CN111886219A - 免疫抑制剂及其制备方法和在药学上的应用 - Google Patents

免疫抑制剂及其制备方法和在药学上的应用 Download PDF

Info

Publication number
CN111886219A
CN111886219A CN201980020074.2A CN201980020074A CN111886219A CN 111886219 A CN111886219 A CN 111886219A CN 201980020074 A CN201980020074 A CN 201980020074A CN 111886219 A CN111886219 A CN 111886219A
Authority
CN
China
Prior art keywords
deuterium
substituted
radical
membered
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.)
Granted
Application number
CN201980020074.2A
Other languages
English (en)
Other versions
CN111886219B (zh
Inventor
张鸣鸣
张永贤
喻红平
陈椎
徐耀昌
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.)
Abbisko Therapeutics Co Ltd
Original Assignee
Abbisko Therapeutics Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Abbisko Therapeutics Co Ltd filed Critical Abbisko Therapeutics Co Ltd
Publication of CN111886219A publication Critical patent/CN111886219A/zh
Application granted granted Critical
Publication of CN111886219B publication Critical patent/CN111886219B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C15/00Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts
    • C07C15/40Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts substituted by unsaturated carbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C15/00Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts
    • C07C15/40Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts substituted by unsaturated carbon radicals
    • C07C15/42Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts substituted by unsaturated carbon radicals monocyclic
    • C07C15/44Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic parts substituted by unsaturated carbon radicals monocyclic the hydrocarbon substituent containing a carbon-to-carbon double bond
    • C07C15/46Styrene; Ring-alkylated styrenes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/26Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C07C211/27Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/26Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C07C211/29Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/10Heterocyclic 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 carbon chain containing aromatic rings
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

一种式(Ⅰ)结构免疫抑制剂及其制备方法和在药学上的应用。系列化合物具有对PD‑1/PD‑L1相互作用有很强的抑制活性,可广泛应用于制备预防和/或治疗由PD‑1/PD‑L1信号通路介导的癌症或肿瘤、免疫相关疾病及紊乱、传染性疾病、感染性疾病或代谢性疾病的药物,有望开发成新一代PD‑1/PD‑L1抑制剂。

Description

PCT国内申请,说明书已公开。

Claims (17)

  1. PCT国内申请,权利要求书已公开。
CN201980020074.2A 2018-07-11 2019-07-10 免疫抑制剂及其制备方法和在药学上的应用 Active CN111886219B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2018107600118 2018-07-11
CN201810760011 2018-07-11
CN201910069224 2019-01-24
CN2019100692240 2019-01-24
PCT/CN2019/095461 WO2020011209A1 (zh) 2018-07-11 2019-07-10 免疫抑制剂及其制备方法和在药学上的应用

Publications (2)

Publication Number Publication Date
CN111886219A true CN111886219A (zh) 2020-11-03
CN111886219B CN111886219B (zh) 2023-04-25

Family

ID=69143179

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980020074.2A Active CN111886219B (zh) 2018-07-11 2019-07-10 免疫抑制剂及其制备方法和在药学上的应用

Country Status (3)

Country Link
CN (1) CN111886219B (zh)
TW (1) TWI798463B (zh)
WO (1) WO2020011209A1 (zh)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113461668A (zh) * 2021-04-30 2021-10-01 西安新通药物研究股份有限公司 一种新型联苯类衍生物及其制备方法与医药用途
CN115232125A (zh) * 2021-05-14 2022-10-25 杭州和正医药有限公司 多取代苯类免疫调节化合物、组合物及其应用
CN115925697A (zh) * 2021-08-24 2023-04-07 昆药集团股份有限公司 一种小分子免疫调节抑制剂及其药物组合和用途

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2017289038B2 (en) 2016-06-27 2021-07-22 Chemocentryx, Inc. Immunomodulator compounds
US11130740B2 (en) 2017-04-25 2021-09-28 Arbutus Biopharma Corporation Substituted 2,3-dihydro-1H-indene analogs and methods using same
CA3070794A1 (en) 2017-07-28 2019-01-31 Chemocentryx, Inc. Immunomodulator compounds
EP3664793B1 (en) 2017-08-08 2022-06-29 ChemoCentryx, Inc. Macrocyclic immunomodulators
WO2019165043A2 (en) 2018-02-22 2019-08-29 Chemocentryx, Inc. Indane-amines as pd-l1 antagonists
CA3093851A1 (en) 2018-03-29 2019-10-03 Arbutus Biopharma Corporation Substituted 1,1'-biphenyl compounds, analogues thereof, and methods using same
JP2022531970A (ja) 2019-05-15 2022-07-12 ケモセントリックス,インコーポレイティド Pd-l1疾患治療用のトリアリール化合物
MA55325A (fr) 2019-06-20 2022-04-27 Chemocentryx Inc Composés pour le traitement de maladies pd-l1
KR20220034829A (ko) 2019-07-10 2022-03-18 케모센트릭스, 인크. Pd-l1 억제제로서의 인단
BR112022006018A2 (pt) 2019-10-16 2022-07-12 Chemocentryx Inc Heteroaril-bifenil amidas para o tratamento de doenças relacionadas à pd-l1
CA3152714A1 (en) 2019-10-16 2021-04-22 Pingchen Fan Heteroaryl-biphenyl amines for the treatment of pd-l1 diseases
EP4089091A4 (en) 2020-01-07 2024-03-20 Abbisko Therapeutics Co., Ltd. DOUBLE BONDED BIPHENYL FLUORINE DERIVATIVE, PREPARATION METHOD THEREOF AND PHARMACEUTICAL USE THEREOF
CA3182595A1 (en) * 2020-06-17 2021-12-23 Mingming Zhang Immunosuppressant, and preparation method therefor and use thereof
CN114075123B (zh) * 2020-08-11 2023-06-06 中国人民解放军军事科学院军事医学研究院 苄胺类衍生物及其制备方法与用途
WO2022257833A1 (zh) * 2021-06-07 2022-12-15 上海海雁医药科技有限公司 取代的苯基丙烯基吡啶类衍生物中间体及其制备方法
CA3240346A1 (en) * 2021-12-16 2023-06-22 Aligos Therapeutics, Inc. Methods and compositions for targeting pd-l1
CN114315787A (zh) * 2021-12-30 2022-04-12 广州佳途科技股份有限公司 一种维兰特罗ep杂质2的制备方法及应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998050030A1 (en) * 1997-05-07 1998-11-12 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
US6358960B1 (en) * 1998-02-17 2002-03-19 Ono Pharmaceutical Co., Ltd. Amidino derivatives and drugs containing the same as the active ingredient
CN101896457A (zh) * 2007-10-22 2010-11-24 幽兰研究实验室有限公司 组蛋白脱乙酰基酶抑制剂
WO2017106634A1 (en) * 2015-12-17 2017-06-22 Incyte Corporation N-phenyl-pyridine-2-carboxamide derivatives and their use as pd-1/pd-l1 protein/protein interaction modulators
CN107573332A (zh) * 2016-07-05 2018-01-12 广州再极医药科技有限公司 芳香乙炔或芳香乙烯类化合物、其中间体、制备方法、药物组合物及应用
WO2018195321A1 (en) * 2017-04-20 2018-10-25 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998050030A1 (en) * 1997-05-07 1998-11-12 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
US6358960B1 (en) * 1998-02-17 2002-03-19 Ono Pharmaceutical Co., Ltd. Amidino derivatives and drugs containing the same as the active ingredient
CN101896457A (zh) * 2007-10-22 2010-11-24 幽兰研究实验室有限公司 组蛋白脱乙酰基酶抑制剂
WO2017106634A1 (en) * 2015-12-17 2017-06-22 Incyte Corporation N-phenyl-pyridine-2-carboxamide derivatives and their use as pd-1/pd-l1 protein/protein interaction modulators
CN107573332A (zh) * 2016-07-05 2018-01-12 广州再极医药科技有限公司 芳香乙炔或芳香乙烯类化合物、其中间体、制备方法、药物组合物及应用
WO2018195321A1 (en) * 2017-04-20 2018-10-25 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113461668A (zh) * 2021-04-30 2021-10-01 西安新通药物研究股份有限公司 一种新型联苯类衍生物及其制备方法与医药用途
CN113461668B (zh) * 2021-04-30 2022-12-09 西安新通药物研究股份有限公司 一种新型联苯类衍生物及其制备方法与医药用途
CN115232125A (zh) * 2021-05-14 2022-10-25 杭州和正医药有限公司 多取代苯类免疫调节化合物、组合物及其应用
CN115925697A (zh) * 2021-08-24 2023-04-07 昆药集团股份有限公司 一种小分子免疫调节抑制剂及其药物组合和用途

Also Published As

Publication number Publication date
TWI798463B (zh) 2023-04-11
WO2020011209A1 (zh) 2020-01-16
TW202019869A (zh) 2020-06-01
CN111886219B (zh) 2023-04-25

Similar Documents

Publication Publication Date Title
CN111886219A (zh) 免疫抑制剂及其制备方法和在药学上的应用
TWI772386B (zh) 雜芳基并[4,3-c]嘧啶-5-胺類衍生物、其製備方法及其在醫藥上的使用
CN108473468B (zh) Ret的抑制剂
TWI718207B (zh) 苯並呋喃類衍生物、其製備方法及其在醫藥上的應用
KR102426043B1 (ko) 액티빈 수용체 유사 키나아제의 저해제
WO2021043077A1 (zh) 一种取代吡嗪化合物、其制备方法和用途
TW202029960A (zh) 新穎吲唑化合物或其鹽
KR20190141215A (ko) N-(아자릴)시클로락탐-1-카르복사미드 유도체 및 합성법과 그 용법
JP2024505732A (ja) ピリドピリミジノン系誘導体及びその製造方法と使用
WO2021185256A1 (zh) 取代的嘧啶或吡啶胺衍生物、其组合物及医药上的用途
WO2020182018A1 (zh) 氮杂环化合物、其制备方法及用途
TW202214639A (zh) 吡啶酮并嘧啶類衍生物、其製備方法及其在醫藥上的應用
CN115605475A (zh) 一种免疫抑制剂、其制备方法和应用
TWI839504B (zh) 吡唑基-氨基-嘧啶基衍生物的苯醚和苯胺及其組合物和方法
WO2020168939A1 (zh) 杂环化合物、包含其的药物组合物及其制备方法和用途
TW202321241A (zh) 嘧啶或吡啶衍生物及其製備方法和在藥學上的應用
CN113173924B (zh) 一种作为cdk抑制剂的吡啶乙酰胺类衍生物、其制备方法及用途
CN115427407A (zh) 一种新型n-杂环bet溴结构域抑制剂、其制备方法及医药用途
CN115340559A (zh) Shp2磷酸酶杂环类抑制剂的制备及其应用
WO2023134753A1 (zh) 微管蛋白-src双靶点抑制剂
WO2023134751A1 (zh) 微管蛋白-Src双靶点抑制剂和用途
CN112601745A (zh) 一种氮杂芳基酰胺衍生物及其制备方法和应用
JP6294561B2 (ja) 多置換ピリジン化合物、調製方法、用途、および医薬組成物
WO2022222911A1 (zh) 嘧啶酮化合物及其用途
JP2024516194A (ja) Pd1/pd-l1阻害剤としての化合物及びその方法

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
GR01 Patent grant
GR01 Patent grant