公开(公告)号：US09051273B2

公开(公告)日：2015-06-09

申请号：US14373347

申请日：2012-08-25

Applicant: Jiangping Xu ,  Zhongzhen Zhou

Inventor： Jiangping Xu ,  Zhongzhen Zhou

IPC: C07D237/14 ,  C07D237/22 ,  C07D403/04 ,  A61K31/496 ,  A61K31/50 ,  A61K31/501 ,  A61P1/08 ,  A61K31/495 ,  C07D295/096 ,  C07D295/092

CPC classification number: C07D237/14 ,  A61K31/495 ,  A61K31/496 ,  A61K31/50 ,  A61K31/501 ,  C07D237/22 ,  C07D295/092 ,  C07D295/096 ,  C07D403/04

Abstract: Phosphodiesterase 4 inhibitors without vomiting of the present invention are compounds or prodrugs or solvates represented by formula (I) wherein R1 is an independent methoxy, bromine and substituted aryl; X is an optionally substituted six-membered heterocyclic ring; Y is —(CH2)n—, —NH(CH2)n—, and —NH(CH2)n—O—, wherein n is any value among 0, 1, 2 and 3; Z is an optionally substituted aromatic ring or an optionally substituted heteroaromatic ring. Phosphodiesterase 4 inhibitor without vomiting of the present invention are novel biphenyl series PDE4D inhibitors, and can be applied to treat depression and Alzheimer's disease, improve cognitive ability and avoid vomiting.

Abstract translation: 本发明的无呕吐物的磷酸二酯酶4抑制剂是由式（I）表示的化合物或前药或溶剂合物，其中R 1是独立的甲氧基，溴和取代的芳基; X是任选取代的六元杂环; Y是 - （CH 2）n - ， - NH（CH 2）n - 和-NH（CH 2）n -O-，其中n是0,1,2和3中的任何值; Z是任选取代的芳族环或任选取代的杂芳族环。 本发明的磷酸二酯酶抑制剂无呕吐是新型联苯系列PDE4D抑制剂，可用于治疗抑郁和阿尔茨海默病，提高认知能力和避免呕吐。

公开(公告)号：US20140364606A1

公开(公告)日：2014-12-11

申请号：US14373347

申请日：2012-08-25

Applicant: Jiangping Xu ,  Zhongzhen Zhou

Inventor： Jiangping Xu ,  Zhongzhen Zhou

IPC: C07D237/14

CPC classification number: C07D237/14 ,  A61K31/495 ,  A61K31/496 ,  A61K31/50 ,  A61K31/501 ,  C07D237/22 ,  C07D295/092 ,  C07D295/096 ,  C07D403/04

Abstract: Phosphodiesterase 4 inhibitors without vomiting of the present invention are compounds or prodrugs or solvates represented by formula (I) wherein R1 is an independent methoxy, bromine and substituted aryl; X is an optionally substituted six-membered heterocyclic ring; Y is —(CH2)n—, —NH(CH2)n—, and —NH(CH2)n—O—, wherein n is any value among 0, 1, 2 and 3; Z is an optionally substituted aromatic ring or an optionally substituted heteroaromatic ring. Phosphodiesterase 4 inhibitor without vomiting of the present invention are novel biphenyl series PDE4D inhibitors, and can be applied to treat depression and Alzheimer's disease, improve cognitive ability and avoid vomiting.

Abstract translation: 本发明的无呕吐物的磷酸二酯酶4抑制剂是由式（I）表示的化合物或前药或溶剂合物，其中R 1是独立的甲氧基，溴和取代的芳基; X是任选取代的六元杂环; Y是 - （CH 2）n - ， - NH（CH 2）n - 和-NH（CH 2）n -O-，其中n是0,1,2和3中的任何值; Z是任选取代的芳族环或任选取代的杂芳族环。 本发明的磷酸二酯酶抑制剂无呕吐是新型联苯系列PDE4D抑制剂，可用于治疗抑郁和阿尔茨海默病，提高认知能力和避免呕吐。

公开(公告)号：US20080176810A1

公开(公告)日：2008-07-24

申请号：US11720451

申请日：2005-11-14

Applicant: Jinhua Zhao ,  Jiangping Xu ,  Hui Kang ,  Bing Wang ,  Jing Li ,  Hanlin Feng ,  Lin Yu

Inventor： Jinhua Zhao ,  Jiangping Xu ,  Hui Kang ,  Bing Wang ,  Jing Li ,  Hanlin Feng ,  Lin Yu

IPC: A61K31/7028 ,  A61P9/10

CPC classification number: A61K31/7032

Abstract: The present invention provides new use of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside. 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside has efficacies of anti-myocardial ischemia by intravenous injection and/or oral administration. It is advantageous that 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside as anti-myocardial ischemia drug is used to prepare the medicine for treating and/or preventing ischemic heart disease.

Abstract translation: 本发明提供3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷的新用途。 3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷通过静脉注射和/或口服给药具有抗心肌缺血的功效。 使用3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷作为抗心肌缺血药物来制备用于治疗和/或预防缺血性心脏病的药物。