JP6640126B2 - セレブロン及び他のｅ３ユビキチンリガーゼの立体構造の変化を誘導するための組成物及び方法 - Google Patents

セレブロン及び他のｅ３ユビキチンリガーゼの立体構造の変化を誘導するための組成物及び方法 Download PDF

Info

Publication number
JP6640126B2
JP6640126B2 JP2016575370A JP2016575370A JP6640126B2 JP 6640126 B2 JP6640126 B2 JP 6640126B2 JP 2016575370 A JP2016575370 A JP 2016575370A JP 2016575370 A JP2016575370 A JP 2016575370A JP 6640126 B2 JP6640126 B2 JP 6640126B2
Authority
JP
Japan
Prior art keywords
crbn
alteration
dimensional structure
compound
test compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
JP2016575370A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017528690A (ja
JP2017528690A5 (enExample
Inventor
チャンバーライン フィリップ
チャンバーライン フィリップ
イー．キャザース ブライアン
イー．キャザース ブライアン
ロペズ‐ジラオナ アントニア
ロペズ‐ジラオナ アントニア
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.)
Celgene Corp
Original Assignee
Celgene Corp
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 Celgene Corp filed Critical Celgene Corp
Publication of JP2017528690A publication Critical patent/JP2017528690A/ja
Publication of JP2017528690A5 publication Critical patent/JP2017528690A5/ja
Application granted granted Critical
Publication of JP6640126B2 publication Critical patent/JP6640126B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • C12Q1/37—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase involving peptidase or proteinase
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00—ICT specially adapted for analysing two-dimensional or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment
    • G16B15/30—Drug targeting using structural data; Docking or binding prediction
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B15/00—ICT specially adapted for analysing two-dimensional or three-dimensional molecular structures, e.g. structural or functional relations or structure alignment

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physics & Mathematics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Biophysics (AREA)
  • Spectroscopy & Molecular Physics (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Analytical Chemistry (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Computational Biology (AREA)
  • Evolutionary Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Medical Informatics (AREA)
  • Theoretical Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Analysing Materials By The Use Of Radiation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2016575370A 2014-06-27 2015-06-26 セレブロン及び他のｅ３ユビキチンリガーゼの立体構造の変化を誘導するための組成物及び方法 Active JP6640126B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462018445P 2014-06-27 2014-06-27
US62/018,445 2014-06-27
PCT/US2015/037980 WO2015200795A1 (en) 2014-06-27 2015-06-26 Compositions and methods for inducing conformational changes in cereblon other e3 ubiquitin ligases

Publications (3)

Publication Number Publication Date
JP2017528690A JP2017528690A (ja) 2017-09-28
JP2017528690A5 JP2017528690A5 (enExample) 2018-08-02
JP6640126B2 true JP6640126B2 (ja) 2020-02-05

Family

ID=54929344

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016575370A Active JP6640126B2 (ja) 2014-06-27 2015-06-26 セレブロン及び他のｅ３ユビキチンリガーゼの立体構造の変化を誘導するための組成物及び方法

Country Status (5)

Country Link
US (3) US10092555B2 (enExample)
EP (2) EP3827836A1 (enExample)
JP (1) JP6640126B2 (enExample)
ES (1) ES2843973T3 (enExample)
WO (1) WO2015200795A1 (enExample)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107445940A (zh) 2006-09-26 2017-12-08 细胞基因公司 作为抗肿瘤剂的5‑取代的喹唑酮衍生物
SG183257A1 (en) 2010-02-11 2012-09-27 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
EA026100B1 (ru) 2011-03-11 2017-03-31 Селджин Корпорейшн Твердые формы 3-(5-амино-2-метил-4-оксо-4н-хиназолин-3-ил)пиперидин-2,6-диона и их фармацевтические композиции и применение
JP2015531776A (ja) 2012-09-04 2015-11-05 セルジーン コーポレイション ３−（５−アミノ−２−メチル−４−オキソキナゾリン−３（４ｈ）−イル）ピペリジン−２，６−ジオンのアイソトポログ及びその製造方法
US9695145B2 (en) 2013-01-22 2017-07-04 Celgene Corporation Processes for the preparation of isotopologues of 3-(4-((4- morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione and pharmaceutically acceptable salts thereof
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Ｋｒａｓ ｇ１２ｃ之抑制劑
EP3827836A1 (en) 2014-06-27 2021-06-02 Celgene Corporation Compositions and methods for inducing conformational changes in cereblon and other e3 ubiquitin ligases
WO2016164675A1 (en) 2015-04-10 2016-10-13 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
ES2856880T3 (es) 2015-04-15 2021-09-28 Araxes Pharma Llc Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10730867B2 (en) 2015-09-28 2020-08-04 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
CN108779097A (zh) 2015-11-16 2018-11-09 亚瑞克西斯制药公司 包含取代的杂环基的2-取代的喹唑啉化合物及其使用方法
WO2017117118A1 (en) 2015-12-28 2017-07-06 Celgene Corporation Compositions and methods for inducing conformational changes in cereblon and other e3 ubiquitin ligases
US11963520B2 (en) 2016-01-19 2024-04-23 Celgene Corporation Transgenic mouse expressing human cereblon
JP2019522633A (ja) 2016-05-20 2019-08-15 ジェネンテック， インコーポレイテッド Ｐｒｏｔａｃ抗体コンジュゲート及び使用方法
US10646488B2 (en) * 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
US10280172B2 (en) 2016-09-29 2019-05-07 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
CN110312711A (zh) 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
EP3573970A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer
US11059819B2 (en) 2017-01-26 2021-07-13 Janssen Biotech, Inc. Fused hetero-hetero bicyclic compounds and methods of use thereof
US11279689B2 (en) 2017-01-26 2022-03-22 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EP3577459A4 (en) 2017-02-03 2020-12-16 Celgene Corporation METHOD OF MEASURING THE AFFINITY OF SMALL MOLECULES FOR CEREBLON
WO2018169777A1 (en) * 2017-03-14 2018-09-20 Biotheryx, Inc. Compounds targeting proteins, compositions, methods, and uses thereof
WO2018200981A1 (en) * 2017-04-28 2018-11-01 Quartz Therapeutics, Inc. Raf-degrading conjugate compounds
AU2018271990A1 (en) 2017-05-25 2019-12-12 Araxes Pharma Llc Covalent inhibitors of KRAS
WO2018218071A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Compounds and methods of use thereof for treatment of cancer
EP3630747A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Quinazoline derivatives as modulators of mutant kras, hras or nras
WO2019060693A1 (en) * 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
AU2018338314B2 (en) 2017-09-22 2024-12-12 Kymera Therapeutics, Inc Protein degraders and uses thereof
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
EP3737666A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES
EP3737675A4 (en) 2018-01-12 2022-01-05 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
JP7321194B2 (ja) * 2018-06-29 2023-08-04 ダナ－ファーバー キャンサー インスティテュート，インコーポレイテッド セレブロン（ｃｒｂｎ）に対するリガンド
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
EP3817748A4 (en) 2018-07-06 2022-08-24 Kymera Therapeutics, Inc. TRICYCLIC CRBN LIGANDS AND USES THEREOF
CN112584833A (zh) 2018-08-01 2021-03-30 亚瑞克西斯制药公司 杂环螺化合物及其用于治疗癌症的使用方法
SG11202105424PA (en) 2018-11-30 2021-06-29 Kymera Therapeutics Inc Irak degraders and uses thereof
EP3897631A4 (en) 2018-12-20 2022-11-23 C4 Therapeutics, Inc. TARGETED PROTEIN BREAKDOWN
KR20220006139A (ko) 2019-04-05 2022-01-14 카이메라 쎄라퓨틱스 인코포레이티드 Stat 분해제 및 이의 용도
US12521438B2 (en) 2019-06-10 2026-01-13 Kymera Therapeutics, Inc. SMARCA degraders and uses thereof
CA3148504A1 (en) 2019-08-08 2021-02-11 Institute For Cancer Research D/B/A/ The Research Institute Of Fox Chase Cancer Center Combination therapy for treatment of cancer
CN114761400B (zh) * 2019-09-12 2024-08-13 南京明德新药研发有限公司 一种可降解蛋白的并环类化合物及其应用
JP2023509366A (ja) 2019-12-17 2023-03-08 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ分解剤およびそれらの使用
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
PH12022551522A1 (en) 2019-12-23 2024-01-29 Kymera Therapeutics Inc Smarca degraders and uses thereof
PH12022552458A1 (en) 2020-03-19 2024-01-22 Kymera Therapeutics Inc Mdm2 degraders and uses thereof
CN115867322A (zh) * 2020-03-31 2023-03-28 奥隆制药 新降解剂缀合物
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
WO2022032026A1 (en) 2020-08-05 2022-02-10 C4 Therapeutics, Inc. Compounds for targeted degradation of ret
WO2022146151A1 (en) * 2020-12-30 2022-07-07 Captor Therapeutics S.A. Novel compounds which bind to cereblon, and methods of use thereof
MX2023007852A (es) 2020-12-30 2023-07-07 Kymera Therapeutics Inc Degradadores de cinasas asociadas al receptor de interleucina-1 (irak) y usos de los mismos.
MX2023008296A (es) 2021-01-13 2023-09-29 Monte Rosa Therapeutics Inc Compuestos de isoindolinona.
WO2022174268A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
WO2023076556A1 (en) 2021-10-29 2023-05-04 Kymera Therapeutics, Inc. Irak4 degraders and synthesis thereof
IL314437A (en) 2022-01-31 2024-09-01 Kymera Therapeutics Inc IRAK joints and their uses
US20250314661A1 (en) * 2022-05-15 2025-10-09 The Regents Of The University Of California Chemigenetic tools and methods of controlling and assessing protein phase separation
EP4584259A1 (en) 2022-09-09 2025-07-16 Innovo Therapeutics, Inc. Ck1alpha and dual ck1alpha / gspt1 degrading compounds
WO2025063888A1 (en) 2023-09-19 2025-03-27 Kancure Pte. Ltd. Survivin-targeted compounds
WO2025179161A1 (en) 2024-02-21 2025-08-28 Innovo Therapeutics, Inc. Protein degrading compounds

Family Cites Families (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
US4994443A (en) 1982-12-20 1991-02-19 The Children's Medical Center Corporation Inhibition of angiogenesis
US5001116A (en) 1982-12-20 1991-03-19 The Children's Medical Center Corporation Inhibition of angiogenesis
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
US4683195A (en) 1986-01-30 1987-07-28 Cetus Corporation Process for amplifying, detecting, and/or-cloning nucleic acid sequences
US5391485A (en) 1985-08-06 1995-02-21 Immunex Corporation DNAs encoding analog GM-CSF molecules displaying resistance to proteases which cleave at adjacent dibasic residues
JPS63500636A (ja) 1985-08-23 1988-03-10 麒麟麦酒株式会社 多分化能性顆粒球コロニー刺激因子をコードするｄｎａ
US4810643A (en) 1985-08-23 1989-03-07 Kirin- Amgen Inc. Production of pluripotent granulocyte colony-stimulating factor
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
DE69330750T2 (de) 1992-03-04 2002-07-04 The Regents Of The University Of California, Oakland Vergleichende genomhybridisierung
US5441050A (en) 1992-12-18 1995-08-15 Neoprobe Corporation Radiation responsive surgical instrument
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
US8143283B1 (en) 1993-03-01 2012-03-27 The Children's Medical Center Corporation Methods for treating blood-born tumors with thalidomide
US6114355A (en) 1993-03-01 2000-09-05 D'amato; Robert Methods and compositions for inhibition of angiogenesis
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5698579A (en) 1993-07-02 1997-12-16 Celgene Corporation Cyclic amides
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
US5573758A (en) 1995-04-28 1996-11-12 Allergan Method for reducing intraocular pressure in the mammalian eye by administration of potassium channel blockers
US6207639B1 (en) 1996-07-12 2001-03-27 Mcgill University Compounds and methods for modulating neurite outgrowth
US6333307B1 (en) 1996-07-12 2001-12-25 Mcgill University Compounds and method for modulating neurite outgrowth
HU228769B1 (en) 1996-07-24 2013-05-28 Celgene Corp Substituted 2(2,6-dioxopiperidin-3-yl)phthalimides and -1-oxoisoindolines and their use for production of pharmaceutical compositions for mammals to reduce the level of tnf-alpha
NZ333903A (en) 1996-07-24 2000-02-28 Celgene Corp Substituted 2(2,6-dioxopiperidin-3-yl)phthalimides and -1oxoisoindolines and method of reducing TNF-alpha levels in a mammal
US6281230B1 (en) 1996-07-24 2001-08-28 Celgene Corporation Isoindolines, method of use, and pharmaceutical compositions
US5635517B1 (en) 1996-07-24 1999-06-29 Celgene Corp Method of reducing TNFalpha levels with amino substituted 2-(2,6-dioxopiperidin-3-YL)-1-oxo-and 1,3-dioxoisoindolines
US5798368A (en) 1996-08-22 1998-08-25 Celgene Corporation Tetrasubstituted 2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolines and method of reducing TNFα levels
JP4214537B2 (ja) 1996-08-12 2009-01-28 セルジーン コーポレーション 新規な免疫治療薬とこの薬物を使用してサイトカインレベルを抵減する方法
US5874448A (en) 1997-11-18 1999-02-23 Celgene Corporation Substituted 2-(2,6 dioxo-3-fluoropiperidin-3-yl)-isoindolines and method of reducing TNFα levels
US5955476A (en) 1997-11-18 1999-09-21 Celgene Corporation Substituted 2-(2,6-dioxo-3-fluoropiperidin-3-yl)-isoindolines and method of reducing inflammatory cytokine levels
US6221585B1 (en) 1998-01-15 2001-04-24 Valigen, Inc. Method for identifying genes underlying defined phenotypes
AU745884B2 (en) 1998-03-16 2002-04-11 Celgene Corporation 2-(2,6-dioxopiperidin-3-yl)isoindoline derivatives, their preparation and their use as inhibitors of inflammatory cytokines
US6433149B1 (en) 1998-05-05 2002-08-13 Adherex Technologies, Inc. Compounds and methods for inhibiting cancer metastasis
US6472367B1 (en) 1998-05-05 2002-10-29 Adherex Technologies, Inc. Compounds and methods for modulating OB-cadherin mediated cell adhesion
US6680175B2 (en) 1998-05-05 2004-01-20 Adherex Technologies, Inc. Methods for diagnosing and evaluating cancer
US6277824B1 (en) 1998-07-10 2001-08-21 Adherex Technologies Compounds and methods for modulating adhesion molecule function
US6322962B1 (en) 1998-08-14 2001-11-27 Board Of Regents, The University Of Texas System Sterol-regulated Site-1 protease and assays of modulators thereof
US6927024B2 (en) 1998-11-30 2005-08-09 Genentech, Inc. PCR assay
NZ513953A (en) 1999-03-18 2001-09-28 Celgene Corp Substituted 1-oxo- and 1,3-dioxoisoindolines and their use in pharmaceutical compositions for reducing inflammatory cytokine levels
US7186507B2 (en) 1999-12-09 2007-03-06 Indiana University Research And Technology Corporation Fluorescent in situ RT-PCR
US6458810B1 (en) 2000-11-14 2002-10-01 George Muller Pharmaceutically active isoindoline derivatives
US20030045552A1 (en) 2000-12-27 2003-03-06 Robarge Michael J. Isoindole-imide compounds, compositions, and uses thereof
US7091353B2 (en) 2000-12-27 2006-08-15 Celgene Corporation Isoindole-imide compounds, compositions, and uses thereof
CN100523216C (zh) 2001-03-02 2009-08-05 匹兹堡大学 Pcr方法
US7981863B2 (en) 2001-09-19 2011-07-19 Neuronova Ab Treatment of Parkinson's disease with PDGF
US20030194708A1 (en) 2002-04-10 2003-10-16 Minke Binnerts Human homolog of crossveinless materials and methods
US7393862B2 (en) 2002-05-17 2008-07-01 Celgene Corporation Method using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for treatment of certain leukemias
US7968569B2 (en) 2002-05-17 2011-06-28 Celgene Corporation Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
US20060134767A1 (en) 2002-07-08 2006-06-22 Buser-Doepner Carolyn A Mitotic kinesin binding site
US20110070376A1 (en) 2002-09-09 2011-03-24 Reactive Surfaces, Ltd. Anti-fouling Paints & Coatings
US7189740B2 (en) 2002-10-15 2007-03-13 Celgene Corporation Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes
US7122799B2 (en) 2003-12-18 2006-10-17 Palo Alto Research Center Incorporated LED or laser enabled real-time PCR system and spectrophotometer
US7244759B2 (en) 2004-07-28 2007-07-17 Celgene Corporation Isoindoline compounds and methods of making and using the same
US20080051379A1 (en) 2004-12-01 2008-02-28 Trustees Of Boston University Compositions and Methods for the Treatment of Peripheral B-Cell Neoplasms
EP1924250B1 (en) 2004-12-01 2017-01-04 Celgene Corporation Methods and compositions comprising immunomodulatory compounds for use for the treatment of immunodeficiency disorders
CN101141960A (zh) 2005-01-25 2008-03-12 细胞基因公司 使用4-氨基-2-(3-甲基-2,6-二氧代哌啶-3-基)-异吲哚-1,3-二酮的方法和组合物
WO2007086915A2 (en) 2005-05-12 2007-08-02 Applied Genomics, Inc. Reagents and methods for use in cancer diagnosis, classification and therapy
US7776551B2 (en) 2005-07-12 2010-08-17 Ramot At Tel Aviv University Ltd. Methods and kits for diagnosing and treating mental retardation
CN101291924A (zh) 2005-08-31 2008-10-22 细胞基因公司 异吲哚-酰亚胺化合物和包含它们的组合物及其使用方法
US8445198B2 (en) 2005-12-01 2013-05-21 Medical Prognosis Institute Methods, kits and devices for identifying biomarkers of treatment response and use thereof to predict treatment efficacy
US20070128636A1 (en) 2005-12-05 2007-06-07 Baker Joffre B Predictors Of Patient Response To Treatment With EGFR Inhibitors
WO2007084992A2 (en) 2006-01-19 2007-07-26 The University Of Chicago Prognosis and therapy predictive markers and methods of use
WO2007108968A2 (en) 2006-03-13 2007-09-27 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
WO2008005281A2 (en) 2006-06-30 2008-01-10 Rosetta Inpharmatics Llc Genes associated with chemotherapy response and uses thereof
US8877780B2 (en) 2006-08-30 2014-11-04 Celgene Corporation 5-substituted isoindoline compounds
CN107445940A (zh) 2006-09-26 2017-12-08 细胞基因公司 作为抗肿瘤剂的5‑取代的喹唑酮衍生物
US20080280779A1 (en) 2006-09-26 2008-11-13 Shaughnessy Jr John D Gene expression profiling based identification of genomic signatures of multiple myeloma and uses thereof
US20090075281A1 (en) 2007-07-10 2009-03-19 Regents Of The University Of California Mtbe genes
CA2707886A1 (en) 2007-12-07 2009-06-18 Celgene Corporation Biomarkers for predicting the sensitivity of cells to immunomodulatory compounds during treatment of non-hodgkin's lymphoma
US20100021437A1 (en) 2008-04-07 2010-01-28 The McLean Hospital Corporation Whitehead Institute for Biomedical Research Neural stem cells derived from induced pluripotent stem cells
WO2009144699A1 (en) 2008-05-26 2009-12-03 Yeda Research And Development Co. Ltd. Methods of treating cancer of the central nervous system
WO2010017515A2 (en) 2008-08-08 2010-02-11 Integrated Diagnostics Inc. Breast cancer specific markers and methods of use
WO2010120759A1 (en) 2009-04-14 2010-10-21 Schering Corporation Interferon-alfa sensitivity biomarkers
EP2436387B1 (en) 2009-05-25 2018-07-25 Celgene Corporation Pharmaceutical composition comprising crbn for use in treating a disease of the cerebral cortex
CN102497870A (zh) 2009-06-03 2012-06-13 戴瑟纳制药公司 肽-dicer底物试剂及其特异性抑制基因表达的方法
KR101692297B1 (ko) * 2009-10-20 2017-01-04 도오쿄 인스티튜드 오브 테크놀로지 탈리도마이드 표적 인자를 이용한 스크리닝 방법
SG183257A1 (en) 2010-02-11 2012-09-27 Celgene Corp Arylmethoxy isoindoline derivatives and compositions comprising and methods of using the same
MX2012010367A (es) 2010-03-12 2012-11-23 Celgene Corp Metodos para el tratamiento de linfomas no hodgkin que usan lenalidomida y biomarcadores de genes y proteinas como un predictor.
MX344636B (es) 2010-09-15 2017-01-04 Almac Diagnostics Ltd Prueba de diagnóstico molecular para cáncer.
EP2683412B1 (en) * 2011-03-11 2017-05-03 Mayo Foundation For Medical Education And Research Methods for assessing responsiveness of cancer cells to lenalidomide, thalidomide, and/or pomalidomide
AU2012229316B2 (en) 2011-03-11 2017-05-11 Celgene Corporation Use of 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2-6-dione in treatment of immune-related and inflammatory diseases
EA026100B1 (ru) 2011-03-11 2017-03-31 Селджин Корпорейшн Твердые формы 3-(5-амино-2-метил-4-оксо-4н-хиназолин-3-ил)пиперидин-2,6-диона и их фармацевтические композиции и применение
CN103688176A (zh) 2011-04-29 2014-03-26 细胞基因公司 利用cereblon作为预报因子治疗癌和炎性疾病的方法
EP2944961A1 (en) 2011-05-06 2015-11-18 XenTech Markers for cancer prognosis and therapy and methods of use
WO2014004990A2 (en) * 2012-06-29 2014-01-03 Celgene Corporation Methods for determining drug efficacy using cereblon-associated proteins
PL2882442T3 (pl) 2012-08-09 2021-12-13 Celgene Corporation Sposoby leczenia nowotworów z wykorzystaniem 3-(4-((4-(morfolinometylo)benzylo)oksy)-1-oksoizoindolin-2-ylo)piperydyno-2,6-dionu
WO2014028445A2 (en) 2012-08-14 2014-02-20 Celgene Corporation Cereblon isoforms and their use as biomarkers for therapeutic treatment
US9694015B2 (en) 2012-09-10 2017-07-04 Celgene Corporation Methods for the treatment of locally advanced breast cancer
US20150051283A1 (en) 2013-06-14 2015-02-19 Complexa, Inc. Composition and method for inhibition of pkng from mycobacterium tuberculosis
WO2015077058A2 (en) 2013-11-08 2015-05-28 The Broad Institute, Inc. Compositions and methods for selecting a treatment for b-cell neoplasias
US20160313300A1 (en) 2013-12-06 2016-10-27 Celgene Corporation Methods for determining drug efficacy for the treatment of diffuse large b-cell lymphoma, multiple myeloma, and myeloid cancers
EP3827836A1 (en) 2014-06-27 2021-06-02 Celgene Corporation Compositions and methods for inducing conformational changes in cereblon and other e3 ubiquitin ligases
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
US9713375B1 (en) 2015-02-26 2017-07-25 Brett Einar Rahm Collapsible portable table
WO2017117118A1 (en) 2015-12-28 2017-07-06 Celgene Corporation Compositions and methods for inducing conformational changes in cereblon and other e3 ubiquitin ligases

Also Published As

Publication number Publication date
ES2843973T3 (es) 2021-07-21
WO2015200795A1 (en) 2015-12-30
US20210000813A1 (en) 2021-01-07
EP3160486A4 (en) 2017-12-13
EP3160486B1 (en) 2020-11-18
US10092555B2 (en) 2018-10-09
JP2017528690A (ja) 2017-09-28
US10668057B2 (en) 2020-06-02
US11419861B2 (en) 2022-08-23
EP3160486A1 (en) 2017-05-03
US20190030019A1 (en) 2019-01-31
US20150374678A1 (en) 2015-12-31
EP3827836A1 (en) 2021-06-02

Similar Documents

Publication Publication Date Title
JP6640126B2 (ja) セレブロン及び他のｅ３ユビキチンリガーゼの立体構造の変化を誘導するための組成物及び方法
WO2017117118A1 (en) Compositions and methods for inducing conformational changes in cereblon and other e3 ubiquitin ligases
JP2017528690A5 (enExample)
JP7336178B2 (ja) 治療における使用のための新規のＴＮＦα構造
AU2023278067A1 (en) ASGR inhibitors
CN101932607B (zh) 针对前蛋白转化酶枯草杆菌蛋白酶kexin9型(pcsk9)的抗原结合蛋白
CA2460151A1 (en) Cytokine receptor
WO2003035846A2 (en) Structure of tall-1 and its cognate receptor
AU2014361662A1 (en) Systems and methods of selecting compounds with reduced risk of cardiotoxicity
WO2009100173A2 (en) Demethylation and inactivation of protein phosphatase 2a
AU2022241573B2 (en) Antigen Binding Proteins to Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9)
WO2012097826A2 (en) Crystal structure of a type ib p-type atpase
KR101421089B1 (ko) 대장암에 특이적인 항암 활성을 갖는 신규 펩타이드, 이를 포함하는 ｎｄｒｇ２ 결정체 및 이의 용도
CN101228270A (zh) 人可溶性腺苷酸环化酶的晶体结构
WO2016201566A1 (en) Systems and methods of selecting compounds with reduced risk of cardiotoxicity using herg models
JP2005137361A (ja) ペプチジルアルギニンデイミナーゼ４又はその変異体タンパク質の結晶、ペプチジルアルギニンデイミナーゼ４変異体タンパク質及びその複合体
JP2002533060A (ja) 結晶化型のＦｃイプシロンレセプタアルファ鎖、その３−Ｄモデル、及びそれらの利用法
JP2003135087A (ja) テロメアｄｎａとヒトｔｒｆ１複合体の立体構造の利用
WO2003096985A2 (en) 3d structure of the tsg101 uev domain
HK1120557A (en) Crystal structure of human soluble adenylate cyclase
JP2006042732A (ja) 酵母ｄｓｋ２のユビキチン結合ドメインとモノユビキチンとの複合体の構造的特徴および酵母ｄｓｋ２のユビキチン結合ドメインによるモノユビキチン認識機構
JP2006158228A (ja) ヒトＶｐｓ４ｂのＭＩＴドメインと二価または三価の金属イオンの複合体の構造的特徴およびヒトＶｐｓ４ｂのＭＩＴドメインによるホスファチジルイノシトールリン酸認識機構
AU5660900A (en) Crystalline zap family proteins

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20171214

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20180620

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20180620

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20190319

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20190320

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190610

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: 20191203

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20191225

R150 Certificate of patent or registration of utility model

Ref document number: 6640126

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R154 Certificate of patent or utility model (reissue)

Free format text: JAPANESE INTERMEDIATE CODE: R154

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250