Alicyclic Acid Moiety Containing N, S, P, B Or Halogen Patents (Class 560/125)
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Patent number: 7179934Abstract: Certain ?-amino acids that bind to the alpha-2-delta (?2?) subunit of a calcium channel are disclosed. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders. Also disclosed are methods of making the ?-amino acids.Type: GrantFiled: September 24, 2004Date of Patent: February 20, 2007Assignee: Warner-Lambert Company LLCInventors: Peter Garth Blazecka, Joseph Richard Bozelak, Norman Lloyd Colbry, Timothy Thomas Curran, Annise Paige Goodman, Kevin E. Henegar, Garrett Hoge, Paul D. Johnson, Augustine Tobi Osuma, Mark Stephen Plummer, Jacob Bradley Schwarz, Derek Clinton Vrieze, Ji Zhang
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Patent number: 7144939Abstract: The use of organic based nucleating agents to induce certain specific polymer orientations into the molded polypropylene articles such that the resultant part has improved stiffness-impact properties without sacrificing other attributes of the polypropylene is provided. Such results have been obtained through the utilization of low amount of organic nucleating compounds, including, without limitation, specific metal salts of hexahydrophthalic acid (hereinafter HHPA). Furthermore, such nucleating compounds have been found to impart, again in such low added amounts, heretofore unforeseen levels of b-axis crystalline orientation which translates into improved physical properties as well.Type: GrantFiled: July 29, 2003Date of Patent: December 5, 2006Assignee: Milliken & CompanyInventors: Darin L. Dotson, Brian M. Burkhart
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Patent number: 7141695Abstract: The invention relates to methods for producing substituted acrylic acid esters and to the use of the latter for producing substituted ?-amino acids, such as gabapentin and pregabalin. The substituted acrylic acid esters are produced by Wadsworth-Emmons olefination with trialkyl phosphonoacetate in the presence of alkali carbonate as the base, in an aqueous solvent.Type: GrantFiled: July 19, 2004Date of Patent: November 28, 2006Assignee: Grunenthal GmbHInventors: Michael Thomas Przewosny, Claudia Pütz
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Patent number: 7109370Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which A, B, G, X, Y, Z and W are each as defined in the description, to processes and intermediates for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: April 11, 2005Date of Patent: September 19, 2006Assignee: Bayer AktiengesellschaftInventors: Hermann Hagemann, Reiner Fischer, Christoph Erdelen, Ulrike Wachendorff-Neumann, Udo Schneider, Wolfram Andersch
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Patent number: 7109383Abstract: The invention relates to a fluorine-containing allyl ether compound represented by the formula 1, wherein R represents an organic group containing at least one fluorine atom and an alicyclic structure. The invention further relates to a fluorine-containing copolymer containing a first unit derived from the fluorine-containing allyl ether represented by the formula 1; and a second unit derived from a vinyl monomer.Type: GrantFiled: September 26, 2003Date of Patent: September 19, 2006Assignee: Central Glass Company, LimitedInventors: Satoru Kobayashi, Katsunori Kawamura, Kazuhiro Yamanaka, Haruhiko Komoriya, Kazuhiko Maeda
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Patent number: 7064231Abstract: The invention relates to stereoisomerically enriched diamines, to metal complexes comprising these diamines and also to their use in a process for asymmetrically reducing ketones using silanes, in particular polymethylhydrosiloxane, as reducing agents.Type: GrantFiled: August 19, 2003Date of Patent: June 20, 2006Assignee: Bayer AktiengesellschaftInventor: Jürgen Köcher
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Patent number: 6951955Abstract: The invention is a process for the preparation of compounds of the Formula I: where R1, R2, R3, R4 and R5 are defined in the specification, which are intermediates useful for the preparation of tubulin inhibitors which are useful in the treatment of cancer.Type: GrantFiled: September 18, 2003Date of Patent: October 4, 2005Assignee: Wyeth Holdings CorporationInventors: Yanzhong Wu, Sreenivasulu Megati, Constantine Gletsos, John Thomas Kendall, Bogdan Kazimierz Wilk, Thurairajah Padmanathan, Panolil Raveendranath
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Patent number: 6946474Abstract: The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such compounds for the treatment of disease states in which glycine is involved.Type: GrantFiled: September 13, 2001Date of Patent: September 20, 2005Assignee: Merck & Co., Inc.Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
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Patent number: 6939986Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.Type: GrantFiled: February 22, 2002Date of Patent: September 6, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Martin Karpf, René Trussardi
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Patent number: 6884821Abstract: Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the derivatives as the active ingredient. In said formula, R1 is hydrogen, hydroxyl, alkyl, or the like; L is a single bond, a double bond, alkylene, or the like; M is a single bond, alkylene, or the like; T is a single bond, alkylene, or the like; W is carboxyl, —CON(RW1)RW2, or the like; represents a single or double bond; X is oxygen, alkenylene, or the like; Y is an aromatic hydrocarbon group which may contain a heteroatom, or the like; and Z is an aromatic hydrocarbon group which may contain a heteroatom.Type: GrantFiled: September 29, 2000Date of Patent: April 26, 2005Assignee: Eisai Co., Ltd.Inventors: Masanobu Shinoda, Eita Emori, Fumiyoshi Matsuura, Toshihiko Kaneko, Norihito Ohi, Shunji Kasai, Hideki Yoshitomi, Kazuto Yamazaki, Sadakazu Miyashita, Taro Hibara, Takashi Seiki, Richard Clark, Hitoshi Harada
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Patent number: 6849756Abstract: The invention includes selected novel optically active ?-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: GrantFiled: February 14, 2003Date of Patent: February 1, 2005Assignee: Monsanto CompanyInventor: John J. Talley
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Publication number: 20040229882Abstract: Compounds having the formula (I), 1Type: ApplicationFiled: October 29, 2003Publication date: November 18, 2004Inventors: Guixue Yu, John Macor, Timothy Herpin, R. Michael Lawrence, George C. Morton, Rejean Ruel, Graham S. Poindexter, Edward H. Ruediger, Carl Thibault
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Patent number: 6784310Abstract: A crystallization is carried out by adding a solution of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxylic anhydride in a good solvent to an aliphatic hydrocarbon solvent while inhibiting the oil formation and scaling of said N-carboxylic anhydride. Further, a crystallization is carried out by adding an aliphatic hydrocarbon solvent sequentially to a solution of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine N-carboxylic anhydride in a good solvent over not less than ¼ of an hour and at a temperature of not higher than 60° C.Type: GrantFiled: April 24, 2002Date of Patent: August 31, 2004Assignee: Kaneka CorporationInventor: Masafumi Fukae
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Patent number: 6777573Abstract: A method has been developed for the preparation of ceralure B1, a potent attractant for the Mediterranean fruit fly. The method utilizes trans-siglure acid as starting material to produce iodolactone which is subsequently reduced to lactone. The lactone is converted to a mixture of epimers ceralure A acid and ceralure B1 acid. The ceralure A acid is recyclized to lactone, leaving epimer ceralure B1 acid intact. Following separation from lactone, the ceralure B1 acid is esterified to produce ceralure B1 of about 92-94% purity. The overall yield is about 58-65%, a significant improvement over currently known methods which result in yields of about 30-33%.Type: GrantFiled: September 26, 2002Date of Patent: August 17, 2004Assignee: The United States of America as represented by the Secretary of AgricultureInventor: Ashot Khrimian
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Patent number: 6770676Abstract: The present invention relates to 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives represented by the formula: the pharmaceutically acceptable salts thereof, or the hydrates thereof. The compounds of the present invention are useful as a medicament, and in particular, are useful as modulators acting on group 2 metabotropic glutamate receptors, having effects for treating and/or preventing psychiatric disorders such as schizophrenia, anxiety and its associated diseases, depression, bipolar disorder, and epilepsy; and/or neurological diseases such as drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, dyskinesia associated with muscular stiffness, cerebral ischemia, cerebral failure, myelopathy, and head trauma.Type: GrantFiled: December 6, 2002Date of Patent: August 3, 2004Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kosuke Kanuma, Kazunari Sakagami
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Publication number: 20040138272Abstract: Allylic compounds represented by the formula (I) are provided, 1Type: ApplicationFiled: August 29, 2003Publication date: July 15, 2004Inventors: Lisa McKerracher, Eryk Thouin, William D. Lubell
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Patent number: 6753445Abstract: A compound selected from 14—O—[(cycloalkyl-sulfanyl)acetyl]mutilins; 14—O—[(cycloalkyl-alkyl-sulfanyl)acetyl] mutilins; 14—O—[(cycloalkoxy)acetyl] mutilins; and 14—O—[(cycloalkyl-alkoxy)acetyl] mutilins and its use as a pharmaceutical.Type: GrantFiled: January 9, 2003Date of Patent: June 22, 2004Assignee: Biochemie Gesellschaft m.b.H.Inventors: Gerd Ascher, Heinz Berner
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Patent number: 6720400Abstract: The present invention relates to an improved process for the continuous preparation of polyisocyanates with a biuret structure comprising the steps of continuously reacting excess amounts of organic diisocyanates having exclusively aliphatically and/or cycloaliphatically bound isocyanate groups with organic diamines having exclusively aliphatically and/or cycloaliphatically bound primary amino groups at temperatures above 170° C. and adding acid before or during the reaction.Type: GrantFiled: May 15, 2001Date of Patent: April 13, 2004Assignee: Bayer AktiengesellschaftInventors: Reinhard Halpaap, Dieter Mager, Siegfried Oeckl, Harald Mertes
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Publication number: 20040063994Abstract: Amino Acids of formula (1) having high purity, free from the corresponding lactams and chloride anions obtained by reduction of oxyaminoacids of formula (II) 1Type: ApplicationFiled: October 20, 2003Publication date: April 1, 2004Inventors: Paolo Rossi, Emilia Vecchio
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Patent number: 6703520Abstract: The present invention provides a process for preparing a desired halogenated ester, which process comprises the steps of: (a) contacting (A) a substantially organic solvent free liquid mixture of (i) an alkanolate of the formula M—O—Z, wherein M is an alkali or alkaline earth metal, and Z is a linear, branched or cyclic alkyl group of 1 to 10 carbon atoms and (ii) a diester with (B) a halogenated ethylenically unsaturated olefin at a temperature of not more than 40° C. and with a mol ratio of halogenated ethylenically unsaturated olefin to alkanolate of not more than 1.1; (b) contacting an acid with a thus obtained reaction mixture thereby obtaining a mixture comprising the desired halogenated ester; and (c) recovering the halogenated ester from said reaction mixture.Type: GrantFiled: April 5, 2002Date of Patent: March 9, 2004Assignee: 3M Innovative Properties CompanyInventors: Klaus Hintzer, Egon Obermaier, Werner Schwertfeger
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Publication number: 20040039223Abstract: The invention relates to novel 4-alkoxy-cyclohexane-1-amino-carboxylic esters of the formula (IV) 1Type: ApplicationFiled: January 3, 2003Publication date: February 26, 2004Inventors: Thomas Himmler, Reiner Fischer, Bernd Gallenkamp, Hans-Joachim Knops, Lubbertus Mulder
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Patent number: 6689898Abstract: This invention relates to novel compounds of the formula: wherein R1 is H or C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; R2 and R3 are each independently C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; X is Cl, Br or I; or stereoisomers thereof.Type: GrantFiled: March 22, 2002Date of Patent: February 10, 2004Assignee: Aventis Pharmaceuticals Inc.Inventor: Timothy A. Ayers
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Publication number: 20040024224Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: ApplicationFiled: May 15, 2003Publication date: February 5, 2004Applicant: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Debendra K. Mohapatra
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Publication number: 20030162831Abstract: A compound selected from 14—O—[(cycloalkyl-sulfanyl)acetyl]mutilins; 14—O—[(cycloalkyl-alkyl-sulfanyl)acetyl] mutilins; 14—O—[(cycloalkoxy)acetyl] mutilins; and 14—O—[(cycloalkyl-alkoxy)acetyl] mutilins and its use as a pharmaceutical.Type: ApplicationFiled: January 9, 2003Publication date: August 28, 2003Inventors: Gerd Ascher, Heinz Berner
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Patent number: 6608061Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.Type: GrantFiled: February 14, 2000Date of Patent: August 19, 2003Assignees: Kyoma Hakko Kogyo Co., Ltd., Fuji Photo Film Co., Ltd.Inventors: Yoshiyuki Yonetani, Takeshi Takahashi, Yuko Kanda, Tamio Mizukami, Tatsuya Tamaoki, Shun-ichi Ikeda, Masanobu Takashima, Naoki Asanuma, Tadashi Inaba, Hiroshi Takeuchi, Hiroshi Kawamoto, Yoshihisa Tsukada, Masato Satomura, Hiroshi Kitaguchi
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Patent number: 6599971Abstract: Compounds and compositions comprising specific metal salts of hexahydrophthalic acid (HHPA) in order to provide highly desirable properties within thermoplastic articles are provided. The inventive HHPA derivatives are useful as nucleating and/or clarifying agents for such thermoplastics, are practical and easy to handle. Such compounds provide excellent crystallization temperatures, stiffness, and acid scavenger compatibility within target polyolefins. Also, such compounds exhibit very low hygroscopicity and therefore excellent shelf stability as powdered or granular formulations. Thermoplastic additive compositions and methods of producing polymers with such compounds are also contemplated within this invention.Type: GrantFiled: March 29, 2001Date of Patent: July 29, 2003Assignee: Milliken & CompanyInventors: Darin L. Dotson, X. Edward Zhao
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Patent number: 6593314Abstract: The present invention provides compounds of formula Ia and Ib or a pharmaceutically acceptable salt, prodrug, or ester thereof, useful in the inhibition of neuraminidase enzymes from disease-causing microorganisms, especially influenza neuraminidase, pharmaceutical formulations containing same, processes and intermediates for preparing said compounds, as well as methods of using said compounds, including preventing and treating diseases caused by microorganisms having said neuraminidase enzyme.Type: GrantFiled: September 22, 2000Date of Patent: July 15, 2003Assignee: Abbott LaboratoriesInventors: Clarence J. Maring, Vincent L. Giranda, Yu Gui Gu, Stephen Hanessian, Dale J. Kempf, Darold L. Madigan, Kent Stewart, Vincent S. Stoll, Minghua Sun, Gary T. Wang, Jianchio Wang, Chen Zhao
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Patent number: 6586626Abstract: The invention provides a process for producing a fluorine-containing compound from an inexpensive material. Namely, Compound I such as RACH2OH is reacted with Compound II such as XCORB to form Compound III such as RACH2OCORB, followed by fluorination in a liquid phase to form Compound IV such as RAFCF2OCORBF, which is converted to Compound V such as RAFCOF and/or Compound VI such as RBFCOF. RA is an alkyl group or the like, RB is a perhalogenoalkyl group or the like, RAF and RBF are fluorinated RA and RB, and X is halogen.Type: GrantFiled: September 24, 2001Date of Patent: July 1, 2003Assignee: Asahi Glass Company, LimitedInventors: Takashi Okazoe, Kunio Watanabe, Shin Tatematsu, Hidenobu Murofushi
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Patent number: 6583216Abstract: The present invention relates to blocked polyisocyanate cross-linking agents and their use in one-component stoving lacquers, in particular in solvent-containing or predominantly water-based plastics coatings having a soft-feel effect.Type: GrantFiled: June 3, 2002Date of Patent: June 24, 2003Assignee: Bayer AktiengesellschaftInventors: Eberhard König, Claus Kobusch, Uwe Klippert, Wolfram Küttner
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Patent number: 6559334Abstract: The invention relates to novel optically active polymerizable dipeptides, to the process for the preparation thereof, to the polymerization thereof and to the use of the polymers as adsorbents for the chromatographic separation of enantiomers.Type: GrantFiled: August 12, 1994Date of Patent: May 6, 2003Assignee: Bayer AktiengesellschaftInventors: Walter Lange, Michael Grosse-Bley, Bruno Bömer, Rolf Grosser, Franz-Peter Hoever
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Patent number: 6555708Abstract: There are provided cosmetics which have not only a reduced effect on the “gleam” caused by irregular light reflection but also a reduced effect on “stickiness” based on an oil raw material, giving a good feeling during use such as spreadability, etc., and being excellent in the sustaining of the makeup effect. There are used N&egr;-long chain acyllysine crystals whose average diameter or mode diameter lies in the range of 3˜15 &mgr;m without being subjected to the mechanical pulverization.Type: GrantFiled: February 19, 2002Date of Patent: April 29, 2003Assignee: Ajinomoto Co., Inc.Inventors: Naoya Yamato, Yasunori Atarashi, Keigo Sano
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Patent number: 6541654Abstract: The invention includes selected novel optically active &agr;-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: GrantFiled: October 11, 2001Date of Patent: April 1, 2003Assignee: Monsanto CompanyInventor: John J. Talley
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Publication number: 20030018070Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof:Type: ApplicationFiled: February 14, 2000Publication date: January 23, 2003Inventors: YOSHIYUKI YONETANI, TAKESHI TAKAHASHI, YUKO KANDA, TAMIO MIZUKAMI, TATSUYA TAMAOKI, SHUN-ICHI IKEDA, MASANOBU TAKASHIMA, NAOKI ASANUMA, TADASHI INABA, HIROSHI TAKEUCHI, HIROSHI KAWAMOTO, YOSHIHISA TSUKADA, MASATO SATOMURA, HIROSHI KITAGUCHI
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Patent number: 6495711Abstract: The invention relates to a process for preparing (−)-(1S,4R) N protected 4-amino-2-cylcopentene-1-carboxylate esters represented by the formula (I) wherein R1 and R2 are as described within the specification.Type: GrantFiled: December 18, 2001Date of Patent: December 17, 2002Assignee: BioCryst Pharmaceuticals Inc.Inventors: Max Rey, Gregor Welti, Cynthia Maryanoff
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Patent number: 6479694Abstract: As process for the preparation of a cyclic carbamate of formula (1), comprises treatment of a cyclopentene of formula (2) wherein R1 is H or an organic group of up to 20 C atoms and R2 is C1-10 alkyl, aralkyl or aryl, with a source of halogen and a base.Type: GrantFiled: August 7, 2001Date of Patent: November 12, 2002Assignee: Chirotech Technology, Ltd.Inventor: Michael Lloyd
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Patent number: 6479627Abstract: An object of the present invention is to provide an aqueous solution of lactoferrin which can be preserved for a long period of time. The aqueous preparation according to the present invention is an aqueous preparation which is characterized by containing a polyvalent inorganic or organic acid or a salt thereof whereby stability of lactoferrin is improved and is an aqueous preparation in which concentration of the polyvalent inorganic or organic acid or a salt thereof is 0.005% (w/v) or more. In the case of ophthalmic solutions, for example, the polyvalent inorganic or organic acid or a salt thereof is preferably 0.01-3.0% (w/v), particularly preferably 0.1-1.0% (w/v).Type: GrantFiled: January 31, 2000Date of Patent: November 12, 2002Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Atsutoshi Ota, Mitsuaki Kuwano, Hiroyuki Asada
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Patent number: 6465686Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: April 13, 2001Date of Patent: October 15, 2002Assignee: Pharmacia CorporationInventors: Margaret L. Grapperhaus, James A. Sikorski, Alok K. Awasthi, Lijuan J. Wang, Barnett S. Pitzele, Donald W. Hansen, Jr., Pamela T. Manning
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Patent number: 6465689Abstract: This invention is novel processes for the stereoselective preparation of gabapentin analogues.Type: GrantFiled: December 8, 1999Date of Patent: October 15, 2002Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, Andrew Ian Morrell
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Patent number: 6462226Abstract: A new process for the preparation of 4,5-diamino shikimic acid derivatives starting from 4-amino-5-azido shikimic acid derivatives is provided. 4,5-diamino shikimic acid derivatives and its pharmaceutically acceptable addition salts are potent inhibitors of viral neuraminidase.Type: GrantFiled: November 17, 2000Date of Patent: October 8, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Hans-Juergen Mair
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Patent number: 6452038Abstract: The present invention provides a compound according to the formula: CH2═C(R1)—C(O)—R6—NHCO2(CH2)p(CF2)q—O—((CF2)aCFXO)m(CF2)r—Z wherein each R1 is independently selected from —H, —CH3, —F and —Cl, wherein each R6 is independently selected from substituted or unsubstituted C1-C10 alkyl, cyclic alkyl, or aryl groups, wherein each a is independently selected from 0-3, wherein each X is independently selected from —F, —CF3 or —CF2CF3, wherein each p is independently selected from 1-4, each q is independently selected from 1-5, each r is independently selected from 1-5, each m is independently selected from 1-50, each Z is independently selected from —F and —(CH2)sOH, and each s is independently selected from 1-4. The present invention also provides for the use of this compound as a surfactant in highly fluorinated liquid solvents. Latexes of dispersed particles utilizing this surfactant are provided.Type: GrantFiled: June 28, 2000Date of Patent: September 17, 2002Assignee: 3M Innovative Properties CompanyInventors: Prabhakara Satyauolu Rao, Naiyong Jing
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Publication number: 20020115721Abstract: Disclosed are prodrug compounds of a class of alkyl carboxy amino acid analogs of glutamic acid that act as specific regulators of the kainate EAA receptor cation channel. These compounds are useful for treating neurological, neuropsychological, neuropsychiatric, neurodegenerative, neuropsychopharmacological and functional disorders associated with excessive or insufficient activation of the kainate subtype of the ionotropic EAA receptors; treating cognitive disorders associated with deactivation, suboptimal activation or over-activation of the kainate receptor; alleviating pain and improving and enhancing memory, learning, and associated mental processes.Type: ApplicationFiled: October 30, 2001Publication date: August 22, 2002Applicant: Annovis, Inc.Inventors: Xue-Feng Pei, Maria-Luisa Maccecchini
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Patent number: 6437171Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds of formula wherein R1, R1′, R2, R2′, R3 and R4 have the meaning given in the specification and pharmaceutically acceptable addition salts thereof, from 1,2-epoxides of formula wherein R1, R′, R2 and R2′ have the meaning given in the specification.Type: GrantFiled: June 8, 2000Date of Patent: August 20, 2002Assignee: Hoffman-La Roche Inc.Inventors: Martin Karpf, René Trussardi
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Publication number: 20020107208Abstract: The present invention relates to novel prodrugs of gabapentin and to pharmaceutical formulations and sustained release formulations containing the prodrugs.Type: ApplicationFiled: October 23, 2001Publication date: August 8, 2002Inventors: Chih-Ming Chen, Jane Chen
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Patent number: 6403824Abstract: The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula wherein R1, R2, R3 and R4 are defined in the specification, starting from furan. 4,5-Diamino shikimic acid derivatives are potent inhibitors of viral neuraminidase.Type: GrantFiled: February 6, 2001Date of Patent: June 11, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Stefan Abrecht, Martin Karpf, René Trussardi, Beat Wirz
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Patent number: 6399808Abstract: A method of preparing carbamates of the general formula RR′—N—CO2—R″ by reacting an amine with carbon dioxide and an organic electrophile in an anhydrous solvent in the presence of a cesium base, whereby carbamate synthesis is accomplished in good yield at mild temperatures, either in solution or on a solid support, and wherein R, R′, and R″ are hydrogen, alkyl of 1-18 carbon atoms, silyl, phenyl, benzyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, allyl, or heterocycle, which are widely used as industrial products, and as intermediates in organic synthesis.Type: GrantFiled: February 25, 2000Date of Patent: June 4, 2002Assignee: University of South FloridaInventor: Kyung Woon Jung
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Patent number: 6399810Abstract: Methyl cyclohexyl-propionate is prepared by the hydrogenation of methyl cinnamate in the presence of a ruthenium and/or palladium catalyst.Type: GrantFiled: August 15, 2000Date of Patent: June 4, 2002Assignee: Haarmann & Reimer GmbHInventors: Walter Kuhn, Hans-Ulrich Funk, Gerhard Senft, Wolfgang Kiel
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Patent number: 6392086Abstract: The present inventions relate to a (1S,5R,6S)- or (1SR, 5RS, 6SR)-3-fluoro-2-oxobicyclo[3.1.0]hex-3-ene-6-carboxylic acid derivative represented by Formula (1): [in the formula, R represents OR1 or NR1R2, wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a (C3-C6 cycloalkyl) (C1-C6 alkyl) group, an aryl group, an aryl (C1-C6 alkyl) group, a (C1-C6 alkoxy) (C1-C6 alkyl) group, a C1-C6 hydroxyalkyl group, a (C1-C6 alkylthio) (C1-C6 alkyl) group, or a C1-C6 mercaptoalkyl group], and a process for producing the same, and a process for efficiently producing a fluorine-containing amino acid compound acting on group 2 metabotropic glutamate receptors, which has treatment effects or prevention effects on psychiatric diseases or neurological diseases, characterized by hydrogenating the derivative, and subsequently, subjecting it to hydantoination or aminocyanidation, followed by hydrolysis.Type: GrantFiled: June 7, 2001Date of Patent: May 21, 2002Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa, Hisanako Ito, Takeo Taguchi
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Patent number: 6388041Abstract: Disclosed are polyoxyethylene derivatives having different functional groups at both ends of the molecule represented by the following formula (I) and a process for producing the derivatives by anionic living polymerization. The present invention provides polymers which are especially suitable for use as medical materials. wherein A′ and B′ are organosilyl type amino-protecting groups, R is a hydrogen atom or a C1-6 alkyl group, and Y is a hydrogen atom, an alkali metal or a certain functional group.Type: GrantFiled: November 7, 2000Date of Patent: May 14, 2002Assignee: Nano Carrier Co LtdInventors: Kazunori Kataoka, Masao Kato, Yukio Nagasaki, Takahisa Hayashida, Michihiro Iijima, Teruo Okano
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Patent number: 6375943Abstract: A method of attracting the Mediterranean fruit fly by subjecting the Mediterranean fruit fly to an attractant, wherein the attractant is ethyl (1R,2R,5R)-5-iodo-2-methylcyclohexane-1-carboxylate in an enantomeric excess of at least 70% and a regio- and diastereochemical purity of >5:1. The compound ethyl (1R,2R,5R)-5-iodo-2-methylcyclohexane-1-carboxylate, in an enantomeric excess of at least 70% and a regio- and diastereochemical purity of >5:1, may be stereoselectively synthesized on a multigram scale in 15% yield by reacting ethyl (1R,2R,5S)-5-hydroxy-2-methyl-1-carboxylate with Ph3P-imidazole-I2 (or Ph3P-2,6-lutidine-I2) in a carbon tetrachloride/methlylene chloride mixture. The 1R,2R,5R enantiomer is significantly more attractive than its enantiomeric counterpart (1S,2S,5S), or either of the commercial products trimedlure or ceralure, each a mixture of 16 regio and stereoisomers.Type: GrantFiled: March 15, 2000Date of Patent: April 23, 2002Assignee: The United States of America as represented by the Secretary of AgricultureInventors: Andre S. Raw, Eric B. Jang
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Patent number: 6369194Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.Type: GrantFiled: November 9, 1998Date of Patent: April 9, 2002Assignee: Yale UniversityInventor: Harry H. Wasserman