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Class 548/200 - Having -C(=X)-, wherein X is chalcogen, bonded directly to the thiazole ring


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein a group, in which X is chalcogen, (i.e.,
No. of patents: 479
Last issue date: 01/31/2012


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NumberTitleIssue Date
81062153-aza-bicyclo[3.3.0]octane compounds
The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R1, R2, R3, and A are as described in the description and their use as orexin receptor antagonists. ...
01/31/2012
8030495Cyclopropyl pyrrolidine orexin receptor antagonists
The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved....
10/04/2011
8017788Heteroaryl (substituted)alkyl -substituted sulfoximines as insecticides
N-Substituted heteroaryl (substituted)alkyl sulfoximines are effective at controlling insects. ...
09/13/2011
7868179Thiazolyl biphenyl amides
The invention relates to novel thiazolylbiphenylamides of the formula (I) in which R1, R2, R3, R4, R5 and R6 are as defined in the d...
01/11/2011
7667044Compounds for the treatment of neurological disorders
The present invention relates to novel inhibitors of prolyl endopeptidase of formula 1 W—KCONH—X—CON—Y—CO—Z  (1) wherein K, W, X, Y and Z are specified in the description. The compounds are useful for the treatment of dise...
02/23/2010
7566787Small molecule cyclin D1 ablative agents
Cyclin D1 ablative agents and methods of using these agents in the treatment of cancers, and particularly breast cancer. Also provided are methods of treating cancer, the method comprising administering a therapeutically effective amount of one of the cyclin D1 abla...
07/28/2009
7560569Bicycloamide derivative
Novel bicycloamide derivatives (general formula (1)) and pharmaceutically acceptable salts thereof effectively inhibit DPP-IV. The bicycloamide derivatives are represented by the general formula (1): Pharmaceutically accept...
07/14/2009
7560570Inhibitors of fatty acid amide hydrolase
Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having Ki's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, ...
07/14/2009
7553975Farnesyl transferase inhibitors
A family of compounds capable of inhibiting the activity of farnesyl transferase. ...
06/30/2009
7452999Chemical process for the preparation of intermediates to obtain -formyl hydroxy-lamine compounds
Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) m...
11/18/2008
7429669Therapeutic compounds
Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed. ...
09/30/2008
7427634Amino 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-...
09/23/2008
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
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
7388017Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease
The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, eith...
06/17/2008
7378397TRH-degrading ectoenzyme inhibitors
Peptide derivatives useful as inhibitors of activity of thyrotropin-releasing hormone-degrading ectoenzyme (TRH-DE) are of formula Ia: wherein: R1 is an optionally su...
05/27/2008
7371777Cyclic compound and PPAR agonist
The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. ...
05/13/2008
7368576Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more pre...
05/06/2008
7348346Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
The present invention relates to compounds of formula (I), which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, sy...
03/25/2008
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
7345180Compound inhibiting dipeptidyl peptidase IV
A dipeptidyl peptidase IV inhibitor which is satisfactory in respect of activity, stability and safety and has an excellent action as a pharmaceutical agent. A compound represented by the following general formula or a pharmaceutically acceptable salt thereof:
03/18/2008
7342032Thiazole derivatives having CB-antagonistic, agonistic or partial agonistic activity
Computer game systems respond to the spatial state of a pointing device. Changes in the spatial state of a hand held or mobile unit, or plurality of units drive a game scheme maintained in a computer. Position and attitude of the mobile device cause program branchin...
03/11/2008
7335645Effectors of dipeptidyl peptidase IV for topical use
The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one f...
02/26/2008
7332513Thiazole-based nitric oxide donors having acyl substituent(s) and uses thereof
Disclosed are novel NO-donating compounds, designed such that when NO is released from the compound a residue which is a naturally occurring metabolite is formed, and thus a development of tolerance to the compounds upon repetitive administration is prevented or dec...
02/19/2008
7332487Nitrogen-containing 5-membered ring compound
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; ...
02/19/2008
7307093Thiazolidinone amides, thiazolidine carboxylic acid amides, methods of making, and uses thereof
Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed where the various substituent groups are as defined in the specification...
12/11/2007
72946421,3-Diamino-2-hydroxypropane pro-drug derivatives
The present invention relates to compounds of formula (AA) (I) and (X): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are ...
11/13/2007
7285670Synthesis of substituted thiazoline carboxylic acids
A useful and efficient method of preparing an alkylated thiazoline carboxylic acid, or a derivative thereof, comprises coupling a substituted aryl nitrile such as, for example, 2,4-dimethoxybenzonitrile or 4-methoxybenzonitrile, with a cysteine ester to form a subst...
10/23/2007
7285554Pyrazole derivative
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors conta...
10/23/2007
72738662-aryl thiazole derivatives as KCNQ modulators
Novel 2-arylthiazole derivatives of Formula I are described which are openers of KCNQ potassium channels and are useful in the treatment of disorders that are responsive to the opening of the KCNQ potassium channels, including pain and migraine
09/25/2007
7273863Benzophenones as inhibitors of reverse transcriptase
The present invention includes benzophenone compounds (I) which are useful in the treatment of HIV infections. ...
09/25/2007
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
7247635Pyrazole derivative
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors conta...
07/24/2007
7244849Process for preparing a thiazole PPAR-ligand and polymorphs thereof
A method of preparing a compound of formula (I), and pharmaceutically acceptable salts and solvates thereof. Polymorphs of this compound and their use as PPAR ligands are also disclosed ...
07/17/2007
7241900Synthesis of indole thiazole compounds as ligands for the Ah receptor
A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of for...
07/10/2007
7238683Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is in...
07/03/2007
72328382-amino-4,5-trisubstituted thiazolyl derivatives
This invention concerns the use of a compound of formula (I′), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6...
06/19/2007
7208528Polyamine analogues as therapeutic and diagnostic agents
Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine t...
04/24/2007
7196201Pyrrolidines as dipeptidyl peptidase inhibitors
The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility
03/27/2007
7196108Bicyclic heterocycles for the treatment of diabetes and other diseases
The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.
03/27/2007
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