867065-53-0Relevant academic research and scientific papers
Chemo-selective syntheses of: N-t -boc-protected amino ester analogs through Buchwald-Hartwig amination
Karambizi, Victoire G.,O'Brien, Gregory,Rahman, Mahmuda,Scott Goodman, M.,Suwal, Sujit,Wrotny, Matthew
supporting information, p. 2605 - 2608 (2022/02/22)
The synthesis of N-protected amino esters is achieved via a chemo-selective Buchwald Hartwig cross-coupling reaction using PEPPSI-IPr Pd-catalyst. Nearly two dozen functionally and structurally diverse amino ester molecules are created by individually cross-coupling eight aryl halo esters and three different secondary amines. We observed that product formation is more facile in those heterocyclic esters where nitrogen is present ortho to the halo substituent in the heteroaromatic ring. Based on this observation, we propose a possible intermediate step in the cross-coupling cycle, where the nitrogen electron lone pair in the heterocycle may play an important role leading to a higher reaction yield.
SMARCA2-VHL DEGRADERS
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Page/Page column 49-50, (2021/07/17)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
SELECTIVE HDAC1,2 INHIBITORS
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Paragraph 0599; 0600; 0601, (2018/06/04)
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
INHIBITORS OF PHOSPHOINOSITIDE 3-KINASE AND HISTONE DEACETYLASE FOR TREATMENT OF CANCER
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Paragraph 00208, (2019/01/10)
The present invention is directed to a dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), including a core containing a quinazoline moiety or a quinazolin-4(3H)-one moiety, a kinase hinge binding moiety, and a histone deacetylase pharmacophore, a pharmaceutically acceptable salt thereof, a prodrug thereof, or solvate thereof. The present invention is also directed to a histone deacetylase inhibitor, including a core containing a quinazolin-4(3H)-one moiety and a histone deacetylase pharmacophore.
OXYMETHYLENE ARYL COMPOUNDS FOR TREATING INFLAMMATORY GASTROINTESTINAL DISEASES OR GASTROINTESTINAL CONDITIONS
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Paragraph 0479; 0480, (2018/03/28)
Use of oxymethylene aryl GPRl 19 agonists, and optionally DPP IV inhibitors and optionally metformin, for the treatment of inflammatory gastrointestinal diseases or gastrointestinal conditions involving malabsorption of nutrients and/or fluids are provide
ACID ADDITION SALTS OF PIPERAZINE DERIVATIVES
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, (2017/09/09)
The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and in particular as glycosidase inhibitors.
GLYCOSIDASE INHIBITORS
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, (2016/03/22)
Compounds of formula (I) wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
HETEROCYCLIC RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND METABOLIC DISORDERS
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Page/Page column 112, (2008/12/07)
Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control. The compounds of the invention are orally active.
FUNGICIDAL MIXTURES
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Page/Page column 108, (2008/12/07)
Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1 N-oxides, and salts thereof, insert Formula 1 here wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of the aforesaid composition.
FUNGICIDAL CARBOXAMIDES
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Page/Page column 91, (2010/11/25)
This invention is directed to compounds of Formula (1) including all geometric and stereoisomers, N oxides, and agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides, ( l ) provided that the compound of Formula 1 is other than 2-[1-[(2-chlorophenyl)acetyl]-4-piperidinyl]-N-methyl-N-[(1R)-1-phenylethyl]-4-thiazolecarboxamide and R1 is other than 4-fluorophenyl; wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, Also disclosed are compositions containing the a compound having a formula corresponding to Formula 1 where the provisos are both omitted; and methods for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound having a formula corresponding to Formula (1) where the provisos are both omitted.
