Nonshared Hetero Atoms In At Least Two Rings Of The Polycyclo Ring System Patents (Class 514/81)
-
Patent number: 9090639Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: December 5, 2013Date of Patent: July 28, 2015Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond W Colburn, Scott L Dax, Christopher M Flores, Jay M Matthews, Ning Qin, Laura W. Andraka, Christopher Teleha, Mark A Youngman
-
Patent number: 9056882Abstract: The present invention provides a process for preparation of tenofovir by dealkylation of its phosphonate ester using Ionic complexes. The present invention also provides a process for preparation of tenofovir disoproxil or a salt thereof using the tenofovir of the present invention.Type: GrantFiled: November 15, 2012Date of Patent: June 16, 2015Assignee: Laurus Labs Private Ltd.Inventors: Venkata Sunil Kumar Indukuri, Sree Rambabu Joga, Seeta Ramanjaneyulu Gorantla, Satyanarayana Chava
-
Publication number: 20150141375Abstract: The present invention provides methods of treating diseases associated with at least one virus. The methods include administering a compound described in the invention in a therapeutically effective amount. According to some aspects of the present invention, the methods may further comprise at least one immunosuppressant agent to treat diseases associated with at least one virus of a subject in need of immunosuppressant agents.Type: ApplicationFiled: November 14, 2014Publication date: May 21, 2015Inventors: George R. Painter, Ernest Randall Lanier, Gwendolyn Painter
-
Publication number: 20150141376Abstract: Pharmaceutical compositions of anti-viral compounds, process for preparation and method of using the same are provided. Particularly, the present invention relates to chemically stable pharmaceutical compositions of efavirenz, emtricitabine and tenofovir disoproxil fumarate with optionally one or more pharmaceutically acceptable excipients, process for preparation and method for the treatment or prevention of the symptoms or effects of an HIV infection in an infected patient.Type: ApplicationFiled: November 18, 2014Publication date: May 21, 2015Inventors: Chandrashekhar Kandi, Nagaprasad Vishnubhotla, Asif Anwar, Krishna Kumar Chegonda, Sivakumaran Meenakshisunderam
-
Publication number: 20150132258Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventor: George D. Hartman
-
Publication number: 20150133400Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.Type: ApplicationFiled: September 15, 2014Publication date: May 14, 2015Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
-
Publication number: 20150133404Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.Type: ApplicationFiled: November 6, 2014Publication date: May 14, 2015Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Somasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda
-
Publication number: 20150119352Abstract: The invention provides a dinucleoside polyphosphate analogue, or a pharmaceutically acceptable salt thereof, for use in the inhibition (or down-regulation) of a pain, via a transducing ATP-gated P2X3 receptor, often by means of high-affinity desensitisation (HAD) mechanism.Type: ApplicationFiled: May 24, 2013Publication date: April 30, 2015Applicant: GlobalAcornLtd.Inventors: Andrew David Miller, Natalya Lozovaya, Nail Burnashev, Rashid Giniatullin
-
Patent number: 9018192Abstract: In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.Type: GrantFiled: October 10, 2013Date of Patent: April 28, 2015Assignee: Bristol-Myers Squibb & Gilead Sciences, Inc.Inventors: Terrence C. Dahl, Munir A. Hussain, Robert A. Lipper, Robert L. Jerzewski, Mark M. Menning, Reza Oliyai, Taiyin Yang
-
Publication number: 20150111856Abstract: The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (?)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.Type: ApplicationFiled: October 24, 2014Publication date: April 23, 2015Applicant: Gilead Sciences, Inc.Inventors: Terrence C. Dahl, Mark M. Menning, Reza Oliyai
-
Publication number: 20150111855Abstract: The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (?)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.Type: ApplicationFiled: October 24, 2014Publication date: April 23, 2015Applicant: Gilead Sciences, Inc.Inventors: Terrence C. Dahl, Mark M. Menning, Reza Oliyai
-
Publication number: 20150104502Abstract: Bolaamphiphilic compounds are provided according to formula I: HG2-L1-HG1??I where HG1, HG2 and L1 are as defined herein. Provided bolaamphiphilic compounds and the pharmaceutical compositions thereof are useful for delivering HIV active drugs into animal or human brain.Type: ApplicationFiled: July 10, 2014Publication date: April 16, 2015Inventors: Charles LINDER, Sarina GRINBERG, Eliahu HELDMAN
-
Publication number: 20150105351Abstract: The present invention is directed to novel nanomolar and picomolar inhibitors of HIV reverse transcriptase, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV-1 and HIV-2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.Type: ApplicationFiled: October 8, 2014Publication date: April 16, 2015Inventors: William L. Jorgensen, Karen S. Anderson
-
Publication number: 20150105350Abstract: The use of the hemifumarate form of {9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine} (tenofovir alafenamide hemifumarate) in combination with cobicistat is disclosed. In addition, the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and elvitegravir, and the combination of tenofovir alafenamide hemifumarate, cobicistat, emtricitabine, and darunavir, are disclosed.Type: ApplicationFiled: February 1, 2013Publication date: April 16, 2015Applicant: Gilead Sciences, Inc.Inventor: Srinivasan Ramanathan
-
Patent number: 9006218Abstract: The present invention relates to compounds and methods for treating viral diseases. Some compounds of the invention are described by Formula I: (I), wherein M+ is Na+, Li+, K+, Ca2+, Mg2+, or NRcRdReRf+ and Rc, Rd, Re and Rf are each independently hydrogen or C1-5 alkyl, or a stereoisomer, a diastereomer, an enantiomer or racemate thereof.Type: GrantFiled: February 14, 2011Date of Patent: April 14, 2015Assignee: Chimerix Inc.Inventors: Merrick Almond, Bernhard Lampert, Ernest Randall Lanier, Roy W. Ware
-
Publication number: 20150099722Abstract: The invention relates to compounds which are useful as inhibitors of 6-oxopurine phosphoribosyltransferases such as hypoxanthine-guanine-(xanthine) phosphoribosyltransferase (HG(X)PRT).Type: ApplicationFiled: May 7, 2013Publication date: April 9, 2015Inventors: John De Jersey, Luke William Guddat, Dana Hockova, Dianne Therese Keough
-
Publication number: 20150080344Abstract: There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.Type: ApplicationFiled: September 29, 2014Publication date: March 19, 2015Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
-
Publication number: 20150065464Abstract: The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions containing them.Type: ApplicationFiled: September 21, 2012Publication date: March 5, 2015Inventors: Rajendra Kharul, Debnath Bhuniya, Kasim A. Mookhtiar, Umesh Singh, Atul Hazare, Satish Patil, Laxmikant Datrange, Mahesh Thakkar
-
Publication number: 20150065465Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: ApplicationFiled: November 4, 2014Publication date: March 5, 2015Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
-
Publication number: 20150065415Abstract: In part, the present disclosure is directed to prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide compounds with significant solubility and bioavailability profiles.Type: ApplicationFiled: November 6, 2014Publication date: March 5, 2015Inventors: John J. Partridge, John Colucci, Yves Gareau, Michel Therien, Robert Zamboni, Barry Hafkin, Anthony Marfat, Helmi Zaghdane
-
Patent number: 8969357Abstract: The present invention features interferon-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to the subject effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), an inhibitor of cytochrome P450 (e.g., ritonavir), and ribavirin.Type: GrantFiled: December 23, 2013Date of Patent: March 3, 2015Assignee: AbbVie Inc.Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
-
Patent number: 8969324Abstract: Provided is a pharmaceutical composition comprising a 11-deoxy-prostaglandin compound represented by formula (I): and a fatty acid ester. By mixing the compound of formula (I) and a fatty acid ester, the compound of formula (I) will be stabilized.Type: GrantFiled: July 16, 2008Date of Patent: March 3, 2015Assignees: R-Tech Ueno, Ltd., Sucampo AGInventors: Yasuhiro Harada, Junichi Kawasaki, Yoshie Nishimura, Ryuji Ueno
-
Publication number: 20150051174Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: ApplicationFiled: October 29, 2014Publication date: February 19, 2015Inventors: Karl Y. Hostetler, James R. Beadle
-
Publication number: 20150045324Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Applicant: HANMI SCIENCE CO., LTDInventors: Mi Young CHA, Seok Jong KANG, Mi Ra KIM, Ju Yeon LEE, Ji Young JEON, Myoung Gi JO, Eun Joo KWAK, Kwang Ok LEE, Tae Hee HA, Kwee Hyun SUH, Maeng Sup KIM
-
Publication number: 20150038463Abstract: Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba(bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded.Type: ApplicationFiled: July 23, 2014Publication date: February 5, 2015Inventors: Bruce Liang, Kenneth A. Jacobson
-
Publication number: 20150038462Abstract: A method of inhibiting replication of a flavivirus in animal cells, and an oligonucleotide compound for use in the method are disclosed. The oligonucleotide analog (i) has a nuclease-resistant backbone, (ii) is capable of uptake by the cells, (iii) contains between 8-40 nucleotide bases, and (iv) has a sequence of at least 8 bases complementary to a region of the virus' positive strand RNA genome that includes at least a portion of SEQ ID NOS:1-4. Exposure of cells infected with a flavivirus to the analog is effective to form within the cells, a heteroduplex structure composed of the virus ssRNA and the oligonucleotide, characterized by a Tm of dissociation of at least 45° C., and having disrupted base pairing between the virus's 5? and 3? cyclization sequences.Type: ApplicationFiled: December 11, 2013Publication date: February 5, 2015Applicant: Sarepta Therapeutics, Inc.Inventors: Patrick L. Iversen, David A. Stein
-
Patent number: 8946244Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Hepatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.Type: GrantFiled: November 16, 2010Date of Patent: February 3, 2015Assignee: University of Georgia Research Foundation, Inc.Inventors: Chung K. Chu, Jianing Wang
-
Publication number: 20150031647Abstract: The present invention relates to a taste-masked dispersible tablet comprising a drug, a cation exchange resin, and other pharmaceutically acceptable excipients, such that the said drug and the said cation exchange resin are present in an un-complexed form in the tablet. It further relates to a process for the preparation of the same.Type: ApplicationFiled: February 21, 2013Publication date: January 29, 2015Applicant: RANBAXY LABORATORIES LIMITEDInventors: Vinod Kumar Arora, Jatin Khurana, Deepak Gaikwad
-
Patent number: 8940736Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: GrantFiled: July 12, 2013Date of Patent: January 27, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
-
Patent number: 8940717Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more inorganic fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. group (A): a group consisting of fludioxonil, pencycuron, ametoctradin, chloroneb, chlorothalonil, oxine-copper, cyflufenamid, dichlofluanid, dicloran, diethofencarb, dinocap, dithianon, edifenphos, fenaminosulf, fentin, fluazinam, fluoroimide, flusulfamide, flutianil, fosetyl-Al, hydrargaphen, iprobenfos, metrafenon, milneb, penflufen, phosdiphen, phthalide, prothiocarb, pyrazophos, sedaxane, silthiofam, spiroxamine, tebufloquin, and tolyfluanid.Type: GrantFiled: March 2, 2011Date of Patent: January 27, 2015Assignee: Sumitomo Chemical Company, LimitedInventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
-
Publication number: 20150025032Abstract: A pharmaceutical dosage system comprising (a) an effective amount of one or more of Doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof; (b) an effective amount of one or more of (i) Pyridoxine, (ii) an analog thereof, (iii) a derivative thereof, (iv) a prodrug thereof, (v) a metabolite thereof and (vi) a salt of any of (i)-(v); and (c) an effective amount of one or more compounds of formula (I) wherein R is H, PO3? or The system exhibits an improved pharmacokinetic profile relative to the current Diclectin®/Diclegis® formulation and is useful for example for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting of pregnancy (NVP).Type: ApplicationFiled: March 27, 2014Publication date: January 22, 2015Applicant: Duchesnay Inc.Inventors: Manon VRANDERICK, Jean-Luc ST-ONGE, Michele GALLO, Éric GERVAIS
-
Publication number: 20150025039Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, 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: ApplicationFiled: June 19, 2014Publication date: January 22, 2015Inventors: Constantine G. BOOJAMRA, Carina E. CANNIZZARO, James M. CHEN, Xiaowu CHEN, Aesop CHO, Lee S. CHONG, Maria FARDIS, Haolun JIN, Ralph HIRSCHMANN, Alan X. HUANG, Choung U. KIM, Thorsten A. KIRSCHBERG, Christopher P. LEE, William A. LEE, Richard L. MACKMAN, David Y. MARKEVITCH, David A. OARE, Vidya K. PRASAD, Hyung-Jung PYUN, Adrian S. RAY, Rosemarie O'SHEA, Sundaramoorthi SWAMINATHAN, William J. WATKINS, Jennifer R. ZHANG
-
Publication number: 20150018298Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
-
Publication number: 20150017651Abstract: Methods and composition for tumor therapy, especially esophageal adenocarcinoma (EAC), are described. For example, in certain aspects methods for determining Hedgehog and mTOR signaling pathway status to select patients for administering a combination therapy of Hedgehog and mTOR signaling inhibitors are described. Furthermore, the invention provides compositions that involve testing kits for determining signaling status.Type: ApplicationFiled: January 14, 2013Publication date: January 15, 2015Applicant: Board of Regents, The University of Texas SystemInventors: Mien-Chie Hung, Yan Wang, Jaffer Ajani
-
Publication number: 20150011509Abstract: Compounds of Formula (I) can be selectively lethal toward a variety of different cancer cell types. The compounds are useful for the management, treatment, control, or adjunct treatment of diseases, where the selective lethality is beneficial in chemotherapeutic therapy.Type: ApplicationFiled: October 12, 2012Publication date: January 8, 2015Applicants: The Board of Trustees of the University of Illnois, The Board of Regents of the University of Texas SystemInventors: Paul J. Hergenrother, David A. Boothman, Joseph S. Bair, Rahul Palchaudhuri, Elizabeth I. Parkinson
-
Publication number: 20150010509Abstract: Disclosed herein are methods for the treatment of cancer and inflammatory-based diseases and disorders, such as hepatitis B virus infection, tuberculosis and type 2 diabetes based upon the administration of CaFolate. In one embodiment is a method of treating cancer comprising administration of CaFolate. In another embodiment is a method of treatment inflammatory-based disease and disorders comprising administration of CaFolate.Type: ApplicationFiled: January 29, 2013Publication date: January 8, 2015Applicant: SanRx Pharmaceuticals, Inc.Inventor: Phillip Moheno
-
Publication number: 20150011488Abstract: Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins are applied (A) directly to a genital wart in the form of a cream, ointment, paste or solution, (B) directly to the genital wart wherein such cream, ointment, paste or solution contains as an additional active ingredient a skin permeabilizing agent, (C) following electrosurgical resection or removal of the genital wart in such form of a cream, ointment, paste or solution, (D) following chemical resection or extirpation of the genital wart in such form, (E) following surgical resection or removal of the genital wart in such form, wherein said Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins both provide antiviral activity against multiple strains of human pappilomavirus (HPV) and promote healing following resection polymers contained in a vehicle. Disclosed are the compositions, therapeutical kits containing such composition, methods of treatment using such composition, and methods of enhancing the stability of such composition.Type: ApplicationFiled: March 10, 2014Publication date: January 8, 2015Applicant: CACAO BIO-TECHNOLOGIES, LLCInventors: Daniel PRESTON, Randall B. MURPHY
-
Publication number: 20150004239Abstract: The invention provides solid particles comprising: a) a solid core that comprises an active pharmaceutical agent and b) a coating of Compound 2: (2) or a pharmaceutically acceptable salt of thereof on the core, as well as compositions comprising such particles, and methods for treating diseases (e.g. HIV infection) with such particles.Type: ApplicationFiled: January 11, 2013Publication date: January 1, 2015Inventors: Aaron J. Cullen, Richard Hung Chiu Yu
-
Publication number: 20140370102Abstract: This invention is directed to a composition comprising dry granulated tenofovir DF and emtricitabine, and a method for making same. Dry granulation was unexpectedly found to be important in preparing a tenofovir DF containing composition suitable for inclusion in a combination dosage form containing emtricitabine, efavirenz and tenofovir DF.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Inventors: Terrence C. Dahl, Mark M. Menning, Reza Oliyai, Taiyin Yang
-
Patent number: 8912170Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.Type: GrantFiled: April 12, 2013Date of Patent: December 16, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Rajinder Singh, Thomas Sun, Esteban Masuda
-
Publication number: 20140364397Abstract: The present disclosure relates, inter alia, to compositions and methods for treating viral diseases and cancer. There are disclosed lipophilic antiviral and anticancer acyclic nucleoside phosphonate diesters, preparation thereof, and methods of using the compounds to treat viral diseases and cancer.Type: ApplicationFiled: August 20, 2014Publication date: December 11, 2014Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
-
Publication number: 20140364389Abstract: The present invention relates to a combination therapy for treating an HIV infection or inhibiting integrase comprising (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (“Compound A”) or a pharmaceutically acceptable solvate or salt thereof in combination with at least one other anti-HIV agent. In some embodiments of the present invention, the other anti-HIV agents are chosen from reverse transcriptase inhibitors and protease inhibitors. In certain embodiments of the present invention, the other anti-HIV agents are chosen from AZT, 3TC, PMPA, efavirenz, indinavir, nelfinavir, a combination of AZT/3TC, and a combination of PMPA/3TC. Since Compound A has a high inhibitory activity specific for integrases, when used in combinations with other anti-HIV agents it can provide a combination therapy with fewer side effects for humans.Type: ApplicationFiled: December 12, 2013Publication date: December 11, 2014Applicant: JAPAN TOBACCO INC.Inventors: YUJI MATSUZAKI, WATARU WATANABE, SATORU IKEDA, MITSUKI KANO
-
Patent number: 8906852Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.Type: GrantFiled: April 8, 2011Date of Patent: December 9, 2014Assignee: MethylGene Inc.Inventors: Stéphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frédéric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
-
Publication number: 20140357598Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.Type: ApplicationFiled: June 20, 2014Publication date: December 4, 2014Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Somasekhar Bhamidipati, Esteban Masuda, Thomas Sun, Valentino J. Stella
-
Patent number: 8901105Abstract: In part, the present disclosure is directed to prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide compounds with significant solubility and bioavailability profiles.Type: GrantFiled: August 26, 2013Date of Patent: December 2, 2014Assignee: Debiopharm International SAInventors: John J. Partridge, John Colucci, Yves Gareau, Michel Therien, Robert Zamboni, Barry Hafkin, Anthony Marfat, Helmi Zaghdane
-
Publication number: 20140349971Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.Type: ApplicationFiled: August 7, 2014Publication date: November 27, 2014Inventor: Paul STOFFELS
-
Publication number: 20140349969Abstract: The present invention relates to new therapies to treat pain and related diseases, as well as pharmaceutical compounds for use in said therapies.Type: ApplicationFiled: May 8, 2014Publication date: November 27, 2014Inventors: Josef PENNINGER, Graham Gregory NEELY, Shane MCMANUS, Henrik NILSSON
-
Publication number: 20140349970Abstract: The invention provides a compound of Formula (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), or (Il) as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Applicant: ABBVIE INC.Inventors: Neil Wishart, Maria A. Argiriadi, Eric C. Breinlinger, David J. Calderwood, Anna M. Ericsson, Bryan A. Fiamengo, Kristine E. Frank, Michael Friedman, Dawn M. George, Eric R. Goedken, Michael Z. Hoemann, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Kelly D. Mullen, Gagandeep Somal, Kent D. Stewart, Jeffrey W. Voss, Grier A. Wallace, Lu Wang, Kevin R. Woller
-
Publication number: 20140343006Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Inventors: Jerome Emile Georges Guillemont, Patrice Palandijian, Marc Rene DeJonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
-
Publication number: 20140323441Abstract: The present invention relates to purine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.Type: ApplicationFiled: November 8, 2012Publication date: October 30, 2014Inventors: Jean-François Bonfanti, Frédéric Marc Maurice Doublet, Werner Embrechts, Jérôme Michel Claude Fortin, David Craig Mc Gowan, Philippe Muller, Piere Jean-Marie Bernand Raboisson