- Betrixaban structural analogue as well as preparation method and application thereof
-
The invention provides a novel compound for preparation of drugs for treating venous thrombosis diseases, and particularly relates to a betrixaban structural analogue with a formula (I) shown in the following description or a pharmaceutically acceptable salt thereof, as well as a preparation method and application of the betrixaban structural analogue.
- -
-
Paragraph 0014; 0032
(2016/10/08)
-
- 2-Aminomethylphenylamine as a novel scaffold for factor Xa inhibitor
-
We have been researching orally active factor Xa inhibitor for a long time. We explored the new diamine linker using effective ligands to obtain a new attractive original scaffold 2-aminomethylphenylamine derivative. Compound 1D showed very strong in vitro and in vivo factor Xa inhibitory activity, as well as favorable PK profiles in po administration to monkeys.
- Mochizuki, Akiyoshi,Nagata, Tsutomu,Kanno, Hideyuki,Suzuki, Makoto,Ohta, Toshiharu
-
experimental part
p. 1623 - 1642
(2011/04/21)
-
- HYDRAZONE COMPOUNDS AND THEIR USE
-
The present invention relates to hydrazone compounds of Formula I: (I) and pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3, R4, L1, and L2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I as inhibitors of TRPM5 protein.
- -
-
Page/Page column 132
(2010/12/17)
-
- Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof
-
γ-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.
- -
-
Page/Page column 223
(2010/01/31)
-
- Amide derivative
-
A compound of the formula: wherein Ar is optionally substituted phenyl, etc.; n is 0, 1 or 2; R1is hydogen atom, optionally substituted alkyl, etc.; R2and R3are independently optionally substituted alkyl, etc.; R4and R5are independently hydrogen atom or optionally substituted alkyl; R6is hydrogen atom, hydroxy or alkyl; or a pharmaceutically acceptable salt thereof is useful as a medicament for treating retinal degenerative disorders and the like.
- -
-
-
- AMIDE DERIVATIVES
-
A prodrug of the compound given by formula:wherein Ar is an optionally substituted phenyl group or optionally substituted aromatic heterocyclic group; n is an integer of 0, 1 or 2;R1is a hydogen atom or an optionally substituted alkyl group; R2and R3are independently an optionally substituted alkyl group, or R2may be bonded with R1or R3and taken together with the carbon atom adjacent thereto to form an optionally substituted cycloalkane ring;R4and R5are independently hydrogen atom or an optionally substituted alkyl group;R6is a hydrogen atom, hydroxy group or alkyl group;which is useful as a medicament for treating neurodegenerative disorders such as retinal neurodegenerative disorders and the like.
- -
-
-
- Process for preparing pyridine 2-carboxamides
-
It has been found that pyridine-2-carboxamides of the formula STR1 wherein R is amino or a residue convertible into amino, and pharmaceutically usable acid addition salts of that carboxamide in which R is amino can be prepared in a simple manner and in good yield by reacting 2,5-dichloropyridine in the presence of a palladium-phosphine catalyst with an alkyne of the formula wherein R1 is hydrogen, lower-alkyl, trimethylsilyl or the group --(R2)(R3)--COH and R2 and R3 each independently are hydrogen or lower-alkyl or together are cyclopentyl or cyclohexyl, oxidizing the resulting alkyne to give 5-chloropyridine-2-carboxylic acid and reacting this acid or a reactive functional derivative thereof with an amino compound of the formula VI. The compound of formula I in which R is amino is a known compound which is a reversible and highly active MAO-B inhibitor.
- -
-
-
- Catechol 2,3-Dioxygenase-catalyzed Synthesis of Picolinic Acids from Catechols
-
Various picolinic acid derivatives were synthesized from ammonia and hydroxymuconic semialdehyde derivatives that were oxidatively prepared from various catechols by the action of Pseudomonas catechol 2,3-dioxygenase (C23O, metapyrocatechase).
- Asano, Yasuhisa,Yamamoto, Yasushi,Yamada, Hideaki
-
p. 2054 - 2056
(2007/10/02)
-