KR102062640B1 - 헤테로아릴-케톤 융합된 아자데칼린 글루코코르티코이드 수용체 조절제 - Google Patents
헤테로아릴-케톤 융합된 아자데칼린 글루코코르티코이드 수용체 조절제 Download PDFInfo
- Publication number
- KR102062640B1 KR102062640B1 KR1020147036405A KR20147036405A KR102062640B1 KR 102062640 B1 KR102062640 B1 KR 102062640B1 KR 1020147036405 A KR1020147036405 A KR 1020147036405A KR 20147036405 A KR20147036405 A KR 20147036405A KR 102062640 B1 KR102062640 B1 KR 102062640B1
- Authority
- KR
- South Korea
- Prior art keywords
- fluorophenyl
- isoquinolin
- sulfonyl
- pyrazolo
- methanone
- 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.)
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- 0 *c1ccnc(N2CCCC2)c1 Chemical compound *c1ccnc(N2CCCC2)c1 0.000 description 7
- DKLMSMGIZPVQIT-UHFFFAOYSA-O C(C1=C2C=CC=CC12)SC1=C[NH2+]NN1 Chemical compound C(C1=C2C=CC=CC12)SC1=C[NH2+]NN1 DKLMSMGIZPVQIT-UHFFFAOYSA-O 0.000 description 1
- ZFQOLZLPZWDUAK-BQYQJAHWSA-N C/N=C(\CCC1)/C1=C Chemical compound C/N=C(\CCC1)/C1=C ZFQOLZLPZWDUAK-BQYQJAHWSA-N 0.000 description 1
- SQINKHDAZFWLJZ-DEOSSOPVSA-N CCC[n]1ncc(S(N(CC2)C[C@](C3)(C(OC)=O)C2=Cc2c3cn[n]2-c(cc2)ccc2F)(=O)=O)c1 Chemical compound CCC[n]1ncc(S(N(CC2)C[C@](C3)(C(OC)=O)C2=Cc2c3cn[n]2-c(cc2)ccc2F)(=O)=O)c1 SQINKHDAZFWLJZ-DEOSSOPVSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/495—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
- 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
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P25/22—Anxiolytics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Child & Adolescent Psychology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Electroluminescent Light Sources (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261651669P | 2012-05-25 | 2012-05-25 | |
| US61/651,669 | 2012-05-25 | ||
| US201261691083P | 2012-08-20 | 2012-08-20 | |
| US61/691,083 | 2012-08-20 | ||
| US201261715907P | 2012-10-19 | 2012-10-19 | |
| US61/715,907 | 2012-10-19 | ||
| US201361759520P | 2013-02-01 | 2013-02-01 | |
| US61/759,520 | 2013-02-01 | ||
| US201361781629P | 2013-03-14 | 2013-03-14 | |
| US61/781,629 | 2013-03-14 | ||
| PCT/US2013/042732 WO2013177559A2 (en) | 2012-05-25 | 2013-05-24 | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20150021955A KR20150021955A (ko) | 2015-03-03 |
| KR102062640B1 true KR102062640B1 (ko) | 2020-01-06 |
Family
ID=49624542
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147036405A Active KR102062640B1 (ko) | 2012-05-25 | 2013-05-24 | 헤테로아릴-케톤 융합된 아자데칼린 글루코코르티코이드 수용체 조절제 |
Country Status (24)
| Country | Link |
|---|---|
| EP (6) | EP3851107B1 (enExample) |
| JP (1) | JP6172871B2 (enExample) |
| KR (1) | KR102062640B1 (enExample) |
| CN (1) | CN104619328B (enExample) |
| AU (1) | AU2013266110C1 (enExample) |
| BR (1) | BR112014028857B1 (enExample) |
| CA (1) | CA2872260C (enExample) |
| CL (1) | CL2014003173A1 (enExample) |
| DK (5) | DK2854814T3 (enExample) |
| ES (5) | ES2930298T3 (enExample) |
| FI (1) | FI4119561T3 (enExample) |
| HK (1) | HK1250014B (enExample) |
| IL (1) | IL235868A (enExample) |
| MX (1) | MX365423B (enExample) |
| MY (1) | MY172739A (enExample) |
| NZ (1) | NZ701469A (enExample) |
| PE (1) | PE20150352A1 (enExample) |
| PH (1) | PH12014502584A1 (enExample) |
| PL (5) | PL3590517T3 (enExample) |
| PT (5) | PT4119561T (enExample) |
| RU (1) | RU2639867C2 (enExample) |
| SG (1) | SG11201407682TA (enExample) |
| WO (1) | WO2013177559A2 (enExample) |
| ZA (1) | ZA201408182B (enExample) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11648245B2 (en) | 2012-05-25 | 2023-05-16 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| US11925626B2 (en) | 2018-12-19 | 2024-03-12 | Corcept Therapeutics Incorporated | Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound |
| US12226412B2 (en) | 2012-05-25 | 2025-02-18 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10047082B2 (en) | 2013-11-25 | 2018-08-14 | Corcept Therapeutics, Inc. | Octahydro fused azadecalin glucocorticoid receptor modulators |
| AU2016226451B2 (en) * | 2015-03-02 | 2019-12-19 | Corcept Therapeutics, Inc. | Use of glucocorticoid receptor antagonist and somatostatin analogues to treat ACTH-secreting tumors |
| KR102495223B1 (ko) * | 2015-03-30 | 2023-02-01 | 코어셉트 쎄라퓨틱스 인코포레이티드 | 부신기능부전을 치료하기 위한 글루코코르티코이드와 조합된 글루코코르티코이드 수용체 길항제의 용도 |
| JP6755264B2 (ja) | 2015-05-18 | 2020-09-16 | コーセプト セラピューティクス, インコーポレイテッド | クッシング症候群についての処置を診断および評価するための方法 |
| WO2017027851A1 (en) * | 2015-08-13 | 2017-02-16 | Corcept Therapeutics, Inc. | Method for differentially diagnosing acth-dependent cushing's syndrome |
| AU2017228329B2 (en) * | 2016-03-01 | 2021-03-11 | Corcept Therapeutics, Inc. | The use of glucocorticoid receptor modulators to potentiate checkpoint inhibitors |
| US9943505B2 (en) | 2016-09-09 | 2018-04-17 | Corcept Therapeutics, Inc. | Glucocorticoid receptor modulators to treat pancreatic cancer |
| PT3600282T (pt) | 2017-03-31 | 2025-11-05 | Corcept Therapeutics Inc | Moduladores de recetores de glucocorticoides para tratar cancro cervical |
| AU2018289307B2 (en) | 2017-06-20 | 2024-02-01 | Corcept Therapeutics, Inc. | Methods of treating neuroepithelial tumors using selective glucocorticoid receptor modulators |
| US10494349B2 (en) * | 2018-04-23 | 2019-12-03 | Corcept Therapeutics, Inc. | Methods of preparing regioselective N-alkyl triazoles |
| SG11202104732UA (en) | 2018-11-09 | 2021-06-29 | Corcept Therapeutics Inc | Methods for shrinking pituitary tumors |
| US11234971B2 (en) | 2018-12-19 | 2022-02-01 | Corcept Therapeutics Incorporated | Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent |
| WO2020132046A1 (en) | 2018-12-19 | 2020-06-25 | Corcept Therapeutics Incorporated | Methods of treating cancer comprising administration of a glucocorticoid receptor modulator and a cancer chemotherapy agent |
| CN113194944A (zh) * | 2018-12-20 | 2021-07-30 | 科塞普特治疗公司 | 用于对生长抑素受体阳性肿瘤进行成像和治疗的方法 |
| CN113490496A (zh) | 2019-02-22 | 2021-10-08 | 科赛普特治疗学股份有限公司 | 一种杂芳基-酮稠合氮杂萘烷糖皮质激素受体调节剂瑞拉可兰的治疗用途 |
| US12440487B2 (en) | 2019-10-16 | 2025-10-14 | Corcept Therapeutics Incorporated | Method of normalizing the neutrophil to lymphocyte ratio in cancer patients with a selective glucocorticoid receptor antagonist |
| WO2021119432A1 (en) | 2019-12-11 | 2021-06-17 | Corcept Therapeutics Incorporated | Methods of treating antipsychotic-induced weight gain with miricorilant |
| EP4076470B1 (en) | 2019-12-21 | 2025-12-03 | Corcept Therapeutics Incorporated | Treatment of, and differential diagnosis between, acth-dependent cushing's syndrome and acth-independent cushing's syndrome |
| WO2021163058A1 (en) * | 2020-02-10 | 2021-08-19 | Corcept Therapeutics Incorporated | Methods of stimulating an anti-tumor response using a selective glucocorticoid receptor modulator |
| WO2022134033A1 (en) * | 2020-12-25 | 2022-06-30 | Corcept Therapeutics Incorporated | Methods of preparing heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
| WO2022166810A1 (zh) * | 2021-02-03 | 2022-08-11 | 江苏恒瑞医药股份有限公司 | 稠合的氮杂三环类衍生物、其制备方法及其在医药上的应用 |
| WO2024077169A1 (en) * | 2022-10-06 | 2024-04-11 | Corcept Therapeutics Incorporated | Formulations of glucocorticoid receptor modulators |
| EP4608402A1 (en) | 2022-10-28 | 2025-09-03 | Corcept Therapeutics Incorporated | Treatments for amyotrophic lateral sclerosis using dazucorilant |
| US20250360125A1 (en) * | 2023-02-17 | 2025-11-27 | Corcept Therapeutics Incorporated | Methods and compositions for treating huntington's disease and its symptoms |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4963558A (en) | 1988-12-08 | 1990-10-16 | Lilly Industries Limited | Pyrazolo-[3,4-g]isoquinoline derivatives useful to treat CNS disorders |
| WO2005087769A1 (en) | 2004-03-09 | 2005-09-22 | Corcept Therapeutics, Inc. | Fused ring azadecalin glucocorticoid receptor modulators |
| US20100179115A1 (en) | 2006-02-28 | 2010-07-15 | Corcept Therapeutics, Inc. | Use of a glucocorticoid receptor ii antagonist to treat depression in patients taking il-2 |
| WO2012027702A1 (en) | 2010-08-27 | 2012-03-01 | Corcept Therapeutics, Inc. | Pyridyl-amine fused azadecalin modulators |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4391904A (en) | 1979-12-26 | 1983-07-05 | Syva Company | Test strip kits in immunoassays and compositions therein |
| EP1932843A1 (en) * | 2006-12-14 | 2008-06-18 | sanofi-aventis | Sulfonyl-phenyl-2H-(1,2,4) oxadiazole-5-one derivatives, processes for their preparation and their use as pharmaceuticals |
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2013
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- 2013-05-24 EP EP24192650.0A patent/EP4434584A3/en active Pending
- 2013-05-24 EP EP18154256.4A patent/EP3338781B1/en active Active
- 2013-05-24 DK DK22193438.3T patent/DK4119561T3/da active
- 2013-05-24 ES ES13793417.0T patent/ES2665338T3/es active Active
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- 2013-05-24 MY MYPI2014003289A patent/MY172739A/en unknown
- 2013-05-24 PL PL21154665.0T patent/PL3851107T3/pl unknown
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2014
- 2014-11-10 ZA ZA2014/08182A patent/ZA201408182B/en unknown
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2018
- 2018-07-23 HK HK18109510.2A patent/HK1250014B/en unknown
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4963558A (en) | 1988-12-08 | 1990-10-16 | Lilly Industries Limited | Pyrazolo-[3,4-g]isoquinoline derivatives useful to treat CNS disorders |
| WO2005087769A1 (en) | 2004-03-09 | 2005-09-22 | Corcept Therapeutics, Inc. | Fused ring azadecalin glucocorticoid receptor modulators |
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| US12226412B2 (en) | 2012-05-25 | 2025-02-18 | Corcept Therapeutics, Inc. | Heteroaryl-ketone fused azadecalin glucocorticoid receptor modulators |
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