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Method for preparing ridinilazole and crystal form thereof

A technology of crystal form and composition, which is applied in the field of preparation of ridinilazole and its crystal form, and can solve problems such as no mention of antibacterial activity

Pending Publication Date: 2022-03-01
サミット(オックスフォード)リミティド
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The literature does not mention potential antimicrobial activity

Method used

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  • Method for preparing ridinilazole and crystal form thereof
  • Method for preparing ridinilazole and crystal form thereof
  • Method for preparing ridinilazole and crystal form thereof

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Embodiment Construction

[0040] All publications, patents, patent applications, and other references mentioned herein are incorporated by reference in their entirety for all purposes as if each individual publication, patent, or patent application were specifically and individually indicated to be Incorporated by reference, and its content is cited in its entirety.

[0041] 5.1 Definition and general preference

[0042] As used herein, unless specifically stated otherwise, the following terms have the following meanings in addition to any broader (or narrower) meanings that term may have in the art:

[0043] Unless the context requires otherwise, the singular used herein shall be understood to include the plural and vice versa. The term "a" or "an" used with reference to an entity should be understood to mean one or more of that entity. Accordingly, the terms "a" (or "an"), "one or more" and "at least one" are used interchangeably herein.

[0044] As used herein, the term "comprise" or variations...

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Abstract

Described are methods of making 2, 2 '-bis (pyridin-4-yl)-1H, 1' H-5, 5 '-dibenzo [d] imidazole (also can be referred to as 5, 5'-bis-[2-(4-pyridinyl)-1H-benzimidazole]) (as mentioned herein as the INN name ridinilazole), and pharmaceutically acceptable derivatives, salts, hydrates, solvates, complexes, bioisosteres, metabolites, or prodrugs thereof. The present invention also relates to various compositions of purified ridinilazole, various crystal forms of ridinilazole, methods for their preparation, and related pharmaceutical formulations and uses thereof, including their medical uses and their uses in efficient large scale synthesis of ridinilazole.

Description

1. Technical field [0001] The present invention relates to the preparation of 2,2'-bis(pyridin-4-yl)-1H,1'H-5,5'-dibenzo[d]imidazole (which may also be referred to as 5,5'-bis[2 -(4-pyridyl)-1H-benzimidazole], 2,2'-bis(4-pyridyl)-3H,3'H-5,5'-dibenzimidazole or 2-pyridine-4- -6-(2-pyridin-4-yl-3H-benzimidazol-5-yl)-1H-benzimidazole) (referred to herein under the INN name ridinilazole), and its pharmaceutically acceptable Derivatives, salts, hydrates, solvates, complexes, bioisosteres, metabolites or prodrugs of . The present invention also relates to various crystal forms of ridinilazole, their preparation methods and related pharmaceutical preparations and uses thereof (including their medical use and their use in efficient large-scale synthesis of ridinilazole). 2. Background technology [0002] Infection with Clostridioides difficile (formerly Clostridium difficile) (CDI) causes Clostridioides difficile-associated disease (CDAD). More than 450,000 cases of CDI occur ann...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14A61K31/444A61P31/04
CPCC07D401/14A61P31/04C07B2200/13Y02A50/30C07D401/04A61K31/444
Inventor F·X·威尔逊J-F·卡尼奥N·亚当斯
Owner サミット(オックスフォード)リミティド
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