142001-84-1Relevant academic research and scientific papers
COMPOUNDS AS INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR
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, (2020/09/27)
The present invention provides compounds of Formula (I) shown above and their pharmaceutically acceptable salt, solvates, isomers, or prodrugs, as well as pharmaceutical compositions containing these compounds. Also provided by the invention is a method for treating a disorder mediated by macrophage migration inhibitory factor in a subject, comprising administering to the subject in need thereof a compound or a pharmaceutical composition of this invention.
TRIAZOLO [4,3-B] PYRIDAZINE DERIVATIVES AND THEIR USES FOR PROSTATE CANCER
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Page/Page column 127, (2010/09/03)
The invention concerns bicyclic compounds of Formula (I) wherein Formula (II), R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen- receptor associated conditions, particularly prostate cancer.
[1,2,4] TRIAZOLO [4,3-B] PYRIDAZINES AS LIGANDS OF THE ANDROGEN RECEPTOR
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Page/Page column 58-59, (2010/12/17)
The invention concerns bicyclic compounds of Formula (I): wherein, R1, R2, R3, R4, R5, X1, X2, Y, k, m, n and p are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen- receptor associated conditions, particularly prostate cancer.
Synthesis and dopaminergic activity of some E-3-(piperidin-1-yl)-1-(4-substituted phenyl)prop-2-en-1-one derivatives
Sakhteman, Amirhossein,Foroumadi, Alireza,Sharifzadeh, Mohammad,Amanlou, Masoud,Rayatnia, Farhoud,Shafiee, Abbas
scheme or table, p. 6908 - 6913 (2009/12/24)
A convenient route for the synthesis of some 2-propen-1-one derivatives with E isomeric configuration is described. The activity of the synthesized compounds was evaluated through behavioral studies of apomorphine-induced licking in animal models. It was demonstrated that most of the synthesized compounds showed moderate activity in inhibition of lickings, among which 6a, was the most active compound at 30 mg/kg.
New μ-opioid receptor agonists with phenoxyacetic acid moiety
Sato, Susumu,Komoto, Teruo,Kanamaru, Yoshihiko,Kawamoto, Noriyuki,Okada, Tomomi,Kaiho, Terumitsu,Mogi, Kinichi,Morimoto, Shinichi,Umehara, Norimitsu,Koda, Tadayuki,Miyashita, Akira,Sakamoto, Takao,Niino, Yasuhiro,Oka, Tetsuo
, p. 292 - 297 (2007/10/03)
New μ-opioid receptor (MOR) agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Among the synthesized compounds, [2-[1-[3-(N,N-dimethylcarbamoyl)-3,3-diphenylpropyl]-4-hydroxypiperidin-4-yl] phenoxy]acetic acid (8: SS620) having phenoxyacetic acid and 4-hydroxypiperidine moieties showed the highest agonist potency on the MOR in an isolated guinea-pig ileum preparation, and it also had selectivity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells compared with the same types of δ- and κ-opioid receptors (DOR and KOR). In addition, compound 8 showed a 10 times more potent MOR agonist activity than loperamide. Furthermore, compound 8 showed a peripheral analgesic activity in vivo screening on rat.
Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4- hydroxybenzyl)piperidines, and (±)-3-(4-hydroxyphenyl)pyrrolidines: Selective antagonists at the 1A/2B NMDA receptor subtype
Guzikowski, Anthony P.,Tamiz, Amir P.,Acosta-Burruel, Manuel,Hong-Bae, Soo,Cai, Sui Xiong,Hawkinson, Jon E.,Keana, John F. W.,Kesten, Suzanne R.,Shipp, Christina T.,Tran, Minhtam,Whittemore, Edward R.,Woodward, Richard M.,Wright, Jon L.,Zhou, Zhang-Lin
, p. 984 - 994 (2007/10/03)
Antagonists at the 1A/2B subtype of the NMDA receptor (NR1A/2B) are typically small molecules that consist of a 4-benzyl- or a 4-phenylpiperidine with an ω-phenylalkyl substituent on the heterocyclic nitrogen. Many of these antagonists, for example ifenprodil (1), incorporate a 4-hydroxy substituent on the ω-phenyl group. In this study, the position of this 4- hydroxy substituent was transferred from the ω-phenyl group to the benzyl or phenyl group located on the 4-position of the piperidine ring. Analogues incorporating pyrrolidine in lieu of piperidine were also prepared. Electrical recordings using cloned receptors expressed in Xenopus oocytes show that high-potency antagonists at the NR1A/2B subtype are obtained employing N-(ω-phenylalkyl)-substituted 4-(4-hydroxyphenyl)piperidine, 4-(4- hydroxybenzyl)piperidine, and (±)3-(4-hydroxyphenyl)pyrrolidine as exemplified by 21 (IC50 = 0.022 μM), 33 (IC50 = 0.059 μM), and 40 (IC50 = 0.017 μM), respectively. These high-potency antagonists are > 1000 times more potent at the NR1A/2B subtype than at either the NR1A/2A or NR1A/2C subtypes. The binding affinities of 21 at α1-adrenergic receptors ([3H]prazosin, IC50 = 0.54 μM) and dopamine D2 receptors ([3H]raclopride, IC50 = 1.2 μM) are reduced by incorporating a hydroxy group onto the 4-position of the piperidine ring and the β-carbon of the N- alkyl spacer to give (±)-27: IC50 NR1A/2B, 0.026; α1, 14; D2, 105 μM. The high-potency phenolic antagonist 21 and its low-potency O-methylated analogue 18 are both potent anticonvulsants in a mouse maximal electroshock- induced seizure (MES) study (ED50 (iv) = 0.23 and 0.56 mg/kg, respectively). These data indicate that such compounds penetrate the blood- brain barrier but their MES activity may not be related to NMDA receptor antagonism.
Arylalkylamines, process for preparing them and pharmaceutical compositions containing them
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, (2008/06/13)
The invention relates to compounds of formula: STR1 in which Y represents--either a group Cy--N in which Cy represents a phenyl, optionally substituted; a C3 -C7 cycloalkyl group; a pyrimidinyl group or a pyridyl group; or a group ST
