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1. 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。

2. 发明申请

WO2017222930A1 THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：治疗性化合物
公开(公告)号：WO2017222930A1
公开(公告)日：2017-12-28
申请号：PCT/US2017/037895
申请日：2017-06-16
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY , WELSH, William J. , BIRGE, Raymond , KHOLODOVYCH, Vladyslav , PENG, Youyi , COMOLLO, Thomas Walter , KIMANI, Stanley G.
发明人： WELSH, William J. , BIRGE, Raymond , KHOLODOVYCH, Vladyslav , PENG, Youyi , COMOLLO, Thomas Walter , KIMANI, Stanley G.
IPC分类号： A61K31/496 , C07C233/64 , C07D241/04
摘要： Certain compounds of formula I: I and salts including pharmaceutically acceptable salts thereof are disclosed. Also disclosed are 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 using a compound of formula I.
摘要翻译：公开了某些式I的化合物：及其盐，包括其药学上可接受的盐。还公开了包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体和使用式I化合物的治疗方法。

3. 发明申请

WO2004074313A2 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：预测淀粉样纤维蛋白形成和鉴定用作治疗剂和诊断剂的肽的方法
公开(公告)号：WO2004074313A2
公开(公告)日：2004-09-02
申请号：PCT/US2004/004122
申请日：2004-02-13
申请人： UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY , WELSH, William J. , YOON, Sukjoon
发明人： WELSH, William J. , YOON, Sukjoon
IPC分类号： 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它们的适当天然结构的构象转变后逐渐聚集成异常富含b链的结构，通常称为淀粉样蛋白原纤维。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的隐藏序列倾向的方法。本发明具有发现特异性靶向这些序列以预防，治疗和诊断淀粉样蛋白疾病的试剂的应用。本发明提供的肽可用作潜在的治疗剂，称为“b片破碎剂” 能够阻断和/或抑制淀粉状蛋白原纤维形成。这些相同的肽也可以用作淀粉样斑块的诊断剂（或其模板）。本发明还应用于蛋白质工程，用于检测和选择性去除或替换与强b链倾向相关的侵犯序列。

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