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JP2007530652A |
The present invention relates to the preparation of a β2 adrenergic agonist in crystalline salt form. In particular the invention relates to preparation of a crystalline salt of compound (I) in particular a crystalline monohydrochloride...
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JP2007269815A |
To provide a compound useful as an agonist for FXR (Farsnesoid X receptor), a preparation containing such the compound, and use thereof on the therapy. The compound useful as the agonist to the FXR is a compound of formula (I) (wherein, ...
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JP3987105B2 |
The present invention relates to certain sterol derivatives for use as medicaments.
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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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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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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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JP2007522087A |
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a...
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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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JP2007500140A |
The present invention relates to thiomorpholino steroid compounds of general formula I, which may advantageously be employed to stimulate meiosis in human oocytes, the steroid being specifically characterized by a thiomorpholino moiety b...
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JP2006528207A |
Compounds and methods for modulating mesenchymal cell function, for instance smooth muscle and fibroblast proliferation or cytokine expression, and for treating conditions associated with mesenchymal cell function, for instance airway hy...
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JP2006306896A |
To provide a novel compound having an antiestrogenic action.The novel compound is 17α-alkyl-17β-oxy-estra-1,3,5(10)-triene which is represented by formula I and has an antiestrogenic action. The 17α-alkyl-17β-oxy-estratriene is used ...
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JP3844358B2 |
Novel acridinium esters that are useful, either alone or when incorporated into liposomes, as chemiluminescent agents in binding assays (e.g., immunoassays and gene probe assays) with improved sensitivity are disclosed. In addition, the ...
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JP2006524664A |
The present invention relates to the chemical synthesis of solanum glycosides, in particular to the synthesis of solasonine as well as to novel beta-monosaccharide intermediate compounds, of Formula (2), where R1 is a benzylidene, 4-nitr...
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JP2006522028A |
A method for the conversion of steroidal 17beta-carboxylic acids to c carbothioic acid and esters thereof such as fluticasone propionate.
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JP3814312B2 |
PURPOSE: To obtain the subject new derivative having anti-glucocorticoid activity and usable in treating or preventing glucocorticoid-dependent diseases such as diabetes, hypertension and arteriosclerosis. CONSTITUTION: This new 11,12-bi...
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JP3814292B2 |
3-Sulphamoyloxy-oestra-1,3,5(10)-triene derivs. of formula (I) are new. R = NR1R2; R1, R2 = H or 1-5C alkyl; or NR1R2 = 4-6C polymethyleneimino or morpholino; R3 = H or 1-5C alkyl; R4 = H, opt. esterified OH, 1-5C haloalkyl or 1-5C alkox...
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JP3805406B2 |
PURPOSE: To obtain the subject new derivatives useful as e.g. active ingredients of medicines for the treatment of cardiovascular disorders such as heart failure and hypertension. CONSTITUTION: This new compound is a 17-substituted hydra...
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JP3798064B2 |
To obtain the subject new derivative consisting of a specific digoxigenin derivative containing carbodiimide group, useful as a determination label for nucleic acid detection method or immunoassay to enable highly sensitive analysis by a...
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JP3796405B2 |
Thiol esters of S-substituted 11beta-benzaldoxime-estra-4,9-dien-carboxylic acids of the formula Itheir pharmaceutically acceptable salts, a method for their synthesis and pharmaceutical preparations containing these compounds are descri...
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JP3789465B1 |
There is provided with a method for manufacturing an isoxazole derivative at a high yield and without discharging waste products, and a novel isoxazole derivative. An isoxazole derivative expressed by Formula (8) is produced by reacting ...
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JP2006151994A |
To provide a simple method for converting a pregnane-3,20-dione compound into a 3α-hydroxy-3β-substituted-pregnane.An unprotected dione is chemoselectively and stereoselelctively converted into a 3(R)-pregnane-3-spiro-2'-oxiran-20-one ...
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JP3780007B2 |
PURPOSE: To obtain a corticosteroid 17-alkyl carbonate 21-[0]-carboxylic acid carbonic ester which has a very strong local and topical anti-inflammatory action and is effctive in treating inflammatory dermatosis by reacting a specific al...
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JP2006508984A |
A method and compositions for treating persistent pulmonary hypertension in human newborns that deploys an intravenous infusion of a modified drug formed by adding one or more of a predetermined chemical arrangement to an efficacious par...
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JP2006508985A |
A method for modifying at least one non-ester-containing parent compound, and the compounds produced using such method, which compounds are deployed to temporarily incapacitate at least one subject are disclosed. The modified compounds a...
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JP2006508962A |
This invention relates to processes for the preparation of novel 7-carboxy substituted steroid compounds of Formula I,
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JP2006501207A |
Polymorphic crystal forms of 3-methylthiophene-2-carboxylic acid (6S,9R,10S,11S,13S,16R, 17R)-9-chloro-6-fluoro-11-hydroxy-17-methoxycarbonyl-10,13,1
6-trimethyl-3-oxo-6,7,8,9,10, 11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanth...
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JP3727332B2 |
Methods of treatment for osteoporosis in a human or other animal subject, comprising: administering a bone-active phosphonate to said subject, at a level of at least about 0.1 LED per day of said treatment; and administering an estrogen ...
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JP3722835B2 |
A method of preparing a 3 beta -hydroxy- or 3 beta -(lower acyloxy) 16,17-ene-17-(3-pyridyl)-substituted steroid, wherein the 3 beta -(lower acyloxy) group of the steroid has from 2 to 4 carbon atoms, which comprises subjecting a 3 beta ...
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JP3710470B2 |
Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid recept...
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JP3678454B2 |
PURPOSE: To provide the subject pharmaceutical composition containing an aromatic steroid substituted in the 3-position with a disubstituted aminoalkyloxy chain, which has controlling activities of fecundity, particularly male fecundity ...
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JP2005516070A |
Nitrooxy derivatives of steroidal compounds of general formula B-X1-NO2 (I) or esters or salts thereof, wherein: B is a steroidal radical, X1 is a bivalent linking group comprising an aromatic or heterocyclic ring.
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JP2005513039A |
17alpha -Alkyl-11beta -halo-17beta -oxy-estratriene derivatives (I), having a 7alpha -side-chain, are new. 17alpha -Alkyl-11beta -halo-17beta -oxy-estratriene derivatives of formula (I), their acid addition salts and esters are new. [Ima...
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JP2005507885A |
The invention concerns a ligand comprising (I) wherein n is an integer from 1 to 5 Y is CO2H or PO3H2T represents -X or -phenyl-X, wherein X represents NO2, NH2, NCS, NHCOCH2-Z, NHCO-W-COCNHS, -NH-Q, -NHCS-Q, -NHCOCH2-Q, or NHCO(CH2)m-Q ...
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JP2005507886A |
Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating a function of the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of ...
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JP3621132B2 |
The compounds of formula (I): in which, R17 and R'17 are such that: - either R17 and R'17 together form a ketone - or R17 represents a hydroxyl radical or an acyloxy radical and R'17 represents a hydrogen atom or an alkyl, alkenyl or alk...
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JP2005500290A |
There are provided compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents a 4-7 membered non-aromatic ring containing 1-3 heteroatoms selected from O, N and S optionally substituted with one or more me...
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JP2004538447A |
A hapten-linker-large group conjugate for use in a rapid assay, wherein the assay is kinetic-based not approaching equilibrium, the hapten-linker-large group conjugate being of the general formula: X-W-Y-Z wherein: X is a hapten; W is an...
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JP2004537563A |
This invention generally pertains to the field of psychiatry. In particular, this invention pertains to the discovery that agents capable of inhibiting the binding of cortisol to its receptors can be used in methods for preventing antips...
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JP2004534011A |
The present invention relates to steroid compounds of general formula I, which may advantageously be employed to stimulate meiosis in human oocytes, the steroid being specifically characterized by amino nitrogen bonded to C<17> of the st...
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JP3585583B2 |
To provide the subject new compound that is hybridized with RNA or the like, is resistant to nuclease, contains riboside, the base moiety and modified deoxyfuranosiyl component, can modulate the production of selected protein and is usef...
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JP3581821B2 |
The present invention provides a pharmaceutical composition comprising a compound admixed with a pharmaceutically acceptable diluent or carrier; wherein the compound has the the formula wherein each of R1 and R2 is independently selected...
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JP3581802B2 |
The present invention provides a pharmaceutical composition comprising a compound admixed with a pharmaceutically acceptable diluent or carrier; wherein the compound has the the formula wherein each of R1 and R2 is independently selected...
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JP3581820B2 |
The present invention provides a pharmaceutical composition comprising a compound admixed with a pharmaceutically acceptable diluent or carrier; wherein the compound has the the formula wherein each of R1 and R2 is independently selected...
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JP3572724B2 |
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JP3549125B2 |
Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic esters 21-carbonic esters of the formula I with A equal to CHOH and CHClm CH2, C=0, 9(11) double bond; Y equal to H, F, Cl; Z equal to H, F, methyl, R(1) equal to aryl, heta...
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JP3546886B2 |
PCT No. PCT/US94/02397 Sec. 371 Date Aug. 18, 1994 Sec. 102(e) Date Aug. 18, 1994 PCT Filed Mar. 16, 1994 PCT Pub. No. WO94/20520 PCT Pub. Date Sep. 15, 1994Compounds having a broad range of antimicrobial activity generally have a struct...
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JP2004521917A |
Amphoteric sterol derivatives, and liposomes containing these derivatives are new. The amphoteric sterol derivatives have an isoelectric point of 4.5-8.5 and are compounds of formula (I): Amphoter-Y-spacer-X-sterol (I) X and Y : linking ...
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JP3545477B2 |
PURPOSE: To provide the subject novel derivatives, that is, specific 17- iminomethylalkenyl- and 17-iminoalkyl-14β-hydroxy-5β-androstane derivatives useful for the treatment or the like of cardiovascular diseases such as heart failure,...
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JP3535519B2 |
This invention presents novel purine-based compounds for inclusion into oligonucleotides. The compounds of the invention, when incorporated into oligonucleotides are especially useful as "antisense" agents-agents that are capable of spec...
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