CN112955438A - 蛋白质酪氨酸磷酸酶抑制剂和其使用方法 - Google Patents
蛋白质酪氨酸磷酸酶抑制剂和其使用方法 Download PDFInfo
- Publication number
- CN112955438A CN112955438A CN201980054332.9A CN201980054332A CN112955438A CN 112955438 A CN112955438 A CN 112955438A CN 201980054332 A CN201980054332 A CN 201980054332A CN 112955438 A CN112955438 A CN 112955438A
- Authority
- CN
- China
- Prior art keywords
- fluoro
- trione
- thiadiazolidine
- lambda
- hydroxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
- C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
- C07D285/13—Oxygen atoms
-
- 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
- A61K31/433—Thidiazoles
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Enzymes And Modification Thereof (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862688226P | 2018-06-21 | 2018-06-21 | |
| US62/688226 | 2018-06-21 | ||
| PCT/US2019/038459 WO2019246513A1 (en) | 2018-06-21 | 2019-06-21 | Protein tyrosine phosphatase inhibitors and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN112955438A true CN112955438A (zh) | 2021-06-11 |
Family
ID=67254011
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980054332.9A Pending CN112955438A (zh) | 2018-06-21 | 2019-06-21 | 蛋白质酪氨酸磷酸酶抑制剂和其使用方法 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US10954202B2 (enExample) |
| EP (1) | EP3810580A1 (enExample) |
| JP (3) | JP7217762B2 (enExample) |
| KR (3) | KR102850637B1 (enExample) |
| CN (1) | CN112955438A (enExample) |
| AR (1) | AR125425A1 (enExample) |
| AU (3) | AU2019290197B2 (enExample) |
| BR (1) | BR112020026086A2 (enExample) |
| CA (1) | CA3104507A1 (enExample) |
| CL (1) | CL2020003316A1 (enExample) |
| CO (1) | CO2021000447A2 (enExample) |
| CR (1) | CR20210017A (enExample) |
| DO (1) | DOP2020000252A (enExample) |
| EC (1) | ECSP21003520A (enExample) |
| IL (1) | IL279587A (enExample) |
| MA (1) | MA52963A (enExample) |
| MX (2) | MX2020014223A (enExample) |
| PE (2) | PE20260750A1 (enExample) |
| PH (1) | PH12020552228A1 (enExample) |
| SG (1) | SG11202012820PA (enExample) |
| TW (2) | TWI888352B (enExample) |
| UY (2) | UY41151A (enExample) |
| WO (1) | WO2019246513A1 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115197167A (zh) * | 2022-07-22 | 2022-10-18 | 中国药科大学 | 1,2,4-噻二唑烷-3,5-二酮化合物及其制备方法和应用 |
| CN117343052A (zh) * | 2023-12-04 | 2024-01-05 | 英矽智能科技(上海)有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其应用 |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3765094A4 (en) | 2018-03-15 | 2021-12-22 | KSQ Therapeutics, Inc. | GENE REGULATORY COMPOSITIONS AND PROCEDURES FOR IMPROVED IMMUNOTHERAPY |
| TWI888352B (zh) * | 2018-06-21 | 2025-07-01 | 美商嘉來克生命科學有限責任公司 | 蛋白質酪胺酸磷酸酯酶抑制劑及其使用方法 |
| KR102983496B1 (ko) * | 2019-03-14 | 2026-06-29 | 칼리코 라이프 사이언시스 엘엘씨 | 단백질 티로신 포스파타제 억제제 및 이의 사용 방법 |
| AU2020395612A1 (en) * | 2019-12-04 | 2022-06-09 | Monash University | Methods of activating cytotoxic leukocytes using PTP1B and PTPN2 inhibitors |
| AU2020401376A1 (en) | 2019-12-12 | 2022-06-30 | Kumquat Biosciences Inc. | Compositions and methods for potentiating immune activity |
| MX2022007441A (es) * | 2019-12-18 | 2022-09-02 | Calico Life Sciences Llc | Inhibidores de proteína tirosina fosfatasa y sus métodos de uso. |
| EP4211122A1 (en) * | 2020-09-11 | 2023-07-19 | Calico Life Sciences LLC | Protein tyrosine phosphatase inhibitors and methods of use thereof |
| EP4351558A4 (en) * | 2021-06-10 | 2025-05-07 | Ness Therapeutics, Inc. | Compounds containing 5-(2-fluoro-6-hydroxyphenyl)-1,2,5-thiazolidin-3-one 1,1-dioxide as inhibitors of protein kinase phosphatase enzymes |
| WO2022271727A1 (en) * | 2021-06-21 | 2022-12-29 | Calico Life Sciences Llc | Degrader compounds and uses thereof |
| CN118556055A (zh) * | 2021-11-11 | 2024-08-27 | 卡里科生命科学有限责任公司 | 蛋白酪氨酸磷酸酶抑制剂及其使用方法 |
| MX2024005658A (es) * | 2021-11-11 | 2024-08-06 | Calico Life Sciences Llc | Inhibidores de proteina tirosina fosfatasa y metodos de uso de estos. |
| IL314650A (en) * | 2022-02-02 | 2024-09-01 | Nerio Therapeutics Inc | Protein tyrosine phosphatase inhibitors and uses thereof |
| KR20250011138A (ko) * | 2022-05-13 | 2025-01-21 | 네스 테라퓨틱스 인코포레이티드 | Ptpn2 저해제 |
| JP2025530135A (ja) * | 2022-09-13 | 2025-09-11 | カムクワット バイオサイエンシーズ インコーポレイテッド | ベンゾ縮合ｎ－複素環及びその使用 |
| EP4615840A1 (en) * | 2022-11-09 | 2025-09-17 | Bristol-Myers Squibb Company | Indazol substituted 1,2,5-thiadiazolidin derivatives as inhibitors of protein tyrosine phosphatase (ptpn2) for the treatment of cancer diseases |
| WO2024243441A1 (en) | 2023-05-24 | 2024-11-28 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2026112350A1 (en) * | 2024-11-22 | 2026-05-28 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003082841A1 (en) * | 2002-04-03 | 2003-10-09 | Novartis Ag | 5-substituted 1,1-dioxo-`1,2,5!thiazolidine-3-one derivatives as ptpase 1b inhibitors |
| WO2004041799A1 (en) * | 2002-11-07 | 2004-05-21 | Astrazeneca Ab | 5- (substituted phenyl) -thiadiazolidine-3-ones and their use as ptp1b |
| WO2007067612A1 (en) * | 2005-12-08 | 2007-06-14 | Novartis Ag | 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors |
Family Cites Families (24)
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| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| DK0495421T3 (da) | 1991-01-15 | 1996-12-09 | Alcon Lab Inc | Anvendelse af carragenaner i topiske ophthalmiske sammensætninger |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| EP1439834A1 (en) | 2001-10-30 | 2004-07-28 | Applied Research Systems ARS Holding N.V. | Oxindole hydrazide modulators of protein tyrosine phosphatases (ptps) |
| AU2003300447B2 (en) | 2002-12-30 | 2009-09-03 | Vertex Pharmaceuticals Incorporated | Sulfhydantoins as phosphate isosteres for use as phosphatase inhibitors in the treatment of cancer and autoimmune disorders |
| UA94724C2 (en) | 2005-12-08 | 2011-06-10 | Новартис Аг | Thiadiazolidinone derivatives as antidiabetic agents |
| EP1963294B1 (en) | 2005-12-08 | 2012-10-10 | Novartis AG | 1,2,5-thiazolidine derivatives useful for treating conditions mediated by protein tyrosine phosphatases (ptpase) |
| RU2008127253A (ru) | 2005-12-08 | 2010-01-20 | Новартис АГ (CH) | 1,1,3-триоксо-1,2,5-тиадиазолидины и их применение в качестве ингибиторов птфаз |
| EP1991544B1 (en) | 2006-01-30 | 2018-08-15 | vTv Therapeutics LLC | Substituted imidazole derivatives and their use as ptpase inhibitors |
| JP2009532379A (ja) | 2006-03-31 | 2009-09-10 | ノバルティス アクチエンゲゼルシャフト | ＰＴＰａｓｅのチアジアゾリジノン阻害剤 |
| WO2008142198A2 (en) | 2007-05-23 | 2008-11-27 | Valtion Teknillinen Tutkimuskeskus | A method for inhibiting or stimulating angiogenesis in an individual |
| WO2010008852A2 (en) | 2008-06-23 | 2010-01-21 | Taiga Biotechnologies, Inc. | Methods of trea fing λλd methods of diagnosing an immunoproliferative disorder |
| US9217012B2 (en) | 2009-04-08 | 2015-12-22 | Indiana University Research And Technology Corporation | Inhibitors of protein tyrosine phosphatases |
| WO2011057331A1 (en) | 2009-11-11 | 2011-05-19 | Monash University | A method for treating obesity |
| EP2531616A4 (en) | 2010-02-03 | 2013-07-10 | Univ Monash | DIAGNOSIS AND FORECAST ASSAY FOR BREAST CANCER |
| CA2977839C (en) | 2014-02-28 | 2022-07-26 | The Royal Institution For The Advancement Of Learning / Mcgill University | Tc-ptp inhibitors as apc activators for immunotherapy |
| JP2017524348A (ja) | 2014-06-10 | 2017-08-31 | モナッシュ ユニバーシティ | 養子細胞移入のためのｐｔｐｎ２阻害を用いた白血球の産生方法 |
| WO2017078499A2 (ko) | 2015-11-06 | 2017-05-11 | 경북대학교 산학협력단 | 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물 |
| KR101826690B1 (ko) | 2015-11-06 | 2018-03-22 | 경북대학교 산학협력단 | 단백질 타이로신 탈인산화효소 억제제를 포함하는 신경염증성 질환의 예방 또는 치료용 조성물 |
| WO2018148378A1 (en) | 2017-02-08 | 2018-08-16 | Dana-Farber Cancer Institute, Inc. | Modulating biomarkers to increase tumor immunity and improve the efficiacy of cancer immunotherapy |
| WO2018227248A1 (en) | 2017-06-13 | 2018-12-20 | Monash University | Methods and compositions for the treatment of obesity |
| WO2019036815A1 (en) | 2017-08-24 | 2019-02-28 | The Royal Institution For The Advancement Of Learning/Mcgill University | ENHANCEMENT OF CD8 + T LYMPHOCYTES FOR ADOPTIVE CELL THERAPY BY INHIBITING PTPN1 (PTP1B) AND PTPN2 (TC-PTP)) |
| TWI888352B (zh) * | 2018-06-21 | 2025-07-01 | 美商嘉來克生命科學有限責任公司 | 蛋白質酪胺酸磷酸酯酶抑制劑及其使用方法 |
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2019
- 2019-06-21 TW TW108121816A patent/TWI888352B/zh active
- 2019-06-21 PE PE2025003287A patent/PE20260750A1/es unknown
- 2019-06-21 MA MA052963A patent/MA52963A/fr unknown
- 2019-06-21 TW TW114106492A patent/TW202600546A/zh unknown
- 2019-06-21 CA CA3104507A patent/CA3104507A1/en active Pending
- 2019-06-21 AR ARP190101729A patent/AR125425A1/es unknown
- 2019-06-21 WO PCT/US2019/038459 patent/WO2019246513A1/en not_active Ceased
- 2019-06-21 KR KR1020237016153A patent/KR102850637B1/ko active Active
- 2019-06-21 PE PE2020002131A patent/PE20210372A1/es unknown
- 2019-06-21 CR CR20210017A patent/CR20210017A/es unknown
- 2019-06-21 EP EP19739482.8A patent/EP3810580A1/en active Pending
- 2019-06-21 SG SG11202012820PA patent/SG11202012820PA/en unknown
- 2019-06-21 UY UY0001041151A patent/UY41151A/es unknown
- 2019-06-21 AU AU2019290197A patent/AU2019290197B2/en active Active
- 2019-06-21 KR KR1020257027922A patent/KR20250133466A/ko active Pending
- 2019-06-21 BR BR112020026086-0A patent/BR112020026086A2/pt unknown
- 2019-06-21 KR KR1020217001743A patent/KR102533477B1/ko active Active
- 2019-06-21 UY UY0001038272A patent/UY38272A/es unknown
- 2019-06-21 MX MX2020014223A patent/MX2020014223A/es unknown
- 2019-06-21 CN CN201980054332.9A patent/CN112955438A/zh active Pending
- 2019-06-21 JP JP2020571382A patent/JP7217762B2/ja active Active
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2020
- 2020-09-18 US US17/025,644 patent/US10954202B2/en active Active
- 2020-12-18 MX MX2024004318A patent/MX2024004318A/es unknown
- 2020-12-20 IL IL279587A patent/IL279587A/en unknown
- 2020-12-21 CL CL2020003316A patent/CL2020003316A1/es unknown
- 2020-12-21 DO DO2020000252A patent/DOP2020000252A/es unknown
- 2020-12-21 PH PH12020552228A patent/PH12020552228A1/en unknown
-
2021
- 2021-01-18 EC ECSENADI20213520A patent/ECSP21003520A/es unknown
- 2021-01-19 CO CONC2021/0000447A patent/CO2021000447A2/es unknown
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2023
- 2023-01-24 JP JP2023008491A patent/JP7704787B2/ja active Active
- 2023-11-10 AU AU2023263567A patent/AU2023263567B2/en active Active
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2025
- 2025-06-26 JP JP2025107930A patent/JP7881804B2/ja active Active
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2026
- 2026-05-15 AU AU2026203759A patent/AU2026203759A1/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003082841A1 (en) * | 2002-04-03 | 2003-10-09 | Novartis Ag | 5-substituted 1,1-dioxo-`1,2,5!thiazolidine-3-one derivatives as ptpase 1b inhibitors |
| WO2004041799A1 (en) * | 2002-11-07 | 2004-05-21 | Astrazeneca Ab | 5- (substituted phenyl) -thiadiazolidine-3-ones and their use as ptp1b |
| WO2007067612A1 (en) * | 2005-12-08 | 2007-06-14 | Novartis Ag | 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115197167A (zh) * | 2022-07-22 | 2022-10-18 | 中国药科大学 | 1,2,4-噻二唑烷-3,5-二酮化合物及其制备方法和应用 |
| CN117343052A (zh) * | 2023-12-04 | 2024-01-05 | 英矽智能科技(上海)有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其应用 |
| CN117343052B (zh) * | 2023-12-04 | 2024-02-06 | 英矽智能科技(上海)有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其应用 |
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