CA2819299A1 - N-substituted azetidine derivatives - Google Patents

N-substituted azetidine derivatives Download PDF

Info

Publication number
CA2819299A1
CA2819299A1 CA2819299A CA2819299A CA2819299A1 CA 2819299 A1 CA2819299 A1 CA 2819299A1 CA 2819299 A CA2819299 A CA 2819299A CA 2819299 A CA2819299 A CA 2819299A CA 2819299 A1 CA2819299 A1 CA 2819299A1
Authority
CA
Canada
Prior art keywords
alkyl
compound
fluorine
optionally substituted
nitrile
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2819299A
Other languages
English (en)
French (fr)
Inventor
Fredricus Antonius Dijcks
Scott James Lusher
Herman Thijs Stock
Gerrit Herman Veeneman
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp & Dohme BV
Original Assignee
Merck Sharp & Dohme BV
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp & Dohme BV filed Critical Merck Sharp & Dohme BV
Publication of CA2819299A1 publication Critical patent/CA2819299A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
CA2819299A 2010-12-24 2011-12-16 N-substituted azetidine derivatives Abandoned CA2819299A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10196960 2010-12-24
EP10196960.8 2010-12-24
PCT/EP2011/073041 WO2012084711A1 (en) 2010-12-24 2011-12-16 N-substituted azetidine derivatives

Publications (1)

Publication Number Publication Date
CA2819299A1 true CA2819299A1 (en) 2012-06-28

Family

ID=43778253

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2819299A Abandoned CA2819299A1 (en) 2010-12-24 2011-12-16 N-substituted azetidine derivatives

Country Status (7)

Country Link
US (1) US9540361B2 (cg-RX-API-DMAC10.html)
EP (1) EP2655367B1 (cg-RX-API-DMAC10.html)
JP (1) JP5886873B2 (cg-RX-API-DMAC10.html)
AU (1) AU2011347718B2 (cg-RX-API-DMAC10.html)
CA (1) CA2819299A1 (cg-RX-API-DMAC10.html)
ES (1) ES2586908T3 (cg-RX-API-DMAC10.html)
WO (1) WO2012084711A1 (cg-RX-API-DMAC10.html)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3205648A1 (en) 2010-06-10 2017-08-16 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
EP2791132A4 (en) 2011-12-14 2015-08-05 Seragon Pharmaceuticals Inc ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
NZ710385A (en) 2013-02-19 2016-10-28 Novartis Ag Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders
TWI784255B (zh) 2014-12-18 2022-11-21 瑞士商赫孚孟拉羅股份公司 四氫-吡啶并[3,4-b]吲哚雌激素受體調節劑及其用途
WO2016174551A1 (en) * 2015-04-27 2016-11-03 Pfizer Inc. Anti-estrogenic compounds
WO2017059139A1 (en) 2015-10-01 2017-04-06 Olema Pharmaceuticals, Inc. TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS
JP6920295B2 (ja) * 2015-11-09 2021-08-18 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト テトラヒドロナフタレンエストロゲン受容体モジュレーター及びその使用
DK3386500T3 (da) 2015-12-09 2022-12-12 Univ Illinois Benzothiophen-baserede selektive østrogenreceptor ned-regulatorer
SG11201806829TA (en) * 2016-02-15 2018-09-27 Sanofi Sa 6,7-dihydro-5h-benzo[7]annulene derivatives as estrogen receptor modulators
EP3440067B1 (en) * 2016-04-08 2021-05-26 F. Hoffmann-La Roche AG Tetrahydroisoquinoline estrogen receptor modulators and uses thereof
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
CN121974842A (zh) 2016-05-10 2026-05-05 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
CN109789143A (zh) 2016-07-01 2019-05-21 G1治疗公司 基于嘧啶的抗增殖剂
UA125824C2 (uk) * 2016-10-24 2022-06-15 Астразенека Аб 6,7,8,9-ТЕТРАГІДРО-3H-ПІРАЗОЛО[4,3-f]ІЗОХІНОЛІНОВІ ПОХІДНІ, ЗАСТОСОВНІ В ЛІКУВАННІ РАКУ
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
EP3541809B1 (en) 2016-11-17 2025-06-25 Sanofi Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof
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
WO2018138739A1 (en) 2017-01-27 2018-08-02 Sun Pharma Advanced Research Company Limited Novel antiestrogenic heterocyclic compounds
KR20190117582A (ko) 2017-02-10 2019-10-16 쥐원 쎄라퓨틱스, 인크. 벤조티오펜 에스트로겐 수용체 조정제
GB201706806D0 (en) 2017-04-28 2017-06-14 Sentinel Oncology Ltd Pharmaceutical compounds
EP4717317A3 (en) 2017-06-20 2026-06-03 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
EP3645001B1 (en) 2017-06-29 2024-07-03 G1 Therapeutics, Inc. Morphic forms of git38 and methods of manufacture thereof
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
KR102765922B1 (ko) * 2018-02-06 2025-02-11 더 보오드 오브 트러스티스 오브 더 유니버시티 오브 일리노이즈 선택적인 에스트로겐 수용체 분해제로서의 치환된 벤조티오펜 유사체
LT3810283T (lt) 2018-06-21 2023-08-25 F. Hoffmann-La Roche Ag 3-((1r,3r)-1-(2,6-difluor-4-((1-(3-fluorpropil)azetidin-3- il)amino) fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)- 2,2- difluorpropan-1-olio tartrato druskos kietosios formos, jų paruošimo procesas ir jų naudojimo būdai vėžiui gydyti
DK3847157T3 (da) 2018-09-07 2022-08-08 Sanofi Sa Fremgangsmåde til fremstilling af methyl-[6-(2,4-dichlorphenyl)-5-[4-[(3s)-1-(3-fluorpropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulen-2-carboxylat] og salt deraf
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN BREAKDOWN
CA3144791A1 (en) 2019-07-07 2021-01-14 Olema Pharmaceuticals, Inc. Regimens of estrogen receptor antagonists
WO2021063967A1 (en) 2019-10-01 2021-04-08 Sanofi Novel substituted 6,7-dihydro-5h-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof
CA3160897A1 (en) 2019-12-09 2021-06-17 Sanofi Crystalline form of a 7h-benzo[7]annulene-2-carboxylic acid derivative
EP4681715A3 (en) 2019-12-20 2026-01-28 C4 Therapeutics, Inc. Isoindolinone and indazole compounds for the degradation of egfr
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
CN119823124A (zh) 2020-03-05 2025-04-15 C4医药公司 用于brd9的靶向降解的化合物
MX2022010425A (es) 2020-03-06 2022-09-07 Olema Pharmaceuticals Inc Metodos de tratamiento de enfermedades asociadas a los receptores de estrogenos.
EP4164653A4 (en) 2020-06-15 2024-06-19 G1 Therapeutics, Inc. MORPHIC FORMS OF TRILACICLIB AND METHODS OF PREPARING THE SAME
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
GB202015187D0 (en) 2020-09-25 2020-11-11 Sentinel Oncology Ltd A pharmaceutical salt
IL302152B1 (en) 2020-10-19 2026-07-01 Sanofi Sa 6,7-DIHYDRO-5H-BENZO[7]ANNULENE COMPOUNDS AND THEIR DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR THERAPEUTIC USES
IL302153B1 (en) 2020-10-19 2026-07-01 Sanofi Sa 6,7-DIHYDRO-5H-BENZO[7]ANNULENE COMPOUNDS AND THEIR DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR THERAPEUTIC USES
CN113248455A (zh) * 2021-05-25 2021-08-13 湖北科技学院 一种3,5-二取代异噁唑类衍生物及其合成方法
BR112023024507A2 (pt) 2021-05-26 2024-02-15 C4 Therapeutics Inc Método para tratar um câncer mediado por receptor do fator de crescimento epidérmico mutante que sofreu metástase para o cérebro ou sistema nervoso central
AU2022290851A1 (en) 2021-06-08 2023-11-23 C4 Therapeutics, Inc. Therapeutics for the degradation of mutant braf
WO2023059714A1 (en) * 2021-10-06 2023-04-13 Olema Pharmaceuticals, Inc. Methods of treating estrogen receptor-mediated disorders
KR20250055538A (ko) 2022-08-03 2025-04-24 브리스톨-마이어스 스큅 컴퍼니 Ret 단백질을 조정하기 위한 화합물
CN117924262A (zh) * 2022-10-14 2024-04-26 中国科学院上海药物研究所 二氢苯并噻喃类衍生物及其制备方法和用途
JP2025540906A (ja) 2022-11-04 2025-12-17 ブリストル-マイヤーズ スクイブ カンパニー Ret-lddタンパク質阻害剤
KR20250117789A (ko) 2022-11-04 2025-08-05 브리스톨-마이어스 스큅 컴퍼니 Ret-ldd 단백질 분해제
CN116813603B (zh) * 2023-06-02 2024-10-22 成都市第三人民医院 一种选择性雌激素受体α降解化合物及其制备方法和应用
CN122206684A (zh) 2023-06-30 2026-06-12 默克专利有限公司 用于kras蛋白降解的异双功能化合物
WO2026139448A1 (en) 2024-12-23 2026-07-02 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras protein

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3983245A (en) * 1975-02-06 1976-09-28 Smithkline Corporation Certain 4-(3-azacycloalkoxy or azacycloalkylmethoxy)benzoylbenzofurans or benzothiophenes
US6750213B2 (en) 2000-10-19 2004-06-15 Merck & Co., Inc. Estrogen receptor modulators
DOP2002000467A (es) * 2001-10-10 2003-04-15 Pfizer Prod Inc 2-amino-6 (fenilo sustituido en las posiciones 2,4,5)-piridinas
TW200304371A (en) * 2002-02-22 2003-10-01 Akzo Nobel Nv Substituted 10-ary1-11H-benzo [b] fluorenes and 7-ary1-5, 6-dihydro-benz [a] anthracenes for selective effects on estrogen receptors
US20030225132A1 (en) 2002-04-11 2003-12-04 Dininno Frank P. Estrogen receptor modulators
ATE481397T1 (de) 2002-04-24 2010-10-15 Merck Sharp & Dohme Modulatoren des östrogenrezeptors
CA2512000C (en) * 2002-12-26 2011-08-09 Eisai Co., Ltd. Selective estrogen receptor modulator
EP2222638A2 (en) * 2007-11-21 2010-09-01 Decode Genetics EHF Biaryl pde4 inhibitors for treating inflammation

Also Published As

Publication number Publication date
WO2012084711A1 (en) 2012-06-28
EP2655367B1 (en) 2016-07-06
EP2655367A1 (en) 2013-10-30
AU2011347718B2 (en) 2016-06-23
ES2586908T3 (es) 2016-10-19
JP5886873B2 (ja) 2016-03-16
US9540361B2 (en) 2017-01-10
JP2014503537A (ja) 2014-02-13
US20160130262A1 (en) 2016-05-12
AU2011347718A1 (en) 2013-05-30

Similar Documents

Publication Publication Date Title
AU2011347718B2 (en) N-substituted azetidine derivatives
WO2022268230A1 (zh) 作为kif18a抑制剂的化合物
BRPI0610183A2 (pt) Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, uso de um composto ou de um sal farmaceuticamente aceitável do mesmo
KR20140103335A (ko) 신규한 벤조피란 화합물, 조성물 및 이의 용도
EA018011B1 (ru) Катехоламиновые производные, полезные для лечения болезни паркинсона
CA2849176A1 (en) Fsh receptor antagonists
US6689798B2 (en) Benzofuran derivatives
TW201710253A (zh) 抗雌激素化合物
BRPI0713743B1 (pt) Composto, pró-droga, e, composição farmacêutica
CN109265471B (zh) Fxr受体激动剂
CN111770924B (zh) 用于治疗乳腺癌的雌激素受体降解剂
JP2022537330A (ja) インダゾール誘導体、その製造方法及び医薬上のその使用
CN102791688A (zh) 雌激素受体配体
JP5947898B2 (ja) Fsh受容体アンタゴニスト
CN111615515A (zh) 杂环化合物、制备方法及其在医药上的应用
US20030130340A1 (en) Novel benzothiophene derivatives
EP2459551B1 (en) Dihydrobenzoindazoles
US8071589B2 (en) Dihydrobenzoindazoles
CN119948023A (zh) 含哌啶多环类衍生物调节剂、其制备方法和应用
JP4304732B2 (ja) エストロゲンレセプターβアイソフォーム活性化剤
US20160052937A1 (en) Tetrahydroimidazo[1,5-d][1,4]oxazepine compound
US10155259B2 (en) FSH receptor antagonists

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20161207

FZDE Dead

Effective date: 20200831