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 |
|---|---|---|---|
| GB1417002.1 | 2014-09-26 | ||
| GBGB1417002.1A GB201417002D0 (en) | 2014-09-26 | 2014-09-26 | Novel compound |
| 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 (enExample) | 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 |
| GB201417018D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| 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 |
| 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 |
| ES2898835T3 (es) | 2016-11-08 | 2022-03-09 | Bristol Myers Squibb Co | Azol amidas y aminas como inhibidores de la integrina alfav |
| 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 |
| AU2017359030A1 (en) | 2016-11-08 | 2019-06-20 | Bristol-Myers Squibb Company | Pyrrole amides as alpha v integrin inhibitors |
| 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 |
| EA201991123A1 (ru) | 2016-11-08 | 2019-11-29 | ИНДАЗОЛОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ АНТАГОНИСТОВ ИНТЕГРИНА αV | |
| USRE50554E1 (en) | 2016-12-23 | 2025-08-26 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| SG11201907820SA (en) | 2017-02-28 | 2019-09-27 | Morphic Therapeutic Inc | Inhibitors of (alpha-v)(beta-6) integrin |
| US11046685B2 (en) | 2017-02-28 | 2021-06-29 | Morphic Therapeutic, Inc. | Inhibitors of (α-v)(β-6) integrin |
| US11332498B2 (en) | 2017-03-17 | 2022-05-17 | Technische Universitat Munchen | Ligands for integrin αVβ8, synthesis and uses thereof |
| US11292802B2 (en) | 2017-11-07 | 2022-04-05 | Bristol-Myers Squibb Company | Substituted tetrahydropyrrolo[1,2-a]pyrazines as alpha v integrin inhibitors |
| 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 |
| ES3027421T3 (en) * | 2018-08-29 | 2025-06-13 | Morphic Therapeutic Inc | Inhibitors of (alpha-v)(beta-6) integrin |
| 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 |
| 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 |
| WO2020074937A1 (en) * | 2018-10-09 | 2020-04-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of alpha-v-integrin (cd51) inhibitors for the treatment of cardiac fibrosis |
| JP2022511029A (ja) * | 2018-12-04 | 2022-01-28 | スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド | がんの処置のための薬剤としての使用のためのｃｄｋ９インヒビターおよびその多形 |
| GB202010626D0 (en) | 2020-07-10 | 2020-08-26 | Univ Nottingham | Compound |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999031061A1 (en) | 1997-12-17 | 1999-06-24 | Merck & Co., Inc. | Integrin receptor antagonists |
| AU736026B2 (en) | 1997-12-17 | 2001-07-26 | 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 |
| US6921767B2 (en) | 2000-06-15 | 2005-07-26 | Pharmacia Corporation | Cycloalkyl alkanoic acids as integrin receptor antagonists derivatives |
| 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 |
| CN1646160A (zh) | 2002-03-13 | 2005-07-27 | 拜奥根Idec马萨诸塞公司 | 抗αvβ6抗体 |
| 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 |
| 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 |
| 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 |
| 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 |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
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2014
- 2014-09-26 GB GBGB1417002.1A patent/GB201417002D0/en not_active Ceased
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2015
- 2015-09-22 TW TW104131366A patent/TW201629056A/zh unknown
- 2015-09-22 HR HRP20181796TT patent/HRP20181796T1/hr unknown
- 2015-09-22 SM SM20180513T patent/SMT201800513T1/it unknown
- 2015-09-22 MA MA40580A patent/MA40580B1/fr unknown
- 2015-09-22 PE PE2017000380A patent/PE20170502A1/es unknown
- 2015-09-22 EP EP15767475.5A patent/EP3197892B1/en active Active
- 2015-09-22 JP JP2017516387A patent/JP6611799B2/ja not_active Expired - Fee Related
- 2015-09-22 SI SI201530476T patent/SI3197892T1/sl unknown
- 2015-09-22 EP EP18191644.6A patent/EP3428167A1/en not_active Withdrawn
- 2015-09-22 CR CR20170112A patent/CR20170112A/es unknown
- 2015-09-22 HU HUE15767475A patent/HUE041827T2/hu unknown
- 2015-09-22 CN CN201580050280.XA patent/CN107074848B/zh not_active Expired - Fee Related
- 2015-09-22 LT LTEP15767475.5T patent/LT3197892T/lt unknown
- 2015-09-22 US US15/514,399 patent/US9956209B2/en not_active Expired - Fee Related
- 2015-09-22 MX MX2017003948A patent/MX2017003948A/es unknown
- 2015-09-22 BR BR112017006251A patent/BR112017006251A2/pt not_active Application Discontinuation
- 2015-09-22 CA CA2962315A patent/CA2962315A1/en not_active Abandoned
- 2015-09-22 JO JOP/2015/0234A patent/JO3413B1/ar active
- 2015-09-22 UA UAA201703900A patent/UA119181C2/uk unknown
- 2015-09-22 RS RS20181417A patent/RS58000B1/sr unknown
- 2015-09-22 PL PL15767475T patent/PL3197892T3/pl unknown
- 2015-09-22 WO PCT/EP2015/071776 patent/WO2016046225A1/en not_active Ceased
- 2015-09-22 PT PT15767475T patent/PT3197892T/pt unknown
- 2015-09-22 ES ES15767475.5T patent/ES2690748T3/es active Active
- 2015-09-22 SG SG11201701183YA patent/SG11201701183YA/en unknown
- 2015-09-22 KR KR1020177007738A patent/KR101998000B1/ko not_active Expired - Fee Related
- 2015-09-22 DK DK15767475.5T patent/DK3197892T3/en active
- 2015-09-22 UY UY0001036314A patent/UY36314A/es not_active Application Discontinuation
- 2015-09-22 AR ARP150103047A patent/AR101994A1/es unknown
- 2015-09-22 EA EA201790715A patent/EA031481B1/ru not_active IP Right Cessation
- 2015-09-22 AU AU2015320858A patent/AU2015320858B2/en not_active Ceased
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2017
- 2017-02-14 IL IL250592A patent/IL250592A0/en unknown
- 2017-02-28 PH PH12017500361A patent/PH12017500361A1/en unknown
- 2017-03-22 CO CONC2017/0002714A patent/CO2017002714A2/es unknown
- 2017-03-23 DO DO2017000081A patent/DOP2017000081A/es unknown
- 2017-03-23 CL CL2017000705A patent/CL2017000705A1/es unknown
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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
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2019
- 2019-05-28 US US16/423,455 patent/US20190275016A1/en not_active Abandoned