JP2010529134A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010529134A5 JP2010529134A5 JP2010511276A JP2010511276A JP2010529134A5 JP 2010529134 A5 JP2010529134 A5 JP 2010529134A5 JP 2010511276 A JP2010511276 A JP 2010511276A JP 2010511276 A JP2010511276 A JP 2010511276A JP 2010529134 A5 JP2010529134 A5 JP 2010529134A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- halogen
- nhc
- cancer
- oxo
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 71
- 229910052736 halogen Inorganic materials 0.000 claims description 56
- 150000002367 halogens Chemical class 0.000 claims description 56
- 125000001931 aliphatic group Chemical group 0.000 claims description 42
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 239000001257 hydrogen Substances 0.000 claims description 36
- 229920006395 saturated elastomer Polymers 0.000 claims description 28
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 26
- -1 1-imidazolyl Chemical group 0.000 claims description 24
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 24
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims description 24
- 150000002431 hydrogen Chemical group 0.000 claims description 20
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 19
- 229910052760 oxygen Inorganic materials 0.000 claims description 19
- 239000001301 oxygen Substances 0.000 claims description 19
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 18
- 201000010099 disease Diseases 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 125000005842 heteroatom Chemical group 0.000 claims description 18
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 18
- 229910052717 sulfur Chemical group 0.000 claims description 18
- 239000011593 sulfur Chemical group 0.000 claims description 18
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims description 16
- 238000000034 method Methods 0.000 claims description 15
- 125000003118 aryl group Chemical group 0.000 claims description 14
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims description 12
- 101150065749 Churc1 gene Proteins 0.000 claims description 12
- 206010016654 Fibrosis Diseases 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 12
- 102100038239 Protein Churchill Human genes 0.000 claims description 12
- 125000002950 monocyclic group Chemical group 0.000 claims description 12
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 12
- 125000000217 alkyl group Chemical group 0.000 claims description 10
- 230000000694 effects Effects 0.000 claims description 10
- 239000003112 inhibitor Substances 0.000 claims description 10
- 108010051742 Platelet-Derived Growth Factor beta Receptor Proteins 0.000 claims description 8
- 102100030485 Platelet-derived growth factor receptor alpha Human genes 0.000 claims description 8
- 101710148465 Platelet-derived growth factor receptor alpha Proteins 0.000 claims description 8
- 125000004429 atom Chemical group 0.000 claims description 8
- 125000002619 bicyclic group Chemical group 0.000 claims description 8
- 230000004761 fibrosis Effects 0.000 claims description 8
- 230000002401 inhibitory effect Effects 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- 206010006187 Breast cancer Diseases 0.000 claims description 6
- 208000026310 Breast neoplasm Diseases 0.000 claims description 6
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims description 6
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 6
- 201000010260 leiomyoma Diseases 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 5
- LBUJPTNKIBCYBY-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline Chemical compound C1=CC=C2CCCNC2=C1 LBUJPTNKIBCYBY-UHFFFAOYSA-N 0.000 claims description 4
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 4
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims description 4
- 206010018364 Glomerulonephritis Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 206010069351 acute lung injury Diseases 0.000 claims description 4
- 230000001476 alcoholic effect Effects 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 230000007882 cirrhosis Effects 0.000 claims description 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 4
- 125000004980 cyclopropylene group Chemical group 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 201000008482 osteoarthritis Diseases 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 claims description 4
- 208000005069 pulmonary fibrosis Diseases 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 208000037803 restenosis Diseases 0.000 claims description 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 4
- 231100000241 scar Toxicity 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 3
- 230000002427 irreversible effect Effects 0.000 claims description 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims description 2
- 206010001233 Adenoma benign Diseases 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims description 2
- 201000003076 Angiosarcoma Diseases 0.000 claims description 2
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims description 2
- 200000000007 Arterial disease Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 208000037260 Atherosclerotic Plaque Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims description 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010006895 Cachexia Diseases 0.000 claims description 2
- 201000009030 Carcinoma Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010012442 Dermatitis contact Diseases 0.000 claims description 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 2
- 201000009273 Endometriosis Diseases 0.000 claims description 2
- 102000010834 Extracellular Matrix Proteins Human genes 0.000 claims description 2
- 108010037362 Extracellular Matrix Proteins Proteins 0.000 claims description 2
- 208000007659 Fibroadenoma Diseases 0.000 claims description 2
- 201000008808 Fibrosarcoma Diseases 0.000 claims description 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- 208000001258 Hemangiosarcoma Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 206010055171 Hypertensive nephropathy Diseases 0.000 claims description 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims description 2
- 208000002260 Keloid Diseases 0.000 claims description 2
- 206010023330 Keloid scar Diseases 0.000 claims description 2
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims description 2
- 206010023825 Laryngeal cancer Diseases 0.000 claims description 2
- 208000004852 Lung Injury Diseases 0.000 claims description 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 206010027406 Mesothelioma Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 208000001132 Osteoporosis Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 2
- 208000012287 Prolapse Diseases 0.000 claims description 2
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims description 2
- 208000017442 Retinal disease Diseases 0.000 claims description 2
- 206010038923 Retinopathy Diseases 0.000 claims description 2
- 206010039491 Sarcoma Diseases 0.000 claims description 2
- 206010039580 Scar Diseases 0.000 claims description 2
- 206010039710 Scleroderma Diseases 0.000 claims description 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims description 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 206010069363 Traumatic lung injury Diseases 0.000 claims description 2
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 238000009825 accumulation Methods 0.000 claims description 2
- 208000002517 adenoid cystic carcinoma Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims description 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims description 2
- 208000028922 artery disease Diseases 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 201000009036 biliary tract cancer Diseases 0.000 claims description 2
- 208000020790 biliary tract neoplasm Diseases 0.000 claims description 2
- 201000003149 breast fibroadenoma Diseases 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 210000003169 central nervous system Anatomy 0.000 claims description 2
- 208000026106 cerebrovascular disease Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 208000018631 connective tissue disease Diseases 0.000 claims description 2
- 208000010247 contact dermatitis Diseases 0.000 claims description 2
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims description 2
- 229940127089 cytotoxic agent Drugs 0.000 claims description 2
- 230000003111 delayed effect Effects 0.000 claims description 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 2
- 210000004696 endometrium Anatomy 0.000 claims description 2
- 210000002744 extracellular matrix Anatomy 0.000 claims description 2
- 208000030533 eye disease Diseases 0.000 claims description 2
- 208000010706 fatty liver disease Diseases 0.000 claims description 2
- 230000003176 fibrotic effect Effects 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 230000002496 gastric effect Effects 0.000 claims description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 2
- GWVMLCQWXVFZCN-UHFFFAOYSA-N isoindoline Chemical compound C1=CC=C2CNCC2=C1 GWVMLCQWXVFZCN-UHFFFAOYSA-N 0.000 claims description 2
- 210000001117 keloid Anatomy 0.000 claims description 2
- 206010023841 laryngeal neoplasm Diseases 0.000 claims description 2
- 210000004185 liver Anatomy 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 231100000515 lung injury Toxicity 0.000 claims description 2
- 208000002780 macular degeneration Diseases 0.000 claims description 2
- 208000008585 mastocytosis Diseases 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 210000004165 myocardium Anatomy 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 230000005855 radiation Effects 0.000 claims description 2
- 201000002793 renal fibrosis Diseases 0.000 claims description 2
- 201000007416 salivary gland adenoid cystic carcinoma Diseases 0.000 claims description 2
- 208000010157 sclerosing cholangitis Diseases 0.000 claims description 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 2
- 208000020431 spinal cord injury Diseases 0.000 claims description 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 2
- 230000007863 steatosis Effects 0.000 claims description 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 208000019553 vascular disease Diseases 0.000 claims description 2
- 230000029663 wound healing Effects 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims 1
- VPXLBSOCFQUCMB-UHFFFAOYSA-N CC(C=C1)N(Cc(cc2)ccc2C(Nc2cc(Nc3nc(-c4cnccc4)ccn3)c(C)cc2)=O)C1=O Chemical compound CC(C=C1)N(Cc(cc2)ccc2C(Nc2cc(Nc3nc(-c4cnccc4)ccn3)c(C)cc2)=O)C1=O VPXLBSOCFQUCMB-UHFFFAOYSA-N 0.000 description 1
- GRJQOOLCMPVSAO-UHFFFAOYSA-N CC1C=CC(C(Nc(cc2-[n]3cnc(C)c3)ccc2NC(C=C)=O)=O)=CC1Nc1nc(-c2cnccc2)ccn1 Chemical compound CC1C=CC(C(Nc(cc2-[n]3cnc(C)c3)ccc2NC(C=C)=O)=O)=CC1Nc1nc(-c2cnccc2)ccn1 GRJQOOLCMPVSAO-UHFFFAOYSA-N 0.000 description 1
- COOJMYWLWNYMCL-UHFFFAOYSA-N Cc(ccc(C(NC(C=C1C(F)(F)F)=CCC1NC(COC(C1C(Cl)=CC=CC1Cl)=O)O)=O)c1)c1Nc1nc(-c2cnccc2)ccn1 Chemical compound Cc(ccc(C(NC(C=C1C(F)(F)F)=CCC1NC(COC(C1C(Cl)=CC=CC1Cl)=O)O)=O)c1)c1Nc1nc(-c2cnccc2)ccn1 COOJMYWLWNYMCL-UHFFFAOYSA-N 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94187307P | 2007-06-04 | 2007-06-04 | |
| US60/941,873 | 2007-06-04 | ||
| US97204807P | 2007-09-13 | 2007-09-13 | |
| US60/972,048 | 2007-09-13 | ||
| PCT/US2008/065646 WO2008151183A1 (en) | 2007-06-04 | 2008-06-03 | Heterocyclic compounds and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013155820A Division JP5845215B2 (ja) | 2007-06-04 | 2013-07-26 | 複素環化合物およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010529134A JP2010529134A (ja) | 2010-08-26 |
| JP2010529134A5 true JP2010529134A5 (https=) | 2012-05-24 |
| JP5526020B2 JP5526020B2 (ja) | 2014-06-18 |
Family
ID=40089003
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010511276A Expired - Fee Related JP5526020B2 (ja) | 2007-06-04 | 2008-06-03 | 複素環化合物およびその使用 |
| JP2013155820A Expired - Fee Related JP5845215B2 (ja) | 2007-06-04 | 2013-07-26 | 複素環化合物およびその使用 |
| JP2015227445A Pending JP2016033142A (ja) | 2007-06-04 | 2015-11-20 | 複素環化合物およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013155820A Expired - Fee Related JP5845215B2 (ja) | 2007-06-04 | 2013-07-26 | 複素環化合物およびその使用 |
| JP2015227445A Pending JP2016033142A (ja) | 2007-06-04 | 2015-11-20 | 複素環化合物およびその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (4) | US8242271B2 (https=) |
| EP (1) | EP2152079A4 (https=) |
| JP (3) | JP5526020B2 (https=) |
| CA (1) | CA2689989A1 (https=) |
| TW (1) | TWI433677B (https=) |
| WO (1) | WO2008151183A1 (https=) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8242271B2 (en) * | 2007-06-04 | 2012-08-14 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| PT2300013T (pt) | 2008-05-21 | 2017-10-31 | Ariad Pharma Inc | Derivados de fósforo como inibidores de cinases |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| US8338439B2 (en) * | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| TWI546290B (zh) | 2008-06-27 | 2016-08-21 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| JP2012501654A (ja) * | 2008-09-05 | 2012-01-26 | アビラ セラピューティクス， インコーポレイテッド | 不可逆的インヒビターの設計のためのアルゴリズム |
| WO2010039545A2 (en) * | 2008-09-23 | 2010-04-08 | Georgetown University | 1,2-benzisothiazolinone and isoindolinone derivatives |
| KR101705158B1 (ko) | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Ｅｇｆｒ 억제제 및 질환 치료방법 |
| EP2440058A4 (en) | 2009-06-12 | 2012-11-21 | Dana Farber Cancer Inst Inc | MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF |
| CN101928277B (zh) * | 2009-06-24 | 2012-09-19 | 浙江九洲药业股份有限公司 | 4-甲基-3-[[4-(3-吡啶基)-2-嘧啶基]氨基]安息香酸的制备方法、相关中间体及其应用 |
| WO2011008788A1 (en) * | 2009-07-14 | 2011-01-20 | Dawei Zhang | Fluoro-substituted compounds as kinase inhibitors and methods of use thereof |
| EP2475375A4 (en) * | 2009-09-09 | 2013-02-20 | Avila Therapeutics Inc | PI3 KINASE INHIBITORS AND USES THEREOF |
| NZ620174A (en) * | 2009-09-16 | 2016-08-26 | Celgene Avilomics Res Inc | Protein kinase conjugates and inhibitors |
| US9180127B2 (en) | 2009-12-29 | 2015-11-10 | Dana-Farber Cancer Institute, Inc. | Type II Raf kinase inhibitors |
| EP2519664A4 (en) | 2009-12-30 | 2014-03-12 | Avila Therapeutics Inc | LIGAND-RELATED COVALENTS MODIFYING A PROTEIN |
| CN105566229A (zh) | 2010-08-10 | 2016-05-11 | 西建阿维拉米斯研究公司 | Btk抑制剂的苯磺酸盐及其用途和制备方法 |
| EP2635285B1 (en) | 2010-11-01 | 2017-05-03 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| MX382354B (es) | 2010-11-01 | 2025-03-13 | Celgene Car Llc | Compuestos heterocíclicos y usos de los mismos. |
| JP5957003B2 (ja) | 2010-11-10 | 2016-07-27 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | 変異体選択的ｅｇｆｒ阻害剤およびその使用 |
| US9834518B2 (en) | 2011-05-04 | 2017-12-05 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| US9428472B2 (en) | 2011-08-16 | 2016-08-30 | Georgetown University | Methods of treating bacterial infections with 1,2-benzisothiazolinone and isoindolinone derivatives |
| AR088570A1 (es) | 2011-10-28 | 2014-06-18 | Celgene Avilomics Res Inc | Metodos para tratar una enfermedad o trastorno relacionado con la tirosina quinasa de bruton |
| CA2856291C (en) | 2011-11-17 | 2020-08-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| KR102081042B1 (ko) | 2012-03-15 | 2020-02-26 | 셀젠 카르 엘엘씨 | 상피 성장 인자 수용체 키나제 억제제의 고체 형태 |
| PL2825042T3 (pl) | 2012-03-15 | 2019-02-28 | Celgene Car Llc | Sole inhibitora kinazy receptora czynnika wzrostu naskórka |
| US20150166591A1 (en) | 2012-05-05 | 2015-06-18 | Ariad Pharmaceuticals, Inc. | Methods and compositions for raf kinase mediated diseases |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
| US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| US9126950B2 (en) | 2012-12-21 | 2015-09-08 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| AU2014214846A1 (en) | 2013-02-08 | 2015-07-23 | Celgene Avilomics Research, Inc. | ERK inhibitors and uses thereof |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| KR101665301B1 (ko) | 2013-08-07 | 2016-10-11 | 카딜라 핼쓰캐어 리미티드 | 야누스 키나제의 억제제로서 n-시아노메틸아미드 |
| US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
| EP3057955B1 (en) | 2013-10-18 | 2018-04-11 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
| US10047070B2 (en) | 2013-10-18 | 2018-08-14 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| CN106458990B (zh) * | 2014-04-04 | 2019-06-07 | 希洛斯医药品股份有限公司 | 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂 |
| US10017477B2 (en) | 2014-04-23 | 2018-07-10 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| US9862688B2 (en) | 2014-04-23 | 2018-01-09 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| US10786578B2 (en) | 2014-08-05 | 2020-09-29 | Novartis Ag | CKIT antibody drug conjugates |
| US10005760B2 (en) | 2014-08-13 | 2018-06-26 | Celgene Car Llc | Forms and compositions of an ERK inhibitor |
| AU2015371251B2 (en) | 2014-12-23 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| HK1246645A1 (zh) | 2015-03-27 | 2018-09-14 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| WO2017030892A1 (en) | 2015-08-14 | 2017-02-23 | Reaction Biology Corp. | Histone deacetylase inhibitors and methods for use thereof |
| EP3347018B1 (en) | 2015-09-09 | 2021-09-01 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| MA46205A (fr) * | 2016-09-08 | 2019-07-17 | Sabila Biosciences Llc | Composés 1,2-dithiolane utiles dans la neuroprotection, les maladies et les états auto-immuns et cancéreux |
| CN107805240A (zh) * | 2016-09-08 | 2018-03-16 | 中国科学院合肥物质科学研究院 | 一种新型的pdgfr激酶抑制剂及其用途 |
| GB201616511D0 (en) | 2016-09-29 | 2016-11-16 | Mission Therapeutics Limited | Novel compounds |
| GB201616627D0 (en) | 2016-09-30 | 2016-11-16 | Mission Therapeutics Limited | Novel compounds |
| GB201708652D0 (en) | 2017-05-31 | 2017-07-12 | Mission Therapeutics Ltd | Novel compounds and uses |
| JP7208931B2 (ja) | 2017-06-20 | 2023-01-19 | ミッション セラピューティクス リミティド | Ｄｕｂ阻害剤としての活性をもつ置換シアノピロリジン類 |
| JP7481329B2 (ja) * | 2018-06-07 | 2024-05-10 | ディスアーム セラピューティクス， インコーポレイテッド | Ｓａｒｍ１阻害剤 |
| CN108623490A (zh) * | 2018-06-22 | 2018-10-09 | 苏州市贝克生物科技有限公司 | (2z)-4-(二甲基氨基)-2-丁烯酸盐酸盐的合成方法 |
| US12187701B2 (en) | 2018-06-25 | 2025-01-07 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| WO2020132045A1 (en) | 2018-12-19 | 2020-06-25 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 in combination with neuroprotective agents |
| JP7660063B2 (ja) | 2018-12-28 | 2025-04-10 | ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼ７のインヒビターおよびそれらの使用 |
| GB201905371D0 (en) | 2019-04-16 | 2019-05-29 | Mission Therapeutics Ltd | Novel compounds |
| GB201905375D0 (en) | 2019-04-16 | 2019-05-29 | Mission Therapeutics Ltd | Novel compounds |
| EP3980011B1 (en) * | 2019-06-06 | 2025-12-17 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| GB201912674D0 (en) | 2019-09-04 | 2019-10-16 | Mission Therapeutics Ltd | Novel compounds |
| CN111253335B (zh) * | 2020-03-12 | 2023-06-06 | 浙江扬帆新材料股份有限公司 | 一种n-取代苯并异噻唑啉-3-酮衍生物的新合成方法 |
| CN111269217B (zh) * | 2020-04-07 | 2021-01-08 | 苏州信诺维医药科技有限公司 | 一种嘧啶胺类化合物、其制备方法及应用 |
| WO2021204856A1 (en) | 2020-04-08 | 2021-10-14 | Mission Therapeutics Limited | N-cyanopyrrolidines with activity as usp30 inhibitors |
| IL298526A (en) | 2020-05-28 | 2023-01-01 | Mission Therapeutics Ltd | N-(1-cyano-pyrrolidin-3-yl)-5-(3-(trifluoromethyl)phenyl)oxazole-2-carboxamide derivatives and the corresponding oxadiazole derivatives as usp30 inhibitors for the treatment of mitochondrial dysfunction |
| BR112022019722A2 (pt) | 2020-06-04 | 2022-12-20 | Mission Therapeutics Ltd | N-cianopirrolidinas com atividade como inibidores de usp30 |
| DK4161929T3 (da) | 2020-06-08 | 2025-08-18 | Mission Therapeutics Ltd | 1-(5-(2-cyanopyridin-4-yl)oxazol-2-carbonyl)-4-methylhexahydropyrrolo[3,4-b]pyrrol-5(1h)-carbonitril som usp30-hæmmer til anvendelse i behandling af mitokondriedysfunktion, cancer og fibrose |
| GB202016800D0 (en) | 2020-10-22 | 2020-12-09 | Mission Therapeutics Ltd | Novel compounds |
| US20250034122A1 (en) | 2021-12-01 | 2025-01-30 | Mission Therapeutics Limited | Substituted n-cyanopyrrolidines with activity as usp30 inhibitors |
| KR20250034169A (ko) * | 2022-07-19 | 2025-03-10 | 키에시 파르마슈티시 엣스. 피. 에이. | Ddr 억제제로서의 헤테로아릴 유도체 |
| GB202408928D0 (en) | 2024-06-21 | 2024-08-07 | Mission Therapeutics Ltd | Novel compounds |
| GB202411060D0 (en) | 2024-07-29 | 2024-09-11 | Mission Therapeutics Ltd | Novel compounds |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| GB0022438D0 (en) | 2000-09-13 | 2000-11-01 | Novartis Ag | Organic Compounds |
| US20040157855A1 (en) | 2001-04-05 | 2004-08-12 | Michael Heinrich | Use of n-phenyl-2-pyrimidineamine derivativea against mast cell-based diseases like allergic disorders |
| AU2002342878A1 (en) | 2001-05-16 | 2002-11-25 | Axxima Pharmaceuticals Ag | Pyridylpyrimidine derivatives as effective compounds against prion diseases |
| EP1408978A4 (en) | 2001-06-21 | 2005-07-13 | Ariad Pharma Inc | NOVEL PHENYLAMINO-PYRIMIDINES AND THEIR USE |
| KR20040062557A (ko) | 2001-11-01 | 2004-07-07 | 얀센 파마슈티카 엔.브이. | 글리코겐 신타제 키나제 3β 억제제로서의아미노벤즈아미드 유도체 |
| MXPA04004178A (es) | 2001-11-01 | 2004-09-06 | Janssen Pharmaceutica Nv | Heteroarilaminas como inhibidores de glucogeno cintasa cinasa 3beta. |
| GB0201508D0 (en) | 2002-01-23 | 2002-03-13 | Novartis Ag | Organic compounds |
| GB0202873D0 (en) | 2002-02-07 | 2002-03-27 | Novartis Ag | Organic compounds |
| GB0215676D0 (en) * | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| US20060105445A1 (en) | 2002-07-29 | 2006-05-18 | Klaus Godl | Medium and method for enriching, purifying or depleting atp binding proteins from a pool of proteins |
| MY139563A (en) * | 2002-09-04 | 2009-10-30 | Bristol Myers Squibb Co | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
| CA2439440A1 (en) | 2002-09-05 | 2004-03-05 | Emory University | Treatment of tuberous sclerosis associated neoplasms |
| GB0222514D0 (en) | 2002-09-27 | 2002-11-06 | Novartis Ag | Organic compounds |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| US7279576B2 (en) * | 2002-12-31 | 2007-10-09 | Deciphera Pharmaceuticals, Llc | Anti-cancer medicaments |
| WO2005065074A2 (en) | 2003-09-09 | 2005-07-21 | Temple University Of The Commonwealth System Of Higher Education | Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors |
| GB0325031D0 (en) | 2003-10-27 | 2003-12-03 | Novartis Ag | Organic compounds |
| WO2005049021A1 (en) | 2003-11-03 | 2005-06-02 | Oy Helsinki Transplantation R & D Ltd | Materials and methods for inhibiting neointimal hyperplasia |
| EP3299358A1 (en) * | 2003-12-25 | 2018-03-28 | Nippon Shinyaku Co., Ltd. | Amide derivative and medicine |
| WO2005063720A1 (ja) | 2003-12-25 | 2005-07-14 | Nippon Shinyaku Co., Ltd. | アミド誘導体及び医薬 |
| ATE481134T1 (de) | 2004-01-21 | 2010-10-15 | Univ Emory | Zusammensetzungen und verwendung von tyrosinkinase-hemmern zur behandlung von pathogenen infektionen |
| EP1751136B1 (en) | 2004-05-07 | 2014-07-02 | Amgen Inc. | Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer |
| WO2005115385A1 (en) | 2004-05-24 | 2005-12-08 | Ab Science | Use of c-kit inhibitors for treating acne |
| WO2006017353A2 (en) | 2004-07-13 | 2006-02-16 | GOVERNMENT OF THE UNITED STATES, as represented byTHE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES | Treatment of viral infections |
| JP2008510766A (ja) | 2004-08-27 | 2008-04-10 | ゲーペーツェー ビオテック アーゲー | ピリミジン誘導体 |
| ES2373912T3 (es) | 2005-01-28 | 2012-02-10 | Novartis Ag | Uso de pirimidilaminobenzamidas para el tratamiento de enfermedades que responden a la modulación de la actividad de quinasa tie-2. |
| CN101160131A (zh) | 2005-02-25 | 2008-04-09 | 诺瓦提斯公司 | Bcr-abl和raf抑制剂的药物组合产品 |
| MX2007013741A (es) | 2005-05-02 | 2008-01-21 | Novartis Ag | Uso de derivados de pirimidilaminobenzamida para el tratamiento de mastocitosis sistemica. |
| SA06270147B1 (ar) | 2005-06-09 | 2009-12-22 | نوفارتيس ايه جي | عملية لتخليق 5-(مثيل–1h–إيميدازول–1-يل )–3-(ثلاثي فلـورو مثيل)–بنزامـين |
| CN101227909A (zh) | 2005-07-20 | 2008-07-23 | 诺瓦提斯公司 | 包含嘧啶基氨基苯甲酰胺化合物和Flt-3抑制剂用于治疗增殖性疾病的组合 |
| KR100674813B1 (ko) | 2005-08-05 | 2007-01-29 | 일양약품주식회사 | Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 |
| ES2549327T3 (es) | 2005-12-06 | 2015-10-27 | Novartis Ag | Derivados de pirimidilaminobenzamida para el tratamiento de la neurofibromatosis |
| WO2008058037A1 (en) * | 2006-11-03 | 2008-05-15 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| US8242271B2 (en) | 2007-06-04 | 2012-08-14 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| JP2012501654A (ja) * | 2008-09-05 | 2012-01-26 | アビラ セラピューティクス， インコーポレイテッド | 不可逆的インヒビターの設計のためのアルゴリズム |
-
2008
- 2008-06-03 US US12/132,537 patent/US8242271B2/en not_active Expired - Fee Related
- 2008-06-03 CA CA2689989A patent/CA2689989A1/en not_active Abandoned
- 2008-06-03 WO PCT/US2008/065646 patent/WO2008151183A1/en not_active Ceased
- 2008-06-03 JP JP2010511276A patent/JP5526020B2/ja not_active Expired - Fee Related
- 2008-06-03 EP EP08770044A patent/EP2152079A4/en not_active Withdrawn
- 2008-06-03 TW TW097120571A patent/TWI433677B/zh active
-
2012
- 2012-05-31 US US13/485,037 patent/US8586600B2/en not_active Expired - Fee Related
-
2013
- 2013-07-26 JP JP2013155820A patent/JP5845215B2/ja not_active Expired - Fee Related
- 2013-11-15 US US14/080,890 patent/US9067929B2/en not_active Expired - Fee Related
-
2015
- 2015-05-21 US US14/718,700 patent/US20150252019A1/en not_active Abandoned
- 2015-11-20 JP JP2015227445A patent/JP2016033142A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2010529134A5 (https=) | ||
| JP7838004B2 (ja) | Ｐｏｌｙｂｒｏｍｏ－１（ｐｂｒｍ１）の小分子分解剤 | |
| Wei et al. | Discovery of potent and selective CDK9 degraders for targeting transcription regulation in triple-negative breast cancer | |
| CN110582483B (zh) | 含邻氨基杂芳环炔基的化合物及其制备方法和用途 | |
| ES2869277T3 (es) | Formas sólidas de un inhibidor selectivo de CDK4/6 | |
| CA2853401C (en) | Anticancer benzopyrazines via the inhibition of fgfr kinases | |
| CA2660899C (en) | Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders | |
| JP5462168B2 (ja) | Ｎ−（５−ｔｅｒｔ−ブチル−イソオキサゾール−３−イル）−Ｎ’−｛４−［７−（２−モルホリン−４−イル−エトキシ）イミダゾ［２，１−ｂ］［１，３］ベンゾチアゾール−２−イル］フェニル｝ウレアを含む固形、その組成物、及びその用途 | |
| TW200301110A (en) | Indole compounds | |
| CN109516961B (zh) | 氨基喹唑啉酮和氨基异喹啉酮衍生物及其应用 | |
| Fan et al. | Design, synthesis, and biological evaluation of novel 3-substituted imidazo [1, 2-a] pyridine and quinazolin-4 (3H)-one derivatives as PI3Kα inhibitors | |
| WO2012007926A1 (en) | Substituted imidazoquinoline derivatives as kinase inhibitors | |
| AU2015227454A1 (en) | Functionalised and substituted indoles as anti-cancer agents | |
| JP2011515370A (ja) | ４−アミノ−５−フルオロ−３−［５−（４−メチルピペラジン−１−イル）−１ｈ−ベンズイミダゾール−２−イル］キノリン−２（１ｈ）−オン乳酸塩の結晶形態及び２つの溶媒和物形態 | |
| WO2016208592A1 (ja) | 二環性複素環アミド誘導体 | |
| EA032838B1 (ru) | Макроциклические ингибиторы lrrk2-киназы | |
| TWI670261B (zh) | 熱休克蛋白90抑制劑 | |
| AU2016214492A1 (en) | 2-phenyl-3H-imidazo[4,5-b]pyridine derivates useful as inhibitors of mammalian tyrosine kinase ROR1activity | |
| CA3216489A1 (en) | Substituted fused bicyclic compounds as parp inhibitors and the use thereof | |
| JPWO2019173516A5 (https=) | ||
| TW200813058A (en) | Quinoline derivatives, their preparation, their use, and medicaments comprising them | |
| CN106117182B (zh) | 喹唑啉-n-苯乙基四氢异喹啉类化合物及其制备方法和应用 | |
| AU2014284013B2 (en) | Five-membered heterocyclic pyridine compounds and preparation method and use thereof | |
| CN109153639B (zh) | 葫芦巴碱类化合物 | |
| JP7849580B2 (ja) | Ｈｅｒ２の強力かつ選択的な阻害剤 |