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JP2023162307A |
To provide lymphatic system-directing lipid prodrugs, pharmaceutical compositions thereof, and methods of producing such lipid prodrugs and pharmaceutical compositions thereof to a patient in need thereof to treat a disease, a disorder, ...
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JP2023113862A |
To provide compositions and methods for treating CNS disorders.Provided herein are compounds of Formula (II-I) in the figure and pharmaceutically acceptable salts thereof. In Formula (II-I), : t is 1, 2 or 3; n is 0, 1 or 2; R19 is subst...
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JP2023105082A |
To provide a method for treating disease.Provided herein is a deuterated compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R3a, R5, R6a, R6b, R17, R21a, R21b, Rm, Rn, R16a, R16b, R7a, R7b, R12a, R12b, R11a, R...
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JP2023071910A |
To provide pharmaceuticals that are neuroactive and suitable for use as an anesthetic.The present invention is generally directed to neuroactive 19-alkoxy-17-substituted steroids with the structure in the figure and pharmaceutically acce...
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JP2023063311A |
To develop novel lipid-pharmaceutical agent conjugates that facilitate stable transport of the pharmaceutical agent to the intestinal lymph.The present invention relates to compounds and uses thereof and particularly to compounds in the ...
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JP2023514873A |
The present application relates to novel compounds that are prodrugs of brexanolone, ganaxolone, and duranolone, pharmaceutical compositions comprising one or more of the compounds disclosed herein and salts thereof, and pharmaceutically...
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JP2023514147A |
The present invention provides lymphotropic lipid prodrugs, pharmaceutical compositions thereof, methods of producing such prodrugs and compositions, and bioavailability or other properties of therapeutic agents comprising portions of li...
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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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JP2023510741A |
G.1is a folate radical, an antifolate radical, or a folate analogue radical; L is a linker; and G2is the radical of the steroid, formula (I): G1-LG2or a pharmaceutically acceptable salt, polymorph, prodrug, solvate or clathrate thereof; ...
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JP2022130546A |
To provide novel neuroactive steroid compounds useful for treatment of central nerve-related diseases.Provided herein are 3,3-disubstituted 19-nor-steroidal compounds represented by Formula (I) in the figure. (R1 is H, Br, OH, heterocycl...
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JP2022105088A |
To provide C7, C12 and C16 substituted neuroactive steroids which have GABA receptor modulation action and are useful in preventing and/or treating CNS-related conditions, and their methods of use.The invention employs neuroactive steroi...
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JP7065825B2 |
Described herein are neuroactive steroids of Formula (I), Formula (V), or Formula (IX) or a pharmaceutically acceptable salt thereof; wherein each instance of R2, R3, R4, R5, R6, R7, R11a, R11b, R12, R16, R17, R19, and are as defined her...
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JP2022523775A |
The present invention generally relates to novel compounds for therapeutic use. In particular, the present disclosure relates to novel tetracyclic compounds useful in the treatment of cancer, especially castration-resistant prostate canc...
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JP2022515373A |
The present invention generally relates to specific pregnenolone derivatives for use in the treatment of cognitive impairment. More specifically, the present invention relates to compounds of formula (I) for use in the treatment of cogni...
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JP2022510536A |
The present invention provides bioavailability or other properties of therapeutic agents comprising a portion of a lymphatic directional lipid prodrug, a pharmaceutical composition thereof, such prodrugs and compositions, as well as a po...
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JP2022505146A |
As used herein, the compound of formula (I) or a pharmaceutically acceptable salt thereof is provided [in the formula, n, R.19, R5, R3, R6a, R6b, R2a, R2b, R4a, R4b, R7a, R7b, R11, R12a, R12b, R16, R21a, R21b, And R21cIs defined herein]....
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JP2021523938A |
The present invention contemplates novel neurosteroid derivative compounds, such as derivatives of ganaxolone and allopregnanolone, with improved solubility and bioavailability. The novel neurosteroid derivative compounds are characteriz...
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JP2021519799A |
This disclosure is GABA for use in the treatment of substance withdrawal disorders.AProvided are a receptor-modulating steroid antagonist and a method for treating the disorder and a pharmaceutical composition for use in the treatment of...
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JP6875996B2 |
Described herein are neuroactive steroids of the Formula (I):or a pharmaceutically acceptable salt thereof; wherein R1, R2, Ra, G, X, Y, Z, and n are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as ...
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JP2021512852A |
Disclosed are steroid dimers and articles formed from the steroid dimers. The steroid dimer is represented by D1-L-D2, where D1 and D2 are steroid moieties and L is a covalent linker. Articles containing steroid dimer are machined, molde...
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JP2021512909A |
The present invention relates to a steroidal derivative modulator, a method for producing the same, and an application thereof. The present invention particularly relates to a compound represented by the general formula (I), a method for...
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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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JP2021500359A |
The present invention is a crystalline form of compound (I) and a method for producing the same, a pharmaceutical composition containing the crystalline form, a pharmaceutical preparation containing a progesterone receptor modulator, and...
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JP6802256B2 |
The present invention provides a composition useful for activating GLP-1 secretion. This composition can be configured from a specific compound such as compound (1). The specific compound of such description can be obtained with good eff...
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JP6796366B2 |
The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-m...
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JP2020180161A |
To provide 19-nor neuroactive steroids and use methods thereof.The invention is based, in part, on the desire to provide novel 19-nor (i.e., C19 desmethyl) compounds, e.g., related to progesterone, deoxycorticosterone, and their metaboli...
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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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JP6745783B2 |
Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I):where R1, R2, R3, R3', R4, R6a, R6a, R11a, and R11bare as defined herein. Compounds of the present invention are contemplated useful for the preven...
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JP6653663B2 |
The present invention relates to an inorganic-organic hybrid compound as ionic compound, composed of an inorganic cation and of an organic active ingredient anion and also, optionally, of an organic fluorescent dye anion.
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JP2020500198A |
The present invention relates to a skeletal muscle hypertrophy inducer and its use in promoting skeletal muscle regeneration, preventing skeletal muscle atrophy, or treating or preventing a disease or injury that causes skeletal muscle t...
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JP2019536821A |
The present invention relates to the medical field, in particular, a water-soluble allopregnenolone (3β, 5α-tetrahydroprogesterone) derivative, a pharmaceutical composition comprising the same, and prevention or treatment of central ne...
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JP6621217B2 |
Chemical compounds and the therapeutic use thereof, in particular for improving muscular quality in mammals. More particularly, a method of improving muscular quality in sarcopenic mammals and treating and/or preventing sarcopenia using ...
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JP2019535826A |
The present disclosure provides a method of treating or preventing cardiovascular disorders and / or associated lung disorders in a subject. In certain embodiments, the method comprises a therapeutically effective amount of an inhibitor ...
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JP6542127B2 |
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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JP2019068741A |
To provide algae that produce sterol, and a method for producing sterol using the same.Algae such as AJ7867 strain (FERM P-22304) and a strain derived therefrom, having a sterol production ability, are cultured. From bodies of the result...
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JP6474722B2 |
A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel c...
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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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JP6335915B2 |
The invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO 2 , amino, COOH, COOCH 3 , OH, N 3 , or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6...
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JP2018512066A |
The present invention discloses a method for making deoxycholic acid (DCA) or an ester thereof or a pharmaceutically acceptable salt thereof. The compound can be applied to remove fat deposits.
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JP6216719B2 |
The present invention relates to pharmaceutical compositions comprising 4-pregenen-11β-17-21-triol-3,20-dione derivatives, and their use as pharmaceuticals as modulators of the glucocorticoid receptors (GR) and/or the mineralocorticoid ...
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JP6204408B2 |
The present invention relates to compounds and methods which may be useful as treatments of neuromuscular diseases such as muscular dystrophy, and as inhibitors of NF-κB for the treatment or prevention of muscular wasting disease, inclu...
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JP6200493B2 |
A novel form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the ulipristal acetate are provided. An amorphous ulipristal acetate or a novel ul...
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JP6130087B1 |
[Subject] Produce a substitute for treating manufacturing a very powerful competitive progesterone receptor antagonist which can be used, i. e., a gynecological disorder. [Means for Solution] Compound of general formula (I) : (Inside of ...
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JP6100798B2 |
A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17α-ethynyl-17β-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are us...
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JP2016188232A |
To provide methods for on-demand contraception in a woman, especially a women who do not have a regular sexual activity.A method for on-demand contraception comprises administering a progestogen agent or progesterone receptor modulator, ...
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JP2016180004A |
To provide novel 19-norsteroids for treating progesterone dependent conditions and use methods thereof.The subject matter of the invention relates to the field of treatment of hormone dependent diseases. Disclosed herein are novel compos...
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JP5913599B2 |
A method as well as new intermediates for preparing Ulipristal acetate (a compound I) and a method for preparing the new intermediates are provided. The intermediate in a constitutional formula IV is conductive to reacting with methyl li...
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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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JP5894739B2 |
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