Cypros Pharmaceutical Corp.

Brian W Sullivan

Paul J Marangos

Lewis R Makings

Anthony W Fox

Torsten Wiemann

Anne M Danks

Marina Sragovicz

Neuroprotective drugs are disclosed with at least 3 branches extending outwardly from a center atom or group, each branch having a guanidino group at its terminus. All branches preferably should be identical, and distributed around the center atom or group in a radial manner. Three branches can be bonded to a nitrogen atom, or four branches can be coupled to a carbon atom; other center groups include stable aromatic, cycloalkyl, heterocyclic, or bicyclic structures. Starting reagents are disclosed with a center atom or group, and with reactive groups (such as primary amines or hydroxyl groups) at the ends of short 'spacer chains' bonded to the center atom or group. Reagents derived from arginine (an amino acid having a terminal guanidino group) can be bonded to these center components, using protective groups on the arginyl reagents to ensure desired final products with accessible guanidino groups at the ends of spacer chains. Alternately, guanylating agents can be used to directly convert primary amine groups at the ends of spacer chains, on starting reagents, into guanidino groups. These drugs can be injected intravenously into patients suffering from ischemic or hypoxic crises (stroke, cardiac arrest, loss of blood, suffocation, etc.), and can penetrate the blood-brain barrier and suppress the entry of calcium into CNS neurons via N-type and P/Q-type calcium channels, thereby reducing excitotoxic damage in the CNS. These drugs are also useful for suppressing other types of unwanted excessive neuronal activation, such as neuropathic pain.

Neuroprotective poly-guanidino compounds which block presynaptic N and

A method and device are disclosed which enable on-site pre-diagnostic emergency treatment of people suffering from life-threatening injuries (such as victims of auto accidents, shootings, stabbings, and near-drownings), or from a collapse or loss of consciousness that might be due to a heart attack, stroke, cardiac arrest, internal hemorrhage, or various other causes that cannot be diagnosed until after a physician or ambulance has arrived on the scene. This on-site pre-diagnostic emergency treatment involves intravenous injection of fructose-1,6-diphosphate (FDP, a naturally-occurring chemical which functions as an intermediate in glycolysis) into the patient. Such injections can be administered by police, firemen, military personnel, lifeguards, nursing home attendants, ambulance attendants, or anyone else who has been trained to administer intravenous injections. The FDP should be injected into the patient as soon as possible, without delaying until the patient can be diagnosed and treated by a doctor. When administered immediately, intravenously injected FDP can reduce ischemic or hypoxic damage to the internal organs, without having any adverse effects or posing any significant risks for patients who may not need it. Injection kits which include vials containing partially lyophilized FDP (which does not require refrigeration), sterile water for reconstitution of the freeze-dried FDP, and a syringe with hypodermic needles are also disclosed, in a hard-shell case that can withstand rough handling, as might occur in a police car or firetruck.

On-site emergency treatment of injured or unconscious patients, using

A method is disclosed for preparing a partially lyophilized (freeze-dried) powder or solidified cake containing fructose-1,6-diphosphate (FDP), a naturally-occurring intermediate in glycolysis. Preferably, about 10% to 25% residual water (by weight) is left in the powder or cake. This high moisture content does not degrade or limit FDP's stability or shelf life, and it provides for faster, less expensive processing. The methods disclosed herein also allow direct lyophilization inside a vial or other sealed container that will hold the lyophilized FDP, to avoid any need for milling, handling, or other treatment under conditions that might endanger its sterility. Lyophilized FDP can be used to create emergency injection kits which also contain aqueous solutions for mixing, and syringes and needles for injection. These kits can be carried in ambulances, police cars, firetrucks, etc., and can be stored at nursing homes, swimming pools, and in the homes of people suffering from various conditions such as heart disease or sicle cell anemia. These kits will allow rapid (even pre-diagnostic) injection of FDP into people suffering medical crises such as heart attacks, severe blood loss, suffocation, etc.

Growing community of inventors

Escondido, CA, United States of America

Brian W Sullivan