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1. 发明申请

US20140024648A1 NEW PYRIDAZINONE AND PYRIDONE COMPOUNDS 有权
标题翻译：新的吡咯烷酮和吡咯烷酮化合物
公开(公告)号：US20140024648A1
公开(公告)日：2014-01-23
申请号：US14003626
申请日：2012-03-06
申请人： Marjo Pihlavisto , David Smith , Auni Juhakoski , Ferenc Fulop , Laszlo Lazar , Istvan Szatmari , Ferenc Miklos , Zsolt Szakonyi , Lorand Kiss , Marta Palko
发明人： Marjo Pihlavisto , David Smith , Auni Juhakoski , Ferenc Fulop , Laszlo Lazar , Istvan Szatmari , Ferenc Miklos , Zsolt Szakonyi , Lorand Kiss , Marta Palko
IPC分类号： C07D237/24 , A61K31/501 , A61K45/06 , A61K31/50 , C07D403/12 , C07D401/04 , C07D405/04 , C07D413/04 , C07D409/04 , C07D403/14 , A61K31/5377 , C07D401/14 , C07D237/16 , C07D405/14 , G01N33/50 , C07D403/04
CPC分类号： C07D237/24 , A61K31/4439 , A61K31/496 , A61K31/50 , A61K31/501 , A61K31/5377 , A61K45/06 , C07C57/15 , C07D237/16 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , G01N33/502
摘要： The invention relates to pyridazinone and pyridone compounds having formula (I) or (I′), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are 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.
摘要翻译：本发明涉及具有式（I）或（I'）的哒嗪酮和吡啶酮化合物及其药学上可接受的盐，水合物和溶剂合物（I），其中R1 / R4和X和X3如权利要求中所定义。本发明还涉及它们作为含铜胺氧化酶抑制剂的用途。本发明还涉及上述化合物的制备以及包含一种或多种上述化合物，药学上可接受的盐，水合物或溶剂合物作为活性成分的药物组合物。

2. 发明授权

US09371290B2 Pyridazinone compounds 有权
标题翻译：哒嗪酮化合物
公开(公告)号：US09371290B2
公开(公告)日：2016-06-21
申请号：US14003626
申请日：2012-03-06
申请人： Marjo Pihlavisto , David Smith , Auni Juhakoski , Ferenc Fulop , Laszlo Lazar , Istvan Szatmari , Ferenc Miklos , Zsolt Szakonyi , Lorand Kiss , Marta Palko
发明人： Marjo Pihlavisto , David Smith , Auni Juhakoski , Ferenc Fulop , Laszlo Lazar , Istvan Szatmari , Ferenc Miklos , Zsolt Szakonyi , Lorand Kiss , Marta Palko
IPC分类号： A61K31/50 , A61K31/501 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D237/24 , C07D405/14 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D401/14 , A61K31/5377 , A61K45/06 , C07D237/16 , C07D403/12 , C07D403/14 , G01N33/50
CPC分类号： C07D237/24 , A61K31/4439 , A61K31/496 , A61K31/50 , A61K31/501 , A61K31/5377 , A61K45/06 , C07C57/15 , C07D237/16 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , G01N33/502
摘要： The invention relates to pyridazinone and pyridone compounds having formula (I) or (I′), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are 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.
摘要翻译：本发明涉及具有式（I）或（I'）的哒嗪酮和吡啶酮化合物及其药学上可接受的盐，水合物和溶剂合物（I），其中R1 / R4和X和X3如权利要求中所定义。本发明还涉及它们作为含铜胺氧化酶抑制剂的用途。本发明还涉及上述化合物的制备以及包含一种或多种上述化合物，药学上可接受的盐，水合物或溶剂合物作为活性成分的药物组合物。

3. 发明授权

US06982286B2 Carbocyclic hydrazino inhibitors of copper-containing amine oxidases 失效
标题翻译：含铜胺氧化酶的碳环肼抑制剂
公开(公告)号：US06982286B2
公开(公告)日：2006-01-03
申请号：US09902789
申请日：2001-07-12
申请人： David John Smith , Ferenc Fülöp , Marjo Pihlavisto , László Lázár , Sakari Alaranta , Petri Vainio , Zsolt Szakonyi
发明人： David John Smith , Ferenc Fülöp , Marjo Pihlavisto , László Lázár , Sakari Alaranta , Petri Vainio , Zsolt Szakonyi
IPC分类号： A61K31/135
CPC分类号： C07D273/00 , A61K31/15 , C07C243/20 , C07C2602/08
摘要： 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 R1 to R11 are as defined herein.
摘要翻译：本发明涉及用作通常称为氨基脲敏感性胺氧化酶（SSAO）的含铜胺氧化酶的抑制剂的碳环肼化合物，包括称为血管粘附蛋白-1（VAP-1）的人SSAO。这些SSAO抑制剂具有用于治疗病症和疾病的药物的治疗用途，包括但不限于许多炎性病症和疾病（特别是慢性炎症病症如慢性关节炎，炎性肠病和慢性皮肤皮肤病），相关疾病到碳水化合物代谢和脂肪细胞分化或功能和平滑肌细胞功能异常以及血管疾病。新化合物具有以下通式：或其药学上可接受的溶剂合物，水合物或盐，其中R 1至R 11如本文所定义。

4. 发明申请

US20100081717A1 Chiral Cyclic Beta-Amino Acids and their Derivatives, Pharmaceutical Compositions Containing Them and the Use of Such Compounds 有权
标题翻译：手性环状β-氨基酸及其衍生物，含有这些化合物及其使用的药物组合物
公开(公告)号：US20100081717A1
公开(公告)日：2010-04-01
申请号：US12513369
申请日：2007-11-14
申请人： Ferenc Fulop , Zsolt Szakonyi
发明人： Ferenc Fulop , Zsolt Szakonyi
IPC分类号： A61K31/195 , C07C229/00
CPC分类号： C07C335/18 , C07B2200/07 , C07C215/42 , C07C229/50 , C07C271/24 , C07C275/30 , C07C275/34 , C07C335/14 , C07C2602/42 , C07C2603/18 , C07D205/12
摘要： The invention relates to chiral cyclic β-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 C1-4 Alk; X stands for —COOH, —CONH2, —CONH(C1-4 Alk), —CON(C1-4 Alk)2, —COO(C1-4 Alk), —COPhe-O-(C1-4 Alk) or —CH2OH; Y stands for —NH2, —NHBoc, —NHFmoc, —NH(C1-4 Alk), —N(C1-4 Alk)2, —NHCH2Ph, or Ar—NH—C(=X0)—N(R0)— wherein Ar stands for a phenyl group substituted by C1-4 alkoxy or halogen, X0 stands for O or S, and R0 stands for hydrogen or benzyl; and X+Y stands for —CONH— vagy —CON(Boc)-; with the proviso that when X stands for —COOH, then Y may be only different from —NH2. 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.
摘要翻译：本发明涉及式（I）的手性环状 - 氨基酸及其与药学上可接受的酸或碱形成的盐，其中取代基的主要含义如下：R代表C1-4烷基; X代表-COOH，-CONH 2，-CONH（C 1-4 Alk），-CON（C 1-4 Alk）2，-COO（C 1-4 Alk），-C OPhe-O-（C 1-4 Alk）或 - CH2OH; Y代表-NH2，-NHBoc，-NHFmoc，-NH（C1-4 Alk），-N（C1-4 Alk）2，-NHCH2Ph或Ar-NH-C（= X0）-N（R0） - 其中Ar表示被C 1-4烷氧基或卤素取代的苯基，X 0表示O或S，R 0表示氢或苄基; 而X + Y代表-CONH- vagy -CON（Boc） - ; 条件是当X代表-COOH时，则Y可以仅与-NH 2不同。本发明还涉及含有一种或多种式（I）化合物或其盐和惰性药物载体和/或辅助剂的具有多重耐药性逆转作用的药物组合物。本发明还涉及式（XX）的羧酸及其盐。

5. 发明授权

US08183292B2 Chiral cyclic β-amino acids and their derivatives, pharmaceutical compositions containing them and the use of such compounds 有权
标题翻译：手性环状 - 氨基酸及其衍生物，含有它们的药物组合物和这些化合物的用途
公开(公告)号：US08183292B2
公开(公告)日：2012-05-22
申请号：US12513369
申请日：2007-11-14
申请人： Ferenc Fulop , Zsolt Szakonyi
发明人： Ferenc Fulop , Zsolt Szakonyi
IPC分类号： A61K31/17
CPC分类号： C07C335/18 , C07B2200/07 , C07C215/42 , C07C229/50 , C07C271/24 , C07C275/30 , C07C275/34 , C07C335/14 , C07C2602/42 , C07C2603/18 , C07D205/12
摘要： The invention relates to chiral cyclic β-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 C1-4 Alk; X stands for —COOH, —CONH2, —CONH(C1-4 Alk), —CON(C1-4 Alk)2, —COO(C1-4 Alk), —COPhe-O—(C1-4 Alk) or —CH2OH; Y stands for —NH2, —NHBoc, —NHFmoc, —NH(C1-4 Alk), —N(C1-4 Alk)2, —NHCH2Ph, or Ar—NH—C(═X0)—N(R0)— wherein Ar stands for a phenyl group substituted by C1-4 alkoxy or halogen, X0 stands for O or S, and R0 stands for hydrogen or benzyl; and X+Y stands for —CONH— vagy —CON(Boc)-; with the proviso that when X stands for —COOH, then Y may be only different from —NH2. 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.
摘要翻译：本发明涉及式（I）的手性环状 - 氨基酸及其与药学上可接受的酸或碱形成的盐，其中取代基的主要含义如下：R代表C1-4烷基; X代表-COOH，-CONH 2，-CONH（C 1-4 Alk），-CON（C 1-4 Alk）2，-COO（C 1-4 Alk），-C OPhe-O-（C 1-4 Alk）或 - CH2OH; Y代表-NH2，-NHBoc，-NHFmoc，-NH（C1-4 Alk），-N（C1-4 Alk）2，-NHCH2Ph或Ar-NH-C（= X0）-N（R0） - 其中Ar表示被C 1-4烷氧基或卤素取代的苯基，X 0表示O或S，R 0表示氢或苄基; 而X + Y代表-CONH- vagy -CON（Boc） - ; 条件是当X代表-COOH时，则Y可以仅与-NH 2不同。本发明还涉及含有一种或多种式（I）化合物或其盐和惰性药物载体和/或辅助剂的具有多重耐药性逆转作用的药物组合物。本发明还涉及式（XX）的羧酸及其盐。

6. 发明授权

US06624202B2 Inhibitors of copper-containing amine oxidases 失效
标题翻译：含铜胺氧化酶的抑制剂
公开(公告)号：US06624202B2
公开(公告)日：2003-09-23
申请号：US09898003
申请日：2001-07-05
申请人： David John Smith , Markku Jalkanen , Ferenc Fülöp , László Lázár , Zsolt Szakonyi , Gábor Bernáth
发明人： David John Smith , Markku Jalkanen , Ferenc Fülöp , László Lázár , Zsolt Szakonyi , Gábor Bernáth
IPC分类号： A61K3115
CPC分类号： A61K31/131 , A61K31/14 , A61K31/15 , A61K31/40 , A61K31/445 , A61K31/472
摘要： The present invention is directed to 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-1 (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 compounds have the general formula: or a pharmaceutically acceptable solvate, hydrate, or salt thereof, wherein R1 to R8 and X are as defined herein.
摘要翻译：本发明涉及用作通常称为氨基脲敏感性胺氧化酶（SSAO）的含铜胺氧化酶的抑制剂的肼基化合物，包括称为血管粘附蛋白-1（VAP-1）的人SSAO。这些SSAO抑制剂具有用于治疗病症和疾病的药物的治疗用途，包括但不限于许多炎性病症和疾病（特别是慢性炎症病症如慢性关节炎，炎性肠病和慢性皮肤皮肤病），相关疾病到碳水化合物代谢和脂肪细胞分化或功能和平滑肌细胞功能异常以及血管疾病。所述化合物具有以下通式：或其药学上可接受的溶剂合物，水合物或盐，其中R 1至R 8和X如本文所定义。

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