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

WO2007011065A2 INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
标题翻译：用于合成药物代理的中间体化合物及其生产方法
公开(公告)号：WO2007011065A2
公开(公告)日：2007-01-25
申请号：PCT/JP2006/314932
申请日：2006-07-21
申请人： MITSUBISHI PHARMA CORPORATION , SANOFI-AVENTIS , OKUYAMA, Masahiro , UEHARA, Fumiaki , IWAMURA, Hiroshi , WATANABE, Kazutoshi
发明人： OKUYAMA, Masahiro , UEHARA, Fumiaki , IWAMURA, Hiroshi , WATANABE, Kazutoshi
IPC分类号： C07D265/30 , C07D265/32
CPC分类号： C07D265/30 , C07D265/32
摘要： The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4']bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
摘要翻译：本发明涉及由式10表示的光学活性吗啉化合物的制备方法，其包括以下步骤：其中每个符号如说明书中所定义。本发明还涉及由式55表示的化合物的制备方法，其包括以下步骤：其中每个符号如说明书中所定义。根据本发明的制备方法，光学活性2-芳基取代的吗啉化合物和3-氧代-3-（嘧啶-4-基）丙酸酯作为合成2-（2-芳基吗啉） -4-基）-1-甲基-1H- [4,4']二嘧啶基-6-酮，其具有tau蛋白激酶1抑制活性，可用作阿尔茨海默氏病等的治疗药物，可以以高通过工业上有利的方法得到。

2. 发明申请

WO2003037888A1 3-SUBSTITUTED-4-PYRIMIDONE DERIVATIVES 审中-公开
标题翻译： 3-取代-4-吡啶酮衍生物
公开(公告)号：WO2003037888A1
公开(公告)日：2003-05-08
申请号：PCT/JP2002/009685
申请日：2002-09-20
申请人： MITSUBISHI PHARMA CORPORATION , SANOFI-SYNTHELABO , UEHARA, Fumiaki , ARITOMO, Keiichi , SHODA, Aya , HIKI, Shinsuke , OKUYAMA, Masahiro , USUI, Yoshihiro , OOIZUMI, Mitsuru , WATANABE, Kazutoshi , YAMAKOSHI, Koichi
发明人： UEHARA, Fumiaki , ARITOMO, Keiichi , SHODA, Aya , HIKI, Shinsuke , OKUYAMA, Masahiro , USUI, Yoshihiro , OOIZUMI, Mitsuru , WATANABE, Kazutoshi , YAMAKOSHI, Koichi
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D239/34 , C07D239/47 , C07D239/56 , C07D401/14 , C07D413/14
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1:wherein R 1 represents a C 1 -C 12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II):wherein R 2 and R 3 independently represent a hydrogen atom or a C 1 -C 8 alkyl group; R 4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
摘要翻译：由式（I）表示的嘧啶酮衍生物或其盐，或其溶剂化物或其水合物对tau蛋白激酶1具有抑制活性：其中R 1表示可被取代的C1-C12烷基; R表示例如由下式（II）表示的基团：其中R 2和R 3独立地表示氢原子或C 1 -C 8烷基; R 4表示可以被取代的苯环，可以被取代的萘环，可以被取代的茚满环，可被取代的四氢萘环，或被选择的具有1-4个杂原子的任意取代的杂环由氧原子，硫原子和氮原子组成的基团，并且总共具有5〜10个构成环的原子。

3. 发明申请

WO2005123676A1 BI- OR TETRA-GUANIDINO-BIPHENYL COMPOUNDS AS SMALL MOLECULE CARRIERS 审中-公开
标题翻译：作为小分子载体的双 - 或四联苯醌二联苯化合物
公开(公告)号：WO2005123676A1
公开(公告)日：2005-12-29
申请号：PCT/GB2005/002399
申请日：2005-06-17
申请人： UNIVERSITY COLLEGE LONDON , SELWOOD, David , VISINTIN , Christina , LAMAN, Heike , OKUYAMA, Masahiro
发明人： SELWOOD, David , VISINTIN , Christina , LAMAN, Heike , OKUYAMA, Masahiro
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , A61K47/54 , C07C279/08 , C07C279/24 , C07D213/70 , C07D213/71 , C07D311/86 , Y02P20/55
摘要： The invention relates to compounds of formula: I, or pharmaceutically acceptable a salts thereof, I wherein X 1 X 2 and X 3 are each independently where Y is an alkylene, alkenylene or alkynylene group, each of which may be optionally substituted with one or more substituents selected from alkyl, halo, CF 3 , OH, alkoxy, NH 2 , CN, NO 2 and COOH; W is absent or is O, S or NH; R l , R 2 , R 3 and R 4 are each independently selected from H, alkyl, aryl and a protecting group P l ; R 7 , R 8 and R 9 are each independently selected from H, alkyl, halo, CF 3 , OH, alkoxy, NH 2 , CN, NO 2 and COOH; q and r are each independently 1, 2, 3 or 4; q' and r' are each independently 0, 1, 2 or 3, where q + q' and r + r' each equal 4; p is 1, 2, 3, 4 or 5, and p' is 0, 1, 2, 3 or 4, where p + p' is 5; n is 0, 1, 2, 3....6; L is (Z) m NR 5 R 6 where Z is a hydrocarbyl group and m is 0 or 1; where R 5 and R 6 are each independently H, CO(CH 2 ) j Q 1 or C=S(NH)(CH 2 ) k Q 2 where j and k are each independently 0, 1, 2, 3, 4 or 5, and Q 1 and Q 2 are each independently selected from COOH, a chromophore or R 5 , R 6 and the nitrogen to which they are attached together form.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，其中X1 X2和X3各自独立地为Y为亚烷基，亚烯基或亚炔基，其各自可任选被一个或多个选自下列的取代基取代：烷基，卤素，CF 3，OH，烷氧基，NH 2，CN，NO 2和COOH; W不存在或是O，S或NH; R1，R2，R3和R4各自独立地选自H，烷基，芳基和保护基P1; R 7，R 8和R 9各自独立地选自H，烷基，卤素，CF 3，OH，烷氧基，NH 2，CN，NO 2和COOH; q和r各自独立地为1,2,3或4; q'和r'各自独立地为0,1,2或3，其中q + q'和r + r'各自等于4; p为1,2,3,4或5，p'为0,1,2,3或4，其中p + p'为5; n为0,1,2,3 ... 6; L是（Z）mNR 5 R 6，其中Z是烃基，m是0或1; 其中R 5和R 6各自独立地为H，CO（CH 2）j Q 1或C = S（NH）（CH 2）k Q 2，其中j和k各自独立地为0,1,2,3,4或5，并且Q1和Q2各自为独立地选自COOH，发色团或R 5，R 6和与它们相连的氮形成。

4. 发明申请

WO2004055007A1 3-SUBSTITUTED-4-PYRIMIDONE DERIVATIVES 审中-公开
标题翻译： 3-取代-4-吡啶酮衍生物
公开(公告)号：WO2004055007A1
公开(公告)日：2004-07-01
申请号：PCT/JP2003/015968
申请日：2003-12-12
申请人： MITSUBISHI PHARMA CORPORATION , SANOFI-SYNTHELABO , USUI, Yoshihiro , OKUYAMA, Masahiro , HANANO, Tokushi
发明人： USUI, Yoshihiro , OKUYAMA, Masahiro , HANANO, Tokushi
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor:wherein X represents CH or nitrogen atom; R 1 represents a C?1#191-C?12#191 alkyl group which may be substituted;R 2 represents a C?1#191-C?8#191 alkyl group which may be substituted, a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom, and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
摘要翻译：用作tau蛋白激酶1抑制剂的由式（I）表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物：其中X表示CH或氮原子; R> 1 <表示可以被取代的C 1〜191-C 12〜191烷基; R 2>表示可被取代的C 1〜19 C 19 -C 18烷基，苯可以被取代的萘环，可被取代的萘环，可被取代的茚满环，可被取代的四氢萘环，或具有1-4个选自氧原子的杂原子的任意取代的杂环，硫原子和氮原子，并且总共具有5至10个环构成原子。

5. 发明申请

WO2007011065A3 INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
标题翻译：用于合成药物的中间体化合物及其生产方法
公开(公告)号：WO2007011065A3
公开(公告)日：2007-08-16
申请号：PCT/JP2006314932
申请日：2006-07-21
申请人： MITSUBISHI PHARMA CORP , SANOFI AVENTIS , OKUYAMA MASAHIRO , UEHARA FUMIAKI , IWAMURA HIROSHI , WATANABE KAZUTOSHI
发明人： OKUYAMA MASAHIRO , UEHARA FUMIAKI , IWAMURA HIROSHI , WATANABE KAZUTOSHI
IPC分类号： C07D265/30 , C07D265/32
CPC分类号： C07D265/30 , C07D265/32
摘要： The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4']bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
摘要翻译：本发明涉及由式10表示的光学活性吗啉化合物的制备方法，其包括以下步骤：其中各符号如说明书中所定义。本发明还涉及由式55表示的化合物的制备方法，其包括以下步骤：其中每个符号如说明书中所定义。根据本发明的制备方法，可以使用作为2-（2-芳基吗啉）合成原料的重要的光学活性2-芳基取代的吗啉化合物和3-氧代-3-（嘧啶-4-基）丙酸酯 -4-基）-1-甲基-1H- [4,4']联嘧啶基-6-酮，可用作阿尔茨海默病等的治疗药物，具有τ蛋白激酶1抑制活性，通过工业上有利的方法获得产量。

6. 发明申请

WO2005080316A3 MODULATORS OF CANNABINOID RECEPTORS 审中-公开
标题翻译：大麻素受体的调节因子
公开(公告)号：WO2005080316A3
公开(公告)日：2005-11-03
申请号：PCT/GB2005000605
申请日：2005-02-21
申请人： UNIV LONDON , OKUYAMA MASAHIRO , SELWOOD DAVID , VISINTIN CRISTINA , BAKER DAVID , PRYCE GARETH
发明人： OKUYAMA MASAHIRO , SELWOOD DAVID , VISINTIN CRISTINA , BAKER DAVID , PRYCE GARETH
IPC分类号： C07C63/04 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/68 , C07C233/69 , C07C233/77 , C07C235/42 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , A61K31/167 , A61K31/192 , A61K31/216 , A61K31/235
CPC分类号： C07C235/42 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR or NR R wherein each of R and R is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR , COOR , NR R , CONR R , SO3H, SO2-R , SO2NR R and CF3, where each of R and R is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X-Y is other than meta-C=-C-(CH2)2CO2H, meta-C=-C-(CH2)2OH, meta-C=C-(CH2)2CO2Me, meta-(CH2)4CO2H, ortho-CH2CO2H, ortho-(CH2)2CO2H and ortho-(CH2)4CO2H; and (ii) when A is phenyl, n is 0, and Z is OMe, X-Y is other than meta-C=C-(CH2)4OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为OR 1或NR 1 R 2，其中R 1和R 2各自独立地为 H或烃基; X为亚烷基，亚烯基或亚炔基，其各自可任选被一个或多个选自烷基，COOH，CO 2 - 烷基，烯基，CN，NH 2，羟基，卤素，烷氧基，CF 3和硝基的取代基取代; Y是选自OH，NO 2，CN，COR 3，COOR 3，NR 3 R 4，CONR 3 R 4，SO 3 H，SO 2 -R 3的极性官能团， SO 2 NR 3 R 4和CF 3，其中R 3和R 4各自独立地为H或烃基; A是芳基或杂芳基，它们中的每一个可以任选被取代; 并且B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A为苯基，n为0且Z为OH时，XY不是间位C = -C-（CH 2）2 CO 2 H，间位C = -C-（CH 2）2 OH，（CH 2）2 CO 2 H，间 - （CH 2）4 CO 2 H，邻 - CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - 和（ii）当A是苯基时，n是0，并且Z是OMe，X-Y不同于间位C = C-（CH 2）4 OH。本发明的其他方面涉及这些化合物在制备用于治疗肌肉疾病，胃肠疾病或用于控制痉挛状态或震颤的药物中的用途。

7. 发明申请

WO2005080316A2 MODULATOR 审中-公开
标题翻译： CANNABINOID受体的调节剂
公开(公告)号：WO2005080316A2
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000605
申请日：2005-02-21
申请人： UNIVERSITY COLLEGE LONDON , OKUYAMA, Masahiro , SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth
发明人： OKUYAMA, Masahiro , SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth
IPC分类号： C07C233/68
CPC分类号： C07C235/42 , A61K31/165 , C07C69/76 , C07C69/78 , C07C233/11 , C07C233/65 , C07C233/66 , C07C233/69 , C07C235/34 , C07C235/78 , C07C235/84 , C07C237/32 , C07C237/38 , C07C237/42 , C07C255/41 , C07C255/44
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is OR 1 or NR 1 R 2 wherein each of R 1 and R 2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO 2 -alkyl, alkenyl, CN, NH 2 , hydroxy, halo, alkoxy, CF 3 and nitro; Y is a polar functional group selected from OH, NO 2 , CN, COR 3 , COOR 3 , NR 3 R 4 , CONR 3 R 4 , SO 3 H, SO 2 -R 3 , SO 2 NR 3 R 4 and CF 3 , where each of R 3 and R 4 is independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH 2 ) n where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X-Y is other than meta -C≡-C-(CH 2 ) 2 CO 2 H, meta -C≡-C-(CH 2 ) 2 OH, meta -C≡C-(CH 2 ) 2 CO 2 Me, meta -(CH 2 ) 4 CO 2 H, ortho -CH 2 CO 2 H, ortho -(CH 2 ) 2 CO 2 H and ortho -(CH 2 ) 4 CO 2 H; and (ii) when A is phenyl, n is 0, and Z is OMe, X-Y is other than meta -C≡C-(CH 2 ) 4 OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中Z为OR 1或NR 1 R 2，其中R 1和R 2各自独立地为 H或烃基; X是亚烷基，亚烯基或亚炔基，其各自可以任选地被一个或多个选自烷基，COOH，CO 2 - 烷基，烯基，CN，NH 2，羟基，卤素，烷氧基，CF 3和硝基的取代基取代; Y是选自OH，NO 2，CN，COR 3，COOR 3，NR 3 R 4，CONR 3 R 4，SO 3 H，SO 2 -R 3的极性官能团。，SO 2 NR 3 R 4和CF 3，其中R 3和R 4各自独立地为H或烃基; A是芳基或杂芳基，其各自可以任选被取代; 和B是（CH 2）n，其中n是0,1,2,3,4或5; 条件是：（i）当A是苯基时，n是0，Z是OH，XY不是间位-C = -C-（CH 2）2 CO 2 H，间位C = -C-（CH 2）2 OH，间 - C（C-（CH 2）2 CO 2 Me，间 - （CH 2）4 CO 2 H，邻-CH 2 CO 2 H，邻 - （CH 2）2 CO 2 H和邻 - （CH 2）4 CO 2 H; 和（ii）当A是苯基时，n是0，Z是OMe，X-Y不是间位C = C-（CH 2）4 OH。本发明的其它方面涉及这些化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。

8. 发明申请

WO2006067450A3 MODULATOR 审中-公开
标题翻译：调制器
公开(公告)号：WO2006067450A3
公开(公告)日：2006-09-14
申请号：PCT/GB2005004990
申请日：2005-12-21
申请人： UCL BIOMEDICA PLC , SELWOOD DAVID , VISINTIN CRISTINA , BAKER DAVID , PRYCE GARETH , OKUYAMA MASAHIRO
发明人： SELWOOD DAVID , VISINTIN CRISTINA , BAKER DAVID , PRYCE GARETH , OKUYAMA MASAHIRO
IPC分类号： C07C39/15 , A61K31/05 , A61K31/055 , A61K31/165 , A61K31/167 , A61P21/00 , C07C37/055 , C07C37/11 , C07C37/62 , C07C39/06 , C07C39/27 , C07C39/367 , C07C45/00 , C07C59/90 , C07C67/343 , C07C233/03 , C07C233/25 , C07C235/26 , C07C235/34 , C07D213/02 , C07D213/30
CPC分类号： C07D213/30 , C07C37/055 , C07C37/18 , C07C37/62 , C07C39/15 , C07C39/367 , C07C41/30 , C07C45/004 , C07C59/90 , C07C67/343 , C07C233/25 , C07C235/34 , C07C49/84 , C07C69/738 , C07C43/205 , C07C39/06 , C07C39/27 , C07C39/12
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R 1 and R 2 are each independently H or alkyl; Y is an alkyl group, CONR 3 R 4 , COOR 5 SO 2 NR 16 R 17 , NHSO 2 R 18 or CN; X is an aryl or heteroaryl group, each of which may be optionally substituted with one or more substituents selected from (CH2) m Z where Z is halogen, OH, CN, alkyl, alkoxy, NO 2 , CF 3 , CONR 6 R 7 , CN, NR 8 R 9 , COOR 10 or NHCOR 11, and m is 0 to 3; R 3 to R 11 are each independently H, alkyl or aryl, wherein said alkyl and aryl groups are optionally substituted by one or more substituents selected from halogen, OH, CN, alkyl, alkoxy, NO 2 , CF 3 , CONR 12 R 13 , CN, NH 2 , COOR 14 , NHCOR 15 , and CN; R 12 to R 18 are each independently H or alkyl, more preferably H or Me; n is 1 to 6; wherein the compound is other than 3' ,5'-dimethyl-4-(1,1-dimethylheptyl)-1,1'-biphenyl-2-ol. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中R 1和R 2各自独立地为H或烷基; Y是烷基，CONR 3，R 4，COOR 5，SO 2，NR 16，或者CN;其中R 1，R 2，R 3，R 4， X是芳基或杂芳基，其各自可以任选地被一个或多个选自（CH 2）m Z的取代基取代，其中Z是卤素，OH，CN，烷基，烷氧基，NO > 2 ，CF 3，CONR 6，R 7，CN，NR 8 R SUP > 9，COOR 10或NHCOR 11，和m为0至3; R 3至R 11各自独立地为H，烷基或芳基，其中所述烷基和芳基任选被一个或多个选自以下的取代基取代：卤素，OH，CN，烷基，烷氧基，NO 2，CF 3，CONR 12，R 13，CN，NH 2 COOR 14，NHCOR 15和CN; R 12至R 18各自独立地为H或烷基，更优选为H或Me; n为1至6; 其中所述化合物不是3'，5'-二甲基-4-（1,1-二甲基庚基）-1,1'-联苯-2-醇。本发明的其它方面涉及这样的化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。

9. 发明申请

WO2006067450A2 MODULATOR 审中-公开
标题翻译：调制器
公开(公告)号：WO2006067450A2
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004990
申请日：2005-12-21
申请人： UCL BIOMEDICA PLC , SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth , OKUYAMA, Masahiro
发明人： SELWOOD, David , VISINTIN, Cristina , BAKER, David , PRYCE, Gareth , OKUYAMA, Masahiro
IPC分类号： C07C37/055 , C07C37/11 , C07C37/62 , C07C39/06 , C07C39/15 , C07C39/27 , C07C39/367 , C07C45/00 , C07C59/90 , C07C67/343 , C07C233/25 , C07C235/34 , C07D213/30
CPC分类号： C07D213/30 , C07C37/055 , C07C37/18 , C07C37/62 , C07C39/15 , C07C39/367 , C07C41/30 , C07C45/004 , C07C59/90 , C07C67/343 , C07C233/25 , C07C235/34 , C07C49/84 , C07C69/738 , C07C43/205 , C07C39/06 , C07C39/27 , C07C39/12
摘要： The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof, Formula (I), wherein R 1 and R 2 are each independently H or alkyl; Y is an alkyl group, CONR 3 R 4 , COOR 5 SO 2 NR 16 R 17 , NHSO 2 R 18 or CN; X is an aryl or heteroaryl group, each of which may be optionally substituted with one or more substituents selected from (CH2) m Z where Z is halogen, OH, CN, alkyl, alkoxy, NO 2 , CF 3 , CONR 6 R 7 , CN, NR 8 R 9 , COOR 10 or NHCOR 11, and m is 0 to 3; R 3 to R 11 are each independently H, alkyl or aryl, wherein said alkyl and aryl groups are optionally substituted by one or more substituents selected from halogen, OH, CN, alkyl, alkoxy, NO 2 , CF 3 , CONR 12 R 13 , CN, NH 2 , COOR 14 , NHCOR 15 , and CN; R 12 to R 18 are each independently H or alkyl, more preferably H or Me; n is 1 to 6; wherein the compound is other than 3' ,5'-dimethyl-4-(1,1-dimethylheptyl)-1,1'-biphenyl-2-ol. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐，式（I）其中R 1和R 2各自独立地为H或烷基; Y是烷基，CONR 3，R 4，COOR 5，SO 2，NR 16，或者CN;其中R 1，R 2，R 3，R 4， X是芳基或杂芳基，其各自可以任选地被一个或多个选自（CH 2）m Z的取代基取代，其中Z是卤素，OH，CN，烷基，烷氧基，NO > 2 ，CF 3，CONR 6，R 7，CN，NR 8 R SUP > 9，COOR 10或NHCOR 11，和m为0至3; R 3至R 11各自独立地为H，烷基或芳基，其中所述烷基和芳基任选被一个或多个选自以下的取代基取代：卤素，OH，CN，烷基，烷氧基，NO 2，CF 3，CONR 12，R 13，CN，NH 2 COOR 14，NHCOR 15和CN; R 12至R 18各自独立地为H或烷基，更优选为H或Me; n为1至6; 其中该化合物不是3'，5'-二甲基-4-（1,1-二甲基庚基）-1,1'-联苯-2-醇。本发明的其它方面涉及这样的化合物在制备用于治疗肌肉疾病，胃肠道疾病或用于控制痉挛或震颤的药物中的用途。

10. 发明申请

WO2004085408A1 2, 3, 6-TRISUBSTITUTED-4-PYRIMIDONE DERIVATIVES 审中-公开
标题翻译： 2,3,6-取代的4-吡啶酮衍生物
公开(公告)号：WO2004085408A1
公开(公告)日：2004-10-07
申请号：PCT/JP2004/004320
申请日：2004-03-26
申请人： MITSUBISHI PHARMA CORPORATION , SANOFI-SYNTHELABO , WATANABE, Kazutoshi , UEHARA, Fumiaki , HIKI, Shinsuke , YOKOSHIMA, Satoshi , USUI, Yoshihiro , OKUYAMA, Masahiro , SHODA, Aya , ARITOMO, Keiichi , KOHARA, Toshiyuki , FUKUNAGA, Kenji
发明人： WATANABE, Kazutoshi , UEHARA, Fumiaki , HIKI, Shinsuke , YOKOSHIMA, Satoshi , USUI, Yoshihiro , OKUYAMA, Masahiro , SHODA, Aya , ARITOMO, Keiichi , KOHARA, Toshiyuki , FUKUNAGA, Kenji
IPC分类号： C07D239/47
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C 1 -C 12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C 1 -C 8 alkyl group, an optionally partially hydrogenated C 6 -C 10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each Y independently represents a halogen atom, a hydroxy group, a cyano group, a C 1 -C 6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C 2 -C 6 alkylene group.
摘要翻译：具有由式（I）表示的tau蛋白激酶1抑制活性的嘧啶酮衍生物或其盐或其溶剂合物或其水合物; 可用于疾病的预防和/或治疗性治疗，例如神经变性疾病（例如阿尔茨海默病）; 其中Q表示CH或氮原子; R代表C1-C12烷基; 式（I）的环表示哌嗪环或哌啶环; 每个X独立地表示C1-C8烷基，任选部分氢化的C 6 -C 10芳基环，茚满环等; m表示1〜3的整数，每个Y独立地表示卤素原子，羟基，氰基，C1-C6烷基等; n表示0〜8的整数，当X和Y或两个Y基团连接在同一个碳原子上时，它们可以彼此结合形成C 2 -C 6亚烷基。

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