摘要:
Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.
摘要:
The present invention provides compounds of the formula (I) ##STR1## wherein A, R.sub.1, R.sub.2 and R.sub.3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmacetical compositions comprising them are also provided.
摘要:
THIS INVENTION CONCERNS THE NEW COMPOUND, (5R,8R)8 - (3-AZABICYCLO(3,2,2)NONAN-3-YLMETHYL) - 6 - METHYLERGOLENE, USEFUL AS A SEDATIVE AND SLEEP-PROMOTING AGENT.
6H-INDOLO(4,3-FG)QUINOLINE WHERE THE 10,10A POSITION IS
X--Y
IN WHICH R1 IS HYDROGEN OR METHYL, AND R2 IS ARALKYL OF 7 TO 9 CARBON ATOMS, ARYL OR ARYL SUBSTITUTED BY ONE OR MORE OF THE FOLLOWING RADICALS: METHYL, ALKOXY OF 1 TO 4 CARBON ATOMS, CHLORINE OR BROMINE, AND
X--Y IS -CH=C AND THEIR ACID ADDITION SALTS. THE COMPOUNDS IN WHICH R1 IS HYDROGEN AND
X--Y IS -CH=C HAVE ANTIDEPRESSIVE PROPERTIES. THE REMAINING COMPOUNDS HAVE SEDATIVE PROPERTIES. THE PREPARATION OF THE COMPOUNDS IS ALSO DESCRIBED.
摘要:
The present invention provides an improved method for the production of lysergic acid diethylamide (LSD) for GMP purposes. Furthermore, the present invention provides novel LSD derivatives of formula I as well as their synthesis and purification. Due to the affinity of the presented substances for the 5-HT2A receptor, the invention may find application in numerous forms of therapy, such as against depression or drug addiction.
摘要:
Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.
摘要:
The invention provides compounds of formula I wherein R1 to R6 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.
AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF. THE COMPOUNDS ARE USEFUL IN THE TREATMENT OF CONDITIONS OF ORTHOSTASIS AND HYPERTONIA, AND ARE ALSO SALIDIURETICS, ANTI-PHLOGISTICS AND EDEMA-INHIBITORS.