Patents by Inventor Hubert Jan Jozef Loozen

Hubert Jan Jozef Loozen 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: 8431564
    Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: April 30, 2013
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
  • Patent number: 8367648
    Abstract: The present invention relates to substituted steroid compounds having the formula Wherein R1 is H or halogen; R2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R3 is H or halogen; R4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R5 is methyl or ethyl; R6 is H or methyl; R7 is H or methyl; R8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.
    Type: Grant
    Filed: June 8, 2010
    Date of Patent: February 5, 2013
    Assignee: MSD OSS B.V.
    Inventors: Fredericus Antonius Dijcks, Hubert Jan Jozef Loozen, Samira Addo, Antonius Gerardus Hendrikus Ederveen
  • Patent number: 8071587
    Abstract: The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: December 6, 2011
    Assignee: N. V. Organon
    Inventors: Hubert Jan Jozef Loozen, Cornelius Marius Timmers
  • Patent number: 8071589
    Abstract: The invention relates to benzoindazole derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: December 6, 2011
    Assignee: N. V. Organon
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen
  • Publication number: 20110224183
    Abstract: The invention discloses a steroid compound having the formula (1): wherein dotted bonds represent optional double bonds; R6 is H, ?CH2, or —CH3, or —CH2—CH3; R7 is H, C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, Cl1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being ? and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.
    Type: Application
    Filed: May 20, 2011
    Publication date: September 15, 2011
    Applicant: N.V. Organon
    Inventor: Hubert Jan Jozef Loozen
  • Publication number: 20110028451
    Abstract: The invention relates to benzoindazole derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Application
    Filed: July 29, 2010
    Publication date: February 3, 2011
    Applicant: N.V. Organon
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen
  • Publication number: 20110028450
    Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Application
    Filed: July 27, 2010
    Publication date: February 3, 2011
    Applicant: N.V. Organon
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
  • Patent number: 7868193
    Abstract: The invention discloses a steroid compound having the formula (1), wherein dotted bonds represent optional double bonds; R6 is H, ?CH2, or —CH3, or —CH2—CH3; R7 is H, C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, C1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1-3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being ? and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: January 11, 2011
    Assignee: N.V. Organon
    Inventor: Hubert Jan Jozef Loozen
  • Publication number: 20100331292
    Abstract: The present invention relates to substituted steroid compounds having the formula Wherein R1 is H or halogen; R2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R3 is H or halogen; R4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R5 is methyl or ethyl; R6 is H or methyl; R7 is H or methyl; R8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.
    Type: Application
    Filed: June 8, 2010
    Publication date: December 30, 2010
    Applicant: N.V. Organon
    Inventors: Fredericus Antonius Dijcks, Hubert Jan Jozef Loozen, Samira Addo, Antonius Gerardus Hendrikus Ederveen
  • Publication number: 20100324021
    Abstract: The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Application
    Filed: May 25, 2010
    Publication date: December 23, 2010
    Applicant: N.V. Organon
    Inventors: Hubert Jan Jozef Loozen, Cornelius Marius Timmers
  • Patent number: 7838516
    Abstract: The invention provides 15?-substituted steroidal compounds having selective estrogen receptor activity according to Formula I: wherein, R1 is H, C1-5 alkyl, C1-12 acyl, di-(C1-5 alkyl)aminocarbonyl, (C1-5alkyl)oxycarbonyl or sulfamoyl, R2 is H, C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl, each of which may be optionally substituted with a halogen, R3 is C1-2 alkyl, ethenyl or ethynyl, each of which may be optionally substituted with a halogen, and R4 is H or C1-12 acyl.
    Type: Grant
    Filed: September 5, 2005
    Date of Patent: November 23, 2010
    Assignee: N.V. Organon
    Inventors: Hubert Jan Jozef Loozen, Antonius Gerardus Hendrikus Ederveen, Fredericus Antonius Dijcks
  • Publication number: 20100249083
    Abstract: The invention discloses a steroid compound having the formula (1): wherein dotted bonds represent optional double bonds; R6 is H, ?CH2, or —CH3, or —CH2—CH3; R7 is H, C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, C1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being ? and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.
    Type: Application
    Filed: June 15, 2010
    Publication date: September 30, 2010
    Applicant: N.V. Organon
    Inventor: Hubert Jan Jozef LOOZEN
  • Patent number: 7696190
    Abstract: 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: Grant
    Filed: July 23, 2001
    Date of Patent: April 13, 2010
    Assignee: N.V. Organon
    Inventors: Jordi Mestres, Hubert Jan Jozef Loozen, Gerrit Herman Veeneman
  • Publication number: 20100029603
    Abstract: 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: Application
    Filed: May 29, 2009
    Publication date: February 4, 2010
    Inventors: Jordi Mestres, Hubert Jan Jozef Loozen, Gerrit Herman Veeneman
  • Patent number: 7655653
    Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: February 2, 2010
    Assignee: N.V. Organon
    Inventor: Hubert Jan Jozef Loozens
  • Patent number: 7528123
    Abstract: Disclosed is a novel class of steroid compounds based on estradiol, and carrying an 11?-substitution. Said substitution is a hydrocarbon group which may be linear or branched, provided that it comprises, as the longest chain on carbon atom no. 11 of the steroid skeleton, one single linear chain having a length of from 5 to 9 carbon atoms, wherein said chain may be saturated or unsaturated. The resulting compounds have a desirable mixed agonist/antagonist profile for estrogen receptor ? and estrogen receptor ?.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: May 5, 2009
    Assignee: N.V. Organon
    Inventors: Hubert Jan Jozef Loozen, Wilhelmus Gerardus Eduardus Joseph Schoonen
  • Patent number: 7335659
    Abstract: This invention provides a compound, or its possible salt, having the formula, wherein: Re and ?Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or —C(R4,R5)—, wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2 and R3 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 wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be 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 or 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-
    Type: Grant
    Filed: February 14, 2003
    Date of Patent: February 26, 2008
    Assignee: N.V. Organon
    Inventors: Hubert Jan Jozef Loozen, Markus Wagener, Gerrit Veeneman, Eduard Willem Zwart
  • Patent number: 7304155
    Abstract: A compound having the formula I wherein the O—(CH2)n—N(R1,R2) substituent on the phenyl ring can be in meta or para position; n is 2-4 Re and ?Re are OH, optionally independently etherified or esterified; R1 and R2 are independently (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(2C-4C)alkyl, (1C-3C)alkoxy(2C-4C)alkyl, aryl or aryl(1C-2C)alkyl; or R1 and R2 together with the nitrogen form an aromatic or non-aromatic heterocyclic ring structure, optionally mono- or poly-substituted with (1C-4C)alkyl, (2C-4C)alkenyl, hydroxy(1C-2C)alkyl, (1C-2C)alkoxy(1C-3C)alkyl or aryl. These compounds can be used for estrogen receptor ? selective medical treatments.
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: December 4, 2007
    Assignee: N.V. Organon
    Inventor: Hubert Jan Jozef Loozen
  • Publication number: 20050159405
    Abstract: This invention provides a compound, or its possible salt, having the formula, wherein: Re and ?Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or —C(R4,R5)—, wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3 , or (1C-4C)alkyl; R2 and R3 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 wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be 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 or 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(1
    Type: Application
    Filed: February 14, 2003
    Publication date: July 21, 2005
    Applicant: Akzo Nobel, N.V. Patent Department
    Inventors: Hubert, Jan, Jozef Loozen, Markus Wagener, Gerrit Veeneman, Eduard, Willem Zwart
  • 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