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).
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Patent number: 8124647Abstract: 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: GrantFiled: September 3, 2010Date of Patent: February 28, 2012Assignee: N.V. OrganonInventors: Pedro Harold Han Hermkens, Herman Thijs Stock, Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse
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Publication number: 20110065768Abstract: 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: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Inventors: PEDRO HAROLD HAN HERMKENS, HERMAN THIJS STOCK, JAAP VAN DER LOUW, NEELTJE MIRANDA TEERHUIS, JOHANNES PETRUS MARIA LOMMERSE
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Publication number: 20110009428Abstract: 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 R4Type: ApplicationFiled: September 22, 2010Publication date: January 13, 2011Applicant: N.V. OrganonInventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
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Patent number: 7812036Abstract: 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: GrantFiled: April 21, 2005Date of Patent: October 12, 2010Assignee: N.V. OrganonInventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
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Patent number: 7795280Abstract: 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: GrantFiled: November 3, 2003Date of Patent: September 14, 2010Assignee: N.V. OrganonInventors: Pedro Harold Han Hermkens, Herman Thijs Stock, Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse
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Publication number: 20090291929Abstract: 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: ApplicationFiled: June 16, 2006Publication date: November 26, 2009Applicant: N.V. ORGANONInventors: Jaap Van Der Louw, Dirk Leysen, Marcel Evert De Gooijer, Joseph Maria Gerardus Barbara Cals
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Patent number: 7582622Abstract: 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: GrantFiled: December 15, 2004Date of Patent: September 1, 2009Assignee: N.V. OrganonInventors: Jaap Van Der Louw, Dirk Leysen, Arij Jan Grootenhuis, Marcel Evert De Gooijer
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Publication number: 20070225352Abstract: 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: ApplicationFiled: April 21, 2005Publication date: September 27, 2007Applicant: Pharmacopela Drug Discovery, Inc.Inventors: Jaap Van Der Louw, Neeltje Teerhuis, Johannes Lommerse, Herman Stock, Pedro Hermkens
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Publication number: 20070155836Abstract: 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: ApplicationFiled: December 15, 2004Publication date: July 5, 2007Applicant: AKZO NOBEL N.V.Inventors: Jaap Van Der Louw, Dirk Leysen, Arii Grootenhuis, Marcel De Gooijer
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Patent number: 7169769Abstract: 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: GrantFiled: September 6, 2002Date of Patent: January 30, 2007Assignee: Akzo Nobel N.V.Inventors: J Jaap Van Der Louw, D Dirk Leysen, M.E. Marcel Evert De Gooijer
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Publication number: 20060128722Abstract: 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: ApplicationFiled: November 3, 2003Publication date: June 15, 2006Applicant: Akzo Nobel N.V.Inventors: Pedro Hermkens, Herman Stock, Jaap Van Der Louw, Neeltje Teerhuis, Johannes Lommerse
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Patent number: 7037916Abstract: 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: GrantFiled: January 10, 2003Date of Patent: May 2, 2006Assignee: 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
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Patent number: 6949531Abstract: 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: GrantFiled: December 5, 2001Date of Patent: September 27, 2005Assignee: Akzo Nobel N.V.Inventors: Jaap Van Der Louw, Dirk Leysen, Marcel Evert De Gooijer
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Patent number: 6881728Abstract: 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: GrantFiled: March 2, 2000Date of Patent: April 19, 2005Assignee: Akzo Nobel N.V.Inventors: Hubert Jan Jozef Loozen, Dirk D. Leysen, Jaap van der Louw
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Publication number: 20040259849Abstract: 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: ApplicationFiled: March 11, 2004Publication date: December 23, 2004Inventors: J Jaap Van Der Louw, D Dirk Leysen, M.E. Marcel Evert De Gooijer
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Patent number: 6780854Abstract: 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: GrantFiled: October 24, 2002Date of Patent: August 24, 2004Assignee: Akzo Nobel NVInventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
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Patent number: 6756366Abstract: 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: GrantFiled: September 24, 2001Date of Patent: June 29, 2004Assignee: Akzo Nobel N.V.Inventors: Jaap van der Louw, Dirk Leysen, Roberta Burma Bursi
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Publication number: 20040087601Abstract: Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed.Type: ApplicationFiled: January 10, 2003Publication date: May 6, 2004Inventors: 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
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Patent number: 6706700Abstract: 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: GrantFiled: September 11, 2002Date of Patent: March 16, 2004Assignee: Akzo-Nobel, N.V.Inventors: Dirk Leysen, Jaap Van der Louw, Roberta Buma Bursi, Marcel Evert De Gooyer
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Publication number: 20040030165Abstract: 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: ApplicationFiled: June 11, 2003Publication date: February 12, 2004Inventors: Jaap Van Der Louw, Dirk Leysen, Marcel Evert De Gooijer