Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Cyclic Imides, Naphthisatins, Etc.) Patents (Class 548/451)
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8415485
    Abstract: Methods for preparation of isoindolin-1-one compounds are described.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: April 9, 2013
    Assignee: Celgene Corporation
    Inventors: Anthony J. Frank, Hon-Wah Man, Chuansheng Ge, Manohar Saindane
  • Patent number: 8283477
    Abstract: The present invention relates to a method of preparing N-substituted maleimide in high purity and high yield, wherein, unlike a conventional method of preparing N-substituted maleimide after preparing N-substituted maleamic acid, an organic solvent, an acid catalyst, a dehydration co-catalyst and a stabilizer are added into a reactor without separately preparing N-substituted maleamic acid, and then a primary amine is added into the reactor to form an amine salt, maleic anhydride is added into the reactor, and the resulting mixture is subjected to a dehydration-cyclization reaction, wherein water produced during the reaction is azeotropically distilled with the organic solvent so as to effectively suppress formation of a maleimide polymer.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: October 9, 2012
    Assignee: Korea Kumho Petrochemical Co., Ltd.
    Inventors: Jin-Eok Kim, Seung-il Kim, Han-Jin Kwag
  • Patent number: 8207213
    Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
    Type: Grant
    Filed: February 1, 2007
    Date of Patent: June 26, 2012
    Assignee: Glaxo Group Limited
    Inventors: Mark Patrick Healy, Gerard Martin Paul Giblin, Helen Susanne Price
  • Patent number: 8093283
    Abstract: Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: January 10, 2012
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge, Jean Xu
  • Patent number: 8026270
    Abstract: The present invention relates to naphthalene derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: September 27, 2011
    Assignee: Glaxo Group Limited
    Inventors: Gerard Martin Paul Giblin, Mark Patrick Healy, Helen Susanne Price
  • Publication number: 20110092561
    Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
    Type: Application
    Filed: February 1, 2007
    Publication date: April 21, 2011
    Inventors: Mark Patrick Healy, Gerard Martin Paul Giblin, Helen Susanne Price
  • Patent number: 7893101
    Abstract: Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: February 22, 2011
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge, Jean Xu
  • Publication number: 20100076048
    Abstract: The present invention relates to indole derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.
    Type: Application
    Filed: October 15, 2007
    Publication date: March 25, 2010
    Inventors: Gerard Martin Paul Giblin, Mark Patrick Healy
  • Publication number: 20100069457
    Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1R2R3, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
    Type: Application
    Filed: July 26, 2007
    Publication date: March 18, 2010
    Inventors: Gerard Martin Paul Giblin, Mark Patrick Healy, Helen Susanne Price
  • Publication number: 20090318523
    Abstract: The present invention relates to benzoisoindole phenylacetic acid derivatives, corresponding pharmaceutical compositions, preparation processes and uses in medicine as EP4 receptor angonists.
    Type: Application
    Filed: November 19, 2007
    Publication date: December 24, 2009
    Inventors: Gerald Martin Paul Giblin, Mark Patrick Healy, Helen Susanne Price
  • Publication number: 20090312388
    Abstract: The present invention relates to naphthalene derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.
    Type: Application
    Filed: July 26, 2007
    Publication date: December 17, 2009
    Inventors: Gerard Martin Paul Giblin, Mark Patrick Healy, Helen Susanne Price
  • Publication number: 20090082577
    Abstract: The present invention provides fluorescent compounds of formula (I) and methods monitoring protein-protein interactions.
    Type: Application
    Filed: September 22, 2008
    Publication date: March 26, 2009
    Applicant: Massachusetts Institute of Technology
    Inventors: Barbara Imperiali, Eugenio Vazquez
  • Publication number: 20090030061
    Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein R1 to R8, X, and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
    Type: Application
    Filed: February 12, 2007
    Publication date: January 29, 2009
    Inventors: Mark Patrick Healy, Gerard Martin Paul Giblin, Neil Derek Miller
  • Patent number: 7427638
    Abstract: Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (?) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.
    Type: Grant
    Filed: April 13, 2005
    Date of Patent: September 23, 2008
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge
  • Patent number: 7345062
    Abstract: Imido and amido substituted acylhydroxamidic acids which reduce the levels of TNF? and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propandylamino)propanoate.
    Type: Grant
    Filed: February 25, 2004
    Date of Patent: March 18, 2008
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W Muller, Shaei Y Huang
  • 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: 6924297
    Abstract: Compounds of formula (I) and pharmaceutically acceptable derivatives thereof bind with high affinity to the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: August 2, 2005
    Assignee: SmithKline Beecham Corporation
    Inventors: Gerard Martin Paul Giblin, Haydn Terence Jones, Andrew McMurtrie Mason, Neil Derek Miller, Susan Roomans, Stephen Edward Shanahan, Ann Louise Walker
  • 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: 6777437
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment of depression, anxiety disorders, premature ejaculation, chronic pain, obsessive-compulsive disorder, feeding disorders, premenstrual dysphoric disorder, panic disorders and psychotic disorders including bipolar disorder and schizophrenia.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: August 17, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald J. Mattson, Derek John Denhart, Jeffrey A. Deskus, Jonathan L. Ditta, Lawrence R. Marcin, James R. Epperson, John D. Catt, Dalton King, Mendi A. Higgins
  • 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.
  • Patent number: 6756398
    Abstract: Compounds of Formula I wherein R1a, R1b, R2b, R3b, R3a, R2a, B1, B2, Z, A2 and A1 are as defined in the specification, enantiomers thereof, pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially for treatment of conditions associated with reductions in nicotinic transmission. Compounds of the invention enhance the efficacy of agonists at nicotinic receptors.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: June 29, 2004
    Assignee: Astrazeneca AB
    Inventors: Michael Balestra, David Gurley, James Rosamond
  • Patent number: 6699899
    Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.
    Type: Grant
    Filed: December 21, 1999
    Date of Patent: March 2, 2004
    Assignee: Celgene Corporation
    Inventors: Hon-Wah Man, George W Muller, Shaei Y Huang
  • Patent number: 6605626
    Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: September 21, 2001
    Date of Patent: August 12, 2003
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6576780
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: October 13, 2000
    Date of Patent: June 10, 2003
    Assignee: GD Searle & Company
    Inventors: Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth
  • Patent number: 6313122
    Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: November 6, 2001
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
  • Patent number: 6294674
    Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds. wherein Q is an un-natural amino acid. More particurlarly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthiritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
    Type: Grant
    Filed: March 2, 1999
    Date of Patent: September 25, 2001
    Assignee: Warner-Lambert Company
    Inventors: Joseph Armand Picard, Drago Robert Sliskovic
  • Patent number: 6288063
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula (T)xA—B—D—E—G wherein A is an aryl or heteroaryl rings; B is an aryl or heteroaryl ring or a bond; each T is a substituent group; x is 0, 1, or 2; the group D represents the group E represents a two or three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents and with the proviso that when G is each of the substituents on E is an independent substituent; and include pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 27, 1998
    Date of Patent: September 11, 2001
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, David Ross Brittelli, William Riley Schoen, Sookhee Nicole Ha
  • Patent number: 6030967
    Abstract: A compound of the formula: whereinQ is an optionally substituted carbon atom or N(O)p wherein p is 0 or 1;Y is an optionally substituted methylene group, S(O)q wherein q is an integer of 0 to 2, or an optionally substituted imino group;Z.sup.1 is a C.sub.1-3 alkylene group which may have an oxo group or a thioxo group and may contain etherified oxygen or sulfur within the carbon chain;Z.sup.2 is an optionally substituted C.sub.1-3 alkylene group;Ar is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group;one of R.sup.1 and R.sup.2 is a hydrogen atom, a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group;the other is a halogen atom, a hydroxyl group, an optionally substituted lower alkyl group, or an optionally substituted lower alkoxy group; orR.sup.1 and R.sup.2 taken together with adjacent --c.dbd.c-- form a ring; andring A is a benzene ring which may be substituted in addition to R.sup.1 and R.
    Type: Grant
    Filed: October 30, 1997
    Date of Patent: February 29, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Masaki Ogino
  • Patent number: 6020358
    Abstract: Phenethylsulfones substituted in the position .alpha. to the phenyl group with a 1-oxoisoindoline or 1,3-dioxoisoindoline group reduce the levels of TNF.alpha. in a mammal. Typical embodiments are 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-aminoisoindoline- 1,3-dione and 2-[1-(3-cyclopentyloxy-4-methoxyphenyl)-2-methylsulfonylethyl]isoindoline- 1,3-dione.
    Type: Grant
    Filed: October 30, 1998
    Date of Patent: February 1, 2000
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Hon-Wah Man
  • Patent number: 6002017
    Abstract: A compound comprising ##STR1## wherein R.sub.f is a perfluorinated moiety which may contain one or more catenary ether oxygen atoms, Q is a linking group selected from alkylene groups having 1 or 2 carbon atoms, sulfonamido groups or combinations thereof, and R.sup.1 is a perfluoroalkyl group.
    Type: Grant
    Filed: December 2, 1997
    Date of Patent: December 14, 1999
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Alan D. Rousseau, Marvin E. Jones, Seyed A. Angadjivand
  • Patent number: 5977379
    Abstract: The invention relates to the preparation of halogenated imides derived from hydrazine, a halogen and a dicarboxylic acid anhydride and capable of being employed as fireproofing agents for plastics.A dicarboxylic acid anhydride is halogenated with bromine, chlorine or a mixture thereof and then the product thus obtained is subsequently reacted with hydrazine. No prior purification or isolation of the intermediate halogenated anhydride is required.
    Type: Grant
    Filed: March 19, 1992
    Date of Patent: November 2, 1999
    Assignee: Atochem
    Inventors: Evelyne Bonnet, Bernard Gurtner
  • Patent number: 5968945
    Abstract: Novel amides and imides are inhibitors of tumor necrosis factor.alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. Typical embodiments include 3-(1,3-dioxobenzo[f]isoindol-2-yl)-3-(3-cyclopentyloxy-4-methoxyphenyl)pro pionamide and 3-(1,3-dioxo-4-azaisoindol-2-yl)-3-(3,4-dimethoxyphenyl)-propionarnide.
    Type: Grant
    Filed: January 14, 1998
    Date of Patent: October 19, 1999
    Assignee: Celgene Corporation
    Inventors: George W. Muller, Mary Shire
  • Patent number: 5877200
    Abstract: Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.
    Type: Grant
    Filed: August 29, 1997
    Date of Patent: March 2, 1999
    Assignee: Celgene Corporation
    Inventor: George W. Muller
  • Patent number: 5854273
    Abstract: A compound of formula (I) ##STR1## in which: X and Y, which may be identical or different, represent hydrogen or halogen or alkyl, trihaloalkyl, alkoxy, hydroxyl, cyano, nitro, amino, alkylamino, or dialkylamino,Z represent a linear or branched C.sub.4 to C.sub.12 alkylene chain in which one or more --CH.sub.2 -- are optionally replaced by any one of the following atoms or groups: --NR--, --O--, --S--, --SO--, --SO.sub.2 --, or --CONH--,A forms, with two adjacent carbon atoms of the phenyl ring, a phenyl, naphthyl or tetrahydronaphthyl ring or a heterocycle, ##STR2## represents any one of the groups as defined in the description, its optical isomers and its addition salts with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful as anticancer agents.
    Type: Grant
    Filed: July 23, 1997
    Date of Patent: December 29, 1998
    Assignee: ADIR et Compagnie
    Inventors: Gilbert Lavielle, Patrick Hautefaye, Ghanem Atassi, Alain Pierre, Laurence Kraus-Berthier, Stephane Leonce
  • Patent number: 5854277
    Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: December 29, 1998
    Assignee: Bayer Corporation
    Inventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, William Harrison Bullock, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, Jill Elizabeth Wood, David Ross Brittelli
  • Patent number: 5654431
    Abstract: Novel 5-alkoxy tryptamine derivatives are provided, corresponding to the general formula: ##STR1## in which R may be alkaline, X may be amino, and Y is various N-heterocyclic or N-branched chain moieties. The compounds show selective binding to 5-HT.sub.1D receptor subtypes, and have potential pharmaceutical utility in manufacture of migraine-treating drugs.
    Type: Grant
    Filed: May 30, 1996
    Date of Patent: August 5, 1997
    Inventors: Qingchang Meng, Abdelmalik Slassi, Sumanas Rakhit
  • Patent number: 5587105
    Abstract: Low molecular weight resins that usually are aliphatic and that include crosslinking thermal functional groups are useful as liquid molding compounds for reaction injection molding or resin transfer molding. The compounds eliminate the need to handle solvents when preparing thermoset composites.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 24, 1996
    Inventors: Clyde H. Sheppard, Hyman R. Lubowitz
  • Patent number: 5565483
    Abstract: There is provided novel substituted 3-phenyl oxindole derivatives of the formula ##STR1## wherein R is hydrogen, hydroxy or fluoro; R.sup.1, R.sup.2, R.sup.3and R.sup.4 each are independently hydrogen, C.sub.1-4 alkyl, halogen, trifluoromethyl, phenyl, p-methylphenyl or p-trifluoromethylphenyl; or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3 or R.sup.3 and R.sup.4 are joined together to form a benzo fused ring;R.sup.5 is hydrogen or C.sub.1-4 alkyl; andR.sup.6 is chlorine or trifluoromethyl;or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof, which are openers of the large-conductance calcium-activated potassium channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 15, 1996
    Assignee: Bristol-Myers Squibb Company
    Inventors: Piyasena Hewawasam, Nicholas A. Meanwell, Valentin K. Gribkoff
  • Patent number: 5520844
    Abstract: Bleaching agents constituted by at least one imidearomatic (poly)peroxyacid, having the formula (I): ##STR1## wherein A represents a residue of a substituted or unsubstituted benzene or naphthalene ring, R is a hydrogen atom, a lower alkyl group, an OH group, a COOH group, a COOOH group or a COOR' group wherein R' represents a C.sub.1 -C.sub.5 alkyl group, and n is an integer from 1 to 5.
    Type: Grant
    Filed: January 4, 1991
    Date of Patent: May 28, 1996
    Assignee: Ausimont S.p.A.
    Inventors: Carlo Venturello, Claudio Cavallotti, Fulvio Burzio
  • Patent number: 5510497
    Abstract: Aliphatic cyclobutene compositions according to the formula ##STR1## can be homopolymerized or copolymerized with a variety of comonomers, including bismaleimides, to produce tough, low dielectric constant resins.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: April 23, 1996
    Assignee: Shell Oil Company
    Inventor: Larry S. Corley
  • Patent number: 5399673
    Abstract: Compounds containing at least one alkenyl group, at least one maleimide group and at least one rodlike mesogenic moiety are prepared by reacting one or more aminophenols containing one or more rodlike mesogenic moieties with a stoichiometric quantity of a maleic anhydride per amine group of said aminophenol and then alkenylating the resulting phenolic functional maleimide.
    Type: Grant
    Filed: February 9, 1993
    Date of Patent: March 21, 1995
    Assignee: The Dow Chemical Company
    Inventor: Robert E. Hefner, Jr.
  • Patent number: 5380650
    Abstract: In an assay in which a ligand is labelled by conjugation to a dihydrophthalazinedione (DPD), e.g. luminol or isoluminol, and the conjugated DPD is reacted with an oxidant, e.g. hydrogen peroxide, and an active heme group catalyst, e.g. microperoxidase, the light intensity is enhanced by certain sterically hindered amines defined as saturated bicyclic compounds having a nitrogen atom at one or both bridgehead positions or a piperidine ring compound having four C.sub.1-4 alkyl groups at the 2- and 6- positions. 1,4-Diazabicyclo[2.2.2]-octane, known as "DABCO" is preferred.
    Type: Grant
    Filed: March 23, 1989
    Date of Patent: January 10, 1995
    Assignee: British Technology Group Ltd.
    Inventors: Geoffrey J. R. Barnard, Dean Goodwin, Robert S. Davidson
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5252560
    Abstract: Compounds are described of the formula ##STR1## wherein: R.sup.1 is C.sub.3-6 alkyl or C.sub.1-3 alkylthioC.sub.1-3 alkyl;R.sup.2 is an optionally substituted C.sub.1-6 alkyl or C.sub.1-6 alkoxy group, aryl, heteroaryl, arylC.sub.1-4 alkyl, heteroarylC.sub.1-4 alkyl or a side-chain of a natural .alpha.-amino acid;R.sup.3 is hydrogen, C.sub.1-6 alkyl, CHR.sup.4 COR.sup.5 (where R.sup.4 is a side-chain of a natural .alpha.-amino acid and R.sup.5 is hydroxyl, C.sub.1-6 alkoxy or NHR.sup.6 where R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group) or a group (CH.sub.2).sub.n X (where n is 1 to 6 and X is hydroxyl, C.sub.1-4 alkoxy, heteroaryl or a group NR.sup.7 R.sup.8 where R.sup.7 and R.sup.8 are each hydrogen or C.sub.1-6 alkyl or the group NR.sup.7 R.sup.
    Type: Grant
    Filed: June 29, 1992
    Date of Patent: October 12, 1993
    Assignee: Glaxo Inc.
    Inventors: Peter L. Myers, Andrew B. McElroy, Michael Gregson, Peter J. Brown, Howard G. Davies, David H. Drewry, Michael A. Foley
  • Patent number: 5238950
    Abstract: A method of inhibiting the binding of PDGF using compounds of the formula I ##STR1## useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery is disclosed.Also disclosed are pharmaceutical compositions and novel PDGF inhibitory compounds of the formula ##STR2## or a pharmaceutically acceptable addition salt thereof, useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery.
    Type: Grant
    Filed: December 17, 1991
    Date of Patent: August 24, 1993
    Assignee: Schering Corporation
    Inventors: John W. Clader, Harry R. Davis, Deborra Mullins, Stuart Rosenblum, Jay Weinstein
  • Patent number: 5237059
    Abstract: A compound capable of generating an acid by light irradiation selected from the group consisting of oxime sulfonic acid esters of formula (I): ##STR1## wherein R.sup.1 is an alkyl group, each of R.sup.2 and R.sup.3 is selected from the group consisting of a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group and a cyano group, and R.sup.2 and R.sup.3 may optionally combine to form a ring; and N-hydroxyimidesulfonic acid esters of formula (II): ##STR2## wherein R.sup.1 is an alkyl group, and A is a group selected from the group consisting of a substituted or unsubstituted arylene group, a substituted or unsubstituted alkylene group and a substituted or unsubstituted alkenylene group, wherein the compound capable of generating an acid by light irradiation is useful as an image-forming materials, etc. and has high reactivity to light of from the near ultraviolet region to the visible region.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: August 17, 1993
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Kan Wakamatsu, Yuichi Wakata
  • Patent number: 5223517
    Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: June 29, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich E. Muller, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
  • Patent number: 5210214
    Abstract: A process for preparing indolenines of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are independently of one another hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, C.sub.3 -C.sub.8 -cycloalkyl, aryl, C.sub.7 -C.sub.20 -alkylphenyl, C.sub.7 -C.sub.20 -phenalkyl, or R.sup.1 and R.sup.2 or R.sup.1 and R.sup.3 together are an unsubstituted or C.sub.1 -C.sub.12 -alkyl-substituted C.sub.3 -C.sub.8 -alkylene chain,X and Y are independently of one another hydrogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.2 -C.sub.8 -alkoxyalkyl, C.sub.2 -C.sub.8 -alkoxycarbonyl, C.sub.1 -C.sub.4 -alkylsulfonyl, halogen, nitro or cyano,by reacting a 4-methylene-1,3-dioxolan-2-one of the formula II ##STR2## where R.sup.1, R.sup.2 and R.sup.3 are each as defined above, with an aniline of the formula III ##STR3## where X and Y are each as defined above, in the presence of a Lewis acid and in the presence or absence of a halide of main group 1 or 2 of the Periodic Table at from 100.degree.
    Type: Grant
    Filed: April 10, 1992
    Date of Patent: May 11, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Diehl, Martin Fischer, Manfred Dimmler
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson