Hydrogen Or Acyclic Hydrocarbyl Substituents Only Bonded Directly To The Part Of The Chain Between The Ether Oxygen And Amino Nitrogen Patents (Class 564/353)
  • Patent number: 9872824
    Abstract: A composition and a process for straightening hair are disclosed. The process includes coating keratin fibers with a composition comprising a thermally-activated agent and contacting the coated keratin fibers with a heating device at a temperature of at least 185° C. for sufficient time to modify the keratin fibers. The thermally-activated agent comprises a heterocyclic compound containing two heteroatoms selected from nitrogen and oxygen in a 5 or 6-membered ring, such as a cyclic alkylene carbonate.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: January 23, 2018
    Assignee: Lubrizol Advanced Materials, Inc.
    Inventors: Murat Kadir, Mark J. McGuiness
  • Patent number: 9000216
    Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: April 7, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Muhammet Uyanik, Takeshi Yasui
  • Patent number: 8865771
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: October 21, 2014
    Assignee: Vertex Pharamaceuticals Incorporated
    Inventors: Weichuan Caroline Chen, Paul Krenitsky, Andreas Termin, Dean Wilson
  • Publication number: 20130338364
    Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.
    Type: Application
    Filed: March 6, 2012
    Publication date: December 19, 2013
    Applicant: NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
    Inventors: Kazuaki Ishihara, Muhammet Uyanik, Takeshi Yasui
  • Publication number: 20130273800
    Abstract: The present disclosure provides novel oligo phenylene ethynylene (OPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various OPEs show antibacterial, antiviral and anti-fungal activity.
    Type: Application
    Filed: July 13, 2011
    Publication date: October 17, 2013
    Applicant: Office of Technology Licensing
    Inventors: David G. Whitten, Kirk S. Schanze, Eunkyung Ji, Thomas S. Corbitt, Zhijun Zhou, Dimitri Dascier, Ying Wang, Linnea K. Ista, Anand Parthsaray
  • Publication number: 20130237692
    Abstract: Anion exchange-hydrophobic mixed mode ligands and methods of their use are provided.
    Type: Application
    Filed: March 5, 2013
    Publication date: September 12, 2013
    Applicant: Bio-Rad Laboratories, Inc.
    Inventors: Jiali Liao, Russell Frost
  • Publication number: 20130230542
    Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 5, 2013
    Applicants: CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER, UNIVERSITY OF CINCINNATI
    Inventors: Edward J. Merino, James C. Mulloy, Guorui Li, Tiffany Bell-Horwath
  • Patent number: 8470209
    Abstract: A paste composition comprises a dye containing a novel oligomeric compound with improved dispersion performance. The oligomeric compound comprises a tail structure consisting of hydrophilic and hydrophobic blocks and an amine or imidazole head structure. The paste composition can be used to prepare a semiconductor electrode of a solar cell. A semiconductor electrode produced using the paste composition and a solar cell fabricated using the semiconductor electrode exhibit greatly improved power conversion efficiency and superior processability.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: June 25, 2013
    Assignees: Samsung SDI Co., Ltd., Samsung Electronics Co., Ltd.
    Inventors: Eun Sung Lee, Sang Cheol Park, Won Cheol Jung, Jin Young Bae
  • Publication number: 20120183984
    Abstract: The invention provides compounds of formula I F-L-Q (I) where F comprises a fluorophore capable of absorbing energy at an excitation wavelength and, in the absence of a quencher, emitting energy at an emission wavelength, which is different than the excitation wavelength; Q comprises a quencher; L comprises a linker moiety having two ends, one end being covalently bound to F and the other end being covalently bound to Q. The compounds are capable of undergoing a reversible reaction (1), provided below: (1) where Q+ is an oxidized form of Q representing the absence of a quencher, Ox comprises an oxidizing agent, which is capable of oxidizing Q to its oxidized form Q, and Red comprises a reducing agent, which is capable of converting Q back to its reduced form Q. The compounds can undergo photo-induced electron transfer when irradiated with energy and when Q exists in its oxidized form, Q+.
    Type: Application
    Filed: July 22, 2010
    Publication date: July 19, 2012
    Applicant: OPTI MEDICAL SYSTEMS
    Inventors: Huarui He, Chao Lin
  • Publication number: 20120046272
    Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.
    Type: Application
    Filed: August 19, 2011
    Publication date: February 23, 2012
    Applicant: GRUNENTHAL GMBH
    Inventor: Ramesh SESHA
  • Publication number: 20110028562
    Abstract: The subject of the invention is a group of new derivatives of aminoalka?ols, more specifically [(phenoxy)alkyl]aminoalkanols and [(phenoxy)acyl)aminoalkanols, their method of obtaining and their use for production of a medicine which is used in the prophylaxis, prevention and/or treatment of diseases or symptoms having neurological background and for production of a medicine with anticonvulsant activity, which is used in seizures of various origin, also in the limbic system, in myoclonic or sound-induced seizures, in psychomotor epilepsy, as well as in relieving neuropathic or inflammatory pain.
    Type: Application
    Filed: January 19, 2009
    Publication date: February 3, 2011
    Inventors: Henryk Marona, Anna Waszkielewicz, Katarzyna Kiec-Kononowicz
  • Patent number: 7834063
    Abstract: This invention relates to benzonitryl and nitrobenzyl derivatives that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds. These compounds are useful, for example, in the treatment or prophylaxis of conditions or disorders that respond to selective androgen receptor modulation.
    Type: Grant
    Filed: October 13, 2005
    Date of Patent: November 16, 2010
    Assignee: GlaxoSmithKline LLC
    Inventors: Philip Stewart Turnbull, Andrew Lamont Larkin, Istvan Kaldor, Rodolfo Cadilla, David John Cowan, Eugene Lee Stewart
  • Publication number: 20100113606
    Abstract: The present invention relates to new aminopropanol modulators of beta-1 adrenergic receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: November 3, 2009
    Publication date: May 6, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20100081720
    Abstract: The present application describes deuterium-enriched atomoxetine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: December 4, 2009
    Publication date: April 1, 2010
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20090156863
    Abstract: The present invention discloses a process for the preparation of atomoxetine hydrochloride in a pure crystalline form, characterised by an XRPD spectrum as in FIG. 1. It is also object of the present invention to provide methods to obtain pure atomoxetine hydrochloride without the use of methylene chloride.
    Type: Application
    Filed: November 17, 2006
    Publication date: June 18, 2009
    Inventors: Luciana Malpezzi, Angelo Bedeschi, Roberta Pizzocaro
  • Publication number: 20090105347
    Abstract: Thyronamine derivatives and analogs, methods of using such compounds, and pharmaceutical compositions containing them are disclosed.
    Type: Application
    Filed: November 30, 2007
    Publication date: April 23, 2009
    Applicants: The Regents of the University of California, Oregon Health & Science University
    Inventors: Thomas S. Scanlan, Matthew E. Hart, David K. Grandy, James R. Bunzow, Mononori Miyakawa, Edwin Saavedra Tan, Katherine L. Suchland
  • Publication number: 20090082597
    Abstract: The invention relates to the use of copper-catalyzed nucleophilic aromatic substitution reaction for preparing 3-aryloxy-3-arylpropylamines and more specifically to a method of preparing certain 3-aryloxy-3-arylpropylamines and the pharmaceutically acceptable addition salts thereof, comprising reacting an amino alcohol with a haloaromatic compound in the presence of a base and a catalytic copper source, and in the absence of a separate ligand.
    Type: Application
    Filed: July 14, 2006
    Publication date: March 26, 2009
    Applicant: FERMION OY
    Inventors: Arne Grumann, Kari Lappalainen, Peter Maiwald, Pekka Pietikainen, Petteri Rummakko
  • Publication number: 20090069440
    Abstract: The present application describes deuterium-enriched atomoxetine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 21, 2008
    Publication date: March 12, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20080146675
    Abstract: Stable Atomoxetine hydrochloride, a process for the manufacture thereof, the use of stable Atomoxetine Hydrochloride for making a pharmaceutical formulation, a process for the preparation of any form of Atomoxetine Hydrochloride, and an analytical method for analyzing the stability of Atomoxetine Hydrochloride are provided.
    Type: Application
    Filed: February 15, 2008
    Publication date: June 19, 2008
    Inventors: Eugenio Castelli, Paolo Riva
  • Patent number: 7355078
    Abstract: Provided are processes for preparing tomoxetine comprising reacting N-methyl-3-hydroxy-3-phenylpropylamine with dimethylsulfoxide (DMSO) and 2-fluorotoluene in the presence of an alkali base to form tomoxetine. Also provided is the conversion of said tomoxetine into atomoxetine or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 28, 2005
    Date of Patent: April 8, 2008
    Assignee: Teva Pharmaceutical Fine Chemicals S.r.l.
    Inventors: Eugenio Castelli, Giuseppe Lo Monaco, Silvia Mantovani, Paola Daverio, Paolo Riva, Alessandra Vailati, Stefano Bianchi
  • Patent number: 7335659
    Abstract: This invention provides a compound, or its possible salt, having the formula, wherein: Re and ?Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or —C(R4,R5)—, wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2 and R3 are independently H, halogen, —CF3, —OCF3, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo(1C-8C)alkyl; or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-
    Type: Grant
    Filed: February 14, 2003
    Date of Patent: February 26, 2008
    Assignee: N.V. Organon
    Inventors: Hubert Jan Jozef Loozen, Markus Wagener, Gerrit Veeneman, Eduard Willem Zwart
  • Patent number: 7297794
    Abstract: Phenoxy amine compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: November 20, 2007
    Assignee: Emisphere Technologies, Inc.
    Inventors: David Gschneidner, Kelly Kraft, Chen Zhu, Yi Chen
  • Patent number: 7183323
    Abstract: The invention provides sodium channel modulating compounds of formula I: wherein X, Y, Q, R1, w, and R2 have any of the values defined in the specification, and salts thereof, which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of formula (I) or a salt thereof, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).
    Type: Grant
    Filed: April 15, 2004
    Date of Patent: February 27, 2007
    Assignee: Theravance, Inc.
    Inventors: Jason P. Chinn, Seok-Ki Choi, Paul R. Fatheree, Daniel Marquess, S. Derek Turner
  • Patent number: 7169818
    Abstract: The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
    Type: Grant
    Filed: October 3, 2001
    Date of Patent: January 30, 2007
    Assignee: University of Virginia Patent Foundation
    Inventors: Kevin R. Lynch, Timothy L. Macdonald, Christopher E. Heise, Webster L. Santos, Mark D. Okusa
  • Patent number: 6939895
    Abstract: A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: September 6, 2005
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
  • Patent number: 6756508
    Abstract: The present invention relates to new cinnamic acid salts of salmeterol, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions.
    Type: Grant
    Filed: February 13, 2003
    Date of Patent: June 29, 2004
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Guenter Linz, Rainer Soyka
  • Patent number: 6750255
    Abstract: A novel calcium receptor active compound having the formula is provided: Ar1—[CR1R2]p—X—[CR3R4]q—[CR5R6]—NR7—[CR8R9]—Ar2 wherein: Ar1 is selected from the group consisting of aryl, heteroaryl, bis(arylmethyl)amino, bis(heteroarylmethyl)amino and arylmethyl(heteroarylmethyl)amino; X is selected from the group consisting of oxygen, sulfur, sulfinyl, sulfonyl, carbonyl and amino; R1, R2, R3, R4, R5, R6, R7, R8 and R9 are, for example, hydrogen or alkyl; Ar2 is selected from the group consisting of aryl and heteroaryl; p is an integer of from 0 to 6, inclusive; and, q is an integer of from 0 to 14, inclusive.
    Type: Grant
    Filed: January 17, 2002
    Date of Patent: June 15, 2004
    Assignees: NPS Pharmaceuticals, Inc., Kirin Beer Kabushiki
    Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
  • Patent number: 6649800
    Abstract: An improved process for the preparation of polyalkylphenoxyaminoalkanes which comprises the aminoethylation of a polyalkylphenol compound in the presence of a basic catalyst with 2-oxazolidinone or a derivative thereof having the following formula: wherein R1 and R2 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms and wherein the polyalkyl group of said polyalkylphenol has an average molecular weight in the range of about 600 to 5,000 and wherein the process is carried out in the presence of an alcohol.
    Type: Grant
    Filed: October 31, 2002
    Date of Patent: November 18, 2003
    Assignee: Chevron Oronite Company LLC
    Inventor: James A. Gray
  • Patent number: 6486352
    Abstract: A process for the preparation of polyalkylphenoxyaminoalkanes which comprises the aminoethylation of a polyalkylphenol compound in the presence of a basic catalyst with &bgr;-amino alcohol or derivative thereof having the following structure: R1NH—CHR2—CH2—OH and a dialkyl carbonate having the following formula: (R3O)2CO wherein R1 and R2 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms, hydroxylalkylene, phenyl, alkaryl, or aralkyl, R3 is lower alkyl having 1 to about 6 carbon atoms, and wherein the polyalkyl group of said polyalkylphenol has an average molecular weight in the range of about 600 to 5,000. Optionally, an alcohol co-solvent having the structure R4—OH wherein R4 is an alkyl group of about 4 to 10 carbon atoms may be used.
    Type: Grant
    Filed: June 28, 2002
    Date of Patent: November 26, 2002
    Assignee: Chevron Oronite Company LLC
    Inventor: James A. Gray
  • Patent number: 6441205
    Abstract: The invention provides a novel compound 4-(p-methoxy-phenyl)-2-aminobutane exhibiting growth inhibition and antifeedant activity and represented by the structural formula. C11H17ON=4-(p-methoxy phenyl)-2-amino butane and an insecticidal composition comprising an effective amount of the novel compound and appropriate adjuvant.
    Type: Grant
    Filed: May 19, 2000
    Date of Patent: August 27, 2002
    Assignee: Council of Scientific and Industrial Research
    Inventors: Sunil Kumar Chattopadhyay, Koneni Venkata Sashidhara, Vinayak Tripathi, Arun Kumar Tripathi, Veena Prajapati, Sushil Kumar
  • Patent number: 6420354
    Abstract: The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.
    Type: Grant
    Filed: December 8, 1999
    Date of Patent: July 16, 2002
    Assignee: Advanced Medicine, Inc.
    Inventors: Daniel Marquess, Seok-Ki Choi, David T. Beattie, John H. Griffin, Scott Armstrong, Timothy J. Church, Thomas E. Jenkins
  • Patent number: 6384280
    Abstract: A process for the preparation of polyalkylphenoxyaminoalkanes which comprises the aminoethylation of a polyalkylphenol compound in the presence of a basic catalyst with 2-oxazolidinone or a derivative thereof having the following formula: wherein R1 and R2 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms and wherein the polyalkyl group of said polyalkylphenol has an average molecular weight in the range of about 600 to 5,000.
    Type: Grant
    Filed: October 12, 2001
    Date of Patent: May 7, 2002
    Assignee: Chevron Oronite Company LLC
    Inventor: Richard E. Cherpeck
  • Patent number: 6350913
    Abstract: The present invention relates to novel 3-alkoxybenzylamine derivatives of general formula (1): which are useful as medicinal products and in particular as antipsychotic agents.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: February 26, 2002
    Assignee: Pierre Fabre Medicament
    Inventors: Bernard Vacher, Stéphane Cuisiat, Wouter Koek
  • Patent number: 6313350
    Abstract: The present invention provides novel processes for the preparation of Form A of fluoxetine hydrochloride.
    Type: Grant
    Filed: January 31, 2001
    Date of Patent: November 6, 2001
    Inventors: Grayson Walker Stowell, Robert R. Whittle
  • Patent number: 6310250
    Abstract: The present invention provides novel amorphous fluoxetine hydrochloride as a useful intermediate for the preparation of Form A of fluoxetine hydrochloride.
    Type: Grant
    Filed: January 31, 2001
    Date of Patent: October 30, 2001
    Inventors: Grayson Walker Stowell, Robert R. Whittle
  • Patent number: 6310251
    Abstract: The present invention provides novel processes for the preparation of Form A of fluoxetine hydrochloride.
    Type: Grant
    Filed: January 31, 2001
    Date of Patent: October 30, 2001
    Inventors: Grayson Walker Stowell, Robert R. Whittle
  • Patent number: 6265445
    Abstract: The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) wherein R1 and R2, independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R3, R4 and R5, independently from each other, stand for hydrogen or C1-4 alkyl group; R6 represents hydrogen, C1-4 alkyl or benzyl group; R7 means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R2 is different from hydrogen, when R1 is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: July 24, 2001
    Assignees: Gyogyszerkutato Intezet Kft, Szent-Gyorgyi Albert Orvostudomanyi Egyetem
    Inventors: Gyula Papp, András Varró, Péter Mátyus, Ildikó Varga, Tivadar Rettegi, Alice Druga, Antal Simay, Imre Moravcsik, Pál Berzsenyi, Daniella Barlocco, Giorgio Cignarella, Márta Pátfalusi
  • Patent number: 6057358
    Abstract: Novel amine derivatives of the following general formula (I): ##STR1## (wherein) A may denote --(CH.sub.2)--O--, --(CH.sub.2).sub.2 --O--, or --(CH.sub.2).sub.2 --NH--;B may denote --(CH.sub.2).sub.2 --;R.sub.1 may denote a hydrogen atom, a halogen atom, a nitro group, a 1-pyrrolyl group, an acetamido group, an amino group or a dimethylamino group;R.sub.2 may denote a hydrogen atom or a nitro group;R.sub.3 and R.sub.4 may denote a hydrogen atom;R.sub.8a and R.sub.8b which are the same may denote a chlorine atom or a methoxy group;R.sub.9 may denote a hydrogen atom or an amino group;R may denote a methyl group; andX may denote a methanesulfonamido group, a 1-imidazolyl group or a nitro group or a salts thereof are useful as antiarrhythmic drugs.
    Type: Grant
    Filed: May 27, 1997
    Date of Patent: May 2, 2000
    Assignee: C&C Research Labs.
    Inventors: You Sup Chung, Hak Yeop Kim, Kyung Yun Jung, Jae Ki Min, Shigeru Tanabe
  • Patent number: 6057371
    Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: May 2, 2000
    Assignee: Virginia Commonwealth University
    Inventor: Richard A. Glennon
  • Patent number: 6017965
    Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: December 11, 1996
    Date of Patent: January 25, 2000
    Assignee: NPS Pharmaceuticals, Inc.
    Inventors: Alan L. Mueller, Manuel F. Balandrin, Bradford C. VanWagenen, Scott T. Moe, Eric G. DelMar, Linda D. Artman, Robert M. Barmore, Daryl L. Smith
  • Patent number: 5952350
    Abstract: The invention provides a compound of formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical compositions containing a compound of formula I, and methods of using a compound of formula I for inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen dependent cancer.
    Type: Grant
    Filed: October 23, 1997
    Date of Patent: September 14, 1999
    Assignee: Eli Lilly and Company
    Inventors: George Joseph Cullinan, Brian Stephen Muehl
  • Patent number: 5889000
    Abstract: The invention provides naphthofluorene compounds, intermediates, formulations, processes, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.
    Type: Grant
    Filed: September 22, 1997
    Date of Patent: March 30, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Jeffrey Alan Dodge, Charles Willis Lugar, III
  • Patent number: 5866611
    Abstract: Compounds of formula I, and their pharmaceutically acceptable salts, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR.sup.1 R.sup.2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: February 2, 1999
    Assignee: Zeneca Limited
    Inventors: George Robert Brown, Murdoch Allan Eakin, Peter John Harrison, deceased, Keith Blakeney Mallion
  • Patent number: 5792762
    Abstract: The invention provides dihydronaphthofluorene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions.
    Type: Grant
    Filed: September 19, 1997
    Date of Patent: August 11, 1998
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
  • Patent number: 5773469
    Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.
    Type: Grant
    Filed: June 18, 1996
    Date of Patent: June 30, 1998
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Ramesh M. Kanojia, James P. Demers, Dennis J. Hlasta, Sigmond G. Johnson, Dieter H. Klaubert
  • Patent number: 5736568
    Abstract: Compounds of the formula I ##STR1## including pharmaceutically acceptable salts thereof are disclosed in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently represent hydrogen, hydroxy, halo, halogenated alkyl, halogenated alkoxy, alkyl, alkoxy, cyano, a carbamoyl group, carbonyl group, or R.sub.1 and R.sub.2 together with the phenyl ring represent a naphthalene ring (optionally substituted); L.sub.1 represents C.sub.2-6 alkylene; R.sub.5 represents hydrogen or alkyl, R.sub.6 represents hydrogen or alkyl, phenylalkyl (optionally substituted) or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring; L.sub.2 represents a C.sub.1-6 alkylene chain; and R.sub.7 and R.sub.8 independently represent hydrogen or alkyl or R.sub.7 and R.sub.8 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring.
    Type: Grant
    Filed: November 25, 1996
    Date of Patent: April 7, 1998
    Assignee: Knoll Aktiengesellschaft
    Inventors: Paul Rafferty, Gerald Bernard Tometzki
  • Patent number: 5688830
    Abstract: This invention relates to a compound of the Formula I: ##STR1## as a racemic mixture and its individual enantiomers, in particular the (R)-enantiomer, and their pharmaceutically acceptable salts. These compounds are useful as sodium channel blockers, and are particularly useful for the alleviation of neuropathic pain.
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: November 18, 1997
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Lee Allen Flippin, John Cureton Hunter, David Garrett Loughhead, Robert James Weikert
  • Patent number: 5684200
    Abstract: Hydroxylamine ethers I ##STR1## (where X is NO.sub.2, CN, halogen, alkyl or haloalkyl, Y is H, NO.sub.2, CN, halogen, alkyl or haloalkyl, n is 0-2 or 1-4 where Y and all radicals X are halogen and Alk is unsubstituted or substituted alkylene) and their salts with mineral acids or strong organic acids are prepared by reacting either a hydroximino compound II ##STR2## (where R.sup.1 is alkyl, R.sup.2 is alkyl or alkoxy or R.sup.1 +R.sup.2 form an alkylene chain) in the presence of an alkali metal hydroxide, alkali metal alcoholate, alkali metal bicarbonate or alkali metal carbonate as the base, or the corresponding anion II directly, with an alkylating agent III ##STR3## (where R.sup.3 is unsubstituted or substituted alkyl or unsubstituted or substituted phenyl) to give an oximino derivative IV ##STR4## said derivative is cleaved by means of a mineral acid or a strong organic acid to give the salt of I and, if desired, the latter is converted by means of a base into the free compound I.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: November 4, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Albrecht Harreus, Norbert Goetz, Volker Maywald, Harald Rang, Ulf Misslitz, Ulrich Klein
  • Patent number: 5669939
    Abstract: Polyalkylphenoxyaminoalkanes having the formula: ##STR1## wherein R is a polyalkyl group having an average molecular weight in the range of about 600 to 5,000;R.sub.1 and R.sub.2 are independently hydrogen or lower alkyl having 1 to 6 carbon atoms; andA is amino, N-alkyl amino having about 1 to about 20 carbon atoms in the alkyl group, N,N-dialkyl amino having about 1 to about 20 carbon atoms in each alkyl group, or a polyamine moiety having about 2 to about 12 amine nitrogen atoms and about 2 to about 40 carbon atoms.The compounds of formula I are useful as fuel additives for the prevention and control of engine deposits.
    Type: Grant
    Filed: May 14, 1996
    Date of Patent: September 23, 1997
    Assignee: Chevron Chemical Company
    Inventor: Richard E. Cherpeck
  • Patent number: 5637771
    Abstract: A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is C.sub.1-7 -alkyl and the other is C.sub.1-7 -alkyl or C.sub.2-6 -alkenyl-methyl;L is C.sub.1-11 -alkylene or C.sub.2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene;n is 0 or, when L contains an O atom, n is 0 or 1;Q is C.sub.1-7 -alkyl, C.sub.2-10 -alkenyl or a group of formula ##STR2## wherein R is H, halogen, CF.sub.3, CN or NO.sub.2 ; R.sup.3 and R.sup.4 are H, C.sub.1-4 -alkyl or halogen; andR.sup.5 is H or, when R is H, R.sup.5 is H or halogen;or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.
    Type: Grant
    Filed: November 8, 1995
    Date of Patent: June 10, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Philipe Guerry, Synese Jolidon, Olivier Morand