And Is Bonded Directly To A Ring Carbon Which Is Adjacent To The Ring Nitrogen Of The Five-membered Hetero Ring (e.g., 4-hydroxy Proline, Etc.) Patents (Class 548/532)
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Publication number: 20100048545Abstract: The invention relates to 4-hydroxyisoleucine, isomers, analogs, lactones, salts, and prodrugs thereof, to processes for their preparation, and to pharmaceutical compositions comprising the same. More particularly, the invention relates to the use of those compounds in the prevention and treatment of disorders of fat metabolism and related syndromes. The invention further relates to the use of those compounds in the prevention and treatment of obesity and related syndromes including, but not limited to, the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body weight, and more particularly loss of body fat.Type: ApplicationFiled: March 22, 2007Publication date: February 25, 2010Applicant: INNODIA INC.Inventors: Lucie Jette, Patricia Mcnicol, Manjinder Gill, André Marette
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Publication number: 20100029609Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1-R5, R10 and X1-X7 are as defined in the specification.Type: ApplicationFiled: September 6, 2007Publication date: February 4, 2010Inventors: Frederic Berst, Philipp Grosche, Philipp Janser, Frederic Zecri, Birgit Bollbuck
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Publication number: 20100016295Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: July 31, 2006Publication date: January 21, 2010Applicant: Bayer Healthcare LLCInventors: Roger A. Smith, Derek Lowe, Tatiana Shelekhin, Georgiy Bondar, Philip Coish, Stephen J. O'Connor
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Publication number: 20090306407Abstract: [Problems] To provide a pyrrolidine analogue having an inhibitory activity on the induction of allodynia, a method for producing the pyrrolidine analogue, and an agent for preventing a neurogenic pain. [Means for Solving the Problems] A pyrrolidine analogue which is a compound represented by the general formula (I) [wherein HOOC-? represents an aromatic substituent having at least one carboxy group attached to the benzene ring] or a salt or ester of the compound. The compound has a potent inhibitory effect on the induction of allodynia.Type: ApplicationFiled: May 23, 2007Publication date: December 10, 2009Applicants: Gifu University, Kansai Medical University, Osaka Medical CollegeInventors: Masaaki Suzuki, Kyouji Furuta, Toshiaki Minami, Seiji Ito
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Patent number: 7615635Abstract: Novel N-formyl hydroxylamine compounds and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed.Type: GrantFiled: May 22, 2006Date of Patent: November 10, 2009Assignees: Novartis AG, Vicuron Pharmaceuticals, Inc.Inventors: Kathryn Rene Bracken, Simon Bushell, Karl Dean, Charles Francavilla, Rakesh K. Jain, Kwangho Lee, Mohindra Seepersaud, Lei Shu, Arathi Sundaram, Zhengyu Yuan
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Patent number: 7612068Abstract: The present invention relates to compounds of formula I wherein the substituents are as defined below. The compounds of formula I are useful for the treatment of diseases such as schizophrenia, including both the positive and the negative symptoms of schizophrenia and other psychoses.Type: GrantFiled: April 27, 2004Date of Patent: November 3, 2009Assignee: H. Lundbeck A/SInventors: Garrick P. Smith, Gitte K. Mikkelsen, Kim Andersen, Daniel R. Greve, Jorgen Eskildsen
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Publication number: 20090209585Abstract: The present invention relates to a cycloalkene derivative represented by the formula (I): wherein each symbol is as defined in the specification, a pharmaceutical agent containing the derivative, and a production method thereof. The cycloalkene derivative of the present invention has high solubility in water and is suitable for use as an injection.Type: ApplicationFiled: July 6, 2007Publication date: August 20, 2009Inventors: Takashi Ichikawa, Tomoyuki Kitazaki, Norikazu Tamura
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Publication number: 20090163719Abstract: There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group V heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or diastereomer in the product composition being greater than the ratio of second to first enantiomer or diastereomer in the enantiomerically enriched composition.Type: ApplicationFiled: October 27, 2005Publication date: June 25, 2009Inventors: Andrew John Blacker, Matthew John Stirling
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Publication number: 20090163705Abstract: Cyclic lipid moieties are described herein.Type: ApplicationFiled: May 20, 2008Publication date: June 25, 2009Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottahil G. Rajeev, Muthusamy Jayraman, K. Narayanannair Jayaprakash
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Publication number: 20090163555Abstract: Novel pyroglutamic acid derivatives (I), wherein R1 is —OH, —ORa, wherein Ra is alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl or heterocyclyl; R2, R3 and R4 are independently H, a nitrogen protecting group which hydrolyzes under acidic conditions or phtalamide; X is a pharmaceutically acceptable anion; and Y is a N-containing group; either in the form of their isolated optically active stereoisomers or in the form of mixtures thereof, are useful compounds for enhancing an immuneresponse in a subject and/or for treating tumours, bacterial, fungal or viral infections, or autoimmune diseases.Type: ApplicationFiled: April 20, 2007Publication date: June 25, 2009Applicant: PRODIMED, S.A.Inventors: Julio Álvarez Builla Gómez, José Luis Novella Robisco, Ma Paz Matia Martin, Sonia Serna Pereda
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Patent number: 7528264Abstract: Hydride process for making acyclic diol intermediates from cyclic intermediates, useful in antibacterial quinolone synthesis.Type: GrantFiled: March 26, 2007Date of Patent: May 5, 2009Assignee: The Procter & Gamble CompanyInventors: Michael Patrick Hayes, Tammy Talbot Schunk
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Publication number: 20080312456Abstract: The present invention relates to processes for preparing peptides and to intermediates involved in such processes, e.g. a process for preparing a compound of formula VIII wherein R12 and R13 are as defined herein.Type: ApplicationFiled: August 25, 2008Publication date: December 18, 2008Inventors: Bernhard Wietfeld, Walter Prikoszovich, Bernhard Erb, Werner Pachinger
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Publication number: 20080293753Abstract: The invention relates to quaternary ?-aminocarboxyamide derivatives of formula (I), wherein R1, R2, R3, R4, R5, R6, X, q and n are as defined in claim 1, for treating diseases and conditions mediated by modulation of voltage-gated sodium channels.Type: ApplicationFiled: October 6, 2006Publication date: November 27, 2008Inventors: Giuseppe Alvaro, David Amantini, Markus Bergauer, Francesca Bonetti, Roberto Profeta
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Patent number: 7449587Abstract: The present invention relates to processes for preparing peptides and to intermediates involved in such processes, e.g. a process for preparing a compound of formula VIII wherein R12 and R13 are as defined herein.Type: GrantFiled: August 16, 2007Date of Patent: November 11, 2008Assignee: Novartis AGInventors: Bernhard Wietfeld, Walter Prikoszovich, Bernhard Erb, Werner Pachinger
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Patent number: 7449547Abstract: A process for the total synthesis of Distamycin, and synthetic poly-(4 aminopyrrole-2-carboxamide) congeners thereof, using 1-methyl-4-forinylamino-2-pyrrolecarbonyl chloride iteratively as an intermediate, is provided. The process finds application for both in solution and solid support synthetic technologies.Type: GrantFiled: May 28, 2004Date of Patent: November 11, 2008Assignee: Naxopharma S.r.l.Inventor: Paolo Lombardi
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Publication number: 20080188546Abstract: In accordance with the present invention, there are provided a preventive or of preventing or therapeutic agent for decubitus comprising an N-acylated derivative of hydroxyproline or a salt thereof; the above preventive or therapeutic agent wherein the N-acylated derivative of hydroxyproline or a salt thereof is contained in an amount of 0.1 to 15% by weight to the total weight; and the preventive or therapeutic agent for decubitus wherein the N-acylated group of the N-acylated derivative of hydroxyproline is an N-acylated group having 1 to 24 carbon atoms.Type: ApplicationFiled: February 8, 2008Publication date: August 7, 2008Inventors: Toshiaki Takeda, Kenjiro Shimada, Hideo Kawabe, Takeshi Shibasaki, Tomoya Takahashi
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Patent number: 7405297Abstract: A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of the formula (II) with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX), to form a compound of formula (XX) The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).Type: GrantFiled: March 9, 2007Date of Patent: July 29, 2008Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Patent number: 7390910Abstract: The invention provides compounds of formula (I): wherein E, A, B?, R6, R7, R8, and R9 are defined in the specification which compounds exhibit anticancer activity and are useful for treating cancer.Type: GrantFiled: August 4, 2004Date of Patent: June 24, 2008Assignee: WyethInventors: Arie Zask, Joshua Kaplan, Ayako Yamashita, Chuan S. Niu, Gary Harold Birnberg, Emily Norton, Kinwang Cheung, Ronald Suayan, Vincent Sandanayaka, Philip Ross Hamann, Semiramis Ayral-Kaloustian
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Publication number: 20080125589Abstract: It was found that a fluoro derivative can be produced by reacting a hydroxy derivative with sulfuryl fluoride (SO2F2) in the presence of an organic base or in the presence of an organic base and “a salt or complex comprising an organic base and hydrogen fluoride”. According to the present production process, it is not necessary to use perfluoroalkanesulfonyl fluoride, which is not preferable in industrial use, and it is possible to advantageously produce optically-active fluoro derivatives, which are important intermediates of medicines, agricultural chemicals and optical materials, specifically 4-fluoroproline derivatives, 2?-deoxy-2?-fluorouridine derivatives, optically-active ?-fluorocarboxylate derivatives, and the like, even in a large scale.Type: ApplicationFiled: March 17, 2006Publication date: May 29, 2008Applicant: CENTRAL GLASS COMPANY, LIMITEDInventors: Akihiro Ishii, Takashi Ootsuka, Manabu Yasumoto, Hideyuki Tsuruta, Kenjin Inomiya, Koji Ueda, Kaori Mogi
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Publication number: 20080014173Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: July 10, 2007Publication date: January 17, 2008Inventors: Paul Michael Scola, Li-Qiang Sun
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Patent number: 7294722Abstract: The present invention relates to processes for preparing peptides and to intermediates involved in such processes, e.g. a process for preparing a compound of formula VIII wherein R12 and R13 are as defined herein.Type: GrantFiled: December 11, 2003Date of Patent: November 13, 2007Assignee: Novartis AGInventors: Bernhard Wietfeld, Walter Prikoszovich, Bernhard Erb, Werner Pachinger
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Patent number: 7282510Abstract: This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.Type: GrantFiled: June 27, 2005Date of Patent: October 16, 2007Assignee: GliaMed, Inc.Inventors: Gregory S. Hamilton, Joseph P. Steiner
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Patent number: 7279584Abstract: The present invention provides a safer method for production of a cis-4-fluoro-L-proline derivative under milder conditions and in good yield to give a product of high purity on an industrial scale at low cost. Namely, the present invention provides a method for producing a cis-4-fluoro-L-proline derivative, which comprises reacting a trans-4-hydroxy-L-proline derivative of the following Formula [I]: (wherein R1 represents a protecting group for an ?-amino group, and R2 represents a protecting group for a carboxyl group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride-scavenger.Type: GrantFiled: August 18, 2004Date of Patent: October 9, 2007Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Kazuyuki Tomisawa, Dai Tatsuta, Tomomichi Yoshida, Chihiro Yokoo
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Patent number: 7211677Abstract: A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted alkyl, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of the formula (II) with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX), to form a compound of formula (XX) The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).Type: GrantFiled: December 8, 2005Date of Patent: May 1, 2007Assignees: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Richard Hubert Furneaux, Peter Charles Tyler, Vern L. Schramm
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Patent number: 7189754Abstract: The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonize the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR6R7, NOR6, NNR6R7; R is selected from the group comprising or consisting of C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, saturated or unsaturated 3–8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl.Type: GrantFiled: March 19, 2002Date of Patent: March 13, 2007Assignee: Applied Research Systems ARS Holding NVInventors: Matthias Schwarz, Anna Quattropani, Alexander Scheer, Jerome Dorbais, Vincent Pomel
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Patent number: 7138386Abstract: The present invention relates to pharmaceuticals, foods and drinks, food additives, animal feeds and feed additives comprising an N-acylated hydroxyproline derivative or a salt thereof, and an amino sugar or a salt thereof and/or a glycosaminoglycan or a salt thereof as active ingredients, use of an Nacylated hydroxyproline derivative or a salt thereof for the production of an arthritis preventing or treating agent, and a method for preventing or treating arthritis which comprises administering an N-acylated hydroxyproline derivative or a salt thereof, and an amino sugar or a salt thereof and/or a glycosaminoglycan or a salt thereof.Type: GrantFiled: December 27, 2001Date of Patent: November 21, 2006Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Ryusuke Nakagiri, Toshikazu Kamiya
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Patent number: 7026345Abstract: The present invention relates to chiral N-acetyl-alpha-amino acid salts of optically active ?-amino alkylnitriles, and also to a process for preparing optically active ?-amino alkylnitriles by resolving racemic ?-amino alkylnitriles using chiral N-acetyl-alpha-amino acids as resolving agent.Type: GrantFiled: September 17, 2004Date of Patent: April 11, 2006Assignee: Pfizer Inc.Inventors: Juan Colberg, Samuela Zambelli Franz, Riccardo Motterle, Mariano Stivanello
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Patent number: 6982265Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.Type: GrantFiled: May 18, 2000Date of Patent: January 3, 2006Assignee: Bristol Myers Squibb CompanyInventors: John T. Hunt, Rajeev S. Bhide, Robert Michael Borzilleri, Ligang Qian
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Patent number: 6946554Abstract: Derivatives of 9-deazaguanine of the formula I: are prepared by reacting an aldehyde or ketone of the formula II: with a dialkylaminomalonate to produce an enamine. The enamine is then reacted with a base to produce a pyrrole represented by the formula: The pyrrole is reacted with a compound represented by the formula R3OC(O)N?C(Z)NHC(O)OR3 or a derivative of carbamimidoic acid to provide a protected guanidine compound. The guanidine compound is converted to the desired deazaguanine by reaction with 1) trifluoracetic acid or 2) C1-C4 alkoxide or alkali metal or alkaline earth metal hydroxide followed by neutralization with an acid.Type: GrantFiled: June 29, 2004Date of Patent: September 20, 2005Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Arthur J. Elliott, David A. Walsh, Philip E. Morris
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Patent number: 6838479Abstract: Inhibitors of serine proteases are provided having formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.Type: GrantFiled: September 5, 2001Date of Patent: January 4, 2005Assignee: Genentech, Inc.Inventors: Richard M Pastor, Dean R. Artis, Alan G. Olivero
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Publication number: 20040259804Abstract: This invention is directed to novel (substituted) acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: ApplicationFiled: July 20, 2001Publication date: December 23, 2004Inventor: Donald S. Karanewsky
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Publication number: 20040235753Abstract: Compounds according to general formula 1, wherein G1 is NR6R7 or a group according to general formula 3 and G2 NR24R25 or a fused polycyclic group are novel. They are selective and potent oxytocin agonists. Pharmaceutical compositions of such compounds are useful in the treatment of, inter alia, erectile dysfunction.Type: ApplicationFiled: December 24, 2003Publication date: November 25, 2004Inventors: Gray Robert William Pitt, Michael Bryan Roe, David Philip Rooker
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Patent number: 6780998Abstract: The oxidation hair dye precursor composition contains from 0.005 to 20.0 percent by weight of one or more coupler compounds and from 0.005 to 20.0 percent by weight of one or more developer compounds. The one or more developer compounds include at least one substituted 2-aminoalkyl-1,4-diaminobenzene compound of the formula (I): New substituted 2-aminoalkyl-1,4-diaminobenzene compounds of formula (I) are described.Type: GrantFiled: April 17, 2002Date of Patent: August 24, 2004Assignee: Wella AktiengesellschaftInventors: Laurent Chassot, Hans-Juergen Braun
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Patent number: 6753431Abstract: There is disclosed an advantageous mixed acid anhydride production method of formula (1): R1C(O)OY(O)n(R2)p (1) wherein R1, R2 and Y denote the same as defined below, n and p denote an integer of 1 or 2, which is characterized by adding a carboxylic acid of formula (2); R1COOH (2) wherein R1 denotes a hydrogen atom, an optionally substituted alkyl group or the like, an organic base to a solution of a carboxylic acid activating agent of formula (3); (R2)pY(O)nX (3) wherein R2 denotes an optionally substituted aliphatic hydrocarbyl group or the like, Y denotes a carbon atom, a phosphorus atom, or a sulfur atom, and X denotes a chlorine atom or the like.Type: GrantFiled: June 1, 2001Date of Patent: June 22, 2004Assignee: Sumitomo Chemical Company LimitedInventors: Takashi Miki, Hideki Ushio, Isao Kurimoto
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Patent number: 6737436Abstract: Compounds of the formula I in which R1 and R2, independently of one another, each denote H, A, OA, SA or HaI, R3 denotes H or A, R4 denotes A or NH2, R5 denotes H, NH2, NHA or NA2, A denotes alkyl having 1 to 10 carbon atoms, alkenyl, cycloalkyl or alkylenecycloalkyl, Hal denotes F, Cl, Br or I, and their physiologically acceptable salts and/or solvates, as phosphodiesterase VII inhibitors.Type: GrantFiled: May 3, 2002Date of Patent: May 18, 2004Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Rochus Jonas, Michael Wolf, Michael Gassen, Thomas Welge
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Publication number: 20030220497Abstract: O-medium alkyl esters of diflunisal and related compounds are disclosed having anti-platelet activity, hydroxy radical scavenging properties, enhanced hepatic clearance and low ulcerogenic potential. These compounds have general formula (I) wherein n equals 3-13.Type: ApplicationFiled: December 27, 2002Publication date: November 27, 2003Applicant: The University of QueenslandInventors: Daniel Yung-Yu Hung, Michael Stephen Roberts
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Publication number: 20030162979Abstract: The invention relates to novel substituted sulphonylamino(thio)carbonyl compounds of the formula (I) 1Type: ApplicationFiled: May 1, 2002Publication date: August 28, 2003Inventors: Klaus-Helmut Muller, Mark Wilhelm Drewes, Kurt Findeisen, Ernst Rudolf F. Gesing, Johannes R. Jansen, Rolf Kirsten, Joachim Kluth, Ulrich Philipp, Hans-Jochem Riebel, Markus Dollinger, Hans-Joachim Santel
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Patent number: 6515142Abstract: A process for preparing a compound represented by general formulae (5) and (6) in the following reaction scheme or salts thereof, wherein R1 represents a protective group for a nitrogen atom; R2 represents a methanesulfonyl group or p-toluenesulfonyl group; R1 represents a hydrogen atom, an aralkyl group, or an alkyl group having 1 to 6 carbon atoms; and X represents a halogen atom. The above process is useful as an industrial process for preparing intermediates of anticoagulant aromatic amidine derivatives described in Japanese Patent Application Laid-Open (kokai) No. 208946/1993.Type: GrantFiled: November 7, 2001Date of Patent: February 4, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Yukio Yokoyama, Tatsuya Kobayashi, Takeo Koyama
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Patent number: 6469171Abstract: The present invention relates to methods for preparing a variety of Lamellarin compounds and analogues via a synthetic intermediate, which methods involved the step of performing an intramolecular cyclization of a compound of Formula (I) to produce compounds of Formula(II), wherein the variables are given in the specification.Type: GrantFiled: February 2, 2001Date of Patent: October 22, 2002Assignee: The Australian National UniversityInventors: Martin Gerhardt Banwell, Bernard Luke Flynn
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Patent number: 6455571Abstract: Disclosed are compounds of the formula: which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.Type: GrantFiled: October 19, 1999Date of Patent: September 24, 2002Assignee: Abbott LaboratoriesInventors: Clarence J. Maring, Yu Gui Gu, Hui-Ju Chen, Yuanwei Chen, David A. Degoey, William J. Flosi, Vincent L. Giranda, David J. Grampovnik, Warren M. Kati, Dale J. Kempf, April Kennedy, Larry L. Klein, Allan C. Krueger, Zhen Lin, Darold L. Madigan, Keith F. McDaniel, Steven W. Muchmore, Hing L. Sham, Kent D. Stewart, Vincent S. Stoll, Minghua Sun, Noah P. Tu, Frank L. Wagenaar, Gary T. Wang, Sheldon Wang, Paul E. Wiedeman, Yibo Xu, Ming C. Yeung, Chen Zhao, Stephen Hanessian, Malken Bayrakdarian, Xuehong Luo
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Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Publication number: 20020037857Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have Pi a group having an amidino or guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.Type: ApplicationFiled: December 7, 2000Publication date: March 28, 2002Applicant: Corvas International, Inc.Inventors: Joseph Edward Semple, Michael I. Weinhouse, Odile Esther Levy, Edwin L. Madison, Amir P. Tamiz
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Patent number: 6346547Abstract: Low-toxicity, highly-bioavailable, pharmaceutical antioxidant compositions for preferred oral administration to mammals are provided which have at least one amino acid-based compound of the general formula (I): A—N(Z)—CH(R1)C(O)—Q (I) wherein A is represented by the formula: XO—[C(R2)2]n— wherein n is an integer of from 1 to about 3, X is selected from the group consisting of a hydrogen atom, an acyl group and a halogenated acyl group and each R2 is independently selected from the group consisting of a hydrogen atom, an alkyl group having from 1 to about 3 carbon atoms, a hydroxyalkyl group having from 1 to about 3 carbon atoms, and CH2OX; Z is selected from the group consisting of a hydrogen atom, an alkyl group of from 1 to about 3 carbon atoms, and A; R1 is an amino acid side chain group or an amino acid side chain group which forms with R2 a single heterocyclic structure having a total of from 5 to 7 atoms in the ring; and wherein Q is a substituent sType: GrantFiled: February 8, 2000Date of Patent: February 12, 2002Assignee: Checkpoint, Genetics, Inc.Inventor: Nathan Tzodikov
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Publication number: 20020016355Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.Type: ApplicationFiled: August 10, 2001Publication date: February 7, 2002Inventors: Francois Soucy, Louis Plamondon, Mark Behnke, William Roush
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Patent number: 6337398Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula: wherein the substituents are as defined in the specification, are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 13, 1995Date of Patent: January 8, 2002Assignee: G.D. Searle & Co.Inventors: Michael L Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6288036Abstract: The substitution of the L-Pro at the 7-position with D-Phe or D-Tic and substitution of the L-Phe at the 8-position with hydroxyproline ethers and thioethers of the peptide hormone bradykinin and other additional substituted analogs of bradykinin converts bradykinin agonists into bradykinin antagonists. The invention further includes additional modifications at other positions within the novel 7- and 8-position modified bradykinin antagonists, which increase enzyme resistance, antagonist potency, and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected as by insect bites.Type: GrantFiled: December 16, 1993Date of Patent: September 11, 2001Assignee: Scios Inc.Inventors: Donald James Kyle, Roger Neal Hiner
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Patent number: 6262089Abstract: New compounds have the formula: wherein R, R1, X and Y have the meanings described herein. Methods are set forth for synthesizing these compounds and using these compounds to treat diseases associated with amyloidosis, such as Alzheimer's disease, maturity onset diabetes mellitus, familial amyloid polyneuropathy, scrapie, and Kreuzfeld-Jacob disease.Type: GrantFiled: February 16, 2000Date of Patent: July 17, 2001Assignee: Hoffman-La Roche Inc.Inventors: Cornelia Hertel, Torsten Hoffmann, Roland Jakob-Roetne, Roger David Norcross
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Patent number: 6239146Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel &agr;,&agr;-difluoroacetamido compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: June 9, 2000Date of Patent: May 29, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Gene M. Dubowchik, Bireshwar Dasgupta, Dolatrai M. Vyas
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Patent number: 6232467Abstract: Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.Type: GrantFiled: June 27, 1997Date of Patent: May 15, 2001Assignee: University of Southern CaliforniaInventors: Nicos A. Petasis, Ilia A. Zavialov
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Publication number: 20010000344Abstract: A family of compounds capable of inhibiting the activity of prenyl transferases.Type: ApplicationFiled: December 1, 2000Publication date: April 19, 2001Applicant: Biomeasure IncorporatedInventor: Sun H. Kim