Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/19—Carboxylic acids, e.g. valproic acid
  • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
• • H—ELECTRICITY
  • H01—ELECTRIC ELEMENTS
  • H01R—ELECTRICALLY-CONDUCTIVE CONNECTIONS; STRUCTURAL ASSOCIATIONS OF A PLURALITY OF MUTUALLY-INSULATED ELECTRICAL CONNECTING ELEMENTS; COUPLING DEVICES; CURRENT COLLECTORS
  • H01R4/00—Electrically-conductive connections between two or more conductive members in direct contact, i.e. touching one another; Means for effecting or maintaining such contact; Electrically-conductive connections having two or more spaced connecting locations for conductors and using contact members penetrating insulation
  • H01R4/28—Clamped connections, spring connections
• • H—ELECTRICITY
  • H01—ELECTRIC ELEMENTS
  • H01R—ELECTRICALLY-CONDUCTIVE CONNECTIONS; STRUCTURAL ASSOCIATIONS OF A PLURALITY OF MUTUALLY-INSULATED ELECTRICAL CONNECTING ELEMENTS; COUPLING DEVICES; CURRENT COLLECTORS
  • H01R13/00—Details of coupling devices of the kinds covered by groups H01R12/70 or H01R24/00 - H01R33/00
  • H01R13/58—Means for relieving strain on wire connection, e.g. cord grip, for avoiding loosening of connections between wires and terminals within a coupling device terminating a cable
  • H01R13/582—Means for relieving strain on wire connection, e.g. cord grip, for avoiding loosening of connections between wires and terminals within a coupling device terminating a cable the cable being clamped between assembled parts of the housing

Definitions

• This invention relates to new anti-fibrinolytic compounds and to a method of counteracting certain hemorrhagic conditions and other disorders resulting from a pathological fibrinolytic state in patients. More specifically, this invention relates to the new compound, 4- aminomethylcubane-1-carboxylic acid having the structure:
• This compound is useful in the prevention or treatment of a pathological fibrinolytic state in mammals including persons and animals by the oral administration of from 1 to 20 and preferably 2 to 8 mg./kg. of body weight per day of the above compound for varying periods of treatment.
• fibrinolytic activity results from an over abundance of such activators.
• plasmin fibrinolysin
• activators in the blood and it would appear that excessive fibrinolytic activity results from an over abundance of such activators.
• fibrinolytic state When too much plasmin is present, the clotting system of the blood becomes unbalanced, viable clots cannot be maintained, and hemorrhage may result. This situation is known as a fibrinolytic state.
• Other enzyme systems i.e., the kallikreins, complement
• anti-fibrinolytic agents i.e. drugs which will inhibit the activation of plasminogen to form plasmin.
• anti-fibrinolytic agents are believed to interfere with the function of the activators of converting plasminogen to plasmin.
• Patented June 23, 1970 clinical uses of such drugs include their administration to persons undergoing various kinds of surgery (such as heart-lung and prostate surgery), obstetrical hemorrhage problems, menorrhagia, and many other uses which have bene suggested in the literature (e.g. see Nilssen, Acta Medica Scand. Suppl. 448, volume 180 (1966).
• EACA epsilon amino caproic acid
• AMCHA trans-4-aminomethylcyclohexane carboxylic acid
• PAMBA 4-aminomethylbenzoic acid
• the compound of this invention is prepared by starting with the known compound dimethyl cubane-l,4-dicarboxylate, also named dimethyl pentacyclo [4.2.0.0. 0. 0. octane-1,4-dicarboxylate. It was prepared essentially as described by P. E. Eaton et al. (J. Am. Chem. Soc' 86 962 (19 64). Infrared spectra, NMR data, melting point and elemental analysis compared favorably with reported values. The material was also found to be homogeneous by thin layer chromatography and vapor phase chromatography.
• the carboxylic ester derivatives of 6) may be prepared by direct esterification of the amino acid such as by the use of alcoholic hydrogen chloride or thionyl chloride followed by alcohol.
• the alkanoyl amino derivatives of (6) are prepared by acylation of the amino acids.
• the compound of this invention is used in the method of this invention by either oral or intravenous administration, although the oral route is preferred.
• the esters and amides of this class of compounds are not themselves very active in vitro but the action of enzymes in HZNCHZ vivo may cause the slow liberation of the highly active amino acids, thus providing a prolonged availability of References Cited the drug in the body. This is important because of the tendency of these drugs to be swiftly eliminated in the 10 phemlsuy of Olgamc Compounds 2nd urine.
• the compound of this invention can be used in any LORRAINE WEINBERGER Primary Examiner pharmaceutically acceptable carrier, in the form of pills, tablets or capsules.
• the pharmaceutically acceptable salts 15 KILLOS: Asslstant Exammer both of the amino group-such as the hydrochloride, hydrobromide, sulfate, citrate, tartrate, etc., and of the carboxy group-such as the alkali metal, alkaline earth 260-464, 468, 501.11; 424319 metal, etc., salts) are readily usable, especially in injectable compositions.

Landscapes

• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Applications Claiming Priority (1)

Publications (1)

Family

ID=24847126

Family Applications (1)

Country Status (7)

Cited By (5)

• 1968
  • 1968-02-28 US US708770A patent/US3517055A/en not_active Expired - Lifetime
• 1969
  • 1969-02-13 NL NL6902278A patent/NL6902278A/xx unknown
  • 1969-02-18 CH CH242469A patent/CH515887A/de not_active IP Right Cessation
  • 1969-02-21 FR FR6904490A patent/FR2002747A1/fr not_active Withdrawn
  • 1969-02-24 GB GB9740/69A patent/GB1203538A/en not_active Expired
  • 1969-02-26 BR BR206663/69A patent/BR6906663D0/pt unknown
  • 1969-02-26 DE DE19691909666 patent/DE1909666A1/de active Pending

Non-Patent Citations (1)

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