ES2660051T3 - Compuestos heterocíclicos condensados como inhibidores selectivos de BMP - Google Patents
Compuestos heterocíclicos condensados como inhibidores selectivos de BMP Download PDFInfo
- Publication number
- ES2660051T3 ES2660051T3 ES13840866.1T ES13840866T ES2660051T3 ES 2660051 T3 ES2660051 T3 ES 2660051T3 ES 13840866 T ES13840866 T ES 13840866T ES 2660051 T3 ES2660051 T3 ES 2660051T3
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- Prior art keywords
- substituted
- compound
- unsubstituted
- cancer
- cycloalkyl
- Prior art date
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- 229940124639 Selective inhibitor Drugs 0.000 title 1
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 13
- 210000000130 stem cell Anatomy 0.000 claims 3
- 206010068715 Fibrodysplasia ossificans progressiva Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000007170 pathology Effects 0.000 claims 2
- 208000030760 Anaemia of chronic disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000015710 Iron-Deficiency Anemia Diseases 0.000 claims 1
- 206010067125 Liver injury Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000035490 Megakaryoblastic Acute Leukemia Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010047295 Ventricular hypertrophy Diseases 0.000 claims 1
- 208000013593 acute megakaryoblastic leukemia Diseases 0.000 claims 1
- 208000020700 acute megakaryocytic leukemia Diseases 0.000 claims 1
- 208000007502 anemia Diseases 0.000 claims 1
- 208000022400 anemia due to chronic disease Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 230000004221 bone function Effects 0.000 claims 1
- 230000003683 cardiac damage Effects 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 230000004069 differentiation Effects 0.000 claims 1
- 208000019622 heart disease Diseases 0.000 claims 1
- 231100000234 hepatic damage Toxicity 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 210000003292 kidney cell Anatomy 0.000 claims 1
- 230000008818 liver damage Effects 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000011164 ossification Effects 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 230000001902 propagating effect Effects 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 abstract description 20
- 125000003118 aryl group Chemical group 0.000 abstract description 9
- 229910052757 nitrogen Inorganic materials 0.000 abstract description 3
- 229910052760 oxygen Inorganic materials 0.000 abstract description 3
- 229910052717 sulfur Inorganic materials 0.000 abstract description 3
- 229910052799 carbon Inorganic materials 0.000 abstract description 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 101100496169 Arabidopsis thaliana CLH1 gene Proteins 0.000 abstract 1
- 101100044057 Mesocricetus auratus SYCP3 gene Proteins 0.000 abstract 1
- 101100080600 Schizosaccharomyces pombe (strain 972 / ATCC 24843) nse6 gene Proteins 0.000 abstract 1
- 101150111293 cor-1 gene Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 description 14
- 125000000753 cycloalkyl group Chemical group 0.000 description 10
- 229920000728 polyester Polymers 0.000 description 6
- 150000002894 organic compounds Chemical class 0.000 description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical group OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 4
- 125000004432 carbon atom Chemical group C* 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 4
- -1 s-pentyl Chemical group 0.000 description 4
- 125000000547 substituted alkyl group Chemical group 0.000 description 4
- 125000003545 alkoxy group Chemical group 0.000 description 3
- 239000013626 chemical specie Substances 0.000 description 3
- 150000004820 halides Chemical class 0.000 description 3
- 125000005842 heteroatom Chemical group 0.000 description 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 3
- CXMXRPHRNRROMY-UHFFFAOYSA-N sebacic acid group Chemical group C(CCCCCCCCC(=O)O)(=O)O CXMXRPHRNRROMY-UHFFFAOYSA-N 0.000 description 3
- 238000006467 substitution reaction Methods 0.000 description 3
- 102100024505 Bone morphogenetic protein 4 Human genes 0.000 description 2
- 101000762379 Homo sapiens Bone morphogenetic protein 4 Proteins 0.000 description 2
- 125000002015 acyclic group Chemical group 0.000 description 2
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 description 2
- 125000005233 alkylalcohol group Chemical group 0.000 description 2
- 125000004122 cyclic group Chemical group 0.000 description 2
- SBOJXQVPLKSXOG-UHFFFAOYSA-N o-amino-hydroxylamine Chemical compound NON SBOJXQVPLKSXOG-UHFFFAOYSA-N 0.000 description 2
- 230000003389 potentiating effect Effects 0.000 description 2
- 125000005415 substituted alkoxy group Chemical group 0.000 description 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 2
- 150000003573 thiols Chemical class 0.000 description 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- SNRUBQQJIBEYMU-UHFFFAOYSA-N Dodecane Natural products CCCCCCCCCCCC SNRUBQQJIBEYMU-UHFFFAOYSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 1
- 125000003282 alkyl amino group Chemical group 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 125000001204 arachidyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 125000002837 carbocyclic group Chemical group 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 239000000460 chlorine Substances 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000003438 dodecyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000000623 heterocyclic group Chemical group 0.000 description 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001183 hydrocarbyl group Chemical group 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000002463 lignoceryl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 125000001421 myristyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000002868 norbornyl group Chemical group C12(CCC(CC1)C2)* 0.000 description 1
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 125000000913 palmityl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 230000008707 rearrangement Effects 0.000 description 1
- 238000007363 ring formation reaction Methods 0.000 description 1
- 229930195734 saturated hydrocarbon Natural products 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000005017 substituted alkenyl group Chemical group 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
Classifications
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
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| US201261707661P | 2012-09-28 | 2012-09-28 | |
| US201261707661P | 2012-09-28 | ||
| PCT/US2013/032588 WO2014051698A1 (en) | 2012-09-28 | 2013-03-15 | Fused heterocyclic compounds as selective bmp inhibitors |
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| ES (1) | ES2660051T3 (enExample) |
| SG (1) | SG11201503299YA (enExample) |
| WO (1) | WO2014051698A1 (enExample) |
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| CN111773213B (zh) | 2010-09-01 | 2023-02-24 | 托马斯杰弗逊大学 | 用于肌肉修复和再生的组合物和方法 |
| WO2015123424A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| LT3105218T (lt) | 2014-02-13 | 2019-12-10 | Incyte Corp | Ciklopropilaminai kaip lsd1 inhibitoriai |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| EA201792205A1 (ru) | 2015-04-03 | 2018-02-28 | Инсайт Корпорейшн | Гетероциклические соединения как ингибиторы lsd1 |
| US10836742B2 (en) | 2015-08-11 | 2020-11-17 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
| HK1256753A1 (zh) | 2015-08-11 | 2019-10-04 | Neomed Institute | 芳基-取代的二氢喹诺酮、它们的制备和它们作为药物的用途 |
| CN114605387A (zh) | 2015-08-12 | 2022-06-10 | 埃皮吉纳提克斯股份有限公司 | 取代的苯并咪唑、它们的制备和它们作为药物的用途 |
| DK3334709T3 (da) | 2015-08-12 | 2025-02-03 | Incyte Holdings Corp | Salte af en lsd1-hæmmer |
| US10501459B2 (en) | 2015-10-21 | 2019-12-10 | Neomed Institute | Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors |
| WO2017127930A1 (en) * | 2016-01-28 | 2017-08-03 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals |
| ES2963348T3 (es) | 2016-06-08 | 2024-03-26 | Clementia Pharmaceuticals Inc | Métodos para tratar la osificación heterotópica |
| KR102359707B1 (ko) * | 2016-07-20 | 2022-02-09 | 노파르티스 아게 | 아미노피리딘 유도체 및 이의 선택적 alk-2 억제제로서의 용도 |
| WO2018053126A1 (en) | 2016-09-14 | 2018-03-22 | Vanderbilt University | Inhibition of bmp signaling, compounds, compositions and uses thereof |
| US20200054643A1 (en) * | 2017-01-18 | 2020-02-20 | Vanderbilt University | Fused heterocyclic compounds as selective bmp inhibitors |
| WO2019178383A1 (en) * | 2018-03-14 | 2019-09-19 | Vanderbilt University | Inhibition of bmp signaling, compounds, compositions and uses thereof |
| CN110496127A (zh) * | 2018-05-17 | 2019-11-26 | 中国科学院上海生命科学研究院 | 一种热休克因子1的抑制剂、其制备方法和应用 |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| JP7414827B2 (ja) * | 2018-12-20 | 2024-01-16 | インサイト・コーポレイション | アクチビン受容体様キナーゼ－２の阻害剤としてのイミダゾピリダジン及びイミダゾピリジン化合物 |
| CA3156007A1 (en) | 2019-09-27 | 2021-04-01 | Disc Medicine, Inc. | METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS |
| TW202131926A (zh) | 2019-11-22 | 2021-09-01 | 美商英塞特公司 | 包含alk2抑制劑及jak2抑制劑的組合療法 |
| ES3075793T3 (en) | 2020-05-13 | 2026-08-07 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| AU2021273014A1 (en) | 2020-05-13 | 2022-11-17 | AbbVie Deutschland GmbH & Co. KG | Anti-hemojuvelin (HJV) antibodies for treating anemia of chronic disease |
| IL298767A (en) | 2020-06-16 | 2023-02-01 | Incyte Corp | ALK2 inhibitors for the treatment of anemia |
| WO2024205336A1 (ko) * | 2023-03-30 | 2024-10-03 | 에이치엘비생명과학알앤디 주식회사 | 튜블린 저해 활성을 갖는 약학적 조성물 |
| AU2023449758A1 (en) * | 2023-05-22 | 2025-12-11 | Iregene Therapeutics Co., Ltd | Use of bmpr1b inhibitor in induced induction of development, and induction culture medium |
Family Cites Families (28)
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| FR2562071B1 (fr) * | 1984-03-30 | 1986-12-19 | Sanofi Sa | Triazolo(4,3-b)pyridazines, procede pour leur preparation et compositions pharmaceutiques les contenant |
| GB9927687D0 (en) * | 1999-11-23 | 2000-01-19 | Merck Sharp & Dohme | Therapeutic agents |
| JP4747396B2 (ja) | 2000-05-17 | 2011-08-17 | 日立化成工業株式会社 | 接着剤組成物、それを用いた回路端子の接続方法及び回路端子の接続構造 |
| BR0207096A (pt) * | 2001-02-20 | 2004-01-20 | Astrazeneca Ab | Uso de um composto, compostos, formulação farmacêutica, e, método de tratamento e/ou profilaxia de condições associadas com a inibição de glicogênio sintase quinase-3 |
| US7125888B2 (en) * | 2002-05-02 | 2006-10-24 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| DOP2006000051A (es) | 2005-02-24 | 2006-08-31 | Lilly Co Eli | Inhibidores de vegf-r2 y métodos |
| EP2086973B1 (en) * | 2006-10-11 | 2012-01-25 | Amgen Inc., | Imidazo- and triazolo-pyridine compounds and methods of use therof |
| CN101679408B (zh) | 2006-12-22 | 2016-04-27 | Astex治疗学有限公司 | 作为fgfr抑制剂的双环杂环化合物 |
| JP5442449B2 (ja) * | 2006-12-22 | 2014-03-12 | アステックス、セラピューティックス、リミテッド | 新規化合物 |
| ES2320955B1 (es) * | 2007-03-02 | 2010-03-16 | Laboratorios Almirall S.A. | Nuevos derivados de 3-((1,2,4)triazolo(4,3-a)piridin-7-il)benzamida. |
| JP2010522765A (ja) * | 2007-03-28 | 2010-07-08 | アレイ バイオファーマ、インコーポレイテッド | 受容体チロシンキナーゼとしてのイミダゾ［１，２−ａ］ピリジン化合物 |
| UA101611C2 (ru) * | 2007-04-03 | 2013-04-25 | Аррей Байофарма Инк. | СОЕДИНЕНИЯ ИМИДАЗО[1,2-а]ПИРИДИНА КАК ИНГИБИТОРЫ ТИРОЗИНКИНАЗЫ РЕЦЕПТОРОВ |
| WO2009002534A1 (en) | 2007-06-26 | 2008-12-31 | Gilead Colorado, Inc. | Imidazopyridinyl thiazolyl histone deacetylase inhibitors |
| KR101150581B1 (ko) * | 2007-07-26 | 2012-06-11 | 노파르티스 아게 | 유기 화합물 |
| EA201000615A1 (ru) * | 2007-10-17 | 2010-12-30 | Новартис Аг | Производные имидазо[1,2-а]пиридина, применимые в качестве ингибиторов апк (активиноподобной киназы) |
| EP2265603B1 (en) | 2008-03-13 | 2014-05-07 | The General Hospital Corporation | Inhibitors of the bmp signaling pathway |
| GB0810902D0 (en) * | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| WO2009157423A1 (ja) * | 2008-06-24 | 2009-12-30 | 財団法人乙卯研究所 | 縮合環を有するオキサゾリジノン誘導体 |
| US8592425B2 (en) | 2009-01-16 | 2013-11-26 | Merck Sharp & Dohme Corp. | Imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as mark inhibitors |
| CA2755285C (en) | 2009-03-20 | 2014-02-11 | Yunxin Y. Bo | Inhibitors of pi3 kinase |
| GB0906470D0 (en) * | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| JPWO2011136264A1 (ja) | 2010-04-28 | 2013-07-22 | 第一三共株式会社 | ［５，６］複素環化合物 |
| WO2011137155A1 (en) * | 2010-04-28 | 2011-11-03 | Bristol-Myers Squibb Company | Imidazopyridazinyl compounds and their uses for cancer |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| US9505763B2 (en) | 2011-07-25 | 2016-11-29 | Vanderbilt University | Cancer treatment using BMP inhibitor |
| EP2615151A1 (en) | 2011-12-23 | 2013-07-17 | Services Pétroliers Schlumberger | Compositions and methods for well cementing |
| EP2964651A4 (en) * | 2013-03-04 | 2016-11-30 | Brigham & Womens Hospital | BMP HEMMER AND METHOD OF USE THEREOF |
| JP6542192B2 (ja) | 2013-03-14 | 2019-07-10 | ザ ブリガム アンド ウィメンズ ホスピタル インコーポレイテッドＴｈｅ Ｂｒｉｇｈａｍ ａｎｄ Ｗｏｍｅｎ’ｓ Ｈｏｓｐｉｔａｌ， Ｉｎｃ． | Ｂｍｐ阻害剤およびその使用方法 |
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| EP2900238A4 (en) | 2016-04-06 |
| US20160068525A1 (en) | 2016-03-10 |
| SG11201503299YA (en) | 2015-06-29 |
| KR102092988B1 (ko) | 2020-03-25 |
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| EP2900238A1 (en) | 2015-08-05 |
| CA2886187A1 (en) | 2014-04-03 |
| US10196392B2 (en) | 2019-02-05 |
| CA2886187C (en) | 2020-04-14 |
| EP2900238B1 (en) | 2017-12-06 |
| JP2015531371A (ja) | 2015-11-02 |
| CN104768548B (zh) | 2018-08-10 |
| AU2013324396B2 (en) | 2018-10-04 |
| US9738636B2 (en) | 2017-08-22 |
| KR20150064137A (ko) | 2015-06-10 |
| US20170313701A1 (en) | 2017-11-02 |
| JP6430383B2 (ja) | 2018-11-28 |
| WO2014051698A1 (en) | 2014-04-03 |
| AU2013324396A1 (en) | 2015-05-14 |
| CN104768548A (zh) | 2015-07-08 |
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