CN104610144A - 氘化的n-乙基-n-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺、其盐和用途 - Google Patents

氘化的n-乙基-n-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺、其盐和用途 Download PDF

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Publication number
CN104610144A
CN104610144A CN201410831557.XA CN201410831557A CN104610144A CN 104610144 A CN104610144 A CN 104610144A CN 201410831557 A CN201410831557 A CN 201410831557A CN 104610144 A CN104610144 A CN 104610144A
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CN
China
Prior art keywords
laquinimod
compound
pharmaceutically acceptable
acceptable salt
chloro
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201410831557.XA
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English (en)
Chinese (zh)
Inventor
维克多·皮尔雅汀斯盖
阿维塔勒·劳尔
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Teva Pharmaceutical Industries Ltd
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Teva Pharmaceutical Industries Ltd
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45439026&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN104610144(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Teva Pharmaceutical Industries Ltd filed Critical Teva Pharmaceutical Industries Ltd
Publication of CN104610144A publication Critical patent/CN104610144A/zh
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • 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
    • 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
    • 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
    • A61K31/455Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • 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
    • A61K31/465Nicotine; Derivatives thereof
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/47042-Quinolinones, e.g. carbostyril
    • 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
    • A61K31/5545Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having eight-membered rings not containing additional condensed or non-condensed nitrogen-containing 3-7 membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
CN201410831557.XA 2010-07-09 2011-07-08 氘化的n-乙基-n-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺、其盐和用途 Pending CN104610144A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39929710P 2010-07-09 2010-07-09
US61/399,297 2010-07-09

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN2011800340883A Division CN102984939A (zh) 2010-07-09 2011-07-08 氘化的n-乙基-n-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺、其盐和用途

Publications (1)

Publication Number Publication Date
CN104610144A true CN104610144A (zh) 2015-05-13

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
CN2011800340883A Pending CN102984939A (zh) 2010-07-09 2011-07-08 氘化的n-乙基-n-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺、其盐和用途
CN201410831557.XA Pending CN104610144A (zh) 2010-07-09 2011-07-08 氘化的n-乙基-n-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺、其盐和用途

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CN2011800340883A Pending CN102984939A (zh) 2010-07-09 2011-07-08 氘化的n-乙基-n-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺、其盐和用途

Country Status (20)

Country Link
US (3) US8580819B2 (enExample)
EP (2) EP2597954A4 (enExample)
JP (2) JP2013535437A (enExample)
KR (1) KR20130092558A (enExample)
CN (2) CN102984939A (enExample)
AR (1) AR082150A1 (enExample)
AU (1) AU2011274496B2 (enExample)
BR (1) BR112013000599A2 (enExample)
CA (1) CA2804986A1 (enExample)
CL (1) CL2013000063A1 (enExample)
EA (1) EA025377B1 (enExample)
IL (1) IL251600A0 (enExample)
MX (1) MX2013000333A (enExample)
NZ (1) NZ606587A (enExample)
PE (1) PE20130396A1 (enExample)
PH (1) PH12013500065A1 (enExample)
SG (2) SG10201505236YA (enExample)
UY (1) UY33504A (enExample)
WO (1) WO2012006538A1 (enExample)
ZA (1) ZA201300956B (enExample)

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TW201400117A (zh) 2012-06-05 2014-01-01 Teva Pharma 使用拉喹莫德治療眼發炎疾病
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WO2014086284A1 (zh) * 2012-12-04 2014-06-12 上海医药集团股份有限公司 一类氘代3-氰基喹啉类化合物、其药用组合物、制备方法及其用途
HK1220125A1 (zh) 2013-03-14 2017-04-28 Teva Pharmaceutical Industries Ltd. 拉喹莫德的透皮配方
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MX2013000333A (es) 2010-07-09 2013-02-26 Teva Pharma N-etil-n-fenil-1,2-dihidro-4-hidroxi-5-cloro-1-metil-2-oxoquinoli na-3-carboxamida deuterada, sales y usos de la misma.
EP2648732A4 (en) 2010-12-07 2014-04-30 Teva Pharma USE OF LAQUINIMOD TO REDUCE TEMPERATURE, IMPROVE FUNCTIONAL STATUS AND IMPROVE LIFE QUALITY IN PATIENTS WITH MULTIPLE SCLEROSIS

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EA025377B1 (ru) 2016-12-30
WO2012006538A8 (en) 2013-05-23
NZ606587A (en) 2015-03-27
CN102984939A (zh) 2013-03-20
ZA201300956B (en) 2014-04-30
UY33504A (es) 2012-02-29
KR20130092558A (ko) 2013-08-20
US20120010238A1 (en) 2012-01-12
PE20130396A1 (es) 2013-04-19
EP3213636A1 (en) 2017-09-06
IL251600A0 (en) 2017-06-29
AU2011274496A1 (en) 2013-02-28
BR112013000599A2 (pt) 2016-07-05
SG10201505236YA (en) 2015-08-28
SG186948A1 (en) 2013-02-28
US20140051723A1 (en) 2014-02-20
US9102620B2 (en) 2015-08-11
US20140343096A1 (en) 2014-11-20
EA201390081A1 (ru) 2013-07-30
MX2013000333A (es) 2013-02-26
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