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JP2023040180A |
To provide new and improved neuroactive steroids that modulate brain excitability for the prevention and treatment of CNS-related conditions.The invention provides compounds represented by formula (I) and pharmaceutically acceptable salt...
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JP7241792B2 |
The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorde...
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JP2022044802A |
To provide neuroactive steroids, compositions, and uses thereof.Provided are methods of evaluating or treating a patient, e.g., a patient having a disorder described herein, comprising: a) optionally, acquiring a patient sample; and b) a...
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JP2022510683A |
As used herein, equation (I) :. [During the ceremony, R19, R5, R3a, R1a, R1b, R2a, R2b, R4a, R4b, R6a, R6b, R7a, R7b, R11a, R11b, R12a, R12b, R18, RD, And Q are as defined herein. L is selected from the group consisting of the above (whe...
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JP6873488B2 |
Provided is a method for manufacturing carboxylic acid or a salt thereof under a moderate condition and in a simple, highly-selective, high-yielding manner. Provided is a method for manufacturing a compound represented by general formula...
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JP6852118B2 |
The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorde...
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JP2021008504A |
To provide compounds and pharmaceutical compositions useful for prevention and treatment of CNS-related conditions.Compounds of a formula (I) in the figure are provided, where Z is selected from, e.g., a substituted or unsubstituted C1-C...
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JP6781148B2 |
The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.
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JP2020523357A |
Strong soft corticosteroids, pharmaceutical compositions containing them, and methods for use as anti-inflammatory agents. Also, a way to soften fluticasone propionate and similar corticosteroids to reach a powerful but safer alternative...
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JP2020062050A |
To provide neuroactive steroids, compositions, and uses thereof.Provided are methods of evaluating or treating a patient, e.g., a patient having a disorder described herein, comprising: a) optionally, acquiring a patient sample; and b) a...
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JP6453337B2 |
The present invention relates to a new stereoselective process for the synthesis of 17(α)-17-acetyl-17-hydroxy-estr-4-en-3-one of formula (I), as well as to the new intermediates of the process. The 17(α)-17-acetyl-17-hy droxy-estr-4-e...
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JP2017031161A |
To provide a novel crystallization process for preparing fluticasone propionate as crystalline form 1 polymorph having controlled particle size and being suitable for micronization.The novel crystallization process comprises the step of ...
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JP2016505038A |
The present invention is a novel compound and composition of 11β-hydroxysteroids, as well as pharmaceuticals for preventing or reversing mitochondrial damage in human or animal subjects, for treating or preventing diseases associated wi...
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JP5808830B2 |
A process for preparing crystalline particles of an active principal in the presence of ultrasonic irradiation that comprises contacting a solution of a solute in a solvent in a first flowing stream with an anti-solvent in a second flowi...
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JP2014520848A |
The invention relates to a novel crystallisation process for preparing fluticasone propionate as crystalline form 1 polymorph with controlled particle size and suitable for micronisation. Said process comprises the step of dissolving flu...
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JP5281291B2 |
The present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched alkyl group, a bicycloalkyl group, or a C5-C6 cycloalkyl which optionally may be substituted with a C1-C4 alkyl group; R2 represents hydr...
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JP5232083B2 |
The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and...
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JP2012528140A |
This invention relates to novel glucocorticoid receptor agonists of formula (I): and to processes and intermediates for their preparation. The present invention also relates to pharmaceutical compositions containing these compounds, to t...
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JP4838493B2 |
There is provided a pharmaceutical formulation comprising an aqueous suspension of particulate compound of formula (I)or a solvate thereof.
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JP4838494B2 |
A pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) a glucocorticoid of formula (I) wherein R represents a 5 membered heterocyclic aromatic ring containing 1 to 3 heteroatoms selected from O, N ...
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JP4749550B2 |
Androgenic steroids having a (14beta,17alpha-)-17-(hydroxymetheyl) configuration, useful for the preparation of male contraceptives and pharmaceutical formulations for the treatment of androgen insufficiency.
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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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JP2011121972A |
To provide fluticasone formulations which can decrease a frequency of dosing, improve clinical efficacy, and potentially reduce side effects.A fluticasone composition formulated for administration selected from the group consisting of or...
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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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JP4698773B2 |
The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and...
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JP2011093929A |
To provide a new compound which is an androstane-type glucocorticoid receptor agonist.The compound is expressed by formula (I) (in the formula, X is O or S; R1 is 1-6C alkyl, 3-8C cycloalkyl, 3-8C cycloalkylmethyl, 3-8C cycloalkenyl or t...
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JP2011507878A |
The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, or isomers of said compounds), having the general structure: wherein L, R1, R2, R3, R4, R5, and R6 are...
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JP2010280701A |
To provide a pharmaceutical formulation for administration by inhalation having a therapeutically useful effect in the treatment of inflammatory disorders of the respiratory tract.The pharmaceutical formulation containing a compound of f...
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JP4598268B2 |
The invention provides sterile glucocorticosteroids and sterile formulations containing glucocorticosteroid and use thereof in the treatment of an allergic and/or inflammatory condition of the nose or the lungs.
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JP2010529174A |
The 17β-cyano-19-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 NNHSO2R, in which...
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JP2010529153A |
The 17β-cyano-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 NNHSO2R, in w...
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JP4508651B2 |
There is provided a crystalline complex comprising a compound of formula (I) in which the crystal lattice is stabilized by the presence of a guest molecule, characterized in that the crystalline complex is of space group P212121 having u...
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JP4490689B2 |
Compounds of structural formula as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the fun...
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JP4450435B2 |
The invention relates to a method of alleviating the symptoms of PMS and anxiety. The method comprises nasally administering a steroid which is a human vomeropherin, such that the vomeropherin binds to a specific neuroepithelial receptor...
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JP2010070567A |
To provide a method for sterilizing a powdery form glucocorticosteroid, sterile glucocorticosteroid, sterile formulation containing glucocorticosteroid, and use thereof for treating an allergic and/or inflammatory condition of the nose o...
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JP4417838B2 |
Disclosed is a new synthetic pathway for the production of precursors for the production of compounds having general formula (8,10,12). During said synthesis, compounds of general formal (4,B) are produced in a microbiological reaction. ...
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JP4331478B2 |
The invention relates to a process for the production of 4-(17alpha-methyl-substituted 3-oxoestra-4,9-dien-11beta-yl)benzaldehyde-(1E or 1Z)-oximes of general formula (I), in which R1 is a hydrogen atom, a C1-6-alkyl radical or a CnF2n+1...
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JP2009515844A |
The present invention is directed to compounds of formula (I): wherein R1 represents C4-C7 branched chain alkyl, C3-C8 cycloalkyl optionally substituted by one or more groups independently selected from C1-C3 alkyl and methoxy, C4-C6 cyc...
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JP4187437B2 |
A compound having the structure: wherein n is an integer from 1-5; each of R1 and R2 independently is optionally substituted C1-C6 alkyl; each of W and X is independently hydrogen or C1-C6 alkyl; Y is O, S or NR3 where R3 is hydrogen, C1...
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JP2008526807A |
The present invention is directed to compounds of formula (I): wherein R1 represents a 1,1-dimethylethyl group or a 1,1-dimethylpropyl group and physiologically acceptable solvates thereof, physiologically functional derivatives thereof,...
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JP4095018B2 |
A process for the preparation of high purity flumethasone in high yield involves C3 protecting 9,11beta-epoxy-17alpha,21-dihydroxy-16alpha-methylpregna-1,4
-diene-3,20-dione,21-acetate, fluorinating at 6alpha, removing the C3 protecting ...
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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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JP4089181B2 |
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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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JP2007534757A |
Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficie...
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JP2007302684A |
To provide a compound for use in the treatment of an inflammatory or obstructive airway disease, a method for producing the same, and a medicament containing the same. Provided is a medicament comprising, separately or together, (A) a co...
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JP2007529426A |
Compositions and methods for treating mammalian diseases or conditions characterized by undesirable angiogenesis by administering an effective amount of a compound of the formulae: wherein Ra is selected from —OCH3, —OCH2CH3 or —CC...
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JP2007527381A |
The invention relates to a novel procedure for the production of a high yield of small crystalline particles of a narrow size distribution.
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