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131. 发明申请

US20090226368A1 Androgen-Receptor (AR) Ligands for Use in the Treatment and Diagnosis of AR-Related Pathologies 审中-公开
标题翻译：雄激素受体（AR）配体用于治疗和诊断AR相关病理
公开(公告)号：US20090226368A1
公开(公告)日：2009-09-10
申请号：US12085226
申请日：2006-11-21
申请人： Eyal Mishani , Orit Jacobson , Einat Even-Sapir Weizer
发明人： Eyal Mishani , Orit Jacobson , Einat Even-Sapir Weizer
IPC分类号： A61K51/04 , C07C237/02 , A61K31/16 , C12Q1/02 , A61P5/00 , A61P5/26 , A61P15/00 , A61P35/00 , A61P9/10
CPC分类号： A61K51/04 , C07B2200/05 , C07C237/04 , C07C255/60
摘要： The present invention discloses novel compounds and compositions suitable for the treatment of androgen related pathologies. The invention also provides diagnostic compositions for the diagnosis or monitoring of such androgen pathologies.
摘要翻译：本发明公开了适用于治疗雄激素相关病变的新型化合物和组合物。本发明还提供用于诊断或监测这种雄激素病理学的诊断组合物。

132. 发明申请

US20090076154A1 DEUTERIUM-ENRICHED VORINOSTAT 审中-公开
标题翻译：卓越的VORINOSTAT
公开(公告)号：US20090076154A1
公开(公告)日：2009-03-19
申请号：US12210298
申请日：2008-09-15
申请人： Anthony W. Czarnik
发明人： Anthony W. Czarnik
IPC分类号： A61K31/164 , C07C237/02 , A61P35/00
CPC分类号： C07C259/06 , A61K31/167 , C07B59/001
摘要： The present application describes deuterium-enriched vorinostat, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
摘要翻译：本申请描述了氘富集的伏立诺他胺，其药学上可接受的盐形式，以及使用其的治疗方法。

133. 发明申请

US20070299269A1 Process for converting primary amidoalcohols to amidocarboxylic acids in high yield 审中-公开
公开(公告)号：US20070299269A1
公开(公告)日：2007-12-27
申请号：US11475824
申请日：2006-06-27
申请人： Bijan Harichian
发明人： Bijan Harichian
IPC分类号： C07C237/02
CPC分类号： C07C231/12 , C07C233/47 , C07C233/49
摘要： The invention relates to an improved process for oxidizing a primary amidoalcohol to the corresponding amidocarboxylic acid in high yield.

134. 发明申请

US20070185208A1 Amide compound 有权
标题翻译：酰胺化合物
公开(公告)号：US20070185208A1
公开(公告)日：2007-08-09
申请号：US10591468
申请日：2005-02-21
申请人： Tetsuya Miyajima , Takeshi Ihara , Hiromoto Mizushima
发明人： Tetsuya Miyajima , Takeshi Ihara , Hiromoto Mizushima
IPC分类号： A61K31/16 , C07C237/02
CPC分类号： A61K8/42 , A61Q13/00 , C07C233/05 , Y10S424/05
摘要： A gelling agent having a high ability of gelling an oily base which is capable of giving a gel composition having a strong gel strength and a good transparency, a gel composition having a strong gel strength and a good transparency, an external composition having a good feel upon use, a cosmetic preparation having a good feel upon use, and a fragrance composition having a good transparency and a good appearance is provided. An amide compound represented by the following formula 1: is used. In formula 1, R1, R2 and R3 are each independently a hydrogen atom or an alkyl group having a carbon number of from 1 to 3 with the proviso that at least one of R1, R2 and R3 is a hydrogen atom. R4, R5 and R6 are each independently a saturated or unsaturated, linear or branched hydrocarbon group having a total carbon number of from 6 to 24 which optionally has at least one group selected from the group consisting of an ether group, amide group, ester group, amino group and hydroxyl group; and m, n and p are each independently an integer of from 0 to 3.
摘要翻译：能够赋予凝胶强度高，透明度好的凝胶组合物的油性基胶凝胶化能力强，凝胶强度高，透明度好的凝胶组合物的胶凝剂，感觉良好的外用组合物使用时具有使用感好的化妆品，透明性好，外观美观的香精组合物。使用由下式1表示的酰胺化合物。在式1中，R 1，R 2和R 3各自独立地为氢原子或碳数为1的烷基至3，条件是R 1，R 2和R 3 3中的至少一个为氢原子。 R 4，R 5和R 6各自独立地为具有总碳数为6的饱和或不饱和的直链或支链烃基至24，其任选具有至少一个选自醚基，酰胺基，酯基，氨基和羟基的基团; m，n和p各自独立地为0〜3的整数。

135. 发明申请

US20070004804A1 Polymorphic forms of nateglinide 审中-公开
标题翻译：那格列奈的多形态
公开(公告)号：US20070004804A1
公开(公告)日：2007-01-04
申请号：US11516363
申请日：2006-09-05
申请人： Ronit Yahalomi , Evgeny Shapiro , Ben-Zion Dolitzky , Igal Gozlan , Boaz Gome , Shlomit Wizel
发明人： Ronit Yahalomi , Evgeny Shapiro , Ben-Zion Dolitzky , Igal Gozlan , Boaz Gome , Shlomit Wizel
IPC分类号： A61K31/198 , C07C237/02
CPC分类号： C07C231/24 , C07B2200/13 , C07C233/63 , C07C2601/14
摘要： Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, 0, P, Q, T, U, V, Y, α, β, γ, δ, ε, δ, σ, 2 and Ω, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.
摘要翻译：提供那格列奈的结晶形式，标记为A，C，D，F，G，I，J，K，L，M，N，0，P，Q，T，U，V，Y，α，β，，δ，ε，δ，σ，2和Omega，其制备方法和制备其他结晶形式的那格列奈的方法。还提供了它们的药物制剂和给药方法。

136. 发明申请

US20060276545A1 Polyhydroxy phenols and their use in binding p-selectin 失效
标题翻译：多羟基酚及其在结合p-选择素中的应用
公开(公告)号：US20060276545A1
公开(公告)日：2006-12-07
申请号：US10558495
申请日：2004-05-07
申请人： Erik Anna Biessen , Chantal Appeldoorn , Arnaud Bonnefoy , Theodorus Van Berkel , Johan Kuiper , Marc Hoylaerts
发明人： Erik Anna Biessen , Chantal Appeldoorn , Arnaud Bonnefoy , Theodorus Van Berkel , Johan Kuiper , Marc Hoylaerts
IPC分类号： A61K31/198 , C07C237/02
CPC分类号： C07D209/20 , A61K9/107 , A61K9/127 , C07C69/96 , C07C237/22
摘要： Polyhydroxy phenols, which are non-peptidic mimetics of galloyl peptides, and a process for the preparation of gallic acid derivatives using a gallic-acid providing moiety are provided as well as polyhydroxy phenol-containing pharmaceutical and nutraceutical compositions. The use of polyhydroxy phenols as a medicament and especially for the manufacture of a medicament for the prevention, treatment or diagnosis of a disease or a condition, wherein P-selectin is involved, is provided. The same compounds can also be used as targeting tools to P-selectin expressing cells or tissues in a composition, further comprising an active compound in a vehicle.
摘要翻译：提供作为酰基肽的非肽模拟物的多羟基酚，以及使用没食子酸提供部分制备没食子酸衍生物的方法以及含有多羟基苯酚的药物和营养组合物。提供了使用多羟基酚作为药物，特别是制备用于预防，治疗或诊断其中涉及P-选择素的疾病或病症的药物。相同的化合物也可以用作组合物中表达P-选择蛋白的细胞或组织的靶向工具，还包含载体中的活性化合物。

137. 发明申请

US20060229470A1 Calcium receptor-active molecules 审中-公开
标题翻译：钙受体活性分子
公开(公告)号：US20060229470A1
公开(公告)日：2006-10-12
申请号：US11242079
申请日：2005-10-04
申请人： Bradford Van Wagenen , Manuel Balandrin , Eric DelMar , Edward Nemeth
发明人： Bradford Van Wagenen , Manuel Balandrin , Eric DelMar , Edward Nemeth
IPC分类号： C07C237/02
CPC分类号： C07C217/74 , A01K2227/50 , A61K31/13 , A61K31/135 , A61K31/137 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/275 , A61K31/335 , A61K31/34 , A61K31/35 , A61K31/36 , A61K31/38 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/55 , A61K31/70 , A61K31/715 , A61K38/16 , C07C211/27 , C07C211/29 , C07C211/30 , C07C211/40 , C07C211/42 , C07C215/52 , C07C217/58 , C07C217/60 , C07C217/62 , C07C225/16 , C07C229/38 , C07C233/05 , C07C255/58 , C07C317/32 , C07C323/32 , C07C2601/14 , C07D209/14 , C07D209/16 , C07D209/18 , C07D213/38 , C07D233/64 , C07D319/18 , C07K14/705 , G01N33/5008 , G01N33/502 , G01N33/5044 , G01N33/5091 , G01N33/566 , G01N33/567 , G01N33/6872 , G01N33/6893 , G01N33/84 , G01N2500/10 , G01N2800/04
摘要： The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.
摘要翻译：本发明涉及无机离子受体在细胞和身体过程中的不同作用。本发明的特征在于：（1）可以调节一种或多种无机离子受体活性的分子，优选分子可以模拟或阻断细胞外离子对具有无机离子受体的细胞的影响，更优选细胞外离子是Ca SUP> 2 + ，其作用在具有钙受体的细胞上; （2）无机离子受体蛋白及其片段，优选钙受体蛋白及其片段; （3）编码无机离子受体蛋白质及其片段的核酸，优选钙受体蛋白及其片段; （4）抗体及其片段，靶向无机离子受体蛋白，优选钙受体蛋白; 和（5）使用这些分子，蛋白质，核酸和抗体。

138. 发明申请

US20040139884A1 Light-resistive dispersant and ink composition containing the same 失效
标题翻译：含有它的耐光分散剂和油墨组合物
公开(公告)号：US20040139884A1
公开(公告)日：2004-07-22
申请号：US10724753
申请日：2003-12-02
申请人： Samsung Electronics Co., Ltd.
发明人： Yeon-Kyoung Jung , Seung-Min Ryu
IPC分类号： C09D011/00 , C07F009/02 , C07C237/02
CPC分类号： C07C43/23 , C07C69/40 , C07C69/734 , C07C233/22 , C07C271/16 , C09D11/03 , C09D11/326
摘要： A 2-methoxyphenol derivative may be used as an ultraviolet (UV) light absorbing dispersant and, an ink composition may include the 2-methoxyphenol derivative as a light-resistant dispersant. The 2-methoxyphenol derivative absorbs UV light and thus provides light resistance to outputs. The 2-methooxyphenol derivative also improves dispersibility. When the 2-methoxyphenol derivative is used to prepare an ink composition, the ink composition has improved dispersibility and light resistance, and there is no need to add a light-resistant additive.
摘要翻译：可以使用2-甲氧基苯酚衍生物作为紫外线（UV）光吸收分散剂，并且油墨组合物可以包括作为耐光分散剂的2-甲氧基苯酚衍生物。 2-甲氧基苯酚衍生物吸收紫外线，从而为输出提供耐光性。 2-代苯氧基苯酚衍生物也提高了分散性。当使用2-甲氧基苯酚衍生物来制备油墨组合物时，油墨组合物具有改善的分散性和耐光性，并且不需要加入耐光添加剂。

139. 发明授权

US5977371A Tandem asymmetric transformation process 失效
标题翻译：串联非对称变换过程
公开(公告)号：US5977371A
公开(公告)日：1999-11-02
申请号：US967127
申请日：1997-11-12
申请人： Joseph D. Armstrong, III , J. Christopher McWilliams
发明人： Joseph D. Armstrong, III , J. Christopher McWilliams
IPC分类号： C07C231/18 , C07C233/01 , C07C235/02 , C07C237/02 , C07C269/06 , C07C271/22 , C07D263/52 , C07D263/62 , C07D307/33 , C07F3/06 , C07C233/00 , C07C235/00
CPC分类号： C07D263/52 , C07C231/18 , C07C269/06 , C07D263/62 , C07D307/33 , C07F3/06 , C07B2200/07
摘要： The instant invention provides a homologation process for making a zincate homoenolate from a carbon bound enolate zincate, by treating the carbon bound enolate zincate with an alkoxy lithium reagent. The homologation step can be coupled with a homoaldol reaction, as well as with other transmetallation reactions, in a one pot process. The zincate homoenolate is a useful intermediate in the preparation of a variety of different end-products, such as HIV protease inhibitors and renin inhibitors.
摘要翻译：本发明提供了通过用烷氧基锂试剂处理碳键合的烯醇化物锌酸盐来制备来自碳键合烯醇化锌酸锌的高酸烯醇化物的同系化方法。在一锅法中，同系步骤可与均聚醇反应以及其它转金属反应相结合。锌酸锌高倍醇酯是制备各种不同终产物如HIV蛋白酶抑制剂和肾素抑制剂的有用中间体。

140. 发明授权

US5945543A Process for producing .alpha.-(N,N dialkyl)-amino carboxlic acid amides 失效
标题翻译：制备α-（N，N二烷基） - 氨基羧酸酰胺的方法
公开(公告)号：US5945543A
公开(公告)日：1999-08-31
申请号：US983287
申请日：1998-01-20
申请人： Ernst Buschmann , Thomas Zierke
发明人： Ernst Buschmann , Thomas Zierke
IPC分类号： C07C231/02 , C07C237/02 , C07K1/06 , C07K1/08 , C07K7/06
CPC分类号： C07K7/06 , C07C231/02 , C07K1/082 , Y02P20/55
摘要： A process for preparing .alpha.-(N,N-dialkylamino) carboxamides of the formula I ##STR1## where the substituents have the stated meanings, comprises reacting the corresponding free acids with primary or secondary amines in the presence of anhydrides of an alkanephosphonic acid.
摘要翻译： PCT No.PCT / EP96 / 03075第 371日期1998年1月20日 102（e）日期1998年1月20日PCT提交1996年7月12日PCT公布。公开号WO97 / 05096 日期1997年2月13日一种制备式I的（N，N-二烷基氨基）甲酰胺的方法，其中取代基具有所述含义，包括在烷基膦酸酐的存在下使相应的游离酸与伯胺或仲胺反应酸。

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