PL2421825T3 - Diamidy azetydynylowe jako inhibitory lipazy monoacyloglicerolowej - Google Patents

Diamidy azetydynylowe jako inhibitory lipazy monoacyloglicerolowej

Info

Publication number
PL2421825T3
PL2421825T3 PL10716205T PL10716205T PL2421825T3 PL 2421825 T3 PL2421825 T3 PL 2421825T3 PL 10716205 T PL10716205 T PL 10716205T PL 10716205 T PL10716205 T PL 10716205T PL 2421825 T3 PL2421825 T3 PL 2421825T3
Authority
PL
Poland
Prior art keywords
lipase inhibitors
monoacylglycerol lipase
diamides
azetidinyl
azetidinyl diamides
Prior art date
Application number
PL10716205T
Other languages
English (en)
Inventor
Haiyan Bian
Kristen M Chevalier
Peter J Connolly
Christopher M Flores
Shu-Chen Lin
Li Liu
John Mabus
Mark J Macielag
Mark E Mcdonnell
Philip M Pitis
Sui-Po Zhang
Yue-Mei Zhang
Bin Zhu
Jose Clemente
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PL2421825T3 publication Critical patent/PL2421825T3/pl

Links

Classifications

    • 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
    • C07D403/10—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 carbon chain containing aromatic 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • 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
    • C07D409/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D417/14—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 three or more hetero rings
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Otolaryngology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Toxicology (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Reproductive Health (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
PL10716205T 2009-04-22 2010-04-22 Diamidy azetydynylowe jako inhibitory lipazy monoacyloglicerolowej PL2421825T3 (pl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US17165809P 2009-04-22 2009-04-22
US17164909P 2009-04-22 2009-04-22
EP10716205.9A EP2421825B9 (en) 2009-04-22 2010-04-22 Azetidinyl diamides as monoacylglycerol lipase inhibitors
PCT/US2010/032082 WO2010124108A1 (en) 2009-04-22 2010-04-22 Azetidinyl diamides as monoacylglycerol lipase inhibitors

Publications (1)

Publication Number Publication Date
PL2421825T3 true PL2421825T3 (pl) 2014-06-30

Family

ID=42208680

Family Applications (1)

Application Number Title Priority Date Filing Date
PL10716205T PL2421825T3 (pl) 2009-04-22 2010-04-22 Diamidy azetydynylowe jako inhibitory lipazy monoacyloglicerolowej

Country Status (21)

Country Link
US (16) US8399454B2 (pl)
EP (8) EP2421824A1 (pl)
JP (8) JP2012524800A (pl)
KR (8) KR101705697B1 (pl)
CN (8) CN102459230A (pl)
AR (8) AR076382A1 (pl)
AU (9) AU2010238736A1 (pl)
BR (8) BRPI1014885A8 (pl)
CA (8) CA2759621C (pl)
DK (1) DK2421825T3 (pl)
ES (2) ES2538326T3 (pl)
HR (1) HRP20140295T1 (pl)
IL (8) IL215785A0 (pl)
PL (1) PL2421825T3 (pl)
PT (1) PT2421825E (pl)
RS (1) RS53235B (pl)
RU (8) RU2011147230A (pl)
SI (1) SI2421825T1 (pl)
SM (1) SMT201400034B (pl)
TW (8) TWI465446B (pl)
WO (8) WO2010124082A1 (pl)

Families Citing this family (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5896404B2 (ja) 2008-07-21 2016-03-30 ノバルティス アーゲー 加水分解性基を有するシリコーン含有ポリマー材料
JP2012524800A (ja) * 2009-04-22 2012-10-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ モノアシルグリセロールリパーゼ阻害剤としてのアゼチジニルジアミド
US9082128B2 (en) * 2009-10-19 2015-07-14 Uniloc Luxembourg S.A. System and method for tracking and scoring user activities
WO2011058766A1 (en) * 2009-11-16 2011-05-19 Raqualia Pharma Inc. Aryl carboxamide derivatives as ttx-s blockers
WO2011112263A1 (en) 2010-03-11 2011-09-15 New York University AMIDO COMPOUNDS AS RORγt MODULATORS AND USES THEREOF
CN103068798A (zh) 2010-09-03 2013-04-24 詹森药业有限公司 作为单酰甘油脂肪酶抑制剂的二-氮杂环丁烷二酰胺
CA2810077A1 (en) 2010-09-27 2012-04-05 Peter J. Connolly Oxopiperazine-azetidine amides and oxodiazepine-azetidine amides as monoacylglycerol lipase inhibitors
CN102417483A (zh) * 2010-09-27 2012-04-18 中国药科大学 作为parp抑制剂的2-苯基-1h-苯并咪唑-4-甲酸酯衍生物
BR112013009828A2 (pt) 2010-10-22 2016-07-26 Janssen Pharmaceutica Nv diamidas de amino-pirrolidina-azetidina como inibidores de monoacilglicerol lipase
JP2013540159A (ja) * 2010-10-22 2013-10-31 ヤンセン ファーマシューティカ エヌ．ベー． モノアシルグリセロールリパーゼ阻害剤としてのピペリジン−４−イル−アゼチジンジアミド
US8513423B2 (en) 2010-10-22 2013-08-20 Janssen Pharmaceutica, Nv Piperidin-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
RU2598842C2 (ru) * 2011-01-20 2016-09-27 Мерк Шарп Энд Домэ Корп. Антагонисты рецептора минералокортикоидов
US9388164B2 (en) 2011-05-03 2016-07-12 Agios Pharmaceuticals, Inc Methods of using pyruvate kinase activators
KR20140068243A (ko) * 2011-09-30 2014-06-05 얀센 파마슈티카 엔.브이. 대사 질환 및 관련 장애의 치료를 위한 모노아실글리세롤 리파제 억제제
MX2014003883A (es) * 2011-09-30 2014-08-27 Janssen Pharmaceutica Nv Inhibidores de monoacilglicerol lipasa para el tratamiento de enfermedades metabolicas y transtornos relacionados.
EP2760861A1 (en) * 2011-09-30 2014-08-06 Janssen Pharmaceutica, N.V. Crystalline hydrochloride salt of (1- (4 -fluorophenyl) - 1h - indol - 5 - yl) - (3- (4- (thiazole - 2 - carbonyl) piperazin- 1 - yl) az etidin- 1 -yl) methanone and its use in the treatment of pain and metabolic disorders
US9487495B2 (en) 2012-01-06 2016-11-08 The Scripts Research Institute Carbamate compounds and of making and using same
CN102603485A (zh) * 2012-02-07 2012-07-25 北京颖新泰康国际贸易有限公司 制备2-甲基-3-苯基苯甲醇的方法
TWI562295B (en) 2012-07-31 2016-12-11 Mediatek Inc Semiconductor package and method for fabricating base for semiconductor package
EA032007B1 (ru) 2012-11-08 2019-03-29 Аджиос Фармасьютикалз, Инк. Терапевтические соединения и композиции и их использование в качестве модуляторов пк-m2
CA2904393A1 (en) * 2013-03-15 2014-09-25 Araxes Pharma Llc Covalent inhibitors of kras g12c
US9745319B2 (en) 2013-03-15 2017-08-29 Araxes Pharma Llc Irreversible covalent inhibitors of the GTPase K-Ras G12C
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
WO2014139144A1 (en) 2013-03-15 2014-09-18 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
EP2999469A1 (de) 2013-05-23 2016-03-30 Bayer Pharma Aktiengesellschaft Pharmazeutische zusammensetzung und deren verwendung sowie anwendungsregime dieser pharmazeutischen zusammensetzung zur bedarfsweisen ( on-demand") kontrazeption
JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
MX2016006052A (es) * 2013-11-12 2016-07-18 Hoffmann La Roche Pirido[4,3-b]pirazin-2-carboxamidas como agentes neurogenicos para el tratamiento de trastornos neurodegenerativos.
EP3087067B1 (en) 2013-12-26 2018-10-24 Takeda Pharmaceutical Company Limited 4-(piperrazin-1-yl)-pyrrolidin-2-one compounds as monoacylglycerol lipase (magl) inhibitors
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
EP3197450A1 (en) * 2014-09-22 2017-08-02 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of fibrosis
JP2017528498A (ja) 2014-09-25 2017-09-28 アラクセス ファーマ エルエルシー Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
JP6653319B2 (ja) * 2015-03-30 2020-02-26 武田薬品工業株式会社 複素環化合物
ES2898765T3 (es) 2015-04-10 2022-03-08 Araxes Pharma Llc Compuestos de quinazolina sustituidos y métodos de uso de los mismos
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
CA3217238A1 (en) 2015-07-20 2017-01-26 Genzyme Corporation Colony stimulating factor-1 receptor (csf-1r) inhibitors
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
UA121775C2 (uk) 2015-07-31 2020-07-27 Пфайзер Інк. 1,1,1-трифтор-3-гідроксипропан-2-ілкарбаматні похідні та 1,1,1-трифтор-4-гідроксибутан-2-ілкарбаматні похідні як інгібітори magl
EP3356347A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058805A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356349A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017070256A2 (en) 2015-10-19 2017-04-27 Araxes Pharma Llc Method for screening inhibitors of ras
KR20180081596A (ko) 2015-11-16 2018-07-16 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017129801A1 (en) 2016-01-27 2017-08-03 Universität Zürich Use of gabaa receptor modulators for treatment of itch
WO2017143283A1 (en) 2016-02-19 2017-08-24 Abide Therapeutics, Inc. Radiolabeled monoacylglycerol lipase occupancy probe
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
WO2017170830A1 (ja) 2016-03-31 2017-10-05 武田薬品工業株式会社 複素環化合物
EA036637B1 (ru) 2016-03-31 2020-12-02 Такеда Фармасьютикал Компани Лимитед Гетероциклические спиросоединения, ингибирующие моноацилглицерин-липазу
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
WO2018064510A1 (en) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3523289A1 (en) 2016-10-07 2019-08-14 Araxes Pharma LLC Heterocyclic compounds as inhibitors of ras and methods of use thereof
JOP20190106A1 (ar) * 2016-11-16 2019-05-09 Lundbeck La Jolla Research Center Inc مثبطات أحادي أسيل جليسرول ليباز (magl)
EP3571191A1 (en) 2017-01-20 2019-11-27 Pfizer Inc 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives as magl inhibitors
EP3571202B1 (en) 2017-01-23 2021-06-30 Pfizer Inc. Heterocyclic spiro compounds as magl inhibitors
WO2018140599A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
US11136308B2 (en) 2017-01-26 2021-10-05 Araxes Pharma Llc Substituted quinazoline and quinazolinone compounds and methods of use thereof
WO2018140513A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer
JP7327802B2 (ja) 2017-01-26 2023-08-16 アラクセス ファーマ エルエルシー 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法
EP3573954A1 (en) 2017-01-26 2019-12-04 Araxes Pharma LLC Fused bicyclic benzoheteroaromatic compounds and methods of use thereof
EA201992409A1 (ru) 2017-05-23 2020-03-23 Лундбекк Ла-Хойя Рисерч Сентер, Инк. Ингибиторы magl на основе пиразола
US10927105B1 (en) 2017-05-23 2021-02-23 Lundbeck La Jolla Research Center, Inc. Pyrazole MAGL inhibitors
CN110869357A (zh) 2017-05-25 2020-03-06 亚瑞克西斯制药公司 化合物及其用于治疗癌症的使用方法
WO2018218069A1 (en) 2017-05-25 2018-11-29 Araxes Pharma Llc Quinazoline derivatives as modulators of mutant kras, hras or nras
US10745385B2 (en) 2017-05-25 2020-08-18 Araxes Pharma Llc Covalent inhibitors of KRAS
MX2020007318A (es) 2017-09-29 2020-08-24 Takeda Pharmaceuticals Co Compuesto heterociclico.
EP3765459A1 (en) 2018-03-13 2021-01-20 Shire Human Genetic Therapies, Inc. Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof
WO2019217307A1 (en) 2018-05-07 2019-11-14 Mirati Therapeutics, Inc. Kras g12c inhibitors
KR20210010475A (ko) 2018-05-15 2021-01-27 룬드벡 라 졸라 리서치 센터 인코포레이티드 Magl 저해제
MX2021000887A (es) 2018-08-01 2021-03-31 Araxes Pharma Llc Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer.
EP3849537B1 (en) 2018-09-10 2024-10-23 Mirati Therapeutics, Inc. Combination therapies
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス， インコーポレイテッド 組み合わせ療法
EP3849535A4 (en) 2018-09-10 2022-06-29 Mirati Therapeutics, Inc. Combination therapies
EA202190749A1 (ru) 2018-09-10 2021-07-09 Мирати Терапьютикс, Инк. Способы комбинированной терапии
CN109020890B (zh) * 2018-09-12 2022-02-08 南京大学 一类饱和脂肪环骈吡唑衍生物的制备及其应用
MY205440A (en) 2018-09-28 2024-10-21 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
KR20210108367A (ko) 2018-11-09 2021-09-02 비바체 테라퓨틱스, 인크. 비시클릭 화합물
AU2019389017B2 (en) * 2018-11-28 2025-01-09 H. Lundbeck A/S Methods of treating disease with MAGL inhibitors
MX2021002804A (es) 2018-12-05 2021-07-15 Mirati Therapeutics Inc Terapias de combinacion.
EP3908283A4 (en) 2019-01-10 2022-10-12 Mirati Therapeutics, Inc. KRAS G12C INHIBITORS
EP3917911A1 (en) * 2019-01-31 2021-12-08 Kyorin Pharmaceutical Co., Ltd. 15-pgdh inhibitors
WO2020179859A1 (ja) 2019-03-06 2020-09-10 第一三共株式会社 ピロロピラゾール誘導体
MX2021012638A (es) 2019-04-16 2022-01-04 Vivace Therapeutics Inc Compuestos biciclicos.
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
EP4031245A1 (en) 2019-09-18 2022-07-27 Takeda Pharmaceutical Company Limited Heteroaryl plasma kallikrein inhibitors
DK4031547T3 (da) 2019-09-18 2024-09-09 Takeda Pharmaceuticals Co Plasmakallikreininhibitorer og anvendelser deraf
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
JP7697934B2 (ja) 2019-09-30 2025-06-24 ヤンセン ファーマシューティカ エヌ．ベー． 放射線標識されたｍｇｌ ｐｅｔリガンド
PH12022551513A1 (en) 2019-12-20 2023-04-24 Mirati Therapeutics Inc Sos1 inhibitors
KR20220146458A (ko) * 2020-01-23 2022-11-01 마이오포르테 테라퓨틱스 인코포레이티드 Pgdh 억제제 및 그의 제조 및 사용 방법
EP3875452A1 (en) * 2020-03-04 2021-09-08 Stichting Het Nederlands Kanker Instituut- Antoni van Leeuwenhoek Ziekenhuis Monoacylglycerol lipase inhibitors
WO2021191391A1 (en) * 2020-03-26 2021-09-30 Janssen Pharmaceutica Nv Aminocyclobutanes as monoacylglycerol lipase modulators
EP4210833A4 (en) 2020-09-11 2024-09-11 Mirati Therapeutics, Inc. CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR
WO2022082009A1 (en) * 2020-10-15 2022-04-21 Epirium Bio Inc. Inhaled formulations of pgdh inhibitors and methods of use thereof
CN117377668A (zh) * 2020-10-15 2024-01-09 迈欧伏特治疗公司 Pgdh抑制剂的吸入制剂及其使用方法
JP2023553492A (ja) 2020-12-15 2023-12-21 ミラティ セラピューティクス， インコーポレイテッド アザキナゾリン汎ＫＲａｓ阻害剤
EP4262803A4 (en) 2020-12-16 2025-03-12 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
JP2024500919A (ja) 2020-12-23 2024-01-10 ジェンザイム・コーポレーション 重水素化コロニー刺激因子－１受容体（ｃｓｆ－１ｒ）阻害剤
KR102682408B1 (ko) * 2021-05-12 2024-07-05 에이치케이이노엔 주식회사 신규한 벤조티아졸 유도체, 이의 제조방법 및 이의 간질환 예방 또는 치료 용도
EP4377314A4 (en) * 2021-07-28 2025-06-18 Epirium Bio Inc. BICYCLIC PGDH INHIBITORS AND METHODS OF PREPARATION AND USE
CA3242372A1 (en) 2021-12-29 2023-07-06 Psy Therapeutics, Inc. Inhibiting monoacylglycerol lipase (magl)

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9600235D0 (en) * 1996-01-05 1996-03-06 Pfizer Ltd Therapeutic agents
EP0968200A1 (en) 1997-02-24 2000-01-05 ZymoGenetics, Inc. Calcitonin mimetics
WO1999019297A1 (en) 1997-10-15 1999-04-22 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
AU3565999A (en) 1999-04-16 2000-11-02 Coelacanth Chemical Corporation Synthesis of azetidine derivatives
US6566356B2 (en) 2000-03-03 2003-05-20 Aventis Pharma S.A. Pharmaceutical compositions containing 3-aminoazetidine derivatives, novel derivatives and their preparation
AR033517A1 (es) 2000-04-08 2003-12-26 Astrazeneca Ab Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos
FR2829028B1 (fr) 2001-08-29 2004-12-17 Aventis Pharma Sa Association d'un antagoniste du recepteur cb1 et d'un produit qui active la neurotransmission dopaminergique dans le cerveau, les compositions pharmaceutiques les contenant et leur utilisation pour le traitement de la maladie de
TW200300757A (en) * 2001-11-16 2003-06-16 Schering Corp Azetidinyl diamines useful as ligands of the nociceptin receptor orl-1
US6995144B2 (en) * 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
JPWO2004002531A1 (ja) * 2002-06-26 2005-10-27 小野薬品工業株式会社 血管の収縮または拡張による疾患治療剤
JP4660199B2 (ja) * 2002-12-23 2011-03-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 置換１−ピペリジン−４−イル−４−アゼチジン−３−イル−ピペラジン誘導体およびそれらのニューロキニン拮抗薬としての使用
FR2854633B1 (fr) * 2003-05-07 2005-06-24 Sanofi Synthelabo Derives de piperidinyl-et piperazinyl-alkylcarbamates, leur preparation et leur application en therapeutique
US20080070924A1 (en) * 2003-06-10 2008-03-20 Frans Eduard Janssens Novel Formulations For Opioid-Based Treatments Of Pain Comprising 1-(1,2-Disubstituted Piperidinyl)-4-Substituted Piperazine Derivatives
EP1702916A1 (en) 2005-03-18 2006-09-20 Santhera Pharmaceuticals (Schweiz) GmbH DPP-IV inhibitors
US20100069346A1 (en) * 2005-06-23 2010-03-18 Sara Holmqvist New Azetidine Derivatives as Neurokinin Receptor Antagonists for the Treatment of Gastrointestinal Diseases
US7879880B2 (en) * 2005-12-21 2011-02-01 Schering Corporation Substituted aniline derivatives useful as histamine H3 antagonists
DE102006016023A1 (de) * 2006-04-05 2007-10-11 Basf Ag Funktionale Expression von Triacylglycerol-Lipasen
US8119676B2 (en) 2006-08-26 2012-02-21 Abbott GmbH & Co. HG Substituted benzimidazolone derivatives, medicaments comprising them and their use
FR2915197B1 (fr) * 2007-04-18 2009-06-12 Sanofi Aventis Sa Derives de triazolopyridine-carboxamides, leur preparation et leur application therapeutique.
FR2915199B1 (fr) * 2007-04-18 2010-01-22 Sanofi Aventis Derives de triazolopyridine-carboxamides et triazolopyrimidine-carboxamides, leur preparation et leur application en therapeutique.
FR2915198B1 (fr) 2007-04-18 2009-12-18 Sanofi Aventis Derives de triazolopyridine-carboxamides et triazolopyridine -carboxamides, leur preparation et leur application en therapeutique.
WO2009117444A1 (en) 2008-03-17 2009-09-24 Northeastern University Inhibitors of fatty acid amide hydrolase and monoacylglycerol lipase for modulation of cannabinoid receptors
JP5715945B2 (ja) 2008-04-25 2015-05-13 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプＪａｎｓｓｅｎ Ｐｈａｒｍａｃｅｕｔｉｃａ Ｎａａｍｌｏｚｅ Ｖｅｎｎｏｏｔｓｃｈａｐ モノアシルグリセロールリパーゼ（ｍｇｌｌ）の結晶構造
EP2180048B1 (en) 2008-10-09 2014-12-17 Janssen Pharmaceutica N.V. Alternative crystal form of monoacylglycerol lipase (MGLL)
JP2012524800A (ja) 2009-04-22 2012-10-18 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ モノアシルグリセロールリパーゼ阻害剤としてのアゼチジニルジアミド
DK2421852T3 (da) 2009-04-22 2014-08-18 Janssen Pharmaceutica Nv Heteroaromatiske og aromatiske piperazinylazetidinylamider som monoacylglycerollipaseinhibitor
US8415341B2 (en) 2009-04-22 2013-04-09 Janssen Pharmaceutica, Nv Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors
DE102012109699A1 (de) * 2012-10-11 2014-04-17 Pavel Abdulkin Verfahren zum Bereitstellen einer Gold-Nano-Hülle um kleine, magnetische Partikel im Submikrometerbereich und so erhaltene Partikel

Also Published As

Publication number Publication date
RU2011147233A (ru) 2013-05-27
CA2759713A1 (en) 2010-10-28
US20130244997A1 (en) 2013-09-19
US20130102585A1 (en) 2013-04-25
IL215781A0 (en) 2012-01-31
JP2012524802A (ja) 2012-10-18
TW201116280A (en) 2011-05-16
KR20120034617A (ko) 2012-04-12
RU2011147230A (ru) 2013-05-27
US8399454B2 (en) 2013-03-19
US8697683B2 (en) 2014-04-15
AU2010238732B2 (en) 2015-06-11
CN102548982A (zh) 2012-07-04
US8697684B2 (en) 2014-04-15
AU2010238740A1 (en) 2011-11-10
TW201105654A (en) 2011-02-16
US20130217669A1 (en) 2013-08-22
EP2421825A1 (en) 2012-02-29
RU2011147206A (ru) 2013-05-27
IL215798A0 (en) 2012-01-31
BRPI1014281A2 (pt) 2019-09-24
AU2016201405A1 (en) 2016-03-24
BRPI1013545A2 (pt) 2019-09-24
IL215775A0 (en) 2012-01-31
AU2010238738A1 (en) 2011-11-10
EP2421825B9 (en) 2014-08-20
KR20120034623A (ko) 2012-04-12
RU2011147207A (ru) 2013-05-27
WO2010124112A1 (en) 2010-10-28
CA2759505A1 (en) 2010-10-28
US20130237517A1 (en) 2013-09-12
SI2421825T1 (sl) 2014-04-30
US8450303B2 (en) 2013-05-28
JP2012524801A (ja) 2012-10-18
US8962607B2 (en) 2015-02-24
US20100331299A1 (en) 2010-12-30
WO2010124116A1 (en) 2010-10-28
BRPI1014885A8 (pt) 2018-04-10
AU2010239188A1 (en) 2011-11-10
ES2455744T3 (es) 2014-04-16
JP2012524807A (ja) 2012-10-18
BRPI1013540A2 (pt) 2020-11-17
US20110015171A1 (en) 2011-01-20
WO2010124086A1 (en) 2010-10-28
IL215773A (en) 2015-05-31
EP2421847A1 (en) 2012-02-29
CN102803210A (zh) 2012-11-28
US20130123232A1 (en) 2013-05-16
WO2010124082A1 (en) 2010-10-28
TW201103918A (en) 2011-02-01
TWI483940B (zh) 2015-05-11
US8426401B2 (en) 2013-04-23
AU2010238736A1 (en) 2011-11-10
TWI465446B (zh) 2014-12-21
AU2010239204A1 (en) 2011-11-10
CN102459255A (zh) 2012-05-16
CN102459166B (zh) 2015-03-25
CA2759547A1 (en) 2010-10-28
US20100324011A1 (en) 2010-12-23
US20130123233A1 (en) 2013-05-16
CA2759614C (en) 2017-09-19
US20130137674A1 (en) 2013-05-30
JP2012524803A (ja) 2012-10-18
IL215785A0 (en) 2012-01-31
US8623858B2 (en) 2014-01-07
WO2010124102A1 (en) 2010-10-28
IL215786A0 (en) 2012-01-31
AR076382A1 (es) 2011-06-08
AR076380A1 (es) 2011-06-08
CA2759697A1 (en) 2010-10-28
AR076381A1 (es) 2011-06-08
RU2549547C2 (ru) 2015-04-27
US8604017B2 (en) 2013-12-10
KR20110137831A (ko) 2011-12-23
WO2010124114A1 (en) 2010-10-28
BRPI1015238A2 (pt) 2019-09-24
CA2759604A1 (en) 2010-10-28
AR076374A1 (es) 2011-06-08
US20140243305A1 (en) 2014-08-28
EP2421851A1 (en) 2012-02-29
CA2759621C (en) 2017-09-26
US8362001B2 (en) 2013-01-29
IL215787A0 (en) 2012-01-31
US8445477B2 (en) 2013-05-21
JP5733840B2 (ja) 2015-06-10
CA2759621A1 (en) 2010-10-28
JP2012524804A (ja) 2012-10-18
EP2421848A1 (en) 2012-02-29
ES2538326T3 (es) 2015-06-19
US20110015170A1 (en) 2011-01-20
WO2010124119A1 (en) 2010-10-28
TW201103932A (en) 2011-02-01
AR076378A1 (es) 2011-06-08
TW201103930A (en) 2011-02-01
CN102459230A (zh) 2012-05-16
EP2421823B1 (en) 2015-01-14
KR20120034615A (ko) 2012-04-12
RS53235B (sr) 2014-08-29
AR076379A1 (es) 2011-06-08
WO2010124108A1 (en) 2010-10-28
US8367653B2 (en) 2013-02-05
HRP20140295T1 (hr) 2014-04-25
EP2421824A1 (en) 2012-02-29
HK1170228A1 (en) 2013-02-22
JP5649644B2 (ja) 2015-01-07
US8691805B2 (en) 2014-04-08
AU2010239184A1 (en) 2011-11-10
RU2011147236A (ru) 2013-05-27
RU2569298C2 (ru) 2015-11-20
EP2421860A1 (en) 2012-02-29
BRPI1014885A2 (pt) 2016-04-19
IL215773A0 (en) 2012-01-31
RU2011147200A (ru) 2013-05-27
DK2421825T3 (da) 2014-02-03
US8722658B2 (en) 2014-05-13
AU2010239188B2 (en) 2016-03-31
KR101705049B1 (ko) 2017-02-09
CN102459240A (zh) 2012-05-16
CN102459228A (zh) 2012-05-16
JP2012524806A (ja) 2012-10-18
AU2010238743A1 (en) 2011-11-10
KR20120034622A (ko) 2012-04-12
RU2011147185A (ru) 2013-05-27
US8741887B2 (en) 2014-06-03
KR20120035146A (ko) 2012-04-13
RU2011147181A (ru) 2013-05-27
US20100324012A1 (en) 2010-12-23
CN102459167A (zh) 2012-05-16
TW201105665A (en) 2011-02-16
AR076377A1 (es) 2011-06-08
SMT201400034B (it) 2014-05-07
HK1170221A1 (en) 2013-02-22
US8362000B2 (en) 2013-01-29
EP2421856A1 (en) 2012-02-29
JP2012524805A (ja) 2012-10-18
CA2759501A1 (en) 2010-10-28
EP2421823A1 (en) 2012-02-29
EP2421825B1 (en) 2014-01-01
CA2759614A1 (en) 2010-10-28
AU2010238732A1 (en) 2011-11-10
CN102459166A (zh) 2012-05-16
BRPI1014284A2 (pt) 2017-10-10
US20100324013A1 (en) 2010-12-23
IL215780A0 (en) 2012-01-31
KR20120034616A (ko) 2012-04-12
BRPI1014876A2 (pt) 2016-04-12
KR20110137834A (ko) 2011-12-23
PT2421825E (pt) 2014-03-13
JP2012524800A (ja) 2012-10-18
CN102459167B (zh) 2015-04-01
US8455476B2 (en) 2013-06-04
TW201103931A (en) 2011-02-01
AR076376A1 (es) 2011-06-08
US20100324014A1 (en) 2010-12-23
TW201105655A (en) 2011-02-16
KR101705697B1 (ko) 2017-02-10
IL215780A (en) 2015-05-31
BRPI1013538A2 (pt) 2019-09-24
US20100331300A1 (en) 2010-12-30

Similar Documents

Publication Publication Date Title
IL215775A0 (en) Azetidinyl diamides as monoacylglycerol lipase inhibitors
IL225769A0 (en) Piperidine-4-yl-azetidine diamides as monoacylglycerol lipase inhibitors
IL225815A0 (en) Amino-pyrrolidine-azetidine diamides as monoacylglycerol lipase inhibitors
GB201004179D0 (en) Enzyme inhibitors
GB201004178D0 (en) Enzyme inhibitors
GB201007384D0 (en) Enzymes
GB0905611D0 (en) Bioreactor
IL215796A0 (en) Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors
IL215797A0 (en) Heteroaromatic and aromatic piperazinyl azetidinyl amides as monoacylglycerol lipase inhibitors
EP2400840A4 (en) LIQUID STATINE FORMULATIONS
ZA201206517B (en) Acetaminophen composition
EP2635287A4 (en) NEDD8 ACTIVATOR ENZYME INHIBITOR ADMINISTRATION
EP2542232A4 (en) FATTY ACID INHIBITORS
GB201105987D0 (en) Enzymes
GB0908068D0 (en) Enzyme inhibitors
GB0901616D0 (en) Enzyme inhibitors
GB201004309D0 (en) New enzyme inhibitors
GB0906304D0 (en) Culture
GB0906303D0 (en) Culture
GB0906302D0 (en) Culture
GB0906307D0 (en) Culture
GB0906306D0 (en) Culture
GB0906308D0 (en) Culture
GB0906311D0 (en) Culture
GB0906301D0 (en) Culture