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US 6,476,028 B1Granted
Compounds and methods
AssigneeSmithKline Beecham Corporation
InventorsWilliam E. Bondinell, James Chan, Roderick A. Porter, Joseph W. Venslavsky, Steven Dabbs, David T. Davies
Life of this patent
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Abstract
A method of treating a CCR5-mediated disease state in mammals which comprises administering to a mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
Claims7
A method of treating a CCR5-mediated disease state in mammals which comprises administering to a mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof:
- wherein:
- X is hydrogen or one or more of C1-6alkyl, CONRR′, trifluoromethyl, hydroxy, C1-6alkoxy, benzyloxy, C1-6alkylthio, or halo where R and R′ are independently hydrogen or C1-6alkyl;
- R1 is hydrogen or C1-6alkyl;
- R2 is hydrogen or C1-6alkyl;
- the dotted line, . . . , indicates a single bond or a double bond;
- R3 is hydrogen or C1-6alkyl;
- A is [C(R″)2]m CR″R4R5 or [C(R″)2]nCR″=C R4R5 where each R″ is independently hydrogen or C1-6alkyl;
- m is 0-3;
- n is 1-2
- R4 is phenyl, biphenyl, naphthyl, 1-benzotriazinyl, or 2-benzotriazinyl, optionally substituted with one or more of C1-6alkyl, cyano, trifluoromethyl, NR6R7, nitro, hydroxy, C1-6alkoxy, benzyloxy, C1-6alkylthio, or halo, where R6 and R7 are independently hydrogen or C1-6alkyl;
- R5 is R′ when m is 0;
- alternatively, R5 is R″, phenyl or naphthyl when m is 1-3 or n is 1-2, wherein phenyl or naphthyl are optionally substituted with one or more of C1-6alkyl, cyano, trifluoromethyl, NR6R7, nitro, hydroxy, C1-6alkoxy, benzyloxy, C1-6alkylthio, or halo.
9 more elements
A compound selected from:
- 5-chloro-3-[1-[3-(dimethylamino)phenylmethyl]-1,2,3,6-tetrahydro-4-pyridinyl]-1H-indole;
- 3-[1-([1,1′-biphenyl]-2-ylmethyl)]-4-piperidinyl]-1H-indol-5-ol;
- 3-[1-([1,1′-biphenyl]4-ylmethyl)]-4-piperidinyl]-1H-indol-5-ol;
- 3-[1-(3,3-diphenylpropyl)4-piperidinyl]-1H-indol-5-ol;
- 3-[1-[4-(2H-benzotriazin-2-yl)butyl]-4-piperidinyl]-1H-indol-5-ol;
- 3-[1-[4-(1H-benzotriazin-1-yl)butyl]-4-piperidinyl]-1H-indol-5-ol;
- 3-[1-(4,4-diphenylbut-3-enyl)-4-piperidinyl]-1H-indol-5-ol;
- 3-[1-(3,3-diphenyl-2-propenyl)-4-piperidinyl]-1H-indol-5-ol;
- and
- 3-[1-(3,3-diphenylpropyl)-4-piperidinyl]-1H-indole.
7 more elements
Dependencies are inferred from the claim text.