AR071811A1 - Derivados de diazol como activadores de glucoquinasa - Google Patents

Derivados de diazol como activadores de glucoquinasa

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Publication number
AR071811A1
AR071811A1 ARP090101763A AR071811A1 AR 071811 A1 AR071811 A1 AR 071811A1 AR P090101763 A ARP090101763 A AR P090101763A AR 071811 A1 AR071811 A1 AR 071811A1
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AR
Argentina
Prior art keywords
alkyl
heterobicycloaryl
heterocycloalkyl
bicycloaryl
cycloalkyl
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English (en)
Inventor
Zacharia Cheruvallath
Stephen L Gwaltney
Mark Sabat
Jeffrey A Stafford
Mingnam Tang
Haxia Wang
Andrew J Jennings
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Takeda Pharmaceutical
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41076813&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR071811(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Takeda Pharmaceutical filed Critical Takeda Pharmaceutical
Publication of AR071811A1 publication Critical patent/AR071811A1/es

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    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero rings
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Adem s se proveen composiciones farmaceuticas, kits y art¡culos de fabricacion que comprenden estos compuestos; metodos e intermediarios utiles para producir los compuestos; y metodos para utilizar dichos compuestos. Reivindicacion 1: Un compuesto que tiene la formula: o un polimorfo, solvato, ester, tautomero, enantiomero, sal o prodroga del mismo aceptable para uso farmaceutico, donde R1 se selecciona del grupo integrado por heterocicloalquilo C3-12, heterobicicicloalquilo C3-12, heteroarilo, y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R2 se selecciona del grupo integrado por hidrogeno y un sustituyente que puede convertirse a hidrogeno in vivo; R3 se selecciona del grupo integrado por hidrogeno, carbonilo, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, aminoalquilo C1-10, iminoalquilo C1-3, cicloalquilo C3-12-alquilo C1-5, heterocicloalquilo C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloarilo C9-12-alquilo C1-5, heterobicicloarilo C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicicloalquilo C3-12, arilo, heteroarilo, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido, o R3 es -L-R18; R4 se selecciona del grupo integrado por hidrogeno, carbonilo, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, aminoalquilo C1-10, iminoalquilo C1-3, cicloalquilo C3-12-alquilo C1-5, heterocicloalquilo C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloarilo C9-12-alquilo C1-5, heterobicicloarilo C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicicloalquilo C3-12, arilo, heteroarilo, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido, o R3 y R4 se toman juntos para formar un anillo sustituido o no sustituido; R5 se selecciona del grupo integrado por hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, ariloxi C4-12, heteroariloxi C1-10, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, oxaalquilo C1-10, oxoalquilo C1-10, iminoalquilo C1-10, cicloalquilo C3-12-alquilo C1-5, heterocicloalquilo C3-12-alquilo C1-10, arilalquilo C1-10, heteroarilo C1-10-alquilo C1-5, bicicloarilo C9-12-alquilo C1-5, heterobicicloarilo C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R6 se selecciona del grupo integrado por hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, ariloxi C4-12, heteroariloxi C1-10, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, oxaalquilo C1-10, oxoalquilo C1-10, iminoalquilo C1-10, cicloalquilo C3-12-alquilo C1-5, heterocicloalquilo C3-12-alquilo C1-10, Arilalquilo C1-10, heteroarilo C1-10-alquilo C1-5, bicicloarilo C9-12-alquilo C1-5, heterobicicloarilo C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, bicicloalquilo C9-12, heterobicicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido, o R6 es -L1-R22 R7 se selecciona del grupo integrado por hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, ariloxi C4-12, heteroariloxi C1-10, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, oxaalquilo C1-10, oxoalquilo C1-10, iminoalquilo C1-10, cicloalquilo C3-12-alquilo C1-5, heterocicloalquilo C3-12-alquilo C1-10, arilalquilo C1-10, heteroarilo C1-10-alquilo C1-5, bicicloarilo C9-12-alquilo C1-5, heterobicicloarilo C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido, o R7 es -L1-R22 o cualquiera dos R5, R6 y R7 se toman juntos para formar un anillo sustituido o no sustituido; L es un conector que suministra 0, 1, 2, 3, 4, 5 o 6 separaciones de  tomo entre el C y R18 al cual L est  unido, donde los  tomos del conector que suministran la separacion se seleccionan del grupo integrado por carbono, ox¡geno, nitrogeno, y azufre; L1 est  ausente o un conector que suministra 1, 2, 3, 4, 5 o 6 separaciones de  tomo entre R22 y el anillo al cual L1 est  unido, donde los  tomos del conector que suministran la separacion se seleccionan del grupo integrado por carbono, ox¡geno, nitrogeno, y azufre; R18 se selecciona del grupo integrado por hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, ariloxi C4-12, heteroariloxi C1-10, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, oxaalquilo C1-10, oxoalquilo C1-10, iminoalquilo C1-10, cicloalquilo C3-12-alquilo C1-5, heterocicloalquilo C3-12-alquilo C1-10, arilalquilo C1-10, heteroarilo C1-10-alquilo C1-5, bicicloarilo C9-12-alquilo C1-5, heterobicicloarilo C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R22 se selecciona del grupo integrado por hidrogeno, halo, nitro, ciano, t¡o, oxi, hidroxi, carboniloxi, alcoxi C1-10, ariloxi C4-12, heteroariloxi C1-10, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, oxaalquilo C1-10, oxoalquilo C1-10, iminoalquilo C1-10, cicloalquilo C3-12-alquilo C1-5, heterocicloalquilo C3-12-alquilo C1-10, arilalquilo C1-10, heteroarilo C1-10-alquilo C1-5, bicicloarilo C9-12-alquilo C1-5, heterobicicloarilo C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido, o R22 es -NR27R28 y R27 y R28 se seleccionan cada uno de ellos independientemente del grupo integrado por hidrogeno, hidroxi, alcoxi, ariloxi, heteroariloxi, carbonilo, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, aminoalquilo C1-10, iminoalquilo C1-3, cicloalquilo C3-12-alquilo C1-5, heterocicloalquilo C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloarilo C9-12-alquilo C1-5, heterobicicloarilo C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicicloalquilo C3-12, arilo, heteroarilo, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido, o R27 y R28 se toman juntos para formar un anillo sustituido o no sustituido, con la condicion que (a) R1 no sea 5-(3-acetamidociclobutil)-1H-pirazol-3-ilo cuando R5 y R6, junto con el anillo al cual ellos est n unidos, formen un indazol-1-ilo no sustituido; y (b) R1 no sea 5-(2-clorobencil)tiazol-2-ilo cuando R3 sea fenilo y R2, R4, R5, R6 y R7 sean todos hidrogeno.
ARP090101763 2008-05-16 2009-05-15 Derivados de diazol como activadores de glucoquinasa AR071811A1 (es)

Applications Claiming Priority (2)

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US5405208P 2008-05-16 2008-05-16
US10837008P 2008-10-24 2008-10-24

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AR071811A1 true AR071811A1 (es) 2010-07-14

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US (4) US8563730B2 (es)
EP (1) EP2294053B1 (es)
JP (1) JP5513492B2 (es)
KR (1) KR20110018366A (es)
CN (1) CN102105451B (es)
AR (1) AR071811A1 (es)
AU (1) AU2009246167B2 (es)
BR (1) BRPI0912802A2 (es)
CA (1) CA2724116A1 (es)
CL (1) CL2009001203A1 (es)
CO (1) CO6321274A2 (es)
CR (1) CR11827A (es)
DO (1) DOP2010000351A (es)
EA (1) EA018988B1 (es)
EC (1) ECSP10010688A (es)
GE (1) GEP20135783B (es)
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