RU2728789C2 - Ингибиторы iap - Google Patents

Ингибиторы iap Download PDF

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Publication number
RU2728789C2
RU2728789C2 RU2016124658A RU2016124658A RU2728789C2 RU 2728789 C2 RU2728789 C2 RU 2728789C2 RU 2016124658 A RU2016124658 A RU 2016124658A RU 2016124658 A RU2016124658 A RU 2016124658A RU 2728789 C2 RU2728789 C2 RU 2728789C2
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RU
Russia
Prior art keywords
compound
iap
cell
pharmaceutically acceptable
acceptable salt
Prior art date
Application number
RU2016124658A
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English (en)
Russian (ru)
Other versions
RU2016124658A (ru
RU2016124658A3 (OSRAM
Inventor
Фредерик Коэн
Льюис Дж. ГАЗЗАРД
Викки Хсяо-Вей ЦУЙ
Джон А. Флайгер
Original Assignee
Кьюрис, Инк.
Дженентек, Инк.
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Publication of RU2016124658A publication Critical patent/RU2016124658A/ru
Publication of RU2016124658A3 publication Critical patent/RU2016124658A3/ru
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • 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
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal 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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Oncology (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)
RU2016124658A 2012-01-03 2013-01-03 Ингибиторы iap RU2728789C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261582760P 2012-01-03 2012-01-03
US61/582,760 2012-01-03

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
RU2014130171/04A Division RU2593259C2 (ru) 2012-01-03 2013-01-03 Ингибиторы iap

Publications (3)

Publication Number Publication Date
RU2016124658A RU2016124658A (ru) 2018-12-04
RU2016124658A3 RU2016124658A3 (OSRAM) 2019-09-09
RU2728789C2 true RU2728789C2 (ru) 2020-07-31

Family

ID=48695302

Family Applications (2)

Application Number Title Priority Date Filing Date
RU2016124658A RU2728789C2 (ru) 2012-01-03 2013-01-03 Ингибиторы iap
RU2014130171/04A RU2593259C2 (ru) 2012-01-03 2013-01-03 Ингибиторы iap

Family Applications After (1)

Application Number Title Priority Date Filing Date
RU2014130171/04A RU2593259C2 (ru) 2012-01-03 2013-01-03 Ингибиторы iap

Country Status (41)

Country Link
US (6) US8716236B2 (OSRAM)
EP (2) EP3133073B1 (OSRAM)
JP (2) JP5747137B2 (OSRAM)
KR (3) KR101553792B1 (OSRAM)
CN (2) CN104159897A (OSRAM)
AR (2) AR089623A1 (OSRAM)
AU (1) AU2013202780B2 (OSRAM)
BR (1) BR112014016637B1 (OSRAM)
CA (1) CA2861637C (OSRAM)
CL (1) CL2014001770A1 (OSRAM)
CO (1) CO7020915A2 (OSRAM)
CR (1) CR20140367A (OSRAM)
CY (2) CY1118371T1 (OSRAM)
DK (2) DK3133073T3 (OSRAM)
EC (1) ECSP14011792A (OSRAM)
ES (2) ES2594856T3 (OSRAM)
HK (1) HK1203949A1 (OSRAM)
HR (2) HRP20161381T1 (OSRAM)
HU (2) HUE037760T2 (OSRAM)
IL (2) IL242314A (OSRAM)
LT (2) LT2800749T (OSRAM)
MA (1) MA35895B1 (OSRAM)
ME (2) ME02526B (OSRAM)
MX (1) MX336294B (OSRAM)
MY (1) MY178390A (OSRAM)
NO (1) NO2755614T3 (OSRAM)
NZ (1) NZ627480A (OSRAM)
PE (1) PE20142182A1 (OSRAM)
PH (2) PH12014501534B1 (OSRAM)
PL (2) PL2800749T3 (OSRAM)
PT (2) PT3133073T (OSRAM)
RS (2) RS55327B1 (OSRAM)
RU (2) RU2728789C2 (OSRAM)
SG (1) SG11201403784QA (OSRAM)
SI (2) SI2800749T1 (OSRAM)
SM (2) SMT201800352T1 (OSRAM)
TR (1) TR201808088T4 (OSRAM)
TW (1) TWI503318B (OSRAM)
UA (1) UA114417C2 (OSRAM)
WO (1) WO2013103703A1 (OSRAM)
ZA (1) ZA201405535B (OSRAM)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO2755614T3 (OSRAM) 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
IL274598B2 (en) 2017-11-13 2025-01-01 Chia Tai Tianqing Pharmaceutical Group Co Ltd SMAC mimetics used as IAP inhibitors and their use
CN112533898A (zh) 2018-07-31 2021-03-19 日商泛美克斯股份有限公司 杂环化合物
US20220402935A1 (en) 2019-07-31 2022-12-22 Fimecs, Inc. Heterocyclic compound
US20230029259A1 (en) * 2019-12-02 2023-01-26 Ascentage Pharma (Suzhou) Co., Ltd. Combination of iap inhibitors and parp or mek inhibitors or other chemotherapeutic agents
EP4093394A1 (en) 2020-01-20 2022-11-30 Astrazeneca AB Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
AU2022463015A1 (en) 2021-10-22 2024-05-09 Tract Pharmaceuticals, Inc. 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

Citations (4)

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Publication number Priority date Publication date Assignee Title
US20060167066A1 (en) * 2004-12-20 2006-07-27 Genentech, Inc. Pyrrolidine inhibitors of IAP
WO2008045905A1 (en) * 2006-10-12 2008-04-17 Novartis Ag Pyrrolydine derivatives as iap inhibitors
WO2008134679A1 (en) * 2007-04-30 2008-11-06 Genentech, Inc. Inhibitors of iap
RU2401840C2 (ru) * 2004-07-02 2010-10-20 Дженентек, Инк. Ингибиторы iap

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US4526988A (en) 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
DE69830577T2 (de) 1997-04-15 2006-05-04 Genentech, Inc., South San Francisco Halo-alkoxycarbonylverbindungen
NO2755614T3 (OSRAM) * 2012-01-03 2018-03-31
USD690416S1 (en) 2012-12-12 2013-09-24 Pharmajet, Inc. Needle-free syringe

Patent Citations (4)

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Publication number Priority date Publication date Assignee Title
RU2401840C2 (ru) * 2004-07-02 2010-10-20 Дженентек, Инк. Ингибиторы iap
US20060167066A1 (en) * 2004-12-20 2006-07-27 Genentech, Inc. Pyrrolidine inhibitors of IAP
WO2008045905A1 (en) * 2006-10-12 2008-04-17 Novartis Ag Pyrrolydine derivatives as iap inhibitors
WO2008134679A1 (en) * 2007-04-30 2008-11-06 Genentech, Inc. Inhibitors of iap

Also Published As

Publication number Publication date
BR112014016637A2 (pt) 2017-06-13
CL2014001770A1 (es) 2015-04-17
UA114417C2 (uk) 2017-06-12
EP3133073B1 (en) 2018-05-02
EP3133073A3 (en) 2017-03-22
ME03084B (me) 2019-01-20
HK1203949A1 (en) 2015-11-06
EP2800749B1 (en) 2016-09-21
PT2800749T (pt) 2016-10-24
DK2800749T3 (en) 2016-11-07
HUE037760T2 (hu) 2018-09-28
NO2755614T3 (OSRAM) 2018-03-31
ME02526B (me) 2017-02-20
KR101553792B1 (ko) 2015-09-16
KR20180051646A (ko) 2018-05-16
MA35895B1 (fr) 2014-12-01
PH12014501534A1 (en) 2014-10-08
US9586991B2 (en) 2017-03-07
RU2016124658A (ru) 2018-12-04
PE20142182A1 (es) 2015-01-16
CA2861637C (en) 2017-07-18
TR201808088T4 (tr) 2018-06-21
LT3133073T (lt) 2018-06-25
CN104159897A (zh) 2014-11-19
JP5747137B2 (ja) 2015-07-08
RU2593259C2 (ru) 2016-08-10
KR20140107670A (ko) 2014-09-04
PH12015501038B1 (en) 2015-09-21
US11963994B2 (en) 2024-04-23
HRP20180976T1 (hr) 2018-08-10
US20160102119A1 (en) 2016-04-14
EP3133073A2 (en) 2017-02-22
MX2014007895A (es) 2015-03-19
US20170136084A1 (en) 2017-05-18
US20220211797A1 (en) 2022-07-07
JP2015504072A (ja) 2015-02-05
AR089623A1 (es) 2014-09-03
BR112014016637B1 (pt) 2022-06-14
US9238675B2 (en) 2016-01-19
ZA201405535B (en) 2017-08-30
RS55327B1 (sr) 2017-03-31
PL3133073T3 (pl) 2018-09-28
US11096982B2 (en) 2021-08-24
BR112014016637A8 (pt) 2017-07-04
RU2016124658A3 (OSRAM) 2019-09-09
US20190224269A1 (en) 2019-07-25
MY178390A (en) 2020-10-12
NZ627480A (en) 2016-04-29
KR101917992B1 (ko) 2018-11-13
CY1118371T1 (el) 2017-06-28
CY1120355T1 (el) 2019-07-10
CR20140367A (es) 2015-02-18
US8716236B2 (en) 2014-05-06
HRP20161381T1 (hr) 2016-12-02
EP2800749A1 (en) 2014-11-12
MX336294B (es) 2016-01-14
CO7020915A2 (es) 2014-08-11
ES2672809T3 (es) 2018-06-18
CN107915728A (zh) 2018-04-17
CA2861637A1 (en) 2013-07-11
PT3133073T (pt) 2018-06-18
US20140235551A1 (en) 2014-08-21
DK3133073T3 (en) 2018-06-18
SG11201403784QA (en) 2014-08-28
AU2013202780B2 (en) 2015-04-16
US20130172264A1 (en) 2013-07-04
TW201333001A (zh) 2013-08-16
CN107915728B (zh) 2021-04-30
RS57438B1 (sr) 2018-09-28
KR20150065960A (ko) 2015-06-15
KR101855566B1 (ko) 2018-05-04
EP2800749A4 (en) 2015-08-05
SMT201600357B (it) 2016-11-10
SI2800749T1 (sl) 2016-11-30
AR123542A2 (es) 2022-12-14
TWI503318B (zh) 2015-10-11
WO2013103703A1 (en) 2013-07-11
IL242314A (en) 2016-08-31
SMT201800352T1 (it) 2018-09-13
ES2594856T3 (es) 2016-12-23
HUE031305T2 (hu) 2017-07-28
RU2014130171A (ru) 2016-02-27
PL2800749T3 (pl) 2017-01-31
AU2013202780A1 (en) 2013-07-18
IL233386A0 (en) 2014-08-31
JP2015199738A (ja) 2015-11-12
LT2800749T (lt) 2016-10-25
PH12015501038A1 (en) 2015-09-21
IL233386A (en) 2016-08-31
PH12014501534B1 (en) 2014-10-08
ECSP14011792A (es) 2015-12-31
SI3133073T1 (en) 2018-06-29

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