3697-66-3Relevant academic research and scientific papers
Efficient method for removal of a carboxylic acid moiety from sterically crowded cyclopropanedicarboxylic acid derivatives
Hell, Zoltan,Toke, Laszlo
, p. 2127 - 2133 (1996)
A versatile method was developed to the dealkoxycarbonylation of sterically crowded cyclopropanecarboxylic acid derivatives via a nonhydrolytic ester cleavage followed by a Barton-type decarboxylation.
BICYCLIC KETONE COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 124; 125, (2019/02/02)
The invention provides novel compounds having the general formula (I): (I) wherein R1, the A ring and the B ring are as described herein, pharmaceutical compositions including the compounds, and methods of using the compounds.
SPIROCYCLE COMPOUNDS AND METHODS OF MAKING AND USING SAME
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Paragraph 00318, (2019/03/17)
Provided herein are compounds and compositions useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
A 4, 7 - diaza spiro [2.5] octane -7 - formic acid tert-butyl synthetic method
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Paragraph 0038; 0051; 0055; 0056, (2019/01/08)
The invention belongs to the technical field of chemical synthesis of N-heterocycle-containing drug intermediates, and particularly relates to a synthesis method of tert-butyl 4,7-diazaspiro[2.5]octyl-7-formate. By using diethyl malonate as a raw material, cyclization reaction, Hofmann reaction, hydrolysis reaction, acylation reaction for recyclization, reduction reaction and the like are performed to conveniently synthesize the target compound product. The method has the advantages of simple synthesis technique, cheap and accessible raw materials, mild reaction conditions, high controllability, low cost and high yield, and is convenient to operate.
TYROSINE KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0380; 0381, (2018/03/25)
The present invention relates to a tyrosine kinase inhibitor and a pharmaceutical composition comprising same. The tyrosine kinase inhibitor of the present invention has the structures as shown in the following formula (I) or (II):
PYRIDAZINE DERIVATIVES AS RORC MODULATORS
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Page/Page column 192, (2018/05/24)
Compounds of formula (I): (I) or pharmaceutical salts thereof, wherein m, n,, p, q A, B, Ri, R2, R3, R4, R5, R6and R7are as defined herein. Also disclosed are methods of making the compounds and using the compounds as RORs modulators for treatment of inflammatory diseases such as arthritis.
A tyrosine kinase inhibitor and intermediate preparation method
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Paragraph 0124-0126, (2017/10/13)
The invention provides preparation methods of a tyrosine kinase inhibitor and intermediates thereof, specifically preparation methods of N-[3-fluoro-4-[[6-methoxy-7-[oxy]quinolin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (Foretinib), and analogs and intermediates thereof. 1,1-cyclopropane dicarboxylic acid diester is used as the raw material to prepare a compound of the formula VI; and the compound of the formula VI is hydrolyzed and then reacts with a compound of the formula VIII, so as to prepare the Foretinib and the analogs thereof. The condition of each reaction step is mild, the preparation method is easy to operate, the price of the raw materials is low, and thus the production cost is reduced, the yield is relatively high, and the preparation methods are suitable for industrialized production.
Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox
Hermant, Paul,Bosc, Damien,Piveteau, Catherine,Gealageas, Ronan,Lam, Baovy,Ronco, Cyril,Roignant, Matthieu,Tolojanahary, Hasina,Jean, Ludovic,Renard, Pierre-Yves,Lemdani, Mohamed,Bourotte, Marilyne,Herledan, Adrien,Bedart, Corentin,Biela, Alexandre,Leroux, Florence,Deprez, Benoit,Deprez-Poulain, Rebecca
, p. 9067 - 9089 (2017/11/14)
Hydroxamic acids are outstanding zinc chelating groups that can be used to design potent and selective metalloenzyme inhibitors in various therapeutic areas. Some hydroxamic acids display a high plasma clearance resulting in poor in vivo activity, though they may be very potent compounds in vitro. We designed a 57-member library of hydroxamic acids to explore the structure-plasma stability relationships in these series and to identify which enzyme(s) and which pharmacophores are critical for plasma stability. Arylesterases and carboxylesterases were identified as the main metabolic enzymes for hydroxamic acids. Finally, we suggest structural features to be introduced or removed to improve stability. This work thus provides the first medicinal chemistry toolbox (experimental procedures and structural guidance) to assess and control the plasma stability of hydroxamic acids and realize their full potential as in vivo pharmacological probes and therapeutic agents. This study is particularly relevant to preclinical development as it allows obtaining compounds equally stable in human and rodent models.
AMINO ESTER DERIVATIVES, SALTS THEREOF AND METHODS OF USE
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Paragraph 0384, (2016/08/17)
The present invention provides amino ester compounds, salts, and pharmaceutical formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
A tyrosine kinase inhibitor and wherein the intermediate preparation method
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Paragraph 0066; 0067; 0068, (2016/10/10)
The invention relates to a preparation method for a tyrosine kinase inhibitor and a midbody thereof. According to the method, a compound 1,1-cyclopropane dicarboxylic acid diester is taken as a raw material, and 1-((4-((6,7-dimethoxy quinoline-4-yl) oxy)
