DK2800749T3 - Iap-hæmmere - Google Patents
Iap-hæmmere Download PDFInfo
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- DK2800749T3 DK2800749T3 DK13733613.7T DK13733613T DK2800749T3 DK 2800749 T3 DK2800749 T3 DK 2800749T3 DK 13733613 T DK13733613 T DK 13733613T DK 2800749 T3 DK2800749 T3 DK 2800749T3
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- DK
- Denmark
- Prior art keywords
- compound
- cell
- pharmaceutically acceptable
- acid
- compound according
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- IARSSOVWSJAVSZ-UHFFFAOYSA-N tris(dimethylamino)sulfanium Chemical compound CN(C)[S+](N(C)C)N(C)C IARSSOVWSJAVSZ-UHFFFAOYSA-N 0.000 description 1
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- 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
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- 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
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- 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
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- 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
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A61K31/425—Thiazoles
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- A—HUMAN NECESSITIES
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- 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
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Claims (18)
1. Forbindelse med formlen I hvor
Ph er phenyl; R1 er C3-7-cycloalkyl; R2, R3, R4, R5 og R6 hver, uafhængigt for hver forekomst, er H eller C-i-6-alkyl; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, som er (S)-1-[(S)-2-cyclohexyl-2-((S)-2-methylamino-propionylamino)-acetyl]-pyrrolidin-2-carboxylsyre-(2-oxazol-2-yl-4-phenyl-thiazol-5-yl)-amid (la), eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifølge krav 1, hvor R2 til R6 hver uafhængigt er H eller methyl.
4. Forbindelse ifølge krav 1, hvor R1 er cyclohexyl.
5. Forbindelse ifølge krav 3, hvor R1 er cyclohexyl.
6. Forbindelse ifølge krav 3, hvor det ene af R2 og R3 er H, og det andet er methyl; eller R4 er methyl; eller R5 og R6 hver er H.
7. Forbindelse ifølge krav 1 eller krav 2 til anvendelse ved en fremgangsmåde til hæmning af bindingen af et ΙΑΡ-protein til et caspaseprotein, hvor fremgangsmåden omfatter at etablere kontakt mellem ΙΑΡ-proteinet og forbindelsen ifølge krav 1 eller krav 2.
8. Forbindelse ifølge krav 1 eller krav 2 til anvendelse ved en fremgangsmåde til hæmning af bindingen af et ΙΑΡ-protein til et caspaseprotein ifølge krav 7, kendetegnet ved, at fremgangsmåden er en in v/Yro-fremgangsmåde.
9. Forbindelse ifølge krav 1 eller krav 2 til anvendelse ved en fremgangsmåde til behandling af en sygdom eller tilstand, som er forbundet med overekspression af en IAP hos et pattedyr.
10. Forbindelse ifølge krav 1 eller krav 2 til anvendelse ved en fremgangsmåde til induktion af apoptose i en celle, hvor fremgangsmåden omfatter at indføre forbindelsen ifølge krav 1 eller krav 2 i cellen.
11. Forbindelse ifølge krav 1 eller krav 2 til anvendelse ved en fremgangsmåde til induktion af apoptose i en celle ifølge krav 10, kendetegnet ved, at fremgangsmåden er en in v/fro-fremgangsmåde.
12. Forbindelse ifølge krav 1 eller krav 2 til anvendelse ved en fremgangsmåde til sensibilisering af en celle over for et apoptotisk signal, hvor fremgangsmåden omfatter at indføre forbindelsen ifølge krav 1 eller krav 2 i cellen.
13. Forbindelse ifølge krav 1 eller krav 2 til anvendelse ved en fremgangsmåde til sensibilisering af en celle over for et apoptotisk signal ifølge krav 12, kendetegnet ved, at fremgangsmåden er en in v/Yro-fremgangsmåde.
14. Forbindelse ifølge krav 1 eller krav 2 til anvendelsen ifølge krav 12 og 13, hvor det apoptotiske signal induceres ved at etablere kontakt mellem cellen og en forbindelse valgt fra gruppen bestående af cytarabin, fludarabin, 5-fluor-2'-deoxyuridin, gemcitabin, methotrexat, bleomycin, cisplatin, cyclophosphamid, adriamycin (doxorubicin), mitoxantron, camptothecin, topotecan, colcemid, colchicin, paclitaxel, vinblastin, vineristin, tamoxifen, finasterid, docetaxel og mitomycin C.
15. Forbindelse ifølge krav 1 eller krav 2 til anvendelsen ifølge krav 12 og 13, hvor det apoptotiske signal induceres ved at etablere kontakt mellem cellen og Apo2L/TRAIL.
16. Forbindelse ifølge krav 1 eller krav 2 til anvendelse ved en fremgangsmåde til behandling af cancer.
17. Farmaceutisk sammensætning, som omfatter forbindelsen ifølge krav 1 og mindst én farmaceutisk acceptabel bærer, mindst ét farmaceutisk acceptabelt fortyndingsmiddel, eller mindst én farmaceutisk acceptabel excipiens.
18. Farmaceutisk sammensætning, som omfatter forbindelsen ifølge krav 2 og mindst én farmaceutisk acceptabel bærer, mindst ét farmaceutisk acceptabelt fortyndingsmiddel, eller mindst én farmaceutisk acceptabel excipiens.
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US201261582760P | 2012-01-03 | 2012-01-03 | |
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NO2755614T3 (da) * | 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 |
EP3712162B1 (en) | 2017-11-13 | 2022-08-24 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Smac mimetics used as iap inhibitors and use thereof |
EP3831811A4 (en) | 2018-07-31 | 2022-04-20 | Fimecs, Inc. | HETEROCYCLIC COMPOUND |
WO2021020585A1 (ja) | 2019-07-31 | 2021-02-04 | ファイメクス株式会社 | 複素環化合物 |
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 |
US20230056604A1 (en) | 2020-01-20 | 2023-02-23 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
US20230233691A1 (en) | 2021-10-22 | 2023-07-27 | University Of Houston System | Methods and compositions for treating chronic inflammatory injury, metaplasia, dysplasia and cancers of epithelial tissues |
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US4526988A (en) | 1983-03-10 | 1985-07-02 | Eli Lilly And Company | Difluoro antivirals and intermediate therefor |
EP0975608B1 (en) | 1997-04-15 | 2005-06-15 | Genentech, Inc. | Halo-alkoxycarbonyl prodrugs |
KR100984459B1 (ko) * | 2004-07-02 | 2010-09-29 | 제넨테크, 인크. | Iap의 억제제 |
JP5007235B2 (ja) * | 2004-12-20 | 2012-08-22 | ジェネンテック, インコーポレイテッド | Iapのピロリジンインヒビター |
KR20090065548A (ko) | 2006-10-12 | 2009-06-22 | 노파르티스 아게 | Iap 억제제로서의 피롤리딘 유도체 |
US8907092B2 (en) * | 2007-04-30 | 2014-12-09 | Genentech, Inc. | Inhibitors of IAP |
NO2755614T3 (da) | 2012-01-03 | 2018-03-31 | ||
USD690416S1 (en) | 2012-12-12 | 2013-09-24 | Pharmajet, Inc. | Needle-free syringe |
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