CA2965336A1 - Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof - Google Patents

Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof Download PDF

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Publication number
CA2965336A1
CA2965336A1 CA2965336A CA2965336A CA2965336A1 CA 2965336 A1 CA2965336 A1 CA 2965336A1 CA 2965336 A CA2965336 A CA 2965336A CA 2965336 A CA2965336 A CA 2965336A CA 2965336 A1 CA2965336 A1 CA 2965336A1
Authority
CA
Canada
Prior art keywords
methyl
pyrimidin
tetrahydroisoquinoline
carboxamide
trifluoromethyl
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.)
Abandoned
Application number
CA2965336A
Other languages
English (en)
French (fr)
Inventor
Rolf A. Brekken
Ke Ding
Xiaomei REN
Zhengchao TU
Zhen Wang
Kristina Y. Aguilera
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.)
Guangzhou Institutes of Biomedicine and Health
The University of Texas System
Original Assignee
Guangzhou Institutes of Biomedicine and Health
The University of Texas System
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 Guangzhou Institutes of Biomedicine and Health, The University of Texas System filed Critical Guangzhou Institutes of Biomedicine and Health
Publication of CA2965336A1 publication Critical patent/CA2965336A1/en
Abandoned legal-status Critical Current

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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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
CA2965336A 2014-10-22 2015-10-21 Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof Abandoned CA2965336A1 (en)

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
CA2965336A1 true CA2965336A1 (en) 2016-04-28

Family

ID=55761466

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2965336A Abandoned CA2965336A1 (en) 2014-10-22 2015-10-21 Small-molecule inhibitors targeting discoidin domain receptor 1 and uses thereof

Country Status (7)

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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3102576T3 (da) 2014-02-03 2019-07-22 Vitae Pharmaceuticals Llc Dihydropyrrolopyridininhibitorer af ror-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
EP3331876B1 (en) 2015-08-05 2020-10-07 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
EP3868750A1 (en) * 2015-11-20 2021-08-25 Vitae Pharmaceuticals, LLC Modulators of ror-gamma
TWI757266B (zh) 2016-01-29 2022-03-11 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
CN109963845B (zh) * 2017-05-23 2021-09-03 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
CN115716826A (zh) 2017-07-24 2023-02-28 生命医药有限责任公司 RORγ的抑制剂
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
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
WO2019243431A1 (en) * 2018-06-20 2019-12-26 INSERM (Institut National de la Santé et de la Recherche Médicale) Compositions for treating melanoma
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
MX2022014295A (es) 2020-05-25 2022-12-07 Chiesi Farm Spa Derivados de la bencilamina como inhibidores de los receptores del dominio de discoidina.
GB202010464D0 (en) * 2020-07-08 2020-08-19 Galapagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of diseases
CN112321591B (zh) * 2020-11-03 2022-11-08 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
WO2022128850A1 (en) * 2020-12-16 2022-06-23 Galapagos Nv Novel isoquinoline derivatives and pharmaceutical copositions thereof for the treatment of diseases
EP4313292B1 (en) * 2021-03-26 2026-02-18 Chiesi Farmaceutici S.p.A. Indoline derivatives as ddr1 and ddr2 inhibitors
GEP20267870B (en) 2021-03-26 2026-03-10 Chiesi Farm Spa Tetrahydrothieno pyridine derivatives as ddrs inhibitors
AU2022242770A1 (en) 2021-03-26 2023-11-09 Chiesi Farmaceutici S.P.A. Tetrahydrothieno pyridine derivatives as ddrs inhibitors
WO2022200577A1 (en) 2021-03-26 2022-09-29 Chiesi Farmaceutici S.P.A. Indoline derivatives as ddrs inhibitors
PT4313293T (pt) * 2021-11-22 2025-07-25 Chiesi Farm Spa Derivados de tetraidrotieno piridina como inibidores de ddrs

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR199901180T2 (xx) * 1996-11-27 1999-08-23 Pfizer Inc. Apo B-Salg�lama/MTP inhibit�r amidler.
IN188411B (enExample) * 1997-03-27 2002-09-21 Yuhan Corp
EP1723134A2 (en) * 2004-02-18 2006-11-22 Pfizer Products Incorporated Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline
US20070054916A1 (en) * 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
KR101699991B1 (ko) * 2009-02-11 2017-01-26 메르크 파텐트 게엠베하 신규의 아미노 아자헤테로시클릭 카르복사미드
AR081034A1 (es) * 2010-05-11 2012-05-30 Sanofi Aventis Derivados de n-heteroaril tetrahidro-isoquinolina sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades del sistema nervioso central
CN103965195B (zh) * 2013-02-01 2016-09-28 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
WO2014167444A1 (en) * 2013-04-08 2014-10-16 Glenmark Pharmaceuticals S.A. SUBSTITUTED BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS

Also Published As

Publication number Publication date
EP3209299A4 (en) 2018-04-04
US10370360B2 (en) 2019-08-06
AU2015335980A1 (en) 2017-05-18
WO2016064970A1 (en) 2016-04-28
CN107206004A (zh) 2017-09-26
JP2018502900A (ja) 2018-02-01
EP3209299A1 (en) 2017-08-30
US20180022730A1 (en) 2018-01-25

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20220112