http://rdf.ncbi.nlm.nih.gov/pubchem/patent/HU-0201539-A2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_7a69996870471830a05654231bec9655 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-75 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-47 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-215 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-72 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4523 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-445 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-335 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4025 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C69-66 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-47 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 |
| filingDate | 2000-05-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_97a6a2c62b49f6949bb3b9fa512f18ff http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5670a25b975c3688db57ee967adcd1d8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e57374a46cc08975a47dbec2caad3190 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_44403f496fe06fca9e0aa2882e8003bd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ce73fc9f717ad8cac46f589fc07b2248 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_272f8f9c4016ab9c3975b993833ee912 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_07a24560e2fdba3871679b8405ae197c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4b0f5af56eaceee674c8f2c4e9c65d46 |
| publicationDate | 2002-08-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | HU-0201539-A2 |
| titleOfInvention | Carboxylic acid derivatives that inhibit the binding of integrins to their receptors |
| abstract | Carboxylic acid derivatives (I) are new. Carboxylic acid derivatives of formula (I) and their salts, esters, carbamates, aminals, amides, optical isomers and prodrugs are new. [Image] Y' : CO, N, CR 1>, CR 2>R 3>, NR 5>, CH, O or S; q : 3-10; A : O, S, CR 1> 6>R 1> 7> or NR 6>; E : CH 2, O, S or NR 7>; J : O, S or NR 8>; T : CO or (CH 2) b; b : 0-3; M : CR 9>R 1> 0> or (CH 2) u; u : 0-3; L : O, NR 1> 1>, S or (CH 2) n; n : 0 - 1; X : CO 2B', PO 3H 2, SO 3H, SO 2NH 2, SO 2NHCOR 1> 2>, OPO 3H 2, C(O)NHC(O)R 1> 3>, C(O)NHSO 2R 1> 4>, OH, tetrazolyl or H; W : C, CR 1> 5> or N; and B', R 1>-R 1> 7>H, halo, OH, alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, alkynoxy, thioalkoxy, hydroxyalkyl, aliphatic acyl, CF 3, NO 2, amino, CN, COOH, N(1-3C alkyl)-C(O)-1-3C alkyl, NHC(O)N(1-3C alkyl)C(O)NH-1-3C alkyl, NHC(O)NH(1-6C alkyl), alkylamino, alkenylamino, di(1-3C amino) (sic), CO 2-1-3C alkyl, C(O)NH-1-3C alkyl, C(O)N(1-3C alkyl) 2, CH=NOH, PO 3H 2, OPO 3H 2, haloalkyl, alkoxyalkoxy, carboxaldehyde, carboxamide, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkylalkyl, aryl, aroyl, aryloxy, arylamino, biaryl, thioaryl, diarylamino, heterocyclo, alkaryl, aralkenyl, aralkyl, alkylheterocyclo, heterocycloalkyl, sulfonyl, SO 2(1-3C alkyl), SO 3-(1-3C alkyl), sulfonamido, carbamate, aryloxyalkyl, COOH or C(O)NHbenzyl (all optionally substituted by at least one electron withdrawing or donating group; or R 9>+R 1> 0>a ring; provided that when L : NR 1> 1>; then R 4>+R 1> 1> may : a ring; and when A : NR 6>; and at least one of Y : CR 1>; then R 1>+R 6>a ring; provided that when A : CR 1> 6>R 1> 7>; then E : other than NR 7>; lower : 1-6C; alkyl groups : 1-12C; cycloalkyl groups : 3-10C; heterocyclic groups : 3-10 membered; and aryl or aromatic groups : 6-12C. ACTIVITY : Anti-inflammatory; Antiallergy; Respiratory; Anticancer; Antidiabetic. MECHANISM OF ACTION : Selective inhibitors of alpha 4beta 1 integrin binding. (3S)-3-((((1-((2-Chlorophenyl)methyl)-4-ethyl-2-oxo-1,2-dihydro-3-pyridinyl)amino)carbonyl)amino)-3-(4-methylphenyl)propanoic acid (Ib) had an IC 5 0 of 10 nM for coupling of a 26-amino acid peptide containing the CSI sequence of fibronectin with an N-terminal Cys ( CDELPQLVTLPHPNLHGPEILDVPST) to maleimide activated ovalbumin. |
| priorityDate | 1999-05-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 948.