AR030026A1 - NEW CARBOXYLIC ACID DERIVATIVES WITH 5,6-REPLACED PYRIMIDINE RING, ITS USE TO PREPARE MEDICINES AND COMBINATIONS AND PHARMACEUTICAL PREPARATIONS UNDERSTANDING THEM - Google Patents

NEW CARBOXYLIC ACID DERIVATIVES WITH 5,6-REPLACED PYRIMIDINE RING, ITS USE TO PREPARE MEDICINES AND COMBINATIONS AND PHARMACEUTICAL PREPARATIONS UNDERSTANDING THEM

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AR030026A1
AR030026A1 ARP000103661A ARP000103661A AR030026A1 AR 030026 A1 AR030026 A1 AR 030026A1 AR P000103661 A ARP000103661 A AR P000103661A AR P000103661 A ARP000103661 A AR P000103661A AR 030026 A1 AR030026 A1 AR 030026A1
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Argentina
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alkyl
halogen
alkoxy
alkylthio
phenyl
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ARP000103661A
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Abbott Gmbh & Co Kg
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28—Oxygen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
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    • 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
    • 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
    • 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
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems

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  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Compuestos derivados de ácido carboxílicos con anillo de pirimidina 5,6 sustituido que responden a la formula 1 en donde R1 representa un tetrazol o un grupo: -C(:O)R en donde R tiene el siguiente significado: a) un radical OR7, en donde R7 significa: hidrogeno, el cation de un metal alcalino, el cation de un metal alcalinotérreo, un ion amonio orgánico fisiologicamente tolerable, como alquilamonio C1-4 terciario o el ion amonio; cicloalquilo-C3-8, alquilo C1-8, CH2-fenilo que puede estar sustituido por uno o varios de los siguientes restos: halogeno, nitro, ciano, alquiloC1-4, halogenoalquilo C1-4, hidroxi, alcoxi C1-4, mercapto, alquiltio C1-4, amino, NH(alquilo C1-4), N(alquilo C1-4)2, un grupo alquenilo-C3-6, o alquinilo C3-6, pudiendo llevar estos grupos a su vez uno a cinco átomos de halogeno; R7 puede ser además un radical fenilo, que puede llevar uno a cinco átomos de halogeno y/o uno a tres de los siguientes restos nitro, ciano, alquilo C1-4, halogenoalquilo C1-4, hidroxi, alcoxi C1-4, mercapto, alquiltio C1-4, amino, NH (alquilo C1-4), N (alquilo C1-4)2; un sistema heteroaromático de 5 miembros, ligado a través de un átomo de nitrogeno, tal como pirrolilo, pirazolilo, imidazolilo y triazolilo, que puede llevar a uno a dos átomos de halogeno, o uno a dos grupos alquilo C1-4 o uno a dos grupos alcoxi C1-4, formula 2 en la cual K puede tomar los valores 0, 1 y 2, p los valores 1, 2, 3, 4 y R8 representa: alquilo C1-4, cicloalquilo C3-8, alquenilo C3-6, alquinilo C3-6 o fenilo, que puede ser sustituido por uno o más, por ej. uno a tres de los siguientes restos: halogeno, nitro, ciano, alquilo C1-4, halogenoalquilo C1-4, hidroxi, alcoxi C1-4, alquiltio C1-4, mercapto, amino, NH(alquilo C1-4), N(alquilo C1-4)2; d) un resto formula 3 en donde R9 significa: alquilo-C1-4, alquenilo-C3-6, alquinilo-C3-8, pudiendo estos restos llevar a un resto alcoxi C1-4, alquiltio C1-4 y/o fenilo, como se indico bajo c); fenilo, que puede ser sustituido por uno a tres de los siguientes restos; halogeno, nitro, ciano, alquilo C1-4, halogenoalquilo C1-4, hidroxi, alcoxi C1-4, alquiltio C1-4, mercapto, amino, NH (alquilo C1-4), N (alquilo C1-4)2; R2 significa hidroxi, NH2, NH(alquilo C1-4)2, alquilo-C1-4, alquenilo-C2-4, alquinilo-C2-4, hidroxialquilo-C1-4, halogenoalquilo-C1-4, alcoxi-C1-, halogenoalcoxi-C1-4, alquiltio-C1-4, o CR2 forma junto con CR3 un anillo alquileno o alquenileno de 5 a 6 miembros, que puede ser sustituido por uno o dos grupos alquilo-C1-4, y en donde uno o más grupos metileno pueden ser reemplazados por oxígeno, azufre, -NH o -N(alquilo-C1-4). R3 significa hidroxi, NH2, NH(alquilo C1-4), N(alquilo C1-4)2, halogeno, alquilo-C1-4, alquenilo-C2-4, alquinilo-C2-4, alqueniloxi-C3-6, alquilcarbonilo-C1-4, alcoxi-carbonilo-C1-4, hidroxialquilo-C1-4, halogenoalquilo-C1-4, alcoxi-C1-4, halogenoalcoxi-C1-4, -NH-O-alquilo-C1-4, alquiltio-C1-4, o CR3 forma junto con CR2, como se indico bajo R2 un anillo de 5 a 6 miembros R4 y R5 (que pueden ser iguales o diferentes): significan fenilo o naftilo, que pueden ser sustituidos una o más veces por uno de los siguientes restos: halogeno, nitro, ciano, hidroxi, alquilo C1-4, halogenoalquilo C1-4, alcoxi C1-4, halogenoalcoxi C1-4, fenoxi, alquiltio C1-4, amino, NH (alquilo C1-4), N(alquilo C1-4)2; o fenilo o naftilo, que pueden estar unidos entre sí en posicion orto, a través de una union directa, un grupo metileno, etileno o etenileno, un átomo de oxígeno o de azufre o un grupo SO2, NH o N-alquilo; o cicloalquilo C3-7; R6 significa hidrogeno; alquilo C1-8, alquenilo C3-6, alquinilo C3-6 o cicloalquilo C3-8, pudiendo cada uno de estos restos ser sustituido una o más veces por hidroxi, mercapto, carboxi, halogeno, nitro, ciano, alcoxi C1-4, alqueniloxi C3-6, alquiniloxi C3-6, alquiltio C1-4, halogenoalcoxi C1-4, alquilcarbonilo C1-4, alcoxicarbonilo C1-4, NH carbonilo (alquilo C1-4), Ncarbonilo(alquilo C1-4)2, alquilcarbonilalquilo C3-8, amino, NH (alquilo C1-4), N(alquilo C1-4)2, fenoxi o fenilo, pudiendo ser sustituidos una o más veces los restos arilo mencionados; fenilo o naftilo que pueden ser sustituidos por uno o más de los siguientes restos: halogeno, nitro, ciano, hidroxi, amino, alquilo C1-4, halogenoalquilo C1-4, alcoxi C1-4, halogenoalcoxi C1-4, NH(alquilo C1-4), N(alquilo C1-4)2, o dioxometileno o dioxoetileno; un sistema heteroaromático de cinco o seis miembros que contiene uno a tres átomos de nitrogeno y/o un átomo de azufre u oxígeno y que puede llevar uno a cuatro átomos de halogeno y/o uno a dos de los siguientes restos: alquilo C1-4, halogenoalquilo C1-4, alcoxi C1-4, halogenoalcoxi C1-4, alquiltio, fenilo, fenoxi o fenilcarbonilo, siendo posible que los restos fenilo lleven a su vez uno a cinco átomos de halogeno y/o uno a tres de los siguientes restos; alquilo C1-4, halogenoalquilo C1-4, alcoxi C1-4, halogenoalcoxi C1-4 y/o alquiltio C1-4; Z es azufre u oxígeno, así como también las sales fisiologicamente aceptables, las formas tautomeras y las formas enantioméricamente y diastereoméricamente puras. Uso de los compuestos de formula 1 para preparar medicamentos para el tratamiento de enfermedades en las cuales hay niveles aumentados de endotelina, o bien la endotelina contribuye al desarrollo y/o al progreso de las mismas. Combinaciones de los compuestos de formula 1 y uno o más ingredientes activos seleccionados entre: inhibidores del sistema de renina-angiotensina, tales como inhibidores de renina, antagonistas de angiotensina 2, inhibidores de la enzima convertidora de angiotensina (ACE); inhibidores de ACE/endopeptidasa neutra (NEP) mixtos, bloqueadores B, diuréticos, antagonistas de calcio y sustancias bloqueadoras de VEGF. Preparados farmacéuticos para la administravion peroral y parenteral, que comprenden por dosis unitaria, además de los auxiliares farmacéuticos convencionales, por lo menos un compuesto de formula 1.Compounds derived from substituted 5.6 pyrimidine ring carboxylic acid which respond to formula 1 wherein R 1 represents a tetrazole or a group: -C (: O) R wherein R has the following meaning: a) an OR7 radical, wherein R7 means: hydrogen, the cation of an alkali metal, the cation of an alkaline earth metal, a physiologically tolerable organic ammonium ion, such as tertiary C1-4 alkylammonium or the ammonium ion; C3-8 cycloalkyl, C1-8 alkyl, CH2-phenyl which may be substituted by one or more of the following moieties: halogen, nitro, cyano, C1-4 alkyl, C1-4 halogenoalkyl, hydroxy, C1-4 alkoxy, mercapto , C1-4 alkylthio, amino, NH (C1-4 alkyl), N (C1-4 alkyl) 2, a C3-6 alkenyl group, or C3-6 alkynyl, these groups being able to take one to five atoms halogen; R7 can also be a phenyl radical, which can carry one to five halogen atoms and / or one to three of the following nitro, cyano, C1-4 alkyl, C1-4 halogenoalkyl, hydroxy, C1-4 alkoxy, mercapto, C1-4 alkylthio, amino, NH (C1-4 alkyl), N (C1-4 alkyl) 2; a 5-membered heteroaromatic system, linked through a nitrogen atom, such as pyrrolyl, pyrazolyl, imidazolyl and triazolyl, which can carry one to two halogen atoms, or one to two C1-4 alkyl groups or one to two C1-4 alkoxy groups, formula 2 in which K can take the values 0, 1 and 2, p the values 1, 2, 3, 4 and R8 represent: C1-4 alkyl, C3-8 cycloalkyl, C3-6 alkenyl , C3-6 alkynyl or phenyl, which may be substituted by one or more, eg. one to three of the following moieties: halogen, nitro, cyano, C1-4 alkyl, halogen C1-4 alkyl, hydroxy, C1-4 alkoxy, C1-4 alkylthio, mercapto, amino, NH (C1-4 alkyl), N ( C1-4 alkyl) 2; d) a formula 3 moiety wherein R9 means: C1-4 alkyl, C3-6 alkenyl, C3-8 alkynyl, these moieties being able to carry a C1-4 alkoxy, C1-4 alkylthio and / or phenyl moiety, as indicated under c); phenyl, which can be substituted by one to three of the following moieties; halogen, nitro, cyano, C1-4 alkyl, halogen C1-4 alkyl, hydroxy, C1-4 alkoxy, C1-4 alkylthio, mercapto, amino, NH (C1-4 alkyl), N (C1-4 alkyl) 2; R2 means hydroxy, NH2, NH (C1-4 alkyl) 2, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 hydroxyalkyl, C1-4 halogenoalkyl, C1- alkoxy, halogenoalkoxy-C1-4, alkylthio-C1-4, or CR2 together with CR3 forms a 5- or 6-membered alkylene or alkenylene ring, which can be substituted by one or two C1-4 alkyl groups, and wherein one or more Methylene groups can be replaced by oxygen, sulfur, -NH or -N (C1-4 alkyl). R3 means hydroxy, NH2, NH (C1-4 alkyl), N (C1-4 alkyl) 2, halogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 alkenyloxy, alkylcarbonyl -C1-4, C1-4 alkoxycarbonyl, C1-4 hydroxyalkyl, C1-4 halogenoalkyl, C1-4 alkoxy, C1-4 halogenoalkoxy, -NH-O-C1-4 alkyl, alkylthio- C1-4, or CR3 forms together with CR2, as indicated under R2 a ring of 5 to 6 members R4 and R5 (which can be the same or different): they mean phenyl or naphthyl, which can be substituted one or more times by one of the following moieties: halogen, nitro, cyano, hydroxy, C 1-4 alkyl, C 1-4 halogenalkyl, C 1-4 alkoxy, C 1-4 halogenoalkoxy, phenoxy, C 1-4 alkylthio, amino, NH (C 1-4 alkyl), N (C1-4 alkyl) 2; or phenyl or naphthyl, which may be linked to each other in ortho position, through a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO2, NH or N-alkyl group; or C3-7 cycloalkyl; R6 means hydrogen; C1-8 alkyl, C3-6 alkenyl, C3-6 alkynyl or C3-8 cycloalkyl, each of these moieties can be substituted one or more times by hydroxy, mercapto, carboxy, halogen, nitro, cyano, C1-4 alkoxy, C3-6 alkenyloxy, C3-6 alkynyloxy, C1-4 alkylthio, C1-4 halogenoalkoxy, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, NH carbonyl (C1-4 alkyl), Ncarbonyl (C1-4 alkyl) 2, C3 alkylcarbonylalkyl -8, amino, NH (C1-4 alkyl), N (C1-4 alkyl) 2, phenoxy or phenyl, the aforementioned aryl moieties may be substituted one or more times; phenyl or naphthyl which may be substituted by one or more of the following moieties: halogen, nitro, cyano, hydroxy, amino, C1-4 alkyl, halogen C1-4 alkyl, C1-4 alkoxy, halogenoalkoxy C1-4, NH (C1 alkyl -4), N (C1-4 alkyl) 2, or dioxomethylene or dioxoethylene; a five or six membered heteroaromatic system that contains one to three nitrogen atoms and / or one sulfur or oxygen atom and that can carry one to four halogen atoms and / or one to two of the following moieties: C1-4 alkyl , C1-4 halogenoalkyl, C1-4 alkoxy, C1-4 halogenoalkoxy, alkylthio, phenyl, phenoxy or phenylcarbonyl, it being possible that the phenyl moieties in turn carry one to five halogen atoms and / or one to three of the following moieties ; C1-4 alkyl, C1-4 halogenoalkyl, C1-4 alkoxy, C1-4 halogenoalkoxy and / or C1-4 alkylthio; Z is sulfur or oxygen, as well as physiologically acceptable salts, tautomeric forms and enantiomerically and diastereomerically pure forms. Use of the compounds of formula 1 to prepare medicaments for the treatment of diseases in which there are increased levels of endothelin, or else endothelin contributes to their development and / or progress. Combinations of the compounds of formula 1 and one or more active ingredients selected from: renin-angiotensin system inhibitors, such as renin inhibitors, angiotensin 2 antagonists, angiotensin-converting enzyme (ACE) inhibitors; ACE / neutral endopeptidase mixed (NEP) inhibitors, B blockers, diuretics, calcium antagonists and VEGF blocking substances. Pharmaceutical preparations for peroral and parenteral administration, comprising per unit dose, in addition to conventional pharmaceutical auxiliaries, at least one compound of formula 1.

ARP000103661A 1999-07-20 2000-07-17 NEW CARBOXYLIC ACID DERIVATIVES WITH 5,6-REPLACED PYRIMIDINE RING, ITS USE TO PREPARE MEDICINES AND COMBINATIONS AND PHARMACEUTICAL PREPARATIONS UNDERSTANDING THEM AR030026A1 (en)

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DE19933164A DE19933164A1 (en) 1999-07-20 1999-07-20 New carboxylic acid derivatives with 5,6 substituted pyrimidine ring, their production and use as endothelin receptor antagonists

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DE19933164A1 (en) 2001-01-25
WO2001005771A1 (en) 2001-01-25
EP1196394A1 (en) 2002-04-17
CZ2002190A3 (en) 2003-08-13
TW555749B (en) 2003-10-01
CA2379545A1 (en) 2001-01-25
MXPA02000616A (en) 2002-08-30

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