JP6016284B2 - ジスピロピロリジン誘導体の結晶 - Google Patents

ジスピロピロリジン誘導体の結晶 Download PDF

Info

Publication number
JP6016284B2
JP6016284B2 JP2014534398A JP2014534398A JP6016284B2 JP 6016284 B2 JP6016284 B2 JP 6016284B2 JP 2014534398 A JP2014534398 A JP 2014534398A JP 2014534398 A JP2014534398 A JP 2014534398A JP 6016284 B2 JP6016284 B2 JP 6016284B2
Authority
JP
Japan
Prior art keywords
crystal
powder
ray diffraction
wavelength
irradiation
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
JP2014534398A
Other languages
English (en)
Japanese (ja)
Other versions
JPWO2014038606A1 (ja
Inventor
祥子 吉田
祥子 吉田
杉本　雄一
雄一 杉本
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 JPWO2014038606A1 publication Critical patent/JPWO2014038606A1/ja
Application granted granted Critical
Publication of JP6016284B2 publication Critical patent/JP6016284B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/10—Spiro-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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2014534398A 2012-09-06 2013-09-05 ジスピロピロリジン誘導体の結晶 Active JP6016284B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2012195761 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
JPWO2014038606A1 JPWO2014038606A1 (ja) 2016-08-12
JP6016284B2 true JP6016284B2 (ja) 2016-10-26

Family

ID=50237214

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2014534398A Active JP6016284B2 (ja) 2012-09-06 2013-09-05 ジスピロピロリジン誘導体の結晶

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 (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2684880T3 (en) 2011-03-10 2018-05-22 Daiichi Sankyo Co Ltd DISPIROPYRROLIDINE DERIVATIVES
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
EP2935263B1 (en) 2012-12-20 2018-12-05 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
HK1245791A1 (zh) 2015-01-20 2018-08-31 阿尔维纳斯运营股份有限公司 用於雄激素受体的靶向降解的化合物和方法
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
EP3260119B1 (en) * 2015-02-20 2023-11-15 Daiichi Sankyo Company, Limited Combination method for treating cancer
US10485794B2 (en) 2015-04-13 2019-11-26 Daiichi Sankyo Company, Limited Treatment method by combined use of MDM2 inhibitor and BTK inhibitor
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
CN108137507A (zh) 2015-07-10 2018-06-08 阿尔维纳斯股份有限公司 基于mdm2的蛋白水解调节剂和相关的使用方法
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
WO2017069288A1 (en) 2015-10-23 2017-04-27 Daiichi Sankyo Company, Limited Pharmaceutical composition for use in treating aml and method of treating aml in a subject in need thereof
TW202332444A (zh) * 2015-10-23 2023-08-16 日商第一三共股份有限公司 用於治療癌症之醫藥組成物
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
EP3535265A4 (en) 2016-11-01 2020-07-08 Arvinas, Inc. PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE
WO2018102725A1 (en) 2016-12-01 2018-06-07 Arvinas, Inc. Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
RU2019121527A (ru) 2016-12-23 2021-01-15 Эрвинэс Оперейшнс, Инк. Химерные молекулы, нацеливающиеся на протеолиз egfr, и связанные с ними способы применения
EP3558994A4 (en) 2016-12-23 2021-05-12 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF FAST ACCELERATED FIBROSARCOMA POLYPEPTIDES
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
EP3559006A4 (en) 2016-12-23 2021-03-03 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF F TAL LIVER KINASE 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
MX2019008934A (es) 2017-01-26 2019-11-05 Arvinas Operations Inc Moduladores de la proteolisis del receptor de estrogeno y métodos asociados de uso,.
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
CN119569702A (zh) 2018-04-04 2025-03-07 阿尔维纳斯运营股份有限公司 蛋白水解调节剂及相关使用方法
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
ES3061133T3 (en) 2019-08-26 2026-03-31 Arvinas Operations Inc Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
AU2021342287A1 (en) 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
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
CN121419983A (zh) 2023-01-26 2026-01-27 阿尔维纳斯运营股份有限公司 基于小脑蛋白的kras降解protac及其相关用途
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
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
PL370909A1 (en) 2001-12-18 2005-05-30 F.Hoffmann-La Roche Ag Cis-imidazolines as mdm2 inhibitors
CN100486969C (zh) 2001-12-18 2009-05-13 霍夫曼-拉罗奇有限公司 顺式-2,4,5-三苯基-咪唑啉及其在肿瘤治疗中的应用
US7425638B2 (en) 2003-06-17 2008-09-16 Hoffmann-La Roche Inc. Cis-imidazolines
US7132421B2 (en) 2003-06-17 2006-11-07 Hoffmann-La Roche Inc. CIS-imidazoles
EP1753727B1 (en) 2004-05-18 2008-11-19 F.Hoffmann-La Roche Ag Novel cis-imidazolines
GB0419481D0 (en) 2004-09-02 2004-10-06 Cancer Rec Tech Ltd Isoindolin-1-one derivatives
AU2006216780B8 (en) * 2005-02-22 2010-04-22 The Regents Of The University Of Michigan Small molecule inhibitors of MDM2 and uses thereof
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
SG174107A1 (en) 2006-08-30 2011-09-29 Univ Michigan New small molecule inhibitors of mdm2 and the uses thereof
CN101516366B (zh) 2006-09-21 2012-05-30 霍夫曼-拉罗奇有限公司 作为抗癌剂的羟吲哚衍生物
US7638548B2 (en) 2006-11-09 2009-12-29 Hoffmann-La Roche Inc. Spiroindolinone derivatives
PE20081897A1 (es) 2007-03-29 2009-02-09 Novartis Ag 3-imidazolil-indoles para el tratamiento de enfermedades 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
TW201011009A (en) 2008-09-15 2010-03-16 Priaxon Ag Novel pyrrolidin-2-ones
US8354444B2 (en) 2008-09-18 2013-01-15 Hoffmann-La Roche Inc. Substituted pyrrolidine-2-carboxamides
CA2734363C (en) 2008-09-18 2016-10-25 F. Hoffmann-La Roche Ag Substituted pyrrolidine-2-carboxamides
CN102356085A (zh) 2009-01-16 2012-02-15 第一三共株式会社 具有脯氨酸环结构的咪唑并噻唑衍生物
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
JP2013510860A (ja) 2009-11-12 2013-03-28 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
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
CA2800519A1 (en) 2010-04-09 2011-10-13 The Regents Of The University Of Michigan Biomarkers for mdm2 inhibitors for use in treating disease
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
JP2013540850A (ja) 2010-09-08 2013-11-07 ビーエーエスエフ ソシエタス・ヨーロピア Ｎ−置換ジアゼニウムジオキシド及び／又はｎ’−ヒドロキシジアゼニウムオキシド塩を含有する水性研磨剤組成物
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
DK2684880T3 (en) 2011-03-10 2018-05-22 Daiichi Sankyo Co Ltd DISPIROPYRROLIDINE DERIVATIVES
ES2624808T3 (es) 2011-05-11 2017-07-17 The Regents Of The University Of Michigan Antagonistas de MDM2 espirooxindólicos
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
US20170081336A1 (en) 2017-03-23
CN104812757B (zh) 2016-11-09
EP2894156A4 (en) 2016-03-23
US20150210707A1 (en) 2015-07-30
US9745315B2 (en) 2017-08-29
RU2015112098A (ru) 2016-10-27
IN2015MN00464A (enExample) 2015-09-04
RU2647840C2 (ru) 2018-03-21
US20170081334A1 (en) 2017-03-23
TWI586668B (zh) 2017-06-11
US9540386B2 (en) 2017-01-10
US20180155355A1 (en) 2018-06-07
US9718830B2 (en) 2017-08-01
KR20150048140A (ko) 2015-05-06
US20170081335A1 (en) 2017-03-23
US9718831B2 (en) 2017-08-01
JPWO2014038606A1 (ja) 2016-08-12
CN104812757A (zh) 2015-07-29
US10023578B2 (en) 2018-07-17
ES2637150T3 (es) 2017-10-11
US10030030B2 (en) 2018-07-24
EP2894156A1 (en) 2015-07-15
BR112015004816A2 (pt) 2017-07-04
US20170081337A1 (en) 2017-03-23
CA2884238A1 (en) 2014-03-13
EP2894156B1 (en) 2017-05-17
BR112015004816B1 (pt) 2022-04-26
KR102217410B1 (ko) 2021-02-18
HK1210172A1 (en) 2016-04-15
WO2014038606A1 (ja) 2014-03-13
US20160244458A1 (en) 2016-08-25
TW201410681A (zh) 2014-03-16
US9884871B2 (en) 2018-02-06
US9359368B2 (en) 2016-06-07
US20180155356A1 (en) 2018-06-07
CA2884238C (en) 2017-10-03

Similar Documents

Publication Publication Date Title
JPWO2014038606A1 (ja) ジスピロピロリジン誘導体の結晶
CA2829188C (en) Dispiropyrrolidine derivatives
US9790212B2 (en) Enhancer of zeste homolog 2 inhibitors
KR20120113760A (ko) 정제된 피롤로퀴놀리닐-피롤리딘-2,5-디온 조성물 및 이의 제조 방법 및 사용 방법
KR20210046717A (ko) Ccr6 억제제로서 유용한 n-치환된-디옥소시클로부테닐아미노-3-히드록시-피콜린아미드
KR20110119641A (ko) 프롤린 고리 구조를 갖는 이미다조티아졸 유도체
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
HK1193818B (en) Dispiropyrrolidine derivative

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160616

A871 Explanation of circumstances concerning accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A871

Effective date: 20160616

A975 Report on accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A971005

Effective date: 20160829

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20160921

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20160923

R150 Certificate of patent or registration of utility model

Ref document number: 6016284

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: R3D02

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250