Processing

Please wait...

PATENTSCOPE will be unavailable a few hours for maintenance reason on Sunday 05.04.2020 at 10:00 AM CEST
Settings

Settings

1. WO2000042849 - COMPLEX OF RAS-FARNESYLTRANSFERASE INHIBITOR AND SULFOBUTYLETHER-7-$g(b)-CYCLODEXTRIN OR 2-HYDROXYPROPYL-$g(b)-CYCLODEXTRIN AND METHOD

Publication Number WO/2000/042849
Publication Date 27.07.2000
International Application No. PCT/US1999/030424
International Filing Date 21.12.1999
Chapter 2 Demand Filed 21.07.2000
IPC
A61K 47/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
CPC
A61K 47/6951
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
6949inclusion complexes, e.g. clathrates, cavitates or fullerenes
6951using cyclodextrin
B82Y 5/00
BPERFORMING OPERATIONS; TRANSPORTING
82NANOTECHNOLOGY
YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
5Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
Y10S 514/97
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
10TECHNICAL SUBJECTS COVERED BY FORMER USPC
STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
514Drug, bio-affecting and body treating compositions
97Containing designated ingredient to stabilize an active ingredient
Y10S 514/973
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
10TECHNICAL SUBJECTS COVERED BY FORMER USPC
STECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
514Drug, bio-affecting and body treating compositions
97Containing designated ingredient to stabilize an active ingredient
973Sulfur compound additive as stabilizer, e.g. sulfites
Applicants
  • BRISTOL-MYERS SQUIBB CO. [US/US]; P.O. Box 4000 Princeton, NJ 08543-4000, US
Inventors
  • RAGHAVAN, Krishnaswamy, S.; US
  • MALLOY, Timothy, M.; US
  • VARIA, Sailesh, A.; US
Agents
  • BABCOCK, Timothy, J. ; Bristol-Myers Squibb Co. P.O. Box 4000 Princeton, NJ 08543, US
Priority Data
60/116,64721.01.1999US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMPLEX OF RAS-FARNESYLTRANSFERASE INHIBITOR AND SULFOBUTYLETHER-7-$g(b)-CYCLODEXTRIN OR 2-HYDROXYPROPYL-$g(b)-CYCLODEXTRIN AND METHOD
(FR) COMPLEXE D'INHIBITEUR DE LA RAS-FARNESYLTRANSFERASE ET DE SULFOBUTYLETHER-7-$g(b)-CYCLODEXTRINE OU DE 2-HYDROXPROPYL-$g(b)-CYCLODEXTRINE ET PROCEDE
Abstract
(EN)
A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of formula (I), wherein n is 0 or 1; R1 is selected from Cl, Br, phenyl, pyridyl or cyano; R2 is aralkyl; R3 is selected from lower alkyl, aryl or substituted aryl or heterocyclo; Z1 is selected from CO, SO2, CO2 or SO2NR5, R5 is selected from hydrogen, lower alkyl or substituted alkyl; and sulfobutylether-7-$g(b)-cyclodextrin or 2-hydroxypropyl-$g(b)-cyclodextrin is provided. The complex has unexpectedly high aqueous solubility of the ras-farnesyltransferase inhibitor and is useful for its intravenous delivery to humans with cancer. Also provided is a method for forming the complex. The ras-farnesyltransferase inhibitors are useful as anti-tumor agents.
(FR)
L'invention concerne un complexe d'inhibiteur de la ras-farnésyltransférase, constitué d'un inhibiteur de la ras-farnésyltransférase ou d'un sel de celui-ci, acceptable au plan pharmaceutique, de formule (I), dans laquelle n vaut 0 ou 1; R1 est choisi parmi Cl, Br, phényle, pyridyle or cyano; R2 représente aralkyle; R3 est choisi parmi alkyle inférieur, aryle ou hérétocyclo ou aryle substitué; Z1 est choisi parmi CO, SO2, CO2 ou SO2NR5, R5 est choisi parmi hydrogène, alkyle inférieur ou alkyle substitué; et sulfobutyléther-7-$g(b)-cyclodextrine ou 2-hydroxypropyl-$g(b)-cyclodextrine. L'inhibiteur de ras-farnésyltransférase dudit complexe présente une solubilité aqueuse étonnamment élevée et ledit complexe est utile dans l'administration intraveineuse à des humains souffrant de cancer. L'invention porte également sur un procédé de formation du complexe. Les inhibiteurs de ras-farnésyltransférase sont utiles en tant qu'agents antitumoraux.
Also published as
CZPV2001-2601
GE5955/1
ININ/PCT/2001/00695/MUM
ININ/PCT/2001/695/MUM
LT2001064
LV200120010101
NO20013585
NZ511995
ROa 2001 00834
SK200100960
SK9602001
TR2001/02109
ZA200104416
Latest bibliographic data on file with the International Bureau