CY1107677T1 - Παραγωγα της 1-[indol-3-yl)carbonyl]piperazine - Google Patents

Παραγωγα της 1-[indol-3-yl)carbonyl]piperazine

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Publication number
CY1107677T1
CY1107677T1 CY20071100804T CY071100804T CY1107677T1 CY 1107677 T1 CY1107677 T1 CY 1107677T1 CY 20071100804 T CY20071100804 T CY 20071100804T CY 071100804 T CY071100804 T CY 071100804T CY 1107677 T1 CY1107677 T1 CY 1107677T1
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Cyprus
Prior art keywords
halogen
optionally substituted
alkyl
pain
derivatives
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CY20071100804T
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English (en)
Inventor
Phillip Martin Cowley
Wilson Caulfield
Jason Tierney
James Cairns
Julia Adam-Worrall
Mark York
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N.V. Organon
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Publication date
Application filed by N.V. Organon filed Critical N.V. Organon
Publication of CY1107677T1 publication Critical patent/CY1107677T1/el

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    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00Drugs for disorders of the respiratory 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • 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
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    • 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
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    • A61P27/06Antiglaucoma agents or miotics
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    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
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  • Pain & Pain Management (AREA)
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  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)

Abstract

Η παρούσα εφεύρεση αφορά σε παράγωγα 1-[(indol-3-yl)carbonyl]piperazine που έχει το γενικό τύπο (I), όπου R αντιπροσωπεύει 1-4 υποκατάστατα που επιλέγονται ανεξάρτητα από Η, (C1-4)alkyl (προαιρετικά υποκαθίστανται με αλογόνο), (C1-4) alkyloxy (προαιρετικά υποκαθίστανται με αλογόνο), αλογόνο, ΟΗ, ΝΗ2, CN και ΝO2. R1 είναι (C5-8)cycloalkyl ή (C5-8)cycloalkenyl. R2 είναι Η, μεθυλ ή αιθυλ. R3, R3', R4R4', R5, R5' και R6' ανεξάρτητα υδρογόνο ή (C1-4)alkyl, προαιρετικά υποκαθίστανται με (C1-4)alkyloxy, αλογόνο ή OH. R6 είναι υδρογόνο ή or (C1-4)alkyl, προαιρετικά υποκαθίστανται με (C1-4)alkyloxy, αλογόνο ή ΟΗ. Ή R6 σχηματίζει μαζί με R7 ένα κορεσμένο ετεροκυκλικό δακτύλιο με 4-7 μέλη, προαιρετικά περιέχει ένα επιπλέον ετεροάτομο που επιλέγεται από Ο και S. R7 σχηματίζει μαζί με R6 ένα κορεσμένο ετεροκυκλικό δακτύλιο με 4-7 μέλη, προαιρετικά περιέχει ένα επιπλέον ετεροάτομο που επιλέγεται από Ο και S. Ή R7 είναι Η, (C1-4)alkyl ή (C3-5)cycloalkyl, αφού οι αλκυλομάδες προαιρετικά υποκαθίστανται με ΟΗ, αλογόνο ή (C1-4) alkyloxy. Ή ένα φαρμακευτικά αποδεκτό άλας τους. Η εφεύρεση επίσης αφορά σε φαρμακευτικές συνθέσεις που περιλαμβάνουν τα εν λόγω παράγωγα 1-[(indol-3-yl)carbonyl]piperazine, και στη χρήση αυτών των παράγωγων για τη θεραπεία του πόνου, τέτοιου όπως περιεγχειρητικου πόνου, χρόνιου πόνου, νευροπαθητικού πόνου, και πόνου και σπαστικότατος που σχετίζεται με πολλαπλή σκλήρωση.
CY20071100804T 2002-06-21 2007-06-18 Παραγωγα της 1-[indol-3-yl)carbonyl]piperazine CY1107677T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02077505 2002-06-21
EP03760704A EP1549637B1 (en) 2002-06-21 2003-06-13 1- (indol-3-yl)carbonyl piperazine derivatives

Publications (1)

Publication Number Publication Date
CY1107677T1 true CY1107677T1 (el) 2013-04-18

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ID=29797228

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20071100804T CY1107677T1 (el) 2002-06-21 2007-06-18 Παραγωγα της 1-[indol-3-yl)carbonyl]piperazine

Country Status (33)

Country Link
US (1) US7304064B2 (el)
EP (1) EP1549637B1 (el)
JP (1) JP4408804B2 (el)
KR (1) KR20050009755A (el)
CN (1) CN1298716C (el)
AR (1) AR040274A1 (el)
AT (1) ATE361290T1 (el)
AU (1) AU2003250245B2 (el)
BR (1) BR0311960A (el)
CA (1) CA2490141C (el)
CO (1) CO5680419A2 (el)
CY (1) CY1107677T1 (el)
DE (1) DE60313640T2 (el)
DK (1) DK1549637T3 (el)
EC (1) ECSP045503A (el)
ES (1) ES2285183T3 (el)
HK (1) HK1076630A1 (el)
HR (1) HRP20041186A2 (el)
IL (1) IL165572A0 (el)
IS (1) IS2443B (el)
MX (1) MXPA04012856A (el)
NO (1) NO20045351L (el)
NZ (1) NZ537143A (el)
PE (1) PE20040578A1 (el)
PL (1) PL375152A1 (el)
PT (1) PT1549637E (el)
RS (1) RS111104A (el)
RU (1) RU2318821C2 (el)
SI (1) SI1549637T1 (el)
TW (1) TW200402417A (el)
UA (1) UA78317C2 (el)
WO (1) WO2004000832A1 (el)
ZA (1) ZA200410057B (el)

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TWI242015B (en) 1999-11-29 2005-10-21 Akzo Nobel Nv 6-mercapto-cyclodextrin derivatives: reversal agents for drug-induced neuromuscular block
US7091216B2 (en) 2002-08-02 2006-08-15 Merck & Co., Inc. Substituted furo[2,3-b]pyridine derivatives
DE10253426B4 (de) * 2002-11-15 2005-09-22 Elbion Ag Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung
ES2284076T3 (es) * 2003-12-17 2007-11-01 N.V. Organon Derivados triciclicos de 1-(indol-3-il)carbonil)piperazina como agonistas del receptor de cannabinoides cb1.
TWI330635B (en) * 2004-03-05 2010-09-21 Organon Nv (indol-3-yl)-heterocycle derivatives
AU2006268680B2 (en) * 2005-07-11 2012-11-22 Msd Oss B.V. Synergistic combination for the treatment of pain (cannabioid receptor agonist and opiod receptor agonist)
EP1917255A2 (en) * 2005-07-29 2008-05-07 F. Hoffmann-Roche AG Indol-3-yl-carbonyl-piperidin and piperazin derivatives
TW200745096A (en) * 2005-08-23 2007-12-16 Organon Nv Indole derivatives
US7763732B2 (en) 2005-08-24 2010-07-27 N.V. Organon Indole derivatives
BRPI0616404A2 (pt) * 2005-09-23 2011-06-21 Janssen Pharmaceutica Nv moduladores de canabinóide de 3-amido-tetraidro-indazolila substituìdo e uso dos mesmos
TW200848417A (en) 2007-02-22 2008-12-16 Organon Nv Indole derivatives
RU2387642C2 (ru) 2007-10-31 2010-04-27 Общество С Ограниченной Ответственностью "Бинатех" Производные 5-замещенных индол-3-карбоновой кислоты, обладающие противовирусной активностью, способ их получения и применение
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
US9783538B2 (en) 2013-12-20 2017-10-10 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
CN111566105A (zh) 2018-01-08 2020-08-21 豪夫迈·罗氏有限公司 作为MAGL抑制剂的八氢吡啶并[1,2-α]吡嗪类化合物
CN108752342A (zh) * 2018-08-17 2018-11-06 西安瑞联新材料股份有限公司 1-H-吡啶并[1,2-a]-6-氢吡嗪-1,4-二酮的制备方法
CN111100063B (zh) * 2018-10-25 2022-05-17 南京药石科技股份有限公司 一种合成2-氟甲基取代的吡咯烷、哌啶以及哌嗪衍生物的制备方法

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PT1549637E (pt) 2007-05-31
AR040274A1 (es) 2005-03-23
US20050250760A1 (en) 2005-11-10
BR0311960A (pt) 2005-03-22
CN1668611A (zh) 2005-09-14
JP2005533801A (ja) 2005-11-10
DK1549637T3 (da) 2007-07-16
ATE361290T1 (de) 2007-05-15
IL165572A0 (en) 2006-01-15
ZA200410057B (en) 2005-10-20
US7304064B2 (en) 2007-12-04
HK1076630A1 (en) 2006-01-20
PL375152A1 (en) 2005-11-28
ES2285183T3 (es) 2007-11-16
KR20050009755A (ko) 2005-01-25
CO5680419A2 (es) 2006-09-29
PE20040578A1 (es) 2004-09-15
MXPA04012856A (es) 2005-03-31
NO20045351L (no) 2005-01-20
CN1298716C (zh) 2007-02-07
HRP20041186A2 (en) 2005-06-30
CA2490141A1 (en) 2003-12-31
EP1549637A1 (en) 2005-07-06
IS7590A (is) 2004-12-09
RS111104A (en) 2007-02-05
TW200402417A (en) 2004-02-16
UA78317C2 (en) 2007-03-15
WO2004000832A1 (en) 2003-12-31
NZ537143A (en) 2005-05-27
RU2005101349A (ru) 2005-06-27
IS2443B (is) 2008-11-15
AU2003250245A1 (en) 2004-01-06
ECSP045503A (es) 2005-03-10
DE60313640D1 (de) 2007-06-14
RU2318821C2 (ru) 2008-03-10
JP4408804B2 (ja) 2010-02-03
SI1549637T1 (sl) 2007-10-31
AU2003250245B2 (en) 2008-07-03
EP1549637B1 (en) 2007-05-02
DE60313640T2 (de) 2007-12-27
CA2490141C (en) 2011-01-25

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