Chalcogen Bonded Directly At 2- And 4-positions Patents (Class 544/285)
  • Patent number: 5017298
    Abstract: Compounds suitable for use as extreme pressure (EP)/anti-wear (AW) agents in lubricating oil compositions, which compounds have the formula:R.sup.1 --S--X--S--S--R (I)wherein R.sup.1 is either R--S-- or hydrogen,R is independently either hydrocarbyl or substituted hydrocarbyl, andX comprises a heterocyclic ring having six atoms of which two are nitrogen atoms.
    Type: Grant
    Filed: March 12, 1990
    Date of Patent: May 21, 1991
    Assignee: BP Chemicals Limited
    Inventor: Sean P. O'Connor
  • Patent number: 5017211
    Abstract: The invention is concerned with novel compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the significances given in the description, as well as enol ethers and salts thereof and their manufacture, weed control compositions which contain such compounds as the active substance and the use of the active substances or compositions for the control of weeds. The invention is also concerned with certain novel starting materials and their production.
    Type: Grant
    Filed: May 19, 1989
    Date of Patent: May 21, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Jean Wenger, Paul Winternitz, Martin Zeller
  • Patent number: 5008266
    Abstract: 4(3H)-Quinazolinone derivative of formula (I) are provided. ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, an aryl group, a substituted aryl group, or an aralkyl group; R.sub.2 is a C.sub.1 -C.sub.6 alkylamino group, a phenyl group, a substituted phenyl group, or a 5- or 6-membered heterocyclic group containing one or more N, O or S as a hetero atom or atoms, said heterocyclic group optionally being substituted or fused with a benzene ring; n is 1 or 2; or R.sub.2 represents a geranyl group or a dipyridylmethyl group together with the group --(CH.sub.2).sub.n --; and X is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a halogen atom, and pharmaceutically acceptable acid addition salts thereof. They are useful as antiucler agents.
    Type: Grant
    Filed: July 26, 1989
    Date of Patent: April 16, 1991
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Toshihiro Takahashi, Tatsuo Horaguchi, Koichi Nakamaru, Yoshikuni Suzuki
  • Patent number: 4992550
    Abstract: A quinazoline of the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylalkyl, halogeno, hydroxy, mercapto, pyridylthio, pyrimidinylthio, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents and wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid;or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumour activity.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: February 12, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventor: Leslie R. Hughes
  • Patent number: 4988809
    Abstract: The invention relates to substituted 2-pyrimidinyl-1- piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.
    Type: Grant
    Filed: February 21, 1990
    Date of Patent: January 29, 1991
    Assignee: Troponwerke GmbH & Co., KG
    Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, THomas Glaser, Teunis Schuurmann
  • Patent number: 4985441
    Abstract: The invention relates to quinazoline derivatives which possess anti-tumor activity; to processes for their manufacture; and to pharmaceutical compositions containing them.The invention provides a quinazoline of the formula: ##STR1## wherein R.sup.1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R.sup.1 is substituted alkyl or alkoxy each of up to 3 carbon atoms;R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl or halogenoalkyl each of up to 6 carbon atoms;Ar is phenylene or heterocyclene;L is a group of the formula --CO.NH-- or --CO.NR.sup.3 --, wherein R.sup.3 is alkyl of up to 6 carbon atoms; andY is hydrogen or alkyl, cycloalkyl, alkenyl or alkynyl each of up to 6 carbon atoms; orY is a group of the formula --A--Y.sup.1 in which A is alkylene of up to 6 carbon atoms and Y.sup.1 includes hydroxy, amino and cyano, and alkoxy, alkylamino and alkylthio each of up to 6 carbon atoms.
    Type: Grant
    Filed: April 3, 1990
    Date of Patent: January 15, 1991
    Assignees: Imperial Chemical Industries plc, National Research Development Corp.
    Inventors: Leslie R. Hughes, John Oldfield, Stephen J. Pegg
  • Patent number: 4985171
    Abstract: An anthraquinone type compound which is represented by the following general formula (I) and which exhibits yellow to orange-colored hue; and a composition for liquid crystal display element obtained by dissolving the compound into liquid crystal: ##STR1## (where: X.sup.1 and X.sup.2 denote sulfur or selenium; and R.sup.1 and R.sup.2 represent a substituted or unsubstituted phenyl group, a substituted or unsubstituted naphthyl group, a substituted or unsubstituted pyridyl group, a substituted or unsubstituted pyrmidyl group or a tetrahydronaphthyl group, with the following exceptions:(1) X.sup.1 =X.sup.2 =S; R.sup.1 =R.sup.2 =a substituted or unsubstituted phenyl group =(2) X.sup.1 =X.sup.2 =S; R.sup.1 =a substituted or unsubstituted naphthyl group; R.sup.2 =a phenyl group or a naphthyl group(3) X.sup.1 =X.sup.2 =Se; R.sup.1 =R.sup.2 =a tetrahydronaphthyl group).
    Type: Grant
    Filed: January 2, 1990
    Date of Patent: January 15, 1991
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Konoe Miura, Tetsuo Ozawa, Junko Kanaya
  • Patent number: 4981856
    Abstract: A quinazoline of the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylthio, arylalkyl, halogeno, hydroxy or mercapto, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl or alkynyl, or substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents;wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid;wherein R.sup.4 is hydrogen or alkyl;wherein R.sup.5 is hydrogen or alkyl; andwherein each of R.sup.6, R.sup.7 and R.sup.8 is hydrogen, hydroxy, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, phenyl, halogeno, nitro, cyano or amino, or substituted alkyl, alkoxy or alkylthio;provided that at least one of R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 is other than hydrogen;or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumour activity.
    Type: Grant
    Filed: April 12, 1990
    Date of Patent: January 1, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventor: Leslie R. Hughes
  • Patent number: 4963550
    Abstract: The invention relates to novel substituted N-phenylthioureas, N-phenylisothioureas and N-phenylcarbodiimides of formula ##STR1## wherein R.sub.1 to R.sub.5 and Z are as defined in the specification.The invention further relates to the preparation of said compounds and to compositions containing them for use in pest control, especially for controlling insects and representatives of the order Acarina that are pests of plants and animals, in particular plant-destructive sucking and eating pests.
    Type: Grant
    Filed: February 7, 1990
    Date of Patent: October 16, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund, Odd Kristiansen
  • Patent number: 4942169
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2.] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.
    Type: Grant
    Filed: March 10, 1989
    Date of Patent: July 17, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 4937343
    Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.
    Type: Grant
    Filed: September 22, 1988
    Date of Patent: June 26, 1990
    Assignee: Troponwerke GmbH & Co. KG
    Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
  • Patent number: 4920224
    Abstract: Variously substituted trans-3-[3-(3-hydroxypiperid-2-yl)-2-oxopropyl]quinazolin-4(3H)-ones, a method of controlling or preventing coccidiosis in poultry therewith, intermediates therefor, and a process for the preparation of certain intermediates therefor.
    Type: Grant
    Filed: March 13, 1989
    Date of Patent: April 24, 1990
    Assignee: Pfizer Inc.
    Inventor: Edward A. Glazer
  • Patent number: 4914098
    Abstract: Substituted N-phenylthioureas, N-phenylisothioureas and N-phenylcarbodiimides of formula ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.8 cycloalkyl, polycyclic alkyl containing a total of 7 to 10 carbon atoms, C.sub.1 -C.sub.12 alkyl which is substituted by 1 to 12 halogen atoms, C.sub.1 -C.sub.4 alkyl which is substituted by one or two C.sub.3 -C.sub.6 cycloalkyl radicals, alkoxyalkyl containing a total of 3 to 10 carbon atoms, C.sub.1 -C.sub.5 alkyl which is substituted by a phenyl radical, C.sub.1 -C.sub.5 alkyl which is substituted by a phenyl radical which is in turn substituted by one or two members selected from the group consisting of halogen, methyl, methoxy and ethoxy; or is C.sub.3 -C.sub.10 -alkenyl or C.sub.3 -C.sub.10 alkynyl, R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.3 is C.sub.1 -C.sub.4 alkyl, R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl, and R.sub.
    Type: Grant
    Filed: August 12, 1987
    Date of Patent: April 3, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund, Odd Kristiansen
  • Patent number: 4908365
    Abstract: The present invention relates to benzhydryloxyethylpiperazine derivatives of the formula: ##STR1## It also relates to processes for the preparation of the said derivatives and pharmaceutical compositions in which they are present. The said derivatives have an antihistaminic activity without a sedative component.
    Type: Grant
    Filed: July 7, 1987
    Date of Patent: March 13, 1990
    Inventors: Andre Buzas, Jean-Yves Merour, Roland Ollivier
  • Patent number: 4888426
    Abstract: Bicyclic heterocyclyl containing N-(bicyclic heterocyclyl)-4-piperidinamines having antihistaminic and serotonin-antagonistic properties which compounds are useful agents in the treatment of allergic diseases.
    Type: Grant
    Filed: June 1, 1987
    Date of Patent: December 19, 1989
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Joseph L. G. Torremans, Jozef F. Hens
  • Patent number: 4883800
    Abstract: The invention relates to compounds having aldose reductase-inhibitory activity of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl,R.sup.3 is phenyl(lower)alkyl which may have one or more substituent(s) selected from the group consisting of halogen, lower alkoxy, halo(lower)alkyl and lower alkyl,R.sup.4 is carboxy or protected carboxy,A is sulfur atom,Y is carbonyl, thiocarbonyl or sulfonyl andZ is lower alkylene,and pharmaceutically acceptable salts thereof, useful in treating diabetic complications.
    Type: Grant
    Filed: December 8, 1987
    Date of Patent: November 28, 1989
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masashi Hashimoto, Teruo Oku, Yoshikuni Ito, Takayuki Namiki, Kozo Sawada, Chiyoshi Kasahara, Yukihisa Baba
  • Patent number: 4861780
    Abstract: 4(3H)-Quinazolinone derivatives of formula (I) are provided. ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, an aryl group, a substituted aryl group, or an aralkyl group; R.sub.2 is a C.sub.1 -C.sub.6 alkylamino group, a phenyl group, a substituted phenyl group, or a 5- or 6-membered heterocyclic group containing one or more N, O or S as a hetero atom or atoms, said heterocyclic group optionally being substituted or fused with a benzene ring; n is 1 or 2; or R.sub.2 represents a geranyl group or a dipyridylmethyl group together with the group --(CH.sub.2).sub.n --; and X is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a halogen atom, and pharmaceutically acceptable acid addition salts thereof.They are useful as antiulcer agents.
    Type: Grant
    Filed: January 26, 1988
    Date of Patent: August 29, 1989
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Toshihiro Takahashi, Tatsuo Horaguchi, Koichi Nakamaru, Yoshikuni Suzuki
  • Patent number: 4854965
    Abstract: Herbicidal compositions containing 2,4-dioxo-and 2,4-dithio-1,3-dihydroquinazolines and a method of controlling broadleaved weeds in cereals applying to said weeds a herbicidally effective amount of a composition containing said dihydroquinazolines.
    Type: Grant
    Filed: June 22, 1987
    Date of Patent: August 8, 1989
    Assignee: Makhteshim Chemical Works, Ltd.
    Inventors: Peretz Bracha, Moshe Korat
  • Patent number: 4849518
    Abstract: Variously substituted trans-3-[3-(3-hydroxypiperid-2-yl)-2-oxopropyl]quinazoline-4(3H)-ones, a method of controlling or preventing coccidiosis in poultry therewith, intermediates therefor, and a process for the preparation of certain intermediates thereof.
    Type: Grant
    Filed: March 24, 1988
    Date of Patent: July 18, 1989
    Assignee: Pfizer Inc.
    Inventor: Edward A. Glazer
  • Patent number: 4849431
    Abstract: A novel piperidine derivative or a pharmacologically acceptable salt thereof is used in the treatment and prevention of dementias and sequelae of cerebrovascular diseases. These compounds also exhibit strong, highly selective anticholinesterase activity and may be orally or parenterally administered.
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: July 18, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 4833144
    Abstract: 2-Alkylsulfinyl-4(3H)-quinazolinone derivatives of formula (I) are provided. ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.6 alkyl group, an aryl group, a substituted aryl group or an aralkyl group, R.sub.2 is a phenyl group, a substituted phenyl group or a 5- or 6-membered heterocyclic group containing one or more N, O or S as a hetero atom or atoms, said heterocyclic group optionally being substituted or fused with a benzene ring, n is 1 or 2 and X is hydrogen, a C.sub.1 -C.sub.6 alkyl group or a halogen atom, and pharmaceutically acceptable acid addition salts thereof. They are useful as antiulcer agents.
    Type: Grant
    Filed: January 26, 1988
    Date of Patent: May 23, 1989
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Toshihiro Takahashi, Tatsuo Horaguchi, Koichi Nakamaru, Yoshikuni Suzuki
  • Patent number: 4831161
    Abstract: Prepare N-(amidoalkyl)imides by contacting an imide with a 2-oxazoline under reaction conditions, optionally in the presence of a solvent.
    Type: Grant
    Filed: June 24, 1987
    Date of Patent: May 16, 1989
    Assignee: The Dow Chemical Company
    Inventors: Pen-Chung Wang, Steven P. Crain
  • Patent number: 4824469
    Abstract: Compounds of the formula: ##STR1## where: A is oxygen or sulphur;R.sup.1 is phenyl or substituted phenyl in which the substituent is at least one member selected from the group consisting of halogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -haloalkoxy and nitro;R.sup.2 is 1-imidazolyl or 1,2,4-triazol-1-yl; andR.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are each hydrogen, halo, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy have valuable fungicidal properties.
    Type: Grant
    Filed: March 11, 1988
    Date of Patent: April 25, 1989
    Assignee: Schering Agrochemicals Ltd.
    Inventors: David E. Green, Albert Percival
  • Patent number: 4818756
    Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: April 4, 1989
    Assignee: Troponwerke GmbH & Co., KG
    Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
  • Patent number: 4812164
    Abstract: The invention is concerned with novel C.sub.1-4 -alkyl, C.sub.2-4 -alkenyl and C.sub.3 or 4 -alkynyl enol ethers of 3-aryluracils of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X are as defined in the specification, their manufacture, weed control compositions which contain such enol ethers as the active substance and the use of the active substances or compositions for the control of weeds. The invention is also concerned with certain novel intermediates, some of which possess herbicidal activity, and with weed control compositions containing such active substances.
    Type: Grant
    Filed: September 15, 1987
    Date of Patent: March 14, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Wenger, Paul Winternitz
  • Patent number: 4797403
    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: July 23, 1987
    Date of Patent: January 10, 1989
    Assignee: Pfizer Inc.
    Inventor: John A. Lowe, III
  • Patent number: 4749705
    Abstract: New quinazoline derivatives are disclosed, as represented by the following formula: ##STR1## wherein A is hydrogen atom or lower alkyloxy group; R.sub.4 is hydrogen atom, a lower alkyl, lower alkyloxy or a halogen atom group. Y is hydrogen atom, lower alkyloxy, sulfamoyl or Y and R.sub.4, taken together, are joined to form --O--CH.sub.2 --CH.sub.2 --O--; Z is a 4-oxopiperidino, 4-thioxopiperidino, 4-oximepiperidino, 4-O-loweralkyl-oxime-piperidino, 4-O-(3-lower alkyl-2-hydroxypropyl)-oxime-piperidino, 4-O-(3-lower alkylamino-2-hydroxypropyl)-oxime-piperidino or 4-O-(3-N'-lower alkyl, N'-benzylamino-2-hydroxypropyl)-oxime-piperidino group. These compounds are useful as anti-hypertensive agents.
    Type: Grant
    Filed: February 13, 1987
    Date of Patent: June 7, 1988
    Assignee: Kotobuki Seiyaku Co., Ltd.
    Inventors: Tsuyoshi Tomiyama, Tomoyuki Kawai, Yumiko Ichikawa
  • Patent number: 4746352
    Abstract: The disclosure is concerned with novel 3-aryluracils of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the significances given in the description, as well as salts thereof and their manufacture, weed control compositions which contain such compounds as active ingredients and the use of the active ingredients or compositions for the control of weeds. The disclosure also concerns certain herbicidally active starting materials and weed control compositions containing these as active ingredients.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: May 24, 1988
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Wenger, Paul Winternitz
  • Patent number: 4734419
    Abstract: The invention relates to compounds of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl,R.sup.3 is dihalophenyl, naphthyl(lower)alkyl, phenyl(lower)alkyl substituted by one or two substituent(s) selected from the group consisting of halogen, lower alkoxy, halo(lower)alkyl and lower alkyl, or thienyl(lower)alkyl,R.sup.4 is carboxy or protected carboxy,Y is carbonyl, thiocarbonyl or sulfonyl andZ is lower alkylene, and pharmaceutically acceptable salts thereof, useful in the treatment of diabetic complications.
    Type: Grant
    Filed: September 16, 1986
    Date of Patent: March 29, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masashi Hashimoto, Teruo Oku, Yoshikuni Ito, Takayuki Namiki, Kozo Sawada, Chiyoshi Kasahara, Yukihisa Baba
  • Patent number: 4731106
    Abstract: Compounds of the formula: ##STR1## where: A is oxygen or sulphur;R.sup.1 is phenyl or substituted phenyl in which the substituent is at least one member selected from the group consisting of halogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -haloalkoxy and nitro;R.sup.2 is 1-imidazoly of 1,2,4-triazol-1-yl; andR.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are each hydrogen, halo, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy have valuable fungicidal properties.
    Type: Grant
    Filed: March 23, 1987
    Date of Patent: March 15, 1988
    Assignee: Schering Agrochemicals Limited
    Inventors: David E. Green, Albert Percival
  • Patent number: 4716161
    Abstract: A phenylpiperazine derivative according to the present invention has the following general formula [I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or alkoxy group having 1 to 3 carbon atoms, orR.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together with carbon atoms to which they are attached form --O(CH.sub.2).sub.m O-- wherein m is an integer of 1 to 3, oreither R.sup.1 or R.sup.2 is amine residue selected from the group consisting of --NH.sub.2 , --NHSO.sub.2 CH.sub.3, --NHCOCH.sub.3 and --NHCONH.sub.2 and the other is hydrogen or alkoxy group of 1 to 3 carbon atoms and R.sup.3 is hydrogen;R.sup.4 and R.sup.5 are independently hydrogen or alkyl group of 1 to 3 carbon atoms;Y is --CO-- or --SO.sub.2 -- provided that at least one of R.sup.1 and R.sup.2 is not hydrogen when Y is --CO--; andn is an integer of 2 to 4.An acid addition salt of the phenylpiperazine derivative having the general formula [I] is included in the present invention.
    Type: Grant
    Filed: April 3, 1985
    Date of Patent: December 29, 1987
    Assignee: Mitsubishi Chemical Industries Limited
    Inventors: Harukazu Fukami, Ryoji Kikumoto, Kenichiro Nakao, Issei Nitta, Shinya Inoue
  • Patent number: 4711883
    Abstract: Novel substituted-3-(4-phenyl-1-piperazinyl)alkyl quinazolin-2,4-(1H,3H)diones are described. These compounds are useful as antihypertensive agents.
    Type: Grant
    Filed: September 30, 1985
    Date of Patent: December 8, 1987
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Victor T. Bandurco, Charles F. Schwender, Robert Falotico, Alfonso J. Tobia
  • Patent number: 4705787
    Abstract: Anti-allergic quinazolinone derivatives are disclosed which have the formula ##STR1## wherein R.sup.3 is hydrogen or lower alkyl and A is lower alkylene.
    Type: Grant
    Filed: June 2, 1986
    Date of Patent: November 10, 1987
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Ikuo Ueda, Masayuki Kato
  • Patent number: 4680296
    Abstract: Piperidine derivatives which are compounds of formula (I) ##STR1## wherein Ar.sub.1 and Ar.sub.2 independently represent a phenyl group optionally substituted by a halogen atom, a thienyl group or a pyridinyl group, A represents an alkylene group of 2 to 6 carbon atoms, X represents a CO group or a bond, R.sub.1 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, either R.sub.2 represents a hydrogen atom and R.sub.3 represents a hydrogen atom or a hydroxy group, or R.sub.2 and R.sub.3 together represent a bond, and R.sub.4 represents a hydrogen or halogen atom, or pharmaceutically acceptable acid addition salts thereof are useful as antiallergics and antipruritics.
    Type: Grant
    Filed: October 15, 1985
    Date of Patent: July 14, 1987
    Assignee: Synthelabo
    Inventors: Philippe Manoury, Jean Binet, Elisabeth Dewitte
  • Patent number: 4672116
    Abstract: Quinazoline derivatives having an oxy substituent in 5 and 6 positions are described. The novel quinazoline derivatives are useful as cardiotonic agents.
    Type: Grant
    Filed: December 20, 1985
    Date of Patent: June 9, 1987
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Victor T. Bandurco, Stanley C. Bell, John H. Dodd, Robert Falotico, Charles F. Schwender, Alfonso J. Tobia
  • Patent number: 4665075
    Abstract: Novel derivatives of hydroxy- or amino-substituted (piperidinylalkyl)quinazolines which are useful agents in the treatment of warmblooded animals suffering from diseases according to the vascular bed in which excessive serotonin release occurs.
    Type: Grant
    Filed: September 26, 1985
    Date of Patent: May 12, 1987
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Vandenberk, Ludo E. J. Kennis, Josephus C. Mertens
  • Patent number: 4652558
    Abstract: Compounds of the formula: ##STR1## wherein X is independently halogen, lower alkyl of 1 to 6 carbon atoms, lower alkoxy of 1 to 6 carbon atoms, nitro, lower alkylsulfinyl of 1 to 6 carbon atoms, lower alkylthio of 1 to 6 carbon atoms, amino or trifluoromethyl; n is 0, 1, 2 or 3; R is hydrogen, alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, lower alkenyl of 2 to 6 carbon atoms, or lower alkynyl of 2 to 6 carbon atoms, all optionally substituted with 1 to 3 of the same or different halogen atoms; or aryl of 6 to 12 carbon atoms; or substituted aryl substituted with 1 to 3 substituents independently selected from lower alkyl of 1 to 4 carbon atoms, lower alkoxy of 1 to 4 carbon atoms, and the group --S(O).sub.k R.sup.2 where k is 0, 1 or 2 and R.sup.2 is lower alkyl of 1 to 4 carbon atoms, nitro, cyano or halogen; and R.sup.1 is lower alkyl of 1 to 6 carbon atoms, lower cycloalkyl of 3 to 8 carbon atoms or aryl of 6 to 12 carbon atoms, provided that R and R.sup.
    Type: Grant
    Filed: February 27, 1986
    Date of Patent: March 24, 1987
    Assignee: Chevron Research Company
    Inventor: Laroy H. Edwards
  • Patent number: 4647563
    Abstract: Compounds of the formula ##STR1## wherein Het is ##STR2## n is an integer from 1 to 4, inclusive, preferably 2 or 3, R.sub.1 is H or acyl,R.sub.2 is H, R.sub.1 O, --NHSO.sub.2 R.sub.7, --NHCOR.sub.8, --NHCONHR.sub.8, --NH--CH.sub.2 --C.sub.6 H.sub.4 --R.sub.9, --CH.sub.2 OH, --CH.sub.2 SO.sub.2 R.sub.7, --CONHR.sub.8, halogen or --CN,R.sub.3 is H, halogen, R.sub.7 or --OR.sub.7,R.sub.2 and R.sub.3 together with each other are ##STR3## R.sub.4 is H, --CH.sub.3 or --C.sub.2 H.sub.5, R.sub.5 and R.sub.6 are each H or --CH.sub.3,R.sub.7 is C.sub.1 -C.sub.4 alkyl,R.sub.8 is H or C.sub.1 -C.sub.4 alkyl,R.sub.9 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy optionally interrupted by oxygen,R.sub.10 and R.sub.12 are each H, CH.sub.3, Cl or OCH.sub.3, or together methylenedioxy,X is ##STR4## or N, and Z is --CH.sub.2 or --CO;in the form of racemates, enantiomers, diastereoisomeric antipode pairs, and non-toxic, pharmacologically acceptable acid addition salts thereof.
    Type: Grant
    Filed: December 9, 1985
    Date of Patent: March 3, 1987
    Assignee: Boehringer Ingelheim KG
    Inventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner, Ilse Streller
  • Patent number: 4644000
    Abstract: 2-(1H-pyrazol-1-yl)-4-(3H)-quinazolinones of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and denote hydrogen, halogen, alkyl, alkoxy, hydroxyl or amino andR.sup.5 represents hydrogen or a cation,are active compounds in microbicidal agents.
    Type: Grant
    Filed: March 25, 1985
    Date of Patent: February 17, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Gauss, Hans-Joachim Kabbe, Wilfried Paulus, Hans-Jurgen Rosslenbroich, Wilhelm Brandes
  • Patent number: 4639518
    Abstract: The synthesis of 5,6-dioxy substituted quinazolinediones is described. The novel quinazolinediones are useful as cardiotonic agents.
    Type: Grant
    Filed: September 24, 1984
    Date of Patent: January 27, 1987
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Victor T. Bandurco, Stanley C. Bell, Donald W. Combs, Robert Falotico, Alfonso J. Tobia
  • Patent number: 4634769
    Abstract: A process for the preparation of 8-halo-5,6-dialkoxyquinazoline-2,4-diones and their metal salts is described. The diones are active cardiotonic agents.
    Type: Grant
    Filed: September 25, 1984
    Date of Patent: January 6, 1987
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Victor T. Bandurco, Robert A. Mallory, Jeffrey B. Press, Harvey M. Werblood
  • Patent number: 4617417
    Abstract: A process for the preparation of alkyl 2-carboxy-3,4-dialkoxybenzenecarbamates is described. The carbamates are useful intermediates in the preparation of 8-halo-5,6-dialkoxyquinazoline-2,4-diones. The diones are useful as cardiotonic agents.
    Type: Grant
    Filed: July 29, 1985
    Date of Patent: October 14, 1986
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Richard A. Conley, Donald L. Barton
  • Patent number: 4608375
    Abstract: The present invention relates to novel quinazolinone derivatives and pharmaceutically acceptable salts thereof. More particularly, it relates to novel quinazolinone derivatives and pharmaceutically acceptable salts thereof which have antiallergic activities, to processes for the preparation thereof, to pharmaceutical composition comprising the same, and to a method of using the same therapeutically in the treatment of allergic symptoms in human being and animals.
    Type: Grant
    Filed: June 21, 1984
    Date of Patent: August 26, 1986
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Ikuo Ueda, Masayuki Kato
  • Patent number: 4605657
    Abstract: Compounds of the formula: ##STR1## wherein X is independently halogen, lower alkyl of 1 to 6 carbon atoms, lower alkoxy of 1 to 6 carbon atoms, nitro, the group R.sup.1 --S(O).sub.m -- wherein R.sup.1 is lower alkyl of 1 to 6 carbon atoms and m is 0, 1 or 2, amino, or trifluoromethyl; n is 0, 1, 2 or 3; and R is alkyl of 1 to 10 carbon atoms; cycloalkyl of 3 to 8 carbon atoms; lower alkenyl of 2 to 6 carbon atoms; or lower alkynyl of 2 to 6 carbon atoms, all optionally substituted with 1 to 3 of the same or different halogen atoms, or aryl of 6 to 12 carbon atoms or substituted aryl substituted with 1 to 3 groups independently selected from lower alkyl of 1 to 4 carbon atoms, lower alkoxy of 1 to 4 carbon atoms, lower alkylthio of 1 to 4 carbon atoms, oxidized alkylthio, nitro, cyano, or halogen are fungicidal.
    Type: Grant
    Filed: April 30, 1985
    Date of Patent: August 12, 1986
    Assignee: Chevron Research Company
    Inventor: Laroy H. Edwards
  • Patent number: 4588722
    Abstract: Novel N-(4-piperidinyl) bicyclic condensed 2-imidazolamine derivatives having antihistaminic properties which compounds are useful in the treatment of allergic diseases.
    Type: Grant
    Filed: October 15, 1984
    Date of Patent: May 13, 1986
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Joseph L. G. Torremans, Jozef F. Hens, Theophilus T. J. M. Van Offenwert
  • Patent number: 4581367
    Abstract: Compounds of the formula whereinHet is a heterocycle;n is an integer from 1 to 4, inclusive, preferably 2 or 3;R.sub.1 is H or acyl;R.sub.2 is H, R.sub.1 O, --NHSO.sub.2 R.sub.7, --NHCOR.sub.8, --NHCONHR.sub.8, --NH--CH.sub.2 --C.sub.6 H.sub.4 --R.sub.9, --CH.sub.2 OH, --CH.sub.2 SO.sub.2 R.sub.7, --CONHR.sub.8, halogen or --CN;R.sub.3 is H, halogen, R.sub.7 or --OR.sub.7 ; orR.sub.2 and R.sub.3, together with each other, are ##STR1## N.sub.4 is H, --CH.sub.3 or --C.sub.2 H.sub.5 ; R.sub.5 and R.sub.6 are each H or --CH.sub.3 ;R.sub.7 is C.sub.1 -C.sub.4 alkyl;R.sub.8 is H or C.sub.1 -C.sub.4 alkyl; andR.sub.9 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy optionally interrupted by oxygen;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as bronchospasmolytics, spasmolytics, muscle-relaxants, antiallergics and hypotensives.
    Type: Grant
    Filed: November 23, 1982
    Date of Patent: April 8, 1986
    Assignee: Boehringer Ingelheim KG
    Inventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner, Ilse Streller
  • Patent number: 4578465
    Abstract: Phenylpiperazine derivatives of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a straight- or branched-chain saturated or unsaturated alkyl group having 1 to 8 carbon atoms which may be substituted at any position by a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group or an oxo group; and R.sub.2 is a hydrogen atom, a halogen atom, a lower alkyl group or a sulfamoyl group, and a process for producing the same are disclosed. The derivatives of the formula have alpha blocking and serotonin antagonizing activities and are useful as a drug.
    Type: Grant
    Filed: April 30, 1984
    Date of Patent: March 25, 1986
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroyuki Nagano, Mitiro Takagi, Noboru Kubodera, Isao Matsunaga, Hiroyuki Nabata, Yasuhiro Ohba, Kazushige Sakai, Shun-ichi Hata, Yasumi Uchida
  • Patent number: 4576941
    Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.
    Type: Grant
    Filed: February 29, 1984
    Date of Patent: March 18, 1986
    Assignee: USV Pharmaceutical Corp.
    Inventors: John T. Suh, John J. Piwinski, Howard Jones, Edward S. Neiss
  • Patent number: 4551458
    Abstract: There are provided novel haloalkylthio-1,3-dihydro 2,4-dioxo-quinazolines having at least one haloalkylthio substituent in the 1- or 3-position; a process for the preparation of such compounds and fungicidal compositions containing same as active ingredient.
    Type: Grant
    Filed: April 11, 1983
    Date of Patent: November 5, 1985
    Assignee: Makhteshim Chemical Works, Ltd.
    Inventors: Peretz Bracha, Solomon Massil
  • Patent number: 4522945
    Abstract: Novel quinazoline derivatives, comprising in the heterocyclic part of their quinazoline nucleus at least one carbonyl or thiocarbonyl group and a particularly substituted piperidinyl-alkyl side chain, said compounds being potent serotonin-antagonists.
    Type: Grant
    Filed: March 26, 1982
    Date of Patent: June 11, 1985
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jan Vandenberk, Ludo Kennis, Marcel Van der Aa, Albert Van Heertum