Patent NZ-589840-A (NZ)
Title: Novel derivatives of (bridged piperazinyl)-1-alkanone and use thereof as p75 inhibitors
Inventor: BARONI MARCO
IPC: A61K31/529
Filed: 2009-06-12
Abstract: The present invention relates to «phenyl)·3,6·dihydropyridin·1·5 yl)(bridged piperazinyl)·1-alkanone derivatives and «phenyl)-2,5-dihydropyrrol-1-yl) (bridged piperazinyl)-1-alkanone derivatives [compounds of formula (I)], to the preparation thereof and to the therapeutic use thereof. The invention also provides a compound of the invention, for the preparation of a medicament for use in the prevention or treatment of central and peripheral neurodegenerative diseases, senile dementia, epilepsy, Alzheimer's disease, Parkinson's disease, Huntington's chorea, Down's syndrome, prion diseases, amnesia, schizophrenia, depression, bipolar disorder, amyotrophic lateral sclerosis, multiple sclerosis, cardiovascular conditions, post-ischaemic cardiac damage, cardiomyopathies, myocardial infarction, heart failure, cardiac ischaemia, cerebral infarction; peripheral neuropathies, damage to the optic nerve and to the retina, retinal pigment degeneration, glaucoma, retinal ischaemia, macular degeneration, spinal chord traumas, cranial traumas, atherosclerosis; stenoses, healing disorders, alopecia, cancers, tumours, metastases, leukaemias, respiratory disorders, pulmonary inflammation, allergy, asthma, chronic obstructive pulmonary disease, cutaneous pain, somatic pain, visceral pain, and neurological pain, chronic neuropathic and inflammatory pain, autoimmune diseases, rheumatoid arthritis, ankylosing spondylarthritis, psoriatic arthritis, plaque psoriasis, bone fractures, bone diseases and osteoporosis. The invention also relates to a use of a compound of the invention, or an acid addition salt thereof, in the preparation of a medicament for use in the prevention or treatment of central and peripheral neurodegenerative diseases, senile dementia, epilepsy, Alzheimer's disease, Parkinson's disease, Huntington's chorea, Down's syndrome, prion diseases, amnesia, schizophrenia, depression, bipolar disorder, amyotrophic lateral sclerosis, multiple sclerosis, cardiovascular conditions, post-ischaemic cardiac damage, cardiomyopathies, myocardial infarction, heart failure, cardiac ischaemia, cerebral infarction; peripheral neuropathies, damage to the optic nerve and to the retina, retinal pigment degeneration, glaucoma, retinal ischaemia, macular degeneration, spinal chord traumas, cranial traumas, atherosclerosis; stenoses, healing disorders, alopecia, cancers, tumours, metastases, leukaemias, respiratory disorders, pulmonary inflammation, allergy, asthma, chronic obstructive pulmonary disease, cutaneous pain, somatic pain, visceral pain, and neurological pain, chronic neuropathic and inflammatory pain, autoimmune diseases, rheumatoid arthritis, ankylosing spondylarthritis, psoriatic arthritis, plaque psoriasis, bone fractures, bone diseases and osteoporosis. Examples include 1-[4-(3-trifluoromethylphenyl)-3,6-dihydro-2H- pyridin-1-yl]-2-[8-(5-trifluoromethylpyridin-2-yl)-3 ,8-d iazabicyclo[3.2.1 } oct-3-yl]ethanone and 1-[4-(4-chlorophenyl)-3,6,-dihydro-2H-pyridin-1-yl]-2-5 (8-pyrimidin-2-yl-3,8-diazabicyclo[3.2.1 Joct-3-yl)ethanone and 1-[4-(4-chloro-3-trifluoromethylphenyl)-3,6-dihydro-2 H-pyridin-1-yl]-2 -[5-(5-trifluoromethyl pyridin-2 -yl )-2,5-diazarncyclo[2.2.1]hept-2-yl]ethanone