摘要:
.alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要:
.alpha.-Amino acid amides of the formula I ##STR1## in which n is the number zero or one; R.sub.1 is C.sub.1 -C.sub.12 alkyl, which is unsubstituted or can be substituted by C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.3 -C.sub.8 cycloalkyl, cyano, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.3 -C.sub.6 alkenyloxycarbonyl or C.sub.3 -C.sub.6 alkynyloxycarbonyl; C.sub.3 -C.sub.8 cycloalkyl; C.sub.2 -C.sub.12 alkenyl; C.sub.2 -C.sub.12 alkynyl; C.sub.1 -C.sub.12 halogenoalkyl or a group NR.sub.13 R.sub.14 ; in which R.sub.13 and R.sub.14 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl or together are tetra- or pentamethylene; R.sub.2 and R.sub.3 independently of one another are hydrogen; C.sub.1 -C.sub.8 alkyl; C.sub.1 -C.sub.8 alkyl which is substituted by hydroxyl, C.sub.1 -C.sub.4 alkoxy, mercapto or C.sub.1 -C.sub.4 alkylthio; C.sub.3 -C.sub.8 alkenyl; C.sub.3 -C.sub.8 alkynyl; C.sub.3 -C.sub.8 cycloalkyl or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl, or in which the two groups R.sub.2 and R.sub.3, together with the carbon atom to which they are bonded, form a three- to eight-membered carbocyclic ring; R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.5 is hydrogen; C.sub.1 -C.sub.6 alkyl or phenyl, which is unsubstituted or can be substituted by halogen, nitro, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 halogenoalkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio; and R.sub.6 is a group G ##STR2## in which R.sub.7 and R.sub.8 independently of one another are hydrogen or C.sub.1 -C.sub.6 alkyl; p is the number zero or one; and R.sub.9, R.sub.10 and R.sub.11 independently of one another are hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 halogenoalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.6 alkenyloxy, C.sub.3 -C.sub.6 alkynyloxy, C.sub.3 -C.sub.6 alkylthio, halogen or nitro are valuable microbicides. They can be employed in crop protection in the form of suitable compositions, for example for controlling fungal diseases.
摘要:
The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.
摘要:
The present technology relates to methods for the synthesis of a lithium single-ion monomer which comprises simultaneously reacting a sulfonyl chloride compound with i) a fluorinated sulfonamide compound and ii) a compound that is suitable to act as a quenching base and a lithium cation source. The simultaneous reaction of sulfonyl chloride with the fluorinated sulfonamide compound and the compound that is suitable to act as a quenching base and a lithium cation source yields the single-ion monomer.
摘要:
Provided herein are compounds that are useful intermediates that may used to synthesize myeloid cell leukemia 1 protein (Mcl-1) inhibitors. Also provided are Mcl-1 inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I,
and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
摘要:
The present invention relates to substituted alkynylene compounds represented by the compounds of formula (I), pharmaceutically acceptable salts and stereoisomers thereof. The present invention further provides the therapeutic uses of the compounds of formula (I) as anti-cancer agents.
摘要:
(1) Prostaglandin (PG) E.sub.2 antagonist or agonist containing carbocyclic sulfonamides represented by the compound of the formula (I): ##STR1## cyclodextrin clathrates thereof, non-toxic salts thereof as active ingredient,(2) carbocyclic sulfonamides represented by the compound of the formula (II): ##STR2## cyclodextrin clathrates thereof, non-toxic salts thereof, (3) process for the preparation of the compound represented by the compound of the formula (II) described hereinbefore,(4) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (II) as active ingredient.The compounds represented by the compounds of the formula (I) and (II) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgetic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE.sub.2 antagonists, and an uterine contractile activity, a promoting effect of digestive peristalsis, a suppressive effect of gastric acid secretion, a hypotensive activity as PGE.sub.2 agonists, because they bind onto PGE.sub.2 receptor and have an activity of antagonist or agonist against the action thereof.
摘要:
.alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要:
The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.
摘要:
The invention relates to a compound selected from those of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and Medicinal product containing the same useful for treating a disorder of the melatoninergic system.