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41. 发明授权

US07354928B2 Small molecule inhibitors targeted at Bcl-2 有权
标题翻译：针对Bcl-2的小分子抑制剂
公开(公告)号：US07354928B2
公开(公告)日：2008-04-08
申请号：US10286085
申请日：2002-11-01
申请人： Shaomeng Wang , Dajun Yang , Istvan J. Enyedy
发明人： Shaomeng Wang , Dajun Yang , Istvan J. Enyedy
IPC分类号： A61K31/44 , A61K31/335 , A61K31/135 , A61K31/505 , A61K31/65
CPC分类号： A61K45/06 , A61K31/00 , A61K31/122 , A61K31/395 , A61K31/404 , A61K31/4184 , A61K31/444 , A61K31/452 , A61K31/473 , A61K31/4745 , A61K31/519 , A61K31/655 , A61K2300/00
摘要： The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.
摘要翻译：本发明涉及Bcl-2家族蛋白质如Bcl-2和/或Bcl-X L的小分子拮抗剂。特别地，本发明提供了结合Bcl-2 / Bcl-XLL中的口袋的非肽细胞可渗透的小分子（例如三环二苯并二氮杂二恶英），其阻断抗这些蛋白在癌细胞和表达Bcl-2蛋白过表达的肿瘤组织中的凋亡功能。在优选的实施方案中，本发明的小分子在Bcl-2家族蛋白（例如Bcl-2，Bcl-X L和Mcl-1）的BH3结合口袋上是有活性的。本发明的组合物和方法单独或与化学治疗剂或其它药物组合用于癌性疾病的有用治疗剂。

42. 发明授权

US07342046B2 Gossypol co-crystals and the use thereof 有权
公开(公告)号：US07342046B2
公开(公告)日：2008-03-11
申请号：US11089096
申请日：2005-03-24
申请人： Shaomeng Wang , Jiangyong Chen
发明人： Shaomeng Wang , Jiangyong Chen
IPC分类号： A61K31/225 , A61K31/11 , A61K31/70
CPC分类号： A61K31/11
摘要： This invention relates to compositions comprising co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.

43. 发明申请

US20050131051A1 2-3-disubstituted quinuclidiness as modulators of monoamine transporters and theraperutic and diagnostic methods based thereon 审中-公开
公开(公告)号：US20050131051A1
公开(公告)日：2005-06-16
申请号：US10362164
申请日：2001-08-21
申请人： Shaomeng Wang , Sukumar Sakamuri , Istvan Enyedey , Alan Kozikowski
发明人： Shaomeng Wang , Sukumar Sakamuri , Istvan Enyedey , Alan Kozikowski
IPC分类号： C07D453/02 , A61K31/407 , A61K31/439 , A61K39/00 , A61K47/48 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/36 , A61P43/00 , C07B57/00 , C07D211/52 , C07D487/04 , C07D491/04
CPC分类号： C07D491/04 , C07D211/52 , C07D453/02
摘要： The present invention relates to a class of compounds of formula (I) and (II): wherein R1 is hydrogen; linear or branched C1-C15 alkyl; C1-C15 alkenyl; C3-C6 cycloalkyl; mono, di, tri, tetra, penta substituted aryl or heteroaryl; COOR3; —(CH2)n-aryl; —COO—(CH2)nR3; —(CH2)n—COOR3; —C(O)R3; —C(O)NHR3; or an unsubstituted or substituted oxadiazole; and R2 is hydrogen; linear or branched C1-C15 alkyl; C1-C15 alkenyl; C3-C6 cycloalkyl; mono, di, tri, tetra, penta substituted aryl or heteroaryl; unsubstituted or substituted naphthyl; 1,3-Benzodioxole; fluorene; indole; isoquinoline; quinoline; pyridine; pyrimidine; onnthracene; or —(CH2)n-Ph; wherein the heteroaryl comprises N, O, or S, the mono or multi substituents on the aryl or heteroaryl are independently C1-C5 alkyl, C1-C5 alkenyl, H, F, Cl, Br, I, —NO2, NHR, or —OR, R is C1-C7 alkyl; R3 is C1-C5 alkyl, C1-C5 alkenyl, benzyl, substituted aryl or heteroaryl; and n=1-7. These compounds are discovered, synthesized and confirmed as potent inhibitors of dopamine (DA), serotonin (5-HT), and norepinephrine inhibitors. These compounds are therefore particularly useful in the treatment conditions or diseases wherein modulation of the monoamine neurotransmitter system involving dopamine (DA), serotonin (5-HT), and norepinephrine plays a role.

44. 发明申请

US20120263675A1 BIVALENT DIAZO BICYCLIC SMAC 有权
公开(公告)号：US20120263675A1
公开(公告)日：2012-10-18
申请号：US13503366
申请日：2010-10-20
申请人： Shaomeng Wang , Haiying Sun
发明人： Shaomeng Wang , Haiying Sun
IPC分类号： A61K31/4184 , A61K31/437 , A61K31/52 , A61K31/423 , A61K31/428 , A61K31/427 , C12N5/071 , A61K38/19 , A61K38/17 , A61K39/395 , A61P35/00 , A61P27/02 , A61P29/00 , A61P19/02 , A61P17/06 , A61P9/10 , A61P27/06 , A61P9/00 , A61P1/00 , A61P17/00 , A61P17/02 , A61M37/00 , C07D487/04
CPC分类号： C07D519/00 , C07D487/04
摘要： The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.
摘要翻译：本发明涉及通过共价接头连接以产生二价物质的重氮二环Smac模拟物。二价重氮双环Smac模拟物作为细胞凋亡蛋白抑制剂（IAP）的抑制剂起作用。本发明还涉及二价重氮二环Smac模拟物用于诱导或致敏细胞诱导凋亡细胞死亡的用途。因此，本发明的化合物可用于治疗，改善或预防过度增殖性疾病如癌症。

45. 发明申请

US20110184033A1 Selective Ligands for the Dopamine 3 (D3) Receptor and Methods of using the Same 有权
标题翻译：多巴胺3（D3）受体的选择性配体及其使用方法
公开(公告)号：US20110184033A1
公开(公告)日：2011-07-28
申请号：US13060306
申请日：2009-08-27
申请人： Shaomeng Wang , Jianyong Chen , Gregory Collins , James H. Woods , Beth Levant
发明人： Shaomeng Wang , Jianyong Chen , Gregory Collins , James H. Woods , Beth Levant
IPC分类号： A61K31/427 , C07D277/82 , A61P25/28 , A61P25/08 , A61P25/30 , A61P25/22
CPC分类号： C07D277/82 , C07D417/12
摘要： Potent and selective ligands for the dopamine 3 (D3) receptor are disclosed. The D3 receptor ligands have a structural formula (I) wherein X is C═O or SO2, R1 is C1-6 alkyl, R2 is aryl, heteroaryl, aryl, —(CH2)1-3aryl, or —(CH2)1-3heteroaryl, and n is 0 or 1. Methods of using the D3 receptor ligands in the treatment of diseases and conditions wherein modulation of the D3 receptor provides a benefit also are disclosed.
摘要翻译：公开了多巴胺3（D3）受体的有效和选择性配体。 D3受体配体具有结构式（I），其中X为C = O或SO 2，R 1为C 1-6烷基，R 2为芳基，杂芳基，芳基， - （CH 2）1-3芳基或 - （CH 2） 3杂芳基，n为0或1.D3受体配体在治疗其中D3受体的调节提供益处的疾病和病症方面也被公开。

46. 发明申请

US20090082445A1 GOSSYPOL CO-CRYSTALS AND THE USE THEREOF 审中-公开
标题翻译： GOSSYPOL CO晶体及其用途
公开(公告)号：US20090082445A1
公开(公告)日：2009-03-26
申请号：US12242419
申请日：2008-09-30
申请人： Shaomeng Wang , Jianyong Chen
发明人： Shaomeng Wang , Jianyong Chen
IPC分类号： A61K31/19 , A61P35/00
CPC分类号： A61K31/11
摘要： This invention relates to compositions comprising co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid which are useful as inhibitors of Bcl-2 family proteins. The invention also relates to the use of co-crystals of (−)-gossypol with a C1-8 carboxylic acid or C1-8 sulfonic acid for inducing apoptosis in cells and for sensitizing cells to the induction of apoptotic cell death.
摘要翻译：本发明涉及包含（ - ） - 棉酚与C 1-8羧酸或C 1-8磺酸的共晶体的组合物，其可用作Bcl-2家族蛋白质的抑制剂。本发明还涉及（ - ） - 棉酚与C 1-8羧酸或C 1-8磺酸的共晶体在细胞中诱导细胞凋亡和促使细胞诱导凋亡细胞死亡的用途。

47. 发明申请

US20090082424A1 SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS 审中-公开
标题翻译： BCL-2家族蛋白的小分子拮抗剂
公开(公告)号：US20090082424A1
公开(公告)日：2009-03-26
申请号：US12242388
申请日：2008-09-30
申请人： Shaomeng Wang , Dajun Yang , Liang Xu
发明人： Shaomeng Wang , Dajun Yang , Liang Xu
IPC分类号： A61K31/11 , A61K31/337 , A61P35/02 , A61P35/04 , A61P35/00
CPC分类号： A61K31/11 , A61K45/06 , A61K2300/00
摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.
摘要翻译：本发明涉及Bcl-2家族蛋白质的天然存在和化学合成的小分子拮抗剂。特别地，本发明提供了棉酚化合物（例如异构体，对映异构体，外消旋化合物，代谢物，衍生物，药学上可接受的盐，与酸或碱的组合等）和使用这些化合物作为抗 - Bcl-2家族蛋白（如Bcl-2，Bcl-XL等）的凋亡作用。本发明还提供包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）的组合物。本发明还提供了治疗疾病和病症（例如，肿瘤疾病）的方法，包括施用包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）和/或技术（例如，放射疗法，外科手术等）到受试者或体外细胞，组织和器官。

48. 发明申请

US20080248566A1 MATRIPTASE, A SERINE PROTEASE AND ITS APPLICATIONS 有权
标题翻译： MATRIPTASE，丝氨酸蛋白酶及其应用
公开(公告)号：US20080248566A1
公开(公告)日：2008-10-09
申请号：US12040467
申请日：2008-02-29
申请人： Robert B. Dickson , Chen-Yong Lin , Michael Johnson , Shaomeng Wang , Istvan Enyedy
发明人： Robert B. Dickson , Chen-Yong Lin , Michael Johnson , Shaomeng Wang , Istvan Enyedy
IPC分类号： C12N5/06 , C12N15/11 , C12N15/00
CPC分类号： A61K49/0039 , A61K38/00 , A61K49/0056 , A61K49/0058 , A61K51/10 , C12Q1/37 , G01N33/573 , G01N2333/96433 , G01N2500/20
摘要： The invention is directed to a method of detecting a malignancy or a pre-malignant lesion in breast or other tissue, or a pathologic condition, by detecting the presence of single-chain or two-chain forms of matriptase in the tissue. The invention is further directed to a method of treating malignancies, which have the phenotype of matriptase production by administering a tumor formation inhibiting effective amount of concentrate of Bowman-Birk inhibitor (BBIC), or other matriptase inhibitor. The invention also is directed to nucleic acids encoding a matriptase protein or fragments thereof, and their use for structure elucidation and modeling to identify other inhibitors of matriptase, as well as to methods of identifying matriptase modulating agents, including activators and inhibitors.
摘要翻译：本发明涉及通过检测组织中单链或双链形式的matriptase的存在来检测乳腺或其他组织或病理状况中的恶性肿瘤或恶性前病变的方法。本发明进一步涉及通过施用抑制有效量的Bowman-Birk抑制剂（BBIC）浓缩物或其它片剂酶抑制剂的肿瘤形成来治疗恶性肿瘤的方法，所述恶性肿瘤具有基质酶产生的表型。本发明还涉及编码matriptase蛋白质或其片段的核酸，以及其用于结构阐明和建模以鉴定其它抑制剂的用途，以及鉴定片段酶调节剂（包括活化剂和抑制剂）的方法。

49. 发明授权

US07432304B2 Small molecule antagonists of Bcl-2 family proteins 有权
标题翻译： Bcl-2家族蛋白的小分子拮抗剂
公开(公告)号：US07432304B2
公开(公告)日：2008-10-07
申请号：US10729156
申请日：2003-12-05
申请人： Shaomeng Wang , Dajun Yang , Liang Xu
发明人： Shaomeng Wang , Dajun Yang , Liang Xu
IPC分类号： A61K31/12
CPC分类号： A61K31/11 , A61K45/06 , A61K2300/00
摘要： The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-XL, and the like). The present invention also provides compositions comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents). The present invention also provides methods for treating diseases and pathologies (e.g., neoplastic diseases) comprising administering a composition comprising gossypol compounds and optionally one or more additional therapeutic agents (e.g., anticancer/chemotherapeutic agents) and/or techniques (e.g., radiation therapies, surgical interventions, and the like) to a subject or in vitro cells, tissues, and organs.
摘要翻译：本发明涉及Bcl-2家族蛋白质的天然存在和化学合成的小分子拮抗剂。特别地，本发明提供了棉酚化合物（例如异构体，对映异构体，外消旋化合物，代谢物，衍生物，药学上可接受的盐，与酸或碱的组合等）和使用这些化合物作为抗 - Bcl-2家族蛋白（例如Bcl-2，Bcl-XL等）的凋亡作用。本发明还提供包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）的组合物。本发明还提供了治疗疾病和病症（例如，肿瘤疾病）的方法，包括施用包含棉酚化合物和任选的一种或多种另外的治疗剂（例如抗癌/化学治疗剂）和/或技术的组合物（例如，放射疗法，外科手术等）到受试者或体外细胞，组织和器官。

50. 发明申请

US20080058322A1 Small molecule inhibitors targeted at Bcl-2 审中-公开
公开(公告)号：US20080058322A1
公开(公告)日：2008-03-06
申请号：US11811019
申请日：2007-06-08
申请人： Shaomeng Wang , Dajun Yang , Istvan Enyedy
发明人： Shaomeng Wang , Dajun Yang , Istvan Enyedy
IPC分类号： A61K31/12 , A61K31/33 , A61K31/40 , A61K31/44 , A61K31/535 , A61P43/00
CPC分类号： A61K45/06 , A61K31/00 , A61K31/122 , A61K31/395 , A61K31/404 , A61K31/4184 , A61K31/444 , A61K31/452 , A61K31/473 , A61K31/4745 , A61K31/519 , A61K31/655 , A61K2300/00
摘要： The present invention relates to small molecule antagonists of Bcl-2 family proteins such as Bcl-2 and/or Bcl-XL. In particular, the present invention provides non-peptide cell permeable small molecules (e.g., tricyclo-dibenzo-diazocine-dioxides) that bind to a pocket in Bcl-2/Bcl-XL that block the anti-apoptotic function of these proteins in cancer cells and tumor tissues exhibiting Bcl-2 protein overexpression. In preferred embodiments, the small molecules of the present invention are active at the BH3 binding pocket of Bcl-2 family proteins (e.g., Bcl-2, Bcl-XL, and Mcl-1). The compositions and methods of the present invention are useful therapeutics for cancerous diseases either alone or in combination with chemotherapeutic or other drugs.

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