Chalcogen Attached Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 544/398)
-
Patent number: 7268140Abstract: This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.Type: GrantFiled: October 13, 2005Date of Patent: September 11, 2007Assignee: Schering AGInventors: John G. Bauman, Brad O. Buckman, Ameen F. Ghannam, Joseph E. Hesselgesser, Richard Horuk, Imadul Islam, Meina Liang, Karen B. May, Sean D. Monahan, Michael M. Morrissey, Howard P. Ng, Kenneth J. Shaw, Guo Ping Wei, Wei Xu, Zuchun Zhao, Wei Zheng
-
Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
-
Patent number: 7135473Abstract: A cyclic diamine compound of formula (1): wherein R1 and R2 are individually a hydrogen atom or a methoxy group, provided R1 is a methoxy group when R2 is a hydrogen atom, or a hydrogen atom when R2 is a methoxy group; A is an oxygen atom, a sulfur atom, CH?CH, CH?N or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; B is a nitrogen atom, CH or CR4, in which R4 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; m is 1 or 2; and n is a number of 1 to 5, an acid-addition salt thereof, or a hydrate thereof. The compound has inhibitory effects on cell adhesion and is useful for treatment of allergy, asthma, rheumatism, arteriosclerosis, and inflammation.Type: GrantFiled: August 13, 2003Date of Patent: November 14, 2006Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Takeshi Doi, Yoshinori Kyotani
-
Patent number: 7122294Abstract: Photoacid generators (PAGs) comprising photoactive moieties and perfluorinated, multifunctional anionic moieties (or incipient anionic moieties) are disclosed which provide photoacids with high acid strength, low volatility and low diffusivity. The present invention further relates to photoacid generators as they are used in photoinitiated or acid-catalyzed processes for uses such as photoresists for microlithography and photopolymerization.Type: GrantFiled: May 22, 2003Date of Patent: October 17, 2006Assignee: 3M Innovative Properties CompanyInventor: William M. Lamanna
-
Patent number: 7115610Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: GrantFiled: December 17, 2004Date of Patent: October 3, 2006Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffrey Zablocki
-
Patent number: 7074820Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: April 23, 2001Date of Patent: July 11, 2006Assignee: AstraZeneca ABInventor: Thomas Antonsson
-
Patent number: 7049306Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: September 20, 2002Date of Patent: May 23, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
-
Patent number: 7019007Abstract: The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: November 27, 2002Date of Patent: March 28, 2006Assignee: Syntex (U.S.A.) LLCInventors: Daisy Joe Du Bois, Beihan Wang
-
Patent number: 6919482Abstract: Disclosed are multibinding compounds which are ?2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: January 30, 2004Date of Patent: July 19, 2005Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
-
Patent number: 6916797Abstract: The invention relates to new ?-arylethylpiperazine of the formula wherein Z represents 0 or S; n? represents 1 or 2; R2 represents a hydrogen atom or a methyl group; W, Ar1 and Ar2 represent various substituents as defined herein; or non-toxic pharmaceutically acceptable salt, individual optical isomer, or individual diastereoisomer thereof, which are useful as neurokinin receptor antagonists (NK1 antagonists). It also relates to processes for their preparation and use in methods for treatment of asthma and/or allergic rhinitis.Type: GrantFiled: December 14, 2000Date of Patent: July 12, 2005Assignee: UCB, S.A.Inventors: Françoise Stiernet, Christophe Genicot, Marie-Agnes Lassoie, Florence Moureau, Thomas Ryckmans, Thierry Taverne, Jean-Pierre Henichart, Michel Neuwels, Solo Goldstein
-
Patent number: 6900350Abstract: The invention relates to a method for the production of ?-aminoalkylsulphonic acids of general formula (I), where R1 and R2=optionally substituted alkyl groups with 1 20 C atoms and n=a whole number from 2 6, whereby an amine of formula (II), where R1 and R2 have the above meanings is reacted with an alkyl dihalide of formula (III), where n has the above meaning and X1 and X2=chlorine or bromine, with addition of alkali hydroxide at a pH of 8 10. The pH is then adjusted to a value of 0 1, by addition of a hydrohalic acid and excess alkyl dihalide is separated off, before the reaction solution is adjusted to a pH of 6 7.5 with alkali liquor, alkali sulphite is added and the product (I) formed at elevated temperate.Type: GrantFiled: April 27, 2001Date of Patent: May 31, 2005Assignee: RASCHIG GmbHInventors: Volker Schaefer, Wolfgang Knoll, Alexander Schmitt, Christoph Huettner
-
Patent number: 6900243Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: GrantFiled: February 20, 2001Date of Patent: May 31, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Antonio Mete
-
Patent number: 6887885Abstract: A compound of formula I, or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions including the compound and methods for treating anxiety, convulsions and cognitive disorders are disclosed.Type: GrantFiled: October 30, 2003Date of Patent: May 3, 2005Assignee: Merck Sharp & Dohme LtdInventor: Simon Charles Goodacre
-
Patent number: 6884803Abstract: Disclosed are substituted phenylalkynes of formula (I), wherein R1, R2, R3, R4, R5 and n are as defined, compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: December 2, 2002Date of Patent: April 26, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard Apodaca, Wei Xiao, Jill A. Jablonowski
-
Patent number: 6846813Abstract: The present invention is disubstituted amines of formula (I) and disubstituted amines of formula (II) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: June 29, 2001Date of Patent: January 25, 2005Assignees: Pharmacia & Upjohn Company, Elan Pharmaceuticals, Inc.Inventors: James P. Beck, Andrea Gailunas, Roy Hom, Barbara Jagodzinska, Varghese John, Michel Maillard
-
Patent number: 6844366Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: October 9, 2002Date of Patent: January 18, 2005Assignee: Syntex (U.S.A.) LLCInventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
-
Publication number: 20040254375Abstract: The present invention relates to a process for the manufacture of 2-{2-[4-(bis(4-fluorophenyl)methyl)-1-piperazinyl]ethoxy}acetic acids, amides or related derivatives, of the general formula (I) wherein: Y represents hydroxy or —NR1R2; R1 and R2 each independently represent hydrogen or C?1-4#191 alkyl; m is 1 or 2, and n is 1 or 2, as well as the non-toxic, pharmaceutically acceptable salts and mixtures thereof. The present invention concerns also a polymorphic form of efletirizine.Type: ApplicationFiled: January 26, 2004Publication date: December 16, 2004Inventors: Ousmane Diouf, John Surtees
-
Publication number: 20040236104Abstract: Substituted 4-aminocyclohexanols, methods of producing the same, pharmaceuticals containing these compounds, the use of substituted 4-aminocyclohexanols for producing pharmaceutical compositions for the treatment of various indications, in particular pain, and for related treatment methods.Type: ApplicationFiled: January 16, 2004Publication date: November 25, 2004Applicant: Gruenenthal GmbhInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Werner Englberger, Stephan Wnendt
-
Publication number: 20040235832Abstract: One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.Type: ApplicationFiled: January 28, 2004Publication date: November 25, 2004Inventors: Xinhe Wu, Brian M. Aquila, Liming Shao, Heike Radeke, Gregory D. Cuny, James R. Hauske, Roger L. Xie
-
Publication number: 20040214822Abstract: 4-aminocyclohexanol compounds, processes for their preparation, pharmaceutical formulations comprising these compounds and the use of substituted 4-aminocyclohexanol compounds for the preparation of pharmaceutical formulations and for the treatment of diverse indications, including, without limitation, pain.Type: ApplicationFiled: January 16, 2004Publication date: October 28, 2004Applicant: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Stephan Wnendt
-
Publication number: 20040192688Abstract: This invention relates to novel {overscore (&ohgr;)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.Type: ApplicationFiled: October 27, 2003Publication date: September 30, 2004Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Devdutt Chaturvedi, Atul Kumar, Reema Rastogi, Arvind Srivastava, Priti Tewari, Rehan Ahmad, Ramesh Chander, Anju Puri, Geetika Bhatia, Farhan Rizvi, Anil Kumar Rastogi, Suprabhat Ray
-
Patent number: 6747027Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.Type: GrantFiled: July 22, 1997Date of Patent: June 8, 2004Assignee: Pharmacia CorporationInventors: Gary DeCrescenzo, Zaheer S. Abbas, John N. Freskos, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
-
Publication number: 20040058916Abstract: A compound having general formula 1Type: ApplicationFiled: June 11, 2003Publication date: March 25, 2004Inventor: Ashokkumar Bhikkappa Shenvi
-
Patent number: 6706745Abstract: The present invention relates to a biphenylamidine derivative of the general formula (1): or a pharmaceutically acceptable salt thereof, which is a novel compound functioning as a clinically applicable FXa inhibitor.Type: GrantFiled: May 18, 2000Date of Patent: March 16, 2004Assignee: Teijin LimitedInventors: Takayuki Hara, Tomohisa Nakada, Yasunobu Takano, Satoshi Sugiura, Takaharu Tsutsumi, Yoshiharu Takazawa, Reiko Takarada
-
Patent number: 6703425Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disordersType: GrantFiled: November 15, 2002Date of Patent: March 9, 2004Assignee: Eli Lilly and CompanyInventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
-
Publication number: 20040044208Abstract: This invention relates to high purity hydrogen ion buffers and in particular amino-organosulfonic acid zwitterionic compositions having low metal content. The concentration of any single metal in the composition is no greater than about 500 ppb, and ideally is less than about 20 ppb.Type: ApplicationFiled: August 29, 2002Publication date: March 4, 2004Applicant: Buffers & Biochemicals CorporationInventors: David Bow, Glenn Thomas Carroll
-
Publication number: 20040034031Abstract: The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.Type: ApplicationFiled: November 19, 2002Publication date: February 19, 2004Inventors: Joseph B. Moon, Shon R. Pulley, Daniel H. Rich, David L. Brown, Barbara Jagodzinska, Varghese John, John Jacobs
-
Publication number: 20040029874Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: ApplicationFiled: July 29, 2003Publication date: February 12, 2004Inventors: Douglas Wade Beight, Trelia Joyce Craft, Carl Penman Denny, Jeffry Bernard Franciskovich, Theodore Goodson, Steven Edward Hall, David Kent Herron, Sajan Joseph, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milet, Marta Maria Pinelro-Nunez, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
-
Patent number: 6686353Abstract: Cyclic diamines of formula (I) or their pharmacologically acceptable acid addition salts, and their medical applications are described. These compounds inhibit the action of chemokines such as MIP-1a and/or MCP-1 on target cells, and are useful as a therapeutic drug and/or preventative drug in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissue.Type: GrantFiled: July 15, 1999Date of Patent: February 3, 2004Assignees: Teijin Intellectual Property Center Limited, Combichem, Inc.Inventors: Tatsuki Shiota, Shinsuke Yamagami, Kenichiro Kataoka, Noriaki Endo, Hiroko Tanaka, Doug Barnum, Jonathan Greene, Wilna Moree, Michele Ramirez Weinhouse, Christine M. Tarby
-
Patent number: 6649616Abstract: The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) to processes for their preparation and to their use in medicaments, in particular for the prevention and/or treatment of cardiovascular disorders.Type: GrantFiled: August 30, 2001Date of Patent: November 18, 2003Assignee: Bayer AktiengesellschaftInventors: Erwin Bischoff, Thomas Krahn, Stephan-Nicholas Müller, Holger Paulsen, Joachim Schuhmacher, Henning Steinhagen, Wolfgang Thielemann
-
Publication number: 20030208074Abstract: In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process: 1Type: ApplicationFiled: March 27, 2003Publication date: November 6, 2003Applicant: Schering CorporationInventors: Wenxue Wu, Hongbiao Liao, David J. S. Tsai, David R. Andrews, Dinesh Gala, Gary M. Lee, Martin Lawrence Schwartz, Timothy L. McAllister, Xiaoyong Fu, Donal Maloney, Tiruvettipuram K. Thiruvengadam, Chou-Hang Tann
-
Publication number: 20030207871Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.Type: ApplicationFiled: February 19, 2003Publication date: November 6, 2003Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
-
Patent number: 6635634Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: October 21, 2003Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
-
Publication number: 20030187295Abstract: The invention relates to a method for the production of &OHgr;-aminoalkylsulphonic acids of general formula (I), where R1 and R2=optionally substituted alkyl groups with 1 20 C atoms and n=a whole number from 2 6, whereby an amine of formula (II), where R1 and R2 have the above meanings is reacted with an alkyl dihalide of formula (III), where n has the above meaning and X1 and X2=chlorine or bromine, with addition of alkali hydroxide at a pH of 8 10. The pH is then adjusted to a value of 0 1, by addition of a hydrohalic acid and excess alkyl dihalide is separated off, before the reaction solution is adjusted to a pH of 6 7.5 with alkali liquor, alkali sulphite is added and the product (I) formed at elevated temperate.Type: ApplicationFiled: November 8, 2002Publication date: October 2, 2003Inventors: Volker Schaefer, Wolfgang Knoll, Alexander Schmitt, Christoph Huettner
-
Patent number: 6608066Abstract: The invention includes pharmaceutically active compounds and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for treating or prophylaxis of undesired thrombosis.Type: GrantFiled: October 27, 2000Date of Patent: August 19, 2003Assignee: Sunol Molecular CorporationInventors: Jin-An Jiao, Lawrence K. Luepschen, Esperanza L. Nieves, Hing C. Wong, Dean P. Taylor
-
Publication number: 20030153555Abstract: The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 17, 2002Publication date: August 14, 2003Inventors: Tomas Eriksson, Krister Henriksson
-
Publication number: 20030153559Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.Type: ApplicationFiled: November 20, 2002Publication date: August 14, 2003Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
-
Patent number: 6579881Abstract: A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: wherein A, B, C, D, T, Y, and Z each represent a methine or a nitrogen linkage; R1, R2, R3, R4, and R5 each represent a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3. The compounds have serotonin antagonism. They are therefore clinically useful as medicaments, in particular, for treating, ameliorating, and preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 18, 2001Date of Patent: June 17, 2003Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
-
Patent number: 6569929Abstract: The present invention relates to a method for preparing phosphoramides having a glass transition temperature in one embodiment of at least about 0° C., in another embodiment of at least about 10° C., and in still another embodiment of at least about 20° C., the phosphoramides being substantially free of acidic, basic, or halide impurities, or their precursors. The invention also relates to resin compositions comprising at least one thermoplastic resin and at least one phosphoramide having a glass transition temperature of at least about 0° C., wherein the phosphoramide is prepared by the method of the invention.Type: GrantFiled: May 4, 2001Date of Patent: May 27, 2003Assignee: General Electric CompanyInventors: Neal Steven Falcone, John Robert Campbell, James Ross Fishburn
-
Publication number: 20030096811Abstract: Aminomethyl-phenyl-cyclohexanone derivatives of formula I or Ia, 1Type: ApplicationFiled: July 5, 2002Publication date: May 22, 2003Inventors: Claudia Puetz, Helmut Buschmann, Babette-Yvonne Koegel
-
Publication number: 20030092911Abstract: The invention refers to a novel process for the preparation of cetirizine of formula (I) as well as to novel {2-[4-(&agr;-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}acetamides of formula II, wherein R1 and R2 represent, independently, a C1-4 alkyl group optionally substituted by a phenyl group, a C2-4 alkenyl group or a cyclohexyl group, or R1 and R2 form together with the adjacent nitrogen atom a morpholino group. According to the novel process, an acetamide of formula (II) is hydrolized, if desired in the presence of a phase transfer catalyst, to obtain cetirizine.Type: ApplicationFiled: July 3, 2002Publication date: May 15, 2003Inventors: Jozsef Reiter, Peter Trinka, Ferenc Bartha, Gyula Simig, Kalman Nagy, Gyorgyi Vereczkeyne Donath, Norbert Nemeth, Gyorgy Clementis, Peter Tompe, Pal Vago
-
Patent number: 6552025Abstract: Compositions, methods of use, isolation and biosynthesis of diimino-piperazine derivatives useful for the modification of sphingolipid metabolism and other biological functions are described. The preferred derivative is 2,6-bis-(&ohgr;-aminobutyl)-3,5-diimino-piperazine. This is a naturally occurring biochemical compound isolated from cells. The diimino-piperazine derivatives are useful as therapeutic agents when administered to patients to treat diseases and disorders involving cell regulation.Type: GrantFiled: November 17, 2000Date of Patent: April 22, 2003Assignee: Emory UniversityInventors: Alfred H. Merrill, Jr., Lisa Warden, Dennis C. Liotta
-
Publication number: 20030064994Abstract: Novel compounds of the general formula: 1Type: ApplicationFiled: September 13, 2002Publication date: April 3, 2003Applicant: CV Therapeutics, Inc.Inventors: Vaibhav Varkhedkar, Venkata P. Palle, Jeff Zablocki, Elfatih Elzein, Brent K. Blackburn
-
Patent number: 6541475Abstract: &agr;, &bgr;-Unsaturated sulfones of the following formulae are provided, which are useful as antiproliferative agents, including, for example, anticancer agents:Type: GrantFiled: April 12, 2001Date of Patent: April 1, 2003Assignee: Temple University - Of the Commonwealth System of Higher EducationInventors: E. Premkumar Reddy, M. V. Ramana Reddy
-
Publication number: 20030060624Abstract: The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: 1Type: ApplicationFiled: April 17, 2002Publication date: March 27, 2003Inventor: Robert A. Singer
-
Publication number: 20030055260Abstract: This invention relates to the novel use of diphenyl sulfamido in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: August 30, 2002Publication date: March 20, 2003Inventors: Michael R. Palovich, Joseph Weinstock, Katherine L. Widdowson
-
Publication number: 20030055248Abstract: This invention relates to novel compounds and compositions thereof useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: October 7, 2002Publication date: March 20, 2003Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
-
Patent number: 6525099Abstract: The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: February 25, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
-
Publication number: 20030009029Abstract: The present invention relates to a process preparing compounds of the general formula (I) 1Type: ApplicationFiled: June 5, 2002Publication date: January 9, 2003Applicant: Merck Patent GmbHInventors: Herwig Buchholz, Urs Welz-Biermann
-
Patent number: 6495546Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.Type: GrantFiled: November 22, 2000Date of Patent: December 17, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka