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1. 发明授权

US5798377A Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US5798377A
公开(公告)日：1998-08-25
申请号：US734148
申请日：1996-10-21
申请人： William C. Lumma , Thomas J. Tucker , Keith M. Witherup , Stephen F. Brady , Willie L. Whitter , Joseph P. Vacca , Craig Coburn , Jules A. Shafer
发明人： William C. Lumma , Thomas J. Tucker , Keith M. Witherup , Stephen F. Brady , Willie L. Whitter , Joseph P. Vacca , Craig Coburn , Jules A. Shafer
IPC分类号： C07D207/16 , A61K31/40 , C07D207/08 , C07D207/09
CPC分类号： C07D207/16
摘要： A compound which inhibits human thrombin and where has the structure ##STR1## such as ##STR2##
摘要翻译：抑制人类凝血酶的化合物，其结构如IMAGE>

2. 发明授权

US07479372B2 Beta-secretase substrates and uses thereof 失效
标题翻译： β-分泌酶底物及其用途
公开(公告)号：US07479372B2
公开(公告)日：2009-01-20
申请号：US11523507
申请日：2006-09-19
申请人： Stephen F. Brady , James E. Bruce , Elizabeth Chen-Dodson , Victor Garsky , Yueming Li , Mohinder Sardana , Jules A. Shafer , Xiaoting Tang
发明人： Stephen F. Brady , James E. Bruce , Elizabeth Chen-Dodson , Victor Garsky , Yueming Li , Mohinder Sardana , Jules A. Shafer , Xiaoting Tang
IPC分类号： G01N33/53
CPC分类号： C12Q1/37 , C07K7/06 , C07K14/4711 , C12P21/06 , G01N33/6896 , G01N2500/00
摘要： The present invention provides synthetic β-secretase peptide substrates useful in various assays for measuring β-secretase activity. Antibodies that recognize the synthetic substrates and uses of the antibodies in various assays are disclosed. The herein disclosed peptide substrates are hydrolyzed at rates substantially faster than the attendant Swedish mutant APP from which the substrate sequences are derived.
摘要翻译：本发明提供用于测量β-分泌酶活性的各种测定中的合成β-分泌酶肽底物。公开了在各种测定中识别合成底物和抗体应用的抗体。本文所公开的肽底物的水解速度明显快于从其中衍生出底物序列的瑞典突变体APP。

3. 发明授权

US07132401B2 Beta-secretase substrates and uses thereof 有权
公开(公告)号：US07132401B2
公开(公告)日：2006-11-07
申请号：US10480954
申请日：2002-05-17
申请人： Stephen F. Brady , James E. Bruce , Elizabeth Chen-Dodson , Victor Garsky , Yueming Li , Mohinder Sardana , Jules A. Shafer , Xiaoting Tang
发明人： Stephen F. Brady , James E. Bruce , Elizabeth Chen-Dodson , Victor Garsky , Yueming Li , Mohinder Sardana , Jules A. Shafer , Xiaoting Tang
IPC分类号： A61K38/08
CPC分类号： C12Q1/37 , C07K7/06 , C07K14/4711 , C12P21/06 , G01N33/6896 , G01N2500/00
摘要： The present invention provides synthetic β-secretase peptide substrates useful in various assays for measuring β-secretase activity. Antibodies that recognize the synthetic substrates and uses of the antibodies in various assays are disclosed. The herein disclosed peptide substrates are hydrolyzed at rates substantially faster than the attendant Swedish mutant APP from which the substrate sequences are derived.

4. 发明授权

US5672582A Thrombin inhibitors 失效
标题翻译：凝血酶抑制剂
公开(公告)号：US5672582A
公开(公告)日：1997-09-30
申请号：US322049
申请日：1994-10-12
申请人： Daniel F. Veber , S. Dale Lewis , Jules A. Shafer , Dong-Mei Feng , Ruth F. Nutt , Stephen F. Brady
发明人： Daniel F. Veber , S. Dale Lewis , Jules A. Shafer , Dong-Mei Feng , Ruth F. Nutt , Stephen F. Brady
IPC分类号： C07D211/36 , A61K31/16 , A61K31/19 , A61K31/215 , A61K31/40 , A61K31/445 , A61K38/00 , A61P7/02 , A61P43/00 , C07C237/10 , C07C271/22 , C07D207/16 , C07D211/60 , C07K5/02 , C07K5/06 , C07K5/065 , C07K5/087 , A61K38/05
CPC分类号： C07K5/0812 , C07K5/0202 , C07K5/06078 , C07K5/06191 , A61K38/00
摘要： 4-substituted cyclohexylamine derivatives which are thrombin catalytic site inhibitors and which are useful as anticoagulants. These compounds show selectivity for thrombin over other trypsin-like enzymes and have oral bioavailability. They have the formula ##STR1## for example ##STR2##
摘要翻译： 4-取代的环己胺衍生物，它们是凝血酶催化位点抑制剂，可用作抗凝剂。这些化合物显示凝血酶比其它胰蛋白酶样酶具有选择性并具有口服生物利用度。它们具有公式，例如

5. 发明授权

US06753410B2 Investigational compounds 失效
标题翻译：调查化合物
公开(公告)号：US06753410B2
公开(公告)日：2004-06-22
申请号：US09797820
申请日：2001-03-02
申请人： Alan John Nadin , Joseph George Neduvelil , Mohinder K. Sardana , Jules A. Shafer , Stephen J. Gardell , Ming-Tain Lai , Yueming Li , Bruce D. Dorsey , Dennis C. Dean
发明人： Alan John Nadin , Joseph George Neduvelil , Mohinder K. Sardana , Jules A. Shafer , Stephen J. Gardell , Ming-Tain Lai , Yueming Li , Bruce D. Dorsey , Dennis C. Dean
IPC分类号： C07K508
CPC分类号： C07K5/0207 , A61K38/00 , A61K38/55
摘要： The present invention is directed to compounds and pharmaceutical compositions comprising the compounds which are inhibitors of the enzyme gamma secretase and which are useful in the treatment or prevention of diseases in which the beta-amyloid peptide is involved, such as Alzheimer's disease.
摘要翻译：本发明涉及化合物和药物组合物，其包含作为γ-分泌酶抑制剂的化合物，其可用于治疗或预防涉及β-淀粉样蛋白肽的疾病，例如阿尔茨海默氏病。

6. 发明授权

US5728557A Method of making herpes simplex type 1 mutants and mutants so produced 失效
标题翻译：使单纯疱疹1型突变体和突变体产生的方法
公开(公告)号：US5728557A
公开(公告)日：1998-03-17
申请号：US458067
申请日：1995-06-01
申请人： R. Bruce Register , Jules A. Shafer
发明人： R. Bruce Register , Jules A. Shafer
IPC分类号： C12N9/50 , C12N15/10 , C12N15/00
CPC分类号： C12N9/503 , C12N15/102
摘要： A method for introducing a mutation into a desired site in Herpes Simplex Virus Type 1 uses a set of starting vectors, where each starting vector has a fragment of the substantially complete HSV-1 genome and also DNA which overlaps with a sequential genomic fragment contained in other starting vectors, so that upon co-transfection of a host cell, replication of viral DNA, and recombination, a mutated replicable virus is formed. The starting vector containing a gene which is to be mutated is replaced by a replacement vectors. The replacement vectors contain a copy of the mutated gene and overlapping DNA, and genomic DNA which was present in the starting vector. A host cell is transformed with the replacement vectors and the remaining starting vectors under conditions allowing replication of viral DNA and recombination to form a replicating mutated virus. In preferred embodiments, the protease gene is mutated.
摘要翻译：将突变引入单克隆单纯疱疹病毒1型中的所需位点的方法使用一组起始载体，其中每个起始载体具有基本上完整的HSV-1基因组的片段，以及与包含在其中的连续基因组片段重叠的DNA 其他起始载体，使得当共转染宿主细胞时，病毒DNA的复制和重组，形成突变的可复制病毒。含有待突变的基因的起始载体被替换载体所取代。替换载体含有突变基因和重叠DNA的拷贝，以及起始载体中存在的基因组DNA。在允许复制病毒DNA并重组以形成复制突变病毒的条件下，用置换载体和剩余起始载体转化宿主细胞。在优选的实施方案中，蛋白酶基因被突变。

7. 发明授权

US5646000A Compounds and methods for identifying activated platelets 失效
标题翻译：用于鉴定活化血小板的化合物和方法
公开(公告)号：US5646000A
公开(公告)日：1997-07-08
申请号：US315034
申请日：1994-09-29
申请人： Bohumil Bednar , Melissa Egbertson , Robert J. Gould , George D. Hartman , Jules A. Shafer
发明人： Bohumil Bednar , Melissa Egbertson , Robert J. Gould , George D. Hartman , Jules A. Shafer
IPC分类号： C07D401/06 , C07D405/14 , C07D491/22 , C07D495/04 , G01N33/569 , G01N33/80 , G01N33/86 , G01N33/567 , C07D401/14
CPC分类号： C07D401/06 , C07D405/14 , C07D495/04 , G01N33/56966 , G01N33/80 , G01N33/86 , G01N2500/00 , Y10S436/80 , Y10S436/811
摘要： The invention is directed to a series of novel compounds, and their pharmaceutically acceptable salts, of the formula ##STR1## wherein R is C.sub.0-6 alkyl substituted with R.sup.5 or a mono or polycyclic aromatic or heteroaromatic system comprised of 5 or 6-membered aromatic or heteroaromatic rings that are either unsubstituted or substituted with one or more of R.sup.1 and R.sup.2 ; R.sup.1 and R.sup.2 are independently C.sub.1-6 alkyl, carboxyl, hydroxyl, azido, nitro, amino, C.sub.1-6 alkylamino, C.sub.1-6 dialkylamino, arylamino, aryl C.sub.1-6 alkylamino, hydroxysulfonyl or arylazo; aryl is a phenyl or naphthyl ring which is unsubstituted or substituted with one or more of R.sup.3 and R.sup.4 ; R.sup.3 and R.sup.4 are independently C.sub.1-6 alkyl, azido, nitro, amino, C.sub.1-6 dialkylamino or hydroxysulfonyl; R.sup.5 is ##STR2## provided that when R is an unsubstituted monocyclic ring, the monocyclic ring is not phenyl or pyridyl. Such compounds are useful as fluorescent probes for identifying antiplatelet agents which selectively bind to activated platelets.
摘要翻译：本发明涉及一系列新颖的化合物及其药学上可接受的盐，其中R是被R 5取代的C 1-6烷基或由5或6元芳族的单或多环芳族或杂芳族体系或未被取代或被一个或多个R 1和R 2取代的杂芳环; R 1和R 2独立地是C 1-6烷基，羧基，羟基，叠氮基，硝基，氨基，C 1-6烷基氨基，C 1-6二烷基氨基，芳基氨基，芳基C 1-6烷基氨基，羟基磺酰基或芳基偶氮; 芳基是未被取代或被一个或多个R 3和R 4取代的苯基或萘基环; R 3和R 4独立地为C 1-6烷基，叠氮基，硝基，氨基，C 1-6二烷基氨基或羟基磺酰基; R5是或，条件是当R是未取代的单环时，单环不是苯基或吡啶基。这样的化合物可用作识别选择性结合活化血小板的抗血小板剂的荧光探针。

8. 发明授权

US07230005B2 Compounds and methods for lowering the abuse potential and extending the duration of action of a drug 有权
标题翻译：用于降低滥用潜力并延长药物作用时间的化合物和方法
公开(公告)号：US07230005B2
公开(公告)日：2007-06-12
申请号：US10800898
申请日：2004-03-15
申请人： Jules A. Shafer , Vladislav V. Telyatnikov , Zhiwei Guo
发明人： Jules A. Shafer , Vladislav V. Telyatnikov , Zhiwei Guo
IPC分类号： A61K31/485 , C07D489/02
CPC分类号： C07D489/08 , A61K47/555 , A61K47/60
摘要： The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.
摘要翻译：降低生物可利用药物如鸦片止痛剂的滥用潜力，并且通过在制剂前将其转化为不良吸收的酯前药或其它前药衍生物来延长其作用时间。与活性药物的许多现有持续释放制剂不同，其中通过咀嚼，破碎或以其它方式破坏含有活性药剂的片剂或胶囊珠可以释放活性药剂，这种包含本发明前药的片剂或胶囊珠粒的机械加工既不释放活性药物也不妥协药物对药物的受控转化。此外，含有本发明前药或其他药物的片剂和胶囊珠可以用足量的增稠剂如羟丙基甲基纤维素或羧甲基纤维素配制，以阻止对这些给药模式未注明的制剂的不适当的静脉内和鼻内施用。

9. 发明授权

US4795714A Compositions for controllably releasing alcohols or amines 失效
标题翻译：用于可控释放醇或胺的组合物
公开(公告)号：US4795714A
公开(公告)日：1989-01-03
申请号：US757649
申请日：1985-07-22
申请人： Jules A. Shafer
发明人： Jules A. Shafer
IPC分类号： G01K3/04 , G01N31/22 , A01N25/10 , A61K7/32 , C09K3/00 , G01N33/00
CPC分类号： G01N31/229 , G01K3/04
摘要： An adjustable accumulated thermal exposure indicator device, and method of use, for affixing to and indicating deterioration of perishable goods and the like, comprising (1) a reactant yielding material that reacts via one or more steps at a rate depending on time, temperature, and pH to provide an amine and (2) an indicator that reacts at a time, temperature, concentration and pH dependent rate with the amine to produce a visible reaction that is indicative of the expiration of a predetermined time-temperature history related to the useful life of the goods to which the device is affixed. Also provided is a device or article that is responsive to accumulated thermal exposure for the controlled release of immobilized alcohols and amines.
摘要翻译：一种可调累积的热曝光指示装置及其使用方法，用于固定和指示易腐货品等的劣化，包括（1）反应物产生材料，其通过一个或多个步骤以取决于时间，温度，和pH以提供胺和（2）指示剂，其随时间，温度，浓度和pH依赖速率与胺反应以产生可见反应，其指示与有用的相关的预定时间历史的期满装置所附货物的寿命。还提供了响应于积累的热暴露以控制固定的醇和胺的释放的装置或制品。

10. 发明授权

US09034893B2 Process for reducing contaminating michael acceptor levels in oxycodone and other compositions 有权
标题翻译：用于减少羟考酮和其他组合物中污染的迈克尔受体水平的方法
公开(公告)号：US09034893B2
公开(公告)日：2015-05-19
申请号：US12960991
申请日：2010-12-06
申请人： Jules A. Shafer , Vladislav V. Telyatnikov , Hao Wang
发明人： Jules A. Shafer , Vladislav V. Telyatnikov , Hao Wang
IPC分类号： A61K31/485 , C07D489/08 , C07D489/02
CPC分类号： A23L5/27 , A23V2002/00 , C07D489/02 , C07D489/08 , G01N30/74 , G01N33/02 , G01N33/15 , G01N2030/027
摘要： The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
摘要翻译：本发明涉及从某些组合物中除去迈克尔受体的方法，其中组合物在足以除去迈克尔受体和所得到的硫醇 - 迈克尔加合物的条件下用含硫醇的化合物处理。本发明的某些实施方案能够定量和/或去除迈克尔受体和/或迈克尔受体前体。

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