PE20230457A1 - Conjugados para reactividad selectiva a dioles vecinales - Google Patents
Conjugados para reactividad selectiva a dioles vecinalesInfo
- Publication number
- PE20230457A1 PE20230457A1 PE2022002154A PE2022002154A PE20230457A1 PE 20230457 A1 PE20230457 A1 PE 20230457A1 PE 2022002154 A PE2022002154 A PE 2022002154A PE 2022002154 A PE2022002154 A PE 2022002154A PE 20230457 A1 PE20230457 A1 PE 20230457A1
- Authority
- PE
- Peru
- Prior art keywords
- formulas
- diols
- conjugates
- integer
- contain
- Prior art date
Links
- 150000002009 diols Chemical class 0.000 title abstract 4
- 230000009257 reactivity Effects 0.000 title 1
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 abstract 2
- 230000000144 pharmacologic effect Effects 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- 102000004877 Insulin Human genes 0.000 abstract 1
- 108090001061 Insulin Proteins 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- -1 boronate compound Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- ZHXTWWCDMUWMDI-UHFFFAOYSA-N dihydroxyboron Chemical compound O[B]O ZHXTWWCDMUWMDI-UHFFFAOYSA-N 0.000 abstract 1
- 230000002124 endocrine Effects 0.000 abstract 1
- MGXWVYUBJRZYPE-YUGYIWNOSA-N incretin Chemical class C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=C(O)C=C1 MGXWVYUBJRZYPE-YUGYIWNOSA-N 0.000 abstract 1
- 239000000859 incretin Substances 0.000 abstract 1
- 229940125396 insulin Drugs 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/28—Insulins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/62—Insulins
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Immunology (AREA)
- Toxicology (AREA)
- Biophysics (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La presente invencion se refiere a un compuesto boronado de formula I, entre otros, donde: R se selecciona de las formula FF1 a FF24; Z se selecciona de uno de : a) NH2 y OH, b) un enlace covalente, ya sea directamente o a traves de un conector opcional, a una sustancia farmacologica, entre otros; B1 y B2 cada uno representa independientemente un grupo seleccionado de las formula F1 a F9; B3 representa un grupo seleccionado de las formulas F1 a F11; X es un enlace covalente, ya sea directamente o a traves del conector opcional, hacia Z en la formula I; el indice i es un numero entero en el rango de 1 a 20; R1 represente (C=O)---, S(=O)(=O)---, entre otros; un R1 en F5 representa B(OH)2, el subindice j es un numero entero en el rango de 1 a 13. Los compuestos de la invencion pueden unirse selectivamente a dioles vecinales especificos en presencia de otros dioles y responder a estas moleculas en el cuerpo. Tambien pueden estar conjugados con una sustancia farmacologica, tal como la insulina, un peptido endocrino o de incretina humana o un analogo de este, y puede contener uno o mas aminoacidos modificados que contienen un sensor que responde al diol vecinal, siendo util en el tratamiento de la diabetes.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202063002662P | 2020-03-31 | 2020-03-31 | |
PCT/US2021/025261 WO2021202802A1 (en) | 2020-03-31 | 2021-03-31 | Conjugates for selective responsiveness to vicinal diols |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20230457A1 true PE20230457A1 (es) | 2023-03-10 |
Family
ID=75588297
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2022002154A PE20230457A1 (es) | 2020-03-31 | 2021-03-31 | Conjugados para reactividad selectiva a dioles vecinales |
Country Status (17)
Country | Link |
---|---|
US (1) | US20230134116A1 (es) |
EP (1) | EP4126058A1 (es) |
JP (1) | JP2023520049A (es) |
KR (1) | KR20220161422A (es) |
CN (1) | CN115843257A (es) |
AU (1) | AU2021247169A1 (es) |
BR (1) | BR112022019687A2 (es) |
CA (1) | CA3173417A1 (es) |
CL (1) | CL2022002662A1 (es) |
CO (1) | CO2022014157A2 (es) |
CR (1) | CR20220555A (es) |
EC (1) | ECSP22076278A (es) |
GB (1) | GB2610490A (es) |
IL (1) | IL296804A (es) |
MX (1) | MX2022012208A (es) |
PE (1) | PE20230457A1 (es) |
WO (1) | WO2021202802A1 (es) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA3198757A1 (en) * | 2020-11-19 | 2022-05-27 | Protomer Technologies Inc. | Aromatic boron-containing compounds and insulin analogs |
TW202409070A (zh) | 2022-05-18 | 2024-03-01 | 美商普羅托莫科技公司 | 芳族含硼化合物及相關胰島素類似物 |
Family Cites Families (38)
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US906028A (en) | 1908-03-27 | 1908-12-08 | Herbert E Jennison | Adjustable foot-block for radiators. |
US4421685A (en) | 1980-03-27 | 1983-12-20 | Eli Lilly And Company | Process for producing an insulin |
US6869930B1 (en) | 1993-09-17 | 2005-03-22 | Novo Nordisk A/S | Acylated insulin |
US6011007A (en) | 1993-09-17 | 2000-01-04 | Novo Nordisk A/S | Acylated insulin |
KR100310122B1 (ko) | 1993-09-17 | 2002-04-24 | 한센 핀 베네드, 안네 제헤르, 웨이콥 마리안느 | 아실화된인슐린 |
US5504188A (en) | 1994-06-16 | 1996-04-02 | Eli Lilly And Company | Preparation of stable zinc insulin analog crystals |
US5461031A (en) | 1994-06-16 | 1995-10-24 | Eli Lilly And Company | Monomeric insulin analog formulations |
US5474978A (en) | 1994-06-16 | 1995-12-12 | Eli Lilly And Company | Insulin analog formulations |
US5547929A (en) | 1994-09-12 | 1996-08-20 | Eli Lilly And Company | Insulin analog formulations |
US5693609A (en) | 1994-11-17 | 1997-12-02 | Eli Lilly And Company | Acylated insulin analogs |
YU18596A (sh) | 1995-03-31 | 1998-07-10 | Eli Lilly And Company | Analogne formulacije monomernog insulina |
US5866538A (en) | 1996-06-20 | 1999-02-02 | Novo Nordisk A/S | Insulin preparations containing NaCl |
PE79099A1 (es) | 1997-06-13 | 1999-08-24 | Lilly Co Eli | Formulaciones de insulina estables |
PE123799A1 (es) | 1997-10-24 | 1999-12-13 | Lilly Co Eli | Composiciones insolubles de insulina |
US6444641B1 (en) | 1997-10-24 | 2002-09-03 | Eli Lilly Company | Fatty acid-acylated insulin analogs |
ZA989744B (en) | 1997-10-31 | 2000-04-26 | Lilly Co Eli | Method for administering acylated insulin. |
JP2002500196A (ja) | 1998-01-09 | 2002-01-08 | ノヴォ ノルディスク アクティーゼルスカブ | 安定化させたインスリン組成物 |
US6586207B2 (en) | 2000-05-26 | 2003-07-01 | California Institute Of Technology | Overexpression of aminoacyl-tRNA synthetases for efficient production of engineered proteins containing amino acid analogues |
AU2002349295A1 (en) * | 2001-12-02 | 2003-06-17 | Novo Nordisk A/S | Glucose dependant release of insulin from glucose sensing insulin derivatives |
WO2003073238A2 (en) | 2002-02-27 | 2003-09-04 | California Institute Of Technology | Computational method for designing enzymes for incorporation of amino acid analogs into proteins |
JP5599543B2 (ja) | 2002-05-07 | 2014-10-01 | ノヴォ ノルディスク アー/エス | 単量体インスリン及びアシル化インスリンを含む可溶性製剤 |
JP2007518811A (ja) | 2004-01-23 | 2007-07-12 | カリフォルニア インスティチュート オブ テクノロジー | 操作されたタンパク質、ならびに作製方法および使用方法 |
CA2553040A1 (en) | 2004-02-02 | 2005-08-18 | Ambrx, Inc. | Modified human four helical bundle polypeptides and their uses |
KR101252835B1 (ko) | 2004-12-22 | 2013-04-10 | 암브룩스, 인코포레이티드 | 아미노아실-tRNA 합성효소의 조성물 및 그것의 용도 |
NZ555386A (en) | 2004-12-22 | 2011-01-28 | Ambrx Inc | Formulations of human growth hormone comprising a non-naturally encoded amino acid |
US20100247433A1 (en) | 2005-10-14 | 2010-09-30 | California Institute Of Technology | Use of non-canonical amino acids as metabolic markers for rapidly-dividing cells |
JP5808882B2 (ja) | 2006-03-03 | 2015-11-10 | カリフォルニア インスティテュート オブ テクノロジー | 分子へのアミノ酸の部位特異的な組み込み |
EP2581450B1 (en) | 2006-05-02 | 2018-08-15 | MedImmune Limited | Non-natural amino acid substituted polypeptides |
US20080096819A1 (en) | 2006-05-02 | 2008-04-24 | Allozyne, Inc. | Amino acid substituted molecules |
MX338336B (es) | 2007-11-20 | 2016-04-07 | Ambrx Inc | Polipeptidos de insulina modificados y sus usos. |
US9996862B2 (en) | 2012-07-23 | 2018-06-12 | @Pay Ip Holdings Llc | Point of sale email-based e-commerce |
US9867869B2 (en) * | 2012-12-12 | 2018-01-16 | Massachusetts Institute Of Technology | Insulin derivatives for diabetes treatment |
WO2015191705A1 (en) | 2014-06-10 | 2015-12-17 | California Institute Of Technology | Non-canonical insulins and their uses |
WO2017070617A1 (en) * | 2015-10-21 | 2017-04-27 | Case Western Reserve University | Diol-modified insulin analogues containing a glucose-regulated conformational switch |
JP7254792B2 (ja) * | 2017-11-09 | 2023-04-10 | ノヴォ ノルディスク アー/エス | グルコース感受性アルブミン結合誘導体 |
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TW202112397A (zh) * | 2019-03-29 | 2021-04-01 | 丹麥商諾佛.儂迪克股份有限公司 | 葡萄糖敏感型胰島素衍生物 |
US20220288213A1 (en) * | 2019-07-31 | 2022-09-15 | Thermalin Inc. | Insulin analogues with glucose regulated conformational switch |
-
2021
- 2021-03-31 AU AU2021247169A patent/AU2021247169A1/en active Pending
- 2021-03-31 CR CR20220555A patent/CR20220555A/es unknown
- 2021-03-31 BR BR112022019687A patent/BR112022019687A2/pt not_active Application Discontinuation
- 2021-03-31 GB GB2214274.9A patent/GB2610490A/en active Pending
- 2021-03-31 CA CA3173417A patent/CA3173417A1/en active Pending
- 2021-03-31 PE PE2022002154A patent/PE20230457A1/es unknown
- 2021-03-31 KR KR1020227037611A patent/KR20220161422A/ko unknown
- 2021-03-31 US US17/907,711 patent/US20230134116A1/en active Pending
- 2021-03-31 JP JP2022559876A patent/JP2023520049A/ja active Pending
- 2021-03-31 IL IL296804A patent/IL296804A/en unknown
- 2021-03-31 EP EP21720368.6A patent/EP4126058A1/en active Pending
- 2021-03-31 CN CN202180038883.3A patent/CN115843257A/zh active Pending
- 2021-03-31 WO PCT/US2021/025261 patent/WO2021202802A1/en active Application Filing
- 2021-03-31 MX MX2022012208A patent/MX2022012208A/es unknown
-
2022
- 2022-09-28 CL CL2022002662A patent/CL2022002662A1/es unknown
- 2022-09-30 EC ECSENADI202276278A patent/ECSP22076278A/es unknown
- 2022-10-03 CO CONC2022/0014157A patent/CO2022014157A2/es unknown
Also Published As
Publication number | Publication date |
---|---|
WO2021202802A1 (en) | 2021-10-07 |
CL2022002662A1 (es) | 2023-07-21 |
ECSP22076278A (es) | 2022-12-30 |
CA3173417A1 (en) | 2021-10-07 |
KR20220161422A (ko) | 2022-12-06 |
AU2021247169A1 (en) | 2022-10-20 |
MX2022012208A (es) | 2022-12-15 |
GB202214274D0 (en) | 2022-11-16 |
GB2610490A (en) | 2023-03-08 |
US20230134116A1 (en) | 2023-05-04 |
CR20220555A (es) | 2023-01-23 |
CO2022014157A2 (es) | 2023-03-27 |
IL296804A (en) | 2022-11-01 |
EP4126058A1 (en) | 2023-02-08 |
JP2023520049A (ja) | 2023-05-15 |
BR112022019687A2 (pt) | 2022-12-20 |
CN115843257A (zh) | 2023-03-24 |
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