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

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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

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
US7541378B2 (en) * 2002-07-25 2009-06-02 Pfizer Italia S.R.L. Condensed heterocyclic pyrazole derivatives as kinase inhibitors
EP1904503B1 (en) 2005-07-19 2013-11-06 Nerviano Medical Sciences S.R.L. 1h-thieno[2,3-c]-pyrazole compounds useful as kinase inhibitors
EP1942885A1 (en) * 2005-10-06 2008-07-16 Merck Sharp & Dohme Ltd. 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
US7803829B2 (en) 2006-03-30 2010-09-28 Nerviano Medical Sciences S.R.L. Use of a kinase inhibitor for the treatment of particular resistant tumors
ATE478875T1 (de) 2006-05-31 2010-09-15 Nerviano Medical Sciences Srl 1h-furoä3,2-cü pyrazolverbindungen, die sich als kinaseinhibitoren eignen
FR2904626B1 (fr) 2006-08-03 2008-09-19 Sanofi Aventis Derives de pyrazolo[4,3]thiazole, leur preparation et leur application en therapeutique
GEP20135728B (en) 2006-10-09 2013-01-25 Takeda Pharmaceuticals Co Kinase inhibitors
KR100923540B1 (ko) 2007-11-23 2009-10-27 한국과학기술연구원 5-아실하이드라진카르보닐-3,4-디치환 피라졸 유도체 및이의 제조방법
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.
AU2010229144B2 (en) * 2009-03-23 2012-07-12 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
EP2836494B1 (en) * 2012-04-05 2019-08-21 Nerviano Medical Sciences S.r.l. New alkylating agents
EP3663299B1 (en) * 2017-08-01 2023-03-08 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Bicyclic compound acting as ror gamma inhibitor
AU2018375456B2 (en) * 2017-11-30 2021-11-18 Hanmi Pharm. Co., Ltd. Thieno(3,2-d)pyrimidine compound having inhibitory activity for protein kinase
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
EP0234622B1 (en) 1986-02-19 1990-06-27 Duphar International Research B.V New thio compounds having fungicidal activity
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
SK1812002A3 (en) 1999-08-12 2003-02-04 Pharmacia Italia Spa 3(5)-Amino-pyrazole derivatives, process for their preparation and their use as antitumor agents
DE60143041D1 (de) * 2000-08-10 2010-10-21 Pfizer Italia Srl Bizyklische pyrazole wirksam als kinase inhibitoren, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zubereitungen
MXPA03004644A (es) 2000-11-27 2003-09-05 Pharmacia Italia Spa Derivados de fenilacetamdia-pirazol y su uso como agentes antitumorales.
MXPA03006478A (es) 2001-01-26 2003-09-22 Pharmacia Italia Spa Derivados de cromano, procedimiento para su preparacion y su uso como agentes antitumorales.
ES2380054T3 (es) 2001-09-26 2012-05-08 Pfizer Italia S.R.L. Derivados de aminoindazol activos como inhibidores de quinasas, procedimientos para su preparación, y composiciones farmacéuticas que los contienen
BR0311291A (pt) * 2002-05-17 2005-03-29 Pharmacia Italia Spa Derivados de aminoindazol ativos como inibidores da cinase, processo para sua preparação e composições farmacêuticas compreendendo os mesmos
DE60320560T2 (de) * 2002-07-17 2008-12-11 Pfizer Italia S.R.L. Heterobicyclische pyrazolderivate als kinaseinhibitoren
US7541378B2 (en) * 2002-07-25 2009-06-02 Pfizer Italia S.R.L. Condensed heterocyclic pyrazole derivatives as kinase inhibitors
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
US20050187209A1 (en) 2005-08-25
CN1946395A (zh) 2007-04-11
BRPI0507375A (pt) 2007-07-10
EA011032B1 (ru) 2008-12-30
DE602005007181D1 (de) 2008-07-10
SI1711177T1 (sl) 2008-10-31
ES2307144T3 (es) 2008-11-16
MXPA06008787A (es) 2007-01-19
CY1108246T1 (el) 2014-02-12
IL177141A0 (en) 2006-12-10
TNSN06244A1 (fr) 2007-12-03
KR20060124734A (ko) 2006-12-05
US20120165311A1 (en) 2012-06-28
JP4908233B2 (ja) 2012-04-04
UY28738A1 (es) 2005-09-30
CN1946395B (zh) 2014-04-02
CA2555262C (en) 2014-10-14
TW200526204A (en) 2005-08-16
AP2006003701A0 (en) 2006-08-31
EA200601418A1 (ru) 2006-12-29
DK1711177T3 (da) 2008-09-29
NO20063768L (no) 2006-11-02
DOP2005000014A (es) 2006-08-15
PE20051095A1 (es) 2005-12-31
MA28429B1 (fr) 2007-02-01
UA86223C2 (uk) 2009-04-10
HK1101343A1 (en) 2007-10-18
GEP20094633B (en) 2009-03-10
US8481584B2 (en) 2013-07-09
WO2005074922A1 (en) 2005-08-18
JP2007520513A (ja) 2007-07-26
ATE396724T1 (de) 2008-06-15
ZA200606179B (en) 2008-02-27
PA8622801A1 (es) 2005-11-25
AU2005210114B2 (en) 2011-07-14
NZ548896A (en) 2010-05-28
AU2005210114A1 (en) 2005-08-18
EP1711177A1 (en) 2006-10-18
ECSP066767A (es) 2006-11-24
CA2555262A1 (en) 2005-08-18
PL1711177T3 (pl) 2008-11-28
EP1711177B1 (en) 2008-05-28
CR8546A (es) 2007-05-30
PT1711177E (pt) 2008-09-04
GT200500020A (es) 2005-09-06
US8138217B2 (en) 2012-03-20

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