ES2901349T3 - Derivado de pirazol pirimidina y usos del mismo - Google Patents
Derivado de pirazol pirimidina y usos del mismo Download PDFInfo
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- ES2901349T3 ES2901349T3 ES16753709T ES16753709T ES2901349T3 ES 2901349 T3 ES2901349 T3 ES 2901349T3 ES 16753709 T ES16753709 T ES 16753709T ES 16753709 T ES16753709 T ES 16753709T ES 2901349 T3 ES2901349 T3 ES 2901349T3
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- branched
- straight
- compound
- alkyl
- halide
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- 238000012216 screening Methods 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- WBHQBSYUUJJSRZ-UHFFFAOYSA-M sodium bisulfate Chemical compound [Na+].OS([O-])(=O)=O WBHQBSYUUJJSRZ-UHFFFAOYSA-M 0.000 description 1
- 229910000342 sodium bisulfate Inorganic materials 0.000 description 1
- 239000012279 sodium borohydride Substances 0.000 description 1
- 229910000033 sodium borohydride Inorganic materials 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- RMBAVIFYHOYIFM-UHFFFAOYSA-M sodium methanethiolate Chemical compound [Na+].[S-]C RMBAVIFYHOYIFM-UHFFFAOYSA-M 0.000 description 1
- 229940054269 sodium pyruvate Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 230000020347 spindle assembly Effects 0.000 description 1
- 125000003003 spiro group Chemical group 0.000 description 1
- 229940031439 squalene Drugs 0.000 description 1
- TUHBEKDERLKLEC-UHFFFAOYSA-N squalene Natural products CC(=CCCC(=CCCC(=CCCC=C(/C)CCC=C(/C)CC=C(C)C)C)C)C TUHBEKDERLKLEC-UHFFFAOYSA-N 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008223 sterile water Substances 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- FEYLUKDSKVSMSZ-UHFFFAOYSA-N tert-butyl n-(4-aminocyclohexyl)carbamate Chemical compound CC(C)(C)OC(=O)NC1CCC(N)CC1 FEYLUKDSKVSMSZ-UHFFFAOYSA-N 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 239000003104 tissue culture media Substances 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- 230000002103 transcriptional effect Effects 0.000 description 1
- 230000026683 transduction Effects 0.000 description 1
- 238000010361 transduction Methods 0.000 description 1
- LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 description 1
- 229910000404 tripotassium phosphate Inorganic materials 0.000 description 1
- 235000019798 tripotassium phosphate Nutrition 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 230000028973 vesicle-mediated transport Effects 0.000 description 1
- 230000035899 viability Effects 0.000 description 1
- 235000012431 wafers Nutrition 0.000 description 1
- 208000016261 weight loss Diseases 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 229910001845 yogo sapphire Inorganic materials 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
Classifications
-
- 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
- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- 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
- 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
- C07D403/08—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 alicyclic rings
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562200846P | 2015-08-04 | 2015-08-04 | |
| US201562268750P | 2015-12-17 | 2015-12-17 | |
| PCT/IL2016/050852 WO2017021969A1 (en) | 2015-08-04 | 2016-08-04 | Pyrazole pyrimidine derivative and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2901349T3 true ES2901349T3 (es) | 2022-03-22 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES16753709T Active ES2901349T3 (es) | 2015-08-04 | 2016-08-04 | Derivado de pirazol pirimidina y usos del mismo |
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|---|---|
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| EP (1) | EP3331877B1 (enExample) |
| JP (1) | JP7083309B2 (enExample) |
| KR (1) | KR102698366B1 (enExample) |
| CN (1) | CN108137562B (enExample) |
| AU (2) | AU2016304464B2 (enExample) |
| CA (1) | CA2994644A1 (enExample) |
| CY (1) | CY1124898T1 (enExample) |
| DK (1) | DK3331877T3 (enExample) |
| ES (1) | ES2901349T3 (enExample) |
| HR (1) | HRP20211949T1 (enExample) |
| HU (1) | HUE057607T2 (enExample) |
| IL (1) | IL257282B (enExample) |
| LT (1) | LT3331877T (enExample) |
| MX (1) | MX384172B (enExample) |
| PL (1) | PL3331877T3 (enExample) |
| PT (1) | PT3331877T (enExample) |
| RS (1) | RS62728B1 (enExample) |
| RU (1) | RU2735522C2 (enExample) |
| SI (1) | SI3331877T1 (enExample) |
| SM (1) | SMT202100720T1 (enExample) |
| WO (1) | WO2017021969A1 (enExample) |
| ZA (1) | ZA201800671B (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US10376511B2 (en) * | 2015-08-04 | 2019-08-13 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Pyrazole pyrimidine derivative and uses thereof |
| MX394556B (es) * | 2017-02-01 | 2025-03-24 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Derivados de n1-(4-(5-(ciclopropilmetil)-1-metil-1h-pirazol-4-il) piridin-2-il) ciclohexano-1,4-diamina y compuestos relacionados como inhibidores de ck1 y/o irak1 para tratar cáncer. |
| JOP20180011A1 (ar) | 2017-02-16 | 2019-01-30 | Gilead Sciences Inc | مشتقات بيرولو [1، 2-b]بيريدازين |
| WO2019155468A1 (en) | 2018-02-08 | 2019-08-15 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use |
| TWI898556B (zh) | 2018-07-13 | 2025-09-21 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒衍生物 |
| 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 |
| US11472791B2 (en) | 2019-03-05 | 2022-10-18 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| SG11202113211PA (en) * | 2019-06-03 | 2021-12-30 | Biotheryx Inc | Non-hygroscopic crystalline salts of a pyrazole compound, and pharmaceutical compositions and use thereof |
| WO2021000957A1 (zh) * | 2019-07-04 | 2021-01-07 | 北京国鸿生物医药科技有限公司 | 一种杂环化合物、其药物组合物及用途 |
| BR112022002698A2 (pt) | 2019-08-14 | 2022-07-19 | Incyte Corp | Compostos de imidazolil pirimidinilamina como inibidores de cdk2 |
| AU2020364007A1 (en) | 2019-10-11 | 2022-04-28 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| AU2021209057A1 (en) * | 2020-01-13 | 2022-06-30 | Yissum Research Development Company Of The Hebrew University Of Jerusalem, Ltd. | Pyrazolylpyrimidines and use thereof |
| WO2021155050A1 (en) * | 2020-01-29 | 2021-08-05 | Biotheryx, Inc. | Kinase modulators, pharmaceutical compositions, and therapeutic applications |
| WO2021191384A1 (en) * | 2020-03-26 | 2021-09-30 | Janssen Pharmaceutica Nv | Aryl piperidines as monoacylglycerol lipase modulators |
| US20240207268A1 (en) * | 2021-03-24 | 2024-06-27 | Biotheryx, Inc. | Pyrazolylpyrimidines for treating malignant solid tumor |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11752151B2 (en) * | 2021-07-12 | 2023-09-12 | Buddhist Tzu Chi Medical Foundation | Method for enhancing hair growth |
| US20230053307A1 (en) * | 2021-07-19 | 2023-02-16 | Buddhist Tzu Chi Medical Foundation | Method for preventing or treating skin disorders and conditions |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| WO2025199440A1 (en) * | 2024-03-21 | 2025-09-25 | Edgewood Oncology | Methods of treating liposarcoma using a pyrazole compound |
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| EP1343781B1 (en) | 2000-12-05 | 2008-09-03 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| US6884804B2 (en) | 2001-05-16 | 2005-04-26 | Vertex Pharmaceuticals Incorporated | Inhibitors of Src and other protein kinases |
| GB0215844D0 (en) | 2002-07-09 | 2002-08-14 | Novartis Ag | Organic compounds |
| US20090036448A1 (en) | 2004-03-30 | 2009-02-05 | Taisho Pharmecutical Co., Ltd. | Pyrimidine derivatives and methods of treatment related to the use thereof |
| JP2007145819A (ja) | 2005-10-28 | 2007-06-14 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| WO2007129195A2 (en) * | 2006-05-04 | 2007-11-15 | Pfizer Products Inc. | 4-pyrimidine-5-amino-pyrazole compounds |
| JP2009538352A (ja) | 2006-05-26 | 2009-11-05 | アストラゼネカ アクチボラグ | 細胞増殖を阻害するための薬剤としての２−カルボシクロアミノ−４−イミダゾリルピリミジン類 |
| EP2231636B1 (en) | 2007-12-07 | 2011-09-14 | Novartis AG | Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases |
| WO2013066684A1 (en) | 2011-11-04 | 2013-05-10 | Jasco Pharmaceuticals, LLC | Aminopyrimidine kinase inhibitors |
| CA2925211A1 (en) | 2013-09-27 | 2015-04-02 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| EP3057956B1 (en) * | 2013-10-18 | 2021-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) |
| US10376511B2 (en) | 2015-08-04 | 2019-08-13 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Pyrazole pyrimidine derivative and uses thereof |
| MX394556B (es) * | 2017-02-01 | 2025-03-24 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Derivados de n1-(4-(5-(ciclopropilmetil)-1-metil-1h-pirazol-4-il) piridin-2-il) ciclohexano-1,4-diamina y compuestos relacionados como inhibidores de ck1 y/o irak1 para tratar cáncer. |
| WO2019155468A1 (en) | 2018-02-08 | 2019-08-15 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use |
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2016
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- 2016-08-04 JP JP2018525826A patent/JP7083309B2/ja active Active
- 2016-08-04 PT PT167537091T patent/PT3331877T/pt unknown
- 2016-08-04 RU RU2018107668A patent/RU2735522C2/ru active
- 2016-08-04 MX MX2018001395A patent/MX384172B/es unknown
- 2016-08-04 CN CN201680059148.XA patent/CN108137562B/zh active Active
- 2016-08-04 SI SI201631426T patent/SI3331877T1/sl unknown
- 2016-08-04 ES ES16753709T patent/ES2901349T3/es active Active
- 2016-08-04 WO PCT/IL2016/050852 patent/WO2017021969A1/en not_active Ceased
- 2016-08-04 KR KR1020187006128A patent/KR102698366B1/ko active Active
- 2016-08-04 AU AU2016304464A patent/AU2016304464B2/en active Active
- 2016-08-04 PL PL16753709T patent/PL3331877T3/pl unknown
- 2016-08-04 DK DK16753709.1T patent/DK3331877T3/da active
- 2016-08-04 RS RS20211558A patent/RS62728B1/sr unknown
- 2016-08-04 SM SM20210720T patent/SMT202100720T1/it unknown
- 2016-08-04 EP EP16753709.1A patent/EP3331877B1/en active Active
- 2016-08-04 HR HRP20211949TT patent/HRP20211949T1/hr unknown
- 2016-08-04 LT LTEPPCT/IL2016/050852T patent/LT3331877T/lt unknown
- 2016-08-04 CA CA2994644A patent/CA2994644A1/en active Pending
- 2016-08-04 HU HUE16753709A patent/HUE057607T2/hu unknown
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2018
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- 2018-01-31 ZA ZA2018/00671A patent/ZA201800671B/en unknown
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2019
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2021
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2024
- 2024-02-05 US US18/432,931 patent/US20250049793A1/en active Pending
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