Beef insulin preparations
    3.
    发明授权
    Beef insulin preparations 失效
    贝类胰岛素制剂

    公开(公告)号:US3657425A

    公开(公告)日:1972-04-18

    申请号:US3657425D

    申请日:1969-03-12

    IPC分类号: A61K38/28 A61K17/02

    CPC分类号: A61K38/28

    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.

    Insulin product
    6.
    发明授权
    Insulin product 失效
    胰岛素产品

    公开(公告)号:US3758683A

    公开(公告)日:1973-09-11

    申请号:US3758683D

    申请日:1971-04-30

    申请人: JACKSON R

    发明人: JACKSON R

    IPC分类号: A61K38/28 A61K17/02

    CPC分类号: A61K38/28

    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.

    {60 -Methyl glutathione, analogs thereof, intermediates therefore and processes for their preparation
    8.
    发明授权
    {60 -Methyl glutathione, analogs thereof, intermediates therefore and processes for their preparation 失效
    因此,{60-甲基谷胱甘肽,其类似物,中间体及其制备方法

    公开(公告)号:US3882097A

    公开(公告)日:1975-05-06

    申请号:US25213972

    申请日:1972-05-10

    申请人: MERCK & CO INC

    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.

    摘要翻译: 本公开描述了通过N-苄氧羰基-α-甲基谷氨酸或天冬氨酸酐与S-苄基 - 半胱氨酰甘氨酸在约0℃的温度下反应制备α-甲基谷胱甘肽及其天冬氨酰基类似物,并且pH为 约11.然后通过用液氨中的钠还原来除去保护基团。 还描述了通过用乙酸酐或二环己基碳二亚胺脱水取代的酸来制备N-苄氧羰基-α-甲基谷氨酸和天冬氨酸酐。

    Protamine-insulin product
    9.
    发明授权
    Protamine-insulin product 失效
    鱼精蛋白 - 胰岛素产品

    公开(公告)号:US3868358A

    公开(公告)日:1975-02-25

    申请号:US33751173

    申请日:1973-03-02

    申请人: LILLY CO ELI

    发明人: JACKSON RICHARD L

    IPC分类号: C07C103/52 A61K17/02 C07G7/00

    CPC分类号: A61K38/28

    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.

    摘要翻译: 本发明涉及鱼精蛋白与胰岛素盐的组合。 胰岛素盐通过在碱性pH范围内在碱金属或准金属例如钠,钾,锂,铯或铵的离子存在下结晶而得到。 鱼精蛋白以约0.2至约1.5mg的量存在。 每100个胰岛素的鱼精蛋白。 胰岛素盐和鱼精蛋白在水性介质中在6.5至8的pH下形成不溶性络合物,当干燥时复合物容易重构而没有活性损失。

    (N{HU Al{b , N{HU Bl{b , N{HU B29{B , carbamoyl)-(O{HU A14{B , O{HU B16{B , O{HU B26{B aryl) insulin derivatives
    10.
    发明授权
    (N{HU Al{b , N{HU Bl{b , N{HU B29{B , carbamoyl)-(O{HU A14{B , O{HU B16{B , O{HU B26{B aryl) insulin derivatives 失效
    (N {HU Al {B,N {HU B 26 {B,N {HU B29 {B,氨基甲酰基) - (O {HU A14 {B,O {HU B16 {B,O

    公开(公告)号:US3864325A

    公开(公告)日:1975-02-04

    申请号:US30636972

    申请日:1972-11-13

    申请人: NAT RES DEV

    CPC分类号: C07K14/62 A61K38/00

    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。