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1. 发明申请

US20110190496A1 FUSED BICYCLIC mTOR INHIBITORS 审中-公开
标题翻译：熔融双相胶体抑制剂
公开(公告)号：US20110190496A1
公开(公告)日：2011-08-04
申请号：US13085722
申请日：2011-04-13
申请人： Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A.R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Quinghua Weng , James David Beard
发明人： Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A.R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Quinghua Weng , James David Beard
IPC分类号： C07D487/04 , C07F5/02 , C07D253/06
CPC分类号： C07D487/04 , A61K31/5025 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要： Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐是mTOR的抑制剂，可用于治疗癌症。

2. 发明申请

US20110171124A1 In situ methods for monitoring the EMT status of tumor cells in vivo 审中-公开
标题翻译：用于监测体内肿瘤细胞EMT状态的原位方法
公开(公告)号：US20110171124A1
公开(公告)日：2011-07-14
申请号：US12660310
申请日：2010-02-24
申请人： Joseph E. Bugaj , Robert C. Wild
发明人： Joseph E. Bugaj , Robert C. Wild
IPC分类号： A61K51/06 , A61K49/00 , G01N33/00 , A61P35/00
CPC分类号： A61K49/0058 , G01N33/574 , G01N2500/00
摘要： The invention provides methods of determining in situ the EMT status of the cells of a tumor in a patient in vivo, including: (a) providing an EMT-status-detecting conjugate containing an antibody that binds to an EMT-status biomarker, and a reporter molecule; (b) introducing the conjugate into a patient with a tumor, such that the conjugate contacts the EMT-status biomarker of the cells of the tumor; (c) employing a means for detection of the signal from the conjugate at the tumor site; and (d) using a means for image analysis to localize and quantify the signal from the conjugate at the tumor site, a positive signal indicating the presence of epithelial tumor cells if the EMT-status biomarker is an epithelial biomarker, and mesenchymal tumor cells if the EMT-status biomarker is a mesenchymal biomarker. Such methods are useful for diagnosing patients who might benefit from treatment with drugs such as EGFR or IGF-1R kinase inhibitors, and for identifying and testing agents that inhibit tumor cells from undergoing an epithelial to mesenchymal transition. This invention also provides the above methods where an AFFIBODY® molecule that binds to an EMT-status biomarker is used instead of an antibody.
摘要翻译：本发明提供了在体内确定患者体内肿瘤细胞的EMT状态的方法，包括：（a）提供包含结合EMT状态生物标志物的抗体的EMT状态检测缀合物，以及报告分子; （b）将缀合物引入患有肿瘤的患者中，使得缀合物与肿瘤细胞的EMT状态生物标志物接触; （c）采用在肿瘤部位检测来自缀合物的信号的方法; 和（d）使用图像分析方法来定位和量化来自肿瘤位点的缀合物的信号，如果EMT状态生物标志物是上皮生物标志物，则表示存在上皮肿瘤细胞的阳性信号，以及间质肿瘤细胞 EMT状态生物标志物是间充质生物标志物。这样的方法可用于诊断可能受益于诸如EGFR或IGF-1R激酶抑制剂的药物治疗的患者，以及用于鉴定和测试抑制肿瘤细胞经历上皮至间质转化的试剂。本发明还提供了上述方法，其中使用结合EMT状态生物标志物的AFFIBODY分子代替抗体。

3. 发明申请

US20100286155A1 ADRENOCORTICAL CARCINOMA TREATMENT 审中-公开
公开(公告)号：US20100286155A1
公开(公告)日：2010-11-11
申请号：US12775556
申请日：2010-05-07
申请人： Elizabeth A. BUCK , Andrew W. STEPHENS
发明人： Elizabeth A. BUCK , Andrew W. STEPHENS
IPC分类号： A61K31/4985 , A61P35/00
CPC分类号： A61K31/4985
摘要： A method of treating adrenocortical carcinoma with OSI-906.
摘要翻译：用OSI-906治疗肾上腺皮质癌的方法。

4. 发明申请

US20100099679A1 FUSED BICYCLIC mTOR INHIBITORS 有权
标题翻译：熔融双相胶体抑制剂
公开(公告)号：US20100099679A1
公开(公告)日：2010-04-22
申请号：US12622545
申请日：2009-11-20
申请人： Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A.R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Quinghua Weng , James David Beard
发明人： Xin Chen , Heather Coate , Andrew Philip Crew , Han-Qing Dong , Ayako Honda , Mark Joseph Mulvihill , Paula A.R. Tavares , Jing Wang , Douglas S. Werner , Kristen Michelle Mulvihill , Kam W. Siu , Bijoy Panicker , Apoorba Bharadwaj , Lee D. Arnold , Meizhong Jin , Brian Volk , Quinghua Weng , James David Beard
IPC分类号： A61K31/53 , C07D487/04 , A61K31/4985 , A61P35/00
CPC分类号： C07D487/04 , A61K31/5025 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要： Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐是mTOR的抑制剂，可用于治疗癌症。

5. 发明授权

US07696225B2 (2-carboxamido)(3-Amino) thiophene compounds 失效
标题翻译：（2-甲酰氨基）（3-氨基）噻吩化合物
公开(公告)号：US07696225B2
公开(公告)日：2010-04-13
申请号：US10973870
申请日：2004-10-26
申请人： Jason Bloxham , Andrew Phillip Crew , Ayako Honda , An-Hu Li , Bijoy Panicker , Graham Michael Wynne , Lawrence Tardibono, Jr.
发明人： Jason Bloxham , Andrew Phillip Crew , Ayako Honda , An-Hu Li , Bijoy Panicker , Graham Michael Wynne , Lawrence Tardibono, Jr.
IPC分类号： A61K31/4745 , A61K31/4709 , A61K31/4436
CPC分类号： A61K31/381 , A61K31/437 , A61K31/4436 , A61K31/4709 , A61K31/4745 , A61K45/06 , C07D409/12 , C07D409/14 , C07D471/04 , A61K2300/00
摘要： Amidoaryl/amidoheteroaryl substituted thiophenes, further substituted with a heteroarylmethylamino group, are useful in the treatment of cancer.
摘要翻译：进一步被杂芳基甲基氨基取代的酰胺芳基/酰胺基芳基取代的噻吩可用于治疗癌症。

6. 发明授权

US07521448B2 N-substituted benzimidazolyl c-Kit inhibitors 失效
标题翻译： N-取代苯并咪唑c-Kit抑制剂
公开(公告)号：US07521448B2
公开(公告)日：2009-04-21
申请号：US10921414
申请日：2004-08-16
申请人： Joshua Bolger , Arlindo L. Castelhano , Andrew Phillip Crew , Han-Qing Dong , Ayako Honda , Radoslaw Laufer , An-Hu Li , Kristen Mulvihill , Li Qiu , Colin Peter Sambrook Smith , Yingchaun Sun , Graham Michael Wynne , Tao Zhang
发明人： Joshua Bolger , Arlindo L. Castelhano , Andrew Phillip Crew , Han-Qing Dong , Ayako Honda , Radoslaw Laufer , An-Hu Li , Kristen Mulvihill , Li Qiu , Colin Peter Sambrook Smith , Yingchaun Sun , Graham Michael Wynne , Tao Zhang
IPC分类号： A61K31/5377 , C07D413/12
CPC分类号： C07D235/06 , C04B35/632 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐或N-氧化物可用于治疗癌症。

7. 发明申请

US20090082369A1 Pyrrolo[2,3d]pyrimidine compositions and their use 审中-公开
标题翻译：吡咯并[2,3d]嘧啶组合物及其用途
公开(公告)号：US20090082369A1
公开(公告)日：2009-03-26
申请号：US12228867
申请日：2008-08-15
申请人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
发明人： Arlindo L. Castelhano , Bryan McKibben , David J. Witter
IPC分类号： A61K31/519 , C07D487/04 , A61P9/00 , A61P25/00
CPC分类号： C07D487/04 , A61K31/519
摘要： This invention pertains to compounds having the structure: wherein R1 and R2 together form a substituted or unsubstituted heterocyclic ring; R3 is a substituted or unsubstituted aryl moiety; R4 is a hydrogen atom, an unsubstituted alkyl, or a substituted or unsubstituted aryl moiety; and R5 and R6 are each independently a halogen atom, a hydrogen atom or a substituted or unsubstituted alkyl, aryl, or alkylaryl moiety, or a pharmaceutically acceptable salt thereof, and the use of these compounds to treat a disease associated with increased levels of adenosine in a subject.
摘要翻译：本发明涉及具有以下结构的化合物：其中R1和R2一起形成取代或未取代的杂环; R3是取代或未取代的芳基部分; R4是氢原子，未取代的烷基或取代或未取代的芳基部分; 并且R 5和R 6各自独立地为卤素原子，氢原子或取代或未取代的烷基，芳基或烷基芳基部分或其药学上可接受的盐，以及这些化合物用于治疗与腺苷水平升高相关的疾病的用途在一个主题

8. 发明授权

US07388012B2 (Hydrazido)(amino)thiophene compounds 失效
标题翻译：（肼基）（氨基）噻吩化合物
公开(公告)号：US07388012B2
公开(公告)日：2008-06-17
申请号：US11227698
申请日：2005-09-15
申请人： Andrew Crew , An-Hu Li , Hanqing Dong , Tao Zhang
发明人： Andrew Crew , An-Hu Li , Hanqing Dong , Tao Zhang
IPC分类号： A61K31/4709 , A61K31/381 , A61K31/497 , C07D215/14 , C07D409/12 , C07D333/36 , C07D333/38
CPC分类号： C07D409/12 , C07D409/14
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J are defined herein, are useful in the treatment of tumors and cancers such as mastocytosis/mast cell leukemia, gastrointestinal stromal tumors (GIST), germ cell tumors, small cell lung carcinoma (SCLC), sinonasal natural killer/T-cell lymphoma, testicular cancer (seminoma), thyroid carcinoma, malignant melanoma, ovarian carcinoma, adenoid cystic carcinoma, acute myelogenous leukemia (AML), breast carcinoma, pediatric T-cell acute lymphoblastic leukemia, neuroblastoma, mast cell leukemia, angiosarcoma, anaplastic large cell lymphoma, endometrial carcinoma, and prostate carcinoma.
摘要翻译：式（I）表示的化合物或其药学上可接受的盐或N-氧化物，其中A和J在本文中定义，可用于治疗肿瘤和癌症如肥大细胞增多症/肥大细胞白血病，胃肠道间质瘤（GIST），生殖细胞肿瘤，小细胞肺癌（SCLC），鼻窦自然杀伤/ T细胞淋巴瘤，睾丸癌（精原细胞瘤），甲状腺癌，恶性黑素瘤，卵巢癌，腺样囊性癌，急性骨髓性白血病（AML），乳腺癌，儿科T细胞急性淋巴细胞白血病，神经母细胞瘤，肥大细胞白血病，血管肉瘤，间变性大细胞淋巴瘤，子宫内膜癌和前列腺癌。

9. 发明授权

US07101893B2 (2-Carboxamido)(3-amino)thiophene compounds 有权
标题翻译：（2-羧甲酰氨基）（3-氨基）噻吩化合物
公开(公告)号：US07101893B2
公开(公告)日：2006-09-05
申请号：US11116007
申请日：2005-04-27
申请人： Andrew Phillip Crew
发明人： Andrew Phillip Crew
IPC分类号： A61K31/4745 , A61K31/4709 , A61K31/4436
CPC分类号： C07D409/12 , A61K31/165 , A61K31/22 , A61K31/277 , A61K31/381 , A61K31/437 , A61K31/4436 , A61K31/444 , A61K31/4709 , A61K31/4745 , A61K45/06 , C07D409/14 , C07D471/04 , A61K2300/00
摘要： A method of treatment of hyperproliferative disorders comprises administering an effective amount of a compound represented by Formula II: or a pharmaceutically acceptable salt thereof.
摘要翻译：治疗过度增殖性疾病的方法包括施用有效量的由式II表示的化合物或其药学上可接受的盐。

10. 发明申请

US20040180375A1 AGS proteins and nucleic acid molecules and uses therefor 失效
标题翻译： AGS蛋白和核酸分子及其用途
公开(公告)号：US20040180375A1
公开(公告)日：2004-09-16
申请号：US10804491
申请日：2004-03-19
申请人： OSI Pharmaceuticals, Inc.
发明人： Mary Cismowski , Emir Duzic
IPC分类号： C12Q001/68 , C07H021/04 , C07K014/705 , C12N001/18 , C12N015/74
CPC分类号： C07K14/4706
摘要： A screening assay in yeast is disclosed wherein G-protein coupled-receptor independent activators and inhibitors of the pheromone pathway can be identified using a mammalian cDNA library. Novel Activator of G protein Signaling (nullAGSnull) proteins, which are Ras-related proteins that stimulate G protein activity in a receptor-independent manner, are disclosed, as well as nucleic acid molecules encoding AGS proteins. In addition to isolated AGS proteins, the invention further provides isolated AGS fusion proteins, antigenic peptides and anti-AGS antibodies. The invention also provides isolated AGS nucleic acid molecules, recombinant expression vectors containing a nucleic acid molecule of the invention, host cells into which the expression vectors have been introduced and non-human transgenic animals in which an AGS gene has been introduced or disrupted. Diagnostic, screening and therapeutic methods utilizing compositions of the invention are also provided.
摘要翻译：公开了酵母中的筛选测定法，其中可以使用哺乳动物cDNA文库鉴定G蛋白偶联受体独立的激活剂和信息素途径的抑制剂。公开了G蛋白信号传导（“AGS”）蛋白的新型活化剂，其是以不依赖于受体的方式刺激G蛋白活性的Ras相关蛋白，以及编码AGS蛋白的核酸分子。除了分离的AGS蛋白，本发明还提供分离的AGS融合蛋白，抗原肽和抗AGS抗体。本发明还提供了分离的AGS核酸分子，含有本发明的核酸分子的重组表达载体，已经引入了表达载体的宿主细胞和已引入或破坏了AGS基因的非人转基因动物。还提供利用本发明组合物的诊断，筛选和治疗方法。

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