Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by
wherein Z represents an optionally substituted tetrahydropyridinyl substituent, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.
Abstract: Novel substituted amino acids of formula
are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
Type:
Grant
Filed:
August 16, 2000
Date of Patent:
November 13, 2001
Assignee:
Warner-Lambert Company
Inventors:
Justin Stephen Bryans, David Christopher Horwell, Jean-Marie Receveur
Abstract: A mixture is made of a plurality of different titanyltetraazaporphyrin compounds, each of which is represented by formula (1):
wherein A, B, C and D are each independently an unsubstituted or substituted benzene ring or pyridine ring, a substituent thereof being selected from the group consisting of nitro group, cyano group, a halogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxyl group having 1 to 8 carbon atoms, and an aryl group. The above-mentioned mixture is contained in a photoconductive layer of an electrophotographic photoconductor as a photoconductive material.
Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by
wherein Z represents cyclobutyl or pyrrolidin-1-yl, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.
Type:
Grant
Filed:
June 28, 2000
Date of Patent:
October 16, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Timothy Harrison, Andrew Madin, Martin Richard Teall
Abstract: A nitro group-containing hexaazaisowurtzitane derivative represented by the following general formula (I):
W An N(6−n) (I)
wherein n is an integer of 4 or 5, A is an acyl group having 1-10 carbon atoms with each acyl group being the same as or different from one or more of the others, N is a nitro group and W is a hexavalent hexaazaisowurtzitane residue represented by the following formula (II):
a nitroso group-containing hexaazaisowurtzitane derivative represented by the following general formula (III):
W An NS(6−n) (III)
wherein n is an integer of 4 or 5, A is an acyl group having 1-10 carbon atoms with each acyl group being the same as or different from one or more of the others, NS is a nitroso group and W is a hexavalent hexaazaisowurtzitane residue of formula (II) above, and an acyl group-containing hexaazaisowurtzitane derivative represented by the following general formula (IV):
W Am H(6−m) (IV)
wherein N is an integer of 4-6,
Abstract: The present invention provides for aminoaryl oxazolidinone N-oxide compounds of Formula I
wherein the variables are as defined herein. These compounds are exceedingly water soluble which is useful in preparing pharmaceutical formulations of these compounds. They are also rapidly converted back to the parent amines in vivo, making them useful as prodrugs of the parent amines. They are effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp., and in organisms such as Mycoplasma spp.