JP2015503504A5 - - Google Patents
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- Publication number
- JP2015503504A5 JP2015503504A5 JP2014548896A JP2014548896A JP2015503504A5 JP 2015503504 A5 JP2015503504 A5 JP 2015503504A5 JP 2014548896 A JP2014548896 A JP 2014548896A JP 2014548896 A JP2014548896 A JP 2014548896A JP 2015503504 A5 JP2015503504 A5 JP 2015503504A5
- Authority
- JP
- Japan
- Prior art keywords
- nitrogen
- optionally substituted
- membered
- oxygen
- sulfur
- 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.)
- Pending
Links
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 311
- 229910052757 nitrogen Inorganic materials 0.000 claims description 208
- 229910052760 oxygen Inorganic materials 0.000 claims description 177
- 229910052717 sulfur Chemical group 0.000 claims description 175
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 170
- 125000005842 heteroatom Chemical group 0.000 claims description 170
- 239000001301 oxygen Chemical group 0.000 claims description 170
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 169
- 239000011593 sulfur Chemical group 0.000 claims description 169
- 229910052739 hydrogen Inorganic materials 0.000 claims description 118
- 239000001257 hydrogen Substances 0.000 claims description 118
- 150000001875 compounds Chemical class 0.000 claims description 98
- 125000001931 aliphatic group Chemical group 0.000 claims description 96
- 125000000623 heterocyclic group Chemical group 0.000 claims description 96
- 125000002723 alicyclic group Chemical group 0.000 claims description 88
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 80
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 74
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 67
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 65
- 150000003839 salts Chemical class 0.000 claims description 56
- 150000002431 hydrogen Chemical class 0.000 claims description 41
- 125000002947 alkylene group Chemical group 0.000 claims description 32
- 229910052736 halogen Inorganic materials 0.000 claims description 21
- 150000002367 halogens Chemical class 0.000 claims description 21
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 19
- 229910052799 carbon Inorganic materials 0.000 claims description 19
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 16
- 125000000217 alkyl group Chemical group 0.000 claims description 13
- 125000003118 aryl group Chemical group 0.000 claims description 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 13
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 10
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 6
- 125000001153 fluoro group Chemical group F* 0.000 claims description 5
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 4
- -1 1,6-dihydro-6-oxo-3-pyridinyl Chemical group 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 125000005843 halogen group Chemical group 0.000 claims description 4
- 208000027866 inflammatory disease Diseases 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 125000001246 bromo group Chemical group Br* 0.000 claims description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 125000000335 thiazolyl group Chemical group 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims description 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
- 206010002198 Anaphylactic reaction Diseases 0.000 claims description 2
- 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
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims description 2
- 208000006029 Cardiomegaly Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- 206010019280 Heart failures Diseases 0.000 claims description 2
- 101000605630 Homo sapiens Phosphatidylinositol 3-kinase catalytic subunit type 3 Proteins 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 108091007960 PI3Ks Proteins 0.000 claims description 2
- 102100038329 Phosphatidylinositol 3-kinase catalytic subunit type 3 Human genes 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
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000007536 Thrombosis Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm 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
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims description 2
- 208000038016 acute inflammation Diseases 0.000 claims description 2
- 230000006022 acute inflammation Effects 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 230000007815 allergy Effects 0.000 claims description 2
- 230000036783 anaphylactic response Effects 0.000 claims description 2
- 208000003455 anaphylaxis Diseases 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 208000037976 chronic inflammation Diseases 0.000 claims description 2
- 230000006020 chronic inflammation Effects 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 210000000496 pancreas Anatomy 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 125000003107 substituted aryl group Chemical group 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- 238000006467 substitution reaction Methods 0.000 description 4
- 125000006413 ring segment Chemical group 0.000 description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 description 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 1
- YZCKVEUIGOORGS-IGMARMGPSA-N Protium Chemical group [1H] YZCKVEUIGOORGS-IGMARMGPSA-N 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- RWRIWBAIICGTTQ-UHFFFAOYSA-N difluoromethane Chemical compound FCF RWRIWBAIICGTTQ-UHFFFAOYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161579711P | 2011-12-23 | 2011-12-23 | |
| US61/579,711 | 2011-12-23 | ||
| US201261672030P | 2012-07-16 | 2012-07-16 | |
| US61/672,030 | 2012-07-16 | ||
| US201261716172P | 2012-10-19 | 2012-10-19 | |
| US61/716,172 | 2012-10-19 | ||
| PCT/US2012/070969 WO2013096630A1 (en) | 2011-12-23 | 2012-12-20 | Heteroaryls and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015503504A JP2015503504A (ja) | 2015-02-02 |
| JP2015503504A5 true JP2015503504A5 (https=) | 2016-02-18 |
Family
ID=48655164
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014548896A Pending JP2015503504A (ja) | 2011-12-23 | 2012-12-20 | ヘテロアリールおよびその使用 |
| JP2014548902A Pending JP2015503505A (ja) | 2011-12-23 | 2012-12-20 | ヘテロアリールおよびその使用 |
| JP2014548899A Pending JP2015506347A (ja) | 2011-12-23 | 2012-12-20 | ヘテロアリールおよびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014548902A Pending JP2015503505A (ja) | 2011-12-23 | 2012-12-20 | ヘテロアリールおよびその使用 |
| JP2014548899A Pending JP2015506347A (ja) | 2011-12-23 | 2012-12-20 | ヘテロアリールおよびその使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US20130165464A1 (https=) |
| EP (3) | EP2793894A4 (https=) |
| JP (3) | JP2015503504A (https=) |
| AR (3) | AR089445A1 (https=) |
| TW (3) | TW201332989A (https=) |
| UY (3) | UY34538A (https=) |
| WO (3) | WO2013096630A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2010090716A1 (en) | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| US8859768B2 (en) | 2010-08-11 | 2014-10-14 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2012021611A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| TW201217365A (en) | 2010-08-11 | 2012-05-01 | Millennium Pharm Inc | Heteroaryls and uses thereof |
| TW201307309A (zh) | 2010-10-13 | 2013-02-16 | Millennium Pharm Inc | 雜芳基化合物及其用途 |
| SI3038622T1 (en) | 2013-08-28 | 2018-08-31 | Medivation Technologies Llc | Heterocyclic compounds and methods of use |
| WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2015108861A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| CN106922146B (zh) * | 2014-10-02 | 2020-05-26 | 豪夫迈·罗氏有限公司 | 用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物 |
| EP3265457A1 (en) | 2015-03-04 | 2018-01-10 | Medivation Technologies LLC | Sterol regulatory element-binding proteins (srebps) inhibitors |
| US10183015B2 (en) | 2015-03-04 | 2019-01-22 | Medivation Technologies Llc | Heterocyclic compounds and methods of use |
| JP2019513700A (ja) | 2016-03-16 | 2019-05-30 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 殺有害生物剤及び植物保護剤としてのｎ−（シアノベンジル）−６−（シクロプロピル−カルボニルアミノ）−４−（フェニル）−ピリジン−２−カルボキサミド誘導体及び関連する化合物 |
| EP3284739A1 (de) | 2017-07-19 | 2018-02-21 | Bayer CropScience Aktiengesellschaft | Substituierte (het)arylverbindungen als schädlingsbekämpfungsmittel |
| MY201038A (en) * | 2017-07-28 | 2024-01-31 | Yuhan Corp | Intermediates useful for the synthesis of a selective inhibitor against protein kinase and processes for preparing the same |
| SG11201913517UA (en) | 2017-07-28 | 2020-02-27 | Yuhan Corp | Improved process for preparing aminopyrimidine derivatives |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CN110041252A (zh) * | 2019-05-22 | 2019-07-23 | 南京合巨药业有限公司 | 一种2-氯-4-肼基吡啶的制备方法 |
| CN114867724B (zh) * | 2019-05-31 | 2025-11-07 | 班塔姆制药有限责任公司 | 用于制备噻唑基吡唑甲酸及其中间体的方法 |
| WO2021011720A2 (en) * | 2019-07-18 | 2021-01-21 | Avidence Therapeutics, Inc. | Anti-osteoarthritis compounds and related compositions and methods |
| WO2025117722A1 (en) * | 2023-11-27 | 2025-06-05 | Rubedo Life Sciences, Inc. | Carbon linked bcl inhibitors and senolytic compounds and uses thereof |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH27357A (en) * | 1989-09-22 | 1993-06-21 | Fujisawa Pharmaceutical Co | Pyrazole derivatives and pharmaceutical compositions comprising the same |
| MX9300141A (es) * | 1992-01-13 | 1994-07-29 | Smithkline Beecham Corp | Compuestos de imidazol novedosos, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen. |
| GB2306108A (en) * | 1995-10-13 | 1997-04-30 | Merck & Co Inc | Treatment of Raf-mediated cancers with imidazole derivatives |
| IL136768A0 (en) * | 1997-12-22 | 2001-06-14 | Bayer Ag | INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS |
| WO2002092573A2 (en) * | 2001-05-16 | 2002-11-21 | Vertex Pharmaceuticals Incorporated | Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases |
| EP1414443B1 (en) * | 2001-08-01 | 2006-11-15 | Merck & Co., Inc. | BENZIMIDAZO 4,5-f|ISOQUINOLINONE DERIVATIVES |
| US7582631B2 (en) * | 2004-01-14 | 2009-09-01 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| CA2589827A1 (en) * | 2004-12-21 | 2006-06-29 | Merck & Co., Inc. | Mitotic kinesin inhibitors |
| MX2007008781A (es) * | 2005-01-21 | 2007-09-11 | Astex Therapeutics Ltd | Compuestos farmaceuticos. |
| AU2007275221A1 (en) * | 2006-07-20 | 2008-01-24 | Allen J. Borchardt | Benzothiophene inhibitors of RHO kinase |
| UY30892A1 (es) * | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| EP2134175A4 (en) * | 2007-03-29 | 2012-01-11 | Glaxosmithkline Llc | HAMMER OF ACT ACTIVITY |
| GB0709031D0 (en) * | 2007-05-10 | 2007-06-20 | Sareum Ltd | Pharmaceutical compounds |
| TW200911798A (en) * | 2007-08-02 | 2009-03-16 | Amgen Inc | PI3 kinase modulators and methods of use |
| WO2009115572A2 (en) * | 2008-03-21 | 2009-09-24 | Novartis Ag | Novel heterocyclic compounds and uses therof |
| ES2491522T3 (es) * | 2008-06-19 | 2014-09-08 | Millennium Pharmaceuticals, Inc. | Derivados de tiofeno o tiazol y su uso como inhibidores de PI3K |
| US9187426B2 (en) * | 2008-06-27 | 2015-11-17 | Novartis Ag | Organic compounds |
| WO2010090716A1 (en) * | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| WO2010127152A2 (en) * | 2009-04-29 | 2010-11-04 | Irm Llc | Compounds and compositions as microsomal prostaglandin e synthase-1 inhibitors |
| EP2430013B1 (en) * | 2009-05-13 | 2014-10-15 | Amgen Inc. | Heteroaryl compounds as pikk inhibitors |
| AR077975A1 (es) * | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| WO2011149874A2 (en) * | 2010-05-26 | 2011-12-01 | Schering Corporation | N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1 |
| WO2012084678A1 (en) * | 2010-12-23 | 2012-06-28 | Syngenta Participations Ag | Novel imidazoles useful as plant fungicides |
| US9090628B2 (en) * | 2011-03-21 | 2015-07-28 | Genentech, Inc. | Benzoxazepin compounds selective for PI3K P110 delta and methods of use |
| US9732085B2 (en) * | 2011-12-21 | 2017-08-15 | Ono Pharmaceutical Co., Ltd. | Pyridinone and pyrimidinone derivatives as factor Xia |
-
2012
- 2012-12-20 TW TW101148909A patent/TW201332989A/zh unknown
- 2012-12-20 WO PCT/US2012/070969 patent/WO2013096630A1/en not_active Ceased
- 2012-12-20 US US13/722,134 patent/US20130165464A1/en not_active Abandoned
- 2012-12-20 WO PCT/US2012/070980 patent/WO2013096637A1/en not_active Ceased
- 2012-12-20 WO PCT/US2012/070988 patent/WO2013096642A1/en not_active Ceased
- 2012-12-20 EP EP12859082.5A patent/EP2793894A4/en not_active Withdrawn
- 2012-12-20 TW TW101148828A patent/TW201331194A/zh unknown
- 2012-12-20 JP JP2014548896A patent/JP2015503504A/ja active Pending
- 2012-12-20 JP JP2014548902A patent/JP2015503505A/ja active Pending
- 2012-12-20 US US13/721,877 patent/US20130165472A1/en not_active Abandoned
- 2012-12-20 JP JP2014548899A patent/JP2015506347A/ja active Pending
- 2012-12-20 EP EP12859324.1A patent/EP2793879A4/en not_active Withdrawn
- 2012-12-20 EP EP12860844.5A patent/EP2793880A4/en not_active Withdrawn
- 2012-12-20 UY UY0001034538A patent/UY34538A/es not_active Application Discontinuation
- 2012-12-20 US US13/722,222 patent/US20130165483A1/en not_active Abandoned
- 2012-12-20 TW TW101148830A patent/TW201332988A/zh unknown
- 2012-12-20 UY UY0001034540A patent/UY34540A/es not_active Application Discontinuation
- 2012-12-20 UY UY0001034539A patent/UY34539A/es not_active Application Discontinuation
- 2012-12-26 AR ARP120104956A patent/AR089445A1/es unknown
- 2012-12-26 AR ARP120104957A patent/AR089446A1/es unknown
- 2012-12-26 AR ARP120104958A patent/AR089447A1/es unknown
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