EA201170899A1 - Производные 2-пиридин-2-ил-пиразол-3(2h)-она, их получение и применение в терапии в качестве активаторов hif - Google Patents
Производные 2-пиридин-2-ил-пиразол-3(2h)-она, их получение и применение в терапии в качестве активаторов hifInfo
- Publication number
- EA201170899A1 EA201170899A1 EA201170899A EA201170899A EA201170899A1 EA 201170899 A1 EA201170899 A1 EA 201170899A1 EA 201170899 A EA201170899 A EA 201170899A EA 201170899 A EA201170899 A EA 201170899A EA 201170899 A1 EA201170899 A1 EA 201170899A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- therapy
- aryl
- heterocycloalkyl
- pyrazol
- Prior art date
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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
- C07D401/02—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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- 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
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- 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
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- 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
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- 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
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- 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
- A61P27/06—Antiglaucoma agents or miotics
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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
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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
- A61P3/08—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
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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
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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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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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
- A61P9/08—Vasodilators for multiple indications
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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
- 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
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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
- A61P9/12—Antihypertensives
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
- G01N33/6875—Nucleoproteins
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2500/00—Screening for compounds of potential therapeutic value
- G01N2500/10—Screening for compounds of potential therapeutic value involving cells
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cell Biology (AREA)
- Microbiology (AREA)
- Pathology (AREA)
- General Physics & Mathematics (AREA)
- Biochemistry (AREA)
- Analytical Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biotechnology (AREA)
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Abstract
Изобретение относится к соединениям, соответствующим формуле (I), в которой: R представляет собой -SO-NR3R4, атом водорода, атом галогена, -галоген(С-С)алкил, -COR5 или SOR4; R1 представляет собой гетероциклоалкил, не содержащий атом азота, -W-(C-C)циклоалкил, -W-арил, -W-гетероарил, -W-гетероциклоалкил, -W-COOR5, -W-CONR5R6; R2 представляет собой атом водорода, -(С-С)алкил, -(С-С)алкилен-О-(С-С)алкил, -галоген(С-С)алкил, -W-COOR5, -W-C(О)NHR5 или -W-C(О)NR5R6; n равно 0, 1 или 2; W означает -(С-С)алкилен- или -(C-C)циклоалкилен-; R3 и R4, являющиеся одинаковыми или разными, независимо друг от друга представляют собой такие группы, как атом водорода, -(С-С)алкил, -(C-C)циклоалкил, -(С-С)алкилен-О-(С-С)алкил, арил, -СН-арил, гетероарил, гетероциклоалкил, -W-OH, -W-CHOH-CHOH, -W-COR5, -W-NR5R6 или -W-О-(CH)-арил; или R3 и R4 совместно с атомом азота, с которым они связаны, образуют гетероциклоалкил; R5 и R6, являющиеся одинаковыми или разными, независимо друг от друга представляют собой атомы водорода, -(С-С)алкилы или (С-С)галогеналкилы; изобретение относится также к способу их получения и их применению в терапии.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0807474A FR2940651B1 (fr) | 2008-12-29 | 2008-12-29 | Derives de 2-pyridin-2-yl-pyrazol-3(2h)-one,leur preparation et leur application en therapeutique comme activateurs de hif |
FR0904092A FR2949466A1 (fr) | 2009-08-28 | 2009-08-28 | Derives de 2-pyridin-2-yl-pyrazol-3(2h)-one, leur preparation et leur application en therapeutique comme activateurs de hif |
PCT/FR2009/052691 WO2010076524A2 (fr) | 2008-12-29 | 2009-12-24 | Derives de 2-pyridin-2-yl-pyrazol-3(2h)-one, leur preparation et leur application en therapeutique comme activateurs de hif |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201170899A1 true EA201170899A1 (ru) | 2012-02-28 |
EA019591B1 EA019591B1 (ru) | 2014-04-30 |
Family
ID=42008610
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201170899A EA019591B1 (ru) | 2008-12-29 | 2009-12-24 | Производные 2-пиридин-2-ил-пиразол-3(2h)-она, их получение и применение в терапии в качестве активаторов hif |
Country Status (35)
Country | Link |
---|---|
US (1) | US8541455B2 (ru) |
EP (1) | EP2382205B1 (ru) |
JP (1) | JP5734870B2 (ru) |
KR (1) | KR20110099786A (ru) |
CN (1) | CN102333769B (ru) |
AR (1) | AR074915A1 (ru) |
AU (1) | AU2009334569B2 (ru) |
BR (1) | BRPI0924060A8 (ru) |
CA (1) | CA2748411A1 (ru) |
CL (1) | CL2011001496A1 (ru) |
CO (1) | CO6400141A2 (ru) |
CR (1) | CR20110361A (ru) |
CY (1) | CY1115368T1 (ru) |
DK (1) | DK2382205T3 (ru) |
EA (1) | EA019591B1 (ru) |
EC (1) | ECSP11011155A (ru) |
ES (1) | ES2481042T3 (ru) |
HR (1) | HRP20140680T1 (ru) |
IL (1) | IL213789A (ru) |
MA (1) | MA32976B1 (ru) |
MX (1) | MX2011007054A (ru) |
MY (1) | MY179093A (ru) |
NZ (1) | NZ593751A (ru) |
PA (1) | PA8856201A1 (ru) |
PE (1) | PE20120416A1 (ru) |
PL (1) | PL2382205T3 (ru) |
PT (1) | PT2382205E (ru) |
SG (1) | SG172803A1 (ru) |
SI (1) | SI2382205T1 (ru) |
SM (1) | SMT201400097B (ru) |
TN (1) | TN2011000267A1 (ru) |
TW (1) | TWI482763B (ru) |
UY (1) | UY32369A (ru) |
WO (1) | WO2010076524A2 (ru) |
ZA (1) | ZA201104783B (ru) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK2382215T3 (da) | 2008-12-29 | 2014-10-27 | Sanofi Sa | Derivater af 2-pyridin-2-yl-pyrazol-3(2h)-on, fremstilling og terapeutisk anvendelse heraf |
WO2012133783A1 (ja) * | 2011-03-31 | 2012-10-04 | キッセイ薬品工業株式会社 | ベンジルピラゾール誘導体の製造方法およびその製造中間体 |
CN104321318A (zh) * | 2012-03-30 | 2015-01-28 | 第一三共株式会社 | 4-烷酰基氨基-3-吡唑啉酮衍生物 |
ME03024B (me) | 2013-03-29 | 2018-10-20 | Takeda Pharmaceuticals Co | Derivati 6-(5-hidroksi-1h-pirazol-1-il)nicotinamida i njihova primjena kao inhibitori phd |
DE102016223133A1 (de) | 2016-11-23 | 2018-05-24 | Deere & Company | Geschwindigkeitskontrolle einer Erntemaschine |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE4023488A1 (de) * | 1990-07-24 | 1992-01-30 | Bayer Ag | 1-(pyri(mi)dyl-(2)) -5-hydroxy-pyrazol-mikrobizide |
US5750088A (en) | 1993-03-30 | 1998-05-12 | The Dupont Merck Pharmaceutical Company | Stable hydrazones linked to a peptide moiety as reagents for the preparation of radiopharmaceuticals |
EP1646382A4 (en) | 2003-06-30 | 2010-07-21 | Hif Bio Inc | COMPOUNDS, COMPOSITIONS AND METHODS |
DE102005019712A1 (de) * | 2005-04-28 | 2006-11-09 | Bayer Healthcare Ag | Dipyridyl-dihydropyrazolone und ihre Verwendung |
PE20071020A1 (es) | 2006-03-07 | 2007-12-11 | Smithkline Beecham Corp | Compuestos derivados de glicina n-sustituidos como inhibidores de prolil hidroxilasa |
ES2435430T3 (es) | 2006-10-16 | 2013-12-19 | Thesan Pharmaceuticals, Inc. | Pirazolil tienopiridinas terapéuticas |
DE102006050516A1 (de) * | 2006-10-26 | 2008-04-30 | Bayer Healthcare Ag | Substituierte Dihydropyrazolone und ihre Verwendung |
KR20100016617A (ko) | 2007-05-18 | 2010-02-12 | 바이엘 쉐링 파마 악티엔게젤샤프트 | 과증식성 장애 및 혈관형성 관련 질환의 치료에 유용한 저산소증 유도성 인자 (hif)의 억제제 |
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2009
- 2009-12-24 EA EA201170899A patent/EA019591B1/ru not_active IP Right Cessation
- 2009-12-24 CA CA2748411A patent/CA2748411A1/fr not_active Abandoned
- 2009-12-24 AU AU2009334569A patent/AU2009334569B2/en not_active Ceased
- 2009-12-24 SG SG2011047503A patent/SG172803A1/en unknown
- 2009-12-24 KR KR1020117017676A patent/KR20110099786A/ko not_active Application Discontinuation
- 2009-12-24 PT PT98057896T patent/PT2382205E/pt unknown
- 2009-12-24 MX MX2011007054A patent/MX2011007054A/es active IP Right Grant
- 2009-12-24 WO PCT/FR2009/052691 patent/WO2010076524A2/fr active Application Filing
- 2009-12-24 MA MA34027A patent/MA32976B1/fr unknown
- 2009-12-24 PE PE2011001292A patent/PE20120416A1/es not_active Application Discontinuation
- 2009-12-24 DK DK09805789.6T patent/DK2382205T3/da active
- 2009-12-24 CN CN200980157590.6A patent/CN102333769B/zh not_active Expired - Fee Related
- 2009-12-24 BR BRPI0924060A patent/BRPI0924060A8/pt not_active IP Right Cessation
- 2009-12-24 PL PL09805789T patent/PL2382205T3/pl unknown
- 2009-12-24 ES ES09805789.6T patent/ES2481042T3/es active Active
- 2009-12-24 MY MYPI2011003012A patent/MY179093A/en unknown
- 2009-12-24 EP EP09805789.6A patent/EP2382205B1/fr active Active
- 2009-12-24 NZ NZ593751A patent/NZ593751A/xx not_active IP Right Cessation
- 2009-12-24 SI SI200930983T patent/SI2382205T1/sl unknown
- 2009-12-24 JP JP2011542886A patent/JP5734870B2/ja not_active Expired - Fee Related
- 2009-12-28 AR ARP090105126A patent/AR074915A1/es unknown
- 2009-12-28 TW TW098145336A patent/TWI482763B/zh not_active IP Right Cessation
- 2009-12-29 PA PA20098856201A patent/PA8856201A1/es unknown
- 2009-12-29 UY UY0001032369A patent/UY32369A/es not_active Application Discontinuation
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2011
- 2011-05-24 TN TN2011000267A patent/TN2011000267A1/fr unknown
- 2011-06-17 CL CL2011001496A patent/CL2011001496A1/es unknown
- 2011-06-22 EC EC2011011155A patent/ECSP11011155A/es unknown
- 2011-06-23 CR CR20110361A patent/CR20110361A/es unknown
- 2011-06-27 IL IL213789A patent/IL213789A/en not_active IP Right Cessation
- 2011-06-28 ZA ZA2011/04783A patent/ZA201104783B/en unknown
- 2011-06-29 US US13/172,305 patent/US8541455B2/en not_active Expired - Fee Related
- 2011-06-29 CO CO11081326A patent/CO6400141A2/es active IP Right Grant
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2014
- 2014-07-15 HR HRP20140680AT patent/HRP20140680T1/hr unknown
- 2014-07-22 SM SM201400097T patent/SMT201400097B/xx unknown
- 2014-07-23 CY CY20141100553T patent/CY1115368T1/el unknown
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