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US 2009/0275571 A1Published application
Morpholinyl and pyrrolidinyl analogs
AssigneeSmithKline Beecham Corporation
InventorsKrista B. Goodman, Michael J. Neeb, Clark A. Sehon, Andrew Q. Viet, Gren Z. Wang
Life of this patent
Estimating the term…
Abstract
The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
Claims11
A compound of Formula (I):
- wherein
- R1 is:
- A is (CH2)n;
- n is 1 or 2;
- the group (a) may be unsubstituted or substituted by one, two, or three substituents chosen from:
- halo, OC1-3 alkyl, OH, CN, C(O)OH, NR7R8, OCF3, C(O)NR9R10, SO2C1-3 alkyl, SO2C3-6 cycloalkyl, SO2-phenyl, SO2NR9R10, CF3, and NO2;
- R2 is hydrogen, halo, OC1-3 alkyl, NHC(O)C1-3 alkyl, NHSO2C1-3alkyl, NHSO2-phenyl, NHC(O)C3-6 cycloalkyl, or NHC(O)-phenyl;
- R3 is C1-3 alkyl or C3-6 cycloalkyl;
- R4, R5, and R6 are independently hydrogen or CH3;
- R7 and R8 are independently hydrogen, C(O)C1-3 alkyl, C(O)C3-6 cycloalkyl, C(O)-phenyl,
- C1-6 alkyl, phenyl, SO2C1-3 alkyl, SO2C3-6 cycloalkyl, SO2-phenyl, or C(O)NHC1-3 alkyl;
- R9 and R10 are independently hydrogen, C1-3 alkyl, C3-6 cycloalkyl, phenyl;
- or taken together R9 and R10 may form a 5 to 7 member ring optionally containing one or two heteroatoms chosen from O, N, and S;
- X is O or a bond;
- B is:
- R12 is hydrogen, C1-3 alkyl, CH2CN, (CH2)m(O)CH3, CH2C(O)NH2, or (CH2)mOH;
- R13 is hydrogen, halo, C1-3 alkyl, CF3, or OC1-3 alkyl;
- m is 2 or 3;
- R14 is hydrogen, halo, C1-3 alkyl, OC1-3 alkyl, OCF3, CF3, C(O)NR15R16, or C(O)OC1-3 alkyl;
- and
- R15 and R16 are independently hydrogen, C1-3 alkyl, C3-6 cycloalkyl, or phenyl;
- or a pharmaceutically acceptable salt thereof.
19 more elements
-8. (canceled)
Dependencies are inferred from the claim text.