JP2008526999A5 - - Google Patents
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- Publication number
- JP2008526999A5 JP2008526999A5 JP2007551435A JP2007551435A JP2008526999A5 JP 2008526999 A5 JP2008526999 A5 JP 2008526999A5 JP 2007551435 A JP2007551435 A JP 2007551435A JP 2007551435 A JP2007551435 A JP 2007551435A JP 2008526999 A5 JP2008526999 A5 JP 2008526999A5
- Authority
- JP
- Japan
- Prior art keywords
- alkylene
- alkyl
- group
- aryl
- carbon atoms
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 30
- 125000003118 aryl group Chemical group 0.000 claims 25
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000002947 alkylene group Chemical group 0.000 claims 18
- 125000004432 carbon atom Chemical group C* 0.000 claims 11
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 7
- 125000004430 oxygen atom Chemical group O* 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 125000004434 sulfur atom Chemical group 0.000 claims 7
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 0 CC(Cc1ccccc1)(c1nnc(*)[o]1)N Chemical compound CC(Cc1ccccc1)(c1nnc(*)[o]1)N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64492405P | 2005-01-19 | 2005-01-19 | |
| US65242105P | 2005-02-11 | 2005-02-11 | |
| PCT/US2006/001367 WO2006078577A1 (en) | 2005-01-19 | 2006-01-13 | Tertiary carbinamines having substituted heterocycles, which are active as inhibitors of beta-secretase, for the treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008526999A JP2008526999A (ja) | 2008-07-24 |
| JP2008526999A5 true JP2008526999A5 (enExample) | 2009-02-19 |
Family
ID=36692561
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007551435A Pending JP2008526999A (ja) | 2005-01-19 | 2006-01-13 | アルツハイマー病治療用ベータ−セクレターゼインヒビターとして活性な置換へテロ環含有三級カルビナミン |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8338614B2 (enExample) |
| EP (1) | EP1841426B1 (enExample) |
| JP (1) | JP2008526999A (enExample) |
| AT (1) | ATE506951T1 (enExample) |
| AU (1) | AU2006206654A1 (enExample) |
| CA (1) | CA2594946A1 (enExample) |
| DE (1) | DE602006021535D1 (enExample) |
| WO (1) | WO2006078577A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7763609B2 (en) | 2003-12-15 | 2010-07-27 | Schering Corporation | Heterocyclic aspartyl protease inhibitors |
| US8426429B2 (en) | 2004-08-06 | 2013-04-23 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US8436006B2 (en) | 2004-08-06 | 2013-05-07 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| US8383637B2 (en) | 2004-08-06 | 2013-02-26 | Jansssen Pharmaceutica N.V. | 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE) |
| CN101106994A (zh) * | 2005-01-19 | 2008-01-16 | 默克公司 | 用于治疗阿尔茨海默氏病的氨基甲基β-分泌酶抑制剂 |
| DE602006021535D1 (de) | 2005-01-19 | 2011-06-09 | Merck Sharp & Dohme | Als inhibitoren von beta-secretase aktive tertiäre carbinamine mit substituierten heterocyclen zur behandlung der alzheimer-krankheit |
| US7932261B2 (en) | 2006-02-06 | 2011-04-26 | Janssen Pharmaceutica Nv | Macrocycle derivatives useful as inhibitors of β-secretase (BACE) |
| US7776882B2 (en) * | 2006-02-06 | 2010-08-17 | Baxter Ellen W | 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE) |
| WO2007092854A2 (en) | 2006-02-06 | 2007-08-16 | Janssen Pharmaceutica N.V. | 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE) |
| EP2178375B1 (en) * | 2007-07-20 | 2014-09-24 | Merck Sharp & Dohme Corp. | Pyrazoloý1,5-a¨pyrimidine derivatives |
| US20090264315A1 (en) | 2007-07-26 | 2009-10-22 | Texas A&M University System | Dipeptide mimics, libraries combining two dipeptide mimics with a third group, and methods for production thereof |
| CA2696609C (en) | 2007-08-27 | 2017-09-05 | Helicon Therapeutics, Inc. | Therapeutic isoxazole compounds |
| BRPI0906962B8 (pt) * | 2008-01-18 | 2021-05-25 | Eisai R&D Man Co Ltd | composto de aminodiidrotiazina fundido |
| CA2713998A1 (en) | 2008-01-28 | 2009-08-06 | Janssen Pharmaceutica N.V. | 6-substituted-thio-2-amino-quinoline derivatives useful as inhibitors of.beta.-secretase (bace) |
| CN101970429B (zh) | 2008-01-29 | 2013-05-29 | 詹森药业有限公司 | 可用作β-分泌酶(BACE)抑制剂的2-氨基喹啉衍生物 |
| WO2010013794A1 (en) * | 2008-07-28 | 2010-02-04 | Eisai R&D Management Co., Ltd. | Spiroaminodihydrothiazine derivatives |
| RU2503681C2 (ru) * | 2008-09-30 | 2014-01-10 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Новое конденсированное производное аминодигидротиазина |
| WO2010038686A1 (ja) * | 2008-09-30 | 2010-04-08 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 新規な縮合アミノジヒドロチアジン誘導体 |
| GB0912778D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydro-oxazine derivatives |
| GB0912777D0 (en) | 2009-07-22 | 2009-08-26 | Eisai London Res Lab Ltd | Fused aminodihydropyrimidone derivatives |
| UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
| US8754113B2 (en) | 2009-12-15 | 2014-06-17 | Shionogi & Co., Ltd. | Oxadiazole derivative having endothelial lipase inhibitory activity |
| TW201300380A (zh) * | 2010-10-19 | 2013-01-01 | Comentis Inc | 抑制β－分泌酶活性之噁二唑化合物及其使用方法 |
| GB201100181D0 (en) | 2011-01-06 | 2011-02-23 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101140D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| GB201101139D0 (en) | 2011-01-21 | 2011-03-09 | Eisai Ltd | Fused aminodihydrothiazine derivatives |
| SG191710A1 (en) | 2011-01-21 | 2013-08-30 | Eisai R&D Man Co Ltd | Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives |
| EP2908813A4 (en) * | 2012-10-12 | 2016-05-11 | Childrens Medical Center | COMPOUNDS FOR THE TREATMENT OF RAC-GTPASE-MEDIATED ILLNESSES |
| CN103848826A (zh) * | 2012-11-30 | 2014-06-11 | 南京大学 | 一类含苯并三氮唑结构的1,3,4-恶二唑类衍生物的制法与用途 |
| CN103848827A (zh) * | 2012-11-30 | 2014-06-11 | 南京大学 | 一种含苯并三氮唑类衍生物在抗癌药物中的应用 |
| US10538516B2 (en) | 2015-03-25 | 2020-01-21 | National Center For Geriatrics And Gerontology | Oxadiazole derivative and pharmaceutical containing same |
| EP3286184B1 (en) | 2015-04-24 | 2020-03-25 | Children's Medical Center Corporation | Compounds for treating rac-gtpase mediated disorder |
| US10653682B2 (en) * | 2017-10-26 | 2020-05-19 | Southern Research Institute | Oxadiazoles and thiadiazoles as TGF-β inhibitors |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2143246C (en) * | 1994-03-16 | 2000-08-22 | Thierry Godel | Imidazodiazepines |
| TWI292316B (en) * | 1999-10-11 | 2008-01-11 | Sod Conseils Rech Applic | Pharmaceutical composition of thiazole derivatives intended to inhibit mao and/or lipidic peroxidation and/or to act as modulators of sodium channels and the use thereof |
| GB0021831D0 (en) * | 2000-09-06 | 2000-10-18 | Astrazeneca Ab | Chemical compounds |
| DE60113032T2 (de) * | 2000-10-30 | 2006-07-06 | Pfizer Products Inc., Groton | Glukokortikoidrezeptor-Modulatoren |
| US6566311B1 (en) * | 2001-11-30 | 2003-05-20 | Uniroyal Chemical Company, Inc. | 1,3,4-oxadiazole additives for lubricants |
| US6951946B2 (en) * | 2002-03-19 | 2005-10-04 | Lexicon Pharmaceuticals, Inc. | Large scale synthesis of 1,2,4- and 1,3,4-oxadiazole carboxylates |
| CN1656079A (zh) * | 2002-05-31 | 2005-08-17 | 卫材株式会社 | 吡唑化合物和含有该化合物的药物组合物 |
| EP1515944A1 (en) * | 2002-06-17 | 2005-03-23 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
| US7115652B2 (en) * | 2002-06-17 | 2006-10-03 | Sunesis Pharmaceuticals, Inc. | Aspartyl protease inhibitors |
| CA2563615A1 (en) * | 2004-04-20 | 2005-11-03 | Merck & Co., Inc. | 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease |
| EP1740581B1 (en) | 2004-04-20 | 2012-08-22 | Merck Sharp & Dohme Corp. | 2, 4, 6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease |
| JP2008520718A (ja) * | 2004-11-23 | 2008-06-19 | メルク エンド カムパニー インコーポレーテッド | アルツハイマー病の治療のためのβ−セクレターゼ阻害剤として有用な２，３，４，６−置換ピリジル誘導体化合物 |
| CN101106994A (zh) * | 2005-01-19 | 2008-01-16 | 默克公司 | 用于治疗阿尔茨海默氏病的氨基甲基β-分泌酶抑制剂 |
| DE602006021535D1 (de) | 2005-01-19 | 2011-06-09 | Merck Sharp & Dohme | Als inhibitoren von beta-secretase aktive tertiäre carbinamine mit substituierten heterocyclen zur behandlung der alzheimer-krankheit |
-
2006
- 2006-01-13 DE DE602006021535T patent/DE602006021535D1/de not_active Expired - Lifetime
- 2006-01-13 WO PCT/US2006/001367 patent/WO2006078577A1/en not_active Ceased
- 2006-01-13 JP JP2007551435A patent/JP2008526999A/ja active Pending
- 2006-01-13 CA CA002594946A patent/CA2594946A1/en not_active Abandoned
- 2006-01-13 AT AT06718444T patent/ATE506951T1/de not_active IP Right Cessation
- 2006-01-13 US US11/795,190 patent/US8338614B2/en active Active
- 2006-01-13 EP EP06718444A patent/EP1841426B1/en not_active Expired - Lifetime
- 2006-01-13 AU AU2006206654A patent/AU2006206654A1/en not_active Abandoned
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