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JP5147814B2 |
To provide a new compound for treating patients having a bacterial infectious disease, and to provide pharmaceutical preparations containing an effective amount of the compound. An antibiotic derived from a steroid is, for example, a com...
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JP5139609B2 |
A series of novel steroid derivatives are described. The steroid derivatives are antibacterial agents. The steroid derivatives also act to sensitize bacteria to other antibiotics including erythromycin and novobiocin.
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JP5133937B2 |
A process for preparing an intermediate compound of formula (II) where X is as defined in the specification, R 1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl; R 2 , R 3 , R 4 and R 5 are ...
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JP2012532833A |
The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group LM, which has increased lipophilicity, of a vecto...
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JP5095413B2 |
There are provided a novel process for producing [{(5Z,7E)-(1S,3R,20S)-1,3-dihydroxy-9,10-secopregna-5,7,10(1
9),16-tetraen-20-yl}oxy]-N-(2,2,3,3,3-pentafluoropropyl)acet
amide, which process is characterized by irradiating a compound re...
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JP5097724B2 |
A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereose...
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JP5094400B2 |
The present invention provides a novel hypertension therapeutic agent. The hypertension therapeutic agent of the present invention contains, as an active ingredient, a compound represented by formula (1): [F1] or a pharmaceutically accep...
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JP5074655B2 |
There is provided a compound of Formula I wherein X is a ring system; R 1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R 2 is any one of a sulphamate group, a...
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JP5052726B2 |
Compounds able to chelate paramagnetic metal ions and the use thereof as contrast agents in the technique known as "Magnetic Resonance Imaging" (M.R.I.).
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JP5052730B2 |
A series of novel steroid derivatives are described. The steroid derivatives are antibacterial agents. The steroid derivatives also act to sensitize bacteria to other antibiotics including erythromycin and novobiocin.
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JP5031942B2 |
The present invention relates to bile acid or bile salt fatty acid conjugates (hereinafter called "BAFAC), to their use in dissolving cholesterol gallstones in bile, preventing their occurrence or recurrence, to their use in reducing or ...
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JP4999784B2 |
Lipopolyamines useful for the transfection of nucleic acid and methods of preparation thereof are disclosed. The lipopolyamines are of general formula I, in which R4 comprises at least one C10-C22 aliphatic radical.
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JP5000294B2 |
There is provided a compound of Formula I wherein (I) R 1 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R 2 is capable of forming a hydrogen bond (iii) alkylaryl group, wherein the aryl group is substitu...
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JP2012517463A |
A process for the preparation of cholyl-L-lysine comprising the steps of: —(a) reacting N-ε-CBZ-cholyl-L-lysine with a hydrogen source in the presence of a catalyst in a solvent comprising one or more alkanols; (b) removing the cataly...
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JP4959276B2 |
Novel and anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependant disorders. Preferred compounds have 1,3,5-estratiene nucleus, and are substituted at the C-17 or C-11 posi...
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JP4958377B2 |
There is provided a compound of Formula I wherein X is a ring system; R 1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R 2 is any one of a sulphamate group, a...
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JP2012511027A |
The invention provides compositions or pharmaceutical compositions of novel high penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capabl...
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JP4933250B2 |
The invention relates to the use of 2-substituted estra-1,3,5(10)-triene-3-yl sulfamates of general formula I, in addition to their pharmaceutically acceptable salts for producing a medicament. Said compounds have an anti-tumour action.
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JP4931312B2 |
A compound is described. The compound has the formula (Ia) as presented in the FIG. 1; wherein: X is a ring having at least 4 atoms in the ring; K is hydrocarbyl group; Rh1 is an optional halo group; Rh2 is an optional halo group; at lea...
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JP4928729B2 |
Diamine compounds, which in particular are useful as precursors for the production of liquid crystal alignment layers, represented by the general formula I: wherein A<1> represents an organic group of 1 to 40 carbon atoms; A<2> repre...
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JP2012051935A |
To provide new steroids which possess antiprogestational activity with minimal antiglucocorticoid activity.In addition to providing compounds of formula I, the present invention relates to methods where the compounds of Formula I are adv...
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JP4866740B2 |
Compounds having the structure or their salts: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, sebor...
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JP4860880B2 |
The invention relates to novel 8ß-substituted estratrienes of the general formula (I), wherein R2, R3, R6, R6', R7, R7', R9, R11, R11', R12, R14, R15, R15', R16, R16', R17 and R17' are defined as in the description and R8 represents a s...
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JP4842475B2 |
A process for the preparation of the compounds of general formula (I)in whichR1 is H or OH;R2 is H, alpha-OH, or beta-OH; andR3 is a straight or branched C1-C4 alkyl group or a benzyl group,comprising the reduction of compounds of formul...
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JP4837858B2 |
The invention is directed to a novel class of 17beta-acyl-17alpha-propynyl steroids which exhibit potent antiprogestational activity.
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JP4833471B2 |
The invention relates to substituted 4-benzylaminoquinolines and their hetero analogs, and to the pharmaceutically acceptable salts and physiologically functional derivatives thereof. Compounds of formula Iin which the radicals are defin...
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JP4778438B2 |
The present invention relates to novel 3, 15 substituted estrone derivatives which represent inhibitory compounds of the 17beta-hydroxysteroid dehydrogenase type I (17beta-HSD1), to their salts, to pharmaceutical preparations containing ...
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JP4768941B2 |
Substituted acylguanidines and their pharmaceutically tolerable salts and physiologically functional derivatives.Compounds of the formula Iin which the radicals have the meanings indicated, and their physiologically tolerable salts, phys...
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JP4750281B2 |
The invention concerns compounds of formula (I) wherein: X, Y, R1, R2, Z, G are as defined in the description, the methods for preparing them and the intermediates in said method, their use as medicine and the pharmaceutical compositions...
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JP2011148821A |
To provide a novel method for preparing a cortisol conjugate.The method for preparing the cortisol conjugate includes reacting 3-cortisolcarboxymethyl oxime conjugated to bovine serum albumin (3-CMO-BSA) with sodium borohydride.
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JP4727923B2 |
Disclosed are aqueous and nonaqueous solution formulations containing agents that are useful for treating cancer.
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JP4719144B2 |
The present invention provides a compound comprising a steroidal ring system and an optional group R1 selected from any one of —OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide ...
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JP4718512B2 |
Novel and anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependant disorders. Preferred compounds have 1,3,5-estratiene nucleus, and are substituted at the C-17 or C-11 posi...
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JP4718439B2 |
This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for ...
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JP2011121966A |
To provide cationic lipids and compositions of the cationic lipids having utility in lipid aggregates for delivery of macromolecules and other materials into cells.There are provided compounds expressed by general structural formula. The...
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JP4709751B2 |
A process for preparing a compound of formula (I): wherein X represents O or S; R 1 represents C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylmethyl or C 3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl g...
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JP4709752B2 |
A process for preparing a compound of formula (I): wherein X represents O or S; R 1 represents C 1-6 alkyl, C 3-8 cycloalkyl, C 3-8 cycloalkylmethyl or C 3-8 cycloalkenyl any of which optionally may be substituted by one or more methyl g...
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JP4648891B2 |
The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, ...
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JP4629333B2 |
The invention concerns novel transfecting compounds consisting of an aminoglycoside bound to a lipid via a spacer, and their polyguanidyl derivatives. Said compounds are useful for in vitro, ex vivo or in vivo transfection of nucleic aci...
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JP4629030B2 |
The invention relates to a process for preparing compounds of formula (I): in which R1, R2, R3, n and X are as defined in the description, and to the intermediate compounds for implementing this process.
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JP4616479B2 |
Substituted phenylalkenoylguanidines, processes for their preparation, uses as medicaments or diagnostics, and medicaments containing them are described. The invention relates to substituted phenylalkenoylguanidines and their pharmaceuti...
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JP4615998B2 |
The invention relates to novel 9 alpha -substituted estratrienes of general formula (I) - wherein R3, R7, R7', R13, R16, R17 and R17' have the designations cited in the description, and R9 represents a linear-chain or branched-chain, opt...
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JP4611019B2 |
This invention relates to novel compounds that are liver selective glucocorticoid receptor antagonists, to methods of preparing such compounds, and to methods for using such compounds in the regulation of metabolism, especially lowering ...
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JP4601297B2 |
Sterol derivatives (I) are new. Sterol derivatives of formula (I) are new. T1, T2 = H or Me, Me being in alpha- or beta-configuration; T4 = H, Me or Et; T3 = H or beta-Me; dotted line = optional additional 5(6) or 6(7) bond; Z = H or OH ...
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JP2010538072A |
This application is directed to the use of steroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.
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JP4586190B2 |
To provide a compound having photoresponsive gelatinizing effect, and to provide a method for easily producing the gelatinizer. The azobenzene compound is provided, being represented by the formula (wherein, m is an integer of 1-7; n is ...
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JP4545929B2 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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JP4545930B2 |
The invention is directed to 17 beta -nitro-11 beta -arylsteroids of formula I: wherein R1, R6, R7, R12 and X are as defined by the specification. The compounds exhibit potent antiprogestational activity and are useful in the treatment o...
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JP4541166B2 |
Methods and compositions for interacting with the GABAA receptor complex to induce sleep in humans using certain 5 3 alpha -hydroxy-5-reduced steroid derivatives.
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JP2010529152A |
The 17beta-cyano-18a-homo-19-nor-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NN...
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