JP2016504387A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016504387A5 JP2016504387A5 JP2015551853A JP2015551853A JP2016504387A5 JP 2016504387 A5 JP2016504387 A5 JP 2016504387A5 JP 2015551853 A JP2015551853 A JP 2015551853A JP 2015551853 A JP2015551853 A JP 2015551853A JP 2016504387 A5 JP2016504387 A5 JP 2016504387A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cancer
- group
- disease
- compound
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 110
- 150000001875 compounds Chemical class 0.000 claims description 90
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 56
- 125000001424 substituent group Chemical group 0.000 claims description 38
- 150000004820 halides Chemical class 0.000 claims description 34
- 208000035475 disorder Diseases 0.000 claims description 30
- -1 carbocyclyl R 11 Chemical compound 0.000 claims description 26
- 201000010099 disease Diseases 0.000 claims description 26
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 206010016654 Fibrosis Diseases 0.000 claims description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 12
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 12
- 230000004761 fibrosis Effects 0.000 claims description 12
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Substances C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 12
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 11
- 150000003839 salts Chemical class 0.000 claims description 10
- 208000011580 syndromic disease Diseases 0.000 claims description 10
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 8
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 208000005069 pulmonary fibrosis Diseases 0.000 claims description 8
- 210000000988 bone and bone Anatomy 0.000 claims description 6
- 210000004027 cell Anatomy 0.000 claims description 6
- 230000003176 fibrotic effect Effects 0.000 claims description 6
- 230000000926 neurological effect Effects 0.000 claims description 6
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 6
- 102000013814 Wnt Human genes 0.000 claims description 5
- 108050003627 Wnt Proteins 0.000 claims description 5
- 125000006545 (C1-C9) alkyl group Chemical group 0.000 claims description 4
- 208000020084 Bone disease Diseases 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000019693 Lung disease Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010025323 Lymphomas Diseases 0.000 claims description 4
- 208000001089 Multiple system atrophy Diseases 0.000 claims description 4
- 208000002158 Proliferative Vitreoretinopathy Diseases 0.000 claims description 4
- 206010038934 Retinopathy proliferative Diseases 0.000 claims description 4
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 4
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 4
- 208000015100 cartilage disease Diseases 0.000 claims description 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 208000021971 neovascular inflammatory vitreoretinopathy Diseases 0.000 claims description 4
- 201000001119 neuropathy Diseases 0.000 claims description 4
- 230000007823 neuropathy Effects 0.000 claims description 4
- 201000008482 osteoarthritis Diseases 0.000 claims description 4
- 230000000750 progressive effect Effects 0.000 claims description 4
- 230000006785 proliferative vitreoretinopathy Effects 0.000 claims description 4
- 201000000849 skin cancer Diseases 0.000 claims description 4
- 229930192474 thiophene Natural products 0.000 claims description 4
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 208000006468 Adrenal Cortex Neoplasms Diseases 0.000 claims description 2
- 206010061424 Anal cancer Diseases 0.000 claims description 2
- 208000009575 Angelman syndrome Diseases 0.000 claims description 2
- 208000007860 Anus Neoplasms Diseases 0.000 claims description 2
- 206010003805 Autism Diseases 0.000 claims description 2
- 208000020706 Autistic disease Diseases 0.000 claims description 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 201000000046 Beckwith-Wiedemann syndrome Diseases 0.000 claims description 2
- 206010004593 Bile duct cancer Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 206010005949 Bone cancer Diseases 0.000 claims description 2
- 208000018084 Bone neoplasm Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010007279 Carcinoid tumour of the gastrointestinal tract Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 201000009273 Endometriosis Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000006168 Ewing Sarcoma Diseases 0.000 claims description 2
- 208000028506 Familial Exudative Vitreoretinopathies Diseases 0.000 claims description 2
- 201000011240 Frontotemporal dementia Diseases 0.000 claims description 2
- 208000008875 Fuhrmann syndrome Diseases 0.000 claims description 2
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims description 2
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims description 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims description 2
- 208000017604 Hodgkin disease Diseases 0.000 claims description 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims description 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 206010021042 Hypopharyngeal cancer Diseases 0.000 claims description 2
- 206010056305 Hypopharyngeal neoplasm Diseases 0.000 claims description 2
- 208000033321 ICF syndrome Diseases 0.000 claims description 2
- 208000029523 Interstitial Lung disease Diseases 0.000 claims description 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010023421 Kidney fibrosis Diseases 0.000 claims description 2
- 206010023825 Laryngeal cancer Diseases 0.000 claims description 2
- 208000009829 Lewy Body Disease Diseases 0.000 claims description 2
- 201000002832 Lewy body dementia Diseases 0.000 claims description 2
- 208000032271 Malignant tumor of penis Diseases 0.000 claims description 2
- 206010027476 Metastases Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 208000021642 Muscular disease Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims description 2
- 201000009623 Myopathy Diseases 0.000 claims description 2
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims description 2
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010031127 Orthostatic hypotension Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010033799 Paralysis Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 208000002471 Penile Neoplasms Diseases 0.000 claims description 2
- 206010034299 Penile cancer Diseases 0.000 claims description 2
- 108091000080 Phosphotransferase Proteins 0.000 claims description 2
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 201000010769 Prader-Willi syndrome Diseases 0.000 claims description 2
- 206010049422 Precancerous skin lesion Diseases 0.000 claims description 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 2
- 208000024777 Prion disease Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000032056 Radiation Fibrosis Syndrome Diseases 0.000 claims description 2
- 206010067953 Radiation fibrosis Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000007135 Retinal Neovascularization Diseases 0.000 claims description 2
- 201000000582 Retinoblastoma Diseases 0.000 claims description 2
- 208000006289 Rett Syndrome Diseases 0.000 claims description 2
- 208000022617 SERKAL syndrome Diseases 0.000 claims description 2
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims description 2
- 206010061934 Salivary gland cancer Diseases 0.000 claims description 2
- 206010039491 Sarcoma Diseases 0.000 claims description 2
- 206010039710 Scleroderma Diseases 0.000 claims description 2
- 206010072610 Skeletal dysplasia Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 2
- 206010057644 Testis cancer Diseases 0.000 claims description 2
- 208000000728 Thymus Neoplasms Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 206010067269 Uterine fibrosis Diseases 0.000 claims description 2
- 206010047486 Virilism Diseases 0.000 claims description 2
- 206010047741 Vulval cancer Diseases 0.000 claims description 2
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims description 2
- 208000008383 Wilms tumor Diseases 0.000 claims description 2
- 210000001766 X chromosome Anatomy 0.000 claims description 2
- 201000006288 alpha thalassemia Diseases 0.000 claims description 2
- 201000011165 anus cancer Diseases 0.000 claims description 2
- 210000004227 basal ganglia Anatomy 0.000 claims description 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 2
- 210000004556 brain Anatomy 0.000 claims description 2
- 210000003169 central nervous system Anatomy 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims description 2
- 230000007882 cirrhosis Effects 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 208000029078 coronary artery disease Diseases 0.000 claims description 2
- 230000007850 degeneration Effects 0.000 claims description 2
- 230000003412 degenerative effect Effects 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 230000002124 endocrine Effects 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 201000006902 exudative vitreoretinopathy Diseases 0.000 claims description 2
- 208000024519 eye neoplasm Diseases 0.000 claims description 2
- 201000010175 gallbladder cancer Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 2
- 208000003884 gestational trophoblastic disease Diseases 0.000 claims description 2
- 206010061989 glomerulosclerosis Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 230000001969 hypertrophic effect Effects 0.000 claims description 2
- 201000006866 hypopharynx cancer Diseases 0.000 claims description 2
- 201000008319 inclusion body myositis Diseases 0.000 claims description 2
- 208000023589 ischemic disease Diseases 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 206010023841 laryngeal neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 231100000794 masculinization Toxicity 0.000 claims description 2
- 230000002503 metabolic effect Effects 0.000 claims description 2
- 230000009401 metastasis Effects 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 208000010125 myocardial infarction Diseases 0.000 claims description 2
- 208000026721 nail disease Diseases 0.000 claims description 2
- 201000008026 nephroblastoma Diseases 0.000 claims description 2
- 201000010193 neural tube defect Diseases 0.000 claims description 2
- 210000004940 nucleus Anatomy 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 201000008106 ocular cancer Diseases 0.000 claims description 2
- 201000001937 osteoporosis-pseudoglioma syndrome Diseases 0.000 claims description 2
- 201000008968 osteosarcoma Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 230000037361 pathway Effects 0.000 claims description 2
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 102000020233 phosphotransferase Human genes 0.000 claims description 2
- 208000010916 pituitary tumor Diseases 0.000 claims description 2
- 208000015768 polyposis Diseases 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims description 2
- 108090000623 proteins and genes Proteins 0.000 claims description 2
- 201000002793 renal fibrosis Diseases 0.000 claims description 2
- 208000037803 restenosis Diseases 0.000 claims description 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims description 2
- 230000036573 scar formation Effects 0.000 claims description 2
- 230000037390 scarring Effects 0.000 claims description 2
- 201000002314 small intestine cancer Diseases 0.000 claims description 2
- 206010062261 spinal cord neoplasm Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 208000035581 susceptibility to neural tube defects Diseases 0.000 claims description 2
- 230000009885 systemic effect Effects 0.000 claims description 2
- 201000003120 testicular cancer Diseases 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 208000037965 uterine sarcoma Diseases 0.000 claims description 2
- 206010046885 vaginal cancer Diseases 0.000 claims description 2
- 208000013139 vaginal neoplasm Diseases 0.000 claims description 2
- 201000005102 vulva cancer Diseases 0.000 claims description 2
- 206010002961 Aplasia Diseases 0.000 claims 1
- 206010061159 Foot deformity Diseases 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 description 1
- 0 C*c1c[s]cc1 Chemical compound C*c1c[s]cc1 0.000 description 1
- ZOBHKNDSXINZGQ-UHFFFAOYSA-N CCN(C)CCN(C)C Chemical compound CCN(C)CCN(C)C ZOBHKNDSXINZGQ-UHFFFAOYSA-N 0.000 description 1
- BLHTXORQJNCSII-UHFFFAOYSA-N Cc1c[n](C)cn1 Chemical compound Cc1c[n](C)cn1 BLHTXORQJNCSII-UHFFFAOYSA-N 0.000 description 1
- KJRRQXYWFQKJIP-UHFFFAOYSA-N Cc1c[o]cc1 Chemical compound Cc1c[o]cc1 KJRRQXYWFQKJIP-UHFFFAOYSA-N 0.000 description 1
- 101100317380 Danio rerio wnt4a gene Proteins 0.000 description 1
- 206010058314 Dysplasia Diseases 0.000 description 1
- 101000814371 Homo sapiens Protein Wnt-10a Proteins 0.000 description 1
- 101000770799 Homo sapiens Protein Wnt-10b Proteins 0.000 description 1
- 101000781981 Homo sapiens Protein Wnt-11 Proteins 0.000 description 1
- 101000781950 Homo sapiens Protein Wnt-16 Proteins 0.000 description 1
- 101000804728 Homo sapiens Protein Wnt-2b Proteins 0.000 description 1
- 101000804792 Homo sapiens Protein Wnt-5a Proteins 0.000 description 1
- 101000804804 Homo sapiens Protein Wnt-5b Proteins 0.000 description 1
- 101000855002 Homo sapiens Protein Wnt-6 Proteins 0.000 description 1
- 101000855004 Homo sapiens Protein Wnt-7a Proteins 0.000 description 1
- 101000814380 Homo sapiens Protein Wnt-7b Proteins 0.000 description 1
- 101000814350 Homo sapiens Protein Wnt-8a Proteins 0.000 description 1
- 101000650149 Homo sapiens Protein Wnt-8b Proteins 0.000 description 1
- 101000650117 Homo sapiens Protein Wnt-9a Proteins 0.000 description 1
- 101000650119 Homo sapiens Protein Wnt-9b Proteins 0.000 description 1
- 101000781955 Homo sapiens Proto-oncogene Wnt-1 Proteins 0.000 description 1
- 101000954762 Homo sapiens Proto-oncogene Wnt-3 Proteins 0.000 description 1
- 102100039461 Protein Wnt-10a Human genes 0.000 description 1
- 102100029062 Protein Wnt-10b Human genes 0.000 description 1
- 102100036567 Protein Wnt-11 Human genes 0.000 description 1
- 102100036587 Protein Wnt-16 Human genes 0.000 description 1
- 102100035289 Protein Wnt-2b Human genes 0.000 description 1
- 102100035331 Protein Wnt-5b Human genes 0.000 description 1
- 102100020732 Protein Wnt-6 Human genes 0.000 description 1
- 102100020729 Protein Wnt-7a Human genes 0.000 description 1
- 102100039470 Protein Wnt-7b Human genes 0.000 description 1
- 102100039453 Protein Wnt-8a Human genes 0.000 description 1
- 102100027542 Protein Wnt-8b Human genes 0.000 description 1
- 102100027503 Protein Wnt-9a Human genes 0.000 description 1
- 102100027502 Protein Wnt-9b Human genes 0.000 description 1
- 206010040869 Skin hypoplasia Diseases 0.000 description 1
- 101150010310 WNT-4 gene Proteins 0.000 description 1
- 101150019524 WNT2 gene Proteins 0.000 description 1
- 102000052547 Wnt-1 Human genes 0.000 description 1
- 102000052556 Wnt-2 Human genes 0.000 description 1
- 108700020986 Wnt-2 Proteins 0.000 description 1
- 102000052549 Wnt-3 Human genes 0.000 description 1
- 102000052548 Wnt-4 Human genes 0.000 description 1
- 108700020984 Wnt-4 Proteins 0.000 description 1
- 102000043366 Wnt-5a Human genes 0.000 description 1
- 102000044880 Wnt3A Human genes 0.000 description 1
- 108700013515 Wnt3A Proteins 0.000 description 1
- 101100485099 Xenopus laevis wnt2b-b gene Proteins 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 230000036244 malformation Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 101150068520 wnt3a gene Proteins 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361750221P | 2013-01-08 | 2013-01-08 | |
| US61/750,221 | 2013-01-08 | ||
| PCT/US2014/010607 WO2014110086A2 (en) | 2013-01-08 | 2014-01-08 | 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016504387A JP2016504387A (ja) | 2016-02-12 |
| JP2016504387A5 true JP2016504387A5 (enExample) | 2017-02-16 |
| JP6355648B2 JP6355648B2 (ja) | 2018-07-11 |
Family
ID=51061428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015551853A Active JP6355648B2 (ja) | 2013-01-08 | 2014-01-08 | Wntシグナル伝達経路の3−(ベンゾイミダゾール−2−イル)−インダゾール阻害剤およびそれらの治療的使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US9908867B2 (enExample) |
| EP (1) | EP2943198B1 (enExample) |
| JP (1) | JP6355648B2 (enExample) |
| CN (1) | CN105120862A (enExample) |
| CA (1) | CA2897400A1 (enExample) |
| MX (1) | MX370487B (enExample) |
| WO (1) | WO2014110086A2 (enExample) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2835553T3 (es) | 2009-08-10 | 2021-06-22 | Biosplice Therapeutics Inc | Inhibidores de indazol de la vía de señalización de Wnt y sus usos terapéuticos |
| CN102821607B (zh) | 2009-12-21 | 2014-12-17 | 萨穆梅德有限公司 | 1H-吡唑并[3,4-b]吡啶及其治疗应用 |
| HRP20190281T1 (hr) | 2011-09-14 | 2019-05-31 | Samumed, Llc | Indazol-3-karboksamidi i njihova uporaba kao inhibitora signalizacijskog puta wnt/b-katenin |
| PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| PL2770994T3 (pl) | 2012-05-04 | 2020-03-31 | Samumed, Llc | 1H-Pirazolo[3,4-b]pirydyny i ich zastosowania terapeutyczne |
| EP2943198B1 (en) | 2013-01-08 | 2019-07-17 | Samumed, LLC | 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof |
| WO2016040181A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040182A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof |
| WO2016040190A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040185A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof |
| WO2016040184A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040188A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040180A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040193A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| JP6800158B2 (ja) | 2015-02-20 | 2020-12-16 | ライジェル ファーマシューティカルズ, インコーポレイテッド | Gdf−8阻害剤 |
| US10188634B2 (en) | 2015-08-03 | 2019-01-29 | Samumed, Llc | 3-(3H-imidazo[4,5-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10166218B2 (en) | 2015-08-03 | 2019-01-01 | Samumed, Llc | 3-(1H-indol-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| US10285982B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-C]pyridines and therapeutic uses thereof |
| WO2017023986A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc | 3-(1h-indol-2-yl)-1h-indazoles and therapeutic uses thereof |
| WO2017023972A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| US10206909B2 (en) | 2015-08-03 | 2019-02-19 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| US10519169B2 (en) | 2015-08-03 | 2019-12-31 | Samumed, Llc | 3-(1H-pyrrolo[2,3-C]pyridin-2-yl)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017023987A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof |
| US10350199B2 (en) | 2015-08-03 | 2019-07-16 | Samumed, Llc | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| WO2017023984A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| US10231956B2 (en) | 2015-08-03 | 2019-03-19 | Samumed, Llc | 3-(1H-pyrrolo[3,2-C]pyridin-2-YL)-1 H-pyrazolo[4,3-B]pyridines and therapeutic uses thereof |
| WO2017024015A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017023993A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-indol-2-yl)-1h-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| WO2017024010A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[3,2-c]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| US10285983B2 (en) | 2015-08-03 | 2019-05-14 | Samumed, Llc | 3-(1H-pyrrolo[2,3-B]pyridin-2-yl)-1H-pyrazolo[3,4-B] pyridines and therapeutic uses thereof |
| WO2017023975A1 (en) | 2015-08-03 | 2017-02-09 | Samumed, Llc. | 3-(1h-pyrrolo[2,3-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridines and therapeutic uses thereof |
| US10392383B2 (en) | 2015-08-03 | 2019-08-27 | Samumed, Llc | 3-(1H-benzo[d]imidazol-2-yl)-1H-pyrazolo[4,3-b]pyridines and therapeutic uses thereof |
| KR20180080262A (ko) * | 2015-11-06 | 2018-07-11 | 사뮤메드, 엘엘씨 | 골관절염의 치료 |
| AR108325A1 (es) | 2016-04-27 | 2018-08-08 | Samumed Llc | Isoquinolin-3-il carboxamidas y preparación y uso de las mismas |
| ES2933109T3 (es) | 2016-06-01 | 2023-02-02 | Biosplice Therapeutics Inc | Proceso para preparar N-(5-(3-(7-(3-fluorofenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida |
| CN110709082A (zh) | 2016-10-21 | 2020-01-17 | 萨穆梅德有限公司 | 吲唑-3-甲酰胺的使用方法及其作为Wnt/β-连环蛋白信号传导途径抑制剂的用途 |
| KR102558716B1 (ko) | 2016-11-07 | 2023-07-21 | 사뮤메드, 엘엘씨 | 단일-투여량, 즉시-사용가능한 주사용 제제 |
| WO2019241540A1 (en) * | 2018-06-15 | 2019-12-19 | Samumed, Llc | Indazole containing macrocycles and therapeutic uses thereof |
| EP3911317A2 (en) | 2019-01-17 | 2021-11-24 | BioSplice Therapeutics, Inc. | Methods of treating cartilage disorders through inhibition of clk and dyrk |
| WO2021227906A1 (zh) * | 2020-05-12 | 2021-11-18 | 苏州阿尔脉生物科技有限公司 | 一种作为cdk抑制剂的吡啶乙酰胺类衍生物、其制备方法及用途 |
| WO2022012058A1 (zh) * | 2020-07-16 | 2022-01-20 | 江苏凯迪恩医药科技有限公司 | 稠环化合物及其中间体、制备方法和应用 |
| US20230404985A1 (en) * | 2020-11-02 | 2023-12-21 | Icahn School Of Medicine At Mount Sinai | Methods of treating tumors and cancers having dysregulated wnt signaling pathways |
Family Cites Families (138)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4164559A (en) | 1977-09-21 | 1979-08-14 | Cornell Research Foundation, Inc. | Collagen drug delivery device |
| ES8401486A1 (es) | 1981-11-10 | 1983-12-01 | Wellcome Found | Un procedimiento para la preparacion de nuevos derivados de imidazo (4,5-c)piridina. |
| US4474752A (en) | 1983-05-16 | 1984-10-02 | Merck & Co., Inc. | Drug delivery system utilizing thermosetting gels |
| US4783443A (en) | 1986-03-03 | 1988-11-08 | The University Of Chicago | Amino acyl cephalosporin derivatives |
| EP0410509A1 (en) | 1989-07-25 | 1991-01-30 | Duphar International Research B.V | New substituted 1H-indazole-3-carboxamides |
| GB9414139D0 (en) | 1994-07-13 | 1994-08-31 | Smithkline Beecham Plc | Novel compounds |
| US6440102B1 (en) | 1998-07-23 | 2002-08-27 | Durect Corporation | Fluid transfer and diagnostic system for treating the inner ear |
| DE19853299C2 (de) | 1998-11-19 | 2003-04-03 | Thomas Lenarz | Katheter zur Applikation von Medikamenten in Flüssigkeitsräumen des menschlichen Innenohrs |
| US6120484A (en) | 1999-02-17 | 2000-09-19 | Silverstein; Herbert | Otological implant for delivery of medicament and method of using same |
| WO2000071129A1 (en) | 1999-05-21 | 2000-11-30 | Bristol-Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| BR0012450B1 (pt) | 1999-06-23 | 2011-08-23 | benzimidazóis substituìdos. | |
| PE20010306A1 (es) | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
| TWI262914B (en) | 1999-07-02 | 2006-10-01 | Agouron Pharma | Compounds and pharmaceutical compositions for inhibiting protein kinases |
| US6844367B1 (en) | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| US6967023B1 (en) | 2000-01-10 | 2005-11-22 | Foamix, Ltd. | Pharmaceutical and cosmetic carrier or composition for topical application |
| YU54202A (sh) * | 2000-01-18 | 2006-01-16 | Agouron Pharmaceuticals Inc. | Jedinjenja indazola, farmaceutske smeše i postupci za stimulisanje i inhibiranje ćelijske proliferacije |
| US6897231B2 (en) | 2000-07-31 | 2005-05-24 | Signal Pharmaceuticals, Inc. | Indazole derivatives as JNK inhibitors and compositions and methods related thereto |
| US20050009876A1 (en) | 2000-07-31 | 2005-01-13 | Bhagwat Shripad S. | Indazole compounds, compositions thereof and methods of treatment therewith |
| US6638926B2 (en) | 2000-09-15 | 2003-10-28 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| WO2002050073A1 (en) | 2000-12-19 | 2002-06-27 | Smithkline Beecham P.L.C. | Pyrazolo[3,4-c]pyridines as gsk-3 inhibitors |
| US20050192262A1 (en) | 2001-03-13 | 2005-09-01 | Tomas Hagstrom | Treatment of tumours |
| US7390808B2 (en) | 2001-04-30 | 2008-06-24 | Vertex Pharmaceuticals Incorporated | Inhibitors of GSK-3 and crystal structures of GSK-3β protein and protein complexes |
| GB0115109D0 (en) | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| US7642278B2 (en) | 2001-07-03 | 2010-01-05 | Novartis Vaccines And Diagnostics, Inc. | Indazole benzimidazole compounds |
| JP2004536113A (ja) * | 2001-07-03 | 2004-12-02 | カイロン コーポレイション | チロシンキナーゼおよびセリン/スレオニンキナーゼのインヒビターとしてのインダゾールベンズイミダゾール化合物 |
| WO2004043335A2 (en) | 2001-09-13 | 2004-05-27 | Genesoft, Inc. | Methods of treating infection by drug resistant bacteria |
| US6648873B2 (en) | 2001-09-21 | 2003-11-18 | Durect Corp. | Aural catheter system including anchor balloon and balloon inflation device |
| FR2831536A1 (fr) | 2001-10-26 | 2003-05-02 | Aventis Pharma Sa | Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr |
| EP1441725A1 (en) | 2001-10-26 | 2004-08-04 | Aventis Pharmaceuticals Inc. | Benzimidazoles and analogues and their use as protein kinases inhibitors |
| US6897208B2 (en) | 2001-10-26 | 2005-05-24 | Aventis Pharmaceuticals Inc. | Benzimidazoles |
| CA2464333C (en) | 2001-10-26 | 2011-07-26 | University Of Connecticut | Heteroindanes: a new class of potent cannabimimetic ligands |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| AU2003218989A1 (en) | 2002-02-19 | 2003-09-09 | Pharmacia Italia S.P.A. | Tricyclic pyrazole derivatives, process for their preparation and their use as antitumor agents |
| CA2476665A1 (en) | 2002-02-19 | 2003-08-28 | Pharmacia Corporation | Tricyclic pyrazole derivatives for the treatment of inflammation |
| ES2411655T3 (es) | 2002-05-17 | 2013-07-08 | Pfizer Italia S.R.L. | Derivados de aminoindazol activos como inhibidores de quinasas, procedimiento para su preparación y composiciones farmacéuticas que los comprenden |
| US7429609B2 (en) | 2002-05-31 | 2008-09-30 | Eisai R & D Management Co., Ltd. | Pyrazole compound and medicinal composition containing the same |
| US7449488B2 (en) | 2002-06-04 | 2008-11-11 | Schering Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
| EP1511751B1 (en) | 2002-06-04 | 2008-03-19 | Neogenesis Pharmaceuticals, Inc. | Pyrazolo[1,5-a]pyrimidine compounds as antiviral agents |
| US20050282733A1 (en) | 2002-06-27 | 2005-12-22 | Prins Johannes B | Differentiation modulating agents and uses therefor |
| GB0218625D0 (en) | 2002-08-10 | 2002-09-18 | Astex Technology Ltd | Pharmaceutical compounds |
| FR2845382A1 (fr) | 2002-10-02 | 2004-04-09 | Sanofi Synthelabo | Derives d'indazolecarboxamides, leur preparation et leur utilisation en therapeutique |
| DE602004029145D1 (de) | 2003-02-27 | 2010-10-28 | Palau Pharma Sa | Pyrazolopyridin-derivate |
| US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| AU2003304380A1 (en) | 2003-07-03 | 2005-02-15 | Aventis Pharmaceuticals Inc. | Pyrazoloisoquinoline derivatives as kinase inhibitors |
| US7008953B2 (en) | 2003-07-30 | 2006-03-07 | Agouron Pharmaceuticals, Inc. | 3, 5 Disubstituted indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| GT200400136A (es) | 2003-07-30 | 2005-05-02 | Compuestos de indazol 3,5-disustituidos, composiciones farmaceuticas y metodos para intervenir en o inhibirlaproliferacion celular. | |
| US20050090529A1 (en) | 2003-07-31 | 2005-04-28 | Pfizer Inc | 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation |
| WO2005014554A1 (en) | 2003-08-08 | 2005-02-17 | Astex Therapeutics Limited | 1h-indazole-3-carboxamide compounds as mapkap kinase modulators |
| WO2005047266A1 (en) | 2003-11-14 | 2005-05-26 | Lorus Therapeutics Inc. | Aryl imidazoles and their use as anti-cancer agents |
| EP1532980A1 (en) | 2003-11-24 | 2005-05-25 | Novo Nordisk A/S | N-heteroaryl indole carboxamides and analogues thereof, for use as glucokinase activators in the treatment of diabetes |
| FR2864084B1 (fr) | 2003-12-17 | 2006-02-10 | Aventis Pharma Sa | Nouveaux derives organophosphores des indazoles et leur utilisation comme medicaments |
| FR2867778B1 (fr) | 2004-03-16 | 2006-06-09 | Sanofi Synthelabo | Utilisation de derives d'indazolecarboxamides pour la preparation d'un medicament destine au traitement et a la prevention du paludisme |
| US20050234095A1 (en) | 2004-03-25 | 2005-10-20 | Wenge Xie | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, and preparation and uses thereof |
| JP2007534692A (ja) | 2004-04-22 | 2007-11-29 | メモリー・ファーマシューティカルズ・コーポレイション | インドール、1h−インダゾール、1,2−ベンズイソキサゾール、1,2−ベンゾイソチアゾール、ならびにその調製および使用 |
| CA2566158A1 (en) | 2004-05-14 | 2005-11-24 | Abbott Laboratories | Kinase inhibitors as therapeutic agents |
| EP1781653A1 (en) | 2004-07-05 | 2007-05-09 | Astex Therapeutics Limited | 3,4-disubstituted pyrazoles as cyclin dependent kinases (cdk) or aurora kinase or glycogen synthase 3 (gsk-3) inhibitors |
| EP1778687A2 (en) | 2004-07-27 | 2007-05-02 | SGX Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| TW200618800A (en) | 2004-08-03 | 2006-06-16 | Uriach Y Compania S A J | Heterocyclic compounds |
| WO2006024945A1 (en) | 2004-09-03 | 2006-03-09 | Pfizer Inc. | Pharmaceutical compositions comprising a cdk inhibitor |
| US7652043B2 (en) | 2004-09-29 | 2010-01-26 | The Johns Hopkins University | WNT pathway antagonists |
| US20060116519A1 (en) | 2004-11-17 | 2006-06-01 | Agouron Pharmaceuticals, Inc. | Synthesis of 5-bromo-4-methyl-pyridin-3-ylmethyl)-ethyl-carbamic acid tert-butyl ester |
| WO2006054143A1 (en) | 2004-11-17 | 2006-05-26 | Pfizer Inc. | Polymorphs of {5-[3-(4,6-difluoro-1h-benzoimidazol-2-yl)-1h-indazol-5-yl]-4-methyl-pyridin-3-ylmethyl}-ethyl-amine |
| US20060127388A1 (en) | 2004-12-10 | 2006-06-15 | Wyeth | Variants of glycogen synthase kinase 3 and uses thereof |
| US20060142247A1 (en) | 2004-12-17 | 2006-06-29 | Guy Georges | Tricyclic heterocycles |
| JP2008537684A (ja) | 2005-01-24 | 2008-09-25 | ニューロシステック コーポレイション | 内耳およびその他の組織へ治療薬および/またはその他の薬剤を送達するための装置および方法 |
| WO2006130673A1 (en) | 2005-05-31 | 2006-12-07 | Janssen Pharmaceutica, N.V. | 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders |
| CA2620105A1 (en) | 2005-08-25 | 2007-03-01 | F. Hoffman-La Roche Ag | P38 map kinase inhibitors and methods for using the same |
| US8106066B2 (en) | 2005-09-23 | 2012-01-31 | Memory Pharmaceuticals Corporation | Indazoles, benzothiazoles, benzoisothiazoles, benzisoxazoles, pyrazolopyridines, isothiazolopyridines, and preparation and uses thereof |
| AR055669A1 (es) | 2005-10-03 | 2007-08-29 | Astrazeneca Ab | Derivados de 3h - imidazo[4, 5 -b]piridina como inhibidores selectivos de gsk3, metodos e internediarios para su preparacion, composiciones farmaceuticas que los contienen y su uso para la elaboracion de un medicamento para el tratamiento de enfermedades neurodegenerativas y mentales. |
| AR057987A1 (es) | 2005-11-24 | 2008-01-09 | Astrazeneca Ab | Compuestos agonistas de cb1 (receptor cannabinoide) |
| GB0602178D0 (en) | 2006-02-03 | 2006-03-15 | Merck Sharp & Dohme | Therapeutic treatment |
| WO2007107346A1 (en) | 2006-03-23 | 2007-09-27 | F. Hoffmann-La Roche Ag | Substituted indazole derivatives, their manufacture and use as pharmaceutical agents |
| US8008481B2 (en) | 2006-03-31 | 2011-08-30 | Ericsson Anna M | Indazole compounds |
| ATE456565T1 (de) | 2006-06-22 | 2010-02-15 | Biovitrum Ab Publ | Pyridin- und pyrazinderivate als mnk- kinaseinhibitoren |
| WO2008061109A2 (en) | 2006-11-15 | 2008-05-22 | Forest Laboratories Holdings Limited | Indazole derivatives useful as melanin concentrating receptor ligands |
| EP1932834B1 (en) | 2006-12-11 | 2011-04-27 | The Genetics Company, Inc. | Aromatic 1,4-DI-Carboxylamides and their use |
| EP1932830A1 (en) | 2006-12-11 | 2008-06-18 | The Genetics Company, Inc. | Sulfonamides and their use as a medicament |
| CL2007003609A1 (es) | 2006-12-14 | 2008-07-25 | Bayer Schering Pharma Ag | Compuestos derivados de dihidropiridinas sustituidas; proceso de preparacion; compuestos intermediarios; composicion farmaceutica; proceso para producir la composicion farmaceutica; y uso en el tratamiento de una enfermedad mejorada con la inhibicion |
| EP2078020A4 (en) | 2007-04-10 | 2011-10-19 | Sgx Pharmaceuticals Inc | HETEROCYCLIC MODULATORS WITH FUSED CYCLES FOR KINASES |
| JP2010526078A (ja) | 2007-04-30 | 2010-07-29 | ジェネンテック, インコーポレイテッド | Wntシグナル伝達のピラゾールインヒビター |
| NZ581647A (en) | 2007-05-10 | 2012-02-24 | Avalon Pharmaceuticals | Derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine and uses thereof |
| US20080287452A1 (en) | 2007-05-16 | 2008-11-20 | Wyeth | Heteroaryl/aryl pyrimidine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system |
| WO2008147713A1 (en) | 2007-05-24 | 2008-12-04 | The Regents Of The University Of California | Wnt signaling inhibitors, and methods for making and using them |
| CL2008001540A1 (es) | 2007-05-29 | 2009-05-22 | Sgx Pharmaceuticals Inc | Compuestos derivados de pirrolopiridinas y pirazolopiridinas; composicion farmaceutica; y uso en el tratamiento del cancer. |
| WO2008150845A1 (en) | 2007-05-31 | 2008-12-11 | Vanderbilt University | Screening for wnt pathway modulators and pyrvinium for the treatment of cance |
| CN101790526A (zh) | 2007-06-08 | 2010-07-28 | 雅培制药有限公司 | 用作激酶抑制剂的5-杂芳基取代的吲唑化合物 |
| US8648069B2 (en) | 2007-06-08 | 2014-02-11 | Abbvie Inc. | 5-substituted indazoles as kinase inhibitors |
| EP2157859A4 (en) | 2007-06-19 | 2011-01-12 | Takeda Pharmaceutical | INDAZOL COMPOUNDS FOR THE ACTIVATION OF GLUCCOKINASE |
| FR2917735B1 (fr) | 2007-06-21 | 2009-09-04 | Sanofi Aventis Sa | Nouveaux indazoles substitutes, leur preparation et leur utilisation en therapeutique |
| US20090069288A1 (en) | 2007-07-16 | 2009-03-12 | Breinlinger Eric C | Novel therapeutic compounds |
| WO2009016072A2 (en) | 2007-08-02 | 2009-02-05 | Nerviano Medical Sciences S.R.L. | A morpholinyl anthracycline derivative combined with protein kinase inhibitors |
| JP2010537998A (ja) | 2007-08-27 | 2010-12-09 | ワイス・エルエルシー | イミダゾピリジン類似体、およびWnt−βカテニン細胞メッセージ伝達系のアゴニストとしてのその使用 |
| US9259399B2 (en) | 2007-11-07 | 2016-02-16 | Cornell University | Targeting CDK4 and CDK6 in cancer therapy |
| KR101061599B1 (ko) | 2008-12-05 | 2011-09-02 | 한국과학기술연구원 | 비정상 세포 성장 질환의 치료를 위한 단백질 키나아제 저해제인 신규 인다졸 유도체, 이의 약학적으로 허용가능한염 및 이를 유효성분으로 함유하는 약학적 조성물 |
| CN101440092B (zh) | 2008-12-25 | 2010-11-17 | 浙江大学 | 2-吲唑-4-氮杂吲哚-5-氨基衍生物及制备和应用 |
| US8637507B2 (en) | 2009-03-18 | 2014-01-28 | Merck Sharp & Dohme Corp. | Bicyclic compounds as inhibitors of diacylglycerol acyltransferase |
| EP2411001B1 (en) | 2009-03-23 | 2018-01-17 | Merck Sharp & Dohme Corp. | P2x3, receptor antagonists for treatment of pain |
| BR112012001532A2 (pt) | 2009-07-23 | 2019-09-24 | Univ Vanderbilt | "substituída azolesulfonamides benzoimid e indolesulfonamides substituído como potenciadores mglur4" |
| WO2011019648A1 (en) | 2009-08-10 | 2011-02-17 | Epitherix, Llc | Indazoles as wnt/b-catenin signaling pathway inhibitors and therapeutic uses thereof |
| ES2835553T3 (es) | 2009-08-10 | 2021-06-22 | Biosplice Therapeutics Inc | Inhibidores de indazol de la vía de señalización de Wnt y sus usos terapéuticos |
| WO2011050245A1 (en) | 2009-10-23 | 2011-04-28 | Yangbo Feng | Bicyclic heteroaryls as kinase inhibitors |
| CN102821607B (zh) * | 2009-12-21 | 2014-12-17 | 萨穆梅德有限公司 | 1H-吡唑并[3,4-b]吡啶及其治疗应用 |
| KR101779630B1 (ko) | 2009-12-21 | 2017-09-18 | 어레이 바이오파마 인크. | cFMS 억제제로서 치환된 N-(1H-인다졸-4-일)이미다조[1,2-a]피리딘-3-카복사미드 화합물 |
| NZ602773A (en) | 2010-04-06 | 2015-05-29 | Peter Maccallum Cancer Inst | Radioprotector compounds and methods |
| DE102010043379A1 (de) | 2010-11-04 | 2012-05-10 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 6-Fluor-1H-Pyrazolo[4,3-b]pyridine und ihre Verwendung |
| WO2012068589A2 (en) | 2010-11-19 | 2012-05-24 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| PT2663561E (pt) | 2011-01-13 | 2016-06-07 | Novartis Ag | Derivados heterocíclicos novos e sua utilização no tratamento de distúrbios neurológicos |
| US8889684B2 (en) | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| US9464065B2 (en) | 2011-03-24 | 2016-10-11 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
| JP2014509660A (ja) | 2011-04-01 | 2014-04-21 | ユニバーシティ・オブ・ユタ・リサーチ・ファウンデイション | PDK1キナーゼの阻害剤としての置換3−(1H−ベンゾ{d}イミダゾール−2−イル)−1H−インダゾール類似体 |
| RU2014105624A (ru) | 2011-08-12 | 2015-09-20 | Ф. Хоффманн-Ля Рош Аг | Соединения индазола, способ их применения и фармацевтическая композиция |
| WO2013024002A1 (en) | 2011-08-12 | 2013-02-21 | F. Hoffmann-La Roche Ag | PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE |
| EP2763990B1 (en) | 2011-09-01 | 2017-02-22 | F. Hoffmann-La Roche AG | Pyrrolopyrazine kinase inhibitors |
| HRP20190281T1 (hr) | 2011-09-14 | 2019-05-31 | Samumed, Llc | Indazol-3-karboksamidi i njihova uporaba kao inhibitora signalizacijskog puta wnt/b-katenin |
| WO2013113722A1 (en) | 2012-01-30 | 2013-08-08 | Universiteit Gent | Anti-invasive compounds |
| EP2827869A4 (en) | 2012-03-23 | 2015-09-23 | Dennis Brown | COMPOSITIONS AND METHODS FOR IMPROVING THE THERAPEUTIC BENEFIT OF INDIRUBIN AND ANALOGUE THEREOF, WITH MEISOINDIGO |
| PH12017500997A1 (en) | 2012-04-04 | 2018-02-19 | Samumed Llc | Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof |
| PL2770994T3 (pl) | 2012-05-04 | 2020-03-31 | Samumed, Llc | 1H-Pirazolo[3,4-b]pirydyny i ich zastosowania terapeutyczne |
| US9056874B2 (en) | 2012-05-04 | 2015-06-16 | Novartis Ag | Complement pathway modulators and uses thereof |
| EP2844651A1 (en) | 2012-05-04 | 2015-03-11 | Basf Se | Substituted pyrazole-containing compounds and their use as pesticides |
| EP2943198B1 (en) | 2013-01-08 | 2019-07-17 | Samumed, LLC | 3-(benzoimidazol-2-yl)-indazole inhibitors of the wnt signaling pathway and therapeutic uses thereof |
| US9327886B2 (en) | 2013-03-13 | 2016-05-03 | Bayer Healthcare Llc | Vial container with collar cap |
| MA39763A (fr) | 2014-03-20 | 2017-01-25 | Samumed Llc | Indazole-3-carboxamides 5-substitués, et préparation et utilisation de ceux-ci |
| WO2016040190A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040180A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040184A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-b]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040193A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-b]pyridine and therapeutic uses thereof |
| WO2016040188A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(3h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040182A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-1h-imidazo[4,5-c]pyridine and therapeutic uses thereof |
| US9538272B2 (en) | 2014-09-08 | 2017-01-03 | Apple Inc. | Acoustic mesh and methods of use for electronic devices |
| WO2016040181A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 3-(1h-imidazo[4,5-c]pyridin-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof |
| WO2016040185A1 (en) | 2014-09-08 | 2016-03-17 | Samumed, Llc | 2-(1h-indazol-3-yl)-3h-imidazo[4,5-b]pyridine and therapeutic uses thereof |
| US10350199B2 (en) | 2015-08-03 | 2019-07-16 | Samumed, Llc | 3-(1h-pyrrolo[2,3-b]pyridin-2-yl)-1h-indazoles and therapeutic uses thereof |
| KR20180080262A (ko) | 2015-11-06 | 2018-07-11 | 사뮤메드, 엘엘씨 | 골관절염의 치료 |
| ES2933109T3 (es) | 2016-06-01 | 2023-02-02 | Biosplice Therapeutics Inc | Proceso para preparar N-(5-(3-(7-(3-fluorofenil)-3h-imidazo[4,5-c]piridin-2-il)-1h-indazol-5-il)piridin-3-il)-3-metilbutanamida |
| CN110709082A (zh) | 2016-10-21 | 2020-01-17 | 萨穆梅德有限公司 | 吲唑-3-甲酰胺的使用方法及其作为Wnt/β-连环蛋白信号传导途径抑制剂的用途 |
| KR102558716B1 (ko) | 2016-11-07 | 2023-07-21 | 사뮤메드, 엘엘씨 | 단일-투여량, 즉시-사용가능한 주사용 제제 |
-
2014
- 2014-01-08 EP EP14737972.1A patent/EP2943198B1/en active Active
- 2014-01-08 US US14/149,948 patent/US9908867B2/en active Active
- 2014-01-08 MX MX2015008860A patent/MX370487B/es active IP Right Grant
- 2014-01-08 CA CA2897400A patent/CA2897400A1/en not_active Abandoned
- 2014-01-08 CN CN201480013031.9A patent/CN105120862A/zh active Pending
- 2014-01-08 JP JP2015551853A patent/JP6355648B2/ja active Active
- 2014-01-08 WO PCT/US2014/010607 patent/WO2014110086A2/en not_active Ceased
-
2018
- 2018-02-06 US US15/889,403 patent/US10183929B2/en active Active
-
2019
- 2019-01-18 US US16/252,055 patent/US10654832B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2016504387A5 (enExample) | ||
| JP2014526510A5 (enExample) | ||
| JP2015512443A5 (enExample) | ||
| JP2019514938A5 (enExample) | ||
| JP2015515989A5 (enExample) | ||
| RU2014144309A (ru) | Индазольные ингибиторы сигнального пути wnt и их терапевтические применения | |
| JP2017508763A5 (enExample) | ||
| ES2445526T3 (es) | Acetamidas con sustitución N-(hetero)aril, 2-(hetero)arilo para utilizar como moduladores de señalización de Wnt | |
| RU2014148773A (ru) | 1н-пиразоло[3,4-b]пиридины и их терапевтические применения | |
| RU2016141088A (ru) | 5-замещённые индазол-3-карбоксамиды и их получение и применение | |
| JP6414286B2 (ja) | ハロゲン置換へテロ環化合物 | |
| TW202128644A (zh) | 作為lpa受體拮抗劑之三唑胺基甲酸酯吡啶基磺醯胺及其用途 | |
| CA3073983C (en) | Lysophosphatidic acid receptor 1 (lpar1) inhibitor compounds | |
| ES2911040T3 (es) | Nuevos derivados de heteroaril amida como inhibidores selectivos de histona deacetilasa 1 y 2 (HDAC1/2) | |
| CA2761859A1 (en) | Aryl pyridine as aldosterone synthase inhibitors | |
| JP2014193925A5 (enExample) | ||
| JP2018531218A5 (enExample) | ||
| JP2016514100A5 (enExample) | ||
| KR20160127138A (ko) | 신규 화합물 | |
| JP5443975B2 (ja) | 新規なスルホンアミド誘導体またはその塩 | |
| CN104994851A (zh) | 作为crac通道抑制剂的基于吡唑基的甲酰胺i | |
| WO2014175832A1 (en) | Wnt pathway modulators | |
| KR20160127838A (ko) | Wnt 신호전달 경로 억제제 | |
| JP2017506267A5 (enExample) | ||
| CN104884058A (zh) | 作为crac通道抑制剂的基于吡唑基的甲酰胺ii |