TWI874834B - 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途 - Google Patents

四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途 Download PDF

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Publication number
TWI874834B
TWI874834B TW111140973A TW111140973A TWI874834B TW I874834 B TWI874834 B TW I874834B TW 111140973 A TW111140973 A TW 111140973A TW 111140973 A TW111140973 A TW 111140973A TW I874834 B TWI874834 B TW I874834B
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Taiwan
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methyl
compound
difluoro
formula
phenyl
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TW111140973A
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Chinese (zh)
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TW202323253A (zh
Inventor
西蒙 查爾斯 古達魁
夏拉達 萊柏迪
梁軍
丹尼爾 佛瑞德 歐文
尼可拉斯 查爾斯 瑞
曉菁 王
傑生 賽比格
必隆 張
光華 賴
廖江鵬
劉治國
小文 衛
弢 王
勵軍
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瑞士商赫孚孟拉羅股份公司
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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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • 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
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW111140973A 2014-12-18 2015-12-17 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途 TWI874834B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201462093929P 2014-12-18 2014-12-18
US62/093,929 2014-12-18
US201562110998P 2015-02-02 2015-02-02
US62/110,998 2015-02-02
US201562142077P 2015-04-02 2015-04-02
US62/142,077 2015-04-02

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TW202323253A TW202323253A (zh) 2023-06-16
TWI874834B true TWI874834B (zh) 2025-03-01

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TW111140973A TWI874834B (zh) 2014-12-18 2015-12-17 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途
TW104142533A TWI699363B (zh) 2014-12-18 2015-12-17 四氫-吡啶并［３，４-ｂ］吲哚雌激素受體調節劑及其用途
TW109111355A TWI784255B (zh) 2014-12-18 2015-12-17 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途
TW114103221A TW202534076A (zh) 2014-12-18 2015-12-17 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途
TW113141976A TWI875674B (zh) 2014-12-18 2015-12-17 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途

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TW104142533A TWI699363B (zh) 2014-12-18 2015-12-17 四氫-吡啶并［３，４-ｂ］吲哚雌激素受體調節劑及其用途
TW109111355A TWI784255B (zh) 2014-12-18 2015-12-17 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途
TW114103221A TW202534076A (zh) 2014-12-18 2015-12-17 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途
TW113141976A TWI875674B (zh) 2014-12-18 2015-12-17 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途

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Families Citing this family (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2952897A1 (en) 2014-06-27 2015-12-30 Nogra Pharma Limited Aryl receptor modulators and methods of making and using the same
WO2016097071A1 (en) 2014-12-18 2016-06-23 F. Hoffmann-La Roche Ag Estrogen receptor modulators and uses thereof
RS60824B1 (sr) 2014-12-18 2020-10-30 Hoffmann La Roche Tetrahidro-pirido[3,4-b]indoli kao modulatori estrogenih receptora i njihova upotreba
NZ779654A (en) * 2015-10-01 2024-12-20 Olema Pharmaceuticals Inc Tetrahydro-1h-pyrido[3,4-b]indole anti-estrogenic drugs
JP2019001715A (ja) * 2015-10-30 2019-01-10 協和発酵キリン株式会社 三環性化合物
EP3386968B1 (en) 2015-12-09 2025-04-02 The Board of Trustees of the University of Illinois Benzothiophene-based selective estrogen receptor downregulator compounds
DK3411034T3 (da) 2016-02-05 2021-01-11 Inventisbio Inc Selektiv østrogenreceptornedbrydere og anvendelser deraf
SI3416962T1 (sl) 2016-02-15 2021-08-31 Sanofi Derivati 6,7-dihidro-5H-benzo(7)anulena, kot modulatorji estrogenskega receptorja
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
ES2990061T3 (es) 2016-05-10 2024-11-28 C4 Therapeutics Inc Degronímeros espirocíclicos para la degradación de proteínas diana
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
JP2019521983A (ja) * 2016-06-16 2019-08-08 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−ピリド［３，４−ｂ］インドールエストロゲン受容体モジュレーター及びその使用
EP3472162B1 (en) * 2016-06-16 2021-11-17 F. Hoffmann-La Roche AG Heteroaryl estrogen receptor modulators and uses thereof
CN107543871A (zh) * 2016-06-29 2018-01-05 重庆华邦胜凯制药有限公司 分离测定帕布昔利布中间体z1及其有关物质的方法
RU2019102647A (ru) 2016-07-01 2020-08-03 Г1 Терапьютикс, Инк. Антипролиферационные средства на основе пиримидина
TW201815789A (zh) 2016-07-25 2018-05-01 瑞典商阿斯特捷利康公司 化合物
SMT202100667T1 (it) * 2016-09-27 2022-01-10 Radius Pharmaceuticals Inc Metodi per trattare il cancro ovarico
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
LT3433256T (lt) * 2016-10-24 2019-11-11 Astrazeneca Ab 6,7,8,9-tetrahidro-3h-pirazolo[4,3-f]izochinolino darinys, naudingas vėžio gydymui
US10774081B2 (en) * 2016-10-28 2020-09-15 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Indolo substituted piperidine compound as estrogen receptor down-regulator
MX394672B (es) * 2016-11-17 2025-03-21 Sanofi Sa Compuestos de n-(3-fluoropropil)-pirrolidina sustituidos novedosos, procesos para su preparacion y usos terapeuticos de los mismos.
WO2018108954A1 (en) 2016-12-12 2018-06-21 F. Hoffmann-La Roche Ag Process for the preparation of 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol
EA037533B9 (ru) * 2016-12-16 2021-05-27 Астразенека Аб 6,7,8,9-ТЕТРАГИДРО-3H-ПИРАЗОЛО[4,3-f]ИЗОХИНОЛИНОВЫЕ ПРОИЗВОДНЫЕ, ПРИМЕНИМЫЕ В ЛЕЧЕНИИ РАКА
AU2018205262A1 (en) 2017-01-06 2019-07-11 G1 Therapeutics, Inc. Combination therapy for the treatment of cancer
WO2018130123A1 (zh) * 2017-01-11 2018-07-19 南京圣和药业股份有限公司 作为选择性雌激素受体下调剂的五环类化合物及其应用
WO2018138739A1 (en) 2017-01-27 2018-08-02 Sun Pharma Advanced Research Company Limited Novel antiestrogenic heterocyclic compounds
MA52555A (fr) * 2017-01-30 2021-03-17 Astrazeneca Ab Modulateurs du récepteur des oestrogènes
WO2018148576A1 (en) 2017-02-10 2018-08-16 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators
EP3641762A4 (en) 2017-06-20 2021-03-10 C4 Therapeutics, Inc. N / O-LINKED DEGRONES AND DEGRONIMERS FOR PROTEIN DEGRADATION
FI3645001T3 (fi) 2017-06-29 2024-09-25 G1 Therapeutics Inc Git38:n morfisia muotoja ja niiden valmistusmenetelmiä
EP3434272A1 (en) 2017-07-25 2019-01-30 Sanofi Combination comprising palbociclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid
US11236088B2 (en) 2017-11-14 2022-02-01 Kind Pharmaceutical Heterocyclic compounds and their application in medicine
EA038160B1 (ru) * 2017-11-30 2021-07-15 Астразенека Аб Модуляторы рецептора эстрогена
US10519152B2 (en) 2017-12-21 2019-12-31 Astrazeneca Ab Compounds and their use in treating cancer
SG11202006942WA (en) 2018-01-22 2020-08-28 Radius Pharmaceuticals Inc Estrogen receptor-modulating compounds
CN110343101B (zh) * 2018-04-04 2022-07-12 青岛福沃药业有限公司 用于治疗乳腺癌的雌激素受体降解剂
WO2019222272A1 (en) 2018-05-14 2019-11-21 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
PL3810283T3 (pl) 2018-06-21 2023-10-16 F. Hoffmann-La Roche Ag Postacie stałe soli winianowej 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropylo)azetydyn-3-ylo)amino)fenylo)-3-metylo-1,3,4,9-tetrahydro-2H-pirydo[3,4-b]indol-2-ilo)-2,2-difluoropropan-1-olu, sposób ich otrzymywania i sposoby ich zastosowania w leczeniu nowotworów
TWI702219B (zh) * 2018-07-12 2020-08-21 美商美國禮來大藥廠 選擇性雌激素受體降解劑
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
TWI803692B (zh) 2018-09-07 2023-06-01 法商賽諾菲公司 用於製備6-(2,4-二氯苯基)-5-[4-[(3s)-1-(3-氟丙基)吡咯啶-3-基]氧基苯基]-8,9-二氫-7h-苯并[7]輪烯-2-甲酸甲酯之方法
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
WO2020132561A1 (en) 2018-12-20 2020-06-25 C4 Therapeutics, Inc. Targeted protein degradation
KR20210131316A (ko) * 2019-02-27 2021-11-02 밀레니엄 파머슈티컬스 인코퍼레이티드 Sumo-활성화 효소 저해제 및 관문 저해제의 투여
BR112021022008A2 (pt) 2019-05-14 2022-05-17 Nuvation Bio Inc Compostos de direcionamento a receptor de hormônio nuclear anticâncer
CA3137091A1 (en) * 2019-06-17 2020-12-24 Ucb Pharma Gmbh N-(phenyl)-indole-3-sulfonamide derivatives and related compounds as gpr17 modulators for treating cns disorders such as multiple sclerosis
JP7616794B2 (ja) * 2019-07-07 2025-01-17 オレマ ファーマシューティカルズ インク． エストロゲン受容体アンタゴニストのレジメン
CA3146365A1 (en) 2019-07-22 2021-01-28 Radius Pharmaceuticals, Inc. Estrogen receptor-modulating compounds
KR20220044528A (ko) 2019-08-06 2022-04-08 리커리엄 아이피 홀딩스, 엘엘씨 돌연변이체를 치료하기 위한 에스트로겐 수용체 조절제
WO2021055749A1 (en) * 2019-09-19 2021-03-25 Totus Medicines Inc. Therapeutic conjugates
TW202131930A (zh) 2019-11-13 2021-09-01 美商諾維雪碧歐公司 抗癌核荷爾蒙受體標靶化合物
IL293999B1 (en) 2019-12-20 2025-10-01 C4 Therapeutics Inc Isoindolinone compounds with a phenylaminoglutarimide residue for degradation of EGFR
KR20220119658A (ko) * 2019-12-20 2022-08-30 리커리엄 아이피 홀딩스, 엘엘씨 조합물
TW202140475A (zh) * 2020-01-16 2021-11-01 大陸商江蘇恆瑞醫藥股份有限公司 稠合醯亞胺類衍生物、其製備方法及其在醫藥上的應用
TW202140448A (zh) * 2020-01-16 2021-11-01 大陸商江蘇恆瑞醫藥股份有限公司 並環醯亞胺類衍生物、其製備方法及其在醫藥上的應用
TW202146007A (zh) 2020-02-27 2021-12-16 法商賽諾菲公司 包含阿培利司（ａｌｐｅｌｉｓｉｂ）與６－（２，４－二氯苯基）－５－［４－［（３ｓ）－１－（３－氟丙基）吡咯啶－３－基］氧苯基］－８，９－二氫－７ｈ－苯并［７］輪烯－２－羧酸之組合
CA3165309A1 (en) 2020-03-05 2021-09-10 Christopher G. Nasveschuk Compounds for targeted degradation of brd9
AU2021230588A1 (en) 2020-03-06 2022-08-25 Olema Pharmaceuticals, Inc. Methods of treating estrogen receptor-associated diseases
WO2021213358A1 (zh) * 2020-04-21 2021-10-28 江苏先声药业有限公司 含硼化合物及其应用
EP4138834A1 (en) 2020-04-24 2023-03-01 Astrazeneca AB Dosage regimen for the treatment of cancer
IL297218A (en) 2020-04-24 2022-12-01 Astrazeneca Ab Pharmaceutical formulations
EP4149476A1 (en) * 2020-05-12 2023-03-22 Genentech, Inc. Treatment of breast cancer using combination therapies comprising gdc-9545 and a cdk4/6 inhibitor
CN115836068B (zh) * 2020-05-15 2025-06-03 南京再明医药有限公司 吡咯烷类化合物及其应用
WO2021249533A1 (zh) * 2020-06-12 2021-12-16 江苏先声药业有限公司 雌激素受体调节剂化合物及其用途
CN120623091A (zh) * 2020-06-30 2025-09-12 基因泰克公司 用于制备具有经取代的苯基或吡啶基部分的serd三环化合物的方法
CN116490186B (zh) 2020-08-05 2025-10-31 C4医药公司 用于ret的靶向降解的化合物
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
JP2024502270A (ja) 2020-12-23 2024-01-18 リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー エストロゲン受容体調節薬
CN116744920A (zh) * 2021-02-08 2023-09-12 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
AU2022269568A1 (en) 2021-05-03 2023-11-16 Nuvation Bio Inc. Anti-cancer nuclear hormone receptor-targeting compounds
CN117940133A (zh) 2021-06-08 2024-04-26 C4医药公司 用于突变braf的降解的治疗剂
TW202317539A (zh) * 2021-07-15 2023-05-01 大陸商四川海思科製藥有限公司 芳氨基衍生物雌激素受體調節劑及其用途
KR102689151B1 (ko) * 2021-09-06 2024-07-29 연세대학교 산학협력단 Akt 신호경로 억제제를 유효성분으로 포함하는 아토피피부염의 예방 또는 치료용 조성물
WO2023060268A1 (en) * 2021-10-08 2023-04-13 Azora Therapeutics, Inc. Derivatives of aryl hydrocarbon receptor agonists
TW202333704A (zh) * 2021-11-12 2023-09-01 大陸商先聲藥業有限公司 用於治療腫瘤的藥物組合及其應用
WO2023091550A1 (en) * 2021-11-18 2023-05-25 Olema Pharmaceuticals, Inc. Methods of treating estrogen receptor-associated diseases
CN118679157A (zh) * 2021-12-28 2024-09-20 深圳扬厉医药技术有限公司 四氢环庚吲唑化合物的盐型、晶型
CN116804008A (zh) * 2022-03-24 2023-09-26 烟台创和生物科技有限公司 雌激素受体降解剂及其制备方法和应用
EP4514792A1 (en) 2022-04-28 2025-03-05 F. Hoffmann-La Roche AG Solid form of 3-((1r,3r)-1-(2,6-difluoro-4-((1-(3- fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9- tetrahydro-2h-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol tartrate
WO2023221122A1 (en) * 2022-05-20 2023-11-23 Olema Pharmaceuticals, Inc. Salts and solid forms of an estrogen receptor antagonist
WO2023221123A1 (en) * 2022-05-20 2023-11-23 Olema Pharmaceuticals, Inc. Crystalline forms of an estrogen receptor antagonist
WO2024015506A1 (en) * 2022-07-14 2024-01-18 Olema Pharmaceuticals, Inc. Methods of treating estrogen receptor-mediated disorders
WO2024017131A1 (zh) * 2022-07-21 2024-01-25 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
CN115109058B (zh) * 2022-07-27 2023-04-07 黑龙江中医药大学 一种用于治疗胃癌的药物及其制备方法
CN119998285A (zh) 2022-08-03 2025-05-13 百时美施贵宝公司 用于调控ret蛋白的化合物
EP4573092A1 (en) * 2022-08-19 2025-06-25 Olema Pharmaceuticals, Inc. 2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole derivatives as estrogen receptor modulators for the treatment of cancer
EP4573091A1 (en) * 2022-08-19 2025-06-25 Olema Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
EP4577542A1 (en) * 2022-08-25 2025-07-02 Sanofi Novel substituted 2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole carboxylic acid derivatives, processes for their preparation and therapeutic uses thereof
IL320302A (en) 2022-10-17 2025-06-01 Astrazeneca Ab SERD combinations for cancer treatment
TW202425966A (zh) * 2022-10-28 2024-07-01 大陸商南京再明醫藥有限公司 用於治療腫瘤的藥物組合、藥物組成物及其用途
CN120530116A (zh) 2022-11-04 2025-08-22 百时美施贵宝公司 Ret-ldd蛋白抑制剂
WO2024097989A1 (en) 2022-11-04 2024-05-10 Bristol-Myers Squibb Company Ret-ldd protein degraders
CN120187416A (zh) 2022-11-11 2025-06-20 阿斯利康(瑞典)有限公司 用于治疗癌症的组合疗法
US20240180893A1 (en) 2022-11-17 2024-06-06 Astrazeneca Ab Methods of treatment of breast cancer
CN115894485B (zh) * 2023-03-03 2023-06-27 山东绿叶制药有限公司 杂芳基并哌啶类衍生物、其制备方法及其在医药上的应用
US11773092B1 (en) 2023-03-27 2023-10-03 King Faisal University Pyrido[3,4-b]indol-1-one compounds as antibacterial agents
WO2024231548A1 (en) 2023-05-11 2024-11-14 Astrazeneca Ab Combination of a parp1 inhibitor and a selective estrogen degrader for treating cancer
WO2025006753A2 (en) 2023-06-30 2025-01-02 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras protein
WO2025103409A1 (zh) * 2023-11-16 2025-05-22 南京同诺康医药科技有限公司 Nmt抑制剂及其制备方法和用途
CN118791392A (zh) * 2024-06-18 2024-10-18 华中科技大学 一种合成依拉司群的方法及中间体化合物

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102408425A (zh) * 2004-03-15 2012-04-11 Ptc医疗公司 用于抑制血管生成的咔啉衍生物及其应用
CN102480957A (zh) * 2009-05-27 2012-05-30 Ptc医疗公司 治疗癌症及非肿瘤病症的方法

Family Cites Families (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE398789C (de) 1923-03-03 1924-07-15 L V Kramolin Verfahren und Einrichtung zur Verhinderung des Mithoerens beim Telephon- und Telegraphenverkehr mittels elektrischer Wellen und zum Vielfachverkehr mittels elektromagnetischer Wellen
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
SE455604B (sv) 1982-06-29 1988-07-25 Stiftelsen Ind Organisk Elektr Sett att framstella fenetylaminer medelst elektrokemisk reduktion
US5206377A (en) 1991-12-05 1993-04-27 Whitby Research, Inc. Compounds useful as antiproliferative agents
EP0620222A3 (en) 1993-04-14 1995-04-12 Lilly Co Eli Tetrahydro-beta-carbolines.
IL115582A0 (en) * 1994-10-14 1996-01-19 Lilly Co Eli Methods for treating resistant tumors
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
GB0000313D0 (en) 2000-01-10 2000-03-01 Astrazeneca Uk Ltd Formulation
EP1347759B1 (en) 2000-12-08 2005-06-29 Smithkline Beecham Corporation Antibacterial compounds
AU2002246728A1 (en) 2001-02-12 2002-08-28 Lilly Icos Llc Carboline derivatives
US6951961B2 (en) 2002-05-17 2005-10-04 Marina Nikolaevna Protopopova Methods of use and compositions for the diagnosis and treatment of infectious disease
TWI329111B (en) 2002-05-24 2010-08-21 X Ceptor Therapeutics Inc Azepinoindole and pyridoindole derivatives as pharmaceutical agents
JP4629657B2 (ja) 2003-04-11 2011-02-09 ハイ・ポイント・ファーマスーティカルズ、エルエルシー １１β−ヒドロキシステロイドデヒドロゲナーゼ１型化活性化合物
EP1670314A4 (en) 2003-09-05 2009-02-25 Sequella Inc METHODS AND COMPOSITIONS INCLUDE DIAMINE AS A NEW THERAPEUTIC FOR TUBERCULOSIS
US8076352B2 (en) 2004-03-15 2011-12-13 Ptc Therapeutics, Inc. Administration of carboline derivatives useful in the treatment of cancer and other diseases
US8076353B2 (en) 2004-03-15 2011-12-13 Ptc Therapeutics, Inc. Inhibition of VEGF translation
US7767689B2 (en) * 2004-03-15 2010-08-03 Ptc Therapeutics, Inc. Carboline derivatives useful in the treatment of cancer
EP1786425A1 (en) 2004-08-02 2007-05-23 SmithKline Beecham Corporation Useful compounds for hpv infection
WO2007002051A1 (en) 2005-06-22 2007-01-04 Smithkline Beecham Corporation Carboline derivatives and their use as inhibitors of flaviviridae infections
CA2622755C (en) 2005-10-07 2017-01-31 Exelixis, Inc. Azetidines as mek inhibitors
NZ601278A (en) 2006-09-22 2013-09-27 Pharmacyclics Inc Inhibitors of Bruton's tyrosine kinase
WO2008127714A1 (en) 2007-04-13 2008-10-23 Ptc Therapeutics, Inc. Administration of carboline derivatives useful in the treatment of cancer and other diseases
KR101390081B1 (ko) 2008-04-29 2014-04-29 노파르티스 아게 기생충 질환의 치료를 위한 스피로－인돌 유도체
US9292307B2 (en) 2008-07-30 2016-03-22 Kyocera Corporation User interface generation apparatus
EP2323651A2 (en) 2008-08-05 2011-05-25 Summit Corporation Plc Compounds for the treatment of flaviviral infections
WO2010015816A2 (en) 2008-08-06 2010-02-11 Summit Corporation Plc Treatment of lysosomal storage disorders and other proteostatic diseases
WO2010029313A1 (en) 2008-09-11 2010-03-18 Summit Corporation Plc. Antiinfective compounds
WO2010049678A2 (en) 2008-10-31 2010-05-06 Summit Corporation Plc Treatment of energy utilization diseases
WO2010075282A1 (en) 2008-12-22 2010-07-01 University Of Washington Molecular inhibitors of the wnt/beta-catenin pathway
WO2010075286A1 (en) 2008-12-24 2010-07-01 University Of Washington MOLECULAR ACTIVATORS OF THE Wnt/β-CATENIN PATHWAY
US20120135089A1 (en) 2009-03-17 2012-05-31 Stockwell Brent R E3 ligase inhibitors
US8497276B2 (en) 2009-03-31 2013-07-30 Arqule, Inc. Substituted indolo-piperidine compounds
US8703726B2 (en) * 2009-05-27 2014-04-22 Ptc Therapeutics, Inc. Methods for treating prostate conditions
WO2010138706A1 (en) * 2009-05-27 2010-12-02 Ptc Therapeutics, Inc. Methods for treating breast cancer
US20120157401A1 (en) * 2009-05-27 2012-06-21 Ptc Therapeutics, Inc. Methods for treating neurofibromatosis
WO2010138652A1 (en) 2009-05-27 2010-12-02 Ptc Therapeutics, Inc. Methods for treating kaposi sarcoma
WO2010138659A1 (en) 2009-05-27 2010-12-02 Ptc Therapeutics, Inc. Methods for treating brain tumors
WO2011150162A1 (en) 2010-05-27 2011-12-01 Ptc Therapeutics, Inc. Methods for treating viral conditions
JP2013528223A (ja) 2010-06-10 2013-07-08 アラゴン ファーマシューティカルズ，インク． エストロゲン受容体モジュレーターおよびその用途
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
MY164910A (en) 2010-12-16 2018-02-15 Hoffmann La Roche Tricyclic pi3k inhibitor compounds and methods of use
ES2586908T3 (es) 2010-12-24 2016-10-19 Merck Sharp & Dohme B.V. Derivados de azetidina N-sustituidos
US9193714B2 (en) 2011-12-14 2015-11-24 Seragon Pharmaceuticals, Inc. Fluorinated estrogen receptor modulators and uses thereof
SG11201405990PA (en) 2012-03-23 2014-11-27 Codexis Inc Biocatalysts and methods for synthesizing derivatives of tryptamine and tryptamine analogs
JP6117906B2 (ja) 2012-03-23 2017-04-19 ノバルティス アーゲー スピロインドロンおよびこれらの中間体を調製するための化学プロセス
DE102012209622A1 (de) 2012-06-08 2013-12-12 Robert Bosch Gmbh Zahnradmaschine mit hydrodynamisch und hydrostatisch gelagertem Lagerzapfen
EP2682119A1 (en) 2012-07-03 2014-01-08 Université Libre de Bruxelles Aromatic N-heterocycle derivatives for use as medicine
BR112015002493A8 (pt) * 2012-08-30 2019-07-30 Hoffmann La Roche composto, composição farmacêutica, processo para a preparação de uma composição farmacêutica, kit e uso de um composto”
EP2738173A1 (en) 2012-11-28 2014-06-04 Commissariat A L'energie Atomique Et Aux Energies Alternatives Heterocyclic compounds as inhibitors of the sodium iodide symporter
PT3004090T (pt) 2013-05-28 2017-12-22 Astrazeneca Ab Compostos químicos
BR112015031903A8 (pt) 2013-06-19 2019-12-31 Seragon Pharmaceuticals Inc composto, sal farmaceuticamente aceitável, composição farmacêutica e uso de um composto
BR112015030595A2 (pt) 2013-06-19 2017-07-25 Seragon Pharmaceuticals Inc moduladores de receptor de estrogênio de azetidina e usos dos mesmos
US9861594B2 (en) 2013-10-28 2018-01-09 Drexel University Treatments for attention and cognitive disorders, and for dementia associated with a neurodegenerative disorder
HK1223557A1 (zh) 2013-12-06 2017-08-04 豪夫迈．罗氏有限公司 用於治疗局部晚期或转移性雌激素受体阳性乳腺癌的雌激素受体调节剂
KR20160124909A (ko) 2014-03-13 2016-10-28 에프. 호프만-라 로슈 아게 에스트로겐 수용체 조절제를 함유하는 치료 조합물
KR20160132029A (ko) 2014-03-13 2016-11-16 에프. 호프만-라 로슈 아게 에스트로젠 수용체 돌연변이체의 조절을 위한 방법 및 조성물
CA2952897A1 (en) 2014-06-27 2015-12-30 Nogra Pharma Limited Aryl receptor modulators and methods of making and using the same
US20160175284A1 (en) 2014-12-18 2016-06-23 Genentech, Inc. Estrogen receptor modulators and uses thereof
RS60824B1 (sr) 2014-12-18 2020-10-30 Hoffmann La Roche Tetrahidro-pirido[3,4-b]indoli kao modulatori estrogenih receptora i njihova upotreba
WO2016097071A1 (en) 2014-12-18 2016-06-23 F. Hoffmann-La Roche Ag Estrogen receptor modulators and uses thereof
NZ779654A (en) 2015-10-01 2024-12-20 Olema Pharmaceuticals Inc Tetrahydro-1h-pyrido[3,4-b]indole anti-estrogenic drugs
DK3411034T3 (da) 2016-02-05 2021-01-11 Inventisbio Inc Selektiv østrogenreceptornedbrydere og anvendelser deraf

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102408425A (zh) * 2004-03-15 2012-04-11 Ptc医疗公司 用于抑制血管生成的咔啉衍生物及其应用
CN102480957A (zh) * 2009-05-27 2012-05-30 Ptc医疗公司 治疗癌症及非肿瘤病症的方法

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