Plural Rings In Acid Moiety With Nitrogen Bonded Directly To At Least One Of The Rings Patents (Class 560/48)
  • Patent number: 5151544
    Abstract: Disclosed is a process for the synthesis of enantiomerically pure R and S isomers of 2,7-difluoro-4-methoxyspiro[9H-fluorene-9,4-imidazolidene]-2',5'-dione from 2,7-difluoro-4-methoxyfluorenone. Intermediate amino acid esters and urea esters and their preparation are also described.
    Type: Grant
    Filed: May 25, 1990
    Date of Patent: September 29, 1992
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark T. DuPriest, Raymond E. Conrow, Daniel Kuzmich
  • Patent number: 5136081
    Abstract: The invention provides a process for the preparation of fungicidally active cyclopentene derivatives of the general formula ##STR1## cyclopentane derivatives of the general formula ##STR2## and cyclohexane derivatives of the general formula ##STR3## in which n, R, R.sup.1, R.sup.2, R.sup.5, X and Y are as herein defined. Compounds of formula II and III are also provided which are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.
    Type: Grant
    Filed: September 11, 1989
    Date of Patent: August 4, 1992
    Assignee: Shell Internationale Research Maatschappij B.V.
    Inventor: Paul H. Briner
  • Patent number: 5128479
    Abstract: Oxidized diphenylheteroalkanes of the formula I ##STR1## where R.sup.1 to R.sup.6 and A have the meanings specified in the description, and the preparation thereof are described. The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: January 29, 1990
    Date of Patent: July 7, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5107053
    Abstract: A ruthenium phosphine complex having catalytic, hydrogenation activity is disclosed. The catalyst as the formula ##STR1## wherein R and R' are the same or different and are C.sub.1 to C.sub.6 linear or branched alkyl; R" is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl; R.sub.1 is C.sub.1 to C.sub.6 linear or branched alkyl; and n is an integer from 1 to 6.The phosphine complex is particularly useful in the asymmetric hydrogenation of unsaturated carboxylic acids or alkyl esters thereof.
    Type: Grant
    Filed: October 25, 1991
    Date of Patent: April 21, 1992
    Assignee: Ethyl Corporation
    Inventor: Tse-Chong Wu
  • Patent number: 5100917
    Abstract: The present invention relates to novel A-nor-steroid-3-carboxylic acid derivatives and to their use as inhibitors of mammalian 5.alpha.-reductase.
    Type: Grant
    Filed: September 11, 1990
    Date of Patent: March 31, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Philippe Bey, Thomas R. Blohm
  • Patent number: 5087743
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: January 23, 1990
    Date of Patent: February 11, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5084593
    Abstract: Leuco dyes of the formula (I) are disclosed, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent an alkyl group having 1 to 10 carbon atoms; X represents hydrogen, an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms or a halogen; and Y represents R.sub.5 --Z--SO.sub.2 NH--, R.sub.6 --Z--CONH--, or ##STR2## in which Z represents ##STR3## R.sub.5 and R.sub.6 each represent hydrogen, an alkyl group having 1 to 10 carbon atoms, or a halogen; and R.sub.7 and R.sub.8 each represent hydrogen, a cyano group, or --COR.sub.9, in which R.sub.9 represents a lower alkyl group, a lower alkoxyl group, a phenyl group which may be substituted by an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms, or a halogen; a naphthyl group which may be substituted by an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms or a halogen with the proviso that R.sub.7 and R.sub.8 are not both hydrogen.
    Type: Grant
    Filed: December 14, 1990
    Date of Patent: January 28, 1992
    Assignee: Ricoh Company, Ltd.
    Inventors: Hiroshi Gotoh, Shigeru Kusakata, Isao Shiojima
  • Patent number: 5068250
    Abstract: Compounds such as 1-(4-bromoacetamidobenzyl)-5-methoxy-2-methylindole-3-acetic acid, N-(4-bromoacetamidophenyl) anthranilic acid and N-(3-bromoacetamidophenyl) anthranilic acid function as irreversible ligands for nonsteroidal antiinflammatory drug (NSAID) and prostaglandin binding sites. It is therefore expected that these compounds, and analogs thereof, will have utility as anti-inflammatory drugs, as affinity labeling agents and as ligands for use in affinity chromatography.
    Type: Grant
    Filed: September 29, 1988
    Date of Patent: November 26, 1991
    Assignee: Trustees of University of Pennsylvania
    Inventors: Trevor M. Penning, Leslie J. Askonas
  • Patent number: 5053525
    Abstract: Mevinolin-like compounds in which the lactone is opened and the hydroxyl function produced thereby is replaced by an oxo function are potent HMG-CoA reductase inhibitors possessing one less asymmetric center.
    Type: Grant
    Filed: February 13, 1986
    Date of Patent: October 1, 1991
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Ta J. Lee, Gerald E. Stokker
  • Patent number: 5026912
    Abstract: A process for selectively producing ortho-alkylated aromatic amines in high selectivity relative to N-alkylated aromatic amines. The process comprises reacting an aromatic amine, having at least one hydrogen atom in a position ortho to the amine functionality, and an olefin under conditions sufficient to effect an alkylation reaction, in the presence of a zeolite catalyst which has been thermally pretreated by heating the catalyst to a temperature greater than about 500.degree. C. for a period ranging from 0.5 to about 10 hours while sweeping an inert gas over the heated catalyst to remove water and ammonia formed during the thermal treatment, and subsequently recovering the alkylated aromatic amine.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: June 25, 1991
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Rakesh Agrawal, Steven R. Auvil
  • Patent number: 4990650
    Abstract: 1. An aromatic derivative having the formula (I) or the salt thereof: ##STR1## wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, hydroxyl, a halogen atom, or OR.sup.3 wherein R.sup.3 is C.sub.1 -C.sub.10 alkyl; A-B represents a hydrocarbon moiety having 1 to 10 carbon atoms and containing at least one double bond or a sulfur- or oxygen-containing hydrocarbon moiety having 1 to 10 carbon atoms; n is an integer of 2 to 4; X represents a group ##STR2## and Y represents a hydrogen atom; alkyl having 1 to 5 carbon atoms which may be substituted with aryl; alkenyl having 2 to 5 carbon atoms which may be substituted with aryl or aryl substituted with at least one C.sub.1 -C.sub.5 alkoxy; aryl which may be substituted with at least one carboxy or C.sub.1 -C.sub.5 alkoxycarbonyl or C.sub.1 -C.sub.5 alkoxy; provided that, when R.sup.1 and R.sup.2 are both hydrogen, the moiety --A--B--(CH.sub.2).sub.n --X--Y does not represent ##STR3## wherein n=2 to 4 and R.sup.4 is hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: May 29, 1990
    Date of Patent: February 5, 1991
    Assignee: Teijin Limited
    Inventors: Atsuo Hazato, Seizi Kurozumi
  • 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: 4952731
    Abstract: Diphenylamines or N,N'-diphenyl-phenylenediamines can be obtained by heat-reacting an aniline or a phenylenediamine with preferably an excess of a phenol in an amount of 4 to 20 moles per mole of the aniline or phenylenediamine in th presence of a hydrogen transfer catalyst and a cyclohexanone corresponding to said phenol.The excess phenol used in the reaction undergoes reduction in the reaction system to form a cyclohexanone, which in turn reacts with the aniline or phenylenediamine to form a Schiff base and is thus consumed. The Schiff base forms the intended product by means of a dehydrogenation reaction, and the hydrogen evolved at this time reduces the phenol to form a cyclohexanone.The phenol present in excess thus becomes in the system a solvent, a starting material for the cyclohexanone, and an acceptor of the hydrogen that forms as a by-product at the time of formation of the intended product.
    Type: Grant
    Filed: August 15, 1988
    Date of Patent: August 28, 1990
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Teruyuki Nagata, Akihiro Tamaki, Nobuyuki Kajimoto, Masaru Wada
  • Patent number: 4906662
    Abstract: Disclosed are phenol derivatives of the formula ##STR1## wherein R.sup.1 is a substituted phenyl group, R.sup.2 and R.sup.3 are C.sub.1 -C.sub.6 alkyl group and of the formula ##STR2## wherein R.sup.8, R.sup.9 and R.sup.10 are C.sub.1 -C.sub.6 alkyl and the like and A is H, C.sub.1 -C.sub.6 alkylsulfonyl and the like substituents. These compounds and some related compounds have anti-inflammatory activity and lipoxygenase inhibitory activity.
    Type: Grant
    Filed: January 27, 1987
    Date of Patent: March 6, 1990
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Kinji Hashimoto, Kiyoto Goto, Ken-ichi Kanai, Yoshiaki Tsuda
  • Patent number: 4889947
    Abstract: Sunscreen compositions are described which contain certain substituted naphthalenylidenes which act as UV filters when incorporated in a carrier in amounts ranging from 0.1-50% by weight.
    Type: Grant
    Filed: July 28, 1988
    Date of Patent: December 26, 1989
    Assignee: ICI Americas Inc.
    Inventors: Charalambos J. Phalangas, Thomas P. Cleary
  • Patent number: 4880810
    Abstract: 1-Phenylquinazoline-1H,3H-2,4-diones and 1-phenylpyrido-[2,3d]-pyrimidine-1H,3H-2,4-diones, their esters and acid addition salts, and pharmaceutical compositions containing such compounds have antidepressant, anti-inflammatory and analgesic activity.
    Type: Grant
    Filed: January 3, 1989
    Date of Patent: November 14, 1989
    Assignee: Pfizer Inc.
    Inventor: John A. Lowe, III
  • Patent number: 4875930
    Abstract: As new compound is provided a cyclohexane derivative of the formula ##STR1## wherein R.sup.1 is a hydrogen or a lower alkyl; R.sup.2 is a lower alkyl; R.sup.3 is a hydrogen, an alkyl, an alkenyl, a hydroxyalkyl, a cycloalkyl, a morpholino, an aminoalkyl, an N-alkylaminoalkyl, an N,N-di-alkylaminoalkyl, an alkoxycarbonylalkyl, a group of the formula --(CH.sub.2).sub.l --R.sup.4 where R.sup.4 is a lower alkoxy, a lower alkylthio, a benzylthio, an anilino, a morpholino, a piperazino, a piperidino or a lower alkyl-substituted piperidino and l is 2 or 3, a group of the formula ##STR2## where X is a halogen, a lower alkyl, a lower alkoxy, a phenoxy or an alkoxycarbonylalkyloxy, m is zero or 1 and n is an integer of zero to 2, inclusive, a group of the formula --CH.sub.2 --R.sup.5 where R.sup.5 is a furyl, a thenyl or a pyridyl, or a group of the formula ##STR3## where R.sup.5 is as defined above; or a salt of said cyclohexane derivative.
    Type: Grant
    Filed: April 26, 1988
    Date of Patent: October 24, 1989
    Inventors: Masafumi Matsuzawa, Hiroshi Hokari, Shoji Kusano, Takeshige Miyazawa, Yasufumi Toyokawa
  • Patent number: 4873350
    Abstract: The present invention relates to new diselenobis-benzoic acid amides of primary and secondary amines of the general formula (I): ##STR1## and processes for the treatment of diseases in humans caused by a cell injury.
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: October 10, 1989
    Assignee: A Nattermann & CIE GmbH
    Inventors: Andre Welter, Harmut Fischer, Leon Christiaens, Albrecht Wendel, Eugen Etschenberg, Norbert Dereu, Peter Kuhl, Eric Graf
  • 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: 4861799
    Abstract: A benzoylurea compound having the formula: ##STR1## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom or a methyl group, provided that X.sub.1 and X.sub.2 are not simultaneously hydrogen atoms, Y is independently a hydrogen atom, a halogen atom, an alkyl group which may be substituted by halogen, a --CO.sub.2 R.sub.1 group wherein R.sub.1 is a hydrogen atom, a cation or an alkyl group, or a --OR.sub.1 group wherein R.sub.1 is as defined above, A.sub.1 is .dbd.N--or ##STR2## wherein Y is as defined above, W is an oxygen atom, a sulfur atom or ##STR3## wherein R.sub.1 is as defined above, k is an integer of from 1 to 3, l is 0 or 1, and Ar is ##STR4## wherein Z is independently a hydrogen atom, a halogen atom, an alkyl group which may be substituted by halogen, an alkoxy group which may be substituted by halogen, a nitro group, a cyano group or a --S(O).sub.n R.sub.2 group wherein R.sub.2 is an alkyl group which may be substituted by halogen and n is 0, 1 or 2, A.sub.
    Type: Grant
    Filed: September 30, 1987
    Date of Patent: August 29, 1989
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Takahiro Haga, Tadaaki Toki, Toru Koyanagi, Yasuhiro Fujii, Kiyomitsu Yoshida, Osamu Imai
  • Patent number: 4859725
    Abstract: A compound of formula I ##STR1## in which R to R.sub.5 are organic radicals, for use as a light stabilizer in polymeric systems.
    Type: Grant
    Filed: August 23, 1988
    Date of Patent: August 22, 1989
    Assignee: Sandoz Ltd.
    Inventor: Lajos Avar
  • Patent number: 4857660
    Abstract: 1-Phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.
    Type: Grant
    Filed: April 22, 1988
    Date of Patent: August 15, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Alex Alder, Jaroslav Stanek, Daniel Bellus
  • Patent number: 4806146
    Abstract: Compounds of the formula ##STR1## wherein R is halogen, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, cyano, nitro, S(O).sub.n R wherein R is C.sub.1 -C.sub.4 alkyl and n is the integer 0, 1 or 2; and R.sup.2 through R.sup.8 are hydrogen or certain substituents, their salts, herbicidal compositions containing the compound or salts and the herbicidal use thereof.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: February 21, 1989
    Assignee: Stauffer Chemical Company
    Inventor: Charles G. Carter
  • Patent number: 4804783
    Abstract: Diphenylamines or N,N'-diphenyl-phenylenediamines can be obtained by heat-reacting an aniline or a phenylenediamine with preferably an excess of a phenol in an amount of 4 to 20 moles per mole of the aniline or phenylenediamine in the presence of a hydrogen transfer catalyst and a cyclohexanone corresponding to said phenol.The excess phenol used in the reaction undergoes reduction in the reaction system to form a cyclohexanone, which in turn reacts with the aniline or phenylenediamine to form a Schiff base and is thus consumed. The Schiff base forms the intended product by means of a dehydrogenation reaction, and the hydrogen evolved at this time reduces the phenol to form a cyclohexanone.The phenol present in excess thus becomes in the system a solvent, a starting material for the cyclohexanone, and an acceptor of the hydrogen that forms as a by-product at the time of formation of the intended product.
    Type: Grant
    Filed: July 31, 1987
    Date of Patent: February 14, 1989
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Teruyuki Nagata, Akihiro Tamaki, Nobuyuki Kajimoto, Masaru Wada
  • Patent number: 4792550
    Abstract: A novel 13-aza-14-oxo-TXA.sub.2 analogue of general formula: ##STR1## wherein symbol A represents --CH.sub.2 CH.sub.2 --(CH.sub.2).sub.m --, cis--CH.dbd.CH--(CH.sub.2).sub.m --, --CH.sub.2 O--(CH.sub.2).sub.m --, --S--(CH.sub.2).sub.m -- ##STR2## R.sup.2 represents a bond or a straight or branched alkylene or alkenylene group of from 1 to 10 carbon atom(s) unsubstituted or substituted;R.sup.3 represents(i) a phenyl, phenoxy or phenylthio group unsubstituted or substituted,(ii) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 6 carbon atom(s) unsubstituted or substituted,(iii) a cycloalkyl, cycloalkyloxy or cycloalkylthio group of from 4 to 7 carbon atoms unsubstituted or substituted,(iv) a naphthyl, indolyl or indanyl group, or(v) an amino group unsubstituted or substitutedR.sup.4 represents a hydrogen atom or a methyl group.
    Type: Grant
    Filed: June 11, 1985
    Date of Patent: December 20, 1988
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hajimu Miyake, Tadao Okegawa, Akiyoshi Kawasaki
  • Patent number: 4775720
    Abstract: Described are schiff base reaction products of alkyl anthranilates having the structure: ##STR1## wherein R.sub.3 represents methyl or ethyl and aldehydes of the generic structure: ##STR2## wherein R represents unsaturated hydrocarbyl and alkoxy hydrocarbyl moieties or mixtures of aldehydes having the structures: ##STR3## wherein R.sub.1 and R.sub.2 are different alkoxy hydrocarbyl moieties and hydrocarbyl moieties including the aldehydes:(a) bergamal having the structure: ##STR4## (b) floralozone having the structure: ##STR5## (c) pino acetaldehyde having the structure: ##STR6## (d) pino isobutyraldehyde having the structure: ##STR7## (e) melonal having the structure: ##STR8## and (f) canthoxal having the structure: ##STR9## and organoleptic uses thereof in augmenting or enhancing the aroma or taste of consumable materials including perfume compositions, colognes, perfumed articles, foodstuffs, chewing gums and beverages.
    Type: Grant
    Filed: October 29, 1987
    Date of Patent: October 4, 1988
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Braja D. Mookherjee, Robert W. Trenkle, Nicholas Calderone, Keith P. Sands, Myrna L. Hagedorn
  • Patent number: 4764640
    Abstract: 1-phenyl-3-azabicyclo[3.1.1]-heptane-2,4-diones of the formula ##STR1## in which R.sub.1 represents hydrogen or a saturated or unsaturated, aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or aromatic-aliphatic hydrocarbon radical having up to and including 18, preferably up to and including 12, carbon atoms, R.sub.2 represents hydrogen, lower alkyl, sulpho or acyl, R.sub.3 represents hydrogen or lower alkyl and R.sub.4 represents hydrogen, lower alkyl, phenyl or phenyl substituted by --N(R.sub.2)(R.sub.3), and salts of these compounds, have valuable pharmacological properties, are effective as aromatase inhibitors and can therefore be used for the treatment of hormone-dependent diseases, especially mammary carcinoma.
    Type: Grant
    Filed: April 1, 1987
    Date of Patent: August 16, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Alex Alder, Jaroslaw Stanek, Daniel Bellus
  • Patent number: 4764619
    Abstract: An optically active compound having the formula: ##STR1## wherein each of Z and Z' is a single bond, --COO--, --OCO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 -- or --CH.sub.2 O--, R is an alkyl group having from 1 to 12 carbon atoms, an alkoxyl group having from 1 to 12 carbon atoms, a cyano group or a halogen atom, each of rings A and B is a 1,4-di-substituted phenylene group or a trans-1,4-di-substituted cyclohexylene group, n is 0 or 1, X is ##STR2## wherein * indicates an optical center, and R' is an alkyl group having from 2 to 12 carbon atoms or ##STR3## where R" is a hydrogen atom, an alkyl or alkoxy group having from 1 to 12 carbon atoms, provided that when X is ##STR4## R is the alkyl group or the alkoxy group.
    Type: Grant
    Filed: March 21, 1986
    Date of Patent: August 16, 1988
    Assignee: Asahi Glass Company Ltd.
    Inventors: Tomoki Gunjima, Ryutaro Takei, Eriko Aoyama
  • Patent number: 4762844
    Abstract: Alkyl-1-cyclopropyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids of the formula ##STR1## in which X.sup.1, X.sup.2 and X.sup.3 each independently is hydrogen, a nitro group, a halogen atom or an alkyl radical with 1 to 3 carbon atoms, with the proviso that at least one of them is an alkyl radical,or pharmaceutically acceptable salts or hydrates thereof, are antibacterially active and promote animal growth.
    Type: Grant
    Filed: November 5, 1985
    Date of Patent: August 9, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Michael Schriewer, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4727181
    Abstract: Prepare esters of .alpha.-halocinnamic acid and related compounds in high yield under relatively mild conditions.
    Type: Grant
    Filed: April 21, 1986
    Date of Patent: February 23, 1988
    Assignee: The Dow Chemical Company
    Inventor: William J. Kruper, Jr.
  • Patent number: 4724263
    Abstract: Compounds of the formula ##STR1## wherein R is hydrogen; halogen; C.sub.1 -C.sub.2 alkyl; C.sub.1 -C.sub.2 alkoxy; nitro; cyano; C.sub.1 -C.sub.2 haloalkyl; or R.sup.a SO.sub.m --wherein m is 0 or 2 and R.sup.a is C.sub.1 -C.sub.2 alkyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl or ethyl;R.sup.5 and R.sup.6 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n --wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R.sup.d independently are hydrogen or C.sub.1 -C.sub.4 alkyl; (11) R.sup.e C(O)--wherein R.sup.e is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; or (12) --SO.sub.2 NR.sup.c R.sup.d wherein R.sup.c and R.sup.d are as defined; and (13) --N(R.sup.c)C(O)R.sup.d wherein R.sup.c and R.sup.
    Type: Grant
    Filed: June 9, 1986
    Date of Patent: February 9, 1988
    Assignee: Stauffer Chemical Company
    Inventor: Charles G. Carter
  • Patent number: 4723005
    Abstract: New anisotropic compounds of the formula (1) are useful in liquid crystal mixtures for electrooptical displays; at least one of the end groups of the compounds (1) is an alkyl group which carries cyano or halogen in a terminal or non-terminal position. This offers advantages for longitudinal polarization and/or cross-polarization of the anisotropic compounds with the aid of the comparatively highly polarizing cyano or halogen substituents, in particular high clear points, low .DELTA..epsilon./.epsilon..perp. values and/or negative .DELTA..epsilon. values.
    Type: Grant
    Filed: September 10, 1984
    Date of Patent: February 2, 1988
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Tuong Huynh-Ba, Maged A. Osman
  • Patent number: 4709096
    Abstract: Stilbene derivatives of the formula (I) ##STR1## and distyryl derivatives of the formula (II), ##STR2## as defined in the specification, and an electrophotographic photoconductor comprising an electroconductive support material and a photosensitive layer overlayed thereon comprising at least one of the above derivatives, are disclosed.
    Type: Grant
    Filed: February 22, 1985
    Date of Patent: November 24, 1987
    Assignee: Ricoh Company, Ltd.
    Inventor: Masaomi Sasaki
  • Patent number: 4709079
    Abstract: Non-steroidal, anti-inflammatory drugs are disclosed which are polyprenyl alcohol esters of indolyl lower carboxylic acids, phenyl lower carboxylic acids, acetyl salicyclic acid, anthranilic acid and derivatives thereof.
    Type: Grant
    Filed: January 17, 1986
    Date of Patent: November 24, 1987
    Assignee: Eisai Co., Ltd.
    Inventors: Isao Yamatsu, Shinya Abe, Yuichi Inai, Takeshi Suzuki, Kensaku Kinoshita, Mannen Mishima, Yoshinori Katoh, Seiichi Kobayashi, Manabu Murakami, Kouzi Yamada
  • Patent number: 4683325
    Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Grant
    Filed: October 17, 1984
    Date of Patent: July 28, 1987
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Richard Frenette, Joshua Rokach, Masatoshi Kakushima, Robert N. Young
  • Patent number: 4666936
    Abstract: Amide derivatives of 2-(p-aminobenzyl)-butyric acid and esters thereof having a hypolipidemizing and hypocholesterolemizing pharmaceutical activity and their preparation are described.Included are compounds of the formula ##STR1## wherein R and R' together represent the group ##STR2## or the group ##STR3## and R" is hydrogen or a 1 to 6 carbon alkyl group.
    Type: Grant
    Filed: August 7, 1985
    Date of Patent: May 19, 1987
    Assignee: Medosan Industrie Biochimiche Riunite S.p.A.
    Inventor: Alessandro Baglioni
  • Patent number: 4654387
    Abstract: Compounds corresponding to the following general formula: ##STR1## wherein R.sup.0 represents H or, together with R.sup.1, represents --CO-- when X represents --CO-- or, together with R.sup.2, represents --CO-- when X represents --CH.sub.2 --CO,a residue of R, R.sup.1 and R.sup.2, H, C.sub.1 -C.sub.4 alkyl, aryl, COOR.sup.5 or, when R.sup.0 represents H and X represents --CO--, ##STR2## and the other residues R, R.sup.1 and R.sup.2 represent H; R.sup.3 represents H or CH.sub.3 ;R.sup.4 represents C.sub.7 -C.sub.20 aralkyl;R.sup.5 represents H, C.sub.1 -C.sub.4 alkyl or C.sub.6 -C.sub.12 aryl;X represents a residue --(CH.sub.2).sub.n CO--, --(CH.sub.2).sub.n SO.sub.2, --CH.sub.2 --, --CH.sub.2 O--CO-- ##STR3## m represents 1 or 2; and n represents 0 or 1;are suitable for use as incorporable antiagers for polymers, particularly nitrile rubber.
    Type: Grant
    Filed: August 7, 1985
    Date of Patent: March 31, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Josef Buysch, Zsolt Szentivanyi, Josef Witte
  • Patent number: 4638078
    Abstract: The invention is a compound which comprises an amido alkenoic acid or a water-soluble salt thereof and and arylcyclobutene moiety, wherein the cyclobutene moiety is fused to the aryl radical, and wherein the amide nitrogen is connected to the aryl radical of the arylcyclobutenyl moiety by a direct bond or a bridging member.
    Type: Grant
    Filed: April 25, 1985
    Date of Patent: January 20, 1987
    Assignee: The Dow Chemical Company
    Inventor: Robert A. Kirchhoff
  • Patent number: 4634777
    Abstract: Compounds of the general formula: ##STR1## wherein A and B are both hydrogen, or one of A and B is a group (G) of the formula: ##STR2## and the other is a group R.sup.5 wherein R.sup.1 is an aryl group or a heterocyclic group, both of them being optionally substituted, and R.sup.4 and R.sup.5 are both hydrogen or together form a single chemical bond,R.sup.2 and R.sup.2 ' are independently hydrogen, halogen, nitro, lower alkyl or lower alkoxy, andR.sup.3 and R.sup.3 ' are independently carboxy or its functional derivative, with the proviso that (a) when A and B are both hydrogen, then R.sup.2 and R.sup.2 ' cannot be both hydrogen,and, where applicable, pharmaceuticably acceptable salts thereof are hyaluronidase inhibitors, and useful as anti-allergic agent and anti-ulcerous agent. Among the compound (I'), those wherein when one of A and B is the group (G) and the other is the group R.sup.5 wherein R.sup.4 and R.sup.5 together form a single chemical bond, R.sup.1 is unsubstituted aryl and R.sup.2 and R.sup.
    Type: Grant
    Filed: February 1, 1985
    Date of Patent: January 6, 1987
    Assignee: Sawai Pharmaceutical Co., Ltd.
    Inventors: Toshio Satoh, Hitoshi Matsumoto, Hisao Kakegawa, Yoshiko Kato, Juichi Riku, Junji Yoshinaga, Yoshifumi Kanamoto
  • Patent number: 4628061
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: August 23, 1983
    Date of Patent: December 9, 1986
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4624964
    Abstract: Aryl oxo-alkynoates are 5-lipoxygenase inhibitors, making them useful for the treatment of inflammation, chronic obstructive lung disease or psoriasis. These compounds have the formula: ##STR1## wherein n is 1-12;R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or phenyl; andAryl is naphthyl, phenyl or phenyl substituted with a variety of groups.
    Type: Grant
    Filed: March 27, 1985
    Date of Patent: November 25, 1986
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: William J. Sipio
  • Patent number: 4595759
    Abstract: The 2-aryl-1-aminoalkylcyclohexane nitrile, carboxylic acid or amide and derivatives thereof and methods of preparing same.
    Type: Grant
    Filed: February 15, 1985
    Date of Patent: June 17, 1986
    Assignee: Pennwalt Corporation
    Inventors: Thomas A. Davidson, Telfer L. Thomas
  • Patent number: 4570006
    Abstract: Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsine, anti-plasmin, anti-kallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: October 24, 1984
    Date of Patent: February 11, 1986
    Assignee: Torii & Co. Ltd.
    Inventors: Setsuro Fujii, Takashi Yaegashi, Toyoo Nakayama, Yojiro Sakurai, Shigeki Nunomura, Toshiyuki Okutome
  • Patent number: 4570014
    Abstract: Novel plant growth regulant composition comprising as an active ingredient at least one cycloalkanecarboxylic acid compound of the formula ##STR1## in which R is hydroxyl, alkoxy, aralkoxy, amino, alkylamino, dialkylamino or the radicalO.sup..crclbar. M.sup..sym.whereinM.sup..sym. is one alkali metal ion equivalent or alkaline earth metal ion equivalent, or an ammonium, alkylammonium, dialkylammonium, trialkylammonium or tetraalkylammonium ion,R.sup.1 is amino or the radical ##STR2## wherein R.sup.2 is hydrogen, alkyl or aryl, orR.sup.1 is the radical --N.sup..sym. H.sub.3 X.sup..crclbar.,wherein X.sup.63 is chloride, bromide or iodide, and n is 1, 2, 3, 4 or 5,in admixture with a solid or liquefied gaseous diluent or carrier or in admixture with a liquid diluent or carrier containing a surface-active agent.
    Type: Grant
    Filed: December 15, 1981
    Date of Patent: February 11, 1986
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Schroder, Klaus Lurssen
  • Patent number: 4568695
    Abstract: Novel 2-amino-3-benzoylphenethylalcohols are provided having the formula: ##STR1## wherein; X is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl, andY is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, --S--loweralkyl, ##STR2## The compounds exhibit anti-inflammatory activity.
    Type: Grant
    Filed: December 7, 1983
    Date of Patent: February 4, 1986
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Henry W. Moran, William J. Welstead, Jr.
  • Patent number: 4567288
    Abstract: The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxylates (Z), their preparation and their use as useful drugs for the treatment of various pains.The new derivatives of the present invention have the general formula I ##STR1## in which: R represents a hydrogen or halogen atom, a C.sub.1 to C.sub.4 lower alkyl group, a C.sub.1 to C.sub.4 lower alkoxy group, or a nitro, amino, sulfamoyl or hydroxy group;n represents the values 1, 2 or 3;(R).sub.n may together with the benzene ring also form the naphthyl group;R.sub.1 represents a linear or branched C.sub.1 to C.sub.5 alkyl or alkenyl group or an aryl or benzyl group;R.sub.2 and R.sub.3 represent a hydrogen atom, a linear or branched C.sub.1 to C.sub.5 alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl or dialkylaminoalkyl group or an aryl, arylalkyl or cycloalkyl group;R.sub.2 and R.sub.3 possibly also forming a heterocycle of 5 or 6 members with the adjacent nitrogen atom,provided however that when R.sub.
    Type: Grant
    Filed: October 1, 1984
    Date of Patent: January 28, 1986
    Assignee: Pierre Fabre S.A.
    Inventors: Henri Cousse, Gilbert Mouzin, Bernard Bonnaud, Marie Charveron, Francois Fauran
  • Patent number: 4551264
    Abstract: New polyhalogenoaromatic compounds of Formula I ##STR1## wherein Y and Z are each independently alkyl, alkoxy or alkanoyl each of 1 to 12 C atoms, --COOR.sup.1, --O--CO--R.sup.1, CN, NO.sub.2, NH.sub.2 or OH;Q is one or two identical or different radicals selected from Ph, Cy, 1,4-bicyclo[2,2,2]octylene or 1,3-dioxane-2,5-diyl;X.sup.1 to X.sup.4 are each independently H, F, Cl or Br;R.sup.1 is alkyl of 1 to 4 C atoms, Ph--R.sup.2 or Cy--R.sup.2 ;R.sup.2 is alkyl or alkoxy each of 1-12 C atoms or CN;Ph is 1,4-phenylene; and Cy is 1,4-cyclohexylene,can be used as components of liquid-crystal dielectrics.
    Type: Grant
    Filed: March 14, 1983
    Date of Patent: November 5, 1985
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rudolf Eidenschink, Michael Romer, Georg Weber
  • Patent number: 4536346
    Abstract: This disclosure describes novel substituted aralkanamidobenzoic acids and analogs thereof. These compounds are useful pharmaceutical agents for ameliorating atherosclerosis by inhibiting the formation and development of atherosclerotic lesions in the arterial wall of mammals.
    Type: Grant
    Filed: May 6, 1983
    Date of Patent: August 20, 1985
    Assignee: American Cyanamid Company
    Inventors: Robert G. Shepherd, Janis Upeslacis
  • Patent number: 4532255
    Abstract: Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula ##STR2## with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: January 20, 1984
    Date of Patent: July 30, 1985
    Assignee: Torii & Co., Ltd.
    Inventors: Setsuro Fujii, Toshiyuki Okutome, Toyoo Nakayama, Takashi Yaegashi, Masateru Kurumi
  • Patent number: 4514416
    Abstract: Amidino compounds represented by the formula (I) ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and anti-thrombin agents. Having strong anti-Cl (Clr, Cls) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula (II)R.sub.1 --COOH (II)with amidinophenol compound (III) and, if necessary, can be transformed into pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: May 21, 1984
    Date of Patent: April 30, 1985
    Assignee: Torii & Co. Ltd.
    Inventors: Setsuro Fujii, Takashi Yaegashi, Toyoo Nakayama, Yojiro Sakurai, Shigeki Nunomura, Toshiyuki Okutome