JP2019515956A5 - - Google Patents
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- JP2019515956A5 JP2019515956A5 JP2019508167A JP2019508167A JP2019515956A5 JP 2019515956 A5 JP2019515956 A5 JP 2019515956A5 JP 2019508167 A JP2019508167 A JP 2019508167A JP 2019508167 A JP2019508167 A JP 2019508167A JP 2019515956 A5 JP2019515956 A5 JP 2019515956A5
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- JP
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- Prior art keywords
- cancer
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- alkyl
- chemical formula
- 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.)
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- 150000001875 compounds Chemical class 0.000 description 35
- 239000000126 substance Substances 0.000 description 13
- 125000000217 alkyl group Chemical group 0.000 description 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 9
- 125000001188 haloalkyl group Chemical group 0.000 description 9
- 229910052739 hydrogen Inorganic materials 0.000 description 7
- 239000001257 hydrogen Substances 0.000 description 7
- 201000010099 disease Diseases 0.000 description 6
- 125000005843 halogen group Chemical group 0.000 description 6
- 150000003839 salts Chemical class 0.000 description 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 5
- 125000000753 cycloalkyl group Chemical group 0.000 description 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 5
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 description 5
- 150000002431 hydrogen Chemical class 0.000 description 5
- 229910052757 nitrogen Inorganic materials 0.000 description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 5
- 125000004076 pyridyl group Chemical group 0.000 description 5
- 206010028980 Neoplasm Diseases 0.000 description 4
- 201000011510 cancer Diseases 0.000 description 4
- -1 pyridinonyl Chemical group 0.000 description 4
- 201000001320 Atherosclerosis Diseases 0.000 description 3
- 208000031226 Hyperlipidaemia Diseases 0.000 description 3
- 208000001145 Metabolic Syndrome Diseases 0.000 description 3
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 description 3
- 125000003342 alkenyl group Chemical group 0.000 description 3
- 208000035475 disorder Diseases 0.000 description 3
- 230000002496 gastric effect Effects 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 3
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 3
- 230000004580 weight loss Effects 0.000 description 3
- 206010052747 Adenocarcinoma pancreas Diseases 0.000 description 2
- 206010061424 Anal cancer Diseases 0.000 description 2
- 208000007860 Anus Neoplasms Diseases 0.000 description 2
- 206010073360 Appendix cancer Diseases 0.000 description 2
- 208000003950 B-cell lymphoma Diseases 0.000 description 2
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 description 2
- 206010004593 Bile duct cancer Diseases 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 2
- 208000026310 Breast neoplasm Diseases 0.000 description 2
- 206010007279 Carcinoid tumour of the gastrointestinal tract Diseases 0.000 description 2
- 208000006332 Choriocarcinoma Diseases 0.000 description 2
- 206010009944 Colon cancer Diseases 0.000 description 2
- 208000031288 Combined hyperlipidaemia Diseases 0.000 description 2
- 208000032928 Dyslipidaemia Diseases 0.000 description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 description 2
- 208000022072 Gallbladder Neoplasms Diseases 0.000 description 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 description 2
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 description 2
- 201000010915 Glioblastoma multiforme Diseases 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 206010020772 Hypertension Diseases 0.000 description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 2
- 206010025323 Lymphomas Diseases 0.000 description 2
- 208000008589 Obesity Diseases 0.000 description 2
- 206010033128 Ovarian cancer Diseases 0.000 description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 description 2
- 206010060862 Prostate cancer Diseases 0.000 description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 2
- 208000015634 Rectal Neoplasms Diseases 0.000 description 2
- 206010038389 Renal cancer Diseases 0.000 description 2
- 208000000453 Skin Neoplasms Diseases 0.000 description 2
- 201000011165 anus cancer Diseases 0.000 description 2
- 208000021780 appendiceal neoplasm Diseases 0.000 description 2
- 208000026900 bile duct neoplasm Diseases 0.000 description 2
- 201000007455 central nervous system cancer Diseases 0.000 description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 description 2
- 208000029742 colonic neoplasm Diseases 0.000 description 2
- 125000004093 cyano group Chemical group *C#N 0.000 description 2
- 230000004064 dysfunction Effects 0.000 description 2
- 201000004101 esophageal cancer Diseases 0.000 description 2
- 201000010175 gallbladder cancer Diseases 0.000 description 2
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 description 2
- 208000005017 glioblastoma Diseases 0.000 description 2
- 201000010536 head and neck cancer Diseases 0.000 description 2
- 208000014829 head and neck neoplasm Diseases 0.000 description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 2
- 201000010982 kidney cancer Diseases 0.000 description 2
- 201000005202 lung cancer Diseases 0.000 description 2
- 208000020816 lung neoplasm Diseases 0.000 description 2
- 235000020824 obesity Nutrition 0.000 description 2
- 201000008968 osteosarcoma Diseases 0.000 description 2
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 125000003373 pyrazinyl group Chemical group 0.000 description 2
- 125000002098 pyridazinyl group Chemical group 0.000 description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 description 2
- 206010038038 rectal cancer Diseases 0.000 description 2
- 201000001275 rectum cancer Diseases 0.000 description 2
- 201000000849 skin cancer Diseases 0.000 description 2
- 201000002314 small intestine cancer Diseases 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- VGDOAPMJMIKSHQ-UHFFFAOYSA-N 6-(1-phenylpyrazol-4-yl)-n-propylpyridazin-3-amine Chemical compound N1=NC(NCCC)=CC=C1C1=CN(C=2C=CC=CC=2)N=C1 VGDOAPMJMIKSHQ-UHFFFAOYSA-N 0.000 description 1
- 0 CC1(C)N=C(*)N=CC(C)=C1 Chemical compound CC1(C)N=C(*)N=CC(C)=C1 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 description 1
- 206010014476 Elevated cholesterol Diseases 0.000 description 1
- 206010014486 Elevated triglycerides Diseases 0.000 description 1
- 201000001376 Familial Combined Hyperlipidemia Diseases 0.000 description 1
- 206010059183 Familial hypertriglyceridaemia Diseases 0.000 description 1
- 208000004930 Fatty Liver Diseases 0.000 description 1
- 206010019708 Hepatic steatosis Diseases 0.000 description 1
- 208000035150 Hypercholesterolemia Diseases 0.000 description 1
- 208000001748 Hyperlipoproteinemia Type V Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 102000004895 Lipoproteins Human genes 0.000 description 1
- 108090001030 Lipoproteins Proteins 0.000 description 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 1
- 208000018262 Peripheral vascular disease Diseases 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 102000009822 Sterol Regulatory Element Binding Proteins Human genes 0.000 description 1
- 108010020396 Sterol Regulatory Element Binding Proteins Proteins 0.000 description 1
- 230000001594 aberrant effect Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 208000029078 coronary artery disease Diseases 0.000 description 1
- 208000033679 diabetic kidney disease Diseases 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 208000016097 disease of metabolism Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 208000010706 fatty liver disease Diseases 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 201000005787 hematologic cancer Diseases 0.000 description 1
- 230000002489 hematologic effect Effects 0.000 description 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 description 1
- 208000000522 hyperlipoproteinemia type IV Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000006372 lipid accumulation Effects 0.000 description 1
- 208000030159 metabolic disease Diseases 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- WWRBHZJBTOPRPE-UHFFFAOYSA-N n-ethyl-6-(1-phenylpyrazol-4-yl)pyridazin-3-amine Chemical compound N1=NC(NCC)=CC=C1C1=CN(C=2C=CC=CC=2)N=C1 WWRBHZJBTOPRPE-UHFFFAOYSA-N 0.000 description 1
- IBDLKKVFIZPXJQ-UHFFFAOYSA-N n-methyl-6-(1-phenylpyrazol-4-yl)pyridazin-3-amine Chemical compound N1=NC(NC)=CC=C1C1=CN(C=2C=CC=CC=2)N=C1 IBDLKKVFIZPXJQ-UHFFFAOYSA-N 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 208000025974 neutral lipid storage disease Diseases 0.000 description 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 description 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 230000002062 proliferating effect Effects 0.000 description 1
- 231100000240 steatosis hepatitis Toxicity 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 230000035924 thermogenesis Effects 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 208000016261 weight loss Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662330049P | 2016-04-29 | 2016-04-29 | |
| US62/330,049 | 2016-04-29 | ||
| PCT/US2017/030261 WO2017190086A1 (en) | 2016-04-29 | 2017-04-28 | Di-substituted pyrazole compounds for the treatment of diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019515956A JP2019515956A (ja) | 2019-06-13 |
| JP2019515956A5 true JP2019515956A5 (https=) | 2020-06-18 |
| JP6931695B2 JP6931695B2 (ja) | 2021-09-08 |
Family
ID=59215955
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019508167A Active JP6931695B2 (ja) | 2016-04-29 | 2017-04-28 | 疾患の治療のための二置換ピラゾール化合物 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US11497738B2 (https=) |
| EP (1) | EP3448851B8 (https=) |
| JP (1) | JP6931695B2 (https=) |
| KR (1) | KR102498741B1 (https=) |
| CN (1) | CN109476635B (https=) |
| AU (1) | AU2017258781C1 (https=) |
| CA (1) | CA3022395C (https=) |
| ES (1) | ES2912921T3 (https=) |
| IL (1) | IL262708B (https=) |
| MX (1) | MX382630B (https=) |
| WO (1) | WO2017190086A1 (https=) |
| ZA (1) | ZA201807509B (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2932187T3 (es) | 2016-09-07 | 2023-01-16 | Fgh Biotech Inc | Compuestos de pirazol disustituidos para el tratamiento de enfermedades |
| WO2019126731A1 (en) | 2017-12-22 | 2019-06-27 | Petra Pharma Corporation | Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors |
| EP3746070A4 (en) * | 2018-01-29 | 2021-09-01 | Capulus Therapeutics, LLC | SREBP INHIBITORS WITH A 6-LINKED CENTER RING |
| 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 |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| CN114728909A (zh) * | 2019-09-25 | 2022-07-08 | 韩国原子力医学院 | 含有新型三氟甲基苯基吡唑衍生物作为活性成分用于预防或治疗癌症的组合物 |
| KR102663365B1 (ko) * | 2019-09-25 | 2024-05-08 | 한국원자력의학원 | 신규 트리플루오로메틸페닐피라졸 유도체를 유효성분으로 함유하는 암 예방 또는 치료용 조성물 |
| EP4096659A4 (en) * | 2020-01-27 | 2023-10-18 | Capulus Therapeutics, LLC | Srebp inhibitors comprising a thiophene central ring |
| KR102258451B1 (ko) * | 2020-11-17 | 2021-05-31 | 주식회사 하이센스바이오 | 지방간질환의 예방 또는 치료용 조성물 |
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| US10328064B2 (en) | 2014-12-23 | 2019-06-25 | Fgh Biotech, Inc. | Compositions of fatostatin based heterocyclic compounds and uses thereof |
| EP3265457A1 (en) | 2015-03-04 | 2018-01-10 | Medivation Technologies LLC | Sterol regulatory element-binding proteins (srebps) inhibitors |
| US10183015B2 (en) | 2015-03-04 | 2019-01-22 | Medivation Technologies Llc | Heterocyclic compounds and methods of use |
| 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 |
| ES2932187T3 (es) | 2016-09-07 | 2023-01-16 | Fgh Biotech Inc | Compuestos de pirazol disustituidos para el tratamiento de enfermedades |
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2017
- 2017-04-28 KR KR1020187033931A patent/KR102498741B1/ko active Active
- 2017-04-28 JP JP2019508167A patent/JP6931695B2/ja active Active
- 2017-04-28 US US16/097,211 patent/US11497738B2/en active Active
- 2017-04-28 WO PCT/US2017/030261 patent/WO2017190086A1/en not_active Ceased
- 2017-04-28 ES ES17733180T patent/ES2912921T3/es active Active
- 2017-04-28 MX MX2018013221A patent/MX382630B/es unknown
- 2017-04-28 CN CN201780034410.XA patent/CN109476635B/zh active Active
- 2017-04-28 CA CA3022395A patent/CA3022395C/en active Active
- 2017-04-28 EP EP17733180.8A patent/EP3448851B8/en active Active
- 2017-04-28 AU AU2017258781A patent/AU2017258781C1/en active Active
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2018
- 2018-10-31 IL IL262708A patent/IL262708B/en unknown
- 2018-11-08 ZA ZA2018/07509A patent/ZA201807509B/en unknown
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2022
- 2022-09-08 US US17/940,640 patent/US20230119547A1/en active Pending
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