- Synthesis and antiviral activity of some 1H-pyrrolo[3,2-b]pyridin-6-yl)acetic acid derivatives
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Pyrrolopyridine derivatives for the treatment of HIV1-infection were synthesized by 10 step reactions. Methyl 2-(3-bromo-7-(4-chlorophenyl)-1,5-dimethyl-1H-pyrrolo[3,2-b]pyridin-6-yl)-2-(tert-butoxy)acetate converted efficiently into the corresponding 1Hpyrrolo[3,2-b]pyridin-6-yl)acetic acid derivatives by Suzuki coupling reaction. Present procedure provides short reaction times and good to excellent yields for a wide range of compounds, including pyrrolopyridine scaffolds. 7-Halogenated 1H-pyrrolo[3,2,b]pyridine acetic acid derivatives of final products showed good activity inthe HIV-1 IN inhibition test, while the other derivatives showed relatively low activity.
- Yoon, Hyun-Ah,Nam, Hwa-Jung,Kim, Uk-Il,Kim, Kyungjin,Kim, Bong Jin
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Read Online
- Novel Substituted Purine Isosteres: Synthesis, Structure-Activity Relationships and Cytotoxic Activity Evaluation
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A number of pyrrolo[2,3-c]pyridines, pyrrolo[3,2-d]pyrimidines and pyrazolo[4,3-d]pyrimidines were designed and synthesized as antiproliferative agents. The target compounds possessed selected substituents in analogous positions on the central scaffold th
- Dimitrakis, Spyridon,Gavriil, Efthymios-Spyridon,Gioti, Katerina,Lougiakis, Nikolaos,Marakos, Panagiotis,Pouli, Nicole,Pousias, Athanasios,Tenta, Roxane
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- HETEROAROMATIC NMDA RECEPTOR MODULATORS AND USES THEREOF
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Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated modulate the NMDA receptor.
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Paragraph 00283
(2017/07/27)
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- SAR156497, an exquisitely selective inhibitor of Aurora kinases
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The Aurora family of serine/threonine kinases is essential for mitosis. Their crucial role in cell cycle regulation and aberrant expression in a broad range of malignancies have been demonstrated and have prompted intensive search for small molecule Auror
- Carry, Jean-Christophe,Clerc, Fran?ois,Minoux, Hervé,Schio, Laurent,Mauger, Jacques,Nair, Anil,Parmantier, Eric,Le Moigne, Ronan,Delorme, Cécile,Nicolas, Jean-Paul,Krick, Alain,Abécassis, Pierre-Yves,Crocq-Stuerga, Véronique,Pouzieux, Stéphanie,Delarbre, Laure,Maignan, Sébastien,Bertrand, Thomas,Bjergarde, Kirsten,Ma, Nina,Lachaud, Sylvette,Guizani, Houlfa,Lebel, Rémi,Doerflinger, Gilles,Monget, Sylvie,Perron, Sébastien,Gasse, Francis,Angouillant-Boniface, Odile,Filoche-Rommé, Bruno,Murer, Michel,Gontier, Sylvie,Prévost, Céline,Monteiro, Marie-Line,Combeau, Cécile
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p. 362 - 375
(2015/03/04)
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- Synthesis and reactivity of pyrrolo[3,2-d][1,3]oxazine-2,4-dione. Access to new pyrrolo[3,2-e][1,4]diazepine-2,5-diones
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A convenient synthesis of pyrrolo[3,2-d][1,3]oxazine-2,4-dione 4 is described and its reactivity towards various nucleophiles studied. The regioselective ring opening of anhydride 4 or its N-alkylated analog 25 in the presence of alanine or proline afforded, respectively, imidazolidinedione 22 and N-protected pyrrolo[3,2-e][1,4]diazepines 30 and 31 in a one-pot process. In a last part of this study, an alternative route to produce a library of eight non protected pyrrolo[3,2-e][1,4]diazepine-2,5-diones 35a-h is described to overcome the limited reactivity of anhydride 4.
- Malcor, Jean-Daniel,Brouillette, Yann,Graffion, Julien,Spielmann, Kim,Masurier, Nicolas,Maillard, Ludovic T.,Martinez, Jean,Lisowski, Vincent
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p. 4631 - 4639
(2014/06/23)
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- HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 128-129
(2012/08/27)
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- ANTI-CANCER COMPOUND AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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The invention relates to a compound of formula (I), more specifically in the levorotatory form (1a) thereof, in particular the form having a rotatory power [α]D=?38.6+0.7 at a concentration of 0.698 mg/ml in methanol. The compound may be in the form of a
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Page/Page column 10
(2012/09/10)
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- COMPOUND ETHYL 8-OXO-9-[3-(1H-BENZIMIDAZOL-2-YLOXY)PHENYL]-4,5,6,7,8,9-HEXAHYDRO-2H-PYRROLO[3,4-B]QUINOLINE-3-CARBOXYLATE, SALT, CRYSTALLINE FORM, COCRYSTAL, FORMULATION, PROCESSES FOR PREPARATION, APPLICATION AS MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS A
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The invention relates more particularly to a new salt, cocrystal and formulations of ethyl 8-oxo-9-[3-(1H-benzimidazol-2-yloxy)phenyl]-4,5,6,7,8,9-hexahydro-2H- pyrrolo[3,4-b]quinoline-3-carboxylate of formula (F) to preparations thereof and to the use th
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Page/Page column 13
(2012/06/01)
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- Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2] thiazolo[5,4- d ]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent
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Structure-activity relationship analysis identified (+)-N-(3-aminopropyl)- N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl) -2-methylpropyl]-4-methylbenzamide (AZD4877), from a series of novel kinesin spindle protein (KSP) inhibitors, as exhibiting both excellent biochemical potency and pharmaceutical properties suitable for clinical development. The selected compound arrested cells in mitosis leading to the formation of the monopolar spindle phenotype characteristic of KSP inhibition and induction of cellular death. A favorable pharmacokinetic profile and notable in vivo efficacy supported the selection of this compound as a clinical candidate for the treatment of cancer.
- Theoclitou, Maria-Elena,Aquila, Brian,Block, Michael H.,Brassil, Patrick J.,Castriotta, Lillian,Code, Erin,Collins, Michael P.,Davies, Audrey M.,Deegan, Tracy,Ezhuthachan, Jayachandran,Filla, Sandra,Freed, Ellen,Hu, Haiqing,Huszar, Dennis,Jayaraman, Muthusamy,Lawson, Deborah,Lewis, Paula M,Nadella, Murali V. P.,Oza, Vibha,Padmanilayam, Maniyan,Pontz, Timothy,Ronco, Lucienne,Russell, Daniel,Whitston, David,Zheng, Xiaolan
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supporting information; experimental part
p. 6734 - 6750
(2011/12/04)
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- Design, synthesis, and in vitro antitumor activity evaluation of novel 4-pyrrylamino quinazoline derivatives
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Here, we describe the design and synthesis of two series of 4-pyrrylamino quinazolines as new analogs of the epidermal growth factor receptor inhibitor gefitinib. In vitro antitumor activity of these novel compounds against pancreatic (Miapaca2) and prostate (DU145) cancer cell lines was evaluated. Compared with the parental gefitinib, all 18 derivatives show a greatly increased cytotoxicity to cancer cells. In vitro kinase inhibitory activity on epidermal growth factor receptor was also investigated. Among them, compounds GI-6, GII-4, GII-6, GII-8, and GII-9 are more potential receptor tyrosine kinase (RTK) inhibitors. Based on these results, we propose simple structure-activity relationship to provide information for designing and developing more potent antitumor agents.
- Wu, Xiaoqing,Li, Mingdong,Tang, Wenhua,Zheng, Youguang,Lian, Jiqin,Xu, Liang,Ji, Min
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experimental part
p. 932 - 940
(2012/03/11)
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- AROMATIC COMPOUND
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An aromatic compound represented by the following formula or a pharmaceutically acceptable salt thereof: , wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., G1, G2, G3, G4 and G5 are CH or N, X is -NH-, -O-, -CH2-, etc., Y is - CH2-,-CO-,-SO2- etc., Z is a single bond, -CO-, -SO2-, -NH-, -O-, -S-, -CONH-,-SO2NH-, etc., R2 is hydrogen, alkyl, alkoxy, halogen, etc., and R3 is carbocyclic group, heterocyclic group, alkyl, etc., is useful as a controlling agent of the function of CCR4 useful for the treatment or therapy for bronchial asthma, atopic dermatitis, etc.
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Page/Page column 37
(2008/12/07)
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- ALICYCLIC HETEROCYCLIC COMPOUND
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An alicyclic heterocyclic compound represented by the following formula or a pharmaceutically acceptable salt thereof: wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., P1 and P2 are CH or N, q and r are 0 to 2, X is -NH-, -O-, -CH2-, etc., Y is -CH2-, -CO-, -SO2-, etc., Z is -CO-, -SO2-, etc., and R3 is carbocyclic group, heterocyclic group, hydroxyl, alkoxy or amino, is useful as a controlling agent of the function of CCR4 useful for the prevention or treatment for bronchial asthma, atopic dermatitis, etc.
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Page/Page column 93
(2008/12/08)
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- HETEROBICYCLIC MATRIX METALLOPROTEASE INHIBITORS
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The present invention relates generally to amide containing heterobicyclic containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors.
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Page/Page column 66-67
(2008/12/05)
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- Process for preparing 2-pyrrolidinyl-1H-pyrrolo[3,2-d]pyrimidine inhibitors of nucleoside metabolism
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A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alkyl, aralkyl or aryl group; and Z is selected from OH, hydrogen, halogen, hydroxy, SQ or OQ, Q is an optionally substituted all, aralkyl or aryl group; or a tautomer thereof; or a pharmaceutically acceptable salt thereof; or an ester thereof; or a prodrug thereof, which comprises reacting a compound of the formula (II) ?with an anion produced by abstraction of the bromine or iodine atom from a compound of formula (XIX), ?to form a compound of formula (XX) The compound of formula (XX) is N- and O-deprotected to obtain the compound of formula (I).
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Page column 13-17
(2008/06/13)
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