CA3004714A1 - Fragment synthesis of cyclic peptides - Google Patents

Fragment synthesis of cyclic peptides Download PDF

Info

Publication number
CA3004714A1
CA3004714A1 CA3004714A CA3004714A CA3004714A1 CA 3004714 A1 CA3004714 A1 CA 3004714A1 CA 3004714 A CA3004714 A CA 3004714A CA 3004714 A CA3004714 A CA 3004714A CA 3004714 A1 CA3004714 A1 CA 3004714A1
Authority
CA
Canada
Prior art keywords
aryl
compound
lower alkyl
amino acid
formula
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
Application number
CA3004714A
Other languages
English (en)
French (fr)
Inventor
Manuel Perez VAZQUEZ
M. Monzur MORSHED
Jennifer L. HICKEY
Marc-Andre Poupart
Gaoqiang Yang
James Gillard
Adam Paul KAFAL
Andrew L. Roughton
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Universite de Montreal
Zealand Pharma AS
Original Assignee
Universite de Montreal
Encycle Therapeutics Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Universite de Montreal, Encycle Therapeutics Inc filed Critical Universite de Montreal
Publication of CA3004714A1 publication Critical patent/CA3004714A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/18—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1075—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of amino acids or peptide residues
    • 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
    • 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
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Analytical Chemistry (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
CA3004714A 2015-11-11 2016-11-14 Fragment synthesis of cyclic peptides Pending CA3004714A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562254003P 2015-11-11 2015-11-11
US62/254,003 2015-11-11
PCT/CA2016/000275 WO2017079821A1 (en) 2015-11-11 2016-11-14 Fragment synthesis of cyclic peptides

Publications (1)

Publication Number Publication Date
CA3004714A1 true CA3004714A1 (en) 2017-05-18

Family

ID=58694457

Family Applications (2)

Application Number Title Priority Date Filing Date
CA3004714A Pending CA3004714A1 (en) 2015-11-11 2016-11-14 Fragment synthesis of cyclic peptides
CA3004641A Pending CA3004641A1 (en) 2015-11-11 2016-11-14 Cyclic peptides targeting .alpha.4.beta.7 integrin

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA3004641A Pending CA3004641A1 (en) 2015-11-11 2016-11-14 Cyclic peptides targeting .alpha.4.beta.7 integrin

Country Status (8)

Country Link
US (4) US11046695B2 (enExample)
EP (2) EP3377471A4 (enExample)
JP (1) JP6961586B2 (enExample)
KR (1) KR102867019B1 (enExample)
CN (2) CN109071602B (enExample)
AU (1) AU2016353547B9 (enExample)
CA (2) CA3004714A1 (enExample)
WO (2) WO2017079821A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3004714A1 (en) 2015-11-11 2017-05-18 Encycle Therapeutics, Inc. Fragment synthesis of cyclic peptides
EP3939989A1 (en) 2016-11-11 2022-01-19 Zealand Pharma A/S Cyclic peptides multimers targeting alpha 4beta 7 integrin
KR20200015540A (ko) 2017-05-10 2020-02-12 인사이클 세라퓨틱스, 인코포레이티드 α4β7 인테그린을 타겟팅하는 호모데틱 사이클릭 펩타이드
CN110551178B (zh) * 2018-06-01 2020-07-21 深圳翰宇药业股份有限公司 一种含脯氨酸的首尾环肽合成方法
WO2020185999A1 (en) 2019-03-14 2020-09-17 Genentech, Inc. Cyclic peptide antibiotics
JP2021106565A (ja) * 2019-12-27 2021-07-29 国立大学法人 東京大学 ライブラリーの製造方法、環状ペプチド、ＦＸＩＩａ結合剤、及びＩＦＮＧＲ１結合剤
WO2021132661A1 (ja) * 2019-12-27 2021-07-01 国立大学法人東京大学 ライブラリーの製造方法、環状ペプチド、ＦＸＩＩａ結合剤、及びＩＦＮＧＲ１結合剤
US20230295235A1 (en) 2020-06-29 2023-09-21 Zealand Pharma A/S Compounds targeting alpha4-beta7 integrin
WO2023118049A1 (en) 2021-12-20 2023-06-29 Zealand Pharma A/S Compounds

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3219113A1 (de) * 1982-05-21 1983-11-24 Bayer Ag, 5090 Leverkusen Verwendung von n-substituierten 2,3-diaminocarbonsaeuren in arzneimitteln und ihre herstellung
ZA906188B (en) 1989-08-10 1991-06-26 Merrell Dow Pharma Cyclic neurokinin a antagonists
US5296604A (en) 1992-05-15 1994-03-22 Miles Inc. Proline derivatives and compositions for their use as inhibitors of HIV protease
US5705481A (en) 1992-11-06 1998-01-06 Merck Patent Gesellschaft Mit Beschrankter Haftung Cyclopeptides
IL109615A (en) 1993-05-17 2000-12-06 Fujisawa Pharmaceutical Co Cyclic polypeptide derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
US5693325A (en) 1994-03-15 1997-12-02 Molecumetics, Ltd. Peptide vaccines and methods relating thereto
DE4415310A1 (de) 1994-04-30 1995-11-02 Merck Patent Gmbh Cyclopeptide
GB9524630D0 (en) * 1994-12-24 1996-01-31 Zeneca Ltd Chemical compounds
US5696084A (en) 1996-08-16 1997-12-09 Abbott Laboratories Amino-lipopetide antifungal agents
US6492553B1 (en) 1998-01-29 2002-12-10 Aventis Pharamaceuticals Inc. Methods for preparing N-[(aliphatic or aromatic)carbonyl)]-2-aminoaetamide compounds and for cyclizing such compounds
DE10107707A1 (de) * 2001-02-19 2002-08-29 Wilex Biotechnology Gmbh Antagonisten für alpha¶4¶beta¶7¶-Integrin
US6667407B2 (en) 2002-05-03 2003-12-23 Bayer Polymers Llc Process of making polyaziridines
SG185306A1 (en) 2004-04-15 2012-11-29 Onyx Therapeutics Inc Compounds for proteasome enzyme inhibition
WO2008046232A1 (en) 2006-10-20 2008-04-24 Yudin Andrei K Aziridine aldehydes, aziridine-conjugated amino derivatives, aziridine-conjugated biomolecules and processes for their preparation
EP1961759A1 (en) * 2007-02-21 2008-08-27 Universita'degli Studi Di Milano Integrin targeted cyclopeptide ligands, their preparation and use
US9243030B2 (en) 2008-05-22 2016-01-26 Centre National De La Recherche Scientifique (Cnrs) Optically pure compounds for improved therapeutic efficiency
DK2408802T3 (en) 2009-03-16 2017-08-28 Governing Council Univ Toronto CYCLIC AMINO ACID MOLECULES AND PROCEDURES FOR PREPARING IT
US20120045393A1 (en) 2009-03-17 2012-02-23 Linder Karen E Lhrh-ii peptide analogs
EP2556060A1 (en) 2010-04-08 2013-02-13 Ah Usa 42 Llc Substituted 3,5- diphenyl-isoxazoline derivatives as insecticides and acaricides
US9238056B2 (en) * 2011-02-22 2016-01-19 Leo Pharma A/S Cyclic peptide and conjugate thereof for binding to keratinocytes
US9273093B2 (en) 2012-10-11 2016-03-01 Protagonist Therapeutics, Inc. α4β7 peptide dimer antagonists
CA2962642A1 (en) 2014-10-01 2016-04-07 Protagonist Therapeutics, Inc. Novel .alpha.4.beta.7 peptide monomer and dimer antagonists
US10301371B2 (en) 2014-10-01 2019-05-28 Protagonist Therapeutics, Inc. Cyclic monomer and dimer peptides having integrin antagonist activity
US10281407B2 (en) 2015-11-02 2019-05-07 Jon A. Petty Multi-fluid strip test
CA3004714A1 (en) 2015-11-11 2017-05-18 Encycle Therapeutics, Inc. Fragment synthesis of cyclic peptides

Also Published As

Publication number Publication date
US11046695B2 (en) 2021-06-29
US20200361944A1 (en) 2020-11-19
EP3387004A1 (en) 2018-10-17
CA3004641A1 (en) 2017-05-18
US11072616B2 (en) 2021-07-27
EP3387004B1 (en) 2021-10-06
EP3377471A4 (en) 2019-11-20
EP3387004A4 (en) 2019-11-20
AU2016353547B2 (en) 2020-08-06
US10981921B2 (en) 2021-04-20
US20210300932A1 (en) 2021-09-30
KR20180095809A (ko) 2018-08-28
CN109071430A (zh) 2018-12-21
CN109071602A (zh) 2018-12-21
JP6961586B2 (ja) 2021-11-05
JP2019503340A (ja) 2019-02-07
US20200165300A1 (en) 2020-05-28
KR102867019B1 (ko) 2025-09-30
AU2016353547B9 (en) 2020-12-03
AU2016353547A1 (en) 2018-06-28
WO2017079821A1 (en) 2017-05-18
WO2017079820A1 (en) 2017-05-18
US20190077805A1 (en) 2019-03-14
CN109071602B (zh) 2022-09-13
EP3377471A1 (en) 2018-09-26

Similar Documents

Publication Publication Date Title
CA3004714A1 (en) Fragment synthesis of cyclic peptides
KR101467598B1 (ko) Ｈｃｖ 프로테아제 억제제 중간체의 제조방법
CA2621360C (en) Ring-closing metathesis process for the preparation of macrocyclic peptides
EP3778621A1 (en) Peptide synthesis method
KR20100045992A (ko) Ｃ형 간염을 치료하는 데 유용한 화합물의 합성 방법
US6716866B2 (en) Aryl-benzimidazole compounds having antiinfective activity
WO2012051405A1 (en) Methods for preparing macrocycles and macrocycle stabilized peptides
KR102303092B1 (ko) 합성 펜타펩티드의 제조법
JP2023052381A (ja) 液相ペプチド合成のための方法およびその保護戦略
Ivanov et al. A convergent approach to synthesis of bortezomib: the use of TBTU suppresses racemization in the fragment condensation
CN101270153B (zh) 一种环五肽及其合成方法
AU2002310004B2 (en) Uronium and immonium salts for peptide coupling
EP3924330A1 (en) Method of preparing a don prodrug from l-glutamic acid
AU2002310004A1 (en) Uronium and immonium salts for peptide coupling
CN110423265A (zh) 一种环肽类trf2抑制剂的制备方法和用途
EP3986400B1 (en) Processes and intermediates for producing diazaspiro lactam compounds
CA3029584A1 (en) Process for preparation of icatibant acetate
CN117003791B (zh) 一种二苯基膦酰氧基双酚a类化合物及其制备美白九肽-1中的应用
US20030130198A1 (en) Halogen-substitued thienyl compounds
JP7640994B2 (ja) ペプチド合成法
US8674020B2 (en) Process for preparing polyamides
Abdelbaky et al. Synthesis of α-(R)-/γ-(S)-Dimethyl Substituted Peptide Nucleic Acid Submonomer Using Mitsunobu Reaction
Ferron et al. Design and scalable synthesis of new chiral selectors. Part 1: Synthesis and characterization of a new constrained cyclopeptide from unnatural bulky amino acids
CN117279928A (zh) 包含n-取代氨基酸残基的环状化合物的制备方法
David et al. Polysubstituted cyclohexane γ-amino acids induce a double α-/β-turn in short non-natural peptides

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20211014

EEER Examination request

Effective date: 20211014

EEER Examination request

Effective date: 20211014

EEER Examination request

Effective date: 20211014

EEER Examination request

Effective date: 20211014

EEER Examination request

Effective date: 20211014

EEER Examination request

Effective date: 20211014

EEER Examination request

Effective date: 20211014

EEER Examination request

Effective date: 20211014