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1. (WO1991005791) GEM-DIPHOSPHONIC ACIDS, A PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/005791 International Application No.: PCT/EP1990/001710
Publication Date: 02.05.1991 International Filing Date: 11.10.1990
Chapter 2 Demand Filed: 18.04.1991
IPC:
C07F 9/38 (2006.01) ,C07F 9/40 (2006.01) ,C07F 9/564 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
28
with one or more P-C bonds
38
Phosphonic acids (R-P(:O)(OH)2); Thiophosphonic acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
28
with one or more P-C bonds
38
Phosphonic acids (R-P(:O)(OH)2); Thiophosphonic acids
40
Esters thereof
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
547
Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
553
having one nitrogen atom as the only ring hetero atom
564
Three-membered rings
Applicants:
BOEHRINGER MANNHEIM ITALIA S.P.A. [IT/IT]; Via S. Uguzzone, 5 I-20126 Milano, IT (AllExceptUS)
TOGNELLA, Sergio [IT/IT]; IT (UsOnly)
LIVI, Valeria [IT/IT]; IT (UsOnly)
MENTA, Ernesto [IT/IT]; IT (UsOnly)
SPINELLI, Silvano [IT/IT]; IT (UsOnly)
Inventors:
TOGNELLA, Sergio; IT
LIVI, Valeria; IT
MENTA, Ernesto; IT
SPINELLI, Silvano; IT
Agent:
MINOJA, Fabrizio; Studio Consulenza Brevettuale Via Rossini, 8 I-20122 Milano, IT
Priority Data:
22004 A/8912.10.1989IT
Title (EN) GEM-DIPHOSPHONIC ACIDS, A PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
(FR) ACIDES GEMINES-DIPHOSPHONIQUES, LEUR PROCEDE DE PREPARATION ET COMPOSITION PHARMACEUTIQUES LES CONTENANT
Abstract:
(EN) Diphosphonic acids of formula (I), wherein R1 and R2 are hydrogen or C1-C4 alkyl; (A) is hydrogen, halogen, hydroxy or C1-C12 alkyl; (B) is a bond, a C1-C8 alkylene chain, a cycloalkylalkylene chain, an alkylene chain substituted by cyclohexyl or cyclopentyl groups, or an aralkyl chain, an alkyl chain containing an heteroatom (O, S or N-CH3) or an ureido residue -(CH2)n1-NHCONH -(CH2)n- with n ranging from 1 to 5, R3 is hydrogen, C1-C9 alkyl, C3-C6 cycloalkyl, benzyl, phenyl or p-methoxybenzyl; (C) is C1-C5 alkyl, phenyl or an aralkyl chain; R4 is hydrogen, C1-C4 alkyl or an amino group optionally substituted by alkyl, phenyl, benzyl, p-methoxybenzyl, acyl, amminoacidic or peptide groups; R5 and R6 are 2-haloethyl or together form a 1-aziridinyl residue, are useful as antitumor agent.
(FR) Acides diphosphoniques de la formule (I), dans laquelle R1 et R2 représentent hydrogène ou alkyle contenant 1 à 4 atomes de carbone; (A) représente hydrogène, halogène, hydroxy ou alkyle contenant 1 à 12 atomes de carbone; (B) représente une liaison, une chaîne alkylène contenant 1 à 8 atomes de carbone, une chaîne cycloalkylalkylène, une chaîne alkylène remplacée par des groupes cyclohexyle ou cyclopentyle, ou une chaîne aralkyle, une chaîne alkyle contenant un hétéroatome (O, S ou N-CH3) ou un reste uréido -(CH2)n1-NHCONH -(CH2n)n-, n étant compris entre 1 et 5, R3 représente hydrogène, alkyle contenant 1 à 9 atomes de carbone, cycloalkyle contenant 3 à 6 atomes de carbone, benzyle, phényle ou p-méthoxybenzyle; (C) représente alkyle contenant 1 à 5 atomes de carbone, phényle ou une chaîne aralkyle; R4 représente hydrogène, alkyle contenant 1 à 4 atomes de carbone ou un groupe amino facultativement remplacé par alkyle, phényle, benzyle, p-méthoxybenzyle, acyle, des groupes amino-acidiques ou peptidiques; R5 et R6 représentent 2- haloéthyle ou forment ensemble un reste 1-aziridinyle, lesdits acides étant utiles en tant qu'agent antitumoral.
Designated States: AU, BB, BG, BR, CA, FI, HU, JP, KP, KR, LK, MC, MG, MW, NO, RO, SD, SU, US
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CM, GA, ML, MR, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
FI921562NO19921406EP0593437ES2090143US5300671JPH05500949
CA2067191DE000069026964KR1019927003610AU1990065108