Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 540/521)
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Publication number: 20080214522Abstract: Compounds of the formula (I): wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing them and their use in medicine are disclosed.Type: ApplicationFiled: December 19, 2007Publication date: September 4, 2008Applicant: Istituto di Ricerche di Biologia Molecolare P. Angeletti SpAInventors: Ian Stansfield, Uwe Koch, Joerg Habermann, Frank Narjes
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Patent number: 7419975Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula IType: GrantFiled: April 6, 2005Date of Patent: September 2, 2008Assignee: Novartis AGInventors: Mark Gabriel Palermo, Sushil Kumar Sharma, Christopher Straub, Run-Ming Wang, Leigh Scott Zawel, Yanlin Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
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Patent number: 7384931Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptorsType: GrantFiled: May 3, 2006Date of Patent: June 10, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang
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Patent number: 7384930Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: October 11, 2005Date of Patent: June 10, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Stephen E. Mercer, Haiquan Fang
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Patent number: 7307162Abstract: The present invention provides for an efficient method of effecting the resolution of a narwedine amide, and the synthesis of galantamine.Type: GrantFiled: September 27, 2004Date of Patent: December 11, 2007Assignee: ScinoPharm Taiwan, Ltd.Inventors: George Schloemer, Tsung-Yu Hsiao
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Publication number: 20070259850Abstract: The invention encompasses constrained bicyclic and tricyclic CGRP-receptor antagonists, methods for identifying them, pharmaceutical compositions comprising them, and methods for their use in therapy for treatment of migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: ApplicationFiled: May 1, 2007Publication date: November 8, 2007Inventors: Stephen E. Mercer, Prasad V. Chaturvedula
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Patent number: 7229985Abstract: Disclosed are 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H), 10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine, which has been rendered amorphous and possesses improved absorption and dissoluvability, and a pharmaceutical composition comprising the same. Also disclosed are processes for producing 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H), 10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine, which has been rendered amorphous, and a pharmaceutical composition comprising the same.Type: GrantFiled: December 25, 2002Date of Patent: June 12, 2007Assignee: Meiji Seika Kaisha, Ltd.Inventors: Toyoaki Ishikura, Takayuki Ishizawa, Kenji Suemune, Mayumi Ishiwata, Chikako Udagawa
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Patent number: 7138408Abstract: Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.Type: GrantFiled: October 14, 2005Date of Patent: November 21, 2006Assignee: Agouron Pharmaceuticals, Inc.Inventors: Atsuo Kuki, Xinqiang Li, Michael Bruno Plewe, Hai Wang, Junhu Zhang
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Ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenylpropanoate], processes for its preparation and its use
Patent number: 7009047Abstract: The present invention relates to ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate], the preparation of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] from (2R)-2-bromo-3-phenylpropionic acid and ethylenediamine in 2-propanol, and the use of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] for the preparation of ACE/NEP inhibitors.Type: GrantFiled: March 17, 2003Date of Patent: March 7, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Javier Manero, Tobias Metzenthin, Rainer Gauler -
Patent number: 7002009Abstract: Disclosed are novel crystalline 2-(1-isopropoxycarbonyloxy-2-methylpropyl)-7,8-dimethoxy-4(5H),10-dioxo-2H-1,2,3-triazolo[4,5-c][1]benzazepine and a pharmaceutical composition comprising the same.Type: GrantFiled: December 25, 2002Date of Patent: February 21, 2006Assignee: Meiji Seika Kaisha, Ltd.Inventors: Shin-Ichi Kitahara, Hanae Furukawa, Toshihiro Yamaguchi, Sachiko Miyamoto, Yumiko Okada
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Patent number: 6958330Abstract: Disclosed are polycyclic ?-amino-?-caprolactams and related compounds which are useful as synthetic intermediates in the preparation of inhibitors of ?-amyloid peptide release and/or its synthesis.Type: GrantFiled: June 14, 2001Date of Patent: October 25, 2005Assignees: Elan Pharmaceuticals, Inc., Eli Lilly and CompanyInventors: James E. Audia, Thomas E. Mabry, Jeffrey A. Nissen, Stacey L. McDaniel, Warren J. Porter
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Patent number: 6916805Abstract: This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable compositions comprising the compounds, their salts or prodrugs, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: January 4, 2002Date of Patent: July 12, 2005Assignee: Warner-Lambert Company LLCInventors: Danette Andrea Dudley, Jeremy John Edmunds
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Publication number: 20040235820Abstract: The synthesis and biological activity of indoloazepines and acid amine salts thereof which are structurally related to naturally-occurring hymenialdisine is disclosed. Naturally-occurring hymenialdisine obtained from the sponge is a potent inhibitor of production of cytokines interleukin-2 (IL-2) and tumor necrosis factor-&agr; (TNF-&agr;). The chemically-synthesized indoloazepines of the invention also inhibit production of IL-2 and TNF-&agr;. The indoloazepines are useful for treating inflammatory diseases, particularly diseases associated with kinases NF-&kgr;B or GSK-3&bgr; activation or NF-&kgr;B activated gene expression products. The indoloazepines are useful for the treatment of cancer by the inhibition of kinases CHK1 and CHK2.Type: ApplicationFiled: April 28, 2004Publication date: November 25, 2004Applicant: Board of Trustees of Michigan State UniversityInventor: Jetze J. Tepe
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Patent number: 6693101Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.Type: GrantFiled: January 23, 2001Date of Patent: February 17, 2004Assignee: Merck & Co., Inc.Inventors: Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
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Patent number: 6664249Abstract: Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH2, O and N-alkyl, Z is either S or —CH═CH—, R1 and R2 are independently selected from H, F, Cl, Br and alkyl, R3 is selected from OH, O-alkyl and NR4R5, R4 and R5 are each independently H or alkyl, or together are —(CH2)q—, p is 0, 1, 2, 3 or 4, and q is 4 or 5, are new. They are agonists at the asopressin V2 receptor and are useful as antidiuretics and pro-coagulants.Type: GrantFiled: June 10, 2002Date of Patent: December 16, 2003Assignee: Ferring BVInventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin
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Patent number: 6632943Abstract: It is provided a method for preparing the pyrroloazepine derivatives, especially in optically active form useful as drugs, by low-priced and simple method and in industrial applicable scale, represented by the following formula (I): wherein Z represents optionally substituted phenyl group, which comprises; a process for the asymmetric reduction of ketone compound with metal hydride compound and alcohol compound in the presence of optically active cobalt complex catalyst, and a process for the purification of the resulting compound.Type: GrantFiled: August 10, 2001Date of Patent: October 14, 2003Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Akira Mizuno, Kazuto Sekiuchi, Takushi Nagata, Teruo Muraishi
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Patent number: 6610684Abstract: A new class of cyclin dependent kinase inhibitors that also have antiproliferative activity in human tumor cell line assays are described.Type: GrantFiled: December 14, 2000Date of Patent: August 26, 2003Assignees: The United States of America as represented by the Department of Health and Human Services, Centre National de la Recherche ScientifiqueInventors: Daniel W. Zaharevitz, Rick P. Gussio, Ravi K. Jalluri, Edward A. Sausville, Conrad Kunick, Laurent Meijer
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Patent number: 6602866Abstract: This invention discloses and claims a series of mercaptoacetylamide derivatives of formula I. Also disclosed and claimed are pharmaceutical compositions incorporating these compounds and processes for preparing said compounds.Type: GrantFiled: April 8, 2002Date of Patent: August 5, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Gary A. Flynn, Barbara A. Anderson, Manfred Gerken, Bernd Jablonka, Heinz-Werner Kleemann, Wolfgang Linz, Werner Seiz, Bernhard Seuring
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Patent number: 6559141Abstract: 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 comprising 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: July 27, 2001Date of Patent: May 6, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6544978Abstract: 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 comprising 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: July 27, 2001Date of Patent: April 8, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6541466Abstract: 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 comprising 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: July 27, 2001Date of Patent: April 1, 2003Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Eugene D. Thorsett, Michael A. Pleiss, Jeffrey S. Nissen, R. Jeffrey Neitz, Lee H. Latimer, Varghese John, Stephen Freedman, Thomas C. Britton, James A. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, James J. Droste, Steven S. Henry, Stacey L. McDaniel, William Leonard Scott, Russell D. Stucky, Warren J. Porter
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Patent number: 6528646Abstract: The synthesis of C11N5 marine sponge alkaloids (±)-hymenin (1), stevensine (2), hymenialdisine (3), and debromohymenialdisine (4) is described. These natural products are the primary family members of the sponge metabolites that contain a fused pyrrolo[2,3-c]lazepin-8-one ring system with either a 2-aminoimidazole (AI) or glycocyamidine appendage. The key steps in the synthesis centered around the generation of novel azafulvenium ions and their regioselective heterodimerization with AI in order to create the tricyclic core. A rarely used protodebromination/oxidation strategy was employed to selectively generate the desired a-bromo substitution pattern seen in hymenialdisine (3). In addition, the AI moiety was shown to be a useful precursor to the glycocyamidine unit found in 3 and 4, which suggests that AI derived natural products may be the biogenic forerunners to glycocyamidine metabolites.Type: GrantFiled: December 28, 2000Date of Patent: March 4, 2003Assignee: The Trustees of Columbia University in the City of New YorkInventors: David A. Horne, Kenichi Yakushijin
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Patent number: 6514964Abstract: The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as &agr;v&bgr;3, &agr;v&bgr;5, &agr;v&bgr;6 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: September 26, 2000Date of Patent: February 4, 2003Assignee: Amgen Inc.Inventors: Zhidong Chen, Celia Dominguez, Ellen Grenzer-Laber, Nianhe Han, Longbing Liu, Ofir A. Moreno, Melvin C. Rutledge, Andrew S. Tasker
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Publication number: 20030022883Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: ApplicationFiled: November 30, 2001Publication date: January 30, 2003Inventors: Dana V. Ferraris, Jia-He Li, Vincent J. Kalish, Jie Zhang
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Patent number: 6489473Abstract: A method of effecting serotonin-2-receptor antagonism in a mammal in need thereof, which entails administering to the mammal an effective amount of a compound of the formula (I), or a pharmaceutically acceptable salt thereof: wherein ring P, the dashed line, Z1, Z2, A and Y are as defined herein.Type: GrantFiled: March 9, 2001Date of Patent: December 3, 2002Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Tetsuo Shimamoto, Kyoko Nakanishi, Norio Inomata
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Patent number: 6486315Abstract: Mercaptoalkanoylamino lactam acids are recrystallized by treatment with an agent that minimizes the formation of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite.Type: GrantFiled: November 16, 2001Date of Patent: November 26, 2002Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Rajendra P. Deshpande, James Simpson
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Patent number: 6423840Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention.Type: GrantFiled: January 31, 2001Date of Patent: July 23, 2002Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Patent number: 6410526Abstract: The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: GrantFiled: May 31, 2000Date of Patent: June 25, 2002Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, Robert S. Meissner, James J. Perkins
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Patent number: 6407229Abstract: The invention relates to processes for the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine, or derivatives thereof. Furthermore, the invention also relates to the compounds formed during the preparation of 4a,5,9,10,11,12-hexahydro-6H-benzofuro(3a,3,2-ef)(2)benzazepine.Type: GrantFiled: April 23, 1999Date of Patent: June 18, 2002Assignee: Sanochemia Pharmazeutika AGInventors: Laszlo Czollner, Johannes Fröhlich, Ulrich Jordis, Bernhard Küenburg
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Publication number: 20020072515Abstract: A method of effecting serotonin-2-receptor antagonism in a mammal in need thereof, which entails administering to the mammal an effective amount of a compound of the formula (I), or a pharmaceutically acceptable salt thereof: 1Type: ApplicationFiled: March 9, 2001Publication date: June 13, 2002Applicant: SUNTORY LIMITEDInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Tetsuo Shimamoto, Kyoko Nakanishi, Norio Inomata
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Publication number: 20020065413Abstract: Methods for producing anhydrous mirtazapine crystals that are either (1) substantially free of lower alcohol insolubles or (2) substantially free of residual solvent and have an average particle diameter of from 10 to 50 &mgr;m, are provided, and the resulting anhydrous mirtazapine crystals produced thereby, which are useful in pharmaceuticals.Type: ApplicationFiled: April 27, 2001Publication date: May 30, 2002Applicant: Sumika Fine Chemicals Co., Ltd.Inventors: Chiharu Maeda, Sadanobu Yoshikawa, Eiichi Iishi
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Patent number: 6372735Abstract: Tricyclic triazolobenzazepine derivatives in the form or a prodrug are provided. The compounds according to the present invention are those represented by formula (I) and pharmacologically acceptable salts and solvates thereof. The compounds are useful as antiallergic agents and exhibit excellent bioavailability.Type: GrantFiled: March 29, 2000Date of Patent: April 16, 2002Assignee: Meiji Seika Kaisha, Ltd.Inventors: Yasuo Ohtsuka, Toshio Nishizuka, Sohjiro Shiokawa, Seiji Tsutsumi, Mami Kawaguchi, Hideo Kitagawa, Hiromi Takata, Takashi Shishikura, Toyoaki Ishikura, Kenichi Fushihara, Yumiko Okada, Sachiko Miyamoto, Maki Shiobara
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Patent number: 6348456Abstract: An essentially pure noribogaine compound having the formula: wherein R is hydrogen or a hydrolyzable group of the formula: wherein X is an unsubstituted C1-C12 group or a C1-C12 group substituted by lower alkyl or lower alkoxy groups, wherein the noribogaine compound having the hydrolyzable group hydrolyzes in vivo to form 12-hydroxy ibogamine.Type: GrantFiled: October 8, 1996Date of Patent: February 19, 2002Inventors: Deborah C. Mash, Juan Sanchez-Ramos, W. Lee Hearn
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Patent number: 6340752Abstract: Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite. Such agents are also employed in the recrystallization and reprocessing of the mercaptoalkanoylamino lactam acids.Type: GrantFiled: December 9, 1998Date of Patent: January 22, 2002Assignee: Bristol-Myers Squibb Co.Inventors: David R. Kronenthal, Theodor Denzel, Bang-Chi Chen, James H. Simpson, Rajendra P. Deshpande
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Patent number: 6313290Abstract: The invention relates to azolobenzazepine derivatives of the formula I: wherein: X is O or S; R1, R2, R3 and R4 are independently hydrogen, perfluorolower-alkyl, halogen, nitro or cyano; and C together with the carbon atoms to which it is attached forms a 5-membered aromatic heterocycle, to pharmaceutical compositions containing them and to methods for the treatment of neurological disorders utilizing them.Type: GrantFiled: September 22, 2000Date of Patent: November 6, 2001Assignee: Zeneca LimitedInventors: Joseph James Lewis, Kelly Anne Brush, Laura Enid Garcia-Davenport, William Jackson Frazee, Marc Jerome Chapdelaine
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Patent number: 6288073Abstract: A compound selected from those of formula (I): in which: X and Y represent hydrogen, halogen, hydroxy, mercapto, cyano, nitro, alkyl, alkoxy, trihaloalkyl, optionally substituted amino, methylenedioxy, or ethylenedioxy, R1 represents hydrogen, or alkyl, R2 represents hydrogen, hydroxy, alkyl, alkoxy, alkylcarbonyloxy, or optionally substituted ammo, R3 and R4 represent hydrogen, or alkyl, A represents —CH═CH—, or —CH(R5)—CH(R6)— wherein R5 and R6 are as defined in the description, their isomers, N-oxides, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of cancer.Type: GrantFiled: June 19, 2000Date of Patent: September 11, 2001Assignee: Adir et CompagnieInventors: Michel Koch, François Tillequin, Sylvie Michel, Ghanem Atassi, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 6281227Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.Type: GrantFiled: December 2, 1999Date of Patent: August 28, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
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Patent number: 6271371Abstract: The subject invention concerns a process for the preparation of a compound of formula (2), which comprises phenolic oxidation of a compound of formula (1) wherein X1 and X2 are independently selected from H or a protecting group for the phenolic function, e.g. acyl or trialkylsilyl; groups A1, A2, B1, B2 and Y are selected so as to render the nitrogen atom non-basic; Z is a blocking group, e.g. Br or t-butyl; and R is H, alkyl, aryl, or arylalkyl, and wherein the process is carried out in a two-phase liquid system comprising an aqueous base and an organic solvent having a dielectric constant below 4.8.Type: GrantFiled: September 23, 1999Date of Patent: August 7, 2001Assignee: Janssen Pharmaceutica, N.V.Inventors: James Henshilwood, Nicholas Bernard Johnson
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Patent number: 6268369Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: May 16, 1997Date of Patent: July 31, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Dhanapalan Nagarathnam, George Chiu, T. G. Murali Dhar, Wai C. Wong, Mohammad R. Marzabadi, Charles Gluchowski, Bharat Lagu, Shou Wu Miao
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Patent number: 6218376Abstract: Compounds of formula I or salts thereof where for example Y is a group of the formula (i) and R1 is a group of formula (ii) are provided along with compositions containing them and processes for their preparation. The compounds are P2-purinoreceptor 7-transmembrane G-protein coupled receptor antagonists, and are useful in the treatment of inflammatory conditions.Type: GrantFiled: December 9, 1998Date of Patent: April 17, 2001Assignee: AstraZeneca UK LimitedInventors: Nicholas Kindon, Premji Meghani, Stephen Thom
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Patent number: 6211362Abstract: Disclosed are pyrroloazepine compounds and their salts. These pyrroloazepine compounds are represented by the following formula: wherein the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 is H but, when the bond is absent, Z1 and Z2 are both Hs; Z1 is H and Z2 is OH; Z1 and Z2 are both SR5s in which R5 is alkyl, aralkyl or aryl; or Z1 and Z2 are combined together to represent O, NOR6 in which R6 is H, alkyl, aralkyl or aryl, or C2-C3 alkylenedithio; R is H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl; and the ring P is a specific pyrrole ring. These pyrroloazepine compounds and salts are effective as preventives or therapeutics for general circulatory diseases such as hypertension, heart failure, ischemic hear diseases, cerebrovascular disturbances and peripheral circulatory disturbances. Their production processes are also disclosed.Type: GrantFiled: August 17, 2000Date of Patent: April 3, 2001Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Norio Inomata
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Patent number: 6211361Abstract: A method for making debromohymenialdisine (DBH) 2 and analogs thereof is described. One embodiment of the present method first comprises forming hymenin 4, and then converting hymenin into DBH 2 as described herein. One such embodiment first comprises providing a compound having Formula 3 where R is independently selected from the group consisting of hydrogen and lower aliphatic, and X is independently selected from the group consisting of hydrogen and halogen. A compound having Formula 3, such as Compound 10 with R and X as hydrogen, is then converted to DBH 2 or an analog thereof. An alternative embodiment of the method comprises forming Compound 30 or Compound 32, which are then directly converted to DBH 2. Alternatively, Compound 30 can be converted to Compound 10, which is then subsequently converted to DBH 2 by reaction with a halogen in the presence of an acid.Type: GrantFiled: July 20, 1999Date of Patent: April 3, 2001Assignee: State of Oregon acting by and through The Oregon State Board of Higher Education on behalf of Oregon, State UniveristyInventors: David A. Horne, Kenichi Yakushijin
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Patent number: 6204261Abstract: The present invention relates to pyradazino[1,2-a][1,2]diazepine-1-carboxamide compounds of formula: which compounds are inhibitors of interleukin-1beta converting enzyme.Type: GrantFiled: December 6, 1996Date of Patent: March 20, 2001Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, Yong Gu, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Philip Nyce, Andrea L. C. Robidoux, Michael Su, M. Woods Wannamaker, Keith P. Wilson, Robert E. Zelle
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Patent number: 6200967Abstract: This invention relates to a compound of the Formula I X—C(O)—Y—G—R I (wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a compound or salt, pharmaceutical compositions comprising such a compound or salt and methods of their use as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.Type: GrantFiled: December 17, 1998Date of Patent: March 13, 2001Assignee: Eli Lilly and CompanyInventors: Valentine J Klimkowski, Aaron L Schacht, Michael R Wiley
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Patent number: 6197954Abstract: The synthesis of C11N5 marine sponge alkaloids (±)-hymenin (1), stevensine (2), hymenialdisine (3), and debromohymenialdisine (4) is described. These natural products are the primary family members of the sponge metabolites that contain a fused pyrrolo[2,3-c]azepin-8-one ring system with either a 2-aminoimidazole (AI) or glycocyamidine appendage. The key steps in the synthesis centered around the generation of novel azafulvenium ions and their regioselective heterodimerization with AI in order to create the tricyclic core. A rarely used protodebromination/oxidation strategy was employed to selectively generate the desired a-bromo substitution pattern seen in hymenialdisine (3). In addition, the AI moiety was shown to be a useful precursor to the glycocyamidine unit found in 3 and 4, which suggests that AI derived natural products may be the biogenic forerunners to glycocyamidine metabolites.Type: GrantFiled: January 30, 1998Date of Patent: March 6, 2001Assignee: The Trustees of Columbia University in the City of New YorkInventors: David A. Horne, Kenichi Yakushijin
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Patent number: 6187772Abstract: Disclosed are pyrroloazepine compounds and their salts. These pyrroloazepine compounds are represented by formula (I) wherein the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 is H but, when the bond is absent, Z1 and Z2 are both Hs; Z1 is H and Z2 is OH; Z1 and Z2 are both SR5s in which R5 is alkyl, aralkyl or aryl; or Z1 and Z2 are combined together to represent O, NOR6 in which R6 is H, alkyl, aralkyl or aryl, or C2-C3 alkylenedithio; R is H, alkyl, cycloalkyl, cycloalkyl alkyl or aralkyl; and the ring P is a specific pyrrole ring. These pyrroloazepine compounds and salts are effective as preventives or therapeutics for general circulatory diseases such as hypertension, heart failure, ischemic hear diseases, cerebrovascular disturbances and peripheral circulatory disturbances.Type: GrantFiled: November 12, 1998Date of Patent: February 13, 2001Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Norio Inomata
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Patent number: 6150355Abstract: A phenylpiperidine derivative or pharmaceutical acceptable salt thereof represented by formula (I): ##STR1## wherein X represents CH or N; Y--Z represents CH.sub.2 --O, CH.sub.2 --S, CH.sub.2 --CH.sub.2, CH.dbd.CH or CONR.sup.5 (wherein R.sup.5 represents hydrogen or lower alkyl); R.sup.1 represents hydrogen, lower alkyl, halogen, lower alkoxy or trifluoromethyl; and R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents hydrogen, lower alkyl or QR.sup.6 (wherein Q represents a single bond or lower alkylene, and R.sup.6 represents hydroxy, lower alkoxyalkoxy, lower alkoxy, lower alkylthio, nitro, halogen, lower alkanoyloxy, lower alkoxycarbonyl, lower alkanoyl or carboxyl).The present invention provides novel phenylpiperidine derivatives useful as analgesics.Type: GrantFiled: March 13, 1998Date of Patent: November 21, 2000Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Hirokazu Koshimura, Shigeru Aono, Shunji Ichikawa, Shigeto Kitamura
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Patent number: 6124281Abstract: The invention relates to azolobenzazepine derivatives of formula (I), wherein: X is O or S; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, perfluorolower-alkyl, halogen, nitro or cyano; and C together with the carbon atoms to which it is attached forms a 5-membered aromatic heterocycle selected from the group consisting of a pyrazol and triazole, to pharmaceutical compositions containing them and to methods for the treatment of neurological disorders utilizing them.Type: GrantFiled: September 3, 1998Date of Patent: September 26, 2000Assignee: Zeneca LimitedInventors: Joseph James Lewis, Kelly Anne Brush, Laura Enid Garcia-Davenport, William Jackson Frazee, Marc Jerome Chapdelaine
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Patent number: 6124278Abstract: Compounds based on the benzoxazine ring system that are remarkably more potent than corresponding benzoyl piperidines for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof, and methods for their use for treatment of 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: April 3, 1998Date of Patent: September 26, 2000Assignee: The Regents of the University of CaliforniaInventors: Gary A. Rogers, Peter Johnstrom
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Patent number: 6103899Abstract: The subject invention provides a bicyclic aminoimidazole compound, a hydroxyalkyl aminoimidazole compound, a bicyclic pyrrole compound, a hymenin compound, an aldehyde aminoimidazole compound, a ketal aminoimidazole compound, a tricyclic compound, and a tetrahydropurine compound. The subject invention also provides for processes for preparing the compounds.Type: GrantFiled: November 4, 1998Date of Patent: August 15, 2000Assignee: The Trustees of Columbia University in the City of New YorkInventors: David A. Horne, Kenichi Yakushijin