JP2014505107A5 - - Google Patents
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- JP2014505107A5 JP2014505107A5 JP2013553557A JP2013553557A JP2014505107A5 JP 2014505107 A5 JP2014505107 A5 JP 2014505107A5 JP 2013553557 A JP2013553557 A JP 2013553557A JP 2013553557 A JP2013553557 A JP 2013553557A JP 2014505107 A5 JP2014505107 A5 JP 2014505107A5
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- JP
- Japan
- Prior art keywords
- hydrogen
- halogen
- syndrome
- use according
- trifluoromethyl
- 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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- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 208000008770 Multiple Hamartoma Syndrome Diseases 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 6
- 201000010917 PTEN hamartoma tumor syndrome Diseases 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 208000002927 Hamartoma Diseases 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 230000035755 proliferation Effects 0.000 claims 3
- 210000004881 tumor cell Anatomy 0.000 claims 3
- 208000012609 Cowden disease Diseases 0.000 claims 2
- 201000002847 Cowden syndrome Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 150000003456 sulfonamides Chemical group 0.000 claims 2
- CWHUFRVAEUJCEF-UHFFFAOYSA-N BKM120 Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2CCOCC2)=NC(N2CCOCC2)=N1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 claims 1
- 208000007531 Proteus syndrome Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
Claims (10)
- ＰＴＥＮ過誤腫性腫瘍症候群を処置する医薬の調製のための、式
- 過誤腫性腫瘍細胞の成長または増殖を阻害するための医薬の調製のための、式
- ＷがＣＨである、請求項１または２のいずれかに記載の使用。
- Ｒ２が水素であり；Ｒ３が水素またはトリフルオロメチルであり；Ｒ４が水素であり；かつＲ６が水素である、請求項１〜３のいずれか１項に記載の使用。
- Ｒ３がトリフルオロメチルである、請求項１〜４のいずれか１項に記載の使用。
- 式（Ｉ）の化合物が４−（トリフルオロメチル）−５−（２，６−ジモルホリノピリミジン−４−イル）ピリジン−２−アミンまたはその医薬的に許容できる塩である、請求項１または２のいずれかに記載の使用。
- ＰＴＥＮ過誤腫性腫瘍症候群を処置する、または過誤腫性腫瘍細胞の成長または増殖を阻害するのに有効な式（Ｉ）の化合物または塩の量が、０．００１から１０００ｍｇ／ｋｇまでの範囲の投与量である、請求項１〜６のいずれか１項に記載の使用。
- ＰＴＥＮ過誤腫性腫瘍症候群を処置する、過誤腫性腫瘍細胞の成長または増殖を阻害するのに有効な式（Ｉ）の化合物または塩の量が、１．０から３０ｍｇ／ｋｇまでの範囲の投与量である、請求項１〜６のいずれか１項に記載の使用。
- ＰＴＥＮ過誤腫性腫瘍症候群が、カウデン症候群、レルミット−デュクロス病、バナヤン−ライリー−ルバルカバ症候群、およびプロテウス症候群からなる群から選択される、請求項１〜８のいずれか１項に記載の使用。
- ＰＴＥＮ過誤腫性腫瘍症候群がカウデン症候群である、請求項９に記載の使用。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161441896P | 2011-02-11 | 2011-02-11 | |
| US61/441,896 | 2011-02-11 | ||
| PCT/US2012/024440 WO2012109423A1 (en) | 2011-02-11 | 2012-02-09 | Method of inhibiting hamartoma tumor cells |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014505107A JP2014505107A (ja) | 2014-02-27 |
| JP2014505107A5 true JP2014505107A5 (ja) | 2015-03-12 |
Family
ID=45809596
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013553557A Withdrawn JP2014505107A (ja) | 2011-02-11 | 2012-02-09 | 過誤腫性腫瘍細胞を阻害する方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20140309221A1 (ja) |
| EP (1) | EP2673268A1 (ja) |
| JP (1) | JP2014505107A (ja) |
| KR (1) | KR20140063509A (ja) |
| CN (1) | CN103476765A (ja) |
| AU (1) | AU2012214413A1 (ja) |
| BR (1) | BR112013020159A2 (ja) |
| CA (1) | CA2826387A1 (ja) |
| MX (1) | MX2013009256A (ja) |
| RU (1) | RU2013141559A (ja) |
| WO (1) | WO2012109423A1 (ja) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| WO2013046136A1 (en) | 2011-09-27 | 2013-04-04 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
| CN103012284A (zh) * | 2012-12-26 | 2013-04-03 | 无锡捷化医药科技有限公司 | 一种2-氨基-5-溴嘧啶类化合物的制备方法 |
| MX355945B (es) | 2013-03-14 | 2018-05-07 | Novartis Ag | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante. |
| CN106458968B (zh) * | 2014-04-22 | 2019-06-25 | 巴塞尔大学 | 三嗪、嘧啶和吡啶衍生物的新制备方法 |
| CN105001151B (zh) * | 2015-08-28 | 2017-07-14 | 苏州明锐医药科技有限公司 | 布帕尼西中间体及其制备方法 |
| WO2017198347A1 (en) * | 2016-05-18 | 2017-11-23 | Piqur Therapeutics Ag | Treatment of skin lesions |
| BR112018073549A8 (pt) | 2016-05-18 | 2023-01-10 | Univ Pennsylvania | Uso de inibidores seletivos e específicos de mtor e/ou de inibidores duplos de pi3k/mtor, e composição farmacêutica |
| CN106905294A (zh) * | 2016-07-08 | 2017-06-30 | 苏州科睿思制药有限公司 | 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法 |
| CN106632443B (zh) * | 2016-11-23 | 2022-06-17 | 山东友帮生化科技有限公司 | 一种2-氨基嘧啶-5-硼酸频哪酯硼酸盐的合成方法 |
| RU2020115351A (ru) * | 2017-11-23 | 2021-12-23 | Пикур Терапьютикс Аг | Лечение кожных заболеваний |
| CN114213340B (zh) | 2022-02-22 | 2022-06-07 | 北京蓝晶微生物科技有限公司 | 2,4-二氨基嘧啶氧化物的制备方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| PL2448927T3 (pl) * | 2009-07-02 | 2014-09-30 | Sanofi Sa | Nowe pochodne (6-okso-1,6-dihydro-pirymidyn-2-ylo)-amidu, ich wytwarzanie i ich zastosowanie farmaceutyczne jako inhibitorów fosforylacji AKT |
-
2012
- 2012-02-09 CN CN201280013673XA patent/CN103476765A/zh active Pending
- 2012-02-09 RU RU2013141559/04A patent/RU2013141559A/ru not_active Application Discontinuation
- 2012-02-09 US US13/984,422 patent/US20140309221A1/en not_active Abandoned
- 2012-02-09 WO PCT/US2012/024440 patent/WO2012109423A1/en active Application Filing
- 2012-02-09 AU AU2012214413A patent/AU2012214413A1/en not_active Abandoned
- 2012-02-09 BR BR112013020159A patent/BR112013020159A2/pt not_active IP Right Cessation
- 2012-02-09 JP JP2013553557A patent/JP2014505107A/ja not_active Withdrawn
- 2012-02-09 EP EP12707171.0A patent/EP2673268A1/en not_active Withdrawn
- 2012-02-09 KR KR1020137023617A patent/KR20140063509A/ko not_active Application Discontinuation
- 2012-02-09 CA CA2826387A patent/CA2826387A1/en not_active Abandoned
- 2012-02-09 MX MX2013009256A patent/MX2013009256A/es not_active Application Discontinuation
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