JP2018502900A - ジスコイジンドメイン受容体１を標的化する小分子阻害剤およびその使用 - Google Patents

ジスコイジンドメイン受容体１を標的化する小分子阻害剤およびその使用 Download PDF

Info

Publication number
JP2018502900A
JP2018502900A JP2017540966A JP2017540966A JP2018502900A JP 2018502900 A JP2018502900 A JP 2018502900A JP 2017540966 A JP2017540966 A JP 2017540966A JP 2017540966 A JP2017540966 A JP 2017540966A JP 2018502900 A JP2018502900 A JP 2018502900A
Authority
JP
Japan
Prior art keywords
methyl
pyrimidin
phenyl
carboxamide
tetrahydroisoquinoline
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.)
Pending
Application number
JP2017540966A
Other languages
English (en)
Japanese (ja)
Other versions
JP2018502900A5 (enExample
Inventor
ロルフ エイ． ブレッカン
ロルフ エイ． ブレッカン
クァ ディン
クァ ディン
シャオメイ レン
シャオメイ レン
チェンチャオ トゥ
チェンチャオ トゥ
チェン ワン
チェン ワン
クリスティーナ ワイ． アギレラ
クリスティーナ ワイ． アギレラ
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.)
University of Texas System
Original Assignee
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 University of Texas System filed Critical University of Texas System
Publication of JP2018502900A publication Critical patent/JP2018502900A/ja
Publication of JP2018502900A5 publication Critical patent/JP2018502900A5/ja
Pending legal-status Critical Current

Links

Images

Classifications

    • 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)
  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (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)
JP2017540966A 2014-10-22 2015-10-21 ジスコイジンドメイン受容体１を標的化する小分子阻害剤およびその使用 Pending JP2018502900A (ja)

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 (2)

Publication Number Publication Date
JP2018502900A true JP2018502900A (ja) 2018-02-01
JP2018502900A5 JP2018502900A5 (enExample) 2018-11-22

Family

ID=55761466

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2017540966A Pending JP2018502900A (ja) 2014-10-22 2015-10-21 ジスコイジンドメイン受容体１を標的化する小分子阻害剤およびその使用

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)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102408261B1 (ko) 2014-02-03 2022-06-10 비타이 파마슈티컬즈, 엘엘씨 Ror-감마의 디하이드로피롤로피리딘 저해제
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US10301261B2 (en) 2015-08-05 2019-05-28 Vitae Pharmaceuticals, Llc Substituted indoles as 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
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
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
CN111225914B (zh) 2017-07-24 2022-10-11 生命医药有限责任公司 RORγ的抑制剂
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
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
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
WO2022200577A1 (en) 2021-03-26 2022-09-29 Chiesi Farmaceutici S.P.A. Indoline derivatives as ddrs inhibitors
KR20230163464A (ko) 2021-03-26 2023-11-30 키에시 파르마슈티시 엣스. 피. 에이. Ddr 억제제로서 테트라하이드로싸이에노 피리딘 유도체
MX2023011058A (es) * 2021-03-26 2023-09-28 Chiesi Farm Spa Derivados de tetrahidrotieno piridina como inhibidores de los receptores del dominio de discoidina (ddr).
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

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000505810A (ja) * 1996-11-27 2000-05-16 ファイザー・インク アポｂ−分泌／ｍｔｐ阻害性アミド
JP2000513014A (ja) * 1997-03-27 2000-10-03 ユハン・コーポレーション 新規ピリミジン誘導体およびその製造方法
JP2007523152A (ja) * 2004-02-18 2007-08-16 ファイザー・プロダクツ・インク キナゾリンおよびイソキノリンのテトラヒドロイソキノリニル誘導体
JP2012517470A (ja) * 2009-02-11 2012-08-02 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規なアミノアザヘテロ環式カルボキサミド
JP2013526528A (ja) * 2010-05-11 2013-06-24 サノフイ 置換されたｎ−ヘテロアリールテトラヒドロ−イソキノリン誘導体、その製造及び治療上の使用
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
WO2014167444A1 (en) * 2013-04-08 2014-10-16 Glenmark Pharmaceuticals S.A. SUBSTITUTED BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000505810A (ja) * 1996-11-27 2000-05-16 ファイザー・インク アポｂ−分泌／ｍｔｐ阻害性アミド
JP2000513014A (ja) * 1997-03-27 2000-10-03 ユハン・コーポレーション 新規ピリミジン誘導体およびその製造方法
JP2007523152A (ja) * 2004-02-18 2007-08-16 ファイザー・プロダクツ・インク キナゾリンおよびイソキノリンのテトラヒドロイソキノリニル誘導体
JP2012517470A (ja) * 2009-02-11 2012-08-02 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規なアミノアザヘテロ環式カルボキサミド
JP2013526528A (ja) * 2010-05-11 2013-06-24 サノフイ 置換されたｎ−ヘテロアリールテトラヒドロ−イソキノリン誘導体、その製造及び治療上の使用
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
WO2014167444A1 (en) * 2013-04-08 2014-10-16 Glenmark Pharmaceuticals S.A. SUBSTITUTED BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, no. 8, JPN6019026881, 2013, pages 3281 - 3295, ISSN: 0004074465 *
JOURNAL OF THE CHEMICAL SOCIETY, JPN6019026878, 1949, pages 1799 - 1803, ISSN: 0004215726 *

Also Published As

Publication number Publication date
US20180022730A1 (en) 2018-01-25
CA2965336A1 (en) 2016-04-28
AU2015335980A1 (en) 2017-05-18
CN107206004A (zh) 2017-09-26
EP3209299A1 (en) 2017-08-30
US10370360B2 (en) 2019-08-06
WO2016064970A1 (en) 2016-04-28
EP3209299A4 (en) 2018-04-04

Similar Documents

Publication Publication Date Title
JP2018502900A (ja) ジスコイジンドメイン受容体１を標的化する小分子阻害剤およびその使用
TWI549954B (zh) 經取代之２，３－二氫咪唑并［１，２－ｃ］喹唑啉鹽
JP6534675B2 (ja) ｍＩＤＨ１阻害剤としてのベンズイミダゾール−２−アミン
JP6688735B2 (ja) ｍＩＤＨ１阻害剤としてのベンズイミダゾール−２−アミン
CN103370322B (zh) 在过度增殖性病症的治疗中用作mps-1和tkk抑制剂的2-取代的咪唑并吡嗪
JP6830948B2 (ja) Ｍｉｄｈ１阻害剤としての縮合イミダゾール
CN102753547B (zh) 三唑并吡啶衍生物
JP6342392B2 (ja) 置換型ピラゾロン化合物及び使用方法
RU2632464C1 (ru) Замещенные триазолопиридины и их применение в качестве ингибиторов тирозин треонин киназы (ттк)
CN102971321B (zh) 咪唑并吡嗪
AU2015311333B2 (en) Quinolinone compound and use thereof
JP6824952B2 (ja) ｍＩＤＨ１阻害剤としての２−アリール−および２−アリールアルキル−ベンズイミダゾール
CN103429591A (zh) 在治疗过度增殖性病症中用作mps-1和tkk抑制剂的6-取代的咪唑并吡嗪
ZA200503663B (en) Aryl sulfonamides
CN102413831A (zh) 取代的咪唑并喹喔啉
MX2013005305A (es) Derivados de 2,3-dihidroimidazo[1,2-c]quinazolina sustituidos con aminoalcoholes que son de utilidad para tratar trastornos hiperproliferativos y enfermedades asociadas a la angiogenesis.
CN102762557A (zh) 三唑并吡啶
JP2016506943A (ja) Ｍｋｎｋ−１キナーゼ阻害剤としてのアミドイミダゾピリダジン類
EA023766B1 (ru) Триазолопиридины
WO2014020043A1 (en) Combinations for the treatment of cancer
JP2017533205A (ja) ｍＩＤＨ１阻害剤としてのベンゾイミダゾール−２−アミン
JP2018138570A (ja) 癌の治療のためのａｍｇ９００の使用
JP2018500344A (ja) ６−ヒドロキシベンゾフラニル置換および６−アルコキシベンゾフラニル置換イミダゾピリダジン
JP2010507626A (ja) Ｖｅｇｆｒ３阻害剤としての大環状キナゾリン誘導体
CN121079296A (zh) α-v-β-8整合素抑制剂及其用途

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181012

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20181012

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190711

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20190711

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190819

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20191001

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20200219