Chalcogen Or Nitrogen Attached Indirectly To The Tricyclo Ring System By Acyclic Nonionic Bonding Patents (Class 548/444)
  • Patent number: 5206380
    Abstract: A chromogenic compound for use in pressure- or heatsensitive record material has the general formula (I):R.sub.1 --CH.dbd.CH--CR.sub.3 (OR.sub.4)--CH.dbd.CH--R.sub.2 (I)in which:R.sub.1 and R.sub.2 are the same or different and each is a group of one of the formulae (II): ##STR1## in which the benzene ring of the group of formula (IIa) is optionally further substituted, and in which:R.sub.10 and R.sub.11 are each independently hydrogen or an optionally-substituted alkyl, aryl or aralkyl group, orR.sub.10 and R.sub.11 together with the nitrogen atom to which they are attached form an optionally-substituted heterocyclic ring, which may include one or more further hetero atoms;R.sub.12, R.sub.13 and R.sub.14 are each independently hydrogen or an optionally-substituted alkyl, aryl or aralkyl group;R.sub.3 is an optionally-substituted aryl group; andR.sub.4 is hydrogen or an optionally-substituted alkyl, aryl or aralkyl group.
    Type: Grant
    Filed: June 8, 1992
    Date of Patent: April 27, 1993
    Assignee: The Wiggins Teape Group Limited
    Inventor: Kenneth J. Shanton
  • Patent number: 5189188
    Abstract: Compounds of the general formula ##STR1## in which the symbols have the meaning given in the description, are highly suitable as color formers in recording materials based on acid developers. They give deep blue, green-blue, green, violet or red shades which have excellent sublimation and light fastness.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: February 23, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventor: Udo Eckstein
  • Patent number: 5166438
    Abstract: A charge transporting material comprising a 1,3-pentadiene derivative having formula (I):A--CH.dbd.CH--CH.dbd.CH--CH.sub.2 --A (I)wherein A represents a 9-anthryl group which may have a substituent, a N-substituted carbazolyl group which may have a substituent, a N-substituted phenothiazinyl group which may have a substituent or ##STR1## in which Ar represents an arylene group which may have a substituent, R.sup.1 and R.sup.2 each represent an alkyl group which may have a substituent, an aralkyl group which may have a substituent, or an aryl group which may have a substituent; an electrophotographic photoconductor comprising an electroconductive support and a photoconductive layer formed thereon, which comprises as an effective component at least one of the 1,3-pentadiene derivatives of the above formula (I); and novel 1,3-pentadiene derivatives of the formula (I), provided that in the formula (I), R.sup.1 and R.sup.2 cannot be a methyl group at the same time, are disclosed.
    Type: Grant
    Filed: August 23, 1991
    Date of Patent: November 24, 1992
    Assignees: Ricoh Company, Ltd., Hodogaya Chemical Co., Ltd.
    Inventors: Mitsuru Hashimoto, Masaomi Sasaki, Tomoyuki Shimada, Nobuo Suzuki, Takayuki Sakai, Susumu Suzuka
  • Patent number: 5132430
    Abstract: Ethylenically unsaturated polymerizable acrylic (or methacrylic) monomers having pendant halogenated carbazole moieties, useful for the production of high refractive index polymers, are disclosed. The monomers are useful for the bonding of optical elements in the fabrication of optical devices.
    Type: Grant
    Filed: June 26, 1991
    Date of Patent: July 21, 1992
    Assignee: Polaroid Corporation
    Inventors: Russell A. Gaudiana, Richard A. Minns, Howard G. Rogers
  • Patent number: 5116995
    Abstract: Carbazole compounds represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, R.sup.2 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkanoyl group having 2 to 6 carbon atoms or a benzoyl group, R.sup.3 and R.sup.4 are the same or different, and are each hydrogen atom, an alkyl group having 1 to 7 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkyl group having 1 to 3 carbon atoms substituted by a phenyl group, or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a morpholino group, a piperidino group, a pyrrolidino group or a piperazino group, and n is an integer from 1 to 3, and salts thereof have strong antipsychotic activity.
    Type: Grant
    Filed: May 20, 1991
    Date of Patent: May 26, 1992
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Atsuro Nakazato, Sanae Kitsukawa, Yutaka Kawashima, Katsuo Hatayama, Satoshi Hibino
  • Patent number: 5097064
    Abstract: This invention relates to a process for preparing an optically active 2-arylpropionic acid of general formula (I), by the hydrogenation, in a heterogeneous aqueous-organic medium, of a 2-arylacrylic acid of general formula (II) in the presence of a catalyst consisting of a rhodium derivative and a water-soluble chiral ligand.
    Type: Grant
    Filed: August 30, 1990
    Date of Patent: March 17, 1992
    Assignee: Rhone-Poulenc Sante
    Inventor: Jean-Michel Grosselin
  • Patent number: 5097034
    Abstract: Color formers of the formula ##STR1## in which X.sup.1 denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy or acyloxy,R.sup.1 denotes hydrogen, halogen, alkyl or alkoxy,R.sup.2 denotes hydrogen, alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sup.1 and Y.sup.2, independently of one another, denote alkyl, cycloalkyl or aralkyl,R.sup.2 can form a heterocyclic ring with A in the o-position, in which a benzene ring can be additionally fused onto ring A in the o-/m-position with respect to R.sup.2,R.sup.3 denotes hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl or aryl, or R.sup.3 is linked to ring B in the o-position with respect to the nitrogen,Z.sup.1 stands for the remaining members of a partially hydrogenated or completely hydrogenated ring, with the proviso that Z.sup.
    Type: Grant
    Filed: May 14, 1991
    Date of Patent: March 17, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventor: Udo Eckstein
  • Patent number: 5094688
    Abstract: Color-forming agents of the present formula ##STR1## wherein X denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkylamino, dialkylamino, acylamino, aralkylamino or arylamino,R denotes alkyl, alkenyl or aralkyl,R.sub.1 denotes hydrogen, halogen or alkyl,R.sub.2 denotes alkoxy, aralkoxy, aryloxy or a radical of the formula ##STR2## Y.sub.1 and Y.sub.2 independently of one another denote alkyl, aryl, cycloalkyl or aralkyl or R.sub.2, with A in the o-position, forms a heterocyclic ring,a benzene ring can be fused onto the ring A, in the o-/m-position relative to R.sub.2, and the ring A and its fused-on rings and the cyclic and acyclic radicals can carry further non-ionic substitutents customary in dyestuffs chemistry,are used in thermoreactive papers and pressure-sensitive recording materials and for the preparation of highly concentrated solutions in organic solvents.
    Type: Grant
    Filed: August 12, 1988
    Date of Patent: March 10, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Eckstein, Hubertus Psaar, Gert Jabs
  • Patent number: 5082938
    Abstract: Enhanced branched chain hydroxyl compounds are provided of formulaY--(Z).sub.1-6wherein Y is the residue of a nucleophile devoid of conjugated divalent linking moieties, and each Z is a poly(oxyalkylene) moiety having a molecular weight of from about 200-10,000 and containing at least one glycidol residue, wherein at least one of the primary oxy sites of said glycidol residue is linked preferably directly to a first epoxide residue of three or more carbons, and wherein said first epoxide residue is linked through a secondary oxy site preferably directly to a second epoxide reside having a primary terminal hydroxyl.
    Type: Grant
    Filed: March 1, 1990
    Date of Patent: January 21, 1992
    Assignee: Milliken Research Corporation
    Inventors: Edward W. Kluger, David J. Moody
  • Patent number: 5071868
    Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbozole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.
    Type: Grant
    Filed: January 28, 1991
    Date of Patent: December 10, 1991
    Assignee: Boehringer Mannheim GmbH
    Inventor: Herbert Leinert
  • Patent number: 5070207
    Abstract: There is disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma, psoriasis, inflammatory bowel disease and inflammation in mammals which comprises administering to a mammal so afflicted an effective amount of a compound having the formula: ##STR1## wherein Z is a group having the formula ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl; R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl of 1-20 carbon atoms, halo, halo lower alkyl, halo lower alkoxy, lower alkoxy, halo lower alkylsulfonyl, nitro or trifluoromethyl, where at least one of R.sup.3 and R.sup.4 is other than hydrogen;R.sup.5 is hydrogen, lower alkyl or halo;A is --CH.sub.2 --, --O-- or --S--;m is 0-10;n is 1-8;X is hydrogen, fluoro, lower alkyl or aralkyl of 7-12 carbon atoms;or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: April 26, 1990
    Date of Patent: December 3, 1991
    Assignee: American Home Products Corporation
    Inventors: Guy A. Schiehser, Gregory F. Von Burg
  • Patent number: 5068350
    Abstract: Polyolefin derivatives, which are useful not only as the photoconductive materials for electrophotography, but also as a charge transporting material employed in a function-separating type photoconductor which uses an organic or inorganic pigment as a charge generating material, and an electrophotographic photoconductor containing at least one of the above polyolefin derivatives in a photoconductive layer thereof, are disclosed.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: November 26, 1991
    Assignees: Ricoh Company, Ltd., Hodogaya Chemical Co., Ltd.
    Inventors: Mitsuru Hashimoto, Tomoyuki Shimada, Nobuo Suzuki, Takayuki Sakai, Susumu Suzuka, Masaomi Sasaki
  • Patent number: 5047539
    Abstract: Heterocyclic amidine derivatives of the general formula I ##STR1## in which the variables R.sup.1 are the same or different and denote hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, hydroxyl or chlorine,R.sup.2 to R.sup.5 denote hydrogen or C.sub.1 -C.sub.4 -alkyl and R.sup.3 and R.sup.4 can together form a five-membered or six-membered ring,R.sup.6 denotes hydrogen or C.sub.1 -C.sub.8 -alkyl,R.sup.7 denotes cyano or --COOR.sup.8, --COR.sup.8, --CONHR.sup.8 or --CONR.sup.8.sub.2, in whichR.sup.8 is a straight-chain or branched-chain C.sub.1 -C.sub.12 -alkyl group which may be interrupted by oxygen atoms, a cyclopentyl or cyclohexyl group or a phenylalkyl group having from 1 to 3 carbon atoms in the alkyl moiety,A is a chemical bond or a methylene group which may additionally carry one or two C.sub.1 -C.sub.4 -alkyl radicals, andm and n are each 1 or 2.The said heterocyclic amidine derivatives I serve as UV stabilizers for organic materials.
    Type: Grant
    Filed: April 19, 1990
    Date of Patent: September 10, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Spang, Peter Neumann, Hubert Trauth
  • Patent number: 5011967
    Abstract: Bischloroformate oligomer compositions are prepared by passing phosgene into a heterogeneous aqueous-organic mixture containing at least one dihydroxyaromatic compound, with simultaneous introduction of a base at a rate to maintain a specific pH range and to produce a specific volume ratio of aqueous to organic phase. By this method, it is possible to employ a minimum amount of phosgene. The reaction may be conducted batchwise or continuously. The bischloroformate composition may be employed for the preparation of cyclic polycarbonate oligomers or linear polycarbonate, and linear polycarbonate formation may be integrated with bischloroformate composition formation in a batch or continuous process.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: April 30, 1991
    Assignee: General Electric Company
    Inventors: James M. Silva, Robert A. Pyles
  • Patent number: 4990625
    Abstract: A process for synthesizing an N,N-disubstituted hydrazone comprises carrying out nitrozation by adding an aqueous solution of sodium nitrite to a solution having one part by weight of an N,N-disubstituted amine dissolved in 3 to 30 parts by weight of an organic acid, then reducing the nitrozated product to an N,N-disubstituted hydrazine by adding a reducing agent to the mixture containing the nitrozated product, and thereafter adding to the mixture containing the N,N-disubstituted hydrazine a carbonyl compound of the formula: ##STR1## wherein A represents an aromatic hydrocarbon group or an aromatic heterocyclic group which may have a substituent, B represents a hydrogen atom, an alkyl group, an aryl group or an aromatic heterocyclic group, which may have a substituent, thereby performing condensation of the N,N-disubstituted hydrazine with the carbonyl compound.
    Type: Grant
    Filed: December 5, 1989
    Date of Patent: February 5, 1991
    Assignee: Canon Kabushiki Kaisha
    Inventors: Tetsuo Arita, Minoru Mabuchi, Shoji Umehara, Kiyoshi Sakai
  • Patent number: 4990668
    Abstract: Described is a process for preparing a racemic or chiral aryloxypropanolamine (1) or arylethanolamine (2) of the formula ##STR1## wherein Ar is aryl, substituted aryl, heteroaryl, or aralkyl and R is alkyl, substituted alkyl, aralkyl, or WB wherein W is a straight or branched chain alkylene of from 1 to about 6 carbon atoms and wherein B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, where R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.3 COOR.sub.5, or R.sub.3 and R.sub.4 may together with N form a 5- to 7-membered heterocyclic group.The process can be used to prepare beta-blocking agents, useful in the treatment of cardiac conditions.
    Type: Grant
    Filed: December 4, 1985
    Date of Patent: February 5, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Khuong H. X. Mai, Ghanshyam Patil, William L. Matier
  • Patent number: 4985454
    Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.
    Type: Grant
    Filed: January 19, 1989
    Date of Patent: January 15, 1991
    Assignee: Boehringer Mannheim GmbH
    Inventor: Herbert Leinert
  • Patent number: 4970227
    Abstract: A compound of the formula (I):ArCH.sub.2 R.sup.1where Ar is ##STR1## where Z is NH, NCH.sub.3 or NEt and R.sup.1 is an hydroxyalkylamino group and pharmaceutically acceptable salts thereof. The compounds are useful as antitumor agents.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: November 13, 1990
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4929751
    Abstract: A vinyl tricarbonyl compound of the formula ##STR1## or its monohydrate of the formula ##STR2## wherein R.sub.1 is a hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, and cycloalkyl with 3 to 7 carbon atoms,R.sub.2 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic,R.sub.3 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic, andR.sub.4 is unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl are 3 to 7 carbon atoms. Such vinyl tricarbonyl compound is effective against tumor cells.
    Type: Grant
    Filed: October 19, 1987
    Date of Patent: May 29, 1990
    Assignee: Yale University
    Inventors: Harry H. Wasserman, Natesan Murugesan, John H. Van Duzer
  • Patent number: 4923641
    Abstract: Highly concentrated stable solutions of color-forming agents of the general formula ##STR1## wherein x denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkylamino, dialkylamino, acylamino, aralkylamino or arylamino andR denotes alkyl, alkenyl or aralkyl,further isocyclic or heterocyclic rings can be fused onto the rings A, B, C and D and the cyclic and acyclic radicals and the rings A, B, C and D can carry further non-ionic substituents which are customary in dyestuff chemistry, or mixtures thereof, in water-insoluble organic solvents from the group comprising optionally chlorinated hydrocarbons, vegetable oils and phthalic acid esters are used for the preparation of pressure-sensitive recording materials.
    Type: Grant
    Filed: September 20, 1988
    Date of Patent: May 8, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Eckstein, Hubertus Psaar
  • Patent number: 4892899
    Abstract: Composition of matter containing(a) a compound of the formula I ##STR1## in which A is one of the groups of the formulae ##STR2## in which B is --O--, --S--, --SO.sub.2 --, --N.dbd.N--, --CH.sub.2 --, --CH.dbd.CH--, ##STR3## --CONH--, --NHCONH--, or --CONHNHCO--, Q is --O-- or --NH-- and Z is --O-- or --S-- and R and R' are independently of each other hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or phenoxy, and(b) a compound of the formula II ##STR4## in which A' is as defined above for A, D is hydrogen, amino or a group of the formula III ##STR5## E is --O-- or --S--, T.sub.1, T.sub.2 and T.sub.3 independently of one another are chlorine or a group --ET', T' is a group of the formulae ##STR6## X.sup..sym. is H.sup..sym. or a group of the formulae M.sup.n.sym. /n or N.sup..beta. (R.sub.1)(R.sub.2)(R.sub.3)(R.sub.4), Mhu n.sym. is an n-valent metal cation, n is 1, 2 or 3, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently of one another hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.
    Type: Grant
    Filed: December 8, 1987
    Date of Patent: January 9, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Edward E. Jaffe, Jost von der Crone, Bernhard Medinger
  • Patent number: 4885404
    Abstract: Disclosed is a process for the production of acids of the formula ##STR1## wherein R is 2-fluoro-4-(1,1'-biphenyl), 4-(2-methylpropyl)phenyl, 6-methoxy-2-napthyl, 3-benzophenyl, 4-(2-thienylcarbonyl)-phenyl or 7-chlorocarbazole-3-yl which comprises contacting an organometallic compound of the formula R--M--R.sub.
    Type: Grant
    Filed: March 6, 1987
    Date of Patent: December 5, 1989
    Assignee: The Upjohn Company
    Inventor: Peter G. M. Wuts
  • Patent number: 4877824
    Abstract: Compounds of the formula (I) ##STR1## in which the Rs independently of one another are H, phenyl, naphthyl or C.sub.7 -C.sub.30 alkaryl and R.sup.1 is H, C.sub.1 -C.sub.8 alkyl, C.sub.7 -C.sub.9 aralkyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl, naphthyl, C.sub.7 -C.sub.30 alkaryl or a group of the formula (II)--(CH.sub.2).sub.a --SR.sup.3 (II)R.sup.2 is C.sub.7 -C.sub.30 alkaryl, phenyl, naphthyl or phenyl containing, in the para-position, an HO or C.sub.1 -C.sub.18 alkoxy group or a group of the formulae ##STR2## or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, are a radical of the formula (III) ##STR3## R.sup.3 is a radical of the formulae --(CH.sub.2).sub.b --COOR.sup.6 or --(CH.sub.2).sub.2 OCOR.sup.7, a is the number 1, 2 or 3 and b is the number 1 or 2, and R.sup.4 is phenyl or a group of the formula (II), the two R.sup.5 s independently of one another are H, C.sub.1 -C.sub.24 alkyl, C.sub.5 -C.sub.12 cycloalkyl or C.sub.7 -C.sub.9 aralkyl, and R.sup.6 is H, C.sub.1 -C.
    Type: Grant
    Filed: January 25, 1989
    Date of Patent: October 31, 1989
    Assignee: Ciba-Geigy Corporation
    Inventor: Samuel Evans
  • Patent number: 4868306
    Abstract: There are provided compounds of formula I, ##STR1## and pharmaceutically acceptable derivatives thereof. There are also described the use of the compounds of formula I as pharmaceuticals, methods for making the compounds and pharmaceutical, e.g. cardiac, compositions containing the compounds.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: September 19, 1989
    Assignee: Fisons plc
    Inventors: Francis Ince, Alan C. Tinker
  • Patent number: 4866073
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a C.sub.8-13 fused heterotricyclic ring system containing at least two aromatic rings and no more than 3 heteroatoms (in separate rings), or a C.sub.10-17 fused heterotetracyclic ring system containing at least two aromatic rings and no more than 4 heteroatoms (in separate rings) or a C.sub.
    Type: Grant
    Filed: October 22, 1987
    Date of Patent: September 12, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4866070
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.
    Type: Grant
    Filed: December 11, 1987
    Date of Patent: September 12, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4863949
    Abstract: The present invention provides compounds of the general formula: ##STR1## wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic radical, A is a straight-chained or branched alkylene chain containing up to 8 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms, B is a straight-chained mono- or bicyclic, optionally branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms and/or up to two --CH.sub.2 -- groups of which can be replaced by an oxygen or a sulphur atom or by an --S(.dbd.O) or --S(.dbd.O).sub.2 group, X is a valency bond, an oxygen atom or an --NR.sup.1 group, in which R.sup.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl or nitroxyalkyl radical containing up to 6 carbon atoms or R.sup.1, together with the nitrogen atom of the --NR.sup.
    Type: Grant
    Filed: September 21, 1987
    Date of Patent: September 5, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Herbert Simon, Helmut Michel, Wolfgang Bartsch, Klaus Strein
  • Patent number: 4855446
    Abstract: Racemic carboxylic acids are resolved into their enantiomers using optically active enantiomers of four lactones as resolving agents. The four lactones are 2,3-isopropylidene-ribonic acid-1,4-lactone, 1,2-isopropylidene-glucofuranurono-3,6-lactone, 2-hydroxy-3,3-dimethyl-1,4-butyrolactone and 3,4-isopropylidene-arabino-1,5-lactone. Novel diastereoisomeric esters of the acids with the lactones are disclosed.
    Type: Grant
    Filed: December 17, 1984
    Date of Patent: August 8, 1989
    Assignee: The Sherwin Williams Company
    Inventors: Colin C. Duke, Robert J. Wells
  • Patent number: 4841050
    Abstract: Benzopyrans of the formula ##STR1## where X is a radical ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and the ring A have the meanings stated in the description, a process for their preparation, and their use in pressure-sensitive or heat-sensitive layers.
    Type: Grant
    Filed: March 12, 1987
    Date of Patent: June 20, 1989
    Assignee: BASF Aktiengesellschaft
    Inventors: Andreas Guentner, Udo Mayer, Andreas Oberlinner
  • Patent number: 4824963
    Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S-(-)-carbozole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.
    Type: Grant
    Filed: May 13, 1987
    Date of Patent: April 25, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventor: Herbert Leinert
  • Patent number: 4822811
    Abstract: Compounds of the formula: ##STR1## wherein R1 is hydrogen, C1 to C4 alkyl, C2 to C4 alkenyl, or NR2R3, wherein R2 and R3 are independently selected from hydrogen, C1 to C4 alkyl and hydroxyl, but R2 and R3 are not simultaneously hydroxyl;X is oxygen, sulfur, CO2, or NR4, wherein R4 is hydrogen, C1 to C6 alkyl, C1 to C6 alkoyl or aroyl;A is selected from C1 to C6 alkylene and C2 to C6 alkenylene;Y is selected independently at each occurrence from hydrogen, halogen, hydroxy, cyano, nitro, halosubstituted alkyl, C1 to C12 alkyl, C2 to C12 alkenyl, C1 to C12 alkoxy, C3 to C8 cycloalkyl, aryl, aryloxy, aroyl, C1 to C12 arylalkyl, C2 to C12 arylalkenyl, C1 to C12 arylalkoxy, C1 to C12 arylthicalkoxy, and substituted derivatives of aryl, aryloxy, aroyl, C1 to C12 arylalkyl, C2 to C12 arylalkenyl, C1 to C12 arylalkoxy, or C1 to C12 arylthioalkoxy, wherein C12 alkyl, alkoxy, and halosubstituted alkyl; n is a number having the values 0-4; when n=0 then Y=hydrogen;and M is hydrogen, a pharmaceutically acceptable cation,
    Type: Grant
    Filed: June 17, 1988
    Date of Patent: April 18, 1989
    Assignee: Abbott Laboratories
    Inventor: James B. Summers
  • Patent number: 4814462
    Abstract: A polyoxyalkylene carbazole adduct represented by the following formula I: ##STR1## wherein R stands for at least one member selected from the group consisting of H, CH.sub.3 and C.sub.6 H.sub.5, R' for at least one member selected from the group consisting of CH.sub.3, C.sub.6 H.sub.5 and H, (providing that R' is at least one member selected from the group consisting of CH.sub.3 and C.sub.6 H.sub.5 when R is H, and R is at least one member selected from the group consisting of CH.sub.3 and C.sub.6 H.sub.5 when R' is H), n for an integer of the value of 0 to 500, m for an integer of the value of 0 to 500, and n+m for an integer of the value of 2 to 1000.
    Type: Grant
    Filed: July 7, 1986
    Date of Patent: March 21, 1989
    Assignees: Nihon Joryu Kogyo Co., Ltd, Nippon Shokubai Kagaku Kogyo Co., Ltd.
    Inventors: Naoji Kurata, Yoshio Sugita, Keiji Kobayashi, Atsushi Kawano
  • Patent number: 4774331
    Abstract: A process for ortho-cyanation of phenols or phenylamines which comprises reacting a phenyl compound having hydroxy or optionally substituted amino or cyclic amino, of which ortho position is vacant, with trichloroacetonitrile, C.sub.1 -C.sub.5 alkyl thiocyanate or C.sub.6 -C.sub.12 aryl thiocyanate in the presence of a boron trihalide and treating the resultant product with an alkali is provided, and said process is useful in the synthesis of intermediates for medicinals or pesticides.
    Type: Grant
    Filed: August 21, 1987
    Date of Patent: September 27, 1988
    Assignee: Shionogi & Co., Ltd.
    Inventors: Makoto Adachi, Hiromu Matsumura, Tsutomu Sugasawa
  • Patent number: 4760085
    Abstract: The present invention is concerned with the topical use of D,L- and D-carazolol and of the pharmacologically acceptable salts in the therapy of glaucoma. The present invention is also concerned with eye drops containing these active materials.
    Type: Grant
    Filed: April 6, 1987
    Date of Patent: July 26, 1988
    Assignee: Boehringer Mannheim GmbH
    Inventor: Wolfgang Bartsch
  • Patent number: 4748174
    Abstract: The water soluble acid addition salts of an NSAID, such as acetylsalicylic acid, fenbufen, diflunisal, piroxicam, naproxen, or the like, with either glucamine or meglumine (N-methylglucamine) are useful anti-inflammatory and analgesic drugs, well adopted for parenteral, oral, rectal or topical administration.
    Type: Grant
    Filed: January 5, 1987
    Date of Patent: May 31, 1988
    Assignee: Therapicon s.r.l.
    Inventor: Paolo A. Veronesi
  • Patent number: 4737587
    Abstract: Disclosed is a colorless dye for use in recording materials comprising a compound represented by the general formula: ##STR1## Said recording materials are of the types which utilize a color developing reaction between an electron-donating colorless dye and an electron-accepting color developer, such as, carbonless pressure-sensitive recording materials, thermosensitive recording materials, etc.
    Type: Grant
    Filed: November 20, 1986
    Date of Patent: April 12, 1988
    Assignee: Mitsubishi Paper Mills, Ltd.
    Inventors: Fumio Okumura, Hirokazu Tsukahara, Haruhiko Ikeda
  • Patent number: 4707548
    Abstract: Novel bisisoindoline pigments of the formula (I) ##STR1## where the radicals A are identical or different radicals of a methylene-active compound, X is a divalent radical and the rings L are each unsubstituted or substituted, possess good fastness properties and are therefore suitable for a very wide range of applications, for example for pigmenting plastics, printing inks and surface coatings.
    Type: Grant
    Filed: January 24, 1986
    Date of Patent: November 17, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang Lotsch, Gustav Bock, Peter Neumann
  • Patent number: 4697022
    Abstract: A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt.The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.
    Type: Grant
    Filed: May 21, 1984
    Date of Patent: September 29, 1987
    Assignee: Boehringer Mannheim GmbH
    Inventor: Herbert Leinert
  • Patent number: 4656182
    Abstract: Substituted trans-1,2-diaminocyclohexyl amide compounds demonstrating selective opioid receptor binding possess utility as analgesic, diuretic, and psychotherapeutic agents. A method of preparing the compounds, pharmaceutical compositions employing the compounds, and a method of alleviating pain employing the compounds are also disclosed.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: April 7, 1987
    Assignee: Warner-Lambert Company
    Inventor: David Horwell
  • Patent number: 4656257
    Abstract: A disazo compound is provided which is represented by the formula (I): ##STR1## (wherein, R.sub.1 and R.sub.2 each stands for hydrogen, a lower alkyl group with 1-4 carbon atoms, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aromatic group, or a substituted or unsubstituted hetero ring group. R.sub.1 and R.sub.2 may be the same or different. And, R.sub.1 and R.sub.2 may mutually bond to form a ring).This disazo compound may be obtained by diazotating 2.6-diaminoanthraquinone and reacting the same with a coupler represented by the formula (IV): ##STR2## (wherein, R.sub.1 and R.sub.2 are the same as defined above). Further, a multilayer type electrophotographic element is provided which comprises a charge carrier generating layer and a charge transfer layer and uses, as a charge carrier generating substance, a disazo compound represented by the formula (I).
    Type: Grant
    Filed: June 20, 1985
    Date of Patent: April 7, 1987
    Assignee: Ricoh Co., Ltd.
    Inventor: Mitsuru Hashimoto
  • Patent number: 4652672
    Abstract: For the analytical and preparative separation of the optical isomers of optically active alkanolamines into their optically pure antipodes a new resolution method is presented which involves an ester formation of the alkanolamines with optically pure and symmetrically O,O disubstituted (R,R)- or (S,S)-tartaric acids. The derivitization reactions are carried out in aprotic solvents and the primary and secondary functions are blocked via ion-pair formations with strong acids, e.g. dichloroacetic acid. The tartaric acid anhydrides are predominantly used as reagents but other ester formation methods are also practicable. The mixture of the diastereomeric alkanolamine tartaric acid monoesters are separable into their optically active and pure isomers by various chromotographic separation techniques, e.g. straight or reverse phase LC, but also by extraction methods e.g. Soxhlet extraction.
    Type: Grant
    Filed: October 17, 1983
    Date of Patent: March 24, 1987
    Inventor: Wolfgang F. Lindner
  • Patent number: 4636820
    Abstract: 3-[(Substituted-amino)(aryl or heteroaryl)methyl]-1H-indoles which are useful as color-formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting 3-[(arylsulfonyl)(aryl or heteroaryl)methyl]-1H-indoles with amines or precursors thereof in the presence of a base.
    Type: Grant
    Filed: January 17, 1985
    Date of Patent: January 13, 1987
    Assignee: The Hilton-Davis Chemical
    Inventors: Paul J. Schmidt, William M. Hung
  • Patent number: 4601797
    Abstract: Hydroxyibuprofen is produced in good yield by reduction of p-isobutylacetophenone at the cathode in the presence of carbon dioxide. Hydroxyibuprofen is readily hydrogenolyzed to ibuprofen. Electrochemical carboxylation of other selected aryl methyl ketones is also effected.
    Type: Grant
    Filed: March 1, 1985
    Date of Patent: July 22, 1986
    Assignee: Monsanto Company
    Inventor: John H. Wagenknecht
  • Patent number: 4540523
    Abstract: Cationic styryl dyestuffs of the formula ##STR1## in which A.sup.1 is an alkyleneoxy or alkyleneamino radical,D.sup.1 is a direct bond or divalent radical,An is an anion, andthe terminal phenyl ring is unsubstituted or substituted by CN, alkyl or alkoxy. The compounds are suitable for dyeing, enscribing and printing paper for dyeing and printing synthetic fibres, especially made of polyacrylonitrile, acid-modified polyesters or polyamides.
    Type: Grant
    Filed: October 17, 1980
    Date of Patent: September 10, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hermann Beecken
  • Patent number: 4535166
    Abstract: Rearrangement of alpha-halo-alkylarylketals in neutral or weakly alkaline conditions and in the presence of a polar-protic medium and subsequent hydrolysis of the thus obtained esters, in the same reaction medium, to afford the corresponding alpha-arylalkanoic acids or their salts which are particularly useful as anti-inflammatory, analgesic and antipyretic agents.
    Type: Grant
    Filed: August 3, 1983
    Date of Patent: August 13, 1985
    Assignee: Zambon S.p.A.
    Inventors: Graziano Castaldi, Claudio Giordano
  • Patent number: 4535172
    Abstract: This invention relates to 3-aryl or heteroaryl-3-alkoxy, phenoxy-, alkylthio- or phenylthiophthalides useful as color formers, particularly in carbonless duplicating and thermal marking systems, which are prepared by the interaction of 2-(disubstituted amino)phenylcarbonylbenzoic acids with an acid chloride or an anhydride of an alkanoic acid in the first step and a further reaction of the product of the first step with an alcohol, a thioalcohol, a phenol or a thiophenol in a second step.
    Type: Grant
    Filed: January 8, 1982
    Date of Patent: August 13, 1985
    Assignee: The Hilton-Davis Chemical Co.
    Inventors: Paul J. Schmidt, William M. Hung
  • Patent number: 4518799
    Abstract: Novel processes for making arylpropionic acids are described. One process comprises carboxylating particular Grignard compounds which are the products of a catalyzed reaction between corresponding arylmagnesium bromides and ethylene. Furthermore, the reaction making the particular Grignard compounds is itself novel. Also, an improved method is disclosed for making coupled aryl compounds useful as intermediates for making compounds having a pharmaceutical use. For example, particular biaryls may be used to make some of the Grignard compounds herein from which the arylpropionic acids are made. Finally, an improved bromination is disclosed giving high yields of 4-bromo-2-fluoroaniline, which is thereafter coupled with benzene, then used to make the arylmagnesium bromide reacted with ethylene to obtain the particular Grignard compound and subsequent desired arylpropionic acid, i.e. 2-(2-fluoro-4-biphenylyl)propionic acid.
    Type: Grant
    Filed: June 8, 1982
    Date of Patent: May 21, 1985
    Assignee: The Upjohn Company
    Inventor: Thomas A. Hylton
  • Patent number: 4503067
    Abstract: Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;R.sub.3 is hydrogen or lower alkyl;R.sub.4 is hydrogen or lower alkyl, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;X is a valency bond, --CH.sub.2 --, oxygen or sulfur;Ar is mono- or bicyclic aryl or pyridyl;R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl;R.sub.5 and R.sub.6 together can represent methylenedioxy;and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.
    Type: Grant
    Filed: April 4, 1983
    Date of Patent: March 5, 1985
    Assignee: Boehringer Mannheim GmbH
    Inventors: Fritz Wiedemann, Wolfgang Kampe, Max Thiel, Gisbert Sponer, Egon Roesch, Karl Dietmann
  • Patent number: 4501908
    Abstract: Racemic carboxylic acids are resolved into their enantiomers using optically active enantiomers of four lactones as resolving agents. The four lactones are 2,3-isopropylidene-ribonic acid-1,4-lactone, 1,2-isopropylideneglucofuranurono-3,6-lactone, 2-hydroxy-3,3-dimethyl-1,4-butyrolactone and 3,4-isopropylidene-arabino-1,5-lactone. Novel diastereoisomeric esters of the acids with the lactones are disclosed.
    Type: Grant
    Filed: March 1, 1982
    Date of Patent: February 26, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Colin C. Duke, Robert J. Wells
  • Patent number: 4495352
    Abstract: 1-Aryloxy-3-[(3-indolyl)-tert.-butyl]amino-2-propanols having a heterocyclic aryl-attached substituent or aryl-fused heterocyclic ring are antihypertensive agents having vasodilator and adrenergic .beta.-receptor blocking action.
    Type: Grant
    Filed: December 3, 1981
    Date of Patent: January 22, 1985
    Assignee: Mead Johnson & Company
    Inventors: William E. Kreighbaum, William T. Comer