Oxygen Containing Hetero Ring Patents (Class 514/99)
  • Patent number: 5709890
    Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.
    Type: Grant
    Filed: March 20, 1997
    Date of Patent: January 20, 1998
    Assignee: Donlar Corporation
    Inventor: J. Larry Sanders
  • Patent number: 5698541
    Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: December 16, 1997
    Assignee: Boehringer Mannheim GmbH
    Inventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
  • Patent number: 5670493
    Abstract: A compound of formula (I): ##STR1## in which: R.sub.1, R.sub.2, which may be identical or different, represent hydrogen or halogen, or alkyl, alkoxy, nitro or trihalomethyl,X represents CO, SO.sub.2 or CH.sub.2,A.sub.1 represents any one of the groups as defined in the description,A.sub.2 represents --(CH.sub.2).sub.n or --CH.dbd.CH--,R.sub.3, R.sub.4, which may be identical or different, represent hydrogen or alkyl,its isomers as well as its addition salts with a pharmaceutically acceptable base and medicinal product containing the same are useful as angiogenesis inhibitors.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: September 23, 1997
    Assignee: Adir et Compagnie
    Inventors: Alex Cordi, Patrice Desos, Angela D. Morris, Ghanem Atassi
  • Patent number: 5658897
    Abstract: The present invention relates to cyclopentane (or cyclopentane) heptanoic or cyclopentane (or cyclopentene) heptenoic acid, 2-hydrocarbyl phosphinyloxyalkyl or phosphonamidoalkyl, 1-esters, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.
    Type: Grant
    Filed: April 8, 1996
    Date of Patent: August 19, 1997
    Assignee: Allergan
    Inventor: Robert M. Burk
  • Patent number: 5646133
    Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.
    Type: Grant
    Filed: March 14, 1996
    Date of Patent: July 8, 1997
    Assignee: Donlar Corporation
    Inventor: J. Larry Sanders
  • Patent number: 5626883
    Abstract: A vitamin C supplement comprising ascorbic acid, ascorbyl palmitate, niacinamide ascorbate, calcium ascorbate, magnesium ascorbate, potassium ascorbate, and sodium ascorbate which together can be administered to a human to avoid the transitory initial suppression of human NK cell activity which is present when ascorbic acid alone is administered. Also included is xylitol, lysine acetate, tetrasodium pyrophosphate, ribose, cysteine, and hesperidin which further prolongs the biological activity of ascorbic acid and promotes the uptake of ascorbic acid by human tissue.
    Type: Grant
    Filed: April 15, 1994
    Date of Patent: May 6, 1997
    Assignee: Metagenics, Inc.
    Inventor: Stephen M. Paul
  • Patent number: 5545631
    Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.3 are hydrogen.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: August 13, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Christian Marescaux, Raymond Bernasconi, Markus Schmutz, Wolfgang Fr ostl, Stuart J. Mickel
  • Patent number: 5545647
    Abstract: 3-Phenylpyrrolidine compounds of the formula ##STR1## effectively inhibit phosphodiesterase (PDE) IV activities and can be used as medicaments for conditions such as asthma.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: August 13, 1996
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Toshihiko Tanaka, Akihiro Yamamoto, Akira Amenomori
  • Patent number: 5527789
    Abstract: A method of combatting cancer in a subject comprising administering to said subject dehydroepiandrosterone (DHEA) or an analog thereof in an amount effective to combat cancer is disclosed in which heart failure induced by the DHEA or analog thereof is combatted by administering to the subject a ubiquinone, in an amount effective to combat heart failure induced by the DHEA or analog thereof.A prefered DHEA analog for carrying out the invention is 16 alpha-fluoroepiandrosterone, and a preferred ubiquinone for carrying out the invention is Coenzyme Q.sub.10.
    Type: Grant
    Filed: August 2, 1994
    Date of Patent: June 18, 1996
    Assignee: East Carolina University
    Inventor: Jonathan W. Nyce
  • Patent number: 5474995
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases, ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: January 10, 1994
    Date of Patent: December 12, 1995
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Yves Ducharme, Jacques Y. Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
  • Patent number: 5472956
    Abstract: Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 21, 1994
    Date of Patent: December 5, 1995
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, James P. Schmidt
  • Patent number: 5451573
    Abstract: Substituted cyclohexane derivatives for the treatment of diseases Esters of cyclohexane derivatives of the formula I ##STR1## in which A--B, R.sup.3, R.sup.4, R.sup.5, Y and Z have the meanings indicated, for use as inhibitors of the glucose-6-phosphatase system of the liver in mammals are described. The compounds are suitable for the production of pharmaceutical preparations.
    Type: Grant
    Filed: September 7, 1993
    Date of Patent: September 19, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Horst Hemmerle, Peter Schindler, Roland Utz, Robert Rippel, Andreas Herling
  • Patent number: 5436245
    Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##
    Type: Grant
    Filed: November 17, 1993
    Date of Patent: July 25, 1995
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Patent number: 5428058
    Abstract: There are disclosed compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, alkyl, cycloalkyl, arylalkyl, --(CH.sub.2).sub.r CH.dbd.CH.sub.2, --(CH.sub.2).sub.s OY, --(CH.sub.2).sub.t CH(OZ)CH.sub.3, or Ar;X is O, S, or NR.sup.2 ;Y and Z are each, independently, hydrogen, alkyl, or --COR.sup.3 ;R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, or arylalkyl;Ar is an aryl radical that may be optionally substituted;m=1-5;n=0-1;p=1-9;r=0-6;s=2-6; andt=0-6or a pharmaceutically acceptable salt thereof which are useful as antiinflammatory agents.
    Type: Grant
    Filed: September 28, 1994
    Date of Patent: June 27, 1995
    Assignee: American Home Products Corporation
    Inventor: Dominic R. Mobilio
  • Patent number: 5409912
    Abstract: A new compound, which we have named Leustroducsin H, has formula (I): ##STR1## and pharmaceutically acceptable salts thereof. This compound may be prepared by hydrolysis of naturally occurring Leustroducsins and the compound may be used for the treatment or prophylaxis of thrombocytopenia.
    Type: Grant
    Filed: April 8, 1994
    Date of Patent: April 25, 1995
    Assignee: Sankyo Company, Limited
    Inventors: Yukio Sugimura, Tomoyuki Shibata, Kazuhiko Tamaki, Shinwa Kurihara, Takafumi Kohama, Akio Shiraishi, Tomowo Kobayashi, Kazuhiko Sasagawa, Naomi Shimazaki
  • Patent number: 5407922
    Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.
    Type: Grant
    Filed: May 3, 1993
    Date of Patent: April 18, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Christian Marescaux, Raymond Bernasconi, Markus Schmutz, Wolfgang Frostl, Stuart J. Mickel
  • Patent number: 5405841
    Abstract: The invention relates to new phosphorylated aza compounds, to processes for their preparation and to their use as pesticides, in particular as soil-acting insecticides and nematicide.The new compounds have the general formula (I) ##STR1## in which R.sup.1 -R.sup.5, X and Y are defined as in the specification, with the exception of compound O-ethyl S-propyl 3-(6-chloro-3-pyridinylmethyl)-2-nitroimino-imidazolidine-1-thiophosphate.
    Type: Grant
    Filed: November 30, 1993
    Date of Patent: April 11, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Jurgen Hartwig, Christoph Erdelen
  • Patent number: 5374628
    Abstract: Phosphonic acid squalene synthetase inhibitors are provided which are effective in lowering serum cholesterol and have the formula ##STR1## wherein m is 0 to 3, n is 1 to 5, Y.sup.1 and Y.sup.2 are H or halogen, R.sup.2, R.sup.3 and R.sup.4 are H, metal ion, C.sub.1 to C.sub.8 alkyl, C.sub.3 to C.sub.12 alkenyl, or prodrug ester, and R.sup.1 is a substituted or unsubstituted heteroaryl group or a substituted phenyl group.
    Type: Grant
    Filed: October 18, 1993
    Date of Patent: December 20, 1994
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Scott A. Biller
  • Patent number: 5338730
    Abstract: A process for preparing the (R) stereoisomer of 2,2-bis(hydroxmethyl)-tetrahydrofuran monobutyrate comprising subjecting the dibutyric ester of the 2,2-bis(hydroxymethyl)-tetrahydrofuran to enzymatic hydrolysis. The invention also relates to the novel (R) stereoisomer prepared by the instant process and to its more stable forms. In addition, the invention relates to the use of the (R) stereoisomer in preparing stereoisomers of pharmacologically active compounds and to certain specific stereoisomers produced thereby.
    Type: Grant
    Filed: June 4, 1993
    Date of Patent: August 16, 1994
    Assignee: Sandoz Ltd.
    Inventors: Heinrich Estermann, Prasad K. Kapa, Russell L. Underwood, William J. Houlihan
  • Patent number: 5334587
    Abstract: New compounds, which we have named the "Leustroducsins" have the formula (I): ##STR1## in which R represents a 5-methylhexanoyloxy group, a 6-methyloctanoyloxy group or a 7-methyloctanoyloxy group, and salts thereof, and may be prepared by fermentation using a microorganism of the genus Streptomyces, especially a strain of the species Streptomyces platensis, such as strain SANK 60191 (FERM BP-3288). These compounds may be used for the treatment or prophylaxis of: adverse reactions resulting from cancer chemotherapy or radiotherapy; infections; cancer; cerebral dysfunction; and fungal infections.
    Type: Grant
    Filed: March 25, 1992
    Date of Patent: August 2, 1994
    Assignee: Sankyo Company, Limited
    Inventors: Takafumi Kohama, Isao Kaneko, Takemichi Nakamura, Takeshi Kagasaki, Ryuzo Enokita, Keiichi Matsuda
  • Patent number: 5314881
    Abstract: Phosphomycin and pharmaceutically acceptable salts thereof topically used as cicatrizing agents.
    Type: Grant
    Filed: February 18, 1993
    Date of Patent: May 24, 1994
    Assignees: Nunzio Rapisarda, Francia Farmaceutici Industria Farmaco-Biologica S.R.L., Salvatore Pignataro
    Inventor: Nunzio Rapisarda
  • Patent number: 5284836
    Abstract: The invention discloses certain heterocyclic, thioether, keto-ester and alkyl phospholipids, e.g., heterocyclic phospholipids having the formula ##STR1## where R is n-C.sub.14 -C.sub.20 alkyl or O-n-C.sub.14 -C.sub.20 alkyl; each R.sub.1 is methyl or ethyl; n is 2-6; and X is --CH.sub.2 --m, where m is 2-4, CH.sub.2 CH.sub.2 O or CH.sub.2 CH.sub.2 S, or a corresponding hydrate thereof, which compounds are useful in treating multiple sclerosis.
    Type: Grant
    Filed: December 4, 1992
    Date of Patent: February 8, 1994
    Assignee: Sandoz Ltd.
    Inventor: William J. Houlihan
  • Patent number: 5260287
    Abstract: Compositions and methods for protecting the luminal lining against gastric acid challenge are disclosed. The compositions provide effective anti-ulcer preparations which include phosphorylated alcohol. Phosphorylated alcohols comprise the active anti-ulcerogenic ingredient of the described therapeutic formulations. The preparation of unique linear and cyclic polyphosphorylated alcohols and methods of using same to protect the stomach luminal lining against acid challenge are also disclosed. Inositol hexaphosphate and mannitol hexaphosphate are demonstrated to provide therapeutic value in the treatment and prevention of gastro-erosive disease precipitated by exposure of biological tissues to highly acidic substances, for example, the gastric digestive acids. While inositol hexaphosphate alone at subthreshold concentrations provides a small gastro-protective activity, a combination of inositol hexaphosphate (at subthreshold concentrations) with polyvalent cations, such as Au.sup.+3 or Bi.sup.
    Type: Grant
    Filed: May 11, 1992
    Date of Patent: November 9, 1993
    Assignee: Board of Regents, The University of Texas System
    Inventors: Jose C. Barreto, Lenard M. Lichtenberger
  • Patent number: 5256653
    Abstract: Platinum complexes of the general formula I[(R.sup.1 NH.sub.2).sub.n Pt].sub.q Y.sub.m X.sub.p (I)in which Y is a phosphonic acid ligand, and the preparation thereof, are described. The platinum complexes are suitable as active substances in pharmaceuticals, in particular for controlling cancers.
    Type: Grant
    Filed: March 26, 1991
    Date of Patent: October 26, 1993
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Bernhard Keppler, Helmut Blum
  • Patent number: 5250522
    Abstract: The present invention relates to the N-phosphonomethyl-biaryl substituted amino acid derivatives of formula I ##STR1## wherein X represents a direct bond, C.sub.1-4 -alkylene or C.sub.2 -C.sub.4 -alkenylene; R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, .alpha.-(trichloromethyl, carboxyl, esterified carboxyl or amidated carboxyl)substituted-(lower alkyl or aryl-lower alkyl), acyloxymethyl optionally monosubstituted on methyl carbon by C.sub.1-20 -alkyl, by C.sub.5 -C.sub.7 -cycloalkyl, by aryl or by aryl-lower alkyl; R.sub.1 represents monocyclic carbocyclic or monocyclic heterocyclic aryl; COR.sub.3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; R.sub.2 and R.sub.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: October 5, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Stephane De Lombaert
  • Patent number: 5229377
    Abstract: A process for preparing the (R) stereoisomer of 2,2-bis(hydroxmethyl)-tetrahydrofuran monobutyrate comprising subjecting the dibutyric ester of the 2,2-bis(hydroxymethyl)-tetrahydrofuran to enzymatic hydrolysis. The invention also relates to the novel (R) stereoisomer prepared by the instant process and to its more stable forms. In addition, the invention relates to the use of the (R) stereoisomer in preparing stereoisomers of pharmacologically active compounds and to certain specific stereoisomers produced thereby.
    Type: Grant
    Filed: April 26, 1991
    Date of Patent: July 20, 1993
    Assignee: Sandoz Ltd.
    Inventors: Heinrich Estermann, Prasad K. Kapa, Russell L. Underwood, William J. Houlihan
  • Patent number: 5229375
    Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: July 20, 1993
    Assignee: Scripps Clinic and Research Foundation
    Inventors: Peter E. Maligres, Kyriacos C. Nicolaou
  • Patent number: 5229378
    Abstract: Presented are a glycyrrhetic acid derivative of the following formula ##STR1## or a pharmacologically acceptable salt thereof, which has antioxidant, antiinflammatory and/or antiallergic activity, a process for producing said compound or salt, and an antioxidant, antiinflammatory and/or antiallergic composition comprising said compound or salt.
    Type: Grant
    Filed: March 10, 1992
    Date of Patent: July 20, 1993
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Kyouzo Yamamoto, Reiko Matsuda
  • Patent number: 5190929
    Abstract: Cyclophosphamides possessing anti-tumor activity and having the formula ##STR1## and salts thereof; wherein R is lower alkyl, aryl, aryl-lower alkyl or a nitrogen, sulfur or oxygen containing heterocyclic or heterocyclic lower alkyl, andR' is hydrogen, hydroxy or OOH with the proviso that when R' is hydrogen, R is other than methyl or phenyl and when R' is hydroxy, R is other than methyl.
    Type: Grant
    Filed: May 25, 1988
    Date of Patent: March 2, 1993
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, Gregory W. Canute
  • Patent number: 5190930
    Abstract: Araliphatylaminoalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is an aromatically substituted aliphatic radical, R.sub.2 is hydrogen or a monovalent aliphatic radical and alk is a divalent aliphatic radical, and their salts, exhibit a pronounced regulatory action on the calcium metabolism and can be used as medicaments for the treatment of diseases that are attributable to calcium metabolsim disorders. They are prepared, for example, by reacting a compound of formula ##STR2## wherein X.sub.3 is carboxy and R.sub.0 is a radical R.sub.2, with phosphorous acid and phosphorus trichloride and hydrolysing the primary product.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: March 2, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Knut A. Jaeggi
  • Patent number: 5190933
    Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.
    Type: Grant
    Filed: March 3, 1992
    Date of Patent: March 2, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Eric K. Baylis, Ludwig Maier, Stuart J. Mickel, Hans-Rudolf Olpe, Helmut Bittiger, Wolfgang Frostl, Roger G. Hall
  • Patent number: 5182271
    Abstract: The invention discloses certain thioether, keto-ester and alkyl phospholipids which are useful in treating multiple sclerosis.
    Type: Grant
    Filed: August 30, 1991
    Date of Patent: January 26, 1993
    Assignee: Sandoz Ltd.
    Inventor: William J. Houlihan
  • Patent number: 5162309
    Abstract: A process is described for the preparation of mono (2-ammonium-2-hydroxymethyl-1,3-propanediol) (2R,cis)-1,2-epoxypropyl-phosphonate with improved characteristics of stability, of processing for the preparation of pharmaceutical forms and of stability of the pharmaceutical forms that contain it.
    Type: Grant
    Filed: July 25, 1990
    Date of Patent: November 10, 1992
    Assignee: Zambon Group
    Inventors: Dario Tentorio, Graziano Castaldi, Claudio Giordano, Franco Pozzi
  • Patent number: 5155100
    Abstract: The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.
    Type: Grant
    Filed: May 1, 1991
    Date of Patent: October 13, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Mark D. Erion, Stephane De Lombaert
  • Patent number: 5145990
    Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.2- C.sub.12 linear or branched unsubstituted alkyl; C.sub.1- C.sub.12 linear or branched substituted alkyl; C.sub.2 -C.sub.12 linear or branched monoalkenyl; C.sub.2 -C.sub.12 linear or branched alkynyl; C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein these values for R.sub.1, other than C.sub.2- C.sub.12 linear or branched unsubstituted alkyl, can be substituted by one or more of C.sub.1 -C.sub.4 alkoxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, C.sub.6- C.sub.12 aryloxy, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.10 aralkyloxy, C.sub.7- C.sub.16 aralkyl-thio; and R.sub.5 is H or C.sub.1- C.sub.12 linear or branched alkyl; C.sub.2- C.sub.12 linear or branched monoalkenyl; C.sub.7- C.sub.
    Type: Grant
    Filed: January 9, 1991
    Date of Patent: September 8, 1992
    Assignee: Merck & Co., Inc.
    Inventors: William H. Parsons, William R. Schoen, Arthur A. Patchett
  • Patent number: 5143716
    Abstract: Methods of providing an image of the gastrointestional region of a patient and diagnosing the presence of any tumorous tissue in that region using contrast media comprising a combination of at least one polyphosphorylated aliphatic or polyphosphorylated alicyclic compound and at least one paramagnetic ion, wherein the aliphatic and alicyclic compounds comprise at least five carbon atoms, is described. Also described are diagnostic kits for gastrointestinal imaging which include the subject contrast media.
    Type: Grant
    Filed: February 1, 1991
    Date of Patent: September 1, 1992
    Inventor: Evan C. Unger
  • Patent number: 5098898
    Abstract: Phospholipid derivatives resulting from coupling of ascorbic acid to a glycerol ester or ether via a phosphoric acid residue and having antioxidant activity and lipid peroxide inhibiting activity, which have the formula ##STR1## wherein R.sup.1 and R.sup.2 represent the same or different and each represents an alkyl or acyl group and neither formula represents any particular configuration nor conformation.
    Type: Grant
    Filed: December 27, 1990
    Date of Patent: March 24, 1992
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Kyozo Yamamoto, Takahiro Matsumoto
  • Patent number: 5090995
    Abstract: Disclosed is an agricultural chemical composition in the form of an aqueous suspension, which comprises fine particles of a water-insoluble physiologically active substance having a melting point of 15.degree. to 70.degree. C., which are stably dispersed in water by a water-soluble or water-dispersible polymer comprising at least one monomer selected from the group consisting of unsaturated carboxylic acids and derivatives thereof as the indispensable component, as a dispersant, and a phthalic acid ester as an agent for preventing precipitation of crystals.In this agricultural chemical composition, the phthalic acid ester bleeds on the surface of the physiologically active substance to modify the surface, and the storage stability of the composition in the form of a suspension is highly improved.
    Type: Grant
    Filed: June 13, 1988
    Date of Patent: February 25, 1992
    Assignees: Mitsui Toatsu Chemicals, Inc., Kao Corporation
    Inventors: Yutaka Kubota, Seiichi Shimono, Tetsuo Yanami, Tetsuji Iwasaki, Kazuhiko Kurita
  • Patent number: 5089485
    Abstract: New furanone compounds have anti-inflammatory, immunosuppressive and anti-proliferative activity and are useful in treating psoriasis and modifying calcium homeostasis. A compound of the invention is 4-(1-thioacetoxytridecyl-5-hydroxy-2(5H)-furanone.
    Type: Grant
    Filed: October 25, 1989
    Date of Patent: February 18, 1992
    Assignee: Allergan, Inc.
    Inventor: Gary C. M. Lee
  • Patent number: 5064816
    Abstract: invention relates to heterocyclic phospholipids of formula III which are useful in treating multiple sclerosis:where R .sub.2 is n-C.sub.14 -C.sub.20 alkyl;each R.sub.1, independently, is methyl or ethyl; Y is --O-- or --S--;n is an integer 2 to 6.
    Type: Grant
    Filed: June 5, 1990
    Date of Patent: November 12, 1991
    Assignee: Sandoz Ltd.
    Inventor: William J. Houlihan
  • Patent number: 5055471
    Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.
    Type: Grant
    Filed: November 15, 1989
    Date of Patent: October 8, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: Paul J. de Fraine, Anne Martin
  • Patent number: 5037811
    Abstract: Compounds of the formula ##STR1## in which R.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.1.sup.* CO--O--R.sub.1.sup.* CO--NH--R.sub.1.sup.* or PO(OR.sub.1.sup.*).sub.2 or PO(OR.sub.1.sup.*)R.sub.1.sup.* where R.sub.1.sup.* independently is H, alkyl of 1 to 20 carbons, phenyl, or substituted phenyl; X is O, S, SO--, SO.sub.2, NH--, or NR.sub.2 where R.sub.2 is phenyl, substituted phenyl or alkyl of 1 to 20 carbons, and Y is alkyl having at least 6 carbon atoms, arylalkyl, aryl, substituted aryl, substituted arylalkyl, alkenyl containing one or more olephinic bonds and at least 6 carbon atoms, CO--R.sub.3, CO--OR.sub.3, CONHR.sub.3, SO.sub.2 R.sub.3, SO.sub.2 NHR.sub.3 where R.sub.3 is aryl, substituted aryl, substituted arylalkyl, alkyl, alkenyl containing one or more olephinic bonds, further Y is (CH.sub.2).sub.n --O--R.sub.4, or (CH.sub.2).sub.n --O--(CH.sub.2).sub.m --O--R.sub.4, where n, and m, are integers and are independently 1 to 25 and R.sub.
    Type: Grant
    Filed: April 17, 1990
    Date of Patent: August 6, 1991
    Assignee: Allergan, Inc.
    Inventor: Gary C. M. Lee
  • Patent number: 5021406
    Abstract: A 2-pyranone derivative represented by the formula (I): ##STR1## wherein R represents a hydrogen atom, or a linear, branched alkylcarbonyloxy, or cyclo-alkylcarbonyloxy group having 3 to 10 carbon atoms, and salts thereof; a process for the production of the above-mentioned 2-pyranone derivative (I), comprising the steps of culturing a microorganism belonging to the genus Streptomyces and capable of producing the derivative, to produce the derivative, and recovering the produced derivative from the cultured product; a biocidal composition comprising the above-mentioned 2-pyranone derivative (I); and a microorganism belonging to the genus Stretromyces and capable of producing the above-mentioned 2-pyranone derivatives.
    Type: Grant
    Filed: February 13, 1989
    Date of Patent: June 4, 1991
    Assignee: Suntory Limited
    Inventors: Mitsuru Maeda, Tohru Kodama, Sumio Asami, Norihide Amano, Takaaki Kusumi, Hidekazu Hosono
  • Patent number: 5013725
    Abstract: Substituted aminomethylenebis(phosphonic acid) derivatives represented by the general formula: ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be the same or different, each represents a hydrogen atom or a lower alkyl group; "m" is zero or represents an integer from 1 to 4; and a ring "A" represents a cycloalkenyl group having 5 to 8 carbon atoms, a bicycloheptyl group, a bicycloheptenyl group or a saturated heterocyclic group having 4 to 7 carbon atoms and containing an oxygen atom, a sulfur atom, a sulfinyl group (--SO--) or a sulfonyl group (--SO.sub.2 --), or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 16, 1990
    Date of Patent: May 7, 1991
    Inventors: Yasuo Isomura, Makoto Takeuchi, Shuichi Sakamoto, Tetsushi Abe
  • Patent number: 4977146
    Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group, Y is an alkyl or substituted alkyl group, R.sup.6 is an alkyl or a substituted alkyl group and the substituents at positions 3, 4 or 5 are acyclic.
    Type: Grant
    Filed: April 11, 1990
    Date of Patent: December 11, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Mitree M. Ponpipom, Nirindar N. Girotra
  • Patent number: 4963538
    Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.
    Type: Grant
    Filed: March 13, 1989
    Date of Patent: October 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman
  • Patent number: 4956355
    Abstract: Compounds of the general Formula (I) ##STR1## in which R is a hydrogen atom or a bromine atom, and R.sub.1 is a hydrogen atom, an SO.sub.2 OM group wherein M is a hydrogen or sodium atom, various sulphatide or phosphatide groups or a glucuronide group are disclosed for use in the prophylaxis and therapy of retroviral infections, especially infection by Human Immunodeficiency Virus. These compounds may be used concomitantly or in combination with various immunomodulators and/or antiviral agents.
    Type: Grant
    Filed: April 15, 1988
    Date of Patent: September 11, 1990
    Assignee: Colthurst Limited
    Inventor: Patrick T. Prendergast
  • Patent number: 4939128
    Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, carboxylic acid acyl or carbamoyl which may be substituted; R is an aliphatic hydrocarbon group which may be substituted or alicylic hydrocarbon group which may be substituted, or a salt thereof.The compound of the present invention has the effects to prevent and improve dysfunctions caused by oxygen free radicals, and can be used as preventive and therapeutic drugs against dysfunctions in the circulatory system.
    Type: Grant
    Filed: April 5, 1989
    Date of Patent: July 3, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Norio Shimamoto
  • Patent number: 4897402
    Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by stuctural formulae (I) and (II): ##STR1## wherein A is O, S(O).sub.n or N--R.sub.13.
    Type: Grant
    Filed: June 29, 1988
    Date of Patent: January 30, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman
  • Patent number: 4880790
    Abstract: Organic platinum complexes active as anti-tumor agents in warm-blooded animals, and methods for synthesis of same, are described.
    Type: Grant
    Filed: January 31, 1986
    Date of Patent: November 14, 1989
    Assignee: American Cyanamid Company
    Inventors: Ralph G. Child, Panayota Bitha, Joseph J. Hlavka, Yang-I Lin