ES2531006T3 - Derivados de benzofurano como moduladores de FXR - Google Patents

Derivados de benzofurano como moduladores de FXR Download PDF

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Publication number
ES2531006T3
ES2531006T3 ES09731855T ES09731855T ES2531006T3 ES 2531006 T3 ES2531006 T3 ES 2531006T3 ES 09731855 T ES09731855 T ES 09731855T ES 09731855 T ES09731855 T ES 09731855T ES 2531006 T3 ES2531006 T3 ES 2531006T3
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Prior art keywords
benzofuran
piperazin
carboxylic acid
bromo
benzenesulfonyl
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Didier Roche
Gisèle Mautino
Ingo Kober
Francis Contard
Serge Christmann-Franck
Saumitra Sengupta
Ramesh Sistla
Rao Gummadi Venkateshwar
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Merck Patent GmbH
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Merck Patent GmbH
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P1/04—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
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P17/18—Antioxidants, e.g. antiradicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—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
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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
    • C07D307/84—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D307/85—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
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  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos seleccionados del grupo - éster terc-butílico del ácido 4-(4-Bromo-2-etoxicarbonil-benzofuran-5-il)-piperazin-1-carboxílico - éster terc-butílico del ácido 4-(4-Bromo-2-carboxi-benzofuran-5-il)-piperazin-1-carboxílico - amida del ácido 5-[4-(3-Metoxi-bencenosulfonil)-piperazin-1-il]-benzofuran-2-carboxílico - amida del ácido 5-[4-(4-Metoxi-bencenosulfonil)-piperazin-1-il]-benzofuran-2-carboxílico - amida del ácido 5-[4-(3-Trifluorometil-bencil)-piperazin-1-il]-benzofuran-2-carboxílico - amida del ácido 5-[4-(3-Cloro-bencil)-piperazin-1-il]-benzofuran-2-carboxílico - amida del ácido 5-[4-(3-Fluoro-benzoil)-piperazin-1-il]-benzofuran-2-carboxílico - amida del ácido 5-[4-(3-Cloro-bencenosulfonil)-piperazin-1-il]-benzofuran-2-carboxílico - amida del ácido 4-Bromo-5-[4-(4-metoxi-bencenosulfonil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 5-(4-Bencenosulfonil-piperazin-1-il)-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(3-fluoro-benzoil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(3-cloro-bencenosulfonil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(3-fluoro-bencenosulfonil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(pirrolidin-1-carbonil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(3-cloro-bencil)-piperazin-1-il]-benzofuran-2-carboxílico - éster terc-butílico del ácido 4-(2-Carboxi-benzofuran-5-ilamino)-piperidin-1-carboxílico - éster terc-butílico del ácido 2-[4-(4-Bromo-2-carboxi-benzofuran-5-il)-piperazin-1-carbonil]-pirrolidin-1-carboxílico~ - éster terc-butílico del ácido 4-(4-Cloro-2-etoxicarbonil-benzofuran-5-il)-piperazin-1-carboxílico - éster terc-butílico del ácido 4-(2-Carboxi-4-cloro-benzofuran-5-il)-piperazin-1-carboxílico - ácido 4-Bromo-5-[4-(3-trifluorometil-bencil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 5-[4-(3-Metoxi-bencenosulfonil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(3-metoxi-bencenosulfonil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(4-metoxi-bencenosulfonil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(pirrolidin-2-carbonil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 5-[4-(Adamantan-1-carbonil)-piperazin-1-il]-4-bromo-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(3-cloro-benzoil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(2-fluoro-bencil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 4-Bromo-5-[4-(3-fluoro-bencil)-piperazin-1-il]-benzofuran-2-carboxílico - ácido 5-(4-Benzoil-piperazin-1-il)-4-bromo-benzofuran-2-carboxílico.
ES09731855T 2008-04-18 2009-03-30 Derivados de benzofurano como moduladores de FXR Active ES2531006T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08300183A EP2110374A1 (en) 2008-04-18 2008-04-18 Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
PCT/EP2009/002297 WO2009127321A1 (en) 2008-04-18 2009-03-30 Benzofurane, benzothiophene, benzothiazol derivatives as fxr modulators

Publications (1)

Publication Number Publication Date
ES2531006T3 true ES2531006T3 (es) 2015-03-09

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ID=39769187

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Application Number Title Priority Date Filing Date
ES09731855T Active ES2531006T3 (es) 2008-04-18 2009-03-30 Derivados de benzofurano como moduladores de FXR

Country Status (26)

Country Link
US (1) US8575161B2 (es)
EP (2) EP2110374A1 (es)
JP (2) JP5616326B2 (es)
KR (1) KR101662853B1 (es)
CN (1) CN101990535B (es)
AR (1) AR071207A1 (es)
AU (1) AU2009238015B2 (es)
BR (1) BRPI0911243B8 (es)
CA (1) CA2721591C (es)
CO (1) CO6311099A2 (es)
CY (1) CY1116333T1 (es)
DK (1) DK2262785T3 (es)
EA (1) EA020454B1 (es)
EC (1) ECSP10010615A (es)
ES (1) ES2531006T3 (es)
HR (1) HRP20150319T1 (es)
IL (1) IL208322A (es)
MX (1) MX2010011292A (es)
MY (1) MY156530A (es)
NZ (1) NZ589327A (es)
PL (1) PL2262785T3 (es)
PT (1) PT2262785E (es)
SI (1) SI2262785T1 (es)
UA (1) UA104140C2 (es)
WO (1) WO2009127321A1 (es)
ZA (1) ZA201008243B (es)

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