AR109650A1 - Compuestos de heteroarilcarboxamida como inhibidores de ripk2 - Google Patents
Compuestos de heteroarilcarboxamida como inhibidores de ripk2Info
- Publication number
- AR109650A1 AR109650A1 ARP170102539A ARP170102539A AR109650A1 AR 109650 A1 AR109650 A1 AR 109650A1 AR P170102539 A ARP170102539 A AR P170102539A AR P170102539 A ARP170102539 A AR P170102539A AR 109650 A1 AR109650 A1 AR 109650A1
- Authority
- AR
- Argentina
- Prior art keywords
- 3alkyl
- 6alkyl
- optionally substituted
- membered
- compounds
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 102000013070 Receptor-Interacting Protein Serine-Threonine Kinase 2 Human genes 0.000 title 1
- 108010079933 Receptor-Interacting Protein Serine-Threonine Kinase 2 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 5
- 229910052757 nitrogen Inorganic materials 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 238000000034 method Methods 0.000 abstract 3
- 229910052717 sulfur Chemical group 0.000 abstract 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 239000011737 fluorine Substances 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 2
- 239000011593 sulfur Chemical group 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—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
- 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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
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Abstract
También composiciones farmacéuticas que comprenden estos compuestos, métodos para usar estos compuestos en el tratamiento de varias enfermedades y trastornos, procesos para preparar estos compuestos e intermediarios útiles en estos procesos. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), o sales de aquel aceptables desde el punto de vista farmacéutico, en donde X es N e Y es CH; o X es CH e Y es N; HET es un anillo de heteroarilo de 5 miembros que contiene de 1 a 3 heteroátomos seleccionados de nitrógeno y azufre, en donde cada anillo de heteroarilo se sustituye opcionalmente con 1 a 2 grupos de sustituyentes seleccionados independientemente de R³ y R⁴; o HET es un anillo de heteroarilo de 5 miembros que contiene de 1 a 3 heteroátomos seleccionados de nitrógeno y azufre, en donde cada anillo de heteroarilo se sustituye con 2 grupos de sustituyentes seleccionados de Rᵃ y Rᵇ, en donde Rᵃ y Rᵇ, junto con los átomos a los que están unidos, forman un anillo heterocíclico o de heteroarilo de 5 - 6 miembros que puede ser opcionalmente sustituido con 1 a 2 sustituyentes seleccionados de R³ y R⁴; R¹ es hidrógeno o F; R² es C₁₋₃alquilo o Cl; R³ y R⁴ se seleccionan cada uno independientemente de: (a) -H, (b) -OR⁵, (c) -O-C₁₋₆alquil-O-C₁₋₃alquilo (d) -O-C₃₋₆cicloalquilo, (e) -C(O)R⁵, (f) C₁₋₆alquilo opcionalmente sustituido con 1 a 3 -OH, flúor, heterociclilo opcionalmente sustituido con oxo, C₃₋₆cicloalquilo, -CO₂R⁵, -O-C₁₋₆alquilo, arilo, -N(R⁵)(R⁶) o -C(O)N(R⁵)(R⁶), (g) C₃₋₆cicloalquilo opcionalmente sustituido con 1 a 3 -OH, 1 a 3 flúor, C₁₋₆alquilo, -OC₁₋₆alquilo, C₁₋₆alquil-OC₁₋₆alquilo, C₁₋₆alquilo-OH, CF₃, -OC₃₋₆cicloalquilo, -CO₂H, -CO₂R⁵, C₃₋₆cicloalquilo, heteroarilo de 5 - 6 miembros, C₃₋₆heterociclilo, N(R⁵)(R⁶) o -C(O)N(R⁵)(R⁶), (h) -CO₂R⁵, (i) -C(O)N(R⁵)(R⁶), (j) -S(O)₂N(R⁵)(R⁶), (k) -S(O)ₙ-R⁵, (l) un grupo heteroarilo de 5 - 6 miembros opcionalmente sustituido con 1 a 3 grupos seleccionados de C₁₋₆alquilo, C₃₋₆cicloalquilo, halógeno, -CF₃, -OH, -(CH₂)ₙCO₂R⁵, -C(O)N(R⁵)(R⁶), -N(R⁵)(R⁶), -NH-SO₂C₁₋₆alquilo, C₁₋₆alcoxilo, C₁₋₆alquil-O-C₁₋₃alquilo, C₁₋₆alquilhidroxilo, C₁₋₃alquil-CN, oxo, fenilo opcionalmente sustituido con halógeno y -S(O)ₙC₁₋₆alquilo, (m) grupo heterociclilo monocíclico, bicíclico o espirocíclico de 4 - 10 miembros que contiene N, S u O, en donde cada heterociclo es opcionalmente sustituido con 1 - 3 sustituyentes seleccionados de anillo heterocíclico de 3 - 6 miembros, halógeno, -C₁₋₃alquilo, -C₁₋₃alquil-O-C₁₋₃alquilo y -C₁₋₃alquil-C(O)N(R⁵)(R⁶), (n) arilo, (o) -N(R⁵)(R⁶); R⁵ y R⁶ se seleccionan cada uno independientemente de -H, heterociclilo de 4 - 6 miembros, -C(O)-C₁₋₃alquil-C(O)-C₁₋₃cicloalquilo y -C₁₋₆alquilo, en donde cada R⁵ y R⁶ se sustituye independientemente, de manera opcional, con -OH, C₃₋₆cicloalquilo, -C₁₋₃alquilo, -O-C₁₋₃alquilo, -NH-C₁₋₃alquilo o -N-(C₁₋₃alquilo)₂; o R⁵ y R⁶, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico de 4 - 6 miembros opcionalmente sustituido con metilo; y n es 0, 1 ó 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662394779P | 2016-09-15 | 2016-09-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR109650A1 true AR109650A1 (es) | 2019-01-09 |
Family
ID=59901598
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170102539A AR109650A1 (es) | 2016-09-15 | 2017-09-14 | Compuestos de heteroarilcarboxamida como inhibidores de ripk2 |
Country Status (31)
| Country | Link |
|---|---|
| US (4) | US10138241B2 (es) |
| EP (1) | EP3512833B1 (es) |
| JP (1) | JP6733050B2 (es) |
| KR (1) | KR102472736B1 (es) |
| CN (1) | CN110023290B (es) |
| AR (1) | AR109650A1 (es) |
| AU (1) | AU2017327539B2 (es) |
| BR (1) | BR112019003320B1 (es) |
| CL (1) | CL2019000476A1 (es) |
| CO (1) | CO2019001181A2 (es) |
| CY (1) | CY1123494T1 (es) |
| DK (1) | DK3512833T3 (es) |
| EA (1) | EA038128B1 (es) |
| ES (1) | ES2816003T3 (es) |
| HR (1) | HRP20201494T1 (es) |
| HU (1) | HUE051551T2 (es) |
| IL (1) | IL265062B (es) |
| LT (1) | LT3512833T (es) |
| MA (1) | MA46229B1 (es) |
| MX (1) | MX387443B (es) |
| NZ (1) | NZ750416A (es) |
| PE (1) | PE20190979A1 (es) |
| PH (1) | PH12019500497A1 (es) |
| PL (1) | PL3512833T3 (es) |
| PT (1) | PT3512833T (es) |
| RS (1) | RS60729B1 (es) |
| SA (1) | SA519401322B1 (es) |
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| DK3464336T3 (da) | 2016-06-01 | 2022-05-09 | Athira Pharma Inc | Forbindelser |
| CN110023290B (zh) | 2016-09-15 | 2022-08-12 | 勃林格殷格翰国际有限公司 | 作为ripk2抑制剂的杂芳基甲酰胺化合物 |
| US10138222B2 (en) | 2016-09-15 | 2018-11-27 | Boehringer Ingelheim International Gmbh | Substituted benzamides as RIPK2 inhibitors |
| EP3824906A1 (en) | 2016-12-21 | 2021-05-26 | Amgen Inc. | Anti-tnf alpha antibody formulations |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| JP7458406B2 (ja) * | 2018-12-21 | 2024-03-29 | セルジーン コーポレーション | Ripk2のチエノピリジン阻害剤 |
| AR118471A1 (es) * | 2019-03-22 | 2021-10-06 | Takeda Pharmaceuticals Co | Derivados de pirrol e imidazol fusionados con piridina como inhibidores de ripk2 |
| CN119698416A (zh) | 2022-06-10 | 2025-03-25 | 英特莱治疗公司 | 作为ripk2抑制剂的咪唑并(1,2-a)吡啶衍生物 |
| AU2024286701A1 (en) | 2023-06-09 | 2026-01-08 | Interline Therapeutics, Inc. | Methods of treating inflammatory diseases |
| WO2024259328A1 (en) * | 2023-06-16 | 2024-12-19 | Odyssey Therapeutics, Inc. | Inhibitors of ripk2 and uses thereof |
| WO2025085928A1 (en) | 2023-10-20 | 2025-04-24 | Odyssey Therapeutics, Inc. | Methods of treating a patient with an inflammatory bowel disease |
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| SI1379525T1 (sl) | 2001-02-21 | 2007-12-31 | Astrazeneca Ab | Heteropoliciklične spojine in njihova uporaba kot antagonisti metabotropnih glutamatnih receptorjev |
| ATE482200T1 (de) | 2003-05-01 | 2010-10-15 | Bristol Myers Squibb Co | Als kinaseinhibitoren geeignete arylsubstituierte pyrazolamidverbindungen |
| AR060635A1 (es) | 2006-04-27 | 2008-07-02 | Banyu Pharma Co Ltd | Derivados de 1,2-dihidro-3h-pirazolo[3,4-d]pirimidin-3-ona, composiciones farmaceuticas que los comprenden y su uso en el tratamiento del cancer |
| NZ574621A (en) | 2006-07-07 | 2012-03-30 | Boehringer Ingelheim Int | Phenyl substituted heteroaryl-derivatives and use thereof as anti-tumour agents |
| CN101528717B (zh) | 2006-11-09 | 2013-04-24 | 弗·哈夫曼-拉罗切有限公司 | 噻唑和*唑-取代的芳基酰胺类化合物 |
| EP2245025A1 (en) | 2008-02-27 | 2010-11-03 | Merck Patent GmbH | Carboxamide-heteroaryl derivatives for the treatment of diabetes |
| CN101671336B (zh) | 2009-09-23 | 2013-11-13 | 辽宁利锋科技开发有限公司 | 芳杂环并嘧啶衍生物和类似物及其制备方法和用途 |
| US8377970B2 (en) | 2009-10-08 | 2013-02-19 | Rhizen Pharmaceuticals Sa | Modulators of calcium release-activated calcium channel |
| US20130023532A1 (en) | 2010-03-26 | 2013-01-24 | Casillas Linda N | Indazolyl-pyrimidines as kinase inhibitors |
| WO2011123609A1 (en) * | 2010-03-31 | 2011-10-06 | Glaxo Group Limited | Imidazolyl-imidazoles as kinase inhibitors |
| UY33808A (es) | 2010-12-17 | 2012-07-31 | Syngenta Participations Ag | Compuestos insecticidas |
| CA2826059A1 (en) | 2011-02-09 | 2012-08-16 | Pierre Joseph Marcel Jung | Insecticidal compounds |
| UY34863A (es) | 2012-06-19 | 2013-12-31 | Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware | Antagonistas de iap |
| AR092529A1 (es) | 2012-09-13 | 2015-04-22 | Glaxosmithkline Llc | Compuesto de aminoquinazolina, composicion farmaceutica que lo comprende y uso de dicho compuesto para la preparacion de un medicamento |
| US20140142129A1 (en) | 2012-11-20 | 2014-05-22 | Celgene Avilomics Research, Inc, | Methods of treating a disease or disorder associated with bruton's tyrosine kinase |
| PT2953942T (pt) | 2013-02-06 | 2018-01-17 | Bayer Cropscience Ag | Derivados de pirazol substituídos com halogéneo como agentes pesticidas |
| EP2968276A4 (en) | 2013-03-15 | 2017-02-15 | President and Fellows of Harvard College | Hybrid necroptosis inhibitors |
| AU2014337044A1 (en) | 2013-10-18 | 2016-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
| WO2015101622A1 (de) | 2014-01-03 | 2015-07-09 | Bayer Cropscience Ag | Neue pyrazolyl-heteroarylamide als schädlingsbekämpfungsmittel |
| CN107454899B (zh) | 2014-10-27 | 2020-05-29 | 大学健康网络 | Ripk2抑制剂及用其治疗癌症的方法 |
| FI3504187T3 (fi) | 2016-08-24 | 2025-04-05 | Prilenia Neurotherapeutics Ltd | Pridopidiinin käyttö toiminnallisen heikkenemisen hoitoa varten |
| CN110023290B (zh) | 2016-09-15 | 2022-08-12 | 勃林格殷格翰国际有限公司 | 作为ripk2抑制剂的杂芳基甲酰胺化合物 |
| US10138222B2 (en) | 2016-09-15 | 2018-11-27 | Boehringer Ingelheim International Gmbh | Substituted benzamides as RIPK2 inhibitors |
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