JP2019501971A5 - - Google Patents
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- Publication number
- JP2019501971A5 JP2019501971A5 JP2018553855A JP2018553855A JP2019501971A5 JP 2019501971 A5 JP2019501971 A5 JP 2019501971A5 JP 2018553855 A JP2018553855 A JP 2018553855A JP 2018553855 A JP2018553855 A JP 2018553855A JP 2019501971 A5 JP2019501971 A5 JP 2019501971A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- optionally substituted
- alkyl
- cycloalkyl
- independently
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 85
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 31
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 26
- 125000005843 halogen group Chemical group 0.000 claims description 22
- 125000000217 alkyl group Chemical group 0.000 claims description 20
- 238000000034 method Methods 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 16
- 125000003282 alkyl amino group Chemical group 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 125000005842 heteroatom Chemical group 0.000 claims description 12
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 11
- 201000011510 cancer Diseases 0.000 claims description 11
- 125000003342 alkenyl group Chemical group 0.000 claims description 10
- 125000003545 alkoxy group Chemical group 0.000 claims description 10
- 125000000304 alkynyl group Chemical group 0.000 claims description 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 206010022489 Insulin Resistance Diseases 0.000 claims description 9
- -1 -OH Chemical group 0.000 claims description 8
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims description 8
- 150000002148 esters Chemical class 0.000 claims description 8
- 125000001153 fluoro group Chemical group F* 0.000 claims description 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 8
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims description 6
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims description 6
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 208000030159 metabolic disease Diseases 0.000 claims description 6
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 4
- 101000777293 Homo sapiens Serine/threonine-protein kinase Chk1 Proteins 0.000 claims description 4
- 102100031081 Serine/threonine-protein kinase Chk1 Human genes 0.000 claims description 4
- 239000002246 antineoplastic agent Substances 0.000 claims description 4
- 229940127089 cytotoxic agent Drugs 0.000 claims description 4
- 239000003112 inhibitor Substances 0.000 claims description 4
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims description 3
- 102100034069 MAP kinase-activated protein kinase 2 Human genes 0.000 claims description 3
- 101710141394 MAP kinase-activated protein kinase 2 Proteins 0.000 claims description 3
- 208000001145 Metabolic Syndrome Diseases 0.000 claims description 3
- 208000008589 Obesity Diseases 0.000 claims description 3
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims description 3
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 3
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims description 3
- 230000001419 dependent effect Effects 0.000 claims description 3
- 208000004104 gestational diabetes Diseases 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 3
- 235000020824 obesity Nutrition 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 2
- 208000004930 Fatty Liver Diseases 0.000 claims description 2
- 206010019708 Hepatic steatosis Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 2
- 239000003472 antidiabetic agent Substances 0.000 claims description 2
- 229940125708 antidiabetic agent Drugs 0.000 claims description 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 2
- 229960004316 cisplatin Drugs 0.000 claims description 2
- 238000002648 combination therapy Methods 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000010706 fatty liver disease Diseases 0.000 claims description 2
- 230000004110 gluconeogenesis Effects 0.000 claims description 2
- 230000009229 glucose formation Effects 0.000 claims description 2
- 230000004116 glycogenolysis Effects 0.000 claims description 2
- 230000002440 hepatic effect Effects 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 201000001421 hyperglycemia Diseases 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 231100000240 steatosis hepatitis Toxicity 0.000 claims description 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 14
- 239000003814 drug Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 230000000694 effects Effects 0.000 description 1
- 125000000623 heterocyclic group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662274640P | 2016-01-04 | 2016-01-04 | |
| US62/274,640 | 2016-01-04 | ||
| PCT/US2017/012092 WO2017120164A1 (en) | 2016-01-04 | 2017-01-04 | Fused quadracyclic compounds, compositions and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019501971A JP2019501971A (ja) | 2019-01-24 |
| JP2019501971A5 true JP2019501971A5 (enExample) | 2020-02-13 |
| JP7068185B2 JP7068185B2 (ja) | 2022-05-16 |
Family
ID=59226993
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018553855A Active JP7068185B2 (ja) | 2016-01-04 | 2017-01-04 | 縮合四環式の化合物、組成物及びその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US10059718B2 (enExample) |
| EP (1) | EP3400228B1 (enExample) |
| JP (1) | JP7068185B2 (enExample) |
| CN (1) | CN108779123B (enExample) |
| AU (1) | AU2017205320B2 (enExample) |
| CA (1) | CA3010213A1 (enExample) |
| ES (1) | ES2915901T3 (enExample) |
| TW (1) | TWI730027B (enExample) |
| WO (1) | WO2017120164A1 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10059718B2 (en) | 2016-01-04 | 2018-08-28 | Tabomedex Biosciences, LLC | Fused quadracyclic compounds, compositions and uses thereof |
| CN107879989B (zh) * | 2017-11-29 | 2020-01-03 | 重庆市中药研究院 | 具有生物活性的3,4,5-取代苯并二氮卓2-酮类药物分子及其制备方法 |
| WO2022150707A1 (en) * | 2021-01-11 | 2022-07-14 | Tabomedex Biosciences, Inc. | Fused quadracyclic compounds, compositions and uses thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4521534A (en) | 1983-12-19 | 1985-06-04 | Ayerst, Mckenna & Harrison, Ltd. | Imidazo[2,1-a]pyrrolo[2,1-c][1,4]benzodiazepine derivatives, methods of preparation and use |
| US4596799A (en) | 1985-01-29 | 1986-06-24 | Ciba-Geigy Corporation | 9H-pyrrolo[2,1-c]-1,2,4-triazolo[4,3-a][1,4]benzodiazepines |
| TWI239333B (en) * | 2000-11-16 | 2005-09-11 | Hoffmann La Roche | Benzodiazepine derivatives as GABA A receptor modulators |
| CN1747949A (zh) | 2002-12-20 | 2006-03-15 | 法马西亚公司 | 无环吡唑化合物 |
| CA2908098A1 (en) | 2013-03-15 | 2014-09-25 | Celgene Avilomics Research, Inc. | Mk2 inhibitors and uses thereof |
| US20160066387A1 (en) * | 2013-03-22 | 2016-03-03 | Lifi Labs Inc | Color selection |
| US10059718B2 (en) | 2016-01-04 | 2018-08-28 | Tabomedex Biosciences, LLC | Fused quadracyclic compounds, compositions and uses thereof |
-
2017
- 2017-01-03 US US15/397,212 patent/US10059718B2/en active Active
- 2017-01-04 EP EP17736213.4A patent/EP3400228B1/en active Active
- 2017-01-04 CA CA3010213A patent/CA3010213A1/en active Pending
- 2017-01-04 TW TW106100215A patent/TWI730027B/zh active
- 2017-01-04 JP JP2018553855A patent/JP7068185B2/ja active Active
- 2017-01-04 WO PCT/US2017/012092 patent/WO2017120164A1/en not_active Ceased
- 2017-01-04 ES ES17736213T patent/ES2915901T3/es active Active
- 2017-01-04 AU AU2017205320A patent/AU2017205320B2/en active Active
- 2017-01-04 CN CN201780005620.6A patent/CN108779123B/zh active Active
-
2018
- 2018-07-19 US US16/039,877 patent/US10562909B2/en active Active
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