937046-95-2Relevant academic research and scientific papers
Preparation method 7-bromopyrrolo [2,1-f][1, 2, 4]-thiazine -4- amine (by machine translation)
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Paragraph 0017-0023, (2020/03/12)
[, ] The preparation method 7 - of [2,1 - f][1, 2, 4]-(, amino - ((((((((aopipelineao :1) aminopyrrolo 2,5 - thiopyrrole I,) obtained by reacting the intermediate 1 - Boc - 1 - with the formamidine in the following step ;2) can obtain the intermediate I (II, amino-(EC 1 - Boc - 1 -) to obtain the intermediate ;3), namely, II amino-(III, aminopyrrolopyrrole - 2 2-methanonitrile hydrochloride 1 -) to form the intermediate ;4) through the reaction of the intermediates III and the bromination reagent to obtain a final product IV, of the present invention. in an acidic condition and reacting the intermediate body with the bromination reagent. to obtain a final product (4 -aminopyrrolopyridine - 4 4) intermediate, [2,1 - f][1, 2, 4] [2,1 - f][1, 2, 4] obtained by the reaction of the intermediate body with the. bromination reagent and ;5) amino- pyrrolidine. IV-amine,aminopyrroyl hydrochloride 7 . (by machine translation)
THE MONOHYDRATE OF ROGARATINIB HYDROCHLORIDE AND SOLID STATES THEREOF
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Page/Page column 29; 48, (2020/08/22)
Compound (III) which is the crystalline form of [4-{[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methyl-l-benzothiophen-2-yl)pyrrolo[2, -f] [ 1,2,4]triazin-7-yl]methyl}piperazin-2-one hydrochloride] which is the monohydrate, processes for its preparation, pharmaceutical compositions comprising it and its use in the control of disorders, including cancer.
CDK kinase inhibitors
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Paragraph 0112-0115, (2020/12/30)
The invention discloses a compound with the general formula (I) and a salt thereof, wherein the compound can be taken as inhibitors of CDK kinase, particularly CDK4/6 kinase, and all variables are defined in the invention. The compound can be used for treating or preventing diseases such as cancer. The present application also relates to pharmaceutical compositions comprising the compound of formula (I).
6-bromo-3H-pyrrolo(2,1-f)(1,2,4)triazine-4-ketone preparation method
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Paragraph 0012; 0035; 0036, (2019/02/06)
The invention belongs to the technical field of medicine and specifically relates to a 6-bromo-3H-pyrrolo(2,1-f)(1,2,4)triazine-4-ketone preparation method. The method comprises the following steps: reacting 2,5-dimethoxy tetrahydrofuran with tert-butylcarbazate to obtain compound IV; then reacting with trichloro-acetic chloride to obtain compound V; bromizing to obtain compound Vi; performing esterification reaction to obtain compound VII; finally, cyclizing to obtain 6-bromo-3H-pyrrolo(2,1-f)(1,2,4)triazine-4-ketone. Compared with the prior art, the preparation method disclosed by the invention greatly improves the yield and the purity of 6-bromo-3H-pyrrolo(2,1-f)(1,2,4)triazine-4-ketone, reduces production cost and has good application value.
Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor
Collin, Marie-Pierre,Lobell, Mario,Hübsch, Walter,Brohm, Dirk,Schirok, Hartmut,Jautelat, Rolf,Lustig, Klemens,B?mer, Ulf,V?hringer, Verena,Héroult, Mélanie,Grünewald, Sylvia,Hess-Stumpp, Holger
, p. 437 - 445 (2018/02/21)
Rogaratinib (BAY 1163877) is a highly potent and selective small-molecule pan-fibroblast growth factor receptor (FGFR) inhibitor (FGFR1–4) for oral application currently being investigated in phase 1 clinical trials for the treatment of cancer. In this publication, we report its discovery by de novo structure-based design and medicinal chemistry optimization together with its pharmacokinetic profile.
NEW CRTH2 ANTAGONISTS
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Page/Page column 147-148, (2013/03/26)
The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS
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Page/Page column 129; 130; 131, (2013/03/28)
The invention provides compounds of formula I: (I) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing com-pounds of formula I, intermediates useful for preparing com-pounds of formula I and therapeutic methods for suppressing an immune response or treating cancer, including a hematologic malignancy, using compounds of formula I
HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS
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Page/Page column 84-85, (2011/12/14)
The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.
Discovery and process synthesis of novel 2,7-pyrrolo[2,1- f ][1,2,4]triazines
Thieu, Tho,Sclafani, Joseph A.,Levy, Daniel V.,McLean, Andrew,Breslin, Henry J.,Ott, Gregory R.,Bakale, Roger P.,Dorsey, Bruce D.
supporting information; experimental part, p. 4204 - 4207 (2011/10/04)
The synthesis of a new kinase inhibitor template 2-anilino-7-aryl- pyrrolo[2,1-f][1,2,4]triazine is described which includes a late stage orthogonally reactive key intermediate amenable to rapid diversification as well an optimized in situ triflate displa
THERAPEUTIC AGENTS
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Page/Page column 29; 33, (2010/04/03)
The invention provides a compound of formula (I): wherein R1, and W have any of the values defined in the application; or a salt thereof. The compounds and salts thereof have beneficial therapeutic properties (e.g. immunosuppressant properties).
