- COMPOSITIONS AND METHODS OF USING THE SAME FOR TREATMENT OF NEURODEGENERATIVE AND MITOCHONDRIAL DISEASE
-
The present disclosure is directed to adenine analogs, methods of making adenine analogs, and methods of treating disorders associated with PINK1 kinase activity including, but not limited to, neurodegenerative diseases, mitochondrial diseases, fibrosis,
- -
-
Paragraph 0328; 0416
(2021/08/27)
-
- Ligand-Controlled Regiodivergence in Nickel-Catalyzed Hydroarylation and Hydroalkenylation of Alkenyl Carboxylic Acids**
-
A nickel-catalyzed regiodivergent hydroarylation and hydroalkenylation of unactivated alkenyl carboxylic acids is reported, whereby the ligand environment around the metal center dictates the regiochemical outcome. Markovnikov hydrofunctionalization products are obtained under mild ligand-free conditions, with up to 99 % yield and >20:1 selectivity. Alternatively, anti-Markovnikov products can be accessed with a novel 4,4-disubstituted Pyrox ligand in excellent yield and >20:1 selectivity. Both electronic and steric effects on the ligand contribute to the high yield and selectivity. Mechanistic studies suggest a change in the turnover-limiting and selectivity-determining step induced by the optimal ligand. DFT calculations reveal that in the anti-Markovnikov pathway, repulsion between the ligand and the alkyl group is minimized (by virtue of it being 1° versus 2°) in the rate- and regioselectivity-determining transmetalation transition state.
- Deng, Ruohan,Engle, Keary M.,Fu, Yue,Gao, Yang,Li, Zi-Qi,Liu, Peng,Tran, Van T.
-
supporting information
p. 23306 - 23312
(2020/10/19)
-
- Synthesis of Novel Pterocarpen Analogues via [3?+?2] Coupling-Elimination Cascade of α,α-Dicyanoolefins with Quinone Monoimines
-
By employing triethylamine as a catalyst, [3?+?2] coupling-elimination cascade of α,α-dicyanoolefins with quinone monoimines was realized. The reactions afforded various novel pterocarpen analogues with generally moderate yields (up to 75%). In addition, a plausible reaction mechanism was proposed.
- Chen, Hui,Zhao, Sihan,Cheng, Shaobing,Dai, Xingjie,Xu, Xiaoying,Yuan, Weicheng,Zhang, Xiaomei
-
p. 1672 - 1683
(2019/04/08)
-
- Highly enantioselective [3+2] coupling of cyclic enamides with quinone monoimines promoted by a chiral phosphoric acid
-
Enantioselective [3+2] coupling of cyclic enamides with quinone monoimines was realised using a chiral phosphoric acid as a catalyst. This transformation allowed for the synthesis of highly enantioenriched polycyclic 2,3-dihydrobenzofurans (up to 99.9% ee). The absolute configuration of one product was determined by an X-ray crystal structural analysis. We also found a possible mechanism for this reaction.
- Zhang, Minmin,Yu, Shuowen,Hu, Fangzhi,Liao, Yijun,Liao, Lihua,Xu, Xiaoying,Yuan, Weicheng,Zhang, Xiaomei
-
supporting information
p. 8757 - 8760
(2016/07/15)
-
- SUBSTITUTED AROMATIC CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
-
The invention relates to substituted aromatic carboxamide and urea derivatives, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions (formula (I)).
- -
-
Page/Page column 131; 133
(2010/11/18)
-
- PROCESS FOR SYNTHESIS OF AMINO-METHYL TETRALIN DERIVATIVES
-
Methods for producing a compound of formula k1 or k2 by reducing a dihydronapthalene amide compound of formula i with hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2 [in-line-formulae]Ru(Z)2(L)??j1;[/in-line-formulae] [
- -
-
Page/Page column 22
(2010/07/04)
-
- TETRALIN AND INDANE DERIVATIVES AND USES THEREOF
-
Compounds of the formula I, II or III; or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.
- -
-
-
- Arylsulfonyl naphthalene derivatives and uses thereof
-
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, q, Ar, R1, R2 and R7 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
- -
-
Page/Page column 29
(2008/06/13)
-
- 4,5-DIHYDRONAPHTHO [1,2-b] THIOPHENE DERIVATIVE
-
A 4,5-dihydronaphtho[1,2-b]thiophene derivative expressed by the formula: (wherein R1 is a C1 to C10 1-hydroxyalkyl group or a C1 to C10 acyl group, and R2 and R3 separately substitute in the 6-, 7-, 8-, or 9-positions, and are each independently a hydrogen atom, a halogen atom, a C1 to C10 alkyl group, a hydroxy group, a C1 to C10 alkoxy group, a C1 to C5 alkenyloxy group, a C1 to C5 alkynyloxy group, a benzyloxy group, or the like, provided that when R1 is an acyl group and R2 is a hydrogen atom, then R3 is neither a hydrogen atom nor an acetyl group), or a pharmaceutically acceptable salt thereof. This is a novel compound that is effective in reducing triglyceride levels in the liver and reducing blood glucose levels.
- -
-
Page/Page column 13
(2010/11/08)
-
- TETRALIN AND INDANE DERIVATIVES AND USES THEREOF
-
Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein R2 is a group of formula (II) and m, n, p, q, r, Rl and X are as defined in the claims, which are selective agonists of 5-HT6 and 5-HT2A. Also provided are compositions comprising these compounds and methods for their use in the preparation of medicaments for treating central nervous system disease states and disorders of the gastrointestinal tract.
- -
-
Page/Page column 21-22
(2008/06/13)
-
- TETRALIN AND INDANE DERIVATIVES AND USES THEREOF AS 5-HT ANTAGONISTS
-
Compounds of the formula (I) or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R 2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula (I).
- -
-
Page/Page column 23; 24
(2008/06/13)
-
- TETRALIN AND INDANE DERIVATIVES AND USES THEREOF
-
Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein R2 is (CR3R4)n-NR5R6 and m, p, q, Ar, R1, R3, R4, R5 and R6 are as defined in the claims, which are selective antagonists of 5-HT6 and/or 5-HT2A. Also provided are compositions comprising these compounds and their use in the preparation of medicaments for treating central nervous system disease states selected from psychoses, schizophrenia, manic depressions, neurological disorders, memory disorders, attention deficit disorder, Parkinson’s disease, amyotrophic lateral scierosis, Alzheimer’s disease, food uptake disorders and Huntington’s disease.
- -
-
Page/Page column 71; 72
(2008/06/13)
-
- BICYCLIC SUBSTITUTED INDOLE-DERIVATIVE STEROID HORMONE NUCLEAR RECEPTOR MODULATORS
-
The present invention provides a compound of the formula: Formula (I); or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, hypertension, and atherosclerosis, comprising administering to a patient in thereof an effective amount of a compound of Formula I. X-16125
- -
-
Page/Page column 51
(2010/02/14)
-
- Aminomethylcarboxylic acid derivatives
-
The present invention relates to aminomethylcarboxylic acid derivatives general formula (I), wherein Z is (CH2)n, O, S, SO, SO2or N—R5; n is 0, 1 or 2; X represents 1-3 substituents independently selected from hydrogen, halogen, (C1-6)alkyloxy, (C3-6)cycloalkyloxy, (C6-12)aryloxy, (C6-12)aryl, thienyl, SR6, SOR6, SO2R6, NR6R6, NHR6, NH2, NHCOR6, NSO2R6, CN, COOR6and (C1-4)alkyl, optionally substituted with halogen, (C6-12)aryl, (C1-6)alkyloxy or (C6-12)aryloxy; or 2 substituents at adjacent positions together represent a fused (C5-6)aryl group, a fused (C5-6)cycloalkyl ring or O—(CH2)m—O; m is 1 or 2; Y represents 1-3 substituents independently selected from hydrogen, halogen, (C1-4)alkyloxy, SR6, NR6R6and (C1-4)alkyl, optionally substituted with halogen; R1is COOR7or CONR8R9; R2and R6are (C1-4)alkyl; R3, R4and R5are independently hydrogen or (C1-4)alkyl; R7, R8and R9are independently hydrogen, (C1-4)alkyl, (C6-12)aryl or arylalkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these aminomethylcarboxylic acid derivatives in therapy, more specifically for the treatment of CNS disorders.
- -
-
-