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EP0055991A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Lysosomotropic detergent therapeutic agents, compositions containing them and their uses

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

Abstract Compositions useful in the control of fertility, the inhibition of malignant cell growth, and the control of other diseases which accumulate macrophages at the disease site, comprising a pharmaceutical carrier and lysosomotropic substance comprising certain heterocyclic amines having at least one hydrophilic substituent and a pK in the range 4.9 to 9. The compositions of the present invention are used to inhibit or alter the functions of lysosome-bearing cells.

Inventors

  • 👤 Raymond A. Firestone

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-29 21:51
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: 4
Claim 1
Independent Claim 95 words
A pharmaceutical composition comprising a pharmaceutical carrier and a lysosomotropic amine compound having a pK of from 4.9 to 9 and that is an alkyl-substituted heterocyclic amine of the formula : wherein z is either 0 or 1; R is alkyl or unsaturated alkyl, each of which contains from 8-30 carbons, substituted alkyl of from 4-30 carbons, or a steroidal radical comprising 3-cholesteryl; R4 is acyl including -COOR 1 m -COR 1 in which R 1 is alkyl or aryl, arylsulfonyl including or phosphoryl (-PO 3 ); and R 5 is H or lower alkyl.
Claim 2
Dependent Claim 95 words
A pharmaceutical composition comprising a pharmaceutical carrier and a lysosomotropic amine compound having a pK of from 4.9 to 9 and that is an alkyl-substituted heterocyclic amine of the formula : wherein z is either 0 or 1; R is alkyl or unsaturated alkyl, each of which contains from 8-30 carbons, substituted alkyl of from 4-30 carbons, or a steroidal radical comprising 3-cholesteryl; R4 is acyl including -COOR 1 m -COR 1 in which R 1 is alkyl or aryl, arylsulfonyl including or phosphoryl (-PO 3 ); and R 5 is H or lower alkyl.
Claim 3
Dependent Claim 32 words
A composition according to Claim 1, in which the lysomo- tropic amine compound has the formula : in which R is alkyl, alkenyl, or substituted alkyl of from 8 to 18 carbons.
Claim 4
Dependent Claim 22 words
A composition as claimed in Claim 1 or 2 for use in the inhibition or alteration of the function of lysosome-bearing cells.

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