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WO/2022/003405A1 |
An industrial scale telescopic process for preparing (2S)-1-[N-(3-hydroxyadamantan-1-yl)glycyl]-2-pyrrolidinecarb
onitrile (Vildagliptin) of formula:, comprising: (a) reacting the compound of formula: with an excess of a compound of form...
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WO/2021/262627A1 |
Provided herein are methods of treating certain cancers comprising administering to the subject in need there of an effective amount of a compound of Formula (I) including stereoisomers and pharmaceutically acceptable salts thereof, wher...
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WO/2021/262483A1 |
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present inven...
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WO/2021/262541A1 |
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present d...
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WO/2021/260232A1 |
The present invention concerns a method for the preparation of an alkyne-linker-payload construct of structure Q-L-C (O)-NR3-D (1), comprising reacting (i) an alkyne compound of structure Q-L- C(O)-X (2), wherein Q is an alkyne moiety se...
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WO/2021/260721A1 |
The present invention relates to novel, economical processes for the preparation of enantiomerically pure Brivaracetam of Formula I having 99-100% diastereomeric excess (de) from its (R)-lactone intermediate that is (4R)-4-propyldihydrof...
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WO/2021/253306A1 |
A method for preparing DL-proline, comprising the following steps: mixing L-proline and glacial acetic acid, stirring and raising the temperature to 60-75°C, continuing to maintain the temperature and stir for 2-6 hours and then distill...
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WO/2021/253162A1 |
Provided is a preparation method for brivaracetam. The method has a synthetic route as shown below. The preparation method for the brivaracetam is simple, economical, environmentally friendly and suitable for industrialization.
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WO/2021/252644A1 |
The disclosure provides compounds of formula II with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provid...
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WO/2021/250355A1 |
The present invention relates to a composition for battery electrodes in which at least one solvent is a composition comprising between 80 and 95 % by mass of N-methylpyrrolidone (NMP).
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WO/2021/251086A1 |
A first problem addressed by the present invention is to provide an active-ray-sensitive or radiation-sensitive resin composition with which a pattern having a favorable form can be obtained. Further, a second problem addressed by the pr...
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WO/2021/250648A1 |
The invention relates to compounds of Formula (I'') wherein R, R1, R2, R3, p, q and q' are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient b...
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WO/2021/250174A1 |
The present invention relates to a process of manufacturing of (2S,5R)-5-(2- chlorophenyl)-1-(2'-methoxy-[1,1'-biphenyl]-4-carbonyl)pyrro
lidine-2-carboxylic acid (1), including the preparation of (2S,5R)-methyl 5-(2-chlorophenyl)pyrroli...
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WO/2021/245405A1 |
The present invention relates to compounds of Formula (I) that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process: Formula (I) wherein R1, R2, R3, R4, R6 and R10 are each as defined herein. ...
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WO/2021/242753A1 |
Mitochondrial targeting compounds for the treatment of cancer and other disorders associated with mitochondrial function, including diabetes, autoimmune diseases, inflammatory diseases, cardiovascular diseases and neurodegenerative disea...
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WO/2021/236449A1 |
Disclosed herein are p38a mitogen-activated protein kinase inhibitors, pharmaceutical compositions thereof, and therapeutic methods of using the p38a mitogen-activated protein kinase inhibitors.
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WO/2021/234449A1 |
New tetrahydrocannabinolic acid cocrystals are disclosed, in particular, a 1:1 tetrahydrocannabinolic acid L-proline cocrystal, a 1:1 tetrahydrocannabinolic acid D-proline cocrystal, a 1:1 tetrahydrocannabinolic acid D, L-proline cocryst...
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WO/2021/236971A1 |
A highly active and selective solid catalyst comprising stable single-atom iridium (Ir) anchored in a zeolite, e.g., ZSM-5, for upcycling of plastics, such as high-density polyethylene, to yield valuable lower molecular weight hydrocarbo...
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WO/2021/236771A1 |
The present disclosure related to compounds that can be useful as inhibitors of PD-1, PD-Ll or the PD-1/PD-Ll interaction. Also disclosed herein are pharmaceutical compositions of that can include a compound of Formula (I), or a pharmace...
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WO/2021/228000A1 |
The preparation of an aromatic heterocyclic derivative as an immunomodulator and the use thereof. Specifically, provided is a compound as represented by formula I below, or an optical isomer, a hydrate, a solvate, or a pharmaceutically a...
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WO/2021/223718A1 |
The present invention relates to the fields of pharmacochemistry and pharmacotherapy, and in particular relates to compounds of general formula I as 3CL protease inhibitors of SARS-CoV-2. At the same time, the compounds have significant ...
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WO/2021/226276A2 |
Provided are compounds of Formula (II): or a pharmaceutically acceptable salt thereof, wherein R1, n, and Y1 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a ph...
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WO/2021/223066A1 |
A raw material filtering device for pyromellitic dianhydride production, comprising a box body (1), a first support plate (21), a second support plate (23), a carrying frame (31), a filter screen (3), and an opening (32); wherein the fir...
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WO/2021/222858A1 |
Novel compounds that act as antagonists to human GPR39 protein are disclosed. Pharmaceutical compositions and methods of use for antagonists to human GPR39 protein are disclosed. In particular, methods of using the antagonists in the tre...
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WO/2021/218992A1 |
Disclosed are a substituted pyrrolidine compound and the use thereof in medicine. In particular, disclosed are a substituted pyrrolidine compound or a stereoisomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, a phar...
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WO/2021/217579A1 |
Disclosed is a method for preparing a brivaracetam intermediate shown in formula B-R, comprising: reacting a compound shown in formula B-P and a resolving agent to prepare a compound shown in formula B-Q; and converting the compound show...
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WO/2021/219661A1 |
The present invention relates to compounds showing pharmacological activity towards the subunit α2δof voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels. More particularly, the in...
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WO/2021/214727A1 |
Cancer stem cells are responsible for tumor recurrence, distant metastasis and drug-resistance, in the vast majority of cancer patients. There exists an urgent need to identify new mitochondrial inhibitor drugs that can target and eradic...
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WO/2021/217053A1 |
Provided herein are methods of treating an acute respiratory syndrome, non-cardiogenic pulmonary edema, viral infections, coronavirus disease 2019 (COVID-19), and/or systemic inflammatory response syndrome (SIRS) in the subject in need t...
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WO/2021/214278A2 |
The present invention relates to regioselective chemical and electrochemical processes for the preparation of an oxidized heterocyclic alpha-amino amide compounds. By applying specific catalysts or catalyst systems during chemical oxidat...
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WO/2021/214283A1 |
The present invention relates to a novel biocatalytic process for the stereoselective preparation of alpha amino amide compounds catalyzed by NHase enzymes. A further aspect of the invention relates to novel NHase enzymes as well as furt...
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WO/2021/216660A1 |
The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for dismption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.
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WO/2021/211913A1 |
Novel direct thrombin inhibitors are provided herein, along with methods for their use as anticoagulants. The direct thrombin inhibitors described herein are useful in treating and/or preventing thromboembolism and bleeding or clotting d...
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WO/2021/209490A1 |
The present disclosure relates to fungicidal active compounds, more specifically to cyclaminephenylaminoquinolines of formula (I), intermediates for their preparation and use thereof as fungicidal active compound, particularly in the for...
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WO/2021/210997A1 |
Water-soluble analogs of compounds intended for the treatment of neurological diseases, epilepsy, neuropathic pain and migraine, and psychiatric disorders, including anxiety and depression, especially suitable for the preparation of oral...
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WO/2021/206876A1 |
Compounds of Formula (I) and methods of inhibiting the replication of viruses in a biological sample or patient, of reducing the amount of viruses in a biological sample or patient, and of treating a virus infection in a patient, compris...
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WO/2021/204175A1 |
Provided herein are lipids that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid...
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WO/2021/202460A1 |
Compounds exhibiting antiviral activity and/or inhibition of viral replication against viruses, particularly those belonging to the picornavirus-like supercluster, including coronavirus having a formula: (I) where X comprises a cyclic mo...
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WO/2021/202781A1 |
Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein L, n, R1, R2, R6, R7, R8, R9, R10, X3, X4 and X5 are defined in the specification. This disclosure also relates to materials and methods for pre...
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WO/2021/197486A1 |
A novel spiro compound and an application thereof in a drug, in particular, use thereof as a drug for treating and/or preventing hepatitis B. Specifically, the present invention relates to a compound represented by formula (I) or a stere...
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WO/2021/202977A1 |
Disclosed are compounds of formula (I), and pharmaceutically acceptable salts thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the comp...
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WO/2021/201126A1 |
An amide compound represented by formula (I-1) or a salt thereof, a pharmaceutical composition that comprises the amide compound or a salt thereof, and a histone deacetylase inhibitor. In the formula: R1 to R4 independently represent a h...
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WO/2021/197303A1 |
Provided in the present invention are a method for preparing a long-chain fatty diacid monobenzyl ester. The method comprises: 1) subjecting a long fatty chain diacid to an esterification reaction in order to obtain a long fatty chain di...
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WO/2021/192488A1 |
The purpose of the present invention is to provide a method for producing an amide bond-containing compound with which an active acid raw material having an aromatic heterocycle to which a carbonyl group is bonded can be easily removed. ...
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WO/2021/195183A1 |
The invention provides compounds that are inhibitors of the protein embryonic ectoderm development (EED), pharmaceutical compositions, their use in modulating the activity of EED, and their use in the treatment of medical disorders, such...
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WO/2021/189143A1 |
There are provided isotope-enriched compounds containing stable heavy isotope-enriched amide functional groups for modulating the pharmacokinetic profile, metabolic profile, and/or delivery efficiency of a drug or prodrug, as well as its...
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WO/2021/185304A1 |
A method for preparing a long aliphatic chain diacid derivative. The method comprises: (1) performing a cyclization reaction on long aliphatic chain diacid, the long aliphatic chain diacid having a structure as shown in formula (A); (2) ...
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WO/2021/179049A1 |
The present invention relates to the treatment of disorders associated with oxidative stress including neuropathic pain and small synthetically derived compounds for treating such disorders.
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WO/2021/183542A1 |
Methods for making a dolastatin, auristatin or related compounds comprising the steps of providing a universal dolastatin core of Formula (I) reacting the C-terminal carboxylic acid group with an amine (A) to form an amide bond and react...
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WO/2021/183639A1 |
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof. The compounds, compositions, methods and kits of the invention are particularly useful for the treatment of itch and other dermal conditions.
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