cas 89151-45-1, 1-BOC-4-[2-(TOLUENE-4-SULFONYLOXY)-ETHYL]-PIPERIDINE

Articles about 89151-45-1Total 19 be found

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BIFUNCTIONAL MOLECULES CONTAINING AN E3 UBIQUITINE LIGASE BINDING MOIETY LINKED TO A BCL6 TARGETING MOIETY
Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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Paragraph 00403; 00404

(2021/04/23)

PROTEIN DEGRADERS AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same for the targeted degradation of proteins, and the treatment of target protein-mediated disorders.
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Paragraph 00513; 00514

(2020/01/31)

SMARCA DEGRADERS AND USES THEREOF
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same for the modulation of one or more SWI/SNF-related matrix associated actin dependent regulator of chromatin subfamily A (SMARCA) and/o
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Paragraph 00465-00466

(2020/12/30)

N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
Provided herein are certain substituted N-aryl and N-heteroaryl piperidine compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R 6 are as defined. The said novel compounds, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-β receptor(LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory disease and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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(2018/04/27)

Biological Evaluation and X-ray Co-crystal Structures of Cyclohexylpyrrolidine Ligands for Trypanothione Reductase, an Enzyme from the Redox Metabolism of Trypanosoma
The tropical diseases human African trypanosomiasis, Chagas disease, and the various forms of leishmaniasis are caused by parasites of the family of trypanosomatids. These protozoa possess a unique redox metabolism based on trypanothione and trypanothione reductase (TR), making TR a promising drug target. We report the optimization of properties and potency of cyclohexylpyrrolidine inhibitors of TR by structure-based design. The best inhibitors were freely soluble and showed competitive inhibition constants (Ki) against Trypanosoma (T.) brucei TR and T. cruzi TR and in vitro activities (half-maximal inhibitory concentration, IC50) against these parasites in the low micromolar range, with high selectivity against human glutathione reductase. X-ray co-crystal structures confirmed the binding of the ligands to the hydrophobic wall of the “mepacrine binding site” with the new, solubility-providing vectors oriented toward the surface of the large active site.
De Gasparo, Raoul,Brodbeck-Persch, Elke,Bryson, Steve,Hentzen, Nina B.,Kaiser, Marcel,Pai, Emil F.,Krauth-Siegel, R. Luise,Diederich, Fran?ois
supporting information
p. 957 - 967
(2018/04/10)

The impact of the halogen bonding on D2 and 5-HT1A/5-HT7 receptor activity of azinesulfonamides of 4-[(2-ethyl)piperidinyl-1-yl]phenylpiperazines with antipsychotic and antidepressant properties
A series of azinesulfonamides of long-chain arylpiperazine derivatives with semi-rigid alkylene spacer was designed, synthesized, and biologically evaluated using in vitro methods for their affinity for dopaminergic D2 and serotoninergic 5-HTs
Partyka, Anna,Kurczab, Rafa?,Canale, Vittorio,Sata?a, Grzegorz,Marciniec, Krzysztof,Pasierb, Agnieszka,Jastrz?bska-Wi?sek, Magdalena,Paw?owski, Maciej,Weso?owska, Anna,Bojarski, Andrzej J.,Zajdel, Pawe?
p. 3638 - 3648
(2017/06/13)

AD-35 preparation technology
The invention discloses a new preparation method of a benzodioxole derivative (AD-35) shown by the formula (I). The method comprises the following steps: with piperic acid as a raw material, performing bromination, esterification, cyaniding, cyclopropane
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Paragraph 0099; 0100; 0101

(2016/10/10)

SERINE/THREONINE KINASE INHIBITORS
Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
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(2015/02/19)

THERAPEUTICS TARGETING TRUNCATED ADENOMATOUS POLYPOSIS COLI (APC) PROTEINS
The described invention provides small molecule anti-cancer compounds that selectively target and inhibit measurable biological activity of truncated APC proteins, an immortalized Human Colonic Epithelial Cell (HCEC) model, and pharmaceutical compositions comprising at least one of the small molecule anti-cancer compounds and a pharmaceutically acceptable carrier.
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(2015/09/22)

Synthesis and evaluation of amide, sulfonamide and urea-benzisoxazole derivatives as potential atypical antipsychotics
In this paper, we report the optimization of a series of novel, potential antipsychotic derivatives combining potent dopamine D2, D3 and serotonin 5-HT1A, 5-HT2A receptor affinities. The pharmacological features of compound 27 are a high affinity for dopamine D2, D3 and serotonin 5-HT1A, 5-HT2A receptors. Moreover it possesses low affinity for 5-HT2C and H1 receptors (to reduce the risk of obesity associated with chronic treatment) and hERG channels (to reduce the incidence of torsade des pointes). Furthermore, compound 27 inhibited apomorphine-induced climbing, MK-801-induced hyperactivity and DOI-induced head twitch without observable catalepsy at the highest dose tested in mice. Taken together, among the amide derivatives, we identified compound 27 as a potential antipsychotic lead candidate.
Chen, Yin,Lan, Yu,Cao, Xudong,Xu, Xiangqing,Zhang, Juecheng,Yu, Minquan,Liu, Xin,Liu, Bi-Feng,Zhang, Guisen
supporting information
p. 831 - 838
(2015/05/27)

Design and synthesis of a hybrid series of potent and selective agonists of α7 nicotinic acetylcholine receptor
α7 nicotinic acetylcholine receptor agonists are promising therapeutic candidates for the treatment of cognitive impairment. As a follow up of our internal medicinal chemistry program we investigated a novel series of α7 nAChR agonists. Starting from molecular docking studies on two series of molecules recently developed in our laboratories, an alternative scaffold was designed attempting to combine the optimal features of these previously identified urea and pyrazole compounds. Based on our previous SAR knowledge and on predicted drug-like properties, a small library was synthesized in parallel manner, affording compounds with excellent α7 nAChR activity, selectivity and preliminary ADME profile.
Nencini, Arianna,Castaldo, Cristiana,Comery, Thomas A.,Dunlop, John,Genesio, Eva,Ghiron, Chiara,Haydar, Simon,Maccari, Laura,Micco, Iolanda,Turlizzi, Elisa,Zanaletti, Riccardo,Zhang, Jean
p. 401 - 418
(2014/04/17)

Quinoline- and isoquinoline-sulfonamide derivatives of LCAP as potent CNS multi-receptor - 5-HT1A/5-HT2A/5-HT7 and D 2/D3/D4 - Agents: The synthesis and pharmacological evaluation
Two series of arylpiperazinyl-alkyl quinoline-, isoquinoline-, naphthalene-sulfonamides with flexible (13-26) and semi-rigid (33-36) alkylene spacer were synthesized and evaluated for 5-HT1A, 5-HT2A, 5-HT6, 5-HT7 and selected compounds for D2, D3, D4 receptors. The compounds with a mixed 5-HT and D receptors profile 16 (N-{4-[4-(3-chlorophenyl)-piperazin-1-yl]-butyl}-3- quinolinesulfonamide) and 36 (4-(4-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]- ethyl}-piperidine-1-sulfonyl)-isoquinoline), displaying antagonistic activity at 5-HT7, 5-HT2A, D2 postsynaptic sites, produced antidepressant-like effects in the forced swim test in mice and showed significant anxiolytic activity in the plus-maze test in rats. The lead compound 36, a multi-receptor 5-HT2A/5-HT7/D2/D 3/D4 agent, also displayed significant antipsychotic properties in the MK-801-induced hyperlocomotor activity in mice.
Zajdel, Pawe?,Marciniec, Krzysztof,Ma?lankiewicz, Andrzej,Sata?a, Grzegorz,Duszyńska, Beata,Bojarski, Andrzej J.,Partyka, Anna,Jastrzbska-Wisek, Magdalena,Wróbel, Dagmara,Weso?owska, Anna,Paw?owski, MacIej
experimental part
p. 1545 - 1556
(2012/04/17)

HETEROCYCLIC COMPOUND
The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
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Page/Page column 52-53

(2010/07/08)

PYRIDINE AND PYRAZINE DERIVATIVES - 083
The invention concerns pyridine and pyrazine derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of W, G1, G2, G3, G4, J, Ring A, n and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
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(2009/05/28)

PIPERIDINE AND PIPERAZINE DERIVATIVES
Compounds of general formula (I) in which R1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
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Page/Page column 18-19

(2008/12/08)

HETERO BICYCLIC CARBOXAMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS
The present invention relates to compounds of Formula (I)I and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds
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Page/Page column 149

(2009/01/24)

MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF
Compounds with α7 nicotinic acetylcholine receptor (α7 nAChR) agonistic activity, processes for their preparation, pharmaceutical compositions containing the same and the use thereof for the treatment of neurological and psychiatric diseases.
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Page/Page column 14-15

(2008/06/13)

PIPERIDINE AND PIPERAZINE DERIVATIVES
Compounds of general formula (Ia): in which R1, A1, m, X, n, Y and R3 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
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Page/Page column 22

(2008/06/13)

TRANSGLUTAMINASE MEDIATED CONJUGATION OF PEPTIDES
Methods for conjugating peptides are provided comprising i) reacting a peptide with a first compound comprising a functional group in the presence of a transglutaminase capa-ble of incorporating said compound into the peptide to form a transaminated pepti
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Page/Page column 85-86

(2008/06/13)