AR078884A1 - Antagonistas del receptor crth2 basados en indol - Google Patents
Antagonistas del receptor crth2 basados en indolInfo
- Publication number
- AR078884A1 AR078884A1 ARP100104065A ARP100104065A AR078884A1 AR 078884 A1 AR078884 A1 AR 078884A1 AR P100104065 A ARP100104065 A AR P100104065A AR P100104065 A ARP100104065 A AR P100104065A AR 078884 A1 AR078884 A1 AR 078884A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- cycloalkyl
- heterocycloalkyl
- Prior art date
Links
- 102000009389 Prostaglandin D receptors Human genes 0.000 title 1
- 108050000258 Prostaglandin D receptors Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Como antagonistas de los receptores CRTH2. También se desvelan composiciones farmacéuticas que contienen compuestos de Formula (1) y el uso de compuestos de Formula (1) para tratar enfermedades o trastornos que son sensibles a la inhibicion de la union de ligandos endogenos al receptor CRTH2. Reivindicacion 1: Un compuesto de Formula (1): o una sal farmacéuticamente aceptable del mismo; en la que: - - - - - es un enlace sencillo o un doble enlace o está ausente; cada uno de R1 y R2 es independientemente H, halogeno, OR6, SO2R7, NR8R9, o alquilo; en los que R6 es H o alquilo; R7 es alquilo; cada uno de R8 y R9 es independientemente H, COCH3 o alquilo; R3 es hidroxi, alquilo, alquenilo, alquinilo, arilo, heteroarilo, cicloalquilo o heterocicloalquilo, en los que cada alquilo, alquenilo, arilo, heteroarilo, cicloalquilo, heterocicloalquilo está opcionalmente sustituido con Ra; siendo Ra alquilo, arilo, heteroarilo, cicloalquilo, alcoxi, fenoxi, halogeno, hidroxi, amino, mono- o di-alquilamino, nitro, haloalquilo, haloalcoxi, halofenoxi, CO, carboxamida, sulfonamida o SO2Me, en los que cada alquilo, arilo, heteroarilo está opcionalmente sustituido adicionalmente con H, alquilo, arilo, alcoxi, fenoxi, halogeno, hidroxi, haloalquilo, haloalcoxi, halofenoxi o SO2Me; R4 es H o alquilo; R5 es CR10R11COOR12, CR10R11CR13NR14R15, COR17, CR10R11CN, CR10R11CR19; en los que cada uno de R10 y R11 es independientemente H o alquilo; R es H o alquilo; R13 es O; cada uno de R14 y R15 es independientemente H, COCH3, SO2R16, alquilo, arilo, heteroarilo, cicloalquilo o heterocicloalquilo; en los que R16 es H, alquilo, arilo, heteroarilo, cicloalquilo o heterocicloalquilo; R17 es alquilo, arilo, heteroarilo, estando cada uno de ellos opcionalmente sustituido con -OH u OR18; en los que R18 es alquilo; R19 es alquilo; arilo, heteroarilo o alquilo opcionalmente sustituido con -OH; X es CH o N; y n es 0 o 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25797509P | 2009-11-04 | 2009-11-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078884A1 true AR078884A1 (es) | 2011-12-07 |
Family
ID=43413493
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104065A AR078884A1 (es) | 2009-11-04 | 2010-11-03 | Antagonistas del receptor crth2 basados en indol |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20110105509A1 (es) |
| AR (1) | AR078884A1 (es) |
| TW (1) | TW201127823A (es) |
| UY (1) | UY32996A (es) |
| WO (1) | WO2011055270A1 (es) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0610680D0 (en) * | 2006-05-31 | 2006-07-12 | Istituto Di Ricerche D Biolog | Therapeutic compounds |
| BR112013000254A2 (pt) | 2010-07-05 | 2016-05-24 | Actelion Pharmaceuticals Ltd | derivados heterocíclicos 1-fenil-substituídos e seu uso como moduladores do receptor de prostaglandina d2 |
| US9044451B2 (en) | 2010-07-19 | 2015-06-02 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Use of delta tocopherol for the treatment of lysosomal storage disorders |
| SG193902A1 (en) | 2011-04-14 | 2013-11-29 | Actelion Pharmaceuticals Ltd | 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives and their use as prostaglandin d2 receptor modulators |
| EP2548863A1 (en) * | 2011-07-18 | 2013-01-23 | Almirall, S.A. | New CRTh2 antagonists. |
| US9206128B2 (en) | 2011-11-18 | 2015-12-08 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US9051269B2 (en) | 2011-11-18 | 2015-06-09 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| WO2013093842A1 (en) | 2011-12-21 | 2013-06-27 | Actelion Pharmaceuticals Ltd | Heterocyclyl derivatives and their use as prostaglandin d2 receptor modulators |
| NZ628762A (en) | 2012-02-10 | 2016-07-29 | Constellation Pharmaceuticals Inc | Modulators of methyl modifying enzymes, compositions and uses thereof |
| CN104428305A (zh) | 2012-07-05 | 2015-03-18 | 埃科特莱茵药品有限公司 | 1-苯基-取代的杂环衍生物及其作为前列腺素d2受体调节剂的用途 |
| WO2014026329A1 (en) * | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof |
| WO2014026328A1 (en) * | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 3-cyclohexenyl substituted indole and indazole compounds as rorgammat inhibitors and uses thereof |
| AR092742A1 (es) * | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| WO2014078573A2 (en) | 2012-11-16 | 2014-05-22 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Tocopherol and tocopheryl quinone derivatives as correctors of lysosomal storage disorders |
| MX365950B (es) * | 2013-03-13 | 2019-06-19 | Flatley Discovery Lab Llc | Compuestos de piridazinona y metodos para el tratamiento de la fibrosis quistica. |
| EP2970305B1 (en) | 2013-03-15 | 2017-02-22 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| WO2015023915A1 (en) | 2013-08-15 | 2015-02-19 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| GB201322273D0 (en) * | 2013-12-17 | 2014-01-29 | Atopix Therapeutics Ltd | Process |
| UA117780C2 (uk) | 2014-03-17 | 2018-09-25 | Ідорсія Фармасьютікалз Лтд | Похідні азаіндолоцтової кислоти та їх застосування як модуляторів рецепторів простагландину d2 |
| TW201620909A (zh) | 2014-03-18 | 2016-06-16 | 艾克泰聯製藥有限公司 | 氮雜吲哚乙酸衍生物及彼等作為前列腺素d2受體調節劑之用途 |
| CA2943363A1 (en) * | 2014-04-02 | 2015-10-08 | Intermune, Inc. | Anti-fibrotic pyridinones |
| TWI695831B (zh) * | 2014-09-13 | 2020-06-11 | 香港商南北兄弟藥業投資有限公司 | Crth2拮抗劑化合物及其用途 |
| CN106467495A (zh) * | 2015-08-19 | 2017-03-01 | 中国科学院上海药物研究所 | 哒嗪酮类化合物、其制备方法、药物组合物及用途 |
| US10577350B2 (en) | 2015-08-28 | 2020-03-03 | Constellation Pharmaceuticals, Inc. | Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide |
| MX379014B (es) | 2015-09-15 | 2025-03-10 | Idorsia Pharmaceuticals Ltd | Formas cristalinas. |
| EP3529242A1 (en) | 2016-10-19 | 2019-08-28 | Constellation Pharmaceuticals, Inc. | Synthesis of inhibitors of ezh2 |
| JP7012822B2 (ja) * | 2017-08-10 | 2022-02-14 | 中国科学院上海薬物研究所 | フタラジノン系化合物、その製造方法、医薬組成物及びその使用 |
| SI3746441T1 (sl) * | 2018-02-02 | 2023-08-31 | Genentech Inc. | Farmacevtska spojina, njene soli, njene formulacije ter postopki izdelave in uporabe le-teh |
| CN110143945B (zh) * | 2018-02-14 | 2021-01-01 | 新发药业有限公司 | 一种4-取代基甲基-1-(2h)酞嗪酮的简便制备方法 |
| CN112125881B (zh) * | 2019-06-25 | 2023-03-28 | 中国科学院上海药物研究所 | 4-吡啶取代酞嗪酮类化合物、其制备方法、药物组合物及用途 |
| CN112679469B (zh) * | 2020-12-29 | 2021-11-16 | 山东研峰新材料科技有限公司 | 一种四氢异喹啉类衍生物、制备方法及应用 |
| CN114835677B (zh) * | 2021-02-02 | 2025-09-26 | 广东东阳光药业股份有限公司 | 吲哚衍生物的盐及其用途 |
| CN114835678A (zh) * | 2021-02-02 | 2022-08-02 | 广东东阳光药业有限公司 | 吲哚衍生物的盐及其用途 |
| CN114989136A (zh) * | 2021-02-02 | 2022-09-02 | 广东东阳光药业有限公司 | 吲哚衍生物的盐及其用途 |
| WO2023086799A1 (en) * | 2021-11-09 | 2023-05-19 | Vigil Neuroscience, Inc. | Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0200411D0 (sv) | 2002-02-05 | 2002-02-05 | Astrazeneca Ab | Novel use |
| SE0200356D0 (sv) | 2002-02-05 | 2002-02-05 | Astrazeneca Ab | Novel use |
| SE0201635D0 (sv) | 2002-05-30 | 2002-05-30 | Astrazeneca Ab | Novel compounds |
| TW200307542A (en) | 2002-05-30 | 2003-12-16 | Astrazeneca Ab | Novel compounds |
| SE0202241D0 (sv) | 2002-07-17 | 2002-07-17 | Astrazeneca Ab | Novel Compounds |
| MX2007003325A (es) | 2004-09-20 | 2007-06-05 | Xenon Pharmaceuticals Inc | Derivados heterociclicos y su uso como inhibidores estearoil-coa-desaturasa. |
| KR20070089908A (ko) * | 2004-09-21 | 2007-09-04 | 아더시스 인코포레이티드 | Crth2 수용체 길항작용을 나타내는 인돌 아세트산 및이의 용도 |
-
2010
- 2010-10-26 WO PCT/IB2010/054845 patent/WO2011055270A1/en not_active Ceased
- 2010-11-01 TW TW099137477A patent/TW201127823A/zh unknown
- 2010-11-03 AR ARP100104065A patent/AR078884A1/es not_active Application Discontinuation
- 2010-11-03 US US12/938,479 patent/US20110105509A1/en not_active Abandoned
- 2010-11-03 UY UY0001032996A patent/UY32996A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011055270A1 (en) | 2011-05-12 |
| US20110105509A1 (en) | 2011-05-05 |
| TW201127823A (en) | 2011-08-16 |
| UY32996A (es) | 2011-06-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |