The Additional Cyclo Has At Least Six Ring Members Patents (Class 540/559)
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20140200209
    Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.
    Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
  • Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • Publication number: 20140163014
    Abstract: The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Inventors: William H. Bunnelle, Marc Scanio, Jason T. Brewer, Ying Wang, Irini Akritopoulou-Zanze
  • Publication number: 20140121367
    Abstract: The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.
    Type: Application
    Filed: April 9, 2012
    Publication date: May 1, 2014
    Inventors: Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
  • Patent number: 8673896
    Abstract: The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: March 18, 2014
    Assignee: AbbVie Inc.
    Inventors: William H. Bunnelle, Marc Scanio, Jason T. Brewer, Ying Wang, Irini Akritopoulou-Zanze
  • Patent number: 8546377
    Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Grant
    Filed: October 21, 2010
    Date of Patent: October 1, 2013
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
  • Publication number: 20120253036
    Abstract: An agent for treating fibromyalgia containing a 5-HT2C receptor agonist as an active ingredient
    Type: Application
    Filed: December 10, 2010
    Publication date: October 4, 2012
    Inventors: Yukinori Nagakura, Mina Tsukamoto, Tomonari Watabiki
  • Publication number: 20120184537
    Abstract: The invention relates to a novel class of [1,4]-benzodiazepine derivatives, processes for their preparation, intermediates usable in these processes, and pharmaceutical compositions containing the compounds. Other aspects of the invention are directed to the use of said [1,4]-benzodiazepine derivatives in therapy based on the capability of said compounds to interfere with the binding of the peptide hormone, vasopressin, to its receptors. In particular as vasopressin V2 receptor antagonists and therefore useful for treating involving increased vascular resistance, cardiac insufficiency, and water retention.
    Type: Application
    Filed: September 23, 2010
    Publication date: July 19, 2012
    Inventors: Ann Meulemans, Karel Lavrijsen, Marina Cools, Erik Keller, Igor Alexnadrovich Mezine, Leen Thielemans, Maarten VAn Geffen
  • Publication number: 20120184734
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: June 14, 2010
    Publication date: July 19, 2012
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20120172352
    Abstract: The present invention is related to pyrazoline dione derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: September 27, 2010
    Publication date: July 5, 2012
    Applicant: GENKYOTEX SA
    Inventors: Patrick Page, Francesca Gaggini, Benoît Laleu
  • Publication number: 20110288069
    Abstract: The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Application
    Filed: April 22, 2011
    Publication date: November 24, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: William H. Bunnelle, Marc Scanio, Jason T. Brewer, Ying Wang, Irini Akritopoulou-Zanze
  • Publication number: 20110207721
    Abstract: The present invention provides kinase inhibitors of Formula I.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 25, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Thomas Albert Engler, Timothy Paul Burkholder, Joshua Ryan Clayton, Clive Gideon Diefenbacher, Kelly Wayne Furness, James Robert Henry, Yihong Li, Sushant Malhotra, Angela Lynn Marquart, Johnathan Alexander McLean, David Mendel, Jon Kevin Reel, Brian Raymond Berridge, Charles Edward Ruegg, John Morris Sullivan
  • Publication number: 20100273767
    Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2 -a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7 -octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2 -a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Application
    Filed: April 22, 2010
    Publication date: October 28, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Bhadra Shelat, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
  • Publication number: 20090318421
    Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
    Type: Application
    Filed: April 28, 2006
    Publication date: December 24, 2009
    Inventors: Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • Publication number: 20090227565
    Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturat
    Type: Application
    Filed: November 10, 2008
    Publication date: September 10, 2009
    Applicant: WYETH
    Inventors: Amedeo A. FAILLI, John P. DUSZA, Thomas J. CAGGIANO, Jay S. SHUMSKY, Kevin A. MEMOLI, Eugene J. TRYBULSKI
  • Publication number: 20090143356
    Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.
    Type: Application
    Filed: October 26, 2006
    Publication date: June 4, 2009
    Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • Publication number: 20090105228
    Abstract: Compounds of formula I: (where variables R2, R7, D, W, X, Y and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: July 25, 2006
    Publication date: April 23, 2009
    Inventor: Theresa M. Williams
  • Publication number: 20080167289
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: February 13, 2007
    Publication date: July 10, 2008
    Inventors: David Kay, Ronald Knegtel, Jean-Damien Charrier, Heather Twin
  • Patent number: 7329653
    Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.
    Type: Grant
    Filed: April 11, 2006
    Date of Patent: February 12, 2008
    Assignee: Wyeth
    Inventors: Amedeo A. Failli, Jay S. Shumsky, Thomas J. Caggiano, John P. Dusza, Kevin A. Memoli
  • Patent number: 7317005
    Abstract: The invention is directed to tricyclic benzodiazepines useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising tricyclic benzodiazepines of the present invention and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.
    Type: Grant
    Filed: February 10, 2004
    Date of Patent: January 8, 2008
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: William J. Hoekstra, Alexey B. Dyatkin, Bruce E. Maryanoff, Jay M. Matthews
  • Patent number: 7223752
    Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1–C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1–C6) lower alkyl, halogen or (C1–C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1–C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1–C6) lower alkoxy, or (C1–C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1–C6) lower alkyl], —CON[(C1–C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturat
    Type: Grant
    Filed: November 4, 2004
    Date of Patent: May 29, 2007
    Assignee: Wyeth
    Inventors: Amedeo Arturo Failli, John P. Dusza, Thomas Joseph Caggiano, Jay Scott Shumsky, Kevin A. Memoli, Eugene J. Trybulski
  • Patent number: 7005430
    Abstract: A condensed purine derivative represented by Formula (I): wherein X—Y-Z represents R1N—C?O or N?C—W, R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, V1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, V2 represents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when V1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X—Y-Z represents R1aN—C?O and R2 represents a substituted lower
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: February 28, 2006
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Kimihisa Ueno, Akira Ogawa, Yoshihisa Ohta, Yuji Nomoto, Kotaro Takasaki, Hideaki Kusaka, Hiroshi Yano, Chiharu Nakagawa, Satoshi Nakanishi
  • Patent number: 6953791
    Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: October 11, 2005
    Assignee: Pfizer, Inc.
    Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
  • Patent number: 6943171
    Abstract: A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases:
    Type: Grant
    Filed: November 7, 2002
    Date of Patent: September 13, 2005
    Assignee: Schering Corporation
    Inventors: Theodros Asberom, John W. Clader, Yueqing Hu, Dmitri A. Pissarnitski, Andrew W. Stamford, Ruo Xu
  • Patent number: 6936604
    Abstract: The invention is directed to bridged bicyclic amino acid-derived [1,4]benzodiazepine compounds, intermediates and pharmaceutical compositions thereof useful as vasopressin receptor antagonists and methods for treating vasopressin mediated disorders.
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: August 30, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Alexey B. Dyatkin, William J. Hoekstra, Bruce E. Maryanoff
  • Publication number: 20040242866
    Abstract: The invention is directed to tricyclic benzodiazepines useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising tricyclic benzodiazepines of the present invention and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.
    Type: Application
    Filed: February 10, 2004
    Publication date: December 2, 2004
    Inventors: William J. Hoekstra, Alexey B. Dyatkin, Bruce E. Maryanoff, Jay M. Matthews
  • Patent number: 6713475
    Abstract: The invention is directed to tricyclic benzodiazepines useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising tricyclic benzodiazepines of the present invention and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.
    Type: Grant
    Filed: July 24, 2001
    Date of Patent: March 30, 2004
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: William J. Hoekstra, Alexey B. Dyatkin, Bruce E. Maryanoff, Jay M. Matthews
  • Publication number: 20030176413
    Abstract: A compound having the formula (Ia) or (b), salt or solvate thereof, with the variables as defined herein, which can inhibit selectively phosphodiesterase V and can be useful for treating sexual dysfunction and other physiological disorders, symptoms and diseases: 1
    Type: Application
    Filed: November 7, 2002
    Publication date: September 18, 2003
    Applicant: Schering Corporation
    Inventors: Theodros Asberom, John W. Clader, Yuequing Hu, Dmitri A. Pissarnitski, Andrew W. Stamford, Ruo Xu
  • Publication number: 20030176698
    Abstract: A condensed purine derivative represented by Formula (I): 1
    Type: Application
    Filed: October 22, 2002
    Publication date: September 18, 2003
    Inventors: Kimihisa Ueno, Akira Ogawa, Yoshihisa Ohta, Yuji Nomoto, Kotaro Takasaki, Hideaki Kusaka, Hiroshi Yano, Chiharu Nakagawa, Satoshi Nakanishi
  • Patent number: 6608193
    Abstract: Methods of preparing amino-substituted-tetrahydroisoquinoline ring compounds include the steps of providing a support-bound amino-substituted-tetrahydroisoquinoline compound; forming an intermediate by reacting the support-bound amino-substituted-tetrahydroisoquinoline compound with a reagent; and cyclizatively cleaving the support-bound amino-substituted-tetrahydroisoquinoline compound to form the amino-substituted-tetrahydroisoquinoline ring compound.
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: August 19, 2003
    Assignee: The Procter & Gamble Company
    Inventors: Song Liu, William Martin Rennells
  • Publication number: 20030135043
    Abstract: The present invention is directed to methods for the preparation of piperazine ring-containing compounds, particularly mirtazapine. According to the present invention, the mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine is made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with a base where the base is present in a ratio of up to about 12 moles of the base per one mole of 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine. The mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine may be made by hydrolyzing 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine with potassium hydroxide at a temperature of at least about 130° C.
    Type: Application
    Filed: February 20, 2003
    Publication date: July 17, 2003
    Inventors: Claude Singer, Anita Liberman, Nina Finkelstein
  • Publication number: 20030130504
    Abstract: Low-hygroscopic anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C. under atmospheric pressure for 500 hours; a process for preparing anhydrous mirtazapine crystals having a hygroscopic degree of not more than 0.6% by weight when the crystals are stored in the air having a relative humidity of 75% at 25° C.
    Type: Application
    Filed: January 7, 2003
    Publication date: July 10, 2003
    Applicant: Sumika Fine Chemicals Co. , Ltd.
    Inventors: Eiichi Iishi, Yoshiyuki Imamiya
  • Publication number: 20030119822
    Abstract: The invention is directed to bridged bicyclic amino acid-derived [1,4]benzodiazepine compounds, intermediates and pharmaceutical compositions thereof useful as vasopressin receptor antagonists and methods for treating vasopressin mediated disorders.
    Type: Application
    Filed: October 11, 2002
    Publication date: June 26, 2003
    Inventors: Alexey B. Dyatkin, William J. Hoekstra, Bruce E. Maryanoff
  • Publication number: 20030120068
    Abstract: The present invention is directed to methods for the preparation of piperazine ring-containing compounds, particularly mirtazapine. According to the present invention, the mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine is made by hydrolyzing 1-(3-cyanopyridyl-2)methyl-2-phenyl-piperazine with a base where the base is present in a ratio of up to about 12 moles of the base per one mole of 1-(3-cyanopyridyl-2)-4-methyl-2-phenyl-piperazine. The mirtazapine intermediate 1-(3-carboxypyridyl-2)-4-methyl-2-phenyl-piperazine may be made by hydrolyzing 1-(3-cyanopyridyl-2)4-methyl-2-phenyl-piperazine with potassium hydroxide at a temperature of at least about 130° C. The method of the present invention also includes reacting 2-amine-3-hydroxymethyl pyridine with N-methyl-1-phenyl-2,2′-iminodiethyl chloride to form 1-(3-hydroxymethylpyridyl-2)-4-methyl-2-phenyl piperazine, and adding sulfuric acid to the 1-(3-hydroxymethylpyridyl-2)-phenyl-4-methylpiperazine to form mirtazapine.
    Type: Application
    Filed: January 23, 2003
    Publication date: June 26, 2003
    Inventors: Claude Singer, Anita Liberman, Nina Finkelstein
  • Patent number: 6569851
    Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: May 27, 2003
    Assignees: Elan Pharmaceutials, Inc., Eli Lilly & Company
    Inventors: Richard C. Thompson, Stephen Wilkie, Douglas R. Stack, Eldon E. VanMeter, Qing Shi, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Publication number: 20020103373
    Abstract: The invention is directed to tricyclic benzodiazepines useful as vasopressin receptor antagonists for treating conditions involving increased vascular resistance and cardiac insufficiency. Pharmaceutical compositions comprising tricyclic benzodiazepines of the present invention and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis, or water retention are also disclosed.
    Type: Application
    Filed: July 24, 2001
    Publication date: August 1, 2002
    Inventors: William J. Hoekstra, Alexey B. Dyatkin, Bruce E. Maryanoff, Jay M. Matthews
  • Patent number: 6306847
    Abstract: The present invention provides condensed purine derivatives or pharmacologically acceptable salts thereof exhibiting adenosine A3 acceptor antagonising activity, and having an antiasthmatic action, a bronchodilator action, an antiantiitching action, etc., and represented by the following formula (I): (wherein R1 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R2 represents hydrogen, lower alkyl, alicyclic alkyl, substituted or unsubstituted aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted aromatic heterocyclic group; R3 represents hydrogen, lower alkyl, or substituted or unsubstituted aralkyl; X1 and X2 are the same or different and each represents hydrogen, lower alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted aryl; and n represents an integer of 0 to 3).
    Type: Grant
    Filed: June 5, 1998
    Date of Patent: October 23, 2001
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hiroshi Tsumuki, Mayumi Saki, Hiromi Nonaka, Michio Ichimura, Junichi Shimada, Fumio Suzuki, Shunji Ichikawa, Nobuo Kosaka
  • Patent number: 6140322
    Abstract: There are provided novel compounds of formula (I) ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the specification and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy.
    Type: Grant
    Filed: January 20, 1999
    Date of Patent: October 31, 2000
    Assignee: Astra Aktiebolag
    Inventors: James MacDonald, James Matz, William Shakespeare
  • Patent number: 5985871
    Abstract: Compounds having a certain benzoxazine ring system and their precursors are disclosed which are useful for enhancing synaptic responses mediated by AMPA receptors. Also disclosed are methods for preparing such compounds, and methods for their use in treating subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.
    Type: Grant
    Filed: December 24, 1997
    Date of Patent: November 16, 1999
    Assignee: Cortex Pharmaceuticals, Inc.
    Inventors: Gary A. Rogers, Christopher Marrs
  • Patent number: 5977101
    Abstract: Vitronectin receptor antagonists having the formula: ##STR1## which are useful for the treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporsis.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: November 2, 1999
    Assignee: SmithKline Beecham Corporation
    Inventors: Fadia El-Fehail Ali, William Bondinell, William Francis Huffman, M. Amparo Lago, Richard McCulloch Keenan, Chet Kwon, William Henry Miller, Thomas Nguyen, Dennis T. Takata
  • Patent number: 5945423
    Type: Grant
    Filed: January 14, 1998
    Date of Patent: August 31, 1999
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: James Francis Bereznak, Zen-Yu Chang, Thomas Paul Selby, Charlene Gross Sternberg
  • 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: 5834464
    Abstract: Imidazolinobenzodiazepines are cholecystokinin B (CCK-B) antagonists useful as anxiolytic agents.
    Type: Grant
    Filed: May 6, 1996
    Date of Patent: November 10, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark G. Bock, Robert M. DiPardo, Roger M. Freidinger
  • Patent number: 5786352
    Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C<, --CO--N< or --CS--N< as the partial structure --X . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.
    Type: Grant
    Filed: March 25, 1996
    Date of Patent: July 28, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura
  • Patent number: 5679672
    Abstract: Compounds of structures (I) and (Ia) are Class III antiarrhythmic agents ##STR1##
    Type: Grant
    Filed: May 14, 1996
    Date of Patent: October 21, 1997
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Nigel Liverton, David C. Remy, Harold G. Selnick
  • Patent number: 5461048
    Abstract: The invention relates to novel cholecystokinin antagonists of the formula ##STR1## wherein R.sup.1 is aryl or substituted aryl, and a pharmaceutically acceptable salt thereof useful as cholecystokinin antagonists.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: October 24, 1995
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshinari Sato, Teruaki Matuo, Takatomo Ogahara
  • Patent number: 5268372
    Abstract: Novel 2,5-benzodiazocines of formulas II and IV, pharmaceutical compositions containing them, processes for preparing them and methods of treating cardiac arrhythmias in mammals utilizing them.
    Type: Grant
    Filed: February 17, 1993
    Date of Patent: December 7, 1993
    Assignee: Sterling Winthrop Inc.
    Inventor: Robert E. Johnson
  • Patent number: 5237060
    Abstract: The invention relates to a process for the preparation of highly antibacterially active enantiomerically pure 1,8-bridged 4-quinolone-3-carboxylic acids and derivatives of the formula (I) ##STR1## in which 1) a compound of the formula ##STR2## is reacted with a compound of the formula ##STR3## to form a compound of the formula ##STR4## followed by cyclization to form a compound of the formula ##STR5## and further cyclization to form a compound of the formula ##STR6## an finally reaction of the cyclized product with amines of the formula ##STR7##
    Type: Grant
    Filed: February 23, 1989
    Date of Patent: August 17, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl Metzger
  • Patent number: 5104868
    Abstract: This invention relates to novel tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and certain esters and cation salts thereof. The compounds of this invention are substituted at the 7-position by vinyl, W--CH.dbd.CH--, CH.sub.3 C.tbd.C--, W--CH.sub.2 C.tbd.C-- or ##STR1## where W is selected from certain substituted alkyl groups. This invention also relates to antibacterial compositions containing the compounds and methods of using the compounds to treat bacterial disease.
    Type: Grant
    Filed: August 29, 1990
    Date of Patent: April 14, 1992
    Assignee: Pfizer Inc.
    Inventor: Paul R. McGuirk