Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): the pharmaceutically acceptable acid or base addition salts thereof, the quaternary amines thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of a bacterial disease including a mycobacterial disease, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of bacterial diseases and a process for preparing the claimed compounds.
Type:
Grant
Filed:
July 26, 2006
Date of Patent:
March 29, 2011
Assignee:
Janssen Pharmaceutica NV
Inventors:
Jérôme Emile Georges Guillemont, David Francis Alain Lançois, Elisabeth Thérèse Jeanne Pasquier, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
Abstract: The invention relates to a method for preparing a benzoxazinone comprising reacting an isatoic anhydride with an acylating compound in the presence of an N-alkyl imidazole, to a method for preparing a photo-stabilised composition, comprising adding a benzoxazinone and to the use of a benzoxazinone as a light-absorber or as a stabiliser for a light-sensitive compound.
Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.
Abstract: A 3,4-dihydrobenzoxazine compound of the present invention is represented by the following formula [1] (wherein X is a nitrogen atom or CR3; R1 is a hydrogen atom or a halogen atom; R2 is a C1-6 alkoxy group which may be substituted with the same or different 1 to 5 substituents selected from a halogen atom and a hydroxyl group; and R3 is a halogen atom. However, R1 is a halogen atom when X is CR3). This compound is effective in treating diseases to which the vanilloid receptor subtype 1 (VR1) activity is involved, such as pain, etc.
Abstract: Substituted fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines, and imidazo[4,5-c]pyridines) with a —CH(—R2)— group in the fused ring at the 2-position of the imidazo ring and a —CH(—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.
Type:
Grant
Filed:
July 12, 2007
Date of Patent:
March 15, 2011
Assignee:
3M Innovative Properties Company
Inventors:
George W. Griesgraber, Sarah C. Johannessen Slania
Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
Type:
Grant
Filed:
May 3, 2010
Date of Patent:
March 15, 2011
Assignee:
Abbott Laboratories
Inventors:
Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
Abstract: The present invention provides methods of use of oxadiazoanthracene derivatives of the formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, R, R1, R2, R3, R4 and R5 are as herein described, and wherein said methods of use include uses for the treatment and/or prevention of disorders and diseases, such as diabetes.
Type:
Grant
Filed:
August 3, 2010
Date of Patent:
March 15, 2011
Assignee:
TransTech Pharma, Inc.
Inventors:
Adnan M. M. Mjalli, Dharma Rao Polisetti, Thomas Scott Yokum, Kalpathy Santhosh, Mustafa Guzel, Christopher Behme, Stephen Thomas Davis
Abstract: Compounds of the formula (I), in which R1, R2, m, Q and B have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
Type:
Grant
Filed:
October 25, 2006
Date of Patent:
March 8, 2011
Assignee:
Merck Patent GmbH
Inventors:
Oliver Schadt, Dieter Dorsch, Melanie Schultz, Andree Blaukat
Abstract: The present invention provides a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, Ar2 represents a phenyl group that may be substituted with a C1-6 alkoxy group, or the like, X1 represents a double bond or the like, and Het represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, which is effective as a therapeutic or prophylactic agent for a disease caused by A?.
Abstract: A compound represented by the following Formula (1): wherein, Het1 represents a bivalent five- or six-membered aromatic heterocyclic residue and may further be substituted; Xa to Xd each independently represent a heteroatom and may further be substituted; Ya to Yf each independently represent a heteroatom or a carbon atom and may further be substituted; the ring bound to Het1 may have a double bond at any position.
Abstract: There is provided a CRF receptor antagonist comprising a compound of the formula (I): A-W—Ar??(I) wherein, A is a group represented by the formula (A1) or (A2): (wherein, ring Aa is a 5- or 6-membered ring which may be further substituted; ring Ab is a 5- or 6-membered ring which may be further substituted; ring Ac is a 5- or 6-membered ring which may be substituted; R1 is optionally substituted alkyl, substituted amino, substituted hydroxy, etc.; X is carbonyl, —O—, —S—, etc.; Y1, Y2 and Q are independently optionally substituted carbon or nitrogen; ?is a single or double bond); W is a bond, optionally substituted methylene, optionally substituted imino, —O—, —S—, etc.; Ar is optionally substituted aryl or optionally substituted heteroaryl; or a salt thereof or a prodrug thereof.
Type:
Grant
Filed:
April 6, 2005
Date of Patent:
March 1, 2011
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho, Timothy Mark Turner, Kazuyoshi Aso, Masakuni Kori, Michiyo Mochizuki, Kevin Ronald Condroski, Christopher Stephen Siedem, Steven Armen Boyd
Abstract: Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPAR? or PPAR?. In particular, the compounds of the invention modulate the function of PPAR? or PPAR?. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.
Type:
Grant
Filed:
November 12, 2008
Date of Patent:
February 22, 2011
Assignee:
Amgen Inc.
Inventors:
Philippe Bergeron, Christopher N. Farthing, Stuart D. Jones, John W. Liebeschuetz, Sarah E. Lively, Lawrence R. McGee, Sharon McKendry, David Sheppard, Stephen C. Young
Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives, compositions containing them, the use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity, and in the treatment of bacterial infections. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined herein and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
Type:
Grant
Filed:
November 6, 2008
Date of Patent:
February 22, 2011
Assignee:
GlaxoSmithKline LLC
Inventors:
Donghui Qin, Beth Norton, Andrew Nicholas Knox, Siegfried B. Christensen, Kelly M. Aubart
Abstract: This invention pertains generally to the field of phenothiazine compounds, and more particularly to certain stably reduced phenothiazine compounds, specifically, certain 3,7 diamino-10H-phenothiazine (DAPTZ) compounds of the following formula wherein: each of R1 and R9 is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of HX1 and HX2 is independently a protic acid; and pharmaceutically acceptable salts, solvates, and hydrates thereof. These compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs (for example, methythioninium chloride, MTC).
Type:
Grant
Filed:
March 28, 2007
Date of Patent:
February 15, 2011
Assignee:
Wista Laboratories Ltd.
Inventors:
Claude Michel Wischik, Janet Elizabeth Rickard, Charles Robert Harrington, David Horsley, John Mervyn David Storey, Colin Marshall, James Peter Sinclair, Thomas Craven Baddeley
Abstract: The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof in which R, R1, R2, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
Type:
Grant
Filed:
April 12, 2007
Date of Patent:
February 1, 2011
Assignee:
Novartis AG
Inventors:
Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stjepan Jelakovic, Stefan Stutz
Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
Type:
Grant
Filed:
January 29, 2010
Date of Patent:
February 1, 2011
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
Abstract: Provided herein are benzoxazinone compounds of formula I and compositions containing the compounds. The compounds and compositions are useful in the methods of inhibiting the action of serine hydrolase, including neutrophil elastase. In certain embodiments, the compounds and compositions are useful in the prevention, amelioration or treatment of serine hydrolase-mediated diseases.
Type:
Grant
Filed:
September 20, 2007
Date of Patent:
February 1, 2011
Assignee:
Kyorin Pharmaceutical Co.., Ltd.
Inventors:
Kevin Shreder, Yi Hu, Allister Fraser, Yasushi Kohno, Akihiko Kojima, Junichi Ishiyama