JP2010515750A5 - - Google Patents
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- Publication number
- JP2010515750A5 JP2010515750A5 JP2009545669A JP2009545669A JP2010515750A5 JP 2010515750 A5 JP2010515750 A5 JP 2010515750A5 JP 2009545669 A JP2009545669 A JP 2009545669A JP 2009545669 A JP2009545669 A JP 2009545669A JP 2010515750 A5 JP2010515750 A5 JP 2010515750A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- carbon atoms
- groups
- nitrogen
- ring
- 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.)
- Abandoned
Links
- 125000004432 carbon atom Chemical group C* 0.000 claims 46
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 15
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 14
- 229910052717 sulfur Inorganic materials 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 125000002837 carbocyclic group Chemical group 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 10
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 10
- 239000001301 oxygen Substances 0.000 claims 10
- 239000011593 sulfur Substances 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 8
- 125000000304 alkynyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 4
- 125000004642 (C1-C12) alkoxy group Chemical group 0.000 claims 2
- 125000004641 (C1-C12) haloalkyl group Chemical group 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 2
- 125000005599 alkyl carboxylate group Chemical group 0.000 claims 2
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 2
- 125000003368 amide group Chemical group 0.000 claims 2
- 125000003277 amino group Chemical group 0.000 claims 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 2
- 230000004071 biological effect Effects 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 150000001721 carbon Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000000664 diazo group Chemical group [N-]=[N+]=[*] 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000004962 sulfoxyl group Chemical group 0.000 claims 2
- 125000004149 thio group Chemical group *S* 0.000 claims 2
- -1 wherein Chemical compound 0.000 claims 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 229940122625 Phosphate antagonist Drugs 0.000 claims 1
- 229940121846 Sphingosine 1-phosphate receptor agonist Drugs 0.000 claims 1
- 229940122286 Sphingosine 1-phosphate receptor antagonist Drugs 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 229940044551 receptor antagonist Drugs 0.000 claims 1
- 239000002464 receptor antagonist Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- DUYSYHSSBDVJSM-KRWOKUGFSA-N sphingosine 1-phosphate Chemical compound CCCCCCCCCCCCC\C=C\[C@@H](O)[C@@H](N)COP(O)(O)=O DUYSYHSSBDVJSM-KRWOKUGFSA-N 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88447007P | 2007-01-11 | 2007-01-11 | |
| PCT/US2008/050695 WO2008089015A1 (en) | 2007-01-11 | 2008-01-10 | 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (s1p) receptor antagonist biological activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010515750A JP2010515750A (ja) | 2010-05-13 |
| JP2010515750A5 true JP2010515750A5 (enExample) | 2011-03-03 |
Family
ID=39399972
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009545669A Abandoned JP2010515750A (ja) | 2007-01-11 | 2008-01-10 | スフィンゴシン−１−ホスフェート（ｓ１ｐ）受容体アンタゴニスト生物活性を有する６−置換インドール−３−カルボン酸アミド化合物 |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP2125723A1 (enExample) |
| JP (1) | JP2010515750A (enExample) |
| KR (1) | KR20090101307A (enExample) |
| CN (1) | CN101668741A (enExample) |
| AU (1) | AU2008206495A1 (enExample) |
| CA (1) | CA2674946A1 (enExample) |
| MX (1) | MX2009007334A (enExample) |
| WO (1) | WO2008089015A1 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8524917B2 (en) * | 2007-01-11 | 2013-09-03 | Allergan, Inc. | 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity |
| JP2011514385A (ja) * | 2008-03-17 | 2011-05-06 | アラーガン、インコーポレイテッド | 炎症を処置するためのｓ１ｐ３受容体阻害剤 |
| MX354134B (es) | 2008-07-23 | 2018-02-14 | Arena Pharm Inc | Derivados de acido 1,2,3,4-tetrahidrociclopenta [b] indol-3-il) acetico sustituidos utiles en el tratamiento de enfermedades autoinmune e inflamatorias. |
| NZ591001A (en) | 2008-08-27 | 2012-11-30 | Arena Pharm Inc | Substituted tricyclic acid derivatives as s1p1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders |
| EP4148045A1 (en) | 2010-01-27 | 2023-03-15 | Arena Pharmaceuticals, Inc. | Intermediate compounds for the preparation of (r)-2-(7-(4-cyclopentyl-3- (trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b] indol-3-yl)acetic acid and salts thereof |
| SG183416A1 (en) | 2010-03-03 | 2012-09-27 | Arena Pharm Inc | Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof |
| TWI522361B (zh) * | 2010-07-09 | 2016-02-21 | 艾伯維公司 | 作為s1p調節劑的稠合雜環衍生物 |
| PE20161035A1 (es) | 2013-03-15 | 2016-11-13 | Global Blood Therapeutics Inc | Compuestos y usos de estos para la modulacion de la hemoglobina |
| EA202092627A1 (ru) | 2013-11-18 | 2021-09-30 | Глобал Блад Терапьютикс, Инк. | Соединения и их применения для модуляции гемоглобина |
| KR102595163B1 (ko) | 2015-01-06 | 2023-10-30 | 아레나 파마슈티칼스, 인크. | S1p1 수용체와 관련된 상태의 치료 방법 |
| EA201890096A1 (ru) | 2015-06-22 | 2018-08-31 | Арена Фармасьютикалз, Инк. | КРИСТАЛЛИЧЕСКАЯ L-АРГИНИНОВАЯ СОЛЬ (R)-2-(7-(4-ЦИКЛОПЕНТИЛ-3-(ТРИФТОРМЕТИЛ)БЕНЗИЛОКСИ)-1,2,3,4-ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛ-3-ИЛ)УКСУСНОЙ КИСЛОТЫ (СОЕДИНЕНИЯ 1) ДЛЯ ПРИМЕНЕНИЯ ПРИ РАССТРОЙСТВАХ, СВЯЗАННЫХ С S1P-РЕЦЕПТОРОМ |
| EP3402780A1 (en) | 2016-01-14 | 2018-11-21 | Beth Israel Deaconess Medical Center, Inc. | Mast-cell modulators and uses thereof |
| CN110545848A (zh) | 2017-02-16 | 2019-12-06 | 艾尼纳制药公司 | 用于治疗具有肠外表现的炎症性肠病的化合物和方法 |
| CA3053418A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
| CN110483437B (zh) * | 2018-05-14 | 2022-12-06 | 嘉兴维眸生物科技有限公司 | 一种含五元环的化合物及其制备和应用 |
| CN112601516A (zh) | 2018-06-06 | 2021-04-02 | 艾尼纳制药公司 | 治疗与s1p1受体相关的病况的方法 |
| WO2020051378A1 (en) | 2018-09-06 | 2020-03-12 | Arena Pharmaceuticals, Inc. | Compounds useful in the treatment of autoimmune and inflammatory disorders |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2121394A1 (fr) | 1971-01-08 | 1972-08-25 | Anvar | Procédé d'obtention de dérivés d'acides indole carboxyliques et produits préparables par ce procédé. |
| EP0146810A3 (de) | 1983-12-05 | 1987-05-13 | Solco Basel AG | Verfahren zur Herstellung von Sphingosinderivaten |
| US5110987A (en) | 1988-06-17 | 1992-05-05 | Emory University | Method of preparing sphingosine derivatives |
| ZA902794B (en) | 1989-04-18 | 1991-04-24 | Duphar Int Res | New 3-n substituted carbamoyl-indole derivatives |
| US5294722A (en) | 1992-04-16 | 1994-03-15 | E. R. Squibb & Sons, Inc. | Process for the preparation of imidazoles useful in angiotensin II antagonism |
| US5403851A (en) | 1994-04-05 | 1995-04-04 | Interneuron Pharmaceuticals, Inc. | Substituted tryptamines, phenalkylamines and related compounds |
| HUP9900424A2 (hu) * | 1996-01-22 | 1999-05-28 | Fujisawa Pharmaceutical Co., Ltd. | Tiazolil-benzfurán-származékok és a vegyületeket tartalmazó gyógyászati készítmények |
| EP1002790B1 (en) | 1997-03-12 | 2005-12-28 | Takara Bio Inc. | Sphingosine analogues |
| EP1020429B1 (en) | 1997-09-11 | 2006-07-12 | Takara Bio Inc. | Sphingosine derivatives and medicinal composition |
| DE19753522A1 (de) | 1997-12-03 | 1999-06-10 | Boehringer Ingelheim Pharma | Substituierte Indole, ihre Herstellung und ihre Verwendung als Arzneimittel |
| MXPA01007033A (es) * | 1999-01-13 | 2003-07-21 | Millennium Pharm Inc | Heterociclos funcionalizados como moduladores de receptores de quimiocinas. |
| AU2001264313A1 (en) | 2000-06-20 | 2002-01-02 | Japan Tobacco Inc. | Pyrazolopyridine compounds and use thereof as drugs |
| DE60221391T2 (de) | 2001-06-20 | 2008-04-17 | Wyeth | Substituierte indolsäurederivate als inhibitoren von plasminogen-aktivator-inhibitor-1 (pai-1) |
| WO2003070691A1 (en) * | 2002-02-21 | 2003-08-28 | Osaka Industrial Promotion Organization | N-hydroxycarboxamide derivative |
| EP1984334B1 (en) | 2006-02-15 | 2014-04-09 | Allergan, Inc. | Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (s1p) receptor antagonist biological activity |
-
2008
- 2008-01-10 KR KR1020097016762A patent/KR20090101307A/ko not_active Withdrawn
- 2008-01-10 CN CN200880007131A patent/CN101668741A/zh active Pending
- 2008-01-10 MX MX2009007334A patent/MX2009007334A/es not_active Application Discontinuation
- 2008-01-10 CA CA002674946A patent/CA2674946A1/en not_active Abandoned
- 2008-01-10 WO PCT/US2008/050695 patent/WO2008089015A1/en not_active Ceased
- 2008-01-10 AU AU2008206495A patent/AU2008206495A1/en not_active Abandoned
- 2008-01-10 EP EP08727502A patent/EP2125723A1/en not_active Withdrawn
- 2008-01-10 JP JP2009545669A patent/JP2010515750A/ja not_active Abandoned
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