Plural Sulfurs Or Nitrogens In The Five-membered Hetero Ring (e.g., Thiatriazole, Etc.) Patents (Class 544/134)
  • Publication number: 20150133446
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, Rx, R1, R2, R3, X1, X2 and s are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 14, 2015
    Inventors: R. Michael Lawrence, Michael M. Miller, Dietmar Alfred Seiffert, Shoshana L. Posy, Pancras C. Wong, Jacques Banville, Edward H. Ruediger, Daniel H. Deon, Alain Martel, François Tremblay, Julia Guy, Jean-François Lavallée, Marc Gagnon
  • Patent number: 9012443
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: April 21, 2015
    Assignee: Amgen Inc.
    Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
  • Publication number: 20150094297
    Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 2, 2015
    Inventors: Jacques Banville, Roger Rèmillard, Edward H. Ruediger, Daniel H. Deon, Marc Gagnon, Laurence Dubé, Julia Guy, Eldon Scott Priestley, Shoshana L. Posy, Brad D. Maxwell, Pancras C. Wong, R. Michael Lawrence, Michael M. Miller
  • Patent number: 8987262
    Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: March 24, 2015
    Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de Bordeaux
    Inventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
  • Publication number: 20150018331
    Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
    Type: Application
    Filed: March 24, 2014
    Publication date: January 15, 2015
    Applicant: Achaogen, Inc.
    Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
  • Publication number: 20140369961
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy F. Stanton, Eric B. Sjogren
  • Publication number: 20140330011
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 6, 2014
    Publication date: November 6, 2014
    Applicant: CYTOKINETICS, INC
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Patent number: 8877748
    Abstract: A heterocyclic fused anthraquinone derivative, which is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of hydrogen, halogens, aminoalkyl group, sulfoalkyl group, haloalkyl group, piperazino group, sulfonyl group, morpholino group, alkali group or one substituent represented by a formula (II): wherein R2 is amino group, oxyl group or a thiol group. In the meantime, a method for manufacturing the above-mentioned heterocyclic fused anthraquinone derivatives and a pharmaceutical composition using thereof are also disclosed here.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: November 4, 2014
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Yu-Ru Lee, Tsung-Chih Chen
  • Publication number: 20140206661
    Abstract: The present invention provides a compound of Formula (X) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: January 21, 2014
    Publication date: July 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Jake AXFORD, Natalie DALES, Moo Je SUNG
  • Patent number: 8703961
    Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: April 22, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Hannes Koolman
  • Publication number: 20140107124
    Abstract: Disclosed herein are compositions comprising an amide related to a prostaglandin and a biogenic amine. Other aspects relate to certain chemical compounds, pharmaceutical compositions, and methods of treating glaucoma.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 17, 2014
    Applicant: Allergan, Inc.
    Inventors: David F. Woodward, Robert M. Burk
  • Publication number: 20140094603
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
    Type: Application
    Filed: December 6, 2013
    Publication date: April 3, 2014
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R. Laird, John Robinson, Shelley Allen
  • Patent number: 8685975
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 1, 2014
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20140039183
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Application
    Filed: July 15, 2013
    Publication date: February 6, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • Publication number: 20130345220
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
    Type: Application
    Filed: August 29, 2013
    Publication date: December 26, 2013
    Applicant: IRM LLC
    Inventors: Valentina MOLTENI, Xiaolin Li, Juliet Nabakka, David Archer Ellis, Beth Anaclerio, Enrique Saez, John Wityak
  • Publication number: 20130289028
    Abstract: A heterocyclic fused anthraquinone derivatives, which is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of hydrogen, halogens, aminoalkyl group, sulfoalkyl group, haloalkyl group, piperazino group, sulfonyl group, morpholino group, alkali group or one substituent represented by a formula (II): wherein R2 is amino group, oxyl group or a thiol group. In the meantime, a method for manufacturing the above-mentioned heterocyclic fused anthraquinone derivatives and a pharmaceutical composition using thereof are also disclosed here.
    Type: Application
    Filed: March 1, 2013
    Publication date: October 31, 2013
    Applicant: NATIONAL DEFENSE MEDICAL CENTER
    Inventors: Hsu-Shan HUANG, Yu-Ru LEE, Tsung-Chih CHEN
  • Patent number: 8563550
    Abstract: There is provided compounds of formula (I), wherein Z, M, R1, X, R2, R3 and B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, and particularly in the treatment of cancer.
    Type: Grant
    Filed: September 29, 2008
    Date of Patent: October 22, 2013
    Inventors: Paolo Pevarello, Ana Maria Garcia Collazo, Ana Belen Garcia Garcia
  • Patent number: 8507538
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: August 13, 2013
    Assignee: Receptos, Inc.
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • Publication number: 20130150339
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 13, 2013
    Applicant: Amgen Inc.
    Inventor: Amgen Inc.
  • Publication number: 20130060025
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 7, 2013
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Patent number: 8343970
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: January 1, 2013
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20120289698
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 13, 2012
    Publication date: November 15, 2012
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Publication number: 20120270868
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: October 17, 2011
    Publication date: October 25, 2012
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thomas Martin KIRRANE, Daniel Richard MARSHALL, Robert SIBLEY, Roger John SNOW, Fariba SOLEYMANZADEH, Ronald John SORCEK
  • Publication number: 20120225879
    Abstract: The present invention is based on the use of a broad family of 5-imino-1,2,4-thiadiazoles as potential new drugs for the treatment of diseases in which PDE7 inhibition is important, specially inflammatory diseases, autoimmune and neurodegenerative disorders. On the other hand, compounds of the 5-imino-1,2,4-thiadiazole family are here described, as well as their synthetic procedures, and they may have great application as drug or drug candidates.
    Type: Application
    Filed: October 4, 2010
    Publication date: September 6, 2012
    Applicant: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFACAS ( CSIC)
    Inventors: Ana Martínez Gil, Carmen Gil Ayuso-Gontan, Valle Palomo Ruiz, Daniel Perez Fernandez, Concepción Perez Martín, Ana María Perez Castillo, María Isabel Loza Garcia, María Isabe Cadavid Torres, José Brea Floriani
  • Publication number: 20120214812
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
    Type: Application
    Filed: March 7, 2012
    Publication date: August 23, 2012
    Applicant: IRM LLC
    Inventors: VALENTINA MOLTENI, XIAOLIN LI, JULIET NABAKKA, DAVID ARCHER ELLIS, BETH ANACLERIO, ENRIQUE SAEZ, JOHN WITAK
  • Patent number: 8227598
    Abstract: The invention relates to novel heteroaryl carboxamides, a process for their preparation, and pharmaceutical compositions containing them. These materials are useful for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Grant
    Filed: August 10, 2007
    Date of Patent: July 24, 2012
    Assignee: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Martin Hendrix, Frank-Gerhard Böβ, Christina Erb, Joachim Krüger, Christoph Methfessel, Rudy Schreiber, Welf-Burkhard Wiese, Joachim Luithle
  • Publication number: 20120040984
    Abstract: The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.
    Type: Application
    Filed: January 27, 2010
    Publication date: February 16, 2012
    Applicant: SANOFI
    Inventors: Eykmar Fett, Patrick Mougenot, Claudie Namane, Eric Nicolai, Christophe Philippo
  • Patent number: 8106046
    Abstract: A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing compounds of Formula I and methods of treating diseases or disorders including metabolic and inflammatory or immune associated diseases or disorders.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: January 31, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventor: Bingwei Vera Yang
  • Publication number: 20120015941
    Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.
    Type: Application
    Filed: July 23, 2008
    Publication date: January 19, 2012
    Applicant: CRESTONE, INC.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
  • Patent number: 8067414
    Abstract: The invention provides compositions and kits comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating ophthalmic disorders; (b) treating cerebrovascular disorders; (c) treating cardiovascular disorders; (d) treating benign prostatic hyperplasia (BPH); (e) treating peptic ulcers; (e) treating sexual dysfunctions and (f) inducing abortions. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: November 29, 2011
    Assignee: NiCox S.A.
    Inventor: David S. Garvey
  • Publication number: 20110288089
    Abstract: A compound of Formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: January 13, 2010
    Publication date: November 24, 2011
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
  • Publication number: 20110224187
    Abstract: The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
    Type: Application
    Filed: October 14, 2009
    Publication date: September 15, 2011
    Inventors: Anandan Palani, Michael Y. Berlin, Aslanian G. Robert, Vaccaro M. Henry, Chan Tin-Yau, Xiao Dong, Degrado Sylvia, Rao U. Ashwin, Chen Xiao, Lee Yoon Joo, Sofolarides J. Michael, Shao Ning, Huang R. Ying, Liu Zhidan, Wang Li Yuan, Pu Haiyan
  • Publication number: 20110190289
    Abstract: There is provided compounds of formula (I), wherein Z, M, R1, X, R2, R3 and B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, and particularly in the treatment of cancer.
    Type: Application
    Filed: September 29, 2008
    Publication date: August 4, 2011
    Applicant: Centro Nacional De Investigaciones Oncologicas (CNIO)
    Inventors: Paolo Pevarello, Ana Maria Garcia Collazo, Ana Belen Garcia Garcia
  • Publication number: 20110183953
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Application
    Filed: November 15, 2010
    Publication date: July 28, 2011
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • Publication number: 20110160186
    Abstract: The invention provides various methods comprising the administration of a CYP2D6 bioactive drug covalently bound to a water-soluble oligomer. Metabolism of CYP2D6 bioactive drug conjugates is diverted from CYP2D6 to alternative pathways, and the conjugates may therefore be utilized to alleviate the problems associated with interpopulation variation resulting from the genetic polymorphism in the CYP2D6 gene.
    Type: Application
    Filed: June 9, 2009
    Publication date: June 30, 2011
    Applicant: Nektar Therapeutics
    Inventors: Michael A. Eldon, C. Simone Jude-Fishburn, Hema Gursahani, Myong Gyong Lee
  • Patent number: 7968577
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: June 28, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
  • Publication number: 20110137021
    Abstract: The use of N-formamidino-5-amino-3H-1,2,4-dithiazole-3-thiones, 5-phenyl-3H-1,2,4-dithiazole-3-thiones, and derivatives thereof as novel, efficient sulfur-transfer reagents is disclosed. Sulfur transfer from these reagents to compounds containing a P(III) atom (e.g., triphenylphosphine, 5?-O-DMT-thymidine 2-cyanoethyl-(N,N-diisopropyl)phosphoramidite, and 5?-O-DMT-3?-O-levulinyl dithymidilyl 2-cyanoethyl phosphite), was studied in solution by 31P NMR and HPLC. The sulfur transfer from title compounds was also studied in the solid-phase synthesis of oligonucleotide phosphorothioates by phosphoramidite methods. In this application, the efficiency of the sulfur transfer reaction for 2?-deoxyoligonucleotides was better than 99.5%. The novel sulfurizing agents are synthesized, at low cost, using simple chemical methods.
    Type: Application
    Filed: December 1, 2010
    Publication date: June 9, 2011
    Inventor: Andrei P. Guzaev
  • Publication number: 20110105495
    Abstract: A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing compounds of Formula I and methods of treating diseases or disorders including metabolic and inflammatory or immune associated diseases or disorders.
    Type: Application
    Filed: June 24, 2009
    Publication date: May 5, 2011
    Inventor: Bingwei Vera Yang
  • Publication number: 20110092507
    Abstract: The present invention provides a process for preparing optically active timolol. The process comprises the following steps. Firstly, reacting 3-hydroxy-4-morpholino-1,2,5-thiadiazole with an optically active epichlorohydrin in the presence of a solvent system, which has a first volume and a catalyst optionally in the presence of a suitable base to obtain an optically active intermediate product. Secondly, treating the optically active intermediate product with a solution, which has a second volume and comprises tert-butylamine to obtain an optically active timolol. The solvent system used in the first step can be an amide solvent, sulfoxide solvent, cyclic hydrocarbon solvent, ketone solvent, or a heterocyclic solvent. The catalyst used in the first step can be an alkali metal hydroxide, alkali metal carbonate, alkali metal hydrogen carbonate, piperidine, pyridine, triethylamine, potassium hydroxide, sodium hydroxide, potassium carbonate, and other heterocyclic bases.
    Type: Application
    Filed: October 20, 2009
    Publication date: April 21, 2011
    Inventors: Chin-Tsai FAN, Chen-Ming Hsiao, Rong-Bin Hsieh
  • Publication number: 20110086847
    Abstract: The present invention relates to new thiadiazole modulators of beta adrenergic receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: June 9, 2010
    Publication date: April 14, 2011
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Tadimeti Rao, Chengzhi Zhang
  • Patent number: 7875609
    Abstract: The present invention provides compounds of Formula (I): in which R1, R?1, R2, R?2, R3, and Y have the meanings given in the description are useful in the treatment of conditions susceptible to modulating ion channels, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: October 31, 2006
    Date of Patent: January 25, 2011
    Assignee: Galapagos Sasu
    Inventors: Hélène Jary, Taoues Temal, Pierre DePrez
  • Publication number: 20100227865
    Abstract: The invention provides Beta-blocker drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a different biological membrane crossing rate as compared to the biological membrane crossing rate of the Beta-blocker drug not attached to the water soluble oligomer.
    Type: Application
    Filed: March 12, 2008
    Publication date: September 9, 2010
    Inventors: Jennifer Riggs-Sauthier, Franco J. Duarte, Aaron S. Hammons
  • Publication number: 20100215710
    Abstract: Methods for increasing rate of healing of wounds in epithelial tissues by administration of beta-2 adrenergic receptor antagonists to target patients are provided. Methods for decreasing cell growth around implanted devices and methods for decreasing wound contraction by administration of beta-2 adrenergic receptor agonists are also provided. Pharmaceutical compositions and kits including beta-2 adrenergic receptor agonists and antagonists are described, as are devices coated with beta-2 adrenergic receptor agonists.
    Type: Application
    Filed: April 10, 2006
    Publication date: August 26, 2010
    Inventors: Roslyn Rivkah Isseroff, Christine E. Pullar
  • Patent number: 7767811
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: June 5, 2006
    Date of Patent: August 3, 2010
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang
  • Publication number: 20100190774
    Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.
    Type: Application
    Filed: April 8, 2010
    Publication date: July 29, 2010
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: David J. Lauffer, Alexander Aronov, Pan Li, David D. Deininger, Kira McGinty, Dean Stamos, Jon H. Come, Michelle Stewart
  • Publication number: 20100168108
    Abstract: Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.
    Type: Application
    Filed: January 18, 2010
    Publication date: July 1, 2010
    Applicant: Adolor Corporation
    Inventors: Roland E. Dolle, Karin Worm, Q. Jean Zhou
  • Patent number: 7691856
    Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, acute pain, acute and chronic inflammatory pain, and neuropathic pain using a compound of formula IA.
    Type: Grant
    Filed: January 9, 2007
    Date of Patent: April 6, 2010
    Assignees: Schering Corporation, Pharmacopeia, Inc.
    Inventors: Arthur G. Taveras, Jianhua Chao, Purakkattle J. Biju, Younong Yu, Cynthia J. Aki, J. Robert Merritt, Ge Li, John J. Baldwin, Gaifa Lai, Minglang Wu, Evan A. Hecker
  • Patent number: 7678789
    Abstract: The present invention relates to 5-imino-5H-[1,2,4]-dithiazol-3-yl-amine and [1,2,4]-dithiazolidine-3,5-diylidene-diamine derivatives as inducers of gluthathione-S-transferase (GST) and NADPH quinone oxidoreductase (NQO), to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said [1,2,4]-dithiazoli(di)ne derivatives. The invention also relates to the use of a compound disclosed herein for the treatment of adverse conditions associated with cytotoxicity in general and apoptosis in particular. The invention relates to compounds of the general formula (I): wherein wherein the symbols have the meanings given in the specification.
    Type: Grant
    Filed: February 9, 2006
    Date of Patent: March 16, 2010
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Roelof W. Feenstra, Hiskias G. Keizer, Maria L. Pras-Raves, Bernard J Van Vliet, Gustaaf J. M. Van Scharrenburg
  • Publication number: 20100063051
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.
    Type: Application
    Filed: October 31, 2007
    Publication date: March 11, 2010
    Inventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T.G. Murali Dhar
  • Publication number: 20100029625
    Abstract: A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R0 represents aryl, —NR1CONR2 (wherein R1 represents a hydrogen atom or the like, and R2 represents lower alkyl or the like) or the like, R3 represents lower alkyl, R4 represents a hydrogen atom or the like, and R5 represents aryl or the like].
    Type: Application
    Filed: June 22, 2006
    Publication date: February 4, 2010
    Applicants: KYOWA HAKKO KIRIN CO., LTD., FUJIFILM CORPORATION
    Inventors: Ryuichiro Nakai, Emi Shimoike, Hideaki Kusaka, Chikara Murakata, Yoshinori Yamashita