MX2022014071A - Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo. - Google Patents
Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo.Info
- Publication number
- MX2022014071A MX2022014071A MX2022014071A MX2022014071A MX2022014071A MX 2022014071 A MX2022014071 A MX 2022014071A MX 2022014071 A MX2022014071 A MX 2022014071A MX 2022014071 A MX2022014071 A MX 2022014071A MX 2022014071 A MX2022014071 A MX 2022014071A
- Authority
- MX
- Mexico
- Prior art keywords
- forms
- bifunctional compound
- compound
- manufacturing
- same
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 230000001588 bifunctional effect Effects 0.000 title 2
- 150000001875 compounds Chemical class 0.000 title 2
- 239000002552 dosage form Substances 0.000 title 1
- 229940126062 Compound A Drugs 0.000 abstract 3
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 abstract 3
- 238000009472 formulation Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- CLCTZVRHDOAUGJ-UHFFFAOYSA-N N-[4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-[[4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindol-5-yl]piperazin-1-yl]methyl]piperidin-1-yl]pyridazine-3-carboxamide Chemical compound FC1=CC2=C(C=C1N1CCN(CC3CCN(CC3)C3=CC=C(N=N3)C(=O)NC3CCC(CC3)OC3=CC(Cl)=C(C=C3)C#N)CC1)C(=O)N(C1CCC(=O)NC1=O)C2=O CLCTZVRHDOAUGJ-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
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- 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
- C07D401/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D231/14—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/16—Halogen atoms or nitro radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Inorganic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente descripción se refiere a formas ultrapuras, polimorfos, formas amorfas y formulaciones de N-[(1r,4r)-4-(3-cloro-4-cianofenoxi)ciclohexil]-6-[4-({4-[2-(2,6- dioxopiperidin-3-il)-6-fluoro-1,3-dioxo-2,3-dihidro-1H-isoindol-5 -il]piperazin-1-il}metil)piperidin-1-il]piridazina-3-carboxamida, denominada en la presente descripción Compuesto A: (ver Fórmula) (Compuesto A). La presente descripción también se refiere a métodos de fabricación y purificación de los mismos, así como también a productos intermedios útiles en la síntesis del Compuesto A. Las formas ultrapuras, polimorfos, formas amorfas y formulaciones del Compuesto A pueden usarse como agentes terapéuticos para el tratamiento de varias enfermedades y afecciones tales como el cáncer.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063022475P | 2020-05-09 | 2020-05-09 | |
| US202163149143P | 2021-02-12 | 2021-02-12 | |
| US202163177378P | 2021-04-20 | 2021-04-20 | |
| PCT/US2021/031091 WO2021231174A1 (en) | 2020-05-09 | 2021-05-06 | Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2022014071A true MX2022014071A (es) | 2023-01-30 |
Family
ID=76305987
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2022014071A MX2022014071A (es) | 2020-05-09 | 2021-05-06 | Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo. |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US12043612B2 (es) |
| EP (1) | EP4146642A1 (es) |
| JP (1) | JP2023524599A (es) |
| KR (1) | KR20230015933A (es) |
| CN (1) | CN115996918A (es) |
| AU (1) | AU2021273458A1 (es) |
| BR (1) | BR112022022753A2 (es) |
| CA (1) | CA3181782A1 (es) |
| CL (1) | CL2023000074A1 (es) |
| CO (1) | CO2022017700A2 (es) |
| CR (1) | CR20220630A (es) |
| EC (1) | ECSP22086223A (es) |
| IL (1) | IL297762A (es) |
| MX (1) | MX2022014071A (es) |
| PE (1) | PE20231204A1 (es) |
| TW (1) | TW202208345A (es) |
| WO (1) | WO2021231174A1 (es) |
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|---|---|---|---|---|
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| CA3038979A1 (en) | 2016-10-11 | 2018-04-19 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| CA3154386A1 (en) | 2019-10-17 | 2021-04-22 | Michael Berlin | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| JP2023541434A (ja) | 2020-09-14 | 2023-10-02 | アルビナス・オペレーションズ・インコーポレイテッド | エストロゲン受容体の標的化分解のための化合物の結晶性形態 |
| WO2023025268A1 (zh) * | 2021-08-27 | 2023-03-02 | 苏州晶云药物科技股份有限公司 | 哒嗪甲酰胺类化合物的晶型及其制备方法 |
| WO2023143427A1 (zh) * | 2022-01-27 | 2023-08-03 | 杭州领业医药科技有限公司 | Arv-110的晶型及其制备方法和用途 |
| WO2023205481A1 (en) | 2022-04-21 | 2023-10-26 | Arvinas Operations, Inc. | A combination for use in treating prostate cancer comprising arv-100 and abiraterone |
| WO2024201244A1 (en) | 2023-03-24 | 2024-10-03 | Assia Chemical Industries Ltd. | Solid state forms of bavdegalutamide and process for preparation thereof |
| CN116282055B (zh) * | 2023-04-04 | 2024-10-15 | 昆明理工大学 | 一种利用酸淬提纯和改性无定形硼粉的方法 |
| CN116585319B (zh) * | 2023-04-14 | 2024-11-12 | 烟台大学 | 芳基氧环己基化合物制备抗前列腺癌药物的应用 |
| CN116444486B (zh) * | 2023-04-14 | 2024-09-03 | 烟台大学 | 一种芳基氧环己基化合物及其制备方法 |
| WO2024220926A1 (en) | 2023-04-21 | 2024-10-24 | Arvinas Operations, Inc. | Use of an androgen receptor degrader protac for the treatment of prostate cancer |
| WO2024233696A1 (en) | 2023-05-09 | 2024-11-14 | Arvinas Operations, Inc. | Bavdegalutamide for treating prostate cancer without ar l702h mutation |
| WO2025122895A1 (en) | 2023-12-08 | 2025-06-12 | Arvinas Operations, Inc. | Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy |
| CN118955474A (zh) * | 2024-07-29 | 2024-11-15 | 浙江爱索拓标记医药科技有限公司 | 一种放射性同位素碳-14标记的巴德卡鲁胺及其制备方法和应用 |
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| WO2021231174A1 (en) | 2021-11-18 |
| CO2022017700A2 (es) | 2022-12-20 |
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| EP4146642A1 (en) | 2023-03-15 |
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