Classifications

• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
  • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
  • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
  • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
  • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
  • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom

Definitions

• This invention relates to the improving of microcirculation and to the treatment of senility, and more partiularly to oral treatments to treat microcirculation and senility, according to which invention a beta-(2-pyridyllower alyl)-amine is administered in order to achieve these results.
• the microcirculatory or microvascular system is generally described as consisting of all vessels with an internal diameter of 100 microns or less. It is possible by microscopy, but not by the naked eye, to see the characteristics of capillary circulation or microcirculation. The tiny vessels through which microcirculation takes place are really only endothelial tubes with no powers of contraction.
• microv-ascular system accounts for the failure of tissue or organ function in a variety of common clinical conditions.
• the microcirculation may be comprised by either arterial occlusions or venous occlusions. In both cases the capillary network immediately ahead or behind the plug will be blocked. Vast numbers of capillary vessels may be obstructed to involve almost an entire organ, and yet central or large vessel flow may give no indication of this.
• impaired microcirculation is to a great extent mediated by histamine.
• Induced histamine is believed to be newly synthesized in free, pharmacologically active form, in or near the vascular endothelial cells.
• histamine can only be administered by injection, and in addition, the dosages of histamine must be very carefully regulated because overdosages of histamine are highly toxic and may be fatal.
• the present invention mainly comprises a method of improving impaired microcirculation by administration of a compound selected from the group consisting of )8-(2-pyridyl lower alkyl)-amines, B-(4-pyridyl lower alkyl)-amines and nontoxic acid addition salts thereof.
• the administration of the 8-(2- or 4-pyridyl lower alkyl)-amines, or their non-toxic acid addition salts is preferably effected orally using a rnicrocirculation-improving effective amount thereof.
• the lower alkyl portion of the pyridyl alkyl amines of the invention may be any alkyl of up to 5 carbon atoms.
• the most preferred alkyl groups are methyl and ethyl.
• the most preferred compounds are B-(2-pyridyl)- ethyl methyl amine, fl-(4-pyridyl)-ethyl methyl amine, l-(2-pyridyl)2methyl amino propane, and non-toxic acid addition salts thereof such as the hydrochloride, the tartrate, the fumarate, the gluconate, etc.
• the 3-(2- or 4-pyridyl alkyl)-amines of the present invention may be administered in amounts as low as 0.5 mg. per day and as high as 4550 mg. per day to achieve the effects of the present invention.
• the compounds are preferably administered in an amount of about 4-45 mg, per day, more preferably in an amount of 12-45 mg. per day, and most preferably in a unit dose of about 4-15 mg. administered three times a day.
• the same can be administered either orally or by injection, the preferred administration route being by oral administration.
• the 5-(2- or 4-pyridyl alkyl)-amines of the invention are preferably administered in the form of a non-toxic acid addition salt thereof, and most preferably in the form of the hydrochloride.
• Example 1 Tablets are prepared by usual tabletting procedure, each tablet containing:
• the above tablet can be administered in all conditions requiring improved microcirculation. Administration of the above tablet has been found to be effective in the treatment of senility.
• Example 2 Tablets are prepared by usual tabletting procedure, each tablet containing:
• the above tablet is highly effective in improving impaired microcirculation and in thetreatment of senility.
• Example 3 Ampoules are prepared each containing 10 cc. and each cc. consisting of mg. 1-(2-pyridyl)-2-methyl amino propane hydrochloride dissolved in 0.9% sodium chloride solution. This solution can be administered parenterally to improve impaired microcirculation, and also in the treatment of senility It is believed that from the foregoing, adaptations and variations of the invention can be made without departing from the spirit or scope of the invention. Such adaptations and variations are of course intended to be comprehended within the meaning and scope of equivalents of the present invention.
• Method of improving impaired microcirculation which comprises administering to a subject requiring the same a microcirculation-improving effective amount of at least one member selected from the group consisting of BQ-pyridyl-lower alkyl)-amine, fi-(4-pyridyl-1ower alkyl)-amine and non-toxic acid addition salts thereof.
• Method of improving impaired microcirculation which comprises orally administering to a subject requiring the same a microcirculation-improving effective amount of at least one member selected from the group consisting of B (2 pyridyl lower alkyl) amine, 5-(4- pyridyl-lower alkyl)-amine and non-toxic acid addition salts thereof.
• Method of improving impaired micro-circulation which comprises administering to a subject requiring the same at least one member selected from the group consisting of ,B-(Z-pyridyl-lower alkyl)-amine, [3-(4-pyridyllower alkyl)-amine and non-toxic acid addition salts thereof in an amount of about 0.5-45 mg. per day.
• Method of improving impaired micro-circulation which comprises orally administering to a subject requiring the same at least one member selected from the group consisting of B-(Z-pyridyl-lower alkyl)-amine, p-(4-pyridyl-lower alkyl)-amine and non-toxic acid addition salts thereof in an amount of about 0.5- mg. per day.
• Method of treating senility which comprises administering to a senile patient an effective amount of at least one member selected from the group consisting of fl-(2-pyridyl-1ower alkyl)-amine, B-(4-pyridyl-lower alkyl)- amine and non-toxic acid addition salts thereof.
• Method of treating senility which comprises administering to a senile patient by oral administration an effective amount of at least one number selected from the group consisting of ,B-(Z-pyridyl-lower alkyl)-amine, B-(4-pyridyl-lower alkyl)-amine and non-toxic acid addition salts thereof.
• Method of treating senility which comprises administering to a patient at least one member selected from the group consisting of B-(Z-pyridyl-lower aIkyD-amine, p-(4-pyridyl-lower alkyl)-amine and non-toxic acid addition salts thereof in an amount of about 05-45 mg. per day.
• Method of treating senility which comprises orally administering to a patient at least one member selected from the group consisting of ,B-(Z-pyridyl-lower alkyl)- amine, fl-(4pyridyl-lower alkyl)-amine and non-toxic acid addition salts thereof in an amount of about 0.5-45 mg. per day.

Landscapes

• Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Pyridine Compounds (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (1)

Publications (1)

Family

ID=23931119

Family Applications (1)

Country Status (7)

Citations (2)

• 1965
  • 1965-09-09 US US486237A patent/US3439096A/en not_active Expired - Lifetime
• 1966
  • 1966-08-02 IL IL26259A patent/IL26259A/xx unknown
  • 1966-08-03 GB GB34822/66A patent/GB1140540A/en not_active Expired
  • 1966-08-19 FR FR73628A patent/FR6333M/fr not_active Expired
  • 1966-08-30 BE BE686194D patent/BE686194A/xx unknown
  • 1966-09-09 NL NL6612711A patent/NL6612711A/xx unknown
  • 1966-09-09 ES ES0331392A patent/ES331392A1/es not_active Expired

Patent Citations (2)

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