KR890006670A - Isopolypeptide and preparation method thereof - Google Patents

Abstract

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Description

Isopolypeptide and preparation method thereof

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Claims (14)

Compounds of the following general formula (I), salts, racemates and optical isomers thereof. [Wherein R ⁴ , R ⁵ , R ⁶ , R ⁷ and R ¹⁰ each represent a hydrogen atom or a C _1-4 alkyl group, R ⁸ and R ⁹ each represent a hydrogen atom and r is an integer of 10 to 400; , m is 0, 1, 2 or 3 and n is 0.] Wherein R ⁴ , R ⁵ , R ⁶ , R ⁷ and R ¹⁰ are each hydrogen atoms, r has a value from 10 to 400, m is 0,1,2 or 3, and n is 0. Compounds of I) and salts, racemates and optical isomers thereof. Polyisorisin having an average molecular weight of 5500 to 25,600. Polyisoornithine with an average molecular weight of 4400 to 13,500. In the formula, which is an active ingredient, R ⁴ , R ⁵ , R ⁶ , R ⁷ , R ⁸ , R ⁹ and R ¹⁰ represent hydrogen, r is an integer from 40 to 200, m is 0,1,2 or 3 and n is A weak formulation having an antitumor and antiviral effect, characterized by containing a compound of formula (I) wherein 0 and the amino group has an L-configuration in admixture with a carrier and / or additives commonly used in the pharmaceutical industry. The pharmaceutical formulation according to claim 5, wherein the active ingredient is polyisorisin having an average MW of 5500 to 22,500. After coupling the monomer or oligomer of the following general formula (II) with the monomer of the following general formula (III) and removing the R ² protecting group from the obtained compound of the general formula (IV), s In the case of 9, the obtained compound is reacted with a monomer of general formula (III) or polycondensed by a known method, and if necessary, converted into a salt when the obtained compound of general formula (I) is in free base form Or, in the case of salts, polyisodiaminocarboxylic acids of the general formula (I), their salts, racemates and optical isomers, characterized in that they are converted to bases or other salts. [Wherein, R ⁴ , R ⁵ , R ⁶ , R ⁷ , R ⁸ , R ⁹ and R ¹⁰ may be the same or different and represent a hydrogen atom or a C _1-4 alkyl group, r is an integer from 10 to 400, m is an integer from 0 to 10, n is an integer from 0 to 10, q is an integer from 1 to 9, R ¹ is an amino protecting group and in the oligomer all R ¹ are the same, R ³ is protected and concurrent activation Is an active ester protecting group of a carboxyl group, R ² is an amino protecting group different from R ¹ and can be selectively removed irrespective of R ¹ , X is a carboxyl-activating group, provided that -COX is more reactive than COOR ³ Is large and s is an integer from 2 to 10, and when the general formula (II) is an oligomer, the substituents may be the same or different.] 8. A compound according to claim 7, wherein R ¹ , R ³ , R ⁴ , R ⁵ , R ⁶ , R ⁷ , R ¹⁰ and q are the same as defined in claim 1 and m and n are the same as defined above. The monomer or oligomer of II) is a general formula wherein R ¹ , R ² , R ⁴ , R ⁵ , R ⁶ , R ⁷ , R ¹⁰ and X are as defined in claim 1 and m and n are as defined above. React with the monomer of (III) and remove the R ² protecting group from the obtained compound of formula (IV), wherein the substituents in the formula are as defined above and the value of s is as defined in claim 7, 9, R ⁴ , R ⁵ , R ⁶ , R ⁷ , R ¹⁰ and r in the formula characterized in that the obtained product is reacted with the monomer of general formula (III) or The same method as defined in the above, wherein m is 3 and n is 0. A method for preparing polyisodiamino carboxylic acid and salt thereof. 8. A compound according to claim 7, wherein R ¹ , R ³ , R ⁴ , R ⁵ , R ⁶ , R ⁷ , R ¹⁰ and q are the same as defined in claim 1 and m and n are the same as defined above. The monomer or oligomer of II) is a general formula wherein R ¹ , R ² , R ⁴ , R ⁵ , R ⁶ , R ⁷ , R ¹⁰ and X are as defined in claim 1 and m and n are as defined above. React with the monomer of (III) and remove the R ² protecting group from the obtained compound of formula (IV), wherein the substituents are as defined above and s is as defined in claim 7, In the case of 9, R ¹ , R ³ , R ⁴ , R ⁵ , R ⁶ , R ⁷ , R ¹⁰ and q in the formula for reacting the obtained product with the compound of general formula (III) or A method for producing a polyisodiamino carboxylic acid and salts thereof of the general formula (I), which is the same as defined in claim 1 and m and n are the same as defined above. 8. The starting material according to claim 7, wherein N ^α -ZN ^ε -BOC-L-lysine is converted to mixed anhydride using N ^α -ZL-lysine-p-nitrophenylester hydrochloride and isobutylchloroformate. Method for producing polyiso-L-lysine and salts thereof, characterized in that the use. 8. The method of claim 7, starting N ^α -ZN ^β -BOC-L-ornithine converted to mixed anhydride using N ^α -ZL-ornithine-p-nitrophenylester hydrochloride and isobutylchloroformate. A method for preparing polyiso-L-ornithine and its salts, which is used as a substance. 8. The starting material according to claim 7, wherein N ^α -ZN ^ε -BOC-D-lysine is converted to mixed anhydride using N ^α -ZD-lysine-p-nitrophenylester hydrochloride and isobutylchloroformate. Method for producing polyiso-D-lysine and salts thereof, characterized in that the use. 8. Starting N ^α -ZN ^β -BOC-D-ornithine converted to mixed anhydride using N ^α -ZD-ornithine-p-nitrophenylester hydrochloride and isobutylchloroformate Method for preparing polyiso-D-ornithine and its salts, characterized in that used as a substance. A method for treating cancer in an animal, comprising using an effective amount of a pharmaceutical product containing the compound of claim 1 as an active ingredient. ※ Note: The disclosure is based on the initial application.