Patents by Inventor Willem J. van der Burg

Willem J. van der Burg 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: 4333935
    Abstract: New and pharmacologically useful tetracyclic compounds are disclosed of the formula (I): ##STR1## and pharmaceutically acceptable non-toxic salts therefor, wherein: (a) R is hydrogen, alkyl of one to six carbons, aralkyl of seven to ten carbons, or an acyl group of one to six carbons;(b) R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, alkyl of one to six carbons, alkoxy of one to six carbons, alkythio of one to six carbons, or trifluromethyl; and(c) R.sub.5 represents hydrogen or an alkyl group of one to six carbons;as well as compositions containing these active compounds and methods of using same. The compounds of the instant invention have a remarkable pharmacological profile--one which clearly indicates the presence of anxiolytic properties with little or no sedative activity. The compounds according to the invention thus possess relatively specific anti-anxiety properties.
    Type: Grant
    Filed: March 27, 1981
    Date of Patent: June 8, 1982
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4284559
    Abstract: New and pharmacologically useful tetracyclic compounds are disclosed of the formula (I): ##STR1## and pharmaceutically acceptable non-toxic salts therefor, wherein: (a) R is hydrogen, alkyl of one to six carbons, aralkyl of seven to ten carbons, or an acyl group of one to six carbons;(b) R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, alkyl of one to six carbons, alkoxy of one to six carbons, alkythio of one to six carbons, or trifluoromethyl; and(c) R.sub.5 represents hydrogen or an alkyl group of one to six carbons;as well as compositions containing these active compounds and methods of using same. The compounds of the instant invention have a remarkable pharmacological profile--one which clearly indicates the presence of anxiolytic properties with little or no sedative activity. The compounds according to the invention thus possess relatively specific anti-anxiety properties.
    Type: Grant
    Filed: September 21, 1979
    Date of Patent: August 18, 1981
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4271177
    Abstract: The invention relates to novel dibenzo[1,2;5,6] cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7] oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7] thiepino pyridine or pyrrole derivatives and dibenzo[b,f] pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,m is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: June 26, 1978
    Date of Patent: June 2, 1981
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4271179
    Abstract: The invention relates to novel dibenzo[1,2;5,6]cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7]oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7]thiepino pyridine or pyrrole derivatives and dibenzo[b,f]pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,m is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: June 26, 1978
    Date of Patent: June 2, 1981
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4271178
    Abstract: The invention relates to novel dibenzo[1,2;5,6] cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7] oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7] thiepino pyridine or pyrrole derivatives and dibenzo[b,f] pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,m is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: June 26, 1978
    Date of Patent: June 2, 1981
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4224321
    Abstract: Novel and biologically active tetracyclic compounds are disclosed of the formula: ##STR1## or a pharmaceutically acceptable non-toxic salt thereof, wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, halogen, or trifluoromethyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; and X is oxygen or methylene. Pharmaceutical compositions containing these compounds are disclosed to take advantage of CNS-inhibiting properties thereof, especially sedative and tranquillizing properties.
    Type: Grant
    Filed: September 23, 1977
    Date of Patent: September 23, 1980
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4177275
    Abstract: The invention relates to novel dibenzo[1,2;5,6]cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7]oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7]thiepino pyridine or pyrrole derivatives and dibenzo[b,f]pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, R.sub.2, R.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,m is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: June 26, 1978
    Date of Patent: December 4, 1979
    Assignee: Akzona Inc.
    Inventor: Willem J. van der Burg
  • Patent number: 4158059
    Abstract: The invention relates to novel dibenzo[1,2;5,6] cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7] oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7] thiepino pyridine or pyrrole derivatives and dibenzo[b,f] pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, r.sub.2, r.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,M is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: June 23, 1978
    Date of Patent: June 12, 1979
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4158058
    Abstract: The invention relates to novel dibenzo[1,2;5,6]cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7]oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7]thiepino pyridine or pyrrole derivatives and dibenzo[b,f]pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, r.sub.2, r.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,M is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## OR THE GROUP --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: June 26, 1978
    Date of Patent: June 12, 1979
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4154836
    Abstract: The invention relates to novel dibenzo[1,2;5,6]cyclohepta pyridine or -pyrrole derivatives, dibenzo[2,3;6,7]oxepino pyridine or pyrrole derivatives, dibenzo[2,3;6,7]thiepino pyridine or pyrrole derivatives and dibenzo[b,f]pyrido or pyrrolo azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, r.sub.2, r.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,M is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C),having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: June 23, 1978
    Date of Patent: May 15, 1979
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg
  • Patent number: 4145434
    Abstract: The invention relates to novel dibenzo?1,2;5,6! cyclophepta pyridine or -pyrrole derivatives, dibenzo?2,3;6,7! oxepino pyridine or pyrrole derivatives, dibenzo?2,3;6,7! thiepino pyridine or pyrrole derivatives and dibenzo?b,f! pyrido or pyrrole azepine derivatives of general formula: ##STR1## as well as the pharmaceutically acceptable salts and nitrogen oxides thereof, whereinR.sub.1, r.sub.2, r.sub.3 and R.sub.4 each represent hydrogen, hydroxy, halogen, an alkyl (1-6 C) group, an alkoxy or alkylthio group in which the alkyl group contains 1-6 C-atoms, or a trifluoromethyl group,R.sub.5 represents hydrogen, an alkyl group with 1-6 carbon atoms or an aralkyl group with 7-10 carbon atoms,M is the number 1 or 2,X represents oxygen, sulphur, the group ##STR2## or the group --CH.sub.2 -- and R.sub.6 represents hydrogen or a lower alkyl group (1-4 C), having CNS-depressant activity and excellent antihistamine and antiserotonin activities.
    Type: Grant
    Filed: May 18, 1977
    Date of Patent: March 20, 1979
    Assignee: Akzona Incorporated
    Inventor: Willem J. VAN DER Burg
  • Patent number: 4125718
    Abstract: The invention discloses novel compounds of the general formula: ##STR1## and salts thereof, in which X stands for oxygen, sulphur, the group >NR.sub.7 or the group --CR.sub.8 R.sub.9 --;R.sub.1, r.sub.2, r.sub.3 and R.sub.4 represent hydrogen, hydroxy, halogen, alkyl (1-6 C), alkoxy (1-6 C), alkylthio (1-6 C) or trifluoromethyl;R.sub.5 and R.sub.6 represent hydrogen, alkyl (1-6 C), aralkyl (7-10 C) or together in combination with the nitrogen atom a heterocyclic five- or six-membered ring;R.sub.7 stands for hydrogen or alkyl (1-4 C);R.sub.8 and R.sub.9 stand for hydrogen or methyl,n is the number 0, 1 or 2 andThe dotted line means an optional C--C bond,With valuable central nervous system (CNS) activities, especially antidepressant activity.
    Type: Grant
    Filed: November 15, 1977
    Date of Patent: November 14, 1978
    Assignee: Akzona Incorporated
    Inventor: Willem J. van der Burg