AU2017349797B2 - 6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer - Google Patents
6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer Download PDFInfo
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- AU2017349797B2 AU2017349797B2 AU2017349797A AU2017349797A AU2017349797B2 AU 2017349797 B2 AU2017349797 B2 AU 2017349797B2 AU 2017349797 A AU2017349797 A AU 2017349797A AU 2017349797 A AU2017349797 A AU 2017349797A AU 2017349797 B2 AU2017349797 B2 AU 2017349797B2
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- Australia
- Prior art keywords
- compound
- formula
- methyl
- pyrazolo
- azetidin
- Prior art date
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- RDUKJIDJNWKKSO-UHFFFAOYSA-N CCC(C)(CC)CC(F)(F)F Chemical compound CCC(C)(CC)CC(F)(F)F RDUKJIDJNWKKSO-UHFFFAOYSA-N 0.000 description 3
- BUVXXDQCPBBBSZ-UHFFFAOYSA-N CCC(C)(CC)CC(CO)(F)F Chemical compound CCC(C)(CC)CC(CO)(F)F BUVXXDQCPBBBSZ-UHFFFAOYSA-N 0.000 description 2
- OKHRYHIXUNLSPK-UHFFFAOYSA-N CCCCC(C)(CO)F Chemical compound CCCCC(C)(CO)F OKHRYHIXUNLSPK-UHFFFAOYSA-N 0.000 description 2
- KWINFSVPUAMGEL-UHFFFAOYSA-N CCCCC(C)(COC)F Chemical compound CCCCC(C)(COC)F KWINFSVPUAMGEL-UHFFFAOYSA-N 0.000 description 2
- VRMZNWBHTQTYGS-UHFFFAOYSA-N CCCCC(COC)(F)F Chemical compound CCCCC(COC)(F)F VRMZNWBHTQTYGS-UHFFFAOYSA-N 0.000 description 2
- MGJHVNHYIFTLOM-UHFFFAOYSA-N CCC(C)(CC)CC(C)(CO)F Chemical compound CCC(C)(CC)CC(C)(CO)F MGJHVNHYIFTLOM-UHFFFAOYSA-N 0.000 description 1
- OKHRYHIXUNLSPK-ZETCQYMHSA-N CCCC[C@@](C)(CO)F Chemical compound CCCC[C@@](C)(CO)F OKHRYHIXUNLSPK-ZETCQYMHSA-N 0.000 description 1
- VFIHAIISGMHQAX-CPJLOUKISA-N CCOc1c([C@H]2N(CC3(CC3)F)[C@H](C)Cc3c(cn[nH]4)c4ccc23)ccc(NC2CNC2)c1 Chemical compound CCOc1c([C@H]2N(CC3(CC3)F)[C@H](C)Cc3c(cn[nH]4)c4ccc23)ccc(NC2CNC2)c1 VFIHAIISGMHQAX-CPJLOUKISA-N 0.000 description 1
- PQQKSRRBSGVAEC-QRQCRPRQSA-N C[C@H](Cc1c(C)c(N)ccc11)N(CC2(CC2)F)[C@@H]1c(ccc(C)c1)c1OC Chemical compound C[C@H](Cc1c(C)c(N)ccc11)N(CC2(CC2)F)[C@@H]1c(ccc(C)c1)c1OC PQQKSRRBSGVAEC-QRQCRPRQSA-N 0.000 description 1
- KFSGBLOJAOPEKF-QRQCRPRQSA-N C[C@H](Cc1c(cn[nH]2)c2ccc11)N(CC2(CC2)F)[C@@H]1c(ccc(C)c1)c1OC Chemical compound C[C@H](Cc1c(cn[nH]2)c2ccc11)N(CC2(CC2)F)[C@@H]1c(ccc(C)c1)c1OC KFSGBLOJAOPEKF-QRQCRPRQSA-N 0.000 description 1
- YNEFHIBJPSZQHX-WYRIXSBYSA-N C[C@H](Cc1c2ccc3c1c(C)n[nH]3)N(CI)[C@@H]2c(ncc(C)c1)c1F Chemical compound C[C@H](Cc1c2ccc3c1c(C)n[nH]3)N(CI)[C@@H]2c(ncc(C)c1)c1F YNEFHIBJPSZQHX-WYRIXSBYSA-N 0.000 description 1
- VOKJSQPDTDRJJN-FATZIPQQSA-N C[C@H](Cc1c2ccc3c1cn[nH]3)N(CC(C)(F)F)[C@@H]2c(ccc(NC1CNC1)c1)c1OC Chemical compound C[C@H](Cc1c2ccc3c1cn[nH]3)N(CC(C)(F)F)[C@@H]2c(ccc(NC1CNC1)c1)c1OC VOKJSQPDTDRJJN-FATZIPQQSA-N 0.000 description 1
- BFXKWHZHXIVGOE-NSYGIPOTSA-N C[C@H](Cc1c2ccc3c1cn[nH]3)N(CC(COC)(F)F)[C@@H]2c(nc1)ccc1NC1CN(CCCF)C1 Chemical compound C[C@H](Cc1c2ccc3c1cn[nH]3)N(CC(COC)(F)F)[C@@H]2c(nc1)ccc1NC1CN(CCCF)C1 BFXKWHZHXIVGOE-NSYGIPOTSA-N 0.000 description 1
- OUKSGPRUQUGEQA-DIFFPNOSSA-N C[C@H](Cc1c2ccc3c1cn[nH]3)N(CC(F)(F)F)[C@@H]2c1ccc(C)c(F)n1 Chemical compound C[C@H](Cc1c2ccc3c1cn[nH]3)N(CC(F)(F)F)[C@@H]2c1ccc(C)c(F)n1 OUKSGPRUQUGEQA-DIFFPNOSSA-N 0.000 description 1
- SAHOIHAQBIIZIL-HJJGIICYSA-N C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC(F)(F)F)[C@@H]2c(c(F)cc(NC(C1)CN1C(OC(C)(C)C)=O)c1)c1F Chemical compound C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC(F)(F)F)[C@@H]2c(c(F)cc(NC(C1)CN1C(OC(C)(C)C)=O)c1)c1F SAHOIHAQBIIZIL-HJJGIICYSA-N 0.000 description 1
- WEYJCSSGGVNWHX-JEEXHXACSA-N C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC(F)F)[C@@H]2c(ccc(Br)c1)c1OC Chemical compound C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC(F)F)[C@@H]2c(ccc(Br)c1)c1OC WEYJCSSGGVNWHX-JEEXHXACSA-N 0.000 description 1
- AWOTUJKILLUTKS-VOCBJCOPSA-N C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC(F)F)[C@@H]2c(ccc(OC(C1)CN1C(OC(C)(C)C)=O)c1)c1OC Chemical compound C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC(F)F)[C@@H]2c(ccc(OC(C1)CN1C(OC(C)(C)C)=O)c1)c1OC AWOTUJKILLUTKS-VOCBJCOPSA-N 0.000 description 1
- GJXAELGRPQRPEL-WIEGDUSSSA-N C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC(F)F)[C@@H]2c(nc1)ccc1OC(C1)CN1C(OC(C)(C)C)=O Chemical compound C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC(F)F)[C@@H]2c(nc1)ccc1OC(C1)CN1C(OC(C)(C)C)=O GJXAELGRPQRPEL-WIEGDUSSSA-N 0.000 description 1
- WNSYRSWYORDZAV-HPTJLLMFSA-N C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC1(CC1)F)[C@@H]2c1ccc(C)cn1 Chemical compound C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC1(CC1)F)[C@@H]2c1ccc(C)cn1 WNSYRSWYORDZAV-HPTJLLMFSA-N 0.000 description 1
- HVYPGORQTGJXNI-VDHQWJSESA-N C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC1(CF)COC1)[C@@H]2c(ccc(C)c1)c1OC Chemical compound C[C@H](Cc1c2ccc3c1cn[n]3C1OCCCC1)N(CC1(CF)COC1)[C@@H]2c(ccc(C)c1)c1OC HVYPGORQTGJXNI-VDHQWJSESA-N 0.000 description 1
- ALSRYEVIHYGVIY-ASSNKEHSSA-N C[C@H](Cc1c2ccc3n[nH]cc13)N(CC1(CC1)F)[C@@H]2c(c(F)cc(C)c1)c1F Chemical compound C[C@H](Cc1c2ccc3n[nH]cc13)N(CC1(CC1)F)[C@@H]2c(c(F)cc(C)c1)c1F ALSRYEVIHYGVIY-ASSNKEHSSA-N 0.000 description 1
- AZXBQHJBZMMCKH-WFVAOBRGSA-N C[C@H](Cc1c2ccc3n[n](C4OCCCC4)cc13)N(CC(F)F)[C@@H]2c(ccc(C)c1)c1OC Chemical compound C[C@H](Cc1c2ccc3n[n](C4OCCCC4)cc13)N(CC(F)F)[C@@H]2c(ccc(C)c1)c1OC AZXBQHJBZMMCKH-WFVAOBRGSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—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
- 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
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662411799P | 2016-10-24 | 2016-10-24 | |
| US62/411,799 | 2016-10-24 | ||
| US201662435159P | 2016-12-16 | 2016-12-16 | |
| US62/435,159 | 2016-12-16 | ||
| PCT/EP2017/076191 WO2018077630A1 (en) | 2016-10-24 | 2017-10-13 | 6,7,8,9-tetrahydro-3h-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2017349797A1 AU2017349797A1 (en) | 2019-05-30 |
| AU2017349797B2 true AU2017349797B2 (en) | 2020-05-21 |
Family
ID=60083331
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017349797A Active AU2017349797B2 (en) | 2016-10-24 | 2017-10-13 | 6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer |
Country Status (37)
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| EP3355884B1 (en) | 2015-10-01 | 2021-04-28 | Olema Pharmaceuticals, Inc. | TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS |
| JP7241542B2 (ja) * | 2016-04-08 | 2023-03-17 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | テトラヒドロイソキノリン エストロゲン受容体モジュレーター及びその使用 |
| WO2017182493A1 (en) | 2016-04-20 | 2017-10-26 | Astrazeneca Ab | Indazole derivatives for use in down-regulation of the estrogen receptor for the treatment of cancer |
| US10149839B2 (en) | 2016-07-25 | 2018-12-11 | Astrazeneca Ab | Chemical compounds |
| AU2017349797B2 (en) * | 2016-10-24 | 2020-05-21 | Astrazeneca Ab | 6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinoline derivatives useful in the treatment of cancer |
| TWI831738B (zh) | 2016-12-16 | 2024-02-11 | 美商瑞塔醫藥有限責任公司 | 用於抑制ＲＯＲγ及其他用途的嘧啶三環烯酮衍生物 |
| DK3555097T3 (da) | 2016-12-16 | 2022-07-25 | Janssen Pharmaceutica Nv | Imidazo[4,5-d]pyrrolo[2,3-b]pyridinforbindelser som inhibitorer af janus-kinaser |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| UA125043C2 (uk) | 2017-01-30 | 2021-12-29 | Астразенека Аб | Модулятори рецептора естрогену |
| WO2019002441A1 (en) * | 2017-06-29 | 2019-01-03 | Astrazeneca Ab | CHEMICAL COMPOUNDS |
| WO2019002442A1 (en) * | 2017-06-29 | 2019-01-03 | Astrazeneca Ab | CHEMICAL COMPOUNDS |
| EP3696178B1 (en) * | 2017-11-14 | 2022-04-06 | Kind Pharmaceutical | Heterocyclic compound and application thereof in medicine |
| TW202016110A (zh) | 2018-06-15 | 2020-05-01 | 比利時商健生藥品公司 | Ｊａｋ激酶家族之小分子抑制劑 |
| US11993574B2 (en) | 2018-06-15 | 2024-05-28 | Reata Pharmaceuticals, Inc | Pyrazole and imidazole compounds for inhibition of IL-17 and RORgamma |
| WO2019246461A1 (en) | 2018-06-20 | 2019-12-26 | Reata Pharmaceuticals, Inc. | Cysteine-dependent inverse agonists of nuclear receptors ror-gamma/ror-gamma-t and methods of treating diseases or disorders therewith |
| CN113490850B (zh) | 2018-08-17 | 2024-12-06 | 基因泰克公司 | 用于治疗乳腺癌的诊断和治疗方法 |
| CN109053524A (zh) * | 2018-09-11 | 2018-12-21 | 山东谛爱生物技术有限公司 | 一种N-Boc-3-羟基氮杂环丁烷的制备方法 |
| WO2021007146A1 (en) | 2019-07-07 | 2021-01-14 | Olema Pharmaceuticals, Inc. | Regimens of estrogen receptor antagonists |
| AU2020407514A1 (en) * | 2019-12-20 | 2022-07-14 | Recurium Ip Holdings, Llc | Combinations |
| US12428428B2 (en) | 2020-01-10 | 2025-09-30 | Jiangsu Hengrui Medicine Co., Ltd. | Tricyclic tetrahydroisoquinoline derivative, preparation method therefor and application thereof in medicine |
| MX2022013258A (es) | 2020-04-24 | 2022-11-14 | Astrazeneca Ab | Formulaciones farmaceuticas. |
| WO2021214253A1 (en) * | 2020-04-24 | 2021-10-28 | Astrazeneca Ab | Dosage regimen for the treatment of cancer |
| EP4151636A4 (en) * | 2020-05-15 | 2024-02-28 | Simcere Pharmaceutical Co. Ltd. | PYRROLIDINE COMPOUND AND ITS USE |
| TW202214626A (zh) * | 2020-06-12 | 2022-04-16 | 大陸商江蘇先聲藥業有限公司 | 雌激素受體調節劑化合物及其用途 |
| EP4174059A4 (en) | 2020-06-28 | 2024-07-03 | Medshine Discovery Inc. | INDAZOLE FUSED CYCLIC COMPOUND |
| CN114105977B (zh) * | 2020-08-28 | 2023-09-01 | 先声再明医药有限公司 | 雌激素受体调节剂化合物及其用途 |
| KR20220107752A (ko) | 2021-01-26 | 2022-08-02 | 충북대학교 산학협력단 | 피라졸로퀴놀린 유도체 및 이의 항암제로서의 용도 |
| WO2022166980A1 (zh) * | 2021-02-08 | 2022-08-11 | 贝达药业股份有限公司 | 杂芳基并哌啶类衍生物及其药物组合物和应用 |
| MX2023010642A (es) | 2021-03-11 | 2023-11-28 | Janssen Pharmaceutica Nv | Lorpucitinib para uso en el tratamiento de trastornos mediados por jak. |
| WO2023125700A1 (zh) * | 2021-12-28 | 2023-07-06 | 南京明德新药研发有限公司 | 四氢环庚吲唑化合物的盐型、晶型 |
| EP4604957A1 (en) | 2022-10-17 | 2025-08-27 | Astrazeneca AB | Combinations of a serd for the treatment of cancer |
| EP4615431A1 (en) | 2022-11-11 | 2025-09-17 | Astrazeneca AB | Combination therapies for the treatment of cancer |
| US20240180893A1 (en) | 2022-11-17 | 2024-06-06 | Astrazeneca Ab | Methods of treatment of breast cancer |
| WO2024231548A1 (en) | 2023-05-11 | 2024-11-14 | Astrazeneca Ab | Combination of a parp1 inhibitor and a selective estrogen degrader for treating cancer |
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