ES2755125T3 - Derivados de 2H-1,2,3-triazol como inhibidores de fibrosis - Google Patents

Derivados de 2H-1,2,3-triazol como inhibidores de fibrosis Download PDF

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Publication number
ES2755125T3
ES2755125T3 ES14807059T ES14807059T ES2755125T3 ES 2755125 T3 ES2755125 T3 ES 2755125T3 ES 14807059 T ES14807059 T ES 14807059T ES 14807059 T ES14807059 T ES 14807059T ES 2755125 T3 ES2755125 T3 ES 2755125T3
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formula
alkyl
compound
refers
ring
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English (en)
Spanish (es)
Inventor
Luke Lairson
Michael Bollong
Peter G Schultz
Arnab K Chatterjee
Baiyuan Yang
Puneet Kumar
Kaveri Urkalan
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Scripps Research Institute
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Scripps Research Institute
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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
    • C07D405/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
    • A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-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
    • 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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not 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
    • A61K31/535—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
    • 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
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/14—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 three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Agronomy & Crop Science (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Dentistry (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
ES14807059T 2013-06-07 2014-06-05 Derivados de 2H-1,2,3-triazol como inhibidores de fibrosis Active ES2755125T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361832768P 2013-06-07 2013-06-07
PCT/US2014/041174 WO2014197738A1 (en) 2013-06-07 2014-06-05 Small molecule inhibitors of fibrosis

Publications (1)

Publication Number Publication Date
ES2755125T3 true ES2755125T3 (es) 2020-04-21

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
ES14807059T Active ES2755125T3 (es) 2013-06-07 2014-06-05 Derivados de 2H-1,2,3-triazol como inhibidores de fibrosis
ES19191562T Active ES2991873T3 (es) 2013-06-07 2014-06-05 Análogos del itraconazol como inhibidores de fibrosis

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES19191562T Active ES2991873T3 (es) 2013-06-07 2014-06-05 Análogos del itraconazol como inhibidores de fibrosis

Country Status (20)

Country Link
US (2) US9663499B2 (https=)
EP (2) EP3626242B1 (https=)
JP (1) JP6414831B2 (https=)
KR (1) KR102240329B1 (https=)
CN (1) CN105392364B (https=)
AU (1) AU2014274830B2 (https=)
BR (1) BR112015030203A2 (https=)
CA (1) CA2913634C (https=)
CL (1) CL2015003569A1 (https=)
DK (1) DK3003038T3 (https=)
EA (1) EA201592157A1 (https=)
ES (2) ES2755125T3 (https=)
HK (1) HK1221606A1 (https=)
MX (1) MX2015016783A (https=)
PE (1) PE20160523A1 (https=)
PL (1) PL3003038T3 (https=)
PT (1) PT3003038T (https=)
SG (1) SG11201510011VA (https=)
TN (1) TN2015000519A1 (https=)
WO (1) WO2014197738A1 (https=)

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EP3626242B1 (en) 2013-06-07 2024-08-07 The Scripps Research Institute Itraconazole analogs as inhibitors of fibrosis
US9585859B2 (en) 2013-10-10 2017-03-07 Amarin Pharmaceuticals Ireland Limited Compositions and methods for lowering triglycerides without raising LDL-C levels in a subject on concomitant statin therapy
WO2015195662A1 (en) 2014-06-16 2015-12-23 Amarin Pharmaceuticals Ireland Limited Methods of reducing or preventing oxidation of small dense ldl or membrane polyunsaturated fatty acids
JP6706023B2 (ja) * 2014-12-10 2020-06-03 ザ・スクリップス・リサーチ・インスティテュート 線維症の小分子阻害剤
IL243707A0 (en) 2016-01-20 2016-05-01 Galmed Res And Dev Ltd Treatment to regulate the microbiota in the intestine
WO2017184586A1 (en) * 2016-04-18 2017-10-26 The Trustees Of Columbia University In The City Of New York Therapeutic targets involved in the progression of nonalcoholic steatohepatitis (nash)
US11197870B2 (en) 2016-11-10 2021-12-14 Galmed Research And Development Ltd Treatment for hepatic fibrosis
CN106866459A (zh) * 2017-03-30 2017-06-20 成都绿林科技有限公司 一种抗真菌药物中间体的制备方法
CN106986787A (zh) * 2017-03-30 2017-07-28 成都绿林科技有限公司 一种泊沙康唑中间体的合成方法
WO2019183006A1 (en) 2018-03-19 2019-09-26 Liang Gui Bai Methods and compositions for treating idiopathic pulmonary fibrosis
LT3750536T (lt) 2018-09-24 2026-03-25 Amarin Pharmaceuticals Ireland Limited Širdies ir kraujagyslių sistemos reiškinių rizikos subjekto organizme sumažinimo būdai
EP3863723A4 (en) * 2018-10-14 2022-09-07 The University of Chicago Compositions and methods for activating nrf2-dependent gene expression
BR112022009189A2 (pt) 2019-11-12 2022-07-26 Amarin Pharmaceuticals Ie Ltd Métodos para reduzir o risco de eventos cardiovasculares em um sujeito com fibrilação atrial e/ou palpitação atrial
EP4132531A4 (en) * 2020-04-07 2024-04-17 Amarin Pharmaceuticals Ireland Limited METHODS OF TREATING AND/OR PREVENTING VIRAL INFECTIONS AND/OR DISEASES CAUSED BY VIRUSES IN A SUBJECT IN NEED THEREOF
AU2022263358A1 (en) 2021-04-21 2023-11-30 Amarin Pharmaceuticals Ireland Limited Methods of reducing the risk of heart failure

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Publication number Publication date
HK1221606A1 (zh) 2017-06-09
US20170217943A1 (en) 2017-08-03
BR112015030203A2 (pt) 2017-07-25
EP3626242B1 (en) 2024-08-07
US9981956B2 (en) 2018-05-29
CN105392364B (zh) 2018-09-14
EA201592157A1 (ru) 2016-05-31
EP3003038A4 (en) 2016-11-16
AU2014274830B2 (en) 2017-11-09
CL2015003569A1 (es) 2016-11-11
CN105392364A (zh) 2016-03-09
CA2913634A1 (en) 2014-12-11
PT3003038T (pt) 2019-11-19
JP6414831B2 (ja) 2018-10-31
AU2014274830A1 (en) 2015-11-26
PL3003038T3 (pl) 2020-02-28
ES2991873T3 (es) 2024-12-05
US9663499B2 (en) 2017-05-30
MX2015016783A (es) 2016-07-18
KR102240329B1 (ko) 2021-04-14
JP2016521710A (ja) 2016-07-25
US20160130258A1 (en) 2016-05-12
WO2014197738A1 (en) 2014-12-11
TN2015000519A1 (en) 2017-04-06
EP3003038B1 (en) 2019-08-14
EP3003038A1 (en) 2016-04-13
DK3003038T3 (da) 2019-11-11
EP3626242A1 (en) 2020-03-25
CA2913634C (en) 2022-08-09
PE20160523A1 (es) 2016-05-25
SG11201510011VA (en) 2016-01-28
KR20160029028A (ko) 2016-03-14

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