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Class 544/379 - The additional hetero ring is five-membered and unsaturated (e.g., thienyl piperazines, etc.)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is five-membered
No. of patents: 292
Last issue date: 10/28/2008


1                
NumberTitleIssue Date
7442692Indanyl-piperazine compounds
A compound selected from those of formula (I): wherein: R3 represents a hydrogen atom, and R1 and R2 together with the carbon atoms carrying them form a be...
10/28/2008
7432264Antimicrobial biaryl compounds
Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain. ...
10/07/2008
7427632Factor Xa inhibitors
Compounds of formula (I) in which R1, n, Z, R3 and R4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of ...
09/23/2008
7419980Fused-aryl and heteroaryl derivatives and methods of their use
The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms...
09/02/2008
73968344(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders
Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the ma...
07/08/2008
7396944Thiophene derivatives, their manufacture and use as pharmaceutical agents
Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as we...
07/08/2008
7390812N, N'-disubstituted piperazine compounds and their use as analgesics
N,N′-disubstituted piperazine compounds, processes for the production thereof, and pharmaceutical preparations containing these compounds. The use of N,N′-disubstituted piperazine compounds for the production of pharmaceutical preparations and in related methods...
06/24/2008
7365196Sulphonamido-substituted bridged bicycloalkyl derivatives
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease. ...
04/29/2008
7351825Cyclopropane compounds and pharmaceutical use thereof
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1):
04/01/2008
7282519Nitrosated and nitrosylated diuretic compounds, compositions and methods of use
The invention describes novel nitrosated and/or nitrosylated diuretic compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated diuretic compound, and, optionally, at least one nitric oxide ...
10/16/2007
7262197Phospholipase C inhibitors for use in treating inflammatory disorders
This invention is directed to heterocyclyl-substituted anilino phospholipase C inhibitor compounds useful in treating or ameliorating an inflammatory disorders and/or restenosis of the general formula (I): and en...
08/28/2007
72299944(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain anxiety or gastrointestinal disorders
Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is indepen...
06/12/2007
7214679Piperidine/piperazine-type inhibitors of p38 kinase
Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase. ...
05/08/2007
7189725Enantiomerically pure opioid diarylmethylpiperazine as a cardioprotection agent
(−)3-((S)-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)(3-thienyl)methyl)phenol and pharmaceutically acceptable esters or salts thereof, in essentially enantiomerically pure form have utility as a cardioprotection agent. ...
03/13/2007
7173132Certain substituted 1-aryl-3-piperazine-1′-yl propanones
Disclosed are compounds of formula I: wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar...
02/06/2007
7160886Acylated piperazine derivatives as melanocortin-4 receptor agonists
Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of disease...
01/09/2007
7115607Substituted piperazinyl amides and methods of use
Selected substituted piperazine compounds of Formula I are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceuti...
10/03/2006
7084144Sulfonyl group containing compounds and their use for the treatment of erectile dysfunction
A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl ...
08/01/2006
70784074-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them
The present invention relates to 4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them. More particularly, it relates to 4-hydroxycinnamamide derivatives showing superior antioxidant activity compared to the known antioxida...
07/18/2006
7056954Means for the modulation of processes mediated by retinoid receptors and compounds useful therefor
In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which ...
06/06/2006
7034110Method of identifying chemical compounds having selected properties for a particular application
A method for obtaining compounds having selected properties for a particular application by forming base modules having at least two structural diversity elements from the reaction of a first compound having at least one structural diversity element and a first reac...
04/25/2006
6982256Tolerance of 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine in intravenous administration
The invention relates to new formulations for improving the local tolerance of intravenously administered 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine or one of the pharmacologically acceptable acid addition salts thereof. ...
01/03/2006
6936715Lipoic acid heterocyclic or benzene derivatives, preparation and use thereof as medicines
Compounds of the formulae wherein the substituents are as defined in the specification useful for inhibiting NO synthase and regenerate antioxidants. ...
08/30/2005
6924288Enantiomerically pure opioid diarylmethylpiperzine and methods of using same
An essentially pure compound of the formula: (−)3-((S)-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)(3-thienyl)methyl)phenol or a pharmaceutically acceptable salt thereof, having utility as a receptor-binding species,...
08/02/2005
6916797α-arylethylpiperazine derivatives as neurokinin antagonists
The invention relates to new α-arylethylpiperazine of the formula wherein Z represents 0 or S; n′ represents 1 or 2; R2 represents a hy...
07/12/2005
6916812Alpha-aminoamide derivatives as melanocortin agonists
Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present inven...
07/12/2005
6906072Piperazine compound and pharmaceutical composition containing the compound
The present invention provides a novel compound having a superior calcium antagonism, in particular, a neuron-selective calcium antagonism. Namely, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.
06/14/2005
6900213Bisaryl derivatives having FSH modulatory activity
The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV ...
05/31/2005
6887876Benzamidine derivatives
Benzamidine derivatives are useful delta-opioid receptor modulators, agonists useful as analgesics and antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psy...
05/03/2005
6878712Amides as inhibitors for pyruvate dehydrogenase
A compound of formula (I): wherein: Ring A is a nitrogen linked mono or bicyclic heterocyclic ring as defined within; R1 and R2 are independentl...
04/12/2005
6849660Antimicrobial biaryl compounds
Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1′ is —C(O)NR5R5′
02/01/2005
6846825Antibacterial agents
Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(═O) or the formula: —C(═O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted...
01/25/2005
6818645Benzocycloalkylenylamine derivatives as muscarinic receptor antagonists
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S, or NR4, and the other substituents are as d...
11/16/2004
6818644Substituted piperazine derivatives, the preparation thereof and their use as medicaments
The present invention relates to substituted piperazine derivatives of general formula wherein Ra, Rb, Rc Rf, Rg and m, n and X ...
11/16/2004
6784173Aromatic dicarboxylic acid derivatives
Compounds of formula I wherein A, R1 and R2 are defined in the specification. These compounds are useful as HDAC inhibitors. Also disclosed are methods of making and using said compounds. ...
08/31/2004
67706491-[1-(hetero)aryl-1-perhydroxyalkylmethyl]-piperazine compounds, process for their preparation and pharmaceutical compositions containing them
Novel 1-[1-(hetero)aryl-1-perhydroxyalkylmethyl]-piperazine compounds which are antagonistic to tachykinin receptors, of the general formula I, wherein R6, R7, A and Z have the meanings given in the...
08/03/2004
6723730Capsaicin receptor ligands
Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin receptors, including human...
04/20/2004
6696447Hydroxyphenyl-piperazinyl-methyl-benzamide derivatives for the treatment of pain
The present application describes compounds of general formula I ##STR1## where R1 is selected from any one of pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; and where each R1 heteroaromatic ring may optionally and independen...
02/24/2004
6686353Diarylalkyl cyclic diamine derivatives as chemokine receptor antagonists
Cyclic diamines of formula (I) or their pharmacologically acceptable acid addition salts, and their medical applications are described. These compounds inhibit the action of chemokines such as MIP-1a and/or MCP-1 on target cells, and are useful as a thera...
02/03/2004
6680321Compounds with analgesic effect
Compounds of the formula (I) ##STR1## as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain....
01/20/2004
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