EA201891503A1 - Производные 4-гидрокси-2-фенил-1,3-тиазол-5-ил метанона как антагонисты trpm8 - Google Patents

Производные 4-гидрокси-2-фенил-1,3-тиазол-5-ил метанона как антагонисты trpm8

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Publication number
EA201891503A1
EA201891503A1 EA201891503A EA201891503A EA201891503A1 EA 201891503 A1 EA201891503 A1 EA 201891503A1 EA 201891503 A EA201891503 A EA 201891503A EA 201891503 A EA201891503 A EA 201891503A EA 201891503 A1 EA201891503 A1 EA 201891503A1
Authority
EA
Eurasian Patent Office
Prior art keywords
disorders
trpm8
antagonists
tiazol
methanon
Prior art date
Application number
EA201891503A
Other languages
English (en)
Other versions
EA037845B1 (ru
Inventor
Андреа Арамини
Жанлука Бианчини
Самюэль Лиллини
Original Assignee
Домпе Фармачеутичи С.П.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 Домпе Фармачеутичи С.П.А. filed Critical Домпе Фармачеутичи С.П.А.
Publication of EA201891503A1 publication Critical patent/EA201891503A1/ru
Publication of EA037845B1 publication Critical patent/EA037845B1/ru

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    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Заявленное изобретение относится к соединениям, действующим в качестве антагонистов 8 члена подсемейства M катионного канала транзиторного рецепторного потенциала (TRPM8) и имеющим формулуУпомянутые соединения применяют в лечении болезней, связанных с активностью TRPM8, таких как боль, ишемия, нейродегенерация, инсульт, психические расстройства, зуд, заболевания раздраженной толстой кишки, вызванные простудой и/или обострившиеся респираторные нарушения и урологические расстройства, корнеальные расстройства, связанные с нарушением слезоотделения и/или моргания, как, например, эпифора и синдром сухих глаз.
EA201891503A 2015-12-21 2016-12-16 Производные 4-гидрокси-2-фенил-1,3-тиазол-5-ил метанона как антагонисты trpm8 EA037845B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP15201788.5A EP3184524A1 (en) 2015-12-21 2015-12-21 4-hydroxy-2-phenyl-1,3-thiazol-5-yl methanone derivatives as trpm8 antagonists
PCT/EP2016/081567 WO2017108632A1 (en) 2015-12-21 2016-12-16 4-hydroxy-2-phenyl-1,3-thiazol-5-yl methanone derivatives as trpm8 antagonists

Publications (2)

Publication Number Publication Date
EA201891503A1 true EA201891503A1 (ru) 2019-01-31
EA037845B1 EA037845B1 (ru) 2021-05-27

Family

ID=54883947

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201891503A EA037845B1 (ru) 2015-12-21 2016-12-16 Производные 4-гидрокси-2-фенил-1,3-тиазол-5-ил метанона как антагонисты trpm8

Country Status (19)

Country Link
US (1) US10246448B2 (ru)
EP (2) EP3184524A1 (ru)
JP (1) JP6908610B2 (ru)
KR (1) KR20180095818A (ru)
CN (1) CN108699053B (ru)
AU (1) AU2016378108B9 (ru)
CY (1) CY1122312T1 (ru)
DK (1) DK3394053T3 (ru)
EA (1) EA037845B1 (ru)
ES (1) ES2757324T3 (ru)
HK (1) HK1257896B (ru)
HR (1) HRP20192008T1 (ru)
HU (1) HUE046284T2 (ru)
LT (1) LT3394053T (ru)
PT (1) PT3394053T (ru)
RS (1) RS59475B1 (ru)
SI (1) SI3394053T1 (ru)
WO (1) WO2017108632A1 (ru)
ZA (1) ZA201803300B (ru)

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2015531A (en) 1932-07-25 1935-09-24 Champion Paper & Fibre Co Roll coating machine
WO2006040136A1 (en) 2004-10-13 2006-04-20 Bayer Healthcare Ag Substituted 4-benzyloxy-phenylmethylamide derivatives as cold menthol receptor-1 (cmr-1) antagonists for the treatment of urological disorder
WO2007017094A1 (en) 2005-08-04 2007-02-15 Bayer Healthcare Ag Substituted benzyloxy-phenylmethylcarbamate derivatives
WO2007017092A1 (en) 2005-08-04 2007-02-15 Bayer Healthcare Ag Substituted 4-benzyloxy-benzoic acid amide derivatives
WO2007017093A1 (en) 2005-08-04 2007-02-15 Bayer Healthcare Ag Substituted 2-benzyloxy-benzoic acid amide derivatives
WO2007080109A1 (en) 2006-01-16 2007-07-19 Bayer Healthcare Ag Substituded benzyloxy-phenylmethylurea derivatives
EP2029614B1 (en) 2006-05-10 2013-01-23 Janssen Pharmaceutica, N.V. Cold menthol receptor-1 antagonists
WO2009012430A1 (en) * 2007-07-18 2009-01-22 Janssen Pharmaceutica N.V. Sulfonamides as trpm8 modulators
WO2010103381A1 (en) 2009-03-13 2010-09-16 Glenmark Pharmaceuticals S.A. Spirocyclic piperidine derivatives as trpm 8 modulators
KR20140071518A (ko) 2009-05-01 2014-06-12 라퀄리아 파마 인코포레이티드 Ｔｒｐｍ8 길항제로서의 설파모일 벤조산 유도체
US20130079348A1 (en) * 2010-03-03 2013-03-28 Calcimedica, Inc. Compounds that modulate intracellular calcium
ES2377785B2 (es) 2010-09-08 2012-09-26 Universidad Miguel Hernández De Elche Composición farmacéutica para el tratamiento del ojo seco.
EP2481727A1 (en) * 2011-01-28 2012-08-01 Dompe S.p.A. TRPM8 receptor antagonists
LT2793883T (lt) * 2011-12-19 2018-08-10 DompƩ farmaceutici s.p.a. Trpm8 antagonistai
US9458092B2 (en) * 2013-05-08 2016-10-04 Kissei Pharmaceutical Co., Ltd. α-Substituted glycinamide derivative
SI3157918T1 (sl) * 2014-06-23 2019-05-31 Dompe Farmaceutici S.P.A. 2-aril-4-hidroksi-1,3-tiazolni derivati, uporabni kot inhibitorji TRPM8 pri zdravljenju nevralgije, bolečine, KOPB in astme

Also Published As

Publication number Publication date
SI3394053T1 (sl) 2019-12-31
WO2017108632A1 (en) 2017-06-29
HK1257896B (zh) 2020-06-19
US10246448B2 (en) 2019-04-02
US20180319785A1 (en) 2018-11-08
HRP20192008T1 (hr) 2020-02-07
ES2757324T3 (es) 2020-04-28
AU2016378108B9 (en) 2021-01-28
AU2016378108A1 (en) 2018-06-21
JP6908610B2 (ja) 2021-07-28
JP2018538334A (ja) 2018-12-27
HUE046284T2 (hu) 2020-02-28
EP3394053A1 (en) 2018-10-31
LT3394053T (lt) 2019-12-10
RS59475B1 (sr) 2019-12-31
ZA201803300B (en) 2019-07-31
AU2016378108B2 (en) 2020-12-17
CN108699053B (zh) 2022-01-14
EP3184524A1 (en) 2017-06-28
DK3394053T3 (da) 2019-11-18
PT3394053T (pt) 2019-10-31
EA037845B1 (ru) 2021-05-27
CN108699053A (zh) 2018-10-23
EP3394053B1 (en) 2019-08-21
KR20180095818A (ko) 2018-08-28
CY1122312T1 (el) 2021-01-27

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