Patent classifications
C07D243/24
Compounds Which Have a Protective Activity with Respect to the Action of Toxins and of Viruses with an Intracellular Mode of Action
The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
Antiviral benzodiazepine compounds
The invention relates to compounds of formula (I), and pharmaceutical uses thereof. Particular aspects of the invention relate to methods of synthesising the compounds and the use of those compounds in treating, ameliorating, or preventing a microbial infection.
Antiviral benzodiazepine compounds
The invention relates to compounds of formula (I), and pharmaceutical uses thereof. Particular aspects of the invention relate to methods of synthesising the compounds and the use of those compounds in treating, ameliorating, or preventing a microbial infection.
COMPOSITIONS COMPRISING SHORT-ACTING BENZODIAZEPINES
The present invention provides novel compositions comprising benzodiazepine derivatives according to formula (I). Also provided are compositions comprising at least one hygroscopic excipient, in particular lactose and/or dextran.
##STR00001##
COMPOSITIONS COMPRISING SHORT-ACTING BENZODIAZEPINES
The present invention provides novel compositions comprising benzodiazepine derivatives according to formula (I). Also provided are compositions comprising at least one hygroscopic excipient, in particular lactose and/or dextran.
##STR00001##
1,4-benzodiazepin-2-one derivatives and use thereof
The invention relates to novel compounds that are derivatives of 1,4-benzodiazepin-2-one, having the general formula I: ##STR00001## and being limited to structural variants 1-6: ##STR00002## on condition that: a) structures 1 (R.sup.1=Br, R.sup.4=F), 3 (R.sup.1=OCF.sub.3, R.sup.4=H), 5 (R.sup.1=NO.sub.2, R.sup.4=Cl) and 6 (R.sup.1=NO.sub.2, R.sup.4=F) have the following substituents R.sup.2 and R.sup.3: R.sup.2=H, CH.sub.2COCH.sub.3, CH.sub.2COOCH.sub.3, CH.sub.2CONHNH.sub.2; R.sup.3=OAlk, NHAr, where Alk=C.sub.2H.sub.5, C.sub.3H.sub.7, C.sub.4H.sub.9, (CH.sub.2).sub.2OH, (CH.sub.2).sub.2OCH.sub.3, ##STR00003## ##STR00004##
R.sup.5=o-, m-, p-COCH.sub.3, Cl, F, Br, NO.sub.2, CF.sub.3; b) structure 2 (R.sup.1=Cl, R.sup.4=H) has the following substituents R.sup.2 and R.sup.3: if R.sup.2=H, then R.sup.3=OAlk, NHAr, where Alk=(CH.sub.2).sub.2OCH.sub.3, ##STR00005## ##STR00006##
R.sup.5=m-, p-COCH.sub.3, o-, m-, p-F, Br, CF.sub.3; if R.sup.2=CH.sub.2COCH.sub.3, CH.sub.2COOCH.sub.3, CH.sub.2CONHNH.sub.2, then R.sup.3=OAlk, NHAr, where Alk=C.sub.2H.sub.5, C.sub.3H.sub.7, C.sub.4H.sub.9, (CH.sub.2).sub.2OH, (CH.sub.2).sub.2OCH.sub.3, ##STR00007## ##STR00008##
R.sup.5=o-, m-, p-COCH.sub.3, Cl, F, Br, NO.sub.2, CF.sub.3; c) structure 4 (R.sup.1=NO.sub.2, R.sup.4=H) has the following substituents R.sup.2 and R.sup.3: if R.sup.2=H, then R.sup.3=OAlk, NHAr, where Alk=(CH.sub.2).sub.2OCH.sub.3, ##STR00009## ##STR00010##
R.sup.5=o-, m-, p-COCH.sub.3, Cl, F, Br, NO.sub.2, CF.sub.3; if R.sup.2=CH.sub.2COCH.sub.3, CH.sub.2COOCH.sub.3, CH.sub.2CONHNH.sub.2, then R.sup.3=OAlk, NHAr, where Alk=C.sub.2H.sub.5, C.sub.3H.sub.7, C.sub.4H.sub.9, (CH.sub.2).sub.2OH, (CH.sub.2).sub.2OCH.sub.3, ##STR00011## ##STR00012##
R.sup.5=o-, m-, p-COCH.sub.3, Cl, F, Br, NO.sub.2, CF.sub.3
and the use of said compounds in the field of medicine as analgesics, anorexigenic or orexigenic agents for weight regulation (loss or gain), antidepressants and anxiolytics for treating psychological disorders, and also antihypoxic and nootropic agents for the prophylaxis and treatment of central nervous system disorders.
1,4-benzodiazepin-2-one derivatives and use thereof
The invention relates to novel compounds that are derivatives of 1,4-benzodiazepin-2-one, having the general formula I: ##STR00001## and being limited to structural variants 1-6: ##STR00002## on condition that: a) structures 1 (R.sup.1=Br, R.sup.4=F), 3 (R.sup.1=OCF.sub.3, R.sup.4=H), 5 (R.sup.1=NO.sub.2, R.sup.4=Cl) and 6 (R.sup.1=NO.sub.2, R.sup.4=F) have the following substituents R.sup.2 and R.sup.3: R.sup.2=H, CH.sub.2COCH.sub.3, CH.sub.2COOCH.sub.3, CH.sub.2CONHNH.sub.2; R.sup.3=OAlk, NHAr, where Alk=C.sub.2H.sub.5, C.sub.3H.sub.7, C.sub.4H.sub.9, (CH.sub.2).sub.2OH, (CH.sub.2).sub.2OCH.sub.3, ##STR00003## ##STR00004##
R.sup.5=o-, m-, p-COCH.sub.3, Cl, F, Br, NO.sub.2, CF.sub.3; b) structure 2 (R.sup.1=Cl, R.sup.4=H) has the following substituents R.sup.2 and R.sup.3: if R.sup.2=H, then R.sup.3=OAlk, NHAr, where Alk=(CH.sub.2).sub.2OCH.sub.3, ##STR00005## ##STR00006##
R.sup.5=m-, p-COCH.sub.3, o-, m-, p-F, Br, CF.sub.3; if R.sup.2=CH.sub.2COCH.sub.3, CH.sub.2COOCH.sub.3, CH.sub.2CONHNH.sub.2, then R.sup.3=OAlk, NHAr, where Alk=C.sub.2H.sub.5, C.sub.3H.sub.7, C.sub.4H.sub.9, (CH.sub.2).sub.2OH, (CH.sub.2).sub.2OCH.sub.3, ##STR00007## ##STR00008##
R.sup.5=o-, m-, p-COCH.sub.3, Cl, F, Br, NO.sub.2, CF.sub.3; c) structure 4 (R.sup.1=NO.sub.2, R.sup.4=H) has the following substituents R.sup.2 and R.sup.3: if R.sup.2=H, then R.sup.3=OAlk, NHAr, where Alk=(CH.sub.2).sub.2OCH.sub.3, ##STR00009## ##STR00010##
R.sup.5=o-, m-, p-COCH.sub.3, Cl, F, Br, NO.sub.2, CF.sub.3; if R.sup.2=CH.sub.2COCH.sub.3, CH.sub.2COOCH.sub.3, CH.sub.2CONHNH.sub.2, then R.sup.3=OAlk, NHAr, where Alk=C.sub.2H.sub.5, C.sub.3H.sub.7, C.sub.4H.sub.9, (CH.sub.2).sub.2OH, (CH.sub.2).sub.2OCH.sub.3, ##STR00011## ##STR00012##
R.sup.5=o-, m-, p-COCH.sub.3, Cl, F, Br, NO.sub.2, CF.sub.3
and the use of said compounds in the field of medicine as analgesics, anorexigenic or orexigenic agents for weight regulation (loss or gain), antidepressants and anxiolytics for treating psychological disorders, and also antihypoxic and nootropic agents for the prophylaxis and treatment of central nervous system disorders.
COMPOSITIONS AND METHODS FOR REDUCING TACTILE DYSFUNCTION, ANXIETY, AND SOCIAL IMPAIRMENT
The present invention provides novel peripherally-restricted benzodiazepines with reduced blood brain barrier permeability and methods of use thereof for reducing tactile dysfunction, social impairment, and anxiety in a subject diagnosed with Autism Spectrum Disorder, Rett syndrome, Phelan McDermid syndrome, or Fragile X syndrome.
COMPOSITIONS AND METHODS FOR REDUCING TACTILE DYSFUNCTION, ANXIETY, AND SOCIAL IMPAIRMENT
The present invention provides novel peripherally-restricted benzodiazepines with reduced blood brain barrier permeability and methods of use thereof for reducing tactile dysfunction, social impairment, and anxiety in a subject diagnosed with Autism Spectrum Disorder, Rett syndrome, Phelan McDermid syndrome, or Fragile X syndrome.
Use of 7-bromo-5-(O-chlorophenyl)-3-propoxy-1,2-dihydro-3H-1,4-benzodiazepin-2-one for inhibition of neuropathic pain and seizures of different etiology
The invention relates to medical chemistry, in particular to the use of 7-bromo-5-(o-chlorophenyl)-3-propoxy-1,2-di-hydro-3H-1,4-benzodiazepin-2-one as a drug which inhibits neuropathic pain without the formation of defects in the gastric mucosa (ulcerogenic effect), and possesses an anticonvulsant property.