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JP2018519246A |
The present invention relates to a cholic acid derivative, a method for producing the same, and a pharmaceutical use. Specifically, the present invention relates to a cholic acid derivative having the structure of formula (I), a stereois...
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JP2018517666A |
Ursodeoxycholic acid, or eicosapentaenoic acid, or docosahexaenoic acid, or rain, or R- (+)-α-lipoic acid, or ursoleic acid, or corosolic acid, or hydroxycitrate, or silicic acid, or cholic acid. Or oleanolic acid, or salicylic acid, or...
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JP2018505206A |
The present invention belongs to the field of medicinal chemistry, and specifically relates to a crystal form of avilateron propionate and a method for producing the same. The crystal form of the avilateron propionate has 2θ values of 5...
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JP2018505190A |
The present invention provides compounds represented by formula I, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating or preventing diseases or disorders mediated by FXR and / or TGR...
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JP6254195B2 |
The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or...
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JP6239091B2 |
Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I):and pharmaceutical compositions thereof for inducing sedation. Such compounds are contemplated useful for the prevention and treatment of a variety...
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JP2017533923A |
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing these compounds and methods of using these compounds to treat TGR5-mediated diseases or condi...
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JP6196302B2 |
The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of dise...
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JP6186125B2 |
Saxitoxin analogue compounds, compositions, pharmaceutical compositions, methods of synthesis of saxitoxin analogues, methods of imaging, methods of treatment, including methods of treating pain, are provided. Saxitoxin (STX), gonyautoxi...
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JP6165843B2 |
This application is directed to the use of aminosteroid compounds for the selective inhibition of the enzyme PTP1B in a mammal for the treatment of diabetes.
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JP2017122133A |
To provide methods and pharmaceutical compositions for treating diseases involving a ceramide-mediated signaling system, e.g. diseases selected from the group consisting of Gaucher disease, Tay-Sachs disease, Sandhoff disease and Niemann...
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JP6157492B2 |
The present invention relates to a process for the preparation of sterol derivatives comprising the reaction of an α-epoxy compound with an amine in an alcohol comprising 3 to 5 carbon atoms as a solvent.
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JP6091510B2 |
The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of synthesizing abiraterone or derivatives thereof in high yield and purity by means of a key 3-forma...
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JP2017039649A |
To provide Fusarium head blight mycotoxin inhibiting agents and methods.The present invention provides Fusarium head blight mycotoxin inhibiting agents comprising at least one of a compound represented by formula (1) and pharmaceutically...
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JP2017019857A |
To provide novel compounds.Disclosed herein are novel compounds, pharmaceutical compositions comprising such compounds and related methods of their use. The compounds described herein are useful, e.g., as liposomal delivery vehicles to f...
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JP2016199587A |
To provide photochromic compounds, such as but not limited to thermally reversible photochromic compounds, that can exhibit useful photochromic and/or dichroic properties in at least one state, and that can be used in a variety of applic...
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JP6004292B2 |
The present invention addresses the problem of providing a copper catalyst which has higher catalytic activity than conventional copper catalysts, is able to be easily recovered, and can be reused repeatedly. The present invention relate...
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JP5992019B2 |
Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitate...
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JP2016527213A |
The present invention relates to the improvement in the manufacturing method of the salt which can be permitted as Avila Theron acetate ester or its medicine. Here, for the improvement, the crystallization from a solvent refines crude 3-...
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JP5956928B2 |
Described herein, in certain embodiments, are steroidal derivatives, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor ...
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JP2016521683A |
The present invention provides antibodies against metabolites in the serotonin, tryptophan, kynurenine pathway, and methods for preparing the antibodies. The prepared antibody has low cross-reactivity to related metabolites and is a usef...
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JP2016520649A |
This specification indicates how to use the pure antagonist concerned about the imidazolyl compound which acts as pure anti-progestin, gynecology indication, and a breast cancer. [Chosen drawing] Drawing 1
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JP2016117735A |
To provide arginase enzyme inhibitors for treating or diagnosing conditions characterized either by abnormally high arginase activity or abnormally low nitric oxide levels in a mammal.An inhibitor comprises a composition comprising an al...
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JP2016514165A |
The present invention provides the design and composition of a new steroid compound which cause lower part control of both the full length of an androgen receptor (AR), and splice variant . The compound concerned is a medicine which may ...
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JP2016056203A |
To provide methods and pharmaceutical compositions for treating diseases involving a ceramide-mediated signaling system, e.g. diseases selected from the group consisting of Gaucher disease, Tay-Sachs disease, Sandhoff disease and Niemann...
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JP2016510754A |
The present invention describes cyclosporin A / steroid hybrid analogs. These single drug entities are formed by binding the steroid to cyclosporin A. Upon topical administration to the eye, conjugate hybrids undergo enzymatic and / or h...
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JP2016510750A |
The present invention describes a novel single drug entity formed by the direct binding of an antibiotic to a steroid drug. Upon topical application to the eye, the conjugate undergoes enzymatic cleavage and / or hydrolysis cleavage to r...
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JP2016034946A |
To provide prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and pharmacokinetics.The present invention provides a prodrug compound represented by the formula I. The compound is an effective inhibitor ...
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JP5886873B2 |
The present invention relates to novel N-substituted azetidine derivatives
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JP5872897B2 |
The present invention relates to novel chemical compounds, in particular cholest-4-en-3-one oxime derivatives and to the use thereof as medicaments, especially as cytoprotective medicaments, in particular neuroprotective, cardioprotectiv...
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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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JP5865845B2 |
The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of the formula I with a progesterone antagonizing effect and processes for their preparation, their use for the treatment and/or prophylaxis o...
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JP2015535223A |
The present invention relates to a method for purifying crude avilateron acetate by treatment with a polymeric resin in an aqueous solvent. The purified product is extracted by simple aggregation and filtration. [Selection diagram] None
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JP2015205899A |
To provide novel medicaments which are useful as cytoprotective medicaments, in particular as neuroprotective, cardioprotective and/or hepatoprotective medicaments which can inhibit and/or treat cell death necrosis and/or pathological ap...
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JP5791810B2 |
The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of dise...
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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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JP5770235B2 |
The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.
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JP2015131844A |
To provide photochromic compounds, including, but not limited to, thermally reversible photochromic compounds, which can exhibit useful photochromic and/or dichroic properties in at least one state, and can be used in a variety of applic...
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JP2015518896A |
It has unique delivery characteristics and may have broad spectrum antiviral activity by covalent incorporation of the tocopherol moiety, or an analog of tocopherol or a selective analog of cholesterol, or its antagonist "Ezitimibe". Cha...
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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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JP2015057424A |
To provide a pain study, imaging and therapeutic method, and a composition for pain study, imaging and therapy.A saxitoxin analogue compound, a composition, a pharmaceutical composition, a synthesis method of a saxitoxin analog, an imagi...
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JP2015502384A |
The present invention is a method for obtaining avilateron and derivatives thereof such as avilateron acetate by Suzuki coupling via steroid borate of general formula (IV) or by CC coupling via steroid hydrazone of general formula (II). ...
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JP2014532077A |
The present invention relates to novel aminosteroid derivatives substituted at the 3 and / or 6 positions and relates to their use in the treatment of type 2 diabetes and insulin resistance.
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JP2014530245A |
The present invention relates to an acid addition salt of 5α-hydroxy-6β- [2- (1H-imidazol-4-yl) ethylamino] cholestane-3β-ol, its preparation and its application.
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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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JP2014521662A |
The invention is directed to novel 17β-heteroaryl substituted steroids of Formula I, pharmaceutical compositions thereof, and their use as modulators of GABAA receptors.
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JP2014518853A |
Novel compounds of Formula I:or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein m, Q, T, U, V, ring A, X, Y, R3, R4, R4a, R5a, R5b, R5c, R5d, R5e, R6a, R6b, and R6c are defined herein, are provided which are TGR5 ...
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JP5561692B2 |
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JP5539735B2 |
Described herein are compounds and methods that prevent the viral infection of cells. The compounds and methods described herein minimize viral resistance and maximize the number of targeted viruses. Additionally, the compounds and metho...
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