The Part Of The Chain Between The Ether Oxygen And Amino Nitrogen Consists Of Two Unsubstituted Saturated Carbons Patents (Class 564/354)
  • Patent number: 9464033
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: October 11, 2016
    Assignee: ACUCELA INC.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Patent number: 9452153
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: May 22, 2015
    Date of Patent: September 27, 2016
    Assignee: ACUCELA INC.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, Jr., Ryo Kubota
  • Patent number: 9056849
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: March 26, 2014
    Date of Patent: June 16, 2015
    Assignee: ACUCELA INC.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, Ryo Kubota
  • Publication number: 20150148426
    Abstract: The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 28, 2015
    Applicant: INTEGRATIVE RESEARCH LABORATORIES SWEDEN AB
    Inventors: Clas SONESSON, Jonas KARLSSON, Peder SVENSSON
  • Publication number: 20150141417
    Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: May 14, 2012
    Publication date: May 21, 2015
    Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
  • Patent number: 8895782
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: November 25, 2014
    Assignee: Acucela Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Publication number: 20140221384
    Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: ERIMOS PHARMACEUTICALS LLC
    Inventors: Jonathan Daniel Heller, Qingqi Chen, Rocio Alejandra Lopez, Amanda Jean Morris
  • Publication number: 20140221286
    Abstract: It is discovered that sodium-channel blockers inhibit the secretion of glucagon from pancreatic alpha cells. The present disclosure, based on such discoveries, provides compositions and methods for the treatment of hyperglycemia and related diseases and conditions with Na-channel blockers.
    Type: Application
    Filed: September 20, 2012
    Publication date: August 7, 2014
    Inventors: Luiz Belardinelli, Arvinder Dhalla
  • Patent number: 8766007
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: July 1, 2014
    Assignee: Acucela Inc
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Patent number: 8716529
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: May 6, 2014
    Assignee: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, Ryo Kubota
  • Publication number: 20140073814
    Abstract: Disclosed is a process for preparing an aryloxyalkylene amine compound via an aminoethylation reaction comprising: a) reacting an aromatic hydroxyl compound in the presence of a basic catalyst with a 2-oxazolidinone compound of the formula II to form an intermediate reaction product; wherein R3 is selected from the group consisting of hydrogen or lower alkyl having 1 to 6 carbon atoms, R4 is selected from the group consisting of hydrogen, straight or branched chain alkyl having from one to six carbon atoms, phenyl, alkaryl, or arylalkyl; and b) reacting the intermediate product of step a) with a polyalkylene polyamine.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 13, 2014
    Applicant: Chevron Oronite Company LLC
    Inventors: Patrick J. McDougall, James Saenz, David Lao
  • Patent number: 8633251
    Abstract: The subject of the invention is a group of new derivatives of aminoalkanols, 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: Grant
    Filed: January 19, 2009
    Date of Patent: January 21, 2014
    Assignees: Uniwersytet Jagiellonski
    Inventors: Henryk Marona, Anna Waszkielewicz, Katarzyna Kiec-Kononowicz
  • Publication number: 20130303531
    Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: May 14, 2012
    Publication date: November 14, 2013
    Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
  • 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: 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: 8492589
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: July 23, 2013
    Assignee: Acucela Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • 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
  • Patent number: 8389771
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: March 5, 2013
    Assignee: Acucela, Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Publication number: 20130030026
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 31, 2013
    Applicant: Acucela Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Publication number: 20130018077
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: Acucela Inc.
    Inventors: Ian Leslie Scott, Vladmir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Patent number: 8299307
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: October 30, 2012
    Assignee: Acucela Inc.
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Publication number: 20120214852
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: November 8, 2011
    Publication date: August 23, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
  • 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: 20120046247
    Abstract: This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.
    Type: Application
    Filed: August 16, 2011
    Publication date: February 23, 2012
    Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
  • Publication number: 20120041038
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 16, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
  • Publication number: 20120041039
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 16, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
  • Publication number: 20110318280
    Abstract: Polymeric anti-microbial agents produced by substituting the nitrogen atoms in the backbone of ethylenimine polymers, for example, substitution with aralkyl groups, are provided. The agents are believed to have low human toxicity while being effective against a variety of pathogens and are useful in applications involving human contact, such as cosmetics, hair care products and textiles, as well as in applications with much less human contact, such as coatings.
    Type: Application
    Filed: September 7, 2011
    Publication date: December 29, 2011
    Inventors: Xinyu Huang, Ted Deisenroth, Andrea Preuss, Sophie Marquais-Bienewald, Carmen Hendricks-Guy, John Jennings
  • Patent number: 8022252
    Abstract: Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.
    Type: Grant
    Filed: August 25, 2008
    Date of Patent: September 20, 2011
    Assignee: Tranzyme Pharma Inc.
    Inventors: Pierre Deslongchamps, Yves Dory, Kamel Benakli, Éric Marsault, Luc Ouellet, Mahesh Ramaseshan, Martin Vezina, Daniel Fortin, Ruoxi Lan, Shigui Li, Gérald Villeneuve, Hamid R. Hoveyda, Sylvie Beaubien, Mark L. Peterson
  • 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
  • Publication number: 20090062353
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: June 30, 2008
    Publication date: March 5, 2009
    Inventors: Ian Leslie Scott, Vladimir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Patent number: 7488833
    Abstract: A process for the enantioselective preparation of amino alcohols of formula I by enantioselective hydrogenation of amino ketones of the formula II in the presence of a non-racemic catalyst. The catalyst is a transition-metal complex in which the transition metal is complexed to a chiral diphosphine ligand.
    Type: Grant
    Filed: August 1, 2003
    Date of Patent: February 10, 2009
    Assignee: Merck Patent GmbH
    Inventors: Joachim Kralik, Kai Fabian, Christoph Mürmann, Norbert Schweickert
  • Patent number: 7473804
    Abstract: The present invention provides novel crystalline polymorph forms of atomoxetine hydrochloride denominated Forms B and C and methods for their preparation, as well as methods for the preparation of Form A. The present invention provides pharmaceutical compositions that comprise atomoxetine hydrochloride Form B, Form C, or mixtures thereof that can be used to treat attention deficit/hyperactivity disorder.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: January 6, 2009
    Assignee: Teva Pharmaceutical Fine Chemicals s.r.l.
    Inventors: Judith Aronhime, Stefano Bianchi, Eugenio Castelli, Paola Daverio, Silvia Mantovani, Adrienne Kovacsne-Mezei
  • Publication number: 20080255124
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
    Type: Application
    Filed: October 13, 2005
    Publication date: October 16, 2008
    Applicant: Smithkline Beecham Corporation
    Inventors: Philip Stewart Turnbull, Andrew Lamont Larkin, Istvan Kaldor, Rodolfo Cadilla, David John Cowan, Eugene Stewart
  • Patent number: 7423181
    Abstract: The invention provides novel alkoxyaminochalcone derivatives and analogues thereof. Use of the compounds, or compositions comprising them, as pharmaceutically active agents, in particular against bacterial and parasitic infections, is also disclosed. The invention further relates to a method for detecting inhibitory effects against e.g., bacteria, parasites, fungi, and helminths. The chalcones of the invention carry amino substituents and exhibit enhanced biological effects combined with improved metabolic and physicochemical properties, making the compounds useful as drug substances, in particular as antiparasitic, bacteriostatic, and bacteriocidal agents.
    Type: Grant
    Filed: May 19, 2003
    Date of Patent: September 9, 2008
    Assignee: Lica Pharmaceuticals A/S
    Inventors: Simon Feldbæk Nielsen, Thomas Boesen, Mogens Larsen, Mette Bjerg Nielsen, Hasse Kromann
  • 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: 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: 6900243
    Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: May 31, 2005
    Assignee: AstraZeneca AB
    Inventors: David Cheshire, Stephen Connolly, David Cox, Antonio Mete
  • 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
  • Publication number: 20040039201
    Abstract: The present invention relates to improved covalent coupling of two or more entities such as biomolecules, polymer compositions, organic/inorganic molecules/materials, and the like, including their combinations, through one or more novel reactive groups attached to linker groups of 2-1000 atoms length. The present invention also contemplates the use of bifunctional bridge molecules to link two or more entities, wherein the functional groups of the bridge molecules are the novel reactive groups of the present invention.
    Type: Application
    Filed: November 14, 2002
    Publication date: February 26, 2004
    Inventors: Ananda G. Lugade, Kurt D. Hoffacker, Adam J. Jenkins, Karri L. Michael-Ballard, Leonid Patsenker, Ewald Terpetchnixg
  • 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: 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: 6310252
    Abstract: There is provided compounds of formula I, wherein R1 represents C3-5 alkyl; and R2 and R3 independently represent C1-3 alkyl; provided that when R2 and R3 both represent ethyl, then R1 does not represent n-butyl, i-butyl or n-pentyl; or a pharmaceutically acceptable salt thereof, which are useful as anaesthetics, in particular local anaesthetics and especially topically applied local anaesthetics.
    Type: Grant
    Filed: January 27, 1997
    Date of Patent: October 30, 2001
    Assignee: AstraZeneca AB
    Inventor: Rune Sandberg
  • 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: 6255496
    Abstract: Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.
    Type: Grant
    Filed: April 27, 1999
    Date of Patent: July 3, 2001
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jacques Banville, Yonghua Gai, Graham Johnson, Fred Christopher Zusi, James R. Burke
  • Patent number: 6235792
    Abstract: The present invention relates to a novel monophosphate salt of isopropyl-methyl-[2-(3-n-propoxyphenoxy)ethyl]amine. Moreover, the present invention also relates to a process for the preparation of the monophosphate salt of isopropyl-methyl-[2-(3-n-propoxyphenoxy)ethyl]amine as well as a pharmaceutical formulation containing it and its use in medicine.
    Type: Grant
    Filed: March 8, 1999
    Date of Patent: May 22, 2001
    Assignee: Astra AB
    Inventors: Karol Horvath, Ulf Larsson, Rune Sandberg
  • 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: 5959103
    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 30, 1998
    Date of Patent: September 28, 1999
    Assignee: Eli Lilly and Company
    Inventors: Henry Uhlman Bryant, Jeffrey Alan Dodge, Charles Willis Lugar, III