N.v. Organon

Merck Sharp + Dohme B.v.

Msd Oss B.v.

Marcelis Van Der Stelt

Joseph Maria Gerardus Barbara Cals

Wesley Peter Blackaby

Naimisha Trivedi

Johannes Petrus Gerardus Klomp

Ines Huisman

Wouter Wiedenhof

Charles Anthony Graham Baker-Glenn

The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders. 

N-piperidin-4-yl derivatives

The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein Ris H, (C)alkyl (optionally substituted with oxo, (C)alkyloxy, (C)alkyloxycarbonyl, halogen or CN), (C)cycloalkyl or (C)cycloalkyl(C)alkyl, each cycloalkyl ring optionally comprising a heteroatom selected from O and S; Rand Rare independently H or (C)alkyl; or Rand Rform together with the carbon atom to which they are bound a (C)cycloalkyl group; Ris H or 1 to 3 F substituents; Ris H or 1 to 4 F substituents; Rand Rare independently H or F; X represents R, OR, NRR, Ris (C)cycloalkyl optionally comprising a heteroatom selected from O, S, SO and SO; Ris H or (C)alkyl; Rrepresents 1-3 substituents independently selected from H, (C)alkyl, halogen, oxo, CN and CF; Y is CF, O, S, SO or SO; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.

1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives

The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula I wherein Ris H, (C)alkyl (optionally substituted with oxo, OR, COOR, halogen or CN), (C)alkenyl, (C)alkynyl, (C)cycloalkyl or (C)cycloalkyl(C)alkyl; Rand R' are independently H or (C)alkyl; or Rand R&#x2032; form together with the carbon atom to which they are bound a (C)cycloalkyl group; Rrepresents H or 1 to 4 F substituents; Y represents or NRR; X represents CHR, CF, O, S, SO or SO; Rand Rare (C)alkyl; Ris H, ORor CN; Ris (C)alkyl; Ris (C)cycloalkyl comprising a heteroatom selected from O, S, SO and SO; Ris H or (C)alkyl; o and m represent the ortho or meta position of the substituent Y&#x2014;CH; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.

1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione

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Oss, Netherlands

Marcelis Van Der Stelt