JP2017528507A5 - - Google Patents
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- Publication number
- JP2017528507A5 JP2017528507A5 JP2017516387A JP2017516387A JP2017528507A5 JP 2017528507 A5 JP2017528507 A5 JP 2017528507A5 JP 2017516387 A JP2017516387 A JP 2017516387A JP 2017516387 A JP2017516387 A JP 2017516387A JP 2017528507 A5 JP2017528507 A5 JP 2017528507A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- pharmaceutical composition
- pharmaceutically acceptable
- naphthyridin
- 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
- 150000001875 compounds Chemical class 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 239000013543 active substance Substances 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 3
- 230000003176 fibrotic effect Effects 0.000 claims 3
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- MKIJZIVRJUMEAD-AMGIVPHBSA-N COCCOC1=CC=CC(=C1)[C@@H](CN1CC[C@@](F)(CCC2=CC=C3CCCNC3=N2)C1)CC(O)=O Chemical compound COCCOC1=CC=CC(=C1)[C@@H](CN1CC[C@@](F)(CCC2=CC=C3CCCNC3=N2)C1)CC(O)=O MKIJZIVRJUMEAD-AMGIVPHBSA-N 0.000 claims 2
- 230000008485 antagonism Effects 0.000 claims 2
- 230000009286 beneficial effect Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- MKIJZIVRJUMEAD-WXVAWEFUSA-N (3R)-4-[(3R)-3-fluoro-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]-3-[3-(2-methoxyethoxy)phenyl]butanoic acid Chemical compound F[C@]1(CN(CC1)C[C@H](CC(=O)O)C1=CC(=CC=C1)OCCOC)CCC1=NC=2NCCCC=2C=C1 MKIJZIVRJUMEAD-WXVAWEFUSA-N 0.000 claims 1
- MKIJZIVRJUMEAD-AJTFRIOCSA-N (3S)-4-[(3R)-3-fluoro-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]-3-[3-(2-methoxyethoxy)phenyl]butanoic acid Chemical compound F[C@]1(CN(CC1)C[C@@H](CC(=O)O)C1=CC(=CC=C1)OCCOC)CCC1=NC=2NCCCC=2C=C1 MKIJZIVRJUMEAD-AJTFRIOCSA-N 0.000 claims 1
- -1 3- (3- (2-methoxyethoxy) phenyl) butanoic acid maleate Chemical compound 0.000 claims 1
- MKIJZIVRJUMEAD-UHFFFAOYSA-N COCCOC1=CC=CC(=C1)C(CN1CCC(F)(CCC2=CC=C3CCCNC3=N2)C1)CC(O)=O Chemical compound COCCOC1=CC=CC(=C1)C(CN1CCC(F)(CCC2=CC=C3CCCNC3=N2)C1)CC(O)=O MKIJZIVRJUMEAD-UHFFFAOYSA-N 0.000 claims 1
- MKIJZIVRJUMEAD-CUNXSJBXSA-N COCCOC1=CC=CC(=C1)[C@H](CN1CC[C@@](F)(CCC2=CC=C3CCCNC3=N2)C1)CC(O)=O Chemical compound COCCOC1=CC=CC(=C1)[C@H](CN1CC[C@@](F)(CCC2=CC=C3CCCNC3=N2)C1)CC(O)=O MKIJZIVRJUMEAD-CUNXSJBXSA-N 0.000 claims 1
- 102000004887 Transforming Growth Factor beta Human genes 0.000 claims 1
- 108090001012 Transforming Growth Factor beta Proteins 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- CPMDPSXJELVGJG-UHFFFAOYSA-N methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate Chemical group OC=1NC2=CC(=CC=C2C=1C(=NC1=CC=C(C=C1)N(C(CN1CCN(CC1)C)=O)C)C1=CC=CC=C1)C(=O)OC CPMDPSXJELVGJG-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- ISWRGOKTTBVCFA-UHFFFAOYSA-N pirfenidone Chemical group C1=C(C)C=CC(=O)N1C1=CC=CC=C1 ISWRGOKTTBVCFA-UHFFFAOYSA-N 0.000 claims 1
- 229960003073 pirfenidone Drugs 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1417002.1A GB201417002D0 (en) | 2014-09-26 | 2014-09-26 | Novel compound |
| GB1417002.1 | 2014-09-26 | ||
| PCT/EP2015/071776 WO2016046225A1 (en) | 2014-09-26 | 2015-09-22 | Novel compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017528507A JP2017528507A (ja) | 2017-09-28 |
| JP2017528507A5 true JP2017528507A5 (https=) | 2018-01-25 |
| JP6611799B2 JP6611799B2 (ja) | 2019-11-27 |
Family
ID=51901158
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017516387A Expired - Fee Related JP6611799B2 (ja) | 2014-09-26 | 2015-09-22 | 新規化合物 |
Country Status (37)
Families Citing this family (27)
| 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 |
| GB201417002D0 (en) * | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201417018D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| 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 |
| WO2018089357A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | INDAZOLE DERIVATIVES AS αV INTEGRIN ANTAGONISTS |
| HRP20210228T1 (hr) * | 2016-11-08 | 2021-03-19 | Bristol-Myers Squibb Company | Amidi pirola kao inhibitori alfa v integrina |
| 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 |
| BR112019009245A2 (pt) | 2016-11-08 | 2019-07-16 | Bristol-Myers Squibb Company | azol amidas e aminas como inibidores de alfav integrina |
| AU2017359023B2 (en) | 2016-11-08 | 2021-12-09 | Bristol-Myers Squibb Company | 3-substituted propionic acids as alpha v integrin inhibitors |
| US10696672B2 (en) | 2016-12-23 | 2020-06-30 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| MX394210B (es) | 2017-02-28 | 2025-03-04 | Morphic Therapeutic Inc | INHIBIDORES DE INTEGRINA AVß6. |
| MA52117A (fr) | 2017-02-28 | 2022-04-06 | Morphic Therapeutic Inc | Inhibiteurs de l'intégrine (alpha-v) (bêta-6) |
| US11332498B2 (en) | 2017-03-17 | 2022-05-17 | Technische Universitat Munchen | Ligands for integrin αVβ8, synthesis and uses thereof |
| KR102700471B1 (ko) | 2017-11-07 | 2024-08-28 | 브리스톨-마이어스 스큅 컴퍼니 | 알파 v 인테그린 억제제로서의 피롤로피라진 유도체 |
| CN108208177A (zh) * | 2017-11-28 | 2018-06-29 | 上海交通大学医学院附属新华医院 | 含丁酸类化合物的组合物及其应用 |
| WO2020047207A1 (en) * | 2018-08-29 | 2020-03-05 | Morphic Therapeutics, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| WO2020047208A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| WO2020047239A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | INHIBITING αV β6 INTEGRIN |
| SI3844162T1 (sl) * | 2018-08-29 | 2025-06-30 | Morphic Therapeutic, Inc. | Zaviralci integrina alfa v beta6 |
| US20240165195A1 (en) * | 2018-10-09 | 2024-05-23 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of alpha-v-integrin (cd51) inhibitors for the treatment of cardiac fibrosis |
| JP2022512648A (ja) * | 2018-10-09 | 2022-02-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 心筋線維化の処置のためのαＶ－インテグリン（ＣＤ５１）阻害剤の使用 |
| US11034710B2 (en) * | 2018-12-04 | 2021-06-15 | Sumitomo Dainippon Pharma Oncology, Inc. | CDK9 inhibitors and polymorphs thereof for use as agents for treatment of cancer |
| GB202010626D0 (en) | 2020-07-10 | 2020-08-26 | Univ Nottingham | Compound |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20010033248A (ko) | 1997-12-17 | 2001-04-25 | 폴락 돈나 엘. | 인테그린 수용체 길항제 |
| CA2315370A1 (en) | 1997-12-17 | 1999-06-24 | Merck & Co., Inc. | Integrin receptor antagonists |
| CN1589145A (zh) | 1999-06-02 | 2005-03-02 | 麦克公司 | αv整联蛋白受体拮抗剂 |
| WO2000078317A1 (en) | 1999-06-23 | 2000-12-28 | Merck & Co., Inc. | Integrin receptor antagonists |
| EP1229910A4 (en) * | 1999-10-04 | 2003-10-01 | Merck & Co Inc | integrin |
| PL355011A1 (en) | 1999-11-08 | 2004-03-22 | Merck & Co, Inc. | Process and intermediates for the preparation of imidazolidinone alpha v integrin antagonists |
| US6921767B2 (en) | 2000-06-15 | 2005-07-26 | Pharmacia Corporation | Cycloalkyl alkanoic acids as integrin receptor antagonists derivatives |
| US7119098B2 (en) * | 2000-06-15 | 2006-10-10 | Pharmacia Corporation | Heteroarylakanoic acids as intergrin receptor antagonists |
| AU7793501A (en) | 2000-07-26 | 2002-02-05 | Merck & Co Inc | Alpha v integrin receptor antagonists |
| WO2002022616A2 (en) | 2000-09-14 | 2002-03-21 | Merck & Co., Inc. | Alpha v integrin receptor antagonists |
| CA2432504A1 (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 |
| NZ535425A (en) | 2002-03-13 | 2008-05-30 | Biogen Idec Inc | Anti-alphavbeta6 antibodies |
| US20040224986A1 (en) * | 2002-08-16 | 2004-11-11 | Bart De Corte | Piperidinyl targeting compounds that selectively bind integrins |
| EP1592421A1 (en) | 2002-12-20 | 2005-11-09 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| US6932865B2 (en) | 2003-04-11 | 2005-08-23 | Lockheed Martin Corporation | System and method of making single-crystal structures through free-form fabrication techniques |
| EP2139882B1 (en) | 2007-03-23 | 2013-12-25 | Amgen Inc. | 3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
| US8563566B2 (en) | 2007-08-01 | 2013-10-22 | Valeant Pharmaceuticals International | Naphthyridine derivatives as potassium channel modulators |
| EP2211615A4 (en) | 2007-10-22 | 2010-10-13 | Glaxosmithkline Llc | PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS |
| 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 |
| GB201417018D0 (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 |
| GB201417002D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201417094D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US9790222B2 (en) | 2015-02-19 | 2017-10-17 | Scifluor Life Sciences, Inc. | Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof |
| WO2016145258A1 (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 |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
-
2014
- 2014-09-26 GB GBGB1417002.1A patent/GB201417002D0/en not_active Ceased
-
2015
- 2015-09-22 LT LTEP15767475.5T patent/LT3197892T/lt unknown
- 2015-09-22 EA EA201790715A patent/EA031481B1/ru not_active IP Right Cessation
- 2015-09-22 CR CR20170112A patent/CR20170112A/es unknown
- 2015-09-22 PT PT15767475T patent/PT3197892T/pt unknown
- 2015-09-22 HU HUE15767475A patent/HUE041827T2/hu unknown
- 2015-09-22 PL PL15767475T patent/PL3197892T3/pl unknown
- 2015-09-22 ES ES15767475.5T patent/ES2690748T3/es active Active
- 2015-09-22 WO PCT/EP2015/071776 patent/WO2016046225A1/en not_active Ceased
- 2015-09-22 CN CN201580050280.XA patent/CN107074848B/zh not_active Expired - Fee Related
- 2015-09-22 EP EP15767475.5A patent/EP3197892B1/en active Active
- 2015-09-22 SM SM20180513T patent/SMT201800513T1/it unknown
- 2015-09-22 RS RS20181417A patent/RS58000B1/sr unknown
- 2015-09-22 MX MX2017003948A patent/MX2017003948A/es unknown
- 2015-09-22 BR BR112017006251A patent/BR112017006251A2/pt not_active Application Discontinuation
- 2015-09-22 UA UAA201703900A patent/UA119181C2/uk unknown
- 2015-09-22 JO JOP/2015/0234A patent/JO3413B1/ar active
- 2015-09-22 PE PE2017000380A patent/PE20170502A1/es unknown
- 2015-09-22 SG SG11201701183YA patent/SG11201701183YA/en unknown
- 2015-09-22 AU AU2015320858A patent/AU2015320858B2/en not_active Ceased
- 2015-09-22 KR KR1020177007738A patent/KR101998000B1/ko not_active Expired - Fee Related
- 2015-09-22 AR ARP150103047A patent/AR101994A1/es unknown
- 2015-09-22 UY UY0001036314A patent/UY36314A/es not_active Application Discontinuation
- 2015-09-22 EP EP18191644.6A patent/EP3428167A1/en not_active Withdrawn
- 2015-09-22 CA CA2962315A patent/CA2962315A1/en not_active Abandoned
- 2015-09-22 DK DK15767475.5T patent/DK3197892T3/en active
- 2015-09-22 JP JP2017516387A patent/JP6611799B2/ja not_active Expired - Fee Related
- 2015-09-22 TW TW104131366A patent/TW201629056A/zh unknown
- 2015-09-22 SI SI201530476T patent/SI3197892T1/sl unknown
- 2015-09-22 HR HRP20181796TT patent/HRP20181796T1/hr unknown
- 2015-09-22 MA MA40580A patent/MA40580B1/fr unknown
- 2015-09-22 US US15/514,399 patent/US9956209B2/en not_active Expired - Fee Related
-
2017
- 2017-02-14 IL IL250592A patent/IL250592A0/en unknown
- 2017-02-28 PH PH12017500361A patent/PH12017500361B1/en unknown
- 2017-03-22 CO CONC2017/0002714A patent/CO2017002714A2/es unknown
- 2017-03-23 CL CL2017000705A patent/CL2017000705A1/es unknown
- 2017-03-23 DO DO2017000081A patent/DOP2017000081A/es unknown
-
2018
- 2018-03-15 US US15/922,674 patent/US10342783B2/en not_active Expired - Fee Related
- 2018-11-27 CY CY181101259T patent/CY1121071T1/el unknown
-
2019
- 2019-05-28 US US16/423,455 patent/US20190275016A1/en not_active Abandoned
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