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JP7248819B2 |
3α5β-steroid compounds of general formula I is disclosed. These compounds are useful in the treatment of epilepsy or comorbidities associated with epilepsy or conditions associated with convulsions, such as seizures associated with hyp...
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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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JP2023022187A |
To provide compositions and methods for treating CNS disorders.Described herein are neuroactive steroids of the formula (II) in the figure or pharmaceutically acceptable salts thereof. Such compounds are supposed, in certain embodiments,...
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JP2022543242A |
The present invention relates generally to novel aminosterol compounds, compositions containing the same, and methods of making and using the novel aminosterol compounds and compositions. [Selection drawing] Fig. 1C
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JP2022543244A |
This application relates generally to novel aminosterol compounds, compositions containing them, and methods of making and using the novel aminosterol compounds and compositions. [Selection drawing] Fig. 1
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JP7136802B2 |
The present invention relates to processes for preparing compounds of Formula (I) and compounds of Formula (II) or a pharmaceutically acceptable salt or solvate thereof. These compounds and pharmaceutical compositions are useful as FXR o...
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JP2022116318A |
To provide compositions and methods for treating CNS disorders.The invention provides a compound of a formula (I) or a pharmaceutically acceptable salt thereof. In the formula (I), A is aryl, heterocyclyl or heteroaryl; R1 and R2a are C1...
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JP2022533069A |
Described herein are methods and compositions for the inhibition of bile salt hydrolases (BSH), as well as their use. Provided herein are metabolic disorders (eg, diabetes, obesity), gastrointestinal disorders (eg, gastrointestinal infec...
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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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JP7083394B2 |
The invention discloses a panaxadiol glycoside derivative and a preparation method and application thereof. Such compounds show strong anti-inflammatory effects in vitro and in animal model experiments, and thus can be used to prepare an...
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JP2022075974A |
To provide C17, C20 and C21 substituted neuroactive steroids and their methods of use.Described herein are neuroactive steroids or pharmaceutically acceptable salts thereof. Such compounds are expected, in certain embodiments, to behave ...
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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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JP7064515B2 |
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereofwherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17β-HSD1 and in treatment or preve...
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JP7057783B2 |
or a pharmaceutically acceptable salt or solvate thereof, and intermediates of use in said processes.
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JP7050008B2 |
The present invention relates to new and improved processes for the preparation of deoxycholic acid (DCA) and pharmaceutically acceptable salts thereof, as well as to novel intermediates useful for the preparation of DCA and pharmaceutic...
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JP7049313B2 |
Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a comp...
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JP7034094B2 |
The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). Th...
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JP7034093B2 |
The invention relates to compounds of general formula (I):wherein: , R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditi...
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JP7034092B2 |
wherein R2, Y, R4 and R5 are as defined herein. The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.
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JP6995757B2 |
The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The s...
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JP2021533206A |
Compound of general formula (I): [Chemical 1](In the formula, R2a, R2b, R3a, R3b, R5, Y and R7Is a selective agonist of FXR receptors, non-alcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; bilia...
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JP6974388B2 |
Described herein are neuroactive steroids of the Formula (I):or a pharmaceutically acceptable salt thereof; wherein R1a and R1b are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. T...
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JP6948680B2 |
Provided are a compound for treating metabolic diseases having the structure as shown in formula (I) or formula (II), or a racemate, stereoisomer, geometric isomer, tautomer, solvate, hydrate, metabolite, pharmaceutically acceptable salt...
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JP2021120396A |
To provide methods and systems for making intermediates in the synthesis of onapristone.A method comprises irradiation with narrow band frequency light from a lamp selected from the group consisting of an excimer DBD light source and an ...
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JP2021518842A |
The present invention generally relates to formulations and methods for treating cancer. Formulations comprising substituted steroid derivatives are provided herein. The subject formulation is useful in the treatment of cancer. [Selectio...
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JP6893173B2 |
Described herein are neuroactive steroids of the Formula (II):or a pharmaceutically acceptable salt thereof; wherein A, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6and------are as defined herein. Such compounds are envisioned, in certain emb...
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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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JP2021073200A |
To provide novel carrier compositions for efficiently delivering a therapeutic agent, diagnostic agent, or targeting agent to a therapeutic site, in the treatment of diseases such as cancer, or in vivo diagnosis.Provided is a carrier com...
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JP2021073250A |
To provide aminosteroid compounds for selective inhibition of the enzyme PTP1B in a mammal, and compositions comprising the aminosteroid compounds.The invention provides various aminosteroid compounds which inhibit protein phosphatase IB...
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JP6867577B2 |
Provided are panaxdiol-type ginsenoside derivatives having structures as shown in formula I or formula II. Also provided are the uses thereof in the preparation of drugs for preventing and treating atherosclerosis. The panaxdiol-type gin...
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JP6861703B2 |
The application relates to compounds of formula (A): or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, includin...
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JP6853833B2 |
Described herein, inter alia, are compositions and methods for treating or preventing hyperproliferative disorders, including cancer.
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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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JP2021046409A |
To provide novel compounds for treating or preventing cancer.Provided herein are substituted steroidal derivative compounds having the structure in the figure, and pharmaceutical compositions comprising the compounds. The subject compoun...
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JP6849233B2 |
Polyethylene glycol (PEG)-conjugated glucocorticoid prodrugs, methods of preparation, and use for the treatment of diseases and disorders are disclosed. In particular, PEG-conjugated dexamethasone compounds and methods of using them for ...
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JP2021504480A |
Cataracts and presbyopia affect billions of people worldwide. Described herein are new compounds and methods for treating and preventing these diseases. The present disclosure provides new compounds, salts, compositions and their use in ...
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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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JP6802862B2 |
The invention provides for treating HBV or HDV infection or inhibiting human sodium taurocholate co-transporting polypeptide (hNTCP) with a polymeric bile acid or salt thereof, and pharmaceutical compositions comprising a polymeric bile ...
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JP2020536566A |
Probe embodiments for targeting, identifying, and isolating enzymes exhibiting BSH activity, as well as devices and kits that use the probes, are described herein. It also describes how to make and use probes, devices, and kits. In some ...
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JP6801093B2 |
The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The s...
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JP6800748B2 |
The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to platinum based compounds comprising platinum moiety, linker moiety and lipid moiety and corres...
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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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JP6785788B2 |
The present invention provides compounds represented by Formula I, or pharmaceutically acceptable salts, stereoisomers, solvates, hydrates or combination thereof,The invention also provides pharmaceutical compositions comprising these co...
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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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JP2020528892A |
The present application relates to isotope-labeled compounds of formula I, as well as methods of their preparation and use.
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JP6735665B2 |
Hydrophilic, high quantum yield, chemiluminescent acridinium compounds with increased light output, improved stability, fast light emission and decreased non specific binding are disclosed. The chemiluminescent acridinium esters possess ...
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JP6712599B2 |
The invention relates to 3α-ethynyl, 3β-hydroxy, 5α-pregnan-20-oxime or a pharmaceutically acceptable salt thereof, which compounds and/or salts are useful as modulators of the mammal brain excitability via the gamma-5 aminobutyric ac...
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JP6704535B2 |
Disclosed are a lanosterol prodrug compound, a pharmaceutically acceptable salt and an isomer thereof, and a pharmaceutical composition comprising the lanosterol prodrug compound and the use thereof in the preparation of a drug for treat...
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JP2020073868A |
To provide a composition for making biological tissue transparent and a method for making biological tissue transparent using the composition.A transparentizing method for transparentizing a biological tissue using a biological tissue tr...
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