Hydroisoindoline tachykinin receptor antagonists
AssigneeMerck Sharp & Dohme Corp.
InventorsJinlong Jiang, Robert J. DeVita, Sanjeev Kumar, Sander G. Mills, Richard A. Tschirret-Guth
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Abstract
The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
Claims9
A compound of the formula I:
- wherein:
- R1 is selected from the group consisting of:
- (1) hydrogen,
- (2) C1-6alkyl, which is unsubstituted or substituted with halogen, hydroxyl or phenyl,
- (3) cyclopentenone, which is unsubstituted or substituted with hydroxyl or methyl,
- (4) —(CO)—C1-6alkyl,
- (5) —(CO)—NH2,
- (6) —(CO)—NHC1-6alkyl, and
- (7) —(CO)—N(C1-6alkyl)(C1-6alkyl);
- X is independently selected from the group consisting of:
- (1) hydrogen,
- (2) fluorine, and
- (3) methyl;
- and pharmaceutically acceptable salts thereof and individual enantiomers and diastereomers thereof.
A compound which is selected from the group consisting of:
A compound of Formula A
- Wherein R1 and X are defined as follows:
- Ex. #
- R1
- X
- 5
- 4-F
- 6
- H
- 7
- 2-Me
- 8
- 4-F
- 9
- 2-Me
- 10
- 2-Me
- 11
- 4-F
- 12
- 2-Me
- 13
- 2-Me
- 14
- 4-F
- 15
- 2-Me, 4-F
- 16
- 2-Me, 4-F
- 17
- 2-Me, 4-F
- 18
- 2-Me, 4-F
- 19
- 2-Me, 4-F
- 20
- 4-F
- 21
- 2-Me
- 22
- 2-Me, 4-F
- 23
- 4-F
- 24
- 2-Me
- 25
- 2-Me, 4-F
- 26
- 4-F
- 27
- 2-Me
- 28
- 2-Me, 4-F
- 29
- 4-F
- 30
- 2-Me
- 31
- 2-Me, 4-F
- 32
- 4-F
- 33
- 2-Me
- 34
- 2-Me, 4-F
- 35
- 4-F
- 36
- 2-Me
- 37
- 2-Me, 4-F
- 38
- 2-Me
- 39
- 2-Me, 4-F
- 40
- 4-F
- 41
- 2-Me
- 42
- 2-Me, 4-F
- 43
- 4-F
- 44
- 2-Me
- 45
- 2-Me, 4-F
- or a pharmaceutically acceptable salt thereof;
- B
- Ex. #
- R1
- X
- 46
- 4-F
- 47
- H
- 48
- 2-Me
- 49
- 4-F
- 50
- 2-Me
- 51
- 2-Me
- 52
- 4-F
- 53
- 2-Me
- 54
- 2-Me
- g 55
- 4-F
- 56
- 2-Me, 4-F
- 57
- 2-Me, 4-F
- 58
- 2-Me, 4-F
- 59
- 2-Me, 4-F
- 60
- 4-F
- 61
- 2-Me, 4-F
- 62
- 4-F
- 63
- 2-Me
- 64
- 2-Me, 4-F
- 65
- 4-F
- 66
- 2-Me
- 67
- 2-Me, 4-F
- 68
- 4-F
- 69
- 2-Me
- 70
- 2-Me, 4-F
- 71
- 4-F
- 72
- 2-Me
- 73
- 2-Me, 4-F
- 74
- 4-F
- 75
- 2-Me
- 76
- 2-Me, 4-F
- 77
- 4-F
- 78
- 2-Me
- 79
- 2-Me, 4-F
- 80
- 2-Me
- 81
- 2-Me, 4-F
- 82
- 4-F
- 83
- 2-Me
- 84
- 2-Me, 4-F
- 85
- 4-F
- 86
- 2-Me
- 87
- 2-Me, 4-F
- or a pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.