Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/65)
-
Publication number: 20090023930Abstract: Methods for preparing compound of formula (I) are described, wherein R1-R3 are defined herein, as are methods for preparing the intermediates formed therein. Also described are methods for enantioselectively preparing a chiral compound of the following structure, wherein R2 and R3 are defined herein.Type: ApplicationFiled: July 14, 2008Publication date: January 22, 2009Applicant: WyethInventors: Asaf Alimardanov, Antonia Nikitenko, Gregg Feigelson, John Potoski
-
Publication number: 20090023903Abstract: A novel trifluoroacetylating agent, i.e., N-trifluoroacetylmorpholine, is described. This reagent is useful in the preparation of phenyl and heterocyclic sulfonamide compounds. Methods are therefore described for preparing sulfonamide compounds of the following structure, wherein R1 and R2 are defined herein, using N-trifluoroacetylmorpholine. The sulfonamide compounds that may be prepared as described herein include 5-chloro-thiophene-2-sulfonic acid [(1S,2R)-2-(3,5-difluoro-phenyl)-3,3,3-trifluoro-1-hydroxymethyl-propyl]-amide using N-trifluoroacetylmorpholine.Type: ApplicationFiled: July 14, 2008Publication date: January 22, 2009Applicant: WyethInventors: Terrence Joseph Connolly, Anita Wai-Yin Chan, Zhixian Ding, Mousumi Ghosh, Xinxu Shi, Jianxin Ren, Eric Hansen, Roger Farr, Michael MacEwan, Asaf Alimardanov, Antonia Nikitenko, John Potoski
-
Publication number: 20090018169Abstract: This present invention is related to sulfonamide derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of bacterial infections such as tuberculosis.Type: ApplicationFiled: February 9, 2007Publication date: January 15, 2009Applicant: Laboratoires Serono SAInventors: Jerome Gonzalez, Dominique Swinnen, Agnes Bombrun, Rob Hooft Van Huijsduijnen, Timothy Wells
-
Publication number: 20080312313Abstract: A compound of formula (I), wherein the residues have various meanings, useful as pharmaceuticals.Type: ApplicationFiled: December 22, 2006Publication date: December 18, 2008Inventors: Jose M. Carballido Herrera, Herbert Jaksche, Philipp Lehr, Gudrun Werner, Anthony Winiski
-
Publication number: 20080300295Abstract: Compounds of formula I, wherein one of R1 and R2 is thienyl which is substituted by halogen and the other of R1 and R2 is substituted phenyl, wherein the substituents are as defined in the claims, with the proviso that the phenyl group is substituted by at least a cyano, carboxy or (C1-4)alkyloxycarbonyl group, are inhibitors of CCR9 activity and useful for therapeutic treatment.Type: ApplicationFiled: December 22, 2006Publication date: December 4, 2008Inventors: Jose M. Carballido Herrera, Herbert Jaksche, Philipp Lehr, Gudrun Werner, Anthony Winiski
-
Patent number: 7446213Abstract: Novel methods allowing for the simple optical detection and electrochemical detection of doubled-straded oligonucleotides are disclosed. The methods are rapid, selective and versatile. Advantageously, they do not require any chemical reaction on the probes or on the analytes since they are based on different electrostatic interactions between cationic poly(3-alkoxy-4-methylthiophene) derivatives and single-stranded or doubled-stranded (hybridized) oligonucleotides.Type: GrantFiled: March 7, 2006Date of Patent: November 4, 2008Assignee: Geneohm Sciences Canada, Inc.Inventors: Mario Leclerc, Hoang Anh Ho, Maurice Boissinot
-
Publication number: 20080255169Abstract: The invention relates to sulphonamide derivatives of formula (I), where RC is optionally substituted 4-6-membered heterocyclic ring containing one or more N atoms, or RC forms together with the phenyl ring to which it is attached a benzodioxolyl group, or RC is —NR1R2, RA is a group having the formula RB is hydrogen or alkyl. The invention also relates to the use of derivatives of formula (I) as inhibitors for collagen receptor integrins and a process for preparing sulphonamides of formula (I).Type: ApplicationFiled: July 12, 2004Publication date: October 16, 2008Inventors: David Smith, Anne Marjamaki, Marika Ojala, Marjo Pihlavisto, Jyrki Heino, Jarmo Kapyla, Olli Pentikainen, Tommi Nyronen, Mark Johnson, Mikko Huhtala
-
Publication number: 20080255108Abstract: Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. Said compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug thereof; wherein Ra, Rb, and Rc are defined in the specification, as are A Z, Q, R1 and R2.Type: ApplicationFiled: April 3, 2008Publication date: October 16, 2008Inventors: Nalin L. Subasinghe, Shelley Ballentine, Jeremy M. Travins, Ehab M. Khalil, Farah Ali, Kristi A. Leonard, Joan M. Gushue, Michael Peter Winters, Heather Hufnagel, Maxwell David Cummings
-
Publication number: 20080194597Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 20, 2007Publication date: August 14, 2008Applicant: Portola Pharmaceuticals, Inc.Inventors: ROBERT M. SCARBOROUGH, Wolin Huang, Charles K. Marlowe, Kim A. Kane-Maguire
-
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
-
Publication number: 20080139825Abstract: There is provided a process for efficiently producing an anti form of an optically active ?-hydroxy-?-aminocarboxylic acid derivative that is useful as an intermediate for pharmaceuticals and agrochemicals. The process for producing optically active ?-hydroxy-?-aminocarboxylic acid derivative of formula (2) or (3) therein R1 is substituted or unsubstituted C1-20 alkyl group, or substituted or unsubstituted C4-12 aromatic group, R2 is substituted or unsubstituted C1-20, alkyl group, or substituted or unsubstituted C4-12 aromatic group, comprising subjecting an ?-aminoacyl acetic acid ester compound of formula (1) wherein R1 and R2 have the same meaning as the above, to hydrogenation by catalytic asymmetric hydrogenation in the presence of an acid by using as a catalyst a rhodium complex containing as a ligand an optically active compound of formula (4), (4?) or (5) characterized in that the hydrogenation is conducted in the presence of an acetic acid salt.Type: ApplicationFiled: January 12, 2006Publication date: June 12, 2008Applicant: Nissan Chemical Industrial, Ltd.Inventors: Yasumasa Hamada, Kazuishi Makino
-
Patent number: 7365196Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.Type: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
-
Patent number: 7358375Abstract: Low molecular weight conjugated nitrogen compounds having linear conjugated chains, and devices fabricated using the conjugated nitrogen compounds as organic semiconductor materials, hole conducting materials, or light-emitting materials. The conjugated nitrogen compounds can be spin-coated at room temperature, are stable, and has superior electrical conductivity.Type: GrantFiled: February 7, 2006Date of Patent: April 15, 2008Assignee: Samsung Electronics Co., Ltd.Inventors: Won Cheol Jung, Jean Roncali, Sang Cheol Park, Antonio Cravino, Philippe Leriche, Pierre Frere, Sophie Roquet
-
Patent number: 7351825Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.Type: GrantFiled: December 15, 2004Date of Patent: April 1, 2008Assignee: Japan Tobacco Inc.Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafumi Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
-
Patent number: 7300951Abstract: Compounds of Formula (I), are provided where T is CHO, CON, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y?C, or substituted diene fused to Y when Y?C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.Type: GrantFiled: March 26, 2004Date of Patent: November 27, 2007Assignee: WyethInventors: Anthony Frank Kreft, Lynn Resnick, Scott Christian Mayer, George Diamantidis, Derek Cecil Cole, Boyd Lynn Harrison, Minsheng Zhang, Molly Hoke, Tingzhong Wang, Rocco John Galante
-
Patent number: 7161006Abstract: The invention provides compounds of formula I: which are inhibitors of ?-secretase and hence useful in the treatment or prevention of Alzheimer's disease.Type: GrantFiled: September 25, 2003Date of Patent: January 9, 2007Assignee: Merck Sharp & Dohme LimitedInventors: James Michael Crawforth, Jason Matthew Elliott, Andrew Pate Owens, Francine Sternfeld
-
Patent number: 7138530Abstract: Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula (I) or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.Type: GrantFiled: May 28, 2003Date of Patent: November 21, 2006Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Nalin Subasinghe, Ehab Khalil, Kristi A. Leonard, Farah Ali, Heather Hufnagel, Jeremy M. Travins, Shelley K. Ballentine, Kenneth T. Wilson, Maxwell D. Cummings, Wenxi Pan, Joan Gushue, Sanath Meegalla, Mark Wall, Jinsheng Chen, Jonathan M. Rudolph, Hui Huang
-
Patent number: 7105545Abstract: The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alkyType: GrantFiled: April 2, 2002Date of Patent: September 12, 2006Assignee: Syngenta Crop Protection, Inc.Inventors: Walter Kunz, Clemens Lamberth, Fredrik Cederbaum, Martin Zeller
-
Patent number: 7094911Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: October 31, 2002Date of Patent: August 22, 2006Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
-
Patent number: 7091219Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.Type: GrantFiled: April 17, 2003Date of Patent: August 15, 2006Assignee: G. D. Searle & Co.Inventors: John N. Freskos, Daniel P. Getman, John J. Talley, James A. Sikorski
-
Patent number: 7084170Abstract: The present invention provides antineoplastic compounds of the formula: and antineoplastic methods.Type: GrantFiled: October 15, 2002Date of Patent: August 1, 2006Assignee: Eli Lilly and CompanyInventors: Cora Sue Grossman, Philip Arthur Hipskind, Ho-Shen Lin, Karen Lynn Lobb, Beatriz Lopez de Uralde Garmendia, Jose Eduardo Lopez, Mary Margaret Mader, Michael Enrico Richett, Chuan Shih, Alfonso De Dios
-
Patent number: 7083928Abstract: Novel methods allowing for the simple optical and electrochemical detection of double-stranded oligonucleotides are disclosed. The methods are rapid, selective and versatile. Advantageously, they do not require any chemical reaction on the probes or on the analytes since they are based on different electrostatic interactions between cationic poly (3-alkoxy-4-methylthiophene) derivatives and single-stranded or double-stranded (hibridized) oligonucleotides.Type: GrantFiled: April 5, 2002Date of Patent: August 1, 2006Assignees: Infectio Diagnostic (I.D.I.), Inc., Universite' LavalInventors: Mario Leclerc, Hoang Anh Ho, Maurice Boissinot
-
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
-
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
-
Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
-
Patent number: 7014796Abstract: Nonlinear optically active compounds, methods for making nonlinear optically active compounds, compounds useful for making nonlinear optically active compounds, methods for making compounds useful for making nonlinear optically active compounds, macrostructures that include nonlinear optically active components, and devices including the nonlinear optically active compounds and the macrostructures.Type: GrantFiled: January 15, 2003Date of Patent: March 21, 2006Assignee: University of WashingtonInventors: Kwan-Yue Jen, Hong Ma, Sen Liu, Larry R. Dalton
-
Patent number: 6960688Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.Type: GrantFiled: October 23, 2002Date of Patent: November 1, 2005Assignee: AstraZeneca ABInventors: Roger J Butlin, Thorsten Nowak, Jeremy N Burrows, Michael H Block
-
Patent number: 6949536Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl; halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring. R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4.Type: GrantFiled: February 3, 2004Date of Patent: September 27, 2005Assignee: Pfizer, Inc.Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
-
Patent number: 6949563Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is R2 is and R3 is C0-4alkyl, are useful in the treatment of cancer.Type: GrantFiled: January 6, 2004Date of Patent: September 27, 2005Inventors: Graham Michael Wynne, Kevin Doyle, Saleh Ahmed, An-Hu Li, John Fraser Keily, Chrystelle Marie Rasamison, Neil Anthony Pegg, Imaad Saba, Claire Thomas, Don Smyth, Shazia Sadiq, Gary Newton, Graham Dawson, Andrew Phillip Crew, Arlindo Lucas Castelhano
-
Patent number: 6927224Abstract: The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for the treatment and/or prevention of estrogen stimulated diseases in mammals including breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.Type: GrantFiled: August 9, 2002Date of Patent: August 9, 2005Assignee: Bristol Myers Squibb CompanyInventors: Robert F. Kaltenbach, Simon P. Robinson, George L. Trainor
-
Patent number: 6919369Abstract: Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: August 19, 2002Date of Patent: July 19, 2005Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
-
Patent number: 6916837Abstract: Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 aryl, etc. and R2 represents hydrogen atom, etc.), etc., Ar1 represents 2,6-naphthylene, etc., R3 represents hydrogen atom, etc. and Y represents carboxyphenyl, etc.} and their pharmacologically acceptable salts or solvates.Type: GrantFiled: November 14, 2002Date of Patent: July 12, 2005Assignee: Eisai Co., Ltd.Inventors: Takashi Satoh, Yasushi Okamoto, Osamu Asano, Nobuhisa Watanabe, Tadashi Nagakura, Takao Saeki, Atsushi Inoue, Masahiro Sakurai
-
Patent number: 6903216Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them. Compounds of formula I, in which R1 to R7 have the meanings stated in the claims, act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. They are therefore suitable as novel antiarrhythmic ingredients, such as for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutter.Type: GrantFiled: June 12, 2002Date of Patent: June 7, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Thomas Böhme, Stefan Peukert, Heinz-Werner Kleemann
-
Patent number: 6890942Abstract: The present invention relates a series of compounds of Formula I wherein R1, R2, R3, and B are as defined in the specification. The compounds are useful for the inhibition of HIV integrase and for the treatment of AIDS or ARC by administering compounds of the formula.Type: GrantFiled: May 5, 2004Date of Patent: May 10, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Hatice Belgin Gulgeze, Jacques Banville, Roger Remillard, Donald Corson
-
Patent number: 6878742Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof.Type: GrantFiled: June 5, 2003Date of Patent: April 12, 2005Assignees: Wyeth, ArQule, Inc.Inventors: Anthony F. Kreft, Derek C. Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
-
Patent number: 6878723Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.Type: GrantFiled: April 6, 2000Date of Patent: April 12, 2005Assignees: Institut National de la Sante et de la rescherche Medicale (INSERM), BioprojetInventors: Denis Danvy, Thierry Monteil, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Nadine Noel, Claude Gros, Olivier Chamard, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Serge Piettre
-
Patent number: 6849635Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.Type: GrantFiled: May 7, 2002Date of Patent: February 1, 2005Assignee: SmithKline Beecham CorporationInventors: Dashyant Dhanak, Timothy F. Gallagher, Steven D. Knight, Stanley J. Schmidt
-
Patent number: 6849660Abstract: Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1? is —C(O)NR5R5?, —C(O)—Q—NR5R5?, —CH2NR5R5? or —S(O)2NR5R5? and the other is H or R3. One of R2 and R2? is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5? or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5? is H or R5 and R5? together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide.Type: GrantFiled: August 1, 2000Date of Patent: February 1, 2005Assignee: ISIS Pharmaceuticals, Inc.Inventors: Elizabeth Jefferson, Eric Swayze
-
Patent number: 6800764Abstract: A process is provided for preparing chirally pure S-enantiomers of &agr;-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an &agr;-azido acid; h) reducing the &agr;-azido acid to the &agr;-amino acid; and i) recrystallizing the &agr;-amino acid to the chirally pure &agr;-amino acid.Type: GrantFiled: November 26, 2002Date of Patent: October 5, 2004Assignee: WyethInventors: Anthony Frank Kreft, Madelene Miyoko Antane, Derek Cecil Cole, Dennis Martin Kubrak, Lynn Resnick, Joseph Raymond Stock, Zheng Wang
-
Publication number: 20040186124Abstract: Compounds represented by Formula (I): 1Type: ApplicationFiled: January 6, 2004Publication date: September 23, 2004Inventors: Graham Michael Wynne, Kevin Doyle, Saleh Ahmed, An-Hu Li, John Fraser Keily, Chrystelle Marie Rasamison, Neil Anthony Pegg, Imaad Saba, Claire Thomas, Don Smyth, Shazia Sadiq, Gary Newton, Graham Dawson, Andrew Phillip Crew, Arlindo Lucas Castelhano
-
Publication number: 20040171616Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: February 19, 2003Publication date: September 2, 2004Inventors: Michael S. South, John J. Parlow
-
Patent number: 6768024Abstract: The invention provides triamine derivative melanocortin receptor ligands of the formula: wherein R1 to R8 and n have the meanings provided herein. The invention further provides methods of using the ligands to alter or regulate the activity of a melanocortin receptor.Type: GrantFiled: August 4, 2000Date of Patent: July 27, 2004Assignee: Lion Bioscience AGInventors: Karen J. Watson-Straughan, Timothy C. Gahman, Ming Qi, Christa Hamashin, James E. Macdonald, Michael J. Green, Kevin R. Holme, Michael C. Griffith
-
Publication number: 20040110804Abstract: The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds.Type: ApplicationFiled: July 9, 2003Publication date: June 10, 2004Inventors: Michael A. Walker, Zhuping Ma, B. Narasimhulu Naidu, Margaret E. Sorenson, Annapurna Pendri, Jacques Banville, Serge Plamondon, Roger Remillard
-
Patent number: 6743929Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 6, 2000Date of Patent: June 1, 2004Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
-
Patent number: 6734207Abstract: Compounds are described that bind to tubulin causing tubulin depolymerization and inhibiting tubulin polymerization. The compounds of the invention are therapeutically effective to inhibit cellular proliferation, for example, as effective anti-cancer agents. The compounds can also induce cytotoxicity in cells such as leukemia cells. The chemical structure of the compounds includes a furan, thiophene, thiazole, oxazole, or imidazole group at one end of the molecule (head) and a hydrophobic, aliphatic chain at the other end of the molecule (tail).Type: GrantFiled: April 18, 2002Date of Patent: May 11, 2004Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Shyi-Tai M. Jan
-
Patent number: 6727238Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 oType: GrantFiled: June 18, 2003Date of Patent: April 27, 2004Assignee: Pfizer Inc.Inventors: Kazuo Ando, Tomoki Kato, Akiyoshi Kawai, Tomomi Nonomura
-
Patent number: 6716995Abstract: In various embodiments, chromophores are described that include novel electron acceptors, novel electron donors, and/or novel conjugated bridges that are useful in nonlinear optical applications. In some embodiments, the present invention provides chromophore architectures wherein a chromophore contains more than one electron acceptor in electronic communication with a single electron donor, and/or more than one electron donor in electronic communication with a single electron acceptor. Also described is processes for providing materials comprising the novel chromophores and polymer matrices containing the novel chromophores. Electro-optic devices described herein contain one or more of the described electron acceptors, electron donors, conjugated bridges, or chromophores.Type: GrantFiled: August 17, 2001Date of Patent: April 6, 2004Assignee: Lumera CorporationInventors: Diyun Huang, Tim Londergan, Galina K. Todorova, Jingsong Zhu
-
Patent number: 6706755Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein a hatched line represents the &agr; configuration, a triangle represents the &bgr; configuration, a straight line, e.g.Type: GrantFiled: August 26, 2002Date of Patent: March 16, 2004Assignee: Allergan, Inc.Inventors: David W. Old, Robert M. Burk
-
Publication number: 20040030156Abstract: Compounds of formula I, or a pharmaceutically acceptable salt thereof, 1Type: ApplicationFiled: May 30, 2003Publication date: February 12, 2004Applicant: Gruenenthal GmbHInventors: Corinna Maul, Werner Englberger, Michael Przewosny
-
Patent number: RE39530Abstract: 3-amino-3-arylpropan-1-ol compounds corresponding to the formula I in which R1 to R5, A and X have the meanings according to claim 1, and their preparation and use as medicaments.Type: GrantFiled: September 11, 2003Date of Patent: March 27, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Helmut Buschmann