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WO/2016/205475A2 |
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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WO/2016/186821A1 |
Cationic steroidal antimicrobial (CSA) compounds having amide functionality and methods of manufacturing such CSA compounds. The CSA compound can be a compound of Formula (I), Formula (II), Formula (III), or a salt thereof: where R18 has...
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WO/2016/184103A1 |
The present invention relates to a cholic acid modified glucosamine derivative and a preparation method and use therefor, the derivative being as shown in formula (I), wherein R1 is H or OH, R2 is H or OH, R3 is H, CH2 = CHCO- or CH2 = C...
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WO/2016/173397A1 |
The present invention relates to a cholic acid derivative, and a preparation method and a medical use thereof. In particular, the present invention relates to a cholic acid derivative with the structure of formula (I), a stereoisomer, or...
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WO/2016/173524A1 |
Disclosed in the present application are the compounds as shown in formulae I, II, III, IV or V, tautomers thereof, stereoisomers thereof or pharmaceutically acceptable salts thereof, and also disclosed is the use thereof in preparing dr...
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WO/2016/173493A1 |
This disclosure is related to a sulfonylaminocarbonyl derivative of formula (I) and/or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the sulfonylaminocarbonyl derivatives of formula (I) and/or a phar...
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WO/2016/154203A1 |
Described herein are new anti-cancer compounds and methods of using such compounds, acting through a new mechanism of action by simultaneous inhibition of leukemia inhibitory factor (LIF) and MDM2. In one embodiment, a cytotoxic compound...
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WO/2015/071657A9 |
Described herein are certain steroid derivative compounds, for example of formula (I): wherein X1, X2, X3 L, and Ar are as defined herein, pharmaceutical compositions comprising such compounds, the use of such compounds and compositions ...
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WO/2016/113549A1 |
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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WO/2016/103280A1 |
The present invention relates to the preparation of novel Steroid-Chitosan ketimine nanoparticles by one pot convenient process and determination of their Antibacterial and Antifungal Activities. This invention also relates to the synthe...
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WO/2016/037956A1 |
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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WO/2016/029888A1 |
The present invention provides amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use as medicaments for treating neuropsychiatric disorders associated with an ...
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WO/2015/197872A1 |
The present invention relates to a compound with the following formula (I): (I) or a salt and/or a pharmaceutically acceptable solvate thereof, the use of same in the treatment of cancer, the pharmaceutical compositions containing same a...
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WO/2015/181275A1 |
13073PTWO 56 ABSTRACT The present invention relates to compounds having cholane scaffolds of formula (I), said compounds for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases. 5
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WO/2015/177469A1 |
The present invention relates to chemical compounds and the therapeutic use thereof, in particular for improving muscular quality in mammals. More particularly, the invention enables improvement of muscular quality in sarcopenic mammals ...
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WO/2015/121840A1 |
The present invention relates to a process for the synthesis of compounds of formula (I), (I) wherein the meaning of R is dimethylamino or acetyl group, using the compound of formula (III) or (IV), wherein the meaning of R' is dimethylam...
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WO/2015/101468A1 |
The present invention relates to a broad spectrum stable sunscreen molecule having the general structure (Formula) where "X" is an organic sunscreen belonging to the UVA class and "Y" is an organic sunscreen belonging to UVB class or vic...
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WO/2015/095971A1 |
The present invention provides bacterial ATP synthase inhibitors such as a compound of formula (I): (Formula (I)) (A) in combination with an aminoglycoside antibiotic for preventing or treating a bacterial infection in a subject; or (B) ...
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WO/2015/092647A1 |
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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WO/2015/087340A1 |
The present invention discloses a novel bile acid derivatives having substituted nitrogen functionality at C-11 and process for synthesis thereof. These C-11 substituted bile acid derivatives shows anticancer and antimycobacterial activity.
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WO/2015/049637A1 |
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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WO/2015/031598A2 |
The present invention includes DNP derivatives that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional t...
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WO/2015/010054A2 |
Described herein are neuroactive steroids of the Formula (I): (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 GAB...
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WO/2014/188445A1 |
The present invention relates to a process for the preparation of (3β)-17-(3- pyridinyl)androsta-5,16-dien-3-yl acetate compound of formula- 1. The present invention also relates to a novel polymorph of compound of formula- 1 and proces...
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WO/2014/184271A1 |
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1 is a hydroxy group and R2, R3, R4, R5, and R6 are as described herein. The present inven...
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WO/2014/164861A1 |
Polymorphic forms of onapristone and methods of making and using such polymorphic forms are provided. Crystalline polymorphic forms can be characterized by their X-ray powder diffraction patterns and other properties.
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WO/2014/122480A1 |
The present invention relates to novel derivatives of estradiol, in particular to deuterated derivatives of estradiol sulfamates. The present invention also relates to compositions comprising said novel derivatives, as well as to uses of...
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WO/2014/117700A1 |
The present invention provides a protopanoxadiol derivative of structural formula I or II, a preparation method and an application thereof. The present invention performs structural modification on protopanoxadiol, and obtains multiple n...
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WO/2014/115170A1 |
The present invention relates to the synthesis of pregnane-oximino-aminoalkyl-ethers and their antidiabetic and antidyslipidemic activities. More particularly, the invention relates to the synthesis of compounds of formula 3 and biologic...
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WO/2014/091158A1 |
The present invention relates to testosterone derivatives of formula (I): in which n is an integer between 1 and 10 and Y is an activated or ready-to-be-activated group which enables the formation of an amide bond with a primary amine of...
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WO/2014/093378A1 |
Compounds useful for molecular imaging of cells expressing estrogen receptors are provided. Also provided are intermediates for making the compounds and methods of making the compounds using a modular convergent strategy. Further, method...
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WO/2014/083068A1 |
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, NO2, amino, COOH, COOCH3, OH, N3, or halogen and R2 is H, OH, Cl-8 alkyl, Cl-8 alkoxy, C2-C6 al...
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WO/2014/083512A1 |
The present invention relates to process for the preparation of abiraterone acetate, its salts and intermediates thereof, crystalline forms of abiraterone acetate salts and purification of abiraterone acetate.
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WO/2014/059499A1 |
The invention, preparation method and composition of a pharmaceutical drug from quenodeoxicholate linked to a natural, d-fructose-analogue, sulfamate-derived monosaccharide (topiramate) and to a phenyl ketone (bupropion) for the treatmen...
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WO/2014/060888A1 |
The present invention is related to a novel process for the preparation of ulipristal (I) that comprises reaction of 17-α-ethynyl-17-β-hydroxy-11-β-(4-N,N-dimethylamino phenyl)- 9-norpregna-4,9-diene-3-one (III) with phenyl sulphenyl ...
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WO/2014/058736A1 |
The present disclosure is generally directed to neuroactive 19-alkoxy-17(20)-Z-vinylcyano-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the tre...
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WO/2014/050107A1 |
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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WO/2014/050105A1 |
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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WO/2014/050106A1 |
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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WO/2013/188792A2 |
Described herein are neuroactive steroids of the Formula (I) or a pharmaceutically acceptable salt, solvate, stereoisomer, tautomer, and/or isotopic variant thereof; wherein ----, X, Z1, Z2, R1, R2, R3, and R4 are as defined herein, prov...
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WO/2013/168096A1 |
The invention relates to novel sterol derivatives, the preparation method thereof, pharmaceutical compositions containing them and use thereof for treating diseases involving transformed astrocyte cells or for treating malignant haemopat...
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WO/2013/158970A2 |
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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WO/2013/133980A1 |
A compound of formula (I) or a pharmaceutically acceptable salt thereof, and an ophthalmic composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof. The invention is also directed to the use of the o...
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WO/2013/104346A1 |
The invention provides new lipopolyamines of spermine type of the general formula I, wherein X is C-N bond or aminopolyethyleneglycolcarboxamide linker or o-hydroxy- alkylcarboxamide linker or ω-hydroxyalkylcarboxamidopolyethyleneglycol...
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WO/2013/100712A1 |
The present invention relates to a novel blocker for vascular leakage. The novel blocker for vascular leakage of the present invention inhibits the apoptosis of endothelial cells, suppresses the formation of actin stress fibers induced b...
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WO/2013/091120A1 |
The invention features protected linker compounds which comprise at one terminus a protected amino group and at another other terminus a phosphorous activating group, such as a phosphoramidite group. These protected linker compounds are ...
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WO/2013/063859A1 |
Provided are an Ulipristal acetate (compound I) preparation method, a novel key intermediate (compound of formula IV) for preparing the Ulipristal acetate and preparation of the key intermediate. It has been surprisingly found in the pre...
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WO/2013/057422A1 |
The present invention concerns new aminosteroid derivatives substituted in positions 3 and/or 6, and the use thereof in the context of the treatment of type 2 diabetes and insulin resistance.
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WO/2013/036835A1 |
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L1, L2, L3, X1, X2, Y, Rz4, Rz5, Rz6, n, R1, R2, R3a, R3b, R4a...
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WO/2013/030410A2 |
The present invention relates to processesfor obtaining abirateroneand derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C-C coupling through a steroid h...
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