Ethyl N-Boc piperidinyl pyrazolo pyridones as Janus kinase inhibitorsThe instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds.The compound of formulas i or its pharmaceutically acceptable salt：a is selected from aryl and heteroaryl；m is 0,1 or 2；r1selected from hydrogen, c1-2alkyl, fluorine and hydroxyl；r2it is selected from：hydrogen,halogen,oxo（=o）、c1-10alkyl (epoxide)0-1(carbonyl)0-1c0-10alkyl,c1-10miscellaneous alkyl (epoxide)0-1(carbonyl)0-1c0-10alkyl,aryl c0-10alkyl (epoxide)0-1(carbonyl)0-1c0-10alkyl,c3-12cycloalkyl c0-10alkyl (epoxide)0-1(carbonyl)0-1c0-10alkyl,heteroaryl c0-10alkyl (epoxide)0-1(carbonyl)0-1c0-10alkyl,(c3-12) heterocyclylalkyl c0-10alkyl (epoxide)0-1(carbonyl)0-1c0-10alkyl,loop coil base c0-10alkyl (epoxide)0-1(carbonyl)0-1c0-10alkyl,spiro heterocyclic radical c0-10alkyl (epoxide)0-1(carbonyl)0-1c0-10alkyl,c0-10alkyl amino c0-10alkyl,(c1-10) miscellaneous alkyl amino c0-10alkyl,(c1-10) miscellaneous alkyl amino c0-10alkyl,c3-12cycloalkyl c0-10alkyl amino c0-10alkyl,aryl c0-10alkyl amino c0-10alkyl,heteroaryl c0-10alkyl amino c0-10alkyl,(c3-12) heterocyclylalkyl c0-10alkyl amino c0-10alkyl,c1-10alkyl sulphonyl,c1-10miscellaneous alkyl sulfonyl,(c3-12) cycloalkyl c0-10alkyl sulphonyl,(c3-12) heterocyclylalkyl c0-10alkyl sulphonyl,heteroaryl c0-10alkyl sulphonyl,aryl c0-10alkyl sulphonyl,-so2nh2、-so2nh(c1-6alkyl),-so2n(c1-6alkyl)2、c1-10miscellaneous alkyl sulfamoyl,(c3-12) cycloalkyl c0-10alkylsulfamoyl group,(c3-12) heterocyclylalkyl c0-10alkylsulfamoyl group,heteroaryl c0-10alkylsulfamoyl group,aryl c0-10alkylsulfamoyl group,(c1-10alkyl)1-2amino,-co2(c0-10alkyl),-(c0-10alkyl) co2h、-so2cf3、-so2cf2h、-so2ch2cf3、c1-10alkyl sulphinyl,c1-4acyl amino c0-10alkyl,hydroxyl,-(c1-10alkyl) oh,c1-10alkoxy c0-10alkyl,cyano group,(c1-6alkyl) cyano group,cyano group c1-6alkyl, andc1-6haloalkyl,wherein r2optionally independently by 0,1,2 or 3 r4substitution；each r3independently selected from：c1-10alkyl,(c3-12) heterocyclylalkyl c0-10alkyl,c1-10alkoxy c0-10alkyl,halogen,c1-6haloalkyl, andoxo；each r4independently selected from：c1-10alkyl,(c3-12) heterocyclylalkyl c0-10alkyl,c1-10alkoxy c0-10alkyl,c0-10alkyl amino c0-10alkyl,halogen,hydroxyl,-(c1-10alkyl) oh,c1-6haloalkyl, andoxo.
야누스 키나제 억제제로서의 에틸 N-Boc 피페리디닐 피라졸로 피리돈본 발명은 JAK 억제제인 화학식 I의 화합물을 제공하며, 이와 같이 JAK-매개 질환 예컨대 류마티스 관절염, 천식, COPD 및 암의 치료에 유용하다. 본 발명은 JAK 억제제인 신규 화합물을 제공한다. 본 발명은 상기 신규 화합물을 사용하는 JAK-매개 질환 및 장애의 치료 및 예방 방법, 뿐만 아니라 상기 화합물을 함유하는 제약 조성물을 또한 제공한다. <화학식 I>화학식 I의 화합물 또는 그의 제약상 허용되는 염.<화학식 I>[이미지]A는 아릴 및 헤테로아릴로부터 선택되고;m은 0, 1, 또는 2이고;R1은 수소, C1-2알킬, 플루오로, 및 히드록시로부터 선택되고;R2는수소,할로겐,옥소 (=O),C1-10 알킬(옥시)0-1(카르보닐)0-1C0-10 알킬,C1-10 헤테로알킬(옥시)0-1(카르보닐)0-1C0-10 알킬,아릴 C0-10 알킬(옥시)0-1(카르보닐)0-1C0-10 알킬,C3-12 시클로알킬 C0-10 알킬(옥시)0-1(카르보닐)0-1C0-10 알킬,헤테로아릴 C0-10 알킬(옥시)0-1(카르보닐)0-1C0-10 알킬,(C3-12)헤테로시클로알킬 C0-10 알킬(옥시)0-1(카르보닐)0-1C0-10알킬,스피로시클릴C0-10 알킬(옥시)0-1(카르보닐)0-1C0-10 알킬,스피로헤테로시클릴C0-10 알킬(옥시)0-1(카르보닐)0-1C0-10 알킬,C0-10 알킬아미노C0-10 알킬,(C1-10)헤테로알킬아미노C0-10알킬,(C1-10)헤테로알킬아미노C0-10알킬,C3-12 시클로알킬 C0-10 알킬아미노C0-10 알킬,아릴 C0-10 알킬아미노C0-10 알킬,헤테로아릴 C0-10 알킬아미노C0-10 알킬,(C3-12)헤테로시클로알킬 C0-10 알킬아미노C0-10 알킬,C1-10 알킬술포닐,C1-10 헤테로알킬술포닐,(C3-12)시클로알킬C0-10알킬술포닐,(C3-12) 헤테로시클로알킬C0-10알킬술포닐,헤테로아릴C0-10 알킬술포닐,아릴C0-10 알킬술포닐,-SO2NH2,-SO2NH(C1-6알킬),-SO2N(C1-6알킬)2,C1-10 헤테로알킬술파모일,(C3-12)시클로알킬C0-10 알킬술파모일,(C3-12) 헤테로시클로알킬C0-10 알킬술파모일,헤테로아릴C0-10 알킬술파모일,아릴C0-10 알킬술파모일,(C1-10 알킬)1-2아미노,-CO2(C0-10 알킬),-(C0-10 알킬)CO2H,-SO2CF3,-SO2CF2H,-SO2CH2CF3,C1-10 알킬술피닐,C1-4아실아미노C0-10 알킬,히드록시,-(C1-10 알킬)OH,C1-10 알콕시C0-10 알킬,시아노,(C1-6알킬)시아노,시아노C1-6알킬, 및C1-6할로알킬로부터 선택되고,여기서 R2는 임의로 독립적으로 0, 1, 2, 또는 3개의 R4에 의해 치환되고;각각의 R3은 독립적으로C1-10 알킬,(C3-12)헤테로시클로알킬 C0-10 알킬,C1-10 알콕시C0-10 알킬,할로겐,C1-6할로알킬, 및옥소로부터 선택되고;각각의 R4는 독립적으로C1-10 알킬,(C3-12)헤테로시클로알킬 C0-10 알킬,C1-10 알콕시C0-10 알킬,C0-10 알킬아미노C0-10 알킬,할로겐,히드록시,-(C1-10 알킬)OH,C1-6할로알킬, 및옥소로부터 선택된다.