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1. 发明申请

US20060198832A1 Peptide drugs for chronic lymphocytic leukemia (CLL) and other cancers 审中-公开
标题翻译：用于慢性淋巴细胞白血病（CLL）和其他癌症的肽药物
公开(公告)号：US20060198832A1
公开(公告)日：2006-09-07
申请号：US11267828
申请日：2005-11-03
申请人： Arnold Satterthwait , Xiuwen Zhu , Shinichi Kitada , John Reed
发明人： Arnold Satterthwait , Xiuwen Zhu , Shinichi Kitada , John Reed
IPC分类号： A61K38/54 , C12N9/99
CPC分类号： C07K14/4702 , A61K38/00 , C07K2319/01
摘要： The present invention provides a modified BAD peptide or peptidomimetic which includes an amino acid sequence having at least 60% amino acid identity with SEQ ID NO: 1, where the modified BAD peptide or peptidomimetic has enhanced affinity for Bcl-2 as compared to wild type BAD peptide (SEQ ID NO: 1). Further provided herein is a composition containing a delivery agent and a modified BAD peptide or peptidomimetic which includes an amino acid sequence having at least 60% amino acid identity with SEQ ID NO: 1, where the modified BAD peptide or peptidomimetic has enhanced affinity for Bcl-2 as compared to wild type BAD peptide (SEQ ID NO: 1).
摘要翻译：本发明提供了一种修饰的BAD肽或肽模拟物，其包括与SEQ ID NO：1具有至少60％氨基酸同一性的氨基酸序列，其中与野生型相比，修饰的BAD肽或肽模拟物对Bcl-2具有增强的亲和力 BAD肽（SEQ ID NO：1）。本文进一步提供的是含有递送剂和修饰的BAD肽或肽模拟物的组合物，其包含与SEQ ID NO：1具有至少60％氨基酸同一性的氨基酸序列，其中修饰的BAD肽或肽模拟物对Bcl具有增强的亲和力 -2与野生型BAD肽（SEQ ID NO：1）相比。

2. 发明申请

US20130157260A1 IDENTIFICATION OF COMPOUNDS THAT REGULATE APOPTOSIS 审中-公开
标题翻译：化合物的鉴定
公开(公告)号：US20130157260A1
公开(公告)日：2013-06-20
申请号：US12959054
申请日：2010-12-02
申请人： Arnold Satterthwait , Xiao-kun Zhang , Xiuwen Zhu , Siva Kolluri , John C. Reed
发明人： Arnold Satterthwait , Xiao-kun Zhang , Xiuwen Zhu , Siva Kolluri , John C. Reed
IPC分类号： G01N33/68
CPC分类号： G01N33/6872 , A61K38/00 , C07K14/4747 , C07K14/70567
摘要： An assay for identifying compounds that affect conversion of Bcl-2 family protein from an antiapoptotic to a proapoptotic form or inhibit activity of Bcl-2 family protein is described.
摘要翻译：描述了用于鉴定影响Bcl-2家族蛋白从抗细胞凋亡转化为促细胞凋亡形式或抑制Bcl-2家族蛋白活性的化合物的测定法。

3. 发明申请

US20070054863A1 Compounds that regulate apoptosis 失效
标题翻译：调节细胞凋亡的化合物
公开(公告)号：US20070054863A1
公开(公告)日：2007-03-08
申请号：US11433783
申请日：2006-05-11
申请人： Arnold Satterthwait , Xiao-kun Zhang , Xiuwen Zhu , Siva Kolluri
发明人： Arnold Satterthwait , Xiao-kun Zhang , Xiuwen Zhu , Siva Kolluri
IPC分类号： A61K38/10 , A61K38/08 , C07K7/06 , C07K7/08
CPC分类号： G01N33/6872 , A61K38/00 , C07K14/4747 , C07K14/70567
摘要： Compounds that modulate the function of anti-apoptotic proteins such as Bcl-2 and related Bcl-2 family members are identified. These compounds have the ability to convert the activity of Bcl-2-family member proteins from anti-apoptotic to pro-apoptotic. Methods for inducing or preventing apoptosis are described, together with methods for identifying molecules that induce or prevent apoptosis through interaction with Bcl-2-family members. Methods for treatment of proliferative diseases and neurodegenerative diseases using the modulators of Bcl-2 and related family members are also disclosed.
摘要翻译：鉴定了调节抗凋亡蛋白如Bcl-2和相关Bcl-2家族成员功能的化合物。这些化合物具有将Bcl-2家族成员蛋白的活性从抗凋亡转化为促凋亡的能力。描述诱导或预防凋亡的方法，以及用于鉴定通过与Bcl-2家族成员相互作用诱导或预防凋亡的分子的方法。还公开了使用Bcl-2和相关家族成员的调节剂治疗增殖性疾病和神经变性疾病的方法。

4. 发明申请

US20100292145A1 METHODS OF REGULATING APOPTOSIS 审中-公开
标题翻译：调节疫苗的方法
公开(公告)号：US20100292145A1
公开(公告)日：2010-11-18
申请号：US12815893
申请日：2010-06-15
申请人： Arnold Satterthwait , Xiao-kun Zhang , Xiuwen Zhu , Siva Kolluri
发明人： Arnold Satterthwait , Xiao-kun Zhang , Xiuwen Zhu , Siva Kolluri
IPC分类号： A61K38/18 , C12N5/071 , A61P35/00
CPC分类号： G01N33/6872 , A61K38/00 , C07K14/4747 , C07K14/70567
摘要： Compounds that modulate the function of anti-apoptotic proteins such as Bcl-2 and related Bcl-2 family members are identified. These compounds have the ability to convert the activity of Bcl-2-family member proteins from anti-apoptotic to pro-apoptotic. Methods for inducing or preventing apoptosis are described, together with methods for identifying molecules that induce or prevent apoptosis through interaction with Bcl-2-family members. Methods for treatment of proliferative diseases and neurodegenerative diseases using the modulators of Bcl-2 and related family members are also disclosed.
摘要翻译：鉴定了调节抗凋亡蛋白如Bcl-2和相关Bcl-2家族成员功能的化合物。这些化合物具有将Bcl-2家族成员蛋白的活性从抗凋亡转化为促凋亡的能力。描述诱导或预防凋亡的方法，以及用于鉴定通过与Bcl-2家族成员相互作用诱导或预防凋亡的分子的方法。还公开了使用Bcl-2和相关家族成员的调节剂治疗增殖性疾病和神经变性疾病的方法。

5. 发明授权

US07745574B2 Compounds that regulate apoptosis 失效
标题翻译：调节细胞凋亡的化合物
公开(公告)号：US07745574B2
公开(公告)日：2010-06-29
申请号：US11433783
申请日：2006-05-11
申请人： Arnold Satterthwait , Xiao-kun Zhang , Xiuwen Zhu , Siva Kolluri
发明人： Arnold Satterthwait , Xiao-kun Zhang , Xiuwen Zhu , Siva Kolluri
IPC分类号： C07K14/00 , A61K38/16
CPC分类号： G01N33/6872 , A61K38/00 , C07K14/4747 , C07K14/70567
摘要： Compounds that modulate the function of anti-apoptotic proteins such as Bcl-2 and related Bcl-2 family members are identified. These compounds have the ability to convert the activity of Bcl-2-family member proteins from anti-apoptotic to pro-apoptotic. Methods for inducing or preventing apoptosis are described, together with methods for identifying molecules that induce or prevent apoptosis through interaction with Bcl-2-family members. Methods for treatment of proliferative diseases and neurodegenerative diseases using the modulators of Bcl-2 and related family members are also disclosed.
摘要翻译：鉴定了调节抗凋亡蛋白如Bcl-2和相关Bcl-2家族成员功能的化合物。这些化合物具有将Bcl-2家族成员蛋白的活性从抗凋亡转化为促凋亡的能力。描述诱导或预防凋亡的方法，以及用于鉴定通过与Bcl-2家族成员相互作用诱导或预防凋亡的分子的方法。还公开了使用Bcl-2和相关家族成员的调节剂治疗增殖性疾病和神经变性疾病的方法。

6. 发明申请

US20110130409A1 SUBSTITUTED 1,2,3,4-TETRAHYDROCYCLOPENTA[B]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 有权
标题翻译：取代的1,2,3,4-四氢环戊二烯并[B]吲哚-3-基）乙酸衍生物用于治疗自身免疫和炎症性疾病
公开(公告)号：US20110130409A1
公开(公告)日：2011-06-02
申请号：US13055333
申请日：2009-07-22
申请人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
发明人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Brett Ullman , Jeanne V. Moody , Xiuwen Zhu , Scott Stirn
IPC分类号： A61K31/497 , C07D209/94 , C07D403/12 , C07D401/12 , C07D417/12 , A61K31/403 , A61K31/4439 , A61K31/433 , A61P37/06 , A61P29/00 , A61P35/00 , A61P17/06 , A61P25/28 , A61P3/10 , A61P1/00 , A61P17/10 , A61P31/00 , A61P31/12
CPC分类号： C07D209/94 , A61K31/137 , A61K31/198 , A61K31/404 , A61K31/433 , A61K31/4439 , A61K31/497 , C07C211/27 , C07C229/26 , C07C255/03 , C07C279/14 , C07D209/70 , C07D209/88 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , Y02A50/475
摘要： The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
摘要翻译：本发明涉及式（Ia）的某些取代的1,2,3,4-四氢环戊并[b]吲哚-3-基）乙酸衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为激动剂的S1P1受体。本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗S1P1受体相关疾病例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应的方法，多发性硬化症，系统性红斑狼疮，溃疡性结肠炎，I型糖尿病，痤疮，微生物感染或疾病以及病毒感染或疾病。

7. 发明授权

US09597340B2 Cannabinoid receptor modulators 有权
公开(公告)号：US09597340B2
公开(公告)日：2017-03-21
申请号：US14001132
申请日：2012-02-24
申请人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/4439 , A61K31/675 , A61K31/416 , A61K45/06 , A61K31/497
CPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K2300/00
摘要： Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;

8. 发明申请

US20150126477A1 CANNABINOID RECEPTOR MODULATORS 有权
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20150126477A1
公开(公告)日：2015-05-07
申请号：US14001132
申请日：2012-02-24
申请人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/675 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K31/416
CPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K2300/00
摘要： Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;
摘要翻译：提供某些方法可用于治疗癌症，包括施用式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性;

9. 发明申请

US20140066369A1 Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto 审中-公开
标题翻译： GPR119受体的调节剂和与之相关的疾病的治疗
公开(公告)号：US20140066369A1
公开(公告)日：2014-03-06
申请号：US14112384
申请日：2012-04-18
申请人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Dawei Yue , Xiuwen Zhu
发明人： Robert M. Jones , Daniel J. Buzard , Sangdon Han , Sun Hee Kim , Juerg Lehmann , Dawei Yue , Xiuwen Zhu
IPC分类号： C07D295/205 , A61K45/06 , C07D239/42 , A61K31/506 , A61K31/496 , A61K31/499 , C07D249/08 , C07D403/12 , C07D257/04 , C07D487/08 , A61K31/4995 , C07D241/38 , A61K31/495 , C07D271/07
CPC分类号： C07D295/205 , A61K31/495 , A61K31/496 , A61K31/499 , A61K31/4995 , A61K31/506 , A61K45/06 , C07D207/325 , C07D213/68 , C07D213/71 , C07D213/85 , C07D231/12 , C07D233/60 , C07D239/34 , C07D239/42 , C07D241/04 , C07D241/08 , C07D241/38 , C07D249/06 , C07D249/08 , C07D249/10 , C07D257/04 , C07D271/06 , C07D271/07 , C07D295/21 , C07D295/26 , C07D305/08 , C07D401/12 , C07D403/12 , C07D471/08 , C07D487/08
摘要： The present invention relates to compounds of Formula I and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as single pharmaceutical agents or in combination with one or more additional pharmaceutical agents, such as, a DPP-IV inhibitor, a biguanide, an alpha-glucosidase inhibitor, an insulin analogue, a sulfonylurea, an SGLT2 inhibitor, a meglitinide, a thiazolidinedione, or an anti-diabetic peptide analogue, in the treatment of for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a condition characterized by low bone mass; a neurological disorder; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.
摘要翻译：本发明涉及式I化合物及其药学上可接受的盐，溶剂合物和水合物，其可用作单一药剂或与一种或多种另外的药剂组合使用，例如DPP-IV抑制剂，双胍类， α-葡糖苷酶抑制剂，胰岛素类似物，磺酰脲类，SGLT2抑制剂，氯噻嗪，噻唑烷二酮或抗糖尿病肽类似物，在治疗中例如选自：GPR119-受体相关病症 ; 通过增加血液肠降血糖水平来改善病情; 以低骨量为特征的病症; 神经障碍代谢相关疾病; 2型糖尿病; 肥胖; 和相关的并发症。

10. 发明申请

US20130165412A1 CANNABINOID RECEPTOR MODULATORS 有权
标题翻译： CANNABINOID受体调节剂
公开(公告)号：US20130165412A1
公开(公告)日：2013-06-27
申请号：US13616918
申请日：2012-09-14
申请人： Robert M. Jones , Sangdon Han , Lars Thoresen , Jae-Kyu Jung , Sonja Strah-Pleynet , Xiuwen Zhu , Yifeng Xiong , Dawei Yue
发明人： Robert M. Jones , Sangdon Han , Lars Thoresen , Jae-Kyu Jung , Sonja Strah-Pleynet , Xiuwen Zhu , Yifeng Xiong , Dawei Yue
IPC分类号： C07F9/6558 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D231/54 , C07D403/04
CPC分类号： C07D231/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07F9/65583
摘要： The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.
摘要翻译：本发明涉及某些式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性。本发明还涉及某些式Ia化合物及其药物组合物，其调节CB1受体和CB2受体的活性。本发明的化合物及其药物组合物涉及可用于治疗以下疼痛的方法：疼痛，例如骨和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛疼痛，炎性疼痛，神经性疼痛，疼痛发生于与骨关节炎相关的治疗和疼痛的不利影响; 痛觉过敏异常性疼痛炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受骨质疏松症多发性硬化相关性痉挛状态; 自身免疫性疾病过敏反应; CNS炎症; 动脉粥样硬化不良免疫细胞活性和炎症; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化和帕金森病。

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