87394-56-7Relevant academic research and scientific papers
2-[4-(PYRAZOL-4-YLALKYL)PIPERAZIN-1-YL]-3-PHENYL PYRAZINES AND PYRIDINES AND 3-[4-(PYRAZOL-4-YLALKYL)PIPERAZIN-1-YL]-2-PHENYL PYRIDINES AS 5-HT7 RECEPTOR ANTAGONISTS
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Page/Page column 48, (2009/01/20)
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)= or N=, provided that at least one of A and B is -N=, n is 1-3, m is 0-3, and R14 are as defined herein.
BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS
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Page 81, (2008/06/13)
Compounds of formula (I) are useful in the treatment of vanilloid-receptor-meditated diseases, such as inflammatory or neuropathic pain and diseases involving sensory nerve function such as asthma, rheumatoid arthritis, osteoarthritis, inflammatory bowel disorders, urinary incontinence, migraine and psoriasis.
4-(2-Pyridyl)piperazine-1-carboxamides: Potent vanilloid receptor 1 antagonists
Sun, Qun,Tafesse, Laykea,Islam, Khondaker,Zhou, Xiaoming,Victory, Sam F.,Zhang, Chongwu,Hachicha, Mohamed,Schmid, Lori A.,Patel, Aniket,Rotshteyn, Yakov,Valenzano, Kenneth J.,Kyle, Donald J.
, p. 3611 - 3616 (2007/10/03)
A series of 4-(2-pyridyl)piperazine-1-carboxamide analogues based on the lead compound 1 was synthesized and evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH (5.5)-induced (pH) FLIPR assays in a rat VR1-expressing HEK293 cell line. Potent VR1 antagonists were identified through SAR studies. From these studies, 18 was found to be very potent in the in vitro assay [IC50=4.8 nM (pH) and 35 nM (CAP)] and orally available in rat (F%=15.1).
Pyridinylpiperazines, a new class of selective α2-adrenoceptor antagonists
Saari, Walfred S.,Halczenko, Wasyl,King, Stella W.,Huff, Joel R.,Guare, James P.,et al.
, p. 1696 - 1701 (2007/10/02)
A series of 1-(2-pyridinyl)piperazine derivatives was synthesized and evaluated for adrenergic activity. In vitro activity was assessed through the antagonism of clonidine's effect in the rat, isolated, field-stimulated vas deferens and by the displacemen
