KR102000319B1 - Trpm8 길항제 - Google Patents

Trpm8 길항제 Download PDF

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KR102000319B1
KR102000319B1 KR1020147019697A KR20147019697A KR102000319B1 KR 102000319 B1 KR102000319 B1 KR 102000319B1 KR 1020147019697 A KR1020147019697 A KR 1020147019697A KR 20147019697 A KR20147019697 A KR 20147019697A KR 102000319 B1 KR102000319 B1 KR 102000319B1
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thiazole
carboxylate
ethyl
oxy
fluorophenyl
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KR20150000870A (ko
Inventor
알레시오 모리코니
지안루카 비안키니
산드로 콜라지오이아
라우라 브란돌리니
안드레아 아라미니
키아라 리베라티
실비아 보볼렌타
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돔페 파르마써티씨 에스.피.에이.
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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
    • C07D417/12—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 chain containing hetero atoms as chain links
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    • 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
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/4245—Oxadiazoles
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    • 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
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A—HUMAN NECESSITIES
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
    • C07D263/36—One oxygen atom
    • C07D263/40—One oxygen atom attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
    • C07D263/36—One oxygen atom
    • C07D263/42—One oxygen atom attached in position 5
    • 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
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D417/10—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 aromatic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1020147019697A 2011-12-19 2012-12-19 Trpm8 길항제 Active KR102000319B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP11194365.0 2011-12-19
EP11194365.0A EP2606888A1 (en) 2011-12-19 2011-12-19 Trpm8 antagonists
EP12178327 2012-07-27
EP12178327.8 2012-07-27
PCT/EP2012/076147 WO2013092711A1 (en) 2011-12-19 2012-12-19 Trpm8 antagonists

Publications (2)

Publication Number Publication Date
KR20150000870A KR20150000870A (ko) 2015-01-05
KR102000319B1 true KR102000319B1 (ko) 2019-09-27

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Application Number Title Priority Date Filing Date
KR1020147019697A Active KR102000319B1 (ko) 2011-12-19 2012-12-19 Trpm8 길항제

Country Status (22)

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US (2) US9585875B2 (OSRAM)
EP (1) EP2793883B1 (OSRAM)
JP (2) JP6238906B2 (OSRAM)
KR (1) KR102000319B1 (OSRAM)
CN (1) CN104220069B (OSRAM)
AU (1) AU2012357747B2 (OSRAM)
CY (1) CY1120403T1 (OSRAM)
DK (1) DK2793883T3 (OSRAM)
EA (1) EA025356B1 (OSRAM)
ES (1) ES2676884T3 (OSRAM)
HR (1) HRP20181086T1 (OSRAM)
HU (1) HUE038407T2 (OSRAM)
LT (1) LT2793883T (OSRAM)
ME (1) ME03038B (OSRAM)
PL (1) PL2793883T3 (OSRAM)
PT (1) PT2793883T (OSRAM)
RS (1) RS57389B1 (OSRAM)
SI (1) SI2793883T1 (OSRAM)
SM (1) SMT201800351T1 (OSRAM)
TR (1) TR201808861T4 (OSRAM)
WO (1) WO2013092711A1 (OSRAM)
ZA (1) ZA201404499B (OSRAM)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2481727A1 (en) * 2011-01-28 2012-08-01 Dompe S.p.A. TRPM8 receptor antagonists
DK2793883T3 (en) 2011-12-19 2018-07-30 Dompe Farm Spa TRPM8 antagonists
TR201906539T4 (tr) * 2013-05-24 2019-05-21 Nestec Sa Mentol, Linalool ve/veya Icilin Kullanarak Beyin Travması ve İnmelerden Kaynaklanan Non-İnflamatuar Nöron Hasarının Tedavisi veya Önlenmesi.
CN106715424B (zh) 2014-06-05 2020-07-14 拜耳作物科学股份公司 作为农药的双环化合物
LT3157918T (lt) * 2014-06-23 2019-05-27 Dompé Farmaceutici S.P.A. 2-aril-4-hidroksi-1,3-tiazolo dariniai, tinkami naudoti kaip trpm8-inhibitoriai neuralgijos, skausmo, lėtinės obstrukcinės plaučių ligos (lopl) ar astmos gydymui
BR112018006471B1 (pt) 2015-10-01 2024-02-27 Senomyx, Inc Composto, composição, método de modular o membro de melastina do canal potencial do receptor transitório 8 (trpm8), método de modular a sensação de resfrescância de uma composição e método de induzir uma sensação de refrescância em um ser humano ou animal
EP3184524A1 (en) 2015-12-21 2017-06-28 Dompé farmaceutici S.p.A. 4-hydroxy-2-phenyl-1,3-thiazol-5-yl methanone derivatives as trpm8 antagonists
CN113384577A (zh) 2016-06-13 2021-09-14 田边三菱制药株式会社 用于治疗或预防血管舒缩症状的组合物
WO2018117166A1 (ja) * 2016-12-21 2018-06-28 キッセイ薬品工業株式会社 チアゾール誘導体、またはその薬理学的に許容される塩

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AU2012357747A2 (en) 2014-08-21
ES2676884T3 (es) 2018-07-25
EP2793883A1 (en) 2014-10-29
CN104220069B (zh) 2018-10-02
JP2015504874A (ja) 2015-02-16
HUE038407T2 (hu) 2018-10-29
CY1120403T1 (el) 2019-07-10
RS57389B1 (sr) 2018-09-28
EA025356B1 (ru) 2016-12-30
HRP20181086T1 (hr) 2018-09-07
PT2793883T (pt) 2018-07-18
JP2017197564A (ja) 2017-11-02
US20170129881A1 (en) 2017-05-11
EP2793883B1 (en) 2018-04-18
CN104220069A (zh) 2014-12-17
EA201491213A1 (ru) 2014-11-28
US9585875B2 (en) 2017-03-07
KR20150000870A (ko) 2015-01-05
US20140371276A1 (en) 2014-12-18
PL2793883T3 (pl) 2018-09-28
LT2793883T (lt) 2018-08-10
SMT201800351T1 (it) 2018-09-13
US9856246B2 (en) 2018-01-02
AU2012357747B2 (en) 2017-09-07
AU2012357747A1 (en) 2014-07-10
DK2793883T3 (en) 2018-07-30
SI2793883T1 (en) 2018-08-31
HK1203810A1 (en) 2015-11-06
AU2012357747A8 (en) 2014-07-24
ME03038B (me) 2018-10-20
JP6238906B2 (ja) 2017-11-29
TR201808861T4 (tr) 2018-07-23
WO2013092711A1 (en) 2013-06-27

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