CN103732583B - Trpv4拮抗剂 - Google Patents

Trpv4拮抗剂 Download PDF

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Publication number
CN103732583B
CN103732583B CN201280039690.0A CN201280039690A CN103732583B CN 103732583 B CN103732583 B CN 103732583B CN 201280039690 A CN201280039690 A CN 201280039690A CN 103732583 B CN103732583 B CN 103732583B
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methyl
oxo
oxa
azaspiro
carbonitrile
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CN103732583A (zh
Inventor
C.布鲁克斯
M.张
H.S.埃达姆
K.B.古德曼
M.哈蒙德
M.A.希尔菲克
T.H.霍安格
J.R.帕特森
P.斯托伊
G.叶
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GlaxoSmithKline LLC
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Ge Lan Element Smith's Gram Lay Intellecture Property (no 2) Co Ltd
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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
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    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • 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]
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D419/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Public Health (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Otolaryngology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201280039690.0A 2011-06-17 2012-06-15 Trpv4拮抗剂 Active CN103732583B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161498110P 2011-06-17 2011-06-17
US61/498,110 2011-06-17
PCT/US2012/042622 WO2013012500A1 (en) 2011-06-17 2012-06-15 Trpv4 antagonists

Publications (2)

Publication Number Publication Date
CN103732583A CN103732583A (zh) 2014-04-16
CN103732583B true CN103732583B (zh) 2015-12-23

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US (1) US9187464B2 (https=)
EP (2) EP3121177B1 (https=)
JP (1) JP5969017B2 (https=)
KR (1) KR101870003B1 (https=)
CN (1) CN103732583B (https=)
AR (1) AR086958A1 (https=)
AU (1) AU2012284540B2 (https=)
BR (1) BR112013032391B1 (https=)
CA (1) CA2839743C (https=)
CL (1) CL2013003602A1 (https=)
CO (1) CO6821953A2 (https=)
CR (1) CR20130671A (https=)
CY (1) CY1117792T1 (https=)
DK (1) DK2721016T3 (https=)
DO (1) DOP2013000307A (https=)
EA (1) EA023616B1 (https=)
ES (2) ES2688733T3 (https=)
HR (1) HRP20160539T1 (https=)
HU (1) HUE029594T2 (https=)
IL (1) IL229872A (https=)
JO (1) JO3154B1 (https=)
MA (1) MA35184B1 (https=)
ME (1) ME02416B (https=)
MX (1) MX337440B (https=)
MY (1) MY173521A (https=)
PE (1) PE20141943A1 (https=)
PH (1) PH12013502463A1 (https=)
PL (1) PL2721016T3 (https=)
PT (1) PT2721016E (https=)
RS (1) RS54858B1 (https=)
SG (1) SG195106A1 (https=)
SI (1) SI2721016T1 (https=)
SM (1) SMT201600150B (https=)
TW (1) TWI538912B (https=)
UA (1) UA113963C2 (https=)
UY (1) UY34138A (https=)
WO (1) WO2013012500A1 (https=)
ZA (1) ZA201308816B (https=)

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EP2720546B1 (en) 2011-06-17 2016-04-06 Glaxosmithkline Intellectual Property (No. 2) Limited Spiro-cyclic trpv4 antagonists
US8927585B2 (en) * 2011-06-17 2015-01-06 Glaxosmithkline Intellectual Property (No.2) Limited TRPV4 antagonists
WO2013146754A1 (ja) 2012-03-27 2013-10-03 塩野義製薬株式会社 Trpv4阻害活性を有する芳香族複素5員環誘導体
WO2015046193A1 (ja) 2013-09-25 2015-04-02 塩野義製薬株式会社 Trpv4阻害活性を有する芳香族複素環式アミン誘導体
CN109153672B (zh) * 2016-05-19 2021-12-07 葛兰素史密斯克莱知识产权(第2 号)有限公司 Trpv4拮抗剂
US10968209B2 (en) 2016-05-19 2021-04-06 Glaxosmithkline Intellectual Property (No.2) Limited TRPV4 antagonist
TN2019000087A1 (en) 2016-10-03 2020-07-15 Janssen Pharmaceutica Nv Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors
WO2018185701A1 (en) 2017-04-06 2018-10-11 Glaxosmithkline Intellectual Property (No.2) Limited Trpv4 antagonists as antitussive agents
CA3081424A1 (en) * 2017-11-01 2019-05-09 Bristol-Myers Squibb Company Spirocyclic compounds as farnesoid x receptor modulators
WO2021170811A1 (en) 2020-02-27 2021-09-02 Glaxosmithkline Intellectual Property (No.2) Limited Method of treating eye disease using trpv4 antagonists
JP7692219B2 (ja) 2020-04-30 2025-06-13 ラクオリア創薬株式会社 Trpv4拮抗薬としてのピリミジン-4(3h)-オン誘導体
CN111704613B (zh) * 2020-06-23 2021-07-06 中国人民解放军军事科学院军事医学研究院 咪唑类衍生物及其作为trpv4抑制剂的用途
JPWO2022014707A1 (https=) * 2020-07-16 2022-01-20
WO2024011214A1 (en) 2022-07-08 2024-01-11 Actio Biosciences, Inc. Therapeutic compounds and methods
CN120641413A (zh) * 2023-04-18 2025-09-12 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2024217446A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2024217452A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2024217439A1 (zh) * 2023-04-18 2024-10-24 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
CN120435476A (zh) * 2023-04-18 2025-08-05 河北乌图药业有限公司 化合物及其在慢性乙型肝炎、肝纤维化、肝癌的治疗中的应用
WO2025014818A1 (en) * 2023-07-07 2025-01-16 Actio Biosciences, Inc. Solid forms of gsk2798745, a trpv4 antagonist
CN117945917A (zh) * 2023-12-26 2024-04-30 衢州康鹏化学有限公司 一种3-氟-4-硝基苯甲酸的制备方法

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CN101384261A (zh) * 2005-12-22 2009-03-11 海德拉生物科学公司 治疗疼痛的方法和组合物
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JO3154B1 (ar) 2017-09-20
PE20141943A1 (es) 2014-12-28
ZA201308816B (en) 2015-02-25
EP3121177A1 (en) 2017-01-25
CR20130671A (es) 2014-02-04
EP3121177B1 (en) 2018-08-01
HUE029594T2 (en) 2017-03-28
CA2839743A1 (en) 2013-01-24
JP5969017B2 (ja) 2016-08-10
HK1195068A1 (zh) 2014-10-31
NZ618221A (en) 2015-02-27
PT2721016E (pt) 2016-06-06
EA023616B1 (ru) 2016-06-30
MY173521A (en) 2020-01-30
HRP20160539T1 (hr) 2016-06-17
EP2721016A1 (en) 2014-04-23
ES2688733T3 (es) 2018-11-06
JP2014518214A (ja) 2014-07-28
CY1117792T1 (el) 2017-05-17
CN103732583A (zh) 2014-04-16
AU2012284540A1 (en) 2013-04-04
SG195106A1 (en) 2013-12-30
MA35184B1 (fr) 2014-06-02
SI2721016T1 (sl) 2016-06-30
DOP2013000307A (es) 2014-06-01
CO6821953A2 (es) 2013-12-31
ES2569193T3 (es) 2016-05-09
UY34138A (es) 2013-01-03
MX337440B (es) 2016-03-03
IL229872A (en) 2017-03-30
AU2012284540B2 (en) 2014-08-28
BR112013032391A2 (pt) 2016-08-16
RS54858B1 (sr) 2016-10-31
DK2721016T3 (en) 2016-06-06
KR20140041733A (ko) 2014-04-04
CA2839743C (en) 2017-03-28
KR101870003B1 (ko) 2018-06-22
ME02416B (me) 2016-09-20
BR112013032391B1 (pt) 2020-11-24
EP2721016A4 (en) 2014-10-08
CL2013003602A1 (es) 2014-07-04
EP2721016B1 (en) 2016-04-06
PL2721016T3 (pl) 2017-01-31
SMT201600150B (it) 2016-07-01
TW201313705A (zh) 2013-04-01
MX2013014898A (es) 2014-03-21
US20140121206A1 (en) 2014-05-01
EA201490037A1 (ru) 2015-12-30
AR086958A1 (es) 2014-02-05
UA113963C2 (xx) 2017-04-10
TWI538912B (zh) 2016-06-21
WO2013012500A1 (en) 2013-01-24
PH12013502463A1 (en) 2014-01-20
US9187464B2 (en) 2015-11-17

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