公开(公告)号：US20160244438A1

公开(公告)日：2016-08-25

申请号：US15024020

申请日：2014-11-27

Applicant: SUNSHINE LAKE PHARMA CO., LTD.

Inventor： Qingyun REN ,  Xinchang LIU ,  Zhifu ZOU ,  Guanghua YAN ,  Mingchao BI ,  Siegfried GOLDMANN ,  Yingjun ZHANG

IPC: C07D417/04 ,  C07D417/14

CPC classification number: C07D417/04 ,  C07D417/14

Abstract: The present invention relates to processes for preparing a dihydropyrimidine derivative having Formula (I) or a tautomer thereof having Formula (Ia), as well as a intermediate thereof. The processes of the invention have simple operation, high optical purity of product, high yield and convenient work-up, which is suitable for industrial production.

Abstract translation: 本发明涉及制备具有式（I）的二氢嘧啶衍生物或其具有式（Ia）的互变异构体的方法及其中间体。 本发明方法操作简单，产品光学纯度高，产量高，加工方便，适用于工业生产。

公开(公告)号：US20160264562A1

公开(公告)日：2016-09-15

申请号：US15023676

申请日：2014-11-27

Applicant: SUNSHINE LAKE PHARMA CO., LTD.

Inventor： Xinchang LIU ,  Qingyun REN ,  Zhifu ZOU ,  Jinsheng LIANG ,  Linjin TU ,  Siegfried GOLDMANN ,  Yingjun ZHANG

IPC: C07D417/04 ,  C07D417/14

CPC classification number: C07D417/04 ,  C07D417/14

Abstract: The present invention refers to processes for preparing a dihydropyrimidine compound having Formula (I), or a tautomer thereof having Formula (la), as well as a intermediate thereof. The process of the invention has simple operation, high optical purity of product, high yield and convenient work-up, which is suitable for industrial production.

公开(公告)号：US20180263991A1

公开(公告)日：2018-09-20

申请号：US15539147

申请日：2016-02-01

Applicant: SUNSHINE LAKE PHARMA CO., LTD

Inventor： Qingyun Ren ,  Liang CHEN ,  Xinchang LIU ,  Jinsheng LIANG ,  Chenliang WU ,  Zhifu ZOU ,  Guanghua YAN ,  Desheng HUANGFU ,  Siegfried GOLDMANN ,  Yingjun ZHANG

IPC: A61K31/5377 ,  A61P1/16 ,  A61P31/20 ,  A61P35/00

Abstract: This invention relates to L-tartaric acid complexes, acid addition salts, base addition salts of the compound named (S)-4-(((R)-6-(2-chloro-4-fluorophenyl)-5-(methoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl) methyl) morpholine-3-carboxylic acid or tautomer thereof and pharmaceutical compositions thereof, and further relates to use of the compounds or the pharmaceutical compositions in the manufacture of a medicament, especially for use in preventing, managing, treating or lessening a HBV infection. The complex, acid addition salt or base addition salt of the present invention is crystalline form, substantially crystalline form, polymorphism, amorphism, hydrate or solvate.

公开(公告)号：US20160264563A1

公开(公告)日：2016-09-15

申请号：US15023688

申请日：2014-11-27

Applicant: SUNSHINE LAKE PHARMA CO., LTD.

Inventor： Qingyun REN ,  Xinchang LIU ,  Zhifu ZOU ,  Linjin TU ,  Yuefeng SHAN ,  Douxing LEI ,  Slegfried GOLDMANN ,  Yingjun ZHANG

IPC: C07D417/04 ,  C07D417/14

CPC classification number: C07D417/04 ,  C07D417/14

Abstract: The present invention refers to processes for preparing a dihydropyrimidine compound having Formula (I), or a tautomer thereof having Formula (Ia), as well as a intermediate thereof. The process of the invention has simple operation, high optical purity of product, high yield and convenient work-up, which is suitable for industrial production.

公开(公告)号：US20160206616A1

公开(公告)日：2016-07-21

申请号：US15022562

申请日：2014-11-18

Applicant: SUNSHINE LAKE PHARMA CO., LTD.

Inventor： Yingjun Zhang ,  Xinchang LIU ,  Zhifu ZOU ,  Jinsheng LIANG ,  Siegfried GOLDMANN ,  Qingyun REN

IPC: A61K31/506 ,  C07D403/14 ,  A61K31/541 ,  A61K45/06 ,  C07D417/14

CPC classification number: A61K31/506 ,  A61K31/541 ,  A61K45/06 ,  C07D403/14 ,  C07D417/14

Abstract: Provided herein are dihydropyrimidine compounds and their pharmaceutical applications, especially for use in treating and preventing HBV diseases. Specifically, provided herein are compounds having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, wherein the variables of the formulas are as defined in the specification. Also provided herein is the use of the compounds having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof for treating and preventing HBV diseases.