CN112585119A - 经取代的吲哚及其使用方法 - Google Patents

经取代的吲哚及其使用方法 Download PDF

Info

Publication number
CN112585119A
CN112585119A CN201980054976.8A CN201980054976A CN112585119A CN 112585119 A CN112585119 A CN 112585119A CN 201980054976 A CN201980054976 A CN 201980054976A CN 112585119 A CN112585119 A CN 112585119A
Authority
CN
China
Prior art keywords
group
alkyl
alkyl group
hydroxy
cycloalkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201980054976.8A
Other languages
English (en)
Chinese (zh)
Inventor
约翰·兰普
约翰·坎贝尔
肯尼思·邓肯
梅根·艾琳·克卢南·弗雷
达伦·马丁·哈维
迈克尔·约翰·芒赤霍夫
迈克尔·托梅纽斯
劳伦斯·艾伦·赖特
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Epizyme Inc
Original Assignee
Epizyme Inc
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 Epizyme Inc filed Critical Epizyme Inc
Publication of CN112585119A publication Critical patent/CN112585119A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/96—Spiro-condensed ring systems
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • C07D487/08—Bridged 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
    • C07D487/10—Spiro-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
    • 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • C07D498/04—Ortho-condensed 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
    • C07D498/02—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
    • C07D498/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10—Spiro-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
    • C12Q1/6876—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
    • 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
    • C12Q2600/106—Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pathology (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Wood Science & Technology (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201980054976.8A 2018-08-14 2019-08-14 经取代的吲哚及其使用方法 Pending CN112585119A (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201862718746P 2018-08-14 2018-08-14
US62/718,746 2018-08-14
US201862773770P 2018-11-30 2018-11-30
US62/773,770 2018-11-30
US201962857120P 2019-06-04 2019-06-04
US62/857,120 2019-06-04
PCT/US2019/046569 WO2020037079A1 (en) 2018-08-14 2019-08-14 Substituted indoles and methods of use thereof

Publications (1)

Publication Number Publication Date
CN112585119A true CN112585119A (zh) 2021-03-30

Family

ID=69525931

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980054976.8A Pending CN112585119A (zh) 2018-08-14 2019-08-14 经取代的吲哚及其使用方法

Country Status (16)

Country Link
US (1) US12116358B2 (https=)
EP (1) EP3837240A4 (https=)
JP (2) JP7627209B2 (https=)
KR (1) KR20210065097A (https=)
CN (1) CN112585119A (https=)
AU (2) AU2019321464B2 (https=)
BR (1) BR112021002633A2 (https=)
CA (1) CA3109214A1 (https=)
CO (1) CO2021003300A2 (https=)
IL (2) IL280709B2 (https=)
MA (1) MA53235A (https=)
MX (2) MX2021001690A (https=)
MY (1) MY207663A (https=)
PH (1) PH12021550296A1 (https=)
SG (1) SG11202101367YA (https=)
WO (1) WO2020037079A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023274251A1 (zh) * 2021-06-29 2023-01-05 深圳开悦生命科技有限公司 一类抑制rna解旋酶dhx33的多环化合物及其应用
WO2024067709A1 (zh) * 2022-09-30 2024-04-04 苏州阿尔脉生物科技有限公司 吡啶酰胺类衍生物、包含其的药物组合物及其医药用途

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN119405809A (zh) 2017-08-14 2025-02-11 Epizyme股份有限公司 通过抑制setd2治疗癌症的方法
MX2021006347A (es) * 2018-11-30 2021-10-13 Epizyme Inc Metodos de tratamiento de cánceres que sobreexpresan whsc1 mediante la inhibición de setd2.
WO2021032935A1 (en) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Enzyme inhibitors
CN115151540A (zh) 2019-12-02 2022-10-04 风暴治疗有限公司 作为mettl3抑制剂的多杂环化合物
IL295654A (en) * 2020-02-19 2022-10-01 Epizyme Inc Setd2 inhibitors and related methods and uses, including combination therapies
KR102682775B1 (ko) * 2020-06-26 2024-07-08 홀로스메딕 주식회사 신규한 화합물의 제조방법
US20240228667A9 (en) * 2021-02-26 2024-07-11 Celgene Corporation Methods for Treating Multiple Myeloma
KR20220148758A (ko) * 2021-04-29 2022-11-07 홀로스메딕 주식회사 신규한 화합물 및 이를 포함하는 암 예방 또는 치료용 약학 조성물
IL308868A (en) * 2021-06-09 2024-01-01 Epizyme Inc Combined treatments with SETD2 inhibitors
WO2023077117A1 (en) * 2021-11-01 2023-05-04 Epizyme, Inc. Crystalline forms of n-((1r,3s)-3-(4-acetylpiperazin-1-yl)cyclohexyl)-4-fluoro-7-methyl-1h-indole-2-carboxamide
CN116794170B (zh) * 2022-03-18 2025-11-14 上海润石医药科技有限公司 一种化合物的生物样品检测方法
WO2024091450A1 (en) * 2022-10-24 2024-05-02 The Regents Of The University Of California Compounds and methods for treating cancer
KR20250095720A (ko) * 2022-10-31 2025-06-26 일라이 릴리 앤드 캄파니 Ahr 효능제
EP4652168A1 (en) * 2023-01-19 2025-11-26 Beone Medicines I GmbH 5-amino-1h-pyrrolo [3, 2-b] pyridine-2-carboxamide derivatives as mta-cooperative inhibitors of prmt5

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL63907A0 (en) 1980-09-24 1981-12-31 Cetus Corp Diagnostic method and antibody probe for use therein
US4582788A (en) 1982-01-22 1986-04-15 Cetus Corporation HLA typing method and cDNA probes used therein
ATE53862T1 (de) 1982-01-22 1990-06-15 Cetus Corp Verfahren zur charakterisierung von hla und die darin benutzten cdns-testmittel.
US4683194A (en) 1984-05-29 1987-07-28 Cetus Corporation Method for detection of polymorphic restriction sites and nucleic acid sequences
US4595766A (en) 1984-10-26 1986-06-17 Ciba-Geigy Corporation Process for the preparation of an indoline carboxylic acid
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
CA1284931C (en) 1986-03-13 1991-06-18 Henry A. Erlich Process for detecting specific nucleotide variations and genetic polymorphisms present in nucleic acids
CA1338457C (en) 1986-08-22 1996-07-16 Henry A. Erlich Purified thermostable enzyme
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
AU2003265382A1 (en) 2002-08-23 2004-03-11 Pharmacia & Upjohn Company Llc Antibacterial benzoic acid derivatives
US20040110802A1 (en) * 2002-08-23 2004-06-10 Atli Thorarensen Antibacterial benzoic acid derivatives
EP1880994A4 (en) 2005-05-11 2010-04-14 Eisai R&D Man Co Ltd INDOLE DERIVED CRYSTAL COMPRISING A PIPERIDINE CYCLE AND PROCESS FOR SYNTHESIZING SAID CRYSTAL
CA2628074C (en) * 2005-10-25 2014-01-14 Shionogi & Co., Ltd. Aminodihydrothiazine derivative
US7838542B2 (en) * 2006-06-29 2010-11-23 Kinex Pharmaceuticals, Llc Bicyclic compositions and methods for modulating a kinase cascade
WO2009158375A1 (en) * 2008-06-25 2009-12-30 Abbott Laboratories Aza-cylic indole- 2 -carboxamides and methods of use thereof
AU2009289649B2 (en) * 2008-09-03 2016-05-05 Biomarin Pharmaceutical Inc. Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors
WO2011011366A2 (en) 2009-07-20 2011-01-27 Constellation Pharmaceuticals Agents for stimulating activity of methyl modifying enzymes and methods of use thereof
AU2010333779A1 (en) * 2009-12-23 2012-07-12 Sanofi Indolyl-piperidinyl benzylamines as beta-tryptase inhibitors
JP2013518560A (ja) 2010-02-03 2013-05-23 オンコセラピー・サイエンス株式会社 がんの治療および診断の標的遺伝子としてのｗｈｓｃ１およびｗｈｓｃ１ｌ１
JP2012107001A (ja) * 2010-10-22 2012-06-07 Shionogi & Co Ltd インドールアミド化合物を含有する医薬
CA2853501A1 (en) 2011-10-27 2013-05-02 Memorial Sloan-Kettering Cancer Center Methyltransferase inhibitors for treating cancer
US9446064B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. Combination therapy for treating cancer
WO2015143424A2 (en) 2014-03-21 2015-09-24 Glaxosmithkline Intellectual Property (No. 2) Limited Methods of treating cancer
US10167257B2 (en) 2014-04-04 2019-01-01 Iomet Pharma Ltd. Indole derivatives for use in medicine
WO2015164482A1 (en) * 2014-04-22 2015-10-29 The Johns Hopkins University Inhibitors of drug-resistant mycobacterium tuberculosis
US9902702B2 (en) * 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
AU2015301746A1 (en) 2014-08-13 2017-02-16 Celgene Corporation Combination therapy for treating cancer
BR112017004612A2 (pt) * 2014-09-10 2018-01-30 Epizyme, Inc. compostos, composição farmacêutica, usos de um composto, e kit
WO2016079321A1 (en) 2014-11-20 2016-05-26 Cemm Forschungszentrum Für Molekulare Medizin Gmbh Antagonists of setdb2 for use in the therapy of infectious diseases
US9717745B2 (en) 2015-03-19 2017-08-01 Zhejiang DTRM Biopharma Co. Ltd. Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases
US20190026440A1 (en) 2015-12-17 2019-01-24 Albert Einstein College Of Medicine, Inc. Nuclear receptor set domain containing protein 2 transition state and uses thereof
CN106317043B (zh) * 2016-08-19 2018-11-02 成都理工大学 一种大麻素受体2激动剂
CN119405809A (zh) 2017-08-14 2025-02-11 Epizyme股份有限公司 通过抑制setd2治疗癌症的方法
MX2021006347A (es) 2018-11-30 2021-10-13 Epizyme Inc Metodos de tratamiento de cánceres que sobreexpresan whsc1 mediante la inhibición de setd2.
IL295654A (en) 2020-02-19 2022-10-01 Epizyme Inc Setd2 inhibitors and related methods and uses, including combination therapies
IL308868A (en) 2021-06-09 2024-01-01 Epizyme Inc Combined treatments with SETD2 inhibitors
WO2023077117A1 (en) 2021-11-01 2023-05-04 Epizyme, Inc. Crystalline forms of n-((1r,3s)-3-(4-acetylpiperazin-1-yl)cyclohexyl)-4-fluoro-7-methyl-1h-indole-2-carboxamide

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023274251A1 (zh) * 2021-06-29 2023-01-05 深圳开悦生命科技有限公司 一类抑制rna解旋酶dhx33的多环化合物及其应用
WO2024067709A1 (zh) * 2022-09-30 2024-04-04 苏州阿尔脉生物科技有限公司 吡啶酰胺类衍生物、包含其的药物组合物及其医药用途

Also Published As

Publication number Publication date
AU2019321464A1 (en) 2021-04-08
CO2021003300A2 (es) 2021-06-21
MX2025006292A (es) 2025-07-01
MA53235A (fr) 2022-04-27
MY207663A (en) 2025-03-11
EP3837240A4 (en) 2022-04-27
IL310632A (en) 2024-04-01
KR20210065097A (ko) 2021-06-03
BR112021002633A2 (pt) 2021-05-04
IL280709A (en) 2021-03-25
JP2021536428A (ja) 2021-12-27
US20230075198A1 (en) 2023-03-09
AU2025204601A1 (en) 2025-07-10
MX2021001690A (es) 2021-07-21
CA3109214A1 (en) 2020-02-20
WO2020037079A1 (en) 2020-02-20
SG11202101367YA (en) 2021-03-30
US12116358B2 (en) 2024-10-15
IL280709B2 (en) 2024-07-01
JP7627209B2 (ja) 2025-02-05
EP3837240A1 (en) 2021-06-23
PH12021550296A1 (en) 2021-10-25
JP2025063306A (ja) 2025-04-15
AU2019321464B2 (en) 2025-03-27
IL280709B1 (en) 2024-03-01

Similar Documents

Publication Publication Date Title
CN112585119A (zh) 经取代的吲哚及其使用方法
CN107922417B (zh) 蝶啶酮衍生物作为egfr抑制剂的应用
CN113490495A (zh) Helios的小分子降解剂及其使用方法
JP2019518776A (ja) Ｅｇｆｒ阻害剤としてのアニリンピリミジン化合物の結晶
CN103930425A (zh) 蝶啶酮衍生物及其作为egfr、blk、flt3抑制剂的应用
CN105315285A (zh) 2,4-二取代7H-吡咯并[2,3-d]嘧啶衍生物、其制法与医药上的用途
WO2020125759A1 (zh) 作为wnt信号通路抑制剂的化合物及其医学应用
CN115380033B (zh) Setd2抑制剂和相关方法和用途，包括组合疗法
US20190375714A1 (en) Quinoline compound, preparation method and medical use therefor
JP2024522184A (ja) Ｓｅｔｄ２阻害剤との併用療法
CN104910140A (zh) 喹唑啉类化合物、其制备方法及应用
TWI443095B (zh) 新穎鹽
CN111349093B (zh) 5,6-双环化合物作为wnt信号通路抑制剂及其医学应用
Yu et al. Design, synthesis and antitumor activity of 4-aminoquinazoline derivatives targeting VEGFR-2 tyrosine kinase
CN108250187B (zh) 吲哚-1-碳酸酯类化合物、其制备方法和应用
CN111247137A (zh) 一种嘧啶类化合物、其制备方法及其医药用途
CN119176770A (zh) Hdac抑制剂、组合物及其用途
CN111116572A (zh) 噁二唑衍生物及其制备方法和用途
JP2024537790A (ja) 癌を処置するための腫瘍形成性ｃｈｄ１ｌの小分子阻害剤
CN116655600B (zh) 一种取代的2-芳氨基嘧啶类化合物、药物组合物及其用途
HK40084091A (en) Setd2 inhibitors and related methods and uses, including combination therapies
JP2025526715A (ja) ピリジノピリミジノン化合物の結晶、その酸塩、その酸塩の結晶及び使用
HK40019956A (en) Pyrimidine compound, preparation method therefor and medical use thereof
HK40081466A (en) Efgr inhibitor, preparation method therefor, and application thereof
WO2021254464A1 (zh) 取代喹唑啉类化合物、其制备方法、药物组合及应用

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination