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1.发明授权公开(公告)号：US08476285B2
公开(公告)日：2013-07-02
申请号：US12494917
申请日：2009-06-30
申请人： Ashok C. Bajji , Se-Ho Kim , Benjamin Markovitz , Richard Trovato , Rajendra Tangallapally , Mark B. Anderson , Daniel Wettstein , Mark Shenderovich , John A. Vanecko
发明人： Ashok C. Bajji , Se-Ho Kim , Benjamin Markovitz , Richard Trovato , Rajendra Tangallapally , Mark B. Anderson , Daniel Wettstein , Mark Shenderovich , John A. Vanecko
IPC分类号： A61K31/52 , C07D473/34 , A61P35/00
CPC分类号： A61K31/52 , A61K31/522 , C07D473/34
摘要： The invention relates to compounds of Formulae I-III: and therapeutic uses thereof, wherein A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group; B is chosen from a substituted or unsubstituted piperidine, homopiperidine, piperazine, pyrrolidine or azetidine group; R1 is chosen from hydro, alkyl, aryl, heteroaryl, amino, or halo; and L1, L2, are as defined herein.
摘要翻译： 本发明涉及式I-III的化合物及其治疗用途，其中A选自取代或未取代的芳基，杂芳基，杂环或碳环基团; B选自取代或未取代的哌啶，高哌啶，哌嗪，吡咯烷或氮杂环丁烷基; R 1选自氢，烷基，芳基，杂芳基，氨基或卤素; 和L1，L2如本文所定义。
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2.发明申请公开(公告)号：US20100292255A1
公开(公告)日：2010-11-18
申请号：US12780828
申请日：2010-05-14
申请人： Ashok C. Bajji , Se-Ho Kim , Rajendra Tangallapally , Benjamin J. Markovitz , Richard Trovato , Mark B. Anderson , Daniel A. Wettstein , Mark D. Shenderovich
发明人： Ashok C. Bajji , Se-Ho Kim , Rajendra Tangallapally , Benjamin J. Markovitz , Richard Trovato , Mark B. Anderson , Daniel A. Wettstein , Mark D. Shenderovich
IPC分类号： A61K31/52 , C07D473/36 , A61P35/00
CPC分类号： C07D473/34
摘要： The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders, such as cancer.
摘要翻译： 本发明提供新颖的治疗化合物，包含这些化合物的药物组合物，以及使用这些化合物和组合物治疗疾病和病症如癌症的方法。
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公开(公告)号：US20100216862A1
公开(公告)日：2010-08-26
申请号：US12775253
申请日：2010-05-06
IPC分类号： A61K31/402 , C07D207/327 , A61P25/28 , C12N5/071
CPC分类号： C07D207/327 , C07D207/325 , C07D207/33 , C07D207/34
摘要： Novel pyrrole derivatives are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid plaques comprising the Aβ42 peptide.
摘要翻译： 公开了新颖的吡咯衍生物作为治疗和预防神经变性疾病的42降低剂，其特征在于包含Aβ42肽的淀粉样蛋白斑的形成或积累。
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公开(公告)号：US20100069383A1
公开(公告)日：2010-03-18
申请号：US12500863
申请日：2009-07-10
申请人： MARK B. ANDERSON , J. Adam Willardsen , Warren S. Weiner , Ashantai Yungai , Robert J. Halter , Yevgeniya Klimova , Kazuyuki Suzuki , Matthew Reeder
发明人： MARK B. ANDERSON , J. Adam Willardsen , Warren S. Weiner , Ashantai Yungai , Robert J. Halter , Yevgeniya Klimova , Kazuyuki Suzuki , Matthew Reeder
IPC分类号： A61K31/517 , A61K31/5377 , A61K31/52 , C07D413/12 , C07D473/00 , C07D401/12 , C07D239/95
CPC分类号： C07D239/94 , C07D239/95 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D487/04
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译： 公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。 本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症。
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5.发明申请PHARMACEUTICAL COMPOUNDS AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF 审中-公开作为细胞增殖抑制剂的药物化合物及其用途公开(公告)号：US20100068197A1
公开(公告)日：2010-03-18
申请号：US12500449
申请日：2009-07-09
申请人： MARK B. ANDERSON , J. Adam Willardsen , Warren S. Weiner , Kazuyuki Suzuki , Robert J. Halter , In Chul Kim , Matthew Reeder , Ashantai Yungai
发明人： MARK B. ANDERSON , J. Adam Willardsen , Warren S. Weiner , Kazuyuki Suzuki , Robert J. Halter , In Chul Kim , Matthew Reeder , Ashantai Yungai
IPC分类号： A61K31/517 , C07D239/95 , C07D403/12 , C07D487/04 , A61K31/5025 , A61P35/00 , A61K39/395 , C12N5/00
CPC分类号： C07D403/12 , C07D239/95 , C07D487/04
摘要： Disclosed are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译： 公开了作为细胞毒性剂有效的式I化合物。 本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症。
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公开(公告)号：US20080249135A1
公开(公告)日：2008-10-09
申请号：US11696526
申请日：2007-04-04
申请人： Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
发明人： Rachel Slade , Yevgeniya Klimova , Robert J. Halter , Ashantai J. Yungai , Warren S. Weiner , Ruth J. Walton , Jon Adam Willardsen , Mark B. Anderson , Kenton Zavitz
IPC分类号： A61K31/44 , A61K31/404 , A61P25/28 , C07D257/04 , C07D401/00 , C07D209/04 , A61K31/41
CPC分类号： C07D209/60 , A61K31/403 , C07D209/08 , C07D209/10 , C07D209/14 , C07D231/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D491/10 , C07F7/1804
摘要： The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH, -L-C(═O)NH2, -L-C(═O)NH(C1-3 alkyl), -L-C(═O)N(C1-3 alkyl)2, -L-S(═O)2(C1-3alkyl), -L-S(═O)2NH2, -L-S(═O)2N(C1-3 alkyl)2, -L-S(═O)2NH(C1-3 alkyl), -L-C(═O)NHOH, -L-C(═O)CH2NH2, -L-C(═O)CH2OH, -L-C(═O)CH2SH, -L-C(═O)NHCN, -L-NHC(═O)ORo, -L-C(═O)NHRo, -L-NH(C═O)NHRo, -L-C(═O)N(Ro)2, -L-NH(C═O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
摘要翻译： 本发明提供了可用于治疗包括阿尔茨海默病和痴呆的神经变性疾病的新化合物。 化合物具有选自-LC（-O）OH，-L-CH-CHC（-O）OH，-LC（-O）NH 2，-LC（-O）NH （C 1-3烷基），-LC（-O）N（C 1-3烷基）亚磺酰基，-LS（-O ）2（C 1-3烷基），-LS（-O）2 NH 2，-LS （-O）2 N（C 1-3烷基）2，-LS（-O）2 NH（C 1-3烷基），-LC（-O）NHOH，-LC（-O）CH 2 NH 2 - ， - LC（-O）CH 2 OH，-LC（-O）CH 2 SH，-LC（-O）NHCN，-L-NHC（-O）OR -OC（-O）NHR o，-L-NH（CO）NHR o，-LC（-O）N（ 2-N，R-NH（CO）N（R 0）2 - ， - 磺基，-L-（2,6-二氟苯酚），-L-膦酰基和-L-四唑基，其中L是连接体。
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7.发明授权Derivatives of triterpenoid acids as inhibitors of cell-adhesion molecules ELAM-1 (e-selectin) and LECAM-1 (l-selectin) 失效三萜酸的衍生物作为细胞粘附分子的抑制剂ELAM-1（e-选择蛋白）和LECAM-1（l-选择素）
公开(公告)号：US5624909A
公开(公告)日：1997-04-29
申请号：US468888
申请日：1995-06-06
IPC分类号： G01N33/53 , A61K31/704 , A61K49/00 , A61K51/00 , A61K51/04 , A61P29/00 , C07H15/18 , C07H15/203 , C07H15/207 , C07H15/24 , C07H15/256 , C07H17/04 , C07J63/00 , A01N37/00 , A01N39/00 , A61K31/00 , A61K31/56
CPC分类号： C07J63/008 , A61K51/04 , C07H15/18 , C07H15/203 , C07H15/24 , C07H15/256 , C07H17/04 , A61K2121/00
摘要： Triterpenoid acid derivatives have been found to have structures similar to natural ligands to the extent that these derivatives bind to natural selectin receptors including endothelial leukocyte adhesion molecule-1 (ELAM-1) and leukocyte/endothelial cell adhesion molecule-1 (LECAM-1). The molecules can be administered to the patients by themselves or in pharmaceutical formulations in order to alleviate inflammation and/or treat other abnormalities associated with the excessive binding of leukocytes to endothelial receptors.
摘要翻译： 已经发现三萜酸衍生物具有与天然配体相似的结构，使得这些衍生物与天然选择素受体结合，包括内皮白细胞粘附分子-1（ELAM-1）和白细胞/内皮细胞粘附分子-1（LECAM-1） 。 分子可以自己或以药物制剂施用于患者，以减轻炎症和/或治疗与白细胞与内皮受体的过度结合相关的其它异常。
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公开(公告)号：US08309562B2
公开(公告)日：2012-11-13
申请号：US12500863
申请日：2009-07-10
申请人： Mark B. Anderson , J. Adam Willardsen , Warren S. Weiner , Ashantai Yungai , Robert J. Halter , Yevgeniya Klimova , Kazuyuki Suzuki , Matthew Reeder
发明人： Mark B. Anderson , J. Adam Willardsen , Warren S. Weiner , Ashantai Yungai , Robert J. Halter , Yevgeniya Klimova , Kazuyuki Suzuki , Matthew Reeder
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72
CPC分类号： C07D239/94 , C07D239/95 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D487/04
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译： 公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。 本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症。
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公开(公告)号：US08258145B2
公开(公告)日：2012-09-04
申请号：US11773285
申请日：2007-07-03
IPC分类号： A61K31/517 , A61K31/535 , A61K31/47
CPC分类号： A61K31/4709 , A61K31/517 , A61K31/5377
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer.
摘要翻译： 公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。 本发明的化合物可用于治疗发生异常细胞的不受控制的生长和扩散的各种临床病症，特别是这些化合物在治疗脑癌中的用途。
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10.发明授权4-arylamin-or-4-heteroarylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效4-芳基氨基 - 或 - 4-杂芳基氨基 - 喹唑啉及其类似物作为胱天蛋白酶的活化剂和凋亡诱导剂及其用途公开(公告)号：US07989462B2
公开(公告)日：2011-08-02
申请号：US11773303
申请日：2007-07-03
申请人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma , Hong Zhang , Kazuyuki Suzuki
发明人： Sui Xiong Cai , Mark B. Anderson , Adam Willardsen , Nilantha Sudath Sirisoma , Hong Zhang , Kazuyuki Suzuki
IPC分类号： A01N43/90 , A61K31/519 , C07D401/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D239/02
CPC分类号： C07D239/94 , C07D239/72 , C07D403/12
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译： 公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。 本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症。
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