-
公开(公告)号：US20240093167A1
公开(公告)日：2024-03-21
申请号：US18262480
申请日：2021-03-02
Applicant: ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD.
Inventor： Hao Hong , James Gage , Yi Xiao , Na Zhang , Xuecheng Jiao , Yiming Yang , Xiang Wang , Junqi Zhao
Abstract: Provided are an esterase mutant and use thereof. The amino acid sequence of the esterase mutant has a sequence as shown in SEQ ID NO: 1, and sites at which amino acid mutations occur include an N51G site.
-
公开(公告)号：US10961516B2
公开(公告)日：2021-03-30
申请号：US16344779
申请日：2016-11-04
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD. , TIANJIN ASYMCHEM PHARMACEUTICALS CO., LTD. , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO., LTD.
Inventor： Hao Hong , Gage James , Jiangping Lu , Na Zhang , Wenyan Yu , Fang Liu , Yanjun Li , Xin Huang , Juan Gao , Kejian Zhang , Yulei Ma , Junlu Wei
Abstract: Provided are a proline hydroxylase and uses thereof. The proline hydroxylase comprises (a) a protein having the amino acid sequence as shown in SEQ ID NO: 2; (b) a protein having an amino acid sequence of SEQ HD NO: 2 with a mutation of one or more amino acids and having a proline hydroxylase activity; or (c) a protein retaining the mutation of one or more amino acids as in (b), and having the proline hydroxylase activity and having at least 78% homology with the amino acid sequence of the protein in (b). Protein having the amino acid sequence as shown in SEQ HD NO: 2 and mutants obtained by genetically engineering have higher catalytic specificity or significantly increased catalytic activity when compared to proline hydroxylases in prior art.
-
公开(公告)号：US10544119B2
公开(公告)日：2020-01-28
申请号：US15309469
申请日：2014-08-04
Applicant: Asymchem Laboratories (Tianjin) Co., Ltd. , Asymchem Life Science (Tianjin) Co., Ltd. , Tianjin Asymchem Pharmaceutical Co., Ltd. , Asymchem Laboratories (Fuxin) Co., Ltd. , Jilin Asymchem Laboratories Co., Ltd.
Inventor： Hao Hong , Chaoyong Chen , Jiuyuan Li , Litao Shen , Lina Guo , Hongying Tian
IPC: C07D319/06 , C12P7/62 , C07C51/367 , C07C67/30 , C07C67/313
Abstract: The present invention relates to a preparation method for a chiral intermediate for use in statins, acquired with chloroacetic acid and benzyl alcohol as starting materials via a series of reactions, namely etherification, condensation, substitution, and asymmetric reduction. The preparation method provided in the present invention has a novel route of synthesis, allows an intermediate compound to be introduced conveniently into the chiral center of a glycol via enzyme reduction, and not only is low in costs, but also is reliable in quality. The route of synthesis provided in the present invention uses raw materials of low costs, has an easy to operate process, and provides a final product of great purity and high yield.
-
公开(公告)号：US10131883B2
公开(公告)日：2018-11-20
申请号：US15309690
申请日：2014-08-04
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD. , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD. , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO., LTD.
Abstract: The application provides a Diketoreductase (DKR) mutant, its nucleotide coding sequence, and an expression cassette, recombinant vector and host cell containing the sequence, as well as a method for application of the mutant to the preparation of 3R,5S-dicarbonyl compound. An ee value of the obtained 3R,5S-dicarbonyl compound is higher than 99%, and a de value is about 90%. The DKR mutant is a key pharmaceutical intermediate, and particularly provides an efficient catalyst for synthesis of a chiral dicarbonyl hexanoic acid chain of a statin drug.
-
公开(公告)号：US20150105555A1
公开(公告)日：2015-04-16
申请号：US14391712
申请日：2012-12-27
Applicant: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO., LTD.
Inventor： Hao Hong , James Gage , Chaoyong Chen , Jiangping Lu , Yan Zhou , Shuangyong Liu
IPC: C07D475/04 , C07D317/32 , C07D317/26 , C07D301/12 , C07C221/00 , C07D239/50 , C07D301/14 , C07D301/03 , C07D317/28
CPC classification number: C07D475/04 , C07C221/00 , C07D239/50 , C07D301/03 , C07D301/12 , C07D301/14 , C07D317/26 , C07D317/28 , C07D317/32
Abstract: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
Abstract translation: 披露了一种合成沙rop in二盐酸盐的方法。 本公开内容减少了沙棘蛋白二盐酸盐的合成途径，以不对称合成方式引入手性中心，其中采用含有钐催化剂的四氢呋喃溶液作为催化剂，并通过方法获得具有高抗反义异构性值的目标化合物 的选择性催化。 产量提高，原料便宜，易于获得，成本显着降低，为大规模工业生产四氢叶酸二盐酸盐提供了有效的方案。
-
公开(公告)号：US20240401091A1
公开(公告)日：2024-12-05
申请号：US18691605
申请日：2021-10-13
Applicant: ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD.
Inventor： Hao Hong , Gage James , Na Zhang , Xuecheng Jiao , Fang Liu , Ru Jia
Abstract: Provided are a lipase mutant and an application thereof. Specifically, one or more mutations selected from A262H, A338V, V3641, A158PN, and 1159N are generated on the basis of an amino acid sequence as shown in SEQ ID NO: 1; and compared with a parental lipase, a change in the structure and function of a protein occurs in the lipase mutant, and the stereoselectivity is improved, such that a usage amount of an enzyme is decreased to a certain extent, the post-treatment difficulty is reduced, and the lipase mutant is suitable for industrial production.
-
公开(公告)号：US20240084271A1
公开(公告)日：2024-03-14
申请号：US18262127
申请日：2021-03-21
Applicant: ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD.
Inventor： Hao Hong , James Gage , Yi Xiao , Na Zhang , Xuecheng Jiao , Rui Li , Yanqing Zhang , Yiming Yang
CPC classification number: C12N9/0016 , C12N15/70 , C12P13/04
Abstract: Provided are an amino acid dehydrogenase mutant and use thereof. The amino acid sequence of the amino acid dehydrogenase mutant has a sequence as shown in SEQ ID NO: 1, and sites at which amino acid mutations occur include a K144G site.
-
公开(公告)号：US11407982B2
公开(公告)日：2022-08-09
申请号：US16756649
申请日：2017-11-06
Applicant: Asymchem Life Science (Tianjin) Co., Ltd
Inventor： Hao Hong , Gage James , Jiangping Lu , Xuecheng Jiao , Na Zhang , Rui Li , Kejian Zhang
Abstract: Disclosed are transaminase mutants and use thereof. The amino acid sequence of the transaminase mutant is obtained by the mutation of the amino acid sequence as shown in SEQ ID NO: 1, and the mutation at least comprises one of the following mutation sites: the 19-th site, the 41-th site, the 43-th site, the 72-th site, the 76-th site, the 92-th site, the 107-th site, the 125-th site, the 132-th site, the 226-th site, the 292-th site, the 295-th site, the 308-th site, and the 332-th site; and the 19-th site is mutated into a serine, the 41-th site is mutated into a serine, the 43-th site is mutated into an asparagine, a glycine in the 72-th site is mutated into a leucine, etc.; or the amino acid sequence of the transaminase mutant has the mutation sites in the mutanted amino acid sequence, and has more than 80% homology to the mutanted amino acid sequence.
-
公开(公告)号：US09926283B2
公开(公告)日：2018-03-27
申请号：US15124083
申请日：2014-03-07
Applicant: Asymchem Laboratories (Tianjin) Co., Ltd. , Asymchem Life Science (Tianjin) Co., Ltd. , Tianjin Asymchem Pharmaceutical Co., Ltd. , Asymchem Laboratories (Fuxin) Co., Ltd. , Jilin Asymchem Laboratories Co., Ltd.
Inventor： Hao Hong , James Gage , Jiuyuan Li , Litao Shen , Lei Zhang , Changming Dong
IPC: C07D239/42 , C07F9/6512
CPC classification number: C07D239/42 , C07B2200/13 , C07F9/6512 , Y02P20/55
Abstract: Provided are an intermediate compound for preparing rosuvastatin calcium and a preparation method of the rosuvastatin calcium. The method comprises: using the foregoing intermediate compound as a raw material, and subjecting the raw material to a step of Wittig reaction, a step of protecting group removal and hydrolysis and a step of calcium salt formation, so as to obtain the rosuvastatin calcium. The product, which is prepared from the intermediate compound, can be substantially enhanced in stereoselectivity and also notably improved in purity and yield; in addition, the method for preparing rosuvastatin calcium from the intermediate compound is simple, convenient and low in cost.
-
公开(公告)号：US20150119573A1
公开(公告)日：2015-04-30
申请号：US14394079
申请日：2012-12-27
Applicant: ASYMCHEM LABORATORIES (TIANJIN)CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD. , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO. LTD.
Inventor： Hao Hong , James Gage , Chaoyong Chen , Jiangping Lu , Yan Zhou , Shuangyong Liu
IPC: C07D475/04 , C07D317/32 , C07D317/26 , C07C221/00 , C07D239/50 , C07C209/62 , C07D317/28 , C07D303/48 , C07C225/06
CPC classification number: C07D475/04 , C07C209/62 , C07C221/00 , C07C225/06 , C07D239/50 , C07D303/48 , C07D317/26 , C07D317/28 , C07D317/32
Abstract: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
Abstract translation: 披露了一种合成沙rop in二盐酸盐的方法。 本公开内容减少了沙棘蛋白二盐酸盐的合成途径，并且通过使用手性拆分试剂拆分外消旋体中间体或具有低antimer异构值的中间体，从而获得具有高antimer异构值的中间体。 原材料便宜，易于获得，成本显着降低，为大规模工业生产四氢叶酸二盐酸盐提供了有效的方案。
