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AR059064A1 - Compuestos de tiazol, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades mediadas por la proteina quinasa b(pkb), tales como cancer. - Google Patents

Compuestos de tiazol, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades mediadas por la proteina quinasa b(pkb), tales como cancer.

Info

Publication number
AR059064A1
AR059064A1 ARP070100212A ARP070100212A AR059064A1 AR 059064 A1 AR059064 A1 AR 059064A1 AR P070100212 A ARP070100212 A AR P070100212A AR P070100212 A ARP070100212 A AR P070100212A AR 059064 A1 AR059064 A1 AR 059064A1
Authority
AR
Argentina
Prior art keywords
alkyl
cr9r10
aryl
heteroaryl
cycloalkyl
Prior art date
Application number
ARP070100212A
Other languages
English (en)
Inventor
Matthew Lee
Celia Dominguez
Fang-Tsao Hong
Qingyian Liu
Christopher H Fotsch
Xin Huang
Matthew Paul Bourbeau
James Thomas Rider
Seifu Tadesse
Andrew Tasker
Vellarkad N Viswa-Nadhan
Kurt Edward Weiler
George Erich Wohlhieter
Guomin Yao
Chester Chenguang Yuan
Qinping Zeng
Nianhe Han
John Gordon Allen
Xianghong Wang
Aiwen Li
Original Assignee
Amgen Inc
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 Amgen Inc filed Critical Amgen Inc
Publication of AR059064A1 publication Critical patent/AR059064A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1) donde: A es como se muestra en la formula (2) o arilo; Y es -N(R5)R6 o -OR6; X es O, S, o -N(R7); R1 es R8, -CHR11-N(H)-R8, -CHR11-O-R8, alquinilo C2-6, hidroxialquinilo C2-6 o -C:::N; R2 es arilo o heteroarilo; R3 es -H, alquilo C1-6, que puede estar interrumpido por uno o más heteroátomos, -(CR9R10)t(arilo), -(CR9R 10)t(heteroarilo), -(CR9R10)t(cicloalquilo) o -(CR9R10)t(heterociclilo); R4 es alquilo C1-6, que puede estar interrumpido por uno o más heteroátomos, -(CR9R10)t(arilo), -(CR9R 10)t(heteroarilo), -(CR9R10)t(cicloalquilo) o -(CR9R10)t(heterociclilo); o R3 y R4, junto con el átomo de carbono al cual ambos están enlazados, se unen para formar un sistema de anillos carbocíclicos o heterocíclicos C3-10, o R4 y R7 se unen para formar un anillo heterocíclico C3-10; R5 es -H, alquilo C1-8, -C(O)(CR9R10)t)N(R7)2, -C(O)(CR9R10)t -C(O)2(CR9R10)t,-(CR9R10)t(arilo), -(CR9R10)t(heteroarilo), -(CR9R10)t(cicloalquilo) o - (CR9R10)t(heterociclilo), o R4 y R5 se unen para formar un anillo heterocíclico C3-10; R6 y R7 se seleccionan, en forma independiente, de -H, alquilo C1-8, -(alquilo C1-6)arilo, o -C(O)(alquilo C1-6), o R6 y R7, junto con los átomos a los cuales están enlazados, se unen para formar un anillo heterocíclico de 5 a 6 miembros, o R5 y R6, junto con el átomo de nitrogeno al cual están enlazados, se unen para formar un anillo heterocíclico o heteroarilo de 5 a 6 miembros; R8 es -H, alquilo C1-6, - (alquilo C1-6)arilo, arilo o heteroarilo; y R9, R10 y R11 se seleccionan, en forma independiente, de -H, alquilo C1-6 o arilo; donde n es un entero de 1 a 6; m es un entero de 0 a 2; y cada t es, en forma independiente, un entero de 0 a 3; donde cada uno de los citados alquilo, arilo, heteroarilo, cicloalquilo y fracciones heterociclilo, y anillos heterocíclicos y carbocíclicos están opcional e independientemente sustituidos por 1 a 3 sustituyentes que se seleccionan de: amino, arilo, heteroarilo, cicloalquilo o heterociclilo opcionalmente sustituido por 1 a 5 sustituyentes que se seleccionan de alcoxi C1-6, alquilo C1-6 opcionalmente sustituido por halo, arilo, halo, hidroxilo, heteroarilo, hidroxialquilo C1-6, o -NHS(O)2- (alquilo C1-6); alquilo C1-6, haloalquilo C2-6, hidroxialquilo C1-6, alcoxi C1-6, alquilo C1-6, amino, alquenilo C2-6 o alquinilo C2-6, donde cada uno de los cuales puede estar interrumpido por uno o más heteroátomos, ciano, halo, hidroxilo, nitro, o -O-arilo; o una sal farmacéuticamente aceptable, hidrato o estereoisomero de éste.
ARP070100212A 2006-01-18 2007-01-18 Compuestos de tiazol, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades mediadas por la proteina quinasa b(pkb), tales como cancer. AR059064A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US75954606P 2006-01-18 2006-01-18

Publications (1)

Publication Number Publication Date
AR059064A1 true AR059064A1 (es) 2008-03-12

Family

ID=38180602

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070100212A AR059064A1 (es) 2006-01-18 2007-01-18 Compuestos de tiazol, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades mediadas por la proteina quinasa b(pkb), tales como cancer.

Country Status (21)

Country Link
US (2) US7514566B2 (es)
EP (1) EP1981884B1 (es)
JP (1) JP5199885B2 (es)
KR (1) KR20080091369A (es)
CN (1) CN101421265A (es)
AR (1) AR059064A1 (es)
AU (1) AU2007207743B2 (es)
BR (1) BRPI0706621A2 (es)
CA (1) CA2636077C (es)
CR (1) CR10211A (es)
EA (1) EA200801716A1 (es)
ES (1) ES2389062T3 (es)
IL (1) IL192751A0 (es)
MY (1) MY149143A (es)
NO (1) NO20083572L (es)
PE (1) PE20071114A1 (es)
TW (1) TW200738657A (es)
UA (1) UA91895C2 (es)
UY (1) UY30098A1 (es)
WO (1) WO2007084391A2 (es)
ZA (1) ZA200806386B (es)

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UA91895C2 (en) 2010-09-10
US20090270445A1 (en) 2009-10-29
EP1981884A2 (en) 2008-10-22
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UY30098A1 (es) 2007-10-31
CR10211A (es) 2008-10-03
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