474013-77-9Relevant academic research and scientific papers
AMIDO-SUBSTITUTED CYCLOHEXANE DERIVATIVES
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Page/Page column 131; 132, (2018/05/24)
The present invention relates to amido-substituted cyclohexane compounds of general formula (I) : in which m, A, R4, R6, R7, R8, R9, R10 and R11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
A class of 4, 5 - disubstituted imidazole derivatives and its preparation and use (by machine translation)
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Paragraph 0087; 0090; 0091, (2017/07/22)
The invention relates to a compound of general formula I indicated by the 4, 5 - disubstituted imidazole compound, or its pharmaceutically acceptable salt, pharmaceutical composition containing the same and its preparation and use, the compounds can be used as a xanthine oxidase (Xanthine oxidase, XO) inhibitor, used for the treatment of uric acid crystallization at the joints to the deposition of Gout and its complications. (by machine translation)
AMIDO-SUBSTITUTED AZOLE COMPOUNDS
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Page/Page column 86-87, (2017/08/01)
The present invention relates to amido-substituted azole compounds of general formula (I), in which X1, X2, R1, R2, R4, R5, R7 and R8 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
AMIDO-SUBSTITUTED CYCLOHEXANE DERIVATIVES
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Page/Page column 187; 188, (2016/11/21)
The present invention relates to amido-substituted cyclohexane compounds of general formula (I), in which A, R4, R6, R7, R8, R9, R10 and R11 are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredient.
AMIDO-SUBSTITUTED AZOLE COMPOUNDS
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Page/Page column 181, (2015/11/02)
The present invention relates to amido-substituted azole compounds of general formula (I), in which X1, X2, R1, R2, R4, R5, R7 and R8 are as defined in the claims which are inhibitors of TNKS1 and/or TNKS2, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
Discovery of a novel 5-carbonyl-1H-imidazole-4-carboxamide class of inhibitors of the HIV-1 integrase-LEDGF/p75 interaction
Serrao, Erik,Xu, Zhong-Liang,Debnath, Bikash,Christ, Frauke,Debyser, Zeger,Long, Ya-Qiu,Neamati, Nouri
, p. 5963 - 5972 (2013/09/23)
Though much progress has been made in the inhibition of HIV-1 integrase catalysis, clinical resistance mutations have limited the promise of long-term drug prescription. Consequently, allosteric inhibition of integrase activity has emerged as a promising approach to antiretroviral discovery and development. Specifically, inhibitors of the interaction between HIV-1 integrase and cellular cofactor LEDGF/p75 have been validated to diminish proviral integration in cells and deliver a potent reduction in viral replicative capacity. Here, we have contributed to the development of novel allosteric integrase inhibitors with a high-throughput AlphaScreen-based random screening approach, with which we have identified novel 5-carbonyl-1H-imidazole-4-carboxamides capable of inhibiting the HIV-1 integrase-LEDGF/p75 interaction in vitro. Following a structure-activity relationship analysis of the initial 1H-imidazole-4,5- dicarbonyl core, we optimized the compound's structure through an industrial database search, and we went further to synthesize a selective and non-cytotoxic panel of inhibitors with enhanced potency.
CYCLIC IMINOCARBAMATES AND USE THEREOF
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Page/Page column 34, (2010/11/08)
The invention relates to novel cyclic iminocarbamates of formula (I), wherein R1, R2, R3, A, Z and n have the meaning cited in the description, to a method for the production thereof, to the use thereof for treating and/or for the prophylaxis of illnesses, and to the use thereof in the production of medicaments for treating and/or for the prophylaxis of diseases, in particular of thromboembolic diseases.
An improved method for the synthesis of dissymmetric N,N′-disubstituted imidazole-4,5-dicarboxamides
Wiznycia, Alexander V.,Baures, Paul W.
, p. 7151 - 7154 (2007/10/03)
Symmetrically and dissymmetrically disubstituted imidazole-4,5-dicarboxamides (I45DCs) have diverse bioactivities and therefore represent useful small molecules for lead structure identification in drug discovery. For this reason, an improved synthesis was developed as a first step in the preparation of greater numbers of analogues. The method involves the transformation of imidazole-4,5-dicarboxylic acid into dissymmetrically disubstituted I45DCs in four steps and in a minimum yield of 51%. This reflects an overall reduction of one synthetic step and a greater than 30% improvement in yield over the known method.
