Benzene Ring Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/346.1)
  • Patent number: 9181233
    Abstract: The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Grant
    Filed: March 3, 2011
    Date of Patent: November 10, 2015
    Assignee: PROBIODRUG AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Patent number: 9156793
    Abstract: The invention discloses a method for the preparation of medetomidine starting from 1-bromo 2,3-dimethylbenzene and chloroacetone.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: October 13, 2015
    Assignee: Lonza Ltd.
    Inventors: Florencio Zaragoza Doerwald, Anna Kulesza, Stephan Elzner, Robert Bujok, Zbigniew Wrobel, Krzysztof Wojciechowski
  • Publication number: 20150099889
    Abstract: The invention discloses a method for the preparation of medetomidine starting from 1-bromo 2,3-dimethylbenzene and chloroacetone.
    Type: Application
    Filed: November 15, 2012
    Publication date: April 9, 2015
    Inventors: Florencio Zaragoza Doerwald, Anna Kulesza, Stephen Elzner, Robert Bujok, Zbigniew Wrobel, Krzysztof Wojciechowski
  • Publication number: 20150080287
    Abstract: The invention discloses a method for preparation of 2-(2,3-dimethylphenyl)-1-proponal from bromo 2,3-dimethyl-benzene and aceton, its use in perfumes and its use for the preparation of medetomidine.
    Type: Application
    Filed: November 15, 2012
    Publication date: March 19, 2015
    Inventors: Florencio Zaragoza Doerwald, Anna Kulesza, Stephan Elzner, Robert Bujok, Zbigniew Wrobel, Krzysztof Wojciechowski
  • Publication number: 20150079519
    Abstract: A photosensitive compound represented by formula (1) or formula (2). (Chemical formula 1) (In formula (1) and formula (2), n is an integer of 1-3; R1 is a linear or branched alkyl group having 1-6 carbon atoms or an alkylene group having 2-6 carbon atoms formed from two R1 together; R2 is —NR3R4; R3 and R4 are each independently a linear or branched alkyl group or alkenyl group having 1-6 carbon atoms, a linear or branched alkylene group having 2-6 carbon atoms formed by R3 and R4 together, or a linear or branched alkylene group or alkenylene group having 3-8 carbon atoms optionally containing an oxygen atom or nitrogen atom.
    Type: Application
    Filed: February 28, 2013
    Publication date: March 19, 2015
    Inventor: Toru Shibuya
  • Publication number: 20150057453
    Abstract: The invention discloses a method for the preparation of medetomidine starting from 1-bromo 2,3-dimethylbenzene and aceton.
    Type: Application
    Filed: November 15, 2012
    Publication date: February 26, 2015
    Inventors: Florencio Zaragoza Doerwald, Anna Kulesza, Stephan Elzner, Robert Bujok, Zbigniew Wrobel, Krzysztof Wojciechowski
  • Patent number: 8962862
    Abstract: There is provided a novel process for the preparation of a compound of formula (I), (Formula (I)). There is also provided novel processes to intermediates of the compound of formula (I), as well as novel intermediates themselves.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: February 24, 2015
    Assignee: Cambrex Karlskoga AB
    Inventors: Lars Eklund, Lars Hansson, Tommy Lundholm, Pär Holmberg, Margus Eek
  • Publication number: 20150045266
    Abstract: A composition including an ionic liquid alkyl ammonium salt (e.g., tetraalkylammonium cation and bis(trifluoromethanesulfonyl)imide anion) or an ionic liquid imidazolium salt (e.g., 1,3-dialkylimidazolium cation and bis(trifluoromethanesulfonyl)imide anion), that have a structure sufficient to exhibit at least partial solubility in one or more Group I-V base stocks. The disclosure also relates to a lubricating oil base stock and lubricating oil containing the composition, a multifunctional functional fluid containing the composition, and a method for improving solubility of an ionic liquid in a lubricating oil by using as the lubricating oil a formulated oil including a lubricating oil base stock as a major component, and an ionic liquid alkylammonium salt cobase stock, or an ionic liquid imidazolium salt cobase stock, as a minor component.
    Type: Application
    Filed: November 14, 2013
    Publication date: February 12, 2015
    Applicant: ExxonMobil Research and Engineering Company
    Inventors: Abhimanyu Onkar Patil, Satish Bodige, Tezcan Guney
  • Patent number: 8901106
    Abstract: Imidazole prodrugs, pharmaceutically acceptable salts, or isomers thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ellen K. Kick, Michael J. Hageman, Victor R. Guarino, Ching-Chiang Su, Chenkou Wei, Jayakumar S. Warrier, Satheesh Nair
  • Patent number: 8883747
    Abstract: Described herein are compositions and methods that treat fungal infections of the skin, reduce the severity and duration of symptoms of fungal infections of the skin, and prevent recurrence of fungal infections. The topical compositions described herein are creamy pastes composed of an admixture of an imidazole antifungal and nystatin. The topical compositions can also include optional fillers. The compositions and methods described herein minimize fungal resistance and maximize the number of targeted fungal strains. Additionally, the compounds and methods do not suppress the body's immune system either locally or systemically, thus allowing for a faster restoration of normal skin flora. The compositions and methods described herein are particularly suitable for use in infants and children as well as in immunocompromised individuals, diabetics, and the obese.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: November 11, 2014
    Inventor: Craig W. Carver
  • Patent number: 8877941
    Abstract: A new and efficient process to obtain Medetomidine enantiomers, a selective and potent ?2-receptor agonist, is presented. Such process comprises a resolution step and a racemization reaction, to be able to recover the unwanted enantiomer which can be recycled as starting material.
    Type: Grant
    Filed: February 26, 2013
    Date of Patent: November 4, 2014
    Assignee: Edmond Pharma S.r.l.
    Inventors: Matteo Zacche', Fulvio Gerli, Pier Andrea Gatti
  • Publication number: 20140249161
    Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.
    Type: Application
    Filed: February 27, 2014
    Publication date: September 4, 2014
    Applicant: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
    Inventors: David WATT, Chunming LIU, Vitaliy M. SVIRIPA, Wen ZHANG
  • Publication number: 20140187789
    Abstract: There is provided a novel process for the preparation of a compound of formula (I), (Formula (I)). There is also provided novel processes to intermediates of the compound of formula (I), as well as novel intermediates themselves.
    Type: Application
    Filed: July 20, 2012
    Publication date: July 3, 2014
    Applicant: CAMBREX KARLSKOGA AB
    Inventors: Lars Eklund, Lars Hansson, Tommy Lundholm, Pär Holmberg, Margus Eek
  • Publication number: 20140142307
    Abstract: Singly and multiply charged imidazolium cations (ICs) have been identified as a class of chemical compositions that possess potent antineoplastic, antibacterial and antimicrobial properties. The imidazolium cations disclosed demonstrate greater or equivalent potency towards cancerous cells as the current clinical standard, cisplatin. These imidazolium cations, however, achieve this efficacy without any of the known toxic side effects caused by heavy metal-based antineoplastic drugs such as cisplati.
    Type: Application
    Filed: April 30, 2012
    Publication date: May 22, 2014
    Inventors: Wiley Youngs, Matthew Panzner, Claire Tessier, Michael Deblock, Brian Wright, Patrick Wagers, Nikki Robishaw
  • Patent number: 8648106
    Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: February 11, 2014
    Assignee: Hospira, Inc.
    Inventors: Priyanka Roychowdhury, Robert A. Cedergren
  • Publication number: 20140018321
    Abstract: Imidazole prodrugs, pharmaceutically acceptable salts, or isomers thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: March 26, 2012
    Publication date: January 16, 2014
    Inventors: Ellen K. Kick, Michael J. Hageman, Victor R. Guarino, Ching-Chiang Su, Chenkou Wei, Jayakumar S. Warrier, Satheesh Nair
  • Patent number: 8623942
    Abstract: The present invention provides a liquid curable epoxy resin composition that has excellent storage stability and curing properties and provides a cured product having excellent properties, particularly, excellent organic solvent resistance. For that purpose, a clathrate containing a carboxylic acid compound and at least one selected from the group consisting of an imidazole compound represented by formula (I), wherein R1 to R4 each represent a hydrogen atom or the like, and 1,8-diazabicyclo[5.4.0]undecene-7 (DBU) is mixed in an epoxy resin. The liquid curable epoxy resin composition uses a liquid epoxy resin or an organic solvent.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: January 7, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Masami Kaneko, Kazuo Ono, Natsuki Amanokura, Naoyuki Kamegaya
  • Patent number: 8604213
    Abstract: This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: December 10, 2013
    Assignee: Nutech Ventures
    Inventor: Stephen Dimagno
  • Publication number: 20130296346
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.
    Type: Application
    Filed: November 22, 2011
    Publication date: November 7, 2013
    Applicant: Faes Farma, S.A.
    Inventors: Rosa Rodes Solanes, Neftali Garcia Dominguez, Beatriz Lopez Ortega, Melchor Alvarez De Mon Soto, Antonio De La Hera Martinez, Ana Munoz Munoz, Francisco Ledo Gomez
  • Publication number: 20130225832
    Abstract: A new and efficient process to obtain Medetomidine enantiomers, a selective and potent ?2-receptor agonist, is presented. Such process comprises a resolution step and a racemisation reaction, to be able to recover the unwanted enantiomer which can be recycled as starting material.
    Type: Application
    Filed: February 26, 2013
    Publication date: August 29, 2013
    Applicant: Edmond Pharma s.r.l.
    Inventors: Matteo Zacche', Fulvio Gerli, Pier Andrea Gatti
  • Patent number: 8513294
    Abstract: Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumor tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: August 20, 2013
    Assignees: Osta Biotechnologies, Queens University at Kingston, The Sir Mortimer B. Davis-Jewish General Hospital
    Inventors: Ajay Gupta, Hyman M. Schipper, Moulay Alaoui-Jamali, Walter A. Szarek, Kanji Nakatsu, Jason Z. Vlahakis
  • Patent number: 8513291
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: August 20, 2013
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Lambertus J. W. M. Oehlen, James G. Tarrant, Dong Sung Lim, Xiaokang Zhu, Dawoon Jung, Rama K. Mishra
  • Patent number: 8492422
    Abstract: The present invention relates to method for treating skin diseases and skin conditions in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, or enantiomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: September 15, 2011
    Date of Patent: July 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Mohammad I. Dibas, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello, Daniel W. Gil
  • Patent number: 8492557
    Abstract: The present invention relates to novel compounds, ester pro-drugs of [3-(1-1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals in the treatment of conditions mediated by adrenergic receptors.
    Type: Grant
    Filed: September 15, 2011
    Date of Patent: July 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Liming Wang, Michael E. Garst, John E. Donello, Daniel W. Gil, Mohammad I. Dibas
  • Publication number: 20130143938
    Abstract: Pharmaceutical compositions for the treatment of nasal congestion or migraine, wherein the pharmaceutical compositions comprise low concentrations of a super-selective subclass of selective ?-2 adrenergic receptor agonists.
    Type: Application
    Filed: February 1, 2013
    Publication date: June 6, 2013
    Applicant: Eye Therapies LLC
    Inventor: Eye Therapies LLC
  • Patent number: 8445526
    Abstract: The invention provides ?-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred ?-2 agonist used in the inventive compositions and methods is dexmedetomidine.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: May 21, 2013
    Assignee: Glaucoma & Nasal Therapies LLC
    Inventor: Gerald Horn
  • Publication number: 20130109684
    Abstract: The present disclosure provides a series of compounds which exhibit isoform selective inhibition of GRP94, a homologue of Hsp90 that is localized to the endoplasmic recticulum. Through GRP94 inhibition, these compounds are likely to manifest anti-cancer, anti-inflammatory, anti-metastasis, and immunosuppressive activities, as well as utility in the treatment of neurodegenerative diseases, and diabetes.
    Type: Application
    Filed: April 6, 2012
    Publication date: May 2, 2013
    Applicant: University of Kansas
    Inventors: Brian S.J. Blagg, Adam S. Duerfeldt
  • Patent number: 8399463
    Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: March 19, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Patent number: 8314137
    Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: November 20, 2012
    Assignee: Trustess of Dartmouth College
    Inventors: Tadashi Honda, Emilie David, Dale Mierke
  • Publication number: 20120202781
    Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
    Type: Application
    Filed: April 8, 2010
    Publication date: August 9, 2012
    Inventors: Kevin James Gillen, Jonathan Gillespie, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
  • Publication number: 20120196838
    Abstract: The invention relates to certain compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders and immune disorders.
    Type: Application
    Filed: January 25, 2012
    Publication date: August 2, 2012
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Junyi Zhang, Shoujun Chen, Lijun Sun
  • Publication number: 20120197005
    Abstract: The invention provides a method for producing a mixture of amorphous compounds, the method comprising supplying a solution containing the compounds; and allowing at least a portion of the solvent of the solution to evaporate while preventing the solute of the solution from contacting a nucleation point. Also provided is a method for transforming solids to amorphous material, the method comprising heating the solids in an environment to form a melt, wherein the environment contains no nucleation points; and cooling the melt in the environment.
    Type: Application
    Filed: January 30, 2012
    Publication date: August 2, 2012
    Applicant: UCHICAGO ARGONNE, LLC
    Inventors: Chris J. Benmore, Johann R. Weber
  • Publication number: 20120196874
    Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. The halogenated stilbene analogs include nitrogen heteroaryl groups and/or amino groups on the stilbene ring.
    Type: Application
    Filed: January 27, 2012
    Publication date: August 2, 2012
    Inventors: David WATT, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang
  • Publication number: 20120196905
    Abstract: Methods and small molecule compounds for smoking and CNS disease harm reduction are provided.
    Type: Application
    Filed: August 5, 2011
    Publication date: August 2, 2012
    Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTE
    Inventor: John R. CASHMAN
  • Patent number: 8232308
    Abstract: A method for treating a disease in which Rho kinase is involved. The method is carried out by administering to a patient in need thereof a pharmaceutically effective amount of a compound of the following formula or a pharmaceutically acceptable salt thereof: wherein the ring X is a benzene ring or a pyridine ring; R1 and R2 are hydrogen or alkyl or together form a cycloalkene ring; R3 is hydrogen, substituted alkyl, unsubstituted alkenyl, carboxyl or an ester or an amide thereof, amino or a cyano; R4 is hydrogen, hydroxyl, substituted or unsubstituted alkoxy, unsubstituted alkenyloxy, unsubstituted cycloalkyloxy substituted or unsubstituted alkyl, unsubstituted alkenyl, unsubstituted cycloalkyl, amino, substituted or unsubstituted alkylamino, nitro, cyano or a monocyclic heterocycle; and R5 is a halogen atom or a hydrogen atom.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: July 31, 2012
    Assignees: UBE Industries, Ltd., Santen Pharmaceutical Co., Ltd.
    Inventors: Masahiko Hagihara, Ken-ichi Komori, Hidetoshi Sunamoto, Hiroshi Nishida, Takeshi Matsugi, Tadashi Nakajima, Masakazu Hatano, Kazutaka Kido, Hideaki Hara
  • Publication number: 20120157474
    Abstract: The present invention is based on the discovery of a cell-based system to identify novel modulators of splicing or splicing dependent processes. The cell-based system of the present invention utilizes a fast and highly sensitive reporter, that responds to defects in the splicing machinery itself and is sensitive to changes in the signals that regulate splicing dependent processes such as those that modulate the EJC, splicing-dependent export, localization or translation efficiency. The present invention further uses the cell-based screen to identify several small molecules that modulate both constitutive and alternative splicing. Accordingly, the present invention includes general or alternative splicing inhibitors identified using the assay described herein. The present invention also provides methods of treating a subject having a condition associated with aberrant target RNA expression.
    Type: Application
    Filed: May 21, 2010
    Publication date: June 21, 2012
    Applicant: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Gideon Dreyfuss, Ihab Younis, Lili Wan
  • Publication number: 20120149746
    Abstract: The present invention relates to method of treating retinal diseases in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: September 15, 2011
    Publication date: June 14, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Mohammed I. Dibas, Daniel W. Gil, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello
  • Publication number: 20120129906
    Abstract: The present invention relates to novel diphenylethyne derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 24, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Michael E. Garst, Wha Bin Im
  • Publication number: 20120004417
    Abstract: This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
    Type: Application
    Filed: October 20, 2009
    Publication date: January 5, 2012
    Inventor: Stephen Dimagno
  • Publication number: 20120004230
    Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.
    Type: Application
    Filed: September 19, 2011
    Publication date: January 5, 2012
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20110301214
    Abstract: Disclosed herein is a pharmaceutical composition comprising (3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl)methanol and methods of using the composition to treat chronic pain.
    Type: Application
    Filed: February 12, 2010
    Publication date: December 8, 2011
    Applicant: ALLEGRAN, INC.
    Inventor: Daniel W. Gil
  • Publication number: 20110263543
    Abstract: Biphenyl compounds of Formula (I) and Formula (II), and their pharmaceutically acceptable salts or solvates or prodrugs, their pharmaceutical compositions, their use and process of preparation are provided. Compounds of Formula (I) and Formula (II) are disclosed to exhibit anti-inflammatory properties.
    Type: Application
    Filed: August 24, 2009
    Publication date: October 27, 2011
    Inventors: Rajiv R. Sakhardande, Vithal Kulkarni, Nilesh Wagh, Manmohan Nimbalkar, Suhas M. Nadkarni
  • Publication number: 20110244058
    Abstract: The invention provides compositions and methods for treating pulmonary diseases and conditions. The provided compositions and methods utilize either low concentrations of selective ?-2 adrenergic receptor agonists having a binding affinity of 300 fold or greater for ?-2 over ?-1 adrenergic receptors or ketamine at specific pH. The compositions preferably comprise brimonidine and/or dexmedetomidine and/or ketamine.
    Type: Application
    Filed: April 13, 2011
    Publication date: October 6, 2011
    Inventor: Gerald Horn
  • Publication number: 20110237633
    Abstract: The present invention provides compounds and pharmaceutically acceptable compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases in which hepatocyte growth factor/scatter factor (HGF/SF) or the activities thereof, or agonists or antagonists thereof, have a therapeutically useful role.
    Type: Application
    Filed: December 11, 2009
    Publication date: September 29, 2011
    Inventors: Bijoy Panicker, Lambertus J.W.M. Oehlen, Itzhak G. Goldberg
  • Patent number: 8026260
    Abstract: The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: September 27, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joshua Close, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, David Sloman, Matthew G Stanton, Paul Tempest, David J. Witter
  • Patent number: 8013169
    Abstract: Disclosed herein is a compound of the formula (a): Therapeutic methods, compositions and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: January 4, 2008
    Date of Patent: September 6, 2011
    Assignee: Allergan, Inc
    Inventors: Todd M. Heidelbaugh, Phong X. Nguyen, Ken Chow, Michael E. Garst
  • Publication number: 20110196007
    Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
    Type: Application
    Filed: July 22, 2009
    Publication date: August 11, 2011
    Inventors: Tadashi Honda, Emilie David, Dale Mierke
  • Publication number: 20110190505
    Abstract: This disclosure relates to compounds, reagents, and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. For example, this disclosure provides universal “locked” aryl substituents that result in StereoElectronic Control of Unidirectional Reductive Elimination (SECURE) from diaryliodonium salts. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
    Type: Application
    Filed: February 4, 2011
    Publication date: August 4, 2011
    Inventor: Stephen DiMagno
  • Publication number: 20110152271
    Abstract: The invention provides compositions and methods for treating nasal congestion through ophthalmic delivery. The provided compositions and methods utilize low concentrations of selective ?-2 adrenergic receptor agonists. The compositions preferably include brimonidine.
    Type: Application
    Filed: December 17, 2010
    Publication date: June 23, 2011
    Inventor: Gerald Horn
  • Publication number: 20110136796
    Abstract: Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
    Type: Application
    Filed: April 24, 2009
    Publication date: June 9, 2011
    Applicants: NEWLINK GENETICS, LANKEANAU INSTITUTE FOR MEDICAL RESEARCH
    Inventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Nicholas N. Vahanian, Charles J. Link, Judith Lalonde, George Prendergast, Alexander Muller, William Malachowski