JP2017528506A5 - - Google Patents

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Publication number: JP2017528506A5
Authority: JP; Japan
Prior art keywords: compound; tetrahydro; ethyl; butanoic acid; naphthyridin
Prior art date: 2015-09-22
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

Application number

JP2017516386A

Other languages

English (en)

Japanese (ja)

Other versions

JP6672276B2 (ja

JP2017528506A (ja

Filing date

2015-09-22

Publication date

2018-10-25

2014-09-26 Priority claimed from GBGB1417018.7A external-priority patent/GB201417018D0/en

2015-09-22 Application filed filed Critical

2017-09-28 Publication of JP2017528506A publication Critical patent/JP2017528506A/ja

2018-10-25 Publication of JP2017528506A5 publication Critical patent/JP2017528506A5/ja

2020-03-25 Application granted granted Critical

2020-03-25 Publication of JP6672276B2 publication Critical patent/JP6672276B2/ja

Status Expired - Fee Related legal-status Critical Current

2035-09-22 Anticipated expiration legal-status Critical

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

JP2017516386A 2014-09-26 2015-09-22 新規化合物 Expired - Fee Related JP6672276B2 (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
GBGB1417018.7A GB201417018D0 (en)	2014-09-26	2014-09-26	Novel compounds
GB1417018.7		2014-09-26
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 (2)	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 (2)
EP (1)	EP3197895B1 (2)
JP (1)	JP6672276B2 (2)
KR (1)	KR20170054413A (2)
CN (1)	CN107074850A (2)
AU (1)	AU2015320874A1 (2)
BR (1)	BR112017006240A2 (2)
CA (1)	CA2962319A1 (2)
ES (1)	ES2796235T3 (2)
GB (1)	GB201417018D0 (2)
RU (1)	RU2017114352A (2)
WO (1)	WO2016046241A1 (2)

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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
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
GB201604680D0 (en)	2016-03-21	2016-05-04	Glaxosmithkline Ip Dev Ltd	Chemical Compounds
KR102506327B1 (ko)	2016-11-08	2023-03-03	브리스톨-마이어스 스큅 컴퍼니	αV 인테그린 길항제로서의 인다졸 유도체
SI3538528T1 (sl)	2016-11-08	2021-03-31	Bristol-Myers Squibb Company	Pirol amidi kot alfa v integrin inhibitorji
AU2017359025A1 (en)	2016-11-08	2019-06-20	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
MX2019005234A (es)	2016-11-08	2019-08-12	Squibb Bristol Myers Co	Amidas y aminas de azol como inhibidores de integrina alfa v.
USRE50554E1 (en)	2016-12-23	2025-08-26	Pliant Therapeutics, Inc.	Amino acid compounds and methods of use
MA52117A (fr)	2017-02-28	2022-04-06	Morphic Therapeutic Inc	Inhibiteurs de l'intégrine (alpha-v) (bêta-6)
MA47697A (fr)	2017-02-28	2020-01-08	Morphic Therapeutic Inc	Inhibiteurs de l'(alpha-v)(bêta-6) intégrine
ES2904645T3 (es)	2017-11-07	2022-04-05	Bristol Myers Squibb Co	Derivados de pirrolopirazina como inhibidores de integrina alfa v
WO2020047208A1 (en)	2018-08-29	2020-03-05	Morphic Therapeutic, Inc.	Inhibitors of (alpha-v)(beta-6) integrin
FI3844162T3 (fi)	2018-08-29	2025-03-27	Morphic Therapeutic Inc	Alfa v beeta6 -integriinin estäjiä
EP4086254B1 (en)	2018-08-29	2024-12-18	Morphic Therapeutic, Inc.	Integrin inhibitors

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WO1999030709A1 (en)	1997-12-17	1999-06-24	Merck & Co., Inc.	Integrin receptor antagonists
PT1187592E (pt)	1999-06-02	2007-10-19	Merck & Co Inc	Antagonistas dos receptores de integrina alfa v
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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
KR102647026B1 (ko)	2015-02-19	2024-03-12	사이플루어 라이프 사이언시즈, 인크	플루오르화 테트라히드로나프티리디닐 노난산 유도체 및 이의 용도
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
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 AU AU2015320874A patent/AU2015320874A1/en not_active Abandoned
- 2015-09-22 EP EP15767479.7A patent/EP3197895B1/en active Active
- 2015-09-22 WO PCT/EP2015/071798 patent/WO2016046241A1/en not_active Ceased
- 2015-09-22 CN CN201580052202.3A patent/CN107074850A/zh active Pending
- 2015-09-22 BR BR112017006240A patent/BR112017006240A2/pt not_active Application Discontinuation
- 2015-09-22 KR KR1020177007735A patent/KR20170054413A/ko not_active Withdrawn
- 2015-09-22 JP JP2017516386A patent/JP6672276B2/ja not_active Expired - Fee Related
- 2015-09-22 CA CA2962319A patent/CA2962319A1/en active Pending
- 2015-09-22 RU RU2017114352A patent/RU2017114352A/ru unknown
- 2015-09-22 ES ES15767479T patent/ES2796235T3/es active Active
- 2015-09-22 US US15/514,414 patent/US10004724B2/en not_active Expired - Fee Related

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