Rimegepant CAS 1289023-67-1

Khoom Piav Qhia

Cov Khoom Npe: Rimegepant CAS TSIS TAU: 1289023-67-1

0010010 nbsp;

0010010 nbsp;

Txhais:

(5 S, 6 S, {{2}} R) - 5 - nitro - 6 - (2, 3- difluorophenyl) - 6, {{8},, {8, {{2}, - tetrahydro - 5 H-cyclohepta [b] pyridin- {{2}} - yl 4 - (2 - oxo - 2, 3-dihydro-1H-imidazo [4, {{0} } -b] pyridin-1-yl) piperidine-1-carboxylate;

[(5 S, 6 S, {{2}} R) - 5 - amino - 6 - (2, 3 -difluorophenyl) - {6, {{8,}, {8, {{2}, - tetrahydro - 5 H-cyclohepta [b] pyridin - {{2}} - yl] 4 - (2 - oxo-3H-imidazo [4, 5 - b] pyridin-1- yl) piperidine-1-carboxylate;

(5 S, 6 S, {{2}} R) - 5 - amino - 6 - (2, 3- difluorophenyl) - 6, {{8},, {8, {{2}, - tetrahydro - 5 H-cyclohepta [b] pyridin- {{2}} - yl 4 - (2 - oxo - 2, 3-dihydro-1H-imidazo [4, {{0} } -b] pyridin-1-yl) piperidine-1-carboxylate;

BMS-927711;

0010010 nbsp;

0010010 nbsp;

Tshuaj Txhaum 0010010 amp; Lub cev nqaij daim tawv

Zog: Zog

Ntsuas: ≥ 99. 0%

0010010 nbsp;

0010010 nbsp;

Rimegepant yog qhov ncauj calcitonin gene-ntsig txog peptide (CGRP) receptor antagonist siv rau kev kho mob ntawm mob taub hau.

0010010 nbsp;

0010010 nbsp;

Phiajzeb

Ki: 0. {{1}} nM (CGRP receptor) [1] IC 50: 0. 1 4 nM (CGRP receptor) [{{2} }]

0010010 nbsp;

Hauv Vitro 0010010 nbsp; 0010010 nbsp; 0010010 nbsp;

Rimegepant (BMS-9277 1 1) yog qhov muaj txhij txhua, kev sib tw CGRP receptor antagonist nrog IC {{1}} ntawm 0. 14 ± 0. {{5} } nM [1].

Hauv Vivo 0010010 nbsp; 0010010 nbsp; 0010010 nbsp; 0010010 nbsp; 0010010 nbsp;

Rimegepant (BMS-9 2 77 1 1) muaj qhov ncauj zoo ntawm lub cev nyob hauv cov nas thiab cynomolgus liab, kev ntxim nyiam tag nrho cov khoom tsim ua ntej, thiab pom tias muaj koob tshuaj rau kev ua si nyob rau hauv tus qauv ntsuas ntawm CGRP- ntxias lub ntsej muag ntshav txaus [1]. Qhov feem pua ​​ntawm txhais tau tias AUC (0 - 2 4 h) qhov tseem ceeb rau Rimegepant (BMS-9 2 77 1 1) (60, {{ 3}} 00, thiab 300 mg / kg) hauv DBS txhooj, piv nrog ntshav, yog 0.5-0. 6 thoob plaws txhua qhov koob tshuaj nas. Cov txiaj ntsig tau los ntawm kev kawm no qhia txog kev sib raug zoo ntawm Rimegepant ntau ntawm cov ntshav plasma thiab cov ntshav ntshav (DBS) [2].

Tsiaj { 0010010 nbsp; 0010010 nbsp; 0010010 nbsp; 0010010 nbsp; 0010010 nbsp; ; 0010010 nbsp; 0010010 nbsp; 0010010 nbsp;

Cov nas [2] Cov nas tsuag raug kho nrog tsheb tsis muaj tshuaj (tswj) lossis Rimegepant (BMS-9 2 77 1 1) hauv tsheb ntawm 60 , {{{{{{{{{26 {}}}}}, thiab {{{{{{26 {} 5}}}} mg / kg ib hnub twg los ntawm kev hais lus qhov ncauj. Muaj cov 6 nas tsuag hauv txhua pawg kho mob. Rau txhua pawg kho mob, cov ntshav tau sau rau ntawm 1, {{{1 {{{{26 {}} 1}} 0}}}}}, thiab 2 {{2 4}} h los ntawm thawj peb nas, thiab ntawm {{1 0}} thiab {{1 1}} ntawm qhov thib peb nas nyob rau hnub 1 thiab Hnub 1 {{2 4}} ntawm tus Tsov tus tw tom qab noj tshuaj txhua hnub ntawm Rimegepant (BMS-9 2 77 {{ 17}} 1) rau ob lub lim tiam. Lub ntsiab lus hematocrits hauv cov ntshav yog {{1 {{2 5}}}. 2 {1. {{1 {{{{ {26 {} {{26 "}}} 1}} 0}}}}%, 49. {{1 {{{26 {} {} 26}}} 1}} 0}}}} ± {{0 0}}. 2%, {{2 3}}. {{{{26 {}} 4}} ± {{{26 {}} 5} }. {{0 0}}% sib haum rau cov pab pawg tsiaj ntawm 60, {{{{{26 {}}}}}, thiab {{{{{26 {}} 5}}}} mg / kg koob tshuaj, ntsig txog. Rau kev ntsuam xyuas DBS, plaub 1 {{2 5}} samples Cov ntshav kuaj pom rau hauv DBS daim npav ({{2 4}} me ntsis rau ib daim npav), ziab hauv chav kub rau tsawg kawg 2 h, thiab txhua daim npav tau ntim txhua qhov sib txawv hauv ib lub hnab ziplock nrog desiccant ua ntej ua zaub mov xa tuaj. Cov ntshav ntxiv nyob rau hauv txhua lub raj xa dej yog ua tiav rau ntshav hauv 1 h ntawm kev sib sau thiab khaws cia ntawm -70 ° C kom txog thaum kuaj. Plasma cov qauv raug xa mus rau cov dej khov qhuav, thiab daim npav DBS raug xa mus ntawm qhov kub nyab. Rimegepant (BMS-9 2 77 1 1) ntau ntau hauv cov ntshav plasma ntsuas. Rimegepant hauv nas DBS tau tshawb xyuas siv qhov txheej txheem DBS. Lub limtiam toxicokinetic (TK) yog suav los ntawm cov ntshav siab thiab cov ntaub ntawv sijhawm siv cov qauv tsis siv hauv kev siv Kinetica.

Cov ntawv qhia; 0010010 nbsp; 0010010 nbsp; 0010010 nbsp; 0010010 nbsp; 0010010 nbsp;

[1]. Luo G, li al. Tshawb nrhiav ntawm (5 S, {{2}} S, 9 R) - 5 - amino - {{2}} - ({{ 6}}, 3-difluorophenyl) - {{2}}, 7, 8, 9 - tetrahydro - 5 H-cyclohepta [b] pyridin - 9 - yl 4 - (2 - oxo - 2, 3-dihydro - 1 H-imidazo [4, { {1}} - b] pyridin - 1 - yl) piperidine - 1 - carboxylate (BMS - 9 2 7 {{9)} { {0}} 1): ib qhov ncauj ntsig txog calcitonin cov noob-hais txog peptide (CGRP) antagonist hauv kev sim tshuaj rau kev kho mob taub hau. J Med Chem. 2 0 1 2 Dec 1 3; 5 5 (2 3): 1 0 { {{{6 "}}} 4 4 - 5 1.

0010010 nbsp; [2]. Zheng N, li al. Txhim kho cov kua ua kua-kua muaj qhov zoo sib xws nrog cov ntim sib xyaw ua kom zoo dua qub kev hloov ua haujlwm thiab nws cov ntawv thov kom muaj nuj nqis BMS-9 2 7711 hauv cov nas ntshav kom qhuav los ntawm UHPLC-MS / MS. J Pharm Biomed Anal. 2 014 Lub Ob Hlis; 89: 2 40-50.

0010010 nbsp;

0010010 nbsp;

Yog tias koj txaus siab rau peb cov khoom lossis muaj lus nug, thov koj xav tiv tauj peb!

0010010 nbsp;

0010010 nbsp;

Cov khoom hauv qab patent yog muab rau R 0010010 amp; D lub hom phiaj nkaus xwb. Txawm li cas los xij, lub luag haujlwm kawg tau txiav txim siab nrog cov neeg yuav khoom.

Cim npe nrov: rimegepant cas 1289023-67-1, tuam ntxhab, lwm tus neeg, Hoobkas, yuav, hauv Tshuag

• Tug: 5 H-Cyclohepta [b] pyridine-7,8-dihydro - 5, 9 ({{6)} H) -dione CAS 3 9 713-40 -1
• Tom ntej: 4- (chloromethyl) -1-cyclohexyl-2- (trifluoromethyl) Benzene CAS 957205-24-2