CA2780777C - 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses - Google Patents

2,4-pyrimidinediamine compounds and prodrugs thereof and their uses Download PDF

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Publication number
CA2780777C
CA2780777C CA2780777A CA2780777A CA2780777C CA 2780777 C CA2780777 C CA 2780777C CA 2780777 A CA2780777 A CA 2780777A CA 2780777 A CA2780777 A CA 2780777A CA 2780777 C CA2780777 C CA 2780777C
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Prior art keywords
compound
compounds
salt
cell
syk
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CA2780777A
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English (en)
French (fr)
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CA2780777A1 (en
Inventor
Rajinder Singh
Somasekhar Bhamidipati
Jeffrey Clough
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Rigel Pharmaceuticals Inc
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Rigel Pharmaceuticals Inc
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Publication of CA2780777A1 publication Critical patent/CA2780777A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2780777A 2009-11-20 2010-11-19 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses Active CA2780777C (en)

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 (2)

Publication Number Publication Date
CA2780777A1 CA2780777A1 (en) 2011-05-26
CA2780777C true CA2780777C (en) 2017-12-05

Family

ID=43430840

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2780777A Active CA2780777C (en) 2009-11-20 2010-11-19 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses

Country Status (6)

Country Link
US (2) US8389515B2 (enExample)
EP (1) EP2501705B1 (enExample)
JP (1) JP5681723B2 (enExample)
CA (1) CA2780777C (enExample)
ES (1) ES2524127T3 (enExample)
WO (1) WO2011063241A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011044545A2 (en) 2009-10-09 2011-04-14 Sigalov Alexander B Methods and compositions for targeted imaging
EP2501705B1 (en) 2009-11-20 2014-08-27 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
JP6067550B2 (ja) * 2010-04-13 2017-01-25 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
SMT201900071T1 (it) 2011-07-28 2019-02-28 Rigel Pharmaceuticals Inc Nuove formulazioni di (trimetossifenilammino)pirimidinile
WO2013130354A1 (en) * 2012-02-29 2013-09-06 University Hospitals Cleveland Medical Center Targeted treatment of anerobic cancer
WO2013189241A1 (zh) * 2012-06-20 2013-12-27 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
CA3186267C (en) * 2013-12-20 2025-09-09 Rigel Pharmaceuticals, Inc. PHARMACEUTICAL PROCESS AND INTERMEDIARIES
US10981951B2 (en) 2014-01-31 2021-04-20 Mayo Foundation For Medical Education And Research Therapeutics for the treatment of glaucoma
EP4072543A4 (en) 2019-12-12 2024-02-07 Qlaris Bio, Inc. CONTROLLED RELEASE 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
IL166241A0 (en) * 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
US20060160834A1 (en) 2003-06-06 2006-07-20 Fong Tung M Combination therapy for the treatment of hypertension
ES2421139T3 (es) * 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
DK1663242T3 (da) * 2003-08-07 2011-08-01 Rigel Pharmaceuticals Inc 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler
US20070092888A1 (en) 2003-09-23 2007-04-26 Cornelius Diamond Diagnostic markers of hypertension and methods of use thereof
US7449458B2 (en) * 2005-01-19 2008-11-11 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
WO2008064274A1 (en) 2006-11-21 2008-05-29 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses
EP2382210B1 (en) * 2008-12-30 2017-03-01 Rigel Pharmaceuticals, Inc. Pyrimidinediamine kinase inhibitors
EP2501705B1 (en) 2009-11-20 2014-08-27 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses

Also Published As

Publication number Publication date
WO2011063241A1 (en) 2011-05-26
JP5681723B2 (ja) 2015-03-11
JP2013511547A (ja) 2013-04-04
EP2501705A1 (en) 2012-09-26
US8389515B2 (en) 2013-03-05
CA2780777A1 (en) 2011-05-26
US20110124599A1 (en) 2011-05-26
EP2501705B1 (en) 2014-08-27
US20130150329A1 (en) 2013-06-13
ES2524127T3 (es) 2014-12-04
US8642593B2 (en) 2014-02-04

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