JP5681723B2 - 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 - Google Patents

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 Download PDF

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JP5681723B2
JP5681723B2 JP2012540093A JP2012540093A JP5681723B2 JP 5681723 B2 JP5681723 B2 JP 5681723B2 JP 2012540093 A JP2012540093 A JP 2012540093A JP 2012540093 A JP2012540093 A JP 2012540093A JP 5681723 B2 JP5681723 B2 JP 5681723B2
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compound
salt
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pharmaceutical composition
compounds
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JP2013511547A (ja
JP2013511547A5 (https=
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ラジンダー シン
ラジンダー シン
ソマセカー バミディパティ
ソマセカー バミディパティ
ジェフリー クロウ
ジェフリー クロウ
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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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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
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    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • 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 Table
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Engineering & Computer Science (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2012540093A 2009-11-20 2010-11-19 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 Expired - Fee Related JP5681723B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US26316909P 2009-11-20 2009-11-20
US61/263,169 2009-11-20
PCT/US2010/057442 WO2011063241A1 (en) 2009-11-20 2010-11-19 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses

Publications (3)

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JP2013511547A JP2013511547A (ja) 2013-04-04
JP2013511547A5 JP2013511547A5 (https=) 2014-01-16
JP5681723B2 true JP5681723B2 (ja) 2015-03-11

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JP2012540093A Expired - Fee Related JP5681723B2 (ja) 2009-11-20 2010-11-19 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

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US (2) US8389515B2 (https=)
EP (1) EP2501705B1 (https=)
JP (1) JP5681723B2 (https=)
CA (1) CA2780777C (https=)
ES (1) ES2524127T3 (https=)
WO (1) WO2011063241A1 (https=)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10525152B2 (en) 2009-10-09 2020-01-07 Signablok, Inc. Methods and compositions for targeted imaging
JP5681723B2 (ja) 2009-11-20 2015-03-11 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
CA2792278C (en) 2010-04-13 2019-05-14 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
HRP20190186T4 (hr) 2011-07-28 2024-12-20 Rigel Pharmaceuticals, Inc. Nove formulacije (trimetoksifenilamino)pirimidinila
US9480745B2 (en) 2012-02-29 2016-11-01 University Hospitals Cleveland Medical Center Targeted treatment of anerobic cancer
CN103958526B (zh) * 2012-06-20 2015-09-09 上海恒瑞医药有限公司 嘧啶二胺类衍生物、其制备方法及其在医药上的应用
RU2519546C1 (ru) * 2013-01-16 2014-06-10 Общество С Ограниченной Ответственностью "Биоинтегратор" (Ооо "Биоинтегратор") КОНЪЮГАТЫ И МАЛЫЕ МОЛЕКУЛЫ, ВЗАИМОДЕЙСТВУЮЩИЕ С РЕЦЕПТОРОМ CD16а
SI3083648T1 (sl) * 2013-12-20 2019-02-28 Rigel Pharmaceuticals, Inc., Farmacevtski postopek in vmesne spojine
US10981951B2 (en) * 2014-01-31 2021-04-20 Mayo Foundation For Medical Education And Research Therapeutics for the treatment of glaucoma
CA3159771A1 (en) 2019-12-12 2021-06-17 Thurein M. Htoo Controlled-delivery cromakalim prodrugs
WO2022175829A1 (en) * 2021-02-17 2022-08-25 Cellix Bio Private Limited Topical formulations and compositions
US20250017895A1 (en) * 2021-11-29 2025-01-16 The Children's Hospital Of Philadelphia Flavanoid containing compositions and methods of use thereof for the treatment of mitochondrial disorders
CN119431398A (zh) * 2023-07-31 2025-02-14 中国科学院上海有机化学研究所 R406及其衍生物协同trail的抗肿瘤应用

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6573256B2 (en) 1996-12-30 2003-06-03 Bone Care International, Inc. Method of inhibiting angiogenesis using active vitamin D analogues
FR2785284B1 (fr) 1998-11-02 2000-12-01 Galderma Res & Dev Analogues de la vitamine d
US6358939B1 (en) 1999-12-21 2002-03-19 Northern Lights Pharmaceuticals, Llc Use of biologically active vitamin D compounds for the prevention and treatment of inflammatory bowel disease
US6924400B2 (en) 2001-12-10 2005-08-02 Galderma Research & Development, Snc Triaromatic vitamin D analogues
US6849245B2 (en) * 2001-12-11 2005-02-01 Catalytic Materials Llc Catalysts for producing narrow carbon nanostructures
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
EP1635773A2 (en) 2003-06-06 2006-03-22 Merck & Co., Inc. (a New Jersey corp.) Combination therapy for the treatment of hypertension
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
US20070092888A1 (en) 2003-09-23 2007-04-26 Cornelius Diamond Diagnostic markers of hypertension and methods of use thereof
AU2006206458B2 (en) * 2005-01-19 2012-10-25 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
US8227455B2 (en) * 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
JP2008013527A (ja) * 2006-07-10 2008-01-24 Sankyo Co Ltd チエノ[3,2−d]ピリミジン−2,4−ジアミン誘導体
ATE540041T1 (de) * 2006-11-21 2012-01-15 Rigel Pharmaceuticals Inc Prodrug-salze von 2,4-pyrimidindiaminverbindungen und anwendungen davon
JP5815411B2 (ja) * 2008-12-30 2015-11-17 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 ピリミジンジアミンキナーゼ阻害剤
JP5681723B2 (ja) 2009-11-20 2015-03-11 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

Also Published As

Publication number Publication date
US20110124599A1 (en) 2011-05-26
WO2011063241A1 (en) 2011-05-26
JP2013511547A (ja) 2013-04-04
US8642593B2 (en) 2014-02-04
EP2501705A1 (en) 2012-09-26
CA2780777C (en) 2017-12-05
US20130150329A1 (en) 2013-06-13
EP2501705B1 (en) 2014-08-27
US8389515B2 (en) 2013-03-05
CA2780777A1 (en) 2011-05-26
ES2524127T3 (es) 2014-12-04

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