CA2884238C - Crystals of dispiropyrrolidine derivatives - Google Patents

Crystals of dispiropyrrolidine derivatives Download PDF

Info

Publication number
CA2884238C
CA2884238C CA2884238A CA2884238A CA2884238C CA 2884238 C CA2884238 C CA 2884238C CA 2884238 A CA2884238 A CA 2884238A CA 2884238 A CA2884238 A CA 2884238A CA 2884238 C CA2884238 C CA 2884238C
Authority
CA
Canada
Prior art keywords
crystal
ray powder
powder diffraction
diffraction pattern
angstroms
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.)
Active
Application number
CA2884238A
Other languages
English (en)
French (fr)
Other versions
CA2884238A1 (en
Inventor
Shoko Yoshida
Yuuichi Sugimoto
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.)
Daiichi Sankyo Co Ltd
Original Assignee
Daiichi Sankyo Co Ltd
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 Daiichi Sankyo Co Ltd filed Critical Daiichi Sankyo Co Ltd
Publication of CA2884238A1 publication Critical patent/CA2884238A1/en
Application granted granted Critical
Publication of CA2884238C publication Critical patent/CA2884238C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2884238A 2012-09-06 2013-09-05 Crystals of dispiropyrrolidine derivatives Active CA2884238C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2012195761 2012-09-06
JP2012-195761 2012-09-06
PCT/JP2013/073865 WO2014038606A1 (ja) 2012-09-06 2013-09-05 ジスピロピロリジン誘導体の結晶

Publications (2)

Publication Number Publication Date
CA2884238A1 CA2884238A1 (en) 2014-03-13
CA2884238C true CA2884238C (en) 2017-10-03

Family

ID=50237214

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2884238A Active CA2884238C (en) 2012-09-06 2013-09-05 Crystals of dispiropyrrolidine derivatives

Country Status (12)

Country Link
US (8) US9359368B2 (cg-RX-API-DMAC7.html)
EP (1) EP2894156B1 (cg-RX-API-DMAC7.html)
JP (1) JP6016284B2 (cg-RX-API-DMAC7.html)
KR (1) KR102217410B1 (cg-RX-API-DMAC7.html)
CN (1) CN104812757B (cg-RX-API-DMAC7.html)
BR (1) BR112015004816B1 (cg-RX-API-DMAC7.html)
CA (1) CA2884238C (cg-RX-API-DMAC7.html)
ES (1) ES2637150T3 (cg-RX-API-DMAC7.html)
IN (1) IN2015MN00464A (cg-RX-API-DMAC7.html)
RU (1) RU2647840C2 (cg-RX-API-DMAC7.html)
TW (1) TWI586668B (cg-RX-API-DMAC7.html)
WO (1) WO2014038606A1 (cg-RX-API-DMAC7.html)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI586668B (zh) 2012-09-06 2017-06-11 第一三共股份有限公司 二螺吡咯啶衍生物之結晶
RU2690663C2 (ru) 2012-12-20 2019-06-05 Мерк Шарп И Доум Корп. Замещенные имидазопиридины в качестве ингибиторов hdm2
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
AU2016209349B2 (en) 2015-01-20 2020-05-07 Arvinas, Inc. Compounds and methods for the targeted degradation of the Androgen Receptor
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
KR102595395B1 (ko) 2015-02-20 2023-10-27 다이이찌 산쿄 가부시키가이샤 암의 병용 치료법
EP3284466A4 (en) * 2015-04-13 2018-12-05 Daiichi Sankyo Company, Limited Treatment method combining mdm2 inhibitor and btk inhibitor
US20180147202A1 (en) 2015-06-05 2018-05-31 Arvinas, Inc. TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE
WO2017030814A1 (en) 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EP3364972A1 (en) * 2015-10-23 2018-08-29 Daiichi Sankyo Company, Limited Dosage regimen of mdm2 inhibitor for treating cancers
CN108135884A (zh) * 2015-10-23 2018-06-08 第三共株式会社 用于治疗aml的药物组合物和治疗有此需要的对象中的aml的方法
JP2019522633A (ja) 2016-05-20 2019-08-15 ジェネンテック, インコーポレイテッド Protac抗体コンジュゲート及び使用方法
IL290809B2 (en) 2016-11-01 2024-01-01 Arvinas Operations Inc Tau-protein targeting protacs and associated methods of use
WO2018102725A1 (en) 2016-12-01 2018-06-07 Arvinas, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
WO2018119448A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
CA3047586A1 (en) 2016-12-23 2018-06-28 Arvinas Operations, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
EP3573977A4 (en) 2017-01-26 2020-12-23 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
WO2019099926A1 (en) 2017-11-17 2019-05-23 Arvinas, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
BR112020020307A2 (pt) 2018-04-04 2021-01-12 Arvinas Operations, Inc. Moduladores de proteólise e métodos de uso associados
EP3841100A1 (en) 2018-08-20 2021-06-30 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
AU2020336309A1 (en) 2019-08-26 2022-03-17 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
JP2023539663A (ja) 2020-08-28 2023-09-15 アルビナス・オペレーションズ・インコーポレイテッド 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法
TW202214236A (zh) 2020-09-14 2022-04-16 美商亞文納營運公司 用於靶向降解雌激素受體之化合物之結晶及非晶形形式
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same
EP4584258A1 (en) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
KR20250151412A (ko) 2023-01-26 2025-10-21 아비나스 오퍼레이션스, 인코포레이티드 세레블론계 kras 분해 단백질 및 이와 관련된 용도
WO2024240858A1 (en) 2023-05-23 2024-11-28 Valerio Therapeutics Protac molecules directed against dna damage repair system and uses thereof

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6740495B1 (en) 2000-04-03 2004-05-25 Rigel Pharmaceuticals, Inc. Ubiquitin ligase assay
US6979551B2 (en) 2000-04-03 2005-12-27 Rigel Pharmaceuticals, Inc. Assays for identifying ubiquitin agents and for identifying agents that modify the activity of ubiquitin agents
JP4361798B2 (ja) 2001-12-18 2009-11-11 エフ.ホフマン−ラ ロシュ アーゲー Mdm2インヒビターとしてのシス−イミダゾリン
CA2469187C (en) 2001-12-18 2012-07-17 F. Hoffmann-La Roche Ag Cis-2,4,5-triphenyl-imidazolines and their use in the treatment of tumors
US7132421B2 (en) 2003-06-17 2006-11-07 Hoffmann-La Roche Inc. CIS-imidazoles
US7425638B2 (en) 2003-06-17 2008-09-16 Hoffmann-La Roche Inc. Cis-imidazolines
CN1953965B (zh) 2004-05-18 2012-07-04 霍夫曼-拉罗奇有限公司 新型顺式咪唑啉类化合物
GB0419481D0 (en) 2004-09-02 2004-10-06 Cancer Rec Tech Ltd Isoindolin-1-one derivatives
EA014445B1 (ru) * 2005-02-22 2010-12-30 Дзе Риджентс Оф Дзе Юниверсити Оф Мичиган Низкомолекулярные ингибиторы mdm2 и их применения
US7576082B2 (en) 2005-06-24 2009-08-18 Hoffman-La Roche Inc. Oxindole derivatives
AR059265A1 (es) * 2006-02-07 2008-03-19 Astrazeneca Ab Compuestos espiro condensados con actividad inhibitoria en el receptor vaniloide1 (vr1)
US20070213341A1 (en) 2006-03-13 2007-09-13 Li Chen Spiroindolinone derivatives
CA2644758A1 (en) 2006-03-13 2007-09-20 F. Hoffmann-La Roche Ag Spiroindolinone derivatives
ZA200901224B (en) 2006-08-30 2010-05-26 Univ Michigan New small molecule inhibitors of MDM2 the uses thereof
JP2010504298A (ja) 2006-09-21 2010-02-12 エフ.ホフマン−ラ ロシュ アーゲー オキシンドール誘導体
US7638548B2 (en) 2006-11-09 2009-12-29 Hoffmann-La Roche Inc. Spiroindolinone derivatives
BRPI0810082A2 (pt) 2007-03-29 2014-10-21 Novartis Ag 3-imidazolil-indóis para o tratamento de doenças proliferativas
US7553833B2 (en) 2007-05-17 2009-06-30 Hoffmann-La Roche Inc. 3,3-spiroindolinone derivatives
US7834179B2 (en) 2007-05-23 2010-11-16 Hoffmann-La Roche Inc. Spiroindolinone derivatives
US8134001B2 (en) 2007-12-14 2012-03-13 Hoffmann-La Roche Inc. Spiroindolinone derivatives
US7776875B2 (en) 2007-12-19 2010-08-17 Hoffman-La Roche Inc. Spiroindolinone derivatives
US7723372B2 (en) 2008-03-19 2010-05-25 Hoffman-La Roche Inc. Spiroindolinone derivatives
AR073578A1 (es) 2008-09-15 2010-11-17 Priaxon Ag Pirrolidin-2-onas
US8354444B2 (en) 2008-09-18 2013-01-15 Hoffmann-La Roche Inc. Substituted pyrrolidine-2-carboxamides
RS52660B (sr) 2008-09-18 2013-06-28 F. Hoffmann-La Roche Ag Supstituisani pirolidin-2-karboksamidi
JP5520236B2 (ja) 2009-01-16 2014-06-11 第一三共株式会社 プロリン環構造を有するイミダゾチアゾール誘導体
US20100190814A1 (en) 2009-01-26 2010-07-29 Li Chen Spiroindolinone derivative prodrugs
US7928233B2 (en) 2009-02-10 2011-04-19 Hoffmann-La Roche Inc. Spiroindolinone pyridine derivatives
US8217051B2 (en) 2009-02-17 2012-07-10 Hoffmann-La Roche Inc. Spiroindolinone derivatives
US8076482B2 (en) * 2009-04-23 2011-12-13 Hoffmann-La Roche Inc. 3,3′-spiroindolinone derivatives
US8017607B2 (en) 2009-10-14 2011-09-13 Hoffmann-La Roche Inc. N-substituted-pyrrolidines as inhibitors of MDM2-P-53 interactions
UA107814C2 (uk) 2009-11-12 2015-02-25 Дзе Ріджентс Оф Дзе Юніверсіті Оф Мічіган Спірооксіндольні антагоністи мdм2
US20110118283A1 (en) 2009-11-17 2011-05-19 Qingjie Ding Substituted Pyrrolidine-2-Carboxamides
US8088815B2 (en) 2009-12-02 2012-01-03 Hoffman-La Roche Inc. Spiroindolinone pyrrolidines
US8288431B2 (en) 2010-02-17 2012-10-16 Hoffmann-La Roche Inc. Substituted spiroindolinones
KR20130050938A (ko) 2010-04-09 2013-05-16 더 리젠츠 오브 더 유니버시티 오브 미시건 질환 치료시 사용하기 위한 mdm2 억제제에 대한 바이오마커
US8217044B2 (en) 2010-04-28 2012-07-10 Hoffmann-La Roche Inc. Spiroindolinone pyrrolidines
US20120010235A1 (en) 2010-07-12 2012-01-12 Xin-Jie Chu N-substituted pyrrolidines
US20120046306A1 (en) 2010-08-18 2012-02-23 David Joseph Bartkovitz Substituted Heteroaryl Spiropyrrolidine MDM2 Antagonists
US20130200039A1 (en) 2010-09-08 2013-08-08 Basf Se Aqueous polishing compositions containing n-substituted diazenium dioxides and/or n'-hydroxy-diazenium oxide salts
US20120065210A1 (en) 2010-09-15 2012-03-15 Xin-Jie Chu Substituted hexahydropyrrolo[1,2-c]imidazolones
US20120071499A1 (en) 2010-09-20 2012-03-22 Xin-Jie Chu Substituted Spiro[3H-Indole-3,6'(5'H)-[1H]Pyrrolo[1,2c]Imidazole-1',2(1H,2'H)-diones
WO2012076513A1 (en) 2010-12-09 2012-06-14 F. Hoffmann-La Roche Ag 3-cyano-1-hydroxymethyl-2-phenylpyrrolidine derivatives as inhibitors of mdm2-p53 interactions useful for the treatment of cancer
MY172862A (en) * 2011-03-10 2019-12-13 Daiichi Sankyo Co Ltd Dispiropyrrolidine derivatives
CN103717605B (zh) * 2011-05-11 2016-05-18 密执安州立大学董事会 螺-羟吲哚mdm2拮抗剂
TWI586668B (zh) 2012-09-06 2017-06-11 第一三共股份有限公司 二螺吡咯啶衍生物之結晶

Also Published As

Publication number Publication date
CN104812757A (zh) 2015-07-29
US9359368B2 (en) 2016-06-07
US20180155355A1 (en) 2018-06-07
RU2647840C2 (ru) 2018-03-21
ES2637150T3 (es) 2017-10-11
EP2894156A1 (en) 2015-07-15
US20150210707A1 (en) 2015-07-30
US9884871B2 (en) 2018-02-06
KR102217410B1 (ko) 2021-02-18
KR20150048140A (ko) 2015-05-06
US20170081335A1 (en) 2017-03-23
HK1210172A1 (en) 2016-04-15
US20160244458A1 (en) 2016-08-25
US9540386B2 (en) 2017-01-10
EP2894156B1 (en) 2017-05-17
US20170081336A1 (en) 2017-03-23
BR112015004816B1 (pt) 2022-04-26
CA2884238A1 (en) 2014-03-13
US10030030B2 (en) 2018-07-24
JP6016284B2 (ja) 2016-10-26
TW201410681A (zh) 2014-03-16
US10023578B2 (en) 2018-07-17
US20170081337A1 (en) 2017-03-23
WO2014038606A1 (ja) 2014-03-13
IN2015MN00464A (cg-RX-API-DMAC7.html) 2015-09-04
RU2015112098A (ru) 2016-10-27
BR112015004816A2 (pt) 2017-07-04
CN104812757B (zh) 2016-11-09
US9718831B2 (en) 2017-08-01
US9745315B2 (en) 2017-08-29
JPWO2014038606A1 (ja) 2016-08-12
TWI586668B (zh) 2017-06-11
EP2894156A4 (en) 2016-03-23
US9718830B2 (en) 2017-08-01
US20170081334A1 (en) 2017-03-23
US20180155356A1 (en) 2018-06-07

Similar Documents

Publication Publication Date Title
CA2884238C (en) Crystals of dispiropyrrolidine derivatives
CN105753872B (zh) 二螺吡咯烷衍生物
WO2023141300A1 (en) Heterocyclic compounds and uses thereof
CA3024180A1 (en) Inhibitors of the menin-mll interaction
JP2018529682A (ja) イソキノリノン誘導体の固体形態、それを製造する方法、それを含む組成物、及びそれを使用する方法
EP3347351B1 (en) Salts of a pim kinase inhibitor
KR20120113760A (ko) 정제된 피롤로퀴놀리닐-피롤리딘-2,5-디온 조성물 및 이의 제조 방법 및 사용 방법
CN111093651A (zh) Ido抑制剂的无定形和结晶形式
WO2019070167A1 (ru) Ингибиторы рецептора эпидермального фактора роста
EP3101020B1 (en) Deuterated quinazolinone compound and pharmaceutical composition comprising same
TW202523326A (zh) 雜環及其用途
HK1210172B (en) Crystal of dispiropyrrolidine derivative
JPWO2012026433A1 (ja) 三環性ピラゾロピリミジン誘導体のフリー体結晶
CN104557955A (zh) 作为PI3K/mTOR抑制剂的三环类化合物,其制备方法和用途

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20150306