http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2601029-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_095fc4a13daf2773d72648d379b28b7d http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_da64fe2e174a6fb670360e7d91fedc7b |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12N9-90 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K7-645 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12Y502-01008 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-13 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K7-64 |
| filingDate | 2012-08-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2017-02-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2c68694a9b1c4f60b0e6033455385c9e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_19dbeb4e634c46c68eb8cae504699c0d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_295e907dd59ac9648eb9d4d5c817d6fa http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dcac0dfef469723c66a8b5fb4b5c4d6d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_35cae49e159529e69d317adb0326f809 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f082cf72e3107724107de0269b89d1fb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_48dafac2257fce4d4e63e3f6a0a6e7a2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1ec39ef0a8dfdb404d2a80bfbb0cad39 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_94affe0350663f28cfaebde9548aa4b4 |
| publicationDate | 2017-02-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2601029-T3 |
| titleOfInvention | Cyclosporine derivative |
| abstract | Compound of formula 1 ** Formula ** where A is an amino acid of the following formula II, ** Formula ** where the bonds, ending in wavy lines represent links to units B and K and R9 is a group of the following formula III, and ** Formula ** in which R8 is a group of the following formula IV, or ** Formula ** in which R8 is a group of the following formula V, or ** Formula ** in the that R8 is a group of the following formula VI, or ** Formula ** in which R8 is a group of the following formula VII, or ** Formula ** where R8 is a group of the following formula VIII, in which the residues of L-R2 and R3 can be attached to the same or different phenyl rings, or ** Formula ** where R8 is a group of the following formula IX, and where the residues of L-R2 and R3 can be attached to the same or different rings Q2 or Q3, or ** Formula ** where R8 is a group of the following formula X, and in which the residues of L-R2 and R3 can be attached to the same or different rings Q2 or Q3, or ** Formula ** where R8 is a group of the following formula XI, and in which the residues of L-R2 and R3 can be attached to the same or different rings Q2 or Q3, or ** Formula ** where R8 is a group of the following formula XII, and in which the residues of L-R2 and R3 may be attached to the same or different phenyl rings, or ** Formula ** in which R8 is a group of the following formula XIII, ** Formula ** where the group of formula II covalently binds to the alpha-amino acid B in formula I through its CO by forming an amide bond and N-Ro in the formula II is covalently linked to a carboxy group of K by forming an amide bond, in which B is an amino acid, selected from the following group: alpha-aminobutyric acid; to the girl; threonine; valine norvaline; and alpha-aminobutyric acid, alanine, threonine, valine or norvaline molecules modified with a hydroxy group on the side chain; C represents sarcosine; D is an amino acid, selected from the following group: leucine; N-methylleucine; valine gamma-hydroxy-N-methylleucine; and gamma-hydroxyleucine; E is an amino acid, selected from the following group: valine; norvaline; and a modified valine or norvaline in which a carbon atom of the side chain is substituted by a hydroxy group; F is an amino acid, selected from the following group: leucine; N-methylleucine; gamma-hydroxy-N-methylleucine; and gamma-hydroxyleucine; G is equal to alpha-aminobutyric acid or alanine; H is equal to D-alanine or D-serine; I and J are amino acids, independently selected from each other from the following group: leucine; N-methylleucine; gamma-hydroxy-N-methylleucine; and gamma-hydroxyleucine; K is equal to N-methylvaline or valine; where amino acids B to K are linked together by forming amide bonds; where the symbols and indices used have the following meanings: X represents O, S, or N-R1; Y represents O, S, N-R1, -CH2- or -CH2CH2-; A as used in formulas IX, X, XI and represents CH or N; L represents a link, -CH2-, -CH2CH2-, -CH2CH2CH2-, -CH2CH2CH2CH2-, -CH> = CH-, -CH> = CHCH2-, - CH2CH> = CH-, -CH2CH2CH> = CH-, - CH2CH> = CHCH2-, -CH> = CHCH2CH2-, -OCH2-, -OCH2CH2-, -OCH2CH2CH2-, - OCH2CH> = CH-, -CONH-, -CONHCH2 or -CONHCH2CH2-, -CONHCH2CH2OCH2CH2-2 - CONHCHCH2-2 ; Q1 represents, together with the two condensed ring atoms, an aromatic or heteroaromatic ring from the group of benzene, pyridine, pyrimidine, pyridazine, pyrazine, triazine, thiophene, furan, pyrrole, thiazole, isothiazole, oxazole, isoxazole, imidazole or pyrazole ; Q2 represents, together with the two atoms in the condensed ring, an aromatic or heteroaromatic ring from the group of benzene, pyridine, pyrimidine, pyridazine, pyrazine, triazine, thiophene, furan, pyrrole, thiazole, isothiazole, oxazole, isoxazole, imidazole, pyrazole , thiadiazole, oxadiazole or triazole; Q3 defines the six-member ring in which it is found; Ro represents H or CH3; R1 represents H, (C1-C4) -alkyl or benzyl, which may also be substituted by a -COOH group; R2 represents a polar deprotonable group Ps selected from the group consisting of: a) -COOH, -SO3H, -CONH2, -CONHNH2, -SO2NH2, -PO3H2, -PO (OH) (NH2), -CO (NHOH), - CO (-NH (O-C1-C4-alkyl)), -CSNH2, -NHCONH2, -N (OH) CONH2, -NHCO (NHOH) -, -NHCSNH2, -CSNHNH2; b) ** Formula ** and R> = - (C1-C4-alkyl), -O (C1-C4-alkyl), -NH (C1-C4-alkyl), -NH (C1-C4-alkenyl), (substituted) aryl, (substituted) O-aryl, (substituted) NH-aryl, -CF3 and other fluorinated groups (C1-C4-alkyl); c) ** Formula ** and R> = (C1-C4-alkyl), (subsituted) aryl, -CF3 and other fluorinated groups (C1-C4-alkyl) and; e) ** Formula ** and R> = - (C1-C4-alkyl), -O (C1-C4-alkyl), -NH (C1-C4-alkyl), -NH (C1-C4-alkenyl), (substituted) aryl, (substituted) O-aryl, (substituted) NH-aryl, -CF3 and other fluorinated groups (C1-C4-alkyl; f) ** Formula ** where R> = H, - (C1-C4 -alkyl) -CF3 and other fluorinated groups 10 (C1-C4-alkyl). g) -OH and -SH, provided that L represents a covalent single bond, and that -OH or -SH can only be a substituent on a ring Q1, Q2 or Q3 and is at the same time linked to a carbon atom that is adjacent to a nitrogen atom or a group Ps', which can be converted under physiological conditions to Ps, or a protonable polar group Pb selected from the group consisting of a) ** Formula ** where Ra, Rb and Rc represent H and - (C1-C4-alkyl), Ra and Rb can be together - (CH2CH2) - or - (CH2CH2CH2) -and Rb and Rc can be, together with the nitrogen atom pyrrolidine, piperidine or morpholine; b) ** Formula ** where Ra, Rb, Rc and Rd represent H and - (C1-C4-alkyl), Ra and Rb, Ra and Rd, as well as Rb and Rd can be together - (CH2CH2) - or - (CH2CH2CH2) - and Rb and Rc can be together with the nitrogen atom pyrrolidine, piperidine or morpholine; c) an amino group selected from -NH2, (C1-C6) alkyl-amino, (C1-C6) dialkyl-amino, pyrrolidine, piperidine, morpholine or piperazine, which may be substituted in the 4-coN (C1-C6) position alkyl, - (C1-C6) alkanoyl, benzyl, benzoyl or phenyl, wherein these substituents optionally carry a -COOH group or a Pb 'group, which can be converted under physiological conditions to Pb; R3 represents H, (C1-C6) -alkyl, (C1-C6) -alkoxy, -OH, (C1-C6) -alkylthio, (C1-C6) alkylsulfonyl, -SH, -CF3, - COOH, -COO ( (C1-C6) alkyl)), -CONH2, -CO-NH ((C1-C6) alkyl-amino), -CON ((C1-C6) alkyl) 2, nitro, halogen, cyano, amino, (C1- C6) alkyl-amino or (C1-C6) dialkyl-amino; or R3 exists in the form of a pair of free electrons, if it would bind to a heteroatom of rings Q1, Q2 or Q3; R4 and R5 independently represent each other H, (C1-C6) -alkyl, (C1-C6) -alkoxy, -CF3, halogen or can form together -OCH2O- or -OCH2CH2O-, if R4 and R5 are attached to the ring in ortho position with each other; R7 represents H, -OH, -OCOOR12, -OCOR13, -OCONR14R15, -O-tetrahydropyran-2-yl), -O- (tetrahydrofuran-2-yl), -O-CHR16-OR17 or -SiR18R19R20; R10 and R11 independently represent each other H, (C1-C6) -alkyl, -CF3 or halogen; or R10 and R11 together form -CH2CH2-, -CH2CH2CH2-, -CH2CH2CH2CH2- or -CH2CH2CH2CH2CH2-; R12 represents (C1-C6) -alkyl, benzyl or phenyl, in which the alkyl group is optionally substituted by fluorine or chlorine and benzyl and phenyl are optionally substituted by one or more substituents selected from the group of (C1-C6) -alkyl, (C1-C6) -alkoxy, -CF3, cyano, nitro or halogen; R13 represents H or R12; R14 and R15 independently represent each other H, (C1-C6) -alkyl, benzyl or phenyl, in which, if necessary, benzyl and phenyl may be substituted by one or more substituents selected from 5 from the group of (C1 -C6) -alkyl, (C1-C6) -alkoxy, -CF3, cyano, nitro or halogen; R16 represents H or (C1-C6) -alkyl; R17 represents (C1-C6) -alkyl, benzyl or phenyl R18, R19 and R20 independently represent each other (C1-C6) -alkyl, benzyl or phenyl; or a pharmaceutically acceptable salt, as well as a tautomeric, enantiomeric or other stereoisomeric form thereof. |
| priorityDate | 2011-08-30-04:00^^<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: 138.