- Synthesis of Electron-Deficient Oxetanes. 3-Azidooxetane, 3-Nitrooxetane, and 3,3-Dinitrooxetane
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A facile synthesis of 3-hydroxyoxetane is described and is based on the addition of acetic acid to epichlorohydrin, protection of the resulting primary alcohol as an acetal, basic acetate hydrolysis and ring closure, and removal of the protecting group. 3-Azidooxetane was prepared from 3-(tosyloxy)oxetane and sodium azide.Reduction of the azide with triphenylphosphine or hydrogen gave 3-aminooxetane, and oxidation of the amine with m-chloroperbenzoic acid gave 3-nitrooxetane.Oxidative nitration or reaction with tetranitromethane gave 3,3-dinitrooxetane. 3-Azidooxetane and 3,3-dinitrooxetane were polymerized with Lewis acids.
- Baum, Kurt,Berkowitz, Phillip T.,Grakauskas, Vytautas,Archibald, Thomas G.
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Read Online
- A GAP Replacement: Improved Synthesis of 3-Azidooxetane and Its Homopolymer Based on Sulfonic Acid Esters of Oxetan-3-ol
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In the field of energetic binders, only hydroxy-terminated glycidyl azide polymer (GAP) has found widespread application and prevailed in the market. However, oxiranes such as glycidyl azide (GA) allow two ring-opening modes during polymerization and thus
- Born, Max,Karaghiosoff, Konstantin,Klap?tke, Thomas M.
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supporting information
p. 12607 - 12614
(2021/09/18)
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- Fused tricyclic derivative as FGFR4 inhibitor
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The present invention provides a fused tricyclic derivative that is the selective inhibitor of fibroblast growth factor receptor 4 (FGFR4), a pharmaceutical composition containing the compound, a method of making the compound and a method of treating cell proliferative diseases, such as cancer, using the compounds of the invention.
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Paragraph 0906-0911
(2021/05/12)
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- AZA-QUINOLINE COMPOUNDS AND USES THEREOF
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Provided aza-quinoline compounds of Formula (I), pharmaceutical compositions comprising such compounds; and the use of such compounds for treating a disease or condition mediated by Enhancer of Zeste Homolog 2 (EZH2), Polycomb Repressive Complex 2 (PRC2), or a combination thereof.
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Page/Page column 66
(2021/04/02)
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- Compounds and their use in treatment on hepatitis B
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The invention provides compounds, a pharmaceutical composition containing the compounds and an application of the compounds. The compound is a compound shown in a formula (I) or a stereoisomer, a tautomer, nitric oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug of the compound shown in the formula (I). The compound provided by the invention can interfere with the shell assembly process of hepatitis B virus, thereby inhibiting hepatitis B virus replication. Moreover, the compound has good absorption, relatively high biological activity and availability and low toxicity, particularly has relatively strong stability in vivo, is not easy to decompose and has long drug effect time, so that an effect of treating hepatitis B is achieved and the compound has a goodapplication prospect.
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Paragraph 0171-0173
(2020/07/15)
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- 8-substituted styryl xanthine derivative and application thereof
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The invention discloses an 8-substituted styryl xanthine derivative and application thereof, and particularly relates to a novel 8-substituted styryl xanthine derivative and a pharmaceutical composition containing the compound, and the 8-substituted styryl xanthine derivative can be used as a selective adenosine A2A receptor antagonist. The invention also relates to a method for preparing the compound and the pharmaceutical composition, and application of the compound and the pharmaceutical composition in preparation of drugs for treating adenosine A2A receptor related diseases, especially Parkinson's disease.
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Paragraph 0268; 0270-0272
(2020/05/01)
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- Nitrogen-containing fused tricyclic derivative and application thereof
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The invention discloses a nitrogen-containing fused tricyclic derivative and application thereof, and particularly relates to a novel nitrogen-containing fused tricyclic derivative and a pharmaceutical composition containing the nitrogen-containing fused tricyclic derivative, and the nitrogen-containing fused tricyclic derivative can be used as a selective adenosine A2A receptor antagonist. The invention also relates to a method for preparing the compound and the pharmaceutical composition and application of the compound and the pharmaceutical composition in preparation of drugs for treating adenosine A2A receptor related diseases, especially Parkinson's disease.
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Paragraph 0238; 0240-0242
(2020/05/08)
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- BICYCLIC AND TRICYCLIC COMPOUNDS
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Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
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Paragraph 0265
(2020/10/28)
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- QUINAZOLINE DERIVATIVE AND USE THEREOF
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The present invention relates to a series of quinazoline compounds, especially compounds as represented by formula (I), isomers thereof or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and use thereof as Pan-HER tyrosine kinase inhibitors.
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Paragraph 0192-0194
(2020/11/26)
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- 2 Tyrosine kinase mediated signal transduction inhibitors
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Disclosed herein are compounds of Formula (), and pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, X, X, X, X, X, and n are as defined herein, pharmaceutical compositions comprising same, and methods of preparation and use.
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Paragraph 0491; 0492; 0493
(2019/09/17)
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- Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865)
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The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective positive allosteric modulators (PAMs) for the GABAA ligand-gated ion channel are described. From a set of initial hits multiple subseries were designed and evaluated based on binding affinity and functional activity. As designing in the desired level of functional selectivity proved difficult, a probability-based assessment was performed to focus the project's efforts on a single subseries that had the greatest odds of delivering the target profile. These efforts ultimately led to the identification of two precandidates from this subseries, which were advanced to preclinical safety studies and subsequently to the identification of the clinical candidate PF-06372865.
- Owen, Robert M.,Blakemore, David,Cao, Lishuang,Flanagan, Neil,Fish, Rebecca,Gibson, Karl R.,Gurrell, Rachel,Huh, Chan Woo,Kammonen, Juha,Mortimer-Cassen, Elisabeth,Nickolls, Sarah A.,Omoto, Kiyoyuki,Owen, Dafydd,Pike, Andy,Pryde, David C.,Reynolds, David S.,Roeloffs, Rosemarie,Rose, Colin,Stead, Clara,Takeuchi, Mifune,Warmus, Joseph S.,Watson, Christine
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supporting information
p. 5773 - 5796
(2019/05/15)
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- PYRROLO[2,3-C]PYRIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF IN MEDICINE
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Disclosed are a pyrrolo[2,3-c]pyridine derivative, a preparation method therefor, and use thereof in medicine. Specifically, disclosed are a pyrrolo[2,3-c]pyridine derivative as represented by general formula (1), a preparation method therefor, a pharmaceutical composition comprising the derivative, as well as use thereof as a BRD4 inhibitor in the treatment of related diseases such as cancers, inflammations, chronic liver diseases, diabetes, cardiovascular diseases and AIDS, each substituent in general formula (I) being same as defined in the description.
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Page/Page column 119
(2018/08/03)
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- CATHEPSIN K INHIBITOR AND APPLICATION THEREOF
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The invention relates to capthepsin K inhibitors and uses thereof, specifically relates to a class of compounds having the formula (I) which are used for treating or preventing cathepsin dependent diseases or conditions, specifically, wherein the cathepsin is capthepsin K. The compounds and compositions thereof can be used as bone resorption inhibitors for the treatment of associated diseases.
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Paragraph 0293
(2018/07/29)
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- HETEROCYCLIC COMPOUNDS AND USE THEREOF AS MODULATORS OF TYPE III RECEPTOR TYROSINE KINASES
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Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFRβ kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
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Paragraph 0974
(2016/08/03)
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- Five-And-Six-Membered Heterocyclic Compound, And Preparation Method, Pharmaceutical Composition And Use Thereof
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A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, pharmaceutical composition, and use thereof; the five-and-six-membered heterocyclic compound has activity as a Janus kinase (JAK) inhibitor, and can be used to prepare drugs for treating diseases caused by the abnormal activity of kinase, such as cell proliferation diseases like cancer.
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Paragraph 0290; 0291
(2015/12/07)
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- GAMMA SECRETASE INHIBITORS
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Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing t
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Page/Page column 33
(2012/10/18)
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- DIOXA-BICYCLO[3.2.1.]OCTANE-2,3,4-TRIOL DERIVATIVES
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Compounds of Formula (I) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).The compounds disclosed herein are useful for the prevention and treatment of obesity and its associated co-morbidities, inn particular type Il (type 2) diabetes.
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Page/Page column 34
(2010/04/06)
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- NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME
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Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R4 is —(CH2)n-Z-(CH2)m—PO(OR7)(OR8), —(CH2)nZ-(CH2)m—PO(OR7)Rg, —(CH2)n-Z-(CH2)m—OPO(OR7)Rg, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10);R5 and R6 are independently selected from H, alkyl and halogen;Y is R7(CH2)s or is absent; andX, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
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Page/Page column 82
(2008/06/13)
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- Preparation of aryloxetanes and arylazetidines by use of an alkyl-aryl suzuki coupling
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(Chemical Equation Presented) The oxetan-3-yl and azetidin-3-yl substituents have previously been identified as privileged motifs within medicinal chemistry. An efficient approach to installing these two modules into aromatic systems, using a nickel-mediated alkyl-aryl Suzuki coupling, is presented.
- Duncton, Matthew A. J.,Estiarte, M. Angels,Tan, Darlene,Kaub, Carl,O'Mahony, Donogh J. R.,Johnson, Russell J.,Cox, Matthew,Edwards, William T.,Wan, Min,Kincaid, John,Kelly, Michael G.
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experimental part
p. 3259 - 3262
(2009/05/07)
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- 2-Heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1-isoxazolyl, R1-oxadiazolyl, R1-dihydrofuranyl, R1-pyrazolyl, R1-imidazolyl, R1-pyrazinyl or R1-pyrimidinyl; R1 is 1, 2 or 3 substituents selected from H, alkyl, alkoxy and halo; Z is optionally substituted-aryl, or optionally substituted-heteroaryl; are disclosed, as well as their use in the treatment of central nervous system diseases, in particular Parkinson's disease and Extra Pyramidal Syndrome, pharmaceutical compositions comprising them, and combinations with other agents.
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Page/Page column 14
(2008/06/13)
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- Preparation and Characterization of Side-Chain Liquid-Crystalline Polyoxetanes Anchoring a Pendant Spacer-Separated Mesogen at the Tertiary-Like C-3 Carbon of the Oxetane Unit
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Polyoxetanes anchoring a pendant spacer-separated mesogen at the tertiary-like C-3 carbon of the oxetane unit were prepared by cationic ring-opening polymerization of the corresponding oxetane derivatives. The resulting polymers were liquid-crystalline substances showing textures assignable to the nematic or smectic mesophase over a wide temperature range from about 260 ° C to room temperature. These mesogens also behaved in the manner similar to that of the mesogens in the analogous polyoxetanes attached by a methyl side chain at the quaternary C-3 carbon, although the less bulky polymer backbone in the present work indicated a somewhat higher Isotropic phase-transition temperature than that of the methyl-substituted analogs. In both types of the polyoxetanes, their mesophase patterns were influenced by the core structure and alkoxy tail length in the pendant mesogen, but not by the bulkiness of the second side chains, H and CH3, attached at the C-3 carbon of the polyoxetane unit.
- Ogawa, Hiroshi,Kodera, Yasutake,Kanoh, Shigeyoshi,Ueyama, Akihiko,Motoi, Masatoshi
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p. 433 - 442
(2007/10/03)
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