CN102428087B - 用作激酶抑制剂的咪唑并吡嗪类化合物 - Google Patents
用作激酶抑制剂的咪唑并吡嗪类化合物 Download PDFInfo
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- CN102428087B CN102428087B CN201080021532.3A CN201080021532A CN102428087B CN 102428087 B CN102428087 B CN 102428087B CN 201080021532 A CN201080021532 A CN 201080021532A CN 102428087 B CN102428087 B CN 102428087B
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- 0 C*N1CC(COC)OCC1 Chemical compound C*N1CC(COC)OCC1 0.000 description 11
- XIMBBVSHOFBHCU-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1NC(c1c(C)nc(c(N2CCOCC2)n2)[n]1cc2Cl)=O)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1NC(c1c(C)nc(c(N2CCOCC2)n2)[n]1cc2Cl)=O)=O XIMBBVSHOFBHCU-UHFFFAOYSA-N 0.000 description 1
- OOQVHKXJHPLWIX-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCN1C(C)(c1c[n](cc(nc2N3CCOCC3)Br)c2n1)C#N)=O Chemical compound CC(C)(C)OC(N(CC1)CCN1C(C)(c1c[n](cc(nc2N3CCOCC3)Br)c2n1)C#N)=O OOQVHKXJHPLWIX-UHFFFAOYSA-N 0.000 description 1
- SLZBUGMRUKWZSQ-UHFFFAOYSA-N CC(C)(C1)OCCN1N Chemical compound CC(C)(C1)OCCN1N SLZBUGMRUKWZSQ-UHFFFAOYSA-N 0.000 description 1
- BLILYDUMQQSINV-UHFFFAOYSA-N CC(C1)OCCN1NC Chemical compound CC(C1)OCCN1NC BLILYDUMQQSINV-UHFFFAOYSA-N 0.000 description 1
- SXKHGQBGFSGDIW-UHFFFAOYSA-N CC(c1c[n](cc(nc2N3CCOCC3)Br)c2n1)=O Chemical compound CC(c1c[n](cc(nc2N3CCOCC3)Br)c2n1)=O SXKHGQBGFSGDIW-UHFFFAOYSA-N 0.000 description 1
- WOQWZFFDMVYHSZ-UHFFFAOYSA-N CCOC(c1c[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1)=O Chemical compound CCOC(c1c[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1)=O WOQWZFFDMVYHSZ-UHFFFAOYSA-N 0.000 description 1
- HJMCQRXFJLZXRT-UHFFFAOYSA-N CN(CC1)CCN1C(c1c[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1)=O Chemical compound CN(CC1)CCN1C(c1c[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1)=O HJMCQRXFJLZXRT-UHFFFAOYSA-N 0.000 description 1
- KRYUJHHIZMCDHF-UHFFFAOYSA-N COC(CC(C1)OCCN1N)=O Chemical compound COC(CC(C1)OCCN1N)=O KRYUJHHIZMCDHF-UHFFFAOYSA-N 0.000 description 1
- HNRYBEBMFRJUCR-UHFFFAOYSA-N CS(N1CCN(Cc2c[n](cc(-c3cc(O)ccc3)nc3N4CCOCC4)c3n2)CC1)(=O)=O Chemical compound CS(N1CCN(Cc2c[n](cc(-c3cc(O)ccc3)nc3N4CCOCC4)c3n2)CC1)(=O)=O HNRYBEBMFRJUCR-UHFFFAOYSA-N 0.000 description 1
- AWIHYPXBMZYRCC-UHFFFAOYSA-N Cc(nc(c(Br)n1)[n]2cc1Br)c2Br Chemical compound Cc(nc(c(Br)n1)[n]2cc1Br)c2Br AWIHYPXBMZYRCC-UHFFFAOYSA-N 0.000 description 1
- ZALQLJINEGWSSO-UHFFFAOYSA-N Cc(nc12)c[n]1c(Cl)c(-c1ccncc1)nc2N1CCOCC1 Chemical compound Cc(nc12)c[n]1c(Cl)c(-c1ccncc1)nc2N1CCOCC1 ZALQLJINEGWSSO-UHFFFAOYSA-N 0.000 description 1
- QALQAQUBQWCUHV-UHFFFAOYSA-N Cc1c(C2CCN(C)CC2)[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1 Chemical compound Cc1c(C2CCN(C)CC2)[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1 QALQAQUBQWCUHV-UHFFFAOYSA-N 0.000 description 1
- LFMSMFUCHFSNRT-UHFFFAOYSA-N Cc1c(C2CCNCC2)[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1 Chemical compound Cc1c(C2CCNCC2)[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1 LFMSMFUCHFSNRT-UHFFFAOYSA-N 0.000 description 1
- VPZRATFCWYCGKR-UHFFFAOYSA-N Cc1c[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1 Chemical compound Cc1c[n](cc(-c2c(cn[nH]3)c3ccc2)nc2N3CCOCC3)c2n1 VPZRATFCWYCGKR-UHFFFAOYSA-N 0.000 description 1
- HJRORMLFDOYZDM-UHFFFAOYSA-N ClCc1c[n](cc(nc2N3CCOCC3)Br)c2n1 Chemical compound ClCc1c[n](cc(nc2N3CCOCC3)Br)c2n1 HJRORMLFDOYZDM-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
- C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
- C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
- C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
- C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
- C07D243/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Molecular Biology (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Gastroenterology & Hepatology (AREA)
- Transplantation (AREA)
- Surgery (AREA)
- Pain & Pain Management (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09380079.5 | 2009-04-16 | ||
| EP09380079 | 2009-04-16 | ||
| PCT/GB2010/000773 WO2010119264A1 (en) | 2009-04-16 | 2010-04-16 | Imidazopyrazines for use as kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102428087A CN102428087A (zh) | 2012-04-25 |
| CN102428087B true CN102428087B (zh) | 2015-06-17 |
Family
ID=40940522
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201080021532.3A Active CN102428087B (zh) | 2009-04-16 | 2010-04-16 | 用作激酶抑制剂的咪唑并吡嗪类化合物 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8778935B2 (enExample) |
| EP (1) | EP2419429B1 (enExample) |
| JP (1) | JP5805623B2 (enExample) |
| KR (2) | KR101792837B1 (enExample) |
| CN (1) | CN102428087B (enExample) |
| AU (1) | AU2010238361B2 (enExample) |
| BR (1) | BRPI1014572B8 (enExample) |
| CA (1) | CA2756759C (enExample) |
| DK (1) | DK2419429T3 (enExample) |
| EA (1) | EA022629B1 (enExample) |
| ES (1) | ES2475091T3 (enExample) |
| IL (1) | IL215297A (enExample) |
| MX (1) | MX2011010915A (enExample) |
| NZ (1) | NZ596185A (enExample) |
| SG (1) | SG175195A1 (enExample) |
| WO (1) | WO2010119264A1 (enExample) |
| ZA (1) | ZA201107717B (enExample) |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| AU2010226490A1 (en) | 2009-03-20 | 2011-10-06 | Amgen Inc. | Inhibitors of PI3 kinase |
| NZ599597A (en) | 2009-10-30 | 2013-05-31 | Janssen Pharmaceutica Nv | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS |
| CA2787714C (en) | 2010-01-22 | 2019-04-09 | Joaquin Pastor Fernandez | Inhibitors of pi3 kinase |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| TW201200518A (en) * | 2010-03-10 | 2012-01-01 | Kalypsys Inc | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| CA2797118C (en) | 2010-04-22 | 2021-03-30 | Vertex Pharmaceuticals Incorporated | Process of producing cycloalkylcarboxamido-indole compounds |
| US20130131057A1 (en) | 2010-05-13 | 2013-05-23 | Centro Nacional De Investigaciones Oncologicas (Cnio | New bicyclic compounds as pi3-k and mtor inhibitors |
| EP2444084A1 (en) * | 2010-10-21 | 2012-04-25 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Use of PI3K inibitors for the treatment of obesity |
| WO2012052745A1 (en) | 2010-10-21 | 2012-04-26 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Combinations of pi3k inhibitors with a second anti -tumor agent |
| TWI617559B (zh) | 2010-12-22 | 2018-03-11 | 江蘇恆瑞醫藥股份有限公司 | 2-芳基咪唑并[1,2-b]嗒.2-苯基咪唑并[1,2-a]吡啶,和2-苯基咪唑并[1,2-a]吡衍生物 |
| EP2524918A1 (en) | 2011-05-19 | 2012-11-21 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Imidazopyrazines derivates as kinase inhibitors |
| WO2013000924A1 (en) | 2011-06-27 | 2013-01-03 | Janssen Pharmaceutica Nv | 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES |
| AU2013251475B2 (en) | 2012-04-26 | 2018-01-04 | The General Hospital Corporation | Agents and methods for treating and preventing seborrheic keratosis |
| CN103450204B (zh) * | 2012-05-31 | 2016-08-17 | 中国科学院上海药物研究所 | 吡咯[2,1-f][1,2,4]并三嗪类化合物,其制备方法及用途 |
| CN102675323B (zh) * | 2012-06-01 | 2014-04-09 | 南京药石药物研发有限公司 | 吡咯并[2,1-f][1,2,4]三嗪衍生物及其抗肿瘤用途 |
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| MX2011010915A (es) | 2012-01-27 |
| AU2010238361B2 (en) | 2015-08-06 |
| EA201101497A1 (ru) | 2012-04-30 |
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| US8778935B2 (en) | 2014-07-15 |
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| KR101792837B1 (ko) | 2017-11-02 |
| NZ596185A (en) | 2013-01-25 |
| BRPI1014572A2 (pt) | 2016-04-26 |
| BRPI1014572B1 (pt) | 2021-07-13 |
| JP5805623B2 (ja) | 2015-11-04 |
| CA2756759C (en) | 2017-11-07 |
| ES2475091T3 (es) | 2014-07-10 |
| KR20170116250A (ko) | 2017-10-18 |
| JP2012524053A (ja) | 2012-10-11 |
| DK2419429T3 (da) | 2014-06-23 |
| EA022629B1 (ru) | 2016-02-29 |
| KR20120034613A (ko) | 2012-04-12 |
| AU2010238361A1 (en) | 2011-11-10 |
| EP2419429B1 (en) | 2014-03-26 |
| US20120083492A1 (en) | 2012-04-05 |
| WO2010119264A1 (en) | 2010-10-21 |
| CA2756759A1 (en) | 2010-10-21 |
| IL215297A0 (en) | 2011-12-29 |
| ZA201107717B (en) | 2015-08-26 |
| BRPI1014572B8 (pt) | 2022-07-19 |
| IL215297A (en) | 2016-08-31 |
| CN102428087A (zh) | 2012-04-25 |
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