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AR061666A1 - Derivados de bencimidazol, metodo de produccion de los mismos y preparaciones farmaceuticas que los contienen - Google Patents

Derivados de bencimidazol, metodo de produccion de los mismos y preparaciones farmaceuticas que los contienen

Info

Publication number
AR061666A1
AR061666A1 ARP070102858A ARP070102858A AR061666A1 AR 061666 A1 AR061666 A1 AR 061666A1 AR P070102858 A ARP070102858 A AR P070102858A AR P070102858 A ARP070102858 A AR P070102858A AR 061666 A1 AR061666 A1 AR 061666A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
carbonyl
alkyl
alkoxy
fluor
Prior art date
Application number
ARP070102858A
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English (en)
Original Assignee
Hoffmann La Roche
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Publication date
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Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR061666A1 publication Critical patent/AR061666A1/es

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    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • A—HUMAN NECESSITIES
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    • 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
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    • A61P3/04—Anorexiants; Antiobesity agents
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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
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    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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  • Urology & Nephrology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Estos compuestos se fijan sobre el FXR y pueden utilizarse como medicamentos. Reivindicacion 1: Compuestos de la formula (1) en la que R1 es alquilo C1-10, (alcoxi inferior)-alquilo inferior, (alcoxi inferior)-carbonil-alquilo inferior, cicloalquilo, cicloalquil-alquilo inferior, arilo, aril-alquilo inferior, di-aril-alquilo inferior, heteroarilo, heteroaril-alquilo inferior, heterociclilo o heterociclil-alquilo inferior, en el que un grupo cicloalquilo, arilo, heteroarilo o heterociclilo está opcionalmente sustituido con 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, alcoxi inferior, (alcoxi inferior)-carbonilo, morfolinilo, formilamino, halogeno, hidroxi, fluor-alquilo inferior, fluor-alcoxi inferior, (alquilo inferior)-carbonil-N(alquilo inferior), (alquilo inferior)-carbonil-N(H), NH2, N(H, alquilo inferior), N(alquilo inferior)2, carboxi, carbamoílo, N(H, alquilo inferior)C(O) y N(alquilo inferior)2C(O); R2 es hidrogeno o alquilo inferior; R3 es alquilo inferior, cicloalquilo, cicloalquilo parcialmente insaturado arilo, aril-alquilo inferior, heteroarilo, heteroaril-alquilo inferior, heterociclilo o heterociclil-alquilo inferior, en los que un grupo arilo, heteroarilo o heterociclilo está opcionalmente sustituido con 1-3 sustituyentes elegidos con independencia entre el grupo formado por halogeno, alquilo inferior, alcoxi inferior, (alcoxi inferior)-carbonilo, hidroxi, fluor-alquilo inferior, fluor-alcoxi inferior, NH2, N(H, alquilo inferior), N(alquilo inferior)2, (alquilo inferior)-carbonil-N(alquilo inferior), (alquilo inferior)-carbonil-N(H), carboxi, carbamoílo, N(H, alquilo inferior)C(O) y N(alquilo inferior)2C(O); R4 es a) heteroarilo que está opcionalmente sustituido con 1-3 sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, fenilo, (alcoxi inferior)-carbonilo, carboxi, carbamoílo, N(H, alquilo inferior)-C(O), N(alquilo inferior)2C(O), NH2, N(H, alquilo inferior), N(alquilo inferior)2, (alquilo inferior)-carbonil-N(alquilo inferior), (alquilo inferior)-carbonil-N(H), hidroxi, alcoxi inferior, halogeno, fluor-alquilo inferior, fluor-alcoxi inferior, ciano y morfolinilo; b) naftilo sin sustituir o naftilo o fenilo que está sustituido con 1-3 sustituyentes elegidos con independencia entre el grupo formado por halogeno, hidroxi, NH2, CN, hidroxi-alquilo inferior, alcoxi inferior, (alquilo inferior)- carbonilo, (alquilo inferior)-carbonil-N(H), (alcoxi inferior)-carbonilo, sulfamoilo, di(alquilo inferior)-sulfamoilo, (alquilo inferior)-sulfonilo, tiofenilo, pirazolilo, tiadiazolilo, imidazolilo, triazolilo, tetrazolilo, 2-oxo-pirrolidinilo, pirrolilo, piridinilo, pirimidinilo, 2-oxo-piperidinilo, pirrolidinilo, piperidinilo, oxazolilo, tiazolilo, oxadiazolilo, carboxi, alquilo inferior, fluor-alquilo inferior, fluor-alcoxi inferior, N(H, alquilo inferior), N(alquilo inferior)2, (alquilo inferior)-carbonil-N(alquilo inferior), carbamoílo, N(H, alquilo inferior)C(O), N(alquilo inferior)2C(O), (alquilo inferior)-sulfamoilo, alquenilo inferior, benzoilo, fenoxi y fenilo que está opcionalmente sustituido con 1-3 sustituyentes elegidos con independencia entre halogeno y fluor-alquilo inferior; o c) si R3 es cicloalquilo y R4 es cicloalquilo, R4 puede ser también fenilo; R5, R6, R7 y R8 con independencia entre si son H, halogeno o alquilo inferior, o R5 y R6 están unidos entre sí, o R6 y R7 están unidos entre sí, o R7 y R8 están unidos entre si, para formar un anillo aromático o no aromático, carbocíclico o heterocíclico de 4-7 miembros junto con los átomos de carbono a los que están unidos; y las sales y los ésteres farmacéuticamente aceptables de los mismos; con la condicion de que el compuesto de la formula (1) no se elija entre el grupo formado por: la butilamida del ácido 2-[2-(2-cloro-fenil)-benzoimidazol-1-il]-4-metil-pentanoico y la 2-(2- benzo[1,3]dioxol-5-il-benzoimidazol-1-il)-N-bencil-butiramida.
ARP070102858A 2006-06-29 2007-06-27 Derivados de bencimidazol, metodo de produccion de los mismos y preparaciones farmaceuticas que los contienen AR061666A1 (es)

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US (1) US7645785B2 (es)
EP (1) EP2038259A1 (es)
JP (1) JP4970538B2 (es)
KR (1) KR101237623B1 (es)
CN (1) CN101479249B (es)
AR (1) AR061666A1 (es)
AU (1) AU2007263807B2 (es)
BR (1) BRPI0713946A2 (es)
CA (1) CA2655395C (es)
CL (1) CL2007001869A1 (es)
IL (1) IL195748A0 (es)
MX (1) MX2008015923A (es)
NO (1) NO20085121L (es)
RU (1) RU2424233C2 (es)
TW (1) TWI329638B (es)
WO (1) WO2008000643A1 (es)
ZA (1) ZA200810481B (es)

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