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Class 546/209 - Ring sulfur or ring oxygen in the additional hetero ring


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the additional heteror ring additionally
No. of patents: 813
Last issue date: 05/17/2011


1                      
NumberTitleIssue Date
7943774Heterocyclyl-substituted thiazoles as crop protection agents
Heterocyclyl-substituted thiazoles of the formula (I), in which the symbols have the meanings given in the description, and also to the agrochemically active salts thereof, and their use for controlling phytopathogenic harm...
05/17/2011
7902367Cyclic amino benzoic acid derivative
The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against h...
03/08/2011
7880008Heterocycles useful as modulators of ion channels
The present invention relates to compounds 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 treatment of various disorder...
02/01/2011
7872139Heteroaryl-ureas and their use as glucokinase activators
This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity i...
01/18/2011
7781590Piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase enzyme inhibitors
The present invention comprises peridinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inte...
08/24/2010
7767819Thiazolylimidazole derivatives and their use as inhibitors of microsomal triglyceride transfer protein
The present invention relates to thiazolylimidazole derivatives of the general formula (I) in which: G represents a bond or a divalent radical chosen from the groups g1, g2 and g3; and R1, R2, R3, R4, R5, R...
08/03/2010
7557214Intermediate products for producing oxazolidinone-quinolone hybrids
The present invention describes intermediates (ZP) for a novel and efficient synthesis of compounds in which the pharmacophores of quinolone and oxazolidinone are linked to one another by way of a chemically stable linker. ...
07/07/2009
7435747Guanidine and amidine derivatives as factor Xa inhibitors
The present invention relates to compounds of the formula I, in which R0; Q; X; Q′, D, R10 and V have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacological...
10/14/2008
7432285Nitrosated and nitrosylated cyclooxygenase-2 inhibitors, compositions and methods of use
The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound that don...
10/07/2008
74296075-HTreceptor antagonists
The present invention relates to compounds of formula I: wherein one of R1 and R4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalky...
09/30/2008
7429667Phenylamino isothiazole carboxamidines as MEK inhibitors
The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones. ...
09/30/2008
7425633Pyrrolidine compounds
A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, T, X, Y, and Z are as defined herein. Also disclosed is a ...
09/16/2008
74230534-Aminothiazole derivatives
Novel 4-aminothiazole derivatives are disclosed. These compounds inhibit cyclin-dependent kinases. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particu...
09/09/2008
7423052Piperidine compounds for use as orexin receptor antagoinst
A invention relates to N aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists. ...
09/09/2008
74140484,5-dihydro-isoxazole derivatives and their pharmaceutical use
The present invention is concerned with the compounds of formula wherein m, n and p are each independently 0 or 1 and q is 0, 1, 2, 3, 4 or 5; -A1=A2-A3=A4- is a pyridinylidene, p...
08/19/2008
7407976Thiazoles and oxazoles useful as modulators of ATP-Binding Cassette transporters
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to meth...
08/05/2008
7405228Antibacterial cyano-(substituted)-methylenepiperidinophenyl oxazolidinones targeting multiple ribonucleoprotein sites
The present invention provides agents having high antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel cyano-(substituted)-methylenepiperidinophenyl oxazolidinone derivatives, processes for making the com...
07/29/2008
7405218Isothiazole derivatives useful as anticancer agents
The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein....
07/29/2008
7390804N-containing five-membered ring compounds and pharmaceutical agents comprising the same as active ingredient
An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity aga...
06/24/2008
73616582-acylaminothiazole derivative or salt thereof
2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of megakaryocytic colonies and which are useful for treating thrombocytop...
04/22/2008
7354919Isoxazole compositions useful as inhibitors of ERK
Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compo...
04/08/2008
7351720N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as auto...
04/01/2008
7351721Amino acid derivatives and pharmaceutical composition comprising, as active ingredients, them
The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-...
04/01/2008
7345043Inhibitors of histone deacetylase
Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by ...
03/18/2008
73420271-phenylpiperidin-3-one derivatives and processes for the preparation thereof
Provided are 1-phenylpiperidin-3-one derivatives and pharmaceutically acceptable salts thereof, having cysteine protease inhibitory activity, pharmaceutical compositions containing the same as an active ingredient, and processes for the preparation thereof. ...
03/11/2008
7335670Derivatives of N-[heteroaryl(piperidine-2-yl) methyl]benzamide, preparation method thereof and application of same in therapeutics
Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyrami...
02/26/2008
7332504Heterocyclic substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions ...
02/19/2008
7326720Phenyl- and pyridylpiperidines with TNF activity
The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; R2 and R3 independent...
02/05/2008
7320978Oxazole derivatives, preparation and therapeutic use thereof
This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The i...
01/22/2008
7312350Process for preparing arylalkynes
The invention relates to a process for preparing arylvinyl halides and sulphonates and arylalkynes by reacting haloaromatics or aryl sulphonates with vinyl halides or sulphonates in the presence of a palladium catalyst and a base and, if appropriate, subsequent elim...
12/25/2007
7309709Thiazole sulfonamide compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula: wherein R1 to R6, X, Z and A are as defined. These compounds have activity inhibiting production of Aβ-peptide. The invention also...
12/18/2007
7304050Antibacterial agents
Compounds of formula I and methods for their preparation are disclosed. Further disclosed are methods of making biologically active compounds of formula I as well as pharmaceutically acceptable compositions comprising compounds of formula I. Compounds of formula I a...
12/04/2007
7273882Aminoacetamide acyl guanidines as β-secretase inhibitors
There is provided a series of substituted acyl guanidines of Formula (Ik) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R2, R3, R4, R5, R
09/25/2007
7265109Thiazole derivatives
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein the substituents have the significance given in the specification, and the compounds are neuropeptide Y(NPY) antagon...
09/04/2007
7265134Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...
09/04/2007
7259157N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ...
08/21/2007
7253186N-substituted piperidine derivatives as serotonin receptor agents
Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contac...
08/07/2007
7238689Isoxazoline derivative and herbicide comprising the same as active ingredient
An isoxazoline derivative represented by the following general formula [I]: wherein R1 and R2 may be the same or different and are each an alkyl group; R
07/03/2007
7229998Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors
The present invention provides a compound of formula (I): wherein R1–R5, R25, R26, Y and X2 are as defined herein. The compounds a...
06/12/2007
72269334-(phenyl-(piperidin-4-yl)-amino)-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, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, and pyridine N-oxide; where each R1 phenyl ring and R...
06/05/2007
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