MXPA06008449A

MXPA06008449A - Bisarylurea derivatives

Info

Publication number: MXPA06008449A
Application number: MXPA/A/2006/008449A
Authority: MX
Inventors: Grell Matthias; Amendt Christiane; Buchstaller Hanspeter; Zenke Frank; Sirrenberg Christian; Burgdorf Lars; Stieber Frank
Original assignee: Amendt Christiane; Buchstaller Hanspeter; Burgdorf Lars; Grell Matthias; Merck Patent Gmbh; Sirrenberg Christian; Stieber Frank; Zenke Frank
Priority date: 2004-01-30
Filing date: 2006-07-26
Publication date: 2006-12-13

Abstract

The present invention relates to bisarylurea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.

Description

SALTY FOOD COMPOSITION COMPRISING LOW COMPOSITION IN TRIGLYCERIDES OF TRANS FATTY ACIDS Field of the Invention The present invention relates to a seasoned food composition in powder form that flows freely without compression, this composition comprises a fat powder and salt. More specifically, the fat is (a mixture of) triglycerides and fatty acids, wherein the composition is low in triglycerides of trans-unsaturated fatty acids.

Antecedents of the Invention There is a huge group of food compositions (eg, seasoned food compositions) that are in powder form that flow freely with tablets, packaged in, eg, divided sachets. These compositions are generally dry, and can produce an edible product when mixed with water, optionally with heating. Dry in this context is understood to comprise at least 15% (by weight), preferably less than 10% (by weight) of water. Examples of these products are, for example, mixtures of powdered soup and sauce (or ingredients thereof, such as binders), but also mixtures of desserts, which can be (part of) instant products (e.g., instant pasta with a sauce composition in REF: 173953 powder, either packed separately or in a mutual package). These compositions usually contain fat and either salt or sugar, together with a variety of other components (seasonings, dyes, fine herbs, spices, dried or powdered vegetable particles, dried pieces of meat or cheese, etc.). The consumer often uses this powder form that flows freely without compressing, and therefore this is a desired physical format. The fats in this composition generally comprise a considerable amount of triglycerides of fatty acids (hereinafter to shorten triglycerides). Fats are usually mixtures of different triglycerides. The type of fat or mixture of fats used for a given purpose is determined (along with availability and price) for example, the properties of the fat and how it develops in a given product, and in the production of this product. The fat should develop good, eg, taste, by dissolving in the mouth / preserving the taste, but also in the ability to be processed into a suitable product as well as the performance in the packaged product, eg, preservation. Additionally, in the present case, the greases must be compatible with the desired shape of the powder composition that flows freely without compression. This means that for the same purposes a small amount of liquid fat (liquid at room temperature, eg, oil) can be used, which can be, eg, adsorbed by other powdered ingredients. However, there are limits to the amount of this liquid oil, eg, it should not form a large piece in the package. When there is more then a certain amount of grasses is desired, not all fat can be in the form of liquid oil. For other purposes (eg, specific manufacturing processes) a liquid fat is not desired at all. Therefore, a grease which is highly "solid at room temperature, and which can be made in a powder form that flows freely without compression, preferably as a free-flowing powder, is needed in this context. The fat is in the form of powder, flakes or granules, all with a small size smaller than 2x2x2 mm, preferably less than lxlxl mm, more preferably less than 0.5x0.5x0.5 mm.The triglycerides (which are part of or all of the fat) are usually obtained from vegetable sources and may have been subjected to different treatments, such as division (dry or wet), purification, hardening, interesterification, mixing, etc., to give the fat the desired properties of the product. unsaturated fats or triglycerides in saturated or partially unsaturated fats or triglycerides is a particular tool used to obtain the desired dissolution behavior. shape, oils or soft fats can be transformed into fats that show more suitable properties for solids or solid formulations. The hardening process may cause the formation of a certain amount of the so-called trans-unsaturated fatty acids (and / or triglycerides of these trans-unsaturated fatty acids), abbreviating TFA 's (for its acronym in English). For different reasons it may be desired to reduce or eliminate the amount of trans-unsaturated fatty acids (and their triglycerides) in the products. For spreading (margarines and the like) a wide variety of possible fat and triglyceride alternatives is proposed, which is disclosed in eg WO 97/16978 and WO 96/39855. The triglycerides mentioned in such applications frequently contain lauric acid (C12 saturated fatty acid). It has been found that when one wishes to find an alternative for trans-unsaturated fatty acids (and fats that contain them) in seasoned applications lauric acid is undesirable. Lauric acid and triglycerides containing lauric acid can show a wide variety of properties, in particular the behavior of the solution, but in a seasoned application we find that the triglycerides of lauric acid give rise to a (soapy) rancid taste, especially after a prolonged storage. Therefore, there is a desire for non-compressed dry, seasoned, free-flowing food products containing fats triglycerides that are low in trans-unsaturated fatty acids (eg, below 5% of the total fats present, preferably less than 2%), but which must still develop well in a (seasoned) composition, in particular that is related to ease of processing, staining with fat, crystallization, buccal perception, and other characteristics mentioned above. Preferably, this product should also be under lauric acid or triglycerides thereof (eg, below 10% of the total fats present, preferably less than 3%, more preferably less than 0.5% by weight of the total fats present ). Solutions to this have been proposed in patent application PCT / EP03 / 12031. However, it is not directed to how a free flowing, low fat, unsaturated fatty acid powder can be obtained which can develop well in a seasoned food composition which is in a free flowing, non-compressed powder form. . A possible solution could be the use of fats with high melting points. However, these fats do not generally show acceptable behavior in the final product, eg,. mouth feeling, dissolving in the mouth (may be waxy), etc. Thus, there is a need for a grease that can be made into a grease that is in the form of powder at room temperature, preferably a free flowing fat powder, in a convenient medium. Additionally, this grease should show good properties in the final product as discussed above. Although the dough (eg, at least 80% by weight of the total formulation) of the ingredients will be a free flowing non-compressed powder material, the seasoned compositions according to the present invention may comprise, e.g. , up to 20% by weight of the total dry matter formulation, which is not powdered, eg, pieces of dried herbs, vegetables, coscurros, cheese or meat. These ingredients are used in, for example, dry soups or sauces formulations and, when dispersed in the mass of the powder material, they do not affect the free flowing nature of the product without compression. Oily, free flowing, non-compressed powder materials, such as starch, maltodextrins, powdered vegetables, monosodium glutamate, etc., may be present together with, for example, grease and salt. Triglyceride fats can be grouped according to the fatty acids of which they consist (ie, the acyl radical of the triglycerides). Such groups can be identified by a letter, and wherein: H means saturated fatty acid of 16 carbon atoms or greater (C16 +, eg, up to C24) U means unsaturated fatty acids in cis conformation (of any chain length) E means unsaturated fatty acids in conformation trans (of any chain length) M means saturated fatty acids of 10-16 carbon atoms (C10-C14) Since the current application is about triglycerides such as fatty acids, the fatty acid composition of triglycerides is given by Example: H3 (means a triglyceride of 3 saturated fatty acids of 16 or more carbon atoms) H2E (means a triglyceride of 2 saturated fatty acids of 16 or more carbon atoms and 1 trans-unsaturated fatty acid) H2M (means a triglyceride of 2 saturated fatty acids of 16 or more carbon atoms and 1 saturated fatty acid of 10-14 carbon atoms) H2U (means a triglyceride of 2 saturated fatty acids of 16 or more carbon atoms) no and 1 cis-unsaturated fatty acid) HE2 (means a triglyceride of 1 saturated fatty acid of 16 or more carbon atoms and 2 trans-unsaturated fatty acids), and so on, three other letter codes. The fat compositions can thus be characterized in that they contain certain percentages by weight (based on the total amount of triglycerides) or triglycerides of the above codes. Although it is mentioned for E and U they can have any length, it is understood that this creates fatty acids of about 8-24 carbon atoms, and more usually of 16-20 carbon atoms. The fatty acids known in triglycerides are palmitic acid (C16: 0) and stearic acid (C18: 0). The contents of these can be measured in the triglycerides of fatty acids.

Brief Description of the Invention It has now been found that the objectives given above can be met (at least in part) with the use of a seasoned food composition which is in a free flowing, uncompressed powder form of a fat particle which comprises triglycerides of fatty acids, wherein the amount of H3 (triglyceride of 3 saturated fatty acids of 16 or more carbon atoms) and H2U (triglycerides of 2 saturated fatty acids of 16 or more carbon atoms and 1 cis-unsaturated fatty acid ) taken together is at least 55% (preferably at least 65%) by weight based on the total amount of triglycerides, and wherein the ratio of palmitic acid / stearic acid in the triglycerides of fatty acid is less than 4. preferably the ratio is less than 3, more preferably below 2. In other words: of the fat in the composition according to the invention H3 + H2U > 55%, preferably > 65% by weight, based on the total triglycerides, together with the referred ratio of palmitic acid / stearic acid in the triglycerides of fatty acid. This means that the total amount of triglycerides present in the fat composition according to the invention is at least 55% by weight (preferably at least 65% by weight) are triglycerides with C16 fully saturated and larger chains (eg, C16, C18, C20, C22 and C24) - and / or triglycerides containing one cis-unsaturated fatty acid of any chain length and two saturated fatty acids of 16 or more carbon atoms. Additionally, it has been found that the quantity is preferred. of stearic acid in the triglycerides of the fat composition is at least 15% of all the fatty acids in the triglycerides, preferably at least 20%, more preferably at least 25%. Preferably, the. The ratio of palmitic acid / stearic acid in the triglycerides of fatty acid is at least 0.2, preferably at least 0.5 (in connection with any of the upper limits given above). With respect to crystallization properties, it was found that for the purpose given, it is important that the composition be such that a combination of high level of solids formation (at a given time) and a rapid full onset of crystallization ( and not only the latter, which can be achieved as known fats, while having good oral sensation and other properties of use.An indication of the formation of solids and the rate of crystallization can be given by crystallization experiments and measurements of N-values It was found that the fat specified above can be processed into required grease particles (or even more preferably into free flowing powder) by spray cooling of the grease.

Detailed Description of the Invention In the fat used in this invention it is preferred that the amount of H3 • (triglyceride of 3 saturated fatty acids of 16 or more carbon atoms) is at least 20% by weight based on the total amount of triglycerides, preferably at least 25%. Also, it is preferred that the amount of H2U (triglyceride of 2 saturated fatty acids of 16 or more carbon atoms and 1 cis-unsaturated fatty acid) taken together is at least 30% by weight based on the total amount of triglycerides. In addition to the amounts of H3 and H2U, the use of fats of this composition with a particular ratio may be preferred. In this case, the ratio of H3 / H2U is preferably between 0.5 and 1.2. It is preferred that the amount of H (ie, saturated fatty acids of 16 or more carbon atoms) of the fat is between 55 and 80%, preferably between 60 and 75% by weight based on the total amount of the fatty acids. Normally, only fatty acids with an even number of carbon atoms are used. Similarly, it is preferred that the amount of U (cis-unsaturated fatty acids with suitable chain length) be between 20- and 45% by weight based on the amount of fatty acids. In the fat as used in the present invention the amount of palmitic fatty acid (C16: 0) in the triglycerides is preferably between 25 and 50% by weight based on the total amount of fatty acids. A preferred (preferably free flowing) fat according to the invention comprises 25-100% of a mixture of interesterified fats of: (a) 40-80% PO (palm oil) and (b) 20-60% of a Fully hardened fat such as rapeseed (with a melting point of 68 ° C, ie RP68) and / or soybean oil (with a melting point of 65 ° C, ie BO 65), and / or sunflower oil or fully hardened). Alternatively to this may be mixtures of interesterified fats from the same part (b) above, but from part (a) a mixture of a dry fractionated palm stearin (e.g., with a melting point of about 53 °). C) and unhardened rapeseed oil. Following the invention, it is possible to make a seasoned food composition in a non-compressed free flowing powder form, comprising 0.5-50% by weight (preferably 1-40% by weight) of particulate fat according to this invention. , 2-80% in -weight (preferably 5-50%) of an edible salt and this composition contains less than 15% by weight (preferably less than 10% by weight) of water. In this, the triglycerides can be selected such that they contain less than 5%, preferably less than 2% by weight of trans-unsaturated fatty acids, and preferably having less than 10% by weight (more preferably less than 3%, more preferably less than 0.5 %) of lauric acid, and where fats still have the desired fusion and crystallization behavior. Generally, these compositions further comprise 0.1-50% by weight of starch and / or flour and / or maltodextrin and / or 0.1-50% by weight of fine powdered herbs and / or spices and / or tomato powder and / or monosodium glutamate. The seasoned compositions according to the present invention may comprise, eg, up to 20% by weight of the dry total formulation of the dry matter which is not powdered, eg, pieces of dried fine herbs, vegetable, custard , cheese or meat. Examples of the composition according to the above are soup concentrates or sauce, which produces a soup or sauce upon mixing and heating with an aqueous liquid. Such soup or sauce concentrates preferably in the form of a free flowing powder, optionally containing vegetable particles such as dried fine herbs or pieces of vegetables. As mentioned, a small amount of liquid oil may be present (eg, 0.1-5% by weight based on the total composition). After the previous one, it is now possible to prepare, eg, dry soup concentrates or sauce in a free flowing, uncompressed powder form containing a large portion of vegetable fats, this composition is substantially free of trans fatty acids or triglycerides of these. In the above compositions at least 50% of the fats are of vegetable origin, and the compositions substantially free of trans-unsaturated fatty acids or triglycerides thereof. Preferably, the compositions according to the invention are substantially free of animal fat.

EXAMPLES Blends of fat 1-3 were prepared by combining different fats and fats produced specifically according to the upper section of Table 1. Pos is a dry fractionated palm ester with a melting point of approximately 53 ° C, the PO is a non-hardened palm oil, PO 58 is a palm oil hardened to the melting point of 58 ° C. The mixture of fats "Mixture A" was prepared by interesterification of a mixture of palm oil (PO) 60%, rapeseed 40% (RP68). In the second half of table 1 the fatty acid composition is given according to the definitions as defined herein. The same data is given for another fat as comparative example (A) and (B). Table 1 Note: The numbers of all fats given with the 3-letter codes are not added up to 100%, while other minor amounts of other fats are also present.

The fats 1, 2 and 3 can be made into freely flowing powder by means of conventional spray cooling. The fats and fat blends of Table 1 have been analyzed for their crystallization rate and N-values, measurements of the N-values are a standard in the fat industry. The crystallization rate as measured in the present was done by completely melting the fat, and then maintained at a temperature of 20 ° C. After intervals of 5, 10, 15 and 20 minutes the crystallized fat content was measured (using NMR). The results are shown in table 2.

Table 2. Crystallization rates and N-values (Continued) Table 2 Crystallization rates and N-values The above fat blend 3 has been used in the following compositions The products were made using conventional processing. Both were powdered mixes, which could be made in a soup and sauce in a conventional way. It is noted that in relation to this date, the best method known to the applicant to carry out the aforementioned invention, is that which is clear from the present description of the invention.

Claims

CLAIMS Having described the invention as above, the content of the following claims is claimed as property. 1. Seasoned food composition in a free flowing powder form not included, this composition comprises 0.5-50% by weight (preferably 1-40% by weight) of powdered fat, "2-80% by weight (preferably 5- 50%) of an edible salt, this composition contains less than 15% by weight (preferably less than 10% by weight) of water, characterized in that the powdered fat comprises triglycerides of fatty acids of which the amount of H3 (triglycerides of 3 saturated fatty acids of 16 or more carbon atoms) and H2U (triglycerides of 2 saturated fatty acids of 16 or more carbon atoms and 1 cis-unsaturated fatty acid) together is at least 55% by weight based on the total amount of triglycerides, and wherein the ratio of palmitic acid / stearic acid in the triglycerides of fatty acid is less than 4 and at least 0.2 2. Seasoned composition according to claim 1, characterized in that the ratio of palmitic acid / Stearic acid in triglycerides of fatty acids is at least 0.5. 3. Seasoned composition according to claim 1-2, characterized in that the amount of stearic acid in the triglycerides is at least 15% of all the fatty acids in the triglycerides. . Seasoned composition according to claim 1-3, characterized in that the amount of H3 + H2U is at least 65% by weight based on the total amount of triglycerides. Seasoned composition according to claim 1-4, characterized in that H3 (triglyceride of 3 saturated fatty acids of 16 or more carbon atoms) is at least 20% based on the total amount of triglycerides, preferably at least 25% . - 6. Seasoned composition according to claim 1-5, characterized in that the amount of H2U (triglyceride of 2 saturated fatty acids of 16 or more carbon atoms and 1 cis-unsaturated fatty acid) taken together is at least 30% by weight based on the total amount of triglycerides. 7. Seasoned composition according to claim 1-6, characterized in that the ratio of H3 / H2U is between 0.5 and 1.2. 8. Seasoned composition according to claim 1-7, characterized in that the amount of palmitic fatty acid (C16: 0) based on the total amount of fatty acids is between 25 and 50% by weight. 9. Seasoned composition according to claim 1-8, characterized in that it comprises 25-100% of a mixture of interesterified fats of 40-80% PO (palm oil) and 20-60% of a fully hardened rapeseed fat. with a melting point of 68 ° C (RP68) and / or a fully hardened soybean oil with a melting point of 65 ° C (BO 65) and / or sunflower (oil or fully hardened). 10. Seasoned composition according to claim 1-9, characterized in that the composition further comprises 0.1-50% by weight of starch and / or flour and / or maltodextrin. 11. Seasoned composition according to claim 1-10, characterized in that the composition further comprises 0.1-50% by weight of powdered fine herbs and / or spices and / or tomato powder and / or monosodium glutamate. 12. Seasoned composition according to claim 1-11, characterized in that a soup or sauce concentrate is formed, which produces a soup or sauce upon mixing and heating with an aqueous liquid.