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US 2002/0165241 A1Published application
N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
AssigneeMerck & Co., Inc.
InventorsChristopher F. Claiborne, John W. Butcher, David A. Claremon, Brian E. Libby, Nigel J. Liverton, Peter M. Munson, Kevin T. Nguyen, Brian Phillips, Wayne Thompson, John A. McCauley
Life of this patent
Estimating the term…
Abstract
Compounds represented by Formula (I): 1 or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
Claims52
A compound having the formula (I):
- 312
- or pharmaceutically acceptable salts thereof, wherein
- NonAr is a nonaromatic 5-7 membered ring containing 1 or 2 nitrogen ring atoms or an aza bicyclo octane ring;
- HetAr is a 5 or 6 membered heteroaromatic ring containing 1-3 nitrogen ring atoms, or isoxazolyl, thiazolyl, thiadiazolyl, quinolinyl, quinazolinyl, purinyl, pteridinyl, benzimidazolyl, pyrrolopyrimidinyl, or imidazopyridinyl;
- HetAr is optionally substituted with 1 or 2 substituents, each substituent independently is C1-4alkyl, C1-4alkoxy, C2-4alkynyl, trifluoromethyl, hydroxy, hydroxyC1-4alkyl, fluoro, chloro, bromo, iodo, cyano, methylsulfanyl, cyclopropylethynyl-, phenylethynyl-, heteroarylethynyl-,—N(C0-4alkyl)(C0-4alkyl), nitro, (C1-2alkyl)(C1-2alkyl)NCH2—, (C1-2alkyl)HNCH2—, Si(CH3)3—C—, or NH2C(O)—;
- A is —C0-4alkyl-;
- B is aryl(CH2)0-3—O—C(O), heteroaryl(CH2)1-3—O—C(O)—, indanyl(CH2)0-3—O—C(O)—, aryl(CH2)1-3—C(O)—, aryl-cyclopropyl-C(O)—, heteroaryl-cyclopropyl-C(O)—, heteroaryl(CH2)1-3—C(O)—, aryl(CH2)1-3—, heteroaryl(CH2)1-3—, aryl(CH2)1-3—NH—C(O)—, aryl(CH2)1-3—NH—C(NCN)—, aryl(CH2)1-3—SO2—, heteroaryl(CH2)1-3—SO2—, wherein any of the aryl or heteroaryl is optionally substituted by 1-5 substituents, each substituent independently is C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, trifluoromethyl, bromo, fluoro, or chloro;
- and
- X is H, OH, F, C1-4alkyl, C1-4alkoxy, NH2, or X taken with an adjacent bond is ═O.
6 more elements
Dependencies are inferred from the claim text.