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1. 发明申请

US20090270447A1 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-杂芳基噻唑化合物，其制备方法及用途
公开(公告)号：US20090270447A1
公开(公告)日：2009-10-29
申请号：US12412538
申请日：2009-03-27
申请人： Nan Zhang , Semiramis Ayral-Kaloustian , Thai Hiep Nguyen , Chuansheng Niu , Edward Christian Rosfjord , Ronald Suayan
发明人： Nan Zhang , Semiramis Ayral-Kaloustian , Thai Hiep Nguyen , Chuansheng Niu , Edward Christian Rosfjord , Ronald Suayan
IPC分类号： A61K31/4439 , C07D471/04 , 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.
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。

2. 发明申请

US20090270363A1 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-杂芳基噻唑化合物，其制备方法及用途
公开(公告)号：US20090270363A1
公开(公告)日：2009-10-29
申请号：US12412506
申请日：2009-03-27
申请人： Nan Zhang , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Thai Hiep Nguyen , Chuansheng Niu , Edward Christian Rosfjord , Ronald Suayan , Hwei-Ru Tsou
发明人： Nan Zhang , Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Thai Hiep Nguyen , Chuansheng Niu , Edward Christian Rosfjord , Ronald Suayan , Hwei-Ru Tsou
IPC分类号： A61K31/428 , C07D277/66 , C07D417/10 , A61K31/506 , A61K31/397 , 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。

3. 发明申请

US20090311217A1 3-SUBSTITUTED-1H-INDOLE 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-吲哚化合物，它们作为MTOR激酶和PI3激酶抑制剂使用，以及它们的合成
公开(公告)号：US20090311217A1
公开(公告)日：2009-12-17
申请号：US12473605
申请日：2009-05-28
申请人： Matthew Gregory Bursavich , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Thai Hiep Nguyen , Sabrina Lombardi , David Malwitz , Natasja Brooijmans , Derek Cecil Cole , Adam Matthew Gilbert , Pawel Wojciech Nowak , Kaapjoo Park , Sasmita Das , Hwei-Ru Tsou , Aranapakam Mudumbai Venkatesan , Mercy Adufa Otteng , Gary Harold Birnberg , Gloria Jean MacEwan
发明人： Matthew Gregory Bursavich , Nan Zhang , Semiramis Ayral-Kaloustian , James Thomas Anderson , Thai Hiep Nguyen , Sabrina Lombardi , David Malwitz , Natasja Brooijmans , Derek Cecil Cole , Adam Matthew Gilbert , Pawel Wojciech Nowak , Kaapjoo Park , Sasmita Das , Hwei-Ru Tsou , Aranapakam Mudumbai Venkatesan , Mercy Adufa Otteng , Gary Harold Birnberg , Gloria Jean MacEwan
IPC分类号： A61K31/404 , C07D405/02 , C07D403/14 , C07D413/02 , A61K31/496 , A61K31/5377 , A61K38/21 , A61K39/395 , A61P35/00
CPC分类号： C07D405/14 , C07D405/06
摘要： The invention relates to 3-substituted-1H-indole 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-吲哚化合物或其药学上可接受的盐，其中组分变量如本文所定义，包含该化合物的组合物，以及制备和使用该化合物的方法。

4. 发明申请

US20090192147A1 [a]-FUSED INDOLE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES 审中-公开
标题翻译： [a] - 兴奋剂化合物，它们作为mTOR激酶和PI3激酶抑制剂使用，以及它们的合成
公开(公告)号：US20090192147A1
公开(公告)日：2009-07-30
申请号：US12363013
申请日：2009-01-30
申请人： Semiramis Ayral-Kaloustian , Nan Zhang , Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Thai Hiep Nguyen , James Thomas Anderson
发明人： Semiramis Ayral-Kaloustian , Nan Zhang , Aranapakam Mudumbai Venkatesan , Tarek Suhayl Mansour , Thai Hiep Nguyen , James Thomas Anderson
IPC分类号： A61K31/5383 , C07D471/00 , A61K31/437 , C07D487/00 , A61K31/4985
CPC分类号： C07D498/04 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D491/04 , C07D491/14 , C07D498/14 , C07D513/04 , C07D513/14
摘要： The invention relates to [a]-fused indole compounds of the Formula II, or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein. The invention also relates to compositions comprising the compounds of Formula II, and methods for making and using the compounds.
摘要翻译：本发明涉及式[II]的[a] - 吲哚化合物或其药学上可接受的盐，其中组分变量如本文所定义。本发明还涉及包含式II化合物的组合物，以及制备和使用该化合物的方法。

5. 发明申请

US20090298820A1 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-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激酶抑制剂使用，以及它们的合成
公开(公告)号：US20090298820A1
公开(公告)日：2009-12-03
申请号：US12473658
申请日：2009-05-28
申请人： Hwei-Ru Tsou , Gary Harold Birnberg , Gloria Jean MacEwan , Semiramis Ayral-Kaloustian , Matthew Gregory Bursavich , Sabrina Lombardi , Nan Zhang , Adam Matthew Gilbert , George Theordore Grosu , Natasja Brooijmans , Thai Hiep Nguyen
发明人： Hwei-Ru Tsou , Gary Harold Birnberg , Gloria Jean MacEwan , Semiramis Ayral-Kaloustian , Matthew Gregory Bursavich , Sabrina Lombardi , Nan Zhang , Adam Matthew Gilbert , George Theordore Grosu , Natasja Brooijmans , Thai Hiep Nguyen
IPC分类号： A61K31/437 , A61K31/5375 , A61K31/5377 , A61K31/496 , C07D471/04 , A61P35/00 , C07D498/08 , A61P29/00 , A61P17/00 , A61P19/00
CPC分类号： C07D471/04 , C07D498/08
摘要： The invention relates to 3-substituted-1H-pyrrolo[2,3-b]pyridine, and 3-substituted-1H-pyrrolo[3,2-b]pyridine compounds of the Formula 1: 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1的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。

6. 发明申请

US20080255157A1 6-Aryl-7-halo-imidazo[1,2-a]pyrimidines as anticancer agents 失效
标题翻译： 6-芳基-7-卤代 - 咪唑并[1,2-a]嘧啶作为抗癌剂
公开(公告)号：US20080255157A1
公开(公告)日：2008-10-16
申请号：US11903100
申请日：2007-09-19
申请人： Nan Zhang , Semiramis Ayral-Kaloustian
发明人： Nan Zhang , Semiramis Ayral-Kaloustian
IPC分类号： A61K31/519 , A61P35/04
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。

7. 发明申请

US20050065167A1 6-Aryl-7-halo-imidazo[1,2-a]pyrimidines as anticancer agents 失效
标题翻译： 6-芳基-7-卤代 - 咪唑并[1,2-a]嘧啶作为抗癌剂
公开(公告)号：US20050065167A1
公开(公告)日：2005-03-24
申请号：US10950542
申请日：2004-09-24
申请人： Nan Zhang , Semiramis Ayral-Kaloustian
发明人： Nan Zhang , Semiramis Ayral-Kaloustian
IPC分类号： A61K31/519 , A61P35/00 , C07D487/02 , C07D487/04
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。

8. 发明申请

US20100061982A1 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：US20100061982A1
公开(公告)日：2010-03-11
申请号：US12556833
申请日：2009-09-10
申请人： Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Hwei-Ru Tsou , Nan Zhang , Aranapakam Mudumbai Venkatesan , Li Di , Edward Harvel Kerns
发明人： Semiramis Ayral-Kaloustian , Tarek Suhayl Mansour , Hwei-Ru Tsou , Nan Zhang , Aranapakam Mudumbai Venkatesan , Li Di , Edward Harvel Kerns
IPC分类号： A61K39/395 , C07D405/06 , A61K31/40 , C07D403/06 , A61K31/497 , C07D498/02 , A61K31/5386
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 1: 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1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。

9. 发明授权

US07507739B2 6-[(substituted)phenyl]triazolopyrimidines as anticancer agents 失效
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：US07507739B2
公开(公告)日：2009-03-24
申请号：US10950543
申请日：2004-09-24
申请人： Nan Zhang , Semiramis Ayral-Kaloustian , Thai Nguyen , Yanzhong Wu , Wei Tong
发明人： Nan Zhang , Semiramis Ayral-Kaloustian , Thai Nguyen , Yanzhong Wu , Wei Tong
IPC分类号： C07D487/04 , A61K31/519 , A61P35/04
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。

10. 发明申请

US20050090508A1 6-[(Substituted)phenyl]triazolopyrimidines as anticancer agents 失效
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：US20050090508A1
公开(公告)日：2005-04-28
申请号：US10950543
申请日：2004-09-24
申请人： Nan Zhang , Semiramis Ayral-Kaloustian , Thai Nguyen , Yanzhong Wu , Wei Tong
发明人： Nan Zhang , Semiramis Ayral-Kaloustian , Thai Nguyen , Yanzhong Wu , Wei Tong
IPC分类号： A61P35/00 , A61P35/04 , C07D487/04 , A61K31/519
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。

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