Appeal No. 1996-1009
Application No. 07/949,551
Naggi ‘063 describes reacting a heparin of natural origin with a sulfuric acid/chlorosulfonic acid
mixture to produce depolymerized and supersulfated heparin products having molecular weights
between 2000 and 9000, with good fibrinolytic and hypolipemic activity joined to a weak anticoagulant
activity (col. 4, line 67 - col. 5, line 2; col. 5, lines 41-45), and which are useful for prevention of
thrombolytic diseases and treatment of atherosclerosis (col. 10, lines 58-66). Naggi ‘063 explicitly
describes at least the relative molecular weights and degree of sulfation (a measure of sulfur content)
between various starting heparin materials and their resulting product(s) and, in some cases, results of
activated partial thromboplastin time (APTT), activity towards blood coagulation factor Xa (anti-Xa
activity), and the ratio anti-Xa/APTT. A summary of this data follows, with calculated APTT/anti-Xa
ratios where data was available.
mol. weight degree of APTT anti-Xa anti-Xa/ (calc.) APTT/
sulfation activity APTT anti-Xa
starting heparin
D212 13,500 1.95 1.000 1.20 1.20 0.83
product AH-16 6,000 3.0 0.06 0.18 3.0 0.33
product AH-19 6,000 3.0 0.05 0.22 4.4 0.23
product AH-104 6,000 2.9 0.078 0.30 3.84 0.26
product AH-103 6,000 2.8
product AH-105 6,000 3.0
product AH-106 6,000 2.8 0.080 0.31 3.87 0.26
product AH-107 6,000 3.0
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