JP2012522060A5 - - Google Patents
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- JP2012522060A5 JP2012522060A5 JP2012503599A JP2012503599A JP2012522060A5 JP 2012522060 A5 JP2012522060 A5 JP 2012522060A5 JP 2012503599 A JP2012503599 A JP 2012503599A JP 2012503599 A JP2012503599 A JP 2012503599A JP 2012522060 A5 JP2012522060 A5 JP 2012522060A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- carbonyl
- dimethyl
- amino
- dioxino
- 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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- -1 benzothiopheneyl Chemical group 0.000 claims 47
- 125000000217 alkyl group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 16
- 125000001424 substituent group Chemical group 0.000 claims 12
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Substances CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 7
- 125000002947 alkylene group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- DEDPYBWOUXWMOX-ZTAAISNPSA-N (2s)-2-[[(3s,8s)-3-[4-[(3,4-dichlorophenyl)methoxy]phenyl]-7-[(1s)-1-phenylpropyl]-3,6,8,9-tetrahydro-2h-[1,4]dioxino[2,3-g]isoquinoline-8-carbonyl]amino]-3-[4-(2,3-dimethylpyridin-4-yl)phenyl]propanoic acid Chemical compound C([C@H](NC(=O)[C@@H]1CC2=CC=3OC[C@@H](OC=3C=C2CN1[C@@H](CC)C=1C=CC=CC=1)C=1C=CC(OCC=2C=C(Cl)C(Cl)=CC=2)=CC=1)C(O)=O)C(C=C1)=CC=C1C1=CC=NC(C)=C1C DEDPYBWOUXWMOX-ZTAAISNPSA-N 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 208000002705 Glucose Intolerance Diseases 0.000 claims 3
- 125000004419 alkynylene group Chemical group 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000001140 1,4-phenylene group Chemical group [H]C1=C([H])C([*:2])=C([H])C([H])=C1[*:1] 0.000 claims 2
- HPYNZHMRTTWQTB-UHFFFAOYSA-N 2,3-dimethylpyridine Chemical compound CC1=CC=CN=C1C HPYNZHMRTTWQTB-UHFFFAOYSA-N 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 201000009104 prediabetes syndrome Diseases 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 239000011593 sulfur Chemical group 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- YIKYLHBXYYFCEZ-WWKIHPBISA-N (2s)-2-[[(3s,8s)-3-[4-[(3,4-dichlorophenyl)methoxy]phenyl]-7-[(1s)-1-phenylpropyl]-3,6,8,9-tetrahydro-2h-[1,4]dioxino[2,3-g]isoquinoline-8-carbonyl]amino]-3-(4-pyridin-4-ylphenyl)propanoic acid Chemical compound C([C@H](NC(=O)[C@@H]1CC2=CC=3OC[C@@H](OC=3C=C2CN1[C@@H](CC)C=1C=CC=CC=1)C=1C=CC(OCC=2C=C(Cl)C(Cl)=CC=2)=CC=1)C(O)=O)C(C=C1)=CC=C1C1=CC=NC=C1 YIKYLHBXYYFCEZ-WWKIHPBISA-N 0.000 claims 1
- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010070901 Diabetic dyslipidaemia Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 claims 1
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 1
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 125000005275 alkylenearyl group Chemical group 0.000 claims 1
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 125000004350 aryl cycloalkyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 230000009286 beneficial effect Effects 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 230000035876 healing Effects 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 claims 1
- 229960003105 metformin Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Chemical group 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 1
- 235000019260 propionic acid Nutrition 0.000 claims 1
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16452309P | 2009-03-30 | 2009-03-30 | |
| US61/164,523 | 2009-03-30 | ||
| US30934810P | 2010-03-01 | 2010-03-01 | |
| US61/309,348 | 2010-03-01 | ||
| PCT/US2010/029172 WO2010114824A1 (en) | 2009-03-30 | 2010-03-30 | Substituted azoanthracene derivatives, pharmaceutical compositions, and methods of use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012522060A JP2012522060A (ja) | 2012-09-20 |
| JP2012522060A5 true JP2012522060A5 (enExample) | 2013-10-17 |
| JP5755217B2 JP5755217B2 (ja) | 2015-07-29 |
Family
ID=42828657
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012503599A Active JP5755217B2 (ja) | 2009-03-30 | 2010-03-30 | 置換アゾアントラセン誘導体、その医薬組成物とその使用の方法 |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US8383644B2 (enExample) |
| EP (1) | EP2413693B1 (enExample) |
| JP (1) | JP5755217B2 (enExample) |
| KR (1) | KR101732978B1 (enExample) |
| CN (1) | CN102378574B (enExample) |
| AU (1) | AU2010232750B2 (enExample) |
| BR (1) | BRPI1013579A2 (enExample) |
| CA (1) | CA2757084C (enExample) |
| DK (1) | DK2413693T3 (enExample) |
| EA (1) | EA023430B1 (enExample) |
| ES (1) | ES2553645T3 (enExample) |
| IL (1) | IL214822A (enExample) |
| MA (1) | MA33219B1 (enExample) |
| MX (1) | MX2011010347A (enExample) |
| SG (1) | SG174205A1 (enExample) |
| TN (1) | TN2011000437A1 (enExample) |
| WO (1) | WO2010114824A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7672201B2 (ja) | 2019-05-20 | 2025-05-07 | ファイザー・インク | Ｎａｓｈ／ｎａｆｌｄおよび関連疾患治療のための組合せ |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2011010347A (es) | 2009-03-30 | 2011-11-29 | Transtech Pharma Inc | Derivados sustituidos de azoantraceno, composiciones farmaceuticas y metodos de uso de los mismos. |
| CN103030646B (zh) * | 2011-09-29 | 2016-08-24 | 上海恒瑞医药有限公司 | 苯并二氧六环类衍生物、其制备方法及其在医药上的应用 |
| WO2013059215A1 (en) | 2011-10-17 | 2013-04-25 | Biotheryx, Inc. | Substituted biaryl alkyl amides |
| SG10201704716XA (en) | 2013-01-17 | 2017-07-28 | Vtv Therapeutics Llc | Combinations Of A GLP1R Agonist And Metformin And Use Thereof For The Treatment Of Type 2 Diabetes And Other Disorders |
| EP3185860A4 (en) | 2014-08-29 | 2018-08-29 | The Board of Regents of the University of Texas System | Novel capsazepine analogs for the treatment of cancer and other proliferative diseases |
| JOP20190060A1 (ar) * | 2016-09-26 | 2019-03-26 | Chugai Pharmaceutical Co Ltd | مشتق بيرازولو بيريدين له تأثير مساعد لمستقبل glp-1 |
| WO2019103060A1 (ja) * | 2017-11-22 | 2019-05-31 | 第一三共株式会社 | 縮合三環化合物 |
| JP7461104B2 (ja) * | 2017-11-29 | 2024-04-03 | 中外製薬株式会社 | Ｇｌｐ－１受容体アゴニスト作用を持つピラゾロピリジン誘導体を含有する医薬組成物 |
| WO2019217165A1 (en) | 2018-05-08 | 2019-11-14 | Vtv Therapeutics Llc | Therapeutic uses of glp1r agonists |
| CA3045644C (en) * | 2018-06-13 | 2024-01-16 | Pfizer Inc. | Glp-1 receptor agonists and uses thereof |
| MX2022008938A (es) * | 2020-01-20 | 2022-10-18 | Crescenta Biosciences | Nuevos compuestos moduladores del metabolismo celular y usos de los mismos. |
| EP4130005A4 (en) * | 2020-04-01 | 2024-04-24 | Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. | CRYSTALLINE FORM A OF A GLP-1 RECEPTOR AGONIST AND METHOD OF MANUFACTURING THEREOF |
| CN115315426B (zh) * | 2020-04-01 | 2023-12-12 | 杭州中美华东制药有限公司 | Glp-1受体激动剂游离碱的药学上可接受的酸式盐及其制备方法 |
| TW202144340A (zh) | 2020-04-03 | 2021-12-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 稠合咪唑類衍生物、其製備方法及其在醫藥上的應用 |
| WO2021238964A1 (zh) | 2020-05-28 | 2021-12-02 | 杭州中美华东制药有限公司 | 一种glp-1受体激动剂游离碱的制备方法 |
| WO2021242806A1 (en) | 2020-05-28 | 2021-12-02 | Vtv Therapeutics Llc | Intermediates and methods for preparing a glp-1 receptor agonist |
| TW202206412A (zh) | 2020-05-28 | 2022-02-16 | 美商維特衛治療有限責任公司 | 製備（ｓ）－２－胺基－３－（４－（２，３－二甲基吡啶－４－基）苯基）丙酸甲酯及其鹽酸鹽的方法 |
| CN115697968B (zh) * | 2020-05-28 | 2024-03-29 | 杭州中美华东制药有限公司 | (s)-2-氨基-3-(4-(2,3-二甲基吡啶-4-基)苯基丙酸甲酯及其盐的制备方法 |
| CN115667219B (zh) * | 2020-05-28 | 2024-11-15 | 杭州中美华东制药有限公司 | 一种(s)-2-氨基-3-(4-(2,3-二甲基吡啶-4-基)苯基)丙酸甲酯二酸盐的制备方法 |
| WO2021238962A1 (zh) | 2020-05-28 | 2021-12-02 | 杭州中美华东制药有限公司 | 一种制备glp-1受体激动剂的方法 |
| JP7812052B2 (ja) | 2020-09-01 | 2026-02-09 | 江蘇恒瑞医薬股▲ふん▼有限公司 | 縮合イミダゾール誘導体、その調製方法及びその医薬的応用 |
| EP4213847A4 (en) * | 2020-09-21 | 2024-12-04 | vTv Therapeutics LLC | AMORPHOUS FORM OF AN ISOQUINOLINE DERIVATIVE |
| JP7214053B2 (ja) * | 2020-10-08 | 2023-01-27 | イーライ リリー アンド カンパニー | 糖尿病治療に有用な６－メトキシ－３，４－ジヒドロ－１ｈ－イソキノリン化合物 |
| CN116348464B (zh) | 2020-10-12 | 2026-06-16 | 杭州中美华东制药有限公司 | 苯并咪唑酮类glp-1受体激动剂及其用途 |
| WO2022111624A1 (zh) | 2020-11-27 | 2022-06-02 | 深圳信立泰药业股份有限公司 | 一种苯并咪唑类衍生物及其制备方法和医药用途 |
| CN116940561B (zh) | 2021-03-22 | 2026-08-11 | 杭州中美华东制药有限公司 | 噻吩类glp-1受体激动剂及其用途 |
| EP4317145A4 (en) | 2021-03-24 | 2025-03-12 | Shionogi & Co., Ltd | Pharmaceutical composition containing glp-1 receptor agonist having fused ring |
| WO2022262143A1 (zh) * | 2021-06-17 | 2022-12-22 | 杭州中美华东制药有限公司 | 一种吡啶硼酸酯的制备方法 |
| WO2022262615A1 (zh) * | 2021-06-17 | 2022-12-22 | 杭州中美华东制药有限公司 | 蒽类化合物、其制备方法和医药用途 |
| CN117098758A (zh) | 2021-06-24 | 2023-11-21 | 杭州中美华东制药有限公司 | Glp-1受体激动剂及其组合物和用途 |
| CN117897387B (zh) * | 2021-09-03 | 2026-06-19 | 杭州中美华东制药有限公司 | Glp-1受体激动剂中间体的制备方法 |
| KR20240056719A (ko) | 2021-09-08 | 2024-04-30 | 시오노기 앤드 컴파니, 리미티드 | 항비만 작용이 관여하는 질환의 예방 및 치료용 의약 |
| US20250332157A1 (en) * | 2021-09-28 | 2025-10-30 | Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. | Solid composition of glp-1 receptor agonist |
| CN119907794A (zh) | 2022-09-22 | 2025-04-29 | 盐野义制药株式会社 | 具有glp-1受体激动剂作用的稠环化合物 |
| EP4777197A2 (en) | 2023-09-14 | 2026-07-22 | Ascletis Pharma (China) Co., Limited | Glp-1r agonist and therapeutic method thereof |
| WO2025109387A1 (en) | 2023-11-24 | 2025-05-30 | Ascletis Pharma (China) Co., Limited | Glp-1r agonist and therapeutic method thereof |
| AU2025207498A1 (en) | 2024-01-09 | 2026-07-09 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Glp-1r agonist pharmaceutical composition and use thereof |
| TW202600132A (zh) | 2024-03-08 | 2026-01-01 | 美商安尼波那生物公司 | 用於治療肥胖症及提高減重之方法 |
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| US8466296B2 (en) * | 2007-03-26 | 2013-06-18 | Ligand Pharmaceuticals | Compounds and processes for preparing substituted aminomethyl-2,3,8,9-tetrahydro-7H-1,4-dioxino[2,3-e]indol-8-ones |
| EA018225B1 (ru) * | 2008-03-07 | 2013-06-28 | Транстек Фарма, Инк. | Соединения оксадиазоантрацена для лечения диабета |
| US8718994B2 (en) | 2008-04-09 | 2014-05-06 | Transtech Pharma, Llc | Ligands for the GLP-1 receptor and methods for discovery thereof |
| MX2011010347A (es) | 2009-03-30 | 2011-11-29 | Transtech Pharma Inc | Derivados sustituidos de azoantraceno, composiciones farmaceuticas y metodos de uso de los mismos. |
| WO2011156655A2 (en) | 2010-06-09 | 2011-12-15 | Receptos, Inc. | Novel glp-1 receptor stabilizers and modulators |
-
2010
- 2010-03-30 MX MX2011010347A patent/MX2011010347A/es active IP Right Grant
- 2010-03-30 AU AU2010232750A patent/AU2010232750B2/en active Active
- 2010-03-30 KR KR1020117024153A patent/KR101732978B1/ko active Active
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7672201B2 (ja) | 2019-05-20 | 2025-05-07 | ファイザー・インク | Ｎａｓｈ／ｎａｆｌｄおよび関連疾患治療のための組合せ |
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