Polycyclo Ring System Having The Additional Oxygen Hetero Ring As One Of The Cyclos Patents (Class 514/254.11)
  • Patent number: 10398674
    Abstract: 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: Grant
    Filed: November 24, 2015
    Date of Patent: September 3, 2019
    Inventors: Henry Lowe, Ngeh J. Toyang
  • Patent number: 10023587
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: July 17, 2018
    Assignee: Lixte Biotechnology, Inc.
    Inventors: John S Kovach, Francis Johnson
  • Patent number: 9974791
    Abstract: 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: Grant
    Filed: June 25, 2015
    Date of Patent: May 22, 2018
    Assignee: GENKYOTEX SUISSE SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Patent number: 9937192
    Abstract: 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: Grant
    Filed: January 19, 2017
    Date of Patent: April 10, 2018
    Assignee: SPERO TRINEM, INC.
    Inventors: Christopher Phillip Locher, Youssef Laafiret Bennani, Anne-Laure Grillot, Hardwin O'Dowd, Emanuele Perola, Arnaud Le Tiran, Paul S. Charifson
  • Patent number: 9493443
    Abstract: 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: Grant
    Filed: April 6, 2015
    Date of Patent: November 15, 2016
    Assignee: Alembic Pharmaceuticals Limited
    Inventors: Venkat Raman Jayaraman, Dhiraj Rathod, Irfan Vohra, Vinayak Bhujade, Viral Modi, Mayur Budh, Ojas Gandhi
  • Patent number: 9422306
    Abstract: 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: Grant
    Filed: December 19, 2013
    Date of Patent: August 23, 2016
    Assignee: UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION
    Inventors: Tomikazu Sasaki, Shusheng Wang
  • Patent number: 9359374
    Abstract: 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: Grant
    Filed: June 13, 2013
    Date of Patent: June 7, 2016
    Assignee: Apotex Pharmachem Inc.
    Inventors: Peter Garth Blazecka, Nageib Mohamed, Cameron L. McPhail, Sammy Chris Duncan, Randa E. El-Haj, Yajun Zhao
  • Patent number: 9271968
    Abstract: 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: Grant
    Filed: April 25, 2014
    Date of Patent: March 1, 2016
    Assignee: ALFA WASSERMANN S.P.A.
    Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Maria Barbanti, Dario Braga
  • Patent number: 9187448
    Abstract: 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: Grant
    Filed: August 6, 2012
    Date of Patent: November 17, 2015
    Assignee: CARDERO THERAPEUTICS, INC.
    Inventors: Cyrus K. Becker, George F. Schreiner, Sundeep Dugar, Dinesh Mahajan
  • Publication number: 20150148353
    Abstract: 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: Application
    Filed: June 28, 2013
    Publication date: May 28, 2015
    Applicant: LIXTE BIOTECHNOLOGY, INC.
    Inventor: John S. Kovach
  • Publication number: 20150147378
    Abstract: 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: Application
    Filed: May 21, 2013
    Publication date: May 28, 2015
    Inventors: David Devore, Paul Ducheyne, Marius C. Costache
  • Publication number: 20150148330
    Abstract: 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: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150140061
    Abstract: 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: Application
    Filed: November 12, 2014
    Publication date: May 21, 2015
    Inventor: Chandrashekhar Pathak
  • Publication number: 20150133469
    Abstract: 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: Application
    Filed: March 13, 2013
    Publication date: May 14, 2015
    Inventors: Anne O'Garra, Chloe Bloom, Matthew Paul Reddoch Berry, Robert Wilkinson, Jacques F. Banchereau, Damien Chaussabel, Maria Virginia Pascual
  • Publication number: 20150126515
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: January 25, 2013
    Publication date: May 7, 2015
    Applicant: PTC Therapeutics, Inc.
    Inventors: Guangming Chen, Amal Dakka, Gary Mitchell Karp, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Marla L. Weetall, Ellen Welch, Xin Zhao
  • Publication number: 20150119380
    Abstract: 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: Application
    Filed: December 28, 2012
    Publication date: April 30, 2015
    Inventors: 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
  • Patent number: 9018213
    Abstract: 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: Grant
    Filed: July 31, 2012
    Date of Patent: April 28, 2015
    Assignees: Huazhong University of Science & Technology, NHWA Pharma. Corporation
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Minquan Yu, Yinli Qiu
  • Publication number: 20150111899
    Abstract: The present invention relates to methods involving avoiding adverse drug interactions with pirfenidone and CYP inducers, such as smoking.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Williamson Z. Bradford, Javier Szwarcberg
  • Publication number: 20150110849
    Abstract: 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: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Kenneth E. COBIAN, Genevieve L. GALLAGHER, Peter M. SEILER, Kiem H. DANG, Michael S. HEMENWAY, Zhongping C. YANG, James L. SCHULD, Tico BLUMENTHAL
  • Publication number: 20150099731
    Abstract: 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 me
    Type: Application
    Filed: May 5, 2014
    Publication date: April 9, 2015
    Applicant: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Patent number: 8999991
    Abstract: 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: Grant
    Filed: October 22, 2012
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Harry R. Chobanian
  • Patent number: 8999990
    Abstract: 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: Grant
    Filed: October 22, 2012
    Date of Patent: April 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
  • Publication number: 20150087656
    Abstract: Prolongation compositions for prolonging the presence of drugs in blood.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Inventors: Aida Salatinjants, Robert Salatinjants
  • Patent number: 8987304
    Abstract: 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: Grant
    Filed: October 4, 2006
    Date of Patent: March 24, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Yoshihiko Shimokawa
  • Publication number: 20150080383
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 19, 2015
    Inventors: Tianle Yang, Gary Mitchell Karp, Hongyan Qi
  • Patent number: 8981131
    Abstract: 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: Grant
    Filed: July 25, 2008
    Date of Patent: March 17, 2015
    Assignee: Piramal Enterprises Limited
    Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
  • Publication number: 20150065431
    Abstract: 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: Application
    Filed: August 27, 2014
    Publication date: March 5, 2015
    Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
  • Publication number: 20150065494
    Abstract: 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: Application
    Filed: April 1, 2013
    Publication date: March 5, 2015
    Inventors: 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
  • Publication number: 20150051205
    Abstract: 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: Application
    Filed: September 23, 2013
    Publication date: February 19, 2015
    Applicant: The University of North Carolina at Chapel Hill
    Inventor: Matthew R. Redinbo
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Patent number: 8957069
    Abstract: 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 n
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
  • Publication number: 20150045373
    Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.
    Type: Application
    Filed: July 10, 2014
    Publication date: February 12, 2015
    Inventors: John S. KOVACH, Francis JOHNSON
  • Patent number: 8946203
    Abstract: 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: Grant
    Filed: March 5, 2013
    Date of Patent: February 3, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: 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
  • Publication number: 20150031640
    Abstract: 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: Application
    Filed: February 5, 2013
    Publication date: January 29, 2015
    Inventor: Richard H. Ebright
  • Publication number: 20150018335
    Abstract: 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: Application
    Filed: January 7, 2013
    Publication date: January 15, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150011566
    Abstract: 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: Application
    Filed: January 4, 2013
    Publication date: January 8, 2015
    Inventors: 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
  • Publication number: 20150011542
    Abstract: 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: Application
    Filed: January 11, 2013
    Publication date: January 8, 2015
    Inventor: Urs A. Boelsterli
  • Patent number: 8911765
    Abstract: 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: Grant
    Filed: March 28, 2008
    Date of Patent: December 16, 2014
    Assignee: Tyrx, Inc.
    Inventors: Arikha Moses, Satish Pulapura, Qing Ge, Sarita Nethula, Irene Shatova, Archana Rajaram
  • Patent number: 8912196
    Abstract: 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: Grant
    Filed: May 26, 2010
    Date of Patent: December 16, 2014
    Assignee: ATIR Holding S.A.
    Inventors: Vladimir Kogan, Lev Tabachnik
  • Publication number: 20140364427
    Abstract: 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: Application
    Filed: December 14, 2012
    Publication date: December 11, 2014
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Andiliy G. Lai
  • Publication number: 20140356455
    Abstract: 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: Application
    Filed: December 6, 2013
    Publication date: December 4, 2014
    Applicants: The Board of Trustees of the Leland Stanford Junior University, Parkinson's Institute
    Inventors: Renee Ann Reijo Pera, J. William Langston, Birgitt Schule, Theodore D. Palmer, Blake Byers, Ha Nam Nguyen, James Anthony Byrne, Branden John Cord
  • Publication number: 20140356417
    Abstract: 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: Application
    Filed: June 12, 2014
    Publication date: December 4, 2014
    Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Patent number: 8901116
    Abstract: 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: Grant
    Filed: September 16, 2013
    Date of Patent: December 2, 2014
    Assignee: 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
  • Publication number: 20140349991
    Abstract: 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: Application
    Filed: July 17, 2014
    Publication date: November 27, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Katsuhiro Kawakami, Toshihiro Kiho, Atsushi Tengeiji, Kentoku Gotanda, Kazumasa Aoki, Kazuki Yano
  • Patent number: 8895047
    Abstract: 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: Grant
    Filed: May 21, 2008
    Date of Patent: November 25, 2014
    Assignee: Arrow International, Inc.
    Inventors: Nisha Gupta, Joel Rosenblatt, Daniel J. Spangler
  • Publication number: 20140341999
    Abstract: 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: Application
    Filed: November 15, 2012
    Publication date: November 20, 2014
    Applicant: 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
  • Publication number: 20140336200
    Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Applicant: ADAMED SP. Z O.O.
    Inventors: Marcin KOŁACZKOWSKI, Piotr KOWALSKI, Jolanta Jaskowska, Monika MARCINKOWSKA, Katarzyna MITKA, Adam BUCKI, Anna WESOŁOWSKA, Maciej PAWŁOWSKI
  • Publication number: 20140336154
    Abstract: 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: Application
    Filed: July 29, 2014
    Publication date: November 13, 2014
    Inventors: 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
  • Patent number: 8883795
    Abstract: Provided for in the instant application are two additional polymorphic forms of rifaximin; namely substantially pure APO-I and APO-II. Also provided are processes for preparing substantially pure 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: Grant
    Filed: June 16, 2011
    Date of Patent: November 11, 2014
    Assignee: Apotex Pharmachem Inc.
    Inventors: Kiran Kumar Kothakonda, Allan W. Rey
  • Publication number: 20140323467
    Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Application
    Filed: May 23, 2014
    Publication date: October 30, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan