CA2867918C - Compounds and methods for kinase modulation, and indications therefor - Google Patents

Compounds and methods for kinase modulation, and indications therefor Download PDF

Info

Publication number
CA2867918C
CA2867918C CA2867918A CA2867918A CA2867918C CA 2867918 C CA2867918 C CA 2867918C CA 2867918 A CA2867918 A CA 2867918A CA 2867918 A CA2867918 A CA 2867918A CA 2867918 C CA2867918 C CA 2867918C
Authority
CA
Canada
Prior art keywords
pyridin
ylmethyl
fluoro
amine
pyrrolo
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
CA2867918A
Other languages
English (en)
French (fr)
Other versions
CA2867918A1 (en
Inventor
Gideon Bollag
Klaus-Peter Hirth
Prabha N. Ibrahim
Paul Lin
Brian West
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 Inc
Original Assignee
Plexxikon Inc
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 Plexxikon Inc filed Critical Plexxikon Inc
Publication of CA2867918A1 publication Critical patent/CA2867918A1/en
Application granted granted Critical
Publication of CA2867918C publication Critical patent/CA2867918C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
CA2867918A 2012-03-19 2013-03-18 Compounds and methods for kinase modulation, and indications therefor Active CA2867918C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201261612912P 2012-03-19 2012-03-19
US61/612,912 2012-03-19
US201361754318P 2013-01-18 2013-01-18
US61/754,318 2013-01-18
US13/802,106 US9358235B2 (en) 2012-03-19 2013-03-13 Kinase modulation, and indications therefor
US13/802,106 2013-03-13
PCT/US2013/032835 WO2013142427A1 (en) 2012-03-19 2013-03-18 Compounds and methods for kinase modulation, and indications therefor

Publications (2)

Publication Number Publication Date
CA2867918A1 CA2867918A1 (en) 2013-09-26
CA2867918C true CA2867918C (en) 2020-05-05

Family

ID=48045777

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2867918A Active CA2867918C (en) 2012-03-19 2013-03-18 Compounds and methods for kinase modulation, and indications therefor

Country Status (16)

Country Link
US (3) US9358235B2 (https=)
EP (2) EP4295912A3 (https=)
JP (1) JP6165837B2 (https=)
KR (2) KR20140144229A (https=)
CN (1) CN104703623B (https=)
AU (2) AU2013235298A1 (https=)
BR (1) BR112014023162A8 (https=)
CA (1) CA2867918C (https=)
EA (1) EA029676B1 (https=)
HK (1) HK1204995A1 (https=)
IL (1) IL234702A (https=)
MY (1) MY176903A (https=)
NZ (1) NZ630483A (https=)
SG (2) SG11201405764YA (https=)
WO (1) WO2013142427A1 (https=)
ZA (1) ZA201407580B (https=)

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
JP2010533729A (ja) 2007-07-17 2010-10-28 プレキシコン，インコーポレーテッド キナーゼ調節のための化合物と方法、及びそのための適応
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
KR101739994B1 (ko) 2009-04-03 2017-05-25 에프. 호프만-라 로슈 아게 프로판-１-술폰산 ｛３-［５-（４-클로로-페닐）-１Ｈ-피롤로［２，３-ｂ］피리딘-３-카르보닐］-２，４-디플루오로-페닐｝-아미드 조성물 및 그의 용도
NZ599866A (en) 2009-11-06 2014-09-26 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
US8673928B2 (en) 2009-11-18 2014-03-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN102753549A (zh) 2009-12-23 2012-10-24 普莱希科公司 用于激酶调节的化合物和方法及其适应症
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
KR101911972B1 (ko) 2011-02-07 2018-10-25 플렉시콘 인코퍼레이티드 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
AU2012255275B2 (en) 2011-05-17 2016-01-28 Plexxikon Inc. Kinase modulation and indications therefor
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
MX2015002887A (es) 2012-09-06 2015-07-06 Plexxikon Inc Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello.
EP2935248B1 (en) 2012-12-21 2018-02-28 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
SG11201506687RA (en) 2013-03-15 2015-09-29 Plexxikon Inc Heterocyclic compounds and uses thereof
EP3004060B1 (en) 2013-05-30 2019-11-27 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
CN104710417B (zh) * 2013-12-11 2020-09-08 上海科州药物研发有限公司 氮杂吲哚类衍生物及其合成方法
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US11331312B2 (en) * 2014-04-25 2022-05-17 Memorial Sloan-Kettering Cancer Center Treatment of H-Ras-driven tumors
TW201613919A (en) 2014-07-02 2016-04-16 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
CN105384754B (zh) * 2014-09-02 2018-04-20 上海科州药物研发有限公司 作为蛋白激酶抑制剂的杂环类化合物及其制备方法和用途
CA2961356C (en) 2014-09-15 2023-03-07 Plexxikon Inc. Heterocyclic compounds and their uses in modulating bromodomain and for treating diseases or conditions relevant thereto
US10160755B2 (en) 2015-04-08 2018-12-25 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
DK3292123T3 (da) 2015-05-06 2020-08-17 Plexxikon Inc Faste former af en forbindelse, der modulerer kinaser
CA2984899C (en) * 2015-05-06 2021-06-15 Plexxikon Inc. Synthesis of 1 h-pyrrolo[2,3-b]pyridin derivatives that modulate kinases
CA2986735A1 (en) 2015-05-22 2016-12-01 Plexxikon Inc. Solid forms of a compound for modulating kinases
CN107801378A (zh) 2015-05-22 2018-03-13 普莱希科公司 用于治疗braf‑v600相关的疾病的plx‑8394或plx‑7904
WO2016188816A1 (en) * 2015-05-22 2016-12-01 Ucb Biopharma Sprl Treatment of epilepsy
CA2987146A1 (en) * 2015-05-27 2016-12-01 Ucb Biopharma Sprl Method for the treatment of neurological disease
AR105392A1 (es) * 2015-07-20 2017-09-27 Genzyme Corp Inhibidores del receptor del factor estimulador de colonias 1 (csf-1r)
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN108137585B (zh) 2015-09-21 2021-10-22 普莱希科公司 杂环化合物及其应用
CN105131013A (zh) * 2015-10-18 2015-12-09 淄博夸克医药技术有限公司 一种新的大环内脂类化合物及其制备方法和医药用途
RU2018123825A (ru) 2015-12-07 2020-01-15 Плексксикон Инк. Соединения и способы для модуляции киназ, и показания для этого
EP3423105B1 (en) * 2016-03-02 2021-05-05 Eisai R&D Management Co., Ltd. Eribulin-based antibody-drug conjugates and methods of use
WO2017161045A1 (en) 2016-03-16 2017-09-21 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
WO2018001270A1 (en) * 2016-06-30 2018-01-04 Noratech Pharmaceuticals, Inc. Palbociclib prodrugs and composition thereof
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症
US10703757B2 (en) 2016-12-23 2020-07-07 Plexxikon Inc. Compounds and methods for CDK8 modulation and indications therefor
ES2928773T3 (es) 2017-01-17 2022-11-22 Heparegenix Gmbh Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos
JP2020511467A (ja) 2017-03-20 2020-04-16 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． ブロモドメインを阻害する４−（１−（１，１−ジ（ピリジン−２−イル）エチル）−６−（３，５−ジメチルイソオキサゾール−４−イル）−１Ｈ−ピロロ［３，２−ｂ］ピリジン−３−イル）安息香酸の結晶形
EP3600322A1 (en) * 2017-03-28 2020-02-05 Boehringer Ingelheim International GmbH Nintedanib for use in methods for the treatment of muscular dystrophy
WO2018182527A1 (en) * 2017-03-30 2018-10-04 National University Of Singapore Method for treating inflammatory complications in eye diseases
US10428067B2 (en) 2017-06-07 2019-10-01 Plexxikon Inc. Compounds and methods for kinase modulation
BR112019028235B1 (pt) 2017-07-25 2024-04-30 Plexxikon, Inc. Composições e seus métodos de preparação
CN109549941A (zh) * 2017-09-26 2019-04-02 广西梧州制药（集团）股份有限公司 一种吡唑并嘧啶衍生物在制备治疗疾病药物方面的用途
CN109549940A (zh) * 2017-09-26 2019-04-02 广西梧州制药（集团）股份有限公司 一种吡唑并嘧啶衍生物外用制剂及其制备方法
JP7675519B2 (ja) 2017-10-13 2025-05-13 オプナ バイオ ソシエテ アノニム キナーゼを調節するための化合物の固体形態
WO2019084462A1 (en) 2017-10-27 2019-05-02 Plexxikon Inc. FORMULATION OF A COMPOUND MODULATING KINASES
AU2019239952A1 (en) 2018-03-20 2020-10-08 Plexxikon Inc. Compounds and methods for IDO and TDO modulation, and indications therefor
KR20210146320A (ko) * 2019-03-29 2021-12-03 교와 가부시키가이샤 신규 아자인돌 유도체
KR20220018475A (ko) 2019-04-09 2022-02-15 플렉시콘 인코퍼레이티드 Ep300 또는 cbp 조절 및 이의 표시를 위한 응축 아진
AU2020271855B2 (en) * 2019-04-12 2025-11-27 National Health Research Institutes Heterocyclic compounds as kinase inhibitors for therapeutic uses
US12509444B2 (en) 2019-12-06 2025-12-30 Plexxikon Inc. Compounds and methods for CD73 modulation and indications therefor
CN114981298B (zh) 2019-12-12 2024-08-20 听治疗有限责任公司 用于预防和治疗听力损失的组合物和方法
US11807626B2 (en) 2020-04-23 2023-11-07 Opna Bio SA Compounds and methods for CD73 modulation and indications therefor
CN115605460A (zh) 2020-04-29 2023-01-13 普莱希科公司（Us） 杂环化合物的合成
WO2022013225A1 (en) 2020-07-13 2022-01-20 Precirix N.V. Antibody fragment against folr1
EP4199926A1 (en) 2020-08-21 2023-06-28 Plexxikon Inc. Combinational drug anticancer therapies
JP2024500919A (ja) 2020-12-23 2024-01-10 ジェンザイム・コーポレーション 重水素化コロニー刺激因子－１受容体（ｃｓｆ－１ｒ）阻害剤
KR102706327B1 (ko) 2021-03-24 2024-09-13 재단법인 아산사회복지재단 악성말초신경초종의 감별진단을 위한 조성물
CN118829635A (zh) * 2022-03-25 2024-10-22 成都嘉葆药银医药科技有限公司 一种1H-吡咯并[2,3-c]吡啶类化合物的晶型及其制备方法
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
CA3251753A1 (en) 2022-05-02 2023-11-09 Precirix N.V. PRE-TARGETTING
CN114736204A (zh) * 2022-05-06 2022-07-12 湖北工业大学 一种培西达替尼结构类似物的制备方法及其抗肿瘤中的应用
CN115054592A (zh) * 2022-07-06 2022-09-16 复旦大学附属中山医院 一种化合物在制备治疗增殖型肝细胞癌药物中的应用
CN115710281B (zh) * 2022-11-14 2024-05-17 南京中医药大学 一种异噁唑并[5,4-b]吡啶类FLT3抑制剂及其制备方法与用途
US12543861B2 (en) * 2023-08-17 2026-02-10 Shanghai Wudi Home Furnishings Co Ltd Seat with health monitoring function
WO2025097033A1 (en) * 2023-11-01 2025-05-08 City Of Hope Metformin combination therapy for use in cancer treatment
CN118614455B (zh) * 2024-06-27 2026-02-03 重庆医科大学附属第二医院 一种腹膜恶性间皮瘤动物模型的构建方法
CN121041304A (zh) * 2025-11-06 2025-12-02 哈尔滨医科大学 Cct018159与奈拉滨联合用药在制备急性白血病药物中的应用

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2248784A1 (en) 1996-06-25 1997-12-31 Takeda Chemical Industries, Ltd. Oxazolone derivatives and their use
US20040171062A1 (en) 2002-02-28 2004-09-02 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
BRPI0314042B8 (pt) 2002-09-06 2021-05-25 Calando Pharmaceuticals Inc polímeros à base de ciclodextrina para o fornecimento de agentes terapêuticos ligados a eles por covalência
AU2003272548A1 (en) 2002-09-16 2004-04-30 Plexxikon, Inc. Crystal structure of pim-1 kinase
US20050048573A1 (en) 2003-02-03 2005-03-03 Plexxikon, Inc. PDE5A crystal structure and uses
WO2004078923A2 (en) 2003-02-28 2004-09-16 Plexxikon, Inc. Pyk2 crystal structure and uses
US20050079548A1 (en) 2003-07-07 2005-04-14 Plexxikon, Inc. Ligand development using PDE4B crystal structures
EP1648867B1 (en) 2003-07-17 2013-09-04 Plexxikon Inc. Ppar active compounds
US7348338B2 (en) 2003-07-17 2008-03-25 Plexxikon, Inc. PPAR active compounds
US20050164300A1 (en) 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
PT2213661E (pt) * 2003-09-26 2011-12-15 Exelixis Inc Moduladores de c-met e métodos de uso
US7517970B2 (en) 2003-12-19 2009-04-14 Plexxikon, Inc. Nucleic acids encoding kinase and phosphatase enzymes, expression vectors and cells containing same
CA2550361C (en) 2003-12-19 2014-04-29 Prabha Ibrahim Compounds and methods for development of ret modulators
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
WO2006078287A2 (en) 2004-05-06 2006-07-27 Plexxikon, Inc. Pde4b inhibitors and uses therefor
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
CA2570817A1 (en) 2004-06-17 2006-01-26 Plexxikon, Inc. Azaindoles modulating c-kit activity and uses therefor
US7361764B2 (en) 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
EP1781654A1 (en) 2004-07-27 2007-05-09 SGX Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7605168B2 (en) 2004-09-03 2009-10-20 Plexxikon, Inc. PDE4B inhibitors
WO2006060535A2 (en) 2004-11-30 2006-06-08 Plexxikon, Inc. Indole derivatives for use as ppar active compounds
EP1819673A2 (en) 2004-11-30 2007-08-22 Plexxikon, Inc. Indole derivatives for use as ppar active compounds
US20060160135A1 (en) 2004-12-08 2006-07-20 Weiru Wang SF-1 and LRH-1 modulator development
WO2006071966A2 (en) * 2004-12-29 2006-07-06 The Brigham And Women's Hospital, Inc. Rapamycin compounds in the treatment of neurofibromatosis type 1
AU2006272951A1 (en) 2005-05-17 2007-02-01 Plexxikon, Inc. Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors
CN102206216B (zh) 2005-06-22 2014-11-12 普莱希科公司 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
RU2419618C2 (ru) 2005-09-07 2011-05-27 Плекссикон, Инк. Соединения, активные в отношении ppar (рецепторов активаторов пролиферации пероксисом)
KR20080042170A (ko) 2005-09-07 2008-05-14 플렉시콘, 인코퍼레이티드 Ｐｐａｒ 활성 화합물
AU2006287528A1 (en) 2005-09-07 2007-03-15 Plexxikon, Inc. 1 , 4 and 1 , 5-disubstituted indole derivatives for use as PPAR active compounds
WO2008063888A2 (en) * 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
PE20081581A1 (es) 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
AU2007336811A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
PE20090159A1 (es) 2007-03-08 2009-02-21 Plexxikon Inc COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs
RU2009137190A (ru) 2007-03-08 2011-04-20 Плексксикон, Инк. (Us) Соединения, обладающие активностью в отношении ppar
JP2010533729A (ja) 2007-07-17 2010-10-28 プレキシコン，インコーポレーテッド キナーゼ調節のための化合物と方法、及びそのための適応
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
US8119637B2 (en) 2008-06-10 2012-02-21 Plexxikon Inc. Substituted pyrrolo[2,3-b]pyrazines and methods for kinase modulation, and indications therefor
US8110576B2 (en) 2008-06-10 2012-02-07 Plexxikon Inc. Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications
SG10201402977WA (en) 2009-03-11 2014-09-26 Plexxikon Inc Pyrolo [2, 3-b] pyridine derivatives for the inhibition of raf kinases
AU2010224184A1 (en) 2009-03-11 2011-09-29 Plexxikon, Inc. Pyrrolo [2, 3-b] pyridine derivatives for the inhibition of Raf kinases
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
KR101739994B1 (ko) 2009-04-03 2017-05-25 에프. 호프만-라 로슈 아게 프로판-１-술폰산 ｛３-［５-（４-클로로-페닐）-１Ｈ-피롤로［２，３-ｂ］피리딘-３-카르보닐］-２，４-디플루오로-페닐｝-아미드 조성물 및 그의 용도
CA2761009A1 (en) 2009-05-04 2010-11-11 Plexxikon, Inc. Compounds and methods for inhibition of renin, and indications therefor
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
NZ599866A (en) * 2009-11-06 2014-09-26 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
US8673928B2 (en) 2009-11-18 2014-03-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN102753549A (zh) 2009-12-23 2012-10-24 普莱希科公司 用于激酶调节的化合物和方法及其适应症
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
US8642606B2 (en) 2010-09-29 2014-02-04 Plexxikon Inc. ZAP-70 active compounds
KR101911972B1 (ko) 2011-02-07 2018-10-25 플렉시콘 인코퍼레이티드 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
TWI558702B (zh) 2011-02-21 2016-11-21 普雷辛肯公司 醫藥活性物質的固態形式
AU2012255275B2 (en) 2011-05-17 2016-01-28 Plexxikon Inc. Kinase modulation and indications therefor
CN102993199A (zh) 2011-09-09 2013-03-27 山东轩竹医药科技有限公司 杂环取代的吡啶并吡咯激酶抑制剂
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
MX2015002887A (es) 2012-09-06 2015-07-06 Plexxikon Inc Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello.
EP2935248B1 (en) 2012-12-21 2018-02-28 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
SG11201506687RA (en) 2013-03-15 2015-09-29 Plexxikon Inc Heterocyclic compounds and uses thereof
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
EP3004060B1 (en) 2013-05-30 2019-11-27 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CA2961356C (en) 2014-09-15 2023-03-07 Plexxikon Inc. Heterocyclic compounds and their uses in modulating bromodomain and for treating diseases or conditions relevant thereto
US10160755B2 (en) 2015-04-08 2018-12-25 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CA2984899C (en) 2015-05-06 2021-06-15 Plexxikon Inc. Synthesis of 1 h-pyrrolo[2,3-b]pyridin derivatives that modulate kinases
DK3292123T3 (da) 2015-05-06 2020-08-17 Plexxikon Inc Faste former af en forbindelse, der modulerer kinaser
CA2986735A1 (en) 2015-05-22 2016-12-01 Plexxikon Inc. Solid forms of a compound for modulating kinases
CN107801378A (zh) 2015-05-22 2018-03-13 普莱希科公司 用于治疗braf‑v600相关的疾病的plx‑8394或plx‑7904
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN108137585B (zh) 2015-09-21 2021-10-22 普莱希科公司 杂环化合物及其应用
RU2018123825A (ru) 2015-12-07 2020-01-15 Плексксикон Инк. Соединения и способы для модуляции киназ, и показания для этого
WO2017161045A1 (en) 2016-03-16 2017-09-21 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症

Also Published As

Publication number Publication date
ZA201407580B (en) 2020-05-27
JP2015510944A (ja) 2015-04-13
NZ630483A (en) 2017-08-25
KR102350088B1 (ko) 2022-01-12
WO2013142427A1 (en) 2013-09-26
US9730918B2 (en) 2017-08-15
EA029676B1 (ru) 2018-04-30
JP6165837B2 (ja) 2017-07-19
US20140037617A1 (en) 2014-02-06
EP2827904A1 (en) 2015-01-28
BR112014023162A8 (pt) 2018-01-16
SG10201607813SA (en) 2016-11-29
KR20200139832A (ko) 2020-12-14
CA2867918A1 (en) 2013-09-26
CN104703623A (zh) 2015-06-10
AU2017254821A1 (en) 2017-11-16
AU2017254821B2 (en) 2019-09-19
EA201491721A1 (ru) 2015-02-27
SG11201405764YA (en) 2014-10-30
MY176903A (en) 2020-08-26
US9358235B2 (en) 2016-06-07
EP4295912A2 (en) 2023-12-27
EP4295912A3 (en) 2024-03-06
AU2013235298A1 (en) 2014-10-30
HK1204995A1 (en) 2015-12-11
US20180055828A1 (en) 2018-03-01
KR20140144229A (ko) 2014-12-18
IL234702A (en) 2017-02-28
US20160243092A1 (en) 2016-08-25
CN104703623B (zh) 2017-06-23
US10123998B2 (en) 2018-11-13
BR112014023162A2 (pt) 2017-06-20

Similar Documents

Publication Publication Date Title
CA2867918C (en) Compounds and methods for kinase modulation, and indications therefor
US9096593B2 (en) Compounds and methods for kinase modulation, and indications therefor
US9771369B2 (en) Compounds and methods for kinase modulation, and indications therefor
US9814714B2 (en) Kinase modulation, and indications therefor
US9682981B2 (en) Compounds and methods for kinase modulation, and indications therefor
US10227357B2 (en) Compounds and methods for kinase modulation, and indications therefor
HK40104784A (en) Compounds and methods for kinase modulation, and indications therefor

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20180305

MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 12TH ANNIV.) - STANDARD

Year of fee payment: 12

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250314

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20250314