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EP0428169A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Aqueous liquid formulations

Assignee: Astellas Pharma Inc
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Filing: 1990-11-15
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Granted: —
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Expires: 2010-11-15
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Abstract

Abstract An aqueous liquid formulation which comprises a compound of the formula : wherein the symbols define certain groups, particularly the compound 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyc!ohexyl)-1-methyivlnyl]-23,25-d!methoxy-13,19,21,27-tetramethyl-11-28-dioxa-4-azatrlcyclo-[22.3.2.0 4,9 ]octacos-18-ene-2,3,10,16-tetraone, and process for its preparation.

Inventors

  • 👤 Toshiyasu Honbo

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-28 16:51
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K31/33; A61K31/395; A61K31/40; A61K31/435; A61K31/44; A61K31/445; A61K31/55; A61K47/00; A61K47/06; A61K47/28; A61K47/44; A61K9/00; A61K9/0012; A61K9/0019

Claims Analysis

Total Claims: 4
Claim 1
Independent Claim 345 words
An aqueous liquid formulation which comprises a compound of the formula : wherein each vicinal pair of substituents [R 1 and R 2 ], [R 3 and R 4 ], [R 5 and R 6 ] independently a) represent two vicinal hydrogen atoms, or b) form a second bond between the vicinal carbon atoms to which they are attached; in addition to its significance above, R 2 may represent an alkyl group; R 7 represents H, OH, protected hydroxy or O-alkyl, or in conjunction with R 1 it may represent =O; R 8 and R 9 independently represent H or OH; R 10 represents H, alkyl, alkyl substituted by one or more hydroxyl groups, alkenyl, alkenyl substituted by one or more hydroxyl groups, or alkyl substituted by = O; X represents 0, (H,OH), (H,H) or -CH 2 0-; Y represents O, (H,OH), (H,H), N-NR 11 R 12 or N-OR 13 ; R" and R 12 independently represent H, alkyl, aryl or tosyl; R1 3, R 14, R1 5, R 16, R 1 7, R 18 , R 19 , R 22 and R 23 independently represent H or alkyl; R 20 and R 21 independently represent O, or they may independently represent (R 20 a,H) and (R 21 a,H) respectively; R 20 a and R 21 a independently represent OH, O-alkyl or OCH 2 0CH 2 CH 2 0CH 3 or R 21 a is protected hydroxy; in addition, R 20 a and R 21 a may together represent an oxygen atom in an epoxide ring; n is 1, 2 or 3; in addition to their significances above, Y, R 10 and R 23 , together with the carbon atoms to which they are attached, may represent a 5- or 6-membered N-, S- or 0- containing heterocyclic ring, which may be saturated or unsaturated, and which may be substituted by one or more groups selected from alkyl, hydroxy, alkyl substituted by one or more hydroxyl groups, O-alkyl, benzyl and -CH 2 Se(C 6 H 5 ), or a pharmaceutically acceptable salt thereof and a surfactant.
Claim 2
Dependent Claim 345 words
An aqueous liquid formulation which comprises a compound of the formula : wherein each vicinal pair of substituents [R 1 and R 2 ], [R 3 and R 4 ], [R 5 and R 6 ] independently a) represent two vicinal hydrogen atoms, or b) form a second bond between the vicinal carbon atoms to which they are attached; in addition to its significance above, R 2 may represent an alkyl group; R 7 represents H, OH, protected hydroxy or O-alkyl, or in conjunction with R 1 it may represent =O; R 8 and R 9 independently represent H or OH; R 10 represents H, alkyl, alkyl substituted by one or more hydroxyl groups, alkenyl, alkenyl substituted by one or more hydroxyl groups, or alkyl substituted by = O; X represents 0, (H,OH), (H,H) or -CH 2 0-; Y represents O, (H,OH), (H,H), N-NR 11 R 12 or N-OR 13 ; R" and R 12 independently represent H, alkyl, aryl or tosyl; R1 3, R 14, R1 5, R 16, R 1 7, R 18 , R 19 , R 22 and R 23 independently represent H or alkyl; R 20 and R 21 independently represent O, or they may independently represent (R 20 a,H) and (R 21 a,H) respectively; R 20 a and R 21 a independently represent OH, O-alkyl or OCH 2 0CH 2 CH 2 0CH 3 or R 21 a is protected hydroxy; in addition, R 20 a and R 21 a may together represent an oxygen atom in an epoxide ring; n is 1, 2 or 3; in addition to their significances above, Y, R 10 and R 23 , together with the carbon atoms to which they are attached, may represent a 5- or 6-membered N-, S- or 0- containing heterocyclic ring, which may be saturated or unsaturated, and which may be substituted by one or more groups selected from alkyl, hydroxy, alkyl substituted by one or more hydroxyl groups, O-alkyl, benzyl and -CH 2 Se(C 6 H 5 ), or a pharmaceutically acceptable salt thereof and a surfactant.
Claim 3
Dependent Claim 17 words
The aqueous liquid formulation of claim 1, in which the compound (I) is 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4- azatricyclo[22.3.1.0 4,9 )octacos-18-ene-2,3,10,16-tetraone.
Claim 4
Dependent Claim 22 words
A process for preparing an aqueous liquid formulation, which comprises admixing the compound (I) as defined in claim 1 with a surfactant.

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