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Class 544/281 - Ring nitrogen is shared by the two cyclos


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which a ring nitrogen is a member of both of
No. of patents: 278
Last issue date: 04/24/2012


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NumberTitleIssue Date
8163903Process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluoro-phenyl]-N-methyl-acetamide
The present invention relates to a new process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluorophenyl]-N-methyl-acetamide (I) in a high yield and high purity, which is an intermediate in the synthesis of compounds with affinity for GABAA re...
04/24/2012
8076479Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates
Disclosed is a process for the synthesis of compounds of Formula I by sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1,
12/13/2011
7772394Zaleplon synthesis
A process for making zaleplon comprising alkylating 3-[3-(dimethylamino)-1-oxo-2-propenyl]-phenyl]-acetamide with ethyl iodide in the presence of an alkali metal hydroxide or alkoxide selected from sodium hydroxide, potassium hydroxide, sodium methoxide, sodium tert...
08/10/2010
7667036Pyrazolo[1,5-a]pyrimidine derivatives
The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent MAPKAP-K2 inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic...
02/23/2010
7566781Imidazopyridine compound
The present invention provides an imidazopyridine compound represented by formula (I), wherein R1 and R2 each independently represent a C1-6 alkyl group et al; R3 and R4
07/28/2009
74296637-(Pyrimidin-4-yl)-Imidazo[1,2-a]Pyrimidin-5(1H)-ones as GSK3β inhibitors
The invention relates to a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: R1 wherein X represents a bond, an ethenylene group, an ethenylene group, a methylene group optionally substituted; a carbonyl group, an oxygen at...
09/30/2008
7420056Substituted bicyclic imidazo-3-ylamine compounds
Substituted bicyclic imidazo-3-yl-amine compounds are provided, as well as processes for the production thereof and pharmaceutical formulations containing these compounds. The use of these compounds for the production of pharmaceutical formulations and related metho...
09/02/2008
7417041Imidazopyrimidines as transforming growth factor (TGF) inhibitors
Novel fused heteroaromatic 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 tran...
08/26/2008
7385056Synthesis of heteroaryl acetamides
An improved process for the preparation of a heteroaryl acetamide from a heteroaryl α-hydroxyacetamide is provied. The process comprises directly hydrogenating the heteroaryl α-hydroxyacetamide in the presence of a strong acid, a halide and a catalyst. In one embo...
06/10/2008
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
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
7358249Heterocyclic compounds having inhibitory activity against HIV integrase
A heterocyclic compound of the formula (I): wherein B1 is —C(R2)═ or —N═; R1′ is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R
04/15/2008
7351826Aryl acid pyrimidinyl methyl amides, pyridazinyl methyl amides and related compounds
The invention provides compounds of Formula (I) that bind to GABAA receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly...
04/01/2008
7351481Imidazole ring-containing compound and organic electroluminescence display device
The present invention is related to an imidazole ring-containing compound and an organic electroluminescence (EL) display device using the same. In particular, the imidazole ring-containing compound may be used alone or in combination with a dopant as a material for...
04/01/2008
7351822Serine protease inhibitors
Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovasc...
04/01/2008
7351710Preparation of amorphous form of indiplon
The present invention is directed to amorphous form of indiplon, to processes for preparing said amorphous form, to pharmaceutical compositions containing the same, and to method of treatment using the same. Additionally, the present invention also relates to the pr...
04/01/2008
7348429Process for purifying N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide(zaleplon) and crystalline forms of zaleplon accessible with the process
Provided are novel Zaleplon crystalline Forms II, III, IV and V, which are useful for the treatment of insomnia. Also provided are processes for making Forms I, II, and V using precipitation methods. ...
03/25/2008
7329662Pyrazolo-pyridine
The present invention relates to novel pyrazolo- and imidazo-pyrimidine derivatives of formula I wherein A, D, E, L, M, Q, R1, R2 and R3 are as defined hereinabove. The present in...
02/12/2008
7309705Pyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of...
12/18/2007
7304069Hydrate of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5α]-pyrimidin-7-yl}phenyl)acetamide and processes and methods related thereto
A novel hydrate form of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide (“Compound No. 1”) and processes related to the use thereof in the synthesis of a polymorphic form of Compound No. 1. ...
12/04/2007
7304068Substituted pyrazolo [1,5-A] pyrimidinyls and pharmaceutical uses therefore
The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. ...
12/04/2007
72855556-aryl-7-halo-imidazo[1,2-a]pyrimidines as anticancer agents
This invention relates to certain 6-aryl-7-halo-imidazo[1,2-a]pyrimidines or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for ...
10/23/2007
7285666Pyrazolo[1,5-a] pyridines and medicines containing the same
Compounds represented by the general formula: [wherein R1 represents methoxy, ethyl, methylthio, etc., R2, R3 and R4 each represent hydrogen, a halogen, etc., R5
10/23/2007
7273100Biodegradable dispersants for cement compositions and methods of cementing in subterranean formations
Methods of cementing in a subterranean formation may include the steps of: providing a cement composition comprising a cement, water, and a dispersant comprising a low molecular weight starch that comprises anionic groups; placing the cement composition in the subte...
09/25/2007
7271170Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands
Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and ...
09/18/2007
7262199Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...
08/28/2007
7247626Pyrazolopyrimidine derivatives and pharmaceutical compositions containing them
The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. ...
07/24/2007
7238699Imidazolyl derivatives as corticotropin releasing factor inhibitors
The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) usefu...
07/03/2007
7238808Acetylenyl-pyrazolo-pyrimidine derivatives
The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for th...
07/03/2007
7232827Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one derivatives
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group,...
06/19/2007
7214682Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido{1,2-a}pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo{1,2-a}pyrimidin-5(1h)one derivatives
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an et...
05/08/2007
7211669Imidazolyl derivatives as corticotropin releasing factor inhibitors
The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF receptor”) usefu...
05/01/2007
7211572Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt th...
05/01/2007
7211545Imidazo[1,2-a]pyrimidine and fungicidal compositions containing thereof
The imidazo[1,2-a]pyrimidines given by the following formula [I]: [wherein R1 and R2 represent a C1–C6 alkyl group optionally substituted by one or more selected from the group consisting ...
05/01/2007
7205316Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R...
04/17/2007
7205308Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of...
04/17/2007
7196078Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of...
03/27/2007
7196111Pyrazolo[1,5a]pyrimidine compounds as antiviral agents
The invention relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and...
03/27/2007
7196095(Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds
Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful in the treatment of cytokine mediated diseases such as arthritis and in the treatment and/or prevention of protozoal diseases such as coccidiosis
03/27/2007
7196092N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of...
03/27/2007
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