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NOVEL COMPOUND THAT SPECIFICALLY BINDS TO AMPA RECEPTOR NEW

外国特許コード F170009020
整理番号 (S2015-1685-N0)
掲載日 2017年3月29日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2016JP069896
国際公開番号 WO 2017006931
国際出願日 平成28年7月5日(2016.7.5)
国際公開日 平成29年1月12日(2017.1.12)
優先権データ
  • 特願2015-135124 (2015.7.6) JP
発明の名称 (英語) NOVEL COMPOUND THAT SPECIFICALLY BINDS TO AMPA RECEPTOR NEW
発明の概要(英語) The present invention provides a compound represented by formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof. This compound is capable of specifically binding to an AMPA receptor, and shows extremely high brain uptake. (In the formula, each of A and Z independently represents CO, SO or SO2; each of X and Y independently represents S or O; each of R1-R4 independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group or a halogen group; each R5 independently represents an alkyl group, an alkenyl group, an alkynyl group or a halogen group; and n represents an integer of 0-4.)
特許請求の範囲(英語) [claim1]
1. The salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine formula (i):
(In formula,
A and Z is, in the respective independence, CO, SO or SO [2];
X and Y, in the respective independence, is S or O;
R (1)-R (4), in the respective independence, hydrogen, is alkyl, [arukeniru], [arukiniru] or the halo;
R (5), in the respective independence, is alkyl, [arukeniru], [arukiniru] or the halo in every appearance;
n is integer of the 0-4;
However, 2- [2,6 - [jihuruoro] - 4- ({2- [(phenyl sulfonyl) amino] ethyl} thio) phenoxy] acetamide, 4- [2- (4 - [kurorohuenirusuruhoniruamino]) ethyl thio] - 2,6 - [jihuruorohuenokishiasetoamido], N and [N]-jimechiru - 4- [2- (4 - [kurorohuenirusuruhoniruamino]) ethyl thio] - 2,6 - [jihuruorohuenokishiasetoamido], 4- [2- (4 - [kurorohuenirusuruhoniruamino]) ethyl thio] - 2 - fluoro phenoxy acetamide, N and [N]-jimechiru - 4- [2- (4 - [kurorohuenirusuruhoniruamino]) ethyl thio] - 2 - fluoro phenoxy acetamide, N and [N]-jimechiru - 4- [2- (phenyl sulfonyl amino) ethyl thio] - 2,6- [jihuruorohuenokishiasetoamido], 4- [2- (phenyl sulfonyl amino) ethyl thio] - 2 - fluoro phenoxy acetamide, and N and [N]-jimechiru - 4- [2- (phenyl sulfonyl amino) ethyl thio] - 2 - fluoro phenoxy acetamide is excluded.).
[claim2]
2. R (1)-R (4) everything, there are no times when it becomes hydrogen, the chemical compound of claim 1 statement.
[claim3]
3. A and Z is, in the respective independence, CO or SO [2], claim the chemical compound of 1 or 2 statements.
[claim4]
4. A is SO [2], at the same time Z is CO, either of the claim 1-3 the chemical compound of one section statement.
[claim5]
5. X is S, at the same time Y is O, either of the claim 1-4 the chemical compound of one section statement.
[claim6]
6. R (2) is alkyl, either of the claim 1-5 the chemical compound of one section statement.
[claim7]
7. R (1) is alkyl or the halo, either of the claim 1-6 the chemical compound of one section statement.
[claim8]
8. R (3) and R (4) one side inside it is hydrogen, another side is alkyl, either of the claim 1-7 the chemical compound of one section statement.
[claim9]
9. R (5) is the halo, either of the claim 1-8 the chemical compound of one section statement.
[claim10]
10. The aforementioned halo is fluoro, the chemical compound of claim 9 statement.
[claim11]
11. N is 2, either of the claim 1-10 the chemical compound of one section statement.
[claim12]
12. It is selected from the group which consists of description below, either of the claim 1-11 the chemical compound of one section statement:
.
[claim13]
13. The salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine formula (i):
(In formula,
A and Z is, in the respective independence, CO, SO or SO [2];
X and Y, in the respective independence, is S or O;
R (1)-R (4), in the respective independence, hydrogen, is alkyl, [arukeniru], [arukiniru] or the halo;
R (5), in the respective independence, is alkyl, [arukeniru], [arukiniru] or the halo in every appearance;
n is integer of the 0-4;
1 or the atom above that is the radioisotope of the said atom).
[claim14]
14. The aforementioned radioisotope, (11) C or (18) is F, the salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine of claim 13 statement.
[claim15]
15. The basis which includes the radioisotope is R (1), the salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine of claim 14 statement.
[claim16]
16. The basis which includes the radioisotope is R (2), the salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine of claim 14 statement.
[claim17]
17. The basis which includes the radioisotope is R (3) and R (4) at least one side, the salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine of claim 14 statement.
[claim18]
18. It is selected from the group which consists of description below, the chemical compound of claim 14 statement:
.
[claim19]
19. The salt or the solvent dishes dressed with sauce which it can allow either of the claim 1-18 as the chemical compound or that medicine of one section statement are included, the composition.
[claim20]
20. ***A-amino - 3 - Hydroxy - 5 - methyl - 4 - [isokisazoru] - can be used in order imaging to do the propionic acid receptor, the composition of claim 19 statement.
[claim21]
21. It is for PET imaging, the composition of claim 20 statement.
[claim22]
22. The salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine formula (i):
(In formula,
A and Z is, in the respective independence, CO, SO or SO [2];
X and Y, in the respective independence, is S or O;
R (1)-R (4), in the respective independence, hydrogen, is alkyl, [arukeniru], [arukiniru] or the halo;
R (5), in the respective independence, is alkyl, [arukeniru], [arukiniru] or the halo in every appearance;
n is integer of the 0-4.)
It includes, ***.alpha.-amino - 3 - hydroxy - 5 - methyl - 4 - [isokisazoru] - the composition which is used in order imaging to do the propionic acid receptor.
[claim23]
23. Being production method of the salt or the solvent dishes dressed with sauce which it can allow as the chemical compound or that medicine formula (i):
(In formula,
A and Z is, in the respective independence, CO, SO or SO [2];
X and Y, in the respective independence, is S or O;
R (1), R (3) and R (4), in the respective independence, hydrogen, is alkyl, [arukeniru], [arukiniru] or the halo;
R (2), is alkyl, [arukeniru] or [arukiniru];
R (5), in the respective independence, is alkyl, [arukeniru], [arukiniru] or the halo in every appearance;
n is integer of the 0-4.);
The salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine formula (ii):
(In formula, A, X, Y, Z and R (1), R (3), R (4), R (5), and n is the same as those which are defined at description above.)The X (1)-R (2) (in formula, R (2) is same as those which are defined at description above, X (1) is halogen.)With the fact that it reacts is included, the aforementioned production method.
[claim24]
24. The description above R (2), [(11) is C] alkyl, production method of claim 23 statement.
[claim25]
25. R in aforementioned formula (i) and formula (ii) (3) and R (4), in each case is hydrogen, claim production method of 23 or 24 statements.
[claim26]
26. Being production method of the salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine formula (i):
(In formula,
A and Z is, in the respective independence, CO, SO or SO [2];
X and Y, in the respective independence, is S or O;
R (1), is alkyl, [arukeniru] or [arukiniru];
R (2)-R (4), in the respective independence, hydrogen, is alkyl, [arukeniru], [arukiniru] or the halo;
R (5), in the respective independence, is alkyl, [arukeniru], [arukiniru] or the halo in every appearance;
n is integer of the 0-4.);
The salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine formula (iii):
(In formula, A, X, Y, Z and R (2), R (3), R (4), R (5), and n is the same, as those which are defined at description above R (a), in the respective independence, is alkyl, [arukeniru] or [arukiniru].)The X (1)-R (1) (in formula, R (1) is same as those which are defined at description above, X (1) is halogen.)With the fact that it reacts is included, the aforementioned production method.
[claim27]
27. The aforementioned reaction, the palladium catalyst, the phosphine ligand, is done under existing of carbonate and the halogenation copper, production method of claim 26 statement.
[claim28]
28. The description above R (1), [(11) is C] alkyl, claim production method of 26 or 27 statements.
[claim29]
29. The intermediate field which is displayed by formula (iii):
(In formula,
A and Z is, in the respective independence, CO, SO or SO [2];
X and Y, in the respective independence, is S or O;
R (2)-R (4), in the respective independence, hydrogen, is alkyl, [arukeniru], [arukiniru] or the halo;
R (5), in the respective independence, is alkyl, [arukeniru], [arukiniru] or the halo in every appearance;
n is integer of the 0-4;
At the same time
R (a), in the respective independence, it is alkyl, [arukeniru] or [arukiniru].).
[claim30]
30. It is displayed by the below-mentioned structure, the intermediate field of claim 29 statement:
.
[claim31]
31. The salt or the solvent dishes dressed with sauce which it can allow as the chemical compound, or that medicine formula (i):
(In formula,
A and Z is, in the respective independence, CO, SO or SO [2];
X and Y, in the respective independence, is S or O;
R (1)-R (4), in the respective independence, hydrogen, is alkyl, [arukeniru], [arukiniru] or the halo;
R (5), in the respective independence, is alkyl, [arukeniru], [arukiniru] or the halo in every appearance;
n is integer of the 0-4.)
It possesses the process which detects the radiation which is given out from the brain of the suffering *** body which is prescribed, imaging method of the AMPA receptor.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • YOKOHAMA CITY UNIVERSITY
  • NATIONAL INSTITUTES FOR QUANTUM AND RADIOLOGICAL SCIENCE AND TECHNOLOGY
  • 発明者(英語)
  • TAKAHASHI TAKUYA
  • MIYAZAKI TOMOYUKI
  • SUHARA TETSUYA
  • HIGUCHI MAKOTO
  • CHO MEIEI
国際特許分類(IPC)
指定国 (WO201706931)
National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
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