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1. WO1999006384 - 1-(N-PHENYLAMINOALKYL)-PIPERAZINE DERIVATIVES SUBSTITUTED AT POSITION 2 OF THE PHENYL RING

Publication Number WO/1999/006384
Publication Date 11.02.1999
International Application No. PCT/EP1998/004804
International Filing Date 31.07.1998
Chapter 2 Demand Filed 23.02.1999
IPC
C07D 209/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
08with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 213/81 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
81Amides; Imides
C07D 213/82 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
81Amides; Imides
82in position 3
C07D 241/24 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
241Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02not condensed with other rings
10having three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 295/13 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04with substituted hydrocarbon radicals attached to ring nitrogen atoms
12substituted by singly or doubly bound nitrogen atoms
125with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
13to an acyclic saturated chain
C07D 295/24 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
22with hetero atoms directly attached to ring nitrogen atoms
24Oxygen atoms
CPC
A61P 13/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07D 209/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
08with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
C07D 213/81
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
81Amides; Imides
C07D 213/82
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78Carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals
81Amides; Imides
82in position 3
Applicants
  • RECORDATI S.A., CHEMICAL AND PHARMACEUTICAL COMPANY [CH]/[CH] (AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CU, CY, CZ, DE, DK, EE, ES, FI, FR, GA, GB, GE, GH, GM, GN, GR, GW, HR, HU, ID, IE, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MC, MD, MG, MK, ML, MN, MR, MW, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZW)
  • RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.P.A. [IT]/[IT] (IT)
Inventors
  • LEONARDI, Amedeo
  • MOTTA, Gianni
  • RIVA, Carlo
  • TESTA, Rodolfo
Agents
  • SERJEANTS
Priority Data
MI97A00186401.08.1997IT
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) 1-(N-PHENYLAMINOALKYL)-PIPERAZINE DERIVATIVES SUBSTITUTED AT POSITION 2 OF THE PHENYL RING
(FR) DERIVES DE 1-(N-PHENYLAMINOALKYL)-PIPERAZINE SUBSTITUES A LA POSITION 2 DU CYCLE PHENYLE
Abstract
(EN) 1-(N-phenylaminoalkyl)-piperazine derivatives of formula (I), (R = H, alkyl-CO, cycloalkyl-CO, substituted cycloalkyl-CO or monocyclic heteroaryl-CO; R1 = H or lower alkyl; R2 = halogen, alkoxy, phenoxy, NO2, CN, acyl, NH2, NH(acyl), alkyl-SO2NH, alkoxycarbonyl, NH2CO, (alkyl)NHCO, (alkyl)2NCO, (acyl)NHCO, CF3 or polyfluoroalkoxy; B = benzyl or mono- or bicyclic aryl or heteroaryl, all optionally substituted) bind to 5HT1A receptors and are useful for the treatment of neuromuscular dysfunctions of the lower urinary tract. The use of these compounds for the preparation of a medicament for this treatment is claimed, and some of the compounds (with restricted B values) are claimed per se.
(FR) L'invention concerne des dérivés de 1-(N-phénylaminoalkyl)-pipérazine qui correspondent à la formule (I) (R=H, alkyl-CO, cycloalkyl-CO, cycloalkyl-CO substitué ou hétéroaryl-CO monocyclique; R1=H ou alkyle inférieur; R2=halogène, alcoxy, phénoxy, NO2, CN, acyle, NH2, NH(acyle), alkyl-SO2NH, alcoxycarbonyle, NH2CO, (alkyl)NHCO, (alkyl)2NCO, (acyl)NHCO, CF3 ou polyfluoroalcoxy; B = benzyle ou hétéroaryle ou aryle mono- ou bicyclique, tous éventuellement substitués). Ces dérivés se lient aux récepteurs 5HT1A, et sont utiles lors du traitement de dysfonctionnements neuro-musculaires des voies urinaires inférieures. Cette invention concerne également l'utilisation de ces composés dans la préparation d'un médicament utilisé pour ce traitement, ainsi que certains de ces composés dont la valeur B est réduite.
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