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1. 发明授权

US09062059B2 Pyrimidine PDE10 inhibitors 有权
标题翻译：嘧啶PDE10抑制剂
公开(公告)号：US09062059B2
公开(公告)日：2015-06-23
申请号：US14239603
申请日：2012-08-20
申请人： Christopher D. Cox , Vadim Y. Dudkin , Jeffrey Kern , Mark E. Layton , Izzat T. Raheem
发明人： Christopher D. Cox , Vadim Y. Dudkin , Jeffrey Kern , Mark E. Layton , Izzat T. Raheem
IPC分类号： C07D487/04 , C07D239/47 , C07D401/14 , C07D417/14 , A61K31/506
CPC分类号： C07D487/04 , A61K31/506 , C07D239/47 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂的嘧啶化合物。本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。

2. 发明授权

US07247625B2 6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators 失效
标题翻译： 6-氨基-1,4-二氢 - 苯并[d] [1,3]恶嗪-2-酮和可用作孕酮受体调节剂的类似物
公开(公告)号：US07247625B2
公开(公告)日：2007-07-24
申请号：US10946476
申请日：2004-09-21
申请人： Puwen Zhang , Jeffrey Kern
发明人： Puwen Zhang , Jeffrey Kern
IPC分类号： C07D265/18 , A61K31/537 , A61K31/536
CPC分类号： A61K31/538 , A61K31/517 , C07D265/18
摘要： Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.
摘要翻译：提供具有式I结构的化合物。在式I中，R 1是H，OH，取代或未取代的C 1至C 3烷基，C 1或N 2 C 3至C 3全氟烷基或COR 6; R 6是H，取代或未取代的C 1至C 4烷基，芳基，取代或未取代的C 1〜至C 4烷氧基，取代或未取代的C 1至C 3氨基烷基; R 2和R 3均为H，取代或未取代的C 1至C 6烷基，C 1至C 6烷基， C 6至C 6全氟烷基，取代或未取代的C 2至C 6链烯基，取代或未取代的C 2，取代或未取代的C 3至C 6环烷基，取代或未取代的芳基或取代或未取代的杂环基; 或R 2和R 3 3稠合形成螺环; R 4是NHR 7，OR 7，NHSO 2 R 7，或 OSO 2 R 7; Q是O，S，NR 8或CR 9 R 10; 或其药学上可接受的盐，酯或前药。这些化合物可用作孕酮受体调节剂和用于治疗孕酮受体相关病症。

3. 发明申请

US20070066675A1 5-Aryl-indan-1-one and analogs useful as progesterone receptor modulators 失效
标题翻译：可用作孕酮受体调节剂的5-芳基 - 茚满-1-酮和类似物
公开(公告)号：US20070066675A1
公开(公告)日：2007-03-22
申请号：US11522862
申请日：2006-09-18
申请人： Puwen Zhang , Jeffrey Kern , Eugene Terefenko , Eugene Trybulski
发明人： Puwen Zhang , Jeffrey Kern , Eugene Terefenko , Eugene Trybulski
IPC分类号： C07D333/22 , C07D207/30 , A61K31/40 , A61K31/381
CPC分类号： C07D207/34 , C07D261/08 , C07D333/22 , C07D333/28
摘要： Compounds of formula I or II are provided, wherein R1—R8 are defined herein, and pharmaceutical compositions and kits containing these compounds. Also provides are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I, formula II, or formula III, wherein R2—R4 and R9 are defined herein.
摘要翻译：提供式I或II的化合物，其中R 1 -R 8是本文定义的，以及含有这些化合物的药物组合物和试剂盒。还提供了使用式I，式II或式III化合物诱导避孕，提供激素替代疗法，治疗周期相关症状或治疗或预防良性或恶性肿瘤疾病的方法，其中R 2，本文定义了本文中定义的SUB-R 4和R 9。

4. 发明申请

US20070066628A1 5-Aryl-indan-1-ol and analogs useful as progesterone receptor modulators 审中-公开
标题翻译： 5-芳基 - 茚满-1-醇和可用作孕酮受体调节剂的类似物
公开(公告)号：US20070066628A1
公开(公告)日：2007-03-22
申请号：US11522881
申请日：2006-09-18
申请人： Puwen Zhang , Jeffrey Kern , Eugene Terefenko , Eugene Trybulski
发明人： Puwen Zhang , Jeffrey Kern , Eugene Terefenko , Eugene Trybulski
IPC分类号： A61K31/44 , C07D213/63
CPC分类号： C07D207/34 , C07C255/53 , C07D409/10
摘要： Compounds of formula I are provided, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R3-R5, R10, and R11 are defined herein.
摘要翻译：提供式I化合物，其中R 1〜R 9和n如本文所定义，以及含有这些化合物的药物组合物和试剂盒。还提供了使用式I或式II化合物诱导避孕，提供激素替代疗法，治疗周期相关症状或治疗或预防良性或恶性肿瘤疾病的方法，其中R 3〜本文定义的是5，R 10和R 11。

5. 发明申请

US20140228368A1 PYRIMIDINE PDE10 INHIBITORS 有权
标题翻译： PYRIMIDINE PDE10抑制剂
公开(公告)号：US20140228368A1
公开(公告)日：2014-08-14
申请号：US14239603
申请日：2012-08-20
申请人： Christopher D. Cox , Vadim Y. Dudkin , Jeffrey Kern , Mark E. Layton , Izzat T. Raheem
发明人： Christopher D. Cox , Vadim Y. Dudkin , Jeffrey Kern , Mark E. Layton , Izzat T. Raheem
IPC分类号： C07D487/04 , C07D417/14 , C07D401/14
CPC分类号： C07D487/04 , A61K31/506 , C07D239/47 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂的嘧啶化合物。本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。

6. 发明申请

US20090235674A1 DEMAND DRIVEN ICE MODE SOFTWARE 审中-公开
标题翻译：需求驱动冰模式软件
公开(公告)号：US20090235674A1
公开(公告)日：2009-09-24
申请号：US12051018
申请日：2008-03-19
申请人： Jeffrey Kern , Richard DeVos , William Newton
发明人： Jeffrey Kern , Richard DeVos , William Newton
IPC分类号： F25C5/02 , F25C5/18
CPC分类号： F25C5/20 , F25C2600/04
摘要： This disclosure is related to software that responds to consumer usage patterns in order to create more ice. The developed software monitors ice dispenses rather they are crushed or cubed. When a threshold of the number of dispenses within the preset time period has been met, the freezer enters a high demand mode. During high demand mode, the freezer is commanded to run at a colder temperature for a preset period of time. The method described in this disclosure includes setting a threshold for the number of dispenses within a time interval and detecting the number of dispenses that are related to a trigger's activation. The method continues with sending a signal when the number of dispenses surpasses the threshold within the time interval and taking a corrective action that increases the production of ice when the signal is received.
摘要翻译：本公开涉及响应消费者使用模式以创建更多冰的软件。开发的软件监视冰分配，而不是破碎或立方。当满足预设时间段内的分配次数的阈值时，冷冻机进入高需求模式。在高需求模式下，冷冻机被命令在较冷的温度下运行一段预设的时间。本公开中描述的方法包括在时间间隔内设置分配数量的阈值并检测与触发器的激活相关的分配数量。该方法继续在分配次数超过阈值的时间间隔内发送信号，并采取在收到信号时增加冰的产生的校正动作。

7. 发明申请

US20070148254A1 COMPOSITIONS AND METHODS FOR DELIVERY OF PROTEINS AND ADJUVANTS ENCAPSULATED IN MICROSPHERES 审中-公开
标题翻译：用于递送蛋白质的组合物和方法和在微生物中包埋的调节物
公开(公告)号：US20070148254A1
公开(公告)日：2007-06-28
申请号：US11681036
申请日：2007-03-01
申请人： MARK JOHNSON , Jay Evans , Jeffrey Kern
发明人： MARK JOHNSON , Jay Evans , Jeffrey Kern
IPC分类号： A61K38/17 , B01J13/04 , A61K9/50
CPC分类号： A61K9/1647 , A61K9/1694 , A61K9/5084 , A61K9/5153 , A61K9/5192 , A61K39/0011 , A61K39/04 , A61K39/39 , A61K2039/55555 , A61K2039/55572
摘要： Hydrophobic ion pairing (HIP) is applied to solubilize proteins and/or adjuvants in an organic medium. A polymer is cosolubilized in the medium and microspheres encapsulating the protein and/or adjuvant can be produced by a single emulsion method. Microspheres prepared by this method exhibit low initial burst of the protein and gradual release over time, and elicit a strong and comprehensive immune response. Compositions comprising a protein and an adjuvant co-encapsulated in microspheres are provided.
摘要翻译：疏水性离子配对（HIP）用于在有机介质中溶解蛋白质和/或佐剂。聚合物在培养基中共溶解，并且包封蛋白质和/或佐剂的微球体可以通过单一乳液法制备。通过该方法制备的微球表现出蛋白质的初始爆发和随着时间的推移逐渐释放，并引起强烈和全面的免疫应答。提供了包含蛋白质和辅助包囊在微球体中的佐剂的组合物。

8. 发明申请

US20080119537A1 5-Aryl indan-1 one and analogs useful as progesterone receptor modulators 审中-公开
标题翻译： 5-芳基茚满-1-酮和类似物可用作孕激素受体调节剂
公开(公告)号：US20080119537A1
公开(公告)日：2008-05-22
申请号：US11985808
申请日：2007-11-16
申请人： Puwen Zhang , Jeffrey Kern , Eugene Terefenko , Eugene Trybulski
发明人： Puwen Zhang , Jeffrey Kern , Eugene Terefenko , Eugene Trybulski
IPC分类号： A61K31/40 , C07D207/30 , A61K31/122 , A61P15/18 , C07C49/297
CPC分类号： C07D207/34 , C07D261/08 , C07D333/22 , C07D333/28
摘要： Compounds of formula I or II and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I, formula II, or formula III.
摘要翻译：提供式I或II的化合物和含有这些化合物的药物组合物和试剂盒。还提供了使用式I，式II或式III化合物诱导避孕，提供激素替代疗法，治疗周期相关症状或治疗或预防良性或恶性肿瘤疾病的方法。

9. 发明申请

US20070066637A1 5-Aryl-indan-1-one oximes and analogs useful as progesterone receptor modulators 失效
标题翻译： 5-芳基 - 茚满-1-酮肟和可用作孕酮受体调节剂的类似物
公开(公告)号：US20070066637A1
公开(公告)日：2007-03-22
申请号：US11522688
申请日：2006-09-18
申请人： Puwen Zhang , Jeffrey Kern , Eugene Terefenko , Eugene Trybulski
发明人： Puwen Zhang , Jeffrey Kern , Eugene Terefenko , Eugene Trybulski
IPC分类号： A61K31/4745 , A61K31/403 , C07D209/54 , C07D209/96
CPC分类号： C07D207/416 , C07C251/44 , C07C255/64
摘要： Compounds of formula I, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, providing hormone replacement therapy, treating cycle-related symptoms, or treating or preventing benign or malignant neoplastic disease using the compounds of formula I or formula II, wherein R3-R5, R10, and R11 are defined herein.
摘要翻译：提供其中R 1〜R 9和n在本文中定义的式I化合物，以及含有这些化合物的药物组合物和试剂盒。还提供了使用式I或式II化合物诱导避孕，提供激素替代疗法，治疗周期相关症状或治疗或预防良性或恶性肿瘤疾病的方法，其中R 3〜本文定义的是5，R 10和R 11。

10. 发明申请

US20050085470A1 6-Amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators 失效
标题翻译： 6-氨基-1,4-二氢 - 苯并[d] [1,3]恶嗪-2-酮和可用作孕酮受体调节剂的类似物
公开(公告)号：US20050085470A1
公开(公告)日：2005-04-21
申请号：US10946476
申请日：2004-09-21
申请人： Puwen Zhang , Jeffrey Kern
发明人： Puwen Zhang , Jeffrey Kern
IPC分类号： A61K31/517 , A61K31/538 , C07D265/18 , C07D265/12
CPC分类号： A61K31/538 , A61K31/517 , C07D265/18
摘要： Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or unsubstituted C1 to C4 alkyl, aryl, substituted or unsubstituted C1 to C4 alkoxy, substituted or unsubstituted C1 to C3 aminoalkyl; R2 and R3 are H, substituted or unsubstituted C1 to C6 alkyl, C1 to C6 perfluoroalkyl, substituted or unsubstituted C2 to C6 alkenyl, substituted or unsubstituted C2 to C6 alkynyl, substituted or unsubstituted C3 to C6 cycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic; or R2 and R3 are fused to form spirocyclic rings; R4 is NHR7, OR7, NHSO2R7, or OSO2R7; Q is O, S, NR8, or CR9R10; or a pharmaceutically acceptable salt, ester, or prodrug thereof. Such compounds are useful as progesterone receptor modulators and for treating progesterone receptor related conditions.
摘要翻译：提供具有式I结构的化合物。在式I中，R 1是H，OH，取代或未取代的C 1至C 3烷基，C 1或N 2 C 3至C 3全氟烷基或COR 6; R 6是H，取代或未取代的C 1至C 4烷基，芳基，取代或未取代的C 1〜至C 4烷氧基，取代或未取代的C 1至C 3氨基烷基; R 2和R 3均为H，取代或未取代的C 1至C 6烷基，C 1至C 6烷基， C 6至C 6全氟烷基，取代或未取代的C 2至C 6链烯基，取代或未取代的C 2，取代或未取代的C 3至C 6环烷基，取代或未取代的芳基或取代或未取代的杂环基; 或R 2和R 3 3稠合形成螺环; R 4是NHR 7，OR 7，NHSO 2 R 7，或 OSO 2 R 7; Q是O，S，NR 8或CR 9 R 10; 或其药学上可接受的盐，酯或前药。这些化合物可用作孕酮受体调节剂和用于治疗孕酮受体相关病症。

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