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Class 514/253.1 - The five-membered nitrogen hetero ring has chalcogen as a ring member


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the five-membered nitrogen hetero
No. of patents: 191
Last issue date: 03/20/2012


1          
NumberTitleIssue Date
8138191Inhibitor compounds and cancer treatment methods
A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods...
03/20/2012
7994174Pyridyl sulfonamides as modulators of ion channels
The present invention relates to pyridyl sulfonamide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatme...
08/09/2011
7943622Piperazines, pharmaceutical compositions and methods of use thereof
Disclosed are novel piperazine derivatives that act as agonists of the α7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian c...
05/17/2011
7786125Neuroprotective small organic molecules, compositions and uses of related thereto
The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS). ...
08/31/2010
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
7393845Heteroaryl derivates, their preparation and use
A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disord...
07/01/2008
7384944Piperazine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R
06/10/2008
73717461,2,4-Thiadiazole compounds and pests controlling composition containing the same
The present invention relates to a 1,2,4-thiadiazole compound of the formula (I) represented by the formula (1): wherein R1? represents C3-C7 alkynyl and X represents C4-C7 straight alkylene optionally substituted with one to four of R2?, C4-C7 straight alkenylene o...
05/13/2008
7361654Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory- and immune-associated disea...
04/22/2008
7300939Substituted 1-propiolylpiperazine compounds, their preparation and use
Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine com...
11/27/2007
7297693Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. ...
11/20/2007
7291639Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
This invention provides methods of inhibiting plasminogen activator inhibitor-1 (PAI-1) in a mammal, utilizing compounds of the formula: wherein: A is C or N; B is O, S, N, or CH═CH;
11/06/2007
7247631Pegylated interferon alfa-CCR5 antagonist combination HIV therapy
Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering a therapeutically effective amount of pegylated interferon-alfa, e.g...
07/24/2007
7247702Periocular drug delivery for diabetic retinopathy
This invention provides reagents and methods for delivering insulin, insulinomimetic agents, and the like to a vertebrate eye via subconjunctival routes, sub-Tenon's routes, or intravitreal routes for treatment of nerve-related vision disorders such as diabetic reti...
07/24/2007
72417644(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders
Compounds of general formula:[Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions includin...
07/10/2007
7238688Piperidine compounds
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such ...
07/03/2007
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
7132438Benzimidazole derivatives
Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins inv...
11/07/2006
7101885Piperazinyl-aryloxy and piperazinyl-heteroaryloxy-n-aryl lactams
The present invention relates to compounds of formula I wherein Ar, Y and G are as defined in the specification, a is 1 to 4, Z and W are carbon or nitrogen and n is 1, 2 or 3; and to pharmaceutical compositions ...
09/05/2006
7101886Phenylalkyl and pyridylalkyl piperazine derivatives
This invention relates to compounds of the formula 1 wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containi...
09/05/2006
RE39265Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compound...
09/05/2006
7094778Heterocyclylalkylamines 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 NR5, and the other substituents are...
08/22/2006
7087610Benzothiazole antiviral agents
The invention encompasses a series of benzothiazole compounds which inhibit HIV entry and are useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for using these compounds. ...
08/08/2006
7052742Five membered-ring compounds and utilization thereof in liquid crystal mixtures
Fluorinated five-membered ring compounds of the formula (I) R1—X—(A1—M1)a—(A2—M2)b—A3—Y—E   (I) where E is a radical T—Z—R2
05/30/2006
7026314Therapeutic chromone compounds
Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds ...
04/11/2006
6992189Synthesis of piperidine and piperazine compounds as CCR5 antagonists
In its several embodiments, this invention discloses novel processes to prepare the compounds of formula II and formula IV: ...
01/31/2006
6939988Tricyclic compounds and their use in medicine process for their preparation and pharmaceutical compositions containing them
Novel β-aryl-α-oxysubstituted alkylcarboxylic acids of the formula (I) and compositions containing them. The compounds have hypolipidemic, antihyperglycemic uses. ...
09/06/2005
6936611Serine protease inhibitors
Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardi...
08/30/2005
6911448Piperazine and piperidine compounds
The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or h...
06/28/2005
6887870Heterocyclic sodium/proton exchange inhibitors and method
Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, a...
05/03/2005
6875767(5-cyano-2-thiazolyl)amino-4-pyridine tyrosine kinase inhibitors
The present invention relates to compounds having the formula I: which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to tre...
04/05/2005
6872724Polymorphs with tyrosine kinase activity
The present invention relates to active polymorphs of 4-[2-(5-cyano-thiazol-2-ylamino)-pyridin-4-ylmethyl]-piperazine-1-carboxylic acid methylamide which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compound...
03/29/2005
6833369Angiogenesis inhibiting 5-substituted-1,2,4,-thiadiazolyl derivatives
This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; R1 is hydrogen, C1-...
12/21/2004
6825200Substituted dipeptides having nos inhibiting activity
The present invention a compound represented by the formula (I): where the structural variables R1-R6 are defined herein. ...
11/30/2004
68219723-heterocyclylpropanohydroxamic acid PCP inhibitors
Compounds of formula (I): and their salts, solvates, hydrates and prodrugs are useful PCP inhibitors, processes for making the same, compositions comprising the same, and methods of treating a PCP-mediated condition or...
11/23/2004
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
6756374Diaminothiazoles having antiproliferative activity
Disclosed are novel diaminothiazoles of formula wherein R1, R2, R3, R4 and R5 are as herein disclosed. These compounds and their pharmaceutically acceptable salts an...
06/29/2004
6689765Piperazine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted hete...
02/10/2004
6638935Heteroary1 derivatives and their use as medicaments
The invention relates to novel pyridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors ##STR1##...
10/28/2003
6635646Pegylated interferon alfa-CCR5 antagonist combination HIV therapy
Methods for treating treatment-naive as well as treatment-experienced adult and pediatric patients having HIV-1 infections as well as patients co-infected with HIV-1 and HCV involving administering a therapeutically effective amount of pegylated interfero...
10/21/2003
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