WO2008104000A2 - Triazole macrocycle systems - Google Patents

Triazole macrocycle systems Download PDF

Info

Publication number
WO2008104000A2
WO2008104000A2 PCT/US2008/054922 US2008054922W WO2008104000A2 WO 2008104000 A2 WO2008104000 A2 WO 2008104000A2 US 2008054922 W US2008054922 W US 2008054922W WO 2008104000 A2 WO2008104000 A2 WO 2008104000A2
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
macrocycle
methyl
compound
peptidomimetic
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
Application number
PCT/US2008/054922
Other languages
English (en)
French (fr)
Other versions
WO2008104000A3 (en
Inventor
Huw M. Nash
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.)
Rein Therapeutics Inc
Original Assignee
Aileron 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
Priority to CA2678941A priority Critical patent/CA2678941C/en
Priority to AU2008218116A priority patent/AU2008218116B2/en
Priority to BRPI0807578-6A priority patent/BRPI0807578A2/pt
Priority to CN200880009510.8A priority patent/CN101663044B/zh
Priority to ES08730678T priority patent/ES2398310T3/es
Priority to EP08730678A priority patent/EP2114428B1/en
Priority to JP2009551061A priority patent/JP4997293B2/ja
Application filed by Aileron Therapeutics Inc filed Critical Aileron Therapeutics Inc
Publication of WO2008104000A2 publication Critical patent/WO2008104000A2/en
Publication of WO2008104000A3 publication Critical patent/WO2008104000A3/en
Priority to IL200532A priority patent/IL200532A/en
Anticipated expiration legal-status Critical
Priority to IL241729A priority patent/IL241729A/en
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • 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
    • A61P35/00—Antineoplastic 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
    • C07C271/22—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
    • 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
    • C07K1/006—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length of peptides containing derivatised side chain amino acids
    • 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
    • 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
    • C07K1/113—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 without change of the primary structure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4748—Tumour specific antigens; Tumour rejection antigen precursors [TRAP], e.g. MAGE
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K4/00—Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
    • 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
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • 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
    • 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

Definitions

  • Ri and R 2 are independently -H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroalkyl, or heterocycloalkyl, unsubstituted or substituted with halo-;
  • a secondary structure of the peptidomimetic macrocycle is more stable than a corresponding secondary structure of a corresponding non-macrocyclic polypeptide.
  • the peptidomimetic macrocycle comprises an ⁇ -helix.
  • the ⁇ -helix may comprise, for example, from 1 turn to 5 turns.
  • the ⁇ -helix is more stable than an ⁇ -helix of a corresponding non-macrocyclic polypeptide.
  • the macrocycle-forming linker may span, or examp e, om turn to 5 turns o t e ⁇ - e x, suc as approximately 1, 2, 3, 4 or 5 turns of the ⁇ -helix.
  • K is O, S, SO, SO 2 , CO, CO 2 , or CONR 3 ;
  • R 4 is alkylene, alkenylene, alkynylene, heteroalkylene, cycloalkylene, heterocycloalkylene, arylene, or heteroarylene; each R 5 is independently halogen, alkyl, -OR 6 , -N(Re) 2 , -SR 6 , -SOR 6 , -SO 2 R 6 , -CO 2 R 6 , a fluorescent moiety, a radioisotope or a therapeutic agent; each R 6 is independently -H, alkyl, alkenyl, alkynyl, arylalkyl, cycloalkylalkyl, heterocycloalkyl, a fluorescent moiety, a radioisotope or a therapeutic agent;
  • compositions of this invention comprise a combination of a peptidomimetic macrocycle and one or more additional therapeutic or prophylactic agents
  • both the compound and the additional agent should be present at dosage levels of between about 1 to 100%, and more preferably between about 5 to 95% of the dosage normally administered in a monotherapy regimen.
  • the additional agents are administered separately, as part of a multiple dose regimen, from the compounds of this invention.
  • those agents are part of a single dosage form, mixed together with the compounds of this invention in a single composition.
  • metastatic tumor can arise from a multitude of primary tumor types, including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • Primary tumor types including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • Primary tumor types including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • Primary tumor types including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • Primary tumor growth including but not limited to those of breast, lung, liver, colon and ovarian origin.
  • “Pathologic hyperproliferative" cells occur in disease states characterized by malignant tumor growth.
  • non-pathologic hyperproliferative cells include proliferation of cells associated with wound repair.
  • cellular proliferative and/or differentiative disorders include cancer, e.g., carcinoma, sarcoma, or metastatic disorders.
  • the peptidomimetics macrocycles are novel therapeutic agents for controlling breast cancer, ovarian cancer, colon cancer, lung cancer, metastasis

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Analytical Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
PCT/US2008/054922 2007-02-23 2008-02-25 Triazole macrocycle systems Ceased WO2008104000A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
AU2008218116A AU2008218116B2 (en) 2007-02-23 2008-02-25 Triazole macrocycle systems
BRPI0807578-6A BRPI0807578A2 (pt) 2007-02-23 2008-02-25 macrociclo peptidomimético, composto, kit e métodos para sintetizar um macrociclo peptidomimético
CN200880009510.8A CN101663044B (zh) 2007-02-23 2008-02-25 三唑大环系统
ES08730678T ES2398310T3 (es) 2007-02-23 2008-02-25 Péptidos macrocíclicos unidos a triazol
EP08730678A EP2114428B1 (en) 2007-02-23 2008-02-25 Triazole linked macrocyclic peptides
CA2678941A CA2678941C (en) 2007-02-23 2008-02-25 Triazole macrocycle systems
JP2009551061A JP4997293B2 (ja) 2007-02-23 2008-02-25 トリアゾール大環状系
IL200532A IL200532A (en) 2007-02-23 2009-08-20 Macrocyclic systems including triazole and a method for their preparation
IL241729A IL241729A (en) 2007-02-23 2015-09-20 Triazole macrocyclization systems

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US90307307P 2007-02-23 2007-02-23
US60/903,073 2007-02-23

Publications (2)

Publication Number Publication Date
WO2008104000A2 true WO2008104000A2 (en) 2008-08-28
WO2008104000A3 WO2008104000A3 (en) 2008-11-27

Family

ID=39710801

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/054922 Ceased WO2008104000A2 (en) 2007-02-23 2008-02-25 Triazole macrocycle systems

Country Status (10)

Country Link
US (6) US7981999B2 (https=)
EP (4) EP2114428B1 (https=)
JP (2) JP4997293B2 (https=)
CN (3) CN104086641A (https=)
AU (1) AU2008218116B2 (https=)
BR (1) BRPI0807578A2 (https=)
CA (1) CA2678941C (https=)
ES (3) ES2398310T3 (https=)
IL (2) IL200532A (https=)
WO (1) WO2008104000A2 (https=)

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WO2010034028A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic marcrocycles
WO2010034029A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034026A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034031A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010034034A1 (en) * 2008-09-22 2010-03-25 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
WO2010099436A1 (en) * 2009-02-27 2010-09-02 Mimetogen Pharmaceuticals, Inc. Methods of treating retinitis pigmentosa
WO2011058188A1 (en) * 2009-11-16 2011-05-19 Centre National De La Recherche Scientifique - Cnrs - Compounds and methods for purifying peptides produced by solid phase peptide synthesis
EP2285970A4 (en) * 2008-06-03 2011-10-12 Aileron Therapeutics Inc COMPOSITIONS AND METHODS FOR REINFORCING THE CELL TRANSPORT OF BIOMOLECULES
EP2334317A4 (en) * 2008-09-16 2012-03-14 Univ New York State Res Found CLAMPED PEPTIDES AND METHOD OF COMPOSITION
EP2242503A4 (en) * 2008-02-08 2012-04-25 Aileron Therapeutics Inc THERAPEUTIC PEPTIDOMIMETIC MACROCYCLES
JP2012515172A (ja) * 2009-01-14 2012-07-05 エルロン・セラピューティクス・インコーポレイテッド ペプチド模倣大環状分子
JP2012515709A (ja) * 2009-01-23 2012-07-12 パシフィック・サイエンティフィック・エナジェティック・マテリアルズ・カンパニー 鉛フリー起爆薬の調合
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US8859723B2 (en) * 2010-08-13 2014-10-14 Aileron Therapeutics, Inc. Peptidomimetic macrocycles
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US9604919B2 (en) 2012-11-01 2017-03-28 Aileron Therapeutics, Inc. Disubstituted amino acids and methods of preparation and use thereof
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