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1. 发明授权

US10221144B2 Antibacterial compounds having broad spectrum of activity 有权
公开(公告)号：US10221144B2
公开(公告)日：2019-03-05
申请号：US15533594
申请日：2015-12-14
申请人： AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
发明人： Rosella Ombrato , Barbara Garofalo , Giorgina Mangano , Alessandra Capezzone De Joannon , Gaia Corso , Claudia Cavarischia , Guido Furlotti , Tommaso Iacoangeli
IPC分类号： C07C241/04 , C07D241/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D497/04 , A61K31/496 , C07D211/94 , C07D211/96
摘要： The present invention relates to novel antibacterial compounds, pharmaceutical compositions containing them and their use as antimicrobials.

2. 发明申请

US20180296553A1 PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF PAIN 审中-公开
公开(公告)号：US20180296553A1
公开(公告)日：2018-10-18
申请号：US15767543
申请日：2016-10-17
申请人： AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
发明人： Beatrice GARRONE , Lucia DURANDO , Fabrizio CALISTI
IPC分类号： A61K31/496 , A61K31/195 , A61P25/00
摘要： The present invention relates to a pharmaceutical composition comprising a combination of trazodone or a salt thereof, and gabapentin or a salt or prodrug thereof, said combination having a synergistic effect in the treatment of pain.

3. 发明授权

US10005730B2 3-aminocarbazole compound, pharmaceutical composition containing it and preparation method therefor 有权
公开(公告)号：US10005730B2
公开(公告)日：2018-06-26
申请号：US14969454
申请日：2015-12-15
申请人： AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F S.p.A.
发明人： Maria Alessandra Alisi , Nicola Cazzolla , Isabella Coletta , Patrizia Dragone , Guido Furlotti , Barbara Garofalo , Angelo Guglielmotti , Giorgina Mangano , Caterina Maugeri
IPC分类号： C07D209/88
CPC分类号： C07D209/88
摘要： The present invention relates to novel benzoyl derivatives of 3-aminocarbazole, to a pharmaceutical composition containing them, to a method for preparing them and to the use of such compounds for the production of a drug that is useful in the treatment or prevention of disturbances associated with the production of prostaglandin E2 (PGE2), for instance inflammatory processes, pain, fever, tumours, Alzheimer's disease and atherosclerosis.

4. 发明申请

US20180000783A1 PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF MYCOSIS 有权
公开(公告)号：US20180000783A1
公开(公告)日：2018-01-04
申请号：US15541245
申请日：2016-01-08
申请人： AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F.S.p.A.
发明人： Claudio MILANESE , Alessandra CAPEZZONE DE JOANNON , Serena TONGIANI , Luca DONATI
IPC分类号： A61K31/416 , A61K9/06 , A61K31/4174 , A61K31/4196
CPC分类号： A61K31/416 , A61K9/0014 , A61K9/06 , A61K31/4174 , A61K31/4196 , A61K45/06 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition comprising a combination of benzydamine and an antimycotic active ingredient, said combination having a synergistic effect in the treatment of mycosis.

5. 发明授权

US09655906B2 Tricyclic indazole compound, method of preparation and pharmaceutical composition containing it 有权
公开(公告)号：US09655906B2
公开(公告)日：2017-05-23
申请号：US14803384
申请日：2015-07-20
申请人： AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F S.p.A.
发明人： Maria Alessandra Alisi , Nicola Cazzolla , Guido Furlotti , Beatrice Garrone , Gabriele Magaro , Giorgina Mangano
IPC分类号： A61K31/4985 , C07D487/04 , A61K31/551
CPC分类号： A61K31/551 , A61K31/4985 , C07D487/04
摘要： Tricyclic indazole compound and its pharmaceutically acceptable salts of acid addition, use thereof, method and intermediates for preparing them, and a pharmaceutical composition containing them.The tricyclic indazole compound has the following general formula (I): in which R1, R2, L1, L2, X1, X2, X3, X4, X5, Y, W, m, and n have the meanings stated in the description.

6. 发明授权

US09416116B2 Method of preparation of metaxalone 有权
标题翻译：美他沙酮的制备方法
公开(公告)号：US09416116B2
公开(公告)日：2016-08-16
申请号：US14742203
申请日：2015-06-17
申请人： AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A.
发明人： Tommaso Iacoangeli , Mario Chiavarini , Antonello Fazio , Marcello Marchetti , Giovanni Battista Ciottoli
IPC分类号： C07D263/24 , C07D405/06 , C07D405/14
CPC分类号： C07D263/24 , C07D405/06 , C07D405/14
摘要： The present invention relates to a method of preparation of metaxalone comprising reaction of triglycidyl isocyanurate (TGIC) with m-xylenol, characterized in that said reaction is carried out in a solvent mixture comprising an aprotic polar solvent with dielectric constant greater than or equal to 30 and at least one other solvent selected from the group comprising apolar solvents and aprotic polar solvents with dielectric constant below 30 said solvent mixture comprising from 5 to 40 wt. % of said first solvent and from 95 to 60 wt. % of said second solvent, adding the TGIC at a temperature between 30° C. and 50° C., and after adding the TGIC, raising the temperature of the reaction solution to a value between 80° C. and 180° C. in a time between 120 and 180 minutes at a rate of increase not greater that 1.25° C. per minute. The invention also relates to a metaxalone with a reduced content of impurities derived from incomplete reactions and/or side reactions of the method of production.
摘要翻译：本发明涉及一种含有三聚甘油基异氰脲酸酯（TGIC）与间二甲苯酚反应的美他沙酮的方法，其特征在于所述反应在包含介电常数大于或等于30的非质子极性溶剂的溶剂混合物中进行和至少一种其它溶剂，其选自包含非极性溶剂和非质子极性溶剂的介质常数低于30的组，所述溶剂混合物包含5至40wt。所述第一溶剂的％和95至60wt。％的所述第二溶剂，在30℃至50℃的温度下加入TGIC，并且在加入TGIC之后，将反应溶液的温度升高至80℃至180℃之间的值时间在120至180分钟之间，增加速率不大于每分钟1.25℃。本发明还涉及衍生自生产方法的不完全反应和/或副反应的杂质含量降低的美他沙酮。

7. 发明授权

US09249097B2 3-aminocarbazole compound, pharmaceutical composition containing it and preparation method therefor 有权
标题翻译： 3-氨基咔唑化合物，含有它的药物组合物及其制备方法
公开(公告)号：US09249097B2
公开(公告)日：2016-02-02
申请号：US14109259
申请日：2013-12-17
申请人： AZIENDE CHIM. RIUN. ANG. FRANC. A.C.R.A.F. S.p.A.
发明人： Maria Alessandra Alisi , Nicola Cazzolla , Isabella Coletta , Patrizia Dragone , Guido Furlotti , Barbara Garofalo , Angelo Guglielmotti , Giorgina Mangano , Caterina Maugeri
IPC分类号： C07D209/88
CPC分类号： C07D209/88
摘要： The present invention relates to novel benzoyl derivatives of 3-aminocarbazole, to a pharmaceutical composition containing them, to a method for preparing them and to the use of such compounds for the production of a drug that is useful in the treatment or prevention of disturbances associated with the production of prostaglandin E2 (PGE2), for instance inflammatory processes, pain, fever, tumours, Alzheimer's disease and atherosclerosis.
摘要翻译：本发明涉及3-氨基咔唑的新型苯甲酰基衍生物，其含有它们的药物组合物，其制备方法和用于制备可用于治疗或预防相关疾病的药物的用途产生前列腺素E2（PGE2），例如炎症过程，疼痛，发烧，肿瘤，阿尔茨海默病和动脉粥样硬化。

8. 发明申请

US20140378532A1 GLYCOGEN-BASED CATIONIC POLYMERS 有权
标题翻译：基于GLYCOGEN的阳离子聚合物
公开(公告)号：US20140378532A1
公开(公告)日：2014-12-25
申请号：US14376299
申请日：2013-02-21
申请人： AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.
发明人： Vincenzo Russo , Elisa Liberati , Nicola Cazzolla
IPC分类号： A61K47/48 , A61K31/713 , C08B37/18
CPC分类号： A61K47/4823 , A61K31/713 , A61K31/716 , A61K47/61 , A61K2201/324 , A61K2201/326 , C08B37/0009 , C08B37/18
摘要： The present invention relates to glycogen-based cationic polymers, to complexes of the said cationic polymers with anionic compounds, to pharmaceutical compositions comprising the said complexes, and to the use of the said complexes for delivering or transfecting the said anionic compounds to a specific pharmacological target, such as, for instance an organ, a tissue or a cell.
摘要翻译：本发明涉及基于糖原的阳离子聚合物，所述阳离子聚合物与阴离子化合物的络合物，包含所述复合物的药物组合物，以及所述复合物用于将所述阴离子化合物递送或转染到特定药理学靶，例如器官，组织或细胞。

9. 发明授权

US08415476B2 Indazole having analgesic activity 有权
标题翻译：吲唑具有止痛活性
公开(公告)号：US08415476B2
公开(公告)日：2013-04-09
申请号：US12638470
申请日：2009-12-15
申请人： Maria Alessandra Alisi , Nicola Cazzolla , Guido Furlotti , Angelo Guglielmotti , Lorenzo Polenzani
发明人： Maria Alessandra Alisi , Nicola Cazzolla , Guido Furlotti , Angelo Guglielmotti , Lorenzo Polenzani
IPC分类号： C07D211/26
CPC分类号： C07D231/56
摘要： An intermediate of formula (II)
摘要翻译：式（II）的中间体

10. 发明授权

US08350052B2 Process for the preparation of 1-benzyl-3-hydroxymethyl-1H-indazole and its derivatives and required magnesium intermediates 有权
标题翻译：制备1-苄基-3-羟甲基-1H-吲唑及其衍生物及所需的镁中间体的方法
公开(公告)号：US08350052B2
公开(公告)日：2013-01-08
申请号：US13381137
申请日：2010-07-28
申请人： Giuliano Caracciolo Torchiarolo , Tommaso Iacoangeli , Guido Furlotti
发明人： Giuliano Caracciolo Torchiarolo , Tommaso Iacoangeli , Guido Furlotti
IPC分类号： C07D231/56
CPC分类号： C07D231/56 , C07F3/02
摘要： The present invention relates to the process for the conversion of 1-benzyl-3-hydroxymethyl-1H-indazole according to formula (II), to the 1-benzyl-3-hydroxylmethyl-1H-indazole according to formula (I).
摘要翻译：本发明涉及将式（II）的1-苄基-3-羟甲基-1H-吲唑转化为式（I）的1-苄基-3-羟甲基-1H-吲唑的方法。

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