Abstract:
The present invention relates to 4-[(alkylsulfanyl)methyl]-1, 2-benzenediol derivative, preparation method thereof and antioxidant containing the same. More particularly, 4-[(alkylsulfanyl)methyl]-1, 2-benzenediol derivative following Formula (1) can inhibit generation of melanin due to its excellent antioxidant activity and can regulate blood cholesterol level by repressing oxidation of low density lipoprotein. Accordingly, the present invention can be useful for treatments of arteriosclerosis and skin deposit by reactive oxygen species.
Abstract:
Offenbart werden Verbindungen der Formel (I), worin Z ein Kohlenwasserstoff mit 2 bis 28 C-Atomen ist, wobei Z auch die Elemente N, O, P, S, Si und Halogen als Heteroatome umfassen kann, R 1 und R 2 sind gleiche oder verschiedene H oder Schwefel-Schutzgruppen, wobei die beiden S-Atome auch eine Disulfid-Brücke ausbilden können und in diesem Fall R 1 , R 2 nicht vorhanden sind, Schutzgruppe-Y 1 ist Schutzgruppe-NH, Schutzgruppe-NR 4 , Schutzgruppe-O, CONH-Schutzgruppe, Schutzgruppe-OOC, Schutzgruppe-S-S, -CH(Schutzgruppe-O) 2 , oder -CR 5 (SchutzgruppeO) 2 oder Schutzgruppe-S, Y 2 ist -OH, -NH 2 , -NHR 3 , -NR 3 R 4 , -COOH, -COCI, -COOCO-R 6 , -CONH 2 , -CONHR 3 , -COOR 3 , -SO 3 H, -SO 3 CI, -SH, -S-SR 3 , -CHO, -COR 3 , -C 2 H 3 O, Halogen, -N 3 , -NH-NH 2 , -NCO, -NCS, wobei R 3 Alkyl, Heteroalkyl, Aryl, Cycloalkyl oder eine Schutzgruppe ist, wobei R 3 in den Gruppen Y 1 und Y 2 gleich oder verschieden vorliegen kann, R 4 eine Schutzgruppe ist, wobei R 4 in den Gruppen Y 1 und Y 2 gleich oder verschieden vorliegen kann, und wobei R 4 und R 3 gleich oder verschieden sein können, R 5 Alkyl, Aryl, Cycloalkyl ist, wobei R 5 in den Gruppen Y 1 und Y 2 gleich oder verschieden vorliegen kann, und R 6 Alkyl, Heteroalkyl, Aryl oder Cycloalkyl ist, wobei R 6 in den Gruppen Y 1 und Y 2 gleich oder verschieden vorliegen kann, wobei Y 2 auch eine Gruppe der Formel (II) oder Formel (III) sein kann, wobei X 1 ein Halogen oder ein substituiertes Amin ist, X 2 ein Alkyl-, Alkoxy-, Aryloxy-Rest oder ein Cyanoderivat eines Alkyl-, Alkoxy-, Aryloxy-Restes ist, X 3 ein Halogen, eine Aminofunktion oder Sauerstoff ist und X 4 ein Alkyl-, Alkoxy-, Aryloxy-Rest ist oder X 4 gleich H ist für den Fall, dass X 3 = Sauerstoff ist.
Abstract:
The invention relates to compounds of formula (I), wherein Z represents a hydrocarbon with 2 to 28 C atoms, wherein Z can also comprise elements N, O, P, S, Si and halogen as heteroatoms, R1 and R2 are identical or different sulfur protecting groups, wherein both S atoms can also form a disulfide bridge and in said case R1 and R2 are not present; protecting group Y1 represents protecting group NH, protecting group NR4, protecting group O, CONH protecting group, protecting group OOC, protecting group S-S, -CH(protecting group O)2 or -CR5(protecting group O)2 or protecting group S; Y2 represents -OH, -NH2, -NHR3, -NR3R4, -COOH, -COCI, -COOCO-R6, -CONH2, -CONHR3, -COOR3, -SO3H, -SO3CI, -SH, -S-SR3, -CHO, -COR3, -C2H3O, halogen, -N3, -NH-NH2, -NCO, -NCS, wherein R3 represents alkyl, heteroalkyl, aryl, cycloalkyl or a protecting group, wherein R3 can be identical or different in groups Y1 and Y2, R4 is s protecting group, wherein R4 can be identical or different in groups Y1 and Y2, and wherein R4 and R3 can be identical or different, R5 represents alkyl, aryl or cycloalkyl, wherein R5 can be identical or different in groups Y1 and Y2 and R6 represents alkyl, heteroalkyl, aryl or cycloalkyl, wherein R6 can be identical or different in groups Y1 and Y2, wherein Y2 can also represent a group of formula (II) or formula (III), wherein X1 represents halogen or a substituted amine, X2 represents an alkyl, alkoxy, aryloxy radical or a cyano derivative of an alkyl, alkoxy, aryloxy radical, X3 represents halogen, an amino function or oxygen and X4 represents an alkyl, alkoxy, aryloxy radical or X4 equals H if X3 = oxygen.
Abstract:
The present invention relates to novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatits, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
Abstract:
In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflammatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provides the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.
Abstract:
Alkenyldiarylmethane (ADAM) compounds have been found effective as anti-HIV agents. Novel ADAM compounds, their pharmaceutical formulations and a method of using same to treat viral infections are described.
Abstract:
Cancer remedies, each containing a compound of the following general formula (I): Ar -S-R -S-Ar [wherein RP represents a non-metallic connecting group; Ar and Ar each independently represents aryl or heteroaryl having 1 to 3 hydroxyls which may be substituted with a monovalent group on the ring thereof (and optionally having 1 to 3 substituents other than the hydroxyl on the ring thereof)] or a physiologically acceptable salt thereof; and compounds of the following general formula (XII): Ar -S-R -N(R )-R -S-Ar [wherein R and R each independently represents a divalent group; R represents a monovalent group or atom, or R may be bonded to R and/or R to form a cyclic structure and further bonded to one or two C1-4 alkylene groups to form a divalent group; and Ar and Ar each independently represents aryl or heteroaryl (optionally having 1 to 3 substituents other than hydroxyl on the ring thereof) having 1 to 3 hydroxyls which may be substituted with a monovalent group; excluding specified compounds] and salts thereof.
Abstract:
Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) lower alkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl -L2-, and (i) heterocyclic -L2-; R2 is selected from (a) formula (1), (b) -C(O)NH-CH(R14)-C(O)OR15, (c) formula (2), (d) -C(O)NH-CH(R14)-C(O)NHSO2R16, (e) -C(O)NH-CH(R14)-tetrazolyl, (f) -C(O)NH-heterocyclic, and (g) -C(O)NH-CH(R14)-C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, formula (3), and -P(W)R R ; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylalkyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) -L4-N(R5)-L5-, (b) -L4-O-L5-, (c) -L4-S(O)n-L5-, (d) -L4-L6-C(W)-N(R5)-L5-, (e) -L4-L6-S(O)m-N(R5)-L5-, (f) -L4-N(R5)-C(W)-L7-L5-, (g) -L4-N(R5)-S(O)p-L7-L5-, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene, (k) a covalent bond, (1) formula (4), and (m) formula (5) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
Abstract translation:具有式(I)的化合物或其药学上可接受的盐,其中R1是(a)氢,(b)低级烷基,(c)烯基,(d)烷氧基,(e)硫代烷氧基,(f)卤素,(g) ,(h)芳基-L2-,和(i)杂环-L 2 - ; R2选自(a)式(1),(b)-C(O)NH-CH(R 14)-C(O)OR 15,(c)式(2),(d)-C(O)NH -CH(R 14)-C(O)NHSO 2 R 16,(e)-C(O)NH-CH(R 14) - 四唑基,(f)-C(O)NH-杂环,和(g)-C NH-CH(R 14)-C(O)NR 17 R 18; R 3是取代或未取代的杂环或芳基,取代或未取代的环烷基或环烯基,式(3)和-P(W)R R 3 R 3' R4是氢,低级烷基,卤代烷基,卤素,芳基,芳烷基,杂环或(杂环)烷基; (a)-L4-N(R5)-L5-,(b)-L4-O-L5-,(c)-L4-S(O)n-L5-,(d) -L4-L6-C(W)-N(R5)-L5-,(e)-L4-L6-S(O)mN(R5)-L5-,(f)-L4-N(R5)-C (W)-L7-L5-,(g)-L4-N(R5)-S(O)p-L7-L5-,(h)任选取代的亚烷基,(i)任选取代的亚烯基,(j) 亚烷基,(k)共价键,(1)式(4)和(m)式(5)是蛋白质异戊二烯基转移酶的抑制剂。 还公开了蛋白质异戊二烯转移酶抑制组合物和抑制蛋白质异戊二烯转移酶的方法。
Abstract:
Calixarene-based compounds are described which have biological activity, particularly anti-bacterial, anti-fungal, anti-cancer and anti-viral activity. Some compounds have been found to have anti-HIV activity. The compounds are calixarenes or oxacalixarenes, acylic phenyl-formaldehyde oligomers, cyclotriveratrylene derivatives, cyclic tetrameric resorcinol-aldehyde derivatives known as Hogberg compounds and cyclic tetrameric pyrogallol-aldehyde derivatives.