CN103298807A - 作为用于治疗自身免疫性疾病和血管疾病的s1p1激动剂的杂环化合物 - Google Patents
作为用于治疗自身免疫性疾病和血管疾病的s1p1激动剂的杂环化合物 Download PDFInfo
- Publication number
- CN103298807A CN103298807A CN2011800639683A CN201180063968A CN103298807A CN 103298807 A CN103298807 A CN 103298807A CN 2011800639683 A CN2011800639683 A CN 2011800639683A CN 201180063968 A CN201180063968 A CN 201180063968A CN 103298807 A CN103298807 A CN 103298807A
- Authority
- CN
- China
- Prior art keywords
- phenyl
- trifluoromethyl
- oxadiazol
- chroman
- isoxazol
- 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.)
- Pending
Links
- 0 CCC(C(*)(C(*)**=C)O)=C(C=C)C=C(C=**)c1n[o]c(-c2c(*)[n](*)nc2)n1 Chemical compound CCC(C(*)(C(*)**=C)O)=C(C=C)C=C(C=**)c1n[o]c(-c2c(*)[n](*)nc2)n1 0.000 description 6
- CSVPEBXYMLNJOT-UZLBHIALSA-N CC(C)N[C@H](COc1cc(-c2n[o]c(-c3c(C(F)(F)F)c(-c4ccccc4)n[o]3)n2)ccc11)[C@H]1O Chemical compound CC(C)N[C@H](COc1cc(-c2n[o]c(-c3c(C(F)(F)F)c(-c4ccccc4)n[o]3)n2)ccc11)[C@H]1O CSVPEBXYMLNJOT-UZLBHIALSA-N 0.000 description 1
- LUZZLRLRKJBLSQ-UHFFFAOYSA-N CCOC(c1c(C(F)(F)F)c(-c2ccccc2)n[o]1)=O Chemical compound CCOC(c1c(C(F)(F)F)c(-c2ccccc2)n[o]1)=O LUZZLRLRKJBLSQ-UHFFFAOYSA-N 0.000 description 1
- CXDNPBDEFFQNRT-JANGERMGSA-N O[C@@H](C(COc1c2)NCC(O)=O)c1ccc2-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1 Chemical compound O[C@@H](C(COc1c2)NCC(O)=O)c1ccc2-c1n[o]c(-c2c(C(F)(F)F)c(-c3ccccc3)n[o]2)n1 CXDNPBDEFFQNRT-JANGERMGSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40968210P | 2010-11-03 | 2010-11-03 | |
| US61/409,682 | 2010-11-03 | ||
| PCT/US2011/058891 WO2012061459A1 (en) | 2010-11-03 | 2011-11-02 | Heterocyclic compounds as s1p1 agonists for the treatment of autoimmune and vascular diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103298807A true CN103298807A (zh) | 2013-09-11 |
Family
ID=44983720
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011800639683A Pending CN103298807A (zh) | 2010-11-03 | 2011-11-02 | 作为用于治疗自身免疫性疾病和血管疾病的s1p1激动剂的杂环化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8629282B2 (https=) |
| EP (1) | EP2635573B1 (https=) |
| JP (1) | JP2013544811A (https=) |
| CN (1) | CN103298807A (https=) |
| ES (1) | ES2525298T3 (https=) |
| WO (1) | WO2012061459A1 (https=) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018014862A1 (zh) * | 2016-07-22 | 2018-01-25 | 南京明德新药研发股份有限公司 | S1p1激动剂及其应用 |
| WO2019141245A1 (zh) * | 2018-01-18 | 2019-07-25 | 南京明德新药研发股份有限公司 | 一种三并环化合物的晶型、盐型及其制备方法 |
| CN115038437A (zh) * | 2019-11-20 | 2022-09-09 | 艾尼纳制药公司 | 治疗与s1p1受体相关的病症的方法 |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5788507B2 (ja) | 2010-07-20 | 2015-09-30 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 置換3−フェニル−1,2,4−オキサジアゾール化合物 |
| EP2619190B1 (en) | 2010-09-24 | 2015-08-12 | Bristol-Myers Squibb Company | Substituted oxadiazole compounds and their use as s1p1 agonists |
| TWI613182B (zh) | 2013-02-21 | 2018-02-01 | 必治妥美雅史谷比公司 | 雙環化合物 |
| TWI689487B (zh) | 2014-08-20 | 2020-04-01 | 美商必治妥美雅史谷比公司 | 經取代雙環化合物 |
| IL271149B2 (en) | 2017-06-14 | 2024-05-01 | Trevena Inc | Compounds for modulating s1p1 activity and methods of using the same |
| EP4061352A4 (en) * | 2019-11-19 | 2024-02-28 | Trevena, Inc. | COMPOUNDS AND METHODS FOR PRODUCING S1P1-MODULATING COMPOUNDS |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1788008A (zh) * | 2003-05-15 | 2006-06-14 | 麦克公司 | 作为s1p受体激动剂的3-(2-氨基-1-氮杂环基)-5-芳基-1,2,4-噁二唑 |
| CN1859908A (zh) * | 2003-10-01 | 2006-11-08 | 默克公司 | 作为s1p受体激动剂的3,5-芳基、杂芳基或环烷基取代的-1,2,4-噁二唑类化合物 |
| WO2009080728A1 (en) * | 2007-12-21 | 2009-07-02 | Glaxo Group Limited | Oxadiazole derivatives active on sphingosine-1-phosphate (sip) |
| WO2010069949A1 (en) * | 2008-12-18 | 2010-06-24 | Merck Serono S.A. | Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis |
| WO2010072352A1 (en) * | 2008-12-26 | 2010-07-01 | Almirall S.A. | 1, 2, 4 -oxadiazole derivatives and their therapeutic use |
| WO2010081692A1 (en) * | 2009-01-19 | 2010-07-22 | Almirall, S.A. | Oxadiazole derivatives as slpl receptor agonists |
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| US4200750A (en) | 1977-01-07 | 1980-04-29 | Westwood Pharmaceuticals Inc. | 4-Substituted imidazo [1,2-a]quinoxalines |
| US6069143A (en) | 1994-12-20 | 2000-05-30 | Smithkline Beecham Corporation | Fibrinogen receptor antagonists |
| ATE448193T1 (de) | 2002-01-18 | 2009-11-15 | Merck & Co Inc | ßN-(BENZYL)AMINOALKYL CARBOXYLATE, PHOSPHINATE, PHOSPHONATE UND TETRAZOLE ALS EDG REZEPTORAGONISTENß |
| US7479504B2 (en) | 2002-01-18 | 2009-01-20 | Merck & Co., Inc. | Edg receptor agonists |
| US20050070506A1 (en) | 2002-01-18 | 2005-03-31 | Doherty George A. | Selective s1p1/edg1 receptor agonists |
| US7309721B2 (en) | 2002-03-01 | 2007-12-18 | Merck + Co., Inc. | Aminoalkylphosphonates and related compounds as Edg receptor agonists |
| JP2005533058A (ja) | 2002-06-17 | 2005-11-04 | メルク エンド カムパニー インコーポレーテッド | Edg受容体アゴニストとしての1−((5−アリール−1,2,4−オキサジアゾール−3−イル)ベンジル)アゼチジン−3−カルボキシラートおよび1−((5−アリール−1,2,4−オキサジアゾール−3−イル)ベンジル)ピロリジン−3−カルボキシラート |
| BRPI0410439A (pt) | 2003-05-19 | 2006-06-06 | Irm Llc | compostos e composições imunossupressoras |
| US7605171B2 (en) | 2003-12-17 | 2009-10-20 | Merck & Co., Inc. | (3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists |
| TW200538433A (en) | 2004-02-24 | 2005-12-01 | Irm Llc | Immunosuppressant compounds and compositiions |
| AU2005299851B2 (en) | 2004-10-22 | 2011-03-17 | Merck Sharp & Dohme Corp. | 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as S1P receptor agonists |
| BRPI0609668A2 (pt) | 2005-03-23 | 2011-10-18 | Actelion Pharmaceuticals Ltd | composto, composição farmacêutica, e, uso de um composto |
| CN101203512A (zh) | 2005-04-22 | 2008-06-18 | 第一三共株式会社 | 杂环化合物 |
| BRPI0612028A2 (pt) | 2005-06-08 | 2010-10-13 | Novartis Ag | oxadiazóis ou isodiazóis policìclicos e uso dos mesmos como ligantes de receptor s1p |
| WO2007024922A1 (en) | 2005-08-23 | 2007-03-01 | Irm Llc | Immunosuppressant compounds and compositions |
| WO2007088450A2 (en) | 2006-02-01 | 2007-08-09 | Pfizer Products Inc. | Chromane antagonist of the h-3 receptor |
| JP2009530389A (ja) | 2006-03-21 | 2009-08-27 | エピックス デラウェア, インコーポレイテッド | S1p受容体調節化合物及びその使用 |
| MX2008012738A (es) | 2006-04-03 | 2009-02-06 | Astellas Pharma Inc | Heterocompuesto. |
| JP2009269819A (ja) | 2006-08-25 | 2009-11-19 | Asahi Kasei Pharma Kk | アミン化合物 |
| ES2400163T3 (es) | 2006-09-08 | 2013-04-08 | Actelion Pharmaceuticals Ltd. | Derivados de piridil-3-ilo como agentes de inmunomodulación |
| GB0625648D0 (en) | 2006-12-21 | 2007-01-31 | Glaxo Group Ltd | Compounds |
| PT2125797E (pt) | 2007-03-16 | 2014-03-11 | Actelion Pharmaceuticals Ltd | Derivados aminopiridina como agonistas do receptor s1p1/edg1 |
| ES2622423T3 (es) | 2007-10-04 | 2017-07-06 | Merck Serono S.A. | Derivados de oxadiazol |
| RU2010121969A (ru) | 2007-11-01 | 2011-12-10 | Актелион Фармасьютиклз Лтд (Ch) | Новые производные пиримидина |
| US20090298894A1 (en) * | 2008-04-21 | 2009-12-03 | Asahi Kasei Pharma Corporation | Amino acid compounds |
| EP2389377B1 (en) | 2009-01-23 | 2014-07-16 | Bristol-Myers Squibb Company | Substituted oxadiazole derivatives as s1p agonists in the treatment of autoimmune and inflammatory diseases |
| JP2012515787A (ja) | 2009-01-23 | 2012-07-12 | ブリストル−マイヤーズ スクイブ カンパニー | 自己免疫疾患および炎症性疾患の処置におけるs1pアゴニストとしての置換オキサジアゾール誘導体 |
| ES2405054T3 (es) * | 2009-01-23 | 2013-05-30 | Bristol-Myers Squibb Company | Derivados de pirazol-1,2,4-oxadiazol como agonistas de esfingosina-1-fosfato |
| US8399451B2 (en) | 2009-08-07 | 2013-03-19 | Bristol-Myers Squibb Company | Heterocyclic compounds |
| JP5728487B2 (ja) | 2009-10-29 | 2015-06-03 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 三環式ヘテロ環化合物 |
| WO2011133734A1 (en) | 2010-04-23 | 2011-10-27 | Bristol-Myers Squibb Company | 4 - (5 - isoxazolyl or 5 - pyrrazolyl -1,2,4- oxadiazol - 3 - yl) -mandelic acid amides as sphingosin- 1 - phosphate 1 rreceptor agonists |
| JP5788507B2 (ja) | 2010-07-20 | 2015-09-30 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 置換3−フェニル−1,2,4−オキサジアゾール化合物 |
| EP2619190B1 (en) | 2010-09-24 | 2015-08-12 | Bristol-Myers Squibb Company | Substituted oxadiazole compounds and their use as s1p1 agonists |
-
2011
- 2011-11-02 WO PCT/US2011/058891 patent/WO2012061459A1/en not_active Ceased
- 2011-11-02 ES ES11782723.8T patent/ES2525298T3/es active Active
- 2011-11-02 US US13/883,358 patent/US8629282B2/en active Active
- 2011-11-02 CN CN2011800639683A patent/CN103298807A/zh active Pending
- 2011-11-02 EP EP11782723.8A patent/EP2635573B1/en not_active Not-in-force
- 2011-11-02 JP JP2013537774A patent/JP2013544811A/ja not_active Ceased
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1788008A (zh) * | 2003-05-15 | 2006-06-14 | 麦克公司 | 作为s1p受体激动剂的3-(2-氨基-1-氮杂环基)-5-芳基-1,2,4-噁二唑 |
| CN1859908A (zh) * | 2003-10-01 | 2006-11-08 | 默克公司 | 作为s1p受体激动剂的3,5-芳基、杂芳基或环烷基取代的-1,2,4-噁二唑类化合物 |
| WO2009080728A1 (en) * | 2007-12-21 | 2009-07-02 | Glaxo Group Limited | Oxadiazole derivatives active on sphingosine-1-phosphate (sip) |
| WO2010069949A1 (en) * | 2008-12-18 | 2010-06-24 | Merck Serono S.A. | Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis |
| WO2010072352A1 (en) * | 2008-12-26 | 2010-07-01 | Almirall S.A. | 1, 2, 4 -oxadiazole derivatives and their therapeutic use |
| WO2010081692A1 (en) * | 2009-01-19 | 2010-07-22 | Almirall, S.A. | Oxadiazole derivatives as slpl receptor agonists |
Non-Patent Citations (1)
| Title |
|---|
| 刘魏,等: "免疫抑制剂的研究新进展", 《药学进展》 * |
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018014862A1 (zh) * | 2016-07-22 | 2018-01-25 | 南京明德新药研发股份有限公司 | S1p1激动剂及其应用 |
| CN109661391A (zh) * | 2016-07-22 | 2019-04-19 | 石家庄智康弘仁新药开发有限公司 | S1p1激动剂及其应用 |
| US11192886B2 (en) | 2016-07-22 | 2021-12-07 | Medshine Discovery Inc. | S1P1 agonist and application thereof |
| CN109661391B (zh) * | 2016-07-22 | 2022-04-19 | 南京明德新药研发有限公司 | S1p1激动剂及其应用 |
| WO2019141245A1 (zh) * | 2018-01-18 | 2019-07-25 | 南京明德新药研发股份有限公司 | 一种三并环化合物的晶型、盐型及其制备方法 |
| CN111683946A (zh) * | 2018-01-18 | 2020-09-18 | 石家庄智康弘仁新药开发有限公司 | 一种三并环化合物的晶型、盐型及其制备方法 |
| US11465995B2 (en) | 2018-01-18 | 2022-10-11 | Medshine Discovery Inc. | Crystal and salt forms of tricyclic compound and preparation process thereof |
| CN115038437A (zh) * | 2019-11-20 | 2022-09-09 | 艾尼纳制药公司 | 治疗与s1p1受体相关的病症的方法 |
| TWI895298B (zh) * | 2019-11-20 | 2025-09-01 | 美商艾尼納製藥公司 | 受體相關之病況的方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| US8629282B2 (en) | 2014-01-14 |
| US20130237566A1 (en) | 2013-09-12 |
| JP2013544811A (ja) | 2013-12-19 |
| EP2635573A1 (en) | 2013-09-11 |
| WO2012061459A1 (en) | 2012-05-10 |
| ES2525298T3 (es) | 2014-12-19 |
| EP2635573B1 (en) | 2014-10-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| AD01 | Patent right deemed abandoned |
Effective date of abandoning: 20170111 |
|
| AD01 | Patent right deemed abandoned |