Classifications

• • C—CHEMISTRY; METALLURGY
  • C07—ORGANIC CHEMISTRY
  • C07D—HETEROCYCLIC COMPOUNDS
  • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
  • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
  • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
  • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
  • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system

Definitions

• the present invention relates to a novel benzothiazine derivative which has a platelet aggregation inhibitory action, a calcium antagonistic action and the like and is useful as a therapeutic agent for cardiovascular diseases.
• the present invention aims at finding a useful therapeutic agent for circulatory system diseases on the basis of conventional technology.
• the present invention relates to the general formula [I]
• R 1 represents a hydrogen atom, a lower aryl group, a halogen atom, a nitro group, a hydroxy group, a lower alkoxy group, or a lower alkoxy group;
• Oxy group, Amino group, lower grade It represents one or more groups selected from the group consisting of a rutile amino group and a lower alcohol group.
• R 2 represents a hydrogen atom, a lower alkyl group, or a (C 3 -C ⁇ ) cycloalkyl group
• R 3 is a hydrogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a halogen atom, a nitro group, or a lower alkyl region.
• Gishi group, lower alkoxy group, lower alkoxy group, amino group, lower aluminum group, lower alkoxy group This indicates one or more groups selected from the group consisting of a group and a lower alkoxycarbonyl group.
• R represents a hydrogen atom or a lower alkyl group.
• ⁇ and ⁇ are the same or different and represent lower alkylene groups having 1 to 6 carbon atoms. same as below . , A salt thereof, a method for producing the same, and a remedy for a circulatory system disease comprising these compounds as an active ingredient.
• lower alkyl groups are methyl, methyl, propyl, and hexyl groups.
• a halogen atom represents fluorine, chlorine, bromine and the like
• a lower alkoxy group represents a meth group: a silicon group, a petroleum group, or a hydroxy group.
• An alkoxy group having 16 carbon atoms, such as a sulfur group or a hexaglyoxy group, is referred to as a low-alkanol group.
• Alkaloids with 16 j ⁇ atoms, such as chloroxy, ⁇ -pionyloxy, hexanoyloxy, etc. Indicates a group, (C 3
• a cycloalkyl group is a cycloalkyl group having 36 carbon atoms, such as a cyclopropyl group or a cyclohexyl group.
• the lower alkylene group refers to a methyloxy group, an ethylene group, or the like. It indicates a group in which an alkylene group having 1 to 6 carbon atoms is present between each enzyme atom, and a lower alkinyl group is a base. It represents an alkoxyl group having 16 carbon atoms, such as a chillyl group, a brovonolyl group, and a hexanoyl group.
• the compound of the present invention can be produced, for example, by the following method.
• the reactions shown above are usually carried out under basic conditions.
• preferred bases include sodium hydrogenated, sodium carbonate, sodium carbonate, sodium hydroxide, Inorganic or organic bases such as sodium alcohol, triazine, viridine, ⁇ , ⁇ -dimethylaniline, etc. .
• the above reaction can also be carried out without using a base, by using an excess of amide components involved in the reaction.
• the derivative compound can be in the form of a salt that is acceptable as a medicinal product.
• salts include hydrochloride, sulfate, phosphate, lactate, maleate, fumarate, oxalate, methansulfonate, There are para-entrance sulfonates and the like.
• the invention compounds can be thrown in through the mouth or non- through the mouth.
• the dosage form include powders, capsules, granules, powders, suppositories, injections, and the like.
• the dosage depends on the symptoms, dosage form, etc., but it is usually 1 to 5 mg / day, preferably 10 to 1 mg / day, once or several times at OOO eg. Divide the potatoes into batches.
• the compound at the onset has platelet aggregation inhibitory action and calcium antagonism, and is useful for cardiovascular diseases such as hypertension, thrombosis and arrhythmia. * The effects of the compound are described below. As an example of a pharmacological test, a test example of calcium antagonism is shown.
• Invention Compound A (Hereinafter abbreviated to * Invention Compound A)) was used for the test.
• As a comparative compound it has a structure similar to that of the compound of the present invention, but does not have a phenyloxy group in the side chain, which is a feature of the present compound.
• Compound 3 4-Hydro 2-
• Example 2 The melting point and IR were the same as those in Example 1. The following compounds can be obtained in the same manner as in Example 2.
• Example 1 The procedure was the same as in Example 1 below. This gave 1.3 g (65%) of the title compound. Melting point and IR were in agreement with those in Example 1. The following compounds can be obtained in the same manner as in Example 3. 3, 4-1H, low 4-1-2-[4-[4-[N -methyl 2-[(3, 4-methyl range)) Nogishi] [chiramino] butoh] [Finyl] 1-3-Ogiso 2H-1,4-Benzothiazine oxalate
• the amount of the component of the large invention compound ft is 10 ⁇ ⁇ / capsule, 30z / capsule, 50 ⁇ g / Capsule and capsule of lOO ⁇ gZ capsule were also drawn down.
• Inventive compound A, 3 ⁇ 4 ⁇ , and varnish 3 starch are mixed together, and 1 liter of hydroxyprobicellulose methanol solution is added as a binder.
• the following granules were prepared by a conventional method.
• Inventive compound A 30 ⁇ g Mannitol 4 65 5 is Boli vinyl vinyl ⁇ Ridone 3 3 0 7 g g git RL 15 Recommend g The area

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• Health & Medical Sciences (AREA)
• Organic Chemistry (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• Engineering & Computer Science (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Hematology (AREA)
• Diabetes (AREA)
• Cardiology (AREA)
• Heart & Thoracic Surgery (AREA)
• Obesity (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Plural Heterocyclic Compounds (AREA)
• Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

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Citations (1)

• 1985
  • 1985-07-29 WO PCT/JP1985/000426 patent/WO1987000837A1/ja unknown
• 1986
  • 1986-07-21 JP JP61169847A patent/JPS62123181A/ja active Granted

Patent Citations (1)

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