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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    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Epidemiology (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

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ID=44533110

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (OSRAM)
EP (1) EP2595982B1 (OSRAM)
JP (1) JP6035238B2 (OSRAM)
CA (1) CA2801781C (OSRAM)
WO (1) WO2012012619A1 (OSRAM)

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
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
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
UA120740C2 (uk) 2011-04-22 2020-02-10 Сігнал Фармасьютікалз, Елелсі Заміщені діамінокарбоксамідні і діамінокарбонітрильні похідні піримідинів, їх композиції і способи лікування з їх допомогою
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
JP6113828B2 (ja) 2012-04-04 2017-04-12 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阻害剤およびその使用
CA2892677A1 (en) 2012-12-04 2014-06-12 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
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
MX2016012574A (es) 2014-03-28 2017-09-26 Calitor Sciences Llc Compuestos heteroarilo sustituidos y metodos de uso.
JP6649540B2 (ja) 2014-10-14 2020-02-19 ノース・アンド・サウス・ブラザー・ファーマシー・インベストメント・カンパニー・リミテッド 置換されたヘテロアリール化合物および使用方法
CA3210612A1 (en) 2014-12-16 2016-06-23 Signal Pharmaceuticals, Llc Formulations of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
JP6903577B2 (ja) 2014-12-16 2021-07-14 シグナル ファーマシューティカルズ，エルエルシー 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法
WO2016123291A1 (en) 2015-01-29 2016-08-04 Signal Pharmaceuticals, Llc Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CA2993173C (en) 2015-07-24 2023-10-03 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
JP7254076B2 (ja) 2017-11-19 2023-04-07 サンシャイン・レイク・ファーマ・カンパニー・リミテッド 置換ヘテロアリール化合物及び使用方法
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
IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
WO2004043386A2 (en) 2002-11-08 2004-05-27 Tolerrx, Inc. Molecules preferentially associated with effector t cells and methods of their use
RS53109B (sr) * 2003-07-30 2014-06-30 Rigel Pharmaceuticals Inc. Jedinjenja 2,4 pirimidindiamina za upotrebu u tretmanu ili prevenciji autoimunih bolesti
ES2365223T3 (es) * 2003-08-07 2011-09-26 Rigel Pharmaceuticals, Inc. Compuestos 2,4-pirimidindiamínicos y usos como agentes antiproliferativos.
WO2005062918A2 (en) 2003-12-24 2005-07-14 Wyeth Methods of treating asthma
MX286273B (es) 2005-06-08 2011-05-04 Rigel Pharmaceuticals Inc Composiciones y metodos para inhibicion de la via jak.
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
WO2009012421A1 (en) 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
CN102066340B (zh) * 2008-04-16 2014-05-14 波托拉医药品公司 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物
WO2010038081A2 (en) * 2008-10-03 2010-04-08 Astrazeneca Ab Heterocyclic derivatives and methods of use thereof
CA2749248A1 (en) * 2009-01-14 2010-07-22 Rigel Pharmaceuticals, Inc. Methods for treating inflammatory disorders using 2,4-pyrimidinediamine compounds
EP2387572B1 (en) 2009-01-15 2015-09-16 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
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
JP5802677B2 (ja) 2009-12-01 2015-10-28 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阻害剤およびその使用

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US20120022092A1 (en) 2012-01-26
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US20140329842A1 (en) 2014-11-06
US8710223B2 (en) 2014-04-29

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