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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

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

WO2008094055A1 PROCESS FOR THE PREPARATION OF (R) -5- (2-AMINOETHYL) -1- (6, 8-DIFLUOROCHROMAN-3-YL) -1, 3-DIHYDROIMIDAZOLE-2-THIONE 审中-公开
标题翻译：制备（R）-5-（2-氨基乙基）-1-（6,8-二氟-3-三氟甲基）-1,3-二氢吲哚-2-酮的方法
公开(公告)号：WO2008094055A1
公开(公告)日：2008-08-07
申请号：PCT/PT2008/000005
申请日：2008-01-31
申请人： PORTELA & CA., S.A. , SOARES DA SILVA, Patrício Manuel Vieira Araújo , BELIAEV, Alexander , LEARMONTH, David Alexander
发明人： SOARES DA SILVA, Patrício Manuel Vieira Araújo , BELIAEV, Alexander , LEARMONTH, David Alexander
IPC分类号： C07D405/04
CPC分类号： C07D405/04
摘要： A process for making (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione and pharmaceutically acceptable salts thereof, and for making intermediates useful in the formation of said compound.
摘要翻译：制备（R）-5-（2-氨基乙基）-1-（6,8-二氟色素-3-基）-1,3-二氢咪唑-2-硫酮及其药学上可接受的盐，以及制备中间体的方法在所述化合物的形成中。

5. 发明申请

WO2004099153A1 METHOD FOR RACEMISATION OF (S)-(+)- AND (R)-(-)-10,11-DIHYDRO-10-HYDROXY-5HDIBENZ/B,F/AZEPINE-5-CARBOXAMIDE AND OPTICALLY ENRICHED MIXTURES THEREOF 审中-公开
标题翻译：（S） - （+） - 和（R） - （ - ） - 10,11-二氢-10-羟基-5H-二苯并/ B，F / AZEPINE-5-羧酰胺和其光学强化混合物
公开(公告)号：WO2004099153A1
公开(公告)日：2004-11-18
申请号：PCT/GB2004/001997
申请日：2004-05-11
申请人： PORTELA & C.A., S.A. , LEARMONTH, David, Alexander
发明人： LEARMONTH, David, Alexander
IPC分类号： C07D223/28
CPC分类号： C07D223/28
摘要： A high-yielding method for racemisation of (S)-(+)- and (R)-(-)-10, 11- dihydro-l0-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide and a useful intermediate, 10-chloro-10, 11 dihydro-5H-dibenz/b,f/azepine-5-carboxamide (VII) are disclosed. Also disclosed are methods for the racemisation of optically pure or optically enriched mixtures of (S)-(+)-10,11-dihydro-l0-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (I) and (R)-(-)-10,11-dihydro-l0-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (II) to racemic (±)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (III).
摘要翻译：（S） - （+） - 和（R） - （ - ） - 10,11-二氢-10-羟基-5H-二苯并/ b，f /氮杂-5-甲酰胺的外消旋化的高产率方法和有用的中间体，10-氯-10,11-二氢-5H-二苯并[b，f]吖庚因-5-甲酰胺（Ⅶ）。还公开了（S） - （+） - 10,11-二氢-10-羟基-5H-二苯并/ b，f /吖庚因-5-甲酰胺（I）的光学纯的或光学富集的混合物的外消旋化的方法（R） - （ - ） - 10,11-二氢-10-羟基-5H-二苯并/ b，f /氮杂-5-甲酰胺（II）与外消旋的（±）-10,11-二氢-10-羟基 - 5H-二苯并/ b，f /氮杂-5-甲酰胺（III）。

6. 发明申请

WO2009116882A1 CRYSTAL FORMS OF 5- [3- (2, 5-DICHLORO-4, 6-DIMETHYL-1-OXY-PYRIDINE-3-YL) [1,2,3] OXADIAZOL-5-YL] -3-NIT ROBENZENE-1, 2-DIOL 审中-公开
标题翻译： 5- [3-（2,5-二氯-4,6-二甲基-1-氧代 - 吡啶-3-基）[1,2,3]氧杂双环-5-YL] -3-硝基苯并噻吩的晶体形式 1，2-DIOL
公开(公告)号：WO2009116882A1
公开(公告)日：2009-09-24
申请号：PCT/PT2009/000013
申请日：2009-03-16
申请人： PORTELA & CA., S.A. , LEARMONTH, David Alexander , LORIMER, Keith , MEYER, Kevin Wayne , ESZENYI, Tibor , KOVÁCH, Álmosné
发明人： LEARMONTH, David Alexander , LORIMER, Keith , MEYER, Kevin Wayne , ESZENYI, Tibor , KOVÁCH, Álmosné
IPC分类号： C07D413/04 , A61K31/4439 , A61P25/16
CPC分类号： C07D413/04 , C07B2200/13
摘要： This invention relates to novel polymorphs of (HO) 2 NO 2 (C 6 H)-(C 2 N 2 O)- (C 5 N)(CH 3 ) 2 Cl 2 O, to processes for their preparation, and to pharmaceutical compositions containing said novel polymorphs as active pharmaceutical ingredient.
摘要翻译：本发明涉及（HO）2 O 2（C 6 H） - （C 2 N 2 O） - （C 5 N）（CH 3）2 Cl 2 O）的新型多晶型物，以及含有所述新型多晶型物作为活性药物成分的药物组合物。

7. 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。

8. 发明申请

WO2008094054A3 6, 8-DICHLORCHROMAN-3-YL-L, 3-DIHYDROIMIDAZOLE-2-THIONE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS 审中-公开
公开(公告)号：WO2008094054A3
公开(公告)日：2008-08-07
申请号：PCT/PT2008/000004
申请日：2008-01-31
申请人： PORTELA & CA., S.A. , SOARES DA SILVA, Patrício Manuel Vieira Araújo , LEARMONTH, David Alexander , BELIAEV, Alexander
发明人： SOARES DA SILVA, Patrício Manuel Vieira Araújo , LEARMONTH, David Alexander , BELIAEV, Alexander
IPC分类号： C07D405/04 , A61K31/352 , A61P9/02
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.

9. 发明申请

WO2007117165A1 NEW PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：新药物化合物
公开(公告)号：WO2007117165A1
公开(公告)日：2007-10-18
申请号：PCT/PT2007/000016
申请日：2007-04-10
申请人： PORTELA & CA. S.A. , LEARMONTH, David, Alexander , KISS, Laszlo, Erno , LEAL PALMA, Pedro, Nuno , DOS SANTOS FERREIRA, Humberto , ARAÚJO SOARES DA SILVA, Patrício, Manuel, Vieira
发明人： LEARMONTH, David, Alexander , KISS, Laszlo, Erno , LEAL PALMA, Pedro, Nuno , DOS SANTOS FERREIRA, Humberto , ARAÚJO SOARES DA SILVA, Patrício, Manuel, Vieira
IPC分类号： C07D213/26 , C07D213/57 , C07D401/04 , C07D407/04 , C07D417/04 , A61K31/506 , A61K31/4439 , A61P25/16
CPC分类号： A61K31/198 , A61K31/4439 , C07D213/26 , C07D213/57 , C07D213/82 , C07D401/04 , C07D407/04 , C07D413/04 , C07D417/04 , A61K2300/00
摘要： This invention relates to novel substituted nitrocatechol derivatives, their use in the treatment of some central and peripheral nervous system disorders and pharmaceutical compositions containing them.
摘要翻译：本发明涉及新的取代的硝基儿茶酚衍生物，它们用于治疗一些中枢和周围神经系统障碍以及含有它们的药物组合物。

10. 发明申请

WO2007081232A1 DRUG COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2007081232A1
公开(公告)日：2007-07-19
申请号：PCT/PT2007/000002
申请日：2007-01-15
申请人： PORTELA & CA., S.A. , LEARMONTH, David Alexander , BELIAEV, Alexander , SOARES DA SILVA, Patrício Manuel Vieira Araújo
发明人： LEARMONTH, David Alexander , BELIAEV, Alexander , SOARES DA SILVA, Patrício Manuel Vieira Araújo
IPC分类号： A61K31/4164 , A61P43/00
CPC分类号： A61K31/4164
摘要： A combination comprising at least two components selected from: (i) compounds of formula I: R where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X signifies CH2, oxygen atom or sulphur atom; n is 1, 2 or 3, with the proviso that when n is 1, X is not CH2; and the individual (R)- and (S)-enantiomers or mixtures of enantiomers and pharmaceutically acceptable salts thereof; 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 hydroxy carbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; the term halogen means fluorine, chlorine, bromine or iodine; and (ii) at least one compound from the following classes of compounds: diuretics; beta-adrenergic antagonists; alpha2-adrenergic agonists; alphal -adrenergic antagonists; dual beta- and alpha-adrenergic antagonists; calcium channel blockers; potassium channel activators; anti-arrhythmics; ACE inhibitors; ATI receptor antagonists; renin inhibitors; lipid lowerers, vasopeptidase inhibitors; nitrates; endothelin antagonists; neutral endopeptidase inhibitors; anti-angiotensin vaccines; vasodilators; phosphodiesterase inhibitors; cardiac glycosides; serotonin antagonists; and CNS acting agents.
摘要翻译：卤素，烷基，烷氧基，羟基，硝基，氨基，烷基羰基氨基，烷基氨基或烷基氨基，其中R 1，R 2和R 3相同或不同，表示氢，二烷基氨基 R4表示氢，烷基或烷基芳基; X表示CH2，氧原子或硫原子; n为1,2或3，条件是当n为1时，X不为CH2; 和（S） - 对映异构体或其对映异构体及其药学上可接受的盐的混合物; 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，卤素或硝基取代的苯基或萘基; 术语卤素是指氟，氯，溴或碘; 和（ii）至少一种下列化合物类型的化合物：利尿剂; β-肾上腺素能拮抗剂; α2-肾上腺素能激动剂; α-肾上腺素能拮抗剂; 双重β-和α-肾上腺素能拮抗剂; 钙通道阻滞剂; 钾通道激活剂; 抗心律失常药; ACE抑制剂; ATI受体拮抗剂; 肾素抑制剂; 脂质降低剂，血管肽酶抑制剂; 硝酸盐; 内皮素拮抗剂; 中性内肽酶抑制剂; 抗血管紧张素疫苗; 血管扩张剂; 磷酸二酯酶抑制剂; 强心苷; 5-羟色胺拮抗剂和CNS代理。

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