Chalcogen Bonded Directly To A Piperazine Ring Carbon Patents (Class 514/255.02)
  • Patent number: 10912821
    Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: February 9, 2021
    Assignee: MannKind Corporation
    Inventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
  • Patent number: 10583176
    Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
    Type: Grant
    Filed: October 4, 2018
    Date of Patent: March 10, 2020
    Assignee: Mannkind corporation
    Inventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
  • Patent number: 10426796
    Abstract: A composition for influencing biological growth includes a solution having a first volume and having low pH fluid base including dextrose, and albumin, wherein the concentration of albumin in the solution is between about 10 mg/ml and about 150 mg/ml.
    Type: Grant
    Filed: June 10, 2017
    Date of Patent: October 1, 2019
    Assignee: SMART Surgical, Inc.
    Inventors: Christopher D. Jones, Nathan Quintanar, Roshan Patel
  • Patent number: 10421729
    Abstract: Disclosed herein are DKP microcrystals made by an improved method where they do not irreversibly self-assemble into microparticles. The microcrystals can be dispersed by atomization and re-formed by spray drying into particles having spherical shell morphology. Active agents and excipients can be incorporated into the particles by spray drying a solution containing the components to be incorporated into microcrystalline diketopiperazine particles. In particular, the microcrystalline particle compositions are suitable for pulmonary drug delivery of one or more peptides, proteins, nucleic acids and/or small organic molecules.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: September 24, 2019
    Assignee: MannKind Corporation
    Inventors: Bryan R. Wilson, Joseph J. Guarneri, Marshall L. Grant
  • Patent number: 10213463
    Abstract: A method for performing a therapy in a subject includes providing a composition including a solution having a first volume and including a low pH fluid base including dextrose, and albumin, wherein the concentration of albumin in the solution is between about 10 mg/ml and about 150 mg/ml, and implanting within, near, or adjacent tissue of the subject an effective amount of the composition.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: February 26, 2019
    Assignee: SMART Surgical, Inc.
    Inventors: Christopher D. Jones, Nathan Quintanar
  • Patent number: 10172850
    Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.
    Type: Grant
    Filed: April 17, 2017
    Date of Patent: January 8, 2019
    Assignee: MannKind Corporation
    Inventor: Kelly Sullivan Kraft
  • Patent number: 10131637
    Abstract: Disclosed are compounds of the class of 2-phenylacetamides that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), and methods of using these modulators to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: November 20, 2018
    Assignees: Shifa Biomedical Corporation, Temple University—Of The Commonwealth System of Higher Education
    Inventors: Sherin Salaheldin Abdel-Meguid, Magid Abou-Gharbia, Benjamin Blass, Wayne Childers, Nabil Elshourbagy, Victor Ghidu, Rogelio Martinez, Harold Meyers, Shaker A. Mousa
  • Patent number: 10130685
    Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
    Type: Grant
    Filed: June 9, 2017
    Date of Patent: November 20, 2018
    Assignee: MannKind Corporation
    Inventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
  • Patent number: 9925300
    Abstract: The present invention relates to the contacting of one or more surfaces of an implantable medical device with one or more diketopiperazines (DKPs).
    Type: Grant
    Filed: October 10, 2012
    Date of Patent: March 27, 2018
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventor: David Bar-Or
  • Patent number: 9675674
    Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: June 13, 2017
    Assignee: MannKind Corporation
    Inventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
  • Patent number: 9259471
    Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: February 16, 2016
    Assignee: MannKind Corporation
    Inventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
  • Patent number: 9108931
    Abstract: The invention relates to novel multifunctional bioactive compounds of the formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds, in particular as therapeutic agents for the treatment of immune disorders.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: August 18, 2015
    Assignee: MANUS PHARMACEUTICALS (CANADA) LTD.
    Inventor: Vladislav I. Deigin
  • Patent number: 9034878
    Abstract: The invention provides (i) a method of treating metabolic syndrome in an animal, (ii) a method of suppressing the appetite of an animal, (iii) a method of treating obesity in an animal, (iv) a method of reducing the weight of an animal in need thereof, (v) a method of reducing a blood lipid level in an animal in need thereof, (vi) a method of treating non-alcoholic steatohepatitis in an animal, and (vii) a method of inhibiting adipogenesis. The methods comprise administering an effective amount of an active ingredient, wherein the active ingredient comprises a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them to the animal. The invention also provides a kit comprising a container holding a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them; and instructions for administration. The diketopiperazines have the formula given in the application.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: May 19, 2015
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventor: David Bar-Or
  • Publication number: 20150133470
    Abstract: Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Michael Neary, James Nieman, Steven Tanis, Daniel Lawton, Garry Smith
  • 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
  • Patent number: 8999995
    Abstract: Provided herein are isotopically enriched arylsulfonamides, for example, of Formula I, that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: April 7, 2015
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter
  • 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
  • Publication number: 20150051224
    Abstract: The invention provides diketopiperazines of formula I. The invention also provides pharmaceutical compositions comprising the diketopiperazines, or pharmaceutically-acceptable salts or prodrugs thereof, as the active ingredient. The invention further provides therapeutic treatments that utilize the diketopiperazines of formula I, including inhibition of a proliferative disease or condition, inhibition of angiogenesis, treatment of an angiogenic disease or condition, treatment of cancer and precancerous conditions, treatment of a fibrotic disorder, treatment of a viral infection, treatment of an Akt-mediated disease or condition, inhibition of the production, release or both of matrix metalloproteinase-9, and inhibition of Akt activation.
    Type: Application
    Filed: August 27, 2014
    Publication date: February 19, 2015
    Inventor: David Bar-Or
  • Publication number: 20150051223
    Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: August 8, 2014
    Publication date: February 19, 2015
    Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K.R. Rao, Greg Thomas
  • Publication number: 20150011550
    Abstract: Use of a synthetic compound selected from the group consisting of JKF-006, JKF-011 and JKF-027 in the preparation of a medicament for treating Alzheimer's disease.
    Type: Application
    Filed: January 25, 2013
    Publication date: January 8, 2015
    Applicant: BEIJING JOEKAI BIOTECHNOLOGY LLC
    Inventor: Weiwei Ma
  • Patent number: 8927546
    Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
    Type: Grant
    Filed: September 22, 2010
    Date of Patent: January 6, 2015
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
  • Patent number: 8916568
    Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: December 23, 2014
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K. R. Rao, Greg Thomas
  • Patent number: 8906926
    Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: December 9, 2014
    Assignee: MannKind Corporation
    Inventor: Kelly Sullivan Kraft
  • Patent number: 8889099
    Abstract: Methods are provided for purifying peptides and proteins by incorporating the peptide or protein into a diketopiperazine or competitive complexing agent to facilitate removal one or more impurities, from the peptide or protein. Formulations and methods also are provided for the improved transport of active agents across biological membranes, resulting for example in a rapid increase in blood agent concentration. The formulations include microparticles formed of (i) the active agent, which may be charged or neutral, and (ii) a transport enhancer that masks the charge of the agent and/or that forms hydrogen bonds with the target biological membrane in order to facilitate transport. In one embodiment, insulin is administered via the pulmonary delivery of microparticles comprising fumaryl diketopiperazine and insulin in its biologically active form. This method of delivering insulin results in a rapid increase in blood insulin concentration that is comparable to the increase resulting from intravenous delivery.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: November 18, 2014
    Assignee: MannKind Corporation
    Inventors: Solomon S. Steiner, Rodney J. Woods, Joseph W. Sulner
  • Patent number: 8871772
    Abstract: The invention provides diketopiperazines of formula I. The invention also provides pharmaceutical compositions comprising the diketopiperazines, or pharmaceutically-acceptable salts or prodrugs thereof, as the active ingredient. The invention further provides therapeutic treatments that utilize the diketopiperazines of formula I, including inhibition of a proliferative disease or condition, inhibition of angiogenesis, treatment of an angiogenic disease or condition, treatment of cancer and precancerous conditions, treatment of a fibrotic disorder, treatment of a viral infection, treatment of an Akt-mediated disease or condition, inhibition of the production, release or both of matrix metalloproteinase-9, and inhibition of Akt activation.
    Type: Grant
    Filed: February 23, 2012
    Date of Patent: October 28, 2014
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventor: David Bar-Or
  • Publication number: 20140296225
    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: Application
    Filed: October 22, 2012
    Publication date: October 2, 2014
    Inventors: Haifeng Tang, Barbara Pio, Nardos Teumelsan, Alexander Pasternak, Reynalda DeJesus
  • Publication number: 20140288077
    Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 25, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Naoaki Fujii, Marcelo Actis, Chandanamali Punchihewa, Michele Connelly, Sean Wu
  • Publication number: 20140288059
    Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.
    Type: Application
    Filed: April 25, 2014
    Publication date: September 25, 2014
    Applicant: THE PENN STATE RESEARCH FOUNDATION
    Inventors: Gong Chen, Yanming Wang, Pingxin Li, Jing Hu, Shu Wang, Yuji Wang
  • Publication number: 20140286913
    Abstract: The invention provides compositions that increase the mobilization, homing, expansion, and/or differentiation of stem cells and methods of using the same for the treatment of mammals.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 25, 2014
    Applicant: Ampio Pharmaceuticals, Inc.
    Inventors: David Bar-Or, Greg Thomas
  • Patent number: 8841307
    Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: September 23, 2014
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K. R. Rao, Greg Thomas
  • Patent number: 8802666
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: August 12, 2014
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Publication number: 20140213597
    Abstract: The invention provides methods for treatment of acute coronary syndrome and prediction of adverse cardiac events on the basis of elevations of catalytic iron in biological fluid of a human subject. An embodiment of the invention provides a method for early detection of acute coronary syndrome (ACS) in a human subject at the time of presentation of the chest pain. The method includes analyzing a test sample of the biological fluid for amount of catalytic iron and detecting acute coronary syndrome in the human subject.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 31, 2014
    Inventors: Mohan Rajapurkar, Suhas Lele, Sudhir Shah
  • Publication number: 20140073649
    Abstract: Provided herein are isotopically enriched arylsulfonamides, for example, of Formula I, that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disease, disorder, or condition.
    Type: Application
    Filed: September 6, 2013
    Publication date: March 13, 2014
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter
  • Publication number: 20140066446
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Application
    Filed: August 30, 2013
    Publication date: March 6, 2014
    Applicant: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter
  • Patent number: 8653085
    Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.
    Type: Grant
    Filed: August 22, 2012
    Date of Patent: February 18, 2014
    Assignee: Mankind Corporation
    Inventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
  • Publication number: 20140038945
    Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds ate inhibitors of PDE4function and are useful for improving cognitive function in animals.
    Type: Application
    Filed: July 31, 2013
    Publication date: February 6, 2014
    Applicant: DART NEUROSCIENCE (CAYMAN) LTD
    Inventors: Terence P. Keenan, Alan P. Kaplan
  • Patent number: 8637521
    Abstract: The present invention discloses multifunctional bioactive compounds of formula (I) constituted of an immunoregulatory portion linked to a stabilizer moiety and pharmaceutical compositions thereof useful in the treatment of immune disorders and hemopoietic disorders such as immune cytopema, multiple myeloma, chronic lymphoid leucosis, lymphocytic lymphomas, lymphosarcomas.
    Type: Grant
    Filed: August 1, 2007
    Date of Patent: January 28, 2014
    Assignee: Manus Pharmaceuticals (Canada) Ltd.
    Inventor: Vladislav I. Deigin
  • Publication number: 20140017199
    Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
    Type: Application
    Filed: July 3, 2013
    Publication date: January 16, 2014
    Inventors: Manoj C. Desai, Allen Yu Hong, Hon Chung Hui, Hongtao Liu, Randall W. Vivian, Lianhong Xu
  • Publication number: 20140018355
    Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.
    Type: Application
    Filed: June 27, 2013
    Publication date: January 16, 2014
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Timothy L. MACDONALD, Jerry L. NADLER, Peng CUI
  • Publication number: 20130345238
    Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: August 28, 2013
    Publication date: December 26, 2013
    Applicant: DMI Acquisition Corp.
    Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K.R. Rao, Greg Thomas
  • Publication number: 20130331386
    Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, irritable bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 12, 2013
    Inventors: Robert Shalwitz, Kevin Gene Peters
  • Patent number: 8592422
    Abstract: In one aspect, the invention relates to bicyclic triazole and pyrazole lactams, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: November 26, 2013
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Gregor James MacDonald, Han Min Tong, Carrie K. Jones, Manuel Jesús Alcázar-Vaca, José Ignacio Andrés-Gil, Chrysa Malosh
  • Patent number: 8557825
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: October 15, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van heusden
  • Publication number: 20130267516
    Abstract: Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: October 10, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Kristoffer Månsson, Lars Kristian Albert Blæhr
  • Publication number: 20130237529
    Abstract: The invention relates to a compound (I) wherein R is a heterocyclyl radical; R1 and R2 are independently H or alkyl; R3 is H, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl; R4 and R5 are independently H or alkyl; q is a number selected from 0 and 1; and the salts, solvates, prodrugs or stereoisomers thereof having inhibitory activity for UBC13-UEV interactions and which can be used in the production of pharmaceutical compositions intended for antitumor therapy or the treatment and/or prophylaxis of diseases associated to metabolic pathways involving the UBC13 enzyme, metabolic pathways involving transcriptional factor NF-?B, or pathways involving PCNA or RAD6.
    Type: Application
    Filed: July 23, 2012
    Publication date: September 12, 2013
    Inventors: María Luz Ortiz Melguizo, Mª Carmen Fabrega Claveria
  • Patent number: 8507496
    Abstract: The invention provides (i) a method of treating metabolic syndrome in an animal, (ii) a method of suppressing the appetite of an animal, (iii) a method of treating obesity in an animal, (iv) a method of reducing the weight of an animal in need thereof, (v) a method of reducing a blood lipid level in an animal in need thereof, (vi) a method of treating non-alcoholic steatohepatitis in an animal, and (vii) a method of inhibiting adipogenesis. The methods comprise administering an effective amount of an active ingredient, wherein the active ingredient comprises a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them to the animal. The invention also provides a kit comprising a container holding a diketopiperazine, a prodrug of a diketopiperazine or a pharmaceutically-acceptable salt of either of them; and instructions for administration. The diketopiperazines have the formula given in the application.
    Type: Grant
    Filed: September 7, 2011
    Date of Patent: August 13, 2013
    Assignee: DMI Acquisition Corp.
    Inventor: David Bar-Or
  • Patent number: 8497373
    Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: July 30, 2013
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael N. Greco, Harold R. Almond, Jr., Lawrence de Garavilla, Michael J. Hawkins, Michael J. Humora, Yun Qian, Donald Gilmore Walker, Sergio Cesco-Cancian, Christopher Norman Nilsen, Mitul N. Patel, Kirk Leonard Sorgi, Eugene Powell
  • Publication number: 20130190288
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Patent number: 8450301
    Abstract: The invention relates to the use of piperazine compounds of formula (I) or the agriculturally useful salts of piperazine compounds of formula (I) as herbicides, the variables in formula (I) being defined as cited in the claims and the description.
    Type: Grant
    Filed: December 29, 2006
    Date of Patent: May 28, 2013
    Assignee: BASF SE
    Inventors: Eike Hupe, Cyrill Zagar, Matthias Witschel, Toralf Kühn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Michael Puhl, Robert Reinhard, Bernd Sievernich, Klaus Groβmann, Thomas Ehrhardt, Michael Rack
  • Patent number: 8426415
    Abstract: Magnesium salts/complexes of compounds useful for inhibiting the ADAM-IO protein and methods of making and purifying them are provided. Further provided are compositions comprising magnesium salts/complexes of the compounds in combination with a pharmaceutically acceptable carrier. The compounds well as such compositions comprising them are useful for the treatment of cancer, arthritis, diseases related to angiogenesis, such as renal diseases, heart diseases, such as heart failure, atherosclerosis, and stroke, inflammation, ulcer, infertility, scleroderma, endometriosis, mesothelioma, and diabetes. In addition, methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role are provided.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: April 23, 2013
    Assignee: Symphony Evolution, Inc.
    Inventors: Sriram Naganathan, JoAnn Wilson, Daniel A. Dickman