Polycylo Ring System Having A Ring Nitrogen In The System Patents (Class 514/80)
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Patent number: 10730833Abstract: Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.Type: GrantFiled: April 5, 2018Date of Patent: August 4, 2020Assignee: Wisconsin Alumni Research FoundationInventors: Weiping Tang, Xiaoxun Li, Dongxu Shu, Gabrielle N. Winston-McPherson
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Patent number: 10729706Abstract: One or more cannabinoids and/or terpenes in combination with psilocybin and/or psilocin may be used in the prevention or treatment of psychological or brain disorders. The one or more cannabinoids may be taken from the group of cannabidiol (CBD); cannabidiolic acid (CBDA); tetrahydrocannbidivarin (THCV); tetrahydrocannbidivarinin acid (THCVA); cannabichromene (CBC); cannabichromenic acid (CBCA); cannabigerol (CBG) and cannabigerolic acid (CBGA).Type: GrantFiled: January 18, 2018Date of Patent: August 4, 2020Assignee: Procare Beheer B.V.Inventors: Murat Küçüksen, Ali Neset Küçüksen
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Patent number: 10550128Abstract: A hydrogenated Diels-Alder adduct of the formula (III) a hydrogenated Diels-Alder adduct of the formula (IV) and a lactone compound of formula (V) are disclosed and described.Type: GrantFiled: March 4, 2019Date of Patent: February 4, 2020Assignees: Avantium Knowledge Centre B.V., Stichting Wageningen ResearchInventors: Jan Cornelis Van Der Waal, Edserd De Jong, Jacco Van Haveren, Shanmugam Thiyagarajan
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Patent number: 10517883Abstract: A method of treating an acute myocardial infarction by administering to an individual an effective amount of a formulation which inhibits and/or depletes phagocytic cells with high specificity, thereby suppressing the inflammatory response that occurs during and following acute myocardial infarction. The formulation comprises an agent which is an intra-cellular inhibitor that is released within the targeted phagocytic cells, specifically macrophage/monocytes, and inhibits and/or destroys the macrophages and/or monocytes, thereby reducing the final zone of infarct and improving cardiac repair and myocardial remodeling. Since macrophages and monocytes possess the unique ability to phagocytose large bodies, the agent is formulated into a specific size such that it can enter cells primarily via phagocytosis. Thus, the specifically sized formulation selectively targets monocytes/macrophages.Type: GrantFiled: June 27, 2003Date of Patent: December 31, 2019Assignee: ZULI HOLDINGS LTD.Inventors: Haim D. Danenberg, Gershon Golomb, Elazer R. Edelman
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Patent number: 10512751Abstract: Methods of modifying the luminal profile of a body vessel are described. An example method comprises advancing a cannula out of the distal end of a catheter disposed within the lumen of a body vessel of an animal and toward a target site on the wall of the body vessel; passing contrast dye through the cannula toward the target site; simultaneously continuing the advancing and passing until the distal end of the cannula punctures the inner layer of the wall of the body vessel at the target site; and passing a bulking agent through the cannula and into a space between connective tissue layers surrounding the vessel wall at the target site. Medical devices, medical device assemblies, and kits are also described.Type: GrantFiled: November 21, 2018Date of Patent: December 24, 2019Assignee: Cook Medical Technologies LLCInventors: John C. Sigmon, Jr., Vihar Surti
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Patent number: 10478494Abstract: Provided herein are combination therapies for the treatment of cancer. In particular, the disclosed methods are directed to treatment of cancer in a patient comprising administering an antibody that blocks the interaction between PD-1 and PD-L1 and an FGFR inhibitor, wherein the antibody that blocks the interaction between PD-1 and PD-L1 and the FGFR inhibitor are administered if one or more FGFR variants are present in a biological sample from the patient.Type: GrantFiled: March 24, 2016Date of Patent: November 19, 2019Assignee: ASTEX THERAPEUTICS LTDInventors: Jayaprakash Karkera, Suso Jesus Platero, Raluca Verona, Matthew V. Lorenzi
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Patent number: 10239869Abstract: The present invention relates to sulfonamide compounds Formula (I) wherein the substituents are as described herein, and their use in a medicine for the treatment of diseases, disorders associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. It further relates to the compounds herein and their pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof useful in treating diseases, disorders, syndromes and/or conditions associated with the inhibition of Voltage-gated sodium channels (VGSC) particularly NaV1.7. The invention also relates to process for the preparation of the compounds of the invention.Type: GrantFiled: September 3, 2016Date of Patent: March 26, 2019Assignee: LUPIN LIMITEDInventors: Vidya Ramdas, Rajeshkumar Maganlal Loriya, Moloy Banerjee, Pradeep Rangrao Patil, Advait Arun Joshi, Laxmikant Shamlal Datrange, Deepak Sahebrao Walke, Talha Hussain Khan, Amit Kumar Das, Ganesh Navinchandra Gote, Vaibhav Madhukar Kalhapure, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 10189802Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.Type: GrantFiled: January 27, 2017Date of Patent: January 29, 2019Assignee: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
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Patent number: 10173027Abstract: Methods of modifying the luminal profile of a body vessel are described. An example method comprises advancing a cannula out of the distal end of a catheter disposed within the lumen of a body vessel of an animal and toward a target site on the wall of the body vessel; passing contrast dye through the cannula toward the target site; simultaneously continuing the advancing and passing until the distal end of the cannula punctures the inner layer of the wall of the body vessel at the target site; and passing a bulking agent through the cannula and into a space between connective tissue layers surrounding the vessel wall at the target site. Medical devices, medical device assemblies, and kits are also described.Type: GrantFiled: October 7, 2016Date of Patent: January 8, 2019Assignee: Cook Medical Technologies LLCInventors: John C. Sigmon, Jr., Vihar Surti
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Patent number: 10155749Abstract: The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z? have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).Type: GrantFiled: January 7, 2016Date of Patent: December 18, 2018Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Dieter Hamprecht, Joerg Kley
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Patent number: 10138213Abstract: Provided, in part, is a composition comprising one or more chemical entities of formula I, each of which is a compound of formula I: a pharmaceutically acceptable salt thereof, a solvate thereof, or a solvate of a pharmaceutically acceptable salt thereof, the composition characterized in that greater than a first threshold amount of the total amount of chemical entities of formula I in the composition: are chemical entities of formula I.a, wherein the first threshold amount is 50%; or are chemical entities of formula I.b.1, wherein the first threshold amount is 25%; or are chemical entities of formula I.b.2, wherein the first threshold amount is 25%, wherein the chemical entities of formula I.a, I.b.1, and I.b.2, are described herein, and methods of using such compositions, for example, for the delivery of a polynucleotide in vivo.Type: GrantFiled: June 24, 2015Date of Patent: November 27, 2018Assignee: Translate Bio, Inc.Inventors: Frank DeRosa, Shrirang Karve, Michael Heartlein
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Patent number: 10131679Abstract: Provided is a compound represented by formula (I) or a pharmacologically acceptable salt thereof: wherein L1 is an optionally substituted C1-6 alkylene group or the like, L2 is a single bond or the like, L3 is a single bond or the like, R1, R2, and R3 are each independently an optionally substituted C1-4 alkyl group or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like.Type: GrantFiled: October 30, 2015Date of Patent: November 20, 2018Assignee: UBE INDUSTRIES, LTD.Inventors: Yasuhiro Aga, Shigeru Ushiyama, Noriaki Iwase, Shigeyuki Kono, Hidetoshi Sunamoto, Takashi Matsushita, Sayaka Ogi, Masayuki Tanaka, Masaaki Matoyama, Satoshi Umezaki, Yusuke Shiraishi, Kazuhiro Onuma, Masahiro Kojima, Hayato Nishiyama, Tomio Kimura
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Patent number: 9993492Abstract: The present invention refers to a compound selected from the group consisting of a lysophospholipid and a lysophospholipid analog for use in the treatment or prophylaxis of honeybee brood diseases, in particular American foulbrood and European foulbrood. The invention also refers to a diet composition, a sprayable composition, a dipping solution for brood combs, a beeswax composition and liposomal and microsphere- or nanosphere-based compositions, comprising a compound according to the invention, for use in the treatment or prophylaxis of bee brood diseases.Type: GrantFiled: May 22, 2014Date of Patent: June 12, 2018Assignee: University of GrazInventors: Wolfgang Schühly, Ulrike Riessberger-Gallé, Javier Hernández-López, Karl Crailsheim
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Patent number: 9987237Abstract: The present invention provides for a method of treating a disease such as cancer, comprising the step of administering to a patient a therapeutically effective amount of an isomer or analog of monoterpene or sesquiterpene (or its derivative), such as an isoperillyl alcohol. The present invention also provides for a method of treating a disease comprising the step of administering to a patient a therapeutically effective amount of a derivative of an isomer or analog of monoterpene or sesquiterpene, such as an isoperillyl alcohol carbamate. The derivative may be an isoperillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The route of administration may vary, including inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.Type: GrantFiled: August 24, 2015Date of Patent: June 5, 2018Assignee: NeOnc Technologies, Inc.Inventors: Thomas Chen, Daniel Levin, Satish Pupalli, Daniel Anthony Dickman
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Patent number: 9981954Abstract: The present invention relates to compounds of formula (I) or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z? have one of the meanings as defined in the specification, to the use of compounds of formula (I) as medicaments, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I). The compounds are ENaC inhibitors useful for the treatment of respiratory diseases and allergic diseases of the airways.Type: GrantFiled: January 7, 2016Date of Patent: May 29, 2018Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Sara Frattini, Joerg Kley
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Patent number: 9867825Abstract: A combination of a CDK4/6 inhibitor and a MEK inhibitor for the treatment of diseases such as cancer.Type: GrantFiled: December 16, 2013Date of Patent: January 16, 2018Assignee: Novartis AGInventors: Giordano Caponigro, Scott Delach, Shivang Doshi, Thomas Horn-Spirohn, Sunkyu Kim
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Patent number: 9809609Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.Type: GrantFiled: May 1, 2012Date of Patent: November 7, 2017Assignee: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
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Patent number: 9777018Abstract: The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them.Type: GrantFiled: August 21, 2015Date of Patent: October 3, 2017Assignee: RHIZEN PHARMACEUTICALS SAInventors: Dhanapalan Nagarathnam, Swaroop K. Vakkalanka, Srikant Viswanadha, Gayatri S. Merikapudi
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Patent number: 9730904Abstract: A pharmaceutical composition which is different from an existing therapeutic agent of an adult disease, of a biochemical reaction-inhibiting type, and which action mechanism is to improve the basal metabolism, wherein the composition has no side effects, and does not generate drug resistance against adult disease; and a method for preventing/treating an adult disease by using the same.Type: GrantFiled: May 8, 2015Date of Patent: August 15, 2017Assignee: SBI Pharmaceuticals Co., Ltd.Inventor: Tohru Tanaka
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Patent number: 9732035Abstract: Presently provided are indoximod prodrug and salt compounds and pharmaceutical compositions comprising salts and prodrugs of indoximod, that produce enhanced plasma concentration and exposure to indoximod compared to direct administration of indoximod, in patients in need of treatment of immunosuppression mediated by the indoleamine-2,3-dioxygenase pathway, such as patients with cancer or chronic infectious diseases.Type: GrantFiled: June 2, 2016Date of Patent: August 15, 2017Assignee: NEWLINK GENETICS CORPORATIONInventors: Mario Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Hima Potturi, Hong Zhuang
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Patent number: 9556110Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.Type: GrantFiled: January 16, 2015Date of Patent: January 31, 2017Assignee: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
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Patent number: 9481698Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of this process.Type: GrantFiled: September 27, 2013Date of Patent: November 1, 2016Assignee: Sandoz AGInventors: Hubert Sturm, Josef Wieser
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Patent number: 9452197Abstract: In certain aspects, the present disclosure relates to the insight that a polypeptide comprising a ligand-binding portion of the extracellular domain of activin-like kinase I (ALK1) polypeptide may be used to inhibit angiogenesis in vivo, particularly in mammals suffering angiogenesis-related disorders. In certain aspects, the disclosure demonstrates that antagonists of BMP9 and/or BMP10, ligands for ALK1, may also be used to inhibit angiogenesis in vivo.Type: GrantFiled: December 27, 2013Date of Patent: September 27, 2016Assignee: Acceleron Pharma, Inc.Inventors: Jasbir Seehra, John Knopf, Robert S. Pearsall, Asya Grinberg, Ravindra Kumar
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Patent number: 9339029Abstract: The present disclosure is directed to hydrazinyl lipidoids, formulations thereof further comprising at least one active agent, as well as methods of delivering the at least one active agent to a target organism.Type: GrantFiled: September 3, 2015Date of Patent: May 17, 2016Assignee: Preceres Inc.Inventors: Richard Wayne Heidebrecht, Jr., Cheng Zhong
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Patent number: 9303052Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.Type: GrantFiled: August 12, 2013Date of Patent: April 5, 2016Assignee: I. OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
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Patent number: 9238627Abstract: The present invention relates to processes for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, processes for preparing crystallized 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, and intermediates useful therefore. Also provided herein are pharmaceutical compositions comprising this crystallized compound.Type: GrantFiled: October 18, 2013Date of Patent: January 19, 2016Assignees: Array BioPharma, Inc., Novartis AGInventors: Christoph Max Krell, Marian Misun, Daniel Andreas Niederer, Werner Heinz Pachinger, Marie-Christine Wolf, Daniel Zimmermann, Weidong Liu, Peter J. Stengel, Paul Nichols
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Patent number: 9181286Abstract: The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders.Type: GrantFiled: January 16, 2014Date of Patent: November 10, 2015Assignee: Retrophin, Inc.Inventors: Andrew Vaino, Marek Biestek, Martin Shkreli
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Patent number: 9095165Abstract: It is to provide a pharmaceutical composition which is different from an existing therapeutic agent of an adult disease, of a biochemical reaction-inhibiting type, and which action mechanism is to improve the basal metabolism, wherein the composition has no side effects, and does not generate drug resistance against adult disease; and a method for preventing/treating an adult disease by using the same.Type: GrantFiled: October 27, 2009Date of Patent: August 4, 2015Assignee: SBI Pharmaceuticals Co., Ltd.Inventor: Tohru Tanaka
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Patent number: 9062053Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.Type: GrantFiled: August 7, 2014Date of Patent: June 23, 2015Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
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Patent number: 9051317Abstract: Azaindoles having inhibitory activity on RSV replication and having the formula I compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: June 9, 2015Assignee: JANSSEN SCIENCES IRELAND UCInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Publication number: 20150148311Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.Type: ApplicationFiled: June 20, 2014Publication date: May 28, 2015Inventors: Jason G. Lewis, Nicholas Reich, Tao Chen, Jeffrey W. Jacobs, Dominique Charmot, Marc Navre, Patricia Finn, Christopher Carreras, Andrew Spencer
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Publication number: 20150148312Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: January 23, 2015Publication date: May 28, 2015Inventors: Herriot Tabuteau, Graeme Jones
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Publication number: 20150141374Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: January 28, 2015Publication date: May 21, 2015Inventors: Herriot Tabuteau, Graeme Jones
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Publication number: 20150141373Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: January 28, 2015Publication date: May 21, 2015Inventors: Herriot Tabuteau, Graeme Jones
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Publication number: 20150133403Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: January 26, 2015Publication date: May 14, 2015Inventors: Herriot Tabuteau, Graeme Jones
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Publication number: 20150126477Abstract: Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;Type: ApplicationFiled: February 24, 2012Publication date: May 7, 2015Inventors: Jayant Thatte, Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Jae-Kyu Jung, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter, Sonja Strah-Pleynet, Lars Thoresen, Yifeng Xiong, Dawei Yue, Xiuwen Zhu
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Patent number: 9018191Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.Type: GrantFiled: August 21, 2012Date of Patent: April 28, 2015Assignee: AstraZeneca ABInventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri Jung, Georges Rene Pasquet
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Publication number: 20150111853Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.Type: ApplicationFiled: October 22, 2014Publication date: April 23, 2015Inventors: Jan-Ji Lai, Pradip M. Pathare, Laxma Kolla, Adrien F. Soret
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Publication number: 20150111854Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: December 5, 2014Publication date: April 23, 2015Inventors: Chika TAKAHASHI, Hindenori MIKAMIYAMA, Toshiyuki AKIYAMA, Kenji TOMITA, Yoshiyuki TAODA, Makoto KAWAI, Kosuke ANAN, Masayoshi MIYAGAWA, Naoyuki SUZUKI
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Patent number: 9006387Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: February 14, 2014Date of Patent: April 14, 2015Assignee: AbbVie Inc.Inventors: Rolf Wagner, John K. Pratt, Dachun Liu, Michael D. Tufano, David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, Yi Gao, Allan C. Krueger
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Publication number: 20150099721Abstract: A method for treating cancer with a mutation in ROS or RET, comprising identifying a subject with a cancer with a mutation in ROS or RET, and administering to the subject an effective amount of a compound according to formulae (I) OR (la) or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables structural formulae are defined herein.Type: ApplicationFiled: May 10, 2013Publication date: April 9, 2015Applicant: Synta Pharmaceuticals Corp.Inventors: Jaime Acquaviva, Suqin He, David Proia
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Patent number: 8993542Abstract: The present invention provides methods of treating human immunodeficiency virus (HIV) and/or hepatitis B virus (HBV) infection, including administering a compound described in the invention in an amount effective treat the HIV and/or HBV infection and at least substantially inhibit the development of resistance to said antiviral compounds in the subject. Pharmaceutical compositions are also provided.Type: GrantFiled: January 23, 2009Date of Patent: March 31, 2015Assignee: Chimerix Inc.Inventors: Ernest Randall Lanier, Merrick R. Almond, George R. Painter
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Publication number: 20150072957Abstract: This disclosure provides compositions containing solid forms of tazobactam arginine, and methods of manufacturing and using these compositions.Type: ApplicationFiled: November 14, 2014Publication date: March 12, 2015Applicant: Calixa Therapeutics, Inc.Inventors: Jan-Ji Lai, Jian-Qiao Gu, Pradip M. Pathare, Valdas Jurkauskas, Joseph Terracciano, Nicole Miller Damour
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Publication number: 20150065463Abstract: Benzothiazole phosphonate analogs and methods of using the same to inhibit the activity of Amyloid Binding Alcohol Dehydrogenase and in the amelioration or treatment of Alzheimer's disease are provided.Type: ApplicationFiled: November 12, 2014Publication date: March 5, 2015Applicant: University of KansasInventors: ShiDu Yan, Koteswara Rao Valasani
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Patent number: 8969359Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.Type: GrantFiled: June 3, 2013Date of Patent: March 3, 2015Assignee: Vertex Pharmaceuticals IncorporatedInventors: Arnaud Le Tiran, Anne-Laure Grillot, Paul S. Charifson, Youssef Laafiret Bennani, Hardwin O'Dowd, Emanuele Perola
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Publication number: 20150057250Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.Type: ApplicationFiled: November 7, 2014Publication date: February 26, 2015Inventor: Herriot Tabuteau
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Patent number: 8956648Abstract: The present invention provides pharmaceutical photosensitizer-loaded nanoparticle formulations and their methods of preparation for photodynamic therapy, comprising a hydrophobic or hydrophilic photosensitizer, nanoparticulate calcium phosphate and in certain cases auxiliary reagents such as stabilizers. The calcium phosphate-based nanoparticle formulations of the present invention provide excellent storage stability and therapeutically effective amounts of photosensitizer for intravenous or topical administration. In a preferred embodiment, tetrapyrrole derivatives such as porphyrins, chlorins and bacteriochlorins, are the preferred hydrophobic photosensitizers to be formulated in calcium phosphate nanoparticle formulations for photodynamic tumor therapy. Additionally, 5,10,15,20-tetrakis(4-phosphonooxyphenyl)porphine (pTPPP) is a preferred hydrophilic photosensitizer for photodynamic tumor therapy.Type: GrantFiled: December 18, 2009Date of Patent: February 17, 2015Assignee: Biolitec PharmaMarketing LtdInventors: Burkhard Gitter, Susanna Gräfe, Arno Wiehe, Volker Albrecht, Matthias Epple, Janine Schwiertz, Kathirvel Ganesan
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Patent number: 8957050Abstract: The present invention is directed to a stabilized cross-linked hydrogel matrix comprising a first high molecular weight component and a second high molecular weight component that are covalently linked, and at least one stabilizing or enhancing agent, wherein the first high molecular weight component and the second high molecular weight component are each selected from the group consisting of polyglycans and polypeptides. This stabilized hydrogel matrix may be prepared as bioactive gels, pastes, slurries, cell attachment scaffolds for implantable medical devices, and casting or binding materials suitable for the construction of medical devices. The intrinsic bioactivity of the hydrogel matrix makes it useful as a gel or paste in multiple applications, including as a cell attachment scaffold that promotes wound healing around an implanted device, as gels and pastes for induction of localized vasculogenesis, wound healing, tissue repair, and regeneration, as a wound adhesive, and for tissue bulking.Type: GrantFiled: March 11, 2013Date of Patent: February 17, 2015Assignee: Pioneer Surgical Technology, Inc.Inventors: Francis Vincent Lamberti, Richard Chris Klann, Ronald Stewart Hill
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Publication number: 20150045323Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.Type: ApplicationFiled: September 13, 2013Publication date: February 12, 2015Inventors: Linda N. Casillas, Pamela A. Haile, Robert W. Marquis, JR., Gren Wang
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Patent number: 8940716Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: GrantFiled: May 4, 2011Date of Patent: January 27, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang