879608-91-0Relevant academic research and scientific papers
Trisubstituted pyrimidines as transient receptor potential vanilloid 1 (TRPV1) antagonists with improved solubility
Wang, Xianghong,Chakrabarti, Partha P.,Ognyanov, Vassil I.,Pettus, Liping H.,Tamir, Rami,Tan, Helming,Tang, Phi,Treanor, James J.S.,Gavva, Narender R.,Norman, Mark H.
, p. 6539 - 6545 (2007)
A series of trisubstituted pyrimidines were synthesized to improve aqueous solubility of our first TRPV1 clinical candidate (1; AMG 517), while maintaining potent TRPV1 inhibitory activity. Structure-activity and structure-solubility studies led to the id
AMINOPYRIMIDINE DERIVATIVES AND THEIR USE AS ARYL HYDROCARBON RECEPTOR MODULATORS
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Paragraph 1764-1770, (2021/10/02)
The present invention relates to novel compounds effective as modulators Aryl hydrocarbon receptor (AhR), pharmaceutical composition comprising the compounds for the modulation of AhR, or prevention or treatment of a disease, disorder, or condition associ
ACETYLCHOLINE BINDING PROTEIN LIGANDS, COOPERATIVE NACHR MODULATORS AND METHODS FOR MAKING AND USING
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Page/Page column 86-87, (2015/05/26)
The invention provides compositions and methods a) for increasing or stimulating the release of other transmitters (excitatory amino acids, inhibitor amino acids and biogenic amines) in the central nervous system (CNS) or the brain, or modulating, decreas
Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists
Tamayo, Nuria,Liao, Hongyu,Stec, Markian M.,Wang, Xianghong,Chakrabarti, Partha,Retz, Dan,Doherty, Elizabeth M.,Surapaneni, Sekhar,Tamir, Rami,Bannon, Anthony W.,Gavva, Narender R.,Norman, Mark H.
, p. 2744 - 2757 (2008/12/22)
Transient receptor potential vanilloid 1 (TRPV1) channel antagonists may have clinical utility for the treatment of chronic nociceptive and neuropathic pain. We recently advanced a TRPV1 antagonist, 3 (AMG 517), into clinical trials as a new therapy for t
Vanilloid receptor ligands and their use in treatments
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Page/Page column 22-23, (2010/10/20)
Substituted pyridines and pyrimidines and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
Vanilloid receptor ligands and their use in treatments
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Page/Page column 49, (2010/11/24)
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
