I-Linagliptin Linagliptin, eyakhiwe ngu-Boehringer Ingelheim, yagunyazwa yi-FDA ngoMeyi 2, 2011. Isetshenziselwa ukuhlanganisa ukudla nokuzivocavoca ukuze kuthuthukiswe ukulawulwa kwamazinga kashukela egazini kubantu abanesifo sikashukela sohlobo 2.I-Linagliptin ithuthukisa ukulawulwa kweglucose yegazi ezigulini ngokuvimbela i-dipeptidyl peptidase-4 (DPP-4).
I-Incretin (i-Incretin) inomphumela wokugqugquzela ukukhiqizwa kwe-insulin ngamaseli e-pancreas islet B, ikakhulukazi okuhlanganisa i-insulinotropic polypeptide (GIP) encike ku-glucose kanye ne-glucagon-like polypeptide-1 (GLP-1).I-DDP-4 i-serine protease etholakala phezu kwamaseli.Ibophezela kumaprotheni futhi ikhona kakhulu ku-plasma kanye nezicubu ezihlukahlukene emzimbeni (njengezinso, isibindi, i-intestinal villi encane, amangqamuzana e-endothelial, njll.).I-Linagliptin iyi-inhibitor ekhethiwe ye-DPP-4 evimbela umsebenzi we-enzyme ngokubopha ngokubuyela emuva ku-DPP-4, ibambezele ukuwohloka kwe-GLP-1, ithuthukise umsebenzi we-GLP-1, futhi ivuselele ngendlela encike ku-glucose ngendlela encike ku-insulin futhi yehlisa izinga le-glucagon ekuhambeni, ngaleyo ndlela ilawule izinga likashukela wegazi ezigulini ezinesifo sikashukela sohlobo 2.
Uma kuqhathaniswa namanye ama-DPP-4 inhibitors, izinzuzo eziyinhloko ze-Linagliptin yilezi: inokuphepha okuhle kakhulu kwezinso futhi inganciphisa ngempumelelo i-glycosylated hemoglobin.I-Linagliptin ikhishwa ikakhulukazi endle ngendlela ye-prototype.Ngemuva kokuphathwa ngomlomo, ukuphuma kwezinso kungu-5% kuphela yenani elilawulwayo.Ngisho noma ifakwa emthanjeni, i-30.8% kuphela ekhishwa ngezinso.Ngakho-ke, asikho isidingo seziguli ezithola ukwelashwa.Njalo hlola ukusebenza kwesibindi nezinso kanye nokulungiswa komthamo.Zonke iziguli zingakwazi ukulungisa umthamo ngendlela efanayo ukuze zibhalwe kalula.
Imiphumela emibi evamile ye-Linagliptin ukutheleleka kokuphefumula, ukuminyana kwamakhala, ubuhlungu bemisipha, ikhanda elibuhlungu kanye nomphimbo obuhlungu.
Izinga eliphezulu:izinga lebhizinisi
Isivivinyo:98-102%
Ingaphandle:Impushana ecwebezelayo emhlophe ukuya kokuphuzi
Iphakheji:25kg/isigubhu
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TECHNOL OGY UBUHLE
●I-High Pressure Catalytic Hydrogenation.I-High Pressure Hydrogenolysis Reaction .Ukusabela kwe-Cryogenic (<-78%C)
● I-Aromatic Heterocyclic Synthesis
●Ukusabela Kabusha
●Chiral Resolution
●Heck, Suzuki,Negishi,Sonogashira .Ukusabela kukaGiignard
Izisetshenziswa
Ilebhu yethu inezinsiza ezihlukahlukene zokuhlola nokuhlola, njenge: NMR (Bruker 400M), HPLC、chiral-HPLC、LC-MS、LC-MS/MS (API 4000),IR,UV,GC,GC,GC-MS, Chromatography, I-Microwave Synthesizer, i-Parallel Synthesizer, i-Differential Scanning Calorimeter (DSC), i-Electron Microscope...
Ithimba le-R&D
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Sisize izinkampani ezimbalwa eziphezulu zasekhaya ezithaka imithi, njengeI-Hansoh, i-Hengrui ne-HEC Pharm.Lapha sizokhombisa ingxenye yazo.
Ikesi Lokwenza Ngokwezifiso:
Inombolo yeCas: 110351-94-5
Ikesi Lokwenza Ngokwezifiso:
Inombolo yeCas: 144848-24-8
Ikesi Lesithathu Lokwenza Ngokwezifiso:
Inombolo yeCas: 200636-54-0
1.Enza ngendlela oyifisayo i-New Intermediates noma ama-API.Ngokufanayo nokwabelana kwecala elingenhla, amakhasimende anezidingo ze-Intermediates ethile noma ama-API, futhi awakwazi ukuthola imikhiqizo edingekayo emakethe, lapho-ke singasiza Ukwenza Ngokwezifiso.
2.Ukuthuthukisa Inqubo Yemikhiqizo Emidala.Ithimba lethu lizosiza Ukuthuthukisa futhi lithuthukise ukukhiqiza okunjalo okuyindlela yokusabela endala, izindleko zokukhiqiza ziphezulu, nokusebenza kahle kuphansi.Singahlinzeka ngemibhalo egcwele yokudluliswa kobuchwepheshe kanye nokuthuthukiswa kwenqubo, sisize ikhasimende ngokukhiqiza okuphumelelayo.
Ukusuka kokuhlosiwe kwezidakamizwa kuye kuma-IND, i-JIN DUN Medical ikunikezaizixazululo zomuntu siqu ze-R&D zokuma okukodwa.
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