preparation containing stabilized physiologically active substance

1
ii New Patents is a mercury cation. The composition is espe- cially useful for removing radioactive iodine from liquid and gaseous waste streams, 4659517 HALOGEN LABELED COMPOUNDS INCLUDING ESTRADIOL DERIVATIVES, THEIR SYNTHETIC INTERMEDIATES AND THE SYNTHESES THEREOF Jay Spicer, William P Duncan, Gary A Rotert assigned to Bio-Medical Research Laboratories Inc A method of preparation of halogen labeled or- ganic compounds is described. In particular, estradiol derivatives labeled by halogen substitu- tion at C- 16 are synthesized according to the pre- sent invention. A triflate intermediate is prepared from which either 16-alpha-halo- substituted-17-beta-estradiols or 16-beta-halo- substituted- 17-beta-estradiols can be rapidly formed as desired. In particular, the preparation of 16-alpha-1231-17-beta-estradiol and 16-beta- 1231-l 7-beta-estradiol are shown and are syn- thesized from a 17-beta-estradiol- 16-beta- triflate. Both 16-alpha-1231- and 16-beta-1231- 17-beta-estradiol made according to the present invention are shown to have a high specific ac- tivity. The method of synthesis is sufficiently rapid so that the relatively short half-life of 1231 is readily accommodated. The high stereospecificity of each step of the reaction sequence in preparing the labeled estradiols pro- vides for highly efficient syntheses and little waste of radio-label. 4659570 PREPARATION CONTAINING STABILIZED PHYSIOLOGICALLY ACTIVE SUBSTANCE Yoshitake Terano, Ikeda, Japan assigned to Suntory Limited A preparation of stabilized physiologically ac- tive substance which is produced by in- corporating a physically and chemically modified gelatin in a physiologically active sub- stance made of basic protein or polypeptide, such as interferons, specially gamma-interferon. 4659678 IMMUNOASSAY OF , ANTIGENS Gordon Forrest, Philip R P Salacinski, Kenneth Siddle, Ingatestone, United Kingdom assigned to Serono Diagnostics Limited A method of immunoassay of an antigen in a li- quid sample wherein a complex is formed bet- ween antigen contained in the said sample and two or more antibody reagents, and the said complex is bound to a solid support by non- covalent bonding as defined herein; and the amount of complex becoming bound to the sup- port is determined; the process employing at least one monoclonal antibody reagent. Label- ling methods including radio-active, fluorimetric and enzyme labelling may be used to effect deter- mination of the binding of the complex to the solid support. The solid support may take the form of particles, beads, wall-coatings on the reaction vessel or an insert of large surface area. The method is particularly applicable to the as- say of TSH, CEA, HCG, alphafeto protein, immunoglobulins, viruses, allergens, bacteria, toxins, drugs and vitamins. Use of monoclonal reagents improves the specificity of the process, and also decreases non-specific binding. 4659733 METHOD FOR TREATING HYPERTENSION WITH 2,3- DIAMINO-1,4=BUTANEDITHIOL; 4, 5-DIAMINO-1,2=DITHIANE; AND N-ACYL AND N-ALKYL DERIVATIVES THEREOF Mark T DuPriest, Billie M York assigned to Al- con Laboratories Inc Disclosed are 2,3-diamino-1,4-butanedithiol; 4,5-diamino-1,2-dithiane; and their N-acyl and N-alkyl derivatives. Also disclosed are processes for preparing the disclosed compounds; pharma- ceutical compositions comprising such com- pounds; and a method of treatment comprising administering such compounds and composi- tions when an antihypertensive effect or radioprotective effect is indicated.

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ii New Patents

is a mercury cation. The composition is espe- cially useful for removing radioactive iodine from liquid and gaseous waste streams,

4659517

HALOGEN LABELED COMPOUNDS INCLUDING ESTRADIOL DERIVATIVES,

THEIR SYNTHETIC INTERMEDIATES AND THE

SYNTHESES THEREOF

Jay Spicer, William P Duncan, Gary A Rotert assigned to Bio-Medical Research Laboratories Inc

A method of preparation of halogen labeled or- ganic compounds is described. In particular, estradiol derivatives labeled by halogen substitu- tion at C- 16 are synthesized according to the pre- sent invention. A triflate intermediate is prepared from which either 16-alpha-halo- substituted-17-beta-estradiols or 16-beta-halo- substituted- 17-beta-estradiols can be rapidly formed as desired. In particular, the preparation of 16-alpha-1231-17-beta-estradiol and 16-beta- 1231-l 7-beta-estradiol are shown and are syn- thesized from a 17-beta-estradiol- 16-beta- triflate. Both 16-alpha-1231- and 16-beta-1231- 17-beta-estradiol made according to the present invention are shown to have a high specific ac- tivity. The method of synthesis is sufficiently rapid so that the relatively short half-life of 1231 is readily accommodated. The high stereospecificity of each step of the reaction sequence in preparing the labeled estradiols pro- vides for highly efficient syntheses and little waste of radio-label.

4659570

PREPARATION CONTAINING STABILIZED PHYSIOLOGICALLY

ACTIVE SUBSTANCE

Yoshitake Terano, Ikeda, Japan assigned to Suntory Limited

A preparation of stabilized physiologically ac- tive substance which is produced by in- corporating a physically and chemically modified gelatin in a physiologically active sub- stance made of basic protein or polypeptide, such as interferons, specially gamma-interferon.

4659678

IMMUNOASSAY OF , ANTIGENS

Gordon Forrest, Philip R P Salacinski, Kenneth Siddle, Ingatestone, United Kingdom assigned to Serono Diagnostics Limited

A method of immunoassay of an antigen in a li- quid sample wherein a complex is formed bet- ween antigen contained in the said sample and two or more antibody reagents, and the said complex is bound to a solid support by non- covalent bonding as defined herein; and the amount of complex becoming bound to the sup- port is determined; the process employing at least one monoclonal antibody reagent. Label- ling methods including radio-active, fluorimetric and enzyme labelling may be used to effect deter- mination of the binding of the complex to the solid support. The solid support may take the form of particles, beads, wall-coatings on the reaction vessel or an insert of large surface area. The method is particularly applicable to the as- say of TSH, CEA, HCG, alphafeto protein, immunoglobulins, viruses, allergens, bacteria, toxins, drugs and vitamins. Use of monoclonal reagents improves the specificity of the process, and also decreases non-specific binding.

4659733

METHOD FOR TREATING HYPERTENSION WITH 2,3-

DIAMINO-1,4=BUTANEDITHIOL; 4, 5-DIAMINO-1,2=DITHIANE; AND

N-ACYL AND N-ALKYL DERIVATIVES THEREOF

Mark T DuPriest, Billie M York assigned to Al- con Laboratories Inc

Disclosed are 2,3-diamino-1,4-butanedithiol; 4,5-diamino-1,2-dithiane; and their N-acyl and N-alkyl derivatives. Also disclosed are processes for preparing the disclosed compounds; pharma- ceutical compositions comprising such com- pounds; and a method of treatment comprising administering such compounds and composi- tions when an antihypertensive effect or radioprotective effect is indicated.