Bicyclo Ring System Patents (Class 514/186)
  • Patent number: 5770591
    Abstract: A bis(platinum) complex having the structure: ##STR1## wherein X, Y, Z, X', Y', and Z' are the same or different ligands and are halide, sulphate, phosphate, nitrate, carboxylate, substituted carboxylate, dicarboxylate, substituted dicarboxylate primary or secondary amine, sulfoxide, phosphine, pyridine-type nitrogen and the like; preferably, there is at least one Pt-anion bond on each Pt molecule; and A is a diamine or polyamine.Complexes of trans geometry ?PtX.sub.2 (L)(L')! where at least L is a planar ligand such as pyridine but preferably quinoline and L' may be amine, sulfoxide or substituted sulfoxide and X is a chloride, nitrate or carboxylate.A process for obtaining bis(platinum) complexes where the two platinum coordination spheres may contain different ligands in each sphere and where the geometry of each platinum coordination sphere may be the same or different.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: June 23, 1998
    Assignee: The University of Vermont and State Agricultural College
    Inventor: Nicholas Farrell
  • Patent number: 5688784
    Abstract: There are provided vanadium compositions for use in the treatment of hypertension, obesity and diabetes, in particular improved oral compositions comprising oxovanadium (IV) chelates of monoprotic, bidentate oxygen, oxygen and oxygen, nitrogen coordinating ligands especially kojic acid and maltol.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 18, 1997
    Assignee: The University of British Columbia
    Inventors: John Hugh McNeill, Hamid Reza Hoveyda, Chris Orvig, Ying Zhou, Jere Douglas Fellmann
  • Patent number: 5637578
    Abstract: The present invention is directed to low molecular weight mimics of superoxide dismutase (SOD) represented by the formula: ##STR1## wherein R, R', R.sub.1, R'.sub.1, R.sub.2, R'.sub.2, R.sub.3, R'.sub.3, R.sub.4, R'.sub.4, R.sub.5, R'.sub.5, R.sub.6, R'.sub.6, R.sub.7, R'.sub.7, R.sub.8, R'.sub.8, R.sub.9, and R'.sub.9 and X, Y, Z and n are as defined herein, useful as therapeutic agents for inflammatory disease states and disorders, ischemic/reperfusion injury, stroke, atherosclerosis, hypertension and all other conditions of oxidant-induced tissue damage or injury.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: June 10, 1997
    Inventors: Dennis P. Riley, Randy H. Weiss, William L. Neuman, Anil S. Modak, Patrick J. Lennon, Karl W. Aston
  • Patent number: 5624919
    Abstract: Novel trans-platinum IV complexes which contain heterocycle ligands such as quinoline or isoquinoline, anionic ligands such as halide or sulfate, and which optionally may contain ammonia, or a primary or secondary amine are provided. These complexes have application as pharmaceuticals, in particular as anti-tumor agents.
    Type: Grant
    Filed: September 13, 1994
    Date of Patent: April 29, 1997
    Assignee: The University of Vermont and State Agricultural College
    Inventor: Nicholas Farrell
  • Patent number: 5620967
    Abstract: There are provided vanadium compositions for use in the treatment of hypertension, obesity and diabetes, in particular improved oral compositions comprising oxovanadium (IV) chelates of monoprotic, bidentate oxygen, oxygen and oxygen, nitrogen coordinating ligands especially kojic acid and maltol.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 15, 1997
    Assignee: The University of British Columbia
    Inventors: John H. McNeill, Hamid R. Hoveyda, Chris Orvig, Ying Zhou, Jere D. Fellmann
  • Patent number: 5541174
    Abstract: Disclosed herein are analgesic copper coordination compounds and a process for using them in the treatment of analgesia in animal bodies. The copper coordination compounds utilized are the reaction products of copper salts with:1. carboxylic acids or their alkaline earth salts;2. aromatic carboxylic acids or their alkaline earth salts;3. heterocyclic carboxylic acids or their alkaline earth salts;4. amino acids or their alkaline earth salts;5. anthranilic acids or their alkaline earth salts;6. salicylic acids or their alkaline earth salts;7. acetylsalicylates or their alkaline earth salts;8. arylacetic acids or their alkaline earth salts;9. disubstituted aminodithiocarbamates, and mixtures of any of the above.The process disclosed comprises administering to animals, orally or parenterally, in controlled dosages, the aforementioned copper coordination compounds.
    Type: Grant
    Filed: January 18, 1995
    Date of Patent: July 30, 1996
    Inventor: John R. J. Sorenson
  • Patent number: 5527790
    Abstract: There are provided vanadium compositions for use in the treatment of hypertension, obesity and diabetes, in particular improved oral compositions comprising oxovanadium (IV) chelates of monoprotic, bidentate oxygen, oxygen and oxygen, nitrogen coordinating ligands especially kojic acid and maltol.
    Type: Grant
    Filed: March 18, 1994
    Date of Patent: June 18, 1996
    Assignee: The University of British Columbia
    Inventors: John H. McNeill, Chris Orvig
  • Patent number: 5516503
    Abstract: A diagnostic composition comprising a binuclear complex between a polyaminopolycarboxylic ligand, such as diethylene triamine pentacetic acid, a paramagnetic metal such as Gd and an endogenous metal such as Ca, optionally mixed with the mononuclear complex of the same paramagnetic metal and the same ligand. This composition can be used as a contrasting agent in magnetic resonance imaging.
    Type: Grant
    Filed: November 7, 1994
    Date of Patent: May 14, 1996
    Assignee: Guerbet S.A.
    Inventors: Corinne Bourgouin, Gerard Desplanches, Michele Lecayon
  • Patent number: 5466692
    Abstract: This invention relates to substituted pyridopyrimidinones of general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, lower alkyl containing 1 to 6 carbon atoms, hydroxyalkyl containing 1 to 6 carbon atoms, formyl, carbonylalkyl containing 1 to 6 carbon atoms, carboxy, or carboxyalkyl containing 1 to 6 carbon atoms; R.sup.3 and R.sup.4 are independently H, lower alkyl containing 1 to 6 carbon atoms, hydroxy; R.sup.3a and R.sup.4a are H, and when taken together with R.sup.3 and R.sup.4 respectively comprise a carbonyl; with the proviso that at least one of the groups R1 and R.sup.2 must be hydroxyalkyl, formyl, carbonylalkyl containing 1 to 6 carbon atoms, carboxy, or carboxyalkyl containing 1 to 6 carbon atoms; or R.sup.3 and R.sup.4 must be hydroxy or taken together with R.sup.3a and R.sup.4a respectively must comprise a carbonyl; n is 0 to 3; Ar.sup.
    Type: Grant
    Filed: January 10, 1994
    Date of Patent: November 14, 1995
    Assignee: American Home Products Corporation
    Inventor: John W. Ellingboe
  • Patent number: 5451577
    Abstract: A composition which contains a 4,5-polymethylene-4-isothiazolin-3-one and a salt or complex of 2-mercaptopyridine-1-oxide with a metal which is at least divalent. The salt or complex is typically zinc 2-thiopyridine-1-oxide. The compositions exhibit anti-microbial activity and certain combinations of isothiazolinones together with zinc 2-thiopyridine-1-oxide are surprisingly effective against both bacteria and fungi.
    Type: Grant
    Filed: September 3, 1993
    Date of Patent: September 19, 1995
    Assignee: Zeneca Limited
    Inventor: Fraser F. Morpeth
  • Patent number: 5444093
    Abstract: Wood preservatives contain a copper salt, a polyamine and a fatty amine and are used for preserving wood from fungi and termites.
    Type: Grant
    Filed: November 3, 1993
    Date of Patent: August 22, 1995
    Assignee: Dr. Wolman GmbH
    Inventors: Reimer Goettsche, Hans-Volker Borck
  • Patent number: 5417959
    Abstract: The present invention provides new and structurally diverse compositions comprising compounds of the general formula: ##STR1## Wherein V is CR.sub.1 or N; W is CR.sub.2 or N; R.sub.1 and R.sub.2 may be the same or different and are hydrogen, C.sub.1 -C.sub.8 alkyl, or C.sub.6 -C.sub.10 aryl, optionally R.sub.1 and R.sub.2 may be substituted by one or more hydroxy, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.6 -C.sub.10 aryl, C.sub.6 -C.sub.10 hydroxyaryl, C.sub.6 -C.sub.10 aryloxy, --CO.sub.2 R.sub.3, CONR.sub.4 R.sub.5, or --NR.sub.4 R.sub.5 ; X and Y may be the same or different and the O, NR.sub.6, S, or CR.sub.7 R.sub.8 ; R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 may be the same or different and are hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl, or C.sub.1 -C.sub.8 alkoxyalkyl; R.sub.4 and R.sub.
    Type: Grant
    Filed: October 4, 1993
    Date of Patent: May 23, 1995
    Assignee: Mallinckrodt Medical, Inc.
    Inventor: Rebecca A. Wallace
  • Patent number: 5401770
    Abstract: An antipruritic agent comprising a zinc-amino acid complex, and an antipruritic composition containing said antipruritic agent at a concentration of 2.6.times.10.sup.-3 to 2.6.times.10.sup.-1 M.
    Type: Grant
    Filed: August 11, 1992
    Date of Patent: March 28, 1995
    Assignee: Shiseido Company Ltd.
    Inventors: Shigeru Taguchi, Miwako Inokuchi, Noriko Nakajima, Mie Inomata, Yasuo Naito
  • Patent number: 5393750
    Abstract: A compound of the general formula ##STR1## or a salt or complex thereof, in which X, Y and Z are all optionally substituted carbon atoms and R is hydrogen, optionally substituted hydrocarbyl or acyl or --COOR.sup.7 and R.sup.7 is hydrocarbyl has anti-microbial properties. Particular examples are compounds in which X is --CH.sub.2 -- or --C(CH.sub.3).sub.2 -- and Y and Z are both --CH.sub.2 -- or X is is --CH.sub.2 -- and Y and Z are carbon atoms of a benzene ring. The zinc complexes have useful properties.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: February 28, 1995
    Assignee: Zeneca, Limited
    Inventors: Mark R. James, Gordon A. Thomson
  • Patent number: 5358704
    Abstract: Novel compounds of the formula ##STR1## and metal chelates of the compounds are useful particularly for MRI of the hepatobiliary system.
    Type: Grant
    Filed: September 30, 1993
    Date of Patent: October 25, 1994
    Assignee: Bristol-Myers Squibb
    Inventors: Jean F. Desreux, Michael F. Tweedle, Peter C. Ratsep, Thomas R. Wagler, Edmund R. Marinelli
  • Patent number: 5348950
    Abstract: A platinum(II) complex represented by the general formula (A), ##STR1## in which R.sub.1 represents a hydrocarbon radical having 1 to 10 carbon atoms, R.sub.2 and R.sub.3 each represent a hydrogen atom or a hydrocarbon radical of 1 to 10 carbon atoms, or R.sub.2 and R.sub.3, together, may form --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --, and X and Y each represent an ammonia molecule or a monodentate amine having 1 to 7 carbon atoms or X and Y, together, may form a bidentate diamine having 2 to 10 carbon atoms. The compounds are useful for treating a tumor.
    Type: Grant
    Filed: June 5, 1992
    Date of Patent: September 20, 1994
    Assignee: Toray Industries, Inc.
    Inventors: Go Hata, Tatsuya Kaneko, Hideki Kawai, Masato Mutoh, Hideyuki Hashimoto
  • Patent number: 5334371
    Abstract: The macrocyclic compounds of the following formula I and IV, defined herein and their salts with inorganic and/or organic bases, amino acids or amino acid amides are valuable diagnostic and therapeutic agents.
    Type: Grant
    Filed: July 6, 1992
    Date of Patent: August 2, 1994
    Assignee: Schering Aktiengesellschaft
    Inventors: Heinz Gries, Bernd Raduchel, Johannes Platzek, Hanns-Joachim Weinmann, Wolf-Rudiger Press, Ulrich Speck
  • Patent number: 5324720
    Abstract: Inhibition of renal cancer, melanoma, colon cancer, lung cancer and leukemia cells by administration of compounds from the bafilomycin and hygrolidin groups of compounds.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: June 28, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Tom G. Holt, Richard L. Monaghan
  • Patent number: 5306716
    Abstract: Inhibition of renal cancer, melanoma, colon cancer, lung cancer and leukemia cells by administration of compounds from the bafilomycin and hygrolidin groups of compounds.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: April 26, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Tom G. Holt, Richard L. Monaghan
  • Patent number: 5302587
    Abstract: A novel platinum (II) complex represented by the following formula (A): ##STR1## wherein R.sub.1 represents C.sub.1 -C.sub.5 lower hydrocarbon group, R.sub.2 and R.sub.3 represents hydrogen atom or C.sub.1 -C.sub.3 lower hydrocarbon group, the configuration of 1,2-diaminocyclohexane being cis, trans-l- or trans-d-. Since the platinum (II) complex has a strong anti-tumor activity and its toxicity is low, it is useful as an agent for treating malignant tumor.
    Type: Grant
    Filed: September 9, 1991
    Date of Patent: April 12, 1994
    Assignee: Toray Industries, Inc.
    Inventors: Go Hata, Masato Mutoh, Hideyuki Hashimoto
  • Patent number: 5300496
    Abstract: A pharmaceutical composition useful for lowering blood sugar and suppressing appetite in mammals. The composition comprises compounds of a formula selected from VOL.sub.2 or VO(OR)L.sub.2 in which L is a bidentate monoprotic ligand and R is an organic group. The composition includes a pharmaceutically acceptable carrier. The invention also provides a method of lowering blood sugar and suppressing appetite in a mammal that comprises administering to the mammal a compound of the above formula.
    Type: Grant
    Filed: September 30, 1991
    Date of Patent: April 5, 1994
    Assignee: The University of British Columbia
    Inventors: John H. McNeill, Hamid R. Hoveyda, Chris Orvig
  • Patent number: 5292731
    Abstract: Compositions containing metal salts of methotrexate and methotrexate derivatives or analogs are disclosed. Such compositions comprise a metal salt, preferably a zinc salt, of methotrexate or a methotrexate derivative or analog and a carrier suitable for delivering the metal salt in the desired pharmacological form. Methods of treatment are also disclosed in which such compositions are topically applied or orally or parenterally administered to a patient. The metal salt is present in the treating composition in an amount sufficient to produce the desired therapeutic effect upon application or administration.
    Type: Grant
    Filed: July 21, 1992
    Date of Patent: March 8, 1994
    Assignee: Chemex Pharmaceuticals, Inc.
    Inventor: Bernard Loev
  • Patent number: 5283242
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.5 is hydrogen, alkyl of 1-6 carbon atoms, benzyl, triphenylmethyl, or Sn(alkyl of 1-6 carbon atoms).sub.3 ;n is 1 to 3;Y is ##STR5## wherein R.sup.3 is hydrogen, perfluoro alkyl of 1-6 carbon atoms, trifluoromethylalkyl of 1-6 carbon atoms, or alkyl of 1-6 carbon atoms; and R.sup.4 is hydrogen or alkyl of 1-6 carbon atoms;with the proviso that when R.sup.1 is ##STR6## then R.sup.2 cannot be ##STR7## wherein X is as defined above; and the pharmaceutically acceptable salts thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure.
    Type: Grant
    Filed: November 12, 1992
    Date of Patent: February 1, 1994
    Assignee: American Home Products Corporation
    Inventor: John W. Ellingboe
  • Patent number: 5256654
    Abstract: This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently H, lower alkyl containing 1 to 6 carbon atoms, or perfluoroalkyl containing 1 to 6 carbon atoms; R.sup.5 is H or when n is 1 R.sup.5 taken together with R.sup.3 comprises a double bond; n is 0 to 1; p is 0 to 2; m is 0 to 3; Ar.sup.1 is ##STR2## wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; Ar.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.6 is H, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereof which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension, congestive heart failure, and restenosis. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: October 26, 1993
    Assignee: American Home Products Corporation
    Inventors: John W. Ellingboe, Madelene Nikaido, Jehan Bagli
  • Patent number: 5248683
    Abstract: Compounds of the formula ##STR1## in which A.sub.1 and A.sub.2 independently of one another are CO--C.sub.1 -C.sub.4 alkyl, COO--C.sub.1 -C.sub.4 alkyl, CO--CF.sub.3, CO--N(R).sub.2 or cyano;A.sub.1 and A.sub.2 together are CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO, CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO which is substituted by C.sub.1 -C.sub.4 alkyl, COOR, CON(R).sub.2, cyano or phenyl, it being possible for the phenyl ring, in turn, to be substituted by halogen, methyl, trifluoromethyl, methoxy, nitro or cyano; CO--N(R)--CO--N(R)--CO;R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 alkynyl;X is oxygen, sulfur or N(CH.sub.3);X.sub.1, X.sub.2 and X.sub.3 independently of one another are hydrogen, halogen, methyl, methylthio, methoxy or nitro;n is 0 or 1;including the salts of the compounds of the formula I with agriculturally acceptable organic or inorganic bases, and including the metal complexes; have valuable microbicidal properties.
    Type: Grant
    Filed: June 4, 1992
    Date of Patent: September 28, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans-Georg Brunner, Walter Kunz, Rolf Schurter
  • Patent number: 5166149
    Abstract: Compositions containing metal salts of methotrexate and methotrexate derivatives or analogs are disclosed. Such compositions comprise a metal salt, preferably a zinc salt, of methotrexate or a methotrexate derivative or analog and a carrier suitable for delivering the metal salt in the desired pharmacological form. Methods of treatment are also disclosed in which such compositions are topically applied or orally or parenterally administered to a patient. The metal salt is present in the treating composition in an amount sufficient to produce the desired therapeutic effect upon application or administration.
    Type: Grant
    Filed: June 10, 1991
    Date of Patent: November 24, 1992
    Assignee: Chemex Pharmaceuticals, Inc.
    Inventor: Bernard Loev
  • Patent number: 5130308
    Abstract: A compound of the general formula: ##STR1## wherein R.sub.1 is hydrogen, a hydroxy group or a C.sub.2 -C.sub.6 alkanoyloxy group, R.sub.2 is hydrogen or a hologen atom, R.sub.3 is hydrogen or a C.sub.1 -C.sub.6 alkyl group, R.sub.4 is a hydroxy group or a C.sub.2 -C.sub.6 alkanoyloxy group, R.sub.5 is hydrogen or a hologen atom and R.sub.6 is hydrogen or a halogen atom, Alk is a C.sub.2 -C.sub.10 alkylene chain where 4 neighboring CH.sub.2 groups may also be replaced by a 1,4-phenylene ring, A-B is the group HN--CH.sub.2 --CH.sub.2 --NH.sub.2, H.sub.2 N--CH.sub.2 --CH--CH.sub.2 --NH.sub.2 or ##STR2## and R.sub.7 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a phenyl radical and X stands for the equivalent of a physiologically acceptable anion. The compound is useful for the treatment of hormone dependent tumors.
    Type: Grant
    Filed: June 7, 1990
    Date of Patent: July 14, 1992
    Assignee: Asta Pharma
    Inventors: Erwin von Angerer, Norbert Knebel, Helmut Schonenberger, Jurgen Engel
  • Patent number: 5082834
    Abstract: Disclosed herein are anti-inflammatory and anti-ulcer copper coordination compounds and a process for using them in the treatment of arthritis and gastrointestinal ulcers in animal bodies. The copper coordination compounds utilized are the reaction products of copper salts with:1. aromatic carboxylic acids or their alkaline earth salts;2. heterocyclic carboxylic acids or their alkaline earth salts;3. amino acids or their alkaline earth salts;4. amines; and5. suitably substituted steroids.The process disclosed comprises administering to experimental animals, orally or parentrally (subcutaneously), in controlled dosages, the aforementioned copper coordination compounds for the treatment of inflammation (i.e., arthritis) and ulcers of the gastrointestinal tract.
    Type: Grant
    Filed: September 18, 1990
    Date of Patent: January 21, 1992
    Inventor: John R. J. Sorensen
  • Patent number: 5002941
    Abstract: Compounds comprising pyridyl and phenyl substituted pyrrolo[1,2-a]imidazole derivatives and pyridyl and phenyl substituted imidazo[1,2-a]pyridine derivatives, pharmaceutical compositions containing said compounds, and their use as 5-lipoxygenase pathway inhibitors.
    Type: Grant
    Filed: October 11, 1988
    Date of Patent: March 26, 1991
    Assignee: SmithKline Beecham Corporation
    Inventors: Jerry L. Adams, Paul E. Bender, John G. Gleason, Nabil Hanna, John F. Newton, Jr., Carl D. Perchonock, Kazys Razgaitis
  • Patent number: 4999347
    Abstract: Disclosed herein are analgesic copper coordination compounds and a process for using them in the treatment of analgesia in animal bodies. The copper coordination compounds utilized are the reaction products of copper salts with:1. carboxylic acids or their alkaline earth salts;2. aromatic carboxylic acids or their alkaline earth salts;3. heterocyclic carboxylic acids or their alkaline earth salts;4. amino acids or their alkaline earth salts;5. anthranilic acids or their alkaline earth salts;6. salicyclic acids or their alkaline earth salts;7. acetylsalicylates or their alkaline earth salts;8. arylacetic acids or their alkaline earth salts;9. disubstituted aminodithiocarbamates, and mixtures of any of the above.The process disclosed comprises administering to animals, orally or parenterally, in controlled dosages, the aforementioned copper coordination compounds.
    Type: Grant
    Filed: October 20, 1989
    Date of Patent: March 12, 1991
    Inventor: John R. J. Sorenson
  • Patent number: 4997820
    Abstract: Novel macrocyclic compounds of the formual I ##STR1## where the dotted line in the 9,10-position is a saturated bond or a double bond, alternatively, and R is hydrogen, methyl or certain acyl radicals, and R.sub.o is hydrogen, halogen, azido, thiol, hydroxyl or --OY, where Y is, among other radicals, an ether radical, a silyl group, a sulfonyl group, a sugar radical or a (thiol)acyl radical, and R being methyl if there is a double bond in the 9,10-position, have microbicidal properties for the control of phytopathogenic microorganisms. They can be employed in the customary formulation for the control of plant disease.
    Type: Grant
    Filed: September 8, 1989
    Date of Patent: March 5, 1991
    Assignees: Gesellschaft fur Biotechnologische Forschung mbH, Ciba-Geigy Corporation
    Inventors: Marius Sutter, Norbert Bedorf, Gerhard Hofle, Dietmar Schummer, Bettina Bohlendorf
  • Patent number: 4980347
    Abstract: A platinum complex represented by the formula: ##STR1## where X is ##STR2## wherein R.sup.1 is a (C1-18) alkyl group, a (C1-18)alkenyl group or a group --Z--R.sup.4 in which Z is --CH.dbd.CH-- or a (C1-5)alkylene group, and R.sup.4 is a phenyl group, a hydroxyphenyl group, a (C7-12)alkoxyphenyl group, a halogenophenyl group, a nitrophenyl group, or (C8-13)alkoxycarbonylphenyl group, a cyclohexyl group having a (C1-5)alkyl substituent, ##STR3## R.sup.2 is hydrogen or a (C1-18)alkyl group, R.sup.3 is hydrogen or a (C1-3) alkyl group, R.sup.2 and R.sup.3 are linked together to form a (C2-7)alkylene group; the dotted line indicates that the bond may be either a single bond or a double bond; the chain line indicates a conjugated system; the 1,2-diaminocyclohexane moiety has a cis-, trans-l- or trans-d-configuration; and Y is an anion. This platinum complex is useful in the treatment of tumors.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: December 25, 1990
    Assignee: Toray Industries
    Inventors: Masaji Ohno, Masato Mutoh, Go Hata, Keiichi Matsunaga, Satoshi Hanada
  • Patent number: 4940586
    Abstract: A method for enhancing the transdermal flux of a transdermally deliverable drug through intact skin is described in which the drug is delivered simultaneously with sucrose monolaurate or a mixture of sucrose esters of coconut fatty acids, which is predominantly sucrose monolaurate. Preferred embodiments of therapeutic systems for delivering the drug and the sucrose ester employ a matrix containing drug at a concentration above saturation.
    Type: Grant
    Filed: October 13, 1988
    Date of Patent: July 10, 1990
    Assignee: Alza Corporation
    Inventors: Yu-Ling Cheng, Robert M. Gale, Edna Sugihara, Harold F. Sanders
  • Patent number: 4939254
    Abstract: A method is provided for a high yield template synthesis of macrocyclic catecholamide ligands.
    Type: Grant
    Filed: October 30, 1989
    Date of Patent: July 3, 1990
    Assignee: The Regents of the University of California
    Inventors: Thomas J. McMurry, Kenneth N. Raymond
  • Patent number: 4912100
    Abstract: A platinum complex represented by the formula: ##STR1## wherein R.sup.1 is a (Cl-18) alkyl group, a (Cl-18)-alkenyl group or a group ----X--R.sup.5 in which X is --CH.dbd.CH-- or a (Cl-5)alkylene group, and R.sup.5 is a phenyl group, a hydroxyphenyl group, a (C7-12) alkoxyphenyl group, a halogenophenyl group, a nitrophenyl group, or (C8-13)alkoxycarbonylphenyl group, a cyclohexyl group having a (Cl--5)alkyl substituent, ##STR2## R.sup.2 is a (Cl-18 alkyl group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 are linked together to form a (C2-7)alkylene group, R.sup.4 is OH or NO.sub.3 ; the dotted line indicates that the bond may be either a single bond or a double bond; the chain line indicates a conjugated system; n is a number of from 1 to 2, and the 1,2-diaminocyclohexane moiety has a cis-, trans-l- or trans-d-configuration. This platinum complex is useful in the treatment of tumors.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: March 27, 1990
    Assignee: Toray Industries, Inc.
    Inventors: Masaji Ohno, Masato Mutoh, Hisao Kondo, Keiichi Matsunaga
  • Patent number: 4877782
    Abstract: Zinc ceftiofur complexes, e.g., zinc ceftiofur hydrochloride and zinc ceftiofur sodium complexes, have been found to provide the good antibiotic activity of ceftiofur while providing low dissolution rate and long half-life properties enabling the formulation of improved long term therapy forms of ceftiofur, useful in antibiotic therapy of valuable warm-blooded animals. Pharmaceutical compositions of such zinc ceftiofur complexes and a method of using such zinc ceftiofur complexes in veterinary antibiotic applications are also provided.
    Type: Grant
    Filed: February 16, 1988
    Date of Patent: October 31, 1989
    Assignee: The Upjohn Company
    Inventors: Alexander R. Cazers, K. Thomas Koshy
  • Patent number: 4873226
    Abstract: A method is provided for inhibiting herpetic lesions associated with herpes virus infection in warm blooded animals comprising topically administering to any such warm blooded animal a lesion-inhibiting amount of antiherpes platinum coordination compound contained in a pharmaceutical composition in topical dosage form.
    Type: Grant
    Filed: July 19, 1985
    Date of Patent: October 10, 1989
    Assignee: Delta Metals, Inc.
    Inventors: Robert C. Talroy, Sarah G. Ward, Parbury P. Schmidt
  • Patent number: 4820716
    Abstract: 7-(1-Pyrrolidinyl)-3-quinolonecarboxylic acid derivatives of the formula ##STR1## in which A is CH, CCl, CF or N,R.sup.1 is hydroxyl, hydroxymethyl or mercapto andR.sup.2 is hydrogen, alkyl, having 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl,with the proviso that, when R.sup.1 is hydroxy, A is not CF or N, or pharmaceutically acceptable hydrates, or salts thereof, are useful as antibacterials and animal feed utilization promoters.
    Type: Grant
    Filed: February 12, 1987
    Date of Patent: April 11, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4760060
    Abstract: Carbacephem and cephem compounds represented by the formula: ##STR1## [Wherein X is S or CH.sub.2 ; n is an integer of 1 to 5; R.sub.1 is an unsubstituted or substituted heterocyclic group (where the heterocyclic group is a 5- or 6-membered heterocyclic group having 1 to 4 of O, S and N); R.sub.2 is a group represented by the formula: ##STR2## (where R.sub.4 is an unsubstituted or substituted phenyl or 2-aminothiazolyl) or a group represented by the formula: ##STR3## (where R.sub.5 is an unsubstituted or substituted lower alkyl); R.sub.3 is hydrogen, an alkali metal, an alkaline earth metal, an organic ammonium group or an ester residue, and R.sub.1 may be a quaternary ammonium group, where --CO.sub.2 R.sub.3 represents --CO.sub.2.sup.- ] have strong antibacterial activity against Gram-positive and Gram-negative bacteria, and are useful for treating various infections.
    Type: Grant
    Filed: November 15, 1985
    Date of Patent: July 26, 1988
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Kenichi Mochida, Takehiro Ogasa, Junichi Shimada, Tadahi Hirata, Kiyoshi Sato, Ryo Okachi
  • Patent number: 4758554
    Abstract: Copper-dependent enzymes are required for normal brain development and function. Copper deficiency can result in pathological disorders accompanied by convulsive seizures or tremors in man and animals. The present invention is directed to a method for treating convulsions or epilepsy comprising administration of a therapeutically effective amount of an organic compound of copper having anticonvulsant activity. Those compounds include copper complexes of carboxylic acids, acylsalicylates, salicylates, amino acids, imines and known anticonvulsant and antiepileptic drugs.
    Type: Grant
    Filed: December 8, 1986
    Date of Patent: July 19, 1988
    Assignee: International Copper Research Association
    Inventor: John R. J. Sorenson
  • Patent number: 4758555
    Abstract: Copper-dependent enzymes are required for normal brain development and function. Copper deficiency can result in pathological disorders accompanied by convulsive seizures or tremors in man and animals. The present invention is directed to a method for treating convulsions or epilepsy comprising administration of a therapeutically effective amount of an organic compound of copper having anticonvulsant activity. Those compounds include copper complexes of carboxylic acids, acylsalicylates, salicylates, amino acids, imines and known anticonvulsant and antiepileptic drugs.
    Type: Grant
    Filed: December 8, 1986
    Date of Patent: July 19, 1988
    Assignee: International Copper Research Association
    Inventor: John R. J. Sorenson
  • Patent number: 4757059
    Abstract: Copper-dependent enzymes are required for normal brain development and function. Copper deficiency can result in pathological disorders accompanied by convulsive seizures or tremors in man and animals. The present invention is directed to a method for treating convulsions or epilepsy comprising administration of a therapeutically effective amount of an organic compound of copper having anticonvulsant activity. These compounds include copper complexes of carboxylic acids, acylsalicylates, salicylates, amino acids, imines and known anticonvulsant and antiepileptic drugs.
    Type: Grant
    Filed: December 8, 1986
    Date of Patent: July 12, 1988
    Assignee: International Copper Research Association
    Inventor: John R. J. Sorenson
  • Patent number: 4694000
    Abstract: The invention relates to novel quinazoline and isoquinoline derivatives of the general formula: ##STR1## and acid addition salts and copper complexes thereof, wherein X represents nitrogen or a CH group,Y represents oxygen or an NH group,R.sub.1 and R.sub.2 represent hydrogen, alkyl(1-6 C), alkoxy (1-6 C), halogen or trifluoromethyl,R.sub.3 represents a substituted or unsubstituted 2-pyridyl group andR.sub.4 represents hydrogen, an alkyl(1-6 C) group unsubstituted or substituted by halogen, alkoxy (1-6 C) or phenyl groups, a cyclic alkyl group or a substituted or unsubstituted aromatic group.
    Type: Grant
    Filed: December 6, 1984
    Date of Patent: September 15, 1987
    Assignee: Akzo N.V.
    Inventors: Hendrik Timmerman, Henderikus Van der Goot
  • Patent number: 4657903
    Abstract: This invention relates to novel transition metal complexes of 2-acetyl- and -propionylpyridine thiosemicarbazones, their selenium analogs. These compounds are useful as antimalarial and antileukemic agents. Also disclosed are several synthetic procedures used to prepare the thiosemicarbazones and their selenium analogs.
    Type: Grant
    Filed: March 31, 1982
    Date of Patent: April 14, 1987
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: John P. Scovill, Daniel L. Klayman, Charles F. Franchino
  • Patent number: 4652558
    Abstract: Compounds of the formula: ##STR1## wherein X is independently halogen, lower alkyl of 1 to 6 carbon atoms, lower alkoxy of 1 to 6 carbon atoms, nitro, lower alkylsulfinyl of 1 to 6 carbon atoms, lower alkylthio of 1 to 6 carbon atoms, amino or trifluoromethyl; n is 0, 1, 2 or 3; R is hydrogen, alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, lower alkenyl of 2 to 6 carbon atoms, or lower alkynyl of 2 to 6 carbon atoms, all optionally substituted with 1 to 3 of the same or different halogen atoms; or aryl of 6 to 12 carbon atoms; or substituted aryl substituted with 1 to 3 substituents independently selected from lower alkyl of 1 to 4 carbon atoms, lower alkoxy of 1 to 4 carbon atoms, and the group --S(O).sub.k R.sup.2 where k is 0, 1 or 2 and R.sup.2 is lower alkyl of 1 to 4 carbon atoms, nitro, cyano or halogen; and R.sup.1 is lower alkyl of 1 to 6 carbon atoms, lower cycloalkyl of 3 to 8 carbon atoms or aryl of 6 to 12 carbon atoms, provided that R and R.sup.
    Type: Grant
    Filed: February 27, 1986
    Date of Patent: March 24, 1987
    Assignee: Chevron Research Company
    Inventor: Laroy H. Edwards
  • Patent number: 4608371
    Abstract: The present invention provides novel insecticidal carbamate derivatives. The invention also provides a method for the control of insects.
    Type: Grant
    Filed: March 11, 1985
    Date of Patent: August 26, 1986
    Assignee: American Cyanamid Company
    Inventors: Narayana M. Mallipudi, John G. Hollingshaus
  • Patent number: 4571335
    Abstract: A method is provided for inhibiting herpetic lesions associated with herpes virus infection in warm blooded animals comprising topically administering to any such warm blooded animal a lesion-inhibiting amount of antiherpes platinum coordination compound contained in a pharmaceutical composition in topical dosage form.
    Type: Grant
    Filed: June 17, 1983
    Date of Patent: February 18, 1986
    Inventors: Robert C. Taylor, Sarah G. Ward, Parbury P. Schmidt
  • Patent number: 4532233
    Abstract: An antibacterial 7.beta.-(fluorinated methylthioacetamido)-7.alpha.-methoxy-3-(1-hydroxyalkyl-5-tetrazolyl)thiom ethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid and its derivatives at the carboxy or hydroxyalkyl represented by the following formula: ##STR1## wherein, R is FCH.sub.2 -- or F.sub.2 CH--; R.sup.1 is R.sup.3 O-substituted-alkyl in which R.sup.3 is hydrogen or a hydroxy-protecting group; and R.sup.2 is a hydrogen or light metal atom or a carboxy-protecting group, antibacterial drugs containing it, its use and production.
    Type: Grant
    Filed: December 22, 1983
    Date of Patent: July 30, 1985
    Assignee: Shionogi & Co., Ltd.
    Inventors: Teruji Tsuji, Hisao Sato, Yoshio Hamashima