30033-24-0Relevant articles and documents
BORON CLUSTER-COUPLED COMPOUND
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Paragraph 0271; 0273-0275, (2021/03/05)
To provide a novel boron-containing compound which increases intratumorous accumulation and tumor retention, and is efficiently taken into a tumor cell.SOLUTION: The present invention relates to a compound represented by formula (I) in the figure or a salt thereof. [In the formula, X represents a divalent to pentavalent organic group; Y represents a linker structure; R represents a monovalent group comprising boron clusters; and n represents 2, 3, 4 or 5.SELECTED DRAWING: None
LIQUID COMPOSITIONS COMPRISING A LEVODOPA AMINO ACID CONJUGATE AND USES THEREOF
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Page/Page column 80, (2021/03/13)
Disclosed herein are liquid pharmaceutical formulations comprising levodopa amino acid conjugates that may further comprise a decarboxylase inhibitor, such as carbidopa, an antioxidant, a solvent, or any other pharmaceutically acceptable excipient. Further disclosed are methods of treating generative conditions and/or conditions characterized by reduced levels of dopamine in the brain, such as Parkinson's disease, comprising administering the disclosed liquid pharmaceutical formulations. Disclosed also are LDAA conjugate compounds.
PROTAC targeting the degradation of tyrosinase and its applications
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Paragraph 0040; 0060-0065, (2021/12/07)
The present invention relates to PROTAC targeting tyrosinase and its applications, belonging to the technical field of new raw materials for skin whitening cosmetics and skin disease treatment drugs. The technical problem solved by the present invention is to provide a compound using PROTAC targeting the degradation of tyrosinase and its salts, prodrugs, hydrates or solvates. The PROTAC molecule, whose structural formula is shown in formula I. The present invention by different types, different chain lengths of the linker will be tyrosinase ligand and E3 ligase ligand coupling, successfully prepared a series of targeted tyrosinase PROTAC molecules, can effectively target the target protein, and reduce the content of tyrosinase in the cell, while having a good in vitro reducing melanin effect, low toxicity to normal cells, in line with the characteristics of high efficiency and low toxicity.
COMPOSITIONS AND METHODS FOR THE TREATMENT OF PAIN AND DEPENDANCE DISORDERS
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Paragraph 00279, (2021/02/12)
Provided herein are (e.g., controlled release) compositions for the treatment of acute or chronic diseases or disorders. Described herein are processable opioid conjugates. Also described herein are compositions and methods for the treatment of central nervous system (CNS) diseases or disorders including chronic pain (e.g., cancer pain), acute pain, opioid addiction, alcohol addiction, alcohol dependence, opioid-induced constipation, and narcotic depression. Said compositions and methods comprise opioid agonists and/or opioid antagonists, which demonstrate CNS activity and/or other desirable activities. Injection of said compositions subcutaneously or intraspinally provides therapeutic benefit to individuals suffering from CNS diseases or disorders
Delivery of a system xc?inhibitor by a redox-responsive levodopa prodrug nanoassembly for combination ferrotherapy
Chen, Yuan,Huang, Yong,Li, Bowen,Ping, Yuan,Tang, Honglin,Xia, Hongguang,Xin, Huhu,Zhang, Fu
supporting information, p. 7172 - 7181 (2021/09/22)
A comprehensive understanding of ferroptosis signaling pathways significantly contributes to the advances in cancer ferrotherapy. Herein, we constructed a self-assembled prodrug nanosystem targeting system xc?, a key regulator for ferroptosis, to amplify the therapeutic efficacy of cancer ferrotherapy. The prodrug nanosystem is assembled between sulfasalazine (SSZ, a ferroptosis resistance inhibitor) and disulfide-bridged levodopa (DSSD) that can chelate Fe2+ions to form SSZ-Fe2+@DSSD, and the resulting nanoassembly can not only inhibit ferroptosis resistance, but also generate ROS in the tumor microenvironment. Whereas the prodrug nanosystem is stable in the physiological environment, it becomes unstable in the tumoral and intracellular reductive microenvironment, where the disulfide linkers are disrupted by high levels of glutathione (GSH), triggering the release of active Fe2+and SSZ. Under the Fenton reaction, the released Fe2+thus can induce ferroptosis, which is amplified by SSZ-mediated inhibition of ferroptosis resistance to synergistically improve the therapeutic efficacy of ferroptosis. Our study thus provides an innovative prodrug strategy to advance anticancer ferroptosis.
An alternative approach to the synthesis of the three fragments of anachelin H
Gamba-Sánchez, Diego,Garzón-Posse, Fabián,Prunet, Jo?lle
, p. 2702 - 2715 (2020/04/17)
The synthesis of the fully protected peptide, polyketide and alkaloid fragments of anachelin H is presented. The peptide fragment was prepared using a liquid phase peptide synthesis; the polyketide fragment was synthetized using a cross metathesis and an intramolecular oxa-Michael reaction as the key steps to introduce the desired stereochemistry; finally, the alkaloid fragment was obtained by an oxidative cyclization of a catechol derivative using potassium ferricyanide. The synthesis of all fragments was based on the use of natural amino acids as sources of asymmetry. The independent synthesis of the three fragments should allow more efficient biological studies on the fragments instead of the whole natural product. Experiments to illustrate the coupling of fragments and the effectiveness of the convergent strategy are also described.
PANTETHEINE DERIVATIVES AND USES THEREOF
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Paragraph 2121, (2020/06/19)
The present disclosure relates to compounds of Formula (I), (II), or (II'): (I), (II), (II'), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.
Water-soluble L-DOPA esters
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Paragraph 0103, (2018/05/24)
The present invention relates to novel compounds of the formula I, methods for their preparation and their use for treatment of diseases. The invention discloses the synthesis of levodopa (L-DOPA) esters by coupling polyhydroxy compounds or their derivatives to the L-DOPA carboxyl group. The synthesis allows to produce L-DOPA derivatives which are highly soluble in water as well as aqueous and biocompatible liquids and have an improved hydrolytic stability in water or aqueous and biocompatible media for an application over several days. The invention helps producing L-DOPA substances for applications in the fields of medicine, biology and medical engineering as well as in the pharmaceutical industry.
Nitrogen (oxygen) heterocyclic pentane - 2 - one (thione) compound, pharmaceutical composition, preparation method and use thereof
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Paragraph 0091; 0092, (2017/08/25)
The invention belongs to the field of pharmacology, and relates to aza (oxa)-cyclopentane-2- ketone (thione) compounds shown in the formula I, medicine compositions thereof, a preparation method, applications in preparation of medicines treating diabetes and glucolipid metabolism, and especially applications in preparation of medicines treating II-type diabetes.
MULTIMODAL CONTRAST AND RADIOPHARMACEUTICAL AGENT FOR AN IMAGING AND A TARGETED THERAPY GUIDED BY IMAGING
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Page/Page column 36, (2013/06/05)
The present invention relates to a multimodal contrast and radiopharmaceutical agent for an imaging and a targeted therapy guided by imaging.