The Ring Is A Benzene Ring Patents (Class 514/485)
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Patent number: 5227401Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.Type: GrantFiled: October 29, 1991Date of Patent: July 13, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5223535Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.5 and R.sub.8 is independently propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.Type: GrantFiled: October 29, 1991Date of Patent: June 29, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5210084Abstract: Combating fungi with substituted amine acid derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, halogenoalkinyl, cycloalkyl or cycloalkenyl,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and represent hydrogen, cycloalkyl or alkyl, orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring, andR.sup.6 represents hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, unsubstituted or substituted phenylalkyl, unsubstituted or substituted phenyl or unsubstituted or substituted cycloalkyl, or represents unsubstituted or substituted heterocyclyl or heterocyclylalkyl, orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a heterocyclyl radical, which can contain further hetero atoms.Type: GrantFiled: April 25, 1990Date of Patent: May 11, 1993Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Thomas Seitz, Wilhelm Brandes
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Patent number: 5151443Abstract: A method of controlling termites employing substituted phenoxy, phenylthio and anilino compounds.Type: GrantFiled: January 16, 1992Date of Patent: September 29, 1992Assignee: Sandoz Ltd.Inventor: Clive A. Henrick
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Patent number: 5091414Abstract: A compound of Formula (I):(I) R.sup.1 (CA.dbd.CA.sup.1).sub.x --C(.dbd.X)NR.sup.2 R.sup.3where R.sup.1 is alkyl optionally substituted by a group selected from alkoxy, alkenyl, alkynyl, alkenyloxy, alkynyloxy, aryl, aryloxy, arylalkoxy and cycloalkyl fused to an aryl ring; x=1 or 2; X=O or S; each A and A.sup.1 is independently hydrogen, alkyl or haloalkyl; R.sup.2 is alkyl, alkenyl or cycloalkyl any of which may be substituted by halo, alkenyl, alkyl, cycloalkyl, alkynyl, dioxalanylalkyl or alkoxy; and R.sup.3 is selected from groups (A) to (D):(A) --Y=X.sup.1 --(R.sup.4).sub.a where X.sup.1 is O or S, Y is phosphorus or carbon, R.sup.4 is hydrogen, alkyl, alkoxy, acyl or CO.sub.2 R.sup.5 where R.sup.5 is alkyl or aryl, and a is 1 or 2(B) --S(R.sup.6)(O).sub.bwhere R.sup.6 is alkyl, aryl, aryloxy, alkoxy, thioalkoxy, thioaryl, alkythio, alkoxythio or arylthio and b is 0, 1 or 2(C) --S(O).sub.c NR.sup.7 R.sup.8where c is 0, 1 or 2, R.sup.7 is --COR.sup.9 or --CO.sub.2 R.sup.9 where R.sup.Type: GrantFiled: November 29, 1990Date of Patent: February 25, 1992Assignee: Burroughs Wellcome Co.Inventors: Malcolm H. Black, Robert J. Blade, Robert J. Peek
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Patent number: 5010105Abstract: Compounds of Formula (I) and (II): ##STR1## are HMG-CoA reductase inhibitors.Type: GrantFiled: May 9, 1990Date of Patent: April 23, 1991Assignee: Merck & Co., Inc.Inventor: Ta J. Lee
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Patent number: 5007953Abstract: Methods of using comminuted Alder bark as a stimulator of seed germination and growth media comprising comminuted Alder bark are disclosed. Also disclosed are seed treatment dusts comprising an active ingredient, a diluent material and comminuted Alder bark and methods of using these dusts. The active ingredients include fungicides, insecticides and other pesticides. The diluent materials used include clays and talcs.Type: GrantFiled: December 22, 1988Date of Patent: April 16, 1991Assignee: Snake River Chemicals, Inc.Inventor: Charles C. Chollet
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Patent number: 4933366Abstract: A fungicidal composition which comprises as an active ingredient a fungicidally effective amount of the compound represented by the general formula, ##STR1## wherein X, which may be the same or different, represents a hydrogen or halogen atom or a lower alkyl group, R.sup.1 and R.sup.2, which may be the same or different, represent a hydrogen atom or a methyl group, and n represents an integer of from 1 to 5, and an inert carrier.Type: GrantFiled: June 22, 1989Date of Patent: June 12, 1990Assignee: Sumitomo Chemical Company, LimitedInventors: Tomoyuki Kusaba, Junya Takahashi, Masayo Sugano, Tamon Uematsu, Yukio Oguri, Tomohiro Teramae
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Patent number: 4927845Abstract: Anthralin analogues containing a thio-substituent, especially in one or more of the positions 2-, 7- and 10- of the anthralin ring. They may be made by reacting an anthralin derivative (e.g. 10-bromoanthralin) with a thiol or a compound containing a group convertible to a thio-group. Alternatively, a 1,8-dihydroxy anthraquinone containing a thio-substituent may be reduced. Reactive intermediates may be made by introducing one or more nuclear allylic groups into a 1,8-dihydroxy anthraquinone and then converting them into a reactive form, e.g. by epoxidation or halide addition. The intermediate can then reduced to the oxidation state corresponding to anthralin.Additional products having the 10-carbon atom of the anthralin ring as part of a heterocyclic ring, may be made by anthralins containing various substitutes thioalkyl groups as the 10-substituent.The compounds are useful for treatment of psoriasis, and may be formulated in the conventional vehicles for topical application, for example petrolatum.Type: GrantFiled: August 15, 1989Date of Patent: May 22, 1990Assignee: The Victoria University of ManchesterInventor: John M. Bruce
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Patent number: 4908383Abstract: Novel N-phenyl-N-carboxythioureas of the formula I ##STR1## in which R.sub.1 and R.sub.2 each represents C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.5 -C.sub.6 cycloalkenyl,R.sub.3 represents hydrogen, halogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy or C.sub.1 -C.sub.10 alkylthio,R.sub.4 represents C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl or phenyl-C.sub.1 -C.sub.7 alkyl; C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl or phenyl-C.sub.1 -C.sub.7 alkyl each mono- or poly-substituted by halogen or interrupted one or several times by oxygen and/or sulphur; C.sub.3 -C.sub.8 cycloalkyl; or C.sub.3 -C.sub.8 cycloalkyl mono- or poly-substituted by halogen or by C.sub.1 -C.sub.5 alkyl, andR.sub.5 represents C.sub.1 -C.sub.10 alkyl; phenyl-C.sub.1 -C.sub.7 alkyl; C.sub.1 -C.sub.10 alkyl or phenyl-C.sub.1 -C.sub.7 alkyl each mono- or poly-substituted by halogen or interrupted one or several times by oxygen and/or sulphur; C.Type: GrantFiled: May 23, 1989Date of Patent: March 13, 1990Assignee: Ciba-Geigy CorporationInventors: Jozef Drabek, Josef Ehrenfreund
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Patent number: 4880831Abstract: Novel fungicidal carbanilates having the general structural formula ##STR1## wherein R is methoxy or allyloxy; R.sub.1 is selected from the group consisting of hydrogen, C.sub.2 -C.sub.4 alkoxyalkyl and formyl; and R.sub.2 is C.sub.1 -C.sub.6 alkyl, preferably C.sub.2 -C.sub.3 alkyl which are highly effective fungicides are disclosed herein.Type: GrantFiled: August 1, 1988Date of Patent: November 14, 1989Assignee: Stauffer Chemical CompanyInventors: Don R. Baker, Keith H. Brownell, Charles Kezerian
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Patent number: 4829089Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: July 22, 1988Date of Patent: May 9, 1989Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4797416Abstract: Novel fungicidal carbanilates having the general structural formula ##STR1## wherein R is methoxy or allyloxy; R.sub.1 is selected from the group consisting of hydrogen, C.sub.2 -C.sub.4 alkoxyalkyl and formyl; and R.sub.2 is C.sub.1 -C.sub.6 alkyl, preferably C.sub.2 -C.sub.3 alkyl which are highly effective fungicides are disclosed herein.Type: GrantFiled: January 5, 1987Date of Patent: January 10, 1989Assignee: Stauffer Chemical Co.Inventors: Don R. Baker, Keith H. Brownell, Charles Kezerian
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Patent number: 4755528Abstract: Disclosed are 2,3-diamino-1,4-butanedithiol; 4,5-diamino-1,2-dithiane; and their N-acyl and N-alkyl derivatives. Also disclosed are processes for preparing the disclosed compounds; pharmaceutical compositions comprising such compounds; and a method of treatment comprising administering such compounds and compositions when an antihypertensive effect or radioprotective effect is indicated.Type: GrantFiled: April 17, 1987Date of Patent: July 5, 1988Assignee: Alcon Laboratories, Inc.Inventors: Mark T. DuPriest, Billie M. York, Jr.
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Patent number: 4755506Abstract: Compounds of the general formula: ##STR1## wherein A and B are both hydrogen, or one of A and B is a group (G) of the formula: ##STR2## and the other is a group R.sup.5 wherein R.sup.1 is an aryl group or a heterocyclic group, both of them being optionally substituted, and R.sup.4 and R.sup.5 are both hydrogen or together form a single chemical bond,R.sup.2 and R.sup.2 ' are independently hydrogen, halogen, nitro, lower alkyl or lower alkoxy, andR.sup.3 and R.sup.3 ' are independently carboxy or its functional derivative, with the proviso that (a) when A and B are both hydrogen, then R.sup.2 and R.sup.2 ' cannot be both hydrogen,and, where applicable, pharmaceuticably acceptable salts thereof are hyaluronidase inhibitors, and useful as anti-allergic agent and anti-ulcerous agent. Among the compound (I'), those wherein when one of A and B is the group (G) and the other is the group R.sup.5 wherein R.sup.4 and R.sup.5 together form a single chemical bond, R.sup.1 is unsubstituted aryl and R.sup.2 and R.sup.Type: GrantFiled: September 19, 1986Date of Patent: July 5, 1988Assignee: Sawai Pharmaceutical Co., Ltd.Inventors: Toshio Satoh, Hitoshi Matsumoto, Hisao Kakegawa, Yoshiko Kato, Juichi Riku, Junji Yoshinaga, Yoshifumi Kanamoto
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Patent number: 4723029Abstract: This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.Type: GrantFiled: September 23, 1983Date of Patent: February 2, 1988Assignee: Schering CorporationInventors: Dhiru B. Vashi, Jeffrey N. Clark, Neil A. Lindo
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Patent number: 4710514Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and/or dicarboximide fungicides.Type: GrantFiled: April 26, 1983Date of Patent: December 1, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Katsuzo Kamoshita
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Patent number: 4692468Abstract: This invention is directed to the use of a class of N-(2,2-difluoroalkanoyl)-o-phenylenediamines as an agent for the control of certain colonial insects, i.e., ants and termites.Type: GrantFiled: September 9, 1982Date of Patent: September 8, 1987Assignee: Eli Lilly and CompanyInventor: Rudolph J. Boisvenue
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Patent number: 4690946Abstract: Use of an N-phenylcarbamate of the formula: ##STR1## as a fungicidal agent against phytopathogenic fungi, particularly strains which are resistant to benzimidazole thiophanate fungicides and/or cyclic imide fungicides.Type: GrantFiled: October 14, 1983Date of Patent: September 1, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Katsuzo Kamoshita
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Patent number: 4668703Abstract: This invention is for .gamma.-allenyl-.gamma.-aminobutyric acid derivatives which are .gamma.-aminobutyric acid transaminase inhibitors.Type: GrantFiled: July 1, 1985Date of Patent: May 26, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Alexander Krantz, Arlindo L. Castelhano, Diana H. Pliura
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Patent number: 4666938Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole and thiophanate fungicides and/or cyclic imide fungicides.Type: GrantFiled: May 24, 1984Date of Patent: May 19, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4647582Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, and particularly against strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.Type: GrantFiled: December 23, 1983Date of Patent: March 3, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4647584Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, and particularly against strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.Type: GrantFiled: December 28, 1983Date of Patent: March 3, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4618623Abstract: The invention relates to new carbazic acid derivatives, a process for the preparation thereof and compositions--particularly feed additives and animal feeds--containing the same. The new compounds according to the invention correspond to the formula (I)R.sup.1 .dbd.N--NH--COOR.sup.3 (I)wherein R.sup.1 stands for a C.sub.7-12 cycloalkylidene group, an indanylidene group or a group of the formula (IX) ##STR1## wherein A represents a phenyl group optionally carrying one or more identical or different substituents selected from the group consisting of halo, nitro, hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, amino or C.sub.1-4 alkoxycarbonylhydrazino; phenyl-(C.sub.1-4 alkyl), C.sub.1-16 alkyl, C.sub.3-7 cycloalkyl or indolyl, or a C.sub.3 -C.sub.6 cycloalkyl group substituted by a C.sub.3 -C.sub.6 cycloalkyl group; R.sup.2 denotes a hydrogen atom, a C.sub.1-16 alkyl or a C.sub.3-7 cycloalkyl group; and R.sup.3 represents a C.sub.1-4 alkyl group.Type: GrantFiled: May 23, 1985Date of Patent: October 21, 1986Assignee: Egyt Gyogyszervegyeszeti GyarInventors: Zoltan Budai, Pal Benko, Ildiko Ratz nee Simonek, Eva Rakoczy nee Pinter, Karoly Magyar, Jozsef Kelemen, Attila Mandi
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Patent number: 4605668Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, and particularly the strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.Type: GrantFiled: April 12, 1984Date of Patent: August 12, 1986Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4507292Abstract: Aryl N-oxalyl-N-methyl-carbamates of the general formula ##STR1## in which X represents an alkoxy, alkenoxy, alkinoxy, aryloxy, alkylthio, alkenylthio, alkinylthio or arylthio radical, each of which may be optionally substituted, or represents a radical of the general formula --N R.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are identical or different and represent a hydrogen atom or an alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl or aryl radical, each of which may be optionally substituted,or the radicals R.sup.3 and R.sup.4, together with the N atom to which they are bonded, form an optionally substituted heterocyclic ring, andR.sup.1 represents an aryl radical which is optionally substituted,are novel and find use as pesticides, especially for combating insects, acarids and nematodes.Type: GrantFiled: January 27, 1983Date of Patent: March 26, 1985Assignee: Bayer AktiengesellschaftInventors: Gerhard Heywang, Engelbert Kuhle, Wolfgang Behrenz, Ingeborg Hammann, Bernhard Homeyer
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Patent number: 4504490Abstract: New benzenesulfonic esters of the formula I ##STR1## and a process for their preparation are described. The new compounds are active against helminths and can thus be used as agents to counter worms in humans and animals.Type: GrantFiled: September 2, 1983Date of Patent: March 12, 1985Assignee: Hoechst AktiengesellschaftInventors: Manfred Rosner, Josef Urbanietz, Heinz Loewe, Dieter Duwel, Reinhard Kirsch