JP2016505012A5 - - Google Patents
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- Publication number
- JP2016505012A5 JP2016505012A5 JP2015552741A JP2015552741A JP2016505012A5 JP 2016505012 A5 JP2016505012 A5 JP 2016505012A5 JP 2015552741 A JP2015552741 A JP 2015552741A JP 2015552741 A JP2015552741 A JP 2015552741A JP 2016505012 A5 JP2016505012 A5 JP 2016505012A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- ring
- nitrogen
- 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 51
- 150000001875 compounds Chemical class 0.000 claims description 36
- 229910052757 nitrogen Inorganic materials 0.000 claims description 34
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 32
- 229910052760 oxygen Inorganic materials 0.000 claims description 32
- 239000001301 oxygen Chemical group 0.000 claims description 32
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 30
- 125000005842 heteroatom Chemical group 0.000 claims description 30
- 229910052717 sulfur Chemical group 0.000 claims description 30
- 239000011593 sulfur Chemical group 0.000 claims description 30
- 150000003839 salts Chemical class 0.000 claims description 28
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 17
- 229920006395 saturated elastomer Polymers 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 14
- 125000004429 atom Chemical group 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- 125000001931 aliphatic group Chemical group 0.000 claims description 6
- 125000002619 bicyclic group Chemical group 0.000 claims description 6
- 125000002837 carbocyclic group Chemical group 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 4
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims description 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 229910052739 hydrogen Inorganic materials 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 125000001841 imino group Chemical group [H]N=* 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 2
- 102100036342 Interleukin-1 receptor-associated kinase 1 Human genes 0.000 description 3
- 101710199015 Interleukin-1 receptor-associated kinase 1 Proteins 0.000 description 3
- 0 C*c1nc(NC)nc2c1c(CCCCCC1)c1[s]2 Chemical compound C*c1nc(NC)nc2c1c(CCCCCC1)c1[s]2 0.000 description 2
- SOKVXDGWLKVBLA-SAABIXHNSA-N CN(C)[C@H]1CC[C@H](CNc2c(c(CCC3)c3[s]3)c3nc(Nc3ccccc3)n2)CC1 Chemical compound CN(C)[C@H]1CC[C@H](CNc2c(c(CCC3)c3[s]3)c3nc(Nc3ccccc3)n2)CC1 SOKVXDGWLKVBLA-SAABIXHNSA-N 0.000 description 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361751000P | 2013-01-10 | 2013-01-10 | |
| US61/751,000 | 2013-01-10 | ||
| PCT/US2014/010652 WO2014110114A1 (en) | 2013-01-10 | 2014-01-08 | Irak inhibitors and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016505012A JP2016505012A (ja) | 2016-02-18 |
| JP2016505012A5 true JP2016505012A5 (enExample) | 2017-02-09 |
Family
ID=51061425
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015552741A Pending JP2016505012A (ja) | 2013-01-10 | 2014-01-08 | Irak阻害剤およびその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US9175007B2 (enExample) |
| EP (1) | EP2943202A4 (enExample) |
| JP (1) | JP2016505012A (enExample) |
| CN (1) | CN105142639A (enExample) |
| AU (1) | AU2014205577A1 (enExample) |
| BR (1) | BR112015014034A2 (enExample) |
| CA (1) | CA2890911A1 (enExample) |
| HK (1) | HK1216859A1 (enExample) |
| WO (1) | WO2014110114A1 (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ772688A (en) | 2010-06-03 | 2022-09-30 | Pharmacyclics Llc | The use of inhibitors of bruton’s tyrosine kinase (btk) |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| HK1210696A1 (en) | 2012-07-11 | 2016-05-06 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| AU2013293087B2 (en) | 2012-07-24 | 2017-08-31 | Pharmacyclics Llc | Mutations associated with resistance to inhibitors of Bruton's tyrosine kinase (BTK) |
| WO2014110114A1 (en) * | 2013-01-10 | 2014-07-17 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2015048281A1 (en) | 2013-09-27 | 2015-04-02 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| US9751888B2 (en) | 2013-10-04 | 2017-09-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| PE20160685A1 (es) | 2013-10-04 | 2016-07-23 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos y usos de los mismos |
| SG10201808053XA (en) | 2014-03-19 | 2018-10-30 | Infinity Pharmaceuticals Inc | Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders |
| CA2942528A1 (en) | 2014-03-20 | 2015-09-24 | Pharmacyclics Inc. | Phospholipase c gamma 2 and resistance associated mutations |
| SG11201700774UA (en) * | 2014-08-01 | 2017-02-27 | Pharmacyclics Llc | Biomarkers for predicting response of dlbcl to treatment with a btk inhibitor |
| US9708348B2 (en) | 2014-10-03 | 2017-07-18 | Infinity Pharmaceuticals, Inc. | Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof |
| WO2017004133A1 (en) * | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CN107531710B (zh) * | 2015-08-13 | 2020-02-14 | 北京韩美药品有限公司 | Irak4抑制剂及其应用 |
| US10160761B2 (en) | 2015-09-14 | 2018-12-25 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones, and process of making, composition comprising, and methods of using the same |
| WO2017161116A1 (en) | 2016-03-17 | 2017-09-21 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors |
| US10919914B2 (en) | 2016-06-08 | 2021-02-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| WO2018077385A1 (en) * | 2016-10-25 | 2018-05-03 | Biontech Rna Pharmaceuticals Gmbh | Dose determination for immunotherapeutic agents |
| TWI733982B (zh) | 2017-02-16 | 2021-07-21 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒衍生物 |
| WO2019001461A1 (zh) * | 2017-06-27 | 2019-01-03 | 南京明德新药研发股份有限公司 | Irak4抑制剂 |
| CN111032642B (zh) * | 2017-06-29 | 2023-07-18 | 里格尔药品股份有限公司 | 激酶抑制剂及制造和使用方法 |
| JP7377207B2 (ja) * | 2018-01-29 | 2023-11-09 | メルク パテント ゲーエムベーハー | Gcn2阻害剤およびその使用 |
| TWI721483B (zh) | 2018-07-13 | 2021-03-11 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒𠯤衍生物 |
| KR102329235B1 (ko) * | 2018-11-21 | 2021-11-22 | 한국화학연구원 | Irak4 저해제로서 신규의 삼중고리 화합물 |
| JP7623943B2 (ja) * | 2018-11-30 | 2025-01-29 | カイメラ セラピューティクス, インコーポレイテッド | Irak分解剤およびそれらの使用 |
| US20220252574A1 (en) * | 2019-07-22 | 2022-08-11 | University Of Louisville Research Foundation, Inc. | Immunomodulatory compositions and methods of using |
| CN116867494A (zh) | 2021-02-15 | 2023-10-10 | 凯麦拉医疗公司 | Irak4降解剂和其用途 |
| WO2023075479A1 (ko) * | 2021-10-28 | 2023-05-04 | 재단법인 대구경북첨단의료산업진흥재단 | 신규한 티에노[2,3-d]피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암 또는 자가면역질환의 예방 또는 치료용 약학적 조성물 |
| US12384775B2 (en) | 2022-03-23 | 2025-08-12 | Rigel Pharmaceuticals, Inc. | Pyrimid-2-yl-pyrazole compounds as IRAK inhibitors |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1937459A1 (de) | 1968-08-02 | 1970-02-05 | Ciba Geigy | Neue Pyrimidinderivate und Verfahren zu ihrer Herstellung |
| US5948911A (en) | 1998-11-20 | 1999-09-07 | Cell Pathways, Inc. | Method for inhibiting neoplastic cells and related conditions by exposure to thienopyrimidine derivatives |
| EP1167367A4 (en) | 1999-03-30 | 2002-04-24 | Nippon Soda Co | THIENOPYRIMIDINE COMPOUNDS AND SALTS THEREOF, AND PROCESS FOR THE PREPARATION THEREOF |
| US6297238B1 (en) | 1999-04-06 | 2001-10-02 | Basf Aktiengesellschaft | Therapeutic agents |
| US6680322B2 (en) | 1999-12-02 | 2004-01-20 | Osi Pharmaceuticals, Inc. | Compounds specific to adenosine A1 receptors and uses thereof |
| CN101100472A (zh) * | 2001-04-30 | 2008-01-09 | 美国拜尔公司 | 4-氨基-5,6-取代的噻吩并[2,3-d]嘧啶化合物及其应用 |
| AU2002360774A1 (en) | 2001-12-28 | 2003-07-24 | Bayer Corporation | 4-substituted fused heteropyrimidines and fused hetero-4-pyrimidones |
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| AU2003270701B2 (en) | 2002-10-31 | 2009-11-12 | Amgen Inc. | Antiinflammation agents |
| NZ542236A (en) | 2003-03-31 | 2008-05-30 | Predix Pharmaceuticals Holding | New piperidinylamino-thieno[2,3-d]pyrimidine compounds |
| US7977366B2 (en) | 2003-10-14 | 2011-07-12 | Cornell Research Foundation, Inc. | Treating an inflammatory disorder or inhibiting respiratory burst in adherent neutrophils with chemical inhibitors of neutrophil activation |
| US7598259B2 (en) | 2004-06-15 | 2009-10-06 | Schering Corporation | mGluR1 antagonists as therapeutic agents |
| WO2006010567A1 (de) | 2004-07-23 | 2006-02-02 | Curacyte Discovery Gmbh | INHIBITOREN DER PHOSPHODIESTERASE 4 UND TNFα-FREISETZUNG |
| WO2006081072A1 (en) | 2005-01-24 | 2006-08-03 | Abbott Laboratories | Antagonists of the mglu receptor and uses thereof |
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| WO2007032854A1 (en) | 2005-08-19 | 2007-03-22 | Schering Corporation | FUSED TRICYCLIC mGluR1 ANTAGONISTS AS THERAPEUTIC AGENTS |
| US7595324B2 (en) | 2006-11-09 | 2009-09-29 | Ardea Biosciences, Inc. | Substituted thieno[3,2-D]pyrimidines as HIV inhibitors |
| US8642660B2 (en) | 2007-12-21 | 2014-02-04 | The University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
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| US8993552B2 (en) | 2009-09-04 | 2015-03-31 | The Regents Of The University Of Michigan | Compositions and methods for treatment of leukemia |
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| CN102985426B (zh) | 2010-07-13 | 2015-10-07 | 弗·哈夫曼-拉罗切有限公司 | 作为irak4调节剂的吡唑并[1,5a]嘧啶和噻吩并[3,2b]嘧啶衍生物 |
| EP2595993B1 (en) | 2010-07-23 | 2018-04-18 | President and Fellows of Harvard College | Tricyclic proteasome activity enhancing compounds |
| EP2663312B1 (en) | 2011-01-10 | 2017-10-11 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CA2855446C (en) | 2011-11-23 | 2021-04-20 | Cancer Research Technology Limited | Thienopyrimidine inhibitors of atypical protein kinase c |
| CN104582705A (zh) | 2012-01-10 | 2015-04-29 | 林伯士艾瑞斯公司 | 白介素-1受体相关激酶(irak)抑制剂和其用途 |
| WO2014011911A2 (en) | 2012-07-11 | 2014-01-16 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| HK1210696A1 (en) * | 2012-07-11 | 2016-05-06 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CN104902959A (zh) | 2012-07-11 | 2015-09-09 | 林伯士艾瑞斯公司 | Irak抑制剂和其用途 |
| WO2014110114A1 (en) * | 2013-01-10 | 2014-07-17 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2014194242A2 (en) * | 2013-05-31 | 2014-12-04 | Nimbus Iris, Inc. | Flt3 inhibitors and uses thereof |
| WO2014194201A2 (en) * | 2013-05-31 | 2014-12-04 | Nimbus Iris, Inc. | Cdk8 inhibitors and uses thereof |
-
2014
- 2014-01-08 WO PCT/US2014/010652 patent/WO2014110114A1/en not_active Ceased
- 2014-01-08 CN CN201480003428.XA patent/CN105142639A/zh active Pending
- 2014-01-08 US US14/150,230 patent/US9175007B2/en not_active Expired - Fee Related
- 2014-01-08 CA CA2890911A patent/CA2890911A1/en not_active Abandoned
- 2014-01-08 HK HK16104934.3A patent/HK1216859A1/zh unknown
- 2014-01-08 AU AU2014205577A patent/AU2014205577A1/en not_active Abandoned
- 2014-01-08 BR BR112015014034A patent/BR112015014034A2/pt not_active IP Right Cessation
- 2014-01-08 JP JP2015552741A patent/JP2016505012A/ja active Pending
- 2014-01-08 EP EP14737658.6A patent/EP2943202A4/en not_active Withdrawn
-
2015
- 2015-09-17 US US14/857,029 patent/US9751892B2/en not_active Expired - Fee Related
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