'CHEMICAL DIVERSITY RESEARCH INSTITUTE' LTD. (Russia)
Inventor
Ivashchenko, Alexander Vasilievich
Ilyin, Aleksei Petrovich
Kysil, Volodymyr Mikhailovich
Trifilenkov, Andrei Sergeevich
Tsirulnikov, Sergey Alexandrovich
Shkirando, Alexander Mikhailovich
Churakova, Marina Vasilievna
Lomakina, Irina Olegovna
Potapov, Viktor Vladimirovich
Zamaletdinova, Anastasiya Iliyasovna
Tkachenko, Sergey Yevgenievich
Kravchenko, Dmitri Vladimirovich
Khvat, Alexander Viktorovich
Okun, Ilya Matusovich
Kyselev, Alexander Sergeevich
Abstract
The invention relates to novel azaheterocycles of interest as potential physiologically active substances (agonists, antagonists, receptor modulators, ferment inhibitors, oncolytics, antibacterial and antiparasitic agent etc.), to combinatory and focused libraries comprising novel azaheterocycles of a pharmaceutical composition containing said novel azaheterocycles in the form of an active substance and to methods for the production and the use thereof. Said novel azaheterocycles are of general formula (1), wherein W is an azaheterocycle which comprises 6-12 atoms, is optionally annelated, has at least one C5-C7 carbocycle and/or heterocycle, and also comprises at least one of heteroatoms and is selected from an O, S or N group; R1ais an aminogroup substituent, apart from hydrogen, preferably C1-C6 alkyl, aryl or heterocycle comprising at least one of heteroatoms selected from theO, S or N group; Rb is a carbamoyl group -C(O)NHRa in which Ra is the aminogroup substituent, apart from hydrogen; Rc is a cyclic system substituent, preferably C1-C6 alkyl, alkyl, aryl or heterocycle comprising at least one of heteroatoms selected from theO, S or N group, or Rb and Rc together form an amino-cyano-methylen [(=C(NH2)CN] group.
C07D 241/06 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
C07D 241/08 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
C07D 241/36 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
C07D 243/06 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
C07D 243/08 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
C07D 243/10 - Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
C07D 245/04 - Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
C07D 245/06 - Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems condensed with one six-membered ring
C07D 255/02 - Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups not condensed with other rings
C07D 255/04 - Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups condensed with carbocyclic rings or ring systems
C07D 507/02 - Heterocyclic compounds containing a condensed beta-lactam ring system, not provided for by groups , or Such ring systems being further condensed containing 3-oxa-1-azabicyclo [3.2.0] heptane ring systems
C40B 40/04 - Libraries containing only organic compounds
C07D 267/00 - Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
C07D 267/14 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
C07D 281/06 - Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
C07D 281/08 - Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
C07D 283/00 - Heterocyclic compounds containing rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms, according to more than one of groups
C07D 321/00 - Heterocyclic compounds containing rings having two oxygen atoms as the only ring hetero atoms, not provided for by groups
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
C07D 417/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
C07D 491/056 - Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 491/147 - Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
C07D 491/153 - Ortho-condensed systems the condensed system containing two rings with oxygen as ring hetero atom and one ring with nitrogen as ring hetero atom
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines having two or more nitrogen atoms in the same ring, e.g. oxadiazines
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem