The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.
1-SUBSTITUTED PHENYL-1-(1H-IMIDAZOL-4-YL) ALCOHOLS, PROCESS FOR PRODUCING THE SAME AND USE THEREOF
申请人:Takeda Chemical Industries, Ltd.
公开号:EP1227086A1
公开(公告)日:2002-07-31
[Problem] To provide a composition having a steroid C17,20 lyase inhibitory activity and useful as an agent for the prophylaxis or treatment of prostatism and tumors such as breast cancer. A compound represented by the formula:
wherein R is a hydrogen atom or a protecting group, R1 is a lower alkyl group or a cyclic hydrocarbon group, R2 is an aromatic hydrocarbon group optionally having substituents or an aromatic heterocyclic group optionally having substituents, R3 is a hydrocarbon group optionally having substituents, a hydroxyl group optionally having substituents, a thiol group optionally having substituents, an amino group optionally having substituents, an acyl group or a halogen atom, and n is an integer of 0 to 4, and a salt thereof have a steroid C17,20-lyase inhibitory activity, and are useful as an agent for the prophylaxis or treatment of prostatism and tumors such as breast cancer and the like.
[问题] 提供一种组合物,该组合物具有类固醇 C17,20 裂解酶抑制活性,可作为预防或治疗前列腺炎和乳腺癌等肿瘤的药物。一种由式表示的化合物:
其中 R 是氢原子或保护基,R1 是低级烷基或环状烃基,R2 是任选具有取代基的芳香烃基或任选具有取代基的芳香杂环基,R3 是任选具有取代基的烃基、任选具有取代基的羟基、R3为可选具有取代基的烃基、可选具有取代基的羟基、可选具有取代基的硫醇基、可选具有取代基的氨基、酰基或卤素原子,且 n 为 0 至 4 的整数,这些化合物及其盐具有类固醇 C17,20-lyase 抑制活性,可用作预防或治疗前列腺疾病和乳腺癌等肿瘤的药物。
SULFONYLAMINO-ACETIC ACID DERIVATIVES AND THEIR USE AS OREXIN RECEPTOR ANTAGONISTS