Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors
US-2016280704-A1 · Sep 29, 2016 · US
N-(2-cyano heterocyclyl) pyrazolo pyridones as janus kinase inhibitors
US2016272633A1 · US · A1
| Field | Value |
|---|---|
| Publication number | US-2016272633-A1 |
| Application number | US-201414778052-A |
| Country | US |
| Kind code | A1 |
| Filing date | Mar 19, 2014 |
| Priority date | Mar 19, 2013 |
| Publication date | Sep 22, 2016 |
| Grant date | — |
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.
Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
First claim
Opening claim text (preview).
1 . A compound of Formula I or a pharmaceutically acceptable salt, or a stereoisomer thereof: A is selected from aryl and heteroaryl; X is independently selected from CH 2 , NH, S, and O, wherein at least one X is other than CH 2 ; n is 0, 1, 2, 3, or 4; m is 0, 1, 2, 3, or 4; p is 1, 2, 3, 4 or 5; R 1 is selected from: halogen, oxo (═O), C 0-10 alkyliminoC 0-10 alkyl, C 1-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 1-10 heteroalkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, aryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 3-12 cycloalkyl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, heteroaryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, (C 3-12 )heterocycloalkyl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 aminoC 0-10 alkyl, (C 1-10 )heteroalkyl(oxy) 0-1 (carbonyl) 0-1 aminoC 0-10 alkyl, C 3-12 cycloalkyl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 aminoC 0-10 alkyl, aryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 aminoC 0-10 alkyl, heteroaryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 aminoC 0-10 alkyl, (C 3-12 )heterocycloalkyl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 aminoC 0-10 alkyl, C 0-10 alkylamino(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, (C 1-10 )heteroalkylamino(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 3-12 cycloalkylamino(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, aryl C 0-10 alkylamino(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, heteroaryl C 0-10 alkylamino(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, (C 3-12 )heterocycloalkylamino(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 0-10 alkylsulfonylC 0-10 alkyl, C 1-10 heteroalkylsulfonylC 0-10 alkyl, (C 3-12 )cycloalkylC 0-10 alkylsulfonylC 0-10 alkyl, (C 3-12 )cycloheteroalkylC 0-10 alkylsulfonylC 0-10 alkyl, heteroarylC 0-10 alkylsulfonylC 0-10 alkyl, arylC 0-10 alkylsulfonylC 0-10 alkyl, C 1-10 alkylsulfamoylC 0-10 alkyl, C 1-10 heteroalkylsulfamoylC 0-10 alkyl, (C 3-12 )cycloalkylC 0-10 alkylsulfamoylC 0-10 alkyl, (C 3-12 )cycloheteroalkylC 0-10 alkylsulfamoylC 0-10 alkyl, heteroarylC 0-10 alkylsulfamoylC 0-10 alkyl, arylC 0-10 alkylsulfamoylC 0-10 alkyl, (C 0-10 alkyl) 1-2 amino, —CO 2 (C 0-10 alkyl), —(C 0-10 alkyl)CO 2 H, —SO 2 NH 2 , —SO 2 NH(C 1-10 alkyl), —SO 2 N(C 1-10 alkyl) 2 , —SO 2 CF 3 , —SO 2 CF 2 H, C 1-10 alkylsulfinylC 0-10 alkyl, C 1-10 heteroalkylsulfinylC 0-10 alkyl, (C 3-12 )cycloalkylC 0-10 alkylsulfinylC 0-10 alkyl, (C 3-12 )cycloheteroalkylC 0-10 alkylsulfinylC 0-10 alkyl, heteroarylC 0-10 alkylsulfinylC 0-10 alkyl, arylC 0-10 alkylsulfinylC 0-10 alkyl, C 0-10 alkylsulfinylaminoC 0-10 alkyl, C 1-4 acylamino C 0-10 alkyl, thioC 1-10 alkyl, hydroxy, —(C 1-10 alkyl)OH, —C 0-10 alkylalkoxy, cyano, (C 1-6 alkyl)cyano, and C 1-6 haloalkyl; R 2 is selected from: halogen, oxo (═O), C 1-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 3-12 cycloalkyl, (C 3-12 )heterocycloalkyl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 0-10 alkylaminoC 0-10 alkyl, (C 1-10 )heteroalkylaminoC 0-10 alkyl, C 3-12 cycloalkyl C 0-10 alkylaminoC 0-10 alkyl, aryl C 0-10 alkylaminoC 0-10 alkyl, heteroaryl C 0-10 alkylaminoC 0-10 alkyl, (C 3-12 )heterocycloalkyl C 0-10 alkylaminoC 0-10 alkyl, C 1-10 alkylsulfonyl, (C 3-12 )cycloalkylC 0-10 alkylsulfonyl, (C 3-12 )cycloheteroalkylC 0-10 alkylsulfonyl, (C 0-10 alkyl) 1-2 amino, —CO 2 (C 0-10 alkyl), —(C 0-10 alkyl)CO 2 H, —SO 2 CF 3 , —SO 2 CF 2 H, C 1-10 alkylsulfinyl, hydroxy, —(C 1-10 alkyl)OH, —C 0-10 alkylalkoxy, cyano, (C 1-6 alkyl)cyano, and C 1-6 haloalkyl, and wherein R 1 and R 2 are each optionally substituted with 1, 2, 3, or 4 R 3 substituents; R 3 is independently selected from: halogen, C 1-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 1-10 heteroalkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, aryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 3-12 cycloalkyl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, heteroaryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, (C 3-12 )heterocycloalkyl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, ((C 0-10 )alkyl) 1-2 aminocarbonyloxy, aryl (C 0-10 )alkylaminocarbonyloxy, —CO 2 (C 0-10 alkyl), —(C 0-10 alkyl)CO 2 H, oxo (═O), —SO 2 NH 2 , —SO 2 NH(C 1-10 alkyl), —SO 2 N(C 1-10 alkyl) 2 , —SO 2 CF 3 , —SO 2 CF 2 H, C 1-10 alkylsulfinyl, amino, (C 0-10 alkyl) 1-2 amino, -(oxy) 0-1 (carbonyl) 0-1 N(C 0-10 alkyl) 1-2 hydroxy, (C 1-10 alkyl)OH, C 1-10 alkoxy, (C 1-10 alkyl)cyano, cyano, and C 1-6 haloalkyl; and R 3 is optionally substituted with 1, 2, or 3 R 4 substituents selected from hydroxy, (C 1-6 )alkyl, (C 1-6 )alkoxy, (C 1-10 alkyl)OH, halogen, CO 2 H, —(C 0-6 )alkylCN, —O(C═O)C 1 -C 6 alkyl, NO 2 , trifluoromethoxy, trifluoroethoxy, trifluoromethyl, trifluoroethyl, —N—C(O)O(C 0-6 )alkyl, C 1-10 alkylsulfonyl, oxo (O═), aminosulfonyl, —SO 2 NH 2 , —SO 2 NH(C 1-10 alkyl), —SO 2 N(C 1-10 alkyl) 2 , —SO 2 C 1-6 alkyl, —SO 2 CF 3 , —SO 2 CF 2 H, —C 1-10 alkylsulfinyl, —O (0-1) (C 1-10 )haloalkyl, amino(C 1-6 alkyl) 0-2 and NH 2 . 2 . A compound of claim 1 , or a pharmaceutically acceptable salt, or a stereoisomer thereof, wherein A is selected from phenyl, pyridinyl, isoindolinyl, indolyl, 1,3-benzothazolyl, benzodioxolyl, benzo[d][1,3]dioxolyl, dihydroisoindolyl, quinolinyl, quinoxalinyl, dihydrobenzisothiazolyl, 2,3-dihydrobenzo[d]isothiazolyl, dihydroindenyl, dihydrobenzofuranyl, 2,3-dihydrobenzofuranyl, 2,3-dihydro-1H-indenyl, isoindolyl, dihydrobenzo[b]thiophenyl, 2,3-dihydrobenzo[b]thiophenyl and 3 . A compound of claim 2 , or a pharmaceutically acceptable salt, or a stereoisomer thereof, wherein A is selected from phenyl, pyridinyl, 2,3-dihydro-1H-indolyl, 1,3-benzothiazolyl, 2,3-dihydroisoindolyl, dihydrobenzisothiazolyl, 2,3-dihydrobenzo[d]isothiazolyl, and 4 . A compound of claim 3 , or a pharmaceutically acceptable salt, or a stereoisomer thereof, wherein R 1 is selected from: halogen, oxo (═O), C 1-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 1-10 heteroalkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, aryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 3-12 cycloalkyl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, heteroaryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, (C 3-12 )heterocycloalkyl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 aminoC 0-10 alkyl, aryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 aminoC 0-10 alkyl, heteroaryl C 0-10 alkyl(oxy) 0-1 (carbonyl) 0-1 aminoC 0-10 alkyl, C 0-10 alkylamino(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, aryl C 0-10 alkylamino(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, heteroaryl C 0-10 alkylamino(oxy) 0-1 (carbonyl) 0-1 C 0-10 alkyl, C 0-10 alkylsulfonylC 0-10 alkyl, C 1-10 heteroalkylsulfonylC 0-10 alkyl, (C 3-12 )cycloalkylC 0-10 alkylsulfonylC 0-10 alkyl, (C 3-12 )cycloheteroalkylC 0-10 alkylsulfonylC 0-10 alkyl, heteroarylC 0-10 alkylsulfonylC 0-10 alkyl, arylC 0-10 alkylsulfonylC 0-10 alkyl, C 1-10 alkylsulfamoylC 0-10 alkyl, C 1-10 heteroalkylsulfamoylC 0-10 alkyl, (C 3-12 )cycloalkylC 0-10 alkylsulfamoylC 0-10 alkyl, (C 3-12 )cycloheteroalkylC 0-10 alkylsulfamoylC 0-10 alkyl, heteroarylC 0-10 alkylsulfamoylC 0-10 alkyl, arylC 0-10 alkylsulfamoylC 0-10 alkyl, (C 0-10 alkyl) 1-2 amino
Assignees
Inventors
Classifications
Immunosuppressants, e.g. drugs for graft rejection · CPC title
Antineoplastic agents · CPC title
Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · 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 US2016272633A1 cover?
- Provided are compounds of Formula I, a JAK inhibitor, and use thereof for the treatment of JAK-mediated diseases by the application.
- Who is the assignee on this patent?
- Dinsmore Christopher, Fuller Peter, Guerin David, and 15 more
- What technology area does this patent fall under?
- Primary CPC classification C07D471/04. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Thu Sep 22 2016 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 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).