Polycyclo Ring System Attached By Nonionic Bonding Patents (Class 514/480)
  • Patent number: 10919916
    Abstract: Compounds, pharmaceutical formulations, and methods of treating bacterial infections are disclosed.
    Type: Grant
    Filed: April 3, 2020
    Date of Patent: February 16, 2021
    Assignee: Bill & Melinda Gates Foundation
    Inventors: Xianfeng Li, Christopher S Lunde, Robert T Jacobs, Vincent S Hernandez, Yi Xia, Jacob J Plattner, Kathy Jingyuan Cao, Yong-Kang Zhang, Matthew Perry
  • Patent number: 10874679
    Abstract: Compounds, pharmaceutical formulations, and methods of treating bacterial infections are disclosed.
    Type: Grant
    Filed: April 3, 2020
    Date of Patent: December 29, 2020
    Assignee: Bill & Melinda Gates Foundation
    Inventors: Xianfeng Li, Christopher S Lunde, Robert T Jacobs, Yasheen Zhou
  • Patent number: 10611780
    Abstract: Compounds, pharmaceutical formulations, and methods of treating bacterial infections are disclosed.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: April 7, 2020
    Assignee: Bill and Melinda Gates Foundation
    Inventors: Xianfeng Li, Christopher S. Lunde, Robert T. Jacobs, Vincent S. Hernandez, Yi Xia, Jacob J. Plattner, Kathy Jingyuan Cao, Yong-Kang Zhang, Matthew Perry
  • Patent number: 10611781
    Abstract: Compounds, pharmaceutical formulations, and methods of treating bacterial infections are disclosed.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: April 7, 2020
    Assignee: Bill and Melinda Gates Foundation
    Inventors: Xianfeng Li, Christopher S. Lunde, Robert T. Jacobs, Yasheen Zhou
  • Patent number: 10434180
    Abstract: The present application relates to methods for the enzymatic functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.
    Type: Grant
    Filed: July 19, 2016
    Date of Patent: October 8, 2019
    Assignees: INNATE PHARMA, PAUL SCHERRER INSTITUT
    Inventors: Delphine Bregeon, Patrick Dennler, Christian Belmant, Laurent Gauthier, François Romagne, Eliane Fischer, Roger Schibli
  • Patent number: 10239807
    Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
    Type: Grant
    Filed: December 22, 2015
    Date of Patent: March 26, 2019
    Assignee: SynAffix B.V.
    Inventors: Floris Louis Van Delft, Floris Petrus Johannes Theodorus Rutjes, Frederik Jan Dommerholt
  • Patent number: 9867798
    Abstract: Methods for treating individuals suffering from inflammation, specifically systemic inflammation including septic shock and inflammatory conditions affecting the gastrointestinal, myocardial and endocrine systems with ladostigil.
    Type: Grant
    Filed: August 6, 2014
    Date of Patent: January 16, 2018
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventor: Marta Weinstock-Rosin
  • Patent number: 9849099
    Abstract: Described herein are antimicrobial compounds identified via a high-throughput screen to identify compounds that produce anucleate cells in E. coli after cell division occurs. Compound 1 (5-nonyloxytryptamine) and its analogs are small molecule inhibitors of the nucleoid occlusion system and/or proteins that are responsible for maintaining the structure of the chromosome. The antimicrobial compounds are useful to treat bacterial infections as well as to inhibit bacterial growth.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: December 26, 2017
    Assignee: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Douglas Benjamin Weibel, Katherine Ann Hurley, Katherine Cassidy Faulkner
  • Patent number: 9458101
    Abstract: The invention relates to colchicine derivatives, methods and uses thereof for treatment of cancer.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 4, 2016
    Assignee: NATIONAL RESEARCH COUNCIL OF CANADA
    Inventors: Jack Tuszynski, Jonathan Y. Mane, John Torin Huzil, Boguslaw Tomanek, Dorota Bartusik
  • Patent number: 9029589
    Abstract: A phenyl alkyl carbamate derivative compound and a pharmaceutical composition containing the compound are provided. More specifically, the phenyl alkyl carbamate derivative compound and a pharmaceutically acceptable salt thereof, a composition for muscle relaxation containing the phenyl alkyl carbamate derivative compounds and/or pharmaceutically acceptable salt thereof as an active ingredient, and a method of muscle relaxation comprising administering a pharmaceutically effective amount of the phenyl alkyl carbamate derivative compound and/or a pharmaceutically acceptable salt thereof to a subject in need of to a subject in need of, are provided.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: May 12, 2015
    Assignee: Bio-Pharm Solutions Co., Ltd.
    Inventor: Yong Moon Choi
  • Publication number: 20150065508
    Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
    Type: Application
    Filed: March 26, 2014
    Publication date: March 5, 2015
    Applicant: ABBVIE INC.
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Vince S. Yeh
  • Publication number: 20140349927
    Abstract: Methods for treating individuals suffering from inflammation, specifically systemic inflammation including septic shock and inflammatory conditions affecting the gastrointestinal, myocardial and endocrine systems with ladostigil.
    Type: Application
    Filed: August 6, 2014
    Publication date: November 27, 2014
    Inventor: Marta Weinstock-Rosin
  • Patent number: 8859629
    Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
    Type: Grant
    Filed: April 26, 2011
    Date of Patent: October 14, 2014
    Assignee: Synaffix B.V.
    Inventors: Floris Louis van Delft, Floris Petrus Johannes Theodorus Rutjes, Frederik Jan Dommerholt
  • Publication number: 20140275091
    Abstract: Provided herein is a pharmaceutical formulation comprising a GGA derivative in the form of an eye drop. Also provided herein are methods of treating neural diseases or disorders by administering such pharmaceutical formulations.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Hiroaki Serizawa, Tilmann M. Brotz
  • Publication number: 20140121187
    Abstract: Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: May 1, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Ihl Young Choi, Hae Soo Kim, Pil Ho Kim, Soo Bong Han, Johan Neyts, Hendrik Jan Thibaut
  • Patent number: 8697743
    Abstract: The present invention is directed to antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs and the preparation of nanometer-sized camptothecin prodrugs. Methods of synthesizing the antioxidant derivatives of camptothecin and antioxidant derivatives of camptothecin analogs, spontaneous emulsification or nanoprecipitation thereof to produce antioxidant camptothecin nanosphere prodrugs and their use in treating cancerous diseases are also provided. A further aspect of this invention is the use of these antioxidant camptothecin nanosphere prodrugs for the preparation of delivery devices of other pharmaceuticals and/or drugs. Additionally, methods of treating cancer with the camptothecin and antioxidant derivatives of camptothecin analogs, and nanometer-sized camptothecin prodrugs are also provided.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: April 15, 2014
    Assignee: Cedars-Sinai Medical Center
    Inventors: John S. Yu, Bong Seop Lee
  • Patent number: 8685936
    Abstract: The invention relates to prodrugs of hydroxyl-substituted adamantane compounds, pharmaceutical compositions thereof, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: April 1, 2014
    Assignee: Apogee Biotechnology Corporation
    Inventors: Charles D. Smith, Yan Zhuang, Lynn W. Maines
  • Publication number: 20140024708
    Abstract: The present invention relates to compounds having the following structure: wherein R is H or OH and X+ is protonated metformin, protonated arginine, protonated lysine and protonated meglumine. The invention also relates to intermediates used in the preparation of such compounds, processes for the preparation of such compounds and intermediates, pharmaceutical compositions comprising such compounds and the methods of treatment using such compounds as antidiabetic, antiobesity, and antisarcopenia agents.
    Type: Application
    Filed: April 17, 2013
    Publication date: January 23, 2014
    Inventors: Banavara L. Mylari, G. Alexander Fleming
  • Patent number: 8609719
    Abstract: A method for treating an individual who has been identified as having Alzheimer's disease by administering orally to the individual a therapeutically effective amount of ladostigil or a pharmaceutically active salt thereof, wherein the therapeutically effective amount is 70 mg per day, 140 mg per day, or 200 mg per day. Also, a unit dosage form of ladostigil or a pharmaceutically active salt thereof in an amount of 50 mg, 70 mg, 80 mg or 100 mg.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: December 17, 2013
    Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem, Technion Research and Development Foundation Ltd.
    Inventors: Victor Piryatinsky, Bronka Cohen, David Lerner, Dalia Pinkert, Istvan Miskolczi, Yaacov Herzig, Hugo Gottlieb, Marta Weinstock-Rosin
  • Publication number: 20130237573
    Abstract: A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.
    Type: Application
    Filed: November 15, 2011
    Publication date: September 12, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventors: Bruce Anthony Dressman, Mark Donald Chappell, Adam Michael Fivush, Charles Howard Mitch, Paul Leslie Ornstein, Eric George Tromiczak, Tatiana Natali Vetman
  • Publication number: 20130184238
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 18, 2013
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • Publication number: 20130165509
    Abstract: A phenyl alkyl carbamate derivative compound and a pharmaceutical composition containing the compound are provided. More specifically, the phenyl alkyl carbamate derivative compound and a pharmaceutically acceptable salt thereof, a composition for muscle relaxation containing the phenyl alkyl carbamate derivative compounds and/or pharmaceutically acceptable salt thereof as an active ingredient, and a method of muscle relaxation comprising administering a pharmaceutically effective amount of the phenyl alkyl carbamate derivative compound and/or a pharmaceutically acceptable salt thereof to a subject in need of to a subject in need of, are provided.
    Type: Application
    Filed: December 27, 2012
    Publication date: June 27, 2013
    Applicant: Bio-Pharm Solutions Co., Ltd.
    Inventor: Bio-Pharm Solutions Co., Ltd.
  • Publication number: 20130150438
    Abstract: The subject invention provides a method of preventing a neurodegenerative disease in a subject or oxidative stress in the brain of a subject, comprising administering to the subject a less than cholinesterase-inhibitory amount or a less than monoamine oxidase-inhibitory amount of R(+)-6-(N-methyl,N-ethyl-carbamoyloxy)-N?-propargyl-1-aminoindan or a salt thereof effective to prevent the neurodegenerative disease or oxidative stress in the subject.
    Type: Application
    Filed: February 5, 2013
    Publication date: June 13, 2013
    Applicants: TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD., Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Yissum Research Development Company of the Hebrew University of Jerusalem, Technion Research and Development Foundation Ltd.
  • Publication number: 20130137710
    Abstract: The present invention relates to the cosmetic, dermatological or therapeutic use of certain cyclohexyl carbamate compounds of formula (I) given below, preferably as anti-cellulite actives.
    Type: Application
    Filed: May 25, 2010
    Publication date: May 30, 2013
    Applicant: SYMRISE AG
    Inventors: Imke Meyer, Heiko Oertling, Nadine Hillebrand, Claudia Gömann, Rahim Brodhage
  • Publication number: 20130137763
    Abstract: The invention relates to fused cyclooctyne compounds, and to a method for their preparation. The invention also relates to a conjugate wherein a fused cyclooctyne compound according to the invention is conjugated to a label, and to the use of these conjugates in bioorthogonal labeling, imaging and/or modification, such as for example surface modification, of a target molecule. The invention further relates to a method for the modification of a target molecule, wherein a conjugate according to the invention is reacted with a compound comprising a 1,3-dipole or a 1,3-(hetero)diene.
    Type: Application
    Filed: April 26, 2011
    Publication date: May 30, 2013
    Inventors: Floris Louis van Delft, Floris Petrus Johannes Theodorus Rutjes, Frederik Jan Dommerholt
  • Publication number: 20130137720
    Abstract: The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an ?-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an ?-ketoglutarate mimic.
    Type: Application
    Filed: November 30, 2012
    Publication date: May 30, 2013
    Applicant: The Regents of the University of Colorado, a body corporated
    Inventors: Xiang Wang, Wenqing Xu
  • Patent number: 8420696
    Abstract: The subject invention provides a method of preventing a neurodegenerative disease in a subject or oxidative stress in the brain of a subject, comprising administering to the subject a less than cholinesterase-inhibitory amount or a less than monoamine oxidase-inhibitory amount of R(+)-6-(N-methyl,N-ethyl-carbamoyloxy)-N?-propargyl-1-aminoindan or a salt thereof effective to prevent the neurodegenerative disease or oxidative stress in the subject.
    Type: Grant
    Filed: December 11, 2006
    Date of Patent: April 16, 2013
    Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem, Technion Research and Development Foundation Ltd.
    Inventors: Marta Weinstock-Rosin, Shai Shoham
  • Publication number: 20130045978
    Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
    Type: Application
    Filed: June 22, 2012
    Publication date: February 21, 2013
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, Jyoti R. Patel, Qi Shuai, James T. Link, Jeffrey J. Rohde, Jurgen Dinges, Bryan K. Sorensen, Martin Winn, Hong Yong, Vince S. Yeh
  • Publication number: 20130011417
    Abstract: The present invention relates to colchicine derivatives expressed in chemical formula 1, or to pharmaceutically acceptable salts thereof, to a method for preparing said derivatives, and to a pharmaceutical composition comprising said derivatives. The colchicine derivatives according to the present invention exhibit superior immunomodulatory effects as compared with conventional immunomodulators or colchicines, and therefore can be valuably used as an immunomodulator for modulating an acute or chronic immune response in organ transplantation.
    Type: Application
    Filed: February 18, 2011
    Publication date: January 10, 2013
    Inventors: Duck Jong Han, Sung-eun Yoo, Jeehee Suh
  • Patent number: 8314217
    Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: December 8, 2010
    Date of Patent: November 20, 2012
    Assignee: Theravance, Inc.
    Inventor: Martin S. Linsell
  • Publication number: 20120058199
    Abstract: The present invention provides the use of surface active proteins, especially class I and class II hydrophobins, in topically applied pharmaceutical formulations. The invention is particularly directed to topically applied pharmaceutical products for enhancing the penetration to achieve a transungual delivery of a prophylactically and/or therapeutically effective amount of an active ingredient (drug) to a patient (including animals and humans) into and/or through a nail, of the animal or human body, in order to treat one or more of a variety of diseases or disorders. Related embodiments of the invention are also disclosed.
    Type: Application
    Filed: February 19, 2010
    Publication date: March 8, 2012
    Applicant: BASF SE
    Inventors: Andreas Buthe, Andreas Hafner, Franz Kaufmann, Babette Fiedler, Guido Meurer, Gordon Bradley
  • Publication number: 20120058966
    Abstract: The invention relates to prodrugs of hydroxyl-substituted adamantane compounds, pharmaceutical compositions thereof, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
    Type: Application
    Filed: March 12, 2010
    Publication date: March 8, 2012
    Applicant: APOGEE BIOTECHNOLOGY CORPORATION
    Inventors: Charles D. Smith, Yan Zhuang, Lynn W. Maines
  • Publication number: 20120028982
    Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration. A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.
    Type: Application
    Filed: October 7, 2011
    Publication date: February 2, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Akito YASUHARA, Kazunari Sakagami, Hiroshi Ohta, Atsuro Nakazato
  • Publication number: 20120004232
    Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.
    Type: Application
    Filed: September 8, 2011
    Publication date: January 5, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Akito YASUHARA, Kazunari SAKAGAMI, Hiroshi OHTA, Atsuro NAKAZATO
  • Publication number: 20110301234
    Abstract: The invention relates to a pharmaceutical composition of R(+)-6-(N-methyl,N-ethyl-carbamoyloxy)-N?-propargyl-1-aminoindan ½ tartrate, at least one pharmaceutically acceptable excipient and up to 5% by weight of the composition of water. The composition is typically in a solid oral form which upon administration to a human subject provides a maximum blood plasma concentration of R(+)-6-(N-methyl,N-ethyl-carbamoyloxy)-N?-propargyl-1-aminoindan of at least 0.7 nmol/mL.
    Type: Application
    Filed: August 17, 2011
    Publication date: December 8, 2011
    Inventors: Daniella Licht, Ioana Lovinger, Fanny Caciularu, Adrian Gilbert
  • Patent number: 8039674
    Abstract: Provided are: a compound represented by formula (I): (wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocyclic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, in which when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt thereof; an N-oxide form thereof; a solvate thereof, a prodrug thereof; and a medicament which includes those. The compound represented by formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: October 18, 2011
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hiromu Habashita, Shinji Nakade
  • Patent number: 8030518
    Abstract: This invention is directed to compounds of formula I, where G is —O—, —S—, —C(g1)(g2)-, or —NH—, and n=1, 2, or 3. Such compounds modulate potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders which are affected by modulation of potassium ion channels. One such condition is seizure disorders.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: October 4, 2011
    Assignee: Valeant Pharmaceuticals International
    Inventors: Huanming Chen, Jianlan Song, Jean-Michel Vernier, Jim Zhen Wu
  • Patent number: 8022104
    Abstract: Disclosed are formulations of ladostigil tartrate, including pharmaceutical compositions, process for the manufacture, and use thereof.
    Type: Grant
    Filed: February 24, 2006
    Date of Patent: September 20, 2011
    Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem, Technion Research and Development Foundation Ltd.
    Inventors: Daniella Licht, Ioana Lovinger, Fanny Caciularu, Adrian Gilbert
  • Publication number: 20110207812
    Abstract: This invention provides compounds of formula I where Ar1 is a 5- to 10-member mono- or bicyclic aromatic group, optionally substituted; where the —NR3R4 group is situated ortho to the NHC(?X) group; n=1 or 2; X=O or S; Y is O or S; and q=1 or 0. The invention also provides pharmaceutical compositions comprising compounds of formula I and/or salts, esters, and prodrugs thereof. These compounds modulate the activation and inactivation of potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders—such as seizure disorders—which are affected by modulation of potassium ion channels.
    Type: Application
    Filed: April 29, 2011
    Publication date: August 25, 2011
    Inventors: Huanming Chen, Jean-Michel Vernier
  • Publication number: 20110130453
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: March 25, 2009
    Publication date: June 2, 2011
    Applicant: AMIRA PHARMACEUTICALS, INC.
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Yen Pham Truong, Thomas Jon Seiders
  • Publication number: 20110130430
    Abstract: The present invention concerns polymeric material containing at least an embedded insecticidally active ingredient and an additive, which are released at room temperature. It similarly concerns materials produced from this polymer, for example in the form of self-supporting film/sheet, threads, wovens, fabrics, textiles, nets, curtains and pellets. The invention further concerns processes for producing such polymeric material and also the use of the self-supporting film/sheet, threads, wovens, fabrics, textiles and nets and curtains produced from the material for protecting humans, animals and plants and buildings, machines and packaging against arthropods, particularly for controlling insects.
    Type: Application
    Filed: April 1, 2009
    Publication date: June 2, 2011
    Applicant: Bayer CropScience AG
    Inventors: Rainer Sonneck, Thomas Böcker, Karin Horn, Guenther Nentwig, Maren Heinemann, Thomas König
  • Publication number: 20100273739
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: February 16, 2010
    Publication date: October 28, 2010
    Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
  • Publication number: 20100144868
    Abstract: Disclosed are novel hybrid compounds having a fullerene core residue, one or more bioavailability enhancing moieties and one or more glutamate receptor ligand residues, whereby the bioavailability enhancing moiety allow the compound to reach an effective concentration in physiological media and pass the blood-brain barrier, as defined in the specification. Also disclosed are pharmaceutical compositions containing these hybrid compounds and uses thereof as antioxidants and/or neuroprotective agents for the treatment of medical conditions associated with oxidative stress and/or neural damage, such as, for example, neurological diseases, disorders and trauma, and hence in the treatment of CNS-associated diseases, disorders and trauma, as well as to uses thereof as antiviral, antibacterial, antiglycemic, antiarrhythmic, antidepressant and antitumor agents.
    Type: Application
    Filed: January 22, 2006
    Publication date: June 10, 2010
    Applicants: Ramot At Aviv University Ltd., The Brigham and Women's Hospital Inc.
    Inventors: Michael Gozin, Howard L. Weiner, Alon Monsonego, Amnon Bar-Shir, Yoni Engel, Dan Frenkel
  • Publication number: 20100093848
    Abstract: A method for treating an individual who has been identified as having Alzheimer's disease by administering orally to the individual a therapeutically effective amount of ladostigil or a pharmaceutically active salt thereof, wherein the therapeutically effective amount is 70 mg per day, 140 mg per day, or 200 mg per day. Also, a unit dosage form of ladostigil or a pharmaceutically active salt thereof in an amount of 50 mg, 70 mg, 80 mg or 100 mg.
    Type: Application
    Filed: October 20, 2009
    Publication date: April 15, 2010
    Inventors: Victor Piryatinsky, Bronka Cohen, David Lerner, Dalia Pinkert, Istvan Miskolczi, Yaacov Herzig, Hugo Gottlieb, Marta Weinstock-Rosin
  • Patent number: 7655695
    Abstract: Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.
    Type: Grant
    Filed: August 3, 2006
    Date of Patent: February 2, 2010
    Assignee: The Regents of The University of California
    Inventors: Trevor C. McMorris, Michael J. Kelner
  • Publication number: 20090306202
    Abstract: The present invention is directed to D-homoandrosta-17-yl-carbamate derivatives as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: May 15, 2006
    Publication date: December 10, 2009
    Inventors: Amjad Ali, Mark L. Greenlee, Carol A. McVean, Robert S. Meissner, Gayle E. Taylor
  • Patent number: 7625946
    Abstract: This invention provides compounds having the structure: wherein R1 is methyl and R2 is H, or R1 is ethyl and R2 is hydroxymethyl; R3 is H or propargyl; and R4 is either H or t-butyloxycarbonyl; or an enantiomer or a pharmaceutically acceptable salt thereof. This invention further provides the use of a therapeutically effective amount of such compounds to treat a subject afflicted with a psychiatric disorder, Parkinson's disease, Alzheimer's disease, dementia, or a neurological disorder.
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: December 1, 2009
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Victor Piryatinsky, Bronka Cohen, David Lerner, Dalia Pinkert, Istvan Miskolczi, Yaacov Herzig, Hugo Gottlieb
  • Patent number: 7618999
    Abstract: The present invention relates to a process of obtaining taxosteroids and precursors thereof from the hydrindane bicyclic ring system. The compounds have a tetracyclic system which combines the structural characteristics of taxanes, such as the bicyclo[5.3.1]undecane system (cycles A and B), fused to a six-membered ring (C), and of steroids, such as the CD bicycle, the A ring and the side chain (Sc). The process of preparing the compounds and their application as compositions with pharmacological properties of interest are described.
    Type: Grant
    Filed: July 2, 2004
    Date of Patent: November 17, 2009
    Assignee: Universidade de Santiago de Compostela
    Inventors: Juan Granja Guillán, Luis Castedo Expósito, Rebeca García Fandiño
  • Publication number: 20090275653
    Abstract: The invention provides for solid state chemistry of ladostigil tartrate, particularly polymorphic forms of ladostigil tartrate, and processes for the preparation thereof.
    Type: Application
    Filed: May 27, 2009
    Publication date: November 5, 2009
    Inventors: Judith ARONHIME, Eliezer Bahar, Anton Frenkel, Ronen Gottesfeld, Amir Gold, Tamas Koltai
  • Patent number: 7560483
    Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
    Type: Grant
    Filed: June 21, 2005
    Date of Patent: July 14, 2009
    Assignee: XenoPort, Inc.
    Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou