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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明申请

WO2003013509A1 N-PHENYLPYRROLE GUANIDINE DERIVATIVES AS MELANOCORTIN RECEPTION LIGANDS 审中-公开
标题翻译：作为MELANOCORTIN接收配体的N-苯基吡咯烷酮衍生物
公开(公告)号：WO2003013509A1
公开(公告)日：2003-02-20
申请号：PCT/GB2002/003620
申请日：2002-08-06
申请人： MELACURE THERAPEUTICS AB , LUNDSTEDT, Torbjörn , SKOTTNER, Anna , BOMAN, Arne , ANDERSSON, Per , SEIFERT, Elisabeth , ANDRIANOV, Victor
发明人： LUNDSTEDT, Torbjörn , SKOTTNER, Anna , BOMAN, Arne , ANDERSSON, Per , SEIFERT, Elisabeth , ANDRIANOV, Victor
IPC分类号： A61K31/402
CPC分类号： C07D207/335 , C07D207/34 , C07D207/36 , C07D207/38 , C07D207/42
摘要： The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or treatment of disorders in the melanocortin system: wherein the variables are as defined in the claims; and the pharmacologically active salts thereof.
摘要翻译：本发明提供作为黑皮质素受体的配体和/或黑皮质素系统中的疾病的治疗的通式（I）的新化合物：其中变量如权利要求中所定义; 及其药理学活性盐。

6. 发明申请

WO2008071980A1 NOVEL AMINOGUANIDINES AS MELANOCORTIN RECEPTOR LIGANDS. 审中-公开
标题翻译：新的氨基葡萄糖作为MELANOCORTIN受体配体。
公开(公告)号：WO2008071980A1
公开(公告)日：2008-06-19
申请号：PCT/GB2007/004793
申请日：2007-12-13
申请人： ACURE PHARMA AB , PETT, Christopher, Phineas , LUNDSTEDT, Torbjörn , SEIFERT, Elisabeth , LEK, Per , BOMAN, Arne
发明人： LUNDSTEDT, Torbjörn , SEIFERT, Elisabeth , LEK, Per , BOMAN, Arne
IPC分类号： C07C281/18 , C07D339/08 , A61K31/155 , A61K31/385 , A61P29/00
CPC分类号： C07D339/08 , C07C281/18 , C07C323/48
摘要： There are described compounds of general formula (I) and isomeric forms thereof wherein n is 0,1,2 or 3, saturated or unsaturated; most preferably at least one of R 1 to R 5 represents halogen; at least one of R 1 , R 2 , R 3 , R 4 and R 5 is selected from -S-R or -COOR, or two or more Of R 1 -R 5 comprise a linking group such as -S-(CH2) m S-, where m is 1, 2 or 3 and R is selected from alkyl having 1 to 5 carbon atoms, cycloalkyl having 3-6 carbon atoms, hydroxy, and aryl having 6 to 10 carbon atoms, such groups being optionally substituted, and when R 1 is selected from -S-R, then at least one of R 2 , R 3 and R 5 is most preferably selected from halogen; and R 1 , R 2 , R 3 , R 4 and R 5 are otherwise 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 pharmacologically acceptable salts thereof. Compounds described have activity on the melanocortin receptors and have application in the treatment of a wide range of inflammatory, arthritic or central nerve regeneration conditions.
摘要翻译：描述了通式（I）的化合物及其异构体形式，其中n为0,1,2或3，饱和或不饱和; 最优选R 1至R 5中的至少一个表示卤素; R 1，R 2，R 3，R 4和R 5中的至少一个， / SUB>选自-SR或-COOR，或者R 1 -R 5中的两个或更多个包含连接基团，例如-S-（CH 2）_{5 <>最优选选自卤素; 和R 1，R 2，R 3，R 4和R 5，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，选自氰基，硝基，三氟烷基或酰胺的电子受体基团; 烷基氨基，苯甲酰氧基，硝酰基，苯基或磺基; 及其药理学上可接受的盐。所描述的化合物对黑皮质素受体具有活性，并且可用于治疗广泛的炎性，关节炎或中枢神经再生条件。}

7. 发明申请

WO2006092619A1 METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF NEUROLOGICAL DAMAGE 审中-公开
标题翻译：用于治疗神经损伤的方法和药物组合物
公开(公告)号：WO2006092619A1
公开(公告)日：2006-09-08
申请号：PCT/GB2006/000774
申请日：2006-03-06
申请人： ACURE PHARMA AB , BAILEY, Lindsey , LUNDSTEDT, Torbjörn , SKOTTNER, Anna , SEIFERT, Elisabeth , LEK, Per , BOMAN, Arne
发明人： LUNDSTEDT, Torbjörn , SKOTTNER, Anna , SEIFERT, Elisabeth , LEK, Per , BOMAN, Arne
IPC分类号： A61K31/155 , A61P25/00
CPC分类号： A61K31/155
摘要： The invention relates to a method of treating neurological damage, preferably spinal chord injury, said treatment comprising the topical administration of guanabenz. The invention also relates to the use of guanabenz for the preparation of a medicament for the treatment of neurological damage, preferably spinal chord injury, wherein said treatment comprises the topical administration of guanabenz to the site of said neurological damage. The invention is also directed to pharmaceutical compositions comprising guanabenz wherein said compositions are in the form of an aqueous gel or non-aqueous ointment.
摘要翻译：本发明涉及一种治疗神经损伤的方法，优选脊髓损伤，所述治疗包括局部给予胍那苯。本发明还涉及胍苯醌用于制备用于治疗神经损伤（优选脊髓损伤）的药物的用途，其中所述治疗包括将神经系统局部施用于所述神经损伤部位。本发明还涉及包含胍苯甲酸酯的药物组合物，其中所述组合物为水性凝胶或非水性软膏剂的形式。

8. 发明申请

WO2011012868A1 COMPOUNDS FOR TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的化合物
公开(公告)号：WO2011012868A1
公开(公告)日：2011-02-03
申请号：PCT/GB2010/001457
申请日：2010-07-30
申请人： ANAMAR AB , PALMQVIST, Niklas , SJÖDIN, Anders , WENGLÉN, Christina , FLOOD, Christofer , LUNDBERG, Lennart , SEIFERT, Elisabeth , LEK, Per , BOMAN, Arne , WEBBER, Philip, Michael
发明人： PALMQVIST, Niklas , SJÖDIN, Anders , WENGLÉN, Christina , FLOOD, Christofer , LUNDBERG, Lennart , SEIFERT, Elisabeth , LEK, Per , BOMAN, Arne
IPC分类号： A61P29/00 , A61K31/155 , A61K31/36 , A61K31/385
CPC分类号： A61K31/385 , A61K31/155 , A61K31/36
摘要： The present invention relates to the use of benzylideneaminoguanidines for the treatment of inflammation and pain. In one preferred embodiment, the invention relates to the use of N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine for the treatment of rheumatoid arthritis.
摘要翻译：本发明涉及用于治疗炎症和疼痛的亚苄氨基鸟嘌呤的用途。在一个优选的实施方案中，本发明涉及N-（2-氯-3,4-二甲氧基亚苄基氨基）胍用于治疗类风湿性关节炎的用途。

9. 发明申请

WO2008058679A3 NOVEL AMIDES ACTING ON THE ADENOSINE RECEPTORS 审中-公开
公开(公告)号：WO2008058679A3
公开(公告)日：2008-05-22
申请号：PCT/EP2007/009721
申请日：2007-11-09
申请人： ACURE PHARMA AB , LUNDSTEDT, Torbjörn , SEIFERT, Elisabeth , LEK, Per , BOMAN, Arne
发明人： LUNDSTEDT, Torbjörn , SEIFERT, Elisabeth , LEK, Per , BOMAN, Arne
IPC分类号： C07K5/023 , C07K5/027 , A61K38/05 , A61P19/02
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.

10. 发明公开

EP1383740A2 NOVEL BENZYLIDENEAMINO GUANIDINES AND THEIR USES AS LIGANDS TO THE MELANOCORTIN RECEPTORS 审中-公开
标题翻译： BENZYLIDENAMINOGUANIDINE及其作为黑皮质素受体配体使用
公开(公告)号：EP1383740A2
公开(公告)日：2004-01-28
申请号：EP02707026.7
申请日：2002-04-05
申请人： Melacure Therapeutics AB
发明人： LUNDSTEDT, Torbjörn , ANDERSSON, Per , BOMAN, Arne , SEIFERT, Elisabeth , SKOTTNER, Anna
IPC分类号： C07C281/18 , A61K31/155 , A61P29/00
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.

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