JP2013523614A5 - - Google Patents
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- Publication number
- JP2013523614A5 JP2013523614A5 JP2013500523A JP2013500523A JP2013523614A5 JP 2013523614 A5 JP2013523614 A5 JP 2013523614A5 JP 2013500523 A JP2013500523 A JP 2013500523A JP 2013500523 A JP2013500523 A JP 2013500523A JP 2013523614 A5 JP2013523614 A5 JP 2013523614A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- propyl
- hydrogen
- methyl
- iso
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 9
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 6
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 239000013543 active substance Substances 0.000 claims 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 239000000825 pharmaceutical preparation Substances 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical group CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 claims 1
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000000824 cytostatic agent Substances 0.000 claims 1
- 230000001085 cytostatic effect Effects 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 230000001472 cytotoxic effect Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000005343 heterocyclic alkyl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- -1 n- propyl Chemical group 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 0 *c(c(N1NNC(c2cc(N(*)*)cnc2)=C1)c1)ccc1[I+]* Chemical compound *c(c(N1NNC(c2cc(N(*)*)cnc2)=C1)c1)ccc1[I+]* 0.000 description 18
- YJIWDDCFWRWGHB-UHFFFAOYSA-N CC(C)c1nc(I)c(C)[o]1 Chemical compound CC(C)c1nc(I)c(C)[o]1 YJIWDDCFWRWGHB-UHFFFAOYSA-N 0.000 description 2
- CUEBVIQLPLQDJA-UHFFFAOYSA-O CC(C)/C(/[OH2+])=N/C(I)=N Chemical compound CC(C)/C(/[OH2+])=N/C(I)=N CUEBVIQLPLQDJA-UHFFFAOYSA-O 0.000 description 1
- CQRJGLBVCJVUAX-UHFFFAOYSA-O CC(C)/C(/[SH2+])=N/C(I)=N Chemical compound CC(C)/C(/[SH2+])=N/C(I)=N CQRJGLBVCJVUAX-UHFFFAOYSA-O 0.000 description 1
- SGLUBESBBHQIBA-MIEAWXDDSA-O CC(C)C(/C=C(\O)/I)=[NH2+] Chemical compound CC(C)C(/C=C(\O)/I)=[NH2+] SGLUBESBBHQIBA-MIEAWXDDSA-O 0.000 description 1
- KLXZRGNTQDXKRY-UHFFFAOYSA-O CC(C)C([NH2+]C)=CC(I)=N Chemical compound CC(C)C([NH2+]C)=CC(I)=N KLXZRGNTQDXKRY-UHFFFAOYSA-O 0.000 description 1
- POKUIYOPHXEYIK-UHFFFAOYSA-N CC(C)c1cc(I)n[n]1C Chemical compound CC(C)c1cc(I)n[n]1C POKUIYOPHXEYIK-UHFFFAOYSA-N 0.000 description 1
- NRTMMWAJFDAYKU-UHFFFAOYSA-N CC(C)c1n[o]c(I)c1 Chemical compound CC(C)c1n[o]c(I)c1 NRTMMWAJFDAYKU-UHFFFAOYSA-N 0.000 description 1
- UDHYCPAIJAAQJT-UHFFFAOYSA-N CC(C)c1nc(I)c(C)[s]1 Chemical compound CC(C)c1nc(I)c(C)[s]1 UDHYCPAIJAAQJT-UHFFFAOYSA-N 0.000 description 1
- WMJOIVQLVJFVFJ-UHFFFAOYSA-N CC(C)c1nccc(C(C)(C)C)c1 Chemical compound CC(C)c1nccc(C(C)(C)C)c1 WMJOIVQLVJFVFJ-UHFFFAOYSA-N 0.000 description 1
- IHPQEILBIOUFAC-UHFFFAOYSA-N CC(C)c1nccc(C(F)(F)F)c1 Chemical compound CC(C)c1nccc(C(F)(F)F)c1 IHPQEILBIOUFAC-UHFFFAOYSA-N 0.000 description 1
- RUBGAEMGCQLQFH-UHFFFAOYSA-N Ic1n[o]cn1 Chemical compound Ic1n[o]cn1 RUBGAEMGCQLQFH-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10158041.3 | 2010-03-26 | ||
| EP10158041 | 2010-03-26 | ||
| PCT/EP2011/054611 WO2011117381A1 (en) | 2010-03-26 | 2011-03-25 | B-raf kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013523614A JP2013523614A (ja) | 2013-06-17 |
| JP2013523614A5 true JP2013523614A5 (enExample) | 2014-05-15 |
| JP5871896B2 JP5871896B2 (ja) | 2016-03-01 |
Family
ID=42244071
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013500523A Active JP5871896B2 (ja) | 2010-03-26 | 2011-03-25 | Ｂ−ｒａｆキナーゼインヒビター |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9290507B2 (enExample) |
| EP (1) | EP2552905B1 (enExample) |
| JP (1) | JP5871896B2 (enExample) |
| WO (1) | WO2011117381A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0712795A2 (pt) | 2006-07-07 | 2012-09-04 | Boehringer Ingelheim Int | derivados de heteroarila substituìdos com fenila e uso dos mesmos como agentes antitumorais |
| PE20090837A1 (es) * | 2007-07-02 | 2009-07-24 | Boehringer Ingelheim Int | Nuevos compuestos quimicos |
| TW201014860A (en) | 2008-09-08 | 2010-04-16 | Boehringer Ingelheim Int | New chemical compounds |
| EA201100564A1 (ru) | 2008-09-29 | 2011-12-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Антипролиферативные соединения |
| US8569316B2 (en) | 2009-02-17 | 2013-10-29 | Boehringer Ingelheim International Gmbh | Pyrimido [5,4-D] pyrimidine derivatives for the inhibition of tyrosine kinases |
| JP5871896B2 (ja) | 2010-03-26 | 2016-03-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｂ−ｒａｆキナーゼインヒビター |
| WO2011117382A1 (en) | 2010-03-26 | 2011-09-29 | Boehringer Ingelheim International Gmbh | Pyridyltriazoles |
| US8546443B2 (en) | 2010-12-21 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Benzylic oxindole pyrimidines |
| US8710055B2 (en) | 2010-12-21 | 2014-04-29 | Boehringer Ingelheim International Gmbh | Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| US8889684B2 (en) | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| US9408885B2 (en) | 2011-12-01 | 2016-08-09 | Vib Vzw | Combinations of therapeutic agents for treating melanoma |
| JO3407B1 (ar) | 2012-05-31 | 2019-10-20 | Eisai R&D Man Co Ltd | مركبات رباعي هيدرو بيرازولو بيريميدين |
| MX363708B (es) | 2013-10-14 | 2019-03-29 | Eisai R&D Man Co Ltd | Compuestos de quinolina selectivamente sustituidos. |
| SG10201704327RA (en) | 2013-10-14 | 2017-06-29 | Eisai R&D Man Co Ltd | Selectively substituted quinoline compounds |
| WO2015171833A1 (en) * | 2014-05-06 | 2015-11-12 | The Regents Of The University Of California | Wound healing using braf inhibitors |
| WO2017100593A1 (en) | 2015-12-09 | 2017-06-15 | Luc Therapeutics | Thienopyrimidinone nmda receptor modulators and uses thereof |
| DK3386591T3 (da) | 2015-12-09 | 2020-09-28 | Cadent Therapeutics Inc | Heteroaromatic nmda receptor modulators and uses thereof |
| US11274107B2 (en) | 2016-12-22 | 2022-03-15 | Cadent Therapeutics, Inc. | NMDA receptor modulators and uses thereof |
| EP3579872A1 (en) | 2017-02-10 | 2019-12-18 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway |
| CA3086765A1 (en) | 2017-12-28 | 2019-07-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
| HUE062566T2 (hu) | 2018-08-03 | 2023-11-28 | Novartis Ag | Heteroaromás NMDA receptor modulátorok és alkalmazásaik |
| RS64618B1 (sr) * | 2019-02-12 | 2023-10-31 | Lutris Pharma Ltd | Upotreba lokalnih kompozicija braf inhibitorа za lečenje radijacijskog dermatitisa |
| CN111606887B (zh) | 2019-02-26 | 2023-03-17 | 安徽中科拓苒药物科学研究有限公司 | 一种新型激酶抑制剂 |
| WO2021035788A1 (zh) * | 2019-08-29 | 2021-03-04 | 中国科学院合肥物质科学研究院 | 吡唑衍生物及其用途 |
| CN116057045A (zh) | 2020-06-05 | 2023-05-02 | 金耐特生物制药公司 | 成纤维细胞生长因子受体激酶抑制剂 |
| WO2022188792A1 (zh) * | 2021-03-12 | 2022-09-15 | 四川科伦博泰生物医药股份有限公司 | 具有蛋白激酶抑制活性的杂环化合物、包含其的药物组合物及其制备方法和用途 |
Family Cites Families (41)
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| AU507066B1 (en) | 1977-09-06 | 1980-01-31 | Sumitomo Chemical Company, Limited | 2-Substituted-5-Hydroxy-1h-Imidazole 4-Carbozamide Derivatives |
| JPH03174153A (ja) | 1989-09-20 | 1991-07-29 | Fuji Photo Film Co Ltd | カラー画像形成方法 |
| CA2212061A1 (en) | 1995-02-02 | 1996-08-08 | Laramie Mary Gaster | Indole derivatives as 5-ht receptor antagonist |
| AU6526896A (en) | 1995-07-22 | 1997-02-18 | Rhone-Poulenc Rorer Limited | Substituted aromatic compounds and their pharmaceutical use |
| JP2003529536A (ja) | 1999-02-09 | 2003-10-07 | ３−ディメンショナル ファーマシューティカルズ， インコーポレイテッド | Ｃ１ｓ介在疾患および状態の処置法、およびそれのための化合物および組成物 |
| UA71971C2 (en) | 1999-06-04 | 2005-01-17 | Agoron Pharmaceuticals Inc | Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases |
| US6531478B2 (en) | 2000-02-24 | 2003-03-11 | Cheryl P. Kordik | Amino pyrazole derivatives useful for the treatment of obesity and other disorders |
| WO2003037274A2 (en) | 2001-11-01 | 2003-05-08 | Icagen, Inc. | Pyrazole-amides and-sulfonamides |
| US20040010027A1 (en) | 2001-12-17 | 2004-01-15 | Pharmacia & Upjohn Spa | Hydroxphenyl-pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical comositions comprising them |
| JP2005162612A (ja) | 2002-01-09 | 2005-06-23 | Ajinomoto Co Inc | アシルスルホンアミド誘導体 |
| US7166628B2 (en) | 2002-11-27 | 2007-01-23 | Boehringer Ingelheim Pharmaceuticals, Inc. | Cytokine inhibitors |
| CN102060806A (zh) | 2003-09-11 | 2011-05-18 | iTherX药品公司 | 细胞因子抑制剂 |
| EP1663953A1 (en) | 2003-09-24 | 2006-06-07 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| WO2005040152A1 (en) | 2003-10-20 | 2005-05-06 | E.I. Dupont De Nemours And Company | Heteroyclylphenyl-and heterocyclylpyridyl-substituted azolecarboxamides as herbicides |
| US7511042B2 (en) | 2003-12-03 | 2009-03-31 | Boehringer Ingelheim Pharmaceuticals, Inc. | Triazole compounds |
| SI1725544T1 (sl) | 2004-03-09 | 2009-10-31 | Boehringer Ingelheim Pharma | 3-(4-heterociklil-1,2,3-triazol-1-il)-N-aril-benzamidi kot inhibitorji proizvodnje citokinov za zdravljenje kroničnih vnetnih bolezni |
| US7485657B2 (en) | 2004-05-12 | 2009-02-03 | Boehringer Ingelheim Pharmaceuticals, Inc. | Anti-cytokine heterocyclic compounds |
| EP1819341A4 (en) | 2004-11-10 | 2011-06-29 | Synta Pharmaceuticals Corp | IL-12 MODULATORY CONNECTIONS |
| US7531560B2 (en) | 2004-11-10 | 2009-05-12 | Boehringer Ingelheim Pharmaceuticals, Inc. | Anti-cytokine heterocyclic compounds |
| JP2007076376A (ja) | 2005-09-09 | 2007-03-29 | Yanmar Co Ltd | トラクタ |
| WO2007056016A2 (en) | 2005-11-02 | 2007-05-18 | Kemia, Inc. | Bisamide cytokine inhibitors |
| WO2007075896A2 (en) | 2005-12-22 | 2007-07-05 | Kemia, Inc. | Heterocyclic cytokine inhibitors |
| JP2009536618A (ja) | 2006-04-18 | 2009-10-15 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ４−及び５−イミダゾリル環を含むサイトカイン阻害化合物の製造方法及びその中間体 |
| RU2009103999A (ru) | 2006-07-07 | 2010-08-20 | Шеринг Корпорейшн (US) | 3,4-дизамещенные циклобутен-1,2-дионы как лиганды схс-хемокиновых рецепторов |
| US8030487B2 (en) | 2006-07-07 | 2011-10-04 | Targegen, Inc. | 2-amino—5-substituted pyrimidine inhibitors |
| PT2041138E (pt) | 2006-07-07 | 2014-10-07 | Bristol Myers Squibb Co | Inibidores de pirrolotriazina quinase |
| BRPI0712795A2 (pt) * | 2006-07-07 | 2012-09-04 | Boehringer Ingelheim Int | derivados de heteroarila substituìdos com fenila e uso dos mesmos como agentes antitumorais |
| PE20080906A1 (es) | 2006-08-17 | 2008-07-05 | Kemia Inc | Derivados heteroarilo como inhibidores de citocina |
| WO2008079909A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
| WO2008089034A2 (en) | 2007-01-11 | 2008-07-24 | Kemia, Inc. | Cytokine inhibitors |
| EP2176249A2 (en) | 2007-07-02 | 2010-04-21 | Boehringer Ingelheim International GmbH | New chemical compounds |
| PE20090837A1 (es) | 2007-07-02 | 2009-07-24 | Boehringer Ingelheim Int | Nuevos compuestos quimicos |
| JP5385382B2 (ja) | 2008-07-24 | 2014-01-08 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | プロテインキナーゼ阻害剤としての３，４−ジアリールピラゾール |
| TW201014860A (en) | 2008-09-08 | 2010-04-16 | Boehringer Ingelheim Int | New chemical compounds |
| EA201100564A1 (ru) | 2008-09-29 | 2011-12-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Антипролиферативные соединения |
| US8569316B2 (en) | 2009-02-17 | 2013-10-29 | Boehringer Ingelheim International Gmbh | Pyrimido [5,4-D] pyrimidine derivatives for the inhibition of tyrosine kinases |
| JP5871896B2 (ja) | 2010-03-26 | 2016-03-01 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｂ−ｒａｆキナーゼインヒビター |
| WO2011117382A1 (en) | 2010-03-26 | 2011-09-29 | Boehringer Ingelheim International Gmbh | Pyridyltriazoles |
| US8710055B2 (en) | 2010-12-21 | 2014-04-29 | Boehringer Ingelheim International Gmbh | Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| US20130023531A1 (en) | 2011-01-27 | 2013-01-24 | Boehringer Ingelheim International Gmbh | Pyrimido[5,4-d]pyrimidylamino phenyl sulfonamides as serine/threonine kinase inhibitors |
| US8889684B2 (en) | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
-
2011
- 2011-03-25 JP JP2013500523A patent/JP5871896B2/ja active Active
- 2011-03-25 EP EP11709962.2A patent/EP2552905B1/en active Active
- 2011-03-25 US US13/636,157 patent/US9290507B2/en active Active
- 2011-03-25 WO PCT/EP2011/054611 patent/WO2011117381A1/en not_active Ceased
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