公开(公告)号：US20160153015A1

公开(公告)日：2016-06-02

申请号：US14782586

申请日：2013-06-27

申请人： 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

发明人： Hao HONG ,  Changsheng ZHENG ,  Lina GUO

IPC分类号： C12P17/12 ,  C12P17/00 ,  A61K31/4409 ,  A61K38/44 ,  A61K31/4406 ,  A61K31/415 ,  A61K31/422 ,  C12P17/10 ,  A61K31/4402

CPC分类号： C12P17/12 ,  A61K31/415 ,  A61K31/422 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K38/44 ,  A61K48/00 ,  C07D213/55 ,  C07D231/12 ,  C07D333/24 ,  C12P13/04 ,  C12P13/22 ,  C12P17/00 ,  C12P17/10 ,  C12P41/006 ,  C12Y102/01002 ,  C12Y104/0102

摘要： A synthesis method for an L-heterocyclic amino acid and a pharmaceutical composition having the said amino acid are provided in the present disclosure. The synthesis method comprises: step A: preparing a heterocyclic keto acid, wherein the heterocycle in the heterocyclic keto acid is selected from any one of a five-membered heterocycle, a six-membered heterocycle, a seven-membered heterocycle, an alkyl-substituted five-membered heterocycle, an alkyl-substituted six-membered heterocycle, and an alkyl-substituted seven-membered heterocycle, and the keto acid group in the heterocyclic keto acid has a structural formula of and is located on any one of the carbon positions of the heterocycle, and step B: mixing the heterocyclic keto acid with ammonium formate, a phenylalanine dehydrogenase, a formate dehydrogenase and a coenzyme NAD+, and carrying out a reductive amination reaction to generate L-heterocyclic amino acid, wherein the amino acid sequence of the phenylalanine dehydrogenase is SEQ ID No. 1.

摘要翻译： 在本公开内容中提供了具有所述氨基酸的L-杂环氨基酸的合成方法和药物组合物。 合成方法包括：步骤A：制备杂环酮酸，其中杂环酮酸中的杂环选自五元杂环，六元杂环，七元杂环，烷基取代的 五元杂环，烷基取代的六元杂环和烷基取代的七元杂环，并且杂环酮酸中的酮酸基具有结构式，位于任何一个碳位上 杂环和步骤B：将杂环酮酸与甲酸铵，苯丙氨酸脱氢酶，甲酸脱氢酶和辅酶NAD +混合，并进行还原胺化反应以产生L-杂环氨基酸，其中氨基酸序列 苯丙氨酸脱氢酶是SEQ ID No.1。

公开(公告)号：US20180148430A1

公开(公告)日：2018-05-31

申请号：US15574528

申请日：2015-05-26

申请人： 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

发明人： Hao HONG ,  Gage JAMES ,  Jiuyuan LI ,  Changfeng LI ,  Gaochao HUANG

IPC分类号： C07D401/14

CPC分类号： C07D401/14

摘要： A method for preparing nilotinib includes the following steps: performing an aminocarbonylation reaction on a compound A and 3-(4-methyl-1H-imidazole-1-yl)-5-(trifluoromethyl) aniline to obtain an amination product; and performing deprotection treatment of an R group on the amination product to obtain the nilotinib, wherein the compound A has a structure shown in formula I, and in formula I, an R group is selected from benzyl, —COCF3, —CHO or —CO2R′, where an R′ group is C1˜C10 alkyl, C1˜C3 alkoxy ethyl or C7˜C19 aralkyl.

公开(公告)号：US20170136450A1

公开(公告)日：2017-05-18

申请号：US15039189

申请日：2014-09-10

申请人： 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.

发明人： Hao HONG ,  Jiuyuan LI ,  Changming DONG ,  Xin ZHANG ,  Gage JAMES

IPC分类号： B01J31/06 ,  B01J31/28 ,  C07D477/04 ,  C08J9/00 ,  C08J9/14 ,  C08F212/08

CPC分类号： B01J31/06 ,  B01J23/464 ,  B01J31/28 ,  C07D477/04 ,  C07D477/06 ,  C08F12/22 ,  C08F12/26 ,  C08F12/32 ,  C08F12/34 ,  C08F212/08 ,  C08F212/14 ,  C08J9/0061 ,  C08J9/141 ,  C08J9/142 ,  C08J9/145 ,  C08J9/149 ,  C08J2203/12 ,  C08J2203/14 ,  C08J2203/142 ,  C08J2325/08 ,  C08J2405/00 ,  C08J2429/04 ,  Y02P20/584 ,  C08F212/34 ,  C08F212/36 ,  C08F212/32

摘要： A polymer containing a carboxyl group, a preparation method and an application thereof, a supported catalyst and a preparation method thereof and preparation methods of penem antibiotic intermediate are disclosed. The polymer has high rigidity and hardness, thus the mechanical properties of the polymer is effectively improved. Meanwhile, in the polymer, the carboxyl group is used as a main functional group, and is used as a carrier to prepare, by means of a coordination reaction between the carboxyl group and a heavy metal, a supported metal catalyst which has better connection stability between the metal and the polymer. The above two factors can improve the stability of the supported metal catalyst, such that the catalyst can be recycled without losing the catalytic activity. Meanwhile, loss of a heavy metal active ingredient and production cost can be reduced.

公开(公告)号：US20170073713A1

公开(公告)日：2017-03-16

申请号：US15039804

申请日：2014-10-31

申请人： 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

发明人： Hao HONG ,  Feng GAO ,  Yanjun LI ,  Yan ZHANG ,  Shaohe Li

IPC分类号： C12P13/00 ,  C12N9/10 ,  C12N15/70 ,  C12P17/12

CPC分类号： C12P13/001 ,  C12N1/20 ,  C12N9/1096 ,  C12N15/70 ,  C12P17/12 ,  C12Y206/01

摘要： A transaminase and a use thereof are provided. The transaminase has the amino acid sequences as shown in SEQ ID NO: 2 or 4, or has at least 80% identity to the amino acid sequences as shown in SEQ ID NO: 2 or 4, or has amino acid sequences which are obtained by the substitution, deletion or addition of one or more amino acids and have an the activity of an omega-transaminase with high stereoselective R-configuration catalytic activity, wherein the high stereoselective refers to the content of one of the stereoisomers being at least about 1.1 times that of the other.

摘要翻译： 提供了转氨酶及其用途。 转氨酶具有如SEQ ID NO：2或4所示的氨基酸序列，或者与SEQ ID NO：2或4所示的氨基酸序列具有至少80％的同一性，或具有通过以下步骤获得的氨基酸序列： 一个或多个氨基酸的取代，缺失或添加并且具有高立体选择性R构型催化活性的ω-转氨酶的活性，其中高立体选择性指立体异构体之一的含量为至少约1.1倍 那另一个。

公开(公告)号：US20170022169A1

公开(公告)日：2017-01-26

申请号：US15124083

申请日：2014-03-07

申请人： 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.

发明人： Hao HONG ,  James GAGE ,  Jiuyuan LI ,  Litao SHEN ,  Lei ZHANG ,  Changming DONG

IPC分类号： C07D239/42

CPC分类号： C07D239/42 ,  C07B2200/13 ,  C07F9/6512 ,  Y02P20/55

摘要： 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.

摘要翻译： 提供了用于制备瑞舒伐他汀钙的中间体化合物和罗苏伐他汀钙的制备方法。 该方法包括：使用上述中间体化合物作为原料，并对原料进行维蒂希反应的步骤，保护基团除去和水解的步骤和钙盐形成步骤，以获得瑞舒伐他汀钙。 由中间体化合物制备的产物可以显着增强立体选择性，并且还显着提高了纯度和产率; 另外，从中间体化合物制备瑞舒伐他汀钙的方法简单，方便，成本低。

公开(公告)号：US20220380817A1

公开(公告)日：2022-12-01

申请号：US17755266

申请日：2019-10-25

申请人： ASYMCHEM LABORATORIES (FUXIN) CO., LTD.

发明人： Hao HONG ,  Gage JAMES ,  Yi XIAO ,  Fang LIU ,  Na ZHANG ,  Zujian WANG ,  Junjie YAN ,  Wanming SHI ,  Mujiao ZHANG ,  Ye LIU

IPC分类号： C12P13/00 ,  C12N9/10 ,  C12N15/70 ,  C12N1/20

摘要： An amino acid sequence of the transaminase mutant is an amino acid sequence obtained by a mutation of an amino acid sequence is shown in SEQ ID NO: 1. The mutation occurred at least one of the following mutation sites: G17V, L36P, Q40H, G69Y, H70T, L73A, V77G, V77S, V77T, A78I, Y130M, Y130V, Y130T, N132I, N132T, K141S, K142S, K142T, R143P, G144F, G144W, G144Y, E145D, E145S, E145G, K146R, L148A, L148I and the like.

公开(公告)号：US20220403421A1

公开(公告)日：2022-12-22

申请号：US17774891

申请日：2019-11-07

申请人： ASYMCHEM LABORATORIES (FUXIN) CO., LTD.

发明人： Hao HONG ,  Gage JAMES ,  Yi HSIAO ,  Na ZHANG ,  Xuecheng JIAO ,  Kejian ZHANG ,  Yiming YANG ,  Xiang WANG ,  Yanqing ZHANG

IPC分类号： C12P7/24 ,  C12N9/04 ,  C12N15/70 ,  C12N1/20

摘要： Disclosed are a ketoreductase mutant and a method for producing a chiral alcohol. The ketoreductase mutant has an amino acid sequence obtained by the mutation of the amino acid sequence shown in SEQ ID NO: 1, and the mutation includes a mutation siteK200H. In the present disclosure, the mutant obtained by mutation takes a ketone compound as a raw material, the chiral alcohol may be efficiently produced by stereoselective reduction, and the stability is greatly improved, which is suitable for popularization and application to the industrial production of the chiral alcohol.

公开(公告)号：US20220297080A1

公开(公告)日：2022-09-22

申请号：US17642194

申请日：2019-09-12

申请人： ASYMCHEM LABORATORIES (FUXIN) CO., LTD.

发明人： Hao HONG ,  Jiangping LU ,  Xichun FENG ,  Xin ZHANG ,  Bo YAN

IPC分类号： B01J19/18 ,  C07C41/54 ,  C07C45/50 ,  C07C45/64

摘要： The present disclosure provides a device for continuously preparing 2,6-dihydroxybenzaldehyde and use thereof. The device includes a first continuous reaction unit for hydroxy protection reaction, a second continuous reaction unit for lithiation and hydroformylation, and a third continuous reaction unit for deprotection reaction that are connected in series. The third continuous reaction unit includes: a first columnar continuous reactor, connected to the second continuous reaction unit and used for deprotection of the lithiated hydroformylated product while performing liquid separation to obtain an organic phase containing 2,6-dihydroxybenzaldehyde and an aqueous phase. When the device is applied in the preparation of 2,6-dihydroxybenzaldehyde, reaction time is shortened and the intermediate purification treatment is no longer required. Therefore, compared with batch process, the present disclosure can greatly save equipment cost and post-processing cost, and greatly improve the production efficiency, more beneficial to the industrial scale-up production of 2,6-dihydroxybenzaldehyde.

公开(公告)号：US20210095262A1

公开(公告)日：2021-04-01

申请号：US17118169

申请日：2020-12-10

申请人： 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.

发明人： Hao HONG ,  Gage JAMES ,  Jiangping LU ,  Na ZHANG ,  Wenyan YU ,  Fang LIU ,  Yanjun LI ,  Xin HUANG ,  Juan GAO ,  Kejian ZHANG ,  Yulei MA ,  Junlu WEI

IPC分类号： C12N9/02 ,  C12N15/70 ,  C12N15/81

摘要： Provided are a proline hydroxylase and uses thereof. The proline hydroxylase comprises having the amino acid sequence of SEQ ID NO: 2 with the exception of a mutation of one or more amino acids; wherein the mutation of one or more amino acids must comprises E27K, and the mutation of one or more amino acids selected from the group consisting of: H14R, L16N, T25R, F26L, E27K, D30S, S33N, E34N, E34G, E34L, E34S, E34D, Y35W, Y35K, S37W, S37F, S37E, S37N, S37T, S37C, W40F, K41E, D54G, H55Q, S57L, I58T, I58Y, I58A, I58R, I58V, I58S, I58C, K86P, T91A, F95Y, C97Y, I98V, K106V, K106T, K106Q, F111S, K112E, K112R, S154A, K162E, L166M, I118F, I118V, I118R, H119R, H119F, I120V, K123D, K123N, K123Q, K123S, K123I, K123T, T130N, D134G, V135K, N165H, D173G, K209R, I223V and S225A, and having proline hydroxylase activity.

公开(公告)号：US20170002338A1

公开(公告)日：2017-01-05

申请号：US15039736

申请日：2014-10-29

申请人： 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

发明人： Hao HONG ,  Feng GAO ,  Yanjun LI ,  Yan ZHANG ,  Shaohe LI

IPC分类号： C12N9/10 ,  C12P13/00 ,  C12P17/12

CPC分类号： C12N9/1096 ,  C12P13/001 ,  C12P17/12 ,  C12P41/006 ,  C12Y206/01

摘要： An omega-transaminase of R-configuration is provided. The omega-transaminase of R-configuration has the amino acid sequence as shown in SEQ ID NO: 2, or has at least 80% identity to the amino acid sequence as shown in SEQ ID NO: 2, or has the amino acid sequence of proteins which have substituted, deleted or added one or more amino acids and have the activity of an omega-transaminase with a high stereoselectivity R-configuration catalytic activity; and does not have the amino acid sequence encoded by the nucleotide sequence as shown in SEQ ID NO: 4. The high stereoselectivity refers to the content of one of the stereoisomers being at least about 1.1 times that of the other. A use of the omega-transaminase of R-configuration is provided.

摘要翻译： 提供R-构型的ω-转氨酶。 R构型的ω-转氨酶具有如SEQ ID NO：2所示的氨基酸序列，或与SEQ ID NO：2所示的氨基酸序列具有至少80％的同一性，或具有SEQ ID NO：2所示的氨基酸序列 具有取代，缺失或添加一个或多个氨基酸并且具有高立体选择性R构型催化活性的ω-转氨酶活性的蛋白质; 并且不具有由SEQ ID NO：4所示的核苷酸序列编码的氨基酸序列。高立体选择性是指立体异构体之一的含量为至少约1.1倍。 提供了R-构型的ω-转氨酶的用途。