Pyridazinedione-based heterobicyclic covalent linkers and methods and applications thereof
US-2024425465-A1 · Dec 26, 2024 · US
Certain protein kinase inhibitors
US9567342B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9567342-B2 |
| Application number | US-201514926729-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 29, 2015 |
| Priority date | Nov 6, 2012 |
| Publication date | Feb 14, 2017 |
| Grant date | Feb 14, 2017 |
How to read this patent
A practical reading order for non-experts. Skip the full description unless you need deep technical detail.
- Title
What the patent document calls the invention.
- Abstract
A short plain-language summary of the technical disclosure.
- Assignees and inventors
Who owns or filed the patent and who is credited as inventor.
- Key dates
Filing, priority, publication, and grant dates set the timeline.
- First independent claim
The legal scope of protection — read this for what is actually claimed.
- CPC / IPC classifications
Technology tags used to group this patent with similar filings.
- Citations and related patents
Prior art links and similar publications in this corpus.
Abstract
Official abstract text for this publication.
Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof.
First claim
Opening claim text (preview).
What is claimed is: 1. A method for inhibiting anaplastic lymphoma kinase in a cell, comprising contacting the cell with an effective amount of at least one compound of formula (I): and/or at least one pharmaceutically acceptable salt thereof, or at least one pharmaceutical composition thereof, wherein each R 1 is independently: hydrogen, halogen, hydroxyl, C 1-10 alkyl, C 3-10 cycloalkyl, C 3-10 cycloalkyl-alkyl, heterocyclyl, heterocyclylalkyl aryl, arylalkyl, heteroaryl, or heteroarylalkyl, wherein alkyl, cycloalkyl, and heterocyclyl are each unsubstituted or substituted with at least one substituent independently selected from R 6a , and wherein aryl and heteroaryl are each unsubstituted or substituted with at least one substituent independently selected from R 6b ; each R 2 is independently: C 1-10 alkyl or piperidinyl, wherein alkyl and piperidinyl are each unsubstituted or substituted with at least one substituent independently selected from R 6a ; each R 3 is independently: hydrogen, halogen, —CN, —NR 7 R 8 , or C 1-10 alkyl; wherein alkyl is unsubstituted or substituted with at least one substituent independently selected from R 6a ; each R 4 is independently: hydrogen, halogen, —CN, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, or C 3-10 cycloalkyl; wherein C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, and C 3-10 cycloalkyl are each unsubstituted or substituted with at least one substituent independently selected from R 6a ; or R 3 and R 4 together with the carbon atoms to which they are attached form a 5-6 membered ring containing 0, 1, 2 or 3 heteroatoms independently selected from the group consisting of oxygen, sulfur and nitrogen, and optionally substituted with 1-2 R 6b groups; each R 5 is independently: C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, C 3-10 cycloalkyl, —OR 8 , —NR 7 S(O) r R 8 , —NO 2 , halogen, —S(O) r R 7 , —SR 8 , —S(O) 2 OR 7 , —OS(O) 2 R 8 , —S(O) r NR 7 R 8 , —NR 7 R 8 , —O(CR 9 R 10 ) t NR 7 R 8 , —C(O)R 7 , —CO 2 R 8 , —CO 2 (CR 9 R 10 ) t CONR 7 R 8 , —OC(O)R 7 , —CN, —C(O)NR 7 R 8 , —NR 7 C(O)R 8 , —OC(O)NR 7 R 8 , —NR 7 C(O)OR 8 , —NR 7 C(O)NR 7 R 8 , —CR 7 (N—OR 8 ), —CHF 2 , —CF 3 , —OCHF 2 , or —OCF 3 ; wherein C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, and C 3-10 cycloalkyl are each unsubstituted or substituted with at least one substituent independently selected from R 6a ; each R 6a is independently: C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, C 3-10 cycloalkyl, —OR 8 , —NR 7 S(O) r R 8 , —NO 2 , halogen, —S(O) r R 7 , —SR 8 , —S(O) 2 OR 7 , —OS(O) 2 R 8 , —S(O) r NR 7 R 8 , —NR 7 R 8 , —(CR 9 R 10 ) t OR 8 , —(CR 9 R 10 ) t NR 7 R 8 , —(CR 9 R 10 ) t SR 8 , —(CR 9 R 10 ) t S(O) r R 8 , —(CR 9 R 10 ) t CO 2 R 8 , —(CR 9 R 10 ) t CONR 7 R 8 , —(CR 9 R 10 ) t NR 7 CO 2 R 8 , —(CR 9 R 10 ) t OCONR 7 R 8 , —(CR 9 R 10 ) t NR 7 CONR 7 R 8 , —(CR 9 R 10 ) t NR 7 SO 2 NR 7 R 8 , —O(CR 9 R 10 ) t NR 7 R 8 , —C(O)R 7 , —C(O)(CR 9 R 10 ) t OR 8 , —C(O)(CR 9 R 10 ) t NR 7 R 8 , —C(O)(CR 9 R 10 ) t SR 8 , —C(O)(CR 9 R 10 ) t S(O) r R 8 , —CO 2 R 8 , —CO 2 (CR 9 R 10 ) t CONR 7 R 8 , —OC(O)R 7 , —CN, —C(O)NR 7 R 8 , —NR 7 C(O)R 8 , —OC(O)NR 7 R 8 , —NR 7 C(O)OR 8 , —NR 7 C(O)NR 7 R 8 , —CR 7 (N—OR 8 ), —CHF 2 , —CF 3 , —OCHF 2 , or —OCF 3 ; each R 6b is independently: R 6a , aryl, aryl-C 1-4 alkyl, heteroaryl, or heteroaryl-C 1-4 alkyl; each R 7 and each R 8 are independently: hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, C 3-10 cycloalkyl, cycloalkyl-C 1-10 alkyl; heterocyclyl, heterocyclyl-C 1-10 alkyl, aryl, heteroaryl, aryl-C 1-10 alkyl, or heteroaryl-C 1-10 alkyl; wherein alkyl, alkenyl, alkynyl, cycloalkyl, and heterocyclyl are each unsubstituted or substituted with at least one substituent independently selected from R 6a , and aryl and heteroaryl are each unsubstituted or substituted with at least one substituent independently selected from R 6b ; or R 7 and R 8 together with the atom(s) to which they are attached form a heterocyclic ring of 4 to 7 members containing 0, 1, or 2 additional heteroatoms independently selected from the group consisting of oxygen, sulfur and NR 11 , each R 7 and R 8 may be unsubstituted or substituted on a carbon or nitrogen atom with at least one substituent independently selected from R 12 ; each R 9 and each R 10 are independently: hydrogen, C 1-10 alkyl, C 2-10 alkenyl, C 2-10 alkynyl, C 3-10 cycloalkyl, cycloalkyl-C 1-10 alkyl, heterocyclyl, heterocyclyl-C 1-10 alkyl, aryl, heteroaryl, aryl-C 1-10 alkyl, or heteroaryl-C 1-10 alkyl; or R 9 and R 10 together with the carbon to which they are attached form a ring of 3 to 7 members containing 0, 1, or 2 heteroatoms independently selected from the group consisting of oxygen, sulfur and nitrogen; each R 11 is independently: hydrogen, C 1-10 alkyl, C 3-10 cycloalkyl, C 3-10 cycloalkyl-C 1-4 alkyl, heterocyclyl, heterocyclyl-C 1-4 alkyl, aryl, aryl-C 1-4 alkyl, heteroaryl, heteroaryl-C 1-4 alkyl, —S(O) r R 7 , —C(O)R 7 , —CO 2 R 7 , —CO 2 (CR 9 R 10 ) t CONR 7 R 8 , or —C(O)NR 7 R 8 , each R 12 is independently: halogen, C 1-10 alkyl, C 3-10 cycloalkyl, C 3-10 cycloalkylalkyl, heterocycyl, heterocyclyalkyl, aryl, aryl-C 1-4 alkyl, heteroaryl, heteroaryl-C 1-4 alkyl, —OR 7 , —NR 7 S(O) r R 8 , —S(O) r R 7 , —SR 7 , —S(O) 2 OR 7 , —OS(O) 2 R 7 , —S(O) r NR 7 R 8 , —NR 7 R 8 , —O(CR 9 R 10 ) t NR 7 R 8 , —C(O)R 7 , —CO 2 R 8 , —CO 2 (CR 9 R 10 ) t CONR 7 R 8 , —OC(O)R 7 , —CN, —C(O)NR 7 R 8 , —NR 7 C(O)R 8 , —OC(O)NR 7 R 8 , —NR 7 C(O)OR 8 , —NR 7 C(O)NR 7 R 8 , —CHF 2 , —CF 3 , —OCHF 2 , or —OCF 3 ; each m is independently 0, 1 or 2; each n is independently 1, 2, or 3; each p is independently 2; each q is independently 0, 1, 2, or 3; each r is independently 1 or 2; each t is independently 1, 2, or 3. 2. A method to treat a
Assignees
Inventors
Classifications
Antineoplastic agents · CPC title
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title
ortho- or peri-condensed with heterocyclic rings · CPC title
- C07D487/04Primary
Ortho-condensed systems · 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 US9567342B2 cover?
- Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof.
- Who is the assignee on this patent?
- Shanghai Fochon Pharmaceutical Co Ltd, Shanghai Inst Materia Medica Cas
- What technology area does this patent fall under?
- Primary CPC classification C07D487/04. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Feb 14 2017 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). 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).