CO2018012181A2 - Compuestos arilo o heteroarilo sustituidos con amino como inhibidores de ehmt1 y ehmt2 - Google Patents

Compuestos arilo o heteroarilo sustituidos con amino como inhibidores de ehmt1 y ehmt2

Info

Publication number
CO2018012181A2
CO2018012181A2 CONC2018/0012181A CO2018012181A CO2018012181A2 CO 2018012181 A2 CO2018012181 A2 CO 2018012181A2 CO 2018012181 A CO2018012181 A CO 2018012181A CO 2018012181 A2 CO2018012181 A2 CO 2018012181A2
Authority
CO
Colombia
Prior art keywords
amino
substituted aryl
ehmt1
ehmt2
compounds
Prior art date
Application number
CONC2018/0012181A
Other languages
English (en)
Spanish (es)
Inventor
John Emmerson Campbell
Kenneth William Duncan
Megan Alene Foley
Darren Martin Harvey
Kevin Wayne Kuntz
James Edward John Mills
Michael John Munchhof
Original Assignee
Epizyme Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Epizyme Inc filed Critical Epizyme Inc
Publication of CO2018012181A2 publication Critical patent/CO2018012181A2/es

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/12—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
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
CONC2018/0012181A 2016-04-15 2018-11-13 Compuestos arilo o heteroarilo sustituidos con amino como inhibidores de ehmt1 y ehmt2 CO2018012181A2 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662323602P 2016-04-15 2016-04-15
US201662348837P 2016-06-10 2016-06-10
US201662402997P 2016-09-30 2016-09-30
PCT/US2017/027918 WO2017181177A1 (en) 2016-04-15 2017-04-17 Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors

Publications (1)

Publication Number Publication Date
CO2018012181A2 true CO2018012181A2 (es) 2019-08-20

Family

ID=58664786

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2018/0012181A CO2018012181A2 (es) 2016-04-15 2018-11-13 Compuestos arilo o heteroarilo sustituidos con amino como inhibidores de ehmt1 y ehmt2

Country Status (24)

Country Link
US (2) US20170355712A1 (https=)
EP (1) EP3442947B1 (https=)
JP (3) JP7041070B2 (https=)
KR (2) KR102571679B1 (https=)
CN (1) CN109153650A (https=)
AU (3) AU2017250369A1 (https=)
BR (1) BR112018071093A2 (https=)
CA (1) CA3021062A1 (https=)
CL (2) CL2018002928A1 (https=)
CO (1) CO2018012181A2 (https=)
DK (1) DK3442947T3 (https=)
ES (1) ES2953512T3 (https=)
FI (1) FI3442947T3 (https=)
HU (1) HUE064145T2 (https=)
IL (3) IL307931A (https=)
LT (1) LT3442947T (https=)
MA (1) MA44666A (https=)
MX (2) MX395342B (https=)
PL (1) PL3442947T3 (https=)
PT (1) PT3442947T (https=)
SG (2) SG10201913471VA (https=)
SI (1) SI3442947T1 (https=)
TW (1) TWI751155B (https=)
WO (1) WO2017181177A1 (https=)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016258192B2 (en) 2015-05-06 2021-07-29 Leidos Biomedical Research, Inc. K-Ras modulators
WO2016183266A1 (en) 2015-05-13 2016-11-17 Enanta Pharmaceuticals, Inc. Ehpatitis b antiviral agents
KR102398439B1 (ko) 2016-03-07 2022-05-16 이난타 파마슈티칼스, 인코포레이티드 B형 간염 항바이러스제
PT3442972T (pt) 2016-04-15 2020-05-29 Abbvie Inc Inibidores de bromodomínio
US11278550B2 (en) 2016-05-17 2022-03-22 Duke University Compositions and methods for the treatment of Prader-Willi syndrome
US20200039998A1 (en) * 2016-12-19 2020-02-06 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
US20200113901A1 (en) * 2017-03-31 2020-04-16 Epizyme, Inc. Methods of using ehmt2 inhibitors
EP3612526A2 (en) * 2017-04-20 2020-02-26 The Regents of the University of California K-ras modulators
CN110621316B (zh) * 2017-04-21 2024-01-26 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
SG11202001685TA (en) 2017-08-28 2020-03-30 Enanta Pharm Inc Hepatitis b antiviral agents
CN109467538A (zh) 2017-09-07 2019-03-15 和记黄埔医药（上海）有限公司 环烯烃取代的杂芳环类化合物及其用途
CA3079260A1 (en) * 2017-10-17 2019-04-25 Epizyme, Inc. Amine-substituted heterocyclic compounds as ehmt2 inhibitors and derivatives thereof
JP2021500326A (ja) * 2017-10-18 2021-01-07 エピザイム，インコーポレイティド 血液障害の予防又は処置にｅｈｍｔ２阻害剤を使用する方法
AU2018353139A1 (en) * 2017-10-18 2020-06-04 Epizyme, Inc. Methods of using EHMT2 inhibitors in immunotherapies
JP2021500334A (ja) * 2017-10-18 2021-01-07 エピザイム，インコーポレイティド Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法
US11058678B2 (en) 2018-01-22 2021-07-13 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
JP2021514359A (ja) 2018-02-15 2021-06-10 ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． キナーゼ阻害剤としての複素環式化合物
CN108822103A (zh) * 2018-07-28 2018-11-16 刘凤娟 一种咪唑并[4,5-b]吡啶化合物及其制备方法和应用
JP2022500466A (ja) 2018-09-21 2022-01-04 エナンタ ファーマシューティカルズ インコーポレイテッド 抗ウイルス剤としての官能化複素環
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
WO2020092528A1 (en) 2018-10-31 2020-05-07 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
US11203591B2 (en) 2018-10-31 2021-12-21 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds
IL283190B2 (en) 2018-11-21 2025-08-01 Enanta Pharm Inc Functionalized heterocycles as antiviral agents
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
MA55909A (fr) * 2019-05-05 2022-03-16 Qilu Regor Therapeutics Inc Inhibiteurs de cdk
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
WO2020247444A1 (en) 2019-06-03 2020-12-10 Enanta Pharmaceuticals, Inc, Hepatitis b antiviral agents
WO2020247575A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
WO2020247561A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc, Hepatitis b antiviral agents
US11738019B2 (en) 2019-07-11 2023-08-29 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
GB201910608D0 (en) 2019-07-24 2019-09-04 Enterprise Therapeutics Ltd Compounds
CA3150681A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
US11236108B2 (en) 2019-09-17 2022-02-01 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
US11851426B2 (en) 2019-10-11 2023-12-26 Incyte Corporation Bicyclic amines as CDK2 inhibitors
CA3163206A1 (en) * 2019-11-27 2021-06-03 Riken G9a inhibitor
UY38994A (es) 2019-12-20 2021-07-30 Nuevolution As Compuestos activos frente a receptores nucleares
WO2021188414A1 (en) 2020-03-16 2021-09-23 Enanta Pharmaceuticals, Inc. Functionalized heterocyclic compounds as antiviral agents
TW202208355A (zh) 2020-05-04 2022-03-01 美商安進公司 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法
JP7741100B2 (ja) 2020-05-04 2025-09-17 アムジェン インコーポレイテッド ミエロイド細胞に発現するトリガー受容体２アゴニストとしての複素環化合物及び使用方法
CN111518015A (zh) * 2020-05-20 2020-08-11 上海合全药物研发有限公司 一种叔丁基-8-氧亚基-2-氮杂螺[4.5]癸烷-2-甲酸基酯的制备方法
AU2022222470A1 (en) 2021-02-19 2023-09-21 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
CA3208361A1 (en) 2021-02-19 2022-08-25 Anjali Pandey Tyk2 inhibitors and uses thereof
EP4294806A1 (en) 2021-02-19 2023-12-27 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
JP2024538128A (ja) * 2021-10-15 2024-10-18 タンゴ セラピューティクス， インコーポレイテッド Ｅｈｍｔ１及びｅｈｍｔ２の新規調節因子及びその治療用途
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
CN119585255A (zh) * 2022-07-20 2025-03-07 S2C生物株式会社 杂芳基衍生化合物及其用途
CN115947692B (zh) * 2022-12-28 2024-12-27 上海再启生物技术有限公司 一种制备2-氯-4-(甲氧基甲基)嘧啶的方法
WO2024216164A1 (en) 2023-04-13 2024-10-17 Tango Therapeutics, Inc. N2-((5-hydroxy)-2-pyridyl)-pyridine-2,4-diamine derivatives as ehmt1/2 modulators for the treatment of cancer
WO2025045203A1 (zh) * 2023-09-01 2025-03-06 葆元生物医药科技(杭州)有限公司 杂环化合物及其中间体和应用

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
EP0585500A1 (en) * 1992-09-04 1994-03-09 Merrell Dow Pharmaceuticals Inc. Diaryl piperazineacetamides as antimuscarinic agents
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
AU2002316421B2 (en) * 2001-06-26 2008-05-15 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-ALPHA expression
WO2003032994A2 (de) * 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg 5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren
HRP20050089B1 (hr) * 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
US20070105839A1 (en) * 2003-09-18 2007-05-10 Patricia Imbach 2, 4-Di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
US20060025406A1 (en) * 2004-07-06 2006-02-02 Angion Biomedica Corporation Modulators of hepatocyte growth factor/c- Met activity
CN101252914B (zh) * 2005-05-05 2013-03-27 塞诺菲-安万特美国有限责任公司 稳定的纳米粒制剂
CA2615420A1 (en) * 2005-07-15 2007-01-25 4Sc Ag 2-arylbenzothiazoles and uses thereof
EP1746096A1 (en) * 2005-07-15 2007-01-24 4Sc Ag 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
WO2007038387A2 (en) * 2005-09-23 2007-04-05 Yale University Compounds and methods for the treatment of viruses and cancer
JP5191391B2 (ja) * 2005-11-01 2013-05-08 ターゲジェン インコーポレーティッド キナーゼのビ−アリールメタ−ピリミジン阻害剤
TW200736232A (en) * 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
CA2647592C (en) * 2006-05-26 2014-01-28 Abbott Laboratories Inhibitors of polo-like kinases
JP5328816B2 (ja) * 2008-02-22 2013-10-30 エフ．ホフマン−ラ ロシュ アーゲー アミロイドβの調節薬
SG165655A1 (en) * 2008-04-16 2010-11-29 Portola Pharm Inc 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors
AU2009279825A1 (en) * 2008-08-05 2010-02-11 Targegen, Inc. Methods of treating thalassemia
KR20110049905A (ko) * 2008-09-03 2011-05-12 바이엘 크롭사이언스 아게 4-알킬-치환된 디아미노피리미딘
US8367689B2 (en) * 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
ES2577829T3 (es) * 2010-06-04 2016-07-19 F. Hoffmann-La Roche Ag Derivados de aminopirimidina como moduladores de la LRRK2
WO2012044936A1 (en) * 2010-09-30 2012-04-05 Portola Pharmaceuticals, Inc. Combination therapy with 4-(3-(2h-1,2,3-triazol-2-yl)phenylamino)-2-((1r,2s)-2-aminocyclohexylamino)pyrimidine-5-carboxamide
KR101682417B1 (ko) * 2011-02-25 2016-12-06 주식회사유한양행 다이아미노피리미딘 유도체 및 그의 제조방법
WO2013054351A1 (en) * 2011-08-08 2013-04-18 Cadila Healthcare Limited Heterocyclic compounds
WO2013033037A2 (en) * 2011-08-26 2013-03-07 The Regents Of The University Of California Novel antiprion compounds
WO2013070852A2 (en) * 2011-11-08 2013-05-16 Emory University Compounds and compositions used to epigenetically transform cells and methods related thereto
KR101452235B1 (ko) * 2012-02-03 2014-10-22 서울대학교산학협력단 신규한 피리미딘계 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 포함하는 ｒａｇｅ 수용체 관련 질환의 예방 또는 치료용 약학적 조성물
AU2013237226A1 (en) * 2012-03-19 2014-10-09 Emory University Quinazoline compounds and their use in therapy
GB201209613D0 (en) * 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
WO2014058921A2 (en) * 2012-10-08 2014-04-17 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
US9145412B2 (en) * 2012-11-02 2015-09-29 Acetylon Pharmaceuticals, Inc. Selective HDAC1 and HDAC2 inhibitors
WO2015109109A1 (en) * 2014-01-15 2015-07-23 Forum Pharmaceuticals Inc. Fused morpholinopyrimidines and methods of use thereof
CN106536509B (zh) * 2014-06-16 2020-06-09 基础应用医学研究基金会 作为组蛋白甲基转移酶和dna甲基转移酶的双重抑制剂的新型化合物

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