摘要:
Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R?1, R2, R3¿, n, A, E, E', L, L', G and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
A is O; S or N-J; J is R 15 ; C(=O)R 16 ; C(=O)OR 17 ; C(=O)SR 18 ; C(=O)NR 19 R 20 ; P(=O)(C 1 -C 4 alkyl) 2 ; or OG; G is H; C 1 -C 6 alkyl; benzyl optinally substituted with R 34 on the phenyl ring; C(=O)(C 1 -C 4 alkyl); C(=O)(C 1 -C 4 alkoxy); or C(=O)NHR 36 ; B is H; halogen; cyano; NC; S=C=N; O=C=N; nitro; R 21 ; OR 29 ; NR 49 R 63 ; N=CR 45 R 46 ; SR 47 ; S(O) n R 48 ; or SO 2 NR 49 R 60 ; n is 1 or 2; R 1 , R 2 , R 3 and R 4 are various groups are disclosed with compositions containing them and methods of their use.
摘要翻译:式I的咪唑啉酮化合物其中:A为O; S或N-J; J为R 15; C(= O)R <16>; C(= O)OR <17>; C(= O)SR <18>; C(= O)NR <19> - [R <20>; P(= O)(C 1 -C 4烷基)2; 或OG; G是H; C1-C6烷基; 在苯环上被R 34选择性取代的苄基; C(= O)(C 1 -C 4烷基); C(= O)(C 1 -C 4烷氧基); 或C(= O)NHR 36; B是H; 卤素; 氰基; NC; S = C = N; O = C = N; 硝基; [R <21>; OR <29>; NR <49> - [R <63>; N = CR <45> - [R <46>; SR <47>; S(O)NR <48>; 或SO 2 NR 49 R 60; n为1或2; R 1,R 2,R 3和R 4各自是含有它们的组合物及其使用方法。
摘要:
Substituted phenylthiohydantoins are provided for use in detecting the presence of tumor cells having androgenic receptors and providing for cytostatic and cytotoxic activity toward such cells. The subject compounds provide for vehicles for specific targeting to the endrogenic receptor containing cells of cytostatic and/or cytotoxic agents, heavy or light radioactive or radioopaque atoms, and the like for detection and treatment of cancer cells involving androgenic receptors or blocking androgenic receptors.
摘要:
A compound is provided represented by the following general formula (A)
wherein two of R a , R b and R c are oxygen; X is a kind of benzyl, a kind of benzothiazolylmethyl, or a kind of naphthylmethyl; R is hydrogen or lower alkyl; n is an integer of 1 to 3; and Z indicates a direct bond or a bridging moiety containing one carbon atom. The compounds act as selective inhibitors of aldose reductase. The compounds provided are useful as drugs for therapy and prevention of various types of diabetic complications.
摘要:
The present invention deals with a product with the formula (I) which is a new prodrug of phenytoin, as well as its therapeutically acceptable solvates and addition salts. This product shows a solubility significantly higher than phenytoin itself. In addition, surprisingly, its hydrolisis rate is far higher than that of other known prodrugs of phenytoin, making it particularly useful as antiepileptic and antiarrhythmic agent.
摘要:
N-Iodopropargyl hydantoin compounds of the formulae (I) and (II)
wherein A is (C₁-C₁₂) straight or branched alkyl; benzyl; phenyl optionally substituted with halogen, nitro, cyano, halo(C₁-C₃)alkyl, or (C₁-C₃)alkoxy; allyl; (C₃-C₆)alkynyl optionally substituted with halogen; or hydrogen; R₁ and R₂ are each independently hydrogen; C₁-C₃ alkyl; or phenyl optionally substituted with halogen, nitro, (C₁-C₃)alkoxy or (C₁-C₃)haloalkyl; or can be joined, together with the hydantoin ring carbon to which they are attached, to form a saturated (C₃-C₇) or unsaturated (C₅-C₇) spiro ring; and R₃ and R₄ are each independently hydrogen or (C₁-C₃)alkyl, and use as antimicrobials and antifungal agents.
摘要:
Die Erfindung betrifft cyclische Harnstoffderivate der allgemeinen Formel
in der R a , R b , X und Y wie im Anspruch 1 definiert sind, deren Stereoisomere, einschließlich ihrer Gemische und deren Salze, insbesondere deren physiologisch verträgliche Salze mit anorganischen oder organischen Säuren oder Basen, welche wertvolle pharmakologische Eigenschaften aufweisen, vorzugsweise aggregationshemmende Wirkungen, die Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung.