SG11201807074VA - Novel pyrrolidine derivatives - Google Patents

Novel pyrrolidine derivatives

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Publication number
SG11201807074VA
SG11201807074VA SG11201807074VA SG11201807074VA SG11201807074VA SG 11201807074V A SG11201807074V A SG 11201807074VA SG 11201807074V A SG11201807074V A SG 11201807074VA SG 11201807074V A SG11201807074V A SG 11201807074VA SG 11201807074V A SG11201807074V A SG 11201807074VA
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SG
Singapore
Prior art keywords
co7d
grenzacherstrasse
basel
roche
international
Prior art date
Application number
SG11201807074VA
Inventor
Wolfgang Haap
Bernd Kuhn
Thomas Luebbers
Jens-Uwe Peters
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of SG11201807074VA publication Critical patent/SG11201807074VA/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41921,2,3-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41961,2,4-Triazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Title: NOVEL PYRROLIDINE DERIVATIVES F (I) W O 20 17 / 144483 Al (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 2017/144483 Al 31 August 2017 (31.08.2017) WIPO I PCT (51) International Patent Classification: CO7D 403/12 (2006.01) CO7D 401/12 (2006.01) A61K 31/4025 (2006.01) CO7D 403/14 (2006.01) A61K 31/41 (2006.01) CO7D 405/12 (2006.01) A61K 31/4155 (2006.01) CO7D 413/12 (2006.01) A61K 31/4192 (2006.01) CO7D 417/12 (2006.01) A61K 31/4196 (2006.01) CO7D 207/16 (2006.01) A61K 31/422 (2006.01) A61P 3/10 (2006.01) A61K 31/427 (2006.01) A61P 7/00 (2006.01) A61K 31/4439 (2006.01) A61P 7/02 (2006.01) A61K 31/506 (2006.01) (21) International Application Number: PCT/EP2017/053967 (22) International Filing Date: 22 February 2017 (22.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 16157679.8 26 February 2016 (26.02.2016) EP (71) Applicant (for all designated States except US): F. HOFF- MANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124, 4070 Basel (CH). (71) Applicant US only): HOFFMANN-LA ROCHE INC. [US/US]; Overlook at Great Notch, 150 Clove Road, 8th Floor, Suite 8 - Legal Department, Little Falls, New Jersey 07424 (US). (72) Inventors: HAAP, Wolfgang; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). KUHN, Bernd; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). LUEBBERS, Thomas; c/o F. Hoff- mann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). PETERS, Jens-Uwe; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). (74) Agent: POMERANC, Didier; Grenzacherstrasse 124, 4070 Basel (CH). (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, [Continued on next page] 11111111111111011101111111111101011111011101011111111111111111111011111111111110111111 (57) : The invention relates to a compound of for- mula (I) wherein R 1 and R 2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament against diabetes, atherosclerosis and other conditions linked to cathepsin. WO 2017/144483 All#110HOMOIDEIR0101301011101110HEIMODEVOIMIE 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). Declarations under Rule 4.17: of inventorship (Rule 4.17(iv)) Published: with international search report (Art. 21(3))
SG11201807074VA 2016-02-26 2017-02-22 Novel pyrrolidine derivatives SG11201807074VA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16157679 2016-02-26
PCT/EP2017/053967 WO2017144483A1 (en) 2016-02-26 2017-02-22 Novel pyrrolidine derivatives

Publications (1)

Publication Number Publication Date
SG11201807074VA true SG11201807074VA (en) 2018-09-27

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SG11201807074VA SG11201807074VA (en) 2016-02-26 2017-02-22 Novel pyrrolidine derivatives

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US (1) US10689339B2 (en)
EP (1) EP3419970B1 (en)
JP (1) JP6952044B2 (en)
KR (1) KR20180111862A (en)
CN (1) CN108699044B (en)
AR (1) AR107717A1 (en)
AU (1) AU2017224343B2 (en)
CA (1) CA3011652C (en)
CL (1) CL2018002347A1 (en)
CO (1) CO2018007756A2 (en)
CR (1) CR20180404A (en)
DK (1) DK3419970T3 (en)
ES (1) ES2775781T3 (en)
HR (1) HRP20200307T1 (en)
HU (1) HUE047842T2 (en)
IL (1) IL260130B (en)
LT (1) LT3419970T (en)
MA (1) MA43667B1 (en)
MX (1) MX2018009638A (en)
MY (1) MY196560A (en)
PH (1) PH12018501585B1 (en)
PL (1) PL3419970T3 (en)
PT (1) PT3419970T (en)
RS (1) RS59938B1 (en)
RU (1) RU2736498C1 (en)
SG (1) SG11201807074VA (en)
SI (1) SI3419970T1 (en)
TW (1) TWI740903B (en)
UA (1) UA122084C2 (en)
WO (1) WO2017144483A1 (en)
ZA (1) ZA201804120B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7001068B2 (en) 2017-01-24 2022-01-19 アステラス製薬株式会社 Phenyldifluoromethyl substituted proline amide compound
TW202023542A (en) 2018-09-18 2020-07-01 瑞士商赫孚孟拉羅股份公司 Use of a cathepsin s inhibitor against the formation of anti-drug antibodies

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5518997B2 (en) * 2009-04-20 2014-06-11 エフ.ホフマン−ラ ロシュ アーゲー Proline derivatives as cathepsin inhibitors
AU2012334123B2 (en) * 2011-11-11 2016-12-15 F. Hoffmann-La Roche Ag Process for the preparation of 1-acyl-4-phenylsulfonylprolinamide derivatives and new intermediates
US8729061B2 (en) * 2011-11-25 2014-05-20 Hoffmann-La Roche Inc. Pyrrolidine derivatives
US9427108B2 (en) * 2011-12-09 2016-08-30 W.C. Bradley Co. Cooking grate with adjustable heating characteristics
US8802665B2 (en) * 2012-02-17 2014-08-12 Genentech, Inc. Pyrrolidine derivatives
EA025166B1 (en) * 2012-08-21 2016-11-30 Ф. Хоффманн-Ля Рош Аг Pyridine derivatives

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AU2017224343B2 (en) 2020-09-10
DK3419970T3 (en) 2020-03-02
HUE047842T2 (en) 2020-05-28
CL2018002347A1 (en) 2018-11-30
PH12018501585A1 (en) 2019-04-08
IL260130B (en) 2020-08-31
HRP20200307T1 (en) 2020-06-12
RU2736498C1 (en) 2020-11-17
JP2019506416A (en) 2019-03-07
CA3011652A1 (en) 2017-08-31
WO2017144483A1 (en) 2017-08-31
EP3419970A1 (en) 2019-01-02
IL260130A (en) 2018-07-31
MX2018009638A (en) 2018-09-11
ZA201804120B (en) 2020-07-29
MA43667B1 (en) 2020-03-31
US10689339B2 (en) 2020-06-23
AR107717A1 (en) 2018-05-23
CN108699044B (en) 2022-03-04
TWI740903B (en) 2021-10-01
KR20180111862A (en) 2018-10-11
CA3011652C (en) 2024-01-09
ES2775781T3 (en) 2020-07-28
PT3419970T (en) 2020-02-28
PL3419970T3 (en) 2020-06-01
US20180362461A1 (en) 2018-12-20
EP3419970B1 (en) 2020-01-01
SI3419970T1 (en) 2020-04-30
PH12018501585B1 (en) 2019-04-08
UA122084C2 (en) 2020-09-10
CN108699044A (en) 2018-10-23
RS59938B1 (en) 2020-03-31
CR20180404A (en) 2018-10-18
MY196560A (en) 2023-04-19
AU2017224343A1 (en) 2018-07-05
JP6952044B2 (en) 2021-10-20
LT3419970T (en) 2020-03-10
CO2018007756A2 (en) 2018-10-10
TW201733981A (en) 2017-10-01

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