PE20230251A1 - Terapia de combinacion que comprende un inhibidor de alk2 y un inhibidor de jak2 - Google Patents
Terapia de combinacion que comprende un inhibidor de alk2 y un inhibidor de jak2Info
- Publication number
- PE20230251A1 PE20230251A1 PE2022000820A PE2022000820A PE20230251A1 PE 20230251 A1 PE20230251 A1 PE 20230251A1 PE 2022000820 A PE2022000820 A PE 2022000820A PE 2022000820 A PE2022000820 A PE 2022000820A PE 20230251 A1 PE20230251 A1 PE 20230251A1
- Authority
- PE
- Peru
- Prior art keywords
- inhibitor
- alk2
- combination therapy
- jak2
- halo
- Prior art date
Links
- 229940126654 ALK2 inhibitor Drugs 0.000 title abstract 3
- 229940121730 Janus kinase 2 inhibitor Drugs 0.000 title abstract 3
- 238000002648 combination therapy Methods 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- KPRPFTOLWQQUAV-UHFFFAOYSA-N 2-amino-N-(4-hydroxy-1-bicyclo[2.2.2]octanyl)-5-[4-[3-(oxan-4-yl)-3-azabicyclo[3.1.0]hexan-1-yl]phenyl]pyridine-3-carboxamide Chemical group NC1=C(C(=O)NC23CCC(CC2)(CC3)O)C=C(C=N1)C1=CC=C(C=C1)C12CN(CC2C1)C1CCOCC1 KPRPFTOLWQQUAV-UHFFFAOYSA-N 0.000 abstract 1
- HFNKQEVNSGCOJV-UHFFFAOYSA-N 3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1-pyrazolyl]propanenitrile Chemical group C1=C(C=2C=3C=CNC=3N=CN=2)C=NN1C(CC#N)C1CCCC1 HFNKQEVNSGCOJV-UHFFFAOYSA-N 0.000 abstract 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000002071 myeloproliferative effect Effects 0.000 abstract 1
- 230000009826 neoplastic cell growth Effects 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 239000008194 pharmaceutical composition 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Referido a una terapia de combinacion que comprende un inhibidor de ALK2 y un inhibidor de JAK2; en donde el inhibidor de JAK2 tiene formula I, o una sal farmaceuticamente aceptable del mismo; caracterizado porque R1, R2 y R3 se seleccionan independientemente del grupo que consiste en H, halo y alquilo C1-4; R4 es H, halo, ciano, nitro, entre otros; Z es cicloalquilo de 3 a 6 miembros; un compuesto seleccionado del mismo es 3-ciclopentil-3-[4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]propanonitrilo; y en donde el inhibidor de ALK2 de formula II, o una sal farmaceuticamente aceptable del mismo; caracterizado porque R1 es cicloalquilo de 5 a 10 miembros con puente opcionalmente sustituido una, dos o tres veces por hidroxilo o alcoxi C1-C3; R2 se selecciona del grupo que consiste de alquilo C1-C3, alquenilo C2-C4, alquinilo de C2-C4, entre otros; un compuesto seleccionado del mismo es 2-amino-N-(4-hidroxibiciclo[2.2.2]octan-1-il)-5-(4-(3-(tetrahidro-2H-piran-4-il)-3-azabiciclo[3.1.0]hexan-1-il)fenil)nicotinamida. Tambien se refiere a composiciones farmaceuticas que comprenden dichos compuestos y su uso en el tratamiento del cancer, como la neoplasia mieloproliferativa o un sindrome mielodisplasico.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962939241P | 2019-11-22 | 2019-11-22 | |
| US202062980562P | 2020-02-24 | 2020-02-24 | |
| US202063035194P | 2020-06-05 | 2020-06-05 | |
| US202063056768P | 2020-07-27 | 2020-07-27 | |
| PCT/US2020/061497 WO2021102258A1 (en) | 2019-11-22 | 2020-11-20 | Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20230251A1 true PE20230251A1 (es) | 2023-02-07 |
Family
ID=73699492
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022000820A PE20230251A1 (es) | 2019-11-22 | 2020-11-20 | Terapia de combinacion que comprende un inhibidor de alk2 y un inhibidor de jak2 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US11738026B2 (es) |
| EP (1) | EP4061367A1 (es) |
| JP (1) | JP7717065B2 (es) |
| KR (1) | KR20220107213A (es) |
| CN (1) | CN115038443A (es) |
| AU (1) | AU2020388638A1 (es) |
| BR (1) | BR112022009710A2 (es) |
| CA (1) | CA3160312A1 (es) |
| CL (1) | CL2022001325A1 (es) |
| CR (1) | CR20220280A (es) |
| EC (1) | ECSP22044525A (es) |
| IL (1) | IL293085A (es) |
| MX (1) | MX2022006176A (es) |
| PE (1) | PE20230251A1 (es) |
| PH (1) | PH12022551052A1 (es) |
| TW (1) | TW202131926A (es) |
| WO (1) | WO2021102258A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3117695A1 (en) | 2018-10-26 | 2020-04-30 | Keros Therapeutics, Inc. | Crystal forms of an alk2 inhibitor |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CN115968289B (zh) | 2020-06-16 | 2025-09-30 | 因赛特公司 | 用于治疗贫血的alk2抑制剂 |
| WO2022098812A1 (en) | 2020-11-04 | 2022-05-12 | Keros Therapeutics, Inc. | Methods of treating iron overload |
| US20250034148A1 (en) * | 2021-11-02 | 2025-01-30 | Keros Therapeutics, Inc. | Methods of using alk2 inhibitors |
| CN116478145B (zh) * | 2022-04-13 | 2024-02-02 | 杭州邦顺制药有限公司 | Alk2激酶抑制剂 |
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| US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| PT3882249T (pt) | 2012-06-15 | 2025-08-06 | Sun Pharmaceutical Ind Inc | Derivados deuterados de ruxolitinib |
| CA2886187C (en) | 2012-09-28 | 2020-04-14 | Vanderbilt University | Fused heterocyclic compounds as selective bmp inhibitors |
| RS62329B1 (sr) | 2012-11-15 | 2021-10-29 | Incyte Holdings Corp | Dozni oblici ruksolitiniba sa produženim vremenom oslobađanja |
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| EP3060550B1 (en) | 2013-10-21 | 2019-05-15 | Merck Patent GmbH | Heteroaryl compounds as btk inhibitors and uses thereof |
| ES2907461T3 (es) | 2015-01-20 | 2022-04-25 | Boehringer Ingelheim Animal Health Usa Inc | Compuestos antihelmínticos, composiciones y procedimientos de uso de los mismos |
| PT3971177T (pt) | 2016-07-20 | 2024-07-30 | Novartis Ag | Derivados de aminopiridina e a sua utilização como inibidores seletivos de alk-2 |
| WO2018106820A1 (en) | 2016-12-07 | 2018-06-14 | Kura Oncology, Inc. | Methods of promoting beta cell proliferation |
| CN113015527A (zh) | 2018-08-21 | 2021-06-22 | 西拉肿瘤学公司 | 治疗骨髓纤维化的血小板计数诊断方法 |
| WO2021062171A1 (en) | 2019-09-27 | 2021-04-01 | Disc Medicine, Inc. | Methods for treating anemia of chronic disease |
| JP2022549506A (ja) | 2019-09-27 | 2022-11-25 | ディスク・メディシン・インコーポレイテッド | 骨髄線維症および関連状態を処置するための方法 |
| CN115968289B (zh) | 2020-06-16 | 2025-09-30 | 因赛特公司 | 用于治疗贫血的alk2抑制剂 |
-
2020
- 2020-11-20 WO PCT/US2020/061497 patent/WO2021102258A1/en not_active Ceased
- 2020-11-20 MX MX2022006176A patent/MX2022006176A/es unknown
- 2020-11-20 KR KR1020227020597A patent/KR20220107213A/ko active Pending
- 2020-11-20 PE PE2022000820A patent/PE20230251A1/es unknown
- 2020-11-20 CA CA3160312A patent/CA3160312A1/en active Pending
- 2020-11-20 US US16/953,989 patent/US11738026B2/en active Active
- 2020-11-20 PH PH1/2022/551052A patent/PH12022551052A1/en unknown
- 2020-11-20 BR BR112022009710A patent/BR112022009710A2/pt unknown
- 2020-11-20 CN CN202080094112.1A patent/CN115038443A/zh active Pending
- 2020-11-20 JP JP2022529824A patent/JP7717065B2/ja active Active
- 2020-11-20 AU AU2020388638A patent/AU2020388638A1/en active Pending
- 2020-11-20 CR CR20220280A patent/CR20220280A/es unknown
- 2020-11-20 TW TW109140802A patent/TW202131926A/zh unknown
- 2020-11-20 IL IL293085A patent/IL293085A/en unknown
- 2020-11-20 EP EP20820023.8A patent/EP4061367A1/en active Pending
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2022
- 2022-05-19 CL CL2022001325A patent/CL2022001325A1/es unknown
- 2022-06-03 EC ECSENADI202244525A patent/ECSP22044525A/es unknown
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2023
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Also Published As
| Publication number | Publication date |
|---|---|
| MX2022006176A (es) | 2022-08-17 |
| KR20220107213A (ko) | 2022-08-02 |
| JP7717065B2 (ja) | 2025-08-01 |
| US11738026B2 (en) | 2023-08-29 |
| US20210154195A1 (en) | 2021-05-27 |
| AU2020388638A1 (en) | 2022-06-30 |
| IL293085A (en) | 2022-07-01 |
| CL2022001325A1 (es) | 2023-03-24 |
| US20240041887A1 (en) | 2024-02-08 |
| JP2023502742A (ja) | 2023-01-25 |
| CA3160312A1 (en) | 2021-05-27 |
| TW202131926A (zh) | 2021-09-01 |
| WO2021102258A1 (en) | 2021-05-27 |
| CN115038443A (zh) | 2022-09-09 |
| PH12022551052A1 (en) | 2023-05-29 |
| ECSP22044525A (es) | 2022-08-31 |
| EP4061367A1 (en) | 2022-09-28 |
| CR20220280A (es) | 2022-09-02 |
| BR112022009710A2 (pt) | 2022-08-09 |
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