90531-98-9Relevant academic research and scientific papers
Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865)
Owen, Robert M.,Blakemore, David,Cao, Lishuang,Flanagan, Neil,Fish, Rebecca,Gibson, Karl R.,Gurrell, Rachel,Huh, Chan Woo,Kammonen, Juha,Mortimer-Cassen, Elisabeth,Nickolls, Sarah A.,Omoto, Kiyoyuki,Owen, Dafydd,Pike, Andy,Pryde, David C.,Reynolds, David S.,Roeloffs, Rosemarie,Rose, Colin,Stead, Clara,Takeuchi, Mifune,Warmus, Joseph S.,Watson, Christine
, p. 5773 - 5796 (2019/05/15)
The design, optimization, and evaluation of a series of novel imidazopyridazine-based subtype-selective positive allosteric modulators (PAMs) for the GABAA ligand-gated ion channel are described. From a set of initial hits multiple subseries were designed and evaluated based on binding affinity and functional activity. As designing in the desired level of functional selectivity proved difficult, a probability-based assessment was performed to focus the project's efforts on a single subseries that had the greatest odds of delivering the target profile. These efforts ultimately led to the identification of two precandidates from this subseries, which were advanced to preclinical safety studies and subsequently to the identification of the clinical candidate PF-06372865.
CONDENSED-RING PYRIMIDYLAMINO DERIVATIVE, PREPARATION METHOD THEREFOR, AND INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND APPLICATIONS THEREOF
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, (2018/03/25)
Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b' to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.
FUSED RING PYRIMIDINE COMPOUND, INTERMEDIATE, AND PREPARATION METHOD, COMPOSITION AND USE THEREOF
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, (2018/08/12)
Disclosed area fused ring pyrimidine compound, and an intermediate, a preparation method, a composition and a use thereof. The fused ring pyrimidine compound is a compound as shown in formula I, a tautomer, an enantiomer, a diastereoisomer, a pharmaceutically acceptable salt, a metabolite, a metabolic precursor or a prodrug thereof, wherein the above-mentioned compound is used for the preparation of a medicine for preventing, remitting or treating one or more of immune system diseases, autoimmune diseases, cell proliferative diseases, allergic disorders and cardiovascular diseases, and the compound has a strong inhibitory effect on the Janues kinase, FGFR kinase, FLT3 kinase and Src family kinase.
Synthesis of functionalized arenes
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Paragraph 0067; 0068; 0069; 0070, (2015/04/22)
The present invention relates to methods of preparing (cyclo)alkoxy-((cyclo)alkylsulfanyl)benzenes, (cyclo)alkoxy-((cyclo)alkylsulfinyl)benzenes and (cyclo)alkoxy-((cyclo)alkylsulfonyl)benzenes of general formula (I): as well as to intermediate compounds useful in the preparation of said compounds.
METHOD FOR PREPARING SUBSTITUTED TRIAZOLOPYRIDINES
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Paragraph 0362-0364, (2015/06/03)
The present invention relates to methods of preparing substituted triazolopyridine compounds of general formula (I) as described and defined herein, as well as to intermediate compounds useful in the preparation of said compounds.
Chemical Compounds
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, (2014/06/25)
The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.
METHOD FOR PREPARING SUBSTITUTED TRIAZOLOPYRIDINES
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Page/Page column 75, (2014/02/15)
The present invention relates to methods o f preparing substituted triazolopyridine compounds of general formula (I) as described and defined herein, as well as to intermediate compounds useful in the preparation of said compounds.
SUBSTITUTED TRIAZOLOPYRIDINES HAVING ACTIVITY AS MPS-1 INHIBITORS
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Page/Page column 101-102, (2015/01/06)
The present invention relates to substituted triazolopyridine compounds of general formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
NOVEL COMPOUNDS FOR THE TREATMENT OF CANCER
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Page/Page column 97; 98, (2015/01/09)
The present invention relates to novel compounds showing an inhibitory effect on Mps-1 kinase, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
PRODRUG DERIVATIVES OF SUBSTITUTED TRIAZOLOPYRIDINES
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Page/Page column 72, (2015/01/09)
The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.
