- Flavin mimetics: Synthesis and photophysical properties
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We report the synthesis of new isoalloxazines using a microwave-assisted approach to make N-substituted-2-nitroanilines followed by one-pot reduction and condensation via Hemmerich's method. The influence of substituents on positions 7, 8, and 10 of flavin core on the optical properties is investigated. The aliphatic functionalities on N10 give rise to quantum yields of 0.7, while aromatic side-chains quench fluorescence. Relaxed geometries (DFT) of chiral and achiral derivatives have been used for TD-DFT calculations, which yielded good agreement with the experimental UV and CD data.
- R?s?dean, Dora-M.,Machida, Takashi,Sada, Kazuki,Pudney, Christopher R.,Panto?, G. Dan
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- 2-(4-ARYL-1H-IMIDAZOL-1-YL)ANILINE COMPOUNDS
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The present invention provides compounds that are useful as vaccine adjuvants and/or antitumor agents and methods for producing and using the same. In one particular aspect of the invention, compounds of the invention are of the formula (I) where R1, R2, R3 and Ar1 are those defined herein.
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Paragraph 0047; 0068
(2015/11/27)
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- Pyrimidineamines as angiogenesis modulators
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Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
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Paragraph 0189; 0190
(2015/11/16)
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- Compounds for use in inhibiting HIV capsid assembly
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The present invention relates to a compound or a pharmaceutically acceptable salt or solvate thereof for use in inhibiting HIV capsid assembly, the compound comprising the core structure wherein E is CR7or S, and wherein f is 0 or 1, and wherein in case E is S, f is 0, and wherein the core structure is at least substituted in 2 and 4 position, and wherein the residue R6 and R7, are, independently of each other, selected from the group consisting of -H, -D, -alkyl, alkoxy, alkenyl, alkynyl, halides, -NO2, - OH, - NH2, -NHR4#, -CN, -S(O)R4#, -SO2R4#, -P(O)R4#R5#, -P(O)(OR4#)R5#, - P(O)(OR4#)(OR5#), -C(O)NR4#R5#, -C(O)SR4#, -C(O)R4#, -C(O)O-R4#, alkoxy and glycol chains; and wherein R6 may optionally form a cyclic residue, with a further substituent present 5 or 6 position, and wherein R4# and R5# are, independently of each other, selected from the group consisting of -H, -alkyl, -alkenyl, - heterocycloalkyl, aryl and heteroaryl.
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Paragraph 0160-0161
(2014/09/03)
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- COMPOUNDS FOR USE IN INHIBITING HIV CAPSID ASSEMBLY
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The present invention relates to a compound or a pharmaceutically acceptable salt or solvate thereof for use in inhibiting HIV capsid assembly, the compound comprising the core structure wherein E is CR7or S, and wherein f is 0 or 1, and wherein in case E is S, f is 0, and wherein the core structure is at least substituted in 2 and 4 position, and wherein the residue R6 and R7, are, independently of each other, selected from the group consisting of -H, -D, -alkyl, alkoxy, alkenyl, alkynyl, halides, -NO2, - OH, -NH2, -NHR4#, -CN, - S(O)R4#, -SO2R4#, -P(O)R4#R5#, -P(O)(OR4#)R5#, -P(O)(OR4#)(OR5#), -C(O)NR4#R5#, - C(O)SR4#, -C(O)R4#, -C(O)O-R4#, alkoxy and glycol chains; and wherein R6 may optionally form a cyclic residue, with a further substituent present 5 or 6 position, and wherein R4# and R5# are, independently of each other, selected from the group consisting of -H, -alkyl, -alkenyl, -heterocyclo alkyl, aryl and heteroaryl.
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Page/Page column 51
(2014/09/03)
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- PROCESS FOR PREPARING BENDAMUS TINE HYDROCHLORIDE MONOHYDRATE
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The present invention provide processes for the preparation of Bendamustine hydrochloride monohydrate of formula (I) The present application also provides a process of purification of Bendamustine hydrochloride or monohydrate to get substantially pure Bendamustine hydrochloride monohydrate crystalline Form-SM. The said Bendamustine hydrochloride monohydrate crystalline Form-SM is characterized by X-ray powder diffraction pattern comprising at least 5 characteristic peaks selected from the XRPD 2 theta degrees peaks at 7.42, 10.60, 11.17, 16.43, 17.94, 22.89, 26.33, 28.77, 30.28, 31.92, 40.89±0.1 2θ°. The present application also provides a process for the preparation of Bendamustine hydrochloride monohydrate crystalline Form-SM useful in making pharmaceutical composition for the treatment of cancer or similar proliferative disorders.
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Paragraph 0160-0162
(2013/08/28)
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- 2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.
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Page/Page column 163
(2012/05/20)
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- PROCESS FOR PREPARING BENDAMUS TINE HYDROCHLORIDE MONOHYDRATE
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A process for preparing Bendamustine hydrochloride monohydrate is provided. A process for purifying said monohydrate to get substantially purne Bendamustine hydrochloride monohydrate crystalline form is also provided.
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Page/Page column 26
(2012/05/20)
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- HYDROXAMIC ACID DERIVATIVES
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The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
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Page/Page column 41
(2010/08/08)
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- INHIBITORS OF HIV REPLICATION
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The present invention relates to compounds of formula (I) wherein R1, R2, R3 and R4 are as defined herein, compositions and uses thereof for treating human immunodeficiency virus (HIV) infection. In particular,
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Page/Page column 46
(2008/12/06)
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- Synthesis of benzo[1,2-d;3,4-d′]diimidazole and 1H-pyrazolo[4,3-b] pyridine as putative A2A receptor antagonists
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The synthesis and the binding affinity for the putative adenosine receptor antagonist 6-methyl-7-[1,2,3]triazol-2-yl-1,6-dihydrobenzo[1,2-d;3,4-d′] diimidazole (10) and 5-oxazol-2-yl-1H-pyrazolo[4,3-b]pyridin-3-ylamine (16) are reported. The title compounds were prepared from commercially available 1-chloro-2,4-dinitrobenzene (1) and 2-chloro-6-methoxy-3nitropyridine (11), respectively, but proved devoid of affinity for the adenosine A1 and A2A receptors. The Royal Society of Chemistry.
- Piersanti, Giovanni,Giorgi, Luca,Bartoccini, Francesca,Tarzia, Giorgio,Minetti, Patrizia,Gallo, Grazia,Giorgi, Fabrizio,Castorina, Massimo,Ghirardi, Orlando,Carminati, Paolo
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p. 2567 - 2571
(2008/03/14)
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- INHIBITORS OF HISTONE DEACETYLASE
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The invention relates to a series of compounds useful for inhibiting histone deacetylase (HDAC) enzymatic activity. The invention also provides a method for inhibiting histone descetylase in a cell using said compounds as well as a method for treating cell proliferative diseases and conditions using said HDAC inhibitors. Further, the invention provides pharmaceutical compositions comprising the HDAC inhibiting compounds and a pharmaceutically acceptable carrier.
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Page/Page column 151-152
(2010/02/14)
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- DIAMINO-PYRIMIDINES AND THEIR USE AS ANGIOGENESIS INHIBITORS
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Benzimidazole derivatives of formula (I) , which are useful as TIE-2 and/or VEGFR-2 inhibitors are described herein. The described invention also includes methods of making such benzimidazole derivatives as well as methods of using the same in the treatme
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Page/Page column 59; 102
(2010/02/07)
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- Efficient solution phase synthesis of 2-(N-acyl)-aminobenzimidazoles
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An efficient solution phase protocol for the synthesis of 2-(N-acyl)-aminobenzimidazoles is reported. The 2-(N-acyl)-aminobenzimidazole ring system was assembled using SNAr reactions, nitro group reduction, acylthiourea formation and cyclization with EDC. The acyl protected 2-aminobenzimidazole derivatives were obtained in high yield and purity without purification of intermediates or final products. This reaction sequence eliminates the use of highly toxic cyanogen bromide, a reagent commonly used to prepare the 2-aminobenzimidazole ring system.
- Seth, Punit P.,Robinson, Dale E.,Jefferson, Elizabeth A.,Swayze, Eric E.
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p. 7303 - 7306
(2007/10/03)
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- Antithrombotic quinoxazolines
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Quinoxazolines having antithrombotic activity. Exemplary of those disclosed are: 4-{[6-(N-carboxymethyl-quinolin-8-yl-sulphonylamino)-1-methyl-2-oxo-1,2-dihydroquinoxalin-3-yl]-methyl}-benzamidine, 4-{[6-(1-(N-cyclopentyl-carboxymethylcarbonylamino)-cyclo-propyl)-1-methyl-2-oxo-1,2-dihydroquinoxalin-3-yl]-methyl}-benzamidine, and 4-{[7-(N-carboxymethylaminocarbonyl-ethylamino)-4-methyl-quinolin-2-yl]-oxo}-benzamidine.
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- Bicyclic heterocycles, the preparation thereof, and their use as pharmaceuticals
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The present invention relates to 5-membered heterocyclic condensed benzoderivatives of formula wherein Ra to Rc, A, X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable properties. The compounds of the above formula I wherein Rc denotes a cyano group are valuable intermediates for preparing the other compounds of formula I, and the compounds of the above formula I wherein Rc denotes one of the following amidino groups and the tautomers and stereoisomers thereof have valuable pharmacological properties, particularly an antithrombotic activity.
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- New Routes to Selectively Methylated Benzimidazoles
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The use of intermediate benzotriazol-1-yl derivatives simplified the procedures for the preparation of 5-methoxy-1-methylbenzimidazole and 6-methoxy-1-methylbenzimidazole starting from 4-methoxy-2-nitroaniline.This strategy represents a novel and potentia
- Katritzky, Alan R.,Rachwal, Stanislaw,Ollmann, Richard
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p. 775 - 780
(2007/10/02)
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- Process for the manufacture of benzimidazolones-(2)
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Process for the manufacture of benzimidazolones-(2) wherein an o-phenylenediamine is reacted with optionally alkylated urea in the ratio of 1 to 1.3 moles per mole o-phenylenediamine in an organic solvent which has a solubility in water of not more than 5 g/l and has a boiling point above 100° C, at a temperature between 100° and 200° C.
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