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US 2002/0177594 A1Published application
Inhibitors of histone deacetylase
OwnerMichael L. Curtin, Yujia Dai +9inventors
InventorsMichael L. Curtin, Yujia Dai, Steven K Davidsen, Robin R. Frey, Yan Guo, Howard R. Heyman, James H. Holms, Zhiqin Ji, Michael R. Michaelides, Anil Vasudevan, Carol K. Wada
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Abstract
Compounds having the formula 1 or therapeutically acceptable salts thereof, are histone deacetylase (HDAC) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.
Claims31
A compound of formula (I)
- 16
- or a therapeutically acceptable salt thereof, wherein
- n is 1 or 2;
- L1 is selected from the group consisting of alkenylene, alkylene, alkynylene, cycloalkylene, heteroalkylene, —(alkylene)—C(O)N(R5)—(alkylene)—, —(alkylene)—O—(alkylene)—;
- wherein each group is drawn with its left-hand end being the end which attaches to L2, and its right-hand end being the end which attaches to the carbon substituted with R1, R2, and R3;
- L2 is selected from the group consisting of a bond, C2 alkenylene, —O—, —S—, —SO2—, —OC(O)NR5—, —N(R6)C(O)—, —C(O)N(R6)—, —SO2N(R6)—,—N(R6)SO2—, —C═N—O—, —N(R6)C(O)N(R6)—, and —C(O)N(R6)N(R6)C(O)—;
- wherein each group is drawn with its left-hand end being the end which attaches to R4, and its right-hand end being the end which attaches to L1;
- R1 is selected from the group consisting of alkanoyl, alkoxycarbonyl, aminocarbonyl, carboxy, haloalkyl, and heterocycle, wherein the heterocycle is selected from the group consisting of oxazolyl, dihydrooxazolyl, oxadiazolyl, and tetraazolyl;
- R2 and R3 are hydroxy;
- or
- R2 and R3 together are oxo;
- R4 is selected from the group consisting of alkoxyalkyl, alkyl, aryl, arylalkyl, cycloalkyl, (cycloalkyl)alkyl, heterocycle, and (heterocycle)alkyl;
- and
- R5 and R6 are independently selected from the group consisting of hydrogen, alkyl, aryl, and arylalkyl;
- or
- R4 and R6, together with the nitrogen atom to which they are attached, form a heterocycle selected from the group consisting of morpholinyl, piperazinyl, piperidinyl, and thiomorpholinyl;
- wherein the morpholinyl, the piperazinyl, the piperidinyl, and the thiomorpholinyl can be optionally substituted with one, two, or three substituents independently selected from the group consisting of alkyl and spiroheterocycle.
14 more elements
Dependencies are inferred from the claim text.