JP2015515989A5 - - Google Patents
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- JP2015515989A5 JP2015515989A5 JP2015510483A JP2015510483A JP2015515989A5 JP 2015515989 A5 JP2015515989 A5 JP 2015515989A5 JP 2015510483 A JP2015510483 A JP 2015510483A JP 2015510483 A JP2015510483 A JP 2015510483A JP 2015515989 A5 JP2015515989 A5 JP 2015515989A5
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- alkyl
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- aryl
- compound
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 84
- 125000006545 (C1-C9) alkyl group Chemical group 0.000 claims description 47
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 47
- 125000000217 alkyl group Chemical group 0.000 claims description 46
- 125000001424 substituent group Chemical group 0.000 claims description 42
- 125000003118 aryl group Chemical group 0.000 claims description 39
- 150000004820 halides Chemical class 0.000 claims description 38
- 125000000623 heterocyclic group Chemical group 0.000 claims description 35
- 201000010099 disease Diseases 0.000 claims description 24
- 208000035475 disorder Diseases 0.000 claims description 23
- 150000003839 salts Chemical class 0.000 claims description 23
- PIGFYZPCRLYGLF-UHFFFAOYSA-N Aluminum nitride Chemical compound [Al]#N PIGFYZPCRLYGLF-UHFFFAOYSA-N 0.000 claims description 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 22
- 125000001072 heteroaryl group Chemical group 0.000 claims description 20
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 12
- 102000013814 Wnt Human genes 0.000 claims description 8
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- 229910052731 fluorine Inorganic materials 0.000 claims description 8
- 125000001153 fluoro group Chemical group F* 0.000 claims description 7
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 6
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 5
- 230000002159 abnormal effect Effects 0.000 claims description 5
- 125000004193 piperazinyl group Chemical group 0.000 claims description 5
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- 125000004429 atom Chemical group 0.000 claims description 4
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- 125000002541 furyl group Chemical group 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 230000011664 signaling Effects 0.000 claims description 4
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- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
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- 0 *c1c(*)ncc2c1nc(-c(c1c3)n[n]c1ncc3-c1c(*)*(*)c(*)nc1)[n]2 Chemical compound *c1c(*)ncc2c1nc(-c(c1c3)n[n]c1ncc3-c1c(*)*(*)c(*)nc1)[n]2 0.000 description 4
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- GHVDUYGLIBYHHD-UHFFFAOYSA-O C(C1CCCC1)NCc1cc(-c(cc23)c[nH+]c2[nH]nc3-c2nc3ccncc3[nH]2)cnc1 Chemical compound C(C1CCCC1)NCc1cc(-c(cc23)c[nH+]c2[nH]nc3-c2nc3ccncc3[nH]2)cnc1 GHVDUYGLIBYHHD-UHFFFAOYSA-O 0.000 description 1
- ADENEOMUUQJZFH-UHFFFAOYSA-N C(c1ccccc1)NCc1cc(-c2cc(c(-c3nc(ccnc4)c4[nH]3)n[nH]3)c3nc2)cnc1 Chemical compound C(c1ccccc1)NCc1cc(-c2cc(c(-c3nc(ccnc4)c4[nH]3)n[nH]3)c3nc2)cnc1 ADENEOMUUQJZFH-UHFFFAOYSA-N 0.000 description 1
- LQGMKRPMUWLRKC-YFVJMOTDSA-N CCCCC(N/C(/C)=C/C(/c(cc12)cnc1[nH]nc2[IH]1=Nc(ccnc2)c2N1)=C\N=C)=O Chemical compound CCCCC(N/C(/C)=C/C(/c(cc12)cnc1[nH]nc2[IH]1=Nc(ccnc2)c2N1)=C\N=C)=O LQGMKRPMUWLRKC-YFVJMOTDSA-N 0.000 description 1
- 208000026010 Caudal duplication Diseases 0.000 description 1
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- 101000814371 Homo sapiens Protein Wnt-10a Proteins 0.000 description 1
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- 101000650119 Homo sapiens Protein Wnt-9b Proteins 0.000 description 1
- 101000781955 Homo sapiens Proto-oncogene Wnt-1 Proteins 0.000 description 1
- 101000954762 Homo sapiens Proto-oncogene Wnt-3 Proteins 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
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- 206010049422 Precancerous skin lesion Diseases 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 102100039461 Protein Wnt-10a Human genes 0.000 description 1
- 102100029062 Protein Wnt-10b Human genes 0.000 description 1
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- 102100035289 Protein Wnt-2b Human genes 0.000 description 1
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- 206010047486 Virilism Diseases 0.000 description 1
- 101150010310 WNT-4 gene Proteins 0.000 description 1
- 101150019524 WNT2 gene Proteins 0.000 description 1
- 208000008383 Wilms tumor Diseases 0.000 description 1
- 102000052547 Wnt-1 Human genes 0.000 description 1
- 102000052556 Wnt-2 Human genes 0.000 description 1
- 108700020986 Wnt-2 Proteins 0.000 description 1
- 102000052549 Wnt-3 Human genes 0.000 description 1
- 102000052548 Wnt-4 Human genes 0.000 description 1
- 108700020984 Wnt-4 Proteins 0.000 description 1
- 102000043366 Wnt-5a Human genes 0.000 description 1
- 102000044880 Wnt3A Human genes 0.000 description 1
- 108700013515 Wnt3A Proteins 0.000 description 1
- 210000001766 X chromosome Anatomy 0.000 description 1
- 101100485099 Xenopus laevis wnt2b-b gene Proteins 0.000 description 1
- 201000006288 alpha thalassemia Diseases 0.000 description 1
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- 230000000112 colonic effect Effects 0.000 description 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261642915P | 2012-05-04 | 2012-05-04 | |
| US61/642,915 | 2012-05-04 | ||
| PCT/US2013/039484 WO2013166396A2 (en) | 2012-05-04 | 2013-05-03 | 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017173614A Division JP6378409B2 (ja) | 2012-05-04 | 2017-09-11 | １Ｈ−ピラゾロ［３，４−ｂ］ピリジンおよびそれらの治療的使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015515989A JP2015515989A (ja) | 2015-06-04 |
| JP2015515989A5 true JP2015515989A5 (enExample) | 2016-06-23 |
| JP6209593B2 JP6209593B2 (ja) | 2017-10-04 |
Family
ID=49513001
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015510483A Active JP6209593B2 (ja) | 2012-05-04 | 2013-05-03 | １Ｈ−ピラゾロ［３，４−ｂ］ピリジンおよびそれらの治療的使用 |
| JP2017173614A Expired - Fee Related JP6378409B2 (ja) | 2012-05-04 | 2017-09-11 | １Ｈ−ピラゾロ［３，４−ｂ］ピリジンおよびそれらの治療的使用 |
| JP2018139863A Pending JP2018162323A (ja) | 2012-05-04 | 2018-07-26 | １Ｈ−ピラゾロ［３，４−ｂ］ピリジンおよびそれらの治療的使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017173614A Expired - Fee Related JP6378409B2 (ja) | 2012-05-04 | 2017-09-11 | １Ｈ−ピラゾロ［３，４−ｂ］ピリジンおよびそれらの治療的使用 |
| JP2018139863A Pending JP2018162323A (ja) | 2012-05-04 | 2018-07-26 | １Ｈ−ピラゾロ［３，４−ｂ］ピリジンおよびそれらの治療的使用 |
Country Status (33)
Families Citing this family (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2835553T3 (es) | 2009-08-10 | 2021-06-22 | Biosplice Therapeutics Inc | Inhibidores de indazol de la vía de señalización de Wnt y sus usos terapéuticos |
| CN102821607B (zh) | 2009-12-21 | 2014-12-17 | 萨穆梅德有限公司 | 1H-吡唑并[3，4-b]吡啶及其治疗应用 |
| WO2012177647A2 (en) | 2011-06-20 | 2012-12-27 | Kerry Lane | Mycotoxin diagnostics and methods thereof |
| HRP20190281T1 (hr) | 2011-09-14 | 2019-05-31 | Samumed, Llc | Indazol-3-karboksamidi i njihova uporaba kao inhibitora signalizacijskog puta wnt/b-katenin |
| PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| PL2770994T3 (pl) * | 2012-05-04 | 2020-03-31 | Samumed, Llc | 1H-Pirazolo[3,4-b]pirydyny i ich zastosowania terapeutyczne |
| EP2943198B1 (en) | 2013-01-08 | 2019-07-17 | Samumed, LLC | 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof |
| WO2015089192A1 (en) | 2013-12-11 | 2015-06-18 | Quanticel Pharmaceuticals, Inc. | Inhibitors of lysine specific demethylase-1 |
| CA2943659C (en) * | 2014-03-27 | 2023-04-25 | Merck Patent Gmbh | Pyridyl piperidines |
| WO2016040181A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040193A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040184A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040180A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040182A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof |
| WO2016040190A1 (en) * | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040185A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof |
| WO2016040188A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| US10231956B2 (en) | 2015-08-03 | 2019-03-19 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017024010A1 (en) * | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| WO2017023987A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| US10350199B2 (en) | 2015-08-03 | 2019-07-16 | Samumed, Llc | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| WO2017023972A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10206909B2 (en) | 2015-08-03 | 2019-02-19 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10166218B2 (en) | 2015-08-03 | 2019-01-01 | Samumed, Llc | 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| US10188634B2 (en) | 2015-08-03 | 2019-01-29 | Samumed, Llc | 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10285982B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| WO2017023984A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| US10519169B2 (en) | 2015-08-03 | 2019-12-31 | Samumed, Llc | 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017024015A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017023993A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017023986A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof |
| WO2017023975A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| US10285983B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof |
| US10392383B2 (en) | 2015-08-03 | 2019-08-27 | Samumed, Llc | 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| KR20180080262A (ko) * | 2015-11-06 | 2018-07-11 | 사뮤메드, 엘엘씨 | 골관절염의 치료 |
| ES2933109T3 (es) | 2016-06-01 | 2023-02-02 | Biosplice Therapeutics Inc | Proceso para preparar N-(5-(3-(7-(3-fluorofenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida |
| CN110709082A (zh) | 2016-10-21 | 2020-01-17 | 萨穆梅德有限公司 | 吲唑-3-甲酰胺的使用方法及其作为Wnt/β-连环蛋白信号传导途径抑制剂的用途 |
| KR102558716B1 (ko) | 2016-11-07 | 2023-07-21 | 사뮤메드, 엘엘씨 | 단일-투여량, 즉시-사용가능한 주사용 제제 |
| EP3644984A1 (en) | 2017-06-26 | 2020-05-06 | The Regents of the University of Colorado, a body corporate | Biomarkers for the diagnosis and treatment of fibrotic lung disease |
| AU2018375719A1 (en) * | 2017-11-29 | 2020-05-28 | Board Of Regents Of The University Of Texas System | Compositions and methods for cancer therapy |
| WO2019241540A1 (en) | 2018-06-15 | 2019-12-19 | Samumed, Llc | Indazole containing macrocycles and therapeutic uses thereof |
| EP3911317A2 (en) | 2019-01-17 | 2021-11-24 | BioSplice Therapeutics, Inc. | Methods of treating cartilage disorders through inhibition of clk and dyrk |
| WO2021168341A1 (en) | 2020-02-21 | 2021-08-26 | Samumed, Llc | Solid forms of 1-(5-(3-(7-(3-fluorophenyl)-3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridin-5-yl)pyridin-3-yl)-n,n-dimethylmethanamine |
| CN111606969B (zh) * | 2020-05-13 | 2023-02-03 | 四川大学 | 一种parp1蛋白降解剂及其在抗肿瘤中的应用 |
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