88950-64-5

Usage

Uses

Used in Pharmaceutical Synthesis:
1-(Boc-amino)cyclopropanecarboxylic acid is used as a reagent in the synthesis of pyrrolotriazinone derivatives, which are therapeutic PI3K inhibitors. These inhibitors play a crucial role in the regulation of cellular processes such as cell growth, survival, and metabolism, making them potential targets for the treatment of various diseases, including cancer.
Used in Antitumor Agent Development:
1-(Boc-amino)cyclopropanecarboxylic acid is also used as a reagent in the synthesis of ether, carbamate, and ester derivatives of adarotene, which are potential antitumor agents. Adarotene is a compound with significant antitumor activity, and its derivatives may offer improved potency, selectivity, and reduced side effects in cancer treatment.

Upstream product

• 22059-21-8 aminocyclopropane-1-carboxylic acid 
• 58632-95-4 2-(tert-Butoxycarbonyloxyimino)-2-phenylacetonitrile 
• 107017-73-2 tert-butyl (1-(hydroxymethyl)cyclopropyl)carbamate 
• 66494-26-6 methyl 1-[[(tert-butoxy)carbonyl]amino]cyclopropane-1-carboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 68781-13-5 α-amino-cyclopropanecarboxylic acid hydrochloride 
• 58632-95-4 2-(tert-Butoxycarbonyloxyimino)-2-phenylacetonitrile 
• 88950-54-3 N-(tert-butoxycarbonyl)-dehydroalanine p-nitrobenzyl ester 
• 88950-55-4 3-tert-Butoxycarbonylamino-4,5-dihydro-3H-pyrazole-3-carboxylic acid 4-nitro-benzyl ester 
• 308266-24-2 (N-tert-butoxycarbonyl)-1-(benzyloxymethyl)cyclopropylamine 
• 107259-05-2 1-tert-butoxycarbonylamino-cyclopropanecarboxylic Acid Ethyl Ester 
• 143521-34-0 benzyl 1-<(tert-butyloxy)carbonylamino>cyclopropane-1-carboxylate 
• 88950-60-1 1-tert-Butoxycarbonylamino-cyclopropanecarboxylic acid 4-nitro-benzyl ester 
• 152449-89-3 [1-((E)-Styryl)-cyclopropyl]-carbamic acid tert-butyl ester 

Downstream Products

• 126902-09-8 1-(t-butoxycarbonyl)aminocyclopropane-1-carbonyl-phenylalanine methyl ester 
• 507264-66-6 tert-butyl N-(1 -carbamoylcyclopropyl)carbamate 
• 66494-26-6 methyl 1-[[(tert-butoxy)carbonyl]amino]cyclopropane-1-carboxylate 
• 625122-56-7 tert-butyl 1-{[(phenylsulfonyl)amino]carbonyl}cyclopropylcarbamate 
• 861648-80-8 tert-butyl (1-((3,5-dichlorophenyl)carbamoyl)cyclopropyl)carbamate 
• 675833-68-8 [1-(3-fluoro-2'-methylsulfanyl-biphenyl-4-ylcarbamoyl)-cyclopropyl]-carbamic acid tert-butyl ester 
• 935430-84-5 methyl 4'-{[({1-[(tert-butoxycarbonyl)amino]cyclopropyl}carbonyl)amino]methyl}-3,3'-difluoro-1,1'-biphenyl-2-carboxylate 
• 925215-17-4 methyl 4'-{(1R)-1-[({1-[(tert-butoxycarbonyl)amino]cyclopropyl}carbonyl)amino]ethyl}-3-chloro-3'-fluoro-1,1'-biphenyl-2-carboxylate 
• 578729-19-8 (1-{1-[3,3'-difluoro-2'-(2-methyl-2H-tetrazol-5-yl)-biphenyl-4-yl]-ethylcarbamoyl}-cyclopropyl)-carbamic acid tert-butyl ester 
• 672960-03-1 C₁₆H₂₂N₂O₃ 
• 864642-89-7 tert-butyl 1-{[((1R)-1-{5-[3,5-dichloro-2-(2,2-difluoroethoxy)phenyl]-3-fluoropyridin-2-yl}ethyl)amino]carbonyl}cyclopropyl carbamate 

Relevant academic research and scientific papers

SUBSTITUTED TRIAZINONES AS THYROID HORMONE RECEPTOR AGONISTS

The application relates to a compound of Formula (I') or (I), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of thyroid hormone receptors, a pharmaceutical composition comprising a compound of Formula (I') or (I), and a method of treating or preventing a disease or disorder regulated by thyroid hormone.

TERTIARY AMINE COMPOUND OR IMINE COMPOUND-POLYMER CONJUGATE AND PRODUCTION METHOD THEREFOR

Provided is a compound obtained by conjugating a tertiary amine compound or imine compound, which is useful as a drug, with a polymer, in which a structure D+ having a quaternary ammonium salt or iminium salt formed from a tertiary amine compound or imine compound D and a polymer residue Poly having a carboxy group are bonded to each other via a structure —C(R1)(R2)OC(O)ANHC(═O)—.

Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1

ERAP1 is an endoplasmic reticulum-resident zinc aminopeptidase that plays an important role in the immune system by trimming peptides for loading onto major histocompatibility complex proteins. Here, we report discovery of the first inhibitors selective for ERAP1 over its paralogues ERAP2 and IRAP. Compound 1 (N-(N-(2-(1H-indol-3-yl)ethyl)carbamimidoyl)-2,5-difluorobenzenesulfonamide) and compound 2 (1-(1-(4-acetylpiperazine-1-carbonyl)cyclohexyl)-3-(p-tolyl)urea) are competitive inhibitors of ERAP1 aminopeptidase activity. Compound 3 (4-methoxy-3-(N-(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl)sulfamoyl)benzoic acid) allosterically activates ERAP1's hydrolysis of fluorogenic and chromogenic amino acid substrates but competitively inhibits its activity toward a nonamer peptide representative of physiological substrates. Compounds 2 and 3 inhibit antigen presentation in a cellular assay. Compound 3 displays higher potency for an ERAP1 variant associated with increased risk of autoimmune disease. These inhibitors provide mechanistic insights into the determinants of specificity for ERAP1, ERAP2, and IRAP and offer a new therapeutic approach of specifically inhibiting ERAP1 activity in vivo.

NLRP3 inflammasome inhibitor and preparation method and application thereof

The invention relates to a class of 1, 2, 3, 5, 6, 7 hexahydrosymmetric indacene compounds containing one or more substituents., pharmaceutically acceptable salts, esters or hydrates thereof, a preparation method thereof, a pharmaceutical composition containing the compounds, and an application of the compounds as a novel NLRP3 inflammasome inhibitor in preparation of drugs for preventing and/or treating diseases related to NLRP3 inflammasome.

Amine compound for inhibiting SSAO/VAP-1 and application thereof in medicines

The present invention relates to an amine compound for inhibiting SSAO/VAP-1 and application thereof in medicines. In particular, the present invention relates to an amine compound for inhibiting a semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1) inhibitor, or a pharmaceutically acceptable salt thereof, a stereoisomer or an/a E/Z isomer, further relates to a pharmaceutical composition containing the amine compound. The invention further relates to the application of the amine compound and the pharmaceutical composition in manufacture of the medicines for treatment of inflammation, inflammation-related diseases and immune diseases.

A 4, 7 - diaza spiro [2.5] octane -7 - formic acid tert-butyl synthetic method

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.

NOVEL SUBSTITUTED AMIDES OF TRITERPENE DERIVATIVES AS HIV INHIBITORS

The present invention relates to compounds of novel substituted amides of triteripene derivatives of formula (I); or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable hydrates, tautomers, stereoisomers, prodrugs, compositions or combination thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y, Z1, Z2, Z3 and formula (II) are as defined herein. The present invention also relates to,, and pharmaceutical compositions comprising compounds of formula (I) useful for the treatment of viral diseases and particularly HIV mediated diseases.

C-3 NOVEL TRITERPENONE WITH C-28 REVERSE AMIDE DERIVATIVES AS HIV INHIBITORS

Formula (I) The invention relates to C-3 novel triterpenone with C-28 reverse amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.

NOVEL COMPOUND HAVING ABILITY TO INHIBIT 11B-HSD1 ENZYME OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11β-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11β-HSD1 (11β-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11β-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.

NOVEL COMPOUND HAVING ABILITY TO INHIBIT 11B-HSD1 ENZYME OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11β-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11β-HSD1 (11β-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11β-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.