- Ionic tags for synthesis of oligoribonucleotides
-
The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II) processes for making these compounds, and the use thereof in the chemical synthesis of o
- -
-
Page/Page column 61-62; 115-117; 155-157
(2018/04/12)
-
- Design and synthesis of a novel series of orally active, selective somatostatin receptor 2 agonists for the treatment of type 2 diabetes
-
The discovery of a novel series of β-methyltryptophan (β MeTrp) derivatives as selective and orally active non-peptide somatostatin receptor 2 (SSTR2) agonists for the treatment of Type 2 diabetes is described. In our previous research, Compound A, β-MeTr
- Banno, Yoshihiro,Sasaki, Shigekazu,Kamata, Makoto,Kunitomo, Jun,Miyamoto, Yasufumi,Abe, Hidenori,Taya, Naohiro,Oi, Satoru,Watanabe, Masanori,Urushibara, Tomoko,Hazama, Masatoshi,Niwa, Shin-ichi,Miyamoto, Saku,Horinouchi, Akira,Kuroshima, Ken-ichi,Amano, Nobuyuki,Matsumoto, Shin-ichi,Matsunaga, Shinichiro
-
p. 5995 - 6006
(2017/10/10)
-
- Synthetic, structural mimetics of the β-hairpin flap of HIV-1 protease inhibit enzyme function
-
Small-molecule mimetics of the β-hairpin flap of HIV-1 protease (HIV-1 PR) were designed based on a 1,4-benzodiazepine scaffold as a strategy to interfere with the flap-flap protein-protein interaction, which functions as a gated mechanism to control acce
- Chauhan, Jay,Chen, Shen-En,Fenstermacher, Katherine J.,Naser-Tavakolian, Aurash,Reingewertz, Tali,Salmo, Rosene,Lee, Christian,Williams, Emori,Raje, Mithun,Sundberg, Eric,Destefano, Jeffrey J.,Freire, Ernesto,Fletcher, Steven
-
p. 7095 - 7109
(2015/11/11)
-
- BENZAMIDE DERIVATIVE USEFUL AS FASN INHIBITORS FOR THE TREATMENT OF CANCER
-
The present invention is directed to benzamide derivatives, pharmaceutical compositions containing them, and their use as FASN inhibitors, in for example, the treatment of cancer, obesity related disorders, liver related disorders and viral infections. Such compounds are represented by formula (I) as follows: wherein R1, R2, R3, R4, R5, m, n, (II) and (III) are defined herein.
- -
-
Page/Page column 128; 129
(2015/06/18)
-
- GPR40 RECEPTOR AGONIST, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE INGREDIENT
-
The present invention relates to a novel compound having GPR40 receptor agonist activity that promotes insulin secretion and inhibits blood sugar rise after glucose loading, and is thereby useful for the treatment of diabetes and complications thereof, the preparation method thereof and pharmaceutical composition containing them as an active ingredient.
- -
-
Paragraph 1151-1154
(2014/05/24)
-
- HISTONE DEMETHYLASE INHIBITORS
-
Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
- -
-
Paragraph 00685; 00686
(2014/06/24)
-
- High-yielding and photolabile approaches to the covalent attachment of biomolecules to surfaces via hydrazone chemistry
-
The development of strategies to couple biomolecules covalently to surfaces is necessary for constructing sensing arrays for biological and biomedical applications. One attractive conjugation reaction is hydrazone formation - the reaction of a hydrazine w
- Lee, Ju Hun,Domaille, Dylan W.,Noh, Hyunwoo,Oh, Taeseok,Choi, Chulmin,Jin, Sungho,Cha, Jennifer N.
-
p. 8452 - 8460
(2014/08/05)
-
- IMIDAZO [4, 5 -C] PYRIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
-
Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, wherein R1 and Cy are as disclosed herein. These compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.
- -
-
Paragraph 00331-00332
(2013/08/28)
-
- In vitro and in vivo uncaging and bioluminescence imaging by using photocaged upconversion nanoparticles
-
Trading up: A bioimaging system that is based on caged D-luciferin/ upconversion nanoparticle conjugate has been developed. The nanoparticles upconvert near-infrared light into UV light, which triggers the photorelease of D-luciferin (see scheme) and lead
- Yang, Yanmei,Shao, Qing,Deng, Renren,Wang, Chao,Teng, Xue,Cheng, Kai,Cheng, Zhen,Huang, Ling,Liu, Zhuang,Liu, Xiaogang,Xing, Bengang
-
supporting information; experimental part
p. 3125 - 3129
(2012/05/05)
-
- PIPERIDINE DERIVATIVES FOR THE TREATMENT OF OBESITY
-
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity, diabetes mellitus, c
- -
-
Page/Page column 224
(2008/12/06)
-
- SULFONAMIDE DERIVATIVES FOR THERAPEUTIC USE AS FATTY ACID SYNTHASE INHIBITORS
-
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus
- -
-
Page/Page column 158-159
(2008/12/06)
-
- AMINE COMPOUNDS
-
The present invention provide a compound of the formula:wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.
- -
-
-
- A simple synthesis of photolabile α-methyl nitrobenzyl compounds
-
α-Methyl nitrobenzyl compounds have demonstrated superior photochemical release properties when compared to nitrobenzyl compounds lacking α-methyl substitution at the benzylic position. The synthesis of 4-(1-hydroxy-ethyl)-3-nitro-benzoic acid ethyl ester
- Salerno, Charles P.,Cleaves, Henderson J.
-
p. 2379 - 2386
(2007/10/03)
-
- Sulfonamide compounds and medicinal use thereof
-
A sulfonamide compound of the formula (I):R 1 --SO 2 NHCO--A--R 2 (I)wherein R 1 is alkyl, alkenyl, alkynyl and the like; A is an optionally substituted heteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyl and 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R 2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.
- -
-
Page column 80
(2010/02/04)
-
- Thiourea and benzamide compounds, compositions and methods of treating or preventing inflammatory diseases and atherosclerosis
-
The present invention provides compounds of formula (I). The present invention also provides methods of treating or preventing inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of formula (I).
- -
-
-