Method for treating conditions related to the glutamate receptor using carboxylic acid amide derivatives
AssigneeHoffmann-La Roche Inc.
InventorsVincent Mutel, Eric Vieira, Juergen Wichmann
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AssigneeHoffmann-La Roche Inc.
InventorsVincent Mutel, Eric Vieira, Juergen Wichmann
Estimating the term…
The present invention is concerned with the use of carbonylamino derivatives of the formula wherein R signifies lower alkyl, lower alkenyl, lower alkinyl, cycloalkyl, lower alkoxy or CF3; R1 signifies hydrogen or lower alkyl; R2 and R3 signify, independently from each other, hydrogen, halogen or nitro; Y signifies CH or N; n is 0-6; m is 0-2; as well as with their pharmaceutically acceptable salts for the treatment of diseases, which relate to metabotropic glutamate receptor antagonists and/or agonists.
A pharmaceutical composition which comprises a compound of the formula
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In the central nervous system (CNS) the transmission of stimuli takes place by the interaction of a neurotransmitter, which is sent out by a neuron, with a neuroreceptor.
L-glutamic acid, the most commonly occurring neurotransmitter in the CNS, plays a critical role in a large number of physiological processes. The glutamate-dependent stimulus receptors are divided into two main groups. The first main group forms ligand-controlled ion channels. The metabotropic glutamate receptors (mGluR) belong to the second main group and, furthermore, belong to the family of G-protein-coupled receptors.
At present, eight different members of these mGluRs' are known and of these some even have sub-types. On the basis of structural parameters, the different second messager signalling pathways and the different affinity to low-molecular weight chemical compounds, these eight receptors can be sub-divided into three sub-groups:
N -Pentyl-2,2-diphenyl-acetamide
To a cooled (0° C.) solution diphenylacetyl chloride (1.73 mmol) and pyridine (0.28 ml, 3.46 mmol) in dichloromethane (12 ml) was added pentylamine (0.39 ml, 2.60 mmol) and the reaction mixture was stirred at RT for 16 h. Aqueous work up and crystallization from ethyl acetate/hexane yielded the product as a light yellow solid, m.p. 101° C. and MS: m/e=281 (M+).
2,2-Diphenyl-N-propyl-acetamide
Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals: amides
Amides, e.g. hydroxamic acids: having aromatic rings, e.g. colchicine, atenolol, progabide
Drugs for disorders of the alimentary tract or the digestive system: for nausea, cinetosis or vertigo; Antiemetics
Drugs for disorders of the cardiovascular system
Term ended 6 Oct 2020 (estimated)
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