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
Links
- 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)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Physical Education & Sports Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
- Compounds Of Unknown Constitution (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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 (26)
| Country | Link |
|---|---|
| US (7) | US20170166551A1 (OSRAM) |
| EP (2) | EP3386500B1 (OSRAM) |
| JP (2) | JP6920709B2 (OSRAM) |
| KR (1) | KR102785173B1 (OSRAM) |
| CN (2) | CN108699024B (OSRAM) |
| AU (1) | AU2016366680B2 (OSRAM) |
| BR (1) | BR112018011607B1 (OSRAM) |
| CA (1) | CA3008020C (OSRAM) |
| CY (1) | CY1125767T1 (OSRAM) |
| DK (1) | DK3386500T3 (OSRAM) |
| EA (1) | EA038180B1 (OSRAM) |
| ES (1) | ES2935125T3 (OSRAM) |
| HR (1) | HRP20221462T1 (OSRAM) |
| HU (1) | HUE061065T2 (OSRAM) |
| IL (1) | IL259566B (OSRAM) |
| LT (1) | LT3386500T (OSRAM) |
| MX (2) | MX393926B (OSRAM) |
| NZ (1) | NZ743651A (OSRAM) |
| PL (1) | PL3386500T3 (OSRAM) |
| PT (1) | PT3386500T (OSRAM) |
| RS (1) | RS63791B1 (OSRAM) |
| RU (1) | RU2747802C2 (OSRAM) |
| SI (1) | SI3386500T1 (OSRAM) |
| SM (1) | SMT202300018T1 (OSRAM) |
| WO (2) | WO2017100715A1 (OSRAM) |
| ZA (2) | ZA201803422B (OSRAM) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| ES2935125T3 (es) | 2015-12-09 | 2023-03-01 | Univ Illinois | Reguladores a la baja selectivos de los receptores de estrógenos con base en benzotiofeno |
| US10599150B2 (en) | 2016-09-29 | 2020-03-24 | The Charles Stark Kraper Laboratory, Inc. | Autonomous vehicle: object-level fusion |
| AR110728A1 (es) * | 2017-01-06 | 2019-04-24 | G1 Therapeutics Inc | Terapia combinada para el tratamiento del cáncer |
| TW201835064A (zh) | 2017-02-10 | 2018-10-01 | 美商G1治療公司 | 苯并噻吩雌激素受體調節劑 |
| CA3067873A1 (en) | 2017-06-29 | 2019-01-03 | G1 Therapeutics, Inc. | Morphic forms of g1t38 and methods of manufacture thereof |
| WO2019157020A1 (en) | 2018-02-06 | 2019-08-15 | The Board Of Trustees Of The University Of Illinois | Substituted benzothiophene analogs as selective estrogen receptor degraders |
| CN112839646A (zh) * | 2018-08-16 | 2021-05-25 | G1治疗公司 | 用于治疗医学疾病的苯并噻吩雌激素受体调节剂 |
| 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 |
| AU2020268762A1 (en) * | 2019-05-09 | 2021-12-02 | Sanofi | 6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid for use in metastatic or advanced breast cancer patients |
| US20220233534A1 (en) * | 2019-07-08 | 2022-07-28 | Dermavant Sciences GmbH | Cerdulatinib-containing topical skin pharmaceutical compositions and uses thereof |
| CA3173678A1 (en) | 2020-05-19 | 2021-11-25 | Jay Copeland Strum | Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders |
| CN115710248B (zh) * | 2022-11-18 | 2024-06-21 | 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 |
| CN116574054B (zh) * | 2023-05-15 | 2025-01-28 | 南京中医药大学 | 选择性雌激素受体下调剂化合物、制备方法及用途 |
| AU2025206255A1 (en) * | 2024-01-05 | 2026-05-14 | Starton Therapeutics, Inc. | Solid state active pharmaceutical compositions for transdermal drug delivery |
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