PE20050325A1 - DERIVADOS DE PIRROLO[3,4-c]PIRAZOL ACTIVOS COMO INHIBIDORES DE QUINASA, PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN - Google Patents

DERIVADOS DE PIRROLO[3,4-c]PIRAZOL ACTIVOS COMO INHIBIDORES DE QUINASA, PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN

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Publication number
PE20050325A1
PE20050325A1 PE2004000657A PE2004000657A PE20050325A1 PE 20050325 A1 PE20050325 A1 PE 20050325A1 PE 2004000657 A PE2004000657 A PE 2004000657A PE 2004000657 A PE2004000657 A PE 2004000657A PE 20050325 A1 PE20050325 A1 PE 20050325A1
Authority
PE
Peru
Prior art keywords
pirazole
pirrolo
derivatives
phenylethanoyl
tetrahydropyrrolo
Prior art date
Application number
PE2004000657A
Other languages
English (en)
Inventor
Daniele Fancelli
Barbara Forte
Jurgen Moll
Paola Vianello
Mario Varasi
Original Assignee
Pharmacia Italia Spa
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
Application filed by Pharmacia Italia Spa filed Critical Pharmacia Italia Spa
Publication of PE20050325A1 publication Critical patent/PE20050325A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A DERIVADOS DEL COMPUESTO PIRROLO[3,4-c]PIRAZOL DE FORMULA I, EN DONDE R ES H o METILO; R1 ES HIDROXI, ALQUILO o ALCOXI C1-C3 DE CADENA RECTA O RAMIFICADA; R2 ES H o HALOGENO; X ES UN GRUPO DIVALENTE SELECCIONADO DE METILENO (-CH2-), FLUOROMETILENO (-CHF-), UN HETEROATOMO SELECCIONADO DE OXIGENO (-O-), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-{5-[(2R)-2-METOXI-2-FENILETANOIL]-1,4,5,6-TETRAHIDROPIRROLO[3,4-c]PIRAZOL-3-IL}-4-(4-METILPIPERAZIN-1-IL)BENZAMIDA; N-{5-[(2R)-2-METOXI-2-FENILETANOIL]-1,4,5,6-TETRAHIDROPIRROLO[3,4-c]PIRAZOL-3-IL}-4-(4-ETILPIPERAZIN-1-IL)BENZAMIDA; N-{5-[(2R)-2-METOXI-2-FENILETANOIL]-1,4,5,6-TETRAHIDROPIRROLO[3,4-c]PIRAZOL-3-IL}-4-(4-ISOPROPILPIPERAZIN-1-IL)BENZAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO PARA PREPARAR DICHOS COMPUESTOS Y UNA COMPOSICION FARMACEUTICA. ADEMAS SE REFIERE A UN METODO PARA TRATAR TRASTORNOS PROLIFERATIVOS CELULARES OCASIONADOS POR UNA ACTIVIDAD DE PROTEINQUINASA ALTERADA Y/O ASOCIADOS CON LA MISMA
PE2004000657A 2003-07-09 2004-07-08 DERIVADOS DE PIRROLO[3,4-c]PIRAZOL ACTIVOS COMO INHIBIDORES DE QUINASA, PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN PE20050325A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US48581403P 2003-07-09 2003-07-09

Publications (1)

Publication Number Publication Date
PE20050325A1 true PE20050325A1 (es) 2005-05-17

Family

ID=34062099

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000657A PE20050325A1 (es) 2003-07-09 2004-07-08 DERIVADOS DE PIRROLO[3,4-c]PIRAZOL ACTIVOS COMO INHIBIDORES DE QUINASA, PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN

Country Status (42)

Country Link
US (2) US7141568B2 (es)
EP (1) EP1644376B1 (es)
JP (1) JP4728232B2 (es)
KR (1) KR101075711B1 (es)
CN (1) CN100564380C (es)
AP (1) AP2214A (es)
AR (1) AR050045A1 (es)
AT (1) ATE480540T1 (es)
AU (1) AU2004255347B2 (es)
BR (1) BRPI0411868B8 (es)
CA (1) CA2531759C (es)
CR (1) CR8171A (es)
CY (1) CY1110832T1 (es)
DE (1) DE602004029045D1 (es)
DK (1) DK1644376T3 (es)
DO (1) DOP2004000949A (es)
EA (1) EA009462B1 (es)
EC (1) ECSP056246A (es)
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GE (1) GEP20084395B (es)
GT (2) GT200400133A (es)
HK (1) HK1089769A1 (es)
HN (1) HN2004000232A (es)
IL (1) IL172923A (es)
IS (1) IS2843B (es)
MA (1) MA28064A1 (es)
ME (1) MEP51908A (es)
MX (1) MXPA06000362A (es)
MY (1) MY139072A (es)
NO (1) NO332361B1 (es)
NZ (1) NZ544514A (es)
PA (1) PA8606201A1 (es)
PE (1) PE20050325A1 (es)
PL (1) PL1644376T3 (es)
PT (1) PT1644376E (es)
RS (2) RS20060004A (es)
SI (1) SI1644376T1 (es)
TN (1) TNSN06009A1 (es)
TW (1) TWI343382B (es)
UA (1) UA81682C2 (es)
WO (1) WO2005005427A1 (es)
ZA (1) ZA200600095B (es)

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EA011815B1 (ru) 2005-01-10 2009-06-30 Пфайзер Инк. Пирролопиразолы в качестве сильнодействующих ингибиторов киназы
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TW200808311A (en) * 2006-03-30 2008-02-16 Nerviano Medical Sciences Srl Use of a kinase inhibitor for the treatment of particular resistant tumors
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EP2223925A1 (en) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase inhibitors
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DE602007008949D1 (de) * 2006-11-03 2010-10-14 Nerviano Medical Sciences Srl Verfahren zur verabreichung einer antitumoralen verbindung
AR071780A1 (es) * 2008-05-15 2010-07-14 Nerviano Medical Sciences Srl Derivados de carbamoilo de carbonilamino-pirazoles biciclicos como profarmacos
JP5518062B2 (ja) * 2008-07-24 2014-06-11 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ オーロラキナーゼ阻害剤および抗悪性腫瘍剤を含む治療用組み合わせ
CN102105148B (zh) * 2008-07-24 2013-04-10 内尔维阿诺医学科学有限公司 包含aurora激酶抑制剂和抗肿瘤药的治疗组合
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Also Published As

Publication number Publication date
NZ544514A (en) 2009-07-31
US20060276471A1 (en) 2006-12-07
MA28064A1 (fr) 2006-08-01
ES2349780T3 (es) 2011-01-11
HN2004000232A (es) 2011-01-17
KR20060033001A (ko) 2006-04-18
WO2005005427A1 (en) 2005-01-20
AU2004255347B2 (en) 2010-04-08
EA200600209A1 (ru) 2006-06-30
BRPI0411868B8 (pt) 2021-05-25
JP4728232B2 (ja) 2011-07-20
BRPI0411868B1 (pt) 2019-11-12
GEP20084395B (en) 2008-06-10
BRPI0411868A (pt) 2006-08-08
ECSP056246A (es) 2006-04-19
CY1110832T1 (el) 2015-06-10
CA2531759C (en) 2013-04-02
JP2009513525A (ja) 2009-04-02
DE602004029045D1 (de) 2010-10-21
TWI343382B (en) 2011-06-11
HK1089769A1 (en) 2006-12-08
AU2004255347A1 (en) 2005-01-20
RS20060004A (en) 2008-06-05
ZA200600095B (en) 2007-01-31
CN1820009A (zh) 2006-08-16
TNSN06009A1 (fr) 2007-10-03
CN100564380C (zh) 2009-12-02
EA009462B1 (ru) 2007-12-28
PT1644376E (pt) 2010-09-24
MY139072A (en) 2009-08-28
AR050045A1 (es) 2006-09-27
KR101075711B1 (ko) 2011-10-21
IL172923A (en) 2011-09-27
RS52155B (en) 2012-08-31
US7141568B2 (en) 2006-11-28
TW200510385A (en) 2005-03-16
EP1644376B1 (en) 2010-09-08
AP2006003480A0 (en) 2006-02-28
IL172923A0 (en) 2006-06-11
GT200400133A (es) 2005-04-18
GT200400133AA (es) 2007-07-10
US7582628B2 (en) 2009-09-01
DOP2004000949A (es) 2005-01-15
IS8192A (is) 2005-12-22
EP1644376A1 (en) 2006-04-12
NO332361B1 (no) 2012-09-03
MEP51908A (en) 2011-05-10
NO20060113L (no) 2006-04-05
UA81682C2 (en) 2008-01-25
PL1644376T3 (pl) 2011-03-31
SI1644376T1 (sl) 2010-11-30
US20050032839A1 (en) 2005-02-10
CA2531759A1 (en) 2005-01-20
AP2214A (en) 2011-03-04
IS2843B (is) 2013-08-15
MXPA06000362A (es) 2006-03-28
CR8171A (es) 2006-08-09
ATE480540T1 (de) 2010-09-15
PA8606201A1 (es) 2005-08-04
DK1644376T3 (da) 2011-01-03

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