JP2015503505A5 - - Google Patents
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- Publication number
- JP2015503505A5 JP2015503505A5 JP2014548902A JP2014548902A JP2015503505A5 JP 2015503505 A5 JP2015503505 A5 JP 2015503505A5 JP 2014548902 A JP2014548902 A JP 2014548902A JP 2014548902 A JP2014548902 A JP 2014548902A JP 2015503505 A5 JP2015503505 A5 JP 2015503505A5
- Authority
- JP
- Japan
- Prior art keywords
- nitrogen
- optionally substituted
- membered
- pharmaceutically acceptable
- 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.)
- Pending
Links
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 246
- 229910052757 nitrogen Inorganic materials 0.000 claims description 157
- 229910052760 oxygen Inorganic materials 0.000 claims description 129
- 229910052717 sulfur Chemical group 0.000 claims description 128
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 123
- 125000005842 heteroatom Chemical group 0.000 claims description 123
- 239000001301 oxygen Chemical group 0.000 claims description 123
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 122
- 239000011593 sulfur Chemical group 0.000 claims description 122
- 229910052739 hydrogen Inorganic materials 0.000 claims description 87
- 239000001257 hydrogen Substances 0.000 claims description 87
- 150000001875 compounds Chemical class 0.000 claims description 86
- 125000000623 heterocyclic group Chemical group 0.000 claims description 71
- 125000001931 aliphatic group Chemical group 0.000 claims description 70
- 125000002723 alicyclic group Chemical group 0.000 claims description 62
- 150000003839 salts Chemical class 0.000 claims description 61
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 59
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 52
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 48
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 46
- 150000002431 hydrogen Chemical class 0.000 claims description 34
- 125000002947 alkylene group Chemical group 0.000 claims description 22
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 20
- 229910052799 carbon Inorganic materials 0.000 claims description 20
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 18
- 229910052736 halogen Inorganic materials 0.000 claims description 17
- 150000002367 halogens Chemical class 0.000 claims description 17
- 125000000217 alkyl group Chemical group 0.000 claims description 13
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 11
- 239000000203 mixture Substances 0.000 claims description 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 7
- 125000004429 atom Chemical group 0.000 claims description 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 5
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 125000001309 chloro group Chemical group Cl* 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
- 125000001188 haloalkyl 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
- 125000001072 heteroaryl group Chemical group 0.000 claims description 3
- 125000001424 substituent 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
- 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
- 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
- 125000001246 bromo group Chemical group Br* 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
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 125000005843 halogen 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
- 230000002401 inhibitory effect Effects 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
- 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
- 241001228709 Suruga Species 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000000034 method Methods 0.000 description 5
- 0 *c1c(*)nc(*)[n]1* Chemical compound *c1c(*)nc(*)[n]1* 0.000 description 2
- YZCKVEUIGOORGS-IGMARMGPSA-N Protium Chemical group [1H] YZCKVEUIGOORGS-IGMARMGPSA-N 0.000 description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 2
- 125000006413 ring segment Chemical group 0.000 description 2
- 238000006467 substitution reaction Methods 0.000 description 2
- 125000000335 thiazolyl group Chemical group 0.000 description 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 description 1
- -1 2-chloro-6-fluorophenyl Chemical group 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/US2012/070988 WO2013096642A1 (en) | 2011-12-23 | 2012-12-20 | Heteroaryls and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015503505A JP2015503505A (ja) | 2015-02-02 |
| JP2015503505A5 true JP2015503505A5 (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 |
| JP2014548899A Pending JP2015506347A (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 |
Family Applications Before (2)
| 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 |
| 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) | US20130165472A1 (https=) |
| EP (3) | EP2793894A4 (https=) |
| JP (3) | JP2015503504A (https=) |
| AR (3) | AR089447A1 (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 |
|---|---|---|---|---|
| JP5581219B2 (ja) | 2008-01-25 | 2014-08-27 | 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 | チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用 |
| US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
| WO2010090716A1 (en) | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
| WO2012021611A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| MX2013001660A (es) | 2010-08-11 | 2013-06-03 | Millenium Pharmaceuticals Inc | Heteroarilos y usos de los mismos. |
| US8859768B2 (en) | 2010-08-11 | 2014-10-14 | Millennium Pharmaceuticals, 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 |
| SG10201806370QA (en) | 2013-08-28 | 2018-08-30 | Medivation Tech Llc | Heterocyclic compounds and methods of use |
| WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| AU2015206652A1 (en) | 2014-01-14 | 2016-08-04 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| JP6507234B2 (ja) * | 2014-10-02 | 2019-04-24 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ブルトンチロシンキナーゼ（ｂｔｋ）によって介入される障害の処置における使用のためのピラゾールカルボキサミド化合物 |
| JP2018507235A (ja) | 2015-03-04 | 2018-03-15 | メディベイション テクノロジーズ エルエルシー | ステロール調節エレメント結合タンパク質（ｓｒｅｂｐ）阻害剤 |
| JP2018507234A (ja) | 2015-03-04 | 2018-03-15 | メディベイション テクノロジーズ エルエルシー | 肝臓線維症、コレステロールの上昇およびインスリン抵抗性を処置する際における使用のためのｓｒｅｂｐ遮断薬 |
| CN109071444A (zh) | 2016-03-16 | 2018-12-21 | 拜耳作物科学股份公司 | 作为农药和植物保护剂的n-(氰苄基)-6-(环丙基-羰基氨基)-4-(苯基)-吡啶-2-羧酰胺衍生物及相关化合物 |
| EP3284739A1 (de) | 2017-07-19 | 2018-02-21 | Bayer CropScience Aktiengesellschaft | Substituierte (het)arylverbindungen als schädlingsbekämpfungsmittel |
| FI3658552T3 (fi) | 2017-07-28 | 2023-11-16 | Yuhan Corp | Menetelmä n-(5-((4-(4-((dimetyyliamino)metyyli)-3-fenyyli-1h-pyratsol-1-yyli)pyrimidin-2-yyli)amino)-4-metoksi-2-morfolinofenyyli)akryyliamidin valmistamiseksi saattamalla vastaava amiini reagoimaan 3-halopropionyylikloridin kanssa |
| ES2959967T3 (es) | 2017-07-28 | 2024-02-29 | Yuhan Corp | Procedimiento de preparación deN-(5-(4-(4-formil-3-fenil-1h-pirazol-1-il)pirimidin-2-ilamino)-4-metoxi-2-morfolinofenil)acrilamida |
| WO2020113094A1 (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 |
| WO2020243582A1 (en) * | 2019-05-31 | 2020-12-03 | Bantam Pharmaceutical, Llc | Methods for making thiszolylpyrazole carboxylic acids and intermediates therefor |
| WO2021011723A1 (en) * | 2019-07-18 | 2021-01-21 | Avidence Therapeutics, Inc. | Anti-osteoarthritis hydantoin compounds and related compositions and methods |
| US20250171435A1 (en) * | 2023-11-27 | 2025-05-29 | 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 |
| DE69836563T2 (de) * | 1997-12-22 | 2007-05-16 | Bayer Pharmaceuticals Corp., West Haven | INHIBIERUNG DER p38 KINASE-AKTIVITÄT DURCH DIE VERWENDUNG VON ARYL- UND HETEROARYL-SUBSTITUIERTEN HARNSTOFFEN |
| AU2002308748A1 (en) * | 2001-05-16 | 2002-11-25 | 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 |
| US20080045492A1 (en) * | 2004-12-21 | 2008-02-21 | Coleman Paul J | Mitotic Kinesin Inhibitors |
| MX2007008781A (es) * | 2005-01-21 | 2007-09-11 | Astex Therapeutics Ltd | Compuestos farmaceuticos. |
| EP2044061A2 (en) * | 2006-07-20 | 2009-04-08 | Mehmet Kahraman | Benzothiophene inhibitors of rho kinase |
| UY30892A1 (es) * | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
| WO2008121786A1 (en) * | 2007-03-29 | 2008-10-09 | Smithkline Beecham Corporation | Inhibitors of akt activity |
| GB0709031D0 (en) * | 2007-05-10 | 2007-06-20 | Sareum Ltd | Pharmaceutical compounds |
| AU2008282728B2 (en) * | 2007-08-02 | 2012-04-19 | Amgen Inc. | Pl3 kinase modulators and methods of use |
| AU2009227013B2 (en) * | 2008-03-21 | 2013-01-10 | Novartis Ag | Novel heterocyclic compounds and uses therof |
| JP5596026B2 (ja) * | 2008-06-19 | 2014-09-24 | 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 | チオフェン又はチアゾール誘導体及びｐｉ３ｋ阻害剤としてのそれらの使用 |
| EP2307379A2 (en) * | 2008-06-27 | 2011-04-13 | 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 |
| MX2011012037A (es) * | 2009-05-13 | 2012-02-28 | Amgen Inc | Compuestos de heteroarilo como inhibidores de pikk. |
| JO3002B1 (ar) * | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
| 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 |
| WO2012126901A1 (en) * | 2011-03-21 | 2012-09-27 | F. Hoffmann-La Roche Ag | Benzoxazepin compounds selective for pi3k p110 delta and methods of use |
| RU2630677C2 (ru) * | 2011-12-21 | 2017-09-12 | Оно Фармасьютикал Ко., Лтд. | Соединения |
-
2012
- 2012-12-20 WO PCT/US2012/070969 patent/WO2013096630A1/en not_active Ceased
- 2012-12-20 EP EP12859082.5A patent/EP2793894A4/en not_active Withdrawn
- 2012-12-20 EP EP12859324.1A patent/EP2793879A4/en not_active Withdrawn
- 2012-12-20 WO PCT/US2012/070980 patent/WO2013096637A1/en not_active Ceased
- 2012-12-20 JP JP2014548896A patent/JP2015503504A/ja active Pending
- 2012-12-20 TW TW101148909A patent/TW201332989A/zh unknown
- 2012-12-20 WO PCT/US2012/070988 patent/WO2013096642A1/en not_active Ceased
- 2012-12-20 UY UY0001034538A patent/UY34538A/es not_active Application Discontinuation
- 2012-12-20 UY UY0001034539A patent/UY34539A/es not_active Application Discontinuation
- 2012-12-20 US US13/721,877 patent/US20130165472A1/en not_active Abandoned
- 2012-12-20 US US13/722,222 patent/US20130165483A1/en not_active Abandoned
- 2012-12-20 UY UY0001034540A patent/UY34540A/es not_active Application Discontinuation
- 2012-12-20 US US13/722,134 patent/US20130165464A1/en not_active Abandoned
- 2012-12-20 JP JP2014548899A patent/JP2015506347A/ja active Pending
- 2012-12-20 JP JP2014548902A patent/JP2015503505A/ja active Pending
- 2012-12-20 EP EP12860844.5A patent/EP2793880A4/en not_active Withdrawn
- 2012-12-20 TW TW101148828A patent/TW201331194A/zh unknown
- 2012-12-20 TW TW101148830A patent/TW201332988A/zh unknown
- 2012-12-26 AR ARP120104958A patent/AR089447A1/es unknown
- 2012-12-26 AR ARP120104957A patent/AR089446A1/es unknown
- 2012-12-26 AR ARP120104956A patent/AR089445A1/es unknown