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1. 发明授权

US5705514A Signal transduction inhibitor compounds 失效
标题翻译：信号转导抑制剂化合物
公开(公告)号：US5705514A
公开(公告)日：1998-01-06
申请号：US455825
申请日：1995-05-31
申请人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
发明人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
IPC分类号： A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4192 , A61P35/00 , C07D233/90 , C07D249/04
CPC分类号： A61K31/4164 , A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4192 , C07D233/90 , C07D249/04
摘要： A method of inhibiting the invasion and metastasis of malignant solid tumors in mammals, said method comprising administering to said mammal an anti-proliferative, anti-invasive and anti-metastasis effective amount of a compound selected from the group of formulas consisting of: ##STR1## wherein: p is an integer of from 0 to 4; Ar.sup.1 is a moiety selected from the group consisting of --Ar.sup.2 --X--Ar.sup.3, phenyl, trioxaadamantyl, anthracenyl, anthraquinonyl, naphthyl, phenanthryl, and substituted versions thereof; Ar.sup.2 and Ar.sup.3 are each aromatic moieties independently selected from the group consisting of phenyl, naphthyl, and substituted versions thereof; X is a linking moiety selected from the group consisting of O, S, SO.sub.2 2, CO, CHCN, straight chain alkyl, alkoxy, and alkoxyalkyl; and Z is a nitrogen-containing heterocyclic moiety selected from the group consisting of imidazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl and substituted versions thereof, said heterocyclic moieties being attached to the --(CH.sub.2).sub.p -- portion of the molecule at the N1 position of the heterocycle.
摘要翻译：一种抑制哺乳动物恶性实体瘤侵袭和转移的方法，所述方法包括对所述哺乳动物施用抗增殖，抗侵袭和抗转移的有效量的选自下组的化合物：Z（ CH 2）pAr 1（I）和（II）其中：p是0至4的整数; Ar1是选自-Ar2-X-Ar3，苯基，三氧杂金刚烷基，蒽基，蒽醌基，萘基，菲基及其取代形式的部分; Ar 2和Ar 3各自独立地选自苯基，萘基及其取代形式的芳族部分; X是选自O，S，SO22，CO，CHCN，直链烷基，烷氧基和烷氧基烷基的连接部分; 并且Z是选自咪唑基，1,2,3-三唑基，1,2,4-三唑基及其取代形式的含氮杂环部分，所述杂环部分连接到 - （CH 2）p - 分子在杂环的N1位的部分。

2. 发明授权

US5602156A Method for inhibiting metalloproteinase expression 失效
标题翻译：抑制金属蛋白酶表达的方法
公开(公告)号：US5602156A
公开(公告)日：1997-02-11
申请号：US209089
申请日：1994-03-10
申请人： Elise C. Kohn , Lance A. Liotta
发明人： Elise C. Kohn , Lance A. Liotta
IPC分类号： A61K31/41 , A61K31/415
CPC分类号： A61K31/415 , A61K31/41
摘要： Calcium homeostasis is an important regulator of MMP-2 transcription, activation and activity. Disclosed herein are compounds which inhibit the expression of matrix metalloproteinases in cells. Pharmaceutical application of these compounds to inhibit the expression of MMPs offers a new approach to cancer treatment as well as treatment for nerve healing, degenerative cartilagenous diseases, decubitus ulcers, arthritis, Alzheimer's disease, wound healing, proliferative retinopathy, proliferative renal diseases, corneal ulcers and fertility problems.
摘要翻译：钙稳态是MMP-2转录，激活和活性的重要调节因子。本文公开了抑制细胞中基质金属蛋白酶表达的化合物。这些化合物抑制MMP表达的药物应用提供了一种新的治疗方法，以及治疗神经愈合，退行性软骨疾病，褥疮性溃疡，关节炎，阿尔茨海默氏病，伤口愈合，增殖性视网膜病变，增殖性肾病，角膜溃疡和生育问题。

3. 发明授权

US6057346A Inhibition of retroviral LTR promoters by calcium response modifiers 失效
标题翻译：通过钙反应调节剂抑制逆转录病毒LTR启动子
公开(公告)号：US6057346A
公开(公告)日：2000-05-02
申请号：US353765
申请日：1994-12-12
申请人： Elise C. Kohn , Lance A. Liotta , Kevin L. Gardner
发明人： Elise C. Kohn , Lance A. Liotta , Kevin L. Gardner
IPC分类号： A61K31/4174 , A61K31/4192 , A61K31/41 , A01N43/64
CPC分类号： A61K31/4174 , A61K31/4192
摘要： A class of calcium-response modification compounds is disclosed which inhibits the activation of retroviral LTR promoters, including the HIV-LTR. This class of compounds are used to delay or suppress the transition of a retroviral infection from a latent to a virulent condition, thereby ameliorating retrovirally caused diseases such as AIDS. The compounds are also useful in cancer treatment, allowing for coordinated therapeutic approaches to retroviral diseases and related cancers such as AIDS and Kaposi's Sarcoma. The compounds are also useful in standardizing in vitro assays of clinical and experimental importance.
摘要翻译：公开了一类钙响应修饰化合物，其抑制包括HIV-LTR在内的逆转录病毒LTR启动子的活化。这类化合物用于延缓或抑制逆转录病毒感染从潜伏状态转变为有毒状态，从而改善逆转录病毒引起的疾病如艾滋病。该化合物也可用于癌症治疗，允许对逆转录病毒疾病和相关癌症如AIDS和卡波西肉瘤的协调治疗方法。该化合物还可用于标准化临床和实验重要性的体外测定。

4. 发明授权

US5405782A Detection and quantitation method for therapeutic agents in blood 失效
标题翻译：血液中治疗剂的检测和定量方法
公开(公告)号：US5405782A
公开(公告)日：1995-04-11
申请号：US41438
申请日：1993-03-31
申请人： Elise C. Kohn , Lance A. Liotta
发明人： Elise C. Kohn , Lance A. Liotta
IPC分类号： G01N30/00 , G01N30/02 , G01N30/06 , G01N30/62 , G01N30/88 , G01N33/94
CPC分类号： G01N33/94 , G01N2030/009 , G01N2030/027 , G01N2030/062 , G01N2030/626 , G01N2030/8804 , G01N2030/8822 , Y10T436/25125 , Y10T436/255
摘要： The present invention relates to an improved method for the determination of therapeutic agents in blood. This method utilizes a solid phase extraction of the solute from plasma followed by reverse phase high performance liquid chromatography on a column of irregularly shaped C-18 modified silica. Comparison of the produced chromatogram with a standard curve provides a precise and accurate quantification of the amount of the solute in blood. Additionally, the extraction and chromatography steps can be readily automated for the rapid determination of multiple samples.
摘要翻译：本发明涉及一种用于测定血液中治疗剂的改进方法。该方法利用等离子体固相萃取溶剂，然后在不规则形状的C-18改性二氧化硅柱上进行反相高效液相色谱。产生的色谱图与标准曲线的比较提供了血液中溶质量的精确和准确的量化。此外，萃取和色谱步骤可以容易地自动化，以快速测定多个样品。

5. 发明授权

US06790936B1 CAI resistance proteins and uses thereof 失效
标题翻译： CAI抗性蛋白及其用途
公开(公告)号：US06790936B1
公开(公告)日：2004-09-14
申请号：US09436469
申请日：1999-11-08
申请人： Elise C. Kohn , Lance A. Liotta , Young Sook Kim
发明人： Elise C. Kohn , Lance A. Liotta , Young Sook Kim
IPC分类号： C07K1475
CPC分类号： C12N15/52 , A61K48/00 , C07K14/47
摘要： The invention provides for proteins correlated with cellular resistance to carboxyamido-triazole (CAI) which have at least one Src homology 3 (SH3) binding domain, and functionally equivalent compounds.
摘要翻译：本发明提供与具有至少一个Src同源性3（SH3）结合结构域和功能等同化合物的羧基酰氨基 - 三唑（CAI）的细胞抗性相关的蛋白质。

6. 发明授权

US5498620A Signal transduction inhibitor 1,2,3-triazolo compounds 失效
标题翻译：信号转导抑制剂1,2,3-三唑类化合物
公开(公告)号：US5498620A
公开(公告)日：1996-03-12
申请号：US455761
申请日：1995-05-31
申请人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
发明人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
IPC分类号： A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4192 , C07D233/90 , C07D249/04 , C07D249/06
CPC分类号： A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4192 , C07D233/90 , C07D249/04
摘要： A compound having the formula: ##STR1## and pharmaceutically acceptable salts thereof.
摘要翻译：具有下式的化合物及其药学上可接受的盐。

7. 发明授权

US5880129A Methods of inhibiting invasion and metastasis of malignant solid tumors 失效
标题翻译：抑制恶性实体瘤侵袭转移的方法
公开(公告)号：US5880129A
公开(公告)日：1999-03-09
申请号：US906542
申请日：1997-08-05
申请人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
发明人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
IPC分类号： A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4192 , C07D233/90 , C07D249/04 , A61K31/495 , A61K31/505 , C07D239/26 , C07D241/10
CPC分类号： A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4192 , C07D233/90 , C07D249/04
摘要： A discovery underlying this invention is the concordance between particular cellular signaling mechanisms and cancer cell growth and metastasis. It has now been discovered that certain compounds inhibit the signal transduction required for the maintenance and driving of the malignant process. These compounds are also effective for the in vivo treatment of solid tumors and related disease states. This invention provides a method for the use of these compounds to inhibit the invasion and metastasis of malignant solid tumors in mammals. This invention further provides a method for using related compounds to treat diseases involving aberrant signal transduction pathways. Some of the compounds used in the methods of the present invention are novel and constitute another aspect of this invention.
摘要翻译：本发明的发现是特定细胞信号传导机制与癌细胞生长和转移之间的一致性。现在已经发现某些化合物抑制维持和驱动恶性过程所需的信号转导。这些化合物对于实体瘤和相关疾病状态的体内治疗也是有效的。本发明提供了一种使用这些化合物抑制哺乳动物恶性实体瘤侵袭和转移的方法。本发明还提供了使用相关化合物治疗涉及异常信号转导途径的疾病的方法。在本发明的方法中使用的一些化合物是新的，构成本发明的另一方面。

8. 发明授权

US5565478A Combination therapy using signal transduction inhibitors with paclitaxel and other taxane analogs 失效
标题翻译：使用信号转导抑制剂与紫杉醇和其他紫杉烷类似物的联合治疗
公开(公告)号：US5565478A
公开(公告)日：1996-10-15
申请号：US212612
申请日：1994-03-14
申请人： Elise C. Kohn , Eddie Reed , Lance A. Liotta
发明人： Elise C. Kohn , Eddie Reed , Lance A. Liotta
IPC分类号： A61K31/40 , A61K31/415 , A61K31/41 , A61K31/335
CPC分类号： A61K31/40 , A61K31/415
摘要： The present invention provides compositions and methods for the treatment of cancer in a subject wherein compounds of formula I defined herein in combination with paclitaxel or other modified taxane analogs provide enhanced anticancer effects over the effects achieved with the individual compounds.
摘要翻译：本发明提供了在受试者中治疗癌症的组合物和方法，其中本文定义的式I化合物与紫杉醇或其他修饰的紫杉烷类似物相结合，提供比单独化合物实现的效果更强的抗癌作用。

9. 发明授权

US5482954A Signal transduction inhibitor triazole and diazole compounds 失效
标题翻译：信号转导抑制剂三唑和二唑化合物
公开(公告)号：US5482954A
公开(公告)日：1996-01-09
申请号：US270181
申请日：1994-07-01
申请人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
发明人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
IPC分类号： A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4192 , A61P35/00 , C07D233/90 , C07D249/04 , C07D249/06
CPC分类号： A61K31/4164 , A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4192 , C07D233/90 , C07D249/04
摘要： A discovery underlying this invention is the concordance between particular cellular signaling mechanisms and cancer cell growth and metastasis. It has now been discovered that certain compounds inhibit the signal transduction required for the maintenance and driving of the malignant process. These compounds are also effective for the in vivo treatment of solid tumors and related disease states. This invention provides a method for the use of these compounds to inhibit the invasion and metastasis of malignant solid tumors in mammals. This invention further provides a method for using related compounds to treat diseases involving aberrant signal transduction pathways. Some of the compounds used in the methods of the present invention are novel and constitute another aspect of this invention.
摘要翻译：本发明的发现是特定细胞信号传导机制与癌细胞生长和转移之间的一致性。现在已经发现某些化合物抑制维持和驱动恶性过程所需的信号转导。这些化合物对于实体瘤和相关疾病状态的体内治疗也是有效的。本发明提供了一种使用这些化合物抑制哺乳动物恶性实体瘤侵袭和转移的方法。本发明还提供了使用相关化合物治疗涉及异常信号转导途径的疾病的方法。在本发明的方法中使用的一些化合物是新的，构成本发明的另一方面。

10. 发明授权

US5359078A Signal transduction inhibitor compounds 失效
标题翻译：信号转导抑制剂化合物
公开(公告)号：US5359078A
公开(公告)日：1994-10-25
申请号：US985402
申请日：1992-12-04
申请人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
发明人： Elise C. Kohn , Lance A. Liotta , Christian C. Felder
IPC分类号： A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4192 , A61P35/00 , C07D233/90 , C07D249/04 , C07D249/06
CPC分类号： A61K31/4164 , A61K31/12 , A61K31/41 , A61K31/415 , A61K31/4192 , C07D233/90 , C07D249/04
摘要： A compound having the formula:Y--(CH.sub.2).sub.p --Ar.sup.11 --X--Ar.sup.12wherein:p is an integer of from 0 to 4;Ar.sup.11 and Ar.sup.12 are each aromatic moieties independently selected from the group consisting of phenyl, naphthyl, and substituted versions thereof in which the substituents are members selected from the group consisting of halogen, nitro, carboxyl and alkoxy;X is a linking moiety selected from the group consisting of O, S, SO.sub.2, CO, CHCN, straight chain alkyl, alkoxy, and alkoxyalkyl; andY is a nitrogen-containing heterocyclic moiety.
摘要翻译：具有下式的化合物：Y-（CH2）p-Ar11-X-Ar12其中：p为0-4的整数; Ar 11和Ar 12各自独立地选自苯基，萘基及其取代形式的芳族部分，其中取代基是选自卤素，硝基，羧基和烷氧基的成员; X是选自O，S，SO 2，CO，CHCN，直链烷基，烷氧基和烷氧基烷基的连接部分; Y是含氮杂环部分。

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