Additional Hetero Ring Patents (Class 514/397)
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Patent number: 9233947Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: GrantFiled: May 7, 2014Date of Patent: January 12, 2016Assignee: Janssen Pharmaceutica, NVInventor: Jay M Matthews
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Patent number: 9226918Abstract: This invention provides methods and pharmaceutical compositions for preventing or treating physical dependence and/or withdrawal associated with narcotic use, in particular by modulating a 5-HT3 receptor. Using a computational genetic approach in mice, a gene conserved between mice and humans was identified as candidate as a modulator of physical dependence to morphine. Administration of compounds that modulate 5-HT3 receptors was found to control withdrawal from morphine in mice and humans.Type: GrantFiled: December 4, 2009Date of Patent: January 5, 2016Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Gary Peltz, David Clark, Lawrence Chu
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Patent number: 9200309Abstract: To provide a method for screening using cultured cells, intended to find a compound which increases the amount of sphingosine-1-phosphate or dihydrosphingosine-1-phosphate by SPL inhibitory activity rapidly, simply and highly sensitively. Provided are: a rapid and simple measurement method employing a scintillation proximity assay (SPA); a method with greatly improved detection sensitivity to the activity of a compound by controlling the concentration of the vitamin B6 group in a culture medium to be used in assaying; and others.Type: GrantFiled: June 24, 2011Date of Patent: December 1, 2015Assignee: Daiichi Sankyo Company, LimitedInventors: Mamoru Otoyo, Masakazu Tamura
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Patent number: 9181251Abstract: Novel compositions and methods for the treatment and prevention of malaria are disclosed herein.Type: GrantFiled: December 12, 2013Date of Patent: November 10, 2015Assignees: University of Central Florida Research Foundation, Inc., Florida Atlantic University Board of TrusteesInventors: Debopam Chakrabarti, Amy Wright
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Patent number: 9173942Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.Type: GrantFiled: May 24, 2013Date of Patent: November 3, 2015Assignees: HELSINN HEALTHCARE SA, Roche Palo Alto LLCInventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Alberto Macciocchi, Andrew Miksztal, Thomas Malefyt, Kathleen M Lee
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Patent number: 9156818Abstract: 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. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with compounds of Formula (I).Type: GrantFiled: September 10, 2010Date of Patent: October 13, 2015Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Yao-Ling Qiu
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Amide derivative and use of the same as stability index of a luliconazole pharmaceutical formulation
Patent number: 9145401Abstract: An object is to establish an index to prepare a stable pharmaceutical formulation by specifying a related substance of luliconazole which appears depending on the type of a selected solvent in the luliconazole pharmaceutical formulation and which is different from the SE form and the Z form. Disclosed is an amide derivative of luliconazole.Type: GrantFiled: February 19, 2013Date of Patent: September 29, 2015Assignees: POLA PHARMA INC., NIHON NOHYAKU CO., LTD.Inventors: Takaaki Masuda, Hiroshi Yamaguchi -
Patent number: 9120830Abstract: 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: GrantFiled: June 27, 2014Date of Patent: September 1, 2015Assignee: Janssen Pharmaceutica NVInventors: Vernon C Alford, Jr., James C Lanter, Raymond A Ng
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Patent number: 9095576Abstract: The present invention relates to pharmaceutical compositions, containing 4-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, (S) 4-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole or (S) [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, their use as pharmaceuticals for the treatment of retinal diseases, for retinal neuroprotection and vision enhancement.Type: GrantFiled: November 19, 2012Date of Patent: August 4, 2015Assignee: Allergan, Inc.Inventors: Mohammed I. Dibas, John E. Donello, Daniel W. Gil
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Patent number: 9090661Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: GrantFiled: August 29, 2014Date of Patent: July 28, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Craig A. Coburn, John A. McCauley, Steven W. Ludmerer, Kun Liu, Joseph P. Vacca, Hao Wu, Bin Hu, Richard Soll, Fei Sun, Xinghai Wang, Man Yan, Chengren Zhang, Mingwei Zheng, Bin Zhong, Jian Zhu
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Patent number: 9085554Abstract: Disclosed is a method of evaluating stability of a pharmaceutical preparation containing luliconazole. The method includes measuring an amount of production of an SE form of luliconazole represented by following formula (2), an amount of production of a Z form of luliconazole represented by following formula (3) and an amount of production of an amide form of luliconazole represented by following formula (1) after storage under a severe condition or an accelerated condition, and judging that the stability of the pharmaceutical preparation is high if each of the amount of production of the SE form, the amount of production of the Z form and the amount of production of the amide form is not more than 5% by weight with respect to a compounded amount of luliconazole.Type: GrantFiled: January 8, 2015Date of Patent: July 21, 2015Assignees: POLA PHARMA INC., NIHON NOHYAKU CO., LTD.Inventors: Takaaki Masuda, Hiroshi Yamaguchi
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Patent number: 9073942Abstract: Disclosed are compounds of formula (I) for use as antiviral agents, particularly as anti-hepatitis virus C agents, wherein A, B, U, R1-R7, m, n, and q are as described herein. Also disclosed are pharmaceutical compositions and methods of treating or preventing viral infection in a host by the use of these compounds, either alone or in combination with other pharmaceutically active agents. Further disclosed are methods of preparing such compounds.Type: GrantFiled: February 9, 2013Date of Patent: July 7, 2015Assignee: Lupin LimitedInventors: Vidya Ramdas, Advait Arun Joshi, Moloy Manoj Banerjee, Amit Kumar Das, Deepak Sahebrao Walke, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 9073943Abstract: Disclosed are compounds of formula (I) for use as antiviral agents, particularly as anti-hepatitis virus C agents, wherein R-R 6 and q are as described herein. Also disclosed are pharmaceutical compositions and methods of treating or preventing viral infection in a host by the use of these compounds, either alone or in combination with other pharmaceutically active agents. Further disclosed are methods of preparing such compounds. (I).Type: GrantFiled: February 8, 2013Date of Patent: July 7, 2015Assignee: Lupin LimitedInventors: Vidya Ramdas, Advait Arun Joshi, Moloy Manoj Banerjee, Amit Kumar Das, Deepak Sahebrao Walke, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 9050271Abstract: In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof, comprised are a higher alcohol which is in a liquid state at 1 atm and 25° C. and/or a diester of a dibasic acid, provided that a diester carbonate is excluded, and a polyoxyethylene alkyl ether and/or a polyoxyethylene alkenyl ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrroridone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60 degrees C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C.Type: GrantFiled: April 9, 2010Date of Patent: June 9, 2015Assignees: POLA PHARMA INC., NIHON NOHYAKU CO., LTD.Inventors: Hirokazu Kobayashi, Eiko Kosugi, Nobuo Kubota
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Patent number: 9050325Abstract: A pharmaceutical composition for treating sudden discomfort associated with nausea and vomiting is disclosed which comprises a therapeutically effective amount of Ondansetron or a pharmaceutical salt thereof formulated for intranaal administration in combination with an antimicrobial preservative yielding enhanced stability of the Ondansetron or pharmaceutical salt thereof with a long chain polymer enhancing the viscosity of the composition.Type: GrantFiled: April 8, 2013Date of Patent: June 9, 2015Inventors: Abdul Zahir, Ryan John Welter
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Publication number: 20150148384Abstract: Disclosed herein are novel A-ring epoxidized triterpenoid compounds and derivatives thereof, including those of the formula (I), wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.Type: ApplicationFiled: June 14, 2013Publication date: May 28, 2015Applicant: REATA PHARMACEUTICALS, INC.Inventors: Eric Anderson, Christopher F. Bender, Xin Jiang, Xiaofeng Liu, Haizhou Sun, Melean Visnick
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Patent number: 9040573Abstract: An antifungal agent against a fungus of the genus Scytalidium (Scytalidium—dimidiatum, Scytalidium—hyalinum etc.), preferably an antifungal agent for superficial mycosis caused by a fungus of the genus Scytalidium as a pathogenic fungus, which contains luliconazole or a pharmaceutically acceptable salt thereof and/or lanoconazole or a pharmaceutically acceptable salt thereof as active ingredient(s).Type: GrantFiled: September 25, 2012Date of Patent: May 26, 2015Assignee: Nihon Nohyaku Co., Ltd.Inventors: Hiroyasu Koga, Yasuko Nanjoh, Ryoji Tsuboi
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Publication number: 20150133431Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.Type: ApplicationFiled: July 10, 2014Publication date: May 14, 2015Applicant: COYOTE PHARMACEUTICALS, INC.Inventor: Gary C. Look
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Publication number: 20150133517Abstract: The invention is directed to sublingual spray formulations containing ondansetron or a pharmaceutically acceptable salt thereof and water. The invention is further directed to methods for treating or preventing nausea and emesis associated with cancer treatments by administering sublingual spray formulations containing ondansetron or a pharmaceutically acceptable salt thereof to a patient in need thereof.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventors: Kiran Kumar Vangara, Chandeshwari Shivani Chilampalli, Venkat R. Goskonda
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Publication number: 20150133471Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: ApplicationFiled: September 15, 2014Publication date: May 14, 2015Inventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
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Publication number: 20150133444Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.Type: ApplicationFiled: November 10, 2014Publication date: May 14, 2015Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
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Patent number: 9029402Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: GrantFiled: January 2, 2014Date of Patent: May 12, 2015Assignee: Nivalis Therapeutics, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Patent number: 9029408Abstract: The present invention relates to a compound of formula XXII and a compound of formula 17ya, which are defined as anywhere in the specification, to a composition comprising the same, and to a method of using thereof in the treatment of various forms of cancer.Type: GrantFiled: October 9, 2013Date of Patent: May 12, 2015Assignees: GTx, Inc., University of Tennessee Research FoundationInventors: Duane D. Miller, Wei Li, Jianjun Chen, James T. Dalton, Chien-Ming Li, Sunjoo Ahn
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Publication number: 20150126570Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: January 15, 2015Publication date: May 7, 2015Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Patent number: 9023850Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.Type: GrantFiled: October 5, 2011Date of Patent: May 5, 2015Assignee: E I du Pont de Nemours and CompanyInventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
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Publication number: 20150119406Abstract: Tricyclic pyrone compounds having high oral bioavailability, excellent blood-brain barrier permeability, and low toxicity are presented. Administration of the compounds to Alzheimer's Disease transgenic models resulted in substantially reduced soluble and insoluble A? species in the brain without affecting general behavior and motor coordination. Furthermore, in addition to blocking the toxicity and formation of both intraneuronal and extracellular A? aggregates, the compounds also increase cellular cholesterol efflux, restore axonal trafficking, and enhance hippocampal synaptic plasticity.Type: ApplicationFiled: September 30, 2014Publication date: April 30, 2015Inventors: Duy H. Hua, Lee-way Jin, Izumi Maezawa, Xinmin Xie
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Publication number: 20150118285Abstract: The present invention relates to a pharmaceutical delivery device for application of a pharmaceutical to mucosal surfaces. The device comprises an adhesive layer and a non-adhesive backing layer, and the pharmaceutical may be provided in either or both layers. Upon application, the device adheres to the mucosal surface, providing localized drug delivery and protection to the treatment site. The kinetics of erodability are easily adjusted by varying the number of layers and/or the components.Type: ApplicationFiled: September 10, 2014Publication date: April 30, 2015Inventors: Gilles H. Tapolsky, David W. Osborne
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Patent number: 9012484Abstract: An object is to provide means for improving the solubility of luliconazole. Disclosed is a crystal consisting of luliconazole and short chain alcohol having a number of carbon atom or atoms of 1 to 4.Type: GrantFiled: September 6, 2013Date of Patent: April 21, 2015Assignees: Pola Pharma Inc., Nihon Nohyaku Co., Ltd.Inventors: Takaaki Masuda, Makoto Gotoh, Yoshiyuki Miyata
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Patent number: 9005643Abstract: Disclosure is provided for imidazole-phenyl derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.Type: GrantFiled: April 3, 2009Date of Patent: April 14, 2015Assignee: North Carolina State UniversityInventors: Christian Melander, Justin J. Richards, Cynthia Bunders
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Publication number: 20150098994Abstract: Pharmaceutical compositions are provided for the pharmacological treatment of breathing disorders and, more specifically, to compositions containing agents having serotonin receptor modulating activity for the alleviation of sleep apnea (central and obstructive) and other sleep-related breathing disorders wherein the active ingredients are released such as to extend effective blood plasma concentrations across the period of sleep.Type: ApplicationFiled: June 17, 2014Publication date: April 9, 2015Applicant: COLLEGIUM PHARMACEUTICAL, INC.Inventors: Roman V. Rariy, Michael Heffernan
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Publication number: 20150099740Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.Type: ApplicationFiled: December 12, 2014Publication date: April 9, 2015Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
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Publication number: 20150094520Abstract: A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.Type: ApplicationFiled: December 8, 2014Publication date: April 2, 2015Inventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Sanath K. MEEGALLA, M. Jonathan RUDOLPH, Mark J. WALL, Kenneth J. WILSON, Renee Louise DESJARLAIS, Carl M. MANTHEY, Christopher J. MOLLOY
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Publication number: 20150093391Abstract: A method of treating cancer or metastasis is provided involving administering at least one oncostatin M (OSM) antagonist to a subject, wherein the subject has been diagnosed with cancer. Administration of an OSM antagonist such as a small molecule pharmaceutical is provided as well as an anti-OSM antibody, an anti-OSM aptamer, and an OSM mRNA antagonist. The OSM antagonists were found to inhibit or prevent tumor cell detachment, proliferation and metastasis in several cancer types.Type: ApplicationFiled: September 5, 2014Publication date: April 2, 2015Applicant: BOISE STATE UNIVERSITYInventors: Cheryl Jorcyk, Dong Xu
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Patent number: 8992891Abstract: The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related disorders. More particularly, the invention relates to combined therapies for treating said disease by affecting PMP22 expression in a subject.Type: GrantFiled: November 28, 2008Date of Patent: March 31, 2015Assignee: PharnextInventors: Daniel Cohen, Ilya Chumakov, Oxana Guerassimenko, Serguei Nabirochkin
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Patent number: 8993609Abstract: The present invention relates to polyamide compositions and therapies for treating cells and subjects infected with papilloma virus.Type: GrantFiled: January 25, 2012Date of Patent: March 31, 2015Assignees: Nanovir, LLC, The Curators of the University of MissouriInventors: James K. Bashkin, Kevin J. Koeller, Terri Grace Edwards, Christopher Fisher
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Publication number: 20150087649Abstract: Methods and agents are provided for treatment of disorders associated with aberrant adrenocortical cell behavior, including (but not limited to) treatment of adrenocortical carcinoma (ACC) and/or Cushing's syndrome. Such methods involve administration of an agent which exhibits an IC50 value against huACAT1 of less than 10 ?M, and one or more further characteristics including effects on adrenocortical cells, disruption of cholesterol homeostasis, reduction in steroid biosynthesis, reduction of mitochondrial function, and/or preferential binding to by low-density lipoprotein (LDL).Type: ApplicationFiled: September 26, 2014Publication date: March 26, 2015Inventors: Stephen Warren Hunt, III, Julia Christine Owens, William E. Rainey, JR., Christopher R. LaPensee, Gary D. Hammer
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Bridged Ring compounds As Hepatitis C Virus (HCV) Inhibitors And Pharmaceutical Applications Thereof
Publication number: 20150079028Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.Type: ApplicationFiled: August 5, 2013Publication date: March 19, 2015Applicant: SUNSHINE LAKE PHARMA CO., LTDInventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo -
Publication number: 20150078998Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA activity: Pharmaceutical compositions may include a complex of a radionuclide and a compound of Formula I or Formula II.Type: ApplicationFiled: November 25, 2014Publication date: March 19, 2015Applicant: MOLECULAR INSIGHT PHARMACEUTICALSInventors: John W. BABICH, Craig ZIMMERMAN, John L. JOYAL, Genliang LU
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Publication number: 20150080398Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
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Publication number: 20150080397Abstract: Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: September 17, 2014Publication date: March 19, 2015Inventors: Tai Wei LY, Erik Dean RAAUM
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Patent number: 8981131Abstract: The present invention provides compounds represented by formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.Type: GrantFiled: July 25, 2008Date of Patent: March 17, 2015Assignee: Piramal Enterprises LimitedInventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
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Patent number: 8980321Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.Type: GrantFiled: July 14, 2014Date of Patent: March 17, 2015Assignee: Bend Research, Inc.Inventors: William J. Curatolo, Ravi M. Shanker, Walter C. Babcock, Dwayne T. Friesen, James A. S. Nightingale, Douglas A. Lorenz
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Patent number: 8980931Abstract: Disclosed is a method of evaluating stability of a pharmaceutical preparation containing luliconazole. The method includes measuring an amount of production of an SE form of luliconazole represented by following formula (2), an amount of production of a Z form of luliconazole represented by following formula (3) and an amount of production of an amide form of luliconazole represented by following formula (1) after storage under a severe condition or an accelerated condition, and judging that the stability of the pharmaceutical preparation is high if each of the amount of production of the SE form, the amount of production of the Z form and the amount of production of the amide form is not more than 5% by weight with respect to a compounded amount of luliconazole.Type: GrantFiled: April 28, 2014Date of Patent: March 17, 2015Assignees: Pola Pharma Inc., Nihon Nohyaku Co., Ltd.Inventors: Takaaki Masuda, Hiroshi Yamaguchi
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Patent number: 8980920Abstract: 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: GrantFiled: May 28, 2010Date of Patent: March 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20150073028Abstract: Disclosed is a pharmaceutical composition for antifungal use, comprising: 1) one or more compounds selected from compounds represented by the general formula (1) below and physiologically acceptable salts thereof; 2) one or more compounds selected from polypropylene glycol, diesters of dibasic acids, triacetin, 2-ethyl-1,3-hexanediol, lauromacrogol, and polyoxyethylene-polyoxypropylene glycol; and 3) one or more compounds selected from glucono-?-lactone, propylene glycol, glycerin, and lactic acid. General formula (1) (In the formula, X represents a halogen or hydrogen). wherein X represents a halogen or hydrogen.Type: ApplicationFiled: November 12, 2014Publication date: March 12, 2015Inventors: Takaaki Masuda, Naoto Nishida, Naoko Kobayashi, Hideaki Sasagawa
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Patent number: 8975290Abstract: Provided are methods of enhancing an immune response and methods for reducing the recruitment of monocytes to a lymph node by administering to an individual an angiotensin II receptor blocker or a compound of Formula (I) in conjunction with an antigen. The invention also provides relate methods for amplifying vaccine immunity by administering to an individual an angiotensin II receptor blocker or a compound of Formula (I) in conjunction with an vaccine. The invention also provides related methods of inhibiting tumor growth and metastasis by administering to an individual with cancer an angiotensin II receptor blocker or a compound of Formula (I) in conjunction with an anti-tumor preparation. In addition, related compositions comprising an ARB or a compound of Formula (I) and an antigen, vaccine, or anti-tumor preparation are provided.Type: GrantFiled: March 3, 2014Date of Patent: March 10, 2015Assignee: Colorado State University Research FoundationInventors: Steven W. Dow, Daniel P. Regan, Amanda M. Guth, Leah Mitchell
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Publication number: 20150065543Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: October 23, 2014Publication date: March 5, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20150065542Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.Type: ApplicationFiled: November 6, 2014Publication date: March 5, 2015Inventors: Allan C. Krueger, Warren M. Kati, Clarence J. Maring, Rolf Wagner, Charles W. Hutchins
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Publication number: 20150065504Abstract: Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).Type: ApplicationFiled: August 19, 2014Publication date: March 5, 2015Inventors: Guangyi Wang, Leonid Beigelman, Anh Truong, Carmela Napolitano, Daniele Andreotti, Haiying He, Karin Ann Stein
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Publication number: 20150065550Abstract: Compounds of formula (I), wherein X and R1-R6, are as defined in the claims, exhibit alpha2 agonistic activity and thus are useful as alpha2 agonists, especially as alpha2A agonists. Methods of use of said compounds are also provided.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Tuula Koskelainen, Tero Linnanen, Anna Minkkilä, Mikko Mäkelä, Antti Pohjakallio