PL1899343T3 - Fluorowcowane pirazolo[1,5-a]pirymidyny, sposób ich wytwarzania, ich zastosowanie jako ligandów receptorów GABA-A, kompozycje je zawierające i związki pośrednie - Google Patents

Fluorowcowane pirazolo[1,5-a]pirymidyny, sposób ich wytwarzania, ich zastosowanie jako ligandów receptorów GABA-A, kompozycje je zawierające i związki pośrednie

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Publication number
PL1899343T3
PL1899343T3 PL06763737T PL06763737T PL1899343T3 PL 1899343 T3 PL1899343 T3 PL 1899343T3 PL 06763737 T PL06763737 T PL 06763737T PL 06763737 T PL06763737 T PL 06763737T PL 1899343 T3 PL1899343 T3 PL 1899343T3
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PL
Poland
Prior art keywords
gaba
pyrimidines
intermediates
compositions
processes
Prior art date
Application number
PL06763737T
Other languages
English (en)
Inventor
Luís Anglada
Albert Palomer
Antonio Guglietta
Original Assignee
Ferrer Int
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 Ferrer Int filed Critical Ferrer Int
Publication of PL1899343T3 publication Critical patent/PL1899343T3/pl

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/12Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/30Carboxylic 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 doubly-bound oxygen atoms
    • C07C233/33Carboxylic 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 doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34Carboxylic 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 amino groups
    • C07C233/42Carboxylic 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 amino 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
    • C07C233/43Carboxylic 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 amino 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 hydrogen atom or to a carbon atom of a saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/36Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
    • C07C303/40Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
PL06763737T 2005-06-21 2006-06-15 Fluorowcowane pirazolo[1,5-a]pirymidyny, sposób ich wytwarzania, ich zastosowanie jako ligandów receptorów GABA-A, kompozycje je zawierające i związki pośrednie PL1899343T3 (pl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US69286605P 2005-06-21 2005-06-21
EP05105478A EP1736475A1 (en) 2005-06-21 2005-06-21 Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates
PCT/EP2006/063243 WO2006136530A1 (en) 2005-06-21 2006-06-15 Halogenated pyrazolo [1,5-a]pyrimidines, processes, uses as gaba-a receptors ligand, compositions and intermediates
EP06763737A EP1899343B1 (en) 2005-06-21 2006-06-15 Halogenated pyrazolo [1,5-a]pyrimidines, processes, uses as gaba-a receptors ligand, compositions and intermediates

Publications (1)

Publication Number Publication Date
PL1899343T3 true PL1899343T3 (pl) 2010-10-29

Family

ID=35311853

Family Applications (1)

Application Number Title Priority Date Filing Date
PL06763737T PL1899343T3 (pl) 2005-06-21 2006-06-15 Fluorowcowane pirazolo[1,5-a]pirymidyny, sposób ich wytwarzania, ich zastosowanie jako ligandów receptorów GABA-A, kompozycje je zawierające i związki pośrednie

Country Status (25)

Country Link
US (3) US8530482B2 (pl)
EP (2) EP1736475A1 (pl)
JP (1) JP5010591B2 (pl)
KR (1) KR101465802B1 (pl)
CN (1) CN101243089B (pl)
AR (1) AR054785A1 (pl)
AT (1) ATE467635T1 (pl)
AU (1) AU2006261025B2 (pl)
BR (1) BRPI0612075A2 (pl)
CA (1) CA2612726C (pl)
CY (1) CY1111452T1 (pl)
DE (1) DE602006014272D1 (pl)
DK (1) DK1899343T3 (pl)
ES (1) ES2345999T3 (pl)
HK (1) HK1116184A1 (pl)
MX (1) MX2007016340A (pl)
NO (1) NO339973B1 (pl)
PE (1) PE20070071A1 (pl)
PL (1) PL1899343T3 (pl)
PT (1) PT1899343E (pl)
RU (1) RU2478101C2 (pl)
SI (1) SI1899343T1 (pl)
TW (1) TWI382985B (pl)
UY (1) UY29618A1 (pl)
WO (1) WO2006136530A1 (pl)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1736475A1 (en) * 2005-06-21 2006-12-27 Ferrer Internacional, S.A. Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates
CA2643968A1 (en) * 2006-03-17 2007-09-27 Wyeth Pyrazolo[1,5-a]pyrimidine derivatives and methods of use thereof
EP1884516A1 (en) * 2006-08-04 2008-02-06 Ferrer Internacional, S.A. Pyrazolo[1,5-a]pyrimidines, processes, uses and compositions
EP1956021A1 (en) 2006-10-11 2008-08-13 Ferrer Internacional, S.A. Process for the manufacture of a crystalline pyrazolo[1,5-a]pyrimidine compound
EP1918290A1 (en) * 2006-10-11 2008-05-07 Ferrer Internacional, S.A. Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a] pyrimidin-7-yl]-phenyl}-N-methyl-acetamide
EP1921079A1 (en) * 2006-11-08 2008-05-14 Ferrer Internacional, S.A. Amorphous form of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a] pyrimidin-7-yl]-phenyl}-N-methyl-acetamide
PL2387557T3 (pl) * 2009-01-13 2013-12-31 Interquim Sa Sposób wytwarzania N-[5-(3-dimetyloamino-akryloilo)-2-fluoro-fenylo]-N-metylo-acetamidu
EP2982670B1 (en) 2013-04-04 2018-11-07 Takeda Pharmaceutical Company Limited Heterocyclic compound
JP2018199623A (ja) * 2015-10-22 2018-12-20 大正製薬株式会社 含窒素縮合複素環化合物

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4521422A (en) * 1983-06-23 1985-06-04 American Cyanamid Company Aryl and heteroaryl[7-(aryl and heteroaryl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones
US6399621B1 (en) * 1999-08-10 2002-06-04 American Cyanamid Company N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1, 5-α]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto
RU2003129060A (ru) * 2001-03-14 2005-04-10 Грюненталь ГмбХ (DE) Замещенные пиразоло-и тиазолопиримидины
EP1458717B1 (en) * 2001-12-21 2005-09-07 Bayer HealthCare AG Aroyl pyridinones
ES2222813B1 (es) * 2003-07-24 2005-12-16 Ferrer Internacional, S.A. N-(3-(3-sustituidas-pirazolo(1,5-a)pirimidin-7-il)-fenil)-sulfonamidas y composiciones y metodos relacionados.
WO2006033796A1 (en) * 2004-09-17 2006-03-30 Wyeth SUBSTITUTED PYRAZOLO [1,5-a] PYRIMIDINES AND PROCESS FOR MAKING SAME
WO2006033795A2 (en) * 2004-09-17 2006-03-30 Wyeth Substituted pyrazolo [1, 5-a] pyrimidines for inhibiting abnormal cell growth
CN100528875C (zh) 2005-02-18 2009-08-19 美德(江西)生物科技有限公司 无结晶型态的印地普隆及其制备方法
EP1736475A1 (en) * 2005-06-21 2006-12-27 Ferrer Internacional, S.A. Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates

Also Published As

Publication number Publication date
US8530482B2 (en) 2013-09-10
AU2006261025A1 (en) 2006-12-28
KR20080032104A (ko) 2008-04-14
ES2345999T3 (es) 2010-10-07
US20160368912A9 (en) 2016-12-22
TW200726769A (en) 2007-07-16
RU2478101C2 (ru) 2013-03-27
MX2007016340A (es) 2008-03-10
ATE467635T1 (de) 2010-05-15
CN101243089B (zh) 2011-07-06
US20130331610A1 (en) 2013-12-12
NO339973B1 (no) 2017-02-27
HK1116184A1 (en) 2008-12-19
RU2008101371A (ru) 2009-07-27
NO20080393L (no) 2008-03-10
BRPI0612075A2 (pt) 2010-10-19
UY29618A1 (es) 2006-10-31
DE602006014272D1 (de) 2010-06-24
US20130331401A1 (en) 2013-12-12
KR101465802B1 (ko) 2014-11-27
DK1899343T3 (da) 2010-09-06
PE20070071A1 (es) 2007-02-01
PT1899343E (pt) 2010-08-17
AR054785A1 (es) 2007-07-18
US20090111848A1 (en) 2009-04-30
SI1899343T1 (sl) 2010-09-30
EP1736475A1 (en) 2006-12-27
EP1899343B1 (en) 2010-05-12
JP2008543913A (ja) 2008-12-04
CA2612726A1 (en) 2006-12-28
CY1111452T1 (el) 2015-08-05
JP5010591B2 (ja) 2012-08-29
WO2006136530A1 (en) 2006-12-28
US10072000B2 (en) 2018-09-11
CN101243089A (zh) 2008-08-13
EP1899343A1 (en) 2008-03-19
AU2006261025B2 (en) 2011-09-08
TWI382985B (zh) 2013-01-21
CA2612726C (en) 2013-10-01

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