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1. 发明授权

US5514777A Methods of synthesis of peptidyl argininals 失效
标题翻译：肽基精氨酸合成方法
公开(公告)号：US5514777A
公开(公告)日：1996-05-07
申请号：US261380
申请日：1994-06-17
申请人： Thomas R. Webb , John E. Reiner , Susan Y. Tamura , William C. Ripka , Raymond Dagnino, Jr.
发明人： Thomas R. Webb , John E. Reiner , Susan Y. Tamura , William C. Ripka , Raymond Dagnino, Jr.
IPC分类号： A61K31/445 , A61K38/00 , A61P43/00 , C07D207/16 , C07D211/56 , C07D401/12 , C07K1/10 , C07K5/06 , C07K5/072 , C07K5/08 , C07K5/00 , C07D211/22 , C07K7/00 , C07K17/00
CPC分类号： C07D401/12 , C07D207/16 , C07D211/56 , C07K5/0606 , C07K5/06113 , A61K38/00
摘要： This invention provides solution-phase methods for the synthesis of peptidyl argininals and to novel reagents useful therein.
摘要翻译：本发明提供了用于合成肽基精氨酸的溶液相方法及其中有用的新型试剂。

2. 发明授权

US09328075B2 Pyrimidinone compounds and methods for treating influenza 有权
标题翻译：嘧啶酮化合物和治疗流行性感冒的方法
公开(公告)号：US09328075B2
公开(公告)日：2016-05-03
申请号：US14115560
申请日：2012-05-05
申请人： Thomas R. Webb , Vincent A. Boyd
发明人： Thomas R. Webb , Vincent A. Boyd
IPC分类号： C07D239/54 , C07D401/04 , C07D401/12 , C07D403/04 , C07D487/04 , A61K31/13 , A61K31/59 , A61K38/21 , A61K45/06 , A61K31/4045 , A61K31/5377 , A61K31/7012 , A61K31/551 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/196 , A61K31/215 , A61K31/351
CPC分类号： C07D239/54 , A61K31/13 , A61K31/196 , A61K31/215 , A61K31/351 , A61K31/4045 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/551 , A61K31/59 , A61K31/7012 , A61K38/21 , A61K45/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D487/04 , A61K2300/00
摘要： In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及可用于治疗和/或预防流感的新型广谱抗病毒，嘧啶酮化合物，使用方法，组合物和试剂盒。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

3. 发明授权

US08969405B2 Anticancer compounds and methods of making and using same 有权
标题翻译：抗癌化合物及其制备和使用方法
公开(公告)号：US08969405B2
公开(公告)日：2015-03-03
申请号：US12999218
申请日：2009-06-22
申请人： Thomas R. Webb , Chandraiah Lagisetti
发明人： Thomas R. Webb , Chandraiah Lagisetti
IPC分类号： C07D493/10 , C07D319/06 , A61K31/351 , A61K31/357
CPC分类号： C07D493/10 , A61K31/351 , A61K31/357 , C07D319/06
摘要： In one aspect, the invention relates to compounds having anticancer activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with uncontrolled cellular proliferation using the compounds and compositions. This abstract is intended to be used as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及具有抗癌活性的化合物; 制备化合物的合成方法; 包含该化合物的药物组合物; 以及使用所述化合物和组合物治疗与不受控制的细胞增殖相关的疾病的方法。该摘要旨在用作扫描工具，用于在特定技术中进行搜索，而不意在限制本发明。

4. 发明授权

US5714580A Trypsin Inhibitors 失效
标题翻译：胰蛋白酶抑制剂
公开(公告)号：US5714580A
公开(公告)日：1998-02-03
申请号：US455974
申请日：1995-05-31
申请人： Terence K. Brunck , Michael G. Pepe , Daniel A. Pearson , Thomas R. Webb
发明人： Terence K. Brunck , Michael G. Pepe , Daniel A. Pearson , Thomas R. Webb
IPC分类号： A61K38/55 , A61P1/00 , C07C251/76 , C07C281/10 , C07K1/113 , C07K5/072 , C07K5/078 , C07K5/093 , C07K14/81 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K5/06139 , C07C281/10 , C07K5/06104 , C07K5/06113
摘要： Novel compounds having activity against trypsin are disclosed. Specifically, novel peptide aldehyde analogues that have substantial potency and specificity as inhibitors of mammalian pancreatic trypsin are presented. The compounds are useful in the prevention and treatment of the tissue damage or destruction associated with pancreatitis.
摘要翻译：公开了具有抗胰蛋白酶活性的新型化合物。具体地说，具有作为哺乳动物胰腺胰蛋白酶抑制剂的实质效力和特异性的新型肽醛类似物。该化合物可用于预防和治疗与胰腺炎相关的组织损伤或破坏。

5. 发明授权

US5367072A Reagents for automated synthesis of peptide analogs 失效
标题翻译：自动合成肽类似物的试剂
公开(公告)号：US5367072A
公开(公告)日：1994-11-22
申请号：US807474
申请日：1991-12-13
申请人： Thomas R. Webb
发明人： Thomas R. Webb
IPC分类号： C07K1/04 , C08F8/30 , C07D225/00
CPC分类号： C07K1/042
摘要： Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
摘要翻译：提供了适用于使用自动肽合成肽合成的试剂和用于合成肽类似物的程序。

6. 发明授权

US06469166B2 Thiophenopyrimidines 有权
标题翻译：噻吩并嘧啶
公开(公告)号：US06469166B2
公开(公告)日：2002-10-22
申请号：US09896250
申请日：2001-06-29
申请人： Thomas R. Webb , Chen Chen , James R. McCarthy , Terence J. Moran
发明人： Thomas R. Webb , Chen Chen , James R. McCarthy , Terence J. Moran
IPC分类号： C07D49504
CPC分类号： C07D495/04
摘要： This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein X is S, SO or SO2; R1 is NR4R5 or OR5; R2 is C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl or C1-6alkyloxyC1-6alkyl; R5 is C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C1-6alkyloxy-C1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl; or a radical of formula -Alk-O—CO-Ar1; or R4 and R5 taken together with the nitrogen atom to which they are attached may form an optionally substituted pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group; Ar is phenyl, substituted phenyl, pyridinyl or substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of treating disorders related to hypersecretion of CRF such as depression, anxiety, substance abuse, by administering an effective amount of a compound of formula (I).
摘要翻译：本发明涉及包括立体异构体及其药学上可接受的酸加成盐形式的化合物，其中X是S，SO或SO 2; R1是NR4R5或OR5; R2是C1-6烷基，C1-6烷氧基或C1-6烷硫基; R3是氢，C1-6烷基，C1-6烷基磺酰基，C1-6烷基亚磺酰基或C1-6烷硫基; R4是氢，C1-6烷基，一或二（C3-6环烷基）甲基，C3-6环烷基，C3-6烯基，羟基C1-6烷基，C1-6烷基羰基氧基C 1-6烷基或C 1-6烷氧基C 1-6烷基; R5是C1-6烷基，单或二（C3-6环烷基）甲基，Ar1CH2，C1-6烷氧基-C 1-6烷基，羟基C 1-6烷基，C 3-6烯基，噻吩基甲基，呋喃基甲基，C 1-6烷硫基C 1-6烷基，吗啉基，单或二（C 1-6烷基）氨基C 1-6烷基，二（C 1-6烷基）氨基，C 1-6烷基羰基C 1-6烷基，被咪唑基取代的C 1-6烷基; 或式-Alk-O-CO-Ar1基团; 或R 4和R 5与它们所连接的氮原子一起可以形成任选取代的吡咯烷基，哌啶基，高哌啶基或吗啉基; Ar是苯基，取代的苯基，吡啶基或取代的吡啶基; 具有CRF受体拮抗特性; 含有这些化合物作为活性成分的药物组合物; 通过施用有效量的式（I）化合物来治疗与CRF过度分泌有关的疾病的方法，例如抑郁症，焦虑症，药物滥用。

7. 发明授权

US5886146A Inhibitors of thrombosis 失效
公开(公告)号：US5886146A
公开(公告)日：1999-03-23
申请号：US459705
申请日：1995-06-02
申请人： George P. Vlasuk , Thomas R. Webb , Daniel A. Pearson , Matthew M. Abelman
发明人： George P. Vlasuk , Thomas R. Webb , Daniel A. Pearson , Matthew M. Abelman
IPC分类号： A61K38/00 , A61K38/05 , A61K38/55 , A61P7/00 , A61P7/02 , A61P7/04 , C07C279/36 , C07C281/06 , C07C281/10 , C07D207/16 , C07D257/04 , C07K5/06 , C07K5/072 , C07K5/078 , A61K38/06
CPC分类号： C07K5/06113 , C07C279/36 , C07C281/06 , C07C281/10 , C07D207/16 , C07D257/04 , C07K5/06078 , C07K5/06104 , C07K5/06139 , A61K38/00
摘要： This invention relates to peptide aldehyde analogs that inhibit the thrombin or Factor Xa. The compounds are thought useful for preventing or treating conditions in mammal characterized by abnormal thrombosis.

8. 发明授权

US5534498A Trypsin inhibitors 失效
标题翻译：胰蛋白酶抑制剂
公开(公告)号：US5534498A
公开(公告)日：1996-07-09
申请号：US11666
申请日：1993-01-29
申请人： Terence K. Brunck , Michael G. Pepe , Daniel A. Pearson , Thomas R. Webb
发明人： Terence K. Brunck , Michael G. Pepe , Daniel A. Pearson , Thomas R. Webb
IPC分类号： A61K38/55 , A61P1/00 , C07C251/76 , C07C281/10 , C07K1/113 , C07K5/072 , C07K5/078 , C07K5/093 , C07K14/81 , A61K38/00 , C07K5/06 , C07K5/08
CPC分类号： C07K5/06139 , C07C281/10 , C07K5/06104 , C07K5/06113
摘要： Novel compounds having activity against trypsin are disclosed. Specifically, novel peptide aldehyde analogues that have substantial potency and specificity as inhibitors of mammalian pancreatic trypsin are presented. The compounds are useful in the prevention and treatment of the tissue damage or destruction associated with pancreatitis.
摘要翻译：公开了具有抗胰蛋白酶活性的新型化合物。具体地说，具有作为哺乳动物胰腺胰蛋白酶抑制剂的实质效力和特异性的新型肽醛类似物。该化合物可用于预防和治疗与胰腺炎相关的组织损伤或破坏。

9. 发明授权

US5492895A Inhibitors of thrombosis 失效
公开(公告)号：US5492895A
公开(公告)日：1996-02-20
申请号：US195995
申请日：1994-02-14
申请人： George P. Vlasuk , Thomas R. Webb , Daniel A. Pearson , Matthew M. Abelman
发明人： George P. Vlasuk , Thomas R. Webb , Daniel A. Pearson , Matthew M. Abelman
IPC分类号： A61K38/00 , A61K38/05 , A61K38/55 , A61P7/00 , A61P7/02 , A61P7/04 , C07C279/36 , C07C281/06 , C07C281/10 , C07D207/16 , C07D257/04 , C07K5/06 , C07K5/072 , C07K5/078 , A61K38/06
CPC分类号： C07K5/06113 , C07C279/36 , C07C281/06 , C07C281/10 , C07D207/16 , C07D257/04 , C07K5/06078 , C07K5/06104 , C07K5/06139 , A61K38/00
摘要： This invention relates to peptide aldehyde analogs that inhibit the thrombin or Factor Xa. The compounds are thought useful for preventing or treating conditions in mammal characterized by abnormal thrombosis.

10. 发明申请

US20140079666A1 PYRIMIDINONE COMPOUNDS AND METHODS FOR PREVENTING AND TREATING INFLUENZA 有权
标题翻译：吡咯米辛酮化合物和预防和治疗流感病毒的方法
公开(公告)号：US20140079666A1
公开(公告)日：2014-03-20
申请号：US14115560
申请日：2012-05-05
申请人： Thomas R. Webb , Vincent A. Boyd
发明人： Thomas R. Webb , Vincent A. Boyd
IPC分类号： C07D239/54 , A61K45/06 , A61K31/505 , A61K31/519 , C07D401/12 , C07D487/04 , A61K31/551 , A61K31/5377 , A61K31/506
CPC分类号： C07D239/54 , A61K31/13 , A61K31/196 , A61K31/215 , A61K31/351 , A61K31/4045 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/551 , A61K31/59 , A61K31/7012 , A61K38/21 , A61K45/06 , C07D401/04 , C07D401/12 , C07D403/04 , C07D487/04 , A61K2300/00
摘要： In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
摘要翻译：一方面，本发明涉及可用于治疗和/或预防流感的新型广谱抗病毒，嘧啶酮化合物，使用方法，组合物和试剂盒。该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。

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