公开(公告)号：EP3377478A1

公开(公告)日：2018-09-26

申请号：EP16797941.8

申请日：2016-11-18

申请人： FAES FARMA, S.A.

发明人： HERNÁNDEZ HERRERO, Gonzalo ,  RUBIO ROYO, Víctor ,  GARCÍA DOMÍNGUEZ, Neftalí ,  CANAL MORI, Gonzalo ,  TESSON, Nicolas ,  JIMÉNEZ GONZÁLEZ, Carme ,  DE MIER VINUE, Jordi

IPC分类号： C07D401/04 ,  A61K31/445 ,  A61P37/08

CPC分类号： C07D401/04 ,  C07B2200/13 ,  C07C39/10 ,  C07C55/10 ,  C07C55/12 ,  C07C55/14 ,  C07C57/10 ,  C07C59/245 ,  C07C63/06 ,  C07C69/88 ,  C07C229/60 ,  C07C235/34

摘要： The invention relates to a cocrystal comprising a) at least a compound of formula (I), and b) at least a cocrystal forming compound selected from an organic molecule, or a solvate thereof. The invention further relates to methods for obtaining said cocrystals and to their use in the treatment and/or prevention of conditions mediated by H 1 histamine receptor, such as allergic disorders or diseases. The invention also relates to a method for increase the aqueous solubility of the above compounds of formula (I).

公开(公告)号：EP3377478B1

公开(公告)日：2019-07-24

申请号：EP16797941.8

申请日：2016-11-18

申请人： FAES FARMA, S.A.

发明人： HERNÁNDEZ HERRERO, Gonzalo ,  RUBIO ROYO, Víctor ,  GARCÍA DOMÍNGUEZ, Neftalí ,  CANAL MORI, Gonzalo ,  TESSON, Nicolas ,  JIMÉNEZ GONZÁLEZ, Carme ,  DE MIER VINUE, Jordi

IPC分类号： C07D401/04 ,  A61K31/445 ,  A61P37/08

公开(公告)号：EP3377479A1

公开(公告)日：2018-09-26

申请号：EP16797944.2

申请日：2016-11-18

申请人： FAES FARMA, S.A.

发明人： HERNÁNDEZ HERRERO, Gonzalo ,  RUBIO ROYO, Víctor ,  GARCÍA DOMÍNGUEZ, Neftalí ,  CANAL MORI, Gonzalo ,  TESSON, Nicolas

IPC分类号： C07D401/04 ,  A61K31/445 ,  A61P37/08

摘要： The invention relates to a stable supersaturated aqueous solution comprising a benzimidazole compound of formula (I) and an organic carboxylic acid selected from the group consisting of substituted or unsubstituted aliphatic C 3 -C 8 ±,É-dicarboxylic acids and substituted or unsubstituted aliphatic C 2 -C 6 monocarboxylic acids and to its use in the treatment and/or prevention of conditions mediated by H 1 histamine receptor, such as allergic disorders or diseases. The invention also relates to the use of the above organic carboxylic acids to increase the aqueous solubility of benzimidazole compounds of formula (I).

公开(公告)号：EP3170816A1

公开(公告)日：2017-05-24

申请号：EP15382574.0

申请日：2015-11-20

申请人： FAES FARMA, S.A.

发明人： HERNÁNDEZ HERRERO, Gonzalo ,  RUBIO ROYO, Víctor ,  GARCÍA DOMÍNGUEZ, Neftalí ,  CANAL MORI, Gonzalo ,  TESSON, Nicolas

IPC分类号： C07D401/04 ,  A61K31/445 ,  A61P37/08

CPC分类号： C07D401/04

摘要： The invention relates to a stable supersaturated aqueous solution comprising a benzimidazole compound of formula (I) and an organic carboxylic acid selected from the group consisting of substituted or unsubstituted aliphatic C 3 -C 8 α,ω-dicarboxylic acids and substituted or unsubstituted aliphatic C 2 -C 6 monocarboxylic acids and to its use in the treatment and/or prevention of conditions mediated by H 1 histamine receptor, such as allergic disorders or diseases. The invention also relates to the use of the above organic carboxylic acids to increase the aqueous solubility of benzimidazole compounds of formula (I).

摘要翻译： 本发明涉及包含式（I）的苯并咪唑化合物和选自取代或未取代的脂族C 3 -C 8α，ω-二羧酸和取代或未取代的脂族C 2 -C 6的有机羧酸的稳定的过饱和水溶液 一元羧酸及其在治疗和/或预防由H1组胺受体介导的病症如过敏性病症或疾病中的用途。 本发明还涉及上述有机羧酸用于提高式（I）的苯并咪唑化合物的水溶性的用途。

公开(公告)号：EP3377479B1

公开(公告)日：2020-01-29

申请号：EP16797944.2

申请日：2016-11-18

申请人： FAES FARMA, S.A.

发明人： HERNÁNDEZ HERRERO, Gonzalo ,  RUBIO ROYO, Víctor ,  GARCÍA DOMÍNGUEZ, Neftalí ,  CANAL MORI, Gonzalo ,  TESSON, Nicolas

IPC分类号： C07D401/04 ,  A61K31/445 ,  A61P37/08

公开(公告)号：EP3170817A1

公开(公告)日：2017-05-24

申请号：EP15382577.3

申请日：2015-11-20

申请人： Faes Farma, S.A.

发明人： HERNÁNDEZ HERRERO, Gonzalo ,  RUBIO ROYO, Víctor ,  GARCÍA DOMÍNGUEZ, Neftalí ,  CANAL MORI, Gonzalo ,  TESSON, Nicolas ,  JIMÉNEZ GONZÁLEZ, Carme ,  DE MIER VINUE, Jordi

IPC分类号： C07D401/04 ,  A61K31/445 ,  A61P37/08

CPC分类号： C07D401/04

摘要： The invention relates to a cocrystal comprising
a) at least a compound of formula (I),

and
b) at least a cocrystal forming compound selected from an organic molecule,

or a solvate thereof. The invention further relates to methods for obtaining said cocrystals and to their use in the treatment and/or prevention of conditions mediated by H 1 histamine receptor, such as allergic disorders or diseases. The invention also relates to a method for increase the aqueous solubility of the above compounds of formula (I).

摘要翻译： 本发明涉及共结晶，其包含a）至少一种式（I）的化合物，和b）至少一种选自有机分子或其溶剂化物的共结晶形成化合物。 本发明进一步涉及获得所述共结晶的方法及其在治疗和/或预防由H1组胺受体介导的病症如过敏性病症或疾病中的用途。 本发明还涉及用于提高上述式（I）化合物的水溶性的方法。