JP2022507958A - 代謝障害の治療用のプロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）阻害薬としての環状四量体化合物 - Google Patents
代謝障害の治療用のプロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）阻害薬としての環状四量体化合物 Download PDFInfo
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- JP2022507958A JP2022507958A JP2021529268A JP2021529268A JP2022507958A JP 2022507958 A JP2022507958 A JP 2022507958A JP 2021529268 A JP2021529268 A JP 2021529268A JP 2021529268 A JP2021529268 A JP 2021529268A JP 2022507958 A JP2022507958 A JP 2022507958A
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- methyl
- benzyl
- chlorobenzyl
- phenoxy
- methoxymethyl
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- 0 CCC*(C)C(C([C@](C*)C(C)CC(*(C)C1(CC1)CC(C(CCC)C(*(CC)N)(C(*C)(C(C)*)*(C(C)C*)C(CC1)=O)O)=O)=*)O)*(C*)C1=O Chemical compound CCC*(C)C(C([C@](C*)C(C)CC(*(C)C1(CC1)CC(C(CCC)C(*(CC)N)(C(*C)(C(C)*)*(C(C)C*)C(CC1)=O)O)=O)=*)O)*(C*)C1=O 0.000 description 39
- XDTMQSROBMDMFD-UHFFFAOYSA-N C1CCCCC1 Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 description 2
- YXFVVABEGXRONW-UHFFFAOYSA-N Cc1ccccc1 Chemical compound Cc1ccccc1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 2
- FJXJUZCEJRNZLV-UHFFFAOYSA-N C=C[n]1c(-c2ccc(CCCc3ccccc3)cc2)cnc1C=O Chemical compound C=C[n]1c(-c2ccc(CCCc3ccccc3)cc2)cnc1C=O FJXJUZCEJRNZLV-UHFFFAOYSA-N 0.000 description 1
- BAFWNPCHALAUSM-LCYFTJDESA-N CC(C)(C)OC(N(C)/C(/CC(O)=O)=C\C1C=CC(Cl)=CC1)=O Chemical compound CC(C)(C)OC(N(C)/C(/CC(O)=O)=C\C1C=CC(Cl)=CC1)=O BAFWNPCHALAUSM-LCYFTJDESA-N 0.000 description 1
- KXVVBQVFWZFADQ-UHFFFAOYSA-N CC(C)(C)OC(N(C)CCN)=N Chemical compound CC(C)(C)OC(N(C)CCN)=N KXVVBQVFWZFADQ-UHFFFAOYSA-N 0.000 description 1
- MPYPTYYDLYVPDI-UHFFFAOYSA-N CC(c([n]1C)ncc1Br)N1CCCC1 Chemical compound CC(c([n]1C)ncc1Br)N1CCCC1 MPYPTYYDLYVPDI-UHFFFAOYSA-N 0.000 description 1
- XTJSZMAMNYEIHD-UHFFFAOYSA-N CCC(C)C(C)C(C)=N Chemical compound CCC(C)C(C)C(C)=N XTJSZMAMNYEIHD-UHFFFAOYSA-N 0.000 description 1
- WKMPCSCJXQRSSS-AATRIKPKSA-N CCC/C=C/B(O)[ClH]C Chemical compound CCC/C=C/B(O)[ClH]C WKMPCSCJXQRSSS-AATRIKPKSA-N 0.000 description 1
- QYYQTLLGVAPKPN-UHFFFAOYSA-N CCC1=CCCC1 Chemical compound CCC1=CCCC1 QYYQTLLGVAPKPN-UHFFFAOYSA-N 0.000 description 1
- QYSNETVLWGIEMW-UHFFFAOYSA-N CCCCCNCc1ccc[n]2c1ncc2Br Chemical compound CCCCCNCc1ccc[n]2c1ncc2Br QYSNETVLWGIEMW-UHFFFAOYSA-N 0.000 description 1
- PWUAKCZNWAGQBS-UHFFFAOYSA-N CCCCN(C)C1(CN)CC1 Chemical compound CCCCN(C)C1(CN)CC1 PWUAKCZNWAGQBS-UHFFFAOYSA-N 0.000 description 1
- ABVJTEADGCZQGR-JTQLQIEISA-N CN[C@H](CC(O)=O)Cc(cc1)ccc1Cl Chemical compound CN[C@H](CC(O)=O)Cc(cc1)ccc1Cl ABVJTEADGCZQGR-JTQLQIEISA-N 0.000 description 1
- BQHZQELTGXDDLO-UHFFFAOYSA-N Cc([n](C)c(C=O)n1)c1I Chemical compound Cc([n](C)c(C=O)n1)c1I BQHZQELTGXDDLO-UHFFFAOYSA-N 0.000 description 1
- DEZBDGYEBAASJG-UHFFFAOYSA-N Cc1ncc(-c(cc2)ccc2NCc2ccccc2)[n]1C Chemical compound Cc1ncc(-c(cc2)ccc2NCc2ccccc2)[n]1C DEZBDGYEBAASJG-UHFFFAOYSA-N 0.000 description 1
- YNDRMCGMKJHLMH-UHFFFAOYSA-N FCC[n]1c(-c(cc2)ccc2OCc2ccccc2)cnc1 Chemical compound FCC[n]1c(-c(cc2)ccc2OCc2ccccc2)cnc1 YNDRMCGMKJHLMH-UHFFFAOYSA-N 0.000 description 1
- NXHWREQSEHABDL-UHFFFAOYSA-N O=C(c1ccc[n]2c1ncc2Br)N1CCCC1 Chemical compound O=C(c1ccc[n]2c1ncc2Br)N1CCCC1 NXHWREQSEHABDL-UHFFFAOYSA-N 0.000 description 1
- VBVLABYWZYPGNO-UHFFFAOYSA-N [U]=C1OC[I](Cc2ccccc2)N1 Chemical compound [U]=C1OC[I](Cc2ccccc2)N1 VBVLABYWZYPGNO-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
- C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862772029P | 2018-11-27 | 2018-11-27 | |
| US62/772,029 | 2018-11-27 | ||
| US201962925108P | 2019-10-23 | 2019-10-23 | |
| US62/925,108 | 2019-10-23 | ||
| PCT/IB2019/060200 WO2020110008A1 (en) | 2018-11-27 | 2019-11-26 | Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022507958A true JP2022507958A (ja) | 2022-01-18 |
| JP2022507958A5 JP2022507958A5 (enExample) | 2022-11-29 |
Family
ID=68808459
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021529268A Pending JP2022507958A (ja) | 2018-11-27 | 2019-11-26 | 代謝障害の治療用のプロタンパク質転換酵素サブチリシン／ケキシン９型（ｐｃｓｋ９）阻害薬としての環状四量体化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20230089867A1 (enExample) |
| EP (1) | EP3887363A1 (enExample) |
| JP (1) | JP2022507958A (enExample) |
| CN (1) | CN113166101A (enExample) |
| WO (1) | WO2020110008A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021156792A1 (en) * | 2020-02-07 | 2021-08-12 | Novartis Ag | Targeted plasma protein degradation |
| CN116171161A (zh) * | 2020-08-25 | 2023-05-26 | 雷杰纳荣制药公司 | 用pcsk9和ldlr调节剂治疗败血症 |
| WO2022150768A1 (en) * | 2021-01-11 | 2022-07-14 | Children's Medical Center Corporation | Yap-tead inhibitors and uses thereof |
| CN114163343A (zh) * | 2021-12-10 | 2022-03-11 | 许昌学院 | 含氟氨基酸及衍生物含氟多肽的制备方法以及应用 |
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| US5120712A (en) | 1986-05-05 | 1992-06-09 | The General Hospital Corporation | Insulinotropic hormone |
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| US5114946A (en) | 1987-06-12 | 1992-05-19 | American Cyanamid Company | Transdermal delivery of pharmaceuticals |
| US4818541A (en) | 1987-08-19 | 1989-04-04 | Schering Corporation | Transdermal delivery of enantiomers of phenylpropanolamine |
| ATE164852T1 (de) | 1990-01-24 | 1998-04-15 | Douglas I Buckley | Glp-1-analoga verwendbar in der diabetesbehandlung |
| US5155100A (en) | 1991-05-01 | 1992-10-13 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipeptide derivatives |
| IL111785A0 (en) | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| US5705483A (en) | 1993-12-09 | 1998-01-06 | Eli Lilly And Company | Glucagon-like insulinotropic peptides, compositions and methods |
| US5512549A (en) | 1994-10-18 | 1996-04-30 | Eli Lilly And Company | Glucagon-like insulinotropic peptide analogs, compositions, and methods of use |
| DE122010000020I1 (de) | 1996-04-25 | 2010-07-08 | Prosidion Ltd | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
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| CN103748070B (zh) | 2011-05-31 | 2015-06-24 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| SMT201700306T1 (it) | 2012-06-08 | 2017-07-18 | Theravance Biopharma R&D Ip Llc | Inibitori di neprilisina |
| DE102012014480A1 (de) | 2012-07-21 | 2014-01-23 | Daimler Ag | Aufbau eines Innendekors |
| MX366149B (es) | 2012-08-08 | 2019-06-28 | Theravance Biopharma R&D Ip Llc | Inhibidores de neprilisina. |
| TR201808541T4 (tr) | 2013-02-14 | 2018-07-23 | Novartis Ag | Nep (nötr endopeptidaz) inhibitörleri olarak ikame edilmiş bisfenil butanoik fosfonik asit türevleri. |
| DK2964616T3 (en) | 2013-03-05 | 2017-08-28 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| CN105473141A (zh) * | 2013-03-15 | 2016-04-06 | 实发生物医学公司 | 治疗和/或预防心血管疾病的抗pcsk9化合物和方法 |
| CA2934936A1 (en) | 2014-01-30 | 2015-08-06 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| CA2934898A1 (en) | 2014-01-30 | 2015-08-06 | Theravance Biopharma R&D Ip, Llc | 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors |
-
2019
- 2019-11-26 JP JP2021529268A patent/JP2022507958A/ja active Pending
- 2019-11-26 EP EP19816904.7A patent/EP3887363A1/en not_active Withdrawn
- 2019-11-26 CN CN201980078050.2A patent/CN113166101A/zh active Pending
- 2019-11-26 US US17/296,895 patent/US20230089867A1/en not_active Abandoned
- 2019-11-26 WO PCT/IB2019/060200 patent/WO2020110008A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| WO2020110008A1 (en) | 2020-06-04 |
| CN113166101A (zh) | 2021-07-23 |
| US20230089867A1 (en) | 2023-03-23 |
| EP3887363A1 (en) | 2021-10-06 |
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