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Class 514/252.16 - Polycyclo ring system having the additional 1,3-diazine ring as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional 1,3-diazine ring is
No. of patents: 349
Last issue date: 04/24/2012


1                  
NumberTitleIssue Date
81637532,3-dihydro-6-nitroimidazo (2,1-b) oxazole compounds for the treatment of tuberculosis
The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 m...
04/24/2012
8163755Hexahydrooxazinopterine compounds
The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods o...
04/24/2012
8163754Purine derivatives for use as adenosine A-2A receptor agonists
Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adeno...
04/24/2012
81148786,7-dihydrothieno[3,2-d]pyrimidine for the treatment of inflammatory diseases
The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but p...
02/14/2012
8114877Organic compounds
Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adeno...
02/14/2012
8093249Pyrazolo[1,5-A]pyrimidine-carbonyl-piperazine derivatives
The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calc...
01/10/2012
80630519-substituted-8-oxo-adenine compounds as toll-like receptor (TLR7) modulators
The present invention provides compounds of formula where n, R1, R2, A, X1, Y1, Z1, X2 and Y2 are as defined in the specification, processes for t...
11/22/2011
8063050Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compou...
11/22/2011
8044056Adenine compound
A novel adenine compound represented by the formula (1): [wherein R1 is substituted or unsubstituted alkyl, etc., X is oxygen, etc., A1 is 4- to 8-membered substituted or unsubstituted saturated nitrog...
10/25/2011
8017614Arylindenopyrimidines compound and use as an adenosine A2a receptor antagonists
This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. ...
09/13/2011
8003651Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of us...
08/23/2011
7994172[1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
The invention provides compounds of formula (I) and methods for inhibition of kinases, more specifically p70S6 kinases, and more preferably p70S6, Akt-1 and Akt-2 kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulati...
08/09/2011
7863279Triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives, preparation thereof and therapeutic use thereof
The invention relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention...
01/04/2011
7863278Isethionate salt of a selective CDK4 inhibitor
Disclosed are polymorphs of the isethionate salt of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor useful for treating inflammation and cell prol...
01/04/2011
7834019Substituted pyrazolo[3,4-d]pyrimidinone derivatives
The invention relates to compounds of a general formula (I): wherein Ar1 is an optionally-substituted aryl or heteroaromatic group; R1 is an optionally-substituted lower alkyl, lower alkenyl, lower alk...
11/16/2010
7825122Diaza heterocyclic sulfonamide derivatives and their uses
Diaza heterocyclic sulfonamide derivatives according to formula I have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: where R7, R8, R...
11/02/2010
7737147Methods and compositions to enhance the efficacy of phosphodiesterase inhibitors
Methods for treatment of sexual dysfunction in men and women using combinations of phosphodiesterase (PDE) type 5 inhibitors and l-deprenyl or propargylamine compounds are described. Methods of reducing the dosage and preventing the side effects of PDE type 5 inhibi...
06/15/2010
7723340Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith
Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and and R3 are as defined herein, compositions comprising an effective amoun...
05/25/2010
7723341Compounds for the treatment of inflammatory diseases
Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or ...
05/25/2010
7691860Sulfonamide derivatives
The present invention relates to compounds of the general formula (I): wherein A, B, C and D each independently are a methine group or a nitrogen atom, said methine group optionally having a substit...
04/06/2010
7666872Use for PDE5 inhibitors
The present invention is concerned with the use of PDE5 inhibitors in medicine. ...
02/23/2010
7662822Substituted azaquinazolines having an antiviral action
This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular agains...
02/16/2010
7550468Theophylline and 3-isobutyl-1 methylxanthine based N-7 substituted derivatives displaying inhibitory activities on PDE-5 phospodiesterase
A variety of N-substituted derivatives are based upon the base chemicals of that provide for the induction of cavernosal relaxation in animals. R2 is a derivative based on a hetroaromatic group, an aromatic group or a cyclo...
06/23/2009
7524847Fused 1,3-dihydro-imidazole ring compounds
The objective of this invention is to provide novel compounds that show excellent DPPIV-inhibiting activity. The present invention provides compounds represented by the general formula (I), salts thereof, or hydrates thereof,
04/28/2009
7511045Compounds for the treatment of inflammatory diseases
Dihydrothienopyrimidines of formula 1 and the pharmacologically acceptable salts, enantiomers, racemates, hydrates, or solvates thereof, which are suitable for the treatment of respiratory or gastrointestinal complaints or ...
03/31/2009
7504398Substituted-4-(pyrrolo pyrimidin-6-yl)benzenesulphonamide derivatives
This invention is directed to selective antagonists of A2A and/or A2B adenosine receptors having the general formula (I); to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
03/17/2009
74706904-(2-Fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-D)pyrimidine in the treatment of functional bowel disorder
Use of 4-(2-Fluorophenyl)-6-Methyl-2-(1-Piperazinyl)Thieno[2,3-D]Pyrimidine or a salt thereof for the manufacture of a medicament for the treatment of functional bowel disorder. ...
12/30/2008
7462618Treatment of inflammatory autoimmune diseases with alpha-adrenergic antagonists and beta-adrenergic agonists
The present invention discloses a novel compound and method for the treatment of inflammatory autoimmune diseases, for example, rheumatoid arthritis, using α-adrenergic antagonists and β-adrenergic agonists in combination. Treatment of animals, namely humans, with...
12/09/2008
74295961H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
This invention generally relates to pyrazolo pyrimidine derivatives useful as inhibitors of short chain dehydrogenase/reductase (SDR) family of NAD(P)(H) dependent oxido-reductases. The invention further relates to pharmaceutical compositions and methods of preventi...
09/30/2008
7419981Synergistic combinations of an alpha-2-delta ligand and a cGMP phosphodieterse 5 inhibitor
The instant invention relates to a combination of an alpha-2-delta ligand and a PDEV inhibitor for use in therapy, particularly in the treatment of pain, particularly neuropathic pain. Particularly preferred alpha-2-delta ligands are gabapentin and pregabalin. A par...
09/02/2008
7414058Adenosine Areceptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
There is disclosed a method for the treatment of Extra Pyramidal syndrome (EPS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS. ...
08/19/2008
73908054-amino-6-phenyl-pyrrolo[2,3-d]pyrimidine derivatives
The invention relates to 7H-pyrrolo[2,3-d]pyrimidine derivatives of formula I wherein the symbols and substituents are as defined in the description, to processes for the preparation thereof, to pharmaceutical compositions ...
06/24/2008
7378417Pyrazolo-pyrimidine derivatives
The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5 and p are as defined in the description and to pharmaceutically acceptable salts thereof, t...
05/27/2008
7371750Compounds and compositions as protein kinase inhibitors
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or d...
05/13/2008
73684492-alkynyl- and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine Areceptor antagonists
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is
05/06/2008
7361659Pyrrazolo-pyrimidine derivatives
The present invention relates to pyrrazolo-pyrimidine derivatives of formula (I): wherein R1 to R4 and A are as defined in the specification, a process for the manufacture thereof, their use for treati...
04/22/2008
7348331Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones
Compounds of the Formula: where X1, Ar1, R1, and R2 are as defined herein, and compositions comprising the same. Also provided are methods for using compounds of Formula I in trea...
03/25/2008
7345046Heteroaryl-fused pyrimidinyl compounds as anticancer agents
Heteroaryl-fused pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the heteroaryl-fused pyrimidinyl compounds, either alone or in combination with at lea...
03/18/2008
7338955Medicament for treatment of neuropathies
Compounds of formula (I) in which R1=C1-6 alkyl, optionally halosubstituted; R2=H, C1-4 alkyl, optionally halosubstituted or replaced by halogen; R3=C2-4 alkyl, optionally halosubstituted; R4
03/04/2008
7329655Nitrogenous heterocyclic compounds
The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to ...
02/12/2008
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