JP2010532381A5 - - Google Patents
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- JP2010532381A5 JP2010532381A5 JP2010515223A JP2010515223A JP2010532381A5 JP 2010532381 A5 JP2010532381 A5 JP 2010532381A5 JP 2010515223 A JP2010515223 A JP 2010515223A JP 2010515223 A JP2010515223 A JP 2010515223A JP 2010532381 A5 JP2010532381 A5 JP 2010532381A5
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- JP
- Japan
- Prior art keywords
- nitrogen
- compound
- optionally substituted
- sulfur
- oxygen
- 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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- 150000001875 compounds Chemical class 0.000 claims description 86
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 67
- 229910052757 nitrogen Inorganic materials 0.000 claims description 50
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 44
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 44
- 229910052760 oxygen Inorganic materials 0.000 claims description 44
- 239000001301 oxygen Chemical group 0.000 claims description 44
- 229910052717 sulfur Chemical group 0.000 claims description 44
- 239000011593 sulfur Chemical group 0.000 claims description 44
- 125000005842 heteroatom Chemical group 0.000 claims description 42
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 33
- 125000003118 aryl group Chemical group 0.000 claims description 23
- 125000004429 atom Chemical group 0.000 claims description 22
- 239000003795 chemical substances by application Substances 0.000 claims description 22
- 201000010099 disease Diseases 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 125000002950 monocyclic group Chemical group 0.000 claims description 18
- 125000002619 bicyclic group Chemical group 0.000 claims description 17
- 239000000203 mixture Substances 0.000 claims description 17
- 239000003814 drug Substances 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 229920006395 saturated elastomer Polymers 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 9
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
- 229940079593 drug Drugs 0.000 claims description 7
- 230000001404 mediated effect Effects 0.000 claims description 7
- 229940124597 therapeutic agent Drugs 0.000 claims description 7
- 208000020084 Bone disease Diseases 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 125000001931 aliphatic group Chemical group 0.000 claims description 6
- 125000002947 alkylene group Chemical group 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 5
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000029462 Immunodeficiency disease Diseases 0.000 claims description 4
- 108010025020 Nerve Growth Factor Proteins 0.000 claims description 4
- 102000007072 Nerve Growth Factors Human genes 0.000 claims description 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 4
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 4
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 4
- 230000001028 anti-proliverative effect Effects 0.000 claims description 4
- 230000001066 destructive effect Effects 0.000 claims description 4
- 206010012601 diabetes mellitus Diseases 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 4
- 125000002541 furyl group Chemical group 0.000 claims description 4
- 206010017758 gastric cancer Diseases 0.000 claims description 4
- 208000014951 hematologic disease Diseases 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 239000002955 immunomodulating agent Substances 0.000 claims description 4
- 229940121354 immunomodulator Drugs 0.000 claims description 4
- 230000002584 immunomodulator Effects 0.000 claims description 4
- 229960003444 immunosuppressant agent Drugs 0.000 claims description 4
- 230000001861 immunosuppressant effect Effects 0.000 claims description 4
- 239000003018 immunosuppressive agent Substances 0.000 claims description 4
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 4
- 208000019423 liver disease Diseases 0.000 claims description 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 4
- 239000003900 neurotrophic factor Substances 0.000 claims description 4
- -1 oxadiadiolyl Chemical group 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 0.000 claims description 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 4
- 201000011549 stomach cancer Diseases 0.000 claims description 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 4
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000001425 triazolyl group Chemical group 0.000 claims description 4
- 208000019838 Blood disease Diseases 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 239000003443 antiviral agent Substances 0.000 claims description 3
- 239000012472 biological sample Substances 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 238000002512 chemotherapy Methods 0.000 claims description 3
- 208000018706 hematopoietic system disease Diseases 0.000 claims description 3
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010023825 Laryngeal cancer Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 241000124008 Mammalia Species 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims description 2
- 208000019622 heart disease Diseases 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 150000008624 imidazolidinones Chemical class 0.000 claims description 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 206010023841 laryngeal neoplasm Diseases 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 230000001926 lymphatic effect Effects 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 210000000056 organ Anatomy 0.000 claims description 2
- 201000008968 osteosarcoma Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 125000000561 purinyl group Chemical group N1=C(N=C2N=CNC2=C1)* 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical class O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 2
- 102000009929 raf Kinases Human genes 0.000 claims description 2
- 108010077182 raf Kinases Proteins 0.000 claims description 2
- 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 description 2
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 claims description 2
- 125000005306 thianaphthenyl group Chemical group 0.000 claims description 2
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims description 2
- 125000004306 triazinyl group Chemical group 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 230000003612 virological effect Effects 0.000 claims description 2
- 238000011374 additional therapy Methods 0.000 claims 1
- 230000000973 chemotherapeutic effect Effects 0.000 claims 1
- 238000002513 implantation Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 8
- 102000001253 Protein Kinase Human genes 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 108060006633 protein kinase Proteins 0.000 description 2
- 208000008385 Urogenital Neoplasms Diseases 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 238000002054 transplantation Methods 0.000 description 1
- 208000037964 urogenital cancer Diseases 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94731907P | 2007-06-29 | 2007-06-29 | |
| PCT/US2008/068789 WO2009006404A2 (en) | 2007-06-29 | 2008-06-30 | Heterocyclic compounds useful as raf kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010532381A JP2010532381A (ja) | 2010-10-07 |
| JP2010532381A5 true JP2010532381A5 (enExample) | 2012-07-26 |
Family
ID=40015666
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010515223A Pending JP2010532381A (ja) | 2007-06-29 | 2008-06-30 | Ｒａｆキナーゼ阻害剤として有用な複素環式化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7968536B2 (enExample) |
| EP (1) | EP2167497A2 (enExample) |
| JP (1) | JP2010532381A (enExample) |
| CN (1) | CN101743242A (enExample) |
| AU (1) | AU2008273017C1 (enExample) |
| CA (1) | CA2694284A1 (enExample) |
| NZ (1) | NZ582349A (enExample) |
| WO (1) | WO2009006404A2 (enExample) |
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| CL2008001933A1 (es) | 2007-06-29 | 2009-09-25 | Millennium Pharm Inc | Compuestos derivados de pirimidina, inhibidores de la raf quinasa; compuestos intermediarios; procedimiento de preparacion; composicion farmaceutica; y su uso para tratar trastornos proliferativos, cardiacos, neurodegenerativos, inflamatorios, oseos, inmunologicos enfermedad viral, entre otros. |
| JP5507567B2 (ja) * | 2008-09-26 | 2014-05-28 | 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 | Ｃｃｒ１受容体拮抗薬としてのアザインダゾール化合物 |
| EP2379513A1 (en) * | 2008-12-30 | 2011-10-26 | Millennium Pharmaceuticals, Inc. | Heteroaryl compounds useful as raf kinase inhibitors |
| GB0910003D0 (en) | 2009-06-11 | 2009-07-22 | Univ Leuven Kath | Novel compounds for the treatment of neurodegenerative diseases |
| AR078793A1 (es) * | 2009-10-27 | 2011-12-07 | Orion Corp | Derivados de carboxamidas no esteroidales y acil hidrazona moduladores de receptores androgenicos de tejido selectivo (sarm), composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del cancer de prostata entre otros |
| WO2011062437A2 (ko) | 2009-11-20 | 2011-05-26 | 에스케이케미칼주식회사 | 고나도트로핀 방출 호르몬 수용체 길항제, 이의 제조방법 및 이를 함유하는 약제학적 조성물 |
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| CN104761502A (zh) * | 2014-01-03 | 2015-07-08 | 中国药科大学 | 苯并咪唑衍生物、其制法及医药用途 |
| US9914698B2 (en) | 2014-01-08 | 2018-03-13 | Shanghai Jiaotong University School Of Medicine | Stearoyl amino acid salt and preparation method and application thereof |
| UY36294A (es) | 2014-09-12 | 2016-04-29 | Novartis Ag | Compuestos y composiciones como inhibidores de quinasa |
| CN106663839B (zh) * | 2015-01-14 | 2019-05-10 | 株式会社东芝 | 非水电解质电池和电池组 |
| EP3185341B1 (fr) * | 2015-12-21 | 2019-09-11 | The Swatch Group Research and Development Ltd | Cathode de pile métal/air et procédés de fabrication d'une telle cathode |
| JP2019196307A (ja) | 2016-09-15 | 2019-11-14 | 武田薬品工業株式会社 | 複素環アミド化合物 |
| EP3515446B1 (en) | 2016-09-19 | 2023-12-20 | Novartis AG | Therapeutic combinations comprising a raf inhibitor and a erk inhibitor |
| US11471538B2 (en) | 2017-02-10 | 2022-10-18 | INSERM (Institut National de la Santéet de la Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the MAPK pathway |
| CN106928152A (zh) * | 2017-03-03 | 2017-07-07 | 符爱清 | 一种尿嘧啶的制备方法 |
| US11266653B2 (en) | 2017-05-02 | 2022-03-08 | Novartis Ag | Combination therapy |
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| EP3732285A1 (en) | 2017-12-28 | 2020-11-04 | Tract Pharmaceuticals, Inc. | Stem cell culture systems for columnar epithelial stem cells, and uses related thereto |
| JP7184383B2 (ja) * | 2018-02-01 | 2022-12-06 | ザ・ユニバーシティ・オブ・シドニー | 抗癌性化合物 |
| ES3025633T3 (en) | 2019-05-13 | 2025-06-09 | Novartis Ag | New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer |
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| JP7807381B2 (ja) * | 2020-03-02 | 2026-01-27 | シロナックス リミテッド． | フェロトーシス阻害剤ジアリールアミンパラアセトアミド類 |
| US12612388B2 (en) | 2020-05-20 | 2026-04-28 | Sironax Ltd. | Receptor-interacting protein 1 inhibitors including piperazine heterocyclic amide ureas |
| BR112023001557A2 (pt) * | 2020-07-28 | 2023-04-04 | Jazz Pharmaceuticals Ireland Ltd | Inibidores de raf bicíclicos fundidos e métodos para uso dos mesmos |
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| CN117567388B (zh) * | 2023-11-14 | 2024-04-16 | 济南悟通生物科技有限公司 | 一种2-乙酰基-5-噻唑甲酸的合成方法 |
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- 2008-06-30 CN CN200880022610A patent/CN101743242A/zh active Pending
- 2008-06-30 WO PCT/US2008/068789 patent/WO2009006404A2/en not_active Ceased
- 2008-06-30 AU AU2008273017A patent/AU2008273017C1/en not_active Expired - Fee Related
- 2008-06-30 CA CA2694284A patent/CA2694284A1/en not_active Abandoned
- 2008-06-30 EP EP08781174A patent/EP2167497A2/en not_active Withdrawn
- 2008-06-30 US US12/164,905 patent/US7968536B2/en not_active Expired - Fee Related
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