http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-035774-A1
Outgoing Links
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| filingDate | 2001-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2004-07-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-035774-A1 |
| titleOfInvention | BENZIMIDAZOL AND PIRIDILIMIDAZOL DERIVATIVES, A PROCEDURE FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND PACKAGES THAT UNDERSTAND THEM, THE USE OF SUCH COMPOUNDS ONLY OR IN COMBINATION FOR THE MANUFACTURE OF MEDICINES AS LIGANDOS FOR GABAAT TREATMENT, AND METHOD |
| abstract | Benzimidazole and pyridylimidazole derivatives, which comprise a compound having the formula (1) or a pharmaceutically acceptable salt, in which: Z1 is nitrogen or CR1; Z2 is nitrogen or CR2; Z3 is nitrogen or CR3; Z4 is nitrogen or CR4; with the proviso that no more than two of Z1, Z2, Z3 and Z4 are nitrogen; R1, R2, R3 and R4 are independently selected from i) hydrogen, halogen, hydroxy, nitro, cyano, amino, haloalkyl and haloalkoxy; ii) alkyl, alkoxy, cycloalkyl, alkenyl, alkynyl, (cycloalkyl) alkyl, -NH (R10), -N (R10) (R11), hydroxyalkyl, aminoalkyl, (R10) NHalkyl, (R10) (R11) Nalkyl, alkanoyl , alkoxycarbonyl, (heterocycloalkyl) alkyl, alkylsulfonyl, alkylthio, mono- or dialkylaminocarbonyl, heterocycloalkyl, aryl and heteroaryl, each of which is optionally substituted with 1, 2, 3 or 4 of R20; wherein R10 and R11 are independently selected from the group consisting of alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, (cycloalkyl) alkyl, aryl, arylalkyl, alkanoyl and mono- and dialkylaminoalkyl; and iii) a group of the formula -G-RA in which G is a bond, alkyl, -O-, -C (= O), or -CH2C (= O) -, and RA is a partially saturated carbocycle unsaturated or aromatic, consisting of a ring or two fused, pending, or spiro rings, where each ring contains 0, 1 or 2 heteroatoms independently selected from N, S and O, and said saturated, partially unsaturated, or aromatic carbocycle is optionally substituted with 1, 2, 3 or 4 of R20; iv) a group of the formula C (= O) J (RB) (RC) in which J is N, CH or C-alkyl and RB and RC are independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl , alkoxy, cycloalkyl, (cycloalkyl) alkyl, heterocycloalkyl, aryl arylalkyl, alkanoyl, heteroaryl, and mono- and dialkylaminoalkyl, each of which is optionally substituted with 1 or 2 substituents independently selected from halogen, hydroxy, cyano, amino, nitro , alkoxy, and alkyl; RB and RC and the atom to which they are attached form a monocyclic or bicyclic ring of 4 to 10 members, which may contain a) one or more double bonds, b) one or more oxo, O, S, SO, SO2 or N -RD where RD is hydrogen, Ar1, alkyl, cycloalkyl, heterocycloalkyl, or Ar1-alkyl; wherein Ar1 is aryl or heteroaryl, each of which is optionally substituted with 1 or 2 substituents independently selected from halogen, hydroxy, cyano, amino, nitro, alkoxy and alkyl, c) one or more R20 substituents; v) -OC (= O) RE, -C (= O) ORE, -C (= O) NH2, -C (= O) NHRE, -C (= O) NRERF, -S (O) mRE, - S (O) mNH2, -S (O) mNHRE, -S (O) mNRERF, -NHC (= O) RE, -C (= NRE) RF, -HC = N-OH, -HC = N (alkoxy) , -HC = N (alkyl), -NREC (= O) RF, -NHS (O) mRE and -NRES (O) mRF, where m is 0, 1 or 2; and RE and RF are independently selected each time it occurs between alkyl, cycloalkyl, heterocycloalkyl, alkoxy, mono- or dialkylamino, aryl, or heteroaryl each of which is optionally substituted with 1, 2 or 3 of R30; R20 is independently selected, each time it occurs, from the group consisting of: halogen, hydroxy, nitro, cyano, amino, alkyl, alkoxy optionally substituted with amino or mono- or dialkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, alkenyl, alkynyl, haloalkyl , oxo, haloalkoxy, mono- and dialkylamino, aminoalkyl and mono- and dialkylaminoalkyl; R30 is independently selected, every time it occurs, from halogen, hydroxy, nitro, cyano, amino, alkyl, alkoxy, optionally substituted with amino or mono- or dialkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkyl, heterocycloalkyl, alkenyl, alkynyl, haloalkyl, haloalkoxy , oxo, mono- and dialkylamino, aminoalkyl, and mono- and dialkylaminoalkyl; R5 represents hydrogen or haloalkyl; or R5 represents alkyl, cycloalkyl or (cycloalkyl) alkyl, each of which may contain one or more double bonds or triple bonds, and each of which is optionally substituted with 1, 2 or 3 of R30; or R5 represents aryl, arylalkyl, heteroaryl, or heteroarylalkyl, each of which is optionally substituted with 1, 2 or 3 substituents selected from the group consisting of haloalkyl, amino, -NH (R10), -N (R10) (R11) ), carboxamido, (R10) NHcarbonyl, (R10) (R11) Ncarbonyl, halogen, hydroxy, nitro, cyano, amino, alkyl, alkoxy optionally substituted with amino or mono- or dialkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, heterocycloalkyl, alkenyl, alkynyl, haloalkyl, haloalkoxy, aminoalkyl, and mono- and dialkylaminoalkyl; Q represents -C (R6) (R7) or oxygen, with the proviso that Q is not oxygen when X28 is nitrogen; R6 and R7 independently represent hydrogen, fluorine or alkyl; the group of formula (2) represents a 5- to 7-membered heteroaryl or heterocycloalkyl ring containing up to 4 heteroatoms selected from nitrogen, sulfur and oxygen and said 5- to 7-membered heteroaryl or heterocycloalkyl ring is substituted on each carbon atom with R , and is substituted on each nitrogen atom available for substitution with R ', where R is independently selected, whenever it occurs, between hydrogen, halogen, amino, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, (cycloalkyl) alkyl, haloalkyl , haloalkoxy, carboxamide, and 3 to 7 membered carbocyclic or heterocyclic groups that are saturated, unsaturated or aromatic, which may be further substituted with one or more substituents independently selected from halogen, oxo, hydroxy, alkyl, and alkoxy; R 'is independently chosen each time it occurs between alkyl, hydrogen, cycloalkyl, cycloalkyl (alkyl) and carbocyclic or heterocyclic groups of 3 to 7 members which are optionally substituted with one or more substituents independently selected from halogen, oxo, hydroxy, alkyl and alkoxy; X1 and X2 independently represent nitrogen, carbon or CH; Y is nitrogen, oxygen, carbon, -CH-, -CH2- or is absent; and W represents aryl or heteroaryl, where the aryl or heteroaryl group is optionally substituted with up to 4 groups independently selected from R30, -CO2H, -C (= O) ORE, -C (= O) NHRE, -C (= O) NRERF, -C (O) RE and -S (O) mRE, -ORE, where R30 and RE are as defined above and m is 0, 1 or 2. The compounds adhere with high selectivity and high affinity to the site GABAA receptor benzodiazepine. Pharmaceutical compositions and packages comprising said compounds and the use of said compounds for the manufacture of medicaments for the treatment of certain diseases of the central nervous system (CNS). Procedures for preparing the compounds of the formula (1). It also refers to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of the formula (1) in combination with one or more other CNS agents to enhance the effects of the other CNS agents. Additionally, use of said compounds as probes for the localization of GABAA receptors in tissue sections. |
| priorityDate | 2000-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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