C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/04 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) A61K 31/675 (2006.01) C07D 221/04 (2006.01) C07D 239/70 (2006.01) C07D 241/38 (2006.01) C07D 401/04 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 419/04 (2006.01) C07D 419/14 (2006.01) C07F 9/576 (2006.01)
Patent
CA 2169737
A heteroaromatic ring-fused cyclopentene derivative of the formula: Image (I) wherein each of Ar1 and Ar2 is independently a phenyl group, a thienyl group, a pyridyl group, an indolyl group, a benzofuranyl group or a dihydrobenzofuranyl group wherein an optional hydrogen atom(s) on the aromatic ring may be replaced with 1 to 4 groups selected from the group consisting of a halogen atom, a hydroxyl group, an amino group, a carboxyl group, a C1-C6 alkoxycarbonyl group, a mono- or di- C1-C6 alkylaminocarbonyl group, a carbamoyl group, a tetrazol-5-yl group, a methylenedioxy group, a C1-C6 alkoxy group, a C2-C6 alkenyloxy group, a mono- or di- C1-C6 alkylamino group, a C1-C6 alkyl group, a C2-C6 alkenyl group and a C2-C6 alkynyl group (provided that the C1-C6 alkoxy group, C2-C6 alkenyloxy group, mono- or di- C1-C6 alkylamino group, C1-C6 alkyl group, C2-C6 alkenyl group and C2-C6 alkynyl group may be substituted by 1 to 3 groups selected from the group consisting of a phenyl group, a pyridyl group, an imidazolyl group, a hydroxyl group, a C1-C6 alkoxy group, an amino group, a mono- or di- C1-C6 alkylamino group, a hydroxy C1-C6 alkylcarbonyl group, a C1-C6 acyloxy C1-C6 alkylcarbonyl group, a carboxy C1-C6 alkoxycarbonyl group, a carboxy C1-C6 alkoxycarbonyl C1-C6 alkoxycarbonyl group, a C1-C6 alkoxycarbonyl group, a mono- or di- C1-C6 alkyl- aminocarbonyl group, a carbamoyl group, a C1-C6 alkylsulfonylaminocarbonyl group, a tetrazol-5-ylamino- carbonyl group, a carboxyl group, SO3H, PO3H2, a tetrazol-5-yl group, a 2-oxo-3H-1,2,3,5-oxathia- diazol-4-yl group and a 5-oxo-4H-1,2,4-oxadiazol-3-yl group (provided that when a hydroxyl group and a carboxyl group are selected as substituents, they may together form a lactone ring)); each of R1, R2 and R3 is independently a hydrogen atom, a hydroxyl group or a C1-C6 alkyl group, or R1 and R2, or R2 and R3 together form a single bond; Y is a group of -CO-R4 (wherein R4 is a hydroxyl group, an amino group, a C1-C6 alkoxy group, a mono- or di- C1-C6 alkylamino group, a C1-C6 alkylsulfonylamino group, or an arylsulfonylamino group or an aryl C1-C6 alkylsulfonylamino group wherein an optional hydrogen atom(s) on the aryl ring may be replaced with a C1-C6 alkyl group), SO3H, PO3H2, a tetrazol-5-yl group, a 2-oxo-3H-1,2,3,5-oxathiadiazol-4-yl group or a 5-oxo-4H-1,2,4-oxadiazol-3-yl group; and A is a group which forms together with the adjacent carbon-carbon double bond a 5- or 6- membered heteroaromatic ring including 1 to 4 hetero atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom (provided that optional 1 or 2 hydrogen atoms on the heteroaromatic ring may be replaced with a hydroxyl group, an amino group, a C1-C6 alkoxy group, a C1-C6 alkylthio group, a halogen atom, a cyano group, a nitro group, a mono- or di- C1-C6 alkylamino group which may be substituted by a hydroxyl group at the alkyl moiety, a C3-C8 cycloalkylamino group which may be substituted by a hydroxyl group at the alkyl or alkylene moiety, a C3-C8 cycloalkyl C1-C6 alkylamino group which may be substituted by a hydroxyl group at the alkyl or alkylene moiety, an N-(C1-C6 alkyl)-N-(C3-C8 cycloalkyl)amino group which may be substituted by a hydroxyl group at the alkyl or alkylene moiety, an N-(C1-C6 alkyl)-N-(aroyl)amino group which may be substituted by a hydroxyl group at the alkyl moiety, a C4-C7 cyclic imino group which may be substituted by a hydroxyl group at the alkylene moiety, a carboxyl group, a C1-C6 alkoxycarbonyl group, a formyl group, a C2-C6 alkanoyl group, an aroyl group, or a C1-C6 alkyl group, C3-C8 cycloalkyl group, C3-C8 cycloalkyl C1-C6 alkyl group, C2-C6 alkenyl group or C2-C6 alkynyl group which may be substituted by 1 to 3 substituents selected from the group consisting of a - 248 - hydroxyl group, an amino group, a C1-C6 alkoxy group and a mono- or di- C1-C6 alkylamino group, and when the heteroaromatic ring includes one or more nitrogen atoms, the nitrogen atom(s) may be oxidized to form an N-oxide group); or a pharmaceutically acceptable salt thereof.
Dérivé de cyclopentène de formule générale (I), et sel pharmaceutiquement acceptable dudit dérivé, dans laquelle Ar<1> et Ar<2> représentent chacun indépendamment phényle, thiényle, pyridyle, indolyle, benzofuranyle ou dihydrobenzofuranyle; A représente un groupe qui est combiné avec la double liaison carbone-carbone adjacente pour former un cycle hétéroaromatique à 5 ou 6 éléments, contenant un à quatre hétéroatomes choisis dans le groupe constitué d'azote, oxygène et soufre, et Y représente CO-R<4>, SO3H, PO3H2, tétrazol-5-yle, 2-oxo-3H-1,2,3,5,-oxathiadiazol-4-yle ou 5-oxo-4H-1,2,4-oxadiazol-3-yle.
Hayama Takashi
Ihara Masaki
Ishikawa Kiyofumi
Mase Toshiaki
Nagase Toshio
Banyu Pharmaceutical Co. Ltd.
Msd K.k.
Smart & Biggar
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