EA201691002A1 - Бициклические гетероарильные аналоги индола, подходящие в качестве модуляторов ror гамма - Google Patents

Бициклические гетероарильные аналоги индола, подходящие в качестве модуляторов ror гамма

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Publication number
EA201691002A1
EA201691002A1 EA201691002A EA201691002A EA201691002A1 EA 201691002 A1 EA201691002 A1 EA 201691002A1 EA 201691002 A EA201691002 A EA 201691002A EA 201691002 A EA201691002 A EA 201691002A EA 201691002 A1 EA201691002 A1 EA 201691002A1
Authority
EA
Eurasian Patent Office
Prior art keywords
indoal
heteroarrynal
bicyclic
rorγt
ror gamma
Prior art date
Application number
EA201691002A
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English (en)
Other versions
EA029489B1 (ru
Inventor
Санджиб Дас
Чаудхари Сачин Сундарлал
Абрахам Томас
Шайлеш Рамеш Пардеши
Вишал Говиндрао Дешмух
Прашант Дилип Вадекар
Неелима Каираткар-Джоши
Дайси Маниш Шах
Малини Бажпай
Original Assignee
Гленмарк Фармасьютикалс С.А.
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 Гленмарк Фармасьютикалс С.А. filed Critical Гленмарк Фармасьютикалс С.А.
Publication of EA201691002A1 publication Critical patent/EA201691002A1/ru
Publication of EA029489B1 publication Critical patent/EA029489B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)

Abstract

Изобретение относится к соединениям формулы (I) и его фармацевтически приемлемым солям, где X, X, М, R, R, R, R, m, n, и р определены в настоящем документе, которые являются активными в качестве модуляторов ретиноид-родственного сиротского рецептора гамма t (RORγt). Данные соединения предотвращают, ингибируют или подавляют действие RORγt, и таким образом подходят для лечения заболеваний, расстройств, синдромов или состояний, опосредованных RORγt, таких как, например, боль, воспаление, ХОБЛ, астма, ревматоидный артрит, колит, множественный склероз, нейродегенеративные заболевания и рак.
EA201691002A 2013-12-10 2014-12-09 Бициклические гетероарильные аналоги индола, подходящие в качестве модуляторов ror гамма EA029489B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN3853MU2013 2013-12-10
IN527MU2014 2014-02-14
IN2172MU2014 2014-07-04
PCT/IB2014/066720 WO2015087234A1 (en) 2013-12-10 2014-12-09 Bicyclic heteroaryl indole analogues useful as ror gamma modulators

Publications (2)

Publication Number Publication Date
EA201691002A1 true EA201691002A1 (ru) 2016-12-30
EA029489B1 EA029489B1 (ru) 2018-04-30

Family

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Family Applications (1)

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EA201691002A EA029489B1 (ru) 2013-12-10 2014-12-09 Бициклические гетероарильные аналоги индола, подходящие в качестве модуляторов ror гамма

Country Status (18)

Country Link
US (1) US9682977B2 (ru)
EP (1) EP3080090B1 (ru)
JP (1) JP2016539989A (ru)
CN (1) CN105980364A (ru)
AP (1) AP2016009281A0 (ru)
AU (1) AU2014363035A1 (ru)
BR (1) BR112016013425A2 (ru)
CA (1) CA2933003A1 (ru)
CL (1) CL2016001441A1 (ru)
EA (1) EA029489B1 (ru)
IL (1) IL246123A0 (ru)
MX (1) MX2016007604A (ru)
PE (1) PE20160687A1 (ru)
PH (1) PH12016501105A1 (ru)
SG (1) SG11201604714SA (ru)
TW (1) TW201605797A (ru)
WO (1) WO2015087234A1 (ru)
ZA (1) ZA201604454B (ru)

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GB201419015D0 (en) 2014-10-24 2014-12-10 Orca Pharmaceuticals Ltd Compounds
EP3256450B1 (en) 2015-02-11 2020-12-02 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as ror-gamma-t inhibitors and uses thereof
WO2017051319A1 (en) * 2015-09-21 2017-03-30 Glenmark Pharmaceuticals S.A. Aryl and heteroaryl ether compounds as ror gamma modulators
EP3368516B1 (en) * 2015-10-27 2020-07-15 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
US10584121B2 (en) 2015-10-27 2020-03-10 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as RORgammaT inhibitors and uses thereof
KR20180070697A (ko) 2015-10-27 2018-06-26 머크 샤프 앤드 돔 코포레이션 Ror감마t 저해제로서의 치환된 인다졸 화합물 및 이의 용도
WO2017197055A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
AR110481A1 (es) 2016-12-05 2019-04-03 Lead Pharma Holding Bv MODULADORES DE ROR g (RORg)
TW201906816A (zh) * 2017-07-06 2019-02-16 大陸商江蘇恆瑞醫藥股份有限公司 吲哚甲醯胺類衍生物、其製備方法及其在醫藥上的應用
EP3663299B1 (en) * 2017-08-01 2023-03-08 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Bicyclic compound acting as ror gamma inhibitor
WO2019100106A1 (en) * 2017-11-24 2019-05-31 The University Of Sydney Antibacterial compounds and methods of use thereof

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TW200621237A (en) 2004-11-01 2006-07-01 Wyeth Corp [(1-h-indazol-3-yl)methyl]phenols and (hydroxyphenyl)(1h-indazol-3-yl)methanones
WO2006075638A1 (ja) * 2005-01-14 2006-07-20 Dainippon Sumitomo Pharma Co., Ltd. 新規ヘテロアリール誘導体
CN103201262B (zh) * 2010-08-20 2016-06-01 艾米拉医药股份有限公司 自分泌运动因子抑制剂及其用途
WO2012027965A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
WO2012028100A1 (en) 2010-09-01 2012-03-08 Glaxo Group Limited Novel compounds
US9512111B2 (en) * 2010-11-08 2016-12-06 Lycera Corporation N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease
WO2012100734A1 (en) 2011-01-24 2012-08-02 Glaxo Group Limited Compounds useful as retinoid-related orphan receptor gamma modulators
WO2012100732A1 (en) 2011-01-24 2012-08-02 Glaxo Group Limited Retinoid-related orphan receptor gamma modulators, composition containing them and uses thereof
EP2487159A1 (en) * 2011-02-11 2012-08-15 MSD Oss B.V. RorgammaT inhibitors
EP2511263A1 (en) 2011-04-14 2012-10-17 Phenex Pharmaceuticals AG Pyrrolo sulfonamide compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (RORgamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases
WO2013171729A2 (en) 2013-01-08 2013-11-21 Glenmark Pharmaceuticals S.A. Aryl and heteroaryl amide compounds as rorgamat modulator

Also Published As

Publication number Publication date
PH12016501105A1 (en) 2016-07-11
US20160326163A1 (en) 2016-11-10
CA2933003A1 (en) 2015-06-18
BR112016013425A2 (pt) 2017-08-08
EP3080090B1 (en) 2018-01-31
IL246123A0 (en) 2016-08-02
WO2015087234A1 (en) 2015-06-18
ZA201604454B (en) 2017-11-29
AP2016009281A0 (en) 2016-06-30
EA029489B1 (ru) 2018-04-30
US9682977B2 (en) 2017-06-20
JP2016539989A (ja) 2016-12-22
AU2014363035A1 (en) 2016-06-30
SG11201604714SA (en) 2016-07-28
MX2016007604A (es) 2017-02-28
EP3080090A1 (en) 2016-10-19
CL2016001441A1 (es) 2017-03-03
TW201605797A (zh) 2016-02-16
CN105980364A (zh) 2016-09-28
PE20160687A1 (es) 2016-08-11

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