SG11201806416XA - Tetrahydroisoquinoline derivatives - Google Patents
Tetrahydroisoquinoline derivativesInfo
- Publication number
- SG11201806416XA SG11201806416XA SG11201806416XA SG11201806416XA SG11201806416XA SG 11201806416X A SG11201806416X A SG 11201806416XA SG 11201806416X A SG11201806416X A SG 11201806416XA SG 11201806416X A SG11201806416X A SG 11201806416XA SG 11201806416X A SG11201806416X A SG 11201806416XA
- Authority
- SG
- Singapore
- Prior art keywords
- honcho
- nihonbashi
- chome
- chuo
- tokyo
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/20—Spiro-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/24—Oxygen atoms
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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
- A61K31/47—Quinolines; Isoquinolines
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- 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
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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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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- 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
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N5/00—Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
- C12N5/06—Animal cells or tissues; Human cells or tissues
- C12N5/0602—Vertebrate cells
- C12N5/0652—Cells of skeletal and connective tissues; Mesenchyme
- C12N5/0658—Skeletal muscle cells, e.g. myocytes, myotubes, myoblasts
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2509/00—Methods for the dissociation of cells, e.g. specific use of enzymes
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N2509/00—Methods for the dissociation of cells, e.g. specific use of enzymes
- C12N2509/10—Mechanical dissociation
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Biotechnology (AREA)
- Heart & Thoracic Surgery (AREA)
- Genetics & Genomics (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Hospice & Palliative Care (AREA)
- Cell Biology (AREA)
- Child & Adolescent Psychology (AREA)
- General Engineering & Computer Science (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
3000 g 2000 .S 0 2 1000 0 N=9/group mean ± SEM *p<0.05, vs. vehicle paired t-test Vehicle 1 mg/kg 3 mg/kg Exam ple 20 3000- 5 2000- +, Vehicle 3 mg/kg Example 22b W O 20 17 / 1395 26 Al 0 1000- 0 N=16/group mean ± SEM *p<0.05, paired t-test (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/139526 Al 17 August 2017 (17.08.2017) WIPO I PCT 11111111111111011101111111111101011111011101110111111111111111111111111111111110111111 (51) International Patent Classification: A61K 31/47 (2006.01) CO7D 217/08 (2006.01) (21) International Application Number: PCT/US2017/017295 (22) International Filing Date: 10 February 2017 (10.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/285,039 12 February 2016 (12.02.2016) US (71) Applicants: ASTELLAS PHARMA INC. [US/US]; 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (US). CYTOKINETICS, INCORPORATED [US/US]; 280 East Grand Avenue, South San Francisco, CA 94080 (US). (72) Inventors: SATO, Ippei; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (JP). KAMIKUBO, Takashi; C/o Astellas Pharma Inc., 5- 1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103- 8411 (JP). MIURA, Masanori; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103- 8411 (JP). MATSUSHIMA, Yuji; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (JP). TANAKA, Hiroaki; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (JP). SHIINA, Yasuhiro; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (JP). YAMAKI, Susumu; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (JP). SAITO, Tomoyuki; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (JP). KIYOHARA, Hiroshi; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (JP). OHE, Munemichi; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (JP). MIHARA, Kayoko; C/o Astellas Pharma Inc., 5-1, Nihonbashi-honcho 2-chome, Chuo-ku, Tokyo, 103-8411 (JP). MORGAN, Bradley, Paul; 1206 Rimer Drive, Moraga, CA 94556 (US). MALIK, Fady; 2884 Hillside Drive, Burlingame, CA 94010 (US). COL- LIBEE, Scott, Emile; 2065 Brittan Avenue, San Carlos, CA 94070 (US). ASHCRAFT, Luke; 668 Caroline Street, San Francisco, CA 94107 (US). LU, Pu-Ping; 1017 Flying Fish Street, Foster City, CA 94404 (US). WARRING- TON, Jeffrey, Michael; 1936 Playa Street, San Mateo, [Continued on next page] (54) Title: TETRAHYDROISOQUINOLINE DERIVATIVES FIG. 1 (57) : Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sar- comere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) dis- orders of voluntary muscle, 3) CNS disorders in which muscle weak- ness, atrophy, and fatigue are prominent symptoms, 4) muscle symp- toms stemming from systemic disorders, and 5) dysfunctions of pel- vic floor and urethral/anal sphincter muscle. 4000- WO 2017/139526 Al MIDEDIMOMOIDIONOIDEMOMMIHIHIMIROMEHOIS CA 94403 (US). GARARD, Marc; 16745 Kildare Road, San Leandro, CA 94578 (US). (74) Agents: BAXTER, Stephen, G. et al.; Oblon, McClel- land, Maier & Neustadt, L.L.P., 1940 Duke Street, Alex- andria, VA 22314 (US). (81) Designated States (unless otherwise indicated, for every 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, 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. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, 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, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: with international search report (Art. 2 1 (3)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h))
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662285039P | 2016-02-12 | 2016-02-12 | |
| PCT/US2017/017295 WO2017139526A1 (en) | 2016-02-12 | 2017-02-10 | Tetrahydroisoquinoline derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201806416XA true SG11201806416XA (en) | 2018-08-30 |
Family
ID=59561239
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201806416XA SG11201806416XA (en) | 2016-02-12 | 2017-02-10 | Tetrahydroisoquinoline derivatives |
Country Status (32)
| Country | Link |
|---|---|
| US (5) | US9914741B2 (en) |
| EP (2) | EP3413892B1 (en) |
| JP (2) | JP6832943B2 (en) |
| KR (1) | KR20180120701A (en) |
| CN (2) | CN109069498B (en) |
| AR (1) | AR107592A1 (en) |
| AU (1) | AU2017217663B2 (en) |
| BR (1) | BR112018016475A2 (en) |
| CA (1) | CA3012839A1 (en) |
| CL (1) | CL2018002287A1 (en) |
| CO (1) | CO2018007920A2 (en) |
| DK (1) | DK3413892T3 (en) |
| ES (1) | ES2913423T3 (en) |
| HR (1) | HRP20220655T1 (en) |
| HU (1) | HUE058820T2 (en) |
| IL (1) | IL261055B (en) |
| LT (1) | LT3413892T (en) |
| MA (1) | MA44018B1 (en) |
| MD (1) | MD3413892T2 (en) |
| MX (1) | MX2018009759A (en) |
| NZ (1) | NZ746311A (en) |
| PH (1) | PH12018501694A1 (en) |
| PL (1) | PL3413892T3 (en) |
| PT (1) | PT3413892T (en) |
| RS (1) | RS63240B1 (en) |
| RU (1) | RU2743424C2 (en) |
| SG (1) | SG11201806416XA (en) |
| SI (1) | SI3413892T1 (en) |
| TW (2) | TWI719138B (en) |
| UA (1) | UA124879C2 (en) |
| WO (1) | WO2017139526A1 (en) |
| ZA (1) | ZA201804947B (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20220655T1 (en) * | 2016-02-12 | 2022-06-24 | Cytokinetics, Incorporated | Tetrahydroisoquinoline derivatives |
| WO2022099011A1 (en) | 2020-11-06 | 2022-05-12 | Cytokinetics, Inc. | Bicyclic 1,4-diazepanones and therapeutic uses thereof |
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| HRP20220655T1 (en) * | 2016-02-12 | 2022-06-24 | Cytokinetics, Incorporated | Tetrahydroisoquinoline derivatives |
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2017
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2018
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2019
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2020
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