US2008075692A1PendingUtilityA1
Methods for treating blood disorders
Est. expiryMay 9, 2026(expired)· nominal 20-yr term from priority
Inventors:Susan P. Perrine
C07D 311/12C07D 285/125A61K 31/517A61K 31/353A61K 31/194A61P 7/06A61P 7/00A61K 31/433A61P 43/00A61K 31/415A61K 31/39A61K 31/36A61K 31/192
59
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
Methods of treating blood disorders are described.
Claims
exact text as granted — not AI-modified1 . A method for treating or preventing a blood disorder in a subject, comprising administering to said subject an effective amount of a compound of formula I:
wherein
R 1 is hydroxy or alkoxy;
X is C(O), C(S), SO, SO 2 or PO 2 ;
R 2 and R 3 are each independently hydrogen, alkyl, halogen, hydroxyl, thiol, alkenyl, alkynyl, aryl, acyl, alkoxy, amino, alkylamino or heterocyclic;
R 4 is alkyl, cycloalkyl, alkenyl, alkynyl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, heteroaryl, halogen or
R 5 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 6 to form a ring;
R 6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 5 or R 7 to form a ring;
R 7 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 6 or R 8 to form a ring;
R 8 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 7 or R 9 to form a ring;
R 9 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 8 to form a ring;
and racemates, isolated enantiomers or diastereomers, and pharmaceutically acceptable salts thereof;
provided that when R 4 is
R 5 , R 6 , R 7 , R 8 , and R 9 are each not hydrogen; and when R 6 , R 7 , R 8 , and R 9 are each hydrogen, R 5 is not methoxy; and when R 5 , R 7 , R 8 , R 9 are hydrogen, R 6 is not methoxy; and when R 5 , R 8 and R 9 are hydrogen, R 6 and R 7 are not methoxy.
2 . The method of claim 1 , wherein R 1 is hydroxy, X is C(O), R 4 is
and R 2 , R 3 and R 5 are each hydrogen.
3 . The method of claim 2 , wherein R 6 , R 8 and R 9 are each hydrogen, and R 7 is alkoxy.
4 . The method of claim 3 , wherein R 7 is methoxy.
5 . The method of claim 2 , wherein R 7 and R 8 are each hydrogen, and R 6 and R 9 are each alkyl.
6 . The method of claim 5 , wherein R 6 and R 9 are methyl.
7 . The method of claim 2 , wherein R 8 are R 9 are each hydrogen and R 6 and R 7 are each hydroxyl.
8 . The method of claim 2 , wherein R 8 are R 9 are each hydrogen and R 6 and R 7 are linked by —O—CH 2 —O— to form a ring.
9 . The method of claim 2 , wherein R 6 and R 9 are each hydrogen, R 7 is alkoxy and R 8 is hydroxyl.
10 . The method of claim 1 , wherein R 4 is heteroaryl.
11 . The method of claim 10 , wherein R 4 is quinoline or substituted or unsubstituted thiophene.
12 . The method of claim 11 , wherein R 4 is chlorothiophene.
13 . The method of claim 1 , wherein said compound is:
14 . A method for treating or preventing a blood disorder in a subject, comprising administering to said subject an effective amount of a compound of formula II:
wherein
R 1′ is hydroxy or alkoxy;
Y is C(O);
n is 0 or an integer from 1 to 5;
R 10 and R 10′ are each independently hydrogen, alkyl, halogen, hydroxyl, thiol, alkenyl, alkynyl, aryl, acyl, alkoxy, amino, alkylamino, heterocyclic or optionally joined to form a ring;
R 11 is CR 11′ R 11″ R 11′″ , alkenyl, cycloalkyl, alkynyl, arylalkyl, amido, alkylamino, amino, arylamino, carbonylalkyl, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, heteroaryl, hydroxy, halogen or
R 11′ and R 11″ are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxyl, halogen or R 11′ and R 11″ are optionally joined to form a ring;
R 11′″ is alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy or halogen;
R 12 is hydrogen, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic or optionally linked to R 13 to form a ring;
R 13 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy or optionally linked to R 12 or R 14 to form a ring;
R 14 is hydrogen, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, halogen or optionally linked to R 13 or R 15 to form a ring;
R 15 is hydrogen, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, halogen or optionally linked to R 14 or R 16 to form a ring;
R 16 is hydrogen, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, halogen or optionally linked to R 15 to form a ring;
and racemates, isolated enantiomers or diastereomers, and pharmaceutically acceptable salts thereof;
provided that when R 11 is
R 12 , R 13 , R 14 , R 15 , and R 16 are each not hydrogen; and provided when n is 2, R 11 is
and R 10 , R 10′ , R 12 , R 15 , and R 16 are hydrogen, then R 14 and R 15 are not methoxy; and provided when n is 1, R 11 is
and R 10 , R 10′ , R 13 , R 14 , and R 16 are hydrogen, then R 12 and R 15 are not methoxy.
15 . The method of claim 14 , wherein R 1′ is hydroxy.
16 . The method of claim 15 , wherein n is 5, R 10 and R 10′ are hydrogen and R 11 is alkylcarbonyl.
17 . The method of claim 15 , wherein n is 2, R 10 and R 10′ are each hydrogen and R 11 is CR 11′ R 11″ R 11′″ .
18 . The method of claim 17 , wherein R 11′ and R 11″ are joined by —(CH 2 ) 5 — to form a cyclohexyl ring and R 11′″ is a substituted or unsubstituted heterocycle.
19 . The method of claim 18 , wherein R 11′″ is chlorothiophene.
20 . The method of claim 15 , wherein n is 0.
21 . The method of claim 20 , wherein R 11 is
22 . The method of claim 21 , wherein R 13 , R 14 , R 15 , and R 16 are hydrogen.
23 . The method of claim 22 , wherein R 12 is arylthioalkyl.
24 . The method of claim 22 , wherein R 12 is alkoxy substituted aryloxy.
25 . The method of claim 21 , wherein R 12 , R 14 , R 15 and R 16 are hydrogen.
26 . The method of claim 25 , wherein R 13 is a substituted or unsubstituted heterocycle.
27 . The method of claim 26 , wherein R 13 is chromen-2-one, nitro-substituted pyrazole, or chloro-substituted pyrazole.
28 . The method of claim 21 , wherein R 12 , R 13 , R 15 and R 16 are hydrogen and R 13 is alkoxy.
29 . The method of claim 28 , wherein R 13 is ethoxy.
30 . The method of claim 21 , wherein R 12 , R 15 and R 16 are hydrogen, and R 13 and R 14 are linked by —N(H)C(O)CH 2 S— to form a ring.
31 . The method of claim 21 , wherein R 14 , R 15 and R 16 are each hydrogen, and R 12 and R 13 are linked by —CH═C(CH 3 )O— to form a ring.
32 . The method of claim 20 , wherein R 11 is a substituted or unsubstituted heterocycle.
33 . The method of claim 32 , wherein R 11 is a substituted aryl-substituted furan.
34 . The method of claim 20 , wherein R 11 is a substituted or unsubstituted cycloalkyl.
35 . The method of claim 34 , wherein R 11 is tetrahydrobenzothiadiazole or dihydrobenzothiophenone.
36 . The method of claim 15 , wherein n is 1.
37 . The method of claim 36 , wherein R 10 and R 10′ are hydrogen.
38 . The method of claim 37 , wherein R 11 is a substituted or unsubstituted cycloalkyl.
39 . The method of claim 38 , wherein R 11 is dimethylcyclobutane carboxylic acid.
40 . The method of claim 37 , wherein R 11 is
41 . The method of claim 40 , wherein R 12 , R 13 and R 16 are hydrogen, and R 14 and R 15 are linked by —O—CH 2 —O— to form a ring.
42 . The method of claim 37 , wherein R 11 is a substituted or unsubstituted heterocycle.
43 . The method of claim 42 , wherein R 11 is substituted thiazolidinedione, substituted pyridinone or substituted pyrazole.
44 . The method of claim 37 , wherein R 11 is substituted or unsubstituted arylamino.
45 . The method of claim 44 , wherein R 11 arylamino is trifluorothio-substituted arylamino.
46 . The method of claim 37 , wherein R 11 is substituted or unsubstituted arylthio or substituted or unsubstituted heterocyclic thio.
47 . The method of claim 46 , wherein R 11 is methoxyphenylthio.
48 . The method of claim 46 , said R 11 is substituted triazolethio, substituted thiadiazolethio or substituted thiophenethio.
49 . The method of claim 37 , wherein R 11 is CR 11′ R 11″ R 11′″ .
50 . The method of claim 49 , wherein R 11′ is hydrogen, R 11″ is amino and R 11′″ is alkoxy-substituted aryl.
51 . The method of claim 36 , wherein R 10 is hydrogen and R 10′ is alkyl.
52 . The method of claim 51 , wherein R 10′ is isopropyl.
53 . The method of claim 52 , wherein R 11 is substituted or unsubstituted arylthio.
54 . The method of claim 53 , wherein R 11 is alkoxy-substituted phenylthio or alkoxy-substituted pyrimadinylthio.
55 . The method of claim 51 , wherein R 10′ is ethyl.
56 . The method of claim 55 , wherein R 11 is heteroarylamino.
57 . The method of claim 56 , wherein R 11 is quinazolinylamino.
58 . The method of claim 36 , wherein R 10 and R 10′ are linked by —(CH 2 ) 5 — to form a cyclohexyl ring.
59 . The method of claim 58 , wherein R 11 is heterocyclic substituted carbonylalkyl.
60 . The method of claim 14 , wherein said compound is
61 . A method for treating or preventing a blood disorder in a subject, comprising administering to said subject an effective amount of a compound of formula III:
wherein
R 1″ is hydroxy or alkoxy;
Z is C(S), SO, SO 2 or PO 2 ;
m is 0 or an integer from 1-5;
R 17 and R 17′ are each independently hydrogen, alkyl, halogen, hydroxyl, thiol, alkenyl, alkynyl, aryl, acyl, alkoxy, amino, alkylamino or heterocyclic;
R 18 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, heteroaryl, hydroxyl or halogen;
and racemates, isolated enantiomers or diastereomers, and pharmaceutically acceptable salts thereof.
62 . The method of claim 61 , wherein R 1″ is hydroxyl, Z is SO 2 , m is 0, and R 18 is disubstituted aryl.
63 . The method of claim 62 , wherein R 18 is substituted by nitro and fluoro.
64 . The method of claim 61 , wherein the compound is of the formula:
65 . A method for treating or preventing a blood disorder in a subject, comprising administering to said subject an effective amount of a compound of formula:
66 . The method of any one of claims 1 , 14 , 61 or 65 , wherein the blood disorder is sickle cell anemia, β-thalassemia, neutropenia or thrombocytopenia.
67 . The method of any one of claims 1 , 14 , 61 or 65 , wherein said compound stimulates fetal hemoglobin production.
68 . The method of any one of claim 1 , 14 , 61 or 65 , wherein said compound stimulates hematopoiesis.
69 . The method of any one of claims 1 , 14 , 61 or 65 , wherein said compound stimulates erythropoiesis.
70 . The method of any one of claims 1 , 14 , 61 or 65 , wherein said compound stimulates myelopoiesis.
71 . The method of any one of claims 1 , 14 , 61 or 65 , wherein said compound stimulates neutrophil production.
72 . The method of any one of claims 1 , 14 , 61 or 65 , wherein said compound is administered in combination with one or more cytokines.
73 . The method of claim 72 , wherein said cytokine is selected from the group consisting of IL-3, GM-CSF, C-CSF, SCF and IL-6.
74 . A pharmaceutical composition comprising an effective amount of a compound of any one of claims 1 , 13 , 14 , 60 , 61 or 65 and racemates, isolated enantiomers or diastereomers thereof, and a pharmaceutically acceptable carrier.
75 . A compound of formula I:
wherein
R 1 is hydroxy or alkoxy;
X is C(O), C(S), SO, SO 2 or PO 2 ;
R 2 and R 3 are each independently hydrogen, alkyl, halogen, hydroxyl, thiol, alkenyl, alkynyl, aryl, acyl, alkoxy, amino, alkylamino or heterocyclic;
R 4 is alkyl, cycloalkyl, alkenyl, alkynyl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, heteroaryl, halogen or
R 5 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 6 to form a ring;
R 6 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 5 or R 7 to form a ring;
R 7 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 6 or R 8 to form a ring;
R 8 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 7 or R 9 to form a ring;
R 9 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy, nitro, halogen or optionally linked to R 8 to form a ring;
and racemates, isolated enantiomers or diastereomers, and pharmaceutically acceptable salts thereof;
provided that when R 4 is
R 5 , R 6 , R 7 , R 8 , and R 9 are each not hydrogen; and when R 6 , R 7 , R 8 , and R 9 are each hydrogen, R 5 is not methoxy; and when R 5 , R 7 , R 8 , R 9 are hydrogen, R 6 is not methoxy; and when R 5 , R 8 and R 9 are hydrogen, R 6 and R 7 are not methoxy;
and provided that the compound is not a compound of claim 13 .
76 . A compound of formula II:
wherein
R 1′ is hydroxy or alkoxy;
Y is C(O);
n is 0 or an integer from 1 to 5;
R 10 and R 10′ are each independently hydrogen, alkyl, halogen, hydroxyl, thiol, alkenyl, alkynyl, aryl, acyl, alkoxy, amino, alkylamino, heterocyclic or optionally joined to form a ring;
R 11 is CR 11′ R 11″ R 11′″ , alkenyl, cycloalkyl, alkynyl, arylalkyl, amido, alkylamino, amino, arylamino, carbonylalkyl, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, heteroaryl, hydroxy, halogen or
R 11′ and R 11″ are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxyl, halogen or R 11′ and R 11″ are optionally joined to form a ring;
R 11′″ is alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy or halogen;
R 12 is hydrogen, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic or optionally linked to R 13 to form a ring;
R 13 is hydrogen, alkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, hydroxy or optionally linked to R 12 or R 14 to form a ring;
R 14 is hydrogen, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, halogen or optionally linked to R 13 or R 15 to form a ring;
R 15 is hydrogen, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, halogen or optionally linked to R 14 or R 16 to form a ring;
R 16 is hydrogen, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, halogen or optionally linked to R 15 to form a ring;
and racemates, isolated enantiomers or diastereomers, and pharmaceutically acceptable salts thereof;
provided that when R 11 is
R 12 , R 13 , R 14 , R 15 , and R 16 are each not hydrogen; and provided when n is 2, R 11 is
and R 10 , R 10′ , R 12 , R 15 , and R 16 are hydrogen, then R 14 and R 15 are not methoxy; and provided when n is 1, R 11 is
and R 10 , R 10′ , R 13 , R 14 , and R 16 are hydrogen, then R 12 and R 15 are not methoxy;
and provided that the compound is not a compound of claim 60 .
77 . A compound of formula III:
wherein
R 1″ is hydroxy or alkoxy;
Z is C(S), SO, SO 2 or PO 2 ;
m is 0 or an integer from 1-5;
R 17 and R 17′ are each independently hydrogen, alkyl, halogen, hydroxyl, thiol, alkenyl, alkynyl, aryl, acyl, alkoxy, amino, alkylamino or heterocyclic;
R 18 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, arylalkyl, amido, alkylamino, amino, arylamino, alkylcarbonyl, arylcarbonyl, alkylaminocarbonyl, alkoxy, alkoxycarbonyl, alkylcarbonyloxy, alkyloxycarbonyloxy, arylcarbonyloxy, aryloxy, thiol, alkylthio, arylthio, alkenyl, heterocyclic, heteroaryl, hydroxyl or halogen;
and racemates, isolated enantiomers or diastereomers, and pharmaceutically acceptable salts thereof;
provided that the compound is not a compound of claim 64.Join the waitlist — get patent alerts
Track US2008075692A1 — get alerts on status changes and closely related new filings.
We store only your email — no account needed. See our privacy policy.