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1. 发明专利

JP2015071622A 医薬品审中-公开
标题翻译：医学
公开(公告)号：JP2015071622A
公开(公告)日：2015-04-16
申请号：JP2014237957
申请日：2014-11-25
申请人：バイアルポルテラアンドシーエイエスエイ , BIAL−Portela & Ca, S.A.
发明人：ラズロエルノキス , ダヴィッドアレクサンダーリアマンス , カーラパトリシアダコスタペレイラローザ , リタグスマンデノローニャ , ペドロヌノレアルパルマ , パトリシオマニュエルヴィエイラアラウージョソアレスダシルヴァ , アレキサンダーベリエフ
IPC分类号： C07D471/04 , A61K31/422 , A61K31/437 , A61P1/04 , A61P1/08 , A61P1/16 , A61P3/00 , A61P3/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/06 , A61P19/02 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/34 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07D413/06
CPC分类号： C07D401/12 , C07D231/12 , C07D233/56 , C07D233/60 , C07D249/10 , C07D249/18 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/10 , C07D405/12 , C07D409/04 , C07D413/06 , C07D413/10 , C07D413/14 , C07D417/14
摘要：【課題】肥満、代謝異常、多発性硬化症、脊髄損傷、パーキンソン病、アルツハイマー病、てんかん、統合失調症、薬物中毒、高血圧、網膜症、がん、等の脂肪酸アミドヒドロラーゼ(FAAH)酵素によって分解される、神経伝達物質であるアナンダミドなどの基質と関連のある疾患の治療または予防に用いる化合物の提供。【解決手段】下記に例示されるFAAH酵素阻害剤及びそれを用いる治療。【選択図】なし
摘要翻译：要解决的问题：提供用于治疗和预防与基质相关的紊乱的化合物，所述基质是作为由脂肪酰胺水解酶（FAAH）酶分解的神经递质的阿那酰胺，所述脂肪酰胺水解酶（FAAH）如脂肪，dysbolism，多发性硬化，脊髓损伤，帕金森病，阿尔茨海默病，癫痫，综合性肌张力障碍，药物中毒，高血压，视网膜病变，癌症等。解决方案：提供如下所述的FAAH酶抑制剂和使用它的治疗。

2. 发明申请

WO2014017936A3 UREA COMPOUNDS AND THEIR USE AS ENZYME INHIBITORS 审中-公开
标题翻译：尿素化合物及其作为酶制剂的用途
公开(公告)号：WO2014017936A3
公开(公告)日：2014-01-30
申请号：PCT/PT2013/000048
申请日：2013-07-24
申请人： BIAL- PORTELA & CA, S.A.
发明人： ROSA, Carla Patrícia da Costa Pereira , GUSMÃO DE NORONHA, Rita , KISS, Laszlo Erno , SOARES DA SILVA, Patrício Manuel Vieira Araújo , RUSSO, Domenico , WAHNON, Jorge Bruno Reis , MATON, William
IPC分类号： C07D233/61 , C07C209/48 , C07D233/88 , A61K31/4178 , A61P31/00
摘要： A compound having the following structure: or a pharmaceutically acceptable salt or derivative thereof. The compound may be used in the treatment or prevention of a disorder selected from appetite regulation, obesity, metabolic disorders, cachexia, anorexia, pain, inflammation, neurotoxicity, neurotrauma, stroke, multiple sclerosis, spinal cord injury, Parkinson's disease, levodopa-induced dyskinesia, Huntington's disease, Gilles de la Tourette's syndrome, tardive dyskinesia, dystonia, amyotrophic lateral sclerosis, Alzheimer's disease, epilepsy, schizophrenia, anxiety, depression, insomnia, nausea, emesis, alcohol disorders, drug addictions such as opiates, nicotine, cocaine, alcohol and psychostimulants, hypertension, circulatory shock, myocardial reperfusion injury, atherosclerosis, asthma, glaucoma, retinopathy, cancer, inflammatory bowel disease, acute and chronic liver disease such as hepatitis and liver cirrhosis, arthritis and osteoporosis.
摘要翻译：具有以下结构的化合物：或其药学上可接受的盐或衍生物。该化合物可用于治疗或预防选自食欲调节，肥胖症，代谢病症，恶病质，厌食症，疼痛，炎症，神经毒性，神经创伤，中风，多发性硬化症，脊髓损伤，帕金森病，左旋多巴诱导的病症运动障碍，亨廷顿舞蹈病，吉莱斯德拉图雷特综合征，迟发性运动障碍，肌张力障碍，肌萎缩侧索硬化，阿尔茨海默病，癫痫，精神分裂症，焦虑症，抑郁症，失眠，恶心，呕吐，酒精紊乱，药物成瘾如阿片制剂，尼古丁，酒精和精神兴奋剂，高血压，循环性休克，心肌再灌注损伤，动脉粥样硬化，哮喘，青光眼，视网膜病，癌症，炎性肠病，急性和慢性肝病如肝炎和肝硬化，关节炎和骨质疏松症。

3. 发明申请

WO2010151160A1 O-SUBSTITUTED 3-N-HETEROARYL-1,3,4-OXADIAZOLONES FOR MEDICAL USE 审中-公开
标题翻译：用于医学用途的O-取代的3-N-异辛基-1,3,4-氧杂环丙烷
公开(公告)号：WO2010151160A1
公开(公告)日：2010-12-29
申请号：PCT/PT2009/000034
申请日：2009-06-24
申请人： BIAL - PORTELA & CA., S.A. , LEARMONTH, David Alexander , SILVA, Patrício Manuel, Vieira, Araújo, Soares da , KISS, Laszlo Erno
发明人： LEARMONTH, David Alexander , SILVA, Patrício Manuel, Vieira, Araújo, Soares da , KISS, Laszlo Erno
IPC分类号： C07D413/04 , C07D417/04 , A61K31/4245 , A61P25/28 , A61P9/12
CPC分类号： C07D413/04 , C07D417/04
摘要： The present invention relates to compound of formula (I), wherein A represents a 5- or 6-membered heteroaromatic ring system containing up to 4 heteroatoms selected from O, S and N, which is optionally substituted, and to a stereoisomer, pharmaceutically acceptable salt or ester, or prodrug thereof.
摘要翻译：本发明涉及式（I）化合物，其中A代表含有至多4个选自O，S和N的任选取代的杂原子的5-或6-元杂芳族环系统，以及立体异构体，其药学上可接受的盐或酯，或前药。

4. 发明申请

WO2010114404A1 PHARMACEUTICAL FORMULATIONS COMPRISING NITROCATECHOL DERIVATIVES AND METHODS OF MAKING THEREOF 审中-公开
标题翻译：包含硝基苯酚衍生物的药物制剂及其制备方法
公开(公告)号：WO2010114404A1
公开(公告)日：2010-10-07
申请号：PCT/PT2010/000014
申请日：2010-03-31
申请人： BIAL - PORTELA & CA., S.A. , VASCONCELOS, Teófilo Cardoso de , LIMA, Ricardo Jorge dos Santos , COSTA, Rui Cerdeira de Campos
发明人： VASCONCELOS, Teófilo Cardoso de , LIMA, Ricardo Jorge dos Santos , COSTA, Rui Cerdeira de Campos
IPC分类号： A61K9/16 , A61K9/20 , A61K31/4245 , A61K31/44
CPC分类号： A61K31/4439 , A61K9/1611 , A61K9/1635 , A61K9/1652 , A61K9/4808 , A61K31/4245 , A61K31/44 , A61K45/06 , A61K2300/00
摘要： The present disclosure relates to compositions and pharmaceutical formulations comprising at least one active pharmaceutical ingredient chosen from nitrocatechol derivatives of formula I as defined herein and salts, esters, hydrates, solvates and derivatives thereof and methods of making said compositions and pharmaceutical formulations.
摘要翻译：本公开内容涉及包含至少一种活性药物成分的组合物和药物制剂，其选自如本文所定义的式I的硝基邻苯二酚衍生物及其盐，酯，水合物，溶剂合物及其衍生物以及制备所述组合物和药物制剂的方法。

5. 发明申请

WO2021240383A1 TABLET COMPRISING OPICAPONE 审中-公开
公开(公告)号：WO2021240383A1
公开(公告)日：2021-12-02
申请号：PCT/IB2021/054574
申请日：2021-05-26
申请人： ONO PHARMACEUTICAL CO., LTD. , BIAL - PORTELA & CA, S.A.
发明人： TANIGUCHI, Koji , SEKIYA, Noboru , VASCONCELOS, Teófilo Cardoso de , LIMA, Ricardo Jorge dos santos
IPC分类号： A61K9/14 , A61K9/20
摘要： The present invention provides a tablet comprising opicapone or a pharmaceutically acceptable salt thereof, having reduced tableting faults during manufacture. It further relates to a tablet comprising opicapone or a pharmaceutically acceptable salt thereof, wherein the tablet comprises particles of opicapone or pharmaceutically acceptable salt thereof having the following particle size, and a manufacturing method thereof:(i) a maximum length D50 value of 45 μm or less, and/or (ii) a maximum length D90 value of 110 μm or less

6. 发明申请

WO2012091593A8 GRANULATES COMPRISING ESLICARBAZEPINE ACETATE 审中-公开
公开(公告)号：WO2012091593A8
公开(公告)日：2012-07-05
申请号：PCT/PT2011/000048
申请日：2011-12-30
申请人： BIAL - PORTELA & CA., S.A. , DA COSTA BARROCAS, Pedro Miguel , DOS SANTOS LIMA, Ricardo Jorge , CARDOSO DE VASCONCELOS, Teófilo , DE CAMPOS COSTA, Rui Cerdeira , DE CASTRO PEREIRA, Lígia Sofia , DE ALMEIDA JERÓNIMO, Paula Cristina
发明人： DA COSTA BARROCAS, Pedro Miguel , DOS SANTOS LIMA, Ricardo Jorge , CARDOSO DE VASCONCELOS, Teófilo , DE CAMPOS COSTA, Rui Cerdeira , DE CASTRO PEREIRA, Lígia Sofia , DE ALMEIDA JERÓNIMO, Paula Cristina
IPC分类号： A61K9/16 , A61K31/55
摘要： The invention relates to a solid pharmaceutical composition, the composition comprising eslicarbazepine acetate and one or more pharmaceutically acceptable excipients, wherein the composition is in the form of granules, and wherein at least 90% of the granules of the composition have a particle size of 90 μπι or more, and/or wherein at least 50% of the granules of the composition have a particle size of 250 μm or more. The invention also relates to a process for producing a granular composition. Further, the invention relates to the use of the composition in therapy and, in particular, in the treatment or prevention a disorder selected from epilepsy, neuropathic pain, migraine, fibromyalgia an affective disorders.

7. 发明申请

WO2009108077A3 PHARMACEUTICAL COMPOSITION FOR POORLY SOLUBLE DRUGS 审中-公开
公开(公告)号：WO2009108077A3
公开(公告)日：2009-09-03
申请号：PCT/PT2009/000009
申请日：2009-02-27
申请人： BIAL - PORTELA & CA., S.A. , VASCONCELOS, Teófilo Cardoso de
发明人： VASCONCELOS, Teófilo Cardoso de
IPC分类号： A61K9/14 , A61K9/20 , A61K31/19
摘要： A pharmaceutical composition containing a solid dispersion of a poorly soluble active pharmaceutical ingredient, an amorphous carrier and a surfactant.

8. 发明申请

WO2009054743A1 ORAL DOSAGE FORMS COMPRISING LICARBAZΞPINE ACETATE 审中-公开
标题翻译：口服剂型包含LICARBAZ？丙酸乙酯
公开(公告)号：WO2009054743A1
公开(公告)日：2009-04-30
申请号：PCT/PT2008/000043
申请日：2008-10-24
申请人： BIAL - PORTELA & CA., S.A. , VASCONCELOS, Teófilo Cardoso de , SANTOS LIMA, Ricardo Jorge dos , CAMPOS COSTA, Rui Cerdeira de
发明人： VASCONCELOS, Teófilo Cardoso de , SANTOS LIMA, Ricardo Jorge dos , CAMPOS COSTA, Rui Cerdeira de
IPC分类号： A61K9/00 , A61K9/20 , A61K47/48
CPC分类号： A61K31/55 , A61K9/0053 , A61K9/0056 , A61K9/16 , A61K9/1635 , A61K9/1652 , A61K9/1682 , A61K9/1694 , A61K9/20 , A61K9/2027 , A61K9/2054 , A61K9/2095 , A61K9/48 , A61K9/4866
摘要： A pharmaceutical composition comprising licarbazepine acetate, especially eslicarbazepine acetate, in combination with suitable excipients, in particular a binder, and a disintegrant. Also disclosed is a granulation process, especially a wet granulation process, for making the pharmaceutical composition
摘要翻译：一种药物组合物，其包含与适宜的赋形剂，特别是粘合剂和崩解剂组合的乙酸泻comprising啶，特别是醋酸西拉西平。还公开了用于制备药物组合物的造粒方法，特别是湿法制粒方法

9. 发明申请

WO2009072915A1 NEW SALTS AND CRYSTAL FORMS 审中-公开
标题翻译：新的销售和结晶形式
公开(公告)号：WO2009072915A1
公开(公告)日：2009-06-11
申请号：PCT/PT2008/000052
申请日：2008-12-05
申请人： BIAL - PORTELA & CA., S.A. , LEARMONTH, David , BELIAEV, Alexander , ROE, Melanie, J. , VLAHOVA, Petinka , HAGEN, Eric , SMOLENSKAYA, Valeriya , YANG, Donglai
发明人： LEARMONTH, David , BELIAEV, Alexander , ROE, Melanie, J. , VLAHOVA, Petinka , HAGEN, Eric , SMOLENSKAYA, Valeriya , YANG, Donglai
IPC分类号： C07D413/04 , A61K31/352 , A61P9/02
CPC分类号： C07D413/04
摘要： The present invention relates to novel salts of the compound (R)-5-(2-Aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione, polymorphs of the salts and methods of their preparation.
摘要翻译：本发明涉及化合物（R）-5-（2-氨基乙基）-1-（6,8-二氟色
素-3-基）-1,3-二氢咪唑-2-硫酮的新型盐，其盐的多晶型物及其制备方法。

10. 发明申请

WO2009054742A2 NOVEL PRECURSORS 审中-公开
标题翻译：新的前体
公开(公告)号：WO2009054742A2
公开(公告)日：2009-04-30
申请号：PCT/PT2008/000042
申请日：2008-10-24
申请人： BIAL - PORTELA & CA., S.A. , KISS, Laszlo Erno , LEARMONTH, David Alexander
发明人： KISS, Laszlo Erno , LEARMONTH, David Alexander
IPC分类号： C07D213/81 , C07D213/89 , C07D213/803 , C07D213/82
CPC分类号： C07D213/80 , C07D213/85 , C07D213/89 , Y02P20/55
摘要： The present invention relates to a Compound of the formula (I), wherein X represents CN, COOR, wherein R represents hydrogen or a carboxyl protecting group, CONR'2, wherein R' represents hydrogen or a carboxyl protecting group, or nitro; R1, R2, R3, R4, R5 independently of each other represent hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; Y represents hydrogen, C1-C6 alkyl, C3-C7 cycloalkyl, C7-C13 alkaryl, trifluoromethyl, cyano, nitro, substituted aryl or substituted heteroaryl group; and wherein the stereochemically unspecified double bonds in the above formula (I) represent either the E,E; E,Z; Z,E or Z,Z configuration.
摘要翻译：本发明涉及式（I）的化合物，其中X代表CN，COOR，其中R代表氢或羧基保护基，CONR'2，其中R'代表氢或羧基保护基或硝基; R 1，R 2，R 3，R 4，R 5彼此独立地表示氢，C 1 -C 6烷基，卤素，三氟甲基，氰基，硝基，取代的芳基或取代的杂芳基; Y代表氢，C1-C6烷基，C3-C7环烷基，C7-C13烷芳基，三氟甲基，氰基，硝基，取代的芳基或取代的杂芳基; 并且其中上式（I）中立体化学未指定的双键代表E，E; E，Z; Z，E或Z，Z配置。

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