[go: up one dir, main page]

CR20220066A - Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2 - Google Patents

Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2

Info

Publication number
CR20220066A
CR20220066A CR20220066A CR20220066A CR20220066A CR 20220066 A CR20220066 A CR 20220066A CR 20220066 A CR20220066 A CR 20220066A CR 20220066 A CR20220066 A CR 20220066A CR 20220066 A CR20220066 A CR 20220066A
Authority
CR
Costa Rica
Prior art keywords
pyrimidinylamine
cdk2
imidazolyl
inhibitors
compounds
Prior art date
Application number
CR20220066A
Other languages
English (en)
Inventor
Qinda Ye
Yvonne Lo
Jingwei Li
Liangxing Wu
Min Ye
Yingnan Chen
Brandon Smith
Wenqing Yao
Margaret Favata
Ken Mukai
Original Assignee
Incyte 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 Incyte Corp filed Critical Incyte Corp
Publication of CR20220066A publication Critical patent/CR20220066A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4738—Cell cycle regulated proteins, e.g. cyclin, CDC, INK-CCR
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
    • C07D471/08—Bridged systems
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • 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
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6844—Nucleic acid amplification reactions
    • C12Q1/6865—Promoter-based amplification, e.g. nucleic acid sequence amplification [NASBA], self-sustained sequence replication [3SR] or transcription-based amplification system [TAS]
    • 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
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
    • 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
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57407—Specifically defined cancers
    • 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
    • G01N33/6893—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to diseases not provided for elsewhere
    • 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
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/158—Expression markers
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/46—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
    • G01N2333/47—Assays involving proteins of known structure or function as defined in the subgroups
    • G01N2333/4701—Details
    • G01N2333/4703—Regulators; Modulating activity
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2440/00—Post-translational modifications [PTMs] in chemical analysis of biological material
    • G01N2440/14—Post-translational modifications [PTMs] in chemical analysis of biological material phosphorylation
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/52—Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
    • 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
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/574—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/57484—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumor, cancer, neoplasia, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides, metabolites

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Analytical Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Zoology (AREA)
  • Pathology (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Cell Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Food Science & Technology (AREA)
  • General Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

La presente solicitud proporciona inhibidores de imidazolil pirimidinilamina de la quinasa 2 dependiente de ciclina (CDK2), así como sus composiciones farmacéuticas, y métodos para tratar el cáncer usando los mismos
CR20220066A 2019-08-14 2020-08-13 Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2 CR20220066A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962886735P 2019-08-14 2019-08-14
PCT/US2020/046078 WO2021030537A1 (en) 2019-08-14 2020-08-13 Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors

Publications (1)

Publication Number Publication Date
CR20220066A true CR20220066A (es) 2022-11-28

Family

ID=72243220

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20220066A CR20220066A (es) 2019-08-14 2020-08-13 Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2

Country Status (19)

Country Link
US (2) US11427567B2 (es)
EP (1) EP4013750A1 (es)
JP (1) JP2023509260A (es)
KR (1) KR20220064369A (es)
CN (1) CN116348458A (es)
AR (1) AR119765A1 (es)
AU (1) AU2020328025A1 (es)
BR (1) BR112022002698A2 (es)
CA (1) CA3150681A1 (es)
CL (1) CL2022000339A1 (es)
CO (1) CO2022001453A2 (es)
CR (1) CR20220066A (es)
EC (1) ECSP22011692A (es)
IL (1) IL290527A (es)
MX (1) MX2022001940A (es)
PE (1) PE20221010A1 (es)
PH (1) PH12022550361A1 (es)
TW (1) TW202115024A (es)
WO (1) WO2021030537A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
CA3157681A1 (en) 2019-10-11 2021-04-15 Incyte Corporation Bicyclic amines as cdk2 inhibitors
WO2022113003A1 (en) 2020-11-27 2022-06-02 Rhizen Pharmaceuticals Ag Cdk inhibitors
AU2021409561A1 (en) 2020-12-22 2023-07-06 Nikang Therapeutics, Inc. Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors
JP2024506039A (ja) * 2021-02-05 2024-02-08 シャンハイ チールー ファーマシューティカル リサーチ アンド ディベロップメント センター リミテッド Ｃｄｋ阻害剤
BR112023023223A2 (pt) 2021-05-07 2024-01-30 Kymera Therapeutics Inc Degradadores de cdk2 e usos dos mesmos
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2023172957A1 (en) * 2022-03-09 2023-09-14 Prelude Therapeutics, Incorporated Thaizole-pyrimdiine cdk inhibitors and their use as pharmaceuticals
TW202417449A (zh) * 2022-07-28 2024-05-01 美商賽迪拉治療股份有限公司 Cdk2抑制劑及使用彼等之方法
TW202408510A (zh) * 2022-08-05 2024-03-01 大陸商齊魯製藥有限公司 Ｃｄｋ抑制劑及其磷酸鹽的多晶型、其製備方法、包含其的醫藥組合物及其用途
WO2024066986A1 (zh) * 2022-09-30 2024-04-04 楚浦创制（武汉）医药科技有限公司 2-氨基嘧啶类化合物及其应用、药用组合物

Family Cites Families (331)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2530632A1 (fr) 1982-07-26 1984-01-27 Bouchara Emile Nouveaux derives substitues du 2,5-diamino 1,4-diazole, leurs procedes de preparation et les compositions pharmaceutiques en renfermant
US4569933A (en) 1984-04-13 1986-02-11 Cornu Pierre Jean Antihypertensive substituted derivatives of 2,5-diamino 1,4-diazole
US5304555A (en) 1987-08-26 1994-04-19 Mitsui Petrochemical Industries, Ltd. Pyrimidines and pharmaceutically acceptable salts thereof useful in treatment of neurological disorders
US5210015A (en) 1990-08-06 1993-05-11 Hoffman-La Roche Inc. Homogeneous assay system using the nuclease activity of a nucleic acid polymerase
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
US5466692A (en) 1993-03-24 1995-11-14 American Home Products Corporation Substituted pyridopyrimidines and antihypertensives
US6498163B1 (en) 1997-02-05 2002-12-24 Warner-Lambert Company Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
BR9912938B1 (pt) 1998-08-11 2011-06-28 derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos.
US6559152B2 (en) 1998-10-13 2003-05-06 Dupont Pharmaceuticals Company 6-substituted pyrazolo[3,4-d]pyrimidin-4-ones useful as cyclin dependent kinase inhibitors
US6596747B2 (en) 1998-10-29 2003-07-22 Bristol-Myers Squibb Company Compounds derived from an amine nucleus and pharmaceutical compositions comprising same
JP2002528533A (ja) 1998-10-29 2002-09-03 ブリストル−マイヤーズ スクイブ カンパニー 酵素ｉｍｐｄｈの新規なインヒビター
CA2348234A1 (en) 1998-10-29 2000-05-11 Chunjian Liu Compounds derived from an amine nucleus that are inhibitors of impdh enzyme
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US6440959B1 (en) 1999-04-21 2002-08-27 Hoffman-La Roche Inc. Pyrazolobenzodiazepines
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
AU6909600A (en) 1999-08-13 2001-03-13 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
MXPA02002559A (es) 1999-09-10 2002-07-30 Merck & Co Inc Inhibidores de tirosina cinasa.
ES2335265T3 (es) 1999-12-28 2010-03-24 Pharmacopeia, Inc. Inhibidores de citoquina, especialmente de tnf-alfa.
KR20030024659A (ko) 2000-02-17 2003-03-26 암겐 인코포레이티드 키나제 억제제
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
IL151946A0 (en) 2000-03-29 2003-04-10 Cyclacel Ltd 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of proliferative disorders
NZ522783A (en) 2000-06-28 2004-07-30 Smithkline Beecham P Wet milling process for pharmaceuticals with agitator or chamber having nylon with internal lubricant
WO2002016348A1 (en) 2000-08-09 2002-02-28 Astrazeneca Ab Antiangiogenic bicyclic derivatives
GB0021726D0 (en) 2000-09-05 2000-10-18 Astrazeneca Ab Chemical compounds
PT1317448E (pt) 2000-09-15 2005-08-31 Vertex Pharma Compostos de pirazole uteis como inibidores de proteina-quinase
DE60138140D1 (de) 2000-10-31 2009-05-07 Aventis Pharma Inc Acyl- und sulfonylderivative 6,9-disubstitutierter 2-(trans-1,4-diaminocyclohexyl)-purine und ihre verwendung als antiproliferative mittel
ATE407132T1 (de) 2000-12-05 2008-09-15 Vertex Pharma Inhibitoren von c-jun n-terminalen kinasen (jnk) und anderen proteinkinasen
US7429599B2 (en) 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
US7122544B2 (en) 2000-12-06 2006-10-17 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
WO2002070751A1 (en) 2001-03-02 2002-09-12 University Of Pittsburgh Of The Commonwealth System Of Higher Education Pcr method
EP1372642A1 (en) 2001-03-30 2004-01-02 SmithKline Beecham Corporation Use of pyrazolopyridines as therapeutic compounds
JP4237497B2 (ja) 2001-03-30 2009-03-11 スミスクライン ビーチャム コーポレーション ピラゾロピリジン類、その調製方法及びその治療用化合物としての使用
US6812341B1 (en) 2001-05-11 2004-11-02 Ambion, Inc. High efficiency mRNA isolation methods and compositions
CA2446864C (en) 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
JP4523271B2 (ja) 2001-06-01 2010-08-11 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 プロテインキナーゼのインヒビターとして有用なチアゾール化合物
CA2450934A1 (en) 2001-06-19 2002-12-27 Marco Dodier Pyrimidine inhibitors of phosphodiesterase (pde) 7
WO2003011837A1 (en) 2001-08-01 2003-02-13 Merck & Co., Inc. Tyrosine kinase inhibitors
US20040181066A1 (en) 2001-08-01 2004-09-16 Fraley Mark E. Tyrosine kinase inhibitors
WO2003011836A1 (en) 2001-08-01 2003-02-13 Merck & Co., Inc. Tyrosine kinase inhibitors
CN100391958C (zh) 2001-09-19 2008-06-04 安万特医药股份有限公司 化合物
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
US7473695B2 (en) 2001-10-22 2009-01-06 Mitsubishi Tanabe Pharma Corporation 4-imidazolin-2-one compounds
HU230798B1 (hu) 2001-10-30 2018-06-28 Novartis Ag Staurosporin-származékok mint az FLT3 receptor tirozin-kináz aktivitás inhibitorai
CA2466279A1 (en) 2001-11-13 2003-05-22 Dana-Farber Cancer Institute, Inc. Agents that modulate immune cell activation and methods of use thereof
AU2002350217A1 (en) 2001-12-04 2003-06-17 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
JP2005524609A (ja) 2001-12-17 2005-08-18 スミスクライン ビーチャム コーポレーション ピラゾロピリダジン誘導体
US7550459B2 (en) 2001-12-28 2009-06-23 Acadia Pharmaceuticals, Inc. Tetrahydroquinoline analogues as muscarinic agonists
GEP20063909B (en) 2002-01-22 2006-08-25 Warner Lambert Co 2-(PYRIDIN-2-YLAMINO)-PYRIDO[2,3d] PYRIMIDIN-7-ONES
US6852730B2 (en) 2002-02-07 2005-02-08 Neurogen Corporation Substituted fused pyrazolecarboxylic acid arylamides and related compounds
ES2245772T3 (es) 2002-03-07 2006-01-16 Smithkline Beecham Corporation Derivados de pirazolopirimidina y pirazolotriazina y composiciones farmaceuticas que los contienen.
CA2478338A1 (en) 2002-03-08 2003-09-18 Signal Pharmaceuticals, Inc. Combination therapy for treating, preventing or managing proliferative disorders and cancers
WO2003076437A1 (de) 2002-03-11 2003-09-18 Schering Aktiengesellschaft Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel
RU2310657C2 (ru) 2002-04-03 2007-11-20 Ф.Хоффманн-Ля Рош Аг Имидазоконденсированные соединения и фармацевтическая композиция, содержащая их
GB0210127D0 (en) 2002-05-02 2002-06-12 Merck Sharp & Dohme Therapeutic agents
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US7252976B2 (en) 2002-08-28 2007-08-07 Board Of Regents The University Of Texas System Quantitative RT-PCR to AC133 to diagnose cancer and monitor angiogenic activity in a cell sample
WO2004035588A1 (en) 2002-10-15 2004-04-29 Smithkline Beecham Corporation Pyradazine compounds as gsk-3 inhibitors
AU2003291310A1 (en) 2002-11-06 2004-06-03 Bristol-Myers Squibb Company Fused heterocyclic compounds and use thereof
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
US7098332B2 (en) 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
AU2003288675B2 (en) 2002-12-23 2010-07-22 Medimmune Limited Antibodies against PD-1 and uses therefor
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
ATE396731T1 (de) 2003-03-25 2008-06-15 Vertex Pharma Thiazole zur verwendung als inhibitoren von protein-kinasen
EP1610793A2 (en) 2003-03-25 2006-01-04 Vertex Pharmaceuticals Incorporated Thiazoles useful as inhibitors of protein kinases
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
JP4881725B2 (ja) 2003-04-09 2012-02-22 エクセリクシス， インク． Ｔｉｅ−２モジュレータと使用方法
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
ES2362877T3 (es) 2003-04-21 2011-07-14 Mitsubishi Tanabe Pharma Corporation Compuestos de imidazolin-2-ona.
WO2004111037A1 (ja) 2003-06-11 2004-12-23 Sankyo Company, Limited 環状3級アミン化合物
US20060293340A1 (en) 2003-06-13 2006-12-28 Novartis Ag 2-Aminopyrimidine derivatives as raf kinase inhibitors
GB0315966D0 (en) 2003-07-08 2003-08-13 Cyclacel Ltd Compounds
JP2007500179A (ja) 2003-07-30 2007-01-11 サイクラセル・リミテッド キナーゼ阻害剤としての２−アミノフェニル−４−フェニルピリミジン
US7160888B2 (en) 2003-08-22 2007-01-09 Warner Lambert Company Llc [1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia
WO2005020921A2 (en) 2003-08-29 2005-03-10 Exelixis, Inc. C-kit modulators and methods of use
WO2005065074A2 (en) 2003-09-09 2005-07-21 Temple University Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
CN1897950A (zh) 2003-10-14 2007-01-17 惠氏公司 稠合芳基和杂芳基衍生物及其使用方法
US7169781B2 (en) 2003-10-17 2007-01-30 Hoffmann-La Roche Inc. Imidazole derivatives and their use as pharmaceutical agents
WO2005040135A1 (ja) 2003-10-24 2005-05-06 Ono Pharmaceutical Co., Ltd. 抗ストレス薬およびその医薬用途
KR20060133552A (ko) 2004-01-16 2006-12-26 노파르티스 아게 2,4-디아미노피리미딘 및 심장근육발생 유도를 위한 그의용도
WO2005080393A1 (en) 2004-02-14 2005-09-01 Irm Llc Compounds and compositions as protein kinase inhibitors
CN1926140A (zh) 2004-03-05 2007-03-07 大正制药株式会社 吡咯并嘧啶衍生物
PL1725544T3 (pl) 2004-03-09 2009-10-30 Boehringer Ingelheim Pharmaceuticals Inc 3-[4-Heterocyklilo-1,2,3-triazol-1-ilo]-N-arylobenzamidy jako inhibitory wytwarzania cytokin, do leczenia przewlekłych chorób zapalnych
US7306631B2 (en) 2004-03-30 2007-12-11 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
CN1946703A (zh) 2004-04-20 2007-04-11 特兰斯泰克制药公司 取代的噻唑和嘧啶衍生物作为黑素细胞皮质激素受体调节剂
WO2005107760A1 (en) 2004-04-30 2005-11-17 Irm Llc Compounds and compositions as inducers of keratinocyte differentiation
US7405220B2 (en) 2004-06-09 2008-07-29 Hoffmann-La Roche Inc. Pyrazolopyrimidines
AR049511A1 (es) 2004-06-10 2006-08-09 Irm Llc Compuestos y composiciones como inhibidores de quinasa de proteina
US7709645B2 (en) 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
EP1786817A1 (de) 2004-08-26 2007-05-23 Boehringer Ingelheim International GmbH Pteridinone als plk (polo like kinase) inhibitoren
US7718801B2 (en) 2004-08-31 2010-05-18 Banyu Pharmaceutical Co., Ltd. Substituted imidazole derivative
EP1794135A1 (en) 2004-09-27 2007-06-13 Amgen Inc. Substituted heterocyclic compounds and methods of use
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
JP2008519814A (ja) 2004-11-12 2008-06-12 ガラパゴス・ナムローゼ・フェンノートシャップ プロテインキナーゼ酵素の活性部位と結合する窒素複素環式芳香族化合物
AU2005309019A1 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors
JP2006188504A (ja) 2004-12-10 2006-07-20 Sankyo Co Ltd 環状３級アミン化合物を含有する医薬組成物
CA2590250A1 (en) 2004-12-14 2006-06-22 Vertex Pharmaceuticals Incorporated Pyrimidine inhibitors of erk protein kinase and uses therof
DE602005014382D1 (de) 2004-12-21 2009-06-18 Smithkline Beecham Corp 2-pyrimidinyl-pyrazolopyridin-erbb-kinaseinhibitoren
US20060142312A1 (en) 2004-12-23 2006-06-29 Pfizer Inc C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones
JP5208516B2 (ja) 2004-12-30 2013-06-12 エグゼリクシス， インコーポレイテッド キナーゼモジュレーターとしてのピリミジン誘導体および使用方法
GB0428514D0 (en) 2004-12-31 2005-02-09 Prosidion Ltd Compounds
CN1939910A (zh) 2004-12-31 2007-04-04 孙飘扬 氨基嘧啶类化合物及其盐和其制备方法与药物用途
AU2006205851A1 (en) 2005-01-14 2006-07-20 Janssen Pharmaceutica N.V. 5-membered annelated heterocyclic pyrimidines as kinase inhibitors
US20060223807A1 (en) 2005-03-29 2006-10-05 University Of Massachusetts Medical School, A Massachusetts Corporation Therapeutic methods for type I diabetes
EP2418278A3 (en) 2005-05-09 2012-07-04 Ono Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1(PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapeutics
US8193206B2 (en) 2005-06-14 2012-06-05 Taigen Biotechnology Co., Ltd. Pyrimidine compounds
MY150958A (en) 2005-06-16 2014-03-31 Astrazeneca Ab Compounds for the treatment of multi-drug resistant bacterial infections
CN102603581B (zh) 2005-06-22 2015-06-24 普莱希科公司 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物
US7442700B2 (en) 2005-07-01 2008-10-28 Bristol-Myers Squibb Company Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith
EP2982379A1 (en) 2005-07-01 2016-02-10 E. R. Squibb & Sons, L.L.C. Human monoclonal antibodies to programmed death ligand 1 (pd-l1)
US7309787B2 (en) 2005-07-13 2007-12-18 Allergan, Inc. Kinase inhibitors
ATE517883T1 (de) 2005-08-25 2011-08-15 Schering Corp Imidazolderivate als funktionelle selektive agonisten des alpha2c-adrenorezeptors
US8003624B2 (en) 2005-08-25 2011-08-23 Schering Corporation Functionally selective ALPHA2C adrenoreceptor agonists
CN101304736A (zh) 2005-09-07 2008-11-12 雪兰诺实验室公司 治疗子宫内膜异位症的ikk抑制剂
JP2009507080A (ja) 2005-09-07 2009-02-19 リゲル ファーマシューティカルズ，インコーポレーテッド Ａｘｌ阻害剤として有用なトリアゾール誘導体
US7705009B2 (en) 2005-11-22 2010-04-27 Hoffman-La Roche Inc. 4-aminopyrimidine-5-thione derivatives
JP5103403B2 (ja) 2005-12-05 2012-12-19 スミスクライン ビーチャム コーポレーション ２−ピリミジニルピラゾロピリジンＥｒｂＢキナーゼ阻害剤
TW200804349A (en) 2005-12-23 2008-01-16 Kalypsys Inc Novel substituted pyrimidinyloxy ureas as inhibitors of protein kinases
WO2007084314A2 (en) 2006-01-12 2007-07-26 Incyte Corporation MODULATORS OF 11-ß HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
EP2013216A2 (en) 2006-02-07 2009-01-14 AstraZeneca AB Novel spiro [imidazolidine-4, 3' -indole] 2, 2', 5' (1h) triones for treatment of conditions associated with vanilloid receptor 1
JP2007217322A (ja) 2006-02-15 2007-08-30 Ube Ind Ltd 慢性閉塞性肺疾患の治療又は予防のための医薬組成物
CA2643066A1 (en) 2006-03-16 2007-09-20 Pfizer Products Inc. Pyrazole compounds
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
AU2007254491A1 (en) 2006-05-15 2007-11-29 Irm Llc Compositions and methods for FGF receptor kinases inhibitors
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
TW200811169A (en) * 2006-05-26 2008-03-01 Astrazeneca Ab Chemical compounds
TW200815417A (en) 2006-06-27 2008-04-01 Astrazeneca Ab New compounds II
EP2043651A2 (en) 2006-07-05 2009-04-08 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
WO2008009435A1 (en) 2006-07-20 2008-01-24 Novartis Ag Amino-piperidine derivatives as cetp inhibitors
US8314234B2 (en) 2006-09-25 2012-11-20 Janssen Pharmaceutica N.V. Bicyclic pyrimidine kinase inhibitors
EA200970512A1 (ru) 2006-11-27 2009-12-30 Арес Трейдинг С.А. Лечение по поводу множественной миеломы
ES2527696T3 (es) 2006-12-21 2015-01-28 Nerviano Medical Sciences S.R.L. Derivados de pirazoloquinazolina sustituidos, procedimientos para su preparación y su uso como inhibidores de la quinasa
PT2170959E (pt) 2007-06-18 2014-01-07 Merck Sharp & Dohme Anticorpos para o receptor humano de morte programada pd-1
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
BRPI0815042A2 (pt) 2007-08-01 2015-02-10 Pfizer Compostos de pirazol
WO2009034390A1 (en) 2007-09-14 2009-03-19 Arrow Therapeutics Limited Heterocyclic derivatives and their use in treating hepatitis c
US8314094B2 (en) 2007-10-05 2012-11-20 Msd K.K Benzoxazinone derivative
GB0719803D0 (en) 2007-10-10 2007-11-21 Cancer Rec Tech Ltd Therapeutic compounds and their use
US9259399B2 (en) 2007-11-07 2016-02-16 Cornell University Targeting CDK4 and CDK6 in cancer therapy
US8309718B2 (en) 2007-11-16 2012-11-13 Incyte Corporation 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
ES2374480T3 (es) 2007-12-07 2012-02-17 Novartis Ag Derivados pirazol y uso de los mismos como inhibidores de quinasas dependientes de ciclina.
PL2217600T3 (pl) 2007-12-12 2013-04-30 Du Pont Grzybobójcze pirazole bicykliczne
AU2008343932B2 (en) 2007-12-19 2013-08-15 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
JP5520831B2 (ja) 2007-12-19 2014-06-11 アムジエン・インコーポレーテツド Ｐｉ３キナーゼの阻害薬
WO2009089508A1 (en) 2008-01-11 2009-07-16 The Regents Of The University Of California Activators of executioner procaspases 3, 6 and 7
KR101247840B1 (ko) 2008-02-22 2013-03-26 에프. 호프만-라 로슈 아게 아밀로이드 베타 조절제
WO2009114335A2 (en) 2008-03-12 2009-09-17 Merck & Co., Inc. Pd-1 binding proteins
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
WO2009115572A2 (en) 2008-03-21 2009-09-24 Novartis Ag Novel heterocyclic compounds and uses therof
EP2108641A1 (en) 2008-04-11 2009-10-14 Laboratorios Almirall, S.A. New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
EP2444403A1 (en) 2008-04-18 2012-04-25 Shionogi Co., Ltd. Heterocyclic compound having inhibitory activity on PI3K
WO2009152027A1 (en) 2008-06-12 2009-12-17 Merck & Co., Inc. 5,7-dihydro-6h-pyrrolo[2,3-d]pyrimidin-6-one derivatives for mark inhibition
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
MX357627B (es) 2008-06-27 2018-07-17 Avila Therapeutics Inc Compuestos de heteroarilo y usos de los mismos.
NZ590283A (en) 2008-07-14 2012-11-30 Gilead Sciences Inc Imidazolylpyrimidine compounds as hdac and / or cdk inhibitors
CN102105459B (zh) 2008-07-24 2014-09-10 内尔维阿诺医学科学有限公司 作为蛋白激酶抑制剂的3,4-二芳基吡唑类
AU2009288399B2 (en) 2008-08-25 2013-03-07 Novartis Ag Hedgehog pathway modulators
WO2010033495A2 (en) 2008-09-16 2010-03-25 Schering Corporation Functionally selective azanitrile alpha2c adrenoreceptor agonists
SI2342226T1 (sl) 2008-09-26 2016-11-30 Dana-Farber Cancer Institute Inc. Humana protitelesa proti PD-1, PD-L1 in PD-L2 in njihove uporabe
US8653097B2 (en) 2008-10-17 2014-02-18 Boehringer Ingelheim International Gmbh Tetra-aza-heterocycles as phosphatidylinositol-3-kinases (P13-kinases) inhibitor
WO2010046780A2 (en) 2008-10-22 2010-04-29 Institut Pasteur Korea Anti viral compounds
TW201022267A (en) 2008-10-23 2010-06-16 Gruenenthal Gmbh Substituierte pyrimidin-und triazin-derivate
UY32203A (es) 2008-10-29 2010-05-31 Astrazeneca Ab Amino pirimidinas y su uso en terapia
CN106336400A (zh) 2008-12-08 2017-01-18 萌蒂制药国际有限公司 酪氨酸激酶蛋白受体拮抗剂
PT2376535T (pt) 2008-12-09 2017-06-23 Hoffmann La Roche Anticorpos anti-pd-l1 e a sua utilização para a melhoria do funcionamento das células t
JO2885B1 (en) 2008-12-22 2015-03-15 ايلي ليلي اند كومباني Protein kinase inhibitors
CN101759683B (zh) 2008-12-25 2011-12-28 哈尔滨誉衡药业股份有限公司 二氢化茚酰胺化合物制备方法、包含其的药物组合物、及其作为蛋白激酶抑制剂的应用
US8394951B2 (en) 2009-01-15 2013-03-12 Rigel Pharmaceuticals Inc. Protein kinase C inhibitors and uses thereof
DK2384327T3 (da) 2009-01-30 2013-10-28 Takeda Pharmaceutical Forbindelse med kondenseret ring og anvendelse deraf.
JP5844159B2 (ja) 2009-02-09 2016-01-13 ユニヴェルシテ デクス−マルセイユＵｎｉｖｅｒｓｉｔｅ Ｄ’Ａｉｘ−Ｍａｒｓｅｉｌｌｅ Ｐｄ−１抗体およびｐｄ−ｌ１抗体ならびにその使用
WO2010116270A1 (en) 2009-04-10 2010-10-14 Pfizer Inc. Ep2/4 agonists
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
WO2010144416A1 (en) 2009-06-08 2010-12-16 Gaeta Federico C A SUBSTITUTED PYRAZOLO [1,5-a] PYRIDINE COMPOUNDS HAVING MULTI-TARGET ACTIVITY
EP2487175A1 (en) 2009-10-06 2012-08-15 Kyowa Hakko Kirin Co., Ltd. Pharmaceutical product containing aromatic heterocyclic compound
EP2308866A1 (de) 2009-10-09 2011-04-13 Bayer CropScience AG Phenylpyri(mi)dinylpyrazole und ihre Verwendung als Fungizide
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
JP2013512251A (ja) 2009-11-24 2013-04-11 アンプリミューン、インコーポレーテッド Ｐｄ−ｌ１／ｐｄ−ｌ２の同時阻害
CA2784830C (en) 2009-12-18 2018-03-27 Sunovion Pharmaceuticals Inc. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
BR112012018358A2 (pt) 2009-12-21 2016-08-09 Bayer Cropscience Ag tienilpiri(mi)dinilazol e seu uso para controlar fungos fitopatogênicos
US20130022629A1 (en) 2010-01-04 2013-01-24 Sharpe Arlene H Modulators of Immunoinhibitory Receptor PD-1, and Methods of Use Thereof
WO2011092293A2 (en) 2010-02-01 2011-08-04 Novartis Ag Cyclohexyl amide derivatives as crf receptor antagonists
US8486967B2 (en) 2010-02-17 2013-07-16 Hoffmann-La Roche Inc. Heteroaryl substituted piperidines
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
ES2689177T3 (es) 2010-04-13 2018-11-08 Novartis Ag Combinación que comprende un inhibidor de cinasa 4 dependiente de ciclina o cinasa dependiente de ciclina (CDK4/6) y un inhibidor de mTOR para tratar cáncer
CN102946881A (zh) 2010-04-23 2013-02-27 奇尼塔公司 抗病毒化合物
JP2013147428A (ja) 2010-04-27 2013-08-01 Dainippon Sumitomo Pharma Co Ltd 新規２−ヘテロアリール単環ピリミジン誘導体
WO2011141848A1 (en) 2010-05-11 2011-11-17 Pfizer Inc. Morpholine compounds as mineralocorticoid receptor antagonists
WO2011143495A1 (en) 2010-05-13 2011-11-17 Amgen Inc. Heteroaryloxyheterocyclyl compounds as pde10 inhibitors
JP2013532153A (ja) 2010-06-18 2013-08-15 ザ ブリガム アンド ウィメンズ ホスピタル インコーポレイテッド 慢性免疫病に対する免疫治療のためのｔｉｍ−３およびｐｄ−１に対する二重特異性抗体
US8907053B2 (en) 2010-06-25 2014-12-09 Aurigene Discovery Technologies Limited Immunosuppression modulating compounds
US8735386B2 (en) 2010-07-23 2014-05-27 Boehringer Ingelheim International Gmbh Aminopyrazoloquinazolines
CN103153980B (zh) 2010-08-03 2015-12-16 内尔维安诺医学科学有限公司 吡唑并苯基苯磺酰胺化合物的衍生物及其作为抗肿瘤药的用途
CN106967074A (zh) 2010-10-25 2017-07-21 G1治疗公司 Cdk抑制剂
EP2638018A1 (en) 2010-11-09 2013-09-18 Cellzome Limited Pyridine compounds and aza analogues thereof as tyk2 inhibitors
WO2012082580A2 (en) 2010-12-17 2012-06-21 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
HUE030364T2 (hu) 2011-02-08 2017-04-28 Pfizer Glukagonreceptor modulátora
TWI532742B (zh) 2011-02-28 2016-05-11 艾伯維有限公司 激酶之三環抑制劑
CA2830516C (en) 2011-03-23 2017-01-24 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3
AR085530A1 (es) 2011-03-25 2013-10-09 Abbott Lab Antagonistas del receptor transitorio potencial de vanilloides 1 (trpv1)
WO2012175513A1 (en) 2011-06-20 2012-12-27 Bayer Intellectual Property Gmbh Thienylpyri(mi)dinylpyrazole
US9073935B2 (en) 2011-11-11 2015-07-07 Vanderbilt University Substituted benzylspiroindolin-2-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1
US20130123281A1 (en) 2011-11-11 2013-05-16 Beta Cat Pharmaceuticals, Llc Compositions and Methods for Inhibition of TBL-1 Binding to Disease-Associated Molecules
US8697888B2 (en) 2012-01-06 2014-04-15 Vanderbilt University Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
EP2807166B1 (en) 2012-01-23 2016-04-06 Boehringer Ingelheim International GmbH 5,8-dihydro-6h-pyrazolo[3,4-h]quinazolines as igf-1r/ir inhibitors
RU2548363C2 (ru) 2012-01-25 2015-04-20 Общество с ограниченной ответственностью "Асинэкс Медхим." СЕЛЕКТИВНЫЕ ИНГИБИТОРЫ Haspin киназы
SG11201404898RA (en) 2012-02-17 2014-09-26 Siga Technologies Inc Antiviral drugs for treatment of arenavirus infection
TW201348231A (zh) 2012-02-29 2013-12-01 Amgen Inc 雜雙環化合物
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
US9096579B2 (en) 2012-04-20 2015-08-04 Boehringer Ingelheim International Gmbh Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments
EP2846803B1 (en) 2012-05-08 2017-06-21 Alpharmagen, LLC Alpha 7 nicotinic acetylcholine receptor allosteric modulators, their derivatives and uses thereof
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
RU2509770C2 (ru) 2012-06-22 2014-03-20 Общество с ограниченной ответственностью "Молекулярные Технологии" Новые химические соединения производные 2,4-диамино-1,3,5-триазина для профилактики и лечения заболеваний человека и животных
WO2014020043A1 (en) 2012-08-02 2014-02-06 Bayer Pharma Aktiengesellschaft Combinations for the treatment of cancer
WO2014028669A1 (en) 2012-08-15 2014-02-20 Biogen Idec Ma Inc. Novel compounds for modulation of ror-gamma activity
WO2014031928A2 (en) 2012-08-24 2014-02-27 Philip Jones Heterocyclic modulators of hif activity for treatment of disease
WO2014040555A1 (zh) 2012-09-12 2014-03-20 山东亨利医药科技有限责任公司 作为酪氨酸激酶抑制剂的含氮杂芳环衍生物
HUE033476T2 (en) 2012-10-16 2017-12-28 Janssen Sciences Ireland Uc Anti-RSV Antibodies
CA2891926A1 (en) 2012-11-20 2014-05-30 Merial, Inc. Anthelmintic compounds and compositions and method of using thereof
CN103864770B (zh) 2012-12-10 2019-06-11 江苏先声药业有限公司 作为Hedgehog信号传导的嘧啶胺类和吡啶胺类抑制剂
CN104968664A (zh) 2012-12-12 2015-10-07 山东亨利医药科技有限责任公司 作为酪氨酸激酶抑制剂的并环化合物
WO2014109858A1 (en) 2013-01-14 2014-07-17 Amgen Inc. Methods of using cell-cycle inhibitors to modulate one or more properties of a cell culture
EP3010908A1 (en) 2013-02-20 2016-04-27 E. I. du Pont de Nemours and Company Fungicidal pyrazoles
US20140357636A1 (en) 2013-02-21 2014-12-04 Wayne Rothbaum Treatment of Skeletal-Related Disorders
KR20150114566A (ko) 2013-03-05 2015-10-12 에프. 호프만-라 로슈 아게 항바이러스 화합물
WO2014155300A2 (en) 2013-03-28 2014-10-02 Aurigene Discovery Technologies Limited Substitued pyrimidine amine derivatives as tak-1 inhibitors
EP3004097B1 (en) 2013-06-06 2018-01-17 Chiesi Farmaceutici S.p.A. Kinase inhibitors
CN105308039B (zh) 2013-06-19 2019-06-28 豪夫迈·罗氏有限公司 吲哚满-2-酮或吡咯并-吡啶/嘧啶-2-酮衍生物
ES2661437T3 (es) 2013-06-21 2018-04-02 Zenith Epigenetics Corp. Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio
WO2015006875A1 (en) 2013-07-18 2015-01-22 Methylgene Inc. Process for the preparation of substituted pyrimidines
CN104418860B (zh) 2013-08-20 2016-09-07 中国科学院广州生物医药与健康研究院 嘧啶并杂环类化合物及其药用组合物和应用
CN105683166B (zh) 2013-08-30 2020-06-16 Ptc医疗公司 取代的嘧啶Bmi-1抑制剂
WO2015038417A1 (en) 2013-09-10 2015-03-19 Asana Biosciences, Llc Compounds for regulating fak and/or src pathways
WO2015047124A1 (ru) 2013-09-26 2015-04-02 Общество с ограниченной ответственностью "Молекулярные Технологии" Новые химические соединения производные 2,4-диамино-1,3,5-триазина для профилактики и лечения заболеваний человека и животных
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3057954A2 (en) 2013-10-18 2016-08-24 Syros Pharmaceuticals, Inc. Heteromaromatic compounds useful for the treatment of proliferative diseases
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
RS59140B1 (sr) 2013-10-21 2019-09-30 Merck Patent Gmbh Heteroarilna jedinjenja kao inhibitori btk i njihova upotreba
GB201321732D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
GB201321738D0 (en) 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic Agents
US11013743B2 (en) 2013-12-20 2021-05-25 Biomed Valley Discoveries, Inc. Cancer treatments using combinations of CDK and ERK inhibitors
CN104761544B (zh) 2014-01-03 2019-03-15 北京轩义医药科技有限公司 Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
CA2935944A1 (en) 2014-01-09 2015-07-16 The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone Substituted benzoxazine and related compounds
LT3126352T (lt) 2014-04-04 2019-01-10 Syros Pharmaceuticals, Inc. Nuo ciklino priklausomos kinazės 7 (cdk7) inhibitoriai
WO2015157556A1 (en) 2014-04-09 2015-10-15 Kadmon Corporation, Llc Treatment of gvhd
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
JP6188179B2 (ja) 2014-05-09 2017-08-30 ピメラ， インコーポレイテッド 新規組成物、使用およびそれを作製する方法
CN104003988A (zh) 2014-06-05 2014-08-27 中国药科大学 基于3-氨基-β-咔啉及其衍生物的CDK2激酶抑制剂及其制备方法和用途
CN105315259B (zh) 2014-07-29 2018-03-09 上海艾力斯医药科技有限公司 吡啶胺基嘧啶衍生物、其制备方法及应用
JP2017527604A (ja) 2014-09-17 2017-09-21 アイアンウッド ファーマシューティカルズ インコーポレイテッド ｓＧＣ刺激剤
CA2963640A1 (en) 2014-10-06 2016-04-14 Flatley Discovery Lab, Llc Triazolopyridine compounds and methods for the treatment of cystic fibrosis
US10308648B2 (en) 2014-10-16 2019-06-04 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CN104447743B (zh) 2014-11-26 2016-03-02 苏州明锐医药科技有限公司 帕博西尼的制备方法
JP2017537914A (ja) 2014-12-02 2017-12-21 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 有害生物防除剤としての二環式化合物
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
KR101864426B1 (ko) 2015-03-27 2018-06-05 영진약품 주식회사 1,2 나프토퀴논 유도체 및 이의 제조방법
CN106795149B (zh) 2015-05-05 2019-09-24 上海海雁医药科技有限公司 双环取代的苯磺酰胺衍生物、其制法与医药上的用途
EP3294742B1 (en) 2015-05-13 2020-01-08 Boehringer Ingelheim International GmbH New (5,8-dimethyl-9-phenyl-5,8-dihydro-6h-pyrazolo[3,4-h)quinazolin-2-yl)-(1h-pyrazol-5-yl)-amines and theri derivatives as igf-1r/1r inhibitors.
GB201509893D0 (en) 2015-06-08 2015-07-22 Ucb Biopharma Sprl Therapeutic agents
WO2017007658A1 (en) 2015-07-07 2017-01-12 Rigel Pharmaceuticals, Inc. A combination for immune mediated cancer treatment
CN106699785A (zh) 2015-07-13 2017-05-24 南开大学 作为CDK4/6抑制剂的2-(N-氧化吡啶-2基氨基)-吡啶并[2,3-d]嘧啶-7-酮类化合物
PL3328419T3 (pl) 2015-07-30 2021-12-27 Macrogenics, Inc. Cząsteczki wiążące pd-1 i sposoby ich zastosowania
JP7083309B2 (ja) 2015-08-04 2022-06-10 イッサム リサーチ ディベロップメント カンパニー オブ ザ ヘブリュー ユニバーシティ オブ エルサレム エルティーディー． ピラゾールピリミジン誘導体及びその使用
GB201514489D0 (en) 2015-08-14 2015-09-30 Bergen Teknologioverføring As Hyperphenylalaninemia
WO2017044889A1 (en) 2015-09-10 2017-03-16 The Regents Of The University Of California Lrh-1 modulators
TW201718581A (zh) 2015-10-19 2017-06-01 英塞特公司 作為免疫調節劑之雜環化合物
US10851082B2 (en) 2015-10-28 2020-12-01 Northwestern University Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (MNK1) and 2 (MNK2)
WO2017075367A1 (en) 2015-10-28 2017-05-04 Northwestern University Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2)
DK3377488T3 (da) 2015-11-19 2022-10-03 Incyte Corp Heterocykliske forbindelser som immunomodulatorer
WO2017087905A1 (en) 2015-11-20 2017-05-26 Denali Therapeutics Inc. Compound, compositions, and methods
TW201726623A (zh) 2015-12-17 2017-08-01 英塞特公司 作為免疫調節劑之雜環化合物
ES2844374T3 (es) 2015-12-22 2021-07-22 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
WO2017110863A1 (ja) 2015-12-25 2017-06-29 住友化学株式会社 オキサジアゾール化合物及びその用途
JP6990657B2 (ja) 2016-02-08 2022-01-13 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト Ｄｄｒ１阻害剤としてのスピロインドリノン
IL261606B (en) 2016-03-16 2022-09-01 Kura Oncology Inc Substituted inhibitors of menin-mll and methods of use
GB201605126D0 (en) 2016-03-24 2016-05-11 Univ Nottingham Inhibitors and their uses
EP3442959A1 (en) 2016-04-12 2019-02-20 Esteve Pharmaceuticals, S.A. Piperidinylalkylamide derivatives having multimodal activity against pain
US10577360B2 (en) 2016-04-12 2020-03-03 Esteve Pharmaceuticals, S.A. Arylamide derivatives having multimodal activity against pain
WO2017181177A1 (en) 2016-04-15 2017-10-19 Epizyme, Inc. Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors
TW201808950A (zh) 2016-05-06 2018-03-16 英塞特公司 作為免疫調節劑之雜環化合物
EP3458604B1 (en) 2016-05-18 2021-04-14 Université Libre de Bruxelles Method for determining sensitivity to a cdk4/6 inhibitor
ES2905980T3 (es) 2016-05-26 2022-04-12 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
PE20190731A1 (es) 2016-06-20 2019-05-23 Incyte Corp Compuestos heterociclicos como inmunomoduladores
CN109789143A (zh) 2016-07-01 2019-05-21 G1治疗公司 基于嘧啶的抗增殖剂
SG11201900328WA (en) 2016-07-13 2019-02-27 Jason Marineau Inhibitors of cyclin-dependent kinase 7 (cdk7)
ES2930092T3 (es) 2016-07-14 2022-12-07 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
WO2018033815A1 (en) 2016-08-15 2018-02-22 Pfizer Inc. Pyridopyrimdinone cdk2/4/6 inhibitors
CN107759587B (zh) 2016-08-19 2021-01-26 中国医药研究开发中心有限公司 [1,2,4]三唑并[1,5-a]吡啶类化合物及其制备方法和医药用途
US20180057486A1 (en) 2016-08-29 2018-03-01 Incyte Corporation Heterocyclic compounds as immunomodulators
CN107793413B (zh) 2016-09-05 2021-09-28 上海科州药物研发有限公司 嘧啶杂环化合物及其制备方法和应用
CN107840846B (zh) 2016-09-19 2020-11-24 郑州泰基鸿诺医药股份有限公司 一种含嘧啶环的化合物、egfr抑制剂及其应用
US20190255042A1 (en) 2016-11-04 2019-08-22 Impact Therapeutics, Inc Application of hedgehog pathway inhibitor in treating fibrosis diseases
JP6905069B2 (ja) 2016-11-11 2021-07-21 上海海雁醫藥科技有限公司 ピリジルアミノ置換へテロ三環式化合物並びにその製造方法及び医薬用途
IL295660A (en) 2016-12-22 2022-10-01 Incyte Corp Benzooxazole derivatives as immunomodulators
WO2018119263A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds derivatives as pd-l1 internalization inducers
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
MD3558990T2 (ro) 2016-12-22 2023-02-28 Incyte Corp Derivați tetrahidro imidazo[4,5-c]piridină ca inductori de internalizare a PD-L1
EP3558963B1 (en) 2016-12-22 2022-03-23 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
US20180179179A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
AU2017382360B2 (en) 2016-12-23 2022-07-28 Aquinnah Pharmaceuticals, Inc. Compounds, compositions and methods of use
WO2018124001A1 (ja) 2016-12-27 2018-07-05 国立研究開発法人理化学研究所 Ｂｍｐシグナル阻害化合物
US11111245B2 (en) 2017-02-01 2021-09-07 Aucentra Therapeutics Pty Ltd Derivatives of N-cycloalkyl/heterocycloalkyl-4-(imidazo[1,2-a]pyridine)pyrimidin-2-amine as therapeutic agents
BR112019017741A2 (pt) 2017-02-28 2020-04-07 Dana Farber Cancer Inst Inc usos de pirimidopirimidinonas como inibidores de sik
US20200113901A1 (en) 2017-03-31 2020-04-16 Epizyme, Inc. Methods of using ehmt2 inhibitors
CN109803972B (zh) 2017-04-01 2021-11-23 晟科药业（江苏）有限公司 1h-咪唑[4,5-h]喹唑啉类化合物作为蛋白激酶抑制剂
US11672800B2 (en) 2017-04-21 2023-06-13 Epizyme, Inc. Combination therapies with EHMT2 inhibitors
WO2018226976A1 (en) 2017-06-08 2018-12-13 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with mll proteins
EA202090955A1 (ru) 2017-10-18 2020-11-27 Эпизайм, Инк. Способы применения ингибиторов ehmt2 в лечении или предупреждении нарушений со стороны крови
JP2021500326A (ja) 2017-10-18 2021-01-07 エピザイム，インコーポレイティド 血液障害の予防又は処置にｅｈｍｔ２阻害剤を使用する方法
FI3774791T3 (fi) 2018-03-30 2023-03-21 Incyte Corp Heterosyklisiä yhdisteitä immunomodulaattoreina
WO2019200214A1 (en) 2018-04-13 2019-10-17 The Regents Of The University Of Michigan Compositions and methods for treating cancer
EP3784664B1 (en) 2018-04-26 2025-02-19 Pfizer Inc. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors
CN112752756B (zh) 2018-05-11 2024-06-25 因赛特公司 作为PD-L1免疫调节剂的四氢-咪唑并[4,5-c]吡啶衍生物
JP2021527714A (ja) 2018-06-20 2021-10-14 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ 抗ｐｄ−１抗体及びその使用
JP2021529740A (ja) 2018-06-29 2021-11-04 キネート バイオファーマ インク． サイクリン依存性キナーゼの阻害剤
EP3847159A2 (en) 2018-09-04 2021-07-14 Magenta Therapeutics, Inc. Aryl hydrocarbon receptor antagonists and methods of use
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US20230065740A1 (en) 2018-12-28 2023-03-02 Spv Therapeutics Inc. Cyclin-dependent kinase inhibitors
EA202192260A1 (ru) 2019-02-15 2021-12-17 Инсайт Корпорейшн Биомаркеры циклин-зависимой киназы 2 и их применение
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
CA3157681A1 (en) 2019-10-11 2021-04-15 Incyte Corporation Bicyclic amines as cdk2 inhibitors

Also Published As

Publication number Publication date
TW202115024A (zh) 2021-04-16
PH12022550361A1 (en) 2023-02-27
EP4013750A1 (en) 2022-06-22
US11427567B2 (en) 2022-08-30
CN116348458A (zh) 2023-06-27
US20210047294A1 (en) 2021-02-18
MX2022001940A (es) 2022-05-10
BR112022002698A2 (pt) 2022-07-19
JP2023509260A (ja) 2023-03-08
CO2022001453A2 (es) 2022-05-31
US20230024173A1 (en) 2023-01-26
WO2021030537A1 (en) 2021-02-18
AR119765A1 (es) 2022-01-12
IL290527A (en) 2022-04-01
CA3150681A1 (en) 2021-02-18
CL2022000339A1 (es) 2022-10-28
KR20220064369A (ko) 2022-05-18
ECSP22011692A (es) 2022-05-31
PE20221010A1 (es) 2022-06-15
AU2020328025A1 (en) 2022-03-03

Similar Documents

Publication Publication Date Title
CO2022001453A2 (es) Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2
CO2022004595A2 (es) Aminas bicíclicas como inhibidoras de la cdk2
CL2019000941A1 (es) Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret.
CO2019000386A2 (es) Compuestos heterocíclicos como inmunomoduladores
CO2018007528A2 (es) Compuestos heterocíclicos como inmunomoduladores
NI201900070A (es) Compuestos heterocíclicos como inmunomoduladores
CO2019013010A2 (es) Inhibidores de kras g12c y métodos para su uso
UY37870A (es) Inhibidores de kras g12c y métodos para utilizarlos campo de la invención
MX2023008031A (es) Inhibidores de la cinasa 2 de control general no desrepresible (gcn2) y usos de los mismos.
MX2020014245A (es) Inhibidores de quinasas dependientes de ciclinas.
BR112018070163A2 (pt) compostos de aminopurina substituída, composições e métodos de tratamento
CO2023010023A2 (es) Inhibidores de cdk2 y métodos de uso de los mismos
CL2019001330A1 (es) Inhibidores de la tirosina quinasa de bruton.
CL2021001198A1 (es) Compuestos heteroaromáticos como inhibidores de vanina
MX2022005256A (es) Inhibidores de cd73.
CL2021000292A1 (es) Benzimidazoles sustituidos como inhibidores de pad4.
MX2024007360A (es) Composiciones que comprenden compuestos de bisfluoroalquil-1,4-ben zodiacepinona y metodos de uso de las mismas.
MX2021009426A (es) Derivados de indazolil-isoxazol para el tratamiento de enfermedades tales como cancer.
CL2019002583A1 (es) Inhibidores duales de magl y faah.
CO2024009144A2 (es) Inhibidores de cinasa met
CL2022003206A1 (es) Compuestos derivados de quinolona y su uso para el tratamiento del cáncer (div. sol. 202102501)
CR20190028A (es) Compuestos heterocíclicos como inmunomoduladores
BR112017021114A8 (pt) Compostos heterocíclicos como inibidores de lsd1