Patent number: 6787522
Abstract: Compounds of formula (I) are antibacterials:
wherein:
R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, an
Type:
Grant
Filed:
April 30, 2002
Date of Patent:
September 7, 2004
Assignee:
British Biotech Pharmaceuticals
Inventors:
Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
Patent number: 6537989
Abstract: The present invention relates to azadioxacycloalkenes of the formula I
in which the substituents R1 to R5 and X, the index n and the bridge member W have the following meanings:
R1 is C1-C4-alkyl, halogen, C1-C4-haloalkyl, C3-C6-cycloalkyl;
R2 is C1-C4-alkyl, C1-C4-haloalkyl, C3-C4-alkenyl, C3-C4-haloalkenyl, C3-C4-alkynyl or C3-C4-haloalkynyl;
R3 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl or unsubstituted or substituted phenyl;
R4 is ═CRaRb, —CRd═CRaRb or ═N—ORc, where Ra, Rb, Rc and Rd are each as defined in claim 1;
R5 is nitro, cyano, halogen, C1-C6-alkyl or, in the case that n is 2, additionally a bridge which is attached to two adjacent ring atoms;
n is 0, 1, 2, 3 or 4, where the substituents R1 may be different if n is greater than 1;
X is C1-C4-alkoxy-N═, C1-C4-alkoxy-CH═ or R6—CH═, where R6 is as defined in claim 1
W is unsubstituted or substituted C1-C3-alkylene.
Type:
Grant
Filed:
April 2, 2001
Date of Patent:
March 25, 2003
Assignee:
BASF Aktiengesellschaft
Inventors:
Markus Gewehr, Wassilios Grammenos, Hubert Sauter, Herbert Bayer, Andreas Gypser, Bernd Müller, Arne Ptock, Oliver Cullmann, Thomas Grote, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Volker Harries
Publication number: 20030050309
Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
Type:
Application
Filed:
September 12, 2001
Publication date:
March 13, 2003
Inventors:
Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike Radeke, Fengjiang Wang, Liming Shao
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