SG11201811712QA - 5,7-dihydro-pyrrolo-pyridine derivatives for treating neurological and neurodegenerative diseases - Google Patents
5,7-dihydro-pyrrolo-pyridine derivatives for treating neurological and neurodegenerative diseasesInfo
- Publication number
- SG11201811712QA SG11201811712QA SG11201811712QA SG11201811712QA SG11201811712QA SG 11201811712Q A SG11201811712Q A SG 11201811712QA SG 11201811712Q A SG11201811712Q A SG 11201811712QA SG 11201811712Q A SG11201811712Q A SG 11201811712QA SG 11201811712Q A SG11201811712Q A SG 11201811712QA
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- CSIRALAEFSXNQJ-UHFFFAOYSA-N C1CN=C2C=CN=C2C1 Chemical class C1CN=C2C=CN=C2C1 CSIRALAEFSXNQJ-UHFFFAOYSA-N 0.000 title abstract 2
- 230000000926 neurological effect Effects 0.000 title abstract 2
- 208000012902 Nervous system disease Diseases 0.000 title 1
- 208000025966 Neurological disease Diseases 0.000 title 1
- 230000004770 neurodegeneration Effects 0.000 title 1
- 208000015122 neurodegenerative disease Diseases 0.000 title 1
- 102220240796 rs553605556 Human genes 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 150000001204 N-oxides Chemical class 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 206010012335 Dependence Diseases 0.000 abstract 1
- 238000006143 Gilbert reaction Methods 0.000 abstract 1
- 230000001149 cognitive effect Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 208000019116 sleep disease Diseases 0.000 abstract 1
- 208000020685 sleep-wake disease Diseases 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
Classifications
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- 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
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Physical Education & Sports Medicine (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1 MI 11111 0 11101 010 11111 01 110 1 0 011101 1101 010 11111 100 110 11110 MAMIE Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\"\"1 WO 2018/002760 Al 04 January 2018 (04.01.2018) W I PO I PCT (51) International Patent Classification: (84) Designated States (unless otherwise indicated, for every C07D 471/04 (2006.01) A61P 25/16 (2006.01) kind of regional protection available): ARIPO (BW, GH, A61K 31/437 (2006.01) A61P 25/18 (2006.01) GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, A61P 25/00 (2006.01) A61P 25/28 (2006.01) UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (21) International Application Number: TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, PCT/IB2017/053565 EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (22) International Filing Date: TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, 15 June 2017 (15.06.2017) KM, ML, MR, NE, SN, TD, TG). (25) Filing Language: English Declarations under Rule 4.17: (26) Publication Language: English — as to the identity of the inventor (Rule 4.17(i) — as to applicant's entitlement to apply for and be granted a (30) Priority Data: patent (Rule 4.17(ii)) 62/357,624 01 July 2016 (01.07.2016) US — as to the applicant's entitlement to claim the priority of the 62/372,421 09 August 2016 (09.08.2016) US earlier application (Rule 4.17(iii)) (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, Published: New York, NY 10017 (US). — with international search report (Art. 21(3)) (72) Inventors: ZHANG, Lei; 75 Bourne Street, Auburndale, MA 02466 (US). BUTLER, Christopher Ryan; 121 Spring Lane, Canton, MA 02021 (US). BECK, Elizabeth Mary; 27A Botley Road, Oxford, Oxfordshire OX2 OBN (GB). BRODNEY, Michael Aaron; 100 Upland Ave., Newton, MA 02461 (US). BROWN, Matthew Frank; 443 Wheeler Road, Stonington, CT 06378 (US). MCAL- LISTER, Laura Ann; 428 Massachusetts Ave., Apt. 6, Ar- lington, MA 02474 (US). LACHAPELLE, Erik Alphie; 69 Richard Brown Drive, Uncasville, CT 06382 (US). GIL- BERT, Adam Matthew; 178 Denison Drive, Guilford, CT 06437 (US). Agent: WALDRON, Roy F.; Pfizer Inc., 235 East 42nd (74) Street, MS 235/9/S20, New York, NY 10017 (US). Designated States (unless otherwise indicated, for every = (81) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. Il ..! (54) Title: 5,7-DIHYDRO-PYRROLO-PYRIDINE DERIVATIVES FOR TREATING NEUROLOGICAL AND NEURODEGEN- ERATWE DISEASES SO (57) : The present invention provides, in part, compounds of Formula N (R), (I): or an N-oxide thereof, or a pharmaceutically acceptable salt of the compound 0 \ 0 ...„, -.....------Y (R 2 )b 0 \......... or the N- oxide, wherein: R 1 , R 2 , L, A, and E are as described herein; process- --.... 1 \N (I) es for the preparation of; intermediates used in the preparation of; and composi- tions containing such compounds, N-oxides, or salts, and their uses for treating 0 C: N N -----'-1 M4-mediated (or M4- associated) disorders including, e.g., Alzheimer's Disease, L—A—E schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662357624P | 2016-07-01 | 2016-07-01 | |
| US201662372421P | 2016-08-09 | 2016-08-09 | |
| PCT/IB2017/053565 WO2018002760A1 (en) | 2016-07-01 | 2017-06-15 | 5,7-dihydro-pyrrolo-pyridine derivatives for treating neurological and neurodegenerative diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201811712QA true SG11201811712QA (en) | 2019-01-30 |
Family
ID=59215839
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201811712QA SG11201811712QA (en) | 2016-07-01 | 2017-06-15 | 5,7-dihydro-pyrrolo-pyridine derivatives for treating neurological and neurodegenerative diseases |
Country Status (20)
| Country | Link |
|---|---|
| US (5) | US10604519B2 (en) |
| EP (2) | EP3478679B1 (en) |
| JP (1) | JP7046018B2 (en) |
| KR (1) | KR102470497B1 (en) |
| CN (1) | CN109641898B (en) |
| AU (1) | AU2017286868B2 (en) |
| CA (1) | CA2972070A1 (en) |
| DK (1) | DK3478679T3 (en) |
| ES (1) | ES2878160T3 (en) |
| HU (1) | HUE054857T2 (en) |
| IL (1) | IL263912B (en) |
| MX (1) | MX386258B (en) |
| PH (1) | PH12019500004A1 (en) |
| PL (1) | PL3478679T3 (en) |
| PT (1) | PT3478679T (en) |
| SG (1) | SG11201811712QA (en) |
| TW (1) | TWI736642B (en) |
| UY (1) | UY37311A (en) |
| WO (1) | WO2018002760A1 (en) |
| ZA (1) | ZA201900519B (en) |
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| US10945771B2 (en) | 2017-06-09 | 2021-03-16 | Merck Sharp & Dohme Corp. | Azabicyclo[4.1.0]heptane allosteric modulators of the M4 muscarinic acetylcholine receptor |
| JP7263266B2 (en) | 2017-06-22 | 2023-04-24 | ファイザー・インク | Dihydro-pyrrolo-pyridine derivatives |
| EP3870292A4 (en) | 2018-10-26 | 2022-11-09 | The Research Foundation for The State University of New York | COMBINATION OF SEROTONIN-SPECIFIC RESUPPUT INHIBITOR AND SEROTONIN 1A RECEPTOR PARTIAL AGONIST TO REDUCE L-DOPA-INDUCED DYSKINESIA |
| WO2021099527A1 (en) | 2019-11-22 | 2021-05-27 | F. Hoffmann-La Roche Ag | Pyrrolidine derivatives |
| EP4143196A4 (en) * | 2020-04-29 | 2024-04-17 | Relay Therapeutics, Inc. | PI3K-A INHIBITORS AND METHODS OF USE THEREOF |
| CN112174869B (en) * | 2020-10-12 | 2023-04-25 | 蔡霈 | Preparation method and medicinal use of N-phenylacetyl-2-hydroxymethylpyrrolidine-2-carboxamide |
| US20220354862A1 (en) * | 2021-05-04 | 2022-11-10 | Mind Medicine, Inc. | Liposome delivery of psychedelics |
| AU2023343985A1 (en) * | 2022-09-23 | 2025-05-08 | Cerevel Therapeutics, Llc | Crystal form of emraclidine, preparation method therefor, and use thereof |
| TW202432557A (en) * | 2022-10-28 | 2024-08-16 | 大陸商紐歐申醫藥（上海）有限公司 | Nitrogen-containing heterocyclic compound, pharmaceutically acceptable salt thereof and preparation method and application thereof |
| KR20250133677A (en) * | 2022-12-16 | 2025-09-08 | 카루나 세러퓨틱스 인코포레이티드 | Substituted dihydropyrrolo[3,4-D]pyrimidine compounds and their use in the treatment of medical conditions |
| WO2024130064A1 (en) * | 2022-12-16 | 2024-06-20 | Karuna Therapeutics, Inc. | Substituted tetrahydropyrrolo-pyridinone compounds and their use in treating medical conditions |
| AU2023398924A1 (en) * | 2022-12-16 | 2025-06-26 | Karuna Therapeutics, Inc. | Substituted tetrahydropyrrolo-pyridinone compounds and their use in treating medical conditions |
| KR20250130621A (en) * | 2022-12-16 | 2025-09-02 | 카루나 세러퓨틱스 인코포레이티드 | Substituted dihydropyrrolo[3,4-D]pyrimidine compounds and their use in the treatment of medical conditions |
| WO2024230794A1 (en) * | 2023-05-11 | 2024-11-14 | 中国药科大学 | Azetidine derivative, preparation method therefor and medical use thereof |
| CN116693437A (en) * | 2023-06-15 | 2023-09-05 | 安徽大学 | A kind of synthetic method of N-Boc-3-azetidine acetic acid |
| WO2024260386A1 (en) * | 2023-06-20 | 2024-12-26 | 西藏海思科制药有限公司 | Muscarinic m4 receptor agonist and use thereof |
| WO2025055965A1 (en) * | 2023-09-13 | 2025-03-20 | 中国药科大学 | Azetidine derivative, and preparation method therefor and pharmaceutical use thereof |
| WO2025055970A1 (en) * | 2023-09-15 | 2025-03-20 | 江苏恩华药业股份有限公司 | Azetidine derivative, preparation method therefor, and pharmaceutical use thereof |
| WO2025083630A1 (en) | 2023-10-19 | 2025-04-24 | Suven Life Sciences Limited | Heteroaromatic compounds as muscarinic m4 receptor positive allosteric modulators (m4 pams) |
| WO2025099660A1 (en) | 2023-11-10 | 2025-05-15 | Suven Life Sciences Limited | Piperidine substituted compounds as muscarinic m4 receptor positive allosteric modulators (m4 pams) |
| WO2025103475A1 (en) * | 2023-11-17 | 2025-05-22 | 上海翰森生物医药科技有限公司 | Heterocyclic carbonyl derivative modulator, preparation method therefor, and use thereof |
| TW202527956A (en) * | 2023-12-07 | 2025-07-16 | 美商阿卡蒂亞藥品公司 | M4 positive allosteric modulators |
| WO2025134078A1 (en) | 2023-12-22 | 2025-06-26 | Suven Life Sciences Limited | Organic compounds as muscarinic m4 receptor positive allosteric modulators (m4 pams) |
| WO2025140364A1 (en) * | 2023-12-27 | 2025-07-03 | 宜昌人福药业有限责任公司 | Fused pyrimidine ring compound, pharmaceutical composition, and use thereof |
| WO2025145091A1 (en) | 2023-12-29 | 2025-07-03 | Pfizer Inc. | Crystalline forms of a muscarinic m4 receptor modulator and methods of treating diseases |
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