JP2012532112A5 - - Google Patents
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- JP2012532112A5 JP2012532112A5 JP2012517917A JP2012517917A JP2012532112A5 JP 2012532112 A5 JP2012532112 A5 JP 2012532112A5 JP 2012517917 A JP2012517917 A JP 2012517917A JP 2012517917 A JP2012517917 A JP 2012517917A JP 2012532112 A5 JP2012532112 A5 JP 2012532112A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halogen
- oxo
- independently
- membered
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000000217 alkyl group Chemical group 0.000 claims 134
- 229910052736 halogen Inorganic materials 0.000 claims 79
- 150000002367 halogens Chemical class 0.000 claims 77
- 125000004043 oxo group Chemical group O=* 0.000 claims 67
- 125000000623 heterocyclic group Chemical group 0.000 claims 60
- 229910052739 hydrogen Inorganic materials 0.000 claims 36
- 239000001257 hydrogen Substances 0.000 claims 36
- 125000004429 atom Chemical group 0.000 claims 25
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 22
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 15
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 15
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 150000002431 hydrogen Chemical class 0.000 claims 12
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- -1 C 1 -C 3 alkyl Chemical group 0.000 claims 3
- VOPWNXZWBYDODV-UHFFFAOYSA-N Chlorodifluoromethane Chemical compound FC(F)Cl VOPWNXZWBYDODV-UHFFFAOYSA-N 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- BRBMJARZVFXESE-UHFFFAOYSA-N CC1=NN(C(=C1)N1CC=C2N1C=CC=N2)C2=CC=CC=C2 Chemical compound CC1=NN(C(=C1)N1CC=C2N1C=CC=N2)C2=CC=CC=C2 BRBMJARZVFXESE-UHFFFAOYSA-N 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- ZZIWHWXPXNFRSR-UHFFFAOYSA-N n-[5-methyl-4-(4-propylphenyl)-1,3-thiazol-2-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamide Chemical compound C1=CC(CCC)=CC=C1C1=C(C)SC(NC(=O)C2=C3N=CC=CN3N=C2)=N1 ZZIWHWXPXNFRSR-UHFFFAOYSA-N 0.000 claims 2
- XMRIUEGHBZTNND-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine-3-carboxamide Chemical compound C1=CC=NC2=C(C(=O)N)C=NN21 XMRIUEGHBZTNND-UHFFFAOYSA-N 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 206010019842 Hepatomegaly Diseases 0.000 claims 1
- 208000029462 Immunodeficiency disease Diseases 0.000 claims 1
- 102000015617 Janus Kinases Human genes 0.000 claims 1
- 108010024121 Janus Kinases Proteins 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 210000001744 T-lymphocyte Anatomy 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000030833 cell death Effects 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 230000001066 destructive effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22291809P | 2009-07-02 | 2009-07-02 | |
| US61/222,918 | 2009-07-02 | ||
| PCT/US2010/040906 WO2011003065A2 (en) | 2009-07-02 | 2010-07-02 | Pyrazolopyrimidine jak inhibitor compounds and methods |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015122441A Division JP6312634B2 (ja) | 2009-07-02 | 2015-06-17 | ピラゾロピリミジンｊａｋ阻害剤化合物及び方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012532112A JP2012532112A (ja) | 2012-12-13 |
| JP2012532112A5 true JP2012532112A5 (enExample) | 2013-08-15 |
| JP5769261B2 JP5769261B2 (ja) | 2015-08-26 |
Family
ID=43411778
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012517917A Active JP5769261B2 (ja) | 2009-07-02 | 2010-07-02 | ピラゾロピリミジンｊａｋ阻害剤化合物及び方法 |
| JP2015122441A Active JP6312634B2 (ja) | 2009-07-02 | 2015-06-17 | ピラゾロピリミジンｊａｋ阻害剤化合物及び方法 |
| JP2018000305A Withdrawn JP2018083828A (ja) | 2009-07-02 | 2018-01-04 | ピラゾロピリミジンｊａｋ阻害剤化合物及び方法 |
| JP2019106948A Pending JP2019194199A (ja) | 2009-07-02 | 2019-06-07 | ピラゾロピリミジンｊａｋ阻害剤化合物及び方法 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015122441A Active JP6312634B2 (ja) | 2009-07-02 | 2015-06-17 | ピラゾロピリミジンｊａｋ阻害剤化合物及び方法 |
| JP2018000305A Withdrawn JP2018083828A (ja) | 2009-07-02 | 2018-01-04 | ピラゾロピリミジンｊａｋ阻害剤化合物及び方法 |
| JP2019106948A Pending JP2019194199A (ja) | 2009-07-02 | 2019-06-07 | ピラゾロピリミジンｊａｋ阻害剤化合物及び方法 |
Country Status (35)
Families Citing this family (128)
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|---|---|---|---|---|
| PT1966202E (pt) | 2005-12-13 | 2012-01-03 | Incyte Corp | Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase |
| RS53245B2 (sr) | 2007-06-13 | 2022-10-31 | Incyte Holdings Corp | Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila |
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| UA110324C2 (en) | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| MX354212B (es) | 2010-03-10 | 2018-02-19 | Incyte Corp | Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1). |
| JP6161537B2 (ja) | 2010-04-07 | 2017-07-12 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ピラゾール−４−イル−ヘテロシクリル−カルボキサミド化合物及び使用の方法 |
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