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BRPI0411868B8 - derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase - Google Patents

derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase

Info

Publication number
BRPI0411868B8
BRPI0411868B8 BRPI0411868A BRPI0411868A BRPI0411868B8 BR PI0411868 B8 BRPI0411868 B8 BR PI0411868B8 BR PI0411868 A BRPI0411868 A BR PI0411868A BR PI0411868 A BRPI0411868 A BR PI0411868A BR PI0411868 B8 BRPI0411868 B8 BR PI0411868B8
Authority
BR
Brazil
Prior art keywords
pyrrole
pyrazole derivatives
kinase inhibitors
derivatives active
active
Prior art date
Application number
BRPI0411868A
Other languages
English (en)
Inventor
Forte Barbara
Fancelli Daniele
Moll Jurgen
Varasi Mario
Vianello Paola
Original Assignee
Nerviano Medical Science S R L
Pfizer Italia Srl
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 Nerviano Medical Science S R L, Pfizer Italia Srl, Pharmacia Italia Spa filed Critical Nerviano Medical Science S R L
Publication of BRPI0411868A publication Critical patent/BRPI0411868A/pt
Publication of BRPI0411868B1 publication Critical patent/BRPI0411868B1/pt
Publication of BRPI0411868B8 publication Critical patent/BRPI0411868B8/pt

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Virology (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

"derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase. a presente invenção refere-se a derivados de pirrol[3,4-c]pirazol de fórmula i e seus sais farmaceuticamente aceitáveis, como definido no relatório descritivo, processo para sua preparação e composições farmacêuticas compreendendo-os; os compostos da invenção podem ser úteis em terapia no tratamento de doenças associadas com uma atividade de proteína cinase desregulada, como câncer.
BRPI0411868A 2003-07-09 2004-07-08 derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase BRPI0411868B8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US48581403P 2003-07-09 2003-07-09
PCT/EP2004/007515 WO2005005427A1 (en) 2003-07-09 2004-07-08 PYRROLO[3,4-c]PYRAZOLE DERIVATIVES ACTIVE AS KINASE INHIBITORS

Publications (3)

Publication Number Publication Date
BRPI0411868A BRPI0411868A (pt) 2006-08-08
BRPI0411868B1 BRPI0411868B1 (pt) 2019-11-12
BRPI0411868B8 true BRPI0411868B8 (pt) 2021-05-25

Family

ID=34062099

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0411868A BRPI0411868B8 (pt) 2003-07-09 2004-07-08 derivados de pirrol[3,4-c]pirazol ativos como inibidores de cinase

Country Status (41)

Country Link
US (2) US7141568B2 (pt)
EP (1) EP1644376B1 (pt)
JP (1) JP4728232B2 (pt)
KR (1) KR101075711B1 (pt)
CN (1) CN100564380C (pt)
AP (1) AP2214A (pt)
AR (1) AR050045A1 (pt)
AT (1) ATE480540T1 (pt)
AU (1) AU2004255347B2 (pt)
BR (1) BRPI0411868B8 (pt)
CA (1) CA2531759C (pt)
CR (1) CR8171A (pt)
CY (1) CY1110832T1 (pt)
DE (1) DE602004029045D1 (pt)
DK (1) DK1644376T3 (pt)
DO (1) DOP2004000949A (pt)
EA (1) EA009462B1 (pt)
EC (1) ECSP056246A (pt)
ES (1) ES2349780T3 (pt)
GE (1) GEP20084395B (pt)
GT (2) GT200400133A (pt)
HN (1) HN2004000232A (pt)
IL (1) IL172923A (pt)
IS (1) IS2843B (pt)
MA (1) MA28064A1 (pt)
ME (1) MEP51908A (pt)
MX (1) MXPA06000362A (pt)
MY (1) MY139072A (pt)
NO (1) NO332361B1 (pt)
NZ (1) NZ544514A (pt)
PA (1) PA8606201A1 (pt)
PE (1) PE20050325A1 (pt)
PL (1) PL1644376T3 (pt)
PT (1) PT1644376E (pt)
RS (2) RS20060004A (pt)
SI (1) SI1644376T1 (pt)
TN (1) TNSN06009A1 (pt)
TW (1) TWI343382B (pt)
UA (1) UA81682C2 (pt)
WO (1) WO2005005427A1 (pt)
ZA (1) ZA200600095B (pt)

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NZ524475A (en) * 2000-08-10 2004-11-26 Pharmacia Italia S Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
JP2007506787A (ja) * 2003-09-23 2007-03-22 バーテックス　ファーマシューティカルズ　インコーポレイテッド プロテインキナーゼインヒビターとしてのピラゾロピロール誘導体
EP1694686A1 (en) * 2003-12-19 2006-08-30 Takeda San Diego, Inc. Kinase inhibitors
US20050250829A1 (en) * 2004-04-23 2005-11-10 Takeda San Diego, Inc. Kinase inhibitors
EP1778669A2 (en) * 2004-08-18 2007-05-02 Takeda San Diego, Inc. Kinase inhibitors
EP1812439B2 (en) * 2004-10-15 2017-12-06 Takeda Pharmaceutical Company Limited Kinase inhibitors
PL1838718T3 (pl) 2005-01-10 2011-10-31 Pfizer Pirolopirazole, silne inhibitory kinazy
US8119655B2 (en) * 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
TW200808311A (en) * 2006-03-30 2008-02-16 Nerviano Medical Sciences Srl Use of a kinase inhibitor for the treatment of particular resistant tumors
WO2008017465A1 (en) * 2006-08-10 2008-02-14 F. Hoffmann-La Roche Ag Bicyclic lactam derivatives, their manufacture and use as pharmaceutical agents
EP2223925A1 (en) * 2006-10-09 2010-09-01 Takeda Pharmaceutical Company Limited Kinase inhibitors
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
MX2009004607A (es) * 2006-11-03 2009-05-22 Nerviano Medical Sciences Srl Metodo para administrar un compuesto antitumoral.
CL2009001158A1 (es) * 2008-05-15 2009-10-23 Nerviano Medical Sciences Srl Compuestos derivados de los acidos carboxilicos, tales como 5,6-dihiro-4h-pirrolo[3,4-c]pirazol, furo[3,2-c]pirazol, tieno[2,3-c]pirazol, 4,5,6,7-tetrahidropirazol[4,3-c]piridina e indazol; composicion farmaceutica; y su uso en el tratamiento de trastornos proliferativos celulares asociados a la actividad de proteina quinasa alterada, tal como el cancer.
US20100022553A1 (en) * 2008-07-24 2010-01-28 Nerviano Medical Sciences S.R.L. Therapeutic Combination Comprising an Aurora Kinase Inhibitor and Imatinib
WO2010009985A2 (en) 2008-07-24 2010-01-28 Nerviano Medical Sciences S.R.L. Therapeutic combination comprising an aurora kinase inhibitor and antiproliferative agents
WO2010009967A1 (en) * 2008-07-24 2010-01-28 Nerviano Medical Sciences S.R.L. Therapeutic combination comprising an aurora kinase inhibitor and an antineoplastic agent
ES2468391T3 (es) 2008-12-22 2014-06-16 Millennium Pharmaceuticals, Inc. Combinación de inhibidores de cinasas Aurora y anticuerpos anti-CD20
BR112014014276A2 (pt) 2011-12-12 2017-06-13 Dr Reddys Laboratories Ltd composto, composição farmacêutica, método para inibir uma cinase receptora, e, métodos para tratar condições, doenças e/ou distúrbios, e dor
CN104072498B (zh) * 2013-03-26 2016-12-28 沈阳药科大学 （R）‑N‑[5‑(2‑甲氧基‑2‑苯基乙酰基)‑1,4,5,6‑四氢吡咯并[3,4‑c]吡唑‑3‑基]‑4‑(4‑甲基哌嗪‑1‑基)苯甲酰胺的合成方法
US10335494B2 (en) 2013-12-06 2019-07-02 Millennium Pharmaceuticals, Inc. Combination of aurora kinase inhibitors and anti-CD30 antibodies
WO2015200341A1 (en) 2014-06-23 2015-12-30 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
EP3309163A4 (en) * 2015-06-15 2019-01-09 UBE Industries, Ltd. SUBSTITUTED DIHYDROPYRROLO PYRAZOL DERIVATIVE
US20180207173A1 (en) 2015-07-21 2018-07-26 Millennium Pharmaceuticals, Inc. Administration of aurora kinase inhibitor and chemotherapeutic agents
CN107337674B (zh) * 2016-04-29 2019-09-20 江苏吉贝尔药业股份有限公司 用于dpp-iv抑制剂的四氢吡喃胺衍生物、其药物组合物和制剂以及用途
WO2019195658A1 (en) 2018-04-05 2019-10-10 Dana-Farber Cancer Institute, Inc. Sting levels as a biomarker for cancer immunotherapy
US20220305048A1 (en) 2019-08-26 2022-09-29 Dana-Farber Cancer Institute, Inc. Use of heparin to promote type 1 interferon signaling
CN113563346A (zh) * 2021-08-19 2021-10-29 守恒(厦门)医疗科技有限公司 吡咯[3,4-c]并吡唑二酰胺类衍生物及其在抗肿瘤药物中的应用
JP2025511697A (ja) 2022-04-07 2025-04-16 イーライ リリー アンド カンパニー Ｋｒａｓ ｇ１２ｃ阻害剤を作製するための方法
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CZ2002422A3 (cs) 1999-08-12 2002-11-13 Pharmacia Italia S. P. A. 3(5)-Aminopyrazolové deriváty, způsob jejich přípravy a jejich pouľití jako protinádorová činidla
NZ524475A (en) 2000-08-10 2004-11-26 Pharmacia Italia S Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
FR2815032B1 (fr) 2000-10-10 2003-08-08 Pf Medicament Nouveaux derives d'aminophenyle piperazine ou d'amino phenyle piperide inhibiteurs de proteines prenyl transferase ainsi que leurs preparations
MXPA03004644A (es) 2000-11-27 2003-09-05 Pharmacia Italia Spa Derivados de fenilacetamdia-pirazol y su uso como agentes antitumorales.
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Also Published As

Publication number Publication date
MA28064A1 (fr) 2006-08-01
CA2531759C (en) 2013-04-02
DE602004029045D1 (de) 2010-10-21
TWI343382B (en) 2011-06-11
US20050032839A1 (en) 2005-02-10
JP4728232B2 (ja) 2011-07-20
EA200600209A1 (ru) 2006-06-30
CR8171A (es) 2006-08-09
MY139072A (en) 2009-08-28
TNSN06009A1 (fr) 2007-10-03
AP2006003480A0 (en) 2006-02-28
AU2004255347B2 (en) 2010-04-08
IS2843B (is) 2013-08-15
GT200400133A (es) 2005-04-18
US7582628B2 (en) 2009-09-01
SI1644376T1 (sl) 2010-11-30
ES2349780T3 (es) 2011-01-11
AP2214A (en) 2011-03-04
TW200510385A (en) 2005-03-16
US20060276471A1 (en) 2006-12-07
AR050045A1 (es) 2006-09-27
PT1644376E (pt) 2010-09-24
PA8606201A1 (es) 2005-08-04
AU2004255347A1 (en) 2005-01-20
US7141568B2 (en) 2006-11-28
JP2009513525A (ja) 2009-04-02
CA2531759A1 (en) 2005-01-20
CY1110832T1 (el) 2015-06-10
GEP20084395B (en) 2008-06-10
EA009462B1 (ru) 2007-12-28
NO20060113L (no) 2006-04-05
RS52155B (en) 2012-08-31
KR101075711B1 (ko) 2011-10-21
IS8192A (is) 2005-12-22
DK1644376T3 (da) 2011-01-03
IL172923A (en) 2011-09-27
CN100564380C (zh) 2009-12-02
ECSP056246A (es) 2006-04-19
EP1644376B1 (en) 2010-09-08
DOP2004000949A (es) 2005-01-15
RS20060004A (en) 2008-06-05
GT200400133AA (es) 2007-07-10
BRPI0411868B1 (pt) 2019-11-12
BRPI0411868A (pt) 2006-08-08
ZA200600095B (en) 2007-01-31
NO332361B1 (no) 2012-09-03
PL1644376T3 (pl) 2011-03-31
EP1644376A1 (en) 2006-04-12
MEP51908A (en) 2011-05-10
ATE480540T1 (de) 2010-09-15
CN1820009A (zh) 2006-08-16
HK1089769A1 (en) 2006-12-08
UA81682C2 (en) 2008-01-25
PE20050325A1 (es) 2005-05-17
KR20060033001A (ko) 2006-04-18
WO2005005427A1 (en) 2005-01-20
IL172923A0 (en) 2006-06-11
HN2004000232A (es) 2011-01-17
NZ544514A (en) 2009-07-31
MXPA06000362A (es) 2006-03-28

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Owner name: PHARMACIA ITALIA S.P.A. (IT)

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