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1. 发明申请

WO2010045251A3 SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译： SPIRO-OXINDOLE化合物及其作为治疗剂的用途
公开(公告)号：WO2010045251A3
公开(公告)日：2010-11-18
申请号：PCT/US2009060537
申请日：2009-10-13
申请人： XENON PHARMACEUTICALS INC , CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FRASER LAUREN , FU JIANMIN , LANGILLE JONATHAN , LIU SHIFENG , SUN JIANYU , SUN SHAOYI , SVIRIDOV SERGUEI , WOOD MARK , ZENOVA ALLA , JIA QI , CADIEUX JEAN-JACQUES , GAUTHIER SIMON J , DOUGLAS AMY FRANCES , HSIEH TOM , CHAKKA NAGASREE , CIKOJEVIC ZORAN
发明人： CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FRASER LAUREN , FU JIANMIN , LANGILLE JONATHAN , LIU SHIFENG , SUN JIANYU , SUN SHAOYI , SVIRIDOV SERGUEI , WOOD MARK , ZENOVA ALLA , JIA QI , CADIEUX JEAN-JACQUES , GAUTHIER SIMON J , DOUGLAS AMY FRANCES , HSIEH TOM , CHAKKA NAGASREE , CIKOJEVIC ZORAN
IPC分类号： C07D491/20 , A61K31/407 , A61P25/00 , C07D491/10 , C07D495/20 , C07D498/20 , C07D513/20
CPC分类号： C07D513/22 , C07D491/10 , C07D491/107 , C07D491/20 , C07D491/22 , C07D495/20 , C07D498/20 , C07D513/20 , C07D519/00
摘要： This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers. tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
摘要翻译：本发明涉及作为立体异构体对映异构体的螺 - 羟吲哚化合物。互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。

2. 发明申请

WO2008046087A3 SPIRO COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS 审中-公开
标题翻译： SPIRO化合物及其作为治疗剂的用途
公开(公告)号：WO2008046087A3
公开(公告)日：2008-11-27
申请号：PCT/US2007081323
申请日：2007-10-12
申请人： XENON PHARMACEUTICALS INC , CHOWDHURY SULTAN , FU JIANMIN , KAMBOJ RAJENDER , LIU SHIFENG , JIA QI , RAINA VANDNA , SUN JIANYU
发明人： CHOWDHURY SULTAN , FU JIANMIN , KAMBOJ RAJENDER , LIU SHIFENG , JIA QI , RAINA VANDNA , SUN JIANYU
IPC分类号： A61K31/404 , A61K31/425 , A61K31/438 , A61P1/00 , A61P3/06 , A61P9/00 , A61P11/00 , A61P25/00 , C07D493/10 , C07D493/20 , C07D493/22
CPC分类号： A61K31/425 , A61K31/404 , A61K31/438 , C07D491/107 , C07D491/20 , C07D493/20
摘要： This invention is directed to spiro-benzoisothiazole derivatives of formula (I), wherein j, k, m, q, Z, Q, R1, R2 and R3 are each as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
摘要翻译：本发明涉及式（I）的螺 - 苯并异噻唑衍生物，其中j，k，m，q，Z，Q，R 1，R 2和R 3各自如本文所定义，为其立体异构体，对映体，互变异构体或其混合物 ; 或其药学上可接受的盐，溶剂合物或前药，其可用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。还公开了包含化合物的药物组合物以及制备和使用化合物的方法。

3. 发明专利

JP2014132025A HETEROCYCLIC INHIBITORS OF STEAROYL-CoA DESATURASE 有权
标题翻译：硬脂酸脱乙酰壳多糖的杂环抑制剂
公开(公告)号：JP2014132025A
公开(公告)日：2014-07-17
申请号：JP2014056951
申请日：2014-03-19
申请人： Novartis Ag , ノバルティスアーゲー , Xenon Pharmaceuticals Inc , ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc.
发明人： SULTAN CHOWDHURY , NATALIE DALES , JULIA FONAREV , FU JIANMIN , DUANJIE HOU , JIA QI , VISHNUMURTHY KODUMURU , NATALIA POKROVSKAIA , SHAOYI SUN , ZHANG ZAIHUI
IPC分类号： C07D417/04 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P17/00 , A61P43/00 , C07D417/14 , C07D471/04
CPC分类号： C07D417/04 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide inhibitors of stearoyl-CoA desaturase, for use in treating and/or preventing various human diseases, including diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, dermatological disorders and the like.SOLUTION: The present invention provides thiazole-based compound heterocyclic inhibitors represented by the formula specified in the figure.
摘要翻译：要解决的问题：提供用于治疗和/或预防各种人类疾病的硬脂酰CoA去饱和酶抑制剂，包括与脂质水平升高相关的疾病，心血管疾病，糖尿病，肥胖症，代谢综合征，皮肤病学疾病等。解决方案：本发明提供了由图中规定的式所表示的噻唑类化合物杂环抑制剂。

4. 发明公开

KR20180008761A 치환된 벤즈아미드 및 이의 이용 방법 审中-公开
标题翻译：取代的苯甲酰胺及其使用方法
公开(公告)号：KR20180008761A
公开(公告)日：2018-01-24
申请号：KR20177036470
申请日：2016-05-20
申请人： GENENTECH INC , XENON PHARMACEUTICALS INC
发明人： CHOWDHURY SULTAN , DEHNHARDT CHRISTOPH MARTIN , HASAN ABID , HEMEON IVAN WILLIAM , JIA QI , LI JUN , LIU ZHIGUO , ORTWINE DANIEL F , SAFINA BRIAN , SUTHERLIN DANIEL , SUN SHAOYI , WHITE ANDREW D , GONG WEI , ZENOVA ALLA YUREVNA , ZHU JIUXIANG
IPC分类号： C07D211/22 , A61K31/445 , A61P25/00 , A61P29/00 , C07D211/34 , C07D211/38 , C07D211/48 , C07D221/20 , C07D401/04 , C07D401/08 , C07D405/08
CPC分类号： C07D211/22 , C07D211/34 , C07D211/38 , C07D211/42 , C07D211/48 , C07D211/62 , C07D221/20 , C07D401/04 , C07D401/08 , C07D401/12 , C07D405/08
摘要： 본발명은, 나트륨채널-매개질환또는병태, 예컨대통증, 뿐만아니라나트륨채널의매개와연관된기타질환및 병태를치료하는데유용한나트륨채널 (예컨대, NaV1.7) 억제제로서의활성을갖는화합물및 상기화합물을함유하는조성물및 상기화합물및 조성물을사용하기위한방법을제공한다.
摘要翻译：本发明的钠通道介导的疾病或病症，例如疼痛，钠通道在治疗与钠通道的调停以及相关的其它疾病和病症的（如G.，NaV1.7）的化合物和具有活性的化合物作为抑制剂是有用的，以及使用这些化合物和组合物的方法。

5. 发明专利

ES2384506T3 1-(3-Metil-2,4-dimetoxifenil)-3-(2',4'-dihidroxifenil)-propano como un potente inhibidor de tirosinasa 未知
公开(公告)号：ES2384506T3
公开(公告)日：2012-07-06
申请号：ES05762186
申请日：2005-05-27
申请人： UNIGEN PHARMACEUTICALS INC , JIA QI , ZHAO JI FU , UNIGEN INC , JIA QI , ZHAO JI FU
发明人： JIA QI , ZHAO JI-FU
IPC分类号： A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , A61P17/00 , A61P35/00 , C07C39/15 , C07C39/367 , C07C43/23 , C07C45/67 , C07C49/835 , C07C215/74 , C07D233/02 , C07D321/12 , C07D323/00
摘要： El compuesto 1-(3-metil-2,4-dimetoxifenil)-3-(2',4'-dihidroxifenil)-propano.

6. 发明公开

EP1748767A4 DIARYLALKANES AS POTENT INHIBITORS OF BINUCLEAR ENZYMES 有权转让
标题翻译：二芳基烷烃AS高效抑制剂双核的酶
公开(公告)号：EP1748767A4
公开(公告)日：2008-12-24
申请号：EP05762186
申请日：2005-05-27
申请人： UNIGEN PHARMACEUTICALS INC , JIA QI , ZHAO JI FU
发明人： JIA QI , ZHAO JI-FU
IPC分类号： A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , A61P17/00 , A61P35/00 , C07C39/15 , C07C39/367 , C07C43/23 , C07C45/67 , C07C49/835 , C07C215/74 , C07D233/02 , C07D321/12 , C07D323/00
CPC分类号： A61K8/347 , A61K8/31 , A61K8/4973 , A61K8/97 , A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , A61K2800/782 , A61Q19/02 , C07C39/15 , C07C39/367 , C07C41/26 , C07C41/32 , C07C43/23 , C07C45/673 , C07C49/835 , C07C215/74 , C07D321/12
摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

7. 发明专利

AU2005249493A1 Diarylalkanes as potent inhibitors of binuclear enzymes 未知
公开(公告)号：AU2005249493A1
公开(公告)日：2005-12-15
申请号：AU2005249493
申请日：2005-05-27
申请人： UNIGEN PHARMACEUTICALS INC , JIA QI , ZHAO JI-FU
发明人： ZHAO JI-FU , JIA QI
IPC分类号： A61K31/015 , A61K31/05 , A61K31/704 , C07C39/15 , C07C39/367 , C07C43/23 , C07C45/67 , C07C49/835 , C07C215/74 , C07D321/12
摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

8. 发明专利

HK1095536A1 1-(3-METHYL-2,4-DIMETHOXYPHENYL)-3-(2',4'-DIHYDROXYPHENYL)-PROPANE AS A POTENT TYROSINASE INHIBITOR 未知
公开(公告)号：HK1095536A1
公开(公告)日：2007-06-29
申请号：HK07102730
申请日：2007-03-13
申请人： UNIGEN INC , JIA QI , ZHAO JI FU
发明人： JIA QI , ZHAO JI-FU
IPC分类号： A61K20060101 , A61K31/015 , A61K31/05 , A61K31/704 , A61P20060101 , C07C39/15 , C07C39/367 , C07C43/23 , C07C45/67 , C07C49/835 , C07C215/74 , C07D20060101 , C07D321/12
摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

9. 发明专利

PL1748767T3 1-(3-metylo-2,4-dimetoksyfenylo)-3-(2',4'-dihydroksyfenylo)-propan jako silny inhibitor tyrozynazy 未知
公开(公告)号：PL1748767T3
公开(公告)日：2012-08-31
申请号：PL05762186
申请日：2005-05-27
申请人： UNIGEN INC , JIA QI , ZHAO JI FU
发明人： JIA QI , ZHAO JI-FU
IPC分类号： A61K31/05 , A61K31/015 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , A61P17/00 , A61P35/00 , C07C39/15 , C07C39/367 , C07C43/23 , C07C45/67 , C07C49/835 , C07C215/74 , C07D233/02 , C07D321/12 , C07D323/00

10. 发明专利

AT538778T 未知
公开(公告)号：AT538778T
公开(公告)日：2012-01-15
申请号：AT05762186
申请日：2005-05-27
申请人： UNIGEN INC , JIA QI , ZHAO JI-FU
发明人： JIA QI , ZHAO JI-FU
IPC分类号： A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , A61P17/00 , A61P35/00 , C07C39/15 , C07C39/367 , C07C43/23 , C07C45/67 , C07C49/835 , C07C215/74 , C07D321/12
摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.

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