JP2020500182A5 - - Google Patents
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- Publication number
- JP2020500182A5 JP2020500182A5 JP2019523772A JP2019523772A JP2020500182A5 JP 2020500182 A5 JP2020500182 A5 JP 2020500182A5 JP 2019523772 A JP2019523772 A JP 2019523772A JP 2019523772 A JP2019523772 A JP 2019523772A JP 2020500182 A5 JP2020500182 A5 JP 2020500182A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- membered
- heterocyclyl
- carbocyclyl
- fibrosis
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 31
- 125000000623 heterocyclic group Chemical group 0.000 claims 21
- 125000004452 carbocyclyl group Chemical group 0.000 claims 20
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000005843 halogen group Chemical group 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- -1 cyano, hydroxyl Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 229940124530 sulfonamide Drugs 0.000 claims 12
- 150000003456 sulfonamides Chemical class 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 11
- 125000004438 haloalkoxy group Chemical group 0.000 claims 11
- 125000001188 haloalkyl group Chemical group 0.000 claims 11
- 206010016654 Fibrosis Diseases 0.000 claims 10
- 125000004103 aminoalkyl group Chemical group 0.000 claims 10
- 230000004761 fibrosis Effects 0.000 claims 10
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 9
- 150000001408 amides Chemical class 0.000 claims 9
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 5
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 5
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 4
- 230000001575 pathological effect Effects 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 2
- 239000004475 Arginine Substances 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 230000001476 alcoholic effect Effects 0.000 claims 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000005884 carbocyclylalkyl group Chemical group 0.000 claims 2
- 230000009787 cardiac fibrosis Effects 0.000 claims 2
- 208000019425 cirrhosis of liver Diseases 0.000 claims 2
- 208000006454 hepatitis Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 2
- 201000002793 renal fibrosis Diseases 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 1
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 claims 1
- 150000004657 carbamic acid derivatives Chemical class 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 150000003457 sulfones Chemical class 0.000 claims 1
- PYHOFAHZHOBVGV-UHFFFAOYSA-N triazane Chemical compound NNN PYHOFAHZHOBVGV-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662418833P | 2016-11-08 | 2016-11-08 | |
| US62/418,833 | 2016-11-08 | ||
| PCT/US2017/060392 WO2018089360A1 (en) | 2016-11-08 | 2017-11-07 | Pyrrole amides as alpha v integrin inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020500182A JP2020500182A (ja) | 2020-01-09 |
| JP2020500182A5 true JP2020500182A5 (https=) | 2020-12-17 |
| JP7220653B2 JP7220653B2 (ja) | 2023-02-10 |
Family
ID=60409438
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019523772A Active JP7220653B2 (ja) | 2016-11-08 | 2017-11-07 | アルファｖインテグリン阻害剤としてのピロールアミド |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US10717736B2 (https=) |
| EP (1) | EP3538528B1 (https=) |
| JP (1) | JP7220653B2 (https=) |
| KR (1) | KR102515507B1 (https=) |
| CN (1) | CN110139864B (https=) |
| AU (1) | AU2017359030A1 (https=) |
| BR (1) | BR112019009293A2 (https=) |
| CA (1) | CA3042693A1 (https=) |
| CY (1) | CY1123893T1 (https=) |
| DK (1) | DK3538528T3 (https=) |
| EA (1) | EA201991124A1 (https=) |
| ES (1) | ES2852351T3 (https=) |
| HR (1) | HRP20210228T1 (https=) |
| HU (1) | HUE053620T2 (https=) |
| IL (1) | IL266469A (https=) |
| LT (1) | LT3538528T (https=) |
| MX (1) | MX377293B (https=) |
| PL (1) | PL3538528T3 (https=) |
| PT (1) | PT3538528T (https=) |
| RS (1) | RS61453B1 (https=) |
| SI (1) | SI3538528T1 (https=) |
| SM (1) | SMT202100089T1 (https=) |
| WO (1) | WO2018089360A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3509590A4 (en) | 2016-09-07 | 2020-12-02 | Pliant Therapeutics, Inc. | N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE |
| 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 |
| US11306084B2 (en) | 2016-12-29 | 2022-04-19 | Saint Louis University | Integrin antagonists |
| MX394210B (es) | 2017-02-28 | 2025-03-04 | Morphic Therapeutic Inc | INHIBIDORES DE INTEGRINA AVß6. |
| MA52117A (fr) | 2017-02-28 | 2022-04-06 | Morphic Therapeutic Inc | Inhibiteurs de l'intégrine (alpha-v) (bêta-6) |
| WO2020047208A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| WO2020047239A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | INHIBITING αV β6 INTEGRIN |
| SI3844162T1 (sl) | 2018-08-29 | 2025-06-30 | Morphic Therapeutic, Inc. | Zaviralci integrina alfa v beta6 |
| ES3013256T3 (en) | 2018-10-30 | 2025-04-11 | Gilead Sciences Inc | Imidazo[1,2-a]pyridine derivatives as alpha4beta7 integrin inhibitors for the treatment of inflammatory diseases |
| JP7189368B2 (ja) | 2018-10-30 | 2022-12-13 | ギリアード サイエンシーズ， インコーポレイテッド | アルファ４ベータ７インテグリンの阻害のための化合物 |
| FI3873884T3 (fi) | 2018-10-30 | 2025-02-24 | Gilead Sciences Inc | 3-(kinolin-8-yyli)-1,4-dihydropyrido[3,4-d]pyrimidiini-2,4-dionijohdannaisia alfa-4-beta-7-integriinin estäjinä tulehdussairauksien hoidossa |
| EP3873605B1 (en) | 2018-10-30 | 2024-10-23 | Gilead Sciences, Inc. | Compounds for inhibition of alpha4beta7 integrin |
| WO2021030438A1 (en) | 2019-08-14 | 2021-02-18 | Gilead Sciences, Inc. | Compounds for inhibition of alpha 4 beta 7 integrin |
| KR20230169979A (ko) * | 2021-03-10 | 2023-12-18 | 다이스 몰레큘스 에스브이, 인크. | 알파 v 베타 6 및 알파 v 베타 1 인테그린 억제제 및 그의 용도 |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5849736A (en) | 1993-11-24 | 1998-12-15 | The Dupont Merck Pharmaceutical Company | Isoxazoline and isoxazole fibrinogen receptor antagonists |
| IL118325A0 (en) * | 1995-05-25 | 1996-10-31 | Pont Merck And Pharmaceutical | Integrin receptor antagonists and pharmaceutical compositions containing them |
| ZA972195B (en) | 1996-03-15 | 1998-09-14 | Du Pont Merck Pharma | Spirocycle integrin inhibitors |
| CA2309204A1 (en) | 1997-11-26 | 1999-06-03 | Dupont Pharmaceuticals Company | 1,3,4-thiadiazoles and 1,3,4-oxadiazoles as .alpha.v.beta.3 antagonists |
| CA2315370A1 (en) | 1997-12-17 | 1999-06-24 | Merck & Co., Inc. | Integrin receptor antagonists |
| KR20010042614A (ko) | 1998-04-10 | 2001-05-25 | 윌리암스 로저 에이 | 비트로넥틴 길항제로서 복소환식 글리실 베타-알라닌 유도체 |
| AU748621B2 (en) | 1998-08-13 | 2002-06-06 | Merck & Co., Inc. | Integrin receptor antagonists |
| AUPP646598A0 (en) | 1998-10-12 | 1998-11-05 | Fujisawa Pharmaceutical Co., Ltd. | New processes for producing alpha-alanine derivative |
| DE19939981A1 (de) | 1999-08-24 | 2001-03-01 | Merck Patent Gmbh | Neue Inhibitoren des Integrins alphavß3 |
| PL355011A1 (en) * | 1999-11-08 | 2004-03-22 | Merck & Co, Inc. | Process and intermediates for the preparation of imidazolidinone alpha v integrin antagonists |
| GB0001447D0 (en) * | 2000-01-21 | 2000-03-08 | Novartis Ag | Organic compounds |
| CA2436130A1 (en) | 2001-01-29 | 2002-08-08 | Ortho-Mcneil Pharmaceutical, Inc. | Substituted indoles and their use as integrin antagonists |
| AU2003259891A1 (en) | 2002-08-16 | 2004-03-19 | Janssen Pharmaceutica N.V. | Piperidinyl compounds that selectively bind integrins |
| TW200526626A (en) | 2003-09-13 | 2005-08-16 | Astrazeneca Ab | Chemical compounds |
| ATE399542T1 (de) | 2003-10-01 | 2008-07-15 | Merck Patent Gmbh | Alfavbeta3 und alfavbeta6 integrin antagonisten als antifibrotische mittel |
| WO2006108040A1 (en) | 2005-04-05 | 2006-10-12 | Janssen Pharmaceutica, N.V. | Substituted indoles and their use as integrin antagonists |
| JP2009539815A (ja) | 2006-06-09 | 2009-11-19 | アストラゼネカ アクチボラグ | 固形腫瘍の治療用のａ５ｂ１アンタゴニストとしてのＮ−（ベンゾイル）−Ｏ−［２−（ピリジン−２−イルアミノ）エチル］−Ｌ−チロシン誘導体と関連化合物 |
| WO2008125811A1 (en) | 2007-04-11 | 2008-10-23 | Astrazeneca Ab | N-[HETEROARYLCARBONYL]-S-THIENYL-L-ALANINE DERIVATIVES AS α5β1 ANTAGONISTS |
| EP2526095A1 (en) * | 2010-01-19 | 2012-11-28 | Theravance, Inc. | Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents |
| ITFI20100019A1 (it) | 2010-02-12 | 2011-08-13 | Univ Firenze | Inibitori peptidomimetici di integrine basati sull'1,2,3-triazolo per la diagnosi e terapia dei tumori. |
| US8969349B2 (en) | 2010-05-26 | 2015-03-03 | Sunovion Pharmaceuticals Inc. | Substituted quinoxalines and quinoxalinones as PDE-10 inhibitors |
| PT2953948T (pt) * | 2013-02-07 | 2017-12-12 | Scifluor Life Sciences Inc | Antagonistas de integrina fluorada |
| GB201305668D0 (en) * | 2013-03-28 | 2013-05-15 | Glaxosmithkline Ip Dev Ltd | Avs6 Integrin Antagonists |
| TWI667233B (zh) | 2013-12-19 | 2019-08-01 | 德商拜耳製藥公司 | 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途 |
| GB201417002D0 (en) | 2014-09-26 | 2014-11-12 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| 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 |
| US9790222B2 (en) | 2015-02-19 | 2017-10-17 | Scifluor Life Sciences, Inc. | Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof |
| WO2016145258A1 (en) | 2015-03-10 | 2016-09-15 | The Regents Of The University Of California | Anti-alphavbeta1 integrin inhibitors and methods of use |
-
2017
- 2017-11-07 HR HRP20210228TT patent/HRP20210228T1/hr unknown
- 2017-11-07 JP JP2019523772A patent/JP7220653B2/ja active Active
- 2017-11-07 PT PT178012365T patent/PT3538528T/pt unknown
- 2017-11-07 KR KR1020197016078A patent/KR102515507B1/ko active Active
- 2017-11-07 DK DK17801236.5T patent/DK3538528T3/da active
- 2017-11-07 SM SM20210089T patent/SMT202100089T1/it unknown
- 2017-11-07 CA CA3042693A patent/CA3042693A1/en not_active Abandoned
- 2017-11-07 WO PCT/US2017/060392 patent/WO2018089360A1/en not_active Ceased
- 2017-11-07 BR BR112019009293A patent/BR112019009293A2/pt not_active Application Discontinuation
- 2017-11-07 AU AU2017359030A patent/AU2017359030A1/en not_active Abandoned
- 2017-11-07 LT LTEP17801236.5T patent/LT3538528T/lt unknown
- 2017-11-07 RS RS20210206A patent/RS61453B1/sr unknown
- 2017-11-07 HU HUE17801236A patent/HUE053620T2/hu unknown
- 2017-11-07 PL PL17801236T patent/PL3538528T3/pl unknown
- 2017-11-07 SI SI201730618T patent/SI3538528T1/sl unknown
- 2017-11-07 ES ES17801236T patent/ES2852351T3/es active Active
- 2017-11-07 MX MX2019005233A patent/MX377293B/es active IP Right Grant
- 2017-11-07 EA EA201991124A patent/EA201991124A1/ru unknown
- 2017-11-07 EP EP17801236.5A patent/EP3538528B1/en active Active
- 2017-11-07 US US16/347,826 patent/US10717736B2/en active Active
- 2017-11-07 CN CN201780082138.2A patent/CN110139864B/zh active Active
-
2019
- 2019-05-06 IL IL266469A patent/IL266469A/en unknown
-
2021
- 2021-02-23 CY CY20211100149T patent/CY1123893T1/el unknown