JP2011500806A5 - - Google Patents
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- JP2011500806A5 JP2011500806A5 JP2010531018A JP2010531018A JP2011500806A5 JP 2011500806 A5 JP2011500806 A5 JP 2011500806A5 JP 2010531018 A JP2010531018 A JP 2010531018A JP 2010531018 A JP2010531018 A JP 2010531018A JP 2011500806 A5 JP2011500806 A5 JP 2011500806A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pyrrolo
- pyrazol
- pyrazin
- independently
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 32
- 229910052760 oxygen Inorganic materials 0.000 claims 32
- 229910052717 sulfur Inorganic materials 0.000 claims 31
- 125000005842 heteroatom Chemical group 0.000 claims 20
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 229920006395 saturated elastomer Polymers 0.000 claims 16
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 15
- 125000003545 alkoxy group Chemical group 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 8
- 125000002393 azetidinyl group Chemical group 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 6
- -1 1H-pyrazol-4-yl Chemical group 0.000 claims 6
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 5
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000006719 (C6-C10) aryl (C1-C6) alkyl group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 2
- 101000600756 Homo sapiens 3-phosphoinositide-dependent protein kinase 1 Proteins 0.000 claims 2
- 101001117146 Homo sapiens [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial Proteins 0.000 claims 2
- 102100024148 [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial Human genes 0.000 claims 2
- 230000001668 ameliorated effect Effects 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- AMYZYDRRAXHIPU-SNVBAGLBSA-N (2r)-1-[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]oxypropan-2-amine Chemical class C[C@@H](N)COC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 AMYZYDRRAXHIPU-SNVBAGLBSA-N 0.000 claims 1
- HAQTZVJKKNBQNQ-SNVBAGLBSA-N (2r)-2-[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]oxypropan-1-amine Chemical class NC[C@@H](C)OC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 HAQTZVJKKNBQNQ-SNVBAGLBSA-N 0.000 claims 1
- AMYZYDRRAXHIPU-JTQLQIEISA-N (2s)-1-[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]oxypropan-2-amine Chemical class C[C@H](N)COC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 AMYZYDRRAXHIPU-JTQLQIEISA-N 0.000 claims 1
- HAQTZVJKKNBQNQ-JTQLQIEISA-N (2s)-2-[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]oxypropan-1-amine Chemical class NC[C@H](C)OC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 HAQTZVJKKNBQNQ-JTQLQIEISA-N 0.000 claims 1
- NHACWTVBXCUZGE-UHFFFAOYSA-N 1-[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]azetidin-3-ol Chemical compound C1C(O)CN1C1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 NHACWTVBXCUZGE-UHFFFAOYSA-N 0.000 claims 1
- RYUQEHUMEFJBIN-UHFFFAOYSA-N 1-[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]piperidin-4-ol Chemical compound C1CC(O)CCN1C1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 RYUQEHUMEFJBIN-UHFFFAOYSA-N 0.000 claims 1
- KWGCBFCBCQFNFN-UHFFFAOYSA-N 2-[4-[3-(6-piperidin-4-yloxypyrazin-2-yl)-1h-pyrrolo[2,3-b]pyridin-5-yl]pyrazol-1-yl]ethanol Chemical compound C1=NN(CCO)C=C1C1=CN=C(NC=C2C=3N=C(OC4CCNCC4)C=NC=3)C2=C1 KWGCBFCBCQFNFN-UHFFFAOYSA-N 0.000 claims 1
- KCNZNTAZCKXQAW-UHFFFAOYSA-N 2-[[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]amino]ethanol Chemical compound OCCNC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 KCNZNTAZCKXQAW-UHFFFAOYSA-N 0.000 claims 1
- FLHIOOJOWXRXKR-UHFFFAOYSA-N 3,3,3-trifluoro-2-[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]oxypropan-1-amine Chemical compound NCC(C(F)(F)F)OC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 FLHIOOJOWXRXKR-UHFFFAOYSA-N 0.000 claims 1
- RMERCXKBQWJSNU-UHFFFAOYSA-N 3-(6-cyclohexyloxypyrazin-2-yl)-5-(1-methylpyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound C1=NN(C)C=C1C1=CN=C(NC=C2C=3N=C(OC4CCCCC4)C=NC=3)C2=C1 RMERCXKBQWJSNU-UHFFFAOYSA-N 0.000 claims 1
- YYEIRBSEECPYGO-UHFFFAOYSA-N 3-(6-piperidin-4-yloxypyrazin-2-yl)-1-(2,2,2-trifluoroethyl)-5-[1-(2,2,2-trifluoroethyl)pyrazol-4-yl]pyrrolo[2,3-b]pyridine Chemical compound C1=NN(CC(F)(F)F)C=C1C1=CN=C(N(CC(F)(F)F)C=C2C=3N=C(OC4CCNCC4)C=NC=3)C2=C1 YYEIRBSEECPYGO-UHFFFAOYSA-N 0.000 claims 1
- QXVNTBKMWPQELL-UHFFFAOYSA-N 3-(6-piperidin-4-yloxypyrazin-2-yl)-5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound C1CNCCC1OC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 QXVNTBKMWPQELL-UHFFFAOYSA-N 0.000 claims 1
- QLDBOOBFMMTKLI-UHFFFAOYSA-N 3-(6-piperidin-4-yloxypyrazin-2-yl)-5-[1-(2,2,2-trifluoroethyl)pyrazol-4-yl]-1h-pyrrolo[2,3-b]pyridine Chemical compound C1=NN(CC(F)(F)F)C=C1C1=CN=C(NC=C2C=3N=C(OC4CCNCC4)C=NC=3)C2=C1 QLDBOOBFMMTKLI-UHFFFAOYSA-N 0.000 claims 1
- SDIHVAHCAIUTLE-UHFFFAOYSA-N 3-[6-(azetidin-3-yloxy)pyrazin-2-yl]-5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound C1NCC1OC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 SDIHVAHCAIUTLE-UHFFFAOYSA-N 0.000 claims 1
- NIGKXPUDCBICHV-CQSZACIVSA-N 3-[6-[(3r)-piperidin-3-yl]oxypyrazin-2-yl]-5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound C1CCNC[C@@H]1OC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 NIGKXPUDCBICHV-CQSZACIVSA-N 0.000 claims 1
- XLIUDGBZOFWPSD-NVXWUHKLSA-N 3-[6-[(3r,4r)-3-fluoropiperidin-4-yl]oxypyrazin-2-yl]-5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound F[C@@H]1CNCC[C@H]1OC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 XLIUDGBZOFWPSD-NVXWUHKLSA-N 0.000 claims 1
- NIGKXPUDCBICHV-AWEZNQCLSA-N 3-[6-[(3s)-piperidin-3-yl]oxypyrazin-2-yl]-5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound C1CCNC[C@H]1OC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 NIGKXPUDCBICHV-AWEZNQCLSA-N 0.000 claims 1
- OAVHEXVWAVEAKU-UHFFFAOYSA-N 3-[[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]amino]propan-1-ol Chemical compound OCCCNC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 OAVHEXVWAVEAKU-UHFFFAOYSA-N 0.000 claims 1
- UGGNJBTVPPMKJQ-UHFFFAOYSA-N 4-[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]oxycyclohexan-1-ol Chemical compound C1CC(O)CCC1OC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 UGGNJBTVPPMKJQ-UHFFFAOYSA-N 0.000 claims 1
- AVLRGAAKHKPNLQ-UHFFFAOYSA-N 5-(1-ethylpyrazol-4-yl)-3-(6-piperidin-4-yloxypyrazin-2-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound C1=NN(CC)C=C1C1=CN=C(NC=C2C=3N=C(OC4CCNCC4)C=NC=3)C2=C1 AVLRGAAKHKPNLQ-UHFFFAOYSA-N 0.000 claims 1
- FARXKXQFXLRXAN-UHFFFAOYSA-N 5-(1-methylpyrazol-4-yl)-3-(6-piperazin-1-ylpyrazin-2-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound C1=NN(C)C=C1C1=CN=C(NC=C2C=3N=C(C=NC=3)N3CCNCC3)C2=C1 FARXKXQFXLRXAN-UHFFFAOYSA-N 0.000 claims 1
- DWOWQKVGKYFEBF-UHFFFAOYSA-N 5-(1-methylpyrazol-4-yl)-3-(6-piperidin-4-yloxypyrazin-2-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound C1=NN(C)C=C1C1=CN=C(NC=C2C=3N=C(OC4CCNCC4)C=NC=3)C2=C1 DWOWQKVGKYFEBF-UHFFFAOYSA-N 0.000 claims 1
- XOXNVWUVMYCOKB-UHFFFAOYSA-N 5-(1h-pyrazol-4-yl)-3-[6-[3-(trifluoromethyl)azetidin-3-yl]oxypyrazin-2-yl]-1h-pyrrolo[2,3-b]pyridine Chemical compound C=1N=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=NC=1OC1(C(F)(F)F)CNC1 XOXNVWUVMYCOKB-UHFFFAOYSA-N 0.000 claims 1
- QZVJPBOTFOEGJG-UHFFFAOYSA-N 5-[1-(cyclopropylmethyl)pyrazol-4-yl]-3-(6-piperidin-4-yloxypyrazin-2-yl)-1h-pyrrolo[2,3-b]pyridine Chemical compound C1=C(C=2C=C3C(C=4N=C(OC5CCNCC5)C=NC=4)=CNC3=NC=2)C=NN1CC1CC1 QZVJPBOTFOEGJG-UHFFFAOYSA-N 0.000 claims 1
- MYMXKHWSRBHYFK-SHTZXODSSA-N C1C[C@@H](O)CC[C@@H]1NC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 Chemical compound C1C[C@@H](O)CC[C@@H]1NC1=CN=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=N1 MYMXKHWSRBHYFK-SHTZXODSSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- QOQLOXINPYFCMT-UHFFFAOYSA-N n-[2-[6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-yl]oxyethyl]cyclohexanamine Chemical compound C1CCCCC1NCCOC(N=1)=CN=CC=1C(C1=C2)=CNC1=NC=C2C=1C=NNC=1 QOQLOXINPYFCMT-UHFFFAOYSA-N 0.000 claims 1
- LGBSCWUGPLIKEM-UHFFFAOYSA-N n-ethyl-n-piperidin-4-yl-6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-amine Chemical compound C=1N=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=NC=1N(CC)C1CCNCC1 LGBSCWUGPLIKEM-UHFFFAOYSA-N 0.000 claims 1
- XSNSTCOTKCEWOW-UHFFFAOYSA-N n-methyl-6-[5-(1-methylpyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]-n-piperidin-4-ylpyrazin-2-amine Chemical class C=1N=CC(C=2C3=CC(=CN=C3NC=2)C2=CN(C)N=C2)=NC=1N(C)C1CCNCC1 XSNSTCOTKCEWOW-UHFFFAOYSA-N 0.000 claims 1
- FUYYQHISLWOVHJ-UHFFFAOYSA-N n-piperidin-4-yl-n-propyl-6-[5-(1h-pyrazol-4-yl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyrazin-2-amine Chemical compound C=1N=CC(C=2C3=CC(=CN=C3NC=2)C2=CNN=C2)=NC=1N(CCC)C1CCNCC1 FUYYQHISLWOVHJ-UHFFFAOYSA-N 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34307P | 2007-10-25 | 2007-10-25 | |
| PCT/US2008/011971 WO2009054941A1 (en) | 2007-10-25 | 2008-10-21 | Therapeutic compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011500806A JP2011500806A (ja) | 2011-01-06 |
| JP2011500806A5 true JP2011500806A5 (https=) | 2011-12-01 |
Family
ID=40579830
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010531018A Pending JP2011500806A (ja) | 2007-10-25 | 2008-10-21 | 治療用化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8183245B2 (https=) |
| EP (1) | EP2211620B1 (https=) |
| JP (1) | JP2011500806A (https=) |
| AU (1) | AU2008317406B2 (https=) |
| CA (1) | CA2703125C (https=) |
| WO (1) | WO2009054941A1 (https=) |
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2211620B1 (en) * | 2007-10-25 | 2013-12-25 | Merck Sharp & Dohme Corp. | 3-PYRAZIN SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AS JANUS KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES |
| JP5576370B2 (ja) * | 2008-08-06 | 2014-08-20 | ファイザー・インク | Ｃｈｋ−１阻害剤としての６置換２−ヘテロシクリルアミノピラジン化合物 |
| WO2010068483A2 (en) | 2008-11-25 | 2010-06-17 | University Of Rochester | Mlk inhibitors and methods of use |
| DE102009019962A1 (de) * | 2009-05-05 | 2010-11-11 | Merck Patent Gmbh | 3-([1,2,3]Triazol-4-yl)-pyrrolo[2,3-b]pyridinderivate |
| ES2540964T3 (es) * | 2009-06-08 | 2015-07-15 | Takeda Pharmaceutical Company Limited | Compuestos de dihidropirrolonaftiridinona como inhibidores de JAK |
| EP2338888A1 (en) * | 2009-12-24 | 2011-06-29 | Almirall, S.A. | Imidazopyridine derivatives as JAK inhibitors |
| SA111320200B1 (ar) | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| WO2011137022A1 (en) * | 2010-04-27 | 2011-11-03 | Merck Sharp & Dohme Corp. | Azaindoles as janus kinase inhibitors |
| JP6086326B2 (ja) | 2010-05-24 | 2017-03-01 | ユニヴァーシティー オブ ロチェスター | 二環式ヘテロアリールキナーゼ阻害剤および使用方法 |
| WO2012054364A2 (en) * | 2010-10-22 | 2012-04-26 | Merck Sharp & Dohme Corp. | Bicyclic diamines as janus kinase inhibitors |
| DE102010049877A1 (de) | 2010-11-01 | 2012-05-03 | Merck Patent Gmbh | 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate |
| KR101905927B1 (ko) | 2010-11-17 | 2018-10-08 | 이도르시아 파마슈티컬스 리미티드 | 가교된 스피로［２．４］헵탄 에스테르 유도체 |
| EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
| DE102010053347A1 (de) * | 2010-12-03 | 2012-06-06 | Merck Patent Gmbh | 3-Hetaryl-substituierte Pyrrolo[2,3-b] pyridin-derivative als PDK1-Inhibitoren |
| DE102011008352A1 (de) | 2011-01-12 | 2012-07-12 | Merck Patent Gmbh | 5-([1,2,3]Triazol-4-yl)-7H-pyrrolo-[2,3-d]pyrimidinderivate |
| DE102011009961A1 (de) | 2011-02-01 | 2012-08-02 | Merck Patent Gmbh | 7-Azaindolderivate |
| CN103547580B (zh) | 2011-03-22 | 2016-12-07 | 阿迪维纳斯疗法有限公司 | 取代的稠合三环化合物、其组合物及医药用途 |
| DE102011105469A1 (de) * | 2011-06-24 | 2012-12-27 | Merck Patent Gmbh | 7-Azaindolderivate |
| EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| DE102011119127A1 (de) | 2011-11-22 | 2013-05-23 | Merck Patent Gmbh | 3-Cyanaryl-1H-pyrrolo[2.3-b]pyridin-Derivate |
| PT2796460T (pt) | 2011-12-21 | 2018-11-05 | Shanghai hengrui pharmaceutical co ltd | Derivado pirrole de anel heteroarilo de seis membros, método de preparação do mesmo e suas utilizações médicas |
| JP6280546B2 (ja) | 2012-06-26 | 2018-02-14 | デル マー ファーマシューティカルズ | ジアンヒドロガラクチトール、ジアセチルジアンヒドロガラクチトール、ジブロモズルシトール、又はこれらの類似体若しくは誘導体を用いた、遺伝子多型又はａｈｉ１の調節不全若しくは変異を有する患者におけるチロシンキナーゼインヒビター抵抗性悪性腫瘍を処置するための方法 |
| WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
| US9593115B2 (en) | 2012-09-21 | 2017-03-14 | Advinus Therapeutics Ltd. | Substituted fused tricyclic compounds, compositions, and medicinal applications thereof |
| DE102012019369A1 (de) | 2012-10-02 | 2014-04-03 | Merck Patent Gmbh | 7-Azaindolderivat |
| CN104884059B (zh) | 2012-11-30 | 2018-08-10 | 罗切斯特大学 | 用于hiv/aids治疗的混合谱系激酶抑制剂 |
| KR20160061911A (ko) | 2013-04-08 | 2016-06-01 | 데니스 엠. 브라운 | 최적하 투여된 화학 화합물의 치료 효과 |
| WO2015131080A1 (en) | 2014-02-28 | 2015-09-03 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| TWI788655B (zh) | 2015-02-27 | 2023-01-01 | 美商林伯士拉克許米公司 | 酪胺酸蛋白質激酶2(tyk2)抑制劑及其用途 |
| TWI707852B (zh) * | 2015-09-02 | 2020-10-21 | 美商林伯士拉克許米公司 | Tyk2 抑制劑及其用途 |
| MX388591B (es) | 2016-06-30 | 2025-03-20 | Daewoong Pharmaceutical Co Ltd | Derivados de pirazolopirimidina como inhibidor de cinasa. |
| WO2018041989A1 (en) | 2016-09-02 | 2018-03-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating refractory celiac disease type 2 |
| KR20190084299A (ko) * | 2016-11-23 | 2019-07-16 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 피롤로 6-원 헤테로방향족 고리 유도체의 제조 방법 및 그의 중간체 |
| WO2018134352A1 (en) * | 2017-01-20 | 2018-07-26 | Leo Pharma A/S | Bicyclic amines as novel jak kinase inhibitors |
| BR112020018094A2 (pt) | 2018-03-08 | 2020-12-22 | Incyte Corporation | Compostos de aminopirazina diol como inibidores de pi3k-¿ |
| AR117398A1 (es) * | 2018-03-12 | 2021-08-04 | Abbvie Inc | Inhibidores de la señalización mediada por tirosina cinasa 2 |
| US11046658B2 (en) | 2018-07-02 | 2021-06-29 | Incyte Corporation | Aminopyrazine derivatives as PI3K-γ inhibitors |
| EP3947737A2 (en) | 2019-04-02 | 2022-02-09 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
| SG11202110714VA (en) * | 2019-04-09 | 2021-10-28 | Plexxikon Inc | Condensed azines for ep300 or cbp modulation and indications therefor |
| EP3955920A1 (en) | 2019-04-16 | 2022-02-23 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| KR20230012539A (ko) | 2020-05-13 | 2023-01-26 | 디스크 메디슨, 인크. | 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체 |
| WO2023222565A1 (en) | 2022-05-16 | 2023-11-23 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation |
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| EP2295433A3 (en) * | 2003-03-06 | 2011-07-06 | Eisai R&D Management Co., Ltd. | JNK inhibitors |
| ES2364340T3 (es) * | 2004-03-30 | 2011-08-31 | Vertex Pharmaceuticals Incorporated | Azaindoles útiles como inhibidores de jak y otras proteína quinasas. |
| WO2006015123A1 (en) * | 2004-07-27 | 2006-02-09 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| US7361764B2 (en) * | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| EP1828180A4 (en) | 2004-12-08 | 2010-09-15 | Glaxosmithkline Llc | 1H-pyrrolo [2,3-BETA] PYRIDINE |
| US20060264442A1 (en) | 2005-05-18 | 2006-11-23 | Allergan, Inc. | Methods for the treatment of ocular and neurodegenerative conditions in a mammal |
| UA95244C2 (ru) | 2005-06-22 | 2011-07-25 | Плексикон, Инк. | Соединения и способ модулирования активности киназ, и показания для их применения |
| WO2007007919A2 (en) * | 2005-07-14 | 2007-01-18 | Astellas Pharma Inc. | Heterocyclic janus kinase 3 inhibitors |
| SG10202003901UA (en) * | 2005-12-13 | 2020-05-28 | Incyte Holdings Corp | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors |
| EP2211620B1 (en) * | 2007-10-25 | 2013-12-25 | Merck Sharp & Dohme Corp. | 3-PYRAZIN SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AS JANUS KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES |
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- 2008-10-21 EP EP08841687.0A patent/EP2211620B1/en not_active Not-in-force
- 2008-10-21 JP JP2010531018A patent/JP2011500806A/ja active Pending
- 2008-10-21 US US12/682,612 patent/US8183245B2/en not_active Expired - Fee Related
- 2008-10-21 WO PCT/US2008/011971 patent/WO2009054941A1/en not_active Ceased
- 2008-10-21 AU AU2008317406A patent/AU2008317406B2/en not_active Expired - Fee Related
- 2008-10-21 CA CA2703125A patent/CA2703125C/en not_active Expired - Fee Related
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