公开(公告)号：WO2022067724A1

公开(公告)日：2022-04-07

申请号：PCT/CN2020/119547

申请日：2020-09-30

Applicant: 北京睿创康泰医药研究院有限公司 ,  天津睿创康泰生物技术有限公司

Inventor： 贾慧娟 ,  侯伟 ,  任晓慧 ,  郭亮 ,  董艳阳

IPC: C07H7/04 ,  C07D409/10 ,  C07D309/10 ,  A61K31/7042 ,  A61P3/10 ,  A61P13/12 ,  A61P9/00

Abstract: 提供了一种SGLT-2抑制剂·肌氨酸共晶体及其制备方法和应用。以肌氨酸为配体，具有较高的安全性和较低的成本；药物共晶体具有较高的稳定性，在制剂组合物生产过程或贮藏过程中，晶型不易发生改变；不会遇热熔融，不会发生粘冲、聚团或产生静电，具有更好的混合均匀性；在制备的药物组合物中分布均匀，使得药物组合物具有更好的体内释放、吸收和药效，且批间差异小；具有较高的稳定性，更利于贮藏、运输；制备工艺简单，重现性高，且析晶时间短，工艺条件要求低，具有更高的经济效益；制备过程中不使用不安全溶剂；可同时对SGLT-2抑制剂粗品或中间体进行纯化。

公开(公告)号：WO2022053576A1

公开(公告)日：2022-03-17

申请号：PCT/EP2021/074852

申请日：2021-09-09

Applicant: STICHTING KATHOLIEKE UNIVERSITEIT

Inventor： PIJNENBORG, Johan Franciscus Adrianus ,  BOLTJE, Thomas Jan ,  ROSSING, Emiel

IPC: C07D309/10 ,  A61K31/351 ,  C07H19/207 ,  C07H11/04

Abstract: The present invention relates to a new class of compounds based on a hexose featuring at least two 6-fluorides. The class is useful as inhibitors of 4,6-dehydratase enzymes. Such inhibitors are suitable for use as a medicament, for example for treating, preventing, or delaying cancer, tumor metastasis, inflammation, infections, or genetic disorders.

公开(公告)号：WO2021245253A1

公开(公告)日：2021-12-09

申请号：PCT/EP2021/065044

申请日：2021-06-04

Applicant: KRKA, D.D., NOVO MESTO

Inventor： POLOVIC, Aleš ,  BENKIC, Primoz ,  OSTERMAN, Nika ,  GRUBAR, Mateja ,  VOVKO, Jernejka ,  KOBAL, Tjaž ,  KUFNER, Monika

IPC: C07D309/10

Abstract: A novel and improved process for the preparation of amorphous dapagliflozin is disclosed. The present invention further provides pharmaceutical compositions containing amorphous dapagliflozin, optionally in a combination with one or more other active substances and methods for making the same.

公开(公告)号：WO2021227441A1

公开(公告)日：2021-11-18

申请号：PCT/CN2020/131253

申请日：2020-11-24

Applicant: 上海喆邺生物科技有限公司

Inventor： 杜锋田 ,  王海波 ,  张强

IPC: C07D309/10 ,  C07H5/00 ,  C07C15/16 ,  A61P9/00 ,  A61P3/10 ,  A61K31/70 ,  A61K31/351

Abstract: 一种抑制钠葡萄糖协同转运蛋白1的化合物及其药学上可接受的盐和立体异构体。该化合物用于药物组合物，以及其制备和使用的方法，包括药物及其组合物在制备用于治疗和改善糖尿病，心脑血管疾病，降低体重，脂肪肝，便秘，代谢相关疾病和肿瘤治疗中应用。

公开(公告)号：WO2021211765A1

公开(公告)日：2021-10-21

申请号：PCT/US2021/027362

申请日：2021-04-14

Applicant: ZYMERGEN INC.

Inventor： KOSINSKI, Szymon ,  LOPEZ, Liza ,  CHAU, Wilson ,  GURAM, Anil ,  LOUIE, Ying Lin

IPC: C07D309/10 ,  B01J23/755 ,  A01N43/16

Abstract: A process for the production of dihydronepetalactone including hydrogenating nepetalactone in the presence of a catalytic metal is provided. The catalytic metal may include nickel. The process may be performed in an aqueous medium.

公开(公告)号：WO2021083209A1

公开(公告)日：2021-05-06

申请号：PCT/CN2020/124381

申请日：2020-10-28

Applicant: ECCOGENE (SHANGHAI) CO., LTD.

Inventor： REN, Zaifang ,  SUN, Xuefeng ,  XU, Qing

IPC: C07D309/04 ,  C07D319/12 ,  C07D309/10 ,  C07D309/08 ,  C07C317/14 ,  C07D307/10 ,  C07D309/12 ,  C07D211/46 ,  C07D309/06 ,  C07D205/04 ,  C07D275/02 ,  C07D207/06 ,  C07D401/04 ,  C07D295/08 ,  A61K31/10 ,  A61P3/00 ,  A61P9/00 ,  A61P29/00

Abstract: Provided are a compound of formula (I') or (I), a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of formula (I') or (I), and a method of treating or preventing a disease in which SSAO plays a role.

公开(公告)号：WO2020050361A1

公开(公告)日：2020-03-12

申请号：PCT/JP2019/034981

申请日：2019-09-05

Applicant: 株式会社トクヤマ

Inventor： 関　雅彦

IPC: C07D309/10 ,  C07B61/00

Abstract: 式（２）で表されるＣ－アリール－ヒドロキシグリコシド誘導体の還元反応が低温で速やかに進行し、式（１）で表されるβ－Ｃ－アリールグリコシド誘導体を高選択的かつ高収率で製造する方法を提供することを目的とし、かかる目的を達成するために、本発明は、式（２）で表されるＣ－アリール－ヒドロキシグリコシド誘導体を、チタン化合物の存在下、シラン化合物と接触させて、式（１）で表されるβ－Ｃ－アリールグリコシド誘導体を製造する工程を含む方法を提供する。

公开(公告)号：WO2019166958A1

公开(公告)日：2019-09-06

申请号：PCT/IB2019/051559

申请日：2019-02-27

Applicant: MYLAN LABORATORIES LTD

Inventor： JAYACHANDRA, Sureshbabu ,  SETHI, Madhuresh ,  KAUSHIK, Vipin, Kumar ,  RAVI, Vijaya, Krishna ,  POTHANI, Jayaram ,  PRATHI, Sivakoteswara, Rao

IPC: C07D309/10

Abstract: Sotagliflozin may be prepared using schemes and intermediates disclosed herein. Sotagliflozin may be incorporated into pharmaceutical dosage forms for treatment of diabetes.

公开(公告)号：WO2019145726A9

公开(公告)日：2019-08-01

申请号：PCT/GB2019/050209

申请日：2019-01-25

Applicant: ENTERPRISE THERAPEUTICS LIMITED

Inventor： COLLINGWOOD, Stephen ,  MCCARTHY, Clive ,  HARGRAVE, Jonathan, David ,  HAY, Duncan, Alexander ,  SCHOFIELD, Thomas, Beauregard ,  ELLAM, Sarah ,  BUXTON, Craig ,  HABGOOD, Matthew ,  INGRAM, Peter ,  MA, Chun Yan ,  NAPIER, Spencer ,  SHAIKH, Abdul ,  SMITH, Matthew ,  STIMSON, Christopher ,  WALKER, Edward

IPC: C07D213/72 ,  C07D309/10 ,  C07C1/00 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61P11/00

Abstract: Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5a , R 5b X 1 , X 2 , Z and Y are as defined herein are positive modulators of the calcium-activated chloride channel (CaCC), TMEM16A. The compounds are useful for treating diseases and conditions affected by modulation of TMEM16A, particularly respiratory diseases and conditions.

公开(公告)号：WO2018193273A1

公开(公告)日：2018-10-25

申请号：PCT/GB2018/051058

申请日：2018-04-23

Applicant: THE UNIVERSITY OF WARWICK

Inventor： CHALLIS, Gregory Leonard ,  JIAN, Xinyun ,  HOBSON, Christian ,  MASSCHELEIN, Joleen Solange Liesbet

IPC: C07C69/732 ,  C07C235/28 ,  A61K31/232 ,  A61P31/00 ,  C12N1/00 ,  C07D309/10

Abstract: The invention provides novel analogues of enacyloxin Ha and their pharmaceutically acceptable salts, metabolites, isomers (e.g. stereoisomers) and prodrugs. Such compounds are effective in the treatment of infections caused by Gram-negative bacteria such as Acinetobacter baumannii . Compounds in accordance with the invention include those of formula (A), and their pharmaceutically acceptable salts, metabolites, isomers (e.g. stereoisomers) and prodrugs: In formula (A): X is 0 or NR x (where R* is either H or C 1-3 alkyl, e.g. CH 3 ); R 1 is a 5- or 6-membered, saturated or unsaturated, carbocyclic ring optionally substituted by one or more substituents, or R 1 is an optionally substituted straight-chained or branched C- 1-6 alkyl group (e.g. C 1-3 alkyl group); R 2 is H, F, CI, Br, I or CH 3 ; R 3 is H or OH; R 8 is a straight-chained or branched C 1-8 alkyl group (e.g. a C 1-6 aikyl group); Y is one of the following groups: (wherein each * denotes the point of attachment of the group to the remainder of the molecule; R 9 is H, F, CI, Br or I; R 4 and R 5 are independently selected from H and OH, or R 4 and R 5 together are =0, preferably R 4 is H and R 5 is OH; R 6 is H, F, CI, Br, I or CH 3 ; R 7 is H and R 7' is OH, or R 7 and R 7' together are =0, preferably R7 is H and R7' is OH); and each— independently represents an optional bond (i.e. each of C 2 -C 3 , C 4 -C 5 , C 6 -C 7 , C 8 -C 9 and C 10 -C 11 are independently either C-C (single) or C=C (double) bonds).