26096-30-0Relevant articles and documents
1-azaspirocycle compound, and preparation method and applications thereof
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, (2018/09/14)
The invention discloses a 1-azaspirocycle compound, and preparation method and applications thereof, and belongs to the field of pharmaceutical chemistry. The 1-azaspirocycle compound with a structurerepresented by formula I, or a pharmaceutically acceptable salt or a stereisomer or a solvate or a prodrug thereof is capable of realzing combination with Autotaxin, can be taken as an Autotaxin inhibitor, and can be used for prevention and treatment of diseases with Autotaxin expression increasing pathological characteristics such as cancer and fibrosis diseases especially pulmonary fibrosis andhepatic fibrosis, metabolic diseases, myelodysplastic syndrome, cardiovascular diseases, autoimmune diseases, inflammation, neurological diseasses, or pain. Compared with single component inhibitors,the 1-azaspirocycle compound and the derivatives possesses following advantages: blocking and interfacing at the upsteam of a plurality of key signal channels are realized, tumor cell growth and transfer are relieved or dalyed, early caused drug resistance is avoided, and novel means are provided for treatment of tumor cells.
FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Paragraph 0576; 0580; 0581, (2018/06/26)
The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton’ s tyrosine kinase (Btk), and for treating disorders mediated thereby.
FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Paragraph 0576; 0580; 0581, (2014/11/13)
The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
Azetidine based transition state analogue inhibitors of N-ribosyl hydrolases and phosphorylases
Evans, Gary B.,Furneaux, Richard H.,Greatrex, Ben,Murkin, Andrew S.,Schramm, Vern L.,Tyler, Peter C.
, p. 948 - 956 (2008/09/19)
N-Ribosyl phosphorylases and hydrolases catalyze nucleophilic displacement reactions by migration of the cationic ribooxacarbenium carbon from the fixed purine to phosphate and water nucleophiles, respectively. As the lysis reaction progresses along the r
AZETIDINE ANALOGUES OF NUCLEOSIDASE AND PHOSPHORYLASE INHIBITORS
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Page/Page column 15-16, (2008/12/07)
Azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors having the general formula (I), the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds wherein W and X are each independently selected from hydrogen, CH2OH, CH2OQ and CH2SQ; Y and Z are each independently selected from hydrogen, halogen, CH2OH, CH2OQ, CH2SQ, SQ, OQ and Q; Q is an alkyl, aralkyl or aryl group each of which may be optionally substituted with one or more substituents selected from hydroxy, halogen, methoxy, amino, or carboxy; R1 is a radical of the formula (II) or R1 is a radical of the formula (III) A is selected from N, CH and CR2, where R2 is selected from halogen, alkyl, aralkyl, aryl, OH, NH2, NHR3, NR3R4 and SR5, where R3, R4 and R5 are each alkyl, aralkyl or aryl groups optionally substituted with hydroxy or halogen, and where R2 is optionally substituted with hydroxy or halogen when R2 is alkyl, aralkyl or aryl; B is selected from hydroxy, NH2, NHR6, SH, hydrogen and halogen, where R6 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; D is selected from hydroxy, NH2, NHR7, hydrogen, halogen and SCH3, where R7 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; E is selected from N and CH; G is a C1-4 saturated or unsaturated alkyl group optionally substituted with hydroxy or halogen, or G is absent; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof.
Synthesis of novel 2,6-diazaspiro[3.3]heptanes
Hamza, Daniel,Stocks, Michael J.,Décor, Anne,Pairaudeau, Garry,Stonehouse, Jeffrey P.
, p. 2584 - 2586 (2008/02/13)
A practical route to 2,6-diazaspiro[3.3]heptanes is described by way of reductive amination of a readily available aldehyde with primary amines or anilines. Cyclisation proceeds in high yield and the methods reported are amenable to either library or larg
Process for preparing azetidine derivatives and intermediates thereof
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, (2008/06/13)
The invention provides a process for preparing azetidine-3-carboxylic acid or salts thereof; useful as chemical hybridizing agents, which comprises treating a compound of the formula STR1 wherein R represents a hydrogen atom or a group of formula R1 R2 CH-- wherein R1 and R2 are independently selected from hydrogen, alkyl or optionally substituted phenyl moieties, with nitric acid and subjecting the resulting initial product to acid conditions to produce an acid-addition salt of azetidine-3-carboxylic acid, and thereafter, if desired, converting the acid-addition salt to the free acid or another salt of the acid, 1-nitrosoazetidine-3,3-dicarboxylic acid, 1-nitrosoazetidine-3-carboxylic acid and salts thereof being intermediates in the process.
