- Copper-Catalyzed Reaction of C60 with Tertiary Amines for the Preparation of Spiro-Linked Methanofullerenes and Fullerenoalkanals
-
CuI-catalyzed reaction of C60 with tertiary amines by using air as the sole oxidant has been developed. Spiro-linked methanofullerenes bearing cyclic amides and fullerenoalkanals can be obtained selectively using the cyclic and acyclic amines a
- Liu, Yong-Jian,Ge, Jie,Miao, Chun-Bao,Yang, Hai-Tao
-
-
Read Online
- Distance of hydroxyl functionality from the quaternized center influence DNA binding and in vitro gene delivery efficacies of cationic lipids with hydroxyalkyl headgroups
-
In vitro gene delivery efficacies of cationic amphiphiles 1-7 (Scheme 1) were measured by both the reporter gene expression assays in CHO, COS-1, HepG2, and MCF7 cells and by the whole cell histochemical X-gal staining of representative Chinese hamster ovary cells. Our results demonstrated that in vitro gene delivery efficiencies of cationic lipids with hydroxyalkyl headgroups are adversely affected by increased covalent distances between the hydroxyl functionality and the cationic centers. Findings in the DNase I protection experiments and transmission electron microscopic study support the notion that such compromised gene delivery efficacies may originate from poor lipid - DNA binding interactions and significantly increased lipoplex nanosizes.
- Mahidhar, Yenugonda Venkata,Rajesh, Mukthavaram,Madhavendra, Sunkara Sakunthala,Chaudhuri, Arabinda
-
-
Read Online
- Acid-Catalyzed Intramolecular Ring-Opening Reactions of Cyclopropanated Oxabenzonorbornadienes with Carboxylic Acid Nucleophiles
-
The present work demonstrates the ability of carboxylic acid tethered cyclopropanated oxabenzonorbornadienes (CPOBDs) to undergo ring-opening reactions in mild acidic conditions. The optimized reaction conditions involve the use of pTsOH in DCE at 90 °C. Two regioisomers are formed but the reactions are highly regioselective towards type 3 ring-opened products. It was observed that substitution at the C5 and aryl positions of CPOBD significantly hinders the ring-opening reactions leading to decreased yields of ring-opened products, although high regioselectivity for the Type 3 ring-opened products is still maintained. Herein, the first examples of acid-catalyzed intramolecular ring-opening reactions of CPOBD with carboxylic acid nucleophiles are reported.
- Ho, Angel,Pounder, Austin,Koh, Samuel,Macleod, Matthew P.,Carlson, Emily,Tam, William
-
p. 1422 - 1430
(2021/12/02)
-
- Degradable resin monomer synthesized from dicyclohexylketone and preparation method of degradable resin monomer
-
The invention belongs to a degradable photoresist resin monomer, and discloses a degradable resin monomer synthesized from dicyclohexylketone and a preparation method of the degradable resin monomer.The structural formula of the resin monomer is shown in
- -
-
Paragraph 0026-0029
(2021/04/03)
-
- Degradable resin monomer synthesized from 2 -cyclopentyl cyclopentanone and preparation method and application thereof
-
The invention relates to the technical field of photoresist and discloses a degradable resin monomer synthesized from 2 - cyclopentylcyclopentanone and a preparation method and application thereof. Wherein R is an alkyl group or a heteroalkyl group. Under the action of the acid, the tert-butyl structure is broken, so that the edge roughness of the photoresist is improved, the resolution of the photoresist is improved, the dissolution in the developing process is improved, the dissolving speed of the photoresist in the developing solution is increased, and the contrast of the photoresist is increased.
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-
Paragraph 0042-0045
(2021/09/26)
-
- SMALL MOLECULE VE-PTP INHIBITORS
-
The present disclosure relates to compounds capable of inhibiting vascular endothelial protein tyrosine phosphatase (VE-PTP). These compounds are also capable of activating Tie2 receptor-mediated signaling. The present disclosure also relates to pharmaceutically acceptable salts of said compounds, to pharmaceutical compositions comprising such compounds and/or pharmaceutically acceptable salts thereof, and to the use of such compounds, pharmaceutically acceptable salts thereof, and/or pharmaceutical compositions comprising the same in treating diseases and/or conditions mediated by VE-PTP signaling, such as those mediated by Angiopoietm/Tie2 signaling.
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Page/Page column 248
(2022/01/05)
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- PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
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Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.
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-
Paragraph 0837-0839
(2020/02/16)
-
- Multiaction Platinum(IV) Prodrug Containing Thymidylate Synthase Inhibitor and Metabolic Modifier against Triple-Negative Breast Cancer
-
Multifunctional platinumIV anticancer prodrugs have the potential to enrich the anticancer properties and overcome the clinical problems of drug resistance and side effects of platinumII anticancer agents. Herein, we develop dual and triple action platinumIV complexes with targeted and biological active functionalities. One complex (PFL) that consists of cisplatin, tegafur, and lonidamine exhibits strong cytotoxicity against triple negative breast cancer (TNBC) cells. Cellular uptake and distribution studies reveal that PFL mainly accumulates in mitochondria. As a result, PFL disrupts the mitochondrial ultrastructure and induces significant alterations in the mitochondrial membrane potential, which further leads to an increase in production of reactive oxygen species (ROS) and a decrease in ATP synthesis in MDA-MB-231 TNBCs. Western blot analysis reveals the formation of ternary complex of thymidylate synthase, which shows the intracellular conversion of tegafur into 5-FU after its release from PFL. Furthermore, treatment with PFL impairs the mitochondrial function, leading to the inhibition of glycolysis and mitochondrial respiration and induction of apoptosis through the mitochondrial pathway. The RNA-sequencing experiment shows that PFL can perturb the pathways involved in DNA synthesis, DNA damage, metabolism, and transcriptional activity. These findings demonstrate that PFL intervenes in several cellular processes including DNA damage, thymidylate synthase inhibition, and perturbation of the mitochondrial bioenergetics to kill the cancer cells. The results highlight the significance of a triple-action prodrug for efficient anticancer therapy for TNBCs.
- Ji, Liang-Nian,Mao, Zong-Wan,Muhammad, Nafees,Nasreen, Sadia,Nawaz, Uroosa,Tan, Cai-Ping,Wang, Fang-Xin,Wang, Jie
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p. 12632 - 12642
(2020/09/12)
-
- Compound
-
PROBLEM TO BE SOLVED: To provide a compound capable of forming a color filter excellent in heat resistance. SOLUTION: The present invention provides a compound represented by formula (I). [In formula (I), R1-R8 independently represen
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-
Paragraph 0195-0197
(2020/05/02)
-
- Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation
-
The efficacy of EGFR inhibitors is frequently affected by acquired resistance. EGFR19D/T790M/C797S mutation is one of the primary reasons for the emergence of resistance after treatment with the third-generation EGFR inhibitors such as AZD9291, CO1686 and Olmutinib. To overcome the resistance mutation 19D/T790M/C797S, we designed and prepared a series of indole derivatives with the terminal hydroxyl of alkyl chain to increase extra interaction with the Asp855 in the conservative DFG site. Activity evaluation, structure-activity relationship and docking analysis were also carried out. Among them, compound 12e displayed significant inhibitory activity against EGFR19D/T790M/C797S (IC50 = 15.3 nM) and good selectivity over EGFR WT (IC50 > 1000 nM), L858R/T790M (IC50, 156.6 nM) and L858R/T790M/C797S (IC50, 218.3 nM) respectively. Furthermore, 12e exhibited good growth inhibition activity, induced G1 phase cell cycle arrest and apoptosis in BaF3/EGFR19D/T790M/C797S cells by suppressing EGFR phosphorylation signaling pathway. In all, our study might provide a novel structural design method and lay the solid foundation for the development of the 4th generation EGFR19D/T790M/C797S inhibitors.
- Chen, Zhuo,Lai, Mengzhen,Li, Honglin,Li, Shengqing,Su, Zhicheng,Tong, Linjiang,Wang, Jie,Wumaier, Gulinuer,Xie, Hua,Yang, Tingyuan,Zhao, Zhenjiang
-
supporting information
(2020/06/26)
-
- PHOSPHONATE CONJUGATES AND USES THEREOF
-
Phosphonate conjugates, preferably, bisphosphonate conjugates; methods of inhibiting Ron receptor tyrosine kinase and methods of treatment of bone destruction due to cancer or other conditions utilizing the provided phosphonate conjugates.
- -
-
Paragraph 00145
(2020/07/31)
-
- Investigation of B,C-ring truncated deguelin derivatives as heat shock protein 90 (HSP90) inhibitors for use as anti-breast cancer agents
-
On the basis of deguelin, a series of the B,C-ring truncated surrogates with N-substituted amide linkers were investigated as HSP90 inhibitors. The structure activity relationship of the template was studied by incorporating various substitutions on the nitrogen of the amide linker and examining their HIF-1α inhibition. Among them, compound 57 showed potent HIF-1α inhibition and cytotoxicity in triple-negative breast cancer lines in a dose-dependent manner. Compound 57 downregulated expression and phosphorylation of major client proteins of HSP90 including AKT, ERK and STAT3, indicating that its antitumor activity was derived from the inhibition of HSP90 function. The molecular modeling of 57 demonstrated that 57 bound well to the C-terminal ATP-binding pocket in the open conformation of the hHSP90 homodimer with hydrogen bonding and pi-cation interactions. Overall, compound 57 is a potential antitumor agent for triple-negative breast cancer as a HSP90 C-terminal inhibitor.
- Kim, Ho Shin,Hoang, Van-Hai,Hong, Mannkyu,Chul Kim, Kyung,Ann, Jihyae,Nguyen, Cong-Truong,Seo, Ji Hae,Choi, Hoon,Yong Kim, Jun,Kim, Kyu-Won,Sub Byun, Woong,Lee, Sangkook,Lee, Seungbeom,Suh, Young-Ger,Chen, Jie,Park, Hyun-Ju,Cho, Tae-Min,Kim, Ji Young,Seo, Jae Hong,Lee, Jeewoo
-
supporting information
p. 1370 - 1381
(2019/03/04)
-
- MACROCYCLIC CHLORINE SUBSTITUTED INDOLE DERIVATIVES
-
The present invention relates to macrocyclic indole derivatives of general formula (I) : (I), in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active 10 ingredients.
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-
Page/Page column 429; 430
(2019/06/13)
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- SUBSTITUTED DIHYDROINDENE-4-CARBOXAMIDES AND ANALOGS THEREOF, AND METHODS USING SAME
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The present invention includes novel substituted bicyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infections in a patient. In certain embodiments, the compounds and compositions of the invention are capsid inhibitors. (Formula I)
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-
Page/Page column 279; 284
(2018/10/19)
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- Synthetic Studies of Haliclonin A: Construction of the 3-Azabicyclo[33.1]nonane Skeleton with a Bridge that Forms the 17-Membered Ring
-
The core structure of haliclonin A, a 3-azabicyclo[3.3.1]nonane with a bridge that forms a 17-membered ring, was constructed. The synthesis features a ring-closing metathesis that constructs the macrocyclic ring, the stereoselective introduction of carbon units via the intramolecular cyclopropanation of a diazoester, the conjugate addition of an organocopper reagent, and the formation of 3-azabicyclo [3.3.1] nonane skeleton via an unexpected 1,5-hydride shift.
- Orihara, Kensuke,Kawagishi, Fumiki,Yokoshima, Satoshi,Fukuyama, Tohru
-
supporting information
p. 769 - 772
(2018/03/26)
-
- AZABENZIMIDAZOLE DERIVATIVES AS PI3K BETA INHIBITORS
-
The present invention relates to azabenzimidazole derivatives of Formula (I) (I) wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active 10 ingredient as well as the use of said compounds as a medicament.
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-
Page/Page column 78
(2018/01/19)
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- 3-(5-FLUOROINDOLYL)-4-ARYLMALEIMIDE COMPOUNDS AND THEIR USE IN TUMOR TREATMENT
-
The present invention relates to 3-(5-fluoroindolyl)-4-arylmaleimide compounds, pharmaceutical compositions containing them. The compounds of the present invention have antineoplastic activity. They can therefore be used for the treatment or prevention of
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-
Paragraph 0041; 0042
(2017/07/14)
-
- NOVEL SGLT INHIBITORS
-
The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synt
- -
-
Paragraph 0124
(2017/06/23)
-
- Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole
-
Due to the low esterase activity in human plasma, many ester and carbonate prodrugs tested in humans may be less effective than that in preclinical animals. In this letter, PTX and SN-38 were attached to the N-1 position of 2-nitroimidazole via a carbonate linker. Presumably, 2-aminoimidazole may help promote the intramolecular hydrolysis of the carbonate bond. The prodrugs exhibited a considerable stability in buffers at different pH values as well as in human plasma. Furthermore, a rapid reduction was exhibited in the presence of nitroreductase. An in vitro cytotoxicity assay demonstrated that hypoxic conditions could increase the toxicity of prodrugs. Potentially, the compound species may form a new class of promising antitumor agents.
- Jin, Chen,Wen, Shuai,Zhang, Qiumeng,Zhu, Qiwen,Yu, Jiahui,Lu, Wei
-
supporting information
p. 762 - 765
(2017/07/22)
-
- Hypoxia-activated prodrug based on 2-nitroimidazole-1-alkanol
-
The invention discloses a hypoxia-activated prodrug based on 2-nitroimidazole-1-alkanol. The 2-nitroimidazole-1-alkanol of the prodrug is connected to an antineoplastic drug through a carbonate bond. The prodrug has a structure shown in the formula I and
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-
Paragraph 0048; 0049; 0050; 0051
(2017/08/29)
-
- Synthesis of Macrocyclic Lactones via Ring Transformation of 4-(ω-Hydroxyalkyl)-1,3-oxazol-5(4H)-ones
-
The synthesis of α-benzamido-α-benzyl lactones 23 of various ring size was achieved either via ‘direct amide cyclization’ by treatment of 2-benzamido-2-benzyl-ω-hydroxy-N,N-dimethylalkanamides 21 in toluene at 90 – 110° with HCl gas or by ‘ring transformation’ of 4-benzyl-4-(ω-hydroxyalkyl)-2-phenyl-1,3-oxazol-5(4H)-ones under the same conditions. The precursors were obtained by C-alkylations of 4-benzyl-2-phenyl-1,3-oxazol-5(4H)-one (15) with THP- or TBDMS-protected ω-hydroxyalkyl iodides. Ring opening of the THP-protected oxazolones by treatment with Me2NH followed by deprotection of the OH group gave the diamides 21, whereas deprotection of the TBDMS series of oxazolones 25 with TBAF followed by treatment with HCl gas led to the corresponding lactones 23 in a one-pot reaction.
- Fritschi, Stephan P.,Linden, Anthony,Heimgartner, Heinz
-
p. 523 - 538
(2016/07/22)
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- INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-c]PYRIDIN-2-ONE DERIVATIVES
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The present invention is concerned with indolin-2-one and l,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula (I) wherein Ar1 is phenyl, pyridinyl or pyrimidinyl; Ar2 is a 5 or 6 membered heteroaryl group, containing 2 or 3 heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, halogen or lower alkoxy; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, lower alkyl substituted by hydroxy, cycloalkyl, oxetan-3-yl, pyridinyl, imidazolyl, pyrazolyl, pyrimidinyl, which rings may optionally substituted by lower alkyl, or is -(CH2)3-S(O)2-cyclopropyl; X is CH or N; n is 1 or 2; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof, for use in the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.
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-
Page/Page column 118
(2015/12/08)
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- HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY
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Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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-
Paragraph 0348; 0349
(2015/11/16)
-
- COMPOUNDS FOR REGULATING FAK AND/OR SRC PATHWAYS
-
The present application provides novel optionally substituted fused pyridine and pyrimidine bicyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating FAK and/or Src activity by administering a therapeutically effective amount of one or more of the compounds to a subject. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the FAK and/or Src pathway. Advantageously, these compounds perform as dual FAK and/or Src inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
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Paragraph 166
(2015/03/28)
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- The flocculated acryloyldimethyltauric molecule ligand
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Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.
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-
Paragraph 0797; 0798
(2016/10/08)
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- Photoageing of cardanol: Characterization, circumvention by side chain methoxylation and application for photocrosslinkable polymers
-
The photosensitivity of cardanol has been evaluated using a multi-technique approach. Among other techniques, size exclusion chromatography, matrix assisted laser desorption ionization mass spectrometry and their off line coupling provided useful details
- Fouquet,Fetzer,Mertz,Puchot,Verge
-
p. 54899 - 54912
(2015/07/07)
-
- GGA DERIVATIVES
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This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.
- -
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Paragraph 0358; 0360
(2015/05/26)
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- METHODS FOR TREATING NEURON DAMAGE
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This invention relates to the use of geranylgeranyl acetone (GGA), its isomers, and GGA derivatives in a method for for treating a disease in a subject mediated in part by miRNA-378 or miRNA-711 increased activity comprising administering to the subject a therapeutically effective amount of 5-trans-GGA or a derivative thereof.
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-
Paragraph 0310
(2014/07/22)
-
- GGA AND GGA DERIVATIVES COMPOSITIONS THEREOF AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES INCLUDING PARALYSIS INCLUDING THEM
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This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.
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Paragraph 0298
(2014/10/18)
-
- NITROIMIDAZOXADIAZOCINE COMPOUNDS
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This invention relates to nitroimidazoxadiazocine compounds having the general Formula I, pharmaceutical compositions and uses of the same. The invention also relates to methods of making such nitroimidazoxadiazocine compounds of Formula I.
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Page/Page column 52; 53
(2013/06/05)
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- NOVEL SGLT INHIBITORS
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The present invention relates to novel compounds of Formula (I), their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the sy
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Page/Page column 55-56
(2013/03/28)
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- Allylation reactions of aldehydes with allylboronates in aqueous media: Unique reactivity and selectivity that are only observed in the presence of water
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Zn(OH)2-catalyzed allylation reactions of aldehydes with allylboronates in aqueous media have been developed. In contrast to conventional allylboration reactions of aldehydes in organic solvents, the α-addition products were obtained exclusively. A catalytic cycle in which the allylzinc species was generated through a B-to-Zn exchange process is proposed and kinetic studies were performed. The key intermediate, an allylzinc species, was detected by HRMS (ESI) analysis and by online continuous MS (ESI) analysis. This analysis revealed that, in aqueous media, the allylzinc species competitively reacted with the aldehydes and water. An investigation of the reactivity and selectivity of the allylzinc species by using several typical allylboronates (6a, 6b, 6c, 6d) clarified several important roles of water in this allylation reaction. The allylation reactions of aldehydes with allylboronic acid 2,2-dimethyl-1,3-propanediol esters proceeded smoothly in the presence of catalytic amounts of Zn(OH)2 and achiral ligand 4d in aqueous media to afford the corresponding syn-adducts in high yields with high diastereoselectivities. In all cases, the α-addition products were obtained and a wide substrate scope was tolerated. Furthermore, this reaction was applied to asymmetric catalysis by using chiral ligand 9. Based on the X-ray structure of the Zn-9 complex, several nonsymmetrical chiral ligands were also found to be effective. This reaction was further applied to catalytic asymmetric alkylallylation, chloroallylation, and alkoxyallylation processes and the synthetic utility of these reactions has been demonstrated. Still waters run deep: The Zn(OH)2-catalyzed allylation of aldehydes with allylboronates in aqueous media exclusively afford the α-addition products. This reaction was also applied to alkylallylation, chloroallylation, and alkoxyallylation reactions. The role of water is discussed. Copyright
- Kobayashi, Shu,Endo, Toshimitsu,Yoshino, Takumi,Schneider, Uwe,Ueno, Masaharu
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supporting information
p. 2033 - 2045
(2013/09/23)
-
- GGA AND GGA DERIVATIVES, COMPOSITIONS THEREOF AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES INCLUDING PARALYSIS INCLUDING THEM
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This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives.
- -
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Paragraph 0284; 0286
(2013/09/12)
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- Efficient synthesis and cell-based silencing activity of siRNAS that contain triazole backbone linkages
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An efficient synthesis of siRNAs modified at the backbone with a triazole functionality is reported. Through the use of 4,4×-dimethoxytrityl (DMT) phosphoramidite chemistry, triazole backbone dimmers were site-specifically incorporated throughout various siRNAs targeting both firefly luciferase and glyceraldehyde- 3-phosphate dehydrogenase (GAPDH) gene transcripts as representatives of an exogenous and endogenous gene, respectively. Following the successful silencing of the firefly luciferase reporter gene, triazole-modified siRNAs were also found to be capable of silencing GAPDH in a dose-dependent manner. Backbone modifications approaching the 3×-end on the sense strand were tolerated without compromising siRNA potency. This study highlights the compatibility of triazole-modified siRNAs within the RNAi pathway, and the modification's potential to impart favorable properties to siRNAs designed to target other endogenous genes.
- Efthymiou, Tim C.,Huynh, Vanthi,Oentoro, Jaymie,Peel, Brandon,Desaulniers, Jean-Paul
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supporting information; experimental part
p. 1722 - 1726
(2012/04/04)
-
- RADIATION SENSITIVE RESIN COMPOSITION, METHOD FOR FORMING A PATTERN, POLYMER AND COMPOUND
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A radiation sensitive resin composition includes a first polymer having a group represented by a following formula (1), and a radiation sensitive acid generator. n is an integer of 2 to 4. X represents a single bond or a bivalent organic group. A represen
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Page/Page column 30
(2012/11/08)
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- METHODS FOR TREATING NEURODEGENERATIVE DISEASES
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This invention relates to the 5-cis and 5-trans isomers of geranylgeranyl acetone, preferably such synthetic isomers, and pharmaceutical compositions containing such isomers. Other aspects of this invention relate to the use of geranylgeranyl acetone and its isomers in methods for inhibiting neural death, increasing neural activity, and increasing axon growth and cell viability. Geranylgeranyl acetone is a known anti-ulcer drug used commercially and in clinical situations. GGA has also been shown to exert cytoprotective effects on a variety of organs, such as the eye, brain, and heart.
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Page/Page column 40-41
(2012/03/26)
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- Conjugated 3-(indolyl)- and 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
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The present invention relates to 3-(Indolyl)- and 3-(azaindolyl)-4-phenylmaleimide compounds of formula I wherein R1, R2 and R3 are as defined in the description, and the physiologically acceptable salts, solvates and solv
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Page/Page column 17
(2012/07/27)
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- CONJUGATED 3-(INDOLYL)- AND 3-(AZAINDOLYL)-4-ARYLMALEIMIDE COMPOUNDS AND THEIR USE IN TUMOR TREATMENT
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The present invention relates to 3-(Indolyl)- and 3-(azaindolyl)-4-phenylmaleimide compounds of formula (I) wherein R1, R2 and R3 are as defined in the description, and the physiologically acceptable salts, solvates and so
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Page/Page column 26
(2012/07/13)
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- 3-(INDOLYL)- OR 3-(AZAINDOLYL)-4-ARYLMALEIMIDE COMPOUNDS AND THEIR USE IN TUMOR TREATMENT
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The present invention relates to a compound of formula (I) wherein R, R and R are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors
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Page/Page column 23; 24
(2011/07/07)
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- One-pot regioselective synthesis and X-ray crystal structure of a stable [60]fullerene trisadduct with the eedge,eface,trans-1 addition pattern
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The Bingel functionalisation of C60 with a structurally novel tether equipped with three reactive malonate groups afforded a C 2v-symmetrical eedge,eface,trans-1 trisadduct in a complete regioselective manner an
- Riala, Maria,Markoulides, Marios S.,Moushi, Eleni E.,Chronakis, Nikos
-
scheme or table
p. 11948 - 11950
(2011/12/02)
-
- ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
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Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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Page/Page column 122
(2012/01/05)
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- 5-LIPOXYGENASE INHIBITORS
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The present invention relates to pyrazole derivatives of formula 1 and to process as for their synthesis as 5-lipoxygenase (5-LO) inhibitors. The present invention also relates to pharmacological compositions containing these pyrazole derivatives, as well as, methods of treating bronchial asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis, Type I diabetes, psoriasis, allograft rejection, inflammatory bowel disease, ulcerative colitis, acne, atherosclerosis, cancer, pruritis, allergic rhinitis and other inflammatory and/or autoimmune disorders.
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Page/Page column 58
(2012/01/13)
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- A HTS assay for the detection of organophosphorus nerve agent scavengers
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A new pro-fluorescent probe aimed at a HTS assay of scavengers is able to selectively and efficiently cleave the P-S bond of organophosphorus nerve agents and by this provides non-toxic phosphonic acid has been designed and synthesised. The previously described pro-fluorescent probes were based on a conventional activated P-Oaryl bond cleavage, whereas our approach uses a self-immolative linker strategy that allows the detection of phosphonothioase activity with respect to a non-activated P-Salkyl bond. Further, we have also developed and optimised a high-throughput screening assay for the selection of decontaminants (chemical or biochemical scavengers) that could efficiently hydrolyse highly toxic V-type nerve agents. A preliminary screening, realised on a small α-nucleophile library, allowed us to identify some preliminary "hits", among which pyridinealdoximes, α-oxo oximes, hydroxamic acids and, less active but more original, amidoximes were the most promising. Their selective phosphonothioase activity has been further confirmed by using PhX as the substrate, and thus they offer new perspectives for the synthesis of more potent V nerve agent scavengers.
- Louise-Leriche, Ludivine,Paunescu, Emilia,Saint-Andre, Geraldine,Baati, Rachid,Romieu, Anthony,Wagner, Alain,Renard, Pierre-Yves
-
experimental part
p. 3510 - 3523
(2010/07/06)
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- NOVEL ORTHO-AMINOANILIDES FOR THE TREATMENT OF CANCER
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The present invention is directed to a compound of formula I, and processes for the manufacture of said compounds as well as medicaments containing said compound. The compounds according to this invention show anti-proliferative and differentiation-induci
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Page/Page column 34
(2010/04/23)
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- MUSCARINIC RECEPTOR ANTAGONISTS
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The present invention generally relates to muscarinic receptor antagonists of formula I, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. Formula (I) wherein Het: is heterocyclyl or heteroaryl X: O, S or NR1 and the other substituents are defined as in the claims.
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Page/Page column 8
(2010/06/19)
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- NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID
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A compound effective as a probe targeting amyloid for image diagnosis and a reagent comprising the compound for detecting amyloid deposited on a biological tissue are provided. Provided are a compound represented by the following formula (1): wherein R1, R2 and R3 independently represent a group selected from the group consisting of a hydrogen, hydroxyl group, alkyl substituent with 1 to 4 carbon atoms, alkoxy substituent having alkyl chain with 1 to 4 carbon atoms and halogen substituent, excluding the case where two or more of the substituents R1, R2 and R3 are hydrogen, R4 is a group selected from the group consisting of a hydrogen, hydroxy group, alkoxy substituent having alkyl chain with 1 to 4 carbon atoms and halogen substituent, and m is an integer of 1 to 4, provided that at least one of R1, R2, R3 and R4 represents a radioactive halogen substituent, and a reagent comprising the same.
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Page/Page column 13; 26
(2010/08/09)
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- MACROCYCLIC GHRELIN RECEPTOR MODULATORS AND METHODS OF USING THE SAME
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The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
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Page/Page column 55
(2008/12/07)
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- MUSCARINIC RECEPTOR ANTAGONISTS
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This present invention generally relates to muscarinic receptor antagonists, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The inve
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Page/Page column 25
(2008/12/07)
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- Integrase inhibitors
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Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
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Page/Page column 47
(2008/06/13)
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- SWALLOWTAIL MOTIFS FOR IMPARTING WATER SOLUBILITY TO PORPHYRINIC COMPOUNDS
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Porphyrinic compounds that contain solubilizing groups are described, along with methods of making and using the same and compositions comprising such compounds. Examples of such compounds include compounds compounds of Formula (I) wherein: Z is a porphyr
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Page/Page column 71-72; 84-85
(2008/06/13)
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- NOVEL THIENOPYRIMIDINE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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The present invention relates to a novel thienopyrimidine derivative having an excellent anti? inflammatory and anti-cancer activity, or a pharmaceutically acceptable salt thereof, a process for the preparation thereof and a pharmaceutical composition comprising the same. The compound according to the present invention strongly inhibits IKB kinase-β (IKK-β) involved in the activation of a transcriptional factor, NF-κB, which is associated with inducing various immune and inflammatory diseases, whereby a composition comprising the compound is a useful therapeutic agent against inflammatory diseases, in particular, arthritis and cancer.
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Page/Page column 110-111
(2010/11/28)
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