JP2019507176A - Ｈｔｒａ１阻害剤としての新規ジフルオロケタミド誘導体 - Google Patents
Ｈｔｒａ１阻害剤としての新規ジフルオロケタミド誘導体 Download PDFInfo
- Publication number
- JP2019507176A JP2019507176A JP2018546501A JP2018546501A JP2019507176A JP 2019507176 A JP2019507176 A JP 2019507176A JP 2018546501 A JP2018546501 A JP 2018546501A JP 2018546501 A JP2018546501 A JP 2018546501A JP 2019507176 A JP2019507176 A JP 2019507176A
- Authority
- JP
- Japan
- Prior art keywords
- amino
- difluoro
- methyl
- methoxyphenyl
- dioxo
- 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.)
- Ceased
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- 0 CC(*)(*C(C(C(*)*)N(*)C(*)=O)=O)C(N(*)C(C)(*)C(C(C(**)=O)(F)F)=O)=O Chemical compound CC(*)(*C(C(C(*)*)N(*)C(*)=O)=O)C(N(*)C(C)(*)C(C(C(**)=O)(F)F)=O)=O 0.000 description 2
- CJBXPBGSXBOTQC-QFIPXVFZSA-N CC(C)(C)OC(COc1ccc(C[C@@H](C(OCc2ccccc2)=O)NC(OC(C)(C)C)=O)cc1)=O Chemical compound CC(C)(C)OC(COc1ccc(C[C@@H](C(OCc2ccccc2)=O)NC(OC(C)(C)C)=O)cc1)=O CJBXPBGSXBOTQC-QFIPXVFZSA-N 0.000 description 1
- XOESAIJAFGHCDL-ZLBDCPSSSA-N CC(C)[C@@H](C(C(C(NCC(F)(F)F)=O)(F)F)=O)NC(C(c(cc1)ccc1OC)NC([C@H](Cc1ccc(CN)cc1)NC(c1cc(Cl)ccc1)=O)=O)=O Chemical compound CC(C)[C@@H](C(C(C(NCC(F)(F)F)=O)(F)F)=O)NC(C(c(cc1)ccc1OC)NC([C@H](Cc1ccc(CN)cc1)NC(c1cc(Cl)ccc1)=O)=O)=O XOESAIJAFGHCDL-ZLBDCPSSSA-N 0.000 description 1
- SBSAFGQHTDAWEI-ZXRKZBAXSA-N CC(C)[C@@H](C(C(C(NCC(F)(F)F)=O)(F)F)=O)NC([C@H](c(cc1)ccc1OC)NC([C@H](Cc(cc1)ccc1OCC(O)=O)NC(C(c1cccc(Cl)c1)(F)F)=O)=O)=O Chemical compound CC(C)[C@@H](C(C(C(NCC(F)(F)F)=O)(F)F)=O)NC([C@H](c(cc1)ccc1OC)NC([C@H](Cc(cc1)ccc1OCC(O)=O)NC(C(c1cccc(Cl)c1)(F)F)=O)=O)=O SBSAFGQHTDAWEI-ZXRKZBAXSA-N 0.000 description 1
- DFKSWVKYZQQDRC-VYCPFJESSA-N CC(C)[C@@H](C(C(C(NCC(F)(F)F)=O)(F)F)=O)NC([C@H](c1ccccc1)NC(C(Cc1cccc(Cl)c1)NC(c1cncnc1)=O)=O)=O Chemical compound CC(C)[C@@H](C(C(C(NCC(F)(F)F)=O)(F)F)=O)NC([C@H](c1ccccc1)NC(C(Cc1cccc(Cl)c1)NC(c1cncnc1)=O)=O)=O DFKSWVKYZQQDRC-VYCPFJESSA-N 0.000 description 1
- NFIGOYFHZHJJJR-HSQYWUDLSA-N CC(C)[C@@H](C(C(C(NCC(F)(F)F)=O)(F)F)=O)NC([C@H](c1ccccc1)NC([C@H](C)NC(C1(CC1)c1cccc(Cl)c1)=O)=O)=O Chemical compound CC(C)[C@@H](C(C(C(NCC(F)(F)F)=O)(F)F)=O)NC([C@H](c1ccccc1)NC([C@H](C)NC(C1(CC1)c1cccc(Cl)c1)=O)=O)=O NFIGOYFHZHJJJR-HSQYWUDLSA-N 0.000 description 1
- LOBFDOHSXOXRKX-CWBXHPNXSA-N CC(C)[C@@H]([C@H](C(C(NCC(F)(F)F)=O)(F)F)O)NC([C@H](c(cc1)ccc1OC)NC([C@H](Cc1cc(C#N)ccc1)N)=O)=O Chemical compound CC(C)[C@@H]([C@H](C(C(NCC(F)(F)F)=O)(F)F)O)NC([C@H](c(cc1)ccc1OC)NC([C@H](Cc1cc(C#N)ccc1)N)=O)=O LOBFDOHSXOXRKX-CWBXHPNXSA-N 0.000 description 1
- PMHITJJFLZOLOY-MYGLTJDJSA-N CC(C)[C@@H]([C@H](C(C(NCC(F)(F)F)=O)(F)F)O)NC([C@H](c(cc1)ccc1OC)NC([C@H](Cc1cc(F)ccc1)N)=O)=O Chemical compound CC(C)[C@@H]([C@H](C(C(NCC(F)(F)F)=O)(F)F)O)NC([C@H](c(cc1)ccc1OC)NC([C@H](Cc1cc(F)ccc1)N)=O)=O PMHITJJFLZOLOY-MYGLTJDJSA-N 0.000 description 1
- ZDNKUWIFZCNSNC-UHFFFAOYSA-N Cc1cccc(CC(C(O)=O)NC(c2ccccc2)=O)c1 Chemical compound Cc1cccc(CC(C(O)=O)NC(c2ccccc2)=O)c1 ZDNKUWIFZCNSNC-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/0606—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing heteroatoms not provided for by C07K5/06086 - C07K5/06139, e.g. Ser, Met, Cys, Thr
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0815—Tripeptides with the first amino acid being basic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0819—Tripeptides with the first amino acid being acidic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
- C07K5/1008—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine 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 |
|---|---|---|---|
| EP16158644.1 | 2016-03-04 | ||
| EP16158644 | 2016-03-04 | ||
| PCT/EP2017/054682 WO2017148967A1 (en) | 2016-03-04 | 2017-03-01 | New difluoroketamide derivatives as htra1 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019507176A true JP2019507176A (ja) | 2019-03-14 |
| JP2019507176A5 JP2019507176A5 (https=) | 2020-04-09 |
Family
ID=55456685
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018546501A Ceased JP2019507176A (ja) | 2016-03-04 | 2017-03-01 | Ｈｔｒａ１阻害剤としての新規ジフルオロケタミド誘導体 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11059858B2 (https=) |
| EP (1) | EP3423467B1 (https=) |
| JP (1) | JP2019507176A (https=) |
| CN (1) | CN108699105A (https=) |
| HK (1) | HK1257567A1 (https=) |
| WO (1) | WO2017148967A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE064412T2 (hu) | 2016-06-21 | 2024-03-28 | Orion Ophthalmology LLC | Heterociklusos prolinamid-származékok |
| JP7164521B2 (ja) | 2016-06-21 | 2022-11-01 | オリオン・オフサルモロジー・エルエルシー | 炭素環式プロリンアミド誘導体 |
| CN109709227B (zh) * | 2018-12-30 | 2021-09-24 | 中国水产科学研究院长江水产研究所 | 高效液相色谱-串联质谱测定水产品中盐酸氯苯胍及其代谢物残留量的方法 |
| TW202128664A (zh) | 2019-10-09 | 2021-08-01 | 德商拜耳廠股份有限公司 | 作為除害劑之新穎雜芳基三唑化合物 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060100158A1 (en) * | 2004-11-10 | 2006-05-11 | Boehringer Ingelheim International Gmbh | Statine derivatives for the treatment of Alzheimer's disease III |
| US20100222283A1 (en) * | 2007-09-14 | 2010-09-02 | Katalin Susztak | Use of gamma secretase inhibitors and notch pathway inhibitors for treatment and prevention of renal desease |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1986006379A1 (en) * | 1985-04-19 | 1986-11-06 | The Upjohn Company | Dihalo-statine substituted renin inhibitors |
| JPH10505582A (ja) | 1994-07-15 | 1998-06-02 | メリル・フアーマシユウテイカルズ・インコーポレイテツド | ジフルオロスタトン抗ウイルス剤 |
| EP1012180B1 (en) | 1997-08-11 | 2004-12-01 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis c inhibitor peptide analogues |
| CN1176941C (zh) | 1999-04-09 | 2004-11-24 | 西托维亚公司 | Caspase抑制剂及其应用 |
| SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
| US7244815B2 (en) | 2001-05-23 | 2007-07-17 | The Curators Of The University Of Missouri | Attachment and elaboration strategies for inverse peptide synthesis |
| UY28500A1 (es) | 2003-09-05 | 2005-04-29 | Vertex Pharma | Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc. |
| US20110207704A1 (en) | 2006-12-15 | 2011-08-25 | Abbott Laboratories | Novel Oxadiazole Compounds |
| PE20081795A1 (es) * | 2007-02-16 | 2009-01-08 | Genentech Inc | Moduladores de htra1-pdz y htra3-pdz |
| EP2661433B1 (en) | 2011-01-04 | 2017-08-16 | Novartis AG | Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd) |
| ES2644700T3 (es) | 2012-06-28 | 2017-11-30 | Novartis Ag | Derivados de pirrolidina y su uso como moduladores de la ruta del complemento |
| WO2016100555A1 (en) | 2014-12-18 | 2016-06-23 | Inception 4, Inc. | Boronic acid derivatives and uses thereof |
| EP3262026B1 (en) * | 2015-02-25 | 2020-03-18 | H. Hoffnabb-La Roche Ag | New trifluoromethylpropanamide derivatives |
| TW201713613A (zh) * | 2015-05-11 | 2017-04-16 | 赫孚孟拉羅股份公司 | 新二氟酮醯胺衍生物 |
-
2017
- 2017-03-01 EP EP17707875.5A patent/EP3423467B1/en active Active
- 2017-03-01 HK HK18116652.5A patent/HK1257567A1/zh unknown
- 2017-03-01 WO PCT/EP2017/054682 patent/WO2017148967A1/en not_active Ceased
- 2017-03-01 CN CN201780012559.8A patent/CN108699105A/zh active Pending
- 2017-03-01 JP JP2018546501A patent/JP2019507176A/ja not_active Ceased
-
2018
- 2018-09-04 US US16/121,244 patent/US11059858B2/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060100158A1 (en) * | 2004-11-10 | 2006-05-11 | Boehringer Ingelheim International Gmbh | Statine derivatives for the treatment of Alzheimer's disease III |
| US20100222283A1 (en) * | 2007-09-14 | 2010-09-02 | Katalin Susztak | Use of gamma secretase inhibitors and notch pathway inhibitors for treatment and prevention of renal desease |
Non-Patent Citations (3)
| Title |
|---|
| BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 24, JPN6021009652, 2014, pages 3582 - 3586, ISSN: 0004468264 * |
| JOURNAL OF MEDICINAL CHEMISTRY, vol. 40, no. 25, JPN6021009655, 1997, pages 4113 - 4135, ISSN: 0004468265 * |
| PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, vol. 86, JPN6021009657, 1989, pages 9752 - 9756, ISSN: 0004468266 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3423467B1 (en) | 2021-04-28 |
| HK1257567A1 (zh) | 2019-10-25 |
| WO2017148967A1 (en) | 2017-09-08 |
| EP3423467A1 (en) | 2019-01-09 |
| US11059858B2 (en) | 2021-07-13 |
| US20180371015A1 (en) | 2018-12-27 |
| CN108699105A (zh) | 2018-10-23 |
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