JP2017071603A5 - - Google Patents
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- JP2017071603A5 JP2017071603A5 JP2016198584A JP2016198584A JP2017071603A5 JP 2017071603 A5 JP2017071603 A5 JP 2017071603A5 JP 2016198584 A JP2016198584 A JP 2016198584A JP 2016198584 A JP2016198584 A JP 2016198584A JP 2017071603 A5 JP2017071603 A5 JP 2017071603A5
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- Prior art keywords
- substituted
- unsubstituted
- alkyl
- ring
- halogen
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000011780 sodium chloride Substances 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000004432 carbon atoms Chemical group C* 0.000 claims 4
- 150000001924 cycloalkanes Chemical class 0.000 claims 4
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 150000002916 oxazoles Chemical class 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003216 pyrazines Chemical class 0.000 claims 1
- 150000004892 pyridazines Chemical class 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Substances C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- 150000003222 pyridines Chemical class 0.000 claims 1
- 150000003230 pyrimidines Chemical class 0.000 claims 1
Claims (5)
(式中、
Xは−S−または−O−であり、
(i)Xが−S−であるとき、
R3aはアルキル、ハロアルキル、ヒドロキシアルキルまたはアルキルオキシアルキルであり、
R2aはハロゲン、アルキルオキシまたはハロアルキルオキシであり、かつ
R3aがハロアルキルであるとき、R2aはアルキルでもよく、
R2bはHであり、
R2aおよびR2bが、それらが結合している炭素原子と一緒になって置換されたシクロアルカンを形成してもよく、
R2aおよびR2bが、それらが結合している炭素原子と一緒になって置換されたシクロアルカンを形成するとき、R3aはHでもよく、
(ii)Xが−O−であるとき、
R3aはアルキルオキシおよびシクロアルキルから選択される一以上の基で置換されていてもよいハロアルキル、またはハロゲンから選択される一以上の基で置換されているシクロアルキルであり、
R2aはH、ハロゲン、アルキル、アルキルオキシまたはハロアルキルオキシであり、
R2bはHであり、
R2aおよびR2bが、それらが結合している炭素原子と一緒になって置換されたシクロアルカンを形成してもよく、
R2aおよびR2bが、それらが結合している炭素原子と一緒になって置換されたシクロアルカンを形成するとき、R3aはHまたはアルキルでもよく、
R3bはHまたはアルキルであり、
であってもよく、
環Aは置換若しくは非置換の芳香族炭素環、置換若しくは非置換の非芳香族炭素環、置換若しくは非置換の芳香族複素環または置換若しくは非置換の非芳香族複素環であり、
環Bは置換若しくは非置換の芳香族炭素環、置換若しくは非置換の非芳香族炭素環、置換若しくは非置換の芳香族複素環または置換若しくは非置換の非芳香族複素環であり、
R1は置換若しくは非置換のアルキル、置換若しくは非置換のアルケニル、置換若しくは非置換のアルキニルまたは置換若しくは非置換のシクロアルキルであり、
R5はハロゲンまたは置換若しくは非置換のアルキルであり、
nは0〜2の整数であり、
ただし、以下の化合物を除く。
(1)Xが−O−であり、R3aがCH2FまたはCF3であり、R3bがHであり、R2aがHであり、かつR2bがHである化合物、
(2)Xが−O−であり、R3aがCHF2であり、R3bがHであり、R2aがOMeであり、かつR2bがHである化合物、および、
(3)以下の化合物:
で示される化合物またはその製薬上許容される塩。 Formula (I):
(Where
X is —S— or —O—;
(I) when X is -S-
R 3a is alkyl, haloalkyl, hydroxyalkyl or alkyloxyalkyl;
R 2a is halogen, alkyloxy or haloalkyloxy, and when R 3a is haloalkyl, R 2a may be alkyl;
R 2b is H;
R 2a and R 2b together with the carbon atom to which they are attached may form a substituted cycloalkane;
When R 2a and R 2b together with the carbon atom to which they are attached form a substituted cycloalkane, R 3a may be H;
(Ii) when X is -O-
R 3a is haloalkyl optionally substituted with one or more groups selected from alkyloxy and cycloalkyl, or cycloalkyl substituted with one or more groups selected from halogen;
R 2a is H, halogen, alkyl, alkyloxy or haloalkyloxy,
R 2b is H;
R 2a and R 2b together with the carbon atom to which they are attached may form a substituted cycloalkane;
When R 2a and R 2b together with the carbon atom to which they are attached form a substituted cycloalkane, R 3a may be H or alkyl;
R 3b is H or alkyl;
May be,
Ring A is a substituted or unsubstituted aromatic carbocyclic ring, a substituted or unsubstituted nonaromatic carbocyclic ring, a substituted or unsubstituted aromatic heterocyclic ring or a substituted or unsubstituted nonaromatic heterocyclic ring,
Ring B is a substituted or unsubstituted aromatic carbocyclic ring, a substituted or unsubstituted non-aromatic carbocyclic ring, a substituted or unsubstituted aromatic heterocyclic ring or a substituted or unsubstituted non-aromatic heterocyclic ring,
R 1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or substituted or unsubstituted cycloalkyl;
R 5 is halogen or substituted or unsubstituted alkyl;
n is an integer from 0 to 2,
However, the following compounds are excluded.
(1) a compound wherein X is —O—, R 3a is CH 2 F or CF 3 , R 3b is H, R 2a is H , and R 2b is H,
(2) a compound wherein X is —O—, R 3a is CHF 2 , R 3b is H, R 2a is OMe and R 2b is H, and
(3) The following compounds:
Or a pharmaceutically acceptable salt thereof .
環Aが
(式中、R 4 はHまたはハロゲンであり、−Z=は−CH=または−N=である)
であり;
環Bが置換若しくは非置換のピリジン、置換若しくは非置換のピラジン、置換若しくは非置換のピリミジン、置換若しくは非置換のピリダジンまたは置換若しくは非置換のオキサゾールである、請求項1または2記載の化合物またはその製薬上許容される塩。 R 3a is CH 2 F in Formula (I), CHF 2, CF 3, CH ( F) CH 3 or CF 2 CH 3, R 3b is Ri H or CH 3 der; R 2a is H, F, CH 3 , OCH 3 or OCH 2 CF 3 ; R 1 is alkyl;
Ring A is
(Wherein R 4 is H or halogen, -Z = is -CH = or -N =)
Is;
The compound according to claim 1 or 2, wherein ring B is substituted or unsubstituted pyridine, substituted or unsubstituted pyrazine, substituted or unsubstituted pyrimidine, substituted or unsubstituted pyridazine or substituted or unsubstituted oxazole, or a compound thereof Pharmaceutically acceptable salt.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2015200650 | 2015-10-09 | ||
JP2015200650 | 2015-10-09 |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2017071603A JP2017071603A (en) | 2017-04-13 |
JP2017071603A5 true JP2017071603A5 (en) | 2019-11-14 |
Family
ID=58538542
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016198584A Pending JP2017071603A (en) | 2015-10-09 | 2016-10-07 | Pharmaceutical composition comprising dihydrothiazine or dihydrooxazine derivative |
Country Status (1)
Country | Link |
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JP (1) | JP2017071603A (en) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2511268B2 (en) † | 2009-12-11 | 2021-02-17 | Shionogi & Co., Ltd. | Oxazine derivative |
CA3098430A1 (en) | 2018-04-27 | 2019-10-31 | Shionogi & Co., Ltd. | Tetrahydropyranooxazine derivatives having selective bace1 inhibitory activity |
WO2020009179A1 (en) * | 2018-07-06 | 2020-01-09 | Shionogi & Co., Ltd. | Fused heterocyclic derivatives having selective bace1 inhibitory activity |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2151435A4 (en) * | 2007-04-24 | 2011-09-14 | Shionogi & Co | Pharmaceutical composition for treatment of alzheimer's disease |
CA2683887A1 (en) * | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group having inhibitory activity against production of amyloid beta protein |
EP2703401A4 (en) * | 2011-04-26 | 2014-12-03 | Shionogi & Co | Pyridine derivative and bace-1 inhibitor containing same |
NZ625684A (en) * | 2012-01-26 | 2016-02-26 | Hoffmann La Roche | Fluoromethyl-5,6-dihydro-4h-[1,3]oxazines |
MX2015014083A (en) * | 2013-04-11 | 2016-07-26 | Hoffmann La Roche | Bace1 inhibitors. |
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2016
- 2016-10-07 JP JP2016198584A patent/JP2017071603A/en active Pending