JP2005513123A5 - - Google Patents
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- Publication number
- JP2005513123A5 JP2005513123A5 JP2003554629A JP2003554629A JP2005513123A5 JP 2005513123 A5 JP2005513123 A5 JP 2005513123A5 JP 2003554629 A JP2003554629 A JP 2003554629A JP 2003554629 A JP2003554629 A JP 2003554629A JP 2005513123 A5 JP2005513123 A5 JP 2005513123A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halogen
- group
- phenyl
- alkoxy
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 125
- 229910052736 halogen Inorganic materials 0.000 claims 79
- 150000002367 halogens Chemical class 0.000 claims 79
- 125000003545 alkoxy group Chemical group 0.000 claims 33
- 125000001424 substituent group Chemical group 0.000 claims 31
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 29
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 22
- 125000004076 pyridyl group Chemical group 0.000 claims 21
- -1 cyan Chemical group 0.000 claims 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 14
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 13
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 13
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 13
- 125000003342 alkenyl group Chemical group 0.000 claims 12
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 11
- 125000004571 thiomorpholin-4-yl group Chemical group N1(CCSCC1)* 0.000 claims 11
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 125000004414 alkyl thio group Chemical group 0.000 claims 7
- 125000002541 furyl group Chemical group 0.000 claims 7
- 125000002971 oxazolyl group Chemical group 0.000 claims 7
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 7
- 125000002883 imidazolyl group Chemical group 0.000 claims 5
- 125000000842 isoxazolyl group Chemical group 0.000 claims 5
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims 5
- 125000003831 tetrazolyl group Chemical group 0.000 claims 5
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 5
- 125000000335 thiazolyl group Chemical group 0.000 claims 5
- 125000005032 thiofuranyl group Chemical group S1C(=CC=C1)* 0.000 claims 5
- 125000001425 triazolyl group Chemical group 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000004174 2-benzimidazolyl group Chemical group [H]N1C(*)=NC2=C([H])C([H])=C([H])C([H])=C12 0.000 claims 3
- 125000004981 cycloalkylmethyl group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 125000004129 indan-1-yl group Chemical group [H]C1=C([H])C([H])=C2C(=C1[H])C([H])([H])C([H])([H])C2([H])* 0.000 claims 2
- 125000004130 indan-2-yl group Chemical group [H]C1=C([H])C([H])=C2C(=C1[H])C([H])([H])C([H])(*)C2([H])[H] 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 231100000252 nontoxic Toxicity 0.000 claims 2
- 230000003000 nontoxic effect Effects 0.000 claims 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34432201P | 2001-12-20 | 2001-12-20 | |
| PCT/US2002/040605 WO2003053912A1 (en) | 2001-12-20 | 2002-12-20 | α-(N-SULPHONAMIDO)ACETAMIDE DERIVATIVES AS β-AMYLOID INHIBITORS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009027648A Division JP5030982B2 (ja) | 2001-12-20 | 2009-02-09 | β−アミロイドインヒビターとしてのα−（Ｎ−スルホンアミド）アセトアミド誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005513123A JP2005513123A (ja) | 2005-05-12 |
| JP2005513123A5 true JP2005513123A5 (https=) | 2006-01-05 |
| JP4287746B2 JP4287746B2 (ja) | 2009-07-01 |
Family
ID=23350031
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003554629A Expired - Fee Related JP4287746B2 (ja) | 2001-12-20 | 2002-12-20 | β−アミロイドインヒビターとしてのα−（Ｎ−スルホンアミド）アセトアミド誘導体 |
| JP2009027648A Expired - Fee Related JP5030982B2 (ja) | 2001-12-20 | 2009-02-09 | β−アミロイドインヒビターとしてのα−（Ｎ−スルホンアミド）アセトアミド誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009027648A Expired - Fee Related JP5030982B2 (ja) | 2001-12-20 | 2009-02-09 | β−アミロイドインヒビターとしてのα−（Ｎ−スルホンアミド）アセトアミド誘導体 |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US7300936B2 (https=) |
| EP (1) | EP1465861B1 (https=) |
| JP (2) | JP4287746B2 (https=) |
| KR (1) | KR100966705B1 (https=) |
| CN (1) | CN1289469C (https=) |
| AT (1) | ATE430727T1 (https=) |
| AU (1) | AU2002357333B2 (https=) |
| BR (1) | BR0215182A (https=) |
| CA (1) | CA2471099C (https=) |
| CO (1) | CO5590894A2 (https=) |
| CY (1) | CY1109275T1 (https=) |
| DE (1) | DE60232276D1 (https=) |
| DK (1) | DK1465861T3 (https=) |
| ES (1) | ES2325205T3 (https=) |
| GE (1) | GEP20063920B (https=) |
| HR (1) | HRP20040566A2 (https=) |
| HU (1) | HUP0500173A3 (https=) |
| IL (2) | IL162498A0 (https=) |
| IS (1) | IS2879B (https=) |
| MX (1) | MXPA04005927A (https=) |
| NO (1) | NO328976B1 (https=) |
| NZ (1) | NZ533603A (https=) |
| PL (1) | PL204281B1 (https=) |
| PT (1) | PT1465861E (https=) |
| RS (1) | RS51155B (https=) |
| RU (1) | RU2300518C2 (https=) |
| SI (1) | SI1465861T1 (https=) |
| UA (1) | UA78537C2 (https=) |
| WO (1) | WO2003053912A1 (https=) |
| ZA (1) | ZA200404811B (https=) |
Families Citing this family (56)
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| CN1289469C (zh) * | 2001-12-20 | 2006-12-13 | 布里斯托尔-迈尔斯斯奎布公司 | α－(N－磺酰氨基)乙酰胺衍生物作为β－淀粉样蛋白抑制剂 |
| CN100562516C (zh) | 2001-12-27 | 2009-11-25 | 第一制药株式会社 | β-淀粉样蛋白产生和分泌的抑制剂 |
| US7279491B2 (en) | 2002-10-23 | 2007-10-09 | Janssen Pharmaceutica N.V. | Phenylpiperidines and phenylpyrrolidines |
| US20070043079A1 (en) * | 2003-04-18 | 2007-02-22 | Hiromu Habashita | Heterocyclic compound containing nitrogen atom and use thereof |
| CA2526487A1 (en) | 2003-06-30 | 2005-01-06 | Daiichi Pharmaceutical Co., Ltd. | Heterocyclic methyl sulfone derivative |
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US8193389B2 (en) | 2004-03-11 | 2012-06-05 | Elan Pharmaceuticals, Inc. | N-substituted benzene sulfonamides |
| US7163942B2 (en) * | 2004-04-01 | 2007-01-16 | Pfizer Inc. | Sulfonamide compounds for the treatment of neurodegenerative disorders |
| MY149038A (en) * | 2004-05-26 | 2013-07-15 | Eisai R&D Man Co Ltd | Cinnamide compound |
| US7144894B2 (en) * | 2004-09-23 | 2006-12-05 | Bristol-Myers Squibb Company | Sulfonamide bicyclic compounds |
| CA2580119A1 (en) | 2004-10-26 | 2006-05-04 | Eisai R & D Management Co., Ltd. | Amorphous object of cinnamide compound |
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| EP1953151A4 (en) * | 2005-11-18 | 2010-06-02 | Eisai R&D Man Co Ltd | SALTS FROM A CYNNAMIDE COMPOUND OR SOLVATE THEREOF |
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| CN102786447A (zh) * | 2011-08-01 | 2012-11-21 | 四川大学 | N,n-二取代芳基磺酰胺类化合物及其制备方法和用途 |
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| US9993005B2 (en) | 2013-03-14 | 2018-06-12 | Georgia State University Research Foundation, Inc. | Preventing or delaying chill injury response in plants |
| DK3330259T3 (da) | 2015-07-27 | 2020-08-10 | Chong Kun Dang Pharmaceutical Corp | 1,3,4-oxadiazolamidderivativ-forbindelse som histondeacetylase-6-inhibitor og farmaceutisk sammensætning indeholdende denne |
| ES2774510T3 (es) | 2015-07-27 | 2020-07-21 | Chong Kun Dang Pharmaceutical Corp | Derivados de 1,3,4-oxadiazol sulfamida como inhibidores de histona desacetilasa 6 y composición farmacéutica que comprende los mismos |
| FI3328843T3 (fi) * | 2015-07-27 | 2023-01-31 | 1,3,4-oksadiatsolisulfonamidijohdannaisyhdisteitä histonideasetylaasi-6:n inhibiittoreina ja samaa käsittävä farmaseuttinen koostumus | |
| RU2709207C2 (ru) | 2015-08-04 | 2019-12-17 | Чонг Кун Данг Фармасьютикал Корп. | 1,3,4-оксадиазольные производные соединения в качестве ингибитора гистондеацетилазы 6 и фармацевтическая композиция, содержащая их |
| HRP20230201T1 (hr) | 2015-10-12 | 2023-03-31 | Chong Kun Dang Pharmaceutical Corp. | Oksadiazol aminski spojevi derivati kao inhibitor histonske deacetilaze 6 i farmaceutska kompozicija koja sadrži iste |
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| KR102316234B1 (ko) | 2018-07-26 | 2021-10-22 | 주식회사 종근당 | 히스톤 탈아세틸화효소 6 억제제로서의 1,3,4-옥사다이아졸 유도체 화합물 및 이를 포함하는 약제학적 조성물 |
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- 2002-12-20 HU HU0500173A patent/HUP0500173A3/hu not_active Application Discontinuation
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