- METHODS OF TREATING OR PREVENTING COGNITIVE IMPAIRMENT USING INDANE ACETIC ACID DERIVATIVES BASED ON APOE4 GENOTYPE
-
The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of cognitive disorders based on the ApoE4 genotype of human subjects.
- -
-
Paragraph 0546; 0547
(2018/06/15)
-
- METHODS OF DOSE ADMINISTRATION FOR TREATING OR PREVENTING COGNITIVE IMPAIRMENT USING INDANE ACETIC ACID DERIVATIVES
-
The present invention provides indane acetic acid and their derivatives and methods for the treating and/or preventing of cognitive disorders.
- -
-
Paragraph 0548; 0549
(2018/06/15)
-
- PROCESS FOR THE SYNTHESIS OF A PHOSPHOINOSITIDE 3-KINASE INHIBITOR
-
The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
- -
-
Page/Page column 49; 50
(2016/11/28)
-
- Design and synthesis of 3-(2-ethyl-4-{2-[2-(4-fluorophenyl)- 5-methyloxazol-4-yl]ethoxy}phenyl)propanoic acid: A novel triple-acting PPARα, -γ, and -δ Agonist
-
The design and synthesis of triple-acting PPARα, -γ, and -δ agonist 3-(2-ethyl-4-{2-[2-(4-fluorophenyl)-5-methyloxazol-4-yl]- ethoxy}phenyl)propanoic acid (1a) is described. The compound possesses a potent triple-acting PPARα, -γ, and -δ agonist profile with an EC50 of 0.029, 0.013, and 0.029 μM, respectively. The synthetic route, involving the synthesis of oxazole rings as the key step, starts from commercially available 3-oxopentanoic acid methyl ester and 3- hydroxyacetophenone to afford the target compound 1 with an overall yield of 32%.
- Zhang, Qijun,Sun, Peng,Zheng, Guojun,Wang, Yaping,Wang, Xiangjing,Wei, Hegeng,Xiang, Wensheng
-
scheme or table
p. 406 - 408
(2012/06/01)
-
- SUBSTITUTED DIAMINO-PYRIMIDINE AND DIAMINO-PYRIDINE DERIVATIVES AS PI3K INHIBITORS
-
The present invention provides substituted diamino-pyrimidine and substituted diamino-pyridine derivatives of Formula I; wherein X, Y, R1, R2, and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks
- -
-
Page/Page column 39-40
(2012/10/07)
-
- PYRIMIDINONES AS PI3K INHIBITORS
-
The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
- -
-
Page/Page column 26
(2011/02/18)
-
- Design, synthesis and antimicrobial activity of chiral 2-(substituted- hydroxyl)-3-(benzo[d]oxazol-5-yl)propanoic acid derivatives
-
Chiral 2-(substituted-hydroxyl)-3-(benzo[d]oxazol-5-yl)propanoic acid derivatives were synthesized and their antibacterial activities were evaluated against fungus, Gram-negative and Gram-positive bacteria. In general, these compounds showed in vitro acti
- Zhang, Wei,Liu, Wenlu,Jiang, Xizhen,Jiang, Faqin,Zhuang, Hao,Fu, Lei
-
experimental part
p. 3639 - 3650
(2011/11/05)
-
- IMIDAZOLE CARBONYL COMPOUND
-
To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.
- -
-
Page/Page column 92
(2010/09/17)
-
- Process development and scale-up of AG035029
-
A practical process for the synthesis of PPARγ agonist AG035029 was developed which involved six steps along the longest linear path. The process development utilized automated technology and computational chemistry extensively to accelerate the speed of
- Saenz, James,Mitchell, Mark,Bahmanyar, Sami,Stankovic, Nebojsa,Perry, Michael,Craig-Woods, Bridgette,Kline, Billie,Yu, Shu,Albizati, Kim
-
-
- INDANE, DIHYDROBENZOFURAN, AND TETRAHYDRONAPHTHALENE CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS ANTIDIABETICS
-
This invention relates to novel indane, dihydrobenzofuran, and tetrahydronaphthalene carboxylic acid derivatives whice are useful in the treatment of diseases such sa diabetes, diabetes-related disorders, obesity, hyperlipidemia, and cardiovascular diseases. The invention also relates to intermediates useful in preparation of said carboxylic derivatives and to methods of preparation.
- -
-
-
- Indane acetic acid derivatives and their use as pharmaceutical agents, intermediates, and method of preparation
-
This invention relates to novel indane acetic acid derivatives which are useful in the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic diseases. The invention also relates to intermediates useful in preparation of indane acetic derivatives and to methods of preparation.
- -
-
-
- Process for the preparation of thiazolidinedione derivatives
-
The present invention is concerned with a novel process for the preparation of compounds of formula I comprising bromomethylation or chloromethylation of a compound of formula II and subsequent reaction with a compound of formula IV The compounds of formu
- -
-
-