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RU2006145875A - Композиция для контроля нейропатической боли - Google Patents

Композиция для контроля нейропатической боли Download PDF

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RU2006145875A
RU2006145875A RU2006145875/04A RU2006145875A RU2006145875A RU 2006145875 A RU2006145875 A RU 2006145875A RU 2006145875/04 A RU2006145875/04 A RU 2006145875/04A RU 2006145875 A RU2006145875 A RU 2006145875A RU 2006145875 A RU2006145875 A RU 2006145875A
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Масаказу ЕСИМУРА (JP)
Масаказу ЕСИМУРА
Норимаса КАНАМИТСУ (JP)
Норимаса КАНАМИТСУ
Йутака ИТСУДЗИ (JP)
Йутака ИТСУДЗИ
Такаси ОСАКА (JP)
Такаси ОСАКА
Мотоко КАВАСИМА (JP)
Мотоко КАВАСИМА
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Маруиси Фармасьютикал Ко., Лтд. (Jp)
Маруиси Фармасьютикал Ко., Лтд.
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Publication of RU2006145875A publication Critical patent/RU2006145875A/ru

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    • CCHEMISTRY; METALLURGY
    • 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
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/46Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D209/56Ring systems containing three or more rings
    • C07D209/58[b]- or [c]-condensed
    • C07D209/62Naphtho [c] pyrroles; Hydrogenated naphtho [c] pyrroles
    • C07D209/64Naphtho [c] pyrroles; Hydrogenated naphtho [c] pyrroles with an oxygen atom in position 1
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (14)

1. Применение соединения, представленное формулой (I)
Figure 00000001
где R1 и R2 могут быть одинаковыми или разными и представляют С1-6алкильные группы, или R1 и R2 вместе формируют 6-членный конденсированный цикл с конъюгированными двойными связями или они вместе формируют звено -O-СН2-O-, -СН2-СН2-СН2- или СН2-O-СН2-;
Х является галогеном или С1-6алкокси или вместе с фенильным звеном, к которому Х присоединен, формирует группу (2)
Figure 00000002
;
m является целым числом от 0 до 2, причем, когда Х является С1-6алкокси-группой, m равно 0 или 1;
Y является
Figure 00000003
,
где R3 является линейным или разветвленным С1-6алкилом, линейным или разветвленным С3-6алкенилом, линейным или разветвленным С3-6алкинилом, С5-6циклоалкилом,
Figure 00000004
,
где R4 является С1-4 алкилом или
Figure 00000005
, или
и
Figure 00000006
Z является кислородом или серой, или его соль для производства фармацевтической композиции для контроля над нейропатической болью.
2. Применение по п.1, где R1 и R2 оба являются метилом.
3. Применение по п.1, где R1 и R2 взятые вместе формируют звено -O-СН2-O-, -СН2-СН2-СН2- или -СН2-O-СН2-.
4. Применение по п.1, где Х является галогеном в пара- и/или метаположении фенильного звена.
5. Применение по п.1, где Х является алкокси- в параположении фенильного звена.
6. Применение по п.1, где Х является водородом или формирует вместе с фенильным звеном, к которому Х присоединен, группу
Figure 00000007
7. Применение по любому из пп.1-6, где Y является
Figure 00000008
и R3 выбирают из группы, состоящей из линейного С1-6алкила, -СН(СН3)2, -СН2СН=СН2, -СН2-С≡CH, С(=O)СН3 и групп
Figure 00000009
,
циклопентила или циклогексила.
8. Применение по любому из пп.1-6, где Y является
Figure 00000010
9. Применение по любому из пп.1-6, где Z является кислородом.
10. Применение по п.1, где соединение формулы (I) выбирают из приведенных ниже
Figure 00000011
, где
R5 L
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000013
Figure 00000015
Figure 00000013
Figure 00000016
Figure 00000013
Figure 00000017
Figure 00000013
Figure 00000018
Figure 00000013
Figure 00000012
Figure 00000019
Figure 00000020
Figure 00000013
Figure 00000021
Figure 00000022
Figure 00000021
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000021
Figure 00000025
Figure 00000021
Figure 00000026
Figure 00000021
Figure 00000027
Figure 00000021
Figure 00000028
Figure 00000024
Figure 00000029
11. Применение по п.1, где соединение формулы (I) выбирают из приведенных ниже
Figure 00000030
, где
М R5 L CH2CH2CH2
Figure 00000024
Figure 00000031
CH2CH2CH2
Figure 00000015
Figure 00000032
CH2CH2CH2
Figure 00000015
Figure 00000033
CH2CH2CH2
Figure 00000015
Figure 00000034
OCH2O
Figure 00000024
Figure 00000035
OCH2O
Figure 00000015
Figure 00000036
CH2OCH2
Figure 00000015
Figure 00000037
CH2OCH2
Figure 00000015
Figure 00000038
CH=CH-CH=CH
Figure 00000039
Figure 00000040
12. Способ контроля над нейропатической болью, который включает назначение эффективного количества соединения, определенного в п.1, субъекту, нуждающемуся в контроле над болью.
13. Соединение, выбранное из группы, состоящей из
Figure 00000041
, где
R5 L
Figure 00000042
Figure 00000040
Figure 00000024
Figure 00000038
Figure 00000015
Figure 00000038
Figure 00000015
Figure 00000043
Figure 00000024
Figure 00000029
Figure 00000044
, где
М R5 L CH2CH2CH2
Figure 00000015
Figure 00000038
CH2CH2CH2
Figure 00000015
Figure 00000033
CH2CH2CH2
Figure 00000015
Figure 00000034
OCH2O
Figure 00000015
Figure 00000038
CH2OCH2
Figure 00000015
Figure 00000045
CH2OCH2
Figure 00000015
Figure 00000038
CH=CH-CH=CH
Figure 00000046
Figure 00000045
14. Соединение по п.13, которое выбирают из группы, состоящей из
Figure 00000041
, где
R5 L
Figure 00000024
Figure 00000038
Figure 00000015
Figure 00000038
Figure 00000024
Figure 00000029
Figure 00000047
, где
М R5 L CH2CH2CH2
Figure 00000015
Figure 00000038
CH2CH2CH2
Figure 00000015
Figure 00000033
CH2CH2CH2
Figure 00000015
Figure 00000034
OCH2O
Figure 00000015
Figure 00000038
CH2OCH2
Figure 00000015
Figure 00000038
RU2006145875/04A 2004-05-24 2005-05-23 Композиция для контроля нейропатической боли RU2006145875A (ru)

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JP2004153206 2004-05-24

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US (1) US20080021042A1 (ru)
EP (1) EP1749817A4 (ru)
JP (1) JPWO2005113501A1 (ru)
CN (1) CN1956955A (ru)
AU (1) AU2005245292A1 (ru)
BR (1) BRPI0511546A (ru)
CA (1) CA2563968A1 (ru)
EC (1) ECSP067107A (ru)
IL (1) IL178814A0 (ru)
MX (1) MXPA06013766A (ru)
NO (1) NO20064868L (ru)
RU (1) RU2006145875A (ru)
TW (1) TW200602318A (ru)
WO (1) WO2005113501A1 (ru)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2343145C2 (ru) * 2002-11-26 2009-01-10 Маруиси Фармасьютикал Ко., Лтд. Производные изоиндолина
EP2044019A1 (en) * 2006-07-12 2009-04-08 Astra Zeneca AB 3-oxoisoindoline-1-carboxamide derivatives as analgesic agents
CN104803905B (zh) * 2015-04-17 2017-10-10 复旦大学 一种合成异吲哚啉‑1‑酮衍生物的方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2117740B1 (ru) * 1970-12-14 1974-04-12 Rhone Poulenc Sa
DE3378763D1 (en) * 1982-04-02 1989-02-02 Takeda Chemical Industries Ltd Condensed pyrrolinone derivatives, and their production
WO1984003089A1 (fr) * 1983-02-05 1984-08-16 Takeda Chemical Industries Ltd Derives condenses de pyrrolinone
IL133621A0 (en) * 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
RU2343145C2 (ru) * 2002-11-26 2009-01-10 Маруиси Фармасьютикал Ко., Лтд. Производные изоиндолина

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IL178814A0 (en) 2007-03-08
NO20064868L (no) 2007-02-26
JPWO2005113501A1 (ja) 2008-03-27
TW200602318A (en) 2006-01-16
MXPA06013766A (es) 2007-02-08
EP1749817A4 (en) 2007-12-26
AU2005245292A1 (en) 2005-12-01
BRPI0511546A (pt) 2008-01-02
CA2563968A1 (en) 2005-12-01
WO2005113501A1 (ja) 2005-12-01
US20080021042A1 (en) 2008-01-24
EP1749817A1 (en) 2007-02-07
CN1956955A (zh) 2007-05-02

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