Unsaturated Carbocyclic Ring Attached Indirectly To The Six-membered Hetero Ring Through An Acyclic Hydrocarbon Chain Patents (Class 546/149)
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Publication number: 20100022776Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate.Type: ApplicationFiled: December 10, 2007Publication date: January 28, 2010Inventors: Gary L. Cantrell, Dan P. Magparangalan, Frank W. Moser, Jian Bao, Christopher W. Grote, Peter X. Wang
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Publication number: 20100010226Abstract: The present invention relates to the compound of formula 7*acetate (see below), a process for its preparation, and its useType: ApplicationFiled: July 2, 2009Publication date: January 14, 2010Inventors: Maria Andreas Hendrikus De Vries, Doris Domin, Matthias Helms, Chistoph Imboden, Ralph Koberstein, Zarghun Nazir, Wolfgang Skranc, Michael Stanek, Wilhelm Tschebull, Maria Gerardus Karel Verzijl, Jürgen Stichler
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Patent number: 7622586Abstract: Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.Type: GrantFiled: April 30, 2007Date of Patent: November 24, 2009Assignee: Mallinckrodt Inc.Inventors: Peter Xianqi Wang, Frank W. Moser, Gary L. Cantrell
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Publication number: 20090275609Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: April 22, 2009Publication date: November 5, 2009Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Patent number: 7601739Abstract: Compounds for the treatment of estrogen-receptor related maladies are provided. Compounds with anti-androgenic properties also are provided. In particular, the invention provides compounds that are tetrahydroquinoline phenylamide derivatives and are useful for the treatment of breast and prostate cancer, and osteoporosis.Type: GrantFiled: February 8, 2006Date of Patent: October 13, 2009Assignee: Virgina Commonwealth UniversityInventors: Richmond Danso-Danquah, Donald J. Abraham, Hsiang-Ru Lin, Jim Christian Burnett
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Publication number: 20090247757Abstract: Novel chemical agents are described herein. More a ligand of general Formula I: wherein R1, R2, R3 and R4, are independently selected from the group consisting of hydrogen, halogen, hydroxy, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C1-C10 alkoxy, C1-C10 alkylthio, C(O)R5, C(O)OR5, C(O)NHR5, Si(R5)3, benzyl and aryl; X is selected from the group consisting of Cl, Br, I, OR6, O-Prot, OPR6, P(R6)2, NHR6, N(R6)2, NHCSNHR6, NHCONHR6 and SR6; and R5 and R6 are independently selected from the group consisting of hydrogen, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C1-10 alkoxy, phenyl, and aryl. These ligands are useful in asymmetric reactions as well as in asymmetric synthesis of molecules of biological interest.Type: ApplicationFiled: November 7, 2008Publication date: October 1, 2009Applicant: Chao-Jun LiInventors: Chao-Jun Li, Jianqing Feng
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Patent number: 7595399Abstract: The compounds of the invention are inhibitors of alpha4 containing integrin-mediated binding to ligands such as VCAM-1 and MAdCAM.Type: GrantFiled: February 4, 2004Date of Patent: September 29, 2009Assignee: Genentech, Inc.Inventors: David Y. Jackson, Frederick C. Sailes, Daniel P. Sutherlin
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Publication number: 20090221829Abstract: The present invention relates to 3,4-dihydroisoquinolinium salt derivatives. More specifically, the present invention relates to 3,4-dihydroisoquinolinium salt derivatives of the following chemical formula (I).Type: ApplicationFiled: June 1, 2006Publication date: September 3, 2009Inventors: Jungho Kim, Sangphil Lee, Junyoung Choi, Young-Ki Paik, Yousuk Lee, Hyungmin Joo
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Patent number: 7538121Abstract: Certain compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, P, X, Y, q, r ans s are as defined in the specification, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds in medicine.Type: GrantFiled: February 13, 2003Date of Patent: May 26, 2009Assignee: Glaxo Group LimitedInventors: Gregor James MacDonald, Darren Jason Mitchell, Harshad Kantilal Rami, Mervyn Thompson, Susan Marie Westaway
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Patent number: 7511060Abstract: Novel opiate intermediate compositions and methods of synthesis that include changing the substitution pattern on the aromatic ring of the pre-Grewe intermediate are provided.Type: GrantFiled: April 30, 2007Date of Patent: March 31, 2009Assignee: Mallinckrodt Inc.Inventors: Peter Xianqi Wang, Frank W. Moser
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Publication number: 20090069328Abstract: The present invention relates to ?-alkyl substituted N-acyltryptophanols of the formula I in which R1, R2, R3, R4, R5, R6, Q, X and W have the meaning as defined in the description. The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.Type: ApplicationFiled: August 14, 2008Publication date: March 12, 2009Inventors: Lars Wortmann, Marcus Koppitz, Hans Peter Muhn, Anna Schrey, Ronald Kuehne
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Publication number: 20090030036Abstract: The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBAs are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, inflammatory diseases, oxidative stress related disorders such as Parkinson's and stroke, neurological disorders, ophthalamic disorders, cardiovascular disease, and obesity.Type: ApplicationFiled: January 22, 2008Publication date: January 29, 2009Inventors: James T. Dalton, Duane D. Miller, Michael L. Mohler, Seoung-Soo Hong, Zhongzhi Wu, Devesh Srivastava
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Publication number: 20080161344Abstract: Melanin concentrating hormone receptor ligands (especially substituted tetrahydroisoquinoline analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: ApplicationFiled: February 9, 2005Publication date: July 3, 2008Inventors: Cheryl K. Steenstra, Taeyoung Yoon, John M. Peterson
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Publication number: 20080153868Abstract: There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.Type: ApplicationFiled: December 6, 2007Publication date: June 26, 2008Inventors: Lorin A. Thompson, Kenneth M. Boy, Jianliang Shi, John E. Macor, Andrew C. Good, Lawrence R. Marcin
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Publication number: 20080146597Abstract: Disclosed are therapeutic tetrahydroisoquinoline compositions for the treatment of cancer, these compositions having selectivity for cancer cells while demonstrating few, if any, deleterious side effects on normal cells.Type: ApplicationFiled: November 21, 2007Publication date: June 19, 2008Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONInventors: Renukadevi Patil, Charles Ryan Yates, Duane D. Miller, Eldon E. Geisert
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Patent number: 7312222Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: March 25, 2004Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 7309708Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: GrantFiled: November 18, 2004Date of Patent: December 18, 2007Assignee: Birstol-Myers Squibb CompanyInventors: Yong Tu, Paul Michael Scola, Andrew Charles Good, Jeffrey Allen Campbell
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7074806Abstract: A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, or a tautomer prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: May 28, 2003Date of Patent: July 11, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Thomas Martin Kirrane, Jr., Daniel Kuzmich, John Robert Proudfoot, Hossein Razavi, David Thomson
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Patent number: 7041664Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.Type: GrantFiled: June 14, 2004Date of Patent: May 9, 2006Assignee: Neurogen CorporationInventors: Jun Yuan, George Maynard, Alan Hutchison
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Patent number: 6949565Abstract: Novel isoquinoline derivatives which are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes are disclosed. Preferred compounds which are specific inhibitors of protein kinase B are also disclosed. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune diseases, are also disclosed.Type: GrantFiled: May 30, 2001Date of Patent: September 27, 2005Assignees: Develogen Israel Ltd., Yissum Research Development Co. of the Hebrew University of JerusalemInventors: Nurit Livnah, Alexander Levitzki, Hadas Reuveni
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Patent number: 6875765Abstract: The novel arylsulfonamide ether compounds, pharmaceutical compositions and uses thereof as inhibitors of interleukin-1? converting enzyme and other cysteine proteases in the ICE family are described. In one embodiment, the compound is described by the generalized structure: and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof. In addition, methods of treating stroke, inflammatory diseases, septic shock, repurfusion injury, Alzheimer's disease, and shigellosis, using a compound of the invention or a pharmaceutical composition thereof, are described.Type: GrantFiled: May 10, 2002Date of Patent: April 5, 2005Assignee: Warner-Lambert CompanyInventors: James Knobelsdorf, Sheryl Hays, Charles J. Stankovic, Kimberly S. Para, Michael K. Connolly, Paul Galatsis, William Harter, Aurash B. Shahripour, Mark Stephen Plummer, Beth Lunney, Bernd Janssen, Jay Bradford Fell
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Patent number: 6825213Abstract: The invention provides &bgr;3-adrenoreceptor agonists, pharmaceutical compositions comprising &bgr;3-adrenoreceptor agonist compounds, and methods of using such compounds for stimulating, regulating or modulating metabolism of fats in adipose tissue in animals.Type: GrantFiled: June 25, 2003Date of Patent: November 30, 2004Assignee: Molecular Design International, Inc.Inventors: Dennis R. Feller, Duane D. Miller
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Patent number: 6809091Abstract: A method for the manufacture of a substance having an apoptosis-inducing ability characterized in including a step of subjecting at least one compound selected from the following (a), (b), (c) and (d) [excluding uronic acid and/or uronic acid derivatives; and compounds which contain uronic acid and/or uronic acid derivatives] to a heating treatment: (a) pentose; (b) pentose derivatives; (c) compounds containing pentose; (d) compounds containing pentose derivatives.Type: GrantFiled: June 28, 2000Date of Patent: October 26, 2004Assignee: Takara Bio Inc.Inventors: Yoko Tatsumi, Hiroaki Sagawa, Hiromu Ohnogi, Eiji Kobayashi, Hua-Kang Wu, Nobuto Koyama, Katsushige Ikai, Ikunoshin Kato
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Patent number: 6784186Abstract: This invention relates to novel structural analogues and derivatives of compounds with general analgesic or related pharmacological activity. In particular the invention relates to derivatives of opioid compounds, particularly morphine and related compounds, in which an opioid compound is linked via the nitrogen at position 17 to a spacer group, which in turn is linked to a charged group, or a pharmaceutically acceptable salt thereof. In particularly preferred embodiments the opioid compound is morphine, codeine, or buprenorphine.Type: GrantFiled: November 20, 2000Date of Patent: August 31, 2004Inventors: Roy W. Jackson, Kamani R. Subasinghe, Alan L. A. Boura
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Patent number: 6780998Abstract: The oxidation hair dye precursor composition contains from 0.005 to 20.0 percent by weight of one or more coupler compounds and from 0.005 to 20.0 percent by weight of one or more developer compounds. The one or more developer compounds include at least one substituted 2-aminoalkyl-1,4-diaminobenzene compound of the formula (I): New substituted 2-aminoalkyl-1,4-diaminobenzene compounds of formula (I) are described.Type: GrantFiled: April 17, 2002Date of Patent: August 24, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6703392Abstract: The invention relates to novel 1,2,3,4-tetrahydroisochinoline derivatives of formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.Type: GrantFiled: February 24, 2003Date of Patent: March 9, 2004Assignee: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Michael Cappi, Martine Clozel, Walter Fischli, Ralf Koberstein
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Publication number: 20040044212Abstract: 3,4-Dihydroisoquinoline and isoquinoline compounds of formula I, in which Ar represents a phenyl raidcal of the formulae IIa, IIb or IIc are novel effective PDE7 inhibitors.Type: ApplicationFiled: August 21, 2003Publication date: March 4, 2004Inventors: Steffen Weinbrenner, Beate Schmidt, Gerlard Grundler, Josef Stadwieser, Armin Hatzelmann, Geert Jan Sterk
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Publication number: 20040019077Abstract: Novel isoquinoline derivatives which are useful as inhibitors of protein kinases for experimental, medical, and drug design purposes are disclosed. Preferred compounds which are specific inhibitors of protein kinase B are also disclosed. Furthermore, pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment and diagnosis of cancers, diabetes, cardiovascular pathologies, hemorrhagic shock, obesity, inflammatory diseases, diseases of the central nervous system, and autoimmune diseases, are also disclosed.Type: ApplicationFiled: April 3, 2003Publication date: January 29, 2004Inventors: Nurit Livnah, Alexander Levitzki, Hadas Reuveni
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Patent number: 6653321Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.Type: GrantFiled: July 28, 2000Date of Patent: November 25, 2003Assignee: Telik, Inc.Inventors: Wayne R. Spevak, Songyuan Shi, Prasad V. V. S. V. Manchem, Michael R. Kozlowski, Steven R. Schow, Robert T. Lum, Louise Robinson, Jeong Weon Park
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Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Antimalarial naphthylisoquinoline alkaloids and pharmaceutical compositions and medical uses thereof
Patent number: 6627641Abstract: The present invention provides antimalarial pharmaceutical compositions containing antimalarial naphthylisoquinoline alkaloids or antimalarial derivatives thereof, useful new antimalarial naphthylisoquinoline alkaloid derivatives, methods for obtaining such derivatives, and methods of using such antimalarial compounds for the prevention of malaria infections in mammals and for treating mammals with malarial infections. The antimalarial compounds of the present invention inhibit the reproduction and cytopathicity of Plasmodium sp. parasites in vitro and in vivo.Type: GrantFiled: April 16, 1997Date of Patent: September 30, 2003Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Guido François, Gerhard Bringmann, J. David Phillipson, Michael R. Boyd, Laurent Aké Assi, Christoph Schneider, Georges Timperman -
Publication number: 20030181723Abstract: The present invention provides a new process for the preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of the present invention results in higher yields of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride without sacrificing its purity. The processes of the present inventin can be used to prepare not only the 2S,3S-derivative, but also the 2R,3S-, 2S,2R- and the 2R,3R-derivatives.Type: ApplicationFiled: March 4, 2003Publication date: September 25, 2003Applicant: Aerojet Fine Chemicals LLC, a Delaware limited liability companyInventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, Roland P. Carlson, John Leach, Thomas G. Archibald, Robert G. Miotke
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Patent number: 6593341Abstract: The invention provides compounds useful as &bgr;3-adrenorecptor agonists and pharmaceutical compositions comprising such compounds. The invention further includes a method for stimulating, regulating, and modulating metabolism in fats of adipose tissue in mammals by administering an effective amount of a compound of the invention.Type: GrantFiled: June 17, 2002Date of Patent: July 15, 2003Assignee: Molecular Design International, Inc.Inventors: Dennis R. Feller, Duane D. Miller
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Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases
Patent number: 6573278Abstract: The present invention relates to new aryl ether sulphonamides and analogues, processes for their preparation and their use for the treatment of neurodegenerative disorders, in particular for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy and craniocerebral trauma.Type: GrantFiled: June 11, 2001Date of Patent: June 3, 2003Assignee: Bayer AktiengesellschaftInventors: Joachim Mittendorf, Jürgen Dressel, Michael Matzke, Jörg Keldenich, Klaus-Helmut Mohrs, Siegfried Raddatz, Jürgen Franz, Peter Spreyer, Verena Vöhringer, Joachim Schuhmacher, Michael-Harold Rock, Ervin Horváth, Arno Friedl, Frank Mauler, Jean Marie Viktor de Vry, Reinhard Jork -
Publication number: 20030087901Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: ApplicationFiled: February 27, 2002Publication date: May 8, 2003Applicant: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
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Publication number: 20030036550Abstract: Compounds which are highly potent and highly specific &bgr;3-Adrenoreceptor agonists are provided. The compounds are formulated into pharmaceutical preparations and administered for stimulating, regulating and modulating metabolism of fats in adipose tissues in animals, particularly humans and other mammals. The compounds of the invention have the structure (A). R1 and R2 arc each independently members selected from the group consisting of H, OH, Cl, NO2, CH3SO2NH, NH2, CH3O and weak e4 acids of the structure R7—NH, where R7 is an acyl group, wherein at least one of R1 and R2 is OH. It is generally preferred that R2 be OH; R3, R4, and R5 are variously and independently members selected from I, Br, Cl, F, OCH3, CH3, alkyl, alkylaryl, aminoalkyl, thioalkyl, and O-alkyl. Preferably, R4 and R5 are each a halogen, the same or different; R6 is an acid moiety which forms an acid salt with the NH group. R6 is desirably HCl or (COOH)2.Type: ApplicationFiled: June 17, 2002Publication date: February 20, 2003Inventors: Dennis R. Feller, Duane D. Miller
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Patent number: 6509351Abstract: The present invention relates to compounds of formula (I): as well as the salts or solvates thereof, to pharmaceutical compositions containing them, to a process for preparing them and to synthetic intermediates in this process.Type: GrantFiled: April 19, 2002Date of Patent: January 21, 2003Assignee: Sanofi-SyntelaboInventors: Marco Baroni, Bernard Bourrie, Rosanna Cardamone, Pierre Casellas, Umberto Guzzi
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Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 6476226Abstract: This invention relates to novel isoxazolines and isoxazoles of formula (I): or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: July 13, 2001Date of Patent: November 5, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Joanne M. Smallheer, Shuaige Wang, Prabhakar Kondaji Jadhav
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Patent number: 6462044Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.Type: GrantFiled: August 30, 2001Date of Patent: October 8, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
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Publication number: 20020107263Abstract: Squaric acid derivatives of formula (1) are described: 1Type: ApplicationFiled: July 5, 2001Publication date: August 8, 2002Inventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
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Patent number: 6420130Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.Type: GrantFiled: April 28, 1999Date of Patent: July 16, 2002Assignee: Aurora Biosciences CorporationInventors: Lewis R. Makings, Gregor Zlokarnik
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Patent number: 6417362Abstract: Disclosed are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof. The compounds can inhibit the biosynthesis of triglycerides in the liver and can inhibit the secretion of lipoprotein containing apolipoprotein B from the liver. Therefore, they are useful for the prevention or treatment of hyperlipidemia (particularly hyper-very-low-density-lipoproteinemia) and arteriosclerotic diseases, such as cardiac infarction, or pancreatitis induced by hyperlipidemia.Type: GrantFiled: November 30, 1999Date of Patent: July 9, 2002Assignee: Meiji Seika Kaisha, Ltd.Inventors: Naoto Ohkura, Takashi Tsuruoka, Takayuki Usui, Yukiko Hiraiwa, Tetsuya Matsushima, Masaharu Shiotani, Tetsutaro Niizato, Yuuko Nakatani, Shigeki Suzuki, Chidsuko Kuroda, Kiyoaki Katano
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Patent number: 6414154Abstract: Compounds of formula (I), wherein: R1 represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy, pentafluoroethyl, C1-4alkyl, C1-4alkoxy, arylC1-4alkoxy, C1-4alkylthio, C1-4alkoxyC1-4alkyl, C3-6cycloalkylC1-4alkoxy, C1-4alkanoyl, C1-4alkoxycarbonyl, C1-4alkylsulfonyl, C1-4alkylsulfonyloxy, C1-4alkylsulfonylC1-4alkyl, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-4alkyl, C1-4alkylsulfonamido, C1-4alkylamido, C1-4alkylsulfonamidoC1-4alkyl, C1-4alkylamidoC1-4alkyl, arylsulfonamido, arylcarboxamido, arylsulfonamidoC1-4alkyl, arylcarboxamidoC1-4alkyl, aroyl, aroylC1-4alkyl, or arylC1-4alkanoyl group; a group R3OCO(CH2)p, R3CON(R4)(CH2)p, R3R4NCO(CH2)p or R3R4NSO2(CH2)p where each of R3 and R4 independently represents a hydrogen atom or a C1-4alkyl group or R3R4 forms part of a C3-6azacyloalkane or C3-6(2-oxo)azacycloalkane ring and p represents zero or an integer from 1 to 4; or a group Ar1—Z,Type: GrantFiled: March 16, 2001Date of Patent: July 2, 2002Assignee: SmithKline Beecham p.l.c.Inventor: Antonio Kuok Keong Vong
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Patent number: 6331543Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.Type: GrantFiled: September 1, 1999Date of Patent: December 18, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada, Richard A. Earl, Subhash P. Khanapure
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Patent number: 6303785Abstract: Compounds having Formula 3 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: October 16, 2001Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Roshantha A. Chandraratna
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: RE37729Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: February 3, 1999Date of Patent: June 4, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley