JP2020504120A5 - - Google Patents
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- Publication number
- JP2020504120A5 JP2020504120A5 JP2019534956A JP2019534956A JP2020504120A5 JP 2020504120 A5 JP2020504120 A5 JP 2020504120A5 JP 2019534956 A JP2019534956 A JP 2019534956A JP 2019534956 A JP2019534956 A JP 2019534956A JP 2020504120 A5 JP2020504120 A5 JP 2020504120A5
- Authority
- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- alkyl
- compound according
- solvate
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims description 87
- 125000000217 alkyl group Chemical group 0.000 claims description 74
- 125000003545 alkoxy group Chemical group 0.000 claims description 30
- 150000003839 salts Chemical class 0.000 claims description 27
- 125000003118 aryl group Chemical group 0.000 claims description 26
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 26
- 108010044426 integrins Proteins 0.000 claims description 24
- 102000006495 integrins Human genes 0.000 claims description 24
- 238000000034 method Methods 0.000 claims description 23
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- 239000001257 hydrogen Substances 0.000 claims description 21
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 20
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
- 125000004423 acyloxy group Chemical group 0.000 claims description 16
- 125000004104 aryloxy group Chemical group 0.000 claims description 16
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- 150000002431 hydrogen Chemical class 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 13
- 208000035475 disorder Diseases 0.000 claims description 13
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 7
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical group C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 6
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims description 4
- 238000006467 substitution reaction Methods 0.000 claims description 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 2
- 230000029936 alkylation Effects 0.000 claims description 2
- 238000005804 alkylation reaction Methods 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims 22
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- -1 t- butyl Chemical group 0.000 claims 1
- 238000003556 assay Methods 0.000 description 8
- 102000005962 receptors Human genes 0.000 description 8
- 108020003175 receptors Proteins 0.000 description 8
- 239000007790 solid phase Substances 0.000 description 8
- 0 CC(C*)[C@@](C*)(*(C)*)N Chemical compound CC(C*)[C@@](C*)(*(C)*)N 0.000 description 7
- 125000005843 halogen group Chemical group 0.000 description 5
- 206010016654 Fibrosis Diseases 0.000 description 4
- 230000004761 fibrosis Effects 0.000 description 4
- 229940123038 Integrin antagonist Drugs 0.000 description 3
- 210000001215 vagina Anatomy 0.000 description 3
- 241000283690 Bos taurus Species 0.000 description 2
- 241000283707 Capra Species 0.000 description 2
- 241000700199 Cavia porcellus Species 0.000 description 2
- 241000282693 Cercopithecidae Species 0.000 description 2
- 241000283073 Equus caballus Species 0.000 description 2
- 241000282326 Felis catus Species 0.000 description 2
- 241000282414 Homo sapiens Species 0.000 description 2
- 241000699666 Mus <mouse, genus> Species 0.000 description 2
- 241001494479 Pecora Species 0.000 description 2
- 241000009328 Perro Species 0.000 description 2
- 241000700159 Rattus Species 0.000 description 2
- 206010039710 Scleroderma Diseases 0.000 description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 2
- 210000002216 heart Anatomy 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 238000001361 intraarterial administration Methods 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 210000000664 rectum Anatomy 0.000 description 2
- SIGFMSBEOZQWSF-FTFSGFEDSA-N CC(C)(C(F)(F)F)c1cc(C(CC(O)=O)Cc2n[n](C)c(OCC/C=N/C(NCCC3)=C3C=C)c2)cc(Cl)c1 Chemical compound CC(C)(C(F)(F)F)c1cc(C(CC(O)=O)Cc2n[n](C)c(OCC/C=N/C(NCCC3)=C3C=C)c2)cc(Cl)c1 SIGFMSBEOZQWSF-FTFSGFEDSA-N 0.000 description 1
- RLVXKYACSNXUET-UHFFFAOYSA-N CC(C)(C(F)(F)F)c1cc(C(CC(O)=O)Cc2n[n](C)c(OCCc3nc(NCCC4)c4cc3)c2)cc(Br)c1 Chemical compound CC(C)(C(F)(F)F)c1cc(C(CC(O)=O)Cc2n[n](C)c(OCCc3nc(NCCC4)c4cc3)c2)cc(Br)c1 RLVXKYACSNXUET-UHFFFAOYSA-N 0.000 description 1
- FFXNYYUSGGMJSF-UHFFFAOYSA-N CC(C)(C(F)(F)F)c1cc(C(CC(O)=O)Cc2n[n](C)c(OCCc3nc(NCCC4)c4cc3)c2)cc(F)c1 Chemical compound CC(C)(C(F)(F)F)c1cc(C(CC(O)=O)Cc2n[n](C)c(OCCc3nc(NCCC4)c4cc3)c2)cc(F)c1 FFXNYYUSGGMJSF-UHFFFAOYSA-N 0.000 description 1
- NNTLDXFWDMKUEA-LAJOBFMHSA-N CC(C)(C)c1cc(C(CC(/C=C(\NC)/OCCC2=NC3NCCCC3C=C2)=N)CC(O)=O)cc(C(C)(C)C)c1 Chemical compound CC(C)(C)c1cc(C(CC(/C=C(\NC)/OCCC2=NC3NCCCC3C=C2)=N)CC(O)=O)cc(C(C)(C)C)c1 NNTLDXFWDMKUEA-LAJOBFMHSA-N 0.000 description 1
- 206010019668 Hepatic fibrosis Diseases 0.000 description 1
- 108010041014 Integrin alpha5 Proteins 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 206010050207 Skin fibrosis Diseases 0.000 description 1
- 125000001246 bromo group Chemical group Br* 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000007917 intracranial administration Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 239000002502 liposome Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
- 230000010412 perfusion Effects 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 208000005069 pulmonary fibrosis Diseases 0.000 description 1
- 201000002793 renal fibrosis Diseases 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000000115 thoracic cavity Anatomy 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 210000003437 trachea Anatomy 0.000 description 1
- 230000009261 transgenic effect Effects 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662440253P | 2016-12-29 | 2016-12-29 | |
| US62/440,253 | 2016-12-29 | ||
| US201762471882P | 2017-03-15 | 2017-03-15 | |
| US62/471,882 | 2017-03-15 | ||
| PCT/US2017/068801 WO2018132268A1 (en) | 2016-12-29 | 2017-12-28 | Integrin antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020504120A JP2020504120A (ja) | 2020-02-06 |
| JP2020504120A5 true JP2020504120A5 (enExample) | 2021-01-21 |
Family
ID=62840040
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019534956A Pending JP2020504120A (ja) | 2016-12-29 | 2017-12-28 | インテグリンアンタゴニスト |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US11306084B2 (enExample) |
| EP (1) | EP3562826A4 (enExample) |
| JP (1) | JP2020504120A (enExample) |
| KR (1) | KR20190100232A (enExample) |
| CN (1) | CN110177787A (enExample) |
| AU (1) | AU2017393297A1 (enExample) |
| BR (1) | BR112019012515A2 (enExample) |
| CA (1) | CA3045491A1 (enExample) |
| CO (1) | CO2019007023A2 (enExample) |
| IL (1) | IL267686A (enExample) |
| MX (1) | MX2019007797A (enExample) |
| PH (1) | PH12019501514A1 (enExample) |
| RU (1) | RU2019116820A (enExample) |
| WO (1) | WO2018132268A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3045491A1 (en) | 2016-12-29 | 2018-07-19 | Indalo Therapeutics, Inc. | Integrin antagonists |
| US11046685B2 (en) | 2017-02-28 | 2021-06-29 | Morphic Therapeutic, Inc. | Inhibitors of (α-v)(β-6) integrin |
| EP4159727B1 (en) | 2017-02-28 | 2026-04-08 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| WO2020047208A1 (en) | 2018-08-29 | 2020-03-05 | Morphic Therapeutic, Inc. | Inhibitors of (alpha-v)(beta-6) integrin |
| PT3844162T (pt) | 2018-08-29 | 2025-03-28 | Morphic Therapeutic Inc | Inibidores da integrina alfa v beta6 |
| AU2019327475B2 (en) | 2018-08-29 | 2025-06-05 | Morphic Therapeutic, Inc. | INHIBITING αV β6 INTEGRIN |
| WO2024145245A2 (en) * | 2022-12-27 | 2024-07-04 | Pliant Therapeutics, Inc. | Alpha-v-beta-8 integrin inhibitors and uses thereof |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004511434A (ja) * | 2000-06-15 | 2004-04-15 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸 |
| MXPA05006588A (es) * | 2002-12-20 | 2005-08-16 | Pharmacia Corp | Compuestos de pirazol como derivados antagonistas del receptor de la integrina. |
| BR0316876A (pt) | 2002-12-20 | 2005-10-25 | Pharmacia Corp | Compostos de tiazol e composição farmacêutica compreendendo o mesmo |
| BR0317600A (pt) | 2002-12-20 | 2005-11-29 | Pharmacia Corp | ácidos heteroarilalcanóicos como derivados de antagonistas de receptor de integrina |
| IN2015DN00099A (enExample) * | 2012-07-18 | 2015-05-29 | Univ Saint Louis | |
| US8716226B2 (en) * | 2012-07-18 | 2014-05-06 | Saint Louis University | 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists |
| AU2014324426A1 (en) | 2013-09-30 | 2016-04-21 | The Regents Of The University Of California | Anti-alphavbeta1 integrin compounds and methods |
| AU2017359028A1 (en) | 2016-11-08 | 2019-06-20 | Bristol-Myers Squibb Company | Azole amides and amines as alpha V integrin inhibitors |
| CN110167934B (zh) | 2016-11-08 | 2022-06-10 | 百时美施贵宝公司 | 作为αV整联蛋白抑制剂的含有环丁烷和含有氮杂环丁烷的单环和螺环化合物 |
| EA201991123A1 (ru) | 2016-11-08 | 2019-11-29 | ИНДАЗОЛОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ АНТАГОНИСТОВ ИНТЕГРИНА αV | |
| EP3538528B1 (en) | 2016-11-08 | 2020-12-23 | Bristol-Myers Squibb Company | Pyrrole amides as alpha v integrin inhibitors |
| PT3538525T (pt) | 2016-11-08 | 2022-08-16 | Bristol Myers Squibb Co | Ácidos propiónicos 3-substituídos por inibidores de alfa v integrina |
| CA3045491A1 (en) | 2016-12-29 | 2018-07-19 | Indalo Therapeutics, Inc. | Integrin antagonists |
| US11046685B2 (en) | 2017-02-28 | 2021-06-29 | Morphic Therapeutic, Inc. | Inhibitors of (α-v)(β-6) integrin |
| TWI841573B (zh) | 2018-06-27 | 2024-05-11 | 美商普萊恩醫療公司 | 具有未分支連接子之胺基酸化合物及使用方法 |
| US20210284638A1 (en) | 2018-07-03 | 2021-09-16 | Saint Louis University | ALPHAvBETA1 INTEGRIN ANTAGONISTS |
-
2017
- 2017-12-28 CA CA3045491A patent/CA3045491A1/en not_active Abandoned
- 2017-12-28 US US16/474,505 patent/US11306084B2/en active Active
- 2017-12-28 MX MX2019007797A patent/MX2019007797A/es unknown
- 2017-12-28 KR KR1020197019720A patent/KR20190100232A/ko not_active Withdrawn
- 2017-12-28 EP EP17891632.6A patent/EP3562826A4/en not_active Withdrawn
- 2017-12-28 BR BR112019012515-9A patent/BR112019012515A2/pt not_active Application Discontinuation
- 2017-12-28 WO PCT/US2017/068801 patent/WO2018132268A1/en not_active Ceased
- 2017-12-28 CN CN201780080614.7A patent/CN110177787A/zh active Pending
- 2017-12-28 JP JP2019534956A patent/JP2020504120A/ja active Pending
- 2017-12-28 AU AU2017393297A patent/AU2017393297A1/en not_active Abandoned
- 2017-12-28 RU RU2019116820A patent/RU2019116820A/ru not_active Application Discontinuation
-
2019
- 2019-06-26 IL IL267686A patent/IL267686A/en unknown
- 2019-06-27 PH PH12019501514A patent/PH12019501514A1/en unknown
- 2019-06-28 CO CONC2019/0007023A patent/CO2019007023A2/es unknown
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