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Inhibitors of indoleamine 2,3-dioxygenase and methods of their use

A C1-C6, OC1-C6 technology, applied in the field of enzyme active compounds, can solve problems such as different functions

Inactive Publication Date: 2019-06-04
BRISTOL MYERS SQUIBB CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

An IDO analog (IDO2) that shares 44% amino acid sequence identity with IDO has been identified, but functions largely differently from IDO

Method used

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  • Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
  • Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
  • Inhibitors of indoleamine 2,3-dioxygenase and methods of their use

Examples

Experimental program
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Effect test

Embodiment approach

[0060] In another embodiment, the present invention provides a combination comprising one or more compounds of the present invention and / or pharmaceutically acceptable salts thereof, stereoisomers thereof, tautomers thereof or solvates thereof things.

[0061] In another embodiment, the present invention provides a compound comprising a pharmaceutically acceptable carrier and at least one compound of the present invention and / or a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a tautomer thereof or Pharmaceutical compositions of its solvates.

[0062] In another embodiment, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one compound of the present invention and / or pharmaceutically acceptable salts, stereoisomers thereof body, its tautomer or its solvate.

[0063] In another embodiment, the present invention provides a process for the preparation...

Embodiment 1

[0242] 4-(( cis )-4-((R)-1-(1H-benzo[d]imidazol-2-yl)ethyl)cyclohexyl)-6-fluoroquinoline

[0243]

[0244] Embodiment 1: 4-(( cis )-4-((R)-1-(1H-benzo[d]imidazol-2-yl)ethyl)cyclohexyl)-6-fluoroquinoline

[0245] Preparation 1A:

[0246]

[0247] in N 2 1,4-dioxaspiro[4.5]decane-8-one (300 g, 1920.86 mmol, 1.0eq) and N To a stirred solution of -phenyltrifluoromethanesulfonimide (823.47 g, 2305.03 mmol, 1.2eq) in MTBE (7.5 L) was added 2.0 M NaHMDS / THF (1152.2 mL, 2305.03 mmol, 1.2eq), and The mixture was stirred for another 60 minutes. The reaction mixture was warmed to room temperature and stirred overnight until TLC showed complete consumption of starting material. The mixture was treated with KHSO 4 Aqueous solution (100 ml) was quenched, filtered to remove solids and the filtrate was concentrated completely. 3 LMTBE was added to the residue, followed by washing with 5% NaOH (1.5 L×3). The organic phase was concentrated to obtain 567 g of crude Preparation 1...

Embodiment 2-7

[0285]

[0286] Examples 2-7 were prepared from Preparation 1K using the procedure of Example 1 and the corresponding phenylenediamines.

[0287] Example number

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PUM

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Abstract

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3 -dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and / or inflammatory disorders utilizing the compounds of the invention.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of US Provisional Application No. 62 / 380,042, filed August 26, 2016, which is hereby incorporated by reference in its entirety. field of invention [0003] The present invention generally relates to compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and the use of compounds of the present invention in the treatment of proliferative disorders such as cancer, viral infections and / or methods for autoimmune diseases. Background of the invention [0004] Indoleamine 2,3-dioxygenase (IDO; also known as IDO1) is an IFN-γ target gene that plays a role in immune regulation. IDO is an oxidoreductase and is one of two enzymes that catalyze the first and rate-limiting step in the conversion of tryptophan to N-formyl-kynurenine. It exists as a 41 kD monomer found in several cell populations includ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4709A61K31/4184C07D235/02
CPCC07D401/08C07D401/12C07D413/08C07D417/08C07D471/04C07D487/04C07D491/056A61P35/00A61K31/4709A61K39/3955A61K2039/505A61K2300/00A61K31/4375A61K31/5025A61K31/517C07D413/12C07D417/12
Inventor E.C.彻尔尼单伟芳张礼萍S.J.纳拉A.黄J.A.巴洛
Owner BRISTOL MYERS SQUIBB CO
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