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ES2539722T3 - Compuesto de tetrahidrobenzotiofeno - Google Patents

Compuesto de tetrahidrobenzotiofeno Download PDF

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Publication number
ES2539722T3
ES2539722T3 ES11775050.5T ES11775050T ES2539722T3 ES 2539722 T3 ES2539722 T3 ES 2539722T3 ES 11775050 T ES11775050 T ES 11775050T ES 2539722 T3 ES2539722 T3 ES 2539722T3
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alkyl
aryl
alkylene
substituted
coo
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Inventor
Shunichiro Hachiya
Masanori Miura
Yoshimasa Imamura
Daisuke Kaga
Ippei Sato
Hiroyuki Moritomo
Koji Kato
Kazuhiro Terai
Yoh Terada
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Astellas Pharma Inc
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Astellas Pharma Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/66—Nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/40—Heterocyclic 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
    • A61K31/4025—Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero 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
    • A61K31/33—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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • 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
    • 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
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Un compuesto de la fórmula (I) o una sal del mismo:**Fórmula** [en donde R1 representa -O-alquilo C1-C6, -alquilen C1-6-fenilo, o -alquilen C1-C6-piridilo (en donde fenilo o piridilo pueden estar sustituidos con carboxi o -CO-O-alquilo C1-C6, -CO-O-alquenilo C1-C6, -CO-O-alquinilo C1-C6, -CO-O-alquileno C1-C6-O-alquilo C1-C6, -CO-O-alquilen C1-C6-arilo, -CO-O-alquilen C1-C6-O-arilo, -CO-NH2, -CO-NH-alquilo C1-C6, -CO-N(alquilo C1-6)2, -CO-N(alquil C1-C6)arilo, -CO-N(alquil C1-C6)-(alquileno C1-C6- arilo), -CO-NH-alquileno C1-C6-OH, -CO-NH-alquileno C1-C6-CO2H, -CO-O-metilo, -CO-O-etilo, o -COO-terc-butilo), R2 y R3 son iguales o diferentes entre sí y representan -H, alquilo C1-C6, cicloalquilo, arilo, heteroarilo, heteroanillo saturado que contiene nitrógeno, -alquilen C1-C6-arilo, o -alquilen C1-C6-heteroarilo (en donde alquilo C1-C6, cicloalquilo, arilo, heteroarilo y heterociclo saturado que contiene nitrógeno pueden estar sustituidos con halógeno, -alquilo C1-C6, piridilo, carboxi, -CO-O-alquilo C1-C6, -CO-O-alquenilo C1-C6, -CO-O-alquinilo C1-C6, -CO-O-alquilen C1-C6-O-alquilo C1-C6, -CO-O-alquilen C1-C6-arilo, -CO-O-alquilen C1-C6- O-arilo, -CO-NH2, -CO-NH-alquilo C1-C6, -CO-N(alquilo C1-C6)2, -CO-N(alquil C1-C6)arilo, -CO-N(alquil C1- C6)-(alquilen C1-C6-arilo), -CO-NH-alquilen C1-C6-OH, -CO-NH-alquilen C1-C6-CO2H, -CO-O-metilo, -CO-O-etilo, -COO-terc-butilo, amino que puede estar sustituido con un grupo -alquilo C1-C6, o los mismos o diferentes dos o más -alquilo C1-C6, -O-alquilo C1-C6, -[CH(-OH)]m-H, u -OH), o R2 y R3 se pueden combinar con un átomo de nitrógeno al que están unidos para formar un amino cíclico saturado de 5 a 7 miembros (en donde el amino cíclico saturado de 5 a 7 miembros que puede estar sustituido con halógeno, -OH, oxo (>= O), -O-alquilo C1-C6, ciano, nitro, cicloalquilo, arilo, heteroanillo, - alquilen C1-C6-arilo, alquileno C1-C6-heteroanillo, -alquilo C1-C6 (que puede estar sustituido con halógeno, - OH, -O-alquilo C1-C6, o ciano), carboxi, -CO-O-alquilo C1-C6, -COO-alquenilo C1-C6, -CO-O-alquinilo C1-C6, -CO-O-alquilen C1-C6-O-alquilo C1-C6, -CO-O-alquilen C1-C6-arilo, -CO-O-alquilen C1-C6-O-arilo, -CO-NH2, - CO-NH-alquilo C1-C6, -CO-N(alquilo C1-C6)2, -CO-N(alquil C1-C6)arilo, -CO-N(alquil C1-C6)-(alquilen C1-C6- arilo), -CO-NH-alquilen C1-C6-OH, -CO-NH-alquilen C1-C6-CO2H, -CO-O-metilo, -CO-O-etilo, -COO-terc-butilo o -CO-alquil C1-C6), los R4' son iguales o diferentes entre sí y representan halógeno, alquilo C1-C6, -OH, -O-alquilo C1-C6, -NO2, o un grupo representado por la fórmula (II): **Fórmula**
ES11775050.5T 2010-04-28 2011-04-27 Compuesto de tetrahidrobenzotiofeno Active ES2539722T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2010104044 2010-04-28
JP2010104044 2010-04-28
PCT/JP2011/060261 WO2011136269A1 (ja) 2010-04-28 2011-04-27 テトラヒドロベンゾチオフェン化合物

Publications (1)

Publication Number Publication Date
ES2539722T3 true ES2539722T3 (es) 2015-07-03

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US (3) US20130029973A1 (es)
EP (1) EP2565190B1 (es)
JP (1) JP5617919B2 (es)
KR (1) KR101721025B1 (es)
CN (1) CN102869656B (es)
AU (1) AU2011246072B2 (es)
BR (1) BR112012025390B8 (es)
CA (1) CA2793856C (es)
EA (1) EA022521B1 (es)
ES (1) ES2539722T3 (es)
MX (1) MX2012012421A (es)
PH (1) PH12012501851A1 (es)
PL (1) PL2565190T3 (es)
PT (1) PT2565190E (es)
WO (1) WO2011136269A1 (es)

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AU2011246072A1 (en) 2012-10-11
KR20130073908A (ko) 2013-07-03
CA2793856A1 (en) 2011-11-03
CN102869656B (zh) 2014-03-12
JPWO2011136269A1 (ja) 2013-07-22
PT2565190E (pt) 2015-08-24
PL2565190T3 (pl) 2015-10-30
AU2011246072B2 (en) 2014-06-26
BR112012025390B8 (pt) 2022-11-22
US20130053369A1 (en) 2013-02-28
KR101721025B1 (ko) 2017-03-29
EP2565190A4 (en) 2013-08-21
JP5617919B2 (ja) 2014-11-05
BR112012025390A2 (pt) 2016-06-28
EP2565190A1 (en) 2013-03-06
EP2565190B1 (en) 2015-06-03
US20130029973A1 (en) 2013-01-31
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EA022521B1 (ru) 2016-01-29
US9284295B2 (en) 2016-03-15
EA201291121A1 (ru) 2013-04-30
CA2793856C (en) 2018-07-17
BR112012025390B1 (pt) 2021-10-13
WO2011136269A1 (ja) 2011-11-03
PH12012501851A1 (en) 2013-02-04
US8729068B2 (en) 2014-05-20

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