PE20051089A1 - PYRAZOLE [1,5-A] PYRIMIDIN-7-IL-AMINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - Google Patents

PYRAZOLE [1,5-A] PYRIMIDIN-7-IL-AMINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

Info

Publication number
PE20051089A1
PE20051089A1 PE2005000080A PE2005000080A PE20051089A1 PE 20051089 A1 PE20051089 A1 PE 20051089A1 PE 2005000080 A PE2005000080 A PE 2005000080A PE 2005000080 A PE2005000080 A PE 2005000080A PE 20051089 A1 PE20051089 A1 PE 20051089A1
Authority
PE
Peru
Prior art keywords
phenyl
pyrimidin
piperazin
methyl
pyrazole
Prior art date
Application number
PE2005000080A
Other languages
Spanish (es)
Inventor
Guido Bold
Andreas Floersheimer
Pascal Furet
Patricia Imbach
Keiichi Masuya
Joseph Schoepfer
Georg Martiny-Baron
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34807167&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20051089(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20051089A1 publication Critical patent/PE20051089A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Reproductive Health (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIRAZOLO [1,5-a] PIRIMIDIN-7-IL-AMINA DE FORMULA (I), EN DONDE R1 ES H, HALOGENO O ALQUILO INFERIOR; R2 ES H, ARILO, HETEROARILO, ALQUILO INFERIOR, CICLOALQUILO, BENCILO, BENZOTIENILO, INDOLILO ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS; R3 ES H, ALQUILO INFERIOR, OPCIONALMENTE SUSTITUIDOS; A ES H, HALOGENO, BENZOTIENILO, PIRIDILO, FENILO, PIPERAZINILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS. SON COMPUESTOS PREFERIDOS: 3-{7-AMINO-3-[4-(4-METIL-PIPERAZIN-1-IL)-FENIL]-PIRAZOLO-[1,5-A]-PIPRIMIDIN-6-IL}-FENOL, 6-(3-BENCILOXI-FENIL)-3-[4-(4-METIL-PIPERAZIN-1-IL)-FENIL]-PIRAZOLO[1,5-A]PIRIMIDIN-7-IL)-FENOL, 6-(3-METOXI-FENIL)-4-[4-(4-METIL-PIPERAZIN-1-IL)-FENIL]-PIRAZOLO[1,5-A]PIRIMIDIN-7-IL-AMINA, ENTRE OTROS. SE REFIERE A UNA COMPOSICION Y UN PROCESO DE PREPARACION. ESTOS COMPUESTOS SON INHIBIDORES DE QUINASA DE DIFERENTES GRADOS DE ESPECIFICIDAD, POR LO QUE SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES PROLIFERATIVAS TALES COMO TUMOR BENIGNO O MALIGNOREFERS TO COMPOUNDS DERIVED FROM PYRAZOLO [1,5-a] PYRIMIDIN-7-IL-AMINE OF FORMULA (I), WHERE R1 IS H, HALOGEN OR LOWER ALKYL; R2 IS H, ARYL, HETEROARYL, LOWER ALKYL, CYCLOALKYL, BENZYL, BENZOTHENYL, INDOLYL, AMONG OTHERS, OPTIONALLY SUBSTITUTED; R3 IS H, LOWER RENT, OPTIONALLY REPLACED; A IS H, HALOGEN, BENZOTHENYL, PYRIDYL, PHENYL, PIPERAZINYL, AMONG OTHERS, OPTIONALLY SUBSTITUTED. PREFERRED COMPOUNDS ARE: 3- {7-AMINO-3- [4- (4-METHYL-PIPERAZIN-1-IL) -PHENYL] -PIRAZOLO- [1,5-A] -PIPRIMIDIN-6-IL} -PHENOL, 6- (3-BENZYLOXY-PHENYL) -3- [4- (4-METHYL-PIPERAZIN-1-IL) -PHENYL] -PYRAZOLO [1,5-A] PYRIMIDIN-7-IL) -PHENOL, 6- ( 3-METHOXY-PHENYL) -4- [4- (4-METHYL-PIPERAZIN-1-IL) -PHENYL] -PIRAZOLO [1,5-A] PYRIMIDIN-7-IL-AMINE, AMONG OTHERS. IT REFERS TO A COMPOSITION AND A PREPARATION PROCESS. THESE COMPOUNDS ARE INHIBITORS OF KINASE OF DIFFERENT DEGREES OF SPECIFICITY, SO THEY ARE USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES SUCH AS BENIGN OR MALIGNANT TUMOR

PE2005000080A 2004-01-22 2005-01-20 PYRAZOLE [1,5-A] PYRIMIDIN-7-IL-AMINE DERIVATIVES AS PROTEIN KINASE INHIBITORS PE20051089A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US53822004P 2004-01-22 2004-01-22

Publications (1)

Publication Number Publication Date
PE20051089A1 true PE20051089A1 (en) 2006-01-25

Family

ID=34807167

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005000080A PE20051089A1 (en) 2004-01-22 2005-01-20 PYRAZOLE [1,5-A] PYRIMIDIN-7-IL-AMINE DERIVATIVES AS PROTEIN KINASE INHIBITORS

Country Status (17)

Country Link
EP (1) EP1708710A1 (en)
JP (1) JP2007519662A (en)
KR (1) KR20070009546A (en)
CN (1) CN1909908A (en)
AR (1) AR049769A1 (en)
AU (1) AU2005205915B2 (en)
BR (1) BRPI0507071A (en)
CA (1) CA2552885A1 (en)
EC (1) ECSP066718A (en)
IL (1) IL176737A0 (en)
MA (1) MA28400B1 (en)
NO (1) NO20063758L (en)
PE (1) PE20051089A1 (en)
RU (1) RU2006130003A (en)
TN (1) TNSN06226A1 (en)
TW (1) TW200528103A (en)
WO (1) WO2005070431A1 (en)

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Also Published As

Publication number Publication date
JP2007519662A (en) 2007-07-19
TW200528103A (en) 2005-09-01
AU2005205915B2 (en) 2009-05-21
RU2006130003A (en) 2008-04-10
TNSN06226A1 (en) 2007-12-03
EP1708710A1 (en) 2006-10-11
AR049769A1 (en) 2006-09-06
IL176737A0 (en) 2006-10-31
BRPI0507071A (en) 2007-06-19
WO2005070431A1 (en) 2005-08-04
NO20063758L (en) 2006-10-23
MA28400B1 (en) 2007-01-02
ECSP066718A (en) 2006-10-31
AU2005205915A1 (en) 2005-08-04
KR20070009546A (en) 2007-01-18
CA2552885A1 (en) 2005-08-04
CN1909908A (en) 2007-02-07

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