JP2013531040A5 - - Google Patents
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- Publication number
- JP2013531040A5 JP2013531040A5 JP2013519760A JP2013519760A JP2013531040A5 JP 2013531040 A5 JP2013531040 A5 JP 2013531040A5 JP 2013519760 A JP2013519760 A JP 2013519760A JP 2013519760 A JP2013519760 A JP 2013519760A JP 2013531040 A5 JP2013531040 A5 JP 2013531040A5
- Authority
- JP
- Japan
- Prior art keywords
- azeno
- metheno
- cyclopenta
- methyl
- hexahydro
- 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.)
- Granted
Links
- -1 4-Chloro-1H-imidazol-1-yl Chemical group 0.000 claims 50
- MPJNYKXXSWCRRM-UHFFFAOYSA-N 1-oxa-2,3,4-triazacycloheptadeca-2,4,6,8,10,12,14,16-octaene Chemical compound C1=CC=CC=CC=NN=NOC=CC=CC=C1 MPJNYKXXSWCRRM-UHFFFAOYSA-N 0.000 claims 45
- 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 20
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 13
- FVFHZKZQBYHTKR-UHFFFAOYSA-N 1-oxa-2,3,4-triazacyclohexadeca-3,5,7,9,11,13,15-heptaene Chemical compound C=1C=CC=CC=CONN=NC=CC=CC=1 FVFHZKZQBYHTKR-UHFFFAOYSA-N 0.000 claims 9
- BBTCVLLKSAWIGB-UHFFFAOYSA-N 1-oxa-2,3-diazacycloheptadeca-2,4,6,8,10,12,14,16-octaene Chemical compound C1=CC=CC=CC=CON=NC=CC=CC=C1 BBTCVLLKSAWIGB-UHFFFAOYSA-N 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- XXVMPTJGGYAODS-UHFFFAOYSA-N 1-oxa-2,3,4,5-tetrazacyclooctadeca-3,5,7,9,11,13,15,17-octaene Chemical compound O1NN=NN=CC=CC=CC=CC=CC=CC=C1 XXVMPTJGGYAODS-UHFFFAOYSA-N 0.000 claims 4
- RPZTVJWNMAAMDR-UHFFFAOYSA-N 1-oxa-2,3,4-triazacyclooctadeca-3,5,7,9,11,13,15,17-octaene Chemical compound N1OC=CC=CC=CC=CC=CC=CC=CN=N1 RPZTVJWNMAAMDR-UHFFFAOYSA-N 0.000 claims 4
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 201000002832 Lewy body dementia Diseases 0.000 claims 2
- WUIQCJWNFQDSMX-UHFFFAOYSA-N O1NNN=CC=CC=CC=C(C=CC=CC=C1)O Chemical compound O1NNN=CC=CC=CC=C(C=CC=CC=C1)O WUIQCJWNFQDSMX-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 201000008319 inclusion body myositis Diseases 0.000 claims 2
- 208000027061 mild cognitive impairment Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000009829 Lewy Body Disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- SXLTZVXYXZVKIU-UHFFFAOYSA-N O1N=NN=CC=C(C=CC=CC=CC=CC=C1)C#N Chemical compound O1N=NN=CC=C(C=CC=CC=CC=CC=C1)C#N SXLTZVXYXZVKIU-UHFFFAOYSA-N 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002560 nitrile group Chemical group 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 229910052717 sulfur Chemical group 0.000 claims 1
- 239000011593 sulfur Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36442510P | 2010-07-15 | 2010-07-15 | |
| US61/364,425 | 2010-07-15 | ||
| PCT/US2011/043628 WO2012009309A1 (en) | 2010-07-15 | 2011-07-12 | Compounds for the reduction of beta-amyloid production |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013531040A JP2013531040A (ja) | 2013-08-01 |
| JP2013531040A5 true JP2013531040A5 (https=) | 2014-08-07 |
| JP5755739B2 JP5755739B2 (ja) | 2015-07-29 |
Family
ID=44511486
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013519760A Expired - Fee Related JP5755739B2 (ja) | 2010-07-15 | 2011-07-12 | β−アミロイド産生の減少のための化合物 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8637523B2 (https=) |
| EP (1) | EP2593461B1 (https=) |
| JP (1) | JP5755739B2 (https=) |
| KR (1) | KR20130041944A (https=) |
| CN (1) | CN102971325B (https=) |
| AR (1) | AR082241A1 (https=) |
| AU (1) | AU2011279412B2 (https=) |
| BR (1) | BR112013000920A2 (https=) |
| CA (1) | CA2805294A1 (https=) |
| CO (1) | CO6670589A2 (https=) |
| EA (1) | EA021527B1 (https=) |
| IL (1) | IL224202A (https=) |
| MX (1) | MX2013000514A (https=) |
| NZ (1) | NZ606950A (https=) |
| SG (1) | SG186392A1 (https=) |
| TW (1) | TW201206946A (https=) |
| WO (1) | WO2012009309A1 (https=) |
| ZA (1) | ZA201301178B (https=) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0696663B2 (ja) | 1986-08-04 | 1994-11-30 | 東レ株式会社 | 樹脂組成物 |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| KR101473081B1 (ko) | 2013-01-25 | 2014-12-16 | 영남대학교 산학협력단 | 고리형 2-다이아조-1,3-다이카보닐 화합물을 출발물질로 하는 고리형 베타-엔아미노아마이드 유도체 및 우라실 유도체의 합성방법 |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| CN105164136B (zh) * | 2013-05-06 | 2017-12-22 | 默克专利股份公司 | 作为激酶抑制剂的大环化合物 |
| JP6368776B2 (ja) | 2013-06-04 | 2018-08-01 | 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 |
| WO2014195323A1 (en) | 2013-06-04 | 2014-12-11 | Acturum Life Science AB | Pyrimidine compounds and their use as gamma secretase modulators |
| 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 |
| US9833454B2 (en) | 2014-04-02 | 2017-12-05 | Bristol-Myers Squibb Company | Difluoromethoxy compound with low bioactivation potential for the reduction of beta-amyloid production |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| US10717749B2 (en) | 2015-09-29 | 2020-07-21 | Bayer Pharma Aktiengesellschaft | Macrocyclic sulfondiimine compounds |
| JP6888000B2 (ja) | 2015-10-08 | 2021-06-16 | バイエル ファーマ アクチエンゲゼルシャフト | 新規な修飾された大環状化合物 |
| WO2017060322A2 (en) | 2015-10-10 | 2017-04-13 | Bayer Pharma Aktiengesellschaft | Ptefb-inhibitor-adc |
| EP3601253B1 (en) | 2017-03-28 | 2021-09-15 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| CA3057891A1 (en) | 2017-03-28 | 2018-10-04 | Bayer Aktiengesellschaft | Novel ptefb inhibiting macrocyclic compounds |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
| MA52493A (fr) | 2018-05-04 | 2021-03-10 | Incyte Corp | Sels d'un inhibiteur de fgfr |
| CN111471056B (zh) * | 2019-01-23 | 2021-07-02 | 成都先导药物开发股份有限公司 | 一种大环类免疫调节剂 |
| PH12021551635A1 (en) | 2019-01-29 | 2022-05-02 | Shandong Xuanzhu Pharma Co Ltd | Hexone glucokinase inhibitor and use thereof |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ568325A (en) * | 2005-11-16 | 2011-05-27 | S Bio Pte Ltd | Macrocyclic oxygen linked pyrimidine derivatives |
| US7932261B2 (en) * | 2006-02-06 | 2011-04-26 | Janssen Pharmaceutica Nv | Macrocycle derivatives useful as inhibitors of β-secretase (BACE) |
| ITMI20061513A1 (it) | 2006-07-31 | 2008-02-01 | Poli Costruzione Materiali Trazione Spa | Unita' frenante compatta a disco per veicoli su rotaia |
| US8450343B2 (en) * | 2007-12-06 | 2013-05-28 | Xianhai Huang | Gamma secretase modulators |
| EP2227471A1 (en) * | 2007-12-11 | 2010-09-15 | Schering Corporation | Gamma secretase modulators |
| ES2375919T3 (es) * | 2008-01-11 | 2012-03-07 | F. Hoffmann-La Roche Ag | Moduladores de beta-amiloide. |
-
2011
- 2011-07-11 TW TW100124501A patent/TW201206946A/zh unknown
- 2011-07-12 CA CA2805294A patent/CA2805294A1/en not_active Abandoned
- 2011-07-12 EP EP11746340.6A patent/EP2593461B1/en not_active Not-in-force
- 2011-07-12 KR KR1020137003728A patent/KR20130041944A/ko not_active Withdrawn
- 2011-07-12 NZ NZ606950A patent/NZ606950A/en not_active IP Right Cessation
- 2011-07-12 AU AU2011279412A patent/AU2011279412B2/en not_active Ceased
- 2011-07-12 SG SG2012093274A patent/SG186392A1/en unknown
- 2011-07-12 WO PCT/US2011/043628 patent/WO2012009309A1/en not_active Ceased
- 2011-07-12 CN CN201180034655.5A patent/CN102971325B/zh not_active Expired - Fee Related
- 2011-07-12 JP JP2013519760A patent/JP5755739B2/ja not_active Expired - Fee Related
- 2011-07-12 BR BR112013000920A patent/BR112013000920A2/pt not_active IP Right Cessation
- 2011-07-12 MX MX2013000514A patent/MX2013000514A/es active IP Right Grant
- 2011-07-12 US US13/180,623 patent/US8637523B2/en active Active
- 2011-07-12 EA EA201270824A patent/EA021527B1/ru not_active IP Right Cessation
- 2011-07-15 AR ARP110102569A patent/AR082241A1/es not_active Application Discontinuation
-
2013
- 2013-01-13 IL IL224202A patent/IL224202A/en not_active IP Right Cessation
- 2013-02-11 CO CO13027683A patent/CO6670589A2/es active IP Right Grant
- 2013-02-14 ZA ZA2013/01178A patent/ZA201301178B/en unknown
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