- A catalytic oxidation fragrant boron class compound preparing phenol method (by machine translation)
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The invention discloses a method for catalytic oxidation of phenolic compounds fragrant boron class compound synthesis method, the flux in the solvent in the aqueous solution, under the action of alkali, adding hydrazine hydrate or acid hydrazides catalyst, catalytic oxidation fragrant boron class compound directly for the preparation of phenolic compound. The invention of the method of preparation of the phenol compound, the catalyst is a cheap hydrazine hydrate or hydrazine compound, the oxidizing agent is atmospheric pressure of air or oxygen, the reaction does not need good and activeness metal catalyst, is extensive and stable substrate, substrate-sensitive functional group compatibility good and wide range of application. In the optimized under the reaction conditions, the yield of the target product separation up to 99%. (by machine translation)
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Paragraph 0073; 0081; 0082
(2017/08/08)
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- Boron-Containing Small Molecules as Anti-Inflammatory Agents
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Compounds and methods of treating anti-inflammatory conditions are disclosed.
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Paragraph 1199
(2015/11/16)
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- Derivatives of azaindoles or diazaindoles for treating pain
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The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; for use in the treatment of pain.
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Paragraph 0238
(2014/02/15)
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- DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE FOR TREATING PAIN
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The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; for use in the treatment of pain.
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Page/Page column 73
(2014/02/16)
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- DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE FOR TREATING A CANCER OVEREXPRESSING TRK
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The present invention relates to a compound of following formula (I) or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.
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Page/Page column 72
(2014/02/16)
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- Derivatives of azaindazole or diazaindazole type for treating a cancer overexpressing trk
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The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture, as well as pharmaceutical composition comprising such a compound, for use in the treatment of a cancer associated with the overexpression of at least one Trk protein.
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Paragraph 0297-0299
(2014/02/15)
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- DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT
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The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
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Paragraph 0394; 0395; 0396
(2013/04/13)
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- DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT
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The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
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Page/Page column 74
(2012/08/08)
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- TRICYCLIC COMPOUNDS, PREPARATION METHODS, AND THEIR USES
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The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
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Page/Page column 42; 57
(2012/04/10)
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- SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Substituted cyclopropyl compounds of formula (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
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Page/Page column 80
(2009/12/02)
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- Synthesis of a fragment a derivative of an antibiotic, nosiheptide
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Two 4-ethoxycarbonyl thiazoyly groups were introduced into 2- and 5- positions of 3-hydroxypyridine in 8 steps using 5-cyano-3-hydroxypyridine (2) as the starting material. The pyridine derivative obtained in the last step was converted to a fragment. A derivative (21) by stepwise introduction of the 2-substituted 4-thiazolyl group into the 6-position. The total yield for the formation of 21 via 14 steps was 7.6%.
- Umemura, Kazuyuki,Noda, Hirofumi,Yoshimura, Juji,Konn, Akihito,Yonezawa, Yasuchika,Shin, Chung-Gi
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p. 1391 - 1396
(2007/10/03)
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- The synthesis of fragment A of an antibiotic, nosiheptide
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Fragment A derivative(13) of nosiheptide, useful for the total synthesis, was obtained by stepwise introduction of the 25-bis{(4ethoxycarbonyl)-2-thiazolyl} groups and 6-{(2-substituted)-4-thiazolyl} group into 3-hydroxy-5-cyanopyridine (3). The total yield was 7.6% via 14 steps.
- Umemura, Kazuyuki,Noda, Hirofumi,Yoshimura, Juji,Konn, Akihito,Yonezawa, Yasuchika,Shin, Chung-Gi
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p. 3539 - 3542
(2007/10/03)
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- Pyridinecarboxyimidamide compounds and the use thereof
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Disclosed are pyridinecarboximidamides having a vasodilating effect (hypotensive activity or antianginal activity), and acid adduct salts thereof. STR1 wherein when R1 represents an alkyl, hydroxyalkyl, carboxyl, amino, acylamino, alkylamino, dialkylamino, aralkylamino, alkylsulfonamide, bisalkylsulfonylamino or hydroxyl group, R2 represents a hydrogen atom and R3 represents a nitroxyl, 2-chlorophenyl or phenyl group; and when R1 represents a hydrogen atom, R2 represents an alkyl, hydroxyalkyl, carboxyl, amino, acylamino, alkylamino, dialkylamino, aralkylamino, alkylsulfonamide, bisalkylsulfonylamino or hydroxyl group and R3 represents a nitroxyl, 2-chlorophenyl or phenyl group. There is also disclosed the use of the compounds represented by the formula (I) for antihypertensive or antianginal purpose.
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