Class 544/354 - Chalcogen bonded directly to diazine ring carbon

Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogen (i.e., oxygen, sulfur, selenium,
No. of patents: 372
Last issue date: 10/07/2008

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Number	Title	Issue Date
7432270	N-aroyl cyclic amines This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists wherein: Y represents a bond, oxygen, or a group (CH2)n, wherein n represents 1, 2 or 3;...	10/07/2008
7432264	Antimicrobial 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
7368445	Fused pyrazole derivatives as TGF-β signal transduction inhibitors for the treatment of fibrosis and neoplasms The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds. ...	05/06/2008
7351709	Estrogen receptor ligands The present invention relates to estrogen receptor ligands, and compounds and methods for treating diseases associated with excessive estrogen receptor activity. Compound of the formula I are disclosed: wherein W is O or (C...	04/01/2008
7294716	Process for preparing isomerically pure prodrugs of proton pump inhibitors Synthetic methods for preparing isomerically pure N-arylsulfonyl derivatives of proton pump inhibitors which include a substituted benzimidazole nucleus are shown by the synthetic schemes and experimental description. ...	11/13/2007
7259161	Compositions useful as inhibitors of JAK and other protein kinases The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the inventio...	08/21/2007
7244722	Amino-substituted 1H-pyrazin-2-ones and 1H-quinoxalin-2-ones Compounds of the general formula (I): wherein m, n, R1, R2, R3 and R4 are as described in the specification.	07/17/2007
7205408	Quinolines and nitrogenated derivative thereof substituted in 4-position by a piperidine-containing moiety and their use as antibacterial agents Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man. ...	04/17/2007
7199259	Resolution of α-(phenoxy)phenylacetic acid derivatives The present invention provides a method for producing an enantiomerically enriched α-(phenoxy)phenylacetic acid compound of the formula (I): from its enantiomeric mixture, where R1 is alkyl or haloalk...	04/03/2007
7183281	Sulfonylquinoxalone derivatives and related compounds as bradykinin antagonists Disclosed are sulfonylquinoxalone derivatives of the general formula: These compounds are useful as bradykinin antagonists. ...	02/27/2007
7176312	Kinase inhibitor scaffolds and methods for their preparation General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor...	02/13/2007
7148224	Pyrazinone derivatives The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc...	12/12/2006
7125863	Inhibitors of dipeptidyl peptidase IV Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of t...	10/24/2006
7109341	Therapeutic amides The invention provides compounds of the formula: wherein A, X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides pharmaceutical compositions ...	09/19/2006
7094784	High affinity ligands for nociceptin receptor ORL-1 Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1	08/22/2006
7071180	Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2�...	07/04/2006
7053104	Metabotropic glutamate receptor antagonists and their use for treating central nervous system diseases The present invention provides compounds, and pharmaceutical compositions containing those compounds, that are active at metabotropic glutamate receptors. The compounds are useful for treating neurological diseases and disorders. Methods of preparing the compounds a...	05/30/2006
7030125	Isothiazole and isoxazole compounds as transforming growth factor (TGF) inhibitors Novel isothiazole and isoxazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of...	04/18/2006
6995154	Heterocyclic topoisomerase poisons The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical co...	02/07/2006
6989384	Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical ...	01/24/2006
6943170	N-cycloalkylglycines as HIV protease inhibitors This invention relates generally to N-cycloalkylglycines of the Formula (I): or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which are useful as HIV protease ...	09/13/2005
6927214	Non-peptide GLP-1 agonists Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of...	08/09/2005
6916805	Quinoxalinones as serine protease inhibitors This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable co...	07/12/2005
6914062	Pyrazinone derivatives The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V i...	07/05/2005
6908921	Quinoxalinone derivatives as bradykinin B1 antagonists 2-Quinoxalinone derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. ...	06/21/2005
6897312	Method for producing high melting point crystals of phenoxypropionic acid derivative A method for producing β crystals of ethyl (R)-2-[4-(6-chloro-2-quinoxalin-2-yloxy)phenoxy]propionate, which is characterized by heating α crystals, or α crystals and β crystals, within a range of from 50° C. to lower than the melting point of the α crystals.	05/24/2005
6890926	Heteroaryl derivatives and their use as medicaments The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors. ...	05/10/2005
6852712	Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a pati...	02/08/2005
6849660	Antimicrobial 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
6846815	Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient...	01/25/2005
6815442	Quinoxalinones for enhancing chemotherapy The present invention provides 1H-quinoxalinones, of the formula: or pharmaceutically acceptable salts thereof, wherein R1, R2, and n are as defined herein. Also disclosed are pharmaceutical compo...	11/09/2004
6777413	2-[1H]-quinolone and 2-[1H]-quinoxalone inhibitors of factor Xa Novel compounds of general formula I: including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivative having activity against mammalian factor Xa is described. Compositions containin...	08/17/2004
6759401	Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alky...	07/06/2004
6723834	Reactive dye compounds A reactive dye compound comprising: (a) at least one chromophore moiety; (b) at least one nitrogen-containing heterocycle (c) a linking group to link each chromophore moiety to each nitrogen-containing heterocycle; characterized in that a...	04/20/2004
6713613	Reactive dye compounds A reactive dye compound comprising: (a) at least one chromophore moiety (b) at least one nitrogen-containing heterocycle (c) a linking group to link each chromophore moiety to each nitrogen-containing heterocycle; characterised in that at...	03/30/2004
6693112	Compounds for enhancing chemotherapy The present invention provides 2,3-dihydro-1H-pyrrolo[2,3-b]quinolin-4-ylamines, of the formula: ##STR1## or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R7 are as defined herein. Also disc...	02/17/2004
6683101	Bicyclic cyclohexylamines and their use as NMDA receptor antagonists Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of the formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders...	01/27/2004
6683184	Piperazine derivatives and process for the preparation thereof The present invention relates to a novel compound of formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antitumor activities and very low toxicity: ##STR1## wherein R	01/27/2004
6667302	Heterocyclic topoisomerase poisons The invention provides compounds of formula I: ##STR1## wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the c...	12/23/2003
6635641	Amide compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use Amide compounds represented by the formula: ##STR1## wherein: R1 is a moiety represented by the formula ##STR2## where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting...	10/21/2003

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Class 544/354 - Chalcogen bonded directly to diazine ring carbon