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11. 发明授权

US5527687A Enzyme induction screen for ergosterol biosynthesis inhibitors 失效
标题翻译：麦角甾醇生物合成抑制剂的酶诱导筛选
公开(公告)号：US5527687A
公开(公告)日：1996-06-18
申请号：US68986
申请日：1993-05-25
申请人： Donald R. Kirsch , Margaret H. K. Lai
发明人： Donald R. Kirsch , Margaret H. K. Lai
IPC分类号： C12Q1/18 , C12Q1/26 , C12Q1/34 , C12Q1/54 , C12Q1/48
CPC分类号： C12Q1/34 , C12Q1/18 , C12Q1/26 , C12Q2334/52 , G01N2333/395 , G01N2333/924 , Y10S435/942
摘要： A method for screening for sterol biosynthesis inhibitors of potential use as fungicides or antihypercholesterolemic agents identifies agents by the induction of lanosterol 14-.alpha.-demethylase, an enzyme in the biosynthetic pathway of ergosterol and cholesterol, in cultures containing the agents. In one screening test, test samples are incubated in a culture of a Saccharomyces cerevisiae strain sensitive to ergosterol biosynthesis and containing a gene fusion of a lanosterol 14-.alpha.-demethylase clone with a gene for bacterial .beta.-galactosidase. After incubation of the culture, an increase in lancsterol 14-.alpha.-demethylase activity is determined indirectly by measuring .beta.-galactosidase activity. The culture media contains a chromogenic substrate of .beta.-galactosidase such as orthonitrophenyl-.beta.-D-galactoside or 5-bromo-4-chloro-3-indoyl-.beta.-D-galactoside, so that active samples are identified by the production of colored product. For comparison purposes, screening tests may employ a lanosterol 14-.alpha.-demethylase inhibitor such as dinaconazole as a positive control.
摘要翻译：用于筛选潜在用作杀真菌剂或抗高胆固醇血症药的甾醇生物合成抑制剂的方法通过诱导羊毛甾醇14-α-甲基化酶（在麦角甾醇和胆固醇的生物合成途径中的酶）在含有该试剂的培养物中鉴定药剂。在一次筛选试验中，将测试样品在对麦角甾醇生物合成敏感的酿酒酵母菌株的培养物中培养，并含有羊毛甾醇14-α-甲基化酶克隆与细菌β-半乳糖苷酶基因的基因融合物。培养物培养后，通过测量β-半乳糖苷酶活性间接测定兰曲星14-α-甲基化酶活性的增加。培养基含有β-半乳糖苷酶如邻硝基苯基-β-D-半乳糖苷或5-溴-4-氯-3-吲哚基-β-D-半乳糖苷的显色底物，使活性样品通过生产有色产品。为了比较目的，筛选试验可以使用羊毛甾醇14-α-甲基化酶抑制剂如依替康唑作为阳性对照。

12. 发明授权

US5512472A DNA sequence encoding sterol .DELTA.14 reductase 失效
标题翻译：编码固醇DELTA14还原酶的DNA序列
公开(公告)号：US5512472A
公开(公告)日：1996-04-30
申请号：US439131
申请日：1995-05-11
申请人： Margaret H. K. Lai , Donald R. Kirsch , Martin Bard
发明人： Margaret H. K. Lai , Donald R. Kirsch , Martin Bard
IPC分类号： C12N9/02 , C12N15/53 , C12N15/09 , C12N15/81
CPC分类号： C12N9/001
摘要： A gene encoding Saccharomyces cerevisiae sterol .DELTA.14 reductase of the ergosterol biosynthetic pathway is isolated and cloned by selecting strains carrying sequences on a 2.mu. based vector for resistance to a morpholine fungicide such as fenpropimorph. Four distinct plasmid inserts which produce morpholine resistance are obtained, and one of these is characterized and sequenced. The purified and isolated DNA sequence encoding sterol .DELTA.14 reductase encodes a polypeptide exhibiting homology to the S. cerevisiae sterol C-24(28) reductase enzyme in the ergosterol biosynthetic pathway.
摘要翻译：通过选择在2基于载体上携带序列的菌株来分离和克隆麦角甾醇生物合成途径的酿酒酵母甾醇DELTA 14还原酶的基因，以抵抗吗啉杀真菌剂例如茴香霉素。获得产生吗啉抗性的四种不同的质粒插入片段，其中之一被表征和测序。编码固醇DELTA14还原酶的纯化和分离的DNA序列编码与麦角甾醇生物合成途径中的酿酒酵母甾醇C-24（28）还原酶具有同源性的多肽。

13. 发明授权

US5024839A Dactylocycline A and dactylocycline B 失效
标题翻译： Dactylocycline A和Dactylocycline B
公开(公告)号：US5024839A
公开(公告)日：1991-06-18
申请号：US137635
申请日：1987-12-24
申请人： Carol A. Aklonis , Helen A. Ax , Donald R. Kirsch , Joseph O'Sullivan , Adrienne Tymiak , J. Scott Wells
发明人： Carol A. Aklonis , Helen A. Ax , Donald R. Kirsch , Joseph O'Sullivan , Adrienne Tymiak , J. Scott Wells
IPC分类号： A61K35/74 , C12P1/06 , C12P29/00 , C12R1/01
CPC分类号： C12P29/00 , C12P1/06
摘要： Cultivation of a strain of the microorganism Dactylosporangium sp. A.T.C.C. No. 53693, yields the antibiotic substance EM5586 which contains the novel useful components dactylocycline A and dactylocycline B.

14. 发明授权

US4754018A Antibiotic prepared from lysobacter sp. SC 14,067 and analogs thereof 失效
标题翻译：溶解细菌制备的抗生素 SC 14,067及其类似物
公开(公告)号：US4754018A
公开(公告)日：1988-06-28
申请号：US23425
申请日：1987-03-09
申请人： Adrienne A. Tymiak , Donald R. Kirsch , Joseph O'Sullivan , John E. McCullough
发明人： Adrienne A. Tymiak , Donald R. Kirsch , Joseph O'Sullivan , John E. McCullough
IPC分类号： C07G11/00 , A61K35/74 , A61P31/04 , C12P1/04 , C12R1/01 , C07K5/12
CPC分类号： C12P1/04 , Y10S930/19
摘要： A novel antibiotic substance EM5587 is prepared by cultivation of a strain of the microorganism Lysobacter sp. SC 14,067, A.T.C.C. No. 53042. Chemical analogs of EM5587 are prepared by chemical synthesis.
摘要翻译：通过培养微生物溶菌杆菌属菌株制备新型抗生素物质EM5587。 SC 14,067，A.T.C.C. 号53042.通过化学合成制备EM5587的化学类似物。

15. 发明授权

US4735901A Transformation of Candida albicans 失效
标题翻译：白念珠菌的转化
公开(公告)号：US4735901A
公开(公告)日：1988-04-05
申请号：US691303
申请日：1985-01-14
申请人： Myra B. Kurtz , Donald R. Kirsch
发明人： Myra B. Kurtz , Donald R. Kirsch
IPC分类号： C12N15/52 , C12N15/81 , C12N15/00 , C12N5/00 , C12N7/00
CPC分类号： C12N15/52 , C12N15/815 , Y10S435/922
摘要： Candida albicans has been transformed by the insertion of a plasmid comprising a fragment of DNA from Candida albicans containing the intact ADE 2 gene.
摘要翻译：通过插入包含含有完整ADE 2基因的白色假丝酵母的DNA片段的质粒已将白色念珠菌转化。

16. 发明授权

US5591576A Sterol .DELTA.14 reductase screen 失效
标题翻译： Sterol DELTA 14还原酶屏
公开(公告)号：US5591576A
公开(公告)日：1997-01-07
申请号：US107348
申请日：1993-08-16
申请人： Margaret H. K. Lai , Donald R. Kirsch , Martin Bard
发明人： Margaret H. K. Lai , Donald R. Kirsch , Martin Bard
IPC分类号： C12N9/02 , C12N15/53 , C12Q1/18 , C12Q1/26 , C12N15/63 , C12Q1/02 , C12Q1/68
CPC分类号： C12N9/001 , C12Q1/18 , C12Q1/26 , C12Y103/0107
摘要： A binary assay identifies agents that inhibit sterol .DELTA.14 reductase involved in ergosterol biosynthesis. In the primary screen, sterol .DELTA.14 reductase inhibition by a test sample is assayed by adding the test sample to a culture of Neurospora crassa having an erg-3 mutation and also to a culture of a strain having an erg-1 mutation, comparing the extent of growth inhibition after incubation in the two cultures, and identifying as positives those samples that show growth inhibition in the erg-3 culture exceeding that in the erg-1 culture. In the secondary screen, samples that test positive in the primary screen are reassayed by adding the test sample to a culture of a Saccharomyces cerevisiae strain into which has been introduced multiple copies of a gene encoding sterol .DELTA.14 reductase and also to a strain of S. cerevisiae that does not have the introduced gene; positive samples are identified after incubation by observation that growth inhibition in the culture having no introduced reductase gene exceeds growth inhibition in the culture having the introduced reductase gene. In preferred embodiments, a known inhibitor of sterol .DELTA.14 reductase is employed in solidified media in both the primary and the secondary screens, resulting in an assay that is highly sensitive and specific for the detection of sterol .DELTA.14 reductase inhibitors.
摘要翻译：二元测定法鉴定了抑制参与麦角固醇生物合成的甾醇DELTA14还原酶的药剂。在主筛网中，通过将测试样品加入到具有erg-3突变的粗糙脉孢菌培养物中，并将其与具有erg-1突变的菌株的培养物进行比较，来测定测试样品的固醇DELTA 14还原酶抑制在两种培养物中孵育后的生长抑制程度，并且鉴定出在erg-3培养物中显示生长抑制的样品超过erg-1培养物中的那些样品的阳性。在次级屏幕中，通过将测试样品加入到已经引入了多拷贝的编码固醇DELTA14还原酶的基因的Saccharomyces cerevisiae菌株的培养物中，并且还添加到S的菌株没有引入基因的酿酒酵母; 通过观察，通过观察到没有引入的还原酶基因的培养物中的生长抑制超过在具有引入的还原酶基因的培养物中的生长抑制的情况下，鉴定阳性样品。在优选的实施方案中，在初级和次级筛中的固化培养基中使用已知的甾醇DELTA 14还原酶抑制剂，导致对检测固醇DELTA14还原酶抑制剂具有高度敏感性和特异性的测定。

17. 发明授权

US5294725A Scopularin 失效
公开(公告)号：US5294725A
公开(公告)日：1994-03-15
申请号：US305338
申请日：1989-01-31
申请人： Donald R. Kirsch , Joseph O'Sullivan , Douglas W. Phillipson
发明人： Donald R. Kirsch , Joseph O'Sullivan , Douglas W. Phillipson
IPC分类号： C07D309/10 , C07D405/04 , C07H15/12 , C07H15/26
CPC分类号： C07D405/04 , C07D309/10 , C07H15/12 , C07H15/26
摘要： A novel antibiotic substance, Scopularin, is prepared by cultivation of a strain of the microorganism, Scopulariopsis, A.T.C.C. No. 20,914. This compound and its alcohol derivative have also been found to have cytochrome P450 inhibition activity.
摘要翻译：通过培养微生物菌株Scopulariopsis，A.T.C.C.制备新型抗生素物质Scopularin。第20,914号。该化合物及其醇衍生物也被发现具有细胞色素P450抑制活性。

18. 发明授权

US4719109A EM5596--an antibiotic 失效
标题翻译： EM5596-一种抗生素
公开(公告)号：US4719109A
公开(公告)日：1988-01-12
申请号：US30536
申请日：1987-03-27
申请人： Donald R. Kirsch , Edward Meyers , Joseph E. Biskupiak
发明人： Donald R. Kirsch , Edward Meyers , Joseph E. Biskupiak
IPC分类号： C12P1/04 , C12P1/06
CPC分类号： C12P1/04
摘要： A novel antibiotic substance EM5596 is prepared by cultivation of a strain of the microorganism Micrococcus luteus A.T.C.C. No. 53598.
摘要翻译：通过培养微生物微球菌A.T.C.C.的菌株制备新的抗生素物质EM5596。第53598号。

19. 发明授权

US07329663B2 Substituted-triazolopyrimidines as anticancer agents 失效
标题翻译：取代三唑并嘧啶作为抗癌剂
公开(公告)号：US07329663B2
公开(公告)日：2008-02-12
申请号：US09895975
申请日：2001-06-29
申请人： Mark R. Schmitt , Donald R. Kirsch , Jane E. Harris , Carl F. Beyer , Klaus-Jüergen Pees , Paul A. Carter , Waldemar Pfrengle , Guido Albert
发明人： Mark R. Schmitt , Donald R. Kirsch , Jane E. Harris , Carl F. Beyer , Klaus-Jüergen Pees , Paul A. Carter , Waldemar Pfrengle , Guido Albert
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention provides a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof and further provides a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by interacting with tubulin and microtubules and promoting microtubule polymerization which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了在有需要的哺乳动物中治疗或抑制癌性肿瘤细胞和相关疾病的生长的方法，该方法包括向所述哺乳动物施用有效量的取代三唑并嘧啶衍生物或其药学上可接受的盐，并且还提供了通过与微管蛋白和微管相互作用并促进微管聚合来治疗或抑制有需要的哺乳动物中癌性肿瘤细胞和相关疾病的生长，其包括向所述哺乳动物施用有效量的取代的三唑并嘧啶衍生物或其药学上可接受的盐。

20. 发明授权

US5846819A Recombinant expression vectors for expression of heterologous proteins 失效
标题翻译：用于表达异源蛋白质的重组表达载体
公开(公告)号：US5846819A
公开(公告)日：1998-12-08
申请号：US472045
申请日：1995-06-06
申请人： Mark H. Pausch , Bradley A. Ozenberger , John R. Hadcock , Laura A. Price , Eileen M. Kajkowski , Donald R. Kirsch , Deborah T. Chaleff
发明人： Mark H. Pausch , Bradley A. Ozenberger , John R. Hadcock , Laura A. Price , Eileen M. Kajkowski , Donald R. Kirsch , Deborah T. Chaleff
IPC分类号： C12N15/09 , C07K14/72 , C12N1/15 , C12N1/19 , C12N15/12 , C12P21/02 , C12Q1/02 , C12R1/865 , C12N15/63 , C07K14/705
CPC分类号： C07K14/723 , C07K2319/00
摘要： The present invention is directed to a expression vectors and yeast cells transformed therewith containing a first heterologous nucleotide sequence which codes for a G protein-coupled receptor, for example, the somatostatin receptor, and a second nucleotide sequence which codes for all or a portion of a G protein .alpha..beta..gamma. complex. Said heterologous protein is physically expressed in a host cell membrane in proper orientation for both stereoselective binding of ligands, as well as functional interaction with G proteins on the cytoplasmic side of the cell membrane. In some embodiments, a nucleotide sequence encoding a heterologous or chimeric G.alpha. protein is expressed in conjunction with nucleotide sequences from the yeast G protein .beta..gamma. subunits. A second aspect of the present invention provides expression vectors and transformed yeast cells encoding chimeric yeast/heterologous G protein coupled receptors. A third aspect of the present invention is directed to methods of assaying compounds using these expression constructs and yeast cell expression systems to determine the effects of ligand binding to the heterologous receptors expressed in the systems.
摘要翻译：本发明涉及转化的表达载体和酵母细胞，其含有编码G蛋白偶联受体（例如生长抑素受体）的第一异源核苷酸序列，以及编码全部或一部分的第二核苷酸序列一个G蛋白αβγ复合物。所述异源蛋白质在适当取向的宿主细胞膜中物理表达，用于配体的立体选择性结合，以及与细胞膜细胞质侧上的G蛋白的功能相互作用。在一些实施方案中，编码异源或嵌合Gα蛋白的核苷酸序列与来自酵母G蛋白βγ亚基的核苷酸序列一起表达。本发明的第二方面提供了编码嵌合酵母/异源G蛋白偶联受体的表达载体和转化的酵母细胞。本发明的第三方面涉及使用这些表达构建体和酵母细胞表达系统测定化合物以确定配体与系统中表达的异源受体结合的作用的方法。

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