CN103906733A - Trpm8拮抗剂及其在治疗中的用途 - Google Patents

Trpm8拮抗剂及其在治疗中的用途 Download PDF

Info

Publication number
CN103906733A
CN103906733A CN201280041145.5A CN201280041145A CN103906733A CN 103906733 A CN103906733 A CN 103906733A CN 201280041145 A CN201280041145 A CN 201280041145A CN 103906733 A CN103906733 A CN 103906733A
Authority
CN
China
Prior art keywords
methyl
trifluoromethyl
phenyl
carboxamide
pyridin
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201280041145.5A
Other languages
English (en)
Chinese (zh)
Inventor
K.比斯瓦斯
J.布朗
坚.J.陈
V.K.戈尔
S.哈里德
D.B.霍尔恩
M.R.卡勒
刘庆艳
马裕
H.莫宁谢恩
T.T.阮
原晨光
W.钟
D.J.小圣让
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Amgen Inc
Original Assignee
Amgen Inc
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 Amgen Inc filed Critical Amgen Inc
Publication of CN103906733A publication Critical patent/CN103906733A/zh
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
CN201280041145.5A 2011-06-24 2012-06-21 Trpm8拮抗剂及其在治疗中的用途 Pending CN103906733A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161500843P 2011-06-24 2011-06-24
US61/500,843 2011-06-24
PCT/US2012/043566 WO2012177893A2 (en) 2011-06-24 2012-06-21 Trpm8 antagonists and their use in treatments

Publications (1)

Publication Number Publication Date
CN103906733A true CN103906733A (zh) 2014-07-02

Family

ID=46384521

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280041145.5A Pending CN103906733A (zh) 2011-06-24 2012-06-21 Trpm8拮抗剂及其在治疗中的用途

Country Status (23)

Country Link
US (3) US8710043B2 (https=)
EP (1) EP2723717A2 (https=)
JP (1) JP2014527511A (https=)
KR (1) KR20140045507A (https=)
CN (1) CN103906733A (https=)
AP (1) AP2013007331A0 (https=)
AR (1) AR086750A1 (https=)
AU (1) AU2012272895B2 (https=)
BR (1) BR112013033316A2 (https=)
CA (1) CA2839699A1 (https=)
CL (1) CL2013003715A1 (https=)
CO (1) CO6852073A2 (https=)
CR (1) CR20140037A (https=)
EA (1) EA201490152A1 (https=)
MA (1) MA35271B1 (https=)
MX (1) MX2013015274A (https=)
MY (1) MY157429A (https=)
PE (1) PE20140868A1 (https=)
PH (1) PH12013502611A1 (https=)
TN (1) TN2013000529A1 (https=)
TW (2) TW201429948A (https=)
UY (1) UY34160A (https=)
WO (1) WO2012177893A2 (https=)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107922332A (zh) * 2015-08-28 2018-04-17 台湾神隆股份有限公司 阿普斯特的新形式及其制备方法
CN110981795A (zh) * 2019-12-18 2020-04-10 武汉世纪久海检测技术有限公司 一种利用2-氰基异烟酸甲酯制备2-酰胺基异烟酸的方法
CN115697327A (zh) * 2020-06-17 2023-02-03 默沙东有限责任公司 作为nav1.8抑制剂的5-氧代-吡咯烷-3-甲酰胺
CN116056697A (zh) * 2020-06-17 2023-05-02 默沙东有限责任公司 作为nav1.8抑制剂的2-氧代-噁唑烷-5-甲酰胺
CN119118901A (zh) * 2024-09-09 2024-12-13 中国人民解放军北部战区总医院 一种氧吲哚类衍生物及其制备方法与在trpa1抑制剂方向的应用
CN120025283A (zh) * 2023-11-28 2025-05-23 成都地奥制药集团有限公司 酰胺类化合物及其用途

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
ES2895174T3 (es) 2014-09-29 2022-02-17 Scripps Research Inst Moduladores del receptor de esfingosina-1-fosfato para el tratamiento de trastornos cardiopulmonares
KR20230005413A (ko) * 2016-06-13 2023-01-09 미쓰비시 타나베 파마 코퍼레이션 혈관운동증상의 치료 또는 예방을 위한 조성물
PE20200696A1 (es) 2017-06-22 2020-06-16 Curadev Pharma Ltd Moduladores de moleculas pequenas de sting humana
US20200138827A1 (en) * 2017-06-22 2020-05-07 Curadev Pharma Limited Small molecule modulators of human sting
BR112020012111A2 (pt) 2017-12-19 2020-11-24 Mitsubishi Tanabe Pharma Corporation composições e métodos para tratar ou prevenir sintomas vasomotores
JP2021523092A (ja) * 2018-03-21 2021-09-02 ピラマル・ファーマ・リミテッドＰｉｒａｍａｌ Ｐｈａｒｍａ Ｌｉｍｉｔｅｄ アルファ−（ジアリールメチル）アルキルアミンの改良された不斉合成
US11279672B2 (en) * 2018-04-18 2022-03-22 Piramal Pharma Limited Asymmetric synthesis of alpha-branched chiral amines
CA3136632A1 (en) 2019-04-11 2020-10-15 Goldfinch Bio, Inc. Spray-dried formulation of a pyridazinone trpc5 inhibitor
GEP20257750B (en) 2020-06-17 2025-03-25 Merck Sharp & Dohme Llc 2-oxoimidazolidine-4-carboxamides as nav1.8 inhibitors
US20240294500A1 (en) * 2021-06-08 2024-09-05 Hangzhou Glubio Pharmaceutical Co., Ltd. Isoindolinone compounds, and uses thereof
CN115108980B (zh) * 2022-06-22 2023-06-16 济南大学 一种2-甲基喹啉类化合物的4号位酰基化衍生物的制备方法

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2483250A (en) * 1949-09-27 Tt a it tt
WO2005005392A1 (en) * 2003-07-07 2005-01-20 Ionix Pharmaceuticals Limited Azacyclic compounds as inhibitors of sensory neurone specific channels
WO2005046683A1 (en) * 2003-10-07 2005-05-26 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2006068594A1 (en) * 2004-12-21 2006-06-29 Astrazeneca Ab HETEROCYCLIC MCHr1 ANTAGONISTS AND THEIR USE IN THERAPY
CN101035783A (zh) * 2004-08-30 2007-09-12 神经医药品有限公司 作为钙通道阻断剂的脲衍生物
WO2008022938A1 (en) * 2006-08-21 2008-02-28 F. Hoffmann-La Roche Ag Di-aromatic substituted amides as inhibitors for glyt1
CN101466676A (zh) * 2006-04-12 2009-06-24 默克公司 吡啶基酰胺类t-型钙通道拮抗剂
US20090239876A1 (en) * 2008-03-18 2009-09-24 Clements Matthew J Substituted 4-Hydroxypyrimidine-5-Carboxamides

Family Cites Families (170)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2417763A1 (de) 1974-04-11 1975-10-30 Bayer Ag Carbonsaeureamide, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
DE2428673A1 (de) 1974-06-14 1976-01-02 Bayer Ag Carbonsaeureamide, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
US5081131A (en) 1986-01-13 1992-01-14 American Cyanamid Company Omega-((hetero)alkyl)benz(cd)-indol-2-amines
US5223499A (en) 1989-05-30 1993-06-29 Merck & Co., Inc. 6-amino substituted imidazo[4,5-bipyridines as angiotensin II antagonists
IL98167A0 (en) 1990-05-30 1992-06-21 Ici Plc Anti-tumour quinazoline derivatives,processes for their preparation and pharmaceutical compositions comprising them
US5380721A (en) 1990-09-10 1995-01-10 Sterling Winthrop Inc. Aryl-fused and hetaryl-fused-2,4-diazepine and 2,4-diazocine antiarrhythmic agents
WO1992012973A1 (en) 1991-01-23 1992-08-06 Nippon Kayaku Kabushiki Kaisha Chroman derivative
ES2036926B1 (es) 1991-08-08 1994-01-16 Uriach & Cia Sa J "procedimiento para la obtencion de derivados de la (2-alquil-3-piridil)metilpiperazina".
JP2600644B2 (ja) 1991-08-16 1997-04-16 藤沢薬品工業株式会社 チアゾリルベンゾフラン誘導体
DE4135474A1 (de) 1991-10-28 1993-04-29 Bayer Ag 2-aminomethyl-chromane
DE4138819A1 (de) 1991-11-26 1993-05-27 Basf Ag Hydroxypyridoncarbonsaeureamide, deren herstellung und verwendung
GB9127041D0 (en) 1991-12-20 1992-02-19 Fujisawa Pharmaceutical Co New use
FR2692895A1 (fr) 1992-06-26 1993-12-31 Adir Nouveaux 1-oxo 2,4,5,6-tétrahydro 2,3,7-triazaphénalènes leurs procédés de préparation et les compositions pharmaceutiques qui les contiennent.
DE4304455A1 (de) 1993-02-15 1994-08-18 Bayer Ag Heterocyclisch substituierte Phenyl-cyclohexan-carbonsäurederivate
JPH07179488A (ja) 1993-11-12 1995-07-18 Tanabe Seiyaku Co Ltd グルコサミン誘導体、その製法及びその合成中間体
AU4432496A (en) 1994-12-23 1996-07-19 Dr. Karl Thomae Gmbh Piperazine derivatives, medicaments containing the same, their use and process for preparing the same
JPH11501934A (ja) 1995-03-14 1999-02-16 シャスカン，エドワード・ジー ニコチニルアラニンと、グリシン抱合の阻害薬又はビタミンｂ６とを含む組成物
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
IN186549B (https=) 1995-04-19 2001-09-29 Kumiai Chemical Co Ltd
DE19518681A1 (de) 1995-05-22 1996-11-28 Bayer Ag Verfahren zur Herstellung von 5,6-Dihydro-1,3-oxazinen
DE19523087A1 (de) 1995-06-26 1997-01-02 Bayer Ag 1,3-Oxa(thia)zin-Derivate
IL118631A (en) 1995-06-27 2002-05-23 Tanabe Seiyaku Co History of pyridazinone and processes for their preparation
GB9518552D0 (en) 1995-09-11 1995-11-08 Fujisawa Pharmaceutical Co New heterocyclic compounds
EP0858457A1 (de) 1995-10-20 1998-08-19 Dr. Karl Thomae GmbH 5-gliedrige heterocyclen, diese verbindungen enthaltende arzneimittel und deren verwendung sowie verfahren zu ihrer herstellung
GB9525828D0 (en) 1995-12-18 1996-02-21 Bayer Ag Use of hetarylacetic acid derivatives
US5977090A (en) 1996-09-27 1999-11-02 Guilford Pharmaceuticals Inc. Pharmaceutical compositions and methods of treating compulsive disorders using NAALADase inhibitors
US6268384B1 (en) 1997-08-29 2001-07-31 Vertex Pharmaceuticals Incorporated Compounds possessing neuronal activity
US6075029A (en) 1998-01-02 2000-06-13 Cell Therapeutics, Inc. Xanthine modulators of metabolism of cellular P-450
JP4432261B2 (ja) 1998-01-21 2010-03-17 萬有製薬株式会社 複素芳香環縮合シクロペンテノピリジン誘導体
EP1082095A1 (en) 1998-06-03 2001-03-14 GPI NIL Holdings, Inc. N-oxide of heterocyclic ester, amide, thioester or ketone hair growth compositions and uses
US5910595A (en) 1998-06-26 1999-06-08 Salsbury Chemicals, Inc. Process for preparing oximidazoles
US6617351B1 (en) 1998-07-31 2003-09-09 Eli Lilly And Company Amide, carbamate, and urea derivatives
US6166028A (en) 1998-12-09 2000-12-26 American Home Products Corporation Diaminopuridine-containing thiourea inhibitors of herpes viruses
WO2000035889A1 (en) 1998-12-11 2000-06-22 Sankyo Company, Limited Substituted benzylamines
WO2000038683A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
US6200993B1 (en) 1999-05-05 2001-03-13 Merck Frosst Canada & Co. Heterosubstituted pyridine derivatives as PDE4 inhibitors
TR200002099A3 (tr) 1999-07-22 2001-06-21 Sankyo Company Limited Siklobüten türevleri, bunlarin hazirlanmasi ve terapötik kullanimlari
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
BR0013593A (pt) 1999-09-01 2002-05-07 Unilever Nv Método para alvejar manchas de tecido
EP1208188A1 (en) 1999-09-01 2002-05-29 Unilever Plc Composition and method for bleaching a substrate
BR0013592A (pt) 1999-09-01 2002-05-07 Unilever Nv Embalagem comercial para alvejar manchas de tecido em um licor de lavagem aquoso, e, uso da mesma
US7291641B2 (en) 1999-10-11 2007-11-06 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
HK1045991B (en) 1999-11-10 2004-12-10 Takeda Pharmaceutical Company Limited 5-membered n-heterocyclic compounds with hypoglycemic and hypolipidemic activity
IL139450A0 (en) 1999-11-10 2001-11-25 Pfizer Prod Inc Methods of administering apo b-secretion/mtp inhibitors
CA2325358C (en) 1999-11-10 2005-08-02 Pfizer Products Inc. 7-¬(4'-trifluoromethyl-biphenyl-2-carbonyl)amino|-quinoline-3-carboxylic acid amides, and methods of inhibiting the secretion of apolipoprotein b
TW574193B (en) 1999-12-03 2004-02-01 Astrazeneca Ab Novel phenalkyloxy-phenyl derivatives, pharmaceutical composition containing the same and their uses
EP1244656A1 (en) 1999-12-28 2002-10-02 Pfizer Products Inc. Non-peptidyl inhibitors of vla-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases
US20030195212A1 (en) 2000-01-28 2003-10-16 Torbjorn Lundstedt Novel melanocortin receptor agonists and antagonists
WO2001058869A2 (en) 2000-02-11 2001-08-16 Bristol-Myers Squibb Company Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators in treating respiratory and non-respiratory diseases
US20020019527A1 (en) 2000-04-27 2002-02-14 Wei-Bo Wang Substituted phenyl farnesyltransferase inhibitors
HK1053833A1 (zh) 2000-04-27 2003-11-07 Abbott Laboratories 取代苯基法呢基转移酶抑制剂
US6448281B1 (en) 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
US6417367B1 (en) 2000-08-11 2002-07-09 Pfizer Inc. Methods of making quinoline amides
US20030050211A1 (en) 2000-12-14 2003-03-13 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Enzymatic detergent compositions
WO2002051396A1 (en) 2000-12-26 2002-07-04 Sankyo Company, Limited Pharmaceutical compositions containing cyclobutene derivatives
AU2002242996A1 (en) 2001-03-29 2002-10-15 Tanabe Seiyaku Co., Ltd. Spiroisoquinoline compounds, methods for their preparation and intermediates
DE10121003A1 (de) 2001-04-28 2002-12-19 Aventis Pharma Gmbh Anthranilsäureamide, Verfahren zur Herstellung, ihrer Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen
MY130373A (en) 2001-10-29 2007-06-29 Malesci Sas Linear basic compounds having nk-2 antagonist activity and formulations thereof
DE60226063T2 (de) 2001-11-27 2009-05-20 F. Hoffmann-La Roche Ag Benzothiazole derivative
JP2005510564A (ja) 2001-11-28 2005-04-21 藤沢薬品工業株式会社 アポリポタンパク質ｂ阻害剤としての複素環式アミド化合物
AR037746A1 (es) 2001-12-06 2004-12-01 Novartis Ag Compuestos derivados de amidoacetonitrilo, un procedimiento para su preparacion, un procedimiento para la preparacion de compuestos intermediarios, una composicion para combatir parasitos, un procedimiento para combatir dichos parasitos, y el empleo de dichos derivados para la preparacion de una com
SE0104248D0 (sv) 2001-12-14 2001-12-14 Astrazeneca Ab Method of treatment
BR0307441A (pt) 2002-02-04 2005-01-04 Hoffmann La Roche Compostos, processo para a preparação de um composto, composição farmacêutica, utilização desses compostos, método para o tratamento e profilaxia de enfermidades e método para o tratamento de obesidade
KR20040095311A (ko) 2002-03-28 2004-11-12 어플라이드 리서치 시스템스 에이알에스 홀딩 엔.브이. 프로스타글란딘 ｆ 수용체의 모듈레이터로서의 티아졸리딘카르복사미드 유도체
DE60335869D1 (de) 2002-04-11 2011-03-10 Merck Sharp & Dohme 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
FR2838739B1 (fr) 2002-04-19 2004-05-28 Sanofi Synthelabo Derives de n-[phenyl(piperidin-2-yl)methyl)benzamide, leur preparation et leur application en therapeutique
BR0309522A (pt) 2002-04-26 2005-02-09 Ishihara Sangyo Kaisha Compostos piridina ou sais destes e herbicidas contendo os mesmos
US7375093B2 (en) 2002-07-05 2008-05-20 Intrexon Corporation Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
FR2842805A1 (fr) 2002-07-29 2004-01-30 Sanofi Synthelabo Derives de n-[phenyl(piperidin-2-yl)methyl]benzamide,leur preparation et leur application et therapeutique
GB0221697D0 (en) 2002-09-18 2002-10-30 Unilever Plc Novel compouds and their uses
JP2006510597A (ja) 2002-09-27 2006-03-30 メルク　エンド　カムパニー　インコーポレーテッド 置換ピリミジン類
WO2004039795A2 (en) 2002-10-29 2004-05-13 Fujisawa Pharmaceutical Co., Ltd. Amide compounds for the treatment of hyperlipidemia
ATE479683T1 (de) 2002-11-05 2010-09-15 Glaxo Group Ltd Antibakterielle mittel
AU2003290333A1 (en) 2002-12-24 2004-07-22 Biofocus Plc Compound libraries of imidazo(1,5-a)pyridin-3-yl derivatives and related heterobicycles for targetting compounds capable of binding to g-protein coupled receptors
WO2004072018A1 (ja) 2003-02-12 2004-08-26 Takeda Pharmaceutical Company Limited アミン誘導体
EP1625115A1 (en) 2003-05-09 2006-02-15 Pharmacia & Upjohn Company LLC Substituted pyrimidine derivatives
EP1776362A1 (en) 2003-07-18 2007-04-25 Virochem Pharma Inc. Spiro compounds and methods for the modulation of chemokine receptor activity
US7094791B2 (en) 2003-07-31 2006-08-22 Avalon Pharmaceuticals, Inc. Derivatives of 3-hydroxy-pyrrole-2,4-dicarboxylic acid and uses thereof
EP1664042A1 (en) 2003-09-03 2006-06-07 Galapagos N.V. IMIDAZO 1,5-a PYRIDINE OR IMIDAZO 1,5-a PIPERIDINE DERIVATIVES AND THEIR USE FOR THE PREPARATION OF MEDICAMENT AGAINST 5-HT2A RECEPTOR-RELATED DISORDERS
GB0320983D0 (en) 2003-09-08 2003-10-08 Biofocus Plc Compound libraries
EP1786816A4 (en) 2003-09-10 2009-11-04 Virochem Pharma Inc SPIROHYDANTOIN COMPOUNDS AND METHODS FOR MODULATING CHEMOKINE RECEPTOR ACTIVITY
US20050176767A1 (en) 2003-10-30 2005-08-11 Laval Chan Chun Kong Pyridine carboxamide and methods for inhibiting HIV integrase
GEP20084360B (en) 2004-02-04 2008-04-29 Pfizer Prod Inc Substituted quinoline compounds
GB0403578D0 (en) 2004-02-18 2004-03-24 Biofocus Discovery Ltd Compounds which interact with the G-protein coupled receptor family
US20070185152A1 (en) 2004-03-02 2007-08-09 Smithkline Beecham Corporation Inhibitors of akt activity
AU2005230902A1 (en) 2004-03-31 2005-10-20 Janssen Pharmaceutica, N.V. Non-imidazole heterocyclic compounds as histamine H3-receptor ligands
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
US7550499B2 (en) 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
US20090105218A1 (en) 2004-05-29 2009-04-23 7Tm Pharma A/S CRTH2 Receptor Ligands For Therapeutic Use
DE102004039876A1 (de) 2004-06-23 2006-01-26 Lanxess Deutschland Gmbh Herstellung von fluorierten 1,3-Benzodioxanen
DE102004031323A1 (de) 2004-06-29 2006-01-19 Bayer Cropscience Ag Substituierte Pyridazincarboxamide und Derivate hiervon
AR050926A1 (es) 2004-09-03 2006-12-06 Astrazeneca Ab Derivados de benzamida como inhibidores de la histonadesacetilasa(hdac)
KR100677149B1 (ko) 2004-11-12 2007-02-02 삼성전자주식회사 잉크 조성물
US20080051418A1 (en) 2004-11-26 2008-02-28 Tsuyoshi Maekawa Arylalkanoic Acid Derivative
US20080207677A1 (en) 2004-12-31 2008-08-28 Gpc Biotech Ag Napthyridine Compounds As Rock Inhibitors
US20060173183A1 (en) 2004-12-31 2006-08-03 Alantos Pharmaceuticals, Inc., Multicyclic bis-amide MMP inhibitors
US20080146612A1 (en) 2005-01-27 2008-06-19 Astrazeneca Ab Novel Biaromatic Compounds, Inhibitors of the P2X7-Receptor
WO2006094246A2 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. N-arylmethyl benzamide sirtuin modulators
US20070155738A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
AU2006252768A1 (en) 2005-06-02 2006-12-07 Bayer Cropscience Ag Phenylalkyl substituted heteroaryl devivatives
EP1899294B1 (en) 2005-06-13 2015-03-18 Merck Sharp & Dohme Limited Therapeutic agents
US8703805B2 (en) 2005-06-27 2014-04-22 Exelixis Patent Company Llc Modulators of LXR
NZ563202A (en) 2005-07-15 2011-02-25 Nissan Chemical Ind Ltd Thiophene compounds and thrombopoietin receptor activators
CN100494167C (zh) 2005-08-02 2009-06-03 天津大学 抗乙肝病毒的叔胺氧化物及制备方法和制备药物的应用
WO2007017093A1 (en) 2005-08-04 2007-02-15 Bayer Healthcare Ag Substituted 2-benzyloxy-benzoic acid amide derivatives
EP1764098A1 (en) 2005-09-17 2007-03-21 Speedel Experimenta AG Diaminoalcohols derivatives for the treatment of Alzheimer, malaria, HIV
WO2007054215A1 (en) 2005-11-10 2007-05-18 Bayer Healthcare Ag Diaryl ureas for treating pulmonary hypertension
WO2007054302A1 (en) 2005-11-10 2007-05-18 Bayer Healthcare Ag Diaryl ureas for treating diabetic neuropathy
US7888376B2 (en) 2005-11-23 2011-02-15 Bristol-Myers Squibb Company Heterocyclic CETP inhibitors
DE102005059479A1 (de) 2005-12-13 2007-06-14 Merck Patent Gmbh Hydroxychinolinderivate
WO2007068383A1 (en) 2005-12-15 2007-06-21 Bayer Healthcare Ag Diaryl ureas for treating virus infections
CA2633411A1 (en) 2005-12-15 2007-06-21 Bayer Healthcare Ag Diaryl ureas for treating inflammatory skin, eye and/or ear diseases
TWI412322B (zh) 2005-12-30 2013-10-21 Du Pont 控制無脊椎害蟲之異唑啉
EP1981882A4 (en) 2006-01-27 2009-11-18 Astrazeneca Ab QUINOLINES SUBSTITUTED BY AN AMIDE
EP1987037A2 (en) 2006-02-23 2008-11-05 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
DE102006012251A1 (de) 2006-03-15 2007-11-08 Grünenthal GmbH Substituierte 4-Amino-chinazolin-Derivate und ihre Verwendung zur Herstellung von Arzneimitteln
US20080045589A1 (en) 2006-05-26 2008-02-21 Susan Kelley Drug Combinations with Substituted Diaryl Ureas for the Treatment of Cancer
GB0611152D0 (en) 2006-06-06 2006-07-19 Ucb Sa Therapeutic agents
WO2008003746A1 (en) 2006-07-06 2008-01-10 Bayer Cropscience Sa N-(4-pyridin-2-ylbutyl) carboxamide derivatives, their process of preparation and their use as fungicides
RU2009106461A (ru) 2006-07-25 2010-08-27 Энвиво Фармасьютикалз, Инк. (Us) Хинолиновые производные
US7834023B2 (en) 2006-09-20 2010-11-16 Portola Pharmaceuticals, Inc. Substituted dihydroquinazolines as platelet ADP receptor inhibitors
WO2008056687A1 (en) 2006-11-09 2008-05-15 Daiichi Sankyo Company, Limited Novel spiropiperidine derivative
AU2007321923A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic matrix metalloprotease inhibitors
CA2670031A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic metalloprotease inhibitors
KR20090094125A (ko) 2006-12-08 2009-09-03 엑셀리시스, 인코포레이티드 Ｌｘｒ 및 ｆｘｒ 조절자
AU2007336811A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US20080293711A1 (en) 2007-03-08 2008-11-27 Clark Michael P Chemokine receptor modulators
JP2010523663A (ja) 2007-04-11 2010-07-15 メルク・シャープ・エンド・ドーム・コーポレイション 第３級アミド、スルホンアミド、カルバミン酸及び尿素末端基をもつｃｇｒｐ受容体アンタゴニスト
JP5511657B2 (ja) 2007-06-05 2014-06-04 メルク・シャープ・アンド・ドーム・コーポレーション カルボキサミドヘテロ環式ｃｇｒｐ受容体アンタゴニスト
EP2178866A2 (en) 2007-07-09 2010-04-28 AstraZeneca AB Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
CA2696725A1 (en) 2007-08-10 2009-03-26 Crystalgenomics, Inc. Pyridine derivatives and methods of use thereof
WO2009023179A2 (en) 2007-08-10 2009-02-19 Genelabs Technologies, Inc. Nitrogen containing bicyclic chemical entities for treating viral infections
WO2009038812A1 (en) 2007-09-20 2009-03-26 Amgen Inc. Condensed piperidine derivatives useful as vanilloid receptor ligands
WO2009073203A1 (en) 2007-12-04 2009-06-11 Amgen Inc. Trp-m8 receptor ligands and their use in treatments
JPWO2009072621A1 (ja) 2007-12-07 2011-04-28 日産化学工業株式会社 置換ジヒドロアゾール化合物及び有害生物防除剤
EP2272841A1 (en) 2008-03-28 2011-01-12 Banyu Pharmaceutical Co., Ltd. Diarylmethylamide derivative having antagonistic activity on melanin-concentrating hormone receptor
AR071310A1 (es) 2008-04-11 2010-06-09 Merck Serono Sa Sulfonamidas
DE102008019838A1 (de) 2008-04-19 2009-12-10 Boehringer Ingelheim International Gmbh Neue Arylsulfonylglycin-Derivate, deren Herstellung und deren Verwendung als Arzneimittel
JP2011523958A (ja) 2008-06-12 2011-08-25 メルク・シャープ・エンド・ドーム・コーポレイション Ｃｇｒｐ受容体アンタゴニストとしての分岐状３−及び６−置換キノリン
KR20110031294A (ko) 2008-06-25 2011-03-25 바이엘 쉐링 파마 악티엔게젤샤프트 심부전 치료를 위한 디아릴 우레아
WO2010021882A2 (en) * 2008-08-19 2010-02-25 Janssen Pharmaceutica Nv Cold menthol receptor antagonists
CN101343313B (zh) 2008-09-03 2011-11-16 南京农业大学 一种葡萄糖二肽类化合物及其制备方法和用途
EP2337563B1 (en) 2008-09-08 2014-04-09 The Board of Trustees of The Leland Stanford Junior University Modulators of aldehyde dehydrogenase activity and methods of use thereof
TWI389913B (zh) 2008-09-08 2013-03-21 Lg Life Sciences Ltd 并合雜環化合物
WO2010046780A2 (en) 2008-10-22 2010-04-29 Institut Pasteur Korea Anti viral compounds
AR074343A1 (es) 2008-11-14 2011-01-12 Amgen Inc Derivados de piridina y pirimidina como inhibidores de la fosfodiesterasa 10
UY32525A (es) 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides
RU2011148937A (ru) * 2009-05-01 2013-06-10 Раквалиа Фарма Инк. Производные сульфамоилбензойной кислоты в качестве антагонистов trpm8
EP2435407B1 (en) 2009-05-29 2019-12-25 RaQualia Pharma Inc. Aryl substituted carboxamide derivatives as calcium or sodium channel blockers
WO2010141330A1 (en) 2009-06-02 2010-12-09 Boehringer Ingelheim International Gmbh DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES
TW201103941A (en) * 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
WO2011014649A1 (en) 2009-07-29 2011-02-03 Duke University Compositions and methods for inhibiting hair growth
DE102009028929A1 (de) 2009-08-27 2011-07-07 Bayer Schering Pharma Aktiengesellschaft, 13353 Heterocyclisch-substituierte 2-Acetamido-5-Aryl-1,2,4-triazolone und deren Verwendung
UY32940A (es) 2009-10-27 2011-05-31 Bayer Cropscience Ag Amidas sustituidas con halogenoalquilo como insecticidas y acaricidas
AU2011204368B2 (en) 2010-01-06 2014-11-27 Joseph P. Errico Methods and compositions of targeted drug development
WO2011094890A1 (en) 2010-02-02 2011-08-11 Argusina Inc. Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators
WO2011106632A1 (en) 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
WO2011142359A1 (ja) 2010-05-10 2011-11-17 日産化学工業株式会社 スピロ化合物及びアディポネクチン受容体活性化薬
WO2011146300A1 (en) 2010-05-17 2011-11-24 Merck Sharp & Dohme Corp. Novel prolylcarboxypeptidase inhibitors
EP2576539B1 (de) 2010-05-27 2017-12-13 Bayer CropScience AG Pyridinylcarbonsäure derivate als fungizide
US9394290B2 (en) 2010-10-21 2016-07-19 Universitaet Des Saarlandes Campus Saarbruecken Selective CYP11B1 inhibitors for the treatment of cortisol dependent diseases
DE202011110963U1 (de) 2010-11-05 2017-11-07 Senomyx, Inc. Verbindungen, die als Modulatoren von TRPM8 nützlich sind
DK2649075T3 (en) 2010-12-08 2018-07-30 Us Health SUBSTITUTED PYRAZOLOPYRIMIDINES AS GLUCOCEREBROSIDASE ACTIVATORS
EP2651412A4 (en) 2010-12-14 2014-08-13 Beth Israel Hospital ANDROGEN RECEPTOR AND HER APPLICATION PROCEDURES
PT2652025T (pt) 2010-12-15 2018-11-02 Ppg Europe B V Composição secante e a sua utilização
WO2012083190A1 (en) 2010-12-17 2012-06-21 The Rockefeller University Insect odorant receptor antagonists
CN103635472B (zh) 2011-02-28 2018-01-12 阵列生物制药公司 丝氨酸/苏氨酸激酶抑制剂
WO2012120398A1 (en) 2011-03-04 2012-09-13 Pfizer Limited Aryl substituted carboxamide derivatives as trpm8 modulators
EP2723718A1 (en) 2011-06-24 2014-04-30 Amgen Inc. Trpm8 antagonists and their use in treatments

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2483250A (en) * 1949-09-27 Tt a it tt
WO2005005392A1 (en) * 2003-07-07 2005-01-20 Ionix Pharmaceuticals Limited Azacyclic compounds as inhibitors of sensory neurone specific channels
WO2005046683A1 (en) * 2003-10-07 2005-05-26 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
CN101035783A (zh) * 2004-08-30 2007-09-12 神经医药品有限公司 作为钙通道阻断剂的脲衍生物
WO2006068594A1 (en) * 2004-12-21 2006-06-29 Astrazeneca Ab HETEROCYCLIC MCHr1 ANTAGONISTS AND THEIR USE IN THERAPY
CN101466676A (zh) * 2006-04-12 2009-06-24 默克公司 吡啶基酰胺类t-型钙通道拮抗剂
WO2008022938A1 (en) * 2006-08-21 2008-02-28 F. Hoffmann-La Roche Ag Di-aromatic substituted amides as inhibitors for glyt1
US20090239876A1 (en) * 2008-03-18 2009-09-24 Clements Matthew J Substituted 4-Hydroxypyrimidine-5-Carboxamides

Non-Patent Citations (13)

* Cited by examiner, † Cited by third party
Title
ACS: "CAS：1214549-94-6", 《REGISTRY》 *
ACS: "CAS：1241062-82-7", 《REGISTRY》 *
ACS: "CAS1280882-39-4", 《REGISTRY》 *
ERUM K. RAJA等: "Superelectrophilic chemistry of amino-nitriles and related substrates", 《TETRAHEDRON》 *
FRANCOISE HEYMANS等: "Quantitative structure-activity relationships for N-[(N’,N’-disubstituted-amino)acetyl]arylamines for local anesthetic activity and acute toxicity", 《J.MED.CHEM.》 *
FRIEDRICH METZGER等: "Sulphonylurea binding in rat isolated glomeruli: pharmacological characterization and dependence on cell metabolism and cytoskeleton", 《NAUNYN-SCHMIEDEBERG’S ARCH PHARMACOL》 *
GUOHUA HOU等: "Iridium-Monodentate Phosphoramidite-Catalyzed Asymmetric Hydrogenation of Substituted Benzophenone N-H Imines", 《J. AM. CHEM. SOC.》 *
J. H. BOYER等: "Diazotization of 2-pyridylmethyl amine", 《J. ORG. CHEM》 *
PUBCHEM: "CID2437712", 《AC1M78XL-COMPOUND SUMMARY》 *
PUBCHEM: "CID52501511", 《ZINC58157967-COMPOUND SUMMARY》 *
TOSHIKATSU MAKI等: "4,5,6,7-Tetrachlorobenzo[d][1,3,2]dioxaborol-2-ol as an Effective Catalyst for the Amide Condensation of Sterically Demanding Carboxylic Acids", 《ORGANIC LETTERS》 *
V.A.KRASNOV等: "SYNTHESIS AND ANTICONVULSIVE ACTIVITY OF FLUORINE-SUBSTITUTED BENZHYDRYLAMIDES", 《PHARMACEUTICAL CHEMISTRY JOURNAL》 *
WAYNE E CHILDERS等: "Advances in the development of novel analgesics", 《EXPERT OPIN. THER. PATENTS》 *

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107922332A (zh) * 2015-08-28 2018-04-17 台湾神隆股份有限公司 阿普斯特的新形式及其制备方法
CN110981795A (zh) * 2019-12-18 2020-04-10 武汉世纪久海检测技术有限公司 一种利用2-氰基异烟酸甲酯制备2-酰胺基异烟酸的方法
CN115697327A (zh) * 2020-06-17 2023-02-03 默沙东有限责任公司 作为nav1.8抑制剂的5-氧代-吡咯烷-3-甲酰胺
CN116056697A (zh) * 2020-06-17 2023-05-02 默沙东有限责任公司 作为nav1.8抑制剂的2-氧代-噁唑烷-5-甲酰胺
US12516046B2 (en) 2020-06-17 2026-01-06 Merck Sharp & Dohme Llc 2-oxo-oxazolidine-5-carboxamides as NAV1.8 inhibitors
CN120025283A (zh) * 2023-11-28 2025-05-23 成都地奥制药集团有限公司 酰胺类化合物及其用途
CN120025283B (zh) * 2023-11-28 2026-01-09 成都地奥制药集团有限公司 酰胺类化合物及其用途
CN119118901A (zh) * 2024-09-09 2024-12-13 中国人民解放军北部战区总医院 一种氧吲哚类衍生物及其制备方法与在trpa1抑制剂方向的应用

Also Published As

Publication number Publication date
PE20140868A1 (es) 2014-07-18
CA2839699A1 (en) 2012-12-27
TWI448454B (zh) 2014-08-11
TW201311643A (zh) 2013-03-16
US20130157996A1 (en) 2013-06-20
MX2013015274A (es) 2014-03-31
US20140171639A1 (en) 2014-06-19
EA201490152A1 (ru) 2014-05-30
AU2012272895A1 (en) 2013-04-11
US20140171406A1 (en) 2014-06-19
MA35271B1 (fr) 2014-07-03
TN2013000529A1 (en) 2015-03-30
US8710043B2 (en) 2014-04-29
TW201429948A (zh) 2014-08-01
CL2013003715A1 (es) 2014-06-27
WO2012177893A2 (en) 2012-12-27
BR112013033316A2 (pt) 2017-01-31
CO6852073A2 (es) 2014-01-30
AP2013007331A0 (en) 2013-12-31
UY34160A (es) 2012-08-31
WO2012177893A3 (en) 2013-06-13
EP2723717A2 (en) 2014-04-30
CR20140037A (es) 2014-03-13
PH12013502611A1 (en) 2014-04-28
KR20140045507A (ko) 2014-04-16
AU2012272895B2 (en) 2015-01-22
MY157429A (en) 2016-06-15
JP2014527511A (ja) 2014-10-16
AR086750A1 (es) 2014-01-22
US9096527B2 (en) 2015-08-04

Similar Documents

Publication Publication Date Title
CN103906733A (zh) Trpm8拮抗剂及其在治疗中的用途
CN104024252B (zh) 用于治疗肺动脉高压的双环杂环衍生物
JP7001682B2 (ja) 置換１Ｈ－イミダゾ［４，５－ｂ］ピリジン－２（３Ｈ）－オン及びＧＬＵＮ２Ｂ受容体調節因子としてのそれらの使用
KR102680164B1 (ko) Rock 억제제로서의 페닐아세트아미드
JP5744021B2 (ja) 新規なニコチンアミド誘導体またはその塩
TWI546302B (zh) 稠合雜環化合物
JP6964576B2 (ja) 置換４−アザインドール及びｇｌｕｎ２ｂ受容体調節因子としてのそれらの使用
TWI706952B (zh) 氮雜苯并咪唑類及其作為ａｍｐａ受體調控劑之用途
JP5931752B2 (ja) 縮環複素環誘導体
JP6545199B2 (ja) ３−アミノ−１，５，６，７−テトラヒドロ−４ｈ−インドール−４−オン類
JP4907746B2 (ja) ヘテロアリールアミド誘導体およびグルコキナーゼ活性化因子としてのその使用
TWI458727B (zh) 作為激酶抑制劑之吡咯并吡啶
TW202214573A (zh) 作為nav1.8抑制劑之2-氧基咪唑啶-4-甲醯胺
JP2025526302A (ja) Ｉｒａｋ４のリガンド指向性分解剤としてのヘテロアリール化合物
TWI577677B (zh) 作爲ｔｔｘ－ｓ阻斷劑之吡咯並吡啶酮衍生物
JP2022554391A (ja) ＭｒｇｐｒＸ２アンタゴニストおよびその使用
TW201418240A (zh) 作爲ｔｒｐｍ８抑制劑之色滿（ｃｈｒｏｍａｎ）衍生物
US6610701B2 (en) Thrombin inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20140702