JP2016510745A5 - - Google Patents
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- JP2016510745A5 JP2016510745A5 JP2015561550A JP2015561550A JP2016510745A5 JP 2016510745 A5 JP2016510745 A5 JP 2016510745A5 JP 2015561550 A JP2015561550 A JP 2015561550A JP 2015561550 A JP2015561550 A JP 2015561550A JP 2016510745 A5 JP2016510745 A5 JP 2016510745A5
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- substituted
- heterocyclyl
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- 150000001875 compounds Chemical class 0.000 claims description 36
- 230000000694 effects Effects 0.000 claims description 34
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 30
- 101000799140 Homo sapiens Activin receptor type-1 Proteins 0.000 claims description 22
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 22
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 229940124530 sulfonamide Drugs 0.000 claims description 19
- 150000003456 sulfonamides Chemical class 0.000 claims description 19
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims description 18
- 125000004442 acylamino group Chemical group 0.000 claims description 18
- 125000000217 alkyl group Chemical group 0.000 claims description 18
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 18
- 125000003118 aryl group Chemical group 0.000 claims description 18
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 208000035150 Hypercholesterolemia Diseases 0.000 claims description 16
- 150000001408 amides Chemical class 0.000 claims description 14
- 208000020346 hyperlipoproteinemia Diseases 0.000 claims description 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 14
- 150000003384 small molecules Chemical class 0.000 claims description 14
- 150000003462 sulfoxides Chemical class 0.000 claims description 14
- -1 cyano, sulfonyl Chemical group 0.000 claims description 13
- 125000002252 acyl group Chemical group 0.000 claims description 12
- 102000054953 human ACVR1 Human genes 0.000 claims description 12
- 230000002401 inhibitory effect Effects 0.000 claims description 12
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- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
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- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 10
- 241000282412 Homo Species 0.000 claims description 9
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims description 9
- 208000000563 Hyperlipoproteinemia Type II Diseases 0.000 claims description 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 8
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- 125000004423 acyloxy group Chemical group 0.000 claims description 6
- 125000003342 alkenyl group Chemical group 0.000 claims description 6
- 125000004414 alkyl thio group Chemical group 0.000 claims description 6
- 125000000304 alkynyl group Chemical group 0.000 claims description 6
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- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
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- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 6
- 239000000651 prodrug Substances 0.000 claims description 5
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- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
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- 102000052842 human TGFBR1 Human genes 0.000 claims description 4
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- JBMKAUGHUNFTOL-UHFFFAOYSA-N Aldoclor Chemical class C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NC=NS2(=O)=O JBMKAUGHUNFTOL-UHFFFAOYSA-N 0.000 claims description 2
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- 102100025423 Bone morphogenetic protein receptor type-1A Human genes 0.000 claims description 2
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- 206010006187 Breast cancer Diseases 0.000 claims description 2
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- 208000031953 Hereditary hemorrhagic telangiectasia Diseases 0.000 claims description 2
- 101000799189 Homo sapiens Activin receptor type-1B Proteins 0.000 claims description 2
- 101000934638 Homo sapiens Bone morphogenetic protein receptor type-1A Proteins 0.000 claims description 2
- 101000984546 Homo sapiens Bone morphogenetic protein receptor type-1B Proteins 0.000 claims description 2
- 101000799194 Homo sapiens Serine/threonine-protein kinase receptor R3 Proteins 0.000 claims description 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 2
- 102100025744 Mothers against decapentaplegic homolog 1 Human genes 0.000 claims description 2
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- 101700032040 SMAD1 Proteins 0.000 claims description 2
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- 241000700605 Viruses Species 0.000 claims description 2
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- 238000010521 absorption reaction Methods 0.000 claims description 2
- 210000004504 adult stem cell Anatomy 0.000 claims description 2
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- 229940124522 antiretrovirals Drugs 0.000 claims description 2
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- 239000002876 beta blocker Substances 0.000 claims description 2
- 229940097320 beta blocking agent Drugs 0.000 claims description 2
- 125000002619 bicyclic group Chemical group 0.000 claims description 2
- 210000000988 bone and bone Anatomy 0.000 claims description 2
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- 230000000747 cardiac effect Effects 0.000 claims description 2
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- 230000024245 cell differentiation Effects 0.000 claims description 2
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- 208000029664 classic familial adenomatous polyposis Diseases 0.000 claims description 2
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- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
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- 210000001671 embryonic stem cell Anatomy 0.000 claims description 2
- 208000028208 end stage renal disease Diseases 0.000 claims description 2
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- 239000000262 estrogen Substances 0.000 claims description 2
- 229940011871 estrogen Drugs 0.000 claims description 2
- 239000003862 glucocorticoid Substances 0.000 claims description 2
- 210000003709 heart valve Anatomy 0.000 claims description 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 2
- 235000009200 high fat diet Nutrition 0.000 claims description 2
- 102000049307 human ACVR1B Human genes 0.000 claims description 2
- 102000047644 human ACVRL1 Human genes 0.000 claims description 2
- 208000003532 hypothyroidism Diseases 0.000 claims description 2
- 230000002989 hypothyroidism Effects 0.000 claims description 2
- 238000000338 in vitro Methods 0.000 claims description 2
- 230000001939 inductive effect Effects 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 230000000366 juvenile effect Effects 0.000 claims description 2
- 150000002632 lipids Chemical class 0.000 claims description 2
- 208000019423 liver disease Diseases 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 230000002503 metabolic effect Effects 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 201000008968 osteosarcoma Diseases 0.000 claims description 2
- 244000045947 parasite Species 0.000 claims description 2
- 208000022560 parathyroid gland disease Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 230000026731 phosphorylation Effects 0.000 claims description 2
- 238000006366 phosphorylation reaction Methods 0.000 claims description 2
- 239000000583 progesterone congener Substances 0.000 claims description 2
- 230000000750 progressive effect Effects 0.000 claims description 2
- GPTFURBXHJWNHR-UHFFFAOYSA-N protopine Chemical compound C1=C2C(=O)CC3=CC=C4OCOC4=C3CN(C)CCC2=CC2=C1OCO2 GPTFURBXHJWNHR-UHFFFAOYSA-N 0.000 claims description 2
- 208000002815 pulmonary hypertension Diseases 0.000 claims description 2
- 230000000276 sedentary effect Effects 0.000 claims description 2
- 230000011664 signaling Effects 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 229940037128 systemic glucocorticoids Drugs 0.000 claims description 2
- 239000003451 thiazide diuretic agent Substances 0.000 claims description 2
- 201000008827 tuberculosis Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 37
- 102000004895 Lipoproteins Human genes 0.000 claims 1
- 108090001030 Lipoproteins Proteins 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 27
- 208000014644 Brain disease Diseases 0.000 description 1
- BBDGBGOVJPEFBT-UHFFFAOYSA-N C(C1)NCCN1c(cc1)ccc1-c1c[n]2ncc(-c3cccc4c3cccn4)c2nc1 Chemical compound C(C1)NCCN1c(cc1)ccc1-c1c[n]2ncc(-c3cccc4c3cccn4)c2nc1 BBDGBGOVJPEFBT-UHFFFAOYSA-N 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
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- 208000029078 coronary artery disease Diseases 0.000 description 1
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- 239000003550 marker Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361772465P | 2013-03-04 | 2013-03-04 | |
| US61/772,465 | 2013-03-04 | ||
| PCT/US2014/020360 WO2014138088A1 (en) | 2013-03-04 | 2014-03-04 | Bmp inhibitors and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016510745A JP2016510745A (ja) | 2016-04-11 |
| JP2016510745A5 true JP2016510745A5 (enExample) | 2017-04-06 |
Family
ID=51491878
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015561550A Withdrawn JP2016510745A (ja) | 2013-03-04 | 2014-03-04 | Ｂｍｐ阻害剤およびその使用方法 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20160115167A1 (enExample) |
| EP (1) | EP2964651A4 (enExample) |
| JP (1) | JP2016510745A (enExample) |
| WO (1) | WO2014138088A1 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5638961B2 (ja) | 2008-03-13 | 2014-12-10 | ザ ジェネラル ホスピタル コーポレイション | Ｂｍｐシグナル伝達経路のインヒビター |
| CN103200937B (zh) | 2010-09-01 | 2020-07-03 | 托马斯杰弗逊大学 | 用于肌肉修复和再生的组合物和方法 |
| ES2660051T3 (es) | 2012-09-28 | 2018-03-20 | Vanderbilt University | Compuestos heterocíclicos condensados como inhibidores selectivos de BMP |
| US10202356B2 (en) | 2013-03-14 | 2019-02-12 | Tolero Pharmaceuticals, Inc. | JAK2 and ALK2 inhibitors and methods for their use |
| US9682983B2 (en) | 2013-03-14 | 2017-06-20 | The Brigham And Women's Hospital, Inc. | BMP inhibitors and methods of use thereof |
| US10513521B2 (en) | 2014-07-15 | 2019-12-24 | The Brigham And Women's Hospital, Inc. | Compositions and methods for inhibiting BMP |
| JP6827954B2 (ja) | 2015-04-16 | 2021-02-10 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ３−（１ｈ−ベンズイミダゾール−２−イル）−１ｈ−ピリジン−２−オン誘導体 |
| EP3313420B1 (en) | 2015-06-25 | 2024-03-13 | The Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance |
| CN105130991B (zh) * | 2015-07-10 | 2017-09-19 | 成都知普莱生物医药科技有限公司 | 一种合成骨形态发生蛋白受体抑制剂的方法 |
| WO2017161001A1 (en) | 2016-03-15 | 2017-09-21 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion |
| EP3442977B1 (en) * | 2016-04-15 | 2023-06-28 | Blueprint Medicines Corporation | Inhibitors of activin receptor-like kinase |
| MX390115B (es) * | 2016-06-08 | 2025-03-20 | Clementia Pharmaceuticals Inc | Metodos para tratar la osificacion heterotopica. |
| LT3971177T (lt) * | 2016-07-20 | 2024-08-26 | Novartis Ag | Aminopiridino dariniai ir jų panaudojimas kaip selektyvių alk-2 inhibitorių |
| JP7018957B2 (ja) | 2016-11-16 | 2022-02-14 | クレメンティア ファーマシューティカルズ インコーポレイテッド | 多発性骨軟骨腫（ｍｏ）を処置するための方法 |
| CA3048376A1 (en) | 2016-12-27 | 2018-07-05 | Riken | Bmp-signal-inhibiting compound |
| CN110392686A (zh) | 2016-12-30 | 2019-10-29 | 频率治疗公司 | 1h-吡咯-2,5-二酮化合物以及使用它们来诱导干/祖支持细胞自我更新的方法 |
| US11026947B2 (en) | 2017-04-27 | 2021-06-08 | The Brigham And Women's Hospital, Inc. | ALK2 inhibitors and methods for inhibiting BMP signaling |
| US11236086B2 (en) | 2017-10-18 | 2022-02-01 | Blueprint Medicines Corporation | Substituted pyrrolopyridines as inhibitors of activin receptor-like kinase |
| CA3081762A1 (en) | 2017-11-15 | 2019-05-23 | Semma Therapeutics, Inc. | Islet cell manufacturing compositions and methods of use |
| WO2019126686A1 (en) | 2017-12-21 | 2019-06-27 | Frequency Therapeutics, Inc. | 1,2-dihydro-3h-pyrazol-3-one compounds and methods of using same |
| WO2019178383A1 (en) | 2018-03-14 | 2019-09-19 | Vanderbilt University | Inhibition of bmp signaling, compounds, compositions and uses thereof |
| MX2021000977A (es) | 2018-07-26 | 2021-04-12 | Sumitomo Pharma Oncology Inc | Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos. |
| CN114269345B (zh) | 2018-10-26 | 2025-06-27 | 科乐斯疗法公司 | Alk2抑制剂的晶体形式 |
| CN111721932B (zh) * | 2019-03-20 | 2024-08-16 | 复旦大学 | 以cd133为靶点的小分子化合物的筛选方法及其在制药中的应用 |
| CN114761013A (zh) | 2019-09-27 | 2022-07-15 | 迪斯克医药公司 | 治疗骨髓纤维化和相关病症的方法 |
| KR20220107213A (ko) | 2019-11-22 | 2022-08-02 | 인사이트 코포레이션 | Alk2 억제제 및 jak2 억제제를 포함하는 병용 요법 |
| KR20230012539A (ko) | 2020-05-13 | 2023-01-26 | 디스크 메디슨, 인크. | 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체 |
| JP2023530316A (ja) | 2020-06-16 | 2023-07-14 | インサイト・コーポレイション | 貧血の治療のためのａｌｋ２阻害剤 |
| WO2022098812A1 (en) | 2020-11-04 | 2022-05-12 | Keros Therapeutics, Inc. | Methods of treating iron overload |
| WO2022099166A1 (en) * | 2020-11-09 | 2022-05-12 | Keros Therapeutics, Inc. | Methods of treating cardiovascular-related disease |
| CN114668764A (zh) * | 2022-04-07 | 2022-06-28 | 中南大学 | 化合物在制备治疗糖尿病足的外用药物上的应用 |
| CN115252618A (zh) * | 2022-08-05 | 2022-11-01 | 大连医科大学附属第二医院 | 一种吡唑喹啉类衍生物的应用及其药物组合物 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010503383A (ja) * | 2006-09-12 | 2010-02-04 | ザ ジェネラル ホスピタル コーポレイション | 細胞シグナリングをモジュレートする化合物を同定するための方法およびこのような化合物を使用する方法 |
| JP5638961B2 (ja) * | 2008-03-13 | 2014-12-10 | ザ ジェネラル ホスピタル コーポレイション | Ｂｍｐシグナル伝達経路のインヒビター |
-
2014
- 2014-03-04 WO PCT/US2014/020360 patent/WO2014138088A1/en not_active Ceased
- 2014-03-04 EP EP14760191.8A patent/EP2964651A4/en not_active Withdrawn
- 2014-03-04 US US14/772,630 patent/US20160115167A1/en not_active Abandoned
- 2014-03-04 JP JP2015561550A patent/JP2016510745A/ja not_active Withdrawn
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