ECSP993188A - SERINE PROTEASE INHIBITOR - Google Patents
SERINE PROTEASE INHIBITORInfo
- 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
Links
Landscapes
- 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.
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) |
-
1999
- 1999-10-22 EC ECSP993188 patent/ECSP993188A/en unknown
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CO5140114A1 (en) | AMINOISOQUINOLINE DERIVATIVES | |
RU2001113734A (en) | SERINE PROTEASES INHIBITOR | |
RU2007123360A (en) | Pyrrolopyrazines and pyrazolopyrazines USEFUL AS PROTEINKINASE INHIBITORS | |
DE60131160D1 (en) | CASPASE INHIBITORS AND ITS USES | |
AR002971A1 (en) | COMPOUNDS OF 3- (1,2,3,6) -TETRAHIDROPIRIDIN-4-ILO AND 3-PIPERIDIN-4-ILO-1H- INDOL, AGONISTS OF 5HT (1f) CONTAINING PHARMACEUTICAL FORMULATIONS AND METHODS FOR ACTIVATING SUCH 5HT RECEPTORS ( 1f) AND / OR TO TREAT MIGRANES AND DISORDERS ASSOCIATED WITH IT. | |
TW200504047A (en) | Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof | |
FI101622B1 (en) | Process for the preparation of therapeutically active N- (4-piperidyl) (dihydrobenzofuran) carboxamide or N- (4-piperidyl) (dihydro-2H-benzopyran) carboxamide derivatives and intermediate | |
AR040390A1 (en) | THYROSINE KINASE INHIBITORS | |
UY28578A1 (en) | AMIDA DERIVATIVES | |
AR046600A1 (en) | DIAZAESPIROALCANOS AND ITS USE AS A TREATMENT FOR DISEASES MEDIATED BY CCR8 | |
AR055669A1 (en) | DERIVATIVES OF 3H - IMIDAZO [4, 5 -B] PIRIDINE AS SELECTIVE INHIBITORS OF GSK3, METHODS AND INTERNEDIARIES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE FOR THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OF NEURODE DISEASE. | |
CO4650042A1 (en) | 6-PHENYLPIRIDYL-2-AMINE DERIVATIVES | |
CY1109748T1 (en) | KINOXALINYL MACROCYCLIC SERIES OF PROTECTION OF SERINE USITIS C | |
AR012631A1 (en) | SERINE PROTEASE INHIBITORS | |
FR2619111B1 (en) | (PIPERIDINYL-4) METHYL-2 TETRAHYDRO-1,2,3,4 9H-PYRIDO (3,4-B) INDOLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION | |
FI952424A (en) | 11,21-bisphenyl-19-norpregnane derivatives | |
ES2195382T3 (en) | INDOLCARBOXYL COMPOUNDS AND THEIR USE AS PHARMACEUTICAL COMPOUNDS. | |
CA2136553A1 (en) | 7-(2-aminoethyl)-Benzothiazolones | |
AR031085A1 (en) | INHIBITING COMPOUNDS OF PROTEINASE C OF PROCOLAGEN, ITS USE IN MEDICINE, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, MANUFACTURING PROCEDURE AND USEFUL COMPOUNDS IN THE SAME | |
CO4970719A1 (en) | PIRROLOPYROLONE DERIVATIVES AS LEUCOCITARY ELASTASE INHIBITORS | |
TR200201150T2 (en) | Method for administering a phosphodiesterase 4 inhibitor. | |
ECSP993188A (en) | SERINE PROTEASE INHIBITOR | |
HUP0202988A2 (en) | Substituted 3-phenyl-5-alkoxi-1,3,4-oxdiazol-2-one derivatives and their use as lipase inhibitors, process for their preparation and pharmaceutical compositions containing them | |
AR039041A1 (en) | CYCLOPENTENE DERIVATIVES | |
PE20040916A1 (en) | PYRIMIDIN-4,6-DICARBOXYL ACID DIAMIDES AS SELECTIVE INHIBITORS OF MMP-13 |