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 (https=) | 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 (https=) |
| EP (1) | EP2997021B1 (https=) |
| JP (1) | JP6387086B2 (https=) |
| KR (1) | KR102286196B1 (https=) |
| CN (1) | CN105473574B (https=) |
| AR (1) | AR096339A1 (https=) |
| AU (1) | AU2014267328B2 (https=) |
| BR (1) | BR112015028452B1 (https=) |
| CA (1) | CA2912486C (https=) |
| CL (1) | CL2015003290A1 (https=) |
| DK (1) | DK2997021T3 (https=) |
| EA (1) | EA032061B1 (https=) |
| ES (1) | ES2658076T3 (https=) |
| IL (1) | IL242313B (https=) |
| JO (1) | JO3475B1 (https=) |
| MX (1) | MX369358B (https=) |
| NO (1) | NO2997021T3 (https=) |
| PH (1) | PH12015502524B1 (https=) |
| PL (1) | PL2997021T3 (https=) |
| PT (1) | PT2997021T (https=) |
| TW (1) | TWI636042B (https=) |
| UA (1) | UA116247C2 (https=) |
| UY (1) | UY35572A (https=) |
| WO (1) | WO2014184275A1 (https=) |
| ZA (1) | ZA201507958B (https=) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SMT201900223T1 (it) | 2013-05-17 | 2019-07-11 | Incyte Corp | Sale di bipirazolo come inibitore di jak |
| US9371282B2 (en) | 2013-05-17 | 2016-06-21 | Centrexion Therapeutics Corporation | Somatostatin receptor subtype 4 (SSTR4) agonists |
| WO2016044095A1 (en) | 2014-09-15 | 2016-03-24 | Inflammatory Response Research, Inc. | Levocetirizine and montelukast in the treatment of inflammation mediated conditions |
| JP6590927B2 (ja) * | 2014-11-14 | 2019-10-16 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ソマトスタチン受容体サブタイプ４（ｓｓｔｒ４）作動薬としてのアリール及びヘテロアリール縮合テトラヒドロ−１，４−オキサゼピンアミド |
| SI3397631T1 (sl) | 2015-12-29 | 2022-01-31 | Pfizer Inc. | Substituirani 3-azabiciklo(3.1.0)heksani kot zaviralci ketoheksokinaze |
| 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 |
| JP7343170B2 (ja) | 2017-05-12 | 2023-09-12 | ボード オブ トラスティーズ オブ ザ サザン イリノイ ユニバーシティ オン ビハーフ オブ サザン イリノイ ユニバーシティ エドワーズビル | ３，４，５－三置換－１，２，４－トリアゾールおよび３，４，５－三置換－３－チオ－１，２，４－トリアゾール、ならびにそれらの使用 |
| 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 |
| IL311485B1 (en) | 2018-02-16 | 2026-01-01 | Incyte Corp | 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 |
| MD3773593T2 (ro) | 2018-03-30 | 2024-10-31 | Incyte Corp | Tratament hidradenitei supurative utilizând inhibitori ai JAK |
| 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 |
| 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 |
| KR20230015333A (ko) * | 2020-05-21 | 2023-01-31 | 광저우 페르미온 테크놀로지 씨오., 엘티디. | 융합된 고리 화합물, 이의 제조 방법, 이의 약제학적 조성물 및 용도 |
| FI4157831T3 (fi) | 2020-06-02 | 2024-12-02 | Incyte Corp | Menetelmiä jak1-estäjän valmistamiseksi |
| 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 |
| US20230287322A1 (en) | 2020-07-28 | 2023-09-14 | Seagen Inc. | Methods and systems for producing polypeptides |
| WO2022072648A1 (en) * | 2020-10-02 | 2022-04-07 | Board Of Regents, The University Of Texas System | Imidazopiperazine inhibitors of transcription activating proteins |
| WO2022125670A1 (en) | 2020-12-08 | 2022-06-16 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of vitiligo |
| RS67455B1 (sr) | 2021-05-03 | 2025-12-31 | Incyte Corp | Inhibitori jak1 puta za lečenje prurigo nodularisa |
| TWI860849B (zh) * | 2021-09-14 | 2024-11-01 | 美商美國禮來大藥廠 | Sstr4促效劑鹽 |
| 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 |
| CN120897906A (zh) | 2023-03-10 | 2025-11-04 | 伊莱利利公司 | 制备sstr4激动剂及其盐的方法 |
| 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 |
| WO2025096300A1 (en) | 2023-10-30 | 2025-05-08 | Eli Lilly And Company | Novel methods for the preparation of 3-azabicylco[3.1,0]hexane-6-carboxamide derivatives |
| TW202600537A (zh) | 2024-03-11 | 2026-01-01 | 美商美國禮來大藥廠 | Ｓｓｔｒ４促效劑化合物及其組合物 |
| WO2025247982A1 (en) | 2024-05-29 | 2025-12-04 | Grünenthal GmbH | Piperazines which act as sstr4 modulators |
| 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 |
| US20100004339A1 (en) | 2003-10-06 | 2010-01-07 | Oy Juvantia Pharma Ltd. | Somatostatin Receptor 1 and/or 4 Selective Agonists and Antagonists |
| FI20031454A0 (fi) | 2003-10-06 | 2003-10-06 | Juvantia Pharma Ltd Oy | Selektiivisiä somatostatiinireseptori 1 ja/tai 4 -agonisteja ja -antagonisteja |
| KR20060095865A (ko) | 2003-10-14 | 2006-09-04 | 화이자 프로덕츠 인크. | 글리신 수송 억제제로서의 비시클릭 [3.1.0] 유도체 |
| EP2129660A2 (en) | 2006-12-19 | 2009-12-09 | Pfizer Products Inc. | Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases |
| 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 |
| WO2012125661A1 (en) | 2011-03-17 | 2012-09-20 | Merck Sharp & Dohme Corp. | Substituted 3-azabicyclo[3.1.0]hexane derivatives useful 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 JP JP2016513359A patent/JP6387086B2/ja active Active
- 2014-05-15 WO PCT/EP2014/059905 patent/WO2014184275A1/en not_active Ceased
- 2014-05-15 KR KR1020157035706A patent/KR102286196B1/ko active Active
- 2014-05-15 CA CA2912486A patent/CA2912486C/en active Active
- 2014-05-15 MX MX2015015620A patent/MX369358B/es active IP Right Grant
- 2014-05-15 BR BR112015028452-3A patent/BR112015028452B1/pt active IP Right Grant
- 2014-05-15 AU AU2014267328A patent/AU2014267328B2/en active Active
- 2014-05-15 PL PL14724085T patent/PL2997021T3/pl unknown
- 2014-05-15 DK DK14724085.7T patent/DK2997021T3/en active
- 2014-05-15 NO NO14724085A patent/NO2997021T3/no unknown
- 2014-05-15 EP EP14724085.7A patent/EP2997021B1/en active Active
- 2014-05-15 CN CN201480040447.XA patent/CN105473574B/zh active Active
- 2014-05-15 ES ES14724085.7T patent/ES2658076T3/es active Active
- 2014-05-15 UA UAA201512356A patent/UA116247C2/uk unknown
- 2014-05-15 PT PT147240857T patent/PT2997021T/pt unknown
- 2014-05-15 EA EA201501122A patent/EA032061B1/ru unknown
- 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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