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Class 544/309 - At 2-position and at 4- or 6-position


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogens (i.e., oxygen, sulfur, selenium,
No. of patents: 302
Last issue date: 05/29/2012


1                
NumberTitleIssue Date
8188275Dipeptidyl peptidase inhibitors
Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independen...
05/29/2012
81485252,4-pyrimidinediamine compounds and their uses
The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a...
04/03/2012
8084605Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
Compositions comprising the succinate salt of 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile (referred to herein as Compound I) which has the formula: wherein the...
12/27/2011
7847097Method for production of 1-alkyl-3-phenyluracils
The present invention relates to a process for preparing 1-alkyl-3-phenyluracils of the formula I where the variables R1 to R7 are as defined in the description by reacting 3-phenyluracils of the fo...
12/07/2010
7795428Dipeptidyl peptidase inhibitors
Compounds are provided for use with DPP-IV of the formula: Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds...
09/14/2010
7781584Dipeptidyl peptidase inhibitors
Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independen...
08/24/2010
7737275Method for producing 3-phenyl(thio)uracils and 3-phenyldithiouracils
A process is described for preparing 3-phenyl(thio)uracils or 3-phenyldithiouracils of the formula I, by reacting a phenyl iso(thio)cyanate of the formula II with an enamine of the formula III and, if appropriate, in a further step, the resulting 3-phenyl(thio)uraci...
06/15/2010
7405221Substituted pyrimidines
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are...
07/29/2008
7402586Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12—R15, R
07/22/2008
7371859PNA 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:
05/13/2008
7250421Diketo acids with nucleobase scaffolds: anti-HIV replication inhibitors targeted at HIV integrase
A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS a...
07/31/2007
7232902Process to prepare (1-carboxymethyl)-pyrimidinone compounds
The invention relates to a process for the preparation of certain pyrimidinone compounds. ...
06/19/2007
7229995Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein n, R
06/12/2007
RE39590Substituted benzene compounds, process for their preparation, and herbicidal and defoliant compositions containing them
Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of ...
04/24/2007
7205307Pyrimidines as novel openers of potassium ion channels
The present invention provides a genus of pyrimidine amides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods. ...
04/17/2007
7179815Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R...
02/20/2007
7176211Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1...
02/13/2007
7160893Pyrimidine-2,4-dione derivatives as matrix metalloproteinase inhibitors
This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, R2, R3, and R4 are as defined in the spec...
01/09/2007
7153963Phenylalanine derivatives
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin ...
12/26/2006
7119096Uracil reductase inactivators
Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 ...
10/10/2006
7101873Pyrimidinedione derivatives
Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them are useful for the tre...
09/05/2006
7078527Method for producing halogenated 2-(3-butenylsulphanyl)-1,3-thiazoles
The present invention relates to a process for preparing compounds of the formula (I) where R is H or F, by (a) reacting a compound of the formula (II)
07/18/2006
7071200Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1...
07/04/2006
7067664Corticotropin releasing factor antagonists
Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 an...
06/27/2006
7056927Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1...
06/06/2006
7034156Method for the production of 1-amino-3-phenyluracil derivatives
The present invention relates to a novel process for preparing known 1-amino-3-phenyluracil derivatives, to novel 1-amino-6-hydroxy-3-phenyldihydro-2,4(1H,3H)pyrimidinedione derivatives of the formula (II) in which ...
04/25/2006
7030130Benzofuran derivatives and their use as antibacterial agents
The invention relates to novel benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical composit...
04/18/2006
7026270Biocidal compounds and their preparation
This invention concerns new biocidal compounds of formula (I) wherein R is H or CH3. Of particular interest are two isomers that are named malayamycin A and desmethylmalayamycin A. These isomers, which may be prepared by growing under controlled condition...
04/11/2006
7015226Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein n, R1a
03/21/2006
7012041Phenylpyridazinones
The invention relates to novel phenylpyridazinones of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, ...
03/14/2006
70090505-Substituted pyrimidine derivatives of conformationally locked nucleoside analogues
The embodiments described herein concern 5-substituted pyrimidine derivatives of conformationally locked nucleoside analogues and to the use of these derivatives as anti-viral and anti-cancer agents. The compounds are of the formula:
03/07/2006
6987114Antiviral pyrimidinedione derivatives and process for the preparation thereof
The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical ...
01/17/2006
6946284Solubilizing cross-linked polymers with photolyase
The invention relates to methods of solubilizing and recycling polymers using irradiation, wherein the polymers comprise photoreactive moieties. These polymers have many applications including use in disposable consumer products such as beverage bottles, eating uten...
09/20/2005
6936620Barbituric acid derivatives as inhibitors of TNF-α converting enzyme (TACE) and/or matrix metalloproteinases
The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, W, Z, Ua, Xa, Y...
08/30/2005
6930112Anti-epileptogenic agents
Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and epileptogenesis. Methods for preparing the compounds of the invention are also d...
08/16/2005
69301076-azauracil derivatives as thyroid receptor ligands
The present invention provides novel compounds of the Formula I and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R...
08/16/2005
6927193Aryl ether derivatives and processes for their preparation and herbicidal and desiccant compositions containing them
Substituted aryl ether derived compounds represented by the general structure (I) are described. X and Y are independent of each other and are represented by hydrogen, halogen, cyano, nitro, (C1-4)alkyl, (C1-4)haloalkyl, or (C1-4)hal...
08/09/2005
6927215Heterocyclic fluoroalkenyl thioethers and the use thereof as pesticides (I)
The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integer...
08/09/2005
69218231,2,3,4,5,6-Hexahydroazepino[4,5-b]indoles containing arylsulfones at the 9-position
The present invention are substituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (X) and unsubstituted 9-arylsulfone-1,2,3,4,5,6-hexahydroazepino[4,5-b]indoles (XI) such as the compound of EXAMPLE 13 whic...
07/26/2005
6908937Heterocyclic fluoroalkenyl thioethers (II)
The present invention relates to novel heterocyclic fluoroalkenyl thioethers of the formula (I) in which X represents hydrogen, halogen or alkyl, m represents integers from 3 to 10,
06/21/2005
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