- NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
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The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.
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Paragraph 0362-0363; 0368
(2021/11/04)
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- Novel hydrazone derivatives comprising aryl or heteroaryl group substituted at terminal amine and use thereof
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The present invention relates to novel hydrazone derivatives with an aryl or heteroaryl group substituted at a terminal amine group thereof and a use thereof.
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Paragraph 1702; 1708; 1709; 1730; 1732-1734
(2020/08/28)
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- Replacement of the Benzylpiperidine Moiety with Fluorinated Phenylalkyl Side Chains for the Development of GluN2B Receptor Ligands
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The 4-benzylpiperidine moiety is a central structural element of potent N-methyl-d-aspartate (NMDA) receptor antagonists containing the GluN2B subunit. To obtain novel GluN2B ligands suitable for positron emission tomography, the benzylpiperidine moiety was replaced with fluorinated ω-phenylalkylamino groups. For this purpose three primary propyl- and butylamines 7 a–c and one butyraldehyde 7 d bearing a fluorine atom and an ω-phenyl moiety were prepared in 3- to 7-step syntheses. Compounds 7 a–d were attached to various scaffolds of potent GluN2B antagonists (scaffold hopping) instead of the original 4-benzylpiperidine moiety. Although benzoxazol-2-ones and indoles with a benzylpiperidine moiety show high GluN2B affinity, the corresponding fluorophenylalkylamine derivatives did not result in high Glu2B affinity. Moderate GluN2B affinity was observed for a 3-(fluoroalkyl)-substituted tetrahydro-1H-3-benzazepine (Ki=239 nm). However, high GluN2B affinity was obtained for the tetrahydro-5H-benzo[7]annulen-7-amines 12 a–c (Ki=17–30 nm). Docking studies resulted in the same binding pose for 12 a as for the lead compound Ro 25-6981. It can be concluded that some GluN2B ligands (benzoxazolones, indoles) do not tolerate replacement of the 4-benzylpiperidine moiety with flexible fluorinated phenylalkyl side chains, but other scaffolds such as tetrahydro-3-benzazepines and -benzo[7]annulenes retain interaction with NMDA receptors containing the GluN2B subunit.
- Thum, Simone,Schepmann, Dirk,Kalinin, Dmitrii V.,Ametamey, Simon M.,Wünsch, Bernhard
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p. 2522 - 2529
(2018/11/23)
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- Novel Compounds as Autotaxin Inhibitors and Pharmaceutical Compositions Comprising the Same
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The present invention relates to a novel autotaxin inhibitor compound for preventing and treating disease or symptoms due to an increase in concentration of lysophosphatidic acid or activation of autotaxin. The present invention further relates to a pharmaceutical composition containing the same. The novel compound of the present invention is an autotaxin inhibitor which inhibits production of lysophosphatidic acid, and thus is useful for treating or preventing cardiovascular disease, cancer, metabolic disease, kidney disease, liver disease, inflammatory diseases, nervous disease, respiratory disease, desmoid disease, eye disease, cholestatic symptoms, other types of chronic pruritus or acute, or chronic rejection of transplanted organs.COPYRIGHT KIPO 2017
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Paragraph 0541-0542; 0551-0552; 0747-0750
(2018/05/17)
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- Comparative study of conventional and microwave-assisted synthesis of novel 6-(arylideneamino)benzo[d]oxazol-2(3H)-ones with potential antibacterial activity
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(Formula presented) The synthesis and characterization of novel class of Schiff bases derivatives 6-(Benzylideneamino)benzo[d]oxazol-2(3H)-ones (5a-d and 6a-d), derived from the condensation reactions of different aromatic aldehydes with 6-amino-2(3H)-benzoxazolone and 3-methyl-6-amino-2(3H)-benzoxazolone, using conventional and microwave irradiation methods was described. The structure of all newly synthesized compounds has been proven by using various spectral methods such as IR, 1H-NMR and 13C-NMR. The results confirmed that benzoxazolinonic amino group reacted with aromatic aldehydes to form the desired Schiff bases.
- Adjeroud, Yasmina,Chabane, Hanane,Liacha, Messaoud
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p. 111 - 117
(2016/07/15)
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- Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents
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The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
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Page/Page column 312
(2015/11/16)
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- Experimental and theoretical investigation of the intramolecular cyclisation of N-(benzoxazolinon-6-Yl) Maleimide derivatives
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A new N-H and N-CH3 2(3H)-benzoxazolones substituted at the C6 position in the aromatic ring by imide group (maleimides) has been synthesized in good yields. The regioselectivity of the cyclisation step has been investigated through DFT calculations at the B3LYP/6-31G (d,p) level of theory. The obtained results indicate that the maleimide is favored both kinetically and thermodynamically as observed experimentally.
- Yahia, Wassila,Nacereddine, Abdelmalek Khorief,Seddiki, Khemissi,Liacha, Messaoud,Nippert
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p. 853 - 859
(2015/11/24)
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- AUTOTAXIN INHIBITORS
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The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propaga
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Page/Page column 71
(2010/11/03)
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- QUINAZOLINONE AND FUSED PYRIMIDINONE COMPOUNDS AND THEIR USE IN TREATING SODIUM CHANNEL-MEDIATED DISEASES OR CONDITIONS
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This invention is directed to compounds of formula (I): wherein (A), n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
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Page/Page column 97
(2008/12/07)
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- NIROGENOUS HETEROCYCLIC DERIVATIVES SUBSTITUTED WITH CYCLIC GROUPS
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It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is -(CR3R4)m-, -CO(CR3R4)n-, -CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.
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Page/Page column 68
(2008/12/08)
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- DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF C-KIT RECEPTORS
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Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.
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Page/Page column 177
(2008/06/13)
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- AGENT FOR PREVENTING OR TREATING NEUROPATHY
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The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula:wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s);B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group;X is a divalent acyclic hydrocarbon group;Z is -O-, -S-, -NR2-, -CONR2- or -NR2CO- (R2 is a hydrogen atom or an optionally substituted alkyl group);Y is a bond or a divalent acyclic hydrocarbon group;R1 is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be -O-, or a salt thereof.
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Page/Page column 150
(2010/02/06)
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- Cardiotonic benzimidazoles
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The present invention provides benzimidazoles of the general formula: STR1 wherein R1, X, A, and R2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles an
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- 2-[4(3)-AMINO-3(4)-HYDROXY-PHENYLIMINO]-IMIDAZOLINES, USEFUL IN THE TREATMENT OF GASTRIC HYPERSECRETION AND HYPERACIDITY
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Imidazolidine derivatives of the formula: STR1 wherein R. sub.1 represents the hydroxy radical and R 2 represents a grouping--NHSO. sub.2 CH 3,--NHCOR' or--NHCONR'R", R' and R" independently of one another representing a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms, or alternatively R 2 represents the hydroxy radical and R 1 represents a grouping--NHSO 2 CH 3,--NHCOR' or ?NHCONR'R", R' and R" independently of one another representing a hydrogen atom or an alkyl radical having from 1 to 4 carbon atoms, and pharmacologically-acceptable acid addition salts thereof, are new therapeutically useful compounds. They are more particularly useful in the treatment of gastric hypersecretion or hyperacidity or glaucoma. "
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- Iminoisoindoline pigments and processes for the preparation thereof
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Iminoisoindolinone pigments of the formula SPC1 Wherein X represents halogen atoms, Y represents a halogen atom, an alkoxy, cycloalkoxy, aralkoxy, aryloxy, alkylthio or arylthio group, R represents an aromatic radical containing a cyclic bound -CONH group, and Q represents an O-atom or the group =N--R and are useful for coloring plastics and lacquers in yellow shades having excellent fastness properties.
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