Benzo Fused At 4,5-positions Of The Diazole Ring Patents (Class 514/394)
  • Publication number: 20140235686
    Abstract: The present invention is based on the identification of novel biomarkers predictive of response to anti-cancer therapies.
    Type: Application
    Filed: October 11, 2012
    Publication date: August 21, 2014
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Ronald A. DePinho, Ji-Hye Paik
  • Publication number: 20140234402
    Abstract: Compositions and methods for treating systemic diseases by intravenous administration of formulations of synthesized curcumin (diferuloylmethane) and concomitantly a calcium channel blocker to human subjects with neoplastic and neurodegenerative diseases are disclosed herein. The diseases are treated by prolonged administration of sub-optimal doses of liposomal curcumin or polymeric nanocurcumin or the sustained release curcumin from PLGA nanocurcumin at dosages below systemic hemolytic thresholds concomitantly with or without calcium channel blockers.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: SignPath Pharma Inc.
    Inventor: Lawrence Helson
  • Patent number: 8809313
    Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
    Type: Grant
    Filed: May 29, 2012
    Date of Patent: August 19, 2014
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Patent number: 8809338
    Abstract: The present invention refers to the field of chemical compounds bearing a 1,2,3-triazole ring of formula (I) and possessing guanidino and carboxylic groups or their isosteres, their preparation by Cu-catalyzed “click-chemistry”, and medical-diagnostic use in pathologies where angiogenesis is altered, for example pathologic conditions of tumor origin, tumor metastasis, osteoporosis, and rheumatoid arthritis.
    Type: Grant
    Filed: February 14, 2011
    Date of Patent: August 19, 2014
    Assignee: Universita' Degli Studi di Firenze
    Inventors: Antonio Guarna, Gloria Menchi, Nicoletta Cini, Andrea Trabocchi, Alberto Pupi, Anna Bottoncetti, Silvia Raspanti, Lido Calorini
  • Patent number: 8809548
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: February 8, 2010
    Date of Patent: August 19, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jeffrey Lee Romine, Denis R. St. Laurent, Makonen Belema, Lawrence B. Snyder, Lawrence G. Hamann, John F. Kadow, Jayne Kapur, Andrew C. Good, Omar D. Lopez, Rico Lavoie, John A. Bender
  • Patent number: 8809549
    Abstract: The present invention relates to particular esters of bendamustine and related compounds, and medical uses thereof.
    Type: Grant
    Filed: April 25, 2013
    Date of Patent: August 19, 2014
    Inventors: Helmut Schickaneder, Armin Buschauer, Guenther Bernhardt, Christian Schickaneder, Michael Limmert, Stefan Huber
  • Publication number: 20140228380
    Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.
    Type: Application
    Filed: August 2, 2013
    Publication date: August 14, 2014
    Applicants: University of Medicine and Dentistry New Jersey Medical School, Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine
    Inventors: Sandhya Kortagere, Eldo V. Kuzhikandahil
  • Publication number: 20140228355
    Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.
    Type: Application
    Filed: February 11, 2013
    Publication date: August 14, 2014
    Applicants: University of Medicine and Dentistry New Jersey Medical School, Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine
    Inventors: Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine, University of Medicine and Dentistry New Jersey Medical School
  • Publication number: 20140228360
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 14, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof
  • Publication number: 20140228367
    Abstract: The present disclosure relates to compounds of the Formula (I): and pharmaceutically acceptable salts, as kinase modulators, compatible with the Type-II inhibition of kinases.
    Type: Application
    Filed: February 5, 2014
    Publication date: August 14, 2014
    Inventor: Gary A. Flynn
  • Patent number: 8802865
    Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: August 12, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Vernon C Alford, Jr., James C Lanter, Raymond A Ng
  • Patent number: 8802707
    Abstract: This invention is a method of killing the stealthy intra-cellular bacteria which are key to the pathogenesis Cancers. These very tiny L-form Cell-Wall-Deficient (CWD) antibiotic-resistant bacteria live within the cytoplasm of cells, including the phagocytic cells (e.g. monocytes, macrophages, lymphocytes, neutrophils and polymorphonuclear cells) of the immune system itself. The cellular proliferation in Cancer is catalysed the action of the same tiny L-form bacteria. They cause the cell nucleus to release mRNA signaling the Th1 cytokine cascade without the need for conventional signaling via, for example, CD4+T -Lymphocytes. Some of these Cytokines and Chemokines, including, without limitation, Cellular Adhesion Molecule (CAM), create the environment which allows the cellular proliferation to start, and then allows the cancerous growth to gain a foothold in the body. Killing these stealthy pathogens removes the environment needed to initiate and feed the cellular proliferation commonly called ‘Cancer’.
    Type: Grant
    Filed: July 31, 2006
    Date of Patent: August 12, 2014
    Inventor: Trevor Gordon Marshall
  • Publication number: 20140221339
    Abstract: The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are the same or different aromatic rings, etc., and ring A is a heterocyclic ring. The compound of the invention or a pharmaceutically acceptable salt thereof has potent mPGES-1 inhibiting activity and is useful as an agent for the treatment or prevention of a disease, such as rheumatoid arthritis, osteoarthritis, temporomandibular joint disorders, low back pain, endometriosis, dysmenorrhea, overactive bladder, malignant tumors or neurodegenerative disease.
    Type: Application
    Filed: August 17, 2012
    Publication date: August 7, 2014
    Applicant: NIPPON SHINYAKU CO., LTD.
    Inventor: Hironori Otsu
  • Publication number: 20140221332
    Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.
    Type: Application
    Filed: May 25, 2012
    Publication date: August 7, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat
  • Publication number: 20140221431
    Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 7, 2014
    Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., Ltd
    Inventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
  • Publication number: 20140221443
    Abstract: The present invention relates to Compound 1 hydrogen sulfate salt and solvates, crystalline forms and amorphous forms thereof, and to processes for their preparation.
    Type: Application
    Filed: January 10, 2014
    Publication date: August 7, 2014
    Applicants: Astrazeneca AB, Array BioPharma Inc.
    Inventors: John DeMattei, Tsung-Hsun Chuang, Gorkhn Sharma-Singh, Paul Alfred Dickinson, Mohammed Pervez, Richard Anthony Storey, Christopher John Squire, James Gair Ford, Ronald John Roberts
  • Publication number: 20140219960
    Abstract: The present invention relates a novel composition for preventing or treating hepatitis C virus, regulating the phosphorylation of a replicase. More specifically, it is possible to prevent or treat hepatitis C using a novel PRK2 inhibitor discovered through structure modeling, and to prevent or treat hepatitis C, particularly, interferon-insensitive hepatitis C through coadministration of an Hsp90 inhibitor.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 7, 2014
    Applicant: Industry-Academic Cooperation Foundation, Yonsei University
    Inventor: Jong-Won Oh
  • Patent number: 8796466
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: August 5, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: John A. Bender, Piyasena Hewawasam, John F. Kadow, Omar D. Lopez, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Lawrence B. Snyder, Denis R. St. Laurent, Gan Wang, Ningning Xu, Makonen Belema
  • Publication number: 20140212487
    Abstract: Disclosed are solid dispersions comprising ledipasvir, wherein ledipasvir is dispersed within a polymer matrix formed by a pharmaceutically acceptable polymer, and further wherein ledipasvir is substantially amorphous. Also disclosed are pharmaceutical compositions comprising solid dispersion and methods of using the solid dispersion.
    Type: Application
    Filed: January 30, 2014
    Publication date: July 31, 2014
    Inventors: Erik Mogalian, Reza Oliyai, Dimitrios Stefanidis, Vahid Zia
  • Publication number: 20140213592
    Abstract: The present invention relates to the treatment of oncological, chronic inflammatory and similar diseases with the aid of new families of chemical compounds having improved efficiency with regard to the inhibition of Abl kinase and mutant forms thereof, as well as other therapeutically significant kinases. It describes protein kinase inhibitors in the form of compounds of general formula (I) and compounds of general formula (II), or a tautomer, an individual isomer, a mixture of isomers, a pharmaceutically acceptable salt, a solvate or a hydrate thereof.
    Type: Application
    Filed: April 1, 2014
    Publication date: July 31, 2014
    Applicant: Obshchestvo s ogranichennoy otvetstvennostyou "Fusion Pharma"
    Inventors: Germes G. CHILOV, Ilya Y. TITOV
  • Patent number: 8791269
    Abstract: A stable complex of tomoxiprole with 2-hydroxypropyl-beta-cyclodextrin with fast dissolution rate and rapid absorption wherein amorphous tomoxiprole forms a complex with 2-hydroxypropyl-beta-cyclodextrin in about equimolecular ratio. The complex shows a remarkably faster dissolution rate and absorption with respect to crystalline tomoxiprole and is particularly suitable for the production of pharmaceutical oral dosage forms, such as tablets and capsules, where rapid onset of therapeutical action is required. A method of manufacture of the complex is also described and claimed.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: July 29, 2014
    Assignees: Fondazione Istituto Insubrico di Ricerca per la Vita, Fondazione Cariplo
    Inventors: Alberto Milanese, Marino Nebuloni, Lucia Carrano
  • Publication number: 20140205564
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Inventors: Jeffrey Lee Romine, Denis R. St. Laurent, Makonen Belema, Lawrence B. Snyder, Lawrence G. Hamann, John F. Kadow, Jayne Kapur, Andrew C. Good, Omar D. Lopez, Rico Lavoie, John A. Bender
  • Publication number: 20140206674
    Abstract: The invention relates to a pharmaceutical combination of 2-aminoethanesulfonic acid with a pharmaceutical agent such as an antihypertensive agent and the use of 2-aminoethanesulfonic acid in a method to lower the bilirubin level in the blood.
    Type: Application
    Filed: January 17, 2014
    Publication date: July 24, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Markus ZWICKL
  • Publication number: 20140206706
    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: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    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: 20140206733
    Abstract: Stable liquid formulations of bendamustine, and pharmaceutically acceptable salts thereof, and polar aprotic solvents, are described.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: Cephalon, Inc.
    Inventors: Anthony S. Drager, Rachel Y. Labell, Piyush R. Patel
  • Publication number: 20140200249
    Abstract: The use of a MEK inhibitor compound of Formula (I), as defined herein, or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of Noonan Syndrome, a method of treating a warm-blooded animal, especially a human, having Noonan Syndrome, comprising administering to said animal a therapeutically effective amount of a MEK inhibitor compound of Formula (I), as defined herein, or a pharmaceutically acceptable salt thereof; and to a pharmaceutical composition and a commercial package comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and a package insert or other labeling including directions for treating Noonan Syndrome.
    Type: Application
    Filed: August 29, 2012
    Publication date: July 17, 2014
    Applicant: Novartis AG
    Inventor: Jessie Gu
  • Publication number: 20140200260
    Abstract: The invention provides methods for determining whether a subject is suffering from a rheumatoid arthritis associated with the BRAF oncogene comprising contacting isolated fibroblasts from the subject with a molecule or pool of molecules directed to the BRAF oncogene; and culturing the sample in the presence of the agent and determining whether BRAF oncogene expression by the cell is decreased and/or whether cells in the sample return to a less transformed phenotype, exhibit decreased cell proliferation and/or exhibit increased contact inhibition, any of which is indicative that the subject is suffering from a rheumatoid arthritis associated with the BRAF oncogene.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Inventor: Richard H. Weisbart
  • 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: 8772242
    Abstract: There is disclosed herein a composition for treating gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhea, chronic idiopathic nausea, IBD-associated constipation and diarrhea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the composition comprising: (i) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (ii) at least one anti-clostridial agent selected from the above combined with an opioid blocking agent.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: July 8, 2014
    Inventor: Thomas Julius Borody
  • Patent number: 8772505
    Abstract: The present invention relates to novel Tricyclic Compounds, compositions comprising at least one Tricyclic Compound, and methods of using Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient. The present invention provides Tricyclic Compounds of Formula (I): Non-limiting examples of the Compounds of Formula (I) include compound 44 The Compounds of Formula (II) can be useful for inhibiting HCV viral replication or replicon activity, and for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin X. Chen, Anilkumar Gopinadhan Nair, Qingbei Zeng, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8772278
    Abstract: The present invention relates to a method of prophylaxis or treatment of systemic diseases in cats, wherein the method comprising administration of a therapeutically effective amount of angiotensin II receptor 1 (AT-1) antagonist (sartan) to a cat in need of such a treatment.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: July 8, 2014
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Marcus Stark, Ulrike Sent, Ingo Lang
  • Publication number: 20140187533
    Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns compounds (e.g., compounds according to any of Formulas (I)-(XIII) or Compounds (1)-(236) of Table 1) that are useful in treatment of a variety of diseases and conditions.
    Type: Application
    Filed: March 2, 2012
    Publication date: July 3, 2014
    Applicant: Zalicus Pharmaceuticals Ltd.
    Inventors: Hassan Pajouhesh, Richard Holland, Lingyun Zhang, Hossein Pajouhesh, Jason Lamontagne, Brendan Whelan
  • Publication number: 20140187598
    Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.
    Type: Application
    Filed: March 7, 2014
    Publication date: July 3, 2014
    Applicant: Cephalon, Inc.
    Inventors: Martin Ian Cooper, Laurent D. Courvoisier, Mark Eddleston, Robert E. McKean
  • Publication number: 20140187537
    Abstract: This disclosure relates to diagnostic and therapeutic methods and systems related thereto. In certain embodiments, the disclosure contemplates methods of improving chemotherapy treatments by administering chemotherapy agents, analyzing CHFR gene expression, methylation, or both, and determining an appropriate therapeutic strategy. Analysis of data herein revealed that reduced CHFR expression levels was a predictor of improved overall survival of subject with non-small cell lung cancer.
    Type: Application
    Filed: January 2, 2014
    Publication date: July 3, 2014
    Applicant: EMORY UNIVERSITY
    Inventor: Johann C. Brandes
  • Patent number: 8765731
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: July 1, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, Jr., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
  • Patent number: 8765748
    Abstract: The present invention is directed to a compound is represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: July 1, 2014
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
  • Publication number: 20140179750
    Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.
    Type: Application
    Filed: June 19, 2012
    Publication date: June 26, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Jianxiong Jiang, Thota Ganesh, Yuhong Du, Pahk Thepchatri, Yi Quan, Ray J. Dingledine
  • Publication number: 20140178336
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: June 26, 2014
    Inventor: Gilead Sciences, Inc.
  • Patent number: 8759539
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: June 24, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Publication number: 20140171363
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, II, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, SU Liansheng
  • Patent number: 8754114
    Abstract: The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: June 17, 2014
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, Colin Zhang, Meizhong Xu, Jincong Zhuo, Chunhong He
  • Publication number: 20140162987
    Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a severe pain in an individual using such pharmaceutical compositions.
    Type: Application
    Filed: January 14, 2014
    Publication date: June 12, 2014
    Applicant: BIOCOPEA LIMITED
    Inventors: Robin M. Bannister, John Brew, Richard R. Reiley, III, Wilson Caparros Wanderley
  • Publication number: 20140162988
    Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.
    Type: Application
    Filed: January 14, 2014
    Publication date: June 12, 2014
    Applicant: BIOCOPEA LIMITED
    Inventors: Robin M. Bannister, John Brew, Richard R. Reiley, III, Wilson Caparros Wanderley
  • Patent number: 8748468
    Abstract: Treatment of cancer and thromboembolic disorders using inhibitors of Factor VIIa are disclosed herein using a compound of Formula I:
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: June 10, 2014
    Assignee: Pharmacyclics, Inc.
    Inventors: David Loury, Tarak Mody
  • Patent number: 8748433
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.
    Type: Grant
    Filed: April 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
  • Publication number: 20140155444
    Abstract: This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.
    Type: Application
    Filed: October 21, 2013
    Publication date: June 5, 2014
    Applicant: Concert Pharmaceuticals Inc.
    Inventors: Roger Tung, Craig E. Masse, Bhaumik A. Pandya
  • Publication number: 20140155382
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: November 22, 2013
    Publication date: June 5, 2014
    Applicant: ABBVIE INC.
    Inventors: David A. DEGOEY, Allan C. KRUEGER, Charles W. HUTCHINS, Warren M. KATI, William A. CARROLL
  • Publication number: 20140155399
    Abstract: The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided.
    Type: Application
    Filed: December 4, 2013
    Publication date: June 5, 2014
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Levi Garraway, Caroline Emery
  • Publication number: 20140148438
    Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.
    Type: Application
    Filed: September 22, 2011
    Publication date: May 29, 2014
    Inventor: Michael Farber
  • Publication number: 20140148490
    Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Applicant: Cephalon, Inc.
    Inventors: Jason Edward Brittain, Joe Craig Franklin