US2004266830A1PendingUtilityA1
Pharmaceutical composition
Est. expiryJun 20, 2015(expired)· nominal 20-yr term from priority
A61P 5/00A61P 31/10A61P 43/00A61P 5/48A61P 3/08A61P 5/50A61K 9/2018A61K 31/70A61K 31/4439A61K 31/135A61K 31/44A61K 31/52A61K 31/50A61K 31/42A61K 31/445A61K 31/19A61P 3/10A61K 9/4858A61P 3/00A61K 9/2054A61K 45/06A61K 31/64A61K 31/4245A61K 31/415A61K 31/535A61K 31/425A61K 31/4427
65
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.
Claims
exact text as granted — not AI-modified1 - 51 . (Canceled)
52 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, and (b) a therapeutically effective amount an antidiabetic, wherein the antidiabetic differs from the insulin sensitivity enhancer in the mechanism of action.
53 . The composition of claim 52 , wherein the antidiabetic is selected from the group consisting of an insulin preparation, a sulfonylurea, a biguanide, and an α-glucosidase inhibitor.
54 . The composition of claim 53 , wherein the antidiabetic is an insulin preparation and wherein the insulin sensitivity enhancer is a compound represented by the formula:
wherein R′ represents an optionally substituted hydrocarbon or heterocycle group;
Y represents a group represented by —CO—, —CH(OH)— or —NR 3 — wherein R 3 represents an optionally substituted alkyl group;
m is 0 or 1;
n is 0, 1 or 2;
X represents CH or N;
A represents a bond or a C 1-7 divalent aliphatic hydrocarbon group;
Q represents oxygen atom or sulfur atom;
R 1 represents hydrogen atom or an alkyl group;
ring E may optionally have further 1 to 4 substituents, and the substituents may optionally be combined with R 1 to form a ring;
L and M respectively represent hydrogen atom, or L and M may optionally be combined with each other to form a bond;
wherein R′ does not represent benzopyranyl group when m and n are O, X represents CH, A represents a bond, Q represents sulfur atom, R 1 , L and M represent hydrogen atom, and ring E does not have further substituents
or a pharmacologically acceptable salt thereof.
55 . A composition for the treatment of diabetes in a mammal comprising:
(a) a therapeutically effective amount of an insulin preparation; and, (b) a therapeutically effective amount of one or more of an orally administrable insulin sensitivity enhancer, wherein the insulin sensitivity enhancer enhances insulin sensitivity and reduces the therapeutically effective amount of insulin preparation per dose of insulin preparation.
56 . The composition of claim 55 , wherein the insulin sensitivity enhancer is a compound represented by the formula:
wherein R′ represents an optionally substituted hydrocarbon or heterocycle group;
Y represents a group represented by —CO—, —CH(OH)— or —NR 3 — wherein R 3 represents an optionally substituted alkyl group;
m is 0 or 1;
n is 0, 1 or 2;
X represents CH or N;
A represents a bond or a C 1-7 divalent aliphatic hydrocarbon group;
Q represents oxygen atom or sulfur atom;
R 1 represents hydrogen atom or an alkyl group;
ring E may optionally have further 1 to 4 substituents, and the substituents may optionally be combined with R 1 to form a ring;
L and M respectively represent hydrogen atom, or L and M may optionally be combined with each other to form a bond;
wherein R′ does not represent benzopyranyl group when m and n are O, X represents CH, A represents a bond, Q represents sulfur atom, R 1 , L and M represent hydrogen atom, and ring E does not have further substituents
or a pharmacologically acceptable salt thereof.
57 . The composition of claim 55 , further comprising a physiologically acceptable carrier.
58 . The composition of claim 55 , wherein the insulin sensitivity enhancer is present in the composition in the range of about 0.01 to 10 mg/kg of subject body weight.
59 . The composition of claim 52 , wherein the insulin sensitivity enhancer is selected from the group consisting of BRL-49653, pioglitazone hydrochloride, and troglitazone.
60 . A method for the treatment of diabetes comprising administering to a mammal in need thereof a therapeutically effective amount of an insulin sensitivity enhancer with a therapeutically effective amount of an antidiabetic.
61 . The method of claim 60 , wherein the antidiabetic is an insulin preparation.
62 . The composition of claim 61 , wherein the insulin sensitivity enhancer is a compound represented by the formula:
wherein R′ represents an optionally substituted hydrocarbon or heterocycle group;
Y represents a group represented by —CO—, —CH(OH)— or —NR 3 — wherein R 3 represents an optionally substituted alkyl group;
m is 0 or 1;
n is 0, 1 or 2;
X represents CH or N;
A represents a bond or a C 1-7 divalent aliphatic hydrocarbon group;
Q represents oxygen atom or sulfur atom;
R 1 represents hydrogen atom or an alkyl group;
ring E may optionally have further 1 to 4 substituents, and the substituents may optionally be combined with R 1 to form a ring;
L and M respectively represent hydrogen atom, or L and M may optionally be combined with each other to form a bond;
wherein R′ does not represent benzopyranyl group when m and n are O, X represents CH, A represents a bond, Q represents sulfur atom, R 1 , L and M represent hydrogen atom, and ring E does not have further substituents;
or a pharmacologically acceptable salt thereof.
63 . The method of claim 60 , wherein a physiologically acceptable carrier is administered with the antidiabetic.
64 . A method as claimed in claim 60 , wherein the antidiabetic is selected from the group consisting of:
(a) an insulin preparation; (b) a sulfonylurea; (c) a biguanide; and (d) an α-glucosidase inhibitor.
65 . A method for the treatment of diabetes comprising administering to a mammal in need thereof a therapeutically effective amount of an insulin sensitivity enhancer with a therapeutically effective amount of an orally administrable antidiabetic, wherein
(1) the insulin sensitivity enhancer is selected from the group consisting of BRL-49653, pioglitazone hydrochloride, and troglitazone, and wherein (2) the antidiabetic is selected from the group consisting of an insulin preparation, a sulfonylurea, a biguanide, and an α-glucosidase inhibitor.
66 . The method of claim 65 , wherein the antidiabetic is an orally administrable antidiabetic.
67 . The method of claim 66 , wherein the antidiabetic is an insulin preparation.
68 . The method of claim 67 , wherein the insulin sensitivity enhancer is a compound represented by the formula:
wherein R′ represents an optionally substituted hydrocarbon or heterocycle group;
Y represents a group represented by —CO—, —CH(OH)— or —NR 3 — wherein R 3 represents an optionally substituted alkyl group;
m is 0 or 1;
n is 0, 1 or 2;
X represents CH or N;
A represents a bond or a C 1-7 divalent aliphatic hydrocarbon group;
Q represents oxygen atom or sulfur atom;
R 1 represents hydrogen atom or an alkyl group;
ring E may optionally have further 1 to 4 substituents, and the substituents may optionally be combined with R 1 to form a ring;
L and M respectively represent hydrogen atom, or L and M may optionally be combined with each other to form a bond;
wherein R′ does not represent benzopyranyl group when m and n are O, X represents CH, A represents a bond, Q represents sulfur atom, R 1 , L and M represent hydrogen atom, and ring E does not have further substituents
or a pharmacologically acceptable salt thereof.
69 . The method of claim 65 , wherein the composition is formulated for injection. PAGE 23.
70 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is an insulin preparation.
71 . The composition of claim 70 , wherein the insulin sensitivity enhancer is a compound represented by the formula:
wherein R′ represents an optionally substituted hydrocarbon or heterocycle group;
Y represents a group represented by —CO—, —CH(OH)— or —NR 3 — wherein R 3 represents an optionally substituted alkyl group;
m is 0 or 1;
n is 0, 1 or 2;
X represents CH or N;
A represents a bond or a C 1-7 divalent aliphatic hydrocarbon group;
Q represents oxygen atom or sulfur atom;
R 1 represents hydrogen atom or an alkyl group;
ring E may optionally have further 1 to 4 substituents, and the substituents may optionally be combined with R 1 to form a ring;
L and M respectively represent hydrogen atom, or L and M may optionally be combined with each other to form a bond;
wherein R′ does not represent benzopyranyl group when m and n are O, X represents CH, A represents a bond, Q represents sulfur atom, R 1 , L and M represent hydrogen atom, and ring E does not have further substituents
or a pharmacologically acceptable salt thereof.
72 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is a sulfonylurea.
73 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is a biguanide.
74 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, wherein the insulin sensitivity enhancer is BRL-49653, and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is an insulin preparation.
75 . The composition of claim 74 , wherein the insulin sensitivity enhancer is a compound represented by the formula:
wherein R′ represents an optionally substituted hydrocarbon or heterocycle group;
Y represents a group represented by —CO—, —CH(OH)— or —NR 3 — wherein R 3 represents an optionally substituted alkyl group;
m is 0 or 1;
n is 0, 1 or 2;
X represents CH or N;
A represents a bond or a C 1-7 divalent aliphatic hydrocarbon group;
Q represents oxygen atom or sulfur atom;
R 1 represents hydrogen atom or an alkyl group;
ring E may optionally have further 1 to 4 substituents, and the substituents may optionally be combined with R 1 to form a ring;
L and M respectively represent hydrogen atom, or L and M may optionally be combined with each other to form a bond;
wherein R′ does not represent benzopyranyl group when m and n are O, X represents CH, A represents a bond, Q represents sulfur atom, R 1 , L and M represent hydrogen atom, and ring E does not have further substituents
or a pharmacologically acceptable salt thereof.
76 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, wherein the insulin sensitivity enhancer is BRL-49653; and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is a sulfonylurea.
77 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, wherein the insulin sensitivity enhancer is BRL-49653, and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is a biguanide.
78 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, wherein the insulin sensitivity enhancer is pioglitazone hydrochloride, and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is an insulin preparation.
79 . The composition of claim 78 , wherein the insulin sensitivity enhancer is a compound represented by the formula:
wherein R′ represents an optionally substituted hydrocarbon or heterocycle group;
Y represents a group represented by —CO—, —CH(OH)— or —NR 3 — wherein R 3 represents an optionally substituted alkyl group;
m is 0 or 1;
n is 0, 1 or 2;
X represents CH or N;
A represents a bond or a C 1-7 divalent aliphatic hydrocarbon group;
Q represents oxygen atom or sulfur atom;
R 1 represents hydrogen atom or an alkyl group;
ring E may optionally have further 1 to 4 substituents, and the substituents may optionally be combined with R 1 to form a ring;
L and M respectively represent hydrogen atom, or L and M may optionally be combined with each other to form a bond;
wherein R′ does not represent benzopyranyl group when m and n are O, X represents CH, A represents a bond, Q represents sulfur atom, R 1 , L and M represent hydrogen atom, and ring E does not have further substituents
or a pharmacologically acceptable salt thereof.
80 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, wherein the insulin sensitivity enhancer is pioglitazone hydrochloride, and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is an insulin preparation, and wherein the composition is formulated for injection.
81 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, wherein the insulin sensitivity enhancer is pioglitazone hydrochloride, and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is a sulfonylurea.
82 . A composition for the treatment of diabetes comprising:
(a) a therapeutically effective amount of an insulin sensitivity enhancer, wherein the insulin sensitivity enhancer is pioglitazone hydrochloride, and (b) a therapeutically effective amount of an antidiabetic, wherein the antidiabetic is a biguanide.
83 . A method for the treatment of diabetes comprising administering to a mammal in need thereof a therapeutically effective amount of an insulin sensitivity enhancer with a therapeutically effective amount of an orally administrable antidiabetic, wherein
(1) the insulin sensitivity enhancer is BRL-49653, and wherein (2) the antidiabetic is a sulfonylurea.
84 . A method for the treatment of diabetes comprising administering to a mammal in need thereof a therapeutically effective amount of an insulin sensitivity enhancer with a therapeutically effective amount of an orally administrable antidiabetic, wherein
(1) the insulin sensitivity enhancer is BRL-49653, and wherein (2) the antidiabetic is a biguanide.
85 . A method for the treatment of diabetes comprising administering to a mammal in need thereof a therapeutically effective amount of an insulin sensitivity enhancer with a therapeutically effective amount of an orally administrable antidiabetic, wherein
(1) the insulin sensitivity enhancer is pioglitazone hydrochloride, and wherein (2) the antidiabetic is a sulfonylurea.
86 . A method for the treatment of diabetes comprising administering to a mammal in need thereof a therapeutically effective amount of an insulin sensitivity enhancer with a therapeutically effective amount of an orally administrable antidiabetic, wherein
(1) the insulin sensitivity enhancer is pioglitazone hydrochloride, and wherein (2) the antidiabetic is a biguanide.Cited by (0)
No later patents cite this yet.
References (0)
No backward citations on record.