AR035040A1 - Derivados de imidazolilo, composiciones farmaceuticas que los comprenden y el uso de los mismos para la preparacion de medicamentos capaces de unir selectivamente a los subtipos del receptor de somatostatina - Google Patents

Derivados de imidazolilo, composiciones farmaceuticas que los comprenden y el uso de los mismos para la preparacion de medicamentos capaces de unir selectivamente a los subtipos del receptor de somatostatina

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Publication number
AR035040A1
AR035040A1 ARP010103657A ARP010103657A AR035040A1 AR 035040 A1 AR035040 A1 AR 035040A1 AR P010103657 A ARP010103657 A AR P010103657A AR P010103657 A ARP010103657 A AR P010103657A AR 035040 A1 AR035040 A1 AR 035040A1
Authority
AR
Argentina
Prior art keywords
alkyl
syndrome
group
optionally substituted
thiophene
Prior art date
Application number
ARP010103657A
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English (en)
Original Assignee
Sod Conseils Rech Applic
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
Application filed by Sod Conseils Rech Applic filed Critical Sod Conseils Rech Applic
Publication of AR035040A1 publication Critical patent/AR035040A1/es

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  • Plural Heterocyclic Compounds (AREA)

Abstract

Derivados de imidazolilo, que comprenden un compuesto de la fórmula (1), las mezclas racémicas, diastereoméricas e isómeros ópticos de dicho compuesto de fórmula (1), sus sales y profármacos farmacéuticamente aceptables o su sal farmacéuticamente aceptable, en donde: la línea de puntos representa un enlace optativo; R1 es H, -(CH2)m-C(O)-(CH2)m-Z1, -(CH2)m-Z1, -(CH2)m-O-Z1 o -alquilo(C0-6)-C(O)-NH-(CH2)m-Z3; Z1 es una porción optativamente sustituida seleccionada entre el grupo que consiste en alquilo C1-12, benzo[b]tiofeno, fenilo, naftilo, benzo[b]furanilo, tiofeno, isoxazolilo, indolilo, o un radical del grupo (2); R2 es H o alquilo(C1-6); o R1 y R2 son tomados juntos con los átomos de nitrógeno a los cuales están unidos para formar un compuesto de fórmula (Ia), (Ib) o (Ic); R3 es -(CH2)m-E-(CH2)m-Z2; E es O, S, -C(O)-, -C(O)-O-, NH-C(O)-O- ó un enlace; Z2 es H, alquilo(C1-12), amino, alquilamino(C1-12), N,N-di-alquilamino(C1-12), alquilguanidino(C1-12), o una porción optativamente sustituida seleccionada entre el grupo que consiste en fenilo, indolilo, imidazolilo, tiofeno, benzotiofeno, piridinilo y naftilo; R4 es H o -(CH2)m-A1; A1 es -C(=Y)-N(X1X2), -C(=Y)-X2, -C(=NH)-X2 ó X2; Y es O u S; X1 es H, alquilo(C1-12), -(CH2)m-NH-alquilo(C1-6), -(CH2)m-N-di-alquilo(C1-6) o -(CH2)m-arilo; X2 es -(CH2)m-Y1-X3 o alquilo(C1-12) optativamente sustituido; Y1 es O, S, NH, C=O, alquenilo(C2-12) que tiene uno o más enlaces dobles, -NH-CO-, -CO-NH-, NH-CO-O-(CH2)m-, -C=C-, SO2 o un enlace; X3 es H, una porción optativamente sustituida seleccionada entre el grupo que consiste en alquilo(C1-12), cicloalquilo(C3-8), alcoxi(C1-12), ariloxi, alquilamino(C1-12), N,N-di-alquilamino(C1-12), -CH-di-alcoxi(C1-12), pirrolidinilo, piridinilo, tiofeno, imidazolilo, piperidinilo, piperazinilo, benzotiazolilo, furanilo, indolilo, morfolino, benzo[b]furanilo, quinolinilo, isoquinolinilo, -(CH2)m-fenilo, naftilo, fluorenilo, ftalamidilo, pirimidinilo, o un radical del grupo (3); o X1 y X2 son tomados conjuntamente con el nitrógeno al cual están unidos para formar una porción optativamente sustituida seleccionada entre el grupo que consiste en tiazolilo; composiciones farmacéuticas que las comprenden y los usos de dichos derivados de imidazolilo para la preparación de medicamentos útiles para acromegalia, restenosis, enfermedad de Crohn, esclerosis sistémica, pseudoquistes y ascitis pancreáticos externos e internos, VIPoma, nesidoblastosis, hiperinsulinismo, gastrinoma, síndrome de Zollinger-Ellison, diarrea, diarrea relacionada con SIDA, diarrea relacionada con la quimioterapia, escleroderma, síndrome de intestino irritable, pancreatitis, obstrucción del intestino delgado, reflujo gastroesofágico, reflujo duodenogástrico, Síndrome de Cushing, gonadotropinoma, hiperparatiroidismo, Mal de Graves, neuropatía diabética, Mal de Paget, síndrome del ovario poliquístico, cáncer, caquexia del cáncer, hipotensión, hipotensión posprandial, ataques de pánico, adenomas secretores de GH o adenomas secretores de TSH, diabetes mellitus, hiperlipidemia, insensibilidad a la insulina, Síndrome X, angiopatía, retinopatía proliferativa, fenómeno del alba Nefropatía, úlceras pépticas, fístulas enterocutáneas y pancreaticocutáneas, síndrome de vaciamiento rápido, síndrome de diarrea acuosa, pancreatitis aguda o crónica, tumores secretores de la hormona gastrointestinal, agiogénesis, trastornos inflamatorios, rechazo al aloinjerto crónico, angioplastía, hemorragias de los vasos de injerto y gastrointestinales, y para inhibir la proliferación de helicobacter pylori en un sujeto que lo necesita.
ARP010103657A 2000-08-01 2001-07-31 Derivados de imidazolilo, composiciones farmaceuticas que los comprenden y el uso de los mismos para la preparacion de medicamentos capaces de unir selectivamente a los subtipos del receptor de somatostatina AR035040A1 (es)

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