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21. 发明授权

US5703067A Inhibitors of farnesyl-protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US5703067A
公开(公告)日：1997-12-30
申请号：US435047
申请日：1995-05-08
申请人： Hiranthi Jayasuriya , Russell B. Lingham , Fernando Pelaez , Manuel Sanchez , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink
发明人： Hiranthi Jayasuriya , Russell B. Lingham , Fernando Pelaez , Manuel Sanchez , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink
IPC分类号： A61K31/575 , C07J9/00 , C07J17/00
CPC分类号： A61K31/573 , A61K31/575 , C07J17/00 , C07J9/00
摘要： The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer. The compounds of this invention have the following structure: ##STR1##
摘要翻译：本发明涉及抑制法呢基蛋白转移酶（FPTase）的甾族化合物或萜类化合物。本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶和治疗癌症的方法。本发明的化合物具有以下结构：

22. 发明授权

US5627057A Inhibitor compounds of farnesyl-protein transferase and chemotherapeutic compositions containing the same, produced by strain ATCC 55532 失效
标题翻译：法呢基蛋白转移酶的抑制剂化合物和含有该化合物的化学治疗组合物，由ATCC 55532
公开(公告)号：US5627057A
公开(公告)日：1997-05-06
申请号：US611700
申请日：1996-03-06
申请人： Sheo B. Singh , George M. Garrity , Olga Genillourd , Russell B. Lingham , Isabel Martin , Mary Nallin-Omstead , Keith C. Silverman , Deborah L. Zink
发明人： Sheo B. Singh , George M. Garrity , Olga Genillourd , Russell B. Lingham , Isabel Martin , Mary Nallin-Omstead , Keith C. Silverman , Deborah L. Zink
IPC分类号： A61K31/225 , A61K31/231 , A61K31/232 , A61K31/365 , C07C69/738 , C07D321/00 , C12P17/08 , C12N1/20 , C12P1/06 , C12P33/00
CPC分类号： C12R1/045 , A61K31/225 , A61K31/231 , A61K31/232 , A61K31/365 , C07C69/738 , C07D321/00 , C12P17/08 , Y10S435/822
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras. Furthermore, Actinoplanes sp. ATCC 55532 and Streptomces sp. ATCC 55550 are microorganisms which are capable of producing the disclosed compounds which are classified as carboxylic acid esters. In addition a method for preparing the compounds is disclosed which includes cultivating strain ATCC 55532 or strain ATCC 55550. The strains are independently capable of producing the carboxylic acid ester compounds.
摘要翻译：本发明涉及抑制法呢基蛋白转移酶（FPTase）和致癌基因蛋白Ras的法呢基化的化合物。本发明进一步涉及含有本发明化合物的化疗组合物和抑制法呢基蛋白转移酶的方法和癌基因蛋白Ras的法呢基化。此外，Actinoplanes sp。 ATCC 55532和Streptomces sp。 ATCC 55550是能够产生被分类为羧酸酯的公开化合物的微生物。此外，公开了制备化合物的方法，其包括培养菌株ATCC 55532或菌株ATCC 55550.菌株独立地能够产生羧酸酯化合物。

23. 发明授权

US5543431A Anti-fungal agents 失效
公开(公告)号：US5543431A
公开(公告)日：1996-08-06
申请号：US449622
申请日：1995-05-24
申请人： Evon A. Bolessa , Robert E. Schwartz , Gerald F. Bills , Robert A. Giacobbe , Fernando Pelaez Perez , Angeles Cabello Arroyo , Teresa Diez Matas , Isabel Martin Fernandez , Francisca Vicente Perez , Suzanne M. Mandala , Deborah L. Zink , Rosemary Thornton , John R. Thompson , James E. Curotto
发明人： Evon A. Bolessa , Robert E. Schwartz , Gerald F. Bills , Robert A. Giacobbe , Fernando Pelaez Perez , Angeles Cabello Arroyo , Teresa Diez Matas , Isabel Martin Fernandez , Francisca Vicente Perez , Suzanne M. Mandala , Deborah L. Zink , Rosemary Thornton , John R. Thompson , James E. Curotto
IPC分类号： C07D207/12 , C07C233/09 , A61K31/16 , A61K31/695 , C07C233/20
CPC分类号： C07D207/12
摘要： A compound having the formula ##STR1## which is an anti-fungal agent is described. The producing organism Colletotricum accutatum is also described, along with a method of production.

24. 发明授权

US5510371A Inhibitors of farnesyl-protein transferase 失效
公开(公告)号：US5510371A
公开(公告)日：1996-04-23
申请号：US254228
申请日：1994-06-06
申请人： Sheo B. Singh , George M. Garrity , Olga Genillourd , Russell B. Lingham , Isabel Martin , Mary N. Omstead , Keith C. Silverman , Deborah L. Zink
发明人： Sheo B. Singh , George M. Garrity , Olga Genillourd , Russell B. Lingham , Isabel Martin , Mary N. Omstead , Keith C. Silverman , Deborah L. Zink
IPC分类号： A61K31/225 , A61K31/231 , A61K31/232 , A61K31/365 , C07C69/738 , C07D321/00 , C12P17/08 , A61K31/335
CPC分类号： C12R1/045 , A61K31/225 , A61K31/231 , A61K31/232 , A61K31/365 , C07C69/738 , C07D321/00 , C12P17/08 , Y10S435/822
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

25. 发明授权

US5310949A Cholesterol lowering compounds 失效
标题翻译：胆固醇降低化合物
公开(公告)号：US5310949A
公开(公告)日：1994-05-10
申请号：US939258
申请日：1992-09-02
申请人： Claude Dufresne , Prakash S. Masurekar , Leslie A. Ferrell , Deborah L. Zink , Margaret S. Sosa
发明人： Claude Dufresne , Prakash S. Masurekar , Leslie A. Ferrell , Deborah L. Zink , Margaret S. Sosa
IPC分类号： C07D493/08 , C07D319/04
CPC分类号： C07D493/08
摘要： New Zaragozic acids have been isolated from a culture of MF5465. These compounds and their derivatives are active as squalene synthetase inhibitors and are useful in the treatment of hypercholesterolemia.
摘要翻译：已经从MF5465的培养物中分离出新的萨拉哥酸。这些化合物及其衍生物作为角鲨烯合成酶抑制剂是有活性的，可用于治疗高胆固醇血症。

26. 发明授权

US5260465A Inhibitors of farnesyl protein transferase 失效
标题翻译：法呢基蛋白转移酶抑制剂
公开(公告)号：US5260465A
公开(公告)日：1993-11-09
申请号：US807695
申请日：1991-12-16
申请人： Sheo B. Singh , Deborah L. Zink
发明人： Sheo B. Singh , Deborah L. Zink
IPC分类号： A61K31/19 , A61K31/23 , A61P35/00 , A61P43/00 , C07C55/02 , C07C57/13 , C07C57/34 , C07C69/593 , C07C69/602 , C12N1/14 , C12N9/99 , C12P7/44 , C12P7/64 , C12P17/04 , C12R1/645 , C11C1/04 , A61K31/20
CPC分类号： C12P7/6427 , C07C57/13 , C07C69/602 , C12P17/04 , C12P7/6436
摘要： This invention relates to pharmaceutical compounds of structural formula (I): ##STR1## and compositions and methods of treatment utilizing these compounds to inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras.

27. 发明授权

US09126983B2 Extracts from kibdelos porangium as antibacterial agents 有权
标题翻译： Kibdelos porangium作为抗菌剂提取物
公开(公告)号：US09126983B2
公开(公告)日：2015-09-08
申请号：US13518613
申请日：2010-12-17
申请人： Sheo Singh , Jon D. Polishook , Deborah L. Zink , Olga Genilloud , Michael Goetz , Francisca Vicente , David Brian Olsen , Scott Knoble Smith
发明人： Sheo Singh , Jon D. Polishook , Deborah L. Zink , Olga Genilloud , Michael Goetz , Francisca Vicente , David Brian Olsen , Scott Knoble Smith
IPC分类号： C07H15/26 , A61P31/04 , A61K31/706 , A61K31/7056 , A01N43/86 , A01N43/36 , C07D407/14 , A61K31/535 , A61K31/4025 , C07D413/14 , C12P17/16 , C12R1/01
CPC分类号： C07D407/14 , A01N43/36 , A01N43/86 , A61K31/4025 , A61K31/535 , C07D413/14 , C12P17/16 , C12R1/01 , Y02A50/473
摘要： The present invention relates to novel compounds of formulae (I) and (II) and pharmaceutically acceptable salts thereof that are useful in the treatment and/or prevention of human and animal bacterial infections and associated diseases and conditions; compositions containing such compounds; derivation of such compounds by fermentation and isolation, partial synthesis and total synthesis; methods of inhibiting bacterial growth; methods of treating, preventing or controlling bacterial infection; biologically pure cultures of bacterial strains from which such compounds may be produced; and processes for preparing compositions containing such compounds.
摘要翻译：本发明涉及可用于治疗和/或预防人和动物细菌感染和相关疾病和病症的式（I）和（II）的新化合物及其药学上可接受的盐; 含有这些化合物的组合物; 通过发酵和分离，部分合成和总合成衍生这些化合物; 抑制细菌生长的方法治疗，预防或控制细菌感染的方法; 细菌菌株的生物纯培养物可从其中产生这些化合物; 以及制备含有这些化合物的组合物的方法。

28. 发明申请

US20130005673A1 Extracts From Kibdelos Porangium As Antibacterial Agents 有权
标题翻译：从Kibdelos Porangium提取物作为抗菌剂
公开(公告)号：US20130005673A1
公开(公告)日：2013-01-03
申请号：US13518613
申请日：2010-12-17
申请人： Sheo Singh , Jon D. Polishook , Deborah L. Zink , Olga Genilloud , Michael Goetz , Francisca Vicente , David Brian Olsen , Scott Knoble Smith
发明人： Sheo Singh , Jon D. Polishook , Deborah L. Zink , Olga Genilloud , Michael Goetz , Francisca Vicente , David Brian Olsen , Scott Knoble Smith
IPC分类号： C07H15/26 , C12P19/46 , A61P31/04 , C12N1/20 , A61K31/706 , A61K31/7056
CPC分类号： C07D407/14 , A01N43/36 , A01N43/86 , A61K31/4025 , A61K31/535 , C07D413/14 , C12P17/16 , C12R1/01 , Y02A50/473
摘要： The present invention relates to novel compounds of formulae (I) and (II) and pharmaceutically acceptable salts thereof that are useful in the treatment and/or prevention of human and animal bacterial infections and associated diseases and conditions; compositions containing such compounds; derivation of such compounds by fermentation and isolation, partial synthesis and total synthesis; methods of inhibiting bacterial growth; methods of treating, preventing or controlling bacterial infection; biologically pure cultures of bacterial strains from which such compounds may be produced; and processes for preparing compositions containing such compounds.
摘要翻译：本发明涉及可用于治疗和/或预防人和动物细菌感染和相关疾病和病症的式（I）和（II）的新化合物及其药学上可接受的盐; 含有这些化合物的组合物; 通过发酵和分离，部分合成和总合成衍生这些化合物; 抑制细菌生长的方法治疗，预防或控制细菌感染的方法; 细菌菌株的生物纯培养物可从其中产生这些化合物; 以及制备含有这些化合物的组合物的方法。

29. 发明授权

US06403347B1 HIV integrase inhibitors 失效
标题翻译： HIV整合酶抑制剂
公开(公告)号：US06403347B1
公开(公告)日：2002-06-11
申请号：US09355692
申请日：1999-10-25
申请人： Gerald F. Bills , Russell B. Lingham , Ali Shafiee , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink , Fernando Pelaez , Ana M. Teran
发明人： Gerald F. Bills , Russell B. Lingham , Ali Shafiee , Keith C. Silverman , Sheo Bux Singh , Deborah L. Zink , Fernando Pelaez , Ana M. Teran
IPC分类号： A61K3135
CPC分类号： A61K31/35
摘要： Natural products such as certain chaetochromins are described. These compounds are useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：描述了天然产物，如某些chaetochromins。这些化合物可用作抑制HIV整合酶，预防或治疗HIV感染和治疗AIDS，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药，免疫调节剂，抗生素或其他抗生素组合使用疫苗。还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

30. 发明授权

US06245806B1 HIV integrase inhibitors 失效
标题翻译： HIV整合酶抑制剂
公开(公告)号：US06245806B1
公开(公告)日：2001-06-12
申请号：US09625246
申请日：2000-07-25
申请人： Anne Dombrowski , Sheo Singh , Deborah L. Zink , Ana Teran , Fernando Pelaez , Daria Hazuda
发明人： Anne Dombrowski , Sheo Singh , Deborah L. Zink , Ana Teran , Fernando Pelaez , Daria Hazuda
IPC分类号： A61K31335
CPC分类号： C07D493/08 , A61K31/352 , A61K45/06 , C12P17/181 , C12R1/645 , A61K2300/00
摘要： Novel tetracyclic aromatic ketones are natural product compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. Further, the novel fungal cultures MF6388 (ATCC 74478), Sterile Fungus, and MF6591 (ATCC 74477), Ascochyta sp. are also disclosed. Further, the cultures Sterile Fungus MF6388 (ATCC 74478) and Ascochyta sp. MF6591 (ATCC 74477) are also disclosed, as well as processes for making compounds of the present invention employing the cultures.
摘要翻译：新型四环芳族酮是用于抑制HIV整合酶，预防或治疗艾滋病毒感染和治疗艾滋病的天然产物化合物，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药物组合，免疫调节剂，抗生素或疫苗。还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。此外，新型真菌培养物MF6388（ATCC 74478），无菌真菌和MF6591（ATCC 74477），Ascochyta sp。也被披露。此外，培养无菌真菌MF6388（ATCC 74478）和Ascochyta sp。还公开了MF6591（ATCC 74477），以及使用培养物制备本发明化合物的方法。

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