Nitrogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/561)
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Publication number: 20080171886Abstract: A plug-in Wi-Fi access point device and system is provided that is configured for Wi-Fi or other wireless network and to be directly plugged into a face plate/workstation. The plug-in Wi-Fi access point device and system advantageously provides ease of integration into an existing wired network without the use of a patch cord, security from removal by unauthorized personnel, non obtrusiveness in relation to other face plate/workstation jacks, and the ability to be powered through an Ethernet connection to avoid the need for a separate power source. Furthermore, the plug-in Wi-Fi access point device and system may beneficially permit the integration of complementary connections within the access point including, for example, data, voice, and video connection types.Type: ApplicationFiled: January 3, 2006Publication date: July 17, 2008Inventors: Benjamin Simon Davies, Alastair Alexander Denholm, Patrick Gerard Thomas Kelleher, William Eugene Tully
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Patent number: 7399870Abstract: The instant invention concerns processes for the production of pyrrole-2-carbonitriles such as 1-methylpyrrole-2-carbonitrile. Such processes preferably comprise the steps of reacting a pyrrole with chlorosulfonyl isocyanate in the presence of a solvent and contacting the resulting product with a molar excess of an amide such as N,N-dimethylformamide. The product of this contacting step is then contacted with a molar excess of an organic base to produce a precipitate and a solution phase. The precipitate is then separated from the solution phase and the corresponding pyrrole-2-carbonitrile is isolated from the resulting solution phase.Type: GrantFiled: March 22, 2005Date of Patent: July 15, 2008Assignee: WyethInventors: Jean Louise Helom, Arkadiy Zinoviy Rubezhov, Anthony Scott Pilcher, Bogdan Kazimierz Wilk
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Publication number: 20080167468Abstract: The present invention relates to a diastereomeric mixture of Silacycle Compounds and methods for using the diastereomeric mixture of Silacycle Compounds for stereoselective synthesis.Type: ApplicationFiled: June 6, 2007Publication date: July 10, 2008Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: James Lincoln Leighton, Richard Berger, Seiji Shirakawa, Gregory T. Notte
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Patent number: 7381842Abstract: Compounds of the formulae I, II, III, IV and V wherein R1 i.a. is C4-C9cycloalkanoyl, C1-C12alkanoyl, C4-C6alkenoyl, or benzoyl; R2 is for example phenyl, C1-C20alkyl, C3-C8cycloalkyl, C2-C20alkanoyl, or benzoyl; Ar1 is R4S-phenyl or NR5R6-phenyl, each of which optionally is substituted; or Ar1 i.a. is optionally substituted; or Ar1 is naphthyl or anthracyl each of which is unsubstituted or substituted; or Ar1 is benzoyl, naphthalenecarbonyl, phenanthrenecarbonyl, anthracenecarbonyl or pyrenecarbonyl, each of which is unsubstituted or substituted, or Ar1 is 3,4,5-trimethoxyphenyl, phenoxyphenyl or biphenyl; Ar2 i.a.Type: GrantFiled: April 11, 2005Date of Patent: June 3, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Kazuhiko Kunimoto, Hidetaka Oka, Masaki Ohwa, Junichi Tanabe, Hisatoshi Kura, Jean-Luc Birbaum
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Publication number: 20080119658Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: ApplicationFiled: October 31, 2007Publication date: May 22, 2008Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Publication number: 20080114036Abstract: Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hyper triglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.Type: ApplicationFiled: May 3, 2005Publication date: May 15, 2008Applicant: Novo Nordisk A/SInventors: Miroslav Havranek, Per Sauerberg, Ingrid Pettersson
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Publication number: 20080114037Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with HDAC that comprise a compound selected from the group consisting of: wherein the substituents are as defined herein.Type: ApplicationFiled: October 31, 2007Publication date: May 15, 2008Inventors: Jerome C. Bressi, Anthony R. Gangloff, Lily Kwok
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Publication number: 20080113976Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.Type: ApplicationFiled: November 28, 2007Publication date: May 15, 2008Inventor: Percy H. Carter
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Patent number: 7361769Abstract: The present invention discloses compounds of formula I wherein m, n, p, R1, R2 and X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: GrantFiled: July 14, 2005Date of Patent: April 22, 2008Assignee: Schering CorporationInventors: Jing Su, Brian A. McKittrick, Haiqun Tang, Thavalakulamgara K. Sasikumar, Li Qiang
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Patent number: 7326812Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.Type: GrantFiled: January 17, 2006Date of Patent: February 5, 2008Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7323490Abstract: The invention provides pyrrole-containing compounds and methods of use thereof. Kits and pharmaceutical compositions comprising the pyrrole compounds of the invention are also provided. The compounds and compositions disclosed herein are preferably used in the treatment of neurodegenerative diseases, cardiovascular diseases, proliferative diseases, and visual disorders. In particular, methods and compositions for the treatment of stroke are disclosed herein.Type: GrantFiled: May 17, 2004Date of Patent: January 29, 2008Assignee: Ambit Biosciences CorporationInventors: David J. Lockhart, Hitesh K. Patel, Zdravko V. Milanov, Shamal Anil Mehta, Patrick Parvis Zarrinkar, William H. Biggs, III, Pietro Ciceri, Miles A. Fabian, Daniel K. Treiber
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Patent number: 7323491Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them This invention also relates to the process for preparing such compounds, a composition containing such a compound and the use of such a compound and composition in medicine.Type: GrantFiled: March 1, 2004Date of Patent: January 29, 2008Assignee: Cadila Healthcare LimitedInventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
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Patent number: 7297713Abstract: Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein. These compounds are useful for contraception and hormone replacement therapy. Also provided are products containing these compounds.Type: GrantFiled: July 27, 2006Date of Patent: November 20, 2007Assignee: WyethInventors: Casey Cameron McComas, Andrew Fensome, Edward George Melenski
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Patent number: 7291643Abstract: Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, are useful for contraception and hormone replacement therapy are described. Also provided are products containing these compounds.Type: GrantFiled: July 27, 2006Date of Patent: November 6, 2007Assignee: WyethInventors: Casey Cameron McComas, Andrew Fensome, Edward George Melenski
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Publication number: 20070232581Abstract: There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 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: March 29, 2007Publication date: October 4, 2007Inventors: Yong-Jin Wu, Samuel Gerritz, Shuhao Shi, Shirong Zhu
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Patent number: 7229991Abstract: 5-aminomethyl-1H-pyrrole-2-carboxylic acid amide compounds corresponding to formula I and processes for the production thereof. Pharmaceutical preparations containing these compounds and the use of these compounds for the production of pharmaceutical preparations and in related treatment methods.Type: GrantFiled: June 20, 2005Date of Patent: June 12, 2007Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Corinna Sundermann, Utz-Peter Jagusch, Werner Englberger, Hagen-Heinrich Hennies, Babette-Yvonne Kögel
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Patent number: 7217707Abstract: N-(2-aminoaryl-propionyl)-amides of formula (1) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear neutrophils (leukocytes PMN) at the inflammatory sites. In particular, the invention relates to the R enantiomers of 2-(aminoaryl)-propionyl amides of formula (1) for use in the ihibition of the chemotaxis of neutrophils induced by IL-8. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, and rheumatoid arthritis.Type: GrantFiled: April 11, 2001Date of Patent: May 15, 2007Assignee: Dompe S.p.A.Inventors: Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Vilma Sabbatini, Ginfranco Caselli, Maria Candida Cesta, Janete Peloia Barroso Gandolfi, legal representative, Giulio Agostino Gandolfi, legal representative, Maria Carla Gandolfi, legal representative, Arrigo Aldo Gandolfi, legal representative, Francesco Colotta, Carmelo Gandolfi, deceased
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Patent number: 7186748Abstract: The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH2)n where n is 0, 1 or 2; R1, R2, R3, R4 and R5 may be the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, alkylsulphonyloxy, cyano, nitro, trihaloalkyl, sulpho or one of the structures given in Scheme 1; or two of R1, R2, R3, R4 and R5 may together form a methylenedioxy or ethylenedioxy moiety; R6, R7, R8 and R9 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, alkoxy having 1 to 5 carbon atoms, hydroxy, amines (primary, secondary or tertiary) having 0, 1 or 2 carbon atoms, cyano, nitro, trihaloalkyl, amide or sulpho, and z where shown represents the point of attachment of the residue to the phenyl or pyrrole ring; and the pharmacologically active salts thereof.Type: GrantFiled: August 6, 2002Date of Patent: March 6, 2007Assignee: Action Pharma A/SInventors: Torbjörn Lundstedt, Anna Skottner, Arne Boman, Per Andersson, Elisabeth Seifert, Victor Andrianov
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Patent number: 7179825Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; or R1 and R2 taken together may form a bivalent radical of formula —(CH2)n— wherein n is 2, 3, 4, 5 or 6; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or —NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aType: GrantFiled: March 16, 2005Date of Patent: February 20, 2007Assignee: Janssen Pharmaceutica N.V.Inventors: Dominique Mabire, Christophe Denis Adelinet, Imré Christian Csoka, Marc Gaston Venet
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Patent number: 7153881Abstract: The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH2)n, where n is 0, 1, 2, 3, 4, or 5, or a combination of these and may contain carbon-carbon multiple bonds and branched chains as well as alicyclic and heterocyclic groups; Q is H or OH; R1 and R2 can be either the same or different and are chosen from hydrogen or the residue of an aromatic group as listed in Scheme 1 and the pharmacologically active salts thereofType: GrantFiled: August 7, 2001Date of Patent: December 26, 2006Assignee: Acure Pharma ABInventors: Torbjörn Lundstedt, Anna Skottner, Arne Boman, Per Andersson, Victor Andrianov, Ivars Kalvins
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Patent number: 7112606Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.Type: GrantFiled: January 29, 2003Date of Patent: September 26, 2006Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, David J. Kopecky, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7071358Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.Type: GrantFiled: January 29, 2003Date of Patent: July 4, 2006Assignee: Amgen Inc.Inventors: Xian Yun Jiao, Frank Kayser, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
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Patent number: 7071338Abstract: Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl] furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.Type: GrantFiled: November 25, 2003Date of Patent: July 4, 2006Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: David W. Boykin, Mariappan Anbazhagan, Richard R. Tidwell
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Patent number: 7030239Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: May 18, 2004Date of Patent: April 18, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Patent number: 7026339Abstract: The present invention relates to compounds, process for their synthesis, compositions and methods for the treatment and prevention of hepatitis C virus (HCV) infection. In particular, the present invention provides novel compounds, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment or prevention of HCV infection. The present invention also provides processes and intermediates for the synthesis of these compounds.Type: GrantFiled: November 3, 2004Date of Patent: April 11, 2006Inventors: Fan Yang, Bo Zhang, Nancy Anne Wicnienski, Jeffrey Allen Pfefferkorn, Meredith L. Greene, Ke Chen, Richard A. Nugent, Matthew Todd Reding, Robert Charles Kelly, Mark A. Mitchell, Lee A. Funk, Richard Frederick Heier, III, Rebecca Merry Anderson
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Patent number: 6949678Abstract: Compounds of the formulae I, II, III, IV and V wherein R1 i.a. is C4-C9cycloalkanoyl, C1-C12alkanoyl, C4-C6alkenoyl, or benzoyl; R2 is for example phenyl, C1-C20alkyl, C3-C8cycloalkyl, C2-C20alkanoyl, or benzoyl; Ar1 is R4S-phenyl or NR5R6-phenyl, each of which optionally is substituted; or Ar1 i.a. is optionally substituted; or Ar1 is naphthyl or anthracyl each of which is unsubstituted or substituted; or Ar1 is benzoyl, naphthalenecarbonyl, phenanthrenecarbonyl, anthracenecarbonyl or pyrenecarbonyl, each of which is unsubstituted or substituted, or Ar1 is 3,4,5-trimethoxyphenyl, phenoxyphenyl or biphenyl; Ar2 i.a.Type: GrantFiled: December 12, 2000Date of Patent: September 27, 2005Assignee: Ciba Specialty Chemicals Corp.Inventors: Kazuhiko Kunimoto, Hidetaka Oka, Masaki Ohwa, Junichi Tanabe, Hisatoshi Kura, Jean-Luc Birbaum
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Patent number: 6936719Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.Type: GrantFiled: December 18, 2003Date of Patent: August 30, 2005Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, R. Scott Rowland, Pooran Chand, Pravin L. Kotian, Yahya El-Kattan, Shri Niwas
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Patent number: 6858637Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: GrantFiled: March 27, 2003Date of Patent: February 22, 2005Assignee: Neurogen CorporationInventors: Yang Gao, Alan J. Hutchison, Wallace C. Pringle, Andrew Thurkauf, Taeyoung Yoon, He Zhao
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Patent number: 6803472Abstract: A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitrites or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.Type: GrantFiled: November 29, 2002Date of Patent: October 12, 2004Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Takashi Emura, Tsuyoshi Haneishi
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Publication number: 20040186099Abstract: The present invention relates to novel substituted pyrrole compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel substituted pyrrole compounds of the general formula (I), their analogs, their derivatives, their polymorphs, their tautomeric forms, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them.Type: ApplicationFiled: March 1, 2004Publication date: September 23, 2004Inventors: Braj Bhushan Lohray, Vidya Bhushan Lohray, Vijay Kumar Gajubhai Barot
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Publication number: 20040171641Abstract: Arylpiperazines of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: ApplicationFiled: February 26, 2004Publication date: September 2, 2004Applicant: AstraZeneca ABInventors: Bernard C. Barlaam, Nicholas J. Newcombe, Howard Tucker, David Waterson
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Publication number: 20040171654Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: November 17, 2003Publication date: September 2, 2004Inventors: Solomon Ugashe, Zheng Wei, J. J. Wright, Andrew Pennell
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Patent number: 6737420Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII): useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: March 23, 2001Date of Patent: May 18, 2004Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Patent number: 6730783Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: April 22, 2003Date of Patent: May 4, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
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Publication number: 20040063643Abstract: Compounds of formula (I): 1Type: ApplicationFiled: April 28, 2003Publication date: April 1, 2004Applicant: Pfizer Inc.Inventors: Michael Higginbottom, Suzanne Ross Kesten, Russell Andrew Lewthwaite, Martyn Clive Pritchard, David James Rawson, Robert Michael Schelkun, Po-Wai Yuen
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Publication number: 20040049049Abstract: A stereoselectively method of preparing a 1,2-disubstituted cycloalkyl, such as aminocycloalkyl ether compounds, from a trans-1,2-disubstituted cycloalkyl or a cis-2-substituted cycloalkanol. For example, a stereoselective method of preparing 1R-(3R-hydroxypyrrolidin-1-yl)-2R-(2-phenylethoxy)-cyclohexane from 1R,2R-cyclohexanediol or from meso-cis-1,2-cyclohexanediol is described. Aminocycloalkyl ethers, such as 1R-(3R-hydroxypyrrolidin-1-yl)-2R-(2-phenylethoxy)-cyclohexane, can be used to treat cardiac disease.Type: ApplicationFiled: June 10, 2003Publication date: March 11, 2004Applicant: Johnson Matthey Pharmaceutical Materials, Inc.Inventors: Jurjus F. Jurayj, Emile Farhan, Pradeep K. Sharma
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Publication number: 20040048907Abstract: One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke.Type: ApplicationFiled: May 15, 2003Publication date: March 11, 2004Inventors: Brian M. Aquila, Seth C. Hopkins, Curtis A. Lockshin, Fengjiang Wang
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Publication number: 20040048895Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: 1Type: ApplicationFiled: June 5, 2003Publication date: March 11, 2004Inventors: Darin Allen, Bruce Fahr, Johan Oslob, Brian C. Raimundo, Michael J. Romanowski
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Publication number: 20040039025Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.Type: ApplicationFiled: August 28, 2003Publication date: February 26, 2004Inventors: Syed M. Ali, Kurt R. Brunden, Dario Doller, Brian Herbert, Jack B. Jiang, Amy Jordan
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Patent number: 6689174Abstract: Dyes, containing N-benzyl-p-phenylenediamine derivatives of the general formula (I) or their physiologically compatible salts, for keratin fibers, and new N-benzyl-p-phenylenediamine derivatives.Type: GrantFiled: January 1, 2002Date of Patent: February 10, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6677341Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6677353Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6649629Abstract: The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or optionally, at least one therapeutic agent, such as, steroids, nonsteroidal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhType: GrantFiled: December 22, 2000Date of Patent: November 18, 2003Assignee: Nitromed, Inc.Inventors: Upul K. Bandarage, Xinqin Fang, David S. Garvey, L. Gordon Letts, Joseph D. Schroeder, Sang William Tam
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Patent number: 6646009Abstract: N-(Aryl)-2-arylethenesulfonamides and pharmaceutically acceptable salts and compositions thereof are useful as antiproliferative agents, including, for example, anticancer agents. They are also useful as radioprotective agents.Type: GrantFiled: February 28, 2002Date of Patent: November 11, 2003Assignees: Temple University — Of Commonwealth System of Higher Education, Onconova Therapeutics, Inc.Inventors: E. Premkumar Reddy, M.V. Ramana Reddy, Stanley C. Bell
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Patent number: 6642392Abstract: Compounds of Formula I are disclosed which are useful as fungicides wherein X is —O—, —CH(R11)— or ═C(R11)—; R1 is H or C1-C2 alkyl; R2 is H; C1-C6 alkyl; C3-C6 cycloalkyl; or phenyl optionally substituted with halogen, cyano, C1-C2 alkyl or C1-C2 alkoxy; and R3-R11 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.Type: GrantFiled: March 2, 2001Date of Patent: November 4, 2003Assignee: Board of Trustees of the University of ArkansasInventors: Gregory Steven Basarab, Douglas Brian Jordan, Thomas Arend Lessen, Stephen L. Hansen
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Patent number: 6638931Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 28, 2000Date of Patent: October 28, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Patent number: 6632840Abstract: Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) isType: GrantFiled: March 24, 2000Date of Patent: October 14, 2003Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
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Publication number: 20030180804Abstract: The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.Type: ApplicationFiled: October 29, 2002Publication date: September 25, 2003Applicant: Corvas International, IncInventors: Kent E. Pryor, Ronald D. Lewis, Jason W. Brown
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Publication number: 20030171411Abstract: This invention relates to compounds of the general formula 1Type: ApplicationFiled: December 19, 2002Publication date: September 11, 2003Inventors: Janos Tibor Kodra, Jesper Lau, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M. M. Mjalli, Robert Carl Andrews, Dharma Rao Polisetti
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Patent number: 6613915Abstract: Selected olefins such as ethylene and &agr;-olefins are polymerized by nickel [II] complexes of certain monoanionic ligands. The polyolefins are useful in many applications such as molding resins, film, fibers and others. Also described are many novel nickel compounds and their precursors, as well a novel ligands.Type: GrantFiled: October 13, 1999Date of Patent: September 2, 2003Assignee: E. I. du Pont de Nemours and CompanyInventors: Lynda Kaye Johnson, Alison Margaret Anne Bennett, Lin Wang, Anju Parthasarathy, Elisabeth Hauptman, Robert D. Simpson, Jerald Feldman, Edward Bryan Coughlin, Steven Dale Ittel