-09-11 Renovis, Inc. Amide compounds, compositions and uses thereof
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
EP3404028A1 (en) 2011-04-15 2018-11-21 Melinta Therapeutics, Inc. Methods of making antimicrobial compounds
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
US10118918B2 (en) 2012-12-21 2018-11-06 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
US9365555B2 (en) 2012-12-21 2016-06-14 Epizyme, Inc. PRMT5 inhibitors and uses thereof
WO2014100764A2 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Methods of inhibiting prmt5
JP2016505002A (ja) 2012-12-21 2016-02-18 エピザイム，インコーポレイティド ジヒドロイソキノリンまたはテトラヒドロイソキノリンを含有するｐｒｍｔ５阻害剤およびその使用
US9908887B2 (en) 2012-12-21 2018-03-06 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
US9394258B2 (en) 2013-03-14 2016-07-19 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP3363434A1 (en) 2013-03-14 2018-08-22 Epizyme Inc Arginine methyltransferase inhibitors and uses thereof
WO2014153172A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
JP2016514164A (ja) 2013-03-14 2016-05-19 エピザイム，インコーポレイティド アルギニンメチルトランスフェラーゼ阻害剤としてのピラゾール誘導体およびその使用
US20160039767A1 (en) 2013-03-14 2016-02-11 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
CA2903394C (en) 2013-03-14 2021-08-31 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
US9346802B2 (en) 2013-03-15 2016-05-24 Epizyme, Inc. CARM1 inhibitors and uses thereof
WO2014144169A1 (en) 2013-03-15 2014-09-18 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
WO2015200680A2 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Prmt5 inhibitors and uses thereof
AU2015301196A1 (en) 2014-08-04 2017-01-12 Epizyme, Inc. PRMT5 inhibitors and uses thereof
WO2016044650A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
US20170283400A1 (en) 2014-09-17 2017-10-05 Epizyme, Inc. Arginine methyltransferase 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
US20170280720A1 (en) 2014-09-17 2017-10-05 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
JP2017533887A (ja) 2014-09-17 2017-11-16 ジェネンテック， インコーポレイテッド ピロロベンゾジアゼピン類及びその抗体ジスルフィドコンジュゲート
WO2016044626A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2016044641A2 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
US20170298073A1 (en) 2014-09-17 2017-10-19 Epizyme, Inc Salts, co-crystals, amorphous forms, and crystalline forms of a co-activator-associated arginine methyltransferase 1 (carm1) inhibitor
WO2016044604A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
WO2017136699A1 (en) 2016-02-05 2017-08-10 Epizyme, Inc Arginine methyltransferase inhibitors and uses thereof
JP2019524740A (ja) 2016-07-25 2019-09-05 エピザイム インコーポレイテッド Ｃｒｅｂｂｐ関連癌の治療法
US20190083482A1 (en) 2017-09-18 2019-03-21 Epizyme, Inc. Prmt5 inhibitors and uses thereof

Also Published As

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

Similar Documents

Publication Publication Date Title
EA201591531A1 (ru) Ингибиторы аргининметилтрансферазы и их применения
PH12020550552A1 (en) Inhibitors of hepatitis c virus
GEP201706671B (en) Heterocyclyl compounds as mek inhibitors
EA201791955A1 (ru) ИНГИБИТОРЫ TGF-β
EA201590975A1 (ru) Ингибиторы prmt5 и их применение
EA201690669A8 (ru) Замещенные производные хинолизина, которые можно использовать как ингибиторы интегразы вич
EA201691803A1 (ru) Ингибиторы калликреина плазмы человека
MX2015012803A (es) Inhibidores de la carm1 y usos de los mismos.
WO2016044641A3 (en) Carm1 inhibitors and uses thereof
CL2015003200A1 (es) Potenciador de inhibidores del homólogo de zeste
EA201891191A1 (ru) 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
EA201690223A1 (ru) Ингибиторы фактора в комплемента на основе производных пиперидинилиндола и их применение
EA201491824A1 (ru) Производные бензамида для ингибирования активности abl1, abl2 и bcr-abl1
EA201690752A1 (ru) Ингибиторы g12c kras
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
WO2014153100A3 (en) Arginine methyltransferase inhibitors and uses thereof
EA201690687A1 (ru) Ингибиторы репликации вируса иммунодефицита
EA201592182A1 (ru) Ингибиторы фосфатидилинозитол-3-киназы
WO2014153235A3 (en) Arginine methyltransferase inhibitors and uses thereof
EA201690094A1 (ru) Ингибиторы syk
EA201591360A1 (ru) Азабензимидазолы в качестве ингибиторов изозимов фдэ4 для лечения цнс и других расстройств
EA029499B9 (ru) Ингибиторы rorc2 и способы их применения
EA201692003A1 (ru) Макроциклические производные пиримидина
EA201591301A1 (ru) Новые пиримидиновые и пиридиновые соединения и их применение
EA201690844A1 (ru) Ингибиторы gsk-3