- Inverse electron demand Diels-Alder reactions of 3,6-dichloro- [1,2,4,5]tetrazine
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3,6-Dichloro-[1,2,4,5]tetrazine has been found to act as an efficient azadiene equivalent in inverse electron demand [4+2] cyclisations with a range of alkenes and alkynes, allowing rapid access to a range of highly functionalised pyridazines.
- Sparey, Tim J.,Harrison, Timothy
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- THRB RECEPTOR AGONIST COMPOUND AND PREPARATION METHOD AND USE THEREOF
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The present invention discloses a compound represented by the following Formula (I) and a pharmaceutically acceptable salt thereof. The compound improves the THRα selectivity while maintaining good THRβ agonistic activity, thereby improving properties of
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Paragraph 0090; 0093
(2020/07/07)
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- NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF FIBROSIS
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The present invention discloses compounds according to Formula (I) Wherein R1, R2, L, A1, A2, A3, Cy and the subscript n are as defined herein. The present invention relates to antagonists compounds of sphingosine 1-phosphate (SIP) receptor, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, inflammatory diseases, respiratory diseases, autoimmune diseases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering the compound of the invention.
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Paragraph 0269
(2019/01/21)
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- TRICYCLIC COMPOUNDS FOR USE AS KINASE INHIBITORS
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There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceuticagy-acceptable esters, amides solvates or salts
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Page/Page column 71
(2011/07/30)
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- Organic Compounds as Smo Inhibitors
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The present invention relates generally to novel compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders. The present invention includes novel compounds, novel compositions, methods of their use and methods of their manufacture, where such compounds are generally pharmacologically useful as agents in therapies whose mechanism of action involve methods of inhibiting tumorigenesis, tumor growth and tumor survival using agents that inhibit the Hedgehog and Smo signaling pathway.
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Page/Page column 42
(2010/03/04)
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- ORGANIC COMPOUNDS AND THEIR USES
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The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula (I).
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Page/Page column 104
(2008/12/07)
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- Aurora kinase modulators and method of use
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The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R1- are defined herein, and synthetic intermediates, which
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Page/Page column 24
(2008/06/13)
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- 3-ARYL-5,6-DISUBSTITUTED PYRIDAZINES
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The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions.
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Page/Page column 58
(2010/02/15)
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- TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF USEFUL IN THE TREATMENT OF NEUROPATHIC PAIN
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The present invention is directed to a method of use of triazolo-pyridazine compounds in the treatment of neuropathic pain. The present invention is also directed to the use of triazolo-pyridazine compounds in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson’s disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders - such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal and other diseases. The present invention is also directed to novel triazolo-pyridazine compounds that selectively bind to α2δ-1 subunit of Ca channels.
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Page/Page column 69
(2010/02/11)
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- Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro- (7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABAAα5 benzodiazepine binding site
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The identification of a novel series of 7,8,9,10-tetrahydro-(7,10-ethano)- 1,2,4-triazolo[3,4-a]phthalazines as GABAAα5 inverse agonists, which have both binding and functional (efficacy) selectivity for the benzodiazepine binding site of α5- over α1-, α2-, and α3-containing GABAA receptor subtypes, is described. Binding selectivity was determined to a large part by the degree of planarity of the fused ring system whereas functional selectivity was dependent on the nature of the heterocycle at the 3-position of the triazolopyridazine ring. 3-Furan and 5-methylisoxazole were shown to be optimal for GABAAα5 functional selectvity. 3-(5-Methylisoxazol-3-yl)-6-(2-pyridyl)methyloxy-1,2,4- triazolo[3,4-a]phthalazine (43) was identified as a full inverse agonist at the GABAAα5 subtype with functional selectivity over the other GABAA receptor subtypes and good oral bioavailability.
- Street, Leslie J.,Sternfeld, Francine,Jelley, Richard A.,Reeve, Austin J.,Carling, Robert W.,Moore, Kevin W.,McKernan, Ruth M.,Sohal, Bindi,Cook, Susan,Pike, Andrew,Dawson, Gerard R.,Bromidge, Frances A.,Wafford, Keith A.,Seabrook, Guy R.,Thompson, Sally A.,Marshall, George,Pillai, Goplan V.,Castro, José L.,Atack, John R.,MacLeod, Angus M.
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p. 3642 - 3657
(2007/10/03)
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- NOVEL ALLYLTHIOPYRIDAZINE DERIVATIVES AND PROCESS FOR PREPARING THE SAME
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The, present invention relates to a novel allylthiopyridazine derivative represented by formula (I) which exhibits a superior effect for prevention and treatment or hepatic diseases induced by toxic substances and for protection of human tissues from radi
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- Substituted triazolo-pyridazine derivatives as ligands for GABA receptors
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Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the α2 and/or α3 subunits.
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- Allylthiopyridazine derivatives and process for preparing the same
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The, present invention relates to a novel allylthiopyridazine derivative represented by formula (I) which exhibits a superior effect for prevention and treatment or hepatic diseases induced by toxic substances and for protection of human tissues from radi
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