- POLYMERIZABLE ABSORBERS OF UV AND HIGH ENERGY VISIBLE LIGHT
-
Described are polymerizable high energy light absorbing compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and X are as described herein. The compounds absorb various wavelengths of ultraviolet and/or high energy visible light and are suitable for incorporation in various products, such as biomedical devices and ophthalmic devices.
- -
-
-
- ALPHA, BETA-UNSATURATED AMIDE COMPOUND
-
An object of the present invention is to provide an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The α,β-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: [wherein, "A" represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents -O-, -S-, -SO2-, -NRX1- (wherein, RX1 represents hydrogen atom or lower alkyl), -CHRX2- (wherein, RX2 represents hydrogen atom or hydroxy), -CH=CH-, -CO- or -NH-CO-, and n1 and n2 are the same or different, and each represents 0 or 1].
- -
-
Paragraph 0604
(2020/12/10)
-
- Chemoselective Hydrosilylation of the α,β-Site Double Bond in α,β- And α,β,γ,δ-Unsaturated Ketones Catalyzed by Macrosteric Borane Promoted by Hexafluoro-2-propanol
-
The B(C6F5)3-catalyzed chemoselective hydrosilylation of α,β- and α,β,γ,δ-unsaturated ketones into the corresponding non-symmetric ketones in mild reaction conditions is developed. Nearly 55 substrates including those bearing reducible functional groups such as alkynyl, alkenyl, cyano, and aromatic heterocycles are chemoselectively hydrosilylated in good to excellent yields. Isotope-labeling studies revealed that hexafluoro-2-propanol also served as a hydrogen source in the process.
- Zhan, Xiao-Yu,Zhang, Hua,Dong, Yu,Yang, Jian,He, Shuai,Shi, Zhi-Chuan,Tang, Lei,Wang, Ji-Yu
-
p. 6578 - 6592
(2020/07/17)
-
- Synthesis of Flavanones via Palladium(II)-Catalyzed One-Pot β-Arylation of Chromanones with Arylboronic Acids
-
A total of 47 flavanones were expediently synthesized via one-pot β-arylation of chromanones, a class of simple ketones possessing chemically unactivated β sites, with arylboronic acids via tandem palladium(II) catalysis. This reaction provides a novel route to various flavanones, including natural products such as naringenin trimethyl ether, in yields up to 92percent.
- Cho, Yang Yil,Jang, Hyu Jeong,Kim, Dong Hwan,Kim, Nam Yong,Kim, Nam-Jung,Kim, Young Min,Lee, Soo Jin,Lee, Yong Sup,Park, Boyoung Y.,Son, Seung Hwan,Yoo, Hyung-Seok
-
p. 10012 - 10023
(2019/08/30)
-
- Synthesis of Phenols: Organophotoredox/Nickel Dual Catalytic Hydroxylation of Aryl Halides with Water
-
A highly effective hydroxylation reaction of aryl halides with water under synergistic organophotoredox and nickel catalysis is reported. The OH group of the resulting phenols originates from water, following deprotonation facilitated by an intramolecular base group on the ligand. Significantly, aryl bromides as well as less reactive aryl chlorides served as effective substrates to afford phenols with a wide range of functional groups. Without the need for a strong inorganic base or an expensive noble-metal catalyst, this process can be applied to the efficient preparation of diverse phenols and enables the hydroxylation of multifunctional pharmaceutically relevant aryl halides.
- Yang, Liu,Huang, Zhiyan,Li, Gang,Zhang, Wei,Cao, Rui,Wang, Chao,Xiao, Jianliang,Xue, Dong
-
supporting information
p. 1968 - 1972
(2018/02/06)
-
- a, ? UNSATURATED AMIDE COMPOUND
-
The present invention provides an α,β-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like represented by the following formula (I): [wherein, "A" represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents -O-, -S-, -SO2-, -NRX1- (wherein, RX1 represents hydrogen atom or lower alkyl), -CHRX2- (wherein, RX2 represents hydrogen atom or hydroxy), -CH=CH-, -CO- or -NH-CO-, and n1 and n2 are the same or different, and each represents 0 or 1].
- -
-
Paragraph 0485
(2018/11/27)
-
- Transition metal free regio-selective C-H hydroxylation of chromanones towards the synthesis of hydroxyl-chromanones using PhI(OAc)2 as the oxidant
-
The chromanone scaffold is considered as a privileged structure in drug discovery. Herein, we report a highly efficient PhI(OAc)2 mediated regioselective, direct C-H hydroxylation of chromanones. This method offers easy access to substituted 6-hydroxy chromanones in moderate to good isolated yields, thus paving the way for their pharmaceutical studies.
- Viswanadh,Ghotekar, Ganesh S.,Thoke, Mahesh B.,Velayudham,Shaikh, Aslam C.,Karthikeyan,Muthukrishnan
-
supporting information
p. 2252 - 2255
(2018/03/06)
-
- Chroman Compound, Processes for Its Preparation, and Its Pharmaceutical Use
-
The present invention provided a chroman compound, the method of its preparation and pharmaceutical applications. The compound are represented by formula (I) and its pharmaceutical salt, where in :x is for O or S; n is for 2, 3 or 4; R1 is 6-situ or 7-situ halogen, C1-4alkyl, C1-4alkyoxyl, benzyloxy, acylamino; R2 is nitrogen-containing pentatomic or hexahydric substituted heterocyclic ring. The compound is useful to prepare anti-arrhythmic drugs, the reaction conditions of the method are mild, the raw material are plenty and easy to be obtained, and the operation and post-treatment are simple.
- -
-
Page/Page column 17
(2008/06/13)
-
- MUSCARINIC ANTAGONISTS
-
Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula (I) (including all isomers, salts, esters, and solvates), wherein Q, n, R, R, R, R, R, R, R, R, X, and Z are as defined herein are mu
- -
-
-
- Inhibitors of prenyl-protein transferase
-
The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemothera-peutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
- -
-
-
- Substituted tetralins, chromans and related compounds in the treatment of asthma
-
PCT No. PCT/US87/02734 Sec. 371 Date Apr. 11, 1990 Sec. 102(e) Date Apr. 11, 1990 PCT Filed Oct. 19, 1987Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals; pharmaceutical compositions comprising said compounds; a method of treatment with said compounds; and intermediates useful in the synthesis of said compounds.
- -
-
-
- Discovery of CP-199,330 and CP-199,331: Two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity
-
CP-199,330 (3) and CP-199,331 (4) are cysLT1 receptor antagonists that are equipotent to marketed cysLT1 receptor antagonists zafirlukast and pranlukast, show good pharmacokinetics in rats and monkeys, and are devoid of liver toxicity in monkeys as seen in CP-85,958 (1).
- Chambers,Marfat,Antognoli,Cheng,Damon,Kuperman,Liston,Mebus,Pillar,Shirley,Watson
-
p. 2773 - 2778
(2007/10/03)
-
- SULFONAMIDE DERIVATIVES OF BENZENEFUSED HYDROXY SUBSTITUTED CYCLOALKYL AND HETEROCYCLIC RING COMPOUNDS
-
Compounds of the formula STR1 and pharmaceutically acceptable salts and prodrugs thereof, wherein X 1, Ar, X, Y 1, R. sup.1, R. sup.2, R 3, R 5 and n are defined below, which are inhibitors of the production of leukotrienes and/or blockers of leukotriene
- -
-
-
- 1,2-Dithiole derivatives and therapeutic agents containing them
-
Novel 1,2-dithiole-3-thione derivatives represented by general formulas (1) and (11); processes for production thereof; and therapeutic or preventive agents for diseases associated with peroxylipid, each containing said derivative as the active ingredient
- -
-
-
- AZABENZIMIDAZOLES IN THE TREATMENT OF ASTHMA, ARTHRITIS AND RELATED DISEASES
-
A series of imidazo[4,5-c]pyridines which inhibit platelet activating factor (PAF) and also block leukotriene D4 receptors are useful in treating asthma, arthritis, psoriasis, gastrointestinal distress, myocardial infarction, stroke and shock.
- -
-
-
- SUBSTITUTED CHROMANS AND THEIR USE IN THE TREATMENT OF ASTHMA, ARTHRITIS AND RELATED DISEASES
-
Substituted chromans which by inhibiting 5-lipoxygenase enzyme are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction, stroke and related disease states in mammals, pharmaceutical compositions thereof, a m
- -
-
-
- Substituted tetralins, chromans and related compounds in the treatment of asthma, arthritis and related diseases
-
Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.
- -
-
-
- Serotonin Receptor Affinity of Cathinone and Related Analogues
-
A series of cathinone (α-aminopropiophenone) analogues was examined using the isolated rat fundus preparation. (S)-(-)-Cathinone possesses twice the serotonin receptor affinity of (+/-)-cathinone and four times the affinity of racemic amphetamine.Several derivatives of cathinone were found to either possess a lower affinity than the parent compound or did not interact with the receptors in a competitive manner.Several novel analogues, 1-(aminomethyl)-3,4-dihydronaphthalene hydrochloride (3), 4-(aminomethyl)-3-chromene hydrochloride (4b), as well as its 6-methoxy derivative, 4a, interact with serotonin receptors but in a fashion which is, most likely, dissimilar to the interaction of the substituted cathinone analogues.
- Glennon, Richard A.,Liebowitz, Stephen M.
-
p. 393 - 397
(2007/10/02)
-
