RU2004132198A - Терапевтическое применение селективных ингибиторов pde10 - Google Patents

Терапевтическое применение селективных ингибиторов pde10 Download PDF

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RU2004132198A
RU2004132198A RU2004132198/15A RU2004132198A RU2004132198A RU 2004132198 A RU2004132198 A RU 2004132198A RU 2004132198/15 A RU2004132198/15 A RU 2004132198/15A RU 2004132198 A RU2004132198 A RU 2004132198A RU 2004132198 A RU2004132198 A RU 2004132198A
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disorder
neurodegenerative
selective
spiky
neurons
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RU2004132198/15A
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Лоррейн Энн ЛЕБЕЛ (US)
Лоррейн Энн ЛЕБЕЛ
Франк Сэмьюэль МЕННИТИ (US)
Франк Сэмьюэль МЕННИТИ
Кристофер Джозеф ШМИДТ (US)
Кристофер Джозеф ШМИДТ
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Пфайзер Продактс Инк. (Us)
Пфайзер Продактс Инк.
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    • AHUMAN NECESSITIES
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    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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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    • G01N33/6893Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to diseases not provided for elsewhere
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    • G01N2800/302Schizophrenia

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Claims (9)

1. Способ определения наличия у химического соединения активности селективного ингибитора PDE10, включающий:
a) введение химического соединения в культуру медиальных шиповатых нейронов; и
b) измерение возможного повышения фосфорилирования CREB в культуре; повышение фосфорилирования CREB, тем самым показывает, что соединение, использованное в стадии (a) обладает селективной ингибиторной активностью в отношении PDE10.
2. Способ определения наличия у химического соединения активности селективного ингибитора PDE10, включающий:
a) введение химического соединения в культуру медиальных шиповатых нейронов; и
b) измерение возможного повышения количества продуцируемого GABA медиальными шиповатыми нейронами в указанной культуре;
повышение продукции GABA указанными медиальными шиповатыми нейронами, тем самым показывает, что соединение, использованное в стадии (a) обладает селективной ингибиторной активностью в отношении PDE10.
3. Способ лечения расстройства, выбранного из обсессивно/компульсивного расстройства, синдрома Туретта и других тиков у млекопитающих, включающий введение указанному млекопитающему количества селективного ингибитора PDE10, эффективного для лечения указанного расстройства.
4. Способ лечения нейродегенеративного расстройства или состояния у млекопитающего, включающий введение указанному млекопитающему количества селективного ингибитора PDE10, эффективного для лечения указанного расстройства или состояния.
5. Способ по п. 4, где нейродегенеративное расстройство или состояние выбрано из болезни Паркинсона; болезни Гентингтона; деменции, например, деменции при болезни Альцгеймера, мультиинфарктной деменции, деменции при СПИДе; и фронто-темпоральной деменции; нейродегенеративного процесса, связанного с травмой головного мозга; нейродегенеративного процесса, связанного с инсультом, нейродегенеративного процесса, связанного с инфарктом мозга; нейродегенеративного процесса, вызванного гипогликемией; нейродегенеративного процесса, связанного с эпилептическими припадками; нейродегенеративного процесса, связанного с нейротоксическим отравлением; и множественной системной атрофии.
6. Способ по п. 4, где нейродегенеративное расстройство или состояние включает в себя нейродегенерацию медиальных шиповатых нейронов млекопитающих.
7. Способ по п. 5, где нейродегенеративным расстройством или состоянием является болезнь Гентингтона.
8. Способ лечения двигательного расстройства, выбранного из болезни Гентингтона и дискинезии, связанной с терапевтическим применением агонистов допамина, у млекопитающих, включающий введение указанному млекопитающему количества селективного ингибитора PDE10, эффективного для ингибирования PDE10.
9. Способ лечения расстройства, выбранного из обсессивно/компульсивного расстройства, синдрома Туретта и других тиков у млекопитающих, включающий введение указанному млекопитающему количества селективного ингибитора PDE10, эффективного для ингибирования PDE10.
RU2004132198/15A 2002-05-03 2003-04-22 Терапевтическое применение селективных ингибиторов pde10 RU2303259C2 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US10/139,183 US20030018047A1 (en) 2001-04-20 2002-05-03 Therapeutic use of selective PDE10 inhibitors
US10/139,183 2002-05-03
US10/177,018 2002-06-20
US10/177,018 US20030032579A1 (en) 2001-04-20 2002-06-20 Therapeutic use of selective PDE10 inhibitors

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RU2303259C2 RU2303259C2 (ru) 2007-07-20

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US (2) US20030032579A1 (ru)
EP (1) EP1504118A2 (ru)
JP (1) JP2005524402A (ru)
KR (1) KR20040106455A (ru)
CN (1) CN1668761A (ru)
AU (1) AU2003222395A1 (ru)
BR (1) BR0309746A (ru)
CA (1) CA2484600A1 (ru)
HR (1) HRP20041029A2 (ru)
IL (1) IL164778A0 (ru)
MX (1) MXPA04010777A (ru)
NO (1) NO20044470L (ru)
PL (1) PL373943A1 (ru)
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RU2657540C2 (ru) * 2012-06-26 2018-06-14 Янссен Фармацевтика Нв Комбинации, содержащие ингибиторы pde 2, такие как 1-арил-4-метил-[1,2,4]триазоло[4,3-а]хиноксалиновые соединения, и ингибиторы pde 10, для применения в лечении неврологических или метаболических расстройств

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