2-Substituted 4-Amino-6,7-Dimethoxyquinolines Novel derivatives of 4-amino-6,7-dimethoxyquinoline are disclosed as regulators of the cardiovascular system, in particular as antihypertensive agents, which have the formula: where R is a dialkylamino, piperidino or 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl group, or a piperazino group optionally substituted in the 4-position by an alkyl, aryl, aromatic heterocyclyl, acyl, N-substituted carbamoyl or esterified carboxyl group. Preparation of such compounds by cyclisation of N-(1R-substituted-ethylidene)-2-cyano-4,5-dimethoxy-anilines, and by appropriate treatment of the compound in which R is an unsubstituted piperazino group, is described.

2-Substituted 4-amino-6,7-dimethoxyquinolines

Compounds useful as cytotoxic agents are selected from the group consisting of compounds of Formula (I) and compounds of Formula (II), wherein: R1, R2, R3 and R4 are each independently selected from the group consisting of: hydrogen, alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, thiophenylcarbonyl; nitro and cyano; thiophenyl and thiophenylthiophenyl, each of which may be unsubstituted or substituted with alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, nitro or cyano; subject to the proviso that at least one of R1, R2, R3 and R4 is not hydrogen; A1 and A2 are each selected from the group consisting of: =O, alkyl, alkoxy, and alkylcarbonyloxy; and the pharmaceutically acceptable salts thereof. When A1 and A2 are =O, the center ring has only two, and not three, double bonds.

Naphtho- and dihydrobenzo-thiophene derivatives as cytotoxic antitumor agents

The hypertensive effect on the development of the prostatic abnormality in spontaneously hypertensive rats (SHRs) was examined using Efonidipine hydrochloride, a calcium antagonist. The control SHRs were given a high sodium and potassium diet (SP-diet) alone, and the treated SHRs were given a SP-diet with 0.15% Efonidipine hydrochloride from 8 to 28 weeks of age. The systolic blood pressure (SBP) in the control SHRs increased with age, while the elevation of SBP was significantly prevented in the treated SHRs. Light-microscopically, the prostatic lesion was observed both in the control and treated SHRs. The glandular lumen was narrowed with papillary protrusions, and the epithelium was composed of tall columnar epithelial cells. However, hypertension-induced complications in kidneys and hearts were not observed in the treated SHRs. These results suggested that the prostatic abnormality of SHRs might not be the consequent lesions upon hypertension.

Influence of efonidipine hydrochloride, calcium antagonist on the epithelium of prostates in spontaneously hypertensive rats

PURPOSE:To shorten the turn-OFF time while sufficiently keeping even other characteristics within a proper range by irradiating a high resistivity region with radiation and shortening the turn-OFF time through heat treatment. CONSTITUTION:A chip 1 consisting of a high resistivity region 4 having 100OMEGAm resistivity and an SEC in 230mum thickness is irradiated with electron beams having acceleration energy of 5MeV up to the exposure of 10Mrad, and an electrostatic induction thyristor is completed through heat treatment for thirty min at 360 deg.C. Various radiation such as electron beams, gamma-rays, neutron beams, X-rays, etc., are used as the kind of radiation, and a plural kind of radiation may be employed in combination. The conditions of heat treatment are selected properly in response to the kind of radiation, exposure, the thickness of the high resistivity region in an element, etc. It is preferable that the temperature of treatment is set between approximately 300-400 deg.C. Accordingly, the balanced electrostatic induction thyristor, the turn-OFF time of which is shortened and which has excellent characteristics while other characteristics are kept sufficiently within a proper range, can easily be acquired.

Manufacture of electrostatic induction thyristor

PURPOSE:To facilitate walking in the case of the waste and knees with the easing of pains by getting two ends of a band-shaped pressure body engaged to make a face fastener for making up a circular body. CONSTITUTION:A headache releasing band 1 has a pressure body 2 comprising crude rubber rings 3a, 3b... joined together and a cover body 4 which covers the pressure body 3 and prevents the pressure body 2 from catching hair when mounted on a head. The band is worn with one end thereof at a margin of the forehead at the front of the head while the rear of the head thereof positioned at the scruff. A crotch adjusting belt 6 is made up of two belt-shaped pressure bodies 7a and 7b comprising fibrous elastic material which is regulated in width-wise expansion while being expanded freely in other directions. The two belt-shaped pressure bodies are joined with rectangular joints 8a and 8b regulated in length-wise and width-wise directions to put them together with both ends thereof piled one upon the other and when the joints are bound together with surface fasteners 9a and 9b provided on the joints 8a and 8b, a double band of the belt-shaped pressure bodies 7a and 7b forms a circular body. The circular body thus obtained is worn wrapping a human hip part and the surface fasteners 9a and 9b are bound together being positioned in front of a human body. In this manner, the belt is fixed with the belt-shaped pressure body 7a wrapping the hip part in double being lowered to the lower part of the hip part.

Physical conditioning apparatus and use thereof

PURPOSE:To prepare the titled compounds (some of which are novel) useful as intermediates of pharmaceuticals, etc., easily, in high yield, by reacting a ketone such as dialkyl ketone, alkyl phenyl ketone, cyclic ketone, etc., with an N-cyano- S-alkyisothiourea. CONSTITUTION:The pyrimidine derivative of formula III (R is 1-5C alkyl or phenyl; R is H or 1-5C alkyl; R and R may together form 3-5C alkylene; R is 1-5C alkyl; m is 0-2) (e.g. 2-methylthio-4-amino-5,6-trimethylenepyrimidine) is prepared by reacting a compound of formula I (e.g. cyclopentanone) with a compound of formula II (e.g. N-cyano-S-methylisothiourea), and if necessary, oxidizing the resulting 4-amino-pyrimidine ring. USE:Antiphlogistic compound. Intermediate for a 2.4-diaminopyridine derivative (antimalarial agent, carcinostatic agent, antibacterial agent, antihypertensive agent, hypoglycemic agent, etc.).

Preparation of pyrimidine derivative

NEW MATERIAL:A compound (salt) shown by the formula I (one of X and Y is O, and the other is methylene or carbonyl; A is H, halogen, methyl, acetyl, cyanoethyl, etc.; B is H, halogen, methyl, alpha-cyanoethyl, methoxycarbonylmethyl, etc.; C is H, halogen, methyl, methoxycarbonylmethyl, etc.; D and E are H, halogen, or methyl; with the proviso that the case wherein X is O, Y is carbonyl, and A-E are H is omitted). EXAMPLE:9H-Thieno[3,2-b][1] benzopyran-2-propionic acid. USE:An antiphlogistic. PROCESS:For example, a 3-alkoxythiophene is reacted with o-anisoyl chloride to give a compound shown by the formula II, which is subjected to ring closure to give 9H-thieno[3,2-b][1] benzopyran shown by the formula III, which is further acetylated, converted into a nitrile group, and hydrolyzed, to give a compound shown by the formula I .

Mizogami Susumu

Papers

Preparation of pyrimidine derivative

9h-thieno(3,2-b) or 4h-thieno(2,3-b)(1) benzopyran derivative

Antihypertensive effect of terazosin on experimental hypertension in rats.

Novel quinazoline derivative*its manufacture and antihypertensive drug

Novel quinazoline derivative and manufacture