- HALOALLYLAMINE COMPOUNDS AND APPLICATION THEREOF
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The present invention relates to the technical field of pharmaceuticals. Specifically, the present invention relates to a halo-allylamine compound, or a pharmaceutically acceptable salt, an ester, a stereoisomer or a tautomer thereof, and a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, and use in preventing and/or treating a disease related to or mediated by the SSAO/VAP-1 protein,wherein R1, R2, R3, R4, R5, R6, L1 and Cy1 are defined in the specification.
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Paragraph 0382-0384
(2021/10/15)
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- CEREBLON BINDERS FOR THE DEGRADATION OF IKAROS
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The present invention provides cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway along with their use in therapeutic applications as described herein.
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Page/Page column 318
(2019/10/23)
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- FUMAGILLOL COMPOUNDS AND METHODS OF MAKING AND USING SAME
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Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
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Paragraph 00194
(2018/03/06)
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- NOVEL FERROPORTIN INHIBITORS
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The invention relates to novel ferroportin inhibitors of the general formula (I) pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.
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Page/Page column 297; 298
(2017/05/10)
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- Silica supported palladium-phosphine as a reusable catalyst for alkoxycarbonylation and aminocarbonylation of aryl and heteroaryl iodides
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Silica-supported palladium phosphine complexes were prepared for alkoxycarbonylation and aminocarbonylation of aryl iodides. These catalysts were highly efficient for the carbonylation of unprotected hydroxy-aryl, amino-aryl, iodoindole and iodopyrazole. The carbonylation of unprotected iodopyrazole is challenging and their carbonylation was achieved for the first and obtained corresponding carbonylative products are biologically active. The applicability of developed protocols tolerates wide range of functional groups with excellent yields. The catalyst was easily recovered and shows significant recyclability up to five consecutive cycles without loss in its catalytic activity and selectivity. The prepared catalysts were characterized by different techniques such as FEG-SEM, EDS, FT-IR, XPS and ICP-AES spectroscopy.
- Mane, Rajendra Shivaji,Sasaki, Takehiko,Bhanage, Bhalchandra Mahadeo
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p. 94776 - 94785
(2015/11/24)
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- NITROGENATED HETEROCYCLIC COMPOUND
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The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
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Paragraph 0842
(2015/03/28)
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- Inverse electron demand diels-alder reactions of 1,2,3-triazines: Pronounced substituent effects on reactivity and cycloaddition scope
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A systematic study of the inverse electron demand Diels-Alder reactions of 1,2,3-triazines is disclosed, including an examination of the impact of a C5 substituent. Such substituents were found to exhibit a remarkable impact on the cycloaddition reactivity of the 1,2,3-triazine without altering, and perhaps even enhancing, the intrinsic cycloaddition regioselectivity. The study revealed not only that the reactivity may be predictably modulated by a C5 substituent (R = CO2Me > Ph > H) but also that the impact is of a magnitude to convert 1,2,3-triazine (1) and its modest cycloaddition scope into a heterocyclic azadiene system with a reaction scope that portends extensive synthetic utility, expanding the range of participating dienophiles. Significantly, the studies define a now powerful additional heterocyclic azadiene, complementary to the isomeric 1,2,4-triazines and 1,3,5-triazines, capable of dependable participation in inverse electron demand Diels-Alder reactions, extending the number of complementary heterocyclic ring systems accessible with implementation of the methodology.
- Anderson, Erin D.,Boger, Dale L.
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supporting information; experimental part
p. 12285 - 12292
(2011/09/16)
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- MALONONITRILE COMPOUND AND USE THEREOF
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A nitrile compound shown by the formula (1) has an excel lent pesticidal activity and it is useful as an active ingredient of pesticide.
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Page/Page column 56
(2008/06/13)
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- Chroman derivative and pharmaceutical use thereof
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Chroman derivatives of the formula ?I! STR1 wherein R1 is a cyano, a nitro, a trihalomethyl, a trihalomethoxy or a halogen atom; R2 is a lower alkoxyalkyl, an aryloxyalkyl or a dialkoxyalkyl; R3 is a lower alkoxyalkyl or an aryloxyalkyl; R4 is a hydroxy, a formyloxy or a lower alkanoyloxy; X is N--H, an N--optionally substituted lower alkyl, an oxygen atom, a sulfur atom or a single bond; and Y is an optionally substituted aromatic ring residue or an optionally substituted heterocyclic residue, pharmaceutically acceptable salts thereof and pharmaceutical use thereof. The compound of the present invention and pharmaceutically acceptable salts thereof have selective and excellent coronary vasodilating action and extremely weak hypotensive action. Accordingly, it is possible to selectively increase the coronary blood flow without causing a sudden hypotention causative of tachycardia which has a detrimental effect on the heart, and they are useful as a coronary vasodilator, in particular, an agent for the prophylaxis and treatment of cardiovascular disorders such as angina pectoris and heart failure.
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- Evolution thermique et photochimique des triazolines resultant de l'addition des diazocomposes aux esters d'oximino-malonodinitriles, oximino-cyanoacetates et oximino-malonates de methyle
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Thermolysis of 1,2,3-triazolines 4,5,6 leads to the corresponding aziridines only when X=Y=CO2Me, and then with a very low yield.However, photolysis or evolution in the presence of trifluoroacetic acid gives good results when carried out at sufficiently low temperature.The thermolysis study of 4-6 shows a new route to 1,2,3-triazoline decomposition that has not yet been mentioned in the literature.The easy elimination of the paratoluenesulfonate or benzoate group explains this particular behaviour.
- Perrocheau, Jacques,Carrie, Robert,Fleury, Jean-Pierre
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p. 2458 - 2467
(2007/10/02)
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- Metallacarborane chelates
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Metallacarborane chelate-antibody compounds which are useful for radioimmunodetection and radiotherapy. The compounds have the formula STR1 wherein X is a metal or radioisotope of said metal, Y is a rotation resistant organic chelate bridge moiety, Z is an antibody linkage moiety and AB is an antibody. Metallacarborane chelate and carborane chelate compounds are also disclosed which are useful in preparing the final metallacarborane chelate-antibody compound which is used for radioimmunodetection and radiotherapy.
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- Pyrimidine Derivatives and Related Compounds. Part 45. Synthesis of 4-Allophanoylpyrazoles via a Pyrimidine-to-pyrazole Ring Transformation
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Reaction of the 5-formyluracil derivatives (1a-f) with hydrazines in the presence of acetic acid produced a ring contraction to give the corresponding 4-allophanoylpyrazoles (2a-h).Further treatment of these pyrazoles (2a-h) with sodium methoxide afforded methyl pyrazole-4-carboxylate (3a).Conceivable mechanisms for the present pyrimidine-to-pyrazole transformation were discussed.
- Hirota, Kosaku,Kitade, Yukio,Shimada, Kaoru,Senda, Shiego,Maki, Yoshifumi
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p. 1293 - 1298
(2007/10/02)
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- A RING TRANSFORMATION OF URACIL INTO THE PYRAZOLE RING SYSTEM. REINVESTIGATION OF THE REACTION OF 5-FORMYLURACILS WITH HYDRAZINES
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Cheng et al. reported that the reaction of 5-formyluracil (1a) with hydrazine hydrate in the presence of acetic acid gave 4-ureidomethylene-1H-5-pyrazolone (3).However, results of our reinvestigation revealed that the Cheng's compound (3) should be 4-urei
- Hirota, Kosaku,Kitade, Yukio,Shimada, Kaoru,Senda, Shigeo
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p. 3760 - 3762
(2007/10/02)
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