WO2008064274A1 - Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses - Google Patents

Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses Download PDF

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Publication number
WO2008064274A1
WO2008064274A1 PCT/US2007/085313 US2007085313W WO2008064274A1 WO 2008064274 A1 WO2008064274 A1 WO 2008064274A1 US 2007085313 W US2007085313 W US 2007085313W WO 2008064274 A1 WO2008064274 A1 WO 2008064274A1
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WO
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Patent type
Prior art keywords
prodrug
prodrugs
method
salt hydrate
prodrug salt
Prior art date
Application number
PCT/US2007/085313
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English (en)
French (fr)
Inventor
Somasekhar Bhamidipati
Rajinder Singh
Thomas Sun
Esteban Masuda
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Rigel Pharmaceuticals, Inc.
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
PCT/US2007/085313 2006-11-21 2007-11-20 Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses WO2008064274A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US86672206 true 2006-11-21 2006-11-21
US60/866,722 2006-11-21

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
DK07864696T DK2078026T3 (da) 2006-11-21 2007-11-20 Prodrug-salte af 2, 4-pyrimidinediamine-forbindelser og anvendelser deraf
EP20070864696 EP2078026B1 (en) 2006-11-21 2007-11-20 Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses
ES07864696T ES2380551T3 (es) 2006-11-21 2007-11-20 Sales de profármaco de compuestos de 2,4-pirimidindiamina y sus usos
AT07864696T AT540041T (de) 2006-11-21 2007-11-20 Prodrug-salze von 2,4-pyrimidindiaminverbindungen und anwendungen davon
CA 2673137 CA2673137C (en) 2006-11-21 2007-11-20 Prodrug salts of 2,4-pyrimidinediamine compounds and their uses
JP2009538501A JP5264759B2 (ja) 2006-11-21 2007-11-20 2,4−ピリミジンジアミン化合物のプロドラッグ塩およびそれらの使用
HK10100267A HK1133257A1 (en14) 2006-11-21 2010-01-11

Publications (1)

Publication Number Publication Date
WO2008064274A1 true true WO2008064274A1 (en) 2008-05-29

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Family Applications (1)

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PCT/US2007/085313 WO2008064274A1 (en) 2006-11-21 2007-11-20 Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses

Country Status (7)

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US (6) US8163902B2 (en14)
EP (2) EP2420505A1 (en14)
JP (1) JP5264759B2 (en14)
CA (1) CA2673137C (en14)
DK (1) DK2078026T3 (en14)
ES (1) ES2380551T3 (en14)
WO (1) WO2008064274A1 (en14)

Cited By (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010013158A1 (en) 2008-07-28 2010-02-04 Pfizer Inc. Phenanthrenone compounds, compositions and methods
WO2010027002A1 (ja) * 2008-09-05 2010-03-11 塩野義製薬株式会社 Pi3k阻害活性を有する縮環モルホリン誘導体
WO2010080563A3 (en) * 2008-12-18 2010-08-26 Sanofi-Aventis Method for treating macular degeneration
WO2011002999A1 (en) * 2009-07-02 2011-01-06 Rigel Pharmaceuticals, Inc. Synthesis of n4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy ] -3-oxo-5-pyrido [1, 4] oxazin-6-yl)-5-fluoro-n2- (3, 4, 5,-trimethoxyphenyl) -2, 4- pyrimidinediamine disodium salt
WO2011009075A2 (en) 2009-07-17 2011-01-20 Rigel Pharmaceuticals, Inc. Deuterated 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
WO2011063241A1 (en) 2009-11-20 2011-05-26 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
WO2011106248A2 (en) * 2010-02-24 2011-09-01 Auspex Pharmaceuticals, Inc. Trimethoxyphenyl inhibitors of tyrosine kinase
WO2011130390A1 (en) 2010-04-13 2011-10-20 Rigel Pharmaceuticals, Inc. 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
CN102746337A (zh) * 2012-06-21 2012-10-24 成都苑东药业有限公司 一种2,4-嘧啶二胺类化合物及其制备方法
US20130058876A1 (en) * 2011-07-28 2013-03-07 Astrazeneca Ab (trimethoxyphenylamino) pyrimidinyl formulations
US8440689B2 (en) 2009-12-23 2013-05-14 Takeda Pharmaceutical Company Limited Fused heteroaromatic pyrrolidinones
US8524733B2 (en) 2008-09-18 2013-09-03 Auspex Pharmaceuticals Benzoquinoline inhibitors of vesicular monoamine transporter 2
US8703782B2 (en) 2011-05-17 2014-04-22 Novartis Ag Substituted indole derivatives
US8895545B2 (en) 2006-07-20 2014-11-25 Debiopharm International Sa Acrylamide derivatives as Fab I inhibitors
US8901105B2 (en) 2012-06-19 2014-12-02 Debiopharm International Sa Prodrug derivatives of (E)-N-methyl-N-((3-M ethylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
US8975249B2 (en) 2010-11-01 2015-03-10 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
US9056873B2 (en) 2011-06-22 2015-06-16 Takeda Pharmaceutical Company Limited Substituted 6-aza-isoindolin-1-one derivatives
US9056839B2 (en) 2012-03-15 2015-06-16 Celgene Avilomics Research, Inc. Solid forms of an epidermal growth factor receptor kinase inhibitor
US9108927B2 (en) 2012-03-15 2015-08-18 Celgene Avilomics Research, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US9145387B2 (en) 2013-02-08 2015-09-29 Celgene Avilomics Research, Inc. ERK inhibitors and uses thereof
US9212181B2 (en) 2008-06-27 2015-12-15 Celgene Avilomics Research, Inc. Substituted 2,4-diaminopyrimidines as kinase inhibitors
US9233959B2 (en) 2012-09-18 2016-01-12 Auspex Pharmaceuticals, Inc. Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9238629B2 (en) 2010-11-01 2016-01-19 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US9295650B2 (en) 2010-05-14 2016-03-29 Mallinckrodt Llc Functional, cross-linked nanostructures for tandem optical imaging and therapy
US9364476B2 (en) 2011-10-28 2016-06-14 Celgene Avilomics Research, Inc. Methods of treating a Bruton's Tyrosine Kinase disease or disorder
US9409887B2 (en) 2010-11-10 2016-08-09 Celgene Avilomics Research, Inc. Mutant-selective EGFR inhibitors and uses thereof
US9409921B2 (en) 2008-06-27 2016-08-09 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines as kinase inhibitors
CN105849115A (zh) * 2013-12-20 2016-08-10 里格尔药品股份有限公司 制药方法和中间体
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
US9550780B2 (en) 2012-09-18 2017-01-24 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9604936B2 (en) 2010-08-10 2017-03-28 Celgene Car Llc Besylate salt of a BTK inhibitor
US10005760B2 (en) 2014-08-13 2018-06-26 Celgene Car Llc Forms and compositions of an ERK inhibitor

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2608367C (en) 2005-06-08 2014-08-19 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2007120980A3 (en) * 2006-02-17 2007-12-27 Somasekhar Bhamidipati 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
ES2380551T3 (es) 2006-11-21 2012-05-16 Rigel Pharmaceuticals, Inc. Sales de profármaco de compuestos de 2,4-pirimidindiamina y sus usos
ES2552518T3 (es) * 2012-02-21 2015-11-30 Merck Patent Gmbh Derivados cíclicos de diaminopiridina como inhibidores de Syk

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5958935A (en) 1995-11-20 1999-09-28 Celltech Therapeutics Limited Substituted 2-anilinopyrimidines useful as protein kinase inhibitors
WO2003063794A2 (en) 2002-02-01 2003-08-07 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
WO2004014382A1 (en) 2002-07-29 2004-02-19 Rigel Pharmaceuticals Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
US20050028212A1 (en) 2003-07-31 2005-02-03 Laronne Shai A. Automated digital voice recorder to personal information manager synchronization
WO2005016893A2 (en) 2003-07-30 2005-02-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
WO2006078846A1 (en) 2005-01-19 2006-07-27 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5087240A (en) 1983-08-18 1992-02-11 Drug Delivery Systems Inc. Transdermal drug patch with conductive fibers
US4921475A (en) 1983-08-18 1990-05-01 Drug Delivery Systems Inc. Transdermal drug patch with microtubes
US4738851A (en) 1985-09-27 1988-04-19 University Of Iowa Research Foundation, Inc. Controlled release ophthalmic gel formulation
US5163899A (en) 1987-03-20 1992-11-17 Drug Delivery Systems Inc. Transdermal drug delivery system
US5312325A (en) 1987-05-28 1994-05-17 Drug Delivery Systems Inc Pulsating transdermal drug delivery system
GB8804164D0 (en) 1988-02-23 1988-03-23 Tucker J M Bandage for administering physiologically active compound
US4882150A (en) 1988-06-03 1989-11-21 Kaufman Herbert E Drug delivery system
US5008110A (en) 1988-11-10 1991-04-16 The Procter & Gamble Company Storage-stable transdermal patch
US5088977A (en) 1988-12-21 1992-02-18 Drug Delivery Systems Inc. Electrical transdermal drug applicator with counteractor and method of drug delivery
US5521222A (en) 1989-09-28 1996-05-28 Alcon Laboratories, Inc. Topical ophthalmic pharmaceutical vehicles
DK0431519T3 (da) 1989-12-04 1994-07-04 Searle & Co System til transdermal indgivelse af albuterol
US5077033A (en) 1990-08-07 1991-12-31 Mediventures Inc. Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide
JP2594486B2 (ja) 1991-01-15 1997-03-26 アルコン ラボラトリーズ インコーポレイテッド 局所的眼薬組成物
US5352456A (en) 1991-10-10 1994-10-04 Cygnus Therapeutic Systems Device for administering drug transdermally which provides an initial pulse of drug
WO1993011938A1 (en) 1991-12-18 1993-06-24 Minnesota Mining And Manufacturing Company Multilayered barrier structures
EP0553769B1 (de) 1992-01-29 1996-01-03 FRANZ VÖLKL GmbH & CO. SKI UND TENNIS SPORTARTIKELFABRIK KG Ballspielschläger, insbesondere Tennisschläger
ES2094688B1 (es) 1994-08-08 1997-08-01 Cusi Lab Manoemulsion del tipo de aceite en agua, util como vehiculo oftalmico y procedimiento para su preparacion.
US5800807A (en) 1997-01-29 1998-09-01 Bausch & Lomb Incorporated Ophthalmic compositions including glycerin and propylene glycol
US6261547B1 (en) 1998-04-07 2001-07-17 Alcon Manufacturing, Ltd. Gelling ophthalmic compositions containing xanthan gum
US6197934B1 (en) 1998-05-22 2001-03-06 Collagenesis, Inc. Compound delivery using rapidly dissolving collagen film
EP1786783A1 (en) * 2004-09-01 2007-05-23 Rigel Pharmaceuticals, Inc. Synthesis of 2,4-pyrimidinediamine compounds
WO2006068770A1 (en) * 2004-11-24 2006-06-29 Rigel Pharmaceuticals, Inc. Spiro-2, 4-pyrimidinediamine compounds and their uses
EP1883302A4 (en) * 2005-05-03 2009-05-20 Rigel Pharmaceuticals Inc Jak kinase inhibitors and their uses
CA2608367C (en) 2005-06-08 2014-08-19 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20070203161A1 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7576053B2 (en) * 2005-06-13 2009-08-18 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders
EP1951261A4 (en) * 2005-10-31 2009-06-24 Rigel Pharmaceuticals Inc Compositions and methods for treating inflammatory disorders
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
WO2007120980A3 (en) * 2006-02-17 2007-12-27 Somasekhar Bhamidipati 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
EP1991532B1 (en) * 2006-02-24 2017-01-11 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
ES2380551T3 (es) 2006-11-21 2012-05-16 Rigel Pharmaceuticals, Inc. Sales de profármaco de compuestos de 2,4-pirimidindiamina y sus usos
US7947698B2 (en) * 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
WO2008118823A3 (en) * 2007-03-26 2009-05-14 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the jak pathway
KR20100049068A (ko) 2007-07-17 2010-05-11 리겔 파마슈티칼스, 인크. Pkc 억제제로서의 시클릭 아민 치환된 피리미딘디아민

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5958935A (en) 1995-11-20 1999-09-28 Celltech Therapeutics Limited Substituted 2-anilinopyrimidines useful as protein kinase inhibitors
WO2003063794A2 (en) 2002-02-01 2003-08-07 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
US20040029902A1 (en) 2002-02-01 2004-02-12 Rajinder Singh 2,4-Pyrimidinediamine compounds and their uses
WO2004014382A1 (en) 2002-07-29 2004-02-19 Rigel Pharmaceuticals Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
WO2005016893A2 (en) 2003-07-30 2005-02-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
US20050234049A1 (en) 2003-07-30 2005-10-20 Rajinder Singh Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds
US20050028212A1 (en) 2003-07-31 2005-02-03 Laronne Shai A. Automated digital voice recorder to personal information manager synchronization
WO2006078846A1 (en) 2005-01-19 2006-07-27 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
KONISHI ET AL., CIRCULATION, vol. 105, 2002, pages 912 - 916
MOCSAI ET AL., IMMUNITY, vol. 16, 2002, pages 547 - 558
MONTEIRO; VAN DE WINKEL, ANNU. REV. IMMUNOL, 2003
TURNER ET AL., IMMUNOLOGY TODAY, vol. 21, 2000, pages 148 - 154
WATSON; GIBBONS, IMMUNOL. TODAY, vol. 19, 1998, pages 260 - 264

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US8895545B2 (en) 2006-07-20 2014-11-25 Debiopharm International Sa Acrylamide derivatives as Fab I inhibitors
US9212181B2 (en) 2008-06-27 2015-12-15 Celgene Avilomics Research, Inc. Substituted 2,4-diaminopyrimidines as kinase inhibitors
US9409921B2 (en) 2008-06-27 2016-08-09 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines as kinase inhibitors
US10010548B2 (en) 2008-06-27 2018-07-03 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
US9296737B2 (en) 2008-06-27 2016-03-29 Celgene Avilomics Research, Inc. Substituted 2,4-diaminopyrimidines as kinase inhibitors
US9987276B2 (en) 2008-06-27 2018-06-05 Celgene Car Llc Substituted 2,4-diaminopyrimidines as kinase inhibitors
US8148409B2 (en) 2008-07-28 2012-04-03 Pfizer Inc. Phenathrenone compounds, compositons and methods
US8552035B2 (en) 2008-07-28 2013-10-08 Pfizer Inc. Phenanthrenone compounds, compositions and methods
WO2010013158A1 (en) 2008-07-28 2010-02-04 Pfizer Inc. Phenanthrenone compounds, compositions and methods
WO2010027002A1 (ja) * 2008-09-05 2010-03-11 塩野義製薬株式会社 Pi3k阻害活性を有する縮環モルホリン誘導体
US8524733B2 (en) 2008-09-18 2013-09-03 Auspex Pharmaceuticals Benzoquinoline inhibitors of vesicular monoamine transporter 2
CN102316868A (zh) * 2008-12-18 2012-01-11 赛诺菲 用于治疗黄斑变性的方法
JP2012512895A (ja) * 2008-12-18 2012-06-07 サノフイ 黄斑変性症を処置する方法
WO2010080563A3 (en) * 2008-12-18 2010-08-26 Sanofi-Aventis Method for treating macular degeneration
WO2011002999A1 (en) * 2009-07-02 2011-01-06 Rigel Pharmaceuticals, Inc. Synthesis of n4- (2, 2-dimethyl-4- [ (dihydrogen phosphonoxy ] -3-oxo-5-pyrido [1, 4] oxazin-6-yl)-5-fluoro-n2- (3, 4, 5,-trimethoxyphenyl) -2, 4- pyrimidinediamine disodium salt
US8691798B2 (en) 2009-07-02 2014-04-08 Rigel Pharmaceuticals, Inc. Synthesis of 2,4-pyrimidinediamines
US8299242B2 (en) 2009-07-02 2012-10-30 Rigel Pharmaceuticals, Inc. Synthesis of 2,4-pyrimidinediamines
JP2012532143A (ja) * 2009-07-02 2012-12-13 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 N4−(2,2−ジメチル−4−[(二水素ホスホノオキシ)メチル]−3−オキソ−5−ピリド[1,4]オキサジン−6−イル)−5−フルオロ−n2−(3,4,5−トリメトキシフェニル)−2,4−ピリミジンジアミン二ナトリウム塩の合成
US8481724B2 (en) 2009-07-02 2013-07-09 Rigel Pharmaceuticals, Inc. Synthesis of 2,4-pyrimidinediamines
CN102482305A (zh) * 2009-07-02 2012-05-30 里格尔药品股份有限公司 N4-(2,2-二甲基-4-[(二氢膦酰氧基)甲基]-3-氧代-5-吡啶并[1,4]噁嗪-6-基)-5-氟-n2-(3,4,5-三甲氧基苯基)-2,4-嘧啶二胺二钠盐的合成
WO2011009075A3 (en) * 2009-07-17 2011-09-09 Rigel Pharmaceuticals, Inc. Deuterated 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
WO2011009075A2 (en) 2009-07-17 2011-01-20 Rigel Pharmaceuticals, Inc. Deuterated 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
WO2011063241A1 (en) 2009-11-20 2011-05-26 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
US8389515B2 (en) 2009-11-20 2013-03-05 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs and their uses
US8642593B2 (en) 2009-11-20 2014-02-04 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs and their uses
JP2013511547A (ja) * 2009-11-20 2013-04-04 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およびそのプロドラッグならびにそれらの使用
US8440689B2 (en) 2009-12-23 2013-05-14 Takeda Pharmaceutical Company Limited Fused heteroaromatic pyrrolidinones
US9108970B2 (en) 2009-12-23 2015-08-18 Takeda Pharmaceutical Company Limited Fused heteroaromatic pyrrolidinones
US9181255B2 (en) 2009-12-23 2015-11-10 Takeda Pharmaceutical Company Limited Fused heteroaromatic pyrrolidinones as SYK inhibitors
WO2011106248A3 (en) * 2010-02-24 2012-01-05 Auspex Pharmaceuticals, Inc. Trimethoxyphenyl inhibitors of tyrosine kinase
WO2011106248A2 (en) * 2010-02-24 2011-09-01 Auspex Pharmaceuticals, Inc. Trimethoxyphenyl inhibitors of tyrosine kinase
CN102892770A (zh) * 2010-02-24 2013-01-23 奥斯拜客斯制药有限公司 酪氨酸激酶三甲氧苯基抑制剂
WO2011130390A1 (en) 2010-04-13 2011-10-20 Rigel Pharmaceuticals, Inc. 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
US9662387B2 (en) 2010-05-14 2017-05-30 Mallinckrodt Llc Functional, cross-linked nanostructures for tandem optical imaging and therapy
US9295650B2 (en) 2010-05-14 2016-03-29 Mallinckrodt Llc Functional, cross-linked nanostructures for tandem optical imaging and therapy
US9604936B2 (en) 2010-08-10 2017-03-28 Celgene Car Llc Besylate salt of a BTK inhibitor
US8975249B2 (en) 2010-11-01 2015-03-10 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
US9867824B2 (en) 2010-11-01 2018-01-16 Celgene Car Llc Heterocyclic compounds and uses thereof
US9238629B2 (en) 2010-11-01 2016-01-19 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US9765038B2 (en) 2010-11-01 2017-09-19 Celgene Car Llc Heteroaryl compounds and uses thereof
US9375431B2 (en) 2010-11-01 2016-06-28 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidine compounds useful as kinase inhibtors
US10081606B2 (en) 2010-11-01 2018-09-25 Celgene Car Llc Heteroaryl compounds and uses thereof
US9868723B2 (en) 2010-11-10 2018-01-16 Celgene Car Llc Mutant-selective EGFR inhibitors and uses thereof
US9409887B2 (en) 2010-11-10 2016-08-09 Celgene Avilomics Research, Inc. Mutant-selective EGFR inhibitors and uses thereof
US8703782B2 (en) 2011-05-17 2014-04-22 Novartis Ag Substituted indole derivatives
US9029396B2 (en) 2011-05-17 2015-05-12 Novartis Ag Substituted indole derivatives
US9663514B2 (en) 2011-06-22 2017-05-30 Takeda Pharmaceutical Company Limited Substituted 6-aza-isoindolin-1-one derivatives
US9056873B2 (en) 2011-06-22 2015-06-16 Takeda Pharmaceutical Company Limited Substituted 6-aza-isoindolin-1-one derivatives
US20130058876A1 (en) * 2011-07-28 2013-03-07 Astrazeneca Ab (trimethoxyphenylamino) pyrimidinyl formulations
US8951504B2 (en) 2011-07-28 2015-02-10 Rigel Pharmaceuticals, Inc. (trimethoxyphenylamino) pyrimidinyl formulations
US8771648B2 (en) * 2011-07-28 2014-07-08 Rigel Pharmaceuticals, Inc. (Trimethoxyphenylamino) pyrimidinyl formulations
US9364476B2 (en) 2011-10-28 2016-06-14 Celgene Avilomics Research, Inc. Methods of treating a Bruton's Tyrosine Kinase disease or disorder
US9540335B2 (en) 2012-03-15 2017-01-10 Celgene Avilomics Research, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
US10004741B2 (en) 2012-03-15 2018-06-26 Celgene Car Llc Solid forms of an epidermal growth factor receptor kinase inhibitor
US9056839B2 (en) 2012-03-15 2015-06-16 Celgene Avilomics Research, Inc. Solid forms of an epidermal growth factor receptor kinase inhibitor
US9108927B2 (en) 2012-03-15 2015-08-18 Celgene Avilomics Research, Inc. Salts of an epidermal growth factor receptor kinase inhibitor
US9539255B2 (en) 2012-03-15 2017-01-10 Celgene Avilomics Research, Inc. Solid forms of an epidermal growth factor receptor kinase inhibitor
US10005738B2 (en) 2012-03-15 2018-06-26 Celgene Car Llc Salts of an epidermal growth factor receptor kinase inhibitor
US8901105B2 (en) 2012-06-19 2014-12-02 Debiopharm International Sa Prodrug derivatives of (E)-N-methyl-N-((3-M ethylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
US10035813B2 (en) 2012-06-19 2018-07-31 Debiopharm International Sa Prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide
CN102746337A (zh) * 2012-06-21 2012-10-24 成都苑东药业有限公司 一种2,4-嘧啶二胺类化合物及其制备方法
US9550780B2 (en) 2012-09-18 2017-01-24 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9346800B2 (en) 2012-09-18 2016-05-24 Auspex Pharmaceuticals, Inc. Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9296739B2 (en) 2012-09-18 2016-03-29 Auspex Pharmaceuticals, Inc. Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9814708B2 (en) 2012-09-18 2017-11-14 Auspex Pharmaceuticals, Inc. Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9233959B2 (en) 2012-09-18 2016-01-12 Auspex Pharmaceuticals, Inc. Formulations and pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2
US9549927B2 (en) 2012-12-21 2017-01-24 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US9796700B2 (en) 2013-02-08 2017-10-24 Celgene Car Llc ERK inhibitors and uses thereof
US9504686B2 (en) 2013-02-08 2016-11-29 Celgene Avilomics Research, Inc. ERK inhibitors and uses thereof
US9561228B2 (en) 2013-02-08 2017-02-07 Celgene Avilomics Research, Inc. ERK inhibitors and uses thereof
US9145387B2 (en) 2013-02-08 2015-09-29 Celgene Avilomics Research, Inc. ERK inhibitors and uses thereof
US9980964B2 (en) 2013-02-08 2018-05-29 Celgene Car Llc ERK inhibitors and uses thereof
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
US9695204B2 (en) * 2013-12-20 2017-07-04 Rigel Pharmaceuticals, Inc. Pharmaceutical process and intermediates
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CN105849115A (zh) * 2013-12-20 2016-08-10 里格尔药品股份有限公司 制药方法和中间体
US10005760B2 (en) 2014-08-13 2018-06-26 Celgene Car Llc Forms and compositions of an ERK inhibitor

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