- Derivatives of pyrazinecarboxylic acid: 1H, 13C and 15N NMR spectroscopic investigations
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NMR spectroscopic studies are undertaken with derivatives of 2-pyrazinecarboxylic acid. Complete and unambiguous assignment of chemical shifts (1H, 13C, 15N) and coupling constants (1H,1H; 13C,1H; 15N,1H) is achieved by combined application of various 1D and 2D NMR spectroscopic techniques. Unequivocal mapping of13C,1H spin coupling constants is accomplished by 2D (S,J) long-range INEPT spectra with selective excitation. Phenomena such as the tautomerism of 3-hydroxy-2-pyrazinecarboxylic acid are discussed.
- Holzer, Wolfgang,Eller, Gernot A.,Datterl, Barbara,Habicht, Daniela
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- Hydrothermal synthesis of 3D Copper(II)-Organic Frameworks: In situ Formation of 3-Hydroxopyrazine-2-carboxylate from 3-Aminopyrazine-2-carboxylic acid
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Themetal organic framework, [Cu5(C5H 2N2O3)4(H2O)4(NO3) 2· 10H2O]n (1), was synthesized by a hydrothermal reaction via copper nitrate and in situ generated 3-hydroxopyrazine-2- carboxylate from 3- aminopyrazine-2-carboxylic acid. Compound 1 was characterized by elemental analysis, infrared spectroscopy, TG analysis, and singlecrystal X-ray diffraction. It has a 3D structure constructed from Cu2+ cations, bridging NO3 anions, and 3-hydroxopyrazine-2-carboxylate units. The NO3 - anions act as μ2-bridging ligand and the 3-hydroxopyrazine- 2-carboxylate units coordinate pentadentately through the two oxygen atoms of their carboxylate group, the oxygen atom of the hydroxyl group and two nitrogen atoms. The ligands link the CuII ions to form trinuclear units. These are further connected to form a novel 3D MOF, with a novel 4-nodal 3,3,3,4-connected net topology of an unprecedented point (Schla?fli) symbol (6.7.9)(64.8.9)(7.102)(72.10).
- Dehghanpour, Saeed,Jahani, Khadijeh,Mahmoudi, Ali,Babakhodaverdi, Mogtaba,Tabatabaei, Robabehsadat,Notash, Behrouz
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- USE OF MORPHINAN DERIVATIVES FOR TREATMENT OF OPIOID RECEPTOR AGONIST-RELATED DISEASES
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The present invention relates to a pharmaceutical composition comprising a morphinan derivative that exhibits an opioid δ receptor agonist activity. By administering the pharmaceutical composition provided by the present invention, opioid δ receptor-related diseases (for example, headache) can be treated or prevented.
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Paragraph 0163; 0164; 0165
(2019/08/01)
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- MORPHINAN DERIVATIVE
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A morphinan derivative represented by the following general formula (I): (wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc., R2 represents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group, Y binds to a carbon atom as a ring-constituting atom of R2, R3, R4, and R5 represent hydrogen; hydroxy, etc., R6a and R6b represent hydrogen, etc., R7 and R8 represent hydrogen, etc., R9 and R10, which are the same or different, represent hydrogen, etc., X represents O or CH2, and Y represents C(=O)), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.
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Paragraph 0180; 0181; 0182
(2018/03/02)
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- Alkylamino derivatives of N-benzylpyrazine-2-carboxamide: synthesis and antimycobacterial evaluation
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A series of alkylamino derivatives of N-benzylpyrazine-2-carboxamide was designed, synthesized and assayed in vitro for their antimycobacterial, antibacterial, antifungal as well as antiviral activities. Final structures were prepared from 6-chloro (1), 5-chloro (2) or 3-chloro (3) derivatives of N-benzylpyrazine-2-carboxamide by nucleophilic substitution of chlorine with n-alkylamines in the range from butylamine to octylamine (labelled a-e). Series 1a-e and 2a-e exerted higher activity against Mycobacterium tuberculosis H37Rv compared to the corresponding pattern compounds and the reference compound pyrazinamide. The most active derivatives reached an activity MIC = 4.6-10 μM (M. tbc H37Rv). More importantly, activity was also observed against other tested mycobacterial strains (including drug-resistant strains). Substitution of 3-chlorine was disadvantageous and led to completely inactive compounds 3a-e. Some compounds showed activity against Gram-positive bacterial strains (including MRSA) or influenza virus, but no antifungal activity was observed.
- Servusova-Vanaskova, Barbora,Jandourek, Ondrej,Paterova, Pavla,Kordulakova, Jana,Plevakova, Magdalena,Kubicek, Vladimir,Kucera, Radim,Garaj, Vladimir,Naesens, Lieve,Kunes, Jiri,Dolezal, Martin,Zitko, Jan
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p. 1311 - 1317
(2015/07/15)
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- ALPHA 7 NICOTINIC ACETYLCHOLINE ALLOSTERIC MODULATORS, THEIR DERIVATIVES AND USES THEREOF
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The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
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Page/Page column 44; 45
(2013/12/03)
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- NEW CHEMICAL COMPOUNDS
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The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
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Page/Page column 35-36
(2012/04/23)
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- NITROGEN- HETEROCYCLIC COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS
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Aryl- and heteroaryl-nitrogen heterocyclic compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDEIO, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
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Page/Page column 62
(2011/12/02)
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- HETEROCYCLIC CARBOXYLIC ACID AMIDES AS PDK1 INIHIBITORS
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The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
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Page/Page column 65
(2011/11/06)
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- 1H - IMIDAZO [4, 5 - C] QUINOLINES
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The present invention encompasses compounds of general formula (1), wherein the groups R1 to R7, Qa, Qb, L, n and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations containing such compounds and their use as medicaments.
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Page/Page column 58
(2011/12/04)
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- Synthesis of 2′-C-methyl ribonucleoside analogues with modified heterocyclic base moieties
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Recently, 2′-C-methyl nucleoside analogues have been reported to exhibit potent anti-hepatitis C virus (HCV) activity through inhibition of HCV RNA replication without significant cytotoxicity. As a part of our continuous efforts of searching for novel antiviral agents, we now report the synthesis of heterobase-modified 2′-C-methyl ribonucleoside analogues. Copyright Taylor & Francis Group, LLC.
- Kim, Myong Jung
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experimental part
p. 2988 - 2999
(2010/11/05)
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- NEW CHEMICAL COMPOUNDS
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The present invention encompasses compounds of general formula (1) wherein the units W, A, L, Q1 and QH are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use as medicaments having the above-mentioned properties.
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Page/Page column 104-105
(2010/04/03)
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- Heterocyclic mutilin esters and their use as antibacterials
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Pleuromutilin compounds of the formula: 1are of use in anti-bacterial therapy.
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- Synthesis of regioisomeric 6,9-(chlorofluoro)-substituted benzo[g]quinoline-5,10-diones, benzo[g]isoquinoline-5,10-diones and 6-chloro-9-fluorobenzo[g]quinoxaline-5,10-dione
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Treatment of difluoro or chloro fluoro-substituted benzyl bromides 5a-c with zinc dust in tetrahydrofuran leads to the corresponding benzylic zinc bromides 6a-c. These organometallics on treatment with chlorosubstituted heterocyclic esters 4A and 4B mediated by nickel catalysis undergo couplings to yield dihalobenzyl substituted heterocyclic esters 7Aa-c and 7Ba-c. Treatment of 4c with 6c under Pd catalysis leads to 7Cc. The acids 8, prepared by hydrolysis of these esters, with treatment of fuming sulfuric acid undergo cyclizations and oxidations to yield the desired regioisomeric dihalo-substituted heterocyclic quinones 2.
- Krapcho, A. Paul,Gallagher, Cynthia E.,Hammach, Abdelhakim,Ellis, Michael,Menta, Ernesto,Oliva, Ambrogio
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