2 Amino Acid Residues In The Peptide Chain Patents (Class 514/21.91)
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Publication number: 20140038910Abstract: Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.Type: ApplicationFiled: July 17, 2013Publication date: February 6, 2014Applicant: Saint Louis UniversityInventors: Peter RUMINSKI, David GRIGGS
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Patent number: 8633154Abstract: The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.Type: GrantFiled: March 6, 2013Date of Patent: January 21, 2014Assignee: Arizona Board of Regents, a body corporate of the State of Arizona Acting for and on behalf of Arizona State UniversityInventors: George R. Pettit, Rui Tan, Robin K. Pettit
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Publication number: 20130345123Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein A is a five to eight membered monocyclic or a nine to twelve membered bicyclic heterocyclic ring, as further defined herein; Y is S, CH2, or CH; Z is CH or N; R7 and R9 are hydrogen or (C1-C6)alkyl; R2 is (C1-C6)alkoxy, OH, CN, (C1-C6)alkyl, halogen, or CF3; r and s are 0, 1, or 2; and R1 and R3 are as further defined herein. These compounds are agonists, partial agonists and/or modulators of the NPY4 receptor and may be used for the treatment and prophylaxis of obesity, food intake, and other diseases and conditions modulated by the NPY4 receptor.Type: ApplicationFiled: March 13, 2012Publication date: December 26, 2013Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Chongqing Sun, William R. Ewing, Scott A. Bolton, Zhengxiang Gu, Yanting Huang, Natesan Murugesan, Yeheng Zhu
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Publication number: 20130345120Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: Glaxosmithkline LLCInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
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Publication number: 20130338084Abstract: Hydrogel compositions comprise an aqueous dispersion phase and a plurality of peptides, or derivatives, or analogues thereof. Each peptide comprises at least two amino acid residues and an aromatic stacking ligand and the hydrogel is formed by self-assembly of said peptides in said aqueous dispersion medium. The aqueous dispersion phase is physiologically acceptable and may have a pH of 6 to 8, as may the hydrogel itself. The hydrogel may be used for cell culture or for treatment of medical conditions characterised by tissue loss/damage.Type: ApplicationFiled: April 15, 2013Publication date: December 19, 2013Applicant: The University of StrathclydeInventors: Rein Vincent Ulijn, Vineetha Jayawarna, Andrew Smith, Julie Elizabeth Gough
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Publication number: 20130336902Abstract: A personal care composition is disclosed comprising a di-amido gellant, wherein the di-amido gellant has a formula: wherein R1 and R2 are aminofunctional end-groups which may be the same or different, and L is a linking moiety of molecular weight from 14 to 500 g/mol. The personal care composition may take a variety of forms such as a leave-on composition or an emulsion and/or may comprise one or more actives or agents.Type: ApplicationFiled: June 13, 2012Publication date: December 19, 2013Inventors: SUSANA FERNANDEZ PRIETO, JOHAN SMETS, BEATRIU ESCUDER GIL, JUAN FELIPE MIRAVET CELADES, VICENT JOSEP NEBOT CARDA, PAUL ROBERT TANNER
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Publication number: 20130331344Abstract: The present invention aims to provide antidepressants which are free from the problem of side effects and are excellent in safety. The present invention also aims to provide learning motivation improvers which are useful for improvement of learning motivation and can be ingested continuously. The present invention provides antidepressants and learning motivation improvers, each comprising a cyclic dipeptide with the 2,5-diketopiperazine structure as an active ingredient.Type: ApplicationFiled: August 13, 2013Publication date: December 12, 2013Applicants: CEREBOS PACIFIC LIMITED, SUNTORY HOLDINGS LIMITEDInventors: Nobuo TSURUOKA, Yoshinori BEPPU, Hirofumi KOUDA, Hiroshi WATANABE
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Publication number: 20130331328Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.Type: ApplicationFiled: February 14, 2012Publication date: December 12, 2013Applicant: GEORGETOWN UNIVERSITYInventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Ziad Sahab
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Patent number: 8598123Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.Type: GrantFiled: September 7, 2012Date of Patent: December 3, 2013Assignee: Pfizer Inc.Inventors: Christopher Gordon Barber, Dafydd Rhys Owen, Lisa Rosemary Thompson
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Publication number: 20130310311Abstract: The present invention relates to compounds of the formulae: in which C5-C16 alkyl, R1 is and isosteres and salts thereof.Type: ApplicationFiled: December 1, 2011Publication date: November 21, 2013Inventors: Ziaeddin Shariat-Madar, John Matthew Rimoldi, Rama Sarma Venkta Subbarahmanya Gadepalli
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Publication number: 20130309247Abstract: The present invention provides compounds of formula M-L-M? (where M and M? are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.Type: ApplicationFiled: December 13, 2011Publication date: November 21, 2013Applicant: NOVARTIS AGInventors: Zhuoliang Chen, Christopher Sean Straub
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Patent number: 8580557Abstract: The present invention relates to a casein hydrolysate containing free amino acids and in vivo indigestible peptides having minimally suppressed in vivo enzymatic digestibility, and expected to express functions, such as hypotensive effect, in living organism, and to a method for preparing such a hydrolysate, and use thereof. The casein hydrolysate of the present invention contains free amino acids and peptides, such as in vivo indigestible peptides including Xaa-Pro and Xaa-Pro-Pro, obtained by hydrolyzing animal milk casein to have an average chain length of not longer than 2.1 in terms of the number of amino acid residues, and has ACE inhibitory activity or hypotensive effect.Type: GrantFiled: September 1, 2010Date of Patent: November 12, 2013Assignee: Calpis Co., Ltd.Inventors: Naoyuki Yamamoto, Seiichi Mizuno, Takanobu Gotou, Keiichi Matsuura, Tadashi Shinoda, Hideo Nishimura
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Publication number: 20130266648Abstract: Disclosed are compressed tablets containing atazanavir sulfate, optionally with another active agents, e.g., anti-HIV agents, granules that contain atazanavir sulfate and an intragranular lubricant that can be used to make the tablets, compositions comprising a plurality of the granules, processes for making the granules and tablets, and methods of treating HIV.Type: ApplicationFiled: May 31, 2013Publication date: October 10, 2013Inventors: Otilia May Koo, Faranak Nikfar, Steven Diaz
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Patent number: 8551953Abstract: The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.Type: GrantFiled: November 14, 2012Date of Patent: October 8, 2013Assignee: DMI Acquisition Corp.Inventors: David Bar-Or, Raphael Bar-Or, Richard Shimonkevitz
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Patent number: 8546336Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: GrantFiled: September 7, 2012Date of Patent: October 1, 2013Assignee: Novartis AGInventors: Zhuoliang Chen, Mark G. Charest, Christine Hiu-Tung Chen, Miao Dai, Feng He, Huangshu Lei, Ly Luu Pham, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming David Wang, Fan Yang, Leigh Zawel
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Patent number: 8541379Abstract: A substance capable of imparting a kokumi having CaSR agonist activity is described. This substance is able to impart kokumi in a superior manner, in particular, at the initial taste, and is also highly stable and can easily be produced at a low cost. The present invention thus provides a kokumi-imparting composition which includes such a substance as well as a complex kokumi-imparting composition which includes the substance and other substances possessing the CaSR agonist activities in combination. More particularly, the present invention herein provides a kokumi-imparting composition including ?-Glu-Nva (L-?-glutamyl-L-norvaline), and a complex kokumi-imparting composition including the foregoing substance and another substance having a CaSR agonist activity, in combination.Type: GrantFiled: June 21, 2012Date of Patent: September 24, 2013Assignee: Ajinomoto Co., Inc.Inventors: Takashi Miyaki, Naohiro Miyamura, Megumi Kaneko, Yusuke Amino, Reiko Yasuda, Yuzuru Eto, Takaho Tajima
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Patent number: 8536137Abstract: The present invention is directed to the use of a class of peptide compounds for treating tumor pain, in particular bone cancer pain, for treating chemotherapy-induced pain and for treating nucleoside-induced pain.Type: GrantFiled: October 12, 2009Date of Patent: September 17, 2013Assignee: UCB Pharma GmbHInventors: Bettina Beyreuther, Thomas Stöhr
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Publication number: 20130231278Abstract: The present invention relates to a process to produce a composition comprising water-soluble peptides and having a Trp/LNAA ratio of more than 0.15, which comprises hydrolyzing lysozyme, preferably hen eggs lysozyme, to prepare a hydrolysate having a DH of between 5 and 45.Type: ApplicationFiled: October 31, 2012Publication date: September 5, 2013Applicant: DSM IP Assets B.V.Inventors: Andre Leonardus De Roos, Luppo Edens, Rudolf Franciscus Van Beckhoven, Alexander Lucia Leonardus Duchateau, Joris Kloek
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Publication number: 20130225509Abstract: The present invention relates to a method of enhancing endurance of a human subject through administration of alanyl-glutamine or alanyl-glutamine salt.Type: ApplicationFiled: November 5, 2010Publication date: August 29, 2013Applicant: KYOWA HAKKO BIO CO., LTD.Inventor: Kentaro Sugimura
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Publication number: 20130225511Abstract: The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.Type: ApplicationFiled: November 8, 2011Publication date: August 29, 2013Inventors: Per-Göran Gillberg, Hans Graffner, Ingemar Starke
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Publication number: 20130225512Abstract: Dipeptide analogs comprising a tryptophan (Trp) moiety coupled to a beta-sheet breaker moiety derived from alpha-aminoisobutyric acid (Aib) are disclosed. The dipeptide analogs exhibit an improved performance in inhibiting amyloid fibril formation, as compared to previously described dipeptides. Compositions containing the dipeptide analogs and uses thereof in treating amyloid-associated diseases and disorders are also disclosed.Type: ApplicationFiled: November 15, 2011Publication date: August 29, 2013Applicant: Merz Pharma GmbH & Co. KGaAInventors: Ehud Gazit, Yaniv Amir, Ludmila Buzhansky, Ulrich Abel, Anat Frydman-Marom
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Publication number: 20130225510Abstract: The invention provides an orally-administrable nutritional product comprising a dipeptide including a branched chain amino acids (BCAA). In one embodiment, the nutritional product comprises a dipeptide selected from at least one of the following: alanyl-leucine, alanyl-isoleucine, alanyl-valine, glycyl-leucine, glycyl-isoleucine, and glycyl-valine.Type: ApplicationFiled: April 11, 2013Publication date: August 29, 2013Applicant: Nestec S.A.Inventor: Nestec S.A.
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Publication number: 20130224294Abstract: The invention relates to dry processes for producing oral dosage forms, more specifically tablets, comprising atazanavir and adhesion enhancers. The invention further relates to compacted intermediates comprising atazanavir and adhesion enhancers.Type: ApplicationFiled: September 27, 2011Publication date: August 29, 2013Applicant: RATIOPHARM GMBHInventors: Dominique Meergans, Ralph Stefan
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Patent number: 8518885Abstract: A novel class of peptide ?-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA2-AA1-CO—NH—(CH2)n—R3. Processes for the synthesis of peptidyl ?-ketoamide derivatives. Compositions and methods for inhibiting cysteine proteases, inhibiting calpains, and treating disease caused by cysteine proteases and calpains are provided.Type: GrantFiled: July 16, 2008Date of Patent: August 27, 2013Assignees: Georgia Tech Research Corporation, Emory UniversityInventors: James C. Powers, Jonathan D. Glass, Asli Ovat, Zhaozhao Li
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Patent number: 8518886Abstract: The present invention relates generally to the use of ?-glutamyl antioxidants, particularly ?-glutamyl-cysteine, as cytoprotective agents to prevent reperfusion injury (i.e., hemorrhagic transformation) of the blood-brain barrier during reperfusion following an ischemic stroke. The ?-glutamyl antioxidants can be used alone or used in combination with an agent which inhibits the reverse movement of Na/Ca exchange in the blood-brain barrier such as 2-[2-[4-(4-nitrobenzyloxy)phenyl]ethyl]isothiourea methanesulphonate (KB-R7943).Type: GrantFiled: April 19, 2011Date of Patent: August 27, 2013Assignee: Rosalind Franklin University of Medicine and ScienceInventor: Darryl R Peterson
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Patent number: 8518874Abstract: The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: October 23, 2009Date of Patent: August 27, 2013Assignee: Virobay, Inc.Inventors: Michael Graupe, John O. Link, Chandrasekar Venkataramani
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Patent number: 8513196Abstract: The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.Type: GrantFiled: November 14, 2012Date of Patent: August 20, 2013Assignee: DMI Acquisition Corp.Inventors: David Bar-Or, Raphael Bar-Or, Richard Shimonkevitz
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Publication number: 20130210751Abstract: The present invention relates to improvements in compositions containing peptides that are ligands of the GHS receptor, or pharmaceutically acceptable salts thereof, methods for preparing such compositions, and methods of using such compositions to treat mammals. In particular, the present invention relates to a pharmaceutical composition comprising a pamoate salt of H-Inp-D-Bal-D-Trp-Phe-Apc-NH2, which is a ligand of the GHS receptor and in which, after subcutaneous or intramuscular administration to a subject, the peptide forms an in situ depot at physiological pH that is slowly dissolved and released into the body fluid and bloodstream. The present invention may further comprise an organic component such as dimethylacetamide (DMA) or polyethylene glycol with an average molecular weight of lower than 1000.Type: ApplicationFiled: March 14, 2011Publication date: August 15, 2013Applicant: IPSEN Pharma, S.A.S.Inventors: Zheng Xin Dong, Jundong Zhang
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Publication number: 20130209439Abstract: The present invention provides methods and materials for use in increasing HSP20 activation in a biological system, for example by increasing phosphorylation of Ser16 of HSP20. In one aspect, the invention provides a method for increasing HSP20 activation in a biological system, comprising contacting the system with an antagonist capable of inhibiting PDE4 binding to HSP20, the antagonist comprising or consisting essentially of a fragment of PDE4 or an analogue thereof. In a further aspect the invention provides a method of screening for an agent able to increase activation of HSP20. A preferred antagonist has a C-terminal lysine residue.Type: ApplicationFiled: October 7, 2011Publication date: August 15, 2013Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF GLASGOWInventors: George S. Baillie, Miles Houslay, Jon Day
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Patent number: 8507449Abstract: A process for making pure crystalline D-isoglutamyl-D-tryptophan is provided which includes the step of deprotecting essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan or its diester to yield essentially pure D-isoglutamyl-D-tryptophan. A process is also provided for the preparation of pure mono ammonium salt of D-isoglutamyl-D-tryptophan from essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan. D-isoglutamyl-D-tryptophan, ammonium salt (1:1) is a stable pharmaceutical solid.Type: GrantFiled: February 20, 2012Date of Patent: August 13, 2013Assignee: Apotex Technologies Inc.Inventors: Tim Fat Tam, Blaise N'Zemba, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Lily Yu
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Patent number: 8501697Abstract: A composition comprising a material at least partially enclosed by a tubular, spherical or planar nanostructure composed of a plurality of peptides, wherein each of the plurality of peptides includes no more than 4 amino acids and whereas at least one of the 4 amino acids is an aromatic amino acid.Type: GrantFiled: November 19, 2012Date of Patent: August 6, 2013Assignee: Ramot at Tel-Aviv University Ltd.Inventors: Ehud Gazit, Meital Reches
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Patent number: 8501240Abstract: The present invention provides a highly dispersible formulation comprising an active agent and a dipeptide or tripeptide comprising at least two leucyl residues. The composition of the invention possesses superior aerosol properties and is thus preferred for aerosolized administration to the lung. Also provided are a method for (i) increasing the dispersibility of an active-agent containing formulation for administration to the lung, and (ii) delivery of the composition to the lungs of a subject.Type: GrantFiled: December 23, 2008Date of Patent: August 6, 2013Assignee: Novartis AGInventors: Mei-chang Kuo, David Lechuga-Ballesteros
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Patent number: 8501685Abstract: A process for producing a peptide product having cholecystokinin secretion promoting effect, said process comprising hydrolyzing soybean residues with one or more proteases so that the peptide product having cholecystokinin secretion promoting effect is obtained. Also disclosed is the composition containing the peptide product and the use thereof.Type: GrantFiled: October 5, 2011Date of Patent: August 6, 2013Assignee: Food Industry Research and Development InstituteInventors: Yi-Hong Chen, Yu-Hui Liu, Chu-Chin Chen, Shiao-Cheng Chuang, Hsiang-Ling Lai, Chien-Ti Chang, Ming-Yu Hung, Su-Er Liou, Fu-Ning Chien
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Patent number: 8497237Abstract: The embodiments provide Compound KC-7, N-1-[(S)-2-(oxycodone-6-enol-carbonyl-methyl-amino)-2-carbonyl-sarcosine-ethyl amine]-arginine-glycine-acetate, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the \compositions comprise a prodrug, Compound KC-7, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.Type: GrantFiled: January 9, 2012Date of Patent: July 30, 2013Assignee: Signature Therapeutics, Inc.Inventors: Thomas E. Jenkins, Craig O. Husfeld
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Publication number: 20130184226Abstract: The present invention provides novel compounds of the Formula (1), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for modulating Protease Activated Receptor-2 (PAR2) and for treating a subject at risk of—or susceptible to—a disease or disorder, or having a disease or disorder associated with undesirable PAR2 activity.Type: ApplicationFiled: July 28, 2011Publication date: July 18, 2013Applicant: THE UNIVERSITY OF QUEENSLANDInventors: David Paul Fairlie, Ligong Liu, Mei Kwan Yau, Jacky Yung Suen
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Publication number: 20130184201Abstract: The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.Type: ApplicationFiled: March 6, 2013Publication date: July 18, 2013Applicants: Arizona State UniversityInventors: George R. Pettit, Rui Tan, Robin K. Pettit
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Patent number: 8481494Abstract: The present invention relates to the field of protein misfolding diseases and thus to diseases which are associated with or induced by abnormal or pathogenic three-dimensional folding of proteins and/or peptides or which are linked to pathogenic conformational changes of proteins and/or peptides, such as Alzheimer's disease. Particularly, the present invention provides novel trimeric pyrazole compounds, which exhibit a therapeutic effectiveness in regard to the aforementioned protein misfolding diseases, and refers to their use for the treatment of such protein misfolding diseases, especially neurodegenerative diseases as well as to medicaments or pharmaceutical compositions comprising these compounds.Type: GrantFiled: January 26, 2010Date of Patent: July 9, 2013Inventors: Thomas Schrader, Katrin Hochdörffer, Julia März-Berberich, Luitgard Nagel-Steger, Gal Bitan, Sharmistha Sinha
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Publication number: 20130171223Abstract: A pharmaceutical or cosmetic composition, comprising a substantially poorly water-soluble pharmaceutical active ingredient; and a nanoporous folic acid material, wherein the active pharmaceutical ingredient is incorporated inside the nanoporous channels of the particles.Type: ApplicationFiled: September 14, 2011Publication date: July 4, 2013Applicant: Nanologica ABInventors: Chunfang Zhou, Xin Xia, Alfonso E. Garcia-Bennett
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Publication number: 20130172232Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathType: ApplicationFiled: June 16, 2011Publication date: July 4, 2013Applicant: MEDIVIR UK LTDInventors: Susana Ayesa, Urszula Grabowska, Ellen Hewitt, Daniel Jonsson, Bjorn Klasson, Pia Kahnberg, Stina Lundgren, Jan Tejbrant, Daniel Wiktelius
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Publication number: 20130171127Abstract: The present invention relates to a pharmaceutical composition and a method for regenerating normal tissue from fibrotic tissue, the pharmaceutical composition and the method employing a collagen-reducing substance. In accordance with the present invention, normal tissue can be therapeutically regenerated from fibrotic tissue.Type: ApplicationFiled: March 7, 2013Publication date: July 4, 2013Applicant: NITTO DENKO CORPORATIONInventor: NITTO DENKO CORPORATION
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Publication number: 20130171209Abstract: Intraperitoneal administration of glutamine to reduce adhesions in the peritoneum of a patient.Type: ApplicationFiled: February 27, 2013Publication date: July 4, 2013Applicant: Ade Therapeutics Inc.Inventor: Ade Therapeutics Inc.
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Patent number: 8476240Abstract: The present disclosure relates to amyloid beta (A?) channels and the diseases and disorders caused by abnormal activity in these channels, such as Alzheimer's disease, Lewy body dementia, inclusion body myositis, or cerebral amyloid angiopathy. The disclosure provides compositions and methods that block A? channel activity and/or reduce A?-induced toxicity in a cell. Compositions comprised of compounds having histidine coordinating capacity are used in methods to prevent, reduce, or eliminate damage caused by A? ion channels.Type: GrantFiled: March 18, 2009Date of Patent: July 2, 2013Assignee: The Henry M. Jackson Foundation for The Advancement of Military Medicine, Inc.Inventor: Nelson Arispe
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Patent number: 8476235Abstract: A process for making pure crystalline D-isoglutamyl-D-tryptophan is provided which includes the step of deprotecting essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan or its diester to yield essentially pure D-isoglutamyl-D-tryptophan. A process is also provided for the preparation of pure mono ammonium salt of D-isoglutamyl-D-tryptophan from essentially pure N-tert-butoxycarbonyl-D-isoglutamyl-D-tryptophan. D-isoglutamyl-D-tryptophan, ammonium salt (1:1) is a stable pharmaceutical solid.Type: GrantFiled: February 20, 2012Date of Patent: July 2, 2013Assignee: Apotex Technologies Inc.Inventors: Tim Fat Tam, Blaise N'Zemba, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Lily Yu
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Patent number: 8466111Abstract: A cyclopenta[g]quinazoline derivative, containing an L-Glu-?-D-Glu dipeptide group, of formula (I): wherein R1 is amino, C1-4 hydroxyalkyl, C1-4 fluoroalkyl or methoxy-C1-4-alkyl; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl C2-4 halogenoalkyl or C1-4 cyanoalkyl; and Ar is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy, the compound (I) optionally being in the form of a pharmaceutically acceptable salt or ester; may be used for the treatment of rheumatoid arthritis or acute myeloid leukaemia.Type: GrantFiled: March 13, 2009Date of Patent: June 18, 2013Assignee: BTG International LimitedInventors: Gerrit Jansen, Ann Jackman
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Patent number: 8454978Abstract: An immunostimulating agent, which can stimulate immunity effectively, is described. The immunostimulating agent contains an active ingredient including a calcium receptor activator such as ?-Glu-X-Gly [wherein X represents an amino acid or a derivative thereof other than Cys], ?-Glu-Val-Y [wherein Y represents an amino acid or a derivative thereof], ?-Glu-Ala, ?-Glu-Gly, ?-Glu-Met, ?-Glu-Thr, ?-Glu-Val, ?-Glu-Orn, Asp-Gly, Cys-Gly, Cys-Met, Glu-Cys, Gly-Cys, Leu-Asp, ?-Glu-Met(O), ?-Glu-?-Glu-Val, ?-Glu-Val-NH2, ?-Glu-Val-ol, ?-Glu-Ser, ?-Glu-Tau, ?-Glu-Cys(S-Me)(O), ?-Glu-Leu, ?-Glu-Ile, ?-Glu-t-Leu, ?-Glu-Cys(S-Me), a cation having a valency of 2 or more, protamine, polylysine, spermine, spermidine, putrescine, cinacalcet, a cinacalcet analogue compound, and a salt of any one of the aforementioned components.Type: GrantFiled: October 6, 2010Date of Patent: June 4, 2013Assignee: Ajinomoto Co., Inc.Inventors: Tomohiro Kodera, Yuzuru Eto, Yoshinori Mine
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Patent number: 8450089Abstract: A method of preventing or inhibiting L-cystine crystallization using the compounds of formula I is disclosed. R1a—O-(-A-L-)m-A-O—R1b??I, wherein A, L, R1a, R1b, and m are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to L-cystine crystallization, such as comprising (but not limited to) kidney stones.Type: GrantFiled: November 23, 2010Date of Patent: May 28, 2013Assignee: New York UniversityInventors: Michael D. Ward, Jeffrey D. Rimer
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Patent number: 8445440Abstract: The present invention provides compounds of formula M-L-M? (where M and M? are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.Type: GrantFiled: February 23, 2011Date of Patent: May 21, 2013Assignee: Novartis AGInventors: Christopher Straub, Zhuoliang Chen, Mark Palermo
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Publication number: 20130116192Abstract: N-(aminoacyl)-amino compound, represented by the following formula Wherein R1 denotes hydrogen, low alkyl or carbonyl, and N1 denotes an NH group and R2 denotes hydrogen or low alkylphenyl or aralkyl or imidazoalkyl or indolylalkyl, R1 and R2 together may complete a pyrrolidine or piperidine or thiazolidine ring and R3 denotes hydrogen or methyl or low alkyl and R4 denotes hydrogen or alkyl or the group remaining on exclusion of R4 from the formula and Z is a straight chain or branched alkylene, which may contain up to 3 carbon atoms. and R5 is nitrogen or sulphur or oxygen or salts thereof and ester compounds, characterised in that A is an ester or amino acid or alternatively sodium or a potassium salt of arginate and/or of ornithate and/or of aspharaginate.Type: ApplicationFiled: March 30, 2011Publication date: May 9, 2013Inventor: Gosbert Weth
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Patent number: 8435955Abstract: By selecting one or more deodorizing agents from among glycine, cysteine and glycylglycine, and incorporating the selected deodorizing agent(s) and a surfactant, the toxicity of the surfactant to men and beasts is controlled without inhibiting the antibacterial actions that the surfactant has inherently. Glycine, cysteine, and glycylglycine each have a strong deodorizing action. The invention causes antibacterial deodorants to further have a deodorizing action by using such deodorizing agents. Moreover, the invention increases the permeating ability, thereby enhancing both the antibacterial action and the deodorizing action by subjecting water to treatment for fragmenting a cluster of the water and then adding the resulting active water as a diluent, or by preparing the diluent by incorporating alcohol with the active water.Type: GrantFiled: September 8, 2009Date of Patent: May 7, 2013Inventors: Yoshiharu Masui, Atsuko Tomida, Hideo Hirata, Koichi Otsuki