[go: up one dir, main page]
More Web Proxy on the site http://driver.im/

EA201992780A1 - Соединения, которые взаимодействуют с суперсемейством ras, для лечения рака, воспалительных заболеваний, ras-опатий и фиброзного заболевания - Google Patents

Соединения, которые взаимодействуют с суперсемейством ras, для лечения рака, воспалительных заболеваний, ras-опатий и фиброзного заболевания

Info

Publication number
EA201992780A1
EA201992780A1 EA201992780A EA201992780A EA201992780A1 EA 201992780 A1 EA201992780 A1 EA 201992780A1 EA 201992780 A EA201992780 A EA 201992780A EA 201992780 A EA201992780 A EA 201992780A EA 201992780 A1 EA201992780 A1 EA 201992780A1
Authority
EA
Eurasian Patent Office
Prior art keywords
ras
inflammatory diseases
compounds
cancer
opatias
Prior art date
Application number
EA201992780A
Other languages
English (en)
Inventor
Ярон Р. Хадари
Лука Карта
Майкл Шмертцлер
Тереза М. Уилльямс
Чарльз Х. Рейнолдс
Ребекка Хатчесон
Original Assignee
ШАЙ ТЕРАПЬЮТИКС ЭлЭлСи
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 ШАЙ ТЕРАПЬЮТИКС ЭлЭлСи filed Critical ШАЙ ТЕРАПЬЮТИКС ЭлЭлСи
Publication of EA201992780A1 publication Critical patent/EA201992780A1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—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
    • A61K31/4365—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 having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/10—Processes for the isolation, preparation or purification of DNA or RNA
    • C12N15/1034—Isolating an individual clone by screening libraries
    • C12N15/1037—Screening libraries presented on the surface of microorganisms, e.g. phage display, E. coli display
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/10—Processes for the isolation, preparation or purification of DNA or RNA
    • C12N15/1034—Isolating an individual clone by screening libraries
    • C12N15/1065—Preparation or screening of tagged libraries, e.g. tagged microorganisms by STM-mutagenesis, tagged polynucleotides, gene tags
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biotechnology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Zoology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Wood Science & Technology (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Plant Pathology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Virology (AREA)
  • Bioinformatics & Computational Biology (AREA)

Abstract

В настоящем документе предложены способы и композиции для лечения рака, воспалительных заболеваний, RAS-опатий и фиброзных заболеваний, включающих в себя аберрантную передачу сигналов суперсемейства Ras через связывающие соединения с ГТФ-связывающим доменом белков суперсемейства Ras, включая, в некоторых случаях, K-Ras и их мутанты, и новый способ анализа таких композиций.
EA201992780A 2017-06-21 2018-06-20 Соединения, которые взаимодействуют с суперсемейством ras, для лечения рака, воспалительных заболеваний, ras-опатий и фиброзного заболевания EA201992780A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762523114P 2017-06-21 2017-06-21
PCT/US2018/038613 WO2018237084A1 (en) 2017-06-21 2018-06-20 COMPOUNDS INTERACTING WITH RAS SUPERFAMIL FOR USE IN THE TREATMENT OF CANCERS, INFLAMMATORY DISEASES, RASOPATHIES AND FIBROTIC DISEASES

Publications (1)

Publication Number Publication Date
EA201992780A1 true EA201992780A1 (ru) 2020-06-02

Family

ID=62904595

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201992780A EA201992780A1 (ru) 2017-06-21 2018-06-20 Соединения, которые взаимодействуют с суперсемейством ras, для лечения рака, воспалительных заболеваний, ras-опатий и фиброзного заболевания

Country Status (14)

Country Link
US (9) US10588894B2 (ru)
EP (2) EP4331679A3 (ru)
JP (3) JP7514005B2 (ru)
KR (1) KR20200041294A (ru)
CN (1) CN111032662B (ru)
AU (2) AU2018288841B2 (ru)
BR (1) BR112019027640A2 (ru)
CA (1) CA3066939A1 (ru)
EA (1) EA201992780A1 (ru)
IL (2) IL310023A (ru)
MA (1) MA49458A (ru)
MX (3) MX2019014875A (ru)
SG (1) SG11201911929XA (ru)
WO (1) WO2018237084A1 (ru)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201607705XA (en) 2014-03-19 2016-10-28 Infinity Pharmaceuticals Inc Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
JP6980649B2 (ja) 2015-09-14 2021-12-15 インフィニティー ファーマシューティカルズ， インコーポレイテッド イソキノリノン誘導体の固体形態、それを製造する方法、それを含む組成物、及びそれを使用する方法
JP7114076B2 (ja) 2015-12-22 2022-08-08 シャイ・セラピューティクス・エルエルシー がん及び炎症性疾患の処置のための化合物
WO2018237084A1 (en) 2017-06-21 2018-12-27 SHY Therapeutics LLC COMPOUNDS INTERACTING WITH RAS SUPERFAMIL FOR USE IN THE TREATMENT OF CANCERS, INFLAMMATORY DISEASES, RASOPATHIES AND FIBROTIC DISEASES
US11439608B2 (en) 2017-09-25 2022-09-13 Qun Lu Roles of modulators of intersectin-CDC42 signaling in Alzheimer's disease
EP3827001A1 (en) * 2018-07-26 2021-06-02 Domain Therapeutics Substituted quinazolinone derivatives and their use as positive allosteric modulators of mglur4
AU2019355870B2 (en) * 2018-10-01 2023-11-16 Genzyme Corporation Thieno[3,2-b]pyridine derivatives as UDP glycosyltransferase inhibitors and methods of use
MX2021003904A (es) 2018-10-05 2021-10-26 Annapurna Bio Inc Compuestos y composiciones para el tratamiento de afecciones asociadas con la actividad del receptor apj.
EP3898609A1 (en) * 2018-12-19 2021-10-27 Shy Therapeutics LLC Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
WO2020159942A1 (en) * 2019-01-29 2020-08-06 Tosk, Inc. Pyrazolopyrimidine modulators of ras gtpase
EP3929185A4 (en) * 2019-02-19 2023-02-15 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. CONDENSED CYCLIC COMPOUND CONTAINING NITROGEN, METHOD FOR PREPARATION AND USE
CA3137193A1 (en) * 2019-04-24 2020-10-29 The Governors Of The University Of Alberta Non-peptidic heterocycle-containing compounds for the treatment of alzheimer's disease
SG11202112790SA (en) * 2019-05-20 2021-12-30 California Inst Of Techn Kras g12c inhibitors and uses thereof
CN113993860B (zh) * 2019-06-25 2023-08-01 正大天晴药业集团股份有限公司 作为kras g12c突变蛋白抑制剂的七元杂环类衍生物
JP2022547426A (ja) * 2019-09-04 2022-11-14 エイジェンシー・フォー・サイエンス，テクノロジー・アンド・リサーチ β－カテニン／ＴＣＦ４相互作用のモジュレーターとしての複素環化合物
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
US20230030517A1 (en) * 2019-12-13 2023-02-02 INSERM (Institut National de la Santé et de la Recherche Médicale) Epac1 inhibitors for the treatment of idiopathic pulmonary fibrosis
AU2021253571A1 (en) * 2020-04-08 2022-11-10 Remix Therapeutics Inc. Compounds and methods for modulating splicing
BR112022021806A2 (pt) * 2020-04-28 2022-12-13 Global Blood Therapeutics Inc Cicloalquilpirimidinas como inibidores de ferroportina
CN115996917A (zh) 2020-05-06 2023-04-21 艾捷斯治疗公司 作为jak2抑制剂的6-杂芳基氧基苯并咪唑和氮杂苯并咪唑
AU2021279023A1 (en) * 2020-05-27 2022-12-15 Constellation Pharmaceuticals, Inc. Substituted benzamides as modulators of TREX1
EP4168414A1 (en) 2020-06-18 2023-04-26 Shy Therapeutics LLC Substituted thienopyrimidines that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease
CA3183032A1 (en) 2020-06-18 2021-12-23 Mallika Singh Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
CN111996251B (zh) * 2020-06-19 2024-03-26 皖南医学院第一附属医院（皖南医学院弋矶山医院） 一种恶性胶质瘤生物标志物的应用
CN116209438A (zh) 2020-09-03 2023-06-02 锐新医药公司 使用sos1抑制剂治疗具有shp2突变的恶性疾病
CA3196694A1 (en) * 2020-11-02 2022-05-05 David Litzinger Crystalline forms of a deoxycytidine kinase inhibitor and uses thereof
WO2022140527A1 (en) 2020-12-23 2022-06-30 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
CN117222407A (zh) * 2021-02-12 2023-12-12 斯克里普斯研究学院 用于再生器官修复的yap转录活性的小分子激活剂
CN117136189A (zh) * 2021-04-09 2023-11-28 先声再明医药有限公司 泛素特异性蛋白酶1（usp1）抑制剂
CN114452286A (zh) * 2021-07-23 2022-05-10 上海交通大学医学院附属新华医院 Ral抑制剂防治骨关节炎
US11970494B2 (en) 2021-11-09 2024-04-30 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
TW202327602A (zh) * 2021-11-12 2023-07-16 香港商英科智能有限公司 泛素特異性蛋白酶1 (usp1)之小分子抑制劑及其用途
CA3235765A1 (en) 2021-11-12 2023-05-19 Jianping Wu Small molecule inhibitors of ubiquitin specific protease 1 (usp1) and uses thereof
CN114959012B (zh) * 2022-05-30 2023-04-07 北京医院 用于检测肌腱损伤的产品
CN115043851B (zh) * 2022-08-15 2023-01-06 山东第一医科大学第一附属医院(山东省千佛山医院) 一种噻吩[2,3-d]嘧啶类杂环化合物及其制备方法和应用
EP4342467A1 (en) * 2022-09-20 2024-03-27 Masarykova Univerzita Ku inhibitors for use in tumor therapy
EP4420661A1 (en) * 2023-02-24 2024-08-28 Universidade de Santiago de Compostela Small molecules targeting glycoprotein vi as antiplatelet agents

Family Cites Families (208)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE295381C (ru)
DE1470356A1 (de) 1964-01-15 1970-04-30 Thomae Gmbh Dr K Neue Thieno[3,2-d]pyrimidine und Verfahren zu ihrer Herstellung
DE1959403A1 (de) 1969-11-26 1971-06-03 Thomae Gmbh Dr K Neue 2-(5-Nitro-2-furyl)-thieno[3,2-d]pyrimidine und Verfahren zu ihrer Herstellung
DE2050815A1 (de) 1970-10-16 1972-04-20 Dr. Karl Thomae Gmbh, 7950 Biberach Neue 2-(5-Nitro-2-furyl)-thieno eckige Klammer auf 3,2-d eckige Klammer zu pyrimidine
DE2050814A1 (de) 1970-10-16 1972-04-20 Dr. Karl Thomae Gmbh, 7950 Biberach Neue Verfahren zur Herstellung von 2-(5-Nitro-2-furyl)-thieno eckige Klammer auf 3,2-d eckige Klammer zu pyrimidinen
DE2050816A1 (de) 1970-10-16 1972-04-20 Dr. Karl Thomae Gmbh, 7950 Biberach Neue 2-(Nitro-2-furyl>thieno eckige Klammer auf 3,2-d eckige Klammer zu pyrimidine
DE1959402A1 (de) 1969-11-26 1971-06-03 Thomae Gmbh Dr K Neue 2-(5-Nitro-2-furyl)-4-oxi-thieno[3,2-d]pyrimidine und Verfahren zu ihrer Herstellung
DE2039662A1 (de) 1970-08-10 1972-02-17 Thomae Gmbh Dr K Neue 2-(5-Nitro-2-furyl)-vinyl-thieno-[3,2-d]pyrimide
JPS5659778A (en) 1979-10-23 1981-05-23 Showa Denko Kk Dimethylthienopyrimidione derivative
IT1208123B (it) 1983-04-19 1989-06-06 Fondedile Spa Colonna in conglomerato realizzata nel terreno in situ mediante immissione di materiali inerti durante la perforazione e contemporaneao successiva iniezione con opportuni leganti, procedimenti di esecuzione relativi
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
EP0276057B1 (en) 1987-01-21 1994-03-09 Merck & Co. Inc. Piperazinylpyrimidines as beta-adrenergic receptor blocking agents
US5102877A (en) 1989-04-28 1992-04-07 Fujisawa Pharmaceutical Co., Ltd. 1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds
GB8912335D0 (en) 1989-05-30 1989-07-12 Smithkline Beckman Intercredit Compounds
DE3922735A1 (de) 1989-07-11 1991-01-24 Hoechst Ag Aminopyrimidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel und ihre verwendung als fungizide
DD295381A5 (de) 1990-10-01 1991-10-31 Karl-Marx-Universitaet Leipzig,De Verfahren zur herstellung von 8-amino-pyrazolo/4',3':4,5/thieno/3,2-d/pyrimidin-4-onen
US5202328A (en) 1991-03-06 1993-04-13 Merck & Co., Inc. Substituted fused pyrimidinones
JP2972843B2 (ja) 1991-04-02 1999-11-08 工業技術院長 有機非線形光学材料
US5223501A (en) 1991-05-10 1993-06-29 Merck & Co., Inc. Substituted pyrimidinones bearing acidic functional groups as angiotensin ii antagonists
TW201311B (ru) 1991-06-17 1993-03-01 Hoffmann La Roche
AU2390792A (en) 1991-08-05 1993-03-02 Taisho Pharmaceutical Co., Ltd. Thienopyrimidin-4-one derivative
US5187168A (en) 1991-10-24 1993-02-16 American Home Products Corporation Substituted quinazolines as angiotensin II antagonists
EP0696588A1 (en) 1992-07-17 1996-02-14 Rohm And Haas Company 2-Arylpyrimidines and herbicidal use thereof
EP0665224A1 (en) 1992-10-16 1995-08-02 Nippon Soda Co., Ltd. Pyrimidine derivative
US5360352A (en) 1992-12-24 1994-11-01 The Whitaker Corporation Wire retainer for current mode coupler
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US5654037A (en) * 1995-03-24 1997-08-05 Apx International Method of minimizing defects in painted composite material products
DK0882051T3 (da) 1996-02-07 2002-02-25 Janssen Pharmaceutica Nv Thiophenopyrimidiner
PT807633E (pt) 1996-05-15 2003-02-28 Pfizer Novas pirimidin-4-onas substituidas em 2,3, e fundidas com heteroarilo em (5,6)
CN1066448C (zh) 1996-06-06 2001-05-30 株式会社大塚制药工场 酰胺衍生物
DE19632423A1 (de) 1996-08-12 1998-02-19 Merck Patent Gmbh Thienopyrimidine
DE19644228A1 (de) * 1996-10-24 1998-04-30 Merck Patent Gmbh Thienopyrimidine
AU3709897A (en) 1996-11-28 1998-06-22 Cheil Jedang Corporation Cathecol derivatives and a method for the preparation thereof and a pharmaceutical composition containing the same
KR20010012319A (ko) 1997-05-08 2001-02-15 디 엘 리처 살진균제
EP0884310B1 (en) 1997-06-09 2005-09-07 Pfizer Products Inc. Quinazolin-4-one ampa antagonists
IL125950A0 (en) 1997-09-05 1999-04-11 Pfizer Prod Inc Methods of administering ampa receptor antagonists to treat dyskinesias associated with dopamine agonist therapy
US6323208B1 (en) 1997-09-05 2001-11-27 Pfizer Inc Atropisomers of 2,3-disubstituted-(5.6)-heteroaryl fused-pyrimidin-4-ones
GB9719411D0 (en) 1997-09-12 1997-11-12 Ciba Geigy Ag New Pesticides
BR9814018A (pt) 1997-11-11 2000-09-26 Pfizer Prod Inc Derivados de tienopirimidina e tienopiridina úteis como agentes anticâncer
US20120046290A1 (en) 1997-12-22 2012-02-23 Jacques Dumas Inhibition of p38 kinase activity using substituted heterocyclic ureas
US6187777B1 (en) 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
US6133271A (en) 1998-11-19 2000-10-17 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure thienopyrimidine derivatives
CN1346358A (zh) 1999-03-30 2002-04-24 日本曹达株式会社 噻吩并嘧啶化合物及其盐和制备方法
GB9915437D0 (en) 1999-07-01 1999-09-01 Cerebrus Ltd Chemical compounds III
CA2407593C (en) 2000-04-27 2011-01-11 Yamanouchi Pharmaceutical Co. Ltd. Fused heteroaryl derivatives
AR028782A1 (es) 2000-07-05 2003-05-21 Taisho Pharmaceutical Co Ltd Derivados heterociclicos tetrahidropiridino o piperidino
EP1322636A1 (en) * 2000-09-25 2003-07-02 Janssen Pharmaceutica N.V. Farnesyl transferase inhibiting 6- (substituted phenyl)methyl]-quinoline and quinazoline derivatives
CN1458933A (zh) 2000-09-29 2003-11-26 日本曹达株式会社 噻吩并嘧啶化合物及其盐以及其制备方法
GB0100620D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical cokpounds V
EP1254903B1 (en) 2001-04-20 2005-06-08 Ciba SC Holding AG 4-Amino-2-(pyridin-2-yl)pyrimidine as microbicidal active substances
GB0124627D0 (en) 2001-10-15 2001-12-05 Smithkline Beecham Plc Novel compounds
WO2003035653A1 (fr) 2001-10-26 2003-05-01 Nippon Soda Co.,Ltd. Compose pyridothienopyrimidine et son sel
SI1441734T1 (sl) 2001-10-26 2007-08-31 Angeletti P Ist Richerche Bio Dihidropirimidin karboksamidni inhibitorji HIV-integraze
EP1463733B1 (en) 2001-12-06 2007-09-05 Merck & Co., Inc. Mitotic kinesin inhibitors
EP1465900B1 (en) 2002-01-10 2008-05-14 Bayer HealthCare AG Rho-kinase inhibitors
WO2003106435A1 (en) 2002-06-18 2003-12-24 Sankyo Company, Limited Fused-ring pyrimidin-4(3h)-one derivatives, processes for the preparation and uses thereof
US20040132732A1 (en) 2002-10-21 2004-07-08 Wei Han Quinazolinones and derivatives thereof as factor Xa inhibitors
WO2004065392A1 (en) 2003-01-24 2004-08-05 Smithkline Beecham Corporation Condensed pyridines and pyrimidines and their use as alk-5 receptor ligands
TW200508224A (en) 2003-02-12 2005-03-01 Bristol Myers Squibb Co Cyclic derivatives as modulators of chemokine receptor activity
US7148226B2 (en) 2003-02-21 2006-12-12 Agouron Pharmaceuticals, Inc. Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
US7345046B2 (en) 2003-05-30 2008-03-18 Chiron Corporation Heteroaryl-fused pyrimidinyl compounds as anticancer agents
GB0315950D0 (en) * 2003-06-11 2003-08-13 Xention Discovery Ltd Compounds
US8309562B2 (en) 2003-07-03 2012-11-13 Myrexis, Inc. Compounds and therapeutical use thereof
JP2006193426A (ja) 2003-09-05 2006-07-27 Sankyo Co Ltd 置換された縮環ピリミジン−４（３ｈ）−オン化合物
JPWO2005026126A1 (ja) 2003-09-09 2006-11-16 小野薬品工業株式会社 Ｃｒｆ拮抗剤および二環式複素環化合物
DE10351436A1 (de) * 2003-11-04 2005-06-09 Merck Patent Gmbh Verwendung von Thienopyrimidinen
US20050176738A1 (en) 2003-11-07 2005-08-11 Neurocrine Biosciences, Inc. Melanin-concentrating hormone receptor antagonists and compositions and methods related thereto
WO2005082887A1 (ja) 2004-02-26 2005-09-09 Aska Pharmaceutical Co., Ltd. ピリミジン誘導体
JP2007535551A (ja) 2004-04-28 2007-12-06 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 Ｒｏｃｋおよび他のプロテインキナーゼの阻害剤として有用な組成物
CA2564085C (en) 2004-04-30 2013-04-02 Takeda Pharmaceutical Company Limited Heterocyclic amide compound and use thereof as an mmp-13 inhibitor
US7683097B2 (en) 2004-05-27 2010-03-23 Propharmacon Inc. Topoisomerase inhibitors
UY28931A1 (es) 2004-06-03 2005-12-30 Bayer Pharmaceuticals Corp Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis
US7598259B2 (en) 2004-06-15 2009-10-06 Schering Corporation mGluR1 antagonists as therapeutic agents
CA2583259C (en) 2004-10-08 2011-08-02 Astellas Pharma Inc. Aromatic ring fused pyrimidine derivative
JP2008517896A (ja) 2004-10-21 2008-05-29 ファイザー・インク Ｃ型肝炎ウイルスプロテアーゼの阻害剤並びにそれを用いた組成物及び治療
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
CA2593428C (en) 2005-01-10 2012-04-17 Pfizer Inc. Pyrrolopyrazoles, potent kinase inhibitors
CA2607929A1 (en) 2005-05-11 2006-11-16 Merck Sharp & Dohme Limited 2,3-substituted fused bicyclic pyrimidin-4(3h)-ones modulating the function of the vanilloid-1 receptor (vr1)
ATE474829T1 (de) 2005-06-27 2010-08-15 Amgen Inc Entzündungshemmende arylnitrilverbindungen
AU2005336552B2 (en) * 2005-09-23 2010-09-16 Equispharm Co., Ltd 5,6-dimethylthieno(2,3-di) pyrimidine derivatives, the preparation method thereof and the pharmaceutical composition comprising the same for anti-virus
US20070213305A1 (en) 2005-11-02 2007-09-13 Cytovia, Inc. N-alkyl-N-aryl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof
US20070099877A1 (en) 2005-11-02 2007-05-03 Cytovia, Inc. N-aryl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof
PE20070855A1 (es) 2005-12-02 2007-10-14 Bayer Pharmaceuticals Corp Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas
WO2007076085A2 (en) 2005-12-22 2007-07-05 Prolexys Pharmaceuticals, Inc . Fused pyrimidones and thiopyrimidones, and uses thereof
EP1987042B1 (en) 2006-02-15 2015-01-21 Sanofi Novel amino alcohol-substituted arylthienopyrimidinones, process for their preparation and their use as medicaments
WO2007102679A1 (en) * 2006-03-06 2007-09-13 Je Il Pharmaceutical Co., Ltd. Novel thienopyrimidine derivatives or pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical composition comprising the same
US8173806B2 (en) * 2006-03-17 2012-05-08 Mitsubishi Gas Chemical Company, Inc. Method for production of quinazolin-4-one derivative
BRPI0710908A2 (pt) * 2006-04-26 2012-06-26 Genentech Inc compostos inibidores de fosfoinositìdeo 3-cinase e composições farmacêuticas contendo-os
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
EP2034995A2 (en) 2006-05-25 2009-03-18 Synta Pharmaceuticals Corporation Method for treating proliferative disorders associated with protooncogene products
CA2654842A1 (en) 2006-06-12 2007-12-21 Vertex Pharmaceuticals Incorporated Thienopyrimidines useful as modulators of ion channels
FR2904318B1 (fr) 2006-07-27 2011-02-25 Scras Derives de pyrimidinone et leur utilisation comme medicament
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
WO2008020622A1 (fr) 2006-08-17 2008-02-21 Kyorin Pharmaceutical Co., Ltd. NOUVEAU COMPOSÉ DE THIÉNO[2,3-d]PYRIMIDINE
AU2007286807B2 (en) 2006-08-21 2013-03-21 Genentech, Inc. Aza-benzothiophenyl compounds and methods of use
ZA200901009B (en) 2006-08-21 2010-05-26 Genentech Inc Aza-benzothiophenyl compounds and methods of use
US20080090845A1 (en) 2006-08-23 2008-04-17 Neurogen Corporation Haloalkyl-substituted pyrimidinone derivatives
EP2066655A2 (en) 2006-09-07 2009-06-10 Neurosearch A/S Pyridinyl-pyrimidine derivatives useful as potassium channel modulating agents
JP2010509224A (ja) 2006-11-06 2010-03-25 ニューロジェン・コーポレーション ｃｉｓ−シクロヘキシル置換ピリミジノン誘導体
NZ576997A (en) 2006-11-13 2012-02-24 Icos Corp Thienopyrimidinones for treatment of inflammatory disorders and cancers
CA2670026A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterotricyclic metalloprotease inhibitors
ES2571028T3 (es) 2006-12-07 2016-05-23 Genentech Inc Compuestos inhibidores de fosfoinositida 3-cinasa y métodos de uso
WO2008082840A1 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
US20090030196A1 (en) 2006-12-29 2009-01-29 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008082839A2 (en) 2006-12-29 2008-07-10 Abbott Laboratories Pim kinase inhibitors as cancer chemotherapeutics
WO2008086053A1 (en) 2007-01-03 2008-07-17 Virobay, Inc. Hcv inhibitors
CL2008000252A1 (es) 2007-01-29 2008-03-14 Xenon Pharmaceuticals Inc Compuestos derivados de quinazolinona o pirimidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar enfermedades mediadas por los canales de calcio, tales como dolor, depresion, enfermedades cardiovasculares, respir
WO2008092861A1 (en) 2007-01-30 2008-08-07 Janssen Pharmaceutica N.V. Bicyclic derivatives as ep4 agonists
WO2008092860A1 (en) 2007-01-30 2008-08-07 Janssen Pharmaceutica N.V. Bicyclic derivatives as ep4 agonists
WO2008092862A1 (en) 2007-01-30 2008-08-07 Janssen Pharmaceutica N.V. Bicyclic derivatives as ep4 agonists
WO2008131050A1 (en) 2007-04-18 2008-10-30 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US7906513B2 (en) 2007-04-26 2011-03-15 Enanta Pharmaceuticals, Inc. Hydrazide-containing hepatitis C serine protease inhibitors
US20080287449A1 (en) 2007-04-26 2008-11-20 Deqiang Niu Aza-tripeptide hepatitis c serine protease inhibitors
EP2014663A1 (de) * 2007-07-12 2009-01-14 Bayer Schering Pharma AG Thienopyrimidylamine als Modulatoren des EP2-Rezeptors
WO2009026241A1 (en) 2007-08-23 2009-02-26 Kalypsys, Inc. Heterocyclic modulators of tgr5
DE102007040243A1 (de) 2007-08-25 2009-02-26 Universität des Saarlandes 17Beta-Hydroxysteriod-Dehydrogenase Typ1 Inhibitoren zur Behandlung hormonabhängiger Erkrankungen
DE102007051762A1 (de) 2007-10-30 2009-05-07 Bayer Healthcare Ag Substituierte Pyrrolotriazine und ihre Verwendung
WO2009064388A2 (en) 2007-11-09 2009-05-22 Liu Jun O Inhibitors of human methionine aminopeptidase 1 and methods of treating disorders
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
CN101969973B (zh) 2008-02-07 2015-07-22 维罗贝股份有限公司 组织蛋白酶b抑制剂
PE20091653A1 (es) 2008-03-26 2009-11-14 Takeda Pharmaceutical Derivados sustituidos de pirazol y su uso
WO2009121036A2 (en) 2008-03-27 2009-10-01 Neurogen Corporation Substituted aryl pyrimidinone derivatives
TWI389913B (zh) 2008-09-08 2013-03-21 Lg Life Sciences Ltd 并合雜環化合物
WO2010037765A2 (en) 2008-10-03 2010-04-08 Merck Serono S.A. 4-morpholino-pyrido[3,2-d]pyrimidines
US20100093702A1 (en) 2008-10-13 2010-04-15 Barbay J Kent METHYLENE AMINES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS
US20110135655A1 (en) 2009-01-13 2011-06-09 PHILADELPHIA HEALTH AND EDUCATION CORPORATION d/b/a Drexel University College of Medicine; Role of PI3K p110 delta Signaling in Retroviral Infection and Replication
EP2424368B1 (en) 2009-04-29 2014-12-31 Locus Pharmaceuticals, Inc. Pyrrolotriazine compounds
US8962639B2 (en) 2009-05-29 2015-02-24 Abbvie Inc. Potassium channel modulators
CA2768843A1 (en) 2009-07-21 2011-01-27 Gilead Calistoga Llc Treatment of liver disorders with pi3k inhibitors
MX2012002366A (es) 2009-08-27 2012-03-29 Merck Sharp & Dohme Agonistas novedosos de receptores beta 3 andrenergicos derivados de pirrolidina.
RS58796B1 (sr) 2010-02-17 2019-07-31 Takeda Pharmaceuticals Co Heterociklična jedinjenja
RU2012139182A (ru) * 2010-02-22 2014-03-27 Ф. Хоффманн-Ля Рош Аг ПИРИДО[3,2-d]ПИРИМИДИНЫ - ИНГИБИТОРЫ PI3К ДЕЛЬТА И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
WO2011104183A1 (en) 2010-02-24 2011-09-01 Syngenta Participations Ag Novel microbicides
WO2012004900A1 (en) 2010-07-09 2012-01-12 Aska Pharmaceutical Co., Ltd. Thienopyrimidine compounds
EP2611812A1 (en) 2010-09-01 2013-07-10 Ambit Biosciences Corporation Thienopyridine and thienopyrimidine compounds and methods of use thereof
AU2011302196B2 (en) 2010-09-14 2016-04-28 Exelixis, Inc. Inhibitors of PI3K-delta and methods of their use and manufacture
JP5972911B2 (ja) 2011-02-18 2016-08-17 アレクシオン ファーマ インターナショナル エスアーアールエル モリブドプテリン前駆体ｚ誘導体を合成するための方法
GB201105659D0 (en) * 2011-04-01 2011-05-18 Xention Ltd Compounds
EP2508184A1 (en) * 2011-04-06 2012-10-10 Æterna Zentaris GmbH Pyridopyrazine derivatives and their use
WO2012151567A1 (en) 2011-05-05 2012-11-08 St. Jude Children's Research Hospital Pyrimidinone compounds and methods for preventing and treating influenza
US9453021B2 (en) 2011-05-10 2016-09-27 Kyowa Hakko Kirin Co., Ltd. Pyrimidodiazepinone compound
DK2710018T3 (da) 2011-05-19 2022-03-21 Fundacion Del Sector Publico Estatal Centro Nac De Investigaciones Oncologicas Carlos Iii F S P Cnio Makrocykliske forbindelser som proteinkinasehæmmere
EP2714665A1 (en) 2011-05-24 2014-04-09 Università degli Studi di Bari "Aldo Moro" New 1-arylpiperazinic ligands of 5-ht7 receptor and use thereof
EP2731940B1 (en) 2011-07-13 2015-08-19 Novartis AG 4 - piperidinyl compounds for use as tankyrase inhibitors
RU2014111823A (ru) * 2011-08-29 2015-10-10 Инфинити Фармасьютикалз, Инк. Гетероциклические соединения и их применения
AR090037A1 (es) * 2011-11-15 2014-10-15 Xention Ltd Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio
ES2575143T3 (es) 2011-11-23 2016-06-24 Cancer Research Technology Limited Inhibidores de tienopiridina de la proteína quinasa C atípica
UY34484A (es) 2011-12-15 2013-07-31 Bayer Ip Gmbh Benzotienilo-pirrolotriazinas disustituidas y sus usos
US8940742B2 (en) * 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US9695133B2 (en) 2012-07-13 2017-07-04 The Trustees Of Columbia University In The City Of New York Quinazolinone-based oncogenic-RAS-selective lethal compounds and their use
US9566310B2 (en) 2012-09-10 2017-02-14 Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Reno Methods of treating muscular dystrophy
US20150291590A1 (en) 2012-09-17 2015-10-15 Cellixbio Private Limited Compositions and methods for the treatment of metabolic diseases
WO2014045039A2 (en) 2012-09-21 2014-03-27 Cancer Research Technology Limited Identification of protein kinase substrates
KR101446680B1 (ko) 2013-02-08 2014-10-07 한국과학기술연구원 ｍＧｌｕＲ1 길항제로 작용하는 사이에노피리미디논 유도체
UY35332A (es) 2013-02-15 2014-11-28 Almirall Sa Derivados de pirrolotriazina como inhibidores de pi3k
WO2014138562A1 (en) 2013-03-07 2014-09-12 Glaxosmithkline Llc Thieno[3,2-d]pyrimidine-6-carboxamides and analogues as sirtuin modulators
US9050345B2 (en) 2013-03-11 2015-06-09 Bristol-Myers Squibb Company Pyrrolotriazines as potassium ion channel inhibitors
RU2015148359A (ru) * 2013-04-12 2017-05-15 Асана Биосайенсис, Ллк Хиназолины и азахиназолины - двойные ингибиторы путей ras/raf/mek/erk и pi3k/akt/pten/mtor
US9797882B2 (en) * 2013-07-09 2017-10-24 The Translational Genomics Research Institute Method of screening for a compound for inhibitory activity of FN14-tweak interaction
EP3019874B1 (en) * 2013-07-09 2019-08-21 The Translational Genomics Research Institute Compositions and methods of screening for compounds that modulate activity at a tweak binding site on a crd of fn14
EP3036229A1 (en) 2013-08-22 2016-06-29 F. Hoffmann-La Roche AG Alkynyl alcohols and methods of use
MY176421A (en) 2013-09-22 2020-08-07 Sunshine Lake Pharma Co Ltd Substituted aminopyrimidine compounds and methods of use
WO2015043398A1 (zh) 2013-09-30 2015-04-02 上海璎黎药业有限公司 稠合嘧啶类化合物、中间体、其制备方法、组合物和应用
EP3052099B1 (en) 2013-10-03 2019-08-21 Merck Sharp & Dohme Corp. Novel pyrrolidine derived beta 3 adrenergic receptor agonists
JO3805B1 (ar) * 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
EA033689B9 (ru) 2013-10-10 2020-04-29 Араксис Фарма Ллк Ингибиторы g12c kras
WO2015148714A1 (en) 2014-03-25 2015-10-01 Duke University Heat shock protein 70 (hsp-70) receptor ligands
WO2015160192A1 (ko) 2014-04-15 2015-10-22 연세대학교 산학협력단 티에노피리미딘 유도체 또는 이의 약학적으로 허용가능한 염을 포함하는 백혈병 치료 및 예방용 약학 조성물
US10174032B2 (en) * 2014-05-05 2019-01-08 Signalrx Pharmaceuticals, Inc. Heterocyclic compound classes for signaling modulation
JP6673853B2 (ja) 2014-05-07 2020-03-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ヘテロシクリル−ブタンアミド誘導体
WO2015183989A1 (en) 2014-05-27 2015-12-03 Navigen, Inc. Arf6 inhibitors and methods of synthesis and use thereof
CN104230952B (zh) 2014-08-16 2017-02-01 沈阳药科大学 含有嘧啶骨架的化合物及其制备方法和用途
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
EP3212647B1 (en) * 2014-10-29 2019-04-03 Dong-A ST Co., Ltd. Novel pyridopyrimidinone compounds for modulating the catalytic activity of histone lysine demethylases (kdms)
KR20180013851A (ko) 2015-03-09 2018-02-07 바이엘 파마 악티엔게젤샤프트 치환된 2,3-디히드로이미다조[1,2-c]퀴나졸린-함유 조합물
US10487078B2 (en) 2015-04-03 2019-11-26 Nantbio, Inc. Compositions and methods of targeting mutant K-RAS
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
US10421764B2 (en) 2015-04-24 2019-09-24 H. Lee Moffitt Cancer Center And Research Institute, Inc. Mutant KRas inhibitors
JP6900320B2 (ja) * 2015-05-13 2021-07-07 メモリアル スローン ケタリング キャンサー センター がんにおけるマイクロピノサイトーシス
US10463649B2 (en) * 2015-06-08 2019-11-05 Texas Tech University System Inhibitors of Mc1-1 as drugs to overcome resistance to BRAF inhibitors and MEK inhibitors
WO2016201257A2 (en) 2015-06-10 2016-12-15 The Johns Hopkins University Compositions and methods for identifying adp-ribosylated sites by mass spectrometry
EP3325447A1 (en) 2015-07-22 2018-05-30 Araxes Pharma LLC Substituted quinazoline compounds and their use as inhibitors of g12c mutant kras, hras and/or nras proteins
CN108026105B (zh) 2015-07-23 2020-10-16 百时美施贵宝公司 TGFβ受体拮抗剂
WO2017031176A1 (en) 2015-08-17 2017-02-23 Duquesne University Of The Holy Spirit Monocyclic, thieno, pyrido, and pyrrolo pyrimidine compounds and methods of use and manufacture of the same
US20170057955A1 (en) * 2015-08-26 2017-03-02 Dong-A Socio Holdings Co., Ltd. Pyridopyrimidinone Compounds for Modulating the Catalytic Activity of Histone Lysine Demethylases (KDMs)
KR20180041752A (ko) 2015-08-31 2018-04-24 브리스톨-마이어스 스큅 컴퍼니 Tgf 베타 수용체 길항제
WO2017058805A1 (en) * 2015-09-28 2017-04-06 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
WO2017058807A1 (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
EP3356351A1 (en) * 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
JP6896715B2 (ja) 2015-09-30 2021-06-30 マックス−プランク−ゲゼルシャフト ツール フェルデルング デル ヴィッセンシャフテン エーファウ −ジェネラルフェルヴァルトゥング セピアプテリン還元酵素としてのヘテロアリール誘導体
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
KR20240113606A (ko) 2015-11-16 2024-07-22 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
JP7114076B2 (ja) 2015-12-22 2022-08-08 シャイ・セラピューティクス・エルエルシー がん及び炎症性疾患の処置のための化合物
JP6918824B2 (ja) 2016-03-28 2021-08-11 武田薬品工業株式会社 ２−［（２Ｓ）−１−アザビシクロ［２．２．２］オクタ−２−イル］−６−（３−メチル−１Ｈ−ピラゾール−４−イル）チエノ［３，２−ｄ］ピリミジン−４（３Ｈ）−オン半水和物の結晶形
EP3290412A1 (en) 2016-08-31 2018-03-07 Università degli Studi di Siena Hiv-1 nucleocapsid inhibitors
KR20180066985A (ko) 2016-12-11 2018-06-20 연세대학교 산학협력단 티에노피리미딘 유도체 및 이의 용도
WO2018237084A1 (en) 2017-06-21 2018-12-27 SHY Therapeutics LLC COMPOUNDS INTERACTING WITH RAS SUPERFAMIL FOR USE IN THE TREATMENT OF CANCERS, INFLAMMATORY DISEASES, RASOPATHIES AND FIBROTIC DISEASES
US20220117968A1 (en) 2017-07-17 2022-04-21 Saint Louis University Thieno[2,3-d)pyrimidines and benzofuro(3,2-d)pyrimidines as antimicrobial agents
CN107721982B (zh) 2017-10-16 2019-12-03 中山大学 一种抗肥胖症化合物及其制备方法和应用
WO2019105734A1 (en) 2017-11-28 2019-06-06 Bayer Consumer Care Ag Combinations of copanlisib
CN111094317B (zh) 2017-12-29 2023-03-31 上海和誉生物医药科技有限公司 一种具有cd73抑制活性的膦酸衍生物、其制备方法和应用
WO2019180141A1 (en) 2018-03-23 2019-09-26 Bayer Aktiengesellschaft Combinations of rogaratinib

Also Published As

Publication number Publication date
CN111032662A (zh) 2020-04-17
US20220347162A1 (en) 2022-11-03
US10588894B2 (en) 2020-03-17
MA49458A (fr) 2020-04-29
US11541041B1 (en) 2023-01-03
IL271230A (en) 2020-01-30
JP2023179774A (ja) 2023-12-19
AU2018288841B2 (en) 2022-09-29
EP4331679A2 (en) 2024-03-06
EP3642209A1 (en) 2020-04-29
MX2022010225A (es) 2022-09-19
MX2019014875A (es) 2021-01-29
US20200054614A1 (en) 2020-02-20
KR20200041294A (ko) 2020-04-21
US11213515B1 (en) 2022-01-04
AU2022263550A1 (en) 2022-12-08
WO2018237084A1 (en) 2018-12-27
US10940139B2 (en) 2021-03-09
US20230149369A1 (en) 2023-05-18
JP7514005B2 (ja) 2024-07-10
MX2022010224A (es) 2022-11-16
EP3642209B1 (en) 2023-11-29
US10933054B2 (en) 2021-03-02
CA3066939A1 (en) 2018-12-27
US20200121660A1 (en) 2020-04-23
IL271230B1 (en) 2024-02-01
US11000515B2 (en) 2021-05-11
US20200061037A1 (en) 2020-02-27
IL310023A (en) 2024-03-01
EP4331679A3 (en) 2024-04-03
IL271230B2 (en) 2024-06-01
US20190022074A1 (en) 2019-01-24
US11026930B1 (en) 2021-06-08
BR112019027640A2 (pt) 2020-07-07
SG11201911929XA (en) 2020-01-30
CN111032662B (zh) 2024-10-15
JP2022177278A (ja) 2022-11-30
AU2022263550B2 (en) 2024-07-04
AU2018288841A1 (en) 2020-01-02
JP2020524703A (ja) 2020-08-20

Similar Documents

Publication Publication Date Title
EA201992780A1 (ru) Соединения, которые взаимодействуют с суперсемейством ras, для лечения рака, воспалительных заболеваний, ras-опатий и фиброзного заболевания
EA202090104A1 (ru) Молекулы антител к cd73 и пути их применения
PH12018500233A1 (en) Single domain antibody programmed death-ligand (pd-l1) and derived protein thereof
EA201890453A1 (ru) Анти-angptl8 антитела и их применение
EA201892294A1 (ru) Антитела и композиции против tim-3
EA201591072A1 (ru) Антитела против pdgfr-бета и их применения
CY1121097T1 (el) Ανθρωπινα αντισωματα κατα toy gfr 3 και μεθοδοι χρησης αυτων
EA201992712A3 (ru) Трициклические гетероциклы как ингибиторы белков бэт
EA201890131A1 (ru) Иммуномодуляция и лечение солидных опухолей антителами, которые специфически связывают cd38
EA201790377A1 (ru) Антитела к глюкагону и их применения
EA201890145A1 (ru) Антитела к фактору xi и способы их применения
EA201892229A1 (ru) Замещенные аминопуриновые соединения, содержащие их композиции и способы лечения с их применением
EA201990296A1 (ru) Антитела против siglec-7 для лечения рака
EA201790413A1 (ru) Антитела против tigit
EA201992808A1 (ru) ПОЛИПЕПТИДЫ, ПРЕПЯТСТВУЮЩИЕ ПЕРЕДАЧЕ Wnt СИГНАЛОВ В ОПУХОЛЕВЫХ КЛЕТКАХ
EA201990778A1 (ru) Анти-il-33 антитела и их применение
EA201692091A1 (ru) Хиноксалиновые соединения и их применение
EA201892225A1 (ru) АНТИТЕЛА К ФАКТОРУ Bb КОМПЛЕМЕНТА И ИХ ПРИМЕНЕНИЕ
EA201201464A1 (ru) Новая комбинированная терапия для лечения онкологических и фиброзных заболеваний
EA201992248A1 (ru) АНТИ-C5a-АНТИТЕЛА И ИХ ПРИМЕНЕНИЯ
MD3522880T2 (ro) Metode de tratare a leziunilor renale acute
CY1121156T1 (el) Μεθοδοι αντιμετωπισης ινωσης και καρκινων
BR112017022022A2 (pt) arenavírus para uso no tratamento e/ou prevenção de tumores e método para a produção de arenavírus com propriedades de regressão de tumor (aprimoradas)
EA202090707A1 (ru) Эндоглиновые пептиды для лечения фиброзных заболеваний
EA201991196A1 (ru) Претерпевшие самосборку диблок-сополимеры, состоящие из pegmema и несущих лекарственное средство полимерных сегментов