Substituted N-phenyl-bipyrrolidine carboxamides and therapeutic use thereof

A pharmaceutical composition comprising a compound of formula (I):

• wherein
• R, R1, R2 and R3 are the same or different and independently of each other chosen from hydrogen, (C1-C4)alkyl or CF3;
• R4 is selected from the group consisting of dimethylaminomethyl, methanesulfonylmethyl, phenoxymethyl, vinylbenzene, ethynylbenzene, vinylpyridine, phenyl, benzofuranyl, dihydro-benzofuranyl, oxo-tetrahydro-benzofuranyl, benzodioxolyl, oxo-chromenyl, dihydrobenzo-dioxinyl, dioxo-tetrahydro-1H-benzo[e]diazepinyl, imidazopyridinyl, benzotriazolyl, benzoimidazolyl, oxo-dihydro-benzoimidazolyl, indolyl, indazolyl, naphthyridinyl, quinolinyl, benzoimidazothiazolyl, pyridinyl, pyrimidinyl, pyrrolyl, triazolyl, thienyl, thiazolyl, tetrahydrofuranyl or pyrrolidinyl;
• wherein said R4 is optionally substituted one or more times with a substituent selected from halogen, methyl, ethyl, isopropyl, propoxyethyl, phenyl, benzoyl, difluoromethoxy, CF3, CN, acetyl, methanesulfonyl, sulfamoyl, dimethylamino, N-formyl-methylamino, 2-hydroxyethylamino, 2-methoxyethylamido, benzyloxymethyl, carboxyphenoxy, pyrazolyl, 3,5-dimethyl-pyrazolyl, imidazolyl, triazolyl, oxazolyl, pyridinyl, oxo-dihydro-pyridinyl, pyrimidinyl-methylamino, N-acetyl-piperidinyl, morpholinyl, morpholinylmethyl or 2-oxo-pyrrolidinyl;
• or
• a pharmaceutically acceptable salt thereof or an enantiomer or a diastereomer thereof in combination with at least one pharmaceutically acceptable excipient, diluent or a carrier.

A method of inhibiting or relieving a disease in a patient, said disease selected from the group consisting of a sleep related disorder selected from the group consisting of narcolepsy, circadian rhythm sleep disorder, obstructive sleep apnea, periodic limb movement and restless leg syndrome, excessive sleepiness and drowsiness due to medication side-effect, dementia, Alzheimer's disease, multiple sclerosis, attention deficit hyperactivity disorder and depression, comprising administering to said patient a therapeutically effective amount of a compound of formula (I):

• wherein
• R, R1, R2 and R3 are the same or different and independently of each other chosen from hydrogen, (C1-C4)alkyl or CF3;
• R4 is selected from the group consisting of dimethylaminomethyl, methanesulfonylmethyl, phenoxymethyl, vinylbenzene, ethynylbenzene, vinylpyridine, phenyl, benzofuranyl, dihydro-benzofuranyl, oxo-tetrahydro-benzofuranyl, benzodioxolyl, oxo-chromenyl, dihydrobenzo-dioxinyl, dioxo-tetrahydro-1H-benzo[e]diazepinyl, imidazopyridinyl, benzotriazolyl, benzoimidazolyl, oxo-dihydro-benzoimidazolyl, indolyl, indazolyl, naphthyridinyl, quinolinyl, benzoimidazothiazolyl, pyridinyl, pyrimidinyl, pyrrolyl, triazolyl, thienyl, thiazolyl, tetrahydrofuranyl or pyrrolidinyl;
• wherein said R4 is optionally substituted one or more times with a substituent selected from halogen, methyl, ethyl, isopropyl, propoxyethyl, phenyl, benzoyl, difluoromethoxy, CF3, CN, acetyl, methanesulfonyl, sulfamoyl, dimethylamino, N-formyl-methylamino, 2-hydroxyethylamino, 2-methoxyethylamido, benzyloxymethyl, carboxyphenoxy, pyrazolyl, 3,5-dimethyl-pyrazolyl, imidazolyl, triazolyl, oxazolyl, pyridinyl, oxo-dihydro-pyridinyl, pyrimidinyl-methylamino, N-acetyl-piperidinyl, morpholinyl, morpholinylmethyl or 2-oxo-pyrrolidinyl;
• or
• a pharmaceutically acceptable salt thereof or an enantiomer or a diastereomer thereof in combination with at least one pharmaceutically acceptable excipient, diluent or a carrier.