1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 548/136)
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Patent number: 4906628Abstract: Phosphodiesterase (type III) inhibitors having the formula: ##STR1## which are useful in stimulating cardiac activity and in treating congestive heart failure and bronchoconstriction, pharmaceutical compositions including these inhibitors, and methods of using these compounds to produce phosphodiesterase (type III) inhibition in mammals.Type: GrantFiled: October 14, 1986Date of Patent: March 6, 1990Assignee: Smith Kline & French Laboratories LimitedInventor: William J. Coates
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Patent number: 4904660Abstract: Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful medical agents, in particular, anti-hypertensive agents.Type: GrantFiled: February 25, 1988Date of Patent: February 27, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kohji Nakano, Takashi Fujikura, Ryuichiro Hara, Masato Ichihara, Yukiko Fukunaga, Masayuki Shibasaki
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Patent number: 4892899Abstract: Composition of matter containing(a) a compound of the formula I ##STR1## in which A is one of the groups of the formulae ##STR2## in which B is --O--, --S--, --SO.sub.2 --, --N.dbd.N--, --CH.sub.2 --, --CH.dbd.CH--, ##STR3## --CONH--, --NHCONH--, or --CONHNHCO--, Q is --O-- or --NH-- and Z is --O-- or --S-- and R and R' are independently of each other hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or phenoxy, and(b) a compound of the formula II ##STR4## in which A' is as defined above for A, D is hydrogen, amino or a group of the formula III ##STR5## E is --O-- or --S--, T.sub.1, T.sub.2 and T.sub.3 independently of one another are chlorine or a group --ET', T' is a group of the formulae ##STR6## X.sup..sym. is H.sup..sym. or a group of the formulae M.sup.n.sym. /n or N.sup..beta. (R.sub.1)(R.sub.2)(R.sub.3)(R.sub.4), Mhu n.sym. is an n-valent metal cation, n is 1, 2 or 3, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently of one another hydrogen, C.sub.1 -C.sub.18 -alkyl, C.sub.Type: GrantFiled: December 8, 1987Date of Patent: January 9, 1990Assignee: Ciba-Geigy CorporationInventors: Edward E. Jaffe, Jost von der Crone, Bernhard Medinger
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Patent number: 4888348Abstract: The invention relates to novel substituted phenylthioureas, phenylisothioureas and phenylcarbodiimides of formula I ##STR1## wherein Z is ##STR2## or --N.dbd.C.dbd.N--; R.sub.1 is C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.10 alkenyl, C.sub.3 -C.sub.10 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.3 alkyl substituted by 1 or 2 C.sub.3 -C.sub.6 cycloalkyl radicals, or is alkoxyalkyl containing a total of 3 to 10 carbon atoms, halogen-substituted C.sub.1 -C.sub.12 alkyl, polycyclic C.sub.7 -C.sub.10 cycloalkyl, or phenyl(C.sub.1 -C.sub.5)alkyl which may be substituted in the phenyl moiety by 1 or 2 identical or different members selected from the group consisting of halogen, methoxy, ethoxy and C.sub.1 -C.sub.5 alkyl,R.sub.2 is hydrogen or C.sub.1 -C.sub.5 alkyl,R.sub.3 is C.sub.1 -C.sub.5 alkyl or C.sub.3 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.Type: GrantFiled: August 28, 1987Date of Patent: December 19, 1989Assignee: Ciba-Geigy CorporationInventors: Josef Ehrenfreund, Manfred Boger, Odd Kristiansen, Jozef Drabek, Haukur Kristinsson
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Patent number: 4882342Abstract: The present invention concerns new 5-alkylbenzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl ring of the formula: ##STR2## or R.sub.1 is naphthyl, heterocycle or a bicyclic heterocycle and R.sub.1 -R.sub.7 are described in claim 1.These compounds are useful for prophylaxis or treatment of heart and circulatory disease especially to increase contractility of the heart, lower blood pressure and/or influence the thrombocyte function and improve the microcirculation.Type: GrantFiled: October 6, 1987Date of Patent: November 21, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Jens-Peter Holck, Alfred Mertens, Bernd Muller-Beckmann, Lothar Kling
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Patent number: 4874544Abstract: Fast-switching displays with memory properties are provided, which can display digits, symbols, and images, and which contain as chemically and thermally stable ferroelectric liquid crystalline substances, according to the invention, liquid crystalline derivatives which contain a chiral alkyl halide residue corresponding to the general formula ##STR1## are used in mixtures of one another as well as in conjunction with other liquid crystalline or non-crystalline liquid substances.Type: GrantFiled: February 3, 1988Date of Patent: October 17, 1989Assignee: VEB Werk fuer Fernsehelektronik im VEB Kombinat MikroelektronikInventors: Bak G. Yong, Barth Petra, Demus Dietrich, Joachimi Detlev, Barbara Kampa, Saskia Kohler, Kristine Mohr, Reinhard Paschke, Gerhard Pelzl, Ulrich Rosenfeld, Wolfgang Schafer, Klaus-Dieter Scherf, Carsten Tschirske, Wolfgang Weissflog, Horst Zaschke
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Patent number: 4871719Abstract: Novel 13-spiro-2'-[tetrahydrofuran]-milbemycins of the formula I ##STR1## in which X represents one of the groups --CH(OR.sub.1)--, --C(.dbd.O)-- or --C(.dbd.N--OH)--;R.sub.1 represents hydrogen or a OH-protecting group;R.sub.2 represents methyl, ethyl, isopropyl or sec.-butyl or the group --C(CH.sub.3).dbd.CH--A in which A represents methyl, ethyl or isopropyl; andR.sub.3 represents hydrogen; C.sub.1 -C.sub.10 -alkyl; C.sub.1 -C.sub.10 -alkyl substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkoxyalkoxy C.sub.3 -C.sub.9 -alkoxyalkoxyalkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.3 -alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, benzyloxy, C.sub.1 -C.sub.6 -acyl and C.sub.1 -C.sub.6 -acyloxy, it being possible for each of the above-mentioned radicals representing or containing an alkoxy group to be terminally substituted at a terminal alkoxy group by hydroxy, halogen, C.sub.1 -C.sub.Type: GrantFiled: March 16, 1988Date of Patent: October 3, 1989Assignee: Ciba-Geigy CorporationInventor: Peter Maienfisch
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Patent number: 4863945Abstract: Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.Type: GrantFiled: December 10, 1987Date of Patent: September 5, 1989Assignee: Boehringer Mannheim GmbHInventors: Walter-Gunar Friebe, Alfred Mertens, Klaus Strein, Erwin Boehm
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Patent number: 4861788Abstract: Compounds of formula (I): ##STR1## wherein ##STR2## is a 5-membered heterocyclic group having a 6-.pi.electron system, the five ring atoms being either(a) one carbon atom and four atoms selected from carbon and nitrogen,(b) two carbon atoms, two nitrogen atoms and one atom selected from oxygen and sulphur, or(c) four carbon atoms and one atom selected from oxygen and sulphurand R.sup.1 is a substituent on a carbon or nitrogen of ##STR3## selected from C.sub.1-20 alkyl, C.sub.2-8 alkenyl aryl, aralkyl and heterocyclyl, each of which may optionally be substituted; hydrogen and C.sub.3-7 cycloalkyl,and, where appropriate, R.sup.2 is a substituent on a carbon or nitrogen of ##STR4## and when present is the same or different to R.sup.1 and is selected from C.sub.1-20 alkyl, C.sub.2-8 alkenyl, aryl, aralkyl and heterocyclyl each of which may optionally be substituted; hydrogen and C.sub.3-7 cycloalkyl, have antibacterial and antimycoplasmal activity.Type: GrantFiled: January 30, 1987Date of Patent: August 29, 1989Assignee: Beecham Group plcInventors: Norman H. Rogers, Graham Walker, Michael J. Crimmin, Peter J. O'Hanlon
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Patent number: 4861787Abstract: Novel compounds of the formula ##STR1## in which R' represents C.sub.1 -C.sub.5 -alkyl, halogen, trifluoromethyl or C.sub.1 -C.sub.3 -alkoxy;R" represents C.sub.1 -C.sub.5 -alkyl or halogen; andR"' represents C.sub.1 -C.sub.5 -alkyl that is unsubstituted or is substituted by from 1 to 6 halogen atoms, C.sub.1 -C.sub.5 -alkenyl that is unsubstituted or is substituted by from 1 to 6 halogen atoms, or C.sub.1 -C.sub.5 - alkynyl that is unsubstituted or is substituted by from 1 to 6 halogen atoms;m represents 0, 1, 2 or 3 andn represents 0 or 1; andX.sub.1 and X.sub.2 each represents, independently of the other, oxygen or sulphur,as active ingredients for controlling plant parasite nematodes and for preventing damage to cultivated plants caused by nematode attack.Type: GrantFiled: October 25, 1988Date of Patent: August 29, 1989Assignee: Ciba-Geigy CorporationInventors: Ernst Beriger, Wolfgang Eckhardt, Robert Nyfeler
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Patent number: 4855441Abstract: 5-pyrazolone compounds which are substituted with a thioether group in the 4-position may be prepared by the reaction of a 5-pyrazolone compound which is unsubstituted in the 4-position with a sulphenic acid amide. The resulting 5-pyrazolone compounds substituted in the 4-position are suitable for use as 2-equivalent magenta couplers in color photographic recording materials.Type: GrantFiled: December 14, 1987Date of Patent: August 8, 1989Assignee: Agfa-Gevaert AktiengesellschaftInventors: Gunter Renner, Erich Illner
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Patent number: 4855310Abstract: Novel heterocyclic compounds shown by the general formula ##STR1## or the pharmaceutically acceptable salts thereof useful as medicament in particular as antagonist of slow reacting substance of anaphylaxis (SRS-A).Type: GrantFiled: March 25, 1988Date of Patent: August 8, 1989Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Murase, Toshiyasu Mase, Hiromu Hara, Kenichi Tomioka
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Patent number: 4851406Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.Type: GrantFiled: September 4, 1986Date of Patent: July 25, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Walter-Gunar Friebe, Bernd Muller-Beckmann, Gisbert Sponer
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Patent number: 4851422Abstract: The compound represented by the formula: ##STR1## where R.sup.1 stands for amino or an organic residue bonded through nitrogen; R.sup.2 stands for carboxyl or a group derivable therefrom; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently stand for hydrogen or an organic residue, including the case where R.sup.5 or R.sup.6 forms a chemical bond or a ring with R.sup.7 or R.sup.8 ; X stands for hydrogen, methoxy or formylamino; or a salt thereof, produceable by the present method, exhibits excellent antimicrobial activity, and is utilized as antimicrobial agents.Type: GrantFiled: April 30, 1986Date of Patent: July 25, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Yasuhiko Kawano, Akira Morimoto, Kouichi Yoshioka
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Patent number: 4849432Abstract: Novel heterocyclic compounds of the formula ##STR1## wherein, R.sup.1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group ##STR2## in which R.sup.2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R.sup.3 represents a hydrogen atom or an alkyl group, and Z represents an optionally sibstituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group.The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 24, 1987Date of Patent: July 18, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hattori
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Lubricant additives derived from aminomercaptothiadiazole and lubricant compositions containing same
Patent number: 4846984Abstract: Disclosed herein is the reaction product of 5-amino-2-mercapto-1,3,4-thiadiazole with hydrocarbyl epoxides. The resulting reaction product finds use as an additive in lubricating oil compositions.Type: GrantFiled: May 2, 1988Date of Patent: July 11, 1989Assignee: Mobil Oil CorporationInventors: Angeline B. Cardis, Robert H. Davis, Alfred B. Piotrowski -
Patent number: 4835272Abstract: A process for formation of a base, which comprises reacting an acetylide compound with a salt. The acetylide compound has the following formula:(R--C.tbd.C--).sub.n Mwherein R is a monovalent group selected from the group consisting of an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aralkyl group, an aryl group and a heterocyclic group, each of which may have one or more substituent groups; M is an n-valent transition metal atom; and n is 1, 2 or 3. The salt is composed of an anion having an affinity for the transition metal (M) (the affinity of the anion for the transition metal is more than that of the acetylide anion (R--C.tbd.C.crclbar.)), and a cation derived from one selected from the group consisting of an alkali metal, an alkaline earth metal, ammonia and an organic base. A light-sensitive material containing the acetylide compound and the salt is also disclosed.Type: GrantFiled: July 16, 1987Date of Patent: May 30, 1989Assignee: Fuji Photo Film Co., Ltd.Inventors: Kozo Sato, Shunichi Ishikawa, Ken Kawata
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Patent number: 4833252Abstract: Substituted N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N'-triazinylureas of the general formula ##STR1## and the salts thereof with amines, alkali metal bases or alkaline earth metal bases, or with quaternary ammonium bases, have good pre- and postemergence selective herbicidal and growth regulating properties.In the above formula the symbols have the following meanings:R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkylsulfinyl, --CO--R.sup.8, --NR.sup.9 R.sup.10, --CO--NR.sup.11 R.sup.12 or --SO.sub.2 --NR.sup.13 R.sup.14,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl or C.sub.1 -C.sub.4 alkylsulfonyl,R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl or cyano,R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sup.5 is hydrogen, C.sub.Type: GrantFiled: September 28, 1988Date of Patent: May 23, 1989Assignee: Ciba-Geigy CorporationInventors: Werner Topfl, Georg Pissiotas
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Patent number: 4826992Abstract: 2,3-(Dihydro) bicyclic pyrazolidinones are intermediates for bicyclic pyrazolidinone antimicrobials.Type: GrantFiled: November 24, 1986Date of Patent: May 2, 1989Assignee: Eli Lilly and CompanyInventors: Louis N. Jungheim, Sandra K. Sigmund
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Patent number: 4824843Abstract: Novel N-(substituted-phenyl)-5-(2,5-dimethylphenoxy)-2,2-dimethylpentanamides which are useful in preventing the intestinal absorption of cholesterol, as well as novel pharmaceutical compositions and methods of use, as well as processes for their manufacture are herein described.Type: GrantFiled: June 25, 1987Date of Patent: April 25, 1989Assignee: Warner-Lambert CompanyInventors: Milton L. Hoefle, Robert F. Meyer
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Patent number: 4803211Abstract: This invention relates to novel heterocyclic compounds structurally characterized by containing a specific heterocyclic group and by the presence of --CH.sub.2 --S-- directly bound to the specific heterocyclic group. These heterocyclic compounds are useful as medicines, particularly as antagonists of SRS-A (slow reacting substance of anaphylaxis).Type: GrantFiled: July 14, 1986Date of Patent: February 7, 1989Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Ryuji Tsuzuki, Hiromu Hara, Kiyoshi Murase, Kenichi Tomioka
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Patent number: 4791208Abstract: 5-Halogenoalkyl-1,3,4-thiadiazol-2-yloxyacetamides of the formula ##STR1## in which R.sup.1 is halogenoalkyl, with the exception of trifluoromethyl, andR.sup.2 and R.sup.3 each independently is hydrogen, alkyl, alkenyl, alkinyl, in each case optionally substituted cycloalkyl or cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxyalkylenoxy, alkoxy, aralkyl or optionally substituted aryl, orR.sup.2 and R.sup.3, together with the nitrogen atom to which they are bonded, form an optionally substituted heterocyclic radical which can contain further hetero-atoms,which possess herbicidal and fungicidal activity. The intermediates 5-chlorodifluoromethyl- and 5-dichlorofluoromethyl-2-chloro-1,3,4- thiadiazole are also new.Type: GrantFiled: August 7, 1987Date of Patent: December 13, 1988Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Hans-Joachim Diehr, Fritz Maurer, Erich Klauke, Ludwig Eue, Hans-Joachim Santel, Robert R. Schmidt, Paul Reinecke, Gerd Hanssler
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Patent number: 4782169Abstract: Compounds of the Formula I, II, III, VI and VII ##STR1## wherein the symbols have defined meanings are herbicides, plant growth regulators or intermediates thereof.Type: GrantFiled: October 6, 1986Date of Patent: November 1, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Samuel B. Soloway, Pierre Vogel, Claude H. Aubin Le Drian, James E. Powell
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Patent number: 4782083Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.Type: GrantFiled: August 29, 1986Date of Patent: November 1, 1988Assignee: Beecham Group P.L.C.Inventors: Frederick Cassidy, Geoffrey Stemp, John M. Evans
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Patent number: 4782072Abstract: 2-Aminomethyl-5-(2-biphenylyl)-1,3,4-thiadiazole and is non-toxic salts.Processes for the preparation and pharmaceutical compositions thereof. The compound exhibits anticonvulsant activity and is indicated for the use in the treatment of epilepsy.Type: GrantFiled: October 27, 1987Date of Patent: November 1, 1988Assignee: Reckitt & Colman Products LimitedInventor: Michael R. Stillings
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Patent number: 4780405Abstract: Nucleic acid hybridization probes are provided which comprise nucleoside bases or terminal nucleotide phosphates chemically linked to aromatic sulfonamide inhibitors of carbonic anhydrase. Methods of preparing probes of the invention, intermediates used in such methods, and methods of using the probes of the invention in hybridization assays are also provided. A probe of the invention is detected by binding to it a reporter group, such as a homopolymer or heteropolymer of enzymes, which includes a carbonic anhydrase which binds to the inhibitor linked to the probe, and then detecting the bound reporter group, as by production of a fluorescent or colored product in a reaction catalyzed by an enzyme component of the reporter group. Also provided are enzyme immunoassays wherein detection of antibody is by a process which comprises a chemical reaction catalyzed by a carbonic anhydrase.Type: GrantFiled: July 9, 1985Date of Patent: October 25, 1988Assignee: Siska Diagnostics, Inc.Inventors: Emil T. Kaiser, Gary F. Musso, Soumitra Ghosh, Leslie E. Orgel, Geoffrey M. Wahl
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Patent number: 4775406Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.Type: GrantFiled: November 21, 1985Date of Patent: October 4, 1988Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
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Patent number: 4774240Abstract: The invention relates to N-indolylethyl-sulphonic acid amides of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are defined in the specification and X is carboxyl, alkoxycarbonyl, cyano or carboxamido. These active compounds are useful in medicaments in combating thromboses, thromboembolisms, allergies or asthmatic disorders.Type: GrantFiled: April 14, 1986Date of Patent: September 27, 1988Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Ulrich Rosentreter, Folker Lieb, Hermann Oediger, Friedel Seuter, Elisabeth Perzborn, Volker-Bernd Fiedler
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Patent number: 4772309Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.Type: GrantFiled: March 19, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Substituted pyrazolin-5-ones, composition containing them, and method of combating fungi or bacteria
Patent number: 4767775Abstract: Microbicidal substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an optionally substituted heterocyclic radical.Intermediates therefor of the formula ##STR2## in which R is alkyl, are also disclosed.Type: GrantFiled: July 24, 1986Date of Patent: August 30, 1988Assignee: Bayer AktiengesellschaftInventors: Klaus Jelich, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke -
Patent number: 4762848Abstract: Heterocyclic sulfides of the general formula heterocycle-S-R, a process for their preparation and, in particular, their use for immunostimulation, immunorestoration and cytostatic treatment, and pharmaceutical agents, which contain a sulfide of this type, for these indications.Type: GrantFiled: March 10, 1986Date of Patent: August 9, 1988Assignee: Hoechst AktiengesellschaftInventors: Karl-Heinz Scheunemann, Walter Durckheimer, Jurgen Blumbach, Michael Limbert, Hans-Ulrich Schorlemmer, Gerhard Dickneite, Hans-Harald Sedlacek
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Patent number: 4756741Abstract: Azolyloxy-carboxylic acid amides of the formula ##STR1## wherein R is a five-membered hetero-aromatic monocyclic radical which contains an oxygen atom or a sulfur atom and 1 to 3 nitrogen atoms; orR is said monocyclic radical substituted by halogen, nitro, cyano, amino, alkylamino, dialkylamino, arylamino, alkylcarbonylamino, alkylcarbonyl, carboxyl, alkoxycarbonyl, carbamoyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl substituted arylaminocarbonyl wherein the substituents are halogen, nitro or alkyl, aryl, substituted aryl wherein the substituents are halogen, nitro, cyano, alkyl, halogenoalkyl or alkoxy, aralkyl, haloaralkyl, alkoxy, halo-alkoxy, alkenoxy, alkynoxy, alkoxycarbonylalkoxy, aralkoxy or aryloxy, optionally halogen-substituted alkylthio, alkenylthio, alkynylthio, alkoxycarbonylalkylthio, aralkylthio, arylthio, alkylsulphinyl or alkylsulphonyl, optionally halogen-substituted alkyl, alkenyl, alkynyl, alkoxyalkyl, aralkoxyalkyl, aryloxyalkyl, alkylthioalkyl, alkylsulphinylalkyl, alType: GrantFiled: January 15, 1986Date of Patent: July 12, 1988Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Wolfgang Hofer, Volker Mues, Ludwig Eue, Robert R. Schmidt
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Patent number: 4748165Abstract: This invention relates to amidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 is hydrogen or a 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl radical, the latter three being optionally substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; and R.sup.2 and R.sup.3 are a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.Type: GrantFiled: May 11, 1982Date of Patent: May 31, 1988Assignee: Imperial Chemical Industries PLCInventors: Derrick F. Jones, Keith Oldham
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Patent number: 4746669Abstract: Thiazole derivatives have been made, for example, by reacting a 2-aryl-2,2-dialkoxyethylamine with an appropriately substituted aryl acetyl halide followed by treating the resulting amide with diphosphoryl pentasulfide. The thiazole derivatives are found to be effective immunoregulants.Type: GrantFiled: March 26, 1987Date of Patent: May 24, 1988Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Ihor Kopka, Milton L. Hammond, Robert A. Zambias
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Patent number: 4742060Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4739083Abstract: A new process for preparing a pyrone-3-carboxamide compound of the formula (IV): ##STR1## wherein R.sub.1 is aryl or heterocyclic group optionally substituted, R.sub.2 is alkyl, aralkyl or like group, comprising reacting a compound of the formula (I) or (I'): ##STR2## wherein R.sub.3 is dialkylamino group and n is 0 to 6, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II): ##STR3## wherein R.sub.4 and R.sub.5 are hydrogen atom, alkyl or like group, or reacting a compound of the formula (III): ##STR4## wherein R.sub.6 is alkyl, aryl or like group, and R.sub.1 and R.sub.2 are as above,with a compound of the formula (II) or diketene in the presence of a tertiary organic base.Type: GrantFiled: January 2, 1986Date of Patent: April 19, 1988Assignee: Daicel Chemical Industries Ltd.Inventors: Yoichiro Ueda, Yukihisa Goto, Kazuhisa Masamoto
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Patent number: 4735955Abstract: Derivatives of 2-substituted-cycloheptoimidazole are disclosed, which are represented by the following formula: ##STR1## wherein R is a hydrogen atom, a lower-alkyl, acetyl, lower-alkylaminoalkyl or ethylenedioxyethyl group. A represents a phenyl, pyridyl, benzimidazolyl, imidazolyl, thiazolyl, thiadiazolyl, oxazolyl or isoxazolyl group; each of which optionally possesses one substituent or more and m is 0 or 1, and n is 1 or 2. These compounds are useful as anti-ulcerative agents.Type: GrantFiled: February 6, 1986Date of Patent: April 5, 1988Assignee: Kotobuki Seiyaku Co., Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama
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Patent number: 4734504Abstract: 1-Alkylated diazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds. The instant compounds have the formula ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3, have the meanings as defined in the specification.Type: GrantFiled: May 14, 1986Date of Patent: March 29, 1988Assignee: Eli Lilly and CompanyInventor: Richard E. Holmes
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Patent number: 4734505Abstract: 1-(Alkylated)-2-(acylated)diazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds. The instant compounds have the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as defined in the specification.Type: GrantFiled: May 14, 1986Date of Patent: March 29, 1988Assignee: Eli Lilly and CompanyInventor: Richard E. Holmes
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Patent number: 4731105Abstract: Herbicidal thiadiazolyloxyacetamides of the formula: ##STR1## wherein: R is an optionally-substituted alkyl, cycloalkyl or aryl group; R.sup.1 and R.sup.2, which may be the same or different, each represent hydrogen, alkyl, cycloalkyl, alkoxy, alkenyl, aryl, aralkyl or aryloxy, any alkyl or aryl moiety thereof being optionally substituted; or R.sup.1 and R.sup.2, together with the nitrogen atom to which they are attached, represent a heterocyclic or benzheterocyclic group, the hetrocyclic ring of which is 5- or 6-membered, and which may be substituted by one or more alkyl groups; and X is oxygen, sulphur or --S(O).sub.n --where n is 1 or 2,process for their preparation, and compositions containing them.Type: GrantFiled: August 13, 1986Date of Patent: March 15, 1988Assignee: FBC LimitedInventor: Graham P. Jones
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Patent number: 4728655Abstract: Sulfonamidine is disclosed of the general formula (I):R--NH--CH.dbd.N--SO.sub.2 --R.sub.1 (I)wherein R is a group selected from 2-[[(5-methyl-1H-imidazole-4-yl)methyl]thio]ethyl], 2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl, 2-[[[2-[(aminoiminomethyl)amino]-4-thiazolyl]methyl]thio]ethyl] or 3-[3-(1-piperidinylmethyl)phenoxy] propyl and R.sub.1 is alkyl; or a phenyl group optionally substituted by alkyl, halogen, nitro, alkoxy, alkanoylamino, carboxylic acid, alkoxycarbonyl, dialkylamino, alkylsulphonyl, alkylsulphonylamino or alkylthio; or 1,3,4-thiadiazole-2-yl substituted by alkanoylamino, and the pharmaceutically acceptable salts thereof, as well as a process for preparing these compounds and pharmaceutical compositions containing the same. These compounds have antiulcer activity and can be used in the treatment of peptic ulcers and other pathologies caused or stimulated by gastric acidity.Type: GrantFiled: April 18, 1985Date of Patent: March 1, 1988Assignee: Ferrer Internacional S.A.Inventors: Rafael Foguet, Luis Anglada, Josep Castello, Aurelio Sacristan, Jose Ortiz
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Patent number: 4722934Abstract: The present invention relates to a thiadiazole derivative of the following general formula (I) and an insecticidal and miticidal composition containing the same as an active ingredient: ##STR1## wherein A represents a group of the formula ##STR2## R.sup.1 and R.sup.2 independently represent a hydrogen atom, a halogen atom, a lower alkyl group, a trifluoromethyl group, a cyano group or a nitro group or jointly represent a methylenedioxy group, R.sup.3 represents a hydrogen atom or a lower alkyl group, R.sup.4 represents a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a monoalkylamino group having a lower alkyl group or a dialkylamino group having lower alkyl group, and n is an integer of from 1 through 3.Type: GrantFiled: March 16, 1987Date of Patent: February 2, 1988Assignee: Mitsubishi Chemical Industries LimitedInventors: Susumu Matsumoto, Shigeru Suzuki, Hiroki Ohta, Yoshiaki Higashino, Toshiki Fukuchi
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Patent number: 4721782Type: GrantFiled: October 10, 1985Date of Patent: January 26, 1988Assignee: Bayer AktiengesellschaftInventor: Fritz Maurer
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Patent number: 4715884Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: A, B and D are selected from CH and N;E is selected from oxygen and sulfur;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, phenyl, substituted phenyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;R.sup.Type: GrantFiled: July 11, 1986Date of Patent: December 29, 1987Assignee: Imperial Chemical Industries PLCInventor: Keith G. Watson
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Patent number: 4708731Abstract: 5-Halogenoalkyl-1,3,4-thiadiazol-2-yloxyacetamides of the formula ##STR1## in which R.sup.1 is halogenoalkyl, with the exception of trifluoromethyl, andR.sup.2 and R.sup.3 each independently is hydrogen, alkyl, alkenyl, alkinyl, in each case optionally substituted cycloalkyl or cycloalkenyl, halogenoalkyl, alkoxyalkyl, alkoxyalkylenoxy, alkoxy, aralkyl or optionally substituted aryl, orR.sup.2 and R.sup.3, together with the nitrogen atom to which they are bonded, form an optionally substituted heterocyclic radical which can contain further hetero-atoms,which possess herbicidal and fungicidal activity. The intermediates 5-chlorodifluoromethyl- and 5-dichlorofluoromethyl-2-chloro-1,3,4-thiadiazole are also new.Type: GrantFiled: December 21, 1984Date of Patent: November 24, 1987Assignee: Bayer AktiengesellschaftInventors: Heinz Forster, Hans-Joachim Diehr, Fritz Maurer, Erich Klauke, Ludwig Eue, Hans-Joachim Santel, Robert R. Schmidt, Paul Reinecke, Gerd Hanssler
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Patent number: 4704157Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: A, B and D are selected from CH and N;E is selected from oxygen and sulfur;X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, alkenyl, alkenyloxy, alkynyl, alkynyloxy, acyloxy, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, sulfamoyl, substituted sulfamoyl, alkanoyloxy, benzyloxy, substituted benzyloxy, phenyl, substituted phenyl, amino, substituted amino, and the groups formyl and alkanoyl and the oxime, imine and Schiff base derivatives thereof;R.sup.1 is selected from hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl, alkylsulfonyl, arylsulfonyl, acyl and an inorglanic or organic cation;R.sup.2 is selected from alkyl substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl;R.sup.Type: GrantFiled: May 8, 1986Date of Patent: November 3, 1987Assignee: CI Australia Ltd.Inventors: Richard J. Conway, Keith G. Watson, Graeme J. Farquharson
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Patent number: 4695567Abstract: The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.Type: GrantFiled: January 17, 1986Date of Patent: September 22, 1987Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein, Egon Roesch
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Patent number: 4694014Abstract: The invention relates to novel compounds of the formulae ##STR1## in which formulae R'is C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, halogen or trifluoromethyl,R" is C.sub.1 -C.sub.5 alkyl or halogen,m is 1 ot 3 and n is 0 to 1,X is oxygen or sulfur,Y is hydrogen, fluorine, trifluoromethyl or the group HC(F)Z,Y' is hydrogen or the group CHF.sub.2 andZ is fluorine or trifluoromethyl,as active ingredients for controlling nematodes which parasitise on plants and for protecting cultivated plants from damage caused by nematode attack.Type: GrantFiled: September 26, 1986Date of Patent: September 15, 1987Assignee: Ciba-Geigy CorporationInventor: Beriger Ernst
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Patent number: 4692513Abstract: Alpha-L-Aspartyl-D-heteroaromatic-substituted glycine esters and amides are disclosed to be useful as high intensity sweeteners. These compounds can be used to sweeten a variety of foods, beverages and other oral products.Type: GrantFiled: December 20, 1985Date of Patent: September 8, 1987Assignee: The Procter & Gamble CompanyInventors: Robert B. Blum, John M. Gardlik, John M. Janusz, George P. Rizzi
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Patent number: 4691023Abstract: The present invention refers to mitomycin analogs containing a disulfide group. These compounds are mitomycin C derivatives in which the 7-amino group bears an organic substituent incorporating a disulfide group. The compounds are inhibitors of experimental animal tumors.Type: GrantFiled: August 7, 1986Date of Patent: September 1, 1987Assignee: Bristol-Myers CompanyInventors: Dolatrai M. Vyas, Yulin Chiang, Terrence W. Doyle