Patents by Inventor Dirk Leysen

Dirk Leysen 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: 6780854
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C,1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: October 24, 2002
    Date of Patent: August 24, 2004
    Assignee: Akzo Nobel NV
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 6756366
    Abstract: Orally Active androgens are derivative of 7&agr;-methyl-19-nortestosterone. The compounds satisfy formula (I) wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl; R2 is selected from the group consisting of (C2-3)alkyl, isopropyl, (C2-3)1-alkenyl, isopropenyl, 1,2-proandienyl, or (C2-3)1-alynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2)alkyl, or halogen; R3 is hydrogen, (C1-2)alkyl, or ethenyl; R4 is (C1-2)alkyl; R5 is hydrogen, or (C1-15)acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: June 29, 2004
    Assignee: Akzo Nobel N.V.
    Inventors: Jaap van der Louw, Dirk Leysen, Roberta Burma Bursi
  • Publication number: 20040087601
    Abstract: Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed.
    Type: Application
    Filed: January 10, 2003
    Publication date: May 6, 2004
    Inventors: Shawn David Erickson, John J. Baldwin, Roland Ellwood Dolle, James Inglese, Michael H.J. Ohlmeyer, Koc-Kan Ho, Adolph C. Bohnstedt, Steven G. Kultgen, Paolo Giovanni Martino Conti, Dirk Leysen, Jaap van der Louw
  • Publication number: 20040059140
    Abstract: Disclosed are androgen-related steroids having a &Dgr;14 double bond and carrying a substituent at either or both of the carbon atoms nos. 15 and 16. The present steroids are characterized by possessing a mixed profile of androgenic and progestagenic activities. This makes these compounds suitable for male or female hormone replacement therapy, as well as male contraception.
    Type: Application
    Filed: October 1, 2003
    Publication date: March 25, 2004
    Inventors: Japp Van Der Louw, Dirk Leysen, Marcel Evert De Gooyer
  • Patent number: 6706700
    Abstract: The disclosed invention relates to the unexpected finding of novel steroids which are characterized by a 14&bgr;,15&bgr;-cyclopropane ring and a 17&agr; hydroxymethyl group. These steroids according to the invention are found to have in common an androgenic activity. They can be used for the preparation of an agent for male contraception, as well as for the preparation of a medicament for the treatment of androgen insufficiency.
    Type: Grant
    Filed: September 11, 2002
    Date of Patent: March 16, 2004
    Assignee: Akzo-Nobel, N.V.
    Inventors: Dirk Leysen, Jaap Van der Louw, Roberta Buma Bursi, Marcel Evert De Gooyer
  • Publication number: 20040030165
    Abstract: Disclosed are androgenic steroids of the (14&bgr;,17&agr;)-17-(hydroxymethyl) type. The invention relates to an improvement hereof, which is based on the presence of a &x3B2;-oriented, annellated cyclopropyl group which includes carbon atoms 16 and 17 of the steroid skeleton, i.e. a 16,17&bgr;-methylene moiety. These steroids show an unexpectedly high androgenic potency.
    Type: Application
    Filed: June 11, 2003
    Publication date: February 12, 2004
    Inventors: Jaap Van Der Louw, Dirk Leysen, Marcel Evert De Gooijer
  • Publication number: 20030100543
    Abstract: The disclosed invention relates to the unexpected finding of novel steroids which are characterized by a 14&bgr;,15&bgr;-cyclopropane ring and a 17&agr; hydroxymethyl group. These steroids according to the invention are found to have in common an androgenic activity. They can be used for the preparation of an agent for male contraception, as well as for the preparation of a medicament for the treatment of androgen insufficiency.
    Type: Application
    Filed: September 11, 2002
    Publication date: May 29, 2003
    Inventors: Dirk Leysen, Jaap Van der Louw, Roberta Buma Bursi, Marcel Evert De Gooyer
  • Publication number: 20030087886
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives.
    Type: Application
    Filed: October 24, 2002
    Publication date: May 8, 2003
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 6552011
    Abstract: The invention relates to (androst-5-en-17beta-yl)alkylsulfoxides and sulfones having general formula (I), wherein R1, R2, R3, X and Y are defined in the specification. The compounds of the invention have meiosis inhibiting activity and can be used for the control of fertility.
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: April 22, 2003
    Assignee: Akzo Nobel NV
    Inventors: Dirk Leysen, Jaap van der Louw, Anja Wiersma
  • Patent number: 6541465
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: July 31, 2001
    Date of Patent: April 1, 2003
    Assignee: Akzo Nobel N.V.
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 6437158
    Abstract: The invention is drawn to (7a, 17b)-7-methyl-17-(1-oxoundecyl)oxy-estr-4-en-3-one, (MENT undecanoate), their pharmaceutical formulation and method of use is described. Unexpected results of the said compound compared with testosterone undecanoate is disclosed.
    Type: Grant
    Filed: December 18, 2000
    Date of Patent: August 20, 2002
    Assignee: Akzo Nobel N.V.
    Inventors: Dirk Leysen D., Hendrikus Adrianus Antonius Van Der Voort H.A.A
  • Patent number: 6403573
    Abstract: The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N,O and S and which may be substituted with oxo or (1-6C) alkyl; R1, R2 and R3 are independently H, (1-6C) alkyl, (1-6C) alkoxy,(1-6C) alkoxy-(1-6C) alkyl, carbo(1-6C) alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrrolidin and 3-(5,6,7,8-tetrahydro-napth-1-yl-oxy)-pyrrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.
    Type: Grant
    Filed: May 30, 2001
    Date of Patent: June 11, 2002
    Assignee: Akzo Nobel N.V.
    Inventors: Dirk Leysen, Johannes Hubertus Wieringa, Christophorus Louis Eduard Broekkamp
  • Publication number: 20020040016
    Abstract: The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2 and R3 are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy-(1-6C)alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrrolidin and 3-(5,6,7,8-tetrahydro-napth-1-yl-oxy)-pyrrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.
    Type: Application
    Filed: May 30, 2001
    Publication date: April 4, 2002
    Inventors: Dirk Leysen, Johannes Hubertus Wieringa, Christophorus Louis Eduard Broekkamp
  • Publication number: 20020022609
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives.
    Type: Application
    Filed: July 31, 2001
    Publication date: February 21, 2002
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 6313139
    Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
    Type: Grant
    Filed: July 22, 1999
    Date of Patent: November 6, 2001
    Assignee: Akzo Nobel N. V.
    Inventors: Fredericus Antonius Dijcks, Dirk Leysen, Joannes Theodorus Maria Linders, Gerardus Stephanus Franciscus Ruigt, Ian Craig Carlyle, Simon James Anthony Grove, Duncan Robertson Rae, Simon N. Thorn
  • Patent number: 6313108
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: July 11, 2000
    Date of Patent: November 6, 2001
    Assignee: Akzo Nobel N.V.
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 6281243
    Abstract: The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2 and R3 are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy(1-6C)-alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrolidin and 3-(5,6,7,8-tetmhydro-naphth-1-yl-oxy)-pyrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.
    Type: Grant
    Filed: August 21, 2000
    Date of Patent: August 28, 2001
    Assignee: Akzo Nobel N.V.
    Inventors: Dirk Leysen, Johannes Hubertus Wieringa, Christophorus Louis Eduard Broekkamp
  • Patent number: 6080773
    Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
    Type: Grant
    Filed: October 14, 1997
    Date of Patent: June 27, 2000
    Assignee: Akzo Nobel, N.V.
    Inventors: Fredericus Antonius Dijcks, Dirk Leysen, Joannes Theodorus Maria Linders, Gerardus Stephanus Franciscus Ruigt, Ian Craig Carlyle, Simon James Anthony Grove, Duncan Robertson Rae, Simon N. Thorn
  • Patent number: 5994366
    Abstract: The present invention relates to certain tetrahydroimidazo[2,1-a]isoquinoline derivatives according to formula I wherein X is a group (A) or (B) ##STR1## R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent one or more substituents selected from hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.4-6 cycloalkenyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl and halogen;R.sup.4, R.sup.5, R.sup.6 and R.sup.7, which may be the same or different, are each selected from hydrogen, C.sub.1-6 alkoxyC.sub.1-6 alkyl, C.sub.4-6 cycloalkenyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl and C.sub.1-6 alkyl; n is 1 or 2; or a pharmaceutically acceptable salt or solvate thereof, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.
    Type: Grant
    Filed: June 25, 1998
    Date of Patent: November 30, 1999
    Assignee: Akzo Nobel NV
    Inventors: Dirk Leysen, Gerardus Stephanus Franciscus Ruigt
  • Patent number: 5430063
    Abstract: The invention concerns a phenoxyphenyl compound having the formula ##STR1## wherein R is one or two halogen atoms; andA is CH.sub.2 NR.sub.1 R.sub.2 or 4,5-dihydro-1H-imidazole, in which R.sub.1 and R.sub.2 are independently selected from hydrogen and lower alkyl; ora pharmaceutically acceptable salt thereof.The compounds have long half-lives and can be used against depression.
    Type: Grant
    Filed: February 3, 1993
    Date of Patent: July 4, 1995
    Assignee: Akzo N.V.
    Inventors: Gerardus S. F. Ruigt, Dirk Leysen, Johannes H. Wieringa