[go: up one dir, main page]

PE20191787A1 - Derivados de indol n-sustituidos - Google Patents

Derivados de indol n-sustituidos

Info

Publication number
PE20191787A1
PE20191787A1 PE2019002413A PE2019002413A PE20191787A1 PE 20191787 A1 PE20191787 A1 PE 20191787A1 PE 2019002413 A PE2019002413 A PE 2019002413A PE 2019002413 A PE2019002413 A PE 2019002413A PE 20191787 A1 PE20191787 A1 PE 20191787A1
Authority
PE
Peru
Prior art keywords
indol
methyl
substitute derivatives
compound
derivatives
Prior art date
Application number
PE2019002413A
Other languages
English (en)
Inventor
Heinz Fretz
Isabelle Lyothier
Julien Pothier
Sylvia Richard-Bildstein
Thierry Sifferlen
Original Assignee
Idorsia Pharmaceuticals Ltd
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 Idorsia Pharmaceuticals Ltd filed Critical Idorsia Pharmaceuticals Ltd
Publication of PE20191787A1 publication Critical patent/PE20191787A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Referido a derivados de indol N-sustituidos, un compuesto de formula I, en donde R1 es H o metilo; R2 es metilo, Br, Cl o ciano; o una sal farmaceutica aceptable del mismo. Un compuesto preferido es: acido 4-{6-[2-(2-metil-indol-1-il)-etilamino]-pirimidin-4-il}-benzoico. Estos compuestos son moduladores del receptor EP2 de la prostaglandina 2. Tambien se refiere a metodos para su preparacion, y su uso como composicion farmaceutica.
PE2019002413A 2017-05-18 2018-05-17 Derivados de indol n-sustituidos PE20191787A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP2017062008 2017-05-18
PCT/EP2018/062865 WO2018210995A1 (en) 2017-05-18 2018-05-17 N-substituted indole derivatives

Publications (1)

Publication Number Publication Date
PE20191787A1 true PE20191787A1 (es) 2019-12-24

Family

ID=62186481

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2019002413A PE20191787A1 (es) 2017-05-18 2018-05-17 Derivados de indol n-sustituidos

Country Status (32)

Country Link
US (2) US20200069686A1 (es)
EP (1) EP3625224B1 (es)
JP (1) JP7065117B2 (es)
KR (1) KR102650756B1 (es)
CN (1) CN110621666A (es)
AR (1) AR111806A1 (es)
AU (1) AU2018269667B2 (es)
BR (1) BR112019024114A2 (es)
CA (1) CA3063637A1 (es)
CL (1) CL2019003257A1 (es)
CO (1) CO2019010804A2 (es)
CR (1) CR20190567A (es)
CY (1) CY1124528T1 (es)
DK (1) DK3625224T3 (es)
EA (1) EA039630B1 (es)
ES (1) ES2894124T3 (es)
HR (1) HRP20211532T1 (es)
HU (1) HUE056406T2 (es)
IL (1) IL270616B (es)
LT (1) LT3625224T (es)
MA (1) MA49127B1 (es)
MX (1) MX394108B (es)
PE (1) PE20191787A1 (es)
PH (1) PH12019502562B1 (es)
PL (1) PL3625224T3 (es)
PT (1) PT3625224T (es)
RS (1) RS62441B1 (es)
SG (1) SG11201908660RA (es)
SI (1) SI3625224T1 (es)
TW (1) TWI768043B (es)
UA (1) UA124748C2 (es)
WO (1) WO2018210995A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
EA201992676A1 (ru) 2017-05-18 2020-05-06 Идорсия Фармасьютиклз Лтд Фенильные производные в качестве модуляторов pge2 рецепторов
CA3063788A1 (en) 2017-05-18 2018-11-22 Idorsia Pharmaceuticals Ltd Pyrimidine derivatives
CA3060394A1 (en) 2017-05-18 2018-11-22 Idorsia Pharmaceuticals Ltd Pyrimidine derivatives as pge2 receptor modulators
WO2018210987A1 (en) 2017-05-18 2018-11-22 Idorsia Pharmaceuticals Ltd Benzofurane and benzothiophene derivatives as pge2 receptor modulators
WO2021060281A1 (ja) * 2019-09-24 2021-04-01 Agc株式会社 プロスタグランジンe2レセプターep2/ep4デュアルアンタゴニスト
WO2021205367A1 (en) * 2020-04-08 2021-10-14 Askat Inc. Use of ep4 receptor antagonists for the treatment of liver cancer, melanoma, lymphoma and leukemia
EP4245301A4 (en) 2020-11-13 2024-08-21 ONO Pharmaceutical Co., Ltd. TREATMENT OF CANCER BY COMBINED USE OF AN EP4 ANTAGONIST AND AN IMMUNE CHECKPOINT INHIBITOR
WO2025229177A1 (en) 2024-05-02 2025-11-06 Idorsia Pharmaceuticals Ltd Crystalline forms of an n-substituted indole derivative

Family Cites Families (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1267867T3 (da) 2000-03-24 2008-08-25 Asterand Uk Ltd Anvendelse af prostanoid-EP4-receptorantagonister til behandling af hovedpine og assays til sådanne antagonister
HN2001000224A (es) 2000-10-19 2002-06-13 Pfizer Compuestos de imidazol condensado con arilo o heteroarilo como agentes anti - inflamatorios y analgesicos.
GB0031302D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Napthalene derivatives
GB0031295D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Naphthalene derivatives
GB0103269D0 (en) 2001-02-09 2001-03-28 Glaxo Group Ltd Napthalene derivatives
BR0309305A (pt) 2002-04-12 2005-02-15 Pfizer Compostos de imidazol como agentes antiinflamatórios e analgésicos
WO2003087061A1 (en) 2002-04-12 2003-10-23 Pfizer Japan Inc. Pyrazole compounds as anti-inflammatory and analgesic agents
JP2006506327A (ja) 2002-05-23 2006-02-23 セラテクノロジーズ インコーポレイティド プロスタグランジンe2の受容体サブタイプep4のアンタゴニスト・ポリペプチド
CN100408570C (zh) 2003-01-29 2008-08-06 阿斯特兰德英国有限公司 Ep4受体拮抗剂
EP1661897B1 (en) * 2003-08-26 2013-12-04 Teijin Pharma Limited Pyrrolopyrimidinone derivative
CN1867551B (zh) 2003-09-03 2013-09-11 拉夸里亚创药株式会社 作为前列腺素e2拮抗剂的苯基或吡啶基酰胺化合物
GB0324269D0 (en) 2003-10-16 2003-11-19 Pharmagene Lab Ltd EP4 receptor antagonists
KR20070006891A (ko) 2004-05-04 2007-01-11 화이자 인코포레이티드 치환된 메틸 아릴 또는 헤테로아릴 아미드 화합물
ES2327760T3 (es) 2004-05-04 2009-11-03 Raqualia Pharma Inc Compuestos de aril-heteroaril-amida ortosustituidos.
GT200500284A (es) 2004-10-15 2006-03-27 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
JP5289046B2 (ja) 2005-05-19 2013-09-11 メルク カナダ インコーポレイテッド Ep4アンタゴニストとしてのキノリン誘導体
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
CA2648729A1 (en) 2006-04-24 2007-11-01 Merck Frosst Canada Ltd. Indole amide derivatives as ep4 receptor antagonists
AU2007260529B2 (en) 2006-06-12 2012-04-19 Merck Canada Inc. Indoline amide derivatives as EP4 receptor ligands
WO2008008059A1 (en) 2006-07-12 2008-01-17 Locus Pharmaceuticals, Inc. Anti-cancer agents ans uses thereof
RU2485115C2 (ru) 2006-07-14 2013-06-20 Новартис Аг Производные пиримидина в качестве ингибиторов alk-5
ES2421453T3 (es) 2006-08-11 2013-09-02 Merck Frosst Canada Ltd Derivados de tiofenocarboxamida como ligandos del receptor EP4
WO2008039882A1 (en) 2006-09-30 2008-04-03 Sanofi-Aventis U.S. Llc A combination of niacin and a prostaglandin d2 receptor antagonist
CN101622230B (zh) 2007-02-26 2012-08-22 默克弗罗斯特加拿大有限公司 作为ep4受体拮抗剂的吲哚和二氢吲哚环丙基酰胺衍生物
WO2008116304A1 (en) 2007-03-26 2008-10-02 Merck Frosst Canada Ltd. Naphthalene and quinoline sulfonylurea derivatives as ep4 receptor antagonists
CA2681861A1 (en) 2007-03-26 2008-10-16 Astellas Pharma Inc. Ornithine derivative
EP2014657A1 (de) * 2007-06-21 2009-01-14 Bayer Schering Pharma Aktiengesellschaft Diaminopyrimidine als Modulatoren des EP2-Rezeptors
WO2009005076A1 (ja) 2007-07-03 2009-01-08 Astellas Pharma Inc. アミド化合物
BRPI0912778B1 (pt) 2008-05-14 2019-04-30 Astellas Pharma Inc. Composto de amida, composição farmacêutica compreendedo dito composto e uso do mesmo para o tratamento de insuficiência renal crônica ou nefropatia diabética
CA2733247C (en) 2008-08-14 2018-04-03 Beta Pharma Canada Inc. Heterocyclic amide derivatives as ep4 receptor antagonists
WO2010032123A1 (en) 2008-09-19 2010-03-25 Biotechnology Research Corporation Limited Triterpenoid compounds and methods of use thereof
US8685999B2 (en) 2008-09-25 2014-04-01 Merck Sharp & Dohme Corp. Beta carboline sulphonylurea derivatives as EP4 receptor antagonists
EP2571867B1 (en) 2010-05-21 2015-11-04 Noviga Research AB Novel pyrimidine derivatives
PT2619182T (pt) 2010-09-21 2017-01-17 Eisai R&D Man Co Ltd Composição farmacêutica
US9175080B2 (en) 2010-09-29 2015-11-03 Nb Health Laboratory Co., Ltd. Antibody against human prostaglandin E2 receptor EP4
ES2545110T3 (es) 2010-12-10 2015-09-08 Rottapharm Biotech S.R.L. Derivados de piridinamida como antagonistas del receptor EP4
WO2012103071A2 (en) 2011-01-25 2012-08-02 Eisai R&D Management Co., Ltd. Compounds and compositions
AU2012230229A1 (en) 2011-03-24 2013-10-10 Noviga Research Ab Novel pyrimidine derivatives
AU2011372747B2 (en) 2011-07-04 2016-12-22 Rottapharm Biotech S.R.L. Cyclic amine derivatives as EP4 receptor antagonists
EP2554662A1 (en) 2011-08-05 2013-02-06 M Maria Pia Cosma Methods of treatment of retinal degeneration diseases
US20150004175A1 (en) 2011-12-13 2015-01-01 Yale University Compositions and Methods for Reducing CTL Exhaustion
SI3459942T1 (sl) 2012-04-24 2021-05-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
AR091429A1 (es) 2012-06-29 2015-02-04 Lilly Co Eli Compuestos de fenoxietil piperidina
TWI572597B (zh) 2012-06-29 2017-03-01 美國禮來大藥廠 二甲基-苯甲酸化合物
UA115576C2 (uk) 2012-12-06 2017-11-27 Байєр Фарма Акцієнгезелльшафт Похідні бензимідазолу як антагоністи ер4
EP2765128A1 (en) 2013-02-07 2014-08-13 Almirall, S.A. Substituted benzamides with activity towards EP4 receptors
TW201443004A (zh) 2013-02-15 2014-11-16 Lilly Co Eli 苯氧基乙氧基化合物
TWI636046B (zh) 2013-05-17 2018-09-21 美國禮來大藥廠 苯氧基乙基二氫-1h-異喹啉化合物
KR102212981B1 (ko) 2013-06-12 2021-02-04 가껭세이야꾸가부시기가이샤 4-알키닐이미다졸 유도체 및 그것을 유효 성분으로서 함유하는 의약
MX2016002544A (es) 2013-09-04 2016-06-17 Squibb Bristol Myers Co Compuestos utiles como inmunomoduladores.
ES2675027T3 (es) 2013-09-06 2018-07-05 Aurigene Discovery Technologies Limited Derivados de 1,2,4-oxadiazol como inmunomoduladores
WO2015044900A1 (en) 2013-09-27 2015-04-02 Aurigene Discovery Technologies Limited Therapeutic immunomodulating compounds
HRP20180804T1 (hr) 2013-10-17 2018-08-10 Vertex Pharmaceuticals Incorporated Inhibitori dnk-pk
KR101807981B1 (ko) 2013-12-17 2017-12-11 일라이 릴리 앤드 캄파니 페녹시에틸 시클릭 아민 유도체 및 ep4 수용체 조절제로서의 그의 활성
TR201904327T4 (tr) 2013-12-17 2019-04-22 Lilly Co Eli Dimetilbenzoik asit bileşikleri.
TW201607943A (zh) 2013-12-19 2016-03-01 拜耳製藥公司 作為ep4配體之新穎苯并咪唑衍生物
TW201623277A (zh) 2014-03-26 2016-07-01 安斯泰來製藥股份有限公司 醯胺化合物
CN106572993B (zh) 2014-05-23 2019-07-16 卫材R&D管理有限公司 Ep4拮抗剂在制备治疗癌症的药物中的应用
WO2016021742A1 (en) 2014-08-07 2016-02-11 Takeda Pharmaceutical Company Limited Heterocyclic compounds as ep4 receptor antagonists
WO2016054807A1 (en) * 2014-10-10 2016-04-14 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
HUE052969T2 (hu) 2015-01-09 2021-05-28 Ono Pharmaceutical Co Triciklusos spiro vegyület
DK3325490T3 (da) 2015-07-23 2020-02-03 Takeda Pharmaceuticals Co 1-substituerede 1,2,3,4-tetrahydro-1,7-naphthyridin-8-aminderivater og deres anvendelse som ep4-receptorantagonister
EP3362454B1 (en) 2015-10-16 2021-12-08 Eisai R&D Management Co., Ltd. Ep4 antagonists

Also Published As

Publication number Publication date
US20230165859A1 (en) 2023-06-01
JP7065117B2 (ja) 2022-05-11
PH12019502562A1 (en) 2020-07-20
CL2019003257A1 (es) 2020-03-27
PT3625224T (pt) 2021-10-06
CR20190567A (es) 2020-02-10
ES2894124T3 (es) 2022-02-11
RS62441B1 (sr) 2021-11-30
HUE056406T2 (hu) 2022-02-28
PH12019502562B1 (en) 2024-06-14
AU2018269667B2 (en) 2022-02-03
DK3625224T3 (da) 2021-11-08
CA3063637A1 (en) 2018-11-22
JP2020520359A (ja) 2020-07-09
SG11201908660RA (en) 2019-10-30
CY1124528T1 (el) 2022-07-22
PL3625224T3 (pl) 2022-01-10
US20200069686A1 (en) 2020-03-05
CO2019010804A2 (es) 2019-10-09
IL270616B (en) 2022-01-01
MA49127B1 (fr) 2022-05-31
KR20200006589A (ko) 2020-01-20
CN110621666A (zh) 2019-12-27
UA124748C2 (uk) 2021-11-10
TW201900637A (zh) 2019-01-01
SI3625224T1 (sl) 2021-11-30
WO2018210995A1 (en) 2018-11-22
EP3625224A1 (en) 2020-03-25
AR111806A1 (es) 2019-08-21
AU2018269667A1 (en) 2019-10-24
MX2019013639A (es) 2020-01-21
BR112019024114A2 (pt) 2020-06-02
MX394108B (es) 2025-03-21
TWI768043B (zh) 2022-06-21
EA039630B1 (ru) 2022-02-18
MA49127A (fr) 2021-05-26
EA201992679A1 (ru) 2020-05-06
LT3625224T (lt) 2021-10-25
HRP20211532T1 (hr) 2022-01-07
EP3625224B1 (en) 2021-08-04
KR102650756B1 (ko) 2024-03-22

Similar Documents

Publication Publication Date Title
PE20191787A1 (es) Derivados de indol n-sustituidos
CY1124913T1 (el) Ν-υποκατεστημενα παραγωγα ινδολης ως διαμορφωτες υποδοχεα pge2
PE20221336A1 (es) Compuestos triciclicos sustituidos
AR079205A1 (es) Morfolinotiazoles como moduladores alostericos positivos alfa 7
EA200901379A1 (ru) Производные никотиновой кислоты как модуляторы метаботропных глутаматных рецепторов 5 подтипа
AR093818A1 (es) Compuesto de 1-(bencil sustituido)piperazina sustituida
CO6280476A2 (es) Derivados de alcanos azabiciclicos sustituidos con biarilo como moduladores de la actividad de los receptores nicotinicos de acetilcolina
PE20142019A1 (es) Nuevos derivados de acidos indaniloxidihidrobenzofuranilaceticos y sus usos como agonistas del receptor gpr40
CY1124608T1 (el) Παραγωγα φαινυλιου ως ρυθμιστες υποδοχεα pge2
EA201390969A1 (ru) Модуляторы глюкагонового рецептора
AR090488A1 (es) Derivados de n-ciclobutilbenzamida, un proceso para su obtencion, intermediarios para su sintesis, composiciones pesticidas y farmaceuticas que los comprenden y metodos para controlar daños debidos a una plaga y/u hongos
EA202091262A1 (ru) Пиперидиновые модуляторы рецепторов cxcr7
AR080056A1 (es) Derivados de ciclohexil-amida como antagonistas de los receptores de crf
PE20171057A1 (es) Derivados espirodiamina como inhibidores de la aldosterona sintasa
AR069480A1 (es) Derivados de 2-amino-pirimidina
AR078756A1 (es) Moduladores alostericos positivos (map)
CL2016001023A1 (es) Compuesto n-(1-(4-(2-(4-cloro-2,6-dimetilpirimidin-5-il)etil)piperidin-1-il)-1-oxopropan-2-il)ciclopropanocarboxamida, estereoisomero, inhibidores de grelina o-aciltransferasa (goat); composición farmaceutica; y uso para reducir la ganancia de peso y para tratar la diabetes tipo 2.
PE20170684A1 (es) Derivados de heterociclilo opcionalmente condensados de pirimidina utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias
AR093937A1 (es) Compuestos quimicos
AR068115A1 (es) Derivado del acido pirazolcarboxilico metodo de produccion del mismo y fungicida
AR103412A1 (es) Derivados de indol mono o disustituido como inhibidores de la replicación del virus del dengue
EP3952865A4 (en) HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS FOR THERAPEUTIC USES
MY161403A (en) 5- (phenyl/pyridinyl-ethinyl) -2-pyridine/ 2-pyrimidine-carborxamides as mglur5 modulators
CL2020002588A1 (es) Compuestos derivados de indol, composiciones que los contienen, útiles en el tratamiento de infestación por helmintos, preferentemente trematodos, en mamíferos. (divisional de solicitud n° 03258-2016)
PE20181274A1 (es) Compuestos utiles para inhibir ror-gamma-t