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Vitronectin receptor antagonist pharmaceuticals for use in combination therapy

A compound, pharmaceutical technology, applied in the field of new drugs

Inactive Publication Date: 2005-02-16
布里期托尔－迈尔斯斯奎布药品公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, even progressive occlusion often results in the formation of an infarcted area because the resulting angiogenesis is insufficient to prevent damage

Method used

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  • Vitronectin receptor antagonist pharmaceuticals for use in combination therapy
  • Vitronectin receptor antagonist pharmaceuticals for use in combination therapy
  • Vitronectin receptor antagonist pharmaceuticals for use in combination therapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[1568] 2-(((4-(4-(((3-(2-(2-(3-((6-((1-aza-2-(2-sulfophenyl))vinyl) Amino)(3-pyridyl))carbonylamino)propoxy)ethoxy)ethoxy)propyl)amino)sulfonyl)phenyl)phenyl)sulfonyl)amino)-3-((7- ((Imidazol-2-ylamino)methyl)-1-methyl-4-oxo(3-hydroquinolyl)carbonylamino)propionic acid Trifluoroacetate

[1569] Part A - N-(3-(2-(2-(3-aminopropoxy)ethoxy)ethoxy)propyl)(phenylmethoxy)formamide

[1570]4,7,10-trioxa-1,13-tridecanediamine (158ml, 0.72mol), TEA (16.7ml, 0.12mol) and methanol (300ml) were dissolved in peroxide-free THF (1000ml) The solution in was placed in a 3-liter three-necked flask with a nitrogen line equipped with a mechanical stirrer, thermometer, and dropping funnel. The dropping funnel was charged with a solution of benzyl chloroformate (17.1 mL, 0.12 mol) in peroxide-free THF (1000 mL). With rapid stirring, the contents of the dropping funnel were added to the flask over 4 hours while maintaining the temperature below 5°C. The solution was stirred for an additional 30 ...

Embodiment 2

[1613] 3-((7-((imidazol-2-ylamino)methyl)-1-methyl-4-oxo(3-hydroquinolyl))carbonylamino)-2-(((4-(4- (((3-(2-(2-(3-(2-(1,4,7,10-tetraaza-4,7,10-tris(carboxymethyl)cyclododecyl)acetyl Amino)propoxy)ethoxy)ethoxy)propyl)amino)sulfonyl)phenyl)phenyl)sulfonyl)amino)propionic acid Bis(trifluoroacetate)

[1614] Part A - Benzyl 2-(1,4,7,10-tetraaza-4,7,10-tris(((tert-butyl)oxycarbonyl)methyl)cyclododecyl)acetate

[1615] Stirring (1,4,7,10-tetraaza-4,7-bis(((tert-butyl)oxycarbonyl)methyl)cyclododecyl)acetic acid at ambient temperature under nitrogen atmosphere A solution of tert-butyl ester (0.9222g, 1.79mmol), TEA (1.8ml) and benzyl bromoacetate (0.86ml, 5.37mmol) in anhydrous DMF (24ml) for 24 hours. DMF was removed in vacuo, and the resulting oil was dissolved in EtOAc (300ml). The solution was washed sequentially with water (2 x 50ml) and saturated sodium chloride (50ml), dried (magnesium sulfate) and concentrated to give the title compound (1.26g) as an amorphous solid. MS: ...

Embodiment 3

[1632] 2-(((4-(3-(N-(3-(2-(2-(3-((6-((1-aza-2-(2-sulfophenyl)vinyl)amino) (3-pyridyl))carbonylamino)propoxy)ethoxy)ethoxy)propyl)carbamoyl)propoxy)-2,6-dimethylphenyl)sulfonyl)amino)- 3-((7-((imidazol-2-ylamino)methyl-1-methyl-4-oxo(3-hydroquinolyl))carbonylamino)propanoic acid Trifluoroacetate

[1633] Part A - Ethyl 4-(3,5-dimethylphenoxy)butanoate

[1634]Sodium metal (17.12 g, 0.744 mmol) was added to absolute ethanol (350 ml), and stirred until dissolved. 3,5-Dimethylphenol was added, and the solution was stirred at ambient temperature for 15 minutes. Ethyl 4-bromoacetate (58.7ml, 0.41mol) was added and the solution was stirred at ambient temperature under nitrogen for 28 hours. Ethanol was removed in vacuo, and the oily solid was partitioned between water (1 L) and EtOAc (500 ml). The aqueous layer was extracted with additional EtOAc (500ml). The combined EtOAc extracts were washed sequentially with saturated sodium bicarbonate (300ml) and saturated sodium chloride ...

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Abstract

The present invention describes novel kits and compositions comprising compounds of the formula (I): (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer in combination therapy in a patient. The present invention provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.

Description

field of invention [0001] The present invention provides novel drugs for use in diagnosing and treating cancer, methods of imaging tumors in patients, and methods of treating cancer in patients. The present invention also relates to novel pharmaceutical compositions and combination therapies comprising a compound of the present invention, or a pharmaceutically acceptable salt thereof, and at least one agent selected from anticancer agents and radiosensitizers. In addition, the present invention also relates to novel pharmaceutical compositions and combination therapies comprising a compound of the present invention or a pharmaceutically acceptable salt thereof and a photosensitizer. The medicament of the present invention consists of a targeting moiety that binds to the vitronectin receptor expressed in tumor vasculature, an optional linker, and a therapeutically effective radioisotope or a diagnostically effective imageable moiety. Therapeutically effective radioisotopes emi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/26A61K31/138A61K31/4164A61K31/4196A61K31/454A61K31/4709A61K31/53A61K31/5377A61K31/566A61K31/569A61K31/57A61K31/58A61K31/7052A61K31/724A61K38/00A61K38/21A61K38/24A61K41/00A61K45/00A61K47/16A61K47/26A61K47/34A61K47/40A61K51/00A61K51/04A61P9/00A61P35/00A61P43/00C07D401/14C08B37/16
CPCA61K41/0038A61K51/0482A61P35/00A61P43/00A61P9/00
Inventor T·D·哈里斯J·A·巴雷特A·P·小卡彭特M·拉乔帕耶
Owner 布里期托尔－迈尔斯斯奎布药品公司
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