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1. 发明授权

US06702705B1 Prodrugs activated by targeted catalytic proteins 失效
标题翻译：由靶向催化蛋白激活的前药
公开(公告)号：US06702705B1
公开(公告)日：2004-03-09
申请号：US08392407
申请日：1995-02-22
申请人： Reid von Borstel , Jan M. Casadei , Balreddy Kamireddy , John Kenten , Mark T. Martin , Richard J. Massey , Andrew D. Napper , David M. Simpson , Rodger Smith , Richard C. Titmas , Richard O. Williams
发明人： Reid von Borstel , Jan M. Casadei , Balreddy Kamireddy , John Kenten , Mark T. Martin , Richard J. Massey , Andrew D. Napper , David M. Simpson , Rodger Smith , Richard C. Titmas , Richard O. Williams
IPC分类号： C12N900
CPC分类号： C07D207/404 , C07C229/46 , C07C229/48 , C07C235/74 , C07C271/24 , C07C311/06 , C07C311/19 , C07C317/44 , C07C2601/04 , C07C2602/42 , C07D205/085 , C07F9/2408 , C07F9/2458 , C07F9/301 , C07F9/3211 , C07F9/4006 , C07F9/4075 , C07F9/5537 , C07F9/650952 , C07F9/657181 , C07H15/252 , C07H19/04 , C07K14/55 , C07K16/00 , C07K16/1063 , C07K16/26 , C07K16/44 , C07K16/468 , C07K2319/00 , C12N9/0002 , C12Q1/25 , G01N33/5008 , G01N33/531 , G01N33/577 , G01N2333/16 , G01N2333/96472 , G01N2500/00
摘要： Catalytic antibodies are disclosed. The catalytic antibodies are specific for prodrug compounds. The catalytic antibodies enhance cleavage of an active drug moiety from a prodrug residue, thereby activating the drug.
摘要翻译：公开了催化抗体。催化抗体对前药化合物是特异性的。催化抗体增强了活性药物部分与前药残留物的切割，从而激活了药物。

2. 发明授权

US06258360B1 Prodrugs activated by targeted catalytic proteins 失效
标题翻译：由靶向催化蛋白激活的前药
公开(公告)号：US06258360B1
公开(公告)日：2001-07-10
申请号：US08325554
申请日：1994-10-18
申请人： Reid von Borstel , Jan M. Casadei , Balreddy Kamireddy , John Henry Kenten , Mark T. Martin , Richard J. Massey , Andrew D. Napper , David M. Simpson , Rodger G. Smith , Richard C. Titmas , Richard O. Williams
发明人： Reid von Borstel , Jan M. Casadei , Balreddy Kamireddy , John Henry Kenten , Mark T. Martin , Richard J. Massey , Andrew D. Napper , David M. Simpson , Rodger G. Smith , Richard C. Titmas , Richard O. Williams
IPC分类号： A61K3944
CPC分类号： C07H15/252 , C07C311/19 , C07F9/2408 , C07F9/2458 , C07F9/4006 , C07F9/4075 , C07F9/650952 , C07F9/657181 , C07H19/04 , C07K14/55 , C07K16/26 , C07K16/44 , C07K16/468 , C07K2319/00 , C12N9/0002 , G01N33/5008 , G01N2500/00
摘要： Prodrugs that are activated by and conjugated to a catalytic antibody conjugated to a moiety that binds to a tumor cell population are provided.
摘要翻译：提供由与结合肿瘤细胞群的部分缀合的催化抗体活化并与其缀合的前药。

3. 发明授权

US5593969A Lipid-A analogs: monosaccharide and dissaccharide compounds for inhibiting binding of lipid A receptors to lipid A receptors 失效
标题翻译：脂质-A类似物：用于抑制脂质A受体与脂质A受体结合的单糖和非糖化合物
公开(公告)号：US5593969A
公开(公告)日：1997-01-14
申请号：US123590
申请日：1993-09-17
申请人： Balreddy Kamireddy , Michael J. Darsley , David M. Simpson , Richard J. Massey
发明人： Balreddy Kamireddy , Michael J. Darsley , David M. Simpson , Richard J. Massey
IPC分类号： A61K38/00 , C07H13/06 , C07H15/04 , C07K16/12 , A61K31/70 , C07H3/02 , C07H3/04
CPC分类号： C07H13/06 , C07H15/04 , C07K16/1203 , A61K38/00
摘要： A compound of the formula: ##STR1## wherein: each of R.sub.1, R.sub.1 ', R.sub.2 and R.sub.2 ' independent of each other is a substituted or unsubstituted, branched or linear C.sub.1-12 alkyl, alkene or alkyne group, R.sub.3 is OH, OCH.sub.3, CH.sub.2 COOH or ##STR2## wherein each of R.sub.2" and R.sub.2 '41 independent of each other is a substituted or unsubstituted, branched or linear C.sub.1-12 alkyl, alkene or alkyne group and:A=NH.sub.2, X=P(OH), Y=Z=C, B=OCH.sub.3, orA=OH, X=P(OH), X=Z=C, B (if present)=OCH.sub.3, orA=OCO(CH.sub.2).sub.n NH.sub.2, X=P(OH), Y=Z=C, B=OCH.sub.3,wherein n=1-10, orA=OH, X=P(OH), Y=Z=C, B=O(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, orA=OH, X=P(OH), Y=Z=C, B=(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, orA=NH.sub.2, X=Z=C, Y=P(OH), B=OCH.sub.3, orA=OH, X=Z=C, Y=P(OH), B (if present)=OCH.sub.3, orA=OCO(CH.sub.2).sub.n NH.sub.2, X=Z=C, Y=P(OH), B=OCH.sub.3, wherein n=1-10, orA=OH, X=Z=C, Y=P(OH), B=O(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, orA=OH, X=Z=C, Y=P(OH), B=(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-11, orA=NH.sub.2, X=Y=C, Z=P(OH), B=OCH.sub.3, orA=OH, X=Y=C, Z=P(OH), B (if present)=OCH.sub.3, orA=OCO(CH.sub.2).sub.n NH.sub.2, X=Y=C, Z=P(OH), B=OCH.sub.3, wherein n=1-10, orA=OH, X=Y=C, Z=P(OH), B=O(CH.sub.2).sub.n CO.sub.2 H, wherein n=1-10, orA=OH, X=Y=C, Z=P (OH), B=(CH.sub.2).sub.n CO.sub.2 H and n=1-11 is disclosed. The compounds may be use to inhibit binding of Lipid A to Lipid A receptors.
摘要翻译：下式的化合物：其中：R 1，R 1'，R 2和R 2'彼此独立地为取代或未取代的支链或直链C 1-12烷基，烯烃或炔基，R 3为 OH，OCH 3，CH 2 COOH或者其中每个R 2“和R 21'彼此独立地是取代或未取代的支链或直链C 1-12烷基，烯烃或炔基，并且：A = NH 2，X = P （OH），Y = Z = C，B = OCH 3或A = OH，X = P（OH），X = Z = C，B（如果存在）= OCH 3或A = OCO（CH 2）n NH 2，X = P（OH），Y = Z = C，B = OCH 3，其中n = 1-10，或A = OH，X = P（OH），Y = Z = C，B = O（CH 2）n CO 2 H，其中 n = 1-10，或A = OH，X = P（OH），Y = Z = C，B =（CH2）nCO2H，其中n = 1-10，或A = NH2，X = Z = C，Y = P（OH），B = OCH3或A = OH，X = Z = C，Y = P（OH），B（如果存在）= OCH 3或A = OCO（CH 2）n NH 2，X = Z = C ，Y = P（OH），B = OCH 3，其中n = 1-10，或A = OH，X = Z = C，Y = P（OH），B = O（CH 2）n CO 2 H，其中n = 10或A = OH，X = Z = C，Y = P（OH），B =（CH2）nCO2H，其中n = 1-11或A = NH2，X = Y = C，Z = P ），B = OCH 3或A = OH，X = Y = C，Z = P（OH），B（如果存在）= OCH 3或A = OCO（CH 2）n NH 2，X = Y = C，Z = P （OH），B = OCH 3，其中n = 1-10，或A = OH，X = Y = C，Z = P（OH），B = O（CH 2）n CO 2 H，其中n = 1-10，或A = OH，X = Y = C ，Z = P（OH），B =（CH2）nCO2H和n = 1-11。该化合物可用于抑制脂质A与脂质A受体的结合。

4. 发明授权

US5597573A Lipid-A analogs: new monosaccharide and disaccharide intermediates for eliciting therapeutic antibodies and for antitumor and antiviral activities 失效
标题翻译：脂类-A类似物：用于引发治疗性抗体和抗肿瘤和抗病毒活性的新单糖和二糖中间体
公开(公告)号：US5597573A
公开(公告)日：1997-01-28
申请号：US405438
申请日：1995-03-14
申请人： Balreddy Kamireddy , Michael J. Darsley , David M. Simpson , Richard J. Massey
发明人： Balreddy Kamireddy , Michael J. Darsley , David M. Simpson , Richard J. Massey
IPC分类号： A61K38/00 , C07H13/06 , C07H15/04 , C07K16/12 , A61K39/02 , A61K31/70 , C07H17/02
CPC分类号： C07H13/06 , C07H15/04 , C07K16/1203 , A61K38/00
摘要： The present invention relates to novel amidine components of formula (II): ##STR1## A method for eliciting antibodies in an animal which bind to Lipid A or LPS comprising administering to the animal as an immunogen a composition comprising such a compound is also disclosed.
摘要翻译：本发明涉及式（II）的新型脒组分：（II）在结合脂质A或LPS的动物中引发抗体的方法，包括向动物作为免疫原施用包含这种化合物的组合物也披露。

5. 发明授权

US5631137A Reaction-based selection for expression of and concentration of catalytic moieties 失效
标题翻译：用于催化部分的表达和浓缩的基于反应的选择
公开(公告)号：US5631137A
公开(公告)日：1997-05-20
申请号：US377495
申请日：1995-01-24
申请人： Mark T. Martin , Rodger G. Smith , Michael J. Darsley , David M. Simpson , Gary F. Blackburn
发明人： Mark T. Martin , Rodger G. Smith , Michael J. Darsley , David M. Simpson , Gary F. Blackburn
IPC分类号： G01N33/53 , B01J20/281 , C12N5/10 , C12N7/02 , C12N15/10 , C12Q1/02 , C12Q1/68 , C12Q1/70 , C40B40/02 , G01N30/88 , G01N33/569 , C12Q1/25 , C12N9/00
CPC分类号： C40B40/02 , C12N15/1037 , C12Q1/02 , C12Q1/6811 , C12Q1/70 , G01N33/56983
摘要： Disclosed and claimed are methods for selecting a recombinant virus, phage or cell expressing a catalytic antibody or catalytic portion thereof, or for selecting catalytic activity by a moiety. The method employs reaction-based selection for catalytic activity. The method can also be used to concentrate (increase the proportion of catalytic to non-catalytic moieties) a sample containing a catalytic moiety or viruses, phages or cells expressing a catalytic moiety. The selection or concentrating can be by employing a mechanism-based inhibitor, catalysis-accelerated movement, surface binding, changes in enthalpic component of binding as a function of temperature, or changes in binding by competition, or combinations thereof. The invention also comprehends a method for producing a recombinant virus or a cell-line expressing a catalytic moiety such as a catalytic antibody or catalytic portion thereof; and, this method can include infecting a suitable host with viruses which are screened for the expression. In addition, recombinant viruses and cell-lines so expressing a catalytic moiety such as a catalytic antibody or catalytic portion thereof are also disclosed and claimed.
摘要翻译：公开并要求的是选择重组病毒，表达催化抗体或其催化部分的噬菌体或细胞，或用于通过部分选择催化活性的方法。该方法采用基于反应的催化活性选择。该方法还可用于浓缩（增加非催化部分的催化剂比例）含有催化部分或表达催化部分的病毒，噬菌体或细胞的样品。选择或浓缩可以通过采用基于机理的抑制剂，催化加速运动，表面结合，作为温度的函数的结合焓分量的变化，或通过竞争的结合变化，或其组合。本发明还包括生产重组病毒或表达催化部分如催化抗体或其催化部分的细胞系的方法; 并且该方法可以包括用筛选表达的病毒感染合适的宿主。此外，还公开和要求保护了重组病毒和表达催化部分如催化抗体或其催化部分的细胞系。

6. 发明授权

US06177270B1 Reaction-based selection for expression of and concentration of catalytic moieties 失效
标题翻译：用于催化部分的表达和浓缩的基于反应的选择
公开(公告)号：US06177270B1
公开(公告)日：2001-01-23
申请号：US09235353
申请日：1999-01-21
申请人： Mark T. Martin , Rodger G. Smith , Michael J. Darsley , David M. Simpson , Gary F. Blackburn
发明人： Mark T. Martin , Rodger G. Smith , Michael J. Darsley , David M. Simpson , Gary F. Blackburn
IPC分类号： C12N700
CPC分类号： C40B40/02 , C12N15/1037 , C12Q1/02 , C12Q1/6811 , C12Q1/70 , G01N33/56983
摘要： Disclosed and claimed are methods for selecting a recombinant virus, phage or cell expressing a catalytic antibody or catalytic portion thereof, or for selecting catalytic activity by a moiety. The method employs reaction-based selection for catalytic activity. The method can also be used to concentrate (increase the proportion of catalytic to non-catalytic moieties) a sample containing a catalytic moiety or viruses, phages or cells expressing a catalytic moiety. The selection or concentrating can be by employing a mechanism-based inhibitor, catalysis-accelerated movement, surface binding, changes in enthalpic component of binding as a function of temperature, or changes in binding by competition, or combinations thereof. The invention also comprehends a method for producing a recombinant virus or a cell-line expressing a catalytic moiety such as a catalytic antibody or catalytic portion thereof; and, this method can include infecting a suitable host with viruses which are screened for the expression. In addition, recombinant viruses and cell-lines so expressing a catalytic moiety such as a catalytic antibody or catalytic portion thereof are also disclosed and claimed.
摘要翻译：公开并要求的是选择重组病毒，表达催化抗体或其催化部分的噬菌体或细胞，或用于通过部分选择催化活性的方法。该方法采用基于反应的催化活性选择。该方法还可用于浓缩（增加非催化部分的催化剂比例）含有催化部分或表达催化部分的病毒，噬菌体或细胞的样品。选择或浓缩可以通过采用基于机理的抑制剂，催化加速运动，表面结合，作为温度的函数的结合焓分量的变化，或通过竞争的结合变化，或其组合。本发明还包括生产重组病毒或表达催化部分如催化抗体或其催化部分的细胞系的方法; 并且该方法可以包括用筛选表达的病毒感染合适的宿主。此外，还公开和要求保护了重组病毒和表达催化部分如催化抗体或其催化部分的细胞系。

7. 发明授权

US6121007A Reaction-based selection for expression of and concentration of catalytic moieties 失效
标题翻译：用于催化部分的表达和浓缩的基于反应的选择
公开(公告)号：US6121007A
公开(公告)日：2000-09-19
申请号：US747654
申请日：1996-11-13
申请人： Mark T. Martin , Rodger G. Smith , Michael J. Darsley , David M. Simpson , Gary F. Blackburn
发明人： Mark T. Martin , Rodger G. Smith , Michael J. Darsley , David M. Simpson , Gary F. Blackburn
IPC分类号： G01N33/53 , B01J20/281 , C12N5/10 , C12N7/02 , C12N15/10 , C12Q1/02 , C12Q1/68 , C12Q1/70 , C40B40/02 , G01N30/88 , G01N33/569 , C12Q1/25
CPC分类号： C40B40/02 , C12N15/1037 , C12Q1/02 , C12Q1/6811 , C12Q1/70 , G01N33/56983
摘要： Disclosed and claimed are methods for selecting a recombinant virus, phage or cell expressing a catalytic antibody or catalytic portion thereof, or for selecting catalytic activity by a moiety. The method employs reaction-based selection for catalytic activity. The method can also be used to concentrate (increase the proportion of catalytic to non-catalytic moieties) a sample containing a catalytic moiety or viruses, phages or cells expressing a catalytic moiety. The selection or concentrating can be by employing a mechanism-based inhibitor, catalysis-accelerated movement, surface binding, changes in enthalpic component of binding as a function of temperature, or changes in binding by competition, or combinations thereof. The invention also comprehends a method for producing a recombinant virus or a cell-line expressing a catalytic moiety such as a catalytic antibody or catalytic portion thereof; and, this method can include infecting a suitable host with viruses which are screened for the expression. In addition, recombinant viruses and cell-lines so expressing a catalytic moiety such as a catalytic antibody or catalytic portion thereof are also disclosed and claimed.
摘要翻译：公开并要求的是选择重组病毒，表达催化抗体或其催化部分的噬菌体或细胞，或用于通过部分选择催化活性的方法。该方法采用基于反应的催化活性选择。该方法还可用于浓缩（增加非催化部分的催化剂比例）含有催化部分或表达催化部分的病毒，噬菌体或细胞的样品。选择或浓缩可以通过采用基于机理的抑制剂，催化加速运动，表面结合，作为温度的函数的结合焓分量的变化，或通过竞争的结合变化，或其组合。本发明还包括生产重组病毒或表达催化部分如催化抗体或其催化部分的细胞系的方法; 并且该方法可以包括用筛选表达的病毒感染合适的宿主。此外，还公开和要求保护了重组病毒和表达催化部分如催化抗体或其催化部分的细胞系。

8. 发明授权

US5891648A Reaction-based selection for expression of and concentration of catalytic moieties 失效
公开(公告)号：US5891648A
公开(公告)日：1999-04-06
申请号：US748415
申请日：1996-11-13
申请人： Mark T. Martin , Rodger G. Smith , Michael J. Darsley , David M. Simpson , Gary F. Blackburn
发明人： Mark T. Martin , Rodger G. Smith , Michael J. Darsley , David M. Simpson , Gary F. Blackburn
IPC分类号： G01N33/53 , B01J20/281 , C12N5/10 , C12N7/02 , C12N15/10 , C12Q1/02 , C12Q1/68 , C12Q1/70 , C40B40/02 , G01N30/88 , G01N33/569 , C12Q1/25
CPC分类号： C40B40/02 , C12N15/1037 , C12Q1/02 , C12Q1/6811 , C12Q1/70 , G01N33/56983
摘要： Disclosed and claimed are methods for selecting a recombinant virus, phage or cell expressing a catalytic antibody or catalytic portion thereof, or for selecting catalytic activity by a moiety. The method employs reaction-based selection for catalytic activity. The method can also be used to concentrate (increase the proportion of catalytic to non-catalytic moieties) a sample containing a catalytic moiety or viruses, phages or cells expressing a catalytic moiety. The selection or concentrating can be by employing a mechanism-based inhibitor, catalysis-accelerated movement, surface binding, changes in enthalpic component of binding as a function of temperature, or changes in binding by competition, or combinations thereof. The invention also comprehends a method for producing a recombinant virus or a cell-line expressing a catalytic moiety such as a catalytic antibody or catalytic portion thereof; and, this method can include infecting a suitable host with viruses which are screened for the expression. In addition, recombinant viruses and cell-lines so expressing a catalytic moiety such as a catalytic antibody or catalytic portion thereof are also disclosed and claimed.

9. 发明授权

US6016999A Spacecraft platforms 失效
标题翻译：航天器平台
公开(公告)号：US6016999A
公开(公告)日：2000-01-25
申请号：US109385
申请日：1998-07-02
申请人： David M. Simpson , Joseph Daniel McCaughey , Charles David Hall
发明人： David M. Simpson , Joseph Daniel McCaughey , Charles David Hall
IPC分类号： B64G1/10 , B64G1/22 , B64G1/66 , B64G1/00
CPC分类号： B64G1/222 , B64G1/1007 , B64G1/1021 , B64G1/66 , B64G2001/1035
摘要： A spacecraft platform essentially having two or more panels hinged at the base and contained for launch in a fairing. The panels are hinged and latched in an open deployment and bear, for example, a SAR antenna or an interferometer. The rear faces of the panels are provided with stiffening ribs, webs and struts and carry elements of the payload module and service module which are normally separate structures on a conventional satellite.
摘要翻译：一个航天器平台基本上具有两个或多个铰接在基座上的面板，用于在整流罩中发射。面板铰接并锁定在开放的部署中，并承载例如SAR天线或干涉仪。面板的后表面设置有加强筋，腹板和支柱以及有效载荷模块和服务模块的承载元件，这些模块和服务模块通常是常规卫星上分离的结构。

10. 发明授权

US06218519B1 Compounds and methods for the selective treatment of cancer and bacterial infections 失效
标题翻译：用于选择性治疗癌症和细菌感染的化合物和方法
公开(公告)号：US06218519B1
公开(公告)日：2001-04-17
申请号：US08635243
申请日：1996-04-12
申请人： John H. Kenten , David M. Simpson
发明人： John H. Kenten , David M. Simpson
IPC分类号： C07H1524
CPC分类号： C07H15/252
摘要： The present invention relates to compounds containing an anthracyclinone group such as doxorubicin, daunorubicin or a derivative thereof. The compounds of the invention also contain ester, glycoside or glucuronide structures which are hydrolyzed by the corresponding esterase, glycosidase or glucuronidase. These compounds possess potent cytotoxic activity which is developed after the hydrolysis of the ester or glycoside group of the compound and are effective in the inhibition of tumor cells and bacterial growth after activation.
摘要翻译：本发明涉及含有蒽环类基团的化合物，例如多柔比星，柔红霉素或其衍生物。本发明的化合物还含有由相应的酯酶，糖苷酶或葡糖苷酸酶水解的酯，糖苷或葡糖苷酸结构。这些化合物具有强效的细胞毒活性，其在化合物的酯或糖苷基团水解后发展，并且在活化后有效抑制肿瘤细胞和细菌生长。

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