83097-87-4Relevant articles and documents
NEW ANALOGS AS ANDROGEN RECEPTOR AND GLUCOCORTICOID RECEPTOR MODULATORS
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Paragraph 0257; 0258; 0260, (2019/05/16)
The present invention relates to novel dihydropyridine derivatives of formula (I): as modulators of nuclear receptors selected from androgen receptor and glucocorticoid receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by modulation of androgen receptor and/or glucocorticoid receptor, selected from cancer, metastasizing cancers, benign prostate hyperplasia, polycystic ovary syndrome (PCOS), hair loss, hirsutism, acne, hypogonadism, muscle wasting diseases, cachexia, Cushing's syndrome, anti-psychotic drug induced weight gain, obesity, post-traumatic stress disorder and alcoholism.
Structure-activity relationship study of 1,4-dihydropyridine derivatives blocking N-type calcium channels
Yamamoto, Takashi,Niwa, Seiji,Ohno, Seiji,Onishi, Tomoyuki,Matsueda, Hiroyuki,Koganei, Hajime,Uneyama, Hisayuki,Fujita, Shin-Ichi,Takeda, Tomoko,Kito, Morikazu,Ono, Yukitsugu,Saitou, Yuki,Takahara, Akira,Iwata, Seinosuke,Shoji, Masataka
, p. 798 - 802 (2007/10/03)
Cilnidipine is a 1,4-dihydropyridine derived L/N-type calcium channel dual blocker possessing neuroprotective and analgesic effects which are related to its N-type calcium channel inhibitory activity. In order to find specific N-type calcium channel blockers with the least effects on cardiovascular system, we performed structure-activity relationship study on APJ2708, which is a derivative of cilnidipine, and found a promising N-type calcium channel blocker 21b possessing analgesic effect in vivo with a 1600-fold lower activity against L-type calcium channels than that of cilnidipine.