JP2006501295A5 - - Google Patents
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- JP2006501295A5 JP2006501295A5 JP2004540932A JP2004540932A JP2006501295A5 JP 2006501295 A5 JP2006501295 A5 JP 2006501295A5 JP 2004540932 A JP2004540932 A JP 2004540932A JP 2004540932 A JP2004540932 A JP 2004540932A JP 2006501295 A5 JP2006501295 A5 JP 2006501295A5
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- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- compound according
- halogen
- acceptable salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000000217 alkyl group Chemical group 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 239000011780 sodium chloride Substances 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 201000002674 obstructive nephropathy Diseases 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 229920000728 polyester Polymers 0.000 claims 3
- -1 6-trifluoromethyl-3-pyridyl Chemical group 0.000 claims 2
- 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 claims 2
- BRNULMACUQOKMR-UHFFFAOYSA-N Thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- RWRDLPDLKQPQOW-UHFFFAOYSA-N pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims 1
- 206010001897 Alzheimer's disease Diseases 0.000 claims 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N Azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- MVTLZJWNRRXFNW-UHFFFAOYSA-N FC1=C(C=C(C=C1)F)C1(CCC(CC1)[NH-])S(=O)(=O)C=1C=NC(=CC=1)C(F)(F)F Chemical compound FC1=C(C=C(C=C1)F)C1(CCC(CC1)[NH-])S(=O)(=O)C=1C=NC(=CC=1)C(F)(F)F MVTLZJWNRRXFNW-UHFFFAOYSA-N 0.000 claims 1
- YBBRCQOCSYXUOC-UHFFFAOYSA-N Sulfuryl chloride Chemical compound ClS(Cl)(=O)=O YBBRCQOCSYXUOC-UHFFFAOYSA-N 0.000 claims 1
- FYSNRJHAOHDILO-UHFFFAOYSA-N Thionyl chloride Chemical compound ClS(Cl)=O FYSNRJHAOHDILO-UHFFFAOYSA-N 0.000 claims 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N Trifluoromethanesulfonic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 150000008064 anhydrides Chemical class 0.000 claims 1
- 125000004429 atoms Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000006448 cycloalkyl cycloalkyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- YNAVUWVOSKDBBP-UHFFFAOYSA-N morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 1
- 229940113083 morpholine Drugs 0.000 claims 1
- 150000002829 nitrogen Chemical group 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 230000001225 therapeutic Effects 0.000 claims 1
Claims (10)
- 下記式I:
nは、1又は2であり;
R1は、CF3を表し、又はC1〜6アルキル、C2〜6アルケニル、C3〜9シクロアルキルもしくはC3〜6シクロアルキルC1〜6アルキル(これらはいずれも、ハロゲン、CN、CF3、OR3、COR3、CO2R3、OCOR4、SO2R4、N(R5)2、およびCON(R5)2から選択された2個以下の置換基を有していてもよい。)を表し、又は
R1は、アリール、アリールC1〜6アルキル、C−ヘテロシクリル又はC−ヘテロシクリルC1〜6アルキルを表し;
R2は、H又はC1〜4アルキルを表し;
R3は、H、C1〜4アルキル、フェニル又はヘテロアリールを表し;
R4は、C1〜4アルキル、フェニル又はヘテロアリールを表し;
R5は、H又はC1〜4アルキルを表し、又は2個のR5基とこれらが相互に結合している窒素原子とが一緒に、アゼチジン、ピロリジン、ピペリジン、モルホリン、チオモルホリン又はチオモルホリン−1,1−ジオキシド環を完成しており;
Ar1およびAr2は、フェニル又はヘテロアリールを独立に表し、これらのうちのいずれかは、ハロゲン、CN、NO2、CF3、CHF2、OH、OCF3、CHO、CH=NOH、C1〜4アルコキシ、C1〜4アルコキシカルボニル、C2〜6アシル、C2〜6アルケニルおよびC1〜4アルキル(これらは、ハロゲン、CN、NO2、CF3、OHおよびC1〜4アルコキシから選択された置換基を場合によって有する。)から独立に選択された0〜3個の置換基を有しており;
「アリール」は、いずれの存在においても、ハロゲン、CN、NO2、CF3、OCF3、OR3、COR3、CO2R3、OCOR4、N(R5)2、CON(R5)2および場合によって置換されているC1〜6アルキル、C1〜6アルコキシ、C2〜6アルケニル又はC2〜6アルケニルオキシ(この場合の置換基は、ハロゲン、CN、CF3、フェニル、OR3、CO2R3、OCOR4、N(R5)2およびCON(R5)2から選択される)から選択された3個以下の置換基を場合によって有するフェニル又はヘテロアリールを指し;ならびに
「C−へテロシクリル」および「N−へテロシクリル」は、いずれの存在においても、炭素又は窒素によって結合されたヘテロ環構造をそれぞれ指し、前記環構造は、非芳香族性であり、および10個以下の原子を含み、このうちの少なくとも1個は、O、N又はSであり、およびオキソ、ハロゲン、CN、NO2、CF3、OCF3、OR3、COR3、CO2R3、OCOR4、OSO2R4、N(R5)2、CON(R5)2および場合によって置換されているフェニル、C1〜6アルキル、C1〜6アルコキシ、C2〜6アルケニル又はC2〜6アルケニルオキシ(この場合の置換基は、ハロゲン、CN、CF3、OR3、CO2R3、OCOR4、N(R5)2、およびCON(R5)2から選択される。)から選択された3個以下の置換基を場合によって有する。)
の化合物又はその医薬適合性の塩。 - Ar1が、6−トリフルオロメチル−3−ピリジル、4−クロロフェニル又は4−トリフルオロメチルフェニルであり、Ar2が、2,5−ジフルオロフェニルである、請求項1に記載の化合物。
- R1が、CF3である、請求項1から3のいずれか一項に記載の化合物。
- トリフルオロメタンスルホン酸、N−[4−(2,5−ジフルオロフェニル)−4−(6−トリフルオロメチル−ピリジン−3−スルホニル)−シクロヘキシル]−アミドである、請求項4に記載の化合物又はその医薬適合性の塩。
- 請求項1から5のいずれか一項に記載の化合物又はその医薬適合性の塩および医薬適合性の担体を含む医薬組成物。
- 人体の治療方法に使用するための、請求項1から5のいずれか一項に記載の化合物又はその医薬適合性の塩。
- アルツハイマー病の治療薬又は予防薬を製造するための、請求項1から5のいずれか一項に記載の化合物又はその医薬適合性の塩の使用。
- 有効量の請求項1から5のいずれか一項に記載の化合物又はその医薬適合性の塩を被験者に投与することを含む、β−アミロイドの沈着を随伴する状態に罹患しているか、罹患しやすい被験者の治療方法。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0223038.1A GB0223038D0 (en) | 2002-10-04 | 2002-10-04 | Therapeutic compounds |
PCT/GB2003/004196 WO2004031139A1 (en) | 2002-10-04 | 2003-09-25 | Cyclohexyl sulphones as gamma-secretase inhibitors |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2006501295A JP2006501295A (ja) | 2006-01-12 |
JP2006501295A5 true JP2006501295A5 (ja) | 2006-11-02 |
JP4653486B2 JP4653486B2 (ja) | 2011-03-16 |
Family
ID=9945312
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004540932A Expired - Fee Related JP4653486B2 (ja) | 2002-10-04 | 2003-09-25 | ガンマ−セクレターゼ阻害剤としてのシクロヘキシルスルホン |
Country Status (9)
Country | Link |
---|---|
US (1) | US6890956B2 (ja) |
EP (1) | EP1551799B1 (ja) |
JP (1) | JP4653486B2 (ja) |
AT (1) | ATE464287T1 (ja) |
AU (1) | AU2003269211C1 (ja) |
CA (1) | CA2500969A1 (ja) |
DE (1) | DE60332137D1 (ja) |
GB (1) | GB0223038D0 (ja) |
WO (1) | WO2004031139A1 (ja) |
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EP0863134A1 (en) | 1997-03-07 | 1998-09-09 | Merck Frosst Canada Inc. | 2-(3,5-difluorophenyl)-3-(4-(methyl-sulfonyl)phenyl)-2-cyclopenten-1-one useful as an inhibitor of cyclooxygenase-2 |
HRP990246A2 (en) * | 1998-08-07 | 2000-06-30 | Du Pont Pharm Co | Succinoylamino benzodiazepines as inhibitors of a beta protein production |
MXPA01008606A (es) | 1999-02-26 | 2003-05-05 | Merck & Co Inc | Compuestos de sulfonamida novedosos y uso de los mismos. |
AU2001240861B2 (en) * | 2000-03-20 | 2006-03-30 | Merck Frosst Canada Ltd | Sulphonamido-substituted bridged bicycloalkyl derivatives |
GB0108591D0 (en) * | 2001-04-05 | 2001-05-23 | Merck Sharp & Dohme | Therapeutic agents |
AR035260A1 (es) * | 2001-08-03 | 2004-05-05 | Schering Corp | Derivados de piperidina amino sustituidas, composiciones farmaceuticas y el uso de dichos derivados para la preparacion de medicamentos como inhibidores de la gama secretasa, y para el tratamiento de la enfermedad de alzheimer |
TWI330176B (en) | 2001-12-27 | 2010-09-11 | Daiichi Seiyaku Co | Inhibitor against the production and secretion of amyloid protein |
DE10201392A1 (de) | 2002-01-16 | 2003-07-31 | Bayer Ag | Phenylsulfoxide und-sulfone |
-
2002
- 2002-10-04 GB GBGB0223038.1A patent/GB0223038D0/en not_active Ceased
-
2003
- 2003-09-25 AU AU2003269211A patent/AU2003269211C1/en not_active Ceased
- 2003-09-25 WO PCT/GB2003/004196 patent/WO2004031139A1/en active Application Filing
- 2003-09-25 CA CA002500969A patent/CA2500969A1/en not_active Abandoned
- 2003-09-25 JP JP2004540932A patent/JP4653486B2/ja not_active Expired - Fee Related
- 2003-09-25 EP EP03750987A patent/EP1551799B1/en not_active Expired - Lifetime
- 2003-09-25 DE DE60332137T patent/DE60332137D1/de not_active Expired - Lifetime
- 2003-09-25 AT AT03750987T patent/ATE464287T1/de not_active IP Right Cessation
- 2003-10-06 US US10/679,902 patent/US6890956B2/en not_active Expired - Lifetime
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