公开(公告)号：WO2022109741A1

公开(公告)日：2022-06-02

申请号：PCT/CA2021/051688

申请日：2021-11-25

Applicant: RISEN (SUZHOU) PHARMA TECH CO., LTD. ,  LU, Jiasheng ,  CHEN, Gang ,  ZHANG, Qiguo ,  KONG, Xianqi ,  CHEN, Dawei ,  HUANG, Chuanhao ,  ZHU, Xingwu ,  ZHANG, Yuhua

Inventor： LU, Jiasheng ,  CHEN, Gang ,  ZHANG, Qiguo ,  KONG, Xianqi ,  CHEN, Dawei ,  HUANG, Chuanhao ,  ZHU, Xingwu ,  ZHANG, Yuhua

IPC: C07H19/20 ,  A61K31/7076 ,  A61P35/00

Abstract: CD73 (also known as ecto-5´-nucleotidase) inhibitor compounds are provided, as well as compositions and uses thereof for treating or preventing CD73-associated or related diseases, disorders and conditions, including cancer- and immune-related disorders. CD73 inhibitor compounds include compounds having the structure set forth in Formula I': (I') and pharmaceutically acceptable esters or salts thereof.

公开(公告)号：WO2009019534A2

公开(公告)日：2009-02-12

申请号：PCT/IB2007004704

申请日：2007-10-12

Applicant: NEURO INTERNATIONAL LTD ,  KONG XIANQI ,  ATFANI MOHAMED ,  BACHAND BENOIT ,  BOUZIDE ABDERRAHIM ,  CIBLAT STEPHANE ,  LEVESQUE SOPHIE ,  MIGNEAULT DAVID ,  VALADE ISABELLE ,  WU XINFU ,  DELORME DANIEL

Inventor： KONG XIANQI ,  ATFANI MOHAMED ,  BACHAND BENOIT ,  BOUZIDE ABDERRAHIM ,  CIBLAT STEPHANE ,  LEVESQUE SOPHIE ,  MIGNEAULT DAVID ,  VALADE ISABELLE ,  WU XINFU ,  DELORME DANIEL

CPC classification number: A61K31/145 ,  A61K47/48023 ,  A61K47/48038 ,  A61K47/48061 ,  A61K47/48092 ,  A61K47/48123 ,  A61K47/48246 ,  A61K47/54 ,  A61K47/542 ,  A61K47/545 ,  A61K47/549 ,  A61K47/554 ,  A61K47/64 ,  C07C309/15 ,  C07C309/18 ,  C07C309/19 ,  C07C309/24 ,  C07D207/16 ,  C07D209/20 ,  C07D217/24 ,  C07D233/64 ,  C07D285/36 ,  C07D285/38 ,  C07D291/02 ,  C07D323/02 ,  C07D333/24 ,  C07H7/02 ,  C07H15/12 ,  C07J9/005 ,  C07K5/06026 ,  C07K5/06052 ,  C07K5/0606 ,  C07K5/06069 ,  C07K5/06086 ,  C07K5/0806 ,  C07K5/081 ,  C12P11/00 ,  C12P13/001 ,  Y02P20/55

Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1 -propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to, the prevention and treatment of Alzheimer's disease.

Abstract translation: 本发明涉及用于在受试者，优选人受试者中递送3-氨基-1-丙磺酸（3APS）的方法，化合物，组合物和载体。 本发明包括在体外或体内产生或产生3APS的化合物。 优选的化合物包括使用3APS的氨基酸前药，包括但不限于预防和治疗阿尔茨海默病。

公开(公告)号：WO2005079780A1

公开(公告)日：2005-09-01

申请号：PCT/IB2004/000617

申请日：2004-01-23

Applicant: NEUROCHEM (INTERNATIONAL) LIMITED ,  KONG, Xianqi ,  WU, Xinfu ,  MIGNEAULT, David

Inventor： KONG, Xianqi ,  WU, Xinfu ,  MIGNEAULT, David

IPC: A61K31/155

CPC classification number: A61K31/155 ,  A61K31/167 ,  A61K31/18 ,  A61K31/4168

Abstract: The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an amyloid-related disease in a subject comprising administering to the subject a therapeutic amount of an amidine compound. Among the compounds for use according to the invention are those according to the following Formula (I), such that, when administered, amyloid fibril formation, neurodegeneration, or cellular toxicity is reduced or inhibited: Formula (I).

Abstract translation: 本发明涉及脒化合物在淀粉样蛋白相关疾病的治疗中的应用。 特别地，本发明涉及治疗或预防受试者中淀粉样蛋白相关疾病的方法，其包括向受试者施用治疗量的脒化合物。 根据本发明使用的化合物是根据下式（I）的化合物，使得当给药时，降低或抑制淀粉样蛋白原纤维形成，神经变性或细胞毒性：式（I）。

公开(公告)号：WO2005000406A3

公开(公告)日：2005-06-23

申请号：PCT/US2004019839

申请日：2004-06-21

Applicant: NEUROCHEM INT LTD ,  KONG XIANQI ,  LU WENSHUO ,  WU XINFU

Inventor： KONG XIANQI ,  LU WENSHUO ,  WU XINFU

IPC: A61K31/185 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P27/00 ,  A61P29/00 ,  C07C309/14 ,  C07C309/26 ,  C07D209/14 ,  C07D213/38 ,  C07D233/24 ,  C07D233/28 ,  C07D239/06 ,  C07D263/10 ,  C07D263/16 ,  C07D265/08 ,  C07D277/10 ,  C07D277/12 ,  C07D279/06 ,  C07D317/58 ,  C07D333/20 ,  C07D333/58

CPC classification number: C07D239/06 ,  A61K31/185 ,  C07C309/14 ,  C07C309/26 ,  C07C2601/14 ,  C07C2602/10 ,  C07D209/14 ,  C07D213/38 ,  C07D233/24 ,  C07D233/28 ,  C07D263/10 ,  C07D263/16 ,  C07D265/08 ,  C07D277/10 ,  C07D277/12 ,  C07D279/06 ,  C07D317/58 ,  C07D333/20 ,  C07D333/58

Abstract: Methods of treating or preventing an amyloid-related disease in a subject by administering to a subject a therapeutic amount of a compound of the invention are described. Also included are methods for inhibiting epileptogenesis in a subject, by administering to a subject an effective amount of an anti-epileptogenic agent. Methods for treating a subject suffering from an epileptogenesis-associated condition, by administering to the subject an effective amount of an anti-epileptogenic agent are also included. Methods for treating convulsions in a subject by administering to the subject an effective amount of a therapeutic amount of a compound of the invention are also described.

Abstract translation: 描述了通过向受试者施用治疗量的本发明化合物来治疗或预防受试者中淀粉样蛋白相关疾病的方法。 还包括通过向受试者施用有效量的抗癫痫发生剂来抑制受试者中癫痫发生的方法。 还包括通过向受试者施用有效量的抗癫痫发生剂来治疗患有癫痫发生相关病症的受试者的方法。 还描述了通过向受试者施用有效量的治疗量的本发明化合物来治疗受试者的抽搐的方法。

公开(公告)号：WO2004113391A3

公开(公告)日：2004-12-29

申请号：PCT/IB2004/002563

申请日：2004-06-21

Applicant: NEUROCHEM (INTERNATIONAL) LIMITED ,  KONG, Xianqi ,  MIGNEAULT, David ,  WU, Xinfu

Inventor： KONG, Xianqi ,  MIGNEAULT, David ,  WU, Xinfu

IPC: C07C303/22

Abstract: The present invention is directed to methods of preparation of sulfonate derivatized compounds, e.g., 3-amino-l-propanesulfonic acid and 1,3-propanedisulfonic acid disodium salt with increased purity, with reduced potential for toxic by-products, and that are pharmaceutically useful, e.g., for the treatment of amyloidosis.

公开(公告)号：WO2021189143A1

公开(公告)日：2021-09-30

申请号：PCT/CA2021/050387

申请日：2021-03-25

Applicant: RISEN (SUZHOU) PHARMA TECH CO., LTD. ,  SHANGHAI JUNSHI BIOSCIENCES CO., LTD. ,  LU, Jiasheng ,  GU, Jiamin ,  JI, Xiang ,  ZHU, Dongqing ,  HE, Xiaolin ,  KONG, Xianqi

Inventor： LU, Jiasheng ,  GU, Jiamin ,  JI, Xiang ,  ZHU, Dongqing ,  HE, Xiaolin ,  KONG, Xianqi

IPC: C07D417/14 ,  A61K51/04 ,  A61P35/00 ,  C07C233/07 ,  C07C233/11 ,  C07C233/26 ,  C07C235/64 ,  C07C237/08 ,  C07D207/16 ,  C07D209/26 ,  C07D209/28 ,  C07D213/56 ,  C07D239/42 ,  C07D241/20 ,  C07D37/81 ,  C07D401/06 ,  C07H19/052 ,  C07K5/10 ,  C12N15/113

Abstract: There are provided isotope-enriched compounds containing stable heavy isotope-enriched amide functional groups for modulating the pharmacokinetic profile, metabolic profile, and/or delivery efficiency of a drug or prodrug, as well as its therapeutic or prophylactic efficacy and/or adverse effects. Use of the isotope-enriched amide-containing drugs and prodrugs for the treatment or prevention of disease states and conditions is also provided. (I)

公开(公告)号：WO2020051686A1

公开(公告)日：2020-03-19

申请号：PCT/CA2019/051268

申请日：2019-09-10

Applicant: RISEN (SUZHOU) PHARMA TECH CO. LTD. ,  LU, Jiasheng ,  GU, Jiamin ,  WU, Dongdong ,  CHEN, Gang ,  SUN, Chengyong ,  JI, Xiang ,  WANG, Lin ,  ZHOU, Feng ,  ZHANG, Xiuchun ,  KONG, Xianqi

Inventor： LU, Jiasheng ,  GU, Jiamin ,  WU, Dongdong ,  CHEN, Gang ,  SUN, Chengyong ,  JI, Xiang ,  WANG, Lin ,  ZHOU, Feng ,  ZHANG, Xiuchun ,  KONG, Xianqi

IPC: C07H19/20 ,  A61K31/7076 ,  A61K39/395 ,  A61K9/00 ,  A61P35/00 ,  C07H19/16

Abstract: CD73 (also known as ecto-5 ' -nucleotidase) inhibitor compounds are provided, as well as compositions and uses thereof for treating or preventing CD73-associated or related diseases, disorders and conditions, including cancer- and immune-related disorders. CD73 inhibitor compounds include compounds having the structure set forth in Formula I and pharmaceutically acceptable esters or salts thereof. (I)

公开(公告)号：WO2006059245A2

公开(公告)日：2006-06-08

申请号：PCT/IB2005/004115

申请日：2005-11-16

Applicant: NEUROCHEM (INTERNATIONAL) LIMITED ,  KONG, Xianqi ,  WU, Xinfu ,  VALADE, Isabelle ,  GERVAIS, Francine

Inventor： KONG, Xianqi ,  WU, Xinfu ,  VALADE, Isabelle ,  GERVAIS, Francine

CPC classification number: C07D401/12 ,  C07D233/84 ,  C07D239/47 ,  C07D239/56 ,  C07D249/12 ,  C07D257/04 ,  C07D271/113 ,  C07D401/04 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing CNS and amyloid associated disease. Also described are methods, compounds, pharmaceutical compositions and kits for detecting, diagnosing, monitoring and treating or preventing CNS and amyloid associated disease.

Abstract translation: 描述了治疗或预防CNS和淀粉样蛋白相关疾病的方法，化合物，药物组合物和试剂盒。 还描述了用于检测，诊断，监测和治疗或预防CNS和淀粉样蛋白相关疾病的方法，化合物，药物组合物和试剂盒。

公开(公告)号：WO2004113277A3

公开(公告)日：2004-12-29

申请号：PCT/IB2004/002337

申请日：2004-06-21

Applicant: NEUROCHEM (INTERNATIONAL) LIMITED ,  QUEEN'S UNIVERSITY AT KINGSTON ,  KONG, Xianqi ,  GERVAIS, Francine ,  SZAREK, Walter, A.

Inventor： KONG, Xianqi ,  GERVAIS, Francine ,  SZAREK, Walter, A.

IPC: C07C309/14

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+ related disease.

公开(公告)号：WO02096937A2

公开(公告)日：2002-12-05

申请号：PCT/CA0200763

申请日：2002-05-29

Applicant: NEUROCHEM INC ,  GERVAIS FRANCINE ,  HEBERT LISE ,  CHALIFOUR ROBERT J ,  KONG XIANQI

Inventor： GERVAIS FRANCINE ,  HEBERT LISE ,  CHALIFOUR ROBERT J ,  KONG XIANQI

IPC: A61K39/00 ,  A61P9/00 ,  A61P25/28 ,  C07K14/47 ,  C07K16/18 ,  C07K14/00

CPC classification number: C07K14/4711 ,  A61K39/0007 ,  A61K2039/505 ,  C07K14/47 ,  C07K16/18 ,  C07K2317/34

Abstract: The present invention relates to a stereochemically based "non-self" antigen vaccine for the prevention and/or treatment of Alzheimer's and other amyloid related diseases. The present invention provides a vaccine for the prevention and treatment of Alzheimer's and other amyloid related diseases, which overcomes the drawbacks associated with using naturally occurring peptides, proteins or immunogens.

Abstract translation: 本发明涉及用于预防和/或治疗阿尔茨海默病和其他淀粉样蛋白相关疾病的基于立体化学的“非自身”抗原疫苗。 本发明提供了用于预防和治疗阿尔茨海默病和其他淀粉样蛋白相关疾病的疫苗，其克服了与使用天然存在的肽，蛋白质或免疫原相关的缺点。