PE20030924A1 - Combinacion de inhibidores de ptm o inhibidores de la secrecion de apob con fibratos para la utilizacion como medicamentos - Google Patents

Combinacion de inhibidores de ptm o inhibidores de la secrecion de apob con fibratos para la utilizacion como medicamentos

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Publication number
PE20030924A1
PE20030924A1 PE2003000036A PE2003000036A PE20030924A1 PE 20030924 A1 PE20030924 A1 PE 20030924A1 PE 2003000036 A PE2003000036 A PE 2003000036A PE 2003000036 A PE2003000036 A PE 2003000036A PE 20030924 A1 PE20030924 A1 PE 20030924A1
Authority
PE
Peru
Prior art keywords
alkyl
inhibitors
ptm
carbonylamine
trifluoromethylbiphenyl
Prior art date
Application number
PE2003000036A
Other languages
English (en)
Inventor
Michael Mark
Leo Thomas
Original Assignee
Boehringer Ingelheim Pharma
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
Priority claimed from DE2002100633 external-priority patent/DE10200633A1/de
Priority claimed from DE10256184A external-priority patent/DE10256184A1/de
Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of PE20030924A1 publication Critical patent/PE20030924A1/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • A—HUMAN NECESSITIES
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
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    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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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
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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
    • A61K31/4427—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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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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Abstract

SE REFIERE AL USO DE FIBRATO SELECCIONADO DE BEZAFIBRATO, CIPROFIBRATO, CLOFIBRATO Y GEMFIBROZIL PARA REDUCIR LA TOXICIDAD DEL HIGADO DE INHIBIDORES DE PTM DE FORMULA I DONDE X1 ES CR1; X2 ES CR2; X3 ES CR3; X4 ES CR4 O UNO O DOS DE LOS GRUPO X1 A X4 SON NITROGENO Y EL RESTO ES CR1 A CR4; R1-R4 SON H, HALO, ALQUILO C1-C3, TRIFLUOROMETILO, OH, ALCOXI C1-C3, ENTRE OTROS; Aa ES O, S, NH, -N(ALQUILO C1-C3)-, SULFINILO, ENTRE OTROS; Ra ES FENILO, 1-NAFTILO, 2-NAFTILO, UN GRUPO HETEROARILO DE 5 MIEMBROS; R5 ES H, ALQUILO C1-C5; HET ES HETEROARILENO DE 5 MIEMBROS UNIDOS A TRAVES DE DOS ATOMOS DE C; R6 ES H, ALQUILO C1-C6; R7 ES ALQUILO C1-C9, ALQUENILO C3-C9, ENTRE OTROS. LOS COMPUESTOS DE FORMULA I SON AMIDA DE ACIDO N-[3-(BIFENIL-4-IL)-PROP-2-INIL]-4-(4´-TRIFLUOROMETILBIFENIL-2-CARBONILAMINO)-1-METIL-PIRROL-2-CARBOXILICO, AMIDA DE ACIDO N-[4-(1,4-DIOXA-8-AZA-ESPIRO[4.5]DEC-8-IL)-FENILMETIL]-4-(4´-TRIFLUOROMETILBIFENIL-2-CARBONILAMINO)-1-METIL-PIRROL-2-CARBOXILICO, AMIDA DE ACIDO N-[4-(3-AZA-ESPIRO[5.5]UNDEC-8-IL)-FENILMETIL]-4-(4´-TRIFLUOROMETILBIFENIL-2-CARBONILAMINO)-1-METIL-PIRROL-2-CARBOXILICO, ENTRE OTROS. SE REFIERE TAMBIEN A COMPOSICIONES FARMACEUTICAS QUE CONTIENEN UN INHIBIDOR DE PTM Y UN FIBRATO. LOS COMPUESTOS MENCIONADOS REDUCEN LA TOXICIDAD HEPATICA DE INHIBIDORES DE LA PROTEINA DE TRANSFERENCA DE TRIGLICERIDOS MICROSOMAL (PTM)
PE2003000036A 2002-01-10 2003-01-09 Combinacion de inhibidores de ptm o inhibidores de la secrecion de apob con fibratos para la utilizacion como medicamentos PE20030924A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2002100633 DE10200633A1 (de) 2002-01-10 2002-01-10 Kombination von MTP Inhibitoren oder apoB-Sekretions-Inhibitoren mit Fibraten zur Verwendung als Arzneimittel
DE10256184A DE10256184A1 (de) 2002-12-02 2002-12-02 Kombination von MTP Inhibitoren oder apoB-Sekretions-Inhibitoren mit Fibraten zur Verwendung als Arzneimittel

Publications (1)

Publication Number Publication Date
PE20030924A1 true PE20030924A1 (es) 2003-12-17

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PE2003000036A PE20030924A1 (es) 2002-01-10 2003-01-09 Combinacion de inhibidores de ptm o inhibidores de la secrecion de apob con fibratos para la utilizacion como medicamentos

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EP (1) EP1465613A2 (es)
JP (1) JP2005525309A (es)
AR (1) AR038178A1 (es)
AU (1) AU2003205570A1 (es)
CA (1) CA2471566A1 (es)
PE (1) PE20030924A1 (es)
TW (1) TW200402292A (es)
UY (1) UY27610A1 (es)
WO (1) WO2003057205A2 (es)

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TW200402292A (en) 2004-02-16
UY27610A1 (es) 2003-08-29
WO2003057205A2 (de) 2003-07-17
AU2003205570A1 (en) 2003-07-24
JP2005525309A (ja) 2005-08-25
CA2471566A1 (en) 2003-07-17

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