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US 2008/0167348 A1Published application
Novel sulfonamide derivatives
AssigneeHoffmann-La Roche Inc.
InventorsDavid Banner, Harald Mauser, Rudolf E. Minder, Hans P. Wessel
Life of this patent
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Abstract
The invention is concerned with the novel sulfonamide derivatives of formula (I) wherein A, R1 to R2″, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.
Claims20
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- A is selected from the group consisting of:
- (1) a phenyl ring,
- (2) a heteroaryl ring, which is a monocyclic aromatic ring of 5 or 6 ring atoms, containing one or two ring heteroatoms of N, O or S, with the remaining ring atoms being carbon, and
- (3) a heterocyclyl ring, which is a non-aromatic monocyclic ring of 5 or 6 ring atoms, containing one or two ring heteroatoms of N or S(O)n (where n is an integer from 0 to 2), with the remaining ring atoms being carbon, wherein one of the ring carbon atoms of the heterocyclyl ring is optionally replaced with a carbonyl group;
- R1 and R1′ are independently selected from the group consisting of:
- (1) hydrogen,
- (2) halogen,
- (3) nitro,
- (4) cyano,
- (5) amino,
- (6) C1-6 alkyl,
- (7) heteroalkyl,
- (8) C3-7 cycloalkyl,
- (9) C2-6 alkenyl,
- (10) C2-6 alkynyl,
- (11) hydroxy,
- (12) C1-6 alkoxy,
- (13) —NR′R″ or —(C0-6 alkylene)-NR′R″, in which R′ and R″ are independently selected from the group consisting of hydrogen, C1-6 alkyl, heteroalkyl, formyl, C1-6 alkylcarbonyl, optionally substituted C3-7 cycloalkylcarbonyl, optionally substituted arylcarbonyl, optionally substituted heteroarylcarbonyl, optionally substituted heterocyclylcarbonyl, C1-6 alkylsulfonyl, optionally substituted C3-7 cycloalkylsulfonyl, optionally substituted arylsulfonyl, optionally substituted heteroarylsulfonyl, and optionally substituted heterocyclylsulfonyl, and
- (14) —(C0-6 alkylene)-OR′, in which R1 is hydrogen, C1-6 alkyl, heteroalkyl, formyl or C1-6 alkylcarbonyl,
- wherein both R1 and R1″ exist or alternatively R1 exists but R1′ does not exist;
- R2, R2′ and R2″ are independently selected from the group consisting of hydrogen, halogen, cyano, nitro, amino, mono-C1-6 alkyl substituted amino, di-C1-6 alkyl substituted amino, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, hydroxy, and C1-6 alkoxy;
- X is phenylene optionally substituted by one, two or three substituents independently selected from the group consisting of halogen, cyano, nitro, amino, mono-C1-6 alkyl substituted amino, di-C1-6 alkyl substituted amino, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, hydroxy, C1-6 alkoxy, halo C1-6 alkyl, halo C1-6 alkoxy, heteroalkyloxy, C1-6 alkylsulfonyl, C1-6 alkylsulfinyl, C1-6 alkylthio, C1-6 alkylsulfonyl-C1-6 alkyl, C1-6 alkylsulfinyl-C1-6 alkyl, C1-6 alkylthio-C1-6 alkyl, acyl, formyl, C1-6 alkoxycarbonyl, halo C1-6 alkoxycarbonyl, heteroalkyloxycarbonyl and heteroalkylcarbonyl;
- and
- Y is selected from the group consisting of:
- (1) an optionally substituted heteroaryl, wherein the heteroaryl is a monocyclic aromatic radical of 6 ring atoms, containing one or two ring heteroatoms of N(O)n(where n is 0 or 1), O or S, with the remaining ring atoms being carbon atoms, and
- (2) an optionally substituted heterocyclyl, wherein the heterocyclyl is a non-aromatic monocyclic radical of six ring atoms, containing one or two ring heteroatoms of N, O, or S(O)n (where n is an integer from 0 to 2), with the remaining ring atoms being carbon atoms.
24 more elements
5-Fluoro-3-methyl-benzo[b]thiophene-2-sulfonic acid (4-pyridin-4-yl-2-trifluoromethyl-phenyl)-amide.
Dependencies are inferred from the claim text.