Plural Chalcogens Bonded Directly To Piperazine Ring Carbons Patents (Class 544/385)
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Publication number: 20110144336Abstract: A process for preparing piperazinedione derivatives of the formula I in which R1 is hydrogen, alkyl, alkenyl, alkynyl and alkylcarbonyl, R2 is hydrogen, alkyl, alkenyl, C3-C4-alkynyl and C(?O)R11, R3, R4 are each hydrogen, alkyl and haloalkyl, where the groups may be substituted, which comprises reacting amines of the formula II H2N—R1??II in which R1 is hydrogen and alkyl which may optionally be substituted with N-acylated amino acid derivatives of the formula III in which X is halogen, Y is halogen, alkoxy or phenyloxy which may be substituted and R2, R3 and R4 are each as defined at the outset, under basic conditions in an aqueous solvent.Type: ApplicationFiled: July 30, 2009Publication date: June 16, 2011Applicant: BASF SEInventors: Thomas Zierke, Eike Hupe, Michael Rack, Liliana Parra Rapado, Timo Frassetto
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Publication number: 20110105719Abstract: Reactors, reactor systems and methods for producing particles in a precipitation process are provided. The reactor includes a housing defining a reaction chamber, a stator assembly including two or more stators, a rotor assembly including two or more rotors, the rotor assembly configured for rotation about an axis of rotation relative to the stator assembly, a first inlet to supply a first reactant material to the reaction chamber at a first radial location, a second inlet to supply a second reactant material to the reaction chamber at a second radial location different from the first radial location, wherein the first and second reactant materials react to produce precipitation of particles in the reaction chamber, and an outlet to supply the particles formed in the reaction chamber.Type: ApplicationFiled: November 2, 2010Publication date: May 5, 2011Applicant: MannKind CorporationInventors: Sanket Gandhi, Karen Moraleda, Jadwiga Jachowicz, Michael Zupon
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Publication number: 20100317574Abstract: Disclosed herein are fumaryl diketopiperazine (FDKP) compositions and microparticles having a specific trans isomer content of about 45% to about 65%. The FDKP microparticles can comprise a drug such as an endocrine hormone, including, peptide, including, insulin, glucagon, parathyroid hormones and the like and can be used to make a powder formulation for pulmonary delivery of the drug.Type: ApplicationFiled: June 11, 2010Publication date: December 16, 2010Inventors: Kelly S. Kraft, Karla Somerville
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Patent number: 7820676Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.Type: GrantFiled: August 23, 2005Date of Patent: October 26, 2010Assignee: MannKind CorporationInventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
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Patent number: 7807678Abstract: The invention relates to a method of deriving a peptidomimetic of a biologically active metallopeptide, wherein the peptidomimetic includes at least one non-peptide ring structure defining a template space superimposable on a corresponding defined template space of the metallopeptide, and where the peptidomimetic further includes at least two elements independently including an amino acid residue, amino acid side chain moiety or derivative thereof, the elements defining and occupying a similar descriptor space as corresponding elements of the metallopeptide. The invention further relates to peptidomimetics with a template space heterocyclic ring structure, including 5-, 6- and 8-membered and 5-5- and 6-5-bicyclic fused ring structure melanocortin receptor-specific peptidomimetics.Type: GrantFiled: February 10, 2004Date of Patent: October 5, 2010Assignee: Palatin Technologies, Inc.Inventors: Shubh D. Sharma, Yi-Qun Shi, Zhijun Wu, Ramesh Rajpurohit
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Publication number: 20100181527Abstract: This invention relates to a stable secondary battery utilizing as active principle the oxidation and reduction cycle of a sterically hindered nitroxide radical, a sterically hindered oxoammonium cation, a sterically hindered hydroxylamine or a sterically hindered aminoxide anion containing a piperazin-2,6-dione, a piperazin-2-one or morpholin-2-one structural unit. Further aspects of the invention are a method for providing such a secondary battery, the use of the respective compounds as active elements in secondary batteries and selected novel compounds.Type: ApplicationFiled: June 9, 2008Publication date: July 22, 2010Inventors: Peter Nesvadba, Lucienne Bugnon Folger, Tobias Hintermann
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Patent number: 7732605Abstract: Disclosed herein are methods for synthesizing diketopiperazines with enantiomeric excess by inducing cyclization of an ?-keto acid with an acid catalyst.Type: GrantFiled: March 27, 2006Date of Patent: June 8, 2010Assignee: Nereus Pharmaceuticals, Inc.Inventor: Yoshio Hayashi
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Patent number: 7723082Abstract: The invention concerns novel isolated natural or synthetic polynucleotides and polypeptides coded by said polynucleotides, involved in the synthesis of diketopiperazine derivatives, vectors comprising said polynucleotides, micro-organisms transformed with said polynucleotides, uses of said polynucleotides and said polypeptides, as well as methods for the synthesis of diketopiperazine derivatives, including cyclodipeptides and diketopiperazine derivatives 3- and 6-substituted by ?,?-unsaturated amino acid side chains.Type: GrantFiled: July 19, 2006Date of Patent: May 25, 2010Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche ScientifiqueInventors: Muriel Gondry, Roger Genet, Sylvie Lautru, Jean-Luc Pernodet
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Patent number: 7709639Abstract: Provided is a method for the synthesis of N-protected bis-3,6-[4-aminobutyl]-2,5-diketopiperazine including the step of heating a solution of ?-amino protected lysine in the presence of a catalyst selected from the group consisting of sulfuric acid, phosphoric acid, and phosphorus pentoxide.Type: GrantFiled: August 19, 2005Date of Patent: May 4, 2010Assignee: MannKind CorporationInventors: John J. Stevenson, Destardi Moye-Sherman
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Publication number: 20100105698Abstract: The invention provides diketopiperazines of formula I. The invention also provides pharmaceutical compositions comprising the diketopiperazines, or pharmaceutically-acceptable salts or prodrugs thereof, as the active ingredient. The invention further provides therapeutic treatments that utilize the diketopiperazines of formula I, including inhibition of a proliferative disease or condition, inhibition of angiogenesis, treatment of an angiogenic disease or condition, treatment of cancer and precancerous conditions, treatment of a fibrotic disorder, treatment of a viral infection, treatment of an Akt-mediated disease or condition, inhibition of the production, release or both of matrix metalloproteinase-9, and inhibition of Akt activation.Type: ApplicationFiled: May 27, 2009Publication date: April 29, 2010Applicant: DMI LIFE SCIENCES, INC.Inventor: David Bar-Or
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Publication number: 20100087642Abstract: Provided is a method for the synthesis of N-protected bis-3,6-[4-aminobutyl]-2,5-diketopiperazine including the step of heating a solution of ?-amino protected lysine in the presence of a catalyst selected from the group consisting of sulfuric acid, phosphoric acid, and phosphorus pentoxide.Type: ApplicationFiled: December 8, 2009Publication date: April 8, 2010Applicant: MANNKIND CORPORATIONInventors: John J. Stevenson, Destardi Moye-Sherman
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Publication number: 20100010011Abstract: Compounds of formula (I), where R1 and R3 are H or (C1-C4)-alkyl; R2 is H or a C-radical derived from one of the known ring systems with 1-4 rings; X1 is a (C1-C6)-alkyl biradical derived from a linear or branched carbon chain; and X2 is —NH—, —NH—(CH2)1-3—COO—, —NH—(CH2)1-3—S—, or —NH—CO—(CH2)1-3—S—, are useful as blood-brain barrier shuttles (BBB). BBB shuttle-cargo constructs, the cargo being a substance susceptible to form an amide or an ester or a disulfide bound with X2 and being unable to cross the blood-brain barrier by itself, are useful as medicaments.Type: ApplicationFiled: August 28, 2007Publication date: January 14, 2010Inventors: Ernest Giralt Lledó, Meritxell Teixidó Turà
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Publication number: 20090281109Abstract: The present invention provides cysteine and cystine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.Type: ApplicationFiled: February 9, 2009Publication date: November 12, 2009Inventors: James M. Cook, David A. Baker, Wenyuan Yin, Edward Merle Johnson, II
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Publication number: 20090275749Abstract: Provided is a method of producing optically active 1-methyl-3-phenylpiperazine of the formula (11) or salt thereof, comprising the following steps 1 to 4, or steps 5 to 7 and step 4, and a method of producing optically active mirtazapine via this method.Type: ApplicationFiled: September 25, 2006Publication date: November 5, 2009Inventors: Hiroshi Maeda, Kozo Matsui, Nobushige Itaya
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Patent number: 7550462Abstract: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.Type: GrantFiled: June 21, 2005Date of Patent: June 23, 2009Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Deirdre Mary Bernadette Hickey, John Liddle, Andrew McMurtrie Mason
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Publication number: 20090156553Abstract: The invention relates to the use of piperazine compounds of formula (I) or the agriculturally useful salts of piperazine compounds of formula (I) as herbicides, the variables in formula (I) being defined as cited in the claims and the description.Type: ApplicationFiled: December 29, 2006Publication date: June 18, 2009Applicant: BASF SEInventors: Eike Hupe, Cyrill Zagar, Matthias Witschel, Toralf Kuhn, William Karl Moberg, Liliana Parra Rapado, Frank Stelzer, Andrea Vescovi, Michael Puhl, Robert Reinhard, Bernd Sievernich, Klaus Grossmann, Thomas Ehrhardt, Michael Rack
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Publication number: 20090043099Abstract: The invention provides isolated agents having novel chemical structures and possessing superior activity as derepressors of IAP inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The invention further provides assay methods employing labeled compounds of the invention, especially fluorescent labeled compounds.Type: ApplicationFiled: October 31, 2007Publication date: February 12, 2009Applicant: The Burnham InstituteInventors: John C. Reed, Richard A. Houghten, Adel Nefzi, John M. Ostresh, Clemencia Pinilla, Kate Welsh
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Publication number: 20090011994Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.Type: ApplicationFiled: June 18, 2008Publication date: January 8, 2009Inventors: Philip D. Stein, Sharon N. Bisaha, Saleen Ahmad, Khehyong Ngu, William N. Washburn
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Patent number: 7288545Abstract: This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula: In the above formula, each of and , independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is CH(RcRd) when is a single bond, or C(RcRd) when is a double bond; each of R1 and R2, independently, is H, C(O)Re, C(O)ORe, C(O)NReRf, or SO2Re; and each of Ra, Rb, Rc, Rd, Re, and Rf, independently, is H, C1-C6 alkyl, aryl, heteroaryl, C3-C8 cycloalkyl, or C3-C8 heterocycloalkyl; or Ra and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; or R1 and Ra or R1 and Rb taken together are C3-C8 cycloalkyl, C3-C8 heterocycloalkyl, aryl, or heteroaryl; provided that one of Rc and Rd is aryl or heteroaryl.Type: GrantFiled: October 20, 2003Date of Patent: October 30, 2007Assignee: AngioRx CorporationInventors: Che-Ming Teng, Hui-Po Wang, Eric I. C. Li, On Lee, Jih-Hwa Guh, Huei-Ting Chen, Ya-Bing Fan, Ya-Lan Chen
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Patent number: 6972289Abstract: The present invention relates to a cell division inhibitor comprising various dehydrodiketopiperazines such as dehydrophenylahistin, or analogs thereof as an active ingredient, and a dehydrogenase and a method for producing the same inhibitor.Type: GrantFiled: September 29, 2000Date of Patent: December 6, 2005Assignee: Nereus Pharmaceuticals, Inc.Inventors: Hiroshi Kanzaki, Kaneo Kanoh, Satohiro Yanagisawa, Teruhiko Nitoda, Kazumi Akazawa
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Patent number: 6900213Abstract: The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.Type: GrantFiled: July 21, 2003Date of Patent: May 31, 2005Assignee: Pharmacopeia Drug Discovery, Inc.Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
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Publication number: 20040236107Abstract: Intermediate compounds for the preparation of mirtazapine and obtention methods thereof.Type: ApplicationFiled: March 4, 2004Publication date: November 25, 2004Inventors: Jordi Bosch i Llado, Pelayo Camps Garcia, Juan Contreras Lascorz, Ma Carmen Onrubia Miguel
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Patent number: 6818645Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S, or NR4, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: August 1, 2003Date of Patent: November 16, 2004Assignee: Syntex (U.S.A.) LLCInventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
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Publication number: 20040152703Abstract: The invention relates to bisaryl derivatives of the formula I, 1Type: ApplicationFiled: July 21, 2003Publication date: August 5, 2004Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
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Publication number: 20040121963Abstract: The present invention relates to a composition for inhibiting HIV activity comprising the extract of Paecilomyces sp. (Tochu-kaso) J300. More particularly, the present invention relates to a composition for inhibiting HIV activity comprising 3-[5-(methoxy-ethyl)-3,6-dioxo-piperazine-2-yl]propionic acid represented by Formula I and 4-methyl-2-[(pyrolidine-2-carbonyl)-2-amino] pentanoic acid represented by Formula 2 that are extracted from Paecilomyces sp. (Tochu-kaso) J300; and to a medical composition and food composition containing the same.Type: ApplicationFiled: January 6, 2004Publication date: June 24, 2004Inventors: Sae-Yun Cho, Sang-Duk Ji, Seong-Kyu Song, Kwan-Hee Lee
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Publication number: 20040002599Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I), 1Type: ApplicationFiled: October 21, 2002Publication date: January 1, 2004Inventors: Klaus-Helmut Muller, Hans-Georg Schwarz, Stefan Herrmann, Dorothee Hoischen, Stefan Lehr, Otto Schallner, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Akihiko Yanagi, Shinichi Narabu, Toshio Goto, Seishi Ito, Chieko Ueno
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Isocyano substituted polystyrene carbonate resin for use in 3 and 4 component condensation reactions
Publication number: 20030225267Abstract: This invention relates to compounds comprising isocyano derivatives tethered to solid supports for use in 3 and 4 component condensation reactions. The invention also relates to methods for synthesizing cyclic derivatives by a 3 and 4 component condensation reaction using the compounds of the invention.Type: ApplicationFiled: January 7, 2003Publication date: December 4, 2003Inventors: April Kennedy, John A. Josey -
Patent number: 6642225Abstract: Compounds of formula I wherein R is carboxy, esterified carboxy or amidated carboxy; R1 and R3 are independently lower alkyl, (hydroxy, lower alkoxy, amino, acylamino, mono- or di-lower alkylamino or mercapto)-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, cycloalkyl, aryl, biaryl, (cycloalkyl, aryl or biaryl)-lower alkyl, or (carboxy, esterified carboxy or amidated carboxy)-lower alkyl; R2 is hydrogen, lower alkyl, cycloalkyl, aryl, biaryl, arylaminocarbonyl, or aryl-(oxy, thio or amino); n is 1 or 2; Y is lower-alkylene or lower alkenylene; and pharmaceutically acceptable salts thereof; which are useful as LFA-1 antagonists.Type: GrantFiled: October 2, 2001Date of Patent: November 4, 2003Assignee: Novartis AGInventors: Rainer Albert, Janet Dawson, Claus Ehrhardt, Sompong Wattanasin, Gabriele Weitz-Schmidt, Karl Welzenbach
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Publication number: 20030060418Abstract: The present invention relates to certain substituted oxadiazole, thiadiazoles and triazole peptoids which are useful as inhibitors of serine proteases. Compounds of the invention are useful for treating, for example, adult respiratory distress syndrome, septic shock, and myocardial ischemia-reperfusion injury.Type: ApplicationFiled: August 10, 2001Publication date: March 27, 2003Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 6525042Abstract: Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1 is hydrogen, hydroxyl, nitro or the like; R2 and R3 are each independently hydrogen, halogeno or the like; R4 and R5 are each dependently hydrogen, halogeno or the like; Q1 is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2 is a single bond, oxygen or the like; Q3 is, e.g., a group represented by formula (a): T1 is carbonyl or the like; and X1 and X2 are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.Type: GrantFiled: March 28, 2000Date of Patent: February 25, 2003Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Syozo Kobayashi, Satoshi Komoriya, Masayuki Ito, Tsutomu Nagata, Akiyoshi Mochizuki, Noriyasu Haginoya, Takayasu Nagahara, Haruhiko Horino
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Publication number: 20030008882Abstract: The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.Type: ApplicationFiled: May 8, 2002Publication date: January 9, 2003Inventors: Andrew D. Hamilton, Justin Ernst, Brendan P. Orner
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Publication number: 20020061878Abstract: Compounds of formula I 1Type: ApplicationFiled: October 2, 2001Publication date: May 23, 2002Inventors: Rainer Albert, Janet Dawson, Claus Ehrhardt, Sompong Wattanasin, Gabriele Weitz-Schmidt, Karl Welzenbach
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Patent number: 6387389Abstract: The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.Type: GrantFiled: June 30, 1999Date of Patent: May 14, 2002Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: Richard B. Rothman, Kenner C. Rice, David Lewis, Dorota Matecka, John R. Glowa
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Patent number: 6376708Abstract: This invention is directed to a process for making a salt of a carboxylic acid. The process comprises contacting a catalyst with an alkaline mixture comprising a primary alcohol. In one embodiment, for example, the catalyst comprises a metal support (preferably a metal sponge support) coated with copper. The support comprises at least about 10% (by weight) non-copper metal, and the copper-containing coating comprises from about 0.005 to about 0.5 grams of copper (per gram of said metal support). In another embodiment, the catalyst comprises a metal support (preferably a metal sponge support) coated with silver. The support comprises at least about 10% (by weight) non-silver metal, and the silver-containing coating comprises from about 0.005 to about 0.5 grams of copper (per gram of said metal support). In another embodiment, the catalyst comprises at least about 15% (by weight) non-copper metal, and at least about 10% (by weight) copper.Type: GrantFiled: April 11, 2000Date of Patent: April 23, 2002Assignee: Monsanto Technology LLCInventors: David A. Morgenstern, Juan P. Arhancet, Howard C. Berk, William L. Moench, Jr., James C. Peterson
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Patent number: 6369063Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: April 9, 2002Assignee: Cor Therapeutics, Inc.Inventors: Ting Su, Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20020038026Abstract: The invention provides a method of synthesizing a diketopiperazine of the formula: 1Type: ApplicationFiled: August 2, 2001Publication date: March 28, 2002Inventors: Nagaraja K.R. Rao, Stephen Turner
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Publication number: 20020019013Abstract: A method for high-speed parallel synthesis of combinatorial libraries is disclosed where two or more resins of dissimilar functionality are combined in the same reaction vessel in which a plurality of chemical reactions are carried out to create multiple compounds which are then sequentially and individually cleaved from the different resins under the appropriate cleavage conditions for each resin. As used herein resins are considered different when they exhibit different chemical activity in the presence of cleaving or releasing agents. The resins are different when the individual resins have either dissimilar polymeric backbones or dissimilar linkers or both and thus have a different chemical activity in the presence of a release or cleaving agent from the other resins in the reaction vessel.Type: ApplicationFiled: May 14, 2001Publication date: February 14, 2002Inventors: Boliang Lou, Tawfik Gharbaoui
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Publication number: 20020010182Abstract: This invention relates to piperazine derivatives of the formula: 1Type: ApplicationFiled: July 9, 2001Publication date: January 24, 2002Applicant: FUJISAWA PHARMACEUTICAL CO., LTD.Inventors: Matsuo Masaaki, Takashi Manabe, Nobukiyo Konishi, Kazuhiko Take, Norihiro Igari, Shinji Shigenaga, Hiroshi Matsuda, Tadashi Terasaka
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Publication number: 20010024798Abstract: The present invention provides biomimetic compounds and libraries thereof, as well as methods for their production. In general, the inventive method involves the selection of a desired biological synthetic pathway and mimics that synthetic pathway utilizing modern synthetic tools. The structures formed from this method are preferably generated in fewer than four steps. These scaffold structures can then be functionalized to yield biomimetic compounds and libraries of compounds. In preferred embodiments, biomimetic compounds and libraries are generated from an oxidative phenolic coupling reaction. In other particularly preferred embodiments, the compounds and libraries of compounds are generated from cascade reactions to yield bicyclo [n.3.1] ring systems, medium ring systems, and fused ring systems.Type: ApplicationFiled: April 19, 2001Publication date: September 27, 2001Inventors: Matthew D. Shair, Craig W. Lindsley, Henry E. Pelish, Scott M. Sheehan, Brian C. Goess, Mark E. Layton, Lawrence K. Chan, Chuo Chen, Nicholas J. Westwood
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Patent number: 6271232Abstract: Novel inhibitors of metalloproteases, in particular collagenase-1 and stromelysin-1, are disclosed. Such compounds are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, such as rheumatoid arthritis.Type: GrantFiled: July 9, 1999Date of Patent: August 7, 2001Assignee: Affymax Technologies, N.V.Inventors: David Campbell, Gary C. Look, Anna Katrin Szardenings, Dinesh V. Patel
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Patent number: 6211183Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: April 3, 2001Assignee: COR Therapeutics, Inc.Inventors: Charles K. Marlowe, Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6204268Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 13, 1998Date of Patent: March 20, 2001Assignee: COR Therapeutics, INCInventors: Robert M. Scarborough, Bing-Yan Zhu, Ting Su
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Patent number: 6153753Abstract: Process for the preparation of an N-acyl amino carboxylic acid by means of a carboxymethylation reaction. In this reaction, a reaction mixture is formed which contains a base pair, carbon monoxide, hydrogen and an aldehyde with the base pair comprising a carbamoyl compound and a carboxymethylation catalyst precursor. In a preferred embodiment, the carbamoyl compound and aldehyde are selected to yield an N-acyl amino carboxylic acid which is readily converted to N-(phosphonomethyl)glycine, or a salt or ester thereof.Type: GrantFiled: February 12, 1998Date of Patent: November 28, 2000Assignee: Monsanto CompanyInventors: Todd J. Johnson, Michael K. Stern, David A. Morgenstern, Michael D. Rogers, Yvette M. Fobian, Jeffrey A. Levine
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Patent number: 6107274Abstract: Compounds of formula A are disclosed: ##STR1## wherein R.sup.1 is aralkyl or cycloalkyl; R.sup.2 is cycloalkylmethyl, alkyl, or aralkyl;R.sup.3 is hydrogen, alkyl, substituted phenyl (including p-phenoxy-phenyl), or fluorene;R.sup.4 is hydrogen, alkyl, substituted phenyls (including 1-alkyl-4-carboxy-substituted phenyls), alkyl carboxylic acids;R.sup.5 is hydrogen or R.sup.1 and R.sup.5 taken together forming a tetrahydroisoquinoline ring or a piperidine ring.These compounds exhibit inhibitory action against fructose-1,6-bisphosphatase (FBPase) and are indicated in the treatment or management of Type II diabetes.Type: GrantFiled: March 15, 1999Date of Patent: August 22, 2000Assignee: Ontogen CorporationInventors: Adnan M. M. Mjalli, James Christopher Mason, Kristen Lee Arienti, Kevin Michael Short, Rachel Denise Anne Kimmich, Todd Kevin Jones
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Patent number: 6020373Abstract: Derivatives useful in the protection of living organisms against damage due to free radical reactions derived from methoxypolyethylene glycols (MPEG), which are modified by chemically attaching chelating groups in an amide or amine linkage to the nonmethyl end of the polymer. Such chelating groups include ethylene-diamine tetraacetic acid (EDTA), diethylene triamine pentaacetic acid (DTPA), and ethylene glycol aminoethyl ether tetraacetic acid (EGTA), and pharmacologically acceptable salts or esters thereof.Type: GrantFiled: April 21, 1997Date of Patent: February 1, 2000Assignee: Eastern Virginia Medical SchoolInventors: Karl A. Schellenberg, James Shaeffer, Frank A. Lattanzio, Jr.
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Patent number: 5994543Abstract: A novel class of antibiotics, designated bravomicins, is obtained by fermentation of a strain of Micromonospora polytrota. Six bioactive compounds, designated bravomicins A, B, C, D, E and F, are obtained and found to be useful in the treatment of a wide variety of bacterial diseases.Type: GrantFiled: March 4, 1999Date of Patent: November 30, 1999Assignee: Bristol-Myers Squibb CompanyInventors: Yue-Zhong Shu, Jie Chen, Kin Sing Lam, Judith A. Veitch, Daniel Brown
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Patent number: 5990112Abstract: Novel inhibitors of metalloproteases are disclosed. Such compounds are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, such as rheumatoid arthritis.Type: GrantFiled: June 18, 1996Date of Patent: November 23, 1999Assignee: Affymax Technologies N.V.Inventors: David Campbell, Gary C. Look, Anna Katrin Szardenings, Dinesh V. Patel
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Patent number: 5977359Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.Type: GrantFiled: October 20, 1998Date of Patent: November 2, 1999Assignee: SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5935955Abstract: A piperazinedione of general formula (I): ##STR1## wherein R.sup.1 is selected from hydrogen;a group of formula --(NH).sub.t --COR.sup.3 wherein t is 0 or 1 and R.sup.3 is an organic substituent as defined herein;a group of formula (D): ##STR2## and a group of formula (E): ##STR3## and the pharmaceutically acceptable salts thereof are useful as modulators of multi-drug resistance.Type: GrantFiled: August 29, 1997Date of Patent: August 10, 1999Assignee: Xenova LimitedInventors: Philip A. Ashworth, Sukhjit Hunjan, Ian A. Pretswell, Harnish Ryder, Stephen J. Brocchini
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Patent number: 5932579Abstract: Novel inhibitors of metalloproteases, in particular collagenase-1 and stromelysin-1, are disclosed. Such compounds are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, such as rheumatoid arthritis.Type: GrantFiled: June 18, 1996Date of Patent: August 3, 1999Assignee: Affymax Technologies N.V.Inventors: David Campbell, Gary C. Look, Anna Katrin Szardenings, Dinesh V. Patel