AR048306A1 - Derivados de acidos carboxilicos aromaticos con capacidad moduladora de los niveles de insulina, composiciones farmaceuticas que los contienen y su uso en el tratamiento de trastornos metabolicos que responden a la regulacion de gpr40 - Google Patents

Derivados de acidos carboxilicos aromaticos con capacidad moduladora de los niveles de insulina, composiciones farmaceuticas que los contienen y su uso en el tratamiento de trastornos metabolicos que responden a la regulacion de gpr40

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Publication number
AR048306A1
AR048306A1 ARP050100748A ARP050100748A AR048306A1 AR 048306 A1 AR048306 A1 AR 048306A1 AR P050100748 A ARP050100748 A AR P050100748A AR P050100748 A ARP050100748 A AR P050100748A AR 048306 A1 AR048306 A1 AR 048306A1
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AR
Argentina
Prior art keywords
acid
phenyl
alkylene
alkyl
hydrogen
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ARP050100748A
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English (en)
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Amgen Inc
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/24—Radicals substituted by oxygen atoms
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
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    • 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
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • A61P9/10—Drugs 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/64—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings
    • C07C59/66—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings the non-carboxylic part of the ether containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Reproductive Health (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Nutrition Science (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Composiciones farmacéuticas que los contienen y uso de éstos compuestos, por ejemplo, para el tratamiento de la diabetes de tipo II. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula: Q-L1-P-L2-M-X-L3-A, o una de sus sales, solvatos o profármacos farmacéuticamente aceptables, en donde: Q es hidrogeno, arilo, heteroarilo, alquilo C1-6 o heteroalquilo C2-6; L1 es un enlace, alquileno C1-4, heteroalquileno C2-4, O, S(O)m, N(R1), C(O)-heterocicloalquilenoC5-7, alquilenC1-4- SO2N(R2), alquilenC1-4-N(R2)SO2 o C(O)N(R2); P es un anillo aromático, un anillo heteroaromático, heterocicloalquileno C3-8 cicloalquileno C3-8; L2 es un enlace, alquileno C1-6, heteroalquileno C2-6, oximetileno, O, S(O)m, N(R1), C(O)N(R2), SO2N(R2), alquilenC1-4-C(O)N(R2), alquilenC1-4-N(R2)C(O), alquilenC2-4-C(O)N(R2), alquilenC2-4-N(R2)C(O), alquilenC1-4-SO2N(R2), alquilenC1-4-N(R2)SO2, alquilenC2-4-SO2N(R2) o alquilenC2-4-N(R2)SO2; M es un anillo aromático, un anillo heteroaromático, cicloalquileno C5-8, arilalquileno C1-4 o heteroarilalquileno C1-4; X es CR3R4, N(R5), O o S(O)n; L3 es enlace, alquileno C1-3 o heteroalquileno C2-5, con la condicion de que L3 no sea un enlace cuando L2 es un enlace; A es -CO2H, tetrazol-5-ilo, -SO3H, -PO3H2, -SO2NH2, -C(O)NHSO2CH3, -CHO, -C(O)R6, -C(O)NHR6, -C(O)NHOR7, tiazolidindion-ilo, hidroxifenilo o piridilo; R1 es alquilo C1-6, arilalquilo C1-3 o heteroalquilo C2-6; R2 es hidrogeno, alquilo C1-6 o heteroalquilo C1-6; R3 es ciano, arilo, heteroarilo, alquilo C1-8, alquilo C2-8, alquenilo C2-8, alquenilo C3-8, alquinilo C2-8, alquinilo C3-8, -NR8R9, -C(O)NR10R11, -NR12C(O)R13 o -NR12S(O)pR13; R4 es hidrogeno, ciano, arilo, hetearilo, alquilo C1-8, alquenilo C2-8 o alquinilo C2-8; opcionalmente, R3 y R4 se combinan para formar un anillo de 3, 4, 5, 6 o 7 miembros que contiene de cero a tres heteroátomos seleccionados de N, O y S; R5 es hidrogeno, arilo, heteroarilo, alquilo C1-8, alquenilo C2-8, alquinilo C2-8 o cicloalquilo C3-8; R6 es heteroarilo; R7 es hidrogeno o alquilo C1-5; R8 y R9 son independientemente hidrogeno, alquilo C1-5, oxialquilo C1-5; o carboxialquilo C1-5; opcionalmente, R8 y R9 se combinan para formar un anillo de 4, 5, 6 o 7 miembros que contiene el átomo de nitrogeno al que están unidos y de 0 a 2 heteroátomos adicionales seleccionados de N, O y S; R10, R11, y R12 se seleccionan independientemente de hidrogeno, arilo, heteroarilo, alquilo C1-8, heteroalquilo C2-8, cicloalquilo C3-8 y heterocicloalquilo C3-8; opcionalmente, R10 y R11 se combinan para formar un anillo de 4, 5, 6 o 7 miembros que contiene el átomo de nitrogeno al cual están unidos y de 0 a 2 heteroátomos adicionales seleccionados de N, O y S; R13 es arilo, heteroarilo, alquilo C1-8, heteroalquilo C2-8, cicloalquilo C3-8 o heterocicloalquilo C3-8; los subíndices m y n son independientemente 0, 1 o 2; y el subíndice p es 1 o 2; y en donde el compuesto es distinto de ácido 3-(4-(4- metoxibenciloxi)fenil)pent-4-inoico; ácido beta-etenil-4-fenilmetoxi-bencenpropanoico; ácido 4-(2-quinolinilmetoxi)-beta-[4-(2-quinolinilmetoxi)fenil]-bencenpropanoico; N-[4-(benzoilamino)fenil]-N-fenil-glicina; 3-(4-(isopentiloxi)benzamido)-3- fenilpropanoato; 3-(4-isobutoxibenzamido)-3-fenilpropanoato; ácido (R)-2-((1R,4R)-4-isopropilciclohexancarboxamido)-3-fenilpropanoico; ácido (R)-3-(4-(benciloxi)fenil)-2-(ter-butoxicarbonil)propanoico; ácido 3-(4-clorofenil)-3-(furan-2- carboxamido)propanoico; ácido 3-(3,4-dimetoxifenil)-3-(furan-2-carboxamido)propanoico; ácido 3-(4-clorobenzamido)-3-(4-(dimetilamino)-fenil)propanoico; ácido 3-(2-(2-(3,4-dimetilfenoxi)etiltio)-1H-benzo[d]imidazol-1-il)propanoico; ácido {2-bromo-4- [(3,4-dicloro-fenil)hidrazonometil]-6-etoxi-fenoxi}-acético; ácido 2-(4-(2-(2-(4-clorofenil)furan-5-carboxamido)etil)fenoxi)-2-metilpropanoico; ácido 5-(3-(3,4-dimetoxifenil)-5-(2-fluorofenil)-4,5-dihidropirazol-1-il)-5-oxopentanoico; ácido 2-(2-(3- (3,4-dihidro-2H-benzo[d][1,4]dioxepin-7-il)-2-metil-4-oxo-4H-cromen-7-iloxi)acetamido)acético; ácido-3-(4'-bromo-bifenil-4-il)-4-fenil-butírico; ácido 3-(4'-bromo-bifenil-4-il)-3-fenilsulfanil-propionico; ácido 3-(5-(2-cloro-6-fluoro-4- (trifluorometil)-fenoxi)-2,4-dinitrofenil)propanoico; ácido 3-(3-(2-cloro-4-(trifluorometil)fenoxi)fenil)propanoico; ácido 3-(4-(4-metoxibenciloxi)fenil)pent-4-inoico; ácido 3-(4-(4-metoxibenciloxi)fenil)-5-(trimetilsilil)pent-4-inoico; ácido beta,beta-dimetil-4-[[[4-metil-2-[4-(trifluorometil)fenil]-5-tiazolil]metil]tio]-bencenpropanoico; ácido beta-amino-4-[(4-bromo-2,5-dihidro-2-metil-5-oxo-1-fenil-1H-pirazol-3-il)metoxi]-3-metoxi-bencepropanoico; o una de sus sales.
ARP050100748A 2004-02-27 2005-02-28 Derivados de acidos carboxilicos aromaticos con capacidad moduladora de los niveles de insulina, composiciones farmaceuticas que los contienen y su uso en el tratamiento de trastornos metabolicos que responden a la regulacion de gpr40 AR048306A1 (es)

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US54874104P 2004-02-27 2004-02-27
US60157904P 2004-08-12 2004-08-12

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US (2) US7816367B2 (es)
EP (1) EP1737809B1 (es)
JP (1) JP5299810B2 (es)
KR (1) KR20070004769A (es)
CN (1) CN1946666A (es)
AR (1) AR048306A1 (es)
AU (1) AU2005220728B2 (es)
BR (1) BRPI0508098A (es)
CA (1) CA2558585C (es)
CR (1) CR8642A (es)
EA (1) EA011010B1 (es)
EC (1) ECSP066887A (es)
ES (1) ES2433466T3 (es)
IL (1) IL177717A0 (es)
IS (1) IS8542A (es)
MA (1) MA28466B1 (es)
NO (1) NO20064362L (es)
TW (1) TW200539854A (es)
WO (1) WO2005086661A2 (es)

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