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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2471099C (en) | 2001-12-20 | 2011-04-12 | Bristol-Myers Squibb Company | .alpha.-(n-sulphonamido)acetamide derivatives as .beta.-amyloid inhibitors |
| KR100927304B1 (ko) | 2001-12-27 | 2009-11-18 | 다이이찌 세이야꾸 가부시기가이샤 | β-아밀로이드 단백 생산·분비 저해제 |
| EP1556046A1 (en) | 2002-10-23 | 2005-07-27 | Janssen Pharmaceutica N.V. | Phenylpiperidines and phenylpyrrolidines as histamine h3 receptor modulators |
| US20070043079A1 (en) * | 2003-04-18 | 2007-02-22 | Hiromu Habashita | Heterocyclic compound containing nitrogen atom and use thereof |
| PL379466A1 (pl) | 2003-06-30 | 2006-09-18 | Daiichi Sankyo Company , Limited | Heterocykliczne pochodne metylosulfonu |
| 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 |
| RU2361872C2 (ru) * | 2004-05-26 | 2009-07-20 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Циннамидное соединение |
| US7144894B2 (en) * | 2004-09-23 | 2006-12-05 | Bristol-Myers Squibb Company | Sulfonamide bicyclic compounds |
| DE602005019602D1 (de) | 2004-10-26 | 2010-04-08 | Eisai R&D Man Co Ltd | Amorphe form einer zimtsäureamidverbindung |
| GB0428526D0 (en) | 2004-12-30 | 2005-02-09 | Novartis Ag | Organic compounds |
| US20090048448A1 (en) * | 2005-11-18 | 2009-02-19 | Ikuo Kushida | Salts of cynnamide compound or solvates thereof |
| CN101309916A (zh) * | 2005-11-18 | 2008-11-19 | 卫材R&D管理有限公司 | 制备肉桂酰胺衍生物的方法 |
| TWI370130B (en) * | 2005-11-24 | 2012-08-11 | Eisai R&D Man Co Ltd | Two cyclic cinnamide compound |
| KR20080069221A (ko) | 2005-11-24 | 2008-07-25 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 모르폴린 타입의 신나미드 화합물 |
| US7579504B2 (en) | 2005-12-07 | 2009-08-25 | Gilead Sciences, Inc. | ABCA1 elevating compounds |
| NZ570825A (en) | 2006-01-30 | 2012-05-25 | Univ Georgia State Res Found | Induction and stabilization of enzymatic activity in microorganisms |
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| KR20090016591A (ko) * | 2006-05-19 | 2009-02-16 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 헤테로사이클 타입의 신나미드 유도체 |
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| RU2448108C2 (ru) * | 2006-07-27 | 2012-04-20 | Эморпасифик Корпорейшн | Новые соединения, их изомер или их фармацевтически приемлемые соли в качестве антагониста ванилоидного рецептора и содержащая их фармацевтическая композиция |
| US7737141B2 (en) * | 2006-07-28 | 2010-06-15 | Eisai R&D Management Co., Ltd. | Prodrug of cinnamide compound |
| CL2008000582A1 (es) * | 2007-02-28 | 2008-06-27 | Eisai R&D Man Co Ltd | Compuestos ciclicos derivados de oximorfolina condensados; farmacos que comprenden a dichos compuestos; y su uso para tratar enfermedad de alzheimer, demencia senil, sindrome de down o amiloidosis. |
| US7943549B2 (en) | 2007-04-02 | 2011-05-17 | Georgia State University Research Foundation, Inc. | Biological-based catalyst to delay plant development processes |
| EP1985612A1 (en) * | 2007-04-26 | 2008-10-29 | Bayer Schering Pharma Aktiengesellschaft | Arymethylen substituted N-Acyl-gamma-aminoalcohols |
| US20080306272A1 (en) * | 2007-05-16 | 2008-12-11 | Eisai R&D Management Co., Ltd. | One-pot methods for preparing cinnamide derivatives |
| BRPI0815773A2 (pt) | 2007-08-31 | 2019-09-24 | Eisai R&D Man Co Ltd | composto, e, medicamento. |
| US7935815B2 (en) | 2007-08-31 | 2011-05-03 | Eisai R&D Management Co., Ltd. | Imidazoyl pyridine compounds and salts thereof |
| AU2008311367B2 (en) * | 2007-10-05 | 2014-11-13 | Ac Immune S.A. | Use of anti-amyloid beta antibody in ocular diseases |
| US8084477B2 (en) * | 2007-10-31 | 2011-12-27 | Bristol-Myers Squibb Company | Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
| 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 |
| WO2009096349A1 (ja) * | 2008-01-28 | 2009-08-06 | Eisai R & D Management Co., Ltd. | 結晶性のシンナミド化合物またはその塩 |
| WO2009137657A1 (en) * | 2008-05-08 | 2009-11-12 | Bristol-Myers Squibb Company | 2-aryl glycinamide derivatives |
| 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 |
| CN102438622A (zh) * | 2009-03-19 | 2012-05-02 | 百时美施贵宝公司 | 作为β淀粉样肽产生抑制剂的新颖α-(N-磺酰氨基)乙酰胺化合物 |
| US20110071199A1 (en) * | 2009-03-20 | 2011-03-24 | Bristol-Myers Squibb Company | Thiophenyl Sulfonamides for the Treatment of Alzheimer's Disease |
| US7977362B2 (en) | 2009-03-20 | 2011-07-12 | Bristol-Myers Squibb Company | Alpha-(N-benzenesulfonamido)cycloalkyl derivatives |
| TW201043269A (en) * | 2009-04-14 | 2010-12-16 | Bristol Myers Squibb Co | Bioavailable compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
| US8252821B2 (en) | 2009-04-14 | 2012-08-28 | Bristol-Myers Squibb Company | Bioavailable capsule compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
| US9023767B2 (en) * | 2009-05-07 | 2015-05-05 | Memorial Sloan-Kettering Cancer Center | γ-Secretase substrates and methods of use |
| 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 |
| WO2012040444A2 (en) * | 2010-09-24 | 2012-03-29 | Bristol-Myers Squibb Company | Treatment of patients with incipient alzheimer's disease |
| CN103619805A (zh) * | 2011-05-27 | 2014-03-05 | 国立大学法人德岛大学 | 苄胺衍生物 |
| 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 |
| MX360847B (es) | 2013-03-14 | 2018-11-20 | Univ Georgia State Res Found | Prevencion o retardo de respuesta al daño por enfriamiento en plantas. |
| PL3328843T3 (pl) | 2015-07-27 | 2023-02-27 | Chong Kun Dang Pharmaceutical Corp. | Związki będące pochodnymi 1,3,4 oksadiazolosulfonamidów jako inhibitor deacetylazy histonowej 6, oraz kompozycja farmaceutyczna je zawierająca |
| CN108026056B (zh) | 2015-07-27 | 2021-08-03 | 株式会社钟根堂 | 作为组蛋白脱乙酰酶6抑制剂的1,3,4-噁二唑酰胺衍生物化合物及其药物组合物 |
| RU2695227C9 (ru) | 2015-07-27 | 2020-03-04 | Чонг Кун Данг Фармасьютикал Корп. | Производные 1,3,4-оксадиазолсульфамида в качестве ингибитора гистондеацетилазы 6 и содержащая их фармацевтическая композиция |
| JP6491393B2 (ja) | 2015-08-04 | 2019-03-27 | チョン クン ダン ファーマシューティカル コーポレーション | ヒストン脱アセチル化酵素６阻害剤としての１，３，４−オキサジアゾール誘導体化合物及びこれを含有する薬剤学的組成物 |
| JP6697074B2 (ja) | 2015-10-12 | 2020-05-20 | チョン クン ダン ファーマシューティカル コーポレーション | ヒストン脱アセチル化酵素６阻害剤としてのオキサジアゾールアミン誘導体化合物及びこれを含有する薬剤学的組成物 |
| 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 |
| MY207444A (en) | 2019-05-31 | 2025-02-27 | Chong Kun Dang Pharmaceutical Corp | 1,3,4-oxadiazole homophthalimide derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same |
| CN111995565B (zh) * | 2020-07-24 | 2022-01-25 | 浙江工业大学 | 一种(s)-2-哌啶甲酸的制备方法 |
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2002
- 2002-12-20 CA CA2471099A patent/CA2471099C/en not_active Expired - Fee Related
- 2002-12-20 US US10/326,365 patent/US7300936B2/en not_active Expired - Lifetime
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- 2002-12-20 AT AT02805633T patent/ATE430727T1/de active
- 2002-12-20 SI SI200230838T patent/SI1465861T1/sl unknown
- 2002-12-20 AU AU2002357333A patent/AU2002357333B2/en not_active Ceased
- 2002-12-20 BR BR0215182-0A patent/BR0215182A/pt not_active Application Discontinuation
- 2002-12-20 GE GE5663A patent/GEP20063920B/en unknown
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- 2002-12-20 NZ NZ533603A patent/NZ533603A/en not_active IP Right Cessation
- 2002-12-20 WO PCT/US2002/040605 patent/WO2003053912A1/en not_active Ceased
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- 2002-12-20 RU RU2004122481/04A patent/RU2300518C2/ru not_active IP Right Cessation
- 2002-12-20 UA UA20040705944A patent/UA78537C2/uk unknown
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