- CHEMICAL COMPOUNDS
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The present disclosure describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the disclosure have activity as Janus kinase (JAK) inhibitors and are useful in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described herein are methods of treating inflammation, auto-immune diseases, cancer, and other conditions susceptible to inhibition of JAK by administering a compound herein described.
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Paragraph 0179-0181
(2021/04/02)
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- IMIDAZOPYRIDINE DERIVATIVE COMPOUNDS AND USE OF SAME
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One aspect of the present invention provides a compound selected from among a compound of chemical formula 1 having lysine-specific demethylase-1 (LSD1) inhibitory activity, and a tautomer, a stereoisomer, and a solvate thereof, and pharmaceutically accep
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- Preparation method of cycloalkane compound
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The invention provides a preparation method of a cycloalkane compound, and concretely provides a new cycloalkane construction method for preparing a compound represented by formula I. The preparationmethod is green and environment-friendly.
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Paragraph 0192-0195
(2020/06/16)
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- PYRAZOLE DERIVATIVE COMPOUND AND USE THEREOF
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Provided is a compound represented by Formula 1 having an inhibitory activity on lysine-specific demethylase-1 (LSD1), an optical isomer, a solvate, a tautomer, or a pharmaceutically acceptable salt thereof, which is effective in preventing or treating a
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- Cu(II)-Mediated N-H and N-Alkyl Aryl Amination and Olefin Aziridination
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Cu(II)-mediated direct NH2 and NH alkyl aryl aminations and olefin aziridinations are described. These room-temperature, one-pot, environmentally friendly procedures replace costly Rh2 catalysts and, in some instances, display important differences with comparable Rh2- and Fe-supported reactions.
- Munnuri, Sailu,Anugu, Raghunath Reddy,Falck, John R.
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supporting information
p. 1926 - 1929
(2019/03/11)
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- TYK2 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
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- IMMUNOREGULATORY AGENTS
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Compounds that modulate the oxidoreductase enzyme indoleamine 2,3- dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases,
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Paragraph 0282
(2016/06/01)
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- Metal Nanoparticles Catalyzed Selective Carbon-Carbon Bond Activation in the Liquid Phase
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Understanding the C-C bond activation mechanism is essential for developing the selective production of hydrocarbons in the petroleum industry and for selective polymer decomposition. In this work, ring-opening reactions of cyclopropane derivatives under hydrogen catalyzed by metal nanoparticles (NPs) in the liquid phase were studied. 40-atom rhodium (Rh) NPs, encapsulated by dendrimer molecules and supported in mesoporous silica, catalyzed the ring opening of cyclopropylbenzene at room temperature under hydrogen in benzene, and the turnover frequency (TOF) was higher than other metals or the Rh homogeneous catalyst counterparts. Comparison of reactants with various substitution groups showed that electron donation on the three-membered ring boosted the TOF of ring opening. The linear products formed with 100% selectivity for ring opening of all reactants catalyzed by the Rh NP. Surface Rh(0) acted as the active site in the NP. The capping agent played an important role in the ring-opening reaction kinetics. Larger particle size tended to show higher TOF and smaller reaction activation energy for Rh NPs encapsulated in either dendrimer or poly(vinylpyrrolidone). The generation/size of dendrimer and surface group also affected the reaction rate and activation energy.
- Ye, Rong,Yuan, Bing,Zhao, Jie,Ralston, Walter T.,Wu, Chung-Yeh,Unel Barin, Ebru,Toste, F. Dean,Somorjai, Gabor A.
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p. 8533 - 8537
(2016/07/26)
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 42
(2013/10/22)
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EPl receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EPl receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EPl receptor as well as to pharmaceutical compositions comprising them.
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- Tricyclic Compounds As mPGES-1 Inhibitors
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The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
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Page/Page column 39
(2012/05/07)
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- N-acylaminophenylcyclopropanes in reaction with nitrous acid generated in situ
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The reaction of N-acylaminophenylcyclopropanes with HNO2 proceeds regioselectively with introduction of an N=O fragment into the three-membered ring and formation of the corresponding Δ2-isoxazolines. For ortho-substituted N-acylaminophenylcyclopropanes side processes were observed, caused by the intramolecular participation of the N-acyl group in conversions of the carbenium ions formed on opening the cyclopropane ring under the action of the nitrosating reagent, and by direct insertion of the modified ortho substituent into the three-membered ring.
- Mochalov,Gazzaeva,Kadzhaeva,Fedotov,Trofimova
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p. 1415 - 1429
(2014/07/21)
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- PYRAZOLE DERIVATIVES AS ANTI-PLATELET AND ANTI-THROMBOTIC AGENTS
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This invention relates to novel compounds of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof wherein Y, R1 through R9, and X1 through X7 are as defined in the specification, pharmaceutical compositions containing said compounds useful as P2Y1 antagonists, and to methods of treating thromboembolic disorders.
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Page/Page column 62
(2010/11/30)
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- Preparation, antimicrobial evaluation, and mutagenicity of [2- hydroxyaryl]-[1-methyl-5-nitro-1H-2-imidazolyl]methanols, [5-tert-butyl-2- methylaminophenyl]-[1-methyl-5-nitro-1H-2-imidazolyl] methanol, and [2- hydroxyaryl]-[1-methyl-5-nitro-1H-2-imidazolyl] ketones
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Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field.
- Arredondo,Moreno-Manas,Pleixats,Palacin,Raga,Castello,Ortiz
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p. 1959 - 1968
(2007/10/03)
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- Synthesis of Certain Mesogenic Azomethines Derived from 4-Cycloalkylanilines and from 4-Cycloalkylbenzaldehydes
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General procedures are described for the synthesis of members of five pairs of related homologous series of mesogenic azomethines differing in the mode of linkage of the CH=N group and containing a cycloalkyl group in a terminal position.
- Byron, D. J.,Matharu, A. S.,Rees, M.,Wilson, R. C.
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p. 229 - 238
(2007/10/02)
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- Electron transfer in P450 mechanisms. Microsomal metabolism of cyclopropylbenzene and p-cyclopropylanisole
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The metabolism of cyclopropylbenzene (1a) and 4-cyclopropylanisole (1b) was studied using liver microsomal preparations from control, phenobarbital- and β-naphthoflavone treated rats. With all three types of microsomes 1a was metabolized by benzylic hydroxylation to give 1-phenylcyclopropanol and by aromatic hydroxylation at C-4; the former predominated by a factor of 2-4. BNF-induced microsomes also formed 2-cyclopropylphenol. No cyclopropyl ring-opened metabolites of 1a, including benzoic acid, were detected in any of the incubations. With PB-induced microsomes 1b underwent O-demethylation (90%) and benzylic hydroxylation; no other metabolites were detected. Progress curves for metabolism of 1a are markedly nonlinear after only limited conversion of substrate, suggesting the possibility that 1a, like other cyclopropyl compounds, could be a suicide substrate for one or more isozymes of P450. For both 1a and b, metabolite formation and enzyme inactivation can be explained by conventional P450 reaction mechanisms not involving electron abstraction.
- Riley,Hanzlik
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