ECSP993188A - SERINE PROTEASE INHIBITOR - Google Patents

SERINE PROTEASE INHIBITOR

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Publication number
ECSP993188A
ECSP993188A ECSP993188A ECSP993188A EC SP993188 A ECSP993188 A EC SP993188A EC SP993188 A ECSP993188 A EC SP993188A EC SP993188 A ECSP993188 A EC SP993188A
Authority
EC
Ecuador
Prior art keywords
cycloalkyl
alkyl
alkoxy
optionally substituted
het
Prior art date
Application number
Other languages
Spanish (es)
Inventor
Cornelis Marius Timmers
Johannes Bernardus Maria Rewinkel
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 filed Critical
Priority to ECSP993188 priority Critical patent/ECSP993188A/en
Publication of ECSP993188A publication Critical patent/ECSP993188A/en

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La invención se refiere a un inhibidor de proteasas de serina que tiene fórmula I (gráfico), donde J es H, R1, R1-O-C (O)-, R1-C(O)-, R1-SO2-, R3OOC- (CHR2)p, (R2a, R2b) N-CO-(CHR2)p - ó Het-CO -(CHR2)p-, D es un amino-ácido de la fórmula-NH-CHR1-C(O)-, -NR4-CH (CH2) qC (O) OR1 -C(O)-, -NR4-CH (CH2) qC(O) N (R2a, R2b) -C(O)-, NR4 -CH (CH2) qC (O) Het -C(O)-, D-1-Tiq, D-3-Tiq, D-Atc, Aic, D-1-Piz ó D-3-Piq; E es -NR2 -CH2- ó el fragmento opcionalmente sustituido con (1-6C)alquilo, (1-6C) alcoxi o benciloxi; R1 se selecciona entre (1-12C) alquilo, (2-12C) alquenilo, (2-12C) alquinilo, (3-12C) cicloalquilo y (3-12C) cicloalquil -(1-6C) alquileno, cuyos grupos pueden estar opcionalmente sustituidos con (3-12C) cicloalquilo; (1-6C) alcoxi, oxo, OH, CF3 ó halógeno y entre (6-14C)arilo, (7-15C)aralquilo, (8-16C) aralquenilo y (14-20C)(bisaril)alquilo, donde los grupos arilo pueden estar opcionalmente sustituidos con (1-6C) alquilo, (3-12C) cicloalquilo, (1-6C) alcoxi, OH, CF3 ó halógeno;R2, R2a y R2b son seleccionados cada uno independientemente entre H, (1-8C) alquilo, (3-8C) alquenilo, (3-8C) alquinilo, (3-8C) cicloalquilo y (3-6C) cicloalquil(1-4C) alquileno, donde cada uno puede estar opcionalmente sustituido con (3-6C) cicloalquilo, (1-6C) alcoxi, CF3 ó halógeno y entre (6-14C) arilo y (7-15C) aralquilo donde los grupos arilo pueden estar opcionalmente sustituidos con (1-6C) alquilo, (3-6C) cicloalquilo, (1-6C) alcoxi, CF3 ó halógeno; R3 es como se definio para R2 ó Het-(1-6C)alquilo; R4 es H ó (1-3C) alquilo; X e Y son CH ó N con la salvedad de que no sean ambos N; Het es un heterociclo de 4, 5 ó 6 miembros que contiene uno o más heteroátomos seleccionados entre O, N y S; m es 1 ó 2; p es 1,2 ó 3; q es 1,2 ó 3; t es 2,3 ó 4; o una prodroga; o una sal de adición y/o solvato farmacéutico aceptable del mismo y su uso en terapia, y a la fabricación de un medicamento para tratar o prevenir enfermedades mediadas por trombina y asociadas con trombina.The invention relates to a serine protease inhibitor having formula I (graph), where J is H, R1, R1-OC (O) -, R1-C (O) -, R1-SO2-, R3OOC- ( CHR2) p, (R2a, R2b) N-CO- (CHR2) p - or Het-CO - (CHR2) p-, D is an amino acid of the formula-NH-CHR1-C (O) -, - NR4-CH (CH2) qC (O) OR1 -C (O) -, -NR4-CH (CH2) qC (O) N (R2a, R2b) -C (O) -, NR4 -CH (CH2) qC ( O) Het -C (O) -, D-1-Tiq, D-3-Tiq, D-Atc, Aic, D-1-Piz or D-3-Piq; E is -NR2 -CH2- or the fragment optionally substituted with (1-6C) alkyl, (1-6C) alkoxy or benzyloxy; R1 is selected from (1-12C) alkyl, (2-12C) alkenyl, (2-12C) alkynyl, (3-12C) cycloalkyl, and (3-12C) cycloalkyl - (1-6C) alkylene, the groups of which can be optionally substituted with (3-12C) cycloalkyl; (1-6C) alkoxy, oxo, OH, CF3 or halogen and between (6-14C) aryl, (7-15C) aralkyl, (8-16C) aralkenyl and (14-20C) (bisaryl) alkyl, where the groups aryl can be optionally substituted with (1-6C) alkyl, (3-12C) cycloalkyl, (1-6C) alkoxy, OH, CF3 or halogen; R2, R2a and R2b are each independently selected from H, (1-8C ) alkyl, (3-8C) alkenyl, (3-8C) alkynyl, (3-8C) cycloalkyl, and (3-6C) cycloalkyl (1-4C) alkylene, where each can be optionally substituted with (3-6C) cycloalkyl, (1-6C) alkoxy, CF3 or halogen and between (6-14C) aryl and (7-15C) aralkyl where aryl groups can be optionally substituted with (1-6C) alkyl, (3-6C) cycloalkyl, (1-6C) alkoxy, CF3 or halogen; R3 is as defined for R2 or Het- (1-6C) alkyl; R4 is H or (1-3C) alkyl; X and Y are CH or N with the exception that they are not both N; Het is a 4-, 5-, or 6-membered heterocycle containing one or more heteroatoms selected from O, N, and S; m is 1 or 2; p is 1,2 or 3; q is 1,2 or 3; t is 2,3 or 4; or a prodrug; or an acceptable pharmaceutical addition and / or solvate salt thereof and its use in therapy, and to the manufacture of a medicament for treating or preventing thrombin-mediated and thrombin-associated diseases.

ECSP993188 1999-10-22 1999-10-22 SERINE PROTEASE INHIBITOR ECSP993188A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
ECSP993188 ECSP993188A (en) 1999-10-22 1999-10-22 SERINE PROTEASE INHIBITOR

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ECSP993188 ECSP993188A (en) 1999-10-22 1999-10-22 SERINE PROTEASE INHIBITOR

Publications (1)

Publication Number Publication Date
ECSP993188A true ECSP993188A (en) 2000-01-27

Family

ID=42044177

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP993188 ECSP993188A (en) 1999-10-22 1999-10-22 SERINE PROTEASE INHIBITOR

Country Status (1)

Country Link
EC (1) ECSP993188A (en)

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