CN107206004A - 靶向盘状结构域受体1的小分子抑制剂及其用途 - Google Patents

靶向盘状结构域受体1的小分子抑制剂及其用途 Download PDF

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Publication number
CN107206004A
CN107206004A CN201580067710.9A CN201580067710A CN107206004A CN 107206004 A CN107206004 A CN 107206004A CN 201580067710 A CN201580067710 A CN 201580067710A CN 107206004 A CN107206004 A CN 107206004A
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Prior art keywords
methyl
bases
phenyl
trifluoromethyl
tetrahydroisoquinoline
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Pending
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CN201580067710.9A
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Chinese (zh)
Inventor
罗尔夫·A·布雷肯
丁可
任晓梅
涂正超
王振
克里斯季娜·Y·阿吉莱拉
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Guangzhou Institute of Biomedicine and Health of CAS
University of Texas System
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Guangzhou Institute of Biomedicine and Health of CAS
University of Texas System
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Publication of CN107206004A publication Critical patent/CN107206004A/zh
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    • 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
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures 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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201580067710.9A 2014-10-22 2015-10-21 靶向盘状结构域受体1的小分子抑制剂及其用途 Pending CN107206004A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462067070P 2014-10-22 2014-10-22
US62/067,070 2014-10-22
US201562204176P 2015-08-12 2015-08-12
US62/204,176 2015-08-12
PCT/US2015/056611 WO2016064970A1 (en) 2014-10-22 2015-10-21 Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof

Publications (1)

Publication Number Publication Date
CN107206004A true CN107206004A (zh) 2017-09-26

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CN201580067710.9A Pending CN107206004A (zh) 2014-10-22 2015-10-21 靶向盘状结构域受体1的小分子抑制剂及其用途

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Country Link
US (1) US10370360B2 (https=)
EP (1) EP3209299A4 (https=)
JP (1) JP2018502900A (https=)
CN (1) CN107206004A (https=)
AU (1) AU2015335980A1 (https=)
CA (1) CA2965336A1 (https=)
WO (1) WO2016064970A1 (https=)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108463458A (zh) * 2015-11-20 2018-08-28 生命医药公司 ROR-γ的调节剂
CN108624590A (zh) * 2018-04-19 2018-10-09 西安医学院 一种抑制DDR2表达的siRNA及其应用
CN111217748A (zh) * 2018-11-23 2020-06-02 江苏恒瑞医药股份有限公司 一种螺环二氢异喹啉甲酰胺类衍生物的晶型及其制备方法
CN112321591A (zh) * 2020-11-03 2021-02-05 中国药科大学 盘状结构域受体1蛋白抑制剂、制备方法及应用
CN117098764A (zh) * 2021-03-26 2023-11-21 奇斯药制品公司 作为ddr抑制剂的四氢噻吩并吡啶衍生物
CN117120434A (zh) * 2021-03-26 2023-11-24 奇斯药制品公司 作为ddr1和ddr2抑制剂的吲哚啉衍生物
CN117157300A (zh) * 2021-03-26 2023-12-01 奇斯药制品公司 作为ddr抑制剂的四氢噻吩并吡啶衍生物

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3102576B8 (en) 2014-02-03 2019-06-19 Vitae Pharmaceuticals, LLC Dihydropyrrolopyridine inhibitors of ror-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
WO2017024018A1 (en) 2015-08-05 2017-02-09 Vitae Pharmaceuticals, Inc. Modulators of ror-gamma
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ＲＯＲ－γ調節劑
CN108276388B (zh) * 2017-03-10 2020-01-14 成都医学院 1h-吲哚类衍生物及其用途
US12133896B2 (en) 2017-03-23 2024-11-05 Kaohsiung Medical University Methods for treating or alleviating a bone-loss related disease or condition by administering a nucleic acid encoding a discoidin domain receptor 1 (DDR1) protein
TWI676482B (zh) * 2017-03-23 2019-11-11 高雄醫學大學 盤基蛋白結構域受體１的抑制劑及活化劑及其用途
WO2018214862A1 (zh) * 2017-05-23 2018-11-29 江苏恒瑞医药股份有限公司 螺环甲酰胺类衍生物、其制备方法及其在医药上的应用
JP2020528904A (ja) 2017-07-24 2020-10-01 ヴァイティー ファーマシューティカルズ，エルエルシー ＲＯＲγの阻害剤
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
KR102066402B1 (ko) * 2017-12-22 2020-01-15 대화제약 주식회사 이리노테칸 또는 그의 약제학적으로 허용가능한 염을 포함하는 경구투여용 약제학적 조성물
WO2019243431A1 (en) * 2018-06-20 2019-12-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Compositions for treating melanoma
CN115697485B (zh) 2020-05-25 2025-03-14 奇斯药制品公司 作为ddr抑制剂的苄胺衍生物
GB202010464D0 (en) * 2020-07-08 2020-08-19 Galapagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of diseases
WO2022128850A1 (en) * 2020-12-16 2022-06-23 Galapagos Nv Novel isoquinoline derivatives and pharmaceutical copositions thereof for the treatment of diseases
PL4313293T3 (pl) 2021-03-26 2025-09-01 Chiesi Farmaceutici S.P.A. Pochodne tetrahydrotienopirydyny jako inhibitory DDR
EP4313972B1 (en) 2021-03-26 2025-01-29 Chiesi Farmaceutici S.p.A. Indoline derivatives as ddrs inhibitors

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CN102317269A (zh) * 2009-02-11 2012-01-11 默克专利有限公司 新氨基氮杂杂环甲酰胺类
CN103965195A (zh) * 2013-02-01 2014-08-06 中国科学院广州生物医药与健康研究院 用于盘状结构域受体小分子抑制剂的化合物及其应用

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Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108463458A (zh) * 2015-11-20 2018-08-28 生命医药公司 ROR-γ的调节剂
CN108463458B (zh) * 2015-11-20 2022-02-01 生命医药有限责任公司 ROR-γ的调节剂
CN108624590A (zh) * 2018-04-19 2018-10-09 西安医学院 一种抑制DDR2表达的siRNA及其应用
CN111217748A (zh) * 2018-11-23 2020-06-02 江苏恒瑞医药股份有限公司 一种螺环二氢异喹啉甲酰胺类衍生物的晶型及其制备方法
CN111217748B (zh) * 2018-11-23 2022-04-12 江苏恒瑞医药股份有限公司 一种螺环二氢异喹啉甲酰胺类衍生物的晶型及其制备方法
CN112321591A (zh) * 2020-11-03 2021-02-05 中国药科大学 盘状结构域受体1蛋白抑制剂、制备方法及应用
CN117098764A (zh) * 2021-03-26 2023-11-21 奇斯药制品公司 作为ddr抑制剂的四氢噻吩并吡啶衍生物
CN117120434A (zh) * 2021-03-26 2023-11-24 奇斯药制品公司 作为ddr1和ddr2抑制剂的吲哚啉衍生物
CN117157300A (zh) * 2021-03-26 2023-12-01 奇斯药制品公司 作为ddr抑制剂的四氢噻吩并吡啶衍生物

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Publication number Publication date
US10370360B2 (en) 2019-08-06
US20180022730A1 (en) 2018-01-25
CA2965336A1 (en) 2016-04-28
WO2016064970A1 (en) 2016-04-28
EP3209299A1 (en) 2017-08-30
JP2018502900A (ja) 2018-02-01
EP3209299A4 (en) 2018-04-04
AU2015335980A1 (en) 2017-05-18

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