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AR062012A1 - Pirazoles como activadores de glucoquinasa - Google Patents

Pirazoles como activadores de glucoquinasa

Info

Publication number
AR062012A1
AR062012A1 ARP070103249A ARP070103249A AR062012A1 AR 062012 A1 AR062012 A1 AR 062012A1 AR P070103249 A ARP070103249 A AR P070103249A AR P070103249 A ARP070103249 A AR P070103249A AR 062012 A1 AR062012 A1 AR 062012A1
Authority
AR
Argentina
Prior art keywords
group
lower alkyl
hydrogen
alkyl
hydroxy
Prior art date
Application number
ARP070103249A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR062012A1 publication Critical patent/AR062012A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38Nitrogen atoms
    • C07D231/40Acylated on said nitrogen atom
    • 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
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Útiles para el tratamiento de enfermedades y trastornos metabólicos, con preferencia la diabetes mellitus. Reivindicación 1: Un compuesto de la fórmula (1) en la que R¹ y R² se eligen con independencia entre el grupo formado por hidrógeno, halógeno, amino, hidroxiamino, ciano, nitro, alquilo inferior, -OR⁵, -C(O)OR⁶, perfluoro-alquilo inferior, alquiltio inferior, perfluoro-alquiltio inferior, alquilsulfinilo inferior, alquilsulfonilo inferior, cicloalquil-alquilsulfonilo inferior, (alcoxi inferior)-alquilsulfonilo inferior, perfluoro-alquilsulfonilo inferior y sulfonamido; o R¹ y R², junto con el anillo fenilo, al que están unidos, se combinan para formar un grupo elegido entre el grupo formado por 2,3-dihidro-benzo[b]tiofeno, 1-óxido de 2,3-dihidro-benzo[b]tiofeno, 1,1-dióxido de 2,3-dihidro-benzo[b]tiofeno, benzo[b]tiofeno, 1-óxido de benzo[b]tiofeno, 1,1-dióxido de benzo[b]tiofeno, tiocromano, 1-óxido de tiocromano y 1,1-dióxido de tiocromano; R³ es un cicloalquilo, un bicicloalquilo o un heterociclo mono- o bicíclico de 1-3 heteroátomos, elegido entre N, O y S, dicho cicloalquilo o heterociclo está sin sustituir o mono-, bi- o trisustituido con grupos elegidos entre el grupo formado por halógeno, alquilo inferior, alcoxi inferior, carbonilo y alquilsulfonilo inferior; R⁴ se elige entre el grupo formado por hidrógeno, los compuestos del grupo de fórmulas (2), alquilo C₁₋₁₀ y alquenilo C₂₋₁₀; R⁵ se elige entre el grupo formado por hidrógeno, alquilo C₁₋₆, fenilo, bencilo, fenilo sustituido y bencilo sustituido; R⁶ se elige entre el grupo formado por hidrógeno, alquilo C₁₋₆, bencilo y bencilo sustituido; R⁷ se elige entre el grupo formado por hidrógeno, hidroxi, alcoxi, perfluoro-alcoxi, amino, alquilamino, dialquilamino, hidroximetilo, C(O)OY', en el que Y' es H o alquilo inferior y -O-C(O)-CH₃; R⁸ es hidrógeno o alquilo inferior; R⁹ se elige entre el grupo formado por hidrógeno, cicloalquilo y alquilo inferior; R¹⁰ se elige entre el grupo formado por hidroxi, alcoxi inferior, amino, metilamino, dimetilamino o -NH-CH₂-cicloalquilo; R¹¹ se elige entre el grupo formado por hidroxi, amino, alquilamino inferior, ciclopropil-metil-amino, metoxi y NHCH₂CH₂CH₂L, en el que L es metoxi, hidroxi o dimetilamino; R¹² es hidrógeno o alquilo inferior; R¹³ es hidrógeno o alquilo inferior; R¹⁴ se elige entre el grupo formado por hidrógeno, alquilo inferior, SO₂X, en el que X es alquilo inferior, y C(O)Y, en el que Y es alquilo inferior u O-alquilo; R¹⁵ se elige entre el grupo formado por hidroxi, metoxi, t-butoxi, alquilo inferior, 2-hidroxi-2-metil-propilo, amino, metilamino, propilamino, dimetilamino, dietilamino, morfolino, fenilamino, bencilamino, alilcarbamoil-alquilo inferior, alilamino, pirazin-2-ilamino y NH-(CH₂)ᵛZ, en el que Z es metoxi o morfolino; R¹⁶ es alquilo inferior; R¹⁷ es metoxi; R¹⁸ se elige entre el grupo formado por hidrógeno, alquilo inferior y C(O)R', en el que R' es alquilo inferior; X e Y se eligen con independencia entre el grupo formado por hidrógeno, halógeno, ciano, alquilo inferior, metoxi, SO₂X, en el que X es alquilo y cicloalquilo; m es el número 0, 1, 2, 3 ó 4; en el que, si m es 0, R⁷ no puede ser hidroxi, alcoxi, perfluoro-alcoxi, amino, alquilamino ni dialquilamino; n es el número 0, 1 ó 2; p es el número 0 ó 1; q es el número 0, 1 ó 2; y v es el número 2 ó 3; o una sal farmacéuticamente aceptable del mismo.
ARP070103249A 2006-07-24 2007-07-20 Pirazoles como activadores de glucoquinasa AR062012A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83290706P 2006-07-24 2006-07-24
US93081907P 2007-05-18 2007-05-18

Publications (1)

Publication Number Publication Date
AR062012A1 true AR062012A1 (es) 2008-08-10

Family

ID=38657003

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070103249A AR062012A1 (es) 2006-07-24 2007-07-20 Pirazoles como activadores de glucoquinasa

Country Status (16)

Country Link
US (1) US7935699B2 (es)
EP (2) EP2046755A2 (es)
JP (1) JP2009544648A (es)
KR (1) KR20090025358A (es)
AR (1) AR062012A1 (es)
AU (1) AU2007278261A1 (es)
BR (1) BRPI0715531A2 (es)
CA (1) CA2657566A1 (es)
CL (1) CL2007002121A1 (es)
IL (1) IL196321A0 (es)
MX (1) MX2009000688A (es)
NO (1) NO20090064L (es)
PE (1) PE20080406A1 (es)
RU (1) RU2009105818A (es)
TW (1) TWI332948B (es)
WO (1) WO2008012227A2 (es)

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Also Published As

Publication number Publication date
TW200812974A (en) 2008-03-16
JP2009544648A (ja) 2009-12-17
AU2007278261A1 (en) 2008-01-31
RU2009105818A (ru) 2010-08-27
EP2046755A2 (en) 2009-04-15
EP2261216A3 (en) 2011-12-14
NO20090064L (no) 2009-02-04
KR20090025358A (ko) 2009-03-10
TWI332948B (en) 2010-11-11
CA2657566A1 (en) 2008-01-31
EP2261216A2 (en) 2010-12-15
US7935699B2 (en) 2011-05-03
WO2008012227A3 (en) 2008-05-15
WO2008012227A2 (en) 2008-01-31
BRPI0715531A2 (pt) 2014-06-24
IL196321A0 (en) 2009-09-22
US20080021032A1 (en) 2008-01-24
MX2009000688A (es) 2009-01-30
WO2008012227A8 (en) 2008-09-12
CL2007002121A1 (es) 2008-02-22
PE20080406A1 (es) 2008-04-28

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