ECSP003860A - NON-PEPTIDIC INHIBITORS OF THE VLA-4 DEPENDENT CELL UNION IN THE TREATMENT OF INFLAMMATORY, AUTOIMMUNE AND RESPIRATORY DISEASES - Google Patents
NON-PEPTIDIC INHIBITORS OF THE VLA-4 DEPENDENT CELL UNION IN THE TREATMENT OF INFLAMMATORY, AUTOIMMUNE AND RESPIRATORY DISEASESInfo
- Publication number
- ECSP003860A ECSP003860A ECSP003860A ECSP003860A EC SP003860 A ECSP003860 A EC SP003860A EC SP003860 A ECSP003860 A EC SP003860A EC SP003860 A ECSP003860 A EC SP003860A
- Authority
- EC
- Ecuador
- Prior art keywords
- substituted
- cycloalkyl
- alkyl
- group
- heterocyclyl
- Prior art date
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se describe un género de compuestos no pepetidicos, siendo los citados compuestos inhibidores de VLA-4 útiles en el tratamiento de enfermedades inflamatorias, autoinmunes y respiratorias y comprendiendo los citados compuestos un compuesto de fórmula (1.0.0) (gráfico), y sales y otros derivados profármacos de éste farmacéuticamente aceptables, en el que: A es alquilo (C1-C6), cicloalquilo, arilo, heteroarilo o heterociclilo opcionalmente sustituidos con 0 a 3 R9 o es un miembro seleccionado del grupo constituido por los siguientes radicales: A1 -NHC(=O)NH-A2-, A1-NHC(=O)=-A2-, A1-OC(=O)NH-A2, A1-NHSO2NH-A2, A1-NHC(=O)-A2-, A1-C(=0)NH-A2-, A1-NHSO2-A2-, A1-SO2NH-A2-, A1-(CH2)r-O-A2-, A1-O-(CH2)r-A2-, A1-(CH2)r-A2-, estando A1 y A2 cada uno seleccionado independientemente del grupo constituido por hidrógeno, arilo, alquilo (C1-C6), alquenilo (C2-C6), alquinilo (C2-C6), cicloalquilo, heteroarilo, y heterociclilo sustituido con 0 a 3 R9, B es un miembro selccionado independientemente del grupo constituidos por los siguientes: (gráfico), E es un enlace sencillo -O- NR10-, -CH=CH-, -C=C-, S(=0), -CR11R12NR10-, o -CR11R12-; X es -O-, -C(=O)-, -S(=O)q- o -NR10-; X1,X2 y X3 se seleccionan cada uno independientemente del grupo constituido por CH, CCR9 o N; y es un enlace sencillo, -C(=O)-, -C(=S)- o -S(=O)2-; -R7 es alquilo (C1-C6), (CH2)kOR5 (CH2)kNR6C(=O)R5, (CH2)xNR6C(=O)OR5, (CH2)kNR6SO2R5, (CH2)kNR6R5, F, CF3, OCF3, arilo sustituido con 0 a 3 R9, heterociclilo sustituido con 0 a 3 R9, heteroarilo sustituido con 0 a 3 R9 , cicloalquilo sustituido con 0 a 3 R9 o R7 puede tomarse conjuntamente con R8 para formar un anillo cicloalquilo o heterociclilo o R7 puede tomarse conjuntamente con R11 para formar un anillo ciccloalquilo o heterociclilo y R8 es hidrógeno F alquilo (C1-C6) o alcoxi (C1-C6).A genus of nonpepetidic compounds is described, said VLA-4 inhibitor compounds being useful in the treatment of inflammatory, autoimmune and respiratory diseases and said compounds comprising a compound of formula (1.0.0) (graph), and salts and other pharmaceutically acceptable prodrug derivatives thereof, in which: A is (C1-C6) alkyl, cycloalkyl, aryl, heteroaryl or heterocyclyl optionally substituted with 0 to 3 R9 or is a member selected from the group consisting of the following radicals: A1 - NHC (= O) NH-A2-, A1-NHC (= O) = - A2-, A1-OC (= O) NH-A2, A1-NHSO2NH-A2, A1-NHC (= O) -A2-, A1-C (= 0) NH-A2-, A1-NHSO2-A2-, A1-SO2NH-A2-, A1- (CH2) rO-A2-, A1-O- (CH2) r-A2-, A1- (CH2) r-A2-, with A1 and A2 each independently selected from the group consisting of hydrogen, aryl, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, cycloalkyl, heteroaryl, and heterocyclyl substituted with 0 to 3 R9, B is an independently selected member e of the group consisting of the following: (graph), E is a single link -O- NR10-, -CH = CH-, -C = C-, S (= 0), -CR11R12NR10-, or -CR11R12-; X is -O-, -C (= O) -, -S (= O) q- or -NR10-; X1, X2 and X3 are each independently selected from the group consisting of CH, CCR9 or N; y is a single bond, -C (= O) -, -C (= S) - or -S (= O) 2-; -R7 is (C1-C6) alkyl, (CH2) kOR5 (CH2) kNR6C (= O) R5, (CH2) xNR6C (= O) OR5, (CH2) kNR6SO2R5, (CH2) kNR6R5, F, CF3, OCF3, aryl substituted with 0 to 3 R9, heterocyclyl substituted with 0 to 3 R9, heteroaryl substituted with 0 to 3 R9, cycloalkyl substituted with 0 to 3 R9 or R7 can be taken together with R8 to form a cycloalkyl or heterocyclyl ring or R7 can be taken together with R11 to form a cycloalkyl or heterocyclyl ring and R8 is hydrogen F (C1-C6) alkyl or (C1-C6) alkoxy.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ECSP003860 ECSP003860A (en) | 2000-12-28 | 2000-12-28 | NON-PEPTIDIC INHIBITORS OF THE VLA-4 DEPENDENT CELL UNION IN THE TREATMENT OF INFLAMMATORY, AUTOIMMUNE AND RESPIRATORY DISEASES |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ECSP003860 ECSP003860A (en) | 2000-12-28 | 2000-12-28 | NON-PEPTIDIC INHIBITORS OF THE VLA-4 DEPENDENT CELL UNION IN THE TREATMENT OF INFLAMMATORY, AUTOIMMUNE AND RESPIRATORY DISEASES |
Publications (1)
Publication Number | Publication Date |
---|---|
ECSP003860A true ECSP003860A (en) | 2001-07-27 |
Family
ID=42041407
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ECSP003860 ECSP003860A (en) | 2000-12-28 | 2000-12-28 | NON-PEPTIDIC INHIBITORS OF THE VLA-4 DEPENDENT CELL UNION IN THE TREATMENT OF INFLAMMATORY, AUTOIMMUNE AND RESPIRATORY DISEASES |
Country Status (1)
Country | Link |
---|---|
EC (1) | ECSP003860A (en) |
-
2000
- 2000-12-28 EC ECSP003860 patent/ECSP003860A/en unknown
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