JP2011524904A5 - - Google Patents
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- Publication number
- JP2011524904A5 JP2011524904A5 JP2011514600A JP2011514600A JP2011524904A5 JP 2011524904 A5 JP2011524904 A5 JP 2011524904A5 JP 2011514600 A JP2011514600 A JP 2011514600A JP 2011514600 A JP2011514600 A JP 2011514600A JP 2011524904 A5 JP2011524904 A5 JP 2011524904A5
- Authority
- JP
- Japan
- Prior art keywords
- membered
- nitrogen
- 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.)
- Granted
Links
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 46
- 229910052757 nitrogen Inorganic materials 0.000 claims 38
- 229910052717 sulfur Inorganic materials 0.000 claims 35
- 229910052760 oxygen Inorganic materials 0.000 claims 34
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 33
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 33
- 125000005842 heteroatom Chemical group 0.000 claims 33
- 239000001301 oxygen Chemical group 0.000 claims 33
- 239000011593 sulfur Chemical group 0.000 claims 33
- 125000000623 heterocyclic group Chemical group 0.000 claims 20
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000002723 alicyclic group Chemical group 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 125000001931 aliphatic group Chemical group 0.000 claims 12
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 239000012472 biological sample Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 1
- 206010002198 Anaphylactic reaction Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims 1
- 208000006029 Cardiomegaly Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 108091007960 PI3Ks Proteins 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000038016 acute inflammation Diseases 0.000 claims 1
- 230000006022 acute inflammation Effects 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 230000036783 anaphylactic response Effects 0.000 claims 1
- 208000003455 anaphylaxis Diseases 0.000 claims 1
- 230000036772 blood pressure Effects 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 230000006020 chronic inflammation Effects 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 0 CCC(C1)*CCN1c([s]c(-c1nnc[n]1)c1-c(cc2)c(*)cc2Cl)c1C#N Chemical compound CCC(C1)*CCN1c([s]c(-c1nnc[n]1)c1-c(cc2)c(*)cc2Cl)c1C#N 0.000 description 5
- LVQANDFSOGVEHX-UHFFFAOYSA-N CC(C)(C1)OCCN1c([s]c(-c1nnc[nH]1)c1-c(ccc(Cl)c2)c2Cl)c1C#N Chemical compound CC(C)(C1)OCCN1c([s]c(-c1nnc[nH]1)c1-c(ccc(Cl)c2)c2Cl)c1C#N LVQANDFSOGVEHX-UHFFFAOYSA-N 0.000 description 1
- RYONLBOWCIKRIL-UHFFFAOYSA-N CC1(c([s]c(N2CCOCC2)c2C#N)c2-c(ccc(Cl)c2)c2Cl)NC(C)=CCC1=N Chemical compound CC1(c([s]c(N2CCOCC2)c2C#N)c2-c(ccc(Cl)c2)c2Cl)NC(C)=CCC1=N RYONLBOWCIKRIL-UHFFFAOYSA-N 0.000 description 1
- IPQBZBUACCKVJZ-UHFFFAOYSA-N COc1cc(-c2c(C3(N)NC=NC3)[s]c(N3CCOCC3)c2C#N)ccc1 Chemical compound COc1cc(-c2c(C3(N)NC=NC3)[s]c(N3CCOCC3)c2C#N)ccc1 IPQBZBUACCKVJZ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13248408P | 2008-06-19 | 2008-06-19 | |
| US61/132,484 | 2008-06-19 | ||
| PCT/US2009/003607 WO2009154741A1 (en) | 2008-06-19 | 2009-06-17 | Thiophene or thiazole derivatives and their use as pi3k inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011524904A JP2011524904A (ja) | 2011-09-08 |
| JP2011524904A5 true JP2011524904A5 (enExample) | 2012-10-18 |
| JP5596026B2 JP5596026B2 (ja) | 2014-09-24 |
Family
ID=41010579
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011514600A Active JP5596026B2 (ja) | 2008-06-19 | 2009-06-17 | 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 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US8183240B2 (enExample) |
| EP (1) | EP2313399B1 (enExample) |
| JP (1) | JP5596026B2 (enExample) |
| KR (1) | KR20110018451A (enExample) |
| CN (1) | CN102066365A (enExample) |
| AU (1) | AU2009260782B2 (enExample) |
| BR (1) | BRPI0914223A2 (enExample) |
| CA (1) | CA2727069A1 (enExample) |
| CL (1) | CL2010001474A1 (enExample) |
| CO (1) | CO6331431A2 (enExample) |
| CR (1) | CR20110032A (enExample) |
| EA (1) | EA201170052A1 (enExample) |
| ES (1) | ES2491522T3 (enExample) |
| GE (1) | GEP20125650B (enExample) |
| IL (1) | IL210055A0 (enExample) |
| MA (1) | MA32468B1 (enExample) |
| MX (1) | MX2010014125A (enExample) |
| NZ (1) | NZ589844A (enExample) |
| UA (1) | UA106206C2 (enExample) |
| WO (1) | WO2009154741A1 (enExample) |
| ZA (1) | ZA201008875B (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9029411B2 (en) | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| BRPI0914223A2 (pt) * | 2008-06-19 | 2019-09-24 | Millennium Pharm Inc | derivados de tiofeno ou tiazol e seus usos como inibidores de p13k |
| 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 |
| US9139589B2 (en) | 2009-01-30 | 2015-09-22 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2012021611A1 (en) * | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| MA34797B1 (fr) * | 2010-08-11 | 2014-01-02 | Millennium Pharm Inc | Hétéroaryles et leurs utilisations |
| EP2603216A4 (en) * | 2010-08-11 | 2013-12-18 | Millennium Pharm Inc | HETEROARYLE AND USES THEREOF |
| JP5726635B2 (ja) | 2010-08-25 | 2015-06-03 | 株式会社Ｎｔｔドコモ | マルチモードフロントエンド回路 |
| WO2012051410A2 (en) | 2010-10-13 | 2012-04-19 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| CN102503930B (zh) * | 2011-10-28 | 2014-07-02 | 浙江大学 | 3,4,5,-三取代氨基噻吩类化合物及其制备和用途 |
| JP6117235B2 (ja) | 2011-12-15 | 2017-04-19 | ノバルティス アーゲー | Ｐｉ３ｋの活性または機能の阻害剤の使用 |
| UY34539A (es) * | 2011-12-23 | 2013-06-28 | Millennium Pharm Inc | Heteroarilos y usos de los mismos |
| EP2825889A4 (en) | 2012-03-14 | 2015-10-28 | Salk Inst For Biological Studi | ADENOVIRAL TUMOR DIAGNOSIS |
| SG11201507393TA (en) | 2013-03-14 | 2015-10-29 | Salk Inst For Biological Studi | Oncolytic adenovirus compositions |
| RU2015143437A (ru) | 2013-03-15 | 2017-04-27 | Дженентек, Инк. | Способы лечения рака и предотвращения устойчивости к лекарственным препаратам для лечения рака |
| RU2016136091A (ru) * | 2014-02-14 | 2018-03-19 | Дзе Юниверсити Оф Бритиш Коламбиа | Соединения, воздействующие на днк-связывающий домен (dbd) андрогенового рецептора человека, в качестве терапевтических средств, а также способы их применения |
| PL3198009T3 (pl) | 2014-09-24 | 2022-01-24 | Salk Institute For Biological Studies | Onkolityczne wirusy nowotworowe i sposoby zastosowania |
| JP7015551B2 (ja) | 2016-02-23 | 2022-02-15 | ソーク インスティテュート フォー バイオロジカル スタディーズ | ウイルス動態への影響を最小限にするための治療用アデノウイルスにおける外因性遺伝子発現 |
| JP7054527B2 (ja) | 2016-02-23 | 2022-04-14 | ソーク インスティテュート フォー バイオロジカル スタディーズ | アデノウイルスの複製動態を測定するための高スループットアッセイ |
| WO2018111767A1 (en) | 2016-12-12 | 2018-06-21 | Salk Institute For Biological Studies | Tumor-targeting synthetic adenoviruses and uses thereof |
| JP7430395B2 (ja) | 2018-04-09 | 2024-02-13 | ソーク インスティテュート フォー バイオロジカル スタディーズ | 複製特質が増強された腫瘍溶解性アデノウイルス組成物 |
| CA3144848C (en) * | 2019-06-28 | 2023-11-21 | Pfizer Inc. | 5-(thiophen-2-yl)-1h-tetrazole derivatives as bckdk inhibitors useful for treating various diseases |
| CN110759900B (zh) * | 2019-10-25 | 2021-07-30 | 沈阳药科大学 | 噻吩类化合物的制备方法和用途 |
| CN118496197A (zh) | 2019-12-20 | 2024-08-16 | 拜耳公司 | 取代的噻吩甲酰胺、噻吩甲酸及其衍生物 |
| CN113527281B (zh) * | 2020-04-20 | 2023-12-22 | 昆山彭济凯丰生物科技有限公司 | 杂环化合物及其制备方法和应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD275870A1 (de) | 1988-09-27 | 1990-02-07 | Univ Leipzig | Verfahren zur herstellung von in 5-position verschiedenartig substituierten 3-aminothiophen-4-carbonitrilen |
| JP2008503446A (ja) | 2004-05-06 | 2008-02-07 | プレキシコン，インコーポレーテッド | Ｐｄｅ４ｂ阻害剤及びその使用 |
| GB0508472D0 (en) * | 2005-04-26 | 2005-06-01 | Glaxo Group Ltd | Compounds |
| RU2439074C2 (ru) | 2006-04-26 | 2012-01-10 | Ф. Хоффманн-Ля Рош Аг | ПРОИЗВОДНОЕ ТИЕНО[3,2-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТОЛ-3-КИНАЗЫ (РI3К) |
| WO2007129044A1 (en) | 2006-05-03 | 2007-11-15 | Astrazeneca Ab | Thiazole derivatives and their use as anti-tumour agents |
| JP5534811B2 (ja) * | 2006-08-24 | 2014-07-02 | アストラゼネカ アクチボラグ | 増殖性疾患の治療に有用なモルホリノピリミジン誘導体 |
| ES2399774T3 (es) * | 2007-09-24 | 2013-04-03 | Genentech, Inc. | Compuestos de tiazolopirimidina inhibidores de PI3K y métodos de uso |
| US9029411B2 (en) * | 2008-01-25 | 2015-05-12 | Millennium Pharmaceuticals, Inc. | Thiophenes and uses thereof |
| BRPI0914223A2 (pt) * | 2008-06-19 | 2019-09-24 | Millennium Pharm Inc | derivados de tiofeno ou tiazol e seus usos como inibidores de p13k |
-
2009
- 2009-06-17 BR BRPI0914223A patent/BRPI0914223A2/pt not_active IP Right Cessation
- 2009-06-17 US US12/456,455 patent/US8183240B2/en active Active
- 2009-06-17 JP JP2011514600A patent/JP5596026B2/ja active Active
- 2009-06-17 GE GEAP200912065A patent/GEP20125650B/en unknown
- 2009-06-17 WO PCT/US2009/003607 patent/WO2009154741A1/en not_active Ceased
- 2009-06-17 NZ NZ589844A patent/NZ589844A/xx not_active IP Right Cessation
- 2009-06-17 AU AU2009260782A patent/AU2009260782B2/en not_active Ceased
- 2009-06-17 MX MX2010014125A patent/MX2010014125A/es active IP Right Grant
- 2009-06-17 EA EA201170052A patent/EA201170052A1/ru unknown
- 2009-06-17 ES ES09767054.1T patent/ES2491522T3/es active Active
- 2009-06-17 KR KR1020117001175A patent/KR20110018451A/ko not_active Ceased
- 2009-06-17 UA UAA201100563A patent/UA106206C2/ru unknown
- 2009-06-17 CN CN2009801230046A patent/CN102066365A/zh active Pending
- 2009-06-17 EP EP09767054.1A patent/EP2313399B1/en active Active
- 2009-06-17 CA CA2727069A patent/CA2727069A1/en not_active Abandoned
-
2010
- 2010-12-09 ZA ZA2010/08875A patent/ZA201008875B/en unknown
- 2010-12-16 IL IL210055A patent/IL210055A0/en unknown
- 2010-12-17 CL CL2010001474A patent/CL2010001474A1/es unknown
- 2010-12-23 CO CO10161488A patent/CO6331431A2/es active IP Right Grant
-
2011
- 2011-01-13 MA MA33511A patent/MA32468B1/fr unknown
- 2011-01-17 CR CR20110032A patent/CR20110032A/es not_active Application Discontinuation
-
2012
- 2012-04-18 US US13/449,341 patent/US8440664B2/en active Active
-
2013
- 2013-04-01 US US13/854,409 patent/US20130217689A1/en not_active Abandoned
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