MX2012002317A - Compuestos de urea que contienen heteroarilo 5,6-biciclicos como inhibidores de cinasa. - Google Patents
Compuestos de urea que contienen heteroarilo 5,6-biciclicos como inhibidores de cinasa.Info
- Publication number
- MX2012002317A MX2012002317A MX2012002317A MX2012002317A MX2012002317A MX 2012002317 A MX2012002317 A MX 2012002317A MX 2012002317 A MX2012002317 A MX 2012002317A MX 2012002317 A MX2012002317 A MX 2012002317A MX 2012002317 A MX2012002317 A MX 2012002317A
- Authority
- MX
- Mexico
- Prior art keywords
- pyrrolo
- urea
- pyridin
- ylmethyl
- indol
- Prior art date
Links
- 150000003672 ureas Chemical class 0.000 title abstract 2
- 229940043355 kinase inhibitor Drugs 0.000 title description 3
- 239000003757 phosphotransferase inhibitor Substances 0.000 title description 3
- -1 CSFlR Proteins 0.000 claims abstract description 924
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims abstract description 32
- 101000851007 Homo sapiens Vascular endothelial growth factor receptor 2 Proteins 0.000 claims abstract description 29
- 102000001253 Protein Kinase Human genes 0.000 claims abstract description 16
- 108060006633 protein kinase Proteins 0.000 claims abstract description 16
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims abstract description 12
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims abstract description 12
- 102100030340 Ephrin type-A receptor 2 Human genes 0.000 claims abstract description 7
- 230000001404 mediated effect Effects 0.000 claims abstract description 7
- 108010055196 EphA2 Receptor Proteins 0.000 claims abstract description 6
- XSQUKJJJFZCRTK-UHFFFAOYSA-N urea group Chemical group NC(=O)N XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 663
- 239000004202 carbamide Substances 0.000 claims description 622
- 150000001875 compounds Chemical class 0.000 claims description 162
- 206010028980 Neoplasm Diseases 0.000 claims description 45
- 125000000217 alkyl group Chemical group 0.000 claims description 31
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 27
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 25
- 125000003118 aryl group Chemical group 0.000 claims description 25
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Substances C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 25
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 24
- 125000004199 4-trifluoromethylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C(F)(F)F 0.000 claims description 22
- 125000001072 heteroaryl group Chemical group 0.000 claims description 22
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims description 21
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 21
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 21
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims description 21
- 238000000034 method Methods 0.000 claims description 21
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 20
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 125000003342 alkenyl group Chemical group 0.000 claims description 17
- 125000004863 4-trifluoromethoxyphenyl group Chemical group [H]C1=C([H])C(OC(F)(F)F)=C([H])C([H])=C1* 0.000 claims description 16
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- 125000000304 alkynyl group Chemical group 0.000 claims description 15
- 125000005843 halogen group Chemical group 0.000 claims description 15
- 125000006276 2-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C(*)C([H])=C1[H] 0.000 claims description 14
- 125000006275 3-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C([H])C(*)=C1[H] 0.000 claims description 14
- 125000002947 alkylene group Chemical group 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 14
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims description 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 13
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims description 12
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- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims description 11
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims description 11
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 11
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- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 9
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims description 8
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- 125000004043 oxo group Chemical group O=* 0.000 claims description 8
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- 239000005441 aurora Substances 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
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- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 4
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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Landscapes
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- Organic Chemistry (AREA)
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- Cardiology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23627409P | 2009-08-24 | 2009-08-24 | |
| PCT/CN2010/076199 WO2011023081A1 (en) | 2009-08-24 | 2010-08-20 | 5,6-bicyclic heteroaryl-containing urea compounds as kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2012002317A true MX2012002317A (es) | 2012-06-25 |
Family
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Family Applications (1)
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| MX2012002317A MX2012002317A (es) | 2009-08-24 | 2010-08-20 | Compuestos de urea que contienen heteroarilo 5,6-biciclicos como inhibidores de cinasa. |
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| EP (1) | EP2470533A4 (enExample) |
| JP (1) | JP2013502444A (enExample) |
| KR (1) | KR20120089459A (enExample) |
| CN (1) | CN102066372B (enExample) |
| AU (1) | AU2010289143A1 (enExample) |
| BR (1) | BR112012003462A2 (enExample) |
| CA (1) | CA2769151A1 (enExample) |
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| EA (1) | EA201290073A1 (enExample) |
| EC (1) | ECSP12011691A (enExample) |
| IL (1) | IL218114A0 (enExample) |
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| PH (1) | PH12012500366A1 (enExample) |
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| TN (1) | TN2012000042A1 (enExample) |
| WO (1) | WO2011023081A1 (enExample) |
| ZA (1) | ZA201200890B (enExample) |
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| US8293897B2 (en) | 2008-10-14 | 2012-10-23 | Ning Xi | Compounds comprising a spiro-ring and methods of use |
| RU2011142597A (ru) | 2009-03-21 | 2013-04-27 | Саншайн Лейк Фарма Ко., Лтд. | Производные сложных эфиров аминокислот, их соли и способы применения |
| JP2013536806A (ja) * | 2010-09-01 | 2013-09-26 | アスセピオン ファーマスーティカル、インコーポレイテッド | キナーゼ阻害剤としての重水素化複素環式化合物 |
| BR112013013659B8 (pt) | 2010-12-03 | 2024-02-27 | Epizyme Inc | Compostos moduladores de enzimas epigenéticas, composição farmacêutica compreendendo ditos compostos e usos da dita composição farmacêutica para tratar câncer, câncer hematológico ou leucemia |
| CN102408426B (zh) * | 2011-09-14 | 2013-07-10 | 湖南有色凯铂生物药业有限公司 | 取代的芳香脲类化合物及其作为抗癌药物的应用 |
| FR2985257B1 (fr) * | 2011-12-28 | 2014-02-14 | Sanofi Sa | Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique |
| CN103420895A (zh) * | 2012-05-18 | 2013-12-04 | 苏州爱斯鹏药物研发有限责任公司 | 一种4-氨基吲哚的制备方法 |
| US20150284422A1 (en) | 2012-08-10 | 2015-10-08 | Epizyme, Inc. | Inhibitors of protein methyltransferase dot1l and methods of use thereof |
| WO2014039839A1 (en) | 2012-09-06 | 2014-03-13 | Epizyme, Inc. | Method of treating leukemia |
| EP2968387A4 (en) | 2013-03-15 | 2017-04-05 | Epizyme, Inc. | Methods of synthesizing substituted purine compounds |
| CN103613580B (zh) * | 2013-09-03 | 2016-02-10 | 遵义医学院 | 用于抗肿瘤药物的3-羟基吲哚-2-酮类化合物或其药学上能够接受的盐 |
| CN106279154A (zh) * | 2016-08-02 | 2017-01-04 | 叶芳 | 一种7‑氮杂吲哚‑3‑甲醛的制备方法 |
| CN108191874B (zh) * | 2018-01-16 | 2019-11-29 | 成都施贝康生物医药科技有限公司 | 一种C-Kit抑制剂及其应用 |
| CN111484442B (zh) * | 2018-06-01 | 2021-11-09 | 杭州阿诺生物医药科技有限公司 | 一种具有抗肿瘤活性的csf1r抑制剂中间体的制备方法 |
| EP3833762A4 (en) | 2018-08-09 | 2022-09-28 | Verseau Therapeutics, Inc. | Oligonucleotide compositions for targeting ccr2 and csf1r and uses thereof |
| TW202237564A (zh) * | 2020-12-11 | 2022-10-01 | 南韓商日東製藥股份有限公司 | 類鴉片受體的偏置激動劑 |
| PE20250155A1 (es) | 2021-06-14 | 2025-01-22 | Scorpion Therapeutics Inc | Derivados de la urea que pueden ser utilizados para tratar el cancer |
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-
2010
- 2010-08-20 KR KR1020127006772A patent/KR20120089459A/ko not_active Withdrawn
- 2010-08-20 IN IN1983DEN2012 patent/IN2012DN01983A/en unknown
- 2010-08-20 WO PCT/CN2010/076199 patent/WO2011023081A1/en not_active Ceased
- 2010-08-20 JP JP2012525875A patent/JP2013502444A/ja active Pending
- 2010-08-20 EP EP10811241A patent/EP2470533A4/en not_active Withdrawn
- 2010-08-20 CA CA2769151A patent/CA2769151A1/en not_active Abandoned
- 2010-08-20 EA EA201290073A patent/EA201290073A1/ru unknown
- 2010-08-20 AU AU2010289143A patent/AU2010289143A1/en not_active Abandoned
- 2010-08-20 PH PH1/2012/500366A patent/PH12012500366A1/en unknown
- 2010-08-20 BR BR112012003462A patent/BR112012003462A2/pt not_active Application Discontinuation
- 2010-08-20 SG SG2012004917A patent/SG178092A1/en unknown
- 2010-08-20 CN CN201080001560.9A patent/CN102066372B/zh not_active Expired - Fee Related
- 2010-08-20 US US12/922,527 patent/US8648086B2/en not_active Expired - Fee Related
- 2010-08-20 MX MX2012002317A patent/MX2012002317A/es not_active Application Discontinuation
-
2012
- 2012-01-26 TN TNP2012000042A patent/TN2012000042A1/en unknown
- 2012-01-26 CO CO12012075A patent/CO6491087A2/es not_active Application Discontinuation
- 2012-02-06 ZA ZA2012/00890A patent/ZA201200890B/en unknown
- 2012-02-14 IL IL218114A patent/IL218114A0/en unknown
- 2012-02-22 MA MA34647A patent/MA33559B1/fr unknown
- 2012-02-23 EC ECSP12011691 patent/ECSP12011691A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US8648086B2 (en) | 2014-02-11 |
| EP2470533A4 (en) | 2013-01-23 |
| PH12012500366A1 (en) | 2012-10-22 |
| CO6491087A2 (es) | 2012-07-31 |
| SG178092A1 (en) | 2012-03-29 |
| TN2012000042A1 (en) | 2013-09-19 |
| CA2769151A1 (en) | 2011-03-03 |
| WO2011023081A1 (en) | 2011-03-03 |
| ZA201200890B (en) | 2012-10-31 |
| CN102066372B (zh) | 2014-09-17 |
| AU2010289143A1 (en) | 2012-02-16 |
| MA33559B1 (fr) | 2012-09-01 |
| US20120122895A1 (en) | 2012-05-17 |
| ECSP12011691A (es) | 2012-04-30 |
| KR20120089459A (ko) | 2012-08-10 |
| BR112012003462A2 (pt) | 2016-02-23 |
| IN2012DN01983A (enExample) | 2015-07-24 |
| EP2470533A1 (en) | 2012-07-04 |
| CN102066372A (zh) | 2011-05-18 |
| IL218114A0 (en) | 2012-04-30 |
| EA201290073A1 (ru) | 2013-01-30 |
| JP2013502444A (ja) | 2013-01-24 |
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