Tripeptides, E.g., Tripeptide Thyroliberin (trh), Melanostatin (mif), Etc. Patents (Class 530/331)
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Patent number: 11596693Abstract: Provided is an antibody-drug conjugate (ADC) using one or more cysteine or derivatives thereof as linkers to couple one or more drugs at the limited binding sites of an antibody, making it possible to produce an ADC product with high drug payload, or to choose a drug with less toxicity, thereby obtaining an ADC product with wide therapeutic window. In addition, since a plurality of drugs may be coupled to one binding site, the ADC products obtained by the method of the present disclosure have better uniformity in the case of same DAR value. Moreover, the amount of antibody required for production may be greatly reduced, thereby lowering the cost. Compared with the antibody-drug conjugates coupled only one drug, the antibody-drug conjugates produced by the method of the present disclosure have the same inhibition or killing effect on tumor cells while using fewer drugs for coupling to the same site.Type: GrantFiled: October 23, 2019Date of Patent: March 7, 2023Assignee: MABPLEX INTERNATIONAL CO., LTDInventors: Lele Li, Changjiang Huang, Youxiang Sun, Lina Liu
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Patent number: 11407787Abstract: The present application discloses a crystal of oxidized glutathione dication salt and a method of producing the same.Type: GrantFiled: June 6, 2018Date of Patent: August 9, 2022Assignee: KYOWA HAKKO BIO CO., LTD.Inventors: Akihiro Fujimoto, Kazunari Fukumoto, Hiroshi Nagano
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Patent number: 11311540Abstract: Provided herein is a combination comprising an HDAC inhibitor and an IMiD for increasing interferon regulated gene expression or decreasing c-MYC gene expression in a cancer cell or tumor in a subject in need thereof. Increasing interferon regulated gene expression may result in increased recognition of tumors by innate or adaptive immune system and an increase in programmed cell death (apoptosis) gene expression, increasing apoptosis in cancer cells and tumors. The cells can be multiple myeloma cells or diffuse large B-cell lymphoma cells. Also provided are methods for treating myelodysplastic syndromes/acute myeloid leukemia (MDS/AML) or pathogen infections in a subject in need thereof comprising administering to the subject an effective amount of HDAC inhibitor and an IMiD. The HDAC inhibitor can be an HDAC6-selective inhibitor.Type: GrantFiled: February 17, 2017Date of Patent: April 26, 2022Assignee: ACETYLON PHARMACEUTICALS, INC.Inventors: Steven Norman Quayle, Jeffrey R. Shearstone
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Patent number: 11274124Abstract: In one aspect, the present disclosure provides tubulysin analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.Type: GrantFiled: November 28, 2018Date of Patent: March 15, 2022Assignee: William Marsh Rice UniversityInventors: Kyriacos C. Nicolaou, Rohan Diliprao Erande, Dionisios Vourloumis, Kiran Kumar Pulukuri, Stephan Rigol
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Patent number: 11186610Abstract: The present invention relates to a crystal of glutathione trisulfide dihydrate and a method for producing the same. According to the present invention, for example, the crystal can be provided by concentrating an aqueous solution in which glutathione trisulfide is dissolved and collecting the precipitated crystal of glutathione trisulfide dihydrate. In addition, the present invention relates to a simple method for producing polysulfide in an aqueous solvent using thiosulfate without using hydrogen sulfide, by stirring an aqueous solution in which a compound having a thiol group or a disulfide bond and thiosulfate are dissolved or by leaving the aqueous solution to stand.Type: GrantFiled: December 20, 2017Date of Patent: November 30, 2021Assignee: KYOWA HAKKO BIO CO., LTD.Inventors: Akihiro Fujimoto, Hiroshi Nagano
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Patent number: 11001820Abstract: Methods of delivering therapeutic agents by administering compositions including a bacterial collagen-binding polypeptide segment linked to the therapeutic agent to subjects in need of treatment with the therapeutic agent are provided. In these methods, the therapeutic agent is not a PTH/PTHrP receptor agonist or antagonist, basic fibroblast growth factor (bFGF) or epidermal growth factor (EGF). The bacterial collagen-binding polypeptide segment delivers the agent to sites of partially untwisted or under-twisted collagen. Methods of treating collagenopathies using a composition including a collagen-binding polypeptide and a PTH/PTHrP receptor agonist are also provided. In addition, methods of treating hyperparathyroidism, and hair loss using compositions comprising a collagen binding polypeptide and a PTH/PTHrP receptor agonist are provided. Finally, methods of reducing hair regrowth by administering a composition including a collagen binding polypeptide and a PTH/PTHrP receptor antagonist are provided.Type: GrantFiled: January 17, 2017Date of Patent: May 11, 2021Assignees: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ARKANSAS, MONTEFIORE MEDICAL CENTERInventors: Tulasi Ponnapakkam, Sagaya Theresa Leena Philominathan, Joshua Sakon, Ranjitha Katikaneni, Takaki Koide, Osamu Matsushita, Robert C. Gensure, Nozomu Nishi
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Patent number: 10668000Abstract: The peptides have the general following formula: X-Pro*-Pro*-Xaa-Y in which: •Xaa is selected from Leucine (Leu, L), Arginine (Arg, R), Lysine (Lys, K), Alanine (Ala, A), Serine (Ser, S), and Aspartic acid (Asp, D); •At the N terminal end of the peptide, X is selected from H, —CO—R1 and —SO2—R1; •At the C terminal end of the peptide, Y is selected from OH, OR1, NH2, NHR1 and NR1R2; •R1 and R2 are, independently from each other, selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group, that can be linear, branched, cyclic, poly-cyclic, non-saturated, hydroxylated, carbonylated, phosphorylated and/or sulfured, and which skeletum can comprise an heteroatom, in particular an O, S and/or N atom; •Pro* correspond to a Proline, an analogue or derivative thereof; •if X is H then Y is selected from OR1, NH2, NHR1 and NR1R2, and if Y is OH then X is —CO— or —SO2—R1; and the peptide hypoxanthine-Pro-Pro-Arg being excluded.Type: GrantFiled: May 21, 2015Date of Patent: June 2, 2020Assignee: SEDERMAInventors: Olivier Peschard, Anne Doucet, Richard Leroux, Philippe Mondon
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Patent number: 10617656Abstract: A method of treating cancer in a subject in need thereof, comprising administering to the subject a first amount of a compound of the HAT inhibitor of the following formula: wherein R is chosen from coenzyme A, (CH2)2NHCO(CH2)2NHCOR2; (CH2)2NHCOR3; (CH2)2NHCO(CH2)2NHCOR4; R1 is H, NH2, NH, N, and R1 can optionally cyclize with at least one other X2 to form a C3-8 membered ring containing C, O, S, or N; R2 is chosen from alkyl, cycloalkyl, aryl, heteroaryl; R3 is chosen from an alkyl, cycloalkyl, aryl, heteroaryl; R4 is chosen from CH(OH)C(CH3)2CH2)OCOR2; X1 is chosen from H or can cyclize with one other X2 or R1 to form a C3-8 membered ring containing C, O, S, or N; and X2 is chosen from C, N, NH, and can optionally cyclize with at least one other X2 or R1 to form a C3-8 membered ring containing C, O, S, or N; or a pharmaceutically acceptable salt or hydrate thereof, thereby treating the cancer.Type: GrantFiled: August 18, 2015Date of Patent: April 14, 2020Assignee: Vanderbilt UniversityInventors: Joseph Parello, Ruth Anne Gjierset, Paul R. Reid
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Patent number: 10597383Abstract: The invention is concerned with the compounds of formula I: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.Type: GrantFiled: January 17, 2019Date of Patent: March 24, 2020Assignee: Genentech, Inc.Inventors: Vishal Verma, Daniel Shore, Matthew Volgraf, Anthony A. Estrada, Joseph Lyssikatos
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Patent number: 10556895Abstract: This invention relates to quaternary amine linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.Type: GrantFiled: May 1, 2017Date of Patent: February 11, 2020Assignee: Genentech, Inc.Inventors: John A. Flygare, Thomas Pillow, Leanna Staben
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Patent number: 10351591Abstract: Some embodiments of the invention involve methods for introduction of various functional groups onto polypeptides, peptides and proteins by alkylation of thioether (a.k.a. sulfide) groups by ring opening reactions, creating new compositions of matter that may be useful for medical therapeutic or diagnostic applications. The thioether groups may either be present in the polypeptides, or may be added to polypeptides by chemical modification, such as by alkylation of thiol (sulfhydryl) groups.Type: GrantFiled: March 21, 2016Date of Patent: July 16, 2019Assignee: The Regents of the University of CaliforniaInventors: Timothy J. Deming, Eric G. Gharakhanian
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Patent number: 10342792Abstract: Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a ?-elimination mechanism.Type: GrantFiled: June 14, 2018Date of Patent: July 9, 2019Assignee: ProLynx LLCInventors: Gary W. Ashley, Eric L. Schneider
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Patent number: 10238771Abstract: Methods for treating a bioprosthetic tissue are described herein. The methods comprise contacting the bioprosthetic tissue with at least one nucleophile and/or at least one electrophile in the presence of a catalytic system comprising at least one or a combination of a fluoride-based salt, a cesium-based salt, a potassium-based salt, a rubidium-based salt, or a carbonate-based salt. The methods may be used to alter functional groups on biological tissue which represent actual and potential calcium binding sites and also processes for cross-linking bioprosthetic tissue. Both processes may be used in conjunction with known fixative techniques, such as glutaraldehyde fixation, or may be used to replace known fixative techniques.Type: GrantFiled: November 7, 2013Date of Patent: March 26, 2019Assignee: Edwards Lifesciences CorporationInventors: Dengfeng Xu, Jeffrey S. Dove
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Patent number: 10231917Abstract: The invention is directed to the use of at least one peptide of formula: X—(Xaa1)n-Pro*-(Xaa2)m-Y (I) With: —n=0, 1 or 2; —m=0 or 1 and if m=0 then n?0-Xaai is: —An hydrophobic amino acid; —A polar amino acid; —or Glycine (Gly, G); When n=2 the two amino acids Xaa1 can be the same or different; —Xaa2 is: —An hydrophobic amino acid; —A basic amino acid Glycine (Gly, G) or Serine (Ser, S); —At the N terminal end of the peptide, X is selected from H, —CO—R1 and —SO2—R1; —At the C terminal end of the peptide, Y is selected from OH, OR1, NH2, NHR1 or NR1R2, R1 and R2 being independently from each other, selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group; Excluding the peptides where X=H and Y=OH, for a non therapeutical cosmetic pro-pigmenting treatment of skin.Type: GrantFiled: November 28, 2016Date of Patent: March 19, 2019Assignee: SedermaInventors: Olivier Peschard, Philippe Mondon
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Patent number: 10072043Abstract: Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.Type: GrantFiled: December 18, 2015Date of Patent: September 11, 2018Assignee: Indiana University Research and Technology CorporationInventors: Zhong-Yin Zhang, Sheng Zhang
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Patent number: 9562069Abstract: 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: GrantFiled: June 17, 2014Date of Patent: February 7, 2017Inventors: Jan-Eric Ahlfors, Khalid Mekouar
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Patent number: 9540346Abstract: The disclosure provides crystalline Sovaprevir forms. The crystalline forms of Sovaprevir comprise a Form A polymorph, a Form B polymorph, a Form C polymorph, a Form D polymorph, and a Form E polymorph. The Form A, B, C, D, and E polymorphs exhibit X-ray powder diffraction patterns having peak locations in accordance with FIGS. 1, 4, 7, 10, and 13, respectively.Type: GrantFiled: November 25, 2015Date of Patent: January 10, 2017Assignee: ACHILLION PHARMACEUTICALS, INC.Inventor: Avinash Phadke
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Patent number: 9482673Abstract: The present invention relates to a chromogenic method for simultaneously determining the activity of multiple coagulation proteases or for simultaneously determining the inhibition of multiple coagulation proteases in a single test reaction. For this purpose, use is made of two chromogenic substrates which have different absorption maxima and whose color signals can be separated spectrally.Type: GrantFiled: January 5, 2015Date of Patent: November 1, 2016Assignee: SIEMENS HEALTHCARE DIAGNOSTICS PRODUCTS GMBHInventor: Norbert Zander
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Patent number: 9421237Abstract: The present invention discloses proteasome inhibitors of tripeptide boronic acids or boronic esters represented by Formula (I), preparative method and use thereof. The proteasome inhibitors are therapeutical agents for treating malignant tumor, various nervous system degenerative diseases, muscle cachexia or diabetes, wherein the malignant tumor is leukemia, gastric cancer, hepatocarcinoma or nasopharyngeal carcinoma.Type: GrantFiled: May 17, 2010Date of Patent: August 23, 2016Assignee: PEKING UNIVERSITYInventors: Runtao Li, Jingrong Cui, Yongqiang Zhu, Shuyang Yao, Zemei Ge, Tieming Cheng
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Patent number: 9353147Abstract: The present invention provides a production method of peptide, which includes the following step (1). (1) removing N-terminal Fmoc group of N-Fmoc C-protected amino acid or N-Fmoc C-protected peptide wherein a C-terminal carboxy group is protected by an anchor group derived from an anchor soluble in halogenated solvents or ether solvents, insoluble in polar solvents and having a molecular weight of not less than 300, with a non-nucleophilic organic base in a halogenated solvent or ether solvent to give a C-protected amino acid or C-protected peptide, neutralizing with an acid, adding N-Fmoc amino acid or N-Fmoc peptide, a condensing agent and a condensation accelerator to the reaction solution after neutralization, and condensing the N-terminal of the C-protected amino acid or C-protected peptide with N-Fmoc amino acid or N-Fmoc peptide to give an N-Fmoc C-protected peptide.Type: GrantFiled: November 26, 2013Date of Patent: May 31, 2016Assignee: AJINOMOTO CO., INC.Inventor: Daisuke Takahashi
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Patent number: 9226974Abstract: 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: GrantFiled: July 7, 2014Date of Patent: January 5, 2016Assignee: E. R. SQUIBB & SONS, L.L.C.Inventors: Heng Cheng, Sanjeev Gangwar, Qiang Cong
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Patent number: 9227995Abstract: A peptide which can adopt a 310-helical conformation in which the side chains of two amino acid residues in the peptide backbone are linked by a group comprising an aromatic 5-membered ring.Type: GrantFiled: April 22, 2011Date of Patent: January 5, 2016Assignees: DRUG DISCOVERY LABORATORY ASInventors: Øyvind Jacobsen, Pål Rongved, Jo Klaveness
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Patent number: 9133501Abstract: The present invention relates to a method for detecting at least one direct factor Xa inhibitor in a sample other than citrate plasma, comprising the step of mixing a sample containing a factor Xa inhibitor with a composition containing factor Xa under conditions which allow the factor Xa to release a detectable substance from a chromogenic substrate.Type: GrantFiled: November 7, 2011Date of Patent: September 15, 2015Assignee: Ruprecht-Karls-Universität HeidelbergInventors: Job Harenberg, Roland Krämer
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Publication number: 20150140139Abstract: The present invention relates to a composition for improving or promoting hair growth, which contains, as an active ingredient, a photosensitizer-peptide conjugate, and to a method for screening for the hair growth promoter using the active ingredients. ALA, which is the photosensitizer of the present invention, is preferably activated by LED radiation, and more preferably activated by radiation having a long wavelength of 650 to 675 nm. The peptide of the present invention is a peptide in which 3 to 7 amino acid residues are incorporated (most preferably, glycine-histidine-lysine), and may cooperate with the photosensitizer to enable very superior hair growth improving or promoting effects using light radiation. Further, the composition of the present invention may exhibit further superior effects when natural extracts (for example, Cimicifuga heracleifolia extracts, Scutellaria baicalensis extracts or Codonopsis lanceolata extracts) are added.Type: ApplicationFiled: May 8, 2013Publication date: May 21, 2015Inventors: Darren Williams, Da-Won Jung, Soon-Ho Yim
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Publication number: 20150132440Abstract: A composition of dipeptides or tripeptides or ester derivatives may be used as a nutritional supplement and to modulate expression of genes associated with healthy maintenance and regulation of muscular and neurological tissue. The compositions include dipeptides and/or tripeptides of branched chain amino acids and optionally include adjuvants, anti-aging compounds and may be provided in a dissolvable powder or liquid form.Type: ApplicationFiled: August 13, 2014Publication date: May 14, 2015Inventor: John H Owoc
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Publication number: 20150126708Abstract: The present invention provides a method of radio fluorination of biological targeting molecules (BTMs) with the radioisotope 18F. Also provided are novel conjugates useful in the 18F-radio fluorination method, and the use of such conjugates and automated synthesizer apparatus including cassettes for carrying out the method.Type: ApplicationFiled: December 20, 2012Publication date: May 7, 2015Applicants: IMPERIAL INNOVATIONS LIMITED, GE HEALTHCARE LIMITEDInventors: Sajinder Kaur Luthra, Robin Fortt, Ramala Osman Awais, Eric Ofori Aboagye, Graham Smith
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Publication number: 20150126450Abstract: Novel peptoid oligomers are disclosed that have a formula represented by the following formula Ia or Ib: The peptoid oligomers are prepared as modulators of androgen receptor (AR), and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals, including humans, associated with unwanted or aberrant AR activity. The present peptoid oligomers are particularly valuable for the treatment of subjects with cancer.Type: ApplicationFiled: April 16, 2013Publication date: May 7, 2015Inventors: Kent Kirshenbaum, Paul Michael Levine, Michael John Garabedian
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Publication number: 20150125422Abstract: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: January 8, 2015Publication date: May 7, 2015Inventors: Sheldon Hiebert, Ramkumar Rajamani, Li-Qiang Sun, Eric Mull, Eric P. Gillis, Michael S. Bowsher, Qian Zhao, Nicholas A. Meanwell, Kishore V. Renduchintala, Kandhasamy Sarkunam, Pulicharla Nagalakshmi, P.V.K. Suresh Babu, Paul Michael Scola
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Patent number: 9023801Abstract: A topical composition for application to aging skin, including an effective amount of S-acyl glutathione derivative of formula (I) wherein R1 consists of an unsaturated or saturated C16 acyl group and R2 is a hydrogen, aliphatic or aromatic acyl group; and a dermatologically acceptable carrier. Preferred compositions include about 1.0% to about 3.0% by weight of S-palmitoyl glutathione.Type: GrantFiled: October 23, 2013Date of Patent: May 5, 2015Assignee: N.V. Perricone LLCInventor: Nicholas V. Perricone
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Publication number: 20150119330Abstract: Inhibitors of fibroblast activation protein alpha (FAP) and Prolyl Oligopeptidase (POP) are disclosed, along with their use in various therapies related to conditions, diseases, and disorders involving abnormal cell proliferation such as malignancies and angiogenesis, and in neural disorders such as Alzheimer's disease. Stalk portions of the inhibitor molecules, and substrates of FAP and POP, are also disclosed and may be used, for example, in screening methods for identifying such inhibitors.Type: ApplicationFiled: May 3, 2013Publication date: April 30, 2015Inventors: Patrick A. McGee, Kenneth W. Jackson, Victoria J. Christiansen
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Publication number: 20150119342Abstract: The present invention relates to conformationally constrained homo- and heterodimeric mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.Type: ApplicationFiled: February 20, 2012Publication date: April 30, 2015Applicants: Universita' Degli Studi Di Milano, Fondazione Cariplo, CISI Scrl, Fondazione IRCCS Istituto Nazionale dei TumoriInventors: Pierfausto Seneci, Laura Belvisi, Federica Cossu, Domenico Delia, Carmelo Drago, Daniele Lecis, Stefano Maiorana, Leonardo Pierpaolo Manzoni, Eloise Mastrangelo, Mario Milani de Mayo de Mari, Paola Maria Chiara Perego, Francesca Vasile
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Publication number: 20150119553Abstract: Compounds are disclosed that are useful for noninvasive imaging in the near-infrared spectral range.Type: ApplicationFiled: November 24, 2014Publication date: April 30, 2015Inventors: Xinshe Xu, Daniel R. Draney, Lael Cheung
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Publication number: 20150119334Abstract: An isolated peptide is disclosed. The peptide comprises a titanium oxide binding amino acid sequence connected to a heterologous biologically active amino acid sequence via a beta sheet breaker linker, wherein: (i) the titanium oxide binding amino acid sequence is selected to bind coordinatively with titanium oxide; (ii) the titanium oxide binding amino acid sequence is selected to induce a beta sheet structure; and (ii) the titanium oxide binding amino acid sequence binds to titanium oxide with a higher affinity than said biologically active amino acid sequence binds to the titanium oxide under physiological conditions. Use of the peptides and titanium devices comprising same are also disclosed.Type: ApplicationFiled: June 3, 2013Publication date: April 30, 2015Applicant: Ben-Gurion niversity of the Negev Research and Development AuthorityInventors: Hanna Rapaport, Anna Gittelman
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Publication number: 20150111837Abstract: The invention relates to the field of biochemistry and concerns of recombinant method for production of peptides and the resulting peptides. In particular, the invention relates to peptides with the following general formula: A-Thr-Lys-Pro-B-C-D-X, where: A—0, Met, Met (O), Thr, Ala, His, Phe, Lys, Gly B—0, Gly, Asp, Trp, Gin, Asn, Tyr, Pro, Arg C—0, Arg, Phe, Tyr, Gly, His, Pro, Lys D—0, Val, Gly, Tyr, Trp, Phe, His X—OH, OCH3, NH2, where 0 is no amino acid residue, provided that if A?0, then B and/or C and/or D?0, if B?0, then C and/or D?0, excluding the peptides Phe-Thr-Lys-Pro-Gly, Thr-Lys-Pro-Pro-Arg, Thr-Lys-Pro-Arg-Gly.Type: ApplicationFiled: May 28, 2013Publication date: April 23, 2015Applicant: "IVIX" Ltd.Inventors: Nikolay Fedorovich Myasoedov, Lyudmila Alexandrovna Andreeva, Dmitriy Viktorovich Golikov
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Publication number: 20150099709Abstract: The present invention relates to a use of a compound having ghrelin receptor agonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for treatment of diseases including achlorhydria in which abnormal gastric acid secretion is involved. In addition, the present invention relates to the method of treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agents. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound of the present invention or a pharmaceutically acceptable salt thereof for the treatment of said diseases.Type: ApplicationFiled: May 27, 2013Publication date: April 9, 2015Inventors: Nobuyuki Takahashi, Masaki Sudo, Kaoru Shimada, Hiroaki Wakabayashi
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Patent number: 9000126Abstract: Provided is a novel crystal of oxidized glutathione hexahydrate. Crystal of oxidized glutathione hexahydrate is produced by cooling an aqueous solution containing oxidized glutathione to 15° C. or lower to precipitate a crystal of oxidized glutathione hexahydrate.Type: GrantFiled: April 21, 2011Date of Patent: April 7, 2015Assignee: Kyowa Hakko Bio Co., Ltd.Inventors: Ken Kimura, Kenta Fukumoto, Hiroshi Tanaka
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Publication number: 20150093370Abstract: The present invention provides albumin-binding probes capable of reversibly linking to short-lived amino-containing drugs and non-covalently associating with albumin in-vivo, thereby converting said drugs into inactive reactivable prodrugs having prolonged lifetime in-vivo. The invention further provides conjugates of said probes with amino-containing drugs, as well as pharmaceutical compositions and uses thereof.Type: ApplicationFiled: December 9, 2014Publication date: April 2, 2015Inventors: Yoram SHECHTER, Matityahu FRIDKIN
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Publication number: 20150087578Abstract: The present invention relates to the use of compounds selected from the group consisting of Lys-(D)Pro-Thr, N-acyl Lys-(D)Pro-Thr, C-amide Lys-(D)Pro-Thr, and C-esters of Lys-(D)Pro-Thr; or a pharmaceutically acceptable salt of said compound for the treatment of inflammatory disorders. The invention also relates to the use of ?MSH for inducing tolerance.Type: ApplicationFiled: August 25, 2014Publication date: March 26, 2015Inventor: Thomas LUGER
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Publication number: 20150080316Abstract: The invention relates to new functionalized thieno-indole derivatives of formula (I) or (II) which have cytotoxic activity and are useful in treating diseases such as cancer and cellular proliferation disorders. The invention also relates to the use of these functionalized thieno-indole derivatives in the preparation of conjugates.Type: ApplicationFiled: March 28, 2013Publication date: March 19, 2015Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Italo Beria, Michele Caruso, Vittoria Lupi, Paolo Orsini, Matteo Salsa
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Publication number: 20150080551Abstract: There is provided a lysine oligomer derivative, wherein an ?-amino group and a carboxyl group of lysines are linked via a peptide bond, and a group capable of generating or absorbing electromagnetic wave is bonded to a C-terminal carboxyl group, an N-terminal amino group and/or an ?-amino group. This lysine oligomer derivative has the characteristic of specifically accumulating in the cartilage matrix and can generate or absorb an electromagnetic wave, and is, therefore, useful as a cartilage tissue marker.Type: ApplicationFiled: March 13, 2013Publication date: March 19, 2015Applicant: NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITYInventors: Toshitaka Oohashi, Hiroki Kakuta
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Publication number: 20150072942Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.Type: ApplicationFiled: April 8, 2014Publication date: March 12, 2015Applicant: Millennium Pharmaceuticals, Inc.Inventors: Julian Adams, Yu-Ting Ma, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
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Publication number: 20150073124Abstract: The invention provides a microRNA inhibitor that has two or more sequences complementary to the sequence of microRNA to be the target of inhibition, which two or more complementary sequences are linked via one or more linker residues.Type: ApplicationFiled: March 4, 2013Publication date: March 12, 2015Inventors: Tadaaki Ohgi, Hisao Shirohzu, Hiroshi Suzuki, Tomohiro Hamasaki, Takayuki Mizutani
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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: 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: 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: 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