摘要:
Compounds of formula (I) wherein R1 or R2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L2 and L3, to a heteroaromatic core, and X, X', Y, Y', Z, Z', R1, R2, R3, R3a, R3b, R4, R5, L, L2, and L3 are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
摘要:
An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.
摘要:
Compounds of formula (I) wherein R1 or R2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R1, R2, R3, R3a, R3b, R4, R5, L, X, X', Y, Y', Z, and Z' are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
摘要:
An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.
摘要:
Compounds of formula (I) wherein R1 or R2 is an aromatic or non-aromatic ring directly joined or joined by a linker, as represented by L2 and L3, to a heteroaromatic core, and X, X', Y, Y', Z, Z', R1, R2, R3, R3a, R3b, R4, R5, L, L2, and L3 are as defined herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
摘要:
The invention discloses compounds of formula ( II ): and methods of making the compounds, which are VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
摘要:
Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).