CA2839699A1 - Trpm8 antagonists and their use in treatments - Google Patents

Trpm8 antagonists and their use in treatments Download PDF

Info

Publication number
CA2839699A1
CA2839699A1 CA2839699A CA2839699A CA2839699A1 CA 2839699 A1 CA2839699 A1 CA 2839699A1 CA 2839699 A CA2839699 A CA 2839699A CA 2839699 A CA2839699 A CA 2839699A CA 2839699 A1 CA2839699 A1 CA 2839699A1
Authority
CA
Canada
Prior art keywords
methyl
phenyl
carboxamide
trifluoromethyl
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.)
Abandoned
Application number
CA2839699A
Other languages
English (en)
French (fr)
Inventor
Kaustav Biswas
James Brown
Jian J. Chen
Vijay Keshav Gore
Scott Harried
Daniel B. Horne
Matthew R. Kaller
Qingyian Liu
Vu Van Ma
Holger Monenschein
Thomas T. Nguyen
Chester Chenguang Yuan
Wenge Zhong
David J. St. Jean, Jr.
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 CA2839699A1 publication Critical patent/CA2839699A1/en
Abandoned 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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
CA2839699A 2011-06-24 2012-06-21 Trpm8 antagonists and their use in treatments Abandoned CA2839699A1 (en)

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
CA2839699A1 true CA2839699A1 (en) 2012-12-27

Family

ID=46384521

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2839699A Abandoned CA2839699A1 (en) 2011-06-24 2012-06-21 Trpm8 antagonists and their use in treatments

Country Status (23)

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

Families Citing this family (17)

* 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
US9765026B2 (en) * 2015-08-28 2017-09-19 Scinopharm Taiwan, Ltd. Forms of apremilast and the process of making the same
KR20230005413A (ko) * 2016-06-13 2023-01-09 미쓰비시 타나베 파마 코퍼레이션 혈관운동증상의 치료 또는 예방을 위한 조성물
JP7296954B2 (ja) 2017-06-22 2023-06-23 キュラデブ・ファーマ・リミテッド ヒトｓｔｉｎｇの小分子調節因子
JP2020524717A (ja) * 2017-06-22 2020-08-20 キュラデブ・ファーマ・リミテッドＣｕｒａｄｅｖ Ｐｈａｒｍａ Ｌｉｍｉｔｅｄ ヒトｓｔｉｎｇの小分子調節因子
AU2018391882A1 (en) 2017-12-19 2020-07-02 Mitsubishi Tanabe Pharma Corporation Compositions and methods for treating or preventing vasomotor symptoms
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
JP2021522176A (ja) * 2018-04-18 2021-08-30 ピラマル ファーマ リミテッド アルファ−分岐キラルアミンの改善された不斉合成
CN110981795B (zh) * 2019-12-18 2021-02-12 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-氨酰基异烟酸的方法
BR112022024450A2 (pt) * 2020-06-17 2022-12-27 Merck Sharp & Dohme Llc 2-oxo-oxazolidina-5-carboxamidas como inibidores de nav1.8
MX2022015580A (es) * 2020-06-17 2023-01-24 Merck Sharp & Dohme Llc 5-oxopirrolidin-3-carboxamidas como inhibidores de nav1.8.
TWI806073B (zh) 2020-06-17 2023-06-21 美商默沙東有限責任公司 作為nav1.8抑制劑之2-氧基咪唑啶-4-甲醯胺
AU2022289605B2 (en) * 2021-06-08 2024-12-19 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
WO2025113520A1 (zh) * 2023-11-28 2025-06-05 成都地奥制药集团有限公司 酰胺类化合物及其用途
CN119118901B (zh) * 2024-09-09 2025-09-30 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

Family Cites Families (178)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2483250A (en) * 1949-09-27 Tt a it tt
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
EP0653434A1 (en) 1993-11-12 1995-05-17 Tanabe Seiyaku Co., Ltd. Glucosamine derivative, process for preparing the same and synthetic intermediate thereof
BR9510360A (pt) 1994-12-23 1997-12-23 Thomae Gmbh Dr K Derivados de piperazina medicamentos contendo esses compostos sua aplicação e processo para sua preparação
AU707084B2 (en) 1995-03-14 1999-07-01 Edward G. Shaskan Compositions comprising nicotynylalanine and an inhibitor of glycine conjugation or vitamin B6
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
IN186549B (enExample) 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
JPH11513382A (ja) 1995-10-20 1999-11-16 ドクトル カルル トーマエ ゲゼルシャフト ミット ベシュレンクテル ハフツング ５員複素環化合物、これらの化合物を含む医薬品、それらの使用及びそれらの調製方法
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
ES2216482T3 (es) 1998-01-21 2004-10-16 Banyu Pharmaceutical Co., Ltd. Derivado de 5-(2,2-difluoro-1,3-benzodioxol-5-il)ciclopentenopiridina sustituido.
JP2002516842A (ja) 1998-06-03 2002-06-11 ジーピーアイ ニル ホールディングズ インコーポレイテッド 複素環式エステル、アミド、チオエステル、またはケトンのｎ−オキシドである毛成長用組成物およびその使用方法
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
AU1684400A (en) 1998-12-11 2000-07-03 Sankyo Company Limited Substituted benzylamines
CA2348740A1 (en) 1998-12-23 2000-07-06 Ruth R. Wexler Thrombin or factor xa inhibitors
US6200993B1 (en) 1999-05-05 2001-03-13 Merck Frosst Canada & Co. Heterosubstituted pyridine derivatives as PDE4 inhibitors
CZ290178B6 (cs) 1999-07-22 2002-06-12 Sankyo Company Limited Deriváty cyklobutenu
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
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
BR0013593A (pt) 1999-09-01 2002-05-07 Unilever Nv Método para alvejar manchas de tecido
CA2383596A1 (en) 1999-09-01 2001-03-08 Unilever Plc Composition and method for bleaching a substrate
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
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
SI1228067T1 (en) 1999-11-10 2005-02-28 Takeda Chemical Industries, Ltd. 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
TW574193B (en) 1999-12-03 2004-02-01 Astrazeneca Ab Novel phenalkyloxy-phenyl derivatives, pharmaceutical composition containing the same and their uses
EE200200372A (et) 1999-12-28 2003-12-15 Pfizer Products Inc. VLA-4 sõltuva raku seostumise mittepeptiidsed inhibiitorid, mis on kasutatavad põletiku-, autoimmuun- ja respiratoorsete haiguste raviks
JP2003520850A (ja) 2000-01-28 2003-07-08 メラキュア セラピューティクス エービー 新規なメラノコルチン受容体作動薬および拮抗薬
CA2399791A1 (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
HK1053833A1 (zh) 2000-04-27 2003-11-07 Abbott Laboratories 取代苯基法呢基转移酶抑制剂
US20020019527A1 (en) 2000-04-27 2002-02-14 Wei-Bo Wang Substituted phenyl farnesyltransferase inhibitors
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
WO2002079189A2 (en) 2001-03-29 2002-10-10 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
WO2003045385A1 (en) 2001-11-27 2003-06-05 F. Hoffmann-La Roche Ag Benzothiazole derivatives
US20050038035A1 (en) 2001-11-28 2005-02-17 Hisashi Takasugi Heterocyclic amide compounds as apolipoprotein b inhibitors
TWI261053B (en) 2001-12-06 2006-09-01 Novartis Ag Amidoacetonitrile compounds, their preparation, compositions and use as pesticides
SE0104248D0 (sv) 2001-12-14 2001-12-14 Astrazeneca Ab Method of treatment
EP1474145B1 (en) 2002-02-04 2008-04-23 F. Hoffmann-La Roche Ag Quinoline derivatives as npy antagonists
WO2003082278A1 (en) 2002-03-28 2003-10-09 Applied Research Systems Ars Holding N.V. Thiazolidine carboxamide derivatives as modulators of the prostaglandin f receptor
WO2003086294A2 (en) 2002-04-11 2003-10-23 Merck & Co., Inc. 1h-benzo[f]indazol-5-yl derivatives as selective glucocorticoid receptor modulators
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
AU2003235125A1 (en) 2002-04-26 2003-11-10 Ishihara Sangyo Kaisha, Ltd. Pyridine compounds or salts thereof and herbicides containing the same
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
WO2004029204A2 (en) 2002-09-27 2004-04-08 Merck & Co., Inc. Substituted pyrimidines
WO2004039795A2 (en) 2002-10-29 2004-05-13 Fujisawa Pharmaceutical Co., Ltd. Amide compounds for the treatment of hyperlipidemia
AU2003291227A1 (en) 2002-11-05 2004-06-07 Smithkline Beecham Corporation Antibacterial agents
WO2004058755A2 (en) 2002-12-24 2004-07-15 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
EP1593667A4 (en) 2003-02-12 2009-03-04 Takeda Pharmaceutical Amine derivative
WO2004099148A1 (en) 2003-05-09 2004-11-18 Pharmacia & Upjohn Company Llc Substituted pyrimidine derivatives
EP1660454A1 (en) * 2003-07-07 2006-05-31 Vernalis (R&D) Limited Azacyclic compounds as inhibitors of sensory neurone specific channels
CA2573951A1 (en) 2003-07-18 2005-01-27 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
WO2005021545A1 (en) 2003-09-03 2005-03-10 Galapagos Nv 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
CA2579609A1 (en) 2003-09-10 2005-03-17 Virochem Pharma Inc. Spirohydantoin compounds and methods for the modulation of chemokine receptor activity
US7432281B2 (en) * 2003-10-07 2008-10-07 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2005042524A1 (en) 2003-10-30 2005-05-12 Virochem Pharma Inc. Pyridine carboxamide and methods for inhibiting hiv integrase
EA010369B1 (ru) 2004-02-04 2008-08-29 Пфайзер Продактс Инк. Замещенные хинолиновые соединения
GB0403578D0 (en) 2004-02-18 2004-03-24 Biofocus Discovery Ltd Compounds which interact with the G-protein coupled receptor family
JP2007526324A (ja) 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性のある阻害剤
CA2561791A1 (en) 2004-03-31 2005-10-20 Janssen Pharmaceutica, N.V. Non-imidazole heterocyclic compounds
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
EP1758571A1 (en) 2004-05-29 2007-03-07 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
CA2577398A1 (en) * 2004-08-30 2006-03-09 Neuromed Pharmaceuticals Ltd. Urea derivatives as calcium channel blockers
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
WO2006057448A1 (ja) 2004-11-26 2006-06-01 Takeda Pharmaceutical Company Limited アリールアルカン酸誘導体
EP1831194A4 (en) * 2004-12-21 2009-12-02 Astrazeneca Ab HETEROCYCLIC ANTAGONISTS OF MCHr1 AND THERAPEUTIC APPLICATIONS THEREOF
CA2593718A1 (en) 2004-12-31 2007-05-31 Gpc Biotech Ag Napthyridine compounds as rock inhibitors
US20060173183A1 (en) 2004-12-31 2006-08-03 Alantos Pharmaceuticals, Inc., Multicyclic bis-amide MMP inhibitors
JP2008528580A (ja) 2005-01-27 2008-07-31 アストラゼネカ・アクチエボラーグ Ｐ２ｘ７受容体の阻害剤である新規二環式芳香族化合物
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
WO2006130403A1 (en) 2005-06-02 2006-12-07 Bayer Cropscience Ag Phenylalkyl substituted heteroaryl devivatives
ES2536351T3 (es) 2005-06-13 2015-05-22 Merck Sharp & Dohme Limited Agentes terapéuticos
EP1910308B1 (en) 2005-06-27 2014-09-03 Exelixis Patent Company LLC Imidazole based lxr modulators
US7968542B2 (en) 2005-07-15 2011-06-28 Nissan Chemical Industries, 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
ATE493986T1 (de) 2005-11-10 2011-01-15 Bayer Schering Pharma Ag Diarylharnstoffe zur behandlung von pulmonaler hypertonie
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
WO2007068381A1 (en) 2005-12-15 2007-06-21 Bayer Healthcare Ag Diaryl ureas for treating inflammatory skin, eye and/or ear diseases
JP2009524585A (ja) 2005-12-15 2009-07-02 バイエル・ヘルスケア・アクチェンゲゼルシャフト ウイルス感染を処置するためのジアリールウレア
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
US20100234351A1 (en) 2006-02-23 2010-09-16 Takeda Pharmaceutical Company Limited Fused nitrogen-comprising heterocyclic compound
DE102006012251A1 (de) 2006-03-15 2007-11-08 Grünenthal GmbH Substituierte 4-Amino-chinazolin-Derivate und ihre Verwendung zur Herstellung von Arzneimitteln
CA2648569C (en) * 2006-04-12 2012-02-07 Merck & Co., Inc. Pyridyl amide t-type calcium channel antagonists
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
CN101611009A (zh) 2006-07-25 2009-12-23 伊维沃制药股份有限公司 喹啉衍生物
WO2008022938A1 (en) * 2006-08-21 2008-02-28 F. Hoffmann-La Roche Ag Di-aromatic substituted amides as inhibitors for glyt1
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
CA2670026A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterotricyclic metalloprotease inhibitors
AU2007321923A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic matrix metalloprotease inhibitors
KR20090094125A (ko) 2006-12-08 2009-09-03 엑셀리시스, 인코포레이티드 Ｌｘｒ 및 ｆｘｒ 조절자
BRPI0720695A2 (pt) 2006-12-21 2014-02-18 Plexxikon Inc Compostos e métodos para modulação de cinase, e indicações para estes
WO2008112156A1 (en) 2007-03-08 2008-09-18 Altiris Therapeutics Chemokine receptor modulators
AU2008239754A1 (en) 2007-04-11 2008-10-23 Merck Sharp & Dohme Corp. CGRP receptor antagonists with tertiary amide, sulfonamide, carbamate and urea end groups
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
JP2010533159A (ja) 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物９４７
CN101842098A (zh) 2007-08-10 2010-09-22 基因实验室技术有限公司 用于治疗病毒感染的含氮的二环化学实体
KR20100045480A (ko) 2007-08-10 2010-05-03 크리스탈지노믹스(주) 피리딘 유도체 및 이들의 사용방법
WO2009038812A1 (en) 2007-09-20 2009-03-26 Amgen Inc. Condensed piperidine derivatives useful as vanilloid receptor ligands
US8476297B2 (en) 2007-12-04 2013-07-02 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
AU2009225869B2 (en) * 2008-03-18 2014-01-23 Merck Sharp & Dohme Llc Substituted 4-hydroxypyrimidine-5-carboxamides
US20110015198A1 (en) 2008-03-28 2011-01-20 Banyu Pharmaceutical Co., Inc. Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism
US20110028509A1 (en) 2008-04-11 2011-02-03 Merck Serono Sa Sulfonamides
DE102008019838A1 (de) 2008-04-19 2009-12-10 Boehringer Ingelheim International Gmbh Neue Arylsulfonylglycin-Derivate, deren Herstellung und deren Verwendung als Arzneimittel
EP2299813B1 (en) 2008-06-12 2015-12-16 Merck Sharp & Dohme Corp. Branched 3- and 6-substituted quinolines as cgrp receptor antagonists
EP2293792A1 (en) 2008-06-25 2011-03-16 Bayer Schering Pharma Aktiengesellschaft Diaryl ureas for treating heart failure
EP2331498B1 (en) * 2008-08-19 2016-11-09 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
JP2012502048A (ja) 2008-09-08 2012-01-26 ボード オブ トラスティーズ オブ ザ レランド スタンフォード ジュニア ユニバーシティ アルデヒドデヒドロゲナーゼ活性のモジュレーターおよびその使用方法
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
TW201030001A (en) 2008-11-14 2010-08-16 Amgen Inc Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors
UY32525A (es) 2009-04-03 2010-10-29 Astrazeneca Ab Compuestos que tienen actividad agonista del receptor de glucocorticosteroides
CN102427810A (zh) * 2009-05-01 2012-04-25 拉夸里亚创药株式会社 作为trpm8拮抗剂的氨磺酰基苯甲酸衍生物
CN102448937A (zh) 2009-05-29 2012-05-09 拉夸里亚创药株式会社 作为钙或钠通道阻滞剂的芳基取代羧酰胺衍生物
JP5384733B2 (ja) 2009-06-02 2014-01-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ６，７−ジヒドロ−５Ｈ−イミダゾ［１，２−ａ］イミダゾール−３−カルボン酸アミドの誘導体
TW201103941A (en) * 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
BR112012002084A2 (pt) 2009-07-29 2016-11-08 Univ Duke composições e métodos para inibir crescimento de pelo
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
US20110212969A1 (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
EP2571855B1 (en) 2010-05-17 2014-12-24 Merck Sharp & Dohme Corp. Novel prolylcarboxypeptidase inhibitors
BR112012030184A2 (pt) 2010-05-27 2015-12-29 Bayer Cropscience Ag derivados de ácido piridinilcarboxílico como fungicidas
JP2013540145A (ja) 2010-10-21 2013-10-31 ウニベルシテート デス ザールランデス コルチゾール依存性疾患の治療用の選択的ｃｙｐ１１ｂ１阻害剤
PH12013500907A1 (en) 2010-11-05 2013-07-08 Firmenich Incorporated Compounds useful as modulators of trpm8
US9353117B2 (en) 2010-12-08 2016-05-31 The United States Of America As Represented By The Secretary, Dept. Of Health And Human Services 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
US20130324522A1 (en) 2010-12-17 2013-12-05 The Rockefeller University Insect odorant receptor antagonists
JP6085866B2 (ja) 2011-02-28 2017-03-01 アレイ バイオファーマ、インコーポレイテッド セリン／トレオニンキナーゼインヒビター
WO2012120398A1 (en) 2011-03-04 2012-09-13 Pfizer Limited Aryl substituted carboxamide derivatives as trpm8 modulators
AU2012272898A1 (en) 2011-06-24 2013-04-11 Amgen Inc. TRPM8 antagonists and their use in treatments

Also Published As

Publication number Publication date
TN2013000529A1 (en) 2015-03-30
US8710043B2 (en) 2014-04-29
US20140171406A1 (en) 2014-06-19
CO6852073A2 (es) 2014-01-30
WO2012177893A2 (en) 2012-12-27
AP2013007331A0 (en) 2013-12-31
AR086750A1 (es) 2014-01-22
WO2012177893A3 (en) 2013-06-13
TW201311643A (zh) 2013-03-16
JP2014527511A (ja) 2014-10-16
CL2013003715A1 (es) 2014-06-27
TW201429948A (zh) 2014-08-01
US9096527B2 (en) 2015-08-04
US20130157996A1 (en) 2013-06-20
MA35271B1 (fr) 2014-07-03
US20140171639A1 (en) 2014-06-19
MX2013015274A (es) 2014-03-31
CN103906733A (zh) 2014-07-02
EA201490152A1 (ru) 2014-05-30
AU2012272895B2 (en) 2015-01-22
CR20140037A (es) 2014-03-13
AU2012272895A1 (en) 2013-04-11
KR20140045507A (ko) 2014-04-16
PH12013502611A1 (en) 2014-04-28
MY157429A (en) 2016-06-15
BR112013033316A2 (pt) 2017-01-31
PE20140868A1 (es) 2014-07-18
TWI448454B (zh) 2014-08-11
EP2723717A2 (en) 2014-04-30
UY34160A (es) 2012-08-31

Similar Documents

Publication Publication Date Title
US9096527B2 (en) TRPM8 antagonists and their use in treatments
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
CA2681015C (en) Inhibitors of focal adhesion kinase
US20230265054A1 (en) Pyridyl inhibitors of hedgehog signalling
KR102680164B1 (ko) Rock 억제제로서의 페닐아세트아미드
KR101458006B1 (ko) Ttx-s 차단제로서의 아릴아미드 유도체
WO2014025651A1 (en) Chroman derivatives as trpm8 inhibitors
JP2008524246A (ja) ヒストンデアセチラーゼ阻害剤
RU2741000C2 (ru) Производное 1,4-дизамещенного имидазола
CA2761639A1 (en) Aryl substituted carboxamide derivatives as calcium or sodium channel blockers
CA2729581A1 (en) Fluorinated heteroaryls
JP2009525955A (ja) ヒストンデアセチラーゼ阻害剤
JP6511450B2 (ja) Ｗｎｔ経路のモジュレーターとしてのマレイミド誘導体
JP2021519263A (ja) 化合物及びその使用
CA2888485A1 (en) Phenyl linked quinolinyl modulators of ror.gamma.t
TR201816624T4 (tr) Pirazol bileşikleri ve t tipi kalsiyum kanalı bloke edicileri olarak kullanımları.
RS63471B1 (sr) Halo-supstituisani piperidini kao modulatori receptora oreksina
AU2012272898A1 (en) TRPM8 antagonists and their use in treatments
WO2019045006A1 (ja) モルヒナン誘導体
US8952009B2 (en) Chroman derivatives as TRPM8 inhibitors
US20150031668A1 (en) Chroman derivatives as trpm8 inhibitors

Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20170621