BR112015032623A2 - composto, composição farmacêutica, métodos para tratar doenças e condições, e para degradar o receptor de estrogênio, usos de um composto e de uma combinação, e, combinação - Google Patents

composto, composição farmacêutica, métodos para tratar doenças e condições, e para degradar o receptor de estrogênio, usos de um composto e de uma combinação, e, combinação

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Publication number
BR112015032623A2
BR112015032623A2 BR112015032623A BR112015032623A BR112015032623A2 BR 112015032623 A2 BR112015032623 A2 BR 112015032623A2 BR 112015032623 A BR112015032623 A BR 112015032623A BR 112015032623 A BR112015032623 A BR 112015032623A BR 112015032623 A2 BR112015032623 A2 BR 112015032623A2
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BR
Brazil
Prior art keywords
compound
combination
estrogen receptor
conditions
degrading
Prior art date
Application number
BR112015032623A
Other languages
English (en)
Other versions
BR112015032623B1 (pt
BR112015032623A8 (pt
Inventor
Hussain Miah Afjal
Edward David Smith Ian
David Harling John
Andre Campos Sebastien
Original Assignee
Glaxosmithkline Ip Dev 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.)
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Publication date
Application filed by Glaxosmithkline Ip Dev Ltd filed Critical Glaxosmithkline Ip Dev Ltd
Publication of BR112015032623A2 publication Critical patent/BR112015032623A2/pt
Publication of BR112015032623A8 publication Critical patent/BR112015032623A8/pt
Publication of BR112015032623B1 publication Critical patent/BR112015032623B1/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

1 / 1 resumo “composto, composiã‡ãƒo farmacãšutica, mã‰todos para tratar doenã‡as e condiã‡ã•es, e para degradar o receptor de estrogãšnio, usos de um composto e de uma combinaã‡ãƒo, e, combinaã‡ãƒo ” um composto de fã³rmula (i), ou um seu sal farmaceuticamente aceitã¡vel, composiã§ãµes, combinaã§ãµes e medicamentos contendo referidos compostos e processos para sua preparaã§ã£o. a invenã§ã£o tambã©m se refere ao uso dos referidos compostos, combinaã§ãµes, composiã§ãµes e medicamentos, por exemplo, como inibidores da atividade do receptor de estrogãªnio, incluindo a degradaã§ã£o do receptor de estrogãªnio, o tratamento de doenã§as e patologias mediadas pelo receptor de estrogãªnio.
BR112015032623-4A 2013-07-03 2014-07-01 Composto, composição farmacêutica, combinação, e, uso de um composto BR112015032623B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1311888.0 2013-07-03
GBGB1311888.0A GB201311888D0 (en) 2013-07-03 2013-07-03 Novel compounds
PCT/EP2014/063899 WO2015000867A1 (en) 2013-07-03 2014-07-01 Benzothiophene derivatives as estrogen receptor inhibitors

Publications (3)

Publication Number Publication Date
BR112015032623A2 true BR112015032623A2 (pt) 2017-07-25
BR112015032623A8 BR112015032623A8 (pt) 2020-01-14
BR112015032623B1 BR112015032623B1 (pt) 2022-01-11

Family

ID=48999418

Family Applications (1)

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BR112015032623-4A BR112015032623B1 (pt) 2013-07-03 2014-07-01 Composto, composição farmacêutica, combinação, e, uso de um composto

Country Status (13)

Country Link
US (1) US9988376B2 (pt)
EP (1) EP3016947B1 (pt)
JP (1) JP6401258B2 (pt)
KR (1) KR102130745B1 (pt)
CN (1) CN105452244A (pt)
AU (1) AU2014286342B2 (pt)
BR (1) BR112015032623B1 (pt)
CA (1) CA2915782C (pt)
ES (1) ES2697686T3 (pt)
GB (1) GB201311888D0 (pt)
MX (1) MX363127B (pt)
RU (1) RU2015154955A (pt)
WO (1) WO2015000867A1 (pt)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102668696B1 (ko) * 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
EP3247708A4 (en) * 2015-01-20 2018-09-12 Arvinas, Inc. Compounds and methods for the targeted degradation of the androgen receptor
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
JP7269731B2 (ja) * 2015-03-18 2023-05-09 アルビナス・オペレーションズ・インコーポレイテッド 標的タンパク質の分解向上のための化合物および方法
GB201506871D0 (en) 2015-04-22 2015-06-03 Glaxosmithkline Ip Dev Ltd Novel compounds
US20180147202A1 (en) 2015-06-05 2018-05-31 Arvinas, Inc. TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE
WO2017030814A1 (en) 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
BR112018008918A8 (pt) 2015-11-02 2019-02-26 Univ Yale compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos
WO2017100715A1 (en) 2015-12-09 2017-06-15 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective estrogen receptor downregulator compounds
BR112018071408A2 (pt) * 2016-04-20 2019-02-05 Glaxosmithkline Ip Dev Ltd “composto inibidor de rip2 quinase, composição farmacêutica, usos de um composto e de uma combinação, e, combinação
WO2017185036A1 (en) 2016-04-22 2017-10-26 Dana Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
WO2017185023A1 (en) * 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Degradation of cyclin-dependent kinase 9 (cdk9) by conjugation of cdk9 inhibitors with e3 ligase ligand and methods of use
GB201610156D0 (en) 2016-06-10 2016-07-27 Otsuka Pharma Co Ltd Cliptac compositions
GB2554071A (en) * 2016-09-14 2018-03-28 Univ Dundee Small molecules
US20180072711A1 (en) 2016-09-15 2018-03-15 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
JP6899993B2 (ja) * 2016-10-04 2021-07-07 国立医薬品食品衛生研究所長 複素環化合物
RS64208B1 (sr) 2016-10-11 2023-06-30 Arvinas Operations Inc Jedinjenja i metode za ciljanu degradaciju androgenog receptora
WO2018081168A2 (en) * 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
AU2017367872B2 (en) 2016-11-01 2022-03-31 Arvinas, Inc. Tau-protein targeting protacs and associated methods of use
KR102173464B1 (ko) 2016-12-01 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
WO2018119448A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
WO2018119441A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
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
BR112019013814A2 (pt) 2017-01-06 2020-01-21 G1 Therapeutics Inc método para tratamento de câncer ou de um tumor em um indivíduo, composição farmacêutica, combinação, e, kit.
MX2019008934A (es) * 2017-01-26 2019-11-05 Arvinas Operations Inc Moduladores de la proteolisis del receptor de estrogeno y métodos asociados de uso,.
JP2020507566A (ja) 2017-02-10 2020-03-12 ジー１ セラピューティクス， インコーポレイテッド ベンゾチオフェンエストロゲン受容体モジュレーター
RU2020108515A (ru) * 2017-07-28 2021-08-27 Эрвинэс Оперейшнс, Инк. Соединения и способы целевого расщепления андрогенного рецептора
EP3710443A1 (en) 2017-11-17 2020-09-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides
US10519152B2 (en) 2017-12-21 2019-12-31 Astrazeneca Ab Compounds and their use in treating cancer
US11220515B2 (en) 2018-01-26 2022-01-11 Yale University Imide-based modulators of proteolysis and associated methods of use
MX2020010420A (es) 2018-04-04 2020-12-11 Arvinas Operations Inc Moduladores de la proteólisis y métodos asociados de uso.
EP3831811A4 (en) 2018-07-31 2022-04-20 Fimecs, Inc. HETEROCYCLIC COMPOUND
JP7297053B2 (ja) 2018-08-20 2023-06-23 アルビナス・オペレーションズ・インコーポレイテッド 神経変性疾患を治療するためのｅ３ユビキチンリガーゼ結合活性を有するキメラ（ｐｒｏｔａｃ）化合物を標的とし、アルファ－シヌクレインタンパク質を標的とするタンパク質分解
CN111205282B (zh) * 2018-11-21 2023-12-01 上海科技大学 Er蛋白调节剂及其应用
KR20210136973A (ko) * 2019-01-03 2021-11-17 더 리젠츠 오브 더 유니버시티 오브 미시간 에스트로겐 수용체 단백질 분해제
EP3999182A1 (en) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Tau-protein targeting compounds and associated methods of use
BR112022012110A2 (pt) 2019-12-19 2022-12-13 Arvinas Operations Inc Compostos e métodos para a degradação direcionada de receptor androgênico
WO2022161166A1 (zh) * 2021-01-28 2022-08-04 江苏亚虹医药科技股份有限公司 靶向嵌合化合物、含其的药物组合物及其制备方法和用途
CN117279910A (zh) 2021-04-16 2023-12-22 阿尔维纳斯运营股份有限公司 Bcl6蛋白水解的调节剂和其相关使用方法
WO2024054591A1 (en) 2022-09-07 2024-03-14 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
GB202214796D0 (en) 2022-10-07 2022-11-23 Tocris Cookson Ltd Compounds

Family Cites Families (234)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4160452A (en) 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5007790A (en) 1989-04-11 1991-04-16 Depomed Systems, Inc. Sustained-release oral drug dosage form
US5169645A (en) 1989-10-31 1992-12-08 Duquesne University Of The Holy Ghost Directly compressible granules having improved flow properties
US6316003B1 (en) 1989-12-21 2001-11-13 Whitehead Institute For Biomedical Research Tat-derived transport polypeptides
US5292638A (en) 1990-12-07 1994-03-08 The Regents Of The University Of California Method of determining functional estrogen receptors for prognosis of cancer
DK0632720T3 (da) 1992-03-25 1999-07-26 Depomed Inc Hydroxyethylcellulosebaserede depotpræparat-doseringsformer
US5582837A (en) 1992-03-25 1996-12-10 Depomed, Inc. Alkyl-substituted cellulose-based sustained-release oral drug dosage forms
DK0693054T3 (da) 1993-04-07 1998-10-19 Pfizer Cycloalkylhydroxyurinstoffer og deres anvendelse som lipoxygenaseinhibitorer
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US20030036654A1 (en) 1994-08-18 2003-02-20 Holt Dennis A. Synthetic multimerizing agents
US5510357A (en) 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
WO1996032937A1 (en) * 1995-04-21 1996-10-24 Eli Lilly And Company Benzothiophenes with novel basic side chains
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
WO1997040065A2 (en) 1996-04-24 1997-10-30 Peptide Therapeutics Limited Substrates and inhibitors of proteolytic enzymes
CA2204082A1 (en) 1996-05-03 1997-11-03 Michael William John Urquhart Pharmaceutical compounds
WO1997047285A1 (en) 1996-06-10 1997-12-18 Depomed, Inc. Gastric-retentive oral controlled drug delivery system with enhanced retention properties
US5972389A (en) 1996-09-19 1999-10-26 Depomed, Inc. Gastric-retentive, oral drug dosage forms for the controlled-release of sparingly soluble drugs and insoluble matter
HRP970566A2 (en) 1996-10-30 1998-08-31 Jones Deborah Defeo Conjugates useful in the treatment of prostate canser
ZA982818B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Prevention of breast cancer using selective estrogen receptor modulators.
ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
ATE460423T1 (de) 1997-05-14 2010-03-15 Sloan Kettering Inst Cancer Verfahren und zubereitungen zur zerstörung bestimmter proteine
US6635280B2 (en) 1997-06-06 2003-10-21 Depomed, Inc. Extending the duration of drug release within the stomach during the fed mode
PT998271E (pt) 1997-06-06 2005-10-31 Depomed Inc Formas de dosagem oral de farmacos com retencao gastrica para a libertacao controlada de farmacos altamente soluveis
AU740597B2 (en) 1997-07-10 2001-11-08 Merck & Co., Inc. Conjugates useful in the treatment of prostate cancer
DE69832715T2 (de) 1997-07-12 2007-01-11 Cancer Research Technology Ltd. Cyclin-abhängige-kinase inhibierende purinderivate
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
AU9386198A (en) 1997-09-10 1999-03-29 President And Fellows Of Harvard College Inducible methods for repressing gene function
WO1999015521A1 (en) * 1997-09-23 1999-04-01 Eli Lilly And Company Benzothiophenes
US6323219B1 (en) 1998-04-02 2001-11-27 Ortho-Mcneil Pharmaceutical, Inc. Methods for treating immunomediated inflammatory disorders
AU4093799A (en) 1998-05-22 1999-12-13 Board Of Trustees Of The Leland Stanford Junior University Bifunctional molecules and therapies based thereon
WO2000022110A2 (en) 1998-10-09 2000-04-20 President And Fellows Of Harvard College Targeted proteolysis by recruitment to ubiquitin protein ligases
US6306663B1 (en) 1999-02-12 2001-10-23 Proteinex, Inc. Controlling protein levels in eucaryotic organisms
US6858709B1 (en) 1999-02-26 2005-02-22 Oklahoma Medical Research Foundation Component of von Hippel-Lindau tumor suppressor complex and SCF ubiquitin ligase
CA2362520A1 (en) 1999-02-26 2000-08-31 Joan W. Conaway Novel component of von hippel-lindau tumor suppressor complex and scf ubiquitin ligase
JP2002543129A (ja) 1999-05-05 2002-12-17 メルク エンド カムパニー インコーポレーテッド 抗微生物剤としての新規なプロリン類
US7087386B2 (en) 1999-06-11 2006-08-08 The Burnham Institute Nucleic acid encoding proteins involved in protein degradation, products and methods related thereto
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
JP2003512339A (ja) 1999-10-19 2003-04-02 メルク エンド カムパニー インコーポレーテッド 前立腺癌の治療に有用な複合体
MXPA02004413A (es) 1999-11-02 2002-09-02 Depomed Inc Induccion farmacologica del modo de alimentacion, para la administracion aumentada de drogas al estomago.
AU1434201A (en) * 1999-11-19 2001-05-30 Eli Lilly And Company Antithrombotic agents
DE60123384T2 (de) 2000-02-04 2007-08-02 DepoMed, Inc., Menlo Park Dosierungsform des typs "hülle und kern" mit einer wirkstofffreisetzung, die sich der nullten ordnung annähert
US6740495B1 (en) 2000-04-03 2004-05-25 Rigel Pharmaceuticals, Inc. Ubiquitin ligase assay
US6488962B1 (en) 2000-06-20 2002-12-03 Depomed, Inc. Tablet shapes to enhance gastric retention of swellable controlled-release oral dosage forms
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
WO2002020740A2 (en) 2000-09-08 2002-03-14 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
US6451808B1 (en) 2000-10-17 2002-09-17 Depomed, Inc. Inhibition of emetic effect of metformin with 5-HT3 receptor antagonists
EP1360205A1 (en) 2001-02-16 2003-11-12 E.I. Dupont De Nemours And Company Angiogenesis-inhibitory tripeptides, compositions and their methods of use
GB0106953D0 (en) 2001-03-20 2001-05-09 Univ Aberdeen Neufofibrillary labels
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
MXPA03011096A (es) 2001-05-29 2004-12-06 Depomed Dev Ltd Metodo para el tratamiento de la enfermedad de reflujo gastroesofagico y la saturacion acida nocturna.
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
JP4342939B2 (ja) 2001-08-03 2009-10-14 バーテックス ファーマシューティカルズ インコーポレイテッド ピラゾール誘導キナーゼインヒビターおよびその使用
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
EP1434579B1 (en) 2001-10-09 2011-06-08 Amgen Inc. Imidazole derivatives as antiinflammatory agents
US20030133927A1 (en) 2001-10-10 2003-07-17 Defeo-Jones Deborah Conjugates useful in the treatment of prostate cancer
CA2409552A1 (en) 2001-10-25 2003-04-25 Depomed, Inc. Gastric retentive oral dosage form with restricted drug release in the lower gastrointestinal tract
CA2464561A1 (en) 2001-10-25 2003-05-01 Depomed, Inc. Methods of treatment using a gastric retained losartan dosage
US6723340B2 (en) 2001-10-25 2004-04-20 Depomed, Inc. Optimal polymer mixtures for gastric retentive tablets
TWI312285B (en) 2001-10-25 2009-07-21 Depomed Inc Methods of treatment using a gastric retained gabapentin dosage
US20030091630A1 (en) 2001-10-25 2003-05-15 Jenny Louie-Helm Formulation of an erodible, gastric retentive oral dosage form using in vitro disintegration test data
US7053046B2 (en) 2001-12-21 2006-05-30 Mcgrath Kevin Peptide activators of VEGF
US6682759B2 (en) 2002-02-01 2004-01-27 Depomed, Inc. Manufacture of oral dosage forms delivering both immediate-release and sustained-release drugs
EP1519918A1 (en) 2002-07-02 2005-04-06 Novartis AG Peptide inhibitors of smac protein binding to inhibitor of apoptosis proteins (iap)
US20040053324A1 (en) 2002-08-30 2004-03-18 Brian Wong Assays and compositions for identifying agents that modulate the activity of deubiquitinating agents
US20040114258A1 (en) 2002-12-17 2004-06-17 Harris Richard Alexander Device and method for combining dynamic mathematical expressions and other multimedia objects within a document
KR20050090415A (ko) 2002-12-25 2005-09-13 이데미쓰 고산 가부시키가이샤 아다만테인 유도체 및 그의 제조 방법
WO2004093871A1 (en) 2003-03-27 2004-11-04 Lankenau Institute For Medical Research Novel methods for the treatment of cancer
WO2004100868A2 (en) 2003-04-23 2004-11-25 Abbott Laboratories Method of treating transplant rejection
US7915293B2 (en) 2003-05-30 2011-03-29 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
US20070281907A1 (en) 2003-12-22 2007-12-06 Watkins William J Kinase Inhibitor Phosphonate Conjugates
BRPI0506883A (pt) 2004-01-16 2007-05-29 Univ Michigan miméticos de smac conformacionalmente comprimidos e seus usos
AU2005228950B2 (en) 2004-03-23 2012-02-02 Genentech, Inc. Azabicyclo-octane inhibitors of IAP
AR048927A1 (es) 2004-04-07 2006-06-14 Novartis Ag Compuestos heterociclicos como inhibidores de proteinas de apoptosis (iap); composiciones farmaceuticas que los contienen y su uso en el tratamiento de una enfermedad proliferativa
MEP8409A (en) 2004-06-02 2011-12-20 Fused heterocyclic compound
CA2570321C (en) 2004-07-02 2013-10-08 Genentech, Inc. Inhibitors of iap
WO2006006065A1 (en) 2004-07-08 2006-01-19 Warner-Lambert Company Llc Androgen modulators
CN103251953A (zh) 2004-07-19 2013-08-21 约翰·霍普金斯大学 供免疫抑制的flt3抑制剂
US7294748B2 (en) 2004-10-19 2007-11-13 Wake Forest University Health Sciences Sulfenic acid-reactive compounds and their methods of synthesis
WO2006062685A2 (en) 2004-11-11 2006-06-15 Affymax, Inc. Novel peptides that bind to the erythropoietin receptor
GB0426661D0 (en) 2004-12-06 2005-01-05 Isis Innovation Pyrrolidine compounds
EA019420B1 (ru) 2004-12-20 2014-03-31 Дженентех, Инк. Пирролидиновые ингибиторы иап (ингибиторов апоптоза)
CN103083644B (zh) 2005-02-25 2014-05-28 泰特拉洛吉克药业公司 Iap二聚体抑制剂
CN100383139C (zh) 2005-04-07 2008-04-23 天津和美生物技术有限公司 可抑制细胞释放肿瘤坏死因子的哌啶-2，6-二酮衍生物
US20060252698A1 (en) 2005-04-20 2006-11-09 Malcolm Bruce A Compounds for inhibiting cathepsin activity
GEP20217221B (en) 2005-05-10 2021-02-10 Incyte Holdings Corp Us Modulators of indoleamine 2,3-dioxygenase and methods of using the same
FR2885904B1 (fr) 2005-05-19 2007-07-06 Aventis Pharma Sa Nouveaux derives du fluorene, compositions les contenant et utilisation
US20070155730A1 (en) 2005-08-26 2007-07-05 Methylgene, Inc. Benzodiazepine And Benzopiperazine Analog Inhibitors Of Histone Deacetylase
DE602006017566D1 (de) 2005-08-30 2010-11-25 Boehringer Ingelheim Pharma Glucopyranosyl-substituierte benzyl-derivate, medikamente mit solchen verbindungen, ihre verwendung und herstellungsverfahren dafür
AU2006304897B2 (en) 2005-10-18 2012-07-12 Janssen Pharmaceutica N.V. Method of inhibiting FLT3 kinase
US7705022B2 (en) 2005-10-27 2010-04-27 Lankenau Institute For Medical Research IDO inhibitors and methods of use thereof
CN101395148A (zh) 2006-03-03 2009-03-25 诺瓦提斯公司 N-甲酰基羟胺化合物
WO2007101347A1 (en) 2006-03-07 2007-09-13 Aegera Therapeutics Inc. Bir domain binding compounds
CN102755318B (zh) 2006-03-29 2014-09-10 加利福尼亚大学董事会 二芳基硫代乙内酰脲化合物
CA2648518C (en) 2006-04-11 2012-06-26 Ramot At Tel Aviv University Ltd. Treatment of hematological malignancies with fts and a bcr-abl tyrosine kinase inhibitor
CA2651072A1 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
PL2019671T3 (pl) 2006-05-05 2015-02-27 Univ Michigan Regents Związki pośrednie do wytwarzania dwuwartościowych mimetyków Smac
JP2009544620A (ja) 2006-07-20 2009-12-17 リガンド・ファーマシューティカルズ・インコーポレイテッド 自己免疫疾患及び炎症のためのプロリン尿素ｃｃｒ１アンタゴニスト
WO2008014236A1 (en) 2006-07-24 2008-01-31 Tetralogic Pharmaceuticals Corporation Dimeric iap inhibitors
EP2089391B1 (en) 2006-11-03 2013-01-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
US8518891B2 (en) 2006-11-29 2013-08-27 Longqin Hu Chemotherapeutic conjugates and methods of use
EP2129668A1 (en) 2007-03-07 2009-12-09 Janssen Pharmaceutica N.V. Substituted phenoxy thiazolidinediones as estrogen related receptor-alpha modulators
EA200970838A1 (ru) 2007-03-07 2010-02-26 Янссен Фармацевтика Н.В. ЗАМЕЩЕННЫЕ ФЕНОКСИПРОИЗВОДНЫЕ N-АЛКИЛИРОВАННЫЕ ТИАЗОЛИДИНДИОНЫ В КАЧЕСТВЕ МОДУЛЯТОРОВ ЭСТРОГЕН-РОДСТВЕННЫХ РЕЦЕПТОРОВ α
EP2137168B1 (en) 2007-03-16 2016-09-14 Lankenau Institute for Medical Research Novel ido inhibitors and methods of use thereof
US20080233850A1 (en) 2007-03-20 2008-09-25 3M Innovative Properties Company Abrasive article and method of making and using the same
AU2008240153B2 (en) 2007-04-12 2013-01-31 Joyant Pharmaceuticals, Inc. SMAC mimetic dimers and trimers useful as anti-cancer agents
NZ580468A (en) 2007-04-13 2012-02-24 Univ Michigan Diazo bicyclic smac mimetics and the uses thereof
JP5368428B2 (ja) 2007-04-30 2013-12-18 ジェネンテック， インコーポレイテッド Ｉａｐのインヒビター
US20100203012A1 (en) 2007-05-30 2010-08-12 Aegera Therapeutics, Inc. Iap bir domain binding compounds
KR20100038108A (ko) 2007-07-25 2010-04-12 브리스톨-마이어스 스큅 컴퍼니 트리아진 키나제 억제제
CA2694953C (en) 2007-07-31 2015-12-01 Androscience Corporation Compositions including androgen receptor degradation (ard) enhancers and methods of prophylactic or therapeutic treatment of skin disorders and hair loss
EP2058312A1 (en) 2007-11-09 2009-05-13 Universita' degli Studi di Milano SMAC mimetic compounds as apoptosis inducers
US20100056524A1 (en) 2008-04-02 2010-03-04 Mciver Edward Giles Compound
US20120135089A1 (en) 2009-03-17 2012-05-31 Stockwell Brent R E3 ligase inhibitors
US8691187B2 (en) 2009-03-23 2014-04-08 Eli Lilly And Company Imaging agents for detecting neurological disorders
US8614201B2 (en) 2009-06-05 2013-12-24 Janssen Pharmaceutica Nv Heterocyclic amides as modulators of TRPA1
WO2011005510A2 (en) 2009-06-22 2011-01-13 Cerapedics, Inc. Peptide conjugates and uses thereof
JP2012532929A (ja) 2009-07-13 2012-12-20 プレジデント アンド フェロウズ オブ ハーバード カレッジ 二機能性のステープリングされたポリペプチドおよびそれらの使用
JP2012254939A (ja) 2009-10-07 2012-12-27 Astellas Pharma Inc オキサゾール化合物
EP2784076A1 (en) 2009-10-28 2014-10-01 Joyant Pharmaceuticals, Inc. Dimeric SMAC mimetics
US20110164191A1 (en) 2010-01-04 2011-07-07 Microvision, Inc. Interactive Projection Method, Apparatus and System
US8198300B2 (en) 2010-04-29 2012-06-12 Universidad De Chile Method for preventing tau protein aggregation and treating Alzheimer's disease with a quinoline derivative compound
MX354217B (es) 2010-05-14 2018-02-19 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
AU2011252808B2 (en) 2010-05-14 2015-05-14 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating neoplasia, inflammatory disease and other disorders
WO2011160016A2 (en) 2010-06-17 2011-12-22 The Trustees Of Columbia University In The City Of New York E3 binding pockets and identification and use of e3 ligase inhibitors
EP2588129A4 (en) 2010-06-30 2014-07-09 Univ Brandeis ON SMALL MOLECULES TARGETED PROTEIN REMOVAL
JP5823514B2 (ja) 2010-07-07 2015-11-25 アーデリクス，インコーポレーテッド リン酸輸送を阻害する化合物及び方法
JP5985473B2 (ja) 2010-07-13 2016-09-06 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ＩＲＡＫ４モジュレーターとしてのピラゾロ［１，５ａ］ピリミジン及びチエノ［３，２ｂ］ピリミジン誘導体
US9050334B2 (en) 2010-07-16 2015-06-09 Innov88 Llc MIF inhibitors and their uses
AU2011305315A1 (en) 2010-09-24 2013-03-28 The Regents Of The University Of Michigan Deubiquitinase inhibitors and methods for use of the same
US8975249B2 (en) 2010-11-01 2015-03-10 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
CN102477033A (zh) * 2010-11-23 2012-05-30 苏州波锐生物医药科技有限公司 苯并噻酚类化合物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012078559A2 (en) 2010-12-07 2012-06-14 Yale University Small-molecule hydrophobic tagging of fusion proteins and induced degradation of same
JP5923110B2 (ja) 2010-12-21 2016-05-24 ザ メディスンズ カンパニー （ライプチヒ） ゲーエムベーハー トリプシン様セリンプロテアーゼ阻害剤、その調製、ならびに凝固因子ＩＩａおよびＸａの選択的阻害剤としての使用
US20140243282A1 (en) 2010-12-31 2014-08-28 Satish Reddy Kallam Methods and compositions for designing novel conjugate therapeutics
WO2012129258A1 (en) 2011-03-22 2012-09-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
US9133164B2 (en) 2011-04-13 2015-09-15 Innov88 Llc MIF inhibitors and their uses
NO2694640T3 (pt) 2011-04-15 2018-03-17
KR20140032430A (ko) 2011-05-17 2014-03-14 플렉시콘, 인코퍼레이티드 키나제 조절 및 그에 대한 적응증
US20140161720A1 (en) 2011-05-26 2014-06-12 The General Hospital Corporation Treatment of angiogenic- or vascular-associated diseases
US9328117B2 (en) 2011-06-17 2016-05-03 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2013042137A1 (en) 2011-09-19 2013-03-28 Aurigene Discovery Technologies Limited Bicyclic heterocycles as irak4 inhibitors
JP6093770B2 (ja) 2011-09-27 2017-03-08 アムジエン・インコーポレーテツド 癌の治療のためのｍｄｍ２阻害剤としての複素環化合物
WO2013066729A1 (en) 2011-10-31 2013-05-10 Merck Sharp & Dohme Corp. Aminopyrimidinones as interleukin receptor-associated kinase inhibitors
JP2015504425A (ja) 2011-11-09 2015-02-12 アンサンブル・セラピューティクス アポトーシスのインヒビターを阻害するための大環状化合物
WO2013071039A1 (en) 2011-11-09 2013-05-16 Ensemble Therapeutics Macrocyclic compounds for inhibition of inhibitors of apoptosis
CN103172648B (zh) 2011-12-20 2016-05-25 上海迪诺医药科技有限公司 三杂环衍生物、制备方法及应用
CN104582705A (zh) 2012-01-10 2015-04-29 林伯士艾瑞斯公司 白介素-1受体相关激酶(irak)抑制剂和其用途
KR102668696B1 (ko) 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
EP2802579B1 (en) 2012-01-13 2016-04-13 Bristol-Myers Squibb Company Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors
US8987311B2 (en) 2012-01-13 2015-03-24 Bristol-Myers Squibb Company Triazolyl-substituted pyridyl compounds useful as kinase inhibitors
JP6109195B2 (ja) 2012-01-13 2017-04-05 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ キナーゼ阻害剤として有用な複素環置換されたピリジル化合物
WO2013157540A1 (ja) 2012-04-17 2013-10-24 富士フイルム株式会社 含窒素複素環化合物またはその塩
EP2846784A4 (en) 2012-05-11 2016-03-09 Univ Yale COMPOUNDS USEFUL FOR STIMULATING PROTEIN DEGRADATION AND METHODS USING THE SAME
CN104321325B (zh) 2012-05-24 2016-11-16 诺华股份有限公司 吡咯并吡咯烷酮化合物
RU2014150492A (ru) 2012-05-30 2016-07-20 Ф. Хоффманн-Ля Рош Аг Замещенные пирролидин-2-карбоксамиды
WO2014011712A1 (en) 2012-07-10 2014-01-16 Bristol-Myers Squibb Company Iap antagonists
WO2014020502A2 (en) 2012-07-31 2014-02-06 Novartis Ag Markers associated with human double minute 2 inhibitors
WO2014025759A1 (en) 2012-08-09 2014-02-13 Bristol-Myers Squibb Company Iap antagonists
TWI586668B (zh) 2012-09-06 2017-06-11 第一三共股份有限公司 二螺吡咯啶衍生物之結晶
EP2897949B1 (en) 2012-09-18 2018-01-10 Bristol-Myers Squibb Company Iap antagonists
KR101738063B1 (ko) 2012-09-21 2017-05-19 아로그 파마슈티칼스, 인코퍼레이티드 구조적으로 활성인 인산화된 ｆｌｔ３ 키나제의 억제 방법
US9603889B2 (en) 2012-10-02 2017-03-28 Bristol-Myers Squibb Company IAP antagonists
WO2014058691A1 (en) 2012-10-08 2014-04-17 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
EP2911669B1 (en) 2012-10-26 2024-04-10 The University of Chicago Synergistic combination of immunologic inhibitors for the treatment of cancer
AR093404A1 (es) 2012-11-09 2015-06-03 Bristol Myers Squibb Co Compuestos macrociclicos que modulan la actividad de los inhibidores de la apoptosis
AU2013361694B2 (en) 2012-12-20 2017-10-26 Merck Sharp & Dohme Corp. Substituted imidazopyridines as HDM2 inhibitors
EP2934535B1 (en) 2012-12-20 2017-07-19 Merck Sharp & Dohme Corp. Substituted pyrrolopyrimidines as hdm2 inhibitors
BR112015016282A2 (pt) 2013-01-07 2017-07-11 Arog Pharmaceuticals Inc crenolanibe para tratamento de distúrbios proliferativos de flt3 mutado
EP2752191A1 (en) 2013-01-07 2014-07-09 Sanofi Compositions and methods using hdm2 antagonist and mek inhibitor
GB201311910D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel Compounds
NL2011274C2 (en) 2013-08-06 2015-02-09 Illumicare Ip B V 51 Groundbreaking platform technology for specific binding to necrotic cells.
CA2902856C (en) 2013-02-28 2021-02-16 Amgen Inc. A benzoic acid derivative mdm2 inhibitor for the treatment of cancer
CA2906538C (en) 2013-03-14 2021-02-02 Ana Gonzalez Buenrostro Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
EP2970334B1 (en) 2013-03-15 2018-05-23 Biogen MA Inc. Macrocyclic compounds as irak4 inhibitors for the treatment of inflammatory diseases
SG11201506918WA (en) 2013-03-15 2015-09-29 Bristol Myers Squibb Co Inhibitors of indoleamine 2,3-dioxygenase (ido)
JP2016528197A (ja) 2013-07-01 2016-09-15 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｉｄｏ阻害剤
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
EP3019488B1 (en) 2013-07-11 2018-11-07 Bristol-Myers Squibb Company Ido inhibitors
EP3019517A1 (en) 2013-07-12 2016-05-18 Bristol-Myers Squibb Company Iap antagonists
CN103570726B (zh) 2013-07-15 2016-04-06 上海天慈生物谷生物工程有限公司 N-烷基色胺酮衍生物及其制备方法和应用
JP2016525135A (ja) 2013-07-23 2016-08-22 バイエル ファーマ アクチエンゲゼルシャフト ＢＥＴタンパク質およびポロ様キナーゼの二重阻害薬としての置換されたジヒドロピリド［３，４−ｂ］ピラジノン類
CN105593224B (zh) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 作为溴结构域抑制剂的新型喹唑啉酮类化合物
US20150051208A1 (en) 2013-08-14 2015-02-19 Boehringer Ingelheim International Gmbh Pyridinones
EA029981B1 (ru) 2013-08-27 2018-06-29 Бристол-Майерс Сквибб Компани Ингибиторы ido
US10463658B2 (en) 2013-10-25 2019-11-05 Videra Pharmaceuticals, Llc Method of inhibiting FLT3 kinase
US9428513B2 (en) 2013-11-07 2016-08-30 Boehringer Ingelheim International Gmbh Triazolopyrazine
TWI696618B (zh) 2013-11-08 2020-06-21 美商英塞特控股公司 用於合成吲哚胺2,3-雙加氧酶抑制劑之方法
CN105899505B (zh) 2013-11-08 2018-08-28 武田药品工业株式会社 用于治疗自身免疫病症的吡唑
CN103570727B (zh) 2013-11-12 2015-08-19 复旦大学 一种n-苄基色胺酮衍生物及其制备方法和应用
PL3071203T3 (pl) 2013-11-18 2021-08-23 Forma Therapeutics, Inc. Kompozycje tetrahydrochinolinowe jako inhibitory bromodomeny bet
UA115388C2 (uk) 2013-11-21 2017-10-25 Пфайзер Інк. 2,6-заміщені пуринові похідні та їх застосування в лікуванні проліферативних захворювань
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US9458156B2 (en) 2014-12-23 2016-10-04 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
AR098991A1 (es) 2014-01-03 2016-06-22 Bristol Myers Squibb Co Compuestos de nicotinamida sustituida con heteroarilo
SG11201605408RA (en) 2014-01-10 2016-07-28 Aurigene Discovery Tech Ltd Indazole compounds as irak4 inhibitors
SI3094329T1 (sl) 2014-01-13 2019-02-28 Aurigene Discovery Technologies Limited Biciklični heterociklilni derivati kot inhibitorji IRAK4
JP6351306B2 (ja) 2014-03-06 2018-07-04 キヤノン株式会社 画像処理装置、画像処理装置の制御方法およびプログラム
US20150259288A1 (en) 2014-03-14 2015-09-17 City Of Hope 5-bromo-indirubins
EP3126330B1 (en) 2014-04-04 2019-02-27 Pfizer Inc Bicyclic-fused heteroaryl or aryl compounds and their use as irak4 inhibitors
US20150291562A1 (en) 2014-04-14 2015-10-15 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20160058872A1 (en) 2014-04-14 2016-03-03 Arvinas, Inc. Imide-based modulators of proteolysis and associated methods of use
US20170166598A1 (en) 2014-05-13 2017-06-15 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
MD20160118A2 (ro) 2014-05-15 2017-04-30 Iteos Therapeutics Derivaţi ai pirolidin-2,5-dionei, compoziţii farmaceutice şi metode de utilizare ca inhibitori ai IDO1
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
US10246456B2 (en) 2014-07-18 2019-04-02 Biogen Ma Inc. IRAK4 inhibiting agents
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
AU2015311826B2 (en) 2014-09-05 2019-05-23 Merck Patent Gmbh Cyclohexyl-ethyl substituted diaza- and triaza-tricyclic compounds as indole-amine-2,3-dioxygenase (IDO) antagonists for the treatment of cancer
EP3200790B1 (en) 2014-09-30 2020-08-26 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
US9926330B2 (en) 2014-09-30 2018-03-27 Merck Sharp & Dohme Corp. Inhibitors of IRAK4 activity
WO2016053771A1 (en) 2014-09-30 2016-04-07 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
WO2016053772A1 (en) 2014-09-30 2016-04-07 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
UY36390A (es) 2014-11-05 2016-06-01 Flexus Biosciences Inc Compuestos moduladores de la enzima indolamina 2,3-dioxigenasa (ido), sus métodos de síntesis y composiciones farmacéuticas que los contienen
AR102537A1 (es) 2014-11-05 2017-03-08 Flexus Biosciences Inc Agentes inmunomoduladores
EP3247708A4 (en) 2015-01-20 2018-09-12 Arvinas, Inc. Compounds and methods for the targeted degradation of the androgen receptor
MA41598A (fr) 2015-02-25 2018-01-02 Constellation Pharmaceuticals Inc Composés thérapeutiques de pyridazine et leurs utilisations
EP3267996B1 (en) 2015-03-12 2020-11-11 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of irak4 activity
EP3268006B1 (en) 2015-03-12 2020-01-08 Merck Sharp & Dohme Corp. Pyrrolotriazine inhibitors of irak4 activity
WO2016144847A1 (en) 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Pyrrolopyridazine inhibitors of irak4 activity
US10155765B2 (en) 2015-03-12 2018-12-18 Merck Sharp & Dohme Corp. Carboxamide inhibitors of IRAK4 activity
WO2016144849A1 (en) 2015-03-12 2016-09-15 Merck Sharp & Dohme Corp. Thienopyrazine inhibitors of irak4 activity
GB201504314D0 (en) 2015-03-13 2015-04-29 Univ Dundee Small molecules
JP7269731B2 (ja) 2015-03-18 2023-05-09 アルビナス・オペレーションズ・インコーポレイテッド 標的タンパク質の分解向上のための化合物および方法
NZ736709A (en) 2015-05-15 2019-05-31 Gilead Sciences Inc Benzimidazole and imidazopyridine carboximidamide compounds having activity as inhibitors of indoleamine 2,3-dioxygenase
KR20180035828A (ko) 2015-07-10 2018-04-06 아비나스 인코포레이티드 단백질 분해의 mdm2계 조절인자 및 관련된 이용 방법
AU2016294450A1 (en) 2015-07-13 2017-12-07 Arvinas Operations, Inc. Alanine-based modulators of proteolysis and associated methods of use
WO2017030814A1 (en) 2015-08-19 2017-02-23 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins

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JP6401258B2 (ja) 2018-10-10
EP3016947B1 (en) 2018-09-05
BR112015032623B1 (pt) 2022-01-11
JP2016523875A (ja) 2016-08-12
RU2015154955A (ru) 2017-08-08
AU2014286342A1 (en) 2016-01-28
US9988376B2 (en) 2018-06-05
KR102130745B1 (ko) 2020-07-06
MX363127B (es) 2019-03-11
BR112015032623A8 (pt) 2020-01-14
EP3016947A1 (en) 2016-05-11
CA2915782C (en) 2021-03-23
GB201311888D0 (en) 2013-08-14
CN105452244A (zh) 2016-03-30
US20160368911A1 (en) 2016-12-22
WO2015000867A1 (en) 2015-01-08
CA2915782A1 (en) 2015-01-08
MX2015017861A (es) 2016-08-11
KR20160027980A (ko) 2016-03-10

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