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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (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
CN201410361634 2014-07-26
CN201410361634X 2014-07-26
CN201510076030 2015-02-12
CN2015100760305 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 (enExample)
EP (1) EP3172214B1 (enExample)
JP (1) JP6631616B2 (enExample)
KR (1) KR20170032244A (enExample)
CN (3) CN105294682B (enExample)
AU (1) AU2015296322B2 (enExample)
CA (1) CA2954189A1 (enExample)
WO (2) WO2016015598A1 (enExample)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2954991T3 (es) 2011-07-29 2023-11-28 Karyopharm Therapeutics Inc Moduladores del transporte nuclear que contienen hidrazida y usos de los mismos
SMT202000347T1 (it) 2012-05-09 2020-07-08 Biogen Ma Inc Modulatori di trasporto nucleare e loro usi
PL3010892T3 (pl) 2013-06-21 2019-07-31 Karyopharm Therapeutics, Inc. 1,2,4-triazole jako modulatory transportu jądrowego i ich zastosowania
CN111484483B (zh) 2014-08-15 2023-05-26 卡尔约药物治疗公司 赛灵克斯的多晶型物
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
JP6951767B2 (ja) 2015-12-13 2021-10-20 ハンジョウ イノゲート ファーマ カンパニー リミテッドＨａｎｇｚｈｏｕ Ｉｎｎｏｇａｔｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． 抗癌薬として使用される複素環式化合物
EP3397634A1 (en) 2015-12-31 2018-11-07 Karyopharm Therapeutics, Inc. Nuclear transport modulators and uses thereof
EP3397633A1 (en) 2015-12-31 2018-11-07 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
JP2019516767A (ja) * 2016-05-23 2019-06-20 イーライ リリー アンド カンパニー 癌の治療のためのペンブロリズマブとアベマシクリブとの組合せ
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
EP3804724B1 (en) 2016-10-20 2022-12-07 Pfizer Inc. Cdk inhibitors for treating pah
US20190275049A1 (en) * 2016-11-16 2019-09-12 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
KR102513448B1 (ko) * 2016-12-16 2023-03-23 씨스톤 파마슈티컬즈 Cdk4/6 억제제
MX393780B (es) 2017-01-17 2025-03-24 Heparegenix Gmbh Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos
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
CN110997920A (zh) * 2017-06-07 2020-04-10 英特拉克森公司 新型细胞标签的表达
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
US11174252B2 (en) 2018-02-15 2021-11-16 Nuvation Bio Inc. Heterocyclic compounds as kinase inhibitors
EP3786161A4 (en) 2018-04-24 2021-05-05 Shanghai Haiyan Pharmaceutical Technology Co., Ltd CDK4 / 6 INHIBITOR AND PHARMACEUTICALLY ACCEPTABLE SALT AND POLYMORPHIC THEREOF, AND USE OF IT
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
CA3107750A1 (en) 2018-07-27 2020-01-30 California Institute Of Technology Cdk inhibitors and uses thereof
US12502391B2 (en) 2018-08-15 2025-12-23 Aiviva Biopharma, Inc. Multi-kinase inhibitors of VEGF and TGF beta and uses thereof
CA3120791A1 (en) * 2018-11-30 2020-06-04 Tuojie Biotech (Shanghai) Co., Ltd. Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof
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
WO2020174420A1 (en) * 2019-02-27 2020-09-03 Astrazeneca Ab Method of treating a fibrotic disease or condition or of an interstitial lung disease using a src kinase inhibitor
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
AR124154A1 (es) 2020-11-27 2023-02-22 Rhizen Pharmaceuticals Ag Inhibidores de cdk
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
JP2025502748A (ja) 2021-12-30 2025-01-28 バイオメア フュージョン，インコーポレイテッド Ｆｌｔ３の阻害剤としてのピラジン化合物
CN119156389A (zh) * 2022-05-05 2024-12-17 百济神州有限公司 杂环化合物、其组合物和其治疗方法
CN119451967A (zh) * 2022-06-22 2025-02-14 霖康疗法公司 用于经由泛素蛋白酶体途径降解细胞周期蛋白依赖性激酶2的含有吡啶并[2,3-d]嘧啶-7(8H)-酮衍生物的双功能化合物
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
WO2024229406A1 (en) 2023-05-04 2024-11-07 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
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
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
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (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
WO2026015796A1 (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
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors

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
PL201475B1 (pl) 1998-09-29 2009-04-30 Wyeth Corp Podstawione 3-cyjanochinoliny jako inhibitory białkowych kinaz tyrozynowych
AU6762400A (en) 1999-08-12 2001-03-13 Cor Therapeutics, 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
WO2001044257A1 (en) 1999-12-17 2001-06-21 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
YU66502A (sh) 2000-03-06 2005-09-19 Warner-Lambert Company 5-alkilpirido(2,3-d)pirimidini, inhibitori tirozinkinaza
ES2311532T3 (es) 2000-08-04 2009-02-16 Warner-Lambert Company Llc 2-(4-pirdil)amino-6-dialcoxifenil-pirido(2.3-d)pirimidin-7-onas.
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
CZ20032416A3 (cs) 2001-02-12 2004-07-14 F. Hoffmann-La Roche Ag 6-Substituované pyridopyrimidiny
PE20030008A1 (es) 2001-06-19 2003-01-22 Bristol Myers Squibb Co Inhibidores duales de pde 7 y pde 4
PA8577501A1 (es) 2002-07-25 2004-02-07 Warner Lambert Co Inhibidores de quinasas
WO2004063195A1 (en) 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
JP2006516561A (ja) 2003-01-17 2006-07-06 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 細胞増殖の阻害剤としての２−アミノピリジン置換ヘテロ環類
US7449582B2 (en) 2003-10-08 2008-11-11 Irm Llc Compounds and compositions as protein kinase inhibitors
JP2007523151A (ja) 2004-02-18 2007-08-16 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー ２−（ピリジン−３−イルアミノ）−ピリド［２，３−ｄ］ピリミジン−７−オン
BRPI0510560A (pt) 2004-05-04 2007-11-20 Warner Lambert Co pirido[2,3-d] pirimidin-7-onas pirrolil substituìdas e seus derivados como agentes terapêuticos
CA2575804A1 (en) 2004-08-26 2006-03-02 Boehringer Ingelheim International Gmbh Pteridinones used as plk (polo like kinase) inhibitors
EP1831215A1 (en) 2004-11-23 2007-09-12 Ranbaxy Laboratories Limited Pyrido[2,3-d]pyrimidines as anti-inflamatory agents
US20060142312A1 (en) 2004-12-23 2006-06-29 Pfizer Inc C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones
JP2008526734A (ja) 2004-12-31 2008-07-24 エスケー ケミカルズ カンパニー リミテッド 糖尿及び肥満治療予防に有効なキナゾリン誘導体
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
MX2008014618A (es) 2006-05-15 2008-11-28 Irm Llc Composiciones y metodos para inhibidores de cinasas del receptor fgf.
GEP20115306B (enExample) 2006-09-15 2011-10-10 Pfizer Prod Inc
EP1914234A1 (en) 2006-10-16 2008-04-23 GPC Biotech Inc. Pyrido[2,3-d]pyrimidines and their use as kinase inhibitors
JP2010509265A (ja) 2006-11-09 2010-03-25 エフ．ホフマン−ラ ロシュ アーゲー キナーゼ阻害剤としての置換６−フェニル−ピリド［２，３−ｄ］ピリミジン−７−オン誘導体及びそれの使用方法
CA2683784A1 (en) 2007-04-11 2008-10-23 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
CN102015704A (zh) 2008-04-29 2011-04-13 霍夫曼-拉罗奇有限公司 Jnk的嘧啶基吡啶酮抑制剂
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
CA2776770A1 (en) 2009-10-09 2011-04-14 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
EP2580213A4 (en) 2010-06-09 2013-12-25 Afraxis Holdings Inc 8- (HETEROARYLMETHYL) PYRIDO [2,3-D] PYRIMIDIN-7 (8H) -ONES FOR THE TREATMENT OF CNS DISORDERS
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
US8680099B2 (en) 2010-06-10 2014-03-25 Afraxis Holdings, Inc. 6-(ethynyl)pyrido[2,3-D]pyrimidin-7(8H)-ones for the treatment of CNS disorders
EP2580216A4 (en) 2010-06-10 2014-07-23 Afraxis Holdings Inc 8- (SULFONYLBENZYL) PYRIDO- [2,3-D-] PYRIMIDIN-7- (8H) -ONE FOR THE TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM
DK2600719T3 (da) 2010-08-05 2014-12-15 Univ Temple 2-substituerede 8-alkyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-6-carbonnitriler og anvendelser deraf
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.
PT2688887E (pt) * 2011-03-23 2015-07-06 Amgen Inc Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3
EP2694504A4 (en) 2011-04-08 2014-08-27 Afraxis Holdings Inc 8-ETHYL-6 (ARYL) PYRIDO [2,3-D] PYRIMIDIN-7 (8H) -ONES FOR THE TREATMENT OF DISEASES AFFECTING THE NERVOUS SYSTEM AND FOR THE TREATMENT OF CANCER
KR20140105451A (ko) 2011-11-04 2014-09-01 아프락시스 홀딩즈 인코포레이티드 유약 x 증후군의 치료를 위한 pak 억제제
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
US9321786B2 (en) 2013-03-15 2016-04-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
AU2014235462C1 (en) 2013-03-15 2018-11-01 Concert Pharmaceuticals, Inc. Deuterated palbociclib
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
WO2014183520A1 (zh) * 2013-05-17 2014-11-20 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
WO2015011252A1 (en) 2013-07-26 2015-01-29 F. Hoffmann-La Roche Ag Pyrimidine-pyridinone serine/threonine kinase inhibitors
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
BR112016008849B8 (pt) 2013-10-25 2022-09-06 Blueprint Medicines Corp Compostos ou sais farmaceuticamente aceitáveis dos mesmos, uso dos referidos compostos e composições farmacêuticas
EP3076789A4 (en) 2013-12-04 2017-11-22 The Scripps Research Institute Novel compounds as jnk kinase inhibitors
CN105814022B (zh) 2013-12-09 2018-09-28 Ucb生物制药私人有限公司 作为tnf活性调节剂的稠合的二环杂芳族衍生物
US9815834B2 (en) 2014-02-07 2017-11-14 Principia Biopharma, Inc. Quinolone derivatives as fibroblast growth factor receptor inhibitors

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

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
CN105294737A (zh) Cdk类小分子抑制剂的化合物及其用途
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

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
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.