http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-029633-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_24e76490bed88751680a5fef9bc73892 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a4b14e936224599e9ceef6151c235adf |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P5-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-404 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-00 |
| filingDate | 2000-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2003-07-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-029633-A1 |
| titleOfInvention | DERIVATIVES OF OXINDOL, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM AND THE USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT |
| abstract | An indole derivative selected from the group consisting of a 1,3-dihydro-indole-2-thione derivative, a 1,3-dihydro-indole-2-ylidenamide derivative and a 2-methylene-2,3-dihydro- derivative 1H-indole, comprising the formula (1) in which R1 and R2 are independently selected from the group consisting of H, alkyl, substituted alkyl, OH, O (alkyl, O (substituted alkyl), OAc, aryl, aryl optionally substituted, heteroaryl, optionally substituted heteroaryl, alkylaryl, alkylheteroaryl, 1-propynyl or 3-propynyl: or R1 and R2 join to form a ring comprising one of the following: -CH2 (CH2) nCH2-; CH2CH2C (CH3) 2CH2 -CH2-; O (CH2) mCH2-; O (CH2) pO-; -CH2CH2OCH2CH2-, -CH2CH2N (H) CH2CH2- or CH2CH2N (alkyl CH2CH2-; m is an integer from 1 to 4; n is an integer of 1 to 5; p is an integer from 1 to 4; or R1 and R2 together comprise a double bond with one of the following: C (CH3) 2; C (cycloalkyl), O, C (cycloether). R3 is selected from H, OH, NH2, C1-6 alkyl, substituted C1-6 alkyl, alkenyl or C3-6, alkynyl, substituted alkynyl, and CORA; RA is selected from H, C1-3 alkyl, substituted C1-3 alkyl, C1-3 alkoxy, substituted C1-3 alkoxy, C1-3 aminoalkyl and substituted C1-3 aminoalkyl; R4 is selected from H, halogen, CN, NH2, C1-6 alkyl substituted C1-6 alkyl, C1-6 alkoxy, substituted C1-6 alkoxy, C1-6 aminoalkyl and substituted C1-6 aminoalkyl; R5 is selected from groups a) b) and c); a) a substituted benzene ring containing the substituents X, Y and Z set forth in the formula (2); X is selected from H, halogen, OH, CN, C1-3 alkyl substituted C1-3 alkyl, C1-3 alkoxy, substituted C1-3 alkoxy, C1-3 thioalkyl or substituted C1-3 thioalkyl; S (O) alkyl, S (O) 2alkyl, C1-3 aminoalkyl, substituted C1-3 aminoalkyl, NO2 perfluoroalkyl C1-3, a 5- to 6-membered heterocyclic ring containing 1 to 3 heteroatoms, CONH2, CSNH2, CONHalkyl , CSNHalkyl, CON (alkyl) 2, CSN (alkyl) 2, CORB, OCORB, NRCCORB, RB is selected from H, C1-3 alkyl, substituted C1-3 alkyl, aryl, substituted aryl, C1-3 alkoxy, C1 alkoxy -3 substituted, C1-3 aminoalkyl and substituted C1-3 aminoalkyl; RC is H, C1-3 alkyl or substituted C1-3 alkyl; Y and Z are independently selected from H, halogen, CN, NO2, C1-3 alkoxy C1-3 alkyl and C1-3 thioalkyl; where not all of X, Y and Z are H; b) is a five or six membered heterocyclic ring having 1, 2 or 3 heteroatoms selected from O, S, SO, SO2 and NR6 in its structure and containing one or two independent substituents of the group consisting of H, halogen, CN, NO2 and C1-3 alkyl, C1-3 alkoxy, C1-3 aminoalkyl, CORD and NRECORD, RD is H, C1-3 alkyl, substituted C1-3 alkyl, aryl, substituted aryl, C1-3 alkoxy, C1 alkoxy -3 substituted, C1-3 aminoalkyl or substituted C1-3 aminoalkyl, RE is H, C1-3 alkyl or substituted C1-3 alkyl; R6 is H or C1-3 alkyl; or c) is an indole-4-yl, indole-7-yl portion or a benzo-2-thiophene portion, which portion is optionally substituted with between 1 and 3 substituents selected from halogen, lower alkyl, CN, NO2 lower alkoxy and CF3 ; Q1 is S, NR7, or CR8R9; R7 is selected from the group consisting of CN, C1-6 alkyl, substituted C1-6 alkyl, C3-8 cycloalkyl, substituted C3-8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, acyl, substituted acyl, aroyl, substituted aroyl, SO2CF3, OR11 or NR11R12; R8 and R9 are independent substituents selected from the group consisting of H, C1-6 alkyl, substituted C1-6 alkyl, C3-8 cycloalkyl, substituted C3-8 cycloalkyl, aryl, substituted aryl, heterocycle, substituted heterocycle, NO2, CN , and CO2R10, R10 is C1-3 alkyl or CR8R9 is a six-membered ring, as illustrated in the formula structure: (3), R11 and R12 are independently selected from H, C1-6 alkyl, C1-6 alkyl substituted, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl, substituted acyl, aroyl, substituted aroyl and sulfonyl; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and the use thereof for the preparation of a medicament for using these compounds to induce contraception or treat carcinomas and adenocarcinomas related to progesterone. |
| priorityDate | 1999-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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