CA2815935A1 - Intermediate compounds and processes for the preparation of quinoline derivatives such as laquinimod sodium - Google Patents

Intermediate compounds and processes for the preparation of quinoline derivatives such as laquinimod sodium Download PDF

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Publication number
CA2815935A1
CA2815935A1 CA2815935A CA2815935A CA2815935A1 CA 2815935 A1 CA2815935 A1 CA 2815935A1 CA 2815935 A CA2815935 A CA 2815935A CA 2815935 A CA2815935 A CA 2815935A CA 2815935 A1 CA2815935 A1 CA 2815935A1
Authority
CA
Canada
Prior art keywords
compound
formula
process according
salt
laquinimod
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.)
Abandoned
Application number
CA2815935A
Other languages
English (en)
French (fr)
Inventor
Ehud Marom
Michael Mizhiritskii
Shai Rubnov
Original Assignee
Mapi Pharma Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Mapi Pharma Ltd filed Critical Mapi Pharma Ltd
Publication of CA2815935A1 publication Critical patent/CA2815935A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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

Landscapes

  • 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)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
CA2815935A 2010-11-28 2011-11-28 Intermediate compounds and processes for the preparation of quinoline derivatives such as laquinimod sodium Abandoned CA2815935A1 (en)

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
CA2815935A1 true CA2815935A1 (en) 2012-05-31

Family

ID=46145452

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2815935A Abandoned CA2815935A1 (en) 2010-11-28 2011-11-28 Intermediate compounds and processes for the preparation of quinoline derivatives such as laquinimod sodium

Country Status (9)

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

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2813711A1 (en) 2010-10-14 2012-04-19 Immunahr Ab 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides as ahr activators.
AU2011333346A1 (en) 2010-11-28 2013-05-30 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
CN115836056A (zh) * 2020-05-21 2023-03-21 Stemsynergy疗法有限责任公司 Notch抑制剂及其用途

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
JP5000068B2 (ja) * 2000-08-11 2012-08-15 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド チロシンキナーゼのインヒビターとして有用な複素環化合物
AU2000275433A1 (en) 2000-10-04 2002-04-15 Prom Limited Process for the preparation of alkyl n-alkylanthranilate
US7560557B2 (en) 2002-06-12 2009-07-14 Active Biotech Ag Process for the manufacture of quinoline derivatives
US6875869B2 (en) 2002-06-12 2005-04-05 Active Biotech Ab Process for the manufacture of quinoline derivatives
JP2008526791A (ja) 2005-01-07 2008-07-24 アルパイダ アーゲー 選択されたベンゾフラン誘導体
US7884208B2 (en) 2005-10-19 2011-02-08 Teva Pharmaceutical Industries, Ltd. Crystals of laquinimod sodium, and process for the manufacture thereof
US8552194B2 (en) * 2008-04-28 2013-10-08 Actavis Group Ptc Ehf Process for preparing quinoline-3-carboxamide derivatives
US8354428B2 (en) 2008-07-01 2013-01-15 Actavis Group Ptc Ehf Solid state forms of laquinimod and its sodium salt
KR20110048571A (ko) * 2008-09-03 2011-05-11 테바 파마슈티컬 인더스트리즈 리미티드 면역 기능을 지닌 ２―옥소―１,２―다이하이드로―퀴놀린 조절제
AU2011333346A1 (en) 2010-11-28 2013-05-30 Mapi Pharma Ltd. Intermediate compounds and processes for the preparation of quinoline derivatives such as Laquinimod sodium

Also Published As

Publication number Publication date
US20130245065A1 (en) 2013-09-19
IN2013MN00811A (https=) 2015-06-12
EP2642855A1 (en) 2013-10-02
US20150051419A1 (en) 2015-02-19
JP2013544819A (ja) 2013-12-19
US9102592B2 (en) 2015-08-11
CN103249306A (zh) 2013-08-14
AU2011333346A1 (en) 2013-05-30
WO2012070051A1 (en) 2012-05-31
EP2642855A4 (en) 2014-05-28
MX2013005954A (es) 2013-07-29
US8865742B2 (en) 2014-10-21

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Date Code Title Description
FZDE Discontinued

Effective date: 20141128