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Class 544/367 - Ring chalcogen in the five-membered hetero ring


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the five-membered hetero ring contains
No. of patents: 431
Last issue date: 11/09/2010


1                      
NumberTitleIssue Date
7829712Pyridazine derivatives for inhibiting human stearoyl-CoA-desaturase
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7...
11/09/2010
7777036Heterocyclic derivatives and their use as therapeutic agents
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where y, G, K, L, M, W, V, R2, R3, R4...
08/17/2010
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
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
7427620Azole derivative useful as antifungal agents with reduced interaction with metabolic cytochromes
The present invention relates to novel compounds, of the general formula (I), the N-oxide forms thereof, the salts thereof with pharmaceutically acceptable acids and the stereochemical isomers thereof, which are useful as antifungal agents; to pharmaceutical composi...
09/23/2008
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
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
7405217N-aroyl piperazine derivatives as orexin receptor antagonists
This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals. ...
07/29/2008
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
7351822Serine 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 cardiovasc...
04/01/2008
7348347Substituted 4,5,6,7-tetrahydrobenzthiazol-2-ylamine compounds
Substituted 4,5,6,7-tetrahydrobenzothiazol-2-ylamine compounds, a method for their production; pharmaceutical compositions comprising them, and methods of use for modulating biological functions and/or treating or inhibiting various medical conditions such as, e.g.,...
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
73420171,2,5-Thiadiazol-3-yl-piperazine therapeutic agents useful for treating pain, depression and anxiety
A compound of formula: (wherein X, R1, R3, R4, and R5 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Thiadiazolylpiperazine Compound”), pharmaceutical...
03/11/2008
7335660Isochroman compounds for treatment of CNS disorders
This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the tre...
02/26/2008
7329749Piperazinylcarbonylquinolines and -isoquinolines
Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkins...
02/12/2008
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
7294628Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; R1 represents a halogen at...
11/13/2007
72916336H-oxazolo[4,5-e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands
Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychose...
11/06/2007
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
72531734(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain of gastrointestinal disorders
Compounds of general formula (I) wherein R1, R2 and R3 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 pa...
08/07/2007
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
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
7220745Heterocyclic compounds useful to treat HCV
The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication a...
05/22/2007
7220744Monocyclic substituted phenyl methanones
The present invention relates to compounds of formula I wherein R1, R2, X1, and X2 are as defined in the specification an...
05/22/2007
7217714CCR5 modulators
Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ]   (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/15/2007
7211668PNA monomer and precursor
This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers:
05/01/2007
7173035Arylsulfonamide compounds
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II...
02/06/2007
7166608-aroyl piperazine derivatives as orexin receptor antagonists
This invention relates to N-aroyl piperazine derivatives of formula (I), wherein: Y represents NR2; m represents 1, 2 or 3; p represents 0 or 1; X is O, S, C═O, SO2, or CH═CH—; Ar1 is aryl, or a mono or bicyclic heteroaryl grou...
01/23/2007
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
7157464Substituted piperazines
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful ...
01/02/2007
7141570N-aryl-2-oxazolidinone-5-carboxamides and their derivatives
The present invention provides antibacterial agents having the formula I described herein. ...
11/28/2006
7119203Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metallop...
10/10/2006
7115639Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists
The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in...
10/03/2006
7105670Intermediates useful in the preparation of diaminothiazoles
Disclosed are novel diaminothiazoles that are selective inhibitors of Cdk4. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and...
09/12/2006
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
7091219Bis-sulfonamide hydroxyethyl-amino retroviral protease inhibitors
Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula:
08/15/2006
7056924Substituted heterocyclic compounds
Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, ...
06/06/2006
7026321Substituted heterocyclic compounds
Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, ...
04/11/2006
7022705Isoxazoline derivatives useful as antimicrobials
Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein, for example, HET is an N-linked 5-membered, fully or partially u...
04/04/2006
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