2 Amino Acid Residues In The Peptide Chain Patents (Class 514/21.91)
  • Patent number: 10292969
    Abstract: The present invention relates to a composition for prevention or treatment of bronchial asthma comprising a PKR inhibitor as an active ingredient. The PKR inhibitor and derivatives thereof according to the present invention can be used as a pharmaceutical for prevention, amelioration or treatment of bronchial asthma and as a supplementary health food because the PKR inhibitor and derivatives thereof reduce the total counts of inflammatory cells, eosinophils, neutrophils and lymphocytes in bronchoalveolar lavage fluid of neutrophilic severe asthma-induced mice, reduce airway inflammation and airway hyper-responsiveness, and reduce inflammatory mediators.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: May 21, 2019
    Assignee: Undustrial Cooperation Foundation Chonbuk National University
    Inventors: Yong Chul Lee, So Ri Kim
  • Patent number: 10052359
    Abstract: Compositions, foods, and medicaments for enhancing memory and learning function and/or cognitive function are provided. Compositions, foods, and medicaments for improving brain function and particularly enhancing memory and learning function and/or cognitive function can be provided by including a peptide including an amino acid sequence set forth in any one of SEQ ID NOs 1 to 16 as an active ingredient.
    Type: Grant
    Filed: June 16, 2015
    Date of Patent: August 21, 2018
    Assignee: KIRIN KABUSHIKI KAISHA
    Inventors: Yasuhisa Ano, Toshiko Kutsukake
  • Patent number: 9782368
    Abstract: According to the invention there is provided N,N-bis-2-mercaptoethyl isophthalamide, or a pharmaceutically acceptable salt or derivative thereof, for use in regenerating ascorbate systemically and thus in the therapeutic treatment of chronic obstructive pulmonary disease.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: October 10, 2017
    Assignee: Emeramed Limited
    Inventors: Boyd Eugene Haley, Ragnar Axel Theodor Klingberg
  • Patent number: 9745276
    Abstract: The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: August 29, 2017
    Assignee: Elobix AB
    Inventors: Martin Bohlin, Erica Tjerneld, Andreas Vestermark, Ingvar Ymen
  • Patent number: 9707228
    Abstract: A dry powder formulation comprising a combination of at least a first pharmaceutically active quinolone and a second pharmaceutically active quinolone.
    Type: Grant
    Filed: May 21, 2013
    Date of Patent: July 18, 2017
    Assignees: Agency for Science, Technology and Research, National University Hospital
    Inventors: Desmond Heng, Sie Huey Lee, Jeanette Teo, Wai Kiong Ng, Reginald Tan
  • Patent number: 9701649
    Abstract: The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: July 11, 2017
    Assignee: Elobix AB
    Inventors: Martin Bohlin, Erica Tjerneld, Andreas Vestermark, Ingvar Ymen
  • Patent number: 9566310
    Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 14, 2017
    Assignee: BOARD OF REGENTS OF THE NEVADA SYSTEM OF HIGHER EDUCATION ON BEHALF OF THE UNIVERSITY OF NEVADA, RENO
    Inventors: Dean Burkin, Ryan Wuebbles
  • Patent number: 9498423
    Abstract: The present invention discloses selenium peptide based synergistic compositions for the protection (morphology and viable numbers) of dermal papilla cells. The synergistic compositions disclosed in the present invention comprise (a) 1-O-galloyl-?-D-glucose (?-glucogallin) or 1-O-galloyl-?-D-glucose (?-glucogallin) and gallates (b) concentrate of liquid endosperm of Cocos nucifera and (c) selenopeptides.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 22, 2016
    Assignee: Sami Labs Limited
    Inventors: Muhammed Majeed, Kalyanam Nagabhushanam
  • Patent number: 9487555
    Abstract: This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.
    Type: Grant
    Filed: June 23, 2015
    Date of Patent: November 8, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Marion W. Wannamaker, Robert J. Davies
  • Patent number: 9327001
    Abstract: According to one embodiment, a nutritional supplement for suppressing an appetite while maintaining muscle mass of a subject during weight loss is provided. The nutritional supplement includes beta-hydroxy beta-methylbutyric acid (HMB), chromium, and Caralluma fimbriata.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: May 3, 2016
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Maria Grant, Ashay D. Bhatwadekar, Debra Carnegie
  • Patent number: 9040261
    Abstract: A method of preventing or inhibiting L-cystine crystallization using the compounds of formula I is disclosed. 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: Grant
    Filed: May 24, 2013
    Date of Patent: May 26, 2015
    Assignee: NEW YORK UNIVERSITY
    Inventors: Michael D. Ward, Jeffrey Rimer
  • Publication number: 20150141352
    Abstract: The present invention relates to a bone regeneration or bone formation promoting pharmaceutical composition comprising muramyl dipeptide, an analogue thereof, a derivative thereof or a pharmaceutically acceptable salt thereof. In contrast to existing passive therapeutic agents which center on bone absorption suppression based on mechanisms for reducing osteoclast functionality, the composition comprising muramyl dipeptide of the present invention promotes the differentiation of osteoblasts, which are bone forming cells, and can advantageously be used in various diseases where bone formation is required as an active therapeutic agent that does not affect osteoclast.
    Type: Application
    Filed: November 1, 2012
    Publication date: May 21, 2015
    Applicant: SNU R&DB FOUNDATION
    Inventors: Seung Hyun Han, Ok-Jin Park, Cheol-Heul Yun
  • Publication number: 20150126462
    Abstract: The present invention relates to a new pharmaceutical composition containing nicotinic acid, nicotinamide, tryptophanor related compounds for positively influencing the intestinal microbiota. In certain embodiments, the pharmaceutical composition is partially or entirely released into the small intestine or large intestine.
    Type: Application
    Filed: June 14, 2013
    Publication date: May 7, 2015
    Applicant: CONARIS RESEARCH INSTITUTE AG
    Inventors: Georg Waetzig, Dirk Seegert
  • Patent number: 9023805
    Abstract: The present invention discloses and claims compositions, methods of treatment, and kits which cause an increase in the time of survival in cancer patients, wherein the cancer: (i) overexpresses thioredoxin or glutaredoxin and/or (ii) exhibits evidence of thioredoxin- or glutaredoxin-mediated resistance to one or more chemotherapeutic interventions. The present invention also discloses and claims methods and kits for the administration of said compositions to properly treat cancer patients. Additionally, the present invention discloses and claims methods and kits for quantitatively determining the level of expression of thioredoxin or glutaredoxin in the cancer cells of a cancer patient, methods of using those determined levels in the initial diagnosis and/or planning of subsequent treatment methodologies for said cancer patient, as well as ascertaining the potential growth “aggressiveness” of the particular cancer and treatment responsiveness of the particular type of cancer.
    Type: Grant
    Filed: September 16, 2010
    Date of Patent: May 5, 2015
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventor: Frederick H. Hausheer
  • Patent number: 9023809
    Abstract: Disclosed are a compound of formula I, stereoisomers, pharmaceutically acceptable salts or hydrates thereof, a pharmaceutical composition comprising the same, a process for preparing the same and use thereof. The compound may also be used to prepare a medicament to treat viral infections, especially to prepare a medicament to treat hepatitis B virus and human immunodeficiency virus with little toxic side effects.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: May 5, 2015
    Assignees: The Key Laboratory of Chemistry For Natural Products of Guizhou Province and Chinese Academy of Sciences, Tianjin Institute of Pharmaceutical Research, 302 Hospital of PLA, China
    Inventors: Guangyi Liang, Bixue Xu, Changxiao Liu, Zhengming Huang, Peixue Cao, Zegui Cai, Yuming Liu
  • Patent number: 9023808
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein the dashed line, X, R1, R2, R3, R4, R5, R6, and R7 have defined meanings; the preparation thereof; compositions containing compounds of formula (I), including bioavailable combinations with ritonavir; and the pharmaceutical uses thereof.
    Type: Grant
    Filed: January 16, 2008
    Date of Patent: May 5, 2015
    Assignees: Medivir AB, Janssen R&D Ireland
    Inventors: Kenneth Alan Simmen, Herman Agustinus De Kock, Carl Erik Daniel Jonsson, Karl Magnus Milsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Susana Ayesa Alverez, Bjorn Olaf Classon, Hans Kristian Wallberg
  • Publication number: 20150118224
    Abstract: Described herein are methods and kits for the detection of endothelial cell injury and/or activation and to the diagnostic of transplant antibody mediated rejection (ABMR). The invention further relates to methods and kits for diagnosing endothelial to mesenchymal transition (EndMT). In various embodiments, the methods comprise assessing expression of one, two or three biomarkers selected from Fascin1, Vimentin and Hsp47.
    Type: Application
    Filed: April 4, 2013
    Publication date: April 30, 2015
    Inventors: Yi-Chun Xu-Dubois, Eric Rondeau, Julie Peltier, Alexandre Hertig, Isabelle Brocheriou
  • Publication number: 20150111828
    Abstract: The invention relates to compounds having either agonist or antagonist activities for the neurotrophins NGF and BDNF and represented by monomeric or dimeric substituted dipeptides that are analogs of the exposed portions of loop 1 or loop 4 regions of these neurotrophins near or at a beta-turn of the respective loop. N-acylated substituents of these dipeptides are biostereoisomers of the amino acid residues preceding these dipeptide sequences in the neurotrophin primary structure. The dimeric structure is produced advantageously by using hexamethylenediamine to which dipeptides are attached via their carboxyl groups. The claimed compounds displayed neuroprotective and differentiation-inducing activities in cellular models and enhanced the amount of phosphorylated tyrosine kinase A and the heat shock proteins Hsp32 and Hsp70 in the concentration range of 10?9 to 10?5 M.
    Type: Application
    Filed: August 15, 2014
    Publication date: April 23, 2015
    Applicant: UCHREZHDENIE ROSSIISKOI AKADEMII MEDITSYNSKIKH NAUK NAUCHNO-ISSLEDOVATELSKY INSTITUT FARMAKOLOGII
    Inventors: Sergey Borisovich SEREDENIN, Alexandrovna Tatyana GUDASHEVA
  • Patent number: 9011883
    Abstract: Intraperitoneal administration of glutamine to reduce adhesions in the peritoneum of a patient.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: April 21, 2015
    Assignee: Ade Therapeutics Inc.
    Inventor: Adebola O. E. Obayan
  • Publication number: 20150099691
    Abstract: A dipeptide derivative as formyl peptide receptor 1 (FPR1) antagonist is provided. The dipeptide derivative is represented by formula (I), wherein: the chiral centers in formula (I) are S and R configurations respectively; each of RK and RT is selected from a group consisting of a hydrogen, a hydroxyl group, a C1-C4 alkyl-substituted hydroxyl group, a C1-C4 alkoxyl group, a carboxylic acid group, a C1-C4 alkyl nitrile-substituted, C1-C4 alkyl-substituted or C1-C4 alkoxyl-substituted amido group, a C1-C4 alkyl-substituted ester group and a benzoyl group having a C1-C4 alkyl-substituted benzene ring; and each of RM and RS is selected from a group consisting of a hydrogen, a hydroxyl group, a phenyl group, a pyridinyl group, a carboxylic acid group, a C1-C4 alkoxyl substituted ester group, and a benzoyl group having a hydroxyl-substituted, a halogen-substituted, a C1-C4 alkoxyl-substituted or a C1-C4 alkyl-substituted benzene ring.
    Type: Application
    Filed: April 9, 2014
    Publication date: April 9, 2015
    Applicant: CHANG GUNG UNIVERSITY
    Inventors: Tsong-Long Hwang, Pei-Wen Hsieh, Yin-Ting Huang, Chih-Hao Hung
  • Patent number: 8993523
    Abstract: 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: Grant
    Filed: December 13, 2011
    Date of Patent: March 31, 2015
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Christopher Sean Straub
  • Publication number: 20150087600
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: January 21, 2013
    Publication date: March 26, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Zhenwei Cai, Shunqi Yan, Ding Zhou
  • Publication number: 20150087578
    Abstract: 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: Application
    Filed: August 25, 2014
    Publication date: March 26, 2015
    Inventor: Thomas LUGER
  • Patent number: 8980845
    Abstract: The present invention relates to a process for the enzymatic production of a dipeptide composition from a cyanophycin (CGP) or CGP-like polymer preparation by degrading the polymer preparation with an CGPase, a CGPase particularly adapted for said process, and the use of cyanophycin (CGP) or CGP-like polymers or fragments thereof, notably a dipeptide composition obtained by the process as defined above, as pharmaceutical composition, medicament, or as food or feed substitute.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: March 17, 2015
    Assignee: Westfälische Wilhelms-Universität Münster
    Inventors: Ahmed Sallam, Alexander Steinbüchel
  • Publication number: 20150072942
    Abstract: 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: Application
    Filed: April 8, 2014
    Publication date: March 12, 2015
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Julian Adams, Yu-Ting Ma, Ross L. Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
  • Publication number: 20150065437
    Abstract: 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: Application
    Filed: March 20, 2014
    Publication date: March 5, 2015
    Applicant: Stealth Peptides International, Inc.
    Inventors: Liping Liu, Lawrence Gu
  • Publication number: 20150056217
    Abstract: The present invention relates to the use of a TLR9 agonist and/or a TLR4 antagonist and/or a NOD2 agonist for treatment or prevention of disorders involving TLR4 activation, such as systemic sepsis and necrotizing enterocolitis.
    Type: Application
    Filed: August 26, 2013
    Publication date: February 26, 2015
    Applicant: University of Pittsburgh - of the Commonwealth System of Highter Education
    Inventor: DAVID J. HACKAM
  • Publication number: 20150056300
    Abstract: The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 0.1 to about 40 weight percent of a therapeutic agent and about 10 to about 90 weight percent a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer, wherein the diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic) acid having a number average molecule weight of about 30 kDa to about 90 kDa or the diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer comprises poly(lactic)-co-poly(glycolic) acid having a number average molecule weight of about 30 kDa to about 90 kDa.
    Type: Application
    Filed: October 24, 2011
    Publication date: February 26, 2015
    Applicant: BIND Therapeutics, Inc.
    Inventors: David Dewitt, Maria Figueiredo, Hong Wang, Greg Troiano, Young-Ho Song
  • Patent number: 8962572
    Abstract: A bortezomib composition includes bortezomib and boric acid in a mass ratio of boric acid to bortezomib is from 1:1 to 10:1. The composition is a solid, and may be prepared by forming a liquid mixture including a solvent, bortezomib and boric acid, and lyophilizing the liquid mixture.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: February 24, 2015
    Assignee: Fresenius Kabi USA, LLC
    Inventors: Arunya Usayapant, David Bowman
  • Publication number: 20150051160
    Abstract: 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: Application
    Filed: October 29, 2012
    Publication date: February 19, 2015
    Applicants: BAYER PHARMA AKTIENGESELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ingo Flamme, Johannes Köbberling, Hans-Georg Lerchen, Nils Griebenow, Rudolf Schohe-Lop, Sven Wittrock, Ursula Krenz
  • Publication number: 20150051161
    Abstract: The present invention provides compositions and methods for detecting carboxymethyl-lysine (CML) and circulating receptor for advanced glycation end (RAGE) products, and methods for correlating CML and RAGE levels with age-related disease. In particular, serum CML and/or circulating receptor for advanced glycation end (RAGE) products can be used as a clinical biomarker in diagnostics to identify people who are at a higher risk of developing adverse ageing-related outcomes.
    Type: Application
    Filed: April 10, 2014
    Publication date: February 19, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Richard David Semba, Luigi Ferruci, Edward G. Lakatta
  • Publication number: 20150045312
    Abstract: Methods of treating autism, autistic spectrum disorders or Fragile X syndrome comprised of administering molecules that engage the cystine-glutamate exchange (System xc?) and/or elevate the extracellular levels of glutathione in the CNS. Preferred compounds are cysteine/cystine prodrugs or N-acetyl cysteine (NAC) prodrugs.
    Type: Application
    Filed: August 11, 2014
    Publication date: February 12, 2015
    Inventors: Michael Neary, Chad Beyer
  • Publication number: 20150031637
    Abstract: The present invention relates to a combination comprising a substance with inhibiting effect on the ileal bile acid transport system (IBAT) and at least one other active substance selected from an IBAT inhibitor; an enteroendocrine peptide or enhancer thereof; a dipeptidyl peptidase-IV inhibitor; a biguanidine; an incretin mimetic; a thiazolidinone; a PPAR agonist; a HMG Co-A reductase inhibitor; a bile acid binder; and a TGR5 receptor modulator; wherein the IBAT inhibitor compound and the at least one other active substance are administered simultaneously, sequentially or separately.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 29, 2015
    Inventors: Per-Göran Gillberg, Hans Graffner, Ingemar Starke
  • Publication number: 20150031635
    Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
    Type: Application
    Filed: June 30, 2014
    Publication date: January 29, 2015
    Inventors: Thomas E. Jenkins, Julie D. Seroogy, Jonathan W. Wray
  • Publication number: 20150031636
    Abstract: 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: Application
    Filed: October 3, 2014
    Publication date: January 29, 2015
    Inventors: Per-Göran Gillberg, Hans Graffner, Ingemar Starke
  • Publication number: 20150011481
    Abstract: The present invention features interferon-free therapies for treating HCV genotype 1b, 2, 3 or 4. In one aspect, the therapies comprise administering Compound 1, ritonavir, and Compound 2 to a subject infected with HCV genotype 1b or 4, wherein the therapies do not include administration of any interferon, and the therapies last for 12 weeks. Preferably, the therapies do not include administration of any ribavirin.
    Type: Application
    Filed: July 1, 2014
    Publication date: January 8, 2015
    Inventors: Regis A. Vilchez, Lino X. Rodrigues, JR., Barry M. Bernstein, Thomas J. Podsadecki, Scott C. Brun, Daniel E. Cohen, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Tolga Baykal
  • Publication number: 20150011484
    Abstract: The present invention provides pro-drugs of D-gamma-glutamyl-[D/L]-tryptophan, said pro-drugs are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein G is C1-C8 alkyl or benzyl, T is C1-C8 alkyl or benzyl, and * is a chiral carbon in a (R) or (S) configuration, provided that when * is in the (R) configuration, at least one of G and T is C5-C8 alkyl; and use of compounds of Formula I in a pharmaceutical composition.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 8, 2015
    Applicant: APTOEX TECHNOLOGIES, INC.
    Inventors: Tim Fat Tam, Regis Leung-Toung, Yinsheng Wang, Yanqing Zhao, Tao Xin, Wanren Li, Jolanta Maria Wodzinska, Vrajlal S. Rabadia, Birenkumar Shah, Christopher John Feeney
  • Patent number: 8927689
    Abstract: A tubular or spherical 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: Grant
    Filed: November 8, 2012
    Date of Patent: January 6, 2015
    Assignee: Ramot at Tel-Aviv University Ltd.
    Inventors: Meital Reches, Ehud Gazit
  • Patent number: 8927499
    Abstract: The invention provides a method for inhibiting melanin formation composition by applying a glycine derivative, having a structure shown in the following general equation (I): wherein R1 represents a C1˜C4 alkyl group; R2 represents a hydrogen atom or a methyl group; and n represents an integer of 1˜6.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: January 6, 2015
    Assignee: Corum Inc.
    Inventors: Nai-Hsuan Hsu, Chiao-Yi Hsu, Ssu-Ching Wang, Ting-Wan Chen, Chu-Yi Pang
  • Patent number: 8927503
    Abstract: 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: Grant
    Filed: July 28, 2011
    Date of Patent: January 6, 2015
    Assignee: The University of Queensland
    Inventors: David Paul Fairlie, Ligong Liu, Mei Kwan Yau, Jacky Yung Suen, Robert Reid
  • Patent number: 8921319
    Abstract: The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: December 30, 2014
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Torsten Steinmetzer, Sebastian Martin Saupe
  • Publication number: 20140364359
    Abstract: The invention provides di-peptide conjugated antitumor agents, pharmaceutical compositions and methods for preparation and use thereof for treating various cancer and inflammation-related diseases and conditions. The present invention addresses the shortcomings of the existing anti-tumor and anti-inflammatory drugs, particularly in that the anti-tumor agents of the invention that selectively kill cancer cells with minimal damage to normal cells.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 11, 2014
    Inventor: Raymond A FIRESTONE
  • Patent number: 8906852
    Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: December 9, 2014
    Assignee: MethylGene Inc.
    Inventors: Stéphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frédéric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
  • Publication number: 20140356322
    Abstract: 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: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Inventors: 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
  • Patent number: 8901085
    Abstract: 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: Grant
    Filed: July 28, 2011
    Date of Patent: December 2, 2014
    Assignee: The University of Queensland
    Inventors: David Paul Fairlie, Ligong Liu, Mei Kwan Yau, Jacky Yung Suen, Robert Reid
  • Publication number: 20140342997
    Abstract: Present invention refers to complex-forming compounds of the general formula and the use and preparation thereof.
    Type: Application
    Filed: December 28, 2012
    Publication date: November 20, 2014
    Applicant: STRATOXER(S) KFT.
    Inventors: G. Imre Csizmadia, Zoltan Mucsi, Andrea Narcisz Koczkas
  • Publication number: 20140336108
    Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Inventors: Xialing Guo, Zhen Zhu
  • Publication number: 20140329754
    Abstract: This invention generally relates to compositions and methods for treating myelodysplastic syndrome. In one embodiment, this invention relates to methods for treating myelodysplastic syndrome with ezatiostat or a salt thereof and lenalidomide.
    Type: Application
    Filed: April 29, 2014
    Publication date: November 6, 2014
    Applicant: Telik, Inc.
    Inventors: Gail L. Brown, Lixin Meng
  • Publication number: 20140329746
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Publication number: 20140323390
    Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.
    Type: Application
    Filed: July 9, 2014
    Publication date: October 30, 2014
    Applicant: IRM LLC
    Inventors: Tom Yao-Hsiang WU, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan