- Gold-Catalyzed Amide/Carbamate-Linked N, O-Acetal Formation with Bulky Amides and Alcohols
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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.
- Ohsawa, Kosuke,Ochiai, Shota,Kubota, Junya,Doi, Takayuki
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p. 1281 - 1291
(2021/01/14)
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- PTERIDINONE COMPOUNDS AND USES THEREOF
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The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).
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Paragraph 0478; 0581
(2019/11/11)
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- A 4, 7 - diaza spiro [2.5] octane -7 - formic acid tert-butyl synthetic method
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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.
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Paragraph 0033; 0039; 0040
(2019/01/08)
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- FLUOROMETHYL-SUBSTITUTED PYRROLE CARBOXAMIDES III
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The invention relates to pyrrole carboxamides bearing a fluoromethyl- moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pa
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Page/Page column 59; 60
(2015/07/07)
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- Potent ketoamide inhibitors of HCV NS3 protease derived from quaternized P1 groups
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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.
- Venkatraman, Srikanth,Velazquez, Francisco,Wu, Wanli,Blackman, Melissa,Madison, Vincent,Njoroge, F. George
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scheme or table
p. 2151 - 2155
(2010/06/19)
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- Oxazolidone derivatives as PR modulators
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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.
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Page/Page column 21
(2008/06/13)
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- Chemokine receptor binding heterocyclic compounds with enhanced efficacy
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The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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Page/Page column 49-50
(2010/02/03)
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- Synthesis and structure-activity relationships of 7-[3-(1- aminoalkyl)pyrrolidinyl]- and 7-[3-1-aminocycloalkyl)pyrrolidinyl]-quinolone antibacterials
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A series of 7-[3-(1-aminoalkyl and 1-aminocycloalkyl)-1- pyrrolidinyl]quinolones have been prepared and their biological properties evaluated. Among them, 1-(S)-aminoalkyl derivatives exhibited potent antibacterial activities against gram-positive and gram-negative organisms. They had moderate lipophilicity and high aqueous solubility compared to their aminomethyl counterparts; e.g., the 3-(1-aminoethyl)-1-pyrrolidinyl compound (83) showed superior pharmacokinetic properties to its aminomethyl counterpart (6).
- Kimura,Atarashi,Takahashi,Hayakawa
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p. 1442 - 1454
(2007/10/02)
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- Pyridonecarboxylic acid derivatives
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This invention provides novel pyridonecarboxylic acid derivatives having a quite high antimicrobial activity. The derivatives have the following formula: STR1 wherein R1, R2 and R3 represent each a hydrogen or C1 -C6 alkyl group; R4 represents an ethyl, 2-fluoroethyl, vinyl, isopropyl, isopropenyl or cyclopropyl group; and X represents CH, C-F, C-Cl or N wherein (i) one of R1, R2 and R3 represents a hydrogen or C1 -C6 alkyl group, and (ii) either R1 forms a methylene chain having 2 to 4 carbon atoms together with R2 or R3, or R2 and R3 form together an alkylene chain having 2 to 5 atoms and R4 represents an ethyl, 2-fluorethyl, vinyl, isopropyl, isopropenyl or cyclopropyl group and X represents CH, C-F, or C-Cl and salt thereof.
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- A CONVENIENT AND EFFICIENT SYNTHESIS OF 1-AMINOCYCLOPROPANECARBOXYLIC ACID (ACC)
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A straightforward synthesis of 1-aminocyclopropanecarboxylic acid (ACC) has been developed.The key step in the synthesis is the thermal conversion of 1-t-butoxycarbonylcyclopropanecarboxylic acid to ACC.
- Wheeler, Thomas N.,Ray, John A.
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p. 141 - 150
(2007/10/02)
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- New "Ofloxacin" Type Antibacterial Agents. Incorporation of the Spiro Cyclopropyl Group at N-1
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The first example incorporating a spiro cyclopropyl group into an "ofloxacin" type of quinolone antibacterial agent has been prepared by potassium fluoride mediated ring closure of the hydroxymethyl cyclopropyl intermediate to give 9'-fluoro-7'-oxo-10'-(1-piperazinyl)spiropyridobenzoxazine>-6'-carboxylic acid.Analogues were made by substitution at C-7 by various complex amines.Evaluation of these compounds for antibacterial activity was carried out.All examples prepared and examined showed in vitro minimum inhibitory values and in vivo mouse protection results to be diminished as compared to the parent, ofloxacin.
- Kiely, John S.,Schroeder, Mel C.,Sesnie, Josephine C.
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p. 2004 - 2008
(2007/10/02)
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- Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative
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A novel conformationally restricted 1-cyclopropylquinolone (1) that incorporates structural features of both ofloxacin and ciprofloxacin has been prepared. Compound 1 was found to be a DNA gyrase inhibitor having potency similar to ofloxacin but less than
- Wentland,Perni,Dorff,Rake
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p. 1694 - 1697
(2007/10/02)
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