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1. 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。

2. 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.

3. 发明申请

WO2008088233A1 THERAPEUTICAL USES OF ESLICARBAZEPINE 审中-公开
标题翻译：西妥昔单抗的治疗用途
公开(公告)号：WO2008088233A1
公开(公告)日：2008-07-24
申请号：PCT/PT2008/000002
申请日：2008-01-14
申请人： PORTELA & CA., S.A. , SOARES DA SILVA, Patrício Manuel Vieira Araújo
发明人： SOARES DA SILVA, Patrício Manuel Vieira Araújo
IPC分类号： A61P25/08 , A61P25/04 , A61P25/28 , A61P25/18 , A61K31/55 , A61K45/06
CPC分类号： A61K31/55 , A61K45/06 , A61K2300/00
摘要： New applications of eslicarbazepine and eslicarbazepine acetate in the treatment of intractable conditions, selected from epilepsy, central and peripheric nervous system disorders, affective disorders, schizoaffective disorders, bipolar disorders, attention disorders, anxiety disorders, neurophatic pain and neuropathic pain- related disorders, sensorimotor disorders, vestibular disorders, and nervous function alterations in degenerative and post-ischemic diseases. Preferably the intractable condition is, at least in part, caused by an overexpression of P-gp or MRP.
摘要翻译： eslicarbazepine和eslicarbazepine acetate的新应用治疗难治性疾病，选自癫痫，中枢和周围神经系统疾病，情感障碍，分裂情感障碍，双相情感障碍，注意力障碍，焦虑症，神经性疼痛和神经性疼痛相关疾病，感觉运动疾病，前庭障碍和退行性和缺血后疾病中的神经功能改变。优选地，难治性病症至少部分地由P-gp或MRP的过度表达引起。

4. 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。

5. 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。

6. 发明申请

WO2006120501A1 METHODS OF PREPARING PHARMACEUTICAL COMPOSITIONS COMPRISING ESLICARBAZEPINE ACETATE AND METHODS OF USE 审中-公开
标题翻译：制备包含醋酸异丙酯的药物组合物的方法和使用方法
公开(公告)号：WO2006120501A1
公开(公告)日：2006-11-16
申请号：PCT/IB2005/002357
申请日：2005-05-06
申请人： PORTELA & C.A., S.A. , ALMEIDA, Jose, Luis , SOARES DA SILVA, Patrício, Manuel, Vieira, Araújo
发明人： ALMEIDA, Jose, Luis , SOARES DA SILVA, Patrício, Manuel, Vieira, Araújo
IPC分类号： A61K9/00 , A61K31/55
CPC分类号： A61K31/55 , A61K9/0053
摘要： The present disclosure relates to the treatment of various diseases and conditions with eslicarbazepine acetate. The present disclosure also relates to the use of eslicarbazepine acetate in a method for reducing or decreasing epileptic seizures in a patient. The present disclosure also relates to a method for increasing the exposure to eslicarbazepine in a patient. The present disclosure also relates to a method of preparing a pharmaceutical composition comprising eslicarbazepine acetate.
摘要翻译：本公开涉及用醋酸西酞替啶治疗各种疾病和病症。本公开还涉及醋酸西酞西泮在减少或减少患者癫痫发作的方法中的用途。本公开还涉及用于增加患者中西酞普兰暴露的方法。本公开还涉及制备包含醋酸巴西平的药物组合物的方法。

7. 发明申请

WO2013032351A1 TREATMENTS INVOLVING ESLICARBAZEPINE ACETATE OR ESLICARBAZEPINE 审中-公开
标题翻译：涉及醋酸乙酯或精氨酸的治疗
公开(公告)号：WO2013032351A1
公开(公告)日：2013-03-07
申请号：PCT/PT2012/000031
申请日：2012-08-24
申请人： BIAL - PORTELA & Cª, S.A. , SOARES DA SILVA, Patrício Manuel Vieira Araújo
发明人： SOARES DA SILVA, Patrício Manuel Vieira Araújo
IPC分类号： A61K31/55 , A61P25/00 , A61P25/08 , A61P25/04 , A61P25/28 , A61P25/55
CPC分类号： A61K31/55 , A61K31/195 , A61K31/4166 , A61K31/4535 , A61K31/515 , A61K45/06 , A61K2300/00
摘要： The invention provides a drug selected from eslicarbazepine acetate and eslicarbazepine, for use in treating or preventing a disorder selected from epilepsy, affective disorders, schizoaffective disorders, bipolar disorders, neuropathic pain and neuropathic pain related disorders, attention disorders, anxiety disorders, sensorimotor disorders, vestibular disorders, and fibromyalgia, in a patient suffering from or susceptible to absence seizures..
摘要翻译：本发明提供了一种选自醋酸西拉西平和西拉西平的药物，用于治疗或预防选自癫痫，情感障碍，分裂情感障碍，双相情感障碍，神经性疼痛和神经性疼痛相关疾病，注意障碍，焦虑症，感觉运动障碍，前庭疾病和纤维肌痛，患有或不易癫痫发作的患者。

8. 发明申请

WO2008136695A1 1, 3-DIHYDROIMIDAZOLE- 2 -THIONE DERIVATIVES AS INHIBITORS OF DOPAMINE-BETA-HYDROXYLASE 审中-公开
标题翻译：作为多巴胺-β-羟基酶的抑制剂的1,3-二氢吲哚-2-酮衍生物
公开(公告)号：WO2008136695A1
公开(公告)日：2008-11-13
申请号：PCT/PT2008/000019
申请日：2008-05-06
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 , A61K31/4178 , A61P25/22
CPC分类号： C07D405/04 , A61K31/4178 , A61K45/06
摘要： Compounds of formula I and a method for their preparation are described, where R 1 , R 2 and R 3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R 4 signifies -alkyl-aryl or alkyl heteroaryl;X signifies CH 2 , oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.
摘要翻译：描述式I化合物及其制备方法，其中R 1，R 2和R 3 3相同或不同，表示氢，卤素，烷基，硝基，氨基，烷基羰基氨基，烷基氨基或二烷基氨基; R 4表示烷基 - 芳基或烷基杂芳基; X表示CH 2，氧原子或硫原子; n为2或3; 包括单体（R） - 和（S） - 对映异构体或其对映异构体的混合物; 并且包括其药学上可接受的盐和酯。这些化合物具有用于治疗心血管疾病如高血压和慢性心力衰竭的潜在有价值的药物性质。

9. 发明申请

WO2008085074A3 1, 3-DIHYDROIMIDAZOLES FOR TREATING CARDIOVASCULAR DISORDERS 审中-公开
公开(公告)号：WO2008085074A3
公开(公告)日：2008-07-17
申请号：PCT/PT2008/000001
申请日：2008-01-10
申请人： PORTELA & CA., S.A. , SOARES DA SILVA, Patrício Manuel Vieira Araújo
发明人： SOARES DA SILVA, Patrício Manuel Vieira Araújo
IPC分类号： A61P9/04 , A61P9/06 , A61P9/10 , A61P25/06 , A61P25/22 , A61K31/4164 , A61K31/4178 , A61K45/06
摘要： Use of a compound of formula I, where R 1 , R 2 and R 3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R 4 signifies hydrogen, alkyl or alkylaryl group; X signifies CH 2 , oxygen atom or sulphur atom; n is 1, 2 or 3, with the proviso that when n is 1, X is not CH 2 ; 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 hydroxycarbonyl 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, in the manufacture of a medicament for the treatment of one or more of the following indications congestive heart failure, angina, arrhythmias, circulatory disorders such as Raynaud's Phenomenon, migraine, and anxiety disorders.

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