- Synthetic studies on a nonsteroidal progesterone metabolite: Regioselective N-alkylation of an activated pyrazole
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This paper describes the large-scale synthesis of a progesterone receptor metabolite. The key step in this sequence was the regioselective pyrazole N-alkylation. Georg Thieme Verlag Stuttgart - New York.
- Bradley, Paul A.,De Koning, Pieter D.,Gibson, Karl R.,Lecouturier, Yann C.,MacKenny, Malcolm C.,Morao, Inaki,Poinsard, Cedric,Underwood, Toby J.
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scheme or table
p. 873 - 876
(2010/07/02)
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- OXYALKYLPYRAZOLE COMPOUNDS USEFUL IN THERAPY
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A compound of Formula (IA) or (IB), or a pharmaceutically acceptable salt, solvate (including hydrate) of said compound and salt, or a prodrug of said compound, or a pharmaceutically acceptable salt or solvate of said prodrug, Formula (IA), (IB) wherein t
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Page/Page column 59-60
(2009/01/20)
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- Compounds Useful In Therapy
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Compounds of Formula (I): and pharmaceutically acceptable salts, solvates (including hydrates) of said compounds and salts, or prodrugs of said compound, or pharmaceutically acceptable salts or solvates of said prodrugs, wherein the substituents are as herein defined, are useful in therapy, for example they may be useful for treating progesterone-mediated conditions such as endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
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Page/Page column 20
(2008/06/13)
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- COMPOUNDS USEFUL IN THERAPY
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Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
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Page/Page column 24
(2010/11/27)
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- Compounds useful in therapy
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Compounds of formula (I), [image] or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6 alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
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Page/Page column 24
(2008/06/13)
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