AR096386A1 - Composición farmacéutica, su uso y régimen de administración para contracepción programada - Google Patents

Composición farmacéutica, su uso y régimen de administración para contracepción programada

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Publication number
AR096386A1
AR096386A1 ARP140102027A ARP140102027A AR096386A1 AR 096386 A1 AR096386 A1 AR 096386A1 AR P140102027 A ARP140102027 A AR P140102027A AR P140102027 A ARP140102027 A AR P140102027A AR 096386 A1 AR096386 A1 AR 096386A1
Authority
AR
Argentina
Prior art keywords
alkyl
pharmaceutical composition
cycloalkyl
members
contraception
Prior art date
Application number
ARP140102027A
Other languages
English (en)
Inventor
Dr Lindenthal Bernhard
Dr Buchmann Bernd
Dr Mengel Anne
Dr Rotgeri Andrea
Dr Ter Laak Antonius
Dr Fuhrmann Ulrike
Dr Bruer Nico
Dr Rhn Ulrike
Dr Serno Peter
Original Assignee
Bayer Pharma AG
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 Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of AR096386A1 publication Critical patent/AR096386A1/es

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Classifications

    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/18Sulfonamides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/192Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • 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
    • A61K31/403Heterocyclic 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 condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • 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
    • A61K31/407Heterocyclic 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 condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/42Oxazoles
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/63Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Urology & Nephrology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Una composición farmacéutica para contracepción programada no hormonal y procesos para preparar la esta composición farmacéutica. Reivindicación 1: Una composición farmacéutica caracterizada porque comprende (a) al menos un antagonista de receptor EP2 de acuerdo a la fórmula (1) en donde R¹: significa H, C₁₋₂ alquilo o C₁₋₂ alquiloxilo; R²: H o metilo; con la condición de que uno de los dos residuos R¹ o R² sea H; X: -(CH₂)ₗ-, -(CH₂)ₖ-O-, -CH₂-S-, CH₂-S(O)₂-, -CH(CH₃)-, -CH(CH₃)-O- o -C(CH₃)₂-O-; k: 1 ó 2; l: 0, 1, ó 2; R⁴: H, C₁₋₄ alquilo, C₃₋₄ cicloalquilo o CH₂-C₃₋₄ cicloalquilo; y en el caso de que X signifique -(CH₂)ₗ- con l significando 0 ó 1 o -CH(CH₃)- R⁴: además significa un residuo de heterocíclico de entre 4 y 6 miembros; y en el caso de que X signifique -(CH₂)ₗ- o -CH(CH₃)- R⁴: además significa CN; m: 1 ó 2; n: 1 ó 2; Ar: un residuo de arilo de entre 6 y 10 miembros o de heteroarilo de entre 5 y 10 miembros; R³: halógeno, CN, SF₅, C₁₋₄ alquilo, C₃₋₆ cicloalquilo, C₄₋₆ heterociclilo, O-C₁₋₄ alquilo, O-C₃₋₆ cicloalquilo, O-C₄₋₆ heterociclilo, S-C₁₋₄ alquilo, S(O)₂-C₁₋₄ alquilo, Ar, O-Ar, C(CH₃)₂-CN o C(CH₃)₂-OH; y Ar un residuo de arilo de 6 miembros o heteroarilo de entre 5 y 6 miembros opcionalmente simplemente o doblemente sustituido; en donde los sustituyentes se eligen de F, Cl, CN, C₁₋₄ alquilo, O-C₁₋₄ alquilo, C(CH₃)₂-CN, C(CH₃)₂-OH y C(O)NH₂; y que comprende (b) al menos un inhibidor de COX que se elige de la siguiente lista: C1) indometacina; C2) diclofenac; C4) naproxeno; C5) ibuprofeno; C6) meloxicam; C7) piroxicam; C8) nimesulida; C9) cetoprofeno; C10) tenoxicam; C11) ácido mafanémico; C12) ketoralac; C13) celecoxib (4-[5-(4-metilfenil)-3-trifluorometil)-1H-pirazol-1-il]bencenosulfonamida; C14) parecoxib (N-[4-(5-metil-3-fenil-4-isoxazolil)fenil]sulfonilpropionamida); C15) rofecoxib (4-(4-mesilfenil)-3-fenilfuran-2(5H)-ona); C16) valdecoxib (4-[5-metil-3-fenil-4-isoxazoil]bencenosulfonamida); C17) etoricoxib; y su uso para contracepción programada.
ARP140102027A 2013-05-23 2014-05-22 Composición farmacéutica, su uso y régimen de administración para contracepción programada AR096386A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13169029 2013-05-23

Publications (1)

Publication Number Publication Date
AR096386A1 true AR096386A1 (es) 2015-12-30

Family

ID=48463871

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140102027A AR096386A1 (es) 2013-05-23 2014-05-22 Composición farmacéutica, su uso y régimen de administración para contracepción programada

Country Status (20)

Country Link
US (1) US9655887B2 (es)
EP (1) EP2999469A1 (es)
JP (1) JP6370887B2 (es)
KR (1) KR20160014598A (es)
CN (1) CN105451737B (es)
AP (1) AP2015008855A0 (es)
AR (1) AR096386A1 (es)
AU (1) AU2014270596A1 (es)
BR (1) BR112015029214A2 (es)
CA (1) CA2913085A1 (es)
CL (1) CL2015003434A1 (es)
EA (1) EA201592207A1 (es)
HK (1) HK1217640A1 (es)
MA (1) MA38606A1 (es)
MX (1) MX2015016121A (es)
PH (1) PH12015502598A1 (es)
TN (1) TN2015000511A1 (es)
TW (1) TW201522325A (es)
UY (1) UY35584A (es)
WO (1) WO2014187744A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10968201B2 (en) 2018-04-17 2021-04-06 Tempest Therapeutics, Inc. Bicyclic carboxamides and methods of use thereof
CN110215447A (zh) * 2019-06-14 2019-09-10 上海市计划生育科学研究所 甲芬那酸在避孕药物中的应用及其制备的杀精避孕药物

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT787002E (pt) 1994-10-24 2007-03-30 Schering Ag Antagonistas de progesterona competitivos para controlo de fertilidade feminina orientado pela necessidade
HU227198B1 (en) 2001-11-27 2010-10-28 Richter Gedeon Nyrt Pharmaceutical composition for emergency contraception containing levonorgestrel
US20040058975A1 (en) * 2002-06-26 2004-03-25 Schering Ag Method for fertility control
DE602006018883D1 (de) 2005-03-31 2011-01-27 Auckland Uniservices Ltd Tricylische 1,2,4-triazinoxide und zusammensetzungen davon zur therapeutischen anwendung bei krebsbehandlungen
DE102005050729A1 (de) 2005-10-19 2007-04-26 Schering Ag Verfahren zur präventiven bedarfsweisen hormonalen Kontrazeption
WO2007091107A1 (en) 2006-02-10 2007-08-16 Summit Corporation Plc Treatment of duchenne muscular dystrophy
CN101616587A (zh) 2006-12-05 2009-12-30 孙仲铭 吲唑化合物
WO2009063365A1 (en) * 2007-11-15 2009-05-22 Pfizer Limited Azetidines as ep2 antagonists
AU2010237120B8 (en) 2009-04-14 2015-11-26 Laboratoire Hra-Pharma Method for on-demand contraception
US20120129825A1 (en) 2009-04-14 2012-05-24 Andre Ulmann Method for on-demand contraception using levonorgestrel or norgestrel
BRPI1013545A2 (pt) 2009-04-22 2019-09-24 Janssen Phamaceutica N V azetidinil diamidas como inibidores de monoacilglicerol lipase
SG177284A1 (en) 2009-06-23 2012-02-28 Bayer Pharma AG Pharmaceutical composition for emergency contraception
DE102009049662A1 (de) 2009-10-13 2011-04-14 Bayer Schering Pharma Aktiengesellschaft 2,5-Disubstituierte 2H-Indazole als EP2-Rezeptor-Antagonisten
US8426392B2 (en) 2009-12-09 2013-04-23 Laboratoire Hra-Pharma Method for providing emergency contraception
US20130045959A1 (en) 2010-02-01 2013-02-21 Andre Ulmann Method for late post coital contraception using ulipristal acetate
TW201326154A (zh) * 2011-11-28 2013-07-01 拜耳知識產權公司 作為ep2受體拮抗劑之新穎2h-吲唑

Also Published As

Publication number Publication date
CA2913085A1 (en) 2014-11-27
JP2016518456A (ja) 2016-06-23
US9655887B2 (en) 2017-05-23
MA38606A1 (fr) 2017-03-31
MX2015016121A (es) 2016-03-31
BR112015029214A2 (pt) 2017-07-25
HK1217640A1 (zh) 2017-01-20
TN2015000511A1 (en) 2017-04-06
TW201522325A (zh) 2015-06-16
JP6370887B2 (ja) 2018-08-08
AU2014270596A1 (en) 2015-12-03
CN105451737A (zh) 2016-03-30
AP2015008855A0 (en) 2015-11-30
WO2014187744A1 (de) 2014-11-27
UY35584A (es) 2014-12-31
EA201592207A1 (ru) 2016-06-30
EP2999469A1 (de) 2016-03-30
CL2015003434A1 (es) 2016-07-22
PH12015502598A1 (en) 2016-02-29
US20160089364A1 (en) 2016-03-31
CN105451737B (zh) 2018-04-10
KR20160014598A (ko) 2016-02-11

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