KR20170109546A - Irak1/4 억제제로서의 매크로시클릭 화합물 및 이들의 용도 - Google Patents

Irak1/4 억제제로서의 매크로시클릭 화합물 및 이들의 용도 Download PDF

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Publication number
KR20170109546A
KR20170109546A KR1020177020263A KR20177020263A KR20170109546A KR 20170109546 A KR20170109546 A KR 20170109546A KR 1020177020263 A KR1020177020263 A KR 1020177020263A KR 20177020263 A KR20177020263 A KR 20177020263A KR 20170109546 A KR20170109546 A KR 20170109546A
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South Korea
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ring
mmol
compound
optionally substituted
nitrogen
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Korean (ko)
Inventor
샤오링 첸
헨리 유
루오씨 란
캐서린 조랑드-르브룅
테레사 엘. 존슨
안드레아스 구토풀로스
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메르크 파텐트 게엠베하
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    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—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 three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—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 four or more hetero rings
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    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Nutrition Science (AREA)
KR1020177020263A 2015-02-05 2016-02-05 Irak1/4 억제제로서의 매크로시클릭 화합물 및 이들의 용도 Ceased KR20170109546A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562112374P 2015-02-05 2015-02-05
US62/112,374 2015-02-05
PCT/US2016/016709 WO2016127025A1 (en) 2015-02-05 2016-02-05 Macrocyclic compounds as irak1/4 inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
KR20170109546A true KR20170109546A (ko) 2017-09-29

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KR1020177020263A Ceased KR20170109546A (ko) 2015-02-05 2016-02-05 Irak1/4 억제제로서의 매크로시클릭 화합물 및 이들의 용도

Country Status (15)

Country Link
US (2) US9708324B2 (enExample)
EP (1) EP3253764B1 (enExample)
JP (1) JP6835727B2 (enExample)
KR (1) KR20170109546A (enExample)
CN (1) CN107849055B (enExample)
AU (1) AU2016215185B2 (enExample)
BR (1) BR112017013677B1 (enExample)
CA (1) CA2970534C (enExample)
ES (1) ES2886577T3 (enExample)
IL (1) IL253520B (enExample)
MX (1) MX383363B (enExample)
NZ (1) NZ732538A (enExample)
RU (1) RU2730016C2 (enExample)
SG (1) SG11201704628VA (enExample)
WO (1) WO2016127025A1 (enExample)

Families Citing this family (18)

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Publication number Priority date Publication date Assignee Title
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN107427521B (zh) 2015-03-27 2021-08-03 达纳-法伯癌症研究所股份有限公司 细胞周期蛋白依赖性激酶的抑制剂
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
US11254667B2 (en) 2016-08-17 2022-02-22 Children's Hospital Medical Center Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitors
US11542261B2 (en) 2016-08-17 2023-01-03 Children's Hospital Medical Center Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors
TW202340194A (zh) 2017-02-16 2023-10-16 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
EP3810132A4 (en) * 2018-06-25 2022-06-22 Dana-Farber Cancer Institute, Inc. TAIRE FAMILY KINASE INHIBITORS AND RELATED USES
TWI721483B (zh) 2018-07-13 2021-03-11 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
CA3108065C (en) 2018-07-31 2025-10-07 Loxo Oncology, Inc. SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
CN113164477A (zh) 2018-12-14 2021-07-23 达纳-法伯癌症研究所股份有限公司 C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途
EP3902542A4 (en) 2018-12-28 2022-09-07 Dana-Farber Cancer Institute, Inc. CYCLIN DEPENDENT KINASE 7 INHIBITORS AND USES THEREOF
KR20210146370A (ko) * 2019-03-28 2021-12-03 루핀 리미티드 Sting 효능제로서의 매크로사이클릭 화합물
CN111603471B (zh) * 2020-06-24 2021-07-09 山东省科学院生物研究所 一种邻二氮杂环化合物在制备抑制tlr4受体的药物中的用途
EP4185568A1 (en) 2020-07-24 2023-05-31 The University of Rochester Inhibitors of interleukin-1 receptor-associated kinases 1 and 4
US12577258B2 (en) 2020-09-30 2026-03-17 Vernalis (R&D) Limited Macrocyclic compound
WO2024030908A1 (en) * 2022-08-01 2024-02-08 Children's Hospital Medical Center Multi-cyclic irak1 and irak4 inhibiting compounds and uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7678783B2 (en) * 2004-11-17 2010-03-16 Merck Sharp & Dohme Corp. Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease
MY169441A (en) * 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
US8933066B2 (en) * 2011-04-14 2015-01-13 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
WO2014058691A1 (en) * 2012-10-08 2014-04-17 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
ES2639717T3 (es) * 2013-02-07 2017-10-30 Merck Patent Gmbh Derivados de piridazinona macrocíclicos
US9617282B2 (en) * 2013-03-15 2017-04-11 Biogen Ma Inc. Macrocyclic compounds as IRAK4 inhibitors for the treatment of inflammatory diseases

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CN107849055A (zh) 2018-03-27
BR112017013677A2 (pt) 2018-01-09
CA2970534A1 (en) 2016-08-11
JP2018506531A (ja) 2018-03-08
JP6835727B2 (ja) 2021-02-24
IL253520A0 (en) 2017-09-28
BR112017013677B1 (pt) 2023-11-21
MX383363B (es) 2025-03-13
US20170275284A1 (en) 2017-09-28
CN107849055B (zh) 2020-08-07
RU2017130762A (ru) 2019-03-05
US9708324B2 (en) 2017-07-18
SG11201704628VA (en) 2017-07-28
ES2886577T3 (es) 2021-12-20
WO2016127025A1 (en) 2016-08-11
US9815836B2 (en) 2017-11-14
RU2017130762A3 (enExample) 2019-04-30
CA2970534C (en) 2023-08-29
RU2730016C2 (ru) 2020-08-14
EP3253764B1 (en) 2021-06-09
EP3253764A1 (en) 2017-12-13
AU2016215185B2 (en) 2020-06-25
AU2016215185A1 (en) 2017-06-29
IL253520B (en) 2020-07-30
NZ732538A (en) 2022-04-29
MX2017009625A (es) 2017-11-20
US20160229856A1 (en) 2016-08-11

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