Compositions of polyhydroxylated benzophenones and methods of treatment of neurodegenerative disorders

US2018290960A1 · US · A1

Patent metadata
FieldValue
Publication numberUS-2018290960-A1
Application numberUS-201816010030-A
CountryUS
Kind codeA1
Filing dateJun 15, 2018
Priority dateDec 17, 2015
Publication dateOct 11, 2018
Grant date

How to read this patent

A practical reading order for non-experts. Skip the full description unless you need deep technical detail.

  1. Title

    What the patent document calls the invention.

  2. Abstract

    A short plain-language summary of the technical disclosure.

  3. Assignees and inventors

    Who owns or filed the patent and who is credited as inventor.

  4. Key dates

    Filing, priority, publication, and grant dates set the timeline.

  5. First independent claim

    The legal scope of protection — read this for what is actually claimed.

  6. CPC / IPC classifications

    Technology tags used to group this patent with similar filings.

  7. Citations and related patents

    Prior art links and similar publications in this corpus.

Abstract

Official abstract text for this publication.

The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.

First claim

Opening claim text (preview).

1 . A compound of formula I: or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, isomer, or tautomer thereof, wherein: R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each independently H, PO(OR x ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), CO(heteroaryl), CON(R y ) 2 , COO(C 1 -C 6 alkyl), COO(C 2 -C 6 alkenyl), COO(C 2 -C 6 alkynyl), COO(C 3 -C 8 cycloalkyl), COO(3 to 8-membered heterocyclyl), or COO(aryl), COO(heteroaryl) wherein each PO(OR x ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), CO(heteroaryl), CON(R y ) 2 , COO(C 1 -C 6 alkyl), COO(C 2 -C 6 alkenyl), COO(C 2 -C 6 alkynyl), COO(C 3 -C 8 cycloalkyl), COO(3 to 8-membered heterocyclyl), COO(aryl) or COO(heteroaryl) is optionally substituted with one or more substituents selected from the group consisting of halogen, OH, NH 2 , CN, C 1 -C 6 alkyl, aryl, heteroaryl and C 1 -C 6 alkoxy; R x is independently H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), or CO(heteroaryl) wherein each C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), or CO(heteroaryl) is optionally substituted with one or more substituents selected from the group consisting of halogen, OH, NH 2 , CN, C 1 -C 6 alkyl, aryl, heteroaryl and C 1 -C 6 alkoxy; R y is independently H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), or CO(heteroaryl) wherein each C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), or CO(heteroaryl) is optionally substituted with one or more substituents selected from the group consisting of halogen, OH, NH 2 , CN, C 1 -C 6 alkyl, aryl, heteroaryl and C 1 -C 6 alkoxy; provided that the compound is not: 2 . The compound of claim 1 having the formula Ia: wherein: R 1 is PO(OR x ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), CO(heteroaryl), CON(R y ) 2 , COO(C 1 -C 6 alkyl), COO(C 2 -C 6 alkenyl), COO(C 2 -C 6 alkynyl), COO(C 3 -C 8 cycloalkyl), COO(3 to 8-membered heterocyclyl), COO(aryl), or COO(heteroaryl), wherein each PO(OR x ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), CO(heteroaryl), CON(R y ) 2 , COO(C 1 -C 6 alkyl), COO(C 2 -C 6 alkenyl), COO(C 2 -C 6 alkynyl), COO(C 3 -C 8 cycloalkyl), COO(3 to 8-membered heterocyclyl), COO(aryl) or COO(heteroaryl) is optionally substituted with one or more substituents selected from the group consisting of halogen, OH, NH 2 , CN, C 1 -C 6 alkyl, aryl, heteroaryl and C 1 -C 6 alkoxy; R 2 , R 3 , R 4 , R 5 and R 6 are each independently H, PO(OR x ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), CO(heteroaryl), CON(R y ) 2 , COO(C 1 -C 6 alkyl), COO(C 2 -C 6 alkenyl), COO(C 2 -C 6 alkynyl), COO(C 3 -C 8 cycloalkyl), COO(3 to 8-membered heterocyclyl), COO(aryl), COO(heteroaryl) wherein each PO(OR x ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), CO(heteroaryl), CON(R y ) 2 , COO(C 1 -C 6 alkyl), COO(C 2 -C 6 alkenyl), COO(C 2 -C 6 alkynyl), COO(C 3 -C 8 cycloalkyl), COO(3 to 8-membered heterocyclyl), COO(aryl) or COO(heteroaryl) is optionally substituted with one or more substituents selected from the group consisting of halogen, OH, NH 2 , CN, C 1 -C 6 alkyl, aryl, heteroaryl and C 1 -C 6 alkoxy; provided that the compound is not: 3 . The compound of claim 1 having the formula Ib: wherein: R 1 is H, PO(OR x ) 2 , C 2 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), CO(heteroaryl), CON(R y ) 2 , COO(C 1 -C 6 alkyl), COO(C 2 -C 6 alkenyl), COO(C 2 -C 6 alkynyl), COO(C 3 -C 8 cycloalkyl), COO (3 to 8-membered heterocyclyl), COO(aryl), or COO(heteroaryl), wherein each PO(OR x ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), CO(heteroaryl), CON(R y ) 2 , COO(C 1 -C 6 alkyl), COO(C 2 -C 6 alkenyl), COO(C 2 -C 6 alkynyl), COO(C 3 -C 8 cycloalkyl), COO(3 to 8-membered heterocyclyl), COO(aryl) or COO(heteroaryl) is optionally substituted with one or more substituents selected from the group consisting of halogen, OH, NH 2 , CN, C 1 -C 6 alkyl, aryl, heteroaryl and C 1 -C 6 alkoxy; R 2 , R 3 , R 4 , R 5 and R 6 are each independently H, PO(OR x ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), CO(C 3 -C 8 cycloalkyl), CO(3 to 8-membered heterocyclyl), CO(aryl), CO(heteroaryl), CON(R y ) 2 , COO(C 1 -C 6 alkyl), COO(C 2 -C 6 alkenyl), COO(C 2 -C 6 alkynyl), COO(C 3 -C 8 cycloalkyl), COO(3 to 8-membered heterocyclyl), COO(aryl), or COO(heteroaryl), wherein each PO(OR x ) 2 , C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, C 3 -C 8 cycloalkyl, 3 to 8-membered heterocyclyl, aryl, heteroaryl, CO(C 1 -C 6 alkyl), CO(C 2 -C 6 alkenyl), CO(C 2 -C 6 alkynyl), C

Assignees

Inventors

Classifications

  • C07C49/83Primary

    polycyclic · CPC title

  • Ketones · CPC title

  • polycyclic · CPC title

  • Nose · CPC title

  • Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

Patent family

Related publications grouped by family.

External sources

Frequently asked questions

Answers are generated from the same data shown on this page.

What does patent US2018290960A1 cover?
The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.
Who is the assignee on this patent?
Massachusetts Inst Technology
What technology area does this patent fall under?
Primary CPC classification C07C49/83. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Thu Oct 11 2018 00:00:00 GMT+0000 (Coordinated Universal Time) (A1). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).