301226-83-5Relevant articles and documents
HETEROCYCLIC COMPOUND, APPLICATION THEREOF, AND COMPOSITION CONTAINING SAME
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, (2022/03/07)
A heterocyclic compound represented by formula XI, a pharmaceutically acceptable salt, a solvate, or a solvate of a pharmaceutically acceptable salt thereof, use thereof, and a composition containing the same. The compound is novel in structure and has good STAT5 inhibitory activity.
Copper-catalysed amination of alkyl iodides enabled by halogen-atom transfer
Barthelemy, Anne-Laure,Douglas, James J.,Górski, Bartosz,Juliá, Fabio,Leonori, Daniele
, p. 623 - 630 (2021/07/25)
Despite the fact that nucleophilic displacement (SN2) of alkyl halides with nitrogen nucleophiles is one of the first reactions introduced in organic chemistry teaching, its practical utilization is largely limited to unhindered (primary) or ac
HYDROXYQUINOXALINECARBOXAMIDE DERIVATIVE
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Page/Page column 53, (2010/12/29)
The present invention provides a novel hydroxyquinoxaline carboxamide derivative that is useful for preventing and/or treating blood coagulation disorders. A compound represented by formula (i), or a pharmacologically acceptable salt thereof: wherein, each of R1 and R2 independently represents a group such as a hydrogen atom or a halogen atom; R3 represents a group such as a hydrogen atom; each of R4 and R5 independently represents a group such as a hydrogen atom, a halogen atom or a C1-4 alkyl group; each of R6 and R7 independently represents a hydrogen atom or a C1-4 alkyl group; X represents a group such as a C3-10 cycloalkyl group, C6-10 aryl group or a 5- to 10-membered heterocyclic group, which may be substituted with substituent(s) selected from substituent group α; Y represents a group such as -CO-, -O- or -NRa-, and Ra represents a group such as a hydrogen atom or a C1-4 alkyl group.
NOVEL 7-SUBSTITUTED 3-CARBOXY-OXADIAZINO-QUINOLONE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION AS ANTI-BACTERIALS
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Page/Page column 33, (2009/09/08)
A subject of the invention is the compounds of formula (I): in which either R1 represents H, OH, NH2, —(CH2)m—NRaRb(m=0.1 or 2),Ra and Rb represent H, linear, branched or cyclic (C1 -C6) alkyl, (C3-C6) cycloalkyl-(C3-C6)— alkyl, Rc, S(O)2Rc, C(O)Rc, S(O)2Rd or C(O)Rd;or Ra and Rb with N form an Rc radical;Rc represents a saturated, unsaturated or 5- or 6-members aromatic ring, containing 1 to 4 heteroatoms chosen from N, O and S, optionally substituted;Rd represents a linear, branched or cyclic (C1-C6) alkyl, optionally substituted by 1 to 4 halogens;or R1 represents Rc or CHReRc or CHReRd;Re represents H, OH, NH2, NH—(C1-C6)-alk or N-(C1-C6)-alk2, or NH—(C1-C7)-acyl or NHRc;R2 represents H, (CH2)m—NRaRb, Rc, CHReRc or CHReRd, and R′2 represents H; it being understood that R1 and R2 cannot at the same time be H or that R1 and R2 or R2 and R1 cannot be one (CH2)m—NRaRb or Rc or H and the other one OH, or one H and the other one NH2, or one H and the other one (CH2)m—NRaRb in which Ra and Rb represent H or alkyl or C(O)Rd, in which Rd represents an unsubstituted alkyl or cycloalkyl; or R1 has the above definition except H and R2 and R′2 together represent gem dialkyl or alkyl-oxime, or R2 and R′2 represent respectively Rc or Rd and OH, NH2, NHRc or NHRf, Rf being a (C1-C7) acyl radical;or R1 represents H and R2 and R′2 together represent alkyl-oxime or one represents Rc and the other one represents OH, NH2, NHRc or NHRf;n is 0 or 1;R3 and R′3 represent H or (C1-C6) alkyl optionally substituted by 1 to 3 halogens or R3 represents (C1-C6) alkoxy carbonyl and R′3 represents H;R4 represents methyl optionally substituted by halogen;R5 represents H, (C1-C6) alkyl or (C7-C12) arylalkyl;R6 represents H, fluorine, NO2, CF3 or CN;in the form of enantiomers or mixtures, as well as their salts with acids and bases; their preparation and their application as anti-bacterials, in both human and veterinary medicine.
BENZIMIDAZOLE ANTAGONISTS OF THE H-3 RECEPTOR
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Page/Page column 21, (2010/11/27)
This invention is directed to a compound of formula (I), as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula (I), a process of preparation of a compound of formula (I), a method o
PHARMACEUTICAL COMPOUNDS
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Page/Page column 62-63, (2008/06/13)
Fused pyrimidines of formula (I); wherein A represents a thiophene or furan ring; n is 1 or 2; R1 is a group of formula (II); wherein m is 0 or 1; R30 is H or C1-C6 alkyl; R4 and R5 form, together with the N atom to which they are attached, a 5- or 6-membered saturated N-containing heterocyclic group which includes 0 or 1 additional heteroatoms selected from N, S and O, which may be fused to a benzene ring and which is unsubstituted or substituted; or one of R4 and R5 is alkyl and the other is a 5- or 6-membered saturated N-containing heterocyclic group as defined above or an alkyl group which is substituted by a 5- or 6-membered saturated N-containing heterocyclic group as defined above; R2 is selected from formula (a); wherein R6 and R7 form, together with the nitrogen atom to which they are attached, a morpholine, thiomorpholine, piperidine, piperazine, oxazepane or thiazepane group which is unsubstituted or substituted; and formula (b); wherein Y is a C2-C4 alkylene chain which contains, between constituent carbon atoms of the chain and/or at one or both ends of the chain, 1 or 2 heteroatoms selected from O, N and S, and which is unsubstituted or substituted; and R3 is an indazole group which is unsubstituted or substituted; and the pharmaceutically acceptable salt thereof have activity as inhibitors of P13K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with P13 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains
Willoughby, Christopher A.,Rosauer, Keith G.,Hale, Jeffery J.,Budhu, Richard J.,Mills, Sander G.,Chapman, Kevin T.,MacCoss, Malcolm,Malkowitz, Lorraine,Springer, Martin S.,Gould, Sandra L.,DeMartino, Julie A.,Siciliano, Salvatore J.,Cascieri, Margaret A.,Carella, Anthony,Carver, Gwen,Holmes, Karen,Schleif, William A.,Danzeisen, Renee,Hazuda, Daria,Kessler, Joseph,Lineberger, Janet,Miller, Michael,Emini, Emilio A.
, p. 427 - 431 (2007/10/03)
A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding affinity (1.8 nM) and antiviral activity in PBMC's (IC95=50 nM). Compound 4a also has improved PK properties relative to 1.