CA2948161C - Pyrrolidine gpr40 modulators for the treatment of diseases such as diabetes - Google Patents

Pyrrolidine gpr40 modulators for the treatment of diseases such as diabetes Download PDF

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Publication number
CA2948161C
CA2948161C CA2948161A CA2948161A CA2948161C CA 2948161 C CA2948161 C CA 2948161C CA 2948161 A CA2948161 A CA 2948161A CA 2948161 A CA2948161 A CA 2948161A CA 2948161 C CA2948161 C CA 2948161C
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substituted
alkyl
independently
occurrence
mmol
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French (fr)
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CA2948161A1 (en
Inventor
Elizabeth A. Jurica
Zhenqiu Hong
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2948161A 2014-05-07 2015-05-06 Pyrrolidine gpr40 modulators for the treatment of diseases such as diabetes Active CA2948161C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461989651P 2014-05-07 2014-05-07
US61/989,651 2014-05-07
PCT/US2015/029409 WO2015171722A1 (en) 2014-05-07 2015-05-06 Pyrrolidine gpr40 modulators for the treatment of diseases such as diabetes

Publications (2)

Publication Number Publication Date
CA2948161A1 CA2948161A1 (en) 2015-11-12
CA2948161C true CA2948161C (en) 2020-10-27

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Family Applications (1)

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CA2948161A Active CA2948161C (en) 2014-05-07 2015-05-06 Pyrrolidine gpr40 modulators for the treatment of diseases such as diabetes

Country Status (33)

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US (4) US9873679B2 (OSRAM)
EP (1) EP3140296B1 (OSRAM)
JP (1) JP6483156B2 (OSRAM)
KR (1) KR102336370B1 (OSRAM)
CN (1) CN106458976B (OSRAM)
AR (1) AR100328A1 (OSRAM)
AU (1) AU2015256120B2 (OSRAM)
BR (1) BR112016024936A2 (OSRAM)
CA (1) CA2948161C (OSRAM)
CL (1) CL2016002809A1 (OSRAM)
CY (1) CY1120340T1 (OSRAM)
DK (1) DK3140296T3 (OSRAM)
EA (1) EA033250B1 (OSRAM)
ES (1) ES2674531T3 (OSRAM)
HR (1) HRP20180641T1 (OSRAM)
HU (1) HUE039288T2 (OSRAM)
IL (1) IL248668B (OSRAM)
MA (1) MA39427B1 (OSRAM)
MX (1) MX378160B (OSRAM)
MY (1) MY181959A (OSRAM)
NZ (1) NZ727146A (OSRAM)
PE (1) PE20161363A1 (OSRAM)
PH (1) PH12016502034B1 (OSRAM)
PL (1) PL3140296T3 (OSRAM)
PT (1) PT3140296T (OSRAM)
RS (1) RS57170B1 (OSRAM)
SG (1) SG11201609170UA (OSRAM)
SI (1) SI3140296T1 (OSRAM)
SM (1) SMT201800342T1 (OSRAM)
TN (1) TN2016000444A1 (OSRAM)
TR (1) TR201809633T4 (OSRAM)
TW (1) TWI659951B (OSRAM)
WO (1) WO2015171722A1 (OSRAM)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR201809633T4 (tr) * 2014-05-07 2018-07-23 Bristol Myers Squibb Co Diyabet gibi hastalıkların tedavisine yönelik pirolidin GPR40 modülatörleri.
KR20170002543A (ko) * 2014-05-07 2017-01-06 브리스톨-마이어스 스큅 컴퍼니 당뇨병과 같은 질환의 치료를 위한 피롤리딘 gpr40 조정제
EP3509588B1 (en) 2016-09-12 2023-06-07 Integral Health,Inc. Bicyclic compounds useful as gpr120 modulators
KR102537985B1 (ko) 2016-09-12 2023-05-30 인테그랄 헬스 인코퍼레이티드 Gpr120 조정제로서 유용한 단환형 화합물
WO2018181847A1 (ja) * 2017-03-31 2018-10-04 武田薬品工業株式会社 芳香環化合物
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
CN107362365B (zh) * 2017-08-21 2020-01-07 武汉大风生物科技有限公司 Gpr31抑制剂在制药中的应用
KR102708681B1 (ko) 2018-02-13 2024-09-26 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
EP4600247A3 (en) 2018-04-19 2025-11-19 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
UA126421C2 (uk) 2018-07-13 2022-09-28 Гіліад Сайєнсіз, Інк. Інгібітори pd-1/pd-l1
US11236085B2 (en) 2018-10-24 2022-02-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CA3217423A1 (en) 2021-06-16 2022-12-22 Jeffrey M. Schkeryantz Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases
CN116283699B (zh) * 2023-03-02 2025-02-11 遵义医科大学 一种合成氟烷基取代的吡咯烷的方法

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US5614492A (en) 1986-05-05 1997-03-25 The General Hospital Corporation Insulinotropic hormone GLP-1 (7-36) and uses thereof
CN102639495A (zh) * 2009-10-06 2012-08-15 百时美施贵宝公司 吡咯烷gpr40调节剂
US7939569B1 (en) * 2009-12-01 2011-05-10 Hoffmann-La Roche Inc. Aniline analogs as glycogen synthase activators
GB2498976A (en) * 2012-02-01 2013-08-07 Prosidion Ltd GPR119 agonists useful in the treatment of type II diabetes
WO2014022253A1 (en) 2012-08-01 2014-02-06 Bristol-Myers Squibb Company Amino-heteroaryl 7-hydroxy-spiropiperidine indolinyl antagonists of p2y1 receptor
KR20150082618A (ko) 2012-11-16 2015-07-15 브리스톨-마이어스 스큅 컴퍼니 디히드로피라졸 gpr40 조절제
US9656963B2 (en) 2012-11-16 2017-05-23 Bristol-Myers Squibb Company Dihydropyrazole GPR40 modulators
HUE032401T2 (en) 2012-11-16 2017-09-28 Bristol Myers Squibb Co Dihydropyrazole GPR40 modulators
BR112015010649A2 (pt) * 2012-11-16 2017-07-11 Bristol Myers Squibb Co moduladores de gpr40 à base de pirrolidina
TR201809633T4 (tr) * 2014-05-07 2018-07-23 Bristol Myers Squibb Co Diyabet gibi hastalıkların tedavisine yönelik pirolidin GPR40 modülatörleri.
WO2015171757A1 (en) 2014-05-07 2015-11-12 Bristol-Myers Squibb Company Pyrrolidine gpr40 modulators
WO2015169728A1 (en) 2014-05-07 2015-11-12 Croma-Pharma Gesellschaft M.B.H. Aqueous ophthalmic solution and method for treating dry eye syndrome

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TR201809633T4 (tr) 2018-07-23
MA39427B1 (fr) 2018-09-28
IL248668B (en) 2019-09-26
US20190112293A1 (en) 2019-04-18
IL248668A0 (en) 2017-01-31
BR112016024936A2 (pt) 2017-08-15
DK3140296T3 (en) 2018-07-23
TWI659951B (zh) 2019-05-21
MX378160B (es) 2025-03-10
PT3140296T (pt) 2018-06-27
US9873679B2 (en) 2018-01-23
AR100328A1 (es) 2016-09-28
KR102336370B1 (ko) 2021-12-06
EP3140296B1 (en) 2018-04-11
HUE039288T2 (hu) 2018-12-28
CN106458976A (zh) 2017-02-22
EA201692037A1 (ru) 2017-06-30
JP2017514856A (ja) 2017-06-08
TW201625585A (zh) 2016-07-16
SMT201800342T1 (it) 2018-09-13
AU2015256120B2 (en) 2019-03-28
ES2674531T3 (es) 2018-07-02
SG11201609170UA (en) 2016-12-29
KR20160147049A (ko) 2016-12-21
EA033250B1 (ru) 2019-09-30
US20200299267A1 (en) 2020-09-24
PL3140296T3 (pl) 2018-08-31
AU2015256120A1 (en) 2016-12-22
MA39427A1 (fr) 2017-11-30
MX2016013801A (es) 2017-03-09
CN106458976B (zh) 2020-05-22
CL2016002809A1 (es) 2017-03-24
SI3140296T1 (en) 2018-06-29
PH12016502034B1 (en) 2022-03-23
WO2015171722A1 (en) 2015-11-12
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JP6483156B2 (ja) 2019-03-13
PE20161363A1 (es) 2016-12-17
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CY1120340T1 (el) 2019-07-10
TN2016000444A1 (en) 2018-04-04
US20180099949A1 (en) 2018-04-12
RS57170B1 (sr) 2018-07-31
HRP20180641T1 (hr) 2018-06-01
US10717725B2 (en) 2020-07-21
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US20150322044A1 (en) 2015-11-12
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