http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2239641-C2
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filingDate | 1998-11-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2004-11-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bc5f6a2271753638c7afb1dc98f5604a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_538dfd3a7555ae3280ef8826758dc032 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b8271320e954800afab62d2771d664a7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cd345e0d4c9311d5c962462ecec81e6f |
publicationDate | 2004-11-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | RU-2239641-C2 |
titleOfInvention | Substituted derivatives of imidazolidine, method for preparing and pharmaceutical preparation |
abstract | FIELD: organic chemistry, medicine, pharmacy. n SUBSTANCE: invention relates to substituted derivatives of imidazolidine of the formula (I): n wherein W means R 1 -A-C(R 13 ) or compound of the formula: n n n n wherein ring system can be substituted with 1, 2 or 3 similar or different substituents R 13 ; L means C(R 13 ); m 1 and m 2 means independently of one another 0, 1, 2, 3 or 4 and sum m 1 + m 2 = 3 or 4; Y means carbonyl group; A means a direct bond or bivalent phenylene residue; B means bivalent (C 1 -C 6 )-alkylene residue wherein (C 1 -C 6 )-alkylene residue is unsubstituted or substituted with one or some similar or different residues taken among (C 1 -C 8 )-alkyl and (C 3 -C 10 )-cycloalkyl-(C 1 -C 6 )-alkyl; E means R 10 CO, HCO or R 8 O-CH 2 ; R means hydrogen atom (H) or (C-C 8 )-alkyl, (C 3 -C 12 )-cycloalkyl-(C 1 -C 8 )-alkyl or, if necessary, substituted (C 6 -C 14 )-aryl wherein all R residues are not dependent of one another and can be similar or different; R 1 means hydrogen atom (H), (C 1 -C 10 )-alkyl that, if necessary, can be substituted one or many times with fluorine atom or residue X-NH-C(=NH)-R 20 wherein X means hydrogen atom (H); R 2 means hydrogen atom (H) or (C 1 -C 8 )-alkyl; R 3 means hydrogen atom (H), (C 1 -C 10 )-alkyl that can be one or many times substituted, if necessary, with fluorine atom, if necessary substituted (C 6 -C 14 )-aryl, if necessary substituted heteroaryl, (C 6 -C 12 )-bicycloalkyl, R 11 NH, COOR 21 , CONHR 4 or CONHR 15 ; R 4 means (C 1 -C 10 )-alkyl that is unsubstituted or substituted once or many times with similar or different residues taken among of the order: hydroxycarbonyl, aminocarbonyl, mono- or di-[(C 1 -C 10 )-alkyl]-aminocarbonyl, (C 1 -C 8 )-alkoxycarbonyl, R 5 , R 6 -CO wherein R 5 means, if necessary, substituted (C 6 -C 14 )-aryl; R 6 means residue of natural or non-natural amino acid; R 8 means hydrogen atom (H) or (C 1 -C 10 )-alkyl wherein R 8 can be similar or different being independent of one another; R 10 means hydroxy-group, (C 1 -C 10 )-alkoxy-group, (C 1 -C 8 )-alkylcarbonyloxy-(C 1 -C 6 )-alkoxy-group, (C 1 -C 8 )-alkoxycarbonyloxy-(C 1 -C 6 )-alkoxy-group, amino-group, mono- or di-[(C 1 -C 10 )-alkyl]-amino-group or R 8 R 8 N-CO-(C 1 -C 6 )-alkoxy-group wherein R 8 residues can be similar or different being independently of one another; R 11 means R 12a -O-CO or R 12a -S(O) 2 wherein R 12a means (C 1 -C 10 )-alkyl, if necessary substituted (C 6 -C 14 )-aryl, if necessary (C 6 -C 14 )-aryl-(C 1 -C 4 )-alkyl substituted by aryl residue or R 15 ; R 13 means hydrogen atom (H) or (C 1 -C 6 )-alkyl that can be substituted, if necessary, one or many times with fluorine atom; R 15 means R 16 -(C 1 -C 6 )-alkyl or R 16 wherein R 16 means form 6-membered to 24-membered bicyclic or tricyclic residue; R 20 means a direct bond or (C 1 -C 6 )-alkylene; R 21 means hydrogen atom (H) or (C 1 -C 8 )-alkyl; R 30 means one of residues R 32 (R)N-CO-N(R)R 31 or R 32 (R)N-CS-N(R)R 31 ; R 32 -CO-N(R)-R 31 or R 12a -O-CO-N(R)-R 31 being R 30 can't mean R 32 -CO-N(R)R 31 if W means simultaneously R 1 -A-C(R 13 ); A means a direct bond; R 1 and R 13 mean hydrogen atom (H); R 31 means bivalent residue -R 33 -R 34 -R 5 -R 36 wherein R 36 is bound with nitrogen atom in imidazoline ring of the formula (I); R 32 means (C 1 -C 8 )-alkyl that, if necessary, can be substituted one or many times with fluorine atom, (C 3 -C 12 )-cycloalkyl, if necessary substituted (C 6 -C 14 )-aryl, (C 6 -C 14 )-aryl-(C 1 -C 8 )-alkyl substituted in aryl group if necessary, substituted heteroaryl; R 33 means a direct bond; R 34 means bivalent residue among order (C 1 -C 8 )-alkylene, if necessary substituted (C 6 -C 14 )-arylene; R 35 means a direct bond or bivalent (C 1 -C 8 )-alkylene residue; R 36 means a direct bond; e and h mean independently of one another 0 or 1; in all their steroisomeric forms and mixtures and in all ratios, and their physiologically acceptable salt. Also, invention relates to a method for preparing compounds of the formula (I) and pharmaceutical preparation eliciting ability to inhibit adhesion and/or migration of leukocytes and/or VLA-4-receptors. n EFFECT: improved preparing method, valuable medicinal properties of preparation. n 23 cl, 13 tbl, 221 ex |
priorityDate | 1997-11-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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