4481195 method for the treatment of tumors with beta-glucuronidase activity dependent...

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114 PATENT ABSTRACTS 4481189 Nonapeptide and decapeptide analogs of LHRH which have the formula See Patent for PROCESS FOR PREPARING Chemical Structure (I) and the pharmaceutically STERILIZED PLASMA AND acceptable salts thereof. PLASMA DERIVATIVES 4481195 Alfred M Prince assigned to New York Blood Center Inc A mammalian blood plasma or plasma deriva- tive substantially free of active hepatitis B or non-A, non-B viruses is disclosed, the plasma being characterized by the presence of factor VIII, the percent by weight of denatured factor VII1 to the sum of undenatured factor VIII and denatured factor VIII being less than 50%. The plasma is sterilized by contact with a detergent, alcohol or ether, preferably a mixture of deter- gent and ether, usually followed by removal of the viral sterilizing agent. 4481190 NONAPEPTIDE AND DECAPEPTIDE ANALOGS OF LHRH USEFUL AS LHRH ANTAGONISTS John Nestor, Brian H Vickery assigned to Syntex (U S A ) Inc A--B--C--D--E~ F--G--Arg--Pro--H (1) I 2 3 4 5 6 7 8 9 10 (ll) H2N--CH--CO2H ~CFt2)~ I NH I R~--C~NR2 I I I I /C~N. tC~ tC-~ HN/'C~N N N HN N HN N \ / ~ ~ A--C--(CH2)nA[ X X H2N--~H--COzH ?5 RQ (IVl (V) NH~ ) - ~ CH2CO2H R9 METHOD FOR THE TREATMENT OF TUMORS WITH BETA- GLUCURONIDASE ACTIVITY DEPENDENT PHARMACEUTICALS David Rubin, Jerusalem, Israel assigned to Schwimmer Adolf; Schwartz Irwin S; Rubin David; Century Science Co Hyperacidified tumors having high beta- glucuronidase activity can be treated with glucuronides with aglycones toxic to the tumor cells with great safety toward the rest of the body by first administering an alkalinizing agent in an amount sufficient to maintain the pH level of non-tumor tissues at approximately 7.4 during the glucuronide treatment. This will cause in- activation of beta-glucuronidase activity in the rest of the body. When nitrile-containing agly- cones are used sodium thiosulfate is also administered to avoid cyanide poisoning. A loading dose of glucaronide greater than 2 mMoles per kilogram body weight is first ad- ministered with additional administration of one third the initial dose each hour as long as beta- glucuronidase activity remains at the tumor site. Bacterial cells having beta-glucuronidase ac- tivity may also be diagnosed and treated in ac- cordance with the present invention. 4481197 ANTI-INFLAMMATORY DEOXYRIBOSIDES Janet L Rideout, Thomas Krenitsky assigned to Burroughs Wellcome Co NH2 N HO--CH 2 OH H The novel compounds 3-deaza-2'- deoxyadenosine and certain of its derivatives and their pharmaceutically acceptable salts have anti-inflammatory activity as well as immune response suppression activity. 3-Deaza-2"-

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114 PATENT ABSTRACTS

4481189 Nonapeptide and decapeptide analogs of LHRH which have the formula See Patent for

P R O C E S S F O R P R E P A R I N G Chemical Structure (I) and the pharmaceutically S T E R I L I Z E D P L A S M A A N D acceptable salts thereof.

P L A S M A D E R I V A T I V E S

4481195 Alfred M Prince assigned to New York Blood Center Inc

A mammalian blood plasma or plasma deriva- tive substantially free of active hepatitis B or non-A, non-B viruses is disclosed, the plasma being characterized by the presence of factor VIII, the percent by weight of denatured factor VII1 to the sum of undenatured factor VIII and denatured factor VIII being less than 50%. The plasma is sterilized by contact with a detergent, alcohol or ether, preferably a mixture of deter- gent and ether, usually followed by removal of the viral sterilizing agent.

4481190

N O N A P E P T I D E A N D D E C A P E P T I D E A N A L O G S O F

L H R H U S E F U L AS L H R H A N T A G O N I S T S

John Nestor, Brian H Vickery assigned to Syntex (U S A ) Inc

A--B--C--D--E~ F--G--Arg--Pro--H (1) I 2 3 4 5 6 7 8 9 10

(ll) H2N--CH--CO2H

~CFt2)~ I NH I

R~--C~NR2

I I I I /C~N. t C ~ t C - ~ H N / ' C ~ N N N HN N HN N

\ / ~ ~ A--C--(CH2)nA[

X X

H2N--~H--COzH

?5 RQ

(IVl

(V) NH~ ) -

~ CH2CO2H

R9

M E T H O D F O R T H E T R E A T M E N T O F T U M O R S W I T H BETA-

G L U C U R O N I D A S E A C T I V I T Y D E P E N D E N T

P H A R M A C E U T I C A L S

David Rubin, Jerusalem, Israel assigned to Schwimmer Adolf; Schwartz Irwin S; Rubin David; Century Science Co

Hyperacidified tumors having high beta- glucuronidase activity can be treated with glucuronides with aglycones toxic to the tumor cells with great safety toward the rest of the body by first administering an alkalinizing agent in an amount sufficient to maintain the pH level of non-tumor tissues at approximately 7.4 during the glucuronide treatment. This will cause in- activation of beta-glucuronidase activity in the rest of the body. When nitrile-containing agly- cones are used sodium thiosulfate is also administered to avoid cyanide poisoning. A loading dose of glucaronide greater than 2 mMoles per kilogram body weight is first ad- ministered with additional administration of one third the initial dose each hour as long as beta- glucuronidase activity remains at the tumor site. Bacterial cells having beta-glucuronidase ac- tivity may also be diagnosed and treated in ac- cordance with the present invention.

4 4 8 1 1 9 7

A N T I - I N F L A M M A T O R Y D E O X Y R I B O S I D E S

Janet L Rideout, Thomas Krenitsky assigned to Burroughs Wellcome Co

NH2

N HO--CH 2

OH H

The novel compounds 3-deaza-2'- deoxyadenosine and certain of its derivatives and their pharmaceutically acceptable salts have anti-inflammatory activity as well as immune response suppression activity. 3-Deaza-2"-