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    USE OF EFAXORAN AND ITS DERIVATIVES FOR THE PRODUCTION OF DRUGS FOR TREATING NEURODEGENERATIVE DISEASES
    2.
    发明申请
    USE OF EFAXORAN AND ITS DERIVATIVES FOR THE PRODUCTION OF DRUGS FOR TREATING NEURODEGENERATIVE DISEASES 审中-公开
    EFAXORAN及其衍生物用于生产用于治疗神经病变性疾病的药物的用途

    公开(公告)号：WO9501791A2

    公开(公告)日：1995-01-19

    申请号：PCT/FR9400841

    申请日：1994-07-07

    Applicant: PF MEDICAMENT ,  COLPAERT FRANCIS ,  BRILEY MICHAEL ,  IMBERT THIERRY

    Inventor： COLPAERT FRANCIS ,  BRILEY MICHAEL ,  IMBERT THIERRY

    IPC: C07D405/04 ,  A61K31/415 ,  A61K31/4178 ,  A61P25/00 ,  A61P25/28

    CPC classification number: A61K31/4178 ,  A61K31/415

    Abstract: Use of a compound of general formula (I) wherein R1 is a hydrogen atom, a linear or branched C1-C6 alkyl radical, R2 is a hydrogen atom, a methyl, chloro, bromo or fluoro group, and R3 is a hydrogen atom, a methyl, hydroxy, methoxy, fluoro, chloro or bromo group, and its therapeutically acceptable salts, its racemic or optically active isomers, for the preparation of a drug for treating Alzheimer-like senile dementia, pre-Alzheimer syndrome, progressive supranuclear palsy and other neurodegenerative diseases.

    Abstract translation: 使用通式（I）的化合物，其中R 1为氢原子，直链或支链C 1 -C 6烷基，R 2为氢原子，甲基，氯，溴或氟基团，R 3为氢原子， 甲基，羟基，甲氧基，氟，氯或溴基及其治疗上可接受的盐，其外消旋或旋光异构体，用于制备用于治疗阿尔茨海默氏老年性痴呆，前阿尔茨海默病综合征，进行性核上性麻痹的药物和 其他神经退行性疾病。

    USE OF PYRIDIN-2-YLMETHYLAMINE DERIVATIVES FOR THE TREATMENT OF CHRONIC NEUROPATHOLOGICAL OR PSYCHOGENIC PAIN SYMPTOMS
    3.
    发明申请
    USE OF PYRIDIN-2-YLMETHYLAMINE DERIVATIVES FOR THE TREATMENT OF CHRONIC NEUROPATHOLOGICAL OR PSYCHOGENIC PAIN SYMPTOMS 审中-公开
    用于治疗慢性神经病学或心脏病性疼痛症状的吡啶-2-甲基胺衍生物的使用

    公开(公告)号：WO2004083171A3

    公开(公告)日：2004-12-23

    申请号：PCT/FR2004000630

    申请日：2004-03-15

    Applicant: PF MEDICAMENT ,  COLPAERT FRANCIS ,  VACHER BERNARD

    Inventor： COLPAERT FRANCIS ,  VACHER BERNARD

    IPC: A61K31/445 ,  A61P25/00

    CPC classification number: A61K31/445

    Abstract: The invention relates to the use of a compound of formula (I) and the therapeutically-acceptable salts thereof, more particularly where u = methyl, v and w = H, x = F, y = Cl, z = F, A = H or aminomethyl and the pharmaceutically-acceptable addition salts with mineral or organic acids, for the production of a medicament for the treatment of chronic pain symptoms of neuropathological or psychogenic origin.

    Abstract translation: 本发明涉及式（I）化合物及其治疗上可接受的盐，特别是其中u =甲基，v和w = H，x = F，y = Cl，z = F，A = H 或氨基甲基和药学上可接受的与矿物或有机酸的加成盐，用于制备用于治疗神经病理学或心源性起源的慢性疼痛症状的药物。

    Use of pyridine-2-ylmethylamine derivatives for the production of a medicament for the treatment of chronic pain symptoms of neuropathological or psychogenic origin
    5.
    发明专利
    Use of pyridine-2-ylmethylamine derivatives for the production of a medicament for the treatment of chronic pain symptoms of neuropathological or psychogenic origin 未知

    公开(公告)号：AU2004222051B2

    公开(公告)日：2009-01-15

    申请号：AU2004222051

    申请日：2004-03-15

    Applicant: PF MEDICAMENT

    Inventor： COLPAERT FRANCIS ,  VACHER BERNARD

    IPC: A61K31/445 ,  A61P25/00

    Abstract: The use of 1-benzoyl-4-(((pyridin-2-ylmethyl)-amino)-methyl)-piperidine derivatives (I) for treating the symptoms of chronic pain of neuropathic or psychogenic origin is new. The use of pyridine derivatives of formula (I), or their mineral or organic acid addition salts, is claimed in the production of medicaments for treating the symptoms of chronic pain of neuropathic or psychogenic origin. [Image] U : H; or may also be Me if V = W = H; V : H or Cl; or may also be Me if U = W = H; W : H or F; or may also be Me if U = V = H; X : H or F; Y : Cl or Me; Z : H, F, Cl or Me; A : H, F, Cl, 1-5C alkyl, fluoroalkyl (e.g. CH 2F, CHF 2, CF 3, CHFMe or CF 2Me), 3-5C cycloalkyl, optionally substituted 5-membered aromatic heterocyclyl containing 1-4 of N, O and/or S as heteroatom(s) (provided that not more than one O and/or S is present), OR 1, SR 1, NR 2R 3, azetidino, pyrrolidino or alkoxycarbonyl (preferably COOMe or COOEt); R 11-5C alkyl, CH 2F, CF 3 or 3-5C cycloalkyl; R 2, R 3H, 1-5C alkyl, CF 3 or cyclopropyl. ACTIVITY : Analgesic. In tests for activity against central neuropathic pain induced by spinal column lesions in rats (see Pain, 1996, 66, 279-286), (3-chloro-4-fluorophenyl)-(4-fluoro-(((5-methyl-pyridin-2-ylmethyl)-amino)-methyl)-piperidin-1-yl)-methanone (Ia) was administered (as the fumarate) at a constant rate of 0.63 mg per day for 14 days using an implanted analgesic pump. Statistically significant analgesia was observed from day 10 of the treatment (demonstrating symptomatic analgesic action); and the analgesia remained at the same level from day 15 after cessation of the treatment for a further 14 days (demonstrating curative analgesic action). MECHANISM OF ACTION : 5-HT-1A receptor agonist.

    UTILIZACION DE DERIVADOS DE PIRIDIN-2-IL-METILAMINA PARA EL TRATAMIENTO DE LOS SINTOMAS DEL DOLOR CRONICO DE ORIGEN NEUROPATICO O PSICOGENO.
    7.
    发明专利
    UTILIZACION DE DERIVADOS DE PIRIDIN-2-IL-METILAMINA PARA EL TRATAMIENTO DE LOS SINTOMAS DEL DOLOR CRONICO DE ORIGEN NEUROPATICO O PSICOGENO. 未知

    公开(公告)号：ES2289494T3

    公开(公告)日：2008-02-01

    申请号：ES04720637

    申请日：2004-03-15

    Applicant: PF MEDICAMENT

    Inventor： COLPAERT FRANCIS ,  VACHER BERNARD

    IPC: A61K31/445 ,  A61P25/00

    Abstract: Utilización de un compuesto de fórmula (I) en la que: u representa un átomo de hidrógeno o un radical metilo con la reserva de que cuando u es un radical metilo, entonces v y w representan un átomo de hidrogeno; v representa un átomo de hidrógeno, un átomo de cloro o un radical metilo con la reserva de que cuando v es un radical metilo, entonces u y w representan un átomo de hidrogeno; w representa un átomo de hidrógeno, un átomo de flúor o un radical metilo con la reserva de que cuando w es un radical metilo entonces u y v representan un átomo de hidrogeno; x representa un átomo de hidrógeno o un átomo de flúor; y representa un átomo de cloro o un radical metilo; z representa un átomo de hidrógeno o un átomo de flúor o un átomo de cloro o un radical metilo; A representa: - un átomo de hidrógeno o un átomo de flúor o un átomo de cloro; - un radical alquilo con C1-C5, i.e. un resto de hidrocarburos alifáticos saturados de cadena recta o ramificada, que contienen 1 a 5 átomos de carbono tal como metilo, etilo, propilo, butilo, pentilo, isopropilo, 1-metil-etilo, 1-metil-propilo, 1-metil-butilo, 2-metil-propilo, 2-metil-butilo o 3-metil-butilo, 1-etil-propilo, 2-etil-propilo; - un radical fluoroalquilo tal como monofluorometilo (-CH2F) o un difluormetilo (-CHF2) o trifluorometilo (-CF3) o 1-fluoro-1-etilo (-CHFCH3) o 1, 1-difluoro-1-etilo (-CF2CH3); - un radical ciclopropilo o ciclobutilo o ciclopentilo; - un grupo heterocíclico aromático de 5 eslabones, sustituido o no, que contiene 1, 2, 3 ó 4 heteroátomos seleccionados de entre el nitrógeno, el oxígeno y el azufre sin que sin embargo esté presente más de un átomo de oxígeno y/o de azufre en el heterociclo A. - siendo los heterociclos aromáticos preferentemente : furano-2-il, (O.CH:CH.CH:C-) o furano-3-il, (CH:CH.O.CH:C-) o 1H-pirrol-2-il, (NH.CH:CH.CH:C-) o 1H-pirrol-3-il, (CH:CH.NH.CH:C-) o 1-metil-pirrol-2-il, (N(CH3).CH:CH.CH:C-) o 1-metil-pirrol-3-il, (CH:CH.N(CH3).CH:C-) o tiofen-2-il, (S.CH:CH.CH:C-) o tiofen-3-il, (CH:CH.S.CH:C-) o pirazol-1-il, (N:CH.CH:CH.N-) o 1H-pirazol-3-il, (CH:CH.NH.N:C-) o 1H-pirazol-4-il, (CH:N.NH.CH:C-) o 1-metil-pirazol-3-il, (CH:CH.N(CH3).N:C-) o imidazol-1-il, (CH:N.CH:CH.N-) o 1H-imidazol-2-il, (NH.CH:CH.N:C-) o 1H-imidazol-4-il, (N:CH.NH.CH:C-) o oxazol-2-il, (O.CH:CH.N:C-) o oxazol-4-il, (N:CH.O.CH:C-) o oxazol-5-il, (O.CH:N.CH:C-) o isoxazol-5-il, (O.N:CH.CH:C-) o isoxazol-4-il, (CH:N.O.CH:C-) o isoxazol-3-il, (CH:CH.O.N:C-) o tiazol-2-il, (S.CH:CH.N:C-) o tiazol-4-il, (N:CH.S.CH:C-) o tiazol-5-il, (S.CH:N.CH:C-) o isotiazol-5-il, (S.N:CH.CH:C-) o isotiazol-4-il, (CH:N.S.CH:C-) o isotiazol-3-il, (CH:CH.S.N:C-) o [1, 2, 4]triazol-1-il, (CH:N.CH:N.N-) o 1H-[1, 2, 4]triazol-3-il, (N:CH.NH.N:C-) o [1, 2, 4]oxadiazol-3-il, (N:CH.O.N:C-) o [1, 2, 4]oxadiazol-5-il, (O.N:CH.N:C-) o 5-metil-[1, 2, 4]oxadiazol-3-il, (N:C(CH3).O.N:C-) o 1H-tetrazol-5-il, (NH.N:N.N:C); - un grupo alcoxi (R1O-) o alquiltio (R1S-) en el que el radical R1 representa: * un radical alquilo con C1-C5 talcomo el definido anteriormente, * un radical monofluorometilo o trifluorometilo, * un radical ciclopropilo o ciclobutilo o ciclopentilo; - un grupo amino de tipo II en el que R2 y R3 idénticos o diferentes representan el hidrógeno, o un radical alquilo con C1-C5 tal como se ha definido anteriormente o un grupo ciclopropil o un grupo trifluorometilo; - un grupo amino cíclico saturado de tipo III

    8.
    发明专利
    未知

    公开(公告)号：FR2852244B1

    公开(公告)日：2007-09-07

    申请号：FR0303099

    申请日：2003-03-13

    Applicant: PF MEDICAMENT

    Inventor： COLPAERT FRANCIS ,  VACHER BERNARD

    IPC: A61K31/4545 ,  A61K31/445 ,  A61P25/00

    Abstract: The use of 1-benzoyl-4-(((pyridin-2-ylmethyl)-amino)-methyl)-piperidine derivatives (I) for treating the symptoms of chronic pain of neuropathic or psychogenic origin is new. The use of pyridine derivatives of formula (I), or their mineral or organic acid addition salts, is claimed in the production of medicaments for treating the symptoms of chronic pain of neuropathic or psychogenic origin. [Image] U : H; or may also be Me if V = W = H; V : H or Cl; or may also be Me if U = W = H; W : H or F; or may also be Me if U = V = H; X : H or F; Y : Cl or Me; Z : H, F, Cl or Me; A : H, F, Cl, 1-5C alkyl, fluoroalkyl (e.g. CH 2F, CHF 2, CF 3, CHFMe or CF 2Me), 3-5C cycloalkyl, optionally substituted 5-membered aromatic heterocyclyl containing 1-4 of N, O and/or S as heteroatom(s) (provided that not more than one O and/or S is present), OR 1, SR 1, NR 2R 3, azetidino, pyrrolidino or alkoxycarbonyl (preferably COOMe or COOEt); R 11-5C alkyl, CH 2F, CF 3 or 3-5C cycloalkyl; R 2, R 3H, 1-5C alkyl, CF 3 or cyclopropyl. ACTIVITY : Analgesic. In tests for activity against central neuropathic pain induced by spinal column lesions in rats (see Pain, 1996, 66, 279-286), (3-chloro-4-fluorophenyl)-(4-fluoro-(((5-methyl-pyridin-2-ylmethyl)-amino)-methyl)-piperidin-1-yl)-methanone (Ia) was administered (as the fumarate) at a constant rate of 0.63 mg per day for 14 days using an implanted analgesic pump. Statistically significant analgesia was observed from day 10 of the treatment (demonstrating symptomatic analgesic action); and the analgesia remained at the same level from day 15 after cessation of the treatment for a further 14 days (demonstrating curative analgesic action). MECHANISM OF ACTION : 5-HT-1A receptor agonist.

    10.
    发明专利
    未知

    公开(公告)号：AT366111T

    公开(公告)日：2007-07-15

    申请号：AT04720637

    申请日：2004-03-15

    Applicant: PF MEDICAMENT

    Inventor： COLPAERT FRANCIS ,  VACHER BERNARD

    IPC: A61K31/445 ,  A61P25/00

    Abstract: The use of 1-benzoyl-4-(((pyridin-2-ylmethyl)-amino)-methyl)-piperidine derivatives (I) for treating the symptoms of chronic pain of neuropathic or psychogenic origin is new. The use of pyridine derivatives of formula (I), or their mineral or organic acid addition salts, is claimed in the production of medicaments for treating the symptoms of chronic pain of neuropathic or psychogenic origin. [Image] U : H; or may also be Me if V = W = H; V : H or Cl; or may also be Me if U = W = H; W : H or F; or may also be Me if U = V = H; X : H or F; Y : Cl or Me; Z : H, F, Cl or Me; A : H, F, Cl, 1-5C alkyl, fluoroalkyl (e.g. CH 2F, CHF 2, CF 3, CHFMe or CF 2Me), 3-5C cycloalkyl, optionally substituted 5-membered aromatic heterocyclyl containing 1-4 of N, O and/or S as heteroatom(s) (provided that not more than one O and/or S is present), OR 1, SR 1, NR 2R 3, azetidino, pyrrolidino or alkoxycarbonyl (preferably COOMe or COOEt); R 11-5C alkyl, CH 2F, CF 3 or 3-5C cycloalkyl; R 2, R 3H, 1-5C alkyl, CF 3 or cyclopropyl. ACTIVITY : Analgesic. In tests for activity against central neuropathic pain induced by spinal column lesions in rats (see Pain, 1996, 66, 279-286), (3-chloro-4-fluorophenyl)-(4-fluoro-(((5-methyl-pyridin-2-ylmethyl)-amino)-methyl)-piperidin-1-yl)-methanone (Ia) was administered (as the fumarate) at a constant rate of 0.63 mg per day for 14 days using an implanted analgesic pump. Statistically significant analgesia was observed from day 10 of the treatment (demonstrating symptomatic analgesic action); and the analgesia remained at the same level from day 15 after cessation of the treatment for a further 14 days (demonstrating curative analgesic action). MECHANISM OF ACTION : 5-HT-1A receptor agonist.

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