Patents by Inventor Filippus J. Zeelen

Filippus J. Zeelen has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4330539
    Abstract: New and pharmacologically useful 17-amino-16-hydroxy-steroids of the androstane and oestrane series are disclosed having the formula I: ##STR1## and pharmaceutically acceptable non-toxic acid addition salts thereof, wherein:R.sub.1 =H or hydrocarbyl of one to six carbon atoms (preferably lower alkyl, such as methyl);R.sub.2 =H or hydrocarbyl of one to six carbon atoms (preferably lower alkyl, such as methyl);R.sub.3 =a free, esterified or etherified hydroxyl group;ring A inclusive carbon atoms 6 and 9 has one of the following configurations: ##STR2## in which R.sub.4 =a free, esterified or etherified hydroxyl group;R.sub.5 =O or H(R.sub.7), wherein R.sub.7 is a free, esterified or etherified hydroxyl group;R.sub.6 =H or methyl; andthe dotted lines represent an optional double bond in 4,5- or 5,6-position;as well as the enantiomers and racemates of these steroids.The novel compounds have antiarrhythmic properties.
    Type: Grant
    Filed: January 29, 1981
    Date of Patent: May 18, 1982
    Assignee: Akzo nv
    Inventors: Thomas Sleigh, David S. Savage, Filippus J. Zeelen
  • Patent number: 4330540
    Abstract: New and pharmacologically useful ent-16-amino-17-hydroxy-oestra-1,3,5(10)-trienes are disclosed having the formula I: ##STR1## and pharmaceutically acceptable non-toxic acid addition salts thereof, wherein:n=1 or 2, preferably 1R.sub.1 =H or hydrocarbyl of 1 to 6 carbon atoms (preferably lower alkyl, such as methyl);R.sub.2 =H or hydrocarbyl of 1 to 6 carbon atoms (preferably lower alkyl, such as methyl); orR.sub.1 and R.sub.2 together is alkylene of 4 or 5 carbon atoms;R.sub.3 =a free, esterified or etherified hydroxyl group; andR.sub.4 =a free, esterified or etherified hydroxyl group.The novel compounds have antiarrhythmic properties.
    Type: Grant
    Filed: January 29, 1981
    Date of Patent: May 18, 1982
    Assignee: Akzo N.V.
    Inventor: Filippus J. Zeelen
  • Patent number: 4232042
    Abstract: The invention relates to novel compounds of general formula I: ##STR1## and salts, esters and amides thereof, in which R.sub.1 and R.sub.2 represent hydrogen, alkyl or alkenyl (1-4 C),R.sub.3 represents hydrogen, halogen, hydroxy, alkyl (1-4 C) or alkoxy (1-4 C),n has the value 0, 1 or 2 andALK is a saturated or unsaturated hydrocarbon radical with 3-12 carbon atoms, in which a straight carbon chain in between the benzene rings is present, containing 3-8 carbon atoms, andthe dotted line indicates an optional extra bond between the first and second carbon counted from the phenyl ring, in case of an extra bond the group R.sub.2 and one hydrogen attached to said second carbon being absent, having valuable hypocholesterolaemic and hypotriglyceriolaemic properties.
    Type: Grant
    Filed: October 4, 1976
    Date of Patent: November 4, 1980
    Assignee: Akzona Incorporated
    Inventors: Alexander C. Campbell, Colin L. Hewett, Filippus J. Zeelen
  • Patent number: 4222940
    Abstract: There are disclosed substrates of the formula: ##STR1## wherein: (a) R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;(b) R.sub.2 is H or C.sub.1 -C.sub.4 alkyl with the proviso that R.sub.1 is H when R.sub.2 is alkyl, and with the proviso that R.sub.2 is H when R.sub.1 is alkyl;(c) R.sub.3 is a leaving group including hydroxy, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkoxalkoxy, C.sub.1 -C.sub.7 acyloxy, and trialkylsilyloxy of less than fifteen carbons; and(d) R.sub.5(1) and R.sub.5(2) are each H, C.sub.1 -C.sub.8 alkyl, or an optionally esterified or etherified hydroxy group including hydroxy, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkoxyalkoxy, C.sub.1 -C.sub.15 trialkylsilyloxy, C.sub.4 -C.sub.8 cycloalkoxy, C.sub.1 -C.sub.7 carboxyacyloxy, or unsubstituted heterocyclic ether of five to seven members, with the proviso that at least one of R.sub.5(1) and R.sub.5(2) is hydrogen.
    Type: Grant
    Filed: October 23, 1978
    Date of Patent: September 16, 1980
    Assignee: Akzona Incorporated
    Inventors: Filippus J. Zeelen, Arnoldus I. A. Broess
  • Patent number: 4221713
    Abstract: Cyclisation substrates are disclosed of the formula: ##STR1## wherein: (a) R.sub.1 is H or alkyl of one to four carbon atoms;(b) R.sub.2 is H or alkyl of one to four carbon atoms, with the proviso that R.sub.1 is H when R.sub.2 is alkyl, and with the proviso that R.sub.2 is H when R.sub.1 is alkyl;(c) R.sub.3 is a suitable leaving group selected from the group consisting of hydroxy, alkoxy of one to four carbons, alkoxyalkoxy of two to four carbons, acyloxy of one to about seven carbon atoms, and trialkylsilyloxy of less than fifteen carbons;(d) R.sub.4 is methyl; and(e) R.sub.5(1) and R.sub.
    Type: Grant
    Filed: October 23, 1978
    Date of Patent: September 9, 1980
    Assignee: Akzona Incorporated
    Inventors: Filippus J. Zeelen, Marinus B. Groen
  • Patent number: 4186142
    Abstract: Novel cyclization substrates of the formula: ##STR1## wherein: (a) R.sub.1 is H or alkyl of one to four carbons;(b) R.sub.2 is H or alkyl of one to four carbons, with the proviso that R.sub.1 is H when R.sub.2 is alkyl; and with the proviso that P.sub.2 is H when R.sub.1 is alkyl;(c) R.sub.3 is a leaving group selected from the group consisting of OH, alkoxy of one to four carbons, alkoxyalkyoxy of from two to about four carbons, acyloxy of from about one to about seven carbons, and trialkylsilyloxy;(d) R.sub.4 is halogen, alkoxy of from one to four carbons, hydrocarbyl of from one to about four carbons, hydrocarbyl of from one to about four carbons substituted by one or more (1) halogens or (2) alkoxy moieties of from one to two carbons; and(e) R.sub.5 is H, alkyl of one to six carbons, hydroxy, or an esterified or estherified moiety of (1) less than eight carbons selected from the group consisting of alkoxy, trialkylsilyloxy, aralkyloxy, cyclo-alkoxy, and heterocyclo-oxy radicals; (2) .alpha.
    Type: Grant
    Filed: February 22, 1978
    Date of Patent: January 29, 1980
    Assignee: Akzona Incorporated
    Inventors: Filippus J. Zeelen, Marinus B. Groen
  • Patent number: 4177197
    Abstract: Novel cyclization substrates are disclosed of the formula ##STR1## wherein: (a) R.sub.1 is H or alkyl of one to four carbon atoms;(b) R.sub.2 is H or alkyl of one to four carbon atoms, with the proviso that R.sub.1 is H when R.sub.2 is alkyl, and with the proviso that R.sub.2 is H when R.sub.1 is alkyl;(c) R.sub.3 is a leaving group selected from the group consisting of hydroxy, alkoxy of one to four carbons, alkoxyalkoxy of two to four carbons, acyloxy of one to about seven carbons, and trialkylsilyloxy of less than fifteen carbons;(d) R.sub.4 is hydrocarbyl of one to four carbon atoms, a hydrocarbyl of one to two carbon atoms substituted by halogen or alkoxy of one to two carbons, or alkoxy of one to four carbon atoms; and(e) R.sub.5 and R.sub.5 ' each are H, OH, alkyl, trialkylsilyloxy, or an esterified or etherified hydroxy-group of about one to ten carbon atoms.
    Type: Grant
    Filed: February 22, 1978
    Date of Patent: December 4, 1979
    Assignee: Akzona Inc.
    Inventors: Filippus J. Zeelen, Marinus B. Groen