Lipophilic Benzothiophenes

Abstract: The invention provides novel benzothiophenes of the formula (I): wherein R1 is N-pyrrolidinyl or N-piperidinyl; R2 and R3 are independently hydrogen,-CO-(C10-C22 alkyl), -CO-(C10-C22 branched alkyl), -CO-(C10-C22 alkenyl), -CO-(C10-C22 polyalkenyl), -CO-(C10-C22 alkynyl),or -CO-(CH2)nCOR4; provided R2 and R3 are not both dodecanoyl, and one of R2 or R3 is not hydrogen R4 is -3-cholesteryl or -O(CH2)2(OR5)CH2OR6; R5 and R6 are independently hydrogen, -CO-(C10-C22 alkyl), -CO-(C10-C22 branched alkyl), -CO-(C10-C22 alkenyl), -CO-(C10-C22 polyalkenyl), or -CO-(C10-C22 alkynyl); provided one of R5 or R6 is not hydrogen; n is 0-4; and pharmaceutically acceptable salts and solvates thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, and the use of such compounds.

Patent Information

Application #

Filing Date

07 October 1996

Publication Number

35/2016

Publication Type

INA

Invention Field

PHARMACEUTICALS

Status

Email

Parent Application

Applicants

ELI LILLY AND COMPANY

LILLY CORPORATE CENTER, CITY OF INDIANAPOLIS, STATE OF INDIANA

Inventors

1. RAYMOND FRANCIS KAUFFMAN

11420 SAINT ANDREWS LANE, CARMEL, INDIANA 46032

2. GEORGE JOSEPH CULLINAN

RURAL ROUTE 1, BOX 468, TRAFALGAR, INDIANA 46181

Specification

The invention provides novel benzothiophenes of the
formula (I):

wherein R1 is N-pyrrolidinyl or N-piperidinyl;
R2 and R3 are independently hydrogen,-CO-(C10-C22
alkyl), -CO-(C10-C22 branched alkyl), -CO-(C10-C22
alkenyl), -CO-(C10-C22 polyalkenyl), -CO-(C10-C22
alkynyl),or -CO-(CH2)nCOR4; provided R2 and R3 are not both
dodecanoyl, and one of R2 or R3 is not hydrogen
R4 is -3-cholesteryl or -O(CH2)2(OR5)CH2OR6;
R5 and R6 are independently hydrogen, -CO-(C10-C22
alkyl), -CO-(C10-C22 branched alkyl), -CO-(C10-C22
alkenyl), -CO-(C10-C22 polyalkenyl), or -CO-(C10-C22
alkynyl); provided one of R5 or R6 is not hydrogen;
n is 0-4; and pharmaceutically acceptable salts and
solvates thereof.
The present invention further provides pharmaceutical
compositions containing compounds of formula I, and the use
of such compounds.

Documents

Application Documents

#	Name	Date
1	1765-CAL-1996-22-05-2024-Others-Offline.pdf	2024-05-22
1	1765-cal-1996-translated copy of priority document.pdf	2011-10-07
2	1765-cal-1996-specification.pdf	2011-10-07
2	1765-CAL-1996-22-05-2024-RELEVANT DOCUMENTS-OFFLINE.pdf	2024-05-22
3	1765-cal-1996-gpa.pdf	2011-10-07
3	1765-cal-1996-abstract.pdf	2011-10-07
4	1765-cal-1996-claims.pdf	2011-10-07
4	1765-cal-1996-form 5.pdf	2011-10-07
5	1765-cal-1996-form 3.pdf	2011-10-07
5	1765-cal-1996-correspondence.pdf	2011-10-07
6	1765-cal-1996-form 2.pdf	2011-10-07
6	1765-cal-1996-description (complete).pdf	2011-10-07
7	1765-cal-1996-form 1.pdf	2011-10-07
8	1765-cal-1996-form 2.pdf	2011-10-07
8	1765-cal-1996-description (complete).pdf	2011-10-07
9	1765-cal-1996-form 3.pdf	2011-10-07
9	1765-cal-1996-correspondence.pdf	2011-10-07
10	1765-cal-1996-claims.pdf	2011-10-07
10	1765-cal-1996-form 5.pdf	2011-10-07
11	1765-cal-1996-abstract.pdf	2011-10-07
11	1765-cal-1996-gpa.pdf	2011-10-07
12	1765-cal-1996-specification.pdf	2011-10-07
12	1765-CAL-1996-22-05-2024-RELEVANT DOCUMENTS-OFFLINE.pdf	2024-05-22
13	1765-cal-1996-translated copy of priority document.pdf	2011-10-07
13	1765-CAL-1996-22-05-2024-Others-Offline.pdf	2024-05-22