Patents Examined by Tamthom N. Truong
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Patent number: 8436006Abstract: The present invention is directed to novel 2-amino-3,4-dihydro-quinazoline derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE.Type: GrantFiled: August 4, 2005Date of Patent: May 7, 2013Assignee: Jansssen Pharmaceutica N.V.Inventors: Francois Paul Bischoff, Mirielle Braeken, Serge Maria Aloysius Pieters, Mark Hubert Mercken, Hans Louis Jos De Winter, Didier Jean-Claude Berthelot
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Patent number: 8138195Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: GrantFiled: April 20, 2005Date of Patent: March 20, 2012Assignee: ICOS CorporationInventors: Chanchal Sadhu, Kenneth O. Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Patent number: 7960387Abstract: The invention relates to dihydroquinazolines and methods for the production thereof, the use thereof in the treatment and/or prophylaxis of diseases, in addition to the use thereof in the production of medicaments in the treatment and/or prophylaxis of diseases, especially for use as anti-viral agents, especially against cytomegalo viruses.Type: GrantFiled: January 29, 2004Date of Patent: June 14, 2011Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Tobias Wunberg, Judith Baumeister, Ulrich Betz, Mario Jeske, Gerald Kleymann, Thomas Lampe, Susanne Nikolic, Jürgen Reefschläger, Rudolf Schohe-Loop, Frank Süβmeier, Holger Zimmermann, Rolf Grosser, Kerstin Henninger, Guy Hewlett, Jörg Keldenich, Thomas Krämer, Peter Nell, Tse-I Lin
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Patent number: 7943635Abstract: This invention comprises the novel compounds of formula (I) wherein r, t, Y1, Y2, R1, R2, R3, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: June 5, 2007Date of Patent: May 17, 2011Assignee: Janssen Pharmaceutica NVInventors: Patrick René Angibaud, Marc Gaston Venet, Christophe Meyer, Henry Joseph Breslin
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Patent number: 7939538Abstract: Compounds are provided having the formula: wherein variables Ra, R1, R2, R3, R4, A1, A4, L, Q, X and subscript n as described herein. The subject compounds are useful for treatment of inflammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.Type: GrantFiled: June 27, 2005Date of Patent: May 10, 2011Assignee: Amgen Inc.Inventors: Zice Fu, Michael G. Johnson, An-Rong Li, Andrew P. Marcus, Julio C. Medina, Philippe Bergeron, Xiaoqi Chen, Xiaohui Du, Jeffrey Deignan, Jason A. Duquette, Darin Gustin, Jeffrey T. Mihalic, Jiwen Liu
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Patent number: 7939539Abstract: Quinazolinone compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the quinazolinone compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the quinazolinone compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.Type: GrantFiled: November 24, 2004Date of Patent: May 10, 2011Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Weibo Wang, Liana M. Lagniton, Ryan N. Constantine, Manoj C. Desai
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Patent number: 7928107Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: March 3, 2006Date of Patent: April 19, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Andreas Termin, Jesus Gonzalez, Lev Fanning, Timothy Neubert, Paul Krenitsky, Pramod Joshi, Dennis Hurley, Urvi Sheth
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Patent number: 7906521Abstract: The present invention relates to compounds useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: September 17, 2004Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Richard Isaacs
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Patent number: 7893071Abstract: The present invention is directed to novel thalidomide derivative compounds that have activity as anti-angiogenic compounds. More particularly the compounds have the general structure: where R1 is selected from the group consisting of H, halo, alkyl, haloalkyl, —NH2, hydroxy and alkoxy; R2 is selected from the group consisting of optionally substituted bicyclic, optionally substituted aryl, and R6 is H, or C1-C8 alkyl; R19 is optionally substituted aryl; and m is 0-6.Type: GrantFiled: April 22, 2002Date of Patent: February 22, 2011Assignee: University of Virginia Patent FoundationInventor: Milton L. Brown
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Patent number: 7888366Abstract: 2,4-Diaminoquinazolines of formulae I-IV and VI are useful for treating spinal muscular atrophy (SMA).Type: GrantFiled: June 7, 2005Date of Patent: February 15, 2011Assignee: Families of Spinal Muscular AtrophyInventors: Jasbir Singh, Mark E. Gurney
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Patent number: 7838530Abstract: The invention concerns quinazoline derivatives of Formula (I), wherein each of R1a, R1b, R2, R3 and a have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.Type: GrantFiled: September 22, 2004Date of Patent: November 23, 2010Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Laurent Francois Andre Hennequin, Christopher Thomas Halsall
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Patent number: 7829566Abstract: Quinazolines of the formula I in which R, R1, R2, R3, R4 and Y have the meaning indicated in Patent Claim 1, and their salts or solvates as glycoprotein IbIX antagonists.Type: GrantFiled: December 14, 2005Date of Patent: November 9, 2010Inventors: Werner Mederski, Ralf Devant, Gerhard Barnickel, Sabine Bernotat-Danielowski, James Vickers, Bertram Cezanne, Daljit Dhanoa, Bao-Ping Zhao, James Rinker, Mark R. Player, Edward Jaeger, Richard Soll
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Patent number: 7825244Abstract: The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: wherein R1, R2, R99, and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.Type: GrantFiled: June 6, 2006Date of Patent: November 2, 2010Assignee: Janssen Pharmaceutica NVInventors: Nand Baindur, Michael David Gaul, Kevin Douglas Kreutter, Guozhang Xu
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Patent number: 7790733Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, and n are as described in the specification and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I can be used for the treatment of 5-HT5A receptor antagonists related diseases, which include depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, dementia in Parkinson's disease, neuroleptic-induced Parkinsonism and tardive dyskinesias, as well as other psychiatric disorders and gastrointestinal disorders such as irritable bowel syndrome.Type: GrantFiled: June 21, 2006Date of Patent: September 7, 2010Assignee: Hoffman-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
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Patent number: 7790732Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3 are as described in the specification and pharmaceutically acceptable acid addition salts and tautomers thereof. Compounds of formula I have good activity on the 5-HT5A receptor. Therefore, the invention provides a method for treating diseases related to this receptor, for example, anxiety, depression, sleep disorders and schizophrenia.Type: GrantFiled: June 21, 2006Date of Patent: September 7, 2010Assignee: Hoffman-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
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Patent number: 7781441Abstract: The present invention relates to compounds of formula I wherein R, R1, R2, R3, R4, aryl, n, and m are as defined in the specification and pharmaceutically acceptable acid addition salts and tautomeric forms thereof. Such compounds have good activity on the 5-HT5A receptor. Therefore, the invention provides methods for the treatment of certain CNS disorders with such compounds.Type: GrantFiled: April 27, 2006Date of Patent: August 24, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
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Patent number: 7772243Abstract: This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n—-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N (C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.Type: GrantFiled: May 5, 2005Date of Patent: August 10, 2010Assignee: Warner-Lambert Company LLCInventors: Stephen Alan Fakhoury, Helen Tsenwhei Lee, Jessica Elizabeth Reed, Kevin Matthew Schlosser, Karen Elaine Sexton, Haile Tecle, Roy Thomas Winters
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Patent number: 7772244Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: March 28, 2005Date of Patent: August 10, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Andrew P. Degnan, Xiaojun Han, Gene M. Dubowchik, John E. Macor, Stephen E. Mercer
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Patent number: RE43098Abstract: The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.Type: GrantFiled: October 2, 2007Date of Patent: January 10, 2012Assignee: Millennium Pharmaceuticals, Inc.Inventors: James Kanter, Anjali Pandey, James Robinson, Robert M. Scarborough, Carroll Scarborough, legal representative
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Patent number: RE43431Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction medType: GrantFiled: August 18, 2009Date of Patent: May 29, 2012Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca