Amino Nitrogen Attached To Aryl Ring Or Ring System By An Acyclic Carbon Or Chain Patents (Class 564/323)
  • Patent number: 10730825
    Abstract: Methods are provided herein for the treatment of ophthalmic diseases or conditions such as an ophthalmic disease or disorder associated with diabetes in a patient. Also provided herein are methods of treating retinopathy of prematurity in a patient. Further, provided herein are methods for treating wet age-related macular degeneration in a patient. The methods comprise administration of compounds disclosed herein to a patient in need thereof that inhibit or slow one or more signs or symptoms of such conditions.
    Type: Grant
    Filed: April 30, 2018
    Date of Patent: August 4, 2020
    Assignee: ACUCELA INC.
    Inventors: Claes Olof Bavik, Susan Hayes Henry, Ryo Kubota, Vladimir A. Kuksa
  • Patent number: 10471027
    Abstract: Described herein are methods for the treatment of an ophthalmic disease or disorder comprising the administration of non-retinoid visual cycle modulators. Ophthalmic diseases and disorders which can be treated according to the methods provided herein include age-related macular degeneration (AMD), Stargardt's disease, glaucoma, and other disorders that adversely affect the retina.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: November 12, 2019
    Assignee: ACUCELA, INC.
    Inventors: Ryo Kubota, Nancy Boman, Claes Bavik, Ian L. Scott
  • Patent number: 9309211
    Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: April 12, 2016
    Assignee: Centaurus Biopharma Co., Ltd.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
  • Patent number: 9133154
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said 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: Grant
    Filed: March 11, 2014
    Date of Patent: September 15, 2015
    Assignee: ACUCELA INC.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Patent number: 8993807
    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: Grant
    Filed: November 8, 2011
    Date of Patent: March 31, 2015
    Assignee: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
  • Patent number: 8987262
    Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: March 24, 2015
    Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de Bordeaux
    Inventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
  • Patent number: 8981153
    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: Grant
    Filed: May 19, 2011
    Date of Patent: March 17, 2015
    Assignee: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
  • Publication number: 20150051199
    Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.
    Type: Application
    Filed: October 31, 2012
    Publication date: February 19, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
  • Patent number: 8846766
    Abstract: Provided is a drug substance and a method of treating an ailment comprising administering an oral dose of a drug product comprising the drug substance wherein the drug substance comprises an organic acid addition salt of methadone. The organic acid addition salt is selected from the group consisting of pamoate and xinafoate wherein the drug substance is bioavailable under gastrointestinal administration but is not bioavailable under administration at a mucosal membrane other than gastrointestinal or release from a depot injectable product.
    Type: Grant
    Filed: July 29, 2013
    Date of Patent: September 30, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol, Michael L. English
  • Patent number: 8829244
    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: Grant
    Filed: September 14, 2012
    Date of Patent: September 9, 2014
    Assignee: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
  • Publication number: 20140094492
    Abstract: Derivatives of sulindac that lack cyclooxygenase inhibitory activity are provided along with pharmaceutical compositions containing them and use for treatment or prevention of cancer. The derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.
    Type: Application
    Filed: March 30, 2012
    Publication date: April 3, 2014
    Applicant: Southern Research Institute
    Inventors: Robert Reynolds, Bini Mathew, Gary A. Piazza
  • Patent number: 8629301
    Abstract: The present invention relates to the economical and separation of benzphetamine hydrochloride and methamphetamine by liquid extraction. An extraction process employing a suitable organic solvent and water at a pH in the range of from about 6 to about 8 provides excellent removal of the methamphetamine by dissolution in the water phase while the benzphetamine dissolves in the organic phase. Simple separation of the two phases results in separation of the two amines.
    Type: Grant
    Filed: November 2, 2005
    Date of Patent: January 14, 2014
    Assignee: Mallinckrodt LLC
    Inventor: Keith G. Tomazi
  • Patent number: 8609736
    Abstract: The present invention is directed to use of a series of compounds and compositions comprising the same for activating telomerase and treating diseases, disorders and/or conditions related thereto.
    Type: Grant
    Filed: June 4, 2008
    Date of Patent: December 17, 2013
    Assignee: Ben-Gurion University of the Negev Research and Development Authority
    Inventors: Aviv Gazit, Shimon Slavin, Esther Priel, Sara Yitzchak
  • Patent number: 8604245
    Abstract: The present invention relates to a novel class of tri-aryl compounds, compositions comprising the same and processes for the preparation thereof.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: December 10, 2013
    Assignee: Ben-Gurion University of the Negev Research and Development Authority
    Inventors: Esther Priel, Aviv Gazit, Shimon Slavin, Sara Yitzchak
  • Patent number: 8501996
    Abstract: The present invention relates to novel iminecalixarene derivatives, method of preparation thereof, and self-assembled monolayer prepared by the method, fixing method of oligo-DNA by using the self-assembled monolayer, and oligo-DNA chip prepared by the method. Also, the present invention relates to novel aminocalixarene derivatives, method of preparation thereof, and self-assembled monolayer prepared by the method, fixing method of oligo-DNA wherein the oligo-DNA is voluntarily fixed by molecular recognition on said self-assembled monolayer in a liquid phase, and oligo-DNA chip prepared by the method.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: August 6, 2013
    Assignee: Biometrix Technology Inc.
    Inventors: Tae Sun Kim, Keum Soo Song, Jung Hoon Kim, Hyung Sub Kim
  • Publication number: 20130150545
    Abstract: Novel benzoxazine-thiol adducts are described, which may be may be cured to produce compositions useful in coating, sealants, adhesive and many other applications.
    Type: Application
    Filed: February 11, 2013
    Publication date: June 13, 2013
    Applicant: 3M INNOVATIVE PROPERTIES COMPANY
    Inventor: 3M INNOVATIVE PROPERTIES COMPANY
  • Patent number: 8461371
    Abstract: The present invention relates to a method of enantioselective addition to imines, including: reacting R3CH?NY with R4ZnR5 in the presence of a compound represented by the following formula (I), in which Y, R1, R2, R3, R4 and R5 are defined the same as the specification. Accordingly, the present invention can prepare secondary amines in high yields and enantiomeric excess by the above-mentioned method.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: June 11, 2013
    Assignee: National Tsing Hua University
    Inventors: Biing-Jiun Uang, Wei-Ming Huang
  • Patent number: 8389758
    Abstract: Novel benzoxazine-thiol adducts are described, which may be may be cured to produce compositions useful in coating, sealants, adhesive and many other applications.
    Type: Grant
    Filed: January 12, 2010
    Date of Patent: March 5, 2013
    Assignee: 3M Innovative Properties Company
    Inventors: Ilya Gorodisher, Robert J. Webb, Robert J. Devoe
  • Patent number: 8329951
    Abstract: The invention provides a process for preparing diphenylmethanediamine, comprising the steps of a) reacting aniline with formaldehyde in the presence of an acid, b) neutralizing the acid with ammonia, c) separating the reaction mixture from step b) into an aqueous phase and an organic phase, d) treating the aqueous phase obtained in step c) with an oxide or hydroxide of an alkaline earth metal, e) separating off the ammonia obtained in step d).
    Type: Grant
    Filed: January 2, 2008
    Date of Patent: December 11, 2012
    Assignee: BASF SE
    Inventors: Veronika Wloka, Torsten Mattke, Daniel Breuninger, Markus Siegert
  • Patent number: 8288591
    Abstract: A variety of curing agents for epoxy resins and methods for preparation thereof are disclosed, including compounds having the structures of formulas III and IV: wherein each of R1, R2, R3, R4, and R5 is independently selected from the group consisting of H, methyl, ethyl, n-propyl, iso-propyl, a butyl, and phenyl. Epoxy-based compositions including various curing agents are also disclosed. Other epoxy curatives containing amino, phenol, and/or imine groups are disclosed.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: October 16, 2012
    Assignee: Designer Molecules, Inc.
    Inventor: Stephen M Dershem
  • Publication number: 20120034270
    Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
    Type: Application
    Filed: October 16, 2009
    Publication date: February 9, 2012
    Applicant: Akaal Pharma Pty Ltd
    Inventors: Damian W. Grobelny, Gurmit S. Gill
  • Patent number: 8013188
    Abstract: The present invention relates to novel iminecalixarene derivatives, method of preparation thereof, and self-assembled monolayer prepared by the method, fixing method of oligo-DNA by using the self-assembled monolayer, and oligo-DNA chip prepared by the method. Also, the present invention relates to novel aminocalixarene derivatives, method of preparation thereof, and self-assembled monolayer prepared by the method, fixing method of oligo-DNA wherein the oligo-DNA is voluntarily fixed by molecular recognition on said self-assembled monolayer in a liquid phase, and oligo-DNA chip prepared by the method.
    Type: Grant
    Filed: May 11, 2006
    Date of Patent: September 6, 2011
    Assignee: Biometrix Technology Inc.
    Inventors: Tae Sun Kim, Keum Soo Song, Jung Hoon Kim, Hyung Sub Kim
  • Patent number: 7982071
    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: Grant
    Filed: October 3, 2008
    Date of Patent: July 19, 2011
    Assignee: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
  • Patent number: 7858825
    Abstract: The invention provides compounds that are useful as linkers for solid phase synthesis and as protecting groups, and methods for producing and using the same.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: December 28, 2010
    Assignee: Colorado State University Research Foundation
    Inventors: Michio Kurosu, Dean Crick
  • Publication number: 20100312004
    Abstract: Novel benzoxazine-thiol adducts are described, which may be may be cured to produce compositions useful in coating, sealants, adhesive and many other applications.
    Type: Application
    Filed: January 12, 2010
    Publication date: December 9, 2010
    Inventors: Ilya Gorodisher, Robert J. Webb, Robert J. Devoe
  • Publication number: 20100144977
    Abstract: A variety of curing agents for epoxy resins and methods for preparation thereof are disclosed, including compounds having the structures of formulas III and IV: wherein each of R1, R2, R3, R4, and R5 is independently selected from the group consisting of H, methyl, ethyl, n-propyl, iso-propyl, a butyl, and phenyl. Epoxy-based compositions including various curing agents are also disclosed. Other epoxy curatives containing amino, phenol, and/or imine groups are disclosed.
    Type: Application
    Filed: November 20, 2009
    Publication date: June 10, 2010
    Applicant: DESIGNER MOLECULES, INC.
    Inventor: Stephen M. Dershem
  • Publication number: 20100063075
    Abstract: A compound of formula (1): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
    Type: Application
    Filed: October 15, 2009
    Publication date: March 11, 2010
    Inventors: Eva Altmann, Rene Beerli, Marc Gerspacher, Johanne Renaud, Sven Weiler, Leo Widler
  • Publication number: 20080220407
    Abstract: The presently described subject matter is directed to water-soluble conjugated polyene compounds that exhibit aggregation induced emission, as well as to water dispersible, fluorescent, polymeric microparticles and/or nanoparticles comprising the water-soluble conjugated polyene compounds. Also provided are methods of making and using the compounds and particles. The described conjugated polyene compounds are useful as bioprobes for the detection biomacromolecules, as well as in the manufacture of sensors.
    Type: Application
    Filed: December 10, 2007
    Publication date: September 11, 2008
    Applicant: The Hong Kong University of Science and Technology
    Inventors: Benzhong Tang, Yuning Hong, Matthias Haeussler, Hui Tong, Yonggiang Dong, Zhen Li, Changmin Xin
  • Patent number: 7416824
    Abstract: According to the present invention, an enamine compound having a specific structure is used as an organic photoconductive material. This enamine compound is obtained based on asymmetrical secondary naphtylamine which is readily available at a lowest price, by introducing phenyl groups containing substituents, as constituents units of the enamine part and presents excellent compatibility with binder resins, will not present detrimental effects such as partial crystallization at film forming and have a high charge mobility. The compound is able to realize highly reliable electrophotographic photoreceptor and an image forming apparatus which present a high electrostatic potential, high sensitivity and high enough light response and are excellent in durability and will not degrade in these characteristics under a low-temperature environment or in a high-speed process and will not lower in these characteristics even due to exposure to light.
    Type: Grant
    Filed: May 10, 2004
    Date of Patent: August 26, 2008
    Assignee: Sharp Kabushiki Kaisha
    Inventors: Akihiro Kondoh, Takatsugu Obata, Kazuya Ishida
  • Patent number: 7034015
    Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: April 25, 2006
    Assignee: Leo Pharma A/S
    Inventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
  • Patent number: 6861561
    Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.
    Type: Grant
    Filed: September 26, 2002
    Date of Patent: March 1, 2005
    Assignee: G. D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
  • Patent number: 6797841
    Abstract: Novel benzophenone derivatives and methods of making and using the same are disclosed. The novel compounds can display highly active photoinitiation and photopolymerization properties.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: September 28, 2004
    Assignee: Albemarle Corporation
    Inventors: John Gabriel Santobianco, Rajamani Nagarajan, August John Muller, Joseph Stanton Bowers, Jr.
  • Patent number: 6781015
    Abstract: Novel benzophenone derivatives and methods of making and using the same are disclosed. The novel compounds can display highly active photoinitiation and photopolymerization properties.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: August 24, 2004
    Assignee: Albemarle Corporation
    Inventors: John Gabriel Santobianco, Rajamani Nagarajan, August John Muller, Joseph Stanton Bowers, Jr.
  • Patent number: 6762323
    Abstract: Novel benzophenone derivatives and methods of making and using the same are disclosed. The novel compounds can display highly active photoinitiation and photopolymerization properties.
    Type: Grant
    Filed: October 1, 2002
    Date of Patent: July 13, 2004
    Assignee: Albemarle Corporation
    Inventors: John Gabriel Santobianco, Rajamani Nagarajan, August John Muller, Joseph Stanton Bowers, Jr.
  • Publication number: 20040096904
    Abstract: Disclosed are efficient methods for loading amino derivatives onto trityl chloride resins and for cleaving chemically modified amino derivatives from trityl chloride resins. Methods for making a library of discrete chemically modified amino derivatives also disclosed.
    Type: Application
    Filed: September 23, 2003
    Publication date: May 20, 2004
    Inventors: Yuan-Ping Pang, Jewn Giew Park
  • Patent number: 6518314
    Abstract: Compositions comprising a pharmaceutically effective amount of a compound that impedes disruption of intact dense microspheres (DMS) by acting on DMS either to prevent disruption, or if disrupted, act on pre-disrupted DMS in such a way that, when the composition is administered to a test animal that has received an injection of DMS, it reduces the mean volume of tissue occupied by disrupted DMS, reduces the ratio of the number of inflammatory cells per DMS, or increases the ratio of the number of macrophages containing disrupted DMS per DMS, are useful for treating cerebral amyloidosis.
    Type: Grant
    Filed: October 6, 2000
    Date of Patent: February 11, 2003
    Assignee: Nymox Corporation
    Inventors: Paul Averback, Hossein Ghanbari, Iraj Beheshti, David Morse
  • Patent number: 6451817
    Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether, amino, hydrazino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: September 17, 2002
    Assignee: Eli Lilly and Company
    Inventor: Brian S. Muehl
  • Patent number: 6391892
    Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)2CH3, CO(CH2)3CH3, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; and pharmaceutically acceptable salts thereof. The invention further provides pharmaceutical compositions containing compounds of formula I and methods of use for the compounds of formula I.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: May 21, 2002
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Jeffrey A. Dodge
  • Patent number: 6384053
    Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: May 7, 2002
    Assignee: Eli Lilly and Company
    Inventor: Brian S. Muehl
  • Patent number: 6379590
    Abstract: A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D wherein A′ is selected from the group consisting of —Br, —Cl, —F, —NO2, and —CN; A is selected from the group consisting of —NO2, —CN, —CO2R, —C(O)R, —SO2R, —SO2RF, —C(CN)═C(CN)2 and —CH═C(CN)2; RF is —CpF2p+1, p=from about 0 to about 10; R is an straight, branched or cyclic aliphatic alkyl group having about 1 to 10 carbon atoms, or an aromatic group such as phenyl or naphthyl; and is a carbonyl or a protected carbonyl such as a ketal or thio-ketal such as wherein R′ is —CrH2r+1; R″ is —(CH2)r—; and r is independently 2 or 3, with a nucleophilic reagent in the presence of an aprotic solvent
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: April 30, 2002
    Assignee: AlliedSignal Inc.
    Inventors: Chengjiu Wu, Jianhui Shan
  • Patent number: 5939554
    Abstract: A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a serine ester derivative with an aryl metal reagent to form diarylaminopropanediol. A diarylmethyloxazolidinone compound is also provided.
    Type: Grant
    Filed: April 17, 1997
    Date of Patent: August 17, 1999
    Assignee: NDSU Research Foundation
    Inventors: Mukund P. Sibi, Prasad K. Despande, Anthony J. LaLoggia
  • Patent number: 5643950
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: July 1, 1997
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: James P. Demers, Sigmond Johnson, Michele Ann Weidner-Wells, Ramesh M. Kanojia, Stephanie A. Fraga, Dieter Klaubert
  • Patent number: 5623087
    Abstract: A method for preparing a diarylalanine compound is provided. The method includes reacting a diarylaminopropanediol with a reducing agent to form a diarylaminopropanol compound and/or contacting a serine ester derivative with an aryl metal reagent to form diarylaminopropanediol. A diarylmethyloxazolidinone compound is also provided.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: April 22, 1997
    Assignee: NDSU-Research Foundation
    Inventors: Mukund P. Sibi, Prasad K. Despande, Anthony J. LaLoggia
  • Patent number: 5578685
    Abstract: Curing components containing amino groups for curing epoxy resins are obtained by the reaction of alkylated polyhydroxy aromatics (A) with polyamines (B) and aldehydes (C) by the mechanism of the Mannich reaction. The preparation of curable mixtures and varnish formulations is also disclosed. The curing components and curable mixtures can also be employed at a low temperature.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: November 26, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Uwe Neumann, Claus Godau
  • Patent number: 5576108
    Abstract: Curing components containing amino groups for curing epoxy resins are obtained by the reaction of alkylated polyhydroxy aromatics (A) with polyamines (B) and aldehydes (C) by the mechanism of the Mannich reaction. The preparation of curable mixtures and varnish formulations is also disclosed. The curing components and curable mixtures can also be employed at a low temperature.
    Type: Grant
    Filed: September 9, 1994
    Date of Patent: November 19, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Uwe Neumann, Claus Godau
  • Patent number: 5525633
    Abstract: The present invention relates to novel triaryl-ethylene derivatives that are useful as anti-neoplastic agents, antiatherosclerotic agents, and hypocholesterolemic agents.
    Type: Grant
    Filed: June 15, 1994
    Date of Patent: June 11, 1996
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Donald P. Matthews, Alan J. Bitonti, William A. Van Sickle, Donald A. Kaplan
  • Patent number: 5495048
    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: June 17, 1994
    Date of Patent: February 27, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Philipe Guerry, Synese Jolidon, Olivier Morand
  • Patent number: 5464836
    Abstract: A description follows of benzophenones having an antifungal activity and responding to the general formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, the same or different, represent C.sub.1 -C.sub.6 alkyl groups, C.sub.7 -C.sub.10 arylalkyl groups; or R.sub.1 and R.sub.2, considered jointly with N, represent a C.sub.3 -C.sub.8 heterocyclic group or a C.sub.2 -C.sub.7 heterocyclic group containing a second hetero-atom selected from O and S, said heterocyclic groups being optionally subsituted with one or more C.sub.1 -C.sub.4 alkyl groups;R.sub.3 and R.sub.4, the same or different, represent H atoms, C.sub.1 -C.sub.3 alkyl groups;K represents an oxygen atom or methylene;A represents a benzene group, optionally sustituted with one or more halogen atoms, C.sub.1 -C.sub.4 alkyl or haloalkyl groups, C.sub.1 -C.sub.4 alkoxylics, C.sub.1 -C.sub.4 haloalkoxylics;Y represents a C.sub.6 -C.sub.10 aryl group; said group may be optionally substituted with one or more halogen atomos, C.sub.1 -C.sub.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: November 7, 1995
    Assignee: Ministero dell'Universita` e della Ricerca Scientifica e Tecnologica
    Inventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Raul Riva, Carlo Garavaglia, Luigi Mirenna
  • Patent number: 5410080
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each selected from the group consisting of C.sub.1 -C.sub.2 lower alkyl; X is NH or S; and n is a whole number within the range of 1-4 inclusive; and when n=0, X is (CH.sub.2).sub.3 and the pharmaceutically acceptable salts thereof have been shown to be effective in treating tamoxifen resistant tumors.
    Type: Grant
    Filed: February 10, 1994
    Date of Patent: April 25, 1995
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Alan J. Bitonti, Russell J. Baumann
  • Patent number: 5395853
    Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: March 7, 1995
    Assignee: Burroughs Wellcome Co.
    Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth