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

WO2007062797A1 AMINO-SUBSTITUTED AZO-HETEROCYCLIC COMPOUNDS FOR TREATING INFLAMMATORY CONDITIONS 审中-公开
标题翻译：用于处理炎症条件的氨基取代的AZO-杂环化合物
公开(公告)号：WO2007062797A1
公开(公告)日：2007-06-07
申请号：PCT/EP2006/011384
申请日：2006-11-23
申请人： 7TM PHARMA A/S , GRIMSTRUP, Marie , RIST, Øystein , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , FRIMURER, Thomas, Michael
发明人： GRIMSTRUP, Marie , RIST, Øystein , RECEVEUR, Jean-Marie , HOEGBERG, Thomas , FRIMURER, Thomas, Michael
IPC分类号： C07D277/42 , C07D417/12 , A61K31/426 , A61K31/4436 , A61P29/00
CPC分类号： C07D277/42 , C07D417/12
摘要： Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of inflammatory, autoimmune, respiratory or allergy disease: wherein X 1 is -S-, -O-, -N=N-. -NR 5 -, -CR 5 =CR 6 -, -CR 5 =N-, wherein R 5 and R 6 are independently hydrogen or C 1 -C 3 alkyl; R 1 is hydrogen or C 1 -C 3 alkyl or cyclopropyl; R 2 is an optionally substituted phenyl or 5- or 6-membered monocyclic heteroaryl ring; R 3 is an optionally substituted carbocyclic ring of 3 to 7 ring atoms, or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; R 4 is a group other than hydrogen, methyl or ethyl of formula Q-[Alk 1 ] m -[X] n -[Alk 2 ] p -[Z} s - wherein m, n p, and s are independently 0 or 1 ; Q is hydrogen or an optionally substituted 4-, 5- or 6-membered monocyclic heterocyclic ring; Alk 1 and Alk 2 are independently optionally substituted C 1 -C 3 alkylene radicals; X is -O-, -S-, -C(=O)-, - S(=O)-, -S(=O) 2 -, -CH(R 7 )-, -N(R 7 )-, or, in either orientation -SO 2 N(R 7 )- or - C(=O)N(R 7 )-, wherein R 7 is hydrogen, or R 7 represents a C 2 -C 4 bridge between the C or N atom of X to which it is attached and a carbon atom of Alk 2 and Z is -CH 2 , - C(=O) or -S(=O) 2 .
摘要翻译：式（I）化合物是可用于治疗炎性，自身免疫，呼吸或过敏疾病的CRTH2拮抗剂：其中X 1 -S-，-O-，-N = N-。 -NR 5 - ，-CR 5 = CR 6 - ，-CR 5 N = N-，其中R R 5和R 6独立地是氢或C 1 -C 3烷基; R 1是氢或C 1 -C 3烷基或环丙基; R 2是任选取代的苯基或5-或6-元单环杂芳基环; R 3是任选取代的3至7个环原子的碳环，或任选取代的4-，5-或6-元单环杂环; R 4是除了氢，甲基或式Q-的基团之外的基团 - [Alk 1] m - [X] n 其中m，np和s独立地为0或1; - 其中m，np和s独立地为0或1; - 其中m，np和s独立地为0或1; Q是氢或任选取代的4-，5-或6-元单环杂环; Alk＆lt; 1＆gt;和Alk 2独立地是任选取代的C 1 -C 3亚烷基; X是-O - ， - S - ， - C（= O） - ， - S（= O） - ， - S（= O）2 - ， - CH -N（R 7） - ，或者以任一取向-SO 2 N（R 7） - ， - （R 7）或-C（= O）N（R 7） - ，其中R 7为氢，或R 7为C 1 -C 6烷基，其连接的X的C或N原子与Alk 2的碳原子之间的2个或更多的桥是-CH _。

2. 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。

3. 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。

4. 发明申请

WO2005123714A1 QUINAZOLINE COMPOUNDS AND THEIR USE IN MCH-RELATED DISEASE 审中-公开
标题翻译：喹唑啉化合物及其在相关疾病中的用途
公开(公告)号：WO2005123714A1
公开(公告)日：2005-12-29
申请号：PCT/EP2004/006539
申请日：2004-06-16
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： C07D401/04
CPC分类号： C07D401/04
摘要： Compounds of formula (I), are Melanin Concentrating Hormone (MCH) ligands, useful in the treatment of obesity and other MCH-related conditions (I) wherein R 1 is: (I) and R 2 is CI-, CH 3 CF 3, or F 3 C-O-.
摘要翻译：式（I）化合物是可用于治疗肥胖症和其它MCH相关病症（I）的黑色素浓度激素（MCH）配体，其中R 1为：（I），R 2为Cl-，CH 3 CF 3或F 3 C- O-。

5. 发明申请

WO2004056869A1 GHRELIN RECEPTOR INVERSE AGONIST FOR REGULATION OF FEEDING BEHAVIOURS 审中-公开
标题翻译： GHRELIN受体反应激素调节饲料行为
公开(公告)号：WO2004056869A1
公开(公告)日：2004-07-08
申请号：PCT/DK2003/000924
申请日：2003-12-20
申请人： 7TM Pharma A/S , LANGE, Brigitte, Holst , SCHWARTZ, Thue, W. , FRIMURER, Thomas, Michael , RIST, Øystein
发明人： LANGE, Brigitte, Holst , SCHWARTZ, Thue, W. , FRIMURER, Thomas, Michael , RIST, Øystein
IPC分类号： C07K14/72
CPC分类号： G01N33/74 , A61K31/00 , A61K38/046 , G01N2333/726 , G01N2500/02
摘要： Compounds of the invention act as inverse agonist ghrelin receptors. Some of the compounds of the invention may have both inverse agonistic and antagonistic properties as they both decrease or eliminate the constitutive activity of he ghrelin receptor and block the effect of ghrelin. Other preferred compounds of the invention have inverse agonistic properties but have little or no antagonistic activity. The compounds are suitable for medical and/or cosmetic use in connection with modulation of feeding behaviors, body composition and reduction of body mass. The invention also relates to methods for identifying inverse agonists for the ghrelin receptor and for monitoring the further development of such compounds.
摘要翻译：本发明的化合物作为反向激动剂ghrelin受体。本发明的一些化合物可以具有反向激动和拮抗性质，因为它们都降低或消除了生长素释放肽受体的组成型活性并阻断了生长素释放肽的作用。本发明的其它优选化合物具有反向激动性质但具有很少或没有拮抗活性。该化合物适用于与调节进食行为，身体组成和减少体重有关的医疗和/或化妆品用途。本发明还涉及用于鉴定生长素释放肽受体的反向激动剂并监测这些化合物的进一步发展的方法。

6. 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，

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