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Berch, Mark L.


Primary examiner statistics: 2687 patents; average approval time: 2686 days
Assistant examiner statistics: 242 patents; average approval time: 711 days

Patents as Primary Examiner

1                      
NumberTitleIssue Date
7678801Compounds
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
RE41149Optically 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
7662812Diazabicyclic 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
7517994Heterocyclic 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
7491722Pyridazin-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
7479558Process 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
7470688Phthalazinone 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
74706894-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
7465795Compounds 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
7462712Process 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
7462621Use 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
7459442Substituted 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
7459453Pyridazin-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
7459550Process 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
74562822-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
7456195Phenylglycinamide 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
7452990Intermediates 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
7452991Aztreonam 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
7452882Thyroid 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
7452894Purine 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
7446194Preparation 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
7446113Acetylenyl-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
7442710Substituted 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
7439359Small 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
7439240Purine-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
7439358Specific 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
7432370Chiral 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
7429595Acyl 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
7429662Red-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
7427680Fluorogenic 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
7425556Compounds 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
7425560Thioxanthine 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
7423042Compounds
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
7423041A1 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
74230301-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
7423038Compounds 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
7419973Phosphonocephem 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
7417143Process 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
7417036Crystal 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
7414053Dihydropteridione 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
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