Patents Issued in September 20, 2016
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Patent number: 9447060Abstract: The present invention provides a small molecule treatment of diseases/conditions caused by a virus carrying a viral oncoprotein. In one embodiment, the virus which carries the viral oncoprotein is HPV. The small molecule useful herein includes thiadiazolin-3,5-dione compounds having an optionally substituted aryl group bound to one nitrogen atom of said thiadiazolin-3,5-dione compound. The small molecules may also be administered with a compound which inhibits binding of HPV E6 to p53. In one embodiment, the thiadiazolin-3,5-dione compound has formula (I), or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R1 and R2 are defined herein.Type: GrantFiled: November 6, 2012Date of Patent: September 20, 2016Assignee: The Wistar Institute of Anatomy and BiologyInventors: Ronen Marmorstein, Daniela Fera
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Patent number: 9447061Abstract: The present invention pertains to a process for preparing a product rich in epichlorohydrin, comprising the steps of: a) reacting a mixture of dichlorohydrin and a base at a temperature in the range of 0-40° C. during a period of time in the range from 1 second to 180 minutes, wherein the base is present in a less than stoichiometric amount, to obtain a reaction mixture comprising epichlorohydrin and brine; b) subjecting at least part of the reaction mixture to a separation step to form a product fraction which is rich in epichlorohydrin and a brine fraction which is lean in epichlorohydrin; c) subjecting at least part of the brine fraction to a purification step to yield a purified brine. It has been found that the process according to the invention allows the manufacture of epichlorohydrin from dichlorohydrin on an industrial scale at high yield, while at the same time providing a brine with a low total organic carbon content without extensive separation being necessary.Type: GrantFiled: October 23, 2013Date of Patent: September 20, 2016Assignee: Akzo Nobel Chemicals International B.V.Inventors: Carolina Anna Maria Christina Dirix, André Michiel Koolaard, Antoon Jacob Berend Ten Kate, Eilertdina Henderika Renkema
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Patent number: 9447062Abstract: A manumycin-type metabolite called Colabomycin E which inhibits caspase 1 and creation of interleukins, strain produces the Colabomycin E and a method of a production of the Colabomycin E. Colabomycin E is a new member of the manumycin-type metabolites produced by the strain Streptomyces aureus SOK1/5-04 deposited in The Czech collection of microorganisms under number CCM8556. The structure of 5 is similar to that of the already known metabolite colabomycin A (3) isolated from Streptomyces griseoflavus. However, the upper polyene chain of 5 is two carbons longer. Therefore, it was named Colabomycin E. Biological activity assays indicated that colabomycin E significantly inhibited IL-1? release from THP-1 cells and might thus potentially act as an anti-inflammatory agent.Type: GrantFiled: December 15, 2014Date of Patent: September 20, 2016Assignees: BIOLOGY CENTRE AS CR, V.V.I., INSTITUTE OF MICROBIOLOGYH AS CR, V.V.I., INSTITUTE FOR CLINICAL AND EXPERIMENTAL MEDICINEInventors: Miroslav Petricek, Katerina Petrickova, Stanislav Pospisil, Marek Kuzma, Alica Chronakova, Vaclav Kristufek, Ilja Striz
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Patent number: 9447063Abstract: The present invention relates to a novel disubstituted adamantyl derivative or the pharmaceutically acceptable salts thereof, a method for preparing the same, and a pharmaceutical anticancer or antimetastasis composition comprising the same as an active ingredient. The disubstituted adamantyl derivative of the present invention suppressed accumulation of HIF-1?, inhibiting the expression of the metastasis related protein Twist dose-dependently. Thus, the disubstituted adamantyl derivative of the invention is effective in inhibiting the expressions of the metastasis related proteins, ?-catenin and RohA, and the EMT related genes such as MMP2 and MMP9, without cytotoxicity. Therefore, the disubstituted adamantyl derivative or the pharmaceutically acceptable salts thereof of the invention can be efficiently used as a pharmaceutical anticancer or antimetastasis composition.Type: GrantFiled: May 28, 2015Date of Patent: September 20, 2016Assignees: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY, DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATIONInventors: Mi Sun Won, Kyeong Lee, Bo Kyung Kim, Hyun Seung Ban, Seohyun Son, Kyung-Sook Chung
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Patent number: 9447064Abstract: Disclosed is a process for selectively producing (D+1)-member heterocyclic compounds from corresponding unactivated dienes or derivatives thereof in the presence of a transition metal or lanthanide catalyst or a precursor thereof, relative to D-member heterocyclic rings.Type: GrantFiled: April 30, 2014Date of Patent: September 20, 2016Assignee: THE CHINESE UNIVERSITY OF HONG KONGInventor: Chun Yu Ho
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Patent number: 9447065Abstract: The present invention provides a pharmaceutical composition which prevents from decreasing the blood exposure of the third generation coxib-drugs, a process for preparing the said pharmaceutical composition and its use. It has been founded in this invention that adding a basic amine or a basic amino acid, or a cyclodextrin to the third generation coxib-drug can afford a pharmaceutical composition which can prevent from decreasing the blood exposure, AUC and bioavailability. The pharmaceutical composition of the present invention has also good stability, which is useful for drugs. Namely, the technological thought that adding a basic amine or a basic amino acid, or a cyclodextrin to the third generation coxib-drug can prevent from decreasing the blood exposure, AUC and bioavailability has been established in this invention.Type: GrantFiled: October 18, 2012Date of Patent: September 20, 2016Assignee: RaQualia Pharma Inc.Inventors: Yasuhiro Iwata, Kaoru Shimada, Yoshiyuki Okumura, Mayumi Kashino, Hiromitsu Yoshida
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Patent number: 9447066Abstract: This invention relates to salts and crystal forms of (S)-6-chloro-7-(1,1-dimethylethyl)-2-trifluoromethyl-2H-1-benzopyran-3-carboxylic acid, Compound A, which is cyclooxygenase-2 inhibitor. The present invention provides a salt of compound A, a crystal form thereof, a process for preparing the said salt and a pharmaceutical composition thereof and its use. The salts and/or co-crystals of Compound A of the present invention show good formulation properties such as high aqueous solubility, good intrinsic dissolution, good crystallinity, good thermal stability or low hygroscopicity.Type: GrantFiled: January 6, 2014Date of Patent: September 20, 2016Assignee: AskAt Inc.Inventors: Yoshiyuki Okumura, Yasuhiro Iwata, Toyoharu Numata, Masaki Sudo, Takako Okumura
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Patent number: 9447067Abstract: A method of preparing an intermediate of salmeterol (Compound 1, 2-amino-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol) includes: reacting compound 2 with 2-methoxypropene in a first organic solvent to produce a reaction solution including compound 3, compound 2 including a 2-bromo precursor of Compound 1; reacting compound 3 with a nitrogen source to produce compound 4; reacting compound 4 with sodium borohydride in a second organic solvent to produce compound 5; and debenzylating compound 5 by ammonium formate/palladium-carbon catalytic transfer hydrogenation in a third organic solvent to produce Compound 1. A method of preparing salmeterol includes preparing Compound 1, and reacting Compound 1 to prepare salmeterol.Type: GrantFiled: May 15, 2015Date of Patent: September 20, 2016Assignee: Amphastar Pahmaceuticals, Inc.Inventors: Yinhua Qiu, Zhengyuan Wu, Song Chen, Haoning Zhang
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Patent number: 9447068Abstract: The invention relates to functionalized polymers including homopolymers and copolymers and their uses in industrial applications and in agricultural applications. In particular, the homopolymers and copolymers may be, for example, used in polymer blends, used as nutritives and in feed compositions, and used in combination with a pharmaceutical or nutritive.Type: GrantFiled: November 10, 2015Date of Patent: September 20, 2016Assignee: NOVUS INTERNATIONAL, INC.Inventors: Graciela B. Arhancet, Matthew Mahoney, Xiaojun Wang, Rangarani Karnati
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Patent number: 9447069Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.Type: GrantFiled: April 30, 2013Date of Patent: September 20, 2016Assignee: INNOV17 LLCInventors: Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn
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Patent number: 9447070Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: September 18, 2014Date of Patent: September 20, 2016Assignee: Celgene CorporationInventors: George W. Muller, Roger Shen-Chu Chen, Alexander L. Ruchelman
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Patent number: 9447071Abstract: Disclosed are crystalline free base ansolvate forms of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1), such as the free base Form I, Form II and Material N. Also disclosed are crystalline free base solvates of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1).Type: GrantFiled: February 6, 2015Date of Patent: September 20, 2016Assignee: Global Blood Therapeutics, Inc.Inventors: Zhe Li, Stephan D. Parent, Travis Houston
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Patent number: 9447072Abstract: General formula (I): The present invention pertains to: a pyridone derivate or a salt thereof represented by general formula (I); or a medicine containing the pyridone derivative or salt thereof as an active ingredient. [In the formula, ring A, R1, R2, R3 and R4 are specific groups.Type: GrantFiled: December 7, 2012Date of Patent: September 20, 2016Assignee: KAKEN PHARMACEUTICAL CO., LTD.Inventors: Noriyuki Kamei, Yoshitake Sumikawa, Daigo Kamimura, Shingo Todo, Takuya Yamada, Shota Tokuoka
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Patent number: 9447073Abstract: The instant invention describes tetrazole compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: May 28, 2014Date of Patent: September 20, 2016Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Michael R. Loso, Gary D. Gustafson, Daniel Knueppel, Zachary A. Buchan, Michael T. Sullenberger
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Patent number: 9447074Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.Type: GrantFiled: February 19, 2015Date of Patent: September 20, 2016Assignee: Glaxo Group LimitedInventors: Francis Louis Atkinson, Michael David Barker, John Liddle, David Matthew Wilson
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Patent number: 9447075Abstract: Pyridazine derivatives that activate the excitatory amino acid transporter 2 (EAAT2), and methods use thereof for treating or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.Type: GrantFiled: August 2, 2012Date of Patent: September 20, 2016Assignees: The Brigham and Women's Hospital, Inc., The Ohio State UniversityInventors: Gregory D. Cuny, Marcie Glicksman, Xeuchao Xing, Chien-Liang Glenn Lin
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Patent number: 9447076Abstract: A compound has the following formula: The compound is a p38 MAP kinase inhibitor. The compound and its pharmaceutically acceptable salts can be used for treatment of conditions, such as inflammatory diseases.Type: GrantFiled: February 13, 2015Date of Patent: September 20, 2016Assignees: RESPIVERT LTD., TOPIVERT PHARMA LTD.Inventors: Alistair Ian Longshaw, Euan Alexander Fraser Fordyce, Stuart Thomas Onions, John King-Underwood, Jennifer Venable
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Patent number: 9447077Abstract: Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.Type: GrantFiled: September 19, 2014Date of Patent: September 20, 2016Assignee: SARcode Bioscience Inc.Inventors: John Burnier, Thomas Gadek, Frederic Naud
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Patent number: 9447078Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: GrantFiled: January 18, 2013Date of Patent: September 20, 2016Assignee: ACUCELA INC.Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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Patent number: 9447079Abstract: Described herein are compounds of Formula (I-a) and (I-b), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.Type: GrantFiled: March 14, 2014Date of Patent: September 20, 2016Assignee: Epizyme, Inc.Inventors: Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin, Oscar Miguel Moradei, Kevin Wayne Kuntz
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Patent number: 9447080Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.Type: GrantFiled: April 11, 2013Date of Patent: September 20, 2016Assignee: BIOTA SCIENTIFIC MANAGEMENT PTY LTD.Inventors: Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding, Silas Bond, Rosliana Halim
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Patent number: 9447081Abstract: The invention discloses a homopiperony lamine compound which has a structural general formula I as follows as shown in the specification: wherein definitions of substituents in the formula are as shown in the specification. The compound shown as the general formula I has broad-spectrum bactericidal and insecticidal activity in the field of agriculture. The compound shown as the general formula I has a good prevention effect on various germs such as cucumber downy mildew, wheat powdery mildew, puccinia sorghi, rice blast and cucumber gray mold, and particularly, still has the good prevention and control effect on the cucumber downy mildew, the puccinia sorghi and the wheat powdery mildew at a lower dosage. At the same time, a part of compound has better insecticidal activity, and can be used for preventing and controlling various insect pests such as diamondback moths, myzus persicae, armyworms and tetranychus cinabarinus boisdu.Type: GrantFiled: October 24, 2013Date of Patent: September 20, 2016Assignee: SHENYANG SINOCHEM AGROCHEMICALS R&D CO., LTD.Inventors: Changling Liu, Aiying Guan, Jie Lan, Lizeng Wang, Bin Wang, Minna Zhu, Qin Sun, Weijing Ren, Cong Feng, Lanhui Ren, Baoshan Chai, Zhinian Li
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Patent number: 9447082Abstract: The invention discloses optically active compounds of Formula (1a) or Formula (1b), wherein R1 and R2 are independently selected from the group consisting of hydrogen and a halogen selected from the group consisting of fluorine, chlorine, bromine, and iodine; and wherein (a) R3 and R4 are independently selected from the group consisting of hydrogen and an alkyl group having a linear or branched chain having 1 to 20 carbon atoms, or (b) R3 and R4 together form a cycloalkyl ring having 3 to 10 carbon atoms fused to the thiophene ring; and wherein R5 is CN or COOR?, where R? is methyl or ethyl. The compounds of Formula (1a) or Formula (1b) may be used in pharmaceutical compositions for treating fungal infections.Type: GrantFiled: April 29, 2014Date of Patent: September 20, 2016Assignees: FDC Limited, Council of Scientific Industrial ResearchInventors: Hanumant Bapurao Borate, Sangeshwer Prabhakar Sawargave, Subhash Prataprao Chavan, Mohan Anand Chandavarkar, Ramakrishnan Ramacahndran Iyer, Amit Chandrakant Tawte, Deepali Damodar Rao
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Patent number: 9447083Abstract: The present invention relates to novel N-acylhydrazone derivatives, and more particularly to novel N-acylhydrazone derivatives having selective T cell inhibitory activity and/or anti-lymphoid malignancy activity, stereoisomers thereof, pharmaceutically acceptable salts thereof, the use thereof for preparing pharmaceutical compositions, pharmaceutical compositions containing the same, treatment methods using the compositions, and methods for preparing the novel N-acylhydrazone derivatives.Type: GrantFiled: August 29, 2013Date of Patent: September 20, 2016Assignees: CHONG KUN DANG PHARMACEUTICAL CORP., INJE UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATIONInventors: HoJin Choi, JaeWon Lee, ChangGon Lee, NiNa Ha, Su Kil Seo, SunMi Lee, Song-Min Lee
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Patent number: 9447084Abstract: The present invention relates to novel and inventive isoxazoline of formula (I) and salts thereof: wherein variables D1, D2, D3, D4, D5, R1, B1, B2, B3, R2, R3, R4, R5, R6, Y, Z, L, a and b are described herein are as defined in the description. The invention also relates to parasiticidal and pesticidal compositions comprising the isoxazoline compounds of formula (I), processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.Type: GrantFiled: October 30, 2014Date of Patent: September 20, 2016Assignee: MERIAL, INC.Inventor: Charles Q Meng
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Patent number: 9447085Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted iminothiadiazine compounds, or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers. The novel compounds of the invention are as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.Type: GrantFiled: December 9, 2013Date of Patent: September 20, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Jared N. Cumming, Jack D. Scott, Tesfaye Biftu
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Patent number: 9447086Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.Type: GrantFiled: September 10, 2013Date of Patent: September 20, 2016Assignee: Hoffmann-LA Roche INC.Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Xianfeng Lin, Haixia Liu, Alexander V Mayweg, Zongxing Qiu, Hong Shen, Guozhi Tang, Lisha Wang, Guolong Wu, Shixiang Yan, Weixing Zhang, Mingwei Zhou, Wei Zhu
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Patent number: 9447087Abstract: Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I).Type: GrantFiled: September 23, 2011Date of Patent: September 20, 2016Assignee: UNIVERSITY OF UTAH RESEARCH FOUNDATIONInventors: Matthew B. Boxer, Martin J. Walsh, Li Liu, Cordelle D. Tanega, Min Shen, Kent Lai, Manshu Tang, Douglas S. Auld
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Patent number: 9447088Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.Type: GrantFiled: March 17, 2014Date of Patent: September 20, 2016Assignee: ArQule, Inc.Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
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Patent number: 9447089Abstract: Provided are solid dispersions, solid molecular complexes, salts and crystalline polymorphs involving propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide.Type: GrantFiled: March 31, 2010Date of Patent: September 20, 2016Assignees: Plexxikon Inc., Hoffman-La Roche Inc.Inventors: Dipen Desai, Ralph Diodone, Zenaida Go, Prabha N. Ibrahim, Raman Iyer, Hans-Juergen Mair, Harpreet K. Sandhu, Navnit H. Shah, Gary Visor, Nicole Wyttenbach, Stephan Lauper, Johannes Pudewell, Frank Wierschem
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Patent number: 9447090Abstract: An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.Type: GrantFiled: November 26, 2013Date of Patent: September 20, 2016Assignee: Astellas Pharma Inc.Inventors: Yuji Koga, Kyoichi Maeno, Ippei Sato, Yoshimasa Imamura, Takeshi Hanazawa, Maiko Iida, Kazuhiko Ohne, Kenichiro Imamura, Tsubasa Watanabe, Eisuke Nozawa, Hiroshi Shibata
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Patent number: 9447091Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.Type: GrantFiled: October 9, 2012Date of Patent: September 20, 2016Assignee: ORION CORPORATIONInventors: Tero Linnanen, Gerd Wohlfahrt, Srinivas Nanduri, Ravi Ujjinamatada, Srinivasan Rajagopalan, Subhendu Mukherjee
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Patent number: 9447092Abstract: The present invention relates to compounds of formula I: wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The compounds of formula I are inhibitors of aurora kinase and/or FLT3. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which aurora kinase and/or FLT3 activity is implicated.Type: GrantFiled: June 21, 2013Date of Patent: September 20, 2016Assignee: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Julian Blagg, Vassilios Bavetsias, Andrew S. Moore, Spyridon Linardopoulos
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Patent number: 9447093Abstract: The present invention discloses compositions of novel DYRK1A protein inhibitors based on a 3,5-diarylazaindole motif and their preparation and use as medications in the treatment of cognitive disorders associated with dysfunction of DYRK1A protein, with Down's syndrome and with Alzheimer's disease.Type: GrantFiled: December 18, 2013Date of Patent: September 20, 2016Assignees: Centre National De La Recherche Scientifique (CNRS), Universite de Reims Champagne-Ardenne, Universite Paris Diderot Paris 7Inventors: Robert Dobb, Kevin Cariou, Stephanie Gourdain, Jean Maurice Delabar, Nathalie Janel, Fernando Rodrigues Lima, Julien Dairou, Clement Denhez
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Patent number: 9447094Abstract: The present invention relates to the preparation of stable pyridone disulphide derivatives having general formula (I) and its stereoisomers, which are useful in the treatment of gastrointestinal disorders. Pyridone disulphide derivatives (I) wherein, R1, R2 and R3 are independently alkyl, alkoxy, halogen, halogenated alkoxy, halogenated alkyl, hydrogen and could be the same or different and X is CH or N. R1 is methyl, methoxy, fluorine, trifluoromethyl, difluoromethoxy and hydrogen, R2 is methyl, methoxy and hydrogen, and R3 is methyl and hydrogen.Type: GrantFiled: May 4, 2015Date of Patent: September 20, 2016Assignee: Emcure Pharmaceuticals LimitedInventors: Mukund Keshav Gurjar, Narendra Kumar Tripathy, Golakchandra Sudarshan Maikap, Rajendra Dagesing Mahale, Tushar Pandurang Khaladkar, Ashok Tukaram Chaudhari, Sanjay Shankar Pawar, Vijay Keshav Kalhapure, Samit Satish Mehta
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Patent number: 9447095Abstract: The present invention relates to novel pyrimidine derivatives of formula (I) as inhibitors of the enzyme phosphodiesterase 10 (PDE-10), pharmaceutical compositions comprising an effective amount of these compounds and the use of the compounds for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by inhibition of the enzyme Phosphodiesterase 10 such as neurological, psychiatric, respiratory or metabolic diseases.Type: GrantFiled: January 24, 2014Date of Patent: September 20, 2016Assignee: PALOBIOFARMA S.L.Inventors: Juan Camacho Gómez, Julio Castro Palomino Laria
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Patent number: 9447096Abstract: The present invention relates to novel crystal forms of 2-amino-N-[2-(3a-(R)-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1-(R)-benzyloxymethyl-2-oxo-ethyl]-isobutyramide L-tartrate. More particularly, the invention relates to polymorph forms, and to processes for the preparation of compositions containing and to uses of such polymorph forms.Type: GrantFiled: May 28, 2014Date of Patent: September 20, 2016Assignee: RaQualia Pharma Inc.Inventors: Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi, Toyoharu Numata
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Patent number: 9447097Abstract: This invention relates to novel 4-amino-imidazoquinoline compounds of the formula wherein R1 to R4 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer or infectious diseases.Type: GrantFiled: April 7, 2016Date of Patent: September 20, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Hoves, Bernd Kuhn, Fabienne Ricklin, Stephan Roever
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Patent number: 9447098Abstract: The invention relates to new pteridine derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g.Type: GrantFiled: May 30, 2013Date of Patent: September 20, 2016Assignee: ASTEX THERAPEUTICS LTDInventors: Gordon Saxty, Christopher Charles Frederick Hamlett, Valerio Berdini, Christopher William Murray, Patrick René Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
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Patent number: 9447099Abstract: The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities.Type: GrantFiled: September 27, 2012Date of Patent: September 20, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Stephan Bachmann, Daniel Bailey, Jodie Brice, Miall Cedilote, Zhiming Dong, Stefan Hildbrand, Doreen Miller, Paul Spurr, Amit Srivastava, Juergen Wichmann, Thomas Woltering, Jason Yang, Pingsheng Zhang
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Patent number: 9447100Abstract: There is provided a calcium receptor modulator comprising a compound of the formula (I): wherein ring A is an optionally substituted 5- to 7-membered ring; ring B is an optionally substituted 5- to 7-membered heterocyclic ring; X1 is CR1, CR1R2, N or NR13; X2 is N or NR3; Y is C, CR4 or N, Z is CR5, CR5R6, N or NR7; Ar is an optionally substituted cyclic group; R is H, an optionally substituted hydrocarbon group, etc.; and is a single bond or a double bond; R1, R2, R3, R4, R5, R6, R7 and R13 are independently H, an optionally substituted hydrocarbon group; or a salt thereof or a prodrug thereof. Compounds of the formula (II) and (III): wherein ring A is an optionally substituted 5- to 7-membered ring; Q is C, CR5 or N; R8, R9, R10, R11 and R12 are independently, H, an optionally substituted hydrocarbon group, etc., or a salt thereof are also provided. Also specify X1, R3, R1, Y and X3 in formula (II) and (III) as before.Type: GrantFiled: November 25, 2013Date of Patent: September 20, 2016Assignee: Takeda Pharmaceutical Company, Ltd.Inventors: Tsuneo Yasuma, Akira Mori, Masahiro Kawase, Hiroyuki Kimura, Masato Yoshida, Albert Charles Gyorkos, Scott Alan Pratt, Christopher Peter Corrette
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Patent number: 9447101Abstract: The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.Type: GrantFiled: April 23, 2013Date of Patent: September 20, 2016Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Haihe Pharmaceutical Co., Ltd.Inventors: Chunhao Yang, Linghua Meng, Yanhong Chen, Xiang Wang, Cun Tan, Jiapeng Li, Jian Ding, Yi Chen
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Patent number: 9447102Abstract: The present invention relates to a novel family of inhibitors of protein kinase of formula 1 and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src and Btk protein kinase families.Type: GrantFiled: July 3, 2013Date of Patent: September 20, 2016Assignee: PHARMASCIENCE, INC.Inventors: Alain Laurent, Yannick Rose
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Patent number: 9447103Abstract: Inauhzin (INZ) was identified as a novel p53 activator, which selectively and efficiently suppressing tumor growth without displaying genotoxicity and with little toxicity to normal cells. A panel of INZ analogs were synthesized and evaluated their ability to induce cellular p53 and to inhibit cell growth in cell-based assays. As described, this leads to the discovery of INZ analog 37, a molecule that exhibits much better potency than INZ in both of p53 activation and cell growth inhibition in several human cancer cell lines including H460 and HCT116+/+ cells. This INZ analog exhibited a much lower effect on p53-null H1299 cells and importantly no toxicity towards normal human p53-containing WI-38 cells. Those results also reveal key chemical features for INZ activity, and identify the newly synthesized INZ analog 37 as a better small molecule for further development of anti-cancer therapies.Type: GrantFiled: July 27, 2013Date of Patent: September 20, 2016Assignee: Indiana University Research & Technology CorporationInventors: Hau Lu, Shelya Zeng, Qi Zhang, Qizhuang Ye, Derong Ding
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Patent number: 9447104Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: GrantFiled: September 18, 2014Date of Patent: September 20, 2016Assignee: Array BioPharma, Inc.Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Patent number: 9447105Abstract: The present invention discloses triazine compounds of Formula II and a process to synthesize these compounds. Particularly, the invention provides one pot method to synthesize triazines nucleus, wherein the method comprises amination followed by using Leuckart reaction conditions of pyrrole/indole-2-carboxylates of Formula I to obtain corresponding triazine compounds of Formula II.Type: GrantFiled: January 24, 2014Date of Patent: September 20, 2016Assignee: Council of Scientific & Industrial ResearchInventors: Pradeep Kumar, Anand Harbindu, Brijesh Sharma
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Patent number: 9447106Abstract: The invention is substituted 4,5-dihydro- and 4,5,6,7-tetrahydro-pyrazolo[1,5-?]pyrimidine compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor, such as inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.Type: GrantFiled: May 27, 2015Date of Patent: September 20, 2016Assignee: BeiGene, Ltd.Inventors: Zhiwei Wang, Yunhang Guo
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Patent number: 9447107Abstract: The present disclosure relates to multichromophoric assemblies comprising metalloporphyrin scaffolds. The present disclosure also relates, in part, to methods for generating electric-field-stabilized geminate polaron pairs comprising applying electric fields to the multichromophoric assemblies described herein, or alternatively, directly to the metalloporphyrins provided by the present disclosure. The present disclosure further relates, in part, to multichromophoric assemblies comprising metalloporphyrin scaffolds, which exhibit enhanced energy transfer properties.Type: GrantFiled: September 9, 2011Date of Patent: September 20, 2016Assignee: University of Southern CaliforniaInventors: Mark E. Thompson, Matthew T. Whited, Peter I. Djurovich
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Patent number: 9447108Abstract: The invention relates to new morphine derivatives deuterated at the 7,8-position of the morphine ring, furthermore to a process for the preparation thereof, and to pharmaceutical compositions comprising them. The new deuterated morphine derivatives show high and selective ?-opioid receptor binding activity leading to the benefit of higher analgesic activity at lower dosages inducing thereby reduced adverse effects compared to the hydrogenated derivatives. The compounds of the invention are useful for example in the treatment of pain or can be used as antitussive agents with a reduced risk of the possibility of drug abuse.Type: GrantFiled: April 14, 2014Date of Patent: September 20, 2016Assignee: Szegedi TudományegyetemInventors: Ferenc Fülöp, István Mándity
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Patent number: 9447109Abstract: Disclosed is asenapine phosphate of formula (I) and its enantiomer (I) which can be used to prepare asenapine maleate. Further disclosed is a monoclinic crystalline form of asenapine maleate.Type: GrantFiled: April 30, 2012Date of Patent: September 20, 2016Assignee: OLON S.P.A.Inventors: Samuele Frigoli, Davide Longoni, Tamara Danelli, Marco Alpegiani