Polycyclo Ring System Having The Oxazine Ring As One Of The Cyclos Patents (Class 544/99)
  • 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: 4990615
    Abstract: Triphendioxazine and triphendithiazine direct dyestuffs of the formula ##STR1## in which the substituents have the meanings given in the description produce on natural and synthetic OH-- and NH-- containing materials clear blue dyeings having good light and wet properties.
    Type: Grant
    Filed: September 12, 1989
    Date of Patent: February 5, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hermann Henk, Wolfgang Harms, Peter Wild
  • Patent number: 4986852
    Abstract: Pigments of the formula I ##STR1## where A is a five- or six-membered aromatic fused or unfused heterocycle which contains one to three hetero atoms from the series consisting of nitrogen and/or oxygen and/or sulfur and which is bonded to the methylene group via a carbon atom, R.sub.1 and R.sub.2 are each hydrogen, alkyl C.sub.1 -C.sub.4, alkylene C.sub.2 or aryl, and together R.sub.1 and R.sub.2 may also be an aliphatic or aromatic ring, R.sub.3 is hydrogen, alkyl C.sub.1 -C.sub.4 hydroxylkyl C.sub.1 -C.sub.3 or alkylene C.sub.2, P is the radical of a polycyclic pigment or a radical of a mix-crystal of polycyclic pigments, and n is a number from 0.0001 to 0.
    Type: Grant
    Filed: December 20, 1988
    Date of Patent: January 22, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Erwin Dietz, Gustav Kapaun, Michael Kappert, Frank Prokschy, Adolf Kroh, Manfred Urban
  • 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: 4968781
    Abstract: A reactive dye of the formula ##STR1## in which Fa is the radical of an organic dye of the monoazo, polyazo, metal complex azo, anthraquinone, phthalocyanine, formazan, azomethine, dioxazine, phenazine, stilbene, triphenylmethane, xanthene, thioxanthone, nitroaryl, naphthoquinone, pyrenequinone or perylenetetracarbimide series, T is a negative substituent, one X is a detachable substituent and the other X is a group of the formula ##STR2## A is arylene, V is hydrogen, a substituted or unsubstituted C.sub.1 -C.sub.4 alkyl radical or a radical of the formula --(CH.sub.2).sub.q --SO.sub.2 --Z, Z is a --CH.dbd.CH.sub.2 or CH.sub.2 --Y radical and Y is an inorganic or organic radical which is detachable under alkaline conditions, q, m and n are independently of one another an integral number from 2 to 6, R and R' are independently of one another hydrogen or substituted or unsubstituted C.sub.1 -C.sub.4 alkyl, and r is 1 or 2.
    Type: Grant
    Filed: March 28, 1988
    Date of Patent: November 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Karl Seitz, Karl Hoegerle
  • Patent number: 4968782
    Abstract: Reactive dyes of the formula ##STR1## in which D is the radial of an anthraquinone, phthalocyanine, formazan, azomethine, dioxazine, phenazine, triphenylmethane, xanthene, thioxanthone, nitroaryl, naphthoquinone, pyrenequinone or perylenetetracarbimide dye; Q is hydrogen or alkyl which has 1 to 4 carbon atoms and can be substituted by carboxyl, sulfo, cyano, hydroxyl, C.sub.1- C.sub.4 alkoxy or halogen; B is a radical --CH.sub.2n, --O--CH.sub.2n or --NH --CH.sub.2n and n is 1 to 6; R is a radical of the formula ##STR2## Z is .beta.-sulfatoethyl, .beta.-thiosulfatoethyl, .beta.-phosphatoethyl, .beta.-acyloxyethyl, .beta.-halogenoethyl or vinyl; alk is an alkylene radical having 1 to 6 C atoms or branched isomers thereof; Y is hydrogen, chlorine, bromine, flourine, hydroxyl, sulfato, acyloxy having 1 to 4 C atoms, cyano, carboxyl, alkoxycarbonyl having 1 to 5 C atoms, carbamoyl or a radical --SO.sub.
    Type: Grant
    Filed: October 13, 1989
    Date of Patent: November 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Athanassios Tzikas, Peter Aeschlimann
  • Patent number: 4962197
    Abstract: A compound having the formula ##STR1## in which X is O, S, or Se; each R.sub.1, R.sub.2, and R.sub.3, independently, is H, a lower alkyl, or aralkyl; A is a saturated or unsaturated ring; and each Z.sub.1, Z.sub.2, Z.sub.3, Z.sub.4, Z.sub.5, Z.sub.6, Z.sub.7, or Z.sub.8, independently, is H or a halogen,provided that when X is O, at least one group Z is a halogen; when either Z.sub.2 or Z.sub.3 is a halogen, at least one of R.sub.2 or R.sub.3 is H; and when both Z.sub.2 and Z.sub.3 are halogens, both R.sub.2 and R.sub.3 are H;or a pharmaceutically acceptable salt thereof.The compounds are useful for photo-inactivation of cancer cells.
    Type: Grant
    Filed: February 12, 1988
    Date of Patent: October 9, 1990
    Assignee: Rowland Institute for Science
    Inventors: James W. Foley, Louis Cincotta
  • Patent number: 4954630
    Abstract: The present invention provides resorufin derivatives of the general formulae: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5, which can be the same or different, are hydrogen, halogen, carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups or lower alkyl or lower alkoxy radicals, which can be substituted by carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups, and wherein R.sup.4 and R.sup.5 can together also represent an anellated aromatic residue, Z is a bridge member, A is the residue of a ligand and n is a whole number of from 1 to 200.The present invention also provides processes for the preparation of these resorufin derivatives, as well as intermediates for the preparation thereof.
    Type: Grant
    Filed: July 24, 1986
    Date of Patent: September 4, 1990
    Assignee: Boehringer Mannheim GmbH
    Inventors: Christian Klein, Hans-Georg Batz, Rupert Herrmann
  • Patent number: 4952679
    Abstract: Reactive dyes suitable for dyeing and printing cellulosic fiber materials by the cold pad-batch process having the formula ##STR1## wherein Fa is a monoazo or polyazo, metal complex azo, anthraquinone, phthalocyanine, formazane, azomethine, dioxazine, phenazine, stilbene, triphenylmethane, xanthene, thioxanthone, nitroaryl, naphthoquinone, pyrenequinone or perylenetetracarbimide dye radical, X.sub.1 is halogen, C.sub.1 -C.sub.4 -alkylsulfonyl, phenylsulfonyl, a sulfonic acid or phosphoric acid group or a quaternized ammonium group, X.sub.2 independently has the meaning of X.sub.1 or is C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by halogen, hydroxy, cyano, carboxyl, sulfo, sulfato, C.sub.1 -C.sub.4 -alkoxycarbonyl or C.sub.1 -C.sub.4 alkoxy, R is hydrogen or C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by halogen, hydroxy, cyano, carboxyl, sulfo, sulfato, C.sub.1 -C.sub.4 -alkoxycarbonyl or C.sub.1 -C.sub.4 -alkoxy, and r is 1 or 2.
    Type: Grant
    Filed: August 19, 1988
    Date of Patent: August 28, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Karl Hoegerle
  • 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: 4942232
    Abstract: Imidazolylmethylene-containing triphendioxazine dyes of the formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, m and n each have defined meanings, A.sup..crclbar. is an anion and F is the radical of a triphendioxazine chromophore of the formula II ##STR2## where X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, L and p each have defined meanings, are useful for dyeing and printing material containing cellulose fibers.
    Type: Grant
    Filed: December 2, 1988
    Date of Patent: July 17, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Manfred Ruske, Manfred Patsch
  • 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: 4906749
    Abstract: Novel chromophor derivatives of cyclic anhydrides are provided which have the ability to react with a variety of organic substrates forming adducts which are useful in analytical techniques for the detection and measurement of biological compounds.
    Type: Grant
    Filed: January 24, 1989
    Date of Patent: March 6, 1990
    Assignee: Viomedics Inc.
    Inventor: Spyros Theodoropulos
  • Patent number: 4904655
    Abstract: Novel compounds selected from the group consisting of all possible racemic or optically active forms of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 5 carbon atoms, -OH, -CF.sub.3 and -NO.sub.2 and ##STR2## is selected from the group consisting of ##STR3## and their non-toxic, pharmaceutically acceptable acid addition salts having a very good analgesic activity as well as antidepressive, neuronal protective, anti-anoxic, anti-ischemic and no-otropic activities.
    Type: Grant
    Filed: January 26, 1989
    Date of Patent: February 27, 1990
    Assignee: Roussel Uclaf
    Inventors: Nurgun Aktogu, Francoise Delevallee, Francois Clemence, Claude Oberlander
  • Patent number: 4879372
    Abstract: A triazine compound having a dye moiety, a sym-monohalotriazine moiety and an aminobenzoylamine moiety, which is represented, for example, by the following formula, ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen or alkyl, A is phenylene or naphthylene, D is a dye moiety, X is chloro or fluoro, Z is --SO.sub.2 CH.dbd.CH.sub.2, --SO.sub.2 CH.sub.2 CH.sub.2 OSO.sub.3 H or the like, and n is 0, 1 or 2, and which is useful for dyeing or printing fiber materials such as cellulose fiber materials with superior dye performance such as build-up property to give dyed or printed products excellent is fastness properties.
    Type: Grant
    Filed: November 6, 1987
    Date of Patent: November 7, 1989
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Toshihiko Morimitsu, Naoki Harada, Takashi Omura
  • Patent number: 4873318
    Abstract: Novel adducts of oxazine urea chromophors or thiazine urea chromophors with organic substrates are provided which are useful in analytical techniques for the detection and measurement of biological and clinical compounds of interest.
    Type: Grant
    Filed: October 20, 1987
    Date of Patent: October 10, 1989
    Inventor: Spyros Theodoropulos
  • Patent number: 4864024
    Abstract: A new leuco dye is capable of developing into a colored dye which has an absorption band in the near infrared region. The new leuco dye has the following formula (I): ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 independently is hydrogen, an alkyl group, an aralkyl group, a cycloalkyl group or an aryl group; each of X.sup.1 and X.sup.2 independently is oxygen, sulfur or --NR.sup.4 -- (R.sup.4 has the same meaning as for R.sup.1, R.sup.2 and R.sup.3); each of the rings A to E independently is benzene ring or naphthalene ring and may have one or more substituent groups; and each of R.sup.1 to R.sup.4 may have one or more substituent groups. A recording material containing the leuco dye is also disclosed.
    Type: Grant
    Filed: February 10, 1988
    Date of Patent: September 5, 1989
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Kozo Sato, Toru Harada
  • 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: 4853469
    Abstract: Novel quinolinecarboxylic derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 is hydrogen atom or a lower alkyl, R.sup.2 is hydrogen atom, hydroxyl or a lower alkyl and R.sup.3 is hydrogen atom, hydroxyl or an amino, and a pharmaceutical salt thereof have excellent antibacterial activities and are useful as an antibacterial agent.
    Type: Grant
    Filed: July 28, 1988
    Date of Patent: August 1, 1989
    Assignee: Kanebo, Ltd.
    Inventors: Masahiro Taguchi, Hirosato Kondo, Yoshimasa Inoue, Yoshihiro Kawahata, Goro Tsukamoto
  • Patent number: 4847375
    Abstract: As antibacterials and animal growth promoters, the compounds of the formula ##STR1## in which Y is --COOH, --COOR.sup.7 or --CONR.sup.8, R.sup.9,X.sup.1 is H, nitro, alkyl or halogen,R.sup.10 and R.sup.11 preferably complete a piperazine ring,Z is oxygen or NR.sup.15,n is 0 or 1, andthe others can have various meanings,and pharmaceutically acceptable hydrate, alkali metal, alkaline earth metal, silver or guanidinium salt or ester thereof.
    Type: Grant
    Filed: June 13, 1986
    Date of Patent: July 11, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Michael Schriewer, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4835280
    Abstract: The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
    Type: Grant
    Filed: July 14, 1987
    Date of Patent: May 30, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Alfred Martens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckman, Klaus Strein, Egon Roesch
  • Patent number: 4826835
    Abstract: This invention relates to compounds of the formula ##STR1## where Het is imidazol-1-y or 1,2,4-triozol-1-yl and py is 2-,3- or 4-pyridyl; and the uses of said compounds including methods for increasing cardio contractility and in the treatment of congestive heart failure, pharmaceutical compositions including the same and methods for the preparation thereof.
    Type: Grant
    Filed: February 5, 1987
    Date of Patent: May 2, 1989
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, William C. Faith
  • 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: 4820837
    Abstract: The compounds represented by the general formula ##STR1## wherein R is an alkyl group having 1-10 carbon atoms are novel compounds which have not been reported in the literature. Since they have excellent affinities for tissues with particular high corneal permeability and show anticataract activity at low concentration, the compounds are of value as prophylactic and therapeutic agents for cataracts.
    Type: Grant
    Filed: June 30, 1987
    Date of Patent: April 11, 1989
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Hideo Terayama, Jun Inoue
  • Patent number: 4812558
    Abstract: A triazine compound having at least one symtriazine moiety of the following formula, ##STR1## wherein R is hydrogen or unsubstituted or substituted alkyl, Y is vinyl or --CH.sub.2 CH.sub.2 L in which L is a group splittable by the action of an alkali, and Z is phenylene or naphthylene unsubstituted or substituted once by sulfo, which is useful for dyeing or printing fiber materials to give dyed or printed products of excellent fastness properties with superior dye performance, even when dyebath conditions including temperatures, pH, amounts of an inorganic salt and bath ratio are varied to some extent.
    Type: Grant
    Filed: November 10, 1987
    Date of Patent: March 14, 1989
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takashi Omura, Kazufumi Yokogawa
  • Patent number: 4808584
    Abstract: Novel quinolinecarboxylic derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 is hydrogen atom or a lower alkyl, R.sup.2 is hydrogen atom, hydroxyl or a lower alkyl and R.sup.3 is hydrogen atom, hydroxyl or an amino, and a pharmaceutical salt thereof have excellent antibacterial activities and are useful as an antibacterial agent.
    Type: Grant
    Filed: April 7, 1988
    Date of Patent: February 28, 1989
    Assignee: Kanebo, Ltd.
    Inventors: Masahiro Taguchi, Hirosato Kondo, Yoshimasa Inoue, Yoshihiro Kawahata, Goro Tsukamoto
  • 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: 4789742
    Abstract: Novel Isomaleimido and isophthalimido derivatives of chromophoric compounds are provided which are useful in analytic techniques for the detection and measurement of biological compounds such as bacteria, enzymes, hormones and the like.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: December 6, 1988
    Inventor: Spyros Theodoropulos
  • Patent number: 4780535
    Abstract: Conjugates of isomaleimides and isophthalimides and organic chromophoric compounds exhibiting fluorescence, luminescence, chemiluminescence or absorption of analytical value having the structural formula I and II ##STR1## wherein R is an organic aromatic molecule which may be substituted, heteroaromatic which may be substituted, aliphatic having 1 to 50 carbon atoms and which may be substituted or an organic chromophoric molecule exhibiting fluorescence, luminescence, chemiluminiescence or absorption of analytical value. R' is an organic chromophoric molecule exhibiting fluorescence, luminescence, chemiluminescence, or absorption of analytical value; R.sub.1 is hydrogen, halogen, carboxylic, alkyl, aryl, hydroxyl, amino group which may be substituted, nitro or sulfonic group. R.sub.2, R.sub.3 and R.sub.4 have the same meaning as R.sub.
    Type: Grant
    Filed: November 21, 1986
    Date of Patent: October 25, 1988
    Inventor: Spyros Theodoropulos
  • Patent number: 4774242
    Abstract: Novel tetrahydrobenz[c,d]indoles of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and cycloalkyl of 3 to 6 carbon atoms and R.sub.1 is selected from the group consisting of hydrogen, chlorine and bromine and their non-toxic, pharmaceutically acceptable acid addition salts having antianoxic, hypotensive, antihypertensive and dopaminergic agonist activity.
    Type: Grant
    Filed: February 18, 1987
    Date of Patent: September 27, 1988
    Assignee: Roussel Uclaf
    Inventors: Lucien Nedelec, Claude Rettien, Claude Gueniau
  • Patent number: 4766212
    Abstract: Derivatives of 2H-[1]benzoxepino[5,4-b]-1,4-oxazine, such as trans-3,4,4a,5,6,11b-hexahydro-10-methoxy-2H-[1]benzoxepino[5,4-b]-1,4-oxa zine, are prepared by acylating a trans-4-amino-2,3,4,5-tetrahydro-1-benzoxepin-5-ol, cyclizing the resulting chloroacetamido alcohol, reducing the 1,4-oxazine-3(4H)-one so obtained, acylating the resulting 2H-[1]-benzoxepino[5,4-b]-1,4-oxazine, and reducing the N-acryl-2H-[1]benzoxepino[5,4-b]-1,4-oxazine so obtained. The novel compounds disclosed herein possess useful antihypertensive properties.
    Type: Grant
    Filed: October 29, 1987
    Date of Patent: August 23, 1988
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Jules Freedman, Richard C. Dage
  • 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: 4725595
    Abstract: Antibacterially active new 1,8-bridged 4-quinolone-3-carboxylic acid derivatives of the formula ##STR1## in which Y is carboxyl or a derivative thereofR.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.5 are H or various radicals,Z is O, NH, substituted NH, --CON< or --SO.sub.2 N<,m and n are 0 or 1, andA, B, D and E are CH or substituted C or up to three of them are N,and physiologically acceptable salts thereof. Novel intermediates are described as well as processes for making the intermediates and end products.
    Type: Grant
    Filed: January 8, 1987
    Date of Patent: February 16, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4710570
    Abstract: Azine redox dyes and their corresponding dyes of the formula: ##STR1## in which: X is O, S, NR.sup.2,Z completes a fused aromatic of heterocyclic ring system,n is 0 or 1 to allow one R.sup.1 ring substituent,Q represents CR.sup.4 R.sup.5 in which at least one of R.sup.4 and R.sup.5 is an electronegative group or R.sup.4 and R.sup.5 may complete a ring, orwhen X is S Q may represent NR.sup.3 in which R.sup.3 is an aromatic or heterocyclic group.The leuco dyes are useful as dye generators in pressure sensitive, thermographic or photothermographic imaging systems.
    Type: Grant
    Filed: September 30, 1985
    Date of Patent: December 1, 1987
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Tran V. Thien
  • Patent number: 4693745
    Abstract: Novel cyclohexanedionecarboxylic acid derivatives have herbicidal and plant growth regulating properties. The cyclohexanedionecarboxylic acid derivatives have the formula I ##STR1## wherein A is an --OR.sub.2 or --NR.sub.3 R.sub.4 radical,R is C.sub.3 -C.sub.6 cycloalkyl,R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.2 -C.sub.10 alkylthioalkyl; C.sub.3 -C.sub.6 alkenyl which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.6 alkynyl; phenyl or C.sub.1 -C.sub.6 aralkyl, wherein the phenyl nucleus is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, nitro or cyano; one of R.sub.3 and R.sub.4 is methoxy; orR.sub.3 and R.sub.
    Type: Grant
    Filed: October 9, 1985
    Date of Patent: September 15, 1987
    Assignee: Ciba-Geigy Corporation
    Inventor: Hans-Georg Brunner
  • Patent number: 4689325
    Abstract: This invention relates to novel isoxazolo-pyrido-phenoxazine and isothiazolo-pyridophenoxazine derivatives having antibacterial properties and compositions containing methods of treating mammalian patients with these new derivatives.
    Type: Grant
    Filed: October 15, 1986
    Date of Patent: August 25, 1987
    Assignee: Abbott Laboratories
    Inventor: Daniel T. Chu
  • Patent number: 4687770
    Abstract: This invention relates to novel isoxazolo-pyrido-benzoxazine and isothiazolo-pyrido-benzoxazine derivatives having antibacterial properties.
    Type: Grant
    Filed: October 15, 1986
    Date of Patent: August 18, 1987
    Assignee: Abbott Laboratories
    Inventor: Daniel T. Chu
  • Patent number: 4677199
    Abstract: Compounds of the general formula I ##STR1## wherein R.sup.1 is hydrogen, fluorine, chlorine or bromine, R.sup.2 is hydrogen, fluorine, chlorine, bromine, or nitro, B is aliphatic or a sulfo-substituted phenylene radical, and X is a dye radical, are useful for dyeing hydroxyl-containing textile material, in particular cotton.
    Type: Grant
    Filed: September 19, 1985
    Date of Patent: June 30, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Dietmar Augart, Heinz Eilingsfeld, Heinz Krueger, Hartmut Lardon, Ortwin Schaffer, Guenther Seybold
  • Patent number: 4668774
    Abstract: Novel dye salts of anionic dyes of the general formula I ##STR1## where F is a radical of an anionic dye, n is 1, 2, 3 or 4, and B.sup.1 and B.sup.2 independently of one another are each unsubstituted or substituted branched alkyl or alkyl-substituted cycloalkyl having a total of 10 to 36 carbon atoms, are very useful for dyeing solvents, printing inks or polymeric film-forming materials.
    Type: Grant
    Filed: April 23, 1985
    Date of Patent: May 26, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Hermann Loeffler, Rainer Dyllick-Brenzinger
  • 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: 4622400
    Abstract: Methods are provided for making certain m-aminophenols using a sulfonation/alkali fusion procedure. The aminophenols are key intermediates in the synthesis of dyes, particularly efficient, stable dyes for laser application. Preparations of some rhodamine and phenoxazone dyes from the m-aminophenols are described.
    Type: Grant
    Filed: December 29, 1983
    Date of Patent: November 11, 1986
    Assignee: The United States of America as represented by the United States Department of Energy
    Inventor: Peter R. Hammond
  • Patent number: 4611056
    Abstract: Pharmaceutical compositions containing a compound of Formula I: ##STR1## wherein X is O, S, SO or SO.sub.2 and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be positioned anywhere on the structure, or a pharmaceutically-acceptable salt thereof and certain novel benzo[a]phenothiazines, which compositions and compounds are useful in treating allergic conditions, asthma, cardiovascular disorders, inflammation and pain and are useful as cytoprotective agents.
    Type: Grant
    Filed: March 28, 1985
    Date of Patent: September 9, 1986
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yvan Guindon, Yves Girard, Cheuk K. Lau, Rejean Fortin, Joshua Rokach, Christiane Yoakim
  • Patent number: 4607032
    Abstract: Quino-benoxazine compounds having the formula: ##STR1## wherein R.sub.2 is one or more substituents, R.sub.1 is a hydrogen or a carboxy-protecting group and Z is an amine group or an aliphatic heterocyclic group. The compounds have antibacterial activity.
    Type: Grant
    Filed: April 26, 1984
    Date of Patent: August 19, 1986
    Assignee: Abbott Laboratories
    Inventor: Daniel T. Chu
  • Patent number: 4604461
    Abstract: 5-[N-(RCO)-N-R.sup.1 -amino] or (RCOO)-9-(N-R.sup.2 -N-R.sup.3 -amino)-12-(RCO)benzo[a]phenoxazines useful as color formers, particularly in electrochromic recording systems, are prepared by the interaction of the corresponding 5-(N-R.sup.1 -amino)-9-(N-R.sup.2 -N-R.sup.3 -amino)benzo[a]phenoxazinium halide or 9-(N-R.sup.2 -N-R.sup.3 -amino)benzo[a]phenoxazin-5-one with a reducing agent to obtain the corresponding leuco compound and subsequently interacting the leuco compound with at least two molecular proportions of an acylating agent.
    Type: Grant
    Filed: September 3, 1985
    Date of Patent: August 5, 1986
    Assignee: The Hilton-Davis Chemical Co.
    Inventor: William M. Hung
  • Patent number: 4604462
    Abstract: 4-(N-Acylamino)-8-(N-R.sup.1 -N-R.sup.2 -amino)imidazophenoxazines useful as color formers, particularly in electrochromic recording systems, are prepared by the interaction of the corresponding 1,3-diamino-7-(N-R.sup.1 -N-R.sup.2 -amino)phenooxazinium halide with a reducing agent to obtain the corresponding leuco compound and subsequently interacting the leuco compound with at least two molecular proportions of an acylating agent.
    Type: Grant
    Filed: September 3, 1985
    Date of Patent: August 5, 1986
    Assignee: The Hilton-Davis Chemical Co.
    Inventor: William M. Hung
  • Patent number: 4600775
    Abstract: Novel isomaleimido and isophthalimido derivatives of chromophoric compounds are provided which are useful in analytical techniques for the detection and measurement of biological compounds such as bacteria, enzymes, hormones and the like.
    Type: Grant
    Filed: August 27, 1984
    Date of Patent: July 15, 1986
    Inventor: Spyros Theodoropulos
  • Patent number: 4569997
    Abstract: By reacting compounds of the formula ##STR1## with diisocyanates or triisocyanates of the formula R.sup.4 (NCO).sub.n at a low temperature, the corresponding 1-carbamyl compounds of the formula I ##STR2## in which n is 2 or 3 and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in claim 1, are obtained. The compounds of the formula 1 are light stabilizers for organic materials, especially for varnishes.
    Type: Grant
    Filed: September 29, 1983
    Date of Patent: February 11, 1986
    Assignee: Ciba Geigy Corporation
    Inventor: Friedrich Karrer
  • 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: 4542133
    Abstract: 1,2-methylenedioxy quino-benoxazine derivatives having the formula: ##STR1## wherein R.sub.2 is a substituent and R.sub.1 is hydrogen or a carboxy protecting group. The compounds of the invention have antibacterial activity.
    Type: Grant
    Filed: April 26, 1984
    Date of Patent: September 17, 1985
    Assignee: Abbott Laboratories
    Inventor: Daniel T. Chu