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| Number | Title | Issue Date |
| 8163903 | Process 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 |
| 8076479 | Process 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 |
| 7772394 | Zaleplon 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 |
| 7667036 | Pyrazolo[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 |
| 7566781 | Imidazopyridine 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 |
| 7429663 | 7-(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 |
| 7420056 | Substituted 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 |
| 7417041 | Imidazopyrimidines 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 |
| 7385056 | Synthesis 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 |
| 7378417 | Pyrazolo-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 |
| 7361659 | Pyrrazolo-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 |
| 7358249 | Heterocyclic 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 |
| 7351826 | Aryl 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 |
| 7351481 | Imidazole 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 |
| 7351822 | Serine 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 |
| 7351710 | Preparation 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 |
| 7348429 | Process 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 |
| 7329662 | Pyrazolo-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 |
| 7309705 | 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... | 12/18/2007 |
| 7304069 | Hydrate 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 |
| 7304068 | Substituted 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 |
| 7285555 | 6-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 |
| 7285666 | Pyrazolo[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 |
| 7273100 | Biodegradable 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 |
| 7271170 | Imidazo-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 |
| 7262199 | Tyrosine 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 |
| 7247626 | Pyrazolopyrimidine 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 |
| 7238699 | Imidazolyl 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 |
| 7238808 | Acetylenyl-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 |
| 7232827 | Heteroaryl 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 |
| 7214682 | Substituted 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 |
| 7211669 | Imidazolyl 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 |
| 7211572 | Nitrogen-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 |
| 7211545 | Imidazo[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 |
| 7205316 | Tri- 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 |
| 7205308 | Trisubstituted 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 |
| 7196078 | Trisubstituted 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 |
| 7196111 | Pyrazolo[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 |
| 7196092 | N-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 |