Chalcogen Or Nitrogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 549/21)
  • Patent number: 11965849
    Abstract: A sensor can include one or more of a semiconducting material, an oxidation catalyst, and an oxidation enhancer, the sensor being configured to detect an analyte, such as methane, a thiol, or both.
    Type: Grant
    Filed: April 29, 2021
    Date of Patent: April 23, 2024
    Assignee: Massachusetts Institute of Technology
    Inventors: Timothy Swager, Mate Bezdek, Richard Liu
  • Patent number: 11760743
    Abstract: Para-acyl substituted diazacyclohexenes, medical formulations thereof and methods for making and using the same.
    Type: Grant
    Filed: October 12, 2021
    Date of Patent: September 19, 2023
    Inventors: Bishwajit Nag, Ananda Sen, Nitish Nag, Arjun Sanyal, Srinivasan Narasimhan
  • Patent number: 9889202
    Abstract: A novel delivery system for drugs, and especially macromolecules such as proteins or oligonucleotides through biological membranes is provided, and specifically delivery of siRNA The delivery system comprises conjugation of the macromolecule drug to a moiety that enables effective passage through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: February 13, 2018
    Assignee: Aposense LTD.
    Inventor: Ilan Ziv
  • Patent number: 9687556
    Abstract: A novel delivery system for drugs, and especially macromolecules such as proteins or oligonucleotides through biological membranes is provided, and specifically delivery of siRNA The delivery system comprises conjugation of the macromolecule drug to a moiety that enables effective passage through the membranes. Respectively, novel compounds and pharmaceutical compositions are provided, utilizing said delivery system. In one aspect of the invention, the compounds may be utilized in medical practice, for example, in delivery of siRNA or antisense oligonucleotides across biological membranes for the treatment of medical disorders.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: June 27, 2017
    Assignee: Aposense Ltd.
    Inventor: Ilan Ziv
  • Patent number: 8754208
    Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl)carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: June 17, 2014
    Assignee: International Business Machines Corporation
    Inventors: James L. Hedrick, Alshakim Nelson, Daniel P. Sanders
  • Patent number: 8722900
    Abstract: The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.
    Type: Grant
    Filed: October 30, 2012
    Date of Patent: May 13, 2014
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: TsungYu Hsiao, Julian Paul Henschke, HsinChang Tseng
  • Publication number: 20130296315
    Abstract: The present invention relates to the use of new and known dithiine derivatives for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to new dithiine derivatives, to processes for preparing them, to their use, and to crop protection compositions comprising these new dithiine derivatives.
    Type: Application
    Filed: March 11, 2013
    Publication date: November 7, 2013
    Inventor: Bayer CropScience AG
  • Publication number: 20130211055
    Abstract: Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. The invention provides S-acylated dithioamines which can be selectively activated reducing agents by removal of the S-acyl groups enzymatically or chemically. The invention further provides dithiane precursors of thioamino reducing agents. The invention provides dithioamine reducing agents, S-acylated dithioamines and dithianes which are immobilized on surfaces, including among others, glass, quartz, microparticles, nanoparticles and resins.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 15, 2013
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventor: Wisconsin Alumni Research Foundation
  • Patent number: 8492562
    Abstract: Provided are a polymerizable compound shown below which is useful as a raw material for a polymer having less swelling in developing, a polymer obtained by polymerizing a raw material containing the above polymerizable compound, a photoresist composition which contains the above polymer and which is improved in LWR and an efficient production process for the polymerizable compound described above: wherein n represents an integer of 0 to 2; R1 represents a hydrogen atom, methyl or trifluoromethyl; R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; W represents an alkylene group having 1 to 10 carbon atoms or the like; and Y1 and Y2 represent an oxygen atom or a sulfur atom.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: July 23, 2013
    Assignee: Kuraray Co., Ltd.
    Inventors: Junko Sato, Osamu Nakayama, Takashi Fukumoto
  • Patent number: 8476428
    Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl)carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: July 2, 2013
    Assignee: International Business Machines Corporation
    Inventors: James Lupton Hedrick, Alshakim Nelson, Daniel Paul Sanders
  • Publication number: 20130116444
    Abstract: The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.
    Type: Application
    Filed: October 30, 2012
    Publication date: May 9, 2013
    Applicant: Scinopharm Taiwan, LTD.
    Inventor: Scinopharm Taiwan, LTD.
  • Publication number: 20130090474
    Abstract: The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapropterin.
    Type: Application
    Filed: June 13, 2011
    Publication date: April 11, 2013
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Emanuele Attolino, Mario Michieletti, Davide Rossi, Pietro Allegrini
  • Publication number: 20130005990
    Abstract: Provided are 1) a production process for an acrylic ester derivative capable of being a raw material of a polymer for obtaining a photoresist composition capable of forming a photoresist film which is excellent in a reactivity to acid and a heat stability and is less swollen in developing and which has a refractive index of preferably 1.72 or more in 193 nm and can be patterned, 2) an acrylic ester derivative obtained by the above production process and 3) alcohol and ester which are synthetic intermediates for the above acrylic ester derivative.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 3, 2013
    Applicant: KURARAY CO., LTD.
    Inventors: Osamu NAKAYAMA, Takashi FUKUMOTO
  • Publication number: 20120329731
    Abstract: In one embodiment the invention provides a method of combating cyanide poisoning, which comprises administering to a subject a compound capable of releasing 3-mercapto-pyruvate in vivo. In other embodiments the invention also provides pharmaceutical compositions comprising a compound capable of releasing 3-mercaptopyruvate in vivo, as well as novel compounds that are capable of releasing 3-mercaptopyruvate in vivo.
    Type: Application
    Filed: October 13, 2011
    Publication date: December 27, 2012
    Inventors: Herbert T. Nagasawa, David J.W. Goon, Daune L. Crankshaw, Robert Vince
  • Publication number: 20120270917
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: July 30, 2010
    Publication date: October 25, 2012
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Jun Wang
  • Publication number: 20120142676
    Abstract: Novel derivatives of dihydro-1,4,2-oxathiazine and dihydro-1,4-dithiine oxides, more particularly, novel derivatives of dihydro-1,4,2-oxathiazine and dihydro-1,4-dithiine oxides that target cysteine residues of biomolecules of pharmacological importance are provided as pharmaceutically useful compounds, for example, as anticancer, antiinfectious, antigastric acid secretion, antiosteoporosic, and antiinflammatory agents.
    Type: Application
    Filed: July 27, 2011
    Publication date: June 7, 2012
    Inventors: Gaik-Lean Chee, Walter G. Brouwer, Ewa Osika, Brian B. Hasinoff, A. David Brewer
  • Patent number: 8178700
    Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl) carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.
    Type: Grant
    Filed: May 4, 2009
    Date of Patent: May 15, 2012
    Assignee: International Business Machines Corporation
    Inventors: James L. Hedrick, Alshakim Nelson, Daniel P. Sanders
  • Patent number: 8119820
    Abstract: A method of preparing a sultine from a dihalogeno compound. The method comprises the steps of reacting the dihalogeno compound with a hydroxymethanesulfinate salt in a DMSO solvent so as to prepare the sultine.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: February 21, 2012
    Assignee: Silverbrook Research Pty Ltd
    Inventors: Sutharsiny Indusegaram, Simone Charlotte Vonwiller, Damon Donald Ridley
  • Publication number: 20110009643
    Abstract: Provided are 1) a production process for an acrylic ester derivative capable of being a raw material of a polymer for obtaining a photoresist composition capable of forming a photoresist film which is excellent in a reactivity to acid and a heat stability and is less swollen in developing and which has a refractive index of preferably 1.72 or more in 193 nm and can be patterned, 2) an acrylic ester derivative obtained by the above production process and 3) alcohol and ester which are synthetic intermediates for the above acrylic ester derivative.
    Type: Application
    Filed: February 20, 2009
    Publication date: January 13, 2011
    Applicant: Kuraray Co., Ltd.
    Inventors: Osamu Nakayama, Takashi Fukumoto
  • Publication number: 20100331508
    Abstract: Provided are a polymerizable compound shown below which is useful as a raw material for a polymer having less swelling in developing, a polymer obtained by polymerizing a raw material containing the above polymerizable compound, a photoresist composition which contains the above polymer and which is improved in LWR and an efficient production process for the polymerizable compound described above: wherein n represents an integer of 0 to 2; R1 represents a hydrogen atom, methyl or trifluoromethyl; R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or the like; W represents an alkylene group having 1 to 10 carbon atoms or the like; and Y1 and Y2 represent an oxygen atom or a sulfur atom.
    Type: Application
    Filed: February 20, 2009
    Publication date: December 30, 2010
    Applicant: KURARAY CO., LTD.
    Inventors: Junko Sato, Osamu Nakayama, Takashi Fukumoto
  • Publication number: 20100280242
    Abstract: A method of preparing a cyclic monomer, comprising: forming a first mixture comprising a precursor compound, bis(pentafluorophenyl) carbonate, and a catalyst; wherein the precursor compound has a structure comprising a) two or more carbons, and b) two functional groups selected from the group consisting of primary amine, secondary amine, thiol group, hydroxyl group, and combinations thereof; and agitating the first mixture at a temperature effective to form a second mixture comprising the cyclic monomer, the cyclic monomer selected from the group consisting of a cyclic carbonate, a cyclic carbamate, a cyclic urea, a cyclic thiocarbonate, a cyclic thiocarbamate, and a cyclic dithiocarbonate.
    Type: Application
    Filed: May 4, 2009
    Publication date: November 4, 2010
    Applicant: International Business Machines Corporation
    Inventors: James L. Hedrick, Alshakim Nelson, Daniel P. Sanders
  • Patent number: 7385067
    Abstract: The invention relates to a process for the preparation of compounds containing at least one —CF2—O— bridge in the molecule, in which a) an acid is added onto at least one ketene dithioketal, b) the resultant bis(alkylthio)carbenium salt is reacted with at least one compound having at least one hydroxyl group in the presence of a base, c) and subsequently, preferably in situ, the resultant dithioorthoester is subjected to oxidative fluorodesulfurisation using a fluorinating agent and an oxidant to give the compound containing at least one —CF2—O— bridge in the molecule.
    Type: Grant
    Filed: June 2, 2006
    Date of Patent: June 10, 2008
    Assignee: Merck Patent GmbH
    Inventors: Peer Kirsch, Andreas Taugerbeck, Alexander Hahn
  • Patent number: 6916346
    Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is selected from C1 to C5 alkyl or hydroxyalkyl, a C3 to C6 cyclic ring containing hetero atoms selected from O, S and N atoms, and —CH2—Ar where Ar is an aromatic ring wherein the aromatic ring may be substituted with one or two hydroxy C1 to C3 alkoxy, or amino groups.
    Type: Grant
    Filed: May 5, 2004
    Date of Patent: July 12, 2005
    Assignee: The Procter & Gamble Company
    Inventors: Mu-Ill Lim, Yuh-Guo Pan
  • Patent number: 6875894
    Abstract: The invention relates to bis(alkylthio)carbenium salts of the formula I with the stated definitions for R1, R2, R3 and Y?, and to a process for the preparation thereof. The compounds according to the invention are advantageously suitable as electrophilic reagents for the transfer of fluorinated alkyl and acyl radicals onto nucleophilic compounds.
    Type: Grant
    Filed: February 11, 2002
    Date of Patent: April 5, 2005
    Assignee: Merck Patent GmbH
    Inventors: Peer Kirsch, Andreas Ruhl, Gerd-Volker Röschenthaler, Dmitrii Sevenard
  • Patent number: 6787062
    Abstract: The invention relates to a process for the preparation of compounds having at least one —CF2O— bridge in the molecule, which comprises initially reacting a bis(alkylthio)carbenium salt with a compound containing at least one hydroxyl group in the presence of a base followed by oxidative fluorination, preferably in situ, with a fluorinating agent and an oxidizing agent to form the compound having at least one —CF2O— bridge in the molecule.
    Type: Grant
    Filed: September 3, 2002
    Date of Patent: September 7, 2004
    Assignee: Merck Patent GmbH
    Inventors: Peer Kirsch, Andreas Taugerbeck, Detlef Pauluth, Matthias Bremer
  • Patent number: 6706891
    Abstract: Processes for the preparation of 4,5-bisimino-[1,3]dithiolanes and 2,3-bisimino-[1,4]dithianes are described. The processes involve conversion of an oxalamide to a dithiooxalamide, followed by conversion of the dithiooxalamide to either a 4,5-bisimino-[1,3]dithiolane or a 2,3-bisimino-[1,4]dithiane.
    Type: Grant
    Filed: November 2, 2001
    Date of Patent: March 16, 2004
    Assignee: Eastman Chemical Company
    Inventors: James Allen Ponasik, Jr., Leslie Shane Moody, Peter Borden Mackenzie
  • Patent number: 6664287
    Abstract: This invention comprises administering to a human or animal in need of treatment an effective amount of an antioxidant lipoic acid derivative and/or pharmaceutically acceptable salts and solvates thereof for the treatment or prevention of pathological (inflammatory, proliferative and degenerative diseases, e.g. diabetes mellitus, atherosclerosis, Alzheimer's disease and chronic viral diseases) and non-pathological (e.g. skin aging and wrinkle formation) conditions caused by oxidative damage. Methods of synthesizing novel antioxidant lipoic acid derivatives and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are described. Another aspect of this invention is the use of these antioxidant compositions for the protection of skin from damage caused by ultraviolet radiation and dessication, and to provide improved skin feel by desquamating, cleansing and clarifying the skin.
    Type: Grant
    Filed: March 14, 2001
    Date of Patent: December 16, 2003
    Assignee: Bethesda Pharmaceuticals, Inc.
    Inventors: Mitchell Allen Avery, Harrihar A. Pershadsingh
  • Patent number: 6472488
    Abstract: Polymerizable compositions from novel monomers that correspond to the formula: in which: Z represents H or CH3 and X represents O or S, and Y is a 5- to 8-membered heterocycle consisting of hydrogen, carbon and sulphur atoms and at least two endocyclic sulphur atoms.
    Type: Grant
    Filed: September 20, 2001
    Date of Patent: October 29, 2002
    Assignee: Essilor International Compagnie Generale D'Optique
    Inventors: Florence Caye, Michèle Sindt, Daniel Paquer, Dorothée Jury, Michel Schneider, Jean-Luc Mieloszynski
  • Patent number: 6407136
    Abstract: The invention is directed to 1,4-dithiin- and 1,4-dithiepin-1,1,4,4-tetroxide derivatives useful as galanin receptor antagonists for treating disorders of the central nervous system. Pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions such as an eating disorder, obesity, bulimia nervosa, anorexia nervosa, binge eating, diabetes, dyslipidemia, hypertension, memory loss, sleep disturbances, pain, depression, anxiety, Alzheimer's disease, senile dementia, cerebral hemorrhage, or diarrhea are also described.
    Type: Grant
    Filed: May 2, 2000
    Date of Patent: June 18, 2002
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Malcolm K. Scott, Daniel H. S. Lee, Allen B. Reitz, Tina Morgan Ross, Haou-Yan Wang
  • Patent number: 6369071
    Abstract: An organic compound is provided which contains at least one nitric oxide donor group and at least one group being, or being adapted to be converted in vivo to a free sulfhydryl group. A preferred compound contains at least one sulfhydryl group, either in the reduced —SH form or in the oxidized —S—S-disulfide form.
    Type: Grant
    Filed: December 30, 1999
    Date of Patent: April 9, 2002
    Assignee: Yissum Research Development Company of The Hebrew University of Jerusalem
    Inventor: Abdullah Haj-Yehia
  • Patent number: 6307062
    Abstract: The novel monomers correspond to the formula: in which: Z represents H or CH3 and X represents O or S, and Y is a 5- to 8-membered heterocycle consisting of hydrogen, carbon and sulphur atoms and at least two endocyclic sulphur atoms.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: October 23, 2001
    Assignee: Essilor International Compagnie Generale d'Optique
    Inventors: Florence Caye, Michèle Sindt, Daniel Paquer, Dorothée Jury, Michel Schneider, Jean-Luc Mieloszynski
  • Patent number: 6046228
    Abstract: The present invention is directed to pharmaceutical compositions including a saturated 1,2-dithiaheterocyclic compound having antiviral activity. The present invention also provides a kit containing the pharmaceutical composition and methods of treating or preventing viral disease using the composition, as well as methods for inactivating retrovirus in a body fluid.
    Type: Grant
    Filed: January 4, 1999
    Date of Patent: April 4, 2000
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: William G. Rice, Robert R. Schultz, David C. Baker, Louis E. Henderson
  • Patent number: 6043361
    Abstract: The invention relates to compounds of the formulae: processes for their preparation, polymers, co-polymers or block co-polymers containing them or their use as monomers or co-monomers in free radical polymerisation and in the manufacture of adhesives, dental composites or optical lenses.
    Type: Grant
    Filed: August 26, 1997
    Date of Patent: March 28, 2000
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Richard Alexander Evans, Ezio Rizzardo, Graeme Moad
  • Patent number: 6034087
    Abstract: Nucleoside derivatives represented by formula (I); ##STR1## wherein, R.sub.1 represents hydrogen, phosphate or phosphonate group, R.sub.2 represents substituted or unsubstituted pyrimidine or purine base, and Z represents S, SO, SO.sub.2, O or C; or pharmaceutically acceptable salts thereof. Compound (I) can be obtained by reacting a compound of the formula (II); ##STR2## wherein, R.sub.7 represents hydrogen or hydroxy-protecting group, L represents aromatic or nonaromatic acyl, halide or alkoxy, and Z represents S, SO, SO.sub.2, O or C, with a base.
    Type: Grant
    Filed: June 11, 1997
    Date of Patent: March 7, 2000
    Assignee: Chong Kun Dang Corp.
    Inventors: Jung Woo Kim, Chong Ryul Lee, Koo Hun Chung, Soon Kil Ahn, Kyung Hoi Cha, Hoe Joo Son, Sung Jo Choi, Byeong Seon Jeong, Kyeong Bok Min
  • Patent number: 6025502
    Abstract: The invention relates to an enantioselective method of making methylphenidate and derivatives thereof. The method involves use of a rhodium catalyst, and selectively produces the D-enantiomer of the methylphenidate derivative in excess of the L-enantiomer thereof. Furthermore, the method selectively produces the threo-diastereomer in excess of the erythro-diastereomer. The method is thus suitable for synthesis of D-threo-methylphenidate (the biologically active form of this compound) and derivatives thereof.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: February 15, 2000
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Jeffrey David Winklter, Jeffrey M. Axten, Lori Krim
  • Patent number: 5834508
    Abstract: A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: February 6, 1997
    Date of Patent: November 10, 1998
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
  • Patent number: 5750729
    Abstract: In accordance with this invention novel compounds are provided that are selected from saturated and unsaturated pyrans and furans substituted with at least a phosphonate group and a heterocyclic base. These compounds are useful as antiinfectives, flame retardants, diagnostic oligonucleotides and immunogens.
    Type: Grant
    Filed: February 25, 1997
    Date of Patent: May 12, 1998
    Assignee: Gilead Sciences,Inc.
    Inventors: Petr Alexander, Ernest J. Prisbe
  • Patent number: 5698580
    Abstract: Antiviral agents comprising, as an active ingredient, a 1,4-dihydro-2,3-benzodithiin derivative of the formula ##STR1## wherein each symbol is as defined in the Specification, or a pharmacologically acceptable salt thereof. The antiviral agents of the present invention have superior antiviral activity and are effective for the preventive and therapeutic treatment of viral diseases caused typically by RS virus.
    Type: Grant
    Filed: December 16, 1996
    Date of Patent: December 16, 1997
    Assignee: Rational Drug Design Laboratories
    Inventors: Tsuyoshi Kajiyashiki, Ryu Sato, Tomoyuki Yokota, Kenji Sudo, Wataru Watanabe, Shiro Shigeta
  • Patent number: 5676884
    Abstract: Nonlinear optical (NLO) compositions are disclosed which contain polar disulfone-functionalized molecules (PDFMs) incorporated in a polymeric material. when aligned noncentrosymmetrically in the polymeric material, the PDFMs generate a second-order NLO response. There is also disclosed: a method of preparing a NLO composition; novel PDFMs and novel polymers; and a new process for preparing PDFMs.
    Type: Grant
    Filed: November 20, 1996
    Date of Patent: October 14, 1997
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: George V. Tiers, Robert J. Koshar, Louis M. Leichter
  • Patent number: 5674894
    Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.
    Type: Grant
    Filed: May 15, 1995
    Date of Patent: October 7, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
  • Patent number: 5508275
    Abstract: Lipid-selective antioxidants of the formula I(A).sub.a (L)(X).sub.a, (I),in whichA=an antioxidative component,L=a bridging member,X=a lipophilic componenta and a'=independently of one another the numbers 1 or 2.The compounds are used for the protection of lipid-containing substances against oxidation and in pharmaceuticals for the prophylaxis and treatment of diseases in which bioradicals are involved, in particular of coronary, circulatory and vascular diseases.
    Type: Grant
    Filed: March 15, 1994
    Date of Patent: April 16, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus-Ulrich Weithmann, Gunther Wess, Dirk Seiffge
  • Patent number: 5453518
    Abstract: A compound of the general formula: ##STR1## wherein X represents --CO--, --COO--, --CONH--, --CON(CH.sub.3)--, --CH.sub.2 NH--, --CH.sub.2 N(CH.sub.3)--, --CH.sub.2 NHCO--, --CH.sub.2 N(CH.sub.3)CO--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, or --CH.sub.2 SO.sub.2 --; n represents an integer from 1 to 4; and B represents one of the following groups: ##STR2## wherein R.sub.1 represents a lower alkyl (C.sub.1 -C.sub.4) group; R.sub.2 represents a hydrogen atom or a lower alkyl (C.sub.1 -C.sub.4) group; R.sub.3 represents a hydrogen atom or OR.sub.4 group wherein R.sub.4 represents a lower alkyl (C.sub.1 -C.sub.4) group; p represents an integer from 1 to 3; and Y represents a valence bond (Y1), or one of the following groups: ##STR3## wherein R.sub.2 is as above defined as well as the enantiomers, diastereomers, N-oxides, prodrugs, metabolites, prodrugs of metabolites, and pharmaceutically acceptable salts of these compounds.
    Type: Grant
    Filed: April 9, 1993
    Date of Patent: September 26, 1995
    Assignee: Recordati S.A., Chemical and Pharmaceutical Company
    Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Luciano Guarneri
  • Patent number: 5360815
    Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
    Type: Grant
    Filed: June 23, 1993
    Date of Patent: November 1, 1994
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Rejean Fortin, Yves Girard, Erich Grimm, John Hutchinson, John Scheigetz
  • Patent number: 5296505
    Abstract: The invention relates to a stereospecific derivative of formula: ##STR1## in which R is hydrogen or a C.sub.1 -C.sub.4 thioalkyl. The invention also relates to the use of these compounds for the manufacture of stereospecific retinal or retinoic acid, as well as to a process for preparing the retinoids of formula (I). The invention finally relates to a cosmetic or pharmaceutcial composition which contains at least one compound of formula (I) in a suitable vehicle; the pharmaceutical composition according to the invention may be used for treating dermatological, rheumatic, respiratory or ophthalmological conditions.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: March 22, 1994
    Assignee: L'Oreal
    Inventors: Guy Solladie, Valerie Berl, Jean Maignan
  • Patent number: 5296611
    Abstract: Propenals of formula: ##STR1## in which formula R is H or a C.sub.1 -C.sub.4 thioalkyl radical, the dithiane ring being at the cis position in relation to the aldehyde function when R is H and at the trans position when R is a thioalkyl radical. The invention also relates to two processes for the preparation of these propenals.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: March 22, 1994
    Assignee: L'Oreal
    Inventors: Guy Solladie, Valerie Berl, Jean Maignan
  • Patent number: 5264455
    Abstract: X is hydrogen or --S(O).sub.m --R.sup.1 and Y is hydrogen or S(O).sub.n --R.sup.2, except that X and Y are not both hydrogen, or one of X and Y is --S--alkyl--SH and the other is hydrogen; ##STR2## and the remaining symbols are as defined in the specification.
    Type: Grant
    Filed: July 1, 1991
    Date of Patent: November 23, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Jeffrey O. Saunders, Sam T. Chao, Eric M. Gordon, Dinos P. Santafianos
  • Patent number: 5227398
    Abstract: Hepatopathy improvers contain as an effective ingredient one or more of benzodioxole derivatives represented by the following formula: ##STR1## wherein A means a particular N- or S-containing group. Most of these benzodioxole derivatives are novel.
    Type: Grant
    Filed: November 26, 1991
    Date of Patent: July 13, 1993
    Assignee: Tsumura & Co.
    Inventors: Masayuki Kimura, Shouichi Nishida, Shigefumi Takeda, Kunio Hosaka
  • Patent number: 5190573
    Abstract: Cyclohexenone oxime ethers ##STR1## where R.sup.1 is alkyl;A is substituted or unsubstituted alkylene or alkenylene, where methylene is replaced by an oxygen atom, a sulfur atom, a sulfoxyl group, a sulfonyl group or --NR.sup.a --,Z is phenyl or a 5- or 6-membered heteroaromatic structure;X is substituted or unsubstituted amino, nitro, cyano, halogen, alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbony or phenyl;n is 0 to 3, or 1 to 5 where X is halogen;R.sup.
    Type: Grant
    Filed: May 8, 1991
    Date of Patent: March 2, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Norbert Goetz, Albrecht Harreus, Bruno Wuerzer, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
  • Patent number: 5098928
    Abstract: The ketenedithioacetal derivatives of formula (I) have a potent hypolipidemic and anti-arteriosclerotic effect and are useful for prophylaxis and treatment of arteriosclerosis or hyperlipidemia.
    Type: Grant
    Filed: October 25, 1990
    Date of Patent: March 24, 1992
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Masashi Nagamine, Kunikazu Hiraga, Atsushi Sakai, Matazaemon Uchida
  • Patent number: 5049673
    Abstract: The present invention discloses a new class of calcium specific fluorescent indicator dyes having visible excitation and emission wavelengths. The new fluorescent indicator dyes combine at least one tricyclic chromophore with a tetracarboxylate parent CA.sup.2+ chelating compound having the octacoordinate pattern of liganding groups characteristic of BAPTA to give a rhodamine-like or fluorescein-like fluorophore. Binding of calcium.sup.2+ increases the fluorescence of the new compounds by up to 40-fold. The calcium.sup.2+ dissociation constants are in the range 0.37-2.3 microM, so that the new indicators give better resolution of high [CA.sup.2+ ] levels than were previously obtainable with predecessor compounds such as quin-2 or fluo-2. The visible excitation wavelengths of the new compounds are more convenient for fluorescent microscopy and flow cytometry than the UV required by previous indicators.
    Type: Grant
    Filed: October 30, 1987
    Date of Patent: September 17, 1991
    Assignee: The Regents of the University of California
    Inventors: Roger Y. Tsien, Akwasi Minta