JP2019530742A5 - - Google Patents
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- JP2019530742A5 JP2019530742A5 JP2019533314A JP2019533314A JP2019530742A5 JP 2019530742 A5 JP2019530742 A5 JP 2019530742A5 JP 2019533314 A JP2019533314 A JP 2019533314A JP 2019533314 A JP2019533314 A JP 2019533314A JP 2019530742 A5 JP2019530742 A5 JP 2019530742A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- compound according
- alkyl
- independently
- haloalkyl
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 55
- 125000000217 alkyl group Chemical group 0.000 claims description 23
- 206010028980 Neoplasm Diseases 0.000 claims description 21
- 201000011510 cancer Diseases 0.000 claims description 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 19
- 125000001188 haloalkyl group Chemical group 0.000 claims description 17
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 15
- 125000005843 halogen group Chemical group 0.000 claims description 14
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 13
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 11
- 201000010099 disease Diseases 0.000 claims description 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 11
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 11
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims description 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 8
- 230000002496 gastric effect Effects 0.000 claims description 8
- 239000001257 hydrogen Substances 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 7
- 201000001320 Atherosclerosis Diseases 0.000 claims description 6
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 6
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 6
- 150000002431 hydrogen Chemical group 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 6
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims description 5
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims description 5
- 125000003342 alkenyl group Chemical group 0.000 claims description 5
- 201000010175 gallbladder cancer Diseases 0.000 claims description 5
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 5
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 5
- 206010052747 Adenocarcinoma pancreas Diseases 0.000 claims description 4
- 206010061424 Anal cancer Diseases 0.000 claims description 4
- 208000007860 Anus Neoplasms Diseases 0.000 claims description 4
- 208000003950 B-cell lymphoma Diseases 0.000 claims description 4
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 4
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 4
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims description 4
- 206010020772 Hypertension Diseases 0.000 claims description 4
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 4
- 208000017170 Lipid metabolism 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
- 208000008589 Obesity Diseases 0.000 claims description 4
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 4
- 201000011165 anus cancer Diseases 0.000 claims description 4
- 210000004252 chorionic villi Anatomy 0.000 claims description 4
- 208000029742 colonic neoplasm Diseases 0.000 claims description 4
- 230000001079 digestive effect Effects 0.000 claims description 4
- 230000004064 dysfunction Effects 0.000 claims description 4
- 201000004101 esophageal cancer Diseases 0.000 claims description 4
- 201000010536 head and neck cancer Diseases 0.000 claims description 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 4
- 230000002489 hematologic effect Effects 0.000 claims description 4
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 201000010982 kidney cancer Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 235000020824 obesity Nutrition 0.000 claims description 4
- 201000008968 osteosarcoma Diseases 0.000 claims description 4
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 claims description 4
- -1 pyridinonyl Chemical group 0.000 claims description 4
- 206010038038 rectal cancer Diseases 0.000 claims description 4
- 201000001275 rectum cancer Diseases 0.000 claims description 4
- 201000000849 skin cancer Diseases 0.000 claims description 4
- 230000004580 weight loss Effects 0.000 claims description 4
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 claims description 3
- 201000007455 central nervous system cancer Diseases 0.000 claims description 3
- 201000002313 intestinal cancer Diseases 0.000 claims description 3
- 231100000240 steatosis hepatitis Toxicity 0.000 claims description 3
- 206010004593 Bile duct cancer Diseases 0.000 claims description 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 2
- 206010014476 Elevated cholesterol Diseases 0.000 claims description 2
- 206010014486 Elevated triglycerides Diseases 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims description 2
- 208000001748 Hyperlipoproteinemia Type V Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 102000004895 Lipoproteins Human genes 0.000 claims description 2
- 108090001030 Lipoproteins Proteins 0.000 claims description 2
- 208000018262 Peripheral vascular disease Diseases 0.000 claims description 2
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 102000009822 Sterol Regulatory Element Binding Proteins Human genes 0.000 claims description 2
- 108010020396 Sterol Regulatory Element Binding Proteins Proteins 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 230000004913 activation Effects 0.000 claims description 2
- 230000001476 alcoholic effect Effects 0.000 claims description 2
- 210000000941 bile Anatomy 0.000 claims description 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 2
- 210000004027 cell Anatomy 0.000 claims description 2
- 208000026106 cerebrovascular disease Diseases 0.000 claims description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 2
- 208000029078 coronary artery disease Diseases 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 230000006372 lipid accumulation Effects 0.000 claims description 2
- 208000030159 metabolic disease Diseases 0.000 claims description 2
- 208000010125 myocardial infarction Diseases 0.000 claims description 2
- 230000007935 neutral effect Effects 0.000 claims description 2
- 230000037361 pathway Effects 0.000 claims description 2
- 201000002511 pituitary cancer Diseases 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 230000007863 steatosis Effects 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 210000001519 tissue Anatomy 0.000 claims description 2
- 150000003626 triacylglycerols Chemical class 0.000 claims description 2
- 206010073360 Appendix cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010045261 Type IIa hyperlipidaemia Diseases 0.000 claims 1
- 208000021780 appendiceal neoplasm Diseases 0.000 claims 1
- 201000005577 familial hyperlipidemia Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 201000002314 small intestine cancer Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 description 8
- 238000000034 method Methods 0.000 description 4
- 125000001309 chloro group Chemical group Cl* 0.000 description 2
- 125000001153 fluoro group Chemical group F* 0.000 description 2
- 206010059183 Familial hypertriglyceridaemia Diseases 0.000 description 1
- 208000004930 Fatty Liver Diseases 0.000 description 1
- 206010019708 Hepatic steatosis Diseases 0.000 description 1
- 206010039491 Sarcoma Diseases 0.000 description 1
- 208000009956 adenocarcinoma Diseases 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 208000010706 fatty liver disease Diseases 0.000 description 1
- 208000000522 hyperlipoproteinemia type IV Diseases 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662384661P | 2016-09-07 | 2016-09-07 | |
| US62/384,661 | 2016-09-07 | ||
| US201662438944P | 2016-12-23 | 2016-12-23 | |
| US62/438,944 | 2016-12-23 | ||
| PCT/US2017/050562 WO2018049080A1 (en) | 2016-09-07 | 2017-09-07 | Di-substituted pyrazole compounds for the treatment of diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019530742A JP2019530742A (ja) | 2019-10-24 |
| JP2019530742A5 true JP2019530742A5 (https=) | 2021-01-28 |
| JP7071981B2 JP7071981B2 (ja) | 2022-05-19 |
Family
ID=59895438
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019533314A Active JP7071981B2 (ja) | 2016-09-07 | 2017-09-07 | 疾患の治療のための二置換ピラゾール化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11339142B2 (https=) |
| EP (1) | EP3510027B1 (https=) |
| JP (1) | JP7071981B2 (https=) |
| CN (1) | CN110072861B (https=) |
| AU (1) | AU2017323521B9 (https=) |
| ES (1) | ES2932187T3 (https=) |
| WO (1) | WO2018049080A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10328064B2 (en) | 2014-12-23 | 2019-06-25 | Fgh Biotech, Inc. | Compositions of fatostatin based heterocyclic compounds and uses thereof |
| KR102498741B1 (ko) * | 2016-04-29 | 2023-02-10 | 에프지에이치 바이오테크 인코포레이티드 | 질환 치료용 이-치환된 피라졸 화합물 |
| ES2932187T3 (es) | 2016-09-07 | 2023-01-16 | Fgh Biotech Inc | Compuestos de pirazol disustituidos para el tratamiento de enfermedades |
| CN108947839A (zh) * | 2018-06-28 | 2018-12-07 | 山东润博生物科技有限公司 | 一种苯氧羧酸类除草剂的制备方法 |
| CN108947841A (zh) * | 2018-06-28 | 2018-12-07 | 山东润博生物科技有限公司 | 一种苯氧羧酸酯的制备方法 |
| CN109265352B (zh) * | 2018-10-31 | 2021-06-04 | 杭州迈世腾药物科技有限公司 | 芳基环丙基醚及其衍生物的制备方法 |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| WO2020132700A1 (en) | 2018-12-21 | 2020-06-25 | Fgh Biotech Inc. | Methods of using inhibitors of srebp in combination with niclosamide and analogs thereof |
| EP4096659A4 (en) * | 2020-01-27 | 2023-10-18 | Capulus Therapeutics, LLC | Srebp inhibitors comprising a thiophene central ring |
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| CN105294584A (zh) | 2015-11-30 | 2016-02-03 | 中国医科大学 | 1-取代苯基-1h-1,2,3-三唑类化合物、制备方法及其用途 |
| KR102498741B1 (ko) | 2016-04-29 | 2023-02-10 | 에프지에이치 바이오테크 인코포레이티드 | 질환 치료용 이-치환된 피라졸 화합물 |
| ES2932187T3 (es) | 2016-09-07 | 2023-01-16 | Fgh Biotech Inc | Compuestos de pirazol disustituidos para el tratamiento de enfermedades |
-
2017
- 2017-09-07 ES ES17768620T patent/ES2932187T3/es active Active
- 2017-09-07 WO PCT/US2017/050562 patent/WO2018049080A1/en not_active Ceased
- 2017-09-07 JP JP2019533314A patent/JP7071981B2/ja active Active
- 2017-09-07 EP EP17768620.1A patent/EP3510027B1/en active Active
- 2017-09-07 CN CN201780062738.2A patent/CN110072861B/zh active Active
- 2017-09-07 US US16/331,505 patent/US11339142B2/en active Active
- 2017-09-07 AU AU2017323521A patent/AU2017323521B9/en active Active
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