The Additional Cyclo Has At Least Six Ring Members Patents (Class 540/559)
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Publication number: 20150065485Abstract: 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: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Publication number: 20140200209Abstract: 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: ApplicationFiled: March 14, 2014Publication date: July 17, 2014Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
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Patent number: 8772301Abstract: 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: GrantFiled: December 17, 2010Date of Patent: July 8, 2014Assignee: Sunovion Pharmaceuticals, Inc.Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
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Publication number: 20140163014Abstract: 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: ApplicationFiled: February 12, 2014Publication date: June 12, 2014Inventors: William H. Bunnelle, Marc Scanio, Jason T. Brewer, Ying Wang, Irini Akritopoulou-Zanze
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Publication number: 20140121367Abstract: 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: ApplicationFiled: April 9, 2012Publication date: May 1, 2014Inventors: Sundeep Dugar, Dinesh Mahajan, Frank Peter Hollinger
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Patent number: 8673896Abstract: 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: GrantFiled: April 22, 2011Date of Patent: March 18, 2014Assignee: AbbVie Inc.Inventors: William H. Bunnelle, Marc Scanio, Jason T. Brewer, Ying Wang, Irini Akritopoulou-Zanze
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Patent number: 8546377Abstract: 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: GrantFiled: October 21, 2010Date of Patent: October 1, 2013Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KGInventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
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Publication number: 20120253036Abstract: An agent for treating fibromyalgia containing a 5-HT2C receptor agonist as an active ingredientType: ApplicationFiled: December 10, 2010Publication date: October 4, 2012Inventors: Yukinori Nagakura, Mina Tsukamoto, Tomonari Watabiki
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Publication number: 20120184537Abstract: 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: ApplicationFiled: September 23, 2010Publication date: July 19, 2012Inventors: Ann Meulemans, Karel Lavrijsen, Marina Cools, Erik Keller, Igor Alexnadrovich Mezine, Leen Thielemans, Maarten VAn Geffen
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Publication number: 20120184734Abstract: 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: ApplicationFiled: June 14, 2010Publication date: July 19, 2012Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
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Publication number: 20120172352Abstract: 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: ApplicationFiled: September 27, 2010Publication date: July 5, 2012Applicant: GENKYOTEX SAInventors: Patrick Page, Francesca Gaggini, Benoît Laleu
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Publication number: 20110288069Abstract: 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: ApplicationFiled: April 22, 2011Publication date: November 24, 2011Applicant: ABBOTT LABORATORIESInventors: William H. Bunnelle, Marc Scanio, Jason T. Brewer, Ying Wang, Irini Akritopoulou-Zanze
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Publication number: 20110207721Abstract: The present invention provides kinase inhibitors of Formula I.Type: ApplicationFiled: May 4, 2011Publication date: August 25, 2011Applicant: ELI LILLY AND COMPANYInventors: 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
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Publication number: 20100273767Abstract: 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: ApplicationFiled: April 22, 2010Publication date: October 28, 2010Applicant: ABBOTT LABORATORIESInventors: Ying Wang, Jason T. Brewer, Irini Akritopoulou-Zanze, Stevan W. Djuric, Bhadra Shelat, Frauke Pohlki, Wilfried Braje, Ana-Lucia Relo
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Publication number: 20090318421Abstract: 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: ApplicationFiled: April 28, 2006Publication date: December 24, 2009Inventors: Brian Alvin Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Publication number: 20090227565Abstract: 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 (unsaturatType: ApplicationFiled: November 10, 2008Publication date: September 10, 2009Applicant: WYETHInventors: Amedeo A. FAILLI, John P. DUSZA, Thomas J. CAGGIANO, Jay S. SHUMSKY, Kevin A. MEMOLI, Eugene J. TRYBULSKI
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Publication number: 20090143356Abstract: 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: ApplicationFiled: October 26, 2006Publication date: June 4, 2009Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
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Publication number: 20090105228Abstract: 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: ApplicationFiled: July 25, 2006Publication date: April 23, 2009Inventor: Theresa M. Williams
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Publication number: 20080167289Abstract: 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: ApplicationFiled: February 13, 2007Publication date: July 10, 2008Inventors: David Kay, Ronald Knegtel, Jean-Damien Charrier, Heather Twin
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Patent number: 7329653Abstract: 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: GrantFiled: April 11, 2006Date of Patent: February 12, 2008Assignee: WyethInventors: Amedeo A. Failli, Jay S. Shumsky, Thomas J. Caggiano, John P. Dusza, Kevin A. Memoli
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Patent number: 7317005Abstract: 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: GrantFiled: February 10, 2004Date of Patent: January 8, 2008Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: William J. Hoekstra, Alexey B. Dyatkin, Bruce E. Maryanoff, Jay M. Matthews
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Patent number: 7223752Abstract: 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 (unsaturatType: GrantFiled: November 4, 2004Date of Patent: May 29, 2007Assignee: WyethInventors: Amedeo Arturo Failli, John P. Dusza, Thomas Joseph Caggiano, Jay Scott Shumsky, Kevin A. Memoli, Eugene J. Trybulski
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Patent number: 7005430Abstract: 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 lowerType: GrantFiled: December 22, 2000Date of Patent: February 28, 2006Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Kimihisa Ueno, Akira Ogawa, Yoshihisa Ohta, Yuji Nomoto, Kotaro Takasaki, Hideaki Kusaka, Hiroshi Yano, Chiharu Nakagawa, Satoshi Nakanishi
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Patent number: 6953791Abstract: 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: GrantFiled: February 21, 2003Date of Patent: October 11, 2005Assignee: Pfizer, Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Patent number: 6943171Abstract: 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: GrantFiled: November 7, 2002Date of Patent: September 13, 2005Assignee: Schering CorporationInventors: Theodros Asberom, John W. Clader, Yueqing Hu, Dmitri A. Pissarnitski, Andrew W. Stamford, Ruo Xu
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Patent number: 6936604Abstract: 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: GrantFiled: October 11, 2002Date of Patent: August 30, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Alexey B. Dyatkin, William J. Hoekstra, Bruce E. Maryanoff
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Publication number: 20040242866Abstract: 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: ApplicationFiled: February 10, 2004Publication date: December 2, 2004Inventors: William J. Hoekstra, Alexey B. Dyatkin, Bruce E. Maryanoff, Jay M. Matthews
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Patent number: 6713475Abstract: 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: GrantFiled: July 24, 2001Date of Patent: March 30, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: William J. Hoekstra, Alexey B. Dyatkin, Bruce E. Maryanoff, Jay M. Matthews
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Publication number: 20030176413Abstract: 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: 1Type: ApplicationFiled: November 7, 2002Publication date: September 18, 2003Applicant: Schering CorporationInventors: Theodros Asberom, John W. Clader, Yuequing Hu, Dmitri A. Pissarnitski, Andrew W. Stamford, Ruo Xu
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Publication number: 20030176698Abstract: A condensed purine derivative represented by Formula (I): 1Type: ApplicationFiled: October 22, 2002Publication date: September 18, 2003Inventors: Kimihisa Ueno, Akira Ogawa, Yoshihisa Ohta, Yuji Nomoto, Kotaro Takasaki, Hideaki Kusaka, Hiroshi Yano, Chiharu Nakagawa, Satoshi Nakanishi
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Patent number: 6608193Abstract: 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: GrantFiled: December 21, 2001Date of Patent: August 19, 2003Assignee: The Procter & Gamble CompanyInventors: Song Liu, William Martin Rennells
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Publication number: 20030135043Abstract: 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: ApplicationFiled: February 20, 2003Publication date: July 17, 2003Inventors: Claude Singer, Anita Liberman, Nina Finkelstein
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Publication number: 20030130504Abstract: 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: ApplicationFiled: January 7, 2003Publication date: July 10, 2003Applicant: Sumika Fine Chemicals Co. , Ltd.Inventors: Eiichi Iishi, Yoshiyuki Imamiya
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Publication number: 20030119822Abstract: 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: ApplicationFiled: October 11, 2002Publication date: June 26, 2003Inventors: Alexey B. Dyatkin, William J. Hoekstra, Bruce E. Maryanoff
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Publication number: 20030120068Abstract: 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: ApplicationFiled: January 23, 2003Publication date: June 26, 2003Inventors: Claude Singer, Anita Liberman, Nina Finkelstein
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Patent number: 6569851Abstract: 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: GrantFiled: June 22, 1999Date of Patent: May 27, 2003Assignees: Elan Pharmaceutials, Inc., Eli Lilly & CompanyInventors: 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
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Publication number: 20020103373Abstract: 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: ApplicationFiled: July 24, 2001Publication date: August 1, 2002Inventors: William J. Hoekstra, Alexey B. Dyatkin, Bruce E. Maryanoff, Jay M. Matthews
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Patent number: 6306847Abstract: 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: GrantFiled: June 5, 1998Date of Patent: October 23, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hiroshi Tsumuki, Mayumi Saki, Hiromi Nonaka, Michio Ichimura, Junichi Shimada, Fumio Suzuki, Shunji Ichikawa, Nobuo Kosaka
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Patent number: 6140322Abstract: 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: GrantFiled: January 20, 1999Date of Patent: October 31, 2000Assignee: Astra AktiebolagInventors: James MacDonald, James Matz, William Shakespeare
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Patent number: 5985871Abstract: 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: GrantFiled: December 24, 1997Date of Patent: November 16, 1999Assignee: Cortex Pharmaceuticals, Inc.Inventors: Gary A. Rogers, Christopher Marrs
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Patent number: 5977101Abstract: 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: GrantFiled: December 20, 1996Date of Patent: November 2, 1999Assignee: SmithKline Beecham CorporationInventors: 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
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Patent number: 5945423Type: GrantFiled: January 14, 1998Date of Patent: August 31, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: James Francis Bereznak, Zen-Yu Chang, Thomas Paul Selby, Charlene Gross Sternberg
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Patent number: 5846969Abstract: 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: GrantFiled: June 11, 1997Date of Patent: December 8, 1998Assignee: 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
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Patent number: 5834464Abstract: Imidazolinobenzodiazepines are cholecystokinin B (CCK-B) antagonists useful as anxiolytic agents.Type: GrantFiled: May 6, 1996Date of Patent: November 10, 1998Assignee: Merck & Co., Inc.Inventors: Mark G. Bock, Robert M. DiPardo, Roger M. Freidinger
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Patent number: 5786352Abstract: 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: GrantFiled: March 25, 1996Date of Patent: July 28, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura
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Patent number: 5679672Abstract: Compounds of structures (I) and (Ia) are Class III antiarrhythmic agents ##STR1##Type: GrantFiled: May 14, 1996Date of Patent: October 21, 1997Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Nigel Liverton, David C. Remy, Harold G. Selnick
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Patent number: 5461048Abstract: 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: GrantFiled: November 30, 1994Date of Patent: October 24, 1995Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshinari Sato, Teruaki Matuo, Takatomo Ogahara
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Patent number: 5268372Abstract: 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: GrantFiled: February 17, 1993Date of Patent: December 7, 1993Assignee: Sterling Winthrop Inc.Inventor: Robert E. Johnson
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Patent number: 5237060Abstract: 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: GrantFiled: February 23, 1989Date of Patent: August 17, 1993Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl Metzger
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Patent number: 5104868Abstract: 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: GrantFiled: August 29, 1990Date of Patent: April 14, 1992Assignee: Pfizer Inc.Inventor: Paul R. McGuirk