The Five-membered Hetero Ring Consists Of One Nitrogen And Four Carbons Patents (Class 514/408)
  • Patent number: 10227298
    Abstract: The present application discloses solid forms of compound (1) (1), methods for making them, as well as compositions comprising said solid forms.
    Type: Grant
    Filed: April 13, 2015
    Date of Patent: March 12, 2019
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Urs Schwitter, Ralph Diodone, Rudolf Benz, Zhongjiang Jia, Choi Duk Soon, Ningxin Yan, Bharat Patel
  • Patent number: 10130625
    Abstract: Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.
    Type: Grant
    Filed: July 22, 2015
    Date of Patent: November 20, 2018
    Assignees: University of Maryland, College Park, University of Maryland, Baltimore
    Inventors: Herman O. Sintim, Jie Zhou, Changhao Wang, Rena Lapidus
  • Patent number: 10112907
    Abstract: The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: September 21, 2017
    Date of Patent: October 30, 2018
    Assignee: NOVARTIS AG
    Inventors: Badry Bursulaya, Andreas Fisch, James Paul Lajiness, Rainer Machauer, Swapnil Malekar, Hank Michael James Petrassi, Farshad Ramazani, Anne-Catherine Remond, Thomas Ullrich, Peggy Usselmann, Eric Vangrevelinghe
  • Patent number: 10035770
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: July 31, 2018
    Assignee: Cytokinetics, Incorporated
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, Jr.
  • Patent number: 10004824
    Abstract: An injectable sterilized aqueous composition including at least one hyaluronic acid, at least one polyol and at least one local anesthetic chosen from the group made of benzocaine, chloroprocaine, procaine, etidocaine, aptocaine, chlorobutanol, diamocaine, dyclonine, guafecainol, polidocanol, mepivacaine, prilocaine, articaine, bupivacaine, ropivacaine, tetracaine and salts thereof and isolated isomers thereof. The invention also relates to a process for adapting the rheological properties of a heat sterilized injectable aqueous composition. The invention also relates to a process for producing an injectable sterilized aqueous composition according to the invention, and also to uses of said injectable sterilized aqueous composition according to the invention.
    Type: Grant
    Filed: May 11, 2015
    Date of Patent: June 26, 2018
    Assignee: LABORATOIRES VIVACY
    Inventors: Guy Vitally, Jérémie Bon Betemps
  • Patent number: 9776968
    Abstract: The present invention relates to a process of providing the 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in substantially free form (Compound 1).
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: October 3, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: David Siesel
  • Patent number: 9750728
    Abstract: A method of treating a patient in need of treatment for a disease selected from the group consisting of cancer, hamartoma syndrome and hereditary myopathy, the method comprising administering to the patient an effective dose of at least one PRCP and PREP dual antagonist pyridine compound of Formula (I) or an acid salt thereof, which can be administered either alone or in combination with at least one mTOR inhibitor.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: September 5, 2017
    Assignee: Targeted Therapeutics, LLC
    Inventors: Lei Duan, Victor Levenson, GuoGuang Ying
  • Patent number: 9657351
    Abstract: Use of at least an MDM2 gene panel, preferably a four gene MDM2 gene panel, as a biomarker for predicting the response to a MDM2 antagonist.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: May 23, 2017
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Hua Zhong, David Geho, Gong Chen, Gwen Nichols, Markus Dangl
  • Patent number: 9643925
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: August 27, 2015
    Date of Patent: May 9, 2017
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, Jr.
  • Patent number: 9545396
    Abstract: The present invention relates to a pharmaceutical composition of PRCP antagonist, PREP antagonist, or PRCP-PREP dual antagonist. The present invention also relates to a pharmaceutical composition jointly using PRCP antagonist and mTOR antagonist, or jointly using PREP antagonist and mTOR antagonist, or jointly using PRCP-PREP dual antagonist and mTOR antagonist. In addition, the present invention also relates to a method for utilizing the pharmaceutical compositions to treat and prevent cancers and diseases related to insulin receptor substrate protein and PI3K/AKT/mTOR signal pathway.
    Type: Grant
    Filed: September 29, 2013
    Date of Patent: January 17, 2017
    Assignee: Targeted Therapeutics, LLC
    Inventors: Lei Duan, Victor Levenson, Guoguang Ying
  • Patent number: 9505716
    Abstract: In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Grant
    Filed: June 1, 2015
    Date of Patent: November 29, 2016
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Jianguo Ma
  • Patent number: 9227933
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: January 12, 2015
    Date of Patent: January 5, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric Stangeland, Daisuke Roland Saito, Priscilla Van Dyke, Lori Jean Patterson
  • Patent number: 9221699
    Abstract: This method of restricting methane production in methanogenic bacteria, by the use of the enzyme and coenzyme inhibitors, works during anaerobic reductive dechlorination. Various compounds such as, but not limited to, red yeast rice, vitamin B10 derivatives, and ethanesulfonates are utilized to disrupt these different enzyme and coenzyme systems responsible for the production of methane. This method affects the competition of the methanogen and halo bacteria for the organic hydrogen donors that are injected in the soil and groundwater system during the remediation process.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: December 29, 2015
    Assignee: Innovative Environment Technologies, Inc.
    Inventors: Michael Scalzi, Antonis Karachalios
  • Patent number: 9119836
    Abstract: Amisulpride is used in the therapy of nausea, vomiting or retches. The therapy may utilize a novel injectable formulation, in unit dosage form, comprising less than 50 mg amisulpride.
    Type: Grant
    Filed: February 4, 2014
    Date of Patent: September 1, 2015
    Assignee: Acacia Pharma Limited
    Inventors: Julian Clive Gilbert, Robert William Gristwood, Nicola Cooper, Gabriel Fox
  • Patent number: 9101611
    Abstract: As it is generally known, when a medication fails to work properly it is increased in dosage and/or changed to another medication. Sulfonylurea medication has known to have secondary failure which increases blood glucose since the mid-1950s. (1) From new research, I have found a new way to overcome sulfonylurea Glimepiride's effectiveness to continue lowering blood glucose when secondary failure occurs which increases blood glucose. The new way is made by stopping taking it for 3 or 5 days which automatically also lower blood glucose and then resuming it which further lowers more blood glucose like the first day taking it. It is assumed that it works because it fools the human body like it's the first day when resuming taking it.
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: August 11, 2015
    Inventor: Howard T Joe
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Patent number: 9023869
    Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: May 5, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 9006281
    Abstract: The present disclosure is directed to compounds and methods for treating irritable bowel syndrome, chronic kidney disease and end stage renal disease by administering to a subject in need thereof a compound or a pharmaceutically acceptable salt thereof, wherein the compound has the structure
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: April 14, 2015
    Assignee: Ardelyx, Inc.
    Inventors: Noah Bell, Christopher Carreras, Dominique Charmot, Jeffrey W Jacobs, Michael Robert Leadbetter, Marc Navre
  • Patent number: 8993614
    Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2, R3 and R4 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: March 31, 2015
    Assignee: F. Hoffmann-La Roche AG
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Binh Thanh Vu, Chunlin Zhao, Daniel Fishlock
  • Publication number: 20150087642
    Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Inventors: Bronislava GEDULIN, Andrew A. YOUNG, Howard E. GREENE
  • Patent number: 8980935
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: March 17, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh
  • Publication number: 20150073030
    Abstract: The T cells specific to human collagen type II, one of the possible autoantigens, have a crucial role in the development of rheumatoid arthritis in the context of HLA-DR4. The protein-protein interactions between the T cell receptor (TCR) and the type II collagen linked to the allele MHC of class II HLA-DR4 may thus represent the target for the development of new drugs against rheumatoid arthritis. Using computational virtual screening techniques, families of pharmacologically active molecules have been identified that interfere with the TCR/collagen ll-MHCII interaction. The compounds identified here open up new possibilities in the treatment of rheumatoid arthritis.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 12, 2015
    Inventors: Maria Cristina De Rosa, Francesco Ria, Bruno Giardina, Gianfranco Ferraccioli, Davide Pirolli, Chiara Nicolo'
  • Patent number: 8945549
    Abstract: The invention relates to methods for treating pain disorders including neuropathic and inflammatory pain and to methods to reduce or eliminate nociceptive tolerance induced by opiate analgesic use by administering an agent that suppresses or blocks S1P biological activity.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: February 3, 2015
    Assignee: Saint Louis University
    Inventor: Daniela Salvemini
  • Publication number: 20150031726
    Abstract: Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N?-substituted aryl urea compounds; N-substituted aryl, N?-substituted heteroaryl urea compounds; N-substituted aryl, N?-substituted aryl thiourea compounds and N-substituted aryl, N?-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
    Type: Application
    Filed: October 15, 2014
    Publication date: January 29, 2015
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 8940782
    Abstract: The present invention is directed to a non-therapeutical process for deterring vermin, which is based on the usage of the largely known beta amino-alcohol derivatives of formula (I) as described herein. Further, the present invention is directed to corresponding vermin-deterring compositions which contain these substances as the active ingredient, compounds of the formula (I) for the preparation of vermin-deterring compositions, and the use of compounds of formula (I) in the defense against vermin.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: January 27, 2015
    Assignee: Novartis AG
    Inventors: Pierre Ducray, Tania Cavaliero, Maike Renner, Jacques Bouvier
  • Patent number: 8940775
    Abstract: The invention relates to the use of 20-(4-carboxyphenyl)-2,13-dimethyl-3,12-diethyl-[22] pentaphyrine as antibacterial agent in photodynamic treatment. This expanded porphyrin derivatized in position 4 with a carboxyphenyl group proved very active after photo-oxidation both against S. aureus and E. hirae. Its high antibacterial activity and its low toxicity make this pentaphyrine particularly useful as antimicrobial agent both for photodynamic therapy against bacterial infections and in the disinfection of microbiologically contaminated liquids.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: January 27, 2015
    Assignee: Universita' Degli Studi di Udine
    Inventors: Rosalisa Fedele, Clara Comuzzi, Giada Rossi, Daniele Goi
  • Publication number: 20140371176
    Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.
    Type: Application
    Filed: September 3, 2014
    Publication date: December 18, 2014
    Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
  • Publication number: 20140371272
    Abstract: The invention provides compounds of formula (I) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for treating cancer or treating autoimmune diseases or preventing transplant rejection using compounds of formula (I).
    Type: Application
    Filed: January 18, 2013
    Publication date: December 18, 2014
    Inventors: Venkatram R. Mereddy, Lester R. Drewes, Mohammed Abrar Alam, Sravan K. Jonnalagadda, Shirisha Gurrapu
  • Publication number: 20140371252
    Abstract: Processes for making and using compounds of formula (I): wherein R1, R2, R3, R4a, R4b, R5 and R6 are defined herein, as well as other indene derivatives are disclosed herein. These compounds are disclosed as being useful in treating inflammatory conditions or diseases.
    Type: Application
    Filed: January 23, 2014
    Publication date: December 18, 2014
    Applicant: Aquinox Pharmaceuticals Inc.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Patent number: 8901157
    Abstract: The present invention discloses compositions and a method of improving the pharmacokinetics of pharmaceutical agents (or pharmaceutically acceptable salts, esters, and prodrugs thereof) which are metabolized by cytochrome P450 monoxygenase comprising coadministering ritonavir or a pharmaceutically acceptable salt, ester, and prodrug thereof.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: December 2, 2014
    Assignee: AbbVie Inc.
    Inventors: Dale J. Kempf, Kennan C. Marsh
  • Publication number: 20140341986
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
  • Patent number: 8883800
    Abstract: The present invention relates to substituted quinazolines of formula (I): wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Patent number: 8865741
    Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.
    Type: Grant
    Filed: February 18, 2012
    Date of Patent: October 21, 2014
    Assignee: Asana Biosciences, LLC
    Inventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8846655
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: September 30, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
  • Patent number: 8841339
    Abstract: The present invention relates to antifouling compositions and particularly to compositions which are able to provide an improved protecting effect against fouling organisms. More particularly, the present invention relates to synergistic antifouling compositions comprising an amount of at least 3.5 wt %, based on the total weight of the dry mass of the composition, of 4-bromo-2-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile, or a salt thereof, together with another biocide selected from bethoxazin, tolylfluanide, dichlofluanide, or DCOIT; for protecting materials against fouling organisms. This invention thus relates to the field of protection of materials, such as underwater objects, protection of wood, wood products, biodegradable materials and coatings.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: September 23, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Mark Arthur Josepha Van der Flaas, Jan Remi Nys
  • Patent number: 8840923
    Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: September 23, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Vincenzo Russo, Elisa Liberati, Nicola Cazzolla, Leonardo Marchitto, Lorella Ragni
  • Patent number: 8841338
    Abstract: The present invention relates to antifouling compositions and particularly to compositions which are able to provide an improved protecting effect against fouling organisms. More particularly, the present invention relates to synergistic antifouling compositions comprising an amount of at least 3.5 wt %, based on the total weight of the dry mass of the composition, of 4-bromo-2-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile, or a salt thereof, together with another biocide selected from bethoxazin, tolylfluanide, dichlofluanide, or DCOIT; for protecting materials against fouling organisms. This invention thus relates to the field of protection of materials, such as underwater objects, protection of wood, wood products, biodegradable materials and coatings.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: September 23, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Mark Arthur Josepha Van Der Flaas, Jan Remi Nys
  • Publication number: 20140275090
    Abstract: Provided herein are methods of treating or ameliorating primary sclerosing cholangitis and inflammatory bowel disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating primary sclerosing cholangitis comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventors: Bronislava GEDULIN, Michael GREY, Niall O'DONNELL, Bradley T. KELLER
  • Publication number: 20140271734
    Abstract: Provided herein are methods of treating or ameliorating Barrett's esophagus by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Provided herein are methods of treating or ameliorating gastroesophageal reflux disease (GERD) by administering to an individual in need thereof a therapeutically effective amount of an ASBTI or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating symptoms or complications associated with Barrett's esophagus or GERD comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Bronislava GEDULIN, Michael GREY, Niall O'DONNELL, Bradley T. KELLER
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Patent number: 8822442
    Abstract: The invention features somatostatin-dopamine chimeric analogs and methods relating to their therapeutic use for the treatment of neoplasia, acromegaly, and other conditions.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: September 2, 2014
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Zheng Xin Dong, Michael Dewitt Culler, Yeelena Shen
  • Publication number: 20140223609
    Abstract: Embodiments of the present invention relate to insecticidal Bacillus thuringiensis Cry1 and Cry2 polypeptides. Methods for using the polypeptides and nucleic acids of embodiments of the invention to synergistically enhance resistance of plants to insect predation are encompassed in embodiments of the present invention.
    Type: Application
    Filed: April 16, 2014
    Publication date: August 7, 2014
    Applicants: E I DU PONT DE NEMOURS AND COMPANY, PIONEER HI BRED INTERNATIONAL INC
    Inventors: John Lindsey Flexner, Deirdre Kapka-Kitzman, Lisa Procyk, Bruce H. Stanley, Jianzhou Zhao
  • Patent number: 8791135
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: July 29, 2014
    Assignee: Purdue Research Foundation
    Inventor: Arun K. Ghosh
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Patent number: 8772293
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: July 8, 2014
    Assignees: Pfizer Limited, Icagen Inc.
    Inventors: Alan Daniel Brown, Marcel John De Groot, Brian Edward Marron, David James Rawson, Thomas Ryckmans, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West
  • Publication number: 20140187557
    Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
    Type: Application
    Filed: March 10, 2014
    Publication date: July 3, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
  • Patent number: 8765816
    Abstract: Compounds that are central nervous system drug candidates for the treatment of cognitive decline and, more particularly, Alzheimer's disease are provided. Methods of treating, inhibiting, and/or abatement of cognitive decline and/or Alzheimer's disease with a compound or pharmaceutically acceptable salt of the invention are also provided. Also provided are methods of preparing the compounds/compositions of the invention.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: July 1, 2014
    Assignee: Cognition Therapeutics, Inc.
    Inventors: Gilbert M. Rishton, Susan Catalano
  • Publication number: 20140179661
    Abstract: A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
    Type: Application
    Filed: April 8, 2012
    Publication date: June 26, 2014
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
  • Publication number: 20140179660
    Abstract: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
    Type: Application
    Filed: August 8, 2012
    Publication date: June 26, 2014
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh