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1.发明授权3-amino-2-oxo-1-piperidineacetic derivatives containing an arginine mimic as enzyme inhibitors 失效含有作为酶抑制剂的精氨酸模拟物的3-氨基-2-氧代-1-哌啶乙酸衍生物
公开(公告)号：US5932733A
公开(公告)日：1999-08-03
申请号：US482117
申请日：1995-06-07
Applicant: Joseph E. Semple , Odile E. Levy , Ruth F. Nutt , William C. Ripka
Inventor： Joseph E. Semple , Odile E. Levy , Ruth F. Nutt , William C. Ripka
IPC: A61K38/55 , A61K38/00 , A61K38/05 , A61P7/02 , C07K5/06 , C07K5/078 , A61K31/445 , C07D211/56
CPC classification number: A61K38/05 , C07K5/06139 , C07K5/06191
Abstract: The present invention discloses peptide aldehydes having a lactam group as part of the peptide backbone and having an original mimic group such as an amidinopiperidine or amidinophengyl tail. These compounds are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Abstract translation: 本发明公开了具有内酰胺基团作为肽主链的一部分并具有原始模拟基团如脒基哌啶或脒基生长基尾的肽醛。 这些化合物是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作特征在于异常血栓形成的哺乳动物中疾病状态的治疗剂的方法。
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公开(公告)号：US20080200371A1
公开(公告)日：2008-08-21
申请号：US12057609
申请日：2008-03-28
Applicant: Zacharia S. CHERUVALLATH , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
Inventor： Zacharia S. CHERUVALLATH , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
IPC: A61K31/675 , A61K38/28 , A61P3/04 , A61K31/426 , C07D277/38 , A61K31/433 , C07D285/135 , C07F9/28 , A61P7/12 , A61P9/12
CPC classification number: C07D277/38 , C07D277/42 , C07D285/135 , C07D417/12 , C07D417/14 , C07F9/6539 , C07F9/65395
Abstract: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.
Abstract translation: 提供化合物和组合物用于调节蛋白酪氨酸磷酸酶的活性。 在一个实施方案中，化合物和组合物是抑制蛋白酪氨酸磷酸酶1B活性的噻唑和噻二唑。
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公开(公告)号：US5567670A
公开(公告)日：1996-10-22
申请号：US468399
申请日：1995-06-06
Applicant: Kofi S. Amuti , Wonpyo Hong , Joseph E. Semple
Inventor： Kofi S. Amuti , Wonpyo Hong , Joseph E. Semple
IPC: A01N43/54 , C07D239/54 , C07D251/46 , C07D407/04 , C07D409/04 , C07D251/30 , A01N43/66
CPC classification number: C07D239/54 , A01N43/54 , C07D251/46 , C07D407/04 , C07D409/04
Abstract: This invention provides herbicides for use in plantation and specialty crops; and further provides novel substituted heterocyclic compounds, their agriculturally suitable compositions, and methods of using these compounds as preemergent or postemergent herbicides.
Abstract translation: 本发明提供用于种植和特种作物的除草剂; 并进一步提供新的取代的杂环化合物，其农业上合适的组合物，以及使用这些化合物作为出芽前或出芽后除草剂的方法。
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公开(公告)号：US4948418A
公开(公告)日：1990-08-14
申请号：US402178
申请日：1989-08-30
Applicant: Joseph E. Semple
Inventor： Joseph E. Semple
IPC: A01N43/12 , A01N43/16 , C07D209/48 , C07D405/04 , C07D471/04
CPC classification number: C07D209/48 , A01N43/12 , A01N43/16 , C07D405/04 , C07D471/04
Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.
Abstract translation: 本发明涉及新型杂环2,3-二氢苯并呋喃和苯并二氢吡喃化合物，包括立体异构体，含有它们的农业合适的组合物，以及它们作为广谱除草剂的用途。
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5.发明授权公开(公告)号：US07157596B2
公开(公告)日：2007-01-02
申请号：US10092004
申请日：2002-03-05
Applicant: Joseph E. Semple , Gary S. Coombs , John E. Reiner , Edgar O Ong , Gian Luca Araldi
Inventor： Joseph E. Semple , Gary S. Coombs , John E. Reiner , Edgar O Ong , Gian Luca Araldi
IPC: C07C261/00 , C07C229/00 , C01D7/37
CPC classification number: C12N9/6424
Abstract: The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions ameliorated by inhibition of matriptase or MTSP1.
Abstract translation: 本发明提供抑制matriptase或MTSP1的丝氨酸蛋白酶活性的化合物。 还提供了包含这些化合物的药物组合物和使用该化合物和药物组合物来治疗通过抑制matriptase或MTSP1而改善的病症的方法。
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Patent Agency Ranking
公开(公告)号：US07019019B2
公开(公告)日：2006-03-28
申请号：US10740946
申请日：2003-12-18
Applicant: David F. Duncan , L. Josue Alfaro-Lopez , Mallareddy Komandla , Odile Esther Levy , Ofir Moreno , Joseph E. Semple , Amir P. Tamiz
Inventor： David F. Duncan , L. Josue Alfaro-Lopez , Mallareddy Komandla , Odile Esther Levy , Ofir Moreno , Joseph E. Semple , Amir P. Tamiz
IPC: A61K31/44 , A61K31/425 , A61K31/38 , C07D333/22 , C07D211/72
CPC classification number: C07D231/56 , C07D333/38
Abstract: The present invention provides matriptase inhibitors and compositions thereof useful for treating cancer. Martripase is a trypsin-like serine protease active in the development of cancerous conditions, such as tumors and metastasis of cancer.
Abstract translation: 本发明提供了可用于治疗癌症的基质酶抑制剂及其组合物。 枸杞子是一种胰蛋白酶样的丝氨酸蛋白酶，可在肿瘤和肿瘤转移等癌症病症中起积极作用。
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7.发明授权Methods for the synthesis of &agr;- hydroxy-&bgr;-amino acid and amide derivatives 失效α-羟基-β-氨基酸和酰胺衍生物的合成方法公开(公告)号：US06376649B1
公开(公告)日：2002-04-23
申请号：US09216134
申请日：1998-12-18
Applicant: Joseph E. Semple , Odile E. Levy
Inventor： Joseph E. Semple , Odile E. Levy
IPC: G07K100
CPC classification number: C07C231/00 , Y02P20/55 , Y10T436/14 , Y10T436/141111
Abstract: Methods for the synthesis of &agr;-hydroxy-&bgr;-amino acid and amide derivatives and &agr;-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-&agr;-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl &agr;-ketoamides and &agr;-hydroxy-&bgr;-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
Abstract translation: 提供了通过这些方法制备的α-羟基-β-氨基酸和酰胺衍生物和α-酮酰胺衍生物和新型衍生物的合成方法。 这些方法包括使N-末端封闭的（保护的）氨基醛与异腈和羧酸反应，得到氨基-α-酰氧基甲酰胺。 可以除去酰氧基以得到衍生物。 或者，除去保护基团并发生酰基转移以得到衍生物。 这些衍生物可用于合成诸如肽基α-酮酰胺和α-羟基-β-羧酸和酰胺衍生物的化合物。 据报道，某些这些化合物具有蛋白酶抑制剂的活性，如丝氨酸蛋白酶和半胱氨酸蛋白酶。
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公开(公告)号：US5602077A
公开(公告)日：1997-02-11
申请号：US256339
申请日：1994-07-13
Applicant: Kofi S. Amuti , Wonpyo Hong , Joseph E. Semple
Inventor： Kofi S. Amuti , Wonpyo Hong , Joseph E. Semple
IPC: A01N43/54 , C07D239/54 , C07D251/46 , C07D407/04 , C07D409/04 , C07D239/553 , C07D239/545 , C07D239/557
CPC classification number: C07D239/54 , A01N43/54 , C07D251/46 , C07D407/04 , C07D409/04
Abstract: A method is disclosed for controlling the growth of undesired vegetation in a plantation crop by applying to the locus of the crop an effective amount of a compound of formula I ##STR1## and A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y and Z are as defined in the disclosure. Also disclosed are novel substituted heterocyclic compounds and their agriculturally suitable compositions which are generally useful as herbicides, as well as methods of their use as general or selective preemergent or postemergent herbicides, or as plant growth regulants.
Abstract translation: PCT No.PCT / US92 / 11330 Sec。 371日期：1994年7月13日 102（e）日期1994年7月13日PCT提交1992年12月30日PCT公布。 公开号WO93 / 14073 日期1993年7月22日公开了一种用于通过向作物场所施用有效量的式I化合物（IMAGE）和A，R1，R2，控制种植作物中不想要的植物生长的方法 ，R3，R4，X，Y和Z如本公开所定义。 还公开了新型取代的杂环化合物及其农业上合适的组合物，其通常可用作除草剂，以及它们用作一般或选择性前消化剂或芽后除草剂或作为植物生长调节剂的方法。
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公开(公告)号：US07381736B2
公开(公告)日：2008-06-03
申请号：US11219402
申请日：2005-09-02
Applicant: Zacharia S. Cheruvallath , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
Inventor： Zacharia S. Cheruvallath , Colin J. Loweth , Ruth F. Nutt , Darryl Rideout , Joseph E. Semple , Jing Wang , Feiyue Wu , Shankari Mylvaganam , Hengyi Zhu , Jianzhong Sun
IPC: A61K31/427 , C07D277/18
CPC classification number: C07D277/38 , C07D277/42 , C07D285/135 , C07D417/12 , C07D417/14 , C07F9/6539 , C07F9/65395
Abstract: Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.
Abstract translation: 提供化合物和组合物用于调节蛋白酪氨酸磷酸酶的活性。 在一个实施方案中，化合物和组合物是抑制蛋白酪氨酸磷酸酶1B活性的噻唑和噻二唑。
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10.发明授权3-amino-2-oxo-1-piperidineacetic derivatives containing an arginine mimic as enzyme inhibitors 失效含有作为酶抑制剂的精氨酸模拟物的3-氨基-2-氧代-1-哌啶乙酸衍生物
公开(公告)号：US5714499A
公开(公告)日：1998-02-03
申请号：US261498
申请日：1994-06-17
Applicant: Joseph E. Semple , Odile E. Levy , Ruth F. Nutt , William C. Ripka
Inventor： Joseph E. Semple , Odile E. Levy , Ruth F. Nutt , William C. Ripka
IPC: A61K38/00 , C07K5/078 , A61K31/445 , C07D401/12
CPC classification number: C07K5/06139 , A61K38/00
Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
Abstract translation: 本发明公开了肽醛，其是凝血酶的有效和特异性抑制剂，其药学上可接受的盐，药学上可接受的组合物，以及将其用作以异常血栓形成为特征的哺乳动物的疾病状态的治疗剂。
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