JP2011502153A5 - - Google Patents
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- Publication number
- JP2011502153A5 JP2011502153A5 JP2010532118A JP2010532118A JP2011502153A5 JP 2011502153 A5 JP2011502153 A5 JP 2011502153A5 JP 2010532118 A JP2010532118 A JP 2010532118A JP 2010532118 A JP2010532118 A JP 2010532118A JP 2011502153 A5 JP2011502153 A5 JP 2011502153A5
- Authority
- JP
- Japan
- Prior art keywords
- compounds
- control
- alzheimer
- fluoro
- disease
- 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
- 150000001875 compounds Chemical class 0.000 claims 16
- 239000003795 chemical substances by application Substances 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- 208000024827 Alzheimer disease Diseases 0.000 claims 5
- 125000001766 1,2,4-oxadiazol-3-yl group Chemical group [H]C1=NC(*)=NO1 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 4
- 230000007306 turnover Effects 0.000 claims 4
- 102000029749 Microtubule Human genes 0.000 claims 3
- 108091022875 Microtubule Proteins 0.000 claims 3
- 239000003999 initiator Substances 0.000 claims 3
- 210000004688 microtubule Anatomy 0.000 claims 3
- OZAIFHULBGXAKX-UHFFFAOYSA-N 2-(2-cyanopropan-2-yldiazenyl)-2-methylpropanenitrile Chemical group N#CC(C)(C)N=NC(C)(C)C#N OZAIFHULBGXAKX-UHFFFAOYSA-N 0.000 claims 2
- FYLZPFSWVMMCQC-UHFFFAOYSA-N 5,5,5-trifluoropentanamide Chemical group NC(=O)CCCC(F)(F)F FYLZPFSWVMMCQC-UHFFFAOYSA-N 0.000 claims 2
- OZAIFHULBGXAKX-VAWYXSNFSA-N AIBN Substances N#CC(C)(C)\N=N\C(C)(C)C#N OZAIFHULBGXAKX-VAWYXSNFSA-N 0.000 claims 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 2
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical group CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 2
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 claims 2
- PCLIMKBDDGJMGD-UHFFFAOYSA-N N-bromosuccinimide Chemical group BrN1C(=O)CCC1=O PCLIMKBDDGJMGD-UHFFFAOYSA-N 0.000 claims 2
- 108010016731 PPAR gamma Proteins 0.000 claims 2
- 102100038825 Peroxisome proliferator-activated receptor gamma Human genes 0.000 claims 2
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 230000006933 amyloid-beta aggregation Effects 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 2
- 238000009169 immunotherapy Methods 0.000 claims 2
- 230000004898 mitochondrial function Effects 0.000 claims 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 2
- 238000006384 oligomerization reaction Methods 0.000 claims 2
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 2
- 230000026731 phosphorylation Effects 0.000 claims 2
- 238000006366 phosphorylation reaction Methods 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000001629 suppression Effects 0.000 claims 2
- KUQQONVKIURIQU-UHFFFAOYSA-N 3-fluoro-4-methylbenzonitrile Chemical compound CC1=CC=C(C#N)C=C1F KUQQONVKIURIQU-UHFFFAOYSA-N 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- LXCYSACZTOKNNS-UHFFFAOYSA-N diethoxy(oxo)phosphanium Chemical compound CCO[P+](=O)OCC LXCYSACZTOKNNS-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000027061 mild cognitive impairment Diseases 0.000 claims 1
- 230000006641 stabilisation Effects 0.000 claims 1
- 238000011105 stabilization Methods 0.000 claims 1
- FXSRCLGHCVIZPP-QGZVFWFLSA-N NC([C@@H](CCC(F)(F)F)N(Cc(ccc(C#N)c1)c1F)S(c(cc1)ccc1Cl)(=O)=O)=O Chemical compound NC([C@@H](CCC(F)(F)F)N(Cc(ccc(C#N)c1)c1F)S(c(cc1)ccc1Cl)(=O)=O)=O FXSRCLGHCVIZPP-QGZVFWFLSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98411807P | 2007-10-31 | 2007-10-31 | |
| US60/984,118 | 2007-10-31 | ||
| PCT/US2008/079798 WO2009058552A1 (en) | 2007-10-31 | 2008-10-14 | A novel alpha-(n-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011502153A JP2011502153A (ja) | 2011-01-20 |
| JP2011502153A5 true JP2011502153A5 (https=) | 2011-11-24 |
| JP5460605B2 JP5460605B2 (ja) | 2014-04-02 |
Family
ID=40193955
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010532118A Expired - Fee Related JP5460605B2 (ja) | 2007-10-31 | 2008-10-14 | βアミロイドペプチド産生の阻害剤としての新規α−（Ｎ−スルホンアミド）アセトアミド化合物 |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US8084477B2 (https=) |
| EP (3) | EP2205575B1 (https=) |
| JP (1) | JP5460605B2 (https=) |
| KR (1) | KR20100075575A (https=) |
| CN (2) | CN101910141B (https=) |
| AR (1) | AR069135A1 (https=) |
| AT (1) | ATE502022T1 (https=) |
| AU (1) | AU2008319122A1 (https=) |
| BR (1) | BRPI0818837A2 (https=) |
| CA (1) | CA2704360A1 (https=) |
| CL (1) | CL2008003271A1 (https=) |
| CO (1) | CO6270332A2 (https=) |
| CY (2) | CY1112337T1 (https=) |
| DE (1) | DE602008005636D1 (https=) |
| DK (2) | DK2205575T3 (https=) |
| EA (2) | EA201171439A1 (https=) |
| ES (2) | ES2390042T3 (https=) |
| HR (2) | HRP20110219T1 (https=) |
| IL (1) | IL205406A0 (https=) |
| MX (1) | MX2010004319A (https=) |
| NZ (1) | NZ584545A (https=) |
| PE (1) | PE20091394A1 (https=) |
| PL (2) | PL2205575T3 (https=) |
| PT (2) | PT2295417E (https=) |
| SG (2) | SG174044A1 (https=) |
| SI (2) | SI2295417T1 (https=) |
| TW (1) | TW200927099A (https=) |
| WO (1) | WO2009058552A1 (https=) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| JP2012520875A (ja) * | 2009-03-19 | 2012-09-10 | ブリストル−マイヤーズ スクイブ カンパニー | ベータアミロイドペプチド産生阻害剤としての新規アルファ−（ｎ−スルホンアミド）アセトアミド化合物 |
| US7977362B2 (en) | 2009-03-20 | 2011-07-12 | Bristol-Myers Squibb Company | Alpha-(N-benzenesulfonamido)cycloalkyl derivatives |
| US8252821B2 (en) * | 2009-04-14 | 2012-08-28 | Bristol-Myers Squibb Company | Bioavailable capsule compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
| TW201043269A (en) * | 2009-04-14 | 2010-12-16 | Bristol Myers Squibb Co | Bioavailable compositions of amorphous alpha-(N-sulfonamido)acetamide compound |
| BR122017023123B1 (pt) | 2010-03-12 | 2018-04-24 | Nippon Soda Co., Ltd. | Método para produzir derivado de picolina halogenada |
| WO2012040444A2 (en) * | 2010-09-24 | 2012-03-29 | Bristol-Myers Squibb Company | Treatment of patients with incipient alzheimer's disease |
| EP2643299B1 (en) | 2010-11-22 | 2016-06-22 | Noscira, S.A. | Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions |
| WO2014047370A1 (en) | 2012-09-21 | 2014-03-27 | Bristol-Myers Squibb Company | Fluoroalkyl dibenzodiazepinone compounds |
| WO2014047369A1 (en) | 2012-09-21 | 2014-03-27 | Bristol-Myers Squibb Company | Substituted 1,5-benzodiazepinone compounds |
| EP2897960B1 (en) | 2012-09-21 | 2016-08-03 | Bristol-Myers Squibb Company | Tricyclic heterocyclic compounds as notch inhibitors |
| EP2897954B1 (en) | 2012-09-21 | 2016-10-26 | Bristol-Myers Squibb Company | Fluoroalkyl-1,4-benzodiazepinone compounds |
| CN103058913B (zh) * | 2012-12-13 | 2015-09-30 | 江苏弘和药物研发有限公司 | 5-氯异吲哚酮的合成方法 |
| CN104163784B (zh) * | 2014-06-20 | 2019-01-08 | 湖南天地恒一制药有限公司 | 一种奥拉西坦的合成工艺 |
| MX390370B (es) | 2016-12-16 | 2025-03-20 | Pipeline Therapeutics Inc | Metodos para tratar la sinaptopatia coclear |
| WO2018201056A1 (en) | 2017-04-28 | 2018-11-01 | Novartis Ag | Cells expressing a bcma-targeting chimeric antigen receptor, and combination therapy with a gamma secretase inhibitor |
| EP3615068A1 (en) | 2017-04-28 | 2020-03-04 | Novartis AG | Bcma-targeting agent, and combination therapy with a gamma secretase inhibitor |
| CN107935957B (zh) * | 2017-12-02 | 2020-08-21 | 江苏仁明生物科技有限公司 | 一种合成高纯度沙坦侧链ttbb的方法 |
| UY38251A (es) | 2018-06-01 | 2019-12-31 | Novartis Ag | Moléculas de unión contra bcma y usos de las mismas |
| CN108640886A (zh) * | 2018-08-01 | 2018-10-12 | 余锋 | 一种作为β-淀粉样肽产生的抑制剂BMS-708163的合成方法 |
| KR20220024729A (ko) | 2019-06-24 | 2022-03-03 | 노파르티스 아게 | B-세포 성숙 항원을 표적으로 하는 다중특이성 항체에 대한 투여 요법 및 병용 요법 |
| CN113466367B (zh) * | 2021-06-25 | 2023-04-14 | 深圳万乐药业有限公司 | 乌苯美司原料药中α-苯乙胺杂质检测方法 |
| CN113816874B (zh) * | 2021-10-30 | 2024-01-26 | 大连双硼医药化工有限公司 | 一种合成4-氰基-2-氟苄醇的工艺方法 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5274094A (en) | 1990-08-15 | 1993-12-28 | British Bio-Technology Limited | Production of heterobicyclic containing benzene sulfonamides |
| GB9202791D0 (en) | 1992-02-11 | 1992-03-25 | British Bio Technology | Compounds |
| US5849736A (en) * | 1993-11-24 | 1998-12-15 | The Dupont Merck Pharmaceutical Company | Isoxazoline and isoxazole fibrinogen receptor antagonists |
| IL123901A (en) | 1995-11-17 | 2003-06-24 | Warner Lambert Co | Sulfonamide inhibitors of matrix metalloproteinases and pharmaceutical compositions comprising them |
| EP0939629A4 (en) | 1996-07-22 | 2002-07-17 | Monsanto Co | THIOL SULFONAMIDE METALLOPROTEASE INHIBITORS |
| JPH11343279A (ja) | 1998-03-16 | 1999-12-14 | Shionogi & Co Ltd | スルホンアミド誘導体およびそれらを含有するＴＮＦ―α産生抑制剤 |
| IL144347A0 (en) | 1999-01-27 | 2002-05-23 | American Cyanamid Co | Acetylenic sulfonamide thiol tace inhibitors |
| US6313123B1 (en) | 1999-01-27 | 2001-11-06 | American Cyanamid Company | Acetylenic sulfonamide thiol tace inhibitors |
| WO2000050391A1 (en) * | 1999-02-26 | 2000-08-31 | Merck & Co., Inc. | Novel sulfonamide compounds and uses thereof |
| US6541467B1 (en) * | 2000-04-14 | 2003-04-01 | Corvas International, Inc. | Thrombin inhibitors having a lactam at P3 |
| US20020115640A1 (en) * | 2000-11-30 | 2002-08-22 | Claiborne Akiyo K. | Farnesyltransferase inhibitors |
| IL159140A0 (en) * | 2001-12-14 | 2004-06-01 | Raytheon Co | Precisely aligned lens structure and a method for its fabrication |
| 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 |
| IL163643A0 (en) * | 2002-02-28 | 2005-12-18 | Astrazeneca Ab | Oxazolidinone derivatives, processes for their forpreparation, and pharmaceutical compositions containing them |
| EP1460070B1 (en) * | 2003-03-20 | 2007-05-16 | Santhera Pharmaceuticals (Schweiz) AG | Substituted piperidine and piperazine derivatives as melanocortin-4 receptor modulators |
| BRPI0408962A (pt) | 2003-03-31 | 2006-04-04 | Wyeth Corp | inibidores sulfonamidas heterocìclicos contendo flúor- e trifluoroalquila da produção de beta amilóide e seus derivados |
| US7144894B2 (en) | 2004-09-23 | 2006-12-05 | Bristol-Myers Squibb Company | Sulfonamide bicyclic compounds |
| PE20080169A1 (es) | 2006-02-17 | 2008-04-11 | Wyeth Corp | Metodo para preparar alcoholes sustituidos con sulfonamidas y sus compuestos intermedios |
| US7838550B2 (en) | 2006-02-17 | 2010-11-23 | Wyeth Llc | Selective N-sulfonylation of 2-amino fluoro- and trifluoroalkyl substituted alcohols |
| WO2008112249A1 (en) | 2007-03-13 | 2008-09-18 | Trustees Of Columbia University In The City Of New York | Synergistic interaction of notch-1 inhibitors with glucocorticoids |
| WO2009005688A2 (en) | 2007-06-29 | 2009-01-08 | Trustees Of Columbia University In The City Of New York | Activating mutations in notch-1 |
| 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 |
| 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 |
-
2008
- 2008-10-10 US US12/249,180 patent/US8084477B2/en active Active
- 2008-10-14 EA EA201171439A patent/EA201171439A1/ru unknown
- 2008-10-14 AU AU2008319122A patent/AU2008319122A1/en not_active Abandoned
- 2008-10-14 WO PCT/US2008/079798 patent/WO2009058552A1/en not_active Ceased
- 2008-10-14 JP JP2010532118A patent/JP5460605B2/ja not_active Expired - Fee Related
- 2008-10-14 EA EA201000714A patent/EA016447B1/ru not_active IP Right Cessation
- 2008-10-14 EP EP08843687A patent/EP2205575B1/en not_active Not-in-force
- 2008-10-14 KR KR1020107009453A patent/KR20100075575A/ko not_active Withdrawn
- 2008-10-14 AT AT08843687T patent/ATE502022T1/de active
- 2008-10-14 EP EP10190591A patent/EP2295417B1/en not_active Not-in-force
- 2008-10-14 HR HR20110219T patent/HRP20110219T1/hr unknown
- 2008-10-14 NZ NZ584545A patent/NZ584545A/en not_active IP Right Cessation
- 2008-10-14 BR BRPI0818837 patent/BRPI0818837A2/pt not_active IP Right Cessation
- 2008-10-14 EP EP12159802A patent/EP2471769A1/en not_active Withdrawn
- 2008-10-14 PT PT10190591T patent/PT2295417E/pt unknown
- 2008-10-14 DK DK08843687.8T patent/DK2205575T3/da active
- 2008-10-14 PL PL08843687T patent/PL2205575T3/pl unknown
- 2008-10-14 PL PL10190591T patent/PL2295417T3/pl unknown
- 2008-10-14 ES ES10190591T patent/ES2390042T3/es active Active
- 2008-10-14 DK DK10190591.7T patent/DK2295417T3/da active
- 2008-10-14 CA CA2704360A patent/CA2704360A1/en not_active Abandoned
- 2008-10-14 SI SI200830775T patent/SI2295417T1/sl unknown
- 2008-10-14 SG SG2011056454A patent/SG174044A1/en unknown
- 2008-10-14 SI SI200830183T patent/SI2205575T1/sl unknown
- 2008-10-14 CN CN2008801240109A patent/CN101910141B/zh not_active Expired - Fee Related
- 2008-10-14 SG SG2011056447A patent/SG174043A1/en unknown
- 2008-10-14 MX MX2010004319A patent/MX2010004319A/es active IP Right Grant
- 2008-10-14 CN CN201210178082XA patent/CN102718689A/zh active Pending
- 2008-10-14 ES ES08843687T patent/ES2361283T3/es active Active
- 2008-10-14 PT PT08843687T patent/PT2205575E/pt unknown
- 2008-10-14 DE DE602008005636T patent/DE602008005636D1/de active Active
- 2008-10-30 CL CL2008003271A patent/CL2008003271A1/es unknown
- 2008-10-30 AR ARP080104770A patent/AR069135A1/es unknown
- 2008-10-31 TW TW097142279A patent/TW200927099A/zh unknown
- 2008-10-31 PE PE2008001866A patent/PE20091394A1/es not_active Application Discontinuation
-
2010
- 2010-04-27 CO CO10049723A patent/CO6270332A2/es not_active Application Discontinuation
- 2010-04-28 IL IL205406A patent/IL205406A0/en unknown
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2011
- 2011-06-15 CY CY20111100570T patent/CY1112337T1/el unknown
- 2011-11-18 US US13/299,703 patent/US8350084B2/en active Active
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2012
- 2012-09-04 HR HRP20120703AT patent/HRP20120703T1/hr unknown
- 2012-09-28 CY CY20121100889T patent/CY1113346T1/el unknown