The Chalcogen Is Single Bonded To Both Acyclic Carbon And Hydrogen Patents (Class 544/401)
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Patent number: 10626097Abstract: The present invention relates to an improved process for making hydroxyethyl piperazine compounds especially mono-hydroxyethyl piperazine. The improvement comprises reacting piperazine and an alkylene oxide, preferably ethylene oxide in a reactive distillation column.Type: GrantFiled: July 8, 2016Date of Patent: April 21, 2020Assignee: Dow Global Technologies LLCInventors: John G. Pendergast, Jr., Ravindra S. Dixit, Stephen W. King, Christophe R. Laroche
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Patent number: 9328080Abstract: A process for selectively preparing dihydroxyethyl piperazine by reacting hydroxyethyloxazolidinone with an acid catalyst wherein the selectivity of hydroxyethyloxazolidinone to dihydroxyethyl piperazine is at least 55%.Type: GrantFiled: September 4, 2013Date of Patent: May 3, 2016Assignee: Dow Global Technologies LLCInventors: Tina L. Arrowood, Jason C. MacDonald
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Patent number: 9169222Abstract: The present invention relates to an improved process for making mono- and di-alkoxylated piperazine compounds especially dihydroxyethylpiperazine. The improvement comprises the addition of an acid to the piperazine compound prior to the addition of an alkylene oxide to a reactor wherein the alkoxylated piperazine compound is prepared. Said improvement reduces the concentration of undesirable glycol ether byproducts which contribute undesirable color and foaming of the alkoxylated piperazine compounds.Type: GrantFiled: August 24, 2012Date of Patent: October 27, 2015Assignee: Dow Global Technologies LLCInventors: Christophe R. Laroche, Daniel A. Aguilar
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Patent number: 9028728Abstract: The present invention relates to photochromic materials that include one or more indeno-fused naphthopyrans that have particular groups at the 7, 11, and 13 positions thereof, and at the position alpha to the oxygen of the pyran ring thereof. With some embodiments, hydrogen or an alkoxy group is bonded to the 7 position, an optionally substituted phenyl is bonded to the 11 position, two alkyl groups are bonded to the 13 position, and two optionally substituted phenyl groups are bonded to the position alpha to the oxygen of the pyran ring of the indeno-fused naphthopyran compound. The 13 position of the indeno-fused naphthopyrans is free of ether groups in which an ether oxygen is bonded to the 13 position, and hydroxyl. The present invention also relates to photochromic articles and compositions that include such indeno-fused naphthopyrans.Type: GrantFiled: December 8, 2011Date of Patent: May 12, 2015Assignee: Transitions Optical, Inc.Inventors: Kevin E. Bancroft, Anu Chopra, Xiao-Man Dai, Beon-Kyu Kim, David B. Knowles, Jason R. Lewis, Victor A. Montes, Stephen D. Straight, Massimiliano Tomasulo, Barry Van Gemert, Robert W. Walters, Wenjing Xiao, Huayun Yu, Elizabeth A. Zezinka
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Publication number: 20150094314Abstract: A method of modulating ribonucleotide reductase activity in a neoplastic cell includes administering to the cell an amount of a ribonucleotide reductase allosteric modulator (RRAmod), the amount being effective to inhibit neoplastic cell growth.Type: ApplicationFiled: March 21, 2013Publication date: April 2, 2015Inventor: Chris Dealwis
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Patent number: 8969353Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.Type: GrantFiled: November 6, 2009Date of Patent: March 3, 2015Assignee: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
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Patent number: 8952198Abstract: Disclosed is a process for the preparation of an amine (particularly diamines and polyamines) by reacting an alkanolamine or a polyol with ammonia in the presence of a catalyst composed of two active metals from the group of transition metals, namely nickel and chromium supported on a microporous refractory substrate, in a hydrogenated, trickle bed reactor.Type: GrantFiled: January 30, 2013Date of Patent: February 10, 2015Inventors: Ian Williams, John Christopher Williams, German Maya Maya-Hernandez, Lilia Patricia Hernandez Salas, Miguel Angel Lopez Guerrero
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Publication number: 20150011566Abstract: The present invention provides N-phenylpiperazine derivatives for use as multiple binders and/or antagonists of ?1A adrenoceptors, ?1D adrenoceptors and 5-HT1A serotonin receptors. These substances are candidates to prototypes for the treatment of benign prostate hyperplasia and lower urinary tract symptoms, and are useful in pharmaceutical compositions.Type: ApplicationFiled: January 4, 2013Publication date: January 8, 2015Inventors: Claudia Lucia Martins Da Silva, Fernanda Chagas Da Silva, Luana Chaves Barberato, Luciana De Camargo Nascente, Jessica Barbosa Do Nascimento Viana, Renata Oliveira Silva, Laís Flávia Nunes Lemes, François German Noël, Luís Antônio Soares Romeiro
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Publication number: 20140309114Abstract: Amine salts of certain herbicides that in free acid form include at least one carboxylic acid moiety are described. Herbicide salts comprising the cation of various imidazole, piperazine, piperidine, and morpholine compounds are provided. The herbicide amine salts described are suitable for formulation into herbicidal application mixtures and/or stable concentration compositions that exhibit acceptable volatility characteristics upon application.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Applicant: MONSANTO TECHNOLOGY LLCInventors: Junhua Zhang, Daniel R. Wright, William Abraham
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Publication number: 20140256944Abstract: The present invention relates to an improved process for making mono- and di-alkoxylated piperazine compounds especially dihydroxyethylpiperazine. The improvement comprises the addition of an acid to the piperazine compound prior to the addition of an alkylene oxide to a reactor wherein the alkoxylated piperazine compound is prepared. Said improvement reduces the concentration of undesirable glycol ether byproducts which contribute undesirable color and foaming of the alkoxylated piperazine compounds.Type: ApplicationFiled: August 24, 2012Publication date: September 11, 2014Applicant: Dow Global Technologies LLCInventors: Christophe R. Laroche, Daniel A. Aguilar
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Publication number: 20140187554Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.Type: ApplicationFiled: May 16, 2012Publication date: July 3, 2014Applicant: The Scripps Research InstituteInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris
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Patent number: 8673920Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: GrantFiled: April 27, 2010Date of Patent: March 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
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Patent number: 8618108Abstract: The present invention provides strategies for making cyclic triamines. Reactant media including certain precursors and/or certain types of catalysts can be converted into cyclic triamines with improved conversion and selectivity. The strategies can be incorporated into reactions that involve transamination schemes and/or reductive amination schemes. In the case of transamination, for instance, using transamination to cause ring closure of higher amines in the presence of a suitable catalyst leads to desired cyclic triamines with notable conversion and yield. In the case of reductive amination, reacting suitable polyfunctional precursors in the presence of a suitable catalyst also yields cyclic triamines via ring closure with notable selectivity and conversion. Both transamination and reductive amination methodologies can be practiced under much milder temperatures than are used when solely acid catalysts are used. Preferred embodiments can produce reaction mixtures that are generally free of salt by-products.Type: GrantFiled: October 6, 2009Date of Patent: December 31, 2013Assignee: Union Carbide Chemicals & Plastics Technology LLCInventors: Stephen W. King, Stefan K. Mierau, Thomas Z. Srnak
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Publication number: 20130280783Abstract: Provided herein are polymeric ?-hydroxy aldehyde or ?-hydroxy ketone reagents which can be conjugated to amine-containing compounds to form stable conjugates in a single-step reaction. In selected embodiments, the polymeric reagent itself incorporates an internal proton-abstracting (basic) functional group, to promote more efficient reaction. The substituent is appropriately situated, via a linker if necessary, to position the group for proton abstraction, preferably providing a 4- or 5-bond spacing between the abstracting atom and the hydrogen atom on the ?-carbon. Also provided are methods of using the reagents and stable, solubilized conjugates of the reagents with biologically active compounds. In preferred embodiments, the polymeric component of the reagent or conjugate is a polyethylene glycol.Type: ApplicationFiled: June 24, 2013Publication date: October 24, 2013Inventors: Sean M. CULBERTSON, Xiaoming Shen, Antoni Kozlowski, Samuel P. McManus
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Publication number: 20130267707Abstract: The invention relates to derivatives of N,N?-substituted piperazines of the general formula (I): where R1 and R2 denote linear or branched (C1-C4)alkyl, linear or branched (C1-C4)alkoxy, CH3C(?O)O or halogen; n=1-5; m=0-3; Z denotes CH2, C?O or SO2; X denotes C(?NH)NH2, C(?NH)NHC(?NH)NH2 or CH2(CHR3)pCH2SO3H, where R3 denotes H, OH, CH3C(?O)O or HOSO2O and p=0-1; and G denotes low-molecular-weight organic or mineral acid, sodium, potassium or ammonium cations, or water. Said derivatives have antiaggregant, anticoagulant and vasodilatory properties. The invention further relates to a method for producing said derivatives by reacting N-substituted piperazines either with carboxamide amidating agents or salts thereof, or with haloalkyl sulfonic acids or salts thereof in organic solvents or in water in the presence of bases. The compounds may be used for the prophylaxis and treatment of disorders of the hemostatic system.Type: ApplicationFiled: November 8, 2011Publication date: October 10, 2013Applicant: ZAKRYTOE AKTSIONERNOE OBSCHSHESTVO "VERTEX"Inventors: Olga Sergejevna Veselkina, Nikolay Borisovich Viktorov, Nikolay Nikolaevich Petrishchev, Yuliya Vyacheslavovna Poplavskaya
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Publication number: 20130225561Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 21, 2011Publication date: August 29, 2013Inventors: Haifeng Tang, Alexander Pasternak, Lihu Yang, Shawn P. Walsh, Barbara Pio, Aurash Shahripour, Nardos Teumelsan
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Patent number: 8388872Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran of structural formulas I or II, having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.Type: GrantFiled: February 21, 2012Date of Patent: March 5, 2013Assignee: Transitions Optical, Inc.Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, Jr., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
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Patent number: 8299249Abstract: The invention relates to a process for preparing triethylenetetramine (TETA), which, comprises the following steps: a) reaction of ethylenediamine (EDA) with formaldehyde and hydrocyanic acid (HCN) in a molar ratio of EDA to formaldehyde to HCN of from 1:1.5:1.5 to 1:2:2 to give ethylenediaminediacetonitrile (EDDN), b) hydrogenation of the EDDN obtained in step a) in the presence of a catalyst and a solvent.Type: GrantFiled: February 28, 2008Date of Patent: October 30, 2012Assignee: BASF SEInventors: Kirsten Dahmen, Alfred Oftring, Katrin Baumann, Randolf Hugo, Thilo Hahn, Johann-Peter Melder
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Patent number: 8273884Abstract: The present invention provides strategies for making cyclic triamines. Reactant media including certain precursors and/or certain types of catalysts can be converted into cyclic triamines with improved conversion and selectivity. The strategies can be incorporated into reactions that involve transamination schemes and/or reductive amination schemes. In the case of transamination, for instance, using transamination to cause ring closure of higher amines in the presence of a suitable catalyst leads to desired cyclic triamines with notable conversion and yield. In the case of reductive amination, reacting suitable polyfunctional precursors in the presence of a suitable catalyst also yields cyclic triamines via ring closure with notable selectivity and conversion. Both transamination and reductive amination methodologies can be practiced under much milder temperatures than are used when solely acid catalysts are used. Preferred embodiments can produce reaction mixtures that are generally free of salt by-products.Type: GrantFiled: October 6, 2009Date of Patent: September 25, 2012Assignee: Union Carbide Chemicals & Plastics Technology LLCInventors: Stephen W. King, Thomas Z. Srnak, Stefan K. Mierau
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Patent number: 8252796Abstract: The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art.Type: GrantFiled: September 29, 2009Date of Patent: August 28, 2012Assignees: CSPC Zhonggi Pharmaceutical Technology (Shijiazhuang) Co. Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Na Lv, Hua Jin, Zhijie Weng, Yongyong Zheng
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Publication number: 20120165463Abstract: A compound having formula (I) wherein R1 is methyl or ethyl; R2 is hydrogen, methyl, CH2C(NH2)(R1)(CH2OH) or R2 groups combine to form a difunctional C2-C6 alkyl group; and X is a difunctional group selected from the group consisting of C2-C20 alkyl, C5-C20 cycloalkyl, C6-C10 aryl, C8-C20 aryl alkyl, C4-C20 heteroalkyl or C10-C20 aryl heteroalkyl.Type: ApplicationFiled: December 13, 2011Publication date: June 28, 2012Inventors: Ian A. Tomlinson, Asghar A. Peera, Glenn Nelson Robinson
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Publication number: 20120108816Abstract: Process for preparing 1,4-bishydroxyethylpiperazine (BHEPIP) of the formula I wherein diethanolamine (DEOA) of the formula II is reacted in the liquid phase in a reactor at a temperature in the range from 130 to 300° C. in the presence of a copper-comprising, chromium-free heterogeneous catalyst.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Applicant: BASF SEInventors: Christof Wilhelm Wigbers, Nina Challand, Johann-Peter Melder, Udo Rheude, Roman Dostalek
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Patent number: 8147725Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.Type: GrantFiled: September 1, 2010Date of Patent: April 3, 2012Assignee: Transitions Optical, IncInventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank Molock, Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
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Publication number: 20120014976Abstract: The disclosure provides adjuvants, immunogenic compositions, and methods useful for vaccination and immune response. In particular, the disclosure provides a class of adjuvants comprising cationic lipid:co-lipid mixtures and methods for delivering formulated compositions.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: Vical IncorporatedInventors: Jukka Hartikka, Sean M. Sullivan, Joel D. Enas, Alain Rolland
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Publication number: 20110223213Abstract: Provided herein is an impurity of ranolazine, 1-[4-[2-hydroxy-3-(2-methoxy-phenoxy)-propyl]-piperazin-1-yl]-3-(2-methoxy-phenoxy)-propan-2-ol (dimer impurity-3), and process for preparing and isolating thereof. Provided further herein is a highly pure ranolazine or a pharmaceutically acceptable salt thereof substantially free of dimer impurity-3, process for the preparation, and pharmaceutical compositions comprising highly pure ranolazine or a pharmaceutically acceptable salt thereof substantially free of dimer impurity-3.Type: ApplicationFiled: October 13, 2009Publication date: September 15, 2011Applicant: ACTAVIS GROUP PTC EHFInventors: Venkata Subbarao Athukuri, Saidugari Swamy, Chandraprakash Narani, Mayur Devjibhai Khunt, Nitin Sharadchandra Pradhan
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THE 1-BUTYL-2-HYDROXYARALKYL PIPERAZINE DERIVATIVES AND THE USES AS ANTI-DEPRESSION MEDICINE THEREOF
Publication number: 20110183996Abstract: The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art.Type: ApplicationFiled: September 29, 2009Publication date: July 28, 2011Applicant: Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Na Lv, Hua Jin, Zhijie Weng, Yongyong Zheng -
Publication number: 20110077376Abstract: To provide a process for producing a hydroxyalkyltriethylenediamine or hydroxytriethylenediamine simply and in a small number of steps without requiring multi-stage reaction steps; a novel catalyst composition whereby a polyurethane product can be obtained with good productivity and good moldability without bringing about odor problems or environmental problems; and a process for producing a polyurethane resin using the catalyst composition. For example, a hydroxyalkyltriethylenediamine or hydroxytriethylenediamine is produced by subjecting a mono-substituted dihydroxyalkylpiperazine and/or a di-substituted hydroxyalkylpiperazine to an intramolecular dehydration condensation reaction in the presence of an acid catalyst.Type: ApplicationFiled: May 29, 2009Publication date: March 31, 2011Inventors: Katsumi Tokumoto, Takao Suzuki, Hiroyuki Kiso, Yoshihiro Takahashi, Yutaka Tamano
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Publication number: 20100331234Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.Type: ApplicationFiled: March 3, 2010Publication date: December 30, 2010Applicant: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher Gerard Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel G. Anderson
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Publication number: 20100279997Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.Type: ApplicationFiled: October 28, 2009Publication date: November 4, 2010Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20100255117Abstract: The instant invention provides methods and compositions for the treatment of cancer.Type: ApplicationFiled: April 6, 2008Publication date: October 7, 2010Applicant: The Johns Hopkins UniversityInventors: Shyam Biswal, Anju Singh, Deepti Malhotra
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Publication number: 20090312344Abstract: The present invention relates to ?1, and/or ?1d adrenergic receptor antagonists, which can function as ?1a and/or ?1d adrenergic receptor antagonist and can be used for the treatment of a disease or disorder mediated through ?1a and/or an adrenergic receptor. Compounds disclosed herein can be used for the treatment of benign prostatic hyperplasia (BPH) and the related symptoms thereof. Further, compounds disclosed herein can be used for the treatment of lower urinary tract symptoms associated with or without BPH. Also provided are processes for preparing such compounds, pharmaceutical compositions thereof, and the methods of treating BPH or related symptoms thereof.Type: ApplicationFiled: May 31, 2005Publication date: December 17, 2009Inventors: Mohammad Salman, Somesh Sharma, Gyan Chand Yadav, Gobind Singh Kapkoti, Anurag Mishra, Praful Gupta, Nitya Anand, Anita Chugh, Kamna Nanda
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Patent number: 7589094Abstract: Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: December 7, 2005Date of Patent: September 15, 2009Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrea Gailunas, John A. Tucker, Ruth TenBrink, John Mickelson
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Publication number: 20090191227Abstract: The disclosure provides adjuvants, immunogenic compositions, and methods useful for vaccination and immune response. In particular, the disclosure provides a class of adjuvants comprising cationic lipid:co-lipid mixtures and methods for delivering formulated compositions.Type: ApplicationFiled: May 23, 2008Publication date: July 30, 2009Applicant: Vical IncorporatedInventors: Jukka Hartikka, Sean M. Sullivan, Joel D. Enas, Alain Rolland
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Publication number: 20090173913Abstract: An asymmetric organomodified disiloxane surfactant having the formula: MM? wherein M comprises branched hydrocarbon substituents and M? comprises a cationic, anionic or zwitterionic substituent and a polyether substituent that may be combined as one moiety, wherein the disiloxane surfactant has an enhanced resistance to hydrolysis between a pH of about 3 to about 12.Type: ApplicationFiled: December 26, 2007Publication date: July 9, 2009Applicant: MOMENTIVE PERFORMANCE MATERIALS INC.Inventors: Mark D. Leatherman, George A. Policello, Wenqing N. Peng, Liping Zheng, Roland Wagner, Suresh K. Rajaraman, Zijun Xia
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Patent number: 7390812Abstract: N,N?-disubstituted piperazine compounds, processes for the production thereof, and pharmaceutical preparations containing these compounds. The use of N,N?-disubstituted piperazine compounds for the production of pharmaceutical preparations and in related methods of treatment.Type: GrantFiled: June 14, 2004Date of Patent: June 24, 2008Assignee: Gruenenthal GmbHInventors: Heinz Uragg, Corinne Maul, Helmut Buschmann, Bernd Sundermann, Hagen-Heinrich Hennies
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Patent number: 7078407Abstract: The present invention relates to 4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them. More particularly, it relates to 4-hydroxycinnamamide derivatives showing superior antioxidant activity compared to the known antioxidant compounds, their pharmaceutically acceptable salt, and pharmaceutical compositions containing them. It can be usefully used in treating neurodegerative diseases such as aging, cancer, diabetes, ischemic stroke, Parkin's disease, dementia and Huntinton's disease.Type: GrantFiled: November 22, 2002Date of Patent: July 18, 2006Assignee: Korea Research Institute of Chemical TechnologyInventors: No-Sang Park, Young-Sik Jung, Churl-Min Seong, Hee-Jong Lim, Joong-Ho Yoon, Jae-Yang Kong, Woo-Kyu Park
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Patent number: 6887872Abstract: The invention refers to novel propenecarboxylic acid amidoxime derivatives furthermore N-oxides and/or geometrical isomers and/or optical isomers and/or pharmaceutically suitable acid addition salts and/or quaternary derivatives thereof. The novel compounds are suitable for the treatment of a state connected with oxygen deficit and/or energy deficit, or a disease based on PARP inhibition, especially an autoimmune or neurodegenerative disease, and/or a viral disease, and/or a disease caused by a toxic effect.Type: GrantFiled: March 13, 2001Date of Patent: May 3, 2005Assignee: N-Gene Research Laboratiories Inc.Inventors: Peter Literati Nagy, Balazs Sumegi, Kalman Takacs
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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: 6875759Abstract: A method for the treatment of cancer and pain in an animal subject is disclosed, comprising administering to said animal in need of such treatment an effective amount of a compound of formula I: wherein R1-R6 are defined herein. Pharmaceutical compositions comprising one or more compounds of formula I and a pharmaceutically acceptable carrier are also disclosed.Type: GrantFiled: July 21, 2000Date of Patent: April 5, 2005Assignee: Kadmus PharmaceuticalsInventors: Andrzej W. Lipkowski, Kelvin Gee
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Patent number: 6776911Abstract: The present invention refers to the use of novel molecules able to bind tenaciously to silica, borosilicate and silicate surfaces, and thus to modify their properties and characteristics. When applied to silica-based chromatography, it offers important advantages in all cases in which it is necessary to modulate the interaction of analytes with the stationary phase. In capillary zone electrophoresis (CZE), such compounds will eliminate or invert the electroendoosmostic (EEO) flow, greatly simplifying the analysis of negatively-charged compounds and permitting the analysis of bio(macro)molecules via the direct use of naked capillaries.Type: GrantFiled: July 3, 2002Date of Patent: August 17, 2004Inventors: Attilio Citterio, Roberto Sebastiano, Cecilia Gelfi, Pier Giorgio Righetti
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Patent number: 6734177Abstract: The present invention relates to certain salts of discodermolide acid, pharmaceutical compositions containing said salts, the use of said salts in treating tumors and to a process for making said salts.Type: GrantFiled: April 15, 2002Date of Patent: May 11, 2004Assignee: Novartis AGInventors: Frederick R. Kinder, Jr., Prasad K. Kapa, Eric M. Loeser
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Patent number: 6703425Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disordersType: GrantFiled: November 15, 2002Date of Patent: March 9, 2004Assignee: Eli Lilly and CompanyInventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6579881Abstract: A 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: wherein A, B, C, D, T, Y, and Z each represent a methine or a nitrogen linkage; R1, R2, R3, R4, and R5 each represent a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3. The compounds have serotonin antagonism. They are therefore clinically useful as medicaments, in particular, for treating, ameliorating, and preventing spastic paralysis. They are also useful as central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 18, 2001Date of Patent: June 17, 2003Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: 6448243Abstract: A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, R4 and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3.) The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.Type: GrantFiled: August 11, 1999Date of Patent: September 10, 2002Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: 6281393Abstract: Mannich polyols having a viscosity of from 300 to 3,500 cps (0.3 to 3.5 Pa*s) at 25° C. are prepared by admixing a phenol, an alkanolamines, and formaldehyde mixed in molar ratios of from 1:1:1 to 1:2.2:2.2 resulting in an initiator which can be alkoxylated using a mixture of ethylene oxide and propylene oxide to prepare polyols that have a nominal functionality of from 3 to 5.4.Type: GrantFiled: September 3, 1999Date of Patent: August 28, 2001Assignee: The Dow Chemical CompanyInventors: Nelson F. Molina, Stanley E. Moore
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Patent number: 6232314Abstract: Arylalkylpiperazine compounds (1) wherein B is aryl or optionally substituted aryl; R1 is hydroxy; R2 and R3 are the same or different and are independently selected from hydrogen or C1-3 alkyl; m is 0, 1 or 2; D is a linking chain of atoms which may be optionally substituted and which contains from 1 to 8 atoms in the chain; E is a phenolic antioxidant group or a corresponding amino derivative thereof wherein the phenolic hydroxyl is replaced by amino, are disclosed. The compounds have both free radical scavenging activity and block excitatory amino acid activity. Some compounds of the present invention also display an affinity for voltage-sensitive sodium channels.Type: GrantFiled: March 18, 1999Date of Patent: May 15, 2001Assignee: Monash UniversityInventors: Bevyn Jarrott, Philip Mark Beart, William Roy Jackson, Vijaya Bhaskar Kenche, Alan Duncan Robertson, Maree Patricia Collis
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Patent number: 6013801Abstract: A method for preparing aminoethylethanolamine, and/or hydroxyethylpiperazine is described. Reaction of ethylene oxide with ethylendiamine, piperazine, or a mixture of both produces these compounds.Type: GrantFiled: October 30, 1998Date of Patent: January 11, 2000Assignee: Akzo Nobel N.V.Inventors: Juhan Koll, deceased, Magnus Frank
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Patent number: 5945393Abstract: Novel nonionic gemini surfactants are extremely effective emulsifiers for oil-in-water emulsions that provide improved detergency at even low concentration levels. The surfactants are characterized by the formula: ##STR1## wherein R.sub.1 is independently H or a C.sub.1 to C.sub.22 alkyl, R.sub.2 is C.sub.6 to C.sub.22 alkyl and R.sub.3 is D.sub.1 --R.sub.4 --D.sub.1 or R.sub.4 --D.sub.1 --R.sub.4 wherein R.sub.4 is independently a C.sub.1 -C.sub.10 alkyl group, --O--R.sub.5 --O--, or aryl, e.g. phenyl, and D.sub.1 is independently --O--, an amide group ?--C(O)N(R.sub.6)--!, an amino group ?--N(R.sub.6)--!, --O--R.sub.5 --O--, or aryl. (EO).sub.a (PO).sub.b is a polyether group and Z is a C.sub.1 -C.sub.4 alkyl, or an alkylaryl or hydrogen wherein EO represents ethyleneoxy radicals, PO represents propyleneoxy radicals, a and b are numbers of from 0 to 100, a is preferably from about 0 to about 30 and b is preferably from about 0 to 10, wherein a plus b is at least one, and the EO and PO alkyl or alkylaryl.Type: GrantFiled: November 7, 1997Date of Patent: August 31, 1999Assignee: Rhodia Inc.Inventors: David James Tracy, Ruoxin Li, Manilal S. Dahanayake, Jiang Yang
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Patent number: 5874436Abstract: The invention relates to triphenylalkyl antibacterial compounds of the general formula: ##STR1## pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are thus useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.Type: GrantFiled: April 23, 1997Date of Patent: February 23, 1999Inventors: James P. Demers, Sigmond Johnson, Michele Ann Weidner-Wells, Ramesh M. Kanojia, Stephanie A. Fraga, Dieter Klaubert
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Patent number: 5872117Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: November 4, 1997Date of Patent: February 16, 1999Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita