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1. 发明授权

US6083926A Water soluble vitamin B.sub.12 receptor modulating agents and methods related thereto 有权
标题翻译：水溶性维生素B12受体调节剂及其相关方法
公开(公告)号：US6083926A
公开(公告)日：2000-07-04
申请号：US200422
申请日：1998-11-23
申请人： A. Charles Morgan, Jr. , D. Scott Wilbur , Pradip M. Pathare
发明人： A. Charles Morgan, Jr. , D. Scott Wilbur , Pradip M. Pathare
IPC分类号： A61K31/70 , A61K31/7135 , A61K31/714 , A61K38/00 , A61P1/00 , A61P1/16 , A61P11/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P25/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07H23/00 , G01N33/567
CPC分类号： C07H23/00 , Y10S530/825
摘要： Vitamin B.sub.12 receptor modulating agents capable of modulating cell surface receptors by affecting the cell surface receptor trafficking pathway are disclosed. The vitamin B.sub.12 receptor modulating agents are comprised of a covalently bound rerouting moiety and targeting moiety linked by a water-solublizing linker.
摘要翻译：公开了能够通过影响细胞表面受体转运途径来调节细胞表面受体的维生素B12受体调节剂。维生素B12受体调节剂由共价结合的重路由部分和通过水溶性接头连接的靶向部分组成。

2. 发明授权

US5739287A Biotinylated cobalamins 失效
标题翻译：生物素化钴胺素
公开(公告)号：US5739287A
公开(公告)日：1998-04-14
申请号：US406192
申请日：1995-03-16
申请人： D. Scott Wilbur , Pradip M. Pathare , A. Charles Morgan, Jr.
发明人： D. Scott Wilbur , Pradip M. Pathare , A. Charles Morgan, Jr.
IPC分类号： C07H23/00 , A61K31/70 , A61K38/16 , C07K1/113
CPC分类号： C07H23/00
摘要： A biotinylated cobalamin, formed from a vitamin B.sub.12 molecule coupled to a biotin molecule, is disclosed. In a preferred embodiment, the vitamin B.sub.12 molecule is cyanocobalamin. The biotin molecule can also be coupled to a rerouting moiety, optionally through a biotin binding protein such as avidin or streptavidin. The biotinylated cobalamin binds to a cell surface receptor, is invaginated, and once internalized affects the receptor trafficking pathway.
摘要翻译：公开了由与生物素分子偶联的维生素B12分子形成的生物素化钴胺素。在优选的实施方案中，维生素B12分子是氰钴胺素。生物素分子还可以任选地通过生物素结合蛋白例如抗生物素蛋白或链霉抗生物素蛋白偶联至重新路由部分。生物素化的钴胺素结合细胞表面受体，是内陷的，一旦内化影响受体转运途径。

3. 发明授权

US5679322A Iodinated borane cage molecules as X-ray contrast media 失效
标题翻译：碘化硼烷笼分子作为X射线造影剂
公开(公告)号：US5679322A
公开(公告)日：1997-10-21
申请号：US596644
申请日：1996-02-05
申请人： D. Scott Wilbur
发明人： D. Scott Wilbur
IPC分类号： A61K49/04 , C07F5/02 , C07H23/00 , A61K33/18
CPC分类号： C07H23/00 , A61K49/0438 , C07F5/027
摘要： Highly iodinated borane and carborane cage molecules, having from 60% to 90% w/w iodine, are disclosed as new and useful X-ray contrast media when combined with a pharmaceutically acceptable carrier. The inclusion of appropriate functional group substituents, such as hydrophilic moieties, increases solubility and lowers toxicity.
摘要翻译：当与药学上可接受的载体组合时，公开了具有60％至90％（重量/重量）碘的高度碘化的硼烷和碳硼烷笼分子作为新的和有用的X射线造影剂。包括适当的官能团取代基，例如亲水部分，增加了溶解性并降低了毒性。

4. 发明授权

US06492560B2 Discrete-length polyethylene glycols 失效
标题翻译：离散长度聚乙二醇
公开(公告)号：US06492560B2
公开(公告)日：2002-12-10
申请号：US09962840
申请日：2001-09-24
申请人： D. Scott Wilbur , Pradip M. Pathare
发明人： D. Scott Wilbur , Pradip M. Pathare
IPC分类号： C07C21103
CPC分类号： C08L71/02 , A61K47/60 , C08G65/329 , C08G65/34 , C08L71/00
摘要： The present invention provides discrete-length polyethylene glycol and polyethylene glycol containing compounds and methods for their preparation.
摘要翻译：本发明提供了离散长度的聚乙二醇和含聚乙二醇的化合物及其制备方法。

5. 发明授权

US5840712A Water soluble vitamin B.sub.12 receptor modulating agents and methods related thereto 失效
标题翻译：水溶性维生素B12受体调节剂及其相关方法
公开(公告)号：US5840712A
公开(公告)日：1998-11-24
申请号：US545151
申请日：1995-10-19
申请人： A. Charles Morgan, Jr. , D. Scott Wilbur , Pradip M. Pathare
发明人： A. Charles Morgan, Jr. , D. Scott Wilbur , Pradip M. Pathare
IPC分类号： A61K31/70 , A61K31/7135 , A61K31/714 , A61K38/00 , A61P1/00 , A61P1/16 , A61P11/00 , A61P13/02 , A61P15/00 , A61P17/00 , A61P25/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07H23/00 , G01N33/567 , A01N43/04
CPC分类号： C07H23/00 , Y10S530/825
摘要： Vitamin B.sub.12 receptor modulating agents capable of modulating cell surface receptors by affecting the cell surface receptor trafficking pathway are disclosed. The vitamin B.sub.12 receptor modulating agents are comprised of a covalently bound rerouting moiety and targeting moiety linked by a water-solublizing linker.
摘要翻译：公开了能够通过影响细胞表面受体转运途径来调节细胞表面受体的维生素B12受体调节剂。维生素B12受体调节剂由共价结合的重路由部分和通过水溶性接头连接的靶向部分组成。

6. 发明授权

US07141676B1 Water soluble multi-biotin-containing compounds 失效
标题翻译：含水溶性多生物素的化合物
公开(公告)号：US07141676B1
公开(公告)日：2006-11-28
申请号：US10261040
申请日：2002-09-30
申请人： D. Scott Wilbur , Pradip M. Pathare , Donald K. Hamlin , Feng Wan
发明人： D. Scott Wilbur , Pradip M. Pathare , Donald K. Hamlin , Feng Wan
IPC分类号： C07D235/02
CPC分类号： A61K31/4188 , A61K31/765 , C07D233/32 , C07D495/04 , C07D519/00 , Y02P20/55 , Y10S424/16
摘要： Water-soluble discrete multi-biotin-containing compounds with at least three (3) biotin moieties are disclosed. The water-soluble biotin-containing compounds may additionally comprise one or more moieties that confer resistance to cleavage by biotinidase or that is cleavable in vitro or in vivo. The discrete multi-biotin-containing compounds may include a reactive moiety that provides a site for reaction with yet another moiety, such as a targeting, diagnostic or therapeutic functional moiety. Biotinylation reagents comprising water-soluble linker moieties are also disclosed and may additionally comprise a biotinidase protective group. Methods for amplifying the number of sites for binding biotin-binding proteins at a selected target using multi-biotin compounds also are disclosed.
摘要翻译：公开了具有至少三（3）个生物素部分的水溶性离散多生物素化合物。含水溶性生物素的化合物可另外包含一种或多种赋予生物素酶切割抗性或在体外或体内可切割的部分。离散的含多生物素的化合物可以包括提供与另一部分例如靶向，诊断或治疗功能部分反应的位点的反应性部分。还公开了包含水溶性接头部分的生物素化试剂，并且还可以包含生物素酶保护基团。还公开了使用多生物素化合物扩增在选定靶标上结合生物素结合蛋白的位点数目的方法。

7. 发明授权

US5869465A Methods of receptor modulation and uses therefor 失效
标题翻译：受体调节方法及其用途
公开(公告)号：US5869465A
公开(公告)日：1999-02-09
申请号：US406194
申请日：1995-03-16
申请人： A. Charles Morgan, Jr. , D. Scott Wilbur
发明人： A. Charles Morgan, Jr. , D. Scott Wilbur
IPC分类号： C07H23/00 , A61K31/68 , C12P19/42
CPC分类号： C07H23/00
摘要： Receptor modulating agents capable of modulating cell surface receptors by affecting the cell surface receptor trafficking pathway are utilized for the treatment and diagnosis of a variety of disorders in warm-blooded animals, including neoplastic disorders. The receptor modulating agents are comprised of a covalently bound rerouting moiety and targeting moiety.
摘要翻译：能够通过影响细胞表面受体转运途径来调节细胞表面受体的受体调节剂用于治疗和诊断温血动物（包括肿瘤性疾病）中的各种疾病。受体调节剂由共价结合的重新路由部分和靶向部分组成。

8. 发明授权

US5840880A Receptor modulating agents 失效
标题翻译：受体调节剂
公开(公告)号：US5840880A
公开(公告)日：1998-11-24
申请号：US406191
申请日：1995-03-16
申请人： A. Charles Morgan, Jr. , D. Scott Wilbur
发明人： A. Charles Morgan, Jr. , D. Scott Wilbur
IPC分类号： C07H23/00 , C12P19/42 , A61K31/68
CPC分类号： C07H23/00
摘要： Receptor modulating agents capable of modulating cell surface receptors by affecting the cell surface receptor trafficking pathway. The receptor modulating agents are comprised of a covalently bound rerouting moiety and targeting moiety.
摘要翻译：能够通过影响细胞表面受体转运途径调节细胞表面受体的受体调节剂。受体调节剂由共价结合的重新路由部分和靶向部分组成。

9. 发明授权

US5609848A Radiohalogenated small molecules for protein labeling 失效
标题翻译：用于蛋白标记的放射性卤代小分子
公开(公告)号：US5609848A
公开(公告)日：1997-03-11
申请号：US764001
申请日：1991-09-23
申请人： D. Scott Wilbur , Alan R. Fritzberg
发明人： D. Scott Wilbur , Alan R. Fritzberg
IPC分类号： C07F3/12 , C07F7/22 , A61K51/02 , C07D207/40 , C07C25/02
CPC分类号： C07F7/2212 , C07F3/12
摘要： Haloaryl compounds are lithiated and thereafter metalated with one of the following organometallic groups: Sn(n--Bu).sub.3 or SnMe.sub.3. The resulting aryltin compound can be transmetalated in site-specific reaction with one of the following organometallic groups: HgX, Hg(OAc).sub.2, BX.sub.3, or BZ.sub.2, wherein X is Cl, Br, or I, and Z is alkyl or alkoxy. The metalated compounds are subsequently radiohalogenated via a demetalation reaction. A functional group suitable for conjugation to protein can be added subsequent or preferably prior to the radiohalogenation.Also compounds of the formula: R.sub.1 --Ar--R.sub.2, wherein R.sub.1 is either a radiohalogen or any one of the organometallic groups stated above, Ar is aromatic or heteroaromatic ring, and R.sub.2 is a short-chain substituent that does not activate the aromatic ring and that bears a functional group, or a precursor thereof, suitable for conjugation to protein under conditions that preserve the biological activity of the protein.The radiohalogenated small molecules are conjugated to proteins such as monoclonal antibodies for use in diagnosis and therapy.
摘要翻译：卤代芳基化合物被锂化，然后用以下有机金属组之一金属化：Sn（n-Bu）3或SnMe 3。所得的芳基锡化合物可以在以下有机金属基团之一的位置特异性反应中转金属：HgX，Hg（OAc）2，BX3或BZ2，其中X为Cl，Br或I，Z为烷基或烷氧基。金属化合物随后通过脱金属反应放射卤化。适于与蛋白质缀合的官能团可以随后或优选在放射性卤化之前添加。还有下式的化合物：R1-Ar-R2，其中R1是放射性卤素或上述有机金属基团中的任何一个，Ar是芳族或杂芳族环，R2是不活化芳环的短链取代基并且在保持蛋白质的生物活性的条件下具有适合于与蛋白质缀合的官能团或其前体。放射性卤化的小分子与蛋白质缀合，例如用于诊断和治疗的单克隆抗体。

10. 发明申请

US20170313656A1 Branched Discrete PEG Constructs 审中-公开
公开(公告)号：US20170313656A1
公开(公告)日：2017-11-02
申请号：US15630986
申请日：2017-06-23
申请人： Paul D. Davis , D. Scott Wilbur
发明人： Paul D. Davis , D. Scott Wilbur
IPC分类号： C07D209/60 , C07K16/30 , C07K14/605 , C07D403/14 , C07D257/02 , C07D209/48 , C07D207/404 , C07C331/28 , C07C317/44 , C07C279/24 , C07C271/16 , C07C235/48 , C07C235/08 , A61K51/10 , C07K16/40 , C07C2603/18
CPC分类号： C07D209/60 , A61K47/60 , A61K51/106 , C07C235/08 , C07C235/48 , C07C271/16 , C07C279/24 , C07C317/44 , C07C331/28 , C07C2603/18 , C07D207/404 , C07D209/48 , C07D257/02 , C07D403/14 , C07K14/605 , C07K16/3069 , C07K16/40
摘要： Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.

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