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EP0044090A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Lysosomotropic detergent therapeutic agents, compositions containing them and their uses

Assignee: Merck and Co Inc
•
Filing: 1979-09-28
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Granted: —
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Expires: 1999-09-28
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Abstract

Abstract Compounds of formula: in which M is a peptide substituent comprising z-gly-phe, gly-phe, z-arg-arg, or benzoyl-arg, and A or N=A is an active lysosome-inhibiting substance comprising a known therapeutic drug residue or an amino radical of the formula: in which R is an alkyl or substituted alkyl substituent of from 8 to 18 carbons and R 2 is fluoroalkyl or hydrogen, are useful in the control of fertility, in the inhibition of malignant cell growth, and in the control of other diseases which accumulate macrophages at the disease site. They can be incorporated in pharmaceutical compositions for this purpose.

Inventors

  • 👤 Raymond A. Firestone

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-30 21:37
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/02; C07D231/10; C07D231/12; A; A61; A61K; A61K31/00; A61K31/13; A61K31/15; A61K31/155; A61K31/21; A61K31/27; A61K31/275; A61K31/33; A61K31/395; A61K31/41; A61K31/415; A61K31/425; A61K31/435; A61K31/44; A61K31/495; A61K31/535; A61K31/56; A61K31/575; A61K31/66; A61K31/675; A61K47/00; A61K47/50; A61K47/51; A61K47/54; A61K47/545; A61K47/62; A61K47/64; A61P; A61P31/00; A61P31/04; A61P35/00; C07D233/00; C07D233/54; C07D233/56; C07D249/00; C07D249/02; C07D249/08; C07J; C07J43/00; C07J43/003; C07J43/006; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026; C07K5/06086; C07K5/06095; A61K38/00

Claims Analysis

Total Claims: 6
Claim 1
Independent Claim 66 words
A compound of formula : in which M is a peptide substituent comprising z-gly-phe, gly - phe, z-arg-arg, or benzoyl-arg, and A or N=A is an active lysosome-inhibiting substance comprising a known therapeutic drug residue or an amino radical of the formula : in which R is an alkyl or substituted alkyl substituent of from 8 to 18 carbons and R 2 is fluoroalkyl or hydrogen.
Claim 2
Dependent Claim 66 words
A compound of formula : in which M is a peptide substituent comprising z-gly-phe, gly - phe, z-arg-arg, or benzoyl-arg, and A or N=A is an active lysosome-inhibiting substance comprising a known therapeutic drug residue or an amino radical of the formula : in which R is an alkyl or substituted alkyl substituent of from 8 to 18 carbons and R 2 is fluoroalkyl or hydrogen.
Claim 3
Dependent Claim 16 words
A pharmaceutical composition comprising a compound as claimed in Claim 1 together with a pharmaceutical carrier.
Claim 4
Independent Claim 42 words
A method for inhibiting or altering the function of lysosome-bearing cells that comprises contacting the said cells with a pharmaceutical composition comprising a pharmaceutical carrier and a lysosomotropic substance comprising a peptide conjugate hydrolysable by lysosomal enzymes to a biologically active substance.
Claim 5
Independent Claim 42 words
A method for inhibiting or altering the function of lysosome-bearing cells that comprises contacting the said cells with a pharmaceutical composition comprising a pharmaceutical carrier and a lysosomotropic substance comprising a peptide conjugate hydrolysable by lysosomal enzymes to a biologically active substance.
Claim 6
Dependent Claim 26 words
For use in inhibiting or altering the function of lysosome-bearing cells, a compound as claimed in Claim 1 or a composition as claimed in Claim 2.

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