JP2014515346A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014515346A5 JP2014515346A5 JP2014510888A JP2014510888A JP2014515346A5 JP 2014515346 A5 JP2014515346 A5 JP 2014515346A5 JP 2014510888 A JP2014510888 A JP 2014510888A JP 2014510888 A JP2014510888 A JP 2014510888A JP 2014515346 A5 JP2014515346 A5 JP 2014515346A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- alkyl
- optionally substituted
- compound
- pharmaceutically acceptable
- 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 26
- 150000001875 compounds Chemical class 0.000 claims 26
- 125000001424 substituent group Chemical group 0.000 claims 19
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 206010028980 Neoplasm Diseases 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 229910052799 carbon Inorganic materials 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 150000001408 amides Chemical class 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 11
- 150000002148 esters Chemical class 0.000 claims 11
- 125000005843 halogen group Chemical group 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 10
- 201000011510 cancer Diseases 0.000 claims 9
- 239000002671 adjuvant Substances 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 7
- 239000003085 diluting agent Substances 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 229910052721 tungsten Inorganic materials 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 239000013066 combination product Substances 0.000 claims 4
- 229940127555 combination product Drugs 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 230000002062 proliferating effect Effects 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 125000002015 acyclic group Chemical group 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 230000005764 inhibitory process Effects 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000020084 Bone disease Diseases 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 102000042867 PIM family Human genes 0.000 claims 2
- 108091082273 PIM family Proteins 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 2
- 201000010208 Seminoma Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 2
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 210000000214 mouth Anatomy 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 210000003800 pharynx Anatomy 0.000 claims 2
- 238000002360 preparation method Methods 0.000 claims 2
- 206010038038 rectal cancer Diseases 0.000 claims 2
- 201000001275 rectum cancer Diseases 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 239000011593 sulfur Chemical group 0.000 claims 2
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- -1 —OR s1 Chemical group 0.000 claims 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 1
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 1
- 208000012124 AIDS-related disease Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 1
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 208000010667 Carcinoma of liver and intrahepatic biliary tract Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010073069 Hepatic cancer Diseases 0.000 claims 1
- 206010019842 Hepatomegaly Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 206010062016 Immunosuppression Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 206010023825 Laryngeal cancer Diseases 0.000 claims 1
- 208000018501 Lymphatic disease Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000009905 Neurofibromatoses Diseases 0.000 claims 1
- 208000031481 Pathologic Constriction Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 230000006044 T cell activation Effects 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 201000001531 bladder carcinoma Diseases 0.000 claims 1
- 201000000220 brain stem cancer Diseases 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 150000001733 carboxylic acid esters Chemical class 0.000 claims 1
- 230000030833 cell death Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 238000011260 co-administration Methods 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 230000001066 destructive effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 230000002124 endocrine Effects 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 230000001506 immunosuppresive effect Effects 0.000 claims 1
- 208000033065 inborn errors of immunity Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000002429 large intestine Anatomy 0.000 claims 1
- 201000011061 large intestine cancer Diseases 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 210000000088 lip Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 201000002250 liver carcinoma Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 208000018555 lymphatic system disease Diseases 0.000 claims 1
- 210000004698 lymphocyte Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 208000007538 neurilemmoma Diseases 0.000 claims 1
- 201000004931 neurofibromatosis Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000010198 papillary carcinoma Diseases 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 208000015768 polyposis Diseases 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 208000028529 primary immunodeficiency disease Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 201000010174 renal carcinoma Diseases 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims 1
- 230000036262 stenosis Effects 0.000 claims 1
- 208000037804 stenosis Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 210000001550 testis Anatomy 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000002105 tongue Anatomy 0.000 claims 1
- 208000010576 undifferentiated carcinoma Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 208000010570 urinary bladder carcinoma Diseases 0.000 claims 1
- 210000004509 vascular smooth muscle cell Anatomy 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11382158.1 | 2011-05-19 | ||
| EP11382158 | 2011-05-19 | ||
| EP12275024.3 | 2012-03-09 | ||
| EP12275024 | 2012-03-09 | ||
| PCT/GB2012/051134 WO2012156756A2 (en) | 2011-05-19 | 2012-05-18 | New compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014515346A JP2014515346A (ja) | 2014-06-30 |
| JP2014515346A5 true JP2014515346A5 (enExample) | 2015-05-07 |
| JP5997763B2 JP5997763B2 (ja) | 2016-09-28 |
Family
ID=46796665
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014510888A Active JP5997763B2 (ja) | 2011-05-19 | 2012-05-18 | タンパク質キナーゼ阻害剤としての大環状化合物 |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US9284334B2 (enExample) |
| EP (1) | EP2710018B8 (enExample) |
| JP (1) | JP5997763B2 (enExample) |
| KR (1) | KR101953210B1 (enExample) |
| CN (1) | CN103748099B (enExample) |
| AU (1) | AU2012257513B2 (enExample) |
| BR (1) | BR112013029711B1 (enExample) |
| CA (1) | CA2872979C (enExample) |
| DK (1) | DK2710018T3 (enExample) |
| ES (1) | ES2907071T3 (enExample) |
| HR (1) | HRP20220319T1 (enExample) |
| MX (1) | MX349366B (enExample) |
| NZ (1) | NZ618157A (enExample) |
| PH (1) | PH12013502400A1 (enExample) |
| PL (1) | PL2710018T3 (enExample) |
| PT (1) | PT2710018T (enExample) |
| RU (1) | RU2598840C2 (enExample) |
| SG (1) | SG11201400681UA (enExample) |
| WO (1) | WO2012156756A2 (enExample) |
| ZA (1) | ZA201309128B (enExample) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9428845B1 (en) | 2010-12-28 | 2016-08-30 | Warp Drive Bio, Inc. | Identifying new therapeutic agents |
| US9284334B2 (en) | 2011-05-19 | 2016-03-15 | Fundación Centro Nacional De Investigaciones Oncologicas Carlos Iii | Macrocyclic compounds as protein kinase inhibitors |
| ES2583477T3 (es) | 2011-09-30 | 2016-09-21 | Ipsen Pharma S.A.S. | Inhibidores macrocíclicos de cinasa de LRRK2 |
| CN103788071A (zh) * | 2012-11-01 | 2014-05-14 | 中国人民解放军第二军医大学 | N-(5-(喹啉-6-基)吡啶-3-基)苯磺酰胺衍生物、制备方法及治疗用途 |
| TWI574962B (zh) | 2012-11-14 | 2017-03-21 | 加拓科學公司 | 作爲pi3激酶調節劑的芳雜環化合物及其使用方法和用途 |
| EP2943485B1 (en) | 2013-01-14 | 2017-09-20 | Incyte Holdings Corporation | Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors |
| HUE050215T2 (hu) | 2013-01-15 | 2020-11-30 | Incyte Holdings Corp | Pim kináz inhibitorokként hasznos tiazolkarboxamid és piridinkarboxamid vegyületek |
| BR112015018318A2 (pt) * | 2013-02-21 | 2017-08-22 | Sunshine Lake Pharma Co Ltd | Composto, composição farmacêutica, uso de um composto ou de uma composição farmacêutica, e, métodos para prevenir, gerenciar, tratar ou diminuir a severidade de um distúrbio proliferativo em um paciente e para inibir ou modular a atividade de uma proteína quinase em uma amostra biológica |
| EP2970297A1 (en) * | 2013-03-14 | 2016-01-20 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| RU2015155595A (ru) * | 2013-06-06 | 2017-07-14 | Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед | Ингибиторы энхансера zeste гомолога 2 область техники, к которой относится изобретение |
| CN104341299B (zh) * | 2013-07-29 | 2016-08-24 | 漳州金富顺生物科技有限公司 | 一种脱臭脂肪酸的酯化 |
| TW201605866A (zh) | 2013-08-23 | 2016-02-16 | 英塞特公司 | 可用作pim激酶抑制劑之呋喃并-及噻吩并-吡啶甲醯胺化合物 |
| CN104418853B (zh) * | 2013-08-28 | 2016-09-07 | 北大方正集团有限公司 | 取代的萘啶-2-酮化合物、制备方法、用途及药物组合物 |
| TW201542550A (zh) * | 2013-09-06 | 2015-11-16 | Lexicon Pharmaceuticals Inc | 吡唑并[1,5-a]嘧啶基化合物、包含彼之組合物以及使用彼之方法 |
| AR097543A1 (es) * | 2013-09-06 | 2016-03-23 | Lexicon Pharmaceuticals Inc | COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO |
| WO2015106158A1 (en) * | 2014-01-09 | 2015-07-16 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| CN105693744B (zh) * | 2014-11-27 | 2018-06-19 | 北大方正集团有限公司 | 一种取代的噻吩并嘧啶化合物及其制备方法 |
| WO2016112295A1 (en) | 2015-01-09 | 2016-07-14 | Warp Drive Bio, Inc. | Compounds that participate in cooperative binding and uses thereof |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| CN104961725B (zh) * | 2015-06-18 | 2017-04-19 | 浙江大学 | 4‑α,β不饱和酰胺基喹啉类化合物及制备和应用 |
| CN106467545B (zh) * | 2015-08-20 | 2018-10-16 | 北大方正集团有限公司 | 一种噻吩并嘧啶化合物 |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Pim激酶抑制劑之鹽 |
| EP4242304A3 (en) | 2015-10-01 | 2024-02-07 | Revolution Medicines, Inc. | Methods and reagents for analyzing protein-protein interfaces |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| SG11201804901WA (en) | 2015-12-22 | 2018-07-30 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| MX386103B (es) * | 2016-04-22 | 2025-03-18 | Astrazeneca Ab | Inhibidores de mcl-1 y metodos de uso de los mismos. |
| WO2017197151A1 (en) * | 2016-05-11 | 2017-11-16 | Emory University | Phosphotidylinositol 3-kinase inhibitors |
| JP2019519593A (ja) * | 2016-07-06 | 2019-07-11 | ザ・リージェンツ・オブ・ザ・ユニバーシティ・オブ・ミシガンThe Regents Of The University Of Michigan | MEK/PI3K及びmTOR/MEK/PI3K生物学的経路の多官能性阻害剤、並びに同多官能性阻害剤を用いた治療方法 |
| US11352328B2 (en) | 2016-07-12 | 2022-06-07 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus |
| RU2019105587A (ru) * | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
| WO2018167713A1 (en) | 2017-03-16 | 2018-09-20 | Waters Technologies Corporation | Chromatographic compositions |
| CA3066939A1 (en) | 2017-06-21 | 2018-12-27 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| TW201920193A (zh) * | 2017-08-15 | 2019-06-01 | 美商艾伯維有限公司 | 大環mel-1抑制劑以及使用方法 |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| ES2950825T3 (es) * | 2018-08-24 | 2023-10-13 | Bayer Ag | Procedimiento para preparar 2-[(3R)-3--metilmofolin--4-il]-4-(1-metil-1H-pirazol-5-il)-8-(1H-pirazol-5-il)-1,7-naftiridina |
| SG11202104609SA (en) | 2018-11-09 | 2021-06-29 | Shandong Xuanzhu Pharma Co Ltd | Macrocyclic tyrosine kinase inhibitor and uses thereof |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
| WO2020132071A1 (en) | 2018-12-19 | 2020-06-25 | Shy Therapeutics. Llc | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and f1brotic disease |
| CN113874015B (zh) | 2018-12-21 | 2024-05-24 | 细胞基因公司 | Ripk2的噻吩并吡啶抑制剂 |
| BR112021012057A2 (pt) * | 2018-12-21 | 2021-10-19 | Revolution Medicines, Inc. | Compostos que participam de ligação cooperativa e usos dos mesmos |
| CN109988165B (zh) * | 2018-12-24 | 2022-10-25 | 华东师范大学 | 作为PI3K/mTOR激酶调节剂芳杂环化合物及其制备方法和应用 |
| CA3160142A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2021091967A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| CN115894606A (zh) | 2019-11-04 | 2023-04-04 | 锐新医药公司 | Ras抑制剂 |
| US20230158153A1 (en) * | 2020-04-09 | 2023-05-25 | Purdue Research Foundation | Pi3 kinase inhibitors and uses thereof |
| EP4148055A4 (en) * | 2020-05-08 | 2023-10-11 | Shandong Xuanzhu Pharma Co., Ltd. | CRYSTAL FORM OF A MACROCYCLIC TYROSINE KINASE INHIBITOR AND PROCESS FOR PRODUCTION THEREOF |
| CN113620976B (zh) * | 2020-05-09 | 2023-09-26 | 中国医学科学院药物研究所 | 噻唑并嘧啶类化合物及其制备方法、用途和药物组合物 |
| EP4167982A4 (en) | 2020-06-22 | 2024-08-07 | PMV Pharmaceuticals, Inc. | METHODS AND COMPOUNDS FOR RESTORING FUNCTION OF P53 MUTANTS |
| KR20230067635A (ko) | 2020-09-15 | 2023-05-16 | 레볼루션 메디슨즈, 인크. | 암의 치료에서 ras 억제제로서 인돌 유도체 |
| CN118852330A (zh) | 2021-05-05 | 2024-10-29 | 锐新医药公司 | 用于治疗癌症的ras抑制剂 |
| CN113416181B (zh) * | 2021-08-02 | 2022-05-03 | 四川大学 | 喹唑啉类衍生物及其用途 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CN116262758B (zh) * | 2021-12-15 | 2025-02-28 | 上海博悦生物科技有限公司 | 7-甲基噻唑并[5,4-d]嘧啶类化合物、制备方法及其用途 |
| WO2025061125A1 (zh) * | 2023-09-22 | 2025-03-27 | 四川汇宇制药股份有限公司 | 一种大环化合物及其制备方法和用途 |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1147478A (en) | 1914-11-03 | 1915-07-20 | Charles H Barker | War-maneuvering game. |
| US5583024A (en) | 1985-12-02 | 1996-12-10 | The Regents Of The University Of California | Recombinant expression of Coleoptera luciferase |
| FR2601675B1 (fr) | 1986-07-17 | 1988-09-23 | Rhone Poulenc Sante | Derives du taxol, leur preparation et les compositions pharmaceutiques qui les contiennent |
| US5698582A (en) | 1991-07-08 | 1997-12-16 | Rhone-Poulenc Rorer S.A. | Compositions containing taxane derivatives |
| US5714512A (en) | 1991-07-08 | 1998-02-03 | Rhone-Poulenc Rorer, S.A. | Compositions containing taxane derivatives |
| US5750561A (en) | 1991-07-08 | 1998-05-12 | Rhone-Poulenc Rorer, S.A. | Compositions containing taxane derivatives |
| FR2698543B1 (fr) | 1992-12-02 | 1994-12-30 | Rhone Poulenc Rorer Sa | Nouvelles compositions à base de taxoides. |
| JPH08336393A (ja) | 1995-04-13 | 1996-12-24 | Mitsubishi Chem Corp | 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法 |
| WO1997018207A2 (en) | 1995-11-14 | 1997-05-22 | The Du Pont Merck Pharmaceutical Company | Novel macrocyclic compounds as metalloprotease inhibitors |
| US6602677B1 (en) | 1997-09-19 | 2003-08-05 | Promega Corporation | Thermostable luciferases and methods of production |
| RS49779B (sr) | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
| AU5783300A (en) | 1999-07-09 | 2001-01-30 | Glaxo Group Limited | Anilinoquinazolines as protein tyrosine kinase inhibitors |
| US6933299B1 (en) | 1999-07-09 | 2005-08-23 | Smithkline Beecham Corporation | Anilinoquinazolines as protein tyrosine kinase inhibitors |
| KR100815681B1 (ko) | 2000-06-30 | 2008-03-20 | 글락소 그룹 리미티드 | 퀴나졸린 디토실레이트 염 화합물 |
| EE05450B1 (et) | 2000-07-19 | 2011-08-15 | Warner-Lambert Company | 4-jodofenlaminobenshdroksaamhapete oksgeenitud estrid, nende kristallvormid ja farmatseutilised kompositsioonid ning kasutamine |
| ATE290882T1 (de) | 2001-01-16 | 2005-04-15 | Glaxo Group Ltd | Pharmazeutische mischung gegen krebs, die ein 4- chinazolinamin in kombination mit paclitaxel, carboplatin or vinorelbine enthält |
| NZ518726A (en) | 2001-05-09 | 2004-06-25 | Warner Lambert Co | Method of treating or inhibiting neutrophil chemotaxis by administering a mek inhibitor |
| DE10239042A1 (de) * | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| MXPA05003431A (es) | 2002-11-15 | 2005-07-05 | Warner Lambert Co | Quimioterapia de combinacion. |
| KR101013932B1 (ko) | 2003-10-21 | 2011-02-14 | 워너-램버트 캄파니 엘엘씨 | N-[(r)-2,3-디히드록시-프로폭시]-3,4-디플루오로-2-(2-플루오로-4-요오도페닐아미노)-벤자미드 다형체 형태 |
| HRP20110498T1 (hr) | 2005-10-07 | 2011-08-31 | Exelixis | Azetidini kao inhibitori mek za liječenje proliferativnih bolesti |
| KR20090089849A (ko) * | 2006-10-27 | 2009-08-24 | 얀센 파마슈티카 엔.브이. | Vegfr3 저해제로서의 마크로사이클릭 퀴나졸린 유도체 |
| JP2010529031A (ja) | 2007-05-29 | 2010-08-26 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Pi3キナーゼ阻害剤としてのナフチリジン誘導体 |
| CN101878219B (zh) | 2007-09-27 | 2014-04-02 | 西班牙国家癌症研究中心 | 用于作为蛋白激酶抑制剂使用的咪唑并噻二唑类 |
| JP2011500823A (ja) * | 2007-10-22 | 2011-01-06 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Pi3キナーゼ阻害物質としてのピリドスルホンアミド誘導体 |
| US8815872B2 (en) * | 2008-09-08 | 2014-08-26 | Merck Patent Gmbh | Macrocyclics pyrimidines as aurora kinase inhibitors |
| US8765727B2 (en) * | 2009-01-23 | 2014-07-01 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| EP2405916B1 (en) | 2009-03-12 | 2018-02-07 | Genentech, Inc. | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents for the treatment of hematopoietic malignancies |
| MX2011009796A (es) * | 2009-03-20 | 2011-12-14 | Amgen Inc | Inhibidores de la cinasa pi3. |
| HUE027964T2 (en) | 2009-04-02 | 2016-11-28 | Fund Centro Nac De Investig Oncologicas Carlos Iii | Imidazo [2,1-b] [1,3,4] thiadiazole derivatives |
| UA111579C2 (uk) | 2009-08-17 | 2016-05-25 | Інтеллікіне Ллк | ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ |
| US9284334B2 (en) | 2011-05-19 | 2016-03-15 | Fundación Centro Nacional De Investigaciones Oncologicas Carlos Iii | Macrocyclic compounds as protein kinase inhibitors |
| WO2013001310A1 (en) | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
-
2012
- 2012-05-18 US US14/118,009 patent/US9284334B2/en active Active
- 2012-05-18 JP JP2014510888A patent/JP5997763B2/ja active Active
- 2012-05-18 EP EP12754044.1A patent/EP2710018B8/en active Active
- 2012-05-18 PL PL12754044T patent/PL2710018T3/pl unknown
- 2012-05-18 ES ES12754044T patent/ES2907071T3/es active Active
- 2012-05-18 CA CA2872979A patent/CA2872979C/en active Active
- 2012-05-18 PT PT127540441T patent/PT2710018T/pt unknown
- 2012-05-18 DK DK12754044.1T patent/DK2710018T3/da active
- 2012-05-18 RU RU2013156361/04A patent/RU2598840C2/ru active
- 2012-05-18 MX MX2013013462A patent/MX349366B/es active IP Right Grant
- 2012-05-18 SG SG11201400681UA patent/SG11201400681UA/en unknown
- 2012-05-18 BR BR112013029711-5A patent/BR112013029711B1/pt active IP Right Grant
- 2012-05-18 PH PH1/2013/502400A patent/PH12013502400A1/en unknown
- 2012-05-18 NZ NZ618157A patent/NZ618157A/en unknown
- 2012-05-18 HR HRP20220319TT patent/HRP20220319T1/hr unknown
- 2012-05-18 CN CN201280024265.4A patent/CN103748099B/zh active Active
- 2012-05-18 KR KR1020137033694A patent/KR101953210B1/ko active Active
- 2012-05-18 WO PCT/GB2012/051134 patent/WO2012156756A2/en not_active Ceased
- 2012-05-18 AU AU2012257513A patent/AU2012257513B2/en active Active
-
2013
- 2013-12-04 ZA ZA2013/09128A patent/ZA201309128B/en unknown
-
2016
- 2016-01-26 US US15/006,755 patent/US9808466B2/en active Active