JP2004534047A5 - - Google Patents
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- Publication number
- JP2004534047A5 JP2004534047A5 JP2003500088A JP2003500088A JP2004534047A5 JP 2004534047 A5 JP2004534047 A5 JP 2004534047A5 JP 2003500088 A JP2003500088 A JP 2003500088A JP 2003500088 A JP2003500088 A JP 2003500088A JP 2004534047 A5 JP2004534047 A5 JP 2004534047A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- alkoxy
- alkylamino
- trifluoromethyl
- 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.)
- Granted
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- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 69
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 29
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000002252 acyl group Chemical group 0.000 claims 18
- 125000004442 acylamino group Chemical group 0.000 claims 18
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 17
- -1 hydroxy, amino Chemical group 0.000 claims 16
- 238000000034 method Methods 0.000 claims 15
- 229920001577 copolymer Chemical group 0.000 claims 14
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 14
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 13
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 12
- 229910052805 deuterium Inorganic materials 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 10
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 9
- 125000001475 halogen functional group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 6
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 6
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 6
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 6
- 125000004423 acyloxy group Chemical group 0.000 claims 6
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 230000000707 stereoselective effect Effects 0.000 claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 5
- 239000002253 acid Substances 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 239000002244 precipitate Substances 0.000 claims 5
- 239000002904 solvent Substances 0.000 claims 5
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 4
- 125000001769 aryl amino group Chemical group 0.000 claims 4
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 4
- 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 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000006624 (C1-C6) alkoxycarbonylamino group Chemical group 0.000 claims 2
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- 102000006500 Janus Kinase 3 Human genes 0.000 claims 2
- 108010019421 Janus Kinase 3 Proteins 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 claims 2
- 125000005110 aryl thio group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000005241 heteroarylamino group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims 2
- 238000001556 precipitation Methods 0.000 claims 2
- 150000003892 tartrate salts Chemical class 0.000 claims 2
- UJLAWZDWDVHWOW-YPMHNXCESA-N tofacitinib Chemical compound C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-YPMHNXCESA-N 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- CMIBUZBMZCBCAT-HZPDHXFCSA-N (2r,3r)-2,3-bis[(4-methylbenzoyl)oxy]butanedioic acid Chemical group C1=CC(C)=CC=C1C(=O)O[C@@H](C(O)=O)[C@H](C(O)=O)OC(=O)C1=CC=C(C)C=C1 CMIBUZBMZCBCAT-HZPDHXFCSA-N 0.000 claims 1
- LRIZCRLAGSEHSM-YPMHNXCESA-N (3r,4r)-n,n,4-trimethyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidine-1-carboxamide Chemical compound C[C@@H]1CCN(C(=O)N(C)C)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 LRIZCRLAGSEHSM-YPMHNXCESA-N 0.000 claims 1
- 125000006763 (C3-C9) cycloalkyl group Chemical group 0.000 claims 1
- SCYULBFZEHDVBN-UHFFFAOYSA-N 1,1-Dichloroethane Chemical compound CC(Cl)Cl SCYULBFZEHDVBN-UHFFFAOYSA-N 0.000 claims 1
- JKTSSZQGORRDDS-PWSUYJOCSA-N 1-[(3r,4r)-3-[(5-chloro-7h-pyrrolo[2,3-d]pyrimidin-4-yl)-methylamino]-4-methylpiperidin-1-yl]propan-1-one Chemical compound C1N(C(=O)CC)CC[C@@H](C)[C@H]1N(C)C1=NC=NC2=C1C(Cl)=CN2 JKTSSZQGORRDDS-PWSUYJOCSA-N 0.000 claims 1
- VNFSWYNIMVHZSO-PWSUYJOCSA-N 1-[(3r,4r)-3-[(5-fluoro-7h-pyrrolo[2,3-d]pyrimidin-4-yl)-methylamino]-4-methylpiperidin-1-yl]propan-1-one Chemical compound C1N(C(=O)CC)CC[C@@H](C)[C@H]1N(C)C1=NC=NC2=C1C(F)=CN2 VNFSWYNIMVHZSO-PWSUYJOCSA-N 0.000 claims 1
- UXLDFTUCNFDMOT-UHFFFAOYSA-N 2,3-dihydroxy-2-(2-methylbenzoyl)butanedioic acid Chemical compound CC1=CC=CC=C1C(=O)C(O)(C(O)C(O)=O)C(O)=O UXLDFTUCNFDMOT-UHFFFAOYSA-N 0.000 claims 1
- OOKSMYZBWRKRGU-UHFFFAOYSA-N 2-benzoyl-2,3-dihydroxybutanedioic acid Chemical compound OC(=O)C(O)C(O)(C(O)=O)C(=O)C1=CC=CC=C1 OOKSMYZBWRKRGU-UHFFFAOYSA-N 0.000 claims 1
- MTRMACOHLXKTOY-PWSUYJOCSA-N 3,3,3-trifluoro-1-[(3r,4r)-4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]propan-1-one Chemical compound C[C@@H]1CCN(C(=O)CC(F)(F)F)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 MTRMACOHLXKTOY-PWSUYJOCSA-N 0.000 claims 1
- KWAQEXMNVBTIQE-PWSUYJOCSA-N 3,3,3-trifluoro-1-[(3r,4r)-4-methyl-3-[methyl-(5-methyl-7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]propan-1-one Chemical compound C[C@@H]1CCN(C(=O)CC(F)(F)F)C[C@@H]1N(C)C1=NC=NC2=C1C(C)=CN2 KWAQEXMNVBTIQE-PWSUYJOCSA-N 0.000 claims 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 125000005153 alkyl sulfamoyl group Chemical group 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 125000005135 aryl sulfinyl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010928 autoimmune thyroid disease Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 239000006184 cosolvent Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- XPOHSMZMNWDIJI-PWSUYJOCSA-N methyl (3r,4r)-4-methyl-3-[methyl(7h-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidine-1-carboxylate Chemical compound C1N(C(=O)OC)CC[C@@H](C)[C@H]1N(C)C1=NC=NC2=C1C=CN2 XPOHSMZMNWDIJI-PWSUYJOCSA-N 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- URCTYVNPUZEJJF-OCCSQVGLSA-N n-methyl-n-[(3r,4r)-4-methyl-1-propylsulfonylpiperidin-3-yl]-7h-pyrrolo[2,3-d]pyrimidin-4-amine Chemical compound C1N(S(=O)(=O)CCC)CC[C@@H](C)[C@H]1N(C)C1=NC=NC2=C1C=CN2 URCTYVNPUZEJJF-OCCSQVGLSA-N 0.000 claims 1
- 238000010899 nucleation Methods 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 235000002906 tartaric acid Nutrition 0.000 claims 1
- 239000011975 tartaric acid Substances 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 238000002689 xenotransplantation Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US29477501P | 2001-05-31 | 2001-05-31 | |
| US34104801P | 2001-12-06 | 2001-12-06 | |
| PCT/IB2002/001905 WO2002096909A1 (en) | 2001-05-31 | 2002-05-29 | Optical resolution of (1-benzyl-4-methylpiperidin-3-yl) -methylamine and the use thereof for the preparation of pyrrolo 2,3-pyrimidine derivatives as protein kinases inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004534047A JP2004534047A (ja) | 2004-11-11 |
| JP2004534047A5 true JP2004534047A5 (enExample) | 2005-12-22 |
| JP4381137B2 JP4381137B2 (ja) | 2009-12-09 |
Family
ID=26968730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003500088A Expired - Lifetime JP4381137B2 (ja) | 2001-05-31 | 2002-05-29 | （１−ベンジル−４−メチルピペリジン−３−イル）−メチルアミンの光学分割および蛋白質キナーゼ阻害剤としてのピロロ２，３−ピリミジン誘導体製造のためのその使用 |
Country Status (52)
Families Citing this family (123)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8474101A1 (es) | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| GEP20053479B (en) | 1999-12-10 | 2005-03-25 | Pfizer Prod Inc | Pyrrolo[2,3-d]Pyrimidine Compounds, Pharmaceutical Composition Containing the Same and Use |
| EA006153B1 (ru) * | 2000-06-26 | 2005-10-27 | Пфайзер Продактс Инк. | СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ |
| GT200200234A (es) | 2001-12-06 | 2003-06-27 | Compuestos cristalinos novedosos | |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| RS51752B (sr) | 2002-07-29 | 2011-12-31 | Rigel Pharmaceuticals | Metode tretiranja i prevencije autoimunih oboljenja jedinjenjima 2,4-pirimidindiamina |
| WO2004019941A1 (en) * | 2002-08-27 | 2004-03-11 | Merck Patent Gmbh | Glycinamide derivatives as raf-kinase inhibitors |
| AU2003276591A1 (en) | 2002-11-26 | 2004-06-18 | Pfizer Products Inc. | Method of treatment of transplant rejection |
| HRP20130602T1 (en) | 2003-07-30 | 2013-07-31 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| KR20070006889A (ko) * | 2004-05-03 | 2007-01-11 | 노파르티스 아게 | Ｓ1ｐ 수용체 작용제 및 ｊａｋ3 키나제 억제제를 포함하는조합물 |
| MXPA06015237A (es) | 2004-06-29 | 2007-12-10 | Amgen Inc | Pirrolo[2-3-d]pirimidinas que modulan la actividad de ack1 y lck. |
| WO2006017443A2 (en) | 2004-08-02 | 2006-02-16 | Osi Pharmaceuticals, Inc. | Aryl-amino substituted pyrrolopyrimidine multi-kinase inhibiting compounds |
| AU2005309019A1 (en) * | 2004-11-24 | 2006-06-01 | Novartis Ag | Combinations of JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors |
| AR054416A1 (es) | 2004-12-22 | 2007-06-27 | Incyte Corp | Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas. |
| CA2608367C (en) | 2005-06-08 | 2014-08-19 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US8163767B2 (en) | 2005-07-14 | 2012-04-24 | Astellas Pharma Inc. | Heterocyclic Janus Kinase 3 inhibitors |
| CN102127078A (zh) | 2005-07-14 | 2011-07-20 | 安斯泰来制药株式会社 | Janus激酶3的杂环类抑制剂 |
| RU2384583C2 (ru) | 2005-07-29 | 2010-03-20 | Пфайзер Продактс Инк. | ПИРРОЛО[2,3-d]ПИРИМИДИНОВЫЕ ПРОИЗВОДНЫЕ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ И СИНТЕЗ |
| WO2007038215A1 (en) | 2005-09-22 | 2007-04-05 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| ATE525374T1 (de) | 2005-12-13 | 2011-10-15 | Incyte Corp | Heteroarylsubstituierte pyrroloä2,3-büpyridine und pyrroloä2,3-büpyrimidine als januskinaseinhibitoren |
| ES2622493T3 (es) | 2006-02-24 | 2017-07-06 | Rigel Pharmaceuticals, Inc. | Composiciones y métodos para la inhibición de la ruta de JAK |
| GB0605691D0 (en) * | 2006-03-21 | 2006-05-03 | Novartis Ag | Organic Compounds |
| JP5492565B2 (ja) | 2006-12-22 | 2014-05-14 | インサイト・コーポレイション | Ｊａｎｕｓキナーゼ阻害剤としての置換複素環 |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| ES2467665T5 (es) | 2007-06-13 | 2022-11-03 | Incyte Holdings Corp | Sales del inhibidor de cinasas Janus (R)-3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo |
| KR20120115413A (ko) * | 2007-07-11 | 2012-10-17 | 화이자 인코포레이티드 | 안구 건조증 치료용 약학 조성물 및 방법 |
| AU2009214440B2 (en) | 2008-02-15 | 2014-09-25 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases |
| SG191660A1 (en) | 2008-03-11 | 2013-07-31 | Incyte Corp | Azetidine and cyclobutane derivatives as jak inhibitors |
| AU2009244897B2 (en) | 2008-04-16 | 2014-11-13 | Alexion Pharmaceuticals, Inc. | 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| WO2009131687A2 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| RU2011105768A (ru) * | 2008-08-01 | 2012-09-10 | Биокрист Фармасьютикалз, Инк. (Us) | Производные пиперидина в качестве ингибиторов jakз |
| PT2384326E (pt) * | 2008-08-20 | 2014-06-09 | Zoetis Llc | Compostos de pirrolo[2,3-d]pirimidina |
| WO2010093808A1 (en) * | 2009-02-11 | 2010-08-19 | Reaction Biology Corp. | Selective kinase inhibitors |
| EP3026052A1 (en) | 2009-04-20 | 2016-06-01 | Auspex Pharmaceuticals, Inc. | Preparation of deuterated piperidine inhibitors of janus kinase 3 |
| JP6172939B2 (ja) | 2009-05-22 | 2017-08-02 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｋ阻害薬としての３−［４−（７ｈ−ピロロ［２，３−ｄ］ピリミジン−４−イル）−１ｈ−ピラゾール−１−イル］オクタン−またはヘプタン−ニトリル |
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