JP2016519078A - Ｃａｒｍ１阻害剤およびその使用 - Google Patents

Ｃａｒｍ１阻害剤およびその使用 Download PDF

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JP2016519078A
JP2016519078A JP2016502796A JP2016502796A JP2016519078A JP 2016519078 A JP2016519078 A JP 2016519078A JP 2016502796 A JP2016502796 A JP 2016502796A JP 2016502796 A JP2016502796 A JP 2016502796A JP 2016519078 A JP2016519078 A JP 2016519078A
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optionally substituted
certain embodiments
hydrogen
alkyl
ring
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JP2016519078A5 (enExample
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チェスウォース リチャード
チェスウォース リチャード
ミゲル モラデル オスカー
ミゲル モラデル オスカー
シャピロ ジディオン
シャピロ ジディオン
ジン レイ
ジン レイ
イー．バービン ロバート
イー．バービン ロバート
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エピザイム，インコーポレイティド
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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

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  • Veterinary Medicine (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (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)
JP2016502796A 2013-03-15 2014-03-14 Ｃａｒｍ１阻害剤およびその使用 Pending JP2016519078A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361794442P 2013-03-15 2013-03-15
US61/794,442 2013-03-15
US201461937333P 2014-02-07 2014-02-07
US61/937,333 2014-02-07
PCT/US2014/028463 WO2014144169A1 (en) 2013-03-15 2014-03-14 Carm1 inhibitors and uses thereof

Related Child Applications (1)

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JP2018071070A Division JP2018118994A (ja) 2013-03-15 2018-04-02 Ｃａｒｍ１阻害剤およびその使用

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JP2016519078A true JP2016519078A (ja) 2016-06-30
JP2016519078A5 JP2016519078A5 (enExample) 2017-02-02

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JP2018071070A Pending JP2018118994A (ja) 2013-03-15 2018-04-02 Ｃａｒｍ１阻害剤およびその使用

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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)
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018118994A (ja) * 2013-03-15 2018-08-02 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
JP2021532157A (ja) * 2018-08-01 2021-11-25 アラクセス ファーマ エルエルシー がんを処置するための複素環式スピロ化合物およびその使用方法

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2753606B1 (en) * 2011-09-02 2017-07-05 Purdue Pharma LP Pyrimidines as sodium channel blockers
US9365555B2 (en) 2012-12-21 2016-06-14 Epizyme, Inc. PRMT5 inhibitors and uses thereof
WO2014100730A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
EP3498701B1 (en) 2012-12-21 2023-02-22 Epizyme Inc Prmt5 inhibitors and uses thereof
JP2016505000A (ja) 2012-12-21 2016-02-18 エピザイム，インコーポレイティド Ｐｒｍｔ５阻害剤およびその使用
US9221794B2 (en) 2012-12-21 2015-12-29 Epizyme, Inc. PRMT5 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
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
DK2970132T3 (da) 2013-03-14 2020-12-21 Epizyme Inc Argininmethyltransferaseinhibitorer og anvendelser deraf
WO2014153172A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives as prmt1 inhibitors and uses thereof
EP2970220A2 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9120757B2 (en) 2013-03-14 2015-09-01 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
US9133189B2 (en) 2013-03-14 2015-09-15 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
US9718816B2 (en) 2013-03-15 2017-08-01 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
EP3177288A4 (en) 2014-08-04 2018-04-04 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2016044604A1 (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
ES2899906T3 (es) 2015-07-06 2022-03-15 Alkermes Inc Inhibidores bicíclicos de histona desacetilasa
EP3319968A1 (en) 2015-07-06 2018-05-16 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
CN109906222B (zh) * 2016-09-07 2023-08-01 加利福尼亚大学董事会 减少p-tau并且改善认知的变构促肾上腺皮质激素释放因子受体1(crfr1)拮抗剂
AU2017355712B2 (en) 2016-11-07 2024-01-11 University Of Massachusetts Therapeutic targets for facioscapulohumeral muscular dystrophy
ES2875562T3 (es) 2017-01-11 2021-11-10 Alkermes Inc Inhibidores bicíclicos de histona desacetilasa
US11274093B2 (en) 2017-01-26 2022-03-15 Araxes Pharma Llc Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
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
WO2018140514A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
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
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
JP2020521740A (ja) 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー 変異体ｋｒａｓ、ｈｒａｓまたはｎｒａｓの調節因子としてのキナゾリン誘導体
TW201900633A (zh) 2017-05-25 2019-01-01 美商亞瑞克西斯製藥公司 Kras之共價抑制劑
US11225475B2 (en) 2017-08-07 2022-01-18 Alkermes, Inc. Substituted pyridines as inhibitors of histone deacetylase
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006514043A (ja) * 2002-12-20 2006-04-27 ファルマシア・コーポレーション マイトジェン活性化タンパク質キナーゼ−活性化タンパク質キナーゼ−２を阻害する化合物
JP2010500332A (ja) * 2006-08-11 2010-01-07 サノフイ−アベンテイス ５，６−ビスアリール−２−ピリジン−カルボキサミド誘導体、これらの調製およびウロテンシンｉｉ受容体アンタゴニストとしてのこれらの治療における使用
JP2016505000A (ja) * 2012-12-21 2016-02-18 エピザイム，インコーポレイティド Ｐｒｍｔ５阻害剤およびその使用
JP2016511744A (ja) * 2012-12-21 2016-04-21 エピザイム，インコーポレイティド Ｐｒｍｔ５を阻害する方法

Family Cites Families (63)

* 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
PL195600B1 (pl) * 1998-05-15 2007-10-31 Astrazeneca Ab Pochodne benzamidowe, sposób ich wytwarzania, zawierające je kompozycje farmaceutyczne oraz ich zastosowanie do wytwarzania leku do leczenia stanów medycznych powstających za pośrednictwem cytokin
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
CA2389034A1 (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
WO2002006276A1 (en) 2000-07-13 2002-01-24 Eli Lilly And Company Beta3 adrenergic agonists
US6864267B2 (en) 2001-07-16 2005-03-08 Smithkline Beecham Corporation Calcilytic compounds
WO2004078114A2 (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)
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
EP2137158A4 (en) 2007-02-28 2012-04-18 Methylgene Inc LOW-MOLECULAR INHIBITORS OF PROTEINARGININE METHYLTRANSFERASES (PRMTS)
EP2262766B1 (en) 2008-02-29 2015-11-11 Evotec AG Amide compounds, compositions and uses thereof
WO2010028179A1 (en) 2008-09-03 2010-03-11 Dr. Reddy's Laboratories Ltd. 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
US8962623B2 (en) 2011-03-04 2015-02-24 Locus Pharmaceuticals, Inc. Aminopyrazine compounds
JP6317669B2 (ja) 2011-04-15 2018-04-25 メリンタ セラピューティクス インコーポレイテッド 抗菌化合物ならびにそれを作製および使用する方法
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
US9221794B2 (en) 2012-12-21 2015-12-29 Epizyme, Inc. PRMT5 inhibitors and uses thereof
EP3498701B1 (en) 2012-12-21 2023-02-22 Epizyme Inc Prmt5 inhibitors and uses thereof
WO2014100730A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof
US9365555B2 (en) 2012-12-21 2016-06-14 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
DK2970132T3 (da) 2013-03-14 2020-12-21 Epizyme Inc Argininmethyltransferaseinhibitorer og anvendelser deraf
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
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
WO2014153090A1 (en) 2013-03-14 2014-09-25 Epizyme, Inc. Pyrazole derivatives asprmt1 inhibitors and uses thereof
EP2970220A2 (en) 2013-03-14 2016-01-20 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970181B1 (en) 2013-03-14 2017-06-07 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP3363434A1 (en) 2013-03-14 2018-08-22 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
EP2970219B1 (en) 2013-03-15 2019-02-27 Epizyme, Inc. Carm1 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
WO2015200677A2 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2015200680A2 (en) 2014-06-25 2015-12-30 Epizyme, Inc. Prmt5 inhibitors and uses thereof
EP3177288A4 (en) 2014-08-04 2018-04-04 Epizyme, Inc. Prmt5 inhibitors and uses thereof
WO2016044585A1 (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
WO2016044604A1 (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
US20170291905A1 (en) 2014-09-17 2017-10-12 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2016044650A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
CA2959689A1 (en) 2014-09-17 2016-03-24 Genentech, Inc. Pyrrolobenzodiazepines and antibody disulfide conjugates 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
WO2016044556A2 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
WO2017136699A1 (en) 2016-02-05 2017-08-10 Epizyme, Inc Arginine methyltransferase inhibitors and uses thereof
EP3487993A1 (en) 2016-07-25 2019-05-29 Epizyme, Inc. Crebbp related cancer therapy
US20190083482A1 (en) 2017-09-18 2019-03-21 Epizyme, Inc. Prmt5 inhibitors and uses thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006514043A (ja) * 2002-12-20 2006-04-27 ファルマシア・コーポレーション マイトジェン活性化タンパク質キナーゼ−活性化タンパク質キナーゼ−２を阻害する化合物
JP2010500332A (ja) * 2006-08-11 2010-01-07 サノフイ−アベンテイス ５，６−ビスアリール−２−ピリジン−カルボキサミド誘導体、これらの調製およびウロテンシンｉｉ受容体アンタゴニストとしてのこれらの治療における使用
JP2016505000A (ja) * 2012-12-21 2016-02-18 エピザイム，インコーポレイティド Ｐｒｍｔ５阻害剤およびその使用
JP2016511744A (ja) * 2012-12-21 2016-04-21 エピザイム，インコーポレイティド Ｐｒｍｔ５を阻害する方法

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018118994A (ja) * 2013-03-15 2018-08-02 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
JP2021532157A (ja) * 2018-08-01 2021-11-25 アラクセス ファーマ エルエルシー がんを処置するための複素環式スピロ化合物およびその使用方法
JP2024149542A (ja) * 2018-08-01 2024-10-18 アラクセス ファーマ エルエルシー がんを処置するための複素環式スピロ化合物およびその使用方法

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