JP2007522098A5 - - Google Patents
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- JP2007522098A5 JP2007522098A5 JP2006538509A JP2006538509A JP2007522098A5 JP 2007522098 A5 JP2007522098 A5 JP 2007522098A5 JP 2006538509 A JP2006538509 A JP 2006538509A JP 2006538509 A JP2006538509 A JP 2006538509A JP 2007522098 A5 JP2007522098 A5 JP 2007522098A5
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- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- groups
- group
- alkyl
- 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 63
- 125000003118 aryl group Chemical group 0.000 claims 58
- 125000000623 heterocyclic group Chemical group 0.000 claims 50
- 150000003893 lactate salts Chemical class 0.000 claims 27
- 125000004103 aminoalkyl group Chemical group 0.000 claims 23
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 18
- 239000000203 mixture Substances 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 13
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 12
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims 12
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 10
- 125000005128 aryl amino alkyl group Chemical group 0.000 claims 9
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 9
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 8
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- -1 guanidinyl groups Chemical group 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 239000002904 solvent Substances 0.000 claims 6
- 125000003277 amino group Chemical group 0.000 claims 5
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 125000004663 dialkyl amino group Chemical group 0.000 claims 3
- 235000014655 lactic acid Nutrition 0.000 claims 3
- 239000004310 lactic acid Substances 0.000 claims 3
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000001769 aryl amino group Chemical group 0.000 claims 2
- 238000001816 cooling Methods 0.000 claims 2
- 125000004986 diarylamino group Chemical group 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical compound C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003418 alkyl amino alkoxy group Chemical group 0.000 claims 1
- 125000002431 aminoalkoxy group Chemical group 0.000 claims 1
- PIQCTGMSNWUMAF-UHFFFAOYSA-N chembl522892 Chemical compound C1CN(C)CCN1C1=CC=C(NC(=N2)C=3C(NC4=CC=CC(F)=C4C=3N)=O)C2=C1 PIQCTGMSNWUMAF-UHFFFAOYSA-N 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 125000004984 dialkylaminoalkoxy group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000005429 oxyalkyl group Chemical group 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 239000003586 protic polar solvent Substances 0.000 claims 1
- 125000005017 substituted alkenyl group Chemical group 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/US2004/036941 WO2005046589A2 (en) | 2003-11-07 | 2004-11-05 | Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011118515A Division 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007522098A JP2007522098A (ja) | 2007-08-09 |
| JP2007522098A5 true JP2007522098A5 (https=) | 2007-12-06 |
| JP4890255B2 JP4890255B2 (ja) | 2012-03-07 |
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 (1)
| 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 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
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 |
| WO2008044041A1 (en) | 2006-10-12 | 2008-04-17 | Astex Therapeutics Limited | Pharmaceutical combinations |
| EP2073807A1 (en) | 2006-10-12 | 2009-07-01 | Astex Therapeutics Limited | Pharmaceutical combinations |
| 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 |
| WO2010075443A1 (en) * | 2008-12-22 | 2010-07-01 | Burnham Institute For Medical Research | Selective inhibitors of akt and methods of using same |
| NZ779754A (en) | 2009-01-16 | 2023-04-28 | Exelixis Inc | Malate salt of n-(4-{ [6,7-bis(methyloxy)quinolin-4-yl] oxy} phenyl)-n’-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| MX2012011090A (es) | 2010-03-26 | 2012-10-10 | Novartis Ag | Preparacion de polimorfos hidratados de sal de acido lactico de la 4-amino-5-fluoro-3-[6-(4-metil-piperazin-1-il)-1h-bencimidazol- 2-il]-1h-quinolin-2-ona. |
| CN102834094B (zh) * | 2010-04-16 | 2015-05-06 | 诺华有限公司 | 有机化合物的组合产品及其制药用途 |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| EA030435B1 (ru) * | 2010-07-16 | 2018-08-31 | Экселиксис, Инк. | ТАБЛЕТКА, СОДЕРЖАЩАЯ МОДУЛЯТОР c-MET В ФОРМЕ КРИСТАЛЛИЧЕСКОЙ L-МАЛАТНОЙ СОЛИ (ВАРИАНТЫ), СПОСОБ ЕЕ ПРОИЗВОДСТВА И СПОСОБ ЛЕЧЕНИЯ ОНКОЛОГИЧЕСКОГО ЗАБОЛЕВАНИЯ С ЕЕ ИСПОЛЬЗОВАНИЕМ |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| BR112013020362A2 (pt) | 2011-02-10 | 2018-05-29 | Exelixis Inc | processos para a preparação de compostos de quinolina, compostos e combinações farmacêuticas que os contem |
| EP2524915A1 (en) * | 2011-05-20 | 2012-11-21 | Sanofi | 2-Amino-3-(imidazol-2-yl)-pyridin-4-one derivatives and their use as VEGF receptor kinase inhibitors |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) * | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| WO2013063003A1 (en) | 2011-10-28 | 2013-05-02 | Novartis Ag | Method of treating gastrointestinal stromal tumors |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| WO2013088191A1 (en) | 2011-12-12 | 2013-06-20 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Antagonist of the fibroblast growth factor receptor 3 (fgfr3) for use in the treatment or the prevention of skeletal disorders linked with abnormal activation of fgfr3 |
| EP2809312A1 (en) | 2012-01-31 | 2014-12-10 | Novartis AG | Combination of a rtk inhibitor with an anti - estrogen and use thereof for the treatment of cancer |
| PL2824181T3 (pl) | 2012-03-08 | 2019-02-28 | Astellas Pharma Inc. | Nowa fuzja fgfr3 |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| IN2014DN10801A (https=) | 2012-07-11 | 2015-09-04 | Novartis Ag | |
| PT2874625T (pt) * | 2012-07-17 | 2017-08-16 | Sanofi Sa | Uso de inibidores vegfr-3 para tratar carcinoma hepatocelular |
| TWI606066B (zh) * | 2012-09-27 | 2017-11-21 | 中外製藥股份有限公司 | FGFR3 Fusion Gene and Its Targeted Medicine |
| WO2014058785A1 (en) | 2012-10-10 | 2014-04-17 | Novartis Ag | Combination therapy |
| CN103804305A (zh) * | 2012-11-05 | 2014-05-21 | 韩文毅 | 一类治疗湿疹的化合物及其用途 |
| ES2675720T3 (es) | 2013-01-10 | 2018-07-12 | Pulmokine, Inc. | Inhibidores de quinasa no selectivos |
| WO2014120995A2 (en) | 2013-02-01 | 2014-08-07 | Wellstat Therapeutics Corporation | Amine compounds having anti-inflammatory, antifungal, antiparasitic and anticancer activity |
| EP2956138B1 (en) | 2013-02-15 | 2022-06-22 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| MX368903B (es) | 2013-02-20 | 2019-10-21 | Kala Pharmaceuticals Inc | Compuestos terapéuticos y sus usos en el tratamiento de enfermedades proliferativas. |
| US9688688B2 (en) | 2013-02-20 | 2017-06-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| US9925184B2 (en) | 2013-10-11 | 2018-03-27 | Pulmokine, Inc. | Spray-dry formulations |
| ES2670550T3 (es) | 2013-10-14 | 2018-05-30 | Eisai R&D Management Co., Ltd. | Derivados de quinolina selectivamente sustituidos |
| SG10202103278TA (en) | 2013-10-14 | 2021-04-29 | Eisai R&D Man Co Ltd | Selectively substituted quinoline compounds |
| US9458169B2 (en) | 2013-11-01 | 2016-10-04 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| TWI541022B (zh) * | 2013-12-18 | 2016-07-11 | 應克隆公司 | 針對纖維母細胞生長因子受體－３（ｆｇｆｒ３）之化合物及治療方法 |
| RU2715236C2 (ru) | 2014-03-26 | 2020-02-26 | Астекс Терапьютикс Лтд | Комбинации |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| HRP20210319T1 (hr) | 2014-03-26 | 2021-04-30 | Astex Therapeutics Ltd. | Kombinacije inhibitora fgfr i inhibitora igf1r |
| EP2977374A1 (en) | 2014-07-21 | 2016-01-27 | Université de Strasbourg | Molecules presenting dual emission properties |
| JP6759514B2 (ja) | 2014-08-01 | 2020-09-23 | ヌエヴォリューション・アクティーゼルスカブＮｕｅｖｏｌｕｔｉｏｎ Ａ／Ｓ | ブロモドメインに対して活性な化合物 |
| TWI719960B (zh) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
| EP3265462A1 (en) | 2015-03-03 | 2018-01-10 | INSERM - Institut National de la Santé et de la Recherche Médicale | Fgfr3 antagonists |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| GB201506660D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| EP3353164B1 (en) | 2015-09-23 | 2021-11-03 | Janssen Pharmaceutica, N.V. | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| US11155555B2 (en) | 2015-09-23 | 2021-10-26 | Janssen Pharmaceutica Nv | Compounds |
| US10689398B2 (en) * | 2015-10-23 | 2020-06-23 | Esteve Pharmaceuticals, S.A. | OXA-Diazaspiro compounds having activity against pain |
| ES2877799T3 (es) * | 2015-12-31 | 2021-11-17 | Shanghai Pharmaceuticals Holding Co Ltd | Sal de derivado de quinolina, formas polimórficas de la misma, métodos de preparación de la misma, composición y aplicaciones |
| MX382436B (es) * | 2016-01-11 | 2025-03-13 | Merck Patent Gmbh | Derivados de quinolin-2-ona. |
| TWI590475B (zh) * | 2016-06-17 | 2017-07-01 | 財團法人工業技術研究院 | 堆疊型太陽能電池模組 |
| US10336767B2 (en) | 2016-09-08 | 2019-07-02 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| EP3509423A4 (en) | 2016-09-08 | 2020-05-13 | Kala Pharmaceuticals, Inc. | CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF |
| AU2017324713B2 (en) | 2016-09-08 | 2020-08-13 | KALA BIO, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| CN107935858B (zh) * | 2016-10-12 | 2020-09-08 | 利尔化学股份有限公司 | 5-氟-2-硝基苯酚的制备方法 |
| CA3041679A1 (en) | 2016-10-27 | 2018-05-03 | Lawrence S. ZISMAN | Combination therapy for treating pulmonary hypertension |
| AU2018291687B2 (en) * | 2017-06-27 | 2022-07-14 | Janssen Pharmaceutica Nv | New quinolinone compounds |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| AU2018370904B2 (en) | 2017-11-24 | 2023-09-21 | Janssen Pharmaceutica Nv | Pyrazolopyridinone compounds |
| KR102763767B1 (ko) | 2017-11-24 | 2025-02-05 | 얀센 파마슈티카 엔브이 | 피라졸로피리디논 화합물 |
| CN112638881B (zh) | 2018-07-31 | 2025-01-07 | 普林斯顿大学托管委员会 | 用于治疗转移性和化疗耐受性癌症的四氢喹啉衍生物 |
| WO2020135483A1 (en) * | 2018-12-26 | 2020-07-02 | Janssen Pharmaceutica Nv | Thienopyridinone compounds |
| CA3163875A1 (en) * | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| IL324964A (en) | 2021-04-22 | 2026-01-01 | Kayothera Inc | Modified heterocycles as aldehyde dehydrogenase inhibitors |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US20250144110A1 (en) * | 2022-01-28 | 2025-05-08 | Washington University | Compositions of autophagy modulating agents and uses thereof |
Family Cites Families (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3663606A (en) * | 1966-06-21 | 1972-05-16 | Mitsui Toatsu Chemicals | Organic imino-compounds |
| DE2363459A1 (de) | 1973-12-20 | 1975-06-26 | Basf Ag | Neue fluoreszierende chinolinverbindungen |
| US4287341A (en) | 1979-11-01 | 1981-09-01 | Pfizer Inc. | Alkoxy-substituted-6-chloro-quinazoline-2,4-diones |
| US4659657A (en) * | 1982-12-24 | 1987-04-21 | Bayer Aktiengesellschaft | Chromogenic and fluorogenic esters for photometric or fluorimetric determination of phosphatases or sulphatases |
| DE3634066A1 (de) * | 1986-10-07 | 1988-04-21 | Boehringer Mannheim Gmbh | Neue 5-alkylbenzimidazole, verfahren zu ihrer herstellung sowie arzneimittel |
| US5073492A (en) * | 1987-01-09 | 1991-12-17 | The Johns Hopkins University | Synergistic composition for endothelial cell growth |
| JPH0699497B2 (ja) | 1987-04-16 | 1994-12-07 | 富士写真フイルム株式会社 | 光重合性組成物 |
| DE3932953A1 (de) * | 1989-10-03 | 1991-04-11 | Boehringer Mannheim Gmbh | Neue 2-bicyclo-benzimidazole, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
| US5151360A (en) * | 1990-12-31 | 1992-09-29 | Biomembrane Institute | Effect of n,n,n-trimethylsphingosine on protein kinase-c activity, melanoma cell growth in vitro, metastatic potential in vivo and human platelet aggregation |
| GB9108547D0 (en) | 1991-04-22 | 1991-06-05 | Fujisawa Pharmaceutical Co | Quinoline derivatives |
| USRE37650E1 (en) * | 1991-05-10 | 2002-04-09 | Aventis Pharmacetical Products, Inc. | Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase |
| US5480883A (en) * | 1991-05-10 | 1996-01-02 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| US5710158A (en) * | 1991-05-10 | 1998-01-20 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| US5856115A (en) * | 1991-05-24 | 1999-01-05 | Fred Hutchinson Cancer Research Center | Assay for identification therapeutic agents |
| PT627940E (pt) * | 1992-03-05 | 2003-07-31 | Univ Texas | Utilizacao de imunoconjugados para o diagnostico e/ou terapia de tumores vascularizados |
| JP3142378B2 (ja) | 1992-06-22 | 2001-03-07 | ティーディーケイ株式会社 | 有機ｅｌ素子 |
| US5330992A (en) * | 1992-10-23 | 1994-07-19 | Sterling Winthrop Inc. | 1-cyclopropyl-4-pyridyl-quinolinones |
| US5763441A (en) | 1992-11-13 | 1998-06-09 | Sugen, Inc. | Compounds for the treatment of disorders related to vasculogenesis and/or angiogenesis |
| US5981569A (en) * | 1992-11-13 | 1999-11-09 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Substituted phenylacrylonitrile compounds and compositions thereof for the treatment of disease |
| US5792771A (en) * | 1992-11-13 | 1998-08-11 | Sugen, Inc. | Quinazoline compounds and compositions thereof for the treatment of disease |
| JPH0743896A (ja) | 1993-07-28 | 1995-02-14 | Toyobo Co Ltd | 光重合性組成物 |
| US5716993A (en) | 1993-12-27 | 1998-02-10 | Eisai Co., Ltd. | Anthranilic acid derivatives |
| JPH0829973A (ja) | 1994-07-11 | 1996-02-02 | Toyobo Co Ltd | 光重合性組成物 |
| JP3441246B2 (ja) * | 1995-06-07 | 2003-08-25 | 富士写真フイルム株式会社 | 光重合性組成物 |
| GB9624482D0 (en) * | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| US6010711A (en) * | 1996-01-26 | 2000-01-04 | University Of Rochester | Methods, articles and compositions for the pharmacologic inhibition of bone resorption with phosphodiesterase inhibitors |
| AU2103097A (en) | 1996-03-15 | 1997-10-10 | Zeneca Limited | Cinnoline derivatives and use as medicine |
| DE19610723A1 (de) | 1996-03-19 | 1997-09-25 | Bayer Ag | Elektrolumineszierende Anordnungen unter Verwendung von Blendsystemen |
| US5942385A (en) * | 1996-03-21 | 1999-08-24 | Sugen, Inc. | Method for molecular diagnosis of tumor angiogenesis and metastasis |
| JP4373497B2 (ja) * | 1996-06-19 | 2009-11-25 | ローン−プーラン・ロレ・リミテツド | 置換されたアザビシクロ化合物、ならびにｔｎｆおよびサイクリックａｍｐホスホジエステラーゼ産生の阻害剤としてのそれらの使用 |
| WO1997048694A1 (en) | 1996-06-20 | 1997-12-24 | Board Of Regents, The University Of Texas System | Compounds and methods for providing pharmacologically active preparations and uses thereof |
| WO1998013350A1 (en) | 1996-09-25 | 1998-04-02 | Zeneca Limited | Qinoline derivatives inhibiting the effect of growth factors such as vegf |
| US6111110A (en) * | 1996-10-30 | 2000-08-29 | Eli Lilly And Company | Synthesis of benzo[f]quinolinones |
| WO2001052904A2 (en) | 2000-01-19 | 2001-07-26 | Gill Parkash S | Pharmaceutical compositions and methods of treatment based on vegf antisense oligonucleotides |
| GB9716557D0 (en) * | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| ES2289791T3 (es) | 1997-08-22 | 2008-02-01 | Astrazeneca Ab | Derivados de oxindolilquinazolina como inhibidores de la angiogenesis. |
| DE19756235A1 (de) * | 1997-12-17 | 1999-07-01 | Klinge Co Chem Pharm Fab | Neue piperidinylsubstituierte Pyridylalkan- alken- und -alkincarbonsäureamide |
| CA2328893A1 (en) | 1998-05-20 | 1999-11-25 | Kyowa Hakko Kogyo Co., Ltd. | Vegf activity inhibitors |
| US6174912B1 (en) * | 1998-08-21 | 2001-01-16 | Dupont Pharmaceuticals Company | Nitrogen substituted imidazo[4,5-C]pyrazoles as corticotropin releasing hormone antagonists |
| DE19841985A1 (de) | 1998-09-03 | 2000-03-09 | Schering Ag | Dialkylsulfonsäure- und Dialkylcarbonsäure-Derivate |
| IL126953A0 (en) | 1998-11-08 | 1999-09-22 | Yeda Res & Dev | Pharmaceutical compositions comprising porphyrins and some novel porphyrin derivatives |
| US20030087854A1 (en) * | 2001-09-10 | 2003-05-08 | Isis Pharmaceuticals Inc. | Antisense modulation of fibroblast growth factor receptor 3 expression |
| PT1133474E (pt) * | 1998-12-04 | 2007-04-30 | Bristol Myers Squibb Co | Derivados da 4-arilquinolin-2-ona substituidos em 3 posições utilizados como moduladores do canal de potássio. |
| PE20010306A1 (es) | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
| KR100298572B1 (ko) * | 1999-08-19 | 2001-09-22 | 박찬구 | 카바아닐라이드로부터 4-니트로디페닐아민과 4-니트로소디페닐아민의 제조방법 |
| CA2387351C (en) * | 1999-10-19 | 2009-09-08 | Merck & Co., Inc. | Indole derivatives as tyrosine kinase inhibitors |
| AU778042B2 (en) * | 1999-10-19 | 2004-11-11 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| YU54202A (sh) | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije |
| WO2001052875A1 (en) | 2000-01-18 | 2001-07-26 | Ludwig Institute For Cancer Research | Vegf-d/vegf-c/vegf peptidomimetic inhibitor |
| GB0001930D0 (en) | 2000-01-27 | 2000-03-22 | Novartis Ag | Organic compounds |
| JP3663382B2 (ja) | 2000-02-15 | 2005-06-22 | スージェン・インコーポレーテッド | ピロール置換２−インドリノン蛋白質キナーゼ阻害剤 |
| EP1259236A4 (en) | 2000-02-25 | 2004-11-03 | Merck & Co Inc | Tyrosine kinase inhibitors |
| US6420382B2 (en) | 2000-02-25 | 2002-07-16 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| US6313138B1 (en) * | 2000-02-25 | 2001-11-06 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| PL202918B1 (pl) * | 2000-03-07 | 2009-08-31 | Rush Presbyterian St Luke | Przeciwbakteryjna i antykoncepcyjna kompozycja oraz jej zastosowanie |
| US6257320B1 (en) * | 2000-03-28 | 2001-07-10 | Alec Wargo | Heat sink device for power semiconductors |
| ATE448226T1 (de) * | 2000-09-01 | 2009-11-15 | Novartis Vaccines & Diagnostic | Aza heterocyclische derivate und ihre therapeutische verwendung |
| WO2002020500A2 (en) * | 2000-09-01 | 2002-03-14 | Icos Corporation | Materials and methods to potentiate cancer treatment |
| US20030028018A1 (en) * | 2000-09-11 | 2003-02-06 | Chiron Coporation | Quinolinone derivatives |
| DE60115069T2 (de) * | 2000-09-11 | 2006-08-03 | Chiron Corp., Emeryville | Chinolinonderivate als tyrosin-kinase inhibitoren |
| EP1188751A1 (en) * | 2000-09-13 | 2002-03-20 | Casale Chemicals SA | Process for the production of high purity melamine from urea |
| US7064215B2 (en) * | 2001-07-03 | 2006-06-20 | Chiron Corporation | Indazole benzimidazole compounds |
| EP1447405A4 (en) * | 2001-10-17 | 2005-01-12 | Kirin Brewery | CHINOLIN OR CHINAZOLINE DERIVATIVES THAT PREVENT THE AUTOPHOSPHORYLATION OF RECEPTORS FOR THE FIBROBLAST GROWTH FACTOR |
| US6476068B1 (en) * | 2001-12-06 | 2002-11-05 | Pharmacia Italia, S.P.A. | Platinum derivative pharmaceutical formulations |
| US20030159702A1 (en) * | 2002-01-21 | 2003-08-28 | Lindell Katarina E.A. | Formulation and use manufacture thereof |
| US6822097B1 (en) * | 2002-02-07 | 2004-11-23 | Amgen, Inc. | Compounds and methods of uses |
| US7825132B2 (en) * | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| US20050256157A1 (en) * | 2002-08-23 | 2005-11-17 | Chiron Corporation | Combination therapy with CHK1 inhibitors |
| EP1539754A4 (en) * | 2002-08-23 | 2009-02-25 | Novartis Vaccines & Diagnostic | BENZIMIDAZOCHINOLINONE AND ITS USE |
| AU2003275282A1 (en) * | 2002-09-30 | 2004-04-23 | Bristol-Myers Squibb Company | Novel tyrosine kinase inhibitors |
| SG148864A1 (en) * | 2002-11-13 | 2009-01-29 | Chiron Corp | Methods of treating cancer and related methods |
| US6774327B1 (en) * | 2003-09-24 | 2004-08-10 | Agilent Technologies, Inc. | Hermetic seals for electronic components |
| EP2060270A3 (en) * | 2003-10-16 | 2009-12-09 | Imclone LLC | Fibroblast growth factor receptor-1 inhibitors and methods of treatment thereof |
| 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 |
| BRPI0613200A2 (pt) * | 2005-05-18 | 2012-01-03 | M & G Polimeri Italia Spa | composiÇço de poliÉster |
-
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
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- 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 BR BRPI0416143-2A patent/BRPI0416143A/pt not_active IP Right Cessation
- 2004-11-05 WO PCT/US2004/037051 patent/WO2005046590A2/en not_active Ceased
- 2004-11-05 EP EP04810468A patent/EP1682529A4/en not_active Withdrawn
- 2004-11-05 JP JP2006538509A patent/JP4890255B2/ja not_active Expired - Fee Related
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- 2004-11-05 KR KR1020067007021A patent/KR101224410B1/ko not_active Expired - Fee Related
- 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
- 2004-11-05 CA CA002544186A patent/CA2544186A1/en not_active Abandoned
- 2004-11-05 ES ES04816941.1T patent/ES2486240T3/es not_active Expired - Lifetime
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- 2006-03-22 IL IL174471A patent/IL174471A/en not_active IP Right Cessation
- 2006-04-04 IL IL174767A patent/IL174767A0/en unknown
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2009
- 2009-03-04 US US12/398,130 patent/US20090181979A1/en not_active Abandoned
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