930122-19-3Relevant academic research and scientific papers
Introduction of substituents on the 2-oxo-piperazine skeleton by [3+2] cycloaddition and subsequent transformation
Wierschem, Frank,Rück-Braun, Karola
, p. 431 - 436 (2006)
The 3,4-substituted 2-oxo-piperazines 5-9 are obtained by [3+2] cycloaddition from nitrone 1 and a variety of alkenes. Subsequent functionalization of the bicyclic adducts involves reductive N-O bond cleavage. A route towards libraries of immobilized 1,3-aminoalcohols with a 3,4-substituted 2-oxo-piperazine scaffold is briefly discussed for adducts derived from N-substituted maleic imides.
Dimer ester micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase
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Paragraph 0133; 0138; 0139; 0168, (2018/10/19)
The invention provides dimer ester micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase. The structure of the PROTACs is shown in the specification, wherein in a compound (I), L1 is C1-C30 linear or branched alkyl with or without a substituent group, and any carbon atom in L1 is optionally replaced by heteroatom; R1, R2, R3 and R4 are C1-C30 linear or branched alkyl with orwithout a substituent group, C1-C30 aryl with or a without substituent group, C1-C30 linear or branched alkylaryl with or without a substituent group or C1-C30 linear or branched aryl alkyl with or without a substituent group respectively and independently; X1, X2, X3 and X4 are halogen respectively and independently.
Dimer amide micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase
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Paragraph 0132; 0137; 0138, (2018/10/19)
The invention provides dimer amide micromolecule PROTACs for inducing MDM2 to self-degrade E3 ubiquitin ligase. The structure of the PROTACs is shown in the specification, wherein in a compound (I), L1 is C1-C30 linear or branched alkyl with or without a substituent group, and any carbon atom in L1 is optionally replaced by heteroatom; R1, R2, R3 and R4 are C1-C30 linear or branched alkyl with orwithout a substituent group, C1-C30 aryl with or without a substituent group, C1-C30 linear or branched alkylaryl with or without a substituent group or C1-C30 linear or branched aryl alkyl with or without a substituent group respectively and independently; X1, X2, X3 and X4 are halogen respectively and independently.
INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN
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Paragraph 0199; 0200, (2018/09/16)
Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of diseases and conditions.
MACROCYLIC PYRIMIDINE DERIVATIVES
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Page/Page column 151; 152, (2015/11/02)
The present invention relates to substituted macrocylic pyrimidine derivatives of Formula (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention have EF2K inhibitory activity and optionally also Vps34 inhibitory activity. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
