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1. 发明授权

US07232805B2 Cobalamin conjugates for anti-tumor therapy 有权
标题翻译：钴胺素共轭物用于抗肿瘤治疗
公开(公告)号：US07232805B2
公开(公告)日：2007-06-19
申请号：US10659501
申请日：2003-09-10
申请人： Ned M. Weinshenker , Frederick G. West , Barbara A. Araneo , Weiping Li
发明人： Ned M. Weinshenker , Frederick G. West , Barbara A. Araneo , Weiping Li
IPC分类号： A01N43/04 , A61K31/70 , C07G3/00 , C07G11/00 , C07H15/00 , C07H17/00
CPC分类号： A61K47/551
摘要： The present invention provides a cobalamin-drug conjugate suitable for the treatment of tumor related diseases. Cobalamin is indirectly covalently bound to an anti-tumor drug via a cleavable linker and one or more optional spacers. Cobalamin is covalently bound to a first spacer or the cleavable linker via the 5′-OH of the cobalamin ribose ring. The drug is bound to a second spacer of the cleavable linker via an existing or added functional group on the drug. After administration, the conjugate forms a complex with transcobalamin (any of its isoforms). The complex then binds to a receptor on a cell membrane and is taken up into the cell. Once in the cell, an intracellular enzyme cleaves the conjugate thereby releasing the drug. Depending upon the structure of the conjugate, a particular class or type of intracellular enzyme affects the cleavage. Due to the high demand for cobalamin in growing cells, tumor cells typically take up a higher percentage of the conjugate than do normal non-growing cells. The conjugate of the invention advantageously provides a reduced systemic toxicity and enhanced efficacy as compared to a corresponding free drug.
摘要翻译：本发明提供了一种适用于治疗肿瘤相关疾病的钴胺素药物缀合物。钴胺素通过可裂解连接体和一个或多个任选的间隔物间接共价结合抗肿瘤药物。钴胺素通过钴胺核糖环的5'-OH共价结合到第一间隔物或可切割的接头。药物通过药物上现有或添加的官能团与可切割接头的第二间隔物结合。给药后，缀合物与转钴胺素（其任何同种型）形成复合物。然后，该复合物与细胞膜上的受体结合，并被吸收到细胞中。一旦在细胞中，细胞内酶切割缀合物从而释放药物。根据缀合物的结构，细胞内酶的特定类别或类型影响切割。由于对生长细胞中钴胺素的高需求，肿瘤细胞通常占有比正常非生长细胞更高的缀合物百分比。与相应的游离药物相比，本发明的缀合物有利地提供降低的全身毒性和增强的功效。

2. 发明授权

US4054676A Edible with polymeric hydroquinone antioxidant 失效
标题翻译：食用聚合氢醌抗氧化剂
公开(公告)号：US4054676A
公开(公告)日：1977-10-18
申请号：US529325
申请日：1974-12-04
申请人： Ned M. Weinshenker , James A. Dale
发明人： Ned M. Weinshenker , James A. Dale
IPC分类号： A23L3/3463 , A23L27/00 , C07C37/16 , C07C39/15 , C11B5/00 , A23D5/04
CPC分类号： A23L3/3463 , A23L27/74 , C07C37/18 , C07C39/15 , C11B5/0035
摘要： Polymeric hydroquinones of the structure ##STR1## , wherein n is from 3 to 10,000 inclusive and R and R' independently are hydrogen or a lower alkyl, are disclosed, as is the preparation and the use of such materials, especially as nonabsorbable polymeric antioxidants for edible materials.
摘要翻译：结构的聚合氢醌，其中n为3至10,000，其中R和R'独立地为氢或低级烷基，这些材料的制备和使用，特别是作为不可吸收的聚合物抗氧化剂食用材料。

3. 发明授权

US5068226A Pharmaceutical preparations containing cyclodextrins and their use in iontophoretic therapies 失效
标题翻译：含有环糊精的药物制剂及其在离子电渗治疗中的应用
公开(公告)号：US5068226A
公开(公告)日：1991-11-26
申请号：US516295
申请日：1990-04-30
申请人： Ned M. Weinshenker , William P. O'Neill
发明人： Ned M. Weinshenker , William P. O'Neill
IPC分类号： A61K9/00 , A61K9/18 , A61K47/40 , A61K47/48
CPC分类号： B82Y5/00 , A61K47/40 , A61K47/48969 , A61K9/0009 , A61K9/0014 , Y10S516/01
摘要： Cyclodextrins and especially ionic cyclodextrin derivatives facilitate the iontophoretic delivery of pharmaceutically active agents.
摘要翻译：环糊精，特别是离子环糊精衍生物有助于药物活性剂的离子电渗疗法。

4. 发明授权

US3959190A Insoluble oxidation reagent 失效
标题翻译：不溶氧化试剂
公开(公告)号：US3959190A
公开(公告)日：1976-05-25
申请号：US479654
申请日：1974-06-17
申请人： Ned M. Weinshenker
发明人： Ned M. Weinshenker
IPC分类号： C07C45/29 , C07C45/30 , C08F8/34 , C08J9/36 , C08F28/04
CPC分类号： C07C45/30 , C07C45/29 , C08F8/22 , C08F8/34 , Y10S521/921
摘要： A polymeric sulfide oxidation reagent comprising a cross-linked polymeric resin carrying a plurality of lower alkyl sulfide groups, its preparation and its use as a co-reactant for the oxidation of primary and secondary alcohols are disclosed.
摘要翻译：公开了一种聚合硫化物氧化试剂，其包含携带多个低级烷基硫醚基团的交联聚合物树脂，其制备方法及其作为用于伯和仲醇氧化的共反应物的用途。

5. 发明授权

US4115545A Pharmaceutical composition containing prostadienoic acid for regulating gastric secretion 失效
标题翻译：含有前列腺素的药物组合物用于调节胃分泌
公开(公告)号：US4115545A
公开(公告)日：1978-09-19
申请号：US823811
申请日：1977-08-11
申请人： Ned M. Weinshenker , Niels H. Anderson
发明人： Ned M. Weinshenker , Niels H. Anderson
IPC分类号： C07C405/00 , C07D307/935 , A61K31/22 , A61K31/19 , A61L9/04
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0041
摘要： Novel alkyl diethers of prostaglandins of the formula; ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.6 are hydrogen when Y is a single bond and R.sub.2 and R.sub.6 are absent when Y is a double bond; R.sub.3 is keto, ##STR2## R'.sub.9 is hydrogen or lower alkyl; R'.sub.10 is lower alkyl; R'.sub.11 is lower alkyl; Z.sub.1 is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; Z.sub.2 is trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; X is a single bond or a double bond and X is a single bond when R.sub.4 and R.sub.5 are hydrogen; Y is a single bond or a double bond; n is 1 to 5, m is 0 to 4; and the non-toxic salts. The prostaglandin ethers possess valuable pharmacological properties as modifiers of smooth muscle activity, gastric secretion, blood pressure, lipolysis and the reproductive system. The compounds also induce labor and menses and they can be used for the relief of asthma and nasal congestion. The compounds are also useful as platelet anti-clumping agents and for the inhibition of peptic ulcers.
摘要翻译：式中前列腺素的新型烷基二醚; 其中R1是氢或低级烷基; 当Y是单键时，R2和R6是氢，当Y是双键时R2和R6不存在; R3是酮基，R'9是氢或低级烷基; R'10是低级烷基; R11为低级烷基; Z 1是顺式或反式-CH = CH-或-CH 2 CH 2 - ; Z2是反式-CH = CH-或-CH2CH2-; X是单键或双键，当R4和R5是氢时X是单键; Y是单键或双键; n为1〜5，m为0〜4; 和无毒盐。前列腺素醚具有作为平滑肌活动，胃分泌，血压，脂肪分解和生殖系统改性剂的有价值的药理学性质。这些化合物还可以诱发劳动和月经，并可用于缓解哮喘和鼻塞。该化合物也可用作血小板抗凝块剂和抑制消化性溃疡。

6. 发明授权

US4025535A Sulfoalkylated flavanone sweeteners 失效
标题翻译：磺烷基化黄烷酮甜味剂
公开(公告)号：US4025535A
公开(公告)日：1977-05-24
申请号：US657905
申请日：1976-02-13
申请人： Guy A. Crosby , Grant E. DuBois , Ned M. Weinshenker
发明人： Guy A. Crosby , Grant E. DuBois , Ned M. Weinshenker
IPC分类号： A23L27/30 , C07C45/62 , C07C49/84 , C07C309/09 , C07D311/32 , C07F1/00 , C07F3/00 , C07D311/02
CPC分类号： C07C45/71 , A23L27/30 , C07C309/00 , C07C45/62 , C07C45/74 , C07D311/32 , C07F1/005 , C07F3/003
摘要： Flavanones represented by the formula ##STR1## wherein R is a lower alkyl of from one to three carbon atoms inclusive, n is an integer of from one to three inclusive and M is hydrogen or a physiologically acceptable metal cation, are disclosed. These materials are themselves useful as dietetic sweeteners as well as being direct intermediates for the preparation of useful dihydrochalcone sweeteners.
摘要翻译：由式表示的黄酮，其中R为含有1至3个碳原子的低级烷基，n为1至3的整数，M为氢或生理学上可接受的金属阳离子。这些材料本身可用作饮食甜味剂，以及用于制备有用的二氢查耳酮甜味剂的直接中间体。

7. 发明授权

US5068227A Cyclodextrins as carriers 失效
标题翻译：环糊精作为载体
公开(公告)号：US5068227A
公开(公告)日：1991-11-26
申请号：US298634
申请日：1989-01-18
申请人： Ned M. Weinshenker
发明人： Ned M. Weinshenker
IPC分类号： A61K47/48 , C08B37/16 , G01N33/531 , G01N33/532
CPC分类号： B82Y5/00 , A61K47/48961 , A61K47/48969 , C08B37/0012 , G01N33/531 , G01N33/532 , Y10T436/13
摘要： Cyclodextrins can be coupled to biorecognition molecules such as antibodies. The cyclodextrins so coupled provide a cavity or complexation zone into which active agents such as labels, drugs and the like may be incorporated. The active agent forms a noncovalently bonded inclusion complex within the cavity of the cyclodextrin. It remains associated with the cyclodextrin and the coupled biorecognition molecule and thus can be delivered to the other half of the biospecific recognition pair. A process for producing these materials is also disclosed. The process includes the steps of activating a primary hydroxyl site on a cyclodextrin; linking a biorecognition molecule to the activated primary hydroxyl site on the cyclodextrin in either a direct covalent linkage or through a covalently linked spacer; and introducing a guest molecule (active agent) into the cavity of the derivatized cyclodextrin to form an inclusion complex.
摘要翻译：环糊精可以与生物识别分子如抗体偶联。如此耦合的环糊精提供空腔或络合区，其中可以并入活性剂如标签，药物等。活性剂在环糊精的空腔内形成非共价键合的包合络合物。它仍然与环糊精和偶联生物识别分子相关联，因此可以被递送到生物特异性识别对的另一半。还公开了这些材料的制造方法。该方法包括在环糊精上活化伯羟基位点的步骤; 将生物识别分子与直链共价键或通过共价连接的间隔基上的环糊精上的活化的伯羟基位点连接; 并将客体分子（活性剂）引入到衍生化的环糊精的空腔中以形成包合物。

8. 发明授权

US4098829A Polymeric hydroquinone antioxidant 失效
标题翻译：聚合氢氧化物抗氧化剂
公开(公告)号：US4098829A
公开(公告)日：1978-07-04
申请号：US798284
申请日：1977-05-19
申请人： Ned M. Weinshenker , James A. Dale
发明人： Ned M. Weinshenker , James A. Dale
IPC分类号： A23L3/3463 , A23L27/00 , C07C37/16 , C07C39/15 , C11B5/00 , C07C39/12 , A23D5/04 , C08G83/00
CPC分类号： A23L3/3463 , A23L27/74 , C07C37/18 , C07C39/15 , C11B5/0035
摘要： Polymeric hydroquinones of the structure ##STR1## WHEREIN N IS FROM 3 TO 10,000 INCLUSIVE AND R and R' independently are hydrogen or a lower alkyl, are disclosed, as is the preparation and the use of such materials, especially as nonabsorbable polymeric antioxidants for edible materials.

9. 发明授权

US4055593A Alkyl diethers of prostaglandins 失效
标题翻译：前列腺素的烷基二醚
公开(公告)号：US4055593A
公开(公告)日：1977-10-25
申请号：US570621
申请日：1975-04-23
申请人： Ned M. Weinshenker , Niels H. Andersen
发明人： Ned M. Weinshenker , Niels H. Andersen
IPC分类号： C07C405/00 , C07D307/935 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07C405/0041
摘要： Novel alkyl diethers of prostaglandins of the formula; ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.6 are hydrogen when Y is a single bond and R.sub.2 and R.sub.6 are absent when Y is a double bond; R.sub.3 is keto, ##STR2## R.sub.4 is hydrogen or ##STR3## R'.sub.9 is hydrogen or lower alkyl; R'.sub.10 is lower alkyl; R'.sub.11 is lower alkyl; Z.sub.1 is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; Z.sub.2 is trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --; X is a single bond or a double bond and X is a single bond when R.sub.4 and R.sub.5 are hydrogen; Y is a single bond or a double bond; n is 1 to 5, m is 0 to 4; and the non-toxic salts. The prostaglandin ethers possess valuable pharmacological properties as modifiers of smooth muscle activity, gastric secretion, blood pressure, lipolysis and the reproductive system. The compounds also induce labor and menses and they can be used for the relief of asthma and nasal congestion. The compounds are also useful as platelet anti-clumping agents and for the inhibition of peptic ulcers.
摘要翻译：式中前列腺素的新型烷基二醚; 其中R1是氢或低级烷基; 当Y是单键时，R2和R6是氢，当Y是双键时R2和R6不存在; R 3是酮基，R 4是氢或R 1是氢或低级烷基; R'10是低级烷基; R11为低级烷基; Z 1是顺式或反式-CH = CH-或-CH 2 CH 2 - ; Z2是反式-CH = CH-或-CH2CH2-; X是单键或双键，当R4和R5是氢时X是单键; Y是单键或双键; n为1〜5，m为0〜4; 和无毒盐。前列腺素醚具有作为平滑肌活动，胃分泌，血压，脂肪分解和生殖系统改性剂的有价值的药理学性质。这些化合物还可以诱发劳动和月经，并可用于缓解哮喘和鼻塞。该化合物也可用作血小板抗凝块剂和抑制消化性溃疡。

10. 发明授权

US3996199A Oil soluble polymeric antioxidant prepared by condensation of divinylbenzene, hydroxyanisole, tertiary butyl hydroquinone, tertiary butyl phenol and bisphenol A under ortho alkylation conditions 失效
标题翻译：通过二乙烯基苯，羟基苯甲醚，叔丁基氢醌，叔丁基苯酚和双酚A在邻位烷基化条件下缩合制备的油溶性聚合物抗氧化剂
公开(公告)号：US3996199A
公开(公告)日：1976-12-07
申请号：US658943
申请日：1976-02-17
申请人： Ned M. Weinshenker , Leonard A. Bunes , Roman Davis
发明人： Ned M. Weinshenker , Leonard A. Bunes , Roman Davis
IPC分类号： A23L3/3463 , C08G61/02 , C08L101/00 , C09K15/08 , C08K5/13
CPC分类号： A23L3/3463 , C08G61/02 , C08L101/00 , C09K15/08 , C08G2261/3424
摘要： Phenolic polymers formed by the reaction of divinylbenzene with a mixture of hydroxyanisole, tertiary butylhydroquinone, tertiary butyl phenol and bisphenol A (and optionally para-cresol) under condensation conditions in the presence of a phenol ortho alkylation catalyst are disclosed. These materials find use as oil-soluble antioxidants especially for edibles.
摘要翻译：公开了在苯酚正烷基化催化剂存在下，在缩合条件下二乙烯基苯与羟基苯甲醚，叔丁基氢醌，叔丁基苯酚和双酚A（和任选的对甲酚）的混合物反应形成的酚醛聚合物。这些材料可用作油溶性抗氧化剂，特别适用于食品。

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