The Spiro Includes The Five-membered Hetero Ring Patents (Class 548/408)
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Patent number: 7632953Abstract: The present invention provides an improved process for the preparation of gabalactam of formula 1 that includes preparing an aqueous solution of an alkali or alkaline earth metal hydroxide, adding bromine to the resulting solution to give an appropriate alkali or alkaline earth metal hypobromite; adding an amide of the formula 4 aging the resultant mixture; heating the mixture to a temperature in a range of 80 to 100 degrees C.; extracting with nonpolar solvent and distilling under reduced pressure to obtain gabalactam.Type: GrantFiled: November 20, 2002Date of Patent: December 15, 2009Assignee: Hikal LimitedInventors: Nagarajan Kuppuswamy, Sivaramakrishnan Hariharan, Arulselvan Mariadas
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Publication number: 20090270637Abstract: The present invention provides a method for effectively producing an optically active form of tetrasubstituted-5-azaspiro[2.4]heptane derivative, which serves as a useful production intermediate for quinolonecarboxylic acid antibacterial agents, and intermediates for the derivative. The present invention is directed to a method for producing a compound (VII) according to the following scheme.Type: ApplicationFiled: September 28, 2006Publication date: October 29, 2009Applicant: Daiichi Sankyo Company, LimitedInventors: Hisashi Takahashi, Rie Miyauchi, Yasuyuki Takeda, Kazuo Kanai, Junichi Kuroyanagi, Satoshi Komoriya, Makoto Takemura
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Publication number: 20090215624Abstract: The invention relates to novel alkoxyalkyl spirocyclic tetramic and tetronic acids of the formula (I), in which A, B, D, Q1, Q2, Q3, Q4, G, W, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides, and also to selective herbicidal compositions comprising, firstly, the alkoxyalkyl spirocyclic tetramic and tetronic acids and, secondly, at least one crop plant compatibility-improving compound.Type: ApplicationFiled: October 20, 2006Publication date: August 27, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Dieter Feucht, Olga Malsam, Mark Wilhelm Drewes, Eva-Maria Franken, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Hugh Rosinger, Thomas Bretschneider, Guido Bojack, Jan Dittgen
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Publication number: 20090209598Abstract: This invention relates to resorcine derivatives of formula (I) wherein R1 is phenyl or a 5- to 6-membered heteroaromatic ring which may contain 1 to 3 heteroatoms selected from oxygen, nitrogen and sulfur, wherein phenyl or the heteroaromatic ring may be fused to a ring selected from phenyl and a 5- to 6-membered saturated, partially unsaturated or aromatic heterocyclic ring which may contain 1 to 3 heteroatoms selected from oxygen, nitrogen and sulfur, wherein phenyl or the 5- to 6-membered heteroaromatic ring or the respective fused ring systems may be unsubstituted or substituted by any combination of 1 to 6 optionally substituted groups R3, wherein R3 is halogen, cyano, nitro, hydroxy, mercapto, amino, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, haloalkyl, haloalkenyl, haloalkynyl, halocycloalkyl, halocycloalkenyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, haloalkenyloxy, haloalkynyloxy, alkylthio, alkenylthio, alkynylthio, haloalkylthio, haloalkenylthio, haloalkynylthio, alkylamino, alkenylaminoType: ApplicationFiled: November 10, 2006Publication date: August 20, 2009Inventors: Michael Puhl, Markus Kordes, Matthias Pohlman, Norbert Götz, Michael Rack, Jürgen Langewald, Felix Schneider, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, David G. Kuhn
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Publication number: 20090156824Abstract: A method includes reacting an amino group, a composition including rhodium and an organic ligand, and a substrate having structural formula (I) in a reaction mixture. R1 is an organic group including a sp3 carbon atom bonded to CA. R2 is selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CA. R3 and R4 independently are selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CB. The method further includes forming a hydroaminated product in the reaction mixture.Type: ApplicationFiled: October 14, 2008Publication date: June 18, 2009Applicant: BOARD OF TRUSTEES OF UNIVERSITY OF ILLINOISInventors: Akihiro Takemiya, Zhijian Liu, John F. Hartwig
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Publication number: 20090099247Abstract: Compounds of the formula (I) in which A, B, G, W, X, Y and Z can have the meanings given in the description are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.Type: ApplicationFiled: September 23, 2008Publication date: April 16, 2009Inventors: Thomas E. Macom, Reiner Fischer, Gerhard Baron, Erich Sanwald, Reed Nathan Royalty, Xavier Alain Marie Van Waetermeulen, Udo Reckmann, Alexandra Gladbach, Stephen Krueger, Peter Marczok
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Publication number: 20090099180Abstract: The present invention discloses novel compounds of Formula (I): having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.Type: ApplicationFiled: April 25, 2007Publication date: April 16, 2009Inventors: Thomas Edward Mabry, Owen Brendan Wallace, Yanping Xu, Nancy June Snyder, Leonard Larry Winneroski, JR.
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Publication number: 20090054648Abstract: The invention provides an industrial method for producing a spiroaminopyrrolidone derivative, which is an intermediate for producing a quinolone antibacterial agent. The invention provides a method for producing a compound represented by formula (2): (wherein n is an integer of 2 to 5; R1 represents a (substituted) alkyl group or a (substituted) aryl group; and R2 represents a (substituted) alkoxycarbonyl group, a (substituted) aralkyloxycarbonyl group, a (substituted) aliphatic acyl group, or a (substituted) aromatic acyl group), which includes treating a compound represented by formula (1): (wherein n, R1, and R2 are the same as defined above; and R3 represents a hydrogen atom, a (substituted) alkyl group, or a (substituted) aralkyl group) under a hydrogen gas atmosphere in the presence of a metallic catalyst.Type: ApplicationFiled: May 19, 2006Publication date: February 26, 2009Applicant: Daiichi Sankyo Company, LimitedInventors: Yuichiro Tani, Yutaka Kitagawa, Makoto Muto, Toshiaki Jyono
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Publication number: 20090042967Abstract: The present invention relates to pharmaceutical agents which are agents for the prophylaxis or treatment of hypogonadism, male climacteric disorder, frailty, cachexia or osteoporosis; the pharmaceutical agents frailty suppressants, muscle strength enhancers, muscle increasing agents, cachexia suppressants, body weight decrease suppressants, agents for the prophylaxis or treatment of prostate hypertrophy, amyotrophy or muscle loss caused by a disease or an agent for reducing the prostate weight.Type: ApplicationFiled: August 6, 2008Publication date: February 12, 2009Applicant: Takeda Pharmaceutical Company LimitedInventor: Atsushi Hasuoka
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Publication number: 20090029858Abstract: The invention relates to novel spirocyclic 3?-alkoxytetramic acids and -tetronic acids of the formula (I), in which A, B, D, Q1, Q2, G, W, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides, and also to selective herbicidal compositions comprising firstly the spirocyclic 3?-alkoxytetramic acids and -tetronic acids and secondly at least one compound which improves crop plant tolerance.Type: ApplicationFiled: June 18, 2005Publication date: January 29, 2009Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Thomas Bretschneider, Dieter Feucht, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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Patent number: 7482372Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: March 30, 2005Date of Patent: January 27, 2009Assignee: Bristol-Myers Squibb CompanyInventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Patent number: 7476688Abstract: A cyclic amidine derivative represented by the formula: [wherein R1, R2 and R3 represent hydrogen, C1-6 alkyl, aryl-C1-6 alkyl, etc.; R4, R5 and R7 represent hydrogen, C1-6 alkyl, etc.; Z represents 0 or 1; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; n represents 1 or 2; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; Ar represents hydrogen, a group represented by the formula: [wherein R10-R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.] or a salt thereof.Type: GrantFiled: April 19, 2002Date of Patent: January 13, 2009Assignee: EISAI R&D Management Co., Ltd.Inventors: Shuichi Suzuki, Masanobu Shinoda, Motoji Kogushi, Hiroko Kobayashi
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Publication number: 20090012120Abstract: An ylide-based aza-Payne rearrangement of 2,3-aziridin-1-ols leads to an efficient process for the preparation of pyrrolidines. The aza-Payne rearrangement under the basic reaction conditions favors the formation of epoxy amines. Subsequent nucleophilic attack of the epoxide by the ylide yields a bis-anion, which upon a 5-exo-tet ring closure yields the desired pyrrolidine, thus completing the relay of the 3-membered the 5-membered nitrogen containing ring system. This process takes place with complete transfer of stereochemical fidelity, and can be applied to sterically hindered aziridinols.Type: ApplicationFiled: May 9, 2007Publication date: January 8, 2009Applicant: Board of Trustees of Michigan State UniversityInventors: Babak Borhan, Jennifer M. Schomaker, Somnath Bhattacharjee, Keith Korthals
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Publication number: 20080318776Abstract: The invention relates to novel 2,6-diethyl-4-methylphenyl-substituted tetramic acid derivatives of the formula (I) in which A, B, D and G are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selectively herbicidal compositions comprising, firstly, the 2,6-diethyl-4-methylphenyl-substituted tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant tolerance promoter compound.Type: ApplicationFiled: October 21, 2005Publication date: December 25, 2008Inventors: Reiner Fischer, Stefan Lehr, Mark Wilhelm Drewes, Dieter Feucht, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Marin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20080305955Abstract: The invention relates to novel spiroketal-substituted cyclic ketoenols of the formula (I) in which A, B, Q1, Q2, D, G, W, X, Y, and Z are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or microbicides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, spiroketal-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound.Type: ApplicationFiled: February 8, 2006Publication date: December 11, 2008Applicant: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Mark Wilhelm Drewes, Dieter Feucht, Olga Malsam, Udo Reckmann, Christian Arnold, Thomas Auler, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Christopher Hugh Rosinger, Erich Sanwald
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Patent number: 7459414Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as herbicides.Type: GrantFiled: March 18, 2005Date of Patent: December 2, 2008Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
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Publication number: 20080287435Abstract: The novel active compound combinations of certain cyclic ketoenols and ethiprole have very good insecticidal and acaricidal properties.Type: ApplicationFiled: February 14, 2006Publication date: November 20, 2008Applicant: Bayer CropScience AGInventors: Reiner Fischer, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20080274893Abstract: The present invention relates to novel phenyl-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y, Z and R3 are as defined above, to processes and intermediates for their preparation and to their use as pesticides, microbicides and herbicides.Type: ApplicationFiled: July 8, 2008Publication date: November 6, 2008Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Mark Wilhelm Drewes, Christoph Erdelen, Angelika Lubos-Erdelen, Dieter Feucht, Udo Reckmann
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Patent number: 7439371Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: July 11, 2006Date of Patent: October 21, 2008Assignee: Allergan, Inc.Inventors: Julie A. Wurster, Richard C. Yee
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Patent number: 7407982Abstract: The present invention relates to novel covalent oligo and polyalkylene glycol conjugates with synthetic inhibitors of trypsin-type serine proteases, in particular inhibitors of the hemocoagulation protease thrombin, synthetic intermediates stages required in their production and their use for producing active ingredients for the treatment or prophylaxis of thrombotic complications.Type: GrantFiled: January 23, 2002Date of Patent: August 5, 2008Assignee: HaemoSys GmbHInventors: Torsten Steinmetzer, Götz Nowak
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Publication number: 20080171788Abstract: The invention relates to a medicament for IBS, which comprises a dual antagonist for 5-HT2B and 5-HT7 receptors having selective binding affinities for 5-HT2B and 5-HT7 receptors. The pharmaceutical composition of the invention is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS, because it showed good pharmacological actions in comparison with the case of independently using a 5-HT2B receptor antagonist having selective binding affinity for 5-HT2B receptor or a 5-HT7 receptor antagonist having selective binding affinity for 5-HT7 receptor.Type: ApplicationFiled: February 7, 2006Publication date: July 17, 2008Inventors: Shinobu Akuzawa, Hiroyuki Ito, Toshihiro Watanabe, Hiroyoshi Yamada
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Patent number: 7399857Abstract: A process for forming a tris-cyclometallated complex comprises the step of reacting; a) an M(I) complex, wherein M represents Rh or Ir, and said complex comprises at least two ligands and contains at least two alkenyl groups pi-bonded to M, with b) a heterocyclic compound capable of forming a organometallic cyclometallated complex.Type: GrantFiled: November 29, 2005Date of Patent: July 15, 2008Assignee: Eastman Kodak CompanyInventors: Barbara B. Lussier, Joseph C. Deaton
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Patent number: 7396846Abstract: This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.Type: GrantFiled: March 31, 2003Date of Patent: July 8, 2008Assignee: Eli Lilly and CompanyInventors: Britta Evers, Ruehter Gerd, Eva Maria Martin De La Nava, Mark Joseph Tebbe
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Patent number: 7297788Abstract: The present invention refers to highly functionalised spiro-fused azetidinones of formula I: having a cyclohexane moiety with the desired number of protected or unprotected hydroxyl groups which are introduced with high stereo and regioselectivity, as well as processes for their synthesis.Type: GrantFiled: May 25, 2004Date of Patent: November 20, 2007Assignee: Laboratorios Del Dr. Esteve. S.A.Inventors: Pedro Noheda Marin, Manuel Bernabe Pajares, Sergio Maroto Quintana, Nuria Tabares Cantero
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Patent number: 7291728Abstract: The present invention is directed to a compound of formula I: wherein R1 and R2 are independently selected from H, halogen, protected or unprotected hydroxy, alkylsilyloxy, substituted or unsubstituted alkyl or cycloalkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, nitro, amino, mercapto or alkylthio; R3 and R4 are independently selected from H, substituted alkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl; Z is —(CRaRb)n— wherein n is a number selected from 1, 2, 3 and Ra and Rb are each independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy, substituted or unsubstituted amino or halogen; Y isType: GrantFiled: May 14, 2004Date of Patent: November 6, 2007Assignee: Laboratories Del Dr. Esteve, S.A.Inventors: Pedro Noheda Marin, Manuel Bernabe Pajares, Sergio Maroto Quintana, Nuria Tabares Cantero
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Publication number: 20070213526Abstract: Processes are provided for purifying a compound of the structure: wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.Type: ApplicationFiled: March 5, 2007Publication date: September 13, 2007Applicant: WyethInventors: Mahmut Levent, Panolil Raveendranath, Bogdan Wilk, Donald Carl Boop, Marinus Cornelis Hofman
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Patent number: 7238703Abstract: Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borne virus, anti-HSV and anti-Hepatitis C virus activity.Type: GrantFiled: August 11, 2005Date of Patent: July 3, 2007Assignee: Merz Pharma GmbH & Co. KGAAInventors: Christopher G. R. Parsons, Markus Henrich, Wojciech Danysz, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons, Markus Gold, Maksims Vanejevs
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Patent number: 7148246Abstract: Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals The invention relates to cycloalkyl derivatives having bioisosteric carboxylic acid groups and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.Type: GrantFiled: February 27, 2004Date of Patent: December 12, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Dirk Gretzke, Heiner Glombik, Eugen Falk, Jochen Goerlitzer, Stefanie Keil, Hans-Ludwig Schaefer, Christian Stapper, Wolfgang Wendler
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Patent number: 7141679Abstract: A process for making N-vinyl-2-pyrrolidone (NVP) is disclosed. The process comprises dehydrating N-(2-hydroxyethyl)-2-pyrrolidone (HEP) in the presence of a catalyst and added water. Adding an effective amount of water into the dehydration process reduces the amount of N-ethyl-2-pyrrolidone (NEP) formed compared with the amount produced in the absence of the added water. Adding water can also sustain high conversions of HEP, minimize heavies formation, and improve selectivity to NVP. The process provides high-purity NVP and avoids a costly crystallization step.Type: GrantFiled: September 26, 2005Date of Patent: November 28, 2006Assignee: Lyondell Chemical Technology,L.P.Inventor: Andrew P. Kahn
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Patent number: 7122677Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceuticals compositions. Methods of treatment and combinations with other agents are also disclosed.Type: GrantFiled: November 12, 2002Date of Patent: October 17, 2006Assignee: Scherig CorporationInventors: Gregory A. Reichard, Sunil Paliwal, Neng-Yang Shih, Dong Xiao, Hon-Chung Tsui, Sapna Majmundar Shah, Cheng Wang, Michelle Laci Wrobleski
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Patent number: 7122678Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.Type: GrantFiled: March 11, 2005Date of Patent: October 17, 2006Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, David Christopher Horwell, Andrew John Thorpe, David Juergen Wustrow, Po-Wai Yuen
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Patent number: 7109350Abstract: A process produces an optically active amine or its salt and includes the steps of reacting a ketone of Formula (1a): wherein R1 is typically an unsubstituted or substituted hydrocarbon group; and R2a is typically a hydrocarbon group having at least one oxo group and optionally having other substituent, with an optically active amine of Formula (2): wherein R3 is an unsubstituted or substituted aryl group; R4 is an unsubstituted or substituted lower alkyl group; and C1 is an asymmetric carbon atom, in the presence of an organic acid to thereby yield a corresponding optically active imine, hydrogenating the imine in the presence of a catalyst to yield a corresponding amine, subjecting the amine or its salt to hydrogenolysis in the presence of a catalyst, and reducing the hydrogenolyzed product with a reducing agent.Type: GrantFiled: June 29, 2004Date of Patent: September 19, 2006Assignee: Daicel Chemical Industries, Ltd.Inventors: Hiroki Tanaka, Li Rui Pan, Kiyoshi Ikura
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Patent number: 7087635Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.Type: GrantFiled: March 16, 2005Date of Patent: August 8, 2006Assignee: Eli Lilly and CompanyInventors: Daniel Jon Sall, Jolie Anne Bastian, Cynthia Darshini Jesudason, Don Richard Finley, Freddie Craig Stevens, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, John Xiaoqiang He, John Arnold Werner, William George Trankle, Andrew Michael Ratz, Theo Schotten, Gerd Reuhter
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Patent number: 7053114Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: April 5, 2004Date of Patent: May 30, 2006Assignee: Sugen, Inc.Inventors: Connie Li Sun, Chung Chen Wei, Peng Cho Tang, Marcel Koenig, Yong Zhou, Tomas Vojkovsky, Asaad S. Nematalla
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Patent number: 6982337Abstract: A process for making N-vinyl-2-pyrrolidone (NVP) is disclosed. The process comprises dehydrating N-(2-hydroxyethyl)-2-pyrrolidone (HEP) in the presence of a catalyst and added water. Adding an effective amount of water into the dehydration process reduces the amount of N-ethyl-2-pyrrolidone (NEP) formed compared with the amount produced in the absence of the added water. Adding water can also sustain high conversions of HEP, minimize heavies formation, and improve selectivity to NVP. The process provides high-purity NVP and avoids a costly crystallization step.Type: GrantFiled: July 28, 2004Date of Patent: January 3, 2006Assignee: Lyondell Chemical Technology, L.P.Inventor: Andrew P. Kahn
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Patent number: 6939888Abstract: The invention concerns 1-H-3-arylpyrrolidine-2,4-dione derivatives of formula (I), in which A, B, G, X, Y and Z are as defined in the description, methods of preparing them and intermediates used in their preparation. The compounds of formula (I) are suitable for use as pest-control agents.Type: GrantFiled: July 3, 2002Date of Patent: September 6, 2005Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Krüger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann
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Patent number: 6906197Abstract: A process produces an optically active amine or its salt and includes the steps of reacting a ketone of Formula (1a) wherein R1 is typically an unsubstituted or substituted hydrocarbon group; and R2a is typically a hydrocarbon group having at least one oxo group and optionally having other substituent, with an optically active amine of Formula (2): wherein R3 is an unsubstituted or substituted aryl group; R4 is an unsubstituted or substituted lower alkyl group; and C1 is an asymmetric carbon atom, in the presence of an organic acid to thereby yield a corresponding optically active imine, hydrogenating the imine in the presence of a catalyst to yield a corresponding amine, subjecting the amine or its salt to hydrogenolysis in the presence of a catalyst, and reducing the hydrogenolyzed product with a reducing agent.Type: GrantFiled: December 6, 2002Date of Patent: June 14, 2005Assignee: Daicel Chemical Industries, LtdInventors: Hiroki Tanaka, Li Rui Pan, Kiyoshi Ikura
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Patent number: 6906053Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: May 12, 2004Date of Patent: June 14, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Patent number: 6894005Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomer of those compounds, are suitable for use as herbicides.Type: GrantFiled: September 5, 2000Date of Patent: May 17, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Thomas Maetzke, André Stoller, Sebastian Wendeborn, Henry Szczepanski
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Patent number: 6890915Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: May 23, 2002Date of Patent: May 10, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: James E. Sheppeck, Jingwu Duan, Chu-Biao Xue, Zelda Wasserman
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Patent number: 6861391Abstract: Trifluoromethyl-substituted spirocyclic ketoenols of the formula (I) are provided wherein Het represents one of the groups and G, V, W, X, Y, and Z are as defined in the specification. Also provides are processes for the preparation of the compounds. The compounds of formula (I) find use as pesticides.Type: GrantFiled: September 19, 2000Date of Patent: March 1, 2005Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht
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Patent number: 6835744Abstract: This invention provides compounds of the formula I: wherein: R1 and R2 are independently H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and substituted alkyl, O(alkyl), aryl, or heteroaryl; or R1 and R2 are joined to form a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2C(CH3)2CH2CH2—; —O(CH2)mCH2— where m=1-4; O(CH2)pO— where p=1-4; —CH2CH2OCH2CH2—; —CH2CH2N(H or alkyl)CH2CH2—; or R1 and R2 together comprise a double bond to C(CH3)2, C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl groups; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is optionally substituted benzene ring; five or six membered heterocyclic ring; 4 or 7-substituted indole or a substituted benzothiophene; or pharmaceutically acceptable salt tType: GrantFiled: April 24, 2002Date of Patent: December 28, 2004Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: John W. Ullrich, Andrew Fensome, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6825220Abstract: The present invention relates to a &bgr;;3 adrenergic receptor agonist of formula I: (1); or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.Type: GrantFiled: April 11, 2003Date of Patent: November 30, 2004Assignee: Eli Lilly and CompanyInventors: Cynthia Darshini Jesudason, Daniel Jon Sall, Freddie Craig Stevens, John Arnold Werner
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Publication number: 20040235928Abstract: A process produces an optically active amine or its salt and includes the steps of reacting a ketone of Formula (1a): 1Type: ApplicationFiled: June 29, 2004Publication date: November 25, 2004Applicant: Daicel Chemical Industries, Ltd.Inventors: Hiroki Tanaka, Li Rui Pan, Kiyoshi Ikura
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Publication number: 20040186088Abstract: The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases.Type: ApplicationFiled: December 19, 2003Publication date: September 23, 2004Inventors: Upul Bandarage, Jon H. Come, Emanuele Perola, Govinda Rao Bhisetti, Jeffrey O. Saundres
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Publication number: 20040097532Abstract: The present invention relates to a &bgr;;3 adrenergic receptor agonist of formula I: (I); or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.Type: ApplicationFiled: April 11, 2003Publication date: May 20, 2004Inventors: Cynthia Darshini Jesudason, Daniel Jon Sall, Freddie Craig Stevens, John Arnold Werner
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Publication number: 20040082642Abstract: The present invention relates to compounds of formula (I) and derivatives thereof, in which the variables are as defined in the claims, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynecomastia, autoimmune disease, vascular smooth muscle cell profileration, obesity, incontinence, and cancer of the lung, colon, breast, uterus, and prostate.Type: ApplicationFiled: November 14, 2003Publication date: April 29, 2004Inventors: Konrad Koehler, Mikael Gillner, Ye Liu, Aiping Cheng, James V Heck, Milton Lloyd Hammond, Ralph Troy Mosley, Mahmoud Rahimi-Ghadim
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Publication number: 20040044018Abstract: There are provided methods for the treatment of diseases involving dysfunction of the peripheral and central nervous system comprising administering one or more Spiro compounds. Also provided and pharmaceutical compositions useful in such methods, compounds for use in the preparation of such pharmaceutical compositions, processes for preparing compounds useful in the practice of such methods, and some novel such compounds per se.Type: ApplicationFiled: May 2, 2003Publication date: March 4, 2004Applicant: ISRAEL INSTITUTE FOR BIOLOGICAL RESEARCHInventors: Abraham Fisher, Nira Bar-Ner, Yishai Karton
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Publication number: 20040023926Abstract: The field of the present invention is that of novel organosilicon compounds comprising a multifunctional polyorganosiloxane (abbreviated as POS) comprising, per molecule, and attached to silicon atoms, firstly at least one hydroxyl radical and/or at least one alkoxy radical, and secondly at least one group containing an activated ethylenic double bond consisting of a maleimide group. The present invention also relates to functionalization processes leading to the POSs targeted above, which consist in particular in reacting an organosilane bearing a maleamic acid function and at least two alkoxy functions with a polysilazane.Type: ApplicationFiled: August 26, 2003Publication date: February 5, 2004Inventors: Nathalie Guennouni, Jean-Jacques Lebrun
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Publication number: 20040019223Abstract: A process for preparing intermediate compound (VII), compound (VIII) and compound (XIV) which will be raw materials for the synthesis of a synthetic antibactrial compound, via compound (I) or compound (X) and then, compound (II), the compounds each being shown below; and novel compounds useful for the preparation.Type: ApplicationFiled: February 10, 2003Publication date: January 29, 2004Inventors: Keiji Nakayama, Makoto Muto, Tatsuru Saito, Yuichiro Tani, Toshifumi Akiba