Amidoximes (i.e., Hon=ch-hnh, Wherein Substitution May Be Made For Hydrogen Only) Patents (Class 564/229)
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Patent number: 5981511Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: March 5, 1997Date of Patent: November 9, 1999Assignee: G.D. Searle & Co.Inventors: Rolando E. Gapud, Timothy J. Hagen, Ann E. Hallinan, Donald W. Hansen, Jr., Robert E. Manning, Suzanne Metz, Barnett S. Pitzele, Foe S. Tjoeng, Mihaly V. Toth, R. Keith Webber
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Patent number: 5955507Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: September 21, 1999Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
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Patent number: 5945408Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: August 8, 1996Date of Patent: August 31, 1999Assignee: G.D. Searle & Co.Inventors: R. Keith Webber, Foe S. Tjoeng, Robert E. Manning
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Patent number: 5922772Abstract: The present invention provides therapeutically useful substituted guanidines and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: July 13, 1999Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
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Patent number: 5859010Abstract: The invention relates to novel compounds that potentiate zinc ion inhibition of the activity of factor VIIa or tissue factor--factor VIIa complex having the formula Ia and Ib and pharmaceutical salts thereof as well as pharmaceutical compositions comprising said novel compounds. The invention is further related to the use of said compositions for inhibiting clotting activity, tissue factor activity and factor VIIa activity.Type: GrantFiled: June 23, 1997Date of Patent: January 12, 1999Assignee: Novo Nordisk A/SInventors: Lars Christian Petersen, Ole Hvilsted Olsen, Stefan Lutz Richter, Palle Jakobsen
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Patent number: 5786383Abstract: The invention relates to a novel pharmaceutical preparation, containing an active ingredient of at least one active amidine group, which contains a pharmaceutically active amidine group which may be a administered orally.The amidine group is present in the form of a compound selected from the group: ##STR1## wherein R.sub.7 is hydrogen, an alkly residue and/or an aryl residue.Type: GrantFiled: February 6, 1996Date of Patent: July 28, 1998Inventor: Bernd Clement
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Patent number: 5728737Abstract: The present invention relates to novel N-alkoxy-arnidine derivatives of the formula (I), to a process for their preparation and to their use as pesticides. In addition, the invention also relates to novel intermediates and to a process for their preparation.Type: GrantFiled: January 23, 1997Date of Patent: March 17, 1998Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Bernd-Wieland Kruger, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
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Patent number: 5723495Abstract: A method of treating Pneumocystis carinii pneumonia in a subject in need of such treatment is disclosed. The method comprises orally administering to the subject a bis-benzamidoxime of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl or alkylaminoalkyl; R.sub.3 is H, loweralkyl, oxyalkyl, alkoxyalkyl, hydroxyalkyl, cycloalkyl, aryl, aminoalkyl, alkylaminoalkyl or halogen; n is from 2 to 6; X is O, N, or S; and Y is H or loweralkyl, or a pharmaceutically acceptable salt thereof, that is reduced in the subject to produce a benzamidine having anti-P, carinii activity. The method of the present invention may alternatively comprise intravenously administering to the subject an active compound as disclosed herein. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.Type: GrantFiled: November 16, 1995Date of Patent: March 3, 1998Assignees: The University of North Carolina at Chapel Hill, Georgia State UniversityInventors: James E. Hall, Richard R. Tidwell, David W. Boykin
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Patent number: 5705531Abstract: 1,5-Disubstituted 5a-methylperhydroinden-3a-ol derivatives of formula (I): ##STR1## where eitherthe symbol - - - - represents a single bond,the group A is in cis configuration with respect to the 3a-hydroxy, 7a-methyl and 1-L groups, andA is (CH.dbd.CH).sub.m (CH.sub.2).sub.n OR, (CH.dbd.CH).sub.m (CH.sub.2).sub.n NR.sup.1 R.sup.2, (CH.dbd.CH).sub.m (CH.sub.2).sub.p B, OH, O(CH.sub.2).sub.q OR, O(CH.sub.2).sub.q NR.sup.1 R.sup.2 or O(CH.sub.2).sub.r B;q is an integer from 2 to 5;r is an integer from 1 to 2;orthe symbol - - - - represents a double bond,A is oxygen, CH(CH.dbd.CH).sub.s (CH.sub.2).sub.n OR,CH(CH.dbd.CH).sub.s (CH.sub.2).sub.n NR.sup.1 R.sup.2 orCH(CH.dbd.CH).sub.s (CH.sub.2).sub.p B; andL is ?CH.dbd.C(R.sup.3)!.sub.s CH.dbd.NR.sup.4 or ?CH.dbd.C(R.sup.3)!.sub.s CH.sub.2 NHR.sup.4, in the E configuration, are useful for treating cardiovascular disorders such as heart failure and hypertension.Type: GrantFiled: November 2, 1995Date of Patent: January 6, 1998Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Nicoletta Almirante, Giuseppe Bianchi, Patrizia Ferrari, Piero Melloni
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Patent number: 5621145Abstract: When a novel bisamidoxime compound represented by the following general formula: ##STR1## where R is an alkylidene group having 1 to 6 carbon atoms, or a perfluoroalkylidene group having 1 to 10 carbon atoms, is used as a vulcanizing agent for fluorine-containing elastomers having cyano groups as cross-linkable groups, the resulting vulcanizates having a satisfactory compression set are obtained without any problem of processability such as roll kneadability, etc.Type: GrantFiled: January 5, 1996Date of Patent: April 15, 1997Assignee: Nippon Mektron, LimitedInventors: Satoru Saito, Haruyoshi Tatsu, Lev Solomonovich, deceased, Ziefman Y. Vilovich, Postovoi S. Anatol'evich, Sterlin S. Rafailovich
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Patent number: 5478946Abstract: Compounds of the formula: ##STR1## useful as regulators of nitric oxide synthase that indirectly modulate cyclic guanosine monophosphate (cGMP), pharmaceutical compositions thereof, for treating disorders of vascular smooth muscles, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, sickle cell anemia and diabetes.Type: GrantFiled: November 30, 1993Date of Patent: December 26, 1995Assignee: Abbott LaboratoriesInventors: Ferid Murad, James F. Kerwin, Lee D. Gorsky
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Patent number: 5380945Abstract: Compounds of the formula: ##STR1## useful as regulators of nitric oxide synthase that indirectly modulate cyclic guanosine monophosphate (cGMP), pharmaceutical compositions thereof, for treating disorders of vascular smooth muscles, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, sickle cell anemia and diabetes.Type: GrantFiled: November 30, 1993Date of Patent: January 10, 1995Assignee: Abbott LaboratoriesInventors: Ferid Murad, James F. Kerwin, Lee D. Gorsky
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Patent number: 5183828Abstract: Polyhydroxy-substituted benz, phenylacet and mandelamidines, amidates, amidoximes and hydroxyamidoximes--ribonucleotide reductase inhibitors, and free radical scavengers.Type: GrantFiled: July 20, 1990Date of Patent: February 2, 1993Inventors: Bartholomeus van't Riet, Howard L. Elford, Galen L. Wampler
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Patent number: 5037467Abstract: The present invention relates to amidoxime derivatives of the formula (I): ##STR1## wherein R.sub.1 is a C.sub.1-3 alkyl or allyl group, a methyl group substituted by chlorine or fluorine atom or ethoxycarbonyl or diethyldithiophosphate group, a phenoxymethyl group unsubstituted or substituted by chlorine atom, a C.sub.2 alkoxy or phenoxy group unsubstituted or substituted by chlorine atom or ethoxycarbonylethoxy group, a phenyl group unsubstituted or substituted by chlorine or fluorine atom, a benzyl group unsubstituted or substituted by chlorine atom, or a morpholine group; R.sub.2 is a phenoxymethyl or phenoxyethyl group substituted by chlorine atom, a phenyl group substituted by chlorine atom or methoxy group, or an ethoxy group. The compounds of the invention have a extremely high selectivity between paddy rice or crop plants and weeds and a strong activity on weeds. Moreover, the compounds have a very low phytotoxicity to paddy rice and crop plants.Type: GrantFiled: June 29, 1989Date of Patent: August 6, 1991Inventors: Kwang Y. Cho, In H. Jeong, Young S. Kim, Beom T. Kim, Yong K. Min, Geun S. Jeon, Jin S. Kim, Kyung S. Hong, In T. Hwang, Suk J. Koo
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Patent number: 4942253Abstract: Polyhydroxy-substituted benz, phenylacet and mandelamidines, amidates, amidoximes and hydroxyamidoximes--ribonucleotide reductase inhibitors, and free radical scavengers.Type: GrantFiled: September 15, 1986Date of Patent: July 17, 1990Inventors: Bartholomeus van't Riet, Howard L. Elford, Galen L. Wampler
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Patent number: 4808750Abstract: Novel fluorophenoxyphenoxypropionates and derivatives thereof possess herbicidal activity selectively in the presence of broadleaf crops. Preemergent and postemergent applications are contemplated.Type: GrantFiled: July 14, 1986Date of Patent: February 28, 1989Assignee: The Dow Chemical CompanyInventors: Richard B. Rogers, B. Clifford Gerwick, III
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Patent number: 4705782Abstract: The invention relates to compounds of the general formula I ##STR1## wherein R.sub.1 represents one up to and including four, the same or different substituents selected from alkyl(1-6 C), alkoxy(1-6 C), hydroxy, halogen, NO.sub.2, CF.sub.3 or the group --NR.sub.5 R.sub.6,whereby two substituents taken together may also represent a methylene-dioxy group,X represents a member selected from ##STR2## --CH.sub.2 --CH.sub.2 -- and --CH.dbd.CH--, n has the value 0, 1 or 2,R.sub.3 represents one of the moieties: ##STR3## and R.sub.2, R.sub.4, R.sub.5 and R.sub.6 represent hydrogen or alkyl(1-6 C),and pharmaceutically acceptable salts thereof, suitable in the treatment of heartfailure.Type: GrantFiled: March 26, 1986Date of Patent: November 10, 1987Assignee: Akzo N.V.Inventors: Robert T. Logan, James Redpath, Robert G. Roy
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Patent number: 4661522Abstract: The present invention is dealing with cycloalkane-indene-carboximidamide derivatives having the general formula: ##STR1## wherein Rx together with either Ry.sub.1 or Ry.sub.2 represent the moiety ##STR2## (the other Ry being hydrogen), n represents the number 1, 2 or 3,R represents hydrogen or a (1-4 C)-alkyl group,R.sub.1 represents hydrogen, (1-4 C)-alkyl, hydroxyl, (1-4 C)-alkoxy or an amino group which is unsubstituted or substituted by (1-4 C)-alkyl andR.sub.2 is hydrogen, hydroxyl or (1-4 C)-alkyl,as well as the pharmaceutically acceptable salts thereof, with powerful blood platelet aggregation-inhibiting activity.Type: GrantFiled: May 15, 1985Date of Patent: April 28, 1987Assignee: Akzo N.V.Inventor: Tom Beetz
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Patent number: 4623659Abstract: Polyhydroxy-substituted benz, phenylacet and mandelamidines, amidates, amidoximes and hydroxyamidoximes--ribonucleotide reductase inhibitors, and free radical scavengers.Type: GrantFiled: May 23, 1983Date of Patent: November 18, 1986Inventors: Bartholomeus van't Riet, Howard L. Elford, Galen L. Wampler
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Patent number: 4554014Abstract: As new compounds, O-aryloxyphenoxyacyl-.alpha.-N,N-dialkylaminooximes having the formula ##STR1## wherein R.sub.1 and R.sub.2 are each the same or different and are selected from alkyl groups having from 1 to 4 carbon atoms or R.sub.1 and R.sub.2 can form a ring containing 3 to 5 carbon atoms, R.sub.Type: GrantFiled: April 20, 1984Date of Patent: November 19, 1985Assignee: Stauffer Chemical CompanyInventors: Charles G. Carter, David L. Lee
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Patent number: 4499105Abstract: The present invention is dealing with compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, in which n and m represent the number 1 or 2, X and Y hydrogen, alkyl (1-4 C), alkoxy (1-4 C), hydroxy, halogen, hydroxymethyl, trifluoromethyl, acyl (1-4 C), acyloxy (1-4 C) or the group NR.sub.x R.sub.y, in which R.sub.x and R.sub.y represent hydrogen, alkyl (1-4 C) or a sulphonyl group and R represents the group ##STR2## in which R.sub.1 and R.sub.2 represent hydrogen, alkyl (1-4 C), hydroxy, alkoxy (1-4 C), phenylalkoxy (7-10 C), acyloxy, amino or mono or dialkyl (1-4 C) amino, having potent platelet aggregation inhibiting properties.Type: GrantFiled: December 28, 1982Date of Patent: February 12, 1985Assignee: Akzo N.V.Inventor: Harm J. Panneman
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Patent number: 4426393Abstract: There are disclosed arylhydrazo-aldoximes which, as such, as tautomers, and in the form of organic or inorganic salts thereof, are active in preventing and treating infections of useful plants by fungi, and in immunizing plants against such infections.Type: GrantFiled: September 29, 1981Date of Patent: January 17, 1984Assignee: Montedison S.p.A.Inventors: Nicola Troiani, Franco Gozzo, Simone Lorusso
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Patent number: 4409242Abstract: The present invention relates as new industrial products to 4-phenoxy-3-butyramidoxime derivatives, characterized in that they are selected from the group consisting of 4-(allylphenoxy)-3-hydroxy-butyramidoximes of formula: ##STR1## and addition salts thereof. These products are useful in therapeutics, particularly as antiarrythmic agents. The compounds of formula I are prepared by reacting the corresponding butyronitrile with hydroxylamine.Type: GrantFiled: March 19, 1982Date of Patent: October 11, 1983Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4325964Abstract: A compound having the general formula: ##STR1## wherein Ar is an aryl group (especially an .alpha.-naphthyl, .beta.-naphthyl or phenyl group) which may be substituted by one or more C.sub.1-4 alkyl, C.sub.1-4 alkoxy, methylenedioxy halogen, CF.sub.3, NH.sub.2 or NO.sub.2 groups;A is a --CH.sub.2 --, --CHOH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 NH--, --OCH.sub.2 --, --SCH.sub.2 --, --NH--, --NHCOCH.sub.2 --, --CH.sub.2 NHCH.sub.2 -- or --NHCH.sub.2 -- group;Y is O or NH; andB is a single bond and, when A is --CH.sub.2 --S, may be a --CH.sub.2 --, or --CH(CH.sub.3)-- group; and their acid addition salts when Y is NH and their metal salts when Y is O.The compounds and their salts have therapeutic utility in treatment of neuropsychic ailments.Type: GrantFiled: December 27, 1979Date of Patent: April 20, 1982Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4316035Abstract: Fluorinated alkyl or alkylether 1,2,4-oxadiazole compounds are prepared by cyclizing the corresponding alkyl or alkylether imidoylamidoximes in vacuo or in an inert atmosphere at a temperature within the range of 40.degree. to 100.degree. C. for a period of 8 to 144 hours in the presence of an acid compound which can accept ammonia to form a salt. The imidoylamidoximes usable in this process may be either polymeric or nonpolymeric. The products, when polymeric, have excellent heat, chemical and solvent resistance.Type: GrantFiled: June 27, 1980Date of Patent: February 16, 1982Inventors: Robert A. Administrator of the National Aeronautics and Space Administration, with respect to an invention of Frosch, Reinhold H. Kratzer, Kazimiera J. L. Paciorek, Thomas I. Ito, Robert W. Rosser
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Patent number: 4308399Abstract: A compound effective in the treatment of diabetic angiopathy, i.e. a selective .beta.-receptor blocker has the formula ##STR1## wherein: R.sup.2 is a hydrogen or alkyl having one to five carbon atoms,R.sup.3 is alkyl having one to five carbon atoms, cycloalkyl or phenyl optionally substituted with hydroxyl or phenyl, or R.sup.2 and R.sup.3 together form a five- to eight-membered ring optionally containing also other heteroatoms and/or fused with another ring, preferably phenyl, naphthyl, quinolyl, isoquinolyl, pyridyl, pyrazolyl,R.sup.5 is hydrogen or alkyl having one to four carbon atoms, cycloalkyl or phenyl optionally substituted with halogen, alkoxy having one to four carbon atoms or alkyl having one to four carbons,R.sup.6 is hydrogen, alkyl having one to four carbon atoms or phenyl, m=0, 1 or 2, and n=0, 1 or 2.Type: GrantFiled: July 5, 1979Date of Patent: December 29, 1981Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Kalman Takacs, Peter N. Literati, Ilona Kiss nee Ajzert, Antal Simay, Matyas Szentivanyi, Sandor Virag, Katalin Farago
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Patent number: 4271194Abstract: The compound (3,4-Dichlorophenylsulphinyl)-acetamidoxime, of the structural formula: ##STR1## and its addition salts with acids. These compounds are useful in therapy as substances acting on the central nervous system.Type: GrantFiled: June 13, 1979Date of Patent: June 2, 1981Assignee: Laboratoire L. LafonInventor: Victor Lafon
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Patent number: 4269787Abstract: New crosslinked 1,2,4-oxadiazole elastomers have been prepared by thermally condensing (a) monomer having the formula H.sub.2 N(HON)C--R--Q, wherein Q is a triazine rig-forming group such as nitrile or amidine or a mixture of such group with amidoxime, or (b) a mixture of said monomer with R[C(NOH)NH.sub.2 ].sub.2, with R in these formulas standing for a bivalent organic radical having the formula--(CX.sub.2).sub.p --, or --CFY(OCF.sub.2 CFY).sub.m O(CX.sub.2).sub.p O(CFYCF.sub.2 O).sub.n CFY--wherein X is fluorine or hydrogen, Y is fluorine or trifluoromethyl, p ranges from 1 to 18, and m+n ranges from 2 to 7. In the monomer charge, the overall proportions of amidoxime groups to triazine ring-forming groups varies depending on the extent of crosslinking desired in the final polymer.Type: GrantFiled: April 30, 1980Date of Patent: May 26, 1981Inventors: Robert A. Administrator of the National Aeronautics and Space Administration, with respect to an invention of Frosch, Robert W. Rosser, Ibrahim M. Shalhoub, Hanoi Kwong
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Patent number: 4268525Abstract: This invention is concerned with certain aryl amidoxime ethers of 3-phenoxybenzyl alcohol, which have insecticidal activity.Type: GrantFiled: April 28, 1980Date of Patent: May 19, 1981Assignee: Mobil Oil CorporationInventor: Jill H. Paul