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 DISEASES

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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
Application number
Other languages
Spanish (es)
Inventor
Allen Jacob Duplantier
Louis Stanley Chupak
Anthony John Milici
Wan F Lau
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 ECSP003860 priority Critical patent/ECSP003860A/en
Publication of ECSP003860A publication Critical patent/ECSP003860A/en

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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.

ECSP003860 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 ECSP003860A (en)

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

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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)

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