Chalcogen Attached Indirectly To The Lactone Ring By Nonionic Bonding Patents (Class 549/323)
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Publication number: 20080319049Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, wherein n is 1 or 2; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (Type: ApplicationFiled: January 22, 2007Publication date: December 25, 2008Applicant: WELLSTAT THERAPEUTICS CORPORATIONInventors: Shalini Sharma, Reid W. von Borstel
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Publication number: 20080275053Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, B, D, Z, R1, R2a, R2b, and Rx are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.Type: ApplicationFiled: October 6, 2004Publication date: November 6, 2008Inventors: Gerard Martin Paul Giblin, Adrian Hall, Ian Reginald Kilford, Xiao Qing Lewell, Neil Derek Miller, Alan Naylor
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Patent number: 7405226Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.Type: GrantFiled: June 26, 2006Date of Patent: July 29, 2008Assignee: Pfizer Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela
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Publication number: 20080103196Abstract: The present invention relates to novel diterpene compounds isolated from the fruiting body of Antrodia camphorata, especially to the new compounds of following structural formula: and pharmaceutically acceptable salt, solvate, hydrate or biologically active equivalent thereof. The present invention also relates to a pharmaceutical composition containing at least one of the novel diterpene compounds, and a use of the diterpene compound as a neuroprotective agent.Type: ApplicationFiled: October 25, 2006Publication date: May 1, 2008Inventors: Min-Nan Lai, Yueh-Hsiung Kuo, Young-Ji Shiao
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Patent number: 7341818Abstract: The disclosed invention relates to novel norborne-type monomers containing pendent lactone or sultone groups. The invention also relates to norborne-type polymers and copolymers containing pendent lactone or sultone groups. These polymers and copolymers are useful in making photoimagable materials. The photoimagable materials are particularly suitable for use in photoresist compositions useful in 193 and 157 nm photolithography.Type: GrantFiled: January 10, 2005Date of Patent: March 11, 2008Assignee: Promerus LLCInventors: Xiaoming Wu, Larry F. Rhodes, Lawrence Seger
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Patent number: 7316884Abstract: A 5-methylene-1,3-dioxolan-4-one derivative and a monomer and copolymer thereof and a resist composition containing the polymer or copolymer where the 5-methylene-1,3 -dioxolan-4-one derivative is of formula (1): wherein R1 represents a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms, or a linear or branched alkyl group containing 1 to 6 carbon atoms which has a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms as a substituent; R2 represents a hydrogen atom, or a linear or branched alkyl group containing 1 to 6 carbon atoms; or R1 and R2 represent a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms together with the carbon atom to which they are bound, provided that the alkyl group and the bridged cyclic hydrocarbon group may have at least one substituent selected from a group consisting of a linear or branched alkyl group containing 1 to 6 carbon atoms which may be optionally substituted, a hydroxy group, a carboxy group, an acyl group containing 2 to 6 carType: GrantFiled: October 22, 2002Date of Patent: January 8, 2008Assignee: Mitsubishi Rayon Co., Ltd.Inventors: Ryuichi Ansai, Yoshihiro Kamon, Tadayuki Fujiwara, Hideaki Kuwano, Atsushi Ootake, Hikaru Momose
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Patent number: 7317039Abstract: The invention concerns deuterated substituted dihydrofuranones and pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated substituted dihydrofuranones for the treatment of symptoms for the irritating states of degenerative joint disorders, of acute pain and primary dysmenorrhea. In addition, the invention discloses pharmaceutical compositions, which contain deuterated substituted dihydrofuranones as well as their physiologically compatible salts, in addition to pharmaceutically compatible adjuvants and/or additives, for the treatment of symptoms for the irritating states of degenerative joint disorders, of acute pain and primary dysmenorrhea.Type: GrantFiled: December 11, 2002Date of Patent: January 8, 2008Assignee: BDD Berolina Drug Development GmbHInventor: Rudolf-Giesbert Alken
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Publication number: 20070259948Abstract: The present invention relates to compounds of formula (1), its solvates and pharmaceutically acceptable salts having antifungal activity and its pharmaceutical composition comprising an effective amount of compound of formula (1) wherein R is substituted alkyl, alkenyl, aryl, heteroaryl, 2-thienyl, 3-thienyl, halothienyl, haloalkyl, halophenyl, or pyrrolyl; and R1 and R2, each independent of the other, are hydrogen, halogen, or alkoxy. The invention also relates to a process for the preparation of said compounds by contacting the intermediate alcohol, prepared from 1,2-O-isopropylideneglyceraldehyde and substituted phenylacetates, with acid chlorides under appropriate conditions to obtain some of the preferred compounds of the invention.Type: ApplicationFiled: August 4, 2006Publication date: November 8, 2007Inventors: Mukund Keshav Gurjar, Radhika Dilip Wakharkar, Hanumant Bapurao Borate, Ramesh Ganesh Kelkar, Andiappan Murugan, Mohan Anand Chandavarkar, Shreerang Vidyadhar Joshi, Sharangi Ravindra Vaiude
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Patent number: 7232930Abstract: A process for preparing (S)-(?)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4-[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide(IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[-4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxylphenyl]methanesulfonamide (I) and then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-IId.Type: GrantFiled: February 28, 2005Date of Patent: June 19, 2007Assignee: Pharmacia & Upjohn CompanyInventors: Sonja Suzanne MacKey, Michael E. Matison, Haifeng Wu, Michael Paul Goble, Moses W. McMillan, Vikram Gurudath Kalthod
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Patent number: 7223792Abstract: Acetogenins isolated from Annona muricata of the family Annonaceae are described. The substantially pure compounds of the invention exhibit to human tumor cell lines as well as selective cytotoxicity for various human tumor cell lines.Type: GrantFiled: December 7, 2001Date of Patent: May 29, 2007Assignees: Advpharma Inc.Inventor: Yang-Chang Wu
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Patent number: 7153982Abstract: A method for the production of hydroxymatairesinol or a hydroxymatairesinol complex from wood, including the steps of a) extracting finely divided wood material with a polar solvent, b) optionally concentrating the extract by separating at least part of the solvent, c) adding to the extract an agent able to form a complex with hydroxymatairesinol, d) precipitating the hydroxymatairesinol complex, and optionally e) releasing the hydroxymatairesinol from the complex.Type: GrantFiled: November 15, 2002Date of Patent: December 26, 2006Assignee: Hormos Medical CorporationInventors: Seppo Parhi, Mervi Puska, Arja Kalapudas, Helena Korte, Petri Hukka
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Patent number: 7144876Abstract: Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, R2, A, B and D are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 18, 2003Date of Patent: December 5, 2006Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, Jared D Kuemmerle, Hong Zhang, William E Kemnitzer
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Patent number: 7101654Abstract: The disclosed invention relates to novel norbornene-type monomers containing pendent lactone or sultone groups. The invention also relates to norbornene-type polymers and copolymers comprising one or more repeating units represented by the formula: and containing pendent lactone or sultone groups. These polymers and copolymers are useful in making photoimagable materials. The photoimagable materials are particularly suitable for use in photoresist compositions useful in 193 and 157 nm photolithography.Type: GrantFiled: January 14, 2004Date of Patent: September 5, 2006Assignee: Promerus LLCInventors: Xiaoming Wu, Larry F. Rhodes, Lawrence Seger
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Patent number: 7071339Abstract: A process for preparing functionalized ?-butyrolactones 3 and various biologically active compounds using mucohalic acid 1 and halide 2 in the presence of indium is disclosed, wherein X, Y, R1, R2, and R3 may have any of the meanings defined hereinType: GrantFiled: June 18, 2003Date of Patent: July 4, 2006Assignee: Warner Lambert Company LLCInventors: Daniel Belmont, Ji Zhang
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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
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Patent number: 6936447Abstract: Autoinducer molecules, e.g., N-(3-oxododecanoyl)homoserine lactone, for Pseudomonas aeruginosa are described. The molecules regulate gene expression in the bacterium. Therapeutic compositions and therapeutic methods involving analogs and/or inhibitors of the autoinducer molecules also are described. The molecules are useful for treating or preventing infection by Pseudomonas aeruginosa.Type: GrantFiled: April 3, 2000Date of Patent: August 30, 2005Assignees: University of Iowa Research Foundation, University of Rochester, Ithaca CollegeInventors: James P. Pearson, Kendall M. Gray, Luciano Passador, Kenneth D. Tucker, Anatol Eberhard, Barbara H. Iglewski, Everett P. Greenberg
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Patent number: 6919465Abstract: A method of synthesizing (3R,3aS,6aR)-3-hydroxyhexahydrofuro[2,3-b]furan (I), and related compounds, in high yield and high enantiomeric selectivity is disclosed. Also disclosed is a method of manufacturing (5S)-5-(benzyloxymethyl)-5H-furan-2-one.Type: GrantFiled: October 8, 2003Date of Patent: July 19, 2005Assignee: The Board of Trustees of the University of IllinoisInventors: Arun K. Ghosh, Marcus Noetzel, Sofiya Leshchenko
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Patent number: 6906051Abstract: The present invention relates to a class of compounds represented by the Formula I: or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?V?3 and/or the ?V?5 integrin.Type: GrantFiled: November 19, 2003Date of Patent: June 14, 2005Assignee: Pharmacia CorporationInventors: Peter Ruminiski, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Thomas Rogers, Jennifer VanCamp, Chester Yuan
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Publication number: 20040267029Abstract: This invention concerns a method for the production of hydroxymatairesinol or a hydroxymatairesinol complex from wood, comprising the steps ofType: ApplicationFiled: April 19, 2004Publication date: December 30, 2004Inventors: Seppo Parhi, Mervi Puska, Arja Kalapudas, Helena Korte, Petri Hukka
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Patent number: 6833460Abstract: The rate of aminolysis of butyrolactones is predictably adjusted by attaching a substituent having a known field effect value (F) to the alpha position before reacting the substituted buytrolactone with an amine. The aminolysis product is a gamma-hydroxy amide. The resulting materials are useful as the cross-linking agents in a variety of coatings and coatings processes.Type: GrantFiled: November 28, 2001Date of Patent: December 21, 2004Assignee: E. I. du Pont de Nemours and CompanyInventor: Albert Gordon Anderson
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Patent number: 6818780Abstract: Derivatives of the compound p-hydroxyphenyl propionic acid characterised by those derivatives having the general formulas (I) and (Ia), where n can take the values 1,2,3; R can be H or CH3 and R1 can be CH3 or H with pharmacological activity and their application in medicine for the treatment of disorders of the immunological system.Type: GrantFiled: September 20, 2002Date of Patent: November 16, 2004Assignee: Consejo Superior de Investigaciones CientificasInventors: Jaime Bermejo Barrera, Margarita Hernández Silva, Melchor Álvarez De Mon, Juan Pablo Pivel Ranieri
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Patent number: 6787655Abstract: One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.Type: GrantFiled: October 15, 2002Date of Patent: September 7, 2004Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Daniel H. Appella, Yasunori Moritani, Ryo Shintani, Valdas Jurkauskas
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Publication number: 20040162340Abstract: The present invention provides a method for producing compound (XIV) useful as an intermediate for pharmaceutical agents efficiently and economically on an industrial scale without using ozone oxidation and highly toxic reagent, and an intermediate used for this method. Particularly, the present invention provides a method for producing a compound having an absolute configuration represented by the formula (XV) and an enantiomer thereof without using a technique such as optical resolution and the like, and an intermediate used for this method.Type: ApplicationFiled: December 23, 2003Publication date: August 19, 2004Applicant: Sumika Fine Chemicals Co., Ltd.Inventors: Tetsuya Ikemoto, Dongguo Piao
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Patent number: 6730798Abstract: Compounds of formula (II) are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is converted into a hydroxylactone and then the hydroxy group into a leaving group, the leaving group is replaced with azide, the lactone amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I).Type: GrantFiled: January 3, 2003Date of Patent: May 4, 2004Assignee: Speedel Pharma AGInventors: Stefan Stutz, Peter Herold, Felix Spindler
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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
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Patent number: 6720327Abstract: The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or the &agr;v&bgr;5 integrin.Type: GrantFiled: September 26, 2001Date of Patent: April 13, 2004Assignee: Pharmacia CorporationInventors: Peter Ruminski, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Thomas Rogers, Jennifer VanCamp, Chester Yuan
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Patent number: 6696217Abstract: A photosensitive monomer including a methylene butyrolactone derivative represented by the following formula: wherein R1 is a hydrogen atom or alkyl group, R2 is an acid-labile group, X is a hydrogen atom, or substituted or unsubstituted alkyl group having 1 to 10 carbon atoms, and Y is a substituted or unsubstitued alkyl group or alicyclic hydrocarbon group having 1 to 20 carbon atoms.Type: GrantFiled: February 20, 2002Date of Patent: February 24, 2004Assignee: Samsung Electronics Co., Ltd.Inventors: Kwang-sub Yoon, Sang-gyun Woo
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Patent number: 6673818Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: wherein A, X, n, R1, R2, and R3 are as described in the specification, and novel fluoro-substituted benzenesulfonyl compounds within Formula I.Type: GrantFiled: April 16, 2002Date of Patent: January 6, 2004Assignee: Pharmacia CorporationInventors: David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
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Patent number: 6660448Abstract: The invention provides a polymer comprising recurring units containing bridged aliphatic rings in the backbone and having a hydroxyl, acyloxy or alkoxylcarbonyloxy group as well as a lactone structure bonded through a spacer, the polymer having a weight average molecular weight of 1,000-500,000. A resist composition comprising the polymer as a base resin is sensitive to high-energy radiation, has excellent sensitivity, resolution, and etching resistance, and lends itself to micropatterning with electron beams or deep-UV.Type: GrantFiled: November 8, 2001Date of Patent: December 9, 2003Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Seiichiro Tachibana, Mutsuo Nakashima, Tsunehiro Nishi, Takeshi Kinsho, Koji Hasegawa, Takeru Watanabe, Jun Hatakeyama
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Publication number: 20030199575Abstract: Derivatives of the compound p-hydroxyphenyl propionic acid characterised by those derivatives having the general formulas (I) and (Ia), where n can take the values 1,2,3; R can be H or CH3 and R1 can be CH3 or H with pharmacological activity and their application in medicine for the treatment of disorders of the immunological system.Type: ApplicationFiled: September 20, 2002Publication date: October 23, 2003Inventors: Jaime Bermejo Barrera, Margarita Hernandez Silva, Melchor Alvarez De Mon, Juan Pablo Pivel Ranieri
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Patent number: 6630596Abstract: The invention relates to an adduct of polyalk(en)yl succinic anhydride and a compound of formula (I): wherein R1 is hydrogen, hydroxyl, hydrocarbyl, hydroxyhydrocarbyl, carbamyl, 1-acetyl, amino, or nitro; R2 is hydrogen, hydroxyl, hydrocarbyl, hydroxyhydrocarbyl, carbamyl, 1-acetyl, amino, or nitro; R3 is hydrogen or hydrocarbyl; and X is O, S or NH; or a derivative of such an adduct. The invention also relates to an emulsifier comprising such an adduct or derivative, and the invention also relates to compositions including such an emulsifier.Type: GrantFiled: March 1, 2002Date of Patent: October 7, 2003Assignee: Chemical Services LimitedInventor: Willem George Boer
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Patent number: 6576662Abstract: The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).Type: GrantFiled: May 4, 2001Date of Patent: June 10, 2003Assignee: Dr. Reddy's Laboratories LimitedInventors: Srinivas Nanduri, Sriram Rajagopal, Venkateswarlu Akella
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Patent number: 6566538Abstract: The invention provides new methods for preparation of cyclic oxygen compounds, including 2,5-disubstituted tetrahydrofurans, 2,6-disubstituted tetrahydropyrans, 2,7-disubstituted oxepanes and 2,8-oxocanes. The invention also provides new cyclic oxygen compounds and pharmaceutical compositions and therapeutic methods that comprise such compounds.Type: GrantFiled: June 27, 2002Date of Patent: May 20, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Mukund Shankar Chorghade, Mukund Keshao Gurjar, Palakodety Radha Krishna, Sista Venkata Sai Lalitha, Kashinath Sadalapure, Susanta Sekhar Adhikari, Andappan Murugaiah Subbaiah Murugaiah, Batchu Venkateswara Rao, Levadala Murali Krishna, Sunil Vyankatesh Mhaskar, Gangavaram Vasantha Madhava Sharma, Tangallapally Rajendra Prasad, Punna Sreenivas, Vavilala Goverdhan Reddy, Aminul Islam, Alla Venkata Rama Rao, Hymavathi Lanka, Bethi Sridhar Reddy, Chittineni Hari Prasad
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Patent number: 6559100Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radicType: GrantFiled: February 7, 2000Date of Patent: May 6, 2003Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6552031Abstract: Disclosed is a pharmaceutical composition, comprising a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxcodone or a pharmaceutically acceptable salt thereof, said combination in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising administering to the patient a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxycodone or a pharmaceutically acceptable salt thereof such that the dosing interval of the rofecoxib overlaps with the dosing interval of the oxycodone, said combination in an amount sufficient to provide an analgesic effect in a human patient.Type: GrantFiled: September 17, 1998Date of Patent: April 22, 2003Assignee: Euro-Celtique S.A.Inventors: Ronald M. Burch, Paul D. Goldenheim, Richard S. Sackler
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Publication number: 20030065195Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: ApplicationFiled: July 26, 2002Publication date: April 3, 2003Applicant: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 6541647Abstract: The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1 -butynyl)-tetrahydrofuran and precursors thereof.Type: GrantFiled: October 2, 2001Date of Patent: April 1, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Mukund Shankar Chorghade, Mukund Keshao Gurjar, Palakodety Radha Krishna, Sista Venkata Sai Lalitha, Kashinath Sadalapure, Susanta Sekhar Adhikari, Andappan Murugaiah Subbaiah Murugaiah, Sunil Vyankatesh Mhaskar, Gangavaram Vasantha Madhava Sharma, Tangallapally Rajendra Prasad, Punna Sreenivas, Vavilala Goverdhan Reddy, Aminul Islam, Chittineni Hari Prasad, Alla Venkata Rama Rao
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Publication number: 20030050337Abstract: This invention is related to a polymorphic B Form of 3-(cyclopropylmethoxy)-4-[4-(methylsulfonyl)phenyl]-5,5-dimethyl-5H-furan-2-one characterized by the following parameters: 1 cristalline system Trigonal space group R-3 description hexagonal unit-cell dimensions a (Å) 18.183 b (Å) 18.183 c (Å) 26.950 &agr; (°) 90 &bgr; (°) 90 &ggr; (°) 120 unit-cell volume (Å3) 7716.5 number of molecules per unit-cell Z 18 Temperature of measurement (° K) 293 calculated specific gravity 1.303 weight absorption coefficient (cm−1) 2.Type: ApplicationFiled: April 8, 2002Publication date: March 13, 2003Inventors: Beatrice Calais, Evelyne Chassagneux, Jean-Michel Bonard
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Patent number: 6531460Abstract: Compounds expressed by the following general formula (1), The compounds can be used as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension; alopecia, acne, psoriasis, dermatitis, hypercalcemia, hypoparathyroidism and metabolic disorder of cartilage.Type: GrantFiled: April 23, 2001Date of Patent: March 11, 2003Assignee: Teijin LimitedInventors: Kazuya Takenouchi, Qingzhi Gao, Kenji Manabe, Ryo Sogawa, Yasuhiro Takano, Seiichi Ishizuka
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Publication number: 20030028036Abstract: The invention relates to a method for producing compounds of general formula (I) wherein R1 is selected from the following groups: (a) OR5 and (b) mono-, di-, or tri-substituted phenyl; and R2 represents a group (C1-C6) alkyl. The method is characterized in that it comprises the following steps: a) reacting a compound of general formula (II) with an acid of general formula R1CH2 COOH (III) in a water-free medium; b) reacting the resulting compound with a strong base in an aprotic solvent in order to obtain an intermediate cyclic compound which forms a compound of general formula (I) after dehydration; and c) isolating said resulting compound of general formula (I).Type: ApplicationFiled: April 8, 2002Publication date: February 6, 2003Inventors: Laetitia Canali, Paul Cruciani, Gilles Oddon
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Patent number: 6512127Abstract: The present invention is directed towards a process for the preparation of enantiomerically enriched 4-hydroxymethyl-&ggr;-butyrolactone (I). By kinetic racemate cleavage of racemic epoxide of the general formula (II) wherein R represents a (C1-C8)-alkyl radical, a (C8-C16)-aryl radical, with a nucleophile and a Jacobsen catalyst there is obtained enantiomerically enriched (I). Use of the lactone so prepared.Type: GrantFiled: August 24, 2001Date of Patent: January 28, 2003Assignee: Degussa AGInventors: Kai Rossen, Stefan Eils
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Publication number: 20030008232Abstract: (Meth)acrylate compounds having a norbornane, bicyclo[2.2.2]octane, 7-oxanorbornane or cyclohexane ring structure and a &ggr;-butyrolactone ring structure connected together by a suitable linker are novel and useful in forming polymers having high transparency, especially at the exposure wavelength of an excimer laser.Type: ApplicationFiled: June 13, 2002Publication date: January 9, 2003Applicant: Shin-Etsu Chemical Co., Ltd.Inventors: Takeshi Kinsho, Koji Hasegawa, Takeru Watanabe
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Patent number: 6500961Abstract: Lactone compounds of formula (1) are useful as monomers to form base resins for use in chemically amplified resist compositions adapted for micropatterning lithography. R1 is H or C1-6 alkyl, R2 is H or an acyl or alkoxycarbonyl group of 1-15 carbon atoms which may be substituted with halogen atoms, Z is a divalent C1-15 organic group which forms a lactone ring with the carbonyloxy group, k is 0 or 1, and m is an integer from 0 to 5.Type: GrantFiled: May 31, 2001Date of Patent: December 31, 2002Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Takeshi Kinsho, Koji Hasegawa, Takeru Watanabe, Tsunehiro Nishi, Mutsuo Nakashima, Seiichiro Tachibana, Jun Hatakeyama
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Patent number: 6488818Abstract: A process for removing impurities from 3-(2′-acetoxyethyl)dihydro-2(3H)furanone (I), where the 3-(2′-acetoxyethyl)dihydro-2(3H)furanone containing the undesirable impurities is initially prepared in a manner known per se by acetylation of 3-(2′-hydroxyethyl)dihydro-2(3H)furanone and the resulting product is subsequently subjected to a distillation or rectification, includes carrying out the distillation or rectification in a plurality of steps, where high-boiling impurities are removed in a first step, the product which is drawn off via the top is subsequently subjected to at least one further step in which low-boilers and intermediate boilers are drawn off via the top and the desired pure I is obtained as bottom product.Type: GrantFiled: September 8, 1999Date of Patent: December 3, 2002Assignee: BASF AktiengesellschaftInventors: Volker Maywald, Horst Hartmann, Norbert Götz, Gernot Reissenweber, Hartmann König
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Patent number: 6465664Abstract: One aspect of the present invention relates to methods for the transition-metal-catalyzed asymmetric 1,4-addition of a nucleophile, e.g., hydride, to cyclic and acyclic enoates and enones. In certain embodiments of the methods of the present invention, the transition metal catalyst consists essentially of copper and an asymmetric bidentate bisphosphine ligand.Type: GrantFiled: September 13, 2000Date of Patent: October 15, 2002Assignee: Massachusetts Institute of TechnologyInventors: Stephen L Buchwald, Daniel H. Appella, Yasunori Moritani, Ryo Shintani, Valdas Jurkauskas
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Patent number: 6433197Abstract: The invention provides new methods for preparation of cyclic oxygen compounds, including 2,5-disubstituted tetrahydrofurans, 2,6-disubstituted tetrahydropyrans, 2,7-disubstituted oxepanes and 2,8-oxocanes. The invention also provides new cyclic oxygen compounds and pharmaceutical compositions and therapeutic methods that comprise such compounds.Type: GrantFiled: October 2, 2001Date of Patent: August 13, 2002Assignee: Millennium Pharmaceuticals, Inc.Inventors: Mukund Shankar Chorghade, Mukund Keshao Gurjar, Palakodety Radha Krishna, Sista Venkata Sai Lalitha, Kashinath Sadalapure, Susanta Sekhar Adhikari, Andappan Murugaiah Subbaiah Murugaiah, Batchu Venkateswara Rao, Levadala Murali Krishna, Sunil Vyankatesh Mhaskar, Gangavaram Vasantha Madhava Sharma, Tangallapally Rajendra Prasad, Punna Sreenivas, Vavilala Goverdhan Reddy, Aminul Islam, Alla Venkata Rama Rao, Hymavathi Lanka, Bethi Sridhar Reddy, Chittineni Hari Prasad
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Patent number: 6423850Abstract: The rate of aminolysis of butyrolactones is predictably adjusted by attaching a substituent having a known field effect value (F) to the alpha position before reacting the substituted buytrolactone with an amine. The aminolysis product is a gamma-hydroxy amide. The resulting materials are useful as the cross-linking agents in a variety of coatings and coatings processes.Type: GrantFiled: June 12, 2000Date of Patent: July 23, 2002Assignee: E.I. du Pont de Nemours and CompanyInventor: Albert Gordon Anderson
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Patent number: 6362346Abstract: This invention pertains to a process for making &agr;-methylene-&ggr;-butyrolactone by acid-catalyzed rearrangement of tetrahydro-3-furoic acid. In a further embodiment, when tetrahydro-3-furoic acid is treated with acetic anhydride and an acid catalyst, &agr;-acetoxymethyl-&ggr;-butyrolactone is produced in high yield. Under basic conditions, &agr;-acetoxymethyl-&ggr;-butyrolactone can readily form&agr;-methylene-&ggr;-butyrolactone by the elimination of acetic acid. These reactions provide &agr;-methylene-&ggr;-butyrolactone by novel routes which do not require butyrolactone or formaldehyde.Type: GrantFiled: November 10, 2000Date of Patent: March 26, 2002Assignee: E. I. du Pont de Nemours and CompanyInventors: Dale Robert Coulson, David L. Thorn, Mark A. Scialdone
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Patent number: 6346629Abstract: Process for producing butyrolactones of the general formula I where R1 and R2 are each hydrogen, alkyl, hydroxyalkyl, substituted or unsubstituted aryl or substituted or unsubstituted trialkylsilyl, by reacting alkynes of the general formula II where R1 and R2 are each as defined above, with carbon monoxide and water in the presence of a rhodium catalyst under pressures from 20 to 300 bar and hydrogenating the unhydrogenated 2(5H)-furanone intermediates comprises a) reacting the carbonylation reaction mixture with hydrogen at from 150 to 250° C. and from 100 to 300 bar, b) removing the precipitated catalyst and returning it into the carbonylation reaction, and c) subjecting the catalyst-free reaction mixture to a distillation to recover the butyrolactone.Type: GrantFiled: November 15, 2000Date of Patent: February 12, 2002Assignee: BASF AktiengesellschaftInventors: Melanie Brunner, Ralf-Thomas Rahn, Udo Rheude, Jochem Henkelmann
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Patent number: RE38324Abstract: Preparation of 4-hydroxy substituted butyrolactones is described. A process for the preparation of 3-hydroxybutyrolactone, 1.2.4-trihydroxybutane and 3,4-dihydroxy acid methyl ester from malic acid is particularly described. The preparation of 4-hydroxymethyl-4-hydroxybutyric acid -1-methyl ester and 4-hydroxymethyl butyrolactone is particularly described. The compounds are intermediates to various pharmaceutical and agricultural products.Type: GrantFiled: March 28, 2002Date of Patent: November 18, 2003Assignee: Board of Trustees of Michigan State UniversityInventor: Rawle I. Hollingworth