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1. 发明申请

US20140329800A1 TRI-HETEROCYCLIC DERIVATIVES, PREPARATION PROCESS AND USES THEREOF 有权
标题翻译：三杂环衍生物，制备方法及其用途
公开(公告)号：US20140329800A1
公开(公告)日：2014-11-06
申请号：US14356982
申请日：2012-12-13
申请人： SHANGHAI DE NOVO PHARMATECH CO LTD.
发明人： Daxin Gao , Heping Yang , Yajun Yu
IPC分类号： C07D513/04 , C07D513/14
CPC分类号： C07D513/04 , A61K31/429 , C07D513/14
摘要： The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
摘要翻译：本发明涉及三杂环衍生物，其制备方法和用途，具体涉及式（I）的三杂环衍生物或其药学上可接受的盐，其制备方法，还涉及药学上可接受的组合物，其包含式（I）化合物或其药学上可接受的盐及其作为激酶抑制剂的药物用途。

2. 发明公开

US20240327425A1 KRAS G12D INHIBITOR AND USE THEREOF 审中-公开
公开(公告)号：US20240327425A1
公开(公告)日：2024-10-03
申请号：US18575206
申请日：2022-06-30
申请人： SHANGHAI DE NOVO PHARMATECH CO., LTD.
发明人： Feng WANG , Jinglu WANG , Chuanxiu ZHANG , Feng Zhou , Man ZHANG , Daxin GAO
IPC分类号： C07D498/22 , A61K31/553 , A61P35/00 , C07D519/00
CPC分类号： C07D498/22 , A61K31/553 , A61P35/00 , C07D519/00
摘要： A KRAS inhibitor compound represented by formula (I), and an isomer or a pharmaceutically acceptable salt thereof. The compound represented by formula (I) and the composition thereof can effectively treat diseases related to KRAS mutation.

3. 发明公开

US20240299572A1 NITROGEN-CONTAINING COMPOUND, CONJUGATE CONTAINING SAID COMPOUND, AND APPLICATION THEREOF 审中-公开
公开(公告)号：US20240299572A1
公开(公告)日：2024-09-12
申请号：US18560986
申请日：2022-05-19
申请人： SHANGHAI DE NOVO PHARMATECH CO., LTD.
发明人： Zhaolong TONG , Man ZHANG , Heping YANG , Xiaohuan LIU , Longsheng WANG , Jicheng REN , Daxin GAO
IPC分类号： A61K47/68 , A61K47/54 , A61K47/65 , A61P35/00 , C07D223/16 , C07D401/12 , C07D471/04 , C07D519/00
CPC分类号： A61K47/6803 , A61K47/545 , A61K47/65 , A61K47/6851 , A61P35/00 , C07D223/16 , C07D401/12 , C07D471/04 , C07D519/00
摘要： The present application relates to a nitrogen-containing compound, a conjugate containing said compound, and an application thereof. Specifically, the present application provides a compound represented by formula (I), a solvate thereof, a pharmaceutically acceptable salt thereof, or a solvate of a pharmaceutically acceptable salt thereof. The nitrogen-containing compound has a good regulating effect on TLR8 and can effectively treat, alleviate, and/or prevent various diseases caused by immunosuppression, such as a cancer or a viral infection.

4. 发明公开

US20240025899A1 TRIHETEROCYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF 审中-公开
公开(公告)号：US20240025899A1
公开(公告)日：2024-01-25
申请号：US18247742
申请日：2021-10-15
申请人： SHANGHAI DE NOVO PHARMATECH CO., LTD.
发明人： Xiaohui LIU , Fengtao LIU , Daxin GAO
IPC分类号： C07D471/14 , A61P35/00
CPC分类号： C07D471/14 , A61P35/00
摘要： A triheterocyclic derivative, and a pharmaceutical composition and an application thereof. The triheterocyclic derivative (I), and a stereoisomer or a pharmacologically acceptable salt thereof have the following structure. The triheterocyclic derivative has good effects of inhibiting ATR levels in vivo and in vitro, and furthermore, the triheterocyclic derivative can also effectively treat diseases caused by abnormal ATR levels, such as cancers.

5. 发明申请

US20200377520A1 MACROCYCLIC DERIVATIVE OF PYRAZOL[3,4-D]PYRIMIDIN-3-ONE, PHARMACEUTICAL COMPOSITION AND USE THEREOF 审中-公开
公开(公告)号：US20200377520A1
公开(公告)日：2020-12-03
申请号：US16496534
申请日：2018-03-21
申请人： SHANGHAI DE NOVO PHARMATECH CO., LTD.
发明人： Zhiming ZHAO , Daxin GAO , Shoujun CHEN , Zhiheng WU
IPC分类号： C07D498/22 , C07D519/00
摘要： A macrocyclic derivative of pyrazol[3,4-d]pyrimidin-3-one as represented by formula (I) and/or a pharmaceutically acceptable salt thereof, a composition comprising the compound as represented by formula (I) and/or a pharmaceutically acceptable salt thereof, a preparation method therefor, use thereof as a Wee1 inhibitor and use thereof as a sensitizer in chemotherapy or a radiotherapy of cancers. The macrocyclic derivative of pyrazol[3,4-d]pyrimidin-3-one can effectively inhibit Wee1 and relating signaling pathways, having good therapeutic and relieving effects on cancers.

6. 发明授权

US10669252B2 Benzazepine derivative, preparation method, pharmaceutical composition and use thereof 审中-公开
公开(公告)号：US10669252B2
公开(公告)日：2020-06-02
申请号：US16098972
申请日：2017-05-04
申请人： SHANGHAI DE NOVO PHARMATECH CO., LTD.
发明人： Daxin Gao , Yuxun Wang , Shoujun Chen , Heping Yang
IPC分类号： C07D401/04 , C07D495/04 , C07D471/04 , C07D413/04 , C07D403/04 , C07D403/06 , C07D417/14 , C07D403/14 , C07D413/14 , C07D401/14 , C07F9/6558 , A61K31/55 , C07D491/048
摘要： Disclosed are a benzazepine derivative, a preparation method, a pharmaceutical composition and the use thereof. A compound as shown in formula (I) of the present invention, and an isomer, a prodrug, a stable isotope derivative or a pharmaceutically acceptable salt thereof have the following structure. The benzazepine derivative of the present invention has a good regulation effect on the TLR family and the related signaling pathway, and in particular, has a good regulation effect on TLR8, can effectively treat, relieve and/or prevent various diseases mediated by TLR family and the TLR-related signaling pathway, and in particular, can effectively treat, relieve and/or prevent various diseases mediated by TLR8, such as cancers, autoimmune diseases, infections, inflammations, transplantation rejections, graft-versus-host diseases, etc.

7. 发明申请

US20170037038A1 C- ARYL GLYCOSID DERIVATIVES, PHARMACEUTICAL COMPOSITION, PREPARATION PROCESS AND USES THEREOF 有权
标题翻译： C- ARYL GLYCOSID衍生物，药物组合物，制备方法及其用途
公开(公告)号：US20170037038A1
公开(公告)日：2017-02-09
申请号：US15304493
申请日：2015-04-01
申请人： SHANGHAI DE NOVO PHARMATECH CO. LTD.
发明人： Daxin GAO , Heping YANG , Pei WANG
IPC分类号： C07D407/12 , A61K31/351 , A61K45/06
CPC分类号： C07D407/12 , A61K31/351 , A61K45/06 , C07H7/04 , Y02P20/55
摘要： This invention relates to a kind of C-aryl glycoside derivatives, its pharmaceutical compositions, preparation methods, and uses thereof. The preparation method comprises: method 1: in a solvent, deprotecting the acetyl protecting groups of compound 1-f in the presence of a base; method 2: 1) compound 2-g reacts with via Mitsunobu reaction; 2) deprotecting the acetyl protecting groups of compound 2-f obtained from step 1; method 3: 1) compound 2-g reacts with via nucleophilic substitution reaction; 2) deprotecting the acetyl protecting groups of compound 3-f obtained from step 1. The pharmaceutical composition comprises a kind of C-aryl glycoside derivatives; it's pharmaceutically acceptable salts and/or prodrugs thereof and excipient thereof. This invention further relates to a kind of C-aryl glycoside derivatives, it's pharmaceutically acceptable salts or pharmaceutical compositions thereof for the use in preparation of a SGLT inhibitor. The C-aryl glycoside derivatives of this invention provides a new direction for the study of SGLT inhibitors.
摘要翻译：本发明涉及一种C-芳基糖苷衍生物，其药物组合物，制备方法和用途。制备方法包括：方法1：在溶剂中，在碱的存在下脱保护化合物1-f的乙酰基保护基; 方法2：1）化合物2-g通过Mitsunobu反应反应; 2）从步骤1获得的化合物2-f的乙酰基保护基脱保护; 方法3：1）化合物2-g通过亲核取代反应反应; 2）使从步骤1获得的化合物3-f的乙酰基保护基脱保护。药物组合物包含一种C-芳基糖苷衍生物; 其药学上可接受的盐和/或其前药和赋形剂。本发明还涉及一种C-芳基糖苷衍生物，其用于制备SGLT抑制剂的药学上可接受的盐或其药物组合物。本发明的C-芳基糖苷衍生物为研究SGLT抑制剂提供了新的方向。

8. 发明申请

US20190152941A1 BENZAZEPINE DERIVATIVE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF 审中-公开
公开(公告)号：US20190152941A1
公开(公告)日：2019-05-23
申请号：US16098972
申请日：2017-05-04
申请人： SHANGHAI DE NOVO PHARMATECH CO., LTD.
发明人： Daxin GAO , Yuxun WANG , Shoujun CHEN , Heping YANG
IPC分类号： C07D401/04 , C07D495/04 , C07D471/04 , C07F9/6558 , C07D413/04 , C07D403/04 , C07D403/06 , C07D417/14 , C07D403/14 , C07D413/14 , C07D401/14 , A61K31/55
摘要： Disclosed are a benzazepine derivative, a preparation method, a pharmaceutical composition and the use thereof. A compound as shown in formula (I) of the present invention, and an isomer, a prodrug, a stable isotope derivative or a pharmaceutically acceptable salt thereof have the following structure. The benzazepine derivative of the present invention has a good regulation effect on the TLR family and the related signaling pathway, and in particular, has a good regulation effect on TLR8, can effectively treat, relieve and/or prevent various diseases mediated by TLR family and the TLR-related signaling pathway, and in particular, can effectively treat, relieve and/or prevent various diseases mediated by TLR8, such as cancers, autoimmune diseases, infections, inflammations, transplantation rejections, graft-versus-host diseases, etc.

9. 发明授权

US09914724B2 C-aryl glycosid derivatives, pharmaceutical composition, preparation process and uses thereof 有权
公开(公告)号：US09914724B2
公开(公告)日：2018-03-13
申请号：US15304493
申请日：2015-04-01
申请人： SHANGHAI DE NOVO PHARMATECH CO. LTD.
发明人： Daxin Gao , Heping Yang , Pei Wang
IPC分类号： C07H7/04 , C07D407/12 , A61K31/351 , A61K45/06
CPC分类号： C07D407/12 , A61K31/351 , A61K45/06 , C07H7/04 , Y02P20/55
摘要： This invention relates to a kind of C- aryl glycoside derivatives, its pharmaceutical compositions, preparation methods, and uses thereof. The preparation method comprises: method 1: in a solvent, deprotecting the acetyl protecting groups of compound 1-f in the presence of a base; method 2: 1) compound 2-g reacts with via Mitsunobu reaction; 2) deprotecting the acetyl protecting groups of compound 2-f obtained from step 1; method 3: 1) compound 2-g reacts with via nucleophilic substitution reaction; 2) deprotecting the acetyl protecting groups of compound 3-f obtained from step 1. The pharmaceutical composition comprises a kind of C- aryl glycoside derivatives; it's pharmaceutically acceptable salts and/or prodrugs thereof and excipient thereof. This invention relates to a kind of C- aryl glycoside derivatives, it's pharmaceutically acceptable salts or compositions thereof for preparing a SGLT inhibitor. The C- aryl glycoside derivatives of this invention provides a new direction for SGLT inhibitors.

10. 发明授权

US09216997B2 Tri-heterocyclic derivatives, preparation process and uses thereof 有权
标题翻译：三杂环衍生物，其制备方法和用途
公开(公告)号：US09216997B2
公开(公告)日：2015-12-22
申请号：US14356982
申请日：2012-12-13
申请人： SHANGHAI DE NOVO PHARMATECH CO LTD.
发明人： Daxin Gao , Heping Yang , Yajun Yu
IPC分类号： C07D513/04 , C07D513/14 , A61K31/429
CPC分类号： C07D513/04 , A61K31/429 , C07D513/14
摘要： The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
摘要翻译：本发明涉及三杂环衍生物，其制备方法和用途，具体涉及式（I）的三杂环衍生物或其药学上可接受的盐，其制备方法，还涉及药学上可接受的组合物，其包含式（I）化合物或其药学上可接受的盐及其作为激酶抑制剂的药物用途。

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