I-China 67630-00-6 I-Tert-butoxycarbonyl-4-NO2-phenylalanine-ethyl ester Umkhiqizi kanye Nemboni |Jiayinglai

67630-00-6 Tert-butoxycarbonyl-4-NO2-phenylalanine-ethyl ester

Incazelo emfushane:

Ukubukeka	Amakristalu amhlophe kuya kokumhlophe noma impushana ecwebezelayo.
MF	I-C16H22N2O6
MW	338.36
Ubumsulwa	98+

Thumela i-imeyili kithi

Imininingwane Yomkhiqizo

Isimo sezokuthutha&indlela yokuthumela enconyiwe:
ngomoya, ngolwandle noma nge-express

Isimo sesitoreji:
Kuvalwe endaweni eyomile, Ngezinga lokushisa Legumbi

Ubuncane be-oda Ubuningi:
Ukuxoxisana

Isitifiketi:
I-COA, HPLC, GC, HNMR, Assay, Water Content(KF), TLC iyatholakala

Omqondofana

(S)-ethyl 2-(tert-butoxycarbonylaMino)-3-(4-nitrophenyl)propanoate;
I-Boc-(4-NO2)-L-Phe-OEt;
I-Boc-(4-NO2)-Oet;
I-Boc-Phe(4-NO2)-Oet;
L-Phenylalanine;
N-[(1,1-dimethylethoxy)carbonyl]-4-nitro-, i-ethyl ester

Ukupakisha kwangaphakathi

Ngokuvamile zisetshenziselwa ukupakisha impushana.Futhi zingavimbela ukukhanya kwelanga namanzi ukuba kungabi kubi.

ukupakisha kwangaphandle

Ibhokisi eliqinile lingavikela imikhiqizo yakho ukuthi ingaphahlazeka futhi ibe manzi.

Izinhlelo zokusebenza

I-Nidanib, ikhemikhali.Igama lekhemikhali 1 h - indole - 6 - carboxylic acid, 2, 3 - dihydro - 3 - [[[4 - (methyl [(4 - methyl - 1 - piperazine) acetyl] amino] phenyl] amino]ne heartland ye-methyl] - 2 - oxygen -, methyl ester, (z) - Ngokomtholampilo, lo mkhiqizo usetshenziselwa ukwelapha idiopathic pulmonary fibrosis (IPF).
I-Nidanib ifunde iziguli eziyi-1,529 ezine-idiopathic pulmonary fibrosis (IPF) ezivivinyweni eziningi zomtholampilo.Idatha yokuphepha eyethulwa isekelwe ekuqhathanisweni kweziguli eziyi-1061 ezinikezwe i-nidanib 150 mg kabili ngosuku kanye ne-placebo esigabeni sesi-3 samaviki angu-52, okungahleliwe, okungaboni kabili, izifundo ezilawulwa yi-placebo (INPULSIS-1 kanye ne-INPULSIS-2).Izenzakalo ezimbi ezivame kakhulu ezihlobene nokusetshenziswa kwe-nidanib zazihlanganisa isifo sohudo, isicanucanu nokuhlanza, ubuhlungu besisu, ukulahlekelwa ukudla, ukuncipha kwesisindo, kanye nama-enzyme esibindi aphakeme.Sicela ubhekisele kokuthi [Izixwayiso] ukuze uthole ukuphathwa kokusabela okungalungile okuhambisanayo.I-Systematic Organ Classification (SOC) ye-MedDRA inikeza isifinyezo sokusabela okungekuhle nokuhlukaniswa kwemvamisa.
I-Nidanib iyi-substrate ye-P-gp (bona i-Pharmacokinetics).Ocwaningweni oluthile lokusebenzisana kwezidakamizwa, ukuphathwa okuhlangene kwe-ketoconazole, i-P-gp inhibitor enamandla, ukwanda kokuchayeka ku-nidanib kuya ezikhathini eziyi-1.61 ngendawo engaphansi kwejika (AUC) kanye nezikhathi eziyi-1.83 ngokugxila okuphezulu (Cmax).
Ocwaningweni lokusebenzelana kwezidakamizwa ne-P-gp inducer rifampicin enamandla, ukuchayeka ku-nidanib kwehle kwafika ku-50.3%, njengoba kulinganiswa ngendawo engaphansi kwejika (AUC), uma kuhlanganiswa ne-rifampicin uma kuqhathaniswa ne-Nidanib iyodwa.Ngokugxila okuphezulu (Cmax), kwehle kwafika ku-60.3%.
Uma isetshenziswa ngokuhambisana nalo mkhiqizo, ama-P-gp inhibitors anamandla (isb., i-ketoconazole noma i-erythromycin) angandisa ukuchayeka ku-nidanib.Kulezi zimo, ukubekezelela kwesiguli i-nidanib kufanele kuqashwe ngokucophelela.Ukulawula ukusabela okubi kungase kudinge ukuyekiswa, ukuncishiswa komthamo, noma ukuyekiswa kokwelashwa ngalo mkhiqizo (bona [Ukusetshenziswa nomthamo]).
I-P-gp inducers enamandla (isb, i-rifampicin, i-carbamazepine, i-phenytoin ne-St. John's wort) inganciphisa ukuchayeka ku-nidanib.Okunye ukuhlanganisa okungenayo noma okuncane kokungeniswa kwe-P-gp kufanele kucatshangelwe.

imikhiqizo ehlobene

Gly-Phe	Boc-Phe-Gly-Ome	HN-Me-L-Phe.Hcl	Boc-D-Phe-D-Phe
I-Boc-D-4-Chloropheny(alanine)	Fmoc-L-Phe-OH	I-L-Phe-NH2.Hcl	Boc-Phe-Gly
L-Ala-Phe-OH	Fmoc-D-Phe-OH	4-NO2-Phe-Oet	I-Boc-L-Phe-Onp
Boc-Ala-Phe-OH	Fmoc-N-Me-L-Phe-OH	4-NO2-Phe-Oet.HCl	Boc-L-Phe-Oet
Boc-Ala-Phe-OH	FMOC-N-Me-D-Phe-OH	I-HD-Phe-OMe·HCl	I-Boc-4-NO2-D-Phe-OEt
Fmoc-β-Ala-D-phe	Fmoc-Phe-Cl	HL-Phe-OMe.HCl	I-Boc-D,L-Phe(4-NO2)-OH
I-Leu-Phe.Hcl	I-Fmoc-Phe(4-NO2)-OH	H-DL-Phe-OBzl .tos	Fmoc-Phe-Phe-OH
Boc-Leu-Phe	Cbz-L-Phe-OH	I-H-DL-Phe(4-NO2)-OH.H2O	Fmoc-Phe-Gly-OH
Cbz-L-Phe-Leu-OH	Cbz-D-Phe-OH	HL-Phe-OBzl.HCl	I-Fmoc-D-Phe(4-NO2)-OH
L-Phe	Cbz-DL-Phe-OH	I-HL-Phe-OEt.HCl	Cbz-Phe-Arg-OH
I-HD-Phe-OH	Cbz-D-Phe-OL	I-L-Phe-NH2	Cbz-Phe-Ala-OH
L-Phe-NCA	ZN-Me-L-Phe-OH	I-D-Phe-NH2	Cbz-Phe-Gly-OH
I-Tos-Phe	cbz-L-Phe-OSU	N-Ac-L-Phe-OH	Cbz-Phe-Met-OH
L-Phe-ol	Phe-Ala	N-AC-L-Phe-Ome	Cbz-Phe-Gly-Oet
I-L-Phe (4-NO2)-OH	L-Phe-Phe	N-Pht-Phe-OH	I-Boc-Phe-Gly-Gly-OH
I-L-Phe (4-NO2).H2O	I-L-Phe-Trp	Boc-Phe-OH	I-Fmoc-L-Thr(tBu)-Phe-OH
I-D-Phe(4-NO2)-OH.h2o	L-Phe-Leu-OH	I-Boc-D-Phe-OH	I-D-Phe-NH2
I-D-Phe(4-NO2)-OH	L-Phe-Tyr-OH	I-Boc-DL-Phe-OH	I-Tyr-Phe
N-Me-D-Phe	L-Phe-Gly	BOC-N-Me-D-Phe-OH	I-DL-Phe-Ome.Hcl
HN-Me-L-Phe-OH	D-Phe-D-Phe	I-Boc-N-Me-DL-Phe-OH	Boc-Met-Leu-Phe
L-Phe.hcl	L-Phe-OBzl-OH	Boc-N-Me-L-Phe-OH	I-Asp-Phe-Ome
4-NO2-D-phe.hcl	I-D-Phe-Obzl.Tos	Boc-N-Me-L-Phe-OH.DCHA	L-Homophe-OH
HL-Phe-OtBu.HCl	Boc-Phe-Ala-OH	I-Boc-DN-Me-Phe•DCHA	D-Homophe-OH
I-HD-Phe-OtBu.HCl	Boc-Phe-Leu-OH	Boc-Phe-Ol	L-Homophe-Oet.Hcl
D,L-Phe-OtBu HCl	I-Boc-Phe-Trp-OH	I-Boc-D-Phe-Ol	I-D-Homophe-Oet.HCl
I-HD-Phe(4-NO2)-Ome.HCl	I-Boc-L-Phe-Tyr-OH	I-Boc-Phe-NH2	Boc-L-Homophe-OH
I-D-Phe-Obzl.Hcl	Boc-Phe-Phe-OH	Boc-L-Phe-Ome	I-Boc-D-Homophe-OH
I-DL-Phe-Ome.Hcl	Boc-D-Phe-Phe	Boc-D-Phe-Ome	Fmoc-L-HomoPhe-OH
I-Boc-D-Phe(4-NO2)-OH	Cbz-D-Homophe-OH	Boc-Phe-Obzl	I-Fmoc-D-Homophe-OH
I-Boc-L-Phe-OSU	Boc-Homophe-Leu-Phe-Ome	I-Boc-4-NO2-Phe-OH	Cbz-L-Homophe-OH
I-Boc-D-Phe-OSU

Ukuphakama

1. Isevisi ye-R&D iyatholakala
2. Umkhiqizi oqinisekisiwe we-ISO, isiqinisekiso sekhwalithi
I-3.Inkambo ephelele yenkonzo yokulandelela ngesikhathi sokukhiqiza
I-4.Izindleko eziphezulu
5.Imibhalo yesitifiketi sekhwalithi enikeziwe ngokwesicelo sekhasimende ngalinye
I-6.Isevisi enhle emva kokuthengisa, ukugcina ubuhlobo obuseduze nekhasimende
7.Insiza egcwele yokusiza ukwehlisa izindleko zokuthumela
8.Isampula yamahhala enikelwe ukuhlola ikhwalithi ngaphambi kwanoma iyiphi inkokhelo
9.Isikhathi sokukhokha okuxoxiswana ngaso
10.Amakhasimende e-Assit abhekana nezindaba zaseShayina