HRP20110892T1 - Policiklični derivati indazola koji su inhibitori erk - Google Patents
Policiklični derivati indazola koji su inhibitori erk Download PDFInfo
- Publication number
- HRP20110892T1 HRP20110892T1 HR20110892T HRP20110892T HRP20110892T1 HR P20110892 T1 HRP20110892 T1 HR P20110892T1 HR 20110892 T HR20110892 T HR 20110892T HR P20110892 T HRP20110892 T HR P20110892T HR P20110892 T1 HRP20110892 T1 HR P20110892T1
- Authority
- HR
- Croatia
- Prior art keywords
- substituted
- group
- image
- pharmaceutically acceptable
- alkyl
- Prior art date
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- -1 Polycyclic indazole derivatives Chemical class 0.000 title claims 2
- 239000012824 ERK inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 82
- 150000003839 salts Chemical class 0.000 claims abstract 70
- 125000000217 alkyl group Chemical group 0.000 claims abstract 43
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 24
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims abstract 19
- 125000001424 substituent group Chemical group 0.000 claims abstract 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 18
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims abstract 15
- 125000003118 aryl group Chemical group 0.000 claims abstract 13
- 125000005843 halogen group Chemical group 0.000 claims abstract 13
- 125000000547 substituted alkyl group Chemical group 0.000 claims abstract 11
- 125000003342 alkenyl group Chemical group 0.000 claims abstract 9
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims abstract 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims abstract 8
- 125000003107 substituted aryl group Chemical group 0.000 claims abstract 8
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims abstract 4
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims abstract 4
- 125000000304 alkynyl group Chemical group 0.000 claims abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 2
- 239000003814 drug Substances 0.000 claims 75
- 229940079593 drug Drugs 0.000 claims 58
- 238000004519 manufacturing process Methods 0.000 claims 47
- 239000002246 antineoplastic agent Substances 0.000 claims 25
- 229940127089 cytotoxic agent Drugs 0.000 claims 25
- 206010028980 Neoplasm Diseases 0.000 claims 13
- 201000011510 cancer Diseases 0.000 claims 12
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 11
- 239000003112 inhibitor Substances 0.000 claims 10
- 206010006187 Breast cancer Diseases 0.000 claims 9
- 208000026310 Breast neoplasm Diseases 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 6
- 150000003384 small molecules Chemical class 0.000 claims 6
- 206010009944 Colon cancer Diseases 0.000 claims 5
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 5
- 206010033128 Ovarian cancer Diseases 0.000 claims 5
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 5
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 5
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 5
- 230000001419 dependent effect Effects 0.000 claims 5
- 201000005202 lung cancer Diseases 0.000 claims 5
- 208000020816 lung neoplasm Diseases 0.000 claims 5
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 5
- 201000001441 melanoma Diseases 0.000 claims 5
- 201000002528 pancreatic cancer Diseases 0.000 claims 5
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 5
- 201000002510 thyroid cancer Diseases 0.000 claims 5
- 208000003174 Brain Neoplasms Diseases 0.000 claims 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 4
- 125000002877 alkyl aryl group Chemical group 0.000 claims 4
- 239000013059 antihormonal agent Substances 0.000 claims 4
- 229940088597 hormone Drugs 0.000 claims 4
- 239000005556 hormone Substances 0.000 claims 4
- 206010005003 Bladder cancer Diseases 0.000 claims 3
- 208000034578 Multiple myelomas Diseases 0.000 claims 3
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 3
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 3
- 108010073929 Vascular Endothelial Growth Factor A Proteins 0.000 claims 3
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 3
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 3
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 3
- 208000025113 myeloid leukemia Diseases 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 2
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims 2
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 2
- 125000005015 aryl alkynyl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 2
- 125000005312 heteroarylalkynyl group Chemical group 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 2
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 239000000333 selective estrogen receptor modulator Substances 0.000 claims 2
- 229940095743 selective estrogen receptor modulator Drugs 0.000 claims 2
- VBEQCZHXXJYVRD-GACYYNSASA-N uroanthelone Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(C)C)[C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C1=CC=C(O)C=C1 VBEQCZHXXJYVRD-GACYYNSASA-N 0.000 claims 2
- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims 1
- 208000001446 Anaplastic Thyroid Carcinoma Diseases 0.000 claims 1
- 206010002240 Anaplastic thyroid cancer Diseases 0.000 claims 1
- 108010024986 Cyclin-Dependent Kinase 2 Proteins 0.000 claims 1
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 claims 1
- 108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 claims 1
- 102100032857 Cyclin-dependent kinase 1 Human genes 0.000 claims 1
- 101710106279 Cyclin-dependent kinase 1 Proteins 0.000 claims 1
- 102100036239 Cyclin-dependent kinase 2 Human genes 0.000 claims 1
- 102100036252 Cyclin-dependent kinase 4 Human genes 0.000 claims 1
- 102100026804 Cyclin-dependent kinase 6 Human genes 0.000 claims 1
- 102100031480 Dual specificity mitogen-activated protein kinase kinase 1 Human genes 0.000 claims 1
- 101710146526 Dual specificity mitogen-activated protein kinase kinase 1 Proteins 0.000 claims 1
- 102100023266 Dual specificity mitogen-activated protein kinase kinase 2 Human genes 0.000 claims 1
- 101710146529 Dual specificity mitogen-activated protein kinase kinase 2 Proteins 0.000 claims 1
- 102000009024 Epidermal Growth Factor Human genes 0.000 claims 1
- 101800003838 Epidermal growth factor Proteins 0.000 claims 1
- 229940102550 Estrogen receptor antagonist Drugs 0.000 claims 1
- 229940123414 Folate antagonist Drugs 0.000 claims 1
- 108090000723 Insulin-Like Growth Factor I Proteins 0.000 claims 1
- 102000004218 Insulin-Like Growth Factor I Human genes 0.000 claims 1
- 102000048143 Insulin-Like Growth Factor II Human genes 0.000 claims 1
- 108090001117 Insulin-Like Growth Factor II Proteins 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 229940124647 MEK inhibitor Drugs 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 claims 1
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 229940123237 Taxane Drugs 0.000 claims 1
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical group O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
- 229940122803 Vinca alkaloid Drugs 0.000 claims 1
- 229940100198 alkylating agent Drugs 0.000 claims 1
- 239000002168 alkylating agent Substances 0.000 claims 1
- 239000004037 angiogenesis inhibitor Substances 0.000 claims 1
- 229940121369 angiogenesis inhibitor Drugs 0.000 claims 1
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 1
- 230000000259 anti-tumor effect Effects 0.000 claims 1
- 239000003124 biologic agent Substances 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 230000022131 cell cycle Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940116977 epidermal growth factor Drugs 0.000 claims 1
- 229930013356 epothilone Natural products 0.000 claims 1
- HESCAJZNRMSMJG-KKQRBIROSA-N epothilone A Chemical class C/C([C@@H]1C[C@@H]2O[C@@H]2CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 HESCAJZNRMSMJG-KKQRBIROSA-N 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 150000003949 imides Chemical class 0.000 claims 1
- 102000006495 integrins Human genes 0.000 claims 1
- 108010044426 integrins Proteins 0.000 claims 1
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 229910052697 platinum Inorganic materials 0.000 claims 1
- 239000003528 protein farnesyltransferase inhibitor Substances 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 108010077182 raf Kinases Proteins 0.000 claims 1
- 102000009929 raf Kinases Human genes 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 1
- 229960004964 temozolomide Drugs 0.000 claims 1
- 229960003433 thalidomide Drugs 0.000 claims 1
- 208000019179 thyroid gland undifferentiated (anaplastic) carcinoma Diseases 0.000 claims 1
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- 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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US74985605P | 2005-12-13 | 2005-12-13 | |
PCT/US2006/046959 WO2007070398A1 (en) | 2005-12-13 | 2006-12-11 | Polycyclic indazole derivatives that are erk inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20110892T1 true HRP20110892T1 (hr) | 2011-12-31 |
Family
ID=37969564
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20110892T HRP20110892T1 (hr) | 2005-12-13 | 2011-11-30 | Policiklični derivati indazola koji su inhibitori erk |
Country Status (29)
Country | Link |
---|---|
US (1) | US20070191604A1 (ko) |
EP (1) | EP1966151B1 (ko) |
JP (1) | JP4881957B2 (ko) |
KR (1) | KR101417136B1 (ko) |
CN (1) | CN101370784B (ko) |
AR (1) | AR056891A1 (ko) |
AT (1) | ATE527240T1 (ko) |
AU (1) | AU2006326616B2 (ko) |
BR (1) | BRPI0619823B8 (ko) |
CA (1) | CA2633023C (ko) |
CY (1) | CY1112760T1 (ko) |
DK (1) | DK1966151T3 (ko) |
EC (1) | ECSP088550A (ko) |
ES (1) | ES2372976T3 (ko) |
HK (1) | HK1114851A1 (ko) |
HR (1) | HRP20110892T1 (ko) |
IL (1) | IL192034A (ko) |
MY (1) | MY149430A (ko) |
NO (1) | NO341831B1 (ko) |
NZ (1) | NZ569087A (ko) |
PE (2) | PE20100562A1 (ko) |
PL (1) | PL1966151T3 (ko) |
PT (1) | PT1966151E (ko) |
RS (1) | RS51981B (ko) |
RU (1) | RU2442778C9 (ko) |
SI (1) | SI1966151T1 (ko) |
TW (1) | TWI344466B (ko) |
WO (1) | WO2007070398A1 (ko) |
ZA (1) | ZA200805525B (ko) |
Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2013109142A1 (en) | 2012-01-16 | 2013-07-25 | Stichting Het Nederlands Kanker Instituut | Combined pdk and mapk/erk pathway inhibition in neoplasia |
WO2015041533A1 (en) | 2013-09-20 | 2015-03-26 | Stichting Het Nederlands Kanker Instituut | Rock in combination with mapk-pathway |
WO2015041534A1 (en) | 2013-09-20 | 2015-03-26 | Stichting Het Nederlands Kanker Instituut | P90rsk in combination with raf/erk/mek |
WO2015156674A2 (en) | 2014-04-10 | 2015-10-15 | Stichting Het Nederlands Kanker Instituut | Method for treating cancer |
WO2015178770A1 (en) | 2014-05-19 | 2015-11-26 | Stichting Het Nederlands Kanker Instituut | Compositions for cancer treatment |
WO2017058007A1 (en) | 2015-10-01 | 2017-04-06 | Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis | Histone deacetylase inhibitors for the use in the treatment of drug resistant melanoma |
WO2017099591A1 (en) | 2015-12-07 | 2017-06-15 | Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis | Treatment of inhibitor resistant braf-mutant cancers |
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Families Citing this family (41)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8546404B2 (en) | 2005-12-13 | 2013-10-01 | Merck Sharp & Dohme | Compounds that are ERK inhibitors |
EP1984331B1 (en) * | 2006-02-16 | 2010-10-20 | Schering Corporation | Pyrrolidine derivatives as erk inhibitors |
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US9062071B2 (en) | 2011-12-21 | 2015-06-23 | Merck Sharp & Dohme Corp. | Substituted piperidines as HDM2 inhibitors |
ITMI20120135A1 (it) * | 2012-02-02 | 2013-08-03 | Diab Int Ab | Procedimento per la produzione di schiume di pet e schiume di pet ottenute con questo procedimento |
US20150141470A1 (en) | 2012-05-08 | 2015-05-21 | The Broad Institute, Inc. | Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy |
CN103450163B (zh) * | 2012-05-29 | 2017-06-23 | 中国医学科学院药物研究所 | 吲唑类化合物、其制备方法及其药物用途 |
JP6186440B2 (ja) | 2012-09-19 | 2017-08-23 | ノバルティス アーゲー | キナーゼ阻害剤としてのジヒドロピロリジノピリミジン |
JP6280554B2 (ja) * | 2012-09-28 | 2018-02-14 | メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. | Erk阻害剤である新規化合物 |
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WO2016095089A1 (en) * | 2014-12-15 | 2016-06-23 | Merck Sharp & Dohme Corp. | Erk inhibitors |
WO2016095088A1 (en) * | 2014-12-15 | 2016-06-23 | Merck Sharp & Dohme Corp. | Erk inhibitors |
EP3365334B1 (en) | 2015-10-21 | 2024-07-17 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
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CN109890827A (zh) * | 2016-10-05 | 2019-06-14 | 芝诺罗耶尔蒂里程碑有限责任公司 | 螺环化合物 |
GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
US10508113B2 (en) | 2018-03-12 | 2019-12-17 | Abbvie Inc. | Inhibitors of tyrosine kinase 2 mediated signaling |
CN114605329B (zh) * | 2022-03-28 | 2024-01-26 | 河南中医药大学 | 取代的吲唑甲酰胺或取代的氮杂吲唑甲酰胺类flt3抑制剂及其用途 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9213077D0 (en) | 1992-06-19 | 1992-08-05 | Erba Carlo Spa | Polymerbound taxol derivatives |
NZ514583A (en) * | 2000-02-05 | 2004-05-28 | Vertex Pharma | Pyrazole compositions useful as inhibitors of ERK |
US6897231B2 (en) * | 2000-07-31 | 2005-05-24 | Signal Pharmaceuticals, Inc. | Indazole derivatives as JNK inhibitors and compositions and methods related thereto |
MY130778A (en) * | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
PL374946A1 (en) * | 2002-09-05 | 2005-11-14 | Aventis Pharma S.A. | Novel aminoindazole derivatives as medicines and pharmaceutical compositions containing same |
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WO2017058007A1 (en) | 2015-10-01 | 2017-04-06 | Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis | Histone deacetylase inhibitors for the use in the treatment of drug resistant melanoma |
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