4021-11-8Relevant academic research and scientific papers
Preparation method of 2-methylpyridine-4-formic acid
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Paragraph 0062-0076, (2019/11/28)
The invention provides a preparation method of 2-methylpyridine-4-formic acid. The preparation method comprises the following steps: carrying out a substitution reaction on 4,4-dialkoxy butyronitrileor 4,4-dialkoxy butyrate (II) with chloroacetone, or carrying out a ring-opening addition reaction and oxidation reaction on 4,4-dialkoxy butyronitrile or 4,4-dialkoxybutyrate with propylene oxide toprepare 6,6-dialkoxy-4-cyano-n-hexyl-2-one or 6,6-dialkoxy-4-alkoxycarbonyl-n-hexyl-2-one (III); then carrying out a cyclization reaction with ammonia and ammonium salt; and finally carrying out an oxidation reaction and hydrolysis, and carrying out acidification by hydrochloric acid to prepare the 2-methylpyridine-4-formic acid (I). The method provided by the invention has mild conditions, concise process flow, and safe and simple operation; the generation amount of waste acid and waste water is small, greenness and environment friendliness are achieved; reaction selectivity is good; productcost is low; the yield and purity of the product are high; and green industrial production of 2-methylpyridine-4-formic acid and popularization of downstream products of 2-methylpyridine-4-formic acidare facilitated.
HUMAN PLASMA KALLIKREIN INHIBITORS
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Page/Page column 150, (2017/05/10)
Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE
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Page/Page column 154, (2016/06/01)
The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
(Aza)pyridopyrazolopyrimidinones and indazolopyrimidinones and their use
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Paragraph 0340 - 0342, (2015/05/13)
The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
(AZA)PYRIDOPYRAZOLOPYRIMIDINONES AND INDAZOLOPYRIMIDINONES AS INHIBITORS OF FIBRINOLYSIS
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Page/Page column 61, (2015/05/26)
The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
HUMAN PLASMA KALLIKREIN INHIBITORS
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Page/Page column 840, (2015/11/02)
Disclosed are compounds of formula (I), as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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Page/Page column 186; 187, (2013/02/27)
The present invention relates to a novel indazole- or pyrrolopyridine-derivative, represented by the formula (1) below, that has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same. Formula (1) [wherein each substituent is as defined in claim 1]
New 2-aminothiadiazole derivatives
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Page/Page column 18, (2011/08/03)
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or N-oxide thereof: wherein: ? L represents a direct bond or a -S(O)2- group, ? n is an integer having a value from 0 to 2, ? R1 represents a pyridyl group or an imidazo[1,2-a]pyridinyl group, wherein the pyridyl group is substituted with one or more substituents selected from halogen atoms, a hydroxy group, a C1-4 alkyl group and a C1-4 alkoxy group, or ? R1 represents a group of formula: wherein: o Ra and Rb independently represent a hydrogen atom, halogen atom or a linear or branched C1-4 alkyl group, o Rc represents a hydroxy group, a linear or branched C1-4 alkyl group or C1-4 alkoxy group wherein the alkyl and the alkoxy groups independently are optionally substituted with one or more substituents selected from hydroxy group, cyano group and-NR'R" groups and wherein ■ R' represents a hydrogen atom or a linear or branched C1-4 alkyl group, ■ R" represents a hydrogen atom or a linear or branched C1-4 alkyl group optionally substituted with a hydroxycarbonyl group; or ■ R' and R" together with the nitrogen atom to which they are attached form a 4 to 6 membered, saturated heterocyclic ring optionally substituted with a hydroxycarbonyl group. ? R2 represents a pyridyl group, a C3-6 cycloalkyl group or a phenyl group which is optionally substituted with one or more substituents selected from halogen atoms, cyano group, and C1-4 alkoxy group; and ? R3 represents a C3-6 cycloalkyl group, a C3-6 cycloalkyl-C1-2 alkyl group or a linear or branched C2-4 alkyl group optionally substituted with one or more substituents selected from halogen atoms and C1-2 alkoxy group.
NON-PEPTIDYL, POTENT, AND SELECTIVE MU OPIOID RECEPTOR ANTAGONISTS
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Page/Page column 62, (2010/08/08)
Selective, non-peptide antagonists of the ma opioid receptor { MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction.
BETA-LACTAMASE INHIBITORY COMPOUNDS
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Page/Page column 46; 47, (2010/02/17)
Inhibitors of the enzyme beta-lactamase are provided. The compounds are adapted to inhibit beta-lactamase as produced by beta-lactam resistant bacterial strains. Methods of treatment of beta-lactam resistant bacterial infections in patients are provided.
