Back to results
US 6,887,864 B2Granted
Azepane derivatives
AssigneeHoffmann-La Roche Inc.
InventorsWalter-Gunar Friebe, Birgit Masjost, Ralf Schumacher
Life of this patent
Estimating the term…
Abstract
This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I) wherein the symbols are defined in the specification, as well as processes for their manufacture. The compounds according to this invention possess anti-cell proliferation activity and show an increased plasma-stability.
Claims15
A compound of formula (I)
- wherein
- A is a non-aromatic, 3 to 7 carbon atom, mono-or bicyclic carbocyclic group or a non-aromatic, 3 to 7 membered, mono- or bicyclic heterocyclic group having one or two heteroatoms chosen from nitrogen, oxygen or sulfur, said groups being substituted by 1, 2, or 3 substituents selected from halogen, alkyl, trifluoromethyl, hydroxy, alkoxy, aryl, hetaryl, arylalkyl, arylalkyloxy, aryloxy, alkylenedioxy, nitro, amino, alkylamino, dialkylamino, alkanoylamino or acyl or unsubstituted and optionally annulated by an aryl or hetaryl group or A is an aryl or hetaryl group said hetaryl groups having one or two hetero atoms chosen from nitrogen, oxygen or sulfur;
- B is a phenyl ring which may be unsubstituted or substituted by 1, 2 or 3 substituents independently selected from a halogen atom, an (1-4C)alkyl, trifluoromethyl, hydroxy, (1-4C)alkoxy, nitro, amino, amino(1-4C)alkyl, (1-4C)alkylamino, di[(1-4C)alkyl]amino, (1-4C)alkanoylamino, (1-4C)alkylthio, (1-4C)alkoxycarbonyl, a (1-3C)alkylenedioxy, an acyl selected from formyl, acetyl, propionyl, benzoyl or phenylacetyl, a non-aromatic, 3 to 7 carbon atom, mono- or bicyclic carbocyclic group or a non-aromatic, 3 to 7 membered, mono- or bicyclic heterocyclic group having one or two heteroatoms, said groups being substituted or unsubstituted and optionally annulated by a non-aromatic, 3 to 7 carbon atom, mono- or bicyclic, substituted or unsubstituted carbocyclic group or by a non-aromatic, 3 to 7 membered, mono- or bicyclic, substituted or unsubstituted heterocyclic group having one or two heteroatoms, or
- a non-aromatic, 3 to 7 membered, mono- or bicyclic, substituted or unsubstituted heterocyclic group having one or two heteroatoms,
- (R1)n is the same or different halogen atom, a (1-4C)alkyl-, or a (1-4C)alkoxy-group, and n=0-4;
- its stereoisomers, enantiomers or racemates;
- or a pharmaceutically acceptable salt thereof.
4 more elements
A compound of formula (IV)
- wherein A′ is a non-aromatic, 3 to 7 carbon atom, mono- or bicyclic, substituted or unsubstituted carbocyclic group or a non-aromatic, 3 to 7 membered, mono- or bicyclic, substituted or unsubstituted heterocyclic group having one or two heteroatoms or A′ is an aryl or hetaryl group having one or two hetero atoms selected from nitrogen, oxygen or sulfur and R2 is a protecting group selected from t-butoxycarbonyl or methoxymethyl,
- or a pharmaceutically acceptable salt thereof.
A compound of formula (V)
- wherein A′ is a non-aromatic, 3 to 7 carbon atom, mono- or bicyclic, substituted or unsubstituted carbocyclic group or a non-aromatic, 3 to 7 membered, mono- or bicyclic, substituted or unsubstituted heterocyclic group having one or two heteroatoms or A′ is an aryl or hetaryl group having one or two hetero atoms selected from nitrogen, oxygen or sulfur and R2 is a protecting group selected from t-butoxycarbonyl or methoxymethyl,
- or a pharmaceutically acceptable salt thereof.
A compound of formula (VI)
- wherein A′ is a non-aromatic, 3 to 7 carbon atom, mono-or bicyclic, substituted or unsubstituted carbocyclic group or a non-aromatic, 3 to 7 membered, mono- or bicyclic, substituted or unsubstituted heterocyclic group having one or two heteroatoms or A′ is an aryl or hetaryl group having one or two hetero atoms selected from nitrogen, oxygen or sulfur and R2 is a protecting group selected from t-butoxycarbonyl or methoxymethyl,
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.