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公开(公告)号：US5861375A
公开(公告)日：1999-01-19
申请号：US789931
申请日：1997-01-28
申请人： Christine Lange Cannova , Anne W. Dombrowski , Michael A. Goetz , Sandra J. Rattray , Sheo Bux Singh , Jon Polishook , Gerald F. Bills , Joyce A. Greene , Gary K. Darland
发明人： Christine Lange Cannova , Anne W. Dombrowski , Michael A. Goetz , Sandra J. Rattray , Sheo Bux Singh , Jon Polishook , Gerald F. Bills , Joyce A. Greene , Gary K. Darland
IPC分类号： A61K38/00 , A61P29/00 , A61P33/02 , C07K5/12 , C12N1/14 , C12P21/04 , C12R1/77 , A61K38/12 , A61K31/445 , C07D471/04
摘要： The present invention provides novel cyclic tetrapeptides useful in the treatment or prevention of protozoal diseases; in particular, the novel compounds are active against the causative pathogens in malaria, toxoplasmosis, and coccidiosis.
摘要翻译： 本发明提供了可用于治疗或预防原生动物疾病的新型环状四肽; 特别是新型化合物对疟疾，弓形虫病和球虫病引起的病原体具有抗性。
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22.发明授权Gamma-pyrone-3-acetic acid as an inhibitor or interleukin-1 .beta. inventory enzyme 失效γ - 吡喃酮-3-乙酸作为抑制剂或白细胞介素-1β库存酶
公开(公告)号：US5411985A
公开(公告)日：1995-05-02
申请号：US62881
申请日：1993-05-17
申请人： Gerald F. Bills , Otto D. Hensens , Jerrold M. Liesch , Russel B. Lingham , Jon D. Polishook , Michael J. Salvatore , Susan L. Raghoobar
发明人： Gerald F. Bills , Otto D. Hensens , Jerrold M. Liesch , Russel B. Lingham , Jon D. Polishook , Michael J. Salvatore , Susan L. Raghoobar
IPC分类号： A61K31/35 , C07D309/38 , C12P17/06
CPC分类号： C12R1/645 , A61K31/35 , C07D309/38 , C12P17/06
摘要： Novel peptidyl derivatives of formula I are found to be potent inhibitors of interleukin-1.beta. converting enzyme (ICE). Compounds of formula I may be useful in the treatment of inflammatory or immune-based diseases of the lung and airways; central nervous system and surrounding membranes; the eyes and ears; joints, bones, and connective tissues; cardiovascular system including the pericardium; the gastrointestinal and urogenital systems; the skin and mucosal membranes. Compounds of formula I are also useful in treating the complications of infection (e.g., gram negative shock) and tumors in which IL 1 functions as an autocrine growth factor or as a mediator of cachexia. ##STR1##
摘要翻译： 发现式I的新型肽基衍生物是白细胞介素-1β转换酶（ICE）的有效抑制剂。 式I化合物可用于治疗肺和气道炎性或免疫性疾病; 中枢神经系统和周围膜; 眼睛和耳朵 关节，骨骼和结缔组织; 包括心包的心血管系统; 胃肠道和泌尿生殖系统; 皮肤和粘膜。 式I化合物也可用于治疗感染（例如，革兰氏阴性休克）的并发症和其中IL1作为自分泌生长因子或作为恶病质介质的肿瘤。
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23.发明授权Biologically pure culture of Cytospora useful as angiotensin II antagonist 失效作为血管紧张素II拮抗剂的细胞生物学纯培养物
公开(公告)号：US5278068A
公开(公告)日：1994-01-11
申请号：US961958
申请日：1992-10-16
申请人： Gerald F. Bills
发明人： Gerald F. Bills
IPC分类号： C07D311/74 , C07D491/10 , C12P17/02 , C12P17/06 , C12R1/645 , C12P17/08
CPC分类号： C07D491/10 , C07D311/74 , C12P17/02 , C12P17/06 , C12R1/645 , Y10S435/911
摘要： An organism of the Cytospora species produces substituted hexahydrobenzopyran compounds of the Formulas A, B, or C which are useful as angiotensin II antagonists: ##STR1##
摘要翻译： Cytospora物种的生物产生用作血管紧张素II拮抗剂的式A，B或C的取代的六氢苯并吡喃化合物：（*化学结构*）A（*化学结构*）B（*化学结构*）C
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公开(公告)号：US5183826A
公开(公告)日：1993-02-02
申请号：US587812
申请日：1990-09-25
申请人： Gerald F. Bills , Otto D. Hensens , Lawrence Koupal , Russell B. Lingham , John G. Ondeyka , Deborah L. Zink
发明人： Gerald F. Bills , Otto D. Hensens , Lawrence Koupal , Russell B. Lingham , John G. Ondeyka , Deborah L. Zink
IPC分类号： A61K31/40 , A61K31/403 , A61P31/12 , A61P31/18 , A61P37/04 , C07D209/58 , C07D209/76 , C12P17/10 , C12R1/645
CPC分类号： C07D209/76 , C12P17/10
摘要： An antiviral agent produced by Hypoxylon fragiforme and having the structure: ##STR1## is described. The product has high activity as an HIV protease enzyme inhibitor and is useful in the treatment of diseases in which control of HIV protease activity is desirable.
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公开(公告)号：US5620953A
公开(公告)日：1997-04-15
申请号：US447664
申请日：1995-05-23
申请人： Christine L. Cannova , Michael A. Goetz , Anne W. Dombrowski , Sandra J. Rattray , Sheo B. Singh , Gerald F. Bills , Jon Polishook , Joyce A. Greene , Gary K. Darland
发明人： Christine L. Cannova , Michael A. Goetz , Anne W. Dombrowski , Sandra J. Rattray , Sheo B. Singh , Gerald F. Bills , Jon Polishook , Joyce A. Greene , Gary K. Darland
IPC分类号： A61K38/00 , A61P29/00 , A61P33/02 , C07K5/12 , C12N1/14 , C12P21/04 , C12R1/77 , A61K38/12 , A61K31/445 , C07D471/04
摘要： The present invention provides novel cyclic tetrapeptides useful in the treatment or prevention of protozoal diseases; in particular, the novel compounds are active against the causative pathogens in malaria, toxoplasmosis, and coccidiosis.
摘要翻译： 本发明提供了可用于治疗或预防原生动物疾病的新型环状四肽; 特别是新型化合物对疟疾，弓形虫病和球虫病引起的病原体具有抗性。
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公开(公告)号：US5420334A
公开(公告)日：1995-05-30
申请号：US222773
申请日：1994-04-04
申请人： Sheo B. Singh , Gerald F. Bills , Russell B. Lingham , Isabel Martin , Keith C. Silverman , Jack L. Smith
发明人： Sheo B. Singh , Gerald F. Bills , Russell B. Lingham , Isabel Martin , Keith C. Silverman , Jack L. Smith
IPC分类号： A61K31/12 , A61K31/215 , A61K31/695 , C07C47/52 , C07C49/747 , C07C49/753 , C07C49/757 , C07C69/007 , C07C69/013 , C07F7/18 , A61K31/66 , A61K31/22 , A61K31/44
CPC分类号： C07C403/02 , A61K31/12 , A61K31/695 , C07C403/12 , C07C49/747 , C07C69/007 , C07C69/013 , C07F7/1852 , C07C2101/14 , C07C2101/16
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 famesyl-protein transferase and the famesylation of the oncogene protein Ras.
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学治疗组合物和抑制FAME基 - 蛋白转移酶的方法和癌基因蛋白Ras的甲酰化。
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公开(公告)号：US5420157A
公开(公告)日：1995-05-30
申请号：US808124
申请日：1991-12-16
IPC分类号： A61K31/19 , A61K31/23 , A61P35/00 , A61P43/00 , C07C57/13 , C07C57/155 , C07C69/347 , C07C69/602 , C12N9/99 , C12P7/26 , C12P7/44 , C12P17/04 , C12R1/01 , A01N43/32 , C07D307/02 , C07D307/34
CPC分类号： C12R1/645 , C07C57/13 , C07C69/602 , C12P17/04 , C12P7/44
摘要： This invention relates to pharmaceutical compounds of structural formulae (I) and (II): ##STR1## and compositions and methods of treatment utilizing these compounds to inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras.
摘要翻译： 本发明涉及结构式（I）和（II）的药物化合物：利用这些化合物抑制法呢基蛋白转移酶和癌基因蛋白法尼基化的组合物和方法Ras 。
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