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PE20161572A1 - Compuestos como moduladores de ror gamma - Google Patents

Compuestos como moduladores de ror gamma

Info

Publication number
PE20161572A1
PE20161572A1 PE2016001963A PE2016001963A PE20161572A1 PE 20161572 A1 PE20161572 A1 PE 20161572A1 PE 2016001963 A PE2016001963 A PE 2016001963A PE 2016001963 A PE2016001963 A PE 2016001963A PE 20161572 A1 PE20161572 A1 PE 20161572A1
Authority
PE
Peru
Prior art keywords
compounds
alkyl
ror gamma
arylus
heteroaryl
Prior art date
Application number
PE2016001963A
Other languages
English (en)
Inventor
Qiang Zhang
Lifen Wu
Michael Robert Turner
Robert Sibley
Johanna Bakonyi
Xiang Li
Robert Owen Hughes
Delphine Collin
Steven Richard Brunette
Shuang Liang
Original Assignee
Boehringer Ingelheim Int
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20161572A1 publication Critical patent/PE20161572A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/10—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with an aromatic or hetero-aromatic ring directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Otolaryngology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PTERIDINA-7(8H)-ONA DE FORMULA (I) DONDE R1 ES -CN, -S(O)nR6, ENTRE OTROS; R2 Y R3 SON CADA UNO H, ALQUILO C1-C3 OPCIONALMENTE SUSTITUIDO, ENTRE OTROS; O R2 Y R3 JUNTO CON EL CARBONO AL QUE SE UNEN FORMAN UN ANILLO CARBOCICLICO C3-C6, UN ANILLO HETEROCICLICLO C3-C6, ENTRE OTROS; R4 ES ALQUILO C1-C6, CICLOALQUILO C3-C12, ENTRE OTROS; R5 ES ARILO, HETEROARILO, ENTRE OTROS; W ES ARILO, HETEROARILO, ENTRE OTROS; R6 ES -OH, ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO, ENTRE OTROS; n ES DE 0 A 2. SON COMPUESTOS PREFERIDOS LOS DE FORMULA (A), (B), ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE ACIDO RETINOICO RELACIONADO CON EL RECEPTOR HUERFANO GAMMA (ROR GAMMA) SIENDO UTILES EN EL TRATAMIENTO DE ARTRITIS REUMATOIDEA, PSORIASIS, LUPUS NEFRITICO
PE2016001963A 2014-04-14 2015-04-10 Compuestos como moduladores de ror gamma PE20161572A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461979231P 2014-04-14 2014-04-14

Publications (1)

Publication Number Publication Date
PE20161572A1 true PE20161572A1 (es) 2017-02-01

Family

ID=52998264

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2016001963A PE20161572A1 (es) 2014-04-14 2015-04-10 Compuestos como moduladores de ror gamma
PE2020001484A PE20211002A1 (es) 2014-04-14 2015-04-10 Compuestos como moduladores de ror gamma

Family Applications After (1)

Application Number Title Priority Date Filing Date
PE2020001484A PE20211002A1 (es) 2014-04-14 2015-04-10 Compuestos como moduladores de ror gamma

Country Status (35)

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US (5) US9242989B2 (es)
EP (2) EP3131902B1 (es)
JP (2) JP6282759B2 (es)
KR (2) KR102410076B1 (es)
CN (3) CN106132965B (es)
AP (1) AP2016009403A0 (es)
AR (2) AR100058A1 (es)
AU (2) AU2015247983B2 (es)
BR (2) BR112016021962A2 (es)
CA (1) CA2944787C (es)
CL (1) CL2016002421A1 (es)
CY (1) CY1122012T1 (es)
DK (1) DK3131902T3 (es)
EA (2) EA031351B1 (es)
ES (1) ES2744299T3 (es)
HR (1) HRP20191579T1 (es)
HU (1) HUE045847T2 (es)
IL (2) IL247419B (es)
LT (1) LT3131902T (es)
MA (1) MA46373A (es)
ME (1) ME03513B (es)
MX (1) MX370780B (es)
MY (1) MY182834A (es)
NZ (1) NZ723530A (es)
PE (2) PE20161572A1 (es)
PH (2) PH12016502019B1 (es)
PL (1) PL3131902T3 (es)
PT (1) PT3131902T (es)
RS (1) RS59170B1 (es)
SG (1) SG11201608537SA (es)
SI (1) SI3131902T1 (es)
TW (2) TWI652268B (es)
UA (2) UA120094C2 (es)
UY (1) UY36077A (es)
WO (1) WO2015160654A1 (es)

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CN108026045B (zh) 2015-05-15 2021-04-27 奥瑞基尼探索技术有限公司 用作RORγ调节剂的经过取代的四氢喹啉酮化合物
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JP6448867B2 (ja) 2015-12-15 2019-01-09 アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ イソインドール化合物
WO2017127375A1 (en) * 2016-01-20 2017-07-27 Boehringer Ingelheim International Gmbh Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma
TWI705958B (zh) 2016-12-05 2020-10-01 荷蘭商領導醫藥控股責任有限公司 ＲＯＲγ調節子
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JP2022504780A (ja) 2018-10-18 2022-01-13 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 光学活性１－シクロプロピルアルキル－１－アミンのスケーラブルな合成
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TW202118751A (zh) 2019-10-31 2021-05-16 大陸商江蘇恒瑞醫藥股份有限公司 RORγ調節劑的酸加成鹽
WO2022106547A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Process for synthesising a ror gamma inhibitor
WO2022106551A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Co-crystals of a ror gamma inhibitor
WO2022106548A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Solid forms of a ror gamma inhibitor
WO2022106550A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Crystalline polymorphic form of a ror gamma inhibitor
WO2022106549A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Crystalline salts of a ror gamma inhibitor
WO2023216910A1 (zh) * 2022-05-07 2023-11-16 苏州浦合医药科技有限公司 取代的双环杂芳基化合物作为usp1抑制剂
WO2023232870A1 (en) 2022-05-31 2023-12-07 Immunic Ag Rorg/rorgt modulators for the treatment of virus infections like covid-19
CN116178279A (zh) * 2023-03-15 2023-05-30 上海药坦药物研究开发有限公司 一种5-溴-4-环丙基-6-甲氧基嘧啶及其中间体的制备方法
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WO2017127375A1 (en) * 2016-01-20 2017-07-27 Boehringer Ingelheim International Gmbh Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma

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WO2015160654A1 (en) 2015-10-22
AP2016009403A0 (en) 2016-08-31
US20160075706A1 (en) 2016-03-17
MA46373A (fr) 2019-08-07
EA201890329A1 (ru) 2018-07-31
JP6463855B2 (ja) 2019-02-06
UA121255C2 (uk) 2020-04-27
MX370780B (es) 2020-01-03
EP3418280B1 (en) 2023-07-12
US20190002465A1 (en) 2019-01-03
JP6282759B2 (ja) 2018-02-21
IL247419B (en) 2019-03-31
IL263878A (en) 2019-01-31
US20180022749A1 (en) 2018-01-25
SG11201608537SA (en) 2016-11-29
AU2015247983B2 (en) 2019-05-16
EA035063B1 (ru) 2020-04-23
CY1122012T1 (el) 2020-10-14
AU2019203027B2 (en) 2020-07-09
KR102410069B1 (ko) 2022-06-20
HK1244800A1 (zh) 2018-08-17
AR100058A1 (es) 2016-09-07
US20150291607A1 (en) 2015-10-15
DK3131902T3 (da) 2019-09-02
HRP20191579T1 (hr) 2019-11-29
CN107266450A (zh) 2017-10-20
NZ723530A (en) 2023-05-26
UA120094C2 (uk) 2019-10-10
RS59170B1 (sr) 2019-10-31
IL263878B (en) 2019-11-28
EP3131902B1 (en) 2019-06-12
JP2017511357A (ja) 2017-04-20
LT3131902T (lt) 2019-09-25
CA2944787A1 (en) 2015-10-22
EA201691978A1 (ru) 2017-02-28
BR112016021962B1 (pt) 2022-12-13
US9598415B2 (en) 2017-03-21
HK1244801A1 (zh) 2018-08-17
CA2944787C (en) 2023-03-14
PH12016502019B1 (en) 2020-10-23
US20170008894A1 (en) 2017-01-12
AU2019203027A1 (en) 2019-05-23
AU2015247983A1 (en) 2016-09-08
CN107266454A (zh) 2017-10-20
TW201841915A (zh) 2018-12-01
EP3418280A1 (en) 2018-12-26
PH12016502019A1 (en) 2017-01-09
TWI655192B (zh) 2019-04-01
CN107266454B (zh) 2019-08-09
KR102410076B1 (ko) 2022-06-22
CL2016002421A1 (es) 2017-03-24
EA031351B1 (ru) 2018-12-28
MX2016013342A (es) 2017-01-26
PT3131902T (pt) 2019-09-17
EP3131902A1 (en) 2017-02-22
BR112016021962A2 (pt) 2023-01-20
ES2744299T3 (es) 2020-02-24
PH12020500252A1 (en) 2021-07-26
US9242989B2 (en) 2016-01-26
PE20211002A1 (es) 2021-06-01
TW201625622A (zh) 2016-07-16
JP2018065874A (ja) 2018-04-26
AR119454A2 (es) 2021-12-22
SI3131902T1 (sl) 2019-10-30
MY182834A (en) 2021-02-05
PL3131902T3 (pl) 2019-11-29
CN106132965A (zh) 2016-11-16
KR20200040917A (ko) 2020-04-20
CN106132965B (zh) 2020-02-07
KR20160142396A (ko) 2016-12-12
UY36077A (es) 2015-10-30
TWI652268B (zh) 2019-03-01
HUE045847T2 (hu) 2020-01-28
ME03513B (me) 2020-04-20
BR122020020657B1 (pt) 2022-12-20
CN107266450B (zh) 2020-07-24

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