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US 2003/0144329 A1Published application
N-substituted heterocycles for the treatment of hypercholesteremia, dyslipidemia and other metabolic disorders; cancer, and other diseases
AssigneesIncyte San Diego Inc., Ortho-McNeil Pharmaceutical, Inc.
InventorsMagnus Pfahl, Catherine Tachdjian, Lyle W. Spruce, Hussien A. Al-Shamma, Mohamed Boudjelal, Andrea N. Fanjul, Torsten R. Wiemann, David P.M. Pleynet
Life of this patent
Estimating the term…
Abstract
The present invention relates to certain compounds of Formula (I) which can be useful in the treatment of diseases, such as, cancer, metabolic disorders, Type 2 Diabetes, dyslipidemia and/or hyperchloesterolemia: 1
Claims50
A compound having the formula
- 91
- wherein,
- a) “- - -” is absent or present;
- b) Ar1 has from six to 25 carbon atoms and has the formula
- 92
- wherein R5 and R6 together with the aromatic ring form a five, six, or seven membered non-aromatic ring which can optionally comprise one, or two ring heteroatoms independently selected from O, S, N, and NRN, wherein RN is hydrogen, hydroxyl, halogen, amino, or an organic radical comprising one to twelve carbon atoms;
- and wherein R7 and R8 are independently selected from hydrogen, alkyl, substituted alkyl, amino, mono-substituted amino, or di-substituted amino;
- c) Ar2 comprises from four to twenty carbon atoms and an aryl ring or heteroaryl ring, and
- d) R1 is hydrogen or a substituted or unsubstituted organic radical comprising from one to four carbon atoms;
- e) R2 is a substituted or unsubstituted organic radical comprising one to twelve carbon atoms;
- f) W is —S—, —O— or —N—R3 wherein R3 is hydrogen, or a substituted or unsubstituted radical comprising from one to 12 carbon atoms;
- and
- g) X is O or S;
- or a pharmaceutically acceptable salt thereof.
11 more elements
A compound having the formula
- 101
- wherein,
- a) “- - -” is absent or present;
- b) Ar1 has the formula
- 102
- c) Ar2 has the formula
- 103
- wherein x is one or two, and R15, R16 and R17 are independently selected from hydrogen, halogen, cyano, nitro, hydroxyl, amino, or an organic radicals comprising one to four carbon atoms selected from an alkyl, substituted alkyl, haloalkyl, haloalkoxy, alkoxy, substituted alkoxy, mono-substituted amino, di-substituted amino having from one to four carbon atoms.
- d) R1 is hydrogen, or an alkyl or substituted alkyl group having one to four carbon atoms;
- e) R2 is a an alkyl or substituted alkyl group having one to four carbon atoms,
- f) W is —S—;
- and
- g) X is O or S;
- or a pharmaceutically acceptable salt thereof.
11 more elements
A compound present as:
- {5-[4-Methoxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen -2-yl)-benzylidene]-4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acid;
- {5-[4-Trifluoromethoxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen -2-yl)-benzylidene]-4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acid;
- {5-[6-Methoxy-5-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen -2-yl)-pyridin-3-yl methylene]-4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acid;
- 3-Ethyl-{5-[4-Trifluoromethoxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-benzylidene]-2-thioxo-thiazolidin-4-one;
- 3-Methyl-{5-[4-Trifluoromethoxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-benzylidene]-2-thioxo-thiazolidin-4-one;
- 5-[4-Methoxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen -2-yl)-benzylidene]-3-(2-pyridin-2-yl-ethyl)-thiazolidine-2,4-dione;
- {5-[6-(3-Dimethylamino-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen -2-yl)-naphthalen-2-yl methylene]-4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acid;
- {5-[5-Phenyl-3-methoxy-2-(3-methoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-benzylidene]-4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acid;
- {5-[3-Methoxy-2-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen -2-yl)-benzylidene]-4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acid;
- {5-[4-Dimethylamino-3-(3-dimethylamino-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-benzylidene]4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acid;
- or
- {5-[(3-t-Butyl-4-methoxyphenyl)-6-ethoxy-benzylidene]-4-oxo-2-thioxo-thiazolidin-3-yl}-acetic acid;
- or
- a pharmaceutically acceptable salt thereof.
11 more elements
Dependencies are inferred from the claim text.