CN108026105B - TGFβ受体拮抗剂 - Google Patents

TGFβ受体拮抗剂 Download PDF

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Publication number
CN108026105B
CN108026105B CN201680055202.3A CN201680055202A CN108026105B CN 108026105 B CN108026105 B CN 108026105B CN 201680055202 A CN201680055202 A CN 201680055202A CN 108026105 B CN108026105 B CN 108026105B
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Prior art keywords
pyridin
pyrrolo
triazin
amino
amine
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CN201680055202.3A
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English (en)
Chinese (zh)
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CN108026105A (zh
Inventor
L·S·卡里克里斯南
B·E·芬克
R·M·博尔齐莱里
G·特奴库奴如
H·拉哈曼
J·S·瓦里尔
B·塞沙德里
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • 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
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201680055202.3A 2015-07-23 2016-07-21 TGFβ受体拮抗剂 Active CN108026105B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562195854P 2015-07-23 2015-07-23
US62/195,854 2015-07-23
PCT/US2016/043252 WO2017015425A1 (en) 2015-07-23 2016-07-21 Tgf beta receptor antagonists

Publications (2)

Publication Number Publication Date
CN108026105A CN108026105A (zh) 2018-05-11
CN108026105B true CN108026105B (zh) 2020-10-16

Family

ID=56609944

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680055202.3A Active CN108026105B (zh) 2015-07-23 2016-07-21 TGFβ受体拮抗剂

Country Status (6)

Country Link
US (1) US10336761B2 (https=)
EP (1) EP3325484A1 (https=)
JP (1) JP2018520201A (https=)
KR (1) KR20180032611A (https=)
CN (1) CN108026105B (https=)
WO (1) WO2017015425A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7114076B2 (ja) 2015-12-22 2022-08-08 シャイ・セラピューティクス・エルエルシー がん及び炎症性疾患の処置のための化合物
JP7514005B2 (ja) 2017-06-21 2024-07-10 シャイ・セラピューティクス・エルエルシー がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのrasスーパーファミリーと相互作用する化合物
CN111655260A (zh) * 2017-10-26 2020-09-11 南方研究院 作为TGF-β抑制剂的噁二唑和噻二唑
JP7407461B2 (ja) 2018-12-19 2024-01-04 シャイ・セラピューティクス・エルエルシー がん、炎症性疾患、ras病、及び線維性疾患の処置のためのrasスーパーファミリーと相互作用する化合物
CA3117838A1 (en) 2018-12-27 2020-07-02 Nexys Therapeutics, Inc. (pyridin-2-yl)amine derivatives as tgf-beta r1 (alk5) inhibitors for the treatment of cancer
CN111825675B (zh) * 2019-04-15 2023-08-01 武汉朗来科技发展有限公司 Rock抑制剂及其制备方法和用途
CN112694477B (zh) * 2019-10-22 2024-02-06 四川科伦博泰生物医药股份有限公司 吡唑并环类化合物,包含其的药物组合物,其制备方法及其用途
WO2021147699A1 (zh) * 2020-01-21 2021-07-29 四川科伦博泰生物医药股份有限公司 吡啶并杂环类化合物、其制备方法及用途
CN113620956B (zh) * 2020-05-06 2023-06-13 赛诺哈勃药业(成都)有限公司 转化生长因子受体拮抗剂、其制备方法和应用
AU2023249795A1 (en) * 2022-04-08 2024-10-17 Shy Therapeutics, Llc Compounds that interact with ras superfamily proteins for treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
US20260028365A1 (en) * 2022-07-14 2026-01-29 Biogen Ma Inc. Tyrosine kinase 2 inhibitors and uses thereof
EP4651950A1 (en) * 2023-01-19 2025-11-26 Skyhawk Therapeutics, Inc. Compositions useful for modulating splicing

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004065392A1 (en) * 2003-01-24 2004-08-05 Smithkline Beecham Corporation Condensed pyridines and pyrimidines and their use as alk-5 receptor ligands

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2497444C (en) * 2002-09-04 2010-11-30 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
JP2006521398A (ja) * 2003-03-28 2006-09-21 サイオス・インコーポレーテツド TGFβの二−環式ピリミジン阻害剤
MX2013010163A (es) * 2011-03-09 2013-10-30 Merck Patent Gmbh Derivados de pirido[2,3-b] pirazina y sus usos terapeuticos.
CN103450204B (zh) * 2012-05-31 2016-08-17 中国科学院上海药物研究所 吡咯[2,1-f][1,2,4]并三嗪类化合物,其制备方法及用途

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004065392A1 (en) * 2003-01-24 2004-08-05 Smithkline Beecham Corporation Condensed pyridines and pyrimidines and their use as alk-5 receptor ligands

Also Published As

Publication number Publication date
JP2018520201A (ja) 2018-07-26
EP3325484A1 (en) 2018-05-30
US10336761B2 (en) 2019-07-02
US20180215761A1 (en) 2018-08-02
KR20180032611A (ko) 2018-03-30
CN108026105A (zh) 2018-05-11
WO2017015425A1 (en) 2017-01-26

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