CN110088099B - 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法 - Google Patents

作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法 Download PDF

Info

Publication number
CN110088099B
CN110088099B CN201780078660.3A CN201780078660A CN110088099B CN 110088099 B CN110088099 B CN 110088099B CN 201780078660 A CN201780078660 A CN 201780078660A CN 110088099 B CN110088099 B CN 110088099B
Authority
CN
China
Prior art keywords
compound
cancer
methyl
halogen
mmol
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201780078660.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN110088099A (zh
Inventor
约翰·埃默森·坎贝尔
肯尼思·W·邓肯
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Epizyme Inc
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
Priority to CN202310013963.4A priority Critical patent/CN116041346A/zh
Publication of CN110088099A publication Critical patent/CN110088099A/zh
Application granted granted Critical
Publication of CN110088099B publication Critical patent/CN110088099B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • 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
    • 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
    • C07D401/14Heterocyclic 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
    • 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
    • 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
    • C07D403/14Heterocyclic 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
    • 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
    • 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
    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/12Heterocyclic 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 three hetero rings
    • C07D491/14Ortho-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
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CN201780078660.3A 2016-12-19 2017-12-19 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法 Active CN110088099B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202310013963.4A CN116041346A (zh) 2016-12-19 2017-12-19 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662436139P 2016-12-19 2016-12-19
US62/436,139 2016-12-19
US201762517840P 2017-06-09 2017-06-09
US62/517,840 2017-06-09
PCT/US2017/067192 WO2018118842A1 (en) 2016-12-19 2017-12-19 Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202310013963.4A Division CN116041346A (zh) 2016-12-19 2017-12-19 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法

Publications (2)

Publication Number Publication Date
CN110088099A CN110088099A (zh) 2019-08-02
CN110088099B true CN110088099B (zh) 2023-01-31

Family

ID=60972416

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201780078660.3A Active CN110088099B (zh) 2016-12-19 2017-12-19 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法
CN202310013963.4A Pending CN116041346A (zh) 2016-12-19 2017-12-19 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202310013963.4A Pending CN116041346A (zh) 2016-12-19 2017-12-19 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法

Country Status (25)

Country Link
US (2) US20200039998A1 (enExample)
EP (2) EP3555070B1 (enExample)
JP (2) JP2020504715A (enExample)
KR (1) KR102693367B1 (enExample)
CN (2) CN110088099B (enExample)
AU (3) AU2017382830A1 (enExample)
BR (1) BR112019012140A2 (enExample)
CA (1) CA3045032A1 (enExample)
CL (2) CL2019001664A1 (enExample)
CO (1) CO2019006787A2 (enExample)
DK (1) DK3555070T3 (enExample)
ES (1) ES2955132T3 (enExample)
FI (1) FI3555070T3 (enExample)
HU (1) HUE063405T2 (enExample)
IL (1) IL267090A (enExample)
LT (1) LT3555070T (enExample)
MA (1) MA47233A (enExample)
MX (1) MX2019007234A (enExample)
PL (1) PL3555070T3 (enExample)
PT (1) PT3555070T (enExample)
SG (1) SG10201913464TA (enExample)
SI (1) SI3555070T1 (enExample)
TW (2) TW202411220A (enExample)
WO (1) WO2018118842A1 (enExample)
ZA (1) ZA201904234B (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10118890B2 (en) 2014-10-10 2018-11-06 The Research Foundation For The State University Of New York Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration
US20200039961A1 (en) * 2016-09-30 2020-02-06 Epizyme, Inc. Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors
PE20191349A1 (es) * 2017-02-14 2019-09-30 Effector Therapeutics Inc Inhibidores de mnk sustituidos con piperidina y metodos relacionados con los mismos
US20200113901A1 (en) * 2017-03-31 2020-04-16 Epizyme, Inc. Methods of using ehmt2 inhibitors
WO2018195450A1 (en) 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
WO2019014402A1 (en) 2017-07-14 2019-01-17 Innate Tumor Immunity, Inc. MODULATORS OF NLRP3
WO2019079485A1 (en) * 2017-10-17 2019-04-25 Epizyme, Inc. AMINO-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS EHMT2 INHIBITORS AND DERIVATIVES THEREOF
AU2018353150B2 (en) * 2017-10-18 2024-06-06 Epizyme, Inc. Methods of using EHMT2 inhibitors in treating or preventing blood disorders
MA50418A (fr) * 2017-10-18 2021-04-07 Epizyme Inc Composés hétérocycliques substitués par une amine, utilisés comme inhibiteurs de l'ehmt2, sels de ceux-ci, et leurs méthodes de synthèse
KR101954370B1 (ko) 2018-07-25 2019-03-05 한미약품 주식회사 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물
CA3117169A1 (en) 2018-10-24 2020-04-30 Effector Therapeutics, Inc. Crystalline forms of mnk inhibitors
WO2020097398A1 (en) 2018-11-07 2020-05-14 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
US12338228B2 (en) * 2019-01-14 2025-06-24 Innate Tumor Immunity, Inc. NLRP3 modulators
US12433867B2 (en) 2019-02-22 2025-10-07 Hanmi Pharm. Co., Ltd. Pharmaceutical composition comprising FLT3 inhibitor and hypomethylating agent for treating acute myeloid leukemia
MX2021011699A (es) * 2019-03-28 2022-01-18 Epizyme Inc Derivados de quinolina y su uso para el tratamiento del cancer.
CA3145391A1 (en) 2019-06-27 2020-12-30 Hanmi Pharm. Co., Ltd. Pharmaceutical composition for treating acute myeloid leukemia, containing flt3 inhibitor and chemotherapeutic agents
CA3181537A1 (en) 2020-05-06 2021-11-11 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
CN115160297B (zh) 2020-12-22 2023-03-31 益方生物科技(上海)股份有限公司 杂芳基化合物及其制备方法和用途
WO2022140527A1 (en) 2020-12-23 2022-06-30 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
AU2022366869A1 (en) * 2021-10-15 2024-05-02 Tango Therapeutics, Inc. Novel modulators of ehmt1 and ehmt2 and therapeutic use thereof
TW202325289A (zh) 2021-11-09 2023-07-01 美商雅捷可斯治療公司 Jak2抑制劑之形式及組合物
TW202334139A (zh) 2021-11-09 2023-09-01 美商雅捷可斯治療公司 作為jak2抑制劑之6-雜芳氧基苯并咪唑及氮雜苯并咪唑
KR20250040981A (ko) * 2022-07-20 2025-03-25 주식회사 에스투시바이오 헤테로아릴 유도체 화합물 및 이의 용도
CN115974727B (zh) * 2023-01-17 2024-03-12 青岛前线生物工程有限公司 一种联苯肼酯的合成方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000025780A1 (en) * 1998-10-29 2000-05-11 Bristol-Myers Squibb Company Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
CN109153650A (zh) * 2016-04-15 2019-01-04 Epizyme股份有限公司 作为ehmt1和ehmt2抑制剂的胺取代的芳基或杂芳基化合物

Family Cites Families (19)

* 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
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
US6596747B2 (en) * 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
ATE337312T1 (de) * 2001-07-03 2006-09-15 Vertex Pharma Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen
WO2003040141A1 (en) * 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
ES2365223T3 (es) * 2003-08-07 2011-09-26 Rigel Pharmaceuticals, Inc. Compuestos 2,4-pirimidindiamínicos y usos como agentes antiproliferativos.
JP2009501164A (ja) * 2005-07-15 2009-01-15 4エスツェー アクチェンゲゼルシャフト 2−アリールベンゾチアゾール及びその使用
MEP3808A (xx) * 2005-12-21 2010-02-10 Novartis Ag Derivati pirimidinil aril uree kao fgf inhibitori
TW200902010A (en) * 2007-01-26 2009-01-16 Smithkline Beecham Corp Anthranilamide inhibitors of aurora kinase
WO2009012421A1 (en) * 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
MX2010008700A (es) * 2008-02-22 2010-08-30 Hoffmann La Roche Moduladores de beta-amiloide.
SG172885A1 (en) * 2009-01-23 2011-08-29 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the jak pathway
US8367689B2 (en) * 2009-05-06 2013-02-05 Portola Pharmaceuticals, Inc. Inhibitors of JAK
CN104640863B (zh) * 2012-09-20 2016-06-08 山东亨利医药科技有限责任公司 嘧啶胺衍生物及其制备方法和应用
CA2892677A1 (en) * 2012-12-04 2014-06-12 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
CA2904610A1 (en) * 2013-03-14 2014-09-25 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
US20160009694A1 (en) * 2013-03-15 2016-01-14 Portola Pharmaceuticals, Inc. Cyclohexanediamine compounds and methods for their preparation
WO2016175264A1 (ja) * 2015-04-28 2016-11-03 カルナバイオサイエンス株式会社 抗マラリア活性を有する新規ヘテロアリール誘導体
CN106083828A (zh) * 2016-06-30 2016-11-09 浙江大学 含吖丙啶环侧链的芳胺嘧啶衍生物及制备和应用

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000025780A1 (en) * 1998-10-29 2000-05-11 Bristol-Myers Squibb Company Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
CN109153650A (zh) * 2016-04-15 2019-01-04 Epizyme股份有限公司 作为ehmt1和ehmt2抑制剂的胺取代的芳基或杂芳基化合物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Discovery of an in Vivo Chemical Probe of the Lysine Methyltransferases G9a and GLP;Feng Liu等;《J. Med. Chem.》;20131008;8931-8942 *
Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase;Pitts, William J等;《Bioorganic & Medicinal Chemistry Letters》;20021231;2137-2140 *
RN:872510-72-0;Registry;《Registry》;20060124;1 *

Also Published As

Publication number Publication date
EP3555070B1 (en) 2023-08-09
MA47233A (fr) 2019-10-23
CL2020001133A1 (es) 2020-11-06
WO2018118842A1 (en) 2018-06-28
US20200039998A1 (en) 2020-02-06
CA3045032A1 (en) 2018-06-28
KR102693367B1 (ko) 2024-08-12
TW202411220A (zh) 2024-03-16
CL2019001664A1 (es) 2019-12-06
FI3555070T3 (fi) 2023-09-12
AU2017382830A1 (en) 2019-06-13
TW201833102A (zh) 2018-09-16
CO2019006787A2 (es) 2019-09-30
MX2019007234A (es) 2019-09-06
LT3555070T (lt) 2023-09-11
SI3555070T1 (sl) 2023-11-30
BR112019012140A2 (pt) 2019-11-05
EP4285906A2 (en) 2023-12-06
AU2024205290A1 (en) 2024-08-22
HUE063405T2 (hu) 2024-01-28
TWI808067B (zh) 2023-07-11
JP2022110080A (ja) 2022-07-28
DK3555070T3 (da) 2023-09-18
PT3555070T (pt) 2023-09-14
CN110088099A (zh) 2019-08-02
ZA201904234B (en) 2025-09-25
SG10201913464TA (en) 2020-03-30
EP4285906A3 (en) 2024-03-13
IL267090A (en) 2019-08-29
KR20190092542A (ko) 2019-08-07
CN116041346A (zh) 2023-05-02
PL3555070T3 (pl) 2023-11-06
EP3555070A1 (en) 2019-10-23
US20220235065A1 (en) 2022-07-28
AU2022202494B2 (en) 2024-05-02
AU2022202494A1 (en) 2022-05-12
ES2955132T3 (es) 2023-11-28
JP2020504715A (ja) 2020-02-13

Similar Documents

Publication Publication Date Title
CN110088099B (zh) 作为ehmt2抑制剂的胺取代的杂环化合物及其使用方法
JP7425724B2 (ja) Ehmt2阻害剤としてのアミン置換複素環化合物及びその誘導体
CN112939967B (zh) 吡唑并[1,5-a]吡啶类化合物及其制备方法和应用
TW201823249A (zh) Menin-mll相互作用之稠合二環抑制劑
CN110869360A (zh) 作为rock抑制剂的苯乙酰胺类
CN115427035B (zh) Enl/af9 yeats抑制剂
MX2014008866A (es) Nuevos derivados fosfatos, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen.
JP2021505684A (ja) ヒストンデアセチラーゼ6阻害剤としての1,2,4−オキサジアゾール誘導体
JP2019533650A (ja) Ehmt2阻害剤としての置換された融合二環式または三環式複素環化合物
CN116262750A (zh) 一种芳杂环类化合物及其制备方法和用途
TWI894448B (zh) Ctla-4小分子降解劑及其應用
CN120282784A (zh) 包含多发性内分泌癌蛋白-mll抑制剂和bcl-2抑制剂的组合
CN114644633A (zh) 杂环类jak抑制剂
HK40012431A (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
HK40012431B (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
HK40098892A (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
WO2025218778A1 (zh) 杂环化合物及其作为ret抑制剂的用途
HK40016100B (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
HK40016100A (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
HK40058867A (en) Imidazopyridinyl compounds and use thereof for treatment of proliferative disorders
NZ795530A (en) Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
OA19666A (en) Amine-substituted heterocyclic compounds as Ehmt2 inhibitors and methods of use thereof.
HK1244803B (zh) 作为抗癌药物的取代的2-氢-吡唑衍生物

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40012431

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant