Amidoximes (i.e., N-c=n-o) Patents (Class 514/633)
  • Patent number: 6153604
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: November 28, 2000
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
  • Patent number: 6147063
    Abstract: 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: Grant
    Filed: June 2, 1995
    Date of Patent: November 14, 2000
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Graham J. Durant, Sharad Magar, Lain-Yen Hu
  • Patent number: 6114392
    Abstract: 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: Grant
    Filed: April 16, 1996
    Date of Patent: September 5, 2000
    Inventors: Gad M. Gilad, Varda H. Gilad
  • Patent number: 6110944
    Abstract: 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: Grant
    Filed: March 12, 1997
    Date of Patent: August 29, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell
  • Patent number: 6025398
    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, 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: July 31, 1998
    Date of Patent: February 15, 2000
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.
    Inventors: James E. Hall, Richard R. Tidwell, David W. Boykin
  • Patent number: 6013675
    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: January 11, 2000
    Assignee: Cambridge NeuroScience, Inc.
    Inventors: Graham J. Durant, Lain-Yen Hu, Sharad Magar
  • 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: 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: 5844000
    Abstract: 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: Grant
    Filed: June 12, 1997
    Date of Patent: December 1, 1998
    Assignee: Sanofi
    Inventors: William Brian, Brian Folk, Juan Shi, Gerard Fabre, Claude Tronquet
  • Patent number: 5821267
    Abstract: The current invention discloses amidino derivatives useful as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: October 13, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Kam F. Fok, Foe S. Tjoeng, R. Keith Webber
  • 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: 5444075
    Abstract: 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: Grant
    Filed: October 20, 1994
    Date of Patent: August 22, 1995
    Inventors: Gevork Minaskanian, James V. Peck
  • Patent number: 5278178
    Abstract: 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: Grant
    Filed: April 29, 1993
    Date of Patent: January 11, 1994
    Assignee: Rohm and Haas Company
    Inventor: Jemin C. Hsu
  • 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: 4957533
    Abstract: 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: Grant
    Filed: September 1, 1988
    Date of Patent: September 18, 1990
    Assignee: Eli Lilly and Company
    Inventors: Wendell R. Arnold, James D. Davenport
  • 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: 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