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1. 发明申请

US20140171649A1 Methods and Compositions for the Synthesis of Multimerizing Agents 有权
标题翻译：用于合成多聚化试剂的方法和组合物
公开(公告)号：US20140171649A1
公开(公告)日：2014-06-19
申请号：US13981051
申请日：2012-01-26
申请人： Feng Li , Yihan Wang
发明人： Feng Li , Yihan Wang
IPC分类号： C07D211/60 , C07D205/04 , C07C231/02 , C07C51/06 , C07C209/08 , C07D319/06 , C07C235/34
CPC分类号： C07D401/12 , C07B53/00 , C07B2200/07 , C07C51/06 , C07C209/08 , C07C209/62 , C07C209/74 , C07C231/02 , C07C231/18 , C07C235/34 , C07D205/04 , C07D211/60 , C07D319/04 , C07D319/06 , C07C211/15 , C07C211/13 , C07C235/20 , C07C59/64
摘要： The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
摘要翻译：本发明的特征在于用于合成多聚化剂的方法和组合物。制备AP20187的示例性方法可以包括：（a）将2-N，N-二甲基氨基甲基-1,3-二氨基丙烷与AP20792偶联以产生二聚醇AP20793; 和（b）将如此生产的AP20793与API7362耦合以产生AP20187。在具体实施方案中，该方法还包括通过将API7360与甲基-L-哌啶酸或其盐偶联制备API7362的步骤。

2. 发明授权

US08461167B2 Acetylenic heteroaryl compounds 有权
公开(公告)号：US08461167B2
公开(公告)日：2013-06-11
申请号：US12227002
申请日：2007-05-08
申请人： Yihan Wang , Xiaotian Zhu , Rajeswari Sundaramoorthi , Wei-Sheng Huang , Dong Zou , R. Mathew Thomas , Jiwei Qi , Jan Antoinette C. Romero , David C. Dalgarno , William C. Shakespeare , Tomi K. Sawyer , Chester A. Metcalf, III
发明人： Yihan Wang , Xiaotian Zhu , Rajeswari Sundaramoorthi , Wei-Sheng Huang , Dong Zou , R. Mathew Thomas , Jiwei Qi , Jan Antoinette C. Romero , David C. Dalgarno , William C. Shakespeare , Tomi K. Sawyer , Chester A. Metcalf, III
IPC分类号： A01N43/54 , A61K31/505 , C07D239/02
CPC分类号： C07D213/56 , C07D213/73 , C07D213/75 , C07D213/78 , C07D217/14 , C07D217/22 , C07D237/20 , C07D237/28 , C07D239/26 , C07D241/12 , C07D241/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D413/12 , C07D417/12 , C07D471/04
摘要： This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.

3. 发明申请

US20130005738A1 Monocyclic Heteroaryl Compounds 审中-公开
标题翻译：单环杂芳基化合物
公开(公告)号：US20130005738A1
公开(公告)日：2013-01-03
申请号：US13612067
申请日：2012-09-12
申请人： William C. Shakespeare , Wei-Sheng Huang , David C. Dalgarno , Xiaotian Zhu , R. Mathew Thomas , Yihan Wang , Jiwei Qi , Rajeswari Sundaramoorthi , Dong Zou , Chester A. Metcalf, III , Tomi K. Sawyer , Jan Antoinette C. Romero
发明人： William C. Shakespeare , Wei-Sheng Huang , David C. Dalgarno , Xiaotian Zhu , R. Mathew Thomas , Yihan Wang , Jiwei Qi , Rajeswari Sundaramoorthi , Dong Zou , Chester A. Metcalf, III , Tomi K. Sawyer , Jan Antoinette C. Romero
IPC分类号： C07D403/12 , A61P35/00 , C07D417/12 , A61K31/427 , A61K31/496 , A61K31/4178
CPC分类号： C07D231/12 , C07D233/64 , C07D233/90 , C07D277/40 , C07D403/12 , C07D403/14 , C07D417/12 , C07D417/14
摘要： This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及以下通式的化合物：其中可变基团如本文所定义，及其制备和用途。

4. 发明申请

US20120202776A1 PHOSPHORUS DERIVATIVES AS KINASE INHIBITORS 有权
标题翻译：磷酸衍生物作为激酶抑制剂
公开(公告)号：US20120202776A1
公开(公告)日：2012-08-09
申请号：US12736910
申请日：2009-05-21
申请人： Yihan Wang , Wei-Sheng Huang , Shuangying Liu , William C. Shakespeare , R. Mathew Thomas , Jiwei Qi , Feng Li , Xiaotian Zhu , Anna Kohlmann , David C. Dalgarno , Jan Antoinette C. Romero , Dong Zou
发明人： Yihan Wang , Wei-Sheng Huang , Shuangying Liu , William C. Shakespeare , R. Mathew Thomas , Jiwei Qi , Feng Li , Xiaotian Zhu , Anna Kohlmann , David C. Dalgarno , Jan Antoinette C. Romero , Dong Zou
IPC分类号： A61K31/675 , C07F9/6512 , C07F9/6561 , A61P35/00 , C07F9/6509 , C07F9/6521 , C07F9/58 , C07F9/6558 , C07F9/6584
CPC分类号： C07F9/6533 , C07D239/48 , C07F9/58 , C07F9/650905 , C07F9/6512 , C07F9/6521 , C07F9/65218 , C07F9/65583 , C07F9/65586 , C07F9/6561 , C07F9/65616 , C07F9/65685 , C07F9/657172 , C07F9/65846
摘要： The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明的特征在于其中可变基团如本文所定义的通式（I）的化合物及其制备和用途。

5. 发明授权

US08114874B2 Substituted acetylenic imidazo[1,2-B]pyridazine compounds as kinase inhibitors 有权
标题翻译：取代的炔属咪唑并[1,2-B]哒嗪化合物作为激酶抑制剂
公开(公告)号：US08114874B2
公开(公告)日：2012-02-14
申请号：US11644849
申请日：2006-12-22
申请人： Dong Zou , Wei-Sheng Huang , R. Mathew Thomas , Jan Antionette C. Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William C. Shakespeare , Rajeswari Sundaramoorthi , Chester A. Metcalf, III , David C. Dalgarno , Tomi K. Sawyer
发明人： Dong Zou , Wei-Sheng Huang , R. Mathew Thomas , Jan Antionette C. Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William C. Shakespeare , Rajeswari Sundaramoorthi , Chester A. Metcalf, III , David C. Dalgarno , Tomi K. Sawyer
IPC分类号： A61K31/495
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use. In particular, the compounds include embodiments in which Ring T is an imidazo[1,2-b]pyridazine ring system, Rings A and B are each aryl and L1 is —C(O)NR1— or —NR1C(O)—. Uses for the compounds and for compositions containing them include treatment of cancer and other diseases mediated by protein kinases.
摘要翻译：本发明涉及以下通式的化合物：其中可变基团如本文所定义，及其制备和用途。特别地，化合物包括其中环T是咪唑并[1,2-b]哒嗪环体系的实施方案，环A和B各自为芳基且L 1为-C（O）NR 1 - 或-NR 1 C（O） - 。用于化合物和含有它们的组合物的用途包括治疗由蛋白激酶介导的癌症和其它疾病。

6. 发明授权

US09834518B2 Compounds for inhibiting cell proliferation in EGFR-driven cancers 有权
公开(公告)号：US09834518B2
公开(公告)日：2017-12-05
申请号：US13464921
申请日：2012-05-04
申请人： David C. Dalgarno , Wei-Sheng Huang , William C. Shakespeare , Yihan Wang , Xiaotian Zhu
发明人： David C. Dalgarno , Wei-Sheng Huang , William C. Shakespeare , Yihan Wang , Xiaotian Zhu
IPC分类号： C07D239/46 , C07D239/50 , C07D401/12 , C07D403/12 , C07D413/12 , A61K31/4025 , A61K31/444 , A61K31/4523 , A61K31/506 , A61K31/505 , A61K31/538 , A61K31/553 , A61P35/00 , C07D239/48 , C07D405/12
CPC分类号： C07D239/48 , A61K31/4025 , A61K31/444 , A61K31/4523 , A61K31/505 , A61K31/506 , A61K31/538 , A61K31/553 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.

7. 发明授权

US08912330B2 Azaindole derivatives as kinase inhibitors 有权
标题翻译： Azaindole衍生物作为激酶抑制剂
公开(公告)号：US08912330B2
公开(公告)日：2014-12-16
申请号：US12998873
申请日：2009-12-11
申请人： Jiwei Qi , Yihan Wang , Feng Li , William C. Shakespeare , Anna Kohlmann , David C. Dalgarno , Xiaotian Zhu
发明人： Jiwei Qi , Yihan Wang , Feng Li , William C. Shakespeare , Anna Kohlmann , David C. Dalgarno , Xiaotian Zhu
IPC分类号： C07D471/04 , C07D401/14 , A61K31/437 , A61K31/44 , A61P35/00
CPC分类号： A61K31/44 , C07D471/04
摘要： This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及其中可变基团如本文所定义的通式（I）的化合物及其制备和用途。

8. 发明申请

US20120316135A1 Compounds for Inhibiting Cell Proliferation in EGFR-Driven Cancers 有权
标题翻译：用于抑制EGFR驱动的癌细胞增殖的化合物
公开(公告)号：US20120316135A1
公开(公告)日：2012-12-13
申请号：US13464921
申请日：2012-05-04
申请人： David C. Dalgarno , Wei-Sheng Huang , William C. Shakespeare , Yihan Wang , Xiaotian Zhu
发明人： David C. Dalgarno , Wei-Sheng Huang , William C. Shakespeare , Yihan Wang , Xiaotian Zhu
IPC分类号： A61K31/675 , C07F9/6558 , C12N5/09 , C07F9/6561 , A61P35/00 , C12N5/071 , C07F9/6512 , C07F9/6509
CPC分类号： C07D239/48 , A61K31/4025 , A61K31/444 , A61K31/4523 , A61K31/505 , A61K31/506 , A61K31/538 , A61K31/553 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.
摘要翻译：本发明的特征在于用于治疗患有EGFR驱动的式I的癌症的患者的化合物，药物组合物和方法：其中变量如本文所定义。

9. 发明申请

US20120135986A1 Bicyclic Heteroaryl Compounds 有权
标题翻译：双环杂芳基化合物
公开(公告)号：US20120135986A1
公开(公告)日：2012-05-31
申请号：US13357745
申请日：2012-01-25
申请人： Dong Zou , Wei-Sheng Huang , R. Mathew Thomas , Jan Antionette C. Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William C. Shakespeare , Rajeswari Sundaramoorthi , Chester A. Metcalf, III , David C. Dalgarno , Tomi K. Sawyer
发明人： Dong Zou , Wei-Sheng Huang , R. Mathew Thomas , Jan Antionette C. Romero , Jiwei Qi , Yihan Wang , Xiaotian Zhu , William C. Shakespeare , Rajeswari Sundaramoorthi , Chester A. Metcalf, III , David C. Dalgarno , Tomi K. Sawyer
IPC分类号： A61K31/5377 , A61K31/4985 , C07D471/04 , A61K31/437 , A61P35/00 , A61K31/5025 , A61K31/53 , A61K31/519 , C07D473/34 , A61K31/52 , C07D487/04 , A61K31/496
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
摘要翻译：本发明涉及以下通式的化合物：其中可变基团如本文所定义，以及其制备和用途。

10. 发明授权

US07709020B2 Implantable device comprising phosphorus-containing macrolides 有权
标题翻译：含有磷的大环内酯类植入装置
公开(公告)号：US07709020B2
公开(公告)日：2010-05-04
申请号：US11650017
申请日：2007-01-05
申请人： David L. Berstein , Leonard W. Rozamus , Yihan Wang , Chester A. Metcalf, III
发明人： David L. Berstein , Leonard W. Rozamus , Yihan Wang , Chester A. Metcalf, III
IPC分类号： A61K31/675 , A61F2/00
CPC分类号： A61K45/06 , A61K31/675 , C07F9/6561
摘要： This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which:A is absent or is —O—, —S— or —NR2—;Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M′ moiety may be saturated or unsaturated; each occurrence of x is independently an integer from 1-6; and the other variables are as defined herein.
摘要翻译：本发明涉及一种含有部分JQA-的含磷化合物的新家族，其中：A不存在或为-O - ， - S-或-NR2-; Q不存在或（如果A是-O-，-S-或-NR2-）Q可以是-V-，-OV-，-SV-或-NR2V-，其中V是脂族，杂脂族，芳基，或杂芳基部分，使得J通过A或通过VA，OVA，SVA或NR2VA直接与环己基环连接; K为O或S; 每个出现的Y独立地是-O - ， - S - ， - NR2-或连接R 5部分与P的键; R 2和R 5各自独立地为脂族，杂脂族，芳基或杂芳基部分，或H; 并且每个出现的R 6独立地是-PK（YR 5）（YR 5），-SO 2（YR 5）或-C（O）（YR 5）; 只要直接与P连接的任何R 2或R 5部分不是H; 其中两个R2，R5和/或R6部分可以彼此化学连接以形成环; 每次出现的G独立为-O - ， - S - ， - NR2-或（M）x; 每次出现的M独立地是取代或未取代的亚甲基部分，任何M-M'部分可以是饱和或不饱和的; 每次出现的x独立为1-6的整数; 其他变量如本文所定义。

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