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1. 发明授权

US5444043A Cyclic heptapeptide anti-inflammatory agent 失效
标题翻译：环七肽抗炎剂
公开(公告)号：US5444043A
公开(公告)日：1995-08-22
申请号：US198859
申请日：1994-02-18
申请人： William H. Fenical , Robert S. Jacobs , Paul R. Jensen
发明人： William H. Fenical , Robert S. Jacobs , Paul R. Jensen
IPC分类号： C12P21/04 , A61K38/00 , A61P3/00 , A61P29/00 , A61P31/04 , C07K7/06 , C07K7/64 , C12R1/465 , A61K38/12
CPC分类号： C07K7/64 , A61K38/00
摘要： A cyclic heptapeptide anti-inflammatory agent named cyclomarin-A is disclosed.Cyclomarin-A is produced by a specific marine actinomycete. The cyclomarin-A producing bacterium is isolated from sediment located in marine estuaries in and around San Diego, Calif. Fermentation of the isolated bacterium in saltwater-based media produces cyclomarin-A as a secondary by-product. The cyclomarin-A is useful as an anti-inflammatory agent.
摘要翻译：公开了一种名为cyclomarin-A的环状七肽抗炎剂。 Cyclomarin-A由特定的海洋放线菌产生。来自加利福尼亚州圣地亚哥市及其周围的海洋河口的沉积物中分离出产生环蛋白A的细菌。在盐水介质中发酵分离的细菌产生作为次生副产物的环亚胺A。环亚胺A可用作抗炎剂。

2. 发明授权

US5688783A Salinamides 失效
标题翻译：盐酸胺
公开(公告)号：US5688783A
公开(公告)日：1997-11-18
申请号：US552841
申请日：1995-11-03
申请人： William H. Fenical , Robert S. Jacobs , Paul R. Jensen
发明人： William H. Fenical , Robert S. Jacobs , Paul R. Jensen
IPC分类号： A61K38/00 , C07K5/087 , C07K5/12 , C07D498/08 , A61K31/395
CPC分类号： C07K5/0812 , C07K5/12 , A61K38/00
摘要： Salinamides A and B are disclosed. These two bicyclic depsipeptides are produced by fermentation of a specific marine actinomycete, a Streptomyces sp, (CNB-091) in saltwater-based media. Salinamides A and B are useful as anti-biotic and anti-inflammatory agents.
摘要翻译：公开了盐酰胺A和B。通过在盐水介质中发酵特定的海洋放线菌（Streptomyces sp）（CNB-091）产生这两种双环脱肽。盐酸胺A和B可用作抗生素和抗炎剂。

3. 发明授权

US5919926A Salinamides 失效
标题翻译：盐酸胺
公开(公告)号：US5919926A
公开(公告)日：1999-07-06
申请号：US186789
申请日：1994-01-25
申请人： William H. Fenical , Robert S. Jacobs , Paul R. Jensen
发明人： William H. Fenical , Robert S. Jacobs , Paul R. Jensen
IPC分类号： A61K38/00 , C07K5/087 , C07K5/12 , C07D498/08 , A61K31/395
CPC分类号： C07K5/0812 , C07K5/12 , A61K38/00
摘要： Salinamides A and B are disclosed. These two bicyclic depsipeptides are produced by fermentation of a specific marine actinomycete, a Streptomyces sp, (CNB-091) in saltwater-based media. Salinamides A and B are useful as anti-biotic and anti-inflammatory agents.
摘要翻译：公开了盐酰胺A和B。通过在盐水介质中发酵特定的海洋放线菌（Streptomyces sp）（CNB-091）产生这两种双环脱肽。盐酸胺A和B可用作抗生素和抗炎剂。

4. 发明授权

US5593960A Cyclic heptapeptide anti-inflammatory agent 失效
标题翻译：环七肽抗炎剂
公开(公告)号：US5593960A
公开(公告)日：1997-01-14
申请号：US447627
申请日：1995-05-23
申请人： William H. Fenical , Robert S. Jacobs , Paul R. Jensen
发明人： William H. Fenical , Robert S. Jacobs , Paul R. Jensen
IPC分类号： C12P21/04 , A61K38/00 , A61P3/00 , A61P29/00 , A61P31/04 , C07K7/06 , C07K7/64 , C12R1/465 , A61K38/12
CPC分类号： C07K7/64 , A61K38/00
摘要： A cyclic heptapeptide anti-inflammatory agent named cyclomarin-A is disclosed. Cyclomarin-A is produced by a specific marine actinomycete. The cyclomarin-A producing bacterium is isolated from sediment located in marine estuaries in and around San Diego, Calif. Fermentation of the isolated bacterium in saltwater-based media produces cyclomarin-A as a secondary by-product. The cyclomarin-A is useful as an anti-inflammatory agent.
摘要翻译：公开了一种名为cyclomarin-A的环状七肽抗炎剂。 Cyclomarin-A由特定的海洋放线菌产生。来自加利福尼亚州圣地亚哥市及其周围的海洋河口的沉积物中分离出产生环蛋白A的细菌。在盐水介质中发酵分离的细菌产生作为次生副产物的环亚胺A。环亚胺A可用作抗炎剂。

5. 发明授权

US4849410A Pseudopterosin and synthetic derivatives thereof 失效
标题翻译：伪蝶呤及其合成衍生物
公开(公告)号：US4849410A
公开(公告)日：1989-07-18
申请号：US85628
申请日：1987-08-14
申请人： Robert S. Jacobs , William H. Fenical
发明人： Robert S. Jacobs , William H. Fenical
IPC分类号： C07H15/256
CPC分类号： C07H15/24
摘要： Methods for treating mammals to reduce pain, reduce cell proliferation and/or reduce inflammation are described based on administering to the mammals compounds having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are hydrogen or an acyl group having from 1 to 6 carbon atoms; R.sub.5 is hydrogen, CH.sub.3 or CH.sub.2 OH and R.sub.6 is a hydrocarbon having from 1 to 10 carbon atoms. Natural and synthetic 1,12-seco derivatives with similar utilities are disclosed. Natural and synthetic derivatives are also disclosed where the sugar moiety is attached at the C-10 carbon on the tricyclic diterpene moiety instead of the C-9 carbon.
摘要翻译：基于给予具有下式的哺乳动物化合物描述哺乳动物治疗哺乳动物减轻疼痛，降低细胞增殖和/或减少炎症的方法，其中R1，R2，R3和R4是氢或具有1至6个碳原子 R5是氢，CH3或CH2OH，R6是具有1-10个碳原子的烃。公开了具有类似实用性的天然和合成的1,212分子衍生物。还公开了天然和合成衍生物，其中糖部分连接在三环二萜部分上的C-10碳上，而不是C-9碳。

6. 发明授权

US08217072B2 Salinosporamides and methods for use thereof 有权
公开(公告)号：US08217072B2
公开(公告)日：2012-07-10
申请号：US10561711
申请日：2004-06-18
申请人： William H. Fenical , Paul R. Jensen , Tracy J. Mincer , Robert H. R. Feling
发明人： William H. Fenical , Paul R. Jensen , Tracy J. Mincer , Robert H. R. Feling
IPC分类号： A61K31/407 , C07D491/044
CPC分类号： C07D491/044 , A61K31/407 , C07D491/04 , 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.

7. 发明授权

US5473057A Eleutherobin and analogs thereof 失效
标题翻译：埃柳塞罗及其类似物
公开(公告)号：US5473057A
公开(公告)日：1995-12-05
申请号：US336518
申请日：1994-11-09
申请人： William H. Fenical , Paul R. Jensen , Thomas Lindel
发明人： William H. Fenical , Paul R. Jensen , Thomas Lindel
IPC分类号： C07H17/04 , A01N43/50 , A61K31/7048 , A61K31/7056 , A61P35/00 , C07H15/00 , C07H15/26 , C07H17/00
CPC分类号： C07H15/26
摘要： Eleutherobin is a glycosylated diterpene which has the structural formula: ##STR1## Eleutherobin is a cytotoxic agent which is toxic to carcinoma cancer cells. Analogs of eleutherobin are also disclosed.
摘要翻译：埃柳替林是一种具有以下结构式的糖基化双萜：结构式：Ele GE bin bin bin bin bin bin。。。。。。。。。。。。。。。。。。。。。。还披露了eleutherobin的类似物。

8. 发明授权

US5624911A Ether derivatives of pseudopterosin 失效
标题翻译：假甲蝶呤的醚衍生物
公开(公告)号：US5624911A
公开(公告)日：1997-04-29
申请号：US487859
申请日：1995-06-07
申请人： William H. Fenical , Robert S. Jacobs
发明人： William H. Fenical , Robert S. Jacobs
IPC分类号： A61K31/70 , A61P29/00 , C07H15/24 , C07H15/256 , C07H15/00
CPC分类号： A61K31/704 , C07H15/256
摘要： Methods for treating mammals to reduce pain and/or reduce inflammation are described based on administering to the mammals synthetic ether derivatives of pseudopterosin having the formula: ##STR1## wherein A is an alkyl, aryl or amide group having from 2 to 20 carbon atoms, R.sub.1, R.sub.2 and R.sub.3 are hydrogen or an acyl residue (--COR) having from 1 to 6 carbon atoms, R.sub.4 is hydrogen or --CH.sub.2 OH and R.sub.5 is a hydrocarbon having from 1 to 10 carbon atoms. Also disclosed are synthetic compositions having the above general formula which are useful in the described method.
摘要翻译：基于向哺乳动物施用具有下式的假蝇甙的合成醚衍生物来描述治疗哺乳动物减轻疼痛和/或减少炎症的方法：其中A是具有2至20个碳原子的烷基，芳基或酰胺基， R 1，R 2和R 3是氢或具有1至6个碳原子的酰基（-COR），R 4是氢或-CH 2 OH，R 5是具有1至10个碳原子的烃。还公开了具有上述通式的合成组合物，其可用于所述方法。

9. 发明申请

US20090318529A1 SALINOSPORAMIDES AND METHODS FOR USE THEREOF 有权
标题翻译：沙胺和其使用方法
公开(公告)号：US20090318529A1
公开(公告)日：2009-12-24
申请号：US10561711
申请日：2004-06-18
申请人： William H. Fenical , Paul R. Jensen , Tracy J. Mincer , Robert H.R. Feling
发明人： William H. Fenical , Paul R. Jensen , Tracy J. Mincer , Robert H.R. Feling
IPC分类号： A61K31/407 , C07D491/044
CPC分类号： C07D491/044 , A61K31/407 , C07D491/04 , 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。

10. 发明申请

US20090142331A1 Method for the Production of Bio-Active Substances from the Novel Actinomycete TAXA MAR3A, MAR3B And MAR4 Belonging to the Family Treptomycetaceae 审中-公开
标题翻译：从新型放线菌生产生物活性物质的方法TAXA MAR3A，MAR3B和MAR4属于家庭链霉菌科
公开(公告)号：US20090142331A1
公开(公告)日：2009-06-04
申请号：US11597963
申请日：2004-06-21
申请人： William H. Fenical , Paul R. Jensen
发明人： William H. Fenical , Paul R. Jensen
IPC分类号： A61K35/00 , C12N1/20 , C07H21/04 , C12N15/63 , C12Q1/02 , G06F19/00 , G01N33/48 , C12Q1/68
CPC分类号： A61K36/06 , Y02A50/473
摘要： This invention provides a method for the isolation and identification of marine actinomycetes tentatively named MAR3A and MAR3B and the use of these groups as a source of new biologically active compositions including pharmaceuticals. The method includes specifics about where these microorganisms occur and their culture requirements. It also provides information describing characteristic DNA sequences that are used to identify members of this group and information demonstrating that members produce metabolites with significant activities in pharmaceutically relevant bioassays.
摘要翻译：本发明提供了一种分离鉴定海洋放线菌MAR3A和MAR3B的方法，以及这些组合作为包括药物在内的新的生物活性成分的来源。该方法包括关于这些微生物发生的位置及其培养要求的细节。它还提供描述用于鉴定该组成员的特征性DNA序列的信息，以及证明成员在药学相关生物测定中产生具有显着活性的代谢物的信息。

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