- Ledipasvir preparation method
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The invention discloses a Ledipasvir preparation method. The Ledipasvir preparation method includes steps: (1) Ledipasvir intermediate product 1-LD-B preparation; (2) Ledipasvir intermediate product 2-LD-E preparation; (3) Ledipasvir intermediate product 3-LD-F preparation; (4) Ledipasvir intermediate product 4-LD-J preparation; (5) Ledipasvir intermediate product 5-LD-L preparation; (6) Ledipasvir-LD-Q preparation. The Ledipasvir preparation method has advantages of technical maturity and stability, product quality stability, safety and reliability in production process and suitableness for industrial production.
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Paragraph 0094; 0095; 0097; 0118; 0120; 0121; 0191; 0260
(2018/05/16)
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- Preparation method of Ledipasvir
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The invention discloses a preparation method of Ledipasvir. The method has no need for chromatographic column separation, reduces the cost of raw materials, and can acquire a high purity product by a simple precipitation or crystallization purification means, thus providing feasible technical conditions for large-scale industrial production.
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Paragraph 0035; 0036;
(2016/10/31)
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- Hepatitis C virus inhibitor, medical composition and application thereof
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The invention provides a hepatitis C virus inhibitor, a medical composition and application thereof. The hepatitis C virus inhibitor is a compound as shown in a formula (I), or salt, hydrate or a solvent compound accepted in crystal forms and pharmacy. The compound disclosed by the invention has better hepatitis C viral protein NS5A restraining activity, has better pharmacodynamics/pharmacokinetics properties, is good in applicability and high in safety, can be used for preparing medicines for treating hepatitis C virus infection, and has favorable market development prospects.
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Paragraph 0066; 0067
(2017/04/18)
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- Discovery of ledipasvir (GS-5885): A potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection
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A new class of highly potent NS5A inhibitors with an unsymmetric benzimidazole-difluorofluorene-imidazole core and distal [2.2.1]azabicyclic ring system was discovered. Optimization of antiviral potency and pharmacokinetics led to the identification of 39 (ledipasvir, GS-5885). Compound 39 (GT1a replicon EC50 = 31 pM) has an extended plasma half-life of 37-45 h in healthy volunteers and produces a rapid >3 log viral load reduction in monotherapy at oral doses of 3 mg or greater with once-daily dosing in genotype 1a HCV-infected patients. 39 has been shown to be safe and efficacious, with SVR12 rates up to 100% when used in combination with direct-acting antivirals having complementary mechanisms.
- Link, John O.,Taylor, James G.,Xu, Lianhong,Mitchell, Michael,Guo, Hongyan,Liu, Hongtao,Kato, Darryl,Kirschberg, Thorsten,Sun, Jianyu,Squires, Neil,Parrish, Jay,Keller, Terry,Yang, Zheng-Yu,Yang, Chris,Matles, Mike,Wang, Yujin,Wang, Kelly,Cheng, Guofeng,Tian, Yang,Mogalian, Erik,Mondou, Elsa,Cornpropst, Melanie,Perry, Jason,Desai, Manoj C.
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p. 2033 - 2046
(2014/04/03)
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- SOLID FORMS OF AN ANTIVIRAL COMPOUND
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Amorphous and crystalline solid forms of the anti-HCV compound (1-{3-[6-(9,9-difluoro-7-{2-[5-(2-methoxycarbonylamino-3-methyl-butyryl)-5-aza-spiro[2.4]hept-6-yl]-3H-imidazol-4-yl}-9H-fluoren-2-yl)-1H-benzoimidazol-2-yl]-2-aza-bicyclo[2.2.1]heptane-2-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the amorphous and crystalline forms.
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Paragraph 0246-0247
(2014/01/07)
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- SYNTHESIS OF ANTIVIRAL COMPOUND
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The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
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