AR093580A1 - Inhibidores bmi-1 de pirimidina sustituidos - Google Patents
Inhibidores bmi-1 de pirimidina sustituidosInfo
- Publication number
- AR093580A1 AR093580A1 ARP130104301A ARP130104301A AR093580A1 AR 093580 A1 AR093580 A1 AR 093580A1 AR P130104301 A ARP130104301 A AR P130104301A AR P130104301 A ARP130104301 A AR P130104301A AR 093580 A1 AR093580 A1 AR 093580A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- carbonyl
- alkoxy
- halo
- Prior art date
Links
- 101100058548 Felis catus BMI1 gene Proteins 0.000 title 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 21
- 125000001072 heteroaryl group Chemical group 0.000 abstract 9
- 125000003545 alkoxy group Chemical group 0.000 abstract 7
- -1 amino-sulfonyl-amino Chemical group 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000005843 halogen group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 101100058550 Mus musculus Bmi1 gene Proteins 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 abstract 2
- 150000001204 N-oxides Chemical class 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 2
- 125000001769 aryl amino group Chemical group 0.000 abstract 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 241000713869 Moloney murine leukemia virus Species 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000006598 aminocarbonylamino group Chemical group 0.000 abstract 1
- 210000003719 b-lymphocyte Anatomy 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000013522 chelant Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000002349 hydroxyamino group Chemical group [H]ON([H])[*] 0.000 abstract 1
- 230000010354 integration Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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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
-
- 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—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
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
En la presente, se describen compuestos de pirimidina sustituidos con amina y sus formas que inhiben la función y reducen el nivel de la proteína del sitio de integración 1 del virus de leucemia murina Moloney específica de células B (Bmi-1) y métodos para su uso para inhibir la función de Bmi-1 y reducir el nivel de Bmi-1 para tratar un cáncer mediado por Bmi-1. Reivindicación 1: Un compuesto de la fórmula (1), o una de sus formas, en donde X es N o N sustituido con un sustituyente de átomo de oxígeno para formar un N-óxido; R¹ es heteroarilo o heterociclilo opcionalmente sustituido en un miembro de anillo de átomo de carbono con uno, dos, tres o cuatro R⁵ sustituyentes o en un miembro de anillo de átomo de nitrógeno con un sustituyente de átomo de oxígeno para formar un N-óxido; R² es hidrógeno, ciano, halo, hidroxilo, nitro, alquilo C₁₋₈, hidroxil-alquilo C₁₋₈, alcoxi C₁₋₈, amino, alquil C₁₋₈-amino, (alquil C₁₋₈)₂-amino, hidroxil-amino, hidroxil-alquil C₁₋₈-amino, alcoxi C₁₋₈-alquil C₁₋₈ amino, alquil C₁₋₈-tio, alquil C₁₋₈-carbonilo, alquil C₁₋₈-carbonil-amino, amino-carbonilo, alquil C₁₋₈-amino-carbonilo, (alquil C₁₋₈)₂-amino-carbonilo, amino-carbonil-amino, alquil C₁₋₈-amino-carbonil-amino, (alquil C₁₋₈)₂-amino-carbonil-amino, alcoxi C₁₋₈-carbonilo, alcoxi C₁₋₈-carbonil-amino, amino-sulfonilo, alquil C₁₋₈-amino-sulfonilo, (alquil C₁₋₈)₂-amino-sulfonilo, amino-sulfonil-amino, alquil C₁₋₈-amino-sulfonil-amino, (alquil C₁₋₈)₂-amino-sulfonil-amino, P(O)(R⁷)₂-amino o heteroarilo, en donde el heteroarilo está opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes de alquilo C₁₋₈; R³ es hidrógeno, ciano, halo o alquilo C₁₋₈, amino, alquil C₁₋₈-amino o (alquil C₁₋₈)₂-amino; R⁴ es cicloalquilo C₃₋₁₄, arilo, heteroarilo o heterociclilo, cada uno opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes R⁶; R⁵ está seleccionado, de modo independiente, de ciano, halo, hidroxilo, nitro, oxo, alquilo C₁₋₈, ciano-alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxil-alquilo C₁₋₈, alcoxi C₁₋₈, alcoxi C₁₋₈-alquilo C₁₋₈, halo-alcoxi C₁₋₈, alquenilo C₂₋₈, alcoxi C₁₋₈-alquenilo C₂₋₈, alquinilo C₂₋₈, alcoxi C₁₋₈-alquinilo C₂₋₈, carboxilo, amino, alquil C₁₋₈-amino, (alquil C₁₋₈)₂-amino, amino-alquilo C₁₋₈, alquil C₁₋₈-amino-alquilo C₁₋₈, (alquil C₁₋₈)₂-amino-alquilo C₁₋₈, hidroxil-alquil C₁₋₈-amino, hidroxil-alquil C₁₋₈-amino-alquilo C₁₋₈, hidroxil-alquil C₁₋₈-amino-alquil C₁₋₈-amino, alquil C₁₋₈-tio, alquil C₁₋₈-carbonilo, alquil C₁₋₈-carbonil-amino, alquil C₁₋₈-carbonil-oxi, alquil C₁₋₈-carbonil-oxi-alquilo C₁₋₈, alcoxi C₁₋₈-carbonilo, alcoxi C₁₋₈-carbonil-alquilo C₁₋₈, alcoxi C₁₋₈-carbonil-amino, alquil C₁₋₈-sulfonilo, cicloalquilo C₃₋₁₄, arilo, aril-alquilo C₁₋₈, aril-amino, aril-alquil C₁₋₈-amino, heteroarilo, heteroaril-alquilo C₁₋₈ o heterociclilo, en donde cicloalquilo C₃₋₁₄, arilo, heteroarilo o heterociclilo y las porciones de arilo y heteroarilo de aril-alquilo C₁₋₈, aril-amino, aril-alquil C₁₋₈-amino y heteroaril-alquilo C₁₋₈ están cada uno opcionalmente sustituidos con uno, dos, tres o cuatro sustituyentes halo, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxil-alquilo C₁₋₈, alcoxi C₁₋₈, halo-alcoxi C₁₋₈, hidroxil-alcoxi C₁₋₈ o carboxilo; R⁶ está seleccionado, de modo independiente, de ciano, halo, hidroxilo, nitro, alquilo C₁₋₈, halo-alquilo C₁₋₈, hidroxil-alquilo C₁₋₈, alcoxi C₁₋₈, halo-alcoxi C₁₋₈, alquenilo C₂₋₈, alcoxi C₁₋₈-alquenilo C₂₋₈, alquinilo C₂₋₈, alcoxi C₁₋₈-alquinilo C₂₋₈, carboxilo, formilo, formil-oxi, alquil C₁₋₈-carbonilo, halo-alquil C₁₋₈-carbonilo, alquil C₁₋₈-tio, halo-alquil C₁₋₈-tio, amino, alquil C₁₋₈-amino, (alquil C₁₋₈)₂-amino, alquil C₁₋₈-carbonilo, alquil C₁₋₈-carbonil-oxi, alquil C₁₋₈-carbonil-oxi-alquilo C₁₋₈, alcoxi C₁₋₈-carbonilo, halo-alcoxi C₁₋₈-carbonilo, alcoxi C₁₋₈ carbonil-alquilo C₁₋₈, alcoxi C₁₋₈-carbonil-amino, alcoxi C₁₋₈-carbonil-amino-alquilo C₁₋₈, amino-carbonilo, alquil C₁₋₈-amino-carbonilo, (alquil C₁₋₈)₂-amino-carbonilo, alquil C₁₋₈-carbonil-amino, alquil C₁₋₈-carbonil-amino-alquilo C₁₋₈, amino-alquilo C₁₋₈, alquil C₁₋₈-amino-alquilo C₁₋₈, (alquil C₁₋₈)₂-amino-alquilo C₁₋₈, amino-alquil C₁₋₈-amino, alquil C₁₋₈-amino-alquil C₁₋₈-amino, (alquil C₁₋₈)₂-amino- alquil C₁₋₈-amino, hidroxil-alquil C₁₋₈-amino, hidroxil-alquil C₁₋₈-amino-alquilo C₁₋₈, hidroxil-alquil C₁₋₈-amino-alquil C₁₋₈-amino, imino-alquilo C₁₋₈, hidroxil-imino-alquilo C₁₋₈, alcoxi C₁₋₈-imino-alquilo C₁₋₈, alquil C₁₋₈-sulfonilo, halo-alquil C₁₋₈-sulfonilo, amino-sulfonilo, alquil C₁₋₈-amino-sulfonilo, (alquil C₁₋₈)₂-amino-sulfonilo, B(OR⁸)₂, cicloalquilo C₃₋₁₄, heterociclilo, arilo o heteroarilo, en donde cicloalquilo C₃₋₁₄, heterociclilo, arilo y heteroarilo están cada uno opcionalmente sustituidos con uno, dos, tres o cuatro sustituyentes de halo o alquilo C₁₋₈; R⁷ es, de modo independiente, hidroxilo o (alcoxi C₁₋₈)ₙ, en donde n representa un número entero de 1 a 5; y, R⁸ es, de modo independiente, hidrógeno o alquilo C₁₋₈; en donde la forma del compuesto está seleccionado de una sal, éster, hidrato, solvatos, quelato, clatrato, polimorfo, isotopólogo, estereoisómero, racemato, enantiómero, diastereómero o tautómero de él.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361872091P | 2013-08-30 | 2013-08-30 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR093580A1 true AR093580A1 (es) | 2015-06-10 |
Family
ID=52587180
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130104301A AR093580A1 (es) | 2013-08-30 | 2013-11-21 | Inhibidores bmi-1 de pirimidina sustituidos |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US10370371B2 (es) |
| EP (1) | EP3039015B1 (es) |
| JP (2) | JP6524094B2 (es) |
| KR (1) | KR102232595B1 (es) |
| CN (1) | CN105683166B (es) |
| AR (1) | AR093580A1 (es) |
| AU (2) | AU2013399092A1 (es) |
| CA (1) | CA2922657C (es) |
| CL (1) | CL2016000466A1 (es) |
| EA (1) | EA034866B1 (es) |
| IL (1) | IL244321B (es) |
| MX (1) | MX370588B (es) |
| NZ (2) | NZ748260A (es) |
| TW (1) | TWI692477B (es) |
| WO (1) | WO2015030847A1 (es) |
| ZA (1) | ZA201601697B (es) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ748260A (en) * | 2013-08-30 | 2020-01-31 | Ptc Therapeutics Inc | Substituted pyrimidine bmi-1 inhibitors |
| GB201321736D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| SG10201912959QA (en) | 2015-10-21 | 2020-02-27 | Otsuka Pharma Co Ltd | Benzolactam compounds as protein kinase inhibitors |
| US10851082B2 (en) | 2015-10-28 | 2020-12-01 | Northwestern University | Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (MNK1) and 2 (MNK2) |
| ES2775449T3 (es) | 2016-01-22 | 2020-07-27 | Janssen Pharmaceutica Nv | Nuevos derivados de cianoindolina sustituida como inhibidores de nik |
| CA3012031C (en) | 2016-01-22 | 2024-03-26 | Janssen Pharmaceutica Nv | 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors |
| MX383920B (es) | 2016-05-26 | 2025-03-14 | Recurium Ip Holdings Llc | Compuestos inhibidores de egfr. |
| CN109641882B (zh) | 2016-06-30 | 2022-10-28 | 杨森制药有限公司 | 作为nik抑制剂的杂芳族衍生物 |
| US20190119299A1 (en) | 2016-06-30 | 2019-04-25 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
| GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| AU2018352695A1 (en) | 2017-10-19 | 2020-05-28 | Effector Therapeutics, Inc. | Benzimidazole-indole inhibitors of Mnk1 and Mnk2 |
| LT3784664T (lt) | 2018-04-26 | 2025-03-25 | Pfizer Inc. | 2-amino-piridino arba 2-amino piridino dariniai kaip nuo ciklino priklausomos kinazės inhibitoriai |
| EP3564235A1 (en) * | 2018-05-03 | 2019-11-06 | Northwestern University | Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2) |
| US11319302B2 (en) * | 2018-06-07 | 2022-05-03 | The Regents Of The University Of Michigan | PRC1 inhibitors and methods of treatment therewith |
| EP3836932A2 (en) | 2018-08-17 | 2021-06-23 | PTC Therapeutics, Inc. | Method for treating pancreatic cancer |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| CA3131249A1 (en) * | 2019-02-28 | 2020-09-03 | Ptc Therapeutics, Inc. | 5-fluoro-2-(6fluoro-2-methyl-1h-benzo(d)imidazol-1-yl)-n4-(4-(trifluoromethyl)phenyl)pyrimidine-4,6-diamine dor treating a multiple myeloma |
| US11472791B2 (en) | 2019-03-05 | 2022-10-18 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors |
| US11919904B2 (en) | 2019-03-29 | 2024-03-05 | Incyte Corporation | Sulfonylamide compounds as CDK2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
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