Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 544/14)
  • Patent number: 5919944
    Abstract: Diketopyrrolopyrroles of formula I ##STR1## wherein R.sub.1 is a radical of formula II--Y--X--Z--Q (II),whereinY is --CR.sub.3 R.sub.4, --SO.sub.2 --, --CO--, --Si(Hal).sub.2 --, --POHal--, wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen or C.sub.1 -C.sub.4 alkyl, and Hal is halogen,X is an unsubstituted or substituted carbocylic or heterocyclic arylene group, Z is a single bond, uninterrupted linear or branched C.sub.1 -C.sub.30 alkylene, or linear or branched C.sub.2 -C.sub.30 alkylene which is interrupted once or more than once by a hetero atom, --CH.dbd.CH--, --C.tbd.C--, --N.dbd.CH--, --CH.dbd.N-- or --NH--, or is C.sub.5 -C.sub.12 cycloalkylene,Q is a polyreactive functional group, andR.sub.2 is C.sub.1 -C.sub.6 alkyl, ##STR2## or R.sub.1, and R.sub.7 is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: July 20, 1998
    Date of Patent: July 6, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventor: Sameer Eldin
  • Patent number: 5854241
    Abstract: Disclosed are pyrido?3,2,1-i,j!?3,1!benzoxazine compounds of the formula (I): ##STR1## wherein z represents a radical having the formula: ##STR2## wherein B represents --CH.sub.2 --, --O-- or a direct bond; and the other variables in formula (I) and Z are as described herein. The compounds have antibacterial properties and also disclosed are antibacterial compositions containing them and methods of using them to prevent or combat bacterial infections. Methods for preparing the compounds are also disclosed.
    Type: Grant
    Filed: January 3, 1997
    Date of Patent: December 29, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Hallenbach, Thomas Himmler, Thomas Jaetsch, Burkhard Mielke, Klaus Dieter Bremm, Rainer Endermann, Franz Pirro, Michael Stegemann, Heinz-Georg Wetzstein
  • Patent number: 5849731
    Abstract: The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: December 15, 1998
    Assignee: Toray Industries, Inc.
    Inventors: Hiroshi Nagase, Koji Kawai, Takashi Endo, Shinya Ueno, Masayuki Maeda, Satoshi Sakami
  • Patent number: 5744478
    Abstract: The present invention relates to new thiazolo?3,2-a!quinoline and thiazolo?3,2-a!naphthyridine derivatives of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, Z and X have the meaning indicated in the description, processes for their preparation and their use in antibacterial compositions.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: April 28, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Thomas Jaetsch, Werner Hallenbach, Thomas Himmler, Klaus-Dieter Bremm, Rainer Endermann, Franz Pirro, Michael Stegemann, Heinz-Georg Wetzstein
  • Patent number: 5739130
    Abstract: Heterotricyclic derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino,R.sup.3 is hydrogen or an organic group,R.sup.4 is hydrogen or lower alkyl,R.sup.8 is hydrogen or lower alkyl, and--Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.
    Type: Grant
    Filed: September 4, 1996
    Date of Patent: April 14, 1998
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
  • Patent number: 5728693
    Abstract: Arthropodicidal compounds, compositions and use of compounds having the formula ##STR1##
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: March 17, 1998
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas Martin Stevenson
  • Patent number: 5721355
    Abstract: Compounds useful to attach a fluorescein label to an oligonucleotide are disclosed. To create these compounds, oxygen groups on the fluorescein moiety are protected (e.g. with acyl groups). One then links a phosphoramidite to the fluorescein moiety via an amide or thiourea linkage to an active site on the fluorescein ring. The resulting compound can then be directly linked to an oligonucleotide as it is being formed in an automated synthesizer and then deprotected using the same deprotection conditions as are used to deprotect the oligonucleotides. Such compounds are, inter alia, useful to create labelled primers for DNA sequencing.
    Type: Grant
    Filed: June 25, 1996
    Date of Patent: February 24, 1998
    Assignee: Pharmacia Biotech Inc.
    Inventor: Charles K. Brush
  • Patent number: 5624924
    Abstract: Quinobenzothiazine derivatives of the formula ##STR1## as well as the pharmaceutically acceptable salts, esters, amides and prodrugs thereof are disclosed, wherein R.sup.1 is hydrogen or acarboxy-protecting group, R.sup.2 and R.sup.3 are substitutents, A is oxygen, sulfur, or carbon, Z is a halogen or a nitrogen-containing group, X is hydrogen, halogen or alkyl, and W is hydrogen, alkyl, amino or halogen. The compounds have potent antineoplastic activity.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: April 29, 1997
    Assignee: Abbott Laboratories
    Inventors: Daniel T. Chu, Jacob J. Plattner, Robert Hallas
  • Patent number: 5583223
    Abstract: There are disclosed compounds ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently of one another hydrogen, a C.sub.1 -C.sub.12 alkyl group, a C.sub.1 -C.sub.12 alkoxy group, a C.sub.5 -C.sub.8 cycycloalkyl group, a C.sub.5 -C.sub.8 cycycloalkoxy group, a C.sub.5 -C.sub.8 cycloalkylthio group, a C.sub.6 -C.sub.10 aryl group, a C.sub.6 -C.sub.10 aryloxy group, a C.sub.6 -C.sub.10 arylthio group, nitro, halogen, cyano, --COOH, --COOR.sub.7, --NR.sub.8 R.sub.9 or --CONR.sub.8 R.sub.9, where R.sub.7 is C.sub.1 -C.sub.20 alkyl, C.sub.5 -C.sub.8 cycloalkyl, phenyl or phenyl-C.sub.1 -C.sub.4 alkyl, and R.sub.8 and R.sub.9 are each independently of the other hydrogen, C.sub.1 -C.sub.8 alkyl, phenyl or phenyl-C.sub.1 -C.sub.4 alkyl, X is nitrogen or CR.sub.4, Y is nitrogen or CR.sub.5 and Z is nitrogen or CR.sub.6, and R.sub.4, R.sub.5 and R.sub.6 are each independently of one another hydrogen, a straight-chain or branched C.sub.1 -C.sub.12 alkyl group or a C.sub.6 -C.sub.
    Type: Grant
    Filed: October 2, 1995
    Date of Patent: December 10, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fischer, Beat Schmidhalter, Heinz Wolleb
  • Patent number: 5583135
    Abstract: wherein R.sup.1 is hydrogen, lower alkyl, lower alkoxy, lower alkylthio, halogen, nitro, amino or protected amino,R.sup.2 is hydroxy, protected hydroxy, halogen, amino or protected amino,R.sup.3 is hydrogen or an organic group,R.sup.4 R is hydrogen or lower alkyl,R.sup.8 is hydrogen or lower alkyl, and--Z-- is --O-- or a group of the formula: ##STR2## (in which n is 0, 1 or 2), and pharmaceutically acceptable salts thereof which are useful as a medicament.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: December 10, 1996
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masaaki Matsuo, Kiyoshi Tsuji, Katsuya Nakamura, Glen W. Spears
  • Patent number: 5576313
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.
    Type: Grant
    Filed: August 29, 1994
    Date of Patent: November 19, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Thorsten E. Fisher, John S. Wai, J. Christopher Culberson, Walfred S. Saari
  • Patent number: 5539107
    Abstract: A process for the production of azophenothiazine derivatives having either of the following structures: ##STR1## where X and Y include alkyl, alkoxy, halogen, hydrogen, carboxy, or carboxy alkyl substituents. These compounds are precursors to pharmaceutically active compounds such as pipacetate. The process involves the reaction of a 2-chloropyridine with a 2-mercaptoaniline or a dimer of 2-(2-mercaptophenylamino)pyridine in an inert solvent, e.g., .gradient.-methylpyrolidone in the presence of an oxidizing agent, e.g., performic acid.
    Type: Grant
    Filed: April 17, 1995
    Date of Patent: July 23, 1996
    Assignee: ASTA Medica Aktiengesellschaft
    Inventors: Bernhard Kutscher, Hans-Reinhold Dieter
  • Patent number: 5482936
    Abstract: Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and pharmaceutical formulations containing such compounds. Said compounds are useful to induce interferon biosynthesis in an animal.
    Type: Grant
    Filed: January 12, 1995
    Date of Patent: January 9, 1996
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Kyle J. Lindstrom
  • Patent number: 5446148
    Abstract: 6-aza-benzo[b]-phenothiazine derivatives having the formula, ##STR1## wherein X and Y can be any of hydrogen, lower alkyl, lower haloalkyl, carboxyl or carboxy alkyl are obtained through a reaction of 2-quinioline derivatives having the formula ##STR2## with a suitable 2-mercaptoaniline derivatives or dimers thereof under oxidative or free radical conditions.The 6-aza-benzo[b]-phenothiazine derivative are valuable precursors for pharmaceutically active substances such as pipacetate, isothioperdyl and prothiperdyl.
    Type: Grant
    Filed: March 9, 1994
    Date of Patent: August 29, 1995
    Assignee: Asta Medica Aktiengesellschaft
    Inventors: Bernhard Kutscher, Hans-Reinhold Dieter
  • Patent number: 5403839
    Abstract: Compounds of the formula ##STR1## wherein the broken line represents an optional double bond; X is O, S, CH.sub.2 or CH.sub.2 CH.sub.2, and the pharmaceutically acceptable salts thereof. The compounds are useful in treating inflammation or other prostaglandin or leukotriene mediated diseases.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: April 4, 1995
    Assignee: Pfizer Inc
    Inventors: Banavara L. Mylari, Joseph G. Lombardino, James M. McManus
  • Patent number: 5349062
    Abstract: Compounds of formula I ##STR1## wherein X.sub.1 and X.sub.2 are each independently of the other O, S or Se, and R.sub.1 and R.sub.2 are each independently of the other a monovalent radical of an aliphatic or aromatic hydrocarbon of 1 to 20 carbon atoms which is unsubstituted or substituted by NH.sub.2, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, phenyl or C.sub.3 -C.sub.8 cycloalkyl. The compounds of formula I are able to form electrically conductive charge transfer complexes.
    Type: Grant
    Filed: June 28, 1993
    Date of Patent: September 20, 1994
    Assignee: Ciba-Geigy Corporation
    Inventor: John Zambounis
  • Patent number: 5334589
    Abstract: Compositions of a quinolone carboxylic acids useful for oral or parenteral administration to a human or veterinary patient are disclosed which comprise quinolone carboxylic acid--metal ion--acid complexes in combination with a physiologically acceptable carrier and having a pH of about 4 to about 10, as well as a method for their production and use in treatment. Such compositions are found to cause unexpectedly low levels of vein irritation upon intravenous administration.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: August 2, 1994
    Assignee: Abbott Laboratories
    Inventors: Laman A. Al-Razzak, Francisco J. Alvarez
  • Patent number: 5329006
    Abstract: Chromogenic lactam compounds of the formula ##STR1## in which the ring A is an aromatic or heteroaromatic radical which has 6 ring atoms and may contain a fused aromatic ring, it being possible for both the ring A and the fused ring to be substituted;the ring B is an unsubstituted or substituted benzene ring;Z is ##STR2## R is hydrogen; unsubstituted or substituted C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 10 carbon atoms; unsubstituted or substituted aryl or aralkyl; C.sub.1 -C.sub.12 acyl; N-(lower alkyl)carbamoyl; or N-arylcarbamoyl which is unsubstituted or substituted on the ring;Q is C.sub.1 -C.sub.12 alkylene, aryl-C.sub.1 -C.sub.4 alkylene, 1,2-cycloalkylene, 1,2- or 1,8-arylene or aralkylene; andX.sub.1 and X.sub.2, independently of one another, are each hydrogen; unsubstituted or substituted alkyl having a maximum of 12 carbon atoms; acyl having 1 to 8 carbon atoms; cycloalkyl having 5 to 10 carbon atoms; or unsubstituted or ring-substituted aralkyl or aryl; or (X.sub.1 and X.sub.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: July 12, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Baumann, Ian J. Fletcher
  • Patent number: 5302589
    Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: April 12, 1994
    Assignee: Glaxo, Inc.
    Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
  • Patent number: 5274097
    Abstract: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A--denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X--denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n--denotes a number from 1 to 19, andB--denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.
    Type: Grant
    Filed: April 9, 1991
    Date of Patent: December 28, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe, Peter-Rudolf Seidel, Jorg Traber, Thomas Glaser
  • Patent number: 5223625
    Abstract: The invention relates to a group of new annelated indolo [3,2-c] lactam derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.
    Type: Grant
    Filed: July 16, 1992
    Date of Patent: June 29, 1993
    Assignee: Duphar International Research B.V.
    Inventors: Ineke Van Wijngaarden, Hans H. Haeck, Derk Hamminga, Wouter Wouters
  • Patent number: 5213582
    Abstract: Light-polarizing films or foils, preferably based on a vinyl alcohol homopolymer or copolymer, contain dyes corresponding to the following formula ##STR1## in which R, R.sup.1, T.sup.1, T.sup.2, n, X and Z are as defined in the specification.
    Type: Grant
    Filed: March 11, 1992
    Date of Patent: May 25, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Peter Wild, Uwe Claussen, Friedrich W. Krock
  • Patent number: 5198437
    Abstract: 1,7-Annelated esters and amides of indolecarboxylic acids having formula 2, ##STR1## wherein R.sub.1 is halogen;n has a value of 0-2;Z together with the carbon atom, the nitrogen atom and the intermediate carbon atom, forms a heterocyclic group consisting of 6 ring atoms in which, besides the nitrogen atom already present, a second hetero atom of S is present, which ring may be annelated with a benzene ring;R.sub.3 is hydrogen, halogen, alkyl, alkoxy or alkylthio having 1-4 carbon atoms; andR.sub.2 is a group --CO--Y--R.sub.7 wherein Y is an oxygen atom, or a group --NR.sub.6, wherein R.sub.6 is hydrogen or alkyl having 1-3 C-atoms, and R.sub.7 represents a group of the formula ##STR2## wherein p has the value 1 or 2, q has the value 2 or 3, R.sub.8 is hydrogen or alkyl or hydroxyalkyl having 1 or 2 C-atoms, r is 0 or 1, and R.sub.10 is absent.
    Type: Grant
    Filed: December 17, 1990
    Date of Patent: March 30, 1993
    Assignee: Duphar International Research B.V.
    Inventors: Derk Hamminga, Hans H. Haeck, Ineke Van Wijngaarden, Wouter Wouters
  • Patent number: 5095103
    Abstract: Heterocyclic compounds of the formula ##STR1## with the substituent meanings given in the description, and derivatives thereof are suitable for dyeing and pigmenting the most diverse substrates.
    Type: Grant
    Filed: December 12, 1990
    Date of Patent: March 10, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hans Hochstetter
  • Patent number: 5055579
    Abstract: Compounds of general formula I are disclosed ##STR1## wherein L denotes a hydrogen atom, an aryl radial or a substituent of the formula ##STR2## M denotes an alkylene radical or alkenylene radical or a 1,2-arylene radical,Q denotes a sulfur, selenium or oxygen atom, a dialkylmethylene group, an alken 1,2-ylene radical, a 1,2-phenylene radical or an N-R.sup.1 group,denotes an alkyl, aralkyl, aryloxyalkyl or alkoxyalkyl radical,R.sup.2 and R.sup.3 denote a hydrogen atom or a 4,6-bis-trichloromethyl-s-triazin-2-yl group, andn is 0 or 1.The compounds are suitable for use as photoinitiators in photosensitive systems that are induced to reaction by free radicals or acid cations. The compounds are characterized by high sensitivity in the visible spectral region.
    Type: Grant
    Filed: March 1, 1989
    Date of Patent: October 8, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Georg Pawlowski, Heidrun Lutz
  • Patent number: 5030728
    Abstract: A molecule capable of forming stable complexes with urea, guanidine or amidine compounds and the acid addition salts thereof comprises a nucleus of heterocyclic rings.
    Type: Grant
    Filed: June 2, 1989
    Date of Patent: July 9, 1991
    Assignee: The Research Foundation State University of New York
    Inventor: Thomas W. Bell
  • Patent number: 4997831
    Abstract: The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof.The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.
    Type: Grant
    Filed: August 31, 1989
    Date of Patent: March 5, 1991
    Assignee: Glaxo Group Limited
    Inventors: David E. Bays, Ian H. Coates, Alexander W. Oxford, Peter C. North
  • Patent number: 4977265
    Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.
    Type: Grant
    Filed: May 15, 1990
    Date of Patent: December 11, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Synese Jolidon, Rita Locher, Ivan Kompis, Ekkehard Weiss, Pierre-Charles Wyss
  • Patent number: 4975427
    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, halogen, alkyl and alkoxy of 1 to 5 carbon atoms, hydroxy, trifluoromethyl and nitro, n is 0,1 or 2 and the group: ##STR2## in all possible racemic or optically active isomer forms and their non-toxic, pharmaceutically acceptable acid addition salts having analgesic, anti-anoxic and anti-ischemic neuronal protective properties.
    Type: Grant
    Filed: September 29, 1989
    Date of Patent: December 4, 1990
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Jean-Luc Haesslein, Claude Oberlander
  • Patent number: 4968679
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: May 22, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4950665
    Abstract: The present invention is a method for using thiazin dyes, especially methylene blue, in combination with light to hydroxylate guanosine or deoxyguanosine at the C8 of the purine ring. The number of guanosines in a nucleic acid strand converted to 8-OH-deoxyguanosine (8-OH-dG) or 8-OH-guanosine (8-OH-G) can be controlled through manipulation of the concentration of methylene blue, light intensity and length of exposure, pH, and buffer strength.The method can be used for the selective mutation or modification of either a DNA or a RNA sequence, or the protein expressed therefrom. The method can also be used in the treatment of viral infectons and in cancer. Methylene blue is FDA approved for topical, i.v., and oral administration. Viruses, bacteria, and cells undergoing rapid DNA synthesis are all inactivated by methylene blue in the presence of light or when irradiated.
    Type: Grant
    Filed: October 28, 1988
    Date of Patent: August 21, 1990
    Assignee: Oklahoma Medical Research Foundation
    Inventor: Robert A. Floyd
  • Patent number: 4946847
    Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as hereinafter described, and salts thereof, prepared starting from corresponding tricyclic compounds, are described. The compounds I and some of the said tricyclic compounds have antibacterial activity, and are therefore useful as antibacterial agents.
    Type: Grant
    Filed: November 21, 1988
    Date of Patent: August 7, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Synese Jolidon, Rita Locher, Ivan Kompis, Ekkehard Weiss, Pierre-Charles Wyss
  • Patent number: 4939136
    Abstract: The invention relates to new anellated indole derivatives of general formula 2, ##STR1## wherein p1 R.sub.0 is alkyl or alkoxy having 1-4 C-atoms, phenylalkoxy having 1-3 C-atoms in the alkoxy group, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or a group R.sub.7 S(O).sub.p, wherein R.sub.7 is alkyl having 1-4 C-atoms and p has the value 0, 1 or 2, or R.sub.0 is a group R.sub.8 R.sub.9 N, R.sub.8 R.sub.9 N--CO--CH.sub.2 -- or R.sub.8 R.sub.9 --N--CO wherein R.sub.8 and R.sub.9 are hydrogen or alkyl having 1-4 C-atoms or R.sub.8 R.sub.9 N forms a saturated 5- or 6-membered ring and n has the value 0, 1 or 2, Z together with the carbon atom and nitrogen atom to which Z is bound and the intermediate carbon atom, forms a heterocyclic group consisting of 5-8 ring atoms, in which, in addition to the nitrogen atom already present, a --CO--group or a second hetero atom from the group N, O, S, S-O or SO.sub.
    Type: Grant
    Filed: June 24, 1988
    Date of Patent: July 3, 1990
    Assignee: Duphar International Research B.V.
    Inventors: Hans H. Haeck, Derk Hamminga, Ineke Van Wijngaarden, Wouter Wouters
  • Patent number: 4876342
    Abstract: Oxazine compounds containing basic groups correspond to the formula ##STR1## wherein the symbols are as defined in the Specification. These compounds are suitable for dyeing or printing organic substrates containing hydroxy groups or nitrogen in accordance with known methods. Preferred substrates are textile materials which consist of or contain natural or regenerated cellulose, e.g. cotton, but also bast fibres or leather. Most preferred substrates are paper or paper products. Furthermore, these compounds can be used to prepare all kinds of inks, such as ball-pen inks or printing inks.Similarly, a mixture of one or more of the above compounds together with one or more copper phthalocyanine dyes containing basic and/or cationic groups can be used as dyeing or printing agent.
    Type: Grant
    Filed: May 26, 1988
    Date of Patent: October 24, 1989
    Assignee: Sandoz Ltd.
    Inventor: Reinhard Pedrazzi
  • Patent number: 4873262
    Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.
    Type: Grant
    Filed: December 15, 1987
    Date of Patent: October 10, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 4859667
    Abstract: Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: August 22, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Cheuk K. Lau, Christiane Yoakim, Joshua Rokach, Rejean Fortin, Yvan Guindon
  • Patent number: 4824999
    Abstract: The compound which is 2,3,3a,3b,4,5,6,6a,7,7a-decahydro-4,6,7-metheno-1H-cyclopenta[a]pentalene- 1,3-dicarboxylic acid is useful as an intermediate for production of the corresponding anhydride from which several of the disclosed antipsychotic/anxiolytic agents are prepared.
    Type: Grant
    Filed: September 23, 1988
    Date of Patent: April 25, 1989
    Assignee: American Home Products Corporation
    Inventor: Gary P. Stack
  • Patent number: 4806541
    Abstract: Tetracyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, X, Y, Z and n are as herein described, and salts thereof, are described. The compounds of formula III have antibacterial activity, and are therefore useful as antibacterial agents.
    Type: Grant
    Filed: September 22, 1986
    Date of Patent: February 21, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Synese Jolidon, Rita Locher, Ivan Kompis, Ekkehard Weiss, Pierre-Charles Wyss
  • Patent number: 4797488
    Abstract: Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: ##STR1## in which X is --O--, --S--, --SO--, --SO.sub.2 --, --CR.sub.3 R.sub.4 -- where R.sub.3 and R.sub.4, independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R.sub.3 and R.sub.4 form a cycloalkyl group of of 3 to 5 carbon atoms; n is one of the integers 2, 3, 4 or 5; R is phenyl, halophenyl, trifluoromethylphenyl, alkoxyphenyl in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; R.sub.1 and R.sub.2, taken together, are alkylene of 3 to 5 carbon atoms or alkenylene of 3 to 5 carbon atoms, or taken with the carbon atoms to which they are attached, R.sub.1 and R.sub.2 complete a benzene ring, or a group of the formula: ##STR2## where Y is --CH.sub.2 --, --CH.sub.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: January 10, 1989
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Thomas D. Golobish, Magid A. Abou-Gharbia
  • Patent number: 4762831
    Abstract: A process for the preparation of a 1,8-bridged 4-quinolone-3-carboxylic acid of the formula ##STR1## wherein the substituents are defined hereinbelow. Some of the compound are new. The old and new compounds are antibacterials and promote animal growth.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: August 9, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Michael Schriewer
  • Patent number: 4678499
    Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.
    Type: Grant
    Filed: January 30, 1986
    Date of Patent: July 7, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
  • Patent number: 4667032
    Abstract: Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.
    Type: Grant
    Filed: October 10, 1985
    Date of Patent: May 19, 1987
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Cheuk K. Lau, Christiane Yoakim, Joshua Rokach, Rejean Fortin, Yvan Guindon
  • Patent number: 4552874
    Abstract: The invention relates to pyrazolooxazines, pyrazolothiazines and pyrazoloquinolines defined herein by Formula I. The invention also includes compositions containing said Formula I compounds and methods for the use of said compounds and compositions for their lipoxygenase-inhibiting properties. Also included in the invention are methods for the manufacture of said compounds of Formula I.
    Type: Grant
    Filed: February 1, 1983
    Date of Patent: November 12, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mithat Mardin, Rudolf Sundermann, Friedrich Hoffmeister, Wolf-Dieter Busse, Harald Horstmann, Siegfried Raddatz
  • Patent number: 4532237
    Abstract: Novel substituted and bridged pyridine compounds useful as calcium channel blockers, pharmaceutical compositions thereof, and methods of treatment are disclosed.
    Type: Grant
    Filed: July 30, 1984
    Date of Patent: July 30, 1985
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, Brian T. Phillips
  • Patent number: 4479946
    Abstract: Novel phosphorus esters of amidoximes and methods of preparing same. This invention is also directed to pesticidal compositions comprising an acceptable carrier and a pesticidally effective amount of a compound of this invention, as well as to a method of controlling pests which comprises subjecting the pests to a pesticidally effective amount of a compound of this invention.
    Type: Grant
    Filed: June 17, 1982
    Date of Patent: October 30, 1984
    Assignee: Union Carbide Corporation
    Inventors: Leonard E. Hodakowski, Dean F. Bushey
  • Patent number: 4469866
    Abstract: A novel compound of the formula ##STR1## wherein R is hydrogen, benzyl or (C.sub.1 -C.sub.3)alkyl; R.sup.1 is benzyl or (C.sub.1 -C.sub.4)alkyl and Z.sup.1 taken together with --C.dbd.
    Type: Grant
    Filed: April 25, 1983
    Date of Patent: September 4, 1984
    Assignee: Pfizer Inc.
    Inventor: Joseph A. Kardys
  • Patent number: 4451650
    Abstract: There are disclosed certain 2H-pyrido[4,3-b][1,4]oxazines and 2H-pyrido[4,3-b][1,4]thiazines which possess biological activity. The compounds have the structure: ##STR1## wherein n has a value of 1,2 or 3; X is oxygen or sulfur; R.sub.1 is a lower alkyl group, e.g., an alkyl group containing up to six carbon atoms such as methyl, ethyl, propyl, butyl, etc.; R.sub.2 is a member selected from the group consisting of hydrogen, alkyl radicals having from about one to about 12 carbon atoms, preferably from about one to about six carbon atoms; alkenyl radicals having from about two to about 15 carbon atoms; preferably from about two to about 10 carbon atoms; cycloalkyl radicals having from about three to about 20 carbon atoms, preferably from about three to about 15 carbon atoms; aryl, aralkyl and alkaryl radicals having from about six to about 20 carbon atoms, preferably from about six to about 15 carbon atoms; a halogen radical, e.g.
    Type: Grant
    Filed: October 26, 1982
    Date of Patent: May 29, 1984
    Assignee: Southern Research Institute
    Inventors: Carroll G. Temple, Jr., John A. Montgomery, Robert D. Elliott, Glynn P. Wheeler
  • Patent number: 4358407
    Abstract: Benzothiazine derivatives represented by the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl, alkoxycarbonyl, alkoxalyl, phenyl which may optionally have a substituent or substituents, cycloalkyl or aralkyl, R.sub.2 is hydrogen or alkyl, X is sulphur or oxygen, and Y is methylene or ethylene, and acid addition salts thereof. These compounds are useful as analgesic agents, anti-inflammatory agents, anti-allergic agents, anti-arthritic agents, circulation-improving agents or like pharmaceutics.
    Type: Grant
    Filed: August 24, 1981
    Date of Patent: November 9, 1982
    Assignee: Yoshitomi Pharmaceutical Industries Ltd.
    Inventors: Tetsuo Yokobe, Mitsuru Masago, Yasuaki Chihara, Yutaka Maruyama
  • Patent number: 4316959
    Abstract: Antibiotic A-32256 which is produced by submerged, aerobic fermentation of a Streptomyces sp. NRRL 12067. The antibiotic has shown antibacterial activity against Staphylococcus and Streptococcus and various anaerobic species. In addition, the antibiotic has shown antitrichomonas activity in vitro, as well as activity for improving ruminant feed efficency and as a mosquito larvacide.
    Type: Grant
    Filed: April 28, 1980
    Date of Patent: February 23, 1982
    Assignee: Eli Lilly and Company
    Inventors: Karl H. Michel, Marvin M. Hoehn
  • Patent number: 4238607
    Abstract: The compounds are prepared by cyclizing compounds of formula II ##STR2## wherein R.sup.2 is R.sup.1 or acyl.
    Type: Grant
    Filed: July 9, 1979
    Date of Patent: December 9, 1980
    Assignee: Endo Laboratories Inc.
    Inventor: Parathasarathi Rajagopalan