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1. 发明申请

WO02081430A3 NOVEL BENZYLIDENEAMINO GUANIDINES AND THEIR USES AS LIGANDS TO THE MELANOCORTIN RECEPTORS 审中-公开
标题翻译：新戊酰胆碱酯酶及其作为MELANOCORTIN受体配体的用途
公开(公告)号：WO02081430A3
公开(公告)日：2003-08-14
申请号：PCT/GB0201593
申请日：2002-04-05
申请人： MELACURE THERAPEUTICS AB , LUNDSTEDT TORBJOERN , ANDERSSON PER , BOMAN ARNE , SEIFERT ELISABETH , SKOTTNER ANNA , TOWLER PHILIP DEAN
发明人： LUNDSTEDT TORBJOERN , ANDERSSON PER , BOMAN ARNE , SEIFERT ELISABETH , SKOTTNER ANNA
IPC分类号： A61K49/00 , A61K31/15 , A61K31/155 , A61K51/00 , A61P1/14 , A61P3/00 , A61P15/00 , A61P17/00 , A61P25/04 , A61P25/30 , A61P25/36 , A61P29/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07C281/18
CPC分类号： A61K31/155
摘要： The present invention relates to novel benzylideneamino guanidines of general formula and to the use of these benzylideneamino guanidines as melanocortin receptor agonists or antagonists. The invention further relates to benzylideneamino guanidines which show selectivity to the MC1 and MC4 melanocortin receptors as agonists and/or antagonists.
摘要翻译：本发明涉及通式的新亚苄基氨基胍，以及这些亚苄基氨基胍用作黑皮质素受体激动剂或拮抗剂。本发明还涉及对MC1和MC4黑皮质素受体作为激动剂和/或拮抗剂显示选择性的亚苄基氨基胍。

2. 发明申请

WO0211715A3 THE USE OF BENZYLIDENEAMINOGUANIDINES AND HYDROXYGUANIDINES AS MELANOCORTIN RECEPTOR LIGANDS 审中-公开
标题翻译：苯丙胺氨基腺嘌呤和羟基甘氨酸作为甲氧苄啶受体配体的应用
公开(公告)号：WO0211715A3
公开(公告)日：2003-01-16
申请号：PCT/GB0103534
申请日：2001-08-07
申请人： MELACURE THERAPEUTICS AB , LUNDSTEDT TORBJOERN , SKOTTNER ANNA , SEIFERT ELISABETH
发明人： LUNDSTEDT TORBJOERN , SKOTTNER ANNA , SEIFERT ELISABETH
IPC分类号： C07D317/58 , A61K8/00 , A61K8/43 , A61K31/155 , A61K31/185 , A61K31/275 , A61K31/36 , A61K51/00 , A61P1/04 , A61P1/14 , A61P1/16 , A61P1/18 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P5/06 , A61P5/10 , A61P5/14 , A61P5/30 , A61P5/40 , A61P7/00 , A61P7/02 , A61P7/04 , A61P7/06 , A61P7/08 , A61P7/10 , A61P9/00 , A61P9/02 , A61P9/04 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , A61P9/14 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P15/00 , A61P15/04 , A61P15/06 , A61P15/08 , A61P15/10 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P17/08 , A61P17/16 , A61P19/02 , A61P19/04 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/36 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/02 , A61P33/10 , A61P35/00 , A61P35/04 , A61P37/02 , A61P37/04 , A61P37/06 , A61P37/08 , A61P39/00 , A61P39/02 , A61P43/00 , A61Q17/04 , A61Q19/00 , A61Q19/02 , C07D317/62
CPC分类号： C07C281/16 , A61K31/155 , C07C53/10 , C07C309/30 , C07C309/46 , C07D317/58
摘要： The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof.
摘要翻译：本发明涉及通式（I）的化合物作为黑皮质素受体的配体和/或用于治疗黑皮质素系统中的病症的用途：其中X是H或OH; R 1，R 2，R 3，R 4和R 5相同或不同，选自氢，卤素，具有1-5个碳原子的烷基，电子给体基团如具有1-5个碳原子的烷氧基或羟基，电子受体基团氰基，硝基，三氟烷基或酰胺; 烷基氨基，苯甲酰氧基，硝酰基，苯基或磺基; 及其药理学活性盐。

3. 发明申请

WO0155107A3 AROMATIC AMINES AND AMIDES ACTING ON THE MELANOCORTIN RECEPTORS 审中-公开
标题翻译：对肌醇激素受体的芳香胺和氨基酸
公开(公告)号：WO0155107A3
公开(公告)日：2002-01-17
申请号：PCT/GB0100356
申请日：2001-01-29
申请人： MELACURE THERAPEUTICS AB , LUNDSTEDT TORBJOERN , SKOTTNER ANNA , SEIFERT ELISABETH , ANDERSSON PER , KAULINA LARISA , DIKOVSKAYA KLARA , MUTULE ILZE , MUTULIS FELIKSS , WIKBERG JARL , STARCHENKOV IGOR , KREICBERGA JANA
发明人： LUNDSTEDT TORBJOERN , SKOTTNER ANNA , SEIFERT ELISABETH , ANDERSSON PER , KAULINA LARISA , DIKOVSKAYA KLARA , MUTULE ILZE , MUTULIS FELIKSS , WIKBERG JARL , STARCHENKOV IGOR , KREICBERGA JANA
IPC分类号： C07C233/40 , C07C237/06 , C07C279/14 , C07D209/08 , C07D209/12 , C07D209/18 , C07D209/20 , C07D209/42 , C07D213/40 , C07D213/61 , C07D405/12 , C07D409/12 , C07D409/14 , A61K31/36 , A61K31/4045 , A61K31/405 , A61K31/4406 , A61K31/443 , C07C233/78 , C07C279/12
CPC分类号： C07D213/40 , C07C233/40 , C07C237/06 , C07C279/14 , C07C2602/10 , C07D209/08 , C07D209/12 , C07D209/18 , C07D209/20 , C07D209/42 , C07D213/61 , C07D405/12 , C07D409/12 , C07D409/14
摘要： The present invention relates to novel aromatic amines and amides of general formula (I) and to the use of these amines and amides for the treatment of obesity, anorexia, inflammation, mental disorders and other diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.
摘要翻译：本发明涉及通式（I）的新型芳族胺和酰胺，以及这些胺和酰胺用于治疗与黑皮质素受体或相关系统相关的肥胖症，厌食症，炎症，精神障碍和其它疾病的用途，例如，黑素细胞刺激激素。

4. 发明申请

WO0155106A3 NOVEL MELANOCORTIN RECEPTOR AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：新的梅兰康宁受体激动剂和拮抗剂
公开(公告)号：WO0155106A3
公开(公告)日：2002-03-21
申请号：PCT/GB0100346
申请日：2001-01-29
申请人： MELACURE THERAPEUTICS AB , LUNDSTEDT TORBJOERN , SKOTTNER ANNA , SEIFERT ELISABETH , STARCHENKOV IGOR , TRAPENCIERIS PETERIS , KAUSS VALERJANS , KALVINS IVARS , BOMAN ARNE
发明人： LUNDSTEDT TORBJOERN , SKOTTNER ANNA , SEIFERT ELISABETH , STARCHENKOV IGOR , TRAPENCIERIS PETERIS , KAUSS VALERJANS , KALVINS IVARS , BOMAN ARNE
IPC分类号： A61K31/403 , A61K31/4045 , A61K31/405 , A61K31/4439 , A61K31/454 , A61K31/455 , A61K31/496 , A61P1/14 , A61P3/04 , A61P3/10 , A61P5/00 , A61P7/00 , A61P9/00 , A61P15/00 , A61P17/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/08 , A61P43/00 , C07D209/14 , C07D209/18 , C07D209/20 , C07D209/42 , C07D209/88 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/06 , A61K31/404 , C07D401/06 , C07D403/12 , C07D405/12
CPC分类号： C07D213/82 , C07D209/18 , C07D209/42
摘要： The present invention relates to novel aromatic amines of general formula (I) and to the use of these amines for the treatment of obesity, anorexia, inflammation, mental disorders an other diseases associated with the melanocortin receptors or related systems, e.g. the melanocyte stimulating hormones.
摘要翻译：本发明涉及通式（I）的新型芳族胺，以及这些胺用于治疗肥胖，厌食，炎症，精神障碍与黑皮质素受体或相关系统相关的其它疾病的用途，例如，黑素细胞刺激激素。

5. 发明申请

WO02068397A8 DIAMINOQUINAZOLINE ESTERS FOR USE AS DIHYDROFOLATE REDUCTADE INHIBITORS 审中-公开
标题翻译：用作二氢呋喃酮减少剂抑制剂的二氨基喹诺酮酯
公开(公告)号：WO02068397A8
公开(公告)日：2003-12-04
申请号：PCT/GB0200888
申请日：2002-02-28
申请人： MELACURE THERAPEUTICS AB , PETT CHRISTOPHER PHINEAS , LUNDSTEDT TORBJOERN , HAELLGREN ANNELI , ANDERSSON PER , HALLBERG ANDERS , NORDBERG MALIN GRAFFNER
发明人： LUNDSTEDT TORBJOERN , HAELLGREN ANNELI , ANDERSSON PER , HALLBERG ANDERS , NORDBERG MALIN GRAFFNER
IPC分类号： A61K31/517 , A61P1/04 , A61P11/00 , A61P11/06 , A61P15/00 , A61P17/06 , A61P19/02 , A61P29/00 , A61P31/04 , A61P33/02 , A61P35/00 , A61P37/06 , A61P43/00 , C07D239/95 , C07D405/12 , C07D407/12 , C07D409/12 , A61K31/505
CPC分类号： C07D405/12 , C07D239/95 , C07D409/12
摘要： Compounds of the formula (I) wherein R1, R2, R1' and R2' are independently hydrogen or a group releasing the free amine in vivo, R6 is a substituted phenyl or an optionally substituted, bicyclic or tricyclic aryl ring system or an optionally substituted mono, bi- or tricyclic heteroaryl ring system having utility as dihydrofolate reductase (DHFR) inhibitors with favourable pharmacokinetic properties.
摘要翻译：式（I）的化合物其中R 1，R 2，R 1'和R 2'独立地是氢或在体内释放游离胺的基团，R 6是取代的苯基或任选取代的双环或三环芳基环系或任选取代的具有有利于药代动力学性质的二氢叶酸还原酶（DHFR）抑制剂的单，双或三环杂芳基环系统。

6. 发明申请

WO0136980A3 A PROCESS FOR IDENTIFYING THE ACTIVE SITE IN A BIOLOGICAL TARGET 审中-公开
标题翻译：用于识别生物目标中活性位点的方法
公开(公告)号：WO0136980A3
公开(公告)日：2002-03-14
申请号：PCT/GB0004420
申请日：2000-11-20
申请人： MELACURE THERAPEUTICS AB , PETT CHRISTOPHER PHINEAS , LUNDSTEDT TORBJOERN , ANDERSSON PER , WIKBERG JARL , MUCENIECE RUTA , PRUSIS PETERIS
发明人： LUNDSTEDT TORBJOERN , ANDERSSON PER , WIKBERG JARL , MUCENIECE RUTA , PRUSIS PETERIS
IPC分类号： G06F19/16 , G06F19/00
CPC分类号： G06F19/16
摘要： The invention relates to processes for characterising the sites of interaction between a Ligand Y and a Target X, comprising the steps of (1) inputting information on the chemical/physical properties of at least two targets of the type X; (2) inputting information on the chemical/physical properties of at least two ligands of the type Y; (3) inputting information on the interactions between at least two of the targets of type X with at least two of the ligands of type Y; and then correlating the information from steps 1, 2 and 3 using one or more multivariate methods in order to produce a model of the interaction between the Ligand Y and Target X, from which the sites of interaction may be identified and/or characterised.
摘要翻译：本发明涉及用于表征配体Y和目标X之间的相互作用位置的方法，包括以下步骤：（1）输入关于X型至少两个靶的化学/物理性质的信息; （2）输入关于Y型至少两种配体的化学/物理性质的信息; （3）输入关于X型至少两个靶与至少两种Y型配体之间的相互作用的信息; 然后使用一个或多个多变量方法将来自步骤1,2和3的信息相关联，以便产生配体Y和目标X之间的相互作用的模型，从中可以识别和/或表征相互作用的位置。

7. 发明申请

WO2008058679A2 NOVEL AMIDES ACTING ON THE ADENOSINE RECEPTORS 审中-公开
标题翻译：对腺苷受体的新陈代谢作用
公开(公告)号：WO2008058679A2
公开(公告)日：2008-05-22
申请号：PCT/EP2007009721
申请日：2007-11-09
申请人： ACURE PHARMA AB , LUNDSTEDT TORBJOERN , SEIFERT ELISABETH , LEK PER , BOMAN ARNE
发明人： LUNDSTEDT TORBJOERN , SEIFERT ELISABETH , LEK PER , BOMAN ARNE
IPC分类号： C07K5/023 , A61K38/05 , A61P19/02 , C07K5/027
CPC分类号： C07D209/14
摘要： There are described Compounds of formula (I) in which R 3 to R 8 are independently selected from hydrogen, halogen, trihaloalkyl, alkyl having 1, 2, 3, 4 or 5 carbon atoms, electron donor groups selected from alkoxy having 1, 2, 3, 4 or 5 carbon atoms, trihaloalkoxy, hydroxy or amino, electron acceptor groups selected from cyano, sulphonic, nitro, or amide; R 1 is an optionally substituted phenyl, benzyl or cyclohexyl group; R 2 is selected from amino, substituted amino or guanidino groups, Z is a saturated or unsaturated C 1-5 hydrocarbon chain, and salts thereof. A process for their preparation and compositions containing them are also described. The Compounds are either agonists or antagonists of a specific adenosine receptor or a number of adenosine receptors and have usefulness for the treatment of inflammation, arthritic conditions, rheumatoid arthritis, Osteoarthritis, mental disorders, or for inducing central nerve regeneration.
摘要翻译：描述了式（I）的化合物，其中R 3至R 8独立地选自氢，卤素，三卤代烷基，具有1,2,3,4或4个碳原子的烷基 5个碳原子，选自具有1,2,3,4或5个碳原子的烷氧基的电子给体基团，三卤代烷氧基，羟基或氨基，选自氰基，磺酸，硝基或酰胺的电子受体基团; R 1是任选取代的苯基，苄基或环己基; R 2选自氨基，取代的氨基或胍基，Z是饱和或不饱和的C 1-5 - 烃链，及其盐。还描述了其制备方法和含有它们的组合物。化合物是特定腺苷受体的激动剂或拮抗剂或多种腺苷受体，并且可用于治疗炎症，关节炎病症，类风湿性关节炎，骨关节炎，精神障碍或诱导中枢神经再生。

8. 发明申请

WO2008061647A8 USE OF A COMPOUND AS VEGF INHIBITOR 审中-公开
标题翻译：化合物作为VEGF抑制剂的使用
公开(公告)号：WO2008061647A8
公开(公告)日：2008-11-27
申请号：PCT/EP2007009767
申请日：2007-11-12
申请人： ACURE PHARMA AB , LUNDSTEDT TORBJOERN , EKSTROEM GUNILLA
发明人： LUNDSTEDT TORBJOERN , EKSTROEM GUNILLA
IPC分类号： A61K31/155 , A61P29/00 , A61P35/00
CPC分类号： A61K31/155
摘要： There is disclosed the use of N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine or a pharmacologically acceptable salt thereof as an agent for use in the inhibition of Vascular Endothelial Growth Factor (VEGF). Such an agent is likely to be of application in the treatment or prevention of undesired blood vessel formation during tumour growth and/or in inflammatory conditions.
摘要翻译：公开了使用N-（2-氯-3,4-二甲氧基亚苄基氨基）胍或其药学上可接受的盐作为用于抑制血管内皮生长因子（VEGF）的药剂。这种药剂很可能用于治疗或预防肿瘤生长期间和/或炎性病症期间不期望的血管形成。

9. 发明专利

SE0400575D0 未知
公开(公告)号：SE0400575D0
公开(公告)日：2004-03-05
申请号：SE0400575
申请日：2004-03-05
申请人： LUNDSTEDT TORBJOERN , SKOTTNER-LUNDIN ANNA
发明人： LUNDSTEDT TORBJOERN , SKOTTNER-LUNDIN ANNA
IPC分类号： A61K20060101 , A61K

10. 发明专利

SE0400576D0 未知
公开(公告)号：SE0400576D0
公开(公告)日：2004-03-05
申请号：SE0400576
申请日：2004-03-05
申请人： LUNDSTEDT TORBJOERN , SKOTTNER-LUNDIN ANNA
发明人： LUNDSTEDT TORBJOERN , SKOTTNER-LUNDIN ANNA
IPC分类号： A61K20060101 , A61K

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