Polycyclo Ring System Having The Additional Oxygen Hetero Ring As One Of The Cyclos Patents (Class 514/254.11)
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Patent number: 11865146Abstract: This document provides biomarkers of gut microbiota dysbiosis. Bacteria that are increased or decreased in gut microbiota dysbiosis can be used as biomarkers to predict dysbiosis in patients with diarrhea and/or to predict susceptibility to Clostridium difficile infection (CDI). In addition, provided herein are compositions including at least three bacteria that are decreased in gut microbiota dysbiosis which can be used, for example, to restore heathy gut microbiota (e.g., by probiotic or by fecal microbiota transplant) to treat CDI.Type: GrantFiled: November 9, 2020Date of Patent: January 9, 2024Assignee: Mayo Foundation for Medical Education and ResearchInventors: Purna C. Kashyap, Eric J. Battaglioli, Vanessa L. Hale
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Patent number: 11337971Abstract: Disclosed herein are novel methods of treating pain in a patient in need thereof by providing to the patient a selective dopamine D3 receptor antagonist/partial agonist which when used with an opioid analgesic, can mitigate the development of opioid dependence, by preventing the need for dose escalation while either maintaining the opioid analgesic effect or providing analgesia with a lower dose of the opioid. In addition, the D3 antagonists/partial agonists described herein may be used to augment the effectiveness of current Medication Assisted Treatment regimens (e.g. methadone or buprenorphine) for the treatment of opioid use disorders.Type: GrantFiled: September 9, 2019Date of Patent: May 24, 2022Assignee: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Amy Hauck Newman, Vivek Kumar, Anver Basha Shaik
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Patent number: 11136339Abstract: Disclosed are a dihydroartemisinin dimer derivative, a pharmaceutical composition, and an application thereof. The derivative is an artemisinin dimer used for drugs treating or preventing malaria caused by plasmodium, drugs treating autoimmune diseases such as lupus erythematosus, and anti-tumour drugs, which is a pharmaceutical composition prepared from the dihydroartemisinin dimer derivative and a pharmaceutically acceptable carrier.Type: GrantFiled: April 11, 2018Date of Patent: October 5, 2021Assignee: SOUTHEAST UNIVERSITYInventors: Xinsong Li, Ma Si, Longbing Ling
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Patent number: 10398674Abstract: An embodiment of the invention provides a cannabis-based flavonoid pharmaceutical composition including any one or more selected, from among the group of Apigenin, Cannflavin. A. Cannflavin B, Cannflavin C, Chrysoeriol, Cosmosiin, Flavocannabiside, Kaempferol, Luteolin, Myricetin, Orientin, Isoorientin (Homoorientin), Quercetin (+)-Taxifolin, Vitexin, and Isovitexin, or their synthases, for the prevention and treatment of certain cancers that can be treated by therapeutically targeting oncogenic factors including kinases, sirtuins, bromodomains, matrix metalloproteinases and BCL-2. Some of the cancers that can be treated by use of cannabis flavonoids based on the inhibition of these therapeutic targets include brain, breast, colon, renal, liver, lung, pancreatic, prostate, leukemia, melanoma as well as any other cancers that overexpress the oncogenic factors inhibited by the cannabis flavonoids identified herein.Type: GrantFiled: November 24, 2015Date of Patent: September 3, 2019Inventors: Henry Lowe, Ngeh J. Toyang
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Patent number: 10023587Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: GrantFiled: February 6, 2017Date of Patent: July 17, 2018Assignee: Lixte Biotechnology, Inc.Inventors: John S Kovach, Francis Johnson
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Patent number: 9974791Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: GrantFiled: June 25, 2015Date of Patent: May 22, 2018Assignee: GENKYOTEX SUISSE SAInventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
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Patent number: 9937192Abstract: 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: January 19, 2017Date of Patent: April 10, 2018Assignee: SPERO TRINEM, INC.Inventors: Christopher Phillip Locher, Youssef Laafiret Bennani, Anne-Laure Grillot, Hardwin O'Dowd, Emanuele Perola, Arnaud Le Tiran, Paul S. Charifson
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Patent number: 9493443Abstract: The present invention relates to an improved process for the preparation of vilazodone hydrochloride and a process for preparation of novel pure amorphous form of vilazodone hydrochloride.Type: GrantFiled: April 6, 2015Date of Patent: November 15, 2016Assignee: Alembic Pharmaceuticals LimitedInventors: Venkat Raman Jayaraman, Dhiraj Rathod, Irfan Vohra, Vinayak Bhujade, Viral Modi, Mayur Budh, Ojas Gandhi
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Patent number: 9422306Abstract: The present disclosure describes artemisinin compounds. The compounds can be synthesized using an Ugi synthesis reaction and can be used in the treatment of cancers, parasitic infections and yeast infections.Type: GrantFiled: December 19, 2013Date of Patent: August 23, 2016Assignee: UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATIONInventors: Tomikazu Sasaki, Shusheng Wang
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Patent number: 9359374Abstract: Provided for in the instant application are two additional forms of rifaximin, namely rifaximin polymorphic forms APO-III and APO-IV. Also provided are allegedly novel processes for preparing the previously disclosed rifaximin polymorphic forms APO-I and APO-II. Rifaximin is a non-aminoglycoside antibiotic that has previously been found to be useful for the treatment of traveller's diarrhea caused by Escherichia coli bacteria, as well as in the treatment of irritable bowel syndrome, diverticular disease, hepatic encephalopathy, pyogenic skin infections and as an antibacterial prophylactic prior to colon surgery.Type: GrantFiled: June 13, 2013Date of Patent: June 7, 2016Assignee: Apotex Pharmachem Inc.Inventors: Peter Garth Blazecka, Nageib Mohamed, Cameron L. McPhail, Sammy Chris Duncan, Randa E. El-Haj, Yajun Zhao
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Patent number: 9271968Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.Type: GrantFiled: April 25, 2014Date of Patent: March 1, 2016Assignee: ALFA WASSERMANN S.P.A.Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Maria Barbanti, Dario Braga
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Patent number: 9187448Abstract: The present invention relates to compounds, compositions, and methods for treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more epicatechin derivatives in an amount effective to stimulate mitochondrial function in cells. The compounds, compositions, and methods described herein provide for reducing infarct size in the heart following permanent ischemia or ischemia/reperfusion event or method for delaying, attenuating or preventing adverse cardiac remodeling, and can assist in prevention of impaired mitochondria biogenesis and thus prevention of the consequences of impaired mitochondrial biogenesis in various diseases and conditions, as well as provide for the active therapy of mitochondrial depletion that may have already occurred.Type: GrantFiled: August 6, 2012Date of Patent: November 17, 2015Assignee: CARDERO THERAPEUTICS, INC.Inventors: Cyrus K. Becker, George F. Schreiner, Sundeep Dugar, Dinesh Mahajan
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Publication number: 20150147378Abstract: Biocompatible, biodegradable copolymer-xerogel nanocomposites contain a biodegradable, biocompatible copolymer, silica nanoparticles and one or more therapeutic agents, that are useful for wound dressings, medical devices and drug delivery applications.Type: ApplicationFiled: May 21, 2013Publication date: May 28, 2015Inventors: David Devore, Paul Ducheyne, Marius C. Costache
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Publication number: 20150148330Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 16, 2015Publication date: May 28, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
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Publication number: 20150148353Abstract: A method of increasing the insulin sensitivity of a mammalian cell by contacting the cell with a protein phosphatase 2A (PP2A) inhibitor having the structure:Type: ApplicationFiled: June 28, 2013Publication date: May 28, 2015Applicant: LIXTE BIOTECHNOLOGY, INC.Inventor: John S. Kovach
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Publication number: 20150140061Abstract: Stents with coatings comprising a combination of a restenosis inhibitor comprising an HMG-CoA reductase inhibitor and a carrier. Also provided are methods of coating stents with a combination of an HMG-CoA reductase inhibitor and a carrier. A preferred example of a restenosis inhibitor is cerivastatin. The stent coatings have been shown to release restenosis inhibitors in their active forms.Type: ApplicationFiled: November 12, 2014Publication date: May 21, 2015Inventor: Chandrashekhar Pathak
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Publication number: 20150133469Abstract: The present invention includes methods for early detection of a treatment response in a patient suspected of being infected with Mycobacterium tuberculosis. Changes in the blood transcriptome are detectable within two weeks of the initiation of antituberculosis therapy.Type: ApplicationFiled: March 13, 2013Publication date: May 14, 2015Inventors: Anne O'Garra, Chloe Bloom, Matthew Paul Reddoch Berry, Robert Wilkinson, Jacques F. Banchereau, Damien Chaussabel, Maria Virginia Pascual
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Publication number: 20150126515Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.Type: ApplicationFiled: January 25, 2013Publication date: May 7, 2015Applicant: PTC Therapeutics, Inc.Inventors: Guangming Chen, Amal Dakka, Gary Mitchell Karp, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Marla L. Weetall, Ellen Welch, Xin Zhao
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Publication number: 20150119380Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.Type: ApplicationFiled: December 28, 2012Publication date: April 30, 2015Inventors: Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
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Patent number: 9018213Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.Type: GrantFiled: July 31, 2012Date of Patent: April 28, 2015Assignees: Huazhong University of Science & Technology, NHWA Pharma. CorporationInventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Minquan Yu, Yinli Qiu
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Publication number: 20150110849Abstract: An antimicrobial accessory may include a pressure sensitive adhesive and an antimicrobial mixed in the pressure sensitive adhesive. In some examples, an antimicrobial accessory may include at least one first domain comprising a pressure sensitive adhesive and a first antimicrobial and at least one second domain including a second polymer and a second antimicrobial. The antimicrobial accessory may be configured to be attached to a housing of an implantable medical device (IMD).Type: ApplicationFiled: December 23, 2014Publication date: April 23, 2015Inventors: Kenneth E. COBIAN, Genevieve L. GALLAGHER, Peter M. SEILER, Kiem H. DANG, Michael S. HEMENWAY, Zhongping C. YANG, James L. SCHULD, Tico BLUMENTHAL
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Publication number: 20150111899Abstract: The present invention relates to methods involving avoiding adverse drug interactions with pirfenidone and CYP inducers, such as smoking.Type: ApplicationFiled: December 23, 2014Publication date: April 23, 2015Inventors: Williamson Z. Bradford, Javier Szwarcberg
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Publication number: 20150099731Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 meType: ApplicationFiled: May 5, 2014Publication date: April 9, 2015Applicant: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Patent number: 8999991Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.Type: GrantFiled: October 22, 2012Date of Patent: April 7, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Haifeng Tang, Barbara Pio, Harry R. Chobanian
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Patent number: 8999990Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.Type: GrantFiled: October 22, 2012Date of Patent: April 7, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
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Publication number: 20150087656Abstract: Prolongation compositions for prolonging the presence of drugs in blood.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Inventors: Aida Salatinjants, Robert Salatinjants
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Patent number: 8987304Abstract: The present invention provides antituberculous therapeutic drugs with a higher potency. The present invention provides also antituberculous therapeutic drugs containing oxazole compounds represented by (I) general formula (1): [wherein R1 represents a hydrogen atom or C1-6 alkyl group, n represents an integer of 0-6, and R2 represents general formula (A) or the like, wherein R3 represents a phenoxy group (at least one group selected from the group consisting of a halogen atom, an optionally halogen-substituted C1-6 alkyl group and an optionally halogen-substituted C1-6 alkoxy group may be substituted on the phenyl ring) or the like], optically active forms thereof or salts thereof, and drugs (II) such as primary antituberculous drugs.Type: GrantFiled: October 4, 2006Date of Patent: March 24, 2015Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Yoshihiko Shimokawa
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Publication number: 20150080383Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.Type: ApplicationFiled: March 14, 2013Publication date: March 19, 2015Inventors: Tianle Yang, Gary Mitchell Karp, Hongyan Qi
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Patent number: 8981131Abstract: The present invention provides compounds represented by formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.Type: GrantFiled: July 25, 2008Date of Patent: March 17, 2015Assignee: Piramal Enterprises LimitedInventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
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Publication number: 20150065431Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.Type: ApplicationFiled: August 27, 2014Publication date: March 5, 2015Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
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Publication number: 20150065494Abstract: The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid.Type: ApplicationFiled: April 1, 2013Publication date: March 5, 2015Inventors: Dong Jin Kim, Kyung Ho Yoo, Young Soo Kim, Woong Seo Park, Yong Koo Kang, Hye Yun Kim, Yun Kyung Kim, Ki Duk Park, Maeng Sup Kim, Kwee Hyun Suh, Young Gil Ahn
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Publication number: 20150051194Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: October 31, 2014Publication date: February 19, 2015Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. WENTLAND
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Publication number: 20150051205Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidase and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplasatic agents or glucuronidase-substrate agents or compounds.Type: ApplicationFiled: September 23, 2013Publication date: February 19, 2015Applicant: The University of North Carolina at Chapel HillInventor: Matthew R. Redinbo
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Patent number: 8957069Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is nType: GrantFiled: March 9, 2010Date of Patent: February 17, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
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Publication number: 20150045373Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: ApplicationFiled: July 10, 2014Publication date: February 12, 2015Inventors: John S. KOVACH, Francis JOHNSON
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Patent number: 8946203Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: GrantFiled: March 5, 2013Date of Patent: February 3, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Steven Richard Brunette, Michael J. Burke, Suresh R. Kapadia, Thomas Martin Kirrane, Matthew Russell Netherton, Hossein Razavi, Sonia Rodriguez, Anjan Saha, Robert Sibley, Lana Louise Smith-Keenan, Hidenori Takahashi, Michael Robert Turner, Jiang-Ping Wu, Erick Richard Roush Young, Qiang Zhang, Qing Zhang, Renee M. Zindell
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Publication number: 20150031640Abstract: It has been determined that co-administration of a rifamycin and a switch-region inhibitor 1) results in synergistic antibacterial effects, enabling efficacy at low, subtoxic doses, and/or 2) results in a low spontaneous resistance frequency, enabling treatment of high-titer infections without treatment failure due to spontaneous resistance. Accordingly, certain embodiments provide composition comprising a rifamycin and a switch region inhibitor, as well as methods of use thereof.Type: ApplicationFiled: February 5, 2013Publication date: January 29, 2015Inventor: Richard H. Ebright
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Publication number: 20150018335Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 7, 2013Publication date: January 15, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
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Publication number: 20150011566Abstract: The present invention provides N-phenylpiperazine derivatives for use as multiple binders and/or antagonists of ?1A adrenoceptors, ?1D adrenoceptors and 5-HT1A serotonin receptors. These substances are candidates to prototypes for the treatment of benign prostate hyperplasia and lower urinary tract symptoms, and are useful in pharmaceutical compositions.Type: ApplicationFiled: January 4, 2013Publication date: January 8, 2015Inventors: Claudia Lucia Martins Da Silva, Fernanda Chagas Da Silva, Luana Chaves Barberato, Luciana De Camargo Nascente, Jessica Barbosa Do Nascimento Viana, Renata Oliveira Silva, Laís Flávia Nunes Lemes, François German Noël, Luís Antônio Soares Romeiro
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Publication number: 20150011542Abstract: Methods of treating adverse intestinal effects of a non-steroidal anti-inflammatory drugs (NSAID) in a subject by administering to the subject a therapeutically effective amount of a selective bacterial beta-glucuronidase inhibitor. The adverse intestinal effects to be treated include the formation or growth of an intestinal ulcer, increased intestinal permeability, the loss of intestinal villi, bleeding of the intestinal mucosa, and an increased intestinal inflammatory response. The methods are useful for treating the adverse effects of any NSAID such as propionic acid derivatives, carboxylic acid derivatives, enolic acid derivatives, fenamic acid derivatives, sulphonanilidies, and selective COX-2 inhibitors. The bacterial beta-glucuronidase inhibitors are selective for the inhibition of bacterial beta-glucuronidase enzymes and do not inhibit mammalian beta-glucuronidase.Type: ApplicationFiled: January 11, 2013Publication date: January 8, 2015Inventor: Urs A. Boelsterli
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Patent number: 8911765Abstract: A biodegradable, flexible covering for a breast implant is provided which comprises one or more biodegradable polymer layers dimensioned and shaped to cover at least a portion of the breast implant. The implant can be inserted into an opening of the covering immediately prior to surgery, but alternate configurations and times of insertion are contemplated as well as open or sheet type devices. The coverings can optionally contain one or more drugs for delivery at the surgical site, particularly for treating or preventing infection, pain, inflammation, capsular contracture, scarring or other complications associated with breast augmentation or breast reconstruction.Type: GrantFiled: March 28, 2008Date of Patent: December 16, 2014Assignee: Tyrx, Inc.Inventors: Arikha Moses, Satish Pulapura, Qing Ge, Sarita Nethula, Irene Shatova, Archana Rajaram
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Patent number: 8912196Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.Type: GrantFiled: May 26, 2010Date of Patent: December 16, 2014Assignee: ATIR Holding S.A.Inventors: Vladimir Kogan, Lev Tabachnik
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Publication number: 20140364427Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: December 14, 2012Publication date: December 11, 2014Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Andiliy G. Lai
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Publication number: 20140356455Abstract: Methods of generating cell lines with a sequence variation or copy number variation of a gene of interest, methods of use thereof, and cell lines with a sequence variation or copy number variation of a gene of interest are provided.Type: ApplicationFiled: December 6, 2013Publication date: December 4, 2014Applicants: The Board of Trustees of the Leland Stanford Junior University, Parkinson's InstituteInventors: Renee Ann Reijo Pera, J. William Langston, Birgitt Schule, Theodore D. Palmer, Blake Byers, Ha Nam Nguyen, James Anthony Byrne, Branden John Cord
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Publication number: 20140356417Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: ApplicationFiled: June 12, 2014Publication date: December 4, 2014Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Patent number: 8901116Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: GrantFiled: September 16, 2013Date of Patent: December 2, 2014Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Byong Sung Kwak, Hong Sik Moon, Han-Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
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Publication number: 20140349991Abstract: Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root.Type: ApplicationFiled: July 17, 2014Publication date: November 27, 2014Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Katsuhiro Kawakami, Toshihiro Kiho, Atsushi Tengeiji, Kentoku Gotanda, Kazumasa Aoki, Kazuki Yano
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Patent number: 8895047Abstract: Implantable catheters are provided which comprise an antimicrobial agent incorporated in a coating or bulk distributed, in combination with a fibrinolytic agent incorporated in a top coating.Type: GrantFiled: May 21, 2008Date of Patent: November 25, 2014Assignee: Arrow International, Inc.Inventors: Nisha Gupta, Joel Rosenblatt, Daniel J. Spangler
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Publication number: 20140341999Abstract: The invention relates to the field of pharmaceutics and medicine and concerns a medicinal composition of antitubercular preparations with a phospholipid transport system, the composition consisting of a fatty acid salt, phosphatidylcholine of vegetative origin (73-97%), maltose and an antitubercular agent selected from rifamycin, protionamide, rifabutin and rifapentine, and a method for producing the composition.Type: ApplicationFiled: November 15, 2012Publication date: November 20, 2014Applicant: OBSCHESTVO S OGRANICHENNOY ONVETSTVENNOSTYU ''IBMKH-EKOBIOFARM'Inventors: Olga Mikhaylovna Ipatova, Natalya Velorikovna Medvedeva, Vladimir Nikolayevich Prozorovskiy, Maksim Aleksandrovich Sanzhakov, Yelena Georgiyevna Tikhonova, Oksana Sergeevna Druzhilovskaya
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Publication number: 20140336154Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: July 29, 2014Publication date: November 13, 2014Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg