Processing

Please wait...

Settings

Settings

Goto Application

1. WO2007096647 - DIARYL COMPOUNDS AS NON-STEROIDAL INHIBITORS OF 17-BETA HYDROXYSTEROID DEHYDROGENASE AND/OR STEROID SULPHATASE FOR THE TREATMENT OF OESTROGEN-RELATED DISEASES SUCH AS HORMONE DEPENDENT BREAST CANCER

Publication Number WO/2007/096647
Publication Date 30.08.2007
International Application No. PCT/GB2007/000655
International Filing Date 26.02.2007
IPC
C07D 213/75 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
72Nitrogen atoms
75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07C 49/757 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
49Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
587Unsaturated compounds containing a keto group being part of a ring
757containing -CHO groups
C07D 231/54 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
54condensed with carbocyclic rings or ring systems
C07D 213/40 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
213Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02having three double bonds between ring members or between ring members and non-ring members
04having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
24with substituted hydrocarbon radicals attached to ring carbon atoms
36Radicals substituted by singly-bound nitrogen atoms
40Acylated substituent nitrogen atom
C07D 231/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
12with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 261/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
261Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
02not condensed with other rings
06having two or more double bonds between ring members or between ring members and non-ring members
08with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
CPC
C07C 235/74
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
70having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
72with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
74of a saturated carbon skeleton
C07C 235/78
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
70having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
72with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
76of an unsaturated carbon skeleton
78the carbon skeleton containing rings
C07C 235/84
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
70having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
84with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
C07C 255/40
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
255Carboxylic acid nitriles
01having cyano groups bound to acyclic carbon atoms
32having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
40the carbon skeleton being further substituted by doubly-bound oxygen atoms
C07C 2602/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2602Systems containing two condensed rings
02the rings having only two atoms in common
04One of the condensed rings being a six-membered aromatic ring
08the other ring being five-membered, e.g. indane
C07C 2602/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2602Systems containing two condensed rings
02the rings having only two atoms in common
04One of the condensed rings being a six-membered aromatic ring
10the other ring being six-membered, e.g. tetraline
Applicants
  • STERIX LIMITED [GB]/[GB] (AllExceptUS)
  • VICKER, Nigel [GB]/[GB] (UsOnly)
  • ALLAN, Gillian, Margaret [GB]/[GB] (UsOnly)
  • LAWRENCE, Harshani, Rithma, Ruchiranani [GB]/[GB] (UsOnly)
  • DAY, Joanna, Mary [GB]/[GB] (UsOnly)
  • PUROHIT, Atul [GB]/[GB] (UsOnly)
  • REED, Michael, John [GB]/[GB] (UsOnly)
  • POTTER, Barry, Victor, Lloyd [GB]/[GB] (UsOnly)
Inventors
  • VICKER, Nigel
  • ALLAN, Gillian, Margaret
  • LAWRENCE, Harshani, Rithma, Ruchiranani
  • DAY, Joanna, Mary
  • PUROHIT, Atul
  • REED, Michael, John
  • POTTER, Barry, Victor, Lloyd
Agents
  • ALCOCK, David
Priority Data
0603894.727.02.2006GB
0615464.503.08.2006GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) DIARYL COMPOUNDS AS NON-STEROIDAL INHIBITORS OF 17-BETA HYDROXYSTEROID DEHYDROGENASE AND/OR STEROID SULPHATASE FOR THE TREATMENT OF OESTROGEN-RELATED DISEASES SUCH AS HORMONE DEPENDENT BREAST CANCER
(FR) COMPOSÉ
Abstract
(EN)
There is provided a compound of Formula (I): wherein R3, R4, R5, R6, R7, R9, and R10, are independently selected from -H, -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO2), and halogens; wherein ring A is optionally further substituted wherein X is a bond or a linker group wherein (A) (i) R9 is selected from alkyl and halogen groups; and (ii) R10 is selected from -OH, oxyhydrocarbyl and -OSO2NR1R2; wherein R1 and R2 are independently selected from H and hydrocarbyl or (B) at least one of R3, R4, R5, R6 and R7 is the group -C(=0)-CR11 R12-R8 wherein R8 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkylheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group (vii) =N-O-alkyl or =N-O-H group (viii) branched alkenyl (ix) alkyl-alcohol group or alkenyl-alcohol group (x) amide or alkylamide wherein (a) the alkyl of the alkylamide is -CH2- or - CH2CH2-, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of alkylheterocycle group, alkenylheterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) -CHO, or together with another of R3, R4, R5, R6 and R7 the enol tautomer thereof wherein R11 and R12 are independently selected from H and hydrocarbyl; or (C) at least one of R3, R4, R5, R6 and R7 together with another of R3, R4, R5, R6 and R7 forms a ring containing -C(=O)-; or (D) at least one of R3, R4, R5, R6 and R7 is selected from alkylheterocycle group, alkenylheterocycle group, alkylheteroaryl group, alkenylheteroaryl group, and heteroaryl groups or (E) at least one of R3, R4, R5, R6 and R7 is selected from -CN, -C(R13)=N-O-alkyl group, - C(R14)=N-O-H group, optionally substituted pyrazole, optionally substituted thiazole, optionally substituted oxazole, optionally substituted isoxazole, optionally substituted pyridine, and optionally substituted pyrimidine, or together with another of R3, R4, R5, R6 and R7 forms a nitrogen containing ring; wherein R13 and R14 are independently selected from H and hydrocarbyl.
(FR)
Cette invention concerne un composé représenté par la formule (I) dans laquelle: R3, R4, R5, R6, R7, R9, et R10 sont indépendamment sélectionnés parmi des groupes -H, -OH, hydrocarbyle, des groupes oxyhydrocarbyle, cyano (-CN), nitro (-NO2), et des halogènes; le noyau A est éventuellement substitué; X représente une liaison ou un groupe de liaison; (A) (i) R9 est sélectionné parmi des groupes alkyle et halogène et (ii) R10 est sélectionné parmi -OH, oxyhydrocarbyle et -OSO2NR1R2, R1 et R2 étant indépendamment sélectionnés parmi H et hydrocarbyle; ou (B) au moins un des éléments R3, R4, R5, R6 et R7 représente le groupe -C(=O)-CR11 R12-R8, R8 étant sélectionné parmi: (i) un groupe alkyloxyalkyle; (ii) un groupe nitrile; (iii) un groupe alkylaryle, le groupe aryle étant substitué par un groupe différent d'un groupe C1-10; (iv) un groupe alcénylaryle, le groupe aryle étant substitué; (v) un groupe alkylhétéroaryle, quand le groupe hétéroaryle comprend uniquement C et N dans le noyau, le groupe aryle étant substitué par un groupe différent d'un groupe méthyle; (vi) un groupe alcénylhétéroaryle; (vii) un groupe =N-O-alkyle ou =N-O-H; (viii) un alcényle ramifié; (ix) un groupe alcool d'alkyle ou un groupe alcool d'alcényle; (x) un amide ou un alkylamide, (a) l'alkyle de l'alkylamide représentant -CH2- ou -CH2CH2-, (b) l'amide étant disubstitué et/ou (c) l'amide étant substitué par un groupe alkylhétérocycle et/ou un groupe alcénylhétérocycle et/ou un groupe alkylhétéroaryle et/ou un groupe alcénylhétéroaryle et/ou un groupe hétéroaryle et/ou un groupe alkylamine et/ou un groupe alkyloxyalkyle et/ou un groupe alkylaryle et/ou un groupe alkyle linéaire ou ramifié; (xi) -CHO, ou conjointement avec un autre élément R3, R4, R5, R6 ou R7 le tautomère énol de celui-ci, R11 et R12 étant indépendamment sélectionnés parmi H et hydrocarbyle; ou (C) au moins un des éléments R3, R4, R5, R6 ou R7 conjointement avec un autre élément R3, R4, R5, R6 ou R7 forme un noyau contenant -C(=O)-; ou (D) au moins un des éléments R3, R4, R5, R6 ou R7 est sélectionné parmi un groupe alkylhétérocycle, un groupe alcénylhétérocycle, un groupe alkylhétéroaryle, un groupe alcénylhétéroaryle, et des groupes hétéroaryle; ou (E) au moins un des éléments R3, R4, R5, R6 ou R7 est sélectionné parmi -CN, un groupe -C(R13)=N-O-alkyle, un groupe -C(R14)=N-O-H, pyrazole éventuellement substitué, thiazole éventuellement substitué, oxazole éventuellement substitué, isoxazole éventuellement substitué, pyridine éventuellement substituée, et pyrimidine éventuellement substituée, ou conjointement avec un autre élément R3, R4, R5, R6 ou R7 forme un noyau contenant l'élément azote, R13 et R14 étant indépendamment sélectionnés parmi H et hydrocarbyle.
Also published as
Latest bibliographic data on file with the International Bureau