iphepha_ibhena

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

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

Inkcazelo emfutshane:

Imbonakalo Iikristale eziMhlophe ukuya kwi-Off-White okanye umgubo wekristale.
MF I-C16H22N2O6
MW 338.36
Ubunyulu 98+


Iinkcukacha zeMveliso

Imeko yezothutho&ecetyiswayo indlela yokuthumela ngenqanawa:
ngomoya, ngolwandle okanye nge-express

Imeko yokugcina:
Itywinwe kwindawo eyomileyo, yoBubushushu beGumbi

Ubuncinci boMyinge woMyalelo:
Uthethathethwano

Isiqinisekiso:
COA, HPLC, GC, HNMR, Assay, Water Content(KF), TLC iyafumaneka

I-D-Ls(tfa)-NCA (2)

Izithethantonye

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

Ukupakishwa kwangaphakathi

Ngokuqhelekileyo zisetyenziselwa ukupakisha umgubo.Yaye anokuthintela ukukhanya kwelanga namanzi ukuba angabi mabi.

Ukupakisha kwangaphakathi 2
Ukupakisha kwangaphakathi 1
Ukupakisha kwangaphakathi 3

ukupakisha kwangaphandle

Ibhokisi elukhuni inokukhusela iimveliso zakho ekuqhekekeni kwaye zibe manzi.

Ukupakisha kwangaphandle 3
Ukupakisha kwangaphandle 2
Ukupakisha kwangaphandle 1

Usetyenziso

Nidanib, yikhemikhali.Igama lekhemikhali 1 h - indole - 6 - carboxylic acid, 2, 3 - dihydro - 3 - [[[4 - (methyl [(4 - methyl - 1 - piperazine) acetyl] amino] phenyl] amino] benzene heartland ye methyl] - 2 - i-oksijini -, i-methyl ester, (z) - Ngokonyango, le mveliso isetyenziselwa ukunyanga i-idiopathic pulmonary fibrosis (IPF).
U-Nidanib uye wafunda izigulane ze-1,529 ezine-idiopathic pulmonary fibrosis (IPF) kwizilingo ezininzi zekliniki.Idatha yokhuseleko enikezelweyo isekelwe ekuthelekisweni kwezigulane ze-1061 ezinikwe i-nidanib i-150 mg kabini imihla ngemihla kunye ne-placebo kwiiveki ezimbini ze-52-isigaba se-3, i-randomized, i-double blind, izifundo ezilawulwa yi-placebo (INPULSIS-1 kunye ne-INPULSIS-2).Iziganeko ezimbi kakhulu ezixhaphakileyo ezinxulumene nokusetyenziswa kwe-nidanib zibandakanya urhudo, isicaphucaphu kunye nokuhlanza, intlungu yesisu, ukulahlekelwa ngumdla, ukulahleka kwesisindo, kunye ne-enzymes yesibindi ephakamileyo.Nceda ubhekisele ku- [IiNgcaciso] zolawulo lweziphumo ezibi ezihambelanayo.UHlelo lweZiko eliCwangcisiweyo (i-SOC) le-MedDRA libonelela ngesishwankathelo seempendulo ezingalunganga kunye nokuhlelwa rhoqo.
I-Nidanib yinxalenye ye-P-gp (jonga i-Pharmacokinetics).Kwisifundo esithile sokusebenzisana kweziyobisi, ukulawulwa okudibeneyo kwe-ketoconazole, i-P-gp inhibitor enamandla, ukunyuka kwe-exposure ye-nidanib kumaxesha e-1.61 kwindawo ephantsi kwe-curve (AUC) kunye namaxesha e-1.83 nge-peak concentration (Cmax).
Kuphononongo lokusebenzisana neziyobisi kunye ne-P-gp inducer rifampicin enamandla, ukutyhileka kwi-nidanib kwehle ukuya kutsho kwi-50.3%, njengoko kulinganiswe ngendawo ephantsi kwegophe (AUC), xa idityaniswe ne-rifampicin xa ithelekiswa ne-Nidanib yodwa.Ngokugxininiswa kwencopho (Cmax), yehla ukuya kwi-60.3%.
Xa ilawulwa ngokudibeneyo nale mveliso, i-P-gp inhibitors enamandla (umzekelo, i-ketoconazole okanye i-erythromycin) inokunyusa ukutyhila kwi-nidanib.Kwezi meko, ukunyamezelana kwesigulane kwi-nidanib kufuneka kubekwe iliso elibukhali.Ukulawulwa kweempembelelo ezimbi kunokufuna ukuyeka, ukunciphisa idosi, okanye ukuyeka unyango ngale mveliso (jonga [Ukusetyenziswa kunye nedosi]).
I-P-gp inducers ezinamandla (umzekelo, i-rifampicin, i-carbamazepine, i-phenytoin kunye ne-St. John's wort) inokunciphisa ukuchanabeka kwi-nidanib.Iindibaniso ezizezinye ezingenayo okanye ezincinci zokungeniswa kwe-P-gp kufuneka ziqwalaselwe.

iimveliso ezinxulumene

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

Ukongama

1. Inkonzo yeR&D iyafumaneka
2. Umvelisi oqinisekisiweyo we-ISO, isiqinisekiso somgangatho
I-3.Ikhosi epheleleyo yenkonzo yokulandelela ngexesha lemveliso
4.Ixabiso eliphezulu elisebenzayo
5.Amaxwebhu esiqinisekiso somgangatho anikwe ngokwesicelo somthengi
I-6.Inkonzo enkulu emva kokuthengisa, ukugcina ubudlelwane obusondeleyo kunye nomthengi
I-7.Isixhobo esipheleleyo sokunceda ukunciphisa iindleko zokuthumela ngenqanawa
I-8.Isampuli yamahhala enikezelwa ukujonga umgangatho ngaphambi kwayo nayiphi na intlawulo
9.Ixesha lentlawulo ekuxoxwe ngalo
Abathengi be-10.Assit bajongana nemicimbi yaseTshayina


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