http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0785943-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_21f23f0c43864bd4d632cd6023e4a66a |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2602-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2601-16 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C255-31 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C265-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J73-005 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C265-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J41-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J73-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C255-31 |
filingDate | 1995-10-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_64a5847c3aa6f6e75a5948eb17973768 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7d2b6ee018247efa2bc47381bd73aa07 |
publicationDate | 1997-07-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | EP-0785943-A1 |
titleOfInvention | Synthesis of 6-azaandrostenones |
abstract | A process for providing novel compounds of formula (I), that are useful as 6-azaadrostenone testosterone 5-alpha-reductase inhibitors, from commercially available compounds of formula (II) wherein, R?1 and R2¿ represent: i) indepedently H or alkyl and the bond between carbons 1 and 2 is a single bond or a double bond, or ii) taken together is a -CH¿2?- group to form a cyclopropane ring, and the bond between the carbons bearing 1 and 2 is a single bond, provided however, in compounds of formula (II); R?1 and R2¿ represent independently H or alkyl or taken together are a -CH¿2?- group to form a cyclopropane ring; R?3¿ represents H, -Alk1- H optionally substituted with one or more halogen atoms, cycloalkyl, cycloalkyl-alkyl, halogen, -(Alk1)n-CO2H, -(Alk1)n-CO2R?8, -(Alk1)¿n-Ar?1, -(Alk1)¿n-CONR?9R10, -(Alk1)¿n-NR?9R10, -(Alk1)¿n-S(O)rR?8, -(Alk1)¿n-CN, -(Alk1)-OH, or -(Alk1)n-OR8; wherein: Alk1 represents alkylenene, alkenylene or alkynylene; n represents 0 or 1; r represents 0, 1 or 2; R8 represents -Alk1-H, -(Alk1)n-Ar1 opr cycloalkyl; wherein: -Ar1 represents an aryl or heteraryl group of 6 to 14 atoms; R?9 and R10¿ represent independently H, -Alk1-H or cycloalkyl; Y represents H or hydroxy; Z represents, -(Alk2)n-COR?11, -(Alk2)¿n-CO2R?11, -(Alk2)¿n-CO-thiopyridinyl or -(Alk2)n-CONR12R13, wherein: Alk2 represents, (C¿2?-12) alkylene, (C2-12) alkenylene or (C2-12) alkynylene; R?11¿ represents H, -Alk1-H, cycloalkyl or adamantyl; R?12 and R13¿ represent, i) independently, H, -Alk2-H, cycloalkyl, alkoxy, adamantyl, -Ar1, -Ar1-alkyl-perhaloalkyl, benzyl, diphenylmethyl, triphenylmethyl or -(Alk1)n-norbornyl; or ii) taken together with the linking nitrogen to form a 4 to 8 atom heterocyclic group (Formula III) wherein: Het represents -O-, -CH2-, -S(O)r-, -NH- or -N(Alk1-H)-; optionally substituted with one or more alkyl groups; R?5 and R6¿ represent H or alkyl; R7 represents hydroxy, alkoxy, halogen or OCOR14, wherein R14 represents H, alkyl, aryl or heteroaryl, and the pharmaceutically acceptable salts and solvates thereof. |
priorityDate | 1994-10-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 259.