专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2004052370A2 QUINOLINE COMPOUNDS FOR USE IN MCH RECEPTOR RELATED DISORDERS 审中-公开
标题翻译：用于MCH受体相关疾病的喹啉化合物
公开(公告)号：WO2004052370A2
公开(公告)日：2004-06-24
申请号：PCT/DK2003/000857
申请日：2003-12-11
申请人： 7TM PHARMA A/S , FRIMURER, Thomas, Michael , ULVEN, Trond , HÖGBERG, Thomas , NØRREGAARD, Pja, Karina , LITTLE, Paul, Brian , RECEVEUR, Jean-Marie
发明人： FRIMURER, Thomas, Michael , ULVEN, Trond , HÖGBERG, Thomas , NØRREGAARD, Pja, Karina , LITTLE, Paul, Brian , RECEVEUR, Jean-Marie
IPC分类号： A61K31/506
CPC分类号： C07D401/04 , A61K31/435 , A61K31/4375 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/519
摘要： The present invention relates to the use of quinoline compounds for the preparation of a pharmaceutical and/or a cosmetic composition for the treatment, prophylaxis and/or diagnosis of a condition caused by or involving a melanin-concentrating hormone. The invention also relates to novel quinoline compounds per se. The quinoline compounds have been found to interact with a melanin-concentrating hormone receptor, a MCH receptor. The compounds have modulating activity on the MCH receptor such as e.g. antagonistic, agonistic or allosteric activity and are useful for medicinal or cosmetic purposes such as, e.g. in the treatment or prevention of feeding disorders like obesity, metabolic syndrome, Type II diabetes, bulimia, etc. or in the treatment or prevention of depression.
摘要翻译：本发明涉及喹啉化合物用于制备用于治疗，预防和/或诊断由黑素浓缩引起的或涉及黑素浓缩的药物和/或化妆品组合物的用途激素。本发明还涉及新型喹啉化合物本身。已经发现喹啉化合物与黑色素浓缩激素受体（MCH受体）相互作用。这些化合物对MCH受体具有调节活性，例如，拮抗，激动或变构活性，并可用于医药或美容目的，例如，在治疗或预防喂食障碍如肥胖，代谢综合征，II型糖尿病，贪食症等或用于治疗或预防抑郁症。

2. 发明申请

WO03018002A3 CYCLOPROPYL AND CYCLOBUTYL EPOTHILONE ANALOGS 审中-公开
标题翻译： CYCLOPROPYL和CYCLOBUTYL EPOTHILONE类似物
公开(公告)号：WO03018002A3
公开(公告)日：2003-09-04
申请号：PCT/EP0209407
申请日：2002-08-22
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , SCRIPPS RESEARCH INST , NICOLAOU KYRIACOS COSTA , NAMOTO KENJI , RITZEN ANDREAS , ULVEN TROND , SHOJI MUTSURU , ALTMANN KARL-HEINZ
发明人： NICOLAOU KYRIACOS COSTA , NAMOTO KENJI , RITZEN ANDREAS , ULVEN TROND , SHOJI MUTSURU , ALTMANN KARL-HEINZ
IPC分类号： A61K31/427 , A61K31/4427 , A61P35/00 , A61P35/02 , C07D313/00 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12 , C07D495/08 , A61K31/365 , C07D407/06 , C07D493/04
CPC分类号： C07D495/08 , C07D313/00 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12
摘要： The invention relates to cis- and trans-12, 13-cyclopropyl and 12, 13-cyclobutyl epothilones of formula (I) to (IV), wherein Ar is a radical represented by the following structure:, and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.
摘要翻译：本发明涉及式（I）至（IV）的顺式 - 和反式-12,13-环丁基埃坡霉素，其中Ar是由以下结构表示的基团：并且其它基团和符号具有本文定义的含义; 对其进行化学合成和生物评估; 它们在治疗肿瘤疾病中的用途以及含有这些化合物的药物制剂。本文所述的化合物是有效的微管蛋白聚合促进剂和细胞毒素剂。

3. 发明申请

WO2003018002A2 CYCLOPROPYL AND CYCLOBUTYL EPOTHILONE ANALOGS 审中-公开
标题翻译：环丙基和环丙基苯酚类似物
公开(公告)号：WO2003018002A2
公开(公告)日：2003-03-06
申请号：PCT/EP2002/009407
申请日：2002-08-22
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , THE SCRIPPS RESEARCH INSTITUTE , NICOLAOU, Kyriacos, Costa , NAMOTO, Kenji , RITZEN, Andreas , ULVEN, Trond , SHOJI, Mutsuru , ALTMANN, Karl-Heinz
发明人： NICOLAOU, Kyriacos, Costa , NAMOTO, Kenji , RITZEN, Andreas , ULVEN, Trond , SHOJI, Mutsuru , ALTMANN, Karl-Heinz
IPC分类号： A61K31/365
CPC分类号： C07D495/08 , C07D313/00 , C07D405/06 , C07D405/12 , C07D417/06 , C07D417/12
摘要： The invention relates to cis- and trans- 12, 13-cyclopropyl and 12, 13-cyclobutyl epothilones of formula (I) to (IV), wherein Ar is a radical represented by the following structure:, and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.
摘要翻译：本发明涉及式（I）至（IV）的顺式和反式12,13-环丙基和12,13-环丁基埃坡霉素，其中Ar是由以下结构表示的基团：其它基团和符号具有本文定义的含义; 对其化学合成和生物学评价; 它们在治疗肿瘤疾病中的用途以及含有这些化合物的药物制剂。本文所述的化合物是有效的微管蛋白聚合启动子和细胞毒性剂。

4. 发明申请

WO2012136221A1 ORTHO-FLUORO SUBSTITUTED COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES 审中-公开
标题翻译：用于治疗代谢性疾病的ORTHO-FLUORO替代化合物
公开(公告)号：WO2012136221A1
公开(公告)日：2012-10-11
申请号：PCT/DK2012/050108
申请日：2012-04-03
申请人： SYDDANSK UNIVERSITET , ULVEN, Trond , CHRISTIANSEN, Elisabeth
发明人： ULVEN, Trond , CHRISTIANSEN, Elisabeth
IPC分类号： C07C57/60 , A61P3/10 , C07C51/00 , C07C253/00 , C07C315/00 , C07C59/56 , C07C255/41 , C07C255/57 , C07C317/44
CPC分类号： C07C57/60 , C07C51/353 , C07C51/367 , C07C59/56 , C07C253/30 , C07C255/41 , C07C255/57 , C07C315/04 , C07C317/44
摘要： There is provided novel fluoro-substituted compounds capable of modulating the G- protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
摘要翻译：提供能够调节G-蛋白偶联受体GPR40的新型氟取代的化合物，包含该化合物的组合物，及其用于控制体内胰岛素水平和用于治疗诸如II型糖尿病，高血压，酮症酸中毒，肥胖症，葡萄糖不耐受和高血胆固醇血症和与异常高或低血浆脂蛋白，甘油三酯或葡萄糖水平相关的相关疾病。

5. 发明申请

WO2007062677A1 THIAZOLYL- AND PYRIMIDINYL-ACETIC ACIDS AND THEIR USE AS CRTH2 RECEPTOR LIGANDS 审中-公开
标题翻译：三唑并 - 吡啶并乙酸及其作为CRTH2受体配体使用
公开(公告)号：WO2007062677A1
公开(公告)日：2007-06-07
申请号：PCT/EP2005/012870
申请日：2005-11-30
申请人： 7TM PHARMA A/S , ULVEN, Trond , FRIMURER, Thomas , RIST, øystein , KOSTENIS, Evi , HÖGBERG, Thomas , RECEVEUR, Jean-Marie , GRIMSTRUP, Marie
发明人： ULVEN, Trond , FRIMURER, Thomas , RIST, øystein , KOSTENIS, Evi , HÖGBERG, Thomas , RECEVEUR, Jean-Marie , GRIMSTRUP, Marie
IPC分类号： C07D417/04 , C07D239/26 , A61K31/4439 , A61K31/505 , A61P11/06
CPC分类号： C07D239/26 , C07D417/04
摘要： [2-[Bis-(4-fluoro-phenyl)methyl]-4-(2-methylpyridin-4-yl)thiazol-5-yl]acetic acid, {4-(2aminopyridin-4-yl)-2-[bis-(4-fluorophenyl)methyl]thiazol-5-yl}acetic acid, [2-[bis-(4-fluorophenyl)-methyl]-4-(3-fluoro-phenyl)-pyrimidin-5-yl]acetic acid, and salts, hydrates and solvates thereof are ligands of the CRTH2 receptor, and of value for the treatment of, inter alia, asthma, rhinitis, allergic airway syndrome, or allergic rhinobronchitis.
摘要翻译： [2- [双（4-氟 - 苯基）甲基] -4-（2-甲基吡啶-4-基）噻唑-5-基]乙酸{4-（2-氨基吡啶-4-基）-2- [2-（4-氟苯基）甲基]噻唑-5-基}乙酸[2- [双 - （4-氟苯基） - 甲基] -4-（3-氟 - 苯基） - 嘧啶-5-基] 乙酸及其盐，水合物和溶剂化物是CRTH2受体的配体，并且其用于治疗哮喘，鼻炎，过敏性气道综合征或过敏性鼻炎支原体的价值。

6. 发明申请

WO2005116001A1 SUBSTITUTED THIAZOLEACETIC AS CRTH2 LIGANDS 审中-公开
标题翻译：作为CRTH2配体取代三氟甲磺酸
公开(公告)号：WO2005116001A1
公开(公告)日：2005-12-08
申请号：PCT/EP2005/005882
申请日：2005-05-30
申请人： 7TM PHARMA A/S , ULVEN, Trond , FRIMURER, Thomas , RIST, Øystein , KOSTENIS, Evi , HÖGBERG, Thomas , RECEVEUR, Jean-Marie , GRIMSTRUP, Marie
发明人： ULVEN, Trond , FRIMURER, Thomas , RIST, Øystein , KOSTENIS, Evi , HÖGBERG, Thomas , RECEVEUR, Jean-Marie , GRIMSTRUP, Marie
IPC分类号： C07D277/30
CPC分类号： C07D277/30 , C07D417/04 , C07D417/06
摘要： Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis; wherein X 1 is -S-, -O-, -N=N-. -NR 7 -, -CR 7 =CR 8 -, -CR 7 =N-, wherein R 7 and R 8 are independently hydrogen or C 1 -C 3 alkyl; A is a carboxyl group -COOH, or a carboxyl bioisostere; rings Ar 2 and Ar 3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; ring B is as defined for Ar 2 and Ar 3 , or an optionally substituted N-pyrrolidinyl, N-piperidinyl or N-azepinyl ring; s is 0 or 1; L1, L2 and L4 are linker radicals as defined in the description; Q 1 and Q 2 represent substituents as defined in the description.
摘要翻译：式（I）化合物可用于治疗对调节CRTH2受体活性如哮喘，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎的疾病的治疗; 其中X1是-S-，-O-，-N = N-。 -NR7-，-CR7 = CR8-，-CR7 = N-，其中R7和R8独立地为氢或C1-C3烷基; A是羧基-COOH或羧基生物电子等排体; 环Ar 2和Ar 3各自独立地表示苯基或5-或6-元单环杂芳基环，或由5-或6-元碳环或杂环组成的双环体系，其是苯并稠合的或与5或6元单环杂芳基环稠合，所述环或环系统任选被取代; 环B如Ar 2和Ar 3所定义，或任选取代的N-吡咯烷基，N-哌啶基或N-氮杂环酮环; s为0或1; L1，L2和L4是描述中定义的连接基团; Q1和Q2表示如说明书中定义的取代基。

7. 发明申请

WO2004079625A2 A PSEUDO-SEQUENCE METHOD FOR COMPARING 7TM RECEPTORS WITH RESPECT TO THE PHYSICOCHEMICAL PROPERTIES OF THEIR BINDING SITES 审中-公开
标题翻译：用于比较7TM受体与其结合位点的物理化学性质的PSEUDO-SEQUENCE方法
公开(公告)号：WO2004079625A2
公开(公告)日：2004-09-16
申请号：PCT/DK2004/000148
申请日：2004-03-05
申请人： 7TM PHARMA A/S , FRIMURER, Thomas, Michael , ULVEN, Trond , HÖGBER, Thomas , ELLING, Christian, E.
发明人： FRIMURER, Thomas, Michael , ULVEN, Trond , HÖGBER, Thomas , ELLING, Christian, E.
IPC分类号： G06F19/00
CPC分类号： G06F19/16 , G06F19/18
摘要： A pseudo-sequence method for comparing 7TM receptors with respect to the physicochemical properties of their binding sites, the method comprising the steps of: (i) optionally, aligning part of or all of the amino acid sequence of the first 7TM receptor with part of or all or the amino acid sequence of the one or more further 7TM receptors, (ii) selecting, in a sequential or non-sequential order, at the most 12 amino acid residues per helix and/or extracellular loops, which are involved in one or more binding sites of each 7TM receptor. (iii) forming a pseudo-sequence comprising at the most 50 amino acid residues from the selected sequential or non-sequential amino acid residues, (iv) for each 7TM receptor assigning one or more physicochemical descriptors to the amino acid residues of the selected amino acid pseudo-sequence involved in one or more binding sites, (v) optionally, for each 7TM receptor mathematically manipulating the physicochemical descriptors of step (iv) to obtain a simplified measure of the physicochemical properties of the binding site. (vi) for each 7TM receptor generating a similarity score as defined herein by comparing the physicochemical descriptor or, if relevant, the simplified measure for the first 7TM receptor with the physicochemical descriptors or, if relevant, the simplified measures for the one or further 7TM receptors, (vii) optionally, ranking the 7TM receptors with respect to the physicochemical properties of their binding sites according to the similarity scores obtained in step vi)
摘要翻译：一种用于比较7TM受体相对于其结合位点的物理化学性质的伪序列方法，所述方法包括以下步骤：（i）任选地将第一7TM受体的部分或全部氨基酸序列与或全部或一个或多个其它7TM受体的氨基酸序列，（ii）以顺序或非顺序的顺序选择每个螺旋和/或细胞外环最多12个氨基酸残基，其参与一个或更多的每个7TM受体的结合位点。（iii）形成包含来自所选顺序或非连续氨基酸残基的最多50个氨基酸残基的伪序列，（iv）对于所选择的氨基酸的氨基酸残基分配一个或多个物理化学描述符的每个7TM受体参与一个或多个结合位点的酸性伪序列，（v）任选地，对于每个7TM受体，在数学上操纵步骤（iv）的物理化学描述符以获得结合位点的物理化学性质的简化测量。（vi）对于每个7TM受体，通过将物理化学描述符或如果相关的第一7TM受体的简化测量与物理化学描述符相比较，或者如果相关的话，通过将一个或另外7个TM的简化测量受体，（vii）任选地，根据步骤vi）中获得的相似性得分，相对于其结合位点的物理化学性质对7TM受体进行排序，

8. 发明申请

WO2004052371A2 CYCLIC QUINOLINE COMPOUNDS FOR USE IN MCH RECEPTOR RELATED DISORDERS 审中-公开
标题翻译：用于MCH受体相关疾病的环喹啉化合物
公开(公告)号：WO2004052371A2
公开(公告)日：2004-06-24
申请号：PCT/DK2003/000858
申请日：2003-12-11
申请人： 7TM PHARMA A/S , FRIMURER, Thomas, Michael , ULVEN, Trond , HÖGBERG, Thomas , NØRREGAARD, Pia, Karina , LITTLE, Paul, Brian , RECEVEUR, Jean-Marie
发明人： FRIMURER, Thomas, Michael , ULVEN, Trond , HÖGBERG, Thomas , NØRREGAARD, Pia, Karina , LITTLE, Paul, Brian , RECEVEUR, Jean-Marie
IPC分类号： A61K31/506
CPC分类号： C07D401/04 , A61K31/435 , A61K31/4375 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/519
摘要： The present invention relates to the use of cyclic quinoline compounds for the preparation of a pharmaceutical and/or a cosmetic composition for the treatment, prophylaxis and/or diagnosis of a condition caused by or involving a melanin-concentrating hormone. The invention also relates to novel cyclic quinoline compounds per se . The cyclic quinoline compounds have been found to interact with a melanin-concentrating hormone receptor, a MCH receptor. The compounds have modulating activity on the MCH receptor such as e.g. antagonisitic, agonistic or allosteric activity and are useful for medicinal or cosmetic purposes such as, e.g. in the treatment or prevention of feeding disorders like obesity, metabolic syndrome, Type II diabetes, bulimia etc. or in the treatment or prevention of depression.
摘要翻译：本发明涉及环喹啉化合物用于制备用于治疗，预防和/或诊断由黑色素瘤引起并涉及黑色素瘤的病症的药物和/或化妆品组合物的用途，集中激素。本发明还涉及本身新型的环喹啉化合物。已经发现环喹啉化合物与黑色素浓缩激素受体（MCH受体）相互作用。这些化合物对MCH受体具有调节活性，例如，拮抗剂，激动剂或变构活性，并可用于医药或美容目的，例如，用于治疗或预防喂养障碍如肥胖症，代谢综合征，II型糖尿病，贪食症等或用于治疗或预防抑郁症。

9. 发明申请

WO2012045363A1 ANTIDIABETIC ENOLIC GLUCOSIDE OF PHENYLPYRUVIC ACID 审中-公开
标题翻译：苯乙酸的抗真菌剂
公开(公告)号：WO2012045363A1
公开(公告)日：2012-04-12
申请号：PCT/EP2010/065052
申请日：2010-10-07
申请人： ZADEC APS , JOUBERT, Elizabeth , FEY, Stephen John , LOUW, Johan , ULVEN, Trond , TYAGI, Rahul
发明人： JOUBERT, Elizabeth , FEY, Stephen John , LOUW, Johan , ULVEN, Trond , TYAGI, Rahul
IPC分类号： C07H15/18 , A61K31/7028 , A61P3/10
CPC分类号： C07H15/203 , C07H15/18 , C07H15/26
摘要： There is provided an antidiabetic enolic glucoside of phenylpyruvic acid and derivatives thereof for use as medicaments, especially normoglycemic agents, i.e. for lowering blood glucose levels to normal levels in mammals that are obese, pre-diabetic or have diabetes, obesity and/or syndrome X.Hence the compounds of the present invention help to manage blood sugar levels, i.e. helping the body by balancing the blood sugar levels; helping to keep balanced blood glucose levels, particularly in humans with diabetes; aiding by enhancing the glucose uptake by the cells and by reducing sugar levels, thus improving or restoring the glucose tolerance; optimizing the glycemic response; normalizing the glucose tolerance.
摘要翻译：提供苯丙酮酸及其衍生物的抗糖尿病烯醇葡糖苷及其衍生物，用作药物，尤其是正常血糖药，即将肥胖，糖尿病前期或糖尿病，肥胖和/或综合征X的哺乳动物血糖水平降低至正常水平本发明的化合物有助于控制血糖水平，即通过平衡血糖水平来帮助身体; 有助于保持平衡的血糖水平，特别是在患有糖尿病的人中; 通过增强细胞的葡萄糖摄取和降低糖水平，从而改善或恢复葡萄糖耐量来辅助; 优化血糖反应; 正常化葡萄糖耐量。

10. 发明申请

WO2010012650A1 COMPOUNDS FOR THE TREATMENT OF METABOLIC DISEASES 审中-公开
标题翻译：用于治疗代谢性疾病的化合物
公开(公告)号：WO2010012650A1
公开(公告)日：2010-02-04
申请号：PCT/EP2009/059527
申请日：2009-07-23
申请人： SYDDANSK UNIVERSITET , ULVEN, Trond , CHRISTIANSEN, Elisabeth
发明人： ULVEN, Trond , CHRISTIANSEN, Elisabeth
IPC分类号： C07C57/42 , C07C57/60 , C07C59/48 , C07C59/52 , C07C59/64 , C07C59/68 , C07C59/70 , C07C59/74 , C07C59/84 , C07C59/86 , C07C61/39 , C07C309/73 , A61P3/10 , A61K31/192 , A61K31/216
CPC分类号： C07D213/55 , C07C57/60 , C07C59/48 , C07C59/52 , C07C59/64 , C07C59/68 , C07C59/70 , C07C59/76 , C07C59/84 , C07C59/86 , C07C59/92 , C07C61/39 , C07C67/307 , C07C67/31 , C07C67/317 , C07C67/343 , C07C205/56 , C07C229/44 , C07C255/41 , C07C309/73 , C07C2601/02 , C07C2602/08 , C07D213/61 , C07D215/18 , C07D253/04 , C07D277/30 , C07D333/24 , C07C69/753 , C07C69/712 , C07C69/618 , C07C69/65 , C07C69/738 , C07C69/734 , C07C69/732
摘要： There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type Il diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.
摘要翻译：提供能够调节G蛋白偶联受体GPR40的新化合物，包含该化合物的组合物，及其用于控制体内胰岛素水平和用于治疗诸如II型糖尿病，高血压，酮症酸中毒，肥胖症，葡萄糖不耐受，以及与异常高或低血浆脂蛋白，甘油三酯或葡萄糖水平相关的高胆固醇血症和相关疾病。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式