INCWADANA YEENDABA
Ngemibuzo malunga neemveliso zethu okanye uluhlu lwamaxabiso, nceda ushiye i-imeyile yakho kuthi kwaye siya kuqhagamshelana phakathi kweeyure ezingama-24.
BUZA NGOKUImeko 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
(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
Ngokuqhelekileyo zisetyenziselwa ukupakisha umgubo.Yaye anokuthintela ukukhanya kwelanga namanzi ukuba angabi mabi.
Ibhokisi elukhuni inokukhusela iimveliso zakho ekuqhekekeni kwaye zibe manzi.
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 zeklinikhi.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 kudityaniswa ne-rifampicin xa kuthelekiswa 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.
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 |
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