TWI503318B - Iap抑制劑 - Google Patents

Iap抑制劑 Download PDF

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Publication number
TWI503318B
TWI503318B TW102100188A TW102100188A TWI503318B TW I503318 B TWI503318 B TW I503318B TW 102100188 A TW102100188 A TW 102100188A TW 102100188 A TW102100188 A TW 102100188A TW I503318 B TWI503318 B TW I503318B
Authority
TW
Taiwan
Prior art keywords
compound
acid
iap
compounds
cancer
Prior art date
Application number
TW102100188A
Other languages
English (en)
Chinese (zh)
Other versions
TW201333001A (zh
Inventor
Frederick Cohen
Michael Koehler
Lewis J Gazzard
Vickie Hsiao-Wei Tsui
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 TW201333001A publication Critical patent/TW201333001A/zh
Application granted granted Critical
Publication of TWI503318B publication Critical patent/TWI503318B/zh

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Classifications

    • 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

Landscapes

  • 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)
TW102100188A 2012-01-03 2013-01-03 Iap抑制劑 TWI503318B (zh)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
TW201333001A TW201333001A (zh) 2013-08-16
TWI503318B true TWI503318B (zh) 2015-10-11

Family

ID=48695302

Family Applications (1)

Application Number Title Priority Date Filing Date
TW102100188A TWI503318B (zh) 2012-01-03 2013-01-03 Iap抑制劑

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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060014700A1 (en) * 2004-07-02 2006-01-19 Genentech, Inc. Inhibitors of 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

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
NZ598890A (en) 2007-04-30 2013-10-25 Genentech Inc Inhibitors of iap
NO2755614T3 (OSRAM) * 2012-01-03 2018-03-31
USD690416S1 (en) 2012-12-12 2013-09-24 Pharmajet, Inc. Needle-free syringe

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060014700A1 (en) * 2004-07-02 2006-01-19 Genentech, Inc. Inhibitors of 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

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
RU2728789C2 (ru) 2020-07-31
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
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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