US5883294A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Selective thyroid hormone analogs
Assignee: University of California
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Filing: 1997-06-18
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Granted: 1999-03-16
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Expires: 2017-06-18
Abstract
Abstract Selective thyroid hormone agonists are disclosed that are highly selective for the TR beta subtype with high binding affinity. Methods of using such agonists and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.
Inventors
- 👤 Thomas S. Scanlan
- 👤 Grazia Chiellini
- 👤 Hikari Yoshihara
- 👤 James Apriletti
- 👤 John D. Baxter
- 👤 Ralff C. J. Ribeiro
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 09:28
CPC Classifications
C; C07; C07C; C07C69/00; C07C69/76; C07C59/00; C07C59/40; C07C59/76; C07C59/84; A; A61; A61P; A61P19/00; A61P19/08; A61P19/10; A61P25/00; A61P25/24; A61P3/00; A61P3/04; A61P3/06; A61P5/00; A61P5/14; A61P9/00; A61P9/10; C07C59/58; C07C59/64; C07C59/66; C07C59/68; C07C59/70
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
126 words
A compound of the formula: ##STR8## wherein: n is 1, 2 or 3; R 1 and R 2 are independently hydrogen or lower alkyl; or R 1 and R 2 when taken together with the carbon to which they are attached represent --CHOH, --C═O or --C═S; R 3 and R 5 are methyl; R 4 is hydrogen, lower alkyl, or cycloalkyl; R 6 and R 9 are hydrogen or lower alkyl; R 7 and R 8 are independently hydrogen, lower alkyl, optionally substituted phenyl, optionally substituted benzyl, or heteroaryl; with the proviso that R 7 and R 8 cannot both be hydrogen; R 10 is hydrogen, lower alkyl, cycloalkyl, or acyl; and R 11 is hydrogen, lower alkyl, or cycloalkyl; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
126 words
A compound of the formula: ##STR8## wherein: n is 1, 2 or 3; R 1 and R 2 are independently hydrogen or lower alkyl; or R 1 and R 2 when taken together with the carbon to which they are attached represent --CHOH, --C═O or --C═S; R 3 and R 5 are methyl; R 4 is hydrogen, lower alkyl, or cycloalkyl; R 6 and R 9 are hydrogen or lower alkyl; R 7 and R 8 are independently hydrogen, lower alkyl, optionally substituted phenyl, optionally substituted benzyl, or heteroaryl; with the proviso that R 7 and R 8 cannot both be hydrogen; R 10 is hydrogen, lower alkyl, cycloalkyl, or acyl; and R 11 is hydrogen, lower alkyl, or cycloalkyl; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
20 words
The compound of claim 1, wherein R 4 , R 6 , R 7 and R 9 are all hydrogen.
Claim 4
Dependent Claim
17 words
The compound of claim 2, wherein R 10 and R 11 are hydrogen and n is 1.
Claim 5
Dependent Claim
11 words
The compound of claim 3, wherein R 8 is lower alkyl.
Claim 6
Dependent Claim
10 words
The compound of claim 4, wherein R 8 is isopropyl.
Claim 7
Dependent Claim
18 words
The compound of claim 5, wherein R 1 and R 2 are both hydrogen, namely 3,5-dimethyl-4-(4'-hydroxy-3'-isopropylbenzyl)-phenoxy! acetic acid.
Claim 8
Dependent Claim
18 words
The compound of claim 5, wherein R.sup. is hydrogen and R 2 is methyl, namely {3,5-dimethyl-4- (4'-hydroxy-3'-isopropylphenyl)ethane!phenoxy}acetic acid.
Claim 9
Dependent Claim
25 words
The compound of claim 5, wherein R 1 and R 2 taken together with the carbon to which they are attached represent --C═O, namely GC3!.
Claim 10
Dependent Claim
43 words
A pharmaceutical composition for administration to a mammal having a disease state which is alleviated by treatment with a thyroid hormone agonist, which comprises a therapeutically effective amount of a compound of claim 1 in admixture with one or more pharmaceutically acceptable excipients.
Claim 11
Dependent Claim
40 words
A method of treating a mammal having a disease state which is alleviated by treatment with a thyroid hormone agonist, which method comprises administering a therapeutically effective amount of a compound of claim 1 to a mammal in need thereof.
Claim 12
Dependent Claim
11 words
The method of claim 10, wherein the disease state is hypercholesterolemia.
Claim 13
Dependent Claim
11 words
The method of claim 10, wherein the disease state is atherosclerosis.
Claim 14
Dependent Claim
11 words
The method of claim 10, wherein the disease state is obesity.
Claim 15
Dependent Claim
12 words
The method of claim 10, wherein the disease state is cardiac arrhythmia.
Claim 16
Dependent Claim
11 words
The method of claim 10, wherein the disease state is hypothyroidism.
Claim 17
Dependent Claim
11 words
The method of claim 10, wherein the disease state is osteoporosis.
Claim 18
Dependent Claim
11 words
The method of claim 10, wherein the disease state is depression.
References Cited (Backward Citations)
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