- A polyfluorene based zwitterionic fluorescent probe for response towards biological species in aqueous media
-
Water soluble zwitterionic fluorescent conjugated boronic acid-bearing polyfluorene (PFBA) has been prepared from poly(9,9′-(6″-bromohexyl) fluorene-co-alt-1,4-phenylene) (polymer 3) through a post-polymerized quaternization with 3-pyridineboronic acid. Titration of diol containing monosaccharides (d-glucose and d-fructose), l-ascorbic acid and l-DOPA with PFBA polymer in 0.1 M phosphate buffer (pH 7.4) solution results in significant concentration dependent quenching of the blue fluorescence of the polymer due to static quenching as the bio-analytes form a ground state boronate ester complex with PFBA. Upon addition of d-glucose, the emission colour of PFBA changes to greenish-yellow owing to the effective induced aggregated polymer structure. PFBA also exhibits maximum response to the biological analytes at pH 7.4 which provides a scope for PFBA to be used in biological systems.
- Chakraborty, Chanchal,Bera, Manas Kumar,Malik, Sudip
-
-
Read Online
- An M2L4 molecular capsule with an anthracene shell: Encapsulation of large guests up to 1nm
-
A new M2L4 molecular capsule with an aromatic shell was prepared using two Pd(II) ions and four bisanthracene ligands. The self-assembled capsule possesses a cavity with a diameter of ～1 nm that can encapsulate medium-sized spherical and planar molecules as well as a very large molecule (C60) in quantitative yields. The encapsulated guests are fully segregated and shielded from the external environment by the large anthracene panels.
- Kishi, Norifumi,Li, Zhiou,Yoza, Kenji,Akita, Munetaka,Yoshizawa, Michito
-
-
Read Online
- SYNTHESIS OF 5-(3-PYRIDYL)-2,2'-BITHIOPHENE(SENSITIZER)
-
Disclosed herein is a novel simple, short process for synthesis of the photosensitizer, 5-(3-pyridyl)-2,2'-bithiophene.
- -
-
Page/Page column 10-11
(2021/02/05)
-
- 2-amino-5-heterocyclyl-substituted pyrazine derivative and application thereof
-
The invention provides a 2-amino-5-heterocyclyl-substituted pyrazine derivative with a chemical structure shown in a formula 1, a pharmaceutical preparation containing the 2-amino-5-heterocyclyl-substituted pyrazine derivative, and application of the 2-amino-5-heterocyclyl-substituted pyrazine derivative in medicines for treating or preventing malaria. The compound provided by the invention has effects significantly superior to those of the prior art against plasmodium falciparum proliferation and against plasmodium falciparum of different strains, and has a longer half-life period, a lower plasma clearance rate, a higher distribution volume and better oral bioavailability.
- -
-
Paragraph 0108-0109; 0111; 0113-0114; 0116; 0118-0119; 0121
(2021/01/11)
-
- New compounds and organic light-emitting diode including the same
-
PURPOSE: A compound is provided to improve luminous efficiency and to make low voltage operation possible when applied to an organic electroluminescence device by having low driving voltage and excellent luminous efficiency. CONSTITUTION: A compound is represented by chemical formula 1. In chemical formula 1, each R is selected from hydrogen, deuterium, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C7-30 alkyl, substituted or unsubstituted C3-30 cycloalkyl, substituted or unsubstituted C5-30 cycloalkenyl, substituted or unsubstituted C1-30 alkoxy, substituted or unsubstituted C6-30 aryloxy, substituted or unsubstituted C1-30 alkylthioxy, substituted or unsubstituted C5-30 arylthioxy, substituted or unsubstituted C1-30 alkylamine, substituted or unsubstituted C5-30 arylamine, substituted or unsubstituted C5-50 aryl, substituted or unsubstituted C3-50 heteroaryl, substituted or unsubstituted silicon, substituted or unsubstituted boron, substituted or unsubstituted silane, carbonyl, phosphoryl, amino, nitrile, hydroxy, nitro, halogen, amide, and ester.
- -
-
Paragraph 0200-0206; 0252; 0255-0258
(2019/08/30)
-
- Iridium metal organic complex and organic light-emitting device thereof
-
The invention provides an iridium metal organic complex and an organic light-emitting device thereof and relates to the technical field of organic optoelectronic materials. An electron-rich double-nitrogen coordination structure in a complex structure is good for stabilizing trivalent iridium ions at the center; a four-membered ring composed of a ligand of the double-nitrogen coordination structure and metal has stronger rigidity, so that higher chemical stability and thermal stability are obtained and the light-emitting efficiency of the complex is improved. The synthesis is simple and easy to operate, and the iridium metal organic complex can be applied to the organic light-emitting device and is used as a light-emitting layer doping material; the problems of the organic light-emitting device that the light-emitting efficiency is low and the driving voltage is high can be effectively solved. The iridium complex is prepared into the device and is especially used as the doping material; the device has the advantages of low driving voltage and high light-emitting efficiency, and is better than a existing common OLED (Organic Light Emitting Diode).
- -
-
Paragraph 0065; 0066; 0067; 0068; 0069
(2018/12/14)
-
- Preparation method of mono-heterocyclic boric acid
-
The invention provides a preparation method of mono-heterocyclic boric acid. The preparation method comprises steps as follows: (1) a compound shown in a formula I and alkyl borate are dissolved in asolvent A, and a liquor A is obtained; an organic lithium reagent is dissolved in a solvent B, and a liquor B is obtained; the liquor A and the liquor B are subjected to a continuous feeding reaction,the reaction is ended after a product flows out of a reaction pipe, and an intermediate is obtained; (2) the intermediate obtained in the step (1) is subjected to a hydrolysis reaction, and mono-heterocyclic boric acid is obtained. According to the provided preparation method, the reaction yield can be increased and can be up to 95% or above, the reaction time is shortened, the reaction can be completed within 5-60 min, the reaction temperature can be increased, energy consumption of the low-temperature reaction is reduced, the temperature is controllable, the safety is improved, the pressureis convenient to control, the automation degree is improved, production operation is facilitated, the cost is reduced, and the economic benefits are improved.
- -
-
Paragraph 0050; 0052; 0067; 0069; 0071; 0073; 0075
(2018/09/13)
-
- Synthesis of Pyridylanthracenes and Their Reversible Reaction with Singlet Oxygen to Endoperoxides
-
The ortho, meta, and para isomers of 9,10-dipyridylanthracene 1 have been synthesized and converted into their endoperoxides 1-O2 upon oxidation with singlet oxygen. The kinetics of this reaction can be controlled by the substitution pattern an
- Fudickar, Werner,Linker, Torsten
-
p. 9258 - 9262
(2017/09/11)
-
- Efficient metal-free photochemical borylation of aryl halides under batch and continuous-flow conditions
-
A rapid, chemoselective and metal-free C-B bond-forming reaction of aryl iodides and bromides in aqueous solution at low temperatures was discovered. This reaction is amenable to batch and continuous-flow conditions and shows exceptional functional group tolerance and broad substrate scope regarding both the aryl halide and the borylating reagent. Initial mechanistic experiments indicated a photolytically generated aryl radical as the key intermediate.
- Chen, Kai,Zhang, Shuai,He, Pei,Li, Pengfei
-
p. 3676 - 3680
(2016/06/09)
-
- Sequential one-pot access to molecular diversity through aniline aqueous borylation
-
On the basis of our recently reported aniline aqueous borylation, molecular diversity was achieved in a one-pot process by combining other reactions such as esterification, Suzuki-Miyaura coupling, hydrogenolysis, or Petasis borono-Mannich.
- Erb, William,Albini, Mathieu,Rouden, Jacques,Blanchet, Jrme
-
p. 10568 - 10580
(2015/01/08)
-
- Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors
-
A series of diphenylmethylamine derivatives were rationally designed, synthesized and biologically evaluated. Most of them exhibited moderate to good Akt1 inhibitory activities, as well as promising anti-proliferative efficacy against cancer cell lines. Besides, molecular docking studies were carried out to probe their binding modes with Akt1. Further kinase selectivity studies of compound 22c were performed, indicating its excellent selectivity against Aurora A, Drak, IKKβ, GSK3β, SYK and JAK2, and moderate selectivity against PKC and BRAF. Finally, a refined pharmacophore model was generated using the most active compounds 2, 12c and 22c via application of HipHop program.
- Liu, Tao,Zhan, Wenhu,Wang, Yanming,Zhang, Liangren,Yang, Bo,Dong, Xiaowu,Hu, Yongzhou
-
p. 167 - 176
(2014/01/17)
-
- Synthesis and antimicrobial activity of 2-fluorophenyl-4,6-disubstituted [1,3,5]triazines
-
A series of 2-fluorophenyl-4,6-disubstituted [1,3,5]triazines (1) and (2) were synthesized and evaluated for their antimicrobial activity against three representative gram-positive bacteria and two fungi. The structure-activity relationship (SAR) demonstrates that the 3- or 4-fluorophenyl component attached directly to the triazine ring was essential for activity. Of these compounds, 14, 15, and 25 demonstrated significant activity against all selected organisms compared to control. These compounds were generally nontoxic and may prove useful as antimicrobial agents.
- Saleh, Mona,Abbott, Shaun,Perron, Valerie,Lauzon, Caroline,Penney, Christopher,Zacharie, Boulos
-
scheme or table
p. 945 - 949
(2010/07/06)
-
- Further delineation of hydrophobic binding sites in dopamine D 2/D3 receptors for N-4 substituents on the piperazine ring of the hybrid template 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5, 6,7,8-tetrahydro-naphthalen-2-ol
-
Here we report a structure-activity relationship (SAR) study of analogues of 5/7-{[2-(4-aryl-piperazin-1-yl)-ethyl]-propyl-amino}-5,6,7,8-tetrahydro- naphthalen-2-ol. Our SAR is focused on introduction of various substitutions in the piperazine ring of the hybrid template. The goal behind this study is to delineate the nature of the binding pocket for N-aryl substitution in the piperazine ring by observing the effect of various hydrophobic and other heteroaromatic substitutions on binding affinity (Ki), as measured with tritiated spiperone and HEK-293 cells expressing either D2 or D3 receptors. Functional activity of selected compounds was assessed with the GTPγS binding assay. Compound 8d was the most selective for the D3 receptor in the spiperone binding assay. An interesting similarity in binding affinity was observed between isoquinoline derivative D-301 and the 2-substituted pyridine derivative 8d, suggesting the importance of relative spatial relationships between the N-atom of the ligand and the molecular determinants of the binding pocket in D2/D3 receptors. Functional activity assays demonstrated high potency and selectivity of (+)-8a and (-)-28b (D2/D3 (ratio of EC50): 105 and 202, respectively) for the D3 receptor and both compounds were more selective compared to the reference drug ropinirole (D2/D3 (ratio of EC50): 29.5).
- Ghosh, Balaram,Antonio, Tamara,Gopishetty, Bhaskar,Reith, Maarten,Dutta, Aloke
-
experimental part
p. 5661 - 5674
(2010/10/01)
-
- KETOLIDE DERIVATIVES AS ANTIBACTERIAL AGENTS
-
The present invention provides ketolide derivatives, which can be used as anti-bacterial agents. Compounds disclosed herein can be used for the treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds disclosed herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods of treating bacterial infections.
- -
-
Page/Page column 23
(2009/07/17)
-
- Energy transfer from rhenium(i) complexes to covalently attached anthracenes and phenanthrenes
-
The synthesis and photophysical properties of a series of chromophore-quencher complexes are reported. They are all comprised of a luminescent rhenium(i) tricarbonyl diimine complex that is covalently attached to anthracene or phenanthrene moieties via rigid rod-like p-xylene bridges of variable lengths. Rhenium-to-anthracene energy transfer is strongly exergonic (-ΔG0≈ 0.9 eV) and causes very efficient rhenium MLCT luminescence quenching. By contrast, rhenium-to-phenanthrene energy transfer is only observed when complexes with sufficiently high MLCT energies are used because for these dyads, the driving force for energy transfer is low (-ΔG0≈ 0.1 eV). For a ～15 donor-acceptor distance, the rate constants of the weakly and the strongly exergonic energy transfer processes differ by more than 3 orders of magnitude. The Royal Society of Chemistry 2008.
- Walther, Mathieu E.,Wenger, Oliver S.
-
p. 6311 - 6318
(2009/03/11)
-
- 3-(Dimethylboryl)pyridine: Synthesis, structure, and remarkable steric effects in scrambling reactions
-
(Chemical Equation Presented) A facile method for the synthesis of 3-(dimethylboryl)pyridine (1a) is described. Compound 1a assembles into a rigid cyclic tetramer stabilized via intermolecular boron-nitrogen coordination bonds both in the crystalline state and in solution. The outstanding structural feature of 1a, as compared with previously reported 3-(diethylboryl)pyridine (2a) (which adopts a cone conformation), is that the tetramer of la adopts a 1,2-alternate conformation. To investigate the effect of substituents at the boron atom on the stabilities of the oligomers, scrambling experiments of the component molecules using 1, 2, and 3-(di-n-butylboryl)pyridines 3 were carried out. Although heating at 80-90°C for 20 h was required to attain the equilibrium of the scrambling reactions when the component molecules of the tetramers were 2 or 3, the scrambling in 1 proceeded under relatively mild conditions (60°C, 3 h). This difference in reaction conditions required for 1, as compared to conditions required for 2 or 3, could not be explained solely by the stabilities based on bond lengths or THC.1g It appears that whereas only an SN1-type pathway may be involved in the scrambling of 2 or 3, both SN1- and SN2-type mechanisms operate simultaneously during scrambling reactions of 1 or an intermediate mechanism between SN1 and SN2 operates, which was supported by kinetic studies and calculations using model compounds.
- Wakabayashi, Shigeharu,Imamura, Saori,Sugihara, Yoshikazu,Shimizu, Makoto,Kitagawa, Toshikazu,Ohki, Yasuhiro,Tatsumi, Kazuyuki
-
-
- Antibacterial Agents
-
The present invention provides acylide derivatives, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed to by Gram-positive, Gram-negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds disclosed herein, pharmaceutical compositions thereof, and method of treating bacterial infections.
- -
-
Page/Page column 17
(2009/01/24)
-
- PHOSPHONIUM SALTS DERIVATIVES AND THEIR USE AS SOLUBILITY CONTROLLING AUXILIARIES
-
The present invention relates to the use of compounds of formula (IA) or (IIA): insert formula (IA) and (IIA) from page 15 of the disclosure wherein A represents various substituted or unsubstituted groups such as furyl, phenyl, pyridyl, naphthyl, or thiophenyl; X- represents an anion; and L1 represents a linker, as solubility controlling auxiliaries. These compounds can also be used as solubility controlling fragments of a molecule. The invention also relates to various methods of controlling the solubility of a molecule or a substrate. Moreover, the invention also relates to various phosphonium supported reagents or various phosphonium salts derivatives.
- -
-
Page/Page column 67
(2010/02/14)
-
- SYNTHETIC COMPOUNDS AND DERIVATIVES AS MODULATORS OF SMOKING OR NICOTINE INGESTION AND LUNG CANCER
-
Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.
- -
-
Page/Page column 92
(2010/02/12)
-
- 5-Substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6
-
A series of 5- and 6-substituted and unsubstituted 3-heteroaromatic analogues of nicotine were synthesized in an effort to delineate the structural requirements for selectively inhibiting human cytochrome P-450 (CYP) 2A6, the major nicotine metabolizing enzyme. Thiophene, substituted thiophene, furan, substituted furan, imidazole, substituted imidazole, pyridine, substituted pyridine, thiazole, and quinoline moieties were used to replace the N-methylpyrrolidine ring of nicotine. Bromo and methyl groups were introduced at the 5-position of the pyridine ring and fluoro, chloro, and methoxy groups were placed at the 6-position of the pyridine ring in order to explore the structure-activity relationship (SAR) of inhibition of CYP2A6. The inhibitory activity of the most potent CYP2A6 inhibitors on the functional activity of human cytochrome P450s 3A4, 2E1, 2B6, 2C9, 2C19, and 2D6 was also examined to determine inhibitor selectivity. We identified 36 compounds that were more potent than nicotine at inhibition of coumarin 7-hydroxylase (CYP2A6) activity. We also found a number of compounds to be highly selective for the inhibition of human CYP2A6 versus the other human CYPs examined.
- Denton, Travis T.,Zhang, Xiaodong,Cashman, John R.
-
p. 224 - 239
(2007/10/03)
-
- Generation of 3-Pyridyl Biaryl Systems Via Palladium-Catalyzed Suzuki Cross-Couplings of Aryl Halides with 3-Pyridylboroxin
-
The synthesis of 3-pyridyl biaryl systems can be readily achieved by means of palladium-catalyzed Suzuki cross-coupling reactions between aryl halides and 3-pyridyl-boroxin. A series of cross-couplings were conducted in order to investigate the scope and limitations of this protocol.
- Cioffi, Christopher L.,Spencer, William T.,Richards, Justin J.,Herr, R. Jason
-
p. 2210 - 2212
(2007/10/03)
-
- (2-Amino-phenyl)-amides of ω-substituted alkanoic acids as new histone deacetylase inhibitors
-
A variety of ω-substituted alkanoic acid (2-amino-phenyl)-amides were designed and synthesized. These compounds were shown to inhibit recombinant human histone deacetylases (HDACs) with IC50 values in the low micromolar range and induce hyperacetylation of histones in whole cells. They induced expression of p21WAF1/Cip1 and caused cell-cycle arrest in human cancer cells. Compounds in this class showed efficacy in human tumor xenograft models.
- Vaisburg, Arkadii,Bernstein, Naomy,Frechette, Sylvie,Allan, Martin,Abou-Khalil, Elie,Leit, Silvana,Moradei, Oscar,Bouchain, Giliane,Wang, James,Woo, Soon Hyung,Fournel, Marielle,Yan, Pu T.,Trachy-Bourget, Marie-Claude,Kalita, Ann,Beaulieu, Carole,Li, Zuomei,MacLeod, A. Robert,Besterman, Jeffrey M.,Delorme, Daniel
-
p. 283 - 287
(2007/10/03)
-
- Improved synthesis of azaheteroarylboronic acids using tris-trimethylsilylborate under mild conditions
-
A new family of azaheteroarylboronic acids was synthesized with good yields (70% to 75%). The proposed strategy utilizes an improved transmetalation reaction from Grignard azine reagents and tris-trimethylsilylborate, little used until now.
- Matondo, Hubert,Souirti, Souad,Baboulene, Michel
-
p. 795 - 800
(2007/10/03)
-
- The synthesis of 4′-aryl substituted terpyridines by Suzuki cross-coupling reactions: Substituent effects on ligand fluorescence
-
Several 4′-aryl-substituted 2,2′:6′,2″-terpyridines (tpy-C6H4R) have been prepared by palladium-catalysed cross-coupling of 4′-bromoterpyridine or 4′-triflate-terpyridine (triflate = trifluoromethylsulfonyloxy) with aryl boronic acids or esters, RC6H4B(OR′)2 (R = H, m-NH2, p-CHO, -NO2, -CN, -NMe2, -NPh2). The new ligand 4′-mesityl-terpyridine (mesityl = 2,4,6-trimethylphenyl) was prepared in the same way. Similarly, 4′-bromophenylterpyridine (tpy-φ-Br) has been cross-coupled with aryl halides to generate several new biaryl-substituted terpyridines (tpy-φ-C6H4R where R = H, p-CN, NMe2, NPh2), together with two related compounds with pendent 3- or 4-pyridyl groups (tpy-φ-C6H4-py). For selected compounds, the alternative coupling strategy of reaction of a terpyridine-4-boronate or terpyridine-4-phenylboronate with the appropriate aryl halide has also been investigated (e.g. to prepare tpy-φ-C6H4NO2), but was generally found to be less satisfactory. All of the compounds are fluorescent in the UV region of the spectrum, the biaryl-substituted compounds being only slightly red-shifted compared to the monoaryl systems, but with the further red-shift that accompanies protonation being more significant for the former. Fluorescence lifetimes in solution are in the range 1-5 ns. The emission spectra of the aminobiphenyl-substituted compounds (tpy-φ-C6H4NR″2, where R″ = Me or Ph) display a large red-shift with increasing solvent polarity, suggesting the involvement of an intramolecular charge transfer state, as found previously for the two analogues omitting the phenyl ring (tpy-C6H4NR″2). In contrast to the latter, however, protonation or binding of a Lewis acidic metal ion to the aminobiphenyl compounds serves to quench almost completely their emission.
- Goodall, Wendy,Wild, Kerstin,Arm, Kathryn J.,Williams, J.A. Gareth
-
p. 1669 - 1681
(2007/10/03)
-
- Effective lithiation of 3-bromopyridine: Synthesis of 3-pyridine boronic acid and variously 3-substituted pyridines
-
By using toluene as a solvent, 3-lithiopyridine can be generated cleanly at -50°C. The addition of various electrophiles affords useful building blocks, such as the 3-pyridine boronic acid in 87% isolated yield.
- Cai, Dongwei,Larsen, Robert D,Reider, Paul J
-
p. 4285 - 4287
(2007/10/03)
-
- Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
-
Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases 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.
- -
-
-
- HETERO-BIARYL-PYRIDOQUINAZOLINONE DERIVATIVES AS ANTI-CANCER AGENTS
-
The invention provides a compound having the formula (1), wherein (A) n = 2-4; (B) R1 and R2 are the same or different and selected from the group consisting of H, (C1-C3) alkyl, -CH2CH2OH, -CH2CH2NH2, and -CH2CH2N(CH3)2 or R1 and R2 are alkyl moieties which are taken together to form a 4- to 7-membered ring; (C) R3 is selected from the group consisting of H, -CH3, -CH2CH3, and -CH2CH2NH2; (D) Y is a heterocyclic radical having 5-14 atoms, located at the 2- or 3-position of the pyridoquinazolinone nucleus, in which 1-3 of the heterocyclic ring atoms are independently nitrogen, oxygen, or sulfur; wherein Y may be optionally mono-, di-, or tri-substituted with -OR4, -NR5R6, -CO2H, -CO2R4, or phenyl; R4 is H or (C1-C4) straight-chain alkyl; R5 and R6 are the same or different and are selected from the group consisting of H, (C1-C4) straight-chain alkyl, -CH2CH2OH, -CH2CH2NH2, and -CH2CH2N(CH3)2 or R5 and R6 are alkyl moieties which are taken together to form a 4-7 membered ring; or a pharmaceutically acceptable salt thereof which is useful as an antineoplastic agent.
- -
-
-
- An improved protocol for the preparation of 3-pyridyl- and some arylboronic acids
-
3-Pyridylboronic acid was prepared in high yield and bulk quantity from 3-bromopyridine via a protocol of lithium-halogen exchange and "in situ quench". This technique was further studied and evaluated on other aryl halides in the preparation of arylboronic acids.
- Li, Wenjie,Nelson, Dorian P.,Jensen, Mark S.,Hoerrner, R. Scott,Cai, Dongwei,Larsen, Robert D.,Reider, Paul J.
-
p. 5394 - 5397
(2007/10/03)
-
- Antagonists of gonadotropin releasing hormone
-
There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
- -
-
-
- ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE
-
There are disclosed compounds of formula (I) STR1 and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
- -
-
-
- ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE
-
There are disclosed compounds of formula (I) STR1 and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
- -
-
-
- ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE
-
There are disclosed compounds of formula (I) STR1 and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
- -
-
-
- Hetero-biaryl-pyridoquinazolinone derivatives as anti-cancer agents
-
This invention provides a compound having the formula: STR1 wherein: (A) n=2-4; (B) R1 and R2 are the same or different and selected from the group consisting of H, (C1 -C3) alkyl, --CH2 CH2 OH, --CH2 CH2 NH2, and --CH2 CH2 N(CH3)2 or R1 and R2 are alkyl moieties which are taken together to form a 4- to 7- membered ring; (C) R3 is selected from the group consisting of H, --CH3, --CH2 CH3, and --CH2 CH2 NH2 ; (D) Y is a heterocyclic radical having 5-14 atoms, located at the 2- or 3- position of the pyridoquinazolinone nucleus, in which 1-3 of the heterocyclic ring atoms are independently nitrogen, oxygen, or sulfur; wherein Y may be optionally mono-, di-, or tri- substituted with --OR4, --NR5 R6, --CO2 H, --CO2 R4, or phenyl; R4 is H or (C1 -C 4) straight-chain alkyl; R5 and R6 are the same or different and are selected from the group consisting of H, (C1 -C4) straight-chain alkyl, --CH2 CH2 OH, --CH2 CH2 NH2, and --CH2 CH2 N(CH3)2 or R5 and R6 are alkyl moieties which are taken together to form a 4-7 membered ring; or a pharmaceutically acceptable salt thereof which is useful as an antineoplastic agent.
- -
-
-
- 6-HETEROCYCLIC-4-AMINO-1,2,2A,3,4,5-HEXAHYDROBENZ[CD]INDOLES
-
6-Heterocyclic-4-amino-l,2,2a,3,4,5-hexahydrobenz[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
- -
-
-
- 6-HETEROCYCLIC-4-AMINO-1,3,4,5-TETRAHYDROBENZ[CD]INDOLES
-
6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.
- -
-
-
