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1. 发明公开

EP1485088A1 OPIOID RECEPTOR ACTIVE 4-(3-HYDROXYPHENYL) OR 4-(3-ALKOXYPHENYL)-1,2,4-TRIAZOLE COMPOUNDS 有权
标题翻译：阿片受体活性的4-（3-羟基苯基），或4-（3-烷氧基苯基）-1,2,4-三唑化合物
公开(公告)号：EP1485088A1
公开(公告)日：2004-12-15
申请号：EP03737705.8
申请日：2003-02-07
申请人： THE CURATORS OF THE UNIVERSITY OF MISSOURI , Welsh, William J. , Yu, Seong-Jae , Nair, Anil
发明人： WELSH, William, J. , YU, Seong-Jae , NAIR, Anil
IPC分类号： A61K31/41 , C07D249/08 , C07D249/10
CPC分类号： C07D249/08 , A61K31/4196 , C07D249/14
摘要： The invention provides compounds of formula I: wherein R1to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.

2. 发明专利

AU2003210916A1 OPIOID RECEPTOR ACTIVE 4-(3-HYDROXYPHENYL) OR 4-(3-ALKOXYPHENYL)-1,2,4-TRIAZOLE COMPOUNDS 未知
公开(公告)号：AU2003210916A1
公开(公告)日：2003-09-02
申请号：AU2003210916
申请日：2003-02-07
申请人： UNIV MISSOURI , WELSH WILLIAM J , YU SEONG JAE , NAIR ANIL
发明人： WELSH WILLIAM J , YU SEONG-JAE , NAIR ANIL
IPC分类号： A61K31/4196 , A61P1/02 , A61P1/04 , A61P3/04 , A61P3/10 , A61P7/06 , A61P9/10 , A61P11/02 , A61P11/06 , A61P11/08 , A61P15/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D249/08 , C07D249/10 , C07D249/14 , A61K31/41
摘要： The invention provides compounds of formula I: wherein R1 to R4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for treating pain and treating other conditions which involve, for example, binding opioid receptors using compounds of formula I.

3. 发明申请

WO2004074313A8 METHODS FOR PREDICTION OF AMYLOID FIBRIL FORMATION AND IDENTIFICATION OF PEPTIDES USEFUL AS THERAPEUTIC AND DIAGNOSTIC AGENTS 审中-公开
标题翻译：用于预测作为治疗和诊断试剂有效的肽的淀粉样蛋白形成和鉴定的方法
公开(公告)号：WO2004074313A8
公开(公告)日：2004-09-30
申请号：PCT/US2004004122
申请日：2004-02-13
申请人： UNIV NEW JERSEY MED , WELSH WILLIAM J , YOON SUKJOON
发明人： WELSH WILLIAM J , YOON SUKJOON
IPC分类号： C07K20060101 , C07K14/47 , G06F17/00 , G06F17/11 , G06F17/30 , G06F17/50 , G06F19/16 , G06F19/22 , G06F19/24 , C07K
CPC分类号： C07K14/4711 , G06F19/16 , G06F19/22 , G06F19/24
摘要： Protein misfolding is the underlying cause of many unrelated human diseases in which normal correctly folded proteins progressively aggregate after undergoing a conformational transformation from their proper native structure into an abnormal b-strand rich structure commonly known as amyloid fibril. The present invention provides methods for detecting hidden sequence propensity for amyloid fibril formation in any protein. This invention has applications for the discovery of agents that specifically target these sequences for the prevention, treatment, and diagnosis of amyloid diseases. The peptides provided by this invention are useful as potential therapeutic agents called "b-sheet breakers" capable of blocking and/or inhibiting amyloid fibril formation. These same peptides can be also used as diagnostic agents (or templates thereof) of amyloid plaque. This invention also has applications in protein engineering for the detection, and selective removal or replacement, of these offending sequences associated with strong b-strand propensity.
摘要翻译：蛋白质错误折叠是许多不相关的人类疾病的根本原因，其中正常正确折叠的蛋白质在经历从其适当的天然结构进入通常称为淀粉样蛋白原纤维的异常b-链富含结构的构象转化后逐渐聚集。本发明提供了用于检测任何蛋白质中淀粉样蛋白原纤维形成隐藏序列倾向的方法。本发明具有专门针对这些序列用于预防，治疗和诊断淀粉样蛋白病的药剂的发现的应用。本发明提供的肽可用作能够阻断和/或抑制淀粉样蛋白原纤维形成的称为“b-片断片”的潜在治疗剂。这些相同的肽也可以用作淀粉样斑块的诊断剂（或其模板）。本发明还在蛋白质工程中用于检测和选择性去除或替代与强b链倾向相关的这些违规序列。

4. 发明申请

WO2011082044A1 TOPICAL LIGHTENING COMPOSITION AND USES THEREOF 审中-公开
标题翻译：主题亮点组合物及其用途
公开(公告)号：WO2011082044A1
公开(公告)日：2011-07-07
申请号：PCT/US2010/061688
申请日：2010-12-22
申请人： AVON PRODUCTS, INC. , LYGA, John W. , SANTHANAM, Uma , WELSH, William J.
发明人： LYGA, John W. , SANTHANAM, Uma , WELSH, William J.
IPC分类号： A61K31/74
CPC分类号： A61K31/74 , A61K8/46 , A61Q19/02
摘要： The disclosure relates to novel topical lightening compositions a tyrosinase inhibitor and a vehicle. There is provided a topical lightening composition comprising a 2-substituted-thio-4-substitued-4-oxobutanoic acid, ester or amide tyrosinase inhibitor, and a vehicle. The tyrosinase inhibitors of this disclosure can be used as such or as a pharmaceutically acceptable salt including conventional non-toxic salts which include a metal salt or an alkaline earth metal salt, an ammonium salt, or an organic base salt. The tyrosinase inhibitors of this disclosure can be incorporated into any cosmetically-, dermatologically-, or cosmeticatically- acceptable vehicle or carrier normally used for topical application. The compositions and methods of the disclosure are effective to lighten skin, hair, lips, and/or nails.
摘要翻译：本公开涉及新型局部减轻组合物酪氨酸酶抑制剂和载体。提供了包含2-取代 - 硫代-4-取代-4-氧代丁酸，酯或酰胺酪氨酸酶抑制剂和载体的局部减轻组合物。本公开的酪氨酸酶抑制剂可以原样使用或作为药学上可接受的盐使用，包括常规无毒盐，其包括金属盐或碱土金属盐，铵盐或有机碱盐。本公开的酪氨酸酶抑制剂可以并入通常用于局部应用的任何美容，皮肤病学或化妆品可接受的载体或载体中。本公开的组合物和方法有效地减轻皮肤，头发，嘴唇和/或指甲。

5. 发明申请

WO2008064317A1 LIPOPHILIC OPIOID RECEPTOR ACTIVE COMPOUNDS 审中-公开
标题翻译： LIPOPHILIC OPIOID RECEPTOR活性化合物
公开(公告)号：WO2008064317A1
公开(公告)日：2008-05-29
申请号：PCT/US2007/085394
申请日：2007-11-21
申请人： UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY , WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
发明人： WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
IPC分类号： A01N57/00 , A61K31/675
CPC分类号： C07D249/08
摘要： Substituted pyrazoles, imidazoles, triazoles, other 5-membered heteroaromatic ring compounds, substituted 6-membered heteroaromatic ring compounds, and fluorene and carbazole compounds, may be included in pharmaceutical central nervous system drug compositions to treat a condition mediated by an opioid receptor in a patient. Such compounds are designed to possess improved transport across the blood-brain barrier. These compounds possess an optimal combination of high lipophilicity, low polarity, limited conformational flexibility, and few hydrogen bonding groups. Such lipophilic opioid receptor active compounds are useful for treating pain, inflammation, arthritis, central nervous system disorders, and other diseases.
摘要翻译：取代的吡唑，咪唑，三唑，其它5元杂芳环化合物，取代的6元杂芳环化合物，以及芴和咔唑化合物可以包括在药物中枢神经系统药物组合物中，以治疗由阿片受体介导的病症患者。这些化合物被设计成具有穿过血脑屏障的改善的运输。这些化合物具有高亲油性，低极性，有限的构象柔性和少量氢键基团的最佳组合。这样的亲脂性阿片受体活性化合物可用于治疗疼痛，炎症，关节炎，中枢神经系统疾病和其他疾病。

6. 发明申请

WO2006047631A3 ANTI-MITOTIC ANTI-PROLIFERATIVE COMPOUNDS 审中-公开
标题翻译：抗细胞增殖的抗增殖化合物
公开(公告)号：WO2006047631A3
公开(公告)日：2006-08-03
申请号：PCT/US2005038655
申请日：2005-10-25
申请人： UNIV NEW JERSEY MED , WELSH WILLIAM J , PENG YOUYI , WANG XIN , KEENAN SUSAN M , ZHANG QUIANG , ARORA SONIA
发明人： WELSH WILLIAM J , PENG YOUYI , WANG XIN , KEENAN SUSAN M , ZHANG QUIANG , ARORA SONIA
IPC分类号： A61K31/4196 , C07D249/08
CPC分类号： C07D249/08 , C07D403/04
摘要： Substituted triazole compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a pathology linked to a hyperproliferative disorder by administering the substituted triazole compounds to a patient in need thereof.
摘要翻译：提出了取代的三唑化合物及其药物组合物。还提供了通过将所述取代的三唑化合物给予有需要的患者来治疗与过度增殖性疾病相关的病理的方法。

7. 发明申请

WO2005013077A2 SYSTEMS AND METHODS FOR MICROARRAY DATA ANALYSIS 审中-公开
标题翻译：微波数据分析的系统和方法
公开(公告)号：WO2005013077A2
公开(公告)日：2005-02-10
申请号：PCT/US2004024351
申请日：2004-07-29
申请人： UNIV NEW JERSEY MED , WELSH WILLIAM J , OUYANG MING , LIOY PAUL , GEORGOPOULOS PANOS
发明人： WELSH WILLIAM J , OUYANG MING , LIOY PAUL , GEORGOPOULOS PANOS
IPC分类号： G01N33/48 , G06F20060101 , G06F19/20 , G06F19/24 , G06F
CPC分类号： G06F19/20 , G06F19/24 , G06K9/6226
摘要： Clustering is routinely applied in the exploratory analysis of microarray data. Missing entries arise from blemishes on the microarrays. The present invention provides a new method, and computer program and/or computer product thereof to impute missing values. The method involves the steps of clustering microarray data by partitioning the data into a select number of clusters, wherein each data point is iteratively moved from one cluster to another, until two consecutive iterations have resulted in the same partition pattern; obtaining a select number of estimates of the data in the clusters by probabilistic interference; and averaging the select number of estimates to obtain missing values in the microarray data. The method is superior to other imputation models as measured by root mean squared errors.
摘要翻译：在微阵列数据的探索性分析中常规应用聚类。缺少的条目是由微阵列上的瑕疵产生的。本发明提供了一种新的方法，以及计算机程序和/或计算机产品来估算缺失值。该方法包括通过将数据分割成选定数量的簇来聚类微阵列数据的步骤，其中每个数据点被迭代地从一个簇移动到另一簇，直到两个连续的迭代已经得到相同的分区模式; 通过概率干扰获得集群中的数据的选择数量的估计; 并且对所选择的估计数进行平均以获得微阵列数据中的缺失值。该方法优于通过均方根误差测量的其他插补模型。

8. 发明申请

WO2008064310A3 MIXED OPIOID RECEPTOR ACTIVE COMPOUNDS 审中-公开
标题翻译：混合的阿片受体活性化合物
公开(公告)号：WO2008064310A3
公开(公告)日：2008-08-21
申请号：PCT/US2007085384
申请日：2007-11-21
申请人： UNIV NEW JERSEY MED , WELSH WILLIAM J , ARORA SONIA , YANG KAIPEEN
发明人： WELSH WILLIAM J , ARORA SONIA , YANG KAIPEEN
IPC分类号： A61K31/53
CPC分类号： C07D249/10
摘要： Pyrazoles, imidazoles, triazoles, other 5-membered heteroaromatic ring compounds substituted with two phenyl groups, and like compounds, may be included in pharmaceutical compositions to treat a condition mediated by an opioid receptor in a patient. The compounds possess a high binding affinity and high selectivity for delta, kappa and mu opioid receptors. Such mixed opioid receptor active compounds are useful for treating pain, inflammation, arthritis, central nervous system disorders, and other diseases.
摘要翻译：吡唑，咪唑，三唑，被两个苯基取代的其它5元杂芳环化合物和类似化合物可以包括在药物组合物中以治疗患者中由阿片受体介导的病症。该化合物对δ，κ和μ阿片受体具有高结合亲和力和高选择性。这样的混合阿片受体活性化合物可用于治疗疼痛，炎症，关节炎，中枢神经系统疾病和其它疾病。

9. 发明申请

WO2008064310A2 MIXED OPIOID RECEPTOR ACTIVE COMPOUNDS 审中-公开
标题翻译：混合阿片类药物受体活性化合物
公开(公告)号：WO2008064310A2
公开(公告)日：2008-05-29
申请号：PCT/US2007/085384
申请日：2007-11-21
申请人： UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY , WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
发明人： WELSH, William, J. , ARORA, Sonia , YANG, Kaipeen
IPC分类号： A01N43/66
CPC分类号： C07D249/10
摘要： Pyrazoles, imidazoles, triazoles, other 5-membered heteroaromatic ring compounds substituted with two phenyl groups, and like compounds, may be included in pharmaceutical compositions to treat a condition mediated by an opioid receptor in a patient. The compounds possess a high binding affinity and high selectivity for delta, kappa and mu opioid receptors. Such mixed opioid receptor active compounds are useful for treating pain, inflammation, arthritis, central nervous system disorders, and other diseases.
摘要翻译：吡唑类，咪唑类，三唑类，被两个苯基取代的其它5元杂芳族环化合物和类似化合物可包含在药物组合物中以治疗患者中由阿片受体介导的病症。这些化合物对δ，κ和μ阿片受体具有高结合亲和力和高选择性。这种混合的阿片受体活性化合物可用于治疗疼痛，炎症，关节炎，中枢神经系统疾病和其他疾病。

10. 发明申请

WO2004026819A2 OPIATE ANALOGS SELECTIVE FOR THE delta-OPIOID RECEPTOR 审中-公开
标题翻译：对于δ-阿片受体选择性的类比物
公开(公告)号：WO2004026819A2
公开(公告)日：2004-04-01
申请号：PCT/US2003/029455
申请日：2003-09-18
申请人： THE CURATORS OF THE UNIVERSITY OF MISSOURI , WELSH, William, J. , YU, Seong Jae , NAIR, Anil
发明人： WELSH, William, J. , YU, Seong Jae , NAIR, Anil
IPC分类号： C07D
CPC分类号： C07D471/10 , C07D498/08
摘要： Novel compounds which selectively bind to the δ-opioid receptor have been designed. These compounds have greater selectivity, improved water (blood) solubility, and enhanced therapeutic value as analgesics. Because agonists with selectivity for the δ-opioid receptor have shown promise in providing enhanced analgesis without the addictive properties, the compounds of the present invention are better than morphine, naltrindole (NTI), spiroindanyloxymorphone (SIOM), and other known µ-opioid receptor selectors as analgesics.
摘要翻译：设计了选择性结合δ-阿片受体的新型化合物。这些化合物具有更高的选择性，改善了水（血液）的溶解度，并且作为止痛剂具有增强的治疗价值。由于对δ-阿片样物质受体具有选择性的激动剂在提供增强镇痛作用而没有成瘾性质方面表现出希望，本发明化合物优于吗啡，纳曲吲哚（NTI），螺二氢化茚氧基吗啡酮（SIOM）和其他已知的β-阿片样物质受体选择剂作为镇痛剂。

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