188641-35-2Relevant academic research and scientific papers
Highly stable atropisomers by electrophilic amination of a chiral γ-lactam within the synthesis of an elusive conformationally restricted analogue of α-methylhomoserine
Amabili, Paolo,Amici, Adolfo,Civitavecchia, Annafelicia,Maggiore, Beatrice,Orena, Mario,Rinaldi, Samuele,Tolomelli, Alessandra
, p. 461 - 478 (2016)
Starting from chiral-protected 4-hydroxymethyl pyrrolidin-2-ones, the otherwise elusive 3,4-trans-3,3,4-trisubstituted isosteres of α-methyl homoserine, tethered on a γ-lactam ring, were prepared exploiting stereoselective electrophilic aminations. These
SUBSTITUTED NAPHTHYRIDINES AND USE THEREOF AS MEDICINES
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Page/Page column 17, (2011/09/14)
The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 denotes a group A selected from among —O—R3, —NR3R4, —CR3R4R5, -(ethyne)-R3, —S—R3, —SO—R3 and SO2—R3 or R1 denotes a group B selected from among C6-10-aryl,five- to ten-membered, mono- or bicyclic heteroaryl with 1-3 heteroatoms selected independently of one another from among N, O and S; while this heteroaryl is linked to the structure according to formula 1 via either a C atom or an N atom,three- to ten-membered, mono- or bicyclic, saturated or partially saturated heterocyclic group with 1-3 heteroatoms selected independently of one another from among N, O and S, while this heterocyclic group is linked to the structure according to formula 1 via either a C atom or an N atom, and 5- to 11-membered spiro group which may optionally contain 1, 2 or 3 heteroatoms selected independently of one another from among N, O and S, while this spiro group is linked to the structure according to formula 1 via either a C atom or an N atom, while this group B may optionally be substituted as described in claim 1 and wherein R2 is and R3, R4, R5, R6, R6′, R7, R8, R9, R10, V, n and m may have the meanings given in claim 1, as well as pharmaceutical compositions containing these compounds.
Alpha2delta ligands for fibromyalgia and other disorders
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, (2008/06/13)
This invention relates to a method of treating a disorder selected from OCD, agoraphobia, agoraphobia without history of panic disorder, specific phobia, social phobia, PTSD, restless legs syndrome, premenstrual dysphoric disorder, hot flashes, and fibromyalgia by administering a compound of the formula 1 or a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen, straight or branched alkyl of from 1 to 6 carbon atoms or phenyl; and R2 is straight or branched alkyl of from 4 to 8 carbon atoms, straight or branched alkenyl of from 2 to 8 carbon atoms, cycloalkyl of from 3 to 7 carbon atoms, alkoxy of from 1 to 6 carbon atoms, -alkylcycloalkyl, -alkylalkoxy, -alkyl OH, -alkylphenyl, -alkylphenoxy, or -substituted phenyl. The invention also relates to a method of treating the above disorders by administering the compound (3S, 5R)-3-Aminomethyl-5-methyl-octanoic acid
Method of treating tinnitus
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, (2008/06/13)
The invention relates to a method of treating tinnitus by administering an alpha2delta ligand such as, for example, a compound of Formula and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or straight or branched lower alkyl, and n is an integer of from 4 to 6.
Mono-and disubstituted 3-propyl gamma-aminobutyric acids
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, (2008/06/13)
The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula I 1The compounds are useful as therapeutic agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, arthritis, sleep disorders, IBS, and gastric damage. Methods of preparing the compounds and useful intermediates are also part of the invention.
Method of treating cartilage damage
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, (2008/06/13)
The invention relates to a method of preventing or treating cartilage damage by administering a GABA analog such as, for example, a compound of Formula 1and pharmaceutically acceptable salts thereof, wherein R1 is hydrogen or straight or branched lower alkyl, and n is an integer of from 4 to 6.
From 3-aza-2-oxobicyclo[3.1.0]hexane to enantiopure disubstituted cyclopropane: A convenient approach to cis-2,3-methano-GABA
Galeazzi, Roberta,Mobbili, Giovanna,Orena, Mario
, p. 133 - 137 (2007/10/03)
Starting from the diastereomerically pure 4-ethenyl pyrrolidin-2-one 5, through simple steps the mesyl derivative 8 was obtained, which underwent intramolecular alkylation to give, in good yield, the 3-aza-2-oxobicyclo[3.1.0]hexane 9. This compound was su
