Patents by Inventor Jaap van der Louw

Jaap van der Louw 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: 8124647
    Abstract: This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula or a salt or hydrate form thereof.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: February 28, 2012
    Assignee: N.V. Organon
    Inventors: Pedro Harold Han Hermkens, Herman Thijs Stock, Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse
  • Publication number: 20110065768
    Abstract: This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula or a salt or hydrate form thereof.
    Type: Application
    Filed: September 3, 2010
    Publication date: March 17, 2011
    Inventors: PEDRO HAROLD HAN HERMKENS, HERMAN THIJS STOCK, JAAP VAN DER LOUW, NEELTJE MIRANDA TEERHUIS, JOHANNES PETRUS MARIA LOMMERSE
  • Publication number: 20110009428
    Abstract: The compounds of the subject invention have a structure according to formula I: wherein X is S or SO2; R1 is (1C-6C)alkyl, (3C-6C)alkenyl, or (3C-6C)alkynyl, each optionally substituted with (3C-6C)cycloalkyl, OH, OC(O)(1C-4C)alkyl, (1C-4C)alkoxy, halogen, cyano, formyl, C(O)(1C-4C)alkyl, CO2H, CO2(1C-4C)alkyl, C(O)NR5R6, S(O)(1C-4C)alkyl or S(O)2(1C-4C)alkyl; R2 is hydrogen, (1C-4C)alkyl or C(O)(1C-4C)alkyl; R3 is a phenyl group optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, (1C-4C)fluoroalkoxy, halogen, cyano or nitro; or R3 is a 5- or 6-membered aromatic heterocyclic ring structure optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, halogen or cyano; R4 is a phenyl group or an aromatic 6-membered heterocycle, substituted at the ortho position with 1-hydroxy(1C-4C)alkyl, (1C-4C)alkoxy, C(O)(1C-4C)alkyl, CO2(1C-4C)alkyl, C(O)NH2, cyano, nitro, or CH?NOR7, and optionally further substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; or R4
    Type: Application
    Filed: September 22, 2010
    Publication date: January 13, 2011
    Applicant: N.V. Organon
    Inventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
  • Patent number: 7812036
    Abstract: The compounds of the subject invention have a structure according to formula I: wherein each of the substituents is given the definition as set forth in the specification and claims, or a salt or hydrate form thereof.
    Type: Grant
    Filed: April 21, 2005
    Date of Patent: October 12, 2010
    Assignee: N.V. Organon
    Inventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
  • Patent number: 7795280
    Abstract: This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula or a salt or hydrate form thereof.
    Type: Grant
    Filed: November 3, 2003
    Date of Patent: September 14, 2010
    Assignee: N.V. Organon
    Inventors: Pedro Harold Han Hermkens, Herman Thijs Stock, Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse
  • Publication number: 20090291929
    Abstract: The invention provides for compounds having formula (1) wherein; R1 is O, (H,H), (H,OH), or NOR, with R being hydrogen, (C1-6) alkyl or (C1-6) acyl; R2 is hydrogen, methyl, ethyl, or ethenyl; R3 is hydrogen, methyl, ethyl, ethenyl, fluoro, or chloro; R4 is methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, ethyl, (C1-3) alkenyl, or (C1-3) alkynyl; R7 is hydrogen or (C1-15) acyl; and at least one of R5 or R6 is hydrogen; or a pharmaceutically acceptable salt thereof, for use as medicine for a treatment to increase androgen levels, for androgen supplementation, for testosterone replacement and for benign prostate hypertrophy and in a method of male contraception, preferably as sole means to achieve both progestagenic sterilitant effect and androgen supplementation.
    Type: Application
    Filed: June 16, 2006
    Publication date: November 26, 2009
    Applicant: N.V. ORGANON
    Inventors: Jaap Van Der Louw, Dirk Leysen, Marcel Evert De Gooijer, Joseph Maria Gerardus Barbara Cals
  • Patent number: 7582622
    Abstract: The invention provides 19-nor-D-homosteroids, having a mixed androgenic/progestagenic profile, which are orally active, prevent trabecular bone mineral density (BMD) loss, and which lack liver toxicity, having a structure according to the formula (I) wherein, R1 is O, or NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl, R2 is methyl or ethyl, and R3 is hydrogen or (C1-15)acyl.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: September 1, 2009
    Assignee: N.V. Organon
    Inventors: Jaap Van Der Louw, Dirk Leysen, Arij Jan Grootenhuis, Marcel Evert De Gooijer
  • Publication number: 20070225352
    Abstract: The compounds of the subject invention have a structure according to formula I: wherein each of the substituents is given the definition as set forth in the specification and claims, or a salt or hydrate form thereof.
    Type: Application
    Filed: April 21, 2005
    Publication date: September 27, 2007
    Applicant: Pharmacopela Drug Discovery, Inc.
    Inventors: Jaap Van Der Louw, Neeltje Teerhuis, Johannes Lommerse, Herman Stock, Pedro Hermkens
  • Publication number: 20070155836
    Abstract: This invention provides 19-nor-D-homos-teroids, having a mixed androgenic/progestagenic profile, which are orally active, prevent trabecular bone mineral density (BMD) loss, and which lack liver toxicity, having a structure according to the formula (I) wherein, R1 is O, or NOR, with R being hydrogen, (C1-6)alkyl or (C1-6)acyl, R2 is methyl or ethyl, and R3 is hydrogen or (C1-15)acyl.
    Type: Application
    Filed: December 15, 2004
    Publication date: July 5, 2007
    Applicant: AKZO NOBEL N.V.
    Inventors: Jaap Van Der Louw, Dirk Leysen, Arii Grootenhuis, Marcel De Gooijer
  • Patent number: 7169769
    Abstract: This invention relates to steroidal compounds having the formula I wherein: R1 is O, (H,H), (H,OH), NOH, whereby OH is optionally etherified or esterified; R2 and R3 are independently hydrogen or (C1-4) alkyl and at least one of R2 and R3 is (C1-4) alkyl; R4 is hydrogen, or (C1-15) acyl for use in androgen-related treatments, such as androgen insufficiency and male or female contraception.
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: January 30, 2007
    Assignee: Akzo Nobel N.V.
    Inventors: J Jaap Van Der Louw, D Dirk Leysen, M.E. Marcel Evert De Gooijer
  • Publication number: 20060128722
    Abstract: This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula or a salt or hydrate form thereof.
    Type: Application
    Filed: November 3, 2003
    Publication date: June 15, 2006
    Applicant: Akzo Nobel N.V.
    Inventors: Pedro Hermkens, Herman Stock, Jaap Van Der Louw, Neeltje Teerhuis, Johannes Lommerse
  • Patent number: 7037916
    Abstract: Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl.
    Type: Grant
    Filed: January 10, 2003
    Date of Patent: May 2, 2006
    Assignee: Pharmacopeia Drug Discovery, Inc.
    Inventors: Shawn David Erickson, John J. Baldwin, Roland Ellwood Dolle, III, 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
  • Patent number: 6949531
    Abstract: Disclosed are androgenic steroids of the (14?,17?)-17-(hydroxymethyl) type. The invention relates to an improvement thereof, which is based on the presence of a ?-oriented, annellated cyclopropyl group which includes carbon atoms 16 and 17 of the steroid skeleton, i.e. a 16,17?-methylene moiety. These steroids show an unexpectedly high androgenic potency.
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: September 27, 2005
    Assignee: Akzo Nobel N.V.
    Inventors: Jaap Van Der Louw, Dirk Leysen, Marcel Evert De Gooijer
  • Patent number: 6881728
    Abstract: Androgenic steroids having a (14?,17?-)-17-(hydroxymetheyl) configuration, useful for the preparation of male contraceptives and pharmaceutical formulations for the treatment of androgen insufficiency.
    Type: Grant
    Filed: March 2, 2000
    Date of Patent: April 19, 2005
    Assignee: Akzo Nobel N.V.
    Inventors: Hubert Jan Jozef Loozen, Dirk D. Leysen, Jaap van der Louw
  • Publication number: 20040259849
    Abstract: This invention relates to steroidal compounds having the formula (I), wherein: R1 is O, (H,H), (H,OH), NOH, whereby OH is optionally etherified or esterified; R2 and R3 are independently hydrogen or (C1-4) alkyl and at least one of R2 and R3 is (C1-4) alkyl; R4 is hydrogen, or (C1-15) acyl for use in androgen-related treatments, such as androgen insufficiency and male or female contraception.
    Type: Application
    Filed: March 11, 2004
    Publication date: December 23, 2004
    Inventors: J Jaap Van Der Louw, D Dirk Leysen, M.E. Marcel Evert De Gooijer
  • 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
  • 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