N.v. Organon

Merck Sharp + Dohme B.v.

Akzo Nobel N.v.

Msd Oss B.v.

Cornelis Marius Timmers

Willem Frederik Johan Karstens

Wesley Peter Blackaby

Martin De Kort

Willem Frederik Karstens

Mark Enthoven

Saskia Verkaik

Paul Stuart Hinchliffe

Hubert Jan Jozef Loozen

Johannes Bernardus Maria Rewinkel

Paolo Giovanni Martino Conti

Christian Bernard Matthijs Poulie

Pedro Manuel Grima Poveda

Christian Bernard Poulie

Ralf Plate

Herman Thijs Stock

Christianus Johannes Van Koppen

Robert Gerardus Jules Marie Hanssen

Cristian Bernard Matthijs Poulie

Jan Kelder

Robert Gerard Jules Marie Hanssen

Rachel Deborah Van Rijn

Hubert Jan Josef Loozen

Lars Anders Van Der Veen

Martin Dekort

The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.

FSH receptor antagonists

The present invention relates the use of a compound, a pharmaceutical composition, compounds and a kit for treating or preventing disorders in a mammal responsive to TSH receptor mediated pathways, including disorders such as hyperthyroidism, Graves' disease, Graves Ophthalmopathy, Graves' associated pretibial dermopathy, nodular goitre and thyroid cancer comprising administering to said mammal an effective amount of a tetrahydroquinoline compound of Formula (I) or an pharmaceutically acceptable salt thereof. 

TSH receptor antagonizing tetrahydroquinoline compounds

The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders. 

The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders. 

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 invention relates to 5,6-dihydropyrrolo[2,1-&#x3b1;]isoquinoline and pyrrolo[2,1-&#x3b1;]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility. 

(Dihydro)pyrrolo[2,1-&#x3b1;]isoquinolines

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 relates to a 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivative according to Formula (I), wherein the substituents are defined as in the description, or a pharmaceutically salt thereof. The compounds of this invention are potent FSH receptor activators and may be used for treating fertility disorders in e.g. controlled ovarian hyperstimulation and IVF procedures. 

4-phenyl-5-OXO-1,4,5,6,7,8-hexahydroquinoline derivatives as medicaments for the treatment of infertility

The present invention relates to 4-phenyl-5-oxo-1,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein Ris (1-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R, Rare independently halogen, (1-4C)allcyl, (2-4C)alkenyl, (2-4C)-alkynyl, (1-4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; Ris phenyl or (2-5C)-heteroaryl, both substituted with Rand optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkylthio and (di)(1-4C)-alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydro-quinoline derivatives in therapy, more specifically for the treatment of infertility.

4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives for the treatment of infertility

The present invention relates to 2-methyl-4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives having the general Formula (I) wherein the substituents are defined as in the description, or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 2-methyl-4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives in therapy, more specifically for the treatment of fertility disorders. 

4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivatives as medicaments for the treatment of infertility

The present invention relates to tetrahydroquinoline derivatives having gene formula (I) or a pharmaceutically acceptable salt thereof, wherein Rand Rare H or Me; Ris H, hydroxy, (1-4C)alkoxy, (di)(1-4C)alkylamino(2-4C)alkoxy or (2-6)heterocycloakl(2-4C)alkoxy; Ris H, OH, (1-4C)alkoxy or R; Ris H, OH, (1-4C)alkoxy or R, with the proviso that if Ris H, Ris not H, OH or (1-4C)alkoxy and that if Ris H, Ris not H, OH or (1-4C)alkoxy; Ris (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2 6C)heterocycloalkyl or (1-6C)alkyl; Ris amino, (di)(1-4C)alkylamino, (6C)arylcarbonylamino, (6C)arylcarbonyloxy, (2-5C) heteroarylcarbonylamino, (2-5C)heteroarylcarbonyloxy, R-(2-4C)alkylamino, R-(2-4C)alkoxy, R-methylamino or R-methoxy; Ris hydroxy, amino, (-14C)alkoxy, (di)(1-4C)alkylamino, (2-6C)heterocycloalkyl, (2-6C) heterocycloalkylcarbonylamino, (di)(1-4C)alkylaminocarbonylamino, (1-4C)alkoxycarbonylamino and Ris aminocarbonyl, (di)(1-4C)alkylaminocarbonyl, (2-5C)heteroaryl or (6C)aryl. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.

Tetrahydroquinoline derivatives

The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein Rand Rare H, Me; Ris (2-6C)heterocycloalkyl(1-4C)alkyl, (2-5C)heteroaryl(1-4C)alkyl, (6C)aryl (1-4C)alkyl, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyl, (2-6C) heterocycloalkylcarbonylamino(2-4C)alkyl, R-(2-4C)alkyl or R-carbonyl(1-4C)alkyl; Ris (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2-6C)heterocycloalkyl or (1-6C) alkyl and Ris (di)(1-4C)alkylamino, (1-4C)alkoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alkenylamino, (2-5C)heteroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1-4C)alkoxy(2-4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2-4C)alkyl]amino or (di)[hydroxy(2-4C)alkyl]amino. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility. 

Tetrahydroquinoline derivatives and their use as FSH receptor modulators

A bicyclic heteroaromatic compound according to general formula I, or a pharmaceutically acceptable salt thereof, wherein

Bicyclic heteroaromatic compounds

The present invention resides in glycine substituted thieno[2,3-d]pyrimidine derivatives according to general formula I, or a pharmaceutically acceptable salt thereof, wherein The compounds of the invention have LH as well as FSH receptor activating activity and can be used in fertility regulating therapies.

Glycine-substituted thieno[2,3-d]pyrimidines with combined LH and FSH agonistic activity

The invention relates to thieno[2,3-d]pyrimidine derivatives according to general formula I, or a pharmaceutically acceptable salt thereof, wherein N(R1)R2 are joined in a (2-6C)heterocycloalkyl ring. The compounds of the invention have LH as well as FSH receptor activating activity and can be used in fertility regulating therapies.

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Oss, Netherlands

Cornelis Marius Timmers