JP2008505100A5 - - Google Patents
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- Publication number
- JP2008505100A5 JP2008505100A5 JP2007519415A JP2007519415A JP2008505100A5 JP 2008505100 A5 JP2008505100 A5 JP 2008505100A5 JP 2007519415 A JP2007519415 A JP 2007519415A JP 2007519415 A JP2007519415 A JP 2007519415A JP 2008505100 A5 JP2008505100 A5 JP 2008505100A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- alkylene
- substituted
- pharmaceutically acceptable
- 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
- 125000003118 aryl group Chemical group 0.000 claims 61
- 125000000217 alkyl group Chemical group 0.000 claims 56
- 150000001875 compounds Chemical class 0.000 claims 47
- 150000003839 salts Chemical class 0.000 claims 41
- 239000012453 solvate Substances 0.000 claims 41
- 125000001424 substituent group Chemical group 0.000 claims 39
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 16
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 125000002947 alkylene group Chemical group 0.000 claims 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 8
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 7
- 125000004350 aryl cycloalkyl group Chemical group 0.000 claims 5
- -1 2 -cyclopropyl Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000002993 cycloalkylene group Chemical group 0.000 claims 3
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 claims 2
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 claims 2
- 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 2
- 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 2
- 125000005605 benzo group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 1
- TVEXGJYMHHTVKP-UHFFFAOYSA-N 6-oxabicyclo[3.2.1]oct-3-en-7-one Chemical compound C1C2C(=O)OC1C=CC2 TVEXGJYMHHTVKP-UHFFFAOYSA-N 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 0 CCC[C@](COC[C@@]12)N1*(c1ccc(*)cc1)=C(C1)C21OC(N(CC1)CCN1C(C)(C)CO)=O Chemical compound CCC[C@](COC[C@@]12)N1*(c1ccc(*)cc1)=C(C1)C21OC(N(CC1)CCN1C(C)(C)CO)=O 0.000 description 10
- DIGDIWHKKJZMKG-YTQUADARSA-N CC(C)[C@H](COC[C@@H]1C2(CC2)OC(N(CC2)C[C@H]2O)=O)N1S(c(cc1)ccc1Cl)(=O)=O Chemical compound CC(C)[C@H](COC[C@@H]1C2(CC2)OC(N(CC2)C[C@H]2O)=O)N1S(c(cc1)ccc1Cl)(=O)=O DIGDIWHKKJZMKG-YTQUADARSA-N 0.000 description 1
- GHHUJPFVTHAWJJ-LEWJYISDSA-N CC(C)[C@H](COC[C@@H]1C2(CC2)OC(N2CCC(CO)CC2)=O)N1S(c(cc1)ccc1Cl)(=O)=O Chemical compound CC(C)[C@H](COC[C@@H]1C2(CC2)OC(N2CCC(CO)CC2)=O)N1S(c(cc1)ccc1Cl)(=O)=O GHHUJPFVTHAWJJ-LEWJYISDSA-N 0.000 description 1
- MVGOFZWJNQXPLL-LGJCEAAXSA-N CCC[C@H](COC[C@@H]12)N1C=C(C1)C21OC(N(CC1)CCC1(CC)OC)=O Chemical compound CCC[C@H](COC[C@@H]12)N1C=C(C1)C21OC(N(CC1)CCC1(CC)OC)=O MVGOFZWJNQXPLL-LGJCEAAXSA-N 0.000 description 1
- ZJTNMXKBOSGJPO-GLTZWUPFSA-N CCC[C@H](COC[C@@H]1C(C2)(/C2=C\C=O)OC(N2CCOCC2)=O)N1Sc(cc1)ccc1Cl Chemical compound CCC[C@H](COC[C@@H]1C(C2)(/C2=C\C=O)OC(N2CCOCC2)=O)N1Sc(cc1)ccc1Cl ZJTNMXKBOSGJPO-GLTZWUPFSA-N 0.000 description 1
- OCEIPUIMZWHBTM-YROPZMMGSA-N CCC[C@H](COC[C@@H]1C2(C=3C2)OC(N2[C@H](CO)CCC2)=O)N1S=3(c(cc1)ccc1Cl)=O Chemical compound CCC[C@H](COC[C@@H]1C2(C=3C2)OC(N2[C@H](CO)CCC2)=O)N1S=3(c(cc1)ccc1Cl)=O OCEIPUIMZWHBTM-YROPZMMGSA-N 0.000 description 1
- QXGBKHUOWLOVRK-RRPNLBNLSA-N CCc1cc(F)cc([C@H](COC[C@@H]2C3(CC3)OC(N(CC3)CCN3C(C)(C)CO)=O)N2S(c(cc2)ccc2Cl)(=O)=O)c1 Chemical compound CCc1cc(F)cc([C@H](COC[C@@H]2C3(CC3)OC(N(CC3)CCN3C(C)(C)CO)=O)N2S(c(cc2)ccc2Cl)(=O)=O)c1 QXGBKHUOWLOVRK-RRPNLBNLSA-N 0.000 description 1
- UANAZMMRKQNCKS-FDZRRXNVSA-N C[C@@H]([C@H]1C2CC2)OC[C@H](C2(CC2)OC[N+](CC2)(C[C@@H]2O)[O-])N1S(c(cc1)ccc1Cl)(=O)=O Chemical compound C[C@@H]([C@H]1C2CC2)OC[C@H](C2(CC2)OC[N+](CC2)(C[C@@H]2O)[O-])N1S(c(cc1)ccc1Cl)(=O)=O UANAZMMRKQNCKS-FDZRRXNVSA-N 0.000 description 1
- NXENLQIGYOVFMG-QGPMSJSTSA-N C[C@H](C(C)(C)OC[C@@H]1C2(CC2)OC(N(CC2)C[C@@H]2O)=O)N1S(c(cc1)ccc1Cl)(=O)=O Chemical compound C[C@H](C(C)(C)OC[C@@H]1C2(CC2)OC(N(CC2)C[C@@H]2O)=O)N1S(c(cc1)ccc1Cl)(=O)=O NXENLQIGYOVFMG-QGPMSJSTSA-N 0.000 description 1
- UBZIWDLPYNPRFW-RHLKJBLCSA-N C[C@H](C(C)(C)OC[C@@H]1C2(CC2)OC2OC2N(CC2)CCC2C(N)=O)N1S(c(cc1)ccc1Cl)(=O)=O Chemical compound C[C@H](C(C)(C)OC[C@@H]1C2(CC2)OC2OC2N(CC2)CCC2C(N)=O)N1S(c(cc1)ccc1Cl)(=O)=O UBZIWDLPYNPRFW-RHLKJBLCSA-N 0.000 description 1
- SWMAUZBTMLMXJB-AOYPEHQESA-N O=C(N(CC1)CCC1N1CCCCC1)OC1(CC1)[C@@H](COC[C@H]1CC2CC2)N1S(c(cc1)ccc1Cl)(=O)=O Chemical compound O=C(N(CC1)CCC1N1CCCCC1)OC1(CC1)[C@@H](COC[C@H]1CC2CC2)N1S(c(cc1)ccc1Cl)(=O)=O SWMAUZBTMLMXJB-AOYPEHQESA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US58401004P | 2004-06-30 | 2004-06-30 | |
| PCT/US2005/023187 WO2006004880A2 (en) | 2004-06-30 | 2005-06-28 | Substituted n-arylsulfonylheterocyclic amines as gamma-secretase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008505100A JP2008505100A (ja) | 2008-02-21 |
| JP2008505100A5 true JP2008505100A5 (enExample) | 2008-08-07 |
Family
ID=35783342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007519415A Pending JP2008505100A (ja) | 2004-06-30 | 2005-06-28 | ガンマ−セクレターゼ阻害剤としての置換ｎ−アリールスルホニル複素環アミン |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US7763613B2 (enExample) |
| EP (1) | EP1789404B1 (enExample) |
| JP (1) | JP2008505100A (enExample) |
| CN (2) | CN101602741A (enExample) |
| AR (1) | AR050994A1 (enExample) |
| AT (1) | ATE461926T1 (enExample) |
| CA (1) | CA2570183A1 (enExample) |
| DE (1) | DE602005020156D1 (enExample) |
| ES (1) | ES2341560T3 (enExample) |
| MX (1) | MX2007000040A (enExample) |
| PE (1) | PE20060481A1 (enExample) |
| TW (1) | TWI297270B (enExample) |
| WO (1) | WO2006004880A2 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR059075A1 (es) | 2006-01-20 | 2008-03-12 | Schering Corp | Bencesulfonil - cromano , tiocromano tetrahidronaftaleno e inhibidores de gamma secretasa relacionados |
| AR059355A1 (es) | 2006-02-07 | 2008-03-26 | Wyeth Corp | Inhibidores de 11-beta hsd1 |
| CA2649996A1 (en) | 2006-04-26 | 2007-11-08 | Merck Sharp & Dohme Limited | Piperidines and related compounds for treatment of alzheimer's disease |
| DK2041181T3 (da) * | 2006-06-08 | 2011-08-29 | Helmholtz Zentrum Muenchen | Specifikke proteaseinhibitorer og deres anvendelse i cancerterapi |
| US8278345B2 (en) | 2006-11-09 | 2012-10-02 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| ATE554085T1 (de) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | Neue inhibitoren von glutaminylcyclase |
| JP5930573B2 (ja) | 2007-03-01 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤の新規使用 |
| WO2008128985A1 (en) | 2007-04-18 | 2008-10-30 | Probiodrug Ag | Thiourea derivatives as glutaminyl cyclase inhibitors |
| ATE543799T1 (de) * | 2007-10-19 | 2012-02-15 | Janssen Pharmaceutica Nv | Piperidinyl- und piperazinylmodulatoren von g- sekretase |
| PL2475428T3 (pl) | 2009-09-11 | 2015-12-31 | Probiodrug Ag | Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej |
| US20110190269A1 (en) * | 2010-02-01 | 2011-08-04 | Karlheinz Baumann | Gamma secretase modulators |
| ES2586231T3 (es) | 2010-03-03 | 2016-10-13 | Probiodrug Ag | Inhibidores de glutaminil ciclasa |
| MX2012010470A (es) | 2010-03-10 | 2012-10-09 | Probiodrug Ag | Inhibidores heterociclicos d ciclasa de glutaminilo (qc, ec .3 2. 5). |
| US8541596B2 (en) | 2010-04-21 | 2013-09-24 | Probiodrug Ag | Inhibitors |
| EP2686313B1 (en) | 2011-03-16 | 2016-02-03 | Probiodrug AG | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| AR091279A1 (es) | 2012-06-08 | 2015-01-21 | Gilead Sciences Inc | Inhibidores macrociclicos de virus flaviviridae |
| PL3461819T3 (pl) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitory cyklazy glutaminylowej |
| CN109705052B (zh) * | 2019-01-25 | 2020-12-08 | 苏州大学 | 一种制备1,4-二氢噁嗪的方法 |
| CN119060034B (zh) * | 2024-09-02 | 2026-03-24 | 上海信诺维生物医药有限公司 | 一种含吡喃取代的吗啉类化合物的制备方法 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH04247081A (ja) | 1991-02-01 | 1992-09-03 | Takeda Chem Ind Ltd | ５員複素環酸アミド類 |
| US5646167A (en) * | 1993-01-06 | 1997-07-08 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamix acids |
| PT885888E (pt) * | 1996-02-02 | 2003-12-31 | Western Therapeutics Inst D | Derivados e farmacos de isoquinolina |
| HUP0102532A3 (en) * | 1998-06-03 | 2002-06-28 | Gpi Nil Holdings Inc Wilmingto | Aza-heterocyclic compounds used to treat neurological disorders and hair loss and process for their preparation and pharmaceutical compositions containing them |
| CN1348442A (zh) | 1999-02-26 | 2002-05-08 | 默克公司 | 新的磺胺化合物及其应用 |
| FR2802206B1 (fr) | 1999-12-14 | 2005-04-22 | Sod Conseils Rech Applic | Derives de 4-aminopiperidine et leur utilisation en tant que medicament |
| SE9904738D0 (sv) * | 1999-12-22 | 1999-12-22 | Astra Pharma Prod | Novel compounds |
| JP2001261657A (ja) * | 2000-03-17 | 2001-09-26 | Yamanouchi Pharmaceut Co Ltd | シアノフェニル誘導体 |
| EP1296950A2 (en) | 2000-04-20 | 2003-04-02 | NPS Allelix Corp. | Aminopiperidines for use as glyt-1 inhibitors |
| US6589978B2 (en) | 2000-06-30 | 2003-07-08 | Hoffman-La Roche Inc. | 1-sulfonyl pyrrolidine derivatives |
| HUP0303360A2 (hu) | 2000-09-25 | 2004-01-28 | Actelion Pharmaceuticals Ltd. | Maláriaellenes hatású szubsztituált amino-aza-cikloalkánok és ezeket tartalmazó gyógyszerkészítmények |
| MXPA04001014A (es) * | 2001-08-03 | 2004-05-27 | Schering Corp | Novedosos inhibidores de la gama secretasa. |
| US7122675B2 (en) * | 2001-08-03 | 2006-10-17 | Schering Corporation | Gamma secretase inhibitors |
| US7256186B2 (en) * | 2002-02-06 | 2007-08-14 | Schering Corporation | Gamma secretase inhibitors |
| US20040171614A1 (en) | 2002-02-06 | 2004-09-02 | Schering-Plough Corporation | Novel gamma secretase inhibitors |
| TW200302717A (en) | 2002-02-06 | 2003-08-16 | Schering Corp | Novel gamma secretase inhibitors |
| TW200510405A (en) | 2003-05-13 | 2005-03-16 | Schering Corp | Bridged n-arylsulfonylpiperidines as gamma-secretase inhibitors |
| JP4247081B2 (ja) | 2003-09-24 | 2009-04-02 | 三菱電機株式会社 | レーザアニール装置のレーザビーム強度モニタ方法とレーザアニール装置 |
| US20060004004A1 (en) * | 2004-04-05 | 2006-01-05 | Schering Corporation | Novel gamma secretase inhibitors |
| WO2005113542A2 (en) * | 2004-05-20 | 2005-12-01 | Elan Pharmaceuticals, Inc. | N-cyclic sulfonamido inhibitors of gamma secretase |
| AR059075A1 (es) * | 2006-01-20 | 2008-03-12 | Schering Corp | Bencesulfonil - cromano , tiocromano tetrahidronaftaleno e inhibidores de gamma secretasa relacionados |
-
2005
- 2005-06-28 AT AT05790194T patent/ATE461926T1/de not_active IP Right Cessation
- 2005-06-28 PE PE2005000751A patent/PE20060481A1/es not_active Application Discontinuation
- 2005-06-28 CN CNA200910152119XA patent/CN101602741A/zh active Pending
- 2005-06-28 CN CNA2005800284229A patent/CN101048393A/zh active Pending
- 2005-06-28 DE DE602005020156T patent/DE602005020156D1/de not_active Expired - Lifetime
- 2005-06-28 CA CA002570183A patent/CA2570183A1/en not_active Abandoned
- 2005-06-28 US US11/168,797 patent/US7763613B2/en not_active Expired - Fee Related
- 2005-06-28 JP JP2007519415A patent/JP2008505100A/ja active Pending
- 2005-06-28 AR ARP050102662A patent/AR050994A1/es not_active Application Discontinuation
- 2005-06-28 WO PCT/US2005/023187 patent/WO2006004880A2/en not_active Ceased
- 2005-06-28 MX MX2007000040A patent/MX2007000040A/es active IP Right Grant
- 2005-06-28 ES ES05790194T patent/ES2341560T3/es not_active Expired - Lifetime
- 2005-06-28 EP EP05790194A patent/EP1789404B1/en not_active Expired - Lifetime
- 2005-06-29 TW TW094121770A patent/TWI297270B/zh not_active IP Right Cessation
-
2009
- 2009-12-08 US US12/633,286 patent/US20100087425A1/en not_active Abandoned
- 2009-12-08 US US12/633,311 patent/US7998958B2/en not_active Expired - Fee Related
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