Chalcogen Bonded Directly At 2- And 4-positions Patents (Class 544/285)
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Patent number: 5017298Abstract: 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: GrantFiled: March 12, 1990Date of Patent: May 21, 1991Assignee: BP Chemicals LimitedInventor: Sean P. O'Connor
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Patent number: 5017211Abstract: 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: GrantFiled: May 19, 1989Date of Patent: May 21, 1991Assignee: Ciba-Geigy CorporationInventors: Jean Wenger, Paul Winternitz, Martin Zeller
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Patent number: 5008266Abstract: 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: GrantFiled: July 26, 1989Date of Patent: April 16, 1991Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Tatsuo Horaguchi, Koichi Nakamaru, Yoshikuni Suzuki
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Patent number: 4992550Abstract: 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: GrantFiled: April 6, 1989Date of Patent: February 12, 1991Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4988809Abstract: 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: GrantFiled: February 21, 1990Date of Patent: January 29, 1991Assignee: Troponwerke GmbH & Co., KGInventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, THomas Glaser, Teunis Schuurmann
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Patent number: 4985441Abstract: 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: GrantFiled: April 3, 1990Date of Patent: January 15, 1991Assignees: Imperial Chemical Industries plc, National Research Development Corp.Inventors: Leslie R. Hughes, John Oldfield, Stephen J. Pegg
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Patent number: 4985171Abstract: 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: GrantFiled: January 2, 1990Date of Patent: January 15, 1991Assignee: Mitsubishi Chemical Industries LimitedInventors: Konoe Miura, Tetsuo Ozawa, Junko Kanaya
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Patent number: 4981856Abstract: 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: GrantFiled: April 12, 1990Date of Patent: January 1, 1991Assignee: Imperial Chemical Industries PLCInventor: Leslie R. Hughes
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Patent number: 4963550Abstract: 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: GrantFiled: February 7, 1990Date of Patent: October 16, 1990Assignee: Ciba-Geigy CorporationInventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund, Odd Kristiansen
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Patent number: 4942169Abstract: 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: GrantFiled: March 10, 1989Date of Patent: July 17, 1990Assignee: 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
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Patent number: 4937343Abstract: 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: GrantFiled: September 22, 1988Date of Patent: June 26, 1990Assignee: Troponwerke GmbH & Co. KGInventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
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Patent number: 4920224Abstract: 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: GrantFiled: March 13, 1989Date of Patent: April 24, 1990Assignee: Pfizer Inc.Inventor: Edward A. Glazer
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Patent number: 4914098Abstract: 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: GrantFiled: August 12, 1987Date of Patent: April 3, 1990Assignee: Ciba-Geigy CorporationInventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund, Odd Kristiansen
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Patent number: 4908365Abstract: 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: GrantFiled: July 7, 1987Date of Patent: March 13, 1990Inventors: Andre Buzas, Jean-Yves Merour, Roland Ollivier
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Patent number: 4888426Abstract: 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: GrantFiled: June 1, 1987Date of Patent: December 19, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Joseph L. G. Torremans, Jozef F. Hens
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Patent number: 4883800Abstract: 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: GrantFiled: December 8, 1987Date of Patent: November 28, 1989Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masashi Hashimoto, Teruo Oku, Yoshikuni Ito, Takayuki Namiki, Kozo Sawada, Chiyoshi Kasahara, Yukihisa Baba
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Patent number: 4861780Abstract: 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: GrantFiled: January 26, 1988Date of Patent: August 29, 1989Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Tatsuo Horaguchi, Koichi Nakamaru, Yoshikuni Suzuki
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Patent number: 4854965Abstract: 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: GrantFiled: June 22, 1987Date of Patent: August 8, 1989Assignee: Makhteshim Chemical Works, Ltd.Inventors: Peretz Bracha, Moshe Korat
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Patent number: 4849518Abstract: 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: GrantFiled: March 24, 1988Date of Patent: July 18, 1989Assignee: Pfizer Inc.Inventor: Edward A. Glazer
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Patent number: 4849431Abstract: 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: GrantFiled: December 24, 1986Date of Patent: July 18, 1989Assignee: 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
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Patent number: 4833144Abstract: 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: GrantFiled: January 26, 1988Date of Patent: May 23, 1989Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Tatsuo Horaguchi, Koichi Nakamaru, Yoshikuni Suzuki
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Patent number: 4831161Abstract: Prepare N-(amidoalkyl)imides by contacting an imide with a 2-oxazoline under reaction conditions, optionally in the presence of a solvent.Type: GrantFiled: June 24, 1987Date of Patent: May 16, 1989Assignee: The Dow Chemical CompanyInventors: Pen-Chung Wang, Steven P. Crain
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Patent number: 4824469Abstract: 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: GrantFiled: March 11, 1988Date of Patent: April 25, 1989Assignee: Schering Agrochemicals Ltd.Inventors: David E. Green, Albert Percival
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Patent number: 4818756Abstract: 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: GrantFiled: March 10, 1986Date of Patent: April 4, 1989Assignee: Troponwerke GmbH & Co., KGInventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
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Patent number: 4812164Abstract: 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: GrantFiled: September 15, 1987Date of Patent: March 14, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Jean Wenger, Paul Winternitz
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Patent number: 4797403Abstract: 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: GrantFiled: July 23, 1987Date of Patent: January 10, 1989Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Patent number: 4749705Abstract: 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: GrantFiled: February 13, 1987Date of Patent: June 7, 1988Assignee: Kotobuki Seiyaku Co., Ltd.Inventors: Tsuyoshi Tomiyama, Tomoyuki Kawai, Yumiko Ichikawa
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Patent number: 4746352Abstract: 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: GrantFiled: March 10, 1986Date of Patent: May 24, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Jean Wenger, Paul Winternitz
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Patent number: 4734419Abstract: 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: GrantFiled: September 16, 1986Date of Patent: March 29, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masashi Hashimoto, Teruo Oku, Yoshikuni Ito, Takayuki Namiki, Kozo Sawada, Chiyoshi Kasahara, Yukihisa Baba
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Patent number: 4731106Abstract: 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: GrantFiled: March 23, 1987Date of Patent: March 15, 1988Assignee: Schering Agrochemicals LimitedInventors: David E. Green, Albert Percival
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Patent number: 4716161Abstract: 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: GrantFiled: April 3, 1985Date of Patent: December 29, 1987Assignee: Mitsubishi Chemical Industries LimitedInventors: Harukazu Fukami, Ryoji Kikumoto, Kenichiro Nakao, Issei Nitta, Shinya Inoue
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Patent number: 4711883Abstract: Novel substituted-3-(4-phenyl-1-piperazinyl)alkyl quinazolin-2,4-(1H,3H)diones are described. These compounds are useful as antihypertensive agents.Type: GrantFiled: September 30, 1985Date of Patent: December 8, 1987Assignee: Ortho Pharmaceutical CorporationInventors: Victor T. Bandurco, Charles F. Schwender, Robert Falotico, Alfonso J. Tobia
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Patent number: 4705787Abstract: 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: GrantFiled: June 2, 1986Date of Patent: November 10, 1987Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato
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Patent number: 4680296Abstract: 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: GrantFiled: October 15, 1985Date of Patent: July 14, 1987Assignee: SynthelaboInventors: Philippe Manoury, Jean Binet, Elisabeth Dewitte
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Patent number: 4672116Abstract: Quinazoline derivatives having an oxy substituent in 5 and 6 positions are described. The novel quinazoline derivatives are useful as cardiotonic agents.Type: GrantFiled: December 20, 1985Date of Patent: June 9, 1987Assignee: Ortho Pharmaceutical CorporationInventors: Victor T. Bandurco, Stanley C. Bell, John H. Dodd, Robert Falotico, Charles F. Schwender, Alfonso J. Tobia
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Patent number: 4665075Abstract: 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: GrantFiled: September 26, 1985Date of Patent: May 12, 1987Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Vandenberk, Ludo E. J. Kennis, Josephus C. Mertens
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Patent number: 4652558Abstract: 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: GrantFiled: February 27, 1986Date of Patent: March 24, 1987Assignee: Chevron Research CompanyInventor: Laroy H. Edwards
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Patent number: 4647563Abstract: 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: GrantFiled: December 9, 1985Date of Patent: March 3, 1987Assignee: Boehringer Ingelheim KGInventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner, Ilse Streller
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Patent number: 4644000Abstract: 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: GrantFiled: March 25, 1985Date of Patent: February 17, 1987Assignee: Bayer AktiengesellschaftInventors: Walter Gauss, Hans-Joachim Kabbe, Wilfried Paulus, Hans-Jurgen Rosslenbroich, Wilhelm Brandes
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Patent number: 4639518Abstract: The synthesis of 5,6-dioxy substituted quinazolinediones is described. The novel quinazolinediones are useful as cardiotonic agents.Type: GrantFiled: September 24, 1984Date of Patent: January 27, 1987Assignee: Ortho Pharmaceutical CorporationInventors: Victor T. Bandurco, Stanley C. Bell, Donald W. Combs, Robert Falotico, Alfonso J. Tobia
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Patent number: 4634769Abstract: 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: GrantFiled: September 25, 1984Date of Patent: January 6, 1987Assignee: Ortho Pharmaceutical CorporationInventors: Victor T. Bandurco, Robert A. Mallory, Jeffrey B. Press, Harvey M. Werblood
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Patent number: 4617417Abstract: 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: GrantFiled: July 29, 1985Date of Patent: October 14, 1986Assignee: Ortho Pharmaceutical CorporationInventors: Richard A. Conley, Donald L. Barton
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Patent number: 4608375Abstract: 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: GrantFiled: June 21, 1984Date of Patent: August 26, 1986Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masayuki Kato
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Patent number: 4605657Abstract: 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: GrantFiled: April 30, 1985Date of Patent: August 12, 1986Assignee: Chevron Research CompanyInventor: Laroy H. Edwards
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Patent number: 4588722Abstract: Novel N-(4-piperidinyl) bicyclic condensed 2-imidazolamine derivatives having antihistaminic properties which compounds are useful in the treatment of allergic diseases.Type: GrantFiled: October 15, 1984Date of Patent: May 13, 1986Assignee: Janssen Pharmaceutica N.V.Inventors: Frans E. Janssens, Joseph L. G. Torremans, Jozef F. Hens, Theophilus T. J. M. Van Offenwert
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Patent number: 4581367Abstract: 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: GrantFiled: November 23, 1982Date of Patent: April 8, 1986Assignee: Boehringer Ingelheim KGInventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner, Ilse Streller
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Patent number: 4578465Abstract: 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: GrantFiled: April 30, 1984Date of Patent: March 25, 1986Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroyuki Nagano, Mitiro Takagi, Noboru Kubodera, Isao Matsunaga, Hiroyuki Nabata, Yasuhiro Ohba, Kazushige Sakai, Shun-ichi Hata, Yasumi Uchida
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Patent number: 4576941Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.Type: GrantFiled: February 29, 1984Date of Patent: March 18, 1986Assignee: USV Pharmaceutical Corp.Inventors: John T. Suh, John J. Piwinski, Howard Jones, Edward S. Neiss
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Patent number: 4551458Abstract: 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: GrantFiled: April 11, 1983Date of Patent: November 5, 1985Assignee: Makhteshim Chemical Works, Ltd.Inventors: Peretz Bracha, Solomon Massil
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Patent number: 4522945Abstract: 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: GrantFiled: March 26, 1982Date of Patent: June 11, 1985Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Vandenberk, Ludo Kennis, Marcel Van der Aa, Albert Van Heertum