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1. 发明申请

WO2013002660A3 PROCESS 审中-公开
标题翻译：处理
公开(公告)号：WO2013002660A3
公开(公告)日：2013-05-02
申请号：PCT/PT2012000024
申请日：2012-06-29
申请人： BIAL PORTELA & CA SA , 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-（6,8-二氟色满-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。本发明还涉及制备可用于形成所述化合物的中间体的方法，以及本身涉及中间体的方法。

2. 发明申请

WO2012087174A2 CRYSTALLINE FORMS AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译：晶体形态及其制备方法
公开(公告)号：WO2012087174A2
公开(公告)日：2012-06-28
申请号：PCT/PT2011000046
申请日：2011-12-21
申请人： BIAL PORTELA & CA SA , BELIAEV ALEXANDER , LEARMONTH DAVID ALEXANDER , BROADBELT BRIAN , ALBERT EKATERINA , ANDRES PATRICIA
发明人： BELIAEV ALEXANDER , LEARMONTH DAVID ALEXANDER , BROADBELT BRIAN , ALBERT EKATERINA , ANDRES PATRICIA
IPC分类号： C07D405/04
CPC分类号： C07D405/04
摘要： The present invention relates to crystalline Form A of 1-[(3R)-6,8-difluoro-3,4-dihydro-2H-1-benzopyran-3-yl]-1,3-dihydro-5-[2-[(phenylmethyl)amino]ethyl]-2H-imidazole-2-thione and crystalline Form B of 1-[(3R)-6,8-difluoro-3,4-dihydro-2H-1-benzopyran-3-yl]-1,3-dihydro-5-[2-[(phenylmethyl)amino]ethyl]-2H-imidazole-2-thione, processes for preparing the forms and their uses in medicine. The present invention also relates to the amorphous form of 1-[(3R)-6,8-difluoro-3,4-dihydro-2H-1-benzopyran-3-yl]-1,3-dihydro-5-[2-[(phenylmethyl)amino]ethyl]-2H-imidazole-2-thione processes for preparing it and its uses in medicine.
摘要翻译：本发明涉及1 - [（3R）-6,8-二氟-3,4-二氢-2H-1-苯并吡喃-3-基] -1,3-二氢-5- [2- [（苯基甲基）氨基]乙基] -2H-咪唑-2-硫酮和1 - [（3R）-6,8-二氟-3,4-二氢-2H-1-苯并吡喃-3-基] -1,3-二氢-5- [2 - [（苯基甲基）氨基]乙基] -2H-咪唑-2-硫酮，其制备方法及其在医学上的用途。本发明还涉及无定形形式的1 - [（3R）-6,8-二氟-3,4-二氢-2H-1-苯并吡喃-3-基] -1,3-二氢-5- [2 - [（苯甲基）氨基]乙基] -2H-咪唑-2-硫酮制备方法及其在医药中的用途。

3. 发明申请

WO2009064210A2 PROCESS 审中-公开
标题翻译：处理
公开(公告)号：WO2009064210A2
公开(公告)日：2009-05-22
申请号：PCT/PT2008000048
申请日：2008-11-13
申请人： BIAL PORTELA & CA SA , BROADBELT BRIAN , BELIAEV ALEXANDER , LEARMONTH DAVID
发明人： BROADBELT BRIAN , BELIAEV ALEXANDER , LEARMONTH DAVID
IPC分类号： C07D311/74
CPC分类号： C07D311/04
摘要： Compounds of formula I, V, VI and II, and processes for their preparation, wherein 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. There is also provided a process for preparing a compound of formula B from the compounds of formula V and I.
摘要翻译：式I，V，VI和II的化合物及其制备方法，其中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; R4是烷基或芳基。还提供了由式V和I化合物制备式B化合物的方法。

4. 发明申请

WO2010074588A3 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2010074588A3
公开(公告)日：2011-05-19
申请号：PCT/PT2009000080
申请日：2009-12-23
申请人： BIAL PORTELA & CA SA , KISS LASZLO ERNO , LEARMONTH DAVID ALEXANDER , ROSA CARLA PATRICIA DA COSTA PEREIRA , GUSMAO DE NORONHA RITA , PALMA PEDRO NUNO LEAL , SOARES DA SILVA PATRICIO MANUEL VIEIRA ARAUJO , BELIAEV ALEXANDER
发明人： KISS LASZLO ERNO , LEARMONTH DAVID ALEXANDER , ROSA CARLA PATRICIA DA COSTA PEREIRA , GUSMAO DE NORONHA RITA , PALMA PEDRO NUNO LEAL , SOARES DA SILVA PATRICIO MANUEL VIEIRA ARAUJO , BELIAEV ALEXANDER
IPC分类号： A61P3/00 , A61K31/33
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： The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.
摘要翻译：本发明涉及用于抑制酶脂肪酸酰胺水解酶（FAAH）的化合物和组合物，该化合物在治疗中的用途，特别是用于治疗或预防其发展或症状与FAAH酶底物相连的病症，以及使用化合物和组合物的治疗或预防方法。

5. 发明申请

WO2009116883A2 PROCESS 审中-公开
标题翻译：处理
公开(公告)号：WO2009116883A2
公开(公告)日：2009-09-24
申请号：PCT/PT2009000014
申请日：2009-03-17
申请人： BIAL PORTELA & CA SA , 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
CPC分类号： C07D311/04 , C07D405/04 , C07F15/0053 , C07F15/008
摘要： A process for preparing the S or R enantiomer of a compound of formula A, (B), (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 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 transition metal catalyst comprises a chiral ligand having the formula (I) wherein p is from 1 to 6, and Ar means aryl group; 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 heteroaromatic group, optionally substituted by 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，（B），（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存在下使式B化合物进行不对称氢化，其中：X为CH 2，氧或硫; 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; 并且R 4是烷基或芳基，其中所述过渡金属催化剂包含具有式（I）的手性配体，其中p为1至6，Ar表示芳基; 其中：术语烷基是指含有1-6个碳原子的直链或支链的烃链，任选被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代; 术语芳基是指任选被烷氧基，卤素或硝基取代的芳族或杂芳基; 术语卤素是指氟，氯，溴或碘。

6. 发明申请

WO2010074588A8 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2010074588A8
公开(公告)日：2011-10-06
申请号：PCT/PT2009000080
申请日：2009-12-23
申请人： BIAL PORTELA & CA SA , KISS LASZLO ERNO , LEARMONTH DAVID ALEXANDER , ROSA CARLA PATRICIA DA COSTA PEREIRA , GUSMAO DE NORONHA RITA , PALMA PEDRO NUNO LEAL , SOARES DA SILVA PATRICIO MANUEL VIEIRA ARAUJO , BELIAEV ALEXANDER
发明人： KISS LASZLO ERNO , LEARMONTH DAVID ALEXANDER , ROSA CARLA PATRICIA DA COSTA PEREIRA , GUSMAO DE NORONHA RITA , PALMA PEDRO NUNO LEAL , SOARES DA SILVA PATRICIO MANUEL VIEIRA ARAUJO , BELIAEV ALEXANDER
IPC分类号： A61P3/00 , A61K31/33
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： The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.
摘要翻译：本发明涉及用于抑制脂肪酸酰胺水解酶（FAAH）的化合物和组合物，所述化合物在治疗中的应用，特别是用于治疗或预防其发展或症状与FAAH酶底物相关的病症，以及使用该化合物和组合物治疗或预防的方法。

7. 发明申请

WO2009116883A8 PROCESS 审中-公开
标题翻译：处理
公开(公告)号：WO2009116883A8
公开(公告)日：2009-12-10
申请号：PCT/PT2009000014
申请日：2009-03-17
申请人： BIAL PORTELA & CA SA , 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
CPC分类号： C07D311/04 , C07D405/04 , C07F15/0053 , C07F15/008
摘要： A process for preparing the S or R enantiomer of a compound of formula A, (B), (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 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 transition metal catalyst comprises a chiral ligand having the formula (I) wherein p is from 1 to 6, and Ar means aryl group; 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 heteroaromatic group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.
摘要翻译：制备式A化合物的S或R对映体的方法，（B），（A）包括使式B化合物在手性过渡金属催化剂和氢源存在下进行不对称氢化的方法，其中：X是CH 2，氧或硫; 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; 并且R 4是烷基或芳基，其中所述过渡金属催化剂包含具有式（I）的手性配体，其中p为1至6，Ar表示芳基; 其中：术语烷基是指任选被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代的含有1至6个碳原子的直链或支链烃链; 术语芳基是指任选被烷氧基，卤素或硝基取代的芳族或杂芳族基团; 而术语卤素是指氟，氯，溴或碘。

8. 发明申请

WO2009136803A2 PROCESS 审中-公开
标题翻译：处理
公开(公告)号：WO2009136803A2
公开(公告)日：2009-11-12
申请号：PCT/PT2009000025
申请日：2009-05-06
申请人： BIAL PORTELA & CA SA , BELIAEV ALEXANDER , LEARMONTH DAVID ALEXANDER
发明人： BELIAEV ALEXANDER , LEARMONTH DAVID ALEXANDER
IPC分类号： C07D217/02 , C07D217/24
CPC分类号： C07D405/04 , C07D233/84 , C07D311/04 , C07D487/04
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.
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，该方法包括在手性催化剂和氢源存在下使式（B）化合物进行不对称氢化，其中：X是CH 2 ，氧或硫; 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; 并且R 4是烷基或芳基，其中：术语烷基是指含有1-6个碳原子的直链或支链的烃链，任选地被芳基，烷氧基，卤素，烷氧基羰基或羟基羰基取代; 术语芳基是指任选被烷氧基，卤素或硝基取代的苯基或萘基; 术语卤素是指氟，氯，溴或碘。

9. 发明专利

CA3082337A1 DOPAMINE-B-HYDROXYLASE INHIBITORS 未知
公开(公告)号：CA3082337A1
公开(公告)日：2019-06-13
申请号：CA3082337
申请日：2018-11-30
申请人： BIAL PORTELA & CA SA
发明人： KISS LASZLO ERNO , BELIAEV ALEXANDER , ROSSI TINO , PALMA PEDRO NUNO LEAL , SOARES DA SILVA PATRICIO MANUEL VIEIRA ARAUJO , PINTO RUI , CARDONA FRANCISCO
IPC分类号： C07D487/14 , A61K31/4188 , A61P25/00
摘要： This invention relates to: (a) compounds of formula Ia (with R1, R4 to R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine- ß-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

10. 发明专利

AR109698A1 INHIBIDORES DE DOPAMINA-b-HIDROXILASA 未知
公开(公告)号：AR109698A1
公开(公告)日：2019-01-16
申请号：ARP170102618
申请日：2017-09-22
申请人： BIAL PORTELA & CA SA
发明人： LEAL PALMA PEDRO NUNO , BELIAEV ALEXANDER , KISS LASZLO ERNO , ROSSI TINO , SOARES DA SILVA PATRCIO
IPC分类号： C07D487/04 , A61K31/407 , A61K31/4188 , A61P9/04 , A61P9/12 , A61P25/00
摘要： La presente se refiere a: (a) compuestos de la fórmula Ia (con R¹, R⁴, R⁵, R⁶, n y A como se definen en la presente) y sus sales o solvatos farmacéuticamente aceptables que son de utilidad como inhibidores de la dopamina-b-hidroxilasa; (b) composiciones farmacéuticas que comprenden estos compuestos, sales o solvatos; (c) el uso de estos compuestos, sales o solvatos en terapia; (d) métodos de tratamiento terapéuticos que usan estos compuestos, sales o solvatos; y (e) procesos e intermediarios útiles para la síntesis de tales compuestos. Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales o solvatos farmacéuticamente aceptables, en donde: R¹ es hidrógeno, alquilo C₁₋₆, alquilo C₁₋₆ parcial o totalmente deuterado, cicloalquilo C₃₋₆, cianoalquilo C₂₋₆, mercaptoalquilo C₁₋₆ o amino; R⁴ es hidrógeno o alquilo C₁₋₃; R⁵ es hidrógeno o alquilo C₁₋₂; o R⁴ y R⁵ se combinan, junto con el átomo de carbono al que se adjuntan, para formar un anillo ciclopropilo en donde el resto de CH₂ está opcionalmente sustituido con dos átomos de deuterio; R⁶ es alquilo C₁₋₆ o alquilo C₁₋₆ parcial o totalmente deuterado; A es cicloalquilo C₅₋₇, furanilo, tiofenilo, metiltiofenilo o un resto de fórmula (2), en donde: X¹ es hidrógeno, halo o metilo; X¹’ es hidrógeno o halo; X² es hidrógeno, halo o metilo; X²’ es hidrógeno o halo; X³ es hidrógeno o fluoro; n es 0 ó 1 y cuando n es 0 un enlace simple se une con los átomos de carbono a los que el resto de CH₂ se uniría cuando n es 1.

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