Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/375)
  • Patent number: 9111461
    Abstract: A kit for demonstrating or explaining the action of a mineral ion scavenger in an oral care composition. A method for demonstrating or explaining the action of a mineral ion scavenger in an oral care composition. A kit and/or method for providing perceptible confirmation of the action and/or effectiveness of an oral care composition comprising a mineral ion scavenger.
    Type: Grant
    Filed: April 2, 2012
    Date of Patent: August 18, 2015
    Assignee: The Iams Company
    Inventor: Melissa Leeann Campbell
  • Patent number: 9018213
    Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.
    Type: Grant
    Filed: July 31, 2012
    Date of Patent: April 28, 2015
    Assignees: Huazhong University of Science & Technology, NHWA Pharma. Corporation
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Minquan Yu, Yinli Qiu
  • Patent number: 8981131
    Abstract: The present invention provides compounds represented by formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: March 17, 2015
    Assignee: Piramal Enterprises Limited
    Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Patent number: 8912196
    Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: December 16, 2014
    Assignee: ATIR Holding S.A.
    Inventors: Vladimir Kogan, Lev Tabachnik
  • Publication number: 20140356417
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: June 12, 2014
    Publication date: December 4, 2014
    Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Patent number: 8790691
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: July 29, 2014
    Assignee: The University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20140176653
    Abstract: There is provided a compound represented by formula (1): in formula (1), L represents a divalent to tetravalent linking group; D represents a residue obtained by removing 1 to 5 hydrogen atoms from a compound represented by formula (2); m represents an integer of 1 to 10, however, each L may be the same with or different from every other L; n represents an integer of 2 to 10, however, each D may be the same with or different from every other D; and in formula (2), each of R4 to R24 independently represents a hydrogen atom or a substituent, provided that formula (2) has at least one or more ionic hydrophilic groups.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Applicant: FUJIFILM CORPORATION
    Inventors: Yoshihiko FUJIE, Keiichi TATEISHI, Clive Edwin FOSTER
  • Publication number: 20140171442
    Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.
    Type: Application
    Filed: July 31, 2012
    Publication date: June 19, 2014
    Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Miquan Yu, Yinli Qiu
  • Publication number: 20140166948
    Abstract: The present invention relates to compounds represented by the following Formula (II), Ring-A of Formula II can be, for example, an aryl group, and Q? and Q?? can each be independently selected from groups, such as, halogen, —OH, —CN, amine groups, amide groups, carboxylic acid ester groups, carboxylic acid groups, alkenyl groups, alkynyl groups, carbonate groups, sulfide groups, and sulfonic acid ester groups. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds such as represented by Formula II.
    Type: Application
    Filed: February 19, 2014
    Publication date: June 19, 2014
    Inventors: Meng He, Anil Kumar, Darrin R. Dabideen
  • Publication number: 20140154514
    Abstract: A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N3, —CN, —COOR?, —CCR?, —C(R?)C(R?)R?, —OCOR?, —OCOOR?, —SR?, —OSO2R??, and/or —CON(R?)R?, wherein each R? is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R?? is —CF3 or a perfluorinated alkyl group having from 2 to 18 carbon atoms. The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound.
    Type: Application
    Filed: February 7, 2014
    Publication date: June 5, 2014
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Terry A. Keller, II
  • Patent number: 8705160
    Abstract: A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N3, —CN, —COOR?, —CCR?, —C(R?)C(R?)R?, —OCOR?, —OCOOR?, —SR?, —OSO2R??, and/or —CON(R?)R?, wherein each R? is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R?? is —CF3 or a perfluorinated alkyl group having from 2 to 18 carbon atoms. The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: April 22, 2014
    Assignee: Transitions Optical, Inc.
    Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Terry A. Kellar, II
  • Publication number: 20140088078
    Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 27, 2014
    Applicant: ZAFGEN, Inc.
    Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
  • Publication number: 20140066451
    Abstract: The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.
    Type: Application
    Filed: November 4, 2013
    Publication date: March 6, 2014
    Applicant: BKG PHARMA APS
    Inventor: Birgit Kjaeldgaard GIWERCMAN
  • Patent number: 8647538
    Abstract: The present invention relates to photochromic compounds that include at least two photochromic moieties that are linked together by a multivalent linking group. The multivalent linking group can be selected so as to be flexible and/or substantially prevent electronic interaction between any two photochromic moieties through the multivalent linking group. The present invention also relates to photochromic compositions and articles that include at least a photochromic amount of one or more photochromic compounds of the present invention.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: February 11, 2014
    Assignee: Transitions Optical, Inc.
    Inventors: Yunyi Lu, Wenjing Xiao, Robert W. Walters, Feng Wang, M. Frank Haley, Jason R. Lewis, Anu Chopra, Beon-Kyu Kim, Huayun Yu
  • Patent number: 8545984
    Abstract: Described herein are compounds generally comprising an indeno[2?,3?:3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: October 1, 2013
    Assignee: Transitions Optical, Inc.
    Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Ruisong Xu
  • Patent number: 8518546
    Abstract: The present invention relates to compounds represented by the following Formula I, Ring-A of the Formula I can be, for example an aryl group, and L1 is a chiral or achiral lengthening group. The compound represented by Formula I can be a photochromic compound. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula I.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: August 27, 2013
    Assignee: Transitions Optical, Inc.
    Inventors: Meng He, Sujit Mondal, Darrin R. Dabideen, Anil Kumar, Xiao-Man Dai
  • Patent number: 8388872
    Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran of structural formulas I or II, having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: March 5, 2013
    Assignee: Transitions Optical, Inc.
    Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, Jr., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
  • Publication number: 20120264736
    Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.
    Type: Application
    Filed: October 6, 2011
    Publication date: October 18, 2012
    Applicant: Schering Corporation
    Inventors: Theodros Asberom, Thomas A. Bara, Chad E. Bennett, Duane A. Burnett, Mary Ann Caplen, John W. Clader, David J. Cole, Martin S. Domalski, Hubert B. Josien, Chad E. Knutson, Hongmei Li, Mark D. McBriar, Dmitri A. Pissarnitski, Li Qiang, Murali Rajagopalan, Thavalakulamgara K. Sasikumar, Jing Su, Haiqun Tang, Wen-Lian Wu, Ruo Xu, Zhiqiang Zhao
  • Publication number: 20120237591
    Abstract: Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.
    Type: Application
    Filed: May 8, 2012
    Publication date: September 20, 2012
    Applicant: The University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20120238563
    Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.
    Type: Application
    Filed: June 4, 2012
    Publication date: September 20, 2012
    Inventors: Jose Maria CID-NÚÑEZ, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Publication number: 20120200907
    Abstract: A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N3, —CN, —COOR?, —CCR?, —C(R?)C(R?)R?, —OCOR?, —OCOOR?, —SR?, —OSO2R??, and/or —CON(R?)R?, wherein each R? is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R?? is —CF3 or a perfluorinated alkyl group having from 2 to 18 carbon atoms. The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound.
    Type: Application
    Filed: April 20, 2012
    Publication date: August 9, 2012
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Terry A. Kellar, II
  • Patent number: 8222255
    Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: July 17, 2012
    Assignees: Merck Sharp & Dohme Corp., Scynexis, Inc.
    Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, legal representative, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
  • Patent number: 8211338
    Abstract: A photochromic compound is provided, which may be a pyran, an oxazine, or a fulgide. The photochromic compound has at least one substituent Q attached thereto, each Q independently being —N3, —CN, —COOR?, —CCR?, —C(R?)C(R?)R?, —OCOR?, —OCOOR?, —SR?, —OSO2R??, and/or —CON(R?)R?, wherein each R? is hydrogen, an unsubstituted or substituted alkyl group having from 1 to 18 carbon atoms; an unsubstituted or substituted aryl group, an unsubstituted or substituted alkene or alkyne group having from 2 to 18 carbon atoms, wherein the substituents are halo or hydroxyl and R?? is —CF3 or a perfluorinated alkyl group having from 2 to 18 carbon atoms The number, locations and nature of the constituents Q are dependent upon the structure of the photochromic compound.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: July 3, 2012
    Assignee: Transitions Optical, Inc
    Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Terry A. Kellar, II
  • Publication number: 20120132870
    Abstract: The present invention relates to indeno-fused naphthopyrans, and in particular indeno[2?,3?:3,4]naphtho[1,2-b]pyrans having certain groups bonded to the 3, 6, 7, 11, and 13 positions thereof. The indeno-fused naphthopyrans of the present invention have an ethylenically unsaturated group selected from (C1-C6 alkyl)acrylate and (C1-C6 alkyl)acrylamide, that is linked to the 11 position or 13 position thereof. The present invention also relates to photochromic articles and photochromic compositions containing such indeno-fused naphthopyrans.
    Type: Application
    Filed: December 15, 2011
    Publication date: May 31, 2012
    Applicant: TRANSITIONS OPTICAL INC.
    Inventors: Wenjing Xiao, Barry Van Gemert
  • Publication number: 20120122880
    Abstract: The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.
    Type: Application
    Filed: April 20, 2010
    Publication date: May 17, 2012
    Applicant: BKG PHARMA APS
    Inventor: Birgit Kjaeldgaard Giwercman
  • Publication number: 20120083488
    Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).
    Type: Application
    Filed: June 9, 2010
    Publication date: April 5, 2012
    Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
  • Patent number: 8147725
    Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: April 3, 2012
    Assignee: Transitions Optical, Inc
    Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank Molock, Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
  • Publication number: 20120071487
    Abstract: Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.
    Type: Application
    Filed: May 26, 2010
    Publication date: March 22, 2012
    Inventors: Vladimir Kogan, Lev Tabachnik
  • Publication number: 20120035170
    Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.
    Type: Application
    Filed: August 22, 2011
    Publication date: February 9, 2012
    Inventors: José Maria Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Patent number: 8101605
    Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds 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. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: January 24, 2012
    Assignee: Aquinox Pharmaceuticals Inc.
    Inventors: Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
  • Patent number: 8058427
    Abstract: Coumarin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, and X are defined herein. Also disclosed is a method for treating cancer with coumarin compounds.
    Type: Grant
    Filed: June 10, 2009
    Date of Patent: November 15, 2011
    Assignee: National Health Research Institutes
    Inventors: Hsing-Pang Hsieh, Jang-Yang Chang, Ching-Chuan Kuo, Yu-Sheng Chao
  • Publication number: 20110257399
    Abstract: A new generation of fluorescent ion indicators for measuring cytosolic concentrations of calcium. These new indicators emit in the red portion of the visible spectrum and are ratiometric. The ratiometry consists of shifting in the emission upon binding calcium when exciting with an argon laser at 488 nm. These indicators also show marked increases in red fluorescence when excited with visible light at longer wavelengths. Like all calcium indicators, they comprise the usual chelating portion based on BAPTA (Bis Amino Phenyl Tetraacetic Acid) and a fluorophore portion, either a seminaphthofluorescein/seminaphthorhodamine or dinaphthofluorescein, which enable ratiometry. Unlike other naphthofluoresceins, the pKa has been adjusted on the naphtho moiety to make it suitable for biological calcium measurements. The invention relates to the structures of the indicators and to the method of synthesizing these indicators.
    Type: Application
    Filed: October 18, 2010
    Publication date: October 20, 2011
    Inventors: Akwasi Minta, Pedro Rogelio Escamilla
  • Publication number: 20110251379
    Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.
    Type: Application
    Filed: March 3, 2011
    Publication date: October 13, 2011
    Applicant: Satori Pharmaceuticals, Inc.
    Inventors: Brian Scott Bronk, Wesley Francis Austin, Steffen Phillip Creaser, Mark A. Findeis, Nathan Oliver Fuller, Jed Lee Hubbs, Jeffrey Lee Ives, Ruichao Shen
  • Patent number: 8017617
    Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: December 12, 2008
    Date of Patent: September 13, 2011
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, Rick Lee, YongQi Mu
  • Publication number: 20110212955
    Abstract: The present invention relates to a new class of rosamine derivatives, in one embodiment, the compounds have the structure (I) or any pharmaceutically acceptable salt or solvate thereof, wherein: R1 represents aryl, Het1 or C1-6 alkyl, which latter group is optionally substituted by aryl or Het2; R2a and R2b together form C3.8 n-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo, C1-4 alkyl, C(O)OH and C(O)O—C1-4, alkyl and which alkylene group is optionally interrupted by X1; R3a and R3b together form C3-6 /7-alkylene, which alkylene group is optionally substituted by one or more substituents selected from halo.
    Type: Application
    Filed: July 2, 2009
    Publication date: September 1, 2011
    Applicant: CANCER RESEARCH INITIATIVES FOUNDATION
    Inventors: Hong Boon Lee, Kevin Burgess, Siang Hui Lim, Liangxing Wu
  • Publication number: 20110172225
    Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
    Type: Application
    Filed: September 25, 2008
    Publication date: July 14, 2011
    Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.
    Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
  • Publication number: 20110171736
    Abstract: The present invention provides novel reactive fluorescent compounds that incorporate stable isotopic (deuterium, 13-carbon, 15-nitrogen, 18-oxygen) substitutions. The invention includes the use of these compounds, in combination with non-isotopically substituted analogs, for the purification, identification and relative quantification of proteins, peptides, saccharides, metabolites, and other biologically important compounds by combining liquid chromatography (LC) and mass spectrometry (MS). Fluorescent labeling of target compounds in this manner provides orders-of-magnitude sensitivity enhancement over traditional stable isotope labels, and also affords the possibility of simultaneous multiplexed analysis due to the multiwavelength nature of different fluorophores.
    Type: Application
    Filed: November 11, 2010
    Publication date: July 14, 2011
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Brian AGNEW, Kyle Richard Gee
  • Publication number: 20110165225
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: May 26, 2009
    Publication date: July 7, 2011
    Inventors: Peter Cullis, Marcel Bally
  • Publication number: 20110143141
    Abstract: The present invention relates to compounds represented by the following Formula I, Ring-A of the Formula I can be, for example an aryl group, and L1 is a chiral or achiral lengthening group. The compound represented by Formula I can be a photochromic compound. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula I.
    Type: Application
    Filed: December 16, 2010
    Publication date: June 16, 2011
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Meng He, Sujit Mondal, Darrin R. Dabideen, Anil Kumar, Xiao-Man Dai
  • Publication number: 20110140056
    Abstract: The present invention relates to compounds represented by the following Formulas (I) and (II), Ring-A of Formulas I and II can be, for example, an aryl group, and Q? and Q?? can each be independently selected from groups, such as, halogen, —OH, —CN, amine groups, amide groups, carboxylic acid ester groups, carboxylic acid groups, alkenyl groups, alkynyl groups, carbonate groups, sulfide groups, and sulfonic acid ester groups. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula II.
    Type: Application
    Filed: December 16, 2010
    Publication date: June 16, 2011
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Meng He, Anil Kumar, Darrin R. Dabideen
  • Patent number: 7960385
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: June 14, 2011
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Publication number: 20110136802
    Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds 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. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
    Type: Application
    Filed: December 3, 2010
    Publication date: June 9, 2011
    Applicant: Aquinox Pharmaceuticals Inc.
    Inventors: Lloyd Mackenzie, Tom MacRury, Curtis Harwig, Jeremy Pettigrew, Noor Aini Bhatti, Sam Place, Paul Bird, Vladimir Khlebnikov, Rudong Shan
  • Publication number: 20110129678
    Abstract: Described herein are compounds generally comprising an indeno[2?,3?:3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.
    Type: Application
    Filed: December 16, 2010
    Publication date: June 2, 2011
    Applicant: Transitions Optical, Inc.
    Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Ruisong Xu
  • Patent number: 7923558
    Abstract: The invention relates to a method for obtaining pure tetrahydrocannabinol from reaction mixtures containing tetrahydrocannabinol compounds or from raw products containing tetrahydrocannabinol compounds. According to said method, the tetrahydrocannabinol compounds in the reaction mixture or in the raw product are converted into crystallisable derivatives, preferably using a suitable solvent, said derivatives are then crystallised and isolated, and the pure tetrahydrocannabinol compounds are then obtained from the crystallised derivatives. The invention also related to the use of compounds produced in this way for the production of a medicament for human therapy, and to the medicaments thus produced.
    Type: Grant
    Filed: July 19, 2004
    Date of Patent: April 12, 2011
    Assignee: Cilag Ltd.
    Inventors: Enver Arslantas, Ulrich Weigl
  • Patent number: 7915249
    Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Grant
    Filed: January 25, 2006
    Date of Patent: March 29, 2011
    Assignee: Janssen Pharmaceutical NV
    Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Publication number: 20110028444
    Abstract: The invention discloses the pharmaceutically acceptable salts of an optically active quinolone compound useful against infection, specifically the pharmaceutically acceptable salts of (S)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid. The pharmaceutically acceptable salts of the present invention are stable and have improved water solubility. They possess higher biological activity, less toxicity for kidney and no irritation to skin and muscle.
    Type: Application
    Filed: April 2, 2009
    Publication date: February 3, 2011
    Inventors: Mao Chen, Shaoxuan Zhu, Lizhen Zheng, Xuebin Liu, Yuping Wang, Shuwen Xu
  • Publication number: 20110009396
    Abstract: The present invention provides compounds represented by formula 1: wherein, R1 R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.
    Type: Application
    Filed: July 25, 2008
    Publication date: January 13, 2011
    Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Rada Dalal, Sapna Parikh, Aditi Amol Tannu
  • Publication number: 20100286152
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof,
    Type: Application
    Filed: June 5, 2008
    Publication date: November 11, 2010
    Applicant: Glaxo Group Limited
    Inventors: Giovanni Bernasconi, Steven Mark Bromidge, Andrew James Carpenter, Lucilla D'Adamo, Romano Di Fabio, Sebastien Guery, Francesca Pavone, Alfonso Pozzan, Marilisa Rinaldi, Fabio Maria Sabbatini, Yves St-Denis
  • Patent number: 7781476
    Abstract: Tetracyclic 3-substituted indoles having serotonin receptor affinity and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: August 24, 2010
    Assignee: Suven Life Sciences Limited
    Inventors: Venkata Satya Nirogi Ramakrishna, Vikas Shreekrishna Shirsath, Rama Sastri Kambhampati, Venkata Satya Veerabhadra Vadlamudi Rao, Venkateswarlu Jasti