TW201617338A - 取代的雜芳基化合物及其組合物和用途 - Google Patents

取代的雜芳基化合物及其組合物和用途 Download PDF

Info

Publication number
TW201617338A
TW201617338A TW104133416A TW104133416A TW201617338A TW 201617338 A TW201617338 A TW 201617338A TW 104133416 A TW104133416 A TW 104133416A TW 104133416 A TW104133416 A TW 104133416A TW 201617338 A TW201617338 A TW 201617338A
Authority
TW
Taiwan
Prior art keywords
group
atoms
cycloalkyl
alkyl
groups
Prior art date
Application number
TW104133416A
Other languages
English (en)
Chinese (zh)
Inventor
寧 習
李敏雄
李曉波
戴偉龍
胡海洋
張濤
陳武宏
Original Assignee
廣東東陽光藥業有限公司
加拓科學公司
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 廣東東陽光藥業有限公司, 加拓科學公司 filed Critical 廣東東陽光藥業有限公司
Publication of TW201617338A publication Critical patent/TW201617338A/zh

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW104133416A 2014-10-14 2015-10-12 取代的雜芳基化合物及其組合物和用途 TW201617338A (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462063460P 2014-10-14 2014-10-14

Publications (1)

Publication Number Publication Date
TW201617338A true TW201617338A (zh) 2016-05-16

Family

ID=55747172

Family Applications (1)

Application Number Title Priority Date Filing Date
TW104133416A TW201617338A (zh) 2014-10-14 2015-10-12 取代的雜芳基化合物及其組合物和用途

Country Status (6)

Country Link
US (1) US10059689B2 (https=)
EP (1) EP3206691B1 (https=)
JP (1) JP6649540B2 (https=)
ES (1) ES2699948T3 (https=)
TW (1) TW201617338A (https=)
WO (1) WO2016060963A1 (https=)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017044434A1 (en) 2015-09-11 2017-03-16 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
CN109776522B (zh) * 2017-10-30 2020-12-29 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
US10683297B2 (en) 2017-11-19 2020-06-16 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
TWI707849B (zh) 2018-02-13 2020-10-21 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
KR102591947B1 (ko) 2018-04-19 2023-10-25 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
EP3820572B1 (en) 2018-07-13 2023-08-16 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
US11236085B2 (en) 2018-10-24 2022-02-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
WO2020097396A1 (en) 2018-11-07 2020-05-14 Dana-Farber Cancer Institute, Inc. Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof
EP3877371A4 (en) 2018-11-07 2022-07-27 Dana-Farber Cancer Institute, Inc. IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF
WO2020097398A1 (en) 2018-11-07 2020-05-14 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
AU2020240382B2 (en) 2019-03-19 2022-08-25 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
AR120331A1 (es) * 2019-10-29 2022-02-09 Shenyang Sinochem Agrochemicals R & D Co Ltd Compuesto de piperidinamina que contiene pirimidina y preparación, método y uso del mismo
CA3181537A1 (en) 2020-05-06 2021-11-11 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
EP4267574B1 (en) 2020-12-23 2025-04-23 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
JP7782035B2 (ja) 2021-11-09 2025-12-08 エイジャックス セラピューティクス, インコーポレイテッド Jak2阻害剤としての6-ヘテロアリールオキシベンゾイミダゾール及びアザベンゾイミダゾール
TW202325289A (zh) 2021-11-09 2023-07-01 美商雅捷可斯治療公司 Jak2抑制劑之形式及組合物

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2274634T3 (es) * 1998-08-29 2007-05-16 Astrazeneca Ab Compuestos de pirimidina.
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
AU2003286711A1 (en) 2002-10-25 2004-05-13 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
EP1763514A2 (en) 2004-05-18 2007-03-21 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
JP2008525422A (ja) 2004-12-23 2008-07-17 ファイザー・プロダクツ・インク 抗癌剤として有用な複素芳香族誘導体
AU2005322855B2 (en) * 2004-12-30 2012-09-20 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
RU2008152195A (ru) * 2006-06-15 2010-07-20 БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) 2-анилино-4-(гетероциклил)аминопиримидины, как ингибиторы протеинкиназы с-альфа
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
CA2693594A1 (en) 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
EA024109B1 (ru) * 2008-04-16 2016-08-31 Портола Фармасьютиклз, Инк. Ингибиторы протеинкиназ
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
TWI546290B (zh) 2008-06-27 2016-08-21 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
JPWO2010058846A1 (ja) * 2008-11-21 2012-04-19 アステラス製薬株式会社 4,6−ジアミノニコチンアミド化合物
US8268851B2 (en) * 2008-12-23 2012-09-18 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
CA2749837C (en) 2009-01-21 2017-07-11 Rigel Pharmaceuticals, Inc. Derivatives of n2-(3-pyridil or phenyl)-n4-(4-piperidyl)-2,4-pyrimidinediamine useful in the treatment of inflammatory, autoimmune or proliferative diseases
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Egfr 억제제 및 질환 치료방법
WO2010144468A1 (en) * 2009-06-10 2010-12-16 Abbott Laboratories 2- ( lh-pyrazol-4 -ylamino ) -pyrimidine as kinase inhibitors
US20110130415A1 (en) 2009-12-01 2011-06-02 Rajinder Singh Protein kinase c inhibitors and uses thereof
EP2595982B1 (en) 2010-07-21 2018-06-13 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
EP2635556B1 (en) 2010-11-01 2017-06-21 Portola Pharmaceuticals, Inc. Benzamides and nicotinamides as syk modulators
HRP20172006T1 (hr) 2010-11-10 2018-02-09 Genentech, Inc. Derivati pirazol-aminopiridina kao lrrk2-modulatori
EP2710003A1 (en) * 2011-05-16 2014-03-26 OSI Pharmaceuticals, LLC Fused bicyclic kinase inhibitors
CA2836449C (en) * 2011-05-17 2021-04-27 The Regents Of The University Of California Kinase inhibitors
EP2554544A1 (en) * 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
CN103159742B (zh) 2011-12-16 2015-08-12 北京韩美药品有限公司 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用
ES2658395T3 (es) 2012-04-04 2018-03-09 Rigel Pharmaceuticals, Inc. Inhibidores de proteína cinasa C y usos de los mismos
ES2792979T3 (es) 2013-08-22 2020-11-12 Jubilant Biosys Ltd Compuestos de pirimidina sustituidos, composiciones y aplicaciones médicas de los mismos
WO2015039613A1 (zh) 2013-09-18 2015-03-26 北京韩美药品有限公司 抑制btk和/或jak3激酶活性的化合物
BR112016008632A8 (pt) 2013-10-21 2020-03-17 Merck Patent Gmbh compostos de heteroarila como inibidores de btk, seus usos, e composição farmacêutica
CN105461694B (zh) * 2014-09-27 2019-05-24 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途

Also Published As

Publication number Publication date
ES2699948T3 (es) 2019-02-13
US10059689B2 (en) 2018-08-28
EP3206691B1 (en) 2018-09-19
EP3206691A4 (en) 2018-04-11
WO2016060963A1 (en) 2016-04-21
EP3206691A1 (en) 2017-08-23
JP2017531000A (ja) 2017-10-19
US20160229837A1 (en) 2016-08-11
JP6649540B2 (ja) 2020-02-19

Similar Documents

Publication Publication Date Title
TW201617338A (zh) 取代的雜芳基化合物及其組合物和用途
US9399637B2 (en) Substituted heteroaryl compounds and methods of use
CN108570048B (zh) 取代的杂芳基化合物及其组合物和用途
CN106478651B (zh) 取代的杂芳基化合物及其组合物和用途
CN109776522B (zh) 取代的杂芳基化合物及其组合物和用途
CN106478607B (zh) 取代的杂芳基化合物及其组合物和用途
JP7254076B2 (ja) 置換ヘテロアリール化合物及び使用方法
CN105461694A (zh) 取代的杂芳基化合物及其组合物和用途
US10266521B2 (en) Substituted heteroaryl compounds and methods of use
CN104974163B (zh) 取代的杂芳基化合物及其组合物和用途
US20170081338A1 (en) Substituted heteroaryl compounds and methods of use
CN106432246A (zh) 杂芳化合物及其在药物中的应用
CN105367555B (zh) 取代的杂芳基化合物及其组合物和用途
CN104926824B (zh) 取代的杂芳基化合物及其组合物和用途
CN104650092B (zh) 取代的杂芳基化合物及其组合物和用途
CN104672250B (zh) 取代的杂芳基化合物及其组合物和用途