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1. 发明申请

US20190315784A1 PRODRUGS OF GLUTAMINE ANALOGS 审中-公开
公开(公告)号：US20190315784A1
公开(公告)日：2019-10-17
申请号：US16454880
申请日：2019-06-27
申请人： THE JOHNS HOPKINS UNIVERSITY , Ústav organické chemie a biochemie AV CR, v.v.i.
发明人： Barbara Slusher , Rana Rais , Lukas Tenora , Pavel Majer , Andrej Jancarik
IPC分类号： C07F9/24 , C07C227/14 , C07K5/083 , C07H19/207 , C07H15/203 , C07D317/40 , A61K31/404 , C07D317/38 , C07D473/34 , C07D263/04 , C07D309/10 , C07C245/18 , C07D211/90 , A61P35/00 , C07C271/22 , C07D209/18 , C07K5/062 , C07D263/18 , C07K5/078 , C07F9/6561 , C07D209/20
摘要： The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

2. 发明授权

US09790483B2 Reagents and methods for esterification 有权
公开(公告)号：US09790483B2
公开(公告)日：2017-10-17
申请号：US15093510
申请日：2016-04-07
申请人： WISCONSIN ALUMNI RESEARCH FOUNDATION
发明人： Ronald T. Raines , Kalie Mix
IPC分类号： C12N9/96 , C07C231/12 , C07C319/12 , C07D207/46 , C07K1/13 , C07C269/06 , C07C245/18
CPC分类号： C12N9/96 , C07C231/12 , C07C245/18 , C07C269/06 , C07C319/12 , C07D207/46 , C07K1/13 , C07C323/52 , C07C271/22 , C07C235/34
摘要： Methods and reagents for esterification of biological molecules including proteins, polypeptides and peptides. Diazo compounds of formula I: where R is hydrogen, an alkyl, an alkenyl or an alkynyl, RA represents 1-5 substituents on the indicated phenyl ring and RM is an organic group, which includes a label, a cell penetrating group, a cell targeting group, or a reactive group or latent reactive group for reaction to bond to a label, a cell penetrating group, or a cell targeting group, among other organic groups are useful for esterification of biological molecules. Also provided are diazo compounds which are bifunctional and trifunctional coupling reagents as well as reagents for the synthesis of compounds of formula I.

3. 发明申请

US20130203974A1 Preparation of Diazo and Diazonium Compounds 有权
标题翻译：重氮和重氮化合物的制备
公开(公告)号：US20130203974A1
公开(公告)日：2013-08-08
申请号：US13715842
申请日：2012-12-14
申请人： Ronald Thaddeus RAINES , Eddie Leonard MYERS
发明人： Ronald Thaddeus RAINES , Eddie Leonard MYERS
IPC分类号： C07C245/18 , C07F9/28 , C07C251/00 , C07D223/16
CPC分类号： C07C245/18 , C07C245/12 , C07C247/10 , C07C247/12 , C07C247/14 , C07C251/00 , C07C271/22 , C07C2601/14 , C07C2603/18 , C07C2603/24 , C07D223/16 , C07F9/28 , C07F9/5022 , C07F9/5325 , C07F9/572
摘要： A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diaz-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compound and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.
摘要翻译：制备重氮化合物，其重氮盐和这些化合物的其它保护形式的方法。通过使带有反应性羰基的叔膦试剂与叠氮化物反应来制备二嗪化合物。反应也可以产生酰基三氮烯，其可以热转化或加入碱形成重氮化合物，或者可以分离酰基三氮烯。该方法对于携带一个或多个吸电子基团的叠氮化物转化为重氮化合物是特别有用的。该方法可以在温和条件下在水性介质中进行，特别适用于在生理条件下将叠氮基糖转化为重氮化合物和重氮盐。提供了叔膦试剂，特别是水溶性试剂，以及制备试剂的前体。

4. 发明申请

US20050240035A1 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US20050240035A1
公开(公告)日：2005-10-27
申请号：US11071675
申请日：2005-03-02
申请人： Stefan Lindstrom , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Oden , Lotta Naeslund
发明人： Stefan Lindstrom , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Oden , Lotta Naeslund
IPC分类号： C07D335/06 , A61K31/4155 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4709 , A61K31/497 , A61K31/506 , A61P31/18 , A61P37/04 , A61P43/00 , C07C43/23 , C07C245/18 , C07D307/93 , C07D311/78 , C07D311/94 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.
摘要翻译：本发明涉及对HIV-1有活性且具有改善的抗药性和药代动力学特征的非核苷逆转录酶抑制剂。本发明还涉及合成这些化合物的新型中间体以及该化合物在抗病毒方法和组合物中的用途。

5. 发明授权

US5494507A Dye having hydrophobic substituent and aqueous ink 失效
标题翻译：具有疏水取代基的染料和含水墨水
公开(公告)号：US5494507A
公开(公告)日：1996-02-27
申请号：US359230
申请日：1994-12-19
申请人： Bradley L. Beach , James F. Feeman , Ann M. Piekunka , Allen C. Sanders
发明人： Bradley L. Beach , James F. Feeman , Ann M. Piekunka , Allen C. Sanders
IPC分类号： C09B29/01 , C09B29/30 , C09B29/50 , C09B31/08 , C09B31/18 , C09B33/10 , C09D11/00 , C09D11/02 , C07C245/08 , C07C245/18
CPC分类号： C09D11/328 , C09B29/0003 , C09B29/30 , C09B29/366 , C09B31/08 , C09B31/18 , C09B33/10
摘要： A dye having a representative formula as follows and an ink providing waterfast printing having the dye, in which a surfactant is not essential: ##STR1##
摘要翻译：具有如下代表性的染料和提供具有染料的耐水印的油墨，其中表面活性剂不是必需的：

6. 发明授权

US5340927A Process for the preparation of 2-diazo-3-trisubstituted silyloxy 3-butenoates 失效
标题翻译： 2-重氮-3-三取代甲硅烷氧基-3-丁烯酸酯的制备方法
公开(公告)号：US5340927A
公开(公告)日：1994-08-23
申请号：US846725
申请日：1992-03-02
申请人： David L. Hughes
发明人： David L. Hughes
IPC分类号： C07F7/18 , C07C245/18
CPC分类号： C07F7/188 , C07F7/1852
摘要： A novel process for preparing 2-diazo-3-trisubstituted silyloxy-3-butenoates, synthons useful in the conversion of 3-substituted-4-acetoxy azetidinones and penicillin to thienamycin, imipenem and other carbapenem antibiotic compounds is provided, comprising the reaction of the appropriate diazo acetoacetate with the substituted silane, base and salt.
摘要翻译：提供了一种用于制备2-重氮-3-三取代的甲硅烷氧基-3-丁烯酸酯的新方法，可用于将3-取代-4-乙酰氧基氮杂环丁酮和青霉素转化成硫霉素，亚胺培南和其他碳青霉烯类抗生素化合物的合成物，其包括适当的重氮乙酰乙酸酯与取代的硅烷，碱和盐。

7. 发明授权

US5198322A Positively operating radiation-sensitive mixture containing a polyfunctional .alpha.-diazo-.beta.-keto ester and radiation-sensitive recording material containing this mixture 失效
标题翻译：含有多官能（ALPHA）-DIAZO-（BETA）-KETO ESTER和含有该混合物的辐射敏感记录材料的正确操作的辐射敏感性混合物
公开(公告)号：US5198322A
公开(公告)日：1993-03-30
申请号：US466007
申请日：1990-01-12
申请人： Peter Wilharm , Hans-Joachim Merrem , Georg Pawlowski , Ralph Dammel
发明人： Peter Wilharm , Hans-Joachim Merrem , Georg Pawlowski , Ralph Dammel
IPC分类号： G03F7/039 , A61K8/00 , A61Q17/04 , C07C245/18 , C07C271/10 , C07C271/20 , C07C271/24 , C07C275/10 , C07C275/26 , C07C275/32 , C07C275/40 , C07C323/12 , C07D209/48 , C07D251/34 , C07D295/14 , C08F2/50 , C09K3/00 , G03C1/52 , G03F7/004 , G03F7/016 , H01L21/027 , H01L21/30
CPC分类号： C07C245/18 , G03F7/0163 , C07C2101/14
摘要： A positively operating radiation-sensitive mixture comprising a binder which is insoluble in water but soluble or at least swellable in aqueous alkaline solution, and as a photoactive component a polyfunctional .alpha.-diazo-.beta.-keto ester of the general formula I ##STR1## in which R.sup.1 denotes an aliphatic, cycloaliphatic or araliphatic or aromatic radical having 4 to 20 carbon atoms, in which individual CH.sub.2 groups can be replaced by oxygen or sulfur atoms or by ##STR2## or NH groups and/or contain keto groups, X denotes an aliphatic, cycloaliphatic, carbocyclic, heterocyclic or araliphatic radical having 2 to 22 carbon atoms, in which individual CH.sub.2 groups can be replaced by oxygen or sulfur atoms or by the groups --NR.sup.2 --, --C(O)--O--, --C(O)--NR.sup.2 --, --C(O)-- ##STR3## --NR.sup.2 --C(O)--NR.sup.3 --, --O--C(O)--NR.sup.2 --, --C(O)-- ##STR4## or --O--C(O)--O--, or CH groups can be replaced by ##STR5## in which R.sup.2 and R.sup.3 independently of one another represent hydrogen or an aliphatic, carbocyclic or araliphatic radical,m denotes an integer from 2 to 10 andn denotes an integer from 0 to 2, whereinm-n is .gtoreq.2,is described.The radiation-sensitive mixture is particularly suitable for exposure using radiation of wavelength 190 to 300 nm.
摘要翻译：一种正面工作的辐射敏感性混合物，其包含不溶于水但在碱性水溶液中可溶或至少可溶胀的粘合剂，以及作为光活性组分的通式I的多官能α-重氮基β-酮酯（IMAGE）（ I），其中R1表示具有4至20个碳原子的脂族，脂环族或芳脂族或芳族基团，其中各个CH 2基团可以被氧或硫原子替代，或者通过<或>或/或含有酮基， X表示具有2至22个碳原子的脂族，脂环族，碳环，杂环或芳脂族基团，其中各个CH 2基团可被氧或硫原子替代，或由-NR 2 - ， - C（O）-O-， -C（O）-NR 2 - ， - C（O）-NR 2 -C（O）-NR 3 - ， - OC（O）-NR 2 - ， - C（O）（O）-O-或CH基团可以被其中R 2和R 3彼此独立地表示氢或脂族，碳环或芳脂族基团的“IMAGE”代替，m表示 s为2至10的整数，n表示0至2的整数，其中m-n为> / = 2。辐射敏感的混合物特别适用于使用波长为190至300nm的辐射的曝光。

8. 发明授权

US5141627A Chelators whose affinity for calcium ion is increased by illumination 失效
标题翻译：通过照明增加对钙离子的亲和力的螯合剂
公开(公告)号：US5141627A
公开(公告)日：1992-08-25
申请号：US412852
申请日：1989-09-25
申请人： Roger Y. Tsien , Stephen R. Adams
发明人： Roger Y. Tsien , Stephen R. Adams
IPC分类号： C07C245/18
CPC分类号： C07C245/18
摘要： The present invention relates to a group of organic chelators whose affinity for calcium ion in solution is increased by electromagnetic radiation. Specifically, the chelators are related to BAPTA and utilize the addition of an electron-withdrawing group (e.g., diazocarbonyl) to a ring of BAPTA, para to the amino group. Photochemical rearrangement of the diazoacetyl group converts the group to the electron-donating carboxymethyl group, causing the calcium ion efficiency to increase 25 to 50 fold. These chelators when incorporated into rat fibroblasts either by microinjection or by incubation as the membrane-permeable, enzymatically-labile tetraacetoxymethyl ester and flash-photolyzed cause a drop in intracellular free calcine ion to or below resting valves of about 10.sup.-7 M. These chelators are used to generate controlled fast removal of intracellular free calcium ion to mimic or modulate a number of important cellular responses, especially in nerve or muscle.
摘要翻译：本发明涉及通过电磁辐射增加溶液中对钙离子的亲和力的一组有机螯合剂。具体地说，螯合剂与BAPTA有关，并利用向吸附对氨基的BAPTA环中加入吸电子基团（如重氮羰基）。重氮乙酰基的光化学重排将该基团转移到给电子的羧甲基基团，导致钙离子效率增加25-50倍。这些螯合剂通过显微注射或通过孵育作为膜可渗透的，酶促不稳定的四乙酰氧基甲基酯并且闪光光引发而引入大鼠成纤维细胞时，导致细胞内游离的煅烧离子降至约10-7M的静止阀或其下面。这些螯合剂用于产生受控的快速去除细胞内游离钙离子以模拟或调节许多重要的细胞反应，特别是在神经或肌肉中。

9. 发明授权

US2965637A Norleucine derivatives and process for producing same 失效
公开(公告)号：US2965637A
公开(公告)日：1960-12-20
申请号：US70897158
申请日：1958-01-15
申请人： PARKE DAVIS & CO
发明人： WESTLAND ROGER D
IPC分类号： C07C245/18
CPC分类号： C07C245/18

10. 发明授权

US2965633A 6-diazo-5-oxonorleucine 失效
标题翻译： 6-重氮-5-氧代亮氨酸
公开(公告)号：US2965633A
公开(公告)日：1960-12-20
申请号：US57041856
申请日：1956-03-09
申请人： PARKE DAVIS & CO
发明人： MOORE ALEXANDER M , DE WALD HORACE A , WESTLAND ROGER D , JOHN EHRLICH , BARTZ QUENTIN R , DLON HENRY W , FUSARI SALVATORE A
IPC分类号： C07C245/18 , C12P13/04
CPC分类号： C12P13/04 , C07C245/18 , Y10S435/886

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