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2017年1月6日星期五

EOS Med Chem produce BLU9931, 1538604-68-0 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Name: BLU9931
CAS#: 1538604-68-0
Chemical Formula: C26H22Cl2N4O3
Exact Mass: 508.1069
Molecular Weight: 509.38
Elemental Analysis: C, 61.31; H, 4.35; Cl, 13.92; N, 11.00; O, 9.42

EOS Med Chem produce BLU9931, 1538604-68-0 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
BLU9931, 1538604-68-0 Intermediates, EOS Med Chem have 8; BLU9931, 1538604-68-0 Impurity we have 10, all from GMP, FDA plant.
Now BLU9931, 1538604-68-0 DMF document is preparing.
Until 2016, Aug, BLU9931, 1538604-68-0 more than produced 25kg API, 120kg Intermediates

BLU-9931 Intermediates 6-(2,6-dichloro-3,5-dimethoxyphenyl)-N-(2-methyl-6-nitrophenyl)quinazolin-2-amine 1538605-09-2


GMP PRODUCE:

Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib 

2016 Mumbai CPHI, Hope to meet!
2016 Barcelona CPHI, Hope to meet!
2016 Korea(한국) CPHI, C40, Welcome!
2016 Shanghai CPHI, W5C47, Welcome!
EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
網址: www.eosmedchem.com 
郵箱: gutian@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp: +8618653174435
Skype: willgutian




Description: BLU9931 is a potent and irreversible small-molecule inhibitor of FGFR4, as a targeted therapy to treat patients with HCC whose tumors have an activated FGFR4 signaling pathway. BLU9931 is exquisitely selective for FGFR4 versus other FGFR family members and all other kinases. BLU9931 shows remarkable antitumor activity in mice bearing an HCC tumor xenograft that overexpresses FGF19 due to amplification as well as a liver tumor xenograft that overexpresses FGF19 mRNA but lacks FGF19 amplification. Approximately one third of patients with HCC whose tumors express FGF19 together with FGFR4 and its coreceptor klotho β (KLB) could potentially respond to treatment with an FGFR4 inhibitor.
Synonym: BLU9931; BLU-9931; BLU 9931.
IUPAC/Chemical Name: N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)-3-methylphenyl)acrylamide
SMILES Code: C=CC(NC1=CC=CC(C)=C1NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)=O

1: Packer LM, Pollock PM. Paralog-Specific Kinase Inhibition of FGFR4: Adding to the Arsenal of Anti-FGFR Agents. Cancer Discov. 2015 Apr;5(4):355-7. doi: 10.1158/2159-8290.CD-15-0246. PubMed PMID: 25847957.
2: Hagel M, Miduturu C, Sheets M, Rubin N, Weng W, Stransky N, Bifulco N, Kim JL, Hodous B, Brooijmans N, Shutes A, Winter C, Lengauer C, Kohl NE, Guzi T. First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway. Cancer Discov. 2015 Apr;5(4):424-37. doi: 10.1158/2159-8290.CD-14-1029. Epub 2015 Mar 16. PubMed PMID: 25776529.
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EOS Med Chem produce BLU554,1707289-21-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

 
EOS Med Chem produce BLU554,1707289-21-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
BLU554,1707289-21-1 Intermediates, EOS Med Chem have 8; BLU554,1707289-21-1 Impurity we have 10, all from GMP, FDA plant.
Now BLU554,1707289-21-1 DMF document is preparing.
Until 2016, Aug, BLU554,1707289-21-1 more than produced 25kg API, 120kg Intermediates

BLU-554 BLU-554 1707289-21-1
BLU-554 Intermediates (2-amino-5-bromophenyl)methanol 20712-12-3
BLU-554 Intermediates 2-amino-5-bromobenzaldehyde 29124-57-0
BLU-554 Intermediates 6-bromoquinazolin-2(1H)-one 79885-37-3
BLU-554 Intermediates 6-bromo-2-chloroquinazoline 882672-05-1
BLU-554 Intermediates 2-chloro-6-(3,5-dimethoxyphenyl)quinazoline 1538605-05-8
BLU-554 Intermediates 2-chloro-6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazoline 1538605-06-9
BLU-554 Intermediates N-((3S,4S)-4-azidotetrahydro-2H-pyran-3-yl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-amine
BLU-554 Intermediates (3S,4S)-N3-(6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)tetrahydro-2H-pyran-3,4-diamine

 

GMP PRODUCE:

Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib 

2016 Mumbai CPHI, Hope to meet!
2016 Barcelona CPHI, Hope to meet!
2016 Korea(한국) CPHI, C40, Welcome!
2016 Shanghai CPHI, W5C47, Welcome!
EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
網址: www.eosmedchem.com 
郵箱: gutian@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp: +8618653174435
Skype: willgutian
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EOS Med Chem produce AZD-4547,1035270-39-3 (1394854-62-6) in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Name: AZD-4547
CAS#: 1035270-39-3 (1394854-62-6)
Chemical Formula: C26H33N5O3
Exact Mass: 463.25834
Molecular Weight: 463.57192
Elemental Analysis: C, 67.36; H, 7.18; N, 15.11; O, 10.35

EOS Med Chem produce AZD-4547,1035270-39-3 (1394854-62-6) in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

AZD-4547,1035270-39-3 (1394854-62-6) Intermediates, EOS Med Chem have 8; AZD-4547,1035270-39-3 (1394854-62-6) Impurity we have 10, all from GMP, FDA plant.
Now AZD-4547,1035270-39-3 (1394854-62-6) DMF document is preparing.
Until 2016, Aug, AZD-4547,1035270-39-3 (1394854-62-6) more than produced 25kg API, 120kg Intermediates

AZD4547 AZD4547 1035270-39-3
AZD4547 Intermediates Ethyl 4-((3S,5R)-3,5-dimethylpiperazin-1-yl)benzoate 234082-05-4
AZD4547 Intermediates (E)-ethyl 3-(3,5-dimethoxyphenyl)acrylate 42174-79-8
AZD4547 Intermediates 3-(3,5-dimethoxyphenyl)propanoic acid 717-94-2
AZD4547 Intermediates Ethyl 3-(3,5-dimethoxyphenyl)propanoate 54901-09-6
AZD4547 Intermediates 5-(3,5-dimethoxyphenyl)-3-oxopentanenitrile 1000895-54-4
AZD4547 Intermediates 5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-amine 1000895-53-3

GMP PRODUCE:

Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib 

2016 Mumbai CPHI, Hope to meet!
2016 Barcelona CPHI, Hope to meet!
2016 Korea(한국) CPHI, C40, Welcome!
2016 Shanghai CPHI, W5C47, Welcome!
EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
網址: www.eosmedchem.com 
郵箱: gutian@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp: +8618653174435
Skype: willgutian


Description: AZD4547 is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor AZD4547 binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways, and, so, the inhibition of tumor cell proliferation and tumor cell death. FGFR, up-regulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cellular proliferation, differentiation and survival.
Synonym: AZD4547; AZD-4547; AZD 4547.
IUPAC/Chemical Name: N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3S,5R)-3,5-dimethylpiperazin-1-yl)benzamide
SMILES Code: O=C(NC1=NNC(CCC2=CC(OC)=CC(OC)=C2)=C1)C3=CC=C(N4C[C@H](C)N[C@H](C)C4)C=C3


Related CAS#
Sci-Finder listed CAS#1394854-62-6 for AZD-4547
ChemIDplus listed CAS#1035270-39-3 for AZD-4547, see website: https://chem.nlm.nih.gov/chemidplus/rn/1035270-39-3
  
According to Sci-Finder,
Chemical name for CAS#1394854-62-6:
N-[3-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl]-4-(3,5-dimethyl-1-piperazinyl)benzamide
Chemical name for CAS#1035270-39-3:
rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benzamide

1: Ramsey MR, Wilson C, Ory B, Rothenberg SM, Faquin W, Mills AA, Ellisen LW. FGFR2 signaling underlies p63 oncogenic function in squamous cell carcinoma. J Clin Invest. 2013 Aug 1;123(8):3525-38. doi: 10.1172/JCI68899. Epub 2013 Jul 8. PubMed PMID: 23867503; PubMed Central PMCID: PMC3726171.
2: Fox EM, Kuba MG, Miller TW, Davies BR, Arteaga CL. Autocrine IGF-I/insulin receptor axis compensates for inhibition of AKT in ER-positive breast cancer cells with resistance to estrogen deprivation. Breast Cancer Res. 2013 Jul 11;15(4):R55. [Epub ahead of print] PubMed PMID: 23844554.
3: Katoh M, Nakagama H. FGF Receptors: Cancer Biology and Therapeutics. Med Res Rev. 2013 May 21. doi: 10.1002/med.21288. [Epub ahead of print] PubMed PMID: 23696246.
4: Ware KE, Hinz TK, Kleczko E, Singleton KR, Marek LA, Helfrich BA, Cummings CT, Graham DK, Astling D, Tan AC, Heasley LE. A mechanism of resistance to gefitinib mediated by cellular reprogramming and the acquisition of an FGF2-FGFR1 autocrine growth loop. Oncogenesis. 2013 Mar 25;2:e39. doi: 10.1038/oncsis.2013.4. PubMed PMID: 23552882; PubMed Central PMCID: PMC3641357.
5: Xie L, Su X, Zhang L, Yin X, Tang L, Zhang X, Xu Y, Gao Z, Liu K, Zhou M, Gao B, Shen D, Zhang L, Ji J, Gavine PR, Zhang J, Kilgour E, Zhang X, Ji Q. FGFR2 gene amplification in gastric cancer predicts sensitivity to the selective FGFR inhibitor AZD4547. Clin Cancer Res. 2013 May 1;19(9):2572-83. doi: 10.1158/1078-0432.CCR-12-3898. Epub 2013 Mar 14. PubMed PMID: 23493349.
6: Zhao R, Xie X, Shen GX. Effects of glycated low-density lipoprotein on cell viability, proliferation, and growth factors of mouse embryo fibroblasts. Can J Physiol Pharmacol. 2013 Jan;91(1):64-70. doi: 10.1139/cjpp-2012-0234. Epub 2013 Jan 21. PubMed PMID: 23369077.
7: Zhang J, Zhang L, Su X, Li M, Xie L, Malchers F, Fan S, Yin X, Xu Y, Liu K, Dong Z, Zhu G, Qian Z, Tang L, Schöttle J, Zhan P, Ji Q, Kilgour E, Smith PD, Brooks AN, Thomas RK, Gavine PR. Translating the therapeutic potential of AZD4547 in FGFR1-amplified non-small cell lung cancer through the use of patient-derived tumor xenograft models. Clin Cancer Res. 2012 Dec 15;18(24):6658-67. doi: 10.1158/1078-0432.CCR-12-2694. Epub 2012 Oct 18. Erratum in: Clin Cancer Res. 2013 Jul 1;19(13):3714. Schöttle, Jakob [added]. PubMed PMID: 23082000.
8: Chell V, Balmanno K, Little AS, Wilson M, Andrews S, Blockley L, Hampson M, Gavine PR, Cook SJ. Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance. Oncogene. 2013 Jun 20;32(25):3059-70. doi: 10.1038/onc.2012.319. Epub 2012 Aug 6. PubMed PMID: 22869148.
9: Singh D, Chan JM, Zoppoli P, Niola F, Sullivan R, Castano A, Liu EM, Reichel J, Porrati P, Pellegatta S, Qiu K, Gao Z, Ceccarelli M, Riccardi R, Brat DJ, Guha A, Aldape K, Golfinos JG, Zagzag D, Mikkelsen T, Finocchiaro G, Lasorella A, Rabadan R, Iavarone A. Transforming fusions of FGFR and TACC genes in human glioblastoma. Science. 2012 Sep 7;337(6099):1231-5. doi: 10.1126/science.1220834. Epub 2012 Jul 26. PubMed PMID: 22837387; PubMed Central PMCID: PMC3677224.
10: Gavine PR, Mooney L, Kilgour E, Thomas AP, Al-Kadhimi K, Beck S, Rooney C, Coleman T, Baker D, Mellor MJ, Brooks AN, Klinowska T. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56. doi: 10.1158/0008-5472.CAN-11-3034. Epub 2012 Feb 27. PubMed 

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We produce Rociletinib, AVL-301, CO1686, 1374640-70-6 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok

​Name: Rociletinib
CAS#: 1374640-70-6
Chemical Formula: C27H28F3N7O3
Exact Mass: 555.22057
Molecular Weight: 555.55
Elemental Analysis: C, 58.37; H, 5.08; F, 10.26; N, 17.65; O, 8.64

We produce Rociletinib, AVL-301, CO1686, 1374640-70-6 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Rociletinib, AVL-301, CO1686, 1374640-70-6 Intermediates, we have 8; Rociletinib, AVL-301, CO1686, 1374640-70-6 Impurity we have 10, all from GMP, FDA plant.
Now Rociletinib, AVL-301, CO1686, 1374640-70-6 DMF document is preparing.
Until 2016, Aug, Rociletinib, AVL-301, CO1686, 1374640-70-6 more than produced 25kg API, 120kg Intermediates

Rociletinib AVL-301; CO-1686 1374640-70-6(free base)
Rociletinib AVL-301; CO-1686 1446700-26-0(Hydrobromide)
Rociletinib Intermediates Tert-butyl (3-((2-chloro-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)carbamate 1374507-23-9
Rociletinib Intermediates Tert-butyl (3-aminophenyl)carbamate 68621-88-5
Rociletinib Intermediates 1-(4-(4-amino-3-methoxyphenyl)piperazin-1-yl)ethanone 1021426-42-5


GMP PRODUCE:

Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib 

2016 Mumbai CPHI, Hope to meet!
2016 Barcelona CPHI, Hope to meet!
2016 Korea(한국) CPHI, C40, Welcome!
2016 Shanghai CPHI, W5C47, Welcome!
EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
網址: www.eosmedchem.com 
郵箱: gutian@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp: +8618653174435
Skype: willgutian


Description: Rociletinib, also known as AVL-301 and CO1686, is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. EGFR inhibitor CO-1686 binds to and inhibits mutant forms of EGFR, including T790M, thereby leading to cell death of resistant tumor cells. Compared to other EGFR inhibitors, CO-1686 inhibits T790M, a secondary acquired resistance mutation, as well as other mutant EGFRs and may have therapeutic benefits in tumors with T790M-mediated resistance to other EGFR tyrosine kinase inhibitors.

Synonym: CO1686; CO-1686; CO 1686; AVL301; AVL 301; AVL-301; CNX419; CNX 419; CNX-419; Rociletinib.
IUPAC/Chemical Name: N-(3-((2-((4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide
SMILES Code: C=CC(NC1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C(C)=O)CC4)C=C3OC)=NC=C2C(F)(F)F)=C1)=O


1: Liu SV, Subramaniam D, Cyriac GC, Abdul-Khalek FJ, Giaccone G. Emerging protein kinase inhibitors for non-small cell lung cancer. Expert Opin Emerg Drugs. 2014 Mar;19(1):51-65. doi: 10.1517/14728214.2014.873403. Epub 2013 Dec 20. PubMed PMID: 24354593.



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We produce Poziotinib ( HM781-36B),1092364-38-9 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok

Name: Poziotinib ( HM781-36B)
CAS#: 1092364-38-9
Chemical Formula: C23H21Cl2FN4O3
Exact Mass: 490.09747
Molecular Weight: 491.34
Elemental Analysis: C, 56.22; H, 4.31; Cl, 14.43; F, 3.87; N, 11.40; O, 9.77

We produce Poziotinib ( HM781-36B),1092364-38-9 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Poziotinib ( HM781-36B),1092364-38-9 Intermediates, we have 8; Poziotinib ( HM781-36B),1092364-38-9 Impurity we have 10, all from GMP, FDA plant.
Now Poziotinib ( HM781-36B),1092364-38-9 DMF document is preparing.
Until 2016, Aug, Poziotinib ( HM781-36B),1092364-38-9 more than produced 25kg API, 120kg Intermediates

Poziotinib HM-781-36; HM-781-36B; NOV-1201;NOV-120101 1092364-38-9
Poziotinib Intermediates 3,4-Dihydro-7-methoxy-4-oxoquinazolin-6-yl acetate 179688-53-0
Poziotinib Intermediates 4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-ol 1429757-65-2


Description: Poziotinib , also known as HM781-36B and NOV120101, is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity. HM781-36B irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. EGFRs, cell surface receptor tyrosine kinases, are often upregulated in a variety of cancer cell types and play key roles in cellular proliferation and survival.
Synonym: HM781-36B; HM78136B; HM-78136B; HM 78136B; NOV120101; NOV-120101; NOV 120101; Poziotinib
IUPAC/Chemical Name: 1-(4-((4-((3,4-dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one
SMILES Code: C=CC(N1CCC(OC2=CC3=C(NC4=CC=C(Cl)C(Cl)=C4F)N=CN=C3C=C2OC)CC1)=O


1: Cha MY, Lee KO, Kim M, Song JY, Lee KH, Park J, Chae YJ, Kim YH, Suh KH, Lee GS, Park SB, Kim MS. Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models. Int J Cancer. 2012 May 15;130(10):2445-54. doi: 10.1002/ijc.26276. Epub 2011 Aug 24. PubMed PMID: 21732342.
  2: Nam HJ, Kim HP, Yoon YK, Hur HS, Song SH, Kim MS, Lee GS, Han SW, Im SA, Kim TY, Oh DY, Bang YJ. Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer. Cancer Lett. 2011 Mar 28;302(2):155-65. PubMed PMID: 21306821.
 
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We produce Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok

Name: Osimertinib mesylate
CAS#: 1421373-66-1 (mesylate)
Chemical Formula: C29H37N7O5S
Exact Mass:
Molecular Weight: 595.72
Elemental Analysis: C, 58.47; H, 6.26; N, 16.46; O, 13.43; S, 5.38

We produce Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0  in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.


Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0  Intermediates, we have 8; Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0  Impurity we have 10, all from GMP, FDA plant.
Now Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0  DMF document is preparing.


Until 2016, Aug, Osimertinib mesylate,Osimertinib free base,AZD 9291,1421373-66-1,1421373-65-0  more than produced 25kg API, 120kg Intermediates
 Osimertinib Mesylate AZD-9291 (Mesylate);Tagrisso; 1421373-66-1
Osimertinib Mesylate Intermediates N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide 1421373-65-0
Osimertinib Mesylate Intermediates N-(5-((4-(1H-indol-3-yl)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide 1421373-98-9
Osimertinib Mesylate Intermediates N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine 1421372-94-2
Osimertinib Mesylate Intermediates 3-(2-chloropyrimidin-4-yl)-1-methyl-1H-indole 1032452-86-0

GMP PRODUCE:

Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib 

2016 Mumbai CPHI, Hope to meet!
2016 Barcelona CPHI, Hope to meet!
2016 Korea(한국) CPHI, C40, Welcome!
2016 Shanghai CPHI, W5C47, Welcome!
EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
網址: www.eosmedchem.com 
郵箱: gutian@eosmedchem.com; eosmedchem@gmail.com 
辦公室: 0086-531-69905422-806(直通)
攜帶番號 & WhatsApp: +8618653174435
Skype: willgutian


Description: Osimertinib, also known as mereletinib and AZD-9291, is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291 is highly active in preclinical models and is well tolerated in animal models. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines. Osimertinib was approved on Nov. 2015.
Synonym: AZD-9291; AZD 9291; AZD9291; AZD-9291 mesylate; Mereletinib; Mereletinib mesylate; Osimertinib mesylate. Brand name: Tagrisso.
IUPAC/Chemical Name: N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide mesylate
SMILES Code: CN(CCN(C)C)C1=CC(OC)=C(C=C1NC(C=C)=O)NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2.OS(=O)(C)=O

1: Lung cancer: Diverse EGFR mutations explain AZD9291 resistance. Nat Rev Clin Oncol. 2015 May 19. doi: 10.1038/nrclinonc.2015.97. [Epub ahead of print] PubMed PMID: 25985937.
2: Thress KS, Paweletz CP, Felip E, Cho BC, Stetson D, Dougherty B, Lai Z, Markovets A, Vivancos A, Kuang Y, Ercan D, Matthews SE, Cantarini M, Barrett JC, Jänne PA, Oxnard GR. Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M. Nat Med. 2015 Jun;21(6):560-2. doi: 10.1038/nm.3854. Epub 2015 May 4. PubMed PMID: 25939061.
3: Jänne PA, Yang JC, Kim DW, Planchard D, Ohe Y, Ramalingam SS, Ahn MJ, Kim SW, Su WC, Horn L, Haggstrom D, Felip E, Kim JH, Frewer P, Cantarini M, Brown KH, Dickinson PA, Ghiorghiu S, Ranson M. AZD9291 in EGFR inhibitor-resistant non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1689-99. doi: 10.1056/NEJMoa1411817. PubMed PMID: 25923549.
4: Eberlein CA, Stetson D, Markovets AA, Al-Kadhimi KJ, Lai Z, Fisher PR, Meador CB, Spitzler P, Ichihara E, Ross SJ, Ahdesmaki MJ, Ahmed A, Ratcliffe LE, O'Brien EL, Barnes CH, Brown H, Smith PD, Dry JR, Beran G, Thress KS, Dougherty B, Pao W, Cross DA. Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models. Cancer Res. 2015 Jun 15;75(12):2489-500. doi: 10.1158/0008-5472.CAN-14-3167. Epub 2015 Apr 13. PubMed PMID: 25870145.
5: Jiang T, Zhou C. Clinical activity of the mutant-selective EGFR inhibitor AZD9291 in patients with EGFR inhibitor-resistant non-small cell lung cancer. Transl Lung Cancer Res. 2014 Dec;3(6):370-2. doi: 10.3978/j.issn.2218-6751.2014.08.02. PubMed PMID: 25806323; PubMed Central PMCID: PMC4367669.
6: Finlay MR, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DA, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67. doi: 10.1021/jm500973a. Epub 2014 Oct 1. PubMed PMID: 25271963.
7: AZD9291 could be an option for NSCLC. Cancer Discov. 2014 Aug;4(8):OF10. doi: 10.1158/2159-8290.CD-NB2014-077. Epub 2014 May 22. PubMed PMID: 25092747.
8: Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA, Mellor MJ, Hughes G, Rahi A, Jacobs VN, Red Brewer M, Ichihara E, Sun J, Jin H, Ballard P, Al-Kadhimi K, Rowlinson R, Klinowska T, Richmond GH, Cantarini M, Kim DW, Ranson MR, Pao W. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. doi: 10.1158/2159-8290.CD-14-0337. Epub 2014 Jun 3. PubMed PMID: 24893891; PubMed Central PMCID: PMC4315625.

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We produce Sotagliflozin,LX4211,1018899-04-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok

Name: Sotagliflozin
CAS#: 1018899-04-1
Chemical Formula: C21H25ClO5S
Exact Mass: 424.11112
Molecular Weight: 424.94
Elemental Analysis: C, 59.36; H, 5.93; Cl, 8.34; O, 18.83; S, 7.55


We produce Sotagliflozin,LX4211,1018899-04-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Sotagliflozin,LX4211,1018899-04-1 Intermediates, we have 8; Sotagliflozin,LX4211,1018899-04-1 Impurity we have 10, all from GMP, FDA plant.
Now Sotagliflozin,LX4211,1018899-04-1 DMF document is preparing.
Until 2016, Aug, Sotagliflozin,LX4211,1018899-04-1 more than produced 25kg API, 120kg Intermediates

Sotagliflozin LP-802034;LX-4211; 1018899-04-1
Sotagliflozin Intermediates ((3aS,5R,6S,6aS)-6-hydroxy-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl)(morpholino)methanone 1103738-19-7
Sotagliflozin Intermediates (3aS,5R,6S,6aS)-6-hydroxy-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxole-5-carboxylic acid 1103738-20-0
Sotagliflozin Intermediates (3aS,5S,6R,6aS)-5-(hydroxymethyl)-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-6-ol 114861-22-2
Sotagliflozin Intermediates (3aS,3bR,7aS,8aS)-2,2,5,5-tetramethyltetrahydro-3aH-[1,3]dioxolo[4',5':4,5]furo[3,2-d][1,3]dioxine 131156-47-3

GMP PRODUCE:

Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib 

2016 Mumbai CPHI, Hope to meet!
2016 Barcelona CPHI, Hope to meet!
2016 Korea(한국) CPHI, C40, Welcome!
2016 Shanghai CPHI, W5C47, Welcome!
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Description: Sotagliflozin, also known as LX4211, is an orally active and a dual SGLT1/SGLT2 inhibitor, which improves glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. LX4211 increases serum glucagon-like peptide 1 and peptide YY levels by reducing sodium/glucose cotransporter 1 (SGLT1)-mediated absorption of intestinal glucose. Sotagliflozin is currently being developed by Lexicon for the treatment of type 1 and type 2 diabetes mellitus. Sotagliflozin may be an effective and promising medication for treating not only Type 2 diabetes (the common target for non-insulin medications for diabetes), but also Type 1 as well.
Synonym: LX4211; LX 4211; LX 4211; Sotagliflozin
IUPAC/Chemical Name: (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol
SMILES Code: O[C@@H]([C@@H]([C@H]([C@H](C1=CC=C(Cl)C(CC2=CC=C(OCC)C=C2)=C1)O3)O)O)[C@H]3SC

1: Zambrowicz B, Lapuerta P, Strumph P, Banks P, Wilson A, Ogbaa I, Sands A, Powell D. LX4211 Therapy Reduces Postprandial Glucose Levels in Patients With Type 2 Diabetes Mellitus and Renal Impairment Despite Low Urinary Glucose Excretion. Clin Ther. 2014 Dec 16. pii: S0149-2918(14)00699-7. doi: 10.1016/j.clinthera.2014.10.026. [Epub ahead of print] PubMed PMID: 25529979.
2: Rosenstock J, Cefalu WT, Lapuerta P, Zambrowicz B, Ogbaa I, Banks P, Sands A. Greater Dose-Ranging Effects on A1C Levels Than on Glucosuria With LX4211, a Dual Inhibitor of Sodium Glucose Transporters SGLT1 and SGLT2, in Type 2 Diabetes on Metformin Monotherapy. Diabetes Care. 2014 Sep 11. pii: DC_140890. [Epub ahead of print] PubMed PMID: 25216510.
3: Powell DR, DaCosta CM, Smith M, Doree D, Harris A, Buhring L, Heydorn W, Nouraldeen A, Xiong W, Yalamanchili P, Mseeh F, Wilson A, Shadoan M, Zambrowicz B, Ding ZM. Effect of LX4211 on glucose homeostasis and body composition in preclinical models. J Pharmacol Exp Ther. 2014 Aug;350(2):232-42. doi: 10.1124/jpet.114.214304. Epub 2014 May 21. PubMed PMID: 24849925.
4: Mauricio D. [Sodium-glucose co-transporter-2 inhibitors: from the bark of apple trees and familial renal glycosuria to the treatment of type 2 diabetes mellitus]. Med Clin (Barc). 2013 Sep;141 Suppl 2:31-5. doi: 10.1016/S0025-7753(13)70061-7. Review. Spanish. PubMed PMID: 24444522.
5: Kanwal A, Banerjee SK. SGLT inhibitors: a novel target for diabetes. Pharm Pat Anal. 2013 Jan;2(1):77-91. doi: 10.4155/ppa.12.78. Review. PubMed PMID: 24236972.
6: Zambrowicz B, Ogbaa I, Frazier K, Banks P, Turnage A, Freiman J, Boehm KA, Ruff D, Powell D, Sands A. Effects of LX4211, a dual sodium-dependent glucose cotransporters 1 and 2 inhibitor, on postprandial glucose, insulin, glucagon-like peptide 1, and peptide tyrosine tyrosine in a dose-timing study in healthy subjects. Clin Ther. 2013 Aug;35(8):1162-1173.e8. doi: 10.1016/j.clinthera.2013.06.011. Epub 2013 Jul 31. PubMed PMID: 23911260.
7: Bloomgarden Z. Sodium glucose transporter 2 inhibition: a new approach to diabetes treatment. J Diabetes. 2013 Sep;5(3):225-7. doi: 10.1111/1753-0407.12065. Epub 2013 Jul 1. PubMed PMID: 23714218.
8: Lapuerta P, Rosenstock J, Zambrowicz B, Powell DR, Ogbaa I, Freiman J, Cefalu WT, Banks P, Frazier K, Kelly M, Sands A. Study design and rationale of a dose-ranging trial of LX4211, a dual inhibitor of SGLT1 and SGLT2, in type 2 diabetes inadequately controlled on metformin monotherapy. Clin Cardiol. 2013 Jul;36(7):367-71. doi: 10.1002/clc.22125. Epub 2013 Apr 29. PubMed PMID: 23630033.
9: Powell DR, Smith M, Greer J, Harris A, Zhao S, DaCosta C, Mseeh F, Shadoan MK, Sands A, Zambrowicz B, Ding ZM. LX4211 increases serum glucagon-like peptide 1 and peptide YY levels by reducing sodium/glucose cotransporter 1 (SGLT1)-mediated absorption of intestinal glucose. J Pharmacol Exp Ther. 2013 May;345(2):250-9. doi: 10.1124/jpet.113.203364. Epub 2013 Mar 13. PubMed PMID: 23487174.
10: Zambrowicz B, Ding ZM, Ogbaa I, Frazier K, Banks P, Turnage A, Freiman J, Smith M, Ruff D, Sands A, Powell D. Effects of LX4211, a dual SGLT1/SGLT2 inhibitor, plus sitagliptin on postprandial active GLP-1 and glycemic control in type 2 diabetes. Clin Ther. 2013 Mar;35(3):273-285.e7. doi: 10.1016/j.clinthera.2013.01.010. Epub 2013 Feb 21. PubMed PMID: 23433601.
11: Zambrowicz B, Freiman J, Brown PM, Frazier KS, Turnage A, Bronner J, Ruff D, Shadoan M, Banks P, Mseeh F, Rawlins DB, Goodwin NC, Mabon R, Harrison BA, Wilson A, Sands A, Powell DR. LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. Clin Pharmacol Ther. 2012 Aug;92(2):158-69. doi: 10.1038/clpt.2012.58. Epub 2012 Jul 4. PubMed PMID: 22739142; PubMed Central PMCID: PMC3400893.
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