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1. 发明申请

WO0177080A3 PYRAZOLE COMPOUNDS HAVING ANTI PROLIFERATIVE ACTIVITY 审中-公开
标题翻译：具有抗增殖活性的吡咯化合物
公开(公告)号：WO0177080A3
公开(公告)日：2002-02-28
申请号：PCT/CA0100089
申请日：2001-01-26
申请人： KINETEK PHARMACEUTICALS INC , ZHANG ZAIHUI , YAN JUN , LEUNG DANNY , COSTELLO PENELOPE C , SANGHERA JASBINDER , DAYNARD TIMOTHY SCOTT , WANG SHISEN , CHAFEEV MIKHAIL
发明人： ZHANG ZAIHUI , YAN JUN , LEUNG DANNY , COSTELLO PENELOPE C , SANGHERA JASBINDER , DAYNARD TIMOTHY SCOTT , WANG SHISEN , CHAFEEV MIKHAIL
IPC分类号： A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/4178 , A61K31/427 , A61K31/454 , A61K31/53 , A61K31/5377 , C07D231/38 , C07D231/46 , C07D231/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , A61P35/00
CPC分类号： C07D231/38 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/4178 , A61K31/427 , A61K31/454 , A61K31/53 , A61K31/5377 , C07D231/46 , C07D231/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.
摘要翻译：提供药物组合物和化合物。本发明化合物具有抗增殖活性，可能促进缺乏细胞周期和死亡正常调节的细胞凋亡。在本发明的一个实施方案中，提供了与生理上可接受的载体组合的化合物的制剂。药物制剂可用于治疗过度增殖性疾病，该疾病包括肿瘤生长，淋巴组织增生性疾病，血管生成。本发明的化合物是取代的吡唑和吡唑啉。

2. 发明申请

WO2004011460A3 PYRAZOLYLBENZOTHIAZOLE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：吡唑并苯并噻唑衍生物及其作为治疗剂的用途
公开(公告)号：WO2004011460A3
公开(公告)日：2004-05-06
申请号：PCT/CA0301078
申请日：2003-07-23
申请人： KINETEK PHARMACEUTICALS INC , ZHANG ZAIHUI , DAYNARD TIMOTHY S , WANG SHISEN , DU XINYAO , CHOPIUK GREGORY B , YAN JUN , CHEN JIANXIN , SVIRIDOV SERGUEI V
发明人： ZHANG ZAIHUI , DAYNARD TIMOTHY S , WANG SHISEN , DU XINYAO , CHOPIUK GREGORY B , YAN JUN , CHEN JIANXIN , SVIRIDOV SERGUEI V
IPC分类号： A61K31/428 , A61P35/00 , C07D413/04 , C07D417/04 , C07D417/14 , C07D513/04 , C07D521/00
CPC分类号： C07D417/04 , A61K31/428 , A61K31/655 , A61K31/675 , C07D231/12 , C07D233/56 , C07D249/08 , C07D413/04 , C07D417/14 , C07D513/04 , A61K2300/00
摘要： A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula (I): wherein R , R and R at each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and R is selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl is described as useful in treatment of disorders associated with dysregulation of cell proliferation.
摘要翻译：包含药学上可接受的赋形剂和式（I）化合物的药物组合物：其中R 1，R 2和R 3在每次出现时独立地选自氨基，氨基亚磺酰基，氨基磺酰基，芳基，叠氮基，卤素，杂烷基，杂芳基，肼基，烃基，氢，羟基，硝基，亚硝基，磷酸根，次膦酸酯，膦酸酯，鏻，硫代磷酸酯，磷酰基，氨磺酰，硫酸根，亚磺酸，亚磺酰氨基，磺酸酯，磺酸，磺酰基，亚砜基，硫醇，硫脲基和脲基，R 4选自氢，杂烷基，杂芳基和烃基可用于治疗与细胞增殖失调相关的病症。

3. 发明申请

WO2006086445A8 COMBINATION THERAPY 审中-公开
标题翻译：联合治疗
公开(公告)号：WO2006086445A8
公开(公告)日：2006-12-07
申请号：PCT/US2006004383
申请日：2006-02-08
申请人： XENON PHARMACEUTICALS INC , KAMBOJ RAJENDER , WINTHER MICHAEL , FRASER ROBERT , CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FU JIAN-MIN , HOU DUANJIE , LIU SHIFENG , RAINA VANDNA , SEID BAGHERZADEH MEHRAN , SVIRIDOV SERGUEI , SADALAPURE KASHINATH , SUN SHAOYI , KODUMURU VISHNUMURTHY , CHAKKA NAGASREE , ZHANG ZAIHUI , ABREO MELWYN , KONDRATENKO MIKHAIL A , HARVEY DANIEL F , HUDSON CINDY J , LI WENBAO , TU CHI , SUN SENGEN , HOLLADAY MARK W , GSCHWEND HEINZ W
发明人： KAMBOJ RAJENDER , WINTHER MICHAEL , FRASER ROBERT , CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FU JIAN-MIN , HOU DUANJIE , LIU SHIFENG , RAINA VANDNA , SEID BAGHERZADEH MEHRAN , SVIRIDOV SERGUEI , SADALAPURE KASHINATH , SUN SHAOYI , KODUMURU VISHNUMURTHY , CHAKKA NAGASREE , ZHANG ZAIHUI , ABREO MELWYN , KONDRATENKO MIKHAIL A , HARVEY DANIEL F , HUDSON CINDY J , LI WENBAO , TU CHI , SUN SENGEN , HOLLADAY MARK W , GSCHWEND HEINZ W
IPC分类号： A61K45/00 , A61P3/04
CPC分类号： A61K31/64 , A61K31/00 , A61K31/4439 , A61K38/28 , A61K45/06 , A61K2300/00
摘要： This invention is directed to the use of SCD-1 inhibitors of the formula (I): where x, y, V, W, G, J, L, M, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, in combination with other drug therapies to treat adverse weight gain.
摘要翻译：本发明涉及式（I）的SCD-1抑制剂的用途：其中x，y，V，W，G，J，L，M，R2，R3，R5，R5a，R6，R6a，R7，本文定义R7a，R8和R8a与其他药物疗法组合以治疗不利的体重增加。

4. 发明申请

WO0202562A3 HETEROPOLYCYCLIC INHIBITORS 审中-公开
标题翻译：杂环化合物抑制剂
公开(公告)号：WO0202562A3
公开(公告)日：2002-05-02
申请号：PCT/IB0101519
申请日：2001-07-06
申请人： KINETEK PHARMACEUTICALS INC , ZHANG ZAIHUI , XINYAO DU , CHOPIUK GREG
发明人： ZHANG ZAIHUI , DU XINYAO , CHOPIUK GREG
IPC分类号： A61P17/06 , A61P35/00 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D487/04 , C07D513/04
摘要： A compound of formula (I) wherein, independently at each occurence, v, w, and x are selected from C, N, O, and S, with H substitition as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R , R , R and R are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R , R , R and R may join together to form a 5, 6 or 7-membered carbocyclic or heterocyclic ring, with the proviso that each of R , R , R , and R is not simultaneously hydrogen. Pharmaceutical compositions of said compounds, and methods of use in the treatment of biological conditions including cellular hyperproliferation, are disclosed.
摘要翻译：式（I）的化合物，其中在每次出现时，v，w和x独立地选自C，N，O和S，根据需要进行H取代以实现开价值位点; y和z选自N和C，H取代作为开放的价键位点，条件是w，v，x，y和z中的每一个不同时为C; 由v，w，x，y和z形成的环可以是饱和或不饱和的; R 1，R 2，R 3和R 4选自氢，烷基，芳基，烷芳基，芳烷基，杂烷基和杂芳基; 其中R 1，R 2，R 3和R 4中的任何相邻的两个可以连接在一起形成5,6或7元碳环或杂环，条件是R“ R 1，R 2，R 3和R 4不同时为氢。公开了所述化合物的药物组合物，以及用于治疗包括细胞过度增殖的生物学条件的方法。

5. 发明申请

WO2005011655A2 PYRIDAZINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：吡啶并吡啶衍生物及其作为治疗剂的用途
公开(公告)号：WO2005011655A2
公开(公告)日：2005-02-10
申请号：PCT/US2004024548
申请日：2004-07-29
申请人： XENON PHARMACEUTICALS INC , ABREO MELWYN , CHAFEEV MIKHAIL , CHAKKA NAGASREE , CHOWDHURY SULTAN , FU JIAN-MIN , GSCHWEND HEINZ W , HOLLADAY MARK W , HOU DUANJIE , KAMBOJ RAJENDER , KODUMURU VISHNUMURTHY , LI WENBAO , LIU SHIFENG , RAINA VANDNA , SUN SENGEN , SUN SHAOYI , SVIRIDOV SERGUEI , TU CHI , WINTHER MICHAEL D , ZHANG ZAIHUI
发明人： ABREO MELWYN , CHAFEEV MIKHAIL , CHAKKA NAGASREE , CHOWDHURY SULTAN , FU JIAN-MIN , GSCHWEND HEINZ W , HOLLADAY MARK W , HOU DUANJIE , KAMBOJ RAJENDER , KODUMURU VISHNUMURTHY , LI WENBAO , LIU SHIFENG , RAINA VANDNA , SUN SENGEN , SUN SHAOYI , SVIRIDOV SERGUEI , TU CHI , WINTHER MICHAEL D , ZHANG ZAIHUI
IPC分类号： A61K31/00 , A61K31/501 , A61K31/551 , A61P3/06 , C07D237/20 , C07D237/24
CPC分类号： A61K31/00 , A61K31/501 , A61K31/551 , C07D237/20 , C07D237/24
摘要： Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I), where x, y, W, V, R , R , R , R , R , R , R , R , R , R , R and R are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
摘要翻译：公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物，其中x，y，W，V，R R 2，R 3，R 4，R 5，R 6，R 6a，R 7，R 7a，R 8，R 8a，R 本文定义<9>和R 9a。还公开了包含式（I）化合物的药物组合物。

6. 发明申请

WO2006086447A3 PYRIDAZINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：吡啶并吡啶衍生物及其作为治疗剂的用途
公开(公告)号：WO2006086447A3
公开(公告)日：2007-04-05
申请号：PCT/US2006004389
申请日：2006-02-08
申请人： XENON PHARMACEUTICALS INC , CHAKKA NAGASREE , CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FU JIAN-MIN , HOU DUANJIE , KAMBOJ RAJENDER , KODUMURU VISHNUMURTHY , LIU SHIFENG , RAINA VANDNA , SUN SHAOYI , SVIRIDOV SERGUEI , WINTHER MICHAEL D , ZHANG ZAIHUI , ABREO MELWYN , HOLLADAY MARK W , LI WENBAO , SUN SENGEN , TU CHI , GSCHWEND HEINZ W
发明人： CHAKKA NAGASREE , CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FU JIAN-MIN , HOU DUANJIE , KAMBOJ RAJENDER , KODUMURU VISHNUMURTHY , LIU SHIFENG , RAINA VANDNA , SUN SHAOYI , SVIRIDOV SERGUEI , WINTHER MICHAEL D , ZHANG ZAIHUI , ABREO MELWYN , HOLLADAY MARK W , LI WENBAO , SUN SENGEN , TU CHI , GSCHWEND HEINZ W
IPC分类号： C07D237/20 , A61K31/00 , A61K31/501 , A61K31/551 , A61P3/06 , C07D237/22 , C07D237/24
CPC分类号： C07D237/20 , A61K31/00 , A61K31/501 , A61K31/551 , C07D237/22 , C07D237/24
摘要： Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (Ia): where x, y, W, V, R 2 , R 3 , R 4 , R 5 , R 6 , R 6a , R 7 , R 7a , R 8 , R 8a , R 9 and R 9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
摘要翻译：公开了治疗哺乳动物，优选人类的SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（Ia）化合物：其中x，y，W，V，R R 2，R 3，R 4，R 5，R 6，R 6，R 4， R 6a，R 7，R 7a，R 8，R 8a，R 8，R 7，本文定义了9和9和9 9。还公开了包含式（I）化合物的药物组合物。

7. 发明申请

WO2008151288A3 AROMATIC AND HETEROAROMATIC COMPOUNDS USEFUL IN TREATING IRON DISORDERS 审中-公开
标题翻译：芳香和异黄酮化合物可用于治疗铁质疾病
公开(公告)号：WO2008151288A3
公开(公告)日：2009-09-24
申请号：PCT/US2008065949
申请日：2008-06-05
申请人： XENON PHARMACEUTICALS INC , CADIEUX JEAN-JACQUES , CHAFEEV MIKHAIL , FONAREV JULIA , FU JIANMIN , KAMBOJ RAJENDER , KODUMURU VISHNUMURTHY , SVIRIDOV SERGUEI , ZHANG ZAIHUI
发明人： CADIEUX JEAN-JACQUES , CHAFEEV MIKHAIL , FONAREV JULIA , FU JIANMIN , KAMBOJ RAJENDER , KODUMURU VISHNUMURTHY , SVIRIDOV SERGUEI , ZHANG ZAIHUI
IPC分类号： A61K31/155 , A61K31/275 , A61K31/381 , A61K31/4196 , A61K31/44 , A61P7/00 , A61P7/06
CPC分类号： A61K31/155 , A61K31/275 , A61K31/381 , A61K31/4196 , A61K31/44
摘要： This invention is directed to compounds of formula (I), wherein m, formula (II), R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.
摘要翻译：本发明涉及式（I）化合物，其中m，式（II），R 1，R 2和R 3如本文所定义，为其立体异构体，对映异构体，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，用于治疗铁疾病。本发明还涉及包含该化合物的药物组合物和使用该化合物治疗铁疾病的方法。

8. 发明申请

WO2008115999A8 BIARYL AND BIHETEROARYL COMPOUNDS USEFUL IN TREATING IRON DISORDERS 审中-公开
标题翻译： BIARYL和BIEETEROARYL化合物有用的治疗铁路疾病
公开(公告)号：WO2008115999A8
公开(公告)日：2008-12-24
申请号：PCT/US2008057519
申请日：2008-03-19
申请人： XENON PHARMACEUTICALS INC , CHAFEEV MIKHAIL , CHAKKA NAGASREE , CADIEUX JEAN-JACQUES , FU JIANMIN , KAMBOJ RAJENDER , KODUMURU VISHNUMURTHY , LANGILLE JONATHAN , LIU SHIFENG , SUN JIANYU , SVIRIDOV SERGUEI , ZHANG ZAIHUI
发明人： CHAFEEV MIKHAIL , CHAKKA NAGASREE , CADIEUX JEAN-JACQUES , FU JIANMIN , KAMBOJ RAJENDER , KODUMURU VISHNUMURTHY , LANGILLE JONATHAN , LIU SHIFENG , SUN JIANYU , SVIRIDOV SERGUEI , ZHANG ZAIHUI
IPC分类号： C07C279/20 , A61K31/155 , A61K31/381 , A61P7/00 , C07C279/28 , C07C317/42 , C07C323/43 , C07D333/34
CPC分类号： C07D333/34 , C07C323/44 , C07C323/62 , C07C335/16 , C07C335/32 , C07D333/38
摘要： This invention is directed to compounds of formula (I), wherein A, B, m, n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.
摘要翻译：本发明涉及式（I）化合物，其中A，B，m，n，R 1，R 2和R 3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，用于治疗铁疾病。本发明还涉及包含该化合物的药物组合物和使用该化合物治疗铁疾病的方法。

9. 发明专利

CA2468562A1 HYDRAZONOPYRAZOLE DERIVATIVES AND THEIR USE AS THERAPEUTICS 未知
公开(公告)号：CA2468562A1
公开(公告)日：2003-06-05
申请号：CA2468562
申请日：2002-10-18
申请人： KINETEK PHARMACEUTICALS INC
发明人： DAYNARD TIMOTHY S , CHAFEEV MIKHAIL A , CHOPIUK GREG B , ZHANG ZAIHUI , WANG SHISEN , SVIRIDOV SERGUEI V
IPC分类号： C07D231/04 , A61K31/403 , A61K31/409 , A61K31/415 , A61K31/4155 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/655 , A61K45/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/08 , C07D231/38 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12
摘要： Pharmaceutical compositions and compounds are provided. The compounds of the invention deomonstrate anti-proliferative activity, and may promote apoptosi s in cells lacking normal regulation of cell cycle and death. In one embodimen t of the invention, pharmaceutical compositions of the compounds in combinatio n with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, Iymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.

10. 发明专利

AU2003254650A1 PYRAZOLYLBENZOTHIAZOLE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 未知
公开(公告)号：AU2003254650A1
公开(公告)日：2004-02-16
申请号：AU2003254650
申请日：2003-07-23
申请人： KINETEK PHARMACEUTICALS INC
发明人： ZHANG ZAIHUI , DAYNARD TIMOTHY S , WANG SHISEN , DU XINYAO , CHOPIUK GREGORY B , YAN JUN , CHEN JIANXIN , SVIRIDOV SERGUEI V
IPC分类号： A61K31/428 , A61P35/00 , C07D413/04 , C07D417/04 , C07D417/14 , C07D513/04 , C07D521/00 , C07D417/00

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