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| Number | Title | Issue Date |
| 7678801 | Compounds Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use use in therapy as CSBP/RK/p38 kinase inhibitors. ... | 03/16/2010 |
| RE41149 | Optically active pyridonecarboxylic acid derivatives N1-(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: These... | 02/23/2010 |
| 7662812 | Diazabicyclic aryl derivatives and their use as chinolinergic ligands at nicotinic acetylcholine receptors This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the in... | 02/16/2010 |
| 7517994 | Heterocyclic inhibitors of MEK and methods of use thereof Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the spe... | 04/14/2009 |
| 7491722 | Pyridazin-3(2H)-one derivatives Pyridazin-3(2H)-one derivatives of formula (I) are found to inhibit PDE-4. R1, R2 and R4 are organic radicals, R3 is a cyclic group, and R5 is an ester or an aryl or heteroaryl group. | 02/17/2009 |
| 7479558 | Process for preparing pyrido[2,3-]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-]pyrimidin-2(1)-one derivatives The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2 o... | 01/20/2009 |
| 7470688 | Phthalazinone derivatives A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) ... | 12/30/2008 |
| 7470689 | 4-benzimidazol-2-ylpyridazin-3-one derivatives Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compound... | 12/30/2008 |
| 7465795 | Compounds and uses thereof This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof. These nove... | 12/16/2008 |
| 7462712 | Process for the preparation of imipenem The present invention relates to an improved process for the preparation of imipenem comprising reacting a bicyclo ketone precursor of the Formula II, wherein R is a protecting group, with a phosphorohalidate in the presenc... | 12/09/2008 |
| 7462621 | Use of 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 as therapeutic agents The invention relates to an use of pyrimidone derivative represented by formula (I) or a salt thereof: wherein m, n, p, X, Y, R1, R2, R3, R4 and R5 are as defined herein for treating a variety of disease states. More specif... | 12/09/2008 |
| 7459442 | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof The present invention provides compounds represented by the structural formula (I): or pharmaceutically acceptable isomers, salts, solvates or esters of the compound of Formula (I), wherein each of the substituents is as sp... | 12/02/2008 |
| 7459453 | Pyridazin-3(2)-one derivatives as PDE4 inhibitors New pyridazin-3(2H)-one derivatives having the chemical structure of general formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of phosphodiesterase 4. | 12/02/2008 |
| 7459550 | Process for the preparation of Cefditoren The present invention relates to an improved process for the preparation of Cefditoren of formula (I), the said process comprising the steps of: i) converting the compound of formula (II) to a compound of the formula (III) using TPP and sodium iodide in the presence... | 12/02/2008 |
| 7456282 | 2-amino-9-(2-substituted ethyl)purines and preparing methods for 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-aminopurine using the same The present invention relates to a new compound of 2-amino-9-(2-substituted ethyl)purine and an effective method for preparing 9-[4-acetoxy-3-(acetoxymethyl)but-1-yl]-2-aminopurin (famciclovir) using the same. The 2-amino-9-(2-substituted ethyl)purine according to t... | 11/25/2008 |
| 7456195 | Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, ... | 11/25/2008 |
| 7452990 | Intermediates for synthesis of cephalosporins and process for preparation of such intermediates A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics wherein X is chlorine or bromine; R is hydrogen, C | 11/18/2008 |
| 7452991 | Aztreonam β polymorph with very low residual solvent content The invention relates to the β polymorph of Aztreonam, which contains less than 2.5% by weight residual solvent and to a process of making said polymorph. In the process of the invention, a polymorph of Aztreonam is dissolved in an absolute C1-6 alcohol ... | 11/18/2008 |
| 7452882 | Thyroid hormone analogs Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi... | 11/18/2008 |
| 7452894 | Purine derivatives as purinergic receptor antagonists Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2 | 11/18/2008 |
| 7446194 | Preparation of penicillin procaine A process for preparing penicillin G procaine comprises the steps of introducing inactive ingredients into a first mixing tank and sterilizing the mixture of inactive ingredients in the first mixing tank. A procaine hydrochloride is dissolved in a second mixing tank... | 11/04/2008 |
| 7446113 | 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 the manufactu... | 11/04/2008 |
| 7442710 | Substituted phenyl methanones The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R″ and R1, R2,R3, R... | 10/28/2008 |
| 7439359 | Small molecule compositions for binding to hsp90 Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with a... | 10/21/2008 |
| 7439240 | Purine-or pyrrolol[2,3-d]pyrimidine-2-carbonitiles for treating diseases associated with cysteine protease activity The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases ... | 10/21/2008 |
| 7439358 | Specific salt, anhydrous and crystalline form of a dihydropteridione derivative The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pt... | 10/21/2008 |
| 7432370 | Chiral salt resolution The present application discloses compounds of the formula wherein R2 and R3 are as defined herein. The present application further discloses certain pyrrolol[2,3-d]pyrimidine ... | 10/07/2008 |
| 7429595 | Acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines and their use as antiproliferative agents The present invention is directed to acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4 -diaminocyclohexyl)-purines of the formula where Z is selected from the group consisting of —S(O)2—, and â€... | 09/30/2008 |
| 7429662 | Red-emitting electrophosphorescent devices This invention relates to an organic electroluminescence (EL) device and to the use of a tris-cyclometalated iridium complex with a 3-Phenyl-azine ligand for thin-film type organic electroluminescence devices. The iridium complexes used have the following for... | 09/30/2008 |
| 7427680 | Fluorogenic substrates for BETA-lactamase gene expression Fluorescent substrates for beta-lactamases having the general formula shown above are provided. Z includes a fluorophore or chromophore and includes a group that may link to the lactam-containing group; R1 and R2 are independently selected from... | 09/23/2008 |
| 7425556 | Compounds and uses thereof This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof. These nove... | 09/16/2008 |
| 7425560 | Thioxanthine derivatives as myeloperoxidase inhibitors There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for t... | 09/16/2008 |
| 7423042 | Compounds This invention relates to a novel group of 8-Alkyl/Aryl-4-aryl-2-N-(alkylamino)-N″-substituted-N′-cyanoguanidino-8H-pyrido[2,3-d]pyrimidin-7-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and p... | 09/09/2008 |
| 7423041 | A1 adenosine receptor antagonists Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described. ... | 09/09/2008 |
| 7423030 | 1-amino-phthalazine derivatives, the preparation and the therapeutic use thereof A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments u... | 09/09/2008 |
| 7423038 | Compounds 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... | 09/09/2008 |
| 7419973 | Phosphonocephem compound A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior... | 09/02/2008 |
| 7417143 | Process for the preparation of Tazobactam in pure form An improved process for the purification of tazobactam or its derivatives of the formula (I) wherein R represents hydrogen, C1-C6alkyl, p-methoxybenzyl, o-nitrobenzyl, p-nitrobenzyl, o-chlorobenzyl, be... | 08/26/2008 |
| 7417036 | Crystal form of adefovir dipivoxil and its preparation A new crystal form of adefovir dipivoxil {9-[2-[bis(pivaloyloxy)-methoxy]-phosphinyl]-methoxyl]-ethyl]-adenime} and its composition is disclosed, as is a method to prepare the crystal comprising placing adefovir dipivoxil in a round bottom flask, adding organic solv... | 08/26/2008 |
| 7414053 | Dihydropteridione derivatives, process for their manufacture and their use as medicament Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes f... | 08/19/2008 |