Polycyclo-carbocyclic Ring System Having At Least Three Cyclos Patents (Class 544/380)
  • Publication number: 20150119373
    Abstract: The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
    Type: Application
    Filed: April 19, 2013
    Publication date: April 30, 2015
    Inventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Mamnoor Prem Kumar, Kasireddy Bhaskar Reddy, Mogili Narsingam, Mukkera Venkati, Lanka VL Subrahmanyam, Ravi Mallikarjun Reddy
  • Publication number: 20140343064
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-substituted oleanolic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 20, 2014
    Applicant: Hanghzhou Bensheng Pharmaceutical Co., Ltd
    Inventors: Rongzhen Xu, Frank Rong, Hongxi Lai, Fuwen Xie
  • Publication number: 20140329834
    Abstract: The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.
    Type: Application
    Filed: July 13, 2012
    Publication date: November 6, 2014
    Applicants: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard College
    Inventors: James Cunningham, Kyungae Lee, Tao Ren, Kartik Chandran
  • Publication number: 20140243527
    Abstract: The present invention provides a method of purifying betulonic acid contained the reaction product of organic synthesis of a Jones oxidation reagent and betulin extracted from the bark of a birch, a method of preparing a piperazine betulonic acid amide derivative, which is used as a chemical having an antibacterial function, using the high-purity betulonic acid obtained by the purification method and a derivative prepared by this method, a method of purifying a Boc-lysinated betulonic acid monomer ester contained in the reaction product of organic synthesis of lysine and the high-purity betulonic acid (starting material) obtained by the purification method, and a method of purifying Boc-lysinated betulonic acid contained in the reaction product of hydrolysis of the high-purity Boc-lysinated betulonic acid monomer ester.
    Type: Application
    Filed: June 29, 2012
    Publication date: August 28, 2014
    Applicant: KOREA INSTITUTE OF ENERGY RESEARCH
    Inventors: Kuck-Tack Chue, Tae-Hwan Kim, Leonid Ten
  • Publication number: 20140228375
    Abstract: The present invention involves new and original sigma receptors ligands: (Mono-or dialkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or diastereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Asteinizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, antimetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotective and cytoregenerative activity against the cytodegenerative diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: August 14, 2014
    Applicant: Anavex Life Sciences Corp.
    Inventor: Alexandre Vamvakides
  • 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: 20140178374
    Abstract: The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.
    Type: Application
    Filed: August 17, 2012
    Publication date: June 26, 2014
    Applicants: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, EMORY UNIVERSITY
    Inventors: Xingming Deng, Jia Zhou, Chunyong Ding
  • Patent number: 8691977
    Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 8, 2014
    Assignee: Neupharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Patent number: 8536182
    Abstract: The present invention relates to novel benzylpiperazine derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: September 17, 2013
    Assignee: Glaxo Group Limited
    Inventors: Christopher Norbert Johnson, David Timothy Macpherson, Steven James Stanway, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway
  • Patent number: 8530465
    Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: September 10, 2013
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Publication number: 20130210785
    Abstract: This disclosure relates to progesterone derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation resulting from traumatic brain injury or stroke.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 15, 2013
    Applicant: EMORY UNIVERSITY
    Inventor: Emory University
  • Publication number: 20130184263
    Abstract: The present invention relates to compounds characterized by having a structure according to the following Formula I: or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 18, 2013
    Applicant: GlaxoSmithKline LLC
    Inventor: GlaxoSmithKline LLC
  • Patent number: 8415354
    Abstract: The present invention relates to inhibitors of 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: Grant
    Filed: February 20, 2009
    Date of Patent: April 9, 2013
    Assignee: Abbott Laboratories
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, James T. Link, Yixian Chen, Hwan-soo Jae, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Qi Shuai, Bryan K. Sorensen, Martin Winn, Dariusz Wodka, Hong Yong
  • Publication number: 20120283201
    Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: July 12, 2012
    Publication date: November 8, 2012
    Applicants: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Y. Ismail, Todd Bowser, Jimmy Dumornay, Glen Rennie, Gui Liu, Darrell J. Koza, Paul Sheahan, Karen Stapleton, Paul Hawkins, Beena Bhalie, Atul K. Verma, Laura Honeyman, Tadeusz Warchol, David Messersmith
  • Patent number: 8304415
    Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: November 6, 2012
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Publication number: 20120135968
    Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.
    Type: Application
    Filed: May 7, 2010
    Publication date: May 31, 2012
    Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus Rönn
  • Publication number: 20120115818
    Abstract: Efficient method for preparing the enone intermediate (VII) used in the synthesis of tetracyclines derivatives. In particular, the invention provides a synthesis which allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
    Type: Application
    Filed: April 30, 2010
    Publication date: May 10, 2012
    Applicant: President and Felows of Harvard College
    Inventors: Andrew G. Myers, David A. Kummer, Derun Li, Evan Hecker, Amelie Dion, Peter M. Wright
  • Publication number: 20120052019
    Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.
    Type: Application
    Filed: August 22, 2011
    Publication date: March 1, 2012
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20120046291
    Abstract: The present invention concerns novel pharmaceutically active triterpene derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (HIV).
    Type: Application
    Filed: November 2, 2007
    Publication date: February 23, 2012
    Inventors: Theodore J. Nitz, Christian Montalbetti, Richard Mears, Xinjie Gai, Edward Glenn
  • Publication number: 20110312965
    Abstract: The present invention relates to new retinoid derivatives of formula I and to pharmaceutical compositions containing them for the treatment of patients affected by pathologies such as arthritic conditions, tumours, metastatic cancer, diabetic retinopathy, psoriasis, chronic inflammatory diseases or atherosclerosis.
    Type: Application
    Filed: December 21, 2009
    Publication date: December 22, 2011
    Inventors: Walter Cabri, Giuseppe Giannini, Gianfranco Battistuzzi, Domenico Alloatti, Claudio Pisano, Sabrina Dallavalle, Tiziana Brunetti
  • Publication number: 20110245501
    Abstract: The present invention relates to substituted tetracycline compounds and related methods for increasing the antifungal activity of an antifungal agent. The methods include administering to a subject an effective amount of a substituted tetracycline compound in combination with an antifungal agent such that the subject is treated for the fungal associated disorder.
    Type: Application
    Filed: June 14, 2011
    Publication date: October 6, 2011
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventors: Michael Draper, Mark L. Nelson
  • 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: 20110077251
    Abstract: The invention relates to 17? lupane derivatives of formula (I): wherein R1 and X are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infection by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
    Type: Application
    Filed: August 16, 2010
    Publication date: March 31, 2011
    Inventors: Christophe Moinet, Bingcan Liu, Liliane Halab, Nathalie Turcotte, Real Denis, Carl Poisson, Paul Nguyen-Ba, Monica Bubenik, Laval Chan Chun Kong
  • Patent number: 7893263
    Abstract: This invention relates to novel corosolic acid analogs of the formula I, wherein R1, R2, R3, R4 and R5 are described herein. These compounds exhibit good hypoglycemic and 5-lipoxygenase inhibitory activities. They also inhibit tumour growth. Pharmaceutical compositions containing known adjutants and the title compounds are also within the scope of this invention.
    Type: Grant
    Filed: July 8, 2004
    Date of Patent: February 22, 2011
    Assignee: Laila Nutraceuticals
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti, Venkateswarlu Somepalli, Venkateswara Rao Chirravuri
  • Patent number: 7888355
    Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: February 15, 2011
    Assignee: Burnham Institute for Medical Research
    Inventors: Ze′ev A. Ronai, Anindita Bhoumik, Nicholas D. P. Cosford, Russell Dahl
  • Patent number: 7880001
    Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: February 1, 2011
    Assignee: Abbott Laboratories
    Inventors: James T. Link, Yixian Chen, Hwan-Soo Jae, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Qi Shuai, Bryan K. Sorensen, Martin Winn, Dariusz Wodka, Hong Yong
  • Publication number: 20110015196
    Abstract: The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
    Type: Application
    Filed: July 2, 2010
    Publication date: January 20, 2011
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi PARTHASARADHI REDDY, Vedula MANOHAR SHARMA, Kura RATHNAKAR REDDY, Musku MADHANMOHAN REDDY, Nelli YELLA REDDY, Lanka VL SUBRAHMANYAM
  • Patent number: 7723337
    Abstract: The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof which possess CSF-1R kinase inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
    Type: Grant
    Filed: September 15, 2008
    Date of Patent: May 25, 2010
    Assignee: AstraZeneca AB
    Inventors: Leslie Dakin, Claude Afona Ogoe, David Scott, XiaoLan Zheng
  • Patent number: 7582639
    Abstract: Disclosed is a series of N-deacetylthiocolchicine derivatives of formula I in which: the linker is a bivalent straight or branched C1-C8 alkyl residue, C3-C8 cycloalkyl, a phenylene or heterocyclic C4-C6 ring; the G1 and G2 junctions, which can be the same or different, are —CO—, —CONH—, —CR2— groups in which R2 is hydrogen or a straight C1-C4 alkyl residue, or the G1-linker-G2 group is the —CO— group. The compounds of formula I have antiproliferative, antiinflammatory, antiarthritic and antiviral activity.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: September 1, 2009
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Gabriele Fontana
  • Publication number: 20090061528
    Abstract: Novel fluorescent dyes are disclosed for use in analyte detection. In particular, mono- and bis-substituted HPTS dyes and methods of making them are provided.
    Type: Application
    Filed: August 6, 2008
    Publication date: March 5, 2009
    Applicant: GLUMETRICS INC.
    Inventor: JEFF T. SURI
  • Publication number: 20090054438
    Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
    Type: Application
    Filed: August 15, 2008
    Publication date: February 26, 2009
    Applicant: Burnham Institute for Medical Research
    Inventors: Ze'ev A. Ronai, Anindita Bhoumik, Nicholas D.P. Cosford, Russell Dahl
  • Patent number: 7495014
    Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
    Type: Grant
    Filed: January 29, 2004
    Date of Patent: February 24, 2009
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven M. Ronkin, Dean Stamos, Emanuele Perola, Tiensheng Wang, Arnaud LeTiran, Joseph Drumm
  • Publication number: 20080287442
    Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-8)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.
    Type: Application
    Filed: January 11, 2007
    Publication date: November 20, 2008
    Applicant: Nabriva Therapeutics Forschungs GmbH
    Inventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
  • Publication number: 20080261985
    Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.
    Type: Application
    Filed: November 16, 2007
    Publication date: October 23, 2008
    Inventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
  • Publication number: 20080255346
    Abstract: A mercury selective fluorescent chemosensor for detecting mercury ions (Hg2+) by a compound represented by formula 1 is provided. A novel fluorescent sensitive compound prepared by introducing two aminopyrene functions as a fluorescent sensitive moiety into a binding site of the compound represented by the formula 1, is used for selectively detecting mercury ions (Hg2+) is also provided. The mercury selective fluorescent sensitive chemosensor is a switch type chemosensor having ON-OFF-type Hg2+-selective fluorescence quenching behavior and is not affected by other coexistent metal ions. The changes in fluorescence of the compounds represented by formula 1 were analyzed by ratiometric approach using monomer and excimer emissions of the pyrene fluorophore to selectively signal the concentration of mercury ions (Hg2+). The chemosensor can detect mercury ions in a micromolar unit even in a solution including an excess of water.
    Type: Application
    Filed: October 9, 2007
    Publication date: October 16, 2008
    Applicant: Chung-Ang University Industry-Academy Cooperation Foundation
    Inventors: Suk-Kyu Chang, Jun Soo Kim, Myung Gil Choi, Ki Cheol Song, Sangdoo Ahn
  • Patent number: 7427632
    Abstract: Compounds of formula (I) in which R1, n, Z, R3 and R4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of thrombotic disorders.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: September 23, 2008
    Assignee: Eli Lilly and Company
    Inventors: Scott Martin Sheehan, Brian Morgan Watson, John Walter Liebeschuetz
  • Publication number: 20080214572
    Abstract: This invention concerns novel tetracyclic tetrahydrofuran derivatives containing a cyclic amine side chain with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors, 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 a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof, and a quaternary ammonium salt thereof, wherein all substituents are defined as in claim 1.
    Type: Application
    Filed: May 17, 2006
    Publication date: September 4, 2008
    Inventors: Francisco Javier Fernandez-Gadea, Jose Ignacio Andres-Gil, Andres Avelino Trabanco-Suarez, Jose Maria Cid-Nunez, Antonius Adrianus Hendrikus Petrus Megens
  • Patent number: 7384943
    Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I) wherein X is N; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycoalkyl or (CH2)n-aryl, wherein aryl is a heteromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or racemates in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.
    Type: Grant
    Filed: June 5, 2006
    Date of Patent: June 10, 2008
    Assignee: AstraZeneca AB
    Inventors: Stefan Berg, Martin Nylöf, Svante Ross, Seth-Olov Thorberg
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7326696
    Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.
    Type: Grant
    Filed: December 15, 2003
    Date of Patent: February 5, 2008
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Kwasi Ohemeng, Roger Frechette, Paul Abato, Victor Amoo, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Laura Honeyman, Mohamed Y. Ismail, Oak Kim, Rachid Mechiche, N. Laxma Reddy, Atul K. Verma, Peter Viski, Tadeusz Warchol, Ivan Yanachkov
  • Patent number: 7271168
    Abstract: The invention provides compounds of formula (1) wherein X, R1 and R2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety and bipolar disorders.
    Type: Grant
    Filed: November 8, 2002
    Date of Patent: September 18, 2007
    Assignee: Novartis AG
    Inventors: Thomas J. Troxler, Daniel Hoyer
  • Patent number: 6916816
    Abstract: Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than hydrogen; A is CH2, SO2 or C?O; X is CO2H, PO3H2, PO2H2, PO2HR5, PO2HOR5, SO3H, SO2H, or tetrazole; and R1, R2, R3, R4 and R5 are independently selected from H, alkyl, alkenyl, alkynyl, aryl and aralkyl; or a pharmaceutically acceptable acid salt or base addition salt or an in vivo hydrolysable ester or amide thereof.
    Type: Grant
    Filed: December 18, 2000
    Date of Patent: July 12, 2005
    Assignees: The Board of Regents of the University of Nebraska, The University of Bristol
    Inventors: Daniel T. Monaghan, David E. Jane, Heong Wai Tse
  • Patent number: 6916812
    Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: July 12, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Graham S. Poindexter, Guanglin Luo, Ling Chen
  • Patent number: 6906046
    Abstract: Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-? and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: June 14, 2005
    Assignee: Celltech R & D Inc.
    Inventors: Randy W. Jackson, Ihab Darwish, Ted A. Baughman, J. Jeffry Howbert
  • Patent number: 6858599
    Abstract: This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.
    Type: Grant
    Filed: December 27, 2001
    Date of Patent: February 22, 2005
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Kousuke Harada, Ikuya Shiromizu, Takafumi Mukaihira
  • Patent number: 6846925
    Abstract: The invention related to colchinol derivatives of the formula (I): Wherein: R1; R2 and R3 are each independently hydroxy, phosphoryloxy (—OP3H2), C1-4alkoxy or an in vivo hydrolysable ester of hydroxy, with the proviso that at least 2 of R1, R2 and R3 are C1-4alkoxy; A is —CO—, —C(O)O—, —CON(R8)— (wherein R8 is hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl or hydroxyC1-3alkly); a is an integer from 1 to 4 inclusive; Ra and Rb are independently selected from hydrogen, hydroxy and amino; B is —O—, —CO—, N(R9)CO—, —CON(R9)—, —N(R9)C(O)O—, —N(R9)CON(R10)—, —N(R9)SO2—, —SO2N(R9)— or a direct single blond (wherein R9 and R10 are independently selected from hydrogen, C1-4alkyl, C1-3alkoxyC1-3alkyl, aminoC1-3alkyl and hydroxyC1-3alkyl); b is O or an integer from 1 to 4 inclusive, (provided that when b is O, B is a single direct bond); D is carboxy, sulpho, tetrazolyl, imidazolyl, phosphoryloxy, hydroxy, amino, N-(C1-4alkyl)amino, N,N-di(C1-3alkyl)amino, or of the formula —Y1(CH2)0R11 or —NHCH(R12)COOH; [wh
    Type: Grant
    Filed: November 12, 2003
    Date of Patent: January 25, 2005
    Assignee: Angiogene Pharmaceuticals Limited
    Inventor: Jean Claude Arnould
  • Patent number: 6831084
    Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection, the compounds having the structure: wherein X is —CH2— or a bond; Y is —(CH2)m— or —(CH2)—O—(CH2)—; m 0 or 1; n is 0 or 1; R1 and R2 are independently selected from optionally substituted aryl or heteroaryl; the optical isomers and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 6, 2000
    Date of Patent: December 14, 2004
    Assignee: Wyeth
    Inventors: Wayne E. Childers, Jr., Horace Fletcher, III, Magid A. Abou-Gharbia, John P. Yardley
  • Patent number: 6828324
    Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection. The compounds having the structure: wherein X is —CH2— or a bond; Y is —(CH2)m— or —(CH2)—O—(CH2)—; m 0 or 1; n is 0 or 1; R1 and R2 are independently selected from optionally substituted aryl or heteroaryl; the optical isomers and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 20, 2004
    Date of Patent: December 7, 2004
    Assignee: Wyeth
    Inventors: Wayne E. Childers, Jr., Horace Fletcher, III, Magid A. Abou-Gharbia, John P. Yardley
  • Patent number: 6821967
    Abstract: The present invention relates to substituted piperazine derivatives of general formula wherein Ra, Rb, Rc, Rf, Rg, X, m and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
    Type: Grant
    Filed: October 9, 2002
    Date of Patent: November 23, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
  • Patent number: 6818644
    Abstract: The present invention relates to substituted piperazine derivatives of general formula wherein Ra, Rb, Rc Rf, Rg and m, n and X are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyseride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
    Type: Grant
    Filed: July 1, 2002
    Date of Patent: November 16, 2004
    Assignee: Boehringer Ingelheim Pharm GmbH & Co, KG
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark