MX2022010439A - Antagonistas covalentes selectivos del receptor de androgenos (sarcas) y metodos de uso de los mismos. - Google Patents
Antagonistas covalentes selectivos del receptor de androgenos (sarcas) y metodos de uso de los mismos.Info
- Publication number
- MX2022010439A MX2022010439A MX2022010439A MX2022010439A MX2022010439A MX 2022010439 A MX2022010439 A MX 2022010439A MX 2022010439 A MX2022010439 A MX 2022010439A MX 2022010439 A MX2022010439 A MX 2022010439A MX 2022010439 A MX2022010439 A MX 2022010439A
- Authority
- MX
- Mexico
- Prior art keywords
- androgen receptor
- prostate cancer
- methods
- selective androgen
- sarcas
- Prior art date
Links
- 102000001307 androgen receptors Human genes 0.000 title abstract 4
- 108010080146 androgen receptors Proteins 0.000 title abstract 4
- 239000005557 antagonist Substances 0.000 title abstract 2
- 206010060862 Prostate cancer Diseases 0.000 abstract 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 208000002223 abdominal aortic aneurysm Diseases 0.000 abstract 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 abstract 2
- 208000007474 aortic aneurysm Diseases 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 230000001717 pathogenic effect Effects 0.000 abstract 2
- 108010040003 polyglutamine Proteins 0.000 abstract 2
- 201000004384 Alopecia Diseases 0.000 abstract 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 abstract 1
- 206010068597 Bulbospinal muscular atrophy congenital Diseases 0.000 abstract 1
- 208000027747 Kennedy disease Diseases 0.000 abstract 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 abstract 1
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 abstract 1
- 206010046798 Uterine leiomyoma Diseases 0.000 abstract 1
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 abstract 1
- 239000003098 androgen Substances 0.000 abstract 1
- 201000002996 androgenic alopecia Diseases 0.000 abstract 1
- 239000006227 byproduct Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 230000002500 effect on skin Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 201000010260 leiomyoma Diseases 0.000 abstract 1
- 230000036210 malignancy Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000035772 mutation Effects 0.000 abstract 1
- 229920000155 polyglutamine Polymers 0.000 abstract 1
- 102000054765 polymorphisms of proteins Human genes 0.000 abstract 1
- 210000002307 prostate Anatomy 0.000 abstract 1
- 208000022679 triple-negative breast carcinoma Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
- C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
-
- 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
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- 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
- A61K31/415—1,2-Diazoles
-
- A—HUMAN NECESSITIES
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- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/08—Antiseborrheics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
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- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/26—Androgens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C255/00—Carboxylic acid nitriles
- C07C255/61—Carboxylic acid nitriles containing cyano groups and nitrogen atoms being part of imino groups bound to the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- 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
- C07D231/12—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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- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Gynecology & Obstetrics (AREA)
- Oncology (AREA)
- Hospice & Palliative Care (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Esta invención se refiere a antagonistas covalentes selectivos de receptores de andrógenos, productos intermediarios sintéticos y subproductos, y compuestos relacionados, y composiciones que comprenden los mismos, y usos de los mismos en el tratamiento de enfermedades y afecciones dependientes del receptor de andrógenos, tales como hiperproliferaciones de la próstata, incluyendo pre malignidades e hiperplasia benigna de próstata, cáncer de próstata, cáncer de próstata avanzado, cáncer de próstata resistente a la castración, cáncer de mama triple negativo, otros cánceres que expresen el receptor de andrógenos, alopecia androgénica u otras enfermedades dérmicas hiperandrogénicas, enfermedad de Kennedy, esclerosis lateral amiotrófica (ALS), aneurisma de aorta abdominal (AAA) y fibromas uterinos, y a los métodos para reducir los niveles del receptor de andrógenos de longitud completa (AR-FL), incluyendo las mutaciones patógenas o de resistencia, variantes de empalme del AR (AR-SV) y los polimorfismos poliglutamínicos (polyQ) patógenos del AR.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062981516P | 2020-02-25 | 2020-02-25 | |
| PCT/US2021/019490 WO2021173731A1 (en) | 2020-02-25 | 2021-02-24 | Selective androgen receptor covalent antagonists (sarcas) and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2022010439A true MX2022010439A (es) | 2022-12-07 |
Family
ID=77492128
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2022010439A MX2022010439A (es) | 2020-02-25 | 2021-02-24 | Antagonistas covalentes selectivos del receptor de androgenos (sarcas) y metodos de uso de los mismos. |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20230303496A1 (es) |
| EP (1) | EP4110322A1 (es) |
| JP (1) | JP2023514455A (es) |
| KR (1) | KR20220146532A (es) |
| CN (1) | CN115427028A (es) |
| AU (1) | AU2021227665A1 (es) |
| CA (1) | CA3172890A1 (es) |
| IL (1) | IL295843A (es) |
| MX (1) | MX2022010439A (es) |
| WO (1) | WO2021173731A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4219454A1 (en) | 2022-01-28 | 2023-08-02 | F.I.S.- Fabbrica Italiana Sintetici S.p.A. | Highly efficient process for the preparation of 4-fluoro-1h-pyrazole or salts thereof |
| WO2023172872A2 (en) * | 2022-03-07 | 2023-09-14 | Cardiff Oncology, Inc. | Biomarkers for combination therapies |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102481319B1 (ko) * | 2016-06-10 | 2022-12-26 | 유니버시티 오브 테네시 리서치 파운데이션 | 선택적 안드로겐 수용체 분해제(sard) 리간드 및 이의 사용 방법 |
| WO2019023651A2 (en) * | 2017-07-28 | 2019-01-31 | Massachusetts Institute Of Technology | MODULATORS OF THE SMALL MOLECULE ANDROGEN RECEPTOR |
-
2021
- 2021-02-24 KR KR1020227032585A patent/KR20220146532A/ko unknown
- 2021-02-24 IL IL295843A patent/IL295843A/en unknown
- 2021-02-24 JP JP2022550924A patent/JP2023514455A/ja active Pending
- 2021-02-24 EP EP21759623.8A patent/EP4110322A1/en active Pending
- 2021-02-24 WO PCT/US2021/019490 patent/WO2021173731A1/en unknown
- 2021-02-24 CN CN202180030579.4A patent/CN115427028A/zh active Pending
- 2021-02-24 CA CA3172890A patent/CA3172890A1/en active Pending
- 2021-02-24 AU AU2021227665A patent/AU2021227665A1/en active Pending
- 2021-02-24 MX MX2022010439A patent/MX2022010439A/es unknown
-
2022
- 2022-08-24 US US17/821,952 patent/US20230303496A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CA3172890A1 (en) | 2021-09-02 |
| JP2023514455A (ja) | 2023-04-05 |
| IL295843A (en) | 2022-10-01 |
| AU2021227665A1 (en) | 2022-09-22 |
| EP4110322A1 (en) | 2023-01-04 |
| KR20220146532A (ko) | 2022-11-01 |
| CN115427028A (zh) | 2022-12-02 |
| WO2021173731A1 (en) | 2021-09-02 |
| US20230303496A1 (en) | 2023-09-28 |
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