Chalcogen Bonded Directly To Ring Carbon Of The Additional Six-membered Nitrogen Containing Hetero Ring Patents (Class 514/253.12)
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Patent number: 7378420Abstract: Derivatives of urea that contain piperazine rings and additional substitution with aromatic groups are effective in ameliorating conditions associated with unwanted calcium ion channel activity.Type: GrantFiled: August 30, 2005Date of Patent: May 27, 2008Assignee: Neuromed Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Hossein Pajouhesh, Yanbing Ding, Terrance P. Snutch
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Publication number: 20080096898Abstract: Compounds of formula I in free or salt form, wherein Ar, R1, R2, R3, X and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: August 9, 2005Publication date: April 24, 2008Applicant: NOVARTIS AGInventor: Darren Mark Legrand
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Publication number: 20080045509Abstract: Certain substituted benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.Type: ApplicationFiled: June 21, 2007Publication date: February 21, 2008Inventors: Brett Allison, Michael P. Curtis, Cheryl A. Grice, John M. Keith, Michael A. Letavic, Jennifer M. B. Miller, Emily M. Stocking
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Publication number: 20080045541Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: ApplicationFiled: February 5, 2005Publication date: February 21, 2008Applicant: Bayer-HealthCare AGInventors: Heike Gielen-Haertwig, Barbara Albrecht, Marcus Bauser, Jorg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
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Publication number: 20080004286Abstract: The present invention discloses a method of using compounds, which have HDM2 protein antagonist activity, to treat or prevent cancer, other diseases caused by abnormal cell proliferation, diseases associated with HDM2, or diseases caused by inadequate P53 activity.Type: ApplicationFiled: June 27, 2007Publication date: January 3, 2008Inventors: Yaolin Wang, Rumin Zhang, Yao Ma, Brian Robert Lahue, Gerald W. Shipps
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Patent number: 7314879Abstract: The present invention relates to melanocortin receptor agonist of the formula (I): which is useful in the treatment for obesity, diabetes, and male and/or female sexual dysfunctionType: GrantFiled: January 21, 2003Date of Patent: January 1, 2008Assignee: Eli Lilly and CompanyInventors: Ryan Thomas Backer, Caño Ivan Collado, Oscar De Frutos-Garcia, Christopher William Doecke, Matthew Joseph Fisher, Steven Lee Kuklish, Vincent Mancuso, Michael John Martinelli, Jeffrey Thomas Mullaney, Paul Leslie Ornstein, Chaoyu Xie
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Patent number: 7288545Abstract: This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula: In the above formula, each of and , independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is CH(RcRd) when is a single bond, or C(RcRd) when is a double bond; each of R1 and R2, independently, is H, C(O)Re, C(O)ORe, C(O)NReRf, or SO2Re; and each of Ra, Rb, Rc, Rd, Re, and Rf, independently, is H, C1-C6 alkyl, aryl, heteroaryl, C3-C8 cycloalkyl, or C3-C8 heterocycloalkyl; or Ra and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; or R1 and Ra or R1 and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; provided that one of Rc and Rd is aryl or heteroaryl.Type: GrantFiled: October 20, 2003Date of Patent: October 30, 2007Assignee: AngioRx CorporationInventors: Che-Ming Teng, Hui-Po Wang, Eric I. C. Li, On Lee, Jih-Hwa Guh, Huei-Ting Chen, Ya-Bing Fan, Ya-Lan Chen
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Patent number: 7271168Abstract: The invention provides compounds of formula (1) wherein X, R1 and R2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety and bipolar disorders.Type: GrantFiled: November 8, 2002Date of Patent: September 18, 2007Assignee: Novartis AGInventors: Thomas J. Troxler, Daniel Hoyer
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Patent number: 7230017Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: August 18, 2003Date of Patent: June 12, 2007Assignee: Bayer Healthcare AGInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenich, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
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Patent number: 7226925Abstract: The invention relates to compounds of the general Formula (I): The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of Formula (I).Type: GrantFiled: June 18, 2003Date of Patent: June 5, 2007Assignee: Biovitrum ABInventors: Björn M. Nilsson, Erik Ringberg, Birger Sjöberg, Mattias Jönsson
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Patent number: 7223757Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.Type: GrantFiled: November 30, 2005Date of Patent: May 29, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Mark D. Wittman, Neelakantan Balasubramanian, Upender Velaparthi, Kurt Zimmermann, Mark G. Saulnier, Peiying Liu, Xiaopeng Sang, David B. Frennesson, Karen M. Stoffan, James G. Tarrant, Anne Marinier, Stephan Roy
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Patent number: 7119203Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.Type: GrantFiled: April 25, 2003Date of Patent: October 10, 2006Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
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Patent number: 7101885Abstract: The present invention relates to compounds of formula I wherein Ar, Y and G are as defined in the specification, a is 1 to 4, Z and W are carbon or nitrogen and n is 1, 2 or 3; and to pharmaceutical compositions comprising the compound of formula I and a pharmaceutically effective carrier; and to a method useful in treating or preventing in mammals, including humans, a disorder or condition selected from the group consisting of anxiety, depression, dysthymia, major depressive disorder, migraine, post-traumatic stress disorder, avoidant personality disorder, borderline personality disorder and phobias.Type: GrantFiled: June 15, 2004Date of Patent: September 5, 2006Assignee: Pfizer IncInventors: John Lowe, III, Mark A. Sanner
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Patent number: 7034042Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C1–C8-alkyl optionally substituted by cyano or halogen, Ar2 is phenyl optionally which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1–C8-alkyl, C1–C8-haloalkyl, C1–C8-alkoxy or C1–C8-alkoxycarbonyl, R1 is C1–C8-alkyl substituted by hydroxy, C1–C8-alkoxy, acyloxy, —N(R2)R3, halogen, carboxy, C1–C8-alkoxycarbonyl, phenyl-C1–C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R?3 are each independently hydrogen or C1–C8-alkyl, or R2 is hydrogen and R3 is acyl or SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen, C1–C8-alkyl optionally substituted by hydroxy or phenyl, or phenyl optionally substituted by C1–C8-alkyl, halogen, cyano or C1–C8-alkoxy, or R4 and R5 togeType: GrantFiled: October 8, 2001Date of Patent: April 25, 2006Assignee: Novartis AGInventors: Gurdip Bhalay, Trevor J Howe, Darren M Le Grand
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Patent number: 7009051Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, X and Y are defined as in the specification. Those compounds are 5HT7 partial agonists and are useful in the treatment of several disorders of the central nervous system.Type: GrantFiled: July 10, 2003Date of Patent: March 7, 2006Assignee: Pfizer IncInventors: Willard M. Welch, Vinod Parikh
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Patent number: 6974817Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof; wherein X, Y, a, b, c, d, R1, R2, R3 and R5 are as defined above useful to treat inflammation and other immune disorders.Type: GrantFiled: June 19, 2002Date of Patent: December 13, 2005Assignee: Pfizer Inc.Inventor: Matthew M. Hayward
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Patent number: 6953801Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), 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: GrantFiled: May 21, 2002Date of Patent: October 11, 2005Assignee: Neurogen CorporationInventors: Alan Hutchison, Linda M. Gustavson, John M. Peterson, Dario Doller, Timothy M. Caldwell, Taeyoung Yoon, Wallace C. Pringle, Yiping Shen, Cheryl Steenstra
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Patent number: 6949552Abstract: There are provided a therapeutic preparation for anxiety neurosis or depression which comprises a MC4 receptor antagonist as an effective ingredient; and a piperazine derivative represented by Formula [1]: [wherein Ar1 is a phenyl group, a substituted phenyl group, a naphthyl group or a substituted naphthyl group; Ar2 is a naphthyl group, a substituted naphthyl group, a quinolyl group, a group represented by the formula: (wherein R4 is a hydrogen atom or a halogen atom; and X—Y is CH—NH, CH—O, CH—S or N—O) or a group represented by the formula: (wherein R5 is a hydrogen atom, a hydroxyl group or a C1-10 alkoxy group); R1 is a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group, a C3-10 alkenyl group, a phenyl group, a 1-cyanoethyl group, a pyrimidin-2-yl group or an amidyl group; R2 and R3 are the same or different, and are each a hydrogen atom or a C1-10 alkyl group; A-B is N—CH2, CH—CH2, C(OH)—CH2 or C?CH; T1 is a single bond, —N(R6)— (wherein R6 is a hydrogen atom or a C1-10 alkyl groupType: GrantFiled: June 27, 2001Date of Patent: September 27, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Shigeyuki Chaki, Taketoshi Okubo, Shin-ichi Ogawa, Takaaki Ishii
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Patent number: 6936610Abstract: The invention relates to heterocyclic derivatives of formula (I) A—B—X1—T1(R2)—L1—T2(R3)—X2—Q??(I) or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.Type: GrantFiled: September 27, 2001Date of Patent: August 30, 2005Assignee: AstraZeneca UK LimitedInventors: Andrew Stocker, John Preston, John Wall Rayner, Michael James Smithers, Paul Turner
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Patent number: 6924289Abstract: The present invention relates to lactam derivatives of the formula wherein R1, R2, R3, A, X, Z, n and the dashed line are defined herein, and pharmaceutical compositions thereof, to processes and intermediates for their preparation, and to their medicinal use as selective agonists and antagonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1D receptors. These compounds are useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.Type: GrantFiled: August 15, 2002Date of Patent: August 2, 2005Assignee: Pfizer IncInventor: Harry R. Howard
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Patent number: 6897218Abstract: A metal complex of a piperazineNONOate derivative of the formula: wherein a) R1 and R2 independently represent hydrogen, linear or branched (C1-C4) alkyl, optionally substituted by 1 or 2 groups selected from the group consisting of hydroxy, (C1-C4) alkoxy, (C1-C4) alkylthio, amino, (C1-C4) alkylamino, di-(C1-C4) alkylamino, carboxy, carbo(C1-C4) alkoxy, aryl, aryloxy, arylthio; or b) R1 and R2 taken together, represent one of the following groups ?CR3-aryl, where R3 represents hydrogen, (C1-C4) linear or branched chain alkyl, optionally substituted by 1 or 2 groups selected from the group consisting of hydroxy, carboxy, aryl; n represents a whole number ranging from 2 to 4; M+ represents a cation of a transition metal or zinc; x represents a whole number which varies from 1 to 3, and indicates the charge units of the cation of the transition metal or of the zinc in relation to its stable oxidation state; A ? represents an inorganic or organic anion which forms stable salts with the NONOate metal complexType: GrantFiled: February 21, 2002Date of Patent: May 24, 2005Assignee: Consiglio Nazionale Delle RicercheInventors: Luigi Casella, Marina Ziche
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Publication number: 20040132710Abstract: Compounds of the formula (I): 1Type: ApplicationFiled: December 17, 2002Publication date: July 8, 2004Applicant: Pfizer Inc.Inventors: Donald Stuart Middleton, Alan Stobie
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Publication number: 20040077647Abstract: Disclosed are compounds of formula (I): 1Type: ApplicationFiled: August 1, 2003Publication date: April 22, 2004Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, Victor Kamhi, Neil Moss, Paul S. Riska, Christopher Pargellis
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Publication number: 20040058933Abstract: The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal health. The compounds according to the invention are preferably 5-HT4 serotoninergic receptor ligands and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, the preparation and use thereof and treatment methods using said compounds.Type: ApplicationFiled: August 13, 2003Publication date: March 25, 2004Inventors: Eric Nicolai, Sophie Curtet, James Sicsic, Frank Lezoualc'h, Rodolphe Fischemeister, Michel Langlois, Magali Maillet, Michele Launay
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Patent number: 6706716Abstract: This invention is directed towards a method of inhibiting activation of a human &agr;1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the receptor, wherein the compound binds selectively to a human &agr;1d adrenergic receptor. This invention provides for a compound which binds selectively to a human &agr;1d adrenergic receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier. This invention further provides for a method of treating a subject afflicted with a disease which is susceptible to treatment by antagonism of the human &agr;1d adrenergic receptor which comprises administering to the subject an amount of the above defined compounds effective to treat the disease.Type: GrantFiled: January 17, 2001Date of Patent: March 16, 2004Assignee: Synaptic Pharmaceutical CorporationInventors: Michael Konkel, John M. Wetzel, Stewart A. Noble, Charles Gluchowski, Douglas A. Craig
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Publication number: 20040048848Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1Type: ApplicationFiled: February 5, 2003Publication date: March 11, 2004Applicant: Schering-Plough Corporation and Pharmacopeia, Inc.Inventors: Dmitri A. Pissarnitski, Hubert B. Josien, Elizabeth M. Smith, John W. Clader, Theodros Asberom, Tao Guo, Douglas W. Hobbs
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Publication number: 20040019047Abstract: The present invention relates to 2,4-disubstituted pyridine-N-oxide compounds of formula (I): 1Type: ApplicationFiled: June 25, 2003Publication date: January 29, 2004Inventors: James D. Rodgers, Haisheng Wang
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Publication number: 20040014769Abstract: The present invention relates to compounds of the formula I 1Type: ApplicationFiled: July 10, 2003Publication date: January 22, 2004Applicant: Pfizer Inc.Inventors: Willard M. Welch, Vinod Parikh
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Publication number: 20030232814Abstract: Compounds of the general formula (I): 1Type: ApplicationFiled: May 16, 2003Publication date: December 18, 2003Inventors: Bjorn M. Nilsson, Erik Ringberg
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Publication number: 20030216387Abstract: The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.Type: ApplicationFiled: April 18, 2003Publication date: November 20, 2003Inventors: Pascal Druzgala, Peter G. Milner, Jurg Pfister, Cyrus Becker
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Publication number: 20030212076Abstract: This invention relates to a compound of the formula (I): 1Type: ApplicationFiled: April 10, 2003Publication date: November 13, 2003Applicant: SmithKline Beecham CorporationInventors: Dirk A. Heerding, James Martin Samanen
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Patent number: 6635649Abstract: Piperazinedione compounds of the formula: Each of and and independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is R3O—(Ar)—B, in which B is CH(Rc) when is a single bond, or C(Rc) when is a double bond; Ar is heteroaryl; and R3 is H, alkyl, aryl, heteroaryl, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; each of R1 and R2, independently, is H, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; and each of Ra, Rb, Rc, Rd, and Re, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl. Optionally, Ra and Rb taken together are cyclyl or heterocyclyl; and, also optionally, R1 and Ra or R1 and Rb taken together are cyclyl or heterocyclyl. Also disclosed is a method for treating tumor with the above described piperazinedione compounds.Type: GrantFiled: May 8, 2001Date of Patent: October 21, 2003Inventors: Che-Ming Teng, Hui-Po Wang, Eric I. C. Li, On Lee, Jih-Hwa Guh, Huei-Ting Chen, Ya-Bing Fan, Ya-Lan Chen
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Publication number: 20030195192Abstract: Compounds having the formula 1Type: ApplicationFiled: April 5, 2002Publication date: October 16, 2003Inventors: Fortuna Haviv, Michael F. Brandley, Jack Henkin
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Publication number: 20030195195Abstract: Compounds having the formula 1Type: ApplicationFiled: September 17, 2002Publication date: October 16, 2003Inventors: Fortuna Haviv, Michael F. Brandley, Jack Henkin, Jurgen Dinges, Daryl R. Sauer
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Publication number: 20030166636Abstract: This invention relates to novel lactams having the formula (I): 1Type: ApplicationFiled: November 4, 2002Publication date: September 4, 2003Inventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
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Publication number: 20030162780Abstract: This invention relates to compounds which are generally muscarinic receptor antagonists and which are represented by Formula I: 1Type: ApplicationFiled: December 2, 2002Publication date: August 28, 2003Inventors: Christine E. Brotherton-Pleiss, Ann Marie Madera, Robert James Weikert
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Patent number: 6608060Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: June 14, 1999Date of Patent: August 19, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, John E. Cochran, Edmund Martin Harrington, Mark A. Murko, Keith P. Wilson, Michael Su, Vincent P. Galullo
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Publication number: 20030130275Abstract: The invention relates to novel sulphonamide compounds having 5-HT7 antagonist activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.Type: ApplicationFiled: November 27, 2002Publication date: July 10, 2003Applicant: SmithKline Beecham p.l.c.Inventor: Peter John Lovell
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Publication number: 20030120070Abstract: The present invention relates to a series of 4-phenylpiperazines of formula (I) 1Type: ApplicationFiled: December 30, 2002Publication date: June 26, 2003Applicant: H. Lundbeck A/SInventors: Jens Kristian Perregaard, Ejner Kund Moltzen
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Patent number: 6559140Abstract: Compounds of formula (I) compounds of formula (II) compounds of formula (III) and compounds of formula (IV) or pharmaceutically acceptable salts thereof are useful as H3 receptor antagonists. Processes to make the compounds and methods of treatment using the compounds are also disclosed.Type: GrantFiled: March 5, 2001Date of Patent: May 6, 2003Assignee: Abbott LaboratoriesInventors: Youssef L. Bennani, Lawrence A. Black, Wesley J. Dwight, Ramin Faghih, Robert G. Gentles, Huaqing Liu, Kathleen M. Phelan, Anil Vasudevan, Henry Q. Zhang
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Publication number: 20030008880Abstract: The present invention relates to compounds of the formula I 1Type: ApplicationFiled: February 13, 2002Publication date: January 9, 2003Applicant: Pfizer Inc.Inventors: Willard M Welch, Vinod Parikh
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Patent number: 6462048Abstract: The present invention relates to lactam derivatives of the formula wherein R1, R2, R3, A, X, Z, n and the dashed line are defined herein, and pharmaceutical compositions thereof, to processes and intermediates for their preparation, and to their medicinal use as selective agonists and antagonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1D receptors. These compounds are useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.Type: GrantFiled: September 24, 1998Date of Patent: October 8, 2002Assignee: Pfizer Inc.Inventor: Harry R. Howard
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Publication number: 20020143011Abstract: Compounds of general formula (1) are described: 1Type: ApplicationFiled: March 14, 2001Publication date: October 3, 2002Applicant: Celltech Therapeutics, LimitedInventors: Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander
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Patent number: 6455528Abstract: The present invention relates to a piperazine compound of the formula wherein R1 and R2 are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4 and R5 are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6 and R7 are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8 and R9 are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds.Type: GrantFiled: April 14, 2000Date of Patent: September 24, 2002Assignee: Mitsubishi Pharma CorporationInventors: Kunitomo Adachi, Yoshiyuki Aoki, Tokushi Hanano, Hiroshi Morimoto, Masao Hisadome
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Patent number: 6432956Abstract: Certain azapirone compounds and their pharmaceutically acceptable salts are useful in the treatment of sleep apneas.Type: GrantFiled: May 3, 1991Date of Patent: August 13, 2002Inventors: William C. Dement, Mark R. Rosekind, Jeffrey L. Schwimmer
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Publication number: 20020107239Abstract: The present invention relates to cyclized amide derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: ApplicationFiled: January 3, 2002Publication date: August 8, 2002Inventors: David Lauffer, Michael Mullican, Brian Ledford
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Patent number: 6420385Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: February 15, 2000Date of Patent: July 16, 2002Assignee: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo, Jeffery A. Zablocki
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Patent number: 6420366Abstract: Novel piperzine derivatives substituted on one nitrogen by an aromatic system and on the other nitrogen by (2,5-dioxopyrrolidin)-1-yl) alkanes or (2,6-dioxopiperidin-1-yl) alkanes have been found to exhibit selective &agr;1A adrenergic activity. The compounds are useful for treatment of disease conditions, such as peripheral vascular disease, congestive heart failure, hypertension and especially benign prostatic hypertrophy.Type: GrantFiled: May 24, 2000Date of Patent: July 16, 2002Assignee: Ranbaxy Laboratories LimitedInventors: Nitya Anand, Neelima Sinha, Sanjay Jain, Anita Mehta, Jang Bahadur Gupta
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Publication number: 20020091122Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.Type: ApplicationFiled: December 6, 2001Publication date: July 11, 2002Applicant: Icagen, Inc.Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
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Patent number: 6387389Abstract: The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.Type: GrantFiled: June 30, 1999Date of Patent: May 14, 2002Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Richard B. Rothman, Kenner C. Rice, David Lewis, Dorota Matecka, John R. Glowa