HRP20221462T1 - Selektivni nishodni regulatori receptora estrogena na bazi benzotiofena - Google Patents
Selektivni nishodni regulatori receptora estrogena na bazi benzotiofena Download PDFInfo
- Publication number
- HRP20221462T1 HRP20221462T1 HRP20221462TT HRP20221462T HRP20221462T1 HR P20221462 T1 HRP20221462 T1 HR P20221462T1 HR P20221462T T HRP20221462T T HR P20221462TT HR P20221462 T HRP20221462 T HR P20221462T HR P20221462 T1 HRP20221462 T1 HR P20221462T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- image
- pharmaceutically acceptable
- acceptable salt
- cancer
- Prior art date
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- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 title 2
- 229940119564 Selective estrogen receptor downregulator Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 29
- 150000003839 salts Chemical class 0.000 claims 17
- 239000000825 pharmaceutical preparation Substances 0.000 claims 10
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 229940011871 estrogen Drugs 0.000 claims 5
- 239000000262 estrogen Substances 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 206010006187 Breast cancer Diseases 0.000 claims 4
- 208000026310 Breast neoplasm Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 206010065687 Bone loss Diseases 0.000 claims 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 206010055113 Breast cancer metastatic Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 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
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 108091008039 hormone receptors Proteins 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000004228 ovarian endometrial cancer Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229960001603 tamoxifen Drugs 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
- C07D333/64—Oxygen atoms
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Physical Education & Sports Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Compounds Of Unknown Constitution (AREA)
Claims (26)
1. Spoj ili njegova farmaceutski prihvatljiva sol formule A:
[image]
naznačeno time što:
m je 0, 1, 2, 3 ili 4;
n je 0, 1, 2, 3 ili 4;
XA je -O-;
prsten B je fenil, naftil, hinolinil, 5- ili 6-člani monociklični heteroaril ili 7-, 8-, 9- ili 10-člani biciklični heterociklil;
prsten C je fenil, tiofenil, 5- ili 6-člani monociklični heteroaril ili 7-, 8-, 9- ili 10-člani biciklični heterociklil;
R1 je hidroksil;
R2 je izabran od -CH=CHCOOH, -NH(CO)COOH, -COOH, C2-C6alkenilen-COOH i C2-C6alkinilen-COOH;
R3 je neovisno izabran pri svakom pojavljivanju od vodika, halogena, -CN, -NO2, C1-C6alkil i C1-C6fluoroalkil; i
R4 je neovisno izabran pri svakom pojavljivanju od vodika, halogena, hidroksila, C1-C6alkil, C1-C6fluoroalkil, -CN, -O(C1-C6 alkil), i -O(C1-C6fluoroalkil).
2. Spoj prema zahtjevu 1, naznačen time što:
a) R2 je izabran od -COOH, -NH(CO)COOH i -CH=CHCOOH; i/ili
b) prsten B je fenil, naftil ili hinolinil i prsten C je fenil ili 5- ili 6-člani monociklični heteroaril gdje je 5- ili 6-člani monociklični heteroaril tienil; i/ili
c) m je 0, m je 1 ili m je 2.
3. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, formule:
[image]
ili
[image]
4. Spoj prema bilo kojem od zahtjeva 1 do 3, naznačen time što R3 je neovisno izabran pri svakom pojavljivanju od vodika, halogena i C1-C6alkil.
5. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, formule: naznačen time što
[image]
Z je CH ili N.
6. Spoj prema bilo kojem od zahtjeva 1 do 5, naznačen time što:
a) R4 je neovisno izabran pri svakom pojavljivanju od halogena, i C1-C6alkil; i/ili
b) n je 0, ili pri čemu n je 1, 2 ili 3.
7. Spoj prema bilo kojem od zahtjeva 1 do 6, naznačen time što C1-C6alkil je metil, i/ili halogen je fluor.
8. Spoj prema zahtjevu 1, izabran od
[image]
[image]
[image]
[image]
[image]
[image]
[image]
i
[image]
ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, strukture:
[image]
10. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, strukture:
[image]
11. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, strukture:
[image]
12. Farmaceutski pripravak koji sadrži spoj ili njegovu farmaceutski prihvatljivu sol prema bilo kojem od zahtjeva 1 do 11 i farmaceutski prihvatljiv nosač ili ekscipijens.
13. Farmaceutski pripravak prema zahtjevu 12, naznačen time što je spoj strukture:
[image]
ili njegova farmaceutski prihvatljiva sol.
14. Farmaceutski pripravak prema zahtjevu 12, naznačen time što je spoj strukture:
[image]
ili njegova farmaceutski prihvatljiva sol.
15. Farmaceutski pripravak prema zahtjevu 12, naznačen time što je spoj strukture:
[image]
ili njegova farmaceutski prihvatljiva sol.
16. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 11 ili farmaceutski pripravak prema bilo kojem od zahtjeva 12 do 15 za uporabu u liječenju poremećaja povezanih sa estrogenom.
17. Spoj ili farmaceutski pripravak za uporabu prema zahtjevu 16, naznačen time što je spoj strukture:
[image]
ili njegova farmaceutski prihvatljiva sol.
18. Spoj ili farmaceutski pripravak za uporabu prema zahtjevu 16, naznačen time što je spoj strukture:
[image]
ili njegova farmaceutski prihvatljiva sol.
19. Spoj ili farmaceutski pripravak za uporabu prema zahtjevu 16, naznačen time što je spoj strukture:
[image]
ili njegova farmaceutski prihvatljiva sol.
20. Spoj ili farmaceutski pripravak za uporabu prema bilo kojem od zahtjeva 16 do 19, naznačen time što, poremećaj povezan sa estrogenom je rak.
21. Spoj ili farmaceutski pripravak za uporabu prema zahtjevu 20, naznačen time što je rak izabran iz grupe koja se sastoji od raka prostate, bubrega, raka pluća, raka dojke, raka jajnika i raka endometrija.
22. Spoj ili farmaceutski pripravak za uporabu prema zahtjevu 20, naznačen time što, rak je rak dojke.
23. Spoj ili farmaceutski pripravak za uporabu prema zahtjevu 22, naznačen time što je rak dojke izabran iz grupe koja se sastoji od metastatskog raka dojke pozitivnog na hormonski receptor, rak dojke otporan na tamoksifen ili trostruko negativan rak dojke.
24. Spoj ili farmaceutski pripravak za uporabu prema bilo kojem od zahtjeva 16 do 19: a) naznačen time što, poremećaj povezan sa estrogenom je gubitak kosti, pri čemu je gubitak kosti uzrokovan osteoporozom; ili b) pri čemu, poremećaj povezan sa estrogenom je tumor.
25. Postupak za pripremu terapeutskog proizvoda koji sadrži efikasnu količinu spoja kako je opisano u bilo kojem od zahtjeva 1 do 11, ili njegove farmaceutski prihvatljive soli.
26. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od zahtjeva 1 do 11 ili farmaceutski pripravak prema bilo kojem od zahtjeva 12 do 15 za uporabu u postupku liječenja raka povezanog sa estrogenom koji je metastazirao na mozak ili kost.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562264971P | 2015-12-09 | 2015-12-09 | |
| US201662322878P | 2016-04-15 | 2016-04-15 | |
| EP16874012.4A EP3386500B1 (en) | 2015-12-09 | 2016-12-09 | Benzothiophene-based selective estrogen receptor downregulators |
| PCT/US2016/066023 WO2017100712A1 (en) | 2015-12-09 | 2016-12-09 | Benzothiophene-based selective estrogen receptor downregulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20221462T1 true HRP20221462T1 (hr) | 2023-01-20 |
Family
ID=59013340
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20221462TT HRP20221462T1 (hr) | 2015-12-09 | 2016-12-09 | Selektivni nishodni regulatori receptora estrogena na bazi benzotiofena |
Country Status (24)
| Country | Link |
|---|---|
| US (7) | US20170166551A1 (hr) |
| EP (2) | EP3386968A4 (hr) |
| JP (2) | JP6920709B2 (hr) |
| KR (1) | KR20180088457A (hr) |
| CN (2) | CN108699024B (hr) |
| AU (1) | AU2016366680B2 (hr) |
| BR (1) | BR112018011607B1 (hr) |
| CA (1) | CA3008020C (hr) |
| DK (1) | DK3386500T3 (hr) |
| EA (1) | EA038180B1 (hr) |
| ES (1) | ES2935125T3 (hr) |
| HR (1) | HRP20221462T1 (hr) |
| HU (1) | HUE061065T2 (hr) |
| IL (1) | IL259566B (hr) |
| LT (1) | LT3386500T (hr) |
| MX (2) | MX2020006991A (hr) |
| NZ (1) | NZ743651A (hr) |
| PL (1) | PL3386500T3 (hr) |
| PT (1) | PT3386500T (hr) |
| RS (1) | RS63791B1 (hr) |
| RU (1) | RU2747802C2 (hr) |
| SI (1) | SI3386500T1 (hr) |
| WO (2) | WO2017100715A1 (hr) |
| ZA (2) | ZA201803422B (hr) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3008020C (en) | 2015-12-09 | 2024-02-20 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective estrogen receptor downregulators |
| US10599150B2 (en) | 2016-09-29 | 2020-03-24 | The Charles Stark Kraper Laboratory, Inc. | Autonomous vehicle: object-level fusion |
| JP7229162B2 (ja) * | 2017-01-06 | 2023-02-27 | ジー１ セラピューティクス， インコーポレイテッド | 癌の治療に対する併用療法 |
| CN110461853A (zh) | 2017-02-10 | 2019-11-15 | G1治疗公司 | 苯并噻吩雌激素受体调节剂 |
| BR112019027967A2 (pt) | 2017-06-29 | 2020-07-14 | G1 Therapeutics, Inc. | forma b cristalina isolada, composição farmacêutica, método para o tratamento de um distúrbio, método de um composto ou composição, e, processo para produzir forma b cristalina. |
| EP3749654A4 (en) | 2018-02-06 | 2021-11-03 | The Board of Trustees of the University of Illinois | BENZOTHIOPHENE ANALOGUES SUBSTITUTED AS SELECTIVE ESTROGEN RECEPTOR DEGRADATION AGENTS |
| US10741313B1 (en) | 2019-02-06 | 2020-08-11 | Eaton Intelligent Power Limited | Bus bar assembly with integrated surge arrestor |
| US11249184B2 (en) | 2019-05-07 | 2022-02-15 | The Charles Stark Draper Laboratory, Inc. | Autonomous collision avoidance through physical layer tracking |
| US20220233534A1 (en) * | 2019-07-08 | 2022-07-28 | Dermavant Sciences GmbH | Cerdulatinib-containing topical skin pharmaceutical compositions and uses thereof |
| CN115710248A (zh) * | 2022-11-18 | 2023-02-24 | 南京中医药大学 | 新型选择性雌激素受体下调剂化合物、制备方法及用途 |
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