cas 19748-66-4, 1-(3-HYDROXYPROPYL)-PYRROLIDINE

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Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2)
Tdp1 and Tdp2 are two tyrosyl-DNA phosphodiesterases that can repair damaged DNA resulting from topoisomerase inhibitors and a variety of other DNA-damaging agents. Both Tdp1 and Tdp2 inhibition could hypothetically potentiate the cytotoxicities of topoisomerase inhibitors. This study reports the successful structure-based design and synthesis of new 7-azaindenoisoquinolines that act as triple inhibitors of Top1, Tdp1, and Tdp2. Enzyme inhibitory data and cytotoxicity data from human cancer cell cultures establish that modification of the lactam side chain of the 7-azaindenoisoquinolines can modulate their inhibitory potencies and selectivities vs Top1, Tdp1, and Tdp2. Molecular modeling of selected target compounds bound to Top1, Tdp1, and Tdp2 was used to design the inhibitors and facilitate the structure-activity relationship analysis. The monitoring of DNA damage by γ-H2AX foci formation in human PBMCs (lymphocytes) and acute lymphoblastic leukemia CCRF-CEM cells documented significantly more DNA damage in the cancer cells vs normal cells.
Wang, Ping,Elsayed, Mohamed S. A.,Plescia, Caroline B.,Ravji, Azhar,Redon, Christophe E.,Kiselev, Evgeny,Marchand, Christophe,Zeleznik, Olga,Agama, Keli,Pommier, Yves,Cushman, Mark
p. 3275 - 3288
(2017)
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Manganese-Catalyzed Anti-Markovnikov Hydroamination of Allyl Alcohols via Hydrogen-Borrowing Catalysis
Controlling the selectivity in a hydroamination reaction is an extremely challenging yet highly desirable task for the diversification of amines. In this article, a selective formal anti-Markovnikov hydroamination of allyl alcohols is presented. It enables the versatile synthesis of valuable γ-amino alcohol building blocks. A phosphine-free Earth's abundant manganese(I) complex catalyzed the reaction under hydrogen-borrowing conditions. A vast range of aliphatic, aromatic amines, drug molecules, and natural product derivatives underwent successful hydroamination with primary and secondary allylic alcohols with excellent functional group tolerance (57 examples). The catalysis could be performed on a gram scale and has been applied for the synthesis of drug molecules. The mechanistic studies revealed the metal-ligand bifunctionality as well as hemilability of the ligand backbone as the key design principle for the success of this catalysis.
Das, Kuhali,Sarkar, Koushik,Maji, Biplab
p. 7060 - 7069
(2021/06/30)

Iron-Catalyzed Anti-Markovnikov Hydroamination and Hydroamidation of Allylic Alcohols
Hydroamination allows for the direct access to synthetically important amines. Controlling the selectivity of the reaction with efficient, widely applicable, and economic catalysts remains challenging, however. This paper reports an iron-catalyzed formal anti-Markovnikov hydroamination and hydroamidation of allylic alcohols, which yields γ-amino and γ-amido alcohols, respectively. Homoallylic alcohol is also feasible. The catalytic system, consisting of a pincer Fe-PNP complex (1-4 mol %), a weak base, and a nonpolar solvent, features exclusive anti-Markovnikov selectivity, broad substrate scope (>70 examples), and good functional group tolerance. The reaction could be performed at gram scale and applied to the synthesis of drug molecules and heterocyclic compounds. When chiral substrates are used, the stereochemistry and enantiomeric excess are retained. Further application of the chemistry is seen in the functionalization of amino acids, natural products, and existing drugs. Mechanistic studies suggest that the reaction proceeds via two cooperating catalytic cycles, with the iron complex catalyzing a dehydrogenation/hydrogenation process while the amine substrate acts as an organocatalyst for the Michael addition step.
Ma, Wei,Zhang, Xiaohui,Fan, Juan,Liu, Yuxuan,Tang, Weijun,Xue, Dong,Li, Chaoqun,Xiao, Jianliang,Wang, Chao
supporting information
p. 13506 - 13515
(2019/09/09)

AZAINDENOISOQUINOLINE COMPOUNDS AND USES THEREOF
Tyrosyl-DNA Phosphodiesterases 1 and 2 (Tdp1 and Tdp2) can repair damaged DNA resulting from topoisomerase inhibitors and a variety of other DNA-damaging agents. Both Tdp1 and Tdp2 inhibition could hypothetically potentiate the cytotoxicities of topoisomerase inhibitors. Series of 7-azaindenoisoquinolines that act as triple inhibitors of Top1, Tdp1 and Tdp2 are disclosed. Also described are methods for treating patients of a cancer using the disclosed azaindenoisoquinoline compounds or a pharmaceutical formulation thereof.
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Paragraph 0072

(2018/07/29)

NAPHTHYLUREA DERIVATIVES AND MEDICAL APPLICATIONS THEREOF
The present invention relates to naphthylurea derivatives. Such substances can significantly inhibit VEGFR2 and PDGFR-β receptor tyrosine kinase phosphorylation at nanomolar concentration levels. It is a novel type of tyrosine kinase inhibitors which can be used in the treatment of tyrosine kinase-mediated diseases or symptoms such as malignancies and ocular diseases accompanied with pathologic neovascularization
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Paragraph 0047; 0050-0051

(2016/08/17)

FUSED 1,4-DIHYDRODIOXIN DERIVATIVES AS INHIBITORS OF HEAT SHOCK TRANSCRIPTION FACTOR 1
The present invention relates to compounds of formula I wherein A1, A2 R4 and Q are as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.
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Paragraph 0068

(2015/04/22)

Platinum-Catalyzed, Terminal-Selective C(sp3)-H Oxidation of Aliphatic Amines
This Communication describes the terminal-selective, Pt-catalyzed C(sp3)-H oxidation of aliphatic amines without the requirement for directing groups. CuCl2 is employed as a stoichiometric oxidant, and the reactions proceed in high yield at Pt loadings as low as 1 mol%. These transformations are conducted in the presence of sulfuric acid, which reacts with the amine substrates in situ to form ammonium salts. We propose that protonation of the amine serves at least three important roles: (i) it renders the substrates soluble in the aqueous reaction medium; (ii) it limits binding of the amine nitrogen to Pt or Cu; and (iii) it electronically deactivates the C-H bonds proximal to the nitrogen center. We demonstrate that this strategy is effective for the terminal-selective C(sp3)-H oxidation of a variety of primary, secondary, and tertiary amines.
Lee, Melissa,Sanford, Melanie S.
supporting information
p. 12796 - 12799
(2015/10/28)

Visible light photooxidative cyclization of amino alcohols to 1,3-oxazines
1,3-Amino alcohols were prepared to examine how structure affects the oxidation of tertiary amines in visible light photocatalysis. These substrates were cyclized to produce oxazines following the photooxidative formation of iminium ions using catalytic Ru(bpy)3Cl2. Amino alcohol derivatives of tetrahydroisoquinoline, tetrahydroquinoline, pyrrolidine, and Δ3-piperidine all were found to be viable substrates. In the case of the unsaturated piperidines, cyclization is accompanied by addition of methanol across the alkene; most likely occurring via a conjugate addition to an intermediate α,β-unsaturated iminium ion prior to oxazine formation.
Mathis, Cheryl L.,Gist, Brandi M.,Frederickson, Conerd K.,Midkiff, Katie M.,Marvin, Christopher C.
p. 2101 - 2104
(2013/04/24)

Catalytic hydrogenation of amides to amines under mild conditions
Under (not so much) pressure: A general method for the hydrogenation of tertiary and secondary amides to amines with excellent selectivity using a bimetallic Pd-Re catalyst has been developed. The reaction proceeds under low pressure and comparatively low temperature. This method provides organic chemists with a simple and reliable tool for the synthesis of amines. Copyright
Stein, Mario,Breit, Bernhard
supporting information
p. 2231 - 2234
(2013/03/28)

Novel antagonists of serotonin-4 receptors: Synthesis and biological evaluation of pyrrolothienopyrazines
Based on the definition of a 5-HT4 receptor antagonist pharmacophore, a series of pyrrolo[1,2-a]thieno[3,2-e] and pyrrolo[1,2-a]thieno[2,3-e] pyrazine derivatives were designed, prepared, and evaluated to determine the properties necessary for high-affinity binding to 5-HT4 receptors. The compounds were synthesized by substituting the chlorine atom of the pyrazine ring with various N-alkyl-4-piperidinylmethanolates. They were evaluated in binding assays with [3H]GR113808 (1) as the 5-HT4 receptor radioligand. The affinity values (Ki or inhibition percentages) were affected by both the substituent on the aromatic ring and the substituent on the lateral piperidine chain. A methyl group on the tricyclic ring produced a marked increase in affinity while an N-propyl or N-butyl group gave compounds with nanomolar affinities. Among the most potent ligands, 34d was selected for further pharmacological studies and evaluated in vivo. This compound acts as an antagonist/weak partial agonist in COS-7 cells stably expressing the 5-HT4(a) receptor and is of great interest as a peripheral antinociceptive agent.
Lemaitre, Stephane,Lepailleur, Alban,Bureau, Ronan,Butt-Gueulle, Sabrina,Lelong-Boulouard, Veronique,Duchatelle, Pascal,Boulouard, Michel,Dumuis, Aline,Daveu, Cyril,Lezoualc'h, Frank,Pfeiffer, Bruno,Dauphin, Francois,Rault, Sylvain
scheme or table
p. 2607 - 2622
(2009/09/06)

TETRAHYDRONAPHTHYRIDINES AND AZA DERIVATIVES THEREOF AS HISTAMINE H3 RECEPTOR ANTAGONISTS
The invention relates to compounds of formula (I), wherein X1a, X1 to X5, Ra, Rb, n and R have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
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Page/Page column 72-73

(2009/10/30)

Substituted 2-arylbenzothiazoles as kinase inhibitors: Hit-to-lead optimization
Based on an (aminoaryl)benzothiazole quinazoline hit structure for kinase inhibition, a systematic optimization program resulted in a lead structure allowing for inhibitory activities in cellular phosphorylation assays in the low nanomolar range.
Tasler, Stefan,Mueller, Oliver,Wieber, Tanja,Herz, Thomas,Pegoraro, Stefano,Saeb, Wael,Lang, Martin,Krauss, Rolf,Totzke, Frank,Zirrgiebel, Ute,Ehlert, Jan E.,Kubbutat, Michael H.G.,Schaechtele, Christoph
supporting information; experimental part
p. 6728 - 6737
(2009/12/09)

Fluorinated non-imidazole histamine H3 receptor antagonists
Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in vivo screenings. The compounds vary in the basic centres (piperidine or pyrrolidine) and are fluoro substituted in different positions of the basic alicyclic moiety. Pharmacological evaluation resulted in ligands with high affinities at hH3 receptor in the nanomolar and subnanomolar concentration range and some with high antagonist in vivo potencies.
Isensee,Amon,Galaparti,Ligneau,Camelin,Capet,Schwartz,Stark
body text
p. 2172 - 2175
(2009/12/03)

SUBSTITUTED SULFONAMIDE COMPOUNDS
Substituted sulfonamide compounds corresponding to formula I processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor
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Page/Page column 62

(2009/10/30)

Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists
A new series of quinazolinone derivatives was synthesized and evaluated as nonimidazole H3 receptor inverse agonists. 2-Methyl-3-(4-{[3-(1- pyrrolidinyl)propyl]oxy}phenyl)-5-(trifluoromethyl)-4(3H)-quinazolinone (1) was identified as a promising derivative for further evaluation following optimization of key parameters. Compound 1 has potent H3 inverse agonist activity and excellent selectivity over other histamine receptor subtypes and a panel of 115 unrelated diverse binding sites. Compound 1 also shows satisfactory pharmacokinetic profiles and brain penetrability in laboratory animals. Two hours after oral administration of 30 mg/kg of 1 to SD rats, significant elevation of brain histamine levels was observed where the brain H3 receptor was highly occupied (>90%). On the basis of species differences in P-glycoprotein (P-gp) susceptibility of 1 between human and rodent P-gps, the observed rodent brain permeability of 1 is significantly limited by P-gp mediated efflux in rodents, whereas the extent of P-gp mediated efflux in humans should be very small or negligible. The potential of 1 to be an efficacious drug was demonstrated by its excellent brain penetrability and receptor occupancy in P-gp-deficient CF-1 mice.
Nagase, Tsuyoshi,Mizutani, Takashi,Ishikawa, Shiho,Sekino, Etsuko,Sasaki, Takahide,Fujimura, Takashi,Ito, Sayaka,Mitobe, Yuko,Miyamoto, Yasuhisa,Yoshimoto, Ryo,Tanaka, Takeshi,Ishihara, Akane,Takenaga, Norihiro,Tokita, Shigeru,Fukami, Takehiro,Sato, Nagaaki
experimental part
p. 4780 - 4789
(2009/07/25)

Synthesis and preliminary evaluation of novel analogues of quindolines as potential stabilisers of telomeric G-quadruplex DNA
Telomeric DNA is a potential selective target for cancer therapy since the tumour-associated enzyme telomerase regulates telomere maintenance in most cancer cells. The 3′ single-stranded ends of telomeric DNA can be folded into quadruplex structures by appropriate small molecules. We describe the preparation of a new class of 2,7-disubstituted 10H-indolo[3,2-b]quinolines with enhanced selectivity for the stabilisation of quadruplex DNA compared to duplex DNA, and also the preparation of a key intermediate for the synthesis of trisubstituted quindolines.
Le Sann, Christine,Huddleston, Jonathan,Mann, John
p. 12903 - 12911
(2008/03/27)

CRYSTAL OF 4(3H)-QUINAZOLINONE DERIVATIVE
A substance that has a potency antagonistic to coupling of histamine with histamine H3 receptor or a potency of inhibiting the constant activity of histamine H3 receptor. There is provided a form I crystal of 2-methy 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that in the powder X- ray diffractometry, has peaks at 6.4°, 9.7°, 10.2°, 12.9°, 14.2°, 14.7°, 16.0°, 16.3°, 16.8°, 17.6°, 19.5°, 20.3°, 20.6°, 21.2°, 21.8°, 22.1°, 22.4°, 22.6°, 24.0°, 24.3°, 24.9°, 25.7°, 25.9°, 26.5°, 26.7°, 27.4°, 29.1°, 29.4°, 32.3° and 39.0° diffraction angles(2θ ± 0.2°).
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Page/Page column 6; 14

(2010/11/28)

Phenylpiperidine derivatives as melanocortin-4 receptor modulators
The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
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Page/Page column 39

(2008/06/13)

2-arylbenzothiazole analogues and uses thereof
The present invention relates to compounds of the general formula (I) and salts, prodrugs, and stereoisomers thereof, wherein Y independently represents S, O, NR2, SO, SO2; A independently represents a fife- or six-membered aromatic carbocycle or heterocycle and wherein R1 to R20 in formula (I) represent independently of each other a variety of different substituents comprising alkyl, aryl, aralkyl, alkylaryl, heteroaryl groups and monofunctional moieties.
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Page/Page column 14

(2008/06/13)

2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
The present invention relates to anticancer compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y independently represents S, O, NR 2 , SO, SO 2 ; A independently represents a five- or six-membered aromatic carbocycle or heterocycle and wherein R 1 in formula (I) represents one of the heteroaryl groups defined in the claims.
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Page/Page column 25

(2010/11/25)

PYRROLO[2,1-F] [1,2,4] TRIAZIN-4-YLAMINES IGF-1R KINASE INHIBITORS FOR THE TREATMENT OF CANCER AND OTHER HYPERPROLIFERATIVE DISEASES
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Page/Page column 107-108

(2010/11/27)

Electrooxidative cyclization of hydroquinolyl alcohols, hydroquinolylamines, and dimethyl aminomalonates
Several hydroquinolyl alcohols and amines were electrochemically oxidized in methanol in the presence of sodium methoxide and potassium iodide to afford the corresponding intramolecular cyclization products. Furthermore, several amino malonates were electrochemically oxidized to yield the corresponding heterocyclic compounds through an intramolecular carbon-carbon bond formation in the presence of sodium cyanide in methanol. CSIRO 2007.
Okimoto, Mitsuhiro,Yoshida, Takashi,Hoshi, Masayuki,Hattori, Kazuyuki,Komata, Masashi,Numata, Kaori,Tomozawa, Kenta
p. 236 - 242
(2008/02/11)

METHOD FOR PRODUCING 4(3H)-QUINAZOLINONE DERIVATIVE
Disclosed is a method for producing 2-methyl-3-{4- [3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone comprising a step for reacting 2-methyl-5-trifluoromethyl-4H-3,1-benzoxazine-4-one with 4-[3-(1-pirrolidinyl)propoxy]aniline or an acid addition salt thereof, or 4-(1-cyclobutyl-4-piperidinyl)oxyaniline or an acid addition salt thereof in the presence of an acetic acid catalyst.
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Page/Page column 9-10

(2008/06/13)

New mustard-linked 2-aryl-bis-benzimidazoles with anti-proliferative activity
We describe new methodology for the synthesis of symmetric bis-benzimidazoles carrying 2-aryl moieties, including 2-[4-(3′- aminopropoxy)phenyl] and 2-[4-(3′-aminopropanamido)phenyl] substituents, together with the synthesis of novel hybrid molecules comprising bis-benzimidazoles in ester and amide combination with the N-mustard chlorambucil. The in vitro activities of these compounds against five cancer cell lines are also provided. The Royal Society of Chemistry 2006.
Le Sann, Christine,Baron, Anne,Mann, John,Van Den Berg, Hendrik,Gunaratnam, Mekala,Neidle, Stephen
p. 1305 - 1312
(2007/10/03)

Phenoxypropylpiperidines and -pyrrolidines and their use as histamine H3-receptor ligands
The present patent application concerns compounds of formula (I), with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
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Page/Page column 36

(2008/06/13)

Estrogen receptor ligands. Part 9: Dihydrobenzoxathiin SERAMs with alkyl substituted pyrrolidine side chains and linkers
A series of benzoxathiin SERAMs was prepared. Minor modifications in the side chain or linker resulted in significant effects on biological activity, especially in uterine tissue. A series of dihydrobenzoxathiin SERAMs with alkylated pyrrolidine side chains or alkylated linkers was prepared. Minor modifications in the side chain or linker resulted in significant effects on biological activity, especially in uterine tissue.
Blizzard, Timothy A.,Dininno, Frank,Morgan II, Jerry D.,Chen, Helen Y.,Wu, Jane Y.,Kim, Seongkon,Chan, Wanda,Birzin, Elizabeth T.,Yang, Yi Tien,Pai, Lee-Yuh,Fitzgerald, Paula M.D.,Sharma, Nandini,Li, Ying,Zhang, Zhoupeng,Hayes, Edward C.,Dasilva, Carolyn A.,Tang, Wei,Rohrer, Susan P.,Schaeffer, James M.,Hammond, Milton L.
p. 107 - 113
(2007/10/03)

Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands
The invention relates to tetrahydronaphthyridine derivatives having formula (I) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said tetrahydronaphthyridine derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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Page/Page column 50

(2008/06/13)

6-[(SUBSTITUTED)PHENYL]TRIAZOLOPYRIMIDINES AS ANTICANCER AGENTS
This invention relates to certain 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable salts thereof, and compositions containing said compounds or pharmaceutically acceptable salts thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or pharmaceutically acceptable salts thereof. The present invention relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal in need thereof by promotion of microtubule polymerization which comprises administering to said mammal an effective amount of said compounds and pharmaceutically acceptable salts thereof.
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Page/Page column 70

(2008/06/13)

QUINAZOLINE DERIVATIVES AS ANGIOGENESIS INHIBITORS
The invention relates to the use of compounds of the formula I: wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1-3 heteroatoms selected independently from O, N and S; Z is -O-, -NH-, -S-, -CH2- or a direct bond; n is 0-5; m is 0-3; R represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylsulphanyl, -NRR (wherein R and R, which may be the same or different, each represents hydrogen or C1-3alkyl), or RX- (wherein X and R are as defined herein; R represents hydrogen, oxo, halogeno, hydroxy, C1-4alkoxy, C1-4alkyl, C1-4alkoxymethyl, C1-4alkanoyl, C1-4haloalkyl, cyano, amino, C2-5alkenyl, C2-5alkynyl, C1-3alkanoyloxy, nitro, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylsulphanyl, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N-C1-4alkylcarbamoyl, N,N-di(C1-4alkyl)carbamoyl, aminosulphonyl, N-C1-4alkylaminosulphonyl, N,N-di(C1-4alkyl)aminosulphonyl, N-(C1-4alkylsulphonyl)amino, N-(C1-4alkylsulphonyl)-N-(C1-4alkyl)amino, N,N-di(C1-4alkylsulphonyl)amino, a C3-7alkylene chain joined to two ring C carbon atoms, C1-4alkanoylaminoC1-4alkyl, carboxy or a group RX (wherein X and R are as defined herein); and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
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Page/Page column 129

(2008/06/13)

Quinazoline derivatives
The invention concerns quinazoline derivatives of Formula (I) wherein Q1includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1includes a direct bond and O and Q3includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2and R3is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.
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Page/Page column 70

(2010/02/08)

Quinoline derivatives having vegf inhibiting activity
The invention relates to compounds of formula (I) wherein: either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH—, or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, —NH—, —S—, —CH2— or a direct bond; Z is linked to any one of G1, G2, G3 and G4; n is an integer from 0 to 5; m is an integer from 0 to 3; Ra represents hydrogen or fluoro; Rb, R1 and R2 are defined herein and salt thereof, process for the preparation so such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of a medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blodded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of diseases states including cancer and rheumatoid arthritis.
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(2008/06/13)

Cinnoline compounds
The invention relatest to compounds of the formula (I) wherein either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH—, or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, —NH—, —S—, —CH2— or a direct bond; Z is linked to any one of G1, G2, G3 and G4 which is a free carbon atom; n is an integer from 0 to 5; any of the substitutents R1 may be attached at any free carbon atom of the indole, azaindole or indazole group; m is an integer from 0 to 3; Ra represents hydrogen; Rb represents hydrogen or another value as defined herein; R1 represents hydrogen, oxo, hydroxy, halogeno, C1-4alkyl, C1-4alkoxy, C1-4alkoxy, C1-4-alkyl, aminoC1-4alkyl, C1-3alkylaminoC1-4alkyl, di(C1-3alkyl)aminoC1-4alkyl, —C1-5alkyl(ring B) wherein ring B is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, N-methylpiperazinly, N-ethylpiperazinyl, morpholino and thiomorpholino; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3aklylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1— (wherein R5 and X1 are as defined herein) and salts thereof, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
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(2008/06/13)

Therapy
The invention concerns the use of a quinazoline derivative of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2 and R3 is hydrogen or (1-6C)alkyl; Z includes O, S and NH; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human.
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Page 41

(2008/06/13)

A hydroformylation route to diazabicycloalkanes and oxazabicycloalkanes containing medium and large rings
Diazabicycloalkanes and oxazabicycloalkanes containing medium and large rings can be prepared by rhodium-catalysed reactions of N-alkenylpropane-1,3-diamines and 2-(alkenylamino)ethanols with H2/CO in excellent yields without the need for high dilution. Selective ring opening of these compounds can lead to large heterocycles. CSIRO 1999.
Bergmann, David J.
p. 1131 - 1138
(2007/10/03)

Intramolecular Quenching of Iminium Ions Generated by Photooxidation of Aminoalcohols with Ketones. A New Synthesis of Oxazines and Oxazoles
The irradiation of tertiary amines in the presence of ketones leads to a regioselective and stereoselective formation of iminium salts which then react to afford the corresponding oxazines or oxazoles. - Key words : Ammoniumyl ions, iminium ions, electron transfer, amines, ketones, tetrahydrooxazine tetrahydrooxazoles.
Cossy, Janine,Guha, Madhumita
p. 1715 - 1718
(2007/10/02)

Omega-quaternary ammonium alkyl esters and thioesters of acidic nonsteroidal antiinflammatory drugs
Quaternary ammonium alkyl esters and thioesters of acidic nonsteroidal anti-inflammatory drugs (NSAIDs) are disclosed. These esters and thioesters display the anti--inflammatory profile of the parent NSAIDs with greatly reduced gastrointestinal irritancy, providing a more favorable separation of therapeutic activity and toxicological side effects than the parent NSAIDs.
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(2008/06/13)

N-Alkylation d'amines en catalyse homogene. Synthese de mono- et de diamines cycliques
Ruthenium compounds are appropriate catalysts in the N-alkylation of amines.The synthesis of N-alkylated cyclic amines from a cyclic amine and an alcohol or via the condensation between a diol and a primary amine are described.The reaction with cyclic amines is highly selective, especially in the presence of a phosphine, making it a high yielding preparative procedure.The catalytic condensation between cyclic amines and diols yields either an aminoalcohol (A) or a bicyclic diamine (B).The temperature, the presence of phosphine, and the ratio of amine to diol are decisive in directing the reaction toward A or B.The proposed mechanism involves the dehydrogenation of the alcohol followed by attack of the amine on the aldehyde intermediate.
Bitsi, G.,Schleiffer, E.,Antoni, F.,Jenner, G.
p. 343 - 352
(2007/10/02)

A biomimetic approach to the Elaeocarpus alkaloids. Syntheses of (±)-Elaeokanine A, (±)-Elaeokanine C, (±)-Elaeocarpidine, and (±)-Tarennine
-
Gribble,Switzer,Soll
p. 3164 - 3170
(2007/10/02)

HYDROBORATION OF N-ALLYL DERIVATIVES OF PYRROLIDINE, PIPERIDINE, HEXAHYDROAZEPINE AND MORPHOLINE
Heating of allyl derivatives I with triethylamine-borane gave spirocyclical amine-boranes II, which were hydrolysed with hydrochloric acid to hydrochlorides of aminoboronic acids, III.Oxidation of these hydrochlorides produced aminoalcohols IV.
Ferles, Miloslav,Kafka, Stanislav
p. 2150 - 2156
(2007/10/02)

Chemical Properties

Boiling Point: 216.9 °C at 760 mmHg
Flash Point:97.7 °C
Density: 0.983 g/cm³
Storage Temp.:2-8°C
Vapor Pressure: 0.0293mmHg at 25°C
Refractive Index: 1.482
PKA: 15.02±0.10(Predicted)
PSA: 23.47000
LogP: 0.40250

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Chemical Properties

Boiling Point: 216.9 °C at 760 mmHg

Flash Point:97.7 °C

Density: 0.983 g/cm³

Storage Temp.:2-8°C

Vapor Pressure: 0.0293mmHg at 25°C

Refractive Index: 1.482

PKA: 15.02±0.10(Predicted)

PSA: 23.47000

LogP: 0.40250

Global suppliers and manufacturers of 19748-66-4total 66 suppliers on LookChem

Article Database

19748-66-4

Articles about 19748-66-4Total 39 be found

More Articles about upstream products of 19748-66-4

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Chemical Properties

Boiling Point: 216.9 °C at 760 mmHg

Flash Point:97.7 °C

Density: 0.983 g/cm3

Storage Temp.:2-8°C

Vapor Pressure: 0.0293mmHg at 25°C

Refractive Index: 1.482

PKA: 15.02±0.10(Predicted)

PSA: 23.47000

LogP: 0.40250

Global suppliers and manufacturers of 19748-66-4total 66 suppliers on LookChem

Density: 0.983 g/cm³