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WO/2023/213151A1 |
The present invention provides a method for preparing abiraterone acetate and an intermediate thereof. The method particularly relates to the steps of: in an organic solvent, in the presence of a metal catalyst, reacting 3-site protected...
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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/2023/148764A1 |
The present invention is to design and develop novel synthetic cholic acid derivatives for treating autoimmune disorders/inflammatory conditions, process of synthesis of the compounds, compositions comprising the said compounds and use 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/2023/035906A1 |
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/2023/003863A1 |
The present disclosure describes novel processes and intermediates for making onapristone.
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WO/2023/001866A1 |
A process for the preparation of a compound of formula (IIa) is described where A is a silyl protecting group, in high diastereoisomeric purity and in crystalline form, comprising the crystallization of a mixture of the compound of formu...
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WO/2023/288123A1 |
The present application relates to methods and novel intermediates useful in the preparation of a compound of formula 100 (Compound 100).
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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/2022/225920A1 |
The present disclosure relates to a crystalline form of (((((E)-1-((8S,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-2,3,
6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta
[a]phenanthren-17-yl)ethylidene)amino)oxy)methyl dihydrogen...
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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/2022/171101A1 |
The present application relates to a steroid conjugate, and in particular, to a compound or a tautomer, a mesomer, a racemate, an enantiomer, and a diastereoisomer thereof, or a mixture form thereof, or a pharmaceutically acceptable salt...
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WO/2022/122042A1 |
Disclosed in the present invention are an abiraterone derivative and a preparation method therefor. The abiraterone derivative of the present invention has a structure as represented by general formula (I). The abiraterone derivative of ...
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WO/2022/115381A1 |
Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein ring D and the substituents are defined herein. Also provided are pharmaceutical compositions comprising a compound of Formula (I) or a p...
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WO/2022/091136A1 |
The present disclosure provides a compound of Formula (I) and its polymorphs, stereoisomers, prodrugs, solvates, co-crystals, intermediates, pharmaceutically acceptable salts, and metabolites thereof. The present disclosure also reveals ...
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WO/2021/262836A1 |
Provided herein is a compound of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R2a, R2b, R3a, R4a, R4b, R5, R6, R7, R11a, R11b, R15a, R15b, R16,R17, R19, RX, RY, and t are defined herein. Also provided herein are...
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WO/2021/236953A1 |
Cationic steroidal antimicrobial (CSA) compounds having a structure of Formula I, II or III, or salt thereof, wherein at least one of R1-R18, (e.g., R18) includes a terpenyl group attached via an ester or amide linkage and at least one R...
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WO/2021/214685A1 |
The present invention refers to a method for the preparation of a compound of formula (I).
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WO/2021/204142A1 |
The present invention provides a salt of a bile acid derivative, a crystal form thereof, a preparation method therefor and use thereof. The salt of a bile acid derivative, the crystal form thereof and a composition thereof provided by th...
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WO/2021/098872A1 |
The present invention relates to a compound represented by general formula (I) or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof, and the pharmaceutical use thereof. The compound of general formula (I) has a str...
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WO/2021/069570A1 |
Compounds and compositions for the activation of SERCA2a are disclosed. In particular, provided are compounds that act as predominantly pure or pure SERCA2a activators while only moderately inhibiting the Na+/K+ ATPase. In general, the d...
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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/2020/222717A1 |
The invention is related to an AG-08 coded novel structured molecule having cytotoxic features against cancer cells. The aim of the invention is to primarily synthesize the astragenol (AG) molecule from cycloastragenol (CA) and then from...
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WO/2020/187658A1 |
The invention relates to a process for the preparation of fulvestrant 3- boronic, comprising the transformation of the compound of formula (IV) into the compound of formula (III). The intermediate of formula (III) also forms part of the ...
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WO/2020/169643A1 |
The present invention relates to the diethylamine salt of 3a- tetrahydropyranyloxy-6a-ethyl-7a-hydroxy-53-cholanic acid (I), which is a new intermediate in the synthesis of obeticholic acid, to the use of said diethylamine salt in the sy...
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WO/2020/168283A1 |
The present disclosure relates to methods of managing cancer by modulating/inhibiting cap methyltransferase enzyme. The modulation/inhibition is carried out by pharmacological or biological inhibitors, including but not limited to compou...
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WO/2020/132504A1 |
Provided herein is a compound of Formula (I) or pharmaceutically acceptable salt thereof, wherein R2a, R2b, R4a, R4b, R6, R7, R11a, R11b, R16, R17, R3, R5, R19 and RX are defined herein and wherein RY represents optionally substituted 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/2020/119836A1 |
A process for preparing obeticholic acid, wherein the 7-keto-litocholic acid amide of formula (II), where R1, R2 are a C1-C6 n-alkyl, or together a C5-C6 cycle and the protecting group on the hydroxyl in position 3 is a carbamoyl with th...
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WO/2020/025942A1 |
Compounds of general formula (I): wherein R2a, R2b, R3a, R3b, R5, Y and R7 are as defined herein are selective agonists at the FXR receptor and are useful for the treatment or prevention of diseases and conditions including nonalcoholic ...
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WO/2019/224790A2 |
The present invention relates to fulvestrant prodrugs of formula II and process for the preparation thereof. The present disclosure also relates to pharmaceutical composition of fulvestrant prodrugs and method of treatment using the same.
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WO/2019/126741A1 |
Provided herein are compounds of Formula (I-I): and pharmaceutically acceptable salts thereof; wherein p, R1, R3a, R2a, R11a, R11b, R6a, and R6b are defined herein. Also provided herein are pharmaceutical compositions comprising a compou...
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WO/2018/103626A1 |
The present invention relates to the field of medicine, and particularly relates to a water-soluble allopregnenolone derivative, a pharmaceutical composition comprising the same, and use thereof in prevention or treatment of central nerv...
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WO/2018/085623A1 |
Disclosed are methods of treating or reducing the occurrence of a steatohepatitis disorder. The disorder may include, for example, NASH, parenteral nutrition associated liver disease (PNALD), or genetic forms of liver disease. The method...
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WO/2018/071544A1 |
This document relates to an abiraterone derivative, 2-(((3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-
2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]ph
enanthren-3-yl)oxy)-2-oxoacetic acid (ABOA). This document also...
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WO/2018/068021A1 |
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/2018/060280A1 |
Compounds of formula (I), wherein Ar is an aryl group optionally further substituted with one or more groups R3; A is a lipophilic, hydrophobic moiety; R1 is a phosphodiester, phosphotriester, thioether or amide group; X is an unsubstitu...
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WO/2018/054300A1 |
Provided is a crystalline form cholic acid derivative free alkali, a preparation method therefor and an application. The chemical name of the cholic acid derivative free alkali is (5R)-5-((2R)-2-((3R,5S,6R,7R,10S,13R)-6-ethyl-3,7-dihydro...
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WO/2018/035079A1 |
A class of cyanosteroid compounds that efficiently inhibit ghrelin acylation by ghrelin O-acyltransferase. The compounds have a steroid scaffold with α,β-unsaturated ketone in the A ring position such an a-cyanoenone. Exemplary compoun...
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WO/2017/207648A1 |
The invention relates to a process for the preparation of obeticholic acid and derivatives thereof comprising: (a) olefination of a compound of formula (II) or a salt or solvate thereof to obtain a compound of formula (III) or a salt or ...
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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/2017/192668A1 |
Disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery. In particular, disclosed are methods for identifying a pregnant female who is susceptible to spontaneous preterm delivery based o...
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WO/2017/150723A1 |
Algae that generates a sterol and a sterol production method that uses the algae. According to the present invention, a sterol is produced by culturing algae, such as strain AJ7867 (FERM BP-22304) and strains derived therefrom, that has ...
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WO/2017/149091A1 |
The invention relates to a process for the preparation of 11 -methylene steroids through selective olefination of the ketone at position 11. The resulting products are useful intermediates in the preparation of several pharmaceutically a...
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WO/2017/149052A1 |
The invention pertains to a process for producing a compound of formula (11) wherein R7 and R8 are each independently selected from H, halogen, alkyl, aryl, or alkylaryl, R42 is H or a protective group, R43 is H or R3, wherein R3 is a pr...
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