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Class 546/138 - Quinolizines (including hydrogenated)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system has the following
No. of patents: 115
Last issue date: 08/19/2008


1      
NumberTitleIssue Date
7414056Pyrazole-amide compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6
08/19/2008
7390810Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6
06/24/2008
72237734-oxoquinolizine antibacterial agent having 2-pyridone skeleton as partial structure
The present invention provides a 4-oxoquinolizine antibacterial agent having a 2-pyridone skeleton as a partial structure and also having a strong antibacterial effect on gram-positive bacteria, gram-negative bacteria or anaerobic bacteria. The compound having the f...
05/29/2007
7148008Methods for predicting drug sensitivity in patients afflicted with an inflammatory disease
Methods are disclosed for predicting the efficacy of a drug for treating an inflammatory disease in a human patient, including: obtaining a sample of cells from the patient; obtaining a gene expression profile of the sample in the absence and presence of in vitro mo...
12/12/2006
7125863Inhibitors of dipeptidyl peptidase IV
Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of t...
10/24/2006
7091352Compounds substituted with bicyclic amino groups
Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof: wherein A is furan, thiophene, pyrazole, imidazole, isoxazole or isothiazole; R1 is a sub...
08/15/2006
6962917Aminopiperidine quinolines and their azaisosteric analogues with antibacterical activity
Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man. ...
11/08/2005
69193712,6-substituted chroman derivatives useful as beta-3 adrenoreceptor agonists
This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions. ...
07/19/2005
6900224Antimicrobial quinolones, their compositions and uses
Compounds of the following formula: are effective antimicrobial agents. ...
05/31/2005
6900322Method for stereochemically controlled production of isomerically pure highly substituted azacyclic compounds
A method for stereochemically controlled production of azacyclic compounds of general formula (I) in which the substituents have the meanings given in the specification. The invention also relates to intermediate produ...
05/31/2005
6884806Bicyclic lactam derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
The present application describes novel bicyclic lactam derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein A, B, C, D, R1, and R2 are defined in the present speci...
04/26/2005
6841559Pyridinones to treat and prevent bacterial infections
Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselectiv...
01/11/2005
6762181Aminomethylpyrrolidine derivatives having aromatic substituents
This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of th...
07/13/2004
6743817Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists...
06/01/2004
6632825Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula: ##STR1## where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containi...
10/14/2003
6630488Quinolizinones as integrin inhibitors
The present invention is directed towards novel compounds that are effective inhibitors of integrins, particularly ଱IIbଲ.sub.3 or ଱v integrins such as ଱vଲ.sub.3 and ଱vଲ.sub.5....
10/07/2003
6608079Indole derivatives and their use as 5-HT1F agonists
The present invention relates to a compound of formula (I), or a pharmaceutical acid addition salt thereof, which are useful for activating 5-HT1F receptors and inhibiting neuronal protein extravasation in a mammal. ##STR1##...
08/19/2003
6602882Quinoline derivatives and their use as antibacterial agents
Piperidine derivatives and pharmaceutical derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man....
08/05/2003
6569871Substituted imidazole compounds
Novel 1,4,5 substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors....
05/27/2003
65628093-bicycloindole compounds
Described herein are compounds selective for a 5-HT1D receptor, which have the general formula: ##STR1##...
05/13/2003
65250664-oxoquinolizine antimicrobial having 2-pyridone skeleton as partial structure
A compound represented by the following Formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R1 represents a hydrogen atom or a carboxyl-protecting group, R2 represents a hydrogen atom, a halogen atom, a lower alkyl...
02/25/2003
65182661- Aryl-3-thioalkyl pyrazoles, the synthesis thereof and the use thereof as insecticides
The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I: ##STR1## or a salt thereof, where R1 represents R5 O, R5 SO2, R5...
02/11/2003
6509349Antimicrobial 2-pyridones, their compositions and uses
Compounds having the general structure: ##STR1## are effective antimicrobial agents....
01/21/2003
6458950Compounds and pharmaceutical compositions containing the same
A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen,...
10/01/2002
6294560Synthesis of clasto-lactacystin ଲ-lactone and analogs thereof
The present invention is directed to an improved synthesis of clasto-lactacystin-ଲ-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies u...
09/25/2001
6251893Bicyclic piperidine and piperazine compounds having 5-HT6 receptor affinity
Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula: ##STR1## wherein R1, R2, R3 and R4 are independently selected from the group consisting of H, halo,...
06/26/2001
6235751Quinolizine carboxylic acid derivatives
A quinolizine carboxylic acid derivative of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R1 and R2 have the same meanings the as defined in the specification....
05/22/2001
6177445Substituted isoquinolines as ultra short acting neuromuscular blockers
Ultra short acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein q and t are independently from 0 to 4;...
01/23/2001
6169181Compounds useful to treat retroviral infections
The present invention relates to compounds of formula I and II which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian c...
01/02/2001
61332905-HT1F agonists
The present invention relates to a compound of formula I: ##STR1## or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT1F receptors and inhibiting neuronal protein extravasation in a mammal....
10/17/2000
6121281Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use
Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof, in which R1 is vinyl or ethyl; and R2 is a group R3, R4 CH2 --, or R5 R6 C.dbd.CH--; wherein ...
09/19/2000
6025371Solid phase and combinatorial library syntheses of fused 2,4-pyrimidinediones
The invention provides chemistry libraries containing fused 2,4-pyrimidinediones. The invention also provides methods for the construction of fused 2,4-pyrimidinedione containing libraries. The invention further provides methods for the identification of ...
02/15/2000
5977133Pyridone antibiotic with improved safety profile
Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infection...
11/02/1999
5955491Method for treating osteoporosis
The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R2 and R...
09/21/1999
5874427Substituted heteroaromatic 5-HT1F agonists
This invention provides novel 5-HT1F agonists of the Formula ##STR1## in which X, Y, E, R, A, B, and n are as defined in the specification, which are useful for the treatment of migraine and associated disorders....
02/23/1999
58721171,2-ethanediol derivative and salt thereof, process for producing the same, and cerebral function-improving agent comprising the same
This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebro...
02/16/1999
5844102Glycohydrolase inhibitors, their preparation and use thereof
A compound of the formula ##STR1## wherein n, m, and p, which may be the same or different, are a number between 0 and 5; q is a number between 0 and 10; R1, R2 R3 R4 and R5, which may be the sam...
12/01/1998
58344995-HT3 receptor agonist, novel thiazole derivative and intermediate thereof
A 5-HT3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic...
11/10/1998
5789591Process for preparing 1-substituted 8-chloro-7-fluoro-9-methyl-4-oxo-4H-quinolizine-3-carboxylic acid ethyl ester compounds
A process for preparing a compound having the formula: ##STR1## wherein R is selected from the group consisting of C3 -C6 -cycloalkyl, C3 -C6 -cycloalkylmethyl, C1 -C6 -alkyl, allyl an...
08/04/1998
5786372Heteroaryl compounds used as pharmaceuticals
Compounds of formula (I), or pharmaceutically acceptable salts thereof are provided: ##STR1## in which X1 --(CH2)x --X2 forms a 5-7 membered ring wherein: X1 is O or S; X2 is O, S or N...
07/28/1998
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