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JP2016029083A |
To provide compositions and methods for non-toxic delivery of antiprogestins.The invention provides a compound represented by the formula (I), and a pharmaceutical composition that comprises the compound in a therapeutically effective am...
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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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JP5795312B2 |
17-Hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives (I) are new. 17-Hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of formula (I) and their stereoisomers, salts, solvate or solvate of the salts, incl...
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JP2015178522A |
To provide production of very potent competitive progesterone receptor antagonists available.Compounds of Formula (I): wherein Ris a residue Y or a phenyl ring once or twice substituted with the residue Y; Y is selected from SRetc.; Ris ...
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JP5781070B2 |
The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-benzylidene derivatives of the formula I, in which Y and X are each as defined in the claims and the description, to a process for preparation thereof and to t...
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JP5745517B2 |
Applicants have discovered a method for the stereoselective and regioselective synthesis of 3α-hydroxy, 3β-methyl-5α-pregnan-20-one (ganaxolone) comprising reacting 5α-pregnane-3,20-dione; with an organometallic methylating agent in ...
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JP5731499B2 |
The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-aryl derivatives of the formula I with progesterone-antagonizing action and to processes for preparation thereof, to use thereof for treatment and/or prophylax...
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JP5731498B2 |
The invention relates to 17-hydroxy-17-pentafluoroethylestra-4,9(10)-diene 11-ethynylphenyl derivatives of the formula I, in which R1 and X are each as defined in the claims and the description, and to a process for preparation thereof a...
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JP2015042686A |
To provide a solid preparation.The present invention provides and describes 17α-ethynyl-androst-5-ene-3β,7β,17β-triol in a solid state form including amorphous and crystalline forms and a specific polymorphic form thereof. Anhydrides...
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JP5657052B2 |
Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treat...
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JP2014528485A |
The 3,3-disubstituted 19-nor-steroid compounds according to formulas (I) and (III) are provided herein: R1, R2, R3, R3', R4, R6a, R6a in the formulas. , R11a and R11b are as defined herein. The compounds of the present invention are inte...
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JP5419750B2 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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JP5417562B2 |
The invention provides 17-alpha-substituted-11-beta-substituted-4-aryl and 21-substituted 19-norpregnadienediones as antiprogestational agents.
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JP5386362B2 |
Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treat...
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JP2013173781A |
To provide a steroid compound suitable for treatment of CNS disorders, and a method for production thereof.There is provided a compound of formula I having unsaturation between C4 and C5 or C5 and C6, its pharmaceutically acceptable salt...
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JP5250174B2 |
The invention relates to a process for the preparation of 7α-methyl hydroxy steroids of the formula I wherein R1 is hydrogen, methyl or C≡CH; R2 is (CH2)nOH, wherein n is 0, 1 or 2; by a copper mediated 1,6-conjugate addition of a Gri...
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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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JP5230449B2 |
The present invention is directed to novel 11-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.
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JP2013514338A |
The present invention relates to a compound of formula (I) for its use for reversing or inhibiting multidrug resistance.
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JP2013010773A |
To provide a prodrug including an NO-releasing prodrug a double prodrug, and mutual prodrug, in which bio-cleavable linker and a remedy are linked covalently.There is provided a compound of formula (I) or a pharmaceutically acceptable sa...
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JP5113832B2 |
A process for the enantioselective reduction of compounds having a steroid structure (ABCD) including one or several heteroatoms, one or several double bonds and/or aromatic components in the ring structure and having at least one oxo gr...
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JP5061061B2 |
The invention provides an improved process for the preparation of 17-esters of 9 alpha ,21-dihalo-pregnane-11 beta ,17 alpha -diol-20-ones, and in particular for the preparation of 17-esters of anti-inflammatory steroids according to the...
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JP5055501B2 |
The subject invention provides an X-ray visible drug delivery device for subdermal administration of a contraceptive or hormone replacement therapy.
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JP5043250B2 |
This invention relates to novel inhibitors of androgen synthesis that are useful in the treatment of prostate cancer and benign prostatic hypertrophy. The present invention also provides methods of synthesizing these novel compounds, pha...
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JP2012149076A |
To provide a process for the preparation of 17-esters of 9 α,21-dihalo-pregnane-11β,17α-diol-20-ones.The process for the preparation of related 17-esters, represented by the following formula, includes reacting 17α-hydroxy of 9α,21-...
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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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JP2012102135A |
To provide a process for producing a mixture of nanometer particles of a poorly water-soluble or water-insoluble compound with a spray-dried carrier excipient, wherein the mixture lies in the form of freely fluidizable powder, and also, ...
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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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JP4886145B2 |
A stable anaesthetic composition is described which is particularly suitable for use in cats and dogs. The composition comprises an aqueous solution of an anaesthetically effective amount of water soluble cyclodextrin or a cyclodextrin d...
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JP2011529933A |
The invention relates to compounds of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof The compounds are useful for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-relate...
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JP2011225629A |
To provide a method of treating a subject with a traumatic central nervous system injury, more particularly, a traumatic brain injury.The method includes a therapy comprising a constant or a two-level dosing regime of progesterone. In on...
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JP2011527986A |
Described herein are solid state 17α-ethynylandrost-5-ene-3β,7β,17β-triol including amorphous and crystalline forms and specific polymorphic forms thereof, and use of solid state 17α-ethynylandrost-5-ene-3β,7β,17β-triol in treati...
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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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JP4716726B2 |
The subject invention provides new progestogen esters and uses thereof.
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JP4712689B2 |
A process for the sterilization of water insoluble solid medicinal substances is described. The process provides the sterilization of drug substances, which are suitable for pulmonary administration. In particular, the process is used in...
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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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JP4598953B2 |
Compounds of formula (I)in which the radicals are as defined in the specification and claims, and physiologically tolerated and physiologically functional derivatives thereof and processes for their preparation are described. The compoun...
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JP4592955B2 |
The present invention is a method of milling materials to form a fine powder with a median particle size below 10 micrometer which is suitable for inhalation and which has substantially no amorphous content generated during milling. The ...
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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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JP2010522732A |
Compounds of the formula (I) are provided having a steroid skeleton and substitution characteristics in the A and B rings of the steroid skeleton effective for mineralocorticoid receptor antagonism, and rings C and D of the steroid skele...
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JP2010516686A |
Compositions with improved stability comprising a pharmaceutically acceptable salt of 11-(4-aminophenyl)-19-nofregna-4,9(10)-diene- 3,20-dione derivatives are provided
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JP2010515777A |
The present invention provides a purification method for air sensitive steroids, by reacting an amino acid or an analogue thereof with the 21-aldehyde oxidation product of such air sensitive steroids to form an adduct that is separated f...
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JP4458853B2 |
A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough:
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JP2010090132A |
To provide a method for producing nanoparticles of a poorly water-soluble or substantially water-insoluble compound applicable for pharmaceuticals, foods, and cosmetics.The nanometer-size particles of a poorly water-soluble or substantia...
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JP2010511729A |
The present invention comprises a composition and method treating eye diseases using a composition having a therapeutically effective amount of a progestagen and a pharmaceutically acceptable carrier, wherein the composition is applied t...
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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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JP2010077081A |
To provide a medicine for treatment of circadian rhythm disorder.The biological clock period elongation agent contains progesterone or its derivative, and the medicine for the treatment of circadian rhythm disorder contains the elongatio...
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JP2010077158A |
To provide a new pharmaceutical composition containing antiprogestin.The method and use for preventing or treating hormone-dependent disease, in particular breast cancer, in a mammal by the antiprogestin, in particular antiprogestin 11-(...
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JP2010507685A |
The subject matter of the instant invention is pertinent to the field of hormone therapy. More specifically, the subject matter of the instant invention concerns methods of treating estrogen-dependent conditions such as endometrial hyper...
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JP2010506867A |
The use of estradiol valerate (I) or 17beta -estradiol (I') in combination with 17alpha -cyanomethyl-17beta -hydroxy-estra-4,9-dien-3-one (dienogest) (II) is claimed in the production of a single- or multiphase combination preparation fo...
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