685-89-2Relevant academic research and scientific papers
HETEROARYL COMPOUNDS FOR TREATMENT OF COMPLEMENT FACTOR D MEDIATED DISORDERS
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Paragraph 112; 148-149, (2021/08/27)
Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.
INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
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Page/Page column 162, (2018/06/30)
Compounds of formula (I') and methods of their use and preparation, as well as compositions comprising compounds of formula (I').
ARYL, HETEROARY, AND HETEROCYCLIC PHARMACEUTICAL COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Page/Page column 48, (2018/09/21)
Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
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Page/Page column 162, (2017/09/02)
The present disclosure is directed to compounds of formula I and methods of their use and preparation, as well as compositions comprising compounds of formula I.
QUINOLINE EZH2 INHIBITORS
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Page/Page column 74-75, (2017/03/08)
The present invention relates to quinolines of general formula (I) to methods for their preparation, to intermediates for their preparation, to pharmaceutical compositions comprising at least one of those compounds, and to the use thereof.
PYRROLIDINE DERIVATIVES AND THEIR USE AS COMPLEMENT PATHWAY MODULATORS
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Page/Page column 58, (2014/01/17)
The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as a factor D inhibitor for the treatment of ophthalmic diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Scope and limitations of the Julia-Kocienski reaction with fluorinated sulfonylesters
Calata, Charlène,Catel, Jean-Marie,Pfund, Emmanuel,Lequeux, Thierry
body text, p. 3967 - 3973 (2009/09/25)
The study of the Julia-Kocienski reaction between fluorinated arylsulfone and ketones is described. The corresponding fluoroalkenes were isolated in moderate to good yields from β- and δ-substituted cyclic ketones. From acyclic ketones and α-substituted c
SPIROINDOLINONE DERIVATIVES
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Page/Page column 89-90, (2008/06/13)
The present invention relates to spiroindolinone derivatives of the formula and their enantiomers and pharmaceutically acceptable salts and esters thereof wherein R1, R2, R3, R4, R5, R6, R7 and R8, are as herein described.
A ONE-POT SYNTHESIS OF UNSYMMETRICAL AND SYMMETRICAL TETRASUBSTITUTED α-FLUORO-α,β-UNSATURATED ESTERS
Tsai, Hou-Jen,Thenappan, Alagappan,Burton, Donald J.
, p. 205 - 212 (2007/10/02)
Acylation of -Li+ 1 with acid chlorides RC(O)Cl or phosgene ClC(O)Cl and subsequent reaction of the acylated phosphonate with organometallic reagents (R'M) provide unsymmetrical and symmetrical tetrasubstituted α-f
Conversion of α-keto esters into β,β-difluoro-α-keto esters and corresponding acids: A simple route to a novel class of serine protease inhibitors
Parisi,Gattuso,Notti,Raymo,Abeles
, p. 5174 - 5179 (2007/10/02)
The preparation of a series of β,β-difluoro-α-keto esters and corresponding acids RCF2COCO2R' (R=Me, Et, i-Pr, Bn, and Ph; R'=Et and H), designed as potential inhibitors of serine proteases, is described. The standard procedure developed consists in the initial formation of an α,α- difluoro ester from an α-keto ester, followed by a simple four-step sequence involving the synthesis of hemiacetal, cyanohydrin, and α-hydroxy ester difluorinated intermediates. This method provides an easy route to β,β- difluoro-α-keto esters and corresponding acids, via 'formal' insertion of a difluoromethylene group between the R substituent and the α-carbonyl group of a generic α-keto ester.
