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 (16)
| 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 |
| 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 |
| GB201604680D0 (en) | 2016-03-21 | 2016-05-04 | Glaxosmithkline Ip Dev Ltd | Chemical Compounds |
| SMT202100089T1 (it) | 2016-11-08 | 2021-03-15 | Bristol Myers Squibb Co | Pirrol ammidi come inibitori delle integrine alfa v |
| EA201991121A1 (ru) | 2016-11-08 | 2019-11-29 | АЗОЛАМИДЫ И АЗОЛАМИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ИНТЕГРИНОВ αV | |
| CA3042710A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Cyclobutane- and azetidine-containing mono and spirocyclic compounds as .alpha.v integrin inhibitors |
| CN110214137A (zh) | 2016-11-08 | 2019-09-06 | 百时美施贵宝公司 | 作为αv整联蛋白拮抗剂的吲唑衍生物 |
| RS63483B1 (sr) | 2016-11-08 | 2022-09-30 | Bristol Myers Squibb Co | 3-supstituisane propionske kiseline kao inhibitori alfa v integrina |
| USRE50554E1 (en) | 2016-12-23 | 2025-08-26 | Pliant Therapeutics, Inc. | Amino acid compounds and methods of use |
| AU2018229275B2 (en) | 2017-02-28 | 2021-12-23 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| MA52117A (fr) | 2017-02-28 | 2022-04-06 | Morphic Therapeutic Inc | Inhibiteurs de l'intégrine (alpha-v) (bêta-6) |
| ES2904645T3 (es) | 2017-11-07 | 2022-04-05 | Bristol Myers Squibb Co | Derivados de pirrolopirazina como inhibidores de integrina alfa v |
| CA3109534A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibiting .alpha.v .beta.6 integrin |
| WO2020081154A1 (en) | 2018-08-29 | 2020-04-23 | Morphic Therapeutic, Inc. | INHIBITORS OF ανβ6 INTEGRIN |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002508323A (ja) * | 1997-12-17 | 2002-03-19 | 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 |
| DE69829996T2 (de) | 1997-12-17 | 2006-02-23 | Merck & Co., Inc. (A New Jersey Corp.) | Integrin-rezeptor-antagonisten |
| 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 |
| YU32502A (sh) | 1999-11-08 | 2004-12-31 | Merck & Co.Inc. | Postupak i intermedijeri za proizvodnju imidazolidinonskih antagonista alfa v integrina |
| US6933304B2 (en) | 2000-06-15 | 2005-08-23 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| JP2004504349A (ja) | 2000-07-26 | 2004-02-12 | メルク エンド カムパニー インコーポレーテッド | αｖインテグリン受容体拮抗薬 |
| WO2002022616A2 (en) | 2000-09-14 | 2002-03-21 | Merck & Co., Inc. | Alpha v integrin receptor antagonists |
| AU2002246757B2 (en) | 2001-01-03 | 2006-02-02 | 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 |
| US20050043344A1 (en) | 2002-12-20 | 2005-02-24 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists derivatives |
| DK2139882T3 (en) | 2007-03-23 | 2014-03-10 | Amgen Inc | 3-substituted quinoline or quinoxaline derivatives and their use as inhibitors of phosphatidylinositol 3-kinase (PI3K) |
| US20100311736A1 (en) | 2007-10-22 | 2010-12-09 | Glaxosmithkline Llc | Pyridosulfonamide derivatives as p13 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 |
| EP3052515A4 (en) | 2013-09-30 | 2017-03-15 | 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 |
| RU2017132433A (ru) | 2015-02-19 | 2019-03-19 | Сайфлуор Лайф Сайенсиз, Инк. | Фторированные производные тетрагидронафтиридинилнонановой кислоты и их применение |
| JP2018515424A (ja) | 2015-03-10 | 2018-06-14 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 抗アルファｖベータ１インテグリン阻害剤及び使用方法 |
| 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 |
-
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 JP JP2017516386A patent/JP6672276B2/ja not_active Expired - Fee Related
- 2015-09-22 RU RU2017114352A patent/RU2017114352A/ru unknown
- 2015-09-22 EP EP15767479.7A patent/EP3197895B1/en active Active
- 2015-09-22 AU AU2015320874A patent/AU2015320874A1/en not_active Abandoned
- 2015-09-22 CA CA2962319A patent/CA2962319A1/en active Pending
- 2015-09-22 CN CN201580052202.3A patent/CN107074850A/zh active Pending
- 2015-09-22 WO PCT/EP2015/071798 patent/WO2016046241A1/en not_active Ceased
- 2015-09-22 US US15/514,414 patent/US10004724B2/en not_active Expired - Fee Related
- 2015-09-22 BR BR112017006240A patent/BR112017006240A2/pt not_active Application Discontinuation
- 2015-09-22 KR KR1020177007735A patent/KR20170054413A/ko not_active Withdrawn