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 (https=) | 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 (https=) |
| EP (1) | EP2379553B1 (https=) |
| JP (1) | JP5638007B2 (https=) |
| CN (1) | CN102356081B (https=) |
| AR (1) | AR075139A1 (https=) |
| ES (1) | ES2426023T3 (https=) |
| TW (1) | TW201030002A (https=) |
| WO (1) | WO2010083141A1 (https=) |
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 |
| EA019685B1 (ru) | 2009-02-06 | 2014-05-30 | Янссен Фармасьютикалз, Инк. | Новые замещенные бициклические гетероциклические соединения в качестве модуляторов гамма-секретазы |
| 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 |
| BRPI1011190A8 (pt) | 2009-05-07 | 2016-11-16 | Janssen Pharmaceuticals Inc | Derivados de indazol e aza-indazol substituídos como moduladores de gama secretase |
| ES2519565T3 (es) | 2009-07-15 | 2014-11-07 | Janssen Pharmaceuticals Inc. | Derivados de triazol e imidazol sustituidos como moduladores de gamma secretasa |
| EP2523949B1 (en) * | 2010-01-15 | 2014-08-20 | Janssen Pharmaceuticals Inc. | Novel substituted triazole derivatives as gamma secretase modulators |
| US9150591B2 (en) | 2010-08-10 | 2015-10-06 | Takeda Pharmaceutical Company Limited | Heterocyclic compound and use thereof |
| KR20130139895A (ko) | 2010-09-02 | 2013-12-23 | 다케다 야쿠힌 고교 가부시키가이샤 | 경도인지 장애의 치료 또는 예방용 융합 트리아졸 |
| 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 |
| CA2827969A1 (en) | 2011-03-24 | 2012-09-27 | Janssen Pharmaceuticals, Inc. | Novel substituted triazolyl piperazine and triazolyl piperidine derivatives as gamma secretase modulators |
| CA2830027C (en) | 2011-03-31 | 2016-04-26 | Pfizer Inc. | Novel bicyclic pyridinones |
| TWI567079B (zh) | 2011-07-15 | 2017-01-21 | 健生醫藥公司 | 作為伽瑪分泌酶調節劑之新穎的經取代的吲哚衍生物 |
| NZ702611A (en) | 2012-05-16 | 2016-10-28 | Cellzome Ltd | Substituted 3, 4 - dihydro - 2h - pyrido [1, 2 -a] pyrazine - 1, 6 - dione derivatives useful for the treatment of (inter alia) alzheimer’s disease |
| 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 |
| ES2612215T3 (es) | 2013-01-17 | 2017-05-12 | Janssen Pharmaceutica, N.V. | Novedosos derivados de pirido-piperazinona sustituidos como moduladores de gamma secretasa |
| WO2014127816A1 (en) * | 2013-02-21 | 2014-08-28 | Boehringer Ingelheim International Gmbh | Dihydropteridinones ii |
| NO3004079T3 (https=) | 2013-06-04 | 2018-06-16 | ||
| 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 |
| MX368391B (es) | 2015-02-03 | 2019-09-30 | Pfizer | Ciclopropabenzofuranil-piridopirazindionas novedosas. |
| 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 |
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
| EP3728262B1 (en) | 2017-12-18 | 2023-03-15 | 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 |
| AU2020321955A1 (en) | 2019-07-30 | 2022-03-17 | Eikonizo Therapapeutics, Inc. | HDAC6 inhibitors and uses thereof |
| CR20220160A (es) | 2019-09-16 | 2022-06-16 | Takeda Pharmaceuticals Co | Derivados de piridazin-3(2h)-ona fusionados con azol |
| CN114787163A (zh) | 2019-11-29 | 2022-07-22 | 豪夫迈·罗氏有限公司 | 用于制备 (9S)-2-溴-9-(2,3,4-三氟苯基)-6,7,8,9-四氢-5H-[1,2,4]三唑并[1,5-a]氮杂䓬的方法 |
| TW202345813A (zh) | 2022-04-08 | 2023-12-01 | 美商艾科尼佐療法股份有限公司 | 㗁二唑hdac6抑制劑及其用途 |
| 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 |
|---|---|---|---|---|
| AR059955A1 (es) * | 2006-03-09 | 2008-05-14 | Eisai R&D Man Co Ltd | Compuestos policiclicos no peptidicos, medicamentos que los contienen, y usos para prevenir o tratar enfermedades causadas por la produccion de beta amiloide |
| RU2009144998A (ru) * | 2007-05-07 | 2011-06-20 | Шеринг Корпорейшн (US) | Модуляторы гамма-секретазы |
| KR101138045B1 (ko) | 2007-05-11 | 2012-04-24 | 에프. 호프만-라 로슈 아게 | 아밀로이드 베타에 대한 조절제로서의 헤트아릴아닐린 |
| US7935815B2 (en) * | 2007-08-31 | 2011-05-03 | Eisai R&D Management Co., Ltd. | Imidazoyl pyridine compounds and salts thereof |
| BRPI0815773A2 (pt) | 2007-08-31 | 2019-09-24 | Eisai R&D Man Co Ltd | composto, e, medicamento. |
| WO2009087127A1 (en) | 2008-01-11 | 2009-07-16 | F. Hoffmann-La Roche Ag | Modulators for amyloid beta |
| JP5328816B2 (ja) | 2008-02-22 | 2013-10-30 | エフ.ホフマン−ラ ロシュ アーゲー | アミロイドβの調節薬 |
-
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 JP JP2011546297A patent/JP5638007B2/ja not_active Expired - Fee Related
- 2010-01-12 EP EP10700643.9A patent/EP2379553B1/en not_active Not-in-force
- 2010-01-12 ES ES10700643T patent/ES2426023T3/es active Active
- 2010-01-15 AR ARP100100099A patent/AR075139A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TW201030002A (en) | 2010-08-16 |
| EP2379553B1 (en) | 2013-06-26 |
| ES2426023T3 (es) | 2013-10-18 |
| WO2010083141A1 (en) | 2010-07-22 |
| JP2012515205A (ja) | 2012-07-05 |
| AR075139A1 (es) | 2011-03-09 |
| EP2379553A1 (en) | 2011-10-26 |
| US20110015175A1 (en) | 2011-01-20 |
| US8349880B2 (en) | 2013-01-08 |
| CN102356081B (zh) | 2014-08-27 |
| CN102356081A (zh) | 2012-02-15 |
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