JP2007510665A5 - - Google Patents
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- JP2007510665A5 JP2007510665A5 JP2006538512A JP2006538512A JP2007510665A5 JP 2007510665 A5 JP2007510665 A5 JP 2007510665A5 JP 2006538512 A JP2006538512 A JP 2006538512A JP 2006538512 A JP2006538512 A JP 2006538512A JP 2007510665 A5 JP2007510665 A5 JP 2007510665A5
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- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- groups
- alkyl
- group
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 51
- 239000000203 mixture Substances 0.000 claims 38
- 125000000623 heterocyclic group Chemical group 0.000 claims 28
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 23
- 208000034578 Multiple myelomas Diseases 0.000 claims 18
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 12
- 125000003710 aryl alkyl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims 6
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 5
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 5
- -1 Substituted Chemical class 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 210000004027 cell Anatomy 0.000 claims 4
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 3
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 206010065687 Bone loss Diseases 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 208000034951 Genetic Translocation Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 230000006907 apoptotic process Effects 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 150000003893 lactate salts Chemical class 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 230000000010 osteolytic effect Effects 0.000 claims 2
- 230000007170 pathology Effects 0.000 claims 2
- 150000004885 piperazines Chemical class 0.000 claims 2
- FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical compound C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 claims 1
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- XRWSZZJLZRKHHD-WVWIJVSJSA-N asunaprevir Chemical compound O=C([C@@H]1C[C@H](CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)(C)C)OC1=NC=C(C2=CC=C(Cl)C=C21)OC)N[C@]1(C(=O)NS(=O)(=O)C2CC2)C[C@H]1C=C XRWSZZJLZRKHHD-WVWIJVSJSA-N 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 229940125782 compound 2 Drugs 0.000 claims 1
- 229940125961 compound 24 Drugs 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- RAOIDOHSFRTOEL-UHFFFAOYSA-N tetrahydrothiophene Chemical compound C1CCSC1 RAOIDOHSFRTOEL-UHFFFAOYSA-N 0.000 claims 1
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US51791503P | 2003-11-07 | 2003-11-07 | |
| US60/517,915 | 2003-11-07 | ||
| US52642503P | 2003-12-02 | 2003-12-02 | |
| US52642603P | 2003-12-02 | 2003-12-02 | |
| US60/526,426 | 2003-12-02 | ||
| US60/526,425 | 2003-12-02 | ||
| US54601704P | 2004-02-19 | 2004-02-19 | |
| US60/546,017 | 2004-02-19 | ||
| PCT/US2004/036956 WO2005047244A2 (en) | 2003-11-07 | 2004-11-05 | Inhibition of fgfr3 and treatment of multiple myeloma |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007510665A JP2007510665A (ja) | 2007-04-26 |
| JP2007510665A5 true JP2007510665A5 (https=) | 2007-11-22 |
| JP4823914B2 JP4823914B2 (ja) | 2011-11-24 |
Family
ID=34596121
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006538526A Expired - Fee Related JP4724665B2 (ja) | 2003-11-07 | 2004-11-05 | キノリノン化合物を合成する方法 |
| JP2006538509A Expired - Fee Related JP4890255B2 (ja) | 2003-11-07 | 2004-11-05 | 改良された薬物特性を有するキノリノン化合物の薬学的に受容可能な塩 |
| JP2006538512A Expired - Fee Related JP4823914B2 (ja) | 2003-11-07 | 2004-11-05 | Ｆｇｆｒ３の阻害および多発性骨髄腫の治療 |
| JP2010258402A Withdrawn JP2011042687A (ja) | 2003-11-07 | 2010-11-18 | キノリノン化合物を合成する方法 |
| JP2011118515A Expired - Fee Related JP5214768B2 (ja) | 2003-11-07 | 2011-05-26 | 改良された薬物特性を有するキノリノン化合物の薬学的に受容可能な塩 |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006538526A Expired - Fee Related JP4724665B2 (ja) | 2003-11-07 | 2004-11-05 | キノリノン化合物を合成する方法 |
| JP2006538509A Expired - Fee Related JP4890255B2 (ja) | 2003-11-07 | 2004-11-05 | 改良された薬物特性を有するキノリノン化合物の薬学的に受容可能な塩 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010258402A Withdrawn JP2011042687A (ja) | 2003-11-07 | 2010-11-18 | キノリノン化合物を合成する方法 |
| JP2011118515A Expired - Fee Related JP5214768B2 (ja) | 2003-11-07 | 2011-05-26 | 改良された薬物特性を有するキノリノン化合物の薬学的に受容可能な塩 |
Country Status (14)
| Country | Link |
|---|---|
| US (7) | US20050209247A1 (https=) |
| EP (4) | EP2762475A1 (https=) |
| JP (5) | JP4724665B2 (https=) |
| KR (3) | KR20060111520A (https=) |
| CN (1) | CN102225926A (https=) |
| AU (3) | AU2004289672C1 (https=) |
| BR (1) | BRPI0416143A (https=) |
| CA (3) | CA2544492C (https=) |
| EA (1) | EA012621B1 (https=) |
| ES (1) | ES2486240T3 (https=) |
| IL (5) | IL174471A (https=) |
| MX (1) | MXPA06004194A (https=) |
| TW (1) | TWI347940B (https=) |
| WO (3) | WO2005046589A2 (https=) |
Families Citing this family (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE448226T1 (de) | 2000-09-01 | 2009-11-15 | Novartis Vaccines & Diagnostic | Aza heterocyclische derivate und ihre therapeutische verwendung |
| DE60115069T2 (de) | 2000-09-11 | 2006-08-03 | Chiron Corp., Emeryville | Chinolinonderivate als tyrosin-kinase inhibitoren |
| US20030028018A1 (en) * | 2000-09-11 | 2003-02-06 | Chiron Coporation | Quinolinone derivatives |
| EP1539754A4 (en) | 2002-08-23 | 2009-02-25 | Novartis Vaccines & Diagnostic | BENZIMIDAZOCHINOLINONE AND ITS USE |
| US7825132B2 (en) * | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| SG148864A1 (en) * | 2002-11-13 | 2009-01-29 | Chiron Corp | Methods of treating cancer and related methods |
| US20050209247A1 (en) * | 2003-11-07 | 2005-09-22 | Chiron Corporation | Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties |
| EP1718306A2 (en) * | 2004-02-20 | 2006-11-08 | Chiron Corporation | Modulation of inflammatory and metastatic processes |
| EP2301546B1 (en) * | 2005-01-27 | 2014-09-10 | Novartis AG | Treatment of metastasized tumors |
| US8034823B2 (en) * | 2005-02-22 | 2011-10-11 | Savvipharm Inc | Method of increasing drug oral bioavailability and compositions of less toxic orotate salts |
| ES2732251T3 (es) * | 2005-04-25 | 2019-11-21 | Enterin Inc | Dilactato de escualamina cristalino |
| EP1885187B1 (en) * | 2005-05-13 | 2013-09-25 | Novartis AG | Methods for treating drug resistant cancer |
| EP2465857B1 (en) * | 2005-05-17 | 2014-06-04 | Novartis AG | Methods for synthesizing heterocyclic compounds |
| AU2012258324B2 (en) * | 2005-05-17 | 2014-07-24 | Novartis Ag | Methods for synthesizing heterocyclic compounds |
| BRPI0611375A2 (pt) * | 2005-05-23 | 2010-08-31 | Novartis Ag | formas cristalinas e outras de sais de ácido láctico de 4-amino-5-flúor-3-[6-(4-metilpiperazin-1-il)-1h-benzimid azol-2-il]-1h-quinolin-2-ona |
| US20080207572A1 (en) * | 2005-07-14 | 2008-08-28 | Ab Science | Use of Dual C-Kit/Fgfr3 Inhibitors for Treating Multiple Myeloma |
| CN101316593B (zh) * | 2005-11-29 | 2012-05-02 | 诺瓦提斯公司 | 喹啉酮类的制剂 |
| NZ567550A (en) * | 2005-11-29 | 2011-08-26 | Novartis Ag | Formulations of lactic acid salts of 4-amino-5-fluoro-3-[6-(4-methyl-piperazin-1-yl)-1 H-benzimidazol-2-yl]1H-quinolin-2-one |
| KR20080080525A (ko) | 2005-12-08 | 2008-09-04 | 노파르티스 아게 | 유전자 전사에 대한 ｆｇｆｒ３의 억제제의 효과 |
| CN100488960C (zh) * | 2006-03-09 | 2009-05-20 | 中国药科大学 | 2-位取代的喹诺酮类化合物及其在制药中的应用 |
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| CA2679268A1 (en) * | 2007-03-09 | 2008-09-18 | Novartis Ag | Treatment of melanoma |
| EP2170859A1 (en) | 2007-06-25 | 2010-04-07 | F. Hoffmann-Roche AG | Benzimidazole amido derivatives as kinase inhibitors |
| GB0800855D0 (en) | 2008-01-17 | 2008-02-27 | Syngenta Ltd | Herbicidal compounds |
| JPWO2009113436A1 (ja) * | 2008-03-14 | 2011-07-21 | 国立大学法人 千葉大学 | Ｆｇｆｒ３遺伝子阻害剤の放射線照射併用による放射線の抗癌作用増強法および副作用軽減法 |
| PE20091628A1 (es) * | 2008-03-19 | 2009-11-19 | Novartis Ag | Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona |
| JP2012509321A (ja) * | 2008-11-21 | 2012-04-19 | ミレニアム ファーマシューティカルズ， インコーポレイテッド | 癌および他の疾患または障害の処置のための、４−［６−メトキシ−７−（３−ピペリジン−１−イル−プロポキシ）キナゾリン−４−イル］ピペラジン−１−カルボン酸（４−イソプロポキシフェニル）−アミドの乳酸塩およびその薬学的組成物 |
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| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
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2004
- 2004-11-05 US US10/982,543 patent/US20050209247A1/en not_active Abandoned
- 2004-11-05 WO PCT/US2004/036941 patent/WO2005046589A2/en not_active Ceased
- 2004-11-05 MX MXPA06004194A patent/MXPA06004194A/es active IP Right Grant
- 2004-11-05 CA CA2544492A patent/CA2544492C/en not_active Expired - Fee Related
- 2004-11-05 KR KR1020067009999A patent/KR20060111520A/ko not_active Abandoned
- 2004-11-05 EP EP14165975.5A patent/EP2762475A1/en not_active Withdrawn
- 2004-11-05 AU AU2004289672A patent/AU2004289672C1/en not_active Ceased
- 2004-11-05 EP EP04816941.1A patent/EP1699421B1/en not_active Expired - Lifetime
- 2004-11-05 KR KR1020067011003A patent/KR101167573B1/ko not_active Expired - Fee Related
- 2004-11-05 EA EA200600928A patent/EA012621B1/ru not_active IP Right Cessation
- 2004-11-05 CN CN2011100963250A patent/CN102225926A/zh active Pending
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- 2004-11-05 WO PCT/US2004/037051 patent/WO2005046590A2/en not_active Ceased
- 2004-11-05 EP EP04810468A patent/EP1682529A4/en not_active Withdrawn
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- 2004-11-05 JP JP2006538512A patent/JP4823914B2/ja not_active Expired - Fee Related
- 2004-11-05 US US10/982,757 patent/US20050137399A1/en not_active Abandoned
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- 2004-11-05 ES ES04816941.1T patent/ES2486240T3/es not_active Expired - Lifetime
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- 2006-04-04 IL IL174767A patent/IL174767A0/en unknown
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