- INHIBITORS OF KEAP1-Nrf2 PROTEIN-PROTEIN INTERACTION
-
Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.
- -
-
Paragraph 1663-1664
(2020/03/01)
-
- HYDROXYPYRIDOXAZEPINES AS NRF2 ACTIVATORS
-
The present invention relates hydroxypyridoxazepine compounds, methods of making them, pharmaceutical compositions containing them and their use as Nrf2 activators. In particular, the invention relates to compounds of Formula (I), and pharmaceutically acc
- -
-
Page/Page column 86
(2020/08/28)
-
- SGLTS INHIBITOR AND APPLICATION THEREOF
-
A compound as an SGLT1/SGLT2 dual inhibitor, and an application thereof in the preparation of a drug as the SGLT1/SGLT2 dual inhibitor. The compound is a compound represented by formula (I), an isomer thereof, or a pharmaceutically acceptable salt thereof
- -
-
Paragraph 0117-0120
(2020/11/30)
-
- Catalyst system for producing polyethylene copolymers in a high temperature solution polymerization process
-
Catalyst system for producing ethylene copolymers in a high temperature solution process, the catalyst system comprising (i) a metallocene complex of formula (I) wherein M is Hf X is a sigma ligand, L is a bridge of the formula —SiR82—, wherein each R8 is independently a C1-C20-hydrocarbyl, tri(C1-C20-alkyl)silyl, C6-C20-aryl, C7-C20-arylalkyl or C7-C20-alkylaryl n is 0, 1 or 2 R1 and R1′ are the same or can be different and can be a linear or branched C1-C6-alkyl group, R2 and R2′ are the same or are different and are a CH2—R9 group, with R9 being H or linear or branched C1-C6-alkyl group R5 and R5′ are the same or are different and can be H or a linear or branched C1-C6-alkyl group or a OR group, wherein R is a C1-C6-alkyl group R6 and R6′ are the same or are different and can be H or a C(R10)3 group, with R10 being the same or different and R10 can be H or a linear or branched C1-C6-alkyl group or R5 and R6 and/or R5′ and R6′ taken together form an unsubstituted 4-7 membered ring condensed to the benzene ring of the indenyl moiety, and R7 and R7′ can be the same or are different and can be H or a linear or branched C1-C6-alkyl group (ii) an aluminoxane cocatalyst and/or (iii) a boron containing cocatalyst and (iv) optionally an aluminum alkyl compound.
- -
-
-
- Method for preparing alcoholic compound from anilino lithium compound as catalyst
-
The invention relates to an application of an anilino lithium compound, in particular to a method for preparing an alcoholic compound from the anilino lithium compound as a catalyst. The catalyst, borane and carboxylic acid are stirred and mixed uniformly, subjected to a reaction and exposed to air to terminate the reaction, a reacted liquid is subjected to reduced-pressure treatment for solvent removal, silica gel and methanol are added, and the alcoholic compound is obtained by hydrolysis. The anilino lithium compound can perform high-activity catalysis on the reaction between carboxylic acid and borane at room temperature, dose of the catalyst is only 0.8mol% of the mole ratio of carboxylic acid, compared with the conventional catalysis system, the commercial reagent anilino lithium compound is used, reaction conditions are mild, and yield of borate with different substituents under limit conditions can reach 90% or higher.
- -
-
Paragraph 0030
(2019/03/06)
-
- Based on n-butyl aromatic carboxylic acid preparation of alcohol compound
-
The present invention relates to n-butyl application, in particular to based on n-butyl aromatic carboxylic acid preparation of alcohol compound, the catalyst sequentially, borane and carboxylic acid uniformly stirred and mixed, exposed to the air after the reaction terminated in the reaction, the reaction solution under reduced pressure to remove the solvent, then adding silica gel methanol hydrolyzed to obtain the alcohol compound. The invention discloses a butyl lithium can be high activity under the room temperature condition of catalytic carboxylic acid and borane borohydride reaction, the catalyst levels are only the molar amount of carboxylic acid 0.5 μM %, compared with the prior catalytic system, using the commercial reagent is BuLi, mild reaction conditions, in under a limited condition of different substituents of the yield of the ester can reach 90% or more.
- -
-
Paragraph 0030
(2019/03/29)
-
- A is by aromatic carboxylic acid non-catalytic reaction of alcohol compound (by machine translation)
-
The present invention discloses a non-catalytic reaction of the aromatic carboxylic acid preparation of alcohol compound. In an inert gas atmosphere, after dehydration and deoxidation treatment of the reaction bottle [...] borane and carboxylic acid stirring and mixing, reaction 6 - 12 hours to obtain borate, further hydrolyzed into alcohol; said carboxylic acid is benzoic acid, 4 - bromobenzoic acid, 4 - fluoro benzoic acid, 1 - naphthoic acid, 2 - methoxybenzene formic acid and the like. The invention for the first time in the absence of catalyst under the conditions of high-efficiently using carboxylic acid with borane generating borohydrite reaction, carbonyl compound with borane generating borohydrite reaction preparation borate, further hydrolysis alcohol, provides new programme. (by machine translation)
- -
-
Paragraph 0028
(2019/04/17)
-
- BISARYL AMIDES AS NRF2 REGULATORS
-
The present invention relates to bisaryl amide analogs, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the invention relates to bisaryl heterocycles of Formula (I).
- -
-
Page/Page column 323
(2018/09/11)
-
- OXOPYRIDINE DERIVATIVES USEFUL AS AMINOCARBOXYMUCONATE SEMIALDEHYDE DECARBOXYLASE (ACMSD) INHIBITORS
-
The present invention is related to a compound represented by the following structural formula: The present invention is also related a method of treating a subject with a disease which can be ameliorated by inhibition of aminocarboxymuconate semialdehyde decarboxylase (ACMSD).
- -
-
Page/Page column 81; 82
(2018/07/29)
-
- 3-OXO-1,4-DIAZEPINYLE COMPOUNDS AS NRF2 ACTIVATORS
-
The present invention relates to bisaryl lactam compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the compounds of this invention include a compound of Formula (I):
- -
-
Page/Page column 92
(2018/07/05)
-
- ETHER LINKED TRIAZOLES AS NRF2 REGULATORS
-
The present invention relates to ether-linked triazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof:
- -
-
Page/Page column 94-95
(2018/07/05)
-
- NRF2 COMPOUNDS
-
The present invention relates to a compound which is (R)-3-(1,4- dimethyl-1 H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3- dihydropyrido[2,3-f][l,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl) propanoic acid (I), or a pharmaceutically acceptable salt
- -
-
Page/Page column 20; 44
(2018/07/05)
-
- NRF2 REGULATORS
-
The present invention relates to aryl analogs Formula (I), pharmaceutical compositions containing them and their use as Nrf2 regulators.
- -
-
Page/Page column 88
(2017/01/02)
-
- NRF2 REGULATORS
-
Provided are aryl analogs,pharmaceutical compositions containing them and their use as NRF2 regulators.
- -
-
Page/Page column 112; 113
(2017/01/02)
-
- NRF2 REGULATORS
-
The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
- -
-
Page/Page column 351
(2015/07/07)
-
- C-Aryl glucoside SGLT2 inhibitors containing a biphenyl motif as potential anti-diabetic agents
-
A series of highly active C-aryl glucoside SGLT2 inhibitors containing a biphenyl motif were designed and synthesized for biological evaluation. Among the compounds tested, compound 16l demonstrated high inhibitory activity against SGLT2 (IC50 = 1.9 nM) with an excellent pharmacokinetic profile. Further study indicated that the in vivo efficacy of compound 16l was comparable to that of dapagliflozin, suggesting that further development would be worthwhile.
- Ding, Yuyang,Mao, Liufeng,Xu, Dengfeng,Xie, Hui,Yang, Ling,Xu, Hongjiang,Geng, Wenjun,Gao, Yong,Xia, Chunguang,Zhang, Xiquan,Meng, Qingyi,Wu, Donghai,Zhao, Junling,Hu, Wenhui
-
supporting information
p. 2744 - 2748
(2015/06/08)
-
- SUBSTITUTED TOLYL FUNGICIDE MIXTURES
-
Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein A, Q, R1 and R2 are as defined in the disclosure; and (b) at least one additional fungicidal compound selected from those disclosed herein. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of the aforesaid composition.
- -
-
Page/Page column 39
(2015/11/03)
-
- TRIAZOLONE COMPOUNDS AND USES THEREOF
-
The invention disclosed herein is directed to compounds of Formula I [Formula should be inserted here] and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leuke
- -
-
Paragraph 00130
(2014/07/08)
-
- SUBSTITUTED TOLYL FUNGICIDES
-
Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, Q, R1 and R2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
- -
-
Page/Page column 28
(2014/05/24)
-
- METHODS FOR PREPARING ISOQUINOLINES
-
Provided herein are novel synthetic methods of making isoquinolines comprising coupling a metalated N-(2-methylbenzylidene)amine with a nitrile, followed by cyclization, to provide a substituted isoquinoline compound. This new methodology for preparing is
- -
-
Paragraph 00201
(2013/03/26)
-
- Intramolecular SN′-type aromatic substitution of benzylic carbonates at their para-position
-
The benzylic carbonates, which connect with an active methine through an o-phenylene tether at their meta-position, are cyclized by Pd(η3- C3H5)Cp-S-Phos catalyst, yielding 3-methyl-9,10- dihydrophenanthrenes. In the catal
- Ueno, Satoshi,Komiya, Sadakazu,Tanaka, Takeshi,Kuwano, Ryoichi
-
supporting information; experimental part
p. 338 - 341
(2012/03/10)
-
- A versatile synthesis of substituted isoquinolines
-
Lithiated o-tolualdehyde tert-butylimines were shown to condense with nitriles to form eneamido anion intermediates that were trapped in situ with various electrophiles, thus affording a diverse array of highly substituted isoquinolines, many of which are
- Si, Chong,Myers, Andrew G.
-
supporting information; experimental part
p. 10409 - 10413
(2011/12/03)
-
- 1H-INDOLE-2-CARBOXYLIC ACID DERIVATIVES USEFUL AS PPAR MODULATORS
-
The present invention relates to certain indole derivatives that are modulators of PPAR, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.
- -
-
Page/Page column 56
(2008/06/13)
-
- Difluoromethyltriazolone compounds, use of the same and intermediates for the production thereof
-
A triazolone compound of the formula [I]: wherein; R1 represents optionally substituted phenyl or the like, T represents m-phenylene optionally substituted by methyl or the like; and a fungicidal composition containing it as an active ingredient.
- -
-
-
- PHENYLALKANOIC ACID AND PHENYLOXYALKANOIC ACID DERIVATIVES AS HPPAR ACTIVATORS
-
The present invention provides a compound of formula (I):wherein:R1 and R2 are independently H or C1-3 alkyl;X represents a O or (CH2)n where n is 0, 1 or 2;R3and R4 independently represent H, C1-3 alkyl, -OCH3, -CF3, allyl, or halogen;X1 represents O, S, SO2, SO, or CH2;R5 and R6 independently represent hydrogen, C1-6 alkyl (including branched alkyl and optionally substituted by one or more halogens or C1-6alkoxy), or together with the carbon atom to which they are bonded form a 3-6 membered cycloalkyl ring;R7 represents a phenyl or a 6 membered heteroaryl group containing 1, 2 or 3 nitrogen atoms wherein the phenyl or heteroaryl group is substituted by 1, 2 or 3 moieties selected from the group consisting of halogen, C1-6 alkoxy, C1-6 alkyl, CF3, hydroxy, or phenyl (which may be optionally substituted by one or more C1-3 alkyl, -OC1-3 alkyl, CN, acetyl, hydroxy, halogen or CF3).
- -
-
-
- Triazolone derivatives, use thereof, and intermediates therefor
-
Triazolone derivatives represented by the formula wherein R1represents optionally substituted C1-10alkyl, A1—L1—, A1—ON═CA2, etc.; R2represents hydrogen, C1-6alkyl, etc.; R3represents C1-6alkoxy, etc.; one of T, U, and V represents CR4, another represents CH or nitrogen, and the remaining one represents CR5or nitrogen; and W represents CR6or nitrogen.
- -
-
-