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1. 发明授权

US06677370B2 Compositions and uses of dictyostatin compounds 有权
标题翻译：丝氨酸蛋白酶抑制剂化合物的组成和用途
公开(公告)号：US06677370B2
公开(公告)日：2004-01-13
申请号：US10360200
申请日：2003-02-06
申请人： Amy E. Wright , Jennifer L. Cummins , Shirley A. Pomponi , Ross E. Longley , Richard A. Isbrucker
发明人： Amy E. Wright , Jennifer L. Cummins , Shirley A. Pomponi , Ross E. Longley , Richard A. Isbrucker
IPC分类号： A61K31335
CPC分类号： A61K31/366 , A61K31/365 , C07K14/43595
摘要： Dictyostatin-1 has been found to stabilize microtubules and prohibit their depolymerization to free tubulin. Because of these activities, the dictyostatin compounds can be used in the treatment of a number of diseases in which aberrant cellular proliferation occurs such as drug-sensitive and drug-resistant cancers, autoimmune disorders, and inflammatory diseases.
摘要翻译：已经发现丝氨酸蛋白酶抑制素-1可以稳定微管，并禁止其解聚游离微管蛋白。由于这些活性，丝氨酸蛋白酶抑制素化合物可用于治疗许多发生异常细胞增殖的疾病，例如药物敏感和耐药性癌症，自身免疫性疾病和炎性疾病。

2. 发明授权

US06476065B2 Discalamide compounds and their use as anti-proliferative agents 失效
标题翻译：仙客来酰胺化合物及其作为抗增殖剂的用途
公开(公告)号：US06476065B2
公开(公告)日：2002-11-05
申请号：US09835692
申请日：2001-04-16
申请人： Sarath P. Gunasekera , Ross E. Longley , Gopal K. Paul , Richard A. Isbrucker , Shirley A. Pomponi
发明人： Sarath P. Gunasekera , Ross E. Longley , Gopal K. Paul , Richard A. Isbrucker , Shirley A. Pomponi
IPC分类号： A61K31335
CPC分类号： C07D493/04 , A61K31/70
摘要： The subject invention provides novel biologically active compounds which are useful for inhibiting cellular proliferation. Because of the biological activity of these compounds, they can be used for immunomodulation and/or treating cancer. In a preferred embodiment, the novel compounds, compositions and methods of use of the subject invention can advantageously be used to inhibit the growth of tumor cells in a mammalian host. More particularly, the subject compounds can be used for inhibiting in a human the growth of tumor cells, including cells of breast, colon, CNS, ovarian, renal, prostate, bone, gastrointestinal, stomach, testicular, or lung tumors, as well as human leukemia or melanoma cells. Specifically exemplified are discalamides A and B.
摘要翻译：本发明提供了可用于抑制细胞增殖的新型生物活性化合物。由于这些化合物的生物活性，它们可用于免疫调节和/或治疗癌症。在优选的实施方案中，本发明的新颖化合物，组合物和使用方法可有利地用于抑制哺乳动物宿主中肿瘤细胞的生长。更具体地，本发明化合物可用于在人体中抑制肿瘤细胞（包括乳腺，结肠，CNS，卵巢，肾，前列腺，骨，胃肠，胃，睾丸或肺肿瘤）的生长，以及人白血病或黑素瘤细胞。具体举例说明的是甲酰胺A和B.

3. 发明授权

US6087363A Use of imidazole and indole compounds as inhibitors of nitric oxide synthase 失效
标题翻译：使用咪唑和吲哚化合物作为一氧化氮合成酶的抑制剂
公开(公告)号：US6087363A
公开(公告)日：2000-07-11
申请号：US356171
申请日：1999-07-16
申请人： Ross E. Longley , Richard A. Isbrucker , Amy E. Wright
发明人： Ross E. Longley , Richard A. Isbrucker , Amy E. Wright
IPC分类号： A61K31/4178 , A61K31/497 , A61K31/495
CPC分类号： A61K31/4178 , A61K31/497
摘要： Imidazole and indole compounds were found to inhibit neural nitric oxide synthase (bNOS) activity. Nortopsentin-C inhibited bNOS as well as calcineurin activities suggesting that its actions are directed against calmodulin, a co-factor common to these two enzymes. Two indole compounds, as well as dragmacidin-D, inhibited bNOS, but not calcineurin, activity. Murine macrophage viability and induced NOS (iNOS) activity in cultured cells was also unaffected by these compounds.
摘要翻译：发现咪唑和吲哚化合物抑制神经一氧化氮合酶（bNOS）活性。诺芬汀C抑制bNOS以及钙调神经磷酸酶活性，表明其作用是针对钙调蛋白，这是这两种酶共同的辅因子。两种吲哚化合物以及dragmacidin-D抑制bNOS，但不抑制钙调神经磷酸酶的活性。培养细胞中的鼠巨噬细胞活力和诱导的NOS（iNOS）活性也不受这些化合物的影响。

4. 发明授权

US6057333A Discorhabdin compounds and methods of use 失效
标题翻译： Discorhabdin化合物和使用方法
公开(公告)号：US6057333A
公开(公告)日：2000-05-02
申请号：US122572
申请日：1998-07-24
申请人： Sarath P. Gunaskera , Peter J. McCarthy , Shirley A. Pomponi , Amy E. Wright , Ross E. Longley
发明人： Sarath P. Gunaskera , Peter J. McCarthy , Shirley A. Pomponi , Amy E. Wright , Ross E. Longley
IPC分类号： C07D471/20 , A61K31/44 , C07D401/14
CPC分类号： C07D471/20
摘要： Discorhabdin compounds are derived from marine sponges of the genus Batzella or prepared by synthetic methods. These compounds, and pharmaceutical compositions containing them as active ingredients, are useful as immunomodulatory, antitumor agents, and/or caspase inhibitors.
摘要翻译： Discorhabdin化合物衍生自Batzella属的海绵或通过合成方法制备。这些化合物和含有它们作为活性成分的药物组合物可用作免疫调节剂，抗肿瘤剂和/或胱天蛋白酶抑制剂。

5. 发明授权

US5478861A Cytotoxic macrolides and methods of use 失效
标题翻译：细胞毒性大环内酯类及其使用方法
公开(公告)号：US5478861A
公开(公告)日：1995-12-26
申请号：US198747
申请日：1994-02-18
申请人： Paul A. Horton , Frank Koehn , Ross E. Longley , Oliver J. McConnell , Shirley A. Pomponi
发明人： Paul A. Horton , Frank Koehn , Ross E. Longley , Oliver J. McConnell , Shirley A. Pomponi
IPC分类号： C07D407/06 , A61K31/35 , A61K31/365 , A61P35/00 , C07D309/10 , C07D309/30 , C07D493/16 , C07D493/18 , C12P17/18 , A61K31/335
CPC分类号： C07D309/30 , C07D309/10 , C12P17/181
摘要： A novel macrolide compound, lasonolide A, has been isolated from a marine sponge. This compound, derivatives of the compound, and compositions comprising the compound or its derivatives, are useful as antitumor agents and as biochemical tools.
摘要翻译：已经从海绵中分离出一种新型的大环内酯类化合物，它们是耐季铵盐A。该化合物，化合物的衍生物和包含该化合物或其衍生物的组合物可用作抗肿瘤剂和生化工具。

6. 发明授权

US5010099A Discodermolide compounds, compositions containing same and method of preparation and use 失效
标题翻译：曲妥珠单抗化合物，含有其的组合物及其制备方法
公开(公告)号：US5010099A
公开(公告)日：1991-04-23
申请号：US519605
申请日：1990-05-07
申请人： Malika Gunasekera , Sarath P. Gunasekera , Ross E. Longley , Neal S. Burres
发明人： Malika Gunasekera , Sarath P. Gunasekera , Ross E. Longley , Neal S. Burres
IPC分类号： C07D309/30
CPC分类号： C07D309/30 , Y10S514/908
摘要： Novel lactone compounds having remarkable immunomodulatory and antitumor activities, pharmaceutical compositions comprising such compounds, methods for the preparation of the novel compounds and compositions and methods of their use for therapeutic purposes are described. The new lactone compounds have the structure according to the formula: ##STR1## wherein: R=--H, --A, --CH.sub.2 --Q, --COA or --COZ,A=lower alkyl,Z=monocyclicaryl,Q=phenyl, tolyl or xylyl,X=--H, --A, --Z or --CH.sub.2 --Z, andY=--H, --A, --Z, --CH.sub.2 --Z, --COA, --COZ,the acid-addition salts, the octahydro and 23,24-dihydro derivatives thereof.
摘要翻译：描述了具有显着免疫调节和抗肿瘤活性的新型内酯化合物，包含这些化合物的药物组合物，制备新化合物的方法及其用于治疗目的的组合物和方法。新的内酯化合物具有下式的结构：其中：R = -H，-A，-CH 2 -Q，-COA或-COZ，A =低级烷基，Z =单环芳基，Q =苯基，甲苯基或二甲苯基，X = -H，-A，-Z或-CH 2 -Z，Y = -H，-A，-Z，-CH 2 -Z，-COA，-COZ，酸加成盐，八氢和23,24-二氢衍生物。

7. 发明授权

US07521474B2 Biologically active lasonolide compounds 失效
标题翻译：生物活性季铵化合物
公开(公告)号：US07521474B2
公开(公告)日：2009-04-21
申请号：US11494229
申请日：2006-07-27
申请人： Amy E. Wright , Shirley A. Pomponi , Peter J. McCarthy , Ying Chen , Ross E. Longley
发明人： Amy E. Wright , Shirley A. Pomponi , Peter J. McCarthy , Ying Chen , Ross E. Longley
IPC分类号： A61K31/335 , C07D325/04 , C07D493/12
CPC分类号： C07D493/18
摘要： The subject invention provides novel compositions of biologically active macrolide compounds which can advantageously be used in blocking cellular proliferation, treatment of cancer, treatment of fungal infections and control of spoilage of food, cosmetic and other consumer items.
摘要翻译：本发明提供生物活性大环内酯化合物的新组合物，其可有利地用于阻断细胞增殖，治疗癌症，治疗真菌感染和控制食品，化妆品和其它消费品的腐败。

8. 发明授权

US07115756B2 Biologically active lasonolide compounds 失效
公开(公告)号：US07115756B2
公开(公告)日：2006-10-03
申请号：US10875670
申请日：2004-06-23
申请人： Amy E. Wright , Shirley A. Pomponi , Peter J. McCarthy , Ying Chen , Ross E. Longley
发明人： Amy E. Wright , Shirley A. Pomponi , Peter J. McCarthy , Ying Chen , Ross E. Longley
IPC分类号： C07D325/04 , C07D493/12
CPC分类号： C07D493/18
摘要： The subject invention provides novel compositions of biologically active macrolide compounds which can advantageously be used in blocking cellular proliferation, treatment of cancer, treatment of fungal infections and control of spoilage of food, cosmetic and other consumer items.

9. 发明授权

US06384187B1 Antiproliferative activity of microsclerodermins 有权
标题翻译：微生物的抗增殖活性
公开(公告)号：US06384187B1
公开(公告)日：2002-05-07
申请号：US09568692
申请日：2000-05-11
申请人： Amy E. Wright , Shirley A. Pomponi , Ross E. Longley , Richard A. Isbrucker
发明人： Amy E. Wright , Shirley A. Pomponi , Ross E. Longley , Richard A. Isbrucker
IPC分类号： C07K750
CPC分类号： C07K7/56 , A61K38/00
摘要： The subject invention pertains to a series of cyclic peptides known as the microsclerodermins, which possess unusual amino acids, and which have been observed to inhibit the proliferation of tumor cell lines. The subject invention also pertains to methods useful in inhibiting pathological cellular proliferation in animals, including humans and other mammals. In accordance with the teachings of the subject invention, microsclerodermin compounds can be used to inhibit cellular proliferation including that which is responsible for tumors and other cancers. In a specific embodiment, the novel compositions and methods of use of the subject invention can advantageously be useful in the treatment of a patient hosting cancer cells, for example, inhibiting the growth of tumor cells in a mammalian host.
摘要翻译：本发明涉及一系列已知为具有不寻常氨基酸的微小霉菌的环状肽，其已被观察到抑制肿瘤细胞系的增殖。本发明还涉及可用于抑制动物（包括人类和其他哺乳动物）的病理性细胞增殖的方法。根据本发明的教导，可以使用微细胞毒素化合物来抑制细胞增殖，包括负责肿瘤和其它癌症的细胞增殖。在一个具体实施方案中，本发明的新颖组合物和使用方法可以有利地用于治疗宿主癌细胞的患者，例如抑制哺乳动物宿主中肿瘤细胞的生长。

10. 发明授权

US5298523A Method for treating transplant patients using mycalamide compounds 失效
标题翻译：使用mycalamide化合物治疗移植患者的方法
公开(公告)号：US5298523A
公开(公告)日：1994-03-29
申请号：US990156
申请日：1992-12-14
申请人： Ross E. Longley , Glynn T. Faircloth
发明人： Ross E. Longley , Glynn T. Faircloth
IPC分类号： A61K31/35 , A61K31/42 , A61K31/695 , C07D413/14 , C07D493/04 , C07F7/18 , A01N43/32
CPC分类号： C07D413/14 , A61K31/35 , A61K31/42 , A61K31/695 , C07D493/04 , C07F7/1856
摘要： Mycalamide compounds are derived from marine sponges of the genus Mycale or prepared by synthetic methods. These compounds, and pharmaceutical compositions containing them as active ingredients, are useful as immunomodulatory agents.
摘要翻译： Mycalamide化合物衍生自Mycale属的海绵或通过合成方法制备。这些化合物和含有它们作为活性成分的药物组合物可用作免疫调节剂。

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