JP2013510884A5 - - Google Patents
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- JP2013510884A5 JP2013510884A5 JP2012539064A JP2012539064A JP2013510884A5 JP 2013510884 A5 JP2013510884 A5 JP 2013510884A5 JP 2012539064 A JP2012539064 A JP 2012539064A JP 2012539064 A JP2012539064 A JP 2012539064A JP 2013510884 A5 JP2013510884 A5 JP 2013510884A5
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- JP
- Japan
- Prior art keywords
- compound
- formula
- alkyl
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- group
- 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 57
- 238000000034 method Methods 0.000 claims 24
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 229910052799 carbon Inorganic materials 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 13
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 10
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 239000012069 chiral reagent Substances 0.000 claims 8
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 claims 6
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 150000002148 esters Chemical class 0.000 claims 5
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 239000003223 protective agent Substances 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 3
- -1 NH 2 Chemical group 0.000 claims 3
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 3
- 230000004913 activation Effects 0.000 claims 3
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 3
- 125000003277 amino group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229940002612 prodrug Drugs 0.000 claims 3
- 239000000651 prodrug Substances 0.000 claims 3
- 102000005962 receptors Human genes 0.000 claims 3
- 108020003175 receptors Proteins 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- IPWKHHSGDUIRAH-UHFFFAOYSA-N bis(pinacolato)diboron Chemical compound O1C(C)(C)C(C)(C)OB1B1OC(C)(C)C(C)(C)O1 IPWKHHSGDUIRAH-UHFFFAOYSA-N 0.000 claims 2
- 239000003638 chemical reducing agent Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- BDOLXPFAFMNDOK-UHFFFAOYSA-N oxazaborolidine Chemical compound B1CCON1 BDOLXPFAFMNDOK-UHFFFAOYSA-N 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- DYHSDKLCOJIUFX-UHFFFAOYSA-N tert-butoxycarbonyl anhydride Chemical group CC(C)(C)OC(=O)OC(=O)OC(C)(C)C DYHSDKLCOJIUFX-UHFFFAOYSA-N 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 235000004279 alanine Nutrition 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 229960001230 asparagine Drugs 0.000 claims 1
- 235000009582 asparagine Nutrition 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 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
- 239000012351 deprotecting agent Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- PQNFLJBBNBOBRQ-UHFFFAOYSA-N indane Chemical group C1=CC=C2CCCC2=C1 PQNFLJBBNBOBRQ-UHFFFAOYSA-N 0.000 claims 1
- 206010022000 influenza Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000000467 secondary amino group Chemical class [H]N([*:1])[*:2] 0.000 claims 1
- WBQTXTBONIWRGK-UHFFFAOYSA-N sodium;propan-2-olate Chemical compound [Na+].CC(C)[O-] WBQTXTBONIWRGK-UHFFFAOYSA-N 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000001010 sulfinic acid amide group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 230000002194 synthesizing effect Effects 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- BCNZYOJHNLTNEZ-UHFFFAOYSA-N tert-butyldimethylsilyl chloride Chemical group CC(C)(C)[Si](C)(C)Cl BCNZYOJHNLTNEZ-UHFFFAOYSA-N 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- QJBPMJZFMIHODS-UHFFFAOYSA-N CC1(C)OB(c2c(CCC#C3)c3ccc2)OC1(C)C Chemical compound CC1(C)OB(c2c(CCC#C3)c3ccc2)OC1(C)C QJBPMJZFMIHODS-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26129509P | 2009-11-13 | 2009-11-13 | |
| US61/261,295 | 2009-11-13 | ||
| US26247409P | 2009-11-18 | 2009-11-18 | |
| US61/262,474 | 2009-11-18 | ||
| PCT/US2010/056759 WO2011060391A1 (en) | 2009-11-13 | 2010-11-15 | Selective heterocyclic sphingosine 1 phosphate receptor modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013510884A JP2013510884A (ja) | 2013-03-28 |
| JP2013510884A5 true JP2013510884A5 (enExample) | 2014-01-09 |
| JP5922027B2 JP5922027B2 (ja) | 2016-05-24 |
Family
ID=43992105
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012539064A Active JP5922027B2 (ja) | 2009-11-13 | 2010-11-15 | 選択的複素環式スフィンゴシン−１−リン酸受容体変調因子 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US8507538B2 (enExample) |
| EP (1) | EP2498609B1 (enExample) |
| JP (1) | JP5922027B2 (enExample) |
| KR (1) | KR101771755B1 (enExample) |
| CN (2) | CN105130922A (enExample) |
| AU (1) | AU2010319982B2 (enExample) |
| BR (1) | BR112012011431A8 (enExample) |
| CA (1) | CA2780641C (enExample) |
| DK (1) | DK2498609T3 (enExample) |
| EA (1) | EA025672B1 (enExample) |
| ES (1) | ES2675799T3 (enExample) |
| HK (1) | HK1213873A1 (enExample) |
| IL (1) | IL219692A (enExample) |
| MX (1) | MX2012005559A (enExample) |
| MY (1) | MY169497A (enExample) |
| NZ (1) | NZ599914A (enExample) |
| PH (1) | PH12012500940B1 (enExample) |
| PT (1) | PT2498609T (enExample) |
| WO (1) | WO2011060391A1 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2902991B2 (ja) | 1996-02-14 | 1999-06-07 | 株式会社安部工業所 | Ｐｃ構造物の自動緊張システム装置 |
| HUE037535T2 (hu) * | 2009-11-13 | 2018-09-28 | Celgene Int Ii Sarl | Szelektív szfingozin-1-foszfát receptor modulátorok és királis szintézis eljárások |
| BR112012011430A8 (pt) * | 2009-11-13 | 2017-12-26 | Celgene Int Ii Sarl | Compostos moduladores de receptor de esfingosina 1 fosfato e composições farmacêuticas |
| ES2758841T3 (es) * | 2011-05-13 | 2020-05-06 | Celgene Int Ii Sarl | Moduladores heterocíclicos selectivos del receptor de la esfingosina-1-fosfato |
| BR112014031565B1 (pt) * | 2012-06-21 | 2022-04-12 | Eisai R&D Management Co., Ltd | Derivado de indanossulfamida inovador |
| EP2958913B1 (en) * | 2013-02-20 | 2018-10-03 | LG Chem, Ltd. | Sphingosine-1-phosphate receptor agonists, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent |
| CN106187945A (zh) * | 2016-07-22 | 2016-12-07 | 辽宁师范大学 | 一种有机合成中间体的合成方法 |
| WO2018028557A1 (zh) * | 2016-08-08 | 2018-02-15 | 南京明德新药研发股份有限公司 | 三环类化合物及其应用 |
| MX2020009100A (es) | 2018-03-20 | 2020-12-03 | Eisai R&D Man Co Ltd | Agente de tratamiento de la epilepsia. |
| CN112062785B (zh) * | 2019-06-11 | 2023-06-27 | 广东东阳光药业有限公司 | 奥扎莫德及其中间体的制备方法 |
| KR20220124209A (ko) * | 2020-01-06 | 2022-09-13 | 아레나 파마슈티칼스, 인크. | S1p1 수용체와 관련된 이상의 치료 방법 |
| EP4212159A4 (en) * | 2020-09-28 | 2024-03-06 | Lg Chem, Ltd. | USE OF SPHINGOSINE-1 PHOSPHATE RECEPTOR AGONISTS |
| KR20220043047A (ko) * | 2020-09-28 | 2022-04-05 | 주식회사 엘지화학 | 스핑고신-1-인산 수용체 효능제의 용도 |
| US20240207242A1 (en) * | 2021-04-14 | 2024-06-27 | Lg Chem, Ltd. | Pharmaceutical composition comprising sphingosine-1-phosphate receptor agonist with controlled particle size |
| WO2022220595A1 (ko) * | 2021-04-14 | 2022-10-20 | 주식회사 엘지화학 | 스핑고신-1-인산 수용체 효능제를 포함하는 고형 제제의 제조 방법 |
| KR102858772B1 (ko) * | 2021-04-14 | 2025-09-11 | 주식회사 엘지화학 | 스핑고신-1-인산 수용체 효능제를 포함하는 직접 타정용 약제학적 조성물 |
| WO2022220596A1 (ko) * | 2021-04-14 | 2022-10-20 | 주식회사 엘지화학 | 습식과립법에 의한 스핑고신-1-인산 수용체 효능제를 포함하는 경구용 고형 제제의 제조 방법 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2628103B1 (fr) * | 1988-03-03 | 1991-06-14 | Roussel Uclaf | Nouveaux esters pyrethrinoides portant un noyau indanyle, leur procede de preparation et leur application comme pesticides |
| US5039802A (en) * | 1990-04-18 | 1991-08-13 | Merck & Co., Inc. | Arylation process for preparation of chiral catalysts for ketone reduction |
| TR200002072T2 (tr) * | 1998-01-23 | 2000-12-21 | Sankyo Company Limited | Spiropiperidin türevleri |
| CA2509218C (en) * | 2002-12-20 | 2010-09-07 | Merck & Co., Inc. | 1-(amino)indanes and (1,2-dihydro-3-amino)-benzofurans, benzothiophenes and indoles as edg receptor agonists |
| AU2004277947A1 (en) | 2003-10-01 | 2005-04-14 | Merck & Co., Inc. | 3,5-aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as S1P receptor agonists |
| AU2004299456B2 (en) * | 2003-12-17 | 2010-10-07 | Merck Sharp & Dohme Corp. | (3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists |
| US7585881B2 (en) | 2004-02-18 | 2009-09-08 | Astrazeneca Ab | Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| US20060173183A1 (en) * | 2004-12-31 | 2006-08-03 | Alantos Pharmaceuticals, Inc., | Multicyclic bis-amide MMP inhibitors |
| EP1851188A1 (en) | 2005-02-22 | 2007-11-07 | Teva Pharmaceutical Industries Limited | Improved process for the synthesis of enantiomeric indanylamine derivatives |
| KR100667075B1 (ko) * | 2005-07-22 | 2007-01-10 | 삼성에스디아이 주식회사 | 주사 구동부 및 이를 포함하는 유기 전계발광 표시장치 |
| US20090163482A1 (en) * | 2006-03-13 | 2009-06-25 | Mchardy Stanton Furst | Tetralines antagonists of the h-3 receptor |
| US20080009534A1 (en) * | 2006-07-07 | 2008-01-10 | Bristol-Myers Squibb Company | Substituted acid derivatives useful as antidiabetic and antiobesity agents and method |
| MX2009006304A (es) | 2006-12-15 | 2009-06-23 | Abbott Lab | Nuevos compuestos de oxadiazol. |
| WO2009131090A1 (ja) * | 2008-04-21 | 2009-10-29 | 旭化成ファーマ株式会社 | アミノ酸化合物 |
| EP2913326B1 (en) * | 2008-05-14 | 2020-07-15 | The Scripps Research Institute | Novel modulators of sphingosine phosphate receptors |
-
2010
- 2010-11-15 CN CN201510369450.2A patent/CN105130922A/zh active Pending
- 2010-11-15 EA EA201290329A patent/EA025672B1/ru not_active IP Right Cessation
- 2010-11-15 PH PH1/2012/500940A patent/PH12012500940B1/en unknown
- 2010-11-15 DK DK10830879.2T patent/DK2498609T3/en active
- 2010-11-15 NZ NZ599914A patent/NZ599914A/en unknown
- 2010-11-15 EP EP10830879.2A patent/EP2498609B1/en active Active
- 2010-11-15 WO PCT/US2010/056759 patent/WO2011060391A1/en not_active Ceased
- 2010-11-15 MY MYPI2012002100A patent/MY169497A/en unknown
- 2010-11-15 BR BR112012011431A patent/BR112012011431A8/pt not_active Application Discontinuation
- 2010-11-15 US US12/946,828 patent/US8507538B2/en active Active
- 2010-11-15 CA CA2780641A patent/CA2780641C/en active Active
- 2010-11-15 AU AU2010319982A patent/AU2010319982B2/en active Active
- 2010-11-15 MX MX2012005559A patent/MX2012005559A/es active IP Right Grant
- 2010-11-15 KR KR1020127015220A patent/KR101771755B1/ko active Active
- 2010-11-15 JP JP2012539064A patent/JP5922027B2/ja active Active
- 2010-11-15 CN CN201080061373.XA patent/CN102753022B/zh active Active
- 2010-11-15 ES ES10830879.2T patent/ES2675799T3/es active Active
- 2010-11-15 PT PT108308792T patent/PT2498609T/pt unknown
-
2012
- 2012-05-09 IL IL219692A patent/IL219692A/en active IP Right Grant
-
2013
- 2013-03-14 HK HK16100725.4A patent/HK1213873A1/zh unknown
- 2013-07-15 US US13/941,695 patent/US20140039183A1/en not_active Abandoned
-
2014
- 2014-12-08 US US14/563,742 patent/US20150252037A1/en not_active Abandoned