JP2022520382A - Ｒｓｋ阻害剤の結晶形態 - Google Patents

Ｒｓｋ阻害剤の結晶形態 Download PDF

Info

Publication number
JP2022520382A
JP2022520382A JP2021546803A JP2021546803A JP2022520382A JP 2022520382 A JP2022520382 A JP 2022520382A JP 2021546803 A JP2021546803 A JP 2021546803A JP 2021546803 A JP2021546803 A JP 2021546803A JP 2022520382 A JP2022520382 A JP 2022520382A
Authority
JP
Japan
Prior art keywords
theta
compound
crystal form
cancer
crystalline
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.)
Pending
Application number
JP2021546803A
Other languages
English (en)
Japanese (ja)
Other versions
JP2022520382A5 (https=
JPWO2020165646A5 (https=
Inventor
ウィニーク，リチャード
マクファーソン，エレイン
フラハイブ，エリック
ダン，サンドラ，イー．
ローアリー，ジョナサン
Original Assignee
フェニックス モレキュラー デザインズ
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 フェニックス モレキュラー デザインズ filed Critical フェニックス モレキュラー デザインズ
Publication of JP2022520382A publication Critical patent/JP2022520382A/ja
Publication of JP2022520382A5 publication Critical patent/JP2022520382A5/ja
Publication of JPWO2020165646A5 publication Critical patent/JPWO2020165646A5/ja
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-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
    • A61K31/495—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Epidemiology (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2021546803A 2019-02-11 2020-02-10 Ｒｓｋ阻害剤の結晶形態 Pending JP2022520382A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962804076P 2019-02-11 2019-02-11
US62/804,076 2019-02-11
PCT/IB2020/000092 WO2020165646A1 (en) 2019-02-11 2020-02-10 Crystalline forms of an rsk inhibitor

Publications (3)

Publication Number Publication Date
JP2022520382A true JP2022520382A (ja) 2022-03-30
JP2022520382A5 JP2022520382A5 (https=) 2023-02-20
JPWO2020165646A5 JPWO2020165646A5 (https=) 2023-02-20

Family

ID=72043971

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021546803A Pending JP2022520382A (ja) 2019-02-11 2020-02-10 Ｒｓｋ阻害剤の結晶形態

Country Status (9)

Country Link
US (1) US12378245B2 (https=)
EP (1) EP3924352A4 (https=)
JP (1) JP2022520382A (https=)
KR (1) KR20210126077A (https=)
CN (1) CN113677681A (https=)
AU (1) AU2020222056A1 (https=)
CA (1) CA3129722A1 (https=)
IL (1) IL285493A (https=)
WO (1) WO2020165646A1 (https=)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12378245B2 (en) 2019-02-11 2025-08-05 Phoenix Molecular Designs Crystalline forms of an RSK inhibitor
CN117186098A (zh) * 2022-06-07 2023-12-08 上海科恩泰生物医药科技有限公司 一种具有rsk抑制作用的羧酰胺衍生物、包含其的药物组合物及其用途
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017141116A1 (en) * 2016-02-19 2017-08-24 Phoenix Molecular Designs Carboxamide derivatives useful as rsk inhibitors

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
AU4652697A (en) 1996-10-08 1998-05-05 Eli Lilly And Company New serotonin 5-ht1f agonists
ZA979961B (en) 1996-11-15 1999-05-05 Lilly Co Eli 5-HT1F agonists
EP0981327B1 (en) 1997-05-07 2002-11-06 Galen (Chemicals) Limited Intravaginal drug delivery devices for the administration of testosterone and testosterone precursors
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
WO2003087087A2 (en) 2002-04-09 2003-10-23 Astex Technology Limited Heterocyclic compounds and their use as modulators of p38 map kinase
US20050032869A1 (en) 2003-07-08 2005-02-10 Pharmacia Italia S.P.A. Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
RS56037B1 (sr) 2004-06-24 2017-09-29 Vertex Pharma Modulatori atp-vezujućih kasetnih transportera
US7790712B2 (en) 2005-03-17 2010-09-07 Boehringer Ingelheim Pharmaceutical, Inc. Substituted [1,4]diazepino[1,2-A]indoles and azepino[1,2-A]indoles as anti-cytokine inhibitors
FR2884516B1 (fr) 2005-04-15 2007-06-22 Cerep Sa Antagonistes npy, preparation et utilisations
ATE482958T1 (de) * 2005-08-09 2010-10-15 Irm Llc Verbindungen und zusammensetzungen als proteinkinaseinhibitoren
US8765802B2 (en) 2007-06-12 2014-07-01 Provid Pharmaceuticals, Inc. Kinase inhibitors, compositions thereof, and methods of use therewith
EP2200977B1 (en) 2007-09-14 2016-11-09 The Regents of the University of Michigan F1f0-atpase inhibitors and related methods
GB0718870D0 (en) 2007-09-27 2007-11-07 Univ Dundee Modulation of RSK
EP2461869B1 (en) * 2009-08-06 2013-08-21 Merck Patent GmbH Novel bicyclic urea compounds
EP2509980A1 (en) 2009-12-07 2012-10-17 Boehringer Ingelheim International GmbH Heterocyclic compounds containing an indole core
US9073926B2 (en) 2009-12-07 2015-07-07 Boehringer Ingelheim International Gmbh Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
DK2676137T3 (en) 2011-02-17 2015-01-19 Nestec Sa TESTS TO DETECT AUTO ANTIBODIES FOR ANTI-TNF PHARMACEUTICALS
WO2013181742A1 (en) 2012-06-04 2013-12-12 Phoenix Molecular Diagnostics Ltd. Methods of inhibiting rsk for treatment of breast cancer
CN103724251B (zh) 2014-01-18 2015-07-22 福州大学 一种靶向stat3的小分子化合物及其制备方法和应用
US9856258B2 (en) 2014-04-07 2018-01-02 Netherlands Translational Research Center B.V. (5,6-dihydro)pyrimido[4,5-E]indolizines
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
JP2018537486A (ja) * 2015-12-14 2018-12-20 センワ バイオサイエンシズ インコーポレイテッド キノロン類似体及びその塩の結晶形
US12378245B2 (en) 2019-02-11 2025-08-05 Phoenix Molecular Designs Crystalline forms of an RSK inhibitor

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017141116A1 (en) * 2016-02-19 2017-08-24 Phoenix Molecular Designs Carboxamide derivatives useful as rsk inhibitors

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
川口洋子ら: "医薬品と結晶多形", 生活工学研究, vol. 4, no. 2, JPN6014015069, 2002, pages 310 - 317, ISSN: 0005345920 *
平山令明, 有機化合物結晶作製ハンドブック, JPN6014035600, 2008, pages 17 - 23, ISSN: 0005345919 *
芦澤一英, 医薬品の多形現象と晶析の化学, JPN6015027444, 2002, pages 273 - 278, ISSN: 0005345921 *

Also Published As

Publication number Publication date
US20220112193A1 (en) 2022-04-14
CN113677681A (zh) 2021-11-19
US12378245B2 (en) 2025-08-05
EP3924352A4 (en) 2022-11-16
KR20210126077A (ko) 2021-10-19
AU2020222056A1 (en) 2021-10-07
IL285493A (en) 2021-09-30
WO2020165646A1 (en) 2020-08-20
EP3924352A1 (en) 2021-12-22
CA3129722A1 (en) 2020-08-20

Similar Documents

Publication Publication Date Title
JP2022520382A (ja) Ｒｓｋ阻害剤の結晶形態
US11919904B2 (en) Sulfonylamide compounds as CDK2 inhibitors
US11866432B2 (en) Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US9498467B2 (en) Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
ES2883285T3 (es) Antagonistas de tlr7/8 y sus usos
JP2019505541A (ja) Ｒｓｋ阻害剤として有用なカルボキサミド誘導体
KR20160012195A (ko) Bet 억제제로서의 피라졸로-피롤리딘-4-온 유도체 및 질환의 치료에서의 그의 용도
US9884874B2 (en) Bromodomain-inhibiting compounds and pharmaceutical composition comprising same for preventing or treating a cancer
KR20160012197A (ko) 피라졸로-피롤리딘-4-온 유도체 및 질환의 치료에서의 그의 용도
JP2022136163A (ja) Ｄｎａ損傷剤とｄｎａ－ｐｋ阻害剤との組合せ物を使用する、がんを処置するための方法
JP7758369B2 (ja) Ｇａｓ４１阻害剤及びその使用方法
CA3173679A1 (en) Inhibitors of the peptidyl-prolyl cis/trans isomerase (pin1) and uses thereof
US12084453B2 (en) Bicyclic amines as CDK12 inhibitors
WO2018028491A1 (zh) 吲哚胺2，3-双加氧酶抑制剂及其在药学中的用途
US20250353842A1 (en) Bicyclic amine cdk12 inhibitors
CN103328461A (zh) 使用渥曼青霉素类似物的结晶形式的组合物及方法
CA3038657C (en) Method for treating cancer using a combination of dna-damaging agents and dna-pk inhibitors
HK40095494A (zh) 作为vhl抑制剂用於治疗贫血的1-(2-(4-环丙基-1h-1，2，3-三唑-1-基)乙酰基)-4-羟基吡咯烷-2-甲酰胺衍生物
US20260070915A1 (en) Substituted 7h-pyrrolo[2,3-d]pyrimidin-2-amines as selective cdk2/4 inhibitors
US20260098044A1 (en) Tricyclic heteroaryl compounds as inhibitors of tyk2 and/or jak1
HK40092810A (zh) 作为vhl抑制剂用於治疗贫血和癌症的1-(2-(4-环丙基-1h-1，2，3-三唑-1-基)乙酰基)-4-羟基-n-(苄基)吡咯烷-2-甲酰胺衍生物
WO2025036479A1 (zh) 驱动蛋白kif18a抑制剂及其应用
CN108424414A (zh) 一类含杂环的吲哚胺2，3-双加氧酶调节化合物及其在药学中的用途
CN108424415A (zh) 一类吲哚胺2，3-双加氧酶调节化合物及其在药学中的用途
HK40043591B (zh) 用作ii型irak抑制剂的杂芳基化合物及其用途

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211020

RD12 Notification of acceptance of power of sub attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7432

Effective date: 20221222

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20221222

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230209

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20230209

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20230704

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20230704

RD14 Notification of resignation of power of sub attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7434

Effective date: 20230704

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20230704

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20240122

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20240125

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240422

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20240612