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WO/2023/209017A1 |
The present invention relates to a process for the preparation of a compound of formula (I), a stereoisomer, a salt, a hydrate or a solvate thereof, comprising the step of desulfinylation of a compound of formula (II) to produce compound...
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WO/2023/178299A1 |
This disclosure relates to ganaxolone derivatives, as well as methods of using the compounds (e.g., for treatment of a disease or disorder), methods of making the compounds, and pharmaceutical compositions and kits comprising the same.
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WO/2023/156803A1 |
The invention relates to novel steroids derived from DHEA of formula (I), as well as their use against arteriosclerosis and/or atherosclerosis. Furthermore, the invention relates to pharmaceutical compositions and medical uses thereof. w...
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WO/2023/143400A1 |
Provided are a steroid compound, a preparation method therefor and a use thereof. The steroid compound may have a structure as shown in formula VI. The compound has SREBP pathway inhibitory activity, and can be used for preventing and/or...
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WO/2023/102613A1 |
The present invention relates to compounds having a range of beneficial therapeutic properties and effects, including neuroprotective effects, anti-inflammatory activity, antioxidative properties, and epithelial cell protective effects. ...
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WO/2023/103929A1 |
Provided are a fulvestrant derivative, and a preparation method therefor and the medical use thereof. Specifically, provided are a fulvestrant derivative represented by general formula (I), a preparation method therefor, a pharmaceutical...
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WO/2023/079362A1 |
Provided herein are compounds having the formula D1-L-D2, wherein D1 is a processable group, L is a linker, and D2 is a drug. Also described herein are pharmaceutical compositions comprising said compounds and methods for the treatment o...
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WO/2023/073413A1 |
The present invention relates to a process for preparing β-[(7α,17β)-17-hydroxy-7[9-[(4,4,5,5,5-pentafluoropentyl)
sulfinyl]nony]estra-1,3,5(10)-trien-3-yl]-boronic acid, also known as Fulvestrant-3-boronic acid or ZB716, whose struct...
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WO/2023/049295A1 |
Deuterated compounds are provided according to Formula (I): Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. These compounds are contemplated as useful for the prevention and treatment o...
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WO/2023/048453A1 |
The present invention relates to nanoparticles comprising a drug dimer, and a use thereof. In addition, the nanoparticles may further comprise fucoidan. The nanoparticles comprising an obeticholic acid dimer compound can be used for trea...
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WO/2023/035906A1 |
The present application provides an intermediate compound and a preparation method therefor and an application thereof. The intermediate compound has the following structural formula (I). By using the intermediate compound of the present...
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WO/2023/021026A1 |
A method of preparing a compound of Formula (VI) is provided wherein: R1, R2 and R3 are independently selected from H, halogen or methyl; and, Pr2 is -Q2, -C(O)Q2 or -Si(Q2)3 wherein each Q2 is independently selected from C1-C6 alkyl, C1...
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WO/2023/008891A1 |
The present invention relates to a novel compound and a preparation method therefor. The compound according to the present invention exhibits inhibitory activity against the generation of TNF-α that is an inflammatory cytokine produced ...
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WO/2022/272103A1 |
25HC3S choline and crystalline 25HC3S choline are described herein. Pharmaceutical formulations of 25HC3S choline such as with crystalline 25HC3S choline and methods of treating or preventing disease with same such as hypercholesterolemi...
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WO/2022/257895A1 |
The present invention relates to an intermediate for fulvestrant and a preparation method therefor. Specifically, the present invention relates to a compound of formula V and a preparation method therefor, wherein R1 is hydrogen or hydro...
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WO/2022/238752A1 |
The present invention relates to a process for preparing B-[(7α,17β)-17-hydroxy-7-[9-[(4,4,5,5,5-pentafluoropentyl)
sulfinyl]estra-1,3,5(10)-trien-3-yl]-boronic acid, known as Fulvestrant-3-boronic acid or ZB716, whose structure is rep...
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WO/2022/238572A1 |
The invention relates to a synthesis of cholesterol; a ring opening step of the compound of formula (I) and subsequent activation and reduction step yielding cholesterol. The inventions relates also to intermediates achieved during said ...
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WO/2022/165512A9 |
Described herein are novel LIF/LIFR inhibitors that exhibit improved cytotoxicity and bioavailability. These LIF/LIFR inhibitors are particularly useful for the treatment of tumors associated with overexpression of LIF.
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WO/2022/207607A1 |
The present invention relates to a process for preparing B-[(7α,17β)-17-hydroxy-7-[9-[(4,4,5,5,5-pentafluoropentyl)
sulfinyl]nonyl]estra-1,3,5(10)-trien-3-yl]-boronic acid, also known as Fulvestrant-3-boronic acid or ZB716, whose struc...
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WO/2022/208157A1 |
The present invention relates to a process for preparing B-[(7α,17β)-17-hydroxy-7-[9-[(4,4,5,5,5~pentafluoropentyl)
sulfinyl]nonyl]estra-1,3,5(10)-trien-3-yl]-boronic acid also known as Fulvestrant-3-boronic acid or ZB716, whose struct...
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WO/2021/252761A2 |
Disclosed herein are monomeric and oligomeric compound embodiments for use as contraceptive agents. Monomeric compound embodiments disclosed herein comprise substituents that facilitate the ability of the compounds to exhibit progestogen...
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WO/2021/248049A1 |
Described herein are compounds and pharmaceutical compositions containing such compounds for the modulation of Hedgehog signaling.
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WO/2021/142477A1 |
The invention of this disclosure is directed to a neuroactive steroid (NAS) of a novel structure. This invention is also directed to a pharmaceutical composition comprising the neuroactive steroid (NAS) and salts thereof. The pharmaceuti...
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WO/2021/140480A1 |
It is provided a method for the preparation of 3β-arachidylamido-7α,12α-dihydroxy-5β-cholan-24-carboxyl
ic acid comprising the step of: d) reacting compound (IV) with methane sulphonyl chloride to get methyl 7α,12α-diacetyloxy-3α-...
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WO/2021/133976A1 |
Crystalline and liquid crystalline forms of 25HC3S sodium are described herein. The disclosure includes Forms I, II, III, V, IX, XI, and XIII of 25HC3S sodium and combinations thereof. Pharmaceutical formulations of said forms, or combin...
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WO/2021/075860A1 |
The present invention relates to novel 2-Methoxyestradiol derivatives and their medical use. In particular, the novel derivatives of the present invention are useful for the treatment or prevention of liver or lung fibrosis. Accordingly,...
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WO/2021/014348A1 |
The present invention relates to an improved process of manufacturing sterile topical ophthalmic aqueous nanosuspensions of nanocrystals of fluticasone propionate Form A. The sterile topical ophthalmic nanosuspensions are useful in the t...
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WO/2020/264495A1 |
Provided herein is a compound of Formula (1-I): or a pharmaceutically acceptable salt thereof, wherein R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R11a, R11b, R16a, R16b, R19, R18, X, q, r, s, t, u, and n are defined herein. Also provided here...
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WO/2020/243488A1 |
Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7a, R7a, R11a, R11b, R12a, R12b, R16a, R16b, R19, R11a, R22, RX, RY and n are defined he...
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WO/2020/128514A1 |
2-Fluorinated bile acid compounds of general formula (I) wherein at least one of R1 and R2 represents F and the other is chosen 3 from H and F and wherein R3 is as defined herein; are of use in the treatment and prevention of neurodegene...
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WO/2020/053664A1 |
Methods for treating estrogen receptor positive (ER+) breast cancer, comprising administering to a subject in need thereof, a BET bromodomain inhibitor in combination with a second agent, selected from a selective-estrogen receptor degra...
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WO/2020/020728A1 |
Disclosed are compounds of formula (I), wherein X, Y, Z are annular atoms comprised in a five-membered carbocyclic or heterocyclic ring, selected from the group consisting of CH, NH, N, O, S; saidcarbocyclic or heterocyclic ring being op...
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WO/2019/101132A1 |
Disclosed in the present invention are a fluorosulfonyl-containing compound, an intermediate thereof, a preparation method therefor and use thereof. The fluorosulfonyl-containing compound disclosed in the present invention comprises a ca...
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WO/2019/089365A1 |
Provided herein are crystalline solid forms of squalamine phosphate designated as Form 1 and Form 2, compositions containing one or both forms, and methods of their preparation and of their use.
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WO/2019/081586A1 |
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 DCA and pharmaceutically acceptable salts thereof, the carbon atoms of...
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WO/2019/015914A1 |
The invention relates to a process for the preparation of obeticholic acid and derivatives thereof comprising: (a) hydrogenation of the double bond and reductive opening of the epoxide of a compound of formula (II) or a salt or solvate t...
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WO/2018/187804A1 |
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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WO/2018/164715A1 |
The present invention relates to methods of treating or preventing cancer in a subject in need thereof comprising administering a therapeutically effective amount of a compound of the invention.
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WO/2018/064649A1 |
Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1A, R1B, n, R2A, R2B, R3, and R4 are as defined herein. Compounds of the present invention ...
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WO/2018/064441A1 |
A crystalline form of a bile acid compound and methods of preparation and use thereof are described.
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WO/2018/026837A1 |
Compositions comprising oxygenated cholesterol sulfates (OCS) are provided. The OCS is, for example, 5-cholesten-3, 25-diol, 3-sulfate (25HC3S) or 5-cholesten, 3, 25-diol, disulfate (25HCDS). The compositions may be used to prevent and/o...
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WO/2018/026781A1 |
Compositions comprising 5-cholesten-3, 25-diol, 3-sulfate (25HC3S) or pharmaceutically acceptable salt thereof and at least one cyclic oligosaccharide, e.g., a cyclodextrin (CD), are provided. The compositions may be used to prevent and/...
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WO/2017/199033A1 |
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 conditio...
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WO/2017/199039A1 |
The invention relates to a process for preparing a compound of general formula (Ia): 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...
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WO/2017/148977A1 |
This invention concerns Selective Progesterone Receptor Modulators (SPRM) in a prodrug form as well as their application in therapy. (3α, 11β,17β)-1 1-[4-(methylsulfonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-
diene-3,17-diol (Compoun...
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WO/2017/129125A1 |
The present invention relates to a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt thereof, and relates to applications thereof in the preparation of drugs for treating FXR related diseases.
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WO/2017/112904A1 |
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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WO/2017/112902A1 |
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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WO/2017/079062A1 |
The present application relates to a method of preparing a bile acid derivative, or a pharmaceutical acceptable salt, solvate, or amino acid conjugate thereof, comprising direct alkylation at the C-6 position of KLCA.
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WO/2017/064724A1 |
The present invention relates to a simple and commercially feasible preparation of high purity Fulvestrant. The present invention also provides improved process for the preparation of Fulvestrant intermediates.
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