JP6035238B2 - プロテインキナーゼｃ阻害剤およびその使用 - Google Patents

プロテインキナーゼｃ阻害剤およびその使用 Download PDF

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JP6035238B2
JP6035238B2 JP2013520865A JP2013520865A JP6035238B2 JP 6035238 B2 JP6035238 B2 JP 6035238B2 JP 2013520865 A JP2013520865 A JP 2013520865A JP 2013520865 A JP2013520865 A JP 2013520865A JP 6035238 B2 JP6035238 B2 JP 6035238B2
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fluoro
substituted
alkyl
cyclopropyl
cycloalkyl
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JP2013531074A5 (enExample
JP2013531074A (ja
Inventor
ホランド，サッシャ
コルリ，ラオ
アルバレス，サルバドール
ダンクトン，マシュー
ラジンダー シング，
ラジンダー シング，
チャン，ジン
エステバン マスダ，
エステバン マスダ，
Original Assignee
ライジェル ファーマシューティカルズ， インコーポレイテッド
ライジェル ファーマシューティカルズ， インコーポレイテッド
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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
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    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
    • C12Y207/11—Protein-serine/threonine kinases (2.7.11)
    • C12Y207/11013—Protein kinase C (2.7.11.13)

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  • Organic Chemistry (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
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  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
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JP2013520865A 2010-07-21 2011-07-21 プロテインキナーゼｃ阻害剤およびその使用 Expired - Fee Related JP6035238B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36646410P 2010-07-21 2010-07-21
US61/366,464 2010-07-21
PCT/US2011/044824 WO2012012619A1 (en) 2010-07-21 2011-07-21 Protein kinase c inhibitors and uses thereof

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JP2013531074A JP2013531074A (ja) 2013-08-01
JP2013531074A5 JP2013531074A5 (enExample) 2014-09-04
JP6035238B2 true JP6035238B2 (ja) 2016-11-30

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US (2) US8710223B2 (enExample)
EP (1) EP2595982B1 (enExample)
JP (1) JP6035238B2 (enExample)
CA (1) CA2801781C (enExample)
WO (1) WO2012012619A1 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0645072B2 (ja) 1986-07-21 1994-06-15 住友特殊金属株式会社 耐食性バイメタル板の製造方法
JPH0645073B2 (ja) 1986-07-21 1994-06-15 住友特殊金属株式会社 耐食性バイメタル板の製造方法
JPH0645071B2 (ja) 1986-07-18 1994-06-15 住友特殊金属株式会社 バイメタル板の製造方法
JPH0647177B2 (ja) 1986-07-21 1994-06-22 住友特殊金属株式会社 耐食性バイメタル板の製造方法

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WO2010090875A1 (en) * 2009-01-21 2010-08-12 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
TWI548621B (zh) 2011-04-22 2016-09-11 標誌製藥公司 經取代之二胺基甲醯胺及二胺基甲腈嘧啶、其組合物、及以該等治療之方法
WO2013138684A1 (en) * 2012-03-15 2013-09-19 Montana Molecular Llc Genetically encoded fluorescent sensors for detecting intracellular signalling through diacylglycerol pathways
US9321763B2 (en) 2012-04-04 2016-04-26 Rigel Pharmaceuticals, Inc. Protein kinase C inhibitors and uses thereof
EP2928891B1 (en) 2012-12-04 2019-02-20 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
US9169249B2 (en) 2013-03-14 2015-10-27 Rigel Pharmaceuticals, Inc. Protein kinase C inhibitors and uses thereof
EP3738971B1 (en) 2013-11-04 2024-07-17 Montana Molecular LLC Genetically encoded fluorescent sensors for detecting ligand bias and intracellular signaling through camp pathways
NZ715903A (en) 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
US9399637B2 (en) 2014-03-28 2016-07-26 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US10059689B2 (en) 2014-10-14 2018-08-28 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
US9513297B2 (en) 2014-12-16 2016-12-06 Signal Pharmaceuticals, Llc Methods for measurement of inhibition of c-Jun N-terminal kinase in skin
EP3712134B1 (en) 2014-12-16 2023-11-29 Signal Pharmaceuticals, LLC Salts of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methycyclohexylamino)-pyrimidine-5-carboxamide
EP3250557B1 (en) 2015-01-29 2024-11-20 Signal Pharmaceuticals, LLC Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
EP3325432B1 (en) 2015-07-24 2020-09-02 Celgene Corporation Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
EP3347097B1 (en) 2015-09-11 2021-02-24 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora
EP3284739A1 (de) 2017-07-19 2018-02-21 Bayer CropScience Aktiengesellschaft Substituierte (het)arylverbindungen als schädlingsbekämpfungsmittel
WO2019099311A1 (en) 2017-11-19 2019-05-23 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
TW202045008A (zh) 2019-02-01 2020-12-16 印度商皮埃企業有限公司 4-取代的異噁唑/異噁唑啉(雜)芳基脒化合物、及其製備與用途

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IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
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JPH0645071B2 (ja) 1986-07-18 1994-06-15 住友特殊金属株式会社 バイメタル板の製造方法
JPH0645072B2 (ja) 1986-07-21 1994-06-15 住友特殊金属株式会社 耐食性バイメタル板の製造方法
JPH0645073B2 (ja) 1986-07-21 1994-06-15 住友特殊金属株式会社 耐食性バイメタル板の製造方法
JPH0647177B2 (ja) 1986-07-21 1994-06-22 住友特殊金属株式会社 耐食性バイメタル板の製造方法

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WO2012012619A1 (en) 2012-01-26
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