http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-064477-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_132aa5ddba376cda52c2bedb26765245 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D333-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C317-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-88 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C235-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-13 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-155 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-192 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C255-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D265-02 |
| filingDate | 2007-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_26f2dd55681aa6d7a5e63336bb0ac8d0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cc3e9e1a1baf3b364dd96638c981be40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c40b78c17c12aee6458cc871ea79ec70 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0b38e5ffe4434cc6f792334e8d89715e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fff352f75e7f8398fa18ff9ae8e49559 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a0cd2acbbf99f86b9af1578eb768e9a8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0c7cf8d5a2b230ad1c6f2ae7cb28b428 |
| publicationDate | 2009-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-064477-A1 |
| titleOfInvention | NON-STEROID MODULATORS OF THE PROGESTERONE RECEIVER |
| abstract | Non-steroidal progesterone receptor modulators of general formula 1, the use of progesterone receptor modulators in the preparation of medicaments, and pharmaceutical compositions containing these compounds. The compounds according to the present are suitable for the therapy and prophylaxis of gynecological diseases, such as endometriosis, uterine leiomyoma, dysfunctional hemorrhage and dysmenorrhea, and also for the therapy and prophylaxis of hormone-dependent tumors, and for use in female fertility control and female hormone replacement therapy. Claim 1: Compounds of the general formula 1 characterized in that q is 0 or 1, R1 represents mono or bicyclic C6-12 aryl, a 5-12 membered heteroaryl, C3-10 cycloalkyl or a 3-10 membered heterocyclic radical , which may not be substituted or may be optionally substituted with up to 3 radicals, where each of the substituents independently has one of the following meanings: C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, partial C1-6 alkyl or completely fluorinated, C1-6 alkoxy partially or completely fluorinated, C1-6 alkoxy-C1-6 alkyl, C1-6 alkoxy-C1-6 alkoxy, (CH2) p-C3-10 cycloalkyl, (CH2) p-heterocycloalkyl, (CH2) pCN, (CH2) pHal, (CH2) pNO2, (CH2) C6-12 p-aryl optionally substituted with Z, (CH2) p-heteroaryl optionally substituted with Z, - (CH2) pPO3 (Rb) 2, - (CH2) pNRcRd, - (CH2) pNReCORb, - (CH2) pNReCSRb, - (CH2) pNReS (O) Rb, - (CH2) pNReS (O) 2Rb, - (CH2) pNReCONRcRd, - (CH2) pNReCOORb, - (CH2) pNReC (NH) nRcRd, - (CH2) pNReCSNRcRd, - (CH 2) pNReS (O) RcRd, - (CH2) pNReS (O) 2NRcRd, - (CH2) pCORb, - (CH2) pCSRb, - (CH2) pS (O) Rb, - (CH2) pS (O) (NH ) Rb, - (CH2) pS (O) 2Rb, - (CH2) pS (O) 2NRcRd, - (CH2) pSO2ORb, - (CH2) pCO2Rb, - (CH2) pCONRcRd, - (CH2) pCSNRcRd, - (CH2 ) pORb, (CH2) pSRb, - (CH2) pCRb (OH) -Rb, - (CH2) pC = NORb, -O- (CH2) nO-, -O- (CH2) n-CH2-, -O- CH = CH- or - (CH2) n + 2-, where n is 1 or 2, and the rest of the oxygen and / or carbon atoms are attached to the directly adjacent ring carbon atoms, and p is 0.1 , 2, 3, 4, 5 or 6, and Z represents cyano, halogen, nitro, - (CH2) pORb, - (CH2) pS (O) 2Rb, -C (O) Rb, CO2Rb, -O-Rb, -S-Rb, SO2NRcRd, - C (O) NRcRd, -OC (O) -NRcRd, -C = NORb, -NRcRd, partial or fully fluorinated C1-6 alkyl, or partially or completely fluorinated C1-6 alkoxy, Rb represents hydrogen or C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl, C6-12 aryl or partially or fully fluorinated C1-3 alkyl, Rc and Rd independently represent hydrogen, optionally substituted C1-6 alkyl with W, C2-8 alkenyl, alkyl C2-8 nyl, C3-10 cycloalkyl, C6-12 aryl, a 5- to 12-membered heteroaryl radical, C (O) Rb or a hydroxyl group, and W represents -NRfRg, where Rf represents hydrogen or C1-3 alkyl and Rg represents hydrogen or C1-3 alkyl, or Rf and Rg, together with the nitrogen, form a ring of between 3 and 7 members, which is optionally extended with O, S or NRh, where Rh represents hydrogen, C1-3 alkyl , C1-3 alkanoyl, C1-3 alkylsulfonyl, or C1-3 alkoxycarbonyl, where when Rc is a hydroxyl group, Rd can only be hydrogen, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl or C6-12 aryl, and vice versa, and also Re represents hydrogen, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl or C6-12 aryl, R2 represents mono or bicyclic C6-12 aryl, or a 5- to 12-membered heteroaryl radical, which is not substituted or can optionally be substituted with up to 3 of the radicals mentioned for R1, R3 has the meanings indicated for R2 , or represents one of the following groups A or B: A: Ring-6 / ring-6 union systems with the basal structures in position 5, 6, 7 or 8, B: Ring-6 / ring-5 systems : union with the basal structures at position 4, 5, 6 or 7 where R4 represents hydrogen or C1-4 alkyl, or partially or completely fluorinated C1-4 alkyl, R5a and R5b independently represent hydrogen, C1-4 alkyl or C1 alkyl -4 partially or completely fluorinated, or together with the carbon atom of the ring, form a ring of 3 to 6 members, and also X represents oxygen or two hydrogen atoms, Y represents - (CH2) m-, -C: :: C- or -CH = CH-, and m is 0 or 1, and its salts acceptable for pharmaceutical use. |
| priorityDate | 2006-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 48.