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Class 544/332 - Chalcogen attached indirectly to the diazine ring by nonionic bonding


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: 685
Last issue date: 04/03/2012


1                      
NumberTitleIssue Date
8148526Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof
The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6. ...
04/03/2012
8063213Production of rosuvastatin calcium salt
An improved process for the manufacture of (E)-7-[4-(4-flurophenyl)-6-isopropyl-2-[methyl(methylsulfony)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, Formula (1), which is useful for the production of a pharmaceutical useful in the treatm...
11/22/2011
7932387Crystalline forms of rosuvastatin calcium salt
Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid] (also known as rosuvastatin) calcium salt and hydrates can exist in new crystal forms B and C. These crystal forms provide a higher diver...
04/26/2011
7868169Crystalline rosuvastatin intermediate
Provided is a crystalline rosuvastatin intermediate and processes for preparation thereof. ...
01/11/2011
7566782Process for the preparation of rosuvastatin
The present invention relates to a process for the preparation of rosuvastatin calcium, a promising new HMG-CoA reductase inhibitor. ...
07/28/2009
7442699Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are...
10/28/2008
7396927Process for preparation of rosuvastatin calcium
The present invention provides processes for preparing calcium salts of statin, particularly rosuvastatin calcium salt substantially free of impurities on an industrial scale. ...
07/08/2008
7396836Pyrimidine compound and medicinal composition thereof
A compound having excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, R1 and R2
07/08/2008
7371759HMG-CoA reductase inhibitors and method
Compounds are provided having the following structure which are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treat...
05/13/2008
7368569Process for making spirolactone compounds
This invention relates to a process for making spirolactone compounds analogous to formula I ...
05/06/2008
73684556,7-Dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines
The present invention relates to 2-(4-fluorophenyl)-3-(2-phenoxy-pyrimidin-4-yl)-6,7-dihydro-5H-pyrazolo-[1,2-a]pyrazol-1-one, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, having the formula: ...
05/06/2008
7358239Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is...
04/15/2008
7348333Cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists
There are described cycloalkyl derivatives of the formula (I) R1—Y-A-B-D-E-F-G  (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds a...
03/25/2008
7338958Sulfoximine-substituted pyrimidines as CDK-and/or VEGF inhibitors, their production and use as pharmaceutical agents
This invention relates to pyrimidine derivatives of general formula I in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, ...
03/04/2008
73210333-B-D-ribofuranosylthiazolo [4,5-] pyrimidine nucleosides and uses thereof
The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compou...
01/22/2008
7304071Protein kinase inhibitors and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formulae I and V: or a pharmaceutically acceptable salt thereof, wherein Ring B, Z1, Z2, U, T, m, n, p,...
12/04/2007
7304072Spiro compounds
Compounds represented by the general formula (I) wherein Ar1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom o...
12/04/2007
7300940Integrin α-v β-3 antagonists for use in imaging and therapy
Integrin receptor antagonists whose molecular structure includes a tetrahydropyridimidinylaminoethyloxybenzoyl group on a sulfonylamino-β-alanine nucleus exhibit increased binding affinity for the αvβ3 receptor when further substituted on the sulfonyl moiety with...
11/27/2007
7279582Retroviral protease inhibiting compounds
A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed. ...
10/09/2007
7276510HIV replication inhibitors
This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, provided that whe...
10/02/2007
7271181Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
09/18/2007
7265115Diazabicyclic CNS active agents
Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals. ...
09/04/2007
7256190Thiazole compounds useful as inhibitors of protein kinase
The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3, Aurora2, and Syk ma...
08/14/2007
72355511,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
Novel substituted pyrimidol[4,5-d]pyrimidin-2-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
06/26/2007
7230002Dipeptidyl peptidase IV inhibitors; processes for their preparation and compositions thereof
The present invention relates to novel dipeptidyl peptidase IV (DPP-IV) inhibitors their analogs, isomers, pharmaceutical compositions, therapeutic uses and methods of making the same. ...
06/12/2007
7223868Heteroaromatic glucokinase activators
2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the ...
05/29/2007
7223760Substituted triazole compounds
Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
05/29/2007
7208510Fungicidal combinations of active substances
The present invention relates to fungicidally active compound combinations of a fluorobenzothiazole derivative of the formula (I) and at least one of the compounds listed in the disclosure. ...
04/24/2007
7205297Substituted 5-alkynyl pyrimidines having neurotrophic activity
The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy, particularly in the treatment of neurodegenerative or other neurological di...
04/17/2007
7183288Amide derivatives as glycogen synthase kinase 3-β inhibitors
This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered hetero...
02/27/2007
7176199Aryl-substituted alicyclic compound and medical composition comprising the same
An aryl-substituted alicyclic compound of the formula (I): wherein U is 1,4,5,6-tetrahydropyrimidin-2-yl, etc., A is phenylene, etc., B is piperidine-1,4-diyl, etc., Z is —CONH—, etc., R3 is hydrog...
02/13/2007
7169802Fused pyrrolocarbazoles
The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrol...
01/30/2007
7161004Processes to produce intermediates for rosuvastatin
Intermediate compounds for preparing rosuvastatin are prepared by a process comprising oxidizing hydroxy groups to aldehyde groups, using sodium hypochlorite and 2,2,6,6-tetramethyl piperidinyl oxy free radical (TEMPO) as a catalyst. ...
01/09/2007
7153815Insecticide containing hydrazone derivative as the active ingredient and novel hydrazone derivative
A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxya...
12/26/2006
7129238Mandelic acid derivatives
The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acc...
10/31/2006
7129352Crystalline salts of 7-′4-(4-fluorophenyl) -6-isopropyl-2-′methyl (methylsulfonyl) amino!pyrimidin-5-yl!- (3R, 5S) -3, 5-dihydroxyhept-6-enoic acid
The invention relates to crystalline salts of the compound (E)-7-[4-(4-fluorophenyl)isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoic acid of formula (I), as well as processes for their manufacture, pharmaceutical composition...
10/31/2006
7122544Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6
10/17/2006
7115593Fungicidal combinations of active substances
The present invention relates to active compound combinations of a fluorobenzo-thiazole of the formula (I) and at least one of the compounds listed herein. The active compound combinations of the present inventio...
10/03/2006
7109243Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present inven...
09/19/2006
7098336FXR NR1H4 nuclear receptor binding compounds
The invention provides compounds according to the general formula (1) which bind to the NR1H4 receptor and act as agonists, antagonists or mixed agonists/antagonists of the NR1H4 receptor. The invention further provides methods of ...
08/29/2006
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