KR102286196B1 - 신규한 소마토스타틴 수용체 아형 4(sstr4) 작용제 - Google Patents

신규한 소마토스타틴 수용체 아형 4(sstr4) 작용제 Download PDF

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KR102286196B1
KR102286196B1 KR1020157035706A KR20157035706A KR102286196B1 KR 102286196 B1 KR102286196 B1 KR 102286196B1 KR 1020157035706 A KR1020157035706 A KR 1020157035706A KR 20157035706 A KR20157035706 A KR 20157035706A KR 102286196 B1 KR102286196 B1 KR 102286196B1
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mmol
give
alkyl
group
compound
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KR20160013081A (ko
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리카르도 지오바니니
유나이 쿠이
헨리 도츠
마르코 페라라
슈테판 유스트
라이문트 퀼처
이언 린가르드
로코 마자페로
클라우스 루돌프
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센트렉시온 테라퓨틱스 코포레이션
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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Families Citing this family (33)

* Cited by examiner, † Cited by third party
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005037216A2 (en) 2003-10-14 2005-04-28 Pfizer Products Inc. Bicyclic [3.1.0] derivatives as glycine transporter inhibitors
WO2010059922A1 (en) 2008-11-21 2010-05-27 Ligand Pharmaceuticals Incorporated Pyrrolidine carboxamide compounds
WO2012125661A1 (en) 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. Substituted 3-azabicyclo[3.1.0]hexane derivatives useful as ccr2 antagonists

Family Cites Families (11)

* Cited by examiner, † Cited by third party
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
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
US8835472B2 (en) 2010-09-02 2014-09-16 Boehringer Ingelheim International Gmbh Compounds, pharmaceutical compositions and uses thereof
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005037216A2 (en) 2003-10-14 2005-04-28 Pfizer Products Inc. Bicyclic [3.1.0] derivatives as glycine transporter inhibitors
WO2010059922A1 (en) 2008-11-21 2010-05-27 Ligand Pharmaceuticals Incorporated Pyrrolidine carboxamide compounds
WO2012125661A1 (en) 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. Substituted 3-azabicyclo[3.1.0]hexane derivatives useful as ccr2 antagonists

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