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JP4184986B2 |
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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JP4176831B2 |
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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JP4145350B2 |
The invention relates to a 3 alpha -hydroxy, 17-(un)substituted derivatives of the androstane series and 3 alpha -hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at the recently identif...
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JP4116080B2 |
This invention describes the new 7alpha-(5-methylaminopentyl)-estratrienes of general formula Iin whichR2 stands for a hydrogen or fluorine atom,R17 stands for a hydrogen atom, a methyl or ethinyl group,n stands for 2, 3 or 4, andx stand...
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JP4104164B2 |
Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum...
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JP4094662B2 |
Sialic acid derivatives represented by the following general formula: wherein R<1> represents a residue of a steroid compound excluding cholestane and cholestene residues, R<2> represents hydrogen or methyl group, R<3> represents a C1-C6...
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JP2008120839A |
To provide a compound useful for treating mammalian diseases characterized by undesired cell mitosis.A new estradiol derivative binds to tubulin, inhibits microtubule formation or exhibits anti-mitotic properties.
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JP2008120840A |
To provide a compound useful for treating mammalian diseases characterized by undesired cell mitosis.A new estradiol derivative binds to tubulin, inhibits microtubule formation or exhibits anti-mitotic properties.
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JP2008081432A |
To provide a new cholesterol derivative which is low in toxicity to living bodies, has a high inclusion rate, high solubility in supercritical carbon dioxide, is excellent in imaging of systemic blood vessels and livers, is also excellen...
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JP4066272B2 |
Methods, compositions and compounds for modulating the GABAA receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.
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JP4065399B2 |
Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals
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JP4061293B2 |
PCT No. PCT/US94/10655 Sec. 371 Date Mar. 20, 1996 Sec. 102(e) Date Mar. 20, 1996 PCT Filed Sep. 20, 1994 PCT Pub. No. WO95/08529 PCT Pub. Date Mar. 30, 1995Chiral surfactants, methods for their synthesis and use, and apparatus designed ...
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JP2008013501A |
To provide a novel diamine compound comprising a steroid skeleton.The diamine compound is represented by formula (I), wherein R represents an organic group comprising a steroid skeleton and R1 represents a divalent organic group comprisi...
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JP2008500368A |
Compounds, compositions and methods for treating degenerative diseases and disorders are disclosed, the compounds having the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherei...
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JP2007538025A |
The invention relates to estradiol prodrugs of general formula (I), in which the group Z is bonded to the steroid. The invention further relates to methods for production thereof, pharamceutical compositions comprising said compounds and...
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JP2007538026A |
The invention relates to steroid prodrugs with androgenic effect of general formula (I), in which the group Z is bonded to the steroid, pharmaceutical compositions comprising said compounds and the use thereof for the production of medic...
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JP2007538027A |
The invention relates to estriol and estetrol prodrugs of general formula (I), in which group Y is bonded to the steroid, the method for production thereof, pharmaceutical compositions comprising said compounds and the use thereof for pr...
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JP2007537131A |
Pharmaceutical compositions for and methods of preventing infection or treating an individual who has been identified as being infected with a Flavivirus, Pestivirus, picornovirus or coronavirus such as HCV, GB virus B, JEV, WNV, CSFV, B...
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JP4023820B2 |
The invention concerns pharmaceutical preparations containing estra-1,3,5(10)-triene derivatives as active ingredients which carry a group of the general formulaat their C3 position whereinR is a R<1>R<2>N group whereinR<1 >and R<2 >are ...
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JP2007314577A |
To provide specific inhibitors of sodium/proton exchanger (NHE), and to provide NHE inhibitors for various therapeutic uses. New isolated or synthesized aminosterol compounds such as compound FX1A, compound FX1B, compound 1360, compound ...
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JP2007532688A |
The invention relates to 17alpha-fluorosteroids of general formula (I), where R<1> = H or CH3, R<2> and R<3> = H, Cl or CH3 and a single- or double-bond is arranged between carbon atoms 6 and 7 and between 9 and 10 and pharmaceutical com...
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JP4008024B2 |
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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JP2007291127A |
To provide nonsteroidal antiinflammatory drugs preventing, reducing toxicities such as gastrointestinal lesions. Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) ...
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JP4002438B2 |
The present invention concerns with steroid compounds of formula (I) wherein R<1> is cyclyhexyl or cycloheptyl, R<2> is hydrogen or C1-C6 alkyl, R<3> is hydrogen, C1-C6 alkyl or methylol, R<4> is hydrogen or hydroxymethylene and a pharma...
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JP2007269808A |
To provide a therapeutic protein, polypeptide (e.g. interferon and intron A) or gene delivery system to an epithelial cell, especially urothelial cell, or a method for improving the delivery of a nucleic acid. A protein or a nucleic acid...
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JP3993228B2 |
The invention presents 17 beta -nitro and 11 beta , 17 beta -dinitro esters of estradiol which are made from 3-acyloxy-17-keto- or 3,17-dihydroxy-1,3,5-estratrienes by processes known in the art. The compounds exhibit estrogenic activity.
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JP2007528358A |
The treatment and/or prevention of depression by the co-administration of an estrogen with the progestin dienogest for HRT and/or contraception.
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JP2007262081A |
To provide a compound which can enhance the amount of a medicine delivered to cells or cell populations, and to provide a method therefor. This compound is represented by formula I [R1and R2are each independently H or OH; (m) and (n) are...
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JP2007254476A |
To provide a new non-estrogenic derivative of estradiol which have no estrogenic activity and an anti-oxidative activity. The invention relates to the non-estrogenic estradiol derivatives with antioxidative activity, for example, such as...
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JP3984315B2 |
The invention relates to a method of the preparation of a steroid derivative ketal according to the general formula I: wherein R1 is CH3 or C2H5; R2 is OH; R3 is H, CH3; C IDENTICAL CH, CH2Hal,, or CH2CN; or R2 and R3 together are O; R4 ...
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JP3983796B2 |
This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3 alpha -hydroxy,3 beta -substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereosele...
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JP2007238624A |
To provide an anti-cancer phosphonate analogue, relating to compounds having anti-cancer activity. By a method and a composition which make cells accumulate or hold a biologically active medicine in them, cell targeting can be done. The ...
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JP3977462B2 |
The invention relates to a 11-(substituted phenyl)-estra-4,9-diene derivative of formula I wherein A is a residue of a 5- or 6-membered ring containing 2 heteroatoms which are not connected to each other and independently selected from O...
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JP3968114B2 |
To provide a new steroid compound useful as an anti-estrogenic agent. The compound has a structure of formula (III). The invention further relates to a pharmaceutical composition containing the compound or its pharmaceutically permissibl...
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JP2007210994A |
To obtain a steroid compound of a kind having an anti-progestin effect and a pharmaceutical value, to provide a method for preparing the steroid compound, to obtain a pharmaceutical composition for treating diseases associated with proge...
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JP2007523876A |
This invention relates to the improved methods of use of Argatroban in heparin-induced thombocytopenia.
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JP2007210888A |
To provide a new method for producing a steroid compound. The present invention provides a method for producing 5β-3,7-dioxocholanic acid or its ester derivative by passing through the following four steps (I) to (IV) by using cholesta-...
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JP2007210973A |
To provide a compound which is excellent in solubility and the like, and is suitable for producing lesion-selective liposome contrast media, and to provide a chelate compound comprising the compound and a metal ion. A compound represente...
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JP2007522211A |
The present invention relates to novel compounds which are 7alpha-substituted 17-alkylene-16alpha-hydroxy steroidal estrogens. This invention specifically relates to estrogen derivatives which contain 7alpha-substituents and which exhibi...
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JP3950489B2 |
PURPOSE: To obtain the subject compound used for betamethasone source material, etc., by dehydrating a 17α-hydroxy-17β-cyanoandrosta-diene-3-one to an novel intermediate, bringing a CN group to a methyl ketone and methylating after epo...
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JP2007520455A |
The present invention provides an ecdysteroid derivative in which a fluorescent moiety is attached to an ecdysteroid moiety by derivatisation of a hydroxyl group on the alkyl side chain of the ecdysteroid moiety. The derivative is capabl...
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JP2007517878A |
The present invention is a di-steroidal prodrug of ethinyl estradiol according to formula I:
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JP2007516946A |
The invention relates to a process for the synthesis of high purity d-(17alpha)-13-ethyl-17hydroxy-18,19-dinorpregn-4-ene-20-y
ne-3-one-oxime (further on norelgestromine) via acetylation of d-norgestrel at position 17, oximation of the...
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JP2007512344A |
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for t...
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JP3913475B2 |
Sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using...
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JP3908162B2 |
A compound of general formula (I): wherein, for example, X<1> and X<2> independently represent a hydrogen atom, R represents a hydrogen atom or a protecting group for a hydroxyl group, R and R form an optionally protected -(C=O)- togethe...
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JP2007509050A |
The invention relates to novel crystalline forms of 3-beta-amino 17-methylene androstane-6-alpha 7-beta-diol hydrochloride, referred to as form A, form B and form C, a method for preparing same, the use thereof as a drug, and pharmaceuti...
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JP3902255B2 |
To provide the subject new compound having excellent antiinflammatory action and low systemic side actions and useful e.g. for an extremely strong local antiinflammatory agent by reacting deoxymethasone, etc., with an activated aromatic ...
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JP3899136B2 |
To obtain the subject new steroid compound, a specific 17-(3-imino-2- alkylpropenyl)-5β,14β-androstane derivative, active on the cardiovascular system and usable in the treatment of cardiovascular disorders such as heart failure and hy...
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JP2007506805A |
Processes useful in the preparation of pharmaceutical compounds such as fulvestrant and processes for the preparation of fulvestrant.
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