Gyogyszerkutato Intezet Kft.

Ivax International Gmbh

N&aacute;ndor Makk

Antal Simay

Endre Kasztreiner

Katalin Horv&aacute;th

P&eacute;ter M&aacute;tyus

Alice Druga

Ildik&oacute; Varga

Gy&ouml;rgy Rabloczky

M&aacute;rta Varga

Egon K&aacute;rp&aacute;ti

Judit Kos&aacute;ry

Istv&aacute;n Kir&aacute;ly

Yemane Tilahun

Gy&ouml;rgy M&aacute;th&eacute;

L&aacute;szl&oacute; Sebesty&eacute;n

L&aacute;szl&oacute; H&aacute;rsing

Edit Horv&aacute;th

G&aacute;bor Ambrus

Ildik&oacute; N&eacute;e Gy&oacute;ry M&aacute;th&eacute;

Erzs&eacute;bet Z&aacute;ra N&eacute;e Kaczi&aacute;n

Andr&aacute;s Jeney

Marianne Tapfer N&eacute;e Karim

Margit Bidl&oacute; N&eacute;e Igl&oacute;y

&Aacute;gnes Papp N&eacute;e Behr

Ildik&oacute; M&aacute;th&eacute; N&eacute;e Gy&oacute;ry

&Aacute;gnes N&eacute;e Behr Papp

&Eacute;va N&eacute;e Joszt Tomori

&Eacute;va Tomori N&eacute;e Joszt

Mariann N&eacute;e Tapfer Karim

Ferenc Tim&aacute;r

Anik&oacute; Tegdes

Erzs&eacute;bet N&eacute;e Kaczi&aacute;n Z&aacute;ra

Margit N&eacute;e Igl&oacute;y Bidl&oacute;

The invention relates to compounds of general formula (I) wherein R stands for a group of general formula &mdash;COOR , &mdash;CONR R , &mdash;CONR CONR R or &mdash;CH OR , wherein R stands for a C alkyl group; a C alkyl group substituted; or a C cycloalkyl group; R and R are identical or different and stand independently from each other for hydrogen atom or a C alkyl group which optionally may be substituted; a 5- or 6-membered cycloalkyl or a heteroaryl group; and their tautomers, solvates and the mixtures thereof and acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising compounds of general formula (I) as active agent. The angiogenesis-inhibitors according to the invention inhibit the neovascularization in living tissues and as such can be used for preventing and inhibiting angiogenesis appearing in connection with tumor growth and for preventing the formation of tumor metastases.

Heterocyclic compounds inhibiting angiogenesis

The invention relates to R-2-&lsqb;3-(&lsqb;1,4&rsqb;benzodioxan-2-ylmethylamino)-1-propyl&rsqb;-3(2H)-pyridazinone of formula (1), and to S-2-&lsqb;3-(&lsqb;1,4&rsqb;benzodioxan-2-ylmethylamino)-1-propyl&rsqb;-3(2H)-pyridazinone of formula (2), and to acid-addition salts thereof as well as pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The new starting compounds of formulae (4) and (5) are also involved in the scope of the invention. The compounds according to the invention possess &agr;,- and &agr;,-adrenoceptor antagonistic effects and urogenital selectivity. Thus, they are useful for the treatment of the benign prostate hyperplasia.

N-(&lsqb;1,4&rsqb;benzodioxan-2-ylmethyl)-N-(3-chloro-1-propyl)-amine

The invention relates to R-2-&lsqb;3-(&lsqb;1,4&rsqb;benzodioxan-2-ylmethylamino)-1-propyl&rsqb;-3(2H)-pyridazionone of formula (1)

3(2H)-pyridazinone derivatives and pharmaceutical compositions containing these compounds

Growing community of inventors

Kismaros, Hungary

Nándor Makk

Growing community of inventors

Kismaros, Hungary

N&aacute;ndor Makk

Nándor Makk