Akzo Nobel N.v.

N.v. Organon

Merck Sharp + Dohme B.v.

Msd Oss B.v.

Hubert Jan Jozef Loozen

Dirk Leysen

Jaap Van Der Louw

Gerrit Herman Veeneman

Cornelis Marius Timmers

Fredericus Antonius Dijcks

Jordi Mestres

Antonius Gerardus Hendrikus Ederveen

Wilhelmus Gerardus Eduardus Joseph Schoonen

Herman Thijs Stock

Eduard Willem Zwart

Eduard Willem De Zwart

Cornelius Marius Timmers

Samira Addo

Markus Wagener

Jane Margretha Lena Van Der Werf-Pieters

Lodewijk Pieter Cornelis Schot

Rachel Deborah Van Rijn

Lars Anders Van Der Veen

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.

Ring-annulated dihydropyrrolo[2,1-&#x3b1;]isoquinolines

The present invention relates to substituted steroid compounds having the formula Wherein Ris H or halogen; Ris H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; Ris H or halogen; Ris H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; Ris methyl or ethyl; Ris H or methyl; Ris H or methyl; Ris 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.

Substituted 16,17-annellated steroid compounds for use in womens healthcare

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.

(Dihydro)imidazoiso[5,1-A]quinolines

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.

Dihydrobenzoindazoles

The invention discloses a steroid compound having the formula (1), wherein dotted bonds represent optional double bonds; Ris H, &#x2550;CH, or &#x2014;CH, or &#x2014;CH&#x2014;CH; Ris H, C-alkyl, Calkenyl or C-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; Ris H, C-alkyl, C-alkenyl, C-alkynyl or C-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 &#x3b1; 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. 

16,17-carbocyclic condensed steroid compounds having selective estrogenic activity

The invention provides 15&#x3b2;-substituted steroidal compounds having selective estrogen receptor activity according to Formula I: wherein,

15 &#x3b2;-substituted steroids having selective estrogenic activity

The invention makes a 16&#x3b1;-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a &#x394;5-10 double bond; Ris (C-C)alkyl or (C-C)alkenyl, and each of these groups can be substituted with one or more halogens; Ris (C-C;)alkyl, (C-C)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; Ris methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor &#x3b1; selective treatment 

16Alpha-methyl or ethyl substituted estrogens

Disclosed is a novel class of steroid compounds based on estradiol, and carrying an 11&#x3b2;-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 &#x3b1; and estrogen receptor &#x3b2;.

Estrogenic estra-1,3,5(10)-trienes with differential effects on the alpha and beta estrogen receptors, having a linear hydrocarbon chain of from 5-9 carbon atoms in position 11

This invention provides a compound, or its possible salt, having the formula, wherein: Rand 'Rare OH, optionally independently etherified or esterified; Z is &#x2014;CHCH&#x2014; or &#x2014;C(R,R)&#x2014;, wherein Rand Rare independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; Ris H, halogen, CF, or (1C-4C)alkyl; Rand Rare independently H, halogen, &#x2014;CF, &#x2014;OCF, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, &#x2014;O(CH)X, wherein X is halogen or phenyl and m=2-4; &#x2014;O(CH)NRR, &#x2014;S(CH)NRRor &#x2014;(CH)NRR, wherein m=2-4 and wherein R, Rare independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, &#x2014;CF, &#x2014;OCF, &#x2014;CN, &#x2014;NO, &#x2014;OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo(1C-8C)alkyl; or Rand Rform a 3-8 membered ring structure, optionally substituted with halogen, &#x2014;CF, &#x2014;OCF, &#x2014;CN, &#x2014;NO, hydroxy, hydroxy(1C-4C)alkyl, (1C-8C)alkoxy, aryloxy, (1C-8C)alkylthio, carboxyl, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl.

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Tetrahydrobenzfluorene derivatives

Androgenic steroids having a (14&#x3b2;,17&#x3b1;-)-17-(hydroxymetheyl) configuration, useful for the preparation of male contraceptives and pharmaceutical formulations for the treatment of androgen insufficiency.

14-&#x3b2;, 17-&#x3b1;-hydroxymethylandrostane derivatives as androgens

Orally active androgens

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 R or R is 'R ; R and 'R are OH, optionally independently etherified or esterified; X is N or &mdash;C(R )&mdash;, wherein R 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 &mdash;C(R )&mdash;, with the proviso that X and Y are not both N, wherein R has the same meaning as defined for R ; Z is C(R ,'R )&mdash; or &mdash;C(R ,&prop;R )&mdash;C(R ,'R )&mdash;, wherein R , 'R , R , 'R , R , and 'R , 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. These compounds are useful for estrogen-receptor related treatments in view of a desirable profile of activity for estrogen &agr; and estrogen &bgr; receptors.

Non-steroidal, tetracylic compounds for estrogen-related treatments

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 R is H, (C -C )alkyl or (C -C )acyl; R is H, &agr;-(C -C )alkyl, &agr;-(C -C )alkenyl or &agr;-(C -C )alkynyl; R is H or (C -C )alkyl, (C -C )alkenyl or (C -C )alkynyl, each at location 15 or 16 of the steroid skeleton; R is H or (C -C )alkyl, (C -C )alkenyl or (C -C )alkynyl, each optionally substituted with halogen; preferred is ethynyl; R is H, (C -C )alkyl or (C -C )acyl; R is (C -C )alkyl, (C -C )alkenyl, (C -C )alkynyl or (C -C )alkylidene, each optionally substituted.

Growing community of inventors

Oss, Netherlands

Hubert Jan Jozef Loozen