Polycylo Ring System Having A Ring Nitrogen In The System Patents (Class 514/80)
  • Patent number: 10239869
    Abstract: 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: Grant
    Filed: September 3, 2016
    Date of Patent: March 26, 2019
    Assignee: LUPIN LIMITED
    Inventors: 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
  • Patent number: 10189802
    Abstract: 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: Grant
    Filed: January 27, 2017
    Date of Patent: January 29, 2019
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Patent number: 10173027
    Abstract: 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: Grant
    Filed: October 7, 2016
    Date of Patent: January 8, 2019
    Assignee: Cook Medical Technologies LLC
    Inventors: John C. Sigmon, Jr., Vihar Surti
  • Patent number: 10155749
    Abstract: 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: Grant
    Filed: January 7, 2016
    Date of Patent: December 18, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Armin Heckel, Dieter Hamprecht, Joerg Kley
  • Patent number: 10138213
    Abstract: 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: Grant
    Filed: June 24, 2015
    Date of Patent: November 27, 2018
    Assignee: Translate Bio, Inc.
    Inventors: Frank DeRosa, Shrirang Karve, Michael Heartlein
  • Patent number: 10131679
    Abstract: 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: Grant
    Filed: October 30, 2015
    Date of Patent: November 20, 2018
    Assignee: 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
  • Patent number: 9993492
    Abstract: 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: Grant
    Filed: May 22, 2014
    Date of Patent: June 12, 2018
    Assignee: University of Graz
    Inventors: Wolfgang Schühly, Ulrike Riessberger-Gallé, Javier Hernández-López, Karl Crailsheim
  • Patent number: 9987237
    Abstract: 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: Grant
    Filed: August 24, 2015
    Date of Patent: June 5, 2018
    Assignee: NeOnc Technologies, Inc.
    Inventors: Thomas Chen, Daniel Levin, Satish Pupalli, Daniel Anthony Dickman
  • Patent number: 9981954
    Abstract: 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: Grant
    Filed: January 7, 2016
    Date of Patent: May 29, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Armin Heckel, Sara Frattini, Joerg Kley
  • Patent number: 9867825
    Abstract: A combination of a CDK4/6 inhibitor and a MEK inhibitor for the treatment of diseases such as cancer.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: January 16, 2018
    Assignee: Novartis AG
    Inventors: Giordano Caponigro, Scott Delach, Shivang Doshi, Thomas Horn-Spirohn, Sunkyu Kim
  • Patent number: 9809609
    Abstract: 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: Grant
    Filed: May 1, 2012
    Date of Patent: November 7, 2017
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
  • Patent number: 9777018
    Abstract: 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: Grant
    Filed: August 21, 2015
    Date of Patent: October 3, 2017
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Dhanapalan Nagarathnam, Swaroop K. Vakkalanka, Srikant Viswanadha, Gayatri S. Merikapudi
  • Patent number: 9730904
    Abstract: 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: Grant
    Filed: May 8, 2015
    Date of Patent: August 15, 2017
    Assignee: SBI Pharmaceuticals Co., Ltd.
    Inventor: Tohru Tanaka
  • Patent number: 9732035
    Abstract: 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: Grant
    Filed: June 2, 2016
    Date of Patent: August 15, 2017
    Assignee: NEWLINK GENETICS CORPORATION
    Inventors: Mario Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Hima Potturi, Hong Zhuang
  • Patent number: 9556110
    Abstract: 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: Grant
    Filed: January 16, 2015
    Date of Patent: January 31, 2017
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Patent number: 9481698
    Abstract: The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of this process.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: November 1, 2016
    Assignee: Sandoz AG
    Inventors: Hubert Sturm, Josef Wieser
  • Patent number: 9452197
    Abstract: 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: Grant
    Filed: December 27, 2013
    Date of Patent: September 27, 2016
    Assignee: Acceleron Pharma, Inc.
    Inventors: Jasbir Seehra, John Knopf, Robert S. Pearsall, Asya Grinberg, Ravindra Kumar
  • Patent number: 9339029
    Abstract: 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: Grant
    Filed: September 3, 2015
    Date of Patent: May 17, 2016
    Assignee: Preceres Inc.
    Inventors: Richard Wayne Heidebrecht, Jr., Cheng Zhong
  • Patent number: 9303052
    Abstract: 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: Grant
    Filed: August 12, 2013
    Date of Patent: April 5, 2016
    Assignee: I. OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Makoto Komatsu, Fumitaka Goto, Yasuhiro Menjo, Keigo Yamada, Takakuni Matsuda, Yusuke Kato
  • Patent number: 9238627
    Abstract: 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: Grant
    Filed: October 18, 2013
    Date of Patent: January 19, 2016
    Assignees: Array BioPharma, Inc., Novartis AG
    Inventors: Christoph Max Krell, Marian Misun, Daniel Andreas Niederer, Werner Heinz Pachinger, Marie-Christine Wolf, Daniel Zimmermann, Weidong Liu, Peter J. Stengel, Paul Nichols
  • Patent number: 9181286
    Abstract: 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: Grant
    Filed: January 16, 2014
    Date of Patent: November 10, 2015
    Assignee: Retrophin, Inc.
    Inventors: Andrew Vaino, Marek Biestek, Martin Shkreli
  • Patent number: 9095165
    Abstract: 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: Grant
    Filed: October 27, 2009
    Date of Patent: August 4, 2015
    Assignee: SBI Pharmaceuticals Co., Ltd.
    Inventor: Tohru Tanaka
  • Patent number: 9062053
    Abstract: 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: Grant
    Filed: August 7, 2014
    Date of Patent: June 23, 2015
    Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Spargo
  • Patent number: 9051317
    Abstract: 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: Grant
    Filed: December 16, 2011
    Date of Patent: June 9, 2015
    Assignee: JANSSEN SCIENCES IRELAND UC
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Publication number: 20150148311
    Abstract: 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: Application
    Filed: June 20, 2014
    Publication date: May 28, 2015
    Inventors: Jason G. Lewis, Nicholas Reich, Tao Chen, Jeffrey W. Jacobs, Dominique Charmot, Marc Navre, Patricia Finn, Christopher Carreras, Andrew Spencer
  • Publication number: 20150148312
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 28, 2015
    Inventors: Herriot Tabuteau, Graeme Jones
  • Publication number: 20150141374
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 21, 2015
    Inventors: Herriot Tabuteau, Graeme Jones
  • Publication number: 20150141373
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: January 28, 2015
    Publication date: May 21, 2015
    Inventors: Herriot Tabuteau, Graeme Jones
  • Publication number: 20150133403
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 14, 2015
    Inventors: Herriot Tabuteau, Graeme Jones
  • Publication number: 20150126477
    Abstract: 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: Application
    Filed: February 24, 2012
    Publication date: May 7, 2015
    Inventors: 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
  • Patent number: 9018191
    Abstract: 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: Grant
    Filed: August 21, 2012
    Date of Patent: April 28, 2015
    Assignee: AstraZeneca AB
    Inventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri Jung, Georges Rene Pasquet
  • Publication number: 20150111853
    Abstract: 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: Application
    Filed: October 22, 2014
    Publication date: April 23, 2015
    Inventors: Jan-Ji Lai, Pradip M. Pathare, Laxma Kolla, Adrien F. Soret
  • Publication number: 20150111854
    Abstract: 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: Application
    Filed: December 5, 2014
    Publication date: April 23, 2015
    Inventors: Chika TAKAHASHI, Hindenori MIKAMIYAMA, Toshiyuki AKIYAMA, Kenji TOMITA, Yoshiyuki TAODA, Makoto KAWAI, Kosuke ANAN, Masayoshi MIYAGAWA, Naoyuki SUZUKI
  • Patent number: 9006387
    Abstract: 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: Grant
    Filed: February 14, 2014
    Date of Patent: April 14, 2015
    Assignee: 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
  • Publication number: 20150099721
    Abstract: 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: Application
    Filed: May 10, 2013
    Publication date: April 9, 2015
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jaime Acquaviva, Suqin He, David Proia
  • Patent number: 8993542
    Abstract: 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: Grant
    Filed: January 23, 2009
    Date of Patent: March 31, 2015
    Assignee: Chimerix Inc.
    Inventors: Ernest Randall Lanier, Merrick R. Almond, George R. Painter
  • Publication number: 20150072957
    Abstract: This disclosure provides compositions containing solid forms of tazobactam arginine, and methods of manufacturing and using these compositions.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Applicant: Calixa Therapeutics, Inc.
    Inventors: Jan-Ji Lai, Jian-Qiao Gu, Pradip M. Pathare, Valdas Jurkauskas, Joseph Terracciano, Nicole Miller Damour
  • Publication number: 20150065463
    Abstract: 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: Application
    Filed: November 12, 2014
    Publication date: March 5, 2015
    Applicant: University of Kansas
    Inventors: ShiDu Yan, Koteswara Rao Valasani
  • Patent number: 8969359
    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: June 3, 2013
    Date of Patent: March 3, 2015
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Arnaud Le Tiran, Anne-Laure Grillot, Paul S. Charifson, Youssef Laafiret Bennani, Hardwin O'Dowd, Emanuele Perola
  • Publication number: 20150057250
    Abstract: Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.
    Type: Application
    Filed: November 7, 2014
    Publication date: February 26, 2015
    Inventor: Herriot Tabuteau
  • Patent number: 8956648
    Abstract: 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: Grant
    Filed: December 18, 2009
    Date of Patent: February 17, 2015
    Assignee: Biolitec PharmaMarketing Ltd
    Inventors: Burkhard Gitter, Susanna Gräfe, Arno Wiehe, Volker Albrecht, Matthias Epple, Janine Schwiertz, Kathirvel Ganesan
  • Patent number: 8957050
    Abstract: 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: Grant
    Filed: March 11, 2013
    Date of Patent: February 17, 2015
    Assignee: Pioneer Surgical Technology, Inc.
    Inventors: Francis Vincent Lamberti, Richard Chris Klann, Ronald Stewart Hill
  • Publication number: 20150045323
    Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.
    Type: Application
    Filed: September 13, 2013
    Publication date: February 12, 2015
    Inventors: Linda N. Casillas, Pamela A. Haile, Robert W. Marquis, JR., Gren Wang
  • Patent number: 8940716
    Abstract: 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: Grant
    Filed: May 4, 2011
    Date of Patent: January 27, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang
  • Patent number: 8937150
    Abstract: 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: Grant
    Filed: May 4, 2011
    Date of Patent: January 20, 2015
    Assignee: AbbVie Inc.
    Inventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
  • Publication number: 20150018313
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT, Armin HECKEL
  • Publication number: 20150018315
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT
  • Publication number: 20150018312
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: May 4, 2014
    Publication date: January 15, 2015
    Applicant: WOCKHARDT LTD.
    Inventors: Vijaykumar Jagdishwar PATIL, Ravikumar TADIPARTHI, Satish BIRAJDAR, Sachin BHAGWAT
  • Publication number: 20150018314
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Joerg KLEY, Sara FRATTINI, Dieter HAMPRECHT
  • Publication number: 20150011508
    Abstract: The invention provides compounds of formulae (I) and (II) and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.
    Type: Application
    Filed: August 28, 2012
    Publication date: January 8, 2015
    Inventors: Xiaodong Liu, Xiaolin Li, Jon Loren, Valentina Molteni, Juliet Nabakka, Bao Nguyen, Hank Michael James Petrassi, Vince Yeh