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US 7,888,503 B2Granted
Benzodiazepine derivatives that inhibit rock
AssigneeGlaxoSmithKline LLC
InventorsMichael John Alberti, David Kendall Jung
Life of this patent
Estimating the term…
Abstract
The present invention relates to dihydrobenzodiazepine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dihydrobenzodiazepine derivatives are useful in the treatment of diseases associated with inappropriate ROCK kinase.
Claims8
A compound of Formula (I):
- wherein
- the dotted line represents a bond or is absent;
- R1 represents pyrazolyl, pyridinyl, pyrimidinyl optionally substituted by NH2, or indazolyl;
- R2 represents phenyl optionally substituted by one or more substituents selected from C1-6 alkyl, CN, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, NO2, halogen;
- or a 5-membered heteroaryl group containing one or more heteroatoms selected from O, N or S optionally substituted by a 5-membered heteroaryl group;
- R3 and R4 independently represent H or C1-6 alkyl;
- or a salt thereof.
4 more elements
A compound selected from the group consisting of:
- Structure
- Name
- 5-(2-fluorophenyl)-7-(4-pyridinyl)-2,3-dihydro-1H-1,4- benzodiazepine
- 5-(2-fluorophenyl)-7-(4-pyridinyl )-2,3,4,5-tetrahydro- 1H-1,4-benzodiazepine
- (3S)-5-(2-fluorophenyl)-3-methyl-7-(4-pyridinyl)-2,3- dihydro-1H-1,4-benzodiazepine
- 7-(4-pyridinyl)-5-(3-thienyl)-2,3-dihydro-1H-1,4- benzodiazepine
- 5-(2,2′-bithien-5-yl)-7-(4-pyridinyl)-2,3-dihydro-1H- 1,4-benzodiazepine
- 7-(4-pyridinyl)-2,3-dihydro-1H-1,4-benzodiazepine
- 5-(3-nitrophenyl)-7-(4-pyridinyl)-2,3-dihydro-1H-1,4- benzodiazepine
- 5-[3-(methyloxy)phenyl]-7-(4-pyridinyl)-2,3-dihydro- 1H-1,4-benzo-diazepine
- 5-phenyl-7-(4-pyridinyl)-2,3-dihydro-1H-1,4- benzodiazepine
- 7-(4-pyridinyl)-5-[2-(trifluoromethyl)phenyl]-2,3- dihydro-1H-1,4-benzodiazepine
- 5-(2-nitrophenyl)-7-(4-pyridinyl)-2,3-dihydro-1H-1,4- benzodiazepine
- -(5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-7-yl)-2- pyrimidinamine
- 5-phenyl-7-(1H-pyrazol-4-yl)-2,3-dihydro-1H-1,4- benzodiazepine
- [2-fluoro-5-(1H-indazol-5- yl)phenyl](phenyl)methanone
- 4-[7-(4-pyridinyl)-2,3-dihydro-1H-1,4-benzodiazepin- 5-yl]benzonitrile
- 5-(4-chlorophenyl)-7-(4-pyridinyl)-2,3-dihydro-1H-1,4- benzodiazepine
- and salts thereof.
16 more elements
A compound of Formula (I):
- wherein
- the dotted line represents a bond or is absent;
- R1 represents pyrazolyl, pyridinyl optionally substituted by halo, pyrimidinyl optionally substituted by NH2, or indazolyl;
- R2 represents phenyl optionally substituted by one or more substituents selected from C1-6 alkyl, CN, C1-6 alkoxy, C1-6 haloalkyl, C1-6 haloalkoxy, NO2, halogen;
- or a 5-membered heteroaryl group containing one or more heteroatoms selected from O, N or S optionally substituted by a 5-membered heteroaryl group;
- R3 and R4 independently represent H or C1-6 alkyl;
- or a salt or thereof.
4 more elements
The compound:
- 7-(3-fluoropyridin-4-yl)-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepine
- or a salt thereof.
Dependencies are inferred from the claim text.