公开(公告)号：ZA9400069B

公开(公告)日：1996-02-01

申请号：ZA9400069

申请日：1994-01-06

Applicant: PF MEDICAMENT

Inventor： COLPAERT FRANCIS ,  IMBERT THIERRY

IPC: C07D405/04 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/415 ,  A61P25/28 ,  A61K

CPC classification number: A61K31/415

公开(公告)号：ZA9404281B

公开(公告)日：1995-02-10

申请号：ZA9404281

申请日：1994-06-16

Applicant: PF MEDICAMENT

Inventor： COLPAERT FRANCIS ,  BRILEY MICHAEL ,  IMBERT THIERRY

IPC: C07D405/04 ,  A61K31/415 ,  A61K31/4178 ,  A61P25/00 ,  A61P25/16 ,  A61K

CPC classification number: A61K31/415

公开(公告)号：AU7230894A

公开(公告)日：1995-02-06

申请号：AU7230894

申请日：1994-07-07

Applicant: PF MEDICAMENT

Inventor： COLPAERT FRANCIS ,  BRILEY MICHAEL ,  IMBERT THIERRY

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

Abstract: PCT No. PCT/FR94/00841 Sec. 371 Date Jan. 11, 1996 Sec. 102(e) Date Jan. 11, 1996 PCT Filed Jul. 7, 1994 PCT Pub. No. WO95/01791 PCT Pub. Date Jan. 19, 1995The present invention relates to the use of efaroxan and derivatives for the treatment of Alzheimer's disease.

公开(公告)号：CA2518591C

公开(公告)日：2012-05-15

申请号：CA2518591

申请日：2004-03-15

Applicant: PF MEDICAMENT

Inventor： COLPAERT FRANCIS ,  VACHER BERNARD

IPC: A61K31/445 ,  A61P25/00

Abstract: La présente invention concerne l'utilisation d'un composé de formule (I) et de ses sels thérapeutiquement acceptables dans laquelle notamment u représente un radical méthyle ; v et w représentent un atome d'hydrogène x représente un atome de fluor; y représente un atome de chlore ; z représente un atome de fluor ; A représente un atome d'hydrogène ou un groupe aminométhyle, ainsi que de ses sels d'addition avec des acides minéraux ou organiques pharmaceutiquement acceptables, pour la préparation d'un médicament destiné au traitement des symptômes de la douleur chronique d'origine neuropathique ou psychogène.

公开(公告)号：AU2003301277B2

公开(公告)日：2009-06-18

申请号：AU2003301277

申请日：2003-10-16

Applicant: PF MEDICAMENT

Inventor： COLPAERT FRANCIS ,  VACHER BERNARD ,  KOEK WOUTER ,  CUISIAT STEPHANE

IPC: C07D307/86 ,  A61P25/18 ,  C07C45/29 ,  C07C47/548 ,  C07C47/55 ,  C07D213/48 ,  C07D307/94 ,  C07D405/12

Abstract: Cyclopentenyl benzyl or heteroaryl amines (I) are new. Cyclopentenyl benzyl or heteroaryl amines of formula (I) and their salts and salt hydrates, their tautomeric and enantiomeric forms, and mixtures, including racemic mixtures, are new. a = single or double bond; W = CH, CH2, CHCH3, CCH3, C(CH3)2, C(CH2)2 (forming a spiro-cyclopropane ring), or C(CH2)3 (forming a spiro-cyclobutane ring); X = CH or N; Y = H or F. An Independent claim is also included for intermediates of formula (II).

公开(公告)号：SI1603564T1

公开(公告)日：2007-10-31

申请号：SI200430374

申请日：2004-03-15

Applicant: PF MEDICAMENT

Inventor： COLPAERT FRANCIS ,  VACHER BERNARD

IPC: A61K31/00 ,  A61P25/00

公开(公告)号：DE60305339T2

公开(公告)日：2007-02-01

申请号：DE60305339

申请日：2003-10-16

Applicant: PF MEDICAMENT

Inventor： VACHER BERNARD ,  CUISIAT STEPHANE ,  KOEK WOUTER ,  COLPAERT FRANCIS

IPC: C07D307/86 ,  A61K31/343 ,  A61P25/18 ,  C07C45/29 ,  C07C47/548 ,  C07C47/55 ,  C07D213/48 ,  C07D307/94 ,  C07D405/12

Abstract: Cyclopentenyl benzyl or heteroaryl amines (I) are new. Cyclopentenyl benzyl or heteroaryl amines of formula (I) and their salts and salt hydrates, their tautomeric and enantiomeric forms, and mixtures, including racemic mixtures, are new. a = single or double bond; W = CH, CH2, CHCH3, CCH3, C(CH3)2, C(CH2)2 (forming a spiro-cyclopropane ring), or C(CH2)3 (forming a spiro-cyclobutane ring); X = CH or N; Y = H or F. An Independent claim is also included for intermediates of formula (II).

公开(公告)号：DE60215947D1

公开(公告)日：2006-12-21

申请号：DE60215947

申请日：2002-07-11

Applicant: PF MEDICAMENT

Inventor： COLPAERT FRANCIS ,  BRUINS SLOT LIESBETH ,  KOEK WOUTER ,  TARAYRE JEAN-PIERRE ,  VACHER BERNARD

IPC: A61K31/4545 ,  C07D401/12 ,  A61P25/36

Abstract: The invention concerns compounds of general formula (I) for treating opioid drug dependence.

公开(公告)号：AT326456T

公开(公告)日：2006-06-15

申请号：AT03808761

申请日：2003-10-16

Applicant: PF MEDICAMENT

Inventor： VACHER BERNARD ,  CUISIAT STEPHANE ,  KOEK WOUTER ,  COLPAERT FRANCIS

IPC: A61P25/18 ,  C07C45/29 ,  C07C47/548 ,  C07C47/55 ,  C07D213/48 ,  C07D307/86 ,  C07D307/94 ,  C07D405/12 ,  A61K31/343

Abstract: Cyclopentenyl benzyl or heteroaryl amines (I) are new. Cyclopentenyl benzyl or heteroaryl amines of formula (I) and their salts and salt hydrates, their tautomeric and enantiomeric forms, and mixtures, including racemic mixtures, are new. a = single or double bond; W = CH, CH2, CHCH3, CCH3, C(CH3)2, C(CH2)2 (forming a spiro-cyclopropane ring), or C(CH2)3 (forming a spiro-cyclobutane ring); X = CH or N; Y = H or F. An Independent claim is also included for intermediates of formula (II).

公开(公告)号：HK1079120A1

公开(公告)日：2006-03-31

申请号：HK06101061

申请日：2006-01-24

Applicant: PF MEDICAMENT

Inventor： COLPAERT FRANCIS ,  VACHER BERNARD

IPC: A61K20060101 ,  A61K31/445 ,  A61P20060101 ,  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.