JP5638007B2 - ベータ−アミロイド産生の減少のための二環式化合物 - Google Patents
ベータ−アミロイド産生の減少のための二環式化合物 Download PDFInfo
- Publication number
- JP5638007B2 JP5638007B2 JP2011546297A JP2011546297A JP5638007B2 JP 5638007 B2 JP5638007 B2 JP 5638007B2 JP 2011546297 A JP2011546297 A JP 2011546297A JP 2011546297 A JP2011546297 A JP 2011546297A JP 5638007 B2 JP5638007 B2 JP 5638007B2
- Authority
- JP
- Japan
- Prior art keywords
- triazolo
- phenyl
- tetrahydro
- amine
- azepin
- 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.)
- Expired - Fee Related
Links
- 0 **c1n[n](CCCC2S*)c2n1 Chemical compound **c1n[n](CCCC2S*)c2n1 0.000 description 7
- WKRPLGPGKTXNET-UHFFFAOYSA-N CCCCC(C(O)=O)C(CC1)=CCC1F Chemical compound CCCCC(C(O)=O)C(CC1)=CCC1F WKRPLGPGKTXNET-UHFFFAOYSA-N 0.000 description 1
- KUXYSUOPKJTPDG-UHFFFAOYSA-N COC(CC[n]1nc(Nc(cc2)cc(OC)c2-[n]2cnc(Cl)c2)nc11)(CC1c(cc1)ccc1F)OC Chemical compound COC(CC[n]1nc(Nc(cc2)cc(OC)c2-[n]2cnc(Cl)c2)nc11)(CC1c(cc1)ccc1F)OC KUXYSUOPKJTPDG-UHFFFAOYSA-N 0.000 description 1
- LCDDVUOFTIETBK-UHFFFAOYSA-N COc(cc(cc1)Nc2nc(C(CCCC3)c(cc4)ccc4F)c3[s]2)c1-[n]1cnc(Cl)c1 Chemical compound COc(cc(cc1)Nc2nc(C(CCCC3)c(cc4)ccc4F)c3[s]2)c1-[n]1cnc(Cl)c1 LCDDVUOFTIETBK-UHFFFAOYSA-N 0.000 description 1
- ROOZINHKDFDHPE-WBPHRXDCSA-N C[C@@](CC[n]1nc(Nc(cc2)cc(F)c2-[n]2ncnc2C)nc11)(CC1c(cc1)ccc1F)O Chemical compound C[C@@](CC[n]1nc(Nc(cc2)cc(F)c2-[n]2ncnc2C)nc11)(CC1c(cc1)ccc1F)O ROOZINHKDFDHPE-WBPHRXDCSA-N 0.000 description 1
- VORUIQGQPLDLLD-MJTSIZKDSA-N C[C@H](CC[n]1nc(Nc(cc2)cc(F)c2-[n]2ncnc2C)nc11)CC1c(cc1)ccc1F Chemical compound C[C@H](CC[n]1nc(Nc(cc2)cc(F)c2-[n]2ncnc2C)nc11)CC1c(cc1)ccc1F VORUIQGQPLDLLD-MJTSIZKDSA-N 0.000 description 1
- BGFUVKQANOXDQS-PYCHMPPTSA-N C[C@H](C[C@@H]([C@@](C1)(C1C1)C#N)N/N=C/C)[C@H]1NC(N)SC Chemical compound C[C@H](C[C@@H]([C@@](C1)(C1C1)C#N)N/N=C/C)[C@H]1NC(N)SC BGFUVKQANOXDQS-PYCHMPPTSA-N 0.000 description 1
- PCKDNFYVFZAHEP-ZAKMOHSYSA-N C[C@H](NC(C(C(C)=[IH])[IH]CC1)N1N)NC(C[C@H]1F)=CC[C@@H]1N Chemical compound C[C@H](NC(C(C(C)=[IH])[IH]CC1)N1N)NC(C[C@H]1F)=CC[C@@H]1N PCKDNFYVFZAHEP-ZAKMOHSYSA-N 0.000 description 1
- RDPYLGGHGCHDQD-DTORHVGOSA-N C[C@H]1N(CCC=O)[C@@H](C)C=C1 Chemical compound C[C@H]1N(CCC=O)[C@@H](C)C=C1 RDPYLGGHGCHDQD-DTORHVGOSA-N 0.000 description 1
- ZJFOKHQCUBVZEG-UHFFFAOYSA-N C[n]1ncc(-c(c(OC)c2)ccc2/N=C(/N)\SC)c1 Chemical compound C[n]1ncc(-c(c(OC)c2)ccc2/N=C(/N)\SC)c1 ZJFOKHQCUBVZEG-UHFFFAOYSA-N 0.000 description 1
- LBLZLJGRKKCSES-UHFFFAOYSA-N Cc(nc1C)c[n]1-c(c(F)cc(/N=C(/N)\SC)c1)c1F Chemical compound Cc(nc1C)c[n]1-c(c(F)cc(/N=C(/N)\SC)c1)c1F LBLZLJGRKKCSES-UHFFFAOYSA-N 0.000 description 1
- KQMYXXUPEAVODS-UHFFFAOYSA-N Cc1n[o]c(-c(c(OC)c2)ccc2/N=C(/N)\SC)c1 Chemical compound Cc1n[o]c(-c(c(OC)c2)ccc2/N=C(/N)\SC)c1 KQMYXXUPEAVODS-UHFFFAOYSA-N 0.000 description 1
- AEOGHGKHDXSBTB-UHFFFAOYSA-N OC(C1(CCCCCl)SCCCS1)=O Chemical compound OC(C1(CCCCCl)SCCCS1)=O AEOGHGKHDXSBTB-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/10—Spiro-condensed systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14531909P | 2009-01-16 | 2009-01-16 | |
| US61/145,319 | 2009-01-16 | ||
| PCT/US2010/020710 WO2010083141A1 (en) | 2009-01-16 | 2010-01-12 | Bicyclic compounds for the reduction of beta-amyloid production |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012515205A JP2012515205A (ja) | 2012-07-05 |
| JP2012515205A5 JP2012515205A5 (enExample) | 2013-01-17 |
| JP5638007B2 true JP5638007B2 (ja) | 2014-12-10 |
Family
ID=42061022
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011546297A Expired - Fee Related JP5638007B2 (ja) | 2009-01-16 | 2010-01-12 | ベータ−アミロイド産生の減少のための二環式化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8349880B2 (enExample) |
| EP (1) | EP2379553B1 (enExample) |
| JP (1) | JP5638007B2 (enExample) |
| CN (1) | CN102356081B (enExample) |
| AR (1) | AR075139A1 (enExample) |
| ES (1) | ES2426023T3 (enExample) |
| TW (1) | TW201030002A (enExample) |
| WO (1) | WO2010083141A1 (enExample) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2011004680A (es) | 2008-11-06 | 2011-05-25 | Astrazeneca Ab | Moduladores de beta amiloide. |
| PA8854101A1 (es) | 2008-12-18 | 2010-07-27 | Ortho Mcneil Janssen Pharm | Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa |
| CN102325765B (zh) | 2009-02-06 | 2014-12-24 | 杨森制药公司 | 作为γ-分泌酶调节剂的取代的双环杂环化合物 |
| TWI461425B (zh) | 2009-02-19 | 2014-11-21 | Janssen Pharmaceuticals Inc | 作為伽瑪分泌酶調節劑之新穎經取代的苯并唑、苯并咪唑、唑并吡啶及咪唑并吡啶衍生物類 |
| CA2755467A1 (en) | 2009-05-07 | 2010-12-23 | Janssen Pharmaceuticals, Inc. | Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| BR112012000915A2 (pt) | 2009-07-15 | 2019-09-24 | Janssen Pharmaceuticals Inc | derivados de triazol e imidazol substituídos como moduladores de gama secretase. |
| AU2011206635B2 (en) | 2010-01-15 | 2015-01-22 | Cellzome Limited | Novel substituted triazole derivatives as gamma secretase modulators |
| SI2603513T1 (sl) | 2010-08-10 | 2020-07-31 | Takeda Pharmaceutical Company Limited | Heterociklična spojina in njena uporaba kot pozitivni alosterični modulator receptorja AMPA |
| EP2611805A1 (en) | 2010-09-02 | 2013-07-10 | Takeda Pharmaceutical Company Limited | Fused triazoles for the treatment or prophylaxis of mild cognitive impairment |
| TW201309655A (zh) * | 2011-01-28 | 2013-03-01 | 必治妥美雅史谷比公司 | 降低β－類澱粉生成之化合物 |
| AU2012230348A1 (en) | 2011-03-24 | 2013-08-29 | Cellzome Limited | Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators |
| WO2012131539A1 (en) | 2011-03-31 | 2012-10-04 | Pfizer Inc. | Novel bicyclic pyridinones |
| ES2555167T3 (es) | 2011-07-15 | 2015-12-29 | Janssen Pharmaceuticals, Inc. | Nuevos derivados de indol sustituidos como moduladores de gamma secretasa |
| CN104583208B (zh) | 2012-05-16 | 2016-09-28 | 杨森制药公司 | 可用于治疗(尤其是)阿尔茨海默病的取代的3,4-二氢-2H-吡啶并[1,2-a]吡嗪-1,6-二酮衍生物 |
| EP2687528A1 (en) | 2012-07-17 | 2014-01-22 | Ares Trading S.A. | Fused triazole derivatives as gamma secretase modulators |
| UA110688C2 (uk) | 2012-09-21 | 2016-01-25 | Пфайзер Інк. | Біциклічні піридинони |
| AU2013366668B2 (en) | 2012-12-20 | 2017-07-20 | Janssen Pharmaceutica Nv | Novel tricyclic 3,4-dihydro-2H-pyrido[1,2-alpha]pyrazine -1,6-dione derivatives as gamma secretase modulators |
| AU2014206834B2 (en) | 2013-01-17 | 2017-06-22 | Janssen Pharmaceutica Nv | Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators |
| WO2014127816A1 (en) * | 2013-02-21 | 2014-08-28 | Boehringer Ingelheim International Gmbh | Dihydropteridinones ii |
| WO2014195323A1 (en) | 2013-06-04 | 2014-12-11 | Acturum Life Science AB | Pyrimidine compounds and their use as gamma secretase modulators |
| US9611254B2 (en) | 2013-06-04 | 2017-04-04 | Acturum Life Science AB | Triazole compounds and their use as gamma secretase modulators |
| DK3004080T3 (da) | 2013-06-04 | 2019-01-02 | Acturum Real Estate Ab | Triazolforbindelser og deres anvendelse som gamma-sekretase-modulatorer |
| US10562897B2 (en) | 2014-01-16 | 2020-02-18 | Janssen Pharmaceutica Nv | Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators |
| TN2017000342A1 (en) | 2015-02-03 | 2019-01-16 | Pfizer | Novel cyclopropabenzofuranyl pyridopyrazinediones |
| JP7012715B2 (ja) * | 2016-06-27 | 2022-01-28 | エフ．ホフマン－ラ ロシュ アーゲー | γ－セクレターゼモジュレーターとしてのトリアゾロピリジン |
| AR109829A1 (es) * | 2016-09-29 | 2019-01-30 | Hoffmann La Roche | Derivados de piperidina puenteados |
| EP3535266B1 (en) * | 2016-11-01 | 2021-12-29 | F. Hoffmann-La Roche AG | Bicyclic heteroaryl derivatives |
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
| WO2019121434A1 (en) * | 2017-12-18 | 2019-06-27 | F. Hoffmann-La Roche Ag | Triazolo-azepine derivatives |
| CN111417636B (zh) * | 2018-01-22 | 2023-09-26 | 豪夫迈·罗氏有限公司 | 三唑并-氮杂䓬衍生物 |
| WO2021021979A2 (en) | 2019-07-30 | 2021-02-04 | Eikonizo Therapapeutics, Inc. | Hdac6 inhibitors and uses thereof |
| PL4031552T3 (pl) | 2019-09-16 | 2025-03-17 | Takeda Pharmaceutical Company Limited | Pochodne azolowo-skondensowanych pirydazyn-3(2h)-onów |
| WO2021105337A1 (en) | 2019-11-29 | 2021-06-03 | F. Hoffmann-La Roche Ag | Process for the preparation (9s)-2-bromo-9-(2,3,4-trifluorophenyl)-6,7,8,9-tetrahydro-5h-[1,2,4]triazolo[1,5-a]azepine |
| EP4504190A4 (en) | 2022-04-08 | 2026-03-25 | Eikonizo Therapeutics Inc | OXADIAZOLE HDAC6 INHIBITORS AND THEIR USES |
| CN119604488A (zh) * | 2022-08-08 | 2025-03-11 | 苏州必扬医药科技有限公司 | 一种蛋白酪氨酸激酶抑制剂及其医疗用途 |
| CN120324393B (zh) * | 2025-05-20 | 2025-11-04 | 广东海洋大学 | (2,4-二氯苯基)甲基硫基甲烷脒及其盐的用途 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL1992618T3 (pl) | 2006-03-09 | 2012-06-29 | Eisai R&D Man Co Ltd | Policykliczna pochodna cynamidowa |
| CA2686589A1 (en) * | 2007-05-07 | 2008-11-13 | Schering Corporation | Gamma secretase modulators |
| AU2008250436B2 (en) | 2007-05-11 | 2013-03-28 | F. Hoffmann-La Roche Ag | Hetarylanilines as modulators for amyloid beta |
| ES2529648T3 (es) | 2007-08-31 | 2015-02-24 | Eisai R&D Management Co., Ltd. | Compuesto policíclico |
| US7935815B2 (en) | 2007-08-31 | 2011-05-03 | Eisai R&D Management Co., Ltd. | Imidazoyl pyridine compounds and salts thereof |
| KR101244517B1 (ko) | 2008-01-11 | 2013-03-18 | 에프. 호프만-라 로슈 아게 | 아밀로이드 베타에 대한 조절제 |
| AU2009216851B2 (en) | 2008-02-22 | 2013-11-07 | F. Hoffmann-La Roche Ag | Modulators for amyloid beta |
-
2009
- 2009-12-31 TW TW098146451A patent/TW201030002A/zh unknown
-
2010
- 2010-01-07 US US12/683,791 patent/US8349880B2/en active Active
- 2010-01-12 EP EP10700643.9A patent/EP2379553B1/en not_active Not-in-force
- 2010-01-12 ES ES10700643T patent/ES2426023T3/es active Active
- 2010-01-12 JP JP2011546297A patent/JP5638007B2/ja not_active Expired - Fee Related
- 2010-01-12 WO PCT/US2010/020710 patent/WO2010083141A1/en not_active Ceased
- 2010-01-12 CN CN201080012637.2A patent/CN102356081B/zh not_active Expired - Fee Related
- 2010-01-15 AR ARP100100099A patent/AR075139A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP2379553A1 (en) | 2011-10-26 |
| CN102356081B (zh) | 2014-08-27 |
| AR075139A1 (es) | 2011-03-09 |
| JP2012515205A (ja) | 2012-07-05 |
| EP2379553B1 (en) | 2013-06-26 |
| CN102356081A (zh) | 2012-02-15 |
| ES2426023T3 (es) | 2013-10-18 |
| WO2010083141A1 (en) | 2010-07-22 |
| US20110015175A1 (en) | 2011-01-20 |
| TW201030002A (en) | 2010-08-16 |
| US8349880B2 (en) | 2013-01-08 |
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