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AR123542A2 - Compuesto inhibidor de iap, método in vitro para inhibir la unión de una proteína iap con una proteína caspasa y método in vitro de sensibilización de una célula a una señal de apoptosis - Google Patents

Compuesto inhibidor de iap, método in vitro para inhibir la unión de una proteína iap con una proteína caspasa y método in vitro de sensibilización de una célula a una señal de apoptosis

Info

Publication number
AR123542A2
AR123542A2 ARP210102590A ARP210102590A AR123542A2 AR 123542 A2 AR123542 A2 AR 123542A2 AR P210102590 A ARP210102590 A AR P210102590A AR P210102590 A ARP210102590 A AR P210102590A AR 123542 A2 AR123542 A2 AR 123542A2
Authority
AR
Argentina
Prior art keywords
protein
cell
vitro method
iap
sensitizing
Prior art date
Application number
ARP210102590A
Other languages
English (en)
Original Assignee
Genentech 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 Genentech Inc filed Critical Genentech Inc
Publication of AR123542A2 publication Critical patent/AR123542A2/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/4211,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0815Tripeptides with the first amino acid being basic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
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  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Compuesto que es (2-oxazol-2-il-4-fenil-tiazol-5-il)-amida del ácido (S)-1-[(S)-2-ciclohexil-2-((S)-2-metilamino-propionilamino)-acetil]-pirrolidin-2-carboxílico de fórmula (1) o una de sus sales farmacéuticamente aceptables. Método para inhibir la unión de una proteína IAP con una proteína caspasa que comprende poner en contacto, in vitro, dicha proteína IAP con dicho compuesto. Método de sensibilización de una célula a una señal de apoptosis que comprende introducir en dicha célula, in vitro, un compuesto de acuerdo con la reivindicación 1. Dicha señal apoptótica es inducida al poner en contacto dicha célula, in vitro, con un compuesto seleccionado del grupo que consiste en citarabina, fludarabina, 5-fluoro-2’-desoxiuiridina, gemcitabina, metotrexato, bleomicina, cisplatino, ciclofosfamida, adriamicina (doxorrubicina), mitoxantrona, camptotecina, topotecano, colcemida, colchicina, paclitaxel, vinblastina, vincristina, tamoxifeno, finasteride, docetaxel y mitomicina C.
ARP210102590A 2012-01-03 2021-09-17 Compuesto inhibidor de iap, método in vitro para inhibir la unión de una proteína iap con una proteína caspasa y método in vitro de sensibilización de una célula a una señal de apoptosis AR123542A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261582760P 2012-01-03 2012-01-03

Publications (1)

Publication Number Publication Date
AR123542A2 true AR123542A2 (es) 2022-12-14

Family

ID=48695302

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP130100006A AR089623A1 (es) 2012-01-03 2013-01-02 Inhibidores de iap
ARP210102590A AR123542A2 (es) 2012-01-03 2021-09-17 Compuesto inhibidor de iap, método in vitro para inhibir la unión de una proteína iap con una proteína caspasa y método in vitro de sensibilización de una célula a una señal de apoptosis

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP130100006A AR089623A1 (es) 2012-01-03 2013-01-02 Inhibidores de iap

Country Status (41)

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US (6) US8716236B2 (es)
EP (2) EP2800749B1 (es)
JP (2) JP5747137B2 (es)
KR (3) KR101917992B1 (es)
CN (2) CN104159897A (es)
AR (2) AR089623A1 (es)
AU (1) AU2013202780B2 (es)
BR (1) BR112014016637B1 (es)
CA (1) CA2861637C (es)
CL (1) CL2014001770A1 (es)
CO (1) CO7020915A2 (es)
CR (1) CR20140367A (es)
CY (2) CY1118371T1 (es)
DK (2) DK2800749T3 (es)
EC (1) ECSP14011792A (es)
ES (2) ES2594856T3 (es)
HK (1) HK1203949A1 (es)
HR (2) HRP20161381T1 (es)
HU (2) HUE031305T2 (es)
IL (2) IL242314A (es)
LT (2) LT3133073T (es)
MA (1) MA35895B1 (es)
ME (2) ME03084B (es)
MX (1) MX336294B (es)
MY (1) MY178390A (es)
NO (1) NO2755614T3 (es)
NZ (1) NZ627480A (es)
PE (1) PE20142182A1 (es)
PH (2) PH12014501534A1 (es)
PL (2) PL2800749T3 (es)
PT (2) PT3133073T (es)
RS (2) RS57438B1 (es)
RU (2) RU2593259C2 (es)
SG (1) SG11201403784QA (es)
SI (2) SI3133073T1 (es)
SM (2) SMT201800352T1 (es)
TR (1) TR201808088T4 (es)
TW (1) TWI503318B (es)
UA (1) UA114417C2 (es)
WO (1) WO2013103703A1 (es)
ZA (1) ZA201405535B (es)

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Publication number Priority date Publication date Assignee Title
NO2755614T3 (es) 2012-01-03 2018-03-31
WO2016079527A1 (en) 2014-11-19 2016-05-26 Tetralogic Birinapant Uk Ltd Combination therapy
WO2016097773A1 (en) 2014-12-19 2016-06-23 Children's Cancer Institute Therapeutic iap antagonists for treating proliferative disorders
CN109705191B (zh) * 2017-10-25 2022-04-29 广东东阳光药业有限公司 Iap抑制剂及其在药物中的应用
SG11202004377XA (en) 2017-11-13 2020-06-29 Chia Tai Tianqing Pharmaceutical Group Co Ltd Smac mimetics used as iap inhibitors and use thereof
JP7515175B2 (ja) 2018-07-31 2024-07-12 ファイメクス株式会社 複素環化合物
EP4006037A4 (en) 2019-07-31 2023-12-13 Fimecs, Inc. HETEROCYCLIC COMPOUND
WO2021110011A1 (en) * 2019-12-02 2021-06-10 Ascentage Pharma (Suzhou) Co., Ltd. Combination of iap inhibitors and parp or mek inhibitors or other chemotherapeutic agents
JP2023510426A (ja) 2020-01-20 2023-03-13 アストラゼネカ・アクチエボラーグ 癌を治療するための上皮細胞増殖因子受容体チロシンキナーゼ阻害剤
EP4419104A2 (en) 2021-10-22 2024-08-28 University of Houston System Methods and compositions for treating chronic inflammatory injury, metaplasia, dysplasia and cancers of epithelial tissues
CN117110469B (zh) * 2023-08-18 2025-12-09 中国检验检疫科学研究院 一种测定防脱发类化妆品中禁用组分的方法

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US4526988A (en) 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
ATE297904T1 (de) 1997-04-15 2005-07-15 Genentech Inc Halo-alkoxycarbonylverbindungen
SI1778718T1 (sl) * 2004-07-02 2015-01-30 Genentech, Inc. Inhibitorji IAP
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CA2666112A1 (en) 2006-10-12 2008-04-17 Novartis Ag Pyrrolydine derivatives as iap inhibitors
CA2683392A1 (en) 2007-04-30 2008-11-06 Genentech, Inc. Inhibitors of iap
NO2755614T3 (es) * 2012-01-03 2018-03-31
USD690416S1 (en) 2012-12-12 2013-09-24 Pharmajet, Inc. Needle-free syringe

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Publication number Publication date
US9238675B2 (en) 2016-01-19
EP3133073B1 (en) 2018-05-02
NZ627480A (en) 2016-04-29
ZA201405535B (en) 2017-08-30
RU2014130171A (ru) 2016-02-27
RU2728789C2 (ru) 2020-07-31
CR20140367A (es) 2015-02-18
TW201333001A (zh) 2013-08-16
CN107915728A (zh) 2018-04-17
DK3133073T3 (en) 2018-06-18
JP2015199738A (ja) 2015-11-12
EP2800749A1 (en) 2014-11-12
PL2800749T3 (pl) 2017-01-31
LT3133073T (lt) 2018-06-25
LT2800749T (lt) 2016-10-25
RS57438B1 (sr) 2018-09-28
JP2015504072A (ja) 2015-02-05
BR112014016637A2 (pt) 2017-06-13
RU2593259C2 (ru) 2016-08-10
UA114417C2 (uk) 2017-06-12
KR20150065960A (ko) 2015-06-15
IL233386A0 (en) 2014-08-31
CA2861637A1 (en) 2013-07-11
JP5747137B2 (ja) 2015-07-08
PT3133073T (pt) 2018-06-18
US20140235551A1 (en) 2014-08-21
PL3133073T3 (pl) 2018-09-28
EP3133073A2 (en) 2017-02-22
WO2013103703A1 (en) 2013-07-11
RU2016124658A (ru) 2018-12-04
HUE031305T2 (hu) 2017-07-28
CN107915728B (zh) 2021-04-30
RU2016124658A3 (es) 2019-09-09
ES2594856T3 (es) 2016-12-23
MX2014007895A (es) 2015-03-19
SI3133073T1 (en) 2018-06-29
IL242314A (en) 2016-08-31
HK1203949A1 (en) 2015-11-06
EP2800749A4 (en) 2015-08-05
PH12015501038A1 (en) 2015-09-21
NO2755614T3 (es) 2018-03-31
CO7020915A2 (es) 2014-08-11
RS55327B1 (sr) 2017-03-31
SG11201403784QA (en) 2014-08-28
PE20142182A1 (es) 2015-01-16
PH12015501038B1 (en) 2015-09-21
PH12014501534B1 (en) 2014-10-08
SI2800749T1 (sl) 2016-11-30
AU2013202780B2 (en) 2015-04-16
CL2014001770A1 (es) 2015-04-17
PT2800749T (pt) 2016-10-24
KR20180051646A (ko) 2018-05-16
HRP20180976T1 (hr) 2018-08-10
IL233386A (en) 2016-08-31
ES2672809T3 (es) 2018-06-18
TR201808088T4 (tr) 2018-06-21
US20160102119A1 (en) 2016-04-14
MA35895B1 (fr) 2014-12-01
EP3133073A3 (en) 2017-03-22
SMT201800352T1 (it) 2018-09-13
ME02526B (me) 2017-02-20
US11963994B2 (en) 2024-04-23
MY178390A (en) 2020-10-12
US8716236B2 (en) 2014-05-06
AR089623A1 (es) 2014-09-03
KR101855566B1 (ko) 2018-05-04
HUE037760T2 (hu) 2018-09-28
US20130172264A1 (en) 2013-07-04
PH12014501534A1 (en) 2014-10-08
EP2800749B1 (en) 2016-09-21
CY1118371T1 (el) 2017-06-28
CY1120355T1 (el) 2019-07-10
HRP20161381T1 (hr) 2016-12-02
ECSP14011792A (es) 2015-12-31
ME03084B (me) 2019-01-20
US20190224269A1 (en) 2019-07-25
US11096982B2 (en) 2021-08-24
US20220211797A1 (en) 2022-07-07
AU2013202780A1 (en) 2013-07-18
CN104159897A (zh) 2014-11-19
KR101553792B1 (ko) 2015-09-16
DK2800749T3 (en) 2016-11-07
US20170136084A1 (en) 2017-05-18
BR112014016637A8 (pt) 2017-07-04
KR101917992B1 (ko) 2018-11-13
KR20140107670A (ko) 2014-09-04
CA2861637C (en) 2017-07-18
MX336294B (es) 2016-01-14
SMT201600357B (it) 2016-11-10
TWI503318B (zh) 2015-10-11
BR112014016637B1 (pt) 2022-06-14
US9586991B2 (en) 2017-03-07

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