公开(公告)号：US5149639A

公开(公告)日：1992-09-22

申请号：US356953

申请日：1989-05-25

申请人： Leonard Katz ,  James Tuan ,  James B. McAlpine

发明人： Leonard Katz ,  James Tuan ,  James B. McAlpine

IPC分类号： C07H17/08 ,  C12N1/21 ,  C12N15/52 ,  C12N15/64 ,  C12N15/76 ,  C12P19/62

CPC分类号： C07H17/08 ,  C12N15/52 ,  C12N15/64 ,  C12N15/76 ,  C12P19/62

摘要： DNA cloning shuttle vectors, including a cosmid shuttle vector, for E. coli and Streptomyces are disclosed. Specifically, disclosed shuttle vectors pAL7002 (NRRL B-18055) and pNJ1 (NRRL B-18054) contain an E. coli origin of replication, Streptomyces replication functions, and antibiotic resistance markers for both E. coli and Streptomyces. In addition, pNJ1 contains a cos sequence. Novel 2-norerythromycin antibiotics A, B, C, and D, which were produced in a strain Streptomyces erythreus 12693-240 (NRRL B-18053) transformed by pNJ1 bearing DNA from Streptomyces antibioticus, are also disclosed. The present invention also provides a method for producing novel antibiotics. This method for antibiotic production is applied to the transformation of a blocked mutant of S. erythreus with genomic DNA from S. antibioticus but may be more broadly applied to genes of antibiotic-producing strains transformed into cells which are blocked in the pathway for production of a different antibiotic.

摘要翻译： 公开了用于大肠杆菌和链霉菌的DNA克隆穿梭载体，包括粘粒穿梭载体。 具体地，披露的穿梭载体pAL7002（NRRL B-18055）和pNJ1（NRRL B-18054）含有大肠杆菌复制起点，链霉菌复制功能和用于大肠杆菌和链霉菌的抗生素抗性标记。 另外，pNJ1包含cos序列。 还公开了在由抗链霉菌（Streptomyces antibioticus）携带DNA的pNJ1转化的菌株Streptomyces erythreus 12693-240（NRRL B-18053）中产生的新型2-赖氨酸霉素A，B，C和D。 本发明还提供了生产新型抗生素的方法。 用于抗生素生产的这种方法被应用于使用来自抗生素抗生素的基因组DNA来阻断红霉素的突变体的转化，但是可以更广泛地应用于转化到生产途径中被阻断的细胞的抗生素产生菌株的基因 不同的抗生素。

公开(公告)号：US4874748A

公开(公告)日：1989-10-17

申请号：US843116

申请日：1986-03-24

申请人： Leonard Katz ,  James Tuan ,  James B. McAlpine

发明人： Leonard Katz ,  James Tuan ,  James B. McAlpine

IPC分类号： C12N15/09 ,  C07H17/08 ,  C07H21/00 ,  C07H21/04 ,  C12N1/20 ,  C12N1/21 ,  C12N15/00 ,  C12N15/52 ,  C12N15/64 ,  C12N15/76 ,  C12P19/62 ,  C12R1/19 ,  C12R1/465

CPC分类号： C07H17/08 ,  C12N15/52 ,  C12N15/64 ,  C12N15/76 ,  C12P19/62 ,  Y10S435/886

摘要： DNA cloning shuttle vectors, including a cosmid shuttle vector, for E. coli and Streptomyces are disclosed. Specifically, disclosed shuttle vectors pAL7002 (NRRL B-18055) and pNJl (NRRL B-18054) contain an E. coli origin of replication, Streptomyces replication functions, and antibiotic resistance markers for both E. coli and Streptomyces. In addition, pNJl contains a cos sequence. Novel 2-norerythromycin antibiotics A, B, C, and D, which were produced in a strain Streptomyces erythreus 12693-240 (NRRL B-18053) transformed by pNJl bearing DNA from Streptomyces antibioticus, are also disclosed. The present invention also provides a method for producing novel antibiotics. This method for antibiotic production is applied to the transformation of a blocked mutant of S. erythreus with genomic DNA from S. antibioticus but may be more broadly applied to genes to antibiotic-producing strains transformed into cells which are blocked in the pathway for production of a different antibiotic.

摘要翻译： 公开了用于大肠杆菌和链霉菌的DNA克隆穿梭载体，包括粘粒穿梭载体。 具体地，披露的穿梭载体pAL7002（NRRL B-18055）和pNJ1（NRRL B-18054）含有大肠杆菌复制起点，链霉菌复制功能和用于大肠杆菌和链霉菌的抗生素抗性标记。 此外，pNJ1包含cos序列。 还公开了在由携带抗链霉菌的DNA携带DNA的pNJ1转化的菌株Streptomyces erythreus 12693-240（NRRL B-18053）中产生的新型2-耐雷霉素抗生素A，B，C和D。 本发明还提供了生产新型抗生素的方法。 抗生素生产的这种方法被应用于使用来自抗生素抗生素的基因组DNA来阻断红霉素的突变体的转化，但是可以更广泛地应用于转化到生产途径中被阻断的细胞的抗生素产生菌株的基因 不同的抗生素。

公开(公告)号：US4272626A

公开(公告)日：1981-06-09

申请号：US79018

申请日：1979-09-26

申请人： Ronald E. Carney ,  James B. McAlpine

发明人： Ronald E. Carney ,  James B. McAlpine

IPC分类号： C07H15/224 ,  C07H15/22

CPC分类号： C07H15/224

摘要： A method of producing 1-epi-2-deoxyfortimicin A, key intermediates therefor and an improved process for synthesizing the key intermediate 1,2-di-epi-fortimicin A.

摘要翻译： 1-epi-2-deoxyfortimicin A的制备方法及其关键中间体，以及合成关键中间体1,2-二表 - 维生素A的改进方法。

公开(公告)号：US4226979A

公开(公告)日：1980-10-07

申请号：US25241

申请日：1979-03-29

申请人： James B. McAlpine

发明人： James B. McAlpine

IPC分类号： C07H15/22 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/224 ,  C12P19/48 ,  A61K31/71

CPC分类号： C07H15/224 ,  C12P19/48 ,  C12R1/29

摘要： A new fortimicin, fortimicin AK. The compound is coproduced in the fermentation of Micromonospora olivoasterospora ATCC No. 21819, 31009 or 31010 along with fortimicin A, fortimicin B isofortimicin, fortimicin E and a number of other minor factors. The compound is useful as an intermediate in synthesizing fortimicin AK derivatives which are useful as antibiotics.

摘要翻译： 一个新的fortimicin，fortimicin AK。 该化合物与Micomonospora olivoasterospora ATCC No.21819,31009或31010以及fortimicin A，fortimicin B异威霉素，fortimicin E和许多其他次要因素一起共同生产。 该化合物可用作合成有用的抗生素的顽固素AK衍生物的中间体。

公开(公告)号：US4213971A

公开(公告)日：1980-07-22

申请号：US25242

申请日：1979-03-29

申请人： James B. McAlpine

发明人： James B. McAlpine

IPC分类号： C07H15/224 ,  A61K31/71 ,  C07H15/22

CPC分类号： C07H15/224

摘要： Derivatives of fortimicin AK are provided by this invention. The derivatives are 4-N, 2'-N- and 4,2'-di-N-derivatives of fortimicin AK which are useful as anti-bacterial agents.

摘要翻译： fortimicin AK的衍生物由本发明提供。 衍生物是可用作抗菌剂的fortimicin AK的4-N，2-N和4,2'-二-N-衍生物。

公开(公告)号：US4208407A

公开(公告)日：1980-06-17

申请号：US9638

申请日：1979-02-05

申请人： Ronald E. Carney ,  Jerry R. Martin ,  James B. McAlpine ,  John S. Tadanier

发明人： Ronald E. Carney ,  Jerry R. Martin ,  James B. McAlpine ,  John S. Tadanier

IPC分类号： C07H15/224 ,  A61K31/71 ,  C07H15/22

CPC分类号： C07H15/224

摘要： 5-Deoxyfortimicin A, 2,5-dideoxyfortimicin A and the corresponding 4-N-acyl and alkyl fortimicin B derivatives thereof, pharmaceutically acceptable salts thereof, intermediates therefor, and pharmaceutical compositions containing the compounds of this invention. The fortimicin derivatives are represented by the formula: ##STR1## wherein R is selected from the group consisting of acyl, hydroxyacyl, aminoacyl, N-monoloweralkylaminoacyl, N,N-diloweralkylaminoacyl, hydroxyacyl, hydroxy-substituted aminoacyl or an amino acid residue other than glycyl, loweralkyl, aminoloweralkyl, hydroxyloweralkyl, N-monoloweralkylaminoloweralkyl, N-N-diloweralkylaminoloweralkyl or hydroxy-substituted aminoloweralkyl; R.sub.1 is hydrogen or hydroxy; and R.sub.2 is hydrogen or hydroxy with the limitation that either R.sub.1 and R.sub.2 each are hydrogen or when only one of R.sub.1 or R.sub.2 are hydrogen, R.sub.2 is hydrogen and R.sub.1 is hydroxy and R.sub.1 and R.sub.2 both cannot be hydroxy.

摘要翻译： 5-脱氧有益霉素A，2,5-双脱氧有益霉素A及其相应的4-N-酰基和烷基苦味素B衍生物，其药学上可接受的盐，其中间体和含有本发明化合物的药物组合物。 所述有害基因衍生物由下式表示：其中R选自酰基，羟基酰基，氨基酰基，N-单低级烷基氨基酰基，N，N-二低级烷基氨基酰基，羟基酰基，羟基取代的氨基酰基或除 甘氨酰，低级烷基，氨基低级烷基，羟基低级烷基，N-单低级烷基氨基低级烷基，N，N'-二烯烷基氨基低级烷基或羟基取代的氨基低级烷基; R1是氢或羟基; 并且R 2是氢或羟基，限制在于R 1和R 2各自为氢或当R 1或R 2中只有一个为氢时，R 2为氢且R 1为羟基，且R 1和R 2均不能为羟基。

公开(公告)号：US08076287B2

公开(公告)日：2011-12-13

申请号：US12294213

申请日：2007-03-28

申请人： Emmanuel Zazopoulos ,  James B. McAlpine ,  Arjun H. Banskota ,  Mahmood Piraee

发明人： Emmanuel Zazopoulos ,  James B. McAlpine ,  Arjun H. Banskota ,  Mahmood Piraee

IPC分类号： A61K38/12

CPC分类号： C07K7/06 ,  A61K38/00 ,  C12P17/188 ,  C12P21/02 ,  C12R1/465

摘要： The present invention provides cyclic hexadepsipeptides and their pharmaceutically acceptable salts, solvates and prodrugs, and methods for obtaining the compounds, by fermentation, optionally followed by post-biosynthesis chemical modification. The present invention further provides uses of cyclic hexadepsipeptides, and their pharmaceutically acceptable salts, solvates and prodrugs as pharmaceuticals, in particular to their use as antibacterial, antifungal or antineoplastic agents, and to pharmaceutical compositions comprising a cyclic hexadepsipeptide, or a pharmaceutically acceptable salt, solvate or prodrug thereof, together with a carrier.

摘要翻译： 本发明提供环状十六肽及其药学上可接受的盐，溶剂合物和前药，以及通过发酵，任选地随后进行生物合成化学修饰来获得化合物的方法。 本发明进一步提供了环状十六肽及其药学上可接受的盐，溶剂合物和前药作为药物，特别是其作为抗细菌剂，抗真菌剂或抗肿瘤剂的用途的用途，以及包含环十六肽或其药学上可接受的盐， 溶剂化物或前药，以及载体。

公开(公告)号：US20090215789A1

公开(公告)日：2009-08-27

申请号：US12294213

申请日：2007-03-28

申请人： Emmanuel Zazopoulos ,  James B. McAlpine ,  Arjun H. Banskota ,  Mahmood Piraee

发明人： Emmanuel Zazopoulos ,  James B. McAlpine ,  Arjun H. Banskota ,  Mahmood Piraee

IPC分类号： A61K31/501 ,  C07D401/14 ,  C12N1/20 ,  C12P17/16 ,  A61P31/04 ,  A61P35/00

CPC分类号： C07K7/06 ,  A61K38/00 ,  C12P17/188 ,  C12P21/02 ,  C12R1/465

摘要： The present invention provides cyclic hexadepsipeptides and their pharmaceutically acceptable salts, solvates and prodrugs, and methods for obtaining the compounds, by fermentation, optionally followed by post-biosynthesis chemical modification. The present invention further provides uses of cyclic hexadepsipeptides, and their pharmaceutically acceptable salts, solvates and prodrugs as pharmaceuticals, in particular to their use as antibacterial, antifungal or antineoplastic agents, and to pharmaceutical compositions comprising a cyclic hexadepsipeptide, or a pharmaceutically acceptable salt, solvate or prodrug thereof, together with a carrier.

摘要翻译： 本发明提供环状十六肽及其药学上可接受的盐，溶剂合物和前药，以及通过发酵，任选地随后进行生物合成化学修饰来获得化合物的方法。 本发明进一步提供了环状十六肽及其药学上可接受的盐，溶剂合物和前药作为药物，特别是其作为抗细菌剂，抗真菌剂或抗肿瘤剂的用途的用途，以及包含环十六肽或其药学上可接受的盐， 溶剂化物或前药，以及载体。

公开(公告)号：US20090029972A1

公开(公告)日：2009-01-29

申请号：US11663890

申请日：2005-09-26

申请人： James B. McAlpine ,  Arjun H. Banskota

发明人： James B. McAlpine ,  Arjun H. Banskota

IPC分类号： A61K31/551 ,  C07D243/38 ,  C12N5/06 ,  A61P35/00

CPC分类号： C07D243/38

摘要： The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, and their use in the preparation of medicaments for the treatment of neoplastic conditions

摘要翻译： 本发明涉及由式I表示的生物活性二苯并二氮杂酮类似物，其生产方法及其在制备用于治疗肿瘤病症的药物中的用途

公开(公告)号：US07312339B2

公开(公告)日：2007-12-25

申请号：US10865767

申请日：2004-06-14

申请人： James B. McAlpine ,  Chris M. Farnet ,  Emmanuel Zazopoulos ,  Nargis Ismail ,  Brian O. Bachmann

发明人： James B. McAlpine ,  Chris M. Farnet ,  Emmanuel Zazopoulos ,  Nargis Ismail ,  Brian O. Bachmann

IPC分类号： C07D207/444 ,  C07D209/48

CPC分类号： C12R1/60 ,  C07D263/32 ,  C07D413/12 ,  C12P17/14

摘要： Polyene oxazoles of the following formula wherein R3 is selected from H and methyl, are disclosed. Such compounds, and pharmaceutically acceptable salts thereof, may be used in the inhibition of tumor cell growth. The polyene oxazoles and their pharmaceutically acceptable salts may be formulated as pharmaceutical compositions with pharmaceutically acceptable carriers for use in the inhibition of tumor cells. The polyene oxazoles may be obtained from strains of Streptomyces sparsogenes, such as strain 022 having deposit number IDAC 270504-04.

摘要翻译： 公开了下式的多烯恶唑，其中R 3选自H和甲基。 这些化合物及其药学上可接受的盐可用于抑制肿瘤细胞生长。 多烯恶唑及其药学上可接受的盐可以配制成具有用于抑制肿瘤细胞的药学上可接受的载体的药物组合物。 多烯恶唑可以从天竺葵链霉菌菌株获得，例如具有保藏号IDAC 270504-04的菌株022。