http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-046321-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D255-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-33 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-395 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D255-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D245-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D281-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D273-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D281-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D255-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D255-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D273-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D245-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-08 |
| filingDate | 2004-11-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-11-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-046321-A1 |
| titleOfInvention | COMPOUNDS OF MACROCICLIC LACTORS, PREPARATION PROCEDURES AND PHARMACEUTICAL COMPOSITIONS. |
| abstract | This refers to its preparation, and pharmaceutical compositions that comprise them. Claim 1: A compound of the formula (1), wherein: R1 is CH (Re) C (= O) N (Ra) Rb or (CH2) kN (Rc) Rd, wherein K is 0, 1 or 2 ; Ra and Rb, independently, are hydrogen or an optionally substituted C 1-8 alkyl group, C 3-7 cycloalkyl, C 3-7 cycloalkyl-C 1-4 alkyl, aryl, C 1-4 arylalkyl, heteroaryl or C 1-4 heteroarylalkyl; Rc and Rd, independently, are hydrogen or an optionally substituted C 1-8 alkyl group, C 3-7 cycloalkyl, C 3-7 cycloalkyl-C 1-4 alkyl, aryl, C 1-4 arylalkyl, heteroaryl, C 1-4 heteroarylalkyl, chroman-4 -yl, isochroman-4-yl, thiochroman-4-yl, isothiochroman-4-yl, 1,1-dioxo-1l * 6 * -thiochroman-4-yl, 2,2-dioxo-2l * 6 * -isothiochroman -4-yl, 1,2,3,4-tetrahydro-quinolin-4-yl, 1,2,3,4-tetrahydro-isoquinolin-4-yl, 1,2,3,4-tetrahydro-naphthalen-1 -yl, 1,1-dioxo-1,2,3,4-tetrahydro-1l * 6 * -benzo [e] [1,2] thiazin-4-yl, 2,2-dioxo-1,2,3 , 4-tetrahydro-2l * 6 * benzo [c] [1,2] thiazin-4-yl, 1,1-dioxo-3,4-dihydro-1H-1l * 6 * [c] [1,2] oxatiin-4-yl, 2,2-dioxo-3,4-dihydro-2H-2l * 6 * [e] [1,2] oxatiin-4-yl, 2,3,4,5-tetrahydro-benzo [ b] oxepin-5-yl or 1,2,3,4-tetrahydro-benzo [c] oxepin-5-yl, or Ra and Rb, or Rc and Rd together with the nitrogen atom to which they are attached, form a optionally substituted pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or piperazinyl group; and Re is optionally substituted C1-8 alkyl, C1-4 alkoxy-C1-4 alkyl, C3-7 cycloalkyl or C3-7 cycloalkyl-C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen, C1-6 alkyl or a C1-6OC alkyl group (= O) NH, C3-7OC cycloalkyl (= O) NH, C3-7 cycloalkyl-C1-4OC alkyl (= O) NH, C1-4OC arylalkyl (= O) NH, C1-4OC heteroarylalkyl (= O) NH, C1-4OC alkyl (= O) NH, C3-7OC cycloalkyl (= O) NH, arylOC (= O) NH, C1-4OC arylalkyl (= O ) NH, heteroarylOC (= O) NH, or heteroarylalkylC 1-4OC (= O) NH; U is a link CF2, CF2CF2, CHF, CHFCHF, cycloprop-1,2-ylene, C1-3 alkyleneoxy, C1-8 alkylene, NRg or an aromatic or heteroaromatic ring, the ring of which is optionally substituted with halogen, C1-4 alkoxy , hydroxy or C1-4 alkyl, wherein Z and V are in the ortho or meta position with respect to each other, where Rg is hydrogen, C1-8 alkyl or C3-7 cycloalkyl; V is CH = CH, cycloprop-1,2-ylene, CH2CH (OH), CH (OH) CH2 or CRhRhCRhRh, wherein each Rh, independently, is hydrogen, fluorine or C1-4 alkyl; W is C1-6 alkylene, O, S, S (= O) 2, C (= O), C (= O) O, OC (= O), C (Rf) C (= O), C (= O) NRf or NRf, wherein Rf is hydrogen or C1-4 alkyl; X is an optionally substituted C1-4 alkanylidene group, C1-4 alkylene, C3-7 cycloalkylene, piperidin-diyl, pyrrolidin-diyl, benzothiazol-4,6-diyl, benzoxazol-4,6-diyl, 1H-benzotriazol-4 , 6-diyl, imidazol [1,2-a] pyridin-6,8-diyl, benzo- [1,2,5] oxadiazol-4,6-diyl, benzo [1,2,5] thiadiazol-4, 6-diyl, 1H-indazol-1,6-diyl, 1H-benzimidazol-4,6-diyl or 1H-indazol-1,6-diyl or an optionally substituted aromatic or heteroaromatic ring, where Y and C (= O ) NR2 are in the target position with respect to each other; Y is a bond, O, S (= O) 2, S (= O) 2NRg, N (Rg) S (= O) 2, NRg, C (Rg) OH, C (= O) NRg, N (Rg ) C (= O), C (= O) N (Rg) O or ON (Rg) C (= O), where Rg is hydrogen, C1-8 alkyl or C3-7 cycloalkyl; Z is O, CH2, CF2, CHF, cycloprop-1,2-ylene or a bond; and n is 0 to 5, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in the form of a free base or in the form of an acid addition salt. |
| priorityDate | 2003-11-05-04:00^^<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: 42.