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AR047531A1 - Derivados 1h-tieno(2,3-c)pirazol utiles como inhibidores de quinasa - Google Patents

Derivados 1h-tieno(2,3-c)pirazol utiles como inhibidores de quinasa

Info

Publication number
AR047531A1
AR047531A1 ARP050100399A ARP050100399A AR047531A1 AR 047531 A1 AR047531 A1 AR 047531A1 AR P050100399 A ARP050100399 A AR P050100399A AR P050100399 A ARP050100399 A AR P050100399A AR 047531 A1 AR047531 A1 AR 047531A1
Authority
AR
Argentina
Prior art keywords
group
branched
linear
hydrogen atom
atom
Prior art date
Application number
ARP050100399A
Other languages
English (en)
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 AR047531A1 publication Critical patent/AR047531A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Proceso para su preparacion y composiciones farmacéuticas que los comprenden; los compuestos pueden ser utiles en terapia, en el tratamiento de enfermedades asociadas con una mala regulacion de la actividad proteína quinasa, como cáncer. Reivindicacion 1: Un compuesto de formula (1), caracterizado porque: R es un grupo arilo o heteroarilo opcionalmente sustituido; R1 y R2 son el mismo o son diferente, y representan independientemente entre sí, un átomo de hidrogeno, un alquilo C1-3 lineal o ramificado o un grupo -CONH2 o -CH2NR'R'' o, tomados juntos con el átomo de carbono al que están unidos, R1 y R2 pueden formar un grupo cicloalquilo C3-6; siempre y cuando por lo menos uno de R1 y R2 sea diferente de un átomo de hidrogeno; R' y R'' son el mismo o diferentes, y representan independientemente entre sí, un átomo de hidrogeno o un grupo alquilo C1-3 lineal o ramificado o, tomados junto con el átomo de nitrogeno al que están unidos, R' y R'' pueden formar un anillo heterocíclico del resto de grupo de formula (2), donde R''' es un átomo de hidrogeno o un grupo alquilo C1-3 lineal o ramificado; R3 es un átomo de hidrogeno o halogeno o un grupo que se selecciona entre hidroxi, ciano, alquilo C1-3 lineal o ramificado o alcoxi C1-3; o isomeros, tautomeros, vehículos, metabolitos, prodrogas, y sales de los mismos aceptables para uso farmacéutico.
ARP050100399A 2004-02-03 2005-02-02 Derivados 1h-tieno(2,3-c)pirazol utiles como inhibidores de quinasa AR047531A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US54145204P 2004-02-03 2004-02-03

Publications (1)

Publication Number Publication Date
AR047531A1 true AR047531A1 (es) 2006-01-25

Family

ID=34837492

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050100399A AR047531A1 (es) 2004-02-03 2005-02-02 Derivados 1h-tieno(2,3-c)pirazol utiles como inhibidores de quinasa

Country Status (38)

Country Link
US (2) US8138217B2 (es)
EP (1) EP1711177B1 (es)
JP (1) JP4908233B2 (es)
KR (1) KR20060124734A (es)
CN (1) CN1946395B (es)
AP (1) AP2006003701A0 (es)
AR (1) AR047531A1 (es)
AT (1) ATE396724T1 (es)
AU (1) AU2005210114B2 (es)
BR (1) BRPI0507375A (es)
CA (1) CA2555262C (es)
CR (1) CR8546A (es)
CY (1) CY1108246T1 (es)
DE (1) DE602005007181D1 (es)
DK (1) DK1711177T3 (es)
DO (1) DOP2005000014A (es)
EA (1) EA011032B1 (es)
EC (1) ECSP066767A (es)
ES (1) ES2307144T3 (es)
GE (1) GEP20094633B (es)
GT (1) GT200500020A (es)
HK (1) HK1101343A1 (es)
IL (1) IL177141A0 (es)
MA (1) MA28429B1 (es)
MX (1) MXPA06008787A (es)
NO (1) NO20063768L (es)
NZ (1) NZ548896A (es)
PA (1) PA8622801A1 (es)
PE (1) PE20051095A1 (es)
PL (1) PL1711177T3 (es)
PT (1) PT1711177E (es)
SI (1) SI1711177T1 (es)
TN (1) TNSN06244A1 (es)
TW (1) TW200526204A (es)
UA (1) UA86223C2 (es)
UY (1) UY28738A1 (es)
WO (1) WO2005074922A1 (es)
ZA (1) ZA200606179B (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0312961A (pt) * 2002-07-25 2005-06-14 Pharmacia Italia Spa Derivados condensados heterociclicos de pirazol como inibidores de cinase
ES2439918T3 (es) 2005-07-19 2014-01-27 Nerviano Medical Sciences S.R.L. Compuestos de 1H-tieno[2,3-c]-pirazol útiles como inhibidores de cinasas
CA2624795A1 (en) * 2005-10-06 2007-04-12 Merck Sharp & Dohme Limited Use of fused pyrrole carboxylic acids for the treatment of neurodegenerative and psychiatric diseases as d-amino acid oxidase inhibitors
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
JP2009534307A (ja) * 2006-03-30 2009-09-24 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 特定の耐性腫瘍の治療のためのキナーゼ阻害剤の使用
US8119641B2 (en) 2006-05-31 2012-02-21 Nerviano Medical Sciences S.R.L. 1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors
FR2904626B1 (fr) * 2006-08-03 2008-09-19 Sanofi Aventis Derives de pyrazolo[4,3]thiazole, leur preparation et leur application en therapeutique
SG158147A1 (en) 2006-10-09 2010-01-29 Takeda Pharmaceutical Kinase inhibitors
KR100923540B1 (ko) 2007-11-23 2009-10-27 한국과학기술연구원 5-아실하이드라진카르보닐-3,4-디치환 피라졸 유도체 및이의 제조방법
AR071780A1 (es) * 2008-05-15 2010-07-14 Nerviano Medical Sciences Srl Derivados de carbamoilo de carbonilamino-pirazoles biciclicos como profarmacos
CA2755768A1 (en) 2009-03-23 2010-09-30 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
US9255072B2 (en) 2011-03-04 2016-02-09 National Health Rsearch Institutes Pyrazole compounds and thiazole compounds as protein kinases inhibitors
US9527863B2 (en) * 2012-04-05 2016-12-27 Nerviano Medical Sciences S.R.L. Thieno-indole moieties and methods of treating using the same
WO2019024809A1 (zh) * 2017-08-01 2019-02-07 正大天晴药业集团股份有限公司 作为RORγ抑制剂的双环化合物
TWI803541B (zh) * 2017-11-30 2023-06-01 韓商韓美藥品股份有限公司 對於蛋白激酶具抑制活性之噻吩并[3,2-d]嘧啶化合物
CN113072562B (zh) * 2021-04-06 2022-01-14 山东大学 一种GSK-3β抑制剂及其制备方法与应用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2015566B3 (es) 1986-02-19 1990-09-01 Duphar Int Res B V Nuevos compuestos tio que tienen actividad fungicida.
GB9911053D0 (en) 1999-05-12 1999-07-14 Pharmacia & Upjohn Spa 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents
US6387900B1 (en) 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
EE200200065A (et) 1999-08-12 2003-04-15 Pharmacia Italia S.P.A. 3-aminopürasooli derivaadid, nende valmistamine ja kasutamine vähivastaste toimeainetena ning neid sisaldav farmatseutiline kompositsioon
US7541354B2 (en) * 2000-08-10 2009-06-02 Pfizer Italia S.R.L. Bicyclo-pyrazoles
AU2002215053A1 (en) 2000-11-27 2002-06-24 Pharmacia Italia S.P.A. Phenylacetamido- pyrazole derivatives and their use as antitumor agents
EP1379524A2 (en) 2001-01-26 2004-01-14 Pharmacia Italia S.p.A. Chromane derivatives, process for their preparation and their use as antitumor agents
CA2460145C (en) 2001-09-26 2011-04-26 Pharmacia Italia S.P.A. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
ES2411655T3 (es) * 2002-05-17 2013-07-08 Pfizer Italia S.R.L. Derivados de aminoindazol activos como inhibidores de quinasas, procedimiento para su preparación y composiciones farmacéuticas que los comprenden
ATE393159T1 (de) * 2002-07-17 2008-05-15 Pfizer Italia Srl Heterobicyclische pyrazolderivate als kinaseinhibitoren
BR0312961A (pt) * 2002-07-25 2005-06-14 Pharmacia Italia Spa Derivados condensados heterociclicos de pirazol como inibidores de cinase
US20050026984A1 (en) * 2003-07-29 2005-02-03 Aventis Pharma S.A. Substituted thieno [2,3-c] pyrazoles and their use as medicinal products

Also Published As

Publication number Publication date
DK1711177T3 (da) 2008-09-29
CA2555262C (en) 2014-10-14
EP1711177B1 (en) 2008-05-28
NO20063768L (no) 2006-11-02
IL177141A0 (en) 2006-12-10
UY28738A1 (es) 2005-09-30
UA86223C2 (uk) 2009-04-10
SI1711177T1 (sl) 2008-10-31
CN1946395A (zh) 2007-04-11
PA8622801A1 (es) 2005-11-25
JP2007520513A (ja) 2007-07-26
ZA200606179B (en) 2008-02-27
US20120165311A1 (en) 2012-06-28
ATE396724T1 (de) 2008-06-15
CR8546A (es) 2007-05-30
KR20060124734A (ko) 2006-12-05
BRPI0507375A (pt) 2007-07-10
US8138217B2 (en) 2012-03-20
MXPA06008787A (es) 2007-01-19
AU2005210114A1 (en) 2005-08-18
ECSP066767A (es) 2006-11-24
MA28429B1 (fr) 2007-02-01
US8481584B2 (en) 2013-07-09
CY1108246T1 (el) 2014-02-12
WO2005074922A1 (en) 2005-08-18
GEP20094633B (en) 2009-03-10
GT200500020A (es) 2005-09-06
AP2006003701A0 (en) 2006-08-31
AU2005210114B2 (en) 2011-07-14
HK1101343A1 (en) 2007-10-18
CN1946395B (zh) 2014-04-02
TW200526204A (en) 2005-08-16
EA200601418A1 (ru) 2006-12-29
EA011032B1 (ru) 2008-12-30
PE20051095A1 (es) 2005-12-31
TNSN06244A1 (fr) 2007-12-03
CA2555262A1 (en) 2005-08-18
DOP2005000014A (es) 2006-08-15
EP1711177A1 (en) 2006-10-18
PT1711177E (pt) 2008-09-04
US20050187209A1 (en) 2005-08-25
NZ548896A (en) 2010-05-28
DE602005007181D1 (de) 2008-07-10
ES2307144T3 (es) 2008-11-16
PL1711177T3 (pl) 2008-11-28
JP4908233B2 (ja) 2012-04-04

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