AR078884A1 - Antagonistas del receptor crth2 basados en indol - Google Patents

Antagonistas del receptor crth2 basados en indol

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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
Application number
ARP100104065A
Other languages
English (en)
Original Assignee
Wyeth Llc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Wyeth Llc filed Critical Wyeth Llc
Publication of AR078884A1 publication Critical patent/AR078884A1/es

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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.
ARP100104065A 2009-11-04 2010-11-03 Antagonistas del receptor crth2 basados en indol AR078884A1 (es)

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0610680D0 (en) * 2006-05-31 2006-07-12 Istituto Di Ricerche D Biolog Therapeutic compounds
JP5800898B2 (ja) 2010-07-05 2015-10-28 アクテリオン ファーマシューティカルズ リミテッドＡｃｔｅｌｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ １−フェニル−置換ヘテロシクリル誘導体及びプロスタグランジンｄ２受容体調節剤としてのそれらの使用
EP2595623B1 (en) 2010-07-19 2018-02-28 The U.S.A. as represented by the Secretary, Department of Health and Human Services Use of delta tocopherol for the treatment of lysosomal storage disorders
MY165623A (en) 2011-04-14 2018-04-18 Idorsia 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.
WO2013075084A1 (en) 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US9206128B2 (en) 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
RU2014129613A (ru) 2011-12-21 2016-02-10 Актелион Фармасьютиклз Лтд Гетероциклильные производные и их применение в качестве модуляторов рецептора простагландина d2
WO2013120104A2 (en) 2012-02-10 2013-08-15 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US9169270B2 (en) 2012-07-05 2015-10-27 Actelion Pharmaceuticals Ltd. 1-phenyl-substituted heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators
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
JP6367211B2 (ja) * 2012-11-16 2018-08-01 ザ ユナイテッド ステイツ オブ アメリカ， アズ リプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ リソソーム蓄積症の改善物質としてのトコフェロール誘導体およびトコフェリルキノン誘導体
US9783529B2 (en) 2013-03-13 2017-10-10 Flatley Discovery Lab, Llc Pyridazinone compounds and methods for the treatment of cystic fibrosis
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP3033334A1 (en) 2013-08-15 2016-06-22 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
HRP20181555T1 (hr) 2014-03-17 2018-11-30 Idorsia Pharmaceuticals Ltd Derivati azaindol-octene kiseline i njihova uporaba kao modulatora receptora prostaglandina d2
RU2016140708A (ru) 2014-03-18 2018-04-18 Идорсиа Фармасьютиклз Лтд Производные азаиндол уксусной кислоты и их применение в качестве модуляторов рецептора простагландина d2
CN106459042B (zh) * 2014-04-02 2019-06-28 英特穆恩公司 抗纤维化吡啶酮类
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
PL3350179T3 (pl) 2015-09-15 2021-08-02 Idorsia Pharmaceuticals Ltd Krystaliczne postacie
CA3039059A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
EP3666767B1 (en) * 2017-08-10 2021-12-01 Shanghai Institute of Materia Medica, Chinese Academy of Sciences Phthalazinone derivatives, method for their preparation thereof, pharmaceutical composition comprising them, and their use
KR20260007293A (ko) * 2018-02-02 2026-01-13 제넨테크, 인크. 약제학적 화합물, 이의 염, 이의 제형, 그리고 이의 제조 방법 및 사용 방법
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
WO2020259539A1 (zh) * 2019-06-25 2020-12-30 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
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
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
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
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)

* Cited by examiner, † Cited by third party
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
CA2580855A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
EP1805171A4 (en) * 2004-09-21 2009-05-13 Wyeth Corp CRTH2 RECEPTOR ANTAGONISM DISPLAYING INDIGENOUS ACIDS AND APPLICATIONS THEREOF

Also Published As

Publication number Publication date
UY32996A (es) 2011-06-30
TW201127823A (en) 2011-08-16
WO2011055270A1 (en) 2011-05-12
US20110105509A1 (en) 2011-05-05

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