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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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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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JP3986313B2 |
This invention discloses a novel method for the conversion of carboxylic acids to carbothioic acids and application of the method to the preparation of androstane carbothiolates, such as fluticasone propionate, which avoids column chroma...
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JP2007523876A |
This invention relates to the improved methods of use of Argatroban in heparin-induced thombocytopenia.
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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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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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JP2007508265A |
This invention relates to a method for preventing or delaying the progression of hormone receptor positive of hormone receptor unknown breast cancer in a patient by following estrogen antagonist therapy by subsequent therapy with an estr...
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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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JP2007506675A |
Fusidic acid derivatives substituted at C-24 may be used in therapy for the treatment of infections.
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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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JP2007063296A |
To provide a medicinal composition useful for treating human prostatic adenocarcinoma.The medicinal composition for treating human prostatic adenocarcinoma comprises a 5-α-reductase inhibiting compound of 17β-(N-t-butylcarboxamide)-5-Î...
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JP3889456B2 |
PURPOSE: To obtain an inhibitor containing a specific active ingredilent, high in safety, having high glycerophosphoric acid dehydrogenase inhibitory activity, capable of its ready formulation in foods, and useful for preventing or treat...
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JP2006526025A |
Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering compounds of the general formula: wherein the variables are defined in the specification.
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JP3844977B2 |
To provide a method for manufacturing squalamine from desmosterol. The 3-keto-7,24(R)-diol derivative of desmosterol is produced via the synthesis of the acetyl derivative of desmosterol, the synthesis of the 24(R),25-diol derivative of ...
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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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JP2006517947A |
The invention relates to the use of compounds of a general formula (I), wherein R2, R14 to R17 and X groups have the following significance: R2 is C1-C5-Alkyl, C1-C5-Alkoxy or a -O-CNFmHo rest, wherein n=1,2,3,4,5 or 6, m>1 and m+o=2n+1,...
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JP2006176427A |
To provide an estrone 3-sulfate transporter activity inhibitor or breast cancer cell proliferation inhibitor or breast cancer curative, with no need of being taken in cells, good in drug delivery tendency and extremely slight in side eff...
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JP3786855B2 |
To obtain a new compound capable of inhibiting the steroid sulfatase activity in vitro and in vivo, a pharmaceutical composition effective in treatment of estrogen-dependent tumors and a pharmaceutical composition effective in treatment ...
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JP2006515581A |
Process for the preparation of polyhalogenated steroids, in particular of androstanic fluoro derivatives corticosteroids by means of the formation of new androstanic S-hydroxy alkyl or aralkyl-17-carbothioate intermediates.
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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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JP3778372B2 |
PURPOSE: To obtain a new compound useful as a therapeutic agent for geriatric dementia, etc., including Alzheimer's disease, due to its activity of activating ChAT in cholinergic neurocytes. CONSTITUTION: A compound of formula I [R1 is a...
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JP3759639B2 |
PURPOSE: To obtain a new 22-thiavitamin D3 derivative having strong suppressive activity against keratinocyte growth. CONSTITUTION: This is a compound of formula I (R1 is a 1-10C alkyl optionally substituted with ≥1 OH; R2 and R3 are e...
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JP2006502172A |
There is provided a crystalline chemical composition comprising a compound of formula (I) in which the crystal lattice is stabilised by the presence of a guest molecule, characterised in the crystalline composition is of space group P212...
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JP2005537278A |
There is provided a crystalline chemical composition comprising a compound of formula (I)in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in the crystalline composition is of space group P2121...
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JP2005537296A |
The invention relates to inhalation compositions derived from dehydroepiandrosterone sulfate. The compositions of the invention involve liquid nebulizer formulations prepared from dehydroepiandrosterone sulfate dihydrate. The composition...
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JP3725158B2 |
A method of treating asthma in a subject in need of such treatment is disclosed. The method comprises administering to the subject dehydroepiandrosterone, analogs thereof, or pharmaceutically acceptable salts thereof in an amount effecti...
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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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JP3715645B2 |
This invention presents alkali metal salts of 8,9 dehydroestrone, salts of its sulfate ester, and stable compositions thereof, as well as processes for their production and use in estrogen replacement therapy and cardiovascular protection.
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JP3713237B2 |
The invention relates to a novel sustained release pharmaceutical formulation adapted for administration by injection containing the compound 7±-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,
3,5(10)-triene-3,17²-diol, more p...
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JP2005306880A |
To obtain a prophylactic drug for treatment of asthma or bronchoconstriction in a patient necessitating treatment for adenosine depletion.This invention relates to the prophylactic drug for treatment of asthma or bronchoconstriction of h...
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JPWO2004000795A1 |
(In the formula, R1, R2, R3, R4 and R5 are the same or different and represent hydrogen atoms, substituted or unsubstituted lower alkyls, substituted or unsubstituted lower alkoxys and the like, and R17 represents trifluoromethyl and the...
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JP2005530820A |
The invention relates to inhalation compositions derived from dehydroepiandrosterone sulfate. The compositions of the invention involve liquid nebulizer formulations prepared from dehydroepiandrosterone sulfate dihydrate. The composition...
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JP2005527496A |
According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), or a solvate thereof, together with a long-acting ² 2 -adrenoreceptor agonis...
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JP2005524680A |
The process for the preparation of 6alpha-fluoro steroids, comprising the reaction of the corresponding 6beta-fluoro steroids, or of 6alpha/6beta isomeric mixtures with an organic base having a diazo iminic group, in a suitably selected ...
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JP2005522442A |
A compound of formula (I) in the form of a substantially amorphous solid, and processes for the production thereof.
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JP2005521680A |
A process for preparing a compound of formula (II) or a salt thereof is described.
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JP2005517019A |
A process for preparing fluticasone propionate as crystalline polymorphic Form 1 which comprises reacting a compound of formula (II) or a salt thereof with a compound of formula LCH2F wherein L represents leaving group optionally in the ...
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JP2005515222A |
A process of producing a stable composition comprising a mixture of sulfated estrogens. The mixture of sulfated estrogens may comprise sulfated alkali metal salts of Delta8,9-dehydroestrone, estrone, and derivatives thereof or other estr...
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JP2005508281A |
A compound of formula (1): wherein each of R1, R2, R4, R4', R7, R11, R12, R15, R16, R17, and R17', independently, is hydrogen, hydroxy, amino, carboxyl, oxo, halo, sulfonic acid, -O-sulfonic acid, or alkyl that is optionally inserted wit...
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JP2005075763A |
To obtain a drug for animals containing cholic acid and/or scymnol, which exhibits remarkable effects on a growth rate, body weight gain, or the like, of animals, particularly domestic animals.This drug for animals contains the cholic ac...
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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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JP2005501849A |
The invention relates to the use of 2-alkoxyestrogen sulfamates of general formula (I) for producing a medicament for the treatment of tumorous diseases, which are positively influenced by the inhibition of tubulin polymerisation. In sai...
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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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JP2004534042A |
Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding alpha,beta-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the alpha,beta-unsaturated ketone structure...
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JP3583776B2 |
Phosphate esters of formula: for use in the inhibition of steroid sulfatase enzyme, wherein R is as defined in the specification and the -O-polycycle represents a residue of a sterol.
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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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