[go: up one dir, main page]

EA201692203A1 - Соединения, ингибирующие tank-связывающую киназу - Google Patents

Соединения, ингибирующие tank-связывающую киназу

Info

Publication number
EA201692203A1
EA201692203A1 EA201692203A EA201692203A EA201692203A1 EA 201692203 A1 EA201692203 A1 EA 201692203A1 EA 201692203 A EA201692203 A EA 201692203A EA 201692203 A EA201692203 A EA 201692203A EA 201692203 A1 EA201692203 A1 EA 201692203A1
Authority
EA
Eurasian Patent Office
Prior art keywords
kinaz
binding
tank
inhibiting compounds
compounds
Prior art date
Application number
EA201692203A
Other languages
English (en)
Other versions
EA031757B1 (ru
Inventor
Чжиминь Ду
Хуан Арнальдо Герреро
Джошуа Аарон Каплан
Джон Эдвард Нокс Джр.
Деван Надутхамби
Бартон В. Филлипс
Чандрасекар Венкатарамани
Пейюань Ван
Уильям Дж. Уоткинс
Джефф Заблоцки
Original Assignee
Джилид Сайэнс, Инк.
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 Джилид Сайэнс, Инк. filed Critical Джилид Сайэнс, Инк.
Publication of EA201692203A1 publication Critical patent/EA201692203A1/ru
Publication of EA031757B1 publication Critical patent/EA031757B1/ru

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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • 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
    • A61K31/495—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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61P1/04—Drugs 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Описаны соединения, имеющие следующую формулу (I), и способы их применения и получения
EA201692203A 2014-06-03 2015-06-02 Соединения, ингибирующие tank-связывающую киназу EA031757B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462007322P 2014-06-03 2014-06-03
PCT/US2015/033769 WO2015187684A1 (en) 2014-06-03 2015-06-02 Tank-binding kinase inhibitor compounds

Publications (2)

Publication Number Publication Date
EA201692203A1 true EA201692203A1 (ru) 2017-06-30
EA031757B1 EA031757B1 (ru) 2019-02-28

Family

ID=53546688

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201692203A EA031757B1 (ru) 2014-06-03 2015-06-02 Соединения, ингибирующие tank-связывающую киназу

Country Status (19)

Country Link
US (2) US10072001B2 (ru)
EP (1) EP3152210B1 (ru)
JP (2) JP6378785B2 (ru)
KR (2) KR20180131640A (ru)
CN (1) CN106459044A (ru)
AR (1) AR100702A1 (ru)
AU (2) AU2015271837B2 (ru)
BR (1) BR112016028288A2 (ru)
CA (1) CA2951126A1 (ru)
EA (1) EA031757B1 (ru)
ES (1) ES2961577T3 (ru)
HK (1) HK1231475A1 (ru)
IL (1) IL248888A0 (ru)
MA (1) MA40058A (ru)
MX (1) MX2016015862A (ru)
NZ (1) NZ726317A (ru)
SG (1) SG11201609570SA (ru)
TW (1) TW201613916A (ru)
WO (1) WO2015187684A1 (ru)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013106643A2 (en) 2012-01-12 2013-07-18 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
ES2881195T3 (es) 2014-09-26 2021-11-29 Gilead Sciences Inc Derivados de aminotriazina útiles como compuestos inhibidores de quinasas que se unen a TANK
WO2016077595A1 (en) 2014-11-12 2016-05-19 The General Hospital Corporation Methods for treating neurodegenerative diseases
KR20230119040A (ko) 2015-01-20 2023-08-14 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적화된 분해를 위한 화합물 및방법
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
EP4414369A3 (en) 2015-03-18 2024-10-16 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
EP3302482A4 (en) 2015-06-05 2018-12-19 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EP3362449B1 (en) * 2015-10-13 2021-06-16 Institut National de la Santé et de la Recherche Médicale (INSERM) Sibiriline derivatives for use for preventing and/or treating disorders associated with cellular necroptosis
PL3383392T3 (pl) 2015-12-04 2025-11-17 Global Blood Therapeutics, Inc. Schematy dawkowania dla 2-hydroksy-6-((2-(1-izopropylo-1H-pirazol-5-ilo)pirydyn3-ylo)metoksy)benzaldehydu
JP2019500368A (ja) 2015-12-17 2019-01-10 ギリアード サイエンシーズ， インコーポレイテッド Ｔａｎｋ結合キナーゼ阻害剤化合物
EP3390387B1 (en) 2015-12-18 2021-11-17 Bayer Pharma Aktiengesellschaft Heteroarylbenzimidazole compounds
WO2017173451A1 (en) * 2016-04-01 2017-10-05 The General Hospital Corporation Targeting innate immune signaling in neuroinflammation and neurodegeneration
JP7017521B2 (ja) 2016-04-15 2022-02-08 ブループリント メディシンズ コーポレイション アクチビン受容体様キナーゼの阻害剤
WO2017207534A1 (en) 2016-06-03 2017-12-07 Bayer Pharma Aktiengesellschaft Substituted heteroarylbenzimidazole compounds
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
KR102173463B1 (ko) 2016-10-11 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적 분해용 화합물 및 방법
EP3535265A4 (en) 2016-11-01 2020-07-08 Arvinas, Inc. PROTACS TARGETING ON TAU PROTEIN AND RELATED METHODS FOR USE
HUE064609T2 (hu) 2016-12-01 2024-04-28 Arvinas Operations Inc Tetrahidronaftalin és tetrahidroizokinolin származékok mint ösztrogénreceptor-lebontó anyagok
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US10723717B2 (en) 2016-12-23 2020-07-28 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
EP3559002A4 (en) 2016-12-23 2021-02-17 Arvinas Operations, Inc. CHEMERICAL MOLECULES TARGETING EGFR PROTEOLYSIS AND RELATED METHODS OF USE
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
CA3049912A1 (en) 2017-01-26 2018-08-02 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
JP2020506922A (ja) 2017-01-31 2020-03-05 アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． セレブロンリガンド、およびセレブロンリガンドを含有する二官能性化合物
SG11201908240YA (en) 2017-03-31 2019-10-30 Dana Farber Cancer Inst Inc Methods for evaluating tumor cell spheroids using 3d microfluidic cell culture device
CN111566102B (zh) 2017-10-18 2023-09-08 缆图药品公司 作为激活素受体样激酶抑制剂的取代的吡咯并吡啶
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
WO2019148055A1 (en) 2018-01-26 2019-08-01 Yale University Imide-based modulators of proteolysis and methods of use
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
CN112218859B (zh) 2018-04-04 2024-10-29 阿尔维纳斯运营股份有限公司 蛋白水解调节剂及相关使用方法
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
BR112022003490A2 (pt) 2019-08-26 2022-05-24 Arvinas Operations Inc Método de tratamento do câncer de mama e mama metastático, método para degradação seletiva, método para inibir uma quinase, kit, composição líquida, e, método de produção de uma composição líquida
EP4045496A1 (en) 2019-10-17 2022-08-24 Arvinas Operations, Inc. Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety
CR20220353A (es) 2019-12-19 2022-10-20 Arvinas Operations Inc Compuestos y métodos para la degradación dirigida del receptor de andrógenos
CN113549065B (zh) * 2020-04-24 2022-05-10 成都先导药物开发股份有限公司 作为JAK抑制剂的吡咯并[2,3-b]吡啶衍生物
TW202208345A (zh) 2020-05-09 2022-03-01 美商亞文納營運公司 雙官能性化合物的製造方法、該雙官能性化合物的超純形式、及含彼之劑型
JP2023539663A (ja) 2020-08-28 2023-09-15 アルビナス・オペレーションズ・インコーポレイテッド 急速進行性線維肉腫タンパク質分解化合物及び関連する使用方法
IL301155A (en) 2020-09-14 2023-05-01 Arvinas Operations Inc Crystalline forms of a compound for the targeted degradation of estrogen receptor
CN114622017A (zh) * 2020-12-14 2022-06-14 中山大学孙逸仙纪念医院 Isg15、isg15诱导的巨噬细胞及其分泌物在肿瘤治疗中的应用
AU2022259683A1 (en) 2021-04-16 2023-10-19 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use
CN120187726A (zh) * 2022-10-27 2025-06-20 香港科技大学 嘧啶并吡咯类似物
WO2024159164A2 (en) 2023-01-26 2024-08-02 Arvinas Operations, Inc. Cereblon-based kras degrading protacs ans uses related thereto
WO2025122895A1 (en) 2023-12-08 2025-06-12 Arvinas Operations, Inc. Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
GB0402809D0 (en) 2004-02-09 2004-03-10 Glaxo Group Ltd Chemical compounds
LT2612862T (lt) 2004-05-13 2017-01-25 Icos Corporation Chinazolinonai kaip žmogaus fosfatidilinozitol-3-kinazės delta inhibitoriai
WO2007002325A1 (en) * 2005-06-22 2007-01-04 Plexxikon, Inc. Pyrrolo[2,3-b] pyridine derivatives as protein kinase inhibitors
JP2010526027A (ja) * 2007-01-23 2010-07-29 パラウ・フアルマ・ソシエダツド・アノニマ プリン誘導体
KR101737753B1 (ko) 2007-03-12 2017-05-18 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 페닐 아미노 피리미딘 화합물 및 이의 용도
WO2009030890A1 (en) 2007-09-03 2009-03-12 University Court Of The University Of Dundee Pyrimidine compounds for the treatment of cancer, septic shock and/or primary open angle glaucoma
US20120009151A1 (en) 2007-12-21 2012-01-12 Progenics Pharmaceuticals, Inc. Triazines And Related Compounds Having Antiviral Activity, Compositions And Methods Thereof
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
GB0805477D0 (en) 2008-03-26 2008-04-30 Univ Nottingham Pyrimidines triazines and their use as pharmaceutical agents
US20100056524A1 (en) 2008-04-02 2010-03-04 Mciver Edward Giles Compound
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
GB0903759D0 (en) 2009-03-04 2009-04-15 Medical Res Council Compound
DE102009019962A1 (de) 2009-05-05 2010-11-11 Merck Patent Gmbh 3-([1,2,3]Triazol-4-yl)-pyrrolo[2,3-b]pyridinderivate
KR20120114224A (ko) * 2009-10-12 2012-10-16 마이렉시스 인코포레이티드 Ｉｋｋ 엡실론 및/또는 ｔｂｋ１의 억제제로서의 아미노-피리미딘 화합물
CN102666545B (zh) 2009-10-20 2016-04-06 塞尔卓姆有限公司 作为jak抑制剂的杂环吡唑并嘧啶类似物
GB201012105D0 (en) 2010-07-19 2010-09-01 Domainex Ltd Novel pyrimidine compounds
DE102010049877A1 (de) 2010-11-01 2012-05-03 Merck Patent Gmbh 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate
DE102011008352A1 (de) 2011-01-12 2012-07-12 Merck Patent Gmbh 5-([1,2,3]Triazol-4-yl)-7H-pyrrolo-[2,3-d]pyrimidinderivate
DE102011009961A1 (de) 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
CN103732067A (zh) 2011-04-12 2014-04-16 美国阿尔茨海默病研究所公司 化合物，组合物及它们的治疗用途
EP2714668B9 (en) 2011-05-23 2017-06-14 Merck Patent GmbH Thiazole derivatives
HRP20181884T1 (hr) 2011-05-23 2019-01-11 Merck Patent Gmbh Derivati piridina i pirazina
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
GB201114051D0 (en) 2011-08-15 2011-09-28 Domainex Ltd Compounds and their uses
EP2562265A1 (en) 2011-08-22 2013-02-27 Lead Discovery Center GmbH Susceptibility to selective CDK9 inhibitors
DE102011111400A1 (de) 2011-08-23 2013-02-28 Merck Patent Gmbh Bicyclische heteroaromatische Verbindungen
DE102011112978A1 (de) 2011-09-09 2013-03-14 Merck Patent Gmbh Benzonitrilderivate
DE102011119127A1 (de) 2011-11-22 2013-05-23 Merck Patent Gmbh 3-Cyanaryl-1H-pyrrolo[2.3-b]pyridin-Derivate
EP2788000B1 (en) 2011-12-06 2018-05-30 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
JP6144698B2 (ja) 2011-12-20 2017-06-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｈｉｖ複製の阻害剤としての縮合三環式化合物
SI2812337T1 (sl) 2012-02-09 2017-01-31 Merck Patent Gmbh Furo (3,2-b) in tieno (3,2-b) piridinski derivati kot zaviralci tbk1 in ikk
WO2014004863A2 (en) 2012-06-27 2014-01-03 Alzheimer's Institute Of America, Inc. Compounds, compositions, and therapeutic uses thereof
GB201303109D0 (en) 2013-02-21 2013-04-10 Domainex Ltd Novel pyrimidine compounds
TW201444836A (zh) 2013-03-14 2014-12-01 Abbvie Inc 吡咯并［２，３－ｂ］吡啶ｃｄｋ９激酶抑制劑
CN103251600B (zh) 2013-05-27 2015-05-20 中南大学 2-氨基-4-(3′-氰基-4′-吡咯烷基)苯基嘧啶化合物的抗肿瘤应用
US10370664B2 (en) 2013-11-07 2019-08-06 University Of Southern California Use of IKK epsilon inhibitors to activate NFAT and T cell response
EP3080122B1 (en) * 2013-12-11 2018-10-31 Biogen MA Inc. Biaryl compounds useful for the treatment of human diseases in oncology, neurology and immunology
US9598424B2 (en) 2014-03-06 2017-03-21 Takeda Pharmaceutical Company Limited Heteroarylamide inhibitors of TBK1
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
ES2881195T3 (es) 2014-09-26 2021-11-29 Gilead Sciences Inc Derivados de aminotriazina útiles como compuestos inhibidores de quinasas que se unen a TANK
US9994547B2 (en) 2014-10-06 2018-06-12 Takeda Pharmaceutical Company Limited Heteroarylamide inhibitors of TBK1
CN108473478A (zh) 2015-06-29 2018-08-31 默克专利有限公司 TBK/IKKε抑制剂化合物及其用途
JP2019500368A (ja) 2015-12-17 2019-01-10 ギリアード サイエンシーズ， インコーポレイテッド Ｔａｎｋ結合キナーゼ阻害剤化合物
WO2018170488A1 (en) 2017-03-17 2018-09-20 Gilead Sciences, Inc. Method of purifying an antibody

Also Published As

Publication number Publication date
CN106459044A (zh) 2017-02-22
AU2015271837A1 (en) 2016-12-01
US20150344473A1 (en) 2015-12-03
US20190016717A1 (en) 2019-01-17
KR20180131640A (ko) 2018-12-10
EP3152210B1 (en) 2023-07-05
KR101926245B1 (ko) 2018-12-06
HK1231475A1 (zh) 2017-12-22
KR20170005876A (ko) 2017-01-16
MA40058A (fr) 2015-12-10
JP2018150358A (ja) 2018-09-27
AU2015271837B2 (en) 2018-06-14
WO2015187684A1 (en) 2015-12-10
AU2018208766A1 (en) 2018-08-16
CA2951126A1 (en) 2015-12-10
BR112016028288A2 (pt) 2017-08-22
EP3152210A1 (en) 2017-04-12
MX2016015862A (es) 2017-03-27
US10259811B2 (en) 2019-04-16
ES2961577T3 (es) 2024-03-12
SG11201609570SA (en) 2016-12-29
TW201613916A (en) 2016-04-16
JP6378785B2 (ja) 2018-08-22
NZ726317A (en) 2018-05-25
EA031757B1 (ru) 2019-02-28
JP2017516814A (ja) 2017-06-22
IL248888A0 (en) 2017-01-31
AR100702A1 (es) 2016-10-26
US10072001B2 (en) 2018-09-11
EP3152210C0 (en) 2023-07-05

Similar Documents

Publication Publication Date Title
EA201692203A1 (ru) Соединения, ингибирующие tank-связывающую киназу
EA201891024A1 (ru) Соединения-ингибиторы tank-связывающей киназы
EA201790395A1 (ru) Производные аминотриазина, подходящие для применения в качестве соединений-ингибиторов tank-связывающей киназы
GEAP201914379A (en) Heteroaryl compounds for kinase inhibition
EA201692219A1 (ru) Способы получения противовирусных соединений
EA201591420A1 (ru) Гетероарильные соединения и их применение
GEAP201814288A (en) Bicyclic-fused heteroaryl or aryl compounds and their use as irak4 inhibitors
LT3594238T (lt) Antikūno kompozicijos, skirtos navikų gydymui
EA201891211A1 (ru) Ингибиторы cxcr2
GEAP201814347A (en) Substituted dihydroisoquinoline compounds
EA201791420A1 (ru) Соединения триазолопиримидина и их применения
LT3190113T (lt) Pirolopirimidino junginiai, naudotini kaip tlr7 agonistai
DK3119762T3 (da) Benzimidazol-derivater som erbb-tyrosin-kinase-inhibitorer til behandlingen af kræft
BR112017005266A2 (pt) inibidores de mk2 e uso dos mesmos
EA201591728A1 (ru) Гетероциклические соединения и способы их применения
EA201691272A1 (ru) Тетрагидропиридопиразины в качестве модуляторов gpr6
EA201692526A1 (ru) Замещенные [1,2,4]триазольные соединения
EA201591634A1 (ru) Дигидропиридопиримидиновые соединения
EA201500801A1 (ru) Бензохинолоновые ингибиторы vmat2
IL252089B (en) 2-amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors
EA201590552A1 (ru) Аминохинолины в качестве ингибиторов киназы
PL3400269T3 (pl) Zastosowanie 4-bora-3a,4a-diaza-s-indacenów do zabezpieczania
LT3210973T (lt) Heteroarilo junginiai, skirti akių ligų gydymui
EA201790982A1 (ru) Синтез копанлисиба и его дигидрохлорида
EA201790156A1 (ru) Азетидинилоксифенилпирролидиновые соединения

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU