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11. 发明申请

WO2006075925A2 METHOD FOR PREPARATION OF 10,11-DIHYDRO-10-HYDROXY-5H-DIBENZ/B,F/AZEPINE-5-CARBOXAMIDE 审中-公开
标题翻译：制备10,11-二氢-10-羟基-5H-二苯并/ B，F / AZEPINE-5-羧酰胺的方法
公开(公告)号：WO2006075925A2
公开(公告)日：2006-07-20
申请号：PCT/PT2006/000002
申请日：2006-01-13
申请人： PORTELA & C.A., S.A. , LEARMONTH, David, Alexander , WEINGÄRTNER, Günter , KRAEMER, Matthias
发明人： LEARMONTH, David, Alexander , WEINGÄRTNER, Günter , KRAEMER, Matthias
IPC分类号： C07D223/22 , C07D491/04 , A61K31/55
CPC分类号： C07D491/04 , C07D223/22
摘要： A process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (1) by ring opening of 11a,10b-dihydro-6H-dibenz/b,f/oxireno[d]azepine-6-carboxamide (5), characterised in that the ring opening is carried out under conditions of elevated pressure.
摘要翻译：制备10,11-二氢-10-羟基-5H-二苯并[b，f /吖庚因-5-甲酰胺（1））的方法，通过11a，10b-二氢-6H-二苯并/ b，f / oxireno [d]吖庚因-6-甲酰胺（5），其特征在于开环在高压条件下进行。

12. 发明申请

WO2013002660A2 PROCESS 审中-公开
标题翻译：处理
公开(公告)号：WO2013002660A2
公开(公告)日：2013-01-03
申请号：PCT/PT2012/000024
申请日：2012-06-29
申请人： BIAL - PORTELA & Cª, S.A. , BELIAEV, Alexander , WAHNON, Jorge Bruno Reis , LEARMONTH, David Alexander , MADEC, Jonathan , SCHNEIDER, Jean-Marie , MATON, William
发明人： BELIAEV, Alexander , WAHNON, Jorge Bruno Reis , LEARMONTH, David Alexander , MADEC, Jonathan , SCHNEIDER, Jean-Marie , MATON, William
IPC分类号： C07C311/19 , C07D403/04
CPC分类号： C07D405/04 , C07C235/80 , C07C311/16 , C07C311/17
摘要： The present invention relates to a process for preparing (R)-5-(2-(benzylamino)ethyl)-1-(6,8-difluorochroman-3-yl)-1H-imidazole-2(3H)-thione, and pharmaceutically acceptable salts thereof, especially the hydrochloride salt. The invention also relates to a process for making intermediates useful in the formation of said compound, and to the intermediates, per se.
摘要翻译：本发明涉及制备（R）-5-（2-（苄基氨基）乙基）-1-（6,8-二氟色
素-3-基）-1H-咪唑-2（3H） - 硫酮的方法，和其药学上可接受的盐，特别是盐酸盐。本发明还涉及可用于形成所述化合物的中间体以及中间体本身的方法。

13. 发明申请

WO2012107708A9 ADMINISTRATION REGIME FOR NITROCATECHOLS 审中-公开
公开(公告)号：WO2012107708A9
公开(公告)日：2012-08-16
申请号：PCT/GB2011/052056
申请日：2011-10-21
申请人： BIAL - PORTELA & CA, S.A. , SOARES DA SILVA, Patricio Manuel Vieira Araujo , NUNES, Teresa Lucia Silva Pereira , WRIGHT, Lyndon Christopher , PALMA, Pedro Nuno Leal , LEARMONTH, David Alexander
发明人： SOARES DA SILVA, Patricio Manuel Vieira Araujo , NUNES, Teresa Lucia Silva Pereira , WRIGHT, Lyndon Christopher , PALMA, Pedro Nuno Leal , LEARMONTH, David Alexander
IPC分类号： A61K31/4439 , A61P25/00 , A61P25/16
摘要： A compound of formula (I) where R 1 , R 2 , X, Y, n, m, R 3 , R 4 , R 5 , R 6 and R 7 are as defined herein, for use in the prophylaxis or treatment of a central and peripheral nervous system disorder, wherein the compound of formula (I) is administered prior to sleep, before bedtime or at bedtime.

14. 发明申请

WO2010074587A3 5-O-SUBSTITUTED 3-N-ARYL-1,3,4-OXADIAZOLONES FOR MEDICAL USE 审中-公开
标题翻译：用于医疗用途的5-O-取代的3-N-芳基-1,3,4-恶二唑啉酮
公开(公告)号：WO2010074587A3
公开(公告)日：2010-11-11
申请号：PCT/PT2009000079
申请日：2009-12-23
申请人： BIAL PORTELA & CA SA , LEARMONTH DAVID ALEXANDER , SILVA PATRICIO MANUEL VIEIRA ARAUJO SOARES DA
发明人： LEARMONTH DAVID ALEXANDER , SILVA PATRICIO MANUEL VIEIRA ARAUJO SOARES DA
IPC分类号： C07D285/13 , A61K31/4245 , A61K31/4709 , C07D413/12 , C07D413/14
CPC分类号： C07D285/13 , C07D413/12 , C07D413/14
摘要： The present invention relates to a compound of formula (I), wherein A represents an optionally substituted phenyl or a 5- or 6-membered heteroaromatic ring system containing up to 4 heteroatoms selected from O, S and N, B represents a single bond, O, S or NR1, wherein R1 is selected from hydrogen or a C1-C6-alkyl group; L represents a linker; C represents an amino moiety; n represents 0 or 1; m represents 0, 1, 2, 3, 4, 5 or 6; X represents O or S; and Y represents hydrogen or an optionally substituted carbon moiety; and to stereoisomers, pharmaceutically acceptable salts or esters, or prodrugs thereof. The compounds of the invention are potent FAAH inhibitors.
摘要翻译：本发明涉及式（I）的化合物，其中A表示任选取代的苯基或含有至多4个选自O，S和N的杂原子的5-或6-元杂芳族环系，B表示单键， O，S或NR 1，其中R 1选自氢或C 1 -C 6烷基; L代表接头; C表示氨基部分; n代表0或1; m代表0,1,2,3,4,5或6; X代表O或S; Y代表氢或任选取代的碳部分; 并涉及其立体异构体，药学上可接受的盐或酯或前药。本发明的化合物是有效的FAAH抑制剂。

15. 发明申请

WO2009136803A3 CATALYTIC PROCESS FOR ASYMMETRIC HYDROGENATION 审中-公开
公开(公告)号：WO2009136803A3
公开(公告)日：2009-11-12
申请号：PCT/PT2009/000025
申请日：2009-05-06
申请人： BIAL - PORTELA & CA., S.A. , BELIAEV, Alexander , LEARMONTH, David Alexander
发明人： BELIAEV, Alexander , LEARMONTH, David Alexander
IPC分类号： C07D311/04
摘要： A process for preparing the S or R enantiomer of a compound of formula (A), the process comprising subjecting a compound of formula (B) to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.

16. 发明申请

WO2009116883A3 CATALYTIC ASYMETRIC HYDROGENATION 审中-公开
公开(公告)号：WO2009116883A3
公开(公告)日：2009-09-24
申请号：PCT/PT2009/000014
申请日：2009-03-17
申请人： BIAL - PORTELA & CA., S. A. , LEARMONTH, David Alexander , BELIAEV, Alexander , LI, Wenge
发明人： LEARMONTH, David Alexander , BELIAEV, Alexander , LI, Wenge
IPC分类号： C01G55/00 , C07D233/84 , C07D311/74 , C07D335/06 , C07D407/04 , C07D409/04
摘要： A process for preparing the S or R enantiomer of a compound of formula A, (see formula (B) and formula (A)), the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral transition metal catalyst and a source of hydrogen.

17. 发明申请

WO2009113891A1 CATALYTIC PROCESS FOR ASYMMETRIC HYDROGENATION 审中-公开
标题翻译：不对称加氢催化工艺
公开(公告)号：WO2009113891A1
公开(公告)日：2009-09-17
申请号：PCT/PT2009/000012
申请日：2009-03-13
申请人： BIAL - PORTELA & CA., S.A. , BELIAEV, Alexander , LEARMONTH, David, Alexander , ALMENA PEREA, Juan José , GEIß, Gerhard , HITZEL, Patrick , KADYROV, Renat , VOIGTLAENDER, David
发明人： BELIAEV, Alexander , LEARMONTH, David, Alexander , ALMENA PEREA, Juan José , GEIß, Gerhard , HITZEL, Patrick , KADYROV, Renat , VOIGTLAENDER, David
IPC分类号： C07D311/04
CPC分类号： C07D311/04
摘要： A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral transition metal catalyst and a source of hydrogen, wherein: X is CH 2 , oxygen or sulphur; R 1 , R 2 and R 3 are the same or different and signify hydrogen, halogen, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R 4 is alkyl or aryl, the transition metal catalyst comprising a chiral ligand having the formula wherein each R and R' independently represents alkyl, aryl, aralkyl, alkenyl, alkynyl, alkoxy, aryloxy, alkylthio, arylthio, unsubstituted or substituted cyclic moiety selected from a group consisting of monocyclic or polycyclic saturated or partially saturated carbocyclic or heterocyclic, aromatic or heteroaromatic rings said rings comprising from 4 to 8 atoms and comprising from 0 to 3 heteroatoms, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means an aromatic or heteraromatic group, optionally substituted one or more times by alkyl, alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.
摘要翻译：一种制备式A化合物的S或R对映异构体的方法，该方法包括在手性过渡金属催化剂和氢源的存在下使式B的化合物进行不对称氢化，其中：X是CH 2，氧或硫磺; R1，R2和R3相同或不同，表示氢，卤素，烷基，烷氧基，羟基，硝基，烷基羰基氨基，烷基氨基或二烷基氨基; 所述过渡金属催化剂包含具有下式的手性配体：其中每个R和R'独立地表示烷基，芳基，芳烷基，烯基，炔基，烷氧基，芳氧基，烷硫基，芳硫基，未取代或取代的环状部分来自由单环或多环饱和或部分饱和的碳环或杂环芳族或杂芳环组成的组，所述环包含4至8个原子并包含0至3个杂原子，其中：术语烷基是指直链或支链的含有 1-6个碳原子，任选被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代; 术语芳基是指芳族或杂芳基，任选被烷基，烷氧基，卤素或硝基取代一次或多次; 术语卤素是指氟，氯，溴或碘。

18. 发明申请

WO2009084970A1 5-O-SUBSTITUTED 3-N-PHENYL-1,3,4-OXADIAZOLONES FOR MEDICAL USE 审中-公开
标题翻译：用于医疗用途的5-O-取代的3-N-苯基-1,3,4-氧杂环丙烷
公开(公告)号：WO2009084970A1
公开(公告)日：2009-07-09
申请号：PCT/PT2008/000054
申请日：2008-12-23
申请人： BIAL-PORTELA & COMPANHIA, S.A. , LEARMONTH, David Alexander , KISS, Laszlo Erno , BELIAEV, Alexander , FERREIRA, Humberto dos Santos , SILVA, Patrício Manuel Vieira Araújo Soares da
发明人： LEARMONTH, David Alexander , KISS, Laszlo Erno , BELIAEV, Alexander , FERREIRA, Humberto dos Santos , SILVA, Patrício Manuel Vieira Araújo Soares da
IPC分类号： C07D413/10 , C07D413/12 , C07D271/113 , A61K31/4245 , A61P25/00 , A61P11/00 , A61P9/00
CPC分类号： C07D413/10 , C07D271/113 , C07D413/12
摘要： The present invention relates to compounds having a 5-O-substituted 3-N-phenyl-1,3,4-oxadiazolone structural unit which have unexpectedly high level of inhibition of FAAH (fatty acid amide hydrolase). (I)
摘要翻译：本发明涉及具有意外高水平的FAAH（脂肪酰胺水解酶）抑制水平的具有5-O-取代的3-N-苯基-1,3,4-恶二酮结构单元的化合物。（一世）

19. 发明申请

WO2009064210A3 PROCESS FOR THE PREPARATION OF 2H-CHROMENE-3-CARBAMATE DERIVATIVES 审中-公开
公开(公告)号：WO2009064210A3
公开(公告)日：2009-05-22
申请号：PCT/PT2008/000048
申请日：2008-11-13
申请人： BIAL - PORTELA & CA., S.A. , BROADBELT, Brian , BELIAEV, Alexander , LEARMONTH, David
发明人： BROADBELT, Brian , BELIAEV, Alexander , LEARMONTH, David
IPC分类号： C07D311/74
摘要： Compounds of formula I, V, VI and II, and processes for their preparation, wherein R 1 , R 2 and R 3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R 4 is alkyl or aryl. There is also provided a process for preparing a compound of formula B from the compounds of formula V and I.

20. 发明申请

WO2008094054A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2008094054A2
公开(公告)日：2008-08-07
申请号：PCT/PT2008000004
申请日：2008-01-31
申请人： PORTELA & CA SA , SOARES DA SILVA PATRICIO MANUE , LEARMONTH DAVID ALEXANDER , BELIAEV ALEXANDER
发明人： SOARES DA SILVA PATRICIO MANUE , LEARMONTH DAVID ALEXANDER , BELIAEV ALEXANDER
IPC分类号： C07D405/04 , A61K31/352 , A61P9/02
CPC分类号： C07D405/04
摘要： This invention relates to new 6,8-difluorochroman-3-yl-1,3-dihydroimidazole-2-thiones, their preparation, and their use as a medicament.
摘要翻译：本发明涉及新的6,8-二氟色素-3-基-1,3-二氢咪唑-2-硫酮，其制备及其作为药物的用途。

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