Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai Patents (Class 514/183)
  • Patent number: 8835409
    Abstract: 3-Alkenyl-6-halo-4-aminopicolinic acids and their derivatives are potent herbicides demonstrating a broad spectrum of weed control.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: September 16, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Paul R. Schmitzer, Thomas L. Siddall
  • Patent number: 8835415
    Abstract: The present disclosure is in relation to antiviral preparations obtained from plant sources namely Cinnamon, Litchi and Arachis. It provides a composition and a process to prepare the composition comprising pentameric procyanidin flavonoid, trimers and tetramers. The composition improves immunity response and found to be useful in treatment and management of HIV infection and AIDS and for the prevention, treatment and management of Influenza virus and infection.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: September 16, 2014
    Assignee: Indus Biotech Private Limited
    Inventors: Sunil Bhaskaran, Mohan Vishwaraman
  • Patent number: 8828983
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: September 9, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mimi L. Quan, Carl P. Decicco, James R. Corte, Cailan Wang
  • Patent number: 8829028
    Abstract: This invention provides the use of a 5-HT4 receptor antagonist in the manufacture of a medicament for treating or preventing heart failure. Particular heart disorders to be treated are selected from the group comprising chronic heart failure, congestive heart failure, chronic congestive heart failure and heart failure resulting from ischaemic heart disease. Methods of treating heart failure using 5-HT4 receptor antagonists and pharmaceutical compositions containing 5-HT4 receptor antagonists are also provided.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: September 9, 2014
    Assignee: Serodus AS
    Inventor: Finn Olav Levy
  • Patent number: 8828982
    Abstract: This invention concerns the use of a compound for the manufacture of a medicament for the prevention of HIV infection via sexual intercourse and related intimate contact between partners, wherein the compound is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: September 9, 2014
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Heeres, Paulus Joannes Lewi, Marc René de Jonge, Lucien Maria Henricus Koymans, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Jéròme Emile Georges Guillemont, Elisabeth Therese Jeanne Pasquier, Frank Xavier Jozef Herwig Arts
  • Publication number: 20140248270
    Abstract: A method of treating a tar-responsive dermatological disorder includes topically applying an anhydrous tar composition to skin of a mammal, preferably a human, that is involved with the disorder, the composition including a wax and a therapeutically effective amount of tar for topical treatment of the tar-responsive dermatological disorder, the composition being in liquid form when at a temperature selected from room temperature and a temperature of skin of a mammal upon application of the composition to the skin of the mammal.
    Type: Application
    Filed: May 13, 2014
    Publication date: September 4, 2014
    Inventors: Ruey J. YU, Eugene J. VAN SCOTT
  • Patent number: 8822444
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: September 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Omar D. Lopez, Qi Chen, Makonen Belema, Lawrence G. Hamann
  • Patent number: 8822443
    Abstract: To provide a solid herbicidal composition in which decomposition of the herbicidal active ingredient is suppressed, and favorable herbicidal activity is stably exhibited. A solid herbicidal composition comprising (1) 1-(4,6-dimethoxypyrimidin-2-yl)-3-(3-trifluoromethyl-2-pyridylsulfonyl)urea or its salt and (2) at least one surfactant selected from the group consisting of a naphthalene sulfonate condensed with formaldehyde, an alkylnaphthalene sulfonate condensed with formaldehyde, a dialkylnaphthalene sulfonate condensed with formaldehyde and a polycarboxylate.
    Type: Grant
    Filed: January 15, 2007
    Date of Patent: September 2, 2014
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Yoshiaki Ishihara, Kazutaka Ikeda
  • 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: 20140242153
    Abstract: Disclosed are novel methods for making cochleates and cochleate compositions that include introducing a cargo moiety to a liposome in the presence of a solvent. Also disclosed are cochleates and cochleate compositions that include an aggregation inhibitor, and optionally, a cargo moiety. Additionally, anhydrous cochleates that include a protonized cargo moiety, a divalent metal cation and a negatively charge lipid are disclosed. Methods of using the cochleate compositions of the invention, including methods of administration, are also disclosed.
    Type: Application
    Filed: January 30, 2014
    Publication date: August 28, 2014
    Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Raphael J. Mannino, Susan Gould-Fogerite, Sara L. Krause-Elsmore, David Delmarre, Ruying Lu
  • Patent number: 8815286
    Abstract: The present invention provides a pharmaceutical composition comprising the following active ingredients: 1) an angiotensin II receptor antagonist or a pharmaceutically acceptable salt thereof, 2) pioglitazone or a pharmaceutically acceptable salt thereof; and 3) rosuvastatin or a pharmaceutically acceptable salt thereof. The present invention also provides use of the pharmaceutical composition in preparing a medicament for treating hypertension or metabolic syndrome. The pharmaceutical composition of the present invention can treat hypertension or metabolic syndrome, while effectively controlling the incidence of associated cardiovascular diseases and more potently improving survival prognosis in hypertensive patients. When blood pressure is lowered to desired level, the risk factors such as cardiovascular diseases are rectified, metabolic disorders and prognosis of patients are improved, and survival rate of hypertensive patients is raised.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: August 26, 2014
    Assignee: Lunan Pharmaceutical Group Corporation
    Inventor: Zhiquan Zhao
  • Patent number: 8815837
    Abstract: There is provided a pharmaceutical composition that is adapted for pulmonary administration by inhalation, which composition comprises a glitazone, such as pioglitazone or rosiglitazone, and one or more pharmaceutically acceptable carriers and/or excipients, and wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer. There is also provided a use and kit.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: August 26, 2014
    Assignee: Pulmagen Therapeutics (Inflammation) Limited
    Inventors: Harry Finch, Craig Fox, Mohammed Sajad, Monique Bondil Van Niel, Andrew Forrest
  • Patent number: 8809311
    Abstract: A process for improving the health of a subject, the process comprising orally administering a composition comprising hydroxytyrosol to the subject to provide the subject with a daily dose of about 0.1 to about 750 ?g hydroxytyrosol per kg of body weight, and a dietary supplement in dosage unit form for oral administration, the dosage unit form comprising a composition containing about 1 microgram to about 50 milligrams hydroxytyrosol or an ester or salt thereof.
    Type: Grant
    Filed: August 10, 2010
    Date of Patent: August 19, 2014
    Inventor: Darlene McCord
  • Patent number: 8809310
    Abstract: Disclosed is a method for the treatment of Multiple System Atrophy comprising administering to a subject an amount of R(+)-N-propargyl-1-aminoindan or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 21, 2007
    Date of Patent: August 19, 2014
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventor: Werner Poewe
  • Patent number: 8809312
    Abstract: A composition including an effective amount of a compound including manganese [III]tetrakis(4-benzoic acid)porphyrin (MnTBAP), derivatives or analogs thereof to induce a reduction in body weight of a mammal or to improve insulin sensitivity of an obese mammal. A method including introducing an effective amount of a compound including manganese [III]tetrakis(4-benzoic acid)porphyrin (MnTBAP), derivatives or analogs thereof to a mammal to induce a reduction in body weight or to induce an increase in metabolism or insulin sensitivity of the mammal.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: August 19, 2014
    Inventors: Jonathan R. Brestoff, Thomas H. Reynolds, IV
  • Patent number: 8809366
    Abstract: A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation.
    Type: Grant
    Filed: November 12, 2012
    Date of Patent: August 19, 2014
    Assignee: Tianjin Institute of Pharmaceutical Research
    Inventors: Dengke Liu, Ying Liu, Nan Yue, Furong Chen, Chubing Tan, Yunsong Zhou, Peng Liu, Yigui Zhao, Deguang Zhi, Mo Liu, Bingni Liu, Changjiang Huang, Lida Tang
  • Patent number: 8809347
    Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: August 19, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Jiaxin Yu, Joane Litvak
  • Patent number: 8809282
    Abstract: The present invention relates, in general, to a method of treating patients undergoing enzyme replacement therapy (ERT) or other therapy involving the administration of a proteinaceous therapeutic agent as well gene replacement therapy with non-viral or viral vectors, or other therapeutic modality or modalities, used alone or in combination, which involve the administration of exogenous substances for potential therapeutic benefit, including, but not limited to DNA vaccines, siRNA, splice-site switching oligomers (SSOs) as well as RNA-based nanoparticles (RNPs) and nanovaccines. The invention further relates to compounds and compositions suitable for use in such methods.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: August 19, 2014
    Assignee: Duke University
    Inventors: Priya S. Kishnani, Suhrad G. Banugaria, Dwight D. Koeberl, Sean N. Prater
  • Publication number: 20140220122
    Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: BHI Limited Partnership
    Inventors: Xianqi KONG, Mohamed ATFANI, Benoit BACHAND, Abderrahim BOUZIDE, Stephane CIBLAT, Sophie LEVESQUE, David MIGNEAULT, Isabelle VALADE, Xinfu WU, Daniel DELORME
  • Publication number: 20140219915
    Abstract: Disclosed herein is a method for coupling a first compound having the formula (I) with a second compound that contains a carbonyl group. Also disclosed herein are compounds that can be formed by this method, and uses for such compounds.
    Type: Application
    Filed: July 6, 2012
    Publication date: August 7, 2014
    Applicants: AUSTRALIAN NUCLEAR SCIENCE AND TECHNOLOGY ORGANISATION, THE AUSTRALIAN NATIONAL UNIVERSITY
    Inventors: Suzanne Virginia Smith, Eskender Mume, Gary James Perkins
  • Publication number: 20140219952
    Abstract: The present invention relates to the field of stem cells. In one aspect, the present invention provides methods of treating a subject with acute liver injury comprising administering to the subject a therapeutically effective amount of at least one stem cell mobilizer.
    Type: Application
    Filed: March 23, 2011
    Publication date: August 7, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventor: Andrew MacGregor Cameron
  • Patent number: 8796251
    Abstract: The invention provides compositions and methods for the treatment of glomerulonephritis. In one embodiment, the invention provides a compound of formula (I) R-L-CO—X??(I) (wherein R is a C10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO2, said hydrocarbon group comprising at least 4 non-conjugated double bonds; L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO; and X is an electron withdrawing group) or a salt thereof for use in the treatment of glomerulonephritis.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: August 5, 2014
    Assignee: Avexxin AS
    Inventors: Berit Johansen, Andrea Huwiler
  • Patent number: 8796327
    Abstract: A method for inhibiting the production of cytokines of T helper cell type II (Th2 cell) and/or inhibiting the production of chemokines in a mammal is provided, wherein the method comprises administrating to the mammal an effective amount of an active component selected from a group consisting of a compound of formula (I), pharmaceutically acceptable salts and esters of the compound, and combinations thereof:
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: August 5, 2014
    Assignee: China Medical University
    Inventors: Chen-Chen Lee, Chien-Neng Wang
  • Patent number: 8795701
    Abstract: The invention relates to a method for improving the utilization of the production potential of transgenic plants which comprises treating the plant with active compound combinations comprising an active compound from the group of the anthranilamides and at least one further insecticide.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer CropScience AG
    Inventors: Wolfram Andersch, Christian Funke, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8796250
    Abstract: The present invention provides methods for treating and/or preventing conditions and diseases in humans and other mammals that are associated with and/or mediated by signal transduction pathways comprising platelet-derived growth factor receptor (PDGFR) by administering diaryl ureas of Formula I. The present invention also provides devices and methods for treating, ameliorating, preventing, or modulating restenosis following angioplastic surgery or other invasive procedures that affect or injure the vascular system, and graft rejection following transplantation of a donor tissue into a host, where a stent or other omplantable device comprises an effective amount of diaryl ureas of Formula I.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: August 5, 2014
    Assignee: Bayer Healthcare LLC
    Inventors: Scott Wilhelm, Jacques Dumas, Gaetan Ladouceur, Mark Lynch, William Scott
  • Publication number: 20140213627
    Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.
    Type: Application
    Filed: January 30, 2014
    Publication date: July 31, 2014
    Applicant: RAMOT AT TEL AVIV UNIVERSITY LTD.
    Inventors: Roni SCHERZER, Ehud GAZIT, Daniel SEGAL
  • Patent number: 8791097
    Abstract: This invention provides the method or use of CCI-779 in the treatment of papillary renal cell carcinoma.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: July 29, 2014
    Assignee: Wyeth LLC
    Inventors: Gary Dukart, James Joseph Gibbons, Jr., Anna Berkenblit, Jay Marshall Feingold
  • Patent number: 8791098
    Abstract: The invention relates to bioactive pre-tubulysin derivatives, their preparation and pharmacological use.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: July 29, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Yi Chai, Angelika Ullrich, Uli Kazmaier, Rolf Müller
  • Publication number: 20140206658
    Abstract: The present invention relates to compounds and compositions useful as antioxidants and in particular to selenium containing compounds of formula (I): wherein n is 1, 2, or 3; m is 2, 3, 4, or 5; and each R] is independently —(optionally substituted C1-C3 alkylene) p-OH, where p is 0 or 1, or a salt thereof. The invention also relates to the use of these seleno-compounds in the treatment of diseases or conditions associated with increased levels of oxidants produced by myeloperoxidase (MPO), such as for instance, atherosclerosis.
    Type: Application
    Filed: October 28, 2011
    Publication date: July 24, 2014
    Applicants: THE HEART RESEARCH INSTITUTE LTD., THE UNIVERSITY OF MELBOURNE
    Inventors: Carl Herbert Schiesser, Corin Storkey, Michael Jonathan Davies
  • Patent number: 8785485
    Abstract: The present invention provides an animal ectoparasite-controlling agent containing as an active ingredient a hydrazide compound represented by the formula (1) wherein R3 represents a fluorine atom, a chlorine atom, a bromine atom, a methyl group, an ethyl group or a hydrogen atom, R5 and R6 are the same or different each other and each represents a methyl group or a hydrogen atom, R4 represents a C1-C6 haloalkyl group, which shows excellent controlling effects on animal ectoparasites.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: July 22, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Kaori Ikari
  • Patent number: 8785156
    Abstract: Methods of using TLE3 as a marker for predicting the likelihood that a patient's cancer will respond to chemotherapy. Methods of using TLE3 as a marker for selecting a chemotherapy for a cancer.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: July 22, 2014
    Assignee: Clarient Diagnostic Services, Inc.
    Inventors: Brian Z. Ring, Douglas T. Ross, Robert S. Seitz, Rodney A. Beck
  • Patent number: 8785446
    Abstract: Patients are subject to a post-seizure treatment regime to separately inhibitor consecutive targets of an epileptogenic cascade comprising neurotransmitter receptor signaling, kinase/phosphatase activity, protein translation, and apoptosis or inflammation.
    Type: Grant
    Filed: January 17, 2010
    Date of Patent: July 22, 2014
    Assignee: Children's Medical Center Corporation
    Inventors: Frances E. Jensen, Sanjay N. Rakhade
  • Patent number: 8785428
    Abstract: Use of an orally or nasally available formulation of Tretazicar for poisoning vermin. An orally available or nasally available formulation of Tretazicar, wherein in the orally available formulation the Tretazicar is protected from acid hydrolysis, and provided that the formulation is not solid Tretazicar in a gelatin capsule. A formulation of Tretazicar in which the Tretazicar is protected from acid hydrolysis, wherein the formulation is present in a liquid form. A combination of Tretazicar and bait. A method of poisoning vermin comprising making available to the vermin an orally or nasally available formulation of Tretazicar and allowing the vermin to ingest or inhale the formulation of Tretazicar.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: July 22, 2014
    Assignee: Morvus Technology Limited
    Inventors: Richard J. Knox, Roger Melton, Philip Burke
  • Patent number: 8785471
    Abstract: Preparation and usage of a pharmaceutical composition containing ferulic acid and matrine compounds are described. The ingredients ferulic acid and matrine compounds in this pharmaceutical composition have synergistic effects which can obviously improve the pharmacology effects of both the ferulic acid and matrine compounds. Moreover, the pharmaceutical composition can significantly increase the aqueous and fat solubility of the individual ingredients.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: July 22, 2014
    Assignee: Qingdao Qiyuan Bio-Technologies Co., Ltd.
    Inventors: Xiaojie Sun, Weifu Ma
  • Publication number: 20140199235
    Abstract: The present invention relates to a nanoparticle having a linker connected to a long alkane or alkene chain, and a method for preparing the nanoparticle. The alkyl chain of C10-30 introduced with a ligand of the present invention can be coated on a hydrophobic nanoparticle through a noncovalent bond, enabling easy introduction of various ligands to the nanoparticle, and the nanoparticle having various functional groups prepared using the method can be applied to fluorescent detection, MRI, raman spectroscopy, optical detection, PET, SPECT, or gamma image device, and the ligand of the visualization agents can be modified to be used for new vessels detection, cancer cell detection, immunocyte detection, hepatocyte detection, cell death detection, and gene detection.
    Type: Application
    Filed: January 31, 2012
    Publication date: July 17, 2014
    Applicant: SNU R&DB FOUNDATION
    Inventors: Jae Min Jeong, Young Kyoung Lee, Dong Soo Lee, June-Key Chung, Myung Chul Lee
  • Patent number: 8778922
    Abstract: Provided herein are steroid containing compositions suitable for providing therapeutically effective amounts of at least one steroid to individuals. Also provided herein are compositions comprising testosterone and/or testosterone derivatives suitable for providing therapeutically effective and safe amounts of testosterone over periods of time. Further provided are methods of treating andro- and/or testosterone deficiency in individuals by administering to the individuals compositions described herein.
    Type: Grant
    Filed: August 22, 2012
    Date of Patent: July 15, 2014
    Assignee: Lipocine Inc.
    Inventors: Chandrashekar Giliyar, Nachiappan Chidambaram, Mahesh V. Patel, Srinivasan Venkateshwaran
  • Patent number: 8778923
    Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: July 15, 2014
    Assignee: Receptos, Inc.
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Patent number: 8779138
    Abstract: Camptothecin-based compounds are useful for treating a neoplasm in mammalian subjects by administering such compound to the subjects in combination with radiotherapy, i.e., the treatment of tumors with radioactive substances or radiation from a source external to the subject. Camptothecin-based compounds are modified by positioning at least one electron-affinic group around the camptothecin structure to enhance their value in combination with radiotherapy. New Camptothecin-based compounds are disclosed that are useful for treating cancer by administering the novel compounds alone or in combination with radiotherapy.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: July 15, 2014
    Assignees: Sutter West Bay Hospital, Catholic Healthcare West
    Inventor: Li-Xi Yang
  • Patent number: 8778920
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferab
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: July 15, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Eddy Jean Edgard Freyne, Peter Jacobus Johannes Antonius Buijnsters, Kristof Van Emelem, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
  • Patent number: 8778919
    Abstract: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N; —X1— represents C1-4alkyl, in particular methyl; —X2— represents —C1-4alkyl- or —C1-4alkyl-NR7—, in particular propyl, -ethyl-NR7— or -propyl-NR7—; —Y— represents —NR2—C1-6alkyl-CO—NR4—, -Het1-C1-6alkyl-CO—NR5— or -Het2-CO—NR6— and wherein the —C1-6alkyl-linker of —NR2—C1-6alkyl-CO—NR4— or -Het1-C1-6alkyl-CO—NR5— is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents —C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolid
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: July 15, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frederik Jan Rita Rombouts, Christopher John Love, Kristof Van Emelen, Sven Franciscus Anna Van Brandt, Tongfei Wu
  • Patent number: 8778914
    Abstract: The present invention relates to a prodrug, comprising a pharmaceutically and/or diagnostically active compound, and one or more bisphosphonate groups, to a process for producing such a prodrug, and to a pharmaceutical composition comprising said prodrug, to be used for the treatment of bone-related disorders such as bone cancer.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: July 15, 2014
    Assignee: KTB Tumorforschungsgesellschaft mbH
    Inventors: Felix Kratz, Katrin Hochdoerffer
  • Patent number: 8778837
    Abstract: The invention relates to the novel use of known active substance combinations which consist firstly of 3,4-dichloro-2?-cyano-1,2-thiazole-5-carboxanilide, of the formula which is known, and secondly further known insecticidal active substances, for controlling animal pests, especially arthropods, in particular insects.
    Type: Grant
    Filed: November 27, 2008
    Date of Patent: July 15, 2014
    Assignee: Bayer CropScience AG
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8778921
    Abstract: Aspects of the present invention provide compositions comprising a sulfur containing compound and a compound of the formula (I); and also provide methods of their preparation and use.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: July 15, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: James R. Porter, Sonali Puri
  • Publication number: 20140193376
    Abstract: The present embodiments provide for combinations of modulators that increase hematopoietic stem cell engraftment or increase mobilization in vivo. Methods and compositions for modulating the mobilization of stem cells, particularly for promoting or increasing the mobilization of hematopoietic stem cells (HSCs) from the bone marrow to the peripheral blood are disclosed. One aspect of the invention relates to the use of a CXCR4 antagonist that act in concert with specific molar ratios of S1P receptor 1 (S1PR1) modulator agents to promote HSC mobilization. The invention also relates to methods of using these combinations of CXCR4 antagonists and S1PR1 modulator agents for enhancing the mobilization of hematopoietic stem cells when harvesting of the stem cells, for example for the treatment of diseases, disabilities or conditions whereby transplantation of such cells would be beneficial in ameliorating a symptom associated with such diseases, disabilities or conditions.
    Type: Application
    Filed: June 18, 2012
    Publication date: July 10, 2014
    Applicant: CHILDREN'S MEDICAL CENTER CORPORATION
    Inventors: Leonard I Zon, Owen J. Tamplin
  • Patent number: 8772273
    Abstract: The invention provides retinoic acid receptor (RAR) selective agonists and formulations thereof for the treatment of disease or for inducing a medically beneficial effect.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: July 8, 2014
    Assignee: QuRetino Therapeutics, Inc.
    Inventor: Ferenc Makra
  • Patent number: 8772306
    Abstract: One embodiment of the present invention is to improve the safety and efficacy of the administration of GHB or a salt thereof to a patient. It has been discovered that the concomitant administration of an MCT inhibitor, such as diclofenac, valproate, or ibuprofen, will affect GHB administration. For example, it has been discovered that diclofenac lowers the effect of GHB in the body, thereby potentially causing an unsafe condition. Furthermore, it has been discovered that valproate increases the effect of GHB on the body, thereby potentially causing an unsafe condition.
    Type: Grant
    Filed: April 29, 2013
    Date of Patent: July 8, 2014
    Assignee: Jazz Pharmaceuticals, Inc.
    Inventor: Mark Eller
  • Patent number: 8772275
    Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: July 8, 2014
    Assignee: Curis, Inc.
    Inventors: Lee L. Rubin, Oivin Guicherit, Stephen Price, Edward Andrew Boyd
  • Patent number: 8772274
    Abstract: Anti-cancer compositions and methods are described including one or more compounds having the structural formula I: R2-R—R1, where R is phenyl, where R1 is (CH2)n—Se—C(?NH)—NH2, where R2 is (CH2)n—Se—C(?NH)—NH2 or R2 is H, and where each n is independently 2, 3, 4, 5, 6, 7, or 8. Methods of treating a subject are provided according to embodiments of the present invention which include administering a therapeutically effective amount of a composition including one or more compounds having the structural formula I to a subject having a condition characterized by Akt dysregulation. Administering a therapeutically effective amount of a composition including one or more compounds having the structural formula I to a subject detectably increases apoptosis and/or decreases proliferation of cancer cells, particularly cancer cells characterized by Akt dysregulation.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: July 8, 2014
    Assignee: The Penn State Research Foundation
    Inventors: Gavin P. Robertson, Subbarao V. Madhunapantula, Shantu Amin, Dhimant Desai
  • Patent number: 8772272
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH?CH—CH, N—CH?N—CH or CH—CH?N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from m
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: July 8, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Eddy Jean Edgard Freyne, Marc Willems, Pierre Henri Storck, Virginie Sophie Poncelet, Kristof Van Emelen, Peter Jacobus Johnnes Antonius Buijnsters, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
  • Publication number: 20140187526
    Abstract: The invention disclosed herein generally relates to methods and compositions for inhibiting proteasome activity comprising a syrbactin compound having the structure of Formula I or II:
    Type: Application
    Filed: December 2, 2013
    Publication date: July 3, 2014
    Applicant: Pono Corporation
    Inventors: Andre S. Bachmann, Robert Dudler, Michael Groll