HRP20211043T1 - Derivati 6,7-dihidro-5h-benzo[7]anulena kao modulatori estrogenskih receptora - Google Patents
Derivati 6,7-dihidro-5h-benzo[7]anulena kao modulatori estrogenskih receptora Download PDFInfo
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- HRP20211043T1 HRP20211043T1 HRP20211043TT HRP20211043T HRP20211043T1 HR P20211043 T1 HRP20211043 T1 HR P20211043T1 HR P20211043T T HRP20211043T T HR P20211043TT HR P20211043 T HRP20211043 T HR P20211043T HR P20211043 T1 HRP20211043 T1 HR P20211043T1
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- DTRRHWQMEXXDFE-UHFFFAOYSA-N 8,9-dihydro-7h-benzo[7]annulene Chemical class C1CCC=CC2=CC=CC=C21 DTRRHWQMEXXDFE-UHFFFAOYSA-N 0.000 title 1
- 239000002834 estrogen receptor modulator Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 125000001153 fluoro group Chemical group F* 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- 239000011593 sulfur Chemical group 0.000 claims 6
- 229910052717 sulfur Chemical group 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229920006395 saturated elastomer Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 206010027476 Metastases Diseases 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 229910052731 fluorine Chemical group 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- BLRPTPMANUNPDV-UHFFFAOYSA-N Silane Chemical group [SiH4] BLRPTPMANUNPDV-UHFFFAOYSA-N 0.000 claims 2
- 125000003368 amide group Chemical group 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 230000009401 metastasis Effects 0.000 claims 2
- 125000004354 sulfur functional group Chemical group 0.000 claims 2
- ORNJMAUSEXCFFI-CGYPVTCASA-N 5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-6-(4-hydroxycyclohexyl)-8,9-dihydro-7H-benzo[7]annulen-2-ol Chemical compound FCCCN1C[C@H](CC1)OC1=CC=C(C=C1)C1=C(CCCC2=C1C=CC(=C2)O)C1CCC(CC1)O ORNJMAUSEXCFFI-CGYPVTCASA-N 0.000 claims 1
- CUVIEOMIPZIETH-MHZLTWQESA-N 5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-6-[4-(trifluoromethoxy)phenyl]-8,9-dihydro-7H-benzo[7]annulen-2-ol Chemical compound FCCCN1C[C@H](CC1)OC1=CC=C(C=C1)C1=C(CCCC2=C1C=CC(=C2)O)C1=CC=C(C=C1)OC(F)(F)F CUVIEOMIPZIETH-MHZLTWQESA-N 0.000 claims 1
- BEMOLRLWONFMRO-NDEPHWFRSA-N 6-(2,3-dihydro-1H-indol-5-yl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulen-2-ol Chemical compound FCCCN1C[C@H](CC1)OC1=CC=C(C=C1)C1=C(CCCC2=C1C=CC(=C2)O)C=1C=C2CCNC2=CC=1 BEMOLRLWONFMRO-NDEPHWFRSA-N 0.000 claims 1
- KISZAGQTIXIVAR-VWLOTQADSA-N 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid Chemical compound ClC1=C(C=CC(=C1)Cl)C1=C(C2=C(CCC1)C=C(C=C2)C(=O)O)C1=CC=C(C=C1)O[C@@H]1CN(CC1)CCCF KISZAGQTIXIVAR-VWLOTQADSA-N 0.000 claims 1
- UBSWKNSSCUADIN-SANMLTNESA-N 6-(2-ethoxypyrimidin-5-yl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulen-2-ol Chemical compound C(C)OC1=NC=C(C=N1)C1=C(C2=C(CCC1)C=C(C=C2)O)C1=CC=C(C=C1)O[C@@H]1CN(CC1)CCCF UBSWKNSSCUADIN-SANMLTNESA-N 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 229910007161 Si(CH3)3 Inorganic materials 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- YICAMVNYUFULBB-MHZLTWQESA-N [5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-6-[4-(trifluoromethoxy)phenyl]-8,9-dihydro-7H-benzo[7]annulen-2-yl] dihydrogen phosphate Chemical compound P(=O)(OC=1C=CC2=C(CCCC(=C2C2=CC=C(C=C2)O[C@@H]2CN(CC2)CCCF)C2=CC=C(C=C2)OC(F)(F)F)C=1)(O)O YICAMVNYUFULBB-MHZLTWQESA-N 0.000 claims 1
- 230000003388 anti-hormonal effect Effects 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 125000004431 deuterium atom Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 230000002357 endometrial effect Effects 0.000 claims 1
- 102000015694 estrogen receptors Human genes 0.000 claims 1
- 108010038795 estrogen receptors Proteins 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000002611 ovarian Effects 0.000 claims 1
- 230000000624 ovulatory effect Effects 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- FFSJPOPLSWBGQY-UHFFFAOYSA-N triazol-4-one Chemical group O=C1C=NN=N1 FFSJPOPLSWBGQY-UHFFFAOYSA-N 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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Claims (14)
1. Spoj s formulom (I):
[image]
naznačen time što:
- R1 i R2 predstavljaju neovisno vodikov atom ili atom deuterija;
- R3 predstavlja vodikov atom , skupinu -COOH, skupinu -OH ili skupinu -OPO(OH)2 ;
- R4 predstavlja vodikov atom ili fluorov atom;
- R5 predstavlja vodikov atom ili skupinu -OH;
- pri čemu:
∘ najmanje jedan od R3 ili R5 se razlikuje od vodikovog atoma;
∘ kada R3 predstavlja -COOH skupinu, -OH skupinu ili -OPO(OH)2 skupinu, tada R5 predstavlja vodikov atom;
∘ kada R5 predstavlja -OH skupinu, tada R3 i R4 predstavljaju vodikove atome;
- R6 je odabran od:
▪ fenilne skupine ili heteroarilne skupine koja sadrži 3 do 9 atoma ugljika i sadrži 1 do 3 heteroatoma neovisno odabrana od kisika, dušika i sumpora, pri čemu su navedene fenilne i heteroarilne skupine nesupstituirane ili supstituirane s 1 do 3 supstituenta neovisno odabranih iz niza koji čine:
(C1-C6)-alkil skupina nesupstituirana ili supstituirana s jednim ili više fluorovih atoma; halogeni atom; -OH skupina; (C1-C6)-alkoksi skupina nesupstituirana ili supstituirana s jednim ili više fluorovih atoma; cijano skupina; sumporna skupina supstituirana s 5 fluorovih atoma ili (C1-C6)-alkil skupine supstituirane s dva ili više fluorovih atoma; sulfonil-(C1-C6)-alkil skupina pri čemu je navedena (C1-C6)-alkil skupina nesupstituirana ili supstituirana s dva ili više fluorovih atoma; silanska skupina supstituirana sa 3 skupine (C1-C6)-alkil; aminska skupina nesupstituirana ili supstituirana s jednom ili više skupina (C1-C6)-alkil; amidna skupina nesupstituirana ili supstituirana s jednom ili više skupina (C1-C6)-alkil; heterocikloalkilne skupine zasićene ili djelomično zasićene, koje sadrže 3 do 5 atoma ugljika i sadrže 1 ili 2 heteroatoma neovisno odabrana između kisika, dušika ili sumpora, ili heteroarilna skupina koja sadrži 2 do 4 atoma ugljika i koja sadrži 1 do 3 heteroatoma odabrana između kisika, dušika ili sumpora i koja je nesupstituirana ili supstituirana s okso skupinom;
▪ cikloalkilna skupina ili heterocikloalkilna skupina koja sadrži 4 do 9 atoma ugljika i koja sadrži 1 ili 2 heteroatoma neovisno odabrana između kisika, dušika ili sumpora, navedene cikloalkilne skupine ili heterocikloalkilne skupine su zasićene ili djelomično zasićene i nesupstituirane ili supstituirane s 1 do 4 supstituenta neovisno odabrana od: fluorovog atoma; skupine -OH; skupine (C1-C6)-alkil; skupine -COOR7 pri čemu R7 je skupina (C1-C6)-alkil; ili okso skupina;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj s formulom (I) prema patentnom zahtjevu 1, naznačen time što je R6 odabran od fenilne skupine nesupstituirane ili supstituirane s 1 do 3 supstituenata neovisno odabrana iz niza koji čine: skupina (C1-C6)-alkil nesupstituirana ili supstituirana s jednim ili više fluorovih atoma; halogeni atom; -OH skupina; (C1-C6)-alkoksi skupina nesupstituirana ili supstituirana s jednim ili više fluorovih atoma; cijano skupina; sumporna skupina supstituirana s 5 fluorovih atoma ili (C1-C6)-alkilne skupine supstituirane s dva ili više fluorovih atoma; sulfonil-(C1-C6)-alkil skupina pri čemu je navedena skupina (C1-C6)-alkil nesupstituirana ili supstituirana s dva ili više fluorovih atoma; silanska skupina supstituirana sa 3 skupine (C1-C6)-alkil; aminska skupina nesupstituirana ili supstituirana s jednom ili više skupina (C1-C6)-alkil; amidna skupina nesupstituirana ili supstituirana s jednom ili više skupina (C1-C6)-alkil; heterocikloalkilna skupina zasićena ili djelomično zasićena, koja sadrži 3 do 5 ugljikovih atoma i sadrži 1 ili 2 heteroatoma neovisno odabrana između kisika, dušika ili sumpora, ili heteroarilna skupina koja sadrži 2 do 4 ugljikova atoma i i koja sadrži 1 do 3 heteroatoma odabrana između kisika, dušika ili sumpora i koja je nesupstituirana ili supstituirana s okso skupinom;
ili njegova farmaceutski prihvatljiva sol.
3. Spoj s formulom (I) prema patentnom zahtjevu 1 ili 2, naznačen time što je R6 odabran od fenilne skupine nesupstituirane ili supstituirane s 1 do 3 supstituenta neovisno odabrana iz niza koji čine metilna skupina; etilna skupina; izopropilna skupina; terc-butilna skupina; -CHF2 skupina; -CF3 skupina; -CF2CH3 skupina; klorov atom; fluorov atom; -OH skupina; -OCH3 skupina; -OCH2CH3 skupina; -OCH2CH2F skupina; -OCHF2 skupina; -OCH2CHF2 skupina; -OCF3 skupina; -OCH2CF3 skupina; cijano skupina; -SCHF2 skupina; -SCF3 skupina; -SF5 skupina; -SO2CH3 skupina; -SO2CF3 skupina; -Si(CH3)3 skupina; oksetanska skupina; piperidinska skupina; morfolinska skupina; pirolidinska skupina ili triazolonska skupina;
ili njegova farmaceutski prihvatljiva sol.
4. Spoj s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time što R3 je -COOH skupina ili -OH skupina;
ili njegova farmaceutski prihvatljiva sol.
5. Spoj s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 4, naznačen time što je spoj 5-[4-[(3S)-1-(3-fluoropropil)pirolidin-3-il]oksifenil]-6-(1H-indol-5-il)-8,9-dihidro-7H-benzo[7]anulen-3-ol s formulom
[image]
5-[4-[(3S)-1-(3-fluoropropil)pirolidin-3-il]oksifenil]-6-indolin-5-il-8,9-dihidro-7H-benzo[7]anulen-2-ol s formulom
[image]
5-[4-[(3S)-1-(3-fluoropropil)pirolidin-3-il]oksifenil]-6-(1,2,3,6-tetrahidropiridin-4-il)-8,9-dihidro-7H-benzo[7]anulen-2-ol s formulom
[image]
6-(2,4-diklorofenil)-5-[4-[(3S)-1-(3-fluoropropil)pirolidin-3-il]oksifenil]-8,9-dihidro-7H-benzo[7]anulen-2-karboksilna kiselina s formulom
[image]
5-[4-[(3S)-1-(3-fluoropropil)pirolidin-3-il]oksifenil]-6-[4-(trifluorometoksi)fenil]-8,9-dihidro-7H-benzo[7]anulen-2-ol s formulom
[image]
6-(6-etoksi-2-fluoro-3-piridil)-1-fluoro-5-[4-[(3S)-1-(3-fluoropropil)pirolidin-3-il]oksifenil]-8,9-dihidro-7H-benzo[7]anulen-2-ol s formulom
[image]
6-(2-etoksipirimidin-5-il)-5-[4-[(3S)-1-(3-fluoropropil)pirolidin-3-il]oksifenil]-8,9-dihidro-7H-benzo[7]anulen-2-ol s formulom
[image]
[5-[4-[(3S)-1-(3-fluoropropil)pirolidin-3-il]oksifenil]-6-[4-(trifluorometoksi)fenil]-8,9-dihidro-7H-benzo[7]anulen-2-il] dihidrogen fosfat s formulom
[image]
ili
5-[4-[(3S)-1-(3-fluoropropil)pirolidin-3-il]oksifenil]-6-(4-hidroksicikloheksil)-8,9-dihidro-7H-benzo[7]anulen-2-ol s formulom
[image]
ili njihova farmaceutski prihvatljiva sol.
6. Spojevi odabrani iz sljedećih formula:
[image]
[image]
pri čemu R3, R4, R5 i R6 su kako je definirano u formuli (I) prema bilo kojem od patentnih zahtjeva 1 do 4.
7. Lijek, naznačen time što sadrži spoj s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 5, ili njegovu farmaceutski prihvatljivu sol.
8. Farmaceutski pripravak, naznačen time što sadrži spoj s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 5, ili njegovu farmaceutski prihvatljivu sol, te najmanje jednu farmaceutski prihvatljivu pomoćnu tvar.
9. Spoj s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, naznačen time što je za uporabu u liječenju ovulacijske disfunkcije, raka, endometrioze, osteoporoze, benigne hipertrofije prostate ili upale.
10. Spoj s formulom (I), ili njegova farmaceutski prihvatljiva sol, za upotrebu prema patentnom zahtjevu 9 naznačen time što je za liječenje raka.
11. Spoj s formulom (I), ili njegova farmaceutski prihvatljiva sol, za upotrebu prema patentnom zahtjevu 10, naznačen time što je rak rak ovisan o estrogenom receptoru.
12. Spoj s formulom (I), ili njegova farmaceutski prihvatljiva sol, za upotrebu prema patentnom zahtjevu 10 ili 11, naznačen time što je rak odabran od karcinoma dojke, jajnika, endometrija, prostate, maternice, vrata maternice i pluća ili njihovih metastaza.
13. Spoj s formulom (I), ili njegova farmaceutski prihvatljiva sol, za upotrebu prema patentnom zahtjevu 12, naznačen time što je metastaza cerebralna metastaza.
14. Spoj s formulom (I), ili njegova farmaceutski prihvatljiva sol, za upotrebu prema patentnom zahtjevu 12, naznačen time što je rak otporan na anti-hormonsko liječenje.
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