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21. 发明申请

WO2008086462A3 AMINO-SUBSTITUTED QUINAZOLINE DERIVATIVES AS INHIBITORS OF β-CANTENIN/TCF-4 PATHWAY AND CANCER TREATMENT AGENTS 审中-公开
公开(公告)号：WO2008086462A3
公开(公告)日：2008-07-17
申请号：PCT/US2008/050728
申请日：2008-01-10
申请人： WYETH , VENKATESAN, Aranapakam, M. , DEHNHARDT, Christoph , CHEN, Zecheng , SANTOS, Osvaldo, Dos , SANTOS, Efren, Delos , CURRAN, Kevin , AYRAL-KALOUSTIAN, Semiramis , CHEN, Lei
发明人： VENKATESAN, Aranapakam, M. , DEHNHARDT, Christoph , CHEN, Zecheng , SANTOS, Osvaldo, Dos , SANTOS, Efren, Delos , CURRAN, Kevin , AYRAL-KALOUSTIAN, Semiramis , CHEN, Lei
IPC分类号： C07D239/95 , C07D401/12 , C07D401/14 , C07D403/12 , A61K31/517 , A61P35/00
摘要： The present invention relates to amino-substituted quinazoline derivatives as inhibitors of β-catenin/tcf-4 pathway, which can be useful in the treatment of cancer; to processes for their preparation; to pharmaceutical compositions comprising them; and to methods of using them.

22. 发明申请

WO2005030775A1 6-[(SUBSTITUTED)PHENYL]TRIAZOLOPYRIMIDINES AS ANTICANCER AGENTS 审中-公开
标题翻译： 6 - [（取代的）苯基]三唑并嘧啶作为反应剂
公开(公告)号：WO2005030775A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/030515
申请日：2004-09-17
申请人： WYETH HOLDINGS CORPORATION , ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep , WU, Yanzhong , TONG, Wei
发明人： ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep , WU, Yanzhong , TONG, Wei
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： This invention relates to certain 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof. The present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及某些6 - [（取代的）苯基]三唑并嘧啶化合物或其药学上可接受的盐，以及含有所述化合物或其药学上可接受的盐的组合物，其中所述化合物是可用于治疗哺乳动物癌症的抗癌剂。本发明还涉及治疗或抑制哺乳动物中癌性肿瘤细胞和相关疾病的生长的方法，并进一步提供了治疗或预防表达多重耐药性（MDR）或耐多药耐药性的癌性肿瘤的方法在有需要的哺乳动物中，所述方法包括向所述哺乳动物施用有效量的所述化合物或其药学上可接受的盐。本发明涉及通过促进微管聚合来治疗或抑制有需要的哺乳动物中癌性肿瘤细胞和相关疾病的生长的方法，其包括对所述哺乳动物施用有效量的所述化合物及其药学上可接受的盐。

23. 发明申请

WO2005030216A1 5-ARYLPYRIMIDINES AS ANTICANCER AGENTS 审中-公开
标题翻译： 5-ARYLPYRIMININES作为反应剂
公开(公告)号：WO2005030216A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/030682
申请日：2004-09-17
申请人： WYETH HOLDINGS CORPORATION , ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep
发明人： ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep
IPC分类号： A61K31/505
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , C07D239/48 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： This invention relates to certain 5-arylpyrimidine compounds or a pharmaceutically acceptable salt thereof, and compositions containing said compounds or a pharmaceutically acceptable salt thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or a pharmaceutically acceptable salt thereof. More specifically, the present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及某些5-芳基嘧啶化合物或其药学上可接受的盐，以及含有所述化合物或其药学上可接受的盐的组合物，其中所述化合物是可用于治疗哺乳动物癌症的抗癌剂。本发明还涉及治疗或抑制哺乳动物中癌性肿瘤细胞和相关疾病的生长的方法，并进一步提供了治疗或预防表达多重耐药性（MDR）或耐多药耐药性的癌性肿瘤的方法在需要的哺乳动物中，所述方法包括向所述哺乳动物施用有效量的所述化合物或其药学上可接受的盐。更具体地，本发明涉及通过促进微管聚合来治疗或抑制有需要的哺乳动物中癌性肿瘤细胞和相关疾病的生长的方法，其包括向所述哺乳动物施用有效量的所述化合物和药学上可接受的盐它们。

24. 发明申请

WO2010030727A1 3-SUBSTITUTED-1H-INDOLE, 3-SUBSTITUTED-1H-PYRROLO[2,3-B]PYRIDINE AND 3-SUBSTITUTED-1H-PYRROLO[3,2-B]PYRIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开
标题翻译： 3-取代的1H-吲哚，3-取代的1H-吡咯并[2,3-b]吡啶和3-取代的1H-吡咯[3,2-B]吡啶化合物，它们作为MTOR激酶和PI3激酶抑制剂，和他们的合成
公开(公告)号：WO2010030727A1
公开(公告)日：2010-03-18
申请号：PCT/US2009/056443
申请日：2009-09-10
申请人： WYETH LLC , AYRAL-KALOUSTIAN, Semiramis , MANSOUR, Tarek Suhayl , TSOU, Hwei-Ru , ZHANG, Nan , VENKATESAN, Aranapakam M. , DI, Li , KERNS, Edward H.
发明人： AYRAL-KALOUSTIAN, Semiramis , MANSOUR, Tarek Suhayl , TSOU, Hwei-Ru , ZHANG, Nan , VENKATESAN, Aranapakam M. , DI, Li , KERNS, Edward H.
IPC分类号： C07D407/06 , C07D471/04 , A61K31/404 , A61P35/00
CPC分类号： C07D407/06 , C07D471/04
摘要： The invention relates to 3-substituted-1H-indole, 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula (I): or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.
摘要翻译：本发明涉及式（I）的3-取代-1H-吲哚，3-取代-1H-吡咯并[2,3-b]吡啶和3-取代-1H-吡咯并[3,2-b]吡啶化合物）或其药学上可接受的盐，其中组成变量如本文所定义，包含该化合物的组合物，以及制备和使用该化合物的方法。

25. 发明申请

WO2009120826A1 2-ARYL- AND 2-HETEROARYLTHIAZOLYL COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE THEREOF 审中-公开
标题翻译： 2-芳基和2-杂环戊二烯化合物，其制备和使用方法
公开(公告)号：WO2009120826A1
公开(公告)日：2009-10-01
申请号：PCT/US2009/038343
申请日：2009-03-26
申请人： WYETH , ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , MANSOUR, Tarek, Suhayl , NGUYEN, Thai, Hiep , NIU, Chuansheng , ROSFJORD, Edward, Christian , SUAYAN, Ronald , TSOU, Hwei-Ru
发明人： ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , MANSOUR, Tarek, Suhayl , NGUYEN, Thai, Hiep , NIU, Chuansheng , ROSFJORD, Edward, Christian , SUAYAN, Ronald , TSOU, Hwei-Ru
IPC分类号： C07D277/60 , C07D417/04 , C07D417/10 , C07D417/12 , A61K31/428 , A61P35/00
CPC分类号： C07D277/66 , C07D277/60 , C07D417/04 , C07D417/10 , C07D417/12
摘要： The present invention discloses fused bicyclic 2-aryl- or 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumor growth in particular and to treat diseases or disorders associated with securin, including elevated securin levels.
摘要翻译：本发明公开了稠合双环2-芳基 - 或2-杂芳基噻唑基化合物及其药学上可接受的盐和酯，其可用于抑制癌细胞的生长，特别是抑制人乳腺癌肿瘤生长，并且治疗相关的疾病或病症与Securin，包括提高的Securin水平。

26. 发明申请

WO2005030218A1 6-ARYL-7-HALO-IMIDAZO[1,2-A]PYRIMIDINES AS ANTICANCER AGENT 审中-公开
标题翻译： 6-ARYL-7-氢化咪唑并[1,2-A]吡啶类作为抗原剂
公开(公告)号：WO2005030218A1
公开(公告)日：2005-04-07
申请号：PCT/US2004/030595
申请日：2004-09-17
申请人： WYETH HOLDINGS CORPORATION , ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis
发明人： ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis
IPC分类号： A61K31/519
CPC分类号： C07D487/04
摘要： This invention relates to certain 6-aryl-7-halo-imidazo[1,2-a]pyrimidines or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals by promotion of microtubule polymerization. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及某些6-芳基-7-卤代咪唑并[1,2-a]嘧啶或其药学上可接受的盐，以及含有所述化合物或其药学上可接受的盐的组合物，其中所述化合物是可用于通过促进微管聚合治疗哺乳动物的癌症。本发明还涉及治疗或抑制哺乳动物中癌性肿瘤细胞和相关疾病的生长的方法，并进一步提供了治疗或预防表达多重耐药性（MDR）或耐多药耐药性的癌性肿瘤的方法在有需要的哺乳动物中，所述方法包括向所述哺乳动物施用有效量的所述化合物或其药学上可接受的盐。

27. 发明申请

WO2009120849A1 2-ARYL- AND 2-HETEROARYLTHIAZOLYL COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE THEREOF 审中-公开
标题翻译： 2-芳基和2-杂环戊二烯化合物，其制备和使用方法
公开(公告)号：WO2009120849A1
公开(公告)日：2009-10-01
申请号：PCT/US2009/038372
申请日：2009-03-26
申请人： WYETH , ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep , NIU, Chuansheng , ROSFJORD, Edward, Christian , SUAYAN, Ronald
发明人： ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep , NIU, Chuansheng , ROSFJORD, Edward, Christian , SUAYAN, Ronald
IPC分类号： C07D513/04 , A61K31/429 , A61P35/00
CPC分类号： C07D513/04
摘要： The present invention discloses fused heterobicyclic 2-aryl- and 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumor growth in particular and to treat diseases or disorders associated with securin (Formula I) and pharmaceutically acceptable salts thereof, wherein A is H, C 1 -C 3 alkyi, or acetyl; Z is NR 3 or O; Q is -NR 1 R 2 , - NR 3 N(R 3 )2. - NR 3 OR 3 , or -OH.
摘要翻译：本发明公开了可用于抑制癌细胞生长，特别是抑制人乳腺癌肿瘤生长以及相关的疾病或病症的融合的杂双环2-芳基和2-杂芳基噻唑基化合物及其药学上可接受的盐和酯与Securin（式I）及其药学上可接受的盐，其中A是H，C 1 -C 3烷基或乙酰基; Z是NR 3或O; Q是-NR1R2，-NR3N（R3）2。 - NR 3 OR 3或-OH。

28. 发明申请

WO2005056560A1 PROCESS FOR THE PREPARATION OF TUBULIN INHIBITORS 审中-公开
标题翻译：制备维生素抑制剂的方法
公开(公告)号：WO2005056560A1
公开(公告)日：2005-06-23
申请号：PCT/US2004/040854
申请日：2004-12-07
申请人： WYETH , WU, Yanzhong , SCHMID, Jean , AFRAGOLA, Jay, Thomas , BLUM, David, Michael , AYRAL-KALOUSTIAN, Semiramis
发明人： WU, Yanzhong , SCHMID, Jean , AFRAGOLA, Jay, Thomas , BLUM, David, Michael , AYRAL-KALOUSTIAN, Semiramis
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a process for the preparation of 6-[(substituted) phenyl]-triazolopyrimidine dicarboxylic acid salt and as a hydrated salt having the structural formula (I) wherein: R 1 is CF 3 or C 2 F 5 ; R 2 is H or C 1 -C 3 alkyl; n is an integer of 2, 3, or 4; X is Cl or Br; R 3 and R 4 are each independently H or C,-C 3 alkyl; or R 3 and R 4 when optionally taken together with the nitrogen atom to which each is attached form a 4 to 6 membered saturated heterocyclic ring having 1-2 nitrogen atoms and 0-1 oxygen atoms or 0-1 sulfur atoms, and optionally substituted with R 5 ; R 5 is C,-C 3 alkyl; wherein the dotted line is an optional bond.
摘要翻译：本发明提供了制备6 - [（取代的）苯基] - 三唑并嘧啶二羧酸盐和具有结构式（I）的水合盐的方法，其中：R 1是CF 3或C 2 F 5; R 2是H或C 1 -C 3烷基; n是2,3或4的整数; X是Cl或Br; R 3和R 4各自独立地为H或C 1 -C 3烷基; 或R 3和R 4当任选地与各自连接的氮原子一起形成具有1-2个氮原子和0-1个氧原子或0-1个硫原子的4至6元饱和杂环时并且任选被R 5取代; R 5是C 1 -C 3烷基; 其中虚线是任选的键。

29. 发明公开

EP1680425A1 6- [(SUBSTITUTED)PHENYL] TRIAZOLOPYRIMIDINES AS ANTICANCER AGENTS 有权
标题翻译： 6 - [（取代的）苯基]三唑并嘧啶作为抗癌剂
公开(公告)号：EP1680425A1
公开(公告)日：2006-07-19
申请号：EP04788820.1
申请日：2004-09-17
申请人： Wyeth Holdings Corporation
发明人： ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep , WU, Yanzhong , TONG, Wei
IPC分类号： C07D487/04 , A61P35/00 , A61P35/04 , A61K31/519 , C07D249/00 , C07D239/00
CPC分类号： C07D487/04
摘要： This invention relates to certain 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof. The present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.

30. 发明公开

EP1663241A1 5-ARYLPYRIMIDINES AS ANTICANCER AGENTS 有权
标题翻译： 5-芳基嘧啶AS抗癌剂
公开(公告)号：EP1663241A1
公开(公告)日：2006-06-07
申请号：EP04784529.2
申请日：2004-09-17
申请人： Wyeth Holdings Corporation
发明人： ZHANG, Nan , AYRAL-KALOUSTIAN, Semiramis , NGUYEN, Thai, Hiep
IPC分类号： A61K31/505 , A61K31/506 , A61P35/00 , C07D239/42 , C07D239/48
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , C07D239/48 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： This invention relates to certain 5-arylpyrimidine compounds or a pharmaceutically acceptable salt thereof, and compositions containing said compounds or a pharmaceutically acceptable salt thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or a pharmaceutically acceptable salt thereof. More specifically, the present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.

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