74531-82-1Relevant academic research and scientific papers
INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS
-
Page/Page column 244; 245, (2021/01/29)
The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
SUBSTITUTED SULPHONAMIDES FOR CONTROLLING ANIMAL PESTS
-
Paragraph 0328-0330, (2020/12/14)
The present invention relates to the use of a compound of the general formula (I) in which M and D have the meanings given in the description for controlling animal pests.
Amino-Indolyl-Substituted Imidazolyl-Pyrimidines and Their Use as Medicaments
-
Paragraph 0226; 0227; 0228, (2013/11/05)
The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 wherein R1, R2, R3, R4 and R5 are defined as in claim 1 and pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system.
AMINO-INDOLYL-SUBSTITUTED IMIDAZOLYL-PYRIMIDINES AND THEIR USE AS MEDICAMENTS
-
Page/Page column 48, (2013/11/05)
The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula (1), wherein R1, R2, R3, R4 and R5 are defined as in claim 1 and pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system
Novel farnesyl protein transferase inhibitors as antitumor agents
-
Page 467-468, (2010/02/07)
Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
Synthesis and structure-activity relationships of new (5R,8R,10R)-ergoline derivatives with antihypertensive or dopaminergic activity
Ohno,Adachi,Koumori,Mizukoshi,Nagasaka,Ichihara,Kato -
, p. 1463 - 1473 (2007/10/02)
A series of new (5R,8R,10R)-ergoline derivatives was synthesized, and their antihypertensive and dopaminergic activities were tested in conscious spontaneously hypertensive rats and in rats with unilateral 6- hydroxydopamine-induced lesions of the substantia nigra. (5R,8R,10R)-6- Alkyl-8-ergolinemethanols, prepared from the corresponding ergolinecarboxylates, were converted to the tosylates, which were treated with various five-membered heterocycles containing nitrogen atoms to afford the new ergolines. (5R,8R,10R)-8-(1,2,4-Triazol-1-ylmethyl)-6-methylergoline (4s, maleate: BAM-1110) exhibited potent dopaminergic activity, about 18- fold greater than that of bromocriptine mesylate. (5R,8R,10R)-8-(1,2,4- Triazol-1-ylmethyl)-6-propylergoline (8b, fumarate: BAM-1602) showed extremely potent dopaminergic activity, being about 220 and 1.15 times more active than bromocriptine mesylate and pergolide mesylate, respectively. Several compounds exhibited potent antihypertensive activity. Structure- activity relationships for antihypertensive and dopaminergic activities are discussed.
