Baloxavir Marboxil CAS 1985606-14-1 API Tayada Sare
Shanghai Ruifu Chemical Co., Ltd. waa saaraha ugu horreeya ee Baloxavir Marboxil (CAS: 1985606-14-1) oo leh tayo sare leh.Kiimikada Ruifu waxay bixin kartaa gaarsiinta adduunka oo dhan, qiimo tartan ah, adeeg aad u wanaagsan, tiro yar iyo tiro badan oo la heli karo.Iibso Baloxavir Marboxil,Please contact: alvin@ruifuchem.com
Magaca Kiimikada | Baloxavir Marboxil |
La mid ah | BXM;S-033188 |
Lambarka CAS | 1985606-14-1 |
Heerka Saamiyada | Kaydka, Miisaanka Wax-soo-saarka Ilaa boqollaal Kiilogaram |
Qaanuunka molecular | C27H23F2N3O7S |
Miisaanka Molecular | 571.55 |
Cufnaanta | 1.57±0.10 g/cm3 |
Solubility | Ku milmay DMSO |
Kaydinta Muddada Dheer | Ku kaydi wakhtiga dheer at -20 ℃ |
COA & MSDS | La heli karo |
Asal ahaan | Shanghai, Shiinaha |
Summada | Kiimikada Ruifu |
Shayga | Tilmaamaha |
Muuqashada | Caddaan ilaa budo cad-cad |
Aqoonsiga | IR Spectrum waxay u dhigantaa heerka tixraaca Waqtiga haynta waxay u dhigantaa heerka tixraaca |
Waxyaalaha biyaha (waxaa qoray KF) | ≤1.0% |
Khasaare xagga qalajinta | ≤1.0% |
Hadhaaga dabka | ≤0.50% |
Biraha culus | ≤20pm |
Walxaha laxidhiidha | |
Xumaanta Shakhsiyeed ee ugu badan | ≤0.50% |
Wadarta wasakhda | ≤1.0% |
Cabbirka Qaybaha | D90 Gudub 150um |
Daahirnimada Chiral | ≥99.0% |
daahirnimo | ≥99.0% |
Qiimayn | 98.0% ~ 102.0% |
Xalalka Haraaga ah | U hogaansan Shuruudaha ICH |
Raridda | Rarista Xidhmada Barafka |
Heerka Imtixaanka | Heerka Ganacsiga |
Isticmaalka | API, ee daawaynta Hargabka A iyo Hargabka B |
Xidhmada:Dhalo, bacda bireed ee aluminium, 25kg/Drum kartoonada, ama sida waafaqsan shuruudaha macmiilka.
Xaaladda Kaydinta:Weelka si adag u xidh oo ku kaydi qabow, qalalan (2 ~ 8 ℃) iyo bakhaar hawo wanaagsan leh oo ka fog walxaha aan ku habboonayn.Ka ilaali iftiinka iyo qoyaanka.
Rarida:Ku gaarsii adduunka oo dhan hawo, by FedEx/DHL Express.Bixi keenid degdeg ah oo la isku halayn karo.
Baloxavir Marboxil (CAS: 1985606-14-1, BXM, S-033188, Xofluza) waa dawada ka hortagga fayraska oo ay samaysay Shionogi Co., shirkad dawooyin ah oo Jabbaan ah iyo Roche oo loogu talagalay daawaynta hargabka A iyo caabuqyada hargabka B.Daawada ayaa markii hore loo oggolaaday in lagu isticmaalo Japan bishii Febraayo 2018 waxaana oggolaatay FDA Oktoobar 24, 2018 daaweynta hargabka ba'an ee ba'an ee bukaannada 12 sano jir iyo ka weyn kuwaas oo calaamadeeyay wax aan ka badnayn saacadaha 48.Baloxavir marboxil, oo ah cap-endonuclease inhibitor, ayaa leh hannaan ficil oo gaar ah marka la barbar dhigo fasalka daawada neuraminidase inhibitor ee hadda jira ee loo isticmaalo in lagu daweeyo caabuqyada hargabka.Baloxavir Marboxil waa dawo cusub oo ka hortagga hargabka oo leh hab cusub oo ficil ah.Baloxavir Marboxil waa dawada Baloxavir Acid (S-033447) taas oo si xoog leh oo xushmad leh u joojisa endonuclease-ka koofiyadda ku tiirsan ee ku jira qaybta polymerase PA ee hargabka A iyo B, taasoo horseedaysa joojinta qoraalka RNA iyo ku celcelinta.Baloxavir ayaa sidoo kale lagu baaray suurtagalnimada in lagu daweeyo COVID-19 laakiin faa'iido la xaqiijiyay lama arag.
Baloxavir Marboxil waa wakiilka daweynta hargabka, gaar ahaan, xannibaadaha enzyme ee bartilmaameedsanaya fayraska hargabka 'cap-dependent endonuclease act, mid ka mid ah hawlaha fayraska polymerase complex.Gaar ahaan, waxa ay joojisaa habka loo yaqaano dafida daboolka, kaas oo fayrasku uu ka soo saaro qormooyin gaagaaban oo daboolan oo ka yimid qoraalada unugyada RNA ee martida loo yahay, kaas oo uu markaa u isticmaalo polymerase-catalyzed synthesis ee mRNA-yada fayraska loo baahan yahay.Qayb ka mid ah polymerase waxay ku xidhan tahay martida loo yahay pre-mRNA-yada 5' koofiyaddooda, ka dib waxqabadka polymerase's endonuclease wuxuu kiciyaa kala-goynta "ka dib 10-13 nucleotides".Sidan oo kale, qaabkeedu wuu ka duwan yahay neuraminidase inhibitors sida Oseltamivir iyo Zanamivir.
Baloxavir Marboxil waa xakameyn la xushay hargabka cap-ku-tiirsan endonuclease kaas oo ka hortagaya shaqada polymerase sidaas darteed fayraska hargabka mRNA ku celcelinta 5, 3. Waxay muujisay waxqabad daweyn oo ka dhan ah hargabka A iyo B, oo ay ku jiraan noocyada u adkeysanaya wakiilada fayraska ee hadda jira 1. Daawadan Waxay joojisaa enzyme-ka looga baahan yahay taranka fayraska, sidaas awgeed si degdeg ah ayey u daawaysaa infekshanka fayraska ifilada 5, Calaamadee oo yaraynaysa calaamadaha caabuqa.Hal qiyaas oo ka mid ah wakiilkan ayaa la muujiyay inuu ka sarreeyo placebo si loo yareeyo calaamadaha hargabka iyo ka sarreeya labadaba oseltamivir iyo placebo ee natiijooyinka fayraska (oo lagu calaamadeeyay hoos u dhaca culeyska fayraska).
Baroxavir waxay ku habboon tahay bukaanada ≥ 12 sano jir ah oo qaba hargab daran oo aan dhib lahayn oo astaamihiisa aan ka badnayn 48 saacadood.Waa in fiiro gaar ah loo yeesho xaddidaadaha daawadu: Fayraska hargabku wuu isbedelaa waqti ka dib, waxaana jira arrimo ay ka mid yihiin nooca fayraska iyo nooca hoose.Marka iska caabbinta daroogada ee fayraska iyo cudur-sidaha fayrasku isbeddelaan, waxtarka bukaan-socodka ee dawooyinka fayraska ayaa la wiiqi kara.Marka la go'aaminayo in la qaato basalovir dipivoxil, macluumaadka la heli karo ee dareenka fayraska faafa ee deegaanka ee daawada waa in la tixgeliyaa.
Baloxavir Marboxil waa dawada hargabka, fayruska ka-hortagga, oo laga qaato hal kiniin ah, afka, shakhsiyaadka da'doodu tahay 12 sano ama ka weyn, oo soo bandhigay calaamadaha caabuqan wax ka badan 48 saacadood. baloxavir marboxil la maamulo 48 saacadood ka dib lama tijaabin.
Baloxavir Marboxil waa in aan lala wadaagin waxyaabaha caanaha laga sameeyo, cabitaannada kaalshiyamku xoojiyaan, ama caloosha jilcisa, antacids, ama supplements afka ah oo ay ku jiraan calcium, iron, magnesium, selenium, aluminium ama zinc.
Dhibaatooyinka soo raaca ee caadiga ah ka dib marka la qaato hal dose ee baloxavir marboxil waxaa ka mid ah shuban, boronkiito, hargab caadi ah, madax-xanuun, iyo lallabbo.Dhacdooyinka xunxun ayaa lagu soo warramey 21% dadka qaatay baloxavir, 25% kuwa hela placebo, iyo 25% Oseltamivir.
Patent Japanese JP6212678 ayaa sheegay habka isku dhafka ah ee Baloxavir Marboxil.3, 4-difluorobenzoic acid ayaa loo isticmaalay walxo ceeriin ah si ay ula falgasho DMF iyada oo la raacayo ficilka LDA si loo helo 2-formyl-3, 4-difluorobenzoic acid.Dabadeed waxay samaysaa thioacetal oo leh thiophenol, ka dibna waa la yareeyaa oo la kala saaraa borane si loo helo 2-phenylthiomethyl -3, 4-difluorob, 8-difluorodibenzo [B, e] thiazepine -11 (6H) -hal, iyo ugu dambeyntii furaha jajabka thiazepine 7, 8-difluoro-6,11-dihydrodibenzo [B, e] thiazepine -11-khamriga waxaa lagu helaa hoos u dhigista sodium borohydride.Isticmaalka 3- (benzyloxy) -4-oxo-4H-pyran-2-carboxylic acid si ay ula falgasho qaabka tert-butyl ka dib markii la nadiifiyo si loo helo 3- (benzyloxy) -1- ((tert-butoxycarbonyl) amino) -4-oxo -1, 4-dihydropyridine-2-methyl formate hydrate, ka dibna leh 2- (2, 2-dimethoxyethoxy) ethylamine waxay martaa falcelinta isdhaafsiga urethane, ka dibna baaskiil ku hoos jira ficilka methanesulfonic acid si loo helo 7- (benzyloxy) -3, 4,12,12a-tetrahydro-1H-[1,4] oxazino [3,4-c] pyridino [2,1-f] [1,2,4] triazine -6, 8-dione hemihydrate, ka dibna waa isku dhafan (R) -tetrahydrofuran -2-formic acid, ka dibna crystallized oo la xalliyo, ka dibna kooxda caawiyayaasha chiral waa la saaraa si loo helo molecule muhiimka ah ee waalidka chiral (R) -7- (benzyloxy) -3,4,12, 12a-tetrahydro-1H-[1,4] oxazino [3,4-c] pyrido [2,1-f] [1,4] Triazine-6, 8-dione.Kadib molecule-ga muhiimka ah ee waalidka ayaa loo isticmaalaa in lagu beddelo n-hexanol iyada oo la raacayo ficilka Grignard reagent, ka dibna iyada oo la raacayo jajabka thiazepine ee muhiimka ah 7,8-difluoro-6, 11-dihydrodibenzo [B, e] thiazepine -11-khamriga. , iyo ugu dambeyntii debutylation iyo uumi leh methyl chloroformate si aad u hesho badeecada kama dambaysta ah Baloxavir Marboxil.