Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/214.02)
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Patent number: 8663700Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.Type: GrantFiled: June 11, 2013Date of Patent: March 4, 2014Assignee: BIND Therapeutics, Inc.Inventors: Greg Troiano, Michael Figa, Abhimanyu Sabnis
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Publication number: 20140057899Abstract: The present invention provides a new compound that has an inhibitory action against EGFR and that has cell growth inhibitory effects. The present invention further provides a pharmaceutical preparation useful for preventing and/or treating cancer, based on the EGFR inhibitory effect of the compound. A compound represented by the following Formula (I) or a salt thereof.Type: ApplicationFiled: February 22, 2013Publication date: February 27, 2014Applicant: Taiho Pharmaceutical Co., Ltd.Inventors: Takeshi Sagara, Satoru Ito, Sachie Otsuki, Katsumasa Nonoshita
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Patent number: 8652528Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.Type: GrantFiled: April 12, 2013Date of Patent: February 18, 2014Assignee: BIND Therapeutics, Inc.Inventors: Greg Troiano, Michael Figa, Abhimanyu Sabnis
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Publication number: 20140045816Abstract: The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: October 8, 2013Publication date: February 13, 2014Inventors: John A. Bender, Min Ding, Robert G. Gentles, Piyasena Hewawasam
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Publication number: 20140045819Abstract: This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.Type: ApplicationFiled: April 20, 2012Publication date: February 13, 2014Applicants: ElexoPharm GmbH, SCHERING CORPORATIONInventors: Scott B. Hoyt, Whitney Lane Petrilli, Clare London, Yusheng Xiong, Jerry Andrew Taylor, Amjad Ali, Michael Man-Chu Lo, Timothy J. Henderson, Qingzhong Hu, Rolf Hartmann, Lina Yin, Ralf Heim, Emmanuel Bey, Rohit Saxena, Swapan Kumar Samanta, Bheemashankar A. Kulkarni
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Publication number: 20140018348Abstract: Compositions and methods tor the treatment of depression and psychoses in humans are disclosed. More particularly, the invention is directed to formulations containing antipsychotic and/or antidepressant medications and also containing an NMPAR antagonist. The present invention is also directed to methods for the treatment of humans suffering from depression and other psychoses, including, schizophrenia, by administration of the inventive compositions in antidepressant and/or antipsychotic effective amounts.Type: ApplicationFiled: July 7, 2013Publication date: January 16, 2014Inventor: Daniel C. Javitt
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Patent number: 8629134Abstract: This invention relates to a process for the hydrogenation of a ketooxime to selectively form an aminoalcohol stereoisomer, and, in particular, to a process for the hydrogenation of 4,5-dihydro-imidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or a salt thereof to selectively form a stereoisomer of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one or a salt thereof. This invention also relates to the use of the 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one hydrogenation product or a salt thereof to selectively make a stereoisomer of zilpaterol or a salt thereof, as well as the use of such a zilpaterol stereoisomer or salt in methods of treatment and medicaments for animals.Type: GrantFiled: January 31, 2008Date of Patent: January 14, 2014Assignee: Intervet International B.V.Inventors: Juan Jose Almena-Perea, Monika Brink, Gerhard Geiβ, Renat Kadyrov, Thorsten Meyer
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Patent number: 8623862Abstract: The present invention relates to compounds corresponding to formula (I): X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.Type: GrantFiled: September 13, 2011Date of Patent: January 7, 2014Assignee: SanofiInventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
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Publication number: 20130345197Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: June 3, 2013Publication date: December 26, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
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Publication number: 20130344139Abstract: A method and preparation for reducing dry eye symptoms and promoting tear secretion in a subject in need of such treatment is disclosed. The method is useful in treating dry eye diseases. The method is also useful in reducing contact lens intolerance in the eyes. The method comprises administering to the eyes of a subject in need thereof a non-drying antihistamine compound, such as epinastine hydrochloride, in an amount effective to reduce dry eye symptoms and stimulate tear fluid secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the compound include topical administration via a liquid, gel, cream, or as part of a contact lens or a continuous or selective release device; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form, injectable, intra-operative instillation or suppository form.Type: ApplicationFiled: August 29, 2013Publication date: December 26, 2013Inventors: Benjamin R. Yerxa, Jason L. Vittitow, John C. Ice, Ramesh Krisnamoorthy
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Publication number: 20130338141Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.Type: ApplicationFiled: August 19, 2013Publication date: December 19, 2013Inventors: Richard C. Isaacs, Wayne J. Thompson, Peter D. Williams, Dai-Shi Su, Shankar Venkatraman, Mark W. Embrey, Thorsten E. Fisher, John S. Wai, David C. Dubost, Richard G. Ball, Eric J. Choi, Tao Pei, Sarah L. Trice, Neil Campbell, Matthew Maddes, Peter E. Maligres, Michael Shevlin, Zhiguo Jake Song, Dietrich P. Steinhuebel, Neil A. Strotman, Jingjun Yin
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Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as Axl inhibitors
Patent number: 8609650Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: July 26, 2011Date of Patent: December 17, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Patent number: 8609142Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.Type: GrantFiled: December 13, 2012Date of Patent: December 17, 2013Assignee: BIND Therapeutics, Inc.Inventors: Greg Troiano, Michael Figa, Abhimanyu Sabnis
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Publication number: 20130331376Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: August 14, 2013Publication date: December 12, 2013Applicant: Elan Corporation, Inc.Inventors: Robert A. Galemmo, Dean R. Artis, Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20130324506Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.Type: ApplicationFiled: June 5, 2013Publication date: December 5, 2013Inventors: Isabelle BERREBI-BERTRAND, Xavier BILLOT, Thierry CALMELS, Marc CAPET, Stéphane KRIEF, Olivier LABEEUW, Jeanne-Marie LECOMTE, Nicolas LEVOIN, Xavier LIGNEAU
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Publication number: 20130310367Abstract: A method of enhancing the performance of chicken comprising administering zilpaterol to the chicken wherein the concentration of zilpaterol is from about 1 ppm to about 13 ppm and is administered every day for a period of about 7 to about 21 days.Type: ApplicationFiled: May 17, 2013Publication date: November 21, 2013Inventor: John A. Rogers
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Publication number: 20130310368Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.Type: ApplicationFiled: July 22, 2013Publication date: November 21, 2013Inventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Bhadra Shelat, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
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Publication number: 20130287687Abstract: The present disclosure relates to organic chemistry and in particular to a series of corticotropin releasing factor type-1 (CRF1) receptor ligand compounds and compositions, as well as methods of preparation and treatment.Type: ApplicationFiled: April 30, 2013Publication date: October 31, 2013Inventor: EMORY UNIVERSITY
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Patent number: 8568975Abstract: Disclosed herein is a method of sorting, treating, and feeding a group of bovine animals in a feed lot, wherein the method may include the steps of determining an ob genotype of each animal, comparing the relative weight and back fat of each animal with the other animals, dividing the animals into subgroups based on weight, back fat, and ob genotype. Zilpaterol hydrochloride (ZH) may be added to a feed ration fed to animals only in selected subgroups. Each group is fed a finishing period and then moved lot to slaughter. Each slaughter date and finishing period is independent of other subgroups.Type: GrantFiled: April 21, 2011Date of Patent: October 29, 2013Inventor: Leigh Marquess
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Publication number: 20130274247Abstract: Methods for stimulating appetite in cats in need thereof are disclosed.Type: ApplicationFiled: June 1, 2012Publication date: October 17, 2013Inventors: Jessica Quimby, Katharine Lunn
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Publication number: 20130237524Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.Type: ApplicationFiled: March 7, 2013Publication date: September 12, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald G. Payan, Sylvia Braselmann
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Publication number: 20130237526Abstract: The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.Type: ApplicationFiled: April 24, 2013Publication date: September 12, 2013Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Hiroshi Kase, Minoru Kobayashi, Shizuo Shiozaki, Akihisa Mori, Naoki Seno
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Patent number: 8524703Abstract: The present application relates to indole and indoline derivatives of formula (I), formula (II), formula (III), or formula (IV) wherein a, R2, R3, h, k, m, n, L, Q, X, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions.Type: GrantFiled: December 14, 2010Date of Patent: September 3, 2013Assignee: AbbVie Inc.Inventors: Lei Shi, William H. Bunnelle, Tao Li, Marc J. Scanio, Michael R. Schrimpf, Chih-Hung Lee
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Publication number: 20130225549Abstract: The present invention relates to dihydropteridinones, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.Type: ApplicationFiled: February 14, 2013Publication date: August 29, 2013Applicant: Boehringer Ingelheim International GmbHInventor: Boehringer Ingelheim International GmbH
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Publication number: 20130225559Abstract: The invention provides a method of treatment of hot flush with S-mirtazapine and the use of S-mirtazapine for the manufacture of a medicament for the treatment of hot flush.Type: ApplicationFiled: April 5, 2013Publication date: August 29, 2013Applicant: N.V. OrganonInventors: Bernardus Wijnand Mathys Marie Peeters, Anton Egbert Peter Adang
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Publication number: 20130225558Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: August 29, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Publication number: 20130217620Abstract: The present invention relates to ionic silicone hydrogel contact lenses which comprise at least one pharmaceutical or nutriceutical component and are formed from reaction mixtures comprising a mixture of slow-reacting hydrophilic monomers, including at least one slow-reacting ionic monomer, at least one silicone-containing component and at least one hydroxyl-containing component, wherein the ratio of the slow-reacting hydrophilic component half lives to the silicone-containing component half life is at least 2.Type: ApplicationFiled: March 14, 2013Publication date: August 22, 2013Applicant: Johnson & Johnson Vision Care, Inc.Inventor: Johnson & Johnson Vision Care, Inc.
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Patent number: 8513235Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.Type: GrantFiled: April 10, 2009Date of Patent: August 20, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
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Patent number: 8513234Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X1, X2, Y, R1A, R1B, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.Type: GrantFiled: October 2, 2009Date of Patent: August 20, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Richard C. A. Isaacs, Wayne J. Thompson, Peter D. Williams, Dai-Shi Su, Shankar Venkatraman, Mark W. Embrey, Thorsten E. Fisher, John S. Wai, David C. Dubost, Richard G. Ball, Eric J. Choi, Tao Pei, Sarah L. Trice, Neil Campbell, Matthew Maddess, Peter E. Maligres, Michael Shevlin, Zhiguo Jake Song, Dietrich P. Steinhuebel, Neil A. Strotman, Jingjun Yin
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Publication number: 20130210803Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: August 15, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Patent number: 8507472Abstract: Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted microorganisms in crop protection and the protection of materials and for reducing mycotoxins in plants and plant parts, and also processes for preparing compounds of the formula (I).Type: GrantFiled: April 5, 2011Date of Patent: August 13, 2013Assignee: Bayer CropScience AGInventors: Amos Mattes, Hendrik Helmke, Stefan Hillebrand, Gorka Peris, Alexander Sudau, Lars Rodefeld, Stefan Gauger, Jürgen Benting, Peter Dahmen, Ruth Meissner, Ulrike Wachendorff-Neumann, Hiroyuki Hadano
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Publication number: 20130189315Abstract: The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 1 to about 20 weight percent of a vinca alkaloid; and about 50 to about 99 weight percent biocompatible polymer.Type: ApplicationFiled: October 25, 2012Publication date: July 25, 2013Inventors: Stephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
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Publication number: 20130165425Abstract: Disclosed herein are sulfate esters of noribogaine or 9,17 dihydronoribogaine, and pharmaceutically acceptable salts of each thereof, pharmaceutical compositions comprising such compounds, and methods of their use, including in treating addiction and/or pain.Type: ApplicationFiled: December 7, 2012Publication date: June 27, 2013Applicant: DEMERX, INC.Inventor: DemeRx, Inc.
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Publication number: 20130165414Abstract: Disclosed herein are phosphate esters of noribogaine and dihydronoribogaine, and esters and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the methods of their use, including in the treatment of addiction and/or pain.Type: ApplicationFiled: December 7, 2012Publication date: June 27, 2013Applicant: DEMERX, INC.Inventor: DemeRx, Inc.
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Publication number: 20130131046Abstract: Disclosed are noribogaine compositions comprising a very high level of the 2(R), 4(S), 5(S), 6(S) and 18(R) enantiomer and not more than 0.5 wt % of ibogaine relative to the total amount of noribogaine.Type: ApplicationFiled: July 22, 2011Publication date: May 23, 2013Inventors: Robert M. Moriarty, Deborah C. Mash
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Publication number: 20130116241Abstract: The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: October 25, 2012Publication date: May 9, 2013Applicants: AbbVie Inc., Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, AbbVie Inc.
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Publication number: 20130116242Abstract: The invention provides a method to effectively wean a woman from hormone therapy for treatment of vasomotor symptoms by reducing the dosage of the hormonal agent to zero, while a non-hormonal drug in an amount, which is therapeutically effective for treating vasomotor symptoms, is administered or initiated and continued for a limited period of a duration between 3 and 8 months.Type: ApplicationFiled: December 20, 2012Publication date: May 9, 2013Inventor: Edward Baker
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Publication number: 20130109673Abstract: This invention generally relates to processes for making zilpaterol and salts thereof, as well as processes for making intermediates that, inter alia, may be used to make zilpaterol and salts thereof. This invention also relates to methods of treatment using zilpaterol and salts prepared in accordance with this invention to increase the rate of weight gain, improve feed efficiency, and/or increase carcass leanness in livestock, poultry, and fish.Type: ApplicationFiled: December 18, 2012Publication date: May 2, 2013Inventors: Stéphane Dubuis, Oliver Krebs
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Patent number: 8420123Abstract: The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.Type: GrantFiled: June 16, 2009Date of Patent: April 16, 2013Assignee: BIND Biosciences, Inc.Inventors: Greg Troiano, Michael Figa, Abhimanyu Sabnis
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Publication number: 20130085133Abstract: The present disclosure relates to novel compounds of formulas (1) through (19) and to a method for treating humans infected with a virus including various respiratory viruses such as members of the Paramyxoviridae family (respiratory syncytial virus (RSV), human metapneumovirus (HMPV), human parainfluenza virus (HPIV), measles virus, and mumps virus) with a compound of formulas (1) through (19). The present disclosure also relates to a cytopathic effect (CPE)-based assay that will assess virus-induced CPE for screening of compounds for treating viral diseases or inhibiting a virus.Type: ApplicationFiled: February 8, 2011Publication date: April 4, 2013Applicant: Sourthern Research Institute Office of Commercialization and Intellectual Prop.Inventors: Bill Severson, Dong Hong Chung, Colleen B. Jonsson, Ellie Lucile White, Lynn Rasmussen, Clinton Boykin Maddox, Subramaniam Ananthan, Ashish K. Pathak, Joseph A. Maddry
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Publication number: 20130079306Abstract: A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.Type: ApplicationFiled: July 1, 2011Publication date: March 28, 2013Inventors: Hiroshi Uchida, Akira Asagarasu, Teruaki Matsui
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Publication number: 20130072472Abstract: Stable noribogaine salt ansolvates are useful for preparing pharmaceutical compositions and for alleviating nociceptive pain in a patient. Such ansolvates can be prepared by slurrying solvated forms, preferably MeOH solvated noribogaine hydrochloride in EtOH/water.Type: ApplicationFiled: September 14, 2012Publication date: March 21, 2013Inventors: Richard D. Gless, JR., William C. Schinzer
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Publication number: 20130045962Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined below and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.Type: ApplicationFiled: November 6, 2008Publication date: February 21, 2013Inventors: Donghui Qin, Beth Norton, Xiangmin Liao, Andrew Nicholson Knox, Jinhwa Lee, Yuhong Fang, Jason Christopher Dreabit, Siegfried Benjamin Christensen, IV, Andrew B. Benowitz, Kelly M. Aubart
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Patent number: 8377923Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.Type: GrantFiled: July 2, 2009Date of Patent: February 19, 2013Assignee: Astellas Pharma Inc.Inventors: Seiji Yoshimura, Noriyuki Kawano, Tomoaki Kawano, Daisuke Sasuga, Takanori Koike, Hideyuki Watanabe, Hiroki Fukudome, Nobuyuki Shiraishi, Ryosuke Munakata, Hiroaki Hoshii, Kayoko Mihara
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Publication number: 20130028865Abstract: The present invention relates to a combination of a macrocyclic HCV protease inhibitor, a macrocyclic non-nucleoside HCV polymerase inhibitor and a nucleoside HCV polymerase inhibitor.Type: ApplicationFiled: April 13, 2011Publication date: January 31, 2013Applicants: MEDIVIR AB, JANSSEN PHARMACEUTICALS, INC.Inventors: Tse-I Lin, Oliver Lenz, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8362007Abstract: This invention relates noribogaine derivatives, compositions and methods of use thereof.Type: GrantFiled: May 10, 2011Date of Patent: January 29, 2013Assignee: Demerx, Inc.Inventors: Deborah C. Mash, Richard D. Gless, Jr., Robert M. Moriarty
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Patent number: 8362006Abstract: This invention generally relates to processes for making zilpaterol and salts thereof, as well as processes for making intermediates that, inter alia, may be used to make zilpaterol and salts thereof. The zilpaterol and salts prepared in accordance with this invention can be used to increase the rate of weight gain, improve feed efficiency, and/or increase carcass leanness in livestock, poultry, and fish.Type: GrantFiled: March 28, 2008Date of Patent: January 29, 2013Assignee: Intervet International B.V.Inventors: Oliver Krebs, Stephane Dubuis
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Publication number: 20130023520Abstract: An eye drop solution includes an anaesthetic and at least one medicament. The anaesthetic is preferably provided in a range of from about 0.001% to about 1.0%. The eye drop solution may further include either a lubricant or a preservative, or both of these.Type: ApplicationFiled: July 24, 2011Publication date: January 24, 2013Inventor: Amir Sahba Jalali
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Publication number: 20130005708Abstract: Presented herein inter alia are compositions, methods, and kits for treating an inflammatory skin disorder using a histamine antagonist. In certain embodiments, the compositions, methods, and kits are for treating urticaria and its symptoms. In certain embodiments, the composition, methods, and kits include a topical pharmaceutical preparation with an effective amount of alcaftadine as an active agent.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Inventor: DINUSHA N. LALWANI
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Patent number: 8343956Abstract: This invention generally relates to processes for making a crystalline zilpaterol salt, particularly zilpaterol hydrochloride. This invention also relates to methods of treatment using a crystalline zilpaterol salt prepared in accordance with this invention to increase the rate of weight gain, improve feed efficiency, and/or increase carcass leanness in livestock, poultry, and fish.Type: GrantFiled: March 3, 2011Date of Patent: January 1, 2013Assignee: Intervet International B.V.Inventors: Oliver Krebs, Philipp Kuenti, Christoph Michlig, Karl Reuter