Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 514/379)
  • Patent number: 10369220
    Abstract: A method of treating a subject having a deficient immune response is described. The method includes administering a therapeutically effective amount of non-immune drug, or an analog or metabolite thereof, known to induce one or more autoimmune syndromes to the subject. Drugs known to induce one or more autoimmune syndromes, such as lupus-like syndromes, include immune checkpoint inhibitor blockers. Methods of identifying drugs capable of enhancing immunity are also described.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: August 6, 2019
    Assignee: CELLPRINT IP HOLDING, LLC
    Inventor: David R. Kaplan
  • Patent number: 10208028
    Abstract: One embodiment is a method of treating cancer. The method includes administering a therapeutically effective amount of a compound to a patient.
    Type: Grant
    Filed: December 13, 2017
    Date of Patent: February 19, 2019
    Assignee: Macau University of Science and Technology
    Inventors: Lai Han Elaine Leung, Xiao Jun Yao, Liang Liu, Jia Hui Xu, Ying Li, Qian Qian Wang
  • Patent number: 10131642
    Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: November 20, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Michael Balestra, Jörg M. Bentzien, Jennifer Burke, Derek Cogan, Xin Guo, Keith R. Hornberger, John Lord, Kenneth M. Meyers, Zhaoming Xiong, Maolin Yu, Zhonghua Zhang
  • Patent number: 9856216
    Abstract: Provided is a compound of formula (I) as a TNIK (Traf2- and NCK-interacting kinase), IKK? (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the compound according to the present invention effectively inhibits TNIK, IKK? and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: January 2, 2018
    Assignee: GREEN CROSS CORPORATION
    Inventors: Soongyu Choi, Eun-Jung Park, Hee Jeong Seo, Younggyu Kong, Ickhwan Son, Sang-ho Ma, Man-Young Cha, Mi-Soon Kim, Kisoo Park
  • Patent number: 9416115
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: August 16, 2016
    Assignee: Gilead Scineces, Inc.
    Inventors: Michael Graupe, Yafan Lu, Jeff A. Zablocki
  • Patent number: 9145453
    Abstract: The present invention is embodied by a composition capable inducing weight loss in a patient in need thereof.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: September 29, 2015
    Assignee: SDG, Inc.
    Inventors: W. Blair Geho, John R. Lau
  • Patent number: 9073835
    Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: July 7, 2015
    Assignees: Centre National De La Recherche Scientifique, Universite De Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
  • Publication number: 20150141418
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Applicant: PTC Therapeutics, Inc.
    Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
  • Patent number: 9029400
    Abstract: The present invention relates to 5-oxoisoxazole derivatives of the formula I, the pharmaceutically usable salts thereof and the use thereof as medicinal substances.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: May 12, 2015
    Assignee: Sanofi
    Inventors: Stefan Petry, Manfred Seidel, Gerhard Zoller, Gunter Müller, Karl-Heinz Baringhaus, Hubert Heuer
  • Patent number: 9012482
    Abstract: Pharmaceutical agents characterized by containing benzophenone derivatives represented by the general formula: wherein the each substituent is as defined in the specification, or salts thereof have suppressive effect on RANKL production, suppressive effect on OPG reduction and inhibitory effects on differentiation/activation of osteoclasts, and are extremely useful for treating, for example therapy and/or prevention, of various diseases in which differentiation/activation of osteoclast are involved, such as osteoporosis.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: April 21, 2015
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Yukihiko Aikawa, Kimiko Morimoto, Mari Yamamoto, Shunichi Shiozawa
  • Patent number: 8980920
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8969587
    Abstract: Compounds, compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: March 3, 2015
    Assignee: Ambit Biosciences Corporation
    Inventors: Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
  • Patent number: 8952041
    Abstract: The invention provides novel compositions and compounds that inhibit CatSper channel activity, that preferentially inhibits sperm hyperactivity over sperm motility, or both. The compounds of the invention are useful as contraceptive agents that may be adminstered to males, females, or concurrently to both sexual partners. The invention further provides methods of conducting drug discovery business and of conducting a reproductive medicine business. The invention also provides methods of identifying compounds that modulate sperm hypermotility.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: February 10, 2015
    Assignee: Hydra Biosciences, Inc.
    Inventors: Jayhong A. Chong, Magdalene M. Moran
  • Patent number: 8933110
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: January 13, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Hui Cao, Yat Sun Or
  • Patent number: 8921404
    Abstract: The invention relates to azole derivatives of the general formula I as defined in the present application as well as to their uses in treatment of conditions that would benefit from their inhibitory effect on hormone sensitive lipase, HSL, an allosteric enzyme in adipocytes which is inhibited by insulin and is responsible for the breakdown of fats in fat cells and thus for transferring fat constituents into the blood stream. Inhibition of this enzyme is therefore equivalent to an insulin-like effect of the compounds of the invention.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: December 30, 2014
    Assignee: Sanofi
    Inventors: Gerhard Zoller, Stefan Petry, Gunter Muller, Hubert Heuer, Norbert Tennagels
  • Patent number: 8916584
    Abstract: Benzisoxazole and azabenzisoxazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: February 11, 2011
    Date of Patent: December 23, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Darren W. Engers
  • Publication number: 20140364468
    Abstract: The present invention relates generally to methods of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight loss-promoting anti-convulsant either alone or in combination with bupropion or metabolites thereof or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.
    Type: Application
    Filed: August 20, 2014
    Publication date: December 11, 2014
    Inventors: Kishore M. Gadde, K. Ranga R. Krishnan
  • Publication number: 20140349990
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 20, 2014
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Jutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
  • Publication number: 20140336184
    Abstract: The present invention concerns methods and compositions regarding suppression of double stranded RNA-activated protein kinase (PKR) to enhance cognition in an individual. In specific cases, an inhibitor of PKR is provided to the individual such that cognition is enhanced thereby, including by enhancing memory, for example. Kits are encompassed in certain embodiments.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventors: Mauro Costa-Mattioli, Ping Jun Zhu, Jeremy A. May
  • Publication number: 20140322318
    Abstract: Methods and systems for administration of pharmaceuticals using a unit dosage package that includes a first unit dosage that has a first drug and a second drug, a second unit dosage that has the first drug and the second drug, where the second unit dosage includes a different amount of the second drug than the first unit dosage and a unit dosage package is configured to hold the first unit dosage and the second unit dosage. In preferred embodiments the methods and systems are used for administration of weight loss medications.
    Type: Application
    Filed: March 20, 2014
    Publication date: October 30, 2014
    Inventors: Anthony A. McKinney, Gary Tollefson, Eckard Weber, Rick Soltero
  • Publication number: 20140323399
    Abstract: Methods and compositions for treating a blood glucose condition involve identifying a suitable subject and administering an effective amount of a composition that contains one or more of an opioid antagonist, an anticonvulsant, and a psychotherapeutic agent. The compositions can include insulin. In some embodiments, such methods and compositions can be used to modulate a blood glucose level. In preferred embodiments, such methods and compositions are useful for increasing a subject's sensitivity to insulin.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: Michael A. Cowley, Anthony A. McKinney, Gary Tollefson
  • Publication number: 20140309210
    Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.
    Type: Application
    Filed: February 12, 2014
    Publication date: October 16, 2014
    Applicant: Genentech, Inc.
    Inventors: Jason Burch, Richard A. Goldsmith, Daniel Fred Ortwine, Richard Pastor, Zhonghua Pei
  • Publication number: 20140296311
    Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and use of the compounds in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Inventors: William Greenlee, Dmitri Pissarnitski, Zhiqiang Zhao, Zhaoning Zhu
  • Publication number: 20140296219
    Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.
    Type: Application
    Filed: November 14, 2013
    Publication date: October 2, 2014
    Applicant: UNIVERSITY OF MASSACHUSETTS
    Inventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
  • Publication number: 20140275186
    Abstract: This invention relates to novel 4,5-dihydroisoxazoles and 4,5-dihydro[1,2,4]-oxadiazoles of formula (I), to their use as androgenic or antiandrogenic agents or androgen receptor modulators, and to methods of their preparation.
    Type: Application
    Filed: October 17, 2012
    Publication date: September 18, 2014
    Inventors: Juha Pulkkinen, Pekka Poutiainen, Tuomas Oravilahti, Jorma Palvimo, Mikael Perakyla, Reino Laatikainen, Tarja Ihalainen
  • Patent number: 8835425
    Abstract: The present invention relates to the pharmaceutical use of selective GABA A ?5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: September 16, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodolfo Gasser, Maria-Clemencia Hernandez, Andrew Thomas
  • Publication number: 20140219989
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 7, 2014
    Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
  • Patent number: 8778392
    Abstract: An oral disintegrating tablet containing (1) D-mannitol, (2) an active ingredient, (3) one or more disintegrating agents selected from the group consisting of crospovidone and carmellose, and (4) one or more lubricants selected from the group consisting of sodium stearyl fumarate and sucrose esters of fatty acids. The oral disintegrating tablet of the present invention has some excellent properties of (1) allowing easy production in a common facility without necessitating a specialized pharmaceutical technique, (2) having an appropriate strength that does not breakdown in the process of distribution, (3) having a fast disintegrating ability in the oral cavity, and (4) also having excellent ingestion feel such as greatly reduced bitterness or gritty feel; therefore, the tablet can be suitably used as a dosage form that is suitable for aged individuals, children, and seriously ill patients.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: July 15, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Makoto Matsuoka, Hiroyuki Nishii, Maki Kawamura
  • Patent number: 8778938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 15, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
  • Publication number: 20140193363
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 10, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Patent number: 8772307
    Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: July 8, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Melanie Reich, Ruth Jostock, Gregor Bahrenberg, Hans Schick, Birgitta Henkel, Helmut Sonnenschein
  • Publication number: 20140135310
    Abstract: Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3; and enancjomers, pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 15, 2014
    Applicant: Adamed Sp. z o.o.
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Maciej Pawlowski, Andrzej Krukowski, Rafal Rusiecki, Agata Magdalena Siwek, Malgorzata Anna Wolak
  • Patent number: 8722651
    Abstract: The present invention relates to the treatment of diseases and conditions with an effective amount of a steroid having those formulas given in the specification, or a pharmacologically-acceptable salt or ester thereof. The disease or conditions treatable according to the invention include angiogenic diseases and conditions of the eye, angiogenic diseases and conditions of the brain, inflammatory diseases and conditions of the eye, inflammatory diseases and conditions of the brain and neurodegenerative diseases.
    Type: Grant
    Filed: July 12, 2006
    Date of Patent: May 13, 2014
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventor: David Bar-Or
  • Patent number: 8716492
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: May 6, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • Publication number: 20140088162
    Abstract: This disclosure relates generally to methods and pharmaceutical compositions useful in treating pulmonary hypertension. In one embodiment, for example, the disclosure provides a method for treating pulmonary hypertension comprising administering a therapeutically effective dose of a carbonic anhydrase inhibitor to a patient in need of treatment. The disclosure finds utility in the fields of medicine and pharmacology.
    Type: Application
    Filed: September 12, 2013
    Publication date: March 27, 2014
    Applicant: VIVUS, INC.
    Inventors: Thomas Najarian, Peter Y. Tam, Leland F. Wilson, Craig Peterson
  • Publication number: 20140080857
    Abstract: Pharmaceutical formulations comprise sustained-release zonisamide. Methods of preparing such pharmaceutical formulations involve intermixing zonisamide with a suitable excipient configured to control the dissolution profile of the zonisamide. Methods of treatment involve administering the pharmaceutical formulations to patients in need of such treatment.
    Type: Application
    Filed: August 13, 2013
    Publication date: March 20, 2014
    Applicant: Orexigen Therapeutics, Inc.
    Inventors: Anthony A. McKinney, Gary Tollefson, Simon Kwok-Pan Yau, Ronald S. Vladyka, Rick Soltero
  • Publication number: 20140066466
    Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.
    Type: Application
    Filed: March 12, 2012
    Publication date: March 6, 2014
    Applicant: President and Fellows of Harvard College
    Inventor: Junying Yuan
  • Patent number: 8637551
    Abstract: The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R1 represents the group CONR2R3 which is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; R2 and R3 are independently H or (C1-4)alkyl; and R4 is cyclopropyl, 2-pyridyl or phenyl, optionally substituted with one or more halogens; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
    Type: Grant
    Filed: July 6, 2010
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventor: Simon James Anthony Grove
  • Publication number: 20140024657
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 23, 2014
    Applicant: President and Fellows of Harvard College
    Inventors: Junying YUAN, Emily S. Hsu
  • Publication number: 20140005187
    Abstract: The present invention identifies the cholesterol biosynthetic pathway, including the enzyme oxidosqualene cyclase, as new protein targets for anti-tumor therapeutics. The present invention further provides a class of oxidosqualene cyclase inhibitors containing a tertiary amine linked with aromatic ring structures, as a new class of anticancer agents. Compounds disclosed herein have been tested in 19 cell lines including breast cancer, prostate cancer, lung cancer (including drug-resistant lung cancer H69AR), colon cancer, ovarian cancer (including drug-resistant OVCAR-3), and pancreatic cancer cells, as wells as in human breast and prostate xenograft tumor growth in nude mice, and have been shown to be active.
    Type: Application
    Filed: December 22, 2011
    Publication date: January 2, 2014
    Applicant: The Curators of the University of Missouri
    Inventors: Salman M. Hyder, Yayun Liang, Xiaoqin Zou, Sam Z. Grinter, Sheng-you Huang
  • Publication number: 20130345270
    Abstract: Active compounds useful for inhibiting fatty acid synthase in a subject in need thereof are described. The active compounds are, in general, a 5-mercapto-1H-Indazole-4,7-dione or an analog thereof. The compounds are useful for treating subjects afflicted with, cancer, obesity, diabetes, a viral infection, a bacterial infection, a fungal infection, or a protozoal infection.
    Type: Application
    Filed: November 7, 2011
    Publication date: December 26, 2013
    Applicant: Waake Forest University Health Sciences
    Inventors: Steven J. Kridel, W. Todd Lowther, Herman W. Odens, Jeffrey D. Schmitt
  • Publication number: 20130338144
    Abstract: The invention described herein pertains to compounds, compositions and formulations comprising the compounds, and methods for use of the compounds, compositions and/or formulations in the treatment of diseases responsive to the inhibition of uPAR-uPA interactions, such as cancer.
    Type: Application
    Filed: March 2, 2012
    Publication date: December 19, 2013
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventor: Samy Meroueh
  • Patent number: 8609849
    Abstract: Pharmaceutical compositions of the invention include hydroxylated sulfamide derivatives having a disease-modifying action in the treatment of diseases associated with excitotoxicity and accompanying oxidative stress that include epilepsy, Alzheimer's disease, and any neurodegenerative disease involving glutamate toxicity.
    Type: Grant
    Filed: November 29, 2011
    Date of Patent: December 17, 2013
    Assignees: Fox Chase Chemical Diversity Center, Inc., Advanced Neural Dynamics, Inc.
    Inventors: Garry Robert Smith, Douglas E. Brenneman, Allen B. Reitz, Yan Zhang, Yanming Du
  • Patent number: 8609663
    Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.
    Type: Grant
    Filed: November 17, 2010
    Date of Patent: December 17, 2013
    Assignee: University of Massachusetts
    Inventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
  • Publication number: 20130310254
    Abstract: The present application relates to novel alpha, beta-unsaturated imines, to processes for their preparation, to their use for controlling animal pests including arthropods and in particular insects and to their use in the control of vectors.
    Type: Application
    Filed: November 24, 2011
    Publication date: November 21, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stefan Werner, Ulrich Ebbinghaus-Kintscher, Sebastian Horstmann, Michael Maue, Hans-Georg Schwarz, Robert Velten, Arnd Voerste, Ulrich Görgens, Andreas Turberg
  • Patent number: 8586568
    Abstract: The present invention relates to the treatment of diseases and conditions with an effective amount of a steroid having those formulas given in the specification, or a pharmacologically-acceptable salt or ester thereof. The disease or conditions treatable according to the invention include angiogenic diseases and conditions of the eye, angiogenic diseases and conditions of the brain, inflammatory diseases and conditions of the eye, inflammatory diseases and conditions of the brain and neurodegenerative diseases.
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: November 19, 2013
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventor: David Bar-Or
  • Publication number: 20130303525
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: July 19, 2011
    Publication date: November 14, 2013
    Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.
    Inventors: Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach
  • Publication number: 20130274256
    Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.
    Type: Application
    Filed: October 11, 2012
    Publication date: October 17, 2013
    Applicant: SEQUOIA SCIENCES, INC.
    Inventor: Sequoia Sciences, Inc.
  • Publication number: 20130267510
    Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: December 6, 2011
    Publication date: October 10, 2013
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large
  • Patent number: 8552041
    Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate cell stress response for treating said disease.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: October 8, 2013
    Assignee: Pharnext
    Inventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko