Biotie Therapies Corporation

Bioblocks Magyarorszag Gyogyszerkemiai Es Fejleszto Kft.

Zsolt Szakonyi

David Smith

Ferenc Fulop

Marjo Pihlavisto

Laszlo Lazar

Istvan Szatmari

Ferenc Miklos

Lorand Kiss

Auni Juhakoski

Marta Palko

Markku Jalkanen

Ferenc Fülöp

Petri Vainio

Ferenc F&uuml;l&ouml;p

L&aacute;szl&oacute; L&aacute;z&aacute;r

László Lázár

Sakari Alaranta

G&aacute;bor Bern&aacute;th

The invention relates to pyridazinone and pyridone compounds having formula (I) or (I'), and pharmaceutically acceptable salts, hydrates, and solvates thereof wherein R/Rand X and Xare as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.

Pyridazinone and pyridone compounds

The invention relates to pyridazinone and pyridone compounds having formula (I) or (I'), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R/Rand X and Xare as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof. 

Pyridazinone compounds

The invention relates to chiral cyclic &#x3b2;-amino acids of Formula (I) and their salts formed with pharmaceutically acceptable acids or bases, wherein the main meanings of the substituents are as follows: R stands for CAlk; X stands for &#x2014;COOH, &#x2014;CONH, &#x2014;CONH(CAlk), &#x2014;CON(CAlk), &#x2014;COO(CAlk), &#x2014;COPhe-O&#x2014;(CAlk) or &#x2014;CHOH; Y stands for &#x2014;NH, &#x2014;NHBoc, &#x2014;NHFmoc, &#x2014;NH(CAlk), &#x2014;N(CAlk), &#x2014;NHCHPh, or Ar&#x2014;NH&#x2014;C(&#x2550;X)&#x2014;N(R)&#x2014; wherein Ar stands for a phenyl group substituted by Calkoxy or halogen, Xstands for O or S, and Rstands for hydrogen or benzyl; and X+Y stands for &#x2014;CONH&#x2014; vagy &#x2014;CON(Boc)-; with the proviso that when X stands for &#x2014;COOH, then Y may be only different from &#x2014;NH. The invention also relates to pharmaceutical compositions having multidrug-resistance reversing effect that contain one or more compound(s) of Formula (I) or a salt thereof and inert pharmaceutical carriers and/or auxiliary agents. The invention also relates to carboxylic acids of Formula (XX) and their salts.

Chiral cyclic &#x3b2;-amino acids and their derivatives, pharmaceutical compositions containing them and the use of such compounds

The present invention is directed to carbocyclic hydrazino compounds that function as inhibitors of copper-containing amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-I (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases. The novel compounds have the general formula:or a pharmaceutically acceptable solvate, hydrate, or salt thereof wherein Rto Rare as defined herein.

Carbocyclic hydrazino inhibitors of copper-containing amine oxidases

Inhibitors of copper-containing amine oxidases

Growing community of inventors

Szeged, Hungary

Zsolt Szakonyi