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 (cg-RX-API-DMAC10.html) | 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 (26)
| 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 |
| GB201417002D0 (en) * | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201417011D0 (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 |
| 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 |
| GB201604681D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| MA46745A (fr) | 2016-11-08 | 2021-03-31 | Bristol Myers Squibb Co | Dérivés d'indazole en tant qu'antagonistes de l'intégrine alpha v |
| BR112019009293A2 (pt) | 2016-11-08 | 2019-07-30 | Bristol-Myers Squibb Company | pirrol amidas como inibidores de integrina alfa v |
| MX377359B (es) | 2016-11-08 | 2025-03-10 | Bristol Myers Squibb Co | Compuestos mono y espirocíclicos que continen ciclobutano y azetidina como inhibidores de la integrina alfa v. |
| NZ754207A (en) | 2016-11-08 | 2025-09-26 | Bristol Myers Squibb Co | 3-substituted propionic acids as alpha v integrin inhibitors |
| EP3538527B1 (en) | 2016-11-08 | 2021-10-13 | Bristol-Myers Squibb Company | Azole amides and amines as alpha v integrin inhibitors |
| USRE50554E1 (en) | 2016-12-23 | 2025-08-26 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| KR102891803B1 (ko) | 2017-02-28 | 2025-11-28 | 모픽 테라퓨틱, 인코포레이티드 | αvβ6 인테그린 억제제 |
| EP3760202A1 (en) | 2017-02-28 | 2021-01-06 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| WO2018167295A1 (en) * | 2017-03-17 | 2018-09-20 | Technische Universität München | LIGANDS FOR INTEGRIN αvβ8, SYNTHESIS AND USES THEREOF |
| BR112020008893A2 (pt) | 2017-11-07 | 2020-10-13 | Bristol-Myers Squibb Company | derivados de pirrolopirazina como inibidores de alfa v integrina |
| 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 |
| EP3843727A4 (en) * | 2018-08-29 | 2022-08-17 | Morphic Therapeutic, Inc. | INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN |
| UY38352A (es) | 2018-08-29 | 2020-03-31 | Morphic Therapeutic Inc | Inhibidores de integrina alfavbeta6 |
| JP7540998B2 (ja) | 2018-08-29 | 2024-08-27 | モーフィック セラピューティック，インコーポレイテッド | αｖβ６インテグリンの阻害 |
| ES3027421T3 (en) * | 2018-08-29 | 2025-06-13 | Morphic Therapeutic Inc | Inhibitors of (alpha-v)(beta-6) integrin |
| US12351634B2 (en) * | 2018-10-09 | 2025-07-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of cilengitide for ameliorating cardiac fibrosis occurring in response to myocardial infarction |
| 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 |
|---|---|---|---|---|
| AU736026B2 (en) | 1997-12-17 | 2001-07-26 | Merck & Co., Inc. | Integrin receptor antagonists |
| ATE294163T1 (de) | 1997-12-17 | 2005-05-15 | Merck & Co Inc | Integrin-rezeptor-antagonisten |
| DE60035779T2 (de) | 1999-06-02 | 2008-04-30 | Merck & Co., Inc. | Alpha v integrin-rezeptor antagonisten |
| EP1194151A4 (en) | 1999-06-23 | 2003-01-15 | Merck & Co Inc | ANTAGONISTS OF THE INTEGRIN RECEPTORS |
| AU7743400A (en) * | 1999-10-04 | 2001-05-10 | Merck & Co., Inc. | Integrin receptor antagonists |
| YU32502A (sh) | 1999-11-08 | 2004-12-31 | Merck & Co.Inc. | Postupak i intermedijeri za proizvodnju imidazolidinonskih antagonista alfa v integrina |
| 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 |
| ATE353219T1 (de) | 2000-07-26 | 2007-02-15 | Merck & Co Inc | Alpha v integrin-rezeptor-antagonisten |
| WO2002022616A2 (en) | 2000-09-14 | 2002-03-21 | Merck & Co., Inc. | Alpha v integrin receptor antagonists |
| JP2004517853A (ja) | 2001-01-03 | 2004-06-17 | メルク エンド カムパニー インコーポレーテッド | 歯周病の治療方法及び治療用組成物 |
| 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 |
| BRPI0308585B8 (pt) | 2002-03-13 | 2021-05-25 | Biogen Idec Inc | anticorpo isolado ou fragmento de ligação a antígeno do mesmo que se liga à alfavbeta6, composição, método de detecção in vitro de alfavbeta6 e construção de dna |
| 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 |
| JP5732701B2 (ja) | 2007-03-23 | 2015-06-10 | アムジエン・インコーポレーテツド | ３−置換キノリンまたはキノキサリン誘導体およびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害剤としてのそれらの使用 |
| 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 |
| GB201417011D0 (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 |
| 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 |
| ES2892954T3 (es) | 2015-02-19 | 2022-02-07 | Ocuterra Therapeutics Inc | Derivados fluorados del ácido 3-(2-oxo-3-(3-(5,6,7,8-tetrahidro-1,8-naftiridin-2-il)propil)imidazolidin-1-il)propanoico y usos de los mismos |
| 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 |
-
2014
- 2014-09-26 GB GBGB1417002.1A patent/GB201417002D0/en not_active Ceased
-
2015
- 2015-09-22 DK DK15767475.5T patent/DK3197892T3/en active
- 2015-09-22 EP EP18191644.6A patent/EP3428167A1/en not_active Withdrawn
- 2015-09-22 CR CR20170112A patent/CR20170112A/es unknown
- 2015-09-22 PE PE2017000380A patent/PE20170502A1/es unknown
- 2015-09-22 CN CN201580050280.XA patent/CN107074848B/zh not_active Expired - Fee Related
- 2015-09-22 CA CA2962315A patent/CA2962315A1/en not_active Abandoned
- 2015-09-22 ES ES15767475.5T patent/ES2690748T3/es active Active
- 2015-09-22 PT PT15767475T patent/PT3197892T/pt unknown
- 2015-09-22 MA MA40580A patent/MA40580B1/fr unknown
- 2015-09-22 RS RS20181417A patent/RS58000B1/sr unknown
- 2015-09-22 MX MX2017003948A patent/MX2017003948A/es unknown
- 2015-09-22 LT LTEP15767475.5T patent/LT3197892T/lt unknown
- 2015-09-22 PL PL15767475T patent/PL3197892T3/pl unknown
- 2015-09-22 HR HRP20181796TT patent/HRP20181796T1/hr unknown
- 2015-09-22 KR KR1020177007738A patent/KR101998000B1/ko not_active Expired - Fee Related
- 2015-09-22 US US15/514,399 patent/US9956209B2/en not_active Expired - Fee Related
- 2015-09-22 JP JP2017516387A patent/JP6611799B2/ja not_active Expired - Fee Related
- 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 HU HUE15767475A patent/HUE041827T2/hu unknown
- 2015-09-22 UA UAA201703900A patent/UA119181C2/uk unknown
- 2015-09-22 TW TW104131366A patent/TW201629056A/zh unknown
- 2015-09-22 BR BR112017006251A patent/BR112017006251A2/pt not_active Application Discontinuation
- 2015-09-22 SI SI201530476T patent/SI3197892T1/sl unknown
- 2015-09-22 JO JOP/2015/0234A patent/JO3413B1/ar active
- 2015-09-22 EP EP15767475.5A patent/EP3197892B1/en active Active
- 2015-09-22 WO PCT/EP2015/071776 patent/WO2016046225A1/en not_active Ceased
- 2015-09-22 AU AU2015320858A patent/AU2015320858B2/en not_active Ceased
- 2015-09-22 SM SM20180513T patent/SMT201800513T1/it unknown
- 2015-09-22 UY UY0001036314A patent/UY36314A/es not_active Application Discontinuation
- 2015-09-22 SG SG11201701183YA patent/SG11201701183YA/en unknown
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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 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