JP2016518430A5 - - Google Patents
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- JP2016518430A5 JP2016518430A5 JP2016513359A JP2016513359A JP2016518430A5 JP 2016518430 A5 JP2016518430 A5 JP 2016518430A5 JP 2016513359 A JP2016513359 A JP 2016513359A JP 2016513359 A JP2016513359 A JP 2016513359A JP 2016518430 A5 JP2016518430 A5 JP 2016518430A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- pain
- group
- compound according
- 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 45
- 208000002193 Pain Diseases 0.000 claims 16
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 125000002950 monocyclic group Chemical group 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000004122 cyclic group Chemical group 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- -1 C 1-6 -alkyl-O— Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 208000008035 Back Pain Diseases 0.000 claims 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 2
- 208000008930 Low Back Pain Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 201000008482 osteoarthritis Diseases 0.000 claims 2
- 208000024891 symptom Diseases 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000001640 Fibromyalgia Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 102100023801 Somatostatin receptor type 4 Human genes 0.000 claims 1
- 206010045171 Tumour pain Diseases 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 108010064556 somatostatin receptor subtype-4 Proteins 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- 0 CC(C)(COc(nc1)c(C)cc1F)NC([C@@]1[C@]2(*)[C@]1CNC2)=O Chemical compound CC(C)(COc(nc1)c(C)cc1F)NC([C@@]1[C@]2(*)[C@]1CNC2)=O 0.000 description 2
- PCINBSQTEDBZDB-ITGUQSILSA-N CC(C)(COc1c(C)cccn1)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O Chemical compound CC(C)(COc1c(C)cccn1)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O PCINBSQTEDBZDB-ITGUQSILSA-N 0.000 description 2
- IRWVCZSJFZFDPK-IMRBUKKESA-N CC(C)(COc1cccnc1C)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O Chemical compound CC(C)(COc1cccnc1C)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O IRWVCZSJFZFDPK-IMRBUKKESA-N 0.000 description 1
- ZKTLIVLGKFXXBA-IWIIMEHWSA-N CC(C)(c1cnc2[n]1nccc2)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O Chemical compound CC(C)(c1cnc2[n]1nccc2)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O ZKTLIVLGKFXXBA-IWIIMEHWSA-N 0.000 description 1
- HKKUYICHOOHPHK-IMRBUKKESA-N CC(C)(c1n[n](C)c2c1cccc2)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O Chemical compound CC(C)(c1n[n](C)c2c1cccc2)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O HKKUYICHOOHPHK-IMRBUKKESA-N 0.000 description 1
- LNAXHAAVFQIIEQ-IMRBUKKESA-N CC(C)(c1nc(C)c2[n]1cccc2)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O Chemical compound CC(C)(c1nc(C)c2[n]1cccc2)NC([C@@H]1[C@@H]2[C@H]1CNC2)=O LNAXHAAVFQIIEQ-IMRBUKKESA-N 0.000 description 1
- HQOVCLBJFYAIIO-DSOUYDQASA-N C[C@H](CCNC)C(NCCCC/C=C\C=C(/C)\N(C)N)=O Chemical compound C[C@H](CCNC)C(NCCCC/C=C\C=C(/C)\N(C)N)=O HQOVCLBJFYAIIO-DSOUYDQASA-N 0.000 description 1
- DMXZPRBKBJQPLV-REBRKWNGSA-N C[C@H]([C@@H]12)NC[C@H]1[C@H]2C(NC(C)(C)c1c(C=CCC=C2C)c2n[nH]1)=O Chemical compound C[C@H]([C@@H]12)NC[C@H]1[C@H]2C(NC(C)(C)c1c(C=CCC=C2C)c2n[nH]1)=O DMXZPRBKBJQPLV-REBRKWNGSA-N 0.000 description 1
- UGIPNJYBVXYNSY-UQACYDQXSA-N C[C@H]([C@H](/C(/C(CCCCCC(F)F)[I]=C(C)C)=N/N)N[C@H](C1C[C@@H](C)NCC1)O)[IH]C Chemical compound C[C@H]([C@H](/C(/C(CCCCCC(F)F)[I]=C(C)C)=N/N)N[C@H](C1C[C@@H](C)NCC1)O)[IH]C UGIPNJYBVXYNSY-UQACYDQXSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13168224.7 | 2013-05-17 | ||
| EP13168224 | 2013-05-17 | ||
| PCT/EP2014/059905 WO2014184275A1 (en) | 2013-05-17 | 2014-05-15 | New somatostatin receptor subtype 4 (sstr4) agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016518430A JP2016518430A (ja) | 2016-06-23 |
| JP2016518430A5 true JP2016518430A5 (enExample) | 2017-11-16 |
| JP6387086B2 JP6387086B2 (ja) | 2018-09-05 |
Family
ID=48428384
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016513359A Active JP6387086B2 (ja) | 2013-05-17 | 2014-05-15 | 新規ソマトスタチン受容体亜型４（ｓｓｔｒ４）作動薬 |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US9371282B2 (enExample) |
| EP (1) | EP2997021B1 (enExample) |
| JP (1) | JP6387086B2 (enExample) |
| KR (1) | KR102286196B1 (enExample) |
| CN (1) | CN105473574B (enExample) |
| AR (1) | AR096339A1 (enExample) |
| AU (1) | AU2014267328B2 (enExample) |
| BR (1) | BR112015028452B1 (enExample) |
| CA (1) | CA2912486C (enExample) |
| CL (1) | CL2015003290A1 (enExample) |
| DK (1) | DK2997021T3 (enExample) |
| EA (1) | EA032061B1 (enExample) |
| ES (1) | ES2658076T3 (enExample) |
| IL (1) | IL242313B (enExample) |
| JO (1) | JO3475B1 (enExample) |
| MX (1) | MX369358B (enExample) |
| NO (1) | NO2997021T3 (enExample) |
| PH (1) | PH12015502524B1 (enExample) |
| PL (1) | PL2997021T3 (enExample) |
| PT (1) | PT2997021T (enExample) |
| TW (1) | TWI636042B (enExample) |
| UA (1) | UA116247C2 (enExample) |
| UY (1) | UY35572A (enExample) |
| WO (1) | WO2014184275A1 (enExample) |
| ZA (1) | ZA201507958B (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9371282B2 (en) * | 2013-05-17 | 2016-06-21 | Centrexion Therapeutics Corporation | Somatostatin receptor subtype 4 (SSTR4) agonists |
| CR20190156A (es) | 2013-05-17 | 2019-05-16 | Incyte Corp | Derivados de bipirazol como inhibidores jak |
| JP2017526728A (ja) | 2014-09-15 | 2017-09-14 | インフラマトリー・レスポンス・リサーチ・インコーポレイテッド | 炎症介在性状態の治療におけるレボセチリジン及びモンテルカスト |
| WO2016075239A1 (en) * | 2014-11-14 | 2016-05-19 | Boehringer Ingelheim International Gmbh | Aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amides as somatostatin receptor subtype 4 (sstr4) agonists |
| TN2018000198A1 (en) | 2015-12-29 | 2019-10-04 | Pfizer | Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors |
| US11912687B2 (en) | 2017-05-12 | 2024-02-27 | Board of Trustees of the Southern Illinois University | 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof |
| WO2018209267A2 (en) | 2017-05-12 | 2018-11-15 | Board Of Trustees Of The Southern Illinois University On Behalf Of Southern Illinois University Edwardsville | 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof |
| US10865163B2 (en) | 2017-12-20 | 2020-12-15 | The University Of Toledo | Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds |
| CA3091339A1 (en) | 2018-02-16 | 2019-08-22 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of cytokine-related disorders |
| TWI834637B (zh) | 2018-03-01 | 2024-03-11 | 日商武田藥品工業有限公司 | 六氫吡啶基-3-(芳氧基)丙醯胺及丙酸酯 |
| KR20260080448A (ko) | 2018-03-30 | 2026-06-02 | 인사이트 코포레이션 | Jak 억제제를 사용하는 화농성 한선염의 치료 |
| US11668295B2 (en) | 2018-12-28 | 2023-06-06 | Avent, Inc. | Pump head for a peristaltic pump |
| CN112979655A (zh) | 2019-12-16 | 2021-06-18 | 上海赛默罗生物科技有限公司 | 三唑并哒嗪类衍生物、其制备方法、药物组合物和用途 |
| AR121682A1 (es) | 2020-03-31 | 2022-06-29 | Takeda Pharmaceuticals Co | Derivados de n-(heterociclil y heterociclilalquil)-3-bencilpiridin-2-amina como agonistas de sstr4 |
| WO2021236518A1 (en) * | 2020-05-19 | 2021-11-25 | IRR, Inc. | Levocetirizine and montelukast in the treatment of sepsis and symptoms thereof |
| CN113717167B (zh) * | 2020-05-21 | 2022-12-02 | 广州费米子科技有限责任公司 | 并环化合物及其制备方法、药物组合物和应用 |
| CN113717161B (zh) * | 2020-05-21 | 2023-06-09 | 广州费米子科技有限责任公司 | 含氮饱和杂环化合物及其制备方法、药物组合物和应用 |
| SI4157831T1 (sl) | 2020-06-02 | 2025-02-28 | Incyte Corporation | Postopki za pripravo zaviralca jak1 |
| TWI910192B (zh) * | 2020-07-13 | 2026-01-01 | 大陸商廣州費米子科技有限責任公司 | 含氮雜環化合物、藥物組合物和應用 |
| CN116601279A (zh) | 2020-07-28 | 2023-08-15 | 思进股份有限公司 | 用于生产多肽的方法和系统 |
| KR20230080441A (ko) * | 2020-10-02 | 2023-06-07 | 더 보드 오브 리젠츠 오브 더 유니버시티 오브 텍사스 시스템 | 전사 활성화 단백질의 이미다조피페라진 억제제 |
| IL303238A (en) | 2020-12-08 | 2023-07-01 | Incyte Corp | Jak1 pathway inhibitors for the treatment of vitiligo |
| AU2022270072A1 (en) | 2021-05-03 | 2023-11-02 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of prurigo nodularis |
| TWI860849B (zh) * | 2021-09-14 | 2024-11-01 | 美商美國禮來大藥廠 | Sstr4促效劑鹽 |
| WO2024191675A1 (en) | 2023-03-10 | 2024-09-19 | Eli Lilly And Company | Methods for the preparation of sstr4 agonists and salts thereof |
| EP4676477A1 (en) * | 2023-03-10 | 2026-01-14 | Eli Lilly And Company | Methods for the preparation and dose regimens for use of sstr4 agonists and salts thereof |
| CN119039274A (zh) * | 2023-05-29 | 2024-11-29 | 武汉熙瑞医药科技有限公司 | 3-氮杂-双环[3.1.0]己烷衍生物、其制备方法及其应用 |
| IL326196A (en) * | 2023-08-02 | 2026-03-01 | Boehringer Ingelheim Int | (2S, 5R)-5-(hydroxymethyl)morpholine-2-carboxamides as SSTR4 agonists |
| CN122295317A (zh) | 2023-10-30 | 2026-06-26 | 伊莱利利公司 | 用于制备3-氮杂双环[3.1.0]己烷-6-甲酰胺衍生物的新方法 |
| WO2025193591A1 (en) | 2024-03-11 | 2025-09-18 | Eli Lilly And Company | Crystalline form of a tartrate salt of an sstr4 agonist |
| WO2025247982A1 (en) | 2024-05-29 | 2025-12-04 | Grünenthal GmbH | Piperazines which act as sstr4 modulators |
| WO2026015686A1 (en) * | 2024-07-11 | 2026-01-15 | HUMANWELL PHARMACEUTICAL US, Inc. | Prodrugs of somatostatin receptors subtype 4 (sstr4) agonists and their applications |
| WO2026019827A1 (en) * | 2024-07-16 | 2026-01-22 | Eli Lilly And Company | Methods for the removal of n-tosyl protecting group |
| WO2026030052A1 (en) | 2024-07-31 | 2026-02-05 | Fmc Corporation | Fungicidal substituted azoles |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6159941A (en) | 1996-05-14 | 2000-12-12 | Novo Nordisk A/S | Use of somatostatin agonists and antagonists for treating diseases related to the eye |
| US6355613B1 (en) | 1996-07-31 | 2002-03-12 | Peptor Limited | Conformationally constrained backbone cyclized somatostatin analogs |
| US6063796A (en) | 1997-04-04 | 2000-05-16 | Merck & Co., Inc. | Somatostatin agonists |
| US6057338A (en) | 1997-04-04 | 2000-05-02 | Merck & Co., Inc. | Somatostatin agonists |
| FI20031454A0 (fi) | 2003-10-06 | 2003-10-06 | Juvantia Pharma Ltd Oy | Selektiivisiä somatostatiinireseptori 1 ja/tai 4 -agonisteja ja -antagonisteja |
| US20100004339A1 (en) | 2003-10-06 | 2010-01-07 | Oy Juvantia Pharma Ltd. | Somatostatin Receptor 1 and/or 4 Selective Agonists and Antagonists |
| EA009903B1 (ru) * | 2003-10-14 | 2008-04-28 | Пфайзер Продактс Инк. | Бициклические [3.1.0] производные в качестве ингибиторов переносчиков глицина |
| JP2010513458A (ja) | 2006-12-19 | 2010-04-30 | ファイザー・プロダクツ・インク | Ｈ−ｐｇｄｓの阻害剤としてのニコチンアミド誘導体、およびプロスタグランジンｄ２の仲介による疾患を治療するためのその使用 |
| WO2010059922A1 (en) | 2008-11-21 | 2010-05-27 | Ligand Pharmaceuticals Incorporated | Pyrrolidine carboxamide compounds |
| US8835472B2 (en) | 2010-09-02 | 2014-09-16 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical compositions and uses thereof |
| EP2685828A4 (en) | 2011-03-17 | 2014-08-13 | Merck Sharp & Dohme | SUBSTITUTED 3-AZABICYCLO [3,1,0-] HEXAN DERIVATIVES AS CCR2 ANTAGONISTS |
| CN102675290B (zh) * | 2011-03-18 | 2014-11-12 | 山东亨利医药科技有限责任公司 | 含有并环的二氢吡唑类化合物 |
| KR101556318B1 (ko) * | 2013-05-15 | 2015-10-01 | 한국과학기술연구원 | 칼슘이온 채널 조절제로서 유효한 6-피라졸일아미도-3-치환된 아자바이사이클로[3.1.0]헥산 유도체 |
| US9371282B2 (en) * | 2013-05-17 | 2016-06-21 | Centrexion Therapeutics Corporation | Somatostatin receptor subtype 4 (SSTR4) agonists |
-
2014
- 2014-05-12 US US14/275,879 patent/US9371282B2/en active Active
- 2014-05-15 PT PT147240857T patent/PT2997021T/pt unknown
- 2014-05-15 EA EA201501122A patent/EA032061B1/ru unknown
- 2014-05-15 WO PCT/EP2014/059905 patent/WO2014184275A1/en not_active Ceased
- 2014-05-15 ES ES14724085.7T patent/ES2658076T3/es active Active
- 2014-05-15 JP JP2016513359A patent/JP6387086B2/ja active Active
- 2014-05-15 KR KR1020157035706A patent/KR102286196B1/ko active Active
- 2014-05-15 MX MX2015015620A patent/MX369358B/es active IP Right Grant
- 2014-05-15 NO NO14724085A patent/NO2997021T3/no unknown
- 2014-05-15 PL PL14724085T patent/PL2997021T3/pl unknown
- 2014-05-15 AU AU2014267328A patent/AU2014267328B2/en active Active
- 2014-05-15 EP EP14724085.7A patent/EP2997021B1/en active Active
- 2014-05-15 BR BR112015028452-3A patent/BR112015028452B1/pt active IP Right Grant
- 2014-05-15 UA UAA201512356A patent/UA116247C2/uk unknown
- 2014-05-15 CA CA2912486A patent/CA2912486C/en active Active
- 2014-05-15 CN CN201480040447.XA patent/CN105473574B/zh active Active
- 2014-05-15 DK DK14724085.7T patent/DK2997021T3/en active
- 2014-05-16 TW TW103117405A patent/TWI636042B/zh active
- 2014-05-16 UY UY0001035572A patent/UY35572A/es unknown
- 2014-05-16 AR ARP140101981A patent/AR096339A1/es unknown
- 2014-05-18 JO JOP/2014/0165A patent/JO3475B1/ar active
-
2015
- 2015-10-26 ZA ZA2015/07958A patent/ZA201507958B/en unknown
- 2015-10-27 IL IL242313A patent/IL242313B/en active IP Right Grant
- 2015-11-04 PH PH12015502524A patent/PH12015502524B1/en unknown
- 2015-11-09 CL CL2015003290A patent/CL2015003290A1/es unknown
-
2016
- 2016-05-18 US US15/157,624 patent/US9789082B2/en active Active
-
2017
- 2017-08-24 US US15/685,588 patent/US10166214B2/en active Active
-
2018
- 2018-11-02 US US16/178,817 patent/US10675268B2/en active Active
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