42303-42-4Relevant articles and documents
Gold-Catalyzed Amide/Carbamate-Linked N, O-Acetal Formation with Bulky Amides and Alcohols
Ohsawa, Kosuke,Ochiai, Shota,Kubota, Junya,Doi, Takayuki
, p. 1281 - 1291 (2021/01/14)
A gold-catalyzed N,O-acetal formation was established to construct an amide/carbamate-linked N,O-acetal substructure with bulky alcohols. The acyliminium cation species generated from o-alkynylbenzoic acid ester in the presence of a gold catalyst is highly reactive and underwent nucleophilic attack of various bulky alcohols and phenols at room temperature under neutral conditions, leading to the corresponding N,O-acetals in yields of 34-89% with good functional group tolerance.
Preparation method of 4,7-diazaspiro[2.5]octane derivative
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Paragraph 0073; 0074; 0075; 0076, (2018/12/13)
The invention provides a preparation method of 4,7-diazaspiro[2.5]octane derivative. The 4,7-diazaspiro[2.5]octane derivative is prepared by taking 1-aminocyclopropane carboxylate as a starting material. The preparation method has the advantages of simple operation steps, stable process conditions, high controllability, high product yield (the four-step reaction yield of compounds shown as formulas II to I can be up to 70 percent), environmental friendliness and the like, and is suitable for large-scale production.
NOVEL COMPOUNDS
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Page/Page column 92; 93, (2015/11/10)
The present invention relates to inhibitors of the Wnt signalling pathways of general formula (I) as described and 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 a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.
NOVEL COMPOUNDS
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Page/Page column 117, (2014/10/03)
The present invention relates substituted N-biphenyl-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-biphenyl-carboxamides of general formula (I) as described and 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 a hyper-proliferative disorder, as a sole agent or in combination with other active ingredients.
NOVEL COMPOUNDS
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Page/Page column 129, (2014/10/03)
The present invention relates to substituted N-(phenyl-heteroaryl)-3-acetylamino-benzamides and N- [3-(acetylamino)phenyl]-phenyl-heteroaryl-carboxamides of general formula(I) as described and 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.
Potent ketoamide inhibitors of HCV NS3 protease derived from quaternized P1 groups
Venkatraman, Srikanth,Velazquez, Francisco,Wu, Wanli,Blackman, Melissa,Madison, Vincent,Njoroge, F. George
scheme or table, p. 2151 - 2155 (2010/06/19)
Blood borne hepatitis C infections are the primary cause for liver cirrhosis and hepatocellular carcinoma. HCV NS3 protease, a pivotal enzyme in the replication cycle of HCV virus has been the primary target for development of new drug candidates. Boceprevir and telaprevir are two novel ketoamide derived inhibitors that are currently undergoing phase-III clinical trials. These inhibitors include ketoamide functionality as serine trap and have an acidic alpha-ketoamide center that undergoes epimerization under physiological conditions. Our initial attempts to arrest this epimerization by introducing quaternary amino acids at P1 had resulted in significantly diminished activity. In this manuscript we describe alpha quaternized P1 group that result in potent inhibitors in the enzyme assay and demonstrate cellular activity comparable to boceprevir.
Oxazolidone derivatives as PR modulators
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, (2008/06/13)
Compounds of the following structure are described: wherein R1, R2, R5, R6, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing fibroids, endometriosis, dysfunctional bleeding, uterine leiomyomata, polycystic ovary syndrome, or hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake or synchronizing estrus.
2-Thiohydantoine derivative compounds and use thereof for the treatment of diabetes
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Page/Page column 9, (2010/02/15)
The invention relates to 2-thiohydantoin compounds selected from compounds of general formula (I): in which, in particular, one of the radicals R1 and R2 comprises two aromatic rings in the structure or is the dibenzofuranyl group, R3 is a hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxy group, a hydroxyl group, a phenyl group or a benzyl group, R4 is a hydrogen atom, a halogen atom or a C1-C4 alkyl group, and their addition salts with a non-toxic acid, especially the pharmaceutically acceptable salts. It further relates to the process for their preparation, to the pharmaceutical compositions in which they are present, and to their use as pharmacologically active substances, especially in the case of the treatment of diabetes, diseases due to hyperglycemia, hypertriglyceridemia, dyslipidemia or obesity.
Inactivation of γ-Aminobutyric Acid Aminotransferase by (S,E)-4-Amino-5-fluoropent-2-enoic Acid and Effect on the Enzyme of (E)-3-(1-Aminocyclopropyl)-2-propenoic Acid
Silverman, Richard B.,Invergo, Benedict J.,Mathew, Jacob
, p. 1840 - 1846 (2007/10/02)
(S,E)-4-Amino-5-fluoropent-2-enoic acid (6) is synthesized in six steps starting from the known γ-aminobutyric acid aminotransferase (γ-Abu-T) inactivator, (S)-4-amino-5-fluoropentanoic acid (1).Compound 6 is a mechanism-based inactivator of γ-Abu-T: time-dependent inactivation is saturable and protected by substrate; thiols do not protect the enzyme from inactivation; no enzyme activity returns upon dialysis.This compound (6) binds 50 times more tightly to γ-Abu-T than does the saturated analogue (1).No transamination of 6 occurs prior to inactivation.However, five molecules of 6 are required to inactivate the enzyme with concomitant release of five fluoride ions.Therefore, four molecules are being converted to product for each inactivation event. (E)-3-(1-Aminocyclopropyl)-2-propenoic acid is synthesized in seven steps from 1-aminocyclopropanecarboxylic acid.It is prepared as a cyclopropyl derivative of the proposed intermediate in the inactivation of γ-Abu-T by 6.The cyclopropyl derivative, however, is a noncompetitive inhibitor and does not inactivate the enzyme.This study shows the usefulness and hazards of incorporation of a trans double bond into potential γ-Abu-T inactivators.