AR104512A1 - Compuestos de pirazol inhibidores de proteína activadora de 5-lipoxigenasa (flap) - Google Patents
Compuestos de pirazol inhibidores de proteína activadora de 5-lipoxigenasa (flap)Info
- Publication number
- AR104512A1 AR104512A1 ARP160101257A ARP160101257A AR104512A1 AR 104512 A1 AR104512 A1 AR 104512A1 AR P160101257 A ARP160101257 A AR P160101257A AR P160101257 A ARP160101257 A AR P160101257A AR 104512 A1 AR104512 A1 AR 104512A1
- Authority
- AR
- Argentina
- Prior art keywords
- ring
- independently
- halo
- alkyl
- heterocyclyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 102000004023 5-Lipoxygenase-Activating Proteins Human genes 0.000 title 1
- 108090000411 5-Lipoxygenase-Activating Proteins Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- -1 -S (O) pR7 Chemical group 0.000 abstract 2
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 2
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic 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
- C07D403/12—Heterocyclic 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
- C07D231/38—Nitrogen atoms
- C07D231/40—Acylated on said nitrogen atom
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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
- A61K31/41—Heterocyclic 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
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic 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
- A61K31/495—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- 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
- A61P1/16—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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- 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
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
- C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
- C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
- C07D231/46—Oxygen atom in position 3 or 5 and nitrogen atom in position 4
- C07D231/50—Acylated on said nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/12—Heterocyclic 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
A su uso en el tratamiento y/o prevención de afecciones clínicas que incluyen enfermedades cardiovasculares (CVD), a métodos para su uso terapéutico, a composiciones farmacéuticas que los contienen y a procesos para preparar dichos compuestos. Reivindicación 1: Un compuesto de acuerdo con la fórmula (1), o una sal farmacéuticamente aceptable de este, donde: R¹ es H, alquilo C₁₋₃, halo, alcoxi C₁₋₃, haloalquilo C₁₋₃ o haloalcoxi C₁₋₃; cada uno de R² y R³ es independientemente H, alquilo C₁₋₃, alcoxi C₁₋₃, -CN o halo; R⁴ es H, -CH₃, -CH₂F, -CHF₂, -CF₃, o halo; Anillo A contiene 2 enlaces dobles; cada X¹, X², X³ y X⁴ del Anillo A es independientemente CR⁵, CH, O, S, NR⁶ o N; donde al menos uno de X¹, X², X³ y X⁴ en el Anillo A es NR⁶; cada R⁵ es opcional e independientemente alquilo C₁₋₆, alcoxi C₁₋₆, haloalquilo C₁₋₃, haloalcoxi C₁₋₃, -S(O)ₚR⁷, -CN, -CONRR, o cicloalquilo C₃₋₆; cada p es independientemente 0, 1 ó 2; R⁶ es H, -CH₃ o -CH₂CH₃; o donde cuando X⁴ es CR⁵ y X³ es NR⁶, entonces R⁵ y R⁶ pueden tomarse juntos para formar un anillo heterociclilo de 5 a 6 miembros fusionado al Anillo A, cuyo heterociclilo puede contener opcionalmente un heteroátomo adicional que se selecciona de N, O y S; tal heterociclilo fusionado puede contener adicionalmente un carbonilo o S(O)₂ directamente adyacente a un heteroátomo en este; y puede además sustituirse con uno o dos sustituyentes que se seleccionan del grupo que consiste en CH₃ y halo; R⁷ es -CH₃ o -NRR; y cada R y R es independientemente -H o -CH₃; siempre que la cantidad total de sustituyentes en el Anillo A sea 0, 1 ó 2; y además siempre que cuando R⁵ y R⁶ no estén combinados para formar un anillo heterociclilo fusionado al Anillo A, que la cantidad total de sustituyentes de R⁵ y R⁶ que es alquilo y/o haloalquilo sea 0 ó 1.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201562156424P | 2015-05-04 | 2015-05-04 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR104512A1 true AR104512A1 (es) | 2017-07-26 |
Family
ID=55910253
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP160101257A AR104512A1 (es) | 2015-05-04 | 2016-05-03 | Compuestos de pirazol inhibidores de proteína activadora de 5-lipoxigenasa (flap) |
Country Status (38)
Country | Link |
---|---|
US (6) | US10183947B2 (es) |
EP (2) | EP3292105B1 (es) |
JP (1) | JP6564062B2 (es) |
KR (1) | KR102623474B1 (es) |
CN (1) | CN107646036B (es) |
AR (1) | AR104512A1 (es) |
AU (1) | AU2016258874B2 (es) |
BR (1) | BR112017022757B1 (es) |
CA (1) | CA2983668C (es) |
CL (1) | CL2017002660A1 (es) |
CO (1) | CO2017011506A2 (es) |
CR (1) | CR20170513A (es) |
CY (2) | CY1122689T1 (es) |
DK (2) | DK3292105T3 (es) |
DO (1) | DOP2017000244A (es) |
EA (1) | EA032221B1 (es) |
ES (2) | ES2902139T3 (es) |
GT (1) | GT201700220A (es) |
HK (1) | HK1245255A1 (es) |
HR (2) | HRP20211993T1 (es) |
HU (2) | HUE056875T2 (es) |
IL (1) | IL255069B (es) |
LT (1) | LT3670499T (es) |
ME (1) | ME03663B (es) |
MX (1) | MX2017013571A (es) |
MY (1) | MY186647A (es) |
PE (1) | PE20180247A1 (es) |
PH (1) | PH12017502112B1 (es) |
PL (2) | PL3292105T3 (es) |
PT (2) | PT3292105T (es) |
RS (2) | RS59671B1 (es) |
SG (1) | SG11201708558RA (es) |
SI (2) | SI3670499T1 (es) |
SV (1) | SV2017005549A (es) |
TN (1) | TN2017000458A1 (es) |
TW (1) | TWI718146B (es) |
WO (1) | WO2016177703A1 (es) |
ZA (1) | ZA201708189B (es) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MX2017013571A (es) | 2015-05-04 | 2018-02-26 | Astrazeneca Ab | Derivados de pirazol utiles como inhibidores de proteina activadora de 5-lipoxigenasa (flap). |
MX2019004574A (es) * | 2016-10-28 | 2019-08-21 | Astrazeneca Ab | Forma cristalina de (1r,2r)-2-[4-(3-metil-1h-pirazol-5-il)benzoil- n-(4-oxo-4,5,6,7-tetrahidropirazolo[1,5-a]pirazin-3-il)ciclohexan ocarboxamida. |
CN110169969B (zh) * | 2019-06-28 | 2022-05-27 | 南京医科大学 | Mk571在制备预防和治疗心脏病药物中应用 |
CN111084775A (zh) * | 2020-02-17 | 2020-05-01 | 牡丹江医学院 | 一种用于治疗癫痫的药物组合物 |
CN111419800B (zh) * | 2020-04-23 | 2021-03-19 | 温州医科大学附属第二医院、温州医科大学附属育英儿童医院 | 用于治疗红斑狼疮的药物制剂及其制备方法 |
CN111643498B (zh) * | 2020-07-20 | 2021-05-07 | 黑龙江中医药大学 | 一种治疗肾结石的药物组合物及其用途 |
CN111714499B (zh) * | 2020-07-27 | 2021-05-11 | 黑龙江中医药大学 | 一种用于治疗多囊卵巢综合征的药物组合物 |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AP9400632A0 (en) | 1993-04-29 | 1995-10-07 | Zeneca Ltd | Ether derivatives. |
US5773422A (en) | 1996-01-29 | 1998-06-30 | Komer; Gene | Avermectin formulation |
US20070275962A1 (en) * | 2003-09-10 | 2007-11-29 | Gpc Biotech Ag | Heterobicyclic Compounds as Pharmaceutically Active Agents |
GB2431927B (en) * | 2005-11-04 | 2010-03-17 | Amira Pharmaceuticals Inc | 5-Lipoxygenase-activating protein (FLAP) inhibitors |
TW200815351A (en) * | 2006-05-02 | 2008-04-01 | Astrazeneca Ab | Novel compounds |
EP2114876A4 (en) * | 2007-02-05 | 2010-12-22 | Amira Pharmaceuticals Inc | INVERSE INDOLES AS INHIBITORS OF THE 5-LIPOXYGENASE ACTIVATION PROTEIN (FLAP) |
GB0702456D0 (en) * | 2007-02-08 | 2007-03-21 | Astrazeneca Ab | New combination |
CA2684618A1 (en) * | 2007-04-20 | 2008-10-30 | Schering Corporation | Tetrahydropyrido[4,3-d]pyrimidinone derivatives and methods of use thereof |
AU2008251557B2 (en) * | 2007-05-10 | 2012-12-06 | Albany Molecular Research, Inc. | Aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin |
WO2009045700A2 (en) * | 2007-10-05 | 2009-04-09 | Amira Pharmaceuticals, Inc. | 5-lipoxygenase-activating protein (flap) inhibitors |
MX2017013571A (es) * | 2015-05-04 | 2018-02-26 | Astrazeneca Ab | Derivados de pirazol utiles como inhibidores de proteina activadora de 5-lipoxigenasa (flap). |
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2016
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2017
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