摘要:
N (A1), N (B29)-di-tert. butyloxycarbonyl insulin, useful as a hypoglycemic agent. A method for its preparation by reacting insulin, in a mixture of an N,N''-dialkylcarboxylic acid amide having a total of from three to six carbon atoms and an aqueous buffer solution having a pH between 8.0 and 9.0, with a 20 to 75 fold molar excess of tert. butyloxycarbonyl azide at 20* to 50*C.
摘要:
A STABLE AND PHARMACEUTICALLY ACCEPTABLE SOLUTION OF INSULIN, COMPRISING BEEF INSULIN WHICH HAS A MOLECULAR WEIGHT OF 5734, SUBSTANTIALLY THE FOLLOWING ELEMENTARY ANALYSIS: CARBON 53.21%, HYDROGEN 6.63%, NITROGEN 15.88%, SULPHUR 3.36%, AND OXYGEN 20.92% (BY DIFFERENCE), AND CHARACTERISTICALLY ALANINE, SERINE, AND VALINE IN THE 8TH, 9TH AND 10TH POSITION OF THE A CHAIN AND ALANINE IN THE 30TH POSITION OF THE B CHAIN, AND HAS (1) A PROTAMINASE CONTENT CAUSING LESS THAN ABOUT 15% W./W. LOSS AT 37*C. IN 30 DAYS WHEN THE INSULIN IS CONVERTED INTO A PROTAMINE-CONTAINING ISOPHANE INSULIN SUSPENSION, (2) AN OPTICAL DENSITY (ABSORBENCE), CORRECTED TO A MANIFOLD DILUTED SAMPLE, OR LESS THAN ABOUT 0.5 AS A 1% ACID SOLUTION IN A 4 CM. CELL AT A WAVELENGTH OF 396 MU, (3) AN OPTICAL DENSITY (ABSORBENCE) OF LESS THAN ABOUT 0.03 AT A WAVELENGTH OF 400 MU WHEN MEASURED AS A 40 INTERNATIONAL UNITS/ML. SOLUTION IN A 1 CM. CELL AT A PH OF 7.4 AFTER STANDING AT 5*C. FOR EIGHT DAYS, WITH AN INSTRUMENT ADAPTED TO EXCLUDE SCATTERED LIGHT, AND, (4) AN INFRA-RED SPECTRUM SUCH AS SHOWN IN THE DRAWING; AS AN AQUEOUS SOLUTION, ADJUSTED TO A PH BETWEEN PH7 AND 8.
摘要:
A new simple protein, described in a copending application, is useful in treating several disease states by enhancing metabolism functions. The protein facilitates glucose uptake in muscle as well as glycogen deposition, leading to utility in the treatment of uremia and shock in animals.
摘要:
1. AN ACIDIC MONOSCCHARIDE-SUBSITUTED PROTEIN SELECTED FROM THE GROUP CONSISTING OF N-ACETYLNEURAMINYL INSULIN (BOVINE), N-ACETYLNEURAMINYL INSULIN (PIRCINE), N-ACETYLNEURAMINYL HUMAN SERUM ALBUMIN, N-ACETYLNEURAMINYL BOVINE SERUM ALBUMIN, N-ACETYLNEURAMINYL HUMAN GROWTH HOMONE, GLUCONYL INSULIN (BOVINE), GLUCONYL INSULIN (PORICE), GLUCONYL HUMAN SERUM ALBUMIN, AND GLUCONYL HUMAN GROWTH HORMONE WHEREIN THE SUBSTITUTION OCCURS AT AN AVALIBLE A-AMINO OR $AMINO GROUP.
摘要:
The invention relates to a combination of protamine with an insulin salt. The insulin salt is derived by crystallization of insulin in the presence of ions of an alkali metal or metalloid such as sodium, potassium, lithium, cesium or ammonium at an alkaline pH range. The protamine is present in an amount from about 0.2 to about 1.5 mg. of protamine for each 100 units of insulin. The insulin salt and protamine form an insoluble complex at a pH from 6.5 to 8 in an aqueous medium, which complex when dried is easily reconstituted without activity loss.
摘要:
This disclosure describes the preparation of Alpha -methyl glutathione and its aspartyl analog by the reaction of Ncarbobenzoxy- Alpha -methyl glutamic or aspartic acid anhydrides with S-benzyl-cysteinyl glycine at a temperature of about 0*C. and a pH of about 11. The protecting groups are subsequently removed by reduction with sodium in liquid ammonia. The preparation of N-carbobenzoxy- Alpha -methyl glutamic and aspartic acid anhydrides by dehydration of the substituted acids with acetic anhydride or dicyclohexylcarbodiimide is also described.
摘要:
The invention relates to a combination of protamine with an insulin salt. The insulin salt is derived by crystallization of insulin in the presence of ions of an alkali metal or metalloid such as sodium, potassium, lithium, cesium or ammonium at an alkaline pH range. The protamine is present in an amount from about 0.2 to about 1.5 mg. of protamine for each 100 units of insulin. The insulin salt and protamine form an insoluble complex at a pH from 6.5 to 8 in an aqueous medium, which complex when dried is easily reconstituted without activity loss.
摘要:
Insulin derivatives which have an improved profile of hypoglycaemic activity, or which are intermediates for the production of such derivatives, are those in which at least one of the A1(glycine, B1(phenylalanine) and B29 (lysine) amino acid units is blocked by a carbamyl group or a substituted carbamyl group R1R2NCO- wherein R1 and R2 can be hydrogen, alkyl, aryl or other radicals. Masking of the initial activity is achieved by blocking tryosine hydroxyl groups with substituents which are releasable in vivo. N, N'', N''''- tricarbamyl and -triethylcarbamyl insulin, and Osubstituted derivatives thereof are typical compounds of the invention.
摘要翻译:具有改善的降血糖活性概况或作为制备这种衍生物的中间体的胰岛素衍生物是其中A1(甘氨酸,B1(苯丙氨酸)和B29(赖氨酸)氨基酸单元)中的至少一种被 氨基甲酰基或取代的氨基甲酰基R 1 R 2 NCO-,其中R 1和R 2可以是氢,烷基,芳基或其它基团。