893724-10-2Relevant articles and documents
Intramolecular functional group differentiation as a strategy for the synthesis of bridged bicyclic β-amino acids
Tymtsunik, Andriy V.,Kokhan, Serhii O.,Ivon, Yevhen M.,Komarov, Igor V.,Grygorenko, Oleksandr O.
, p. 22737 - 22748 (2016/03/26)
Differentiation of identical electrophilic functional groups (carboxylates) by a strategically placed internal nucleophile (an amino group) in cyclic precursors was used as a key general approach to functionalized azabicyclic scaffolds. The utility of the method was demonstrated by the synthesis of three bicyclic β-amino acids (analogues of nipecotic acid), which were prepared in good yields and on a relatively large scale.
SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE
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Page/Page column 752, (2016/04/10)
Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
COMBINATIONS OF HEPATITIS C VIRUS INHIBITORS
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Page/Page column 702, (2015/02/02)
The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
NOVEL AZA-OXO-INDOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION
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Page/Page column 44; 45, (2015/02/25)
The invention provides novel compounds having the general formula:(I) wherein R1, R2, R3, R4, W and X are as described herein, compositions including the compounds and methods of using the compounds.
Gram-scale synthesis of 3,5-methanonipecotic acid, a nonchiral bicyclic β-amino acid
Tymtsunik, Andriy V.,Bilenko, Vitaliy A.,Grygorenko, Oleksandr O.,Komarov, Igor V.
, p. 355 - 358 (2014/03/21)
A scalable synthesis was developed of 3,5-methanoni?pecotic acid (3-azabicyclo[3.1.1]heptane-1-carboxylic acid), a rare example of a conformationally constrained nonchiral β-amino acid, potentially useful in peptide engineering and peptidomimetic drug design. A retrosynthetic strategy based on disconnections exclusively within the symmetry planes of the target and the intermediate molecules was found to be useful and might deliver expedite syntheses in other similar cases. Georg Thieme Verlag Stuttgart New York.
Trifluoromethyl-substituted analogues of 1-aminocyclobutane-1-carboxylic acid
Radchenko, Dmytro S.,Mykhailiuk, Pavel K.,Bezdudny, Andrii V.,Komarova, Igor V.
scheme or table, p. 1827 - 1829 (2009/12/04)
Trifluoromethyl-substituted analogues of the 1-amino-cyclobutane-1- carboxylic acid - 1-amino-3-(trifluoromethyl) cyclobutanecarboxylic and 1-amino-3,3-bis(trifluoromethyl)cyclobutane-carboxylic acids - have been synthesized from 1,3-dibromoacetone dimethyl ketal. The key step of the syntheses is a transformation of the acid moiety into the trifluoromethyl group using SF4 and HF. Georg Thieme Verlag Stuttgart.
AZETIDINE AND CYCLOBUTANE DERIVATIVES AS JAK INHIBITORS
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Page/Page column 52, (2009/09/28)
The present invention relates to azetidine and cyclobutane derivatives, as well as their compositions, methods of use, and processes for preparation, which are JAK inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.