JP2017528504A5 - - Google Patents
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- Publication number
- JP2017528504A5 JP2017528504A5 JP2017516367A JP2017516367A JP2017528504A5 JP 2017528504 A5 JP2017528504 A5 JP 2017528504A5 JP 2017516367 A JP2017516367 A JP 2017516367A JP 2017516367 A JP2017516367 A JP 2017516367A JP 2017528504 A5 JP2017528504 A5 JP 2017528504A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrazol
- methyl
- linked
- imidazol
- dimethyl
- 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 di-substituted pyrazole Chemical class 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 2
- 230000004060 metabolic process Effects 0.000 claims 2
- 125000001607 1,2,3-triazol-1-yl group Chemical group [*]N1N=NC([H])=C1[H] 0.000 claims 1
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims 1
- 125000001401 1,2,4-triazol-4-yl group Chemical group N=1N=C([H])N([*])C=1[H] 0.000 claims 1
- YWYXOEPVLRALTC-CILPGNKCSA-N FCC1=NN(C(=C1)C)C=1C=C(C=CC=1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 Chemical compound FCC1=NN(C(=C1)C)C=1C=C(C=CC=1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 YWYXOEPVLRALTC-CILPGNKCSA-N 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 229940123038 Integrin antagonist Drugs 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000008485 antagonism Effects 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 claims 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 150000002460 imidazoles Chemical class 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 150000003217 pyrazoles Chemical class 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1417094.8 | 2014-09-26 | ||
| GBGB1417094.8A GB201417094D0 (en) | 2014-09-26 | 2014-09-26 | Novel compounds |
| PCT/EP2015/071782 WO2016046230A1 (en) | 2014-09-26 | 2015-09-22 | Naphthyridine derivatives as alpha v beta 6 integrin antagonists for the treatment of e.g. fibrotic diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017528504A JP2017528504A (ja) | 2017-09-28 |
| JP2017528504A5 true JP2017528504A5 (enExample) | 2018-10-25 |
| JP6657196B2 JP6657196B2 (ja) | 2020-03-04 |
Family
ID=51901231
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017516367A Expired - Fee Related JP6657196B2 (ja) | 2014-09-26 | 2015-09-22 | 線維性疾患などの治療のためのαｖβ６インテグリンアンタゴニストとしてのナフチリジン誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US10144733B2 (enExample) |
| EP (1) | EP3197894B1 (enExample) |
| JP (1) | JP6657196B2 (enExample) |
| KR (1) | KR20170053638A (enExample) |
| CN (1) | CN107074851B (enExample) |
| AU (1) | AU2015320863B2 (enExample) |
| BR (1) | BR112017006242A2 (enExample) |
| CA (1) | CA2962321A1 (enExample) |
| ES (1) | ES2811119T3 (enExample) |
| GB (1) | GB201417094D0 (enExample) |
| RU (1) | RU2692775C2 (enExample) |
| WO (1) | WO2016046230A1 (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201305668D0 (en) | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| GB201417094D0 (en) * | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417011D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417018D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417002D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| HK1254295A1 (zh) * | 2015-11-23 | 2019-07-19 | 默克专利股份有限公司 | 用於治疗纤维化和/或纤维化病症的抗-αＶ整合素抗体 |
| EP3429355B1 (de) | 2016-03-15 | 2020-02-05 | Bayer CropScience AG | Substituierte sulfonylamide zur bekämpfung tierischer schädlinge |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| EA201991123A1 (ru) | 2016-11-08 | 2019-11-29 | ИНДАЗОЛОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ АНТАГОНИСТОВ ИНТЕГРИНА αV | |
| ES2984394T3 (es) | 2016-11-08 | 2024-10-29 | Bristol Myers Squibb Co | Compuestos mono y espirocíclicos que contienen ciclobutano y azetidina como inhibidores de la integrina alfa v |
| AU2017359030A1 (en) | 2016-11-08 | 2019-06-20 | Bristol-Myers Squibb Company | Pyrrole amides as alpha v integrin inhibitors |
| MA46743A (fr) | 2016-11-08 | 2019-09-18 | Bristol Myers Squibb Co | Acides propioniques à substitution en position 3 en tant qu'inhibiteurs d'intégrine alpha v |
| ES2898835T3 (es) | 2016-11-08 | 2022-03-09 | Bristol Myers Squibb Co | Azol amidas y aminas como inhibidores de la integrina alfav |
| USRE50554E1 (en) | 2016-12-23 | 2025-08-26 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| US11046685B2 (en) | 2017-02-28 | 2021-06-29 | Morphic Therapeutic, Inc. | Inhibitors of (α-v)(β-6) integrin |
| SG11201907820SA (en) | 2017-02-28 | 2019-09-27 | Morphic Therapeutic Inc | Inhibitors of (alpha-v)(beta-6) integrin |
| US11292802B2 (en) | 2017-11-07 | 2022-04-05 | Bristol-Myers Squibb Company | Substituted tetrahydropyrrolo[1,2-a]pyrazines as alpha v integrin inhibitors |
| CA3109534A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibiting .alpha.v .beta.6 integrin |
| UY38352A (es) * | 2018-08-29 | 2020-03-31 | Morphic Therapeutic Inc | Inhibidores de integrina alfavbeta6 |
| EP3843727A4 (en) | 2018-08-29 | 2022-08-17 | Morphic Therapeutic, Inc. | INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN |
| GB202010626D0 (en) | 2020-07-10 | 2020-08-26 | Univ Nottingham | Compound |
| WO2023170680A1 (en) | 2022-03-08 | 2023-09-14 | Equashield Medical Ltd | Fluid transfer station in a robotic pharmaceutical preparation system |
| AU2023399039A1 (en) | 2022-12-14 | 2025-05-22 | Alnylam Pharmaceuticals, Inc. | ALPHA-V BETA-6(ανβ6) INTEGRIN LIGANDS FOR EXTRAHEPATIC DELIVERY |
| WO2025259743A1 (en) | 2024-06-12 | 2025-12-18 | Alnylam Pharmaceuticals, Inc. | Dual conjugate compounds for extrahepatic delivery |
| WO2025259747A2 (en) | 2024-06-12 | 2025-12-18 | Alnylam Pharmaceuticals, Inc. | Dystrophy myotonic protein kinase (dmpk) irna compositions and methods of use thereof |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU736026B2 (en) | 1997-12-17 | 2001-07-26 | Merck & Co., Inc. | Integrin receptor antagonists |
| WO1999031061A1 (en) | 1997-12-17 | 1999-06-24 | Merck & Co., Inc. | Integrin receptor antagonists |
| DK1187592T3 (da) | 1999-06-02 | 2007-11-05 | Merck & Co Inc | Alfa v-integrinreceptorantagonister |
| AU748949B2 (en) | 1999-06-23 | 2002-06-13 | Merck & Co., Inc. | Integrin receptor antagonists |
| JP2003510360A (ja) * | 1999-10-04 | 2003-03-18 | メルク エンド カムパニー インコーポレーテッド | インテグリン受容体拮抗薬 |
| CZ20021508A3 (cs) | 1999-11-08 | 2002-10-16 | Merck & Co., Inc. | Způsob výroby imidazolidinonových derivátů |
| US6933304B2 (en) | 2000-06-15 | 2005-08-23 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| DE60126496T2 (de) | 2000-07-26 | 2007-11-15 | Merck & Co., Inc. | Alpha v integrin-rezeptor-antagonisten |
| AU2001290772A1 (en) | 2000-09-14 | 2002-03-26 | Merck And Co., Inc. | Alpha v integrin receptor antagonists |
| WO2002053099A2 (en) | 2001-01-03 | 2002-07-11 | Merck & Co., Inc. | Methods and compositions for treating periodontal disease |
| DE10112771A1 (de) | 2001-03-16 | 2002-09-26 | Merck Patent Gmbh | Inhibitoren des Integrins alpha¶v¶beta¶6¶ |
| AR037517A1 (es) * | 2001-11-05 | 2004-11-17 | Novartis Ag | Derivados de naftiridinas, un proceso para su preparacion, composicion farmaceutica y el uso de los mismos para la preparacion de un medicamento para el tratamiento de una enfermedad inflamatoria |
| US20040224986A1 (en) | 2002-08-16 | 2004-11-11 | Bart De Corte | Piperidinyl targeting compounds that selectively bind integrins |
| US20050043344A1 (en) | 2002-12-20 | 2005-02-24 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists derivatives |
| US6932865B2 (en) | 2003-04-11 | 2005-08-23 | Lockheed Martin Corporation | System and method of making single-crystal structures through free-form fabrication techniques |
| MX2009010050A (es) | 2007-03-23 | 2009-10-12 | Amgen Inc | Derivados de quinolina o quinoxalina 3-sustituidos y su uso como inhibidores de fosfotidilinositol 3-cinasa (p13k). |
| US8563566B2 (en) * | 2007-08-01 | 2013-10-22 | Valeant Pharmaceuticals International | Naphthyridine derivatives as potassium channel modulators |
| JP2011500823A (ja) | 2007-10-22 | 2011-01-06 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体 |
| WO2011111880A1 (ko) | 2010-03-08 | 2011-09-15 | 주식회사 메디젠텍 | 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물 |
| GB201305668D0 (en) * | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| WO2015048819A1 (en) | 2013-09-30 | 2015-04-02 | The Regents Of The University Of California | Anti-alphavbeta1 integrin compounds and methods |
| GB201417094D0 (en) * | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417011D0 (en) * | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417018D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201417002D0 (en) * | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| WO2016134223A2 (en) | 2015-02-19 | 2016-08-25 | Scifluor Life Sciences, Inc. | Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof |
| CA2981371A1 (en) | 2015-03-10 | 2016-09-15 | The Regents Of The University Of California | Anti-alphavbeta1 integrin inhibitors and methods of use |
| GB201604589D0 (en) | 2016-03-18 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical compound |
| GB201604681D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
-
2014
- 2014-09-26 GB GBGB1417094.8A patent/GB201417094D0/en not_active Ceased
-
2015
- 2015-09-22 RU RU2017114355A patent/RU2692775C2/ru not_active IP Right Cessation
- 2015-09-22 CA CA2962321A patent/CA2962321A1/en not_active Abandoned
- 2015-09-22 KR KR1020177007736A patent/KR20170053638A/ko not_active Withdrawn
- 2015-09-22 EP EP15767478.9A patent/EP3197894B1/en active Active
- 2015-09-22 BR BR112017006242A patent/BR112017006242A2/pt not_active Application Discontinuation
- 2015-09-22 US US15/514,416 patent/US10144733B2/en not_active Expired - Fee Related
- 2015-09-22 ES ES15767478T patent/ES2811119T3/es active Active
- 2015-09-22 CN CN201580052204.2A patent/CN107074851B/zh not_active Expired - Fee Related
- 2015-09-22 WO PCT/EP2015/071782 patent/WO2016046230A1/en not_active Ceased
- 2015-09-22 JP JP2017516367A patent/JP6657196B2/ja not_active Expired - Fee Related
- 2015-09-22 AU AU2015320863A patent/AU2015320863B2/en not_active Ceased
-
2018
- 2018-10-19 US US16/165,506 patent/US10513517B2/en not_active Expired - Fee Related
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