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 (enExample) | 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 (enExample) |
| EP (1) | EP1465861B1 (enExample) |
| JP (2) | JP4287746B2 (enExample) |
| KR (1) | KR100966705B1 (enExample) |
| CN (1) | CN1289469C (enExample) |
| AT (1) | ATE430727T1 (enExample) |
| AU (1) | AU2002357333B2 (enExample) |
| BR (1) | BR0215182A (enExample) |
| CA (1) | CA2471099C (enExample) |
| CO (1) | CO5590894A2 (enExample) |
| CY (1) | CY1109275T1 (enExample) |
| DE (1) | DE60232276D1 (enExample) |
| DK (1) | DK1465861T3 (enExample) |
| ES (1) | ES2325205T3 (enExample) |
| GE (1) | GEP20063920B (enExample) |
| HR (1) | HRP20040566A2 (enExample) |
| HU (1) | HUP0500173A3 (enExample) |
| IL (2) | IL162498A0 (enExample) |
| IS (1) | IS2879B (enExample) |
| MX (1) | MXPA04005927A (enExample) |
| NO (1) | NO328976B1 (enExample) |
| NZ (1) | NZ533603A (enExample) |
| PL (1) | PL204281B1 (enExample) |
| PT (1) | PT1465861E (enExample) |
| RS (1) | RS51155B (enExample) |
| RU (1) | RU2300518C2 (enExample) |
| SI (1) | SI1465861T1 (enExample) |
| UA (1) | UA78537C2 (enExample) |
| WO (1) | WO2003053912A1 (enExample) |
| ZA (1) | ZA200404811B (enExample) |
Families Citing this family (56)
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| KR100966705B1 (ko) | 2001-12-20 | 2010-06-29 | 브리스톨-마이어스 스큅 컴퍼니 | β-아밀로이드 저해제로서의α-(Ν-술폰아미도)아세트아미드 유도체 |
| AU2002367147A1 (en) | 2001-12-27 | 2003-07-15 | Daiichi Pharmaceutical Co., Ltd. | Beta-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS |
| JP2006505590A (ja) | 2002-10-23 | 2006-02-16 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ヒスタミンｈ３受容体調節物質としてのフェニルピペリジンおよびフェニルピロリジン |
| EP1616862A4 (en) * | 2003-04-18 | 2008-07-16 | Ono Pharmaceutical Co | HETEROCYCLIC NITROGEN COMPOUND 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 |
| EP2360142A1 (en) * | 2004-03-11 | 2011-08-24 | 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 |
| US7667041B2 (en) * | 2004-05-26 | 2010-02-23 | Eisai R&D Management Co., Ltd. | Cinnamide compound |
| US7144894B2 (en) * | 2004-09-23 | 2006-12-05 | Bristol-Myers Squibb Company | Sulfonamide bicyclic compounds |
| ATE458729T1 (de) * | 2004-10-26 | 2010-03-15 | Eisai R&D Man Co Ltd | Amorphe form einer zimtsäureamidverbindung |
| GB0428526D0 (en) | 2004-12-30 | 2005-02-09 | Novartis Ag | Organic compounds |
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| US8093276B2 (en) * | 2007-10-31 | 2012-01-10 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
| AU2009210070A1 (en) * | 2008-01-28 | 2009-08-06 | Eisai R & D Management Co., Ltd. | Crystalline cinnamide compounds or salts thereof |
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| KR20110133046A (ko) * | 2009-03-19 | 2011-12-09 | 브리스톨-마이어스 스큅 컴퍼니 | 베타 아밀로이드 펩티드 생성의 억제제로서의 신규 알파-(ｎ-술폰아미도)아세트아미드 화합물 |
| US8044077B2 (en) | 2009-03-19 | 2011-10-25 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compounds incorporating deuterium as inhibitors of beta amyloid peptide production |
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| US7977362B2 (en) | 2009-03-20 | 2011-07-12 | Bristol-Myers Squibb Company | Alpha-(N-benzenesulfonamido)cycloalkyl derivatives |
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| CN103502466A (zh) | 2010-09-07 | 2014-01-08 | 斯隆－凯特林纪念癌症中心 | 用于γ-分泌酶测定的方法和组合物 |
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| WO2012165262A1 (ja) * | 2011-05-27 | 2012-12-06 | 国立大学法人徳島大学 | ベンジルアミン誘導体 |
| 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 |
| US9216988B2 (en) * | 2011-12-22 | 2015-12-22 | Genentech, Inc. | Benzyl sulfonamide derivatives as RORc modulators |
| EP2970889A4 (en) | 2013-03-14 | 2016-10-19 | Univ Georgia State Res Found | PREVENTING OR DELAYING FROSTICIDE REACTIONS IN PLANTS |
| CN107980040B (zh) | 2015-07-27 | 2021-11-26 | 株式会社钟根堂 | 作为组蛋白去乙酰酶6抑制剂的1,3,4-噁二唑磺酰胺衍生物及含其的医药组合物 |
| MY197262A (en) | 2015-07-27 | 2023-06-08 | Chong Kun Dang Pharmaceutical Corp | 1,3,4-oxadiazole sulfonamide derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same |
| US10584117B2 (en) | 2015-07-27 | 2020-03-10 | Chong Kun Dang Pharmaceutical Corp. | 1,3,4-oxadiazole amide derivative compound as histone deacetylase 6 inhibitor, and pharmaceutical composition containing same |
| HRP20220003T1 (hr) | 2015-08-04 | 2022-04-01 | Chong Kun Dang Pharmaceutical Corp. | Spojevi derivata 1,3,4-oksadiazola kao inhibitori histonske deacetilaze 6, i farmaceutski pripravak koji ih sadrži |
| HUE061967T2 (hu) | 2015-10-12 | 2023-09-28 | Chong Kun Dang Pharmaceutical Corp | Hiszton deacetiláz-6 inhibitor oxadiazol-amin származékok és az azokat tartalmazó gyógyászati készítmény |
| US10338754B2 (en) * | 2015-12-18 | 2019-07-02 | Synaptics Incorporated | Edge-effect mitigation for capacitive sensors |
| 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 |
| CA3136223C (en) | 2019-05-31 | 2023-09-12 | Chong Kun Dang Pharmaceutical Corp. | 1,3,4-oxadiazole homophthalimide derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same |
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