[EN] NOVEL GALACTOSIDE INHIBITOR OF GALECTINS<br/>[FR] NOUVEAU GALACTOSIDE COMME INHIBITEUR DE GALECTINES
申请人:GALECTO BIOTECH AB
公开号:WO2021001528A1
公开(公告)日:2021-01-07
The present invention relates to a D-galactopyranose compound of formula (1) wherein the pyranose ring is α-D-galactopyranose, and these compounds are high affinity galectin-1 and/or galectin 3 inhibitors for use in treatment of inflammation; fibrosis; scarring; keloid formation; aberrant scar formation; surgical adhesions; septic shock; cancer; metastasising cancers; autoimmune diseases, metabolic disorders; heart disease; heart failure; pathological angiogenesis; eye diseases; atherosclerosis; metabolic diseases; diabetes type I; diabetes type II; insulin resistance; Diastolic heart failure; asthma; liver disorders.
A process for the preparation of a hetaryloxyacetamide of the formula ##STR1## in which R.sup.1 is an optionally substituted oxazole, thiazole or tetrazole radical, comprising reacting a hydroxyacetamide of the formula ##STR2## with a halogeno-hetarene of the formula R.sup.1 --Hal in which Hal represents a fluorine, chlorine, bromine or iodine atom, in the presence of solid, anhydrous potassium hydroxide and in the presence of an aprotic diluent at a temperature between about -50.degree. and +50.degree. C.
Seventy novel benzoylphenylurea compounds were synthesized and their antitumor activities were examined in vivo against P388 leukemia. N-(2-Nitrobenzoyl)-N'-[4-(2-pyrimidinyloxy)phenyl]ureas showed the highest antitumor activities when dosed intraperitoneally or orally. Their structure-activity relationships were examined with particular focus on the position and the variety of subsitituent on each aryl ring.
Trichlorothiazole is prepared by reacting 1,2-dichloroethyl-isocyanide dichloride with a sulphur chloride at elevated temperatures in the presence of catalytic amounts of a Friedel-Crafts catalyst.
[EN] MICROBIOCIDAL PHENYLAMIDINE DERIVATIVES WITH IMPROVED PLANT SAFETY PROPERTIES<br/>[FR] DÉRIVÉS PHÉNYLAMIDINES MICROBIOCIDES AYANT DES PROPRIÉTÉS AMÉLIORÉES DE SÉCURITÉ DES PLANTES
申请人:SYNGENTA PARTICIPATIONS AG
公开号:WO2018178057A1
公开(公告)日:2018-10-04
A method of improving plant safety and/or reducing phytotoxicity and/or reducing plant necrosis whilst combating, preventing or controlling phytopathogenic diseases, which comprises applying to a phytopathogen, to the locus of a phytopathogen, or to a plant susceptible to attack by a phytopathogen, or to propagation material thereof, a fungicidally effective amount of a compound of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in claim 1. Furthermore, the present invention relates to novel compounds of formula (I) and to agrochemical compositions which comprise them, to the preparation of these compounds and compositions, and to the use of the compounds or compositions in the aforementioned methods.