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1. 发明授权

US06391900B1 Cytotoxic tris(oxazole)-containing macrolides 失效
标题翻译：含有细菌毒性的三（恶唑）大环内酯类
公开(公告)号：US06391900B1
公开(公告)日：2002-05-21
申请号：US09601146
申请日：2001-01-12
申请人： Tatsuo Higa , Dolores Garcia Gravalos , Jose Luis Fernandez Puentes
发明人： Tatsuo Higa , Dolores Garcia Gravalos , Jose Luis Fernandez Puentes
IPC分类号： A61P3500
CPC分类号： C07D498/22
摘要： The present invention discloses new cytotoxic tris(oxazole)-containing macrolides having the formula: wherein X represents a lower alkyl; R1 and R2 represent hydrogen or lower alkyl; R3a represents hydrogen, and R3b represents or R3a and R3b together represent oxygen; R4 represents hydrogen, lower alkoxy or lower alkyl; R5 represents hydrogen, carbamoyl, or lower alkanoyl; R6a represents hydrogen, and R6b represents hydroxy, or R6a and R6b together represent oxygen; R7 represents hydrogen, lower alkyl, or hydroxymethyl; R8 represents lower alkoxy or lower alkyl; Y1 represents hydrogen or methyl, and y2 represents hydrogen, or Y1 and Y2 together represent a double bond. Also disclose are methods for treating mammals using the macrolides and pharmaceutical preparations including the macrolides.
摘要翻译：本发明公开了具有下式的新的具有细胞毒性的三（恶唑）的大环内酯类：其中X代表低级烷基; R1和R2表示氢或低级烷基; R3a表示氢，R3b表示R3a和R3b表示氧; R4代表氢，低级烷氧基或低级烷基; R5表示氢，氨基甲酰基或低级烷酰基; R6a表示氢，R6b表示羟基，R6a和R6b表示氧; R7表示氢，低级烷基或羟甲基; R8表示低级烷氧基或低级烷基; Y1表示氢或甲基，y2表示氢，Y1或Y2表示双键。还公开了使用大环内酯类和包括大环内酯类药物制剂治疗哺乳动物的方法。

2. 发明授权

US06350755B1 Inhibitors of prenyl-protein transferase 失效
标题翻译：异戊烯基蛋白转移酶的抑制剂
公开(公告)号：US06350755B1
公开(公告)日：2002-02-26
申请号：US09757218
申请日：2001-01-09
申请人： S. Jane deSolms , Anthony W. Shaw
发明人： S. Jane deSolms , Anthony W. Shaw
IPC分类号： A61P3500
CPC分类号： C07D498/18 , C07D515/18
摘要： The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
摘要翻译：本发明涉及抑制异戊烯基 - 蛋白转移酶和致癌基因蛋白Ras的异戊烯化的拟肽大环化合物。本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。

3. 发明授权

US06759431B2 Compositions and methods for treating or preventing diseases of body passageways 失效
公开(公告)号：US06759431B2
公开(公告)日：2004-07-06
申请号：US09933652
申请日：2001-08-20
申请人： William L. Hunter , Lindsay S. Machan
发明人： William L. Hunter , Lindsay S. Machan
IPC分类号： A61P3500
CPC分类号： A61K9/0024 , A61K9/10 , A61K9/1075 , A61K9/12 , A61K9/1635 , A61K9/1647 , A61K9/1652 , A61K9/167 , A61K9/5031 , A61K9/5138 , A61K9/5146 , A61K9/5153 , A61K9/5192 , A61K9/70 , A61K9/7007 , A61K31/00 , A61K31/28 , A61K31/335 , A61K31/337 , A61K33/24 , A61K47/34
摘要： The present invention provides methods for treating or preventing diseases associated with body passageways, comprising the step of delivering to an external portion of the body passageway a therapeutic agent. Representative examples of therapeutic agents include anti-angiogenic factors, anti-proliferative agents, anti-inflammatory agents, and antibiotics.

4. 发明授权

US06313143B1 Substituted pyrroles 有权
标题翻译：取代吡咯
公开(公告)号：US06313143B1
公开(公告)日：2001-11-06
申请号：US09707678
申请日：2000-11-07
申请人： Nader Fotouhi , Emily Aijun Liu , Allen John Lovey , John Guilfoyle Mullin, Jr. , Giuseppe Federico Weber
发明人： Nader Fotouhi , Emily Aijun Liu , Allen John Lovey , John Guilfoyle Mullin, Jr. , Giuseppe Federico Weber
IPC分类号： A61P3500
CPC分类号： C07D403/14 , C07F9/5728 , C07F9/65583
摘要： Disclosed are novel substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are suitable for administration to patients as continuous infusion solution and are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds and methods for the treatment and/or control of cancer.
摘要翻译：公开了具有下式的新颖的取代的吡咯。这些化合物及其药学上可接受的盐适于作为连续输注溶液施用于患者，并且可用于治疗和/或控制细胞增殖性疾病，特别是癌症。还公开了含有前述化合物的药物组合物和用于治疗和/或控制癌症的方法。

5. 发明授权

US06790437B2 Method of treating cancerous tumors with a dendritic-platinate drug delivery system 有权
标题翻译：用树突状药物递送系统治疗癌性肿瘤的方法
公开(公告)号：US06790437B2
公开(公告)日：2004-09-14
申请号：US09881126
申请日：2001-06-14
申请人： Navid Malik , Ruth Duncan
发明人： Navid Malik , Ruth Duncan
IPC分类号： A61P3500
CPC分类号： B82Y5/00 , A61K47/6949 , C08G69/00 , C08G69/02 , C08G83/003 , Y10S424/16
摘要： Dendritic polymer conjugates which are useful drug delivery systems for carrying platinum containing anti-tumor agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to a platinum containing compound capable of interacting with the functional groups, contacting the dendritic polymer with the platinum containing compound, and reacting the dendritic polymer with the platinum containing compound. The dendritic polymer platinates may be administered intravenously, orally, parentally, subcutaneously or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The dendritic polymer platinates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.
摘要翻译：作为携带含有抗肿瘤剂的含铂药物的有用的药物递送系统的树突状聚合物缀合物通过获得具有官能团的树枝状聚合物来制备，所述树枝状聚合物具有能够与所述官能团相互作用的含铂化合物，所述树枝状聚合物接触所述树枝状聚合物与含铂化合物反应，并使树枝状聚合物与含铂化合物反应。树突状聚合物平板可以静脉内，口服，亲本，皮下或局部给予具有有效抑制恶性肿瘤生长的恶性肿瘤的动物。树状聚合物平板显示出高的药物效率，高的药物携带能力，良好的水溶性，良好的储存稳定性，降低的毒性和改善的体内抗肿瘤活性。

6. 发明授权

US06358940B1 Modified 2-Alkoxyestradiol derivatives with prolonged pharmacological activity 失效
标题翻译：具有延长药理活性的改性2-烷氧基雌二醇衍生物
公开(公告)号：US06358940B1
公开(公告)日：2002-03-19
申请号：US09644021
申请日：2000-08-23
申请人： Allan H. Conney
发明人： Allan H. Conney
IPC分类号： A61P3500
CPC分类号： A61K31/56
摘要： Modified 2-alkoxyestradiol compounds wherein all hydrogens of the carbon next to the oxygen of the alkoxy moiety at position 2 are substituted with a halogen, alkyl or aromatic group, or a trifluoromethyl group are provided. Methods of using compositions containing these compounds to inhibit microtubule formation and tubulin polymerization or depolymerization in cells and to treat diseases characterized by abnormal cell mitosis are also provided.
摘要翻译：提供其中在位置2处的烷氧基部分的氧的邻近碳被卤素，烷基或芳基或三氟甲基取代的改性的2-烷氧基二氢化合物。还提供了使用含有这些化合物的组合物抑制微管形成和细胞中的微管蛋白聚合或解聚并且治疗以异常细胞有丝分裂为特征的疾病的方法。

7. 发明授权

US06831090B2 2,3-olefinic epothilone derivatives 有权
标题翻译： 2,3-烯属埃坡霉素衍生物
公开(公告)号：US06831090B2
公开(公告)日：2004-12-14
申请号：US10242437
申请日：2002-09-13
申请人： Gregory D. Vite , Robert M. Borzilleri , Gerhard Höfle , Thomas Leibold
发明人： Gregory D. Vite , Robert M. Borzilleri , Gerhard Höfle , Thomas Leibold
IPC分类号： A61P3500
CPC分类号： C07D491/04 , A61K31/438 , A61K31/5513 , A61K31/5517
摘要： The present invention relates to 2,3-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor. The compounds of the invention as 16-membered macrolides having the general structure, which have microtubule-stabilizing effects and cytotoxic activity against rapidly proliferating cells, such as, tumor cells or other hyperproliferative cellular disease.
摘要翻译：本发明涉及2,3-位修饰的埃坡霉素衍生物，衍生物的制备方法及其中间体。具有一般结构的本发明化合物为具有微管稳定作用和对快速增殖细胞如肿瘤细胞或其它过度增殖性细胞病的细胞毒性活性的16-元大环内酯。

8. 发明授权

US06414015B1 Laulimalide microtubule stabilizing agents 失效
公开(公告)号：US06414015B1
公开(公告)日：2002-07-02
申请号：US09493897
申请日：2000-01-28
申请人： Susan L. Mooberry , Bradley S. Davidson
发明人： Susan L. Mooberry , Bradley S. Davidson
IPC分类号： A61P3500
CPC分类号： A61K31/365
摘要： A method of inhibiting the proliferation of a hyperproliferative mammalian cell having a multiple drug resistant phenotype utilizing an amount of a laulimalide compound effective to disrupt the dynamic state of microtubule polymerization and depolymerization to arrest cell mitosis is disclosed, together with laulimalide compounds which find use in such method.

9. 发明授权

US06326367B1 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents 有权
标题翻译： 2-苯基-1- [4-（2-氨基乙氧基） - 苄基] - 吲哚作为雌激素剂
公开(公告)号：US06326367B1
公开(公告)日：2001-12-04
申请号：US09388581
申请日：1999-09-02
申请人： Chris P. Miller , Michael D. Collini , Bach D. Tran , Arthur A. Santilli
发明人： Chris P. Miller , Michael D. Collini , Bach D. Tran , Arthur A. Santilli
IPC分类号： A61P3500
CPC分类号： C07D403/12 , A61K31/404 , A61K31/405 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/55 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/30 , C07D209/42 , C07D405/04 , C07D405/12
摘要： The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:
摘要翻译：本发明涉及可用作雌激素剂的新的2-苯基-1- [4-（2-氨基乙氧基） - 苄基] - 吲哚化合物，以及使用这些化合物的药物组合物和治疗方法，其具有一般结构如下：

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