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1. 发明申请

WO2006121390A8 BENZOIC ACID DERIVATIVES THAT ARE MODULATORS OR AGONISTS OF GLYR 审中-公开
标题翻译：作为GLYR的调节剂或激动剂的苯甲酸衍生物
公开(公告)号：WO2006121390A8
公开(公告)日：2007-11-15
申请号：PCT/SE2006000547
申请日：2006-05-08
申请人： ASTRAZENECA AB , MOLIN BERIT , GYBAECK HELENA , HAEBERLEIN MARKUS , JONASSON CATRIN , KIHLSTROEM JACOB , PLOBECK NIKLAS , HETTMAN ANDREAS , VIKLUND JENNY , YNGVE ULRIKA
发明人： GYBAECK HELENA , HAEBERLEIN MARKUS , JONASSON CATRIN , KIHLSTROEM JACOB , PLOBECK NIKLAS , HETTMAN ANDREAS , VIKLUND JENNY , YNGVE ULRIKA , MOLIN HAAKAN
IPC分类号： C07C65/10 , A61K31/192 , A61P29/00 , C07C65/32 , C07C309/30 , C07C327/16
CPC分类号： C07C323/62 , C07C65/105 , C07C65/24 , C07C65/40 , C07C205/45 , C07C229/64 , C07C251/48 , C07C255/57 , C07C317/46 , C07C2601/14 , C07D213/32 , C07D213/34 , C07D213/55 , C07D213/70 , C07D215/14 , C07D217/16 , C07D241/42 , C07D271/06 , C07D277/36 , C07D277/64 , C07D295/155 , C07D307/80 , C07D309/04 , C07D333/60
摘要： Compounds of formula I, wherein Y = H, -OH, halo, -OC 1-6 alkyl, -C 1-6 alkyl, the two latter optionally substituted with halo, -CN, -OH, -CF 3 , -NH 2 ; Rl = -C 3-6 cycloaUcyl, heterocycloalkyl, aryl, alkylaryl, heteroaryl, -C 3-6 -alkyl, optionally substituted with halo, -CN, -OH, -CF 3 , -OCF 3 , -NH 2 , -CONH 2 ; M = -C(O)-, -C(H 2 )-, -CH(OR 3 )-, -N(R a )-, -S(O) r -, heteroaryl and a bond; wherein R a = H or C 1-6 alkyl and r = 0, 1 or 2; R2 = H, halo, -CN, or D = -C 1-6 alkyl, C 3-6 cycloalkyl, heterocycloalkyl, -N(CH 3 ) 2 , aryl, alkylaryl, heteroaryl, and heterocyclic groups; where D is optionally substituted with G = halo, -NO 2 , -CN, -OH, -CF 3 , -OCF 3 , -NH 2 , -CONH 2 , -COOH, aryl, heteroaryl, heterocyclic groups, -C 1-6 alkyl, -C 1-6 alkoxy, heterocycloalkyl, and C 1-6 alkylcarboxylate; where D may be connected to G by L = -C(O)-, -S-, or -S(O 2 )-; and G may be further substituted with substituents selected from halo, -NO 2 , -CN, -OH, -CH 3 , -OCH 3 , -CF 3 , -OCF 3 , -NH 2 , -CONH 2 , -COOH, C 1-6 alkylcarboxylate; and R3 = -OH or C 1-6 alkoxy.
摘要翻译：式I化合物，其中Y = H，-OH，卤素，-OC 1-6烷基，-C 1-6烷基，后两个任选被卤代，-CN，-OH，-CF 3，-NH 2，环烷基，芳基，烷基芳基，杂芳基，-C 3-6烷基，任选被卤素，-CN，-OH，-NH 2， -CF 3，-OCF 3，-NH 2，-CONH 2 2， M（= O） - ， - C（H 2） - ， - CH（OR 3） - ， - N（R a）） - ， - S（O）r - ，杂芳基和键; 其中R 1 = H或C 1-6烷基并且r = 0,1或2; R 2 = H，卤素，-CN或D = -C 1-6烷基，C 3-6环烷基，杂环烷基，-N（CH 3）），芳基，烷芳基，杂芳基和杂环基; 其中D任选被G =卤素，-NO 2，-CN，-OH，-CF 3，-OCF 3，-OCF 3取代， NH 2，-CONH 2，-COOH，芳基，杂芳基，杂环基，-C 1-6烷基，-C≡CONH2， 1-6烷氧基，杂环烷基和C 1-6烷基羧酸酯; 其中D可以通过L = -C（O） - ， - S-或-S（O _{2） - 连接到G; 并且G可以进一步被选自卤素，-NO 2，-CN，-OH，-CH 3，-OCH 3，，-CF 3，-OCF 3，-NH 2，-CONH 2，-COOH，C 1 -C 4烷基， SUB> 1-6 烷基羧酸; 和R3 = -OH或C 1-6烷氧基。}

2. 发明申请

WO2006121390A2 NEW COMPOUNDS II 审中-公开
标题翻译：新化合物II
公开(公告)号：WO2006121390A2
公开(公告)日：2006-11-16
申请号：PCT/SE2006000547
申请日：2006-05-08
申请人： ASTRAZENECA AB , GYBAECK HELENA , HAEBERLEIN MARKUS , JONASSON CATRIN , KIHLSTROEM JACOB , MOLIN HAAKAN , PLOBECK NIKLAS , SVENSSON ANDREAS , VIKLUND JENNY , YNGVE ULRIKA
发明人： GYBAECK HELENA , HAEBERLEIN MARKUS , JONASSON CATRIN , KIHLSTROEM JACOB , MOLIN HAAKAN , PLOBECK NIKLAS , SVENSSON ANDREAS , VIKLUND JENNY , YNGVE ULRIKA
IPC分类号： C07C65/10 , A61K31/192 , A61P29/00 , C07C65/32 , C07C309/30 , C07C327/16
CPC分类号： C07C323/62 , C07C65/105 , C07C65/24 , C07C65/40 , C07C205/45 , C07C229/64 , C07C251/48 , C07C255/57 , C07C317/46 , C07C2601/14 , C07D213/32 , C07D213/34 , C07D213/55 , C07D213/70 , C07D215/14 , C07D217/16 , C07D241/42 , C07D271/06 , C07D277/36 , C07D277/64 , C07D295/155 , C07D307/80 , C07D309/04 , C07D333/60
摘要： Compounds of formula I, wherein Y = H, -OH, halo, -OC 1-6 alkyl, -C 1-6 alkyl, the two latter optionally substituted with halo, -CN, -OH, -CF 3 , -NH 2 ; Rl = -C 3-6 cycloaUcyl, heterocycloalkyl, aryl, alkylaryl, heteroaryl, -C 3-6 -alkyl, optionally substituted with halo, -CN, -OH, -CF 3 , -OCF 3 , -NH 2 , -CONH 2 ; M = -C(O)-, -C(H 2 )-, -CH(OR 3 )-, -N(R a )-, -S(O) r -, heteroaryl and a bond; wherein R a = H or C 1-6 alkyl and r = 0, 1 or 2; R2 = H, halo, -CN, or D = -C 1-6 alkyl, C 3-6 cycloalkyl, heterocycloalkyl, -N(CH 3 ) 2 , aryl, alkylaryl, heteroaryl, and heterocyclic groups; where D is optionally substituted with G = halo, -NO 2 , -CN, -OH, -CF 3 , -OCF 3 , -NH 2 , -CONH 2 , -COOH, aryl, heteroaryl, heterocyclic groups, -C 1-6 alkyl, -C 1-6 alkoxy, heterocycloalkyl, and C 1-6 alkylcarboxylate; where D may be connected to G by L = -C(O)-, -S-, or -S(O 2 )-; and G may be further substituted with substituents selected from halo, -NO 2 , -CN, -OH, -CH 3 , -OCH 3 , -CF 3 , -OCF 3 , -NH 2 , -CONH 2 , -COOH, C 1-6 alkylcarboxylate; and R3 = -OH or C 1-6 alkoxy.
摘要翻译：式I的化合物，其中Y = H，-OH，卤素，-OC 1-6烷基，-C 1-6烷基，后者任选被卤素，-CN，-OH，-CF 3，-NH 2， R 1 = -C 3-6环烷基，杂环烷基，芳基，烷基芳基，杂芳基，-C 3-6 - 烷基，任选被卤素，-CN，-OH， -CF 3，-OCF 3，-NH 2，-CONH 2， M = -C（O） - ， - C（H 2 - ） - ， - CH（OR 3） - ， - N（R a） - ） - ， - S（O） - ， - 杂芳基和一个键; 其中R a = H或C 1-6烷基，r = 0,1或2; R 2 = H，卤素，-CN或D = -C 1-6烷基，C 3-6环烷基，杂环烷基，-N（CH 3） 2，芳基，烷基芳基，杂芳基和杂环基; 其中D任选被G =卤素，-NO 2，-CN，-OH，-CF 3，-OCF 3 - ， - NH 2，-CONH 2，-COOH，芳基，杂芳基，杂环基，-C 1-6烷基，-C 1-6烷氧基，杂环烷基和C 1-6烷基羧酸酯; 其中D可以通过L = -C（O） - ， - S-或-S（O）2 - ）与G连接。并且G可以进一步被选自卤素，-NO 2，-CN，-OH，-CH 3，-OCH 3 N的取代基取代。，-CF 3，-OCF 3，-NH 2，-CONH 2，-COOH，C 1〜 SUB> 1-6 烷基羧酸; 并且R 3 = -OH或C 1-6烷氧基。

3. 发明公开

EP1981883A4 NOVEL HETEROARYL SUBSTITUTED BENZOTHIAZOLES 审中-公开
标题翻译：新杂 - 苯并噻唑
公开(公告)号：EP1981883A4
公开(公告)日：2010-10-06
申请号：EP07709290
申请日：2007-01-25
申请人： ASTRAZENECA AB
发明人： GRAVENFORS YLVA , JONASSON CATRIN , MALMSTROEM JONAS , NORDVALL GUNNAR , PYRING DAVID , SLIVO CAN , SOHN DANIEL , STROEM PETER , WENSBO DAVID
IPC分类号： C07D417/04 , A61K31/4436 , A61K31/496 , A61P25/28 , C07D417/14 , C07D513/04
CPC分类号： C07D417/04 , C07B59/002 , C07D513/04

4. 发明公开

EP1890993A4 BENZOIC ACID DERIVATIVES THAT ARE MODULATORS OR ANTAGONISTS OF GLYR 审中-公开
标题翻译： BENZOEDERIVATE THAT调节剂或：GlyRS拮抗剂是
公开(公告)号：EP1890993A4
公开(公告)日：2010-09-08
申请号：EP06733399
申请日：2006-05-08
申请人： ASTRAZENECA AB
发明人： GYBAECK HELENA , HAEBERLEIN MARKUS , JONASSON CATRIN , KIHLSTROEM JACOB , MOLIN HAAKAN , PLOBECK NIKLAS , HETTMAN ANDREAS , VIKLUND JENNY , YNGVE ULRIKA , MOLIN BERIT
IPC分类号： C07C65/10 , A61K31/192 , A61P29/00 , C07C65/32 , C07C309/30 , C07C327/16
CPC分类号： C07C323/62 , C07C65/105 , C07C65/24 , C07C65/40 , C07C205/45 , C07C229/64 , C07C251/48 , C07C255/57 , C07C317/46 , C07C2601/14 , C07D213/32 , C07D213/34 , C07D213/55 , C07D213/70 , C07D215/14 , C07D217/16 , C07D241/42 , C07D271/06 , C07D277/36 , C07D277/64 , C07D295/155 , C07D307/80 , C07D309/04 , C07D333/60

5. 发明专利

ZA200806075B NOVEL HETEROARYL SUBSTITUTED BENZOTHIAZOLES 未知
公开(公告)号：ZA200806075B
公开(公告)日：2012-12-27
申请号：ZA200806075
申请日：2008-07-11
申请人： ASTRAZENECA AB
发明人： GRAVENFORS YLVA , JONASSON CATRIN , MALMSTROM JONAS , NORDVALL GUNNAR , PYRING DAVID , SLIVO CAN , SOHN DANIEL , STROM PETER
IPC分类号： A61K20060101 , A61P20060101 , C07D20060101
摘要： The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.

6. 发明专利

NZ569667A Novel heteroaryl substituted benzothiazoles 未知
公开(公告)号：NZ569667A
公开(公告)日：2011-09-30
申请号：NZ56966707
申请日：2007-01-25
申请人： ASTRAZENECA AB
发明人： GRAVENFORS YLVA , JONASSON CATRIN , MALMSTROM JONAS , NORDVALL GUNNAR , PYRING DAVID , SLIVO CAN , SOHN DANIEL , STROM PETER , WENSBO DAVID
IPC分类号： C07D417/04 , A61K31/4436 , A61K31/496 , A61P25/28 , C07D417/14 , C07D513/04
摘要： Disclosed herein is a compound 2-[6-(methylamino)pyridine-3-yl]-1,3-benzothiazol-6-ol wherein one or more of the atoms are optionally a detectable isotope; as a free base or a pharmaceutically acceptable salt, solvate or solvate of a salt thereof. Also disclosed is { N-methyl-11C]-2-(6-(methylamino)pyridine-3-yl]-benzothiazole-6-ol. Use of said compounds in the manufacture of a medicament for measuring amyloid deposits in a subject, wherein the measuring of amyloid deposits comprises a) administering a detectable quantity of a composition comprising said compounds and b) detecting the binding of the compound to amyloid deposit in the subject. Such compounds are also useful in the treatment of Alzheimer's disease, familial Alzheimer's disease, cognitive deficit in Schizophrenia, Down 's syndrome and homozygotes for the apolipoprotein E4 allele.

7. 发明专利

BRPI0707283A2 未知
公开(公告)号：BRPI0707283A2
公开(公告)日：2011-04-26
申请号：BRPI0707283
申请日：2007-01-25
申请人： ASTRAZENECA AB
发明人： GRAVENFORS YLVA , JONASSON CATRIN , MALMSTROEM JONAS , NORDVALL GUNNAR , PYRING DAVID , SLIVO CAN , SOHN DANIEL , STROEM PETER , WENSBO DAVID
IPC分类号： C07D417/04 , A61K31/4436 , A61K31/496 , A61P25/28 , C07D417/14 , C07D513/04
摘要： The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.

8. 发明专利

BRPI0610240A2 未知
公开(公告)号：BRPI0610240A2
公开(公告)日：2012-09-25
申请号：BRPI0610240
申请日：2006-05-08
申请人： ASTRAZENECA AB
发明人： GYBACK HELENA , JONASSON CATRIN , KIHLSTROEM JACOB , MOLIN HAKAN , PLOBECK NIKLAS , HETTMAN ANDREAS , VIKLUND JENNY , HAEBERLEIN MARKUS , YNGVE ULRIKA
IPC分类号： C07C65/10 , A61K31/192 , A61P29/00 , C07C65/32 , C07C309/30 , C07C327/16
摘要： Compounds of formula I, wherein R1, Z, Y, M and R2 are as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical composition containing the same, methods of using the same for therapeutic purposes and methods of making the same.

9. 发明专利

NO20083394L 未知
公开(公告)号：NO20083394L
公开(公告)日：2008-10-02
申请号：NO20083394
申请日：2008-08-01
申请人： ASTRAZENECA AB
发明人： NORDVALL GUNNAR , SOHN DANIEL , JONASSON CATRIN , GRAVENFORS YLVA , MALMSTROM JONAS , PYRING DAVID , SLIVO CAN , STROM PETER , WENSBO DAVID
IPC分类号： C07D417/04
摘要： The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.

10. 发明专利

MX2007013879A DERIVADOS DE ACIDO BENZOICO QUE SON MODULADORES O AGONISTAS DE RECEPTORES INHIBITORIOS DE GLICINA. 未知
公开(公告)号：MX2007013879A
公开(公告)日：2008-01-24
申请号：MX2007013879
申请日：2006-05-08
申请人： ASTRAZENECA AB
发明人： HAEBERLEIN MARKUS , PLOBECK NIKLAS , GYBACK HELENA , JONASSON CATRIN , KIHLSTROM JACOB , HETTMAN ANDREAS , VIKLUND JENNY , YNGVE ULRIKA , MOLIN HAKAN
IPC分类号： C07C65/10 , A61K31/192 , A61P29/00 , C07C65/32 , C07C309/30 , C07C327/16
摘要： Se describen los compuestos de la formula I (ver formula I) en donde Y se selecciona de hidrogeno, -OH, halo, -O(alquilo de 1 a 6 atomos de carbono), y alquilo de 1 a 6 atomos de carbono, los dos ultimos estan opcionalmente sustituidos con halo, -CN, -OH, -CF3, -NH2; R1 se selecciona de cicloalquilo de 3 a 6 atomos de carbono, heterocicloalquilo, arilo, alquilarilo, heteroarilo, y alquilo de 3 a 6 atomos de carbono, opcionalmente sustituidos con halo, -CN, -OH, -CF3, -OCF3, -NH2, -CONH2; M se selecciona de -C(O)-, -C(H2)-, -CH(OR3)-, -N(OH)-, -N(Ra)-, -S(0)r, heteroarilo y un enlace; en donde Ra es hidrogeno o alquilo de 1 a 6 atomos de carbono y r es 0, 1 o 2; R2 se selecciona ya sea de hidrogeno, halo, -CN, o es un grupo D seleccionado de alquilo de 1 a 6 atomos de carbono, cicloalquilo de 3 a 6 atomos de carbono, heterocicloalquilo, -N(CH3)2, arilo, alquilarilo, heteroarilo, y grupos heterociclicos; donde D esta opcionalmente sustituido con G seleccionados de halo, -NO2, -CN, -OH, -CF3, -OCF3, -NH2, -CONH2, -COOH, arilo, heteroarilo, grupos heterociclicos, alquilo de 1 a 6 atomos de carbono, alcoxi de 1 a 6 atomos de carbono, heterocicloalquilo, y carboxilatos de alquilo de 1 a 6 atomos de carbono; donde D puede estar opcionalmente conectado a G por un grupo ligador L seleccionado de -C(O)-, -S-, and -S(O2)-; y G, si es sustituible, esta opcionalmente sustituido ademas con uno o mas sustituyentes seleccionados de halo, -NO2, -CN, -OH, -CH3, -OCH3, -CF3, -OCF3, -NH2, -CONH2, -COOH, y carboxilato de alquilo de 1 a 6 atomos de carbono; y R3 se selecciona de -OH y alcoxi de 1 a 6 atomos de carbono; con la condicion de cuando M sea un enlace y R3 sea -OH, entonces R2 no sea alquilo de 1 a 6 atomos de carbono, y que cuando M sea -C(O)- entonces R2 no sea hidrogeno o -CH3.

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