CN105473548B - 作为溶血磷脂酸受体拮抗剂的酰胺衍生物 - Google Patents

作为溶血磷脂酸受体拮抗剂的酰胺衍生物 Download PDF

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Publication number
CN105473548B
CN105473548B CN201480046178.8A CN201480046178A CN105473548B CN 105473548 B CN105473548 B CN 105473548B CN 201480046178 A CN201480046178 A CN 201480046178A CN 105473548 B CN105473548 B CN 105473548B
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methyl
benzoic acid
benzamido
fluorophenoxies
methoxyphenoxies
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Expired - Fee Related
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Chinese (zh)
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CN105473548A (zh
Inventor
W.巴夫汉
H.坎宁
R.达文波特
W.法纳比
S.麦克
A.帕马尔
S.怀特
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Takeda Pharmaceutical Co Ltd
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Takeda Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/46—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/52—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/04—Systems containing only non-condensed rings with a four-membered ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
CN201480046178.8A 2013-08-20 2014-08-20 作为溶血磷脂酸受体拮抗剂的酰胺衍生物 Expired - Fee Related CN105473548B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1314926.5 2013-08-20
GBGB1314926.5A GB201314926D0 (en) 2013-08-20 2013-08-20 Novel Compounds
PCT/GB2014/052558 WO2015025164A1 (en) 2013-08-20 2014-08-20 Amide derivatives as lysophosphatidic acid receptor antagonists

Publications (2)

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CN105473548A CN105473548A (zh) 2016-04-06
CN105473548B true CN105473548B (zh) 2018-03-23

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CN201480046178.8A Expired - Fee Related CN105473548B (zh) 2013-08-20 2014-08-20 作为溶血磷脂酸受体拮抗剂的酰胺衍生物

Country Status (24)

Country Link
US (3) US9464060B2 (https=)
EP (1) EP3036215A1 (https=)
JP (1) JP6422974B2 (https=)
KR (1) KR20160045797A (https=)
CN (1) CN105473548B (https=)
AR (1) AR097403A1 (https=)
AU (1) AU2014310404B2 (https=)
CA (1) CA2921742A1 (https=)
CL (1) CL2016000387A1 (https=)
CR (1) CR20160084A (https=)
EA (1) EA028818B1 (https=)
GB (1) GB201314926D0 (https=)
HK (1) HK1225712A1 (https=)
IL (1) IL243780A0 (https=)
MA (1) MA38854B1 (https=)
MX (1) MX2016001896A (https=)
PE (1) PE20160284A1 (https=)
PH (1) PH12016500322A1 (https=)
SG (1) SG11201601250TA (https=)
TN (1) TN2016000061A1 (https=)
TW (1) TW201536722A (https=)
UY (1) UY35708A (https=)
WO (1) WO2015025164A1 (https=)
ZA (1) ZA201600753B (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201314926D0 (en) * 2013-08-20 2013-10-02 Takeda Pharmaceutical Novel Compounds
US20210393621A1 (en) 2018-10-26 2021-12-23 The Research Foundation For The State University Of New York Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia
CN119823001A (zh) 2019-07-30 2025-04-15 大正制药株式会社 拮抗lpa1受体的脲化合物
AU2020384883B2 (en) 2019-11-15 2023-11-16 Gilead Sciences, Inc. Triazole carbamate pyridyl sulfonamides as LPA receptor antagonists and uses thereof
TWI843503B (zh) 2020-06-03 2024-05-21 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
CN115867556B (zh) 2020-06-03 2025-05-06 吉利德科学公司 Lpa受体拮抗剂及其用途
TWI853704B (zh) 2021-05-11 2024-08-21 美商基利科學股份有限公司 Lpa受體拮抗劑及其用途
KR20240007233A (ko) 2021-05-13 2024-01-16 길리애드 사이언시즈, 인코포레이티드 Lpa 수용체 길항제 및 이의 용도
WO2023107938A1 (en) 2021-12-08 2023-06-15 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
EP4724096A1 (en) * 2023-06-06 2026-04-15 GPCR Therapeutics, Inc. Gpcr inhibitors and uses thereof

Citations (2)

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Publication number Priority date Publication date Assignee Title
FR2707641B1 (fr) * 1993-07-16 1995-08-25 Fournier Ind & Sante Composés de l'imidazol-5-carboxamide, leur procédé de préparation leurs intermédiaires et leur utilisation en thérapeutique.
EP1550461A1 (en) * 2002-06-26 2005-07-06 Ono Pharmaceutical Co., Ltd. Remedy for chronic disease

Family Cites Families (10)

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Publication number Priority date Publication date Assignee Title
ES2239203T3 (es) 2001-01-31 2005-09-16 Pfizer Products Inc. Derivados nicotinamida y sus mimeticos como inhibidores de isozimas pde4.
DE10110749A1 (de) 2001-03-07 2002-09-12 Bayer Ag Substituierte Aminodicarbonsäurederivate
JP4691988B2 (ja) * 2002-10-03 2011-06-01 小野薬品工業株式会社 Ｌｐａ受容体拮抗剤
WO2011017350A2 (en) * 2009-08-04 2011-02-10 Amira Pharmaceuticals, Inc. Compounds as lysophosphatidic acid receptor antagonists
BR112012006686B8 (pt) 2009-09-25 2021-05-25 Astellas Pharma Inc compostos de amida substituída, composições farmacêuticas contendo os ditos compostos, e uso dos mesmos para prevenir e/ou tratar doenças causadas pelo lpa
GB2474748B (en) 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
PH12012500542A1 (en) 2010-09-24 2012-11-12 Astellas Pharma Inc Substituted amide compound
US8785442B2 (en) * 2011-01-30 2014-07-22 Curegenix, Inc. Compound as antagonist of lysophosphatidic acid receptor, composition, and use thereof
EP2765128A1 (en) * 2013-02-07 2014-08-13 Almirall, S.A. Substituted benzamides with activity towards EP4 receptors
GB201314926D0 (en) * 2013-08-20 2013-10-02 Takeda Pharmaceutical Novel Compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2707641B1 (fr) * 1993-07-16 1995-08-25 Fournier Ind & Sante Composés de l'imidazol-5-carboxamide, leur procédé de préparation leurs intermédiaires et leur utilisation en thérapeutique.
EP1550461A1 (en) * 2002-06-26 2005-07-06 Ono Pharmaceutical Co., Ltd. Remedy for chronic disease

Also Published As

Publication number Publication date
ZA201600753B (en) 2019-07-31
US20190010129A1 (en) 2019-01-10
GB201314926D0 (en) 2013-10-02
JP2016528274A (ja) 2016-09-15
TN2016000061A1 (en) 2017-07-05
AR097403A1 (es) 2016-03-09
CL2016000387A1 (es) 2016-12-16
CN105473548A (zh) 2016-04-06
CR20160084A (es) 2016-05-27
TW201536722A (zh) 2015-10-01
AU2014310404B2 (en) 2018-07-12
US10100018B2 (en) 2018-10-16
US20160207880A1 (en) 2016-07-21
UY35708A (es) 2014-12-31
CA2921742A1 (en) 2015-02-26
EA201690390A1 (ru) 2016-08-31
MX2016001896A (es) 2016-05-26
MA38854A1 (fr) 2017-07-31
EA028818B1 (ru) 2018-01-31
JP6422974B2 (ja) 2018-11-14
KR20160045797A (ko) 2016-04-27
EP3036215A1 (en) 2016-06-29
MA38854B1 (fr) 2018-05-31
PE20160284A1 (es) 2016-04-27
SG11201601250TA (en) 2016-03-30
AU2014310404A1 (en) 2016-03-10
US20150057298A1 (en) 2015-02-26
HK1225712A1 (zh) 2017-09-15
US9464060B2 (en) 2016-10-11
WO2015025164A1 (en) 2015-02-26
PH12016500322A1 (en) 2016-05-02
IL243780A0 (en) 2016-04-21

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