JP6854386B2 - リゾホスファチジン酸受容体１（ｌｐａｒ１）阻害剤化合物 - Google Patents
リゾホスファチジン酸受容体１（ｌｐａｒ１）阻害剤化合物 Download PDFInfo
- Publication number
- JP6854386B2 JP6854386B2 JP2020512678A JP2020512678A JP6854386B2 JP 6854386 B2 JP6854386 B2 JP 6854386B2 JP 2020512678 A JP2020512678 A JP 2020512678A JP 2020512678 A JP2020512678 A JP 2020512678A JP 6854386 B2 JP6854386 B2 JP 6854386B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- phenyl
- amino
- mmol
- pyridyl
- 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.)
- Active
Links
- AMDKQWQKUHMBDZ-UHFFFAOYSA-N CC(C)(C)OC(Nc([n](C)nc1)c1-c1ncc(-c2ccc(C3(CC3)C(OC)=O)cc2)nc1)=O Chemical compound CC(C)(C)OC(Nc([n](C)nc1)c1-c1ncc(-c2ccc(C3(CC3)C(OC)=O)cc2)nc1)=O AMDKQWQKUHMBDZ-UHFFFAOYSA-N 0.000 description 1
- FFCFNXICCFFWSL-WWIRCMRFSA-N CC(C)(C)Oc1cncc(N/C(/NC)=C(/C=N)\c(cc2)ncc2-c2ccc(C3(CC3)C(OC)=O)cc2)n1 Chemical compound CC(C)(C)Oc1cncc(N/C(/NC)=C(/C=N)\c(cc2)ncc2-c2ccc(C3(CC3)C(OC)=O)cc2)n1 FFCFNXICCFFWSL-WWIRCMRFSA-N 0.000 description 1
- GSXYTVAMZJDKQH-UHFFFAOYSA-N CC(C)(c1nc(Cl)cnc1)F Chemical compound CC(C)(c1nc(Cl)cnc1)F GSXYTVAMZJDKQH-UHFFFAOYSA-N 0.000 description 1
- GELKLBRDTBTEQS-UHFFFAOYSA-N CC(C)(c1nc(Cl)cnc1)O Chemical compound CC(C)(c1nc(Cl)cnc1)O GELKLBRDTBTEQS-UHFFFAOYSA-N 0.000 description 1
- QZCCZGAALUACDQ-XAHJZKJCSA-N CC(C)Cc1cncc(N/C(/NC)=C(/C=N)\c(cc2)ccc2-c2ccc(C3(CC3)C(O)=O)cc2)n1 Chemical compound CC(C)Cc1cncc(N/C(/NC)=C(/C=N)\c(cc2)ccc2-c2ccc(C3(CC3)C(O)=O)cc2)n1 QZCCZGAALUACDQ-XAHJZKJCSA-N 0.000 description 1
- HXMMSYGOOFGCOQ-UHFFFAOYSA-N CC(C)Oc1cncc(Nc2c(C3N=CC(c4ccc(C5(CC5)C(OC)=O)cc4)=CC3F)cn[n]2C)n1 Chemical compound CC(C)Oc1cncc(Nc2c(C3N=CC(c4ccc(C5(CC5)C(OC)=O)cc4)=CC3F)cn[n]2C)n1 HXMMSYGOOFGCOQ-UHFFFAOYSA-N 0.000 description 1
- ONZFBBWRSJRDQO-CZJUZCBCSA-N CC(C)c1cncc(N/C(/NC)=C(/C=N)\c(nc2)ccc2-c2c(COC)cc(C3(CC3)C(OC)=O)cc2)n1 Chemical compound CC(C)c1cncc(N/C(/NC)=C(/C=N)\c(nc2)ccc2-c2c(COC)cc(C3(CC3)C(OC)=O)cc2)n1 ONZFBBWRSJRDQO-CZJUZCBCSA-N 0.000 description 1
- QULQVCSHCACLOQ-UHFFFAOYSA-N CC(C)c1cncc(Nc([n](C)nc2)c2-c(cc2)ncc2-c2ccc(C3(CC3)C(O)=O)cc2)n1 Chemical compound CC(C)c1cncc(Nc([n](C)nc2)c2-c(cc2)ncc2-c2ccc(C3(CC3)C(O)=O)cc2)n1 QULQVCSHCACLOQ-UHFFFAOYSA-N 0.000 description 1
- XGGYBDMIXLZPFU-UHFFFAOYSA-N CC(C)c1cncc(Nc([n](C)nc2)c2-c(cc2)ncc2-c2ccc(C3(CC3)C(O)=O)cc2CC#N)n1 Chemical compound CC(C)c1cncc(Nc([n](C)nc2)c2-c(cc2)ncc2-c2ccc(C3(CC3)C(O)=O)cc2CC#N)n1 XGGYBDMIXLZPFU-UHFFFAOYSA-N 0.000 description 1
- VJJQHOLIFWTIIJ-NDAYZCAMSA-O CC(C)c1nc(N/C(/NC)=C(/C=[NH2+])\c(cc2)ncc2-c2ccc(C3(CC3)C(O)=O)cc2)cnc1 Chemical compound CC(C)c1nc(N/C(/NC)=C(/C=[NH2+])\c(cc2)ncc2-c2ccc(C3(CC3)C(O)=O)cc2)cnc1 VJJQHOLIFWTIIJ-NDAYZCAMSA-O 0.000 description 1
- PEPQJERQQQDLNI-UHFFFAOYSA-N CC(c1nc(Cl)cnc1)=C Chemical compound CC(c1nc(Cl)cnc1)=C PEPQJERQQQDLNI-UHFFFAOYSA-N 0.000 description 1
- WBWJWTUMSZVMKK-UHFFFAOYSA-N CCOC(C1(CC1)c(cc1CC#N)ccc1Br)=O Chemical compound CCOC(C1(CC1)c(cc1CC#N)ccc1Br)=O WBWJWTUMSZVMKK-UHFFFAOYSA-N 0.000 description 1
- UZLRYHOHMVGASW-UHFFFAOYSA-N CCOC(Cc(cc1)c(C(F)(F)F)cc1Br)=O Chemical compound CCOC(Cc(cc1)c(C(F)(F)F)cc1Br)=O UZLRYHOHMVGASW-UHFFFAOYSA-N 0.000 description 1
- CKUVSPQGYLELRG-UHFFFAOYSA-N Cc1cncc(Cl)n1 Chemical compound Cc1cncc(Cl)n1 CKUVSPQGYLELRG-UHFFFAOYSA-N 0.000 description 1
- JNRJVPPAAXUGMP-UHFFFAOYSA-N Cc1cncc(OC2CC2)n1 Chemical compound Cc1cncc(OC2CC2)n1 JNRJVPPAAXUGMP-UHFFFAOYSA-N 0.000 description 1
- FBIJKNDFKKNDOI-UHFFFAOYSA-N N#CC1(CC1)c(cn1)ccc1Cl Chemical compound N#CC1(CC1)c(cn1)ccc1Cl FBIJKNDFKKNDOI-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2017/100354 WO2019041340A1 (en) | 2017-09-04 | 2017-09-04 | LYSOPHOSPHATIDE ACID RECEPTOR 1 RECEPTOR INHIBITORS (LPAR1) |
| CNPCT/CN2017/100354 | 2017-09-04 | ||
| PCT/US2018/048249 WO2019046239A1 (en) | 2017-09-04 | 2018-08-28 | LYSOPHOSPHATIDE ACID RECEPTOR 1 RECEPTOR INHIBITORS (LPAR1) |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020532550A JP2020532550A (ja) | 2020-11-12 |
| JP2020532550A5 JP2020532550A5 (enExample) | 2020-12-24 |
| JP6854386B2 true JP6854386B2 (ja) | 2021-04-07 |
Family
ID=63528947
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020512678A Active JP6854386B2 (ja) | 2017-09-04 | 2018-08-28 | リゾホスファチジン酸受容体１（ｌｐａｒ１）阻害剤化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US11365185B2 (enExample) |
| EP (1) | EP3679032B1 (enExample) |
| JP (1) | JP6854386B2 (enExample) |
| KR (1) | KR102341064B1 (enExample) |
| CN (1) | CN111032647B (enExample) |
| AU (1) | AU2018323969B2 (enExample) |
| CA (1) | CA3073983C (enExample) |
| EA (1) | EA039482B1 (enExample) |
| ES (1) | ES2966827T3 (enExample) |
| IL (1) | IL273000B2 (enExample) |
| MX (1) | MX2020002430A (enExample) |
| SA (1) | SA520411406B1 (enExample) |
| WO (2) | WO2019041340A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2020384883B2 (en) | 2019-11-15 | 2023-11-16 | Gilead Sciences, Inc. | Triazole carbamate pyridyl sulfonamides as LPA receptor antagonists and uses thereof |
| TWI838626B (zh) | 2020-06-03 | 2024-04-11 | 美商基利科學股份有限公司 | Lpa受體拮抗劑及其用途 |
| JP7591066B2 (ja) | 2020-06-03 | 2024-11-27 | ギリアード サイエンシーズ， インコーポレイテッド | Ｌｐａ受容体アンタゴニスト及びそれらの使用 |
| WO2022240879A1 (en) | 2021-05-11 | 2022-11-17 | Gilead Sciences, Inc. | Lpa receptor antagonists and uses thereof |
| KR20240007233A (ko) | 2021-05-13 | 2024-01-16 | 길리애드 사이언시즈, 인코포레이티드 | Lpa 수용체 길항제 및 이의 용도 |
| CN113461640B (zh) * | 2021-06-17 | 2023-08-11 | 中央民族大学 | Lpar1抑制剂、医药用途及其制备方法 |
| JP7709612B2 (ja) | 2021-12-08 | 2025-07-16 | ギリアード サイエンシーズ， インコーポレイテッド | Ｌｐａ受容体アンタゴニスト及びそれらの使用 |
| AR128613A1 (es) | 2022-02-25 | 2024-05-29 | Lhotse Bio Inc | Compuestos y composiciones para el tratamiento de afecciones asociadas con la actividad del receptor de lpa |
| JP2025540714A (ja) * | 2022-11-24 | 2025-12-16 | ローツェ・バイオ・インコーポレイテッド | Ｌｐａ受容体活性と関連する状態を処置するための化合物および組成物 |
| CN121419961A (zh) * | 2023-06-02 | 2026-01-27 | 迈塔免疫科技股份有限公司 | 用于治疗纤维化疾病的化合物 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2466121B (en) * | 2008-12-15 | 2010-12-08 | Amira Pharmaceuticals Inc | Antagonists of lysophosphatidic acid receptors |
| GB2474120B (en) * | 2009-10-01 | 2011-12-21 | Amira Pharmaceuticals Inc | Compounds as Lysophosphatidic acid receptor antagonists |
| GB2474748B (en) * | 2009-10-01 | 2011-10-12 | Amira Pharmaceuticals Inc | Polycyclic compounds as lysophosphatidic acid receptor antagonists |
| CN103347510B (zh) * | 2010-12-07 | 2015-11-25 | 艾米拉医药股份有限公司 | 溶血磷脂酸受体拮抗剂及其在治疗纤维化中的用途 |
| CN103596947A (zh) * | 2011-04-05 | 2014-02-19 | 艾米拉医药股份有限公司 | 用于治疗纤维化、疼痛、癌症和呼吸、过敏性、神经系统疾病或心血管疾病的基于3-或5-联苯-4-基异噁唑的化合物 |
| WO2012138648A1 (en) * | 2011-04-06 | 2012-10-11 | Irm Llc | Compositions and methods for modulating lpa receptors |
| US9526091B2 (en) * | 2012-03-16 | 2016-12-20 | Intel Corporation | Method and apparatus for coordination of self-optimization functions in a wireless network |
| WO2017086430A1 (ja) * | 2015-11-20 | 2017-05-26 | 宇部興産株式会社 | Ｎａｓｈの治療又は予防のための医薬組成物 |
-
2017
- 2017-09-04 WO PCT/CN2017/100354 patent/WO2019041340A1/en not_active Ceased
-
2018
- 2018-08-28 US US16/633,371 patent/US11365185B2/en active Active
- 2018-08-28 MX MX2020002430A patent/MX2020002430A/es unknown
- 2018-08-28 JP JP2020512678A patent/JP6854386B2/ja active Active
- 2018-08-28 EP EP18766481.8A patent/EP3679032B1/en active Active
- 2018-08-28 ES ES18766481T patent/ES2966827T3/es active Active
- 2018-08-28 KR KR1020207006096A patent/KR102341064B1/ko active Active
- 2018-08-28 WO PCT/US2018/048249 patent/WO2019046239A1/en not_active Ceased
- 2018-08-28 AU AU2018323969A patent/AU2018323969B2/en active Active
- 2018-08-28 CN CN201880053540.2A patent/CN111032647B/zh active Active
- 2018-08-28 CA CA3073983A patent/CA3073983C/en active Active
- 2018-08-28 EA EA202090368A patent/EA039482B1/ru unknown
-
2020
- 2020-02-25 SA SA520411406A patent/SA520411406B1/ar unknown
- 2020-03-01 IL IL273000A patent/IL273000B2/en unknown
-
2022
- 2022-05-18 US US17/747,261 patent/US12145924B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| IL273000A (en) | 2020-04-30 |
| EA039482B1 (ru) | 2022-02-01 |
| EA202090368A1 (ru) | 2020-06-09 |
| WO2019041340A1 (en) | 2019-03-07 |
| CN111032647A (zh) | 2020-04-17 |
| KR102341064B1 (ko) | 2021-12-20 |
| JP2020532550A (ja) | 2020-11-12 |
| IL273000B2 (en) | 2023-08-01 |
| US11365185B2 (en) | 2022-06-21 |
| MX2020002430A (es) | 2020-07-13 |
| CA3073983A1 (en) | 2019-03-07 |
| CN111032647B (zh) | 2023-05-02 |
| AU2018323969B2 (en) | 2020-07-16 |
| CA3073983C (en) | 2023-10-17 |
| EP3679032A1 (en) | 2020-07-15 |
| WO2019046239A1 (en) | 2019-03-07 |
| IL273000B1 (en) | 2023-04-01 |
| US20200231568A1 (en) | 2020-07-23 |
| AU2018323969A1 (en) | 2020-02-20 |
| EP3679032B1 (en) | 2023-10-04 |
| US12145924B2 (en) | 2024-11-19 |
| ES2966827T3 (es) | 2024-04-24 |
| SA520411406B1 (ar) | 2022-08-28 |
| BR112020002217A2 (pt) | 2020-07-28 |
| KR20200035440A (ko) | 2020-04-03 |
| US20220281845A1 (en) | 2022-09-08 |
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