Abstract: Compounds of the formula (I): wherein variable groups are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
Type:
Application
Filed:
March 7, 2006
Publication date:
September 17, 2009
Inventors:
David Andrews, Maurice Raymond Finlay, Clive Green, Clifford Jones, Vibha Oza
Abstract: A compound of formula 1 efficiently inhibits several protein kinases including glycogen synthase kinase 3 (GSK), aurora kinase, extracellular signal-regulated kinase (ERK), protein kinase B (AKT), and the likes, to control signal transductions involved in variable disorders such as diabetes, obesity, dementia, cancer, and inflammation.
Type:
Application
Filed:
December 22, 2006
Publication date:
September 10, 2009
Inventors:
Boonsaeng Park, Mi Jung Lee, Yu-Mi Song, Do Young Lee, Seung Chul Lee, Cheol Min Kim, Seoggu Ro, Joeng Myung Cho
Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.
Abstract: The invention relates to diastereomerically pure rosuvastatin and processes for preparing diastereomerically pure rosuvastatin and its intermediates.
Type:
Grant
Filed:
September 12, 2006
Date of Patent:
September 1, 2009
Assignee:
Teva Pharmaceutical Industries Ltd.
Inventors:
Valerie Niddam-Hildesheim, Natalia Shenkar, Kobi Chen, Anna Balanov
Abstract: The present invention relates to compounds of formula (I) or formula (II), or pharmaceutically acceptable salts thereof. Further aspects relate to pharmaceutical compositions comprising compounds according to the invention, and the use of said compounds in the preparation of a medicament for treating a variety of disorders, including proliferative disorders, viral disorders, stroke, etc.
Type:
Application
Filed:
October 9, 2006
Publication date:
August 27, 2009
Applicant:
Cyclacel Limited
Inventors:
Gavin Wood, Christopher Meades, Peter Martin Fischer, Shudong Wang, Kenneth Duncan, Daniella I. Zheleva, Campbell Mcinnes, Mark Thomas
Abstract: The present invention provides compounds of formula (1) wherein R1, R2, R3 and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Application
Filed:
November 20, 2008
Publication date:
August 20, 2009
Applicant:
AstraZeneca AB
Inventors:
Nicholas J. BENNETT, Thomas MCINALLY, Tobias MOCHEL, Stephen THOM, Anna-Karin TIDEN
Abstract: The present invention relates to methods and systems for de novo iterative synthesis, an automated iterative drug discovery method and system providing for rapid identification and synthesis of novel compounds.
Type:
Application
Filed:
June 18, 2007
Publication date:
August 20, 2009
Applicant:
Cresset Biomolecular Discovery, Ltd.
Inventors:
Brian Warrington, Jeremy Vinter, Mark Mackey
Abstract: The present invention provides rosuvastatin and intermediates thereof having a low level of alkylether impurity and processes for the preparation thereof.
Type:
Application
Filed:
March 11, 2009
Publication date:
August 20, 2009
Inventors:
Valerie Niddam-Hildesheim, Anna Balanov, Natalia Shenkar
Abstract: Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
Type:
Grant
Filed:
June 22, 2005
Date of Patent:
August 4, 2009
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Andreas Termin, Esther Martinborough, Nicole Zimmerman, Charles Cohen, Corey Gutierrez
Abstract: Multicyclic compounds and pharmaceutical compositions comprising them are described, along with methods of their use in the treatment of diseases such as age-associated memory impairment, Alzheimer's disease, Attention-Deficit/Hyperactivity Disorder (ADD/ADHD), autism, Down syndrome, Fragile X syndrome, Huntington's disease, Parkinson's disease, and schizophrenia.
Type:
Application
Filed:
March 24, 2009
Publication date:
July 16, 2009
Inventors:
Joseph Barbosa, Yingzhi Bi, Cynthia Anne Fink, Michael Alan Green, Jian Cheng Wang
Abstract: The present invention provides stereoisomers and stereoisomeric mixtures of 3-amino carbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.
Abstract: The present invention concerns a compound of formula (I) or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R1, R2, Ar?, A and B are defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
Type:
Application
Filed:
July 28, 2008
Publication date:
June 25, 2009
Inventors:
Ian Bruce, Andrew Dunstan, Thomas Anthony Hunt, Catherine Howsham
Abstract: The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
Type:
Application
Filed:
December 4, 2006
Publication date:
June 11, 2009
Inventors:
David Edward Uehling, Robert Dale Hubbard, Alex Gregory Waterson, Kimberly Petrov, Neil Bifulco, JR., Joseph Wendell Wilson, Jennifer Gabriel Badiang, Mui Cheung, Mariko Yamabe
Abstract: The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
Type:
Application
Filed:
February 5, 2009
Publication date:
June 11, 2009
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Heinz STADTMUELLER, Harald ENGELHARDT, Martin STEEGMAIER, Anke BAUM, Ulrich GUERTLER, Andreas SCHOOP, Jens Juergen QUANT, Flavio SOLCA, Rudolf HAUPTMANN, Ulrich REISER, Stephan Karl ZAHN, Lars HERFURTH
Abstract: The present invention relates to a compound of formula I and derivatives thereof. Furthermore, the invention relates to the use of such compounds as medicaments. In addition, the invention relates to the use of such compounds for manufacturing a medicament useful for treating proliferative diseases.
Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.
Type:
Application
Filed:
November 20, 2008
Publication date:
May 28, 2009
Applicant:
DECODE GENETICS EHF
Inventors:
Jasbir Singh, Mark E. Gurney, Alex Burgin, Alexander Kiselyov, Munagala Rao, Timothy Hagen
Abstract: Antitumoural compounds of general formula (I); wherein Ar is an heterocyclic group of formula (a) and R1, R2, R3, R4, R5, R6, R7, n and the dotted line take permitted meanings can be obtained from a tunicate of the family Polyclinidae, genus Aplidium, species cyaneum, and the invention further provides derivatives thereof.
Type:
Application
Filed:
November 13, 2006
Publication date:
May 14, 2009
Applicant:
PHARMA MAR, S.A.
Inventors:
Jose Fernando Reyes Benitez, Andres Francesch Solloso, Carmen Cuevas Marchante, Marta Altuna Urquijo, Daniel Pla Queral, Mercedes Alvarez Domingo, Fernando Albericio Palomera
Abstract: A pure amorphous form of rosuvastatin calcium substantially free from alkali metal impurities is disclosed. A process of preparing a pure amorphous form of rosuvastatin calcium is disclosed, which comprises hydrolysis of C1-C5 alkyl esters of rosuvastatin, preferably tert-butyl ester of rosuvastatin, with an organic nitrogen base, e.g. guanidines, amidines, amines and quaternary ammonium hydroxides, in the presence of water, optionally containing aprotic solvent, following the conversion of thus obtained rosuvastatin salt with a source of calcium to obtain rosuvastatin calcium, which is then isolated. An alternative process is disclosed, which comprises the conversion of numerous novel ammonium salts of rosuvastatin, preferably tert-octylammonium salt of rosuvastatin, with the source of calcium to desired commercial rosuvastatin calcium. Rosuvastatin calcium is an inhibitor of HMG CoA reductase, useful in the treatment of hyperlipidemia, hypercholesterolemia and atherosclerosis.
Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, two or more ring constitutional atoms of the heterocyclic group are a nitrogen atom, and the heterocyclic group may be substituted with at least one group selected from the group consisting of a C1-C3 alkyl group etc.], and a plant disease controlling agent comprising this as an active ingredient.
Abstract: A process for the preparation of a compound of Formula (I) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1—CO—CH2-E with a compound of formula R2—CHX1X2 in the presence of a compound of formula R3R4N—C(?NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidising the dihydropyrimidine to form the compound of Formula (1). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, and aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ?O.
Abstract: The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus, fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii. These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
Type:
Application
Filed:
June 4, 2008
Publication date:
April 23, 2009
Applicant:
University of Connecticut
Inventors:
Amy C. Anderson, Dennis L. Wright, Phillip M. Pelphrey, Tammy M. Joska, Erin S.D. Bolstad, David B. Bolstad, Veljko Popov
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
Type:
Application
Filed:
October 26, 2005
Publication date:
April 9, 2009
Applicant:
ASTRAZENECA AB
Inventors:
Hakan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepisto
Abstract: The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
Type:
Grant
Filed:
February 11, 2004
Date of Patent:
April 7, 2009
Assignee:
SmithKline Beecham Corporation
Inventors:
Ronda Davis-Ward, Robert Anthony Mook, Jr., Michael J Neeb, James M Salovich
Abstract: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl)(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.
Abstract: The present application describes deuterium-enriched rosuvastatin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Abstract: The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with t-butoxybisdimethylaminomethane, dimethylformamidedimethylacetal or dimethylformamidediethylacetal to produce a dialkylaminomethylene compound represented by the formula (2), reacting the compound of formula (2) in the presence of an acid to produce a hydroxymethylene compound represented by the formula (3), and reacting the compound of formula (3) with an amidine compound represented by the formula (4) or a salt thereof.
Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.
Type:
Application
Filed:
November 21, 2007
Publication date:
March 19, 2009
Inventors:
Jiazhong Zhang, Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Guoxian Wu, Hongyao Zhu, Marika Nespi, Chao Zhang
Abstract: Compounds of Formula (I); in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
Type:
Application
Filed:
October 31, 2005
Publication date:
February 19, 2009
Inventors:
Neil John Press, Stephen Paul Collingwood, Urs Baettig, Brian Cox, Sudhakar Devidasrao Garad, Hyungchul Kim, Dimitris Papoutsakis, Simon James Watson
Abstract: A compound represented by the following formula (I), a salt, or a solvate thereof: wherein, R1 and R2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a non-aromatic heterocyclic group, an aromatic hydrocarbon cyclic group, an aromatic heterocyclic group, an acyl group or an alkylsulfonyl group all of which may be substituted and wherein one, or both, of R1 or R2 is an aromatic, or non-aromatic, heterocyclic group which may be substituted; R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, an aromatic heterocyclic group, a nitrogen atom, an oxygen atom or a sulfur atom all of which may be substituted if possible; and R4 is a pyridyl group which may be substituted.
Abstract: The invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.
Type:
Application
Filed:
July 11, 2008
Publication date:
January 29, 2009
Applicant:
Dow AgroSciences LLC
Inventors:
Benjamin M. Nugent, Ann M. Buysse, Jonathan M. Babcock, Matthias S. Ober, Timothy P. Martin
Abstract: Compounds of formulae: (I), (II), (IIIa), (IIIb), (IVa) and (IVb): or a pharmaceutically acceptable salt thereof, for use as pharmaceuticals, in particular for the treatment of a condition alleviated by antagonism of a 5-HT2B receptor.
Type:
Application
Filed:
July 23, 2004
Publication date:
January 15, 2009
Applicant:
ASTERAND UK LIMITED
Inventors:
Richard Anthony Borman, Robert Alexander Coleman, Kenneth Lyle Clark, Alexander William Oxford, George Hynd, Janet Ann Archer, Amanda Aley, Neil Victor Harris
Abstract: Particulate (3?-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl)methanone is disclosed. Also disclosed are pharmaceutical formulations and dosage forms comprising particulate (3?-chlorobiphenyl-4-yl)(1-(pyrimidin-2-yl)piperidin-4-yl) and methods of their use.
Abstract: The invention relates to novel compounds with formula I and their use in stabilization of Factor Vila or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof.
Type:
Application
Filed:
February 24, 2006
Publication date:
December 18, 2008
Inventors:
Anders Klarskov Petersen, Andrew Neil Bowler
Abstract: The present invention relates to novel intermediates useful for the preparation of novel phenylaminopyrimidine derivatives, novel phenylaminopyrimidine derivatives. Pharmaceutical composition containing the novel phenylaminopyrimidine derivatives and processes for their preparation. The invention particularly relates to novel Phenyl pyrimidine amine derivatives of the general formula (I). The novel compounds of the formula 1 can be used in the therapy of Chronic Myeloid Leukemia (CML). Since the IC50; 191 values of these molecules are in the range 0.1 to 10.0 nm, these novel compounds are potentially useful for the treatment of CML. The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and their use as anti tumor agent in humans.
Type:
Application
Filed:
March 4, 2008
Publication date:
December 11, 2008
Applicant:
Natco Pharma Limited
Inventors:
Amala Kishan KOMPELLA, Bhujanga Rao ADIBHATLA KALI SATYA, Sreenivas RACHAKONDA, Nannapaneni VENKAIAH CHOWDARY
Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
Type:
Application
Filed:
February 12, 2008
Publication date:
December 11, 2008
Inventors:
Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
Abstract: Stating nitro derivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for treating and/or preventing several diseases, in particular coronary syndromes, neurodegenerative disorders as well as for reducing cholesterol levels.
Type:
Grant
Filed:
October 5, 2007
Date of Patent:
December 9, 2008
Assignee:
Nicox S.A.
Inventors:
Francesca Benedini, Ennio Ongini, Piero Del Soldato
Abstract: The present invention relates to a compound of the formula 1 wherein R1-R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
Type:
Application
Filed:
July 29, 2008
Publication date:
December 4, 2008
Inventors:
John Charles Kath, Michael Joseph Luzzio
Abstract: A novel synthesis of statins uses Wittig reaction of a heterocyclic core of statin with a lactonized side chain already possessing needed stereochemistry. Any separation of diastereoisomers is performed early in the course of synthesis.
Abstract: Compounds of Formula (I): (formula) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
Type:
Application
Filed:
November 11, 2006
Publication date:
November 27, 2008
Inventors:
Matthew Colin Thor Fyfe, Martin James Procter
Abstract: The present invention relates to substituted pyrimidines of formula I, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders and/or viral disorders.
Type:
Application
Filed:
July 29, 2008
Publication date:
November 20, 2008
Applicant:
Cyclacel Limited
Inventors:
Shudong Wang, Christopher Meades, Gavin Wood, Janice O'Boyle, Campbell McInnes, Peter Martin Fischer
Abstract: The disclosure relates to compounds of formula (I): wherein R1-R5, A and Y are as defined in the disclosure, to compositions comprising said compounds, and to processes for making and methods of using the same.
Type:
Application
Filed:
January 9, 2008
Publication date:
October 30, 2008
Applicant:
sanofi-aventis
Inventors:
Michael Bosch, Monsif Bouaboula, Pierre Casellas, Samir Jegham, Serge Mignani, Jean-Flaubert Nguefack, Jacob-Alsboek Olsen, Bernard Tonnerre, Jean Wagnon
Abstract: Polymorphic forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.
Type:
Application
Filed:
July 18, 2006
Publication date:
October 30, 2008
Inventors:
Paul W. Manley, Wen-Chung Shieh, Paul Allen Sutton, Piotr H. Karpinski, Raeann Wu, Stephanie Monnier, Jorg Brozio