CA2648923A1 - Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases - Google Patents

Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases Download PDF

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Publication number
CA2648923A1
CA2648923A1 CA002648923A CA2648923A CA2648923A1 CA 2648923 A1 CA2648923 A1 CA 2648923A1 CA 002648923 A CA002648923 A CA 002648923A CA 2648923 A CA2648923 A CA 2648923A CA 2648923 A1 CA2648923 A1 CA 2648923A1
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Canada
Prior art keywords
aliphatic
compound
disease
formula
ring
Prior art date
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Abandoned
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CA002648923A
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English (en)
French (fr)
Inventor
Juan-Miguel Jimenez
Ronald Knegtel
Daniel Robinson
Philip Collier
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Vertex Pharmaceuticals Inc
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Individual
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Publication of CA2648923A1 publication Critical patent/CA2648923A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/587—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with aliphatic hydrocarbon radicals substituted by 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, said aliphatic radicals being substituted in the alpha-position to the ring by a hetero atom, e.g. with m >= 0, Z being a singly or a doubly bound hetero atom
    • C07D277/593—Z being doubly bound oxygen or doubly bound nitrogen, which nitrogen is part of a possibly substituted oximino radical
    • 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
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
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    • A61P11/02—Nasal agents, e.g. decongestants
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings 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
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Psychology (AREA)
  • AIDS & HIV (AREA)
CA002648923A 2006-04-11 2007-04-11 Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases Abandoned CA2648923A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US79108306P 2006-04-11 2006-04-11
US60/791,083 2006-04-11
PCT/US2007/008819 WO2007117692A2 (en) 2006-04-11 2007-04-11 Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases

Publications (1)

Publication Number Publication Date
CA2648923A1 true CA2648923A1 (en) 2007-10-18

Family

ID=38508761

Family Applications (1)

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CA002648923A Abandoned CA2648923A1 (en) 2006-04-11 2007-04-11 Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases

Country Status (9)

Country Link
US (3) US7589214B2 (enExample)
EP (1) EP2007732B1 (enExample)
JP (1) JP2009536617A (enExample)
CN (1) CN101460466B (enExample)
AT (1) ATE534632T1 (enExample)
AU (1) AU2007235237B2 (enExample)
CA (1) CA2648923A1 (enExample)
ES (1) ES2376765T3 (enExample)
WO (1) WO2007117692A2 (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7589214B2 (en) * 2006-04-11 2009-09-15 Vertex Pharmaceuticals Incorporated Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases
BRPI1016172A2 (pt) * 2009-04-24 2016-04-19 Tibotec Pharm Ltd éteres diarílicos
US8735417B2 (en) 2009-12-17 2014-05-27 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
US8759366B2 (en) 2009-12-17 2014-06-24 Merck Sharp & Dohme Corp. Aminopyrimidines as SYK inhibitors
CA2834062A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
EP2706853B1 (en) 2011-05-10 2017-06-14 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
JP6170944B2 (ja) 2011-12-28 2017-07-26 ヤンセン・サイエンシズ・アイルランド・ユーシー Ｈｃｖ阻害剤としてのヘテロ−二環式誘導体
MX2015001802A (es) 2012-08-10 2015-05-07 Boehringer Ingelheim Int Compuestos heteroaromaticos como inhibidores de btk.
MD20150035A2 (ro) * 2012-11-02 2015-10-31 Pfizer Inc. Inhibitori de tirozinkinaza Bruton
CN103848810A (zh) * 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
WO2014151620A1 (en) * 2013-03-14 2014-09-25 Boehringer Ingelheim International Gmbh 5-thiazolecarboxamide dervatives and their use as btk inhibitors
JP6495886B2 (ja) 2013-03-15 2019-04-03 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｔｋ阻害剤としての複素環式芳香族化合物
PL3052476T3 (pl) * 2013-09-30 2021-01-11 Guangzhou Innocare Pharma Tech Co., Ltd. Podstawione nikotynoimidowe inhibitory btk oraz sposób ich wytwarzania i zastosowanie w leczeniu raka, stanu zapalnego i chorób automunnologicznych
EP3080097B1 (en) 2013-12-13 2018-04-18 F.Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
WO2015116485A1 (en) * 2014-01-29 2015-08-06 Boehringer Ingelheim International Gmbh Pyrazole compounds as btk inhibitors
CN105085474B (zh) * 2014-05-07 2018-05-18 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
CN106687446B (zh) * 2014-07-18 2020-04-28 百济神州(北京)生物科技有限公司 作为t790m/wt-egfr的选择性和不可逆的激酶抑制剂的5-氨基-4-氨甲酰基-吡唑化合物及其用途
JP6976947B2 (ja) 2015-12-16 2021-12-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 自己免疫疾患の処置に有用なビピラゾリル誘導体
JP6916185B2 (ja) 2016-01-13 2021-08-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｔｋ阻害剤としてのイソキノロン類
CN113454066B (zh) * 2019-02-25 2024-02-09 北京诺诚健华医药科技有限公司 制备6-(1-丙烯酰基哌啶-4-基)-2-(4-苯氧基苯基)尼克酰胺的工艺
CN116018138B (zh) * 2020-07-13 2025-08-15 河南知微生物医药有限公司 作为布鲁诺酪氨酸激酶抑制剂的取代的1H-咪唑并[1,2-b]吡唑-3-甲酰胺

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GB9608435D0 (en) * 1996-04-24 1996-06-26 Celltech Therapeutics Ltd Chemical compounds
US6288061B1 (en) * 1997-12-26 2001-09-11 Welfide Corporation Imidazole derivatives
ATE346064T1 (de) * 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
ES2274005T3 (es) * 2001-01-26 2007-05-16 Chugai Seiyaku Kabushiki Kaisha Inhibidores de malonyl-coa decarboxilasa usados como moduladores metabolicos.
NZ544756A (en) 2003-07-22 2009-09-25 Astex Therapeutics Ltd 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
WO2005123671A1 (ja) * 2004-06-22 2005-12-29 Taisho Pharmaceutical Co., Ltd. ピロール誘導体
FR2881426B1 (fr) 2005-02-03 2007-03-30 Aventis Pharma Sa Pyrolles et imidazoles substitues, compositions les contenant, procede de frabrication et utilisation
US7589214B2 (en) * 2006-04-11 2009-09-15 Vertex Pharmaceuticals Incorporated Thiazoles, imidazoles, and pyrazoles useful as inhibitors of protein kinases

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ES2376765T3 (es) 2012-03-16
CN101460466B (zh) 2012-06-13
CN101460466A (zh) 2009-06-17
WO2007117692A2 (en) 2007-10-18
US7589214B2 (en) 2009-09-15
AU2007235237B2 (en) 2011-08-18
US8236832B2 (en) 2012-08-07
US20070298065A1 (en) 2007-12-27
US20090306155A1 (en) 2009-12-10
EP2007732B1 (en) 2011-11-23
AU2007235237A1 (en) 2007-10-18
WO2007117692A3 (en) 2008-01-10
US20130090479A1 (en) 2013-04-11
EP2007732A2 (en) 2008-12-31
JP2009536617A (ja) 2009-10-15
ATE534632T1 (de) 2011-12-15
US8865751B2 (en) 2014-10-21

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