Other

National Science Council

Kaohsiung Medical University

Syn-tech Chem. & Pharm. Co., Ltd.

Cho-jan Liang

Ing-jun Chen

Syn-rech Chem & Phan Co., Ltd

Tong-ho Lin

Ing-Jun Chen

Che-Ming Teng

Feng-Nien Ko

Chun-Nan Lin

Tong-Ho Lin

Shorong-Shii Liou

Jwu-Lai Yeh

Shwu-Jen Liou

The theophylline derivative disclosed in the present invention is characterized by having the pharmaceutical functions of osteoporosis. The theophylline derivative protects against bone resorption and inflammatory mediator infiltration.

Theophylline derivative inhibits osteoporosis

A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R, Rand RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function. 

Processes for preparing amine salts of sildenafil-analogues and use thereof

A series of monoquarternary piperazium salts including a structure of a formula I or II are provided. In formula I or II, R, R, and RX are as defined in the specification. The monoquarternary piperazium salt of KMUP or piperazine disclosed in the present invention is characterized by being presented in a pro-drug form and having various pharmaceutical functions. 

Processes for preparing piperazinium salts of KMUP and use thereof

A variety of N-substituted derivatives are based upon the base chemicals of that provide for the induction of cavernosal relaxation in animals. R2 is a derivative based on a hetroaromatic group, an aromatic group or a cyclohexane.

Theophylline and 3-isobutyl-1 methylxanthine based N-7 substituted derivatives displaying inhibitory activities on PDE-5 phospodiesterase

The present invention provides isoeugenol derivative compounds having the moiety and having &#x3b1;-adrenergic/5-HTantagonist, 5-HT re-uptake inhibition, and anti-oxidant activities.

Eugenosedin-A based pharmacoligical agents

The invention pertains to theophylline (1-methyl, 3-methyl xanthine) and IBMX (1-methyl, 3-isobutyl xanthine) derivatives of formulas I and II:where Ris &#x2014;CHor &#x2014;CHCH(CH), andRiswhere Rand Rare independently selected from the group consisting of OCH, CH, NO, F, Cl, Br and I.

Theophylline-based soluble guanylyl cyclase activators KMUP-1 analogues enhanced cyclic GMP and K+ channel activities on rabbit corpus cavernosum smooth muscle and intercavernous pressure activities

A compound having the following formula I:

KMST isoeugenol derivatives and pharmaceutical activity

Certain 1,4-dihydropyridine compounds, useful as adrenergic blocking agents and as calcium channel blocking agents, the compounds having the formulawherein Ris hydrogen, halogen, C-alkyl, or C-alkoxy, Ris hydrogen, halogen, C-alkyl, C-alkoxy, or CF(CH)O&#x2014; wherein n is, or, and Ris &#x2014;NHCHCHO&#x2014; or &#x2014;N(CHCH)N&#x2014;.

Phenoxypropanol connected with phenylpiperazine and phenoxyalkylamine terminal in its side chain

1,4-dihydropyridine derivative with a guaiacoxypropanolamine and/or phenoxypropanolamine moiety

Guaiacoxypropanolamines with alpha/beta adrenergic blocking activity

This invention is related to novel vasomolol, compounds of this invention have the following formula wherein R.sub.1 represents C.sub.1-4 alkyl group. ##STR1## vasomolol is an ultra short-acting and vasodilatory selective .beta..sub.1 -adrenoceptor antagonist, and is devoid of ISA. Vasomolol is an utra short acting and vasodilatory selective .beta..sub.1 -adrenoceptor antagonist, and is devoid of IA. The ultra short-acting and vsodilatory .beta..sub.1 -adrenoceptor blocking activities of vasomolol-a guaiacoxypropanolamine derivative of vanillic acid ethyl ester--were studied. Vasomolol (0.5, 1.0, 3.0 mg/kg, I.v.) produced a dose-dependent bradycardia rsponse, and particularly a hypotensive action with an ultra short-acting property in pentobarbital-anesthetized normotensive rats. Vasomolol's steady-state of .beta.-blockade was attained within 10 min after initiation of an infuson and a rapid recovery from blockade took place after termination of the infusion. In isolated rat aorta, vasomolol (10.sup.-6 M-10.sup.-5 M) inhibit both henylephrine (10.sup.-6 M) and High K.sup.+ (75 mM)--induced smooth muscle contractions, concentration-dependently. This inhibitory effect of vasomolol was more sensitive on K.sup.+ than on phenylephrine-induced contractions.

Vasomolol: an ultra short-acting and vasodilatory vanilloid type

A series of 4-O & 5-aminomethylation of synthetic capsaicin derivatives selectively reveal antagonist activity on capsaicin-sensitive sensory neurons, and inhibit its innervating atrium, airway, and ileum smooth muscles in vitro. The compound of this invention has the following formula ##STR1## wherein R is a member selected from the group consisting of ##STR2## wherein R.sub.1 is a member selected from the group consisting of C.sub.1-12 alkyl, C.sub.1-12 alkenyl, C.sub.1-12 alkylene, and C.sub.1-12 alkenylene, and wherein R.sub.2 is a member selected from the group consisting of H, C.sub.1-3 alkylene-NR.sub.1 R.sub.1, and C.sub.1-6 alkenylene-NR.sub.1 R.sub.1.

4-O and 5-aminomethylation of synthetic capsaicin derivatives, a new

Compounds of formula I ##STR1## in which OR.sup.1 is --OR.sub.3 NR.sub.4, in which R3 is a secondary alcohol group with 1.0 to 6 carbon atoms; a cyclic oxygen containing group with two carbon atoms; a pyridylmethyl or a piperidyl-ethyl group, R.sub.2 is alkyl, an ester group, an aldehyde group, a carboxylic acid group or a ketone group with 3 to 6 carbon --O--CONHR.sub.9 atoms, the group O--R.sub.7 NCOR.sub.8 or the group --O--CONHR.sub.9 in which R.sub.4 is an alkyl group with 1 to 8 carbon atoms, R.sub.7 is an alkylene group with 1 to 6 carbon atoms, each of R.sub.8 and R9 is an alkyl group with 1 to 12 carbon atoms and their pharmaceutically acceptable acid addition salts, are selective .beta.-blockers, antagonists of platelet aggregation, and .beta.-receptor binding. The processes of preparation, compositions, method of treatment are also described.

Synthesized .beta.-adrenergic blockers derivatives of guaiacol

This invention introduces a novel anti-glaucoma solution which comprises of Clozapine or Sulpiride and a pharmaceutical vehicle. This is the first time all the above agents have been prepared in ophthalmologic solutions, which will be able to decrease the IOP in animals.

Hypotensive intraocular pressure activity of clozapine and sulpiride

A compound, and salts thereof, represented by either formula I or formula II below: (1) Formula I: ##STR1## wherein substituents R.sub.1 -R.sub.7 can be, independently, hydrogen, hydroxy group, C.sub.1-6 alkyl(oxy) group, acetyl ester, or C.sub.1-12 alkyl propanolamine; at least three but no more than four of the substituents are alkyl(oxy) group, hydroxyl group or acetyl ester; no more than one of the substituents can be C.sub.1-12 alkyl propanolamines; R.sub.1, R.sub.3, R.sub.7 cnnnot all be hydroxy groups at the same time; and R.sub.6 is either an hydroxy group or an oxygen-containing glucose. (2) Formula II: ##STR2## wherein substituents R.sub.1 -R.sub.9 can be, indenpendently, hydrogen, hydroxy group and C.sub.1-6 alkyl(oxy) group; and no more then four of the substituents can be methoxy group, hydroxy group, or acetyl ester. These compounds were tested to be capable of inhibiting platelet aggregation, atrioventricular conduction, and calcium influx in myocardiac cells.

Growing community of inventors

Kaohsiung, Taiwan

Ing-Jun Chen