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1. 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.

2. 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。

3. 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.

4. 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。

5. 发明申请

WO2008143540A1 PROCESS FOR PREPARING CHROMAN DERIVATIVES 审中-公开
标题翻译：制备色氨酸衍生物的方法
公开(公告)号：WO2008143540A1
公开(公告)日：2008-11-27
申请号：PCT/PT2008/000023
申请日：2008-05-21
申请人： BIAL-PORTELA & CA, S.A. , LEARMONTH, David Alexander , BELIAEV, Alexander
发明人： LEARMONTH, David Alexander , BELIAEV, Alexander
IPC分类号： C07D311/22 , C07D311/58
CPC分类号： C07D311/22 , C07D311/58
摘要： A process for preparing a compound of formula (22), comprising reducing a compound of formula (21), to produce a compound of formula (23), followed by the hydrogenolysis of the compound of formula 23 in a solvent comprising a C 1 to C 6 alkyl sulfonic acid and optionally a chlorinated solvent.
摘要翻译：一种制备式（22）化合物的方法，包括还原式（21）化合物，制备式（23）化合物，然后在包含C C 1 -C 6烷基磺酸和任选的氯化溶剂。

6. 发明申请

WO2012087174A3 CRYSTALLINE FORMS AND PROCESSES FOR THEIR PREPARATION 审中-公开
公开(公告)号：WO2012087174A3
公开(公告)日：2012-06-28
申请号：PCT/PT2011/000046
申请日：2011-12-21
申请人： BIAL - PORTELA & Cª., S.A. , 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
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.

7. 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。

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

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。

10. 发明申请

WO2008094056A1 PROCESS FOR THE PREPARATION OF (R) -5- (2-AMINOETHYL) -1- (6, 8 -DI FLUOROCHROMAN- S -YL ) -1, 3-DIHYDROIMIDAZOLE-2-THIONE 审中-公开
标题翻译：制备（R）-5-（2-氨基乙基）-1-（6,7,8-二氟甲基） - 1,3-二氢吲哚-2-酮的方法
公开(公告)号：WO2008094056A1
公开(公告)日：2008-08-07
申请号：PCT/PT2008/000006
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。

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