JP2013542941A5 - - Google Patents
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- JP2013542941A5 JP2013542941A5 JP2013534002A JP2013534002A JP2013542941A5 JP 2013542941 A5 JP2013542941 A5 JP 2013542941A5 JP 2013534002 A JP2013534002 A JP 2013534002A JP 2013534002 A JP2013534002 A JP 2013534002A JP 2013542941 A5 JP2013542941 A5 JP 2013542941A5
- Authority
- JP
- Japan
- Prior art keywords
- membered
- nitrogen
- sulfur
- oxygen
- optionally substituted
- 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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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 563
- 229910052757 nitrogen Inorganic materials 0.000 claims description 408
- 229910052760 oxygen Inorganic materials 0.000 claims description 388
- 229910052717 sulfur Inorganic materials 0.000 claims description 383
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 369
- 239000001301 oxygen Substances 0.000 claims description 369
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 363
- 239000011593 sulfur Substances 0.000 claims description 362
- 125000005842 heteroatom Chemical group 0.000 claims description 360
- 229910052739 hydrogen Inorganic materials 0.000 claims description 223
- 125000001931 aliphatic group Chemical group 0.000 claims description 217
- 239000001257 hydrogen Substances 0.000 claims description 213
- 125000000623 heterocyclic group Chemical group 0.000 claims description 205
- 125000002723 alicyclic group Chemical group 0.000 claims description 200
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 163
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 156
- 150000001875 compounds Chemical class 0.000 claims description 145
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 122
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 112
- 150000002431 hydrogen Chemical class 0.000 claims description 78
- 125000002947 alkylene group Chemical group 0.000 claims description 54
- 125000003118 aryl group Chemical group 0.000 claims description 54
- 125000000217 alkyl group Chemical group 0.000 claims description 50
- 229910052736 halogen Inorganic materials 0.000 claims description 44
- 150000002367 halogens Chemical class 0.000 claims description 44
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 36
- 150000003839 salts Chemical class 0.000 claims description 24
- 125000001072 heteroaryl group Chemical group 0.000 claims description 20
- 125000004429 atom Chemical group 0.000 claims description 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 19
- 125000005843 halogen group Chemical group 0.000 claims description 17
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 16
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 13
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 11
- 229910052731 fluorine Inorganic materials 0.000 claims description 11
- 239000011737 fluorine Substances 0.000 claims description 11
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims description 10
- 125000001188 haloalkyl group Chemical group 0.000 claims description 10
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims description 7
- 101100347605 Arabidopsis thaliana VIII-A gene Proteins 0.000 claims description 5
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000027866 inflammatory disease Diseases 0.000 claims description 4
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims description 3
- 108091007960 PI3Ks Proteins 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- -1 substituted Chemical class 0.000 claims description 3
- 101100347612 Arabidopsis thaliana VIII-B gene Proteins 0.000 claims description 2
- BUDQDWGNQVEFAC-UHFFFAOYSA-N Dihydropyran Chemical compound C1COC=CC1 BUDQDWGNQVEFAC-UHFFFAOYSA-N 0.000 claims description 2
- 101150097381 Mtor gene Proteins 0.000 claims description 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 13
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 13
- 125000004354 sulfur functional group Chemical group 0.000 claims 6
- 238000006467 substitution reaction Methods 0.000 claims 5
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 description 3
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 1
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 208000003174 Brain Neoplasms Diseases 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 description 1
- 208000006029 Cardiomegaly Diseases 0.000 description 1
- 206010008342 Cervix carcinoma Diseases 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 206010014733 Endometrial cancer Diseases 0.000 description 1
- 206010014759 Endometrial neoplasm Diseases 0.000 description 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 description 1
- 208000032612 Glial tumor Diseases 0.000 description 1
- 206010018338 Glioma Diseases 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 208000008839 Kidney Neoplasms Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 206010038389 Renal cancer Diseases 0.000 description 1
- 208000005718 Stomach Neoplasms Diseases 0.000 description 1
- 208000007536 Thrombosis Diseases 0.000 description 1
- 208000024770 Thyroid neoplasm Diseases 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 150000001345 alkine derivatives Chemical class 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 230000036783 anaphylactic response Effects 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- LCIYFINKFGDAHD-UHFFFAOYSA-N azepane;3-nitrobenzoic acid Chemical group C1CCCNCC1.OC(=O)C1=CC=CC([N+]([O-])=O)=C1 LCIYFINKFGDAHD-UHFFFAOYSA-N 0.000 description 1
- 201000010881 cervical cancer Diseases 0.000 description 1
- 208000037976 chronic inflammation Diseases 0.000 description 1
- 230000006020 chronic inflammation Effects 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 125000004663 dialkyl amino group Chemical group 0.000 description 1
- 201000004101 esophageal cancer Diseases 0.000 description 1
- 206010017758 gastric cancer Diseases 0.000 description 1
- 208000005017 glioblastoma Diseases 0.000 description 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 201000010982 kidney cancer Diseases 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 201000002528 pancreatic cancer Diseases 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39251510P | 2010-10-13 | 2010-10-13 | |
| US61/392,515 | 2010-10-13 | ||
| PCT/US2011/056135 WO2012051410A2 (en) | 2010-10-13 | 2011-10-13 | Heteroaryls and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013542941A JP2013542941A (ja) | 2013-11-28 |
| JP2013542941A5 true JP2013542941A5 (cg-RX-API-DMAC7.html) | 2014-12-04 |
Family
ID=45938970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013534002A Pending JP2013542941A (ja) | 2010-10-13 | 2011-10-13 | ヘテロアリールおよびその使用 |
Country Status (24)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| 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 |
| AR082665A1 (es) | 2010-08-11 | 2012-12-26 | Millennium Pharm Inc | Derivados heteroarilicos inhibidores de quinasas pi3k, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos proliferativos, inflamatorios y/o cardiovasculares |
| EP2603216A4 (en) | 2010-08-11 | 2013-12-18 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
| CN103467481B (zh) * | 2012-06-07 | 2016-08-31 | 上海汇伦生命科技有限公司 | 二氢吡啶类化合物、其组合物、制备方法和用途 |
| US9586949B2 (en) | 2015-02-09 | 2017-03-07 | Incyte Corporation | Aza-heteroaryl compounds as PI3K-gamma inhibitors |
| PT3371190T (pt) | 2015-11-06 | 2022-07-08 | Incyte Corp | Compostos heterocíclicos como inibidores de pi3k-gamma |
| ES2833955T3 (es) | 2016-01-05 | 2021-06-16 | Incyte Corp | Piridinas sustituidas con pirazol/imidazol como inhibidores de PI3K-Gamma |
| WO2017223414A1 (en) | 2016-06-24 | 2017-12-28 | Incyte Corporation | HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS |
| US11236128B2 (en) | 2017-07-31 | 2022-02-01 | Agency For Science, Technology And Research | Method of preparing stapled peptides |
| MD3697789T2 (ro) | 2017-10-18 | 2022-02-28 | Incyte Corp | Derivați imidazol condensați substituiți cu grupări hidroxi terțiare ca inhibitori PI3K-GAMA |
| CR20250050A (es) | 2018-09-05 | 2025-03-19 | Incyte Corp | Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165) |
| CN110041349B (zh) * | 2019-05-15 | 2021-06-01 | 湖南科技大学 | 一种含螺二氢嘧啶衍生物及其制备方法和应用 |
| CN117486890A (zh) | 2019-06-06 | 2024-02-02 | 和记黄埔医药（上海）有限公司 | 三环类化合物及其用途 |
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| UA106206C2 (ru) | 2008-06-19 | 2014-08-11 | Милленниум Фармасьютикалз, Инк. | Производные тиофена или тиазола и их применение как ингибиторов pi3k |
| WO2009158374A2 (en) | 2008-06-26 | 2009-12-30 | Smithkline Beecham Corporation | Inhibitors of akt activity |
| GB0812309D0 (en) | 2008-07-03 | 2008-08-13 | Ucb Pharma Sa | Therapeutic agents |
| AU2009268875A1 (en) | 2008-07-09 | 2010-01-14 | Merck Sharp & Dohme Corp. | Inhibitors of janus kinases |
| JP5698666B2 (ja) | 2008-08-04 | 2015-04-08 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | Ｆａａｈの阻害剤として有用なオキサゾール誘導体 |
| US8586582B2 (en) | 2008-11-11 | 2013-11-19 | Xcovery Holding Company, Llc | PI3K/mTOR kinase inhibitors |
| GB0820819D0 (en) | 2008-11-13 | 2008-12-24 | Sareum Ltd | Pharmaceutical compounds |
| WO2010080873A1 (en) | 2009-01-08 | 2010-07-15 | Glaxo Group Limited | Oxazoles as modulators of chemokine receptors |
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| EP2793894A4 (en) | 2011-12-23 | 2015-07-08 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
-
2011
- 2011-10-13 SG SG2013027958A patent/SG189396A1/en unknown
- 2011-10-13 TW TW100137181A patent/TW201307309A/zh unknown
- 2011-10-13 BR BR112013009166A patent/BR112013009166A2/pt not_active IP Right Cessation
- 2011-10-13 WO PCT/US2011/056135 patent/WO2012051410A2/en not_active Ceased
- 2011-10-13 US US13/272,413 patent/US8765746B2/en active Active
- 2011-10-13 UY UY0001033671A patent/UY33671A/es not_active Application Discontinuation
- 2011-10-13 KR KR1020137012227A patent/KR20140091462A/ko not_active Withdrawn
- 2011-10-13 EP EP11833402.8A patent/EP2627181A4/en not_active Withdrawn
- 2011-10-13 JP JP2013534002A patent/JP2013542941A/ja active Pending
- 2011-10-13 AR ARP110103813A patent/AR083450A1/es unknown
- 2011-10-13 CA CA2814688A patent/CA2814688A1/en not_active Abandoned
- 2011-10-13 PE PE2013000845A patent/PE20141044A1/es not_active Application Discontinuation
- 2011-10-13 AU AU2011316016A patent/AU2011316016A1/en not_active Abandoned
- 2011-10-13 MX MX2013004003A patent/MX2013004003A/es not_active Application Discontinuation
- 2011-10-13 CN CN2011800586347A patent/CN103237450A/zh active Pending
- 2011-10-13 EA EA201390539A patent/EA201390539A1/ru unknown
- 2011-10-13 PH PH1/2013/500723A patent/PH12013500723A1/en unknown
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2013
- 2013-04-07 IL IL225607A patent/IL225607A0/en unknown
- 2013-04-12 CL CL2013001009A patent/CL2013001009A1/es unknown
- 2013-04-16 DO DO2013000082A patent/DOP2013000082A/es unknown
- 2013-05-06 MA MA35882A patent/MA34652B1/fr unknown
- 2013-05-08 CR CR20130204A patent/CR20130204A/es unknown
- 2013-05-10 CO CO13117641A patent/CO6801713A2/es not_active Application Discontinuation
- 2013-05-13 EC ECSP13012621 patent/ECSP13012621A/es unknown
-
2014
- 2014-06-27 US US14/318,223 patent/US20150148334A1/en not_active Abandoned
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