KR102217410B1 - 디스피로피롤리딘 유도체의 결정 - Google Patents

디스피로피롤리딘 유도체의 결정 Download PDF

Info

Publication number
KR102217410B1
KR102217410B1 KR1020157005386A KR20157005386A KR102217410B1 KR 102217410 B1 KR102217410 B1 KR 102217410B1 KR 1020157005386 A KR1020157005386 A KR 1020157005386A KR 20157005386 A KR20157005386 A KR 20157005386A KR 102217410 B1 KR102217410 B1 KR 102217410B1
Authority
KR
South Korea
Prior art keywords
crystal
ray diffraction
powder
chloro
wavelength
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
KR1020157005386A
Other languages
English (en)
Korean (ko)
Other versions
KR20150048140A (ko
Inventor
쇼코 요시다
유우이치 스기모토
Original Assignee
다이이찌 산쿄 가부시키가이샤
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 다이이찌 산쿄 가부시키가이샤 filed Critical 다이이찌 산쿄 가부시키가이샤
Publication of KR20150048140A publication Critical patent/KR20150048140A/ko
Application granted granted Critical
Publication of KR102217410B1 publication Critical patent/KR102217410B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • 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)
KR1020157005386A 2012-09-06 2013-09-05 디스피로피롤리딘 유도체의 결정 Active KR102217410B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JPJP-P-2012-195761 2012-09-06
JP2012195761 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
KR20150048140A KR20150048140A (ko) 2015-05-06
KR102217410B1 true KR102217410B1 (ko) 2021-02-18

Family

ID=50237214

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020157005386A Active KR102217410B1 (ko) 2012-09-06 2013-09-05 디스피로피롤리딘 유도체의 결정

Country Status (12)

Country Link
US (8) US9359368B2 (enExample)
EP (1) EP2894156B1 (enExample)
JP (1) JP6016284B2 (enExample)
KR (1) KR102217410B1 (enExample)
CN (1) CN104812757B (enExample)
BR (1) BR112015004816B1 (enExample)
CA (1) CA2884238C (enExample)
ES (1) ES2637150T3 (enExample)
IN (1) IN2015MN00464A (enExample)
RU (1) RU2647840C2 (enExample)
TW (1) TWI586668B (enExample)
WO (1) WO2014038606A1 (enExample)

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
CA2895504A1 (en) 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as hdm2 inhibitors
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
KR102564925B1 (ko) 2015-01-20 2023-08-07 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법
CA2976752C (en) * 2015-02-20 2019-12-17 Daiichi Sankyo Company, Limited Method for treating cancer by combined use
WO2016167236A1 (ja) 2015-04-13 2016-10-20 第一三共株式会社 Mdm2阻害剤とbtk阻害剤との併用治療法
EP3302482A4 (en) 2015-06-05 2018-12-19 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
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
TWI806822B (zh) * 2015-10-23 2023-07-01 日商第一三共股份有限公司 製備治療癌症之醫藥組成物之用途
CN118436801A (zh) 2016-05-20 2024-08-06 豪夫迈·罗氏有限公司 Protac抗体缀合物及其使用方法
CA3042260C (en) 2016-11-01 2023-10-03 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
RS64976B1 (sr) 2016-12-01 2024-01-31 Arvinas Operations Inc Derivati tetrahidronaftalena i tetrahidroizohinolina kao degradatori estrogenih receptora
CN110741004B (zh) 2016-12-23 2023-10-17 阿尔维纳斯运营股份有限公司 用于迅速加速性纤维肉瘤多肽的靶向降解的化合物和方法
JP2020505327A (ja) 2016-12-23 2020-02-20 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Egfrタンパク質分解標的化キメラ分子およびその関連する使用方法
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
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
AU2018211975B2 (en) 2017-01-26 2022-05-26 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, 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
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
CN114667147B (zh) 2019-08-26 2024-09-06 阿尔维纳斯运营股份有限公司 用四氢萘衍生物作为雌激素受体降解剂的治疗乳腺癌的方法
US12180193B2 (en) 2020-08-28 2024-12-31 Arvinas Operations, Inc. Accelerating fibrosarcoma protein degrading compounds and associated methods of use
CR20230162A (es) 2020-09-14 2023-06-02 Arvinas Operations Inc Formas cristalinas y amorfas de un compuesto para la degradación dirigida del receptor de estrógenos
WO2023056069A1 (en) 2021-09-30 2023-04-06 Angiex, Inc. Degrader-antibody conjugates and methods of using same
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
EP4655073A2 (en) 2023-01-26 2025-12-03 Arvinas Operations, Inc. Cereblon-based kras degrading protacs ans uses related thereto
WO2024240858A1 (en) 2023-05-23 2024-11-28 Valerio Therapeutics Protac molecules directed against dna damage repair system and uses thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101779644B1 (ko) 2011-03-10 2017-09-18 다이이찌 산쿄 가부시키가이샤 디스피로피롤리딘 유도체

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US6740495B1 (en) 2000-04-03 2004-05-25 Rigel Pharmaceuticals, Inc. Ubiquitin ligase assay
RU2312101C2 (ru) 2001-12-18 2007-12-10 Ф.Хоффманн-Ля Рош Аг Цис-имидазолины в качестве ингибиторов mdm2
EP1458380B1 (en) 2001-12-18 2008-03-19 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
RU2006144811A (ru) 2004-05-18 2008-06-27 Ф.Хоффманн-Ля Рош Аг (Ch) Новые цис-имидазолины
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)
KR101052706B1 (ko) 2006-03-13 2011-08-01 에프. 호프만-라 로슈 아게 스피로인돌리논 유도체
US20070213341A1 (en) 2006-03-13 2007-09-13 Li Chen Spiroindolinone derivatives
CA2661354C (en) 2006-08-30 2012-12-18 The Regents Of The University Of Michigan New small molecule inhibitors of mdm2 and the uses thereof
ES2342854T3 (es) 2006-09-21 2010-07-15 F. Hoffmann-La Roche Ag Derivados de oxindol como agentes anticancerosos.
US7638548B2 (en) 2006-11-09 2009-12-29 Hoffmann-La Roche Inc. Spiroindolinone derivatives
AU2008234954B9 (en) 2007-03-29 2012-02-02 Novartis Ag 3-imidazolyl-indoles for the treatment of proliferative diseases
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
AU2009294673B2 (en) 2008-09-18 2014-08-14 F. Hoffmann-La Roche Ag Substituted pyrrolidine-2-carboxamides
EP2380892B1 (en) 2009-01-16 2014-04-02 Daiichi Sankyo Company, Limited Imidazothiazole derivative having proline ring structure
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
BR112012011317A2 (pt) 2009-11-12 2019-09-24 Univ Michigan Regents antagonistas espiro-oxindóis de mdm2
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
CN103153302A (zh) 2010-04-09 2013-06-12 密歇根大学董事会 针对用于治疗疾病的mdm2抑制剂的生物标记
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
JP2014513699A (ja) 2011-05-11 2014-06-05 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン スピロ−オキシインドールmdm2アンタゴニスト
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101779644B1 (ko) 2011-03-10 2017-09-18 다이이찌 산쿄 가부시키가이샤 디스피로피롤리딘 유도체

Also Published As

Publication number Publication date
US20180155355A1 (en) 2018-06-07
CN104812757A (zh) 2015-07-29
ES2637150T3 (es) 2017-10-11
BR112015004816A2 (pt) 2017-07-04
HK1210172A1 (en) 2016-04-15
US20170081335A1 (en) 2017-03-23
RU2015112098A (ru) 2016-10-27
US20170081337A1 (en) 2017-03-23
CA2884238A1 (en) 2014-03-13
US9359368B2 (en) 2016-06-07
US9718830B2 (en) 2017-08-01
US20150210707A1 (en) 2015-07-30
WO2014038606A1 (ja) 2014-03-13
TWI586668B (zh) 2017-06-11
JP6016284B2 (ja) 2016-10-26
IN2015MN00464A (enExample) 2015-09-04
TW201410681A (zh) 2014-03-16
JPWO2014038606A1 (ja) 2016-08-12
US20170081336A1 (en) 2017-03-23
CN104812757B (zh) 2016-11-09
US9745315B2 (en) 2017-08-29
RU2647840C2 (ru) 2018-03-21
KR20150048140A (ko) 2015-05-06
US9718831B2 (en) 2017-08-01
US20160244458A1 (en) 2016-08-25
EP2894156A1 (en) 2015-07-15
US9884871B2 (en) 2018-02-06
BR112015004816B1 (pt) 2022-04-26
US20180155356A1 (en) 2018-06-07
US9540386B2 (en) 2017-01-10
US10030030B2 (en) 2018-07-24
US10023578B2 (en) 2018-07-17
US20170081334A1 (en) 2017-03-23
CA2884238C (en) 2017-10-03
EP2894156B1 (en) 2017-05-17
EP2894156A4 (en) 2016-03-23

Similar Documents

Publication Publication Date Title
KR102217410B1 (ko) 디스피로피롤리딘 유도체의 결정
KR101779644B1 (ko) 디스피로피롤리딘 유도체
EP3378861B1 (en) Acrylic acid derivative, preparation method and use in medicine thereof
KR20250060956A (ko) 헤테로환 화합물 및 이의 용도
KR20120113760A (ko) 정제된 피롤로퀴놀리닐-피롤리딘-2,5-디온 조성물 및 이의 제조 방법 및 사용 방법
KR20110119641A (ko) 프롤린 고리 구조를 갖는 이미다조티아졸 유도체
KR20110131190A (ko) 3 고리성 피라졸로피리미딘 유도체
JP5701884B2 (ja) 三環性ピラゾロピリミジン誘導体の結晶
HK1210172B (en) Crystal of dispiropyrrolidine derivative
EP3845534A1 (en) Salt form and crystal form of novel azatricyclic compound and use thereof
KR20130099006A (ko) 3 고리성 피라졸로피리미딘 유도체의 프리체 결정

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20150302

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20180510

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20200211

Patent event code: PE09021S01D

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20200701

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20201111

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20210215

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20210215

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20240125

Start annual number: 4

End annual number: 4

PR1001 Payment of annual fee

Payment date: 20250123

Start annual number: 5

End annual number: 5