CN106061966B - 用作溴区结构域抑制剂的双环杂环衍生物 - Google Patents

用作溴区结构域抑制剂的双环杂环衍生物 Download PDF

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CN106061966B
CN106061966B CN201580004048.2A CN201580004048A CN106061966B CN 106061966 B CN106061966 B CN 106061966B CN 201580004048 A CN201580004048 A CN 201580004048A CN 106061966 B CN106061966 B CN 106061966B
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alkyl
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synthesis
pharmaceutically acceptable
methoxy
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CN106061966A (zh
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S·萨玛伊达尔
C·阿比奈尼
S·赛斯迈尔
S·霍沙哈利
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Orion Oyj
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201580004048.2A 2014-01-09 2015-01-06 用作溴区结构域抑制剂的双环杂环衍生物 Expired - Fee Related CN106061966B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN125/CHE/2014 2014-01-09
IN125CH2014 2014-01-09
PCT/IB2015/050090 WO2015104653A1 (en) 2014-01-09 2015-01-06 Bicyclic heterocyclic derivatives as bromodomain inhibitors

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CN106061966A CN106061966A (zh) 2016-10-26
CN106061966B true CN106061966B (zh) 2018-12-07

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US (2) US10077259B2 (https=)
EP (1) EP3092227B1 (https=)
JP (1) JP6480944B2 (https=)
KR (1) KR102394518B1 (https=)
CN (1) CN106061966B (https=)
AU (1) AU2015205339B2 (https=)
BR (1) BR112016015311B1 (https=)
CA (1) CA2934788C (https=)
CL (1) CL2016001737A1 (https=)
CY (1) CY1122046T1 (https=)
DK (1) DK3092227T3 (https=)
EA (1) EA029224B1 (https=)
ES (1) ES2687497T3 (https=)
HR (1) HRP20181650T1 (https=)
HU (1) HUE041546T2 (https=)
IL (1) IL246140B (https=)
LT (1) LT3092227T (https=)
MA (1) MA39172B1 (https=)
MX (1) MX2016009052A (https=)
MY (1) MY190835A (https=)
PE (1) PE20161021A1 (https=)
PH (1) PH12016501355B1 (https=)
PL (1) PL3092227T3 (https=)
PT (1) PT3092227T (https=)
RS (1) RS57586B1 (https=)
SA (1) SA516371448B1 (https=)
SG (1) SG11201604916YA (https=)
SI (1) SI3092227T1 (https=)
UA (1) UA117165C2 (https=)
WO (1) WO2015104653A1 (https=)

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JP2018527340A (ja) 2015-08-11 2018-09-20 ネオメド インスティテュートNeomed Institute アリール置換ジヒドロキノリノン、その調製及び医薬品としてのその使用
WO2017024406A1 (en) 2015-08-11 2017-02-16 Neomed Institute N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals
KR102784592B1 (ko) 2015-08-12 2025-03-19 에피제네틱스, 인크. 치환된 벤즈이미다졸, 그의 제조법 및 제약으로서의 그의 용도
US10501459B2 (en) 2015-10-21 2019-12-10 Neomed Institute Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN105198871A (zh) * 2015-11-06 2015-12-30 中国药科大学 一类喹喔啉酮类化合物及其制备方法和用途
US10519151B2 (en) 2016-01-28 2019-12-31 Neomed Institute Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals
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CN108570038B (zh) * 2017-03-08 2021-09-28 中国科学院上海药物研究所 二氢喹喔啉类溴结构域识别蛋白抑制剂及制备方法和用途
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CN110960528A (zh) * 2018-09-30 2020-04-07 四川大学 Ar和bet双重抑制剂及其用途
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AU2015205339B2 (en) 2018-07-05
ES2687497T3 (es) 2018-10-25
NZ721993A (en) 2021-05-28
MY190835A (en) 2022-05-12
EP3092227A1 (en) 2016-11-16
JP2017502057A (ja) 2017-01-19
PL3092227T3 (pl) 2018-12-31
KR20160106164A (ko) 2016-09-09
EA029224B1 (ru) 2018-02-28
US10077259B2 (en) 2018-09-18
PH12016501355B1 (en) 2019-11-06
JP6480944B2 (ja) 2019-03-13
US10590118B2 (en) 2020-03-17
SA516371448B1 (ar) 2018-10-15
KR102394518B1 (ko) 2022-05-06
EA201691404A1 (ru) 2016-10-31
IL246140A0 (en) 2016-08-02
HRP20181650T1 (hr) 2018-12-14
EP3092227B1 (en) 2018-07-11
PH12016501355A1 (en) 2017-02-06
US20160368906A1 (en) 2016-12-22
CL2016001737A1 (es) 2017-02-03
RS57586B1 (sr) 2018-11-30
BR112016015311B1 (pt) 2023-01-24
LT3092227T (lt) 2018-08-10
CA2934788A1 (en) 2015-07-16
BR112016015311A2 (https=) 2017-08-08
MX2016009052A (es) 2016-09-09
CN106061966A (zh) 2016-10-26
MA39172B1 (fr) 2018-10-31
DK3092227T3 (en) 2018-09-03
SI3092227T1 (sl) 2018-10-30
PT3092227T (pt) 2018-10-24
SG11201604916YA (en) 2016-07-28
WO2015104653A1 (en) 2015-07-16
PE20161021A1 (es) 2016-11-09
US20180339982A1 (en) 2018-11-29
UA117165C2 (uk) 2018-06-25
MA39172A1 (fr) 2018-04-30
CA2934788C (en) 2021-12-07
AU2015205339A1 (en) 2016-07-07
HUE041546T2 (hu) 2019-05-28
IL246140B (en) 2019-09-26
CY1122046T1 (el) 2020-07-31

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