Polycyclo Ring System Patents (Class 514/765)
  • Patent number: 10703698
    Abstract: Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: July 7, 2020
    Assignees: The Board of Trustees of the University of Illinois, Board of Regents of the University of Texas System
    Inventors: John A. Katzenellenbogen, Benita Katzenellenbogen, Sung Hoon Kim, Zeynep Madak-Erdogan, Philip Shaul
  • Patent number: 10662218
    Abstract: Described herein, inter alia, are compositions and methods for treating or preventing obesity and using the same.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: May 26, 2020
    Inventors: Ralph Mazitschek, Yanbing Ding, Kaisheng Shen
  • Patent number: 10301253
    Abstract: Provided herein are compounds of formula I: and salts thereof and compositions and uses thereof. The compounds are useful as inhibitors of LSD1. Also included are pharmaceutical compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various LSD1-mediated disorders.
    Type: Grant
    Filed: July 24, 2017
    Date of Patent: May 28, 2019
    Assignees: GENENTECH, INC., CONSTELLATION PHARMACEUTICALS, INC.
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Cote, Martin Duplessis, Victor S. Gehling, Andrew Charles Good, Jean-Christophe Harmange, Yves LeBlanc, Christopher G. Nasveschuk, Alexander M. Taylor, Rishi G. Vaswani
  • Patent number: 10206964
    Abstract: The present invention discloses synergistic nutraceutical or pharmaceutical or dietary supplement anti-inflammatory compositions comprising therapeutically effective combination of an extract selectively enriched in 3-O-acetyl-1 1-keto-?-boswellic acid (AKBA) derived from Boswellia serrata and Boswellia serrata non-acidic resin extract (BNRE). The composition(s) can be used to prevent, control and treat inflammation and several inflammatory related diseases including asthma, osteoarthritis, rheumatoid arthritis, endothelial dysfunction and the like. The invention further discloses the amelioration of pro-inflammatory biomarker proteins or molecules, whose expression/production is altered during inflammatory diseases.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: February 19, 2019
    Assignee: LAILA NUTRACEUTICALS
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Trimurtulu Golakoti, Kiran Bhupathiraju, Venkata Krishna Raju Alluri
  • Patent number: 9101599
    Abstract: The present invention discloses synergistic nutraceutical or pharmaceutical or dietary supplement anti-inflammatory compositions comprising therapeutically effective combination of an extract selectively enriched in 3-O-acetyl-11-keto-?-boswellic acid (AKBA) derived from Boswellia serrata and Boswellia serrata non- acidic resin extract (BNRE). The composition(s) can be used to prevent, control and treat inflammation and several inflammatory related diseases including asthma, osteoarthritis, rheumatoid arthritis, endothelial dysfunction and the like. The invention further discloses the amelioration of pro-inflammator biomarker proteins or molecules, whose expression/production is altered during inflammatory diseases.
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: August 11, 2015
    Assignee: Laila Nutraceuticals
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Trimurtulu Golakoti, Kiran Bhupathiraju, Venkata Krishna Raju Alluri
  • Patent number: 9000050
    Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 7, 2015
    Assignee: The University of British Columbia
    Inventors: Xiaoxia Wang, Labros George Meimetis, Matthew Bruce Nodwell, Raymond Andersen
  • Patent number: 8921369
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: December 30, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 8853275
    Abstract: A novel therapy regime/regimen for the treatment of acne related diseases includes administering a topical fixed-dose combination of a retinoid and an anti-bacterial agent, such as BPO, to a course of oral antibiotic therapy.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: October 7, 2014
    Assignee: Galderma Research & Development
    Inventors: Jean-Charles Dhuin, Nabil Kerrouche, Stéphanie Arsonnaud, Pascale Soto
  • Publication number: 20140243404
    Abstract: This disclosure is related to halonium compounds useful for cyclization of polyenes, alkenoic acids, and alkenyl alkyl ethers, and halogenation of aromatic compounds. The synthesis of such halonium compounds, compounds made using such halonium compounds, and synthesis of natural compounds, including decalins, using the halonium compounds is also disclosed.
    Type: Application
    Filed: September 13, 2011
    Publication date: August 28, 2014
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Scott Alan Snyder, Daniel S. Treitler, Alexandria P. Brucks, Andreas Gollner, Maria I. Chiriac, Nathan E. Wright, Jason J. Pflueger, Steven P. Breazzano
  • Patent number: 8809402
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: August 19, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
  • Patent number: 8765820
    Abstract: Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: July 1, 2014
    Assignees: Universita Degli Studi di Roma “La Sapienza”, Fondazione IEO, Universita Degli Studi di Pavia, Universita Degli Studi di Milano
    Inventors: Saverio Minucci, Antonello Mai, Andrea Mattevi
  • Patent number: 8722746
    Abstract: The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.
    Type: Grant
    Filed: April 16, 2007
    Date of Patent: May 13, 2014
    Assignee: Fab Pharma S.A.S.
    Inventors: Alexis Denis, Vincent Gerusz, Yannick Bonvin
  • Patent number: 8604086
    Abstract: The present invention relates to a method of treating and preventing a papillomavirus infection in an individual, comprising administering to the individual a therapeutically effective amount of a condensation polymer of an aromatic sulfonic acid and an aldehyde, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: December 10, 2013
    Assignee: Endo Pharmaceuticals Solutions Inc.
    Inventor: Albert T. Profy
  • Patent number: 8586634
    Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: November 19, 2013
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond G. Booth
  • Patent number: 8394357
    Abstract: The present invention concerns an improved optical method and optical sensing device for determining the levels of polyhydroxyl-substituted organic molecules in vitro and/or in vivo in aqueous media. The range of detection is between about 400 and 800 nm. In particular, a sensory devise is implemented in a mammal to determine sugar levels. Specifically, a dye is combined with a conjugated nitrogen-containing heterocyclic aromatic boronic acid-substituted bis-onium compound in the presence of a sugar, such as fructose or glucose. The viologens are preferred as the aromatic conjugated nitrogen-containing boronic acid substituted compounds. The method is useful to determine sugar levels in a human being.
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: March 12, 2013
    Assignee: The Regents of the University of California
    Inventors: Bakthan Singaram, Ritchie A. Wessling
  • Patent number: 8394859
    Abstract: Analogs of combretastatin have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.
    Type: Grant
    Filed: August 22, 2008
    Date of Patent: March 12, 2013
    Assignee: Baylor University
    Inventors: Kevin G. Pinney, Madhavi Sriram
  • Patent number: 8367735
    Abstract: The present invention relates to compounds of formula I or II:—wherein R is an alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, or aralkynyl group, that may be substituted or unsubstituted, and that optionally includes at least one heteroatom in its carbon skeleton; R1 is hydrogen, or an alkyl, substituted alkyl, alkenyl, alkynyl, aryl, substituted aryl, or aralkyl group; and R2 is an alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, or aralkynyl group containing 4-12 carbon atoms, that may be substituted or unsubstituted, and that optionally includes at least one heteroatom in its carbon skeleton; provided that in a compound of formula I, when R1 is an iso-propyl or phenyl group, R2 is not an acetyl or tert-butyldimethylsilyl group; and their use in therapeutic, diagnostic and research methods.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: February 5, 2013
    Assignee: Crawford Healthcare Holdings Limited
    Inventors: Stanley M. Roberts, Gabriella M. Santoro
  • Publication number: 20130019813
    Abstract: A growing medium for use in plugging pest orifices includes a bulking agent and a water-retentive polymer blended together and compressed at a volume-to-volume ratio greater than 3:1, wherein the growing medium is at least 50% superabsorbing polymer.
    Type: Application
    Filed: June 25, 2012
    Publication date: January 24, 2013
    Inventors: Patti D. Rubin, Jessica Nielsen
  • Patent number: 8283383
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: October 9, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Patent number: 8273757
    Abstract: The present invention is a novel analgesic combination and its use. It is classified to be an invention in the field of medicine and technology. The purpose of this invention is to solve the problem that existing analgesics does not effectively attenuate pain or produces serious side-effects in clinic. The ingredients of the analgesic combination include ketanserin and propranolol. This combination is used to make a drug to treat pain. Because the ingredients of the analgesic combination target peripheral receptors, the unwanted effects could be only minimal. The big advantage of this combination is that each of the ingredients acts on the different receptors producing the synergizing analgesic. Therefore, the analgesia that the combination produces is remarkable and the effective doses are low.
    Type: Grant
    Filed: August 30, 2010
    Date of Patent: September 25, 2012
    Inventor: Yanguo Hong
  • Patent number: 8158685
    Abstract: The present invention relates to novel chemical compositions and methods of treating and regenerating bone in a patient in need thereof. This invention presents a novel chemical composition of matter that stimulates osteoblast formation and inhibits osteoclastic and phagocytosis activity thereby resulting in a significant increase in bone formation.
    Type: Grant
    Filed: June 25, 2005
    Date of Patent: April 17, 2012
    Inventor: Gregory Gene Steiner
  • Publication number: 20120054920
    Abstract: The present invention provides a composition comprising an amphiphile and an active ingredient whose solubility in water at 20° C. is not more than 10 g/L. Likewise provided is an amphiphile comprising a hyperbranched polycarbonate which is joined to at least one linear or comb-type polymer, a process for preparing the amphiphile, and the use of the amphiphile in compositions comprising an active ingredient whose solubility in water at 20° C. is not more than 10 g/L.
    Type: Application
    Filed: May 4, 2010
    Publication date: March 1, 2012
    Applicant: BASF SE
    Inventors: Holger Tuerk, Monika Haberecht, Michael Ishaque, Hiroe Yamada, Daniel Schoenfelder, Bernd Bruchmann
  • Patent number: 8105836
    Abstract: Dominant negative alleles of human mismatch repair genes can be used to generate hypermutable cells and organisms. By introducing these genes into cells and transgenic animals, new cell lines and animal varieties with novel and useful properties can be prepared more efficiently than by relying on the natural rate of mutation. Methods of generating mutations in genes of interest and of making various cells mismatch repair defective through the use of chemicals to block mismatch repair in in vivo are disclosed.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: January 31, 2012
    Assignee: Morphotek, Inc.
    Inventors: Nicholas C. Nicolaides, Luigi Grasso, Philip M. Sass
  • Patent number: 8075917
    Abstract: The present invention relates to a paclitaxel composition and the preparation methods thereof to solubilize paclitaxel wherein said composition comprises 4 to 90% by weight of at least one selected from the monoglycerides, 0.01 to 90% by weight of at least one oil and 0.01 to 20% by weight of paclitaxel. Also the present invention relates to a paclitaxel composition including emulsifiers and the preparation methods thereof to solubilize paclitaxel wherein said composition comprises 4 to 90% by weight of at least one selected from the monoglycerides, 0.01 to 90% by weight of at least one emulsifier and 0.01 to 20% by weight of paclitaxel. The composition of the present invention is an effective paclitaxel delivery system since the composition solubilizes paclitaxel, does not form aggregates after being dispersed in water, adsorbs well on the intestinal wall, and therefore has high bioavailability.
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: December 13, 2011
    Assignee: Daehwa Pharm. Co., Ltd.
    Inventors: Hesson Chung, Seo-Young Jeong, Ick-Chan Kwon, Yeong-Taek Park, In-Hyun Lee, Soon-Hong Yuk, Young-Wook Choi, Jae-Hyung Park, Jin-Wook Chung
  • Publication number: 20110300239
    Abstract: An object of the present invention to obtain a blood flow improving agent composed of natural components, which increase activity or circulation of blood flow and accelerate decomposition, detoxication and elimination of toxic substances and supplement each other, and the production method thereof. The blood flow improving agent of the present invention is prepared by blending a nano-colloidized marine organic compound, more than one of trace elements containing minerals extracted from a mineral ore and nano-colloidized plant minerals and amino acids derived from a fuvic acid in nano-bubble water containing dissolved oxygen.
    Type: Application
    Filed: February 18, 2010
    Publication date: December 8, 2011
    Inventor: Yukio Hasegawa
  • Publication number: 20110251292
    Abstract: The invention consists of a mixture of organic chemicals avoiding the use of insecticides, and a method for pest control based on the mixture consisting in bringing about the premature eclosion of the hibernating larva and its possible death through inanition; experimentation has demonstrated it to be effective in bringing about the premature eclosion of the pecan nut casebearer or Acrobasis nuxvorella (Lepidoptera: Pyralidae) on pecan trees (Carya illinoiensis). The objective is to provide an ecological method for controlling pests such as the pecan nut casebearer, in this manner reducing or avoiding the use of inorganic chemical insecticides which have a significant impact on the environment.
    Type: Application
    Filed: November 3, 2008
    Publication date: October 13, 2011
    Applicant: CENTRO DE INVESTIGACION EN ALIMENTACION Y DESARROLLO A.C.
    Inventors: Irasema Del Carmen Vargas Arispuro, Miguel Angel Martínez Téllez, María Alba Guadalupe Corella
  • Patent number: 7994220
    Abstract: The present invention is directed to methods for providing long-term treatment of fibromyalgia syndrome (FMS) by administering a dual re-uptake inhibitor to a patient with FMS. More particularly, the present invention is directed to the long-term treatment of FMS by administering a norepinephrine-serotonin reuptake inhibitor (NSRI) to a patient with FMS.
    Type: Grant
    Filed: September 26, 2006
    Date of Patent: August 9, 2011
    Assignee: Cypress Bioscience, Inc.
    Inventors: Srinivas G. Rao, Michael Gendreau, Jay D. Kranzler
  • Publication number: 20110117202
    Abstract: Methods and systems for producing a change in a medium. A first method and system (1) place in a vicinity of the medium at least one upconverter including a gas for plasma ignition, with the upconverter being configured, upon exposure to initiation energy, to generate light for emission into the medium, and (2) apply the initiation energy from an energy source including the first wavelength ?1 to the medium, wherein the emitted light directly or indirectly produces the change in the medium. A second method and system (1) place in a vicinity of the medium an agent receptive to microwave radiation or radiofrequency radiation, and (2) apply as an initiation energy the microwave radiation or radiofrequency radiation by which the agent directly or indirectly generates emitted light in the infrared, visible, or ultraviolet range to produce at least one of physical and biological changes in the medium.
    Type: Application
    Filed: November 10, 2010
    Publication date: May 19, 2011
    Applicants: Immunolight, LLC, Duke University
    Inventors: Frederic A. Bourke, JR., Zakaryae Fathi, Ian Nicholas Stanton, Michael J. Therien, Paul Rath Stauffer, Paolo MacCarini, Katherine Sarah Hansen, Diane Renee Fels, Cory Robert Wyatt, Mark Wesley Dewhirst
  • Publication number: 20100216835
    Abstract: The present invention provides compositions and methods for modulating bacterial quorum sensing using antagonist or agonist compounds. Further, the present invention provides methods of treating or preventing microbial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.
    Type: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Inventors: Jo E. Handelsman, Bradley R. Borlee
  • Patent number: 7781412
    Abstract: Compositions of matter and methods of treating cancer patients may prevent or limit cardiotoxicity during or after chemotherapy, and/or may prevent or lower resistance to anthracycline drugs, both of which are believed to be caused by the human enzyme carbonyl reductase. Thus, the compositions and methods may be used to reduce the dosages of anthracycline anti-cancer drugs necessary to produce a desired cancer-cell-killing performance. Preferred embodiments comprise treating cancer patients with a pharmaceutical composition comprising biphenyl compounds having two halogenated (or pseudo-halogenated) and/or hydroxylated, aryl groups that are linked by a bridging atom. The preferred composition of biphenyl compound(s) may be administered in a pharmaceutical composition also comprising at least one anthracycline compound, or may be administered separately than the at least one anthracycline compound. Especially-preferred biphenyl compounds include triclosan, hexachlorophene, and dichlorophene.
    Type: Grant
    Filed: September 27, 2007
    Date of Patent: August 24, 2010
    Assignee: Boise State University
    Inventors: Henry A. Charlier, Jr., Christopher K. Ewing
  • Patent number: 7750033
    Abstract: The present invention relates to a prophylactic agent or a therapeutic agent for a disorder of collagen or elastin metabolism, which comprises a substance possessing JNK inhibitory activity as an active ingredient.
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: July 6, 2010
    Assignee: Yamaguchi University
    Inventors: Koichi Yoshimura, Hiroki Aoki, Masunori Matsuzaki
  • Patent number: 7709537
    Abstract: This invention relates to drinks and foods having osteogenetic function, each of which comprises as an active ingredient an effective amount of a culture of a propionic acid bacterium and/or a lactic acid bacterium, said culture containing 2-amino-3-carboxy-1,4-naphthoquinone; and preventives and/or remedies for metabolic bone diseases, each of which comprises as an active ingredient a naphthoquinone compound selected from the group consisting of 2-amino-3-carboxy-1,4-naphthoquinone, 1,4-naphthoquinone, 2-hydroxy-1,4-naphthoquinone, 2,3-dichloro-1,4-naphthoquinone, 5-hydroxy-1,4-naphthoquinone, 8-hydroxy-1,4-naphthoquinone, 2-(?-hydroxy-?-methylpentenyl)-5,8-dihydroxy-1,4-naphthoquinone and salts thereof. These cultures and naphthoquinones promote bone metabolism and increase bone mass and bone strength.
    Type: Grant
    Filed: October 18, 2000
    Date of Patent: May 4, 2010
    Assignee: Meiji Dairiese Corporation
    Inventors: Kazuo Nagai, Jetae Woo, Yoshiro Sato, Kouichiro Hashimoto, Naoki Taketomo, Nobuo Yoda, Hiroshi Tsuchida
  • Publication number: 20090280147
    Abstract: According to the invention, a cosmetic composition is provided comprising: (a) amorphous particles, each amorphous particle comprising a homogeneous distribution of one or more dyes encapsulated by an amorphous, siliceous encapsulating agent, wherein the amorphous particle comprises from 3% to 20%, preferably 5% to 15%, more preferably 8% to 12% dye, by weight of the particle; (b) a cosmetically acceptable carrier.
    Type: Application
    Filed: August 12, 2008
    Publication date: November 12, 2009
    Inventors: Peter Carl Anders Alberius, Robert William Corkery, Alison Fiona Stephens
  • Publication number: 20090274621
    Abstract: Described are methods for delivering a non-peptide agent across the blood-brain barrier, comprising administering to a subject a conjugate comprising (i) a non-peptide agent and (ii) pyrene, and related detection and therapeutic method.
    Type: Application
    Filed: January 30, 2009
    Publication date: November 5, 2009
    Inventors: Renee Wegrzyn, Andrew Nyborg, D. Roxanne Duan, Alan Rudolph
  • Publication number: 20090275608
    Abstract: Disclosed are methods of identifying a disease treatable with modulators of differentially expressed genes in a disease, including at least PARP modulators, by identifying the level of expression of differentially expressed genes, including at least PARP, in a plurality of samples from a population, making a decision regarding identifying the disease treatable by modulators to the differentially expressed genes wherein the decision is made based on the level of expression of the differentially expressed genes. The method can further comprise treating the disease in a subject population with modulators of identified differentially expressed genes. The methods relate to identifying up-regulated expression of identified differentially-expressed genes in a disease and making a decision regarding the treatment of the disease. The level of expression of the differentially expressed genes in a disease can also help in determining the efficacy of the treatment with modulators to the differentially expressed genes.
    Type: Application
    Filed: February 4, 2009
    Publication date: November 5, 2009
    Applicant: BiPar Sciences, Inc.
    Inventors: Valeria S. Ossovskaya, Barry M. Sherman
  • Publication number: 20090238754
    Abstract: Described are methods for delivering a peptide agent across the blood-brain barrier, comprising administering to a subject a conjugate comprising (i) a peptide agent and pyrene, and related detection and therapeutic methods.
    Type: Application
    Filed: January 30, 2009
    Publication date: September 24, 2009
    Inventors: Renee WEGRZYN, Andrew Nyborg, D. Roxanne Duan, Alan Rudolph
  • Patent number: 7566741
    Abstract: Methods of inhibiting osteoclastogenesis and the activity of osteoclasts are disclosed. Methods of treating patients who have diseases characterized bone loss are disclosed. According to the methods, an amount of a TRANCE/RANK inhibitor effective to inhibit osteoclastogenesis is administered to the patient. Pharmaceutical compositions which comprise TRANCE/RANK inhibitor in an amount effective to inhibit osteoclastogenesis. Methods of modulating dendritic cell maturation, T cell proliferation, and/or CD40 receptor systems in an individual are disclosed. The methods comprise the step of administering to the individual an amount of a TRANCE/RANK inhibitor effective to modulating dendritic cell maturation, T cell proliferation, and/or CD40 receptor systems.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: July 28, 2009
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Mark I. Greene, Ramachandran Murali, Masahiko Kinosaki
  • Patent number: 7553877
    Abstract: The present invention provides compounds of the formula wherein A is of the formula and X, Y, n, R1—R25 are as described in the specification which are modulators of the glucocorticoid receptor and are thus useful for the treatment of animals requiring glucocorticoid receptor agonist therapy. Glucocorticoid receptor modulators are useful in the treatment of certain inflammatory conditions.
    Type: Grant
    Filed: July 13, 2006
    Date of Patent: June 30, 2009
    Assignee: Pfizer, Inc.
    Inventors: Yves A. Chantigny, Edward F. Kleinman, Ralph P. Robinson
  • Patent number: 7470420
    Abstract: The present invention concerns an improved optical method and optical sensing device for determining the levels of polyhydroxyl-substituted organic molecules in vitro and/or in vivo in aqueous media. The range of detection is between about 400 and 800 nm. In particular, a sensory devise is implemented in a mammal to determine sugar levels. Specifically, a dye is combined with a conjugated nitrogen-containing heterocyclic aromatic boronic acid-substituted bis-onium compound in the presence of a sugar, such as fructose or glucose. The viologens are preferred as the aromatic conjugated nitrogen-containing boronic acid substituted compounds. The method is useful to determine sugar levels in a human being.
    Type: Grant
    Filed: December 7, 2005
    Date of Patent: December 30, 2008
    Assignee: The Regents of the University of California
    Inventors: Bakthan Singaram, Ritchie A. Wessling
  • Publication number: 20080279940
    Abstract: The present invention relates to a novel spontaneously dispersible pharmaceutical composition, e.g. a microemulsion preconcentrate, in which the active drug substance is a cannabinoid receptor binding compound, in particular a corresponding naphthalene derivative, that is useful, e.g., for the treatment or prevention of chronic pain.
    Type: Application
    Filed: March 10, 2006
    Publication date: November 13, 2008
    Inventors: Thomas Rigassi, Bruno Galli
  • Publication number: 20080275016
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are fulvene and/or fulvalene analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, as well as numerous inflammatory, degenerative and vascular diseases, including various ocular diseases. Representative fulvene and/or fulvalene analogs include fulvene and fulvalene analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function, at least, by inhibiting Nox or ROS. In some embodiments, the Nox is one that is selectively expressed in cancer cells over normal cells, or one that is expressed in higher amounts in cancer cells over normal cells. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
    Type: Application
    Filed: May 2, 2008
    Publication date: November 6, 2008
    Inventor: Jack L. Arbiser
  • Publication number: 20080153859
    Abstract: The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as anti-inflammatory agents.
    Type: Application
    Filed: February 25, 2008
    Publication date: June 26, 2008
    Inventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
  • Patent number: 7335675
    Abstract: The present invention provides an aqueous suspension formulation containing (RS)-N-[2-(1,3-dimethylbutyl)thiophene-3-yl]-1-methyl-3-trifluoromethyl-1H-pyrazole-4-carboxamide and having high rain resistance and stable residual effectiveness. A aqueous suspension formulation for foliar application fungicide of the present invention contains a fungicidal active ingredient, (RS)-N-[2-(1,3-dimethylbutyl)thiophene-3-yl]-1-methyl-3-trifluoromethyl-1H-pyrazole-4-carboxamide, and a polyoxyalkylene rosin acid ester or liquid paraffin, and has improved rain resistance on plant leaves and excellent residual effectiveness.
    Type: Grant
    Filed: July 7, 2004
    Date of Patent: February 26, 2008
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Koichi Morinaga, Yuji Yanase, Kanemitsu Miyama, Hideo Kawashima
  • Patent number: 7153889
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: October 22, 2003
    Date of Patent: December 26, 2006
    Assignee: Abbott Laboratories
    Inventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
  • Patent number: 7033580
    Abstract: Disclosed is a safe and effective hair-growing agent comprising a protein kinase C-specific inhibitor.
    Type: Grant
    Filed: December 4, 2002
    Date of Patent: April 25, 2006
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Tomoya Takahashi, Yoshiharu Yokoo, Toshikazu Kamiya, Akio Shirai, Tatsuya Tamaoki
  • Patent number: 6955804
    Abstract: Disclosed are methods and compositions for regulating the melanin content of mammalian melanocytes; regulating pigmentation in mammalian skin, hair, wool or fur; treating or preventing various skin and proliferative disorders; by administration of various compounds, including alcohols, diols and/or triols and their analogues.
    Type: Grant
    Filed: September 22, 2003
    Date of Patent: October 18, 2005
    Assignee: Applied Genetics Incorporated Dematics
    Inventors: David A. Brown, Alexander A. Khorlin, Krystyna Lesiak, Wu Yun Ren
  • Patent number: 6852328
    Abstract: A method and device are disclosed which prevents the decay and deterioration of wooden objects caused by pests by using a controlled release device. This controlled release device utilizes polymers which incorporate pesticides. In the disclosed method, the controlled release device is placed in contact with the wood of the wooden object. The pesticide is gradually released from the device and absorbed into the wood structure. The pesticide absorbed by the wood creates a barrier or an exclusion zone to penetration by inserts. The controlled release device maintains a minimal effective level of pesticide in the barrier or exclusion zone for a predetermined period of time.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: February 8, 2005
    Assignee: Battelle Memorial Institute K1-53
    Inventors: Peter Van Voris, Dominic A. Cataldo, Frederick G. Burton
  • Publication number: 20040253286
    Abstract: A new use for chemicals paradichlorobenzene (10) and naphthalene (20), colorless or white, volatile crystals with a strong coal tar odor, that when positioned in areas where birds gather or roost, such as rooftops, eaves or ledges, diffuses into the surrounding air resulting in birds being deterred from affected area.
    Type: Application
    Filed: June 11, 2003
    Publication date: December 16, 2004
    Inventors: Robert J. Pado, Christine Linda Hemphill
  • Patent number: RE39199
    Abstract: A psoriasis treatment composition derived from the plant Asphodelus Microcarpus includes 3-methylanthralin, chrysophanol, aloe-emodin, aloe-emodin monoacetate, and/or derivatives thereof. The composition is prepared by extracting a liquid from the Asphodelus Microcarpus root and mixing the liquid with acetic acid. A method of treatment includes applying the composition to an affected area of skin at a frequency sufficient to effect an alleviation of symptoms, typically once per day for 14-56 days.
    Type: Grant
    Filed: December 21, 2000
    Date of Patent: July 18, 2006
    Inventors: Naseba Moady, Marzook Moady
  • Patent number: RE39866
    Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N?N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
    Type: Grant
    Filed: June 23, 2005
    Date of Patent: October 2, 2007
    Assignee: Telik, Inc.
    Inventors: Richard Sportsman, Hugo O. Villar, Lawrence M Kauvar, Wayne R Spevak