CN110719906B - Bcl-2相关死亡促进因子(BAD)磷酸化的小分子抑制剂 - Google Patents

Bcl-2相关死亡促进因子(BAD)磷酸化的小分子抑制剂 Download PDF

Info

Publication number
CN110719906B
CN110719906B CN201880026001.XA CN201880026001A CN110719906B CN 110719906 B CN110719906 B CN 110719906B CN 201880026001 A CN201880026001 A CN 201880026001A CN 110719906 B CN110719906 B CN 110719906B
Authority
CN
China
Prior art keywords
methyl
piperazin
dichlorophenyl
aryl
heteroaryl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201880026001.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN110719906A (zh
Inventor
彼得·爱德华·罗别
维贾伊·库马·潘迪
兰加帕·坎楚加拉科帕尔苏贝戈达
巴萨帕·萨隆地
莫汉·查克拉巴维达南贾亚
肖比思·兰加帕
斯里尼瓦萨·文卡塔恰拉亚
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.)
BANGALORE UNIVERSITY
University of Mysore
National University of Singapore
Original Assignee
BANGALORE UNIVERSITY
University of Mysore
National University of Singapore
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 BANGALORE UNIVERSITY, University of Mysore, National University of Singapore filed Critical BANGALORE UNIVERSITY
Publication of CN110719906A publication Critical patent/CN110719906A/zh
Application granted granted Critical
Publication of CN110719906B publication Critical patent/CN110719906B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
    • C07D213/53—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D471/06—Peri-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Furan Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Management, Administration, Business Operations System, And Electronic Commerce (AREA)
  • Professional, Industrial, Or Sporting Protective Garments (AREA)
CN201880026001.XA 2017-04-19 2018-04-18 Bcl-2相关死亡促进因子(BAD)磷酸化的小分子抑制剂 Active CN110719906B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1706162.3 2017-04-19
GBGB1706162.3A GB201706162D0 (en) 2017-04-19 2017-04-19 Compounds
PCT/SG2018/050194 WO2018194520A1 (en) 2017-04-19 2018-04-18 Small molecule inhibitors of bcl-2-associated death promoter (bad) phosphorylation

Publications (2)

Publication Number Publication Date
CN110719906A CN110719906A (zh) 2020-01-21
CN110719906B true CN110719906B (zh) 2023-07-28

Family

ID=58744515

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880026001.XA Active CN110719906B (zh) 2017-04-19 2018-04-18 Bcl-2相关死亡促进因子(BAD)磷酸化的小分子抑制剂

Country Status (12)

Country Link
US (1) US11292773B2 (https=)
EP (1) EP3612518A4 (https=)
JP (1) JP7423010B2 (https=)
KR (1) KR102753110B1 (https=)
CN (1) CN110719906B (https=)
AU (1) AU2018256285B2 (https=)
CA (1) CA3060939A1 (https=)
GB (1) GB201706162D0 (https=)
IL (1) IL270078B (https=)
MX (1) MX2024000001A (https=)
SG (1) SG11201909418WA (https=)
WO (1) WO2018194520A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201706162D0 (en) * 2017-04-19 2017-05-31 Nat Univ Singapore Compounds
CN112481298A (zh) * 2020-11-11 2021-03-12 清华-伯克利深圳学院筹备办公室 重组质粒及其应用
CN115340527B (zh) * 2021-05-13 2023-09-15 成都先导药物开发股份有限公司 一种bcl-xl抑制剂及其制备方法和用途

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001007050A1 (en) * 1999-07-26 2001-02-01 Schering Corporation Nociceptin receptor orl-1 agonists for use in treating cough
CN101939005A (zh) * 2007-12-14 2011-01-05 诺瓦提斯公司 作为癌症治疗剂的驱动蛋白抑制剂

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU4513699A (en) * 1998-06-25 2000-01-10 Ciba Specialty Chemicals Holding Inc. Process for the preparation of 3-aryl-benzofuranones
DE10348044A1 (de) * 2003-10-15 2005-05-19 Imtm Gmbh Duale Alanyl-Aminopeptidase- und Dipeptidylpeptidase IV-Inhibitoren zur funktionellen Beeinflussung unterschiedlicher Zellen und zur Behandlung immunologischer, entzündlicher, neuronaler und anderer Erkrankungen
WO2010052448A2 (en) * 2008-11-05 2010-05-14 Ucb Pharma S.A. Fused pyrazine derivatives as kinase inhibitors
US8916705B2 (en) * 2011-10-14 2014-12-23 The Board of Trustees of The University of Illilnois Procaspase-activating compounds and compositions
JP2017128541A (ja) * 2016-01-21 2017-07-27 学校法人東京女子医科大学 アポトーシス誘導剤
GB201706162D0 (en) * 2017-04-19 2017-05-31 Nat Univ Singapore Compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001007050A1 (en) * 1999-07-26 2001-02-01 Schering Corporation Nociceptin receptor orl-1 agonists for use in treating cough
CN101939005A (zh) * 2007-12-14 2011-01-05 诺瓦提斯公司 作为癌症治疗剂的驱动蛋白抑制剂

Non-Patent Citations (12)

* Cited by examiner, † Cited by third party
Title
"A green protocol for the one-pot multicomponent Petasis boronic Mannich reaction using ball milling";R. Hosseinzadeh等;《J.IRAN.CHEM.SOC.》;20161004;第14卷(第2期);第347-355页 *
"Amino(hetero)arylmethylation of Phenols with N-[α-Amino(hetero)arylmethyl]benzotriazoles";Alan R. Katritzky等;《J. Org. Chem.》;19990714;第64卷(第16期);第6071-6075页 *
"FeCl3‑Mediated One-Pot Domino Reactions for the Synthesis of 9‑Aryl/9-Arylethynyl-2,3,4,9-tetrahydro‑1H‑xanthen-1-ones from Propargylic Amines/Diaryl Amines and 1,3-Cyclohexanediones";Xinwei He等;《J. Org. Chem.》;20160215;第81卷(第5期);第2062-2069页 *
"Hydroxyquinoline-derived compounds and analoguing of selective Mcl-1 inhibitors using a functional biomarker";David J. Richard等;《Bioorganic & Medicinal Chemistry》;20130815;第21卷(第21期);第6642-6649页 *
"Induction of apoptosis and cell-cycle arrest in human colon cancer cells by meclizine";Jiunn-Chang Lin等;《Food and Chemical Toxicology》;20061209;第45卷(第6期);第935-944页 *
"Short-term Modulation of Cell Proliferation and Apoptosis and Preventive/Therapeutic Efficacy of Various Agents in a Mammary Cancer Model";Konstantin Christov等;《Clin.Cancer Res.》;20070915;第13卷(第18期);第5488-5496页 *
"Sonochemistry – an innovative opportunity towards a one-pot three-component synthesis of novel pyridylpiperazine derivatives catalysed by meglumine in water";S. Tabassum等;《New J. Chem.》;20170101;第41卷(第9期);第3515-3523页 *
"SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF 1-BENZ-HYDRYL PIPERAZINE DERIVATIVES";Atul Kumar Thakran等;《Int. J.Pharm. Sci. Res.》;20120101;第3卷(第1期);第213–217页 *
1088182-85-7;REGISTRY;《ACS on STN》;20081222 *
Jiunn-Chang Lin等."Induction of apoptosis and cell-cycle arrest in human colon cancer cells by meclizine".《Food and Chemical Toxicology》.2006,第45卷(第6期),第935-944页. *
Konstantin Christov等."Short-term Modulation of Cell Proliferation and Apoptosis and Preventive/Therapeutic Efficacy of Various Agents in a Mammary Cancer Model".《Clin.Cancer Res.》.2007,第13卷(第18期),第5488-5496页. *
R. Hosseinzadeh等."A green protocol for the one-pot multicomponent Petasis boronic Mannich reaction using ball milling".《J.IRAN.CHEM.SOC.》.2016,第14卷(第2期),第347-355页. *

Also Published As

Publication number Publication date
WO2018194520A9 (en) 2019-10-17
IL270078B (en) 2022-09-01
US20200131139A1 (en) 2020-04-30
WO2018194520A1 (en) 2018-10-25
JP2020517745A (ja) 2020-06-18
EP3612518A1 (en) 2020-02-26
GB201706162D0 (en) 2017-05-31
JP7423010B2 (ja) 2024-01-29
CA3060939A1 (en) 2018-10-25
US11292773B2 (en) 2022-04-05
CN110719906A (zh) 2020-01-21
MX2024000001A (es) 2024-02-20
KR102753110B1 (ko) 2025-01-09
KR20200029384A (ko) 2020-03-18
AU2018256285B2 (en) 2022-08-04
RU2019135562A (ru) 2021-05-19
SG11201909418WA (en) 2019-11-28
AU2018256285A1 (en) 2019-11-07
IL270078A (https=) 2019-12-31
RU2019135562A3 (https=) 2021-07-21
BR112019022015A2 (pt) 2020-05-12
EP3612518A4 (en) 2020-11-25

Similar Documents

Publication Publication Date Title
CA2868081C (en) Inhibition of mcl-1 and/or bfl-1/a1
TWI693220B (zh) １,３,４-噻二唑化合物及其用於治療癌症之用途
JP2017505787A (ja) 治療薬としてのヒトアンドロゲン受容体ｄｎａ結合ドメイン（ｄｂｄ）化合物およびそれらを使用する方法
Kump et al. Discovery and characterization of 2, 5-substituted benzoic acid dual inhibitors of the anti-apoptotic Mcl-1 and Bfl-1 proteins
CN110719906B (zh) Bcl-2相关死亡促进因子(BAD)磷酸化的小分子抑制剂
AU2017258304B2 (en) 1,5-disubstituted 1,2,3-triazoles are inhibitors of Rac/Cdc42 GTPases
Li et al. Design and biological evaluation of novel triaryl pyrazoline derivatives with dioxane moiety for selective BRAFV600E inhibition
CN110305126A (zh) 一种基于crbn配体诱导cdk4/6降解的化合物及其制备方法、药物组合物和应用
Meduri et al. New LPA1 receptor modulators: Design, synthesis, in-silico, and anticancer studies of triazole and oxadiazole analogs
CN113543852A (zh) 吡咯并吡唑衍生物
RU2799873C9 (ru) Низкомолекулярные ингибиторы фосфорилирования BCL-2-ассоциированного промотора смерти (BAD)
RU2799873C2 (ru) Низкомолекулярные ингибиторы фосфорилированные BCL-2-ассоциированного промотора смерти (BAD)
EP3568391B1 (en) Benzene disulfonamide for the treatment of cancer
Sang et al. Design, synthesis, biological evaluation and molecular docking of novel metronidazole derivatives as selective and potent JAK3 inhibitors
WO2024117980A1 (en) Compounds for modulating src family kinases and uses thereof
BR112019022015B1 (pt) Inibidores de moléculas pequenas de fosforilação de promotor de morte associado a bcl-2 (bad)
CN111247137A (zh) 一种嘧啶类化合物、其制备方法及其医药用途
WO2018160967A1 (en) Indolinone derivatives as inhibitors of maternal embryonic leucine zipper kinase
JP6853833B2 (ja) エストロゲン受容体調節物質の組合せ
CA2963601A1 (en) Benzylhydroxyde derivatives, preparation thereof and therapeutic use as inhibitors of the complex 1 of the mitochondrial respiratory chain

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