Amidoximes (i.e., Hon=ch-hnh, Wherein Substitution May Be Made For Hydrogen Only) Patents (Class 564/229)
  • Patent number: 5981511
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: March 5, 1997
    Date of Patent: November 9, 1999
    Assignee: 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
  • Patent number: 5955507
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: September 21, 1999
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
  • Patent number: 5945408
    Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: August 8, 1996
    Date of Patent: August 31, 1999
    Assignee: G.D. Searle & Co.
    Inventors: R. Keith Webber, Foe S. Tjoeng, Robert E. Manning
  • Patent number: 5922772
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: July 13, 1999
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
  • Patent number: 5859010
    Abstract: 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: Grant
    Filed: June 23, 1997
    Date of Patent: January 12, 1999
    Assignee: Novo Nordisk A/S
    Inventors: Lars Christian Petersen, Ole Hvilsted Olsen, Stefan Lutz Richter, Palle Jakobsen
  • Patent number: 5786383
    Abstract: 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: Grant
    Filed: February 6, 1996
    Date of Patent: July 28, 1998
    Inventor: Bernd Clement
  • Patent number: 5728737
    Abstract: 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: Grant
    Filed: January 23, 1997
    Date of Patent: March 17, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Bernd-Wieland Kruger, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 5723495
    Abstract: 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: Grant
    Filed: November 16, 1995
    Date of Patent: March 3, 1998
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University
    Inventors: James E. Hall, Richard R. Tidwell, David W. Boykin
  • Patent number: 5705531
    Abstract: 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: Grant
    Filed: November 2, 1995
    Date of Patent: January 6, 1998
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Nicoletta Almirante, Giuseppe Bianchi, Patrizia Ferrari, Piero Melloni
  • Patent number: 5621145
    Abstract: 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: Grant
    Filed: January 5, 1996
    Date of Patent: April 15, 1997
    Assignee: Nippon Mektron, Limited
    Inventors: Satoru Saito, Haruyoshi Tatsu, Lev Solomonovich, deceased, Ziefman Y. Vilovich, Postovoi S. Anatol'evich, Sterlin S. Rafailovich
  • Patent number: 5478946
    Abstract: 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: Grant
    Filed: November 30, 1993
    Date of Patent: December 26, 1995
    Assignee: Abbott Laboratories
    Inventors: Ferid Murad, James F. Kerwin, Lee D. Gorsky
  • Patent number: 5380945
    Abstract: 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: Grant
    Filed: November 30, 1993
    Date of Patent: January 10, 1995
    Assignee: Abbott Laboratories
    Inventors: Ferid Murad, James F. Kerwin, Lee D. Gorsky
  • Patent number: 5183828
    Abstract: Polyhydroxy-substituted benz, phenylacet and mandelamidines, amidates, amidoximes and hydroxyamidoximes--ribonucleotide reductase inhibitors, and free radical scavengers.
    Type: Grant
    Filed: July 20, 1990
    Date of Patent: February 2, 1993
    Inventors: Bartholomeus van't Riet, Howard L. Elford, Galen L. Wampler
  • Patent number: 5037467
    Abstract: 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: Grant
    Filed: June 29, 1989
    Date of Patent: August 6, 1991
    Inventors: 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
  • Patent number: 4942253
    Abstract: Polyhydroxy-substituted benz, phenylacet and mandelamidines, amidates, amidoximes and hydroxyamidoximes--ribonucleotide reductase inhibitors, and free radical scavengers.
    Type: Grant
    Filed: September 15, 1986
    Date of Patent: July 17, 1990
    Inventors: Bartholomeus van't Riet, Howard L. Elford, Galen L. Wampler
  • Patent number: 4808750
    Abstract: Novel fluorophenoxyphenoxypropionates and derivatives thereof possess herbicidal activity selectively in the presence of broadleaf crops. Preemergent and postemergent applications are contemplated.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: February 28, 1989
    Assignee: The Dow Chemical Company
    Inventors: Richard B. Rogers, B. Clifford Gerwick, III
  • Patent number: 4705782
    Abstract: 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: Grant
    Filed: March 26, 1986
    Date of Patent: November 10, 1987
    Assignee: Akzo N.V.
    Inventors: Robert T. Logan, James Redpath, Robert G. Roy
  • Patent number: 4661522
    Abstract: 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: Grant
    Filed: May 15, 1985
    Date of Patent: April 28, 1987
    Assignee: Akzo N.V.
    Inventor: Tom Beetz
  • Patent number: 4623659
    Abstract: Polyhydroxy-substituted benz, phenylacet and mandelamidines, amidates, amidoximes and hydroxyamidoximes--ribonucleotide reductase inhibitors, and free radical scavengers.
    Type: Grant
    Filed: May 23, 1983
    Date of Patent: November 18, 1986
    Inventors: Bartholomeus van't Riet, Howard L. Elford, Galen L. Wampler
  • Patent number: 4554014
    Abstract: 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: Grant
    Filed: April 20, 1984
    Date of Patent: November 19, 1985
    Assignee: Stauffer Chemical Company
    Inventors: Charles G. Carter, David L. Lee
  • Patent number: 4499105
    Abstract: 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: Grant
    Filed: December 28, 1982
    Date of Patent: February 12, 1985
    Assignee: Akzo N.V.
    Inventor: Harm J. Panneman
  • Patent number: 4426393
    Abstract: 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: Grant
    Filed: September 29, 1981
    Date of Patent: January 17, 1984
    Assignee: Montedison S.p.A.
    Inventors: Nicola Troiani, Franco Gozzo, Simone Lorusso
  • Patent number: 4409242
    Abstract: 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: Grant
    Filed: March 19, 1982
    Date of Patent: October 11, 1983
    Assignee: Laboratoire L. Lafon
    Inventor: Louis Lafon
  • Patent number: 4325964
    Abstract: 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: Grant
    Filed: December 27, 1979
    Date of Patent: April 20, 1982
    Assignee: Laboratoire L. Lafon
    Inventor: Louis Lafon
  • Patent number: 4316035
    Abstract: 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: Grant
    Filed: June 27, 1980
    Date of Patent: February 16, 1982
    Inventors: 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
  • Patent number: 4308399
    Abstract: 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: Grant
    Filed: July 5, 1979
    Date of Patent: December 29, 1981
    Assignee: 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
  • Patent number: 4271194
    Abstract: 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: Grant
    Filed: June 13, 1979
    Date of Patent: June 2, 1981
    Assignee: Laboratoire L. Lafon
    Inventor: Victor Lafon
  • Patent number: 4269787
    Abstract: 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: Grant
    Filed: April 30, 1980
    Date of Patent: May 26, 1981
    Inventors: 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
  • Patent number: 4268525
    Abstract: This invention is concerned with certain aryl amidoxime ethers of 3-phenoxybenzyl alcohol, which have insecticidal activity.
    Type: Grant
    Filed: April 28, 1980
    Date of Patent: May 19, 1981
    Assignee: Mobil Oil Corporation
    Inventor: Jill H. Paul