CA2801781C - Protein kinase c inhibitors and uses thereof - Google Patents

Protein kinase c inhibitors and uses thereof Download PDF

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Publication number
CA2801781C
CA2801781C CA2801781A CA2801781A CA2801781C CA 2801781 C CA2801781 C CA 2801781C CA 2801781 A CA2801781 A CA 2801781A CA 2801781 A CA2801781 A CA 2801781A CA 2801781 C CA2801781 C CA 2801781C
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alkyl
compound
substituted
salt
hydrogen
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English (en)
French (fr)
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CA2801781A1 (en
Inventor
Sacha Holland
Rao Kolluri
Salvador Alvarez
Matthew Duncton
Rajinder Singh
Jing Zhang
Esteban Masuda
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Rigel Pharmaceuticals Inc
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Rigel Pharmaceuticals Inc
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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
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    • 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
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    • C—CHEMISTRY; METALLURGY
    • 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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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • 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)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Microbiology (AREA)
CA2801781A 2010-07-21 2011-07-21 Protein kinase c inhibitors and uses thereof Active CA2801781C (en)

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

Publications (2)

Publication Number Publication Date
CA2801781A1 CA2801781A1 (en) 2012-01-26
CA2801781C true CA2801781C (en) 2018-02-27

Family

ID=44533110

Family Applications (1)

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CA2801781A Active CA2801781C (en) 2010-07-21 2011-07-21 Protein kinase c inhibitors and uses thereof

Country Status (5)

Country Link
US (2) US8710223B2 (https=)
EP (1) EP2595982B1 (https=)
JP (1) JP6035238B2 (https=)
CA (1) CA2801781C (https=)
WO (1) WO2012012619A1 (https=)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
US7722620B2 (en) 2004-12-06 2010-05-25 Dfine, Inc. Bone treatment systems and methods
JP5781943B2 (ja) * 2009-01-21 2015-09-24 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 炎症性疾患、自己免疫疾患または増殖性疾患の治療に有用なｎ２−（３−ピリジルまたはフェニル）−ｎ４−（４−ピペリジル）−２，４−ピリミジンジアミン誘導体
US9139534B2 (en) 2011-04-22 2015-09-22 Signal Pharmaceuticals, Llc Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
EP2825887A4 (en) * 2012-03-15 2015-08-19 Montana Molecular Llc GENETICALLY-CODED, FLUORESCENT SENSORS FOR THE DETECTION OF INTRA-CELLULAR SIGNALS BY DIACYLGLYCEROL SIGNAL PATHS
ES2658395T3 (es) 2012-04-04 2018-03-09 Rigel Pharmaceuticals, Inc. Inhibidores de proteína cinasa C y usos de los mismos
EP2928891B1 (en) 2012-12-04 2019-02-20 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
CA2904610A1 (en) 2013-03-14 2014-09-25 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
US11366114B2 (en) 2013-11-04 2022-06-21 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
WO2015148867A1 (en) 2014-03-28 2015-10-01 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
WO2016060963A1 (en) 2014-10-14 2016-04-21 Sunshine Lake Pharma Co., Ltd. Substituted heteroaryl compounds and methods of use
CN107108524A (zh) 2014-12-16 2017-08-29 西格诺药品有限公司 2‑(叔丁基氨基)‑4‑((1r,3r,4r)‑3‑羟基‑4‑甲基环己基氨基)‑嘧啶‑5‑甲酰胺的配制物
US9513297B2 (en) 2014-12-16 2016-12-06 Signal Pharmaceuticals, Llc Methods for measurement of inhibition of c-Jun N-terminal kinase in skin
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
CN107922287B (zh) 2015-07-24 2021-04-09 细胞基因公司 合成(1r,2r,5r)-5-氨基-2-甲基环己醇盐酸盐的方法和其中可用的中间体
JP2018527362A (ja) 2015-09-11 2018-09-20 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． 置換されたヘテロアリール化合物および使用方法
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

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
WO2004043386A2 (en) 2002-11-08 2004-05-27 Tolerrx, Inc. Molecules preferentially associated with effector t cells and methods of their use
WO2005012294A1 (en) 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
ATE506953T1 (de) * 2003-08-07 2011-05-15 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
US20050164323A1 (en) 2003-12-24 2005-07-28 Wyeth Methods of treating asthma
BRPI0610876B8 (pt) 2005-06-08 2021-05-25 Rigel Pharmaceuticals Inc composto, formulação farmacêutica, e métodos de inibir uma atividade de uma jak cinase, e de inibir uma cascata de transdução de sinal em que jak3 cinase desempenha um papel
NZ541934A (en) 2005-08-19 2008-05-30 Splintiz Invest Ltd Carbonated milk product comprising a combination of agents that control the foaming of the product while retaining an effective effervescence in the carbonated milk-based beverage
CN101903357A (zh) 2007-07-17 2010-12-01 里格尔药品股份有限公司 作为pkc抑制剂的环状胺取代的嘧啶二胺
HRP20161310T1 (hr) * 2008-04-16 2016-12-02 Portola Pharmaceuticals, Inc. 2,6-diamino-pirimidin-5-il-karboksamidi kao inhibitori syk ili jak kinaza
TW201016676A (en) * 2008-10-03 2010-05-01 Astrazeneca Ab Heterocyclic derivatives and methods of use thereof
JP5781942B2 (ja) 2009-01-14 2015-09-24 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 ２，４−ピリミジンジアミン化合物を用いた炎症性障害の治療法
JP5603881B2 (ja) 2009-01-15 2014-10-08 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 プロテインキナーゼｃ阻害剤とその使用
JP5781943B2 (ja) * 2009-01-21 2015-09-24 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 炎症性疾患、自己免疫疾患または増殖性疾患の治療に有用なｎ２−（３−ピリジルまたはフェニル）−ｎ４−（４−ピペリジル）−２，４−ピリミジンジアミン誘導体
EP2507227B1 (en) 2009-12-01 2014-10-08 Rigel Pharmaceuticals, Inc. Tetrazolones as protein kinase c inhibitors and uses thereof

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US20120022092A1 (en) 2012-01-26
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CA2801781A1 (en) 2012-01-26
US9181222B2 (en) 2015-11-10

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