CA2781056A1 - Kinase inhibitors - Google Patents

Kinase inhibitors Download PDF

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Publication number
CA2781056A1
CA2781056A1 CA2781056A CA2781056A CA2781056A1 CA 2781056 A1 CA2781056 A1 CA 2781056A1 CA 2781056 A CA2781056 A CA 2781056A CA 2781056 A CA2781056 A CA 2781056A CA 2781056 A1 CA2781056 A1 CA 2781056A1
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CA
Canada
Prior art keywords
substituted
unsubstituted
heteroaryl
heterocycloalkyl
alkyl
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
CA2781056A
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English (en)
French (fr)
Inventor
Rebecca Maglathlin
Iana Serafimova
Michael S. Cohen
Rand Miller
Ville Paavilainen
Jesse Mcfarland
Shyam Krishnan
John William Taunton, Jr.
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 California San Diego UCSD
Original Assignee
University of California San Diego UCSD
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 California San Diego UCSD filed Critical University of California San Diego UCSD
Publication of CA2781056A1 publication Critical patent/CA2781056A1/en
Abandoned legal-status Critical Current

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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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • 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
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36Oxygen or sulfur atoms
    • C07D207/402,5-Pyrrolidine-diones
    • C07D207/4162,5-Pyrrolidine-diones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
CA2781056A 2009-11-16 2010-11-16 Kinase inhibitors Abandoned CA2781056A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US26169609P 2009-11-16 2009-11-16
US61/261,696 2009-11-16
US33027110P 2010-04-30 2010-04-30
US61/330,271 2010-04-30
PCT/US2010/056890 WO2011060440A2 (en) 2009-11-16 2010-11-16 Kinase inhibitors

Publications (1)

Publication Number Publication Date
CA2781056A1 true CA2781056A1 (en) 2011-05-19

Family

ID=43992477

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2781056A Abandoned CA2781056A1 (en) 2009-11-16 2010-11-16 Kinase inhibitors

Country Status (9)

Country Link
US (2) US20130035325A1 (https=)
EP (1) EP2558099A4 (https=)
JP (1) JP2013510886A (https=)
CN (1) CN102711765A (https=)
AU (1) AU2010319964A1 (https=)
BR (1) BR112012011528A2 (https=)
CA (1) CA2781056A1 (https=)
MX (1) MX2012005678A (https=)
WO (1) WO2011060440A2 (https=)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11524968B2 (en) 2017-10-18 2022-12-13 Hk Inno.N Corporation Heterocyclic compound as a protein kinase inhibitor
US12180185B2 (en) 2018-11-15 2024-12-31 Hk Inno.N Corporation Compound as protein kinase inhibitor, and pharmaceutical composition comprising thereof

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CA2836449C (en) * 2011-05-17 2021-04-27 The Regents Of The University Of California Kinase inhibitors
US9376438B2 (en) 2011-05-17 2016-06-28 Principia Biopharma, Inc. Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors
EA025496B1 (ru) 2011-05-17 2016-12-30 Принсипиа Биофарма Инк. Ингибиторы тирозинкиназы
CN104487441B (zh) 2012-06-18 2018-06-01 普林斯匹亚生物制药公司 有用于治疗癌症和自身免疫性疾病的可逆的共价吡咯并嘧啶或吡唑并嘧啶
JP2015526520A (ja) 2012-08-31 2015-09-10 プリンシピア バイオファーマ インコーポレイテッド Itk阻害剤としてのベンズイミダゾール誘導体
ME03455B (me) 2012-09-10 2020-01-20 Principia Biopharma Inc Jedinjenja pirazolopirimidina kao inhibitori kinaze
WO2014093230A2 (en) 2012-12-10 2014-06-19 Merck Patent Gmbh Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity
US8957080B2 (en) 2013-04-09 2015-02-17 Principia Biopharma Inc. Tyrosine kinase inhibitors
PT3107544T (pt) 2014-02-21 2021-01-05 Principia Biopharma Inc Sais e forma sólida de um inibidor de btk
EP3166608B1 (en) 2014-07-07 2018-12-12 Jiangsu Hengrui Medicine Co., Ltd. Aminopyridazinone compounds as protein kinase inhibitors
US10485797B2 (en) 2014-12-18 2019-11-26 Principia Biopharma Inc. Treatment of pemphigus
TW201718572A (zh) 2015-06-24 2017-06-01 普林斯匹亞生物製藥公司 酪胺酸激酶抑制劑
CN106939002B (zh) * 2016-01-05 2019-09-24 江苏恒瑞医药股份有限公司 一种btk激酶抑制剂的结晶形式及其制备方法
CA3009256C (en) * 2016-01-05 2023-08-22 Jiangsu Hengrui Medicine Co., Ltd. Crystalline form of btk kinase inhibitor and preparation method thereof
MA45547A (fr) 2016-06-29 2019-05-08 Principia Biopharma Inc Formulations à libération modifiée à base de 2-[3-[4-amino-3-(2-fluoro-4-phénoxy-phényl)pyrazolo[3,4-d]pyrimidine-1-yl]pipéridine-1-carbonyl]-4-méthyl-4-[4-(oxétane-3-yl)pipérazine-1-yl]pent-2-ènenitrile
TWI877239B (zh) 2019-10-14 2025-03-21 美商普林斯匹亞生物製藥公司 藉由投予(R)-2-[3-[4-胺基-3-(2-氟-4-苯氧基-苯基)吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧呾-3-基)哌-1-基]戊-2-烯腈來治療免疫血小板減少症之方法
JP2023511105A (ja) 2020-01-22 2023-03-16 プリンシピア バイオファーマ インコーポレイテッド 2-[3-[4-アミノ-3-(2-フルオロ-4-フェノキシ-フェニル)-1h-ピラゾロ[3,4-d]ピリミジン-1-イル]ピペリジン-1-カルボニル]-4-メチル-4-[4-(オキセタン-3-イル)ピペラジン-1-イル]ペンタ-2-エンニトリルの結晶形態
CN111205232B (zh) * 2020-02-26 2022-07-01 浙江天宇药业股份有限公司 一种替格瑞洛中间体的合成方法
TW202307005A (zh) 2021-05-28 2023-02-16 美商邊際分析公司 以核醣體蛋白質S6激酶α-1 (RSK1)及核醣體蛋白質S6激酶α-3 (RSK2)之調節劑治療神經病症之方法
CN116332996B (zh) * 2023-05-04 2025-04-01 南京颐媛生物医学研究院有限公司 L-呋喃核糖型抗冠状病毒化合物及其制备方法和应用
CN116284135B (zh) * 2023-05-04 2025-03-21 南京颐媛生物医学研究院有限公司 抗冠状病毒核苷类化合物的制备方法及其应用
CN116410228B (zh) * 2023-05-04 2025-10-31 南京颐媛生物医学研究院有限公司 一种抗冠状病毒核苷类化合物的制备方法及其应用

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11524968B2 (en) 2017-10-18 2022-12-13 Hk Inno.N Corporation Heterocyclic compound as a protein kinase inhibitor
US12180185B2 (en) 2018-11-15 2024-12-31 Hk Inno.N Corporation Compound as protein kinase inhibitor, and pharmaceutical composition comprising thereof

Also Published As

Publication number Publication date
US20130035325A1 (en) 2013-02-07
CN102711765A (zh) 2012-10-03
US20150045343A1 (en) 2015-02-12
WO2011060440A3 (en) 2011-11-03
MX2012005678A (es) 2012-09-07
WO2011060440A2 (en) 2011-05-19
JP2013510886A (ja) 2013-03-28
AU2010319964A1 (en) 2012-06-07
AU2010319964A2 (en) 2012-08-02
US9505766B2 (en) 2016-11-29
EP2558099A4 (en) 2013-07-17
BR112012011528A2 (pt) 2019-09-24
EP2558099A2 (en) 2013-02-20

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