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WO/2021/018298A1 |
Disclosed is a class of indolo-seven-membered acyloxime compounds, and specifically disclosed are compounds as shown in formula (I), and pharmaceutically acceptable salts thereof.
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WO/2020/245213A1 |
The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising ...
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WO/2020/242923A1 |
This disclosure relates to uses of radiation and benzodiazepines optionally in combination with other anticancer agents for treating cancer. In certain embodiments, this disclosure relates to methods of using radiation, benzodiazepines, ...
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WO/2020/210662A1 |
The present disclosure provides compounds of formula (I), as described herein, their pharmaceutically acceptable salts, and their pharmaceutical compositions, which are effective in reducing the expression level of KLF5 or EGR1 in a livi...
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WO/2020/200283A1 |
In an embodiment of the present invention, a fluorenone ligand compound for an α7 nicotinic acetylcholine receptor represented by the following formula (I) is provided, wherein, X is a 6- to 10-membered nitrogen-containing heterocyclic ...
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WO/2020/192637A1 |
Disclosed are a solid form and a crystal form of a compound represented by formula (1) used as a BRD4 inhibitor, a preparation method therefor, and an application thereof in the preparation of a medicine for treating BRD4-related disease...
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WO/2020/184670A1 |
The present invention relates to a method for monodeuterated lower alkylating an amine moiety of a compound which contains an amine that is protected by an aralkyl group, wherein a monodeuterated lower alkyl is introduced into the amine ...
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WO/2020/131000A1 |
The invention relates to a crystalline form of the Compound (I), wherein the crystalline form displays its strongest reflection, stated as a 2Θ value, at 25±0.2°, in an X-ray powder diffraction pattern. The invention also relates to a...
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WO/2020/127390A1 |
A method is provided for preparing a compound d having the formula (D) The method comprises carrying out the following reaction (c) → (d), where the reaction is carried out at a temperature of at least 100 °C and in the presence of a ...
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WO/2020/127385A1 |
A method is provided for preparing a compound d having the formula: Formula (I). The method comprises carrying out the following reaction: Formula (i), (ii), (d) where: step (i) is carried out in the presence of a metal catalyst and a hy...
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WO/2020/039631A1 |
Disclosed is a compound represented by formula (1): Q-CHR2 (1) (in the formula, Q represents a nitrogen-containing aliphatic group that includes two or more tertiary nitrogen atoms, and does not include oxygen, and R represents an alipha...
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WO/2020/035464A1 |
The present invention relates to compounds of formula (I): wherein Q is selected from O or S; R1 and R3 are each independently hydrogen or an optionally substituted hydrocarbyl group, or R1 and R3 together with the nitrogen atom to which...
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WO/2020/027304A1 |
Provided are carotenoid derivatives having exceptional hydrophilicity and oral absorptivity. A carotenoid-related compound represented by the formula (in the formula, X represents a carbonyl group or a methylene group, and Z1 and Z2 are ...
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WO/2020/021021A1 |
The present invention relates to ortho substituted phenoxypropylamino and benzyloxypropylamino derivatives having pharmacological activity towards the α2δ subunit of the voltage-gated calcium channel, in particular to ortho substituted...
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WO/2020/011086A1 |
Involved are a class of benzodiazepine heterocyclic compounds, a preparation method therefor and the use thereof, as well as a pharmaceutical composition containing the compound. In particular, the present invention relates to the compou...
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WO/2019/246541A1 |
The application relates to compounds, or pharmaceutically acceptable salts, hydrates, solvates, or stereoisomers thereof, which modulate the activity of EGFR, a pharmaceutical composition comprising said compounds, and methods of treatin...
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WO/2019/245047A1 |
The purpose of the present invention is to provide a technique for imaging the brain of a living animal and application of the technique. A radiolabeled dibenzoazepine derivative, which shows excellent brain transferability, high recepto...
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WO/2019/222298A1 |
The present invention provides methods of use for compositions comprising bisfluoroalkyl-l,4-benzodiazepinone compounds, including compounds of Formula (I) or prodmgs thereof; for treating diseases and disorders such as cancer.
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WO/2019/168688A9 |
The present invention includes a solid lyophilized form of 2-(4-Methyl-[1,4]diazepan-1-yl)-5-oxo-5H-7-thia-1,11b-diaza-
benzo[c]fluorene-6-carboxylic acid (5-methyl-pyrazin-2-ylmethyl)-amide (Compound I) and the process of producing the ...
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WO/2019/215427A1 |
A process for forming a carbon-carbon bond to couple an aryl or heteroaryl group of a first compound with an alkyl or cycloalkyl moietyof a second compound, the process comprising reacting the first compound with the second compound in t...
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WO/2019/168688A3 |
The present invention includes a solid lyophilized form of 2-(4-Methyl-[1,4]diazepan-1-yl)-5-oxo-5H-7-thia-1,11b-diaza-
benzo[c]fluorene-6-carboxylic acid (5-methyl-pyrazin-2-ylmethyl)-amide (Compound I) and the process of producing the ...
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WO/2019/173327A1 |
Disclosed are compounds according to Formula (I) or (II), and pharmaceutical compositions comprising them. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (I) or (II).
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WO/2019/164947A1 |
The application relates to a compound having Formula Ia or Ib: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method o...
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WO/2019/164948A1 |
The application relates to a compound having Formula Ia or Ib: (Ia) or (Ib), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, ...
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WO/2018/119362A8 |
Provided herein are compounds and methods for inhibiting histone deacetylase ("HDAC") enzymes (e.g., HDAC1, HDAC2, and HDAC3).
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WO/2019/103658A3 |
Derivatives having the general formula (I) and being limited to structural variants. The claimed compounds are used in the field of medicine as analgesics, anorexigenic or orexigenic agents for regulating weight (loss or gain), antidepre...
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WO/2019/120212A1 |
Disclosed in the present invention is a new class of compounds that act as indoleamine-pyrrole 2,3-dioxygenase (IDO) inhibitors, and specifically disclosed thereby are a compound represented by formula (I) and a pharmaceutically acceptab...
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WO/2019/115429A1 |
The invention relates to compounds according to the general formula (I) or a pharmaceutically acceptable salt of an inorganic or organic acid, a hydrate, a stereoisomer or a solvate thereof, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 a...
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WO/2019/103658A2 |
The invention relates to novel compounds that are derivatives of 1,4-benzodiazapin-2-one, having the general formula (I) and being limited to structural variants (1-6), on the condition that: а) structures 1 (R1=Br, R4=F), 3 (R1=OCF3, R...
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WO/2019/099560A1 |
The present subject matter provides compositions, formulations and methods for preventing or reducing proliferation or migration of retinal cells or epithelial to mesenchymal transition in ocular cells or cells from other tissues.
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WO/2019/094903A1 |
The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors. The present invention also relates to p...
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WO/2019/086902A1 |
The disclosures herein relate to novel compounds of formula (1) and salts thereof, wherein X;Y; R1; R2; R3; R4; R5; R6; R7 and R8 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk o...
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WO/2019/087149A1 |
The present invention provides in one aspect azabicycio and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, t...
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WO/2019/082910A1 |
Provided are: a V2 receptor antagonist which has high water solubility and which is particularly suitable for injections; and a medicine containing the V2 receptor antagonist or the like. The present invention is a compound represented b...
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WO/2019/081691A1 |
The present invention relates to new compounds of formula (I) that show great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), or dual activity towards the subunit α2δ of voltage-gated calcium c...
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WO/2019/067864A1 |
The present invention relates to pharmaceutical agents administered to a subject either in combination or in series for the treatment of a Respiratory Syncytial Virus (RSV) infection, wherein treatment comprises administering a compound ...
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WO/2019/056950A1 |
The present invention relates to a class of thienodiazepine derivatives and an application thereof in the preparation of a drug for the treatment of diseases associated with bromodomain and extra-terminal (BET) Bromodomain inhibitors. Sp...
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WO/2019/034532A1 |
The present invention covers 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7- carboxamide compounds of general formula (I): in which R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5 and X are as defined herein, methods of preparing said compou...
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WO/2019/006459A1 |
Disclosed are methods and compositions related to STK1 inhibitors, such as Inh2-B1 (methyl 5-oxo-3-(phenyl carbamoyl)-1-thioxo-4,5dihydro[1,3]thiazolo[3,4-a]quinazolin
e-8-carboxylate). The STK1 inhibitors can act as an antibiotic resist...
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WO/2018/233727A1 |
Provided are an indole compound and an application thereof. The compound is capable of effectively inhibiting CBP/EP300 bromodomain receptors, and may be used as a drug for cancers, inflammatory diseases, autoimmune diseases, septicaemia...
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WO/2018/216800A1 |
The present invention provides: a compound represented by general formula (I) or a salt thereof; an LSD1 inhibitor which contains the compound or a salt thereof as an active ingredient; a pharmaceutical composition which contains the com...
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WO/2018/119362A3 |
Provided herein are compounds and methods for inhibiting histone deacetylase ("HDAC") enzymes (e.g., HDAC1, HDAC2, and HDAC3).
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WO/2018/140186A1 |
The disclosure provides a simple and efficient method for producing a compound of Formula I. The method includes treating an N-substitututed-4-nitro-phthalimide of Formula VII with sodium or potassium phenoxide to form an N-substituted-4...
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WO/2018/129046A1 |
Disclosed herein are methods for modifying ciliogenesis in one or more cells of a subject, the method comprising administering to the subject an effective amount of a composition comprising a Notch signaling inhibitor, wherein the modifi...
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WO/2018/119362A2 |
Provided herein are compounds and methods for inhibiting histone deacetylase ("HDAC") enzymes (e.g., HDAC1, HDAC2, and HDAC3).
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WO/2018/083051A1 |
The present invention provides compounds that are muscarinic M1 receptor positive allosteric modulators (PAM) and useful in the treatment of diseases, mediated by the muscarinic M1 receptor, such as Alzheimer's disease, cognitive impairm...
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WO/2018/069732A1 |
This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compo...
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WO/2018/067102A1 |
The invention relates to medical chemistry, in particular to the use of 7-bromo-5-(o-chlorophenyl)-3-propoxy-l,2-dihydro-3H-l,4-benz
odiazepin-2-one as a drug which inhibits neuropathic pain without the formation of defects in the gastri...
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WO/2018/044838A1 |
Methods for treating HIV in a human using combinations of: bictegravir and a maturation inhibitor, as well as compositions containing such compounds.
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WO/2018/044852A1 |
Methods for treating HIV in a human using combinations of: bictegravir and one two different maturation inhibitors are disclosed, as well as compositions containing such compounds are provided.
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