204078-35-3Relevant articles and documents
Azaindolylidene derivatives as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
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Page/Page column 40, (2010/11/27)
The present invention is directed to compounds of the formula or pharmaceutically acceptable salts, prodrug, solvate or optical isomer thereof, pharmaceutical compositions containing same and use thereof for treating diseases linked to disregulated cell p
PYRAZOLO[1,5-A]PYRIMIDIN-7-YL-AMINE DERIVATIVES FOR USE IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES
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Page/Page column 82, (2008/06/13)
The invention relates to the use of pyrazolo[1,5a]pyrimidin-7-yl amine compounds and salts thereof in the treatment of kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds, and a process for the preparation of the novel pyrazolo[1,5a]pyrimidin-7-yl amine compounds.
Synthesis and evaluation of cyclic secondary amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents
Tangallapally, Rajendra P.,Yendapally, Raghunandan,Lee, Robin E.,Lenaerts, Anne J. M.,Lee, Richard E.
, p. 8261 - 8269 (2007/10/03)
In an ongoing effort to develop new and potent antituberculosis agents, a second-generation series of nitrofuranyl amides was synthesized on the basis of the lead compound 5-nitrofuran-2-carboxylic acid 3,4-dimethoxybenzylamide. The primary design consideration was to improve the solubility and consequently the bioavailability of the series by the addition of hydrophilic rings to the benzyl and phenyl B ring core. The synthesis of 27 cyclic, secondary amine substituted phenyl and benzyl nitrofuranyl amides is described and their activity against Mycobacterium tuberculosis reported. The series showed a strong structure-activity relationship as the benzyl nitrofuranyl amides were significantly more active than similarly substituted phenyl nitrofuranyl amides. Para-substituted benzyl piperazines showed the most antituberculosis activity. Compounds in the series were subsequently selected for bioavailability and in vivo testing. This study led to the successful discovery of novel compounds with increased antituberculosis activity in vitro and a better understanding of the requisite pharmacological properties to advance this class.
HETEROCYCLIC AMIDES WITH ANTI-TUBERCULOSIS ACTIVITY
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Page 64, (2010/02/10)
Compounds having the general structure (I) : wherein A is selected from the group consisting of oxygen, sulfur, and NR15, and R15 is selected from the group consisting of H, alkyl, aryl, substituted alkyl, and substituted aryl; B, D, and E are each independently selected from the group consisting of CH, nitrogen, sulfur and oxygen; R1 is selected from the group consisting of nitro, halo, alkyl ester, phenylsulfanyl, phenylsulfinyl, phenylsulfonyl and sulfonic acid; t is an integer from 1 to 3; and X is a substituted amide and methods of using the novel compounds for treating infections caused microorganisms, including Mycobacterium tuberculosis.
Heterocyclic amides with anti-tuberculosis activity
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, (2008/06/13)
Compounds having the general structure: wherein A is selected from the group consisting of oxygen, sulfur, and NR15, and R15 is selected from the group consisting of H, alkyl, aryl, substituted alkyl, and substituted aryl; B,D, and E are each independently selected from the group consisting of CH, nitrogen, sulfur and oxygen; R1 is selected from the group consisting of nitro, halo, alkyl ester, arylsulfanyl, arylsulfinyl, arylsulfonyl and sulfonic acid; t is an integer from 1 to 3; and X is a substituted amide, and methods of using the novel compounds for treating infections caused by microorganisms, including Mycobacterium tuberculosis.
Method of inhibiting neoplastic cells with imidazoquinazoline derivatives
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, (2008/06/13)
A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to imidazoquinazoline derivatives.
Improved yields of meta-amination and symmetrical and unsymmetrical diamination of benzenes
Brown, George R.,Foubister, Alan J.,Roberts, Craig A.,Wells, Stuart L.,Wood, Robin
, p. 3917 - 3919 (2007/10/03)
Much higher yields were found after shorter reaction times for the meta-substituted amination of benzenes in DMPU with microwave heating in a sealed tube (180°C, 5 h), e.g. piperidine and m-fluorobenzonitrile 1 gave the m-substituted 3 in 92% yield. These
Imidazoquinazoline derivatives
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, (2008/06/13)
PCT No. PCT/JP97/03023 Sec. 371 Date Apr. 27, 1998 Sec. 102(e) Date Apr. 27, 1998 PCT Filed Aug. 29, 1997 PCT Pub. No. WO98/08848 PCT Pub. Date Mar. 5, 1998Imidazoquinoline derivatives of the formula (wherein X may be O or S) provide selective cyclic guanosine 3',5' monophosphate (cGMP)-specific phosphodiesterase (PDE) inhibitory activity. The compounds are useful for treating or ameliorating cardiovascular disease such as thrombosis, angina pectoris, hypertension, heart failure and arterial sclerosis, as well as asthma, impotence and the like.
High yields of meta-substituted amination products in the S(N)Ar substitution of benzenes
Brown,Foubister,Ratcliffe
, p. 1219 - 1222 (2007/10/03)
Morpholine substitution in fluorobenzenes containing a meta-substituted electron withdrawing group proceeds in DMSO at 100 °C over 60 h to give meta-substitution products (by fluoride ion displacement) in pure isolated yields of 19-98%.
Synthesis of meta-substituted aniline derivatives by nucleophilic substitution
Belfield, Andrew J.,Brown, George R.,Foubister, Alan J.,Ratcliffe, Paul D.
, p. 13285 - 13300 (2007/10/03)
Substitution by amines of fluorobenzenes containing a meta- substituted electron withdrawing group (EWG), in DMSO at 100 °C over 60 h gave meta-substituted aniline derivatives in isolated yields of up to 98%. The scope of the reaction is explored in terms of reaction conditions and substrates. It is postulated that facile meta-substitutions are facilitated through field stabilisation of the intermediate anion by EWG substituents.