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51. 发明申请

WO2009010491A1 6-PHENYL-1H-IMIDAZO[4,5-C]PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN INHIBITORS 审中-公开
标题翻译： 6-苯基-1H-咪唑并[4,5-C]吡啶-4-羰基酮衍生物作为CATHEPSIN抑制剂
公开(公告)号：WO2009010491A1
公开(公告)日：2009-01-22
申请号：PCT/EP2008/059172
申请日：2008-07-14
申请人： N.V. ORGANON , CAI, Jiaqiang , RANKOVIC, Zoran , JONES, Philip, Stephen , BENNETT, David, Jonathan , FRADERA, Xavier
发明人： CAI, Jiaqiang , RANKOVIC, Zoran , JONES, Philip, Stephen , BENNETT, David, Jonathan , FRADERA, Xavier
IPC分类号： C07D471/04 , A61K31/437 , A61P19/00 , A61P17/00 , A61P29/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I), to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such asatherosclerosis,obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer,and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式（I）的6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物，涉及包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖，炎症和免疫疾病如类风湿性关节炎，牛皮癣，癌症和慢性疼痛如神经性疼痛的药物。

52. 发明申请

WO2008138389A1 A METHOD OF PREPARATION OF QUATERNARY NITROGEN COMPOUNDS 审中-公开
标题翻译：一种制备季铵化合物的方法
公开(公告)号：WO2008138389A1
公开(公告)日：2008-11-20
申请号：PCT/EP2007/054478
申请日：2007-05-09
申请人： N.V. ORGANON , WIEGERINCK, Peter Hermanus Gerardus , KASPERSEN, Franciscus Michael , WESTERDUIN, Pieter , OVERKLEEFT, Herman, Steven , MAREL VAN DER, Gijbert Arie , LUIJENDIJK, Jacob Bastiaan
发明人： WIEGERINCK, Peter Hermanus Gerardus , KASPERSEN, Franciscus Michael , WESTERDUIN, Pieter , OVERKLEEFT, Herman, Steven , MAREL VAN DER, Gijbert Arie , LUIJENDIJK, Jacob Bastiaan
IPC分类号： C07C209/00 , C07H1/00 , C07H3/10 , C07H7/033 , C07H19/23
CPC分类号： C07H19/23 , C07H1/00 , C07H3/10 , C07H7/033
摘要： The invention relates to a method of preparation of a quaternary amine having formula 2, by reacting an epoxide having formula 3, Formula 3 with an aliphatic tertiairy amine group in the presence of a suitable Lewis acid.
摘要翻译：本发明涉及一种制备具有式2的季胺的方法，该方法是通过在合适的路易斯酸存在下使具有式3，式3的环氧化物与脂族叔胺基团进行反应。

53. 发明申请

WO2008125578A2 A METHOD FOR THE PREPARATION OF AN ENANTIOMER OF A TETRACYCLIC BENZAZEPINE 审中-公开
标题翻译：一种制备四羧酸苯并噻唑类化合物的方法
公开(公告)号：WO2008125578A2
公开(公告)日：2008-10-23
申请号：PCT/EP2008/054316
申请日：2008-04-10
申请人： N.V. ORGANON , KEMPERMAN, Gerardus Johannes
发明人： KEMPERMAN, Gerardus Johannes
IPC分类号： C07D471/14
CPC分类号： C07D471/14
摘要： The present invention relates to a method for the preparation of mirtazapine and tetracyclic analogous compounds having substantial enantiomeric excess of the R or S form. The invention further relates to a novel intermediate and its use for the preparation of mirtazapine having a substantial enantiomeric excess of the R or S form. The method comprising the steps of a: providing a carboxylic acid compound according to Formula (I) having a substantial enantiomeric excess of the R or S form, b: converting the carboxylic acid group of compound I into a ketone group, producing a ketone compound of Formula (II), c: optionally reducing ketone compound II with a mild reduction agent to form the intermediate hydroxy compound of Formula (III) and d: forming the mirtazapine of Formula (IV) by reduction of the ketone compound II or of the hydroxy compound III using a strong reduction agent.
摘要翻译：本发明涉及制备具有R或S形式的显着对映体过量的米氮平和四环类似物的方法。本发明还涉及一种新的中间体及其用于制备具有R或S形式的基本对映体过量的米氮平的用途。该方法包括以下步骤：a）提供具有R或S形式的基本对映异构体过量的式（I）的羧酸化合物，b：将化合物I的羧酸基团转化为酮基，产生酮化合物式（II）的化合物，c：任选地用温和的还原剂还原酮化合物II以形成式（III）的中间体羟基化合物，和d：通过还原酮化合物II或式羟基化合物III使用强还原剂。

54. 发明申请

WO2008101995A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO2008101995A1
公开(公告)日：2008-08-28
申请号：PCT/EP2008/052141
申请日：2008-02-21
申请人： N.V. ORGANON , ADAM, Julia
发明人： ADAM, Julia
IPC分类号： C07D413/04 , C07D417/04 , A61K31/425 , A61K31/433 , A61K31/4245 , A61P29/00
CPC分类号： C07D417/04 , C07D413/04
摘要： The invention relates to indole derivative having the general Formula (I) wherein A represents a 5-membered aromatic heterocyclic ring, wherein X 1 , X 2 and X 3 are independently selected from N, O, S and CH;Y represents CH 2 , O, S or SO 2 ;R 1 is H, (C 1-4 )-alkyl, (C 1-4 )alkyloxy, CN orhalogen;R 2 , R 2 ', R 3 , R 3 ', R 4 ,R 4 ', R 5 and R 5 ' are independently hydrogen, (C 1-4 )alkyl (optionally substituted with OH) or CO-OR 8 ; orone pair of geminal substituents R 3 and R 3 ' or R 5 and R 5 ' together represent a keto group, and the others are all hydrogen or (C 1-4 )alkyl; or R 2 and R 5 together represent a methylene or an ethylene bridge, and R 2 '2, R 3 , R 3 ', R 4 , R 4 ' and R 5 ' are hydrogen; n is 1 or 2; R 6 is H, (C 1-4 )alkyl (optionally substituted with OH, (C 1-4 )alkyloxy, CO-NR 9 R 10 , CO-OR 11 or 1,2,4-oxadiazol-3-yl), SO 2 NR 12 R 13 or COOR 14 ; R 7 is H or halogen; R 8 is (C 1-4 )alkyl; R 9 and R 10 are independently hydrogen, (C 1-4 )alkyl or (C 3-7 )cycloalkyl, the alkyl groups being optionally substituted with OH or (C 1-4 )alkyloxy; R 11 is H or (C 1-4 )alkyl; R 12 and R 13 are independently H or (C 1-4 )alkyl; R 14 is (C 1-6 )alkyl; or a pharmaceutically acceptable salt thereof,as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
摘要翻译：本发明涉及具有通式（I）的吲哚衍生物，其中A表示5元芳族杂环，其中X 1，X 2和X 3 独立地选自N，O，S和CH; Y表示CH 2，O，S或SO 2; R 1 8 ; 一对偕取代基R 3和R 3或R 5和R 5一起代表酮基基团，其余全部是氢或（C 1-4烷基）烷基; 或R 2和R 5一起表示亚甲基或乙烯桥，R 2'2，R 3

55. 发明申请

WO2008065142A1 STABILIZED SOLUTION OF ROCURONIUM COMPRISING A SULFOALKYL-ETHER-BETA-CYCLODEXTRIN DERIVATIVE 审中-公开
标题翻译：包含硫代甲基 - β-环糊精衍生物的硫酸钠的稳定溶液
公开(公告)号：WO2008065142A1
公开(公告)日：2008-06-05
申请号：PCT/EP2007/062958
申请日：2007-11-28
申请人： N.V. ORGANON , VROMANS, Herman , DE RONDE, Hendrikus, A.G.
发明人： VROMANS, Herman , DE RONDE, Hendrikus, A.G.
IPC分类号： A61K31/58 , A61K9/00 , A61K9/08 , A61K47/40
CPC分类号： A61K9/0019
摘要： The present invention relates to a pharmaceutical composition in the form of an aqueous solution for parenteral administration comprising rocuronium and a sulfoalkylether-ß-cyclodextrin derivative or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及用于肠胃外给药的水溶液形式的药物组合物，其包含罗库溴铵和磺基烷基醚-β-环糊精衍生物或其药学上可接受的盐。

56. 发明申请

WO2008058923A2 A SYSTEM AND METHOD TO IDENTIFY THE METABOLITES OF A DRUG 审中-公开
标题翻译：鉴定药物代谢物的系统和方法
公开(公告)号：WO2008058923A2
公开(公告)日：2008-05-22
申请号：PCT/EP2007/062199
申请日：2007-11-12
申请人： N.V. ORGANON , RIDDER, Lars. Olaf , WAGENER, Markus , LOMMERSE, Johannes, Petrus, Maria
发明人： RIDDER, Lars. Olaf , WAGENER, Markus , LOMMERSE, Johannes, Petrus, Maria
IPC分类号： G06F19/00
CPC分类号： G06F19/702 , G06F19/12 , G06F19/703
摘要： The invention provides for a method for predicting potential metabolites for a compound, comprising the steps of receiving a target compound from a user applying a set of optimized reaction rules to said target compound to generate a list of potential metabolites and calculating a probability score for each product compound on said list of potential metabolites. The reaction set is optimized by starting from a starting set of reaction rules and replacing at least one reaction rule for a reaction center in said starting set of reaction rules by one, or preferably two or more new rules, which are defined to apply to a reaction of said reaction center, but now specifying or differentiating based on the structural environments of said reaction center, if at least one of said new rules has a higher probability score than the replaced reaction rule when the starting set of reaction rules and the optimized set of reaction rules are both tested with a database of known metabolites of compounds.
摘要翻译：本发明提供了一种用于预测化合物的潜在代谢物的方法，包括以下步骤：从使用者接收目标化合物，将一组优化的反应规则应用于所述目标化合物以产生潜在代谢物的列表，并计算每个产物化合物列在可能的代谢物列表上。通过从起始的反应规则集合开始并且将所述起始反应规则中的反应中心的至少一个反应规则替换为一个或优选两个或更多个新的规则来优化反应集合，其被定义为适用于所述反应中心的反应，但是现在基于所述反应中心的结构环境来指定或区分，如果所述新规则中的至少一个在反应规则和优化集合的起始集合上具有比替换的反应规则更高的概率得分的反应规则都用已知的化合物代谢物的数据库进行测试。

57. 发明申请

WO2008049785A1 IH CHANNEL INHIBITORS FOR THE PROMOTION OF WAKEFULNESS 审中-公开
标题翻译： IH通道抑制剂促进有害性
公开(公告)号：WO2008049785A1
公开(公告)日：2008-05-02
申请号：PCT/EP2007/061168
申请日：2007-10-18
申请人： N.V. ORGANON , WARD, Nicholas Matthew , RUIGT, Gerardus, Stephanus, Franciscus , MARSTON, Hugh
发明人： WARD, Nicholas Matthew , RUIGT, Gerardus, Stephanus, Franciscus , MARSTON, Hugh
IPC分类号： A61K31/4168 , A61K31/423 , A61K31/55 , A61P25/26
CPC分类号： A61K31/55 , A61K31/00 , A61K31/4168 , A61K31/423
摘要： The present invention relates to use of an l h channel inhibitor for the manufacture of a medicament for the promotion of wakefulness in a subject in need thereof, in particular, wherein the subject is suffering from excessive sleepiness which may result from a sleep disorder.
摘要翻译：本发明涉及用于制造用于促进有需要的受试者的觉醒的药物的特异性通道抑制剂，特别是其中受试者患有过度嗜睡，其可能由睡眠障碍引起。

58. 发明申请

WO2007082890A1 SELECTIVE ENZYMATIC HYDROLYSIS OF C-TERMINAL tert-BUTYL ESTERS OF PEPTIDES 审中-公开
标题翻译：肽末端叔丁基酯的选择性酶水解
公开(公告)号：WO2007082890A1
公开(公告)日：2007-07-26
申请号：PCT/EP2007/050409
申请日：2007-01-16
申请人： N.V. ORGANON , EGGEN, Ivo, Franci , BOERIU, Carmen, G.
发明人： EGGEN, Ivo, Franci , BOERIU, Carmen, G.
IPC分类号： C07K1/02 , C07K1/06
CPC分类号： C07K1/023
摘要： The present invention relates to a process for the selective enzymatic hydrolysis of C-terminal esters of peptide substrates in the synthesis of peptides, comprising hydrolysing C-terminal tert -butyl esters using the protease subtilisin. This process is useful in the production of protected or unprotected peptides.
摘要翻译：本发明涉及肽合成中肽底物的C末端酯选择性酶水解的方法，包括使用蛋白酶枯草杆菌蛋白酶水解C末端叔丁基酯。该方法在生产受保护或未受保护的肽中是有用的。

59. 发明申请

WO2007054474A1 2-(BENZIMIDAZOL-1-YL)-N-(4-PHENYLTHIAZOL-2-YL) ACETAMIDE DERIVATIVES USEFUL IN TREATMENT OF TRPV1 RELATED DISORDERS 审中-公开
标题翻译：用于治疗TRPV1相关疾病的2-（苯并咪唑-1-基）-N-（4-苯乙烯基-2-基）乙酰胺衍生物
公开(公告)号：WO2007054474A1
公开(公告)日：2007-05-18
申请号：PCT/EP2006/068109
申请日：2006-11-06
申请人： N.V. ORGANON , PALIN, Ronald , GRAY, Colin Alasdair
发明人： PALIN, Ronald , GRAY, Colin Alasdair
IPC分类号： C07D417/12 , A61K31/427
CPC分类号： C07D417/12
摘要： The invention relates to 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives having the general Formula (I) wherein R 1 is H, (C 1-4 )alkyl, (C 1-4 )alkyloxy or halogen; R 2 represents 1-3 substituents selected from H, (C 1-4 )alkyl (optionally substituted with 1 or more halogens), (C 1-4 )alkyloxy (optionally substituted with 1 or more halogens), halogen, CF 3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives in the treatment of TRPV1 mediated disorders.
摘要翻译：本发明涉及具有通式（I）的2-（苯并咪唑-1-基）-N-（4-苯基噻唑-2-基）乙酰胺衍生物，其中R 1是H，（C < （C 1-4）烷氧基或卤素;（C 1-4）烷氧基或卤素; R 2表示1-3个选自H，（C 1-4烷基）烷基（任选被1个或多个卤素取代）的取代基，（C 1-4）烷氧基（任选被一个或多个卤素取代），卤素，CF 3或氰基; 或其药学上可接受的盐; 涉及包含其的药物组合物和所述2-（苯并咪唑-1-基）-N-（4-苯基噻唑-2-基）乙酰胺衍生物在治疗TRPV1介导的病症中的用途。

60. 发明申请

WO2007042469A2 ANTITHROMBOTIC DUAL INHIBITORS COMPRISING A BIOTIN LABEL 审中-公开
标题翻译：抗生素双重抑制剂包含生物标签
公开(公告)号：WO2007042469A2
公开(公告)日：2007-04-19
申请号：PCT/EP2006/067127
申请日：2006-10-06
申请人： N.V. ORGANON , DE KORT, Martin , VAN BOECKEL, Constant, Adriaan, Anton , NICHOLSON, Charles, David
发明人： DE KORT, Martin , VAN BOECKEL, Constant, Adriaan, Anton , NICHOLSON, Charles, David
IPC分类号： A61K47/48 , C07H15/26 , A61P7/02
CPC分类号： C07H15/26 , A61K47/60 , A61K47/61 , A61K47/65 , A61K47/665 , B82Y5/00
摘要： The present invention relates compounds of the formula: oligosaccharide-spacer-(GpIIb/IIIa antagonist), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising four to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is a bond or an essentially pharmacologically inactive linking residue; the GpIIb/IIIa antagonist is a residue mimicking the RGD and/or K(QA)GD fragment of fibrinogen, comprising a carboxylate moiety and a basic moiety located within the residue at a distance of 10-20 Å from each other; or a pharmaceutically acceptable salt thereof or a prodrug or a solvate thereof; wherein the compound of formula I further comprises at least one covalent bond with a biotin label or an analogue thereof. The compounds of the invention have antithrombotic activity and can be used in treating or preventing thrombotic diseases. The antithrombotic activity of the compound of this invention can be neutralized in case of emergency upon adminstration of avidin, streptavidin and analogues thereof having high biotin affinity.
摘要翻译：本发明涉及下式的寡糖 - 间隔基（GpIIb / IIIa拮抗剂）的化合物，其中寡糖是包含4至25个单糖单元的带负电荷的寡糖残基，该电荷通过带正电荷的抗衡离子补偿，并且其中寡糖残基衍生自具有（AT-III介导的）抗Xa活性本身的寡糖; 间隔基是键或基本上药理学上无活性的连接残基; GpIIb / IIIa拮抗剂是模拟纤维蛋白原的RGD和/或K（QA）GD片段的残基，其包含彼此间隔10-20处的残基中的羧酸盐部分和碱性部分; 或其药学上可接受的盐或其前药或溶剂合物; 其中式I化合物还包含与生物素标记或其类似物的至少一个共价键。本发明化合物具有抗血栓形成活性，可用于治疗或预防血栓形成疾病。在施用具有高生物素亲和力的抗生物素蛋白，链霉抗生物素蛋白及其类似物的紧急情况下，本发明化合物的抗血栓形成活性可被中和。

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