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1. 发明授权

US09133195B2 Quaternary ammonium salt compounds of spirocyclopiperazines, preparation methods and uses thereof 有权
标题翻译：螺环吡嗪的季铵盐化合物，其制备方法和用途
公开(公告)号：US09133195B2
公开(公告)日：2015-09-15
申请号：US12305174
申请日：2007-06-15
申请人： Runtao Li , Qi Sun , Jia Ye , Caiqin Yue , Xin Wang , Zemei Ge , Changling Li , Tieming Cheng
发明人： Runtao Li , Qi Sun , Jia Ye , Caiqin Yue , Xin Wang , Zemei Ge , Changling Li , Tieming Cheng
IPC分类号： A61K31/55 , C07D471/10 , A61K31/438 , A61K31/5386 , C07D498/10 , C07D487/10 , C07D513/10 , C07D519/00
CPC分类号： C07D471/10 , C07D487/10 , C07D498/10 , C07D513/10 , C07D519/00
摘要： Compounds represented by general formula (I), their stereoisomers, tautomers, derivatives, prodrugs or pharmaceutically acceptable salts, and their preparation methods or uses for the manufacture of a medicament of analgesics. In which R1 is selected from H, substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; A is bond, or saturated or unsaturated straight-chain or branched-chain hydrocarbon radical; R2, R3 are each independently hydrogen or methyl, which linked with any position of spirocyclo-structure; n and m are each independently integer between 0-2, do not represent 0 at the same time; B and D are each independently C1-C3 straight-chain or branched-chain alkylene; Y is selected from —CHR4—, O, S, —S(O)—, —SO2—, —NR4— and substituted or unsubstituted phenylene, in which R4 represents H, C1-C6 saturated or unsaturated alkyl, methyl or ethyl substituted by substituted or unsubstituted aryl or heteroaryl; and X− is pharmaceutical acceptable organic or inorganic anion. These compounds can be used as muscarine receptor (M-receptor) and/or nicotine acetylcholine receptor (N-receptor) agonist or antagonist. These compounds have good analgesic effect without side effect such as addiction.
摘要翻译：由通式（I）表示的化合物，其立体异构体，互变异构体，衍生物，前药或药学上可接受的盐，及其制备方法或用途，用于制备镇痛药物。其中R1选自H，取代或未取代的苯基或取代或未取代的杂芳基; A是键或饱和或不饱和的直链或支链烃基; R2，R3各自独立地为氢或甲基，其与任何位置的螺环结构连接; n和m各自独立地为0-2之间的整数，不同时为0; B和D各自独立地为C1-C3直链或支链亚烷基; Y选自-CHR 4 - ，O，S，-S（O） - ， - SO 2 - ， - NR 4 - 和取代或未取代的亚苯基，其中R 4表示H，C 1 -C 6饱和或不饱和烷基，甲基或乙基取代由取代或未取代的芳基或杂芳基取代; X-是药学上可接受的有机或无机阴离子。这些化合物可用作毒蕈碱受体（M-受体）和/或尼古丁乙酰胆碱受体（N-受体）激动剂或拮抗剂。这些化合物具有良好的止痛效果，无副作用，如成瘾。

2. 发明申请

US20130136794A1 HETEROARYL (ALKYL) DITHIOCARBAMATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF 审中-公开
标题翻译：二（ALKYL）二异氰酸酯化合物，其制备方法及其用途
公开(公告)号：US20130136794A1
公开(公告)日：2013-05-30
申请号：US13642298
申请日：2011-04-21
申请人： Runtao Li , Zemei Ge , Jingrong Cui , Xingyl Sun , Zhongqing Wang , Xu Yan
发明人： Runtao Li , Zemei Ge , Jingrong Cui , Xingyl Sun , Zhongqing Wang , Xu Yan
IPC分类号： C07D213/36 , C07D307/52 , C07F5/02 , C07D215/12 , C07D405/04 , C07D498/04 , C07D213/64 , C07D213/75 , C07D263/32 , C07D231/12 , C07D239/26 , C07D277/28 , C07D241/12 , C07D271/10 , C07D239/42 , C07D285/12 , C07D207/335 , C07D417/06
CPC分类号： C07D213/36 , C07D207/335 , C07D213/40 , C07D213/64 , C07D213/75 , C07D215/12 , C07D231/12 , C07D239/26 , C07D239/42 , C07D241/12 , C07D263/32 , C07D271/10 , C07D277/28 , C07D285/12 , C07D307/52 , C07D405/04 , C07D417/02 , C07D417/06 , C07D417/14 , C07D498/04 , C07F5/025
摘要： Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.
摘要翻译：公开了通式（I）表示的杂芳基（烷基）二硫代氨基甲酸酯化合物或其药学上可接受的盐，其制备方法及其用于制备抗肿瘤药物的用途，其中每个所述取代基如说明书所述定义。该化合物是可用作抗肿瘤剂的新的酪氨酸激酶抑制剂，优选用于制备用于治疗乳腺癌，肝癌，非小细胞肺癌，胃癌，结肠癌，白血病或鼻癌的药物。

3. 发明申请

US20120135921A1 TRIPETIDE BORONIC ACID OR BORONIC ESTER, PREPARATIVE METHOD AND USE THEREOF 有权
标题翻译：三硝基硼酸或硼酸酯，其制备方法及其用途
公开(公告)号：US20120135921A1
公开(公告)日：2012-05-31
申请号：US13379142
申请日：2010-05-17
申请人： Runtao Li , Jingrong Cui , Yongqiang Zhu , Shuyang Yao , Zemei Ge , Tieming Cheng
发明人： Runtao Li , Jingrong Cui , Yongqiang Zhu , Shuyang Yao , Zemei Ge , Tieming Cheng
IPC分类号： A61K38/06 , A61P35/00 , A61P21/00 , A61P3/10 , A61P35/02 , C07K5/08 , A61P25/28
CPC分类号： A61K38/06 , A61K31/69 , C07F5/025 , C07K5/08 , C07K5/0808 , C07K5/0812 , C07K5/0821
摘要： The present invention discloses proteasome inhibitors of tripeptide boronic acids or boronic esters represented by Formula (I), preparative method and use thereof. The proteasome inhibitors are therapeutical agents for treating malignant tumor, various nervous system degenerative diseases, muscle cachexia or diabetes, wherein the malignant tumor is leukemia, gastric cancer, hepatocarcinoma or nasopharyngeal carcinoma.
摘要翻译：本发明公开了由式（I）表示的三肽硼酸或硼酸酯的蛋白酶体抑制剂，其制备方法和用途。蛋白酶体抑制剂是治疗恶性肿瘤，各种神经系统变性疾病，肌肉恶病质或糖尿病的治疗剂，其中恶性肿瘤是白血病，胃癌，肝癌或鼻咽癌。

4. 发明授权

US09421237B2 Tripeptide boronic acid or boronic ester, preparative method and use thereof 有权
标题翻译：三肽硼酸或硼酸酯，制备方法及其用途
公开(公告)号：US09421237B2
公开(公告)日：2016-08-23
申请号：US13379142
申请日：2010-05-17
申请人： Runtao Li , Jingrong Cui , Yongqiang Zhu , Shuyang Yao , Zemei Ge , Tieming Cheng
发明人： Runtao Li , Jingrong Cui , Yongqiang Zhu , Shuyang Yao , Zemei Ge , Tieming Cheng
IPC分类号： C07K5/08 , C07F5/02 , C07F5/04 , A61K31/69 , A61K38/06 , A61P43/00 , C07K5/083 , C07K5/087 , C07K5/097
CPC分类号： A61K38/06 , A61K31/69 , C07F5/025 , C07K5/08 , C07K5/0808 , C07K5/0812 , C07K5/0821
摘要： The present invention discloses proteasome inhibitors of tripeptide boronic acids or boronic esters represented by Formula (I), preparative method and use thereof. The proteasome inhibitors are therapeutical agents for treating malignant tumor, various nervous system degenerative diseases, muscle cachexia or diabetes, wherein the malignant tumor is leukemia, gastric cancer, hepatocarcinoma or nasopharyngeal carcinoma.
摘要翻译：本发明公开了由式（I）表示的三肽硼酸或硼酸酯的蛋白酶体抑制剂，其制备方法和用途。蛋白酶体抑制剂是治疗恶性肿瘤，各种神经系统变性疾病，肌肉恶病质或糖尿病的治疗剂，其中恶性肿瘤是白血病，胃癌，肝癌或鼻咽癌。

5. 发明申请

US20090325929A1 QUATERNARY AMMONIUM SALT COMPOUNDS OF SPIROCYCLOPIPERAZINES, PREPARATION METHODS AND USES THEREOF 有权
标题翻译：螺环磷脂的季铵盐化合物，其制备方法及其用途
公开(公告)号：US20090325929A1
公开(公告)日：2009-12-31
申请号：US12305174
申请日：2007-06-15
申请人： Runtao Li , Qi Sun , Jia Ye , Caiqin Yue , Xin Wang , Zemei Ge , Changling Li , Tieming Cheng
发明人： Runtao Li , Qi Sun , Jia Ye , Caiqin Yue , Xin Wang , Zemei Ge , Changling Li , Tieming Cheng
IPC分类号： A61K31/55 , C07D471/10 , A61K31/438 , A61K31/5386 , C07D498/10 , C07D487/10
CPC分类号： C07D471/10 , C07D487/10 , C07D498/10 , C07D513/10 , C07D519/00
摘要： Compounds represented by general formula (I), their stereoisomers, tautomers, derivatives, prodrugs or pharmaceutically acceptable salts, and their preparation methods or uses for the manufacture of a medicament of analgesics. In which R1 is selected from H, substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; A is bond, or saturated or unsaturated straight-chain or branched-chain hydrocarbon radical; R2, R3 are each independently hydrogen or methyl, which linked with any position of spirocyclo-structure; n and m are each independently integer between 0-2, do not represent 0 at the same time; B and D are each independently C1-C3 straight-chain or branched-chain alkylene; Y is selected from —CHR4—, O, S, —S(O)—, —SO2—, —NR4— and substituted or unsubstituted phenylene, in which R4 represents H, C1-C6 saturated or unsaturated alkyl, methyl or ethyl substituted by substituted or unsubstituted aryl or heteroaryl; and X− is pharmaceutical acceptable organic or inorganic anion. These compounds can be used as muscarine receptor (M-receptor) and/or nicotine acetylcholine receptor (N-receptor) agonist or antagonist. These compounds have good analgesic effect without side effect such as addiction.
摘要翻译：由通式（I）表示的化合物，其立体异构体，互变异构体，衍生物，前药或药学上可接受的盐，及其制备方法或用途，用于制备镇痛药物。其中R1选自H，取代或未取代的苯基或取代或未取代的杂芳基; A是键或饱和或不饱和的直链或支链烃基; R2，R3各自独立地为氢或甲基，其与螺环结构的任何位置连接; n和m各自独立地为0-2之间的整数，不同时为0; B和D各自独立地为C1-C3直链或支链亚烷基; Y选自-CHR 4 - ，O，S，-S（O） - ， - SO 2 - ， - NR 4 - 和取代或未取代的亚苯基，其中R 4表示H，C 1 -C 6饱和或不饱和烷基，甲基或乙基取代由取代或未取代的芳基或杂芳基取代; X-是药学上可接受的有机或无机阴离子。这些化合物可用作毒蕈碱受体（M-受体）和/或尼古丁乙酰胆碱受体（N-受体）激动剂或拮抗剂。这些化合物具有良好的止痛效果，无副作用，如成瘾。

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