Class 544/330 - At 2-position

Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the nitrogen is attached directly to the
No. of patents: 362
Last issue date: 05/15/2012

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Number	Title	Issue Date
8178672	Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described. ...	05/15/2012
8080659	CXCR4 antagonists including diazine and triazine structures for the treatment of medical disorders The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors or for the treatment of viral infecti...	12/20/2011
8063211	Rosuvastatin and salts thereof free of rosuvastatin alkylether and a process for the preparation thereof The present invention provides rosuvastatin and intermediates thereof having a low level of alkylether impurity and processes for the preparation thereof. ...	11/22/2011
8034932	Chemical process A process for formation of a compound of formula (I) or a pharmaceutically acceptable salt thereof, (A chemical formula should be inserted here—please see paper copy enclosed herewith) I via a Heck reaction is described. Intermediates useful in the process and pro...	10/11/2011
7919618	Synthesis of piperazines, piperidines and related compounds Novel methods of synthesizing piperazines, piperidines and related compounds are disclosed, as are compounds useful for their preparation. ...	04/05/2011
7834182	Piperidine derivative Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/conge...	11/16/2010
7799915	Anilino-pyrimidine analogs The present invention relates to compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are defined herein. ...	09/21/2010
7563894	Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments c...	07/21/2009
7538215	Compounds which inhibit leukocyte adhesion mediated by VLA-4 Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su...	05/26/2009
7423148	Small molecule PI 3-kinase inhibitors and methods of their use Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable ca...	09/09/2008
7414011	Phenylsulfonyl ureas, process for their preparation and their use as herbicides and plant growth regulators Disclosed are compounds of the formula (I) or salts thereof in which R1, R2, R3, R4, I, R5, Q, R4, W, X, Y, V and Z, are as defined in the specification, whi...	08/19/2008
7414046	Gyrase inhibitors and uses thereof The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also re...	08/19/2008
7399856	Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-2pyrimidinyl]amino]benzonitrile Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are pr...	07/15/2008
7396927	Process 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
7396836	Pyrimidine 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
7371759	HMG-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
RE40245	Gyrase inhibitors and uses thereof The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates ...	04/15/2008
7358239	Pyrrolidinyl, 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
7358359	Antibacterial agents Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacteria...	04/15/2008
7351711	Tricyclic indanyls as integrin inhibitors The present invention is directed to substituted indanyl compounds of Formula (I): Useful for treating integrin-mediated disorders such as, but not limited to unstable angina, thromboemboic disorders, osteoporosis, growth a...	04/01/2008
7348335	Compositions useful as inhibitors of JAK and other protein kinases The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and metho...	03/25/2008
7332485	Peptide deformylase inhibitors Novel PDF inhibitors and novel methods for their use are provided. ...	02/19/2008
7321033	3-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
7312227	Compositions useful as inhibitors of JAK and other protein kinases The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the inventio...	12/25/2007
7312329	Process for the preparation of pyrimidine derivatives An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R	12/25/2007
7312216	N-phenyl-2-pyrimidine-amine derivatives The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments compris...	12/25/2007
7309704	Heteroaryl urea neuropeptide Y Y5 receptor antagonists The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obes...	12/18/2007
7304156	Preparation of aminopyrimidine compounds A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; ...	12/04/2007
7288544	Pyrimidine compounds useful as N-type calcium channel antagonists Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally. They are useful as therapeutic agents for pains ...	10/30/2007
7279576	Anti-cancer medicaments Novel compounds and methods of using those compounds for the treatment of oncological conditions are provided. In a preferred embodiment, modulation of the activation states of abl or bcr-abl α-kinase proteins comprises the step of contacting the kinase proteins wi...	10/09/2007
7279577	Method for producing 2-anilino-4,6-dimethylpyrimidine In this method for producing 2-anilino-4,6-dimethylpyrimidine by reacting phenylguanidine and/or one of its salts with acetylacetone the reaction takes place in the presence of water and/or without separating the amounts of water that are formed during the reaction....	10/09/2007
7276510	HIV 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
7265115	Diazabicyclic CNS active agents Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals. ...	09/04/2007
7256190	Thiazole 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
7217716	N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain ...	05/15/2007
7205297	Substituted 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
7202236	Modified release pharmaceutical formulation A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R1 represents C?1-2#191 alkyl substituted by one or more fluoro substituents; R2 represents hydrogen, hydroxy, methoxy or ethoxy;...	04/10/2007
7176312	Kinase inhibitor scaffolds and methods for their preparation General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor...	02/13/2007
7129233	Mandelic acid derivatives and their use as thrombin inhibitors There is provided a compound of formula I wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically-acceptable derivatives (including pro...	10/31/2006
7122670	Selective synthesis of CF3-substituted pyrimidines The present invention relates to a method of making a compound of the formula wherein X1, X2 and R3—R4 are as defined herein. The method includes reacting a compound ...	10/17/2006

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Class 544/330 - At 2-position