WO2019051198A1 - Inhibiteurs de promédicaments d'indoléamine 2,3-dioxygénase-1 (jdo1) - Google Patents

Inhibiteurs de promédicaments d'indoléamine 2,3-dioxygénase-1 (jdo1) Download PDF

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Publication number
WO2019051198A1
WO2019051198A1 PCT/US2018/049906 US2018049906W WO2019051198A1 WO 2019051198 A1 WO2019051198 A1 WO 2019051198A1 US 2018049906 W US2018049906 W US 2018049906W WO 2019051198 A1 WO2019051198 A1 WO 2019051198A1
Authority
WO
WIPO (PCT)
Prior art keywords
hydroxylamine
prodrug
subject
dioxygenase
alkylhydroxylamine
Prior art date
Application number
PCT/US2018/049906
Other languages
English (en)
Inventor
William P. Malachowski
Alexander J. Muller
George C. Prendergast
James B. Duhadaway
Original Assignee
Lankenau Institute For Medical Research
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 Lankenau Institute For Medical Research filed Critical Lankenau Institute For Medical Research
Publication of WO2019051198A1 publication Critical patent/WO2019051198A1/fr

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Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C239/00—Compounds containing nitrogen-to-halogen bonds; Hydroxylamino compounds or ethers or esters thereof
    • C07C239/08—Hydroxylamino compounds or their ethers or esters
    • C07C239/20—Hydroxylamino compounds or their ethers or esters having oxygen atoms of hydroxylamino groups etherified

Definitions

  • the instant invention also encompasses derivatives of the prodrugs.
  • the -CH2- in the above moiety may comprise one or more substituents (e.g., see substituents below for term "alkyl") or replaced with an alkyl (e.g., a lower alkyl such as a C1-C3 alkyl).
  • the benzene ring may comprise one or more substituents (e.g., X and Y as described hereinbelow).
  • the O- alkylhydroxylamine IDO inhibitor is 0-(4-iodobenzyl)hydroxylamine or 0-(3- chlorobenzyl)hydroxylamine. In a particular embodiment, the O-alkylhydroxylamine IDO inhibitor is 0-(3-chlorobenzyl)hydroxylamine.
  • the ocular disease is characterized by abnormal/aberrant vascularization.
  • the ocular disease is characterized by intraocular neovascularization.
  • the intraocular neovascularization may be, without limitation, neovascularization of the optic disc, iris, retina, choroid, cornea, and/or vitreous humour.
  • Each dosage should contain a quantity of active ingredient calculated to produce the desired effect in association with the selected pharmaceutical carrier. Procedures for determining the appropriate dosage unit are well known to those skilled in the art. Dosage units may be proportionately increased or decreased based on the weight of the patient.
  • Appropriate concentrations for alleviation of a particular pathological condition may be determined by dosage concentration curve calculations, as known in the art.
  • a “carrier” refers to, for example, a diluent, adjuvant, excipient, auxilliary agent or vehicle with which an active agent of the present invention is administered.
  • Pharmaceutically acceptable carriers can be sterile liquids, such as water and oils, including those of petroleum, animal, vegetable or synthetic origin, such as peanut oil, soybean oil, mineral oil, sesame oil and the like. Water or aqueous saline solutions and aqueous dextrose and glycerol solutions are preferably employed as carriers, particularly for injectable solutions. Suitable pharmaceutical carriers are described, for example, in "Remington's Pharmaceutical Sciences” by E.W. Martin.
  • aryl refers to monocyclic and bicyclic aromatic groups containing about 6 to 10 carbons in the ring portion.
  • the bicyclic aromatic group may only contain one aromatic ring.
  • Aryl groups may be optionally substituted through available carbon atoms.
  • the aromatic groups may be a heteroaryl (e.g., a ring system that includes at least one sulfur, oxygen, or nitrogen heteroatom ring members).

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne des promédicaments d'indoléamine 2,3-dioxygénase-1 et leurs procédés d'utilisation.
PCT/US2018/049906 2017-09-08 2018-09-07 Inhibiteurs de promédicaments d'indoléamine 2,3-dioxygénase-1 (jdo1) WO2019051198A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762555726P 2017-09-08 2017-09-08
US62/555,726 2017-09-08

Publications (1)

Publication Number Publication Date
WO2019051198A1 true WO2019051198A1 (fr) 2019-03-14

Family

ID=65635249

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2018/049906 WO2019051198A1 (fr) 2017-09-08 2018-09-07 Inhibiteurs de promédicaments d'indoléamine 2,3-dioxygénase-1 (jdo1)

Country Status (1)

Country Link
WO (1) WO2019051198A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112557372A (zh) * 2020-12-07 2021-03-26 福建师范大学 一种基于表面增强拉曼技术检测吲哚胺2，3双加氧酶的方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050107334A1 (en) * 2003-08-20 2005-05-19 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
US20110053941A1 (en) * 2007-11-30 2011-03-03 Newlink Genetics IDO Inhibitors
US20160046596A1 (en) * 2013-03-14 2016-02-18 Curadev Pharma Private Ltd. Inhibitors of the kynurenine pathway

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050107334A1 (en) * 2003-08-20 2005-05-19 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
US20110053941A1 (en) * 2007-11-30 2011-03-03 Newlink Genetics IDO Inhibitors
US20160046596A1 (en) * 2013-03-14 2016-02-18 Curadev Pharma Private Ltd. Inhibitors of the kynurenine pathway

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MALACHOWSKI ET AL.: "O-Alkylhydroxylamines as Rationally-designed Mechanism-based Inhibitors of Indoleamine 2,3-Dioxygenase-1", EUR J MED CHEM., vol. 108, 2016, pages 564 - 576, XP029383533, DOI: doi:10.1016/j.ejmech.2015.12.028 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112557372A (zh) * 2020-12-07 2021-03-26 福建师范大学 一种基于表面增强拉曼技术检测吲哚胺2，3双加氧酶的方法
CN112557372B (zh) * 2020-12-07 2023-04-18 福建师范大学 一种基于表面增强拉曼技术检测吲哚胺2，3双加氧酶的方法

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