78551-60-7Relevant academic research and scientific papers
Histamine H3 receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation
Falkenstein, Markus,Reiner-Link, David,Zivkovic, Aleksandra,Gering, Ian,Willbold, Dieter,Stark, Holger
, (2021/10/29)
Alzheime?s disease (AD) is the most prominent neurodegenerative disorder with high medical need. Protein-protein-interactions (PPI) interactions have a critical role in AD where β-amyloid structures (Aβ) build toxic oligomers. Design of disease modifying multi target directed ligand (MTDL) has been performed, which disable PPI on the one hand and on the other hand, act as procognitive antagonists at the histamine H3 receptor (H3R). The synthetized compounds are structurally based on peptidomimetic amino acid-like structures mainly as keto, diketo-, or acyl variations of a piperazine moiety connected to an H3R pharmacophore. Most of them showed low nanomolar affinities at H3R and some with promising affinity to Aβ-monomers. The structure–activity relationships (SAR) described offer new possibilities for MTDL with an optimized profile combining symptomatic and potential causal therapeutic approaches in AD.
(S)-3-(2-(4-(BENZYL)-3-OXOPIPERAZIN-1-YL)ACETAMIDO)-4-OXO-5-(2,3,5,6-TETRAFLUOROPHENOXY)PENTANOIC ACID DERIVATIVES AND RELATED COMPOUNDS AS CASPASE INHIBITORS FOR TREATING CARDIOVASCULAR DISEASES
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Paragraph 00323; 00335, (2020/01/24)
The present invention relates to (S)-3-(2-(4-(benzyl)-3-oxopiperazin-l- yl)acetamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid derivatives and related compounds as caspase inhibitors for treating e.g. cardiovascular, kidney, liver, lung, skin, joints, CNS, inflammatory and autoimmune diseases.
INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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Page/Page column 108-109, (2020/02/16)
The present invention provides compounds of formula (I): wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases.
NOVEL SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2, 3-DIOXYGENASE (IDO) INHIBITORS
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Page/Page column 160, (2020/06/19)
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
2-PHENYLIMIDAZO[4,5-B]PYRIDIN-7-AMINE DERIVATES USEFUL AS INHIBITORS OF MAMMALIAN TYROSINE KINASE ROR1 ACTIVITY
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Page/Page column 115-116, (2018/03/26)
Compound of formula (I′) or (I′′) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of mammalian kinase enzyme activity, including ROR1 tyrosine kinase activity and may be used in the treatment of disorders associated with such activity.
Transition-Metal-Free Amine Oxidation: A Chemoselective Strategy for the Late-Stage Formation of Lactams
Griffiths, Robert J.,Burley, Glenn A.,Talbot, Eric P. A.
supporting information, p. 870 - 873 (2017/02/26)
A metal-free strategy for the formation of lactams via selective oxidation of cyclic secondary and tertiary amines is described. Molecular iodine facilitates both chemoselective and regioselective oxidation of C-H bonds directly adjacent to a cyclic amine. The mild conditions, functional group tolerance, and substrate scope are demonstrated using a suite of diverse small molecule cyclic amines, including clinically approved drug scaffolds.
6 Phenyl or 6 Pyridin 3 YL Indazole Derivatives and Methods of Use
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Paragraph 0650, (2017/01/19)
Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, R2, R3, R4, R5, R6, and X are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
6-PHENYL- OR 6-(PYRIDIN-3-YL)INDAZOLE DERIVATIVES AND METHODS OF USE
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Page/Page column 150; 151, (2015/08/06)
Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R1, R2, R3, R4, R5, R6, and X are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
Discovery of DA-1229: A potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes
Kim, Heung Jae,Kwak, Woo Young,Min, Jong Pil,Lee, Jae Young,Yoon, Tae Hyun,Kim, Ha Dong,Shin, Chang Yell,Kim, Mi Kyung,Choi, Song Hyen,Kim, Hae Sun,Yang, Eun Kyoung,Cheong, Ye Hwang,Chae, Yu Na,Park, Kyung Jin,Jang, Ji Myun,Choi, Soo Jung,Son, Moon Ho,Kim, Soon Hoe,Yoo, Moohi,Lee, Bong Jin
scheme or table, p. 3809 - 3812 (2011/07/31)
A series of β-amino amide containing substituted piperazine-2-one derivatives was synthesized and evaluated as inhibitors of dipeptidyl pepdidase-4 (DPP-4) for the treatment of type 2 diabetes. As results of intensive SAR study of the series, (R)-4-[(R)-3-amino-4-(2,4,5-trifluorophenyl)- butanoyl]-3-(t-butoxymethyl)-piperazin-2-one (DA-1229) displayed potent DPP-4 inhibition pattern in several animal models, was selected for clinical development.
Arylpiperazine derivatives and uses thereof
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Page/Page column 14-15, (2009/09/05)
Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3 and R4 are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
