Tripeptides, E.g., Tripeptide Thyroliberin (trh), Melanostatin (mif), Etc. Patents (Class 530/331)
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Publication number: 20150065437Abstract: The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant.Type: ApplicationFiled: March 20, 2014Publication date: March 5, 2015Applicant: Stealth Peptides International, Inc.Inventors: Liping Liu, Lawrence Gu
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Publication number: 20150064143Abstract: The present invention provides an ionically cross-linkable alginate-grafted hyaluronate compound containing alginate and hyaluronate, the alginate and the hyaluronate forming a covalent linkage. The use of the compound can easily provide a cross-linked hyaluronate by adding a divalent cation without using a chemical cross-linking agent. The present invention also provides a method for cell transplantation that includes preparing a composition comprising the compound of claim 1 and cells for transplantation, and administering to a subject in need thereof the composition.Type: ApplicationFiled: September 3, 2014Publication date: March 5, 2015Inventors: Kuen Yong LEE, Hong Hyun PARK
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Publication number: 20150057218Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: November 3, 2014Publication date: February 26, 2015Inventors: Min ZHONG, Leping LI
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Publication number: 20150050212Abstract: Conjugates are described herein where CCK2R targeting ligands are attached to an active moiety, such as therapeutic agent or an imaging agent, through a linker. The conjugates can be used in the detection, diagnosis, imaging and treatment of cancer.Type: ApplicationFiled: February 22, 2013Publication date: February 19, 2015Inventors: Philip S. Low, Charity Wayua
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Publication number: 20150051160Abstract: The invention relates to novel tyrosine based linkers that allow the releasable connection of peptides or proteins with other molecular entities, e.g. polyethylene glycol, to processes for their preparation and their use for preparing medicaments for the treatment and/or prophylaxis of diseases.Type: ApplicationFiled: October 29, 2012Publication date: February 19, 2015Applicants: BAYER PHARMA AKTIENGESELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBHInventors: Ingo Flamme, Johannes Köbberling, Hans-Georg Lerchen, Nils Griebenow, Rudolf Schohe-Lop, Sven Wittrock, Ursula Krenz
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Publication number: 20150051154Abstract: The present invention relates to a novel class of alkylating agents comprising a thieno-indole moiety linked to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.Type: ApplicationFiled: March 28, 2013Publication date: February 19, 2015Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa, Achille Panzeri
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Patent number: 8957025Abstract: The present invention relates to dipeptide enkephalin analogues of Formula (I) and their tautomers, ionic forms and pharmaceutically acceptable salts, and their use in medicine, in particular as opioid agonists.Type: GrantFiled: June 29, 2012Date of Patent: February 17, 2015Assignee: Pfizer Inc.Inventor: Dafydd Rhys Owen
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Patent number: 8957030Abstract: The invention provides a method of reducing or preventing mitochondrial permeability transitioning. The method comprises administering an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (pm) and the total number of amino acid residues (r) wherein 3pm is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (pt) wherein 2 a is the largest number that is less than or equal to pt+1, except that when a is 1, pt may also be 1.Type: GrantFiled: February 27, 2013Date of Patent: February 17, 2015Assignees: Cornell Research Foundation, Inc., Institute de Recherches Cliniques de MontrealInventors: Hazel H. Szeto, Peter W. Schiller, Kesheng Zhao
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Publication number: 20150045282Abstract: Suppository, hot melt and ophthalmic formulations containing amino esters of the formulae (I), (II) and (III), where R1, R2 and R3 are residues of amino acids such as, but not limited to, valine, sarcosine, leucine, glutamine, tryptophan, tyrosine, alanine and 4(4-aminophenyl)butyric acid or combination thereof, and salts thereof.Type: ApplicationFiled: August 18, 2014Publication date: February 12, 2015Inventors: Mahmoud A. ELSOHLY, Waseem GUL, Michael A. REPKA, Soumyajit MAJUMDAR, Mohammad Khalid ASHFAQ
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Publication number: 20150037268Abstract: Provided is niacin-peptide which has skin whitening activity. The peptide of the present invention has skin whitening activity by inhibiting melanogenesis, that is, by inhibiting the expression of a gene related to melanogenesis (for example, TRP-1, TRP2, or MIFT). The peptide of the present invention has high stability and skin permeability. Also provided is a cosmetic composition for skin whitening which contains the niacin-peptide.Type: ApplicationFiled: August 22, 2012Publication date: February 5, 2015Inventors: Sung-Ae Choi, Hyuk-Kwang Jeong, Young-Mi Byoun, Jun-Seob Shin, Seo Joon Yoo, Sang-Chul Yoo
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Publication number: 20150031854Abstract: The invention relates to novel hemin derivatives of general formula (I), preparing and use thereof as antibacterial and/or antiviral agents, including, as a component in a pharmaceutical compositions. Advantages of the novel antibacterial and antiviral agents based on the hemin derivatives are in their biocompatibility, biodegradability, a high efficacy against resistant bacteria and widespread viruses which are dangerous to humans, and the lack of toxicity.Type: ApplicationFiled: November 15, 2012Publication date: January 29, 2015Applicant: OBSSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU "PHARMENTERPRISES"Inventors: Vladimir Evgenievich Nebolsin, Galina Alexandrovna Zheltukhina, Sergei Alexandrovich Okorochenkov
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Patent number: 8940697Abstract: The present invention provides a method of treating, ameliorating or preventing myocardial ischemia/reperfusion injury in a subject in need thereof, by administering to the subject a therapeutically effective amount of an annexin A1 short peptide (ANXA1sp).Type: GrantFiled: October 15, 2010Date of Patent: January 27, 2015Assignee: Duke UniversityInventors: Mihai V. Podgoreanu, Zhiquan Zhang, Qing Ma
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Publication number: 20150023874Abstract: The invention described herein pertains to targeted drug delivery conjugates comprising folate receptor ? (FR-?) selective binding ligands and methods for diagnosing, monitoring, and eliminating pathological cells that express FR-?.Type: ApplicationFiled: February 28, 2013Publication date: January 22, 2015Inventors: Philip Stewart Low, Balasubramanian Vaitilingam, Venkatesh Chelvam
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Patent number: 8936781Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: April 13, 2010Date of Patent: January 20, 2015Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yonghua Gai, Yat Sun Or, Guoqiang Wang
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Publication number: 20150017192Abstract: The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.Type: ApplicationFiled: July 11, 2014Publication date: January 15, 2015Inventors: Aimee Usera, Zachary Robinson, Jennifer Cobb
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Publication number: 20150011730Abstract: Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.Type: ApplicationFiled: September 22, 2014Publication date: January 8, 2015Inventors: Campbell McInnes, Shu Liu
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Publication number: 20150011458Abstract: The present invention relates to compounds of Formula I, IA, II, HA, III, or IHA and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, IA, II, IIA, III, or IIIA are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases).Type: ApplicationFiled: June 17, 2014Publication date: January 8, 2015Inventors: Jan-Eric Ahlfors, Khalid Mekouar
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Publication number: 20150011003Abstract: A medium which comprises a fibroblast growth factor (FGF), and a sulfated compound or a pharmaceutically acceptable salt thereof at a concentration which promotes the growth of a stem cell in the presence of FGF, is useful for culturing stem cells.Type: ApplicationFiled: September 26, 2014Publication date: January 8, 2015Applicant: AJINOMOTO CO., INC.Inventors: Yoko KURIYAMA, Nao SUGIMOTO, Manabu KITAZAWA, Satoru OKAMOTO, Sho SENDA, Ikue HARATA, Satoru OHASHI
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Patent number: 8927503Abstract: 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: GrantFiled: July 28, 2011Date of Patent: January 6, 2015Assignee: The University of QueenslandInventors: David Paul Fairlie, Ligong Liu, Mei Kwan Yau, Jacky Yung Suen, Robert Reid
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Publication number: 20150004698Abstract: Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.Type: ApplicationFiled: August 29, 2014Publication date: January 1, 2015Applicants: YALE UNIVERSITY, UNIVERSITY OF SOUTH FLORIDAInventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
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Publication number: 20150005239Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.Type: ApplicationFiled: June 11, 2014Publication date: January 1, 2015Inventors: Pablo VILLOSLADA, Angel Messeguer
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Publication number: 20140377178Abstract: The present invention relates to a method of labelling biological molecules with 18F, via attachment to fluorine to a macrocyclic metal complex of a non-radioactive metal, where the metal complex is conjugated to the biological molecule. Also provided are pharmaceutical compositions, kits and methods of in vivo imaging.Type: ApplicationFiled: January 22, 2013Publication date: December 25, 2014Applicants: UNIVERSITY OF SOUTHAMPTON, GE HEALTHCARE LIMITEDInventors: Rajiv Bhalla, Sajinder Kaur Luthra, Gill Reid, I, William Levason
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Publication number: 20140378396Abstract: The present disclosure provides aromatic-cationic peptide compositions and methods of using the same. The methods comprise use of the peptides in electron transport, inhibition of cardiolipin peroxidation, apoptosis inhibition and electrical conductance.Type: ApplicationFiled: October 11, 2012Publication date: December 25, 2014Inventors: D. Travis Wilson, Hazel Szeto, Alex Birk
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Publication number: 20140364586Abstract: Reagents and methods for functionalizing polypeptides with moieties (alkylene glycol) molecules and glycan groups are disclosed that are based on a functionalizing reagent which comprises a nitrogen containing heterocyclic aromatic ring having a vinyl substituent that is capable of reacting with one or more thiol groups that are naturally present, or have been introduced into, the polypeptide, for example by employing a thiol group of one or more cysteine residues. The functionalizing reagent is covalently linked to a poly(alkylene glycol) molecule, such as a polyethylene glycol (PEG) molecule, or a glycan group so that the reaction between the vinyl group and the thiol group in the polypeptide covalently links the polypeptide to the poly(alkylene glycol) molecule and/or the glycan group.Type: ApplicationFiled: June 26, 2014Publication date: December 11, 2014Inventors: Andrew Graham WATTS, Terrence Kantner, Amanda Barbara MacKenzie
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Publication number: 20140364585Abstract: An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates.Type: ApplicationFiled: August 28, 2014Publication date: December 11, 2014Inventors: Qian ZHANG, Sanjeev Gangwar, Chin Pan, Daniel W. Derwin
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Publication number: 20140357551Abstract: The present application describes organic compounds of Formula (II) that are useful for the treatment, prevention and/or amelioration of human diseases.Type: ApplicationFiled: August 18, 2014Publication date: December 4, 2014Applicant: Novartis AGInventors: Trixi Brandl, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
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Publication number: 20140356319Abstract: The present invention describes peptides comprising phycocyanobilin (PCB), as well as the medical use of said peptides and that of PCB, due to the neuroprotector and/or neuroregenerative effects identified for them. Furthermore, pharmaceutical combinations of said peptides and of PCB with proteins or other peptides with synergic effect justify their use for ischemic or neurodegenerative CNS disease treatment.Type: ApplicationFiled: June 29, 2012Publication date: December 4, 2014Applicant: CENTRO DE INGENIERÍA GENÉTICA Y BIOTECNOLOGÍAInventors: Giselle Penton Rol, Alexey Llopiz Arzuaga, Javier Marin Prida, Eduardo Pentón Arias, Efraín Rodríguez Jiménez, Alexis Musacchio Lasa, Vladimir Armando Besada Perez, Gilberto Lázaro Pardo Andreu, Luis Javier González López, Nancy Pavón Fuentes, Gerardo Enrique Guillen Nieto, Pedro Antonio López Saura
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Publication number: 20140356322Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.Type: ApplicationFiled: January 11, 2013Publication date: December 4, 2014Inventors: Craig M. Crews, Dennis Buckley, Alessio Ciulli, William Jorgensen, Peter C. Gareiss, Inge Van Molle, Jeffrey Gustafson, Hyun-Seop Tae, Julien Michel, Dentin Wade Hoyer, Anke G. Roth, John David Harling, Ian Edward David Smith, Afjal Hussain Miah, Sebastien Andre Campos, Joelle Le
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Patent number: 8901085Abstract: 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: GrantFiled: July 28, 2011Date of Patent: December 2, 2014Assignee: The University of QueenslandInventors: David Paul Fairlie, Ligong Liu, Mei Kwan Yau, Jacky Yung Suen, Robert Reid
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Patent number: 8895515Abstract: The present invention relates to a cosmetic composition which mimics the extracellular matrix to stimulate the regeneration of skin cells, and more particularly to a cosmetic composition which contains active ingredients consisting of low-molecular-weight materials, which easily permeate through the skin, at a composition ratio similar to that in the extracellular matrix. The cosmetic composition stimulates the repair of the skin to maintain homeostasis and is effective for the regeneration of skin cells.Type: GrantFiled: November 29, 2010Date of Patent: November 25, 2014Assignee: Amorepacific CorporationInventors: Mi Jin Kim, Jong Won Shim, Yong Jin Kim, Eun Jung An, Chan Woo Lee, Soo Jin Lee, Jin Woong Kim
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Publication number: 20140341804Abstract: The present invention provides bivalent and multivalent ligands with a view to improving the affinity and pharmacokinetic properties of a urea class of PSMA inhibitors. The compounds and their synthesis can be generalized to multivalent compounds of other target antigens. Because they present multiple copies of the pharmacophore, multivalent ligands can bind to receptors with high avidity and affinity, thereby serving as powerful inhibitors. The modular multivalent scaffolds of the present invention, in one or more embodiments, contains a lysine-based (?-, ?-)dialkyne residue for incorporating two or more antigen binding moieties, such as PSMA binding Lys-Glu urea moieties, exploiting click chemistry and one or more additional lysine residues for subsequent modification with an imaging and/or therapeutic nuclides or a cytotoxic ligands for tumor cell killing.Type: ApplicationFiled: November 30, 2012Publication date: November 20, 2014Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Martin Gilbert Pomper, Sangeeta Ray, Ronnie C. Mease
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Patent number: 8889828Abstract: A series of peptides with divergent confirmations including structures of formula (1A), (1B), (2) and (3) are provided. In the formula, wherein U, G, A, B, R1, R2 and T are as defined in the specification. The divergent peptides disclosed in the present invention are characterized in a mineral binding affinity function.Type: GrantFiled: October 21, 2011Date of Patent: November 18, 2014Assignee: Kaohsiung Medical UniversityInventors: Hui-Ting Chen, Kuang-Chan Hsieh, Je-Ken Chang, Gwo-Jaw Wang, Yin-Chih Fu, Mei-Ling Ho, Cherng-Chyi Tzeng
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Publication number: 20140336115Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of diseases through inhibiting the activity of the transforming growth factor beta (TGF-?). More specifically, the disclosed compounds, compositions and methods are useful in the treatment of certain cancers (e.g. multiple myeloma, hematologic malignancies), diseases associated with excessive TGF-? activity including fibrosis, dermal scarring, immune dysfunction, and bone loss by inhibiting the conversion of latent TGF-? to active TGF-?. A method of preventing the activation of TGF-? in pathology is also provided, comprising administering an amount of the compounds sufficient to inhibit conversion of latent TGF-? to active TGF-? by thrombospondinl (TSP1), resulting in reduced TGF-? activity and reduced adverse effects such as fibrosis, bone loss, and immune dysfunction.Type: ApplicationFiled: May 9, 2014Publication date: November 13, 2014Applicants: Southern Research Institute, THE UAB RESEARCH FOUNDATIONInventors: Mark J. Suto, Joanne E. Murphy-Ullrich
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Publication number: 20140336106Abstract: Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.Type: ApplicationFiled: March 14, 2014Publication date: November 13, 2014Applicant: Onyx Therapeutics, Inc.Inventors: Dustin McMinn, Henry Johnson, Simeon Bowers, David C. Moebius
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Publication number: 20140329990Abstract: The present invention provides, among other things, polymeric reagents suitable for reaction with biologically active agents to form conjugates, the polymeric reagents comprising one or more polymer chains and a plurality of hydroxyapatite-targeting moieties, and optionally the reagents include one or more degradable linkages that serve to divide the polymer chains into polymer segments having a molecular weight suitable for renal clearance.Type: ApplicationFiled: July 18, 2014Publication date: November 6, 2014Applicant: Nektar TherapeuticsInventors: Samuel P. McManus, Antoni Kozlowski
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Publication number: 20140329775Abstract: Disclosed herein are compositions and methods for generating ribo-nucleic neutral (RNN) or deoxyribo-nucleic-neutral (DNN) polynucleotides with reduced anionic charge, for improved intracellular delivery. Also disclosed herein are methods of using RNN and DNN compositions.Type: ApplicationFiled: February 17, 2014Publication date: November 6, 2014Inventor: Scott G. Petersen
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Publication number: 20140323394Abstract: The present invention is related to the tripeptide (I)Lys-(d)Pro-(I)Thr (KdPT) or pharmaceutically acceptable salts thereof for therapeutic, prophylactic therapeutic or cosmetic treatment of a disease with increased apoptosis, wherein the treatment has an anti-apoptotic effect. The present invention is also related to the use of KdPT or pharmaceutically acceptable salts thereof for the manufacture of a pharmaceutical or cosmetic composition for an anti-apoptotic treatment of disorders that are related with increased apoptosis.Type: ApplicationFiled: September 24, 2012Publication date: October 30, 2014Applicant: WESTFAELISCHE WILHELMS-UNIVERSITAET MUENSTERInventors: Dominik Bettenworth, Markus Boehm, Andreas Luegering
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Publication number: 20140323690Abstract: Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:Type: ApplicationFiled: July 7, 2014Publication date: October 30, 2014Inventors: Heng Cheng, Sanjeev Gangwar, Qiang Cong
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Publication number: 20140325712Abstract: In order to develop a technique for increasing an amino acid content and to provide a technique for easily producing a plant having an increased amino acid content, an amino acid content in a plant is increased by an amino acid content promoting agent, a composition containing the amino acid content promoting agent, a kit including an amino acid content promoting agent, or a kit including a composition containing the amino acid content promoting agent, and a plant having an increased amino acid content is produced.Type: ApplicationFiled: November 28, 2012Publication date: October 30, 2014Inventors: Kenichi Ogawa, Kenji Henmi, Aya Iwasaki
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Publication number: 20140315785Abstract: The invention includes methods of neuroprotection, inducing release of neurotrophic factors, inhibiting the over-activation of innate immune cells, attenuating the toxin-induced death and/or damage of tissues, reducing inflammation, treating an inflammation-related condition, and inhibiting NADPH oxidase, that includes contacting or administering an effective amount of at least one compound of the invention that include: valproic acid, sodium butyrate, and salts thereof; opioid peptides; a peptide comprising the tripeptide GGF; and morphinans, such as naloxone, naltrexone, 3-hydroxy-morphinan and dextromethorphan.Type: ApplicationFiled: July 3, 2014Publication date: October 23, 2014Inventors: Jau-Shyong Hong, Liya Qin, Guorong Li, Michelle Block, Wei Zhang, Po-See Chen, Giia-Shuen Peng
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Publication number: 20140315185Abstract: Methods for improving the functionality and/or fertility of sperm, for example, by enhancing motility and extending the lifespan of sperm in the FRT, by adding functional molecules of interest attached to a membrane anchoring agent-PEG conjugate to the surface of the sperm are provided. Such methods may be used in AI to reduce the number of sperm needed for insemination and to improve conception rates.Type: ApplicationFiled: August 8, 2012Publication date: October 23, 2014Applicant: ANDROGENIX LTD.Inventors: Bridget Lee Dicker, Jiwon Hong, Keith Hudson, Shakeela Nathalia Jayasinghe
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Publication number: 20140315831Abstract: The present disclosure is directed to a novel class of peptide-like oligomers called peptide tertiary amides (PTAs) and a combinatorial library of PTAs along with synthetic routes for the preparation of large combinatorial libraries of these compounds. The peptide tertiary amides provide an exceptional source of high affinity and selective protein ligands that are useful as tools for biological research and as drug leads, among others.Type: ApplicationFiled: October 25, 2012Publication date: October 23, 2014Inventors: Thomas Kodadek, Yu Gao
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Patent number: 8865857Abstract: A medical device includes a substrate having at least a portion thereof functionalized with at least one reactive member and a chemotactic agent functionalized with at least one complementary reactive member. The at least one reactive member and the at least one complementary reactive member are covalently bonded, adhering the chemotactic agent to the substrate.Type: GrantFiled: June 30, 2011Date of Patent: October 21, 2014Assignee: Sofradim ProductionInventors: Sébastien Ladet, Philippe Gravagna
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Publication number: 20140309401Abstract: A DPP-4 inhibitor comprising a peptide represented by the formula (1): Xe-Pro/Ala/Hyp-Xa-Xb-Xc-Xd (wherein Xe is an amino acid residue with an isoelectric point of 5.9 to 6.3; Pro/Ala/Hyp represents Pro, Ala, or Hyp; Xa is an amino acid residue other than Hyp, Pro, and Arg, or deletion; Xb is Gly, Pro, or deletion; Xc is Pro, Ala, or deletion; and Xd is an amino acid residue or deletion) as an active component. The inhibitor can be expected to bring out an effect of lowering blood glucose levels by enhancing effects of incretins; and the inhibitor may be used as a therapeutic agent for diabetes and, in addition, can act on the immune system or the like to be thus used in treatment for skin diseases or the like.Type: ApplicationFiled: November 2, 2012Publication date: October 16, 2014Inventors: Osamu Hayashida, Masashi Kusubata, Yuji Atsuzawa, Yuki Taga, Youichi Koyama, Shunji Hattori
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Publication number: 20140309174Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.Type: ApplicationFiled: November 12, 2013Publication date: October 16, 2014Applicant: Eisai Co., LtdInventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
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Patent number: 8859505Abstract: 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 caType: GrantFiled: June 16, 2011Date of Patent: October 14, 2014Assignee: 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: 20140303095Abstract: Novel peptidomimetics exhibiting affinity for opioid receptors, possessing general formula show on FIG. 1, for gastrointestinal or peripheral administration in the form of a pill, infusion, injection or implant in the treatment of peripheral opioids side effects, particularly constipation or/and respiratory depression.Type: ApplicationFiled: December 28, 2012Publication date: October 9, 2014Applicant: Instytut Medycyny Doswiadczalnej i Klinicznej im. Miroslawa Mossakowskiego Polskiej Akademii NaukInventor: Andrzej Lipkowski
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Publication number: 20140303082Abstract: In the past decade a great deal of structural information for class A-GPCRs (G protein-coupled receptors) has emerged. However, the structural and electronic basis of ligand selectivity for closely related receptor subtypes such as the angiotensin receptors AT1aR and AT2R, which present completely diverse biological functions in response to the same ligand, is poorly understood. In order to monitor complex responses in biosystems it is useful to have ligands that present a gradient in terms of selectivity. In this study we present an efficient method to tune ligand selectivity for the two angiotensin II receptor subtypes, AT1aR and AT2R, by controlling aromatic-prolyl interactions in angiotensin II, through alternation of aromatic electronics. On the basis of this strategy, an AT2R selective and high affinity agonist analogue (Ki=3 nM) was obtained.Type: ApplicationFiled: June 20, 2014Publication date: October 9, 2014Inventor: Andreas Tzakos
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Publication number: 20140302066Abstract: This invention relates to pyrrolobenzodiazepines (PBDs), in particular pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position in each monomer unit, and their inclusion in targeted conjugates. The differing substituent groups may offer advantages in the preparation and use of the compounds, particularly in their biological properties and the synthesis of conjugates, and the biological properties of these conjugates.Type: ApplicationFiled: October 12, 2012Publication date: October 9, 2014Inventors: Scott Jeffrey, Patrick Burke, Philip Wilson Howard
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Publication number: 20140303344Abstract: The invention relates to a process for the stereoselective preparation of amino acid derivatives, comprising a hydrogenation reaction of the compound of formula (III), alternatively its enantiomer, wherein R is (C1-C8)-alkyl; followed by a hydrolysis reaction to obtain L-mesityl alanine, alternatively its enantiomer D-mesityl alanine and, optionally, subjecting said compound to an amino group protection reaction, particularly as Fmoc. It also comprises Fmoc-L- or Fmoc-D- mesityl alanine as products per se, useful as intermediates in preparing peptides or peptide analogs with therapeutic or biological activity.Type: ApplicationFiled: March 12, 2014Publication date: October 9, 2014Applicant: BCN PÉPTIDES, S.A.Inventors: Llorenç RAFECAS JANE, Antoni RIERA ESCALE, Rosario RAMON ALBALATE, Monica ALONSO XALMA