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1. 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。

2. 发明申请

WO2002080896A1 USES OF BENZYLIDENEAMINO GUANIDINES AS LIGANDS TO THE MELANOCORTIIN RECEPTORS 审中-公开
标题翻译：苯并噻吩类化合物作为MILANOCORTIIN受体配体的使用
公开(公告)号：WO2002080896A1
公开(公告)日：2002-10-17
申请号：PCT/GB2002/001589
申请日：2002-04-05
申请人： MELACURE THERAPEUTICS AB , TOWLER, Philip, Dean , LUNDSTEDT, Torbjörn , ANDERSSON, Per , BOMAN, Arne , SEIFERT, Elisabeth , SKOTTNER, Anna
发明人： LUNDSTEDT, Torbjörn , ANDERSSON, Per , BOMAN, Arne , SEIFERT, Elisabeth , SKOTTNER, Anna
IPC分类号： A61K31/155
CPC分类号： A61K31/155
摘要： The present invention relates to the use of benzylideneamino guanidines of general formula (I) as melanocortin receptor agonists or antagonist, and in particular, the use of benzylideneamino guanidines which show selectivity to the MC1 and MC4 melanocortin receptors as argonists and/or antagonists.
摘要翻译：本发明涉及通式（I）的亚苄基氨基胍类作为黑皮质素受体激动剂或拮抗剂，特别是使用显示对MC1和MC4黑皮质素受体的选择性的亚苄基氨基胍类作为氩学和/或拮抗剂。

3. 发明申请

WO2004020417A8 2,4-DIAMINOQUINAZOLINE, 2-AMINO-4-HYDROXYPTERIDINE AND 2,4-DIAMINOPYRIMIDINE ESTER DERIVATIVES AS DIHYDROFOLATE REDUCTASE INHIBITORS 审中-公开
标题翻译：作为二氢叶酸还原酶抑制剂的2,4-二氨基喹唑啉，2-氨基-4-羟基哌啶和2,4-二氨基嘧啶酯衍生物
公开(公告)号：WO2004020417A8
公开(公告)日：2004-04-15
申请号：PCT/GB0303704
申请日：2003-08-27
申请人： MELACURE THERAPEUTICS AB , BOMAN ARNE , LUNDSTEDT TORBJORN , ANDERSSON PER , SEIFERT ELISABETH , PETT CHRISTOPHER PHINEAS
发明人： BOMAN ARNE , LUNDSTEDT TORBJORN , ANDERSSON PER , SEIFERT ELISABETH
IPC分类号： C07D239/48 , C07D239/95 , C07D487/04 , A61K31/505 , A61K31/517 , A61K31/519
CPC分类号： C07D239/48 , C07D239/95 , C07D487/04
摘要： This invention relates to novel esters of the general formula (III), which are Dihydrofolate Reductase Inhibitors; Wherein A is a heteroaromatic group, preferably selected from formula (a), formula (b), formula (c); Wherein Rl is either hydrogen or CH3; Wherein B is selected from formula (d), formula (e), formula (f), formula (g), formula (h), formula (i), formula (j): and salts thereof.
摘要翻译：本发明涉及通式（III）的新型酯，它们是二氢叶酸还原酶抑制剂; 其中A是杂芳族基团，优选选自式（a），式（b），式（c）; 其中R1为氢或CH3; 其中B选自式（d），式（e），式（f），式（g），式（h），式（i），式（j）：及其盐。

4. 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。

5. 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。

6. 发明申请

WO2004020417A1 2,4-DIAMINOQUINAZOLINE, 2-AMINO-4-HYDROXYPTERIDINE AND 2,4-DIAMINOPYRIMIDINE ESTER DERIVATIVES AS DIHYDROFOLATE REDUCTASE INHIBITORS 审中-公开
标题翻译： 2,4-二氨基喹唑啉，2-氨基-4-羟基喹啉和2,4-二氨基吡啶酯衍生物作为二氢呋喃糖酸盐还原酶抑制剂
公开(公告)号：WO2004020417A1
公开(公告)日：2004-03-11
申请号：PCT/GB2003/003704
申请日：2003-08-27
申请人： MELACURE THERAPEUTICS AB , PETT, Christopher, Phineas , BOMAN, Arne , LUNDSTEDT, Torbjorn , ANDERSSON, Per , SEIFERT, Elisabeth
发明人： BOMAN, Arne , LUNDSTEDT, Torbjorn , ANDERSSON, Per , SEIFERT, Elisabeth
IPC分类号： C07D239/95
CPC分类号： C07D239/48 , C07D239/95 , C07D487/04
摘要： This invention relates to novel esters of the general formula (III), which are Dihydrofolate Reductase Inhibitors; Wherein A is a heteroaromatic group, preferably selected from formula (a), formula (b), formula (c); Wherein R l is either hydrogen or CH 3 ; Wherein B is selected from formula (d), formula (e), formula (f), formula (g), formula (h), formula (i), formula (j): and salts thereof.
摘要翻译：本发明涉及通式（III）的新型酯类，它们是二氢叶酸还原酶抑制剂; 其中A是杂芳基，优选选自式（a），式（b），式（c）; 其中R1是氢或CH3; 其中B选自式（d），式（e），式（f），式（g），式（h），式（i），式（j）：及其盐。

7. 发明申请

WO2002081430A2 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：WO2002081430A2
公开(公告)日：2002-10-17
申请号：PCT/GB2002/001593
申请日：2002-04-05
申请人： MELACURE THERAPEUTICS AB , TOWLER, Philip, Dean , LUNDSTEDT, Torbjörn , ANDERSSON, Per , BOMAN, Arne , SEIFERT, Elisabeth , SKOTTNER, Anna
发明人： LUNDSTEDT, Torbjörn , ANDERSSON, Per , BOMAN, Arne , SEIFERT, Elisabeth , SKOTTNER, Anna
IPC分类号： 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。

8. 发明申请

WO2002068397A1 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：WO2002068397A1
公开(公告)日：2002-09-06
申请号：PCT/GB2002/000888
申请日：2002-02-28
申请人： MELACURE THERAPEUTICS AB , PETT, Christopher, Phineas , LUNDSTEDT, Torbjörn , HÄLLGREN, Anneli , ANDERSSON, Per , HALLBERG, Anders , NORDBERG, Malin, Graffner
发明人： LUNDSTEDT, Torbjörn , HÄLLGREN, Anneli , ANDERSSON, Per , HALLBERG, Anders , NORDBERG, Malin, Graffner
IPC分类号： C07D239/95
CPC分类号： C07D405/12 , C07D239/95 , C07D409/12
摘要： Compounds of the formula (I) wherein R 1 , R 2 , R 1 ' and R 2 ' are independently hydrogen or a group releasing the free amine in vivo , R 6 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：其中R 1，R“2，R”1“和R”2“的式（I）化合物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环系统或任选取代的具有有利的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。

9. 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。

10. 发明申请

WO2004020418A1 2,4- DIAMINO QUINAZOLINE AND PYRIDOPYRIMIDINE ESTER DERIVATIVES AS DIHYDROFOLATE REDUCTASE INHIBITORS 审中-公开
标题翻译： 2,4-二氨基喹唑啉和吡咯烷酮衍生物作为二氢叶酸还原酶抑制剂
公开(公告)号：WO2004020418A1
公开(公告)日：2004-03-11
申请号：PCT/GB2003/003714
申请日：2003-08-27
申请人： MELACURE THERAPEUTICS AB , PETT, Christopher, Phineas , HALLBERG, Anders , GRAFFNER-NORDBERG, Malin , BOMAN, Arne , SEIFERT, Elisabeth
发明人： HALLBERG, Anders , GRAFFNER-NORDBERG, Malin , BOMAN, Arne , SEIFERT, Elisabeth
IPC分类号： C07D239/95
CPC分类号： C07D239/95
摘要： The invention provides novel compounds of the formula 11: wherein R 1 , R 2 , R 3 and R 4 are independently hydrogen or a group that liberates the free amine in vivo , for example -CO-alkyl, preferably -CO-C 1 -C 3 alkyl or pivalate; or -COhaloalkyl, preferably -CO-C 1 -C 3 haloalkyl, most preferably -CO-C 1 -C 3 chloroalkyl; wherein W is; and @ denotes the points of attachment and wherein the ester can be located in either direction; wherein n and m are independently 0-5; wherein one but not both of X and Y can be nitrogen, or X is C-A and/or Y is C-B; wherein A and B are independently selected from hydrogen, alkyl optionally substituted with a halogen, an electron donor group such as amino, alkylamino, dialkylamino or hydroxy, or an electron acceptor group such as nitro, cyano, trihaloalkyl or amido, alkoxy or halogen; and pharmacologically acceptable salts thereof. Provided that when R 1 to R 4 are hydrogen, both X and Y are C-H, n is 1 and -(CH 2 ) n - is attached to the bridging oxygen of the ester group W, then m cannot be 0 or 1.
摘要翻译：本发明提供式11的新化合物：其中R 1，R 2，R 3和R 4独立地为氢或在体内释放游离胺的基团，例如-CO-烷基，优选-CO-C 1 -C 3烷基或特戊酸酯; 或-CO卤代烷基，优选-CO-C 1 -C 3卤代烷基，最优选-CO-C 1 -C 3氯代烷基; 其中W是; 和@表示连接点，并且其中酯可以位于任一方向上; 其中n和m独立地为0-5; 其中X和Y中的一个但不是二者可以是氮，或X是C-A和/或Y是C-B; 其中A和B独立地选自氢，任选被卤素取代的烷基，电子给体基团如氨基，烷基氨基，二烷基氨基或羟基，或电子受体基团如硝基，氰基，三卤代烷基或酰胺基，烷氧基或卤素; 及其药理学上可接受的盐。假设当R1至R4为氢时，X和Y均为C-H，n为1， - （CH2）n-连接到酯基W的桥连氧上，则m不能为0或1。

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