Quinazoline (including Hydrogenated)(i.e., The Second Cyclo In The Bicyclo Ring System Is An Ortho-fused Six-membered Carbocycle) Patents (Class 514/266.1)
  • Patent number: 8809354
    Abstract: Surprising antiviral activity of 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.
    Type: Grant
    Filed: December 31, 2011
    Date of Patent: August 19, 2014
    Inventors: Sheikh Riazuddin, Osman Ali, Usman Ashfaq, Shaheen N. Khan, Javed Akram, Atta-ur Rahman, M. Iqbal Choudhary, Khalid M. Khan, Zulfiqar Ali Khan
  • Patent number: 8809353
    Abstract: 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: Grant
    Filed: March 18, 2008
    Date of Patent: August 19, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Wilson, Lev T. D. Fanning, Paul Krenitsky, Andreas Termin, Pramod Joshi, Urvi Sheth
  • Patent number: 8802659
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: August 12, 2014
    Assignee: Biogen Idec MA Inc.
    Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
  • Patent number: 8802675
    Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.
    Type: Grant
    Filed: January 31, 2010
    Date of Patent: August 12, 2014
    Assignees: Technion Research and Development Foundation Ltd, Yeda Research and Development Company Ltd.
    Inventors: Moussa B. H. Youdim, Mati Fridkin, Hailin Zheng
  • Patent number: 8796180
    Abstract: The invention relates to aminoquinazoline compounds or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein A1, A2, A3, A4, R1, R2, R3, R4, R5a, R5b, R5c, R5d and p are defined as in the description.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: August 5, 2014
    Assignee: BASF SE
    Inventors: Steffen Gross, Matthias Pohlman, Arun Narine, Claudia Rosenbaum, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Karsten Koerber, Florian Kaiser, Wolfgang Von Deyn, Juergen Langewald, Deborah L. Culbertson, Cecille Ebuenga
  • Patent number: 8796294
    Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: August 5, 2014
    Assignee: Exelixis Patent Company LLC
    Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
  • Patent number: 8791129
    Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R43 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
  • Patent number: 8765773
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, Ra, R2a, R2b, R1, and X have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: July 1, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Dylan B. England, Kenneth M. Gigstad, Alexandra E. Gould, Liting Ma, He Xu
  • Patent number: 8754092
    Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: June 17, 2014
    Assignee: Exelixis Patent Company LLC
    Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
  • Patent number: 8748441
    Abstract: The subject matter of the present invention is the use of compounds of formula (I) in the form of a base, a hydrate or a solvate, or of mixtures thereof, as a medicament or for preparing a medicament intended for the treatment and/or prevention of disorders associated with the central nervous system (abbreviated to CNS) and/or associated with the peripheral nervous system (abbreviated to PNS).
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: June 10, 2014
    Assignee: SANOFI
    Inventors: Gilbert Marciniak, Jean-Francois Nave, Fabrice Viviani
  • Patent number: 8748440
    Abstract: Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: June 10, 2014
    Assignee: Exelixis, Inc.
    Inventors: Richard Martin, Jeffrey D Kahl, Brenton T Flatt, Ronald Griffith
  • Patent number: 8735409
    Abstract: This disclosure concerns novel quinazoline compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful anticancer agents, especially in inhibiting the function of the EGF receptor tyrosine kinases, HER1 tyrosine kinase, and HER2 tyrosine kinase. Thus, the disclosure also concerns a method of treating hyperproliferative diseases or conditions, such as various cancers and benign prostate hyperplasia (BPH), by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: May 27, 2014
    Inventors: Qiang Zhang, Hongwen Zhu
  • Patent number: 8722580
    Abstract: Disclosed are: a substance which has an activity of inhibiting the intracellular signaling from a plant-derived cytokinin receptor and which can control the growth or differentiation of a plant. Also, disclose is a method for searching for a chemical substance capable of promoting the growth of a root of a plant, which comprises measuring the level of intracellular signaling from the receptor in a system where a cell having the receptor is contacted with a chemical substance having an agonistic activity on the receptor and a substance to be tested, comparing the level of intracellular signaling measured in the preceding step with a level of intracellular signaling measured in the absence of the chemical substance, and determining the chemical substance as being a chemical substance capable of promoting the growth of a root of a plant based on the difference obtained by the comparison; and others.
    Type: Grant
    Filed: November 22, 2007
    Date of Patent: May 13, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Asako Nagasawa, Yuto Arata, Hideki Uneme
  • Publication number: 20140128390
    Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.
    Type: Application
    Filed: September 5, 2013
    Publication date: May 8, 2014
    Inventors: JACK LIN, JOHN BUELL, KATRINA CHAN, TODD EWING, PRABHA IBRAHIM, MARIKA NESPI, PHUONGLY PHAM, SONGYUAN SHI, WAYNE SPEVAK, GUOXIAN WU, JIAZHONG ZHANG, YING ZHANG
  • Patent number: 8716475
    Abstract: 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Grant
    Filed: February 13, 2013
    Date of Patent: May 6, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frank Chavez, James P. Edwards, Brad M. Savall, Jennifer D. Venable
  • Patent number: 8703782
    Abstract: The present invention relates to substituted indole derivatives, to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: April 22, 2014
    Assignee: Novartis AG
    Inventors: Nigel Graham Cooke, Maurice Van Eis, Rita Ramos, Karen Kammertoens
  • Patent number: 8697714
    Abstract: The present invention relates to a compound of the general formula (I) useful in the determining the presence, amount or activity of an enzyme in living cells, a method of preparing said compounds and a kit thereof.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: April 15, 2014
    Assignee: Nanyang Technological University
    Inventors: Bengang Xing, Junxin Aw, Qing Shao, Yanmei Yang, Tingting Jiang, Chungyen Ang
  • Publication number: 20140094465
    Abstract: The present invention is directed to compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: June 5, 2012
    Publication date: April 3, 2014
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Patent number: 8673929
    Abstract: This invention provides the treatment of viral infections with a 4,6-disubstituted or 2,4,6-trisubstituted quinazoline derivative represented by the structural formula [(I)] wherein: R2 is selected from the group consisting of hydrogen, NR?R? and C1-7 alkyl; —A is selected from the group consisting of a bond, O, S(O)n, C1-7 alkylene, C2-7 alkenylene and C2-7 alkynylene; R4 is selected from the group consisting of C1-7 alkyl, C2-7 alkenyl, C3-10cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted alkyl and cycloalkyl-alkyl; —Y is selected from the group consisting of a single bond, C1-7 alkylene, C2-7 alkenylene, and C2-7 alkynylene; n is 0, 1 or 2; and R6 is selected from the group consisting of halogen, heteroaryl and aryl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-?/-oxide, a solvate or a pro-drug thereof.
    Type: Grant
    Filed: July 20, 2007
    Date of Patent: March 18, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Ling-Jie Gao, Piet André Maurits Maria Herdewijn, Steven Cesar Alfons De Jonghe, William John Watkins, Lee Shun Chong
  • Patent number: 8658655
    Abstract: Compounds, compositions, and methods for specific inhibition of activated cdc42-associated kinase 1 (Ack1) are provided.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: February 25, 2014
    Assignees: Fox Chase Cancer Center, Reaction Biology Corporation
    Inventors: Jeffrey R. Peterson, Haiching Ma, Sean Deacon
  • Patent number: 8658654
    Abstract: The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: February 25, 2014
    Assignee: Symphony Evolution, Inc.
    Inventors: Kenneth D. Rice, Neel K. Anand, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Csaba J. Peto, Tsze H. Tsang, Charles M. Blazey
  • Patent number: 8648087
    Abstract: This invention provides compounds of Formula I wherein B, G, A, E, R1, R2, R3, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.
    Type: Grant
    Filed: November 15, 2006
    Date of Patent: February 11, 2014
    Assignee: Array Biopharma, Inc.
    Inventors: Joseph P. Lyssikatos, Julie Marie Greschuk, Fredrik P. Marmsäter, Qian Zhao, D. David Hennings, Weidong Liu
  • Patent number: 8642608
    Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: February 4, 2014
    Assignee: AstraZeneca AB
    Inventors: Andrew Peter Thomas, Elaine Sophie Elizabeth Stokes, Laurent Francois Andre Hennequin
  • Patent number: 8637533
    Abstract: 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: Grant
    Filed: February 17, 2012
    Date of Patent: January 28, 2014
    Assignee: ICOS Corporation
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 8637532
    Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: January 28, 2014
    Assignee: Merck Patent GmbH
    Inventors: Amanda E. Sutton, Ruoxi Lan, Thomas E. Richardson, David Perrey, Harold George Vandeveer, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Yufang Xiao, Lesley Liu-Bujalski, Andreas Goutopoulos, Frank Stieber, Brian L. Hodous, Hui Qiu, Reinaldo Jones, Brian H. Heasley
  • Patent number: 8633209
    Abstract: Provided herein are hydrobromide salts of a pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating a proliferative disease.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: January 21, 2014
    Assignee: Ambit Biosciences Corporation
    Inventors: Timothy David Gross, Patrick B. O'Donnell
  • Patent number: 8633207
    Abstract: Provided herein are quinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: January 21, 2014
    Assignee: Ambit Biosciences Corporation
    Inventors: Michael J. Hadd, Mark W. Holladay, Martin Rowbottom
  • Patent number: 8629153
    Abstract: The present invention relates to the use of quinazoline derivatives, which show EGFR inhibitory activity, for the prevention and/or treatment of virus-induced diseases, preferably virus induced respiratory diseases and exacerbation in chronic airway diseases such as COPD or asthma.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Birgit Jung
  • Patent number: 8623883
    Abstract: 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: Grant
    Filed: June 10, 2013
    Date of Patent: January 7, 2014
    Assignee: Warner-Lambert Company LLC
    Inventors: Stephen Alan Fakhoury, Helen Tsenwhei Lee, Jessica Elizabeth Reed, Kevin Matthew Schlosser, Karen Elaine Sexton, Haile Tecle, Roy Thomas Winters
  • Patent number: 8609672
    Abstract: The invention provides novel compounds based on piperazinylpyrimidine derivatives to be used as protein kinase inhibitors. The compounds may be useful in treating or preventing different cellular proliferation disorders, such as cancer. The present invention also provides methods of preparing these compounds, and methods of using the same.
    Type: Grant
    Filed: August 24, 2011
    Date of Patent: December 17, 2013
    Assignee: University of the Pacific
    Inventors: Wade A. Russu, Hassan M. Shallal
  • Patent number: 8586597
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. 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, using the compounds also are disclosed. An exemplary compound disclosed in this application is shown below.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: November 19, 2013
    Assignee: ICOS Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
  • Patent number: 8586505
    Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: November 19, 2013
    Assignee: SDS Biotech K. K.
    Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
  • Patent number: 8580804
    Abstract: The invention provides a compound having a heterocyclic skeleton of formula (I): wherein the indicated moieties are as described in the specification, as well as a tautomer thereof or a salt thereof. The compound is useful as a catalyst for an asymmetric synthesis.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: November 12, 2013
    Assignees: Kyoto University, Sumitomo Chemical Company Limited
    Inventors: Yoshiji Takemoto, Kazuo Murakami
  • Patent number: 8575184
    Abstract: A compound of formula (I) wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: November 5, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: James A. Johnson, John Lloyd, Heather Finlay, Ji Jiang, James Neels, Naveen Kumar Dhondi, Prashantha Gunaga, Abhisek Banerjee
  • Publication number: 20130289044
    Abstract: The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R1-R4 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: October 5, 2011
    Publication date: October 31, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: R. Richard Goehring, Laykea Tafesse, Jiangchao Yao
  • Patent number: 8552018
    Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: October 8, 2013
    Assignees: Arizona Board of Regents on behalf of the University of Arizona, Astex Pharmaceutials, Inc.
    Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Sridevi Bashyam, Steven L. Warner, James Welsh
  • Publication number: 20130261052
    Abstract: Proteases such as memapsin-1 are import enzymes, playing roles in a variety of diseases including diabetes. The inventors have developed inhibitors of memapsin 1 and methods of use therefore in the treatment of disease.
    Type: Application
    Filed: March 11, 2013
    Publication date: October 3, 2013
    Applicant: Oklahoma Medical Research Foundation
    Inventors: Jordan Tang, Xiangping Huang, Deborah Downs
  • Publication number: 20130261123
    Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: December 16, 2011
    Publication date: October 3, 2013
    Inventors: Xicheng Sun, Jian Qiu, Adam Stout
  • Patent number: 8546409
    Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such compound admixed with at least one pharmaceutically acceptable excipient.
    Type: Grant
    Filed: April 20, 2010
    Date of Patent: October 1, 2013
    Assignee: Gilead Calistoga LLC
    Inventors: Kamal D. Puri, Jerry B. Evarts, Brian Lannutti, Neill Giese
  • Patent number: 8546565
    Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R5 and X have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: October 1, 2013
    Assignee: Merck Patent Gesellschaft
    Inventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
  • Patent number: 8541428
    Abstract: The present invention relates to novel quinoxaline, quinazoline and phthalazine derivatives as well as multimeric derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds for the treatment and prevention of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in treating and preventing neurodegenerative diseases.
    Type: Grant
    Filed: August 22, 2006
    Date of Patent: September 24, 2013
    Assignee: Technion Research and Development Foundation Ltd.
    Inventors: Moshe Gavish, Jehuda Arieh Veenman, Alex Shterenberg, Ilan Marek
  • Patent number: 8518959
    Abstract: The invention relates to methods of screening for binding partners, especially binding partners essential for the biological activity of erastin (e.g. VDACs such as VDAC3). The invention also provides reagents and methods for effective killing of cancer cells with erastin and related compounds or derivatives.
    Type: Grant
    Filed: January 25, 2006
    Date of Patent: August 27, 2013
    Assignee: Prolexys Pharmaceuticals, Inc.
    Inventors: Robert R. Becklin, Cindy Lou Chepanoske, John M. Peltier, Longwu Qi, Paul B. Robbins, Sudhir R. Sahasrabudhe, Robert Selliah, Keith Simmon, Brent R. Stockwell, Raj Gopal Venkat, Moritz von Rechenberg, Eugene Y. Zhen
  • Patent number: 8513267
    Abstract: The present invention relates to the use of 4-anilinoquinazoline derivatives as adenosine-kinase inhibitors. The present invention also relates to a method for protecting tissues and organs like heart, brain and kidneys affected by ischemia, and for treating heart insufficiency, myocardium infarct, arrhythmia, arterial hypertension, atherosclerosis, coronary artery restenosis after angioplasty, chronic renal insufficiency, cerebral vascular accident, and chronic inflanunatory diseases (e.g., rheumatoid arthritis). The present invention also relates to the compound 6,7-dimethoxy-4-(3?-N?,N?-dimethylaminoanilino)quinazoline, or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising it and use of such compound in the manufacture of a medicament for treating or preventing diseases or conditions that are benefited from the adenosine-kinase inhibition.
    Type: Grant
    Filed: September 1, 2006
    Date of Patent: August 20, 2013
    Assignee: Universidade Estadual de Campinas-Unicamp
    Inventors: Kleber Gomes Franchini, Mario Jose Abdalla Saad, Roberto Rittner Neto, Rodrigo Miguel Marin, Silvana Aparecida Rocco
  • Publication number: 20130210821
    Abstract: The disclosure provides for methods of treating obesity and related disorders. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.
    Type: Application
    Filed: May 27, 2011
    Publication date: August 15, 2013
    Inventor: James E. Vath
  • Patent number: 8507509
    Abstract: Compounds of the general formula (I), wherein the substituents are as defined in claim 1, are useful as fungicides.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: August 13, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Fiona Murphy Kessabi, Hans-Georg Brunner, Renaud Beaudegnies, Laura Quaranta, Fredrik Cederbaum, Jayant Umarye
  • Patent number: 8501754
    Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R3 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: August 6, 2013
    Assignee: MERCK PATENT GmbH
    Inventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
  • Patent number: 8496957
    Abstract: Disclosed herein are methods for the treatment of otic diseases or conditions with intratympanic compositions and formulations of multiparticulate auris sensory cell modulating agent administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).
    Type: Grant
    Filed: July 16, 2009
    Date of Patent: July 30, 2013
    Assignees: Otonomy, Inc, The Regents of the University of California
    Inventors: Jay Lichter, Benedikt Vollrath, Sergio G. Duron, Carl Lebel, Fabrice Piu, Qiang Ye, Luis A. Dellamary, Andrew M. Trammel, Michael Christopher Scaife, Jeffrey P. Harris
  • Patent number: 8461166
    Abstract: Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK inhibitors as their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are further disclosed. The disclosed EGFR-TK inhibitors comprise a polyalkylene glycol moiety and/or a hydroxy-containing moiety and are characterized by improved solubility, biostability and bioavailability. Processes of preparing the disclosed EGFR-TK inhibitors and of radiolabeling same, via, for example, one-step radiosyntheses, are also disclosed.
    Type: Grant
    Filed: March 7, 2007
    Date of Patent: June 11, 2013
    Assignees: Hadasit Medical Research Services and Development Ltd., Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Eyal Mishani, Samar Dissoki, Galith Abourbeh, Alexander Levitzki
  • Patent number: RE44599
    Abstract: Compounds that inhibit P13K? activity, including compounds that selectively inhibit P13K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (P13K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which P13K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: November 12, 2013
    Assignee: ICOS Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri
  • Patent number: RE44638
    Abstract: The invention provides a class of substituted quinazolinone compounds and methods of treating diseases mediated by PI3K? activity. The disclosed compounds are useful in treating diseases such as bone-resorption disorders; and cancer, especially hematopoietic cancers, lymphomas, multiple myelomas and leukemia. The compounds are also useful in disrupting or inhibiting cellular processes such as leukocyte function or accumulation, neutrophils function, lymphocyte proliferation, and endogenous immune responses.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: December 10, 2013
    Assignee: ICOS Corporation
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri