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Formulations of suberoylanilide hydroxamic acid and methods for producing same

A technology for suberoylanilide hydroxamic acid and suberoylanilide hydroxime, which is applied in the field of preparing the crystalline composition or pharmaceutical composition, and can solve the problems that DNA is difficult to achieve transcriptional regulatory elements and structures.

Active Publication Date: 2007-11-28
MERCK SHARP & DOHME BV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This affinity causes DNA to bind tightly to histones and makes DNA inaccessible to transcriptional regulatory elements and structures

Method used

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  • Formulations of suberoylanilide hydroxamic acid and methods for producing same
  • Formulations of suberoylanilide hydroxamic acid and methods for producing same
  • Formulations of suberoylanilide hydroxamic acid and methods for producing same

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preparation example Construction

[0073] The preparation of pharmaceutical compositions containing the active ingredients is well known in the art, for example by blending, granulating or tableting. The active therapeutic ingredient is often mixed with excipients which are pharmaceutically acceptable and compatible with the active ingredient. For oral administration, the active agent is mixed with the usual additives used for this purpose, such as carriers, stabilizers or inert diluents. And converted into suitable dosage forms for administration such as tablets as mentioned above, coated tablets, hard or soft gelatin capsules, aqueous, alcoholic or oily suspensions and the like by conventional methods.

[0074] In one embodiment, the oral compositions are formulated in dosage unit form for ease of administration and uniformity of dosage. Unit dosage forms as used herein are physically discrete units suited as unitary dosages for the treatment of individual subjects; each unit containing a predetermined quant...

Embodiment 1

[0242] Synthesis of SAHA Form I

[0243] The SAHA crystalline form can be synthesized according to the method outlined below or any modification and variation thereof

[0244] Synthetic SAHA

[0245] Step 1 - Synthesis of Octanoanilide

[0246]

[0247] 3,500 g (20.09 mol) of suberic acid was placed in a 22 L flask, and the acid was heated to melt. The temperature was raised to 175°C, and then 2,040 g (21.92 mol) of aniline were added. The temperature was raised to 190°C and held at this temperature for 20 minutes. The melt was poured into a Nalgene tank containing 4,017 g potassium hydroxide dissolved in 50 L of water. The melt was added and the mixture was stirred for 20 minutes. The reaction was repeated on the same scale and the second melt was poured into the same sodium hydride solution. After stirring the mixture well, the stirrer was turned off, and the mixture was left to stand. The mixture was...

Embodiment 1A

[0262] Preparation of SAHA Form I

[0263] Step 18 - Anilino-8-oxooctanoic acid; Octanoanilide acid (Compound 3)

[0264] Suberic acid (Compound 1, 174.2 g, 1.0 mol), aniline (Compound 2, 85.8-94.9 g) and toluene (0.1-0.2 L) were combined, heated to reflux, and refluxed for at least 60 hours. The reaction was quenched at reflux by adjusting the pH to >11 with 10% sodium hydroxide solution. The organic layer was combined with toluene (0.11-0.13 L) and water (0.3-0.4 L), and the aqueous layer was separated. The extracted aqueous layer was combined with toluene (0.11-0.13 L), separated into layers, and then separated. The aqueous layer was extracted twice with toluene (0.2-0.3 L) at 60-70°C. The aqueous layer was adjusted to pH 5.8-6.2 using hydrochloric acid and if necessary 10% sodium hydroxide solution at 20-30°C. The mixture was filtered, washed with cold water (0.2-0.3 L), then cold isopropanol. The wet cake was vacuum dried at a maximum of 65°C to obta...

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Abstract

The present invention provides a medicine composition or crystal composition which is provided with specific solubility characters, which includes octanedioyl aniline hydroxamic acids or its medicinal salt or hydrated compound as the active component. The invention also provides a method for preparing the crystal composition or medicine composition. The invention also provides a composition which is provided with specific particle size distribution.

Description

field of invention [0001] The present invention provides a pharmaceutical or crystalline composition having specific dissolution characteristics, said composition comprising suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt thereof as an active ingredient. The present invention provides methods for preparing said crystalline or pharmaceutical compositions. The present invention also provides compositions having a particular particle size distribution. Background of the invention [0002] In this application, various publications are cited as references by Arabic numerals within parentheses. Full citations for these publications can be found at the end of the specification. [0003] Cancer is one in which a population of cells has become, to varying degrees, unresponsive to the control mechanisms that normally govern proliferation and differentiation. For many years, there have been two basic strategies for cancer chemotherapy: a) ...

Claims

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Application Information

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IPC IPC(8): A61K31/19A61P35/00A61K31/00
CPCA61K31/19A61P35/00
Inventor J·C·王A·S·科特E·A·迪恩曼K·加拉赫尔C·伊克达J·莫塞P·拉尼亚克R·A·里德C·斯塔布克H·-H·董Q·王B·M·科亨V·R·卡波丹诺B·塞尔T·A·米勒
Owner MERCK SHARP & DOHME BV
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