JP2012500805A5 - - Google Patents
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- Publication number
- JP2012500805A5 JP2012500805A5 JP2011524034A JP2011524034A JP2012500805A5 JP 2012500805 A5 JP2012500805 A5 JP 2012500805A5 JP 2011524034 A JP2011524034 A JP 2011524034A JP 2011524034 A JP2011524034 A JP 2011524034A JP 2012500805 A5 JP2012500805 A5 JP 2012500805A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- pharmaceutically acceptable
- aryl
- heterocyclyl
- 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
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- 150000003839 salts Chemical class 0.000 claims 20
- 125000000623 heterocyclic group Chemical group 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical group 0.000 claims 13
- -1 acetoxy, sulfonylamino Chemical group 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 11
- 125000003107 substituted aryl group Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 150000002431 hydrogen Chemical group 0.000 claims 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000003386 piperidinyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000000547 substituted alkyl group Chemical group 0.000 claims 5
- 150000003857 carboxamides Chemical group 0.000 claims 4
- 125000003725 azepanyl group Chemical group 0.000 claims 3
- 125000002393 azetidinyl group Chemical group 0.000 claims 3
- QYJXLKYOBNZROU-UHFFFAOYSA-N carboxysulfonylformic acid Chemical group OC(=O)S(=O)(=O)C(O)=O QYJXLKYOBNZROU-UHFFFAOYSA-N 0.000 claims 3
- 125000005959 diazepanyl group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 125000006528 (C2-C6) alkyl group Chemical group 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 2
- 125000000676 alkoxyimino group Chemical group 0.000 claims 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 2
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- JAAJQSRLGAYGKZ-UHFFFAOYSA-N 1,2,3,4-tetrahydronaphthalen-1-ol Chemical compound C1=CC=C2C(O)CCCC2=C1 JAAJQSRLGAYGKZ-UHFFFAOYSA-N 0.000 claims 1
- KYNSBQPICQTCGU-UHFFFAOYSA-N Benzopyrane Chemical compound C1=CC=C2C=CCOC2=C1 KYNSBQPICQTCGU-UHFFFAOYSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 125000004619 benzopyranyl group Chemical group O1C(C=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- HPXRVTGHNJAIIH-UHFFFAOYSA-N cyclohexanol Chemical compound OC1CCCCC1 HPXRVTGHNJAIIH-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000006575 electron-withdrawing group Chemical group 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 150000004820 halides Chemical class 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- UHHKSVZZTYJVEG-UHFFFAOYSA-N oxepane Chemical compound C1CCCOCC1 UHHKSVZZTYJVEG-UHFFFAOYSA-N 0.000 claims 1
- 125000003551 oxepanyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- WSDQIHATCCOMLH-UHFFFAOYSA-N phenyl n-(3,5-dichlorophenyl)carbamate Chemical group ClC1=CC(Cl)=CC(NC(=O)OC=2C=CC=CC=2)=C1 WSDQIHATCCOMLH-UHFFFAOYSA-N 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12/196,516 | 2008-08-22 | ||
| US12/196,516 US7902187B2 (en) | 2006-10-04 | 2008-08-22 | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression |
| PCT/US2009/054663 WO2010022358A1 (en) | 2008-08-22 | 2009-08-21 | 6-substituted 2-(benzimidazolyl)purine and purinone derivatives and 6-substituted 2-(imidazoio[4,5- c]pyridinyl)purine and purinone derivatives for immunosuppression |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012500805A JP2012500805A (ja) | 2012-01-12 |
| JP2012500805A5 true JP2012500805A5 (enExample) | 2012-09-27 |
Family
ID=41707479
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011524034A Pending JP2012500805A (ja) | 2008-08-22 | 2009-08-21 | 免疫抑制のための６−置換２−（ベンズイミダゾリル）プリンおよびプリノン誘導体ならびに６−置換２−（イミダゾロ［４，５−ｃ］ピリジニル）プリンおよびプリノン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US7902187B2 (enExample) |
| EP (1) | EP2326647A4 (enExample) |
| JP (1) | JP2012500805A (enExample) |
| CA (1) | CA2735048A1 (enExample) |
| WO (1) | WO2010022358A1 (enExample) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101304748A (zh) * | 2005-08-22 | 2008-11-12 | 加利福尼亚大学董事会 | Tlr激动剂 |
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| UA114496C2 (uk) | 2011-12-02 | 2017-06-26 | Сігнал Фармасьютікалз, Елелсі | ФАРМАЦЕВТИЧНІ КОМПОЗИЦІЇ 7-(6-(2-ГІДРОКСИПРОПАН-2-ІЛ)ПІРИДИН-3-ІЛ)-1-((ТРАНС)-4-МЕТОКСИЦИКЛОГЕКСИЛ)-3,4-ДИГІДРОПІРАЗИНО[2,3-b]ПІРАЗИН-2(1H)-ОНУ, ЇХ ТВЕРДІ ФОРМИ І СПОСОБИ ЇХ ЗАСТОСУВАННЯ |
| CN104271159B (zh) | 2012-02-24 | 2017-11-28 | 西格诺药品有限公司 | 利用tor激酶抑制剂联合治疗来治疗非小细胞肺癌的方法 |
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| JP2016516815A (ja) | 2013-04-17 | 2016-06-09 | シグナル ファーマシューティカルズ，エルエルシー | １−エチル−７−（２−メチル−６−（１Ｈ−１，２，４−トリアゾール−３−イル）ピリジン−３−イル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オンに関する医薬製剤、プロセス、固形形態、及び使用方法 |
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| TWI631949B (zh) | 2013-04-17 | 2018-08-11 | 標誌製藥公司 | 使用ｔｏｒ激酶抑制劑組合療法以治療癌症之方法 |
| BR112015026238A8 (pt) | 2013-04-17 | 2019-12-24 | Signal Pharm Llc | composto dihidropirazino-pirazina, composição farmacêutica que o compreende, uso do composto, métodos para inibir ou medir a fosforilação e para inibir a atividade da proteína quinase, bem como kit |
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| US9512129B2 (en) | 2014-04-16 | 2016-12-06 | Signal Pharmaceuticals, Llc | Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer |
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| US9718824B2 (en) | 2014-04-16 | 2017-08-01 | Signal Pharmaceuticals, Llc | Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof |
| KR20170024120A (ko) | 2014-07-14 | 2017-03-06 | 시그날 파마소티칼 엘엘씨 | 치환된 피롤로피리미딘 화합물을 사용한 암의 치료방법, 이의 조성물 |
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| US10183949B2 (en) | 2014-08-29 | 2019-01-22 | The University Of Tokyo | Pyrimidinone derivative having autotaxin-inhibitory activity |
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-
2008
- 2008-08-22 US US12/196,516 patent/US7902187B2/en active Active
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2009
- 2009-08-21 EP EP09808894A patent/EP2326647A4/en not_active Withdrawn
- 2009-08-21 WO PCT/US2009/054663 patent/WO2010022358A1/en not_active Ceased
- 2009-08-21 JP JP2011524034A patent/JP2012500805A/ja active Pending
- 2009-08-21 CA CA2735048A patent/CA2735048A1/en not_active Abandoned