- BCL-2 INHIBITOR
-
Disclosed herein is a compound of Formula (I) for inhibiting both Bcl-2 wild type and mutated Bcl-2, in particular, Bcl-2 G101V and D103Y, and a method of using the compound disclosed herein for treating dysregulated apoptotic diseases.
- -
-
Paragraph 0847-0849
(2021/10/22)
-
- A 5, 6 - dimethoxy -2 - picolinic acid synthesis method
-
This invention relates to a 5, 6 - dimethoxy - 2 - pyridine carboxylic acid synthesis method. To solve the synthetic method on the reaction of high temperature, operation of the experiment is difficult, high requirements on equipment, unfavorable to industrialization production and amplification of the technical problem. The invention synthetic method comprises the following steps: 1st step, at room temperature, 2 - bromo - 3 - hydroxy pyridine in the potassium carbonate aqueous solution and hydrazine hydrate in the reaction, to obtain compound 1, product need purification, directly used for the next step reaction; 2nd step, compound 1 in N, N - dimethyl formamide and potassium carbonate in the reaction after adding methyl iodide, stirring overnight, to obtain compound 2; 3rd step, compound 2 and sodium methoxide in N, N - dimethyl formamide in reaction, bromine quilt methoxy selectively substituted, to obtain compound 3; 4th step, at the low temperature compound 3 and butyl lithium in tetrahydrofuran reaction, then added with the solid carbon dioxide, the reaction at room temperature, acidified by hydrochloric acid, to obtain the target compound 4, in petroleum ether and ethyl acetate mixed solvent recrystallization purification get the pure product.
- -
-
Paragraph 0009
(2019/02/13)
-
- TRIPYRIDYL CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
-
The present invention is directed to tripyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
- -
-
Page/Page column 17-18
(2010/03/02)
-
- ISONICOTINAMIDE OREXIN RECEPTOR ANTAGONISTS
-
The present invention is directed to isonicotinamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. Th
- -
-
Page/Page column 48
(2010/05/14)
-
- PYRIDAZINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
-
The present invention is directed to pyridazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
- -
-
Page/Page column 45-46
(2010/05/14)
-
- PYRAZINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
-
The present invention is directed to pyrazine carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involve
- -
-
Page/Page column 41
(2010/12/29)
-
- Design of potent IGF1-R inhibitors related to bis-azaindoles
-
From an azaindole lead, identified in high throughput screen, a series of potent bis-azaindole inhibitors of IGF1-R have been synthesized using rational drug design and SAR based on a in silico binding mode hypothesis. Although the resulting compounds produced the expected improved potency, the model was not validated by the co-crystallization experiments with IGF1-R.
- Nemecek, Conception,Metz, William A.,Wentzler, Sylvie,Ding, Fa-Xiang,Venot, Corinne,Souaille, Catherine,Dagallier, Anne,Maignan, Sebastien,Guilloteau, Jean-Pierre,Bernard, Francois,Henry, Alain,Grapinet, Sandrine,Lesuisse, Dominique
-
scheme or table
p. 100 - 106
(2011/03/19)
-
- PYRIDINE CARBOXAMIDE OREXIN RECEPTOR ANTAGONISTS
-
The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved
- -
-
Page/Page column 70-71
(2009/07/03)
-
- Novel Bis-Azaindole Derivatives, Preparation And Pharmaceutical Use Thereof As Kinase Inhibitors
-
Disclosed are compounds of formula (I): wherein R1, R2, R3, R4, and R5 have the meanings given in the description, and to salts thereof, pharmaceutical compositions comprising said compounds and the use thereof as protein kinase inhibitors.
- -
-
Page/Page column 25-26; 22
(2010/11/30)
-
- Total synthesis of (±)-cytisine
-
(equation presented) The nicotine partial agonist cytisine was prepared in five steps featuring an "in situ" Stille or Suzuki biaryl pyridine coupling. Differentiation of the pyridyl rings was accomplished via selective benzylation and then reduction of a pyridinium ring. The penultimate diazabicyclo[3.3.1]-nonane intermediate was obtained with high diastereoselectivity. A similar sequence has been employed for the synthesis of novel derivative 9-methoxycytisine.
- O'Neill, Brian T.,Yohannes, Daniel,Bundesmann, Mark W.,Arnold, Eric P.
-
p. 4201 - 4204
(2007/10/03)
-