HRP20130056T1 - Specifiäśni glukokortikosteroidni spoj s protuupalnim djelovanjem - Google Patents
Specifiäśni glukokortikosteroidni spoj s protuupalnim djelovanjem Download PDFInfo
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- HRP20130056T1 HRP20130056T1 HRP20130056TT HRP20130056T HRP20130056T1 HR P20130056 T1 HRP20130056 T1 HR P20130056T1 HR P20130056T T HRP20130056T T HR P20130056TT HR P20130056 T HRP20130056 T HR P20130056T HR P20130056 T1 HRP20130056 T1 HR P20130056T1
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- Prior art keywords
- methyl
- hydroxy
- diene
- difluoro
- oxoandrosta
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- 150000001875 compounds Chemical class 0.000 title claims 25
- 230000003110 anti-inflammatory effect Effects 0.000 title 1
- 239000003862 glucocorticoid Substances 0.000 title 1
- 239000002253 acid Substances 0.000 claims 18
- -1 4-(diethylamino) sulfonylphenyl Chemical group 0.000 claims 16
- 150000002148 esters Chemical class 0.000 claims 13
- 239000012453 solvate Substances 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- SFHVXKNMCGSLAR-UHFFFAOYSA-N 2,2,3,3-tetramethylcyclopropanecarboxylic acid Chemical compound CC1(C)C(C(O)=O)C1(C)C SFHVXKNMCGSLAR-UHFFFAOYSA-N 0.000 claims 3
- 208000010668 atopic eczema Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 206010027654 Allergic conditions Diseases 0.000 claims 2
- 206010012434 Dermatitis allergic Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical class [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000037062 Polyps Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 206010039083 rhinitis Diseases 0.000 claims 2
- IHFCLFDIMLPWBJ-UHFFFAOYSA-M (2,3-dimethylimidazol-3-ium-1-yl)-(2,2,3,3-tetramethylcyclopropyl)methanone;chloride Chemical group [Cl-].C1=C[N+](C)=C(C)N1C(=O)C1C(C)(C)C1(C)C IHFCLFDIMLPWBJ-UHFFFAOYSA-M 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- 201000009053 Neurodermatitis Diseases 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- KYKAJFCTULSVSH-UHFFFAOYSA-N chloro(fluoro)methane Chemical compound F[C]Cl KYKAJFCTULSVSH-UHFFFAOYSA-N 0.000 claims 1
- 239000006184 cosolvent Substances 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000004981 cycloalkylmethyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- NBVXSUQYWXRMNV-UHFFFAOYSA-N fluoromethane Chemical compound FC NBVXSUQYWXRMNV-UHFFFAOYSA-N 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 239000007789 gas Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 230000007803 itching Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008249 pharmaceutical aerosol Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000003380 propellant Substances 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
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- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
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- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with 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
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Claims (24)
1. Spoj formule (I):
[image]
,
naznačen time što
X predstavlja O ili S;
R1 predstavlja C1-6 alkil, C3-8 cikloalkil, C3-8 cikloalkilmetil ili C3-8 cikloalkenil, od kojih bilo koji izborno može biti supstituiran s jednom ili više metilnih skupina ili atoma halogena, ili R1 predstavlja aril, 4-(dietilamino)sulfonilfenil, 2,6-difluorfenil, 4-metoksifenil, 3-difluormetiltiofenil, 4-cijanofenil, heteroaril, 5-klor-4-metoksitiofen-3-il, 2-izopropil-1,3-tiazol-4-il, 5-trifluormetilfuran-2-il, 5-metilsulfoniltiofen-2-il, 5-metiltiotiofen-2-il ili 5-etilizoksazol-3-il;
R2 predstavlja vodik, metil, koji može biti bilo u konfiguraciji α ili β, ili metilen;
R3 i R4 su isti ili različiti i svaki neovisno predstavlja vodik, halogen ili metilnu skupinu;
a ----- predstavlja jednostruku ili dvostruku vezu;
ili njegova fiziološki prihvatljiva sol ili solvat.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što X predstavlja O.
3. Spoj u skladu s patentnim zahtjevom 1 ili patentni zahtjev 2, naznačen time što R1 predstavlja C3-6 cikloalkilna skupina, izborno supstituirana s jednom ili više metilnih ili klornih skupina.
4. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što R1 predstavlja 2,2,3,3-tetrametilciklopropil.
5. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što R2 predstavlja metil u konfiguraciji α.
6. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što su R3 i R4 oba fluori.
7. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što ----- predstavlja dvostruku vezu.
8. Spoj u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što je
S-Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-3-okso-17α-(2,2,3,3-tetrametilciklopropilkarbonil)oksiandrosta-1,4-dien-17β-karbotiojske kiseline;
S-Cijanometilni ester 17α-(4-[(dietilamino)sulfonil]benzoil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline;
S-Cijanometilni ester 17α-(5-klor-4-metoksitiofen-3-karbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline;
Cijanometilni ester 17α-(cikloheksilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-17α-(2,6-difluorbenzoil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-11β-hidroksi-17α-(4-metoksibenzoil)oksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 17α-(4-cijanobenzoil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 17α-(ciklopentilmetilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-17α-(3,3-dimetilbutanoil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-11β-hidroksi-17α-(2-izopropil-1,3-tiazol-4-karbonil)oksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-3-okso-17α-(kinolin-2-karbonil)oksiandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-3-okso-17α-(5-trifluormetilfuran-2-karbonil)oksiandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-17α-(5-metilsulfoniltiofen-2-karbonil)oksi-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-17α-(5-metiltiotiofen-2-karbonil)oksi-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-17α-(5-etilizoksazol-3-karbonil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 9α-fluor-11β-hidroksi-16β-metil-3-okso-17α-(2,2,3,3-tetrametilciklopropilkarbonil)oksiandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-3-okso-17α-(2,2,3,3-tetrametilciklopropilkarbonil)oksiandrost-4-en-17β-karboksilne kiseline;
Cijanometilni ester 17α-(5-klor-4-metoksitiofen-3-karbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 17α-(2,2-diklor-3,3-dimetilciklopropilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
S-Cijanometilni ester 17α-(2,2-diklor-3,3-dimetilciklopropilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline;
S-Cijanometilni ester 17α-(cikloheksilekarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline;
S-Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-17α-(5-metilsulfoniltiofen-2-karbonil)oksi-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline;
S-Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-3-okso-17α-(5-trifluormetilfuran-2-karbonil)oksiandrosta-1,4-dien-17β-karbotiojske kiseline; ili
S-Cijanometilni ester 6α,9α-difluor-17α-(3-(difluormetiltio)benzoil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline.
9. Spoj u skladu s patentnim zahtjevom 8, naznačen time što je
S-Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-3-okso-17α-(2,2,3,3-tetrametilciklopropilkarbonil)oksiandrosta-1,4-dien-17β-karbotiojske kiseline;
Cijanometilni ester 9α-fluor-11β-hidroksi-16β-metil-3-okso-17α-(2,2,3,3-tetrametilciklopropilkarbonil)oksiandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 17α-(cikloheksilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 17α-(ciklopentilmetilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-17α-(3,3-dimetilbutanoil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
S-Cijanometilni ester 6α,9α-difluor-17α-(3-(difluormetiltio)benzoil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline;
S-Cijanometilni ester 17α-(cikloheksilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline;
Cijanometilni ester 6α,9α-difluor-17α-(5-etilizoksazol-3-karbonil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-17α-(5-metiltiotiofen-2-karbonil)oksi-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
Cijanometilni ester 6α,9α-difluor-11β-hidroksi-17α-(2-izopropil-1,3-tiazol-4-karbonil)oksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline;
S-Cijanometilni ester 17α-(2,2-diklor-3,3-dimetilciklopropilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojske kiseline; ili
Cijanometilni ester 17α-(2,2-diklor-3,3-dimetilciklopropilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline.
10. Spoj u skladu s patentnim zahtjevom 9, naznačen time što je
Cijanometilni ester 17α-(2,2-diklor-3,3-dimetilciklopropilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilne kiseline; ili
S-Cijanometilni ester 6α,9α-difluor-11β-hidroksi-16α-metil-3-okso-17α-(2,2,3,3-tetrametilciklopropilkarbonil)oksiandrosta-1,4-dien-17β-karbotiojske kiseline.
11. Spoj formule (I) u skladu s bilo kojem od patentnih zahtjeva 1 do 10, ili njegov fiziološki prihvatljiv solvat, naznačen time što je namijenjen upotrebi u veterini ili medicini.
12. Spoj formule (I) u skladu s bilo kojem od patentnih zahtjeva 1 do 10, ili njegov fiziološki prihvatljiv solvat, naznačen time što je namijenjen upotrebi u liječenju pacijenata s upalnim i/ili alergijskim stanjima.
13. Spoj formule (I), ili njegov fiziološki prihvatljiv solvat, u skladu s patentnim zahtjevom 12, naznačen time što je namijenjen upotrebi u liječenju pacijenata s ekcemom, psorijazom, alergijskim dermatitisom, neurodermatitisom, svrbežom, reakcijama preosjetljivosti, astmom, rinitisom, polipima u nosu, kroničnom opstruktivnom plućnom bolešću, intersticijskom plućnom bolešću, fibrozom, ulceroznim kolitisom, Crohnovom bolešću, reumatoidnim artritisom i lonjunktivitisom.
14. Spoj formule (I), ili njegov fiziološki prihvatljiv solvat, u skladu s patentnim zahtjevom 13, naznačen time što je namijenjen upotrebi u liječenju pacijenata s alergijskim dermatitisom.
15. Spoj formule (I), ili njegov fiziološki prihvatljiv solvat, u skladu s patentnim zahtjevom 13, naznačen time što je namijenjen upotrebi u liječenju pacijenata s astmom.
16. Spoj formule (I), ili njegov fiziološki prihvatljiv solvat, u skladu s patentnim zahtjevom 13, naznačen time što je namijenjen upotrebi u liječenju pacijenata s rinitisom.
17. Spoj formule (I), ili njegov fiziološki prihvatljiv solvat, u skladu s patentnim zahtjevom 13, naznačen time što je namijenjen upotrebi u liječenju pacijenata s polipima u nosu.
18. Upotreba spoja formule (I) u skladu s bilo kojem od patentnih zahtjeva 1 do 10, ili njegovog fiziološki prihvatljivog solvata, naznačena time što je navedeni spoj namijenjen proizvodnji medikamenta za liječenje upalnih i/ili alergijskih stanja.
19. Farmaceutski pripravak, naznačen time što sadrži spoj formule (I) u skladu s bilo kojem od patentnih zahtjeva 1 do 10, ili njegov fiziološki prihvatljiv solvat, u smjesi, ako je to poželjno, s jednim ili više fiziološki prihvatljivih razrjeđivača ili podloga.
20. Farmaceutska aerosolna formulacija, naznačena time što sadrži spoj formule (I) u skladu s bilo kojem od patentnih zahtjeva 1 do 10, ili njegov fiziološki prihvatljiv solvat, te fluorugljik ili klorfluorugljik koji sadrži vodik kao potisni plin, izborno u kombinaciji sa surfaktantom i/ili suotapalom.
21. Spoj, naznačen time što je
17α-(4-[(Dietilamino)sulfonil]benzoil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojska kiselina;
6α,9α-Difluor-17a-(2,6-difluorbenzoil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
6α,9α-Difluor-11β-hidroksi-17α-(4-metoksibenzoil)oksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
17α-(4-Cijanobenzoil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
6α,9α-Difluor-17α-(3,3-dimetilbutanoil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
6α,9α-Difluor-11β-hidroksi-17a-(2-izopropil-1,3-tiazol-4-karbonil)oksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
6α,9α-Difluor-11β-hidroksi-16α-metil-3-okso-17α-(kinolin-2-karbonil)oksiandrosta-1,4-dien-17β-karboksilna kiselina;
6α,9α-Difluor-11β-hidroksi-16α-metil-3-okso-17α-(5-trifluormetilfuran-2-karbonil)oksiandrosta-1,4-dien-17β-karboksilna kiselina;
6α,9α-Difluor-11β-hidroksi-16α-metil-17α-(5-metilsulfoniltiofen-2-karbonil)oksi-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
6α,9α-Difluor-11β-hidroksi-16α-metil-17α-(5-metiltiotiofen-2-karbonil)oksi-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
6α,9α-Difluor-17α-(5-etilizoksazol-3-karbonil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
17α-(5-Klor-4-metoksitiofen-3-karbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
17α-(2,2-Diklor-3,3-dimetilciklopropilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karboksilna kiselina;
17α-(2,2-Diklor-3,3-dimetilciklopropilkarbonil)oksi-6α,9α-difluor-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojska kiselina;
6α,9α-Difluor-11β-hidroksi-16α-metil-17α-(5-metilsulfoniltiofen-2-karbonil)oksi-3-oksoandrosta-1,4-dien-17β-karbotiojska kiselina;
6α,9α-Difluor-11β-hidroksi-16α-metil-3-okso-17α-(5-trifluormetilfuran-2-karbonil)oksiandrosta-1,4-dien-17β-karbotiojska kiselina; ili
6α,9α-Difluor-17α-(3-(difluormetiltio)benzoil)oksi-11β-hidroksi-16α-metil-3-oksoandrosta-1,4-dien-17β-karbotiojska kiselina.
22. Spoj formule (IV):
[image]
,
naznačen time što je 2,3-dimetil-1-[(2,2,3,3-tetrametilciklopropil)karbonil]-1H-imidazol-3-ijev klorid.
23. Postupak dobivanja spoja formule (II)
[image]
gdje R1 predstavlja 2,2,3,3-tetrametilciklopropil, a R2, R3, R4, X i ----- su definirani kao u bilo kojem od patentnih zahtjeva 1 do 7, naznačen time što se navedeni postupak sastoji u reakciji 1,2-dimetil-1H-imidazolijevog estera 2,2,3,3-tetrametilciklopropankarboksilne kiseline (IV)
[image]
s odgovarajućim 17α-hidroksilnim derivatom formule (III)
[image]
.
24. Postupak u skladu s patentnim zahtjevom 23, naznačen time što X predstavlja O.
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