- INHIBITORS OF MLH1 AND/OR PMS2 FOR CANCER TREATMENT
-
The present invention relates to compounds of Formula (I) that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process: Formula (I) wherein R1, R2, R3, R4, R6
- -
-
Paragraph 00517-005118
(2021/12/28)
-
- SUBSTITUTED ARYLMETHYLUREAS AND HETEROARYLMETHYLUREAS, ANALOGUES THEREOF, AND METHODS USING SAME
-
The present invention includes substituted arylmethyl ureas and heteroarylmethyl-ureas, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infections in a patient.
- -
-
Page/Page column 113; 114
(2020/07/07)
-
- DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF
-
The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer, reducing inflammation and/or treating an autoimmune or inflammatory disease.
- -
-
Paragraph 0367-0369
(2020/12/13)
-
- DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF
-
The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3- dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlogumine; and use of the derivatives and analogs for treating cancer.
- -
-
Page/Page column 90
(2019/06/11)
-
- ISOQUINOLINESULFONYL DERIVATIVE AS RHO KINASE INHIBITOR
-
The present invention discloses a class of isoquinolinesulfonyl derivatives as RHO kinase inhibitors, and pharmaceutical compositions thereof, and relates to pharmaceutically acceptable uses thereof. Specifically, the present invention relates to a compound as represented by formula (I), or a pharmaceutically acceptable salt thereof.
- -
-
Paragraph 0346-0349
(2017/06/12)
-
- Palladium-catalyzed reductive carbonylation of aryl halides with N-formylsaccharin as a CO source
-
Easy peasy: The title reaction employs N-formylsaccharin, which is an easily accessible crystalline compound, as an effective CO source. The reactions proceed with a small excess of the CO source at moderate temperatures and were successfully applied to a wide range of aryl bromides. DMF=N,N- dimethylformamide, dppb=1,4-bis-(diphenylphosphino)butane. Copyright
- Ueda, Tsuyoshi,Konishi, Hideyuki,Manabe, Kei
-
supporting information
p. 8611 - 8615
(2013/09/12)
-
- TRPA1 ANTAGONISTS
-
Compounds of formula (I), wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
- -
-
Page/Page column 32
(2009/09/04)
-
- Highly selective recognition of a-chiral primary organoammonium ions by C3-symmetric peptide receptors
-
A straightforward synthesis of C3-symmet:ric, imidazole-containing, macrocyclic peptides with different binding arms is presented, The chirality of the backbone and the selection of adequate receptor arms make these systems highly selective receptors for α-chiral primary organoammonium ions. Furthermore, the receptors have the ability to discriminate between enantiomeric guests with selectivity ratios of up to 87:13, The binding constants and the selectivity ratios were estimated by standard 1H NMR titration techniques in CDCl3.
- Schnopp, Markus,Haberhauer, Gebhard
-
experimental part
p. 4458 - 4467
(2010/02/16)
-
- 4-AMINO-PIPERIDINE DERIVATIVES AS MONOAMINE UPTAKE INHIBITORS
-
The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such,
- -
-
Page/Page column 60; 61
(2008/06/13)
-
- Amide compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
-
Amide compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.
- -
-
-
- Preparation of 2-alkyl- and 2-acylpropenals from 5-(trifluoromethanesulfonyloxy)-4H-1,3-dioxin: A versatile acrolein α-cation synthon
-
5-(Trifluoromethanesulfonyloxy)-4H-1,3-dioxin (3) participates in a variety of nucleophilic substitution reactions with cuprate reagents or in palladium catalyzed cross-coupling reactions to provide 5-substituted-4H-1,3-dioxins 5. Upon thermolysis, these compounds undergo facile retrocycloaddition reactions to generate the corresponding 2-substituted acroleins which, if necessary, can be trapped in situ with dienes or heterodienophiles. In particular, the heretofore unknown 2-acylacroleins can be generated using this methodology and trapped with enol ethers to afford 5-acyl-3,4-dihydro-2H-pyrans (6g,h), a substructural unit common to many natural products. (C) 2000 Elsevier Science Ltd.
- Fearnley, Stephen P.,Funk, Raymond L.,Gregg, Robert J.
-
p. 10275 - 10281
(2007/10/03)
-
- Formylations of anions with a 'Weinreb' formamide: N-methoxy-N-methylformamide
-
Treatment of organolithiums, Grignard reagents, or enolates with N-methoxy-N-methylformamide leads to formylated products in good yields without competing secondary processes.
- Lipshutz, Bruce H.,Pfeiffer, Steven S.,Chrisman, Will
-
p. 7889 - 7892
(2007/10/03)
-
- New strategy for the preparation of nitrogen- and phosphorus-containing chiral polyfunctional secondary alcohols
-
The use of borane-derived protecting groups for aldehydes containing pyridine and phosphine functionalities allows the performance of highly enantioselective additions of functionalized diorganozincs leading to polyfunctional chiral hydroxy-pyridines and
- Lutz, Christian,Graf, Claus-Dieter,Knochel, Paul
-
p. 10317 - 10328
(2007/10/03)
-
- Isoquinoline thromboxane synthetase inhibitors
-
4-[(4-Isoquinolinylmethyl)amino]benzoic acid derivatives useful as selective thromboxane synthetase inhibitors are described herein. The compounds are obtained from the appropriate 4-isoquinolinecarboxylic acid derivative and an aminobenzoic acid derivati
- -
-
-
