JP2021502358A5 - - Google Patents
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- Publication number
- JP2021502358A5 JP2021502358A5 JP2020524801A JP2020524801A JP2021502358A5 JP 2021502358 A5 JP2021502358 A5 JP 2021502358A5 JP 2020524801 A JP2020524801 A JP 2020524801A JP 2020524801 A JP2020524801 A JP 2020524801A JP 2021502358 A5 JP2021502358 A5 JP 2021502358A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- alkyl
- amino
- pharmaceutically acceptable
- acceptable salt
- 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
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- -1 (dihydroimidazolyl) amino Chemical group 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000001475 halogen functional group Chemical group 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 206010016654 Fibrosis Diseases 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000000428 dust Substances 0.000 claims 3
- 230000004761 fibrosis Effects 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000003965 isoxazolidinyl group Chemical group 0.000 claims 3
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000004622 benzoxazinyl group Chemical group O1NC(=CC2=C1C=CC=C2)* 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000000723 dihydrobenzofuranyl group Chemical group O1C(CC2=C1C=CC=C2)* 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 210000003739 neck Anatomy 0.000 claims 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 2
- 210000003491 skin Anatomy 0.000 claims 2
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 125000005529 alkyleneoxy group Chemical group 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 230000002357 endometrial effect Effects 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000001508 eye Anatomy 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 210000004392 genitalia Anatomy 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 210000002216 heart Anatomy 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 210000002429 large intestine Anatomy 0.000 claims 1
- 210000002200 mouth mucosa Anatomy 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 210000002850 nasal mucosa Anatomy 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 210000003800 pharynx Anatomy 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 210000000952 spleen Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762582693P | 2017-11-07 | 2017-11-07 | |
| US62/582,693 | 2017-11-07 | ||
| PCT/US2018/059157 WO2019094319A1 (en) | 2017-11-07 | 2018-11-05 | Pyrrolopyrazine derivatives as alpha v integrin inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021502358A JP2021502358A (ja) | 2021-01-28 |
| JP2021502358A5 true JP2021502358A5 (https=) | 2021-12-16 |
| JP7291696B2 JP7291696B2 (ja) | 2023-06-15 |
Family
ID=64362756
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020524801A Active JP7291696B2 (ja) | 2017-11-07 | 2018-11-05 | アルファｖインテグリン阻害剤としてのピロロピラジン誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US11292802B2 (https=) |
| EP (1) | EP3707142B1 (https=) |
| JP (1) | JP7291696B2 (https=) |
| KR (1) | KR102700471B1 (https=) |
| CN (1) | CN111433207B (https=) |
| AU (1) | AU2018365793A1 (https=) |
| BR (1) | BR112020008893A2 (https=) |
| CA (1) | CA3081805A1 (https=) |
| EA (1) | EA202091136A1 (https=) |
| ES (1) | ES2904645T3 (https=) |
| IL (1) | IL274425A (https=) |
| MX (1) | MX2020004455A (https=) |
| SG (1) | SG11202004077WA (https=) |
| WO (1) | WO2019094319A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102700471B1 (ko) * | 2017-11-07 | 2024-08-28 | 브리스톨-마이어스 스큅 컴퍼니 | 알파 v 인테그린 억제제로서의 피롤로피라진 유도체 |
| 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 |
| 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 |
| 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 |
| 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 |
| US20230060422A1 (en) * | 2019-12-20 | 2023-03-02 | Novartis Ag | Combination treatment of liver diseases using integrin inhibitors |
Family Cites Families (25)
| 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 |
| 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 |
| AU748621B2 (en) | 1998-08-13 | 2002-06-06 | Merck & Co., Inc. | Integrin receptor antagonists |
| JP2004521079A (ja) | 2000-08-29 | 2004-07-15 | ファルマシア・コーポレーション | アルファーｖベータ３アンタゴニストとして有用な二環式環系を含有する化合物 |
| CA2436130A1 (en) * | 2001-01-29 | 2002-08-08 | Ortho-Mcneil Pharmaceutical, Inc. | Substituted indoles and their use as integrin antagonists |
| EP1592421A1 (en) | 2002-12-20 | 2005-11-09 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| US7365209B2 (en) | 2003-02-11 | 2008-04-29 | Pharmacopeia, Inc. | Nitrogen heterocycle biaryls for osteoporosis and other diseases |
| TW200526626A (en) | 2003-09-13 | 2005-08-16 | Astrazeneca Ab | Chemical compounds |
| 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 |
| JP2011184298A (ja) | 2008-06-02 | 2011-09-22 | Sanwa Kagaku Kenkyusho Co Ltd | 新規化合物及びその医薬用途 |
| 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 |
| 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 |
| KR102700471B1 (ko) * | 2017-11-07 | 2024-08-28 | 브리스톨-마이어스 스큅 컴퍼니 | 알파 v 인테그린 억제제로서의 피롤로피라진 유도체 |
-
2018
- 2018-11-05 KR KR1020207015957A patent/KR102700471B1/ko active Active
- 2018-11-05 EA EA202091136A patent/EA202091136A1/ru unknown
- 2018-11-05 JP JP2020524801A patent/JP7291696B2/ja active Active
- 2018-11-05 WO PCT/US2018/059157 patent/WO2019094319A1/en not_active Ceased
- 2018-11-05 BR BR112020008893-5A patent/BR112020008893A2/pt not_active Application Discontinuation
- 2018-11-05 ES ES18804882T patent/ES2904645T3/es active Active
- 2018-11-05 SG SG11202004077WA patent/SG11202004077WA/en unknown
- 2018-11-05 CN CN201880071717.1A patent/CN111433207B/zh active Active
- 2018-11-05 MX MX2020004455A patent/MX2020004455A/es unknown
- 2018-11-05 EP EP18804882.1A patent/EP3707142B1/en active Active
- 2018-11-05 AU AU2018365793A patent/AU2018365793A1/en not_active Abandoned
- 2018-11-05 CA CA3081805A patent/CA3081805A1/en not_active Abandoned
- 2018-11-05 US US16/761,286 patent/US11292802B2/en active Active
-
2020
- 2020-05-04 IL IL274425A patent/IL274425A/en unknown
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