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Class 514/260.1 - Ring chalcogen in the bicyclo ring system


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the second ring of the bicyclo
No. of patents: 251
Last issue date: 05/22/2012


1              
NumberTitleIssue Date
8183246Acyclically substituted furopyrimidine derivatives and use thereof
The present application relates to novel, acyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or pro...
05/22/2012
8153639Substituted thieno- and furano- fused pyrimidines as PI3K inhibitors
Fused pyrimidines of formula (I): wherein A, n, R1, R2, and R3 have any of the values defined herein and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K and...
04/10/2012
8148384Substituted thieno[3,2-d]pyrimidine PIM kinase inhibitors as cancer chemotherapeutics
Compounds of formula I wherein A1, A2, and A3 are as defined herein are inhibitors of PIM kinase. The compounds of formula I are useful for the treatment of diseases such as cancer. ...
04/03/2012
8143261Thiazolo (4,5-D) pyrimidine compounds
The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. ...
03/27/2012
8138194Fused bicyclic pyrimidine compounds as aurora kinase inhibitors
Fused bicyclic pyrimidine compounds of formula (I): wherein R1, R3, R4, X1, X2, Y, Z, A, B, C, D, n, and the two bonds are defined herein. Also disclosed are a method ...
03/20/2012
8129397Substituted thieno[2,3-d]pyrimidines as AMPA modulators
The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention...
03/06/2012
80887805,7-disubstituted thiazolo[4,5-D]pyrimidines for the selective inhibition of chemokine receptors
There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable s...
01/03/2012
8058280Substituted thieno[2,3-d]pyrimidin-2,4-dione compounds and uses thereof
The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substit...
11/15/2011
8022076Substituted thieno[2,3-d]pyrimidines as potassium channel inhibitors
This invention relates to novel compound of formula (I) or pharmaceutically acceptable salts thereof. The invention is also directed to the uses of compounds having formula (I) in the treatment or prevention of diseases or ...
09/20/2011
79603955,7-disubstituted thiazolo[4,5-d]pyrimidines for the selective inhibition of chemokine receptors
There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, an...
06/14/2011
7947690Pyrimidine derivative condensed with a non-aromatic ring
The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one...
05/24/2011
79476935,7-disubstituted thiazolo[4,5-D]pyrimidines as chemokine inhibitors
There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in the specification, and pharmaceutically acceptable salts ...
05/24/2011
7947691Cyclic n-hydroxy imides as inhibitors of flap endonuclease and uses thereof
Acrylic n-hydroxy imides and their use in pharmaceutical compositions and in the inhibition of flap endonuclease are disclosed. ...
05/24/2011
7947692Substituted thiazolo[5,4-d]pyrimidine urea derivatives
There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are active adenosine A2B receptor antagonists and useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhe...
05/24/2011
7928111Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
The present invention provides compounds including substituted thienopyrimidinone derivatives of Formula (IIc) as ligands for modulating chemosensory receptors: These compounds are useful as sweet taste enhancers in comesti...
04/19/2011
7915267Heterocyclic amide compound and use thereof
The present invention provides a novel amide compound represented by the following formula, which has a matrix metalloproteinase inhibitory activity and is useful as a pharmaceutical agent. wherein each symbol is as defined...
03/29/2011
7829570Substituted 4-amino isoxazolo[5,4-d]pyrimidines as kinase inhibitors
The present application is directed to compounds of the formula (I) wherein the substituents are as defined herein, which are useful as kinase inhibitors. ...
11/09/2010
7807684HIV reverse transcriptase inhibitors
Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the i...
10/05/2010
7776868Substituted bicyclic and tricyclic thieno[2,3-d]pyrimidines as Aadenosine receptor antagonists
The present invention relates to novel compounds that are A2A adenosine receptor antagonists having the structure of Formula I and to their use in treating mammals for various disease states, such as obesity, CNS...
08/17/2010
7776867Furanopyrimidines
The present invention relates to furanopyrimidine compounds having the general Formula I: and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also i...
08/17/2010
7763623Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia
A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dy...
07/27/2010
7750015Nitrogen-containing heterocyclic compounds and methods of use thereof
The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of: ...
07/06/2010
7745447Substituted thieno[3,2-D]pyrimidines as non-basic melanin concentrating hormone receptor-1 antagonists
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compo...
06/29/2010
7745448Crystalline N-(4-(4-aminothieno[2,3-d]pyrimidin-5-yl)phenyl)-N′-(2-fluoro-5-(trifluoromethyl)phenyl)urea ethanolate
A crystalline N-(4-(4-aminothieno[2,3 -d]pyrimidin-5-yl)phenyl)-N′-(2-fluoro-5-(trifluoromethyl)phenyl)urea ethanolate characterized in the monoclinic crystal system and P21/n space group, when measured with radiation at 0.7107 Å, by lattice parameter...
06/29/2010
7745449Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wh...
06/29/2010
7737155Nitrogen-containing heterocyclic compounds and methods of use thereof
The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts, solvates, esters, and tautomers thereof, wherein: Q is selected from the group consisting of...
06/15/2010
7723342Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia
A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group c...
05/25/2010
7612078Piperidinylamino-thieno[2,3-D] pyrimidine compounds
The invention relates to 5-HT receptor modulators, particularly 5-HT2B antagonists. Novel piperidinylamino-thieno[2,3-d]pyrimidine compounds represented by Formula I, II and III, and uses thereof for treating conditions including pulmonary arterial hypert...
11/03/2009
7601725Thienopyrimidines useful as Aurora kinase inhibitors
The present invention provides compounds having the formula: wherein R1, R2, X1, X2, L1, L2, Y and Z are as defined in classes and s...
10/13/2009
7598254Substituted 1,3-thiazolo[5,4-d]pyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts: in which R1 is a group of phenyl, naphthyl, pyridyl or the like which may have a substituent such as an alkyl group having 1-8 carbo...
10/06/2009
7595324Substituted thieno[3,2-D]pyrimidines as HIV inhibitors
This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A...
09/29/2009
7585867Substituted thiazolo[4,5-d]pyrimidin-2(3H)-one
A compound of formula (I) and pharmaceutically acceptable salts or solvates thereof for use in therapy. ...
09/08/2009
7569570Thienopyrimidines, process for preparing the same and use thereof
The present invention provides a thienopyrimidine compound, represented by the formula [wherein, R1 is C1-4 alkyl, R2 is (1) phenyl optionally having a substituent such as amino, mono C1-...
08/04/2009
7566721Substituted thienol[2,3-d]pyrimidines as kinase inhibitors
Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment a...
07/28/2009
7557111Substituted thieno[3,2-d]pyrimidines as CRF receptor antagonists
An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disea...
07/07/2009
7557112Aromatic-ring-fused pyrimidine derivative
There are provided novel pyrimidine derivatives which has been fused with an aromatic heterocycle selected from thiophene, thiazole and pyridine or pharmaceutically acceptable salts thereof; and a pharmaceutical composition comprising said compound as an active ingr...
07/07/2009
7498333Enantiomers of selected fused heterocyclics and uses thereof
This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer. ...
03/03/2009
7456187Furanopyrimidine compounds as potassium ion channel inhibitors
A compound of formula (I) wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, —CO2R7, CONR
11/25/2008
7449472Methods of inhibiting p38 with substituted bicyclic pyrimidines
The present invention discloses compounds corresponding to the formula wherein A, X, Y, R, R1 and R2 are as defined within, pharmaceutical formulations, methods of making and uses thereof. ...
11/11/2008
7439247Bicyclic pyridine and pyrimidine P38 kinase inhibitors
The present invention discloses compounds corresponding to formula wherein A, R, X, Y, R, R1 and R2 are as defined above, pharmaceutical formulations, methods of making and uses thereof. ...
10/21/2008
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