Patents by Inventor Gerrit Herman Veeneman
Gerrit Herman Veeneman 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: 11633484Abstract: The invention is in the field of medical sciences. It provides new pharmaceutical methods and preparations. In particular, the invention relates to a method for increasing the oral bioavailability of drugs. The invention also provides new compositions comprising a drug covalently attached to a saccharide as in formula (I) below. More in particular, the invention relates to a method for increasing the oral bioavailability of a drug by covalently attaching a sugar-linked, N-substituted or unsubstituted carbamoylalkylidene moiety to a hydroxyl or thiol group of a drug, wherein the substituents are as defined in the claims.Type: GrantFiled: December 18, 2018Date of Patent: April 25, 2023Assignee: PharmaCytics B.V.Inventors: Somhairle MacCormick, Gerrit Herman Veeneman
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Publication number: 20200330602Abstract: The invention is in the field of medical sciences. It provides new pharmaceutical methods and preparations. In particular, the invention relates to a method for increasing the oral bioavailability of drugs. The invention also provides new compositions comprising a drug covalently attached to a saccharide as in formula (I) below. More in particular, the invention relates to a method for increasing the oral bioavailability of a drug by covalently attaching a sugar-linked, N-substituted or unsubstituted carbamoylalkylidene moiety to a hydroxyl or thiol group of a drug, wherein the substituents are as defined in the claims.Type: ApplicationFiled: December 18, 2018Publication date: October 22, 2020Inventors: Somhairle MAC CORMICK, Gerrit Herman VEENEMAN
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Patent number: 9540361Abstract: The present invention relates to novel N-substituted azetidine derivatives < of the formula (I); wherein SERMF is a Selective Estrogen Receptor Modilator fragment; X is no atom, O, S, CH2, carbonyl, N—R5; R1 is H, (C1-8)alkyl, (C3-8)cycloalkyl, (C3-6)heterocycloalkyl, (C2-6)alkenyl, (C2-6)alkynyl, (C1-4)alkylcarbonyl, (C1-4)alkoxy(C2-4)alkyl, (C3-6)cycloalkyl(C1-3)-alkyl, (C3-6)heterocycloalkyl(C1-3)alkyl, each independently optionally substituted with one or more halogen, nitrile, hydroxyl or (C1-2)alkyl; R5 is H, (C1-3)alkyl, optionally substituted with one or more fluorine; R17, R18 and R19 are independently of each other H, fluorine, nitrile or (C1-3)-alkyl, optionally substituted with one or more fluorine; or a prodrug, isotopically-labelled derivative or pharmaceutically acceptable salt thereof, > to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium canType: GrantFiled: December 16, 2011Date of Patent: January 10, 2017Assignee: Merck Sharp & Dohme B.V.Inventors: Fredericus Antonius Dijcks, Scott James Lusher, Herman Thijs Stock, Arthur Oubrie, Gerrit Herman Veeneman
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Publication number: 20160130262Abstract: The present invention relates to novel N-substituted azetidine derivatives<of the formula (I); wherein SERMF is a Selective Estrogen Receptor Modilator fragment; X is no atom, O, S, CH2, carbonyl, N—R5; R1 is H, (C1-8)alkyl, (C3-8)cycloalkyl, (C3-6)heterocycloalkyl, (C2-6)alkenyl, (C2-6)alkynyl, (C1-4)alkylcarbonyl, (C1-4)alkoxy(C2-4)alkyl, (C3-6)cycloalkyl(C1-3)-alkyl, (C3-6)heterocycloalkyl(C1-3)alkyl, each independently optionally substituted with one or more halogen, nitrile, hydroxyl or (C1-2)alkyl; R5 is H, (C1-3)alkyl, optionally substituted with one or more fluorine; R17, R18 and R19 are independently of each other H, fluorine, nitrile or (C1-3)-alkyl, optionally substituted with one or more fluorine; or a prodrug, isotopically-labelled derivative or pharmaceutically acceptable salt thereof, >to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancerType: ApplicationFiled: December 16, 2011Publication date: May 12, 2016Inventors: Fredericus Antonius Dijcks, Scott James Lusher, Herman Thijs Stock, Arthur Oubrie, Gerrit Herman Veeneman
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Patent number: 8063102Abstract: The present invention relates to novel tetrahydronaphthalen-2-ol derivatives, to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the manufacture of a medicament for the prevention or treatment of lower urinary tract symptoms, benign prostate hyperplasia, prostate cancer, hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer.Type: GrantFiled: March 11, 2010Date of Patent: November 22, 2011Assignee: N.V. OrganonInventors: Herman Thijs Stock, Neeltje Miranda Teerhuis, Gerrit Herman Veeneman
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Patent number: 7846966Abstract: The invention provides chroman compounds having formula 1 wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is H, Hal, CF3, OH or (1C-2C)alkyloxy; R2, R3, and R5 are independently H, Hal, CF3, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.Type: GrantFiled: May 8, 2009Date of Patent: December 7, 2010Assignee: N.V. OrganonInventors: Gerrit Herman Veeneman, Neeltje Miranda Teerhuis
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Publication number: 20100240748Abstract: The present invention relates to novel tetrahydronaphthalen-2-ol derivatives, to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the manufacture of a medicament for the prevention or treatment of lower urinary tract symptoms, benign prostate hyperplasia, prostate cancer, hot flushes, anxiety, depression, breast cancer, medullary thyroid carcinoma, ovarian cancer, inflammatory bowel disease, arthritis, endometriosis, and colon cancer.Type: ApplicationFiled: March 11, 2010Publication date: September 23, 2010Inventors: Herman Thijs Stock, Neeltje Miranda Teerhuis, Gerrit Herman Veeneman
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Patent number: 7696190Abstract: The invention makes a 16?-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a ?5-10 double bond; R1 is (C1-C3)alkyl or (C2-C3)alkenyl, and each of these groups can be substituted with one or more halogens; R2 is (C1-C4;)alkyl, (C2-C4)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R3 is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor ? selective treatmentType: GrantFiled: July 23, 2001Date of Patent: April 13, 2010Assignee: N.V. OrganonInventors: Jordi Mestres, Hubert Jan Jozef Loozen, Gerrit Herman Veeneman
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Publication number: 20100029603Abstract: The invention makes a 16?-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a ?5-10 double bond; R1 is (C1-C3)alkyl or (C2-C3)alkenyl, and each of these groups can be substituted with one or more halogens; R2 is (C1-C4)alkyl, (C2-C4)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R3 is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor ? selective treatment.Type: ApplicationFiled: May 29, 2009Publication date: February 4, 2010Inventors: Jordi Mestres, Hubert Jan Jozef Loozen, Gerrit Herman Veeneman
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Publication number: 20090221695Abstract: The invention provides chroman compounds having formula 1 wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is H, Hal, CF3, OH or (1C-2C)alkyloxy; R2, R3, and R5 are independently H, Hal, CF3, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.Type: ApplicationFiled: May 8, 2009Publication date: September 3, 2009Inventors: Gerrit Herman Veeneman, Neeltje Miranda Teerhuis
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Patent number: 7531571Abstract: The invention provides chroman compounds having formula 1 wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is H, Hal, CF3, OH or (1C-2C)alkyloxy; R2, R3, and R5are independently H, Hal, CF3, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.Type: GrantFiled: January 10, 2006Date of Patent: May 12, 2009Assignee: N.V. OrganonInventors: Gerrit Herman Veeneman, Neeltje Miranda Teerhuis
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Patent number: 7214706Abstract: The invention provides chroman compounds having Formula (1), wherein R1 is (1C–4C)alkyl, (2C–4C)alkenyl or (2C–4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is Hal, CF3, OH or (1C–2C)alkyloxy; R2, R3, and R5 are independently H, Hal, CF3, (1C–4C)alkyl, (2C–4C)alkenyl or (2C–4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.Type: GrantFiled: February 26, 2001Date of Patent: May 8, 2007Assignee: Akzo Nobel N.V.Inventors: Gerrit Herman Veeneman, Neeltje Miranda Teerhuis
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Patent number: 6756375Abstract: The invention provides for a non-steroidal compound having the formula wherein Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2— or —CH2CH2—; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2, R3 and R4 are independently H, halogen, —CF3, —OCF3, (1C-8C)Alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-4C)aType: GrantFiled: July 24, 2003Date of Patent: June 29, 2004Assignee: Akzo Nobel N.V.Inventors: Gerrit Herman Veeneman, Hubert JanJozef Loozen, Jordi Mestres, Eduard Willem De Zwart
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Publication number: 20040059004Abstract: The invention provides for a non-steroidal compound having the formula 1Type: ApplicationFiled: July 24, 2003Publication date: March 25, 2004Inventors: Gerrit Herman Veeneman, Hubert JanJozef Loozen, Eduard Willem De Zwart, Jordi Mestres
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Publication number: 20040043976Abstract: The invention makes a 16&agr;-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a &Dgr;5-10 double bond; R1 is (C1-C3)alkyl or (C2-C3)alkenyl, and each of these groups can be substituted with one or more halogens; R2 is (C1-C4;)alkyl, (C2-C4)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R3 is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor &agr; selective treatment.Type: ApplicationFiled: July 17, 2003Publication date: March 4, 2004Inventors: Jordi Mestres, Hubert Jan Jozef Loozen, Gerrit Herman Veeneman
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Patent number: 6686371Abstract: The invention provides non-steroidal estrogenic compounds with estrogenic and anti-estrogenic compounds effects for treatment of estrogen-deficiency related disorders, which compounds are having formula (I) wherein, one of Ra or Rb is 'Re; Re and 'Re are OH, optionally independently etherified or esterified; X is N or —C(R1)—, wherein R1 is H1 halogen, CN, optionally substituted aryl, (1C-4C)alkyl, (2C-4C)alkenyl, (2C-4C)alkynyl or (3C-6C)cycloalkyl, which alkyl, alkenyl, alkynyl and cycloalkyl groups can optionally be substituted with one or more halogens; Y is N or —C(R2)—, with the proviso that X and Y are not both N, wherein R2 has the same meaning as defined for R1; Z is C(R3,'R3)— or —C(R4,∝R4)—C(R5,'R5)—, wherein R3, 'R3, R4, 'R4, R5, and 'R5, independently arc H, (1C-4C)alkyl, (2C-4C)alkenyl or (3C-6C) cycloalkyl, which alkyl, alkenyl and cycloalkyl groups can optionally be substituted with one or more halogens.Type: GrantFiled: December 2, 2002Date of Patent: February 3, 2004Assignee: Akzo Nobel N.V.Inventors: Gerrit Herman Veeneman, Eduard Willem De Zwart, Hubert Jan Jozef Loozen, Jordi Mestres
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Patent number: 6677329Abstract: Disclosed are novel, selective estrogens type having a steroid skeleton with a non-aromatic A-ring and a free or capped hydroxyl group at carbon atom No. 3. The estrogens satisfy general formula (I), in which R1 is H, (C1-C3)alkyl or (C2-C3)acyl; R2 is H, &agr;-(C1-C4)alkyl, &agr;-(C2-C4)alkenyl or &agr;-(C2-C4)alkynyl; R3 is H or (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl, each at location 15 or 16 of the steroid skeleton; R4 is H or (C1-C5)alkyl, (C2-C5)alkenyl or (C2-C5)alkynyl, each optionally substituted with halogen; preferred is ethynyl; R5 is H, (C1-C3)alkyl or (C2-C3)acyl; R6 is (C1-C5)alkyl, (C2-C5)alkenyl, (C2-C5)alkynyl or (C1-C5)alkylidene, each optionally substituted.Type: GrantFiled: May 29, 2002Date of Patent: January 13, 2004Assignee: Akzo Nobel N V.Inventors: Hubert Jan Jozef Loozen, Gerrit Herman Veeneman, Wilhelmus Gerardus Eduardus Joseph Schoonen
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Publication number: 20030144313Abstract: The invention provides non-steroidal estrogenic compounds with estrogenic and anti-estrogenic compounds effects for treatment of estrogen-deficiency related disorders, which compounds are having formula (I) wherein, one of Ra or Rb is 'Re; Re and 'Re are OH, optionally independently etherified or esterified; X is N or —C(R1)—, wherein R1 is H, halogen, CN, optionally substituted aryl, (1C-4C)alkyl, (2C-4C)alkenyl, (2C-4C)alkynyl or (3C-6C)cycloalkyl, which alkyl, alkenyl, alkynyl and cycloalkyl groups can optionally be substituted with one or more halogens; Y is N or —C(R2)—, with the proviso that X and Y are not both N, wherein R2 has the same meaning as defined for R1; Z is C(R3,'R3)— or —C(R4,'R4)—C(R5,'R5)—, wherein R3, 'R3, R4, 'R4, R5, and 'R5, independently arc H, (1C-4C)alkyl, (2C-4C)alkenyl or (3C-6C) cycloalkyl, which alkyl, alkenyl and cycloalkyl groups can optionally be substituted with one or more halogens.Type: ApplicationFiled: December 2, 2002Publication date: July 31, 2003Inventors: Gerrit Herman Veeneman, Eduard Willem De Zwart, Hubert Jan Jozef Loozen, Jordi Mestres
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Publication number: 20030069303Abstract: The invention provides chroman compounds having Formula (1), wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is Hal, CF3, OH or (1C-2C)alkyloxy; R2, R3, and R5 are independently H, Hal, CF3, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.Type: ApplicationFiled: August 30, 2002Publication date: April 10, 2003Inventors: Gerrit Herman Veeneman, Neeltje Miranda Teerhuis