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EA201290840A1 - Антагонисты ванилоидного рецептора trpv1 с бициклической частью - Google Patents

Антагонисты ванилоидного рецептора trpv1 с бициклической частью

Info

Publication number
EA201290840A1
EA201290840A1 EA201290840A EA201290840A EA201290840A1 EA 201290840 A1 EA201290840 A1 EA 201290840A1 EA 201290840 A EA201290840 A EA 201290840A EA 201290840 A EA201290840 A EA 201290840A EA 201290840 A1 EA201290840 A1 EA 201290840A1
Authority
EA
Eurasian Patent Office
Prior art keywords
antagonists
trpv1
receptor trpv1
bicyclic part
vaniloid receptor
Prior art date
Application number
EA201290840A
Other languages
English (en)
Inventor
Мауро Наполетано
Марчелло Тревизани
Мария Джованна Павани
Франческа Фруттароло
Original Assignee
Фарместе С.Р.Л.
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 Фарместе С.Р.Л. filed Critical Фарместе С.Р.Л.
Publication of EA201290840A1 publication Critical patent/EA201290840A1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/26Oxygen atoms
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32Oxygen atoms
    • C07D209/34Oxygen atoms in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; Hydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/341,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/361,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

В изобретении раскрыты соединения формулы (I)где Y представляет группу формул А, В, С, D или Еи W, Q, n, R, R, R, U-U, J и K имеют значения, данные в описании. Соединения формулы (I) являются антагонистами TRPV1 и полезны в качестве активных ингредиентов фармацевтических композиций при лечении боли и других состояний, улучшаемых при ингибировании ванилоидного рецептора TRPV1.
EA201290840A 2010-03-30 2010-12-22 Антагонисты ванилоидного рецептора trpv1 с бициклической частью EA201290840A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10158292A EP2377850A1 (en) 2010-03-30 2010-03-30 TRPV1 vanilloid receptor antagonists with a bicyclic portion
PCT/EP2010/070538 WO2011120604A1 (en) 2010-03-30 2010-12-22 "trpv1 vanilloid receptor antagonists with a bicyclic portion"

Publications (1)

Publication Number Publication Date
EA201290840A1 true EA201290840A1 (ru) 2013-04-30

Family

ID=42320777

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201290840A EA201290840A1 (ru) 2010-03-30 2010-12-22 Антагонисты ванилоидного рецептора trpv1 с бициклической частью

Country Status (11)

Country Link
US (3) US9216975B2 (ru)
EP (2) EP2377850A1 (ru)
JP (1) JP5927174B2 (ru)
KR (1) KR20130065634A (ru)
CN (1) CN102858742B (ru)
BR (1) BR112012024712A2 (ru)
CA (1) CA2794773A1 (ru)
EA (1) EA201290840A1 (ru)
IL (1) IL222153A0 (ru)
MX (1) MX2012011244A (ru)
WO (1) WO2011120604A1 (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2641648C1 (ru) 2009-12-04 2018-01-19 Суновион Фармасьютикалз, Инк. Полициклические соединения и способы их применения
AU2013355220B2 (en) * 2012-12-06 2018-08-02 Baruch S. Blumberg Institute Functionalized benzamide derivatives as antiviral agents against HBV infection
CN107108593B (zh) * 2014-11-24 2020-03-24 美迪福伦Dbt有限公司 作为类香草素受体配体ii的基于取代的恶唑和噻唑的羧酰胺和脲衍生物
MA45857A (fr) 2016-07-29 2021-05-19 Sunovion Pharmaceuticals Inc Composés et compositions, et utilisations associées
AU2017301767A1 (en) 2016-07-29 2019-02-14 Pgi Drug Discovery Llc Compounds and compositions and uses thereof
JP7146782B2 (ja) 2017-02-16 2022-10-04 サノビオン ファーマシューティカルズ インク 統合失調症を処置する方法
AU2018312559B2 (en) 2017-08-02 2022-06-02 Pgi Drug Discovery Llc Isochroman compounds and uses thereof
EA202091945A1 (ru) 2018-02-16 2021-01-18 Суновион Фармасьютикалз Инк. Соли, кристаллические формы и способы их получения
JP6994061B2 (ja) 2019-02-15 2022-01-14 ノバルティス アーゲー 4-(7-ヒドロキシ-2-イソプロピル-4-オキソ-4h-キナゾリン-3-イル)-ベンゾニトリルの製剤
MX2021009702A (es) 2019-02-15 2021-09-14 Novartis Ag Metodos para tratar el dolor de la superficie ocular.
US11136304B2 (en) 2019-03-14 2021-10-05 Sunovion Pharmaceuticals Inc. Salts of a heterocyclic compound and crystalline forms, processes for preparing, therapeutic uses, and pharmaceutical compositions thereof
CN114585357A (zh) * 2019-10-04 2022-06-03 千寿制药株式会社 含有杂环亚基乙酰胺衍生物的药物
CN111362878B (zh) * 2020-03-18 2023-09-19 湖南复瑞生物医药技术有限责任公司 一种4-氨基-1,3-二氢-苯并咪唑-2-酮的制备方法
JP2023523569A (ja) 2020-04-14 2023-06-06 サノビオン ファーマシューティカルズ インク 神経学的および精神障害の治療方法
KR102334947B1 (ko) 2020-04-22 2021-12-06 주식회사 제이맥켐 Trpv1 길항제로서 벤즈이미다졸론계 시남아마이드 유도체 및 이를 유효성분으로 함유하는 통증의 치료 또는 예방용 약학적 조성물

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3975531A (en) * 1973-10-02 1976-08-17 A. H. Robins Company, Incorporated 4-(5- And 7-)benzoylindolin-2-ones and pharmaceutical uses thereof
CH577461A5 (ru) * 1975-08-13 1976-07-15 Robins Co Inc A H
US4503073A (en) * 1981-01-07 1985-03-05 A. H. Robins Company, Incorporated 2-Amino-3-(alkylthiobenzoyl)-phenylacetic acids
US4582909A (en) * 1984-02-02 1986-04-15 Warner-Lambert Company Benzobicyclic lactam acids and derivatives as cognition activators
US4644005A (en) * 1984-10-31 1987-02-17 Pfizer Inc. Oxindole antiinflammatory agents
CO5190696A1 (es) * 1999-06-16 2002-08-29 Smithkline Beecham Corp Antagonistas de los receptores il-8
EP1294688A2 (en) * 2000-06-02 2003-03-26 Sugen, Inc. Indolinone derivatives as protein kinase/phosphatase inhibitors
DE60208630T2 (de) 2001-05-11 2006-08-17 Pfizer Products Inc., Groton Thiazolderivate und ihre Verwendung als cdk-Inhibitoren
JP2003192587A (ja) * 2001-12-26 2003-07-09 Bayer Ag 尿素誘導体
GB0206876D0 (en) * 2002-03-22 2002-05-01 Merck Sharp & Dohme Therapeutic agents
SE0302546D0 (sv) * 2003-09-24 2003-09-24 Astrazeneca Ab New compounds
US6933311B2 (en) * 2003-02-11 2005-08-23 Abbott Laboratories Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
EP1628661A2 (en) * 2003-06-05 2006-03-01 Vertex Pharmaceuticals Incorporated Modulators of vr1 receptor
KR20060027338A (ko) * 2003-06-12 2006-03-27 아스텔라스세이야쿠 가부시키가이샤 벤즈 아미드 유도체 또는 그 염
GB0322016D0 (en) * 2003-09-19 2003-10-22 Merck Sharp & Dohme New compounds
WO2005040100A1 (en) * 2003-10-15 2005-05-06 Bayer Healthcare Ag Tetrahydro-naphthalene and urea derivatives
US7683076B2 (en) * 2003-11-08 2010-03-23 Bayer Schering Pharma Aktiengesellschaft Tetrahydro-quinolinylurea derivatives
SE0303280D0 (sv) 2003-12-05 2003-12-05 Astrazeneca Ab Novel compounds
CA2563494A1 (en) * 2004-04-20 2005-11-03 Bayer Healthcare Ag Urea derivatives as antagonists of the vanilloid receptor (vr1)
CA2566332A1 (en) 2004-05-14 2005-11-24 Pfizer Products Inc. Pyrimidine derivatives for the treatment of abnormal cell growth
CA2583828A1 (en) 2004-10-12 2006-04-27 Decode Genetics, Inc. Carboxylic acid peri-substituted bicyclics for occlusive artery disease
US7423040B2 (en) 2005-02-18 2008-09-09 Irene Eijgendaal Stable crystalline form of bifeprunox mesylate, dosage forms thereof and methods for using same
CA2680173A1 (en) * 2007-03-07 2008-09-12 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors containing a heterocyclic moiety
CL2008001003A1 (es) * 2007-04-11 2008-10-17 Actelion Pharmaceuticals Ltd Compuestos derivados de oxazolidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para preparar un medicamento para tratar una infeccion bacteriana.
EP2181108A2 (en) * 2007-06-12 2010-05-05 Boehringer Ingelheim International GmbH 3-hetrocyclylidene-indolinone derivatives as inhibitors of specific cell cycle kinases
US8969342B2 (en) 2009-03-20 2015-03-03 Brandeis University Compounds and methods for treating mammalian gastrointestinal microbial infections

Also Published As

Publication number Publication date
MX2012011244A (es) 2013-02-07
CN102858742A (zh) 2013-01-02
CA2794773A1 (en) 2011-10-06
JP5927174B2 (ja) 2016-06-01
EP2552888B1 (en) 2018-09-26
EP2552888A1 (en) 2013-02-06
US9216975B2 (en) 2015-12-22
US20170152252A1 (en) 2017-06-01
KR20130065634A (ko) 2013-06-19
WO2011120604A1 (en) 2011-10-06
JP2013523663A (ja) 2013-06-17
US10233177B2 (en) 2019-03-19
US20130079339A1 (en) 2013-03-28
US20160289199A1 (en) 2016-10-06
IL222153A0 (en) 2012-12-02
CN102858742B (zh) 2015-05-27
EP2377850A1 (en) 2011-10-19
BR112012024712A2 (pt) 2016-06-07

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