JP2016505012A5 - - Google Patents
Download PDFInfo
- 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 |
|---|---|---|---|---|
| MX380504B (es) | 2010-06-03 | 2025-03-12 | Pharmacyclics Llc | El uso de inhibidores de la tirosina quinasa de bruton (btk). |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| EP2872144A4 (en) | 2012-07-11 | 2015-12-02 | Nimbus Iris Inc | IRAQ INHIBITOR AND USES THEREOF |
| HK1206073A1 (en) | 2012-07-24 | 2015-12-31 | 药品循环有限责任公司 | 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 |
| EP3049086A4 (en) | 2013-09-27 | 2017-02-22 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| EP3964507A1 (en) | 2013-10-04 | 2022-03-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| WO2015051241A1 (en) | 2013-10-04 | 2015-04-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN106456628A (zh) | 2014-03-19 | 2017-02-22 | 无限药品股份有限公司 | 用于治疗PI3K‑γ介导的障碍的杂环化合物 |
| US9885086B2 (en) | 2014-03-20 | 2018-02-06 | Pharmacyclics Llc | Phospholipase C gamma 2 and resistance associated mutations |
| BR112017001677A2 (pt) * | 2014-08-01 | 2018-07-17 | Pharmacyclics Llc | biomarcadores para predizer resposta de dlbcl ao tratamento com um inibidor de btk |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| WO2017004133A1 (en) * | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| KR102048719B1 (ko) * | 2015-08-13 | 2019-11-26 | 베이징 한미 파마슈티컬 컴퍼니 리미티드 | Irak4억제제 및 이의 용도 |
| CN114230571B (zh) | 2015-09-14 | 2025-07-08 | 无限药品股份有限公司 | 异喹啉酮的固体形式、其制备方法、包含其的组合物及其使用方法 |
| 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 |
| TW202340194A (zh) | 2017-02-16 | 2023-10-16 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒𠯤衍生物 |
| 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 |
| JP7167069B2 (ja) * | 2017-06-29 | 2022-11-08 | ライジェル ファーマシューティカルズ， インコーポレイテッド | キナーゼ阻害剤ならびに作製および使用のための方法 |
| AU2019212969B2 (en) * | 2018-01-29 | 2025-01-23 | Merck Patent Gmbh | GCN2 inhibitors and uses thereof |
| 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 |
| AU2019389174A1 (en) * | 2018-11-30 | 2021-07-01 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| US20220252574A1 (en) * | 2019-07-22 | 2022-08-11 | University Of Louisville Research Foundation, Inc. | Immunomodulatory compositions and methods of using |
| MX2023009178A (es) | 2021-02-15 | 2023-08-21 | Kymera Therapeutics Inc | Degradadores de la cinasa 4 asociada al receptor de interleucina 1 (irak4) y usos de los mismos. |
| 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 |
| ES3075943T3 (en) | 2022-03-23 | 2026-08-10 | 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 |
| CA2365578A1 (en) | 1999-03-30 | 2000-10-12 | Seiichi Uchida | Thienopyrimidine compounds and salts thereof and process for the preparation of the same |
| 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 |
| WO2003057149A2 (en) | 2001-12-28 | 2003-07-17 | Bayer Corporation | 4-substituted fused heteropyrimidines and fused hetero-4-pyrimidones |
| US20030225098A1 (en) | 2002-03-21 | 2003-12-04 | Hirst Gavin C. | Kinase inhibitors |
| EP1556053A4 (en) | 2002-10-31 | 2006-04-19 | Amgen Inc | ANTI-INFLAMMATORY AGENTS |
| BRPI0408988A (pt) | 2003-03-31 | 2006-03-28 | Predix Pharmaceuticals Holding | composto de piperidinilamino-tieno[2,3-d]pirimidina |
| WO2005037213A2 (en) | 2003-10-14 | 2005-04-28 | Cornell Research Foundation, Inc. | Antiinflammatory inhibitors of respiratory burst in adherent neutrophils |
| US7598259B2 (en) | 2004-06-15 | 2009-10-06 | Schering Corporation | mGluR1 antagonists as therapeutic agents |
| ATE455777T1 (de) | 2004-07-23 | 2010-02-15 | Medicines Co Leipzig Gmbh | Substituierte pyridoä3',2':4,5üthienoä3,2- düpyrimidine und pyridoä3',2':4,5üfuroä3,2-dü- pyrimidine zur verwendung als inhibitoren der pda-4 und/oder tnf-alpha freisetzung |
| WO2006081072A1 (en) | 2005-01-24 | 2006-08-03 | Abbott Laboratories | Antagonists of the mglu receptor and uses thereof |
| AU2006261082B2 (en) | 2005-06-22 | 2012-04-19 | Boehringer Ingelheim International Gmbh | Thienopyrimidines for pharmaceutical compositions |
| JP2009504752A (ja) | 2005-08-19 | 2009-02-05 | シェーリング コーポレイション | 治療剤としての縮合三環式ｍＧｌｕＲ１アンタゴニスト |
| ATE516292T1 (de) | 2005-08-19 | 2011-07-15 | Schering Corp | Kondensierte tricyclische mglur1-antagonisten als therapeutische mittel |
| EP2132211A4 (en) * | 2006-11-09 | 2011-12-07 | Ardea Biosciences Inc | 4-CYANPHENYLAMINO-SUBSTITUTED BICYCLIC AND HETEROCYCLIC COMPOUNDS AS AN HIV HEMMER |
| AU2008345225A1 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| US20100227853A1 (en) | 2008-04-18 | 2010-09-09 | Trustees Of Boston College | Inhibitors of cyclic amp phosphodiesterases |
| AR073739A1 (es) | 2008-09-10 | 2010-12-01 | Kalypsys Inc | Aminopirimidinas como inhibidores de los receptores de histamina |
| AU2010289321A1 (en) | 2009-09-04 | 2012-04-05 | The Regents Of The University Of Michigan | Compositions and methods for treatment of leukemia |
| CA2783701A1 (en) | 2009-12-10 | 2011-06-16 | The University Of North Carolina At Chapel Hill | Selective beta-glucuronidase inhibitors as a treatment for side effects of camptothecin antineoplastic agents |
| JP5985473B2 (ja) | 2010-07-13 | 2016-09-06 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体 |
| CN103119047B (zh) | 2010-07-23 | 2016-06-15 | 哈佛大学校长及研究员协会 | 三环类蛋白酶体活性增强化合物 |
| EP3239154A1 (en) | 2011-01-10 | 2017-11-01 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| IN2014CN04558A (enExample) | 2011-11-23 | 2015-09-18 | Cancer Rec Tech Ltd | |
| TW201728592A (zh) * | 2012-01-10 | 2017-08-16 | 林伯士艾瑞斯公司 | Ｉｒａｋ抑制劑及其用途 |
| WO2014011911A2 (en) | 2012-07-11 | 2014-01-16 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| HK1210732A1 (en) | 2012-07-11 | 2016-05-06 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| EP2872144A4 (en) | 2012-07-11 | 2015-12-02 | Nimbus Iris Inc | IRAQ INHIBITOR AND USES THEREOF |
| WO2014110114A1 (en) * | 2013-01-10 | 2014-07-17 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2014194245A2 (en) * | 2013-05-31 | 2014-12-04 | Nimbus Iris, Inc. | Cdk8 inhibitors and uses thereof |
| WO2014194242A2 (en) * | 2013-05-31 | 2014-12-04 | Nimbus Iris, Inc. | Flt3 inhibitors and uses thereof |
-
2014
- 2014-01-08 WO PCT/US2014/010652 patent/WO2014110114A1/en not_active Ceased
- 2014-01-08 AU AU2014205577A patent/AU2014205577A1/en not_active Abandoned
- 2014-01-08 JP JP2015552741A patent/JP2016505012A/ja active Pending
- 2014-01-08 CA CA2890911A patent/CA2890911A1/en not_active Abandoned
- 2014-01-08 CN CN201480003428.XA patent/CN105142639A/zh active Pending
- 2014-01-08 BR BR112015014034A patent/BR112015014034A2/pt not_active IP Right Cessation
- 2014-01-08 EP EP14737658.6A patent/EP2943202A4/en not_active Withdrawn
- 2014-01-08 HK HK16104934.3A patent/HK1216859A1/zh unknown
- 2014-01-08 US US14/150,230 patent/US9175007B2/en not_active Expired - Fee Related
-
2015
- 2015-09-17 US US14/857,029 patent/US9751892B2/en not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2016519078A5 (enExample) | ||
| RU2350605C2 (ru) | Аналоги хиназолина в качестве ингибиторов рецепторных тирозинкиназ | |
| PE20190811A1 (es) | Derivados de pirazolopirimidinas como inhibidor de quinasa | |
| AR038914A1 (es) | Indazoles substituidos, composiciones que los contienen, procedimiento de fabricacion y utilizacion para fabricar un medicamento | |
| NZ630457A (en) | Compounds useful as inhibitors of atr kinase | |
| CY1111702T1 (el) | Τα παραγωγα ινδολης ως αγωνιστες υποδοχεων s1p1 | |
| EA201890888A1 (ru) | Новые спиро[3h-индол-3,2'-пирролидин]-2(1h)-оновые соединения и производные в качестве ингибиторов mdm2-p53 | |
| JP2017506675A5 (enExample) | ||
| PE20090556A1 (es) | DERIVADOS DE 6-CICLOAMINO-3-(PIRIDIN-4-IL) IMIDAZO [1,2-b]-PIRIDAZINA COMO INHIBIDORES DE CASEINA QUINASAS Y SU PREPARACION | |
| TW200612895A (en) | Bis(thio-hydrazide amide) salts for treatment of cancers | |
| PE20141553A1 (es) | Compuestos de triazolopiridina como inhibidores de la ped10a | |
| JP2016530283A5 (enExample) | ||
| JP2015143283A5 (enExample) | ||
| DE602004002087D1 (de) | Bis(thio-hydrazid amid) verbindungen zur behandlung von mehrfach resistenten krebs | |
| AR046600A1 (es) | Diazaespiroalcanos y su uso como tratamiento para enfermedades mediadas por ccr8 | |
| NI201000145A (es) | DERIVADOS DE IMIDAZO - [1, 2-b] - PIRIDAZINA PARA EL TRATAMIENTO DE ENFERMEDAD MEDIADA POR CINASA DE TIROSINA C-MET. | |
| JP2006523238A5 (enExample) | ||
| ECSP13012852A (es) | Derivados de 6-ciclobutil-1,5-dihidro-pirazolo [3,4-d]pirimidin-4-ona y su uso como inhibidores de pde9a. | |
| JP2023520330A5 (enExample) | ||
| CY1122514T1 (el) | Σουλφονικος υδροξυαιθυλεστερας του αναστολεα της εξαρτωμενης απο κυκλινη πρωτεϊνικης κινασης, κρυσταλλικη μορφη αυτου και μεθοδος παρασκευης αυτου | |
| AR061583A1 (es) | Acidos 6-(bencilo sustituido con heterociclil)-4-oxiquinolin carboxilicos, inhibidores de vih-integrasas, composiciones farmaceuticas que los contienen y usos como agentes anti-vih. | |
| JP2014509600A5 (enExample) | ||
| MX2021013576A (es) | Compuesto utilizado como inhibidor de la quinasa y aplicación del mismo. | |
| RU2014152790A (ru) | Пирролопиразоновые ингибиторы танкиразы | |
| AR072809A1 (es) | Compuesto de (3- piridinilcarbonil)-4-(fenilsulfonilpiperazina ), su uso para la elaboracion de unmedicamento para el tratamiento del dolor y composicion farmaceutica que lo comprende |