CN103249306A - 中间体化合物以及用于制备喹啉衍生物如拉喹莫德钠的方法 - Google Patents

中间体化合物以及用于制备喹啉衍生物如拉喹莫德钠的方法 Download PDF

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Publication number
CN103249306A
CN103249306A CN2011800561301A CN201180056130A CN103249306A CN 103249306 A CN103249306 A CN 103249306A CN 2011800561301 A CN2011800561301 A CN 2011800561301A CN 201180056130 A CN201180056130 A CN 201180056130A CN 103249306 A CN103249306 A CN 103249306A
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CN
China
Prior art keywords
compound
formula
salt
laquinimod
sodium
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Pending
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CN2011800561301A
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English (en)
Chinese (zh)
Inventor
埃胡德·马罗姆
迈克尔·米治里特斯基
塞·鲁比诺夫
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Mapi Pharma Ltd
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Mapi Pharma Ltd
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Publication of CN103249306A publication Critical patent/CN103249306A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/76—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C235/78—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/52—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C229/54—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C229/56—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho-position
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C233/11—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/53—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/55—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C63/00—Compounds having carboxyl groups bound to a carbon atoms of six-membered aromatic rings
    • C07C63/68—Compounds having carboxyl groups bound to a carbon atoms of six-membered aromatic rings containing halogen
    • C07C63/70—Monocarboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN2011800561301A 2010-11-28 2011-11-28 中间体化合物以及用于制备喹啉衍生物如拉喹莫德钠的方法 Pending CN103249306A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41743110P 2010-11-28 2010-11-28
US61/417,431 2010-11-28
PCT/IL2011/050030 WO2012070051A1 (en) 2010-11-28 2011-11-28 Intermediate compounds and processes for the preparation of quinoline derivatives such as laquinimod sodium

Publications (1)

Publication Number Publication Date
CN103249306A true CN103249306A (zh) 2013-08-14

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Family Applications (1)

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CN2011800561301A Pending CN103249306A (zh) 2010-11-28 2011-11-28 中间体化合物以及用于制备喹啉衍生物如拉喹莫德钠的方法

Country Status (9)

Country Link
US (2) US8865742B2 (enExample)
EP (1) EP2642855A4 (enExample)
JP (1) JP2013544819A (enExample)
CN (1) CN103249306A (enExample)
AU (1) AU2011333346A1 (enExample)
CA (1) CA2815935A1 (enExample)
IN (1) IN2013MN00811A (enExample)
MX (1) MX2013005954A (enExample)
WO (1) WO2012070051A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20130065728A (ko) 2010-10-14 2013-06-19 임뮤나르 에이비 Ahr 활성화제로서의 1,2-디히드로-4-히드록시-2-옥소-퀴놀린-3-카르복사닐리드
US8865742B2 (en) 2010-11-28 2014-10-21 Mapi Pharma Ltd. Intermediate compounds and processes for the preparation of quinoline derivatives such as Laquinimod sodium
US10655779B2 (en) 2011-12-21 2020-05-19 Deka Products Limited Partnership System, method, and apparatus for clamping
JP2023527782A (ja) * 2020-05-21 2023-06-30 ステムシナジー セラピューティクス， インク． Ｎｏｔｃｈ阻害剤及びその使用

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4633009A (en) 1985-06-18 1986-12-30 Frizsche Dodge & Olcott Inc. Synthesis of methyl N-methylanthranilate
GB2236318A (en) 1989-09-26 1991-04-03 Nitrokemia Ipartelepek Process for preparing pure N-methyl-anthranilic acid methylester
GB9108547D0 (en) * 1991-04-22 1991-06-05 Fujisawa Pharmaceutical Co Quinoline derivatives
JPH07224040A (ja) 1994-02-07 1995-08-22 Fujisawa Pharmaceut Co Ltd キノリン誘導体
US6077851A (en) * 1998-04-27 2000-06-20 Active Biotech Ab Quinoline derivatives
EP1309596B1 (en) * 2000-08-11 2008-02-06 Boehringer Ingelheim Pharmaceuticals Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
EP1322594B1 (en) 2000-10-04 2005-06-08 Prom Limited Process for the preparation of alkyl n-alkylanthranilate
US6875869B2 (en) * 2002-06-12 2005-04-05 Active Biotech Ab Process for the manufacture of quinoline derivatives
US7560557B2 (en) * 2002-06-12 2009-07-14 Active Biotech Ag Process for the manufacture of quinoline derivatives
KR20070094957A (ko) 2005-01-07 2007-09-27 아르피다 아게 선택된 벤조퓨란 유도체
BRPI0617477A2 (pt) * 2005-10-19 2011-07-26 Teva Pharma mistura de partÍculas cristalinas de laquinimod sàdica, composiÇço, processo de cristalizaÇço de laquinimod sàdica, laquinimod sàdica, e, processo para produzir uma composiÇço farmacÊutica
PL2276740T3 (pl) * 2008-04-28 2015-01-30 Actavis Group Ptc Ehf Ulepszony sposób wytwarzania pochodnych chinolino-3-karboksyamidowych
US8354428B2 (en) 2008-07-01 2013-01-15 Actavis Group Ptc Ehf Solid state forms of laquinimod and its sodium salt
AU2009288108B2 (en) 2008-09-03 2013-10-17 Teva Pharmaceutical Industries, Ltd. 2-oxo-1,2-dihydro-quinoline modulators of immune function
US8865742B2 (en) * 2010-11-28 2014-10-21 Mapi Pharma Ltd. Intermediate compounds and processes for the preparation of quinoline derivatives such as Laquinimod sodium

Also Published As

Publication number Publication date
EP2642855A4 (en) 2014-05-28
US9102592B2 (en) 2015-08-11
JP2013544819A (ja) 2013-12-19
US20150051419A1 (en) 2015-02-19
AU2011333346A1 (en) 2013-05-30
WO2012070051A1 (en) 2012-05-31
EP2642855A1 (en) 2013-10-02
US8865742B2 (en) 2014-10-21
IN2013MN00811A (enExample) 2015-06-12
MX2013005954A (es) 2013-07-29
CA2815935A1 (en) 2012-05-31
US20130245065A1 (en) 2013-09-19

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Application publication date: 20130814