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)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (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 (37)
| 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 |
| EA019702B1 (ru) | 2009-05-07 | 2014-05-30 | Янссен Фармасьютикалз, Инк. | Замещенные производные индазола и азаиндазола в качестве модуляторов гамма-секретазы |
| WO2011006903A1 (en) | 2009-07-15 | 2011-01-20 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Substituted triazole and imidazole derivatives as gamma secretase modulators |
| PH12012501381A1 (en) | 2010-01-15 | 2012-10-22 | Janssen Pharmaceuticals Inc | Novel substituted bicyclic triazole derivatives as gamma secretase modulators |
| WO2012020848A1 (en) | 2010-08-10 | 2012-02-16 | Takeda Pharmaceutical Company Limited | Heterocyclic compound and use thereof |
| UY33586A (es) * | 2010-09-02 | 2012-03-30 | Takeda Pharmaceutical | Compuesto heterocíclico y sus usos |
| 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 |
| ES2536442T3 (es) | 2011-03-24 | 2015-05-25 | Janssen Pharmaceuticals, Inc. | Derivados novedosos de triazolil piperazina y triazolil piperidina como moduladores de la gamma secretasa |
| WO2012131539A1 (en) | 2011-03-31 | 2012-10-04 | Pfizer Inc. | Novel bicyclic pyridinones |
| CN103874702B (zh) | 2011-07-15 | 2015-12-09 | 杨森制药公司 | 作为γ分泌酶调节剂的经取代的吲哚衍生物 |
| 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 |
| WO2014096212A1 (en) | 2012-12-20 | 2014-06-26 | Janssen Pharmaceutica Nv | NOVEL TRICYCLIC 3,4-DIHYDRO-2H-PYRIDO[1,2-α]PYRAZINE-1,6-DIONE DERIVATIVES AS GAMMA SECRETASE MODULATORS |
| KR102171710B1 (ko) | 2013-01-17 | 2020-10-30 | 얀센 파마슈티카 엔.브이. | 감마 세크레타제 조절 인자로서의 신규 치환 피리도-피페라지논 유도체 |
| JP6072308B2 (ja) * | 2013-02-21 | 2017-02-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ジヒドロプテリジノンii |
| ES2665421T3 (es) | 2013-06-04 | 2018-04-25 | Acturum Real Estate Ab | Compuestos de pirimidina y su uso como moduladores de la gamma secretasa |
| JP6396438B2 (ja) | 2013-06-04 | 2018-09-26 | アクチュラム・ライフ・サイエンス・アクチエボラーグ | トリアゾール化合物およびガンマセクレターゼモジュレーターとしてのその使用 |
| US9611254B2 (en) | 2013-06-04 | 2017-04-04 | Acturum Life Science AB | Triazole compounds and their use as gamma secretase modulators |
| 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 |
| KR102000382B1 (ko) | 2015-02-03 | 2019-07-15 | 화이자 인코포레이티드 | 신규 시클로프로파벤조푸라닐 피리도피라진디온 |
| CN109311878B (zh) * | 2016-06-27 | 2022-05-24 | 豪夫迈·罗氏有限公司 | 作为γ-分泌酶调节剂的三唑并吡啶类化合物 |
| 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 |
| US10357493B2 (en) | 2017-03-10 | 2019-07-23 | Selenity Therapeutics (Bermuda), Ltd. | Metalloenzyme inhibitor compounds |
| EP3728262B1 (en) * | 2017-12-18 | 2023-03-15 | F. Hoffmann-La Roche AG | Triazolo-azepine derivatives |
| US11370802B2 (en) * | 2018-01-22 | 2022-06-28 | Hoffmann-La Roche, Inc. | Triazolo-azepine derivatives |
| CN114727974A (zh) | 2019-07-30 | 2022-07-08 | 艾科尼佐治疗股份有限公司 | Hdac6抑制剂及其用途 |
| TWI873185B (zh) | 2019-09-16 | 2025-02-21 | 日商武田藥品工業股份有限公司 | 唑稠合之嗒-3(2h)-酮衍生物 |
| 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 |
| WO2022169985A1 (en) | 2021-02-03 | 2022-08-11 | Eikonizo Therapeutics, Inc. | Hdac6 inhibitors and uses thereof |
| AU2023250964A1 (en) | 2022-04-08 | 2024-11-07 | Eikonizo Therapeutics, Inc. | Oxadiazole hdac6 inhibitors and uses thereof |
| US20260049071A1 (en) * | 2022-08-08 | 2026-02-19 | Beyang Therapeutics Co., Ltd. | Protein tyrosine kinase inhibitor and medical use thereof |
| 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 |
|---|---|---|---|---|
| GEP20115139B (en) | 2006-03-09 | 2011-01-10 | Eisai R&D Man Co Ltd | Polycyclic cinnamide derivative |
| MX2009012177A (es) * | 2007-05-07 | 2009-11-23 | Schering Corp | Moduladores de gamma-secretasa. |
| CN101675045B (zh) | 2007-05-11 | 2012-11-28 | 弗·哈夫曼-拉罗切有限公司 | 作为β-淀粉样蛋白调节剂的杂芳基苯胺 |
| US7935815B2 (en) * | 2007-08-31 | 2011-05-03 | Eisai R&D Management Co., Ltd. | Imidazoyl pyridine compounds and salts thereof |
| AR068121A1 (es) | 2007-08-31 | 2009-11-04 | Eisai R&D Man Co Ltd | Compuestos multiciclicos para tratar enfermedades neurodegenerativas |
| ATE535515T1 (de) | 2008-01-11 | 2011-12-15 | Hoffmann La Roche | Modulatoren für amyloid beta |
| KR101247840B1 (ko) | 2008-02-22 | 2013-03-26 | 에프. 호프만-라 로슈 아게 | 아밀로이드 베타 조절제 |
-
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 CN CN201080012637.2A patent/CN102356081B/zh not_active Expired - Fee Related
- 2010-01-12 WO PCT/US2010/020710 patent/WO2010083141A1/en not_active Ceased
- 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
- 2010-01-15 AR ARP100100099A patent/AR075139A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CN102356081A (zh) | 2012-02-15 |
| US20110015175A1 (en) | 2011-01-20 |
| EP2379553A1 (en) | 2011-10-26 |
| TW201030002A (en) | 2010-08-16 |
| JP2012515205A (ja) | 2012-07-05 |
| US8349880B2 (en) | 2013-01-08 |
| WO2010083141A1 (en) | 2010-07-22 |
| CN102356081B (zh) | 2014-08-27 |
| AR075139A1 (es) | 2011-03-09 |
| EP2379553B1 (en) | 2013-06-26 |
| ES2426023T3 (es) | 2013-10-18 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP2379553B1 (en) | Bicyclic compounds for the reduction of beta-amyloid production | |
| TWI468402B (zh) | 降低β-類澱粉生成之化合物 | |
| US7935815B2 (en) | Imidazoyl pyridine compounds and salts thereof | |
| US9453000B2 (en) | Polycyclic compound | |
| JP5755739B2 (ja) | β−アミロイド産生の減少のための化合物 | |
| US9365588B2 (en) | Benzoxazines as modulators of ion channels | |
| US20110306607A1 (en) | Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels | |
| WO2015138689A1 (en) | Fused morpholinopyrimidines and methods of use thereof | |
| HK1164732B (en) | Compounds for the reduction of beta-amyloid production |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20121116 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20121116 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20140311 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20140319 |
|
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20140930 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20141021 |
|
| LAPS | Cancellation because of no payment of annual fees |