Polycyclo Ring System Having The Thiadiazine Ring As One Of The Cyclos Patents (Class 544/9)
  • Publication number: 20150051197
    Abstract: Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease, attention deficit hyperactivity disorder (ADHD) and the like. The compound represented by formula (I): wherein each symbol is as defined in the DESCRIPTION, or a salt thereof has an AMPA receptor function enhancing action, and is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
    Type: Application
    Filed: February 7, 2013
    Publication date: February 19, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masashi Toyofuki, Shinji Nakamura, Eiji Honda
  • Publication number: 20120214803
    Abstract: The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
    Type: Application
    Filed: February 2, 2012
    Publication date: August 23, 2012
    Applicant: VIFOR (INTERNATIONAL) AG
    Inventors: Wilm Buhr, Susanna Burckhardt, Franz Dürrenberger, Felix Funk, Peter O. Geisser, Vincent A. Corden, Stephen M. Courtney, Graham Dawson, Tara Davenport, Mark Slack, Mark P. Ridgill, Chrostopher J. Yarnold, Susan Boyce, Albertus A. Ellenbroek
  • Publication number: 20110271363
    Abstract: A soybean cultivar designated 93360433 is disclosed. The invention relates to the seeds of soybean cultivar 93360433, to the plants of soybean 93360433, to plant parts of soybean cultivar 93360433, and to methods for producing a soybean plant produced by crossing soybean cultivar 93360433 with itself or with another soybean variety. The invention also relates to methods for producing a soybean plant containing in its genetic material one or more transgenes and to the transgenic soybean plants and plant parts produced by those methods. This invention also relates to soybean cultivars, or breeding cultivars, and plant parts derived from soybean variety 93360433, to methods for producing other soybean cultivars, lines or plant parts derived from soybean cultivar 93360433, and to the soybean plants, varieties, and their parts derived from use of those methods. The invention further relates to hybrid soybean seeds, plants, and plant parts produced by crossing the cultivar 93360433 with another soybean cultivar.
    Type: Application
    Filed: April 29, 2010
    Publication date: November 3, 2011
    Applicants: MONSANTO TECHNOLOGY LLC, STINE SEED FARM, INC.
    Inventor: William H. Eby
  • Publication number: 20110224155
    Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
    Type: Application
    Filed: June 3, 2008
    Publication date: September 15, 2011
    Applicant: SENOMYX INC.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D.A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Mark Zoller, Karen Zoller
  • Publication number: 20110110948
    Abstract: Disclosed are novel gamma secretase inhibitors of the formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, wherein L1, n, X, Ar, Y, Z, Q, and Q1 are as defined herein. Also disclosed are methods for inhibiting gamma secretase, methods for treating Alzheimer's disease, methods of treating one or more neurodegenerative diseases, and methods of inhibiting the deposition of amyloid protein (e.g., amyloid beta protein) in, on or around neurological tissue (e.g., the brain) using the compounds of formula 1.0.
    Type: Application
    Filed: July 15, 2008
    Publication date: May 12, 2011
    Applicant: SCHERING CORPORATION
    Inventors: Thavalakulamgara K. Sasikumar, Duane A. Burnett, Theodros Asberom, Wen-Lian Wu, Hongmei Li, Ruo Xu, Hubert B. Josien
  • Patent number: 7902203
    Abstract: The present invention provides an HCV polymerase inhibiting compound having the formula (I) and a composition comprising a therapeutically effective amount of said compound. The present invention also provides a method for inhibiting hepatitis C virus (HCV) polymerase, a method for inhibiting HCV viral replication, and a method for treating or preventing HCV infection. Processes for making said compounds, and synthetic intermediates employed in said processes, are also provided.
    Type: Grant
    Filed: October 31, 2003
    Date of Patent: March 8, 2011
    Assignee: Abbott Laboratories, Inc.
    Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang, Hui-Ju Chen, William J. Flosi, Larry L. Klein, Allan C. Krueger, Dachun Liu, Darold L. Madigan, Laura M. Maymon, Todd W. Rockway, Kent D. Stewart, Ming C. Yeung, Qinghua Xie
  • Publication number: 20110009624
    Abstract: The present invention provides a compound that has superior gastric acid secretion inhibitory action, ample long-lasting gastric acid secretion inhibitory action, and is able to maintain intragastric pH at a high level for an extended period of time, making it useful as a therapeutic or prophylactic agent for diseases or symptoms caused by gastric acid, as well as an active form of this compound (form to which the compound is converted in the body following administration thereof) in the form of a compound represented by general formula (1a) (wherein R2 represents a group represented by formula (I) or the like, and R1, R3, W1 and X? are as defined in the description).
    Type: Application
    Filed: October 11, 2007
    Publication date: January 13, 2011
    Inventors: Masato Ueda, Daisuke Iida, Sachiko Kikuchi, Masaharu Gotoda
  • Publication number: 20110010787
    Abstract: The invention relates to the soybean variety designated A1016497. Provided by the invention are the seeds, plants and derivatives of the soybean variety A1016497. Also provided by the invention are tissue cultures of the soybean variety A1016497 and the plants regenerated therefrom. Still further provided by the invention are methods for producing soybean plants by crossing the soybean variety A1016497 with itself or another soybean variety and plants produced by such methods.
    Type: Application
    Filed: February 3, 2010
    Publication date: January 13, 2011
    Inventor: CRAIG MOOTS
  • Publication number: 20100305109
    Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring G1, X, R1, and R2 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Application
    Filed: May 28, 2010
    Publication date: December 2, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Marc J. Scanio, William H. Bunnelle, William A. Carroll, Sridhar Peddi, Arturo Perez-Medrano, Lei Shi
  • Publication number: 20100261714
    Abstract: Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: April 8, 2010
    Publication date: October 14, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Claudio STURINO, Patrick DEROY, Martin DUPLESSIS, Paul J. EDWARDS, Anne-Marie FAUCHER, Teddy HALMOS, Clint JAMES, Jean-Eric LACOSTE, Eric MALENFANT, Joannie MINVILLE, Louis MORENCY, Sebastien MORIN, Martin TREMBLAY, Christiane YOAKIM
  • Publication number: 20100234350
    Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 14, 2009
    Publication date: September 16, 2010
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
  • Publication number: 20090292120
    Abstract: The present invention provides a compound that has superior gastric acid secretion inhibitory action, ample long-lasting gastric acid secretion inhibitory action, and is able to maintain intragastric pH at a high level for an extended period of time, making it useful as a therapeutic or prophylactic agent for diseases or symptoms caused by gastric acid, as well as an active form of this compound (form to which the compound is converted in the body following administration thereof) in the form of a compound represented by general formula (1a) (wherein R2 represents a group represented by formula (I) or the like, and R1, R3, W1 and X? are as defined in the description).
    Type: Application
    Filed: October 11, 2007
    Publication date: November 26, 2009
    Inventors: Masato Ueda, Daisuke Iida, Sachiko Kikuchi, Masaharu Gotoda
  • Publication number: 20080312218
    Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.
    Type: Application
    Filed: September 21, 2006
    Publication date: December 18, 2008
    Inventors: Duane A. Burnett, Wen-Lian Wu
  • Patent number: 7262189
    Abstract: Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, X represents oxygen or sulphur, Y represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or halogen, their isomers and also their addition salts Medicaments.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: August 28, 2007
    Assignee: Les Laboratoires Server
    Inventors: Alex Cordi, Patrice Desos, Pierre Lestage
  • Patent number: 7262190
    Abstract: The invention relates to compounds of formula (I): wherein: R1 represents hydrogen, alkyl or cycloalkyl, R2 represents hydrogen, halogen or hydroxy, A represents CR3R4 or NR3 wherein R3 and R4 are as defined in the description, Y represents an alkylene chain as described in the description, X represents NR5R6, S(O)nR7, OR8, C(O)R9, amidino or a heterocycle, their isomers, and addition salts thereof; and medicinal products containing the same which are useful in the prevention or treatment of diseases associated with AMPA flux.
    Type: Grant
    Filed: December 8, 2005
    Date of Patent: August 28, 2007
    Assignee: Les Laboratoires Servier
    Inventors: Patrice Desos, Alexis Cordi, Pierre Lestage, Laurence Danober
  • Patent number: 7253161
    Abstract: Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or halogen, their isomers and also their addition salts. Medicaments.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: August 7, 2007
    Assignee: Les Laboratoires Servier
    Inventors: Alex Cordi, Patrice Desos, Pierre Lestage
  • Patent number: 7253163
    Abstract: Compounds of formula (I): wherein: R1 represents a heterocycle, R2 represents hydrogen, a halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with the adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or a halogen, their isomers, and also addition salts thereof.
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: August 7, 2007
    Assignee: Les Laboratoires Servier
    Inventors: Patrice Desos, Alex Cordi, Pierre Lestagé
  • Patent number: 7253162
    Abstract: Compounds of formula (I): wherein: R1 represents hydrogen, a halogen or alkyl, R1a represents hydrogen or alkyl, R2 represents hydrogen, a halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with the adjacent —CHR3—, forms the ring ?wherein m represents 1, 2 or 3, R5 represents hydrogen or a halogen, X is as defined in the description, their isomers, and also addition salts thereof.
    Type: Grant
    Filed: June 10, 2004
    Date of Patent: August 7, 2007
    Assignee: Les Laboratoires Servier
    Inventors: Patrice Desos, Alex Cordi, Pierre Lestage
  • Patent number: 7244843
    Abstract: The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
    Type: Grant
    Filed: October 5, 2004
    Date of Patent: July 17, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Dean A. Wacker, Jeffrey G. Varnes
  • Patent number: 7196194
    Abstract: A yellow dye-forming coupler represented by formula (I): wherein Q represents a group of nonmetallic atoms that form a 5- to 7-membered ring in combination with the —N?C—N(R1)—; R1 and R2 each represent a substituent; R4 represents an alkyl group; m represents an integer of 0 to 4; and X represents a hydrogen atom, or a group capable of being split-off upon a coupling reaction with an oxidized product of a developing agent; and when R4 represents a primary alkyl group, R1 represents —(CH2)3O—R101 in which R101 is an alkyl group having 4 to 8 carbon atoms. A silver halide color photographic light-sensitive material having at least one yellow dye-forming coupler represented by formula (I) in at least one layer provided on a support.
    Type: Grant
    Filed: October 7, 2003
    Date of Patent: March 27, 2007
    Assignee: Fuji Photo Film Co., Ltd
    Inventors: Kiyoshi Takeuchi, Shigeki Uehira, Mario Aoki, Jun Ogasawara, Yasuhiro Shimada, Seiji Ichijima, Yasuaki Deguchi, Naoto Matsuda, Akira Ikeda, Hisashi Mikoshiba, Masaharu Sugai, Taiji Katsumata
  • Patent number: 6943159
    Abstract: The invention provides novel compounds represented by general formula (I) wherein the bond represented by the broken line may be a single, double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R2; X represents SO2 or C?O of CH2; Y represents —CH(R4)—, —N(R4)—CH2—, O; and the meaning of R2, R3, R4, R5, R6, R7, and R8 are as defined in the application. The compounds are useful as positive modulators of the AMPA-receptor.
    Type: Grant
    Filed: August 18, 2000
    Date of Patent: September 13, 2005
    Assignee: Neurosearch A/S
    Inventors: Alex Haahr Gouliaev, Mogens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Jørgen Scheel-Krüger, Gunnar M. Olsen, Elsebet Østergaard Nielsen
  • Patent number: 6906063
    Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: June 14, 2005
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-MaGuire
  • Patent number: 6878711
    Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: April 12, 2005
    Assignee: Lilly Icos LLC
    Inventors: Mark W. Orme, Jason Scott Sawyer, Lisa M. Schultze
  • Publication number: 20040162285
    Abstract: Compounds having the formula 1
    Type: Application
    Filed: July 23, 2003
    Publication date: August 19, 2004
    Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang
  • Publication number: 20040039197
    Abstract: The invention relates to novel, substituted, fused indole and heteroindole derivatives of the general formula I 1
    Type: Application
    Filed: August 30, 2002
    Publication date: February 26, 2004
    Inventors: Heinz Weinberger, Thomas Beckers, Mathias Schmidt, Silke Baasner, Bernd Nickel
  • Publication number: 20040023953
    Abstract: The invention relates to mercaptomethyl-substituted thiazolo[2,3-b]quinazolines, oxazolo[2,3-b]quinazolines and imidazolo[2,1-b]quinazolines.
    Type: Application
    Filed: July 30, 2003
    Publication date: February 5, 2004
    Inventors: Uwe Kausmeier, Jochen Heinicke, Christoph Arkona
  • Patent number: 6683028
    Abstract: The invention relates to novel guanidine derivatives of the formula (I) in which A, R1, R2, R3 and Z are as defined in the description, to a process for their preparation and to their use for controlling animal pests.
    Type: Grant
    Filed: August 17, 2001
    Date of Patent: January 27, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Wagner, Christoph Erdelen, Andreas Turberg, Norbert Mencke, Olaf Hansen
  • Publication number: 20040014747
    Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animal, such as stroke.
    Type: Application
    Filed: February 3, 2003
    Publication date: January 22, 2004
    Applicant: Neurocrine Biosciences, Inc.
    Inventor: Mustapha Haddach
  • Patent number: 6667306
    Abstract: The invention relates to novel compounds of formula (I) containing fused heterocyclic ring systems which are effective platelet ADP receptor inhibitors: In formula (I), W is carbon or nitrogen, wherein at least one W is a carbon; and Y is nitrogen, oxygen, or sulfur. Such compounds including pharmaceutically acceptable salts are useful in various pharmaceutical compositions for the prevention and/or treatment of cardiovascular disease particularly those related to thrombosis.
    Type: Grant
    Filed: January 7, 1999
    Date of Patent: December 23, 2003
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Alan M. Laibelman, Hans-Michael Jantzen, Pamela B. Conley, Larry J. Fretto, Robert M. Scarborough
  • Publication number: 20030229080
    Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Application
    Filed: April 9, 2003
    Publication date: December 11, 2003
    Inventors: Mark W Orme, Jason Scott Sawyer, Lisa M Schultze
  • Publication number: 20030207867
    Abstract: Compounds of general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Application
    Filed: January 15, 2003
    Publication date: November 6, 2003
    Inventors: Mark W. Orme, Jason Scott Sawyer, Lisa M Schultze
  • Patent number: 6635635
    Abstract: Compound of formula (I): wherein: R1 represents hydroxy, RCO—O— or RCO—NRa—, R2 represents hydrogen, halogen, or hydroxy, R′CO—O or R′CO—NR′a—, R and R′, which may be identical or different, represent linear or branched (C1-C6)alkyl optionally substituted by aryl, linear or branched (C2-C6)alkenyl optionally substituted by aryl, linear or branched (C1-C6)perhaloalkyl, (C3-C7)cycloalkyl, adamantyl, aryl or heteroaryl, Ra and R′a, which may be identical or different, represent hydrogen or linear or branched (C1-C6)alkyl, linear or branched (C1-C6)perhaloalkyl, linear or branched (C1-C6)acyl, aryl or heteroaryl, its isomer and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as AMPA modulators.
    Type: Grant
    Filed: July 27, 2001
    Date of Patent: October 21, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Alex Cordi, Patrice Desos, François Lefoulon, Pierre Lestage
  • Patent number: 6624159
    Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
    Type: Grant
    Filed: June 22, 2001
    Date of Patent: September 23, 2003
    Assignee: Pharmacia & Upjohn Company
    Inventors: David John Anderson, Gordon L. Bundy, Fred L. Ciske, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Ronald Turner, Valerie A. Vaillancourt, Allison J. Wolf
  • Patent number: 6541469
    Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein X is nitrogen or CR3; A is O, S, or NR4, and R, R1, R2are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.
    Type: Grant
    Filed: May 18, 2001
    Date of Patent: April 1, 2003
    Assignee: Neurocrine Biosciences, Inc.
    Inventor: Mustapha Haddach
  • Patent number: 6518422
    Abstract: Process for the industrial synthesis of (3aS)-5,5-dioxo-2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c][1,2,4]benzothiadiazine of formula (I): by enantioselective catalytic hydrogenation of 5,5-dioxo-2,3-dihydro-1H-pyrrolo[2,1-c][1,2,4]benzothiadiazine.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: February 11, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Elsa Foucher, Gilles Thominot, Jean-Pierre Lecouve, James Andrew Ramsden, Christopher James Cobley
  • Publication number: 20020161222
    Abstract: Process for the industrial synthesis of (3aS)-5,5-dioxo-2,3,3a,4-tetrahydro-1H-pyrrolo-[2,1-c][1,2,4]benzothiadiazine of formula (I): 1
    Type: Application
    Filed: April 18, 2002
    Publication date: October 31, 2002
    Inventors: Elsa Foucher, Gilles Thominot, Jean-Pierre Lecouve, James Andrew Ramsden, Christopher James Cobley
  • Publication number: 20020037894
    Abstract: Compound of formula (I): 1
    Type: Application
    Filed: July 27, 2001
    Publication date: March 28, 2002
    Inventors: Alex Cordi, Patrice Desos, Francois Lefoulon, Pierre Lestage
  • Publication number: 20020032194
    Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.
    Type: Application
    Filed: May 18, 2001
    Publication date: March 14, 2002
    Inventor: Mustapha Haddach
  • Patent number: 5846969
    Abstract: A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).
    Type: Grant
    Filed: June 11, 1997
    Date of Patent: December 8, 1998
    Assignee: Eisai Co., Ltd.
    Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
  • Patent number: 5817820
    Abstract: The present invention relates to optical isomers of quinoline compounds of Formula (IA) or Formula (IA'), their pharmaceutically acceptable salts and their intermediates: ##STR1## In the above formulae, A represent nitrogen or ##STR2## in which Y represents hydrogen, halogen such as fluorine or chlorine, lower alkyl or lower alkoxy such as methoxy, or together with R.sub.1 forms --CH.sub.2 CH.sub.2 CH.sub.2 --, CH.sub.2 CH.sub.2 CH(CH.sub.3)--, --OCH.sub.2 CH.sub.2 --, --OCH.sub.2 CH(CH.sub.3)--, --SCH.sub.2 CH.sub.2 -- or --SCH.sub.2 CH(CH.sub.3)--; R.sub.1 is as defined above or represents straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms, a straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms which is substituted with a halogen atom, a phenyl group or a phenyl group substituted with one or two halogen atoms, such as ethyl, cyclopropyl or 2,4-difluorophenyl; R.sub.
    Type: Grant
    Filed: July 20, 1994
    Date of Patent: October 6, 1998
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Wan Joo Kim, Tae Ho Park, Moon Hwan Kim, Jewn Giew Park, Bong Jin Kim
  • Patent number: 5728693
    Abstract: Arthropodicidal compounds, compositions and use of compounds having the formula ##STR1##
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: March 17, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas Martin Stevenson
  • Patent number: 5602126
    Abstract: Substituted anilides of formula (I), wherein Q is one of (Q-1), (Q-2) and (Q-3), and R.sup.1 to R.sup.5, Y, Z and Z.sup.1 are as defined in the text, arthropodicidal compositions containing such compounds; and a method for controlling arthropods by use of such compounds.
    Type: Grant
    Filed: November 22, 1995
    Date of Patent: February 11, 1997
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: William E. Barnette, Charles R. Harrison, George P. Lahm, David W. Piotrowski, Keith D. Wing
  • Patent number: 5536719
    Abstract: A compound of formula (I): ##STR1## in the form of its S enantiomer, its addition salts with a pharmaceutically acceptable acid or base and medicinal product containing the same are useful for the treatment or prevention of pathologies associated with dysfunction of glutamatergic neurotransmission.
    Type: Grant
    Filed: July 11, 1995
    Date of Patent: July 16, 1996
    Assignee: Adir et Compagnie
    Inventors: Alex Cordi, Michael Spedding, Bernard Serkiz, Jean Lepagnol, Patrice Desos, Philippe Morain
  • Patent number: 5403837
    Abstract: This invention relates to compounds of formula (I): ##STR1## wherein R is a polyfluoroalkoxy, polyfluoroalkyl, alkoxy or alkyl radical and R.sub.1 is a hydrogen atom or an alkyl radical; salts thereof; the preparation thereof; and drugs containing same.
    Type: Grant
    Filed: December 7, 1993
    Date of Patent: April 4, 1995
    Assignee: Rhone Poulenc Rorer S.A.
    Inventors: Francois Audiau, Patrick Jimonet, Serge Mignani
  • Patent number: 5356862
    Abstract: The invention relates to herbicidal sulfonylurea compounds, agriculturally suitable compositions thereof and a method for their use as general or selective preemergent or postemergent herbicides or plant growth regulants.
    Type: Grant
    Filed: July 22, 1992
    Date of Patent: October 18, 1994
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: William T. Zimmerman
  • Patent number: 5210209
    Abstract: The invention provides a method for the production of a pyrazolo(1,5-a)benzimidazole of the general formula (A): ##STR1## wherein R is a substituted or unsubstituted alkyl or aryl group, andR.sup.1 -R.sup.4 =R, H, halogen, OR, COOR, CONHR, SO.sub.2, NO.sub.2 NHR, NR.sub.2, or CN, andX is hydogen or a reactive group releasable on coupling with an oxidized color developer, wherein the invention provides reacting a 2-amino or 2-mercapto substituted benzimidazole to form a triazepinone or a thiadiazino derivative respectively, ring contracting said triazepinone or thiadiazino derivative to give the corresponding 2-methylpyrazolobenzimidazole product, and subsequently removing the substituents at the -3 or -4 positions to provide a compound of the general formula (1).
    Type: Grant
    Filed: June 3, 1991
    Date of Patent: May 11, 1993
    Assignee: Eastman Kodak Company
    Inventor: Michael W. Crawley
  • Patent number: 5166348
    Abstract: Bornyl and isobornyl esters of carboxylic acids of condensed tetrahydroquinoxalines having the general formula ##STR1## where R.sup.1 is CH.sub.3 or C.sub.2 H.sub.5 ##STR2## where R.sup.2 is ##STR3## The proposed compounds are active against viruses and can therefore be used in medicine.
    Type: Grant
    Filed: August 5, 1991
    Date of Patent: November 24, 1992
    Assignees: Uralsky politekhnichesky institut, Institut organicheskogo sinteza AN Latvii
    Inventors: Oleg N. Chupakhin, Valery N. Charushin, Galina M. Petrova, Mikhail G. Ponizovsky, Vasily G. Baklykov, Gunar Y. Dubur, Egils A. Biseniex, Yan R. Uldrikis, Oleg U. Kiselev, Vera I. Ilienko, Vitaly G. Platonov, Valentina M. Guseva
  • Patent number: 5162317
    Abstract: A pyridinium salt useful as an antiulcer agent, defined by formula (I) is disclosed. It includes a sulphenamide compound and a pyridinium compound. J is benzimidazole, K is --S-- or --SSR-- and Z is hydroxy or alkoxy.
    Type: Grant
    Filed: December 5, 1989
    Date of Patent: November 10, 1992
    Assignee: Esai Co., Ltd.
    Inventors: Shigeru Souda, Shuhei Miyazawa, Norihiro Ueda, Katsuya Tagami, Seiichiro Nomoto, Makoto Okita, Naoyuki Shimomura, Toshihiko Kaneko, Masatoshi Fujimoto, Manabu Murakami, Kiyoshi Oketani, Hideaki Fujisaki, Hisashi Shibata, Tsuneo Wakabayashi
  • Patent number: 5130313
    Abstract: This invention relates to compounds of formula: ##STR1## in which R.sub.1 denotesa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by an optionally substituted phenyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical,a 1-piperazinyl radical substituted in the 4-position by an optionally substituted phenyl, 1,2-benzisothiazol-3-yl, 1,2-benzisoxazol-3-yl or 2-pyridyl radical,a piperidino radical substituted in the 4-position by an optionally substituted phenyl, bis(4-fluorophenyl)methylene, 4-fluorobenzoyl, optionally substituted 2-oxo-1-benzimidazolinyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical, by two phenyl radicals or a hydroxyl radical and an optionally substituted phenyl radicalR.sub.2 denotes a radical SO.sub.2 R.sub.4 in which R.sub.4 denotes an alkyl or phenyl radical,R.sub.3 denotes a phenyl or naphthyl radical,or else R.sub.2 and R.sub.
    Type: Grant
    Filed: December 13, 1990
    Date of Patent: July 14, 1992
    Assignee: Rhone-Poulenc Sante
    Inventors: Marie-Therese Comte, Claude Gueremy, Jean-Luc Malleron, Jean-Francois Peyronel, Alain Truchon
  • Patent number: 4943570
    Abstract: Benzimidazole-2-sulfonamide and imidazopyridine-2-sulfonamide derivatives corresponding to the general formula: ##STR1## and their pharmaceutically acceptable salts in which: Z.sup.1 to Z.sup.4 represent a nitrogen atom or a substituted or unsubstituted carbon atom;R.sup.3 represents a hydrogen atom or an alkyl, aryl, heteroaryl, alkylaryl, hydroxyalkyl, alkylheteroaryl, mono-, bi- or tri-cycloalkyl, alkylamino, N-alkyl-alkylamino, alkylcarboxyalkyl, acyl, alkylthioalkyl, alkylsulfinylalkyl or alkylsulfonylalkyl, alkylthioaryl, alkylsulfinylaryl or alkylsulfonylaryl, alkylthioheteroaryl, alkylsulfinylheteroaryl or alkylsulfonylheteroaryl, alkylthioalkylaryl, alkylsulfinylalkylaryl or alkylsulfonylalkylaryl, alkylthioalkylheteroaryl, alkylsulfinylalkylheteroaryl or alkylsulfonylalkylheteroaryl, halogenoalkyl, cyanoalkyl, N-alkylaryl-alkylamino, N-alkyl-N-alkylaryl-alkylamino, N,N-dialkyl-alkylamino, alkylpiperazinyl, alkylpiperidinyl or alkylmorpholinyl radical;X represents --(CHR.sup.8).sub.n --(CHR.sup.9).
    Type: Grant
    Filed: April 28, 1989
    Date of Patent: July 24, 1990
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Jordi F. Constansa, Juan P. Corominas, Augusto C. Pinol