CN105294682B - Cdk类小分子抑制剂的化合物及其用途 - Google Patents

Cdk类小分子抑制剂的化合物及其用途 Download PDF

Info

Publication number
CN105294682B
CN105294682B CN201510439488.2A CN201510439488A CN105294682B CN 105294682 B CN105294682 B CN 105294682B CN 201510439488 A CN201510439488 A CN 201510439488A CN 105294682 B CN105294682 B CN 105294682B
Authority
CN
China
Prior art keywords
compound
independently
present
alkyl
compounds
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
CN201510439488.2A
Other languages
English (en)
Chinese (zh)
Other versions
CN105294682A (zh
Inventor
刘兵
张英俊
聂凛凛
柏舜
管鸣宇
李旭珂
郑常春
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.)
Guangdong HEC Pharmaceutical Co Ltd
Original Assignee
Guangdong HEC Pharmaceutical 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 Guangdong HEC Pharmaceutical Co Ltd filed Critical Guangdong HEC Pharmaceutical Co Ltd
Priority to CN201510439488.2A priority Critical patent/CN105294682B/zh
Publication of CN105294682A publication Critical patent/CN105294682A/zh
Application granted granted Critical
Publication of CN105294682B publication Critical patent/CN105294682B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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
    • C07D471/02—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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Virology (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
CN201510439488.2A 2014-07-26 2015-07-23 Cdk类小分子抑制剂的化合物及其用途 Active CN105294682B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201510439488.2A CN105294682B (zh) 2014-07-26 2015-07-23 Cdk类小分子抑制剂的化合物及其用途

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201410361634X 2014-07-26
CN201410361634 2014-07-26
CN2015100760305 2015-02-12
CN201510076030 2015-02-12
CN201510439488.2A CN105294682B (zh) 2014-07-26 2015-07-23 Cdk类小分子抑制剂的化合物及其用途

Publications (2)

Publication Number Publication Date
CN105294682A CN105294682A (zh) 2016-02-03
CN105294682B true CN105294682B (zh) 2017-07-07

Family

ID=55192593

Family Applications (3)

Application Number Title Priority Date Filing Date
CN201510439488.2A Active CN105294682B (zh) 2014-07-26 2015-07-23 Cdk类小分子抑制剂的化合物及其用途
CN201510439329.2A Active CN105294681B (zh) 2014-07-26 2015-07-23 Cdk类小分子抑制剂的化合物及其用途
CN201510443167.XA Active CN105294736B (zh) 2014-07-26 2015-07-24 Cdk类小分子抑制剂的化合物及其用途

Family Applications After (2)

Application Number Title Priority Date Filing Date
CN201510439329.2A Active CN105294681B (zh) 2014-07-26 2015-07-23 Cdk类小分子抑制剂的化合物及其用途
CN201510443167.XA Active CN105294736B (zh) 2014-07-26 2015-07-24 Cdk类小分子抑制剂的化合物及其用途

Country Status (8)

Country Link
US (1) US9828373B2 (cg-RX-API-DMAC7.html)
EP (1) EP3172214B1 (cg-RX-API-DMAC7.html)
JP (1) JP6631616B2 (cg-RX-API-DMAC7.html)
KR (1) KR20170032244A (cg-RX-API-DMAC7.html)
CN (3) CN105294682B (cg-RX-API-DMAC7.html)
AU (1) AU2015296322B2 (cg-RX-API-DMAC7.html)
CA (1) CA2954189A1 (cg-RX-API-DMAC7.html)
WO (2) WO2016015597A1 (cg-RX-API-DMAC7.html)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA115532C2 (uk) 2011-07-29 2017-11-27 Каріофарм Терапеутікс, Інк. Модулятори нуклеарного транспорту, що містять гідразид, і їхнє застосування
KR102163377B1 (ko) 2012-05-09 2020-10-08 바이오젠 엠에이 인코포레이티드 핵 수송 조절인자 및 이의 용도
AU2014284168B2 (en) 2013-06-21 2018-10-25 Karyopharm Therapeutics Inc. Nuclear transport modulators and uses thereof
WO2016025904A1 (en) 2014-08-15 2016-02-18 Karyopharm Therapeutics Inc. Polymorphs of selinexor
CN105130986B (zh) * 2015-09-30 2017-07-18 广州科擎新药开发有限公司 嘧啶或吡啶并吡啶酮类化合物及其应用
WO2017101763A1 (en) 2015-12-13 2017-06-22 Hangzhou Innogate Pharma Co., Ltd. Heterocycles useful as anti-cancer agents
EP3397634A1 (en) 2015-12-31 2018-11-07 Karyopharm Therapeutics, Inc. Nuclear transport modulators and uses thereof
US10526295B2 (en) 2015-12-31 2020-01-07 Karyopharm Therapeutics Inc. Nuclear transport modulators and uses thereof
WO2017161253A1 (en) 2016-03-18 2017-09-21 Tufts Medical Center Compositions and methods for treating and preventing metabolic disorders
US10449195B2 (en) 2016-03-29 2019-10-22 Shenzhen Pharmacin Co., Ltd. Pharmaceutical formulation of palbociclib and a preparation method thereof
CN105777749A (zh) * 2016-04-06 2016-07-20 中国药科大学 吡啶并嘧啶类化合物、其制备方法及其用途
CN105968109B (zh) * 2016-05-13 2017-11-17 聂红梅 一种制备帕博西尼中间体的方法
EP3463453A1 (en) * 2016-05-23 2019-04-10 Eli Lilly and Company Combination of pembrolizumab and abemaciclib for the treatment of cancer
CN106083844B (zh) * 2016-06-05 2017-11-10 陈志明 一种制备抗乳腺癌药物帕博西尼中间体的方法
WO2018001270A1 (en) * 2016-06-30 2018-01-04 Noratech Pharmaceuticals, Inc. Palbociclib prodrugs and composition thereof
CA3040815C (en) 2016-10-20 2021-07-20 Steven Martin Evans Anti-proliferative agents for treating pah
CA3043681A1 (en) * 2016-11-16 2018-05-24 Pfizer Inc. Combination of an egfr t790m inhibitor and a cdk inhibitor for the treatment of non-small cell lung cancer
US11602530B2 (en) 2016-11-28 2023-03-14 Biogen Ma Inc. CRM1 inhibitors for treating epilepsy
SI3546458T1 (sl) 2016-11-28 2021-03-31 Teijin Pharma Limited Derivati ((piridin-2-il)-amino)pirido(3,4-d)pirimidina in ((piridazin-3-il)amino)pirido(3,4-d)pirimidina kot zaviralci CDK4/6 za zdravljenje npr. revmatoidnega artritisa, arterioskleroze, pljučne fibroze, možganske kapi ali raka
CN110382495B (zh) * 2016-12-16 2022-04-05 基石药业（苏州）有限公司 Cdk4/6抑制剂
US11040027B2 (en) 2017-01-17 2021-06-22 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
US20190388407A1 (en) 2017-02-12 2019-12-26 Aiviva Biopharma, Inc. Multikinase inhibitors of vegf and tfg beta and uses thereof
CN108929324A (zh) * 2017-05-22 2018-12-04 南开大学 新型1,1-环丙基二酰胺衍生物的制备与应用
WO2018226897A1 (en) * 2017-06-07 2018-12-13 Intrexon Corporation Expression of novel cell tags
CN109384767B (zh) * 2017-08-08 2020-05-05 江苏恒瑞医药股份有限公司 一种吡啶并嘧啶类衍生物的制备方法及其中间体
CN109394767A (zh) * 2017-12-19 2019-03-01 清华大学 化合物在制备药物中的用途
JP2021514359A (ja) 2018-02-15 2021-06-10 ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． キナーゼ阻害剤としての複素環式化合物
WO2019206154A1 (zh) 2018-04-24 2019-10-31 上海海雁医药科技有限公司 Cdk4/6抑制剂及其药学上可接受的盐和多晶型物及其应用
CN110496223B (zh) * 2018-05-17 2021-09-10 复旦大学附属肿瘤医院 一种治疗非霍奇金氏淋巴瘤的药物组合物
CN108524938B (zh) * 2018-06-15 2020-06-19 深圳大学 Cdk6小分子抑制剂在降低肝癌细胞对抗肿瘤药或放疗的耐受性中的应用
US12312346B2 (en) * 2018-06-27 2025-05-27 Tufts Medical Center, Inc. Pyridopyrimidine compounds and methods of their use
MX2021000895A (es) 2018-07-27 2021-08-24 California Inst Of Techn Inhibidores de cinasas dependientes de ciclinas (cdk) y usos de los mismos.
KR20210044833A (ko) * 2018-08-15 2021-04-23 아이비바 바이오파마, 인크. Vegf 및 tgf 베타의 다중 키나아제 억제제 및 이의 용도
CN113272303B (zh) * 2018-11-30 2024-09-17 上海拓界生物医药科技有限公司 嘧啶并五元氮杂环类衍生物、其制备方法及其在医药上的应用
WO2020114519A1 (zh) * 2018-12-07 2020-06-11 杭州英创医药科技有限公司 作为cdk-hdac双通路抑制剂的杂环化合物
PT3930715T (pt) * 2019-02-27 2024-08-02 Astrazeneca Ab Saracatinib para uso no tratamento de fibrose pulmonar idiopática
CN114306245A (zh) 2020-09-29 2022-04-12 深圳市药欣生物科技有限公司 无定形固体分散体的药物组合物及其制备方法
TW202237585A (zh) 2020-11-27 2022-10-01 瑞士商瑞森製藥公司 Ｃｄｋ抑制劑
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors
CN114907339B (zh) * 2021-02-08 2023-07-14 成都奥睿药业有限公司 4-（4-氨基苯氧基）吡啶-2-胺衍生物及其用途
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
CN114306255B (zh) * 2021-12-30 2023-05-23 北京鑫开元医药科技有限公司 一种甲基酮类衍生物药物制剂及其制备方法
WO2023129667A1 (en) 2021-12-30 2023-07-06 Biomea Fusion, Inc. Pyrazine compounds as inhibitors of flt3
WO2023249968A1 (en) * 2022-06-22 2023-12-28 Nikang Therapeutics, Inc. Bifunctional compounds containing pyrido[2,3-djpyrimidin-7(8h)-one derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway
WO2024107730A1 (en) * 2022-11-14 2024-05-23 Onconova Therapeutics, Inc. Methods and compositions for treating cancer
WO2024173833A1 (en) * 2023-02-16 2024-08-22 Mei Pharma, Inc. Combination of a cdk inhibitor and a flt3 inhibitor for the treatment of cancer
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217307A1 (en) 2024-04-09 2025-10-16 Revolution Medicines, Inc. Methods for predicting response to a ras(on) inhibitor and combination therapies
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003062236A1 (en) * 2002-01-22 2003-07-31 Warner-Lambert Company Llc 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d]PYRIMIDIN-7-ONES
WO2005005426A1 (en) * 2003-07-11 2005-01-20 Warner-Lambert Company Llc Isethionate salt of a selective cdk4 inhibitor
WO2010132725A2 (en) * 2009-05-13 2010-11-18 The University Of North Carolina At Chapel Hill Cyclin dependent kinase inhibitors and methods of use

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5620981A (en) 1995-05-03 1997-04-15 Warner-Lambert Company Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation
US6498163B1 (en) 1997-02-05 2002-12-24 Warner-Lambert Company Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
UA72749C2 (en) 1998-09-29 2005-04-15 White Holdings Corp Substituted 3-cyanoquinolines, a method for the preparation thereof (variants), pharmaceutical composition based thereon, a method for the treatment, inhibiting the growth or elimination of neoplasms and a method for the treatment, inhibiting progressing or elimination of polycystic kidney disease using them
US6534535B1 (en) 1999-08-12 2003-03-18 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
JP4411709B2 (ja) 1999-11-02 2010-02-10 凸版印刷株式会社 キノロン誘導体ならびにそれを使用した有機ｅｌ素子
US6420384B2 (en) 1999-12-17 2002-07-16 Ariad Pharmaceuticals, Inc. Proton pump inhibitors
US6777413B2 (en) 2000-02-01 2004-08-17 Millennium Pharmaceuticals, Inc. 2-[1H]-quinolone and 2-[1H]-quinoxalone inhibitors of factor Xa
JP2003528101A (ja) * 2000-03-06 2003-09-24 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー ５−アルキルピリド［２，３−ｄ］ピリミジンチロシンキナーゼ阻害剤
WO2002012238A2 (en) 2000-08-04 2002-02-14 Warner-Lambert Company 2-(4-PYRIDYL)AMINO-6-DIALKOXYPHENYL-PYRIDO[2,3-d]PYRIMIDIN-7-ONES
US6506749B2 (en) 2000-08-31 2003-01-14 Syntex (U.S.A.) Llc 7-oxo-pyridopyrimidines (I)
CA2356544C (en) 2000-10-03 2006-04-04 Warner-Lambert Company Pyridotriazines and pyridopyridazines
CN100376571C (zh) 2001-02-12 2008-03-26 霍夫曼-拉罗奇有限公司 6-取代的吡啶并嘧啶类化合物
PE20030008A1 (es) 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
US7196090B2 (en) 2002-07-25 2007-03-27 Warner-Lambert Company Kinase inhibitors
US20050009849A1 (en) 2003-01-03 2005-01-13 Veach Darren R. Pyridopyrimidine kinase inhibitors
WO2004065378A1 (en) 2003-01-17 2004-08-05 Warner-Lambert Company Llc 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
CA2542105C (en) 2003-10-08 2011-08-02 Irm Llc Compounds and compositions as protein kinase inhibitors
EP1718645A1 (en) 2004-02-18 2006-11-08 Warner-Lambert Company LLC 2-(pyridin-3-ylamino)-pyrido 2,3-d pyrimidin-7-ones
US20080255162A1 (en) 2004-05-04 2008-10-16 Warner-Lambert Company Llc Pyrrolyl Substituted Pyrido[2,3-D]Pyrimidin-7-Ones and Derivatives Thereof as Therapeutic Agents
CA2575804A1 (en) 2004-08-26 2006-03-02 Boehringer Ingelheim International Gmbh Pteridinones used as plk (polo like kinase) inhibitors
US20090131430A1 (en) 2004-11-23 2009-05-21 Palle Venkata P Pyrido'2,3-dipyrimidines as anti-inflammatory agents
US20060142312A1 (en) 2004-12-23 2006-06-29 Pfizer Inc C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones
EP1844023A1 (en) 2004-12-31 2007-10-17 Sk Chemicals Co., Ltd. Quinazoline derivatives for the treatment and prevention of diabetes and obesity
EP1846403A1 (en) 2005-02-02 2007-10-24 Ranbaxy Laboratories Limited Azabicyclo derivatives as anti-inflammatory agents
US8247408B2 (en) 2005-10-07 2012-08-21 Exelixis, Inc. Pyridopyrimidinone inhibitors of PI3Kα for the treatment of cancer
FR2896246B1 (fr) 2006-01-13 2008-08-15 Sanofi Aventis Sa Derives de pyrido-pyrimidone, leur preparation, leur application en therapeutique.
CA2651072A1 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
EP2018167A4 (en) 2006-05-15 2010-07-14 Irm Llc COMPOSITIONS AND METHODS AS INHIBITORS OF FGF RECEPTOR KINASES
MY146420A (en) 2006-09-15 2012-08-15 Pfizer Prod Inc Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors
EP1914234A1 (en) 2006-10-16 2008-04-23 GPC Biotech Inc. Pyrido[2,3-d]pyrimidines and their use as kinase inhibitors
EP2094698A1 (en) 2006-11-09 2009-09-02 F. Hoffmann-Roche AG Substituted 6-phenyl-pyrido [2,3-d]pyrimidin-7-one derivatives as kinase inhibitors and methods for using the same
AU2008239655B2 (en) 2007-04-11 2013-06-20 Exelixis, Inc. Pyrido (2, 3-d) pyrimidin-7-one compounds as inhibitors of PI3k-alpha for the treatment of cancer
WO2008157500A1 (en) 2007-06-17 2008-12-24 Kalypsys, Inc. Aminoquinazoline cannabinoid receptor modulators for treatment of disease
EP2280969A1 (en) 2008-04-29 2011-02-09 F. Hoffmann-La Roche AG Pyrimidinyl pyridone inhibitors of jnk.
CN101747306B (zh) 2008-11-28 2012-08-29 中国中化股份有限公司 取代醚类化合物及其应用
EP2486037A4 (en) 2009-10-09 2013-01-16 Afraxis Inc 8-ETHYL-6- (ARYL) PYRIDO [2,3-D] PYRIMIDIN-7 (8H) -ONES FOR THE TREATMENT OF CNS DISORDERS
CA2784749C (en) 2009-12-18 2017-12-12 E. Premkumar Reddy Substituted pyrido[2,3-d]pyrimidin-7(8h)-ones and therapeutic uses thereof
AU2011240735B2 (en) * 2010-04-13 2015-01-29 Novartis Ag Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (CDK4/6) inhibitor and an mTOR inhibitor for treating cancer
US8912203B2 (en) 2010-06-09 2014-12-16 Afraxis Holdings, Inc. 6-(sulfonylaryl)pyrido[2,3-D]pyrimidin-7(8H)-ones for the treatment of CNS disorders
WO2011156640A2 (en) 2010-06-09 2011-12-15 Afraxis, Inc. 8-(HETEROARYLMETHYL)PYRIDO[2,3-d]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS
WO2011156780A2 (en) 2010-06-10 2011-12-15 Afraxis, Inc. 8-(sulfonylbenzyl)pyrido[2,3-d]pyrimidin-7(8h)-ones for the treatment of cns disorders
EP2580217A4 (en) 2010-06-10 2014-06-18 Afraxis Holdings Inc 6- (ETHYNYL-) PYRIDO- [2,3-D-] PYRIMIDIN-7- (8H) -ONE FOR THE TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM
NZ606281A (en) 2010-08-05 2014-09-26 Univ Temple 2-substituted-8-alkyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitriles and uses thereof
ES2377610B1 (es) 2010-09-01 2013-02-05 Institut Químic de Sarriá CETS Fundació Privada Preparación de compuestos pirido[2,3-d]pirimidin-7(8h)-ona sustituidos.
ES2543569T3 (es) * 2011-03-23 2015-08-20 Amgen Inc. Inhibidores duales tricíclicos condensados de CDK 4/6 y FLT3
CA2832309A1 (en) 2011-04-08 2013-03-28 David Campbell 8-ethyl-6-(aryl)pyrido[2,3-d]pyrimidin-7(8h)-ones for the treatment of nervous system disorders and cancer
US20130116263A1 (en) 2011-11-04 2013-05-09 Afraxis, Inc. Pak inhibitors for the treatment of cell proliferative disorders
CN106008511B (zh) 2012-05-14 2018-08-14 华东理工大学 蝶啶酮衍生物及其作为egfr、blk、flt3抑制剂的应用
WO2014074926A1 (en) 2012-11-09 2014-05-15 Rutgers, The State University Of New Jersey Therapeutic hydroxyquinolones
CN103012399B (zh) 2012-11-22 2015-06-17 中国科学院广州生物医药与健康研究院 7-氧代吡啶并嘧啶类化合物及其药用组合物和应用
TW201522332A (zh) 2013-03-01 2015-06-16 Amgen Inc 經取代之７－酮基－吡啶并［２，３－ｄ］嘧啶及其使用方法
AR095464A1 (es) 2013-03-15 2015-10-21 Celgene Avilomics Res Inc Compuestos de heteroarilo y usos de los mismos
EP2970209B1 (en) 2013-03-15 2018-12-26 CoNCERT Pharmaceuticals, Inc. Deuterated palbociclib with improved metabolic stability
WO2014174745A1 (ja) 2013-04-26 2014-10-30 国立大学法人京都大学 Ｅｇ５阻害剤
US20140323477A1 (en) 2013-04-30 2014-10-30 Genentech, Inc. Serine/threonine kinase inhibitors
US20140323478A1 (en) 2013-04-30 2014-10-30 Afraxis Holdings, Inc. Serine/threonine kinase inhibitors
US9630963B2 (en) 2013-05-09 2017-04-25 Principia Biopharma, Inc. Quinolone derivatives as fibroblast growth factor inhibitors
CN104470921B (zh) * 2013-05-17 2017-05-03 上海恒瑞医药有限公司 吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
EP2813504A1 (en) 2013-06-14 2014-12-17 Institut Quimic De Sarriá Cets, Fundació Privada 4-Amino-6-(2,6-dichlorophenyl)-2-(phenylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one derivatives, synthesis and uses thereof
TW201516045A (zh) 2013-07-26 2015-05-01 Hoffmann La Roche 絲胺酸／蘇胺酸激酶抑制劑
CN104418860B (zh) 2013-08-20 2016-09-07 中国科学院广州生物医药与健康研究院 嘧啶并杂环类化合物及其药用组合物和应用
PH12016500739B1 (en) 2013-10-25 2022-04-29 Blueprint Medicines Corp Inhibitors of the fibrolast growth factor receptor
EP3076789A4 (en) 2013-12-04 2017-11-22 The Scripps Research Institute Novel compounds as jnk kinase inhibitors
WO2015086523A1 (en) 2013-12-09 2015-06-18 Ucb Biopharma Sprl Fused bicyclic heteroaromatic derivatives as modulators of tnf activity
PL3102577T3 (pl) 2014-02-07 2019-03-29 Principia Biopharma Inc. Pochodne chinolonowe jako inhibitory receptora czynnika wzrostu fibroblastów

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003062236A1 (en) * 2002-01-22 2003-07-31 Warner-Lambert Company Llc 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d]PYRIMIDIN-7-ONES
WO2005005426A1 (en) * 2003-07-11 2005-01-20 Warner-Lambert Company Llc Isethionate salt of a selective cdk4 inhibitor
WO2010132725A2 (en) * 2009-05-13 2010-11-18 The University Of North Carolina At Chapel Hill Cyclin dependent kinase inhibitors and methods of use

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"Discovery of a Potent and Selective Inhibitor of Cyclin-Dependent Kinase 4/6";Peter L. Toogood et al.;《Journal of Medicinal Chemistry》;20050302;第48卷(第7期);第2391页 *

Also Published As

Publication number Publication date
US20170121323A1 (en) 2017-05-04
CN105294736B (zh) 2020-01-14
JP2017524702A (ja) 2017-08-31
AU2015296322B2 (en) 2019-09-19
EP3172214A1 (en) 2017-05-31
AU2015296322A1 (en) 2017-01-12
WO2016015598A1 (en) 2016-02-04
WO2016015597A1 (en) 2016-02-04
JP6631616B2 (ja) 2020-01-15
CN105294681B (zh) 2017-07-07
EP3172214A4 (en) 2018-02-07
CN105294681A (zh) 2016-02-03
CN105294682A (zh) 2016-02-03
CN105294736A (zh) 2016-02-03
EP3172214B1 (en) 2020-05-13
HK1232223A1 (en) 2018-01-05
US9828373B2 (en) 2017-11-28
CA2954189A1 (en) 2016-02-04
KR20170032244A (ko) 2017-03-22

Similar Documents

Publication Publication Date Title
CN105294682B (zh) Cdk类小分子抑制剂的化合物及其用途
CN105294683B (zh) Cdk类小分子抑制剂的化合物及其用途
CN105272930B (zh) 取代脲衍生物及其在药物中的应用
AU2014375500B2 (en) Kinase inhibitor and use thereof
CN104513252B (zh) 取代脲衍生物及其在药物中的应用
CN104513257B (zh) 取代脲衍生物及其在药物中的应用
TWI690533B (zh) Ｃｄｋ類小分子抑制劑的化合物及其用途
TWI684591B (zh) 取代脲衍生物及其在藥物中的應用
HK1232223B (en) 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one derivatives as cdk inhibitors and uses thereof
HK1232224B (en) 1-(5-(tert.-butyl)isoxazol-3-yl)-3-(4-((phenyl)ethynyl)phenyl)urea derivatives and related compounds as flt3 inhibitors for treating cancer

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant
CP03 Change of name, title or address

Address after: 523808 No.1, Gongye North Road, Songshanhu Park, Dongguan City, Guangdong Province

Patentee after: Guangdong Dongyangguang Pharmaceutical Co.,Ltd.

Address before: 523000 Songshan Lake Science and Technology Industrial Park, Dongguan, Guangdong (No. 1 Industrial North Road, Hubei Industrial Park, Songshan)

Patentee before: SUNSHINE LAKE PHARMA Co.,Ltd.

CP03 Change of name, title or address