JP2017528506A5 - - Google Patents
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- Publication number
- JP2017528506A5 JP2017528506A5 JP2017516386A JP2017516386A JP2017528506A5 JP 2017528506 A5 JP2017528506 A5 JP 2017528506A5 JP 2017516386 A JP2017516386 A JP 2017516386A JP 2017516386 A JP2017516386 A JP 2017516386A JP 2017528506 A5 JP2017528506 A5 JP 2017528506A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- tetrahydro
- ethyl
- butanoic acid
- 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 14
- 150000003839 salts Chemical class 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- QESJLCKQPIPWOH-RXVAYIKUSA-N 3-[3-(3,5-dimethylpyrazol-1-yl)-5-morpholin-4-ylphenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid Chemical compound CC1=NN(C(=C1)C)C=1C=C(C=C(C=1)N1CCOCC1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 QESJLCKQPIPWOH-RXVAYIKUSA-N 0.000 claims 3
- 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
- 230000002265 prevention Effects 0.000 claims 3
- NIVBRIPUAQCFIE-CILPGNKCSA-N 3-(3-morpholin-4-ylphenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid Chemical compound O1CCN(CC1)C=1C=C(C=CC=1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 NIVBRIPUAQCFIE-CILPGNKCSA-N 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 230000004060 metabolic process Effects 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- NIVBRIPUAQCFIE-QPPBQGQZSA-N (3R)-3-(3-morpholin-4-ylphenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid Chemical compound O1CCN(CC1)C=1C=C(C=CC=1)[C@@H](CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 NIVBRIPUAQCFIE-QPPBQGQZSA-N 0.000 claims 1
- SDXAWLJRERMRKF-UHFFFAOYSA-N 3,5-dimethyl-1h-pyrazole Chemical group CC=1C=C(C)NN=1 SDXAWLJRERMRKF-UHFFFAOYSA-N 0.000 claims 1
- DSIZWMBDZKYEIX-GEPVFLLWSA-N 3-(3-morpholin-4-yl-5-pyrazol-1-ylphenyl)-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid Chemical compound O1CCN(CC1)C=1C=C(C=C(C=1)N1N=CC=C1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 DSIZWMBDZKYEIX-GEPVFLLWSA-N 0.000 claims 1
- ZDOSPEWESKOOOH-DXDQHDRFSA-N 3-[3-(3-methylpyrazol-1-yl)-5-morpholin-4-ylphenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid Chemical compound CC1=NN(C=C1)C=1C=C(C=C(C=1)N1CCOCC1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 ZDOSPEWESKOOOH-DXDQHDRFSA-N 0.000 claims 1
- HSFMXGFHWOJUJH-BRIWLPCBSA-N 3-[3-(5-methyl-1H-pyrazol-3-yl)-5-morpholin-4-ylphenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid Chemical compound CC1=NNC(=C1)C=1C=C(C=C(C=1)N1CCOCC1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 HSFMXGFHWOJUJH-BRIWLPCBSA-N 0.000 claims 1
- ZDRHQMNDLFXLFL-FPSALIRRSA-N 3-[3-morpholin-4-yl-5-(1H-pyrazol-4-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid Chemical compound O1CCN(CC1)C=1C=C(C=C(C=1)C=1C=NNC=1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 ZDRHQMNDLFXLFL-FPSALIRRSA-N 0.000 claims 1
- QEIWHNLFOUGMMS-FPSALIRRSA-N 3-[3-morpholin-4-yl-5-(1H-pyrazol-5-yl)phenyl]-4-[(3R)-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]pyrrolidin-1-yl]butanoic acid Chemical compound O1CCN(CC1)C=1C=C(C=C(C=1)C1=CC=NN1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 QEIWHNLFOUGMMS-FPSALIRRSA-N 0.000 claims 1
- XKVUYEYANWFIJX-UHFFFAOYSA-N 5-methyl-1h-pyrazole Chemical group CC1=CC=NN1 XKVUYEYANWFIJX-UHFFFAOYSA-N 0.000 claims 1
- OGWLKQKCWNAXLA-XVPAFAEQSA-N C1(CC1)C=1C=C(C=C(C=1)N1CCOCC1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 Chemical compound C1(CC1)C=1C=C(C=C(C=1)N1CCOCC1)C(CC(=O)O)CN1C[C@@H](CC1)CCC1=NC=2NCCCC=2C=C1 OGWLKQKCWNAXLA-XVPAFAEQSA-N 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 229940123038 Integrin antagonist Drugs 0.000 claims 1
- NIVBRIPUAQCFIE-ZJSXRUAMSA-N OC(=O)C[C@H](CN1CC[C@@H](CCC2=CC=C3CCCNC3=N2)C1)C1=CC(=CC=C1)N1CCOCC1 Chemical compound OC(=O)C[C@H](CN1CC[C@@H](CCC2=CC=C3CCCNC3=N2)C1)C1=CC(=CC=C1)N1CCOCC1 NIVBRIPUAQCFIE-ZJSXRUAMSA-N 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- -1 amino compound Chemical class 0.000 claims 1
- 230000008485 antagonism Effects 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000003176 fibrotic effect Effects 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
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1417018.7 | 2014-09-26 | ||
| GBGB1417018.7A GB201417018D0 (en) | 2014-09-26 | 2014-09-26 | Novel compounds |
| PCT/EP2015/071798 WO2016046241A1 (en) | 2014-09-26 | 2015-09-22 | Novel compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017528506A JP2017528506A (ja) | 2017-09-28 |
| JP2017528506A5 true JP2017528506A5 (enExample) | 2018-10-25 |
| JP6672276B2 JP6672276B2 (ja) | 2020-03-25 |
Family
ID=51901174
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017516386A Expired - Fee Related JP6672276B2 (ja) | 2014-09-26 | 2015-09-22 | 新規化合物 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10004724B2 (enExample) |
| EP (1) | EP3197895B1 (enExample) |
| JP (1) | JP6672276B2 (enExample) |
| KR (1) | KR20170054413A (enExample) |
| CN (1) | CN107074850A (enExample) |
| AU (1) | AU2015320874A1 (enExample) |
| BR (1) | BR112017006240A2 (enExample) |
| CA (1) | CA2962319A1 (enExample) |
| ES (1) | ES2796235T3 (enExample) |
| GB (1) | GB201417018D0 (enExample) |
| RU (1) | RU2017114352A (enExample) |
| WO (1) | WO2016046241A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201305668D0 (en) | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| 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 |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| CA3042714A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Indazole derivatives as a .alpha.v integrin antagonists |
| BR112019009245A2 (pt) | 2016-11-08 | 2019-07-16 | Bristol-Myers Squibb Company | azol amidas e aminas como inibidores de alfav integrina |
| HRP20210228T1 (hr) | 2016-11-08 | 2021-03-19 | Bristol-Myers Squibb Company | Amidi pirola kao inhibitori alfa v integrina |
| WO2018089355A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Cyclobutane- and azetidine-containing mono and spirocyclic compounds as alpha v integrin inhibitors |
| WO2018089353A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | 3-substituted propionic acids as alpha v integrin inhibitors |
| USRE50554E1 (en) | 2016-12-23 | 2025-08-26 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| EP4147698A1 (en) | 2017-02-28 | 2023-03-15 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| US20180244648A1 (en) | 2017-02-28 | 2018-08-30 | Lazuli, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| WO2019094319A1 (en) | 2017-11-07 | 2019-05-16 | Bristol-Myers Squibb Company | Pyrrolopyrazine derivatives as alpha v integrin inhibitors |
| CR20210109A (es) | 2018-08-29 | 2021-06-24 | Morphic Therapeutic Inc | INHIBICIÓN DE LA INTEGRINA av ß6 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2241192T3 (es) | 1997-12-17 | 2005-10-16 | MERCK & CO., INC. (A NEW JERSEY CORP.) | Antagonistas del receptor de integrina. |
| EP1047425A4 (en) * | 1997-12-17 | 2009-04-22 | 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 |
| AU748949B2 (en) | 1999-06-23 | 2002-06-13 | Merck & Co., Inc. | Integrin receptor antagonists |
| AU7743400A (en) * | 1999-10-04 | 2001-05-10 | Merck & Co., Inc. | Integrin receptor antagonists |
| IL149313A0 (en) | 1999-11-08 | 2002-11-10 | Merck & Co Inc | Process and intermediates for the preparation of imidazolidinone alpha v integrin antagonists |
| WO2001096334A2 (en) | 2000-06-15 | 2001-12-20 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| CA2416751A1 (en) | 2000-07-26 | 2002-01-31 | Merck & Co., Inc. | Alpha v integrin receptor antagonists |
| 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¶ |
| US20040224986A1 (en) * | 2002-08-16 | 2004-11-11 | Bart De Corte | Piperidinyl targeting compounds that selectively bind integrins |
| CA2507699A1 (en) | 2002-12-20 | 2004-07-15 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| PT2139882E (pt) | 2007-03-23 | 2014-01-30 | Amgen Inc | Derivados de quinolina ou quinoxalina 3-substituídos e sua utilização como inibidores de fosfatidilinositol 3-cinase (pi3k) |
| 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 |
| 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 |
| JP2018510139A (ja) | 2015-02-19 | 2018-04-12 | サイフルーア ライフ サイエンシズ インコーポレイテッド | フッ化テトラヒドロナフチリジニルノナン酸誘導体およびその使用法 |
| EP3268369A4 (en) | 2015-03-10 | 2018-08-08 | 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 GBGB1417018.7A patent/GB201417018D0/en not_active Ceased
-
2015
- 2015-09-22 ES ES15767479T patent/ES2796235T3/es active Active
- 2015-09-22 RU RU2017114352A patent/RU2017114352A/ru unknown
- 2015-09-22 BR BR112017006240A patent/BR112017006240A2/pt not_active Application Discontinuation
- 2015-09-22 CN CN201580052202.3A patent/CN107074850A/zh active Pending
- 2015-09-22 EP EP15767479.7A patent/EP3197895B1/en active Active
- 2015-09-22 KR KR1020177007735A patent/KR20170054413A/ko not_active Withdrawn
- 2015-09-22 US US15/514,414 patent/US10004724B2/en not_active Expired - Fee Related
- 2015-09-22 AU AU2015320874A patent/AU2015320874A1/en not_active Abandoned
- 2015-09-22 CA CA2962319A patent/CA2962319A1/en active Pending
- 2015-09-22 JP JP2017516386A patent/JP6672276B2/ja not_active Expired - Fee Related
- 2015-09-22 WO PCT/EP2015/071798 patent/WO2016046241A1/en not_active Ceased
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