Cyano Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Triazole Ring Patents (Class 548/266.8)
  • Patent number: 9040653
    Abstract: This disclosure provides methods of controlled polymerization of cyclic compounds catalyzed by carbene derivatives having a general formula as shown below, and to obtain a biodegradable polymeric material having a large molecular weight, a narrow dispersity, and no metallic impurity.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: May 26, 2015
    Assignee: NANJING UNIVERSITY OF TECHNOLOGY
    Inventors: Zhenjiang Li, Pingkai Ouyang, He Huang
  • Publication number: 20150133658
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: August 15, 2014
    Publication date: May 14, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20150011730
    Abstract: Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.
    Type: Application
    Filed: September 22, 2014
    Publication date: January 8, 2015
    Inventors: Campbell McInnes, Shu Liu
  • Publication number: 20140364603
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Patent number: 8871792
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: October 28, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • Patent number: 8865755
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: October 21, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Robert Murray McKinnell, Brooke Blair
  • Patent number: 8846913
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3—R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: September 30, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20140288301
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Inventors: Dinesh U. Chimmanamada, Joseph A. Burlison, Weiwen Ying, Lijun Sun, Stefan M. Schweizer, Shijie Zhang, Zachary Demko, David James, Teresa Kowalczyk-Przewloka
  • Publication number: 20140275523
    Abstract: Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: and intermediates useful for the preparation of I.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Genentech, Inc.
    Inventors: Remy Angelaud, Danial R. Beaudry, Diane E. Carrera, Sushant Malhotra, Travis Remarchuk, Frederic St-Jean
  • Patent number: 8703784
    Abstract: This invention relates to novel fused tricyclic compounds under Formula I that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 22, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoyang Meng, Panduranga Adulla P. Reddy, M. Arshad Siddiqui, Amit K. Mandal, Duan Liu, Lianyun Zhao, Andrew McRiner
  • Publication number: 20140046053
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 13, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Publication number: 20130303493
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 14, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Patent number: 8563526
    Abstract: The present invention relates to novel compounds of formula (A): in the form of a free base or of an addition salt with an acid. The invention also relates to process of preparation of compounds of formula (A), to composition comprising them and to their application in therapeutics and in particular in cancers.
    Type: Grant
    Filed: April 29, 2009
    Date of Patent: October 22, 2013
    Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Ling Peng, Palma Rocchi, Juan Iovanna, Yi Xia, Fanqi Qu, Jinqiao Wan, Yang Liu, Menghua Wang
  • Publication number: 20130245260
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: April 24, 2013
    Publication date: September 19, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20130245084
    Abstract: Compounds of general formula (I) their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: September 19, 2013
    Applicant: LEO PHARMA A/S
    Inventor: Kristoffer Mansson
  • Patent number: 8519137
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: October 10, 2008
    Date of Patent: August 27, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson
  • Publication number: 20130210874
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: November 20, 2012
    Publication date: August 15, 2013
    Applicant: THERAVANCE, INC.
    Inventor: THERAVANCE, INC.
  • Patent number: 8497292
    Abstract: Provided are methods and compositions for inhibiting eukaryotic translation initiation factor. Such methods and compositions may be used alone or in conjunction with other therapies, such as gene therapies, for inhibiting cell proliferation and/or treating cancer.
    Type: Grant
    Filed: June 27, 2008
    Date of Patent: July 30, 2013
    Assignee: Translational Therapeutics, Inc.
    Inventors: Gordon A. Jamieson, Jr., Katherine L. B. Borden, Biljana Culjkovic, Alex Kentsis
  • Publication number: 20130085276
    Abstract: The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives.
    Type: Application
    Filed: June 9, 2011
    Publication date: April 4, 2013
    Inventors: Steven P. Nolan, Catherine Cazin
  • Publication number: 20130053387
    Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.
    Type: Application
    Filed: May 4, 2011
    Publication date: February 28, 2013
    Applicant: FerroKin BioScience, Inc.
    Inventor: James W. Malecha
  • Publication number: 20130053416
    Abstract: 3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: July 26, 2012
    Publication date: February 28, 2013
    Applicant: SANOFI
    Inventors: Sven RUF, Josef PERNERSTORFER, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Klaus WIRTH
  • Publication number: 20130005739
    Abstract: The present invention relates to pharmaceutical compositions comprising a COS releasing compound according to formula (I) and to methods of preparing such compositions. Said pharmaceutical compositions may preferably be used for the treatment and/or the prevention of cardiovascular diseases.
    Type: Application
    Filed: December 28, 2010
    Publication date: January 3, 2013
    Applicants: LUDWIG BOLTZMANN CLUSTER FUER KARDIOVASKULAERE FORSCHUNG, UNIVERSITAET WIEN
    Inventors: Thomas Erker, Gerda Brunhofer, Christian Studenik, Bruno Podesser, Gabriela Pomper
  • Publication number: 20120309724
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: May 18, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
  • Publication number: 20120213807
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Cameron Smith
  • Publication number: 20120213806
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: February 16, 2012
    Publication date: August 23, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Patent number: 8198461
    Abstract: The present invention provides compounds and methods that can be used to convert 1,2,4-triazole-3-carboxamides to the corresponding 3-cyano-1,2,4-triazoles reliably in one step, with high yields and without the need for elaborate purification.
    Type: Grant
    Filed: May 8, 2009
    Date of Patent: June 12, 2012
    Assignee: AMPAC Fine Chemicals LLC.
    Inventors: Der-Shing Huang, Benjamin Mendoza, Aslam A. Malik
  • Publication number: 20120129901
    Abstract: Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.
    Type: Application
    Filed: May 20, 2010
    Publication date: May 24, 2012
    Inventors: Jorge Antonio Ribeiro Salvador, Rita Catarina Mendes Dos Santos, Marta Cascante Serratosa
  • Publication number: 20120116095
    Abstract: The present invention aims to provide novel compounds represented by formula [I] or pharmaceutically acceptable salts thereof: which are useful for prevention or treatment of diseases such as schizophrenia, Alzheimer's disease, cognitive impairment, dementia, anxiety disorders (e.g., generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, acute stress disorder), depression, drug dependence, convulsion, tremor, pain, or sleep disorders, based on their inhibitory effect against glycine uptake.
    Type: Application
    Filed: July 15, 2010
    Publication date: May 10, 2012
    Applicant: TAISHO PHARMACEUTICAL C0., LTD.
    Inventors: Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Masato Hayashi, Yoshihisa Shirasaki, Shuji Yamamoto, Youichi Shimazaki, Yuko Araki, Kumi Abe, Xiang-Min Sun
  • Publication number: 20120101072
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: December 21, 2011
    Publication date: April 26, 2012
    Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Publication number: 20120065191
    Abstract: The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.
    Type: Application
    Filed: December 23, 2009
    Publication date: March 15, 2012
    Applicant: BIAL - PORTELA & Cª, S.A.
    Inventors: Laszlo Erno Kiss, David Alexander Learmonth, Carla Patrícia da Costa Pereira Rosa, Rita Gusmão de Noronha, Pedro Nuno Leal Palma, Patrício Manuel Vieira Araújo Soares da Silva, Alexander Beliaev
  • Publication number: 20110237528
    Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-3 or encompassed by formulas (I), (IA), (IB), (II), and (III)) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
    Type: Application
    Filed: September 16, 2009
    Publication date: September 29, 2011
    Applicant: INSTITUTE FOR ONEWORLD HEALTH
    Inventors: Graham Peter Jones, Kevin James Doyle
  • Publication number: 20110224206
    Abstract: The present invention relates to substituted pyrrole compounds of formula I and compositions comprising substituted tri-substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a tri-substituted’ triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: August 7, 2009
    Publication date: September 15, 2011
    Inventors: Weiwen Ying, Dinesh U. Chimmanamada, Joseph A. Burlison, Shijie Zhang, Minghu Song, Junghyun Chae
  • Publication number: 20110136754
    Abstract: The present invention relates to novel compounds of formula (A): in the form of a free base or of an addition salt with an acid. The invention also relates to process of preparation of compounds of formula (A), to composition comprising them and to their application in therapeutics and in particular in cancers.
    Type: Application
    Filed: April 29, 2009
    Publication date: June 9, 2011
    Inventors: Ling Peng, Palma Rocchi, Juan Iovanna, Yi Xia, Fanqi Qu, Jinqiao Wan, Yang Liu, Menghua Wang
  • Publication number: 20110092368
    Abstract: The present invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y and CKE have the meanings given in the disclosure, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention further relates to selectively herbicidal compositions containing 2,4,6-phenyl-substituted cyclic ketoenols and a compound which improves crop plant tolerance.
    Type: Application
    Filed: December 17, 2010
    Publication date: April 21, 2011
    Inventors: Reiner Fischer, Klaus Kunz, Stefan Lehr, Michael Ruther, Udo Schneider, Markus Dollinger, Mark Wilhelm Drewes, Dieter Feucht, Jörg Konze, Ulrike Wachendorff-Neumann, Guido Bojack, Thomas Auler, Martin Jeffrey Hills, Thomas Bretschneider, Olga Malsam, Christoph Erdelen, Angelika Lubos-Erdelen, Alfred Angermann, Hein Kehne, Christopher Hugh Rosinger
  • Publication number: 20100324071
    Abstract: Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
    Type: Application
    Filed: August 30, 2010
    Publication date: December 23, 2010
    Inventors: Yan Shi, Peter T. W. Cheng, Ying Wang, Denis E. Ryono
  • Publication number: 20100267725
    Abstract: The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or 2 or encompassed by formula I) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
    Type: Application
    Filed: April 20, 2010
    Publication date: October 21, 2010
    Inventors: Michael Geoffrey Neil Russell, Kevin James Doyle
  • Publication number: 20100256357
    Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.
    Type: Application
    Filed: July 30, 2007
    Publication date: October 7, 2010
    Inventors: Wesley Kwan Mung Chong, Andrew M. Haidle, Martha Alicia Ornelas, Lin Li, Seiji Nukui, Eugene Yuanjin Rui, Min Teng, William Francois Vernier, Joe Zhongxiang Zhou
  • Publication number: 20100113447
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: August 10, 2009
    Publication date: May 6, 2010
    Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Publication number: 20100113277
    Abstract: The present invention provides a broadleaf perennial weed control agent for grass, which has a powerful herbicide effect on weeds that have proven difficult to control with conventional herbicides for grass and/or on weeds having resistance to conventional herbicides, and yet is safe for use on grasses; and a method for controlling broadleaf perennial weeds in grass by applying the control agent to the soil or the foliage.
    Type: Application
    Filed: February 1, 2008
    Publication date: May 6, 2010
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Akira Ohno, Yasuji Okunishi, Takashi Sato
  • Publication number: 20100035929
    Abstract: Disclosed are dispyrin analogue compounds useful as H3 receptor activity modulators, methods of making same, pharmaceutical compositions comprising same, and methods of treating neurological and psychiatric disorders associated with histamine H3 receptor activity using same. In one aspect, the disclosed analogues can have a structure represented by a formula: This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 8, 2009
    Publication date: February 11, 2010
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, J. Phillip Kennedy, John T. Brogan
  • Publication number: 20100022599
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: July 23, 2009
    Publication date: January 28, 2010
    Inventors: Seok-Ki CHOI, Paul R. FATHEREE, Roland GENDRON, Robert Murray MCKINNELL, Brooke BLAIR
  • Publication number: 20090292122
    Abstract: The present invention provides compounds and methods that can be used to convert nitrogen-containing-heteroaryl carboxamides to the corresponding nitrogen-containing-heteroaryl nitriles reliably in one step, with high yields and without the need for elaborate purification.
    Type: Application
    Filed: May 8, 2009
    Publication date: November 26, 2009
    Applicant: Ampac Fine Chemicals LLC
    Inventors: Der-Shing Huang, Benjamin Mendoza, Aslam A. Malik
  • Patent number: 7572822
    Abstract: Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: August 11, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Prasun K. Chakravarty, Louis L. Zuegner, III, legal representative, William H. Parsons, Brenda Palucki, Bishan Zhou, Min K. Park, Michael H. Fisher
  • Publication number: 20090176837
    Abstract: Disclosed herein are novel compounds with activity at RAR? 2 receptors. Further disclosed are the use of such compounds for treatment of or to alleviate symptoms of cancer, neurological disorders such as memory deficits and schizophrenia, neurodegenerative disorders such as Parkinson's and Alzheimer's diseases, inflammatory disorders such as psoriasis and rheumatoid arthritis, eye disorders and depression.
    Type: Application
    Filed: July 12, 2006
    Publication date: July 9, 2009
    Applicant: SONY CORPORATION
    Inventors: Roger Olsson, Fabrice Piu, Birgitte Lund
  • Publication number: 20090099233
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: October 10, 2008
    Publication date: April 16, 2009
    Inventors: Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson
  • Publication number: 20090074890
    Abstract: Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: November 5, 2004
    Publication date: March 19, 2009
    Inventors: Min K. Park, Prasun K. Chakravarty, Bishan Zhou, Edward Gonzalez, Hyun Ok, Brenda Palucki, William H. Parsons, Rosemary Sisco, Michael H. Fisher, Louis L. Zuegner, III
  • Publication number: 20090076282
    Abstract: To provide novel 3-triazolylphenyl sulfide derivatives having excellent soil treatment activity as insecticides, miticides or nematicides for agricultural and horticultural plants. 3-Triazolylphenyl sulfide derivatives represented by the formula [1]: wherein R is a cyclopropylmethyl group or a trifluoroethyl group, B2 is a hydrogen atom, a halogen atom or a methyl group, B4 is a halogen atom, a cyano group, a nitro group or a C1-C6 alkyl group, and each of A1 and A3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group which may be substituted or an amino group which may be substituted.
    Type: Application
    Filed: October 20, 2005
    Publication date: March 19, 2009
    Applicants: KUMIAI CHEMICAL INDUSTRY CO., LTD, IHARA CHEMICAL INDUSTRY CO., LTD
    Inventors: Keiji Toriyabe, Mikio Yamaguchi, Yoshihiro Ito, Shiori Kinpara, Hiroyuki Yano, Satoru Takahashi, Norihisa Yonekura, Ryuji Hamaguchi
  • Publication number: 20090069288
    Abstract: Disclosed herein are novel compounds of Formula (I), wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases as well as proliferative disorders such as cancer.
    Type: Application
    Filed: July 15, 2008
    Publication date: March 12, 2009
    Inventors: Eric C. Breinlinger, Kevin P. Cusack, Adrian D. Hobson, Bin Li, Thomas D. Gordon, Robert H. Stoffel, Grier A. Wallace, Pintipa Grongsaard, Lu Wang, Lu Wang
  • Publication number: 20090036451
    Abstract: The present invention relates to compounds and methods for inducing neuronal differentiation in normal neural stem cells and brain cancer stem cells. The methods may take place in vitro, such as in isolates from the adult mammalian brain, or in vivo. Compounds and methods described herein may find use in the treatment of neurodegenerative and psychiatric diseases, the repair and regeneration of the nervous system, and in treatment of neurologic malignancy.
    Type: Application
    Filed: October 12, 2007
    Publication date: February 5, 2009
    Inventors: Jay Schneider, Jenny Hsieh, Douglas Frantz, Steven L. McKnight, Joseph M. Ready
  • Patent number: 7402606
    Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.
    Type: Grant
    Filed: April 1, 2003
    Date of Patent: July 22, 2008
    Assignee: SmithKline Beecham Corporation
    Inventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano