The 4-position Of The Hetero Ring Is Unsubstituted Or Alkyl Substituted Only Patents (Class 540/362)
  • Publication number: 20150126371
    Abstract: The present invention relates to a pyrazolopyran of the general formula I wherein the variables are defined according to the description, including a tautomer, salt, cleavable prodrug, or mixtures thereof, in particular to said pyrazolopyran for use as a medicament and/or an inhibitor of the enzyme serinehydroxymethyltransferase (SHMT). The invention also relates to a process the preparation of a pyrazolopyran of the formula I, to compositions comprising said compound and processes for the preparation of these compositions. Further it relates to use of the pyrazolopyran of formula I as an herbicide as well as to a method of controlling undesired vegetation.
    Type: Application
    Filed: May 29, 2013
    Publication date: May 7, 2015
    Inventors: Matthias Witschel, Frank Stelzer, Johannes Hutzler, Tao Qu, Thomas Mietzner, Klaus Kreuz, Klaus Grossmann, Raphael Aponte, Hans Wolfgang Hoeffken, Frederick Calo, Thomas Ehrhardt, Anja Simon, Liliana Parra Rapado
  • Publication number: 20150105365
    Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7 R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 16, 2015
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
  • Publication number: 20150031108
    Abstract: The present invention provides a process for preparing a compound of Formula 5b, as well as intermediates thereof, and novel classes of compounds useful in process for preparing these and similar compounds.
    Type: Application
    Filed: December 10, 2012
    Publication date: January 29, 2015
    Inventors: Javier Magano, Mark Thomas Maloney, Olivier J. Marcq, Durgesh Vasant Nadkarni, Mark John Pozzo, John Joseph Teixeira, JR.
  • Patent number: 8859529
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: October 14, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Publication number: 20140296196
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
  • Publication number: 20140194389
    Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: WARNER CHILCOTT COMPANY, LLC
    Inventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
  • Patent number: 8765940
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: July 1, 2014
    Assignee: Amgen Inc.
    Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
  • Patent number: 8710215
    Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: April 29, 2014
    Assignee: Warner Chilcott Company, LLC
    Inventors: Frank Hallock Ebetino, Adam Wieslaw Mazur, Roy Lee Martin Dobson
  • Publication number: 20140093518
    Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
    Type: Application
    Filed: August 26, 2013
    Publication date: April 3, 2014
    Applicant: The Scripps Research Institute
    Inventor: Carlos F. Barbas, III
  • Publication number: 20140018342
    Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Application
    Filed: April 4, 2012
    Publication date: January 16, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
  • Publication number: 20130316999
    Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.
    Type: Application
    Filed: August 7, 2013
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
  • Publication number: 20130090323
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Application
    Filed: June 30, 2011
    Publication date: April 11, 2013
    Applicant: Amgen Inc.
    Inventors: Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
  • Publication number: 20130065875
    Abstract: The invention provides derivatives and analogues of triazatetracyclo[7.7.0.01,13,02,7]-hexadeca-2,4,6,10,12-pentaenes, 5,7,11-triazatetracyclo[8.7.0.01,6,012,17]-heptadeca-6,8,12,14,16-pentaenes, pharmaceutical compositions comprising these compounds and methods for treatment of hepatitis C viral infections using these compounds.
    Type: Application
    Filed: October 27, 2010
    Publication date: March 14, 2013
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, TRUSTEES OF BOSTON UNIVERSITY
    Inventors: John K. Snyder, Wanguo Wei, Feng Ni, Arthur Donny Strosberg, Smitha Kota, Virginia Takahashi
  • Publication number: 20130040930
    Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: April 27, 2011
    Publication date: February 14, 2013
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
  • Publication number: 20130035482
    Abstract: Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
    Type: Application
    Filed: October 12, 2012
    Publication date: February 7, 2013
    Applicant: WARNER CHILCOTT COMPANY, LLC
    Inventor: WARNER CHILCOTT COMPANY, LLC
  • Publication number: 20130023514
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) pyrrolotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: March 30, 2011
    Publication date: January 24, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventors: Jay A. Markwalder, Brian E. Fink, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Steven P. Seitz
  • Publication number: 20120101078
    Abstract: Disclosed are a series of neuropeptide Y Y5 receptor ligands, and as such are useful to treat disorders related to mood, stress, ADHD, cognition, stress and dementia.
    Type: Application
    Filed: March 19, 2010
    Publication date: April 26, 2012
    Applicant: H. Lundbrck A/S
    Inventors: Bin Chen, James Ford Burns, Dario Doller
  • Publication number: 20120094972
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Application
    Filed: June 25, 2010
    Publication date: April 19, 2012
    Applicant: AMGEN INC.
    Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
  • Publication number: 20120071459
    Abstract: The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.
    Type: Application
    Filed: June 2, 2010
    Publication date: March 22, 2012
    Inventors: Siegfried Benjamin Christensen, IV, Donghui Qin, Shuhul Chen, Shi Lu
  • Publication number: 20120015926
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Application
    Filed: November 9, 2009
    Publication date: January 19, 2012
    Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K.C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Publication number: 20120010181
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.
    Type: Application
    Filed: November 9, 2009
    Publication date: January 12, 2012
    Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K.C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Publication number: 20110311516
    Abstract: Provided herein is a method for chemically programmed vaccination. Methods include inducing a covalent-binding polyclonal antibody response in a subject and programming the polyclonal response with a targeting compound.
    Type: Application
    Filed: February 10, 2010
    Publication date: December 22, 2011
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventor: Carlos F. Barbas, III
  • Publication number: 20110288054
    Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
    Type: Application
    Filed: September 22, 2009
    Publication date: November 24, 2011
    Applicant: Schering Corporation
    Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K.C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Publication number: 20110166118
    Abstract: The present invention relates to a compound of Formula (I) in particular compounds of formula (Ia), the use of a therapeutically effective amount of one or more compounds of formula (I) or (Ia) as a broad-spectrum antibiotic and the use of a pharmaceutical composition comprising said compounds for the treatment of bacterial infections in humans or animals.
    Type: Application
    Filed: June 18, 2009
    Publication date: July 7, 2011
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Ivan Plantan, Andrej Prezelj, Uros Urleb, Barbara Mohar, Michel Stephan
  • Publication number: 20110144081
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Application
    Filed: December 7, 2010
    Publication date: June 16, 2011
    Inventors: Henner Knust, Andreas Koblet, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Publication number: 20110112063
    Abstract: The invention provides novel pyrimidine derivatives of formula I and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-IR) or analplastic lymphoma kinase (ALK).
    Type: Application
    Filed: June 24, 2009
    Publication date: May 12, 2011
    Inventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
  • Publication number: 20110105457
    Abstract: The purpose of the present invention is to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prevention/treatment of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. This was achieved by providing a substituted 2-amino-5,6-nitrogenated fused ring compound shown in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 16, 2009
    Publication date: May 5, 2011
    Inventors: Daisuke Taniyama, Kazuya Kano, Kazuya Okamoto, Masahiko Fujioka, Yasunori Mitsuoka
  • Publication number: 20110104043
    Abstract: The subject of the invention is the (50) continuous flow system for the synthesis of nanoparticles which consist of the (1a) feeding unit connected to the flow path, at least one (2) first reactor unit possessing the (13) heatable reactor-zone, the (3) second reactor unit which follows (2) in the same cascade; the (5) mixing unit and the (1b) second feeding unit between (2) and (3) reactor units, the (9) and (10) feeding pumps connected to the raw material source and/or (22) control unit which is capable of controlling at least one (18) pressure controller and/or controlling the temperature of at least one (13) heatable reactor-zone; each (13) heatable reactor-zone is followed by (14) cooling unit in the cascade. In addition, the subject of this invention is a process for the synthesis of nanoparticles, preferably metal-containing nanoparticles, and nanoparticles of biologically active organic molecules wherein the process is accomplished in the device according to FIG. 1.
    Type: Application
    Filed: April 28, 2009
    Publication date: May 5, 2011
    Applicant: Nangenex Nanotechnology Incorporated
    Inventors: Krisztián Niesz, Attila Wootsch, Maxime Groualle, Zsolt Ötvös, Ferenc Darvas
  • Publication number: 20110082129
    Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
    Type: Application
    Filed: June 25, 2009
    Publication date: April 7, 2011
    Inventors: Christopher Adams, Qi-Ying Hu, Leslie Wighton McQuire, Julien Papillon
  • Publication number: 20110046599
    Abstract: Compositions and methods for modifying biologically active substances to achieve multi-day delivery of such substances, particularly through oral or parenteral administration, are disclosed. The compositions include the biologically active substance conjugated to a carrier having a suitably long half life, typically more than one day, wherein the conjugate optionally contains a spacer linking the carrier to the biologically active substance. Pharmaceutical formulations of the conjugates are also disclosed, as are methods of extending delivery of a single dose of a biologically active substance for more than one day.
    Type: Application
    Filed: June 26, 2008
    Publication date: February 24, 2011
    Inventor: Agis Kydonieus
  • Publication number: 20110015389
    Abstract: Preparation of new heterocyclic compounds characterised by 1,3-imidazolidine structure useful for stereoselective synthesis of optically pure key intermediates in 1?-methylcarbapenem production
    Type: Application
    Filed: October 1, 2009
    Publication date: January 20, 2011
    Applicant: ACS DOBFAR S.p.A.
    Inventors: Mauro Freccero, Giovanni Fogliato, Antonio Manca, Michele Bassanini
  • Publication number: 20100311709
    Abstract: The present invention is directed to 2-[1-phenyl-5-hydroxy or methoxy-4alpha-methyl-hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives of formula I (I) as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: October 23, 2007
    Publication date: December 9, 2010
    Inventors: Christopher J. Bungard, Jesse J. Manikowski, James J. Perkins, Robert Meissner
  • Publication number: 20090227557
    Abstract: Disclosed herein is a compound comprising a formula or a pharmaceutically acceptable salt or a prodrug or a metabolite thereof; Y is A is —(CH2)6—, cis —CH2CH?CH—(CH2)3—, or —CH2C?C—(CH2)3—, wherein 1 or 2 carbon atoms may be substituted with S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is from 1 to 4, and wherein one CH2 may be substituted with S or O; and D is aryl or heteroaryl. Methods of use are also disclosed.
    Type: Application
    Filed: March 2, 2009
    Publication date: September 10, 2009
    Applicant: ALLERGAN, INC.
    Inventor: David W. Old
  • Publication number: 20090221546
    Abstract: Compounds useful as intermediates for synthesis of compounds of Formula (1): wherein A, B, C, G, and W1 have any of the values defined in the specification.
    Type: Application
    Filed: June 16, 2008
    Publication date: September 3, 2009
    Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
  • Publication number: 20090137546
    Abstract: This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.
    Type: Application
    Filed: September 29, 2006
    Publication date: May 28, 2009
    Inventors: Robert J. DeVita, Gregori J. Morriello, Peter Lin
  • Patent number: 7501404
    Abstract: Compounds are provided which have the structure Wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd? are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor VIIa, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.
    Type: Grant
    Filed: April 4, 2006
    Date of Patent: March 10, 2009
    Assignee: DAIMED
    Inventors: Thomas Bannister, Cassandra Celatka, Nizal S. Chandrakumar, Hongfeng Deng, Zihong Guo, Lei Jin, Tsvetelina Lazarova, Jian Lin, Scott T. Moe, Pamela Nagafuji, Manuel Navia, Amy Ripka, Michael J. Rynkiewicz, Kerry L. Spear, James E. Stickler, Roger Xie
  • Publication number: 20090023701
    Abstract: Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: August 29, 2008
    Publication date: January 22, 2009
    Inventors: Ronald A. Aungst, Derek Cogan, Amy L. Davis, Daniel R. Goldberg, Ming-Hong Hao, Zhaoming Xiong
  • Publication number: 20080287674
    Abstract: Compounds useful as intermediates for synthesis of compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification.
    Type: Application
    Filed: June 26, 2008
    Publication date: November 20, 2008
    Inventors: Christopher Franklin Bigge, Agustin Casimiro-Garcia, Danette Andrea Dudley, Jeremy John Edmunds, Kevin James Filipski, Jeffrey Thomas Kohrt, Chad Alan Van Huis
  • Publication number: 20080280869
    Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.
    Type: Application
    Filed: October 13, 2005
    Publication date: November 13, 2008
    Inventors: Neil Almstead, Gary M. Karp, Richard Wilde, Ellen Welch, Jeffrey A. Campbell, Hongyu Ren, Guangming Chen
  • Patent number: 7285545
    Abstract: Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 29, 2005
    Date of Patent: October 23, 2007
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Derek Cogan, Daniel R. Goldberg, Ming-Hong Hao, Zhaoming Xiong, Ronald A. Aungst, Amy L. Davis
  • Patent number: 7179907
    Abstract: The present invention provides methods for identifying (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity. The method involves the selection of RNA biocatalysts that promote the formation of (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity from component reactants. The invention also provides novel (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives with anti-PBP2a activity identified by these methods. The invention also provides RNA biocatalysts that are capable of catalyzing the formation of (3-amino-2-oxo-azetidin-1-yl) acetic acid derivatives from component reactants.
    Type: Grant
    Filed: December 18, 2002
    Date of Patent: February 20, 2007
    Inventors: Bruce Eaton, Theodore M. Tarasow, Dan Nieuwlandt, Torin Dewey
  • Patent number: 7176196
    Abstract: The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.
    Type: Grant
    Filed: May 11, 2005
    Date of Patent: February 13, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: B. Narasimhulu Naidu, Jacques Banville, Francis Beaulieu, Timothy P. Connolly, Mark R. Krystal, John D. Matiskella, Carl Ouellet, Serge Plamondon, Roger Remillard, Margaret E. Sorenson, Yasutsugu Ueda, Michael A. Walker
  • Patent number: 7157447
    Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.
    Type: Grant
    Filed: November 29, 2005
    Date of Patent: January 2, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: B. Narasimhulu Naidu, Jacques Banville, Francis Beaulieu, Timothy P. Connolly, Mark R. Krystal, John D. Matiskella, Carl Ouellet, Serge Plamondon, Roger Remillard, Margaret E. Sorenson, Yasutsugu Ueda, Michael A. Walker
  • Patent number: 7022842
    Abstract: It is an object of the present invention to provide a method for synthesizing ?-lactams and a method for manufacturing ?-lactams in water of high-temperature and under high-pressure, and the present invention relates to a ?-lactam synthesis method which is characterized in that ?-lactams are synthesized by reacting ?-amino acids in water at high-temperature and under high-pressure, this method being further characterized in that ?-lactams are synthesized at a high speed by cyclizing ?-amino acids in water at high-temperature and under high-pressure in which the temperature range is 200° C. or higher and the pressure range is 10 MPa or greater, and the present invention also relates to a method for manufacturing ?-lactams which is characterized in that ?-lactams are synthesized by reacting ?-amino acids in water at high-temperature and under high-pressure, and are then separated and purified using a column separation medium.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: April 4, 2006
    Assignee: National Institute of Advanced Industrial Science and Technology
    Inventors: Kiyotaka Hatakeda, Osamu Sato, Mitsuhiro Kanakubo, Yutaka Ikushima, Kazuo Torii
  • Patent number: 7018642
    Abstract: The present invention provides nitrogen heterocyclic compounds, compositions, and methods for controlling biofilms, i.e., disrupting biofilms, preventing biofilm formation, enhancing biofilms, or modifying biofilms. Methods for screening test compounds for control of biofilms and devices for use therein are also provided.
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: March 28, 2006
    Assignee: The Procter & Gamble Company
    Inventors: Charles Raymond Degenhardt, Rowan Andrew Grayling, Christopher Andrew Dille, Cheryl Sue Tansky
  • Patent number: 7015320
    Abstract: The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) process, comprising: contacting a compound of formula (II): with hydrogen under a suitable pressure in the presence of an iridium complex of the formula (R2)IrL+X? wherein L is a chelating diene, X is a non coordinating anion, and R2 is selected from
    Type: Grant
    Filed: March 18, 2003
    Date of Patent: March 21, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: William A. Nugent, Tai Yue
  • Patent number: 6967196
    Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: November 22, 2005
    Assignees: Bristol-Myers Squibb Company, Merck & Co. Inc.
    Inventors: David W. Smith, Benito Munoz, Kumar Srinivasan, Carl P. Bergstrom, Prasad V. Chaturvedula, Milind S. Deshpande, Daniel J. Keavy, Wai Yu Lau, Michael F. Parker, Charles P. Sloan, Owen B. Wallace, Henry Hui Wang
  • Patent number: 6900312
    Abstract: The present discovery consists in new thiazole-substituted ?-lactams of general formula (I), as well as the method for their preparation. R1, R2, R3, R4, R5, R6, R7, and R8 are, independently from each other, a hydrogen atom, a halogen, a hydroxy, amino, nitro, or thiol group, an optionally substituted alkyl, heteroalkyl, aryl, aralkyl, cycloalkyl, cycloaralkyl, heterocycloalkyl, heteroaralkyl, or heteroaryl rest.
    Type: Grant
    Filed: July 16, 2002
    Date of Patent: May 31, 2005
    Assignee: Priaton GmbH
    Inventors: Juergen Kolb, Alexander Doemling
  • Patent number: 6890921
    Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the ?-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.
    Type: Grant
    Filed: March 15, 2000
    Date of Patent: May 10, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Linda Jolliffe, William Murray, Virginia Pulito, Allen Reitz, Xiaobing Li, Linda Mulcahy, Cynthia Maryanoff, Frank Villani
  • Patent number: RE38947
    Abstract: A chiral catalyst is disclosed together with methods of using it for enantioselective syntheses. The chiral catalyst includes a nucleus with two metal atoms that has four bridging ligands oriented radially to the axis of the nucleus. Each of these ligands includes a two complexing atoms each complexed to one of the metal atoms. At least one of the bridging ligands includes a chiral center which is bonded to one of the complexing atoms. Preferably, all four of the bridging ligands include a chiral center bonded to one of the complexing atoms. The catalyst of the invention has been found to be useful in catalyzing carbenoid transformation reactions such as cyclopropanation.
    Type: Grant
    Filed: February 14, 1996
    Date of Patent: January 24, 2006
    Assignee: Research Corporation Technologies, Inc.
    Inventor: Michael P. Doyle