摘要:
Chromogenic enzyme substrate compounds comprising a dibenz[b,e] [1,4]oxazepinone or dibenzo[b,e][1,4]thiazepinone nucleus having an enzyme-cleavable group such as a radical of a sugar, carboxylic acid, amino acid, peptide, phosphoric acid, or sulfuric acid. The substrate compounds are, in general, highly soluble in aqueous media and only slightly colored, and produce, upon enzyme cleavage, a chromogen exhibiting a large change in absorbance and a pKa below 7. Such substrates find use as indicators for the determination of enzyme analytes and enzymes used as markers in a variety of assays, including immunoassays.
摘要:
Disclosed are the novel compounds represented by structural Formula (I), wherein A is a lipophilic group comprising an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptable salts and individual isomers thereof, which have growth hormone releasing activity in humans or animals.
摘要:
Chromogenic enzyme substrate compounds comprising a dibenz[b,e] [1,4]oxazepinone or dibenzo[b,e][1,4]thiazepinone nucleus having an enzyme-cleavable group such as a radical of a sugar, carboxylic acid, amino acid, peptide, phosphoric acid, or sulfuric acid. The substrate compounds are, in general, highly soluble in aqueous media and only slightly colored, and produce, upon enzyme cleavage, a chromogen exhibiting a large change in absorbance and a pKa below 7. Such substrates find use as indicators for the determination of enzyme analytes and enzymes used as markers in a variety of assays, including immunoassays.
摘要:
The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
摘要:
Novel antitumor sulfonamide and sulfonic ester derivatives each having a tricyclic hetero ring, represented by general formula (I), and a process for producing the same, wherein G represents a 5- or 6-membered aromatic ring; L represents O or NR1, wherein R1 represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from the members (a), (b), (c), (d), (e), (f), wherein rings A and B represent each a 5- or 6-membered unsaturated ring; X represents NR2 (wherein R2 represents hydrogen or lower alkyl) or NHCO; Y represents O, S(O)¿n?, CR?3R4¿, CO, NR?5, CHR6CHR7, CR8=CR9, NR10¿CO, N=CR?11, OCHR12¿, S(O)¿n?CHR?13 or NR14CHR15¿; and Z represents N or CR16, wherein n represents 0, 1 or 2; R?3-R13, R15 and R16¿ represent each hydrogen or lower alkyl; and R14 represents hydrogen, lower alkyl or lower acyl.
摘要:
Novel antitumor sulfonamide and sulfonic ester derivatives each having a tricyclic hetero ring, represented by general formula (I), and a process for producing the same, wherein G represents a 5- or 6-membered aromatic ring; L represents O or NR¹, wherein R¹ represents hydrogen or lower alkyl; and M represents a tricyclic structure selected from the members (a), (b), (c), (d), (e), (f), wherein rings A and B represent each a 5- or 6-membered unsaturated ring; X represents NR² (wherein R² represents hydrogen or lower alkyl) or NHCO; Y represents O, S(O) n , CR³R⁴, CO, NR⁵, CHR⁶CHR⁷, CR⁸=CR⁹, NR¹⁰CO, N=CR¹¹, OCHR¹², S(O) n CHR¹³ or NR¹⁴CHR¹⁵; and Z represents N or CR¹⁶, wherein n represents 0, 1 or 2; R³-R¹³, R¹⁵ and R¹⁶ represent each hydrogen or lower alkyl; and R¹⁴ represents hydrogen, lower alkyl or lower acyl.
摘要:
Use of compounds of formula (I): wherein X is S, O, S=O, SO2, NRa, or CRbRc;R1,R2 are halogen, OH, SH, NH2, CN, NO2, alkyl, alkoxy, alkylamino, dialkylamino, alkylthio, alkenyl, alkenyloxy, alkenylamino, alkenylthio, alkynyl, alkynyloxy, alkynylamino, alkynylthio, alkylsulfonyl, alkylsulfoxyl, alkenylsulfonyl, alkynylsulfoxyl, formyl, alkylcarbonyl, hydroxycarbonyl, alkoxycarbonyl, carbonyloxy, alkylcarbonyloxy, phenyloxy, alkylcarbonylamino, C(O)NRdRe, or (SO2)NRdRe, or C=NORf)-Gp-Rf', ora mono- or bicyclic 5- to 10-membered aromatic or heteroaromatic ringsystem, optionally substituted, which is unfused or fused to the aromatic group to which it is bonded and which, when unfused, is bonded directly or through an O, S, alkyl, or alkoxy linkage, or cycloalkyl, wherein the carbon atoms in these groups may be substituted.R3,R4 are each independently H, alkyl, haloalkyl, alkylamino, alkoxy, cycloalkyl, wherein the carbon atoms in these groups may be substituted, or R3 and R4 together with the nitrogen atom to which they are attached form a saturated or partially saturated mono- or bicyclic 5- to 10-membered ringsystem or 5-membered hetaryl, phenyl or benzyl, wherein the rings are optionally sub-stituted, or R3 and R4 together form the chains -(CH2)2N+(O-)(CH2)2- or -(CH2)3N+(O-)(CH2)2-;and Ra, Rb, Rc, Rd, Re, Rf', Rf, G, and p are as defined in the description;m is 0, 1, 2, 3 or 4;n is 0, 1, 2, 3 or 4;or the enantiomers or diastereomers, salts or esters thereof for combatting insects, arachnids, or nematodes, methods for the control of these pests and of protecting growing plants from attack or infestation by these pests by applying a pesticidally effective amount of compounds of formula ( I), compounds of formula (I), processes for preparing them, and compositions comprising them.
摘要:
A process for producing dibenzothiazepine derivatives typified by dibenzo[b,f][1,4]thiazepin-11-one which are usable as the starting material for producing 11-[4-(2-(2-hydroxyethoxy)ethyl)]-1-piperazinyldibenzothiazepine derivatives useful as a psychotropic drug, which comprises reacting a nitrobenzene derivative with a thiosalicylic acid derivative, reducing the thus obtained 2-nitro-2'-carboxy-diphenylsulfide derivative, and then further dehydrating and condensing the thus obtained 2-amino-2'-carboxy-diphenylsulfide derivative.