公开(公告)号：US20060079508A1

公开(公告)日：2006-04-13

申请号：US11130295

申请日：2005-05-16

Applicant: Pierre Falardeau ,  Francois Berger ,  Henriette Gourdeau ,  James McAlpine ,  Chris Farnet ,  Violetta Dimitriadou

Inventor： Pierre Falardeau ,  Francois Berger ,  Henriette Gourdeau ,  James McAlpine ,  Chris Farnet ,  Violetta Dimitriadou

IPC: A61K31/551 ,  C07D243/10

CPC classification number: C07D243/38 ,  A61K31/551

Abstract: This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms using the farnesylated dibenzodiazepinone compound of Formula I. The invention includes pharmaceutical compositions comprising the compound of Formula I:

Abstract translation: 本发明涉及抑制肿瘤细胞生长和/或增殖的方法，以及使用式I的法呢基化二苯并二氮杂酮化合物治疗肿瘤的方法。本发明包括药物组合物，其包含式I化合物：

公开(公告)号：US20050004185A1

公开(公告)日：2005-01-06

申请号：US10844701

申请日：2004-05-13

Applicant: Brian Bachmann ,  James McAlpine ,  Emmanuel Zazopoulos ,  Chris Farnet

Inventor： Brian Bachmann ,  James McAlpine ,  Emmanuel Zazopoulos ,  Chris Farnet

IPC: A61P31/00 ,  C07C215/24 ,  C07C279/14 ,  C07C279/22 ,  C07C305/14 ,  C12P7/42 ,  C12P11/00 ,  C12P13/00 ,  C12P19/44 ,  C07D213/42 ,  C07D207/10

CPC classification number: C07C59/42 ,  C07C59/90 ,  C07C215/24 ,  C07C279/14 ,  C07C279/22 ,  C07C305/14 ,  C07C2601/14 ,  C07D207/16 ,  C07D213/53 ,  C07D213/82 ,  C07D303/36 ,  C07D317/30 ,  C12P7/42 ,  C12P11/00 ,  C12P13/001 ,  C12P13/02 ,  C12P19/44 ,  C12R1/465

Abstract: This invention relates to a novel class of linear polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for their production. The compounds may be obtained by cultivation of Streptomyces melanosporafaciens species and isolation of the polyene polyketide, followed by optional chemical production of the isolated polyene polyketide. The compounds may also be produced by other known bacteria. The invention further includes the use of these compounds as inhibitors of fungal cell growth and inhibitors of cancer cell growth. Finally, the invention encompasses pharmaceutical compositions comprising these novel polyketide compounds, or their pharmaceutically acceptable salts or derivatives thereof.

Abstract translation: 本发明涉及新型线型多烯聚酮化合物，其药学上可接受的盐和衍生物及其生产方法。 可以通过培养黑色链霉菌属物种并分离多烯聚酮来获得化合物，然后任选化学制备分离的多烯聚酮化合物。 化合物也可以由其他已知细菌产生。 本发明还包括这些化合物作为真菌细胞生长抑制剂和癌细胞生长抑制剂的用途。 最后，本发明包括包含这些新型聚酮化合物或其药学上可接受的盐或衍生物的药物组合物。

公开(公告)号：US09090667B2

公开(公告)日：2015-07-28

申请号：US14112720

申请日：2012-04-18

Applicant: Jong Woo Kim ,  Sang Wook Lee ,  Sang Jin Park ,  Joo Won Suh ,  In Ae Lee ,  Tae Mi Yoon ,  Jong Keun Choi ,  Ji Ean Lee ,  Jin Yong Kim ,  Ying Yu Jin ,  Scott Franzblau ,  Sanghyun Cho ,  Wei Gao ,  Guido Pauli ,  James McAlpine ,  Jose Napolitano ,  Birgit Jaki ,  Brent Friesen ,  Maria Florencia Rodriguez Brasco ,  David Lankin

Inventor： Jong Woo Kim ,  Sang Wook Lee ,  Sang Jin Park ,  Joo Won Suh ,  In Ae Lee ,  Tae Mi Yoon ,  Jong Keun Choi ,  Ji Ean Lee ,  Jin Yong Kim ,  Ying Yu Jin ,  Scott Franzblau ,  Sanghyun Cho ,  Wei Gao ,  Guido Pauli ,  James McAlpine ,  Jose Napolitano ,  Birgit Jaki ,  Brent Friesen ,  Maria Florencia Rodriguez Brasco ,  David Lankin

IPC: C07K7/54 ,  C07K7/08 ,  A61K38/00

CPC classification number: C07K7/54 ,  A61K38/00 ,  C07K7/08

Abstract: The present invention relates to novel anti-TB cyclic peptides from Nonomuraea sp. MJM5123, a process for the production of the anti-Tuberculosis peptide and a pharmaceutical composition for the prevention and treatment of mycobacterial infection comprising the same. The composition of the present invention is highly active against replicating/non-replicating M. tuberculosis, including MDR and XDR strains, so that it can be effectively used as a therapeutic agent for tuberculosis.

Abstract translation: 本发明涉及来自Nonomuraea sp。的新型抗TB环肽。 MJM5123是生产抗结核肽的方法和用于预防和治疗包含其的分枝杆菌感染的药物组合物。 本发明的组合物对复制/非复制性结核分枝杆菌（包括MDR和XDR菌株）具有高度活性，因此可有效地用作结核病的治疗剂。

公开(公告)号：US20140142031A1

公开(公告)日：2014-05-22

申请号：US14112720

申请日：2012-04-18

Applicant: Jong Woo Kim ,  Sang Wook Lee ,  Sang jin Park ,  Joo Won Suh ,  In Ae Lee ,  Tae Mi Yoon ,  Jong Keun Choi ,  Ji Ean Lee ,  Jin Yong Kim ,  Ying Yu Jin ,  Scott Franzblau ,  Sanghyum Cho ,  Wei Gao ,  Guido Pauli ,  James McAlpine ,  Jose Napolitano ,  Birgit Jaki ,  Brent Friesen ,  Maria Florencia Rodriguez Brasco ,  David Lankin

Inventor： Jong Woo Kim ,  Sang Wook Lee ,  Sang jin Park ,  Joo Won Suh ,  In Ae Lee ,  Tae Mi Yoon ,  Jong Keun Choi ,  Ji Ean Lee ,  Jin Yong Kim ,  Ying Yu Jin ,  Scott Franzblau ,  Sanghyum Cho ,  Wei Gao ,  Guido Pauli ,  James McAlpine ,  Jose Napolitano ,  Birgit Jaki ,  Brent Friesen ,  Maria Florencia Rodriguez Brasco ,  David Lankin

IPC: C07K7/54

CPC classification number: C07K7/54 ,  A61K38/00 ,  C07K7/08

Abstract: The present invention relates to novel anti-TB cyclic peptides from Nonomuraea sp. MJM5123, a process for the production of the anti-Tuberculosis peptide and a pharmaceutical composition for the prevention and treatment of mycobacterial infection comprising the same. The composition of the present invention is highly active against replicating/non-replicating M. tuberculosis, including MDR and XDR strains, so that it can be effectively used as a therapeutic agent for tuberculosis.

Abstract translation: 本发明涉及来自Nonomuraea sp。的新型抗TB环肽。 MJM5123是生产抗结核肽的方法和用于预防和治疗包含其的分枝杆菌感染的药物组合物。 本发明的组合物对复制/非复制性结核分枝杆菌（包括MDR和XDR菌株）具有高度活性，因此可有效地用作结核病的治疗剂。

公开(公告)号：US20060080763A1

公开(公告)日：2006-04-20

申请号：US11245484

申请日：2005-10-06

Applicant: James McAlpine

Inventor： James McAlpine

IPC: E03D13/00

CPC classification number: F16L27/12 ,  E03D11/14

Abstract: A urinal outlet assembly comprises a urinal outlet pipe and a connector for coupling the outlet pipe to a waste pipe inlet. The connector is adapted to receive the outlet pipe in a sliding sealing fit.

Abstract translation: 小便器出口组件包括小便器出口管和用于将出口管连接到废料管入口的连接器。 连接器适于以滑动密封配合接收出口管。

公开(公告)号：US20060079512A1

公开(公告)日：2006-04-13

申请号：US11253658

申请日：2005-10-20

Applicant: James McAlpine ,  Arjun Banskota ,  Mustapha Aouidate

Inventor： James McAlpine ,  Arjun Banskota ,  Mustapha Aouidate

IPC: A61K31/551 ,  C07D243/10

CPC classification number: C12N9/93 ,  A61K38/00 ,  C07D243/38 ,  C07D405/06 ,  C07D405/14 ,  C12N9/0004 ,  C12N9/10 ,  C12N9/12 ,  C12N9/14 ,  C12N9/88 ,  C12N9/90 ,  C12N15/52 ,  C12P17/10 ,  C12R1/29 ,  Y02A50/473

Abstract: The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.

Abstract translation: 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，其制备方法，包含它们的药物组合物和治疗肿瘤病症的方法。

公开(公告)号：US20050187167A1

公开(公告)日：2005-08-25

申请号：US10760493

申请日：2004-01-21

Applicant: Brian Bachmann ,  James McAlpine ,  Emmanuel Zazopoulos ,  Chris Farnet

Inventor： Brian Bachmann ,  James McAlpine ,  Emmanuel Zazopoulos ,  Chris Farnet

IPC: A61K31/70 ,  A61P31/00 ,  C07C215/24 ,  C07C225/14 ,  C07C235/28 ,  C07C237/16 ,  C07C279/22 ,  C07C305/14 ,  C07H5/06 ,  C07H15/10 ,  C07H15/18 ,  C07H15/203 ,  C07H15/26 ,  C12P7/42 ,  C12P11/00 ,  C12P13/00 ,  C12P13/02 ,  C12P19/44 ,  C12R1/465

CPC classification number: C07H15/203 ,  C07C215/24 ,  C07C225/14 ,  C07C235/28 ,  C07C237/16 ,  C07C279/22 ,  C07C305/14 ,  C07C2601/10 ,  C07C2601/14 ,  C07H15/10 ,  C07H15/18 ,  C07H15/26 ,  C12P7/42 ,  C12P11/00 ,  C12P13/001 ,  C12P13/02 ,  C12P19/44 ,  C12R1/465 ,  Y10S435/886

Abstract: This invention relates to a new class of polyene polyketides, their pharmaceutically acceptable salts and derivatives, and to methods for obtaining the compounds. One method of obtaining these compounds is by cultivation of novel strains of Streptomyces aizunensis; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to the novel strains of Streptomyces aizunensis used to produce these compounds, to the use of these compounds and their pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of fungal cell growth and cancer cell growth. The invention also relates to pharmaceutical compositions comprising these novel polyketides or a pharmaceutically acceptable salts or derivatives thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of these novel polyketides.

Abstract translation: 本发明涉及新类型的多烯聚酮化合物，其药学上可接受的盐和衍生物，以及获得化合物的方法。 获得这些化合物的一种方法是通过培养新的链霉菌链霉菌菌株; 另一种方法涉及在转化的宿主细胞中表达生物合成途径基因。 本发明还涉及用于制备这些化合物的新型链霉菌Streptomyces aizunensis菌株，使用这些化合物及其药学上可接受的盐和衍生物作为药物，特别是其作为真菌细胞生长抑制剂和癌细胞生长的用途。 本发明还涉及包含这些新型聚酮化合物或其药学上可接受的盐或衍生物的药物组合物。 最后，本发明涉及参与这些新型聚酮化合物的生物合成的新型多核苷酸序列及其编码的蛋白质。

公开(公告)号：US20050043297A1

公开(公告)日：2005-02-24

申请号：US10762107

申请日：2004-01-21

Applicant: Brian Bachmann ,  James McAlpine ,  Emmanuel Zazopoulos ,  Chris Farnet ,  Mahmood Piraee

Inventor： Brian Bachmann ,  James McAlpine ,  Emmanuel Zazopoulos ,  Chris Farnet ,  Mahmood Piraee

IPC: A61K38/00 ,  C07D243/38 ,  C12N9/00 ,  C12N9/02 ,  C12N9/10 ,  C12N9/12 ,  C12N9/14 ,  C12N9/88 ,  C12N9/90 ,  C12N15/52 ,  C12P17/10 ,  A61K31/551 ,  C07D243/10

CPC classification number: C12N9/93 ,  A61K38/00 ,  C07D243/38 ,  C07D405/06 ,  C07D405/14 ,  C12N9/0004 ,  C12N9/10 ,  C12N9/12 ,  C12N9/14 ,  C12N9/88 ,  C12N9/90 ,  C12N15/52 ,  C12P17/10 ,  C12R1/29 ,  Y02A50/473

Abstract: This invention relates to a novel farnesylated dibenzodiazepinone, named ECO-04601, its pharmaceutically acceptable salts and derivatives, and to methods for obtaining such compounds. One method of obtaining the ECO-04601 compound is by cultivation of a novel strain of Micromonospora sp., 046-ECO11; another method involves expression of biosynthetic pathway genes in transformed host cells. The present invention further relates to Micromonospora sp. strain 046-ECO11, to the use of ECO-04601 and its pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use as inhibitors of cancer cell growth, bacterial cell growth, mammalian lipoxygenase, and to pharmaceutical compositions comprising ECO-04601 or a pharmaceutically acceptable salt or derivative thereof. Finally, the invention relates to novel polynucleotide sequences and their encoded proteins, which are involved in the biosynthesis of ECO-04601.

Abstract translation: 本发明涉及名为ECO-04601的新型法呢基化二苯并二氮杂酮，其药学上可接受的盐和衍生物，以及获得这些化合物的方法。 获得ECO-04601化合物的一种方法是通过培养一种新型的小单孢菌属菌株046-ECO11; 另一种方法涉及在转化的宿主细胞中表达生物合成途径基因。 本发明还涉及小单孢菌属 应用046-ECO11，使用ECO-04601及其药学上可接受的盐和衍生物作为药物，特别是其作为癌细胞生长抑制剂，细菌细胞生长，哺乳动物脂氧合酶的用途，以及包含ECO-04601或 其药学上可接受的盐或衍生物。 最后，本发明涉及参与ECO-04601的生物合成的新型多核苷酸序列及其编码的蛋白质。