CN108699105A - 作为htra1抑制剂的新型二氟酮酰胺衍生物 - Google Patents

作为htra1抑制剂的新型二氟酮酰胺衍生物 Download PDF

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Publication number
CN108699105A
CN108699105A CN201780012559.8A CN201780012559A CN108699105A CN 108699105 A CN108699105 A CN 108699105A CN 201780012559 A CN201780012559 A CN 201780012559A CN 108699105 A CN108699105 A CN 108699105A
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CN
China
Prior art keywords
amino
difluoro
methyl
methoxyphenyl
trifluoroethylamino
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Pending
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CN201780012559.8A
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English (en)
Chinese (zh)
Inventor
汉斯·P·梅尔基
佰努瓦·霍恩斯普格
彼得·莫尔
米夏埃尔·罗伊特林格
罗伯托·亚科内
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication of CN108699105A publication Critical patent/CN108699105A/zh
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (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)
CN201780012559.8A 2016-03-04 2017-03-01 作为htra1抑制剂的新型二氟酮酰胺衍生物 Pending CN108699105A (zh)

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 (1)

Publication Number Publication Date
CN108699105A true CN108699105A (zh) 2018-10-23

Family

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Family Applications (1)

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CN201780012559.8A Pending CN108699105A (zh) 2016-03-04 2017-03-01 作为htra1抑制剂的新型二氟酮酰胺衍生物

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=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109709227A (zh) * 2018-12-30 2019-05-03 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

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Publication number Priority date Publication date Assignee Title
PL3472149T3 (pl) 2016-06-21 2024-02-12 Orion Ophthalmology LLC Heterocykliczne pochodne prolinamidu
US10526315B2 (en) 2016-06-21 2020-01-07 Orion Ophthalmology LLC Carbocyclic prolinamide derivatives
UY38911A (es) 2019-10-09 2021-05-31 Bayer Ag Compuestos de heteroarilo-triazol como pesticidas, formulaciones, usos y métodos de uso de los mismos

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WO2008101160A2 (en) * 2007-02-16 2008-08-21 Genentech, Inc. Htra1-pdz and htra3-pdz modulators
WO2016180751A1 (en) * 2015-05-11 2016-11-17 F. Hoffmann-La Roche Ag New difluoroketamide derivatives

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AU711035B2 (en) 1994-07-15 1999-10-07 Merrell Pharmaceuticals Inc. Difluorostatone antiviral agents
ES2234144T3 (es) 1997-08-11 2005-06-16 Boehringer Ingelheim (Canada) Ltd. Analogos de peptidos inhibidores de la hepatitis c.
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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
TWI359147B (en) 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
WO2006050862A1 (en) * 2004-11-10 2006-05-18 Boehringer Ingelheim International Gmbh Statine derivatives for the treatment of alzheimer's disease
US20110207704A1 (en) 2006-12-15 2011-08-25 Abbott Laboratories Novel Oxadiazole Compounds
US8377886B2 (en) * 2007-09-14 2013-02-19 Albert Einstein College Of Medicine Of Yeshiva University Use of gamma secretase inhibitors and notch pathway inhibitors for treatment and prevention of renal disease
PT2661433T (pt) 2011-01-04 2017-10-24 Novartis Ag Compostos de indole ou seus análogos úteis para o tratamento da degeneração macular relacionada com a idade (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
CN107207421B (zh) * 2015-02-25 2021-04-20 豪夫迈·罗氏有限公司 新的三氟甲基丙酰胺衍生物

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WO2008101160A2 (en) * 2007-02-16 2008-08-21 Genentech, Inc. Htra1-pdz and htra3-pdz modulators
WO2016180751A1 (en) * 2015-05-11 2016-11-17 F. Hoffmann-La Roche Ag New difluoroketamide derivatives

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109709227A (zh) * 2018-12-30 2019-05-03 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
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

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Publication number Publication date
US20180371015A1 (en) 2018-12-27
JP2019507176A (ja) 2019-03-14
US11059858B2 (en) 2021-07-13
WO2017148967A1 (en) 2017-09-08
EP3423467B1 (en) 2021-04-28
EP3423467A1 (en) 2019-01-09
HK1257567A1 (zh) 2019-10-25

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