JP6669745B2 - ブロモドメインのインヒビターとしての置換ピロロピリジン - Google Patents

ブロモドメインのインヒビターとしての置換ピロロピリジン Download PDF

Info

Publication number
JP6669745B2
JP6669745B2 JP2017525078A JP2017525078A JP6669745B2 JP 6669745 B2 JP6669745 B2 JP 6669745B2 JP 2017525078 A JP2017525078 A JP 2017525078A JP 2017525078 A JP2017525078 A JP 2017525078A JP 6669745 B2 JP6669745 B2 JP 6669745B2
Authority
JP
Japan
Prior art keywords
oxo
alkyl
methyl
heterocyclyl
optionally substituted
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.)
Expired - Fee Related
Application number
JP2017525078A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017533249A (ja
JP2017533249A5 (enExample
Inventor
ブライアン ケー. アルブレヒト,
ブライアン ケー. アルブレヒト,
スティーブン エフ. ベロン,
スティーブン エフ. ベロン,
ダニエル ジェイ. バーディック,
ダニエル ジェイ. バーディック,
アレクサンドル コート,
アレクサンドル コート,
テリー クローフォード,
テリー クローフォード,
レス エー. デイキン,
レス エー. デイキン,
マイケル チャールズ ヒューイット,
マイケル チャールズ ヒューイット,
ツイ, ビッキー シャオ−ウェイ
ツイ, ビッキー シャオ−ウェイ
イブ レブラン,
イブ レブラン,
スティーブン アール. マグヌソン,
スティーブン アール. マグヌソン,
クリストファー ジー. ナスヴェスチャック,
クリストファー ジー. ナスヴェスチャック,
エフ. アントニー ロメロ,
エフ. アントニー ロメロ,
ヨン タン,
ヨン タン,
アレクサンダー エム. テイラー,
アレクサンダー エム. テイラー,
シューメイ ワン,
シューメイ ワン,
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.)
Constellation Pharmaceuticals Inc
Original Assignee
Constellation Pharmaceuticals 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 Constellation Pharmaceuticals Inc filed Critical Constellation Pharmaceuticals Inc
Publication of JP2017533249A publication Critical patent/JP2017533249A/ja
Publication of JP2017533249A5 publication Critical patent/JP2017533249A5/ja
Application granted granted Critical
Publication of JP6669745B2 publication Critical patent/JP6669745B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/40Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Obesity (AREA)
  • AIDS & HIV (AREA)
  • Transplantation (AREA)
  • Molecular Biology (AREA)
JP2017525078A 2014-11-10 2015-11-10 ブロモドメインのインヒビターとしての置換ピロロピリジン Expired - Fee Related JP6669745B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462077707P 2014-11-10 2014-11-10
US62/077,707 2014-11-10
PCT/US2015/060007 WO2016077380A1 (en) 2014-11-10 2015-11-10 Substituted pyrrolopyridines as inhibitors of bromodomain

Publications (3)

Publication Number Publication Date
JP2017533249A JP2017533249A (ja) 2017-11-09
JP2017533249A5 JP2017533249A5 (enExample) 2018-12-20
JP6669745B2 true JP6669745B2 (ja) 2020-03-18

Family

ID=54602075

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2017525078A Expired - Fee Related JP6669745B2 (ja) 2014-11-10 2015-11-10 ブロモドメインのインヒビターとしての置換ピロロピリジン

Country Status (6)

Country Link
US (1) US10150767B2 (enExample)
EP (1) EP3218374B1 (enExample)
JP (1) JP6669745B2 (enExample)
CN (1) CN107108614B (enExample)
MA (1) MA40940A (enExample)
WO (1) WO2016077380A1 (enExample)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA40943A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
EP3218376B1 (en) * 2014-11-10 2019-12-25 Genentech, Inc. Bromodomain inhibitors and uses thereof
JP6709792B2 (ja) 2015-01-29 2020-06-17 ジェネンテック, インコーポレイテッド 治療用化合物およびその使用
EP3265453B1 (en) 2015-03-05 2022-06-29 Boehringer Ingelheim International GmbH New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9
AR104259A1 (es) * 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
ES2793239T3 (es) 2016-04-15 2020-11-13 Abbvie Inc Inhibidores del bromodominio
CN109475528B (zh) 2016-04-22 2022-01-11 达纳-法伯癌症研究所股份有限公司 用于egfr降解的双功能分子和使用方法
WO2018130174A1 (zh) * 2017-01-11 2018-07-19 江苏豪森药业集团有限公司 吡咯并[2,3-c]吡啶类衍生物、其制备方法及其在医药上的应用
JP7300394B2 (ja) 2017-01-17 2023-06-29 ヘパリジェニックス ゲーエムベーハー 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害
US20210130346A1 (en) * 2017-04-14 2021-05-06 Abbvie Inc. Bromodomain Inhibitors
WO2018223909A1 (zh) * 2017-06-05 2018-12-13 成都海创药业有限公司 一种嵌合分子及其制备和应用
JP2021506903A (ja) * 2017-12-20 2021-02-22 貝達薬業股▲ふん▼有限公司Betta Pharmaceuticals Co.,Ltd ブロモドメインタンパク質阻害剤である化合物、および組成物
CN111683932A (zh) * 2018-02-06 2020-09-18 上海海和药物研究开发有限公司 具有bet抑制活性的化合物及其制备方法和用途
CN108465108B (zh) * 2018-03-12 2020-07-07 上海宇玫博生物科技有限公司 一种预防或治疗脑胶质瘤的特异性基因靶点
US10442799B1 (en) 2018-04-07 2019-10-15 Fuqiang Ruan Heterocyclic compounds and uses thereof
CN110372693B (zh) * 2018-07-04 2022-05-03 清华大学 一种靶向降解bet蛋白的化合物及其应用
CN110776508B (zh) * 2018-07-27 2021-07-16 海创药业股份有限公司 一种brd4抑制剂及其制备方法和用途
CN110818609A (zh) * 2018-08-11 2020-02-21 中国药科大学 3-乙酰基吲哚类brpf1抑制剂的制备方法及其用途
US20210198629A1 (en) * 2018-08-20 2021-07-01 University Of Georgia Research Foundation, Inc. Compositions and methods for increasing beiging of white adipose tissue
CN109125729A (zh) * 2018-09-06 2019-01-04 苏州吉玛基因股份有限公司 与非小细胞肺癌诊疗相关的基因BRD9及其siRNAs和应用
WO2020132004A1 (en) * 2018-12-20 2020-06-25 Saint Louis University Bet inhibitors for modulating dux4 expression in fshd
JP7603613B2 (ja) * 2019-04-24 2024-12-20 コンバージーン・リミテッド・ライアビリティ・カンパニー 小分子ブロモドメイン阻害剤およびそれらの使用
GB201905721D0 (en) * 2019-04-24 2019-06-05 Univ Dundee Compounds
US11171132B2 (en) * 2019-10-03 2021-11-09 Globalfoundries U.S. Inc. Bi-directional breakdown silicon controlled rectifiers
CN112625036A (zh) * 2019-10-08 2021-04-09 上海海和药物研究开发股份有限公司 一类具有brd4抑制活性的化合物、其制备方法及用途
CN115667237A (zh) * 2020-07-17 2023-01-31 成都苑东生物制药股份有限公司 作为bet抑制剂的新型杂环化合物
TW202237095A (zh) 2020-12-03 2022-10-01 德商艾斯巴赫生物有限公司 Alc1抑制劑及與parpi之協同性
IL309651A (en) * 2021-06-29 2024-02-01 Tay Therapeutics Ltd History Pyrolopyridone is useful in the treatment of cancer
CN115611890B (zh) * 2021-07-15 2024-05-31 成都硕德药业有限公司 一种新型噻吩类bet溴结构域抑制剂、其制备方法及医药用途
TW202330519A (zh) * 2021-09-29 2023-08-01 香港商德琪研發有限公司 作為tam抑制劑的吡唑并吡啶化合物
CN119365198A (zh) 2022-05-02 2025-01-24 艾斯巴赫生物有限公司 ALC1抑制剂的用途和与PARPi的协同作用
CN117304205A (zh) * 2022-06-20 2023-12-29 中国科学院广州生物医药与健康研究院 一种苯并咪唑类三元并环化合物、其药学上可接受的盐及其应用
EP4637754A2 (en) * 2022-12-23 2025-10-29 Tay Therapeutics Limited Selective bet inhibitors and uses thereof
WO2024193527A1 (zh) * 2023-03-20 2024-09-26 山东新时代药业有限公司 作为溴结构域抑制剂的吡咯并[2,3-c]吡啶类化合物

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CU22545A1 (es) 1994-11-18 1999-03-31 Centro Inmunologia Molecular Obtención de un anticuerpo quimérico y humanizado contra el receptor del factor de crecimiento epidérmico para uso diagnóstico y terapéutico
US4943533A (en) 1984-03-01 1990-07-24 The Regents Of The University Of California Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor
EP0491007B1 (en) 1989-09-08 1996-03-13 The Johns Hopkins University Structural alterations of the egf receptor gene in human gliomas
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
DE69428764T2 (de) 1993-12-24 2002-06-20 Merck Patent Gmbh Immunokonjugate
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
HU216142B (hu) 1994-07-21 1999-04-28 Akzo Nobel N.V. Ciklusos keton-peroxidokat tartalmazó kompozíciók, és azok alkalmazása (ko)polimerek módosítására
US5804396A (en) 1994-10-12 1998-09-08 Sugen, Inc. Assay for agents active in proliferative disorders
ES2332984T3 (es) 1995-03-30 2010-02-16 Pfizer Products Inc. Derivados de quinazolinas.
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
GB9508565D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quiazoline derivative
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
EP0831880A4 (en) 1995-06-07 2004-12-01 Imclone Systems Inc ANTIBODIES AND FRAGMENTS OF ANTIBODIES INHIBITING TUMOR GROWTH
WO1997002266A1 (en) 1995-07-06 1997-01-23 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
CN1923818A (zh) 1996-04-12 2007-03-07 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
ATE227283T1 (de) 1996-07-13 2002-11-15 Glaxo Group Ltd Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
US6235883B1 (en) 1997-05-05 2001-05-22 Abgenix, Inc. Human monoclonal antibodies to epidermal growth factor receptor
AU7165698A (en) 1997-05-06 1998-11-27 American Cyanamid Company Use of quinazoline compounds for the treatment of polycystic kidney disease
ZA986729B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
TW436485B (en) 1997-08-01 2001-05-28 American Cyanamid Co Substituted quinazoline derivatives
BR9814116A (pt) 1997-11-06 2000-10-03 American Cyanamid Co Uso de derivados de quinazolina como inibidores de cinase de tirosina para tratamento de pólipo colÈnico
BR9915487A (pt) 1998-11-19 2001-07-31 Warner Lambert Co N-[4-(3-cloro-4-flúor-fenilamino) - 7 - (3-morfolin-4-il-propóxi)-quinazolin-6-il]-acrilamida, um inibidor irreversìvel de tirosina quinases
EP1953147A1 (en) 2005-11-21 2008-08-06 Japan Tobacco, Inc. Heterocyclic compound and medicinal application thereof
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20140094456A1 (en) * 2012-10-02 2014-04-03 Intermune, Inc. Anti-fibrotic pyridinones
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
WO2014125408A2 (en) * 2013-02-12 2014-08-21 Aurigene Discovery Technologies Limited Substituted 1h-pyrrolopyridinone derivatives as kinase inhibitors
BR112015022674A2 (pt) 2013-03-11 2017-07-18 Abbvie Inc inibidores de bromodomínio
US10035800B2 (en) * 2013-03-12 2018-07-31 Abbvie Inc. Substituted 1,4,10-triazadibenzo[cd,f]azulenes, substituted 1,4,5,10-tetraazadibenzo[cd,f]azulenes and substituted 1,4,5,7,10-pentaazadibenzo[cd,f]azulenes as bromodomain inhibitors
CN104211639A (zh) 2013-06-05 2014-12-17 中国科学院上海药物研究所 一类炔基杂环类化合物及其应用
WO2014201161A1 (en) 2013-06-12 2014-12-18 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitor compounds
EP3013828A4 (en) * 2013-06-28 2016-11-23 Abbvie Inc BROMDOMÄNENINHIBITOREN
WO2015081280A1 (en) * 2013-11-26 2015-06-04 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution
US20150148372A1 (en) * 2013-11-26 2015-05-28 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081203A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
KR102373700B1 (ko) 2014-04-02 2022-03-11 인터뮨, 인크. 항섬유성 피리디논
WO2015164480A1 (en) * 2014-04-23 2015-10-29 Incyte Corporation 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS
EP3218376B1 (en) 2014-11-10 2019-12-25 Genentech, Inc. Bromodomain inhibitors and uses thereof
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
US9763922B2 (en) * 2014-11-27 2017-09-19 Genentech, Inc. Therapeutic compounds and uses thereof
HK1245677A1 (zh) 2015-01-23 2018-08-31 Aclaris Therapeutics, Inc. 用於治疗炎症和癌症的杂环itk抑制剂
JP6709792B2 (ja) 2015-01-29 2020-06-17 ジェネンテック, インコーポレイテッド 治療用化合物およびその使用

Also Published As

Publication number Publication date
US20170342067A1 (en) 2017-11-30
CN107108614A (zh) 2017-08-29
JP2017533249A (ja) 2017-11-09
WO2016077380A1 (en) 2016-05-19
US10150767B2 (en) 2018-12-11
EP3218374A1 (en) 2017-09-20
HK1243076A1 (zh) 2018-07-06
EP3218374B1 (en) 2021-12-29
MA40940A (fr) 2017-09-19
CN107108614B (zh) 2021-06-01

Similar Documents

Publication Publication Date Title
JP6669745B2 (ja) ブロモドメインのインヒビターとしての置換ピロロピリジン
JP6669744B2 (ja) ブロモドメインのインヒビターとしての置換ピロロピリジン
JP6639497B2 (ja) ブロモドメインインヒビターおよびその使用
JP6636031B2 (ja) 治療用化合物およびその使用
JP6847844B2 (ja) 治療用ピリダジン化合物およびその使用
JP6767969B2 (ja) がんの処置における使用のためのpcafおよびgcn5阻害剤としての式(i)のフタラジン誘導体
CN107074823B (zh) 治疗性化合物及其用途
JP6709792B2 (ja) 治療用化合物およびその使用
JP6659703B2 (ja) ピリダジノン誘導体および癌の処置におけるそれらの使用
HK1243076B (zh) 作為布羅莫結構域抑制劑的取代的吡咯並吡啶
HK1242696A1 (en) Therapeutic compounds and uses thereof
HK1247193A1 (en) Pyridazinone derivatives and their use in the treatment of cancer
HK1247193B (zh) 噠嗪酮衍生物及其在治療癌症中的用途
HK1242696B (zh) 治療性化合物及其用途
HK1242695A1 (en) Phthalazine derivatives of formula (i) as pcaf and gcn5 inhibitors for use in the treatment of cancer
HK1242695B (zh) 作為用於治療癌症的pcaf和gcn5抑制劑的式(i)的酞嗪衍生物

Legal Events

Date Code Title Description
RD03 Notification of appointment of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7423

Effective date: 20171018

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20171018

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181108

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20181108

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190718

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20190718

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20191017

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200120

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

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20200130

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20200227

R150 Certificate of patent or registration of utility model

Ref document number: 6669745

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees