Abstract: The present invention relates to indolone-acetamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as for the treatment of epilepsy, epileptogenesis, seizure disorders and convulsion.
Abstract: The invention relates to compounds of the general formula (I) wherein Ar, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, W, a, b, m, n, o and p are as defined in claim 1, and to any enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are particularly suitable for controlling parasites in warm-blooded animals.
Type:
Grant
Filed:
June 9, 2005
Date of Patent:
January 5, 2010
Assignee:
Novartis AG
Inventors:
Noëlle Gauvry, Pierre Ducray, Thomas Goebel, Ronald Kaminsky
Abstract: The present invention relates to nitrooxyderivatives or salts thereof having the following general formula (I): R—NR1c—(K)k0—(B)b0—(C)c0—NO2??(I) wherein c0, b0 and k0 are 0 or 1; R is the radical of an analgesic drug for chronic pain, for instance neurophatic pain; R1c is H or alkyl with from 1 to 5 carbon atoms; B is such that its precursor is selected from amino acids, hydroxy acids, polyalcohol, compounds; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.
Type:
Grant
Filed:
December 3, 2003
Date of Patent:
January 5, 2010
Assignee:
Nicox S.A.
Inventors:
Ennio Ongini, Nicoletta Almirante, Piero Del Soldata
Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms; and R3 is selected from hydroxy and —NRN1RN2, where RN1 and RN2 are independently selected from hydrogen, optionally substituted C1-7 alkyl groups, optionally substituted C3-20 heterocyclyl groups and optionally substituted C5-20 aryl groups, or together form, along with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing heterocyclic ring having from 4 to 8 ring atoms, and its use in inhibiting ATM.
Type:
Grant
Filed:
February 9, 2006
Date of Patent:
January 5, 2010
Assignee:
Kudos Pharmaceuticals Limited
Inventors:
Marc Geoffrey Hummersone, Keith Allan Menear, Laurent Jean Martin Rigoreau, Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Roger John Griffin
Abstract: The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein: W, A, Y, Z, R101 and R200 are described in the specification.
Type:
Grant
Filed:
September 12, 2006
Date of Patent:
January 5, 2010
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Mark R. Player, Hui Huang, Daniel A. Hutta, Renee L. DesJarlais
Abstract: Pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound with the formula: where the labeled substituents are as described herein.
Type:
Grant
Filed:
May 13, 2004
Date of Patent:
December 29, 2009
Assignee:
Takeda San Diego, Inc.
Inventors:
Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Michael B. Wallace, Xiao-Yi Xiao, Zhiyuan Zhang
Abstract: The present invention relates to a benzofuran compound of the formula (I) wherein each symbol is as defined in the description, a pharmaceutically acceptable salt thereof and the like. The compound of the present invention has superior leukotriene inhibitory action, BLT2 competitive inhibitory action, BLT2 blocking action, action for the prophylaxis or treatment of allergy, action for the prophylaxis or treatment of asthma and action for the prophylaxis or treatment of inflammation, and is useful as an agent for the prophylaxis or treatment of diseases such as allergic disease, asthma, inflammation and the like, and other diseases.
Abstract: There are provided compounds of the general formulas wherein X, Y, R1, R2, R3 and R4 are as described herein. The compounds exhibit anticancer activity.
Abstract: A process for preparing 2-amino-6-alkyl-amino-4,5,6,7-tetrahydrobenzothiazoles of formula (I) wherein the asterisk (*) represents an asymmetric carbon and R1 is C1-C6 alkyl; and enantiomers and mixtures thereof, and their solvates, hydrates and pharmaceutically acceptable salts. The process involves (a) reacting with a secondary amine, optionally in the presence of an acid and a first solvent, to form an enamine; (b) optionally removing the acid and first solvent, and then reacting the enamine with sulfur in the presence of a second solvent; and (c) reacting the previously obtained compound with cyanamide to obtain the formula (I) compound. Pramipexole, a dopamine D-2 agonist, can be made by such process, and is useful for the treatment of Parkinson's disease and schizophrenia.
Abstract: The present invention relates to 3-guanidinocarbonyl-1-heteroaryl-indole derivatives, pharmaceutical compositions comprising such derivatives, methods of treatment comprising administering such derivatives, and processes for their preparation.
Abstract: Substituted pyrrolidine compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteoporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin family of compounds. In a preferred aspect, a substituted pyrrolidine compound is administered to a subject in coordination with a phosphodiesterase inhibitor compound.
Type:
Grant
Filed:
November 21, 2007
Date of Patent:
December 22, 2009
Assignee:
Laboratoires Serono SA
Inventors:
Yihua Liao, Zhong Zhao, Gian Luca Araldi
Abstract: The instant invention provides compounds of formula: (I) which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cyto-protective agents.
Inventors:
Lin Chu, Mark T. Goulet, Feroze Ujjainwalla, Linda Chang, Richard Frenette, Yves Girard, Michel Therien, Dwight Macdonald, John H. Hutchinson
Abstract: This invention pertains to compounds of Formula I, their N-oxides and suitable salts wherein A is O or S; G is a 5- or 6-membered heteroaromatic ring or a 5- or 6-membered nonaromatic heterocyclic ring optionally including one or two ring members selected from the group consisting of C(?O), SO or S(O)2, each ring optionally substituted with from one to four R2; each J is independently a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system, wherein each ring or ring system is optionally substituted with from one to four R3; and R1, R2, R3, R4 and n are as defined in the disclosure. A composition comprising a compound of Formula I, and a method for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I are also disclosed.
Type:
Grant
Filed:
December 19, 2007
Date of Patent:
December 8, 2009
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
David Alan Clark, Bruce Lawrence Finkelstein, George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
Abstract: The invention relates to a method of treatment and/or prophylaxis of diseases and conditions mediated by peroxysome proliferator-activated receptor gamma (PPAR?) in a mammal subject in need thereof, said method comprising administration to said mammal a compound of formula (I) or a pharmaceutically acceptable salt thereof in a therapeutically or prophylactically effective amount wherein in formula (I) W represents a COOH group or its bioisosters, or COO—C1-C4-alkyl group; Y represents NH or N—C1-C10-alkyl; Z represents NH, N—C1-C10-alkyl, N-aryl, N-heteroaryl, S, or O; X represents O, S, NH, N—C1-C10-alkyl, N-aryl, NSO2—C1-C10-alkyl, N—SO2-aryl, or N S02-heteroaryl; R1 to R6 each independently represents a hydrogen atom or a substituent defined in the description; A is as defined in the description; n represents an integer from 0 to 4, inclusive. The compounds of formula (I) are the ligands of PPAR-gamma receptor.
Type:
Grant
Filed:
March 6, 2007
Date of Patent:
December 8, 2009
Assignee:
Adamed Sp. z o.o.
Inventors:
Zbigniew Majka, Katarzyna Ewa Rusin, Dominik Daniel Kludkiewicz, Krzysztof Kurowski, Katarzyna Joanna Matusiewicz, Tomasz Stawinski, Daniel Sulikowski, Piotr Kowalczyk
Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
March 16, 2005
Date of Patent:
December 8, 2009
Assignee:
Pfizer Inc
Inventors:
Alan Daniel Brown, Charlotte Alice Louise Lane, Paul Alan Glossop, David Anthony Price, Russell Andrew Lewthwaite, Mark Edward Bunnage, Kim James, Graham Lunn
Abstract: Alkoxy indolinone based acid and amide derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.
Abstract: The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate, etc.), and/or solvates thereof, compositions containing the aforementioned salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.
Type:
Grant
Filed:
June 25, 2007
Date of Patent:
December 1, 2009
Assignee:
SmithKline Beecham (Cork) Ltd
Inventors:
Christopher S. Brook, Wei Chen, Philip C. Dell'orco, Lee M. Katrincic, Ann Marie Louvet, Choon K. Oh, Paul G. Spoors, Christopher Werner
Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses of the compounds.
Type:
Grant
Filed:
August 9, 2006
Date of Patent:
December 1, 2009
Assignee:
Novartis Vaccines and Diagnostics, Inc.
Inventors:
Paul A. Barsanti, Yi Xia, Weibo Wang, Kris G. Mendenhall, Liana M. Lagniton, Savithri Ramurthy, Megan C. Phillips, Sharadha Subramanian, Rustum Boyce, Nathan M. Brammeier, Ryan Constantine, David Duhl, Annette O. Walter, Tinya J. Abrams, Paul A. Renhowe
Abstract: Disclosed are a novel dye, having a dispersant functional group to simultaneously exhibit a dye function and a dispersant function, and a dye-sensitized solar cell including the same. According to this invention, the dye may simultaneously manifest a dye function for absorbing light, made possible by being adsorbed on the entire surface of metal oxide particles, to thus produce excited electrons which are then transferred into a conduction band of metal oxide, and a dispersant function for preventing the agglomeration of the particles to thus improve the uniformity of the metal oxide particles in a paste and film density.
Type:
Grant
Filed:
November 16, 2006
Date of Patent:
December 1, 2009
Assignee:
Samsung Electronics Co., Ltd.
Inventors:
Eun Sung Lee, Won Cheol Jung, Sang Cheol Park, Young Jun Park, Jung Gyu Nam, Jin Young Bae