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PE20080058A1 - Derivados de azol con actividad en dgat1 - Google Patents

Derivados de azol con actividad en dgat1

Info

Publication number
PE20080058A1
PE20080058A1 PE2007000357A PE2007000357A PE20080058A1 PE 20080058 A1 PE20080058 A1 PE 20080058A1 PE 2007000357 A PE2007000357 A PE 2007000357A PE 2007000357 A PE2007000357 A PE 2007000357A PE 20080058 A1 PE20080058 A1 PE 20080058A1
Authority
PE
Peru
Prior art keywords
phenyl
acid
group
acetic
alkyl
Prior art date
Application number
PE2007000357A
Other languages
English (en)
Inventor
Michael H Serrano-Wu
Young-Shin Kwak
Wenming Liu
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38564569&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20080058(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20080058A1 publication Critical patent/PE20080058A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/10—Heterocyclic 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 aromatic rings
    • 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
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    • 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
    • A61K31/426—1,3-Thiazoles
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

REFERIDA A UN COMPUESTO DE FORMULA: A-L1-B-C-D-L2-E, DONDE A ES ALQUILO, CICLOALQUILO, ARILO, ENTRE OTROS; L1 ES NH, -CH2-CH2-NH-, AMIDA, ENTRE OTROS; B ES UN GRUPO HETEROARILO MONOCICLICO DE 5 O 6 MIEMBROS, SUSTITUIDO O NO SUSTITUIDO; C-D ES UNA ESTRUCTURA CICLICA DONDE C-D JUNTOS FORMAN UN GRUPO BIFENILO, C ES FENILO Y D ES UN ENLACE SIMPLE, C ES FENILO Y D ES UN ANILLO MONOCICLICO NO AROMATICO, ENTRE OTROS; L2 ES UN ENLACE SIMPLE O UN RESIDUO DE ESTRUCTURA -[R1]a-[R2]b-[C(O)]c-[N(R3)]d-[R4]e-[R5]f-, DONDE a, b, c, d, e Y f SON 0 O 1, CON LA CONDICION DE QUE (a+b+c+d+e+f) > 0 Y c=1 SI d=1; R1, R2, R4 Y R5 SON ALQUILO, ARILO, CICLOALQUILO, ENTRE OTROS; R3 ES H O HIDROCARBILO; E ES UN GRUPO ACIDO SULFONICO, UN GRUPO ALFA-CETO-HIDROXI-ALQUILO, UN GRUPO CARBOXILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO (4-{4-[2-(3-FLUORO-FENIL-AMINO)-PIRIMIDIN-5-IL]-FENIL}-CICLO-HEXIL)-ACETICO, ACIDO {4-[4-(2-FENIL-AMINO-PIRIMIDIN-5-IL)-FENIL]-CICLOHEXIL}-ACETICO, ACIDO (4-{4-[2-(3-METOXI-FENILAMINO)-TIAZOL-4-IL]-FENIL}-CICLOHEXIL)-ACETICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMBINACION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD SOBRE LA DGAT1 (ACIL COA-DIACIL-GLICEROL ACIL TRANSFERASA 1) Y SON UTILES EN EL TRATAMIENTO DE LA OBESIDAD Y COMPLICACIONES ASOCIADAS A LA OBESIDAD
PE2007000357A 2006-03-31 2007-03-29 Derivados de azol con actividad en dgat1 PE20080058A1 (es)

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