Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/455)
  • Patent number: 10258636
    Abstract: Provided are novel prodrug salts of selective aquaporin inhibitors, their use as pharmaceuticals, and pharmaceutical compositions comprising them, and novel processes for their synthesis and novel intermediates for use in their synthesis. Also provided is use of a compound for the prophylaxis, treatment, and control of aquaporin-mediated conditions. Aquaporin inhibitors, e.g., inhibitors of AQP4 and/or AQP2, may be of utility in the treatment or control of diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord), hyponatremia, and excess fluid retention, as well as diseases such as epilepsy, retinal ischemia and other diseases of the eye, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines.
    Type: Grant
    Filed: October 24, 2017
    Date of Patent: April 16, 2019
    Assignee: AEROMICS, INC.
    Inventors: Marc F. Pelletier, Paul Robert McGuirk, George William Farr, Robert Zamboni, John Colucci, Helmi Zaghdane
  • Patent number: 9827253
    Abstract: Provided are novel prodrug salts of selective aquaporin inhibitors, their use as pharmaceuticals, and pharmaceutical compositions comprising them, and novel processes for their synthesis and novel intermediates for use in their synthesis. Also provided is use of a compound for the prophylaxis, treatment, and control of aquaporin-mediated conditions. Aquaporin inhibitors, e.g., inhibitors of AQP4 and/or AQP2, may be of utility in the treatment or control of diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord), hyponatremia, and excess fluid retention, as well as diseases such as epilepsy, retinal ischemia and other diseases of the eye, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines.
    Type: Grant
    Filed: November 6, 2014
    Date of Patent: November 28, 2017
    Assignee: AEROMICS, INC.
    Inventors: Marc F. Pelletier, Paul Robert McGuirk, George William Farr, Robert Zamboni, John Colucci, Helmi Zaghdane
  • Patent number: 9035046
    Abstract: 25-desacetyl rifaximin or a pharmaceutically acceptable salt thereof is provided. Methods of treatment of bowl related disorders using isolated and/or purified 25-desacetyl rifaximin or a pharmaceutically acceptable salt thereof are also provided.
    Type: Grant
    Filed: June 30, 2014
    Date of Patent: May 19, 2015
    Assignees: Salix Pharmaceuticals, Inc., Alfa Wassermann, S.P.A.
    Inventors: Pam Golden, Mohammed A. Kabir, Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Miriam Barbanti
  • Publication number: 20150133426
    Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
  • Patent number: 9018225
    Abstract: The present invention is directed to methods for preparation of a composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ?. For example, practice of a method of the invention can provide the composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ? wherein the rifaximin ? is present in about 3-12% (w/w) or is present in about 5-8% (w/w). The composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ? is prepared by dissolving raw rifaximin in a water-soluble organic solvent, for example ethanol, at reflux, then adding water to achieve a final mixed solvent of about 7:3 (v/v) solvent to water ratio, then cooling to 35-40° C. until crystallization commences, then further cooling with stirring to 0° C., then recovery of the crystallized material, and drying to a water content of between 2.5% and 5.0%, to provide the composition comprising mixed crystalline polymorphs rifaximin ? and rifaximin ?.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: April 28, 2015
    Assignee: Novel Laboratories
    Inventor: Kishore Kumar Hotha
  • Patent number: 9012441
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: April 21, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Patent number: 8987274
    Abstract: The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: March 24, 2015
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Latha G. Nair, Stephane L. Bogen, Ronald J. Doll, Yao Ma, Yuan Tian
  • Publication number: 20150050706
    Abstract: Disclosed is a process for carrying out a cyclisation reaction, a polymerization reaction, an enzymatic reaction showing substrate inhibition, an enzymatic reaction showing product inhibition, a reaction showing precipitation of the substrate or of a reactant, the process comprising the steps of a) diluting a fresh substrate with solvent to form a diluted substrate-solvent mixture, and supplying this mixture to a reactor, b) causing the reaction medium in the reactor to react, c) discharging reaction mixture comprising reaction product, solvent, and substrate that has not reacted, to a first filtration membrane which is permeable to the solvent and impermeable to the substrate and to the catalyst or at least one of the reactants, d) returning solvent from the permeate side of the first membrane to dilute the fresh substrate, and e) returning retentate comprising substrate which has not reacted, from the first filtration membrane to the reactor.
    Type: Application
    Filed: April 19, 2013
    Publication date: February 19, 2015
    Inventors: Anita Buekenhoudt, Pieter Vandezande, Dominique Ormerod
  • Patent number: 8921542
    Abstract: The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: December 30, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Soong-Hoon Kim, Robert M. Borzilleri, Gregory D. Vite, James A. Johnson
  • Publication number: 20140378433
    Abstract: The invention relates to bicydic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.
    Type: Application
    Filed: January 25, 2013
    Publication date: December 25, 2014
    Applicant: SANOFI
    Inventors: Alain Braun, Olivier Crespin, Yann Foricher, Gilbert Marciniak, Nicolas Muzet, Eric Nicolai, Cecile Pascal, Bertrand Vivet, Fabrice Viviani
  • Publication number: 20140323465
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Inventors: Deqiang Niu, Russell C. Petter, Juswinder Singh, Arthur F. Kluge, Lixin Qiao
  • Publication number: 20140315916
    Abstract: The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Application
    Filed: October 23, 2012
    Publication date: October 23, 2014
    Inventors: Latha G. Nair, Stephane L. Bogen, Ronald J. Doll, Yao Ma, Yuan Tian
  • Publication number: 20140221417
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: January 9, 2014
    Publication date: August 7, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, Yunfeng Eric HU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
  • Publication number: 20140206760
    Abstract: The invention relates to compounds of the formula (I) which are inhibitors of activated thrombin-activable fibrinolysis inhibitor. The compounds of the formula I are suitable for producing medicaments for prophylaxis, secondary prevention and treatment of one or more disorders associated with thromboses, embolisms, hypercoaguability or fibrotic changes.
    Type: Application
    Filed: March 26, 2014
    Publication date: July 24, 2014
    Applicant: SANOFI
    Inventors: Christopher Kallus, Mark Broenstrup, Andreas Evers, Anja Globisch, Herman Schreuder, Michael Wagner
  • Patent number: 8759513
    Abstract: The present invention discloses a stable amorphous form of Rifaximin characterized by having X-ray powder diffraction pattern as given in FIG. 1, having a 2? peaks at 7.2 and having moisture content in the range of 3% to 4% preferably, 3.4% to 3.7%. This invention also discloses a novel process for its preparation.
    Type: Grant
    Filed: August 24, 2011
    Date of Patent: June 24, 2014
    Assignee: Sequent Scientific Limited
    Inventors: Sumangala Venkatramana, Vijesh Alanthatta Madathil, Pejala Kakrannaya Vasudeva, Thangavel Arulmoli
  • Patent number: 8759512
    Abstract: The instant invention describes methods for producing macrocyclic compounds having antiproliferation activity, and useful in methods of treating disorders such as cancer, tumors and cell proliferation related disorders.
    Type: Grant
    Filed: February 24, 2009
    Date of Patent: June 24, 2014
    Assignees: University of Florida Research Foundation, Inc., Duke University
    Inventors: Hendrik Luesch, Jiyong Hong
  • Patent number: 8754105
    Abstract: Inhibitors of HCV replication of formula (I) the N-oxides, salts, and stereochemically isomeric forms thereof, wherein each dashed line (represented by ) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(?O)—, —O—C(?O)—NR4a— or —O—C(?O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(?O)OR5, —C(?O)R6, —C(?O)NR4aR4b, —C(?O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and whe
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: June 17, 2014
    Assignees: Medivir AB, Janssen R&D Ireland
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Rabiosson, Abdellah Tahri, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Dmitry Antonov
  • Patent number: 8754078
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: June 17, 2014
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Publication number: 20140094462
    Abstract: Sonic Hedgehog modulators and methods of use thereof are provided for.
    Type: Application
    Filed: February 28, 2013
    Publication date: April 3, 2014
    Inventors: Sara Buhrlage, Chris Dockendorff, Mike Foley, Han-Je Kim, Andrew Germain, Lawrence MacPherson, Partha Nag, Stuart Schreiber, Amal Ting, Michel Weiwer, Willmen Youngsaye
  • Publication number: 20140051678
    Abstract: The present invention relates to compounds which are inhibitors of the activity of Complex III of the mitochondrial electron transport chain and pharmaceutical compositions comprising said compounds alone or in combination with other active agents. The present invention further relates to use of the compounds of the invention as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit. More particularly the present invention relates to the use of the compounds of the invention in a method of treating and/or preventing cancers presenting tumor-initiating cells.
    Type: Application
    Filed: November 24, 2011
    Publication date: February 20, 2014
    Applicant: STEMERGIE BIOTECHNOLOGY SA
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Riccardo Cribiu
  • Publication number: 20140045821
    Abstract: Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 13, 2014
    Inventors: Peter Wipf, Qiming Jan Wang
  • Publication number: 20140045860
    Abstract: The invention relates to a compound of Formula I or a pharmaceutically acceptable ester, salt, prodrug or metabolite thereof;
    Type: Application
    Filed: August 13, 2013
    Publication date: February 13, 2014
    Applicants: NEW YORK UNIVERSITY, THE BROAD INSTITUTE, INC.
    Inventors: Leigh C. Carmody, Ana Rodriguez, Esther Bettiol, Michelle Palmer, Andrew Germain, Benito Munoz, Sivaraman Dandapani, Michael Foley
  • Patent number: 8642014
    Abstract: Luminescent reporter compounds that are rotaxanes having the structure where B—Z—C is a reporter molecule based on a cyanine, squaric acid, or other reporter, and K is a macrocycle that encircles and interlocks with the reporter molecule. Applications of the reporter compounds are provided, as well as reactive intermediates used to synthesize the reporter compounds, and methods of synthesizing the reporter compounds.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: February 4, 2014
    Assignee: SETA BioMedicals, LLC
    Inventors: Ewald A. Terpetschnig, Leonid D. Patsenker, Oleksii Klochko, Yuliia Kudriavtseva, Anatoliy L. Tatarets, Inna G. Yermolenko, Yevgen A. Povrozin
  • Publication number: 20130317043
    Abstract: The invention relates to a compound of Formula I:
    Type: Application
    Filed: May 6, 2013
    Publication date: November 28, 2013
    Applicants: President and Fellows of Harvard College, The Broad Institute, Inc.
    Inventors: The Broad Institute, Inc., President and Fellows of Harvard College
  • Patent number: 8536327
    Abstract: The present invention relates to compounds of the formula where the variables are as defined in the disclosure.
    Type: Grant
    Filed: June 15, 2007
    Date of Patent: September 17, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Soong-Hoon Kim, Robert M. Borzilleri, James A. Johnson
  • Publication number: 20130217874
    Abstract: Disclosed embodiments concern a method for making substantial quantities of desired macrocycles. Disclosed ring closing reactions make the macrocycle with desired olefin geometry in excellent yield and E/Z ratio. Particular embodiments of the current method concern intermediates that are obtained from commercially available starting materials in a small number of steps, thereby illustrating the commercial importance and applicability of the disclosed method. The macrocycle produced by the ring closing reaction can be further derivatized to provide analogs of the macrocyclic compounds.
    Type: Application
    Filed: November 1, 2011
    Publication date: August 22, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Thilo J. Heckrodt, Rajinder Singh
  • Publication number: 20130096162
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 3, 2012
    Publication date: April 18, 2013
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Publication number: 20130065872
    Abstract: The disclosure relates generally to methods for the preparation of a family of natural compounds, the syrbactins and their analogs.
    Type: Application
    Filed: December 3, 2010
    Publication date: March 14, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventor: Michael C. Pirrung
  • Patent number: 8324155
    Abstract: The present invention discloses compounds of formula I and II or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: December 4, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yonghua Gai, Yat Sun Or, Zhe Wang
  • Patent number: 8304385
    Abstract: The present invention relates to compounds of Formula I, II, III or IV, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: November 6, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Ying Sun, Dong Liu, Yat Sun Or, Zhe Wang
  • Publication number: 20120270881
    Abstract: Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the ?-catenin-dependent “canonical” Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.
    Type: Application
    Filed: August 3, 2010
    Publication date: October 25, 2012
    Applicant: POLYPHOR AG
    Inventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Franck Lach, Anatol Luther, Karsten Marx, Kerstin Möhle
  • Publication number: 20120258993
    Abstract: The present invention relates to novel amide compounds of formula I, and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC6 is responsive, and the pharmaceutical composition containing such compounds.
    Type: Application
    Filed: September 21, 2010
    Publication date: October 11, 2012
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
    Inventors: Giuseppe Giannini, Walter Cabri, Stephan Hanessian, Luciana Auzzas, Andreas Larsson
  • Patent number: 8278322
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: M. Katharine Holloway, Nigel J. Liverton, John A. McCauley, Michael T. Rudd, Joseph P. Vacca, Steven W. Ludmerer, David B. Olsen
  • Patent number: 8263579
    Abstract: This invention relates to novel compounds obtained by fermentation of Myxobacteria strain (PM0670013/MTCC 5570). The present invention further relates to the processes for the production of the novel anti-inflammatory compounds, to the culture no. PM0670013 (MTCC 5570), and to pharmaceutical compositions containing compounds of the present invention as an active ingredient and its use in medicines for the treatment of inflammatory diseases or disorders mediated by proinflammatory cytokines such as Tumor Necrosis Factor-alpha (TNF-?) and/or interleukins such as IL-6, having anti-inflammatory activity The invention also includes all stereoisomeric forms of compounds of the present invention.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: September 11, 2012
    Assignee: Piramal Healthcare Limited
    Inventors: Koteppa Pari, Girish Badrinath Mahajan, Nidhi Tomar, Vijaya Phani Kumar Yemparala, Asha Adrian Kulkarni-Almeida, Saji George
  • Publication number: 20120202821
    Abstract: Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.
    Type: Application
    Filed: August 5, 2009
    Publication date: August 9, 2012
    Applicant: POLYPHOR AG
    Inventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Franck Lach, Anatol Luther, Karsten Marx, Kerstin Möhle
  • Patent number: 8236807
    Abstract: The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: July 20, 2009
    Date of Patent: August 7, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Suanne Nakajima, Zhenwei Miao, Ying Sun, Datong Tang, Guoyou Xu, Brian Porter, Yat Sun Or, Zhe Wang
  • Publication number: 20120190651
    Abstract: This invention relates to novel compounds obtained by fermentation of Myxobacteria strain (PM0670013/MTCC 5570). The present invention further relates to the processes for the production of the novel anti-inflammatory compounds, to the culture no. PM0670013 (MTCC 5570), and to pharmaceutical compositions containing compounds of the present invention as an active ingredient and its use in medicines for the treatment of inflammatory diseases or disorders mediated by proinflammatory cytokines such as Tumor Necrosis Factor-alpha (TNF-?) and/or interleukins such as IL-6, having anti-inflammatory activity The invention also includes all stereoisomeric forms of compounds of the present invention.
    Type: Application
    Filed: January 24, 2011
    Publication date: July 26, 2012
    Inventors: Koteppa Pari, Girish Badrinath Mahajan, Nidhi Tomar, Vijaya Phani Kumar Yemparala, Asha Adrian Kulkarni-Almeida, Saji George
  • Patent number: 8216999
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: December 1, 2008
    Date of Patent: July 10, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: M. Katharine Holloway, Nigel J. Liverton, Steven W. Ludmerer, John A. McCauley, David B. Olsen, Michael T. Rudd, Joseph P. Vacca, Charles J. McIntyre
  • Publication number: 20120164039
    Abstract: To provide a solid-liquid palladium ion adsorbent which has both extraction performance and selectivity of a liquid-liquid palladium extracting agent in a conventional solvent extraction method and which does not require use of an organic solvent, and methods for selectively separating and recovering palladium, using it.
    Type: Application
    Filed: August 20, 2010
    Publication date: June 28, 2012
    Applicant: TOSOH CORPORATION
    Inventor: Yukinori Sudo
  • Publication number: 20120108499
    Abstract: The invention relates to new peptoid compounds of formula (I), as well as their use in the treatment of bacterial infections, such as those caused by vancomycin resistant microorganisms, and to compositions thereof.
    Type: Application
    Filed: September 6, 2011
    Publication date: May 3, 2012
    Applicant: University of Wollongong
    Inventors: John BREMNER, Stephen PYNE, Paul KELLER, Dan COGHLAN, Adel GARAS, Helen WITCHARD, Tim BOYLE, Jonathan COATES
  • Patent number: 8153619
    Abstract: Novel diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders are provided.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: April 10, 2012
    Assignee: Joyant Pharmaceuticals, Inc.
    Inventors: Gunnar James Hanson, Ming Zhou, Qi Wei, Charles Caldwell
  • Patent number: 8138164
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: March 20, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel J. Liverton, Vincenzo Summa, Joseph P. Vacca
  • Publication number: 20120039848
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: August 11, 2011
    Publication date: February 16, 2012
    Inventors: Yao-Ling Qiu, Xiaowen Peng, Ce Wang, Yat Sun Or
  • Publication number: 20120028978
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.
    Type: Application
    Filed: March 26, 2010
    Publication date: February 2, 2012
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Min Zhong, Leping Li
  • Patent number: 8093379
    Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: January 10, 2012
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Adel Moussa, Benjamin Alexander Mayes, Elodie Rosinovsky, Alistair Stewart
  • Patent number: 8093235
    Abstract: The invention provides compounds of formula I: wherein A, B, D, E, R1, R2, R3, R4, R5, X, and ----- have any values defined herein, as well as salts thereof. The compounds have activity as G-quadruplex DNA stabilizers and as anti-proliferative agents.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: January 10, 2012
    Assignees: Rutgers, The State University of New Jersey, University of Medicine and Dentistry of New Jersey
    Inventors: Edmond J. Lavoie, Joseph E. Rice, Leroy F. Liu
  • Patent number: 8030307
    Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: October 4, 2011
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Joel D. Moore, Yat Sun Or, Zhe Wang
  • Publication number: 20110237621
    Abstract: Inhibitors of HCV replication of formula (I) the N-oxides, salts, and stereochemically isomeric forms thereof, wherein each dashed line (represented by ) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(?O)—, —O—C(?O)—NR4a— or —O—C(?O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(?O)OR5, —C(?O)R6, —C(?O)NR4aR4b, —C(?O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and whe
    Type: Application
    Filed: May 17, 2011
    Publication date: September 29, 2011
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist, Dmitry Antonov
  • Publication number: 20110230515
    Abstract: A prodrug compound of a rapamycin analog and methods for inhibiting, treating, and preventing mammalian diseases.
    Type: Application
    Filed: May 27, 2011
    Publication date: September 22, 2011
    Inventors: Karl W. Mollison, Angela M. LeCaptain, Sandra E. Burke, Keith R. Cromack, Peter J. Tarcha, Yen-Chih J. Chen, John L. Toner
  • Patent number: 8012953
    Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: September 6, 2011
    Assignee: Schering Corporation
    Inventors: Andrew W. Stamford, Ying Huang, Guoqing Li, Corey O. Strickland, Johannes H. Voigt