Unsubstituted Or Hydrocarbyl Substituted Only, Or Salt Thereof Patents (Class 544/410)
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Patent number: 12187688Abstract: A crystal form of tetramethylpyrazine nitrone (TBN), and a preparation method and use thereof is provided. A crystal form A of TBN has characteristic diffraction peaks in the XRPD pattern at 2?°: 10.60±0.2, 11.03±0.2, 15.31±0.2, 15.55±0.2, 17.14±0.2, 17.93±0.2, and 23.81±0.2. The crystal form A has low risk of polymorphism transformation and good stability, which contribute to the stability of the preparations during the production and storage processes, and effectively guarantee the consistency of the content of the crystal form in the preparations. Therefore, the preparations are safe, effective, and controllable in quality. Also, the crystal form A has high biological activity, good druggability, and high bioavailability, fast onset of action.Type: GrantFiled: July 31, 2019Date of Patent: January 7, 2025Assignee: GUANGZHOU MAGPIE PHARMACEUTICALS CO., LTD.Inventors: Wei Liu, Yewei Sun, Yuqiang Wang
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Patent number: 11667612Abstract: Provided herein are compositions and methods for treating pulmonary arterial hypertension. In particular, provided herein are dry powder formulations of TMP for delivery to the lung.Type: GrantFiled: October 25, 2018Date of Patent: June 6, 2023Assignee: Arizona Board of Regents on Behalf of the University of ArizonaInventors: Heidi M. Mansour, Jason Yuan, Jian Wang, Alexan I. Gomez, Priyardarshini Muralidharan, Yali Gu
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Patent number: 9284368Abstract: This invention provides for a method of preventing or treating a cadherin-11 related disease in a subject, which includes administering to the subject an effective amount of a compound of the following formula: or a pharmaceutically acceptable salt or prodrug thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X1 and X2 are as defined herein.Type: GrantFiled: July 3, 2014Date of Patent: March 15, 2016Assignee: GEORGETOWN UNIVERSITYInventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Jaime M. Guidry Auvil, Milton L. Brown
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Patent number: 9227803Abstract: The device for separating product parts of a multi-part, flat product includes a receiving unit for receiving the product, a device for separating the product parts and a retaining device for acting on one of the product parts for the purpose of maintaining the separation of the product parts. The receiving unit includes a first friction element and a second friction element, which is movable with respect to the first friction element. The two friction elements are arranged on the receiving unit such that the product can be firmly clamped between the friction elements. The friction elements are designed such that the static friction between the product part and the friction element assigned to this is greater than the static friction between the product parts, so that the product parts can be moved with respect to one another given a relative movement between the two friction elements firmly clamping the product.Type: GrantFiled: August 8, 2014Date of Patent: January 5, 2016Assignee: FERAG AGInventors: Othmar Brunschwiler, Erwin Stauber
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Publication number: 20150141427Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: ApplicationFiled: May 9, 2013Publication date: May 21, 2015Applicant: Novartis AGInventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
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Publication number: 20150087837Abstract: The present invention provides techniques that selectively recover Re from reductive amination catalysts. In particular, the present invention allows Re to be recovered selectively relative to Ni, Co, and/or Cu, and particularly Ni, that are often present on reductive amination catalysts. The present invention uses a combination of oxidation and extraction techniques to selectively recover Re relative to Ni, Co, and/or Cu. Advantageously, the recovery is selective even when using aqueous solutions for extraction.Type: ApplicationFiled: March 11, 2013Publication date: March 26, 2015Inventors: Stephen W. King, William C. Hoffman
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Publication number: 20150030782Abstract: A composition comprising dihydropyrazinyl anions that can be coordinated as 6 electron ligands to a broad range of different metals to yield volatile metal complexes for ALD and CVD depositions are described herein. Also described herein are undeprotonated dihydropyrazines that can coordinate to metals as stabilizing neutral ligands. In one embodiment, the composition is used for the direct liquid injection delivery of the metal dihydropyrazinyl complex precursor to the chamber of an ALD or CVD chamber for the deposition of metal-containing thin films such as, for example, ruthenium or cobalt metal films.Type: ApplicationFiled: July 11, 2014Publication date: January 29, 2015Applicant: AIR PRODUCTS AND CHEMICALS, INC.Inventors: Sergei Vladimirovich Ivanov, Xinjian Lei, John Anthony Thomas Norman
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Patent number: 8735399Abstract: The invention provides oxazolidine and thiazolidine derivatives that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.Type: GrantFiled: January 14, 2009Date of Patent: May 27, 2014Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Santosh C. Sinha, Phong X. Nguyen, Wenkui K. Fang, Ling Li, Janet A. Takeuchi, Smita S. Bhat
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Patent number: 8735581Abstract: Provided is a novel organometallic complex which can be synthesized easily and emits phosphorescence, or a compound which emits red phosphorescence. The inventors focused on easy synthesis of an m-aminophenyl pyrazine derivative represented by the following general formula (G0), synthesized an organometallic complex having a structure in which the derivative is coordinated to a Group 9 or Group 10 metal ion, and further synthesized a useful substance which emits red phosphorescence.Type: GrantFiled: December 21, 2011Date of Patent: May 27, 2014Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hideko Inoue, Tomoka Nakagawa, Satoshi Seo
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Publication number: 20130281664Abstract: The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e.Type: ApplicationFiled: October 11, 2011Publication date: October 24, 2013Inventors: David Milstein, Ekambaram Balaraman, Chidambaram Gunanathan, Boopathy Gnanaprakasam, Jing Zhang
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Patent number: 8415507Abstract: Cocrystals of pterostilbene are disclosed, including: pterostilbene:caffeine cocrystal, pterostilbene:carbamazepine cocrystal, pterostilbene:glutaric acid cocrystal, and pterostilbene:piperazine cocrystal. The pterostilbene:caffeine cocrystal is polymorphic. Forms I and II of the pterostilbene:caffeine cocrystal are disclosed. The therapeutic uses of the pterostilbene cocrystals and of pharmaceutical/nutraceutical compositions containing them are also disclosed. The disclosure sets out various methods of making and characterizing the pterostilbene cocrystals.Type: GrantFiled: July 30, 2010Date of Patent: April 9, 2013Assignee: Laurus Labs Private LimitedInventors: Nathan C. Schultheiss, Sarah J. Bethune
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Patent number: 8350033Abstract: Ligustrazine aromatic acid ether derivative of general formula I, its preparation method, pharmaceutical composition and application, wherein Ar is selected from aryl substituted aryl and substituted styryl, R is selected from hydrogen and alkyl with no more than 6 carbon atoms.Type: GrantFiled: October 27, 2008Date of Patent: January 8, 2013Inventors: Jiaming Li, Guangwei He, Yonghai Zhao, Fengshi Ma, Yong He, Qiang Wu, Feng Li
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Patent number: 8299246Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: March 6, 2012Date of Patent: October 30, 2012Assignee: AstraZeneca ABInventors: Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
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Patent number: 8288588Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: June 21, 2011Date of Patent: October 16, 2012Assignee: Novartis AGInventors: Urs Baettig, Anne-Marie D'souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20120255898Abstract: A polyamide membrane comprising reaction product of an anhydrous solution comprising an anhydrous solvent, at least one polyfunctional secondary amine and a pre-polymer deposition catalyst; and an anhydrous, organic solvent solution comprising a polyfunctional aromatic amine-reactive reactant comprising one ring. A composite semipermeable membrane comprising the polyamide membrane on a porous support. A method of making a composite semipermeable membrane by coating a porous support with an anhydrous solution comprising an anhydrous solvent, a polyfunctional secondary amine and a pre-polymer deposition catalyst, to form an activated pre-polymer layer on the porous support and contacting the activated pre-polymer layer with an anhydrous, organic solvent solution comprising a polyfunctional amine-reactive reactant to interfacially condense the amine-reactive reactant with the polyfunctional secondary amine, thereby forming a cross-linked, interfacial polyamide layer on the porous support.Type: ApplicationFiled: March 5, 2012Publication date: October 11, 2012Applicant: Eltron Research & Development, Inc.Inventor: Wayne E. Buschmann
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Publication number: 20120253042Abstract: A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.Type: ApplicationFiled: May 14, 2012Publication date: October 4, 2012Applicant: YEDA RESEARCH AND DEVELOPMENT CO. LTD.Inventors: David Milstein, Chidambaram Gunanathan, Yehoshua Ben-David, Ekambaram Balaraman, Boopathy Gnanaprakasam, Jing Zhang
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Patent number: 8163905Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: June 26, 2008Date of Patent: April 24, 2012Assignee: AstraZeneca ABInventors: Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
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Publication number: 20110245444Abstract: A method for processing biomass comprising heating an aqueous slurry comprising biomass, water and a phosphate catalyst in a pressure vessel at a temperature of about 150° C. to about 500° C. to produce a mixture comprising a dispersion of an organic phase and an aqueous phase.Type: ApplicationFiled: September 11, 2009Publication date: October 6, 2011Applicant: AQUAFLOW BIONOMIC CORPORATION LIMITEDInventors: Ian James Miller, Rhys Antony Batchelor
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Publication number: 20110224202Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Applicant: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Publication number: 20100324049Abstract: [Problems] To provide an antagonist of a melanin-concentrating hormone receptor, which is useful as a medicine for a central nervous system disease, a cardiovascular disease or a metabolic disease. [Means for Solving Problems] The antagonist comprises, as an active ingredient, a compound represented by the formula (I) wherein R1a and R1b independently represent a hydrogen atom or a C1-6 alkyl group; R2a, R2b, R3a and R3b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Y represents H or —OH; Z represents —OR8, or the like; R8 represents a hydrogen atom, a C1-6 alkyl group which may have a substituent, or the like; R9a and R9b independently represent a hydrogen atom, a C1-6 alkyl group, or the like; Ar1 represents an aromatic carbon ring group, or an aromatic heteroring group; Ar2 represents a group produced by removing two hydrogen atoms from an aromatic carbon ring, or the like; and the ring group A represents an unsaturated heteroring group.Type: ApplicationFiled: September 26, 2008Publication date: December 23, 2010Inventors: Makoto Ando, Minoru Kameda, Hiroshi Miyazoe, Minoru Moriya, Etsuko Hirose, Takao Suzuki
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Publication number: 20100187505Abstract: The present invention relates to the compounds of the formula (1) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.Type: ApplicationFiled: April 29, 2008Publication date: July 29, 2010Inventors: Philipp Stoessel, Arne Buesing, Holger Heil
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Patent number: 7358359Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: July 22, 2005Date of Patent: April 15, 2008Assignee: University of WashingtonInventors: Niels H. Andersen, Jason Bowman
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Patent number: 7332623Abstract: This invention provides aryl-substituted acyclic enediyne compounds of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1=R2=H; or R1 and R2 together form a moiety represented by the formula R3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and R4 represents a substituted or unsubstituted aryl group having 3-30 carbon atoms; with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1=R2=H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1=R2=H and R4 is phenyl. The compounds of formula (I) are found to have inhibitory activities against topoisomerase I or act as a S phase or G2/M phase blocker.Type: GrantFiled: May 18, 2004Date of Patent: February 19, 2008Assignee: Kaohsiung Medical UniversityInventors: Ming-Jung Wu, Chi-Fong Lin
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Patent number: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
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Publication number: 20070191606Abstract: The present invention provides novel 2,2-bis(4-hydroxyphenyl)-alkyl onium salts as illustrated by 2,2-bis(4-hydroxyphenyl)-tridecyl(1,2-dimethylimidazolium)bromide and a process for preparation thereof by hydroxyalkylating acetoacetate to the corresponding hyroxyalkylacetoacetate, dealkoxycarbonylating the hydroxyalkyl acetoacetate to ?-hydroxyalkan-2-one and contacting the ?-hydroxyalkan-2-one with phenol in the presence of an acidic catalyst to give 2,2-bis(4-hydroxyphenyl)alkanol, brominating the 2,2-bis(4-hydroxyphenyl)alkanol to 2,2-bis(4-hydroxyphenyl)alkyl bromide, quaternizing 1,2-dimethylimidazole with the 2,2-bis(4-hydroxyphenyl)alkyl bromide to 2,2-bis(4-hydroxyphenyl)alkyl(1,2-dimethylimidazolium)bromide. The products can be used as reactive modifiers for layered phyllosilicates that can be used in the preparation of polymer-nanocomposites, wherein the said polymers are prepared from 2,2-bis(4-hydroxyphenyl)propane as one of the reacting monomers.Type: ApplicationFiled: October 13, 2006Publication date: August 16, 2007Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Shroff Rama Mallikarjuna, Swaminathan Sivaram
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Patent number: 7208169Abstract: The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: GrantFiled: April 16, 2003Date of Patent: April 24, 2007Assignee: Bayer CropScience LPInventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Robert Markert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Martin Kugler, Thomas Jaetsch
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Patent number: 7160872Abstract: The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have activity in standard tests against HIV-infected cells as well as other biological activity related to binding of ligands to chemokine receptors that mediate a number of mammalian embryonic developmental processes.Type: GrantFiled: June 21, 2004Date of Patent: January 9, 2007Assignee: AnorMED Inc.Inventors: Gary Bridger, Eva Maria Boehringer, Zhongren Wang, Dominique Schols, Renato Skerlj, David Bogucki
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Patent number: 7153815Abstract: A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxyalkylene group or an alkyleneoxy, X1 and X2 are hydrogen atom, an alkyl, an alkenyl, an alkynyl, an aryl, a heterocyclic group, formyl, an acyl, an alkoxycarbonyl, an aryloxycarbonyl, a heterocyclic oxycarbonyl, an alkylsulfinyl, an arylsulfinyl, a heterocyclic sulfinyl, an alkylsulfonyl, an arylsulfonyl or a heterocyclic sulfonyl, Y is oxygen atom or sulfur atom, Z is hydrogen atom, a halogen atom, cyano, an alkyl, an alkenyl, an alkynyl, an amino, an alkoxy or an alkylthio, the substituents may be substituted; and novel hydrazon derivatives.Type: GrantFiled: January 10, 2003Date of Patent: December 26, 2006Assignee: Nihon Nohyaku Co., Ltd.Inventors: Shinji Kawata, Shuko Okui, Shigeru Suzuki, Toshiki Fukuchi, Akiyuki Suwa
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Patent number: 7125878Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.Type: GrantFiled: May 6, 2003Date of Patent: October 24, 2006Assignee: Janssen PharmaceuticaInventors: Han-Cheng Zhang, Gee-Hong Kuo, Bruce E. Maryanoff, Hong Ye, David O'Neill, Lan Shen, Keith Demarest, Bruce R. Conway, David F. McComsey
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Patent number: 7026478Abstract: A process for the production of compounds Ar—R1 by means of a cross-coupling reaction of an organometallic reagent R1-M with an aromatic or heteroaromatic substrate Ar—X catalyzed by one or several iron salts or iron complexes as catalysts or pre-catalysts, present homogeneously or heterogeneously in the reaction mixture. This new invention exhibits substantial advantages over established cross coupling methodology using palladium- or nickel complexes as the catalysts. Most notable aspects are the fact that (i) expensive and/or toxic nobel metal catalysts are replaced by cheap, stable, commercially available and toxicologically benign iron salts or iron complexes as the catalysts or pre-catalysts, (ii) commercially attractive aryl chlorides as well as various aryl sulfonates can be used as starting materials, (iii) the reaction can be performed under “ligand-free” conditons, and (iv) the reaction times are usually very short.Type: GrantFiled: May 10, 2002Date of Patent: April 11, 2006Assignee: Studiengesellschaft Kohle mbHInventors: Alois Fürstner, Andreas Leitner, María Méndez
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Patent number: 6972297Abstract: 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infectionsType: GrantFiled: March 29, 2001Date of Patent: December 6, 2005Assignee: SmithKline Beecham p.l.c.Inventors: Gerald Brooks, Eric Hunt, Steven Howard
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Patent number: 6897313Abstract: The invention relates to a novel, industrial synthesis of 2-ethyl-3-methyl-1,4-diazine.Type: GrantFiled: April 26, 2001Date of Patent: May 24, 2005Assignee: Symrise GmbH & Co. KGInventor: Stefan Lambrecht
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Patent number: 6881738Abstract: The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected.Type: GrantFiled: July 18, 2002Date of Patent: April 19, 2005Assignees: Medical College of Georgia Research Institute, University of Georgia Research Foundation, IncInventors: Jerry J. Buccafusco, Alvin V. Terry, J. Warren Beach, Rammamohanna R. Jonnala
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Patent number: 6693137Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: January 23, 2001Date of Patent: February 17, 2004Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, David Michael Bender, Buddy Eugene Cantrell, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Edward C. R. Smith, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6689781Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.Type: GrantFiled: July 20, 2001Date of Patent: February 10, 2004Assignees: Elan Pharmaceuticals, Inc., American Home Products CorporationInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Patent number: 6635641Abstract: Amide compounds represented by the formula: wherein: R1 is a moiety represented by the formula where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting of CH2, O, and S, provided that at least one of X and Y is CH2, or X and Y together with the bond there-between form a cyclopropyl; are described. These compounds and pharmaceutical compositions containing them modulate and/or inhibit the activity of certain protein kinases and are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation.Type: GrantFiled: January 19, 2001Date of Patent: October 21, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Dilip Bhumralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
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Patent number: 6624168Abstract: 7, 8 and 9-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.Type: GrantFiled: June 29, 2001Date of Patent: September 23, 2003Assignee: Trustees of Tufts CollegeInventors: Mark L. Nelson, Darrell Koza
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Patent number: 6562817Abstract: The present invention provides a compound of the formula (I): wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.Type: GrantFiled: July 21, 2000Date of Patent: May 13, 2003Assignee: Shionogi & Co., Ltd.Inventors: Norihiko Tanimoto, Yasushi Hasegawa, Nobuhiro Haga
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Patent number: 6521755Abstract: This invention provides a process to prepare 10,11-(optionally substituted)methanodibenzosuberane derivatives. The invention also provides an intermediate in this process.Type: GrantFiled: November 15, 2001Date of Patent: February 18, 2003Assignee: Eli Lilly and CompanyInventors: Bret Eugene Huff, Michael Edward LeTourneau, Thomas Michael Wilson, Julie Kay Bush, Susan Marie Reutzel-Edens
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Publication number: 20020143180Abstract: The present invention relates to enhancement of the cycle life of a zinc chromium based catalyst used in the synthesis of 2-methylpyrazine by increasing the reaction temperature step-wise, starting from a low temperature, while monitoring the levels of total conversion and selectivity towards pyrazine. The catalyst can be regenerated after each cycle of use without substantial loss of activity.Type: ApplicationFiled: March 27, 2001Publication date: October 3, 2002Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Sai Prasad Potharaju Seetharamanjaneya, Kondapuram Vijaya Raghavan, Panja Kanta Rao, Shivanand Janardan Kulkarni, Katabathini Narasimha Rao, Rajesh Gopinath, Suresh Farsinavis, Harshadas Mitaram Meshram
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Patent number: 6444662Abstract: Described are salts of hyperforin and adhyperforin of formula I [A−]m[B]p+ (I) wherein m is an integer from 1 to 3, p is equal to m and gives the total number of positive charges of the residue [B], [A−] is an anion of formula II with n=0 or 1 and [B]p+ is an ion of an alkali metal or an ammonium ion of a salt-forming nitrogen base of formula III wherein R1 through R4 have a variety of meanings including hydrogen, alkyl, cycloalkyl and similar groups which in turn may be substituted with one or more substituents. The salts serve inter alia for enriching or purifying hyperforin and adhyperforin from St. John's Wort extracts. Pharmaceutical preparations containing the salts are used for treating Alzheimer's Disease.Type: GrantFiled: August 11, 2000Date of Patent: September 3, 2002Assignee: Willmar Schwabe GmbH & Co.Inventors: Shyam Sunder Chatterjee, Clemens Erdelmeier, Klaus Klessing, Dieter Marme, Christoph Schächtele
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Patent number: 6417353Abstract: Amines are prepared by reacting aldehydes or ketones at elevated temperature under elevated pressure with nitrogen compounds selected from the group of ammonia, primary and secondary amines, and with hydrogen in the presence of a catalyst containing copper, wherein the catalytically active mass of the catalyst contains, before the reduction with hydrogen, 20 to 85% by weight of oxygen-containing compounds of zirconium, calculated as ZrO2, 1 to 30% by weight of oxygen-containing compounds of copper, calculated as CuO, 14 to 70% by weight of oxygen-containing compounds of nickel, calculated as NiO, 0 to 5% by weight of oxygen-containing compounds of molybdenum, calculated as MoO3, and 0 to 10% by weight of oxygen-containing compounds of aluminum, calculated as Al2O3.Type: GrantFiled: March 7, 2000Date of Patent: July 9, 2002Assignee: BASF AktiengesellschaftInventors: Frank Funke, Joachim Wulff-Döring, Gerhard Schulz, Wolfgang Siegel, Andreas Kramer, Johann-Peter Melder, Arthur Höhn, Philipp Buskens, Wolfgang Reif, Jan Nouwen
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Patent number: 6329378Abstract: Disclosed are pharmaceutical compositions comprising aryl and heteroaryl hydrazone, hydrazine and thiosemicarbazone derivatives of formulae I and II, and methods for using the compositions as antifungal agents. The invention also relates to novel aryl and heteroaryl hydrazone, hydrazine and thiosemicarbazone derivatives of formulae I and II, their preparation, to pharmaceutical compositions containing them, and to methods of using them to alleviate fungal infections.Type: GrantFiled: February 10, 2000Date of Patent: December 11, 2001Assignee: Anadys Pharmaceuticals, Inc.Inventors: Xiaodan Mei, Peng Wang, Andrei Caracoti, Pamela Mingo, Vincent Boyd, Robert Murray, Nicholas J. Sisti, Yi Bin Xiang, Shuhao Zhu, C. Richard Wobbe, Daniel Moore
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Patent number: 6300498Abstract: The 1,5′-bitetrazole of the invention comprises 1,5′-bitetrazole, and ammonia or an amine. The 1,5′-bitetrazole of the invention decomposes sharply and generates a nontoxic gas.Type: GrantFiled: July 23, 1999Date of Patent: October 9, 2001Assignee: Toyo Kasei Kogyo Company LimitedInventors: Hiroaki Tanaka, Kunihiro Shimamoto, Atuhiro Onishi
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Patent number: 6225471Abstract: Alkyl pyrazine compounds are prepared by heating and refluxing an aqueous mixture of an ammonium-containing compound and at least one acyloin compound. Reaction product may be isolated from the reacted mixture by adjusting the pH of the reacted mixture, separating solid material from the pH-adjusted reacted mixture, adding water to the separated solid material to form a solution, allowing product to crystallyze from the solution and then collecting the crystalline product. Alternatively, the reactants may be heated, refluxed and sublimed to collect the pyrazine reaction product on a cooled sublimation collection surface.Type: GrantFiled: March 16, 1992Date of Patent: May 1, 2001Assignee: Nestec S.A.Inventor: Teh-Kuei Chen
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Patent number: 6114421Abstract: Flame-retarding composition for polymers, copolymers and mixed polymers comprising piperazine diacid pyrophosphate, piperazine acid phosphate, melamine acid phosphate, melamine and possibly though not necessarily, an alkaline phosphate. Process for the preparation of said flame-retarding composition, consisting in reacting a mixture comprising phosphoric anhydride, piperazine and melamine with water in controlled conditions, either with mass reaction or suspension reaction with a suitable solvent/dispersing agent.Type: GrantFiled: July 2, 1998Date of Patent: September 5, 2000Assignee: Domus Industria Chimica S.p.A,Inventor: Alessandro Malcangi
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Patent number: 6096761Abstract: The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R.sup.1 is C.sub.1-6 alkyloxy, C.sub.2-6 alkenyloxy or C.sub.2-6 alkynyloxy; R.sup.2 is hydrogen or C.sub.1-6 alkyloxy, or when taken together R.sup.1 and R.sup.2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C.sub.1-6 alkyl; R.sup.3 is hydrogen or halo; R.sup.4 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.2-6 alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R.sup.5 -, Alk-X--R.sup.6, -Alk-Y--C(.dbd.O)--R.sup.8, or -Alk-Y--C(.dbd.O)--NR.sup.10 R.sup.11 wherein each Alk is C.sub.1-12 alkanediyl; and R.sup.5 is hydrogen, cyano, C.sub.1-6 alkylsulfonylamino, C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, aryl, di(aryl)methyl or a heterocyclic ringsystem; R.sup.6 is hydrogen, C.sub.Type: GrantFiled: August 11, 1998Date of Patent: August 1, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Paul Rene Marie Bosmans, John Christopher Love, Michel Anna Jozef Decleyn, Henri Elisabeth Frans D'Haen
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Patent number: 5919930Abstract: Process for cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates.In a process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates under palladium catalysis in the presence of at least one water-soluble complex ligand, the reaction medium comprises an aqueous and an organic phase and the palladium is added in the form of a palladium compound soluble in the organic phase.Polycyclic aromatic compounds can thus be prepared economically and in very good yields and simultaneously very high purity, in particular without contamination by the complexing ligands.Type: GrantFiled: July 26, 1995Date of Patent: July 6, 1999Assignee: Hoechst AktiengesellschaftInventors: Steffen Haber, Javier Manero
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Patent number: 5880129Abstract: A discovery underlying this invention is the concordance between particular cellular signaling mechanisms and cancer cell growth and metastasis. It has now been discovered that certain compounds inhibit the signal transduction required for the maintenance and driving of the malignant process. These compounds are also effective for the in vivo treatment of solid tumors and related disease states. This invention provides a method for the use of these compounds to inhibit the invasion and metastasis of malignant solid tumors in mammals. This invention further provides a method for using related compounds to treat diseases involving aberrant signal transduction pathways. Some of the compounds used in the methods of the present invention are novel and constitute another aspect of this invention.Type: GrantFiled: August 5, 1997Date of Patent: March 9, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Elise C. Kohn, Lance A. Liotta, Christian C. Felder
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Patent number: H2007Abstract: Compounds of the following structure are disclosed as effective insecticides: in which: A and B are independently lower alkyl; U is lower alkylidene, lower alkenylidene, or CH—Z, where Z is hydrogen, lower alkyl, lower cycloalkyl, or phenyl; R is phenyl or a dibenzocyclo(C5-8)alkyl, each optionally substituted, or where R3 and R4 are independently selected from phenyl, optionally substituted with, halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, lower alkenyl, or phenyl; R1 is selected from a variety of substituents, including 3-R2, where R2 is where D, E, and G are hydrogen, hydroxy, halogen, cyano, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy, nitro, lower haloalkylsuffonyloxy, lower alkylcarboxylato, lower alkylcarbonylamino, lower alkylcarbonyl, lower alkoxycarbonyl, arylcarbonylamino; D and E taken together may form the group —O(CH2)O—; J is hydrogen or lower alkyl; m is 2 or 3, n is 1, 2, or 3; and halogType: GrantFiled: January 9, 1997Date of Patent: December 4, 2001Assignee: FMC CorporationInventors: Ian R. Silverman, Syed F. Ali, Daniel H. Cohen, John W. Lyga, Kirk A. Simmons, Thomas G. Cullen