Back to results
US 6,548,637 B1Granted
Ligands for opioid receptors
AssigneeSepracor Inc.
InventorsPaul E. Persons, James R. Hauske, Roushan A. Hussoin
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds, and pharmaceutical preparations thereof, that bind selectively to mammalian opioid receptors. The present set of compounds comprises full agonists, partial agonists, and antagonists of mammalian opioid receptors.
Claims79
A compound of structure 33:
- wherein
- X represents, independently for each occurrence, O, S, H2, or NR;
- Y represents, independently for each occurrence, F, Cl, Br, or I;
- R represents, independently for each occurrence, H, Me, lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl;
- R5, independently for each occurrence, is absent, or present between one and the maximum number of times permitted by the additional substitution on the relevant aromatic ring;
- R5, when present, is selected independently for each occurrence from the set consisting of Me, lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, heterocycloalkyl, halogen, hydroxyl, alkoxyl, nitro, nitroso, cyano, acyl, acylamino, amido, sulfonyl, sulfonamido, and acyloxy;
- and
- the stereochemical configuration at any stereocenter of a compound represented by 33 is R, S, or a mixture of these configurations.
5 more elements
A compound of structure 35:
- wherein
- X represents, independently for each occurrence, O, S, H,, or NR;
- Y represents —OR;
- R represents, independently for each occurrence, H, Me, lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl;
- R5, independently for each occurrence, is absent, or present between one and the maximun number of times permitted by the additional substitution on the relevant aromatic ring;
- R5, when present, is selected independently for each occurrence from the set consisting of Me, lower alkyl, lower heteroalkyl, aryl, heteroaryl aralkyl, heteroaralkyl, cycloalkyl, heterocycloalkyl, halogen, hydroxyl, alkoxyl, nitro, nitroso, cyano, acyl, acylamino, amido, sulfonyl, sulfonamido, and acyloxy;
- p is an integer in the range 1 to 3 inclusive;
- and
- the stereochemical configuration at any stereocenter of a compound represented by 35 may be R, S, or a mixture of these configurations.
6 more elements
A compound of structure 45:
- wherein
- X independently for each occurrence represents O, S, H2, or NR:
- Y represents (C(R2))p, (O(CR2)m), (S(CR2)m), (C(O)(CR2)m, (CH(OR)(CR2)m), or (CR(NR2)(CR2)m);
- R independently for each occurrence represents H, Me, lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, or heterocycloalkyl;
- R′ represents lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, or heterocycloalkyl;
- R″ independently for each occurrence represents aryl, heteroaryl, aralkyl, or heteroaralkyl;
- m is an integer in the range 0 to 2 inclusive;
- p is an integer in the range 1 to 3 inclusive;
- n is an integer in the range 0 to 3 inclusive;
- and
- the stereochemical configuration at any stereocenter of a compound represented by 45 is R, S, or a mixture of these configurations.
8 more elements
A compound of structure 46:
- wherein
- X independently for each occurrence repesents O, S, H2, or NR;
- Y represents (C(R2))p, (O(CR2)m), (S(CR2)m), (C(O)(CR2)m), (CH(OR)(CR2)m), or (CR(NR2)(CR2)m);
- R independently for each occurrence represents H, lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, or heterocycloalkyl;
- R″ independently for each occurrence represents aryl, heteroaryl, aralkyl, or heteroaralkyl;
- R1, independently for each occurrence, is absent, or present between one and the maximum number of times permitted by the additional substitution on the relevant aromatic ring;
- R1, when present, is selected independently for each occurrence from the set consisting of lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, heterocycloalkyl, halogen, hydroxyl, alkoxyl, nitro, nitroso, cyano, acyl, acylamino, amido, sulfonyl, sulfonamido, and acyloxy;
- p is an integer in the range 1 to 3 inclusive;
- m is an integer in the range 0 to 2 inclusive;
- n is an integer in the range 0 to 3 inclusive;
- and
- the stereochemical configuration at any stereocenter of a compound represented by 46 is R, S, or a mixture of these configurations.
9 more elements
A compound of structure 47:
- wherein
- X independently for each occurrence represents O, S, or NR;
- W represents lower alkyl;
- R independently for each occurrence represents H, Me, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, or heterocycloalkyl;
- R′ represents lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, or heterocycloalkyl;
- R″ independently for each occurrence represents aryl, heteroaryl, aralkyl, or heteroaralkyl;
- n is an integer in the range 0 to 3 inclusive;
- and
- the stereochemical configuration at any stereocenter of a compound represented by 47 is R, S, or a mixture of these configurations.
6 more elements
A compound of structure 48:
- wherein
- X independently for each occurrence represents O, S, H2, or NR;
- W represents lower alkyl;
- R independently for each occurrence represents H, lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, or heterocycloalkyl;
- R″ independently for each occurrence represents aryl, heteroaryl, aralkyl, or heteroaralkyl;
- R1, independently for each occurrence, is absent, or present between one and the maximum number of times permitted by the additional substitution on the relevant aromatic ring;
- R1, when present, is selected independently for each occurrence from the set consisting of lower alkyl, lower heteroalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, cycloalkyl, heterocycloalkyl, halogen, hydroxyl, alkoxyl, nitro, nitroso, cyano, acyl, acylamino, amido, sulfonyl, sulfonamido, and acyloxy;
- n is an integer in the range 0 to 3 inclusive;
- and
- the stereochemical configuration at any stereocenter of a compound represented by 48 is R, S, or a mixture of these configurations.
7 more elements
Dependencies are inferred from the claim text.