HRP20161381T1 - Inhibitori iap - Google Patents
Inhibitori iap Download PDFInfo
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- HRP20161381T1 HRP20161381T1 HRP20161381TT HRP20161381T HRP20161381T1 HR P20161381 T1 HRP20161381 T1 HR P20161381T1 HR P20161381T T HRP20161381T T HR P20161381TT HR P20161381 T HRP20161381 T HR P20161381T HR P20161381 T1 HRP20161381 T1 HR P20161381T1
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- Prior art keywords
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- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 22
- 238000000034 method Methods 0.000 claims 17
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 4
- 230000001640 apoptogenic effect Effects 0.000 claims 4
- 238000000338 in vitro Methods 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 claims 2
- 108010076667 Caspases Proteins 0.000 claims 2
- 102000011727 Caspases Human genes 0.000 claims 2
- NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 2
- 230000006907 apoptotic process Effects 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 230000001939 inductive effect Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 230000001235 sensitizing effect Effects 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- NNJPGOLRFBJNIW-HNNXBMFYSA-N (-)-demecolcine Chemical compound C1=C(OC)C(=O)C=C2[C@@H](NC)CCC3=CC(OC)=C(OC)C(OC)=C3C2=C1 NNJPGOLRFBJNIW-HNNXBMFYSA-N 0.000 claims 1
- LFIPKBDLYATZMF-UBHSHLNASA-N (2s)-1-[(2s)-2-cyclohexyl-2-[[(2s)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidine-2-carboxylic acid Chemical group C1([C@H](NC(=O)[C@H](C)NC)C(=O)N2[C@@H](CCC2)C(O)=O)CCCCC1 LFIPKBDLYATZMF-UBHSHLNASA-N 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- GABDXHKNDJOYMX-UHFFFAOYSA-N 2-(1,3-oxazol-2-yl)-4-phenyl-1,3-thiazol-5-amine Chemical compound NC=1SC(C=2OC=CN=2)=NC=1C1=CC=CC=C1 GABDXHKNDJOYMX-UHFFFAOYSA-N 0.000 claims 1
- 108010006654 Bleomycin Proteins 0.000 claims 1
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims 1
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims 1
- NNJPGOLRFBJNIW-UHFFFAOYSA-N Demecolcine Natural products C1=C(OC)C(=O)C=C2C(NC)CCC3=CC(OC)=C(OC)C(OC)=C3C2=C1 NNJPGOLRFBJNIW-UHFFFAOYSA-N 0.000 claims 1
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims 1
- 229940009456 adriamycin Drugs 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 229960001561 bleomycin Drugs 0.000 claims 1
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims 1
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 1
- 229940127093 camptothecin Drugs 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 229960001338 colchicine Drugs 0.000 claims 1
- 229960004397 cyclophosphamide Drugs 0.000 claims 1
- 229960000684 cytarabine Drugs 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- DBEPLOCGEIEOCV-WSBQPABSSA-N finasteride Chemical compound N([C@@H]1CC2)C(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)NC(C)(C)C)[C@@]2(C)CC1 DBEPLOCGEIEOCV-WSBQPABSSA-N 0.000 claims 1
- 229960004039 finasteride Drugs 0.000 claims 1
- ODKNJVUHOIMIIZ-RRKCRQDMSA-N floxuridine Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(F)=C1 ODKNJVUHOIMIIZ-RRKCRQDMSA-N 0.000 claims 1
- 229960000390 fludarabine Drugs 0.000 claims 1
- GIUYCYHIANZCFB-FJFJXFQQSA-N fludarabine phosphate Chemical compound C1=NC=2C(N)=NC(F)=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@@H]1O GIUYCYHIANZCFB-FJFJXFQQSA-N 0.000 claims 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- 229960004857 mitomycin Drugs 0.000 claims 1
- KKZJGLLVHKMTCM-UHFFFAOYSA-N mitoxantrone Chemical compound O=C1C2=C(O)C=CC(O)=C2C(=O)C2=C1C(NCCNCCO)=CC=C2NCCNCCO KKZJGLLVHKMTCM-UHFFFAOYSA-N 0.000 claims 1
- 229960001156 mitoxantrone Drugs 0.000 claims 1
- 230000002018 overexpression Effects 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 229960001603 tamoxifen Drugs 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- 229960000303 topotecan Drugs 0.000 claims 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 1
- 229960003048 vinblastine Drugs 0.000 claims 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
- 229960004528 vincristine Drugs 0.000 claims 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims 1
Classifications
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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
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- 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
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- 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
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- 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
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- 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
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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
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- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Thiazole And Isothizaole Compounds (AREA)
Claims (18)
1. Spoj formule I
[image]
,
naznačen time što
Ph je fenil;
R1 je C3-7 cikloalkil;
svaki od R2, R3, R4, R5 i R6 je neovisno u svakom slučaju H ili C1-6 alkil; ili
njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (2-oksazol-2-il-4-feniltiazol-5-il)amid (S)-1-[(S)-2-cikloheksil-2-((S)-2-metilaminopropionilamino)acetil]pirolidin-2-karboksilne kiseline (Ia), ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je svaki od R2-R6 neovisno H ili metil.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je R1 cikloheksil.
5. Spoj u skladu s patentnim zahtjevom 3, naznačen time što je R1 cikloheksil.
6. Spoj u skladu s patentnim zahtjevom 3, naznačen time što je jedan od R2 i R3 H, a drugi je metil; ili je R4 metil; ili je svaki od R5 i R6 H.
7. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je namijenjen upotrebi u postupku inhibiranja vezanja proteina IAP na protein kaspazu, gdje se navedeni postupak sastoji u stavljanju u kontakt navedenog proteina IAP s navedenim spojem u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2.
8. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je namijenjen upotrebi u postupku inhibiranja vezanja proteina IAP na protein kaspazu u skladu s patentnim zahtjevom 7, naznačen time što je navedeni postupak postupak in vitro.
9. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je namijenjen upotrebi u postupku liječenja bolesti ili stanja povezanog s prekomjernom ekspresijom IAP kod sisavca.
10. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je namijenjen upotrebi u postupku izazivanja apoptoze u stanici, gdje se navedeni postupak sastoji u uvođenju navedenog spoja u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2 u navedenu stanicu.
11. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, namijenjen upotrebi u postupku izazivanja apoptoze u stanici u skladu s patentnim zahtjevom 10, naznačen time što je navedeni postupak postupak in vitro.
12. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je namijenjen upotrebi u postupku sensibiliziranja stanice na apoptotski signal, gdje se navedeni postupak sastoji u uvođenju navedenog spoja u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2 u navedenu stanicu.
13. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, namijenjen upotrebi u postupku sensibiliziranja stanice na apoptotski signal u skladu s patentnim zahtjevom 12, naznačen time što je navedeni postupak postupak in vitro.
14. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevima 12 i 13, gdje se navedeni apoptotski signal izaziva stavljanjem navedene stanice u kontakt sa spojem kojeg se bira iz skupine koju čine citarabin, fludarabin, 5-fluor-2′-deoksiuiridin, gemcitabin, metotreksat, bleomicin, cisplatin, ciklofosfamid, adriamicin (doksorubicin), mitoksantron, kamptotecin, topotekan, kolcemid, kolhicin, paklitaksel, vinblastin, vinkristin, tamoksifen, finasterid, docetaksel i mitomicin C.
15. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevima 12 i 13, gdje se navedeni apoptotski signal izaziva stavljanjem navedene stanice u kontakt s Apo2L/TRAIL.
16. Spoj u skladu s patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što je namijenjen upotrebi u postupku liječenja raka.
17. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s patentnim zahtjevom 1, kao i najmanje jednu farmaceutski prihvatljivu podlogu, razrjeđivač ili pomoćnu tvar.
18. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s patentnim zahtjevom 2, kao i najmanje jednu farmaceutski prihvatljivu podlogu, razrjeđivač ili pomoćnu tvar.
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| US201261582760P | 2012-01-03 | 2012-01-03 | |
| EP13733613.7A EP2800749B1 (en) | 2012-01-03 | 2013-01-03 | Inhibitors of iap |
| PCT/US2013/020124 WO2013103703A1 (en) | 2012-01-03 | 2013-01-03 | Inhibitors of iap |
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| HRP20161381T1 true HRP20161381T1 (hr) | 2016-12-02 |
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| HRP20161381TT HRP20161381T1 (hr) | 2012-01-03 | 2016-10-25 | Inhibitori iap |
| HRP20180976TT HRP20180976T1 (hr) | 2012-01-03 | 2018-06-26 | Inhibitori iap |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NO2755614T3 (hr) * | 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 |
| PL3712162T3 (pl) * | 2017-11-13 | 2022-11-14 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | MIMETYKI SMAC STOSOWANE JAKO INHIBITORY lAP I ICH ZASTOSOWANIE |
| US11639354B2 (en) | 2018-07-31 | 2023-05-02 | Fimecs, Inc. | Heterocyclic compound |
| JPWO2021020585A1 (hr) | 2019-07-31 | 2021-02-04 | ||
| MX2022008874A (es) | 2020-01-20 | 2022-08-11 | Astrazeneca Ab | Inhibidores de la tirosina cinasa del receptor del factor de creciminto epidermico para el tratamiento del cancer. |
| WO2023239422A2 (en) | 2021-10-22 | 2023-12-14 | University Of Houston System | Methods and compositions for treating chronic inflammatory injury, metaplasia, dysplasia and cancers of epithelial tissues |
Family Cites Families (8)
| 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 |
| 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 |
| ATE477254T1 (de) * | 2004-12-20 | 2010-08-15 | Genentech Inc | Pyrrolidine als inhibitoren von iap |
| EP2102229B1 (en) | 2006-10-12 | 2014-03-26 | Novartis AG | Pyrrolydine derivatives as iap inhibitors |
| MX2009011783A (es) | 2007-04-30 | 2009-12-04 | Genentech Inc | Inhibidores de iap. |
| NO2755614T3 (hr) | 2012-01-03 | 2018-03-31 | ||
| USD690416S1 (en) | 2012-12-12 | 2013-09-24 | Pharmajet, Inc. | Needle-free syringe |
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2012
- 2012-09-13 NO NO12832667A patent/NO2755614T3/no unknown
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2013
- 2013-01-02 AR ARP130100006A patent/AR089623A1/es not_active Application Discontinuation
- 2013-01-03 BR BR112014016637-4A patent/BR112014016637B1/pt active IP Right Grant
- 2013-01-03 CN CN201380012308.1A patent/CN104159897A/zh active Pending
- 2013-01-03 TW TW102100188A patent/TWI503318B/zh active
- 2013-01-03 KR KR1020157014670A patent/KR101855566B1/ko active IP Right Grant
- 2013-01-03 KR KR1020147021597A patent/KR101553792B1/ko active IP Right Grant
- 2013-01-03 JP JP2014551313A patent/JP5747137B2/ja active Active
- 2013-01-03 MY MYPI2014001966A patent/MY178390A/en unknown
- 2013-01-03 US US13/733,244 patent/US8716236B2/en active Active
- 2013-01-03 PE PE2014001069A patent/PE20142182A1/es active IP Right Grant
- 2013-01-03 NZ NZ627480A patent/NZ627480A/en unknown
- 2013-01-03 SI SI201330343A patent/SI2800749T1/sl unknown
- 2013-01-03 EP EP16189661.8A patent/EP3133073B1/en active Active
- 2013-01-03 DK DK13733613.7T patent/DK2800749T3/en active
- 2013-01-03 CN CN201711212712.XA patent/CN107915728B/zh active Active
- 2013-01-03 KR KR1020187012124A patent/KR101917992B1/ko active IP Right Grant
- 2013-01-03 WO PCT/US2013/020124 patent/WO2013103703A1/en active Application Filing
- 2013-01-03 RS RS20160910A patent/RS55327B1/sr unknown
- 2013-01-03 RU RU2016124658A patent/RU2728789C2/ru active
- 2013-01-03 HU HUE13733613A patent/HUE031305T2/hu unknown
- 2013-01-03 PT PT161896618T patent/PT3133073T/pt unknown
- 2013-01-03 TR TR2018/08088T patent/TR201808088T4/tr unknown
- 2013-01-03 HU HUE16189661A patent/HUE037760T2/hu unknown
- 2013-01-03 ME MEP-2018-161A patent/ME03084B/me unknown
- 2013-01-03 PL PL16189661T patent/PL3133073T3/pl unknown
- 2013-01-03 AU AU2013202780A patent/AU2013202780B2/en active Active
- 2013-01-03 UA UAA201408260A patent/UA114417C2/uk unknown
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- 2013-01-03 DK DK16189661.8T patent/DK3133073T3/en active
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- 2013-01-03 PL PL13733613T patent/PL2800749T3/pl unknown
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- 2014-07-25 ZA ZA2014/05535A patent/ZA201405535B/en unknown
- 2014-07-31 CR CR20140367A patent/CR20140367A/es not_active Application Discontinuation
- 2014-07-31 EC ECIEPI201411792A patent/ECSP14011792A/es unknown
- 2014-08-03 MA MA37254A patent/MA35895B1/fr unknown
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2015
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- 2015-05-11 JP JP2015096425A patent/JP2015199738A/ja active Pending
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2017
- 2017-01-31 US US15/420,817 patent/US20170136084A1/en not_active Abandoned
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2018
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2019
- 2019-04-02 US US16/372,940 patent/US11096982B2/en active Active
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