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 (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112019012515A2 (pt) | 2016-12-29 | 2019-11-19 | Saint Louis University | antagonistas de integrina |
| TW201835078A (zh) | 2017-02-28 | 2018-10-01 | 美商萊築理公司 | αvβ6整合蛋白之抑制劑 |
| MA52117A (fr) | 2017-02-28 | 2022-04-06 | Morphic Therapeutic Inc | Inhibiteurs de l'intégrine (alpha-v) (bêta-6) |
| MX2021002181A (es) | 2018-08-29 | 2021-07-15 | Morphic Therapeutic Inc | Inhibicion de la integrina alfa v beta 6. |
| US20240245682A1 (en) * | 2022-12-27 | 2024-07-25 | Pliant Therapeutics, Inc. | Alpha-v-beta-8 integrin inhibitors and uses thereof |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6933304B2 (en) * | 2000-06-15 | 2005-08-23 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| MXPA05006587A (es) | 2002-12-20 | 2005-12-14 | Pharmacia Corp | Compuestos de tiazol como derivados de antagonistas del receptor de la integrina. |
| CA2507699A1 (en) * | 2002-12-20 | 2004-07-15 | Pharmacia Corporation | Heteroarylalkanoic acids as integrin receptor antagonists |
| US20050004200A1 (en) * | 2002-12-20 | 2005-01-06 | Pharmacia Corporation | Pyrazole compounds as integrin receptor antagonists derivatives |
| US9085606B2 (en) * | 2012-07-18 | 2015-07-21 | Saint Louis University | Beta amino acid derivatives as integrin antagonists |
| US8716226B2 (en) * | 2012-07-18 | 2014-05-06 | Saint Louis University | 3,5 phenyl-substituted beta amino acid derivatives as integrin antagonists |
| WO2015048819A1 (en) | 2013-09-30 | 2015-04-02 | The Regents Of The University Of California | Anti-alphavbeta1 integrin compounds and methods |
| EP3538525B1 (en) | 2016-11-08 | 2022-06-22 | Bristol-Myers Squibb Company | 3-substituted propionic acids as alpha v integrin inhibitors |
| TW201819378A (zh) | 2016-11-08 | 2018-06-01 | 美商必治妥美雅史谷比公司 | 作為αｖ整合素抑制劑之含環丁烷及氮雜環丁烷之單及螺環化合物 |
| EP3538527B1 (en) | 2016-11-08 | 2021-10-13 | Bristol-Myers Squibb Company | Azole amides and amines as alpha v integrin inhibitors |
| WO2018089360A1 (en) | 2016-11-08 | 2018-05-17 | Bristol-Myers Squibb Company | Pyrrole amides as alpha v integrin inhibitors |
| ES2886650T3 (es) | 2016-11-08 | 2021-12-20 | Bristol Myers Squibb Co | Derivados de indazol como antagonistas de integrina alfaV |
| BR112019012515A2 (pt) | 2016-12-29 | 2019-11-19 | Saint Louis University | antagonistas de integrina |
| MA52117A (fr) | 2017-02-28 | 2022-04-06 | Morphic Therapeutic Inc | Inhibiteurs de l'intégrine (alpha-v) (bêta-6) |
| 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 |
| WO2020009889A1 (en) | 2018-07-03 | 2020-01-09 | Saint Louis University | ALPHAvBETA1 INTEGRIN ANTAGONISTS |
-
2017
- 2017-12-28 BR BR112019012515-9A patent/BR112019012515A2/pt not_active Application Discontinuation
- 2017-12-28 KR KR1020197019720A patent/KR20190100232A/ko not_active Withdrawn
- 2017-12-28 RU RU2019116820A patent/RU2019116820A/ru not_active Application Discontinuation
- 2017-12-28 WO PCT/US2017/068801 patent/WO2018132268A1/en not_active Ceased
- 2017-12-28 US US16/474,505 patent/US11306084B2/en active Active
- 2017-12-28 CA CA3045491A patent/CA3045491A1/en not_active Abandoned
- 2017-12-28 JP JP2019534956A patent/JP2020504120A/ja active Pending
- 2017-12-28 EP EP17891632.6A patent/EP3562826A4/en not_active Withdrawn
- 2017-12-28 MX MX2019007797A patent/MX2019007797A/es unknown
- 2017-12-28 CN CN201780080614.7A patent/CN110177787A/zh active Pending
- 2017-12-28 AU AU2017393297A patent/AU2017393297A1/en not_active Abandoned
-
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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