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1. 发明申请

US20090069401A1 MARINE ACTINOMYCETE TAXON FOR DRUG AND FERMENTATION PRODUCT DISCOVERY 有权
公开(公告)号：US20090069401A1
公开(公告)日：2009-03-12
申请号：US11966787
申请日：2007-12-28
申请人： William Fenical , Paul R. Jensen , Tracy J. Mincer
发明人： William Fenical , Paul R. Jensen , Tracy J. Mincer
IPC分类号： C07D491/044 , A61K31/407
CPC分类号： C12Q1/18 , C12N1/10 , C12P17/188 , C12R1/01 , G01N2333/36
摘要： The invention is the discovery of an actinomycete genus, given the name Salinospora gen. nov., that displays an obligate requirement of seawater (Na+) for growth and unique 16S rRNA signature nucleotides. The invention is also the use of the genus for the production and discovery of active biomolecules such as pharmaceutical agents, agrichemicals, immunomodifiers, enzymes and enzyme inhibitors.

2. 发明申请

US20050153389A1 Method for the production of bioactive substances from the novel actinomycete taxon MAR2 ("Marinophilus") 审中-公开
标题翻译：从新型放线菌MAR2（“Marinophilus”）生产生物活性物质的方法
公开(公告)号：US20050153389A1
公开(公告)日：2005-07-14
申请号：US10972530
申请日：2004-10-25
申请人： William Fenical , Paul Jensen , Tracy Mincer
发明人： William Fenical , Paul Jensen , Tracy Mincer
IPC分类号： A61K31/7048 , A61K35/74 , C07D321/00 , C07H17/08 , C12N1/20 , C12P1/00 , C12P1/06 , C12P19/62
CPC分类号： C07D321/00 , A61K31/7048 , C07H17/08 , C12P1/06 , C12R1/01
摘要： The present invention provides methods for the isolation of a new group of actinomycetes and for the identification of members of this group based on characteristic nucleotide sequences and phylogenetic analyses. This group is phylogenetically distinct from all other known actinomycetes and represents a novel genus that includes multiple new species. Members of this group can be recognized by signature MAR2 nucleotides present in their 16S rRNA gene sequences and by standard phylogenetic treeing methods.
摘要翻译：本发明提供了基于特征性核苷酸序列和系统发育分析来分离新组放线菌和鉴定该组成员的方法。该组与所有其他已知的放线菌在系统发育上是不同的，并且代表一种包括多种新物种的新颖属。该组的成员可以通过其16S rRNA基因序列中存在的签名MAR2核苷酸和标准系统发育树方法来识别。

3. 发明授权

US6069146A Halimide, a cytotoxic marine natural product, and derivatives thereof 失效
标题翻译： Halimide，细胞毒性海洋天然产物及其衍生物
公开(公告)号：US6069146A
公开(公告)日：2000-05-30
申请号：US191475
申请日：1998-11-12
申请人： William Fenical , Paul R. Jensen , Xing C. Cheng
发明人： William Fenical , Paul R. Jensen , Xing C. Cheng
IPC分类号： A61K31/497 , A61P35/00 , C07D403/06 , A61K31/496
CPC分类号： C07D403/06 , A61K31/497
摘要： The present invention provides a substantially purified compound having the structure: ##STR1## wherein R.sub.1 to R.sub.9 are defined; or a salt of the compound, and provides pharmaceutical compositions comprising a compound of the invention and a pharmaceutically acceptable carrier. The invention also provides methods of reducing or inhibiting mitosis of a cell by contacting the cell with a compound of the invention, which blocks the cell at the G2/M phase of the cell cycle. The invention also provides a method of reducing the severity of a pathology characterized, at least in part, by undesirable proliferation of a population of cells in a subject by administering to the subject a compound of the invention in an amount sufficient to reduce or inhibit proliferation of the population of cells.
摘要翻译：本发明提供了具有以下结构的基本上纯化的化合物：其中R1至R9被定义; 或化合物的盐，并提供包含本发明化合物和药学上可接受的载体的药物组合物。本发明还提供了通过使细胞与本发明的化合物接触来减少或抑制细胞有丝分裂的方法，该化合物在细胞周期的G2 / M期阻断细胞。本发明还提供了一种降低病症严重性的方法，所述方法至少部分地由受试者中细胞群的不期望的增殖表达，所述方法通过向受试者施用足以减少或抑制增殖的量的本发明化合物的细胞群体。

4. 发明授权

US6066635A Avrainvillamide, a cytotoxic marine natural product, and derivatives thereof 失效
标题翻译：阿维林酰胺，细胞毒性海洋天然产物及其衍生物
公开(公告)号：US6066635A
公开(公告)日：2000-05-23
申请号：US274899
申请日：1999-03-23
申请人： William Fenical , Paul R. Jensen , Xing C. Cheng
发明人： William Fenical , Paul R. Jensen , Xing C. Cheng
IPC分类号： C07D491/22 , A61K31/4985 , A61K31/4995 , C07D241/00
CPC分类号： C07D491/22
摘要： The present invention provides a compound having the structure ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently selected from H, alkyl, aminoalkyl, perfluoroalkyl, orpharmaceutically acceptable salts thereof, useful for treating cancer.
摘要翻译：本发明提供具有以下结构的化合物，其中R1，R2，R3，R4和R5独立地选自H，烷基，氨基烷基，全氟烷基或其药学上可接受的盐，其可用于治疗癌症。

5. 发明申请

US20120230972A1 Salinosporamides and Methods for Use Thereof 有权
标题翻译： Salinosporamides及其使用方法
公开(公告)号：US20120230972A1
公开(公告)日：2012-09-13
申请号：US13477364
申请日：2012-05-22
申请人： William Fenical , Paul Jensen , Tracy Mincer , Robert H.R. Feling
发明人： William Fenical , Paul Jensen , Tracy Mincer , Robert H.R. Feling
IPC分类号： A61K31/407 , A61K31/519 , A61K31/513 , A61K31/52 , A61K31/7068 , A61K31/7076 , A61K31/664 , A61K31/437 , A61K31/704 , A61K38/14 , A61K31/56 , A61K38/46 , A61K31/473 , A61P35/00 , A61P35/02 , A61K38/43
CPC分类号： A61K31/407 , A61K31/397 , A61K31/424 , A61K31/43 , A61K45/06 , C07D491/04 , C07D491/044 , C12P17/18 , C12P17/188
摘要： The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
摘要翻译：本发明基于以下发现：海洋放线菌株CNB392和CNB476的某些发酵产物是过度增殖哺乳动物细胞的有效抑制剂。 CNB392和CNB476菌株位于Micromonosporaceae中，并且为该专业海洋群体提出了通用表型Salinospora。由该菌株产生的反应产物分类为salinosporamide，并且由于其低分子量，低IC 50值，高药物效力和对真菌的癌细胞的选择性而特别有利于治疗肿瘤性疾病。

6. 发明申请

US20100144826A1 Salinosporamides and Methods for Use Thereof 有权
标题翻译： Salinosporamides及其使用方法
公开(公告)号：US20100144826A1
公开(公告)日：2010-06-10
申请号：US12638860
申请日：2009-12-15
申请人： William Fenical , Paul Jensen , Tracy Mincer , Robert H. R. Feling
发明人： William Fenical , Paul Jensen , Tracy Mincer , Robert H. R. Feling
IPC分类号： A61K31/407 , C07D491/044 , A61P35/00
CPC分类号： A61K31/407 , A61K31/397 , A61K31/424 , A61K31/43 , A61K45/06 , C07D491/04 , C07D491/044 , C12P17/18 , C12P17/188
摘要： The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
摘要翻译：本发明基于以下发现：海洋放线菌株CNB392和CNB476的某些发酵产物是过度增殖哺乳动物细胞的有效抑制剂。 CNB392和CNB476菌株位于Micromonosporaceae中，并且为该专业海洋群体提出了通用表型Salinospora。由该菌株产生的反应产物分类为salinosporamide，并且由于其低分子量，低IC 50值，高药物效力和对真菌的癌细胞的选择性而特别有利于治疗肿瘤性疾病。

7. 发明申请

US20070155815A1 Salinosporamides and methods for use thereof 有权
公开(公告)号：US20070155815A1
公开(公告)日：2007-07-05
申请号：US11705694
申请日：2007-02-12
申请人： William Fenical , Paul Jensen , Tracy Mincer , Robert Feling
发明人： William Fenical , Paul Jensen , Tracy Mincer , Robert Feling
IPC分类号： A61K31/407
CPC分类号： A61K31/407 , A61K31/397 , A61K31/424 , A61K31/43 , A61K45/06 , C07D491/04 , C07D491/044 , C12P17/18 , C12P17/188
摘要： The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

8. 发明申请

US20050239866A1 Salinosporamides and methods for use thereof 有权
标题翻译： Salinosporamide及其使用方法
公开(公告)号：US20050239866A1
公开(公告)日：2005-10-27
申请号：US11147622
申请日：2005-06-07
申请人： William Fenical , Paul Jensen , Tracy Mincer , Robert Feling
发明人： William Fenical , Paul Jensen , Tracy Mincer , Robert Feling
IPC分类号： A61K31/397 , A61K31/407 , A61K31/424 , A61K31/43 , C07D491/02 , C07D491/04 , C07D491/044 , C12P17/18
CPC分类号： A61K31/407 , A61K31/397 , A61K31/424 , A61K31/43 , A61K45/06 , C07D491/04 , C07D491/044 , C12P17/18 , C12P17/188
摘要： The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
摘要翻译：本发明基于以下发现：海洋放线菌株CNB392和CNB476的某些发酵产物是过度增殖哺乳动物细胞的有效抑制剂。 CNB392和CNB476菌株位于Micromonosporaceae中，并且为该专业海洋群体提出了通用表型Salinospora。由该菌株产生的反应产物被归类为salinosporamide，并且由于其低分子量，低IC 50值，高药物效力和对真菌的癌细胞的选择性而特别有利于治疗肿瘤性疾病。

9. 发明申请

US20110092534A1 Ammosamides as Anticancer Agents 有权
标题翻译：氨甲酰胺作为抗癌剂
公开(公告)号：US20110092534A1
公开(公告)日：2011-04-21
申请号：US12666269
申请日：2008-06-27
申请人： William Fenical , Paul Jensen , John Macmillan , Chambers C. Hughes , James J. Laclair
发明人： William Fenical , Paul Jensen , John Macmillan , Chambers C. Hughes , James J. Laclair
IPC分类号： A61K31/437 , C07D471/06 , C12P17/18 , A61P35/00 , B65D85/00
CPC分类号： C07D471/06
摘要： A compound having the general the general structure I is provided: (Formula I), wherein Z is a substituent selected from a group consisting of S and O; X is a substituent selected from a group consisting of Cl, Br, I, OH and NH2; each of R1 and R2 is a substituent independently selected from a group consisting of H, a linear, cyclic or branched, substituted or unsubstituted C1-C6 alkyl, a substituted or unsubstituted aryl, and a substituted or unsubstituted heteroaryl; and each of Y and Y1 is a substituent independently selected from a group consisting of H and C(O)—C6H4—Br.
摘要翻译：提供通式为通式I的化合物：式（I）其中Z为选自S和O的取代基; X是选自Cl，Br，I，OH和NH 2的取代基; R 1和R 2中的每一个是独立地选自H，直链，环状或支链的，取代或未取代的C 1 -C 6烷基，取代或未取代的芳基和取代或未取代的杂芳基的取代基; 并且Y和Y1各自为独立地选自H和C（O）-C 6 H 4 -Br的取代基。

10. 发明授权

US07179834B2 Salinosporamides and methods for use thereof 有权
公开(公告)号：US07179834B2
公开(公告)日：2007-02-20
申请号：US10600854
申请日：2003-06-20
申请人： William Fenical , Paul Jensen , Tracy Mincer , Robert H. R. Feling
发明人： William Fenical , Paul Jensen , Tracy Mincer , Robert H. R. Feling
IPC分类号： A61K31/407 , C07D491/044
CPC分类号： A61K31/397 , A61K31/407 , A61K31/424 , A61K31/43 , C07D491/04 , C12P17/18
摘要： The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

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