ES2391948T3 - Compuestos de pirazolo-pirimidina anilina útiles como inhibidores de quinasa - Google Patents
Compuestos de pirazolo-pirimidina anilina útiles como inhibidores de quinasa Download PDFInfo
- Publication number
- ES2391948T3 ES2391948T3 ES03731307T ES03731307T ES2391948T3 ES 2391948 T3 ES2391948 T3 ES 2391948T3 ES 03731307 T ES03731307 T ES 03731307T ES 03731307 T ES03731307 T ES 03731307T ES 2391948 T3 ES2391948 T3 ES 2391948T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- substituted
- cycloalkyl
- heterocycle
- heteroaryl
- 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.)
- Expired - Lifetime
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- 229940043355 kinase inhibitor Drugs 0.000 title description 6
- 239000003757 phosphotransferase inhibitor Substances 0.000 title description 6
- YKKUNOSQQQYXIQ-UHFFFAOYSA-N NC1=CC=CC=C1.N1=CN=C2C=NNC2=C1 Chemical class NC1=CC=CC=C1.N1=CN=C2C=NNC2=C1 YKKUNOSQQQYXIQ-UHFFFAOYSA-N 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 164
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 102
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 70
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 68
- 239000001257 hydrogen Substances 0.000 claims abstract description 67
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 67
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 60
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract description 59
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- 150000002431 hydrogen Chemical group 0.000 claims abstract description 49
- -1 hydroxy, methoxy Chemical group 0.000 claims abstract description 48
- 229910052736 halogen Inorganic materials 0.000 claims abstract description 45
- 150000002367 halogens Chemical group 0.000 claims abstract description 45
- 125000000547 substituted alkyl group Chemical group 0.000 claims abstract description 45
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract description 31
- 150000003839 salts Chemical class 0.000 claims abstract description 29
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 22
- 125000003342 alkenyl group Chemical group 0.000 claims abstract description 20
- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 18
- 239000012453 solvate Substances 0.000 claims abstract description 16
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract description 16
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract description 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract description 15
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract description 12
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- 125000004432 carbon atom Chemical group C* 0.000 claims description 25
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- 150000001721 carbon Chemical group 0.000 claims description 4
- 125000004122 cyclic group Chemical group 0.000 claims description 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 4
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims description 4
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims description 3
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- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims description 2
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims description 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims description 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
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- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
- 206010018634 Gouty Arthritis Diseases 0.000 claims description 2
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- 125000003277 amino group Chemical group 0.000 claims description 2
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- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 2
- 229910052794 bromium Inorganic materials 0.000 claims description 2
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims description 2
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- 239000003937 drug carrier Substances 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
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- 125000005843 halogen group Chemical group 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 239000011630 iodine Substances 0.000 claims description 2
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- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 2
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- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 abstract 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38201402P | 2002-05-20 | 2002-05-20 | |
| US382014P | 2002-05-20 | ||
| PCT/US2003/016072 WO2003099820A1 (en) | 2002-05-20 | 2003-05-16 | Pyrazolo-pyrimidine aniline compounds |
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| JP (1) | JP2005531584A (enExample) |
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| TW200401638A (en) * | 2002-06-20 | 2004-02-01 | Bristol Myers Squibb Co | Heterocyclic inhibitors of kinases |
| TWI329112B (en) * | 2002-07-19 | 2010-08-21 | Bristol Myers Squibb Co | Novel inhibitors of kinases |
| AU2003265349A1 (en) * | 2002-08-02 | 2004-02-23 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| TW200420565A (en) * | 2002-12-13 | 2004-10-16 | Bristol Myers Squibb Co | C-6 modified indazolylpyrrolotriazines |
| CN1771234A (zh) | 2003-02-05 | 2006-05-10 | 布里斯托尔-迈尔斯斯奎布公司 | 吡咯并三嗪激酶抑制剂的制备方法 |
| US7419978B2 (en) * | 2003-10-22 | 2008-09-02 | Bristol-Myers Squibb Company | Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors |
| JP2007517052A (ja) * | 2003-12-23 | 2007-06-28 | ノバルティス アクチエンゲゼルシャフト | 二環式ヘテロ環式ｐ−３８キナーゼ阻害剤 |
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| US3720674A (en) * | 1970-09-02 | 1973-03-13 | Squibb & Sons Inc | 4-amino-1h-pyrazolo(3,4-d)pyrimidine derivatives |
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| PL219736B1 (pl) | 2002-04-23 | 2015-07-31 | Bristol Myers Squibb Co | Pochodna pirolotriazynoaniliny, kompozycja farmaceutyczna i jej zastosowanie |
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2003
- 2003-05-14 TW TW092113120A patent/TW200400034A/zh unknown
- 2003-05-16 ES ES03731307T patent/ES2391948T3/es not_active Expired - Lifetime
- 2003-05-16 WO PCT/US2003/016072 patent/WO2003099820A1/en not_active Ceased
- 2003-05-16 AU AU2003241561A patent/AU2003241561A1/en not_active Abandoned
- 2003-05-16 AR ARP030101712A patent/AR040031A1/es unknown
- 2003-05-16 MY MYPI20031804A patent/MY135309A/en unknown
- 2003-05-16 EP EP03731307A patent/EP1507780B1/en not_active Expired - Lifetime
- 2003-05-16 JP JP2004507477A patent/JP2005531584A/ja not_active Withdrawn
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- 2003-05-19 US US10/440,864 patent/US6962915B2/en not_active Expired - Lifetime
- 2003-05-20 PE PE2003000490A patent/PE20040512A1/es not_active Application Discontinuation
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2004
- 2004-11-09 NO NO20044866A patent/NO20044866L/no not_active Application Discontinuation
- 2004-11-16 IS IS7534A patent/IS7534A/is unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2005531584A (ja) | 2005-10-20 |
| PL374218A1 (en) | 2005-10-03 |
| TW200400034A (en) | 2004-01-01 |
| MY135309A (en) | 2008-03-31 |
| EP1507780B1 (en) | 2012-08-22 |
| NO20044866L (no) | 2004-12-17 |
| PE20040512A1 (es) | 2004-08-25 |
| AR040031A1 (es) | 2005-03-09 |
| US6962915B2 (en) | 2005-11-08 |
| US20040023992A1 (en) | 2004-02-05 |
| AU2003241561A1 (en) | 2003-12-12 |
| EP1507780A1 (en) | 2005-02-23 |
| EP1507780A4 (en) | 2006-08-02 |
| WO2003099820A1 (en) | 2003-12-04 |
| IS7534A (is) | 2004-11-16 |
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