Amidoximes (i.e., N-c=n-o) Patents (Class 514/633)
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Patent number: 6153604Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: November 28, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6147063Abstract: The present invention provides therapeutically useful substituted guanidines of the following Formula: ##STR1## and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 2, 1995Date of Patent: November 14, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
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Patent number: 6114392Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.Type: GrantFiled: April 16, 1996Date of Patent: September 5, 2000Inventors: Gad M. Gilad, Varda H. Gilad
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Patent number: 6110944Abstract: The present invention provides compounds having the structureAr.sub.1 --Q--Ar.sub.2 --O--(CH.sub.2).sub.n --Zand pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.Type: GrantFiled: March 12, 1997Date of Patent: August 29, 2000Assignee: G. D. Searle & Co.Inventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell
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Patent number: 6025398Abstract: 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, 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: July 31, 1998Date of Patent: February 15, 2000Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.Inventors: James E. Hall, Richard R. Tidwell, David W. Boykin
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Patent number: 6013675Abstract: 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: January 11, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
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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: 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: 5844000Abstract: This invention relates to novel propenone oxime ethers, methods of preparing them and pharmaceutical compositions containing them. The compounds have the formula: ##STR1## wherein R.sup.1 is H, or glucuronide;R.sup.2 and R.sup.3 are independently H or methyl;R.sup.4 is 0, or glucuronide, andn is 0 or 1, provided that when R.sup.1 is H, n is 1.Type: GrantFiled: June 12, 1997Date of Patent: December 1, 1998Assignee: SanofiInventors: William Brian, Brian Folk, Juan Shi, Gerard Fabre, Claude Tronquet
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Patent number: 5821267Abstract: The current invention discloses amidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: March 20, 1996Date of Patent: October 13, 1998Assignee: G.D. Searle & Co.Inventors: Kam F. Fok, Foe S. Tjoeng, R. Keith Webber
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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: 5444075Abstract: This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals and into the blood stream in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer.Type: GrantFiled: October 20, 1994Date of Patent: August 22, 1995Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 5278178Abstract: This invention relates to synergistic antimicrobial and biocidal compositions comprising 5-chloro-2-methyl-4-isothiazolin-3-one and 2-methyl-4-isothiazolin-3-one and one or more commercial biocides for more effective, and broader control of microorganisms in various industrial systems.Type: GrantFiled: April 29, 1993Date of Patent: January 11, 1994Assignee: Rohm and Haas CompanyInventor: Jemin C. Hsu
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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: 4957533Abstract: Compounds of the formula (I): ##STR1## wherein: X=O, S, or NOH;R.sup.1 is H or CH.sub.3 ;n=1, 2, or 3;R.sup.2, R.sup.3, and R.sup.4 are as defined in one of the following paragraphs(a) R.sup.2 and R.sup.3 are independently Cl or Br, and R.sup.4 is H;(b) R.sup.2, R.sup.3 and R.sup.4 are independently Cl or Br;(c) R.sup.2 is F, R.sup.3 is Cl, and R.sup.4 is H; or(d) R.sup.2 and R.sup.3 are CH.sub.3 or C.sub.2 H.sub.5, and R.sup.4 is H;R.sup.5, R.sup.6 and R.sup.7 are as defined in one of the following paragraphs(a) one of R.sup.6 and R.sup.7 is CF.sub.3, R.sup.5 and the other of R.sup.6 and R.sup.7 is H;(b) R.sup.5 and R.sup.6 are H; and R.sup.7 is F, Cl, or Br;(c) R.sup.5 and R.sup.7 are independently F, Cl or Br and R.sup.6 is H;(d) R.sup.5 and R.sup.6 are independently F, Cl, or Br, and R.sup.7 is H;(e) R.sup.6 and R.sup.7 are independently F, Cl, or Br, and R.sup.5 is H; or(f) R.sup.6 is phenoxy and R.sup.5 and R.sup.7 are Hare plant fungicides.Type: GrantFiled: September 1, 1988Date of Patent: September 18, 1990Assignee: Eli Lilly and CompanyInventors: Wendell R. Arnold, James D. Davenport
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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: 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